Table of Contents     Library of Abstracts

 

 

LIBRARY OF ABSTRACTS OF PEER-REVIEWED PROFESSIONAL JOURNAL ARTICLES ON LESSER GALANGAL, WITH INTRODUCTION AND EDITORIAL COMMENTARY


This site provides a comprehensive and balanced overview of scientific research on lesser galangal.  It is extensively referenced for those wishing to pursue further inquiries and study.  It is not intended to provide medical advice or to substitute for the services of a qualified health care professional.  Responsibility is specifically disclaimed for consequences incurred by those using the information reported.


INTRODUCTION 

Lesser galangal (Alpinia officinarum, Hance) is one of a number of herbal plant species that has been and continues to be extensively studied.  The plant has many consistently identifiable active compounds.  By and large, the studies focus on one or more such compounds.     

The following bullet points summarize the effects attributable to compounds found in lesser galangal.  They are listed in the same sequence as documented by the articles abstracted below. 

•   Anti-Inflammatory

•   Antioxidant

•   Tumor Suppressive/Cancer preventive

  • Apoptosis
  • Enhancing anti cancer drug efficacy
  • Effect on Fatty Acid Synthase
  • Binds Adenosine receptors
  • Free radical scavenging
  • Chemoprotection prevents genotoxicity
  • COX-2 Inhibition

•   Anti-atherogenic (preventive against atherosclerosis)

  • Diminishes lipid peroxidation and free radical formation

o       Scavenges free radicals

o       Lowers cholesterol and triglycerides

  • Inhibits the inflammatory component of plaque formation

•   Antibiotic/antiviral/antiparasitic/antifungal

•   Antiemetic

•   May enhance cancer drug efficacy by reducing tumor resistance

•   Long history in folk medicine world wide 

Following are the active chemical compounds identified in lesser galangal to date: 

Major Compounds: beta-Sitosterol (I), Galangin (II), Emodin (III) and            Quercetin (IV)

Seven phenylpropanoids:

1,7-diphenyl-5-ol-3-heptone, 1-phenyl-7-(3'-methoxyl-4'-hydroxyl) phenyl-5-ol- 3-heptone, glandin, kaempferol-4'-methylether and 3,4-dihydroxylbenzoic acid

Five diarylheptanoids: 1,7-diphenylhept-4-en-3-one, dihydroyashabushiketol             (1,7-diphenyl-5-hydroxy-3-heptanone), 5-hydroxy-7-(4"-hydroxy-3"-methoxyphenyl)-1-phenyl-3-heptanone and 5-hydroxy-7-(4"-hydroxyphenyl)-1-phenyl-3-heptanone; 5TH diarylheptanoid:7-(4'-hydroxy-3'-methoxyphenyl)-1-  phenylhept-4-en-3-one (HMP)

Nine glycosides (1-9):  three known glycosides, (1R,3S,4S)-trans-3-hydroxy-1,8-cineole beta-D-glucopyranoside (1), benzyl beta-D-glucopyranoside (3), and 1-O-beta-D-glucopyranosyl-4-allylbenzene (chavicol beta-D-glucopyranoside, 4); and the six novel glycosides, 3-methyl-but-2-en-1-yl beta-D-glucopyranoside (2), 1-hydroxy-2-O-beta-D-glucopyranosyl-4-allylbenzene (5), 1-O-beta-D- glucopyranosyl-2-hydroxy-4-allylbenzene (demethyleugenol beta-D-glucopyranoside, 6), 1-O-(6-O-alpha-L-rhamnopyranosyl-beta-D-glucopyranosyl)-2-hydroxy-4-allylbenzene (demethyleugenol beta-rutinoside, 7), 1-O-(6-O-alpha-L-rhamnopyranosyl-beta-D-glucopyranosyl)-4-allylbenzene (chavicol beta-rutinoside, 8), and 1,2-di-O-beta-D-glucopyranosyl-4-allylbenzene (9) 


NARRATIVE 

Anti-inflammatory 

Many of the abstracts in the library focus on how Lesser Galangal ingredients work to prevent or stop inflammation.  Inflammation is a very important part of many diseases of aging, immune dysfunction, autoimmune disease, cancer, and coronary artery disease.

Inflammation is a biochemical/physiological response to injury.  No matter what the site of injury is and what the stimulating factor of injury is, inflammation follows certain fixed genetically controlled, biochemically induced reactions that lead to the same biochemical and physiological consequences.  From the list of active compounds above, the Diarylheptanoids have been most heavily studied and have the most well defined mechanisms of action.  Three abstracts defining these mechanisms have been included for detailed examination. 

Some chemicals created as a result of injury are called proinflammatory mediators of inflammation.  Some examples in these studies are called prostaglandins, leukotrienes, nitric oxide, and proinflammatory cytokines like interleukin-1 beta and tumor necrosis factor alpha.   

Specific genes which activate production of certain enzymes are also involved.  The diarylheptanoids have been shown to block the production of proinflammatory cytokines and the activation of these gene mediated signaling pathways that generate enzymes that in turn create the inflammation.  The abstracts chosen to illustrate these points all demonstrate that lesser galangal’s active ingredients block inflammation. 

Inflammation is a subtle cause of hardening of the arteries or atherosclerosis.  So overlapping evidence of anti-inflammatory efficacy impacts upon one of the ways in which lesser galangal inhibits atherogenesis (follow the bullet link above to anti-atherogenic).  Lipid peroxidation products cause the cox-2 enzymes to activate an inflammatory response that causes these peroxidation products to be incorporated into inflammatory white blood cells (foamy monocytes) that become a part of atheromatous plaque.  The diarylheptanoid abbreviated “HMP” is clearly shown to block lipid peroxidation products, and therefore, inhibit plaque formation.


Antioxidant 

One of the causes of inflammation and aging is oxidation of different substances forming high energy and unstable free radicals.  These unstable molecules release their oxygen and energy causing destruction.  Lesser galangal is shown to be a strong antioxidant and scavenger of free radicals protecting the body. 

Lesser galangal is clearly a potent antioxidant.  This property is both preventive of atherogenesis and cancer, as well as other degenerative diseases of aging.  The N-phenylpropanoids (1-7) listed were demonstrated to be antioxidants.  

Lipid peroxidation products cause the cox-2 enzymes to activate an inflammatory response that causes these products to be incorporated into inflammatory white blood cells (foamy monocytes) that become a part of atheromatous plaque.  The diarylheptanoid in Lesser Galangal, abbreviated “HMP” is clearly shown to block lipid peroxidation products, and therefore, inhibit plaque formation.


Tumor suppressive/Cancer preventive

As noted above lesser galangal has a high number of active ingredients.  These ingredients work simultaneously on different points of attack both to prevent cancer and to suppress tumor growth and metastasis.  Follow the text to learn greater detail of each of the mechanisms and the specific classes and ingredients which operate these mechanisms.  There are other cancer preventive mechanisms besides its antioxidant properties operating from the ingredients of lesser galangal.  Free radical scavenging is one of them by preventing their toxicity to genes. 

Apoptosis: Apoptosis is programmed cell death. Any substance that selectively induces apoptosis in cancer cells would be considered useful therapeutically against cancer.  Flavonoids galangin and quercitin are main constituents in Lesser Galangal, as stated previously, and for this additional reason of having been proven to induce apoptosis in cancer cells, they are to be considered relevant for consideration as cancer therapeutic agents.

Enhancing anti cancer drug efficacy:  In addition to free radical scavenging, lesser galangal ingredients have been shown to enhance the ability of certain   cancer fighting drugs to be more available. An example is certain cancer fighting drugs which are applied topically to skin cancers. The drug 5-fluorouracil (5-fu) is one such drug.  Volatile oils from Lesser Galangal have been shown to enhance the penetration of 5-fu into the skin, enhancing its cancer fighting ability.

Effect on Fatty Acid Synthase: Compared to normal human tissues, many common human cancers, including carcinoma of the colon, prostate, ovary, breast, and endometrium, express high levels of fatty acid synthase (FAS), the primary enzyme responsible for the synthesis of fatty acids. This differential expression of FAS between normal tissues and cancer has led to the notion that FAS is a target for anticancer drug development. Recent studies with C 75, a drug which is an inhibitor of fatty acid synthesis, have shown significant antitumor activity with concomitant inhibition of fatty acid synthesis in tumor tissue and normal liver. Importantly, histopathological analysis of normal tissues after treatment with this drug showed no adverse effects on normally proliferating cellular compartments, such as bone marrow, gastrointestinal tract, skin, or   lymphoid tissues. 

The significance of the above referenced  studies is that there are 3 components             within Lesser Galangal which have been identified to be powerful inhibitors of the enzyme FAS.  The inhibition of FAS by galangin, quercitin, and kaempferol, which are the main flavonoids existing in the Galangal, showed that quercitin and kaempferol had powerful reversible inhibitory activity without any evidence of slow binding inactivation.  An analysis of the kinetic results led to the conclusion that the blocking mechanism of galangal is different from other previously reported inhibitors of FAS like cerulenin, epigallocatechtin gallate, and the drug discussed above called C75. 

Binds adenosine receptors: Adenosine receptors play a role in a number of   processes.  Endogenous adenosine may play a role in generating cancer.  By binding adenosine receptors galangin, a bioflavonoid of LG may be preventing a cancer causing mechanism.         
Free radical scavenging:
  Free radicals are high energy unstable molecules that cause oxidative damage to genes. When strands of DNA are damaged by free radicals, the damaged parts of DNA are referred to as adducts.  When adducts are present within cells in sufficient quantity, this is considered genetic damage, or genotoxicity. When adducts are reproduced during cell division, they create rapidly dividing cells that do not obey the normal signals controlling cellular reproduction.  This is a simplified explanation of how a cancer can be formed.

Substances that find and destroy free radicals before they damage genes are called         free radical scavengers. This is another aspect of cancer chemoprotection and anti-genotoxicity exhibited by lesser galangal. The class of chemicals in lesser galangal that does this job is called flavones, like galangin and quercitin.  When flavones are complexed with zinc they are even more potent scavengers then when they act alone.  The results from both in vitro and in vivo studies indicate that galangin with both antioxidative and free radical scavenging ability is capable of modulating enzyme activities and suppressing genotoxicity of chemicals.

Chemoprotection prevents genotoxicity: Another aspect of lesser galangal is its        capacity to protect against environmental pollutants and their impact of toxicity on immune system function.  Reducing toxicity of unavoidable environmental pollutants helps prevent cancer. This is called cancer chemoprotection.  Along these same lines, galangin, a member of the flavonol class of flavonoids is present in high concentrations in Lesser Galangal.  The results from both in vitro and in vivo studies indicate that galangin with antioxidative and free radical scavenging ability as well, is capable of modulating enzyme activities and suppressing genotoxicity of chemicals.

 COX-2 Inhibition:  Flavonoids like galangin, by inhibiting cyclo-oxygenase-2  (COX-2) enzymes can be considered anticarcinogenic.  COX-2 –catalysed synthesis of pro-inflammatory prostaglandin E2 plays a key role in inflammation and its associated diseases, such as cancer and cardiovascular disease.

There are reports in the library demonstrating that lesser galangal flavonoids block COX-2 activity. However, in addition, the genetic transcriptional regulation of COX-2 can also be important (Transcriptional regulation means genes on DNA transcribe messenger RNA, which in turn make complex proteins called enzymes).  “…., quercetin, quercetin penta-acetate, flavone, resveratrol, ., kaempferol, galangin,,” many of which  are in Galangal and have been reported to modulate (down regulate) COX-2 transcription in a wide variety of systems.  In addition the following constituents in Lesser Galangal inhibited COX-2 activity:

Quercetin, quercetin 3-glucuronide, quercetin 3'-sulfate and 3'methylquercetin 3-glucuronide reduced COX-2 mRNA expression in both unstimulated and interleukin-1beta stimulated colon cancer (Caco2) cells. Quercetin and quercetin 3'-sulfate, unlike quercetin 3-glucuronide and 3'methylquercetin 3-glucuronide, also inhibited COX-2 activity.

What this means is that the process of genetic activation and expression of cox-2 being inhibited reduces the presence of cox-2 enzyme quantity.  As well as these same agents blocking its activity, they reduce the presence of cancer producing pro-inflammatory cytokines like PGE2.  Less COX-2 with less activity means less cancer producing pro-inflammatory compounds.


Anti-atherogenic (preventive against atherosclerosis)  

There are several mechanisms by which ingredients in lesser galangal fight against the formation of atherosclerosis or plaque formation.  The many ingredients in lesser galangal diminish the oxidation of critical fats and diminish the formation of inflamma-tion provoking free radicals that contribute to injury to the inside lining of blood vessels large and small.  Lesser galangal scavenges free radicals, which means the free radicals are found and destroyed before they do harm.  Ingredients in lesser galangal have been shown to reduce the concentration of fats in the serum, like cholesterol and triglycerides.  Lesser galangal also reduces platelet stickiness, which helps prevent unwanted clot formation in narrowed arteries.  By inhibiting the inflammatory reactions described elsewhere, plaque formation is likewise blocked. 

Diminishes lipid peroxidation products and free radical formation: The many ingredients in lesser galangal diminish the oxidation of critical fats and diminish the formation of inflammation provoking free radicals that contribute to injury to the inside lining of blood vessels large and small.  Peroxidation products that do occur cause the COX-2 enzymes to activate an inflammatory response that causes these products to be incorporated into inflammatory white blood cells (foamy monocytes) that become a part of atheromatous plaque. The diarylheptanoid in galangal abbreviated “HMP” is clearly shown to block lipid peroxidation products, and therefore, inhibit plaque formation. 

Scavenges free radicals: Substances that have the ability to find and destroy free        radicals before they damage the inside lining of blood vessels are called free radical scavengers. This is another aspect of atherosclerosis protection exhibited by lesser galangal. The class of chemicals in lesser galangal that does this job is the class called flavones, like galangin and quercitin.  When flavones are complexed with zinc they are even more potent scavengers then when they act alone.  The results from both in vitro and in vivo studies indicate that galangin has antioxidative and free radical scavenging ability as well.

 Lowers cholesterol and triglycerides:  A well known way to lower risk of hardening of the arteries is to lower serum cholesterol, other lipids, and triglycerides.  We include papers which demonstrate Lesser Galangal’s ability to do this.  A pancreatic lipase inhibitor called: “HPH” (another diarylheptanoid) lowered cholesterol and triglycerides. Pancreatic Lipase inhibition is a well recognized mechanism to reduce serum lipid concentration. 

Inhibits the inflammatory component of plaque formation:  Inflammation is one of the subtle causes of hardening of the arteries or atherosclerosis.  So overlapping evidence of anti-inflammatory efficacy is one of the ways lesser galangal inhibits atherogenesis.


Antibiotic / antiviral / anti-parasitic / anti-fungal 

Lesser Galangal has natural antibiotic/antiviral/antifungal and anti parasite properties that make it useful to treat or prevent infections.   

The flavonoids in Lesser Galangal have antiviral, antibacterial, and antifungal properties, and even in one case anti-parasitic properties against the Trypanosome, T. cruzi, which contaminates blood supplies in Africa and Asia and causes Chagas disease.  These properties have been discovered and explored in depth in abstracts in this library. We present one article demonstrating antiviral properties and six exploring the mechanisms and the susceptible strains of bacteria and one dealing with Chagas disease.


Antiemetic 

Although not much is presented in this library, lesser galangal also has shown the property of combating nausea.  It is, therefore, considered an anti-emetic. 


May enhance anticancer drug efficacy by reducing tumor resistance  

In conclusion of the scientific sections, we present one article in which there is a discussion as to how natural herbal substances like lesser galangal may actually work to facilitate pharmaceuticals’ activity against cancer and also protect against the development of resistance to drug efficacy in cancer treatment. 


Long history in Folk Medicine worldwide   

Before concluding the library itself, we included a presentation of the history of lesser galangal’s use in the world with special attention to its presentation as a folk remedy. Although not scientific in the western sense, many schools of thought from traditional Chinese medicine, to Naturopathy, to Aeurvedic medicine, which have endured for thousands of years, embrace this substance as well.  Their descriptions of it are significantly similar to the western science we have presented.


THE LIBRARY

 

Papers with the analyses of compounds chemically active in Lesser Galangal

 

Zhong Yao Cai. 1998 Jul;21(7):349-51.

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[Study on the chemical components of Alpinia officinarum]

[Article in Chinese]

Luo H, Cai C, Zhang J, Mo L.

Guangdong Medical College, Zhanjiang 524023.

Four crystalline substances were isolated from rhizome of Alpinia officinarum Hance. They were identified as beta-Sitosterol (I), Galangin (II), Emodin (III) and Quercetin (IV), I and III were separated from this plant for the first time.

 

 

J Agric Food Chem. 2003 Aug 13;51(17):4924-9.

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Isolation and characterization of some antioxidative compounds from the rhizomes of smaller galanga (Alpinia officinarum Hance).

Ly TN, Shimoyamada M, Kato K, Yamauchi R.

The United Graduate School of Agricultural Science, Department of Bioprocessing, Faculty of Agriculture, Gifu University, 1-1 Yanagido, Gifu City, Gifu 501-1193, Japan.

Antioxidative compounds were isolated from the methanol extract of fresh rhizome of smaller galanga (Alpinia officinarum Hance). Seven phenylpropanoids (1-7) were finally obtained by reversed-phase HPLC, and their structures were elucidated by MS and NMR analyses. They comprised the two known compounds, (E)-p-coumaryl alcohol gamma-O-methyl ether (1) and (E)-p-coumaryl alcohol (6), and the five novel compounds, stereoisomers of (4E)-1,5-bis(4-hydroxyphenyl)-1-methoxy-2-(methoxymethyl)-4-pentene (2a and 2b), stereoisomers of (4E)-1,5-bis(4-hydroxyphenyl)-1-ethoxy-2-(methoxymethyl)-4-pentene (3a and 3b), (4E)-1,5-bis(4-hydroxyphenyl)-1-[(2E)-3-(4-acetoxyphenyl)-2-propenoxy]-2-(methoxymethyl)-4-pentene (4), (4E)-1,5-bis(4-hydroxyphenyl)-2-(methoxymethyl)-4-penten-1-ol (5), and (4E)-1,5-bis(4-hydroxyphenyl)-2-(hydroxymethyl)-4-penten-1-ol (7). Compounds 1-7 were detected for the first time as constituents of galanga rhizomes and exhibited antioxidative activities against the autoxidation of methyl linoleate in bulk phase.

 

Zhong Yao Cai. 2000 Feb;23(2):84-7.

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[Chemical study of Alpinia officinarum]

[Article in Chinese]

Bu X, Xiao G, Gu L, Zhang M.

Zhongshan University, Guangzhou 510275.

Seven compounds were isolated from Alinia officinarum Hance and were identified as beta-sitoSterol, 1,7-diphenyl-5-ol-3-heptone, 1-phenyl-7-(3'-methoxyl-4'-hydroxyl) phenyl-5-ol-3-heptone, glandin, kaempferol-4'-methylether and 3,4-dihydroxylbenzoic acid by IR, 1HNMR, 13CNMR, FAB-MS and EA. Among these compounds, 3,4-dihydroxylbenzoic acid was the first time obtained from Alpinia officinarum Hance. Furthermore, 1-phenyl-7-(3'-methoxyl-4'-hydroxyl) phenyl-5-ol-3-heptone and a new compound 1,7-diphenyl-3,5-heptandiol-phenyl-7-(3'-methoxyl-4'-hydroxyl) phenyl-3,5-heptaxdiol were obtained from 1,7-diphenyl-5-ol-3-heptone and 1-phenyl-7-(3'-methoxyl-4'-hydroxyl) phenyl-5-ol-3-heptone via chemical reductions.

Planta Med. 2003 Jan;69(1):72-4.

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Inhibition of 5alpha-reductase activity by diarylheptanoids from Alpinia officinarum.

Kim YU, Son HK, Song HK, Ahn MJ, Lee SS, Lee SK.

The acetone extract from the rhizomes of Alpinia officinarum was evaluated for activity against 5alpha-reductase which had been prepared from rat prostate. The fraction responsible for the inhibition of the enzyme was purified, analyzed, and the active constituents were identified as four diarylheptanoids, 1,7-diphenylhept-4-en-3-one, dihydroyashabushiketol (1,7-diphenyl-5-hydroxy-3-heptanone), 5-hydroxy-7-(4"-hydroxy-3"-methoxyphenyl)-1-phenyl-3-heptanone and 5-hydroxy-7-(4"-hydroxyphenyl)-1-phenyl-3-heptanone.

 

 

J Agric Food Chem. 2002 Aug 14;50(17):4919-24.

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Isolation and structural elucidation of some glycosides from the rhizomes of smaller galanga (Alpinia officinarum Hance).

Ly TN, Yamauchi R, Shimoyamada M, Kato K.

The United Graduate School of Agricultural Science, Department of Bioprocessing, Gifu University, 1-1 Yanagido, Gifu City, Gifu 501-1193, Japan.

Glycosidically bound compounds were isolated from the methanol extract of fresh rhizomes of smaller galanga (Alpinia officinarum Hance). Nine glycosides (1-9) were finally obtained by reversed-phase HPLC and their structures were elucidated by MS and NMR analyses. They were the three known glycosides, (1R,3S,4S)-trans-3-hydroxy-1,8-cineole beta-D-glucopyranoside (1), benzyl beta-D-glucopyranoside (3), and 1-O-beta-D-glucopyranosyl-4-allylbenzene (chavicol beta-D-glucopyranoside, 4); and the six novel glycosides, 3-methyl-but-2-en-1-yl beta-D-glucopyranoside (2), 1-hydroxy-2-O-beta-D-glucopyranosyl-4-allylbenzene (5), 1-O-beta-D-glucopyranosyl-2-hydroxy-4-allylbenzene (demethyleugenol beta-D-glucopyranoside, 6), 1-O-(6-O-alpha-L-rhamnopyranosyl-beta-D-glucopyranosyl)-2-hydroxy-4-allylbenzene (demethyleugenol beta-rutinoside, 7), 1-O-(6-O-alpha-L-rhamnopyranosyl-beta-D-glucopyranosyl)-4-allylbenzene (chavicol beta-rutinoside, 8), and 1,2-di-O-beta-D-glucopyranosyl-4-allylbenzene (9). Compounds 2-9 were detected for the first time as constituents of galanga rhizomes.

Anti-inflammatory mechanisms are applicable to Lesser Galangal:

Chem Pharm Bull (Tokyo). 1992 Feb;40(2):387-91.

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Inhibition of prostaglandin and leukotriene biosynthesis by gingerols and diarylheptanoids.

Kiuchi F, Iwakami S, Shibuya M, Hanaoka F, Sankawa U.

Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.

The rhizomes of Zingiber officinale (ginger) and Alpinia officinarum contain potent inhibitors against prostaglandin biosynthesizing enzyme (PG synthetase). Gingerols and diarylhepatanoids were identified as active compounds. Their possible mechanism of action which was deduced from the structures of active compounds indicated that the inhibitors would also be active against arachidonate 5-lipoxygenase, an enzyme of leukotriene (LT) biosynthesis. This was verified by testing their inhibitory effects on 5-lipoxygenase prepared from RBL-1 cells. A diarylheptanoid with catechol group was the most active compound against 5-lipoxygenase, while yakuchinone A was the most active against PG synthetase.

More on anti inflammatory activity (Galangin and Quercitin present in Lesser Galangal) blocking prostaglandin synthesis, nitric oxide free radical formation, and cox-2 enzyme activation: especially relating to arthritides.  Remember Vioxx, Celebrex, and other new and controversial arthritis drugs are COX-2 inhibitors.

Life Sci. 2001 Jan 12;68(8):921-31.

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Inhibition of inducible nitric oxide synthase and cyclooxygenase-2 expression by flavonoids in macrophage J774A.1.

Raso GM, Meli R, Di Carlo G, Pacilio M, Di Carlo R.

Department of Experimental Pharmacology, University of Naples Federico II, Italy.

The present study focuses on the effect of various naturally occurring flavonoids (apigenin, galangin, morin, naringenin, quercetin, and silymarin) on nitric oxide (NO) and prostaglandin E2 (PGE2) production induced by lipopolysaccharide (LPS) in the macrophage cell line J774A.1. Moreover, we evaluated flavonoid modulation of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) enzyme expression by western blot analysis. Apigenin and quercetin (0.5-50 microM) were the most potent inhibitors of NO production and this effect was concentration-dependent and significant at 5 and 50 microM. These data were consistent with the modulation of iNOS enzyme expression. A similar pattern was observed considering the inhibitory effect of flavonoids on LPS-induced PGE2 release and COX-2 expression.
Quercetin, galangin, apigenin, and naringenin markedly decreased PGE2 release and COX-2 expression in a concentration-dependent manner. This study suggests that inhibition of iNOS and COX-2 expression by flavonoids may be one of the mechanisms responsible for their anti-inflammatory effects.

Further the principal diarylheptanoid HMP in Lesser Galangal’s role as an anti-inflammatory substance:

 

J Pharmacol Exp Ther. 2003 Jun;305(3):925-31. Epub 2003 Mar 06.

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A diarylheptanoid from lesser galangal (Alpinia officinarum) inhibits proinflammatory mediators via inhibition of mitogen-activated protein kinase, p44/42, and transcription factor nuclear factor-kappa B.

Yadav PN, Liu Z, Rafi MM.

Department of Food Science, Cook College, New Jersey Agricultural Experimentation Station, Rutgers, The State University of New Jersey, New Brunswick, NJ 08901, USA.

The diarylheptanoid 7-(4'-hydroxy-3'-methoxyphenyl)-1-phenylhept-4-en-3-one (HMP) is a naturally occurring phytochemical found in lesser galangal (Alpinia officinarum).
In the present study, we have demonstrated the anti-inflammatory properties of this compound on mouse macrophage cell line (RAW 264.7) and human peripheral blood mononuclear cells (PBMCs) in vitro. Treatment of RAW 264.7 cells with HMP (6.25-25 microM) significantly inhibited lipopolysaccharide (LPS)-stimulated nitric oxide (NO) production. This compound also inhibited the release of LPS-induced proinflammatory cytokines interleukin-1 beta (IL-1 beta) and tumor necrosis factor-alpha (TNF-alpha) from human PB-MCs in vitro. In addition, Western blotting and reverse transcription-polymerase chain reaction analysis demonstrated that HMP decreased LPS-induced inducible nitric-oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) protein and mRNA expression in RAW 264.7 cells. Furthermore, HMP treatment also reduced nuclear factor-kappa B (NF-kappa B) DNA binding induced by LPS in RAW 264.7 cells. To elucidate the molecular mechanism for inhibition of proinflammatory mediators by HMP (25 microM), we have studied the effect of HMP on LPS-induced p38 and p44/42 mitogen-activated protein kinase (MAPK). We observed that the phosphorylation of p44/42 MAPK in LPS-stimulated RAW 264.7 cells was markedly inhibited by HMP, whereas activation of p38 MAPK was not affected. These results suggested that HMP from lesser galangal suppressed the LPS-induced production of NO, IL-1 beta, and TNF-alpha and expression of iNOS and COX-2 gene expression by inhibiting NF-kappa B activation and phosphorylation of p44/42 MAPK.

We include this next abstract on inflammation mechanisms in this section even though this abstract also applies to how lesser galangal prevents atherogenesis as an anti-inflammatory:

Editor’s note: This paper is very technical and is not directly discussing lesser galangal, but relates back to the last paper showing the mechanisms currently investigated and understood as part of the inflammatory  cause of atherosclerosis.     Lesser galangal’s ingredients’ mechanisms of action on inflammation apply very closely to the discussion below.  Lesser galangal does not contain the compound “HNE” discussed next. HNE acts to induce pro-inflammatory cytokines like oxidation products of  lipopolysacharrides ( LPS) do, but as illustrated above LG does have the compound “HMP” which blocks the inflammation in macrophages and prevents induction of the COX-2 enzymes, thus inhibiting the accumulation of inflammatory peroxidation products which contribute to the formation of plaque. This principle is generalized to the same cascade of events that occurs in inflammatory reactions in other tissues as well as on the inside of arteries.


Originally published In Press as doi:10.1074/jbc.M409935200 on September 8, 2004

J. Biol. Chem., Vol. 279, Issue 46, 48389-48396, November 12, 2004

A Lipid Peroxidation-derived Inflammatory Mediator

IDENTIFICATION OF 4-HYDROXY-2-NONENAL AS A POTENTIAL INDUCER OF CYCLOOXYGENASE-2 IN MACROPHAGES

Takeshi Kumagai, Nao Matsukawa, Yayoi Kaneko, Yoshiaki Kusumi, Masako Mitsumata, and Koji Uchida

From the Graduate School of Bioagricultural Sciences and Institute for Advanced Research, Nagoya University, Nagoya 464–8601 and the Department of Pathology, Nihon University School of Medicine, Tokyo 173–8610, Japan

Received for publication, August 30, 2004, and in revised form, September 7, 2004.  
Cyclooxygenases (COXs) catalyze the conversion of arachidonic acid to eicosanoids, which mediate a variety of biological actions involved in vascular pathophysiology. In the present study, we investigated the role of lipid peroxidation products in the up-regulation of COX-2, an inducible isoform responsible for high levels of prostaglandin production during inflammation and immune responses. COX-2 was found to colocalize with 4-hydroxy-2-nonenal (HNE), a major lipid peroxidation-derived aldehyde, in foamy macrophages within human atheromatous lesions, suggesting that COX-2 expression may be associated with the accumulation of lipid peroxidation products within macrophages. To test the hypothesis that lipid peroxidation products might be involved in the regulation of prostanoid biosynthesis, we conducted a screen of oxidized fatty acid metabolites and found that, among the compounds tested, only HNE showed inducibility of the COX-2 protein in RAW264.7 macrophages. In addition, intraperitoneal administration of HNE resulted in an increase in cell numbers in the peritoneal cavity that was associated with significant increases in the peritoneal and tissue levels of COX-2 in mice. To understand the possible signaling mechanism underlying the inducing effect of HNE on COX-2 up-regulation, we examined the phosphorylation events that may lead to COX-2 induction and found that HNE did not stimulate the induction of nitric oxide synthase and activation of NF-{kappa}B but significantly activated p38 mitogen-activated protein kinase and its upstream kinase in RAW264.7 macrophages. Tyrosine kinases, such as the epidermal growth factor-like and Src family tyrosine kinases, appeared to mediate the stabilization of COX-2 mRNA via the p38 mitogen-activated protein kinase pathway. These findings suggest that HNE accumulated in macrophages/foam cells may represent an inflammatory mediator that plays a role in stimulation of the inflammatory response and contributes to the progression of atherogenesis.

Contrasting view in the following study: in their experimental model, galangal did not stand out among plant remedies tested for effect on rheumatic (inflammatory) conditions:

Drugs Exp Clin Res. 1989;15(8):369-72.

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Experimental studies on antirheumatic crude drugs used in Saudi traditional medicine.

Ageel AM, Mossa JS, al-Yahya MA, al-Said MS, Tariq M.

College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

A large number of herbal drugs are used in the traditional medicine of Saudi Arabia for the treatment of rheumatism, arthritis, gout and other forms of inflammation. In the present study seven of these crude drugs, namely Francoeuria crispa, Hammada elegans, Malus pumila, Ruta chalepensis, Smilax sarsaparilla, Achillea fragrantissima and Alpinia officinarum were tested against carrageenan-induced acute inflammation in rats. The plant materials were extracted with 96% ethanol. The dried extract was dissolved in water for pharmacological testing. The rats were administered an oral dose of 500 mg/kg body weight of each extract 1 h prior to production of inflammation by carrageenan injection (0.05 ml of 1% carrageenan suspension in the planter aponeurosis of the right hind foot). The paw volume was measured at 0,2,3 and 4 h after the injection. Four of the seven plants, namely Francoeuria crispa (24%), Malus pumila (23%), Ruta chalepensis (30%) and Smilax sarsaparilla (25%), produced significant inhibition of carrageenan-induced inflammation in rats. These plants also inhibited cotton pellet-induced exudation. Further studies are suggested to isolate the active principles and for the determination of the mechanism of action of these drugs.

Editor’s note: The extraction process used in the above study in 1989 does not necessarily bring out all of the active ingredients recently studied for their anti inflammatory effects.  So in effect we do not really know the significance or lack thereof of the study.  We simply include it as a contrasting view.

 

Antioxidants have been found to be preventative in aging, cancer, atherogenesis and other degenerative diseases. The following article shows that Lesser Galangal has significant antioxidant properties:.

 

Life Sci. 2003 May 30;73(2):167-79.

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Screening of medicinal plant extracts for antioxidant activity.

Lee SE, Hwang HJ, Ha JS, Jeong HS, Kim JH.

Department of Biochemistry, College of Dentistry, Kyung Hee University, 1 Hoegi-Dong, Dongdaemoon-Ku, Seoul 130-701, South Korea.

The methanol extracts of nine medicinal plants traditionally used in Chinese medicine were screened for antioxidant activity versus resveratrol, which has been shown to protect cells from oxidative damage [Toxicol. Lett. 102 (1998) 5]. Most of the plant extracts used in this study inhibited the H(2)O(2)-induced apoptosis of Chinese hamster lung fibroblast (V79-4) cells. The extracts of Areca catechu var. dulcissima, Paeonia suffruticosa,
Alpinia officinarum, Glycyrrhiza uralensis and Cinnamomun cassia strongly enhanced viability against H(2)O(2)-induced oxidative damage in V79-4 cells. Relatively high levels of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity were detected in extracts of Areca catechu var. dulcissima, Paeonia suffruticosa and Cinnamomun cassia (IC(50) < 6.0 microg/ml). The activities of superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPX) were dose-dependently enhanced in V79-4 cells treated with most of the plant extracts. The extracts of Areca catechu var. dulcissima showed higher antioxidant activity than resveratrol in all experiments. These results suggest that the plant extracts prevent oxidative damage in normal cells probably because of their antioxidant characteristics.

 

More on antioxidant compounds operating in Lesser Galangal:

 

J Agric Food Chem. 2003 Aug 13;51(17):4924-9.

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Isolation and characterization of some antioxidative compounds from the rhizomes of smaller galanga (Alpinia officinarum Hance).

Ly TN, Shimoyamada M, Kato K, Yamauchi R.

The United Graduate School of Agricultural Science, Department of Bioprocessing, Faculty of Agriculture, Gifu University, 1-1 Yanagido, Gifu City, Gifu 501-1193, Japan.

Antioxidative compounds were isolated from the methanol extract of fresh rhizome of smaller galanga (Alpinia officinarum Hance). Seven phenylpropanoids (1-7) were finally obtained by reversed-phase HPLC, and their structures were elucidated by MS and NMR analyses. They comprised the two known compounds, (E)-p-coumaryl alcohol gamma-O-methyl ether (1) and (E)-p-coumaryl alcohol (6), and the five novel compounds, stereoisomers of (4E)-1,5-bis(4-hydroxyphenyl)-1-methoxy-2-(methoxymethyl)-4-pentene (2a and 2b), stereoisomers of (4E)-1,5-bis(4-hydroxyphenyl)-1-ethoxy-2-(methoxymethyl)-4-pentene (3a and 3b), (4E)-1,5-bis(4-hydroxyphenyl)-1-[(2E)-3-(4-acetoxyphenyl)-2-propenoxy]-2-(methoxymethyl)-4-pentene (4), (4E)-1,5-bis(4-hydroxyphenyl)-2-(methoxymethyl)-4-penten-1-ol (5), and (4E)-1,5-bis(4-hydroxyphenyl)-2-(hydroxymethyl)-4-penten-1-ol (7). Compounds 1-7 were detected for the first time as constituents of galanga rhizomes and exhibited antioxidative activities against the autoxidation of methyl linoleate in bulk phase.

Complexing flavones such as galangin with metal ions like zinc, potentiate the antioxidant and free radical scavenging capabilities of LG:

Redox Rep. 2004;9(2):97-104.

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Antioxidant properties of complexes of flavonoids with metal ions.

de Souza RF, De Giovani WF.

Departamento de Quimica, Faculdade de Filosofia Ciencias e Letras de Ribeirao Preto, Universidade de Sao Paulo, Brazil.

The formation of complexes of metal ions with the flavonoids quercetin (L1), rutin (L2), galangin (L3) and catechin (L4) has been investigated by UV-visible spectroscopy. The antioxidant activities of the compounds were evaluated by using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging method. In this work, we have shown that the complexed flavonoids are much more effective free radical scavengers than the free flavonoids. We suggest that the higher antioxidant activity of the complexes is due to the acquisition of additional superoxide dismutating centers. Radical scavenging activities of the compounds were also investigated from an electrochemical point of view. There is a relationship between the logarithm of the antioxidant activity (represented by EC50) and the oxidation potential. The synergic effect of the complexes and ascorbic acid were studied by [13C]-NMR analyses. The results show that ascorbic acid can protect flavonoids from oxidative degradation, and reveal antioxidant synergies between ascorbic acid and the compounds.

 

Tumor Suppressive/Cancer preventive

 

Apoptosis is programmed cell death. Any substance that selectively induces apoptosis in cancer cells would be considered useful therapeutically. Flavonoids Galangin and Quercitin mentioned below are present as main constituent compounds in Lesser Galangal and, therefore, relevant to therapeutic consideration:

Nutr Cancer. 2004;50(1):90-100.

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Flavonoids induce apoptosis in human leukemia U937 cells through caspase- and caspase-calpain-dependent pathways.

Monasterio A, Urdaci MC, Pinchuk IV, Lopez-Moratalla N, Martinez-Irujo JJ.

Departamento di Bioquimica y Biologia Molecular, Universidad de Navarra, Pamplona, Spain.

Flavonoids are polyphenolic phytochemicals that are ubiquitous in plants and present in the common human diet. They may exert diverse beneficial effects, including antioxidant and anticarcinogenic activities. In this study we tested the apoptotic activity of 22 flavonoids and related compounds in leukemic U937 cells. Several flavones but none of the isoflavones or flavanones tested induced apoptotic cell death under these conditions, as determined by reduction in cell viability, flow cytometry, and oligonucleosomal DNA fragmentation. Structure-activity relationship showed that at least two hydroxylations in positions 3, 5, and 7 of the A ring were needed to induce apoptosis, whereas hydroxylation in 3' and/or 4' of the B ring enhanced proapoptotic activity. At lower concentrations, these compounds were also able to sensitize these cells to apoptosis induced by tumor necrosis factor-alpha.
Regarding the mechanisms, galangin, luteolin, chrysin, and quercetin induced apoptosis in a way that required the activation of caspases 3 and 8, but not caspase 9. In contrast, an active role of calpains in addition to caspases was demonstrated in apoptosis induced by fisetin, apigenin, and 3,7-dihydroxyflavone. Our data show evidence of the proapoptotic properties of some flavonoids that could support their rational use as chemopreventive and therapeutic agents against carcinogenic disease.

 

Enhancing cancer drug efficacy: The following is an example of how LG when combined in a vanishing crème containing the cancer drug 5-fluorouracil may enhance the skin penetration of the drug, and its efficacy.

 

Zhong Yao Cai. 2000 Nov;23(11):697-9.

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[The study on Rhizoma Alpiniae officinarum and other herbs as penetration enhancer for the permeation of 5-fluorouacil]

[Article in Chinese]

Shen Q, Li W, Xu L.

Changhai Hospital, Second Military Medical University, Shanghai 200032.

OBJECTIVE: To study the effects of volatile oils from Rhizoma Alpiniae Officinarum, Pericarpium Zanthoxyli, Herba Asari, cineaol and ethanol extracts on the percutaneous penetration of 5-fluorouracil. METHODS: By Valia-Chienhorizontal diffusion cell and HPLC, the effects of volatile oils from Rhizoma Alpiniae Officinarum, Pericarpium Zanthoxyli, Herba Asari, cineol and ethanol extracts on the percutaneous penetration of 5-fluorouracil were observed and compared with azone. RESULT: 1%, 3% volatile oils from Rhizoma Alpiniae Officinarum, Pericarpium Zanthoxyli and cineol possessed strong promoting action on percutaneous absorption of 5-fluorouracil. The effects of volatile oils from Rhizoma Alpiniae Officinarum were stronger than that of azone; the effects of volatile oils from Pericarpium Zanthoxyli were the same as that of azone. CONCLUSION:
The volatile oils from Rhizoma Alpiniae Officinarum, Pericarpium Zanthoxyli, Herba Asari can enhance effectively the skin permeation of 5-fluorouracil. They deserved to be researched and developed further.

Effect on Fatty Acid Synthase: Fatty acid synthase (FAS) is an enzyme closely correlated with cancer cell proliferation.  The following article explains the role of FAS. The article afterwards shows how Galangal with its three main flavonoids opposes this critical cancer enzyme:

Proc Natl Acad Sci U S A. 2000 Mar 28;97(7):3450-4.

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Synthesis and antitumor activity of an inhibitor of fatty acid synthase.

Kuhajda FP, Pizer ES, Li JN, Mani NS, Frehywot GL, Townsend CA.

Department of Pathology, The Johns Hopkins University School of Medicine, 4940 Eastern Avenue, Baltimore, MD 21224, USA. fkuhajda@jhmi.edu

Compared to normal human tissues, many common human cancers, including carcinoma of the colon, prostate, ovary, breast, and endometrium, express high levels of fatty acid synthase (FAS, EC ), the primary enzyme responsible for the synthesis of fatty acids. This differential expression of FAS between normal tissues and cancer has led to the notion that FAS is a target for anticancer drug development. Recent studies with C75, an inhibitor of fatty acid synthesis, have shown significant antitumor activity with concomitant inhibition of fatty acid synthesis in tumor tissue and normal liver. Importantly, histopathological analysis of normal tissues after C75 treatment showed no adverse effects on proliferating cellular compartments, such as bone marrow, gastrointestinal tract, skin, or lymphoid tissues. In this study, we describe the de novo synthesis of C75 based on the known mechanism of action of cerulenin and the theoretical reaction intermediates of the beta-ketoacyl synthase moiety of FAS. In addition, we demonstrate that C75 is a synthetic, chemically stable inhibitor of FAS. C75 inhibits purified mammalian FAS with characteristics of a slow-binding inhibitor and also inhibits fatty acid synthesis in human cancer cells. Treatment of human breast cancer cells with [5-(3)H]C75 demonstrates that C75 reacts preferentially with FAS in whole cells. Therefore, we have shown that the primary mechanism of the antitumor activity of C75 is likely mediated through its interaction with, and inhibition of, FAS. This development will enable the in vivo study of FAS inhibition in human cancer and other metabolic diseases.

J Enzyme Inhib Med Chem. 2003 Aug;18(4):349-56.

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Presence of fatty acid synthase inhibitors in the rhizome of Alpinia officinarum hance.

Li BH, Tian WX.

Department of Biology, Graduate School of Chinese Academy of Sciences, PO Box 3908, Beijing 100039, People's Republic of China.

The galangal (the rhizome of Alpinia officinarum, Hance) is popular in Asia as a traditional herbal medicine.
The present study reports that the galangal extract (GE) can potently inhibit fatty-acid synthase (FAS, E.C.2.3.1.85). The inhibition consists of both reversible inhibition with an IC50 value of 1.73 microg dried GE/ml, and biphasic slow-binding inactivation. Subsequently the reversible inhibition and slow-binding inactivation to FAS were further studied. The inhibition of FAS by galangin, quercetin and kaempferol, which are the main flavonoids existing in the galangal, showed that quercetin and kaempferol had potent reversible inhibitory activity, but all three flavonoids had no obvious slow-binding inactivation. Analysis of the kinetic results led to the conclusion that the inhibitory mechanism of GE is totally different from that of some other previously reported inhibitors of FAS, such as cerulenin, EGCG (epigallocatechin gallate) and C75.

 

            Binds Adenosine Receptors: Adenosine receptors play a role in a number of                     processes.  Endogenous adenosine may play a role in generating cancer.  By     binding adenosine receptors  galangin, a bioflavonoid of LG may be preventing a        cancer causing mechanism. The following article explores mechanisms:

 

Adv Exp Med Biol. 2002;505:163-71.

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Interactions of flavones and other phytochemicals with adenosine receptors.

Jacobson KA, Moro S, Manthey JA, West PL, Ji XD.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes, Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0810, USA. kajacobs@helix.nih.gov

Dietary flavonoids have varied effects on animal cells, such as inhibition of platelet binding and aggregation, inhibition of inflammation, and anticancer properties, but the mechanisms of these effects remain largely unexplained. Adenosine receptors are involved in the homeostasis of the immune, cardiovascular, and central nervous systems, and adenosine agonists/antagonists exert many similar effects. The affinity of flavonoids and other phytochemicals to adenosine receptors suggests that a wide range of natural substances in the diet may potentially block the effects of endogenous adenosine. We used competitive radioligand binding assays to screen flavonoid libraries for affinity and a computational CoMFA analysis of flavonoids to compare steric and electrostatic requirements for ligand recognition at three subtypes of adenosine receptors. Flavone derivatives, such as galangin, were found to bind to three subtypes of adenosine receptors in the microM range. Pentamethylmorin (Ki 2.65 microM) was 14- to 17-fold selective for human A3 receptors than for A1 and A2A receptors. An isoflavone, genistein, was found to bind to A1 receptors. Aurones, such as hispidol (Ki 350 nM) are selective A1 receptor antagonists, and, like genistein, are present in soy. The flavones, chemically optimized for receptor binding, have led to the antagonist, MRS 1067 (3,6-dichloro-2'-(isopropoxy)4'-methylflavone), which is 200-fold more selective for human A3 than A1 receptors. Adenosine receptor antagonism, therefore, may be important in the spectrum of biological activities reported for the flavonoids.

 

Chemoprotection prevents genotoxicity: Another aspect of lesser galangal is its ability to protect against environmental pollutants and their impact of toxicity on immune system function. Toxicity predisposes to developing cancer. The next article explores how this is so: 

 

Mol Pharmacol. 2000 Sep;58(3):515-25.

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The bioflavonoid galangin blocks aryl hydrocarbon receptor activation and polycyclic aromatic hydrocarbon-induced pre-B cell apoptosis.

Quadri SA, Qadri AN, Hahn ME, Mann KK, Sherr DH.

Department of Environmental Health, Boston University School of Public Health, Boston, Massachusetts 02118, USA.

Bioflavonoids are plant compounds touted for their potential to treat or prevent several diseases including cancers induced by common environmental chemicals. Much of the biologic activity of one such class of pollutants, polycyclic aromatic hydrocarbons (PAH), is mediated by the aryl hydrocarbon receptor/transcription factor (AhR). For example, the AhR regulates PAH immunotoxicity that manifests as pre-B cell apoptosis in models of B cell development. Because bioflavonoids block PAH-induced cell transformation and are structurally similar to AhR ligands, it was postulated that some of them would suppress PAH-induced, AhR-dependent immunotoxicity, possibly through a direct AhR blockade. This hypothesis was tested using a model of B cell development in which pre-B cells are cultured with and are dependent on bone marrow stromal or hepatic parenchymal cell monolayers. Of seven bioflavonoids screened, galangin (3,5,7-trihydroxyflavone) blocked PAH-induced but not C(2)-ceramide- or H(2)O(2)-induced pre-B cell apoptosis. Because galangin blocked AhR-dependent reporter gene expression, AhR complex-DNA binding, and AhR nuclear translocation, inhibition of a relatively early step in AhR signaling was implicated. This hypothesis was supported by the ability of galangin to bind the AhR and stabilize AhR-90-kDa heat shock protein complexes in the presence of AhR agonists. These studies demonstrate the utility of pre-B cell culture systems in identifying compounds capable of blocking PAH immunotoxicity, define at least one mechanism of galangin activity (i.e., repression of AhR activation), and motivate the use of this and similar dietary bioflavonoids as relatively nontoxic inhibitors of AhR agonist activity and as pharmacologic agents with which to dissect AhR signaling pathways.

Genotoxicity is an inducer of cancer. Anti-genotoxicity renders a substance potentially chemopreventive of cancer:

 

Mutat Res. 2001 May;488(2):135-50.

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Anti-genotoxicity of galangin as a cancer chemopreventive agent candidate.

Heo MY, Sohn SJ, Au WW.

College of Pharmacy, Kangwon National University, Chunchon 200, South Korea. h0858my@hanmail.net

Flavonoids are polyphenolic compounds that are present in plants. They have been shown to possess a variety of biological activities at non-toxic concentrations in organisms. Galangin, a member of the flavonol class of flavonoid, is present in high concentrations in medicinal plants (e.g. Alpinia officinarum) and propolis, a natural beehive product. Results from in vitro and in vivo studies indicate that galangin with anti-oxidative and free radical scavenging activities is capable of modulating enzyme activities and suppressing the genotoxicity of chemicals. These activities will be discussed in this review. Based on our review, galangin may be a promising candidate for cancer chemoprevention.

More of the same story as to chemoprotective mechanisms:

Br J Cancer. 1999 Mar;79(9-10):1340-6.

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The flavonoid galangin is an inhibitor of CYP1A1 activity and an agonist/antagonist of the aryl hydrocarbon receptor.

Ciolino HP, Yeh GC.

Cellular Defense and Carcinogenesis Section, Basic Research Laboratory, Division of Basic Sciences, National Cancer Institute-Frederick Cancer Research and Development Center, NIH, MD 21702-1201, USA.

The effect of the dietary flavonoid galangin on the metabolism of 7,12-dimethylbenz[a]anthracene (DMBA), the activity of cytochrome P450 1A1 (CYP1A1), and the expression of CYP1A1 in MCF-7 human breast carcinoma cells was investigated. Galangin inhibited the catabolic breakdown of DMBA, as measured by thin-layer chromatography, in a dose-dependent manner. Galangin also inhibited the formation of DMBA-DNA adducts, and prevented DMBA-induced inhibition of cell growth. Galangin caused a potent, dose-dependent inhibition of CYP1A1 activity, as measured by ethoxyresorufin-O-deethylase activity, in intact cells and in microsomes isolated from DMBA-treated cells. Analysis of the inhibition kinetics by double-reciprocal plot demonstrated that galangin inhibited CYP1A1 activity in a noncompetitive manner. Galangin caused an increase in the level of CYP1A1 mRNA, indicating that it may be an agonist of the aryl hydrocarbon receptor, but it inhibited the induction of CYP1A1 mRNA by DMBA or by 2,3,5,7-tetrachlorodibenzo-p-dioxin (TCDD). Galangin also inhibited the DMBA- or TCDD-induced transcription of a reporter vector containing the CYP1A1 promoter. Thus, galangin is a potent inhibitor of DMBA metabolism and an agonist/antagonist of the AhR, and may prove to be an effective chemopreventive agent.

Cancer prevention mechanisms expanded in the next abstract:

Drug Metab Dispos. 1998 Oct;26(10):989-92.

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Comparative inhibition of human cytochromes P450 1A1 and 1A2 by flavonoids.

Zhai S, Dai R, Friedman FK, Vestal RE.

Clinical Pharmacology and Gerontology Research Unit, Department of Veterans Affairs Medical Center and Mountain States Medical Research Institute, Boise, ID 83702, USA.

Flavonoids are a class of dietary phytochemicals that modulate various biological activities. The effects of flavone and five hydroxylated derivatives on the methoxyresorufin O-demethylase activity catalyzed by cDNA-expressed human cytochromes P450 (CYP)1A1 and 1A2 were examined. Flavone was a less potent inhibitor of CYP1A1 (IC50 = 0.14 microM) than CYP1A2 (IC50 = 0.066 microM). Four hydroxylated flavone derivatives (3-hydroxy-, 5-hydroxy-, 7-hydroxy-, and 3,7-dihydroxyflavone) were also potent inhibitors of CYP1A1 (IC50 < 0.1 microM) and CYP1A2 (IC50 < 0.3 microM). For CYP1A1, 7-hydroxyflavone exhibited a competitive mode of inhibition, with a Ki value of 0.015 microM and 6-fold selectivity for CYP1A1 over CYP1A2. 3,5,7-Trihydroxyflavone (galangin) showed the highest potency toward CYP1A2. The inhibition by galangin of the methoxyresorufin O-demethylase activity of CYP1A2 was mixed-type, with a Ki value of 0.008 microM. Galangin showed 5-fold selectivity in its inhibition of CYP1A2 over CYP1A1. The results indicate that some flavonoids have high potencies and selectivities for inhibition of CYP1A isozymes. This may have important implications for cancer prevention, as well as other pharmacological and toxicological effects of these compounds.

How flavonoids like Galangin by inhibiting COX-2 Enzymes can be anti-carcinogenic:

Mutat Res. 2004 Jul 13;551(1-2):245-54.

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Effect of flavonoids and vitamin E on cyclooxygenase-2 (COX-2) transcription.

O'Leary KA, de Pascual-Tereasa S, Needs PW, Bao YP, O'Brien NM, Williamson G.

Institute of Food Research, Norwich Research Park, Colney, Norwich NR4 7UA, UK.

Cyclooxygenase-2 (COX-2)-catalysed synthesis of prostaglandin E2 plays a key role in inflammation and its associated diseases, such as cancer and cardiovascular disease. There are numerous reports demonstrating that flavonoids inhibit COX-2 activity. However, transcriptional regulation of COX-2 can also be important. Nobiletin, amentoflavone, quercetin, quercetin penta-acetate, flavone, resveratrol, apigenin, chrysin, kaempferol, galangin, and genistein have been reported to modulate COX-2 transcription in a wide variety of systems. Here, we briefly review the literature on regulation of COX-2 transcription by flavonoids, and report some new preliminary data on Vitamin E and quercetin conjugates. Quercetin, quercetin 3-glucuronide, quercetin 3'-sulfate and 3'methylquercetin 3-glucuronide reduced COX-2 mRNA expression in both unstimulated and interleukin-1beta stimulated colon cancer (Caco2) cells. Quercetin and quercetin 3'-sulfate, unlike quercetin 3-glucuronide and 3'methylquercetin 3-glucuronide, also inhibited COX-2 activity. In contrast, tocopherols (alpha-tocopherol, alpha-tocopherol acetate, and gamma-tocopherol at 10microM) did not affect COX-2 mRNA expression in unstimulated Caco2 cells. However, the tocopherols inhibited COX-2 activity showing that the tocopherols act post-transcriptionally on activity, whereas quercetin and some quercetin conjugates affect both the transcription and activity of COX-2. Flavonoid modulation of COX-2 transcription may therefore be an important mechanism in anti-carcinogenesis.

 

Anti-atherogenic:

Lowering serum lipids like cholesterol and triglycerides helps prevent atherosclerosis. The following articles address this property of lesser galangal due to pancreatic lipase inhibition:

Biol Pharm Bull. 2004 Jan;27(1):138-40.

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5-Hydroxy-7-(4'-hydroxy-3'-methoxyphenyl)-1-phenyl-3-heptanone: a pancreatic lipase inhibitor isolated from Alpinia officinarum.

Shin JE, Han MJ, Song MC, Baek NI, Kim DH.

Department of Food Science, Kyung Hee University, 1 Hoegi-Dong, Dongdaemun-Gu, Seoul 130-701, Korea.

A pancreatic lipase inhibitor, 5-hydroxy-7-(4'-hydroxy-3'-methoxyphenyl)-1-phenyl-3-heptanone (HPH), from the rhizome of Alpinia officinarum (AO) was isolated and its antihyperlipidemic activity was measured. HPH inhibited a pancreatic lipase with an IC(50) value of 1.5 mg/ml (triolein as a substrate). HPH significantly lowered the serum TG level in corn oil feeding-induced triglyceridemic mice, and reduced serum triglyceride (TG) and cholesterol in Triton WR-1339-induced hyperlipidemic mice. However, HPH did not show hypolipidemic activity in high cholesterol diet-induced hyperlipidemic mice. Based on these findings, we propose that PL inhibitors may be effective as hypolipidemic agents.

Pancreatic Lipase inhibition again

Biol Pharm Bull. 2003 Jun;26(6):854-7.

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3-Methylethergalangin isolated from Alpinia officinarum inhibits pancreatic lipase.

Shin JE, Joo Han M, Kim DH.

Department of Food Science, Kyung Hee University, 1 Hoegi, Dongdaemun-ku, Seoul 130-701, Republic of Korea.

The pancreatic lipase inhibitory activity of the rhizome of Alpinia officinarum (AO) and its antihyperlipidemic activity were measured. When the water extract of AO was fractionated stepwise with organic solvents, the ethyl acetate fraction exhibited the most potent inhibition. 3-Methylethergalangin was isolated from that fraction as an inhibitor of pancreatic lipase with an IC(50) value of 1.3 mg/ml (triolein as a substrate). AO and its ethyl acetate fraction significantly inhibited the serum TG level in corn oil feeding-induced triglyceridemic mice, and serum triglyceride (TG) and cholesterol in Triton WR-1339-induced hyperlipidemic mice. However, this compound and the AO ethyl acetate fraction did not show hypolipidemic activity in high cholesterol diet-induced hyperlipidemic mice. The results suggest that the hypolipidemic activity of AO and 3-methylethergalangin is due to the inhibition of pancreatic lipase.

To review the added mechanisms of anti-atherogenesis of diminished lipid peroxidation and free radical formation; free radical scavenging; inhibition of inflammatory component of plaque formation return to these topics presented earlier in the library under anti-inflammatory, antioxidant and tumor suppressive/cancer preventive sections.

Natural antibiotic properties of Lesser Galangal:

 

Microbiol Res. 2003;158(4):281-9.

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Assessment of the antibacterial activity of selected flavonoids and consideration of discrepancies between previous reports.

Cushnie TP, Hamilton VE, Lamb AJ.

School of Pharmacy, The Robert Gordon University, Schoolhill, Aberdeen, AB10 1FR, UK.

Activity of the flavonoids apigenin, baicalin and galangin against sensitive and antibiotic resistant strains of Staphylococcus aureus, Enterococcus faecalis, E. faecium, Escherichia coli and Pseudomonas aeruginosa was investigated. Using an agar dilution assay, galangin was shown to have a minimum inhibitory concentration (MIC) of 25 to 50 microg/mL against all six strains of S. aureus but negligible activity against the other species. Apigenin displayed only marginal activity against S. aureus and no activity was detected from baicalin. In inhibition curve studies, galangin caused a 100,000-fold decrease in the viability of a growing population of S. aureus NCTC 6571 within the first two hours of treatment. Decreases in viability of S. aureus NCTC 11561 and NCIMB 9968 populations were also observed.

 

Galangin has substantial antibacterial and antifungal properties:

 

J Ethnopharmacol. 1997 Aug;57(3):177-81.

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The antimicrobial activity of 3,5,7-trihydroxyflavone (GALANGIN) isolated from the shoots of Helichrysum aureonitens.

Afolayan AJ, Meyer JJ.

Department of Botany, University of Pretoria, South Africa.

Extracts from Helichrysum aureonitens are used topically by the indigenous people of South Africa against infections. The antimicrobial activity-guided fractionation by bioautography of the acetone extract from the aerial parts of H. aureonitens led to the isolation of 3,5,7-trihydroxyflavone GALANGIN. Evaluation of the antibacterial activity of the compound against ten randomly selected bacteria indicated significant activity against all the Gram-positive bacteria tested with the minimum inhibitory concentration (MIC) ranging from 0.1 to 0.5 mg/ml. The compound was not active on Gram-negative bacteria except for Enterobacter cloacae which was significantly inhibited at an MIC of 0.1 mg/ml. Galangin indicated considerable activity against the fungi tested with the exception of Cladosporium herbarum. Penicillium digitatum and P. italicum appeared to be particularly susceptible at a concentration of 0.01 mg/ml.

 

The flavonoids discussed below except rutin are in Lesser Galangal (Galangin, Kaempherol, and Quercitin):

 

Biosci Biotechnol Biochem. 2002 May;66(5):1009-14.

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Rutin-enhanced antibacterial activities of flavonoids against Bacillus cereus and Salmonella enteritidis.

Arima H, Ashida H, Danno G.

Division of Life Science, Graduate School of Science and Technology, Kobe University, Japan.

The antibacterial activities of flavonoids were found by the paper disk method to be enhanced by combining or mixing them (as found naturally in the whole plant rhizome of Lesser Galangal) The combinations of quercetin and quercitrin, quercetin and morin, and quercetin and rutin were much more active than either flavonoid alone. Although rutin did not show activity in itself, the antibacterial activities of quercetin and morin were enhanced in the presence of rutin. The antibacterial activities of flavonoids, in combination with morin and rutin, were evaluated, based on the minimum inhibition concentration (MIC) in a liquid culture, by using Salmonella enteritidis and Bacillus cereus as the test bacteria. The activities of galangin, kaempherol, myricetin and fisetin were each enhanced in the presence of rutin when S. enteritidis was used as the test bacterium. The MIC value for kaempherol was markedly decreased by the addition of rutin. Morin inhibited DNA synthesis, and this effect was promoted by rutin at a concentration of 25 microg/ml.

 

FEMS Microbiol Lett. 2004 Nov 1;240(1):111-6.

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Galangin expresses bactericidal activity against multiple-resistant bacteria: MRSA, Enterococcus spp. and Pseudomonas aeruginosa.

Pepeljnjak S, Kosalec I.

Institute of Microbiology, Faculty of Pharmacy and Biochemistry, University of Zagreb, Schrottova 39/I, HR-10 000 Zagreb, Croatia.

The antimicrobial activity of three propolis ethanol extracts (EEP) was examined for various Gram-negative and Gram-positive bacterial species, including multiple-resistant Staphylococcus aureus, Enterococcus spp. and Pseudomonas aeruginosa strains. EEP had a good bactericidal activity against Gram-positive species, and all multiple-resistant bacterial strains tested were sensitive to EEP. Minimal inhibitory concentrations (MICs) were lower in samples of higher flavonoid content (from 0.65 to 7.81 mg mL(-1)), indicating the influence of the concentration of some potent bactericidal compound(s) in propolis or synergism among some bactericidal compounds.
Antimicrobial-guided separation of flavonoid aglycones (bioassay in situ on thin-layer chromatogram) showed that galangin (3,5,7-trihydroxyflavone) is one compound in EEP with bactericidal activity. Galangin was isolated by preparative chromatography. After determining the quantity present, the MIC against multiple-resistant bacteria was determined. The MIC of galangin against multiple-resistant bacterial strains was significantly lower (from 0.16 to 0.44 mg mL(-1), p < 0.05) than that of EEP. The bactericidal activity of galangin against P. aeruginosa strains was present at 0.17+/-0.05 mg mL(-1).

 

Antiviral properties of Galangal, one of the flavonoids from Lesser Galangal:

J Ethnopharmacol. 1997 Apr;56(2):165-9.

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Antiviral activity of galangin isolated from the aerial parts of Helichrysum aureonitens.

Meyer JJ, Afolayan AJ, Taylor MB, Erasmus D.

Department of Botany, University of Pretoria, South Africa. Marion@scientia.up.ac.za

The in vitro antiviral activity of galangin (3,5,7-trihydroxyflavone), the major antimicrobial compound isolated from the shoots of Helichrysum aureonitens, was investigated against herpes simplex virus type 1 (HSV-1), coxsackie B virus type 1 (Cox B1), adenovirus type 31 (Ad31) and reovirus. At concentrations ranging from 12-47 micrograms/ml galangin showed significant antiviral activity against HSV-1 and CoxB1, limited activity against reovirus, and no antiviral activity against Ad31.

 

The lower the mean inhibitory concentration, the more potent the substance is. Galangin (3,5,7-trihydroxyflavone) was most potent:

 

·         J Pharm Pharmacol 2001 Dec;53(12):1729.

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Vancomycin resistance reversal in enterococci by flavonoids.

Liu LX, Durham DG, Richards RM.

School of Pharmacy, Faculty of Health and Social Care, The Robert Gordon University, Aberdeen, UK.

The development of clinical Vancomycin-resistant strains of enterococci (VRE) is a major cause for concern. Here we show that a combination of galangin or 3,7-dihydroxyflavone with Vancomycin may be used to sensitize resistant strains of Enterococcus faecalis and Enterococcus faecium to the level of vancomycin-sensitive strains. Minimum inhibitory concentrations (MICs) and viable counts were determined in Iso-sensitest broth using a microtitre method. MICs of vancomycin against 67% of resistant clinical isolates and a type strain of enterococci were lowered from > 250 microg mL(-1) to < 4 microg mL(-1) in the presence of galangin (12.5 microg mL(-1)) or 3,7-dihydroxyflavone (6.25 microg mL(-1)). Viable counts for type culture E. faecalis ATCC 51299 showed the flavonoids alone significantly lowered numbers of colony forming units (CFUs). CFUs were maintained at low levels (< 10(3) CFU mL(-1)) for 24 h by vancomycin/flavone combinations. This combinational action in reversing vancomycin resistance of enterococci highlights novel drug targets and has importance in the design of new therapeutic regimes against resistant pathogens.

 

Indian J Exp Biol. 1975 Jul;13(4):409.

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New antifungal substance from Alpinia officinarum Hance.

Ray PG, Majumdar SK.

PMID: 1205540 [PubMed - indexed for MEDLINE]

No Abstract Available 

Flavonoids in Lesser Galangal may work against the parasite causing Chagas Disease: 

 

Phytomedicine. 2003;10(6-7):490-3.

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Trypanocidal activity of Lychnophora staavioides Mart. (Vernonieae, Asteraceae).

Takeara R, Albuquerque S, Lopes NP, Lopes JL.

Departamento de Fisica e Quimica, Faculdade de Ciencias Farmaceuticas de Ribeirao Preto-USP, Ribeirao Preto, SP, Brazil.

In the continuing search for new compounds with trypanocidal activity for use in blood banks to prevent the transmission of Chagas' disease, a trypanocidal extract of Lychnophora staavioides Mart. (Vernonieae, Asteraceae) was fractionated using several chromatographic techniques and afforded the following flavonoids: tectochrysin, pinostrobin, pinobanksin, pinobanksin 3-acetate, pinocembrin, chrysin, galangin 3-methyl ether, quercetin 3-methyl ether, chrysoeriol and vicenin-2. The most active compound was quercetin 3-methyl ether, which showed no blood lysis activity and which represents a promising compound for use against T. cruzi in blood banks.

 

As an antiemetic (stops nausea and vomiting):

 

J Nat Prod. 2002 Sep;65(9):1315-8.

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Antiemetic principles of Alpinia officinarum.

Shin D, Kinoshita K, Koyama K, Takahashi K.

Department of Pharmacognosy and Phytochemistry, Meiji Pharmaceutical University, Noshio 2-522-1, Kiyose-shi, Tokyo 204-8588, Japan.

Bioasay-guided fractionation of the antiemetic constituents of Alpinia officinarum was performed, and eight compounds (1-8) including a new compound were isolated. Among the seven known compounds, two flavonoids (1, 2), four diarylheptanoids (3, 5, 6, 8), and one sterol (4) were obtained, with five (2-6) of those compounds showing antiemetic activity in a copper sulfate induced emesis assay in young chicks. The structure of the new compound 7, which also showed antiemetic activity, was determined as 5-hydroxy-7-(4-hydroxy-3-methoxyphenyl)-1-(4-hydroxyphenyl)-3-heptanone. The structure of 7 was established on the basis of spectroscopic data interpretation.

How natural substances like Lesser Galangal may actually work to facilitate pharmaceuticals against cancer, and also protect against development of resistance to drug efficacy in cancer treatment:

Drug Metab Rev. 2004 Feb;36(1):57-104.

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Herbal modulation of P-glycoprotein.

Zhou S, Lim LY, Chowbay B.

Department of Pharmacy, Faculty of Science, National University of Singapore, Singapore. phazsf@nus.edu.sg

P-glycoprotein (Pgp) is a 170 kDa phosphorylated glycoprotein encoded by human MDR1 gene. It is responsible for the systemic disposition of numerous structurally and pharmacologically unrelated lipophilic and amphipathic drugs, carcinogens, toxins, and other xenobiotics in many organs, such as the intestine, liver, kidney, and brain. Like cytochrome P450s (CYP3A4), Pgp is vulnerable to inhibition, activation, or induction by herbal constituents. This was demonstrated by using an ATPase assay, purified Pgp protein or intact Pgp-expressing cells, and proper probe substrates and inhibitors. Curcumin, ginsenosides, piperine, some catechins from green tea, and silymarin from milk thistle were found to be inhibitors of Pgp, while some catechins from green tea increased Pgp-mediated drug transport by heterotropic allosteric mechanism, and St. John's wort induced the intestinal expression of Pgp in vitro and in vivo. Some components (e.g., bergamottin and quercetin) from grapefruit juice were reported to modulate Pgp activity. Many of these herbal constituents, in particular flavonoids, were reported to modulate Pgp by directly interacting with the vicinal ATP-binding site, the steroid-binding site, or the substrate-binding site. Some herbal constituents (e.g., hyperforin and kava) were shown to activate pregnane X receptor, an orphan nuclear receptor acting as a key regulator of MDR1 and many other genes. The inhibition of Pgp by herbal constituents may provide a novel approach for reversing multidrug resistance in tumor cells, whereas the stimulation of Pgp expression or activity has implication for chemoprotective enhancement by herbal medicines. Certain natural flavonols (e.g., kaempferol, quercetin, and
galangin) are potent stimulators of the Pgp-mediated efflux of 7,12-dimethylbenz(a)-anthracene (a carcinogen). The modulation of Pgp activity and expression by these herb constituents may result in altered absorption and bioavailability of drugs that are Pgp substrates. This is exemplified by increased oral bioavailability of phenytoin and rifampin by piperine and decreased bioavailability of indinavir, tacrolimus, cyclosporine, digoxin, and fexofenadine by coadministered St. John's wort. However, many of these drugs are also substrates of CYP3A4. Thus, the modulation of intestinal Pgp and CYP3A4 represents an important mechanism for many clinically important herb-drug interactions. Further studies are needed to explore the relative role of Pgp and CYP3A4 modulation by herbs and the mechanism for the interplay of these two important proteins in herb-drug interactions.

 

History and anecdotal attributes described of Lesser Galangal

SERIE CODE:R16·Lesser Galangal Rhizoma P.E.(10:1)Alpiniae Officinarum P.E.What is Galangal(Alpiniae Officinarum.,Lesser Galangal)?What is Kaempferia Galanga. Arabic Khalanjan ginger?Origin,narrative history and modern application of Galangal and Lesser Galangal Rhizoma Extracts?


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Posted by michael derrida on March 10, 19104 at 23:00:14:

SERIE CODE:R16·Lesser Galangal Rhizoma P.E.(10:1)Alpiniae Officinarum P.E.What is Galangal(Alpiniae Officinarum.,Lesser Galangal)?What is Kaempferia Galanga. Arabic Khalanjan ginger?Origin,narrative history and modern application of Galangal and Lesser Galangal Rhizoma Extracts?


Composition&Application:
Properties:Sweet in flavour,Sweet and neutral, neutral in property;acting on the spleen and lung channels.Invigorates the spleen.Replenishes the middle-jiao energy.Promotes the production of normal body fluids. Nourishes the blood.Promotes production of body fluid and blood circulation.

What is Galangal(Alpiniae Officinarum.,Lesser Galangal)?What is Kaempferia Galanga. Arabic Khalanjan ginger?Origin,narrative history and modern application of Galangal and Lesser Galangal Rhizoma Extracts?

Botanical Basic Data:Galangal

Botanical: Alpinia officinarum (HANCE.),Lesser Galangal.
Family: N.O. Zingaberaceae or Scilaminae
Latin: Rhizoma Alpiniae Officinarum.
Synonyms---Galangal,Galanga. China Root. India Root. East India Catarrh Root. Lesser Galangal. Rhizoma Galangae. Gargaut. Colic Root. Kaempferia Galanga. Arabic Khalanjan ginger.mild ginger.the Chinese Ko-liang-kiang,the mild ginger from Ko.
Part Used---Dried rhizome(dried root).Galangal.
Habitat---China,Java,India.

Origin of Galangal(Alpiniae Officinarum.,Lesser Galangal):
The rhizome of Alpinia officinarum Hance, a perennial plant, of the family Zingiberaceae. It is much like ginger, its use into curry's, stew and every dish where ginger is used.In China, it is mainly produced in Guangdong, Guangxi, Taiwan, etc.
Harvested at the turn of summer and autumn, the rhizome that has grown for 4 to 6 years is dug up and picked for use. Procedure: Remove the stems, fibrous roots and remaining scales above the ground from the rhizome, wash it clean, cut it into lengths and dry it in the sun for use when raw.

Description of Galangal(Alpiniae Officinarum.,Lesser Galangal):
The genus Alpinia was named by Plumier after Prospero Alpino, a famous Italian botanist of the early seventeenth century. The name Galangal is derived from theArabic Khalanjan, perhaps a perversion of a Chinese word meaning 'mild ginger.'
The drug has been known in Europe for seven centuries longer than its botanical origin, for it was only recognized in 1870, when specimens were examined that had been found near Tung-sai, in the extreme south of China, and later, on the island of Hainan, just opposite. The name of Alpinia officinarum was given to the herb, as the source of Lesser Galangal.

The Greater Galangal is a native of Java (A. Galanga or Maranta Galanga), and is much larger, of an orange-brown colour, with a feebler taste and odour. It is occasionally seen at London drug sales, but is scarcely ever used. There is also a resemblance to A. calcarata.The herb grows to a height of about 5 feet, the leaves being long, rather narrow blades, and the flowers, of curious formation, growing in a simple, terminal spike, the petals white, with deep-red veining distinguishing the lippetal.
The branched pieces of rhizome are from 1 1/2 to 3 inches in length, and seldom more than 3/4 inch thick. They are cut while fresh, and the pieces are usually cylindrical, marked at short intervals by narrow, whitish, somewhat raised rings, which are the scars left by former leaves. They are dark reddish-brown externally, and the section shows a dark centre surrounded by a wider, paler layer which becomes darker in drying.
Their odour is aromatic, and their taste pungent and spicy. They are tough and difficult to break, the fracture being granular, with small, ligneous fibres interspersed throughout one side. The drug is exported, chiefly from Shanghai, in bales made of split cane, plaited, and bound round with cane. The root has been used in Europe as a spice for over a thousand years, having probably been introduced by Arabian or Greek physicians, but it has now largely gone out of use except in Russia and India. Closely resembling ginger, it is used in Russia for flavouring vinegar and the liqueur 'nastoika': it is a favourite spice and medicine in Lithuania and Esthonia. Tartars prepare a kind of tea that contains it, and it is used by brewers. The reddishbrown powder is used as snuff, and in India the oil is valued in perfumery.

Properties: Pungent in flavor, hot in nature, it is related to the spleen and stomach channels.

Constituents of Galangal(Alpiniae Officinarum.,Lesser Galangal):
The root contains a volatile oil, resin, galangol, kaempferid, galangin and alpinin, starch, etc. The active principles are the volatile oil and acrid resin. Galangin is dioxyflavanol, and has been obtained synthetically. Alcohol freely extracts all the properties, and for the fluid extract there should be no admixture of water or glycerin.
Medicinal Action and Uses of Galangal(Alpiniae Officinarum.,Lesser Galangal): Stimulant and carminative. It is especially useful in flatulence, dyspepsia, vomiting and sickness at stomach, being recommended as a remedy for sea-sickness. It tones up the tissues and is sometimes prescribed in fever. Homoeopaths use it as a stimulant. Galangal is used in cattle medicine, and the Arabs use it to make their horses fiery. It is included in several compound preparations, but is not now often employed alone.

Functions: Dispels cold, kills pain, warms the spleen and stomach and arrests coughing. The powder is used as a snuff for catarrh.

Applications of Galangal(Alpiniae Officinarum.,Lesser Galangal):
1. To treat cold pain in the abdomen due to stomach-cold:
This herb is always used in mutual enforcement with blast-fried ginger, e.g., Er Jiang Wan.
2. To treat distending pain in the abdomen due to stomach-cold and stagnation of liver-qi:
This herb is mostly used together with nutgrass flatsedge rhizome (Rhizoma Cyperi) in order to soothe the liver, regulate the circulation of qi, dispel cold and relieve pain, e.g., Liang Fu Wan.
3. To treat vomiting due to stomach-cold:
This herb can be used together with dangshen (Radix Codonopsis Pilosulae), tuckahoe (Poria Cocos), largehead atractylodes rhizome (Rhizoma Atractylodis Macrocephalae), etc.

Modern Researches of Galangal(Alpiniae Officinarum.,Lesser Galangal):
This herb contains a volatile oil with cineole and methyl cinnamate as its main ingredients. It also contains galangin, galangol, etc.
The 0.25% or 0.75% water decoction of this herb can stimulate isolated intestinal ducts. Its 1% or 0.2% water decoction and the saturated water solution of its volatile oil have inhibitory effects.
The decoction of this herb can inhibit anthrax bacillus, Bacillus Diphtheriae, hemolytic streptococcus, hay bacillus, Diplococcus pneumoniae, Staphylococcus aureus, Mycobacterium tuberculosis hominis, etc., to different extents.
Dosage---From 15 to 30 grains in substance, and double in infusion. Fluid extract, 30 to 60 minims.

Scientific References:

1.What is Galangal(Alpiniae Officinarum.,Lesser Galangal)?What is Kaempferia Galanga. Arabic Khalanjan ginger?Origin,narrative history and modern application of Galangal and Lesser Galangal Rhizoma Extracts?Via Michael Derrida

SERIE CODE:R16
·Lesser Galangal Rhizoma P.E. (10:1)Alpiniae Officinarum P.E.

Editor’s Conclusion: In conclusion of this library, the editor wishes to urge the readers to continue their vigilance on this and other topics in alternative therapeutics, supplements, and preventics. Many pharmaceutical products (drugs) of great value began with the discovery of a plant that when chewed, soaked in hot water to make tea, tinctured from soaking in alcohol, extracted using other solvents, or ground into powder and ingested, or applied to the skin, had profound healing effects.  

One is urged to explore libraries similar to this one on plant remedies such as bloodroot, olive leaf extract, Aloe vera, and Stevia rebaudiana.  Additional alternative remedies have been found in replenishing trace minerals often deficient in modern diets.  Examples to be noted especially include special attention to zinc and chromium. 

Another important point to consider when reading about these remedies is that with every plant remedy, there are specific chemical compounds, which may act to generate similar results, but through vastly different mechanisms biochemically.  The significance of this fact is that when combined, many of these plant remedies will work synergistically to potentiate each other in a manner similar to that found in some research quoted in this library when plant remedies are combined with drugs. 

In general the reader must realize that remedies derived from the whole plant as nature designed them have less toxic potential downsides than highly chemically engineered derivatives consisting of single active ingredients. 

As a reader of this library, we urge you to continue your investigation into the science behind the advocacy of nature’s alternatives to pharmaceuticals.  We are not advocating the abandonment of pharmaceutical products in elucidating these natural wonders. Rather as many of the papers show, drugs can be combined with natural remedies to enhance the effects of both.  Also, sometimes drugs are mandatory interventions, while other times natural remedies may obviate the need for some drugs in some circumstances. 

The reader should be made aware that there is an insidious movement to limit people’s access to natural remedies in the form of vitamins, minerals, and herbal supplements based upon spurious claims and false science.  The tragedy is that the effort to establish world wide regulatory authority over the availability and cost of these natural remedies, may if unchecked, lead to a complete lack of availability.  We urge the reader to become familiar with the CODEX REGULATIONS now in force in some European countries and the effort through the World Health Organization to extend their regulatory authority into the United States of America.  

Anyone who is impressed by the reality of the science proving the safety and efficacy of herbal or medicinal plant products will have to actively fight to preserve the right of access.  This library is not written for political purposes, and this notice is simply our effort to bring about awareness that just because remedies may now be available from carefully regulated companies, things could change, if we as consumers remain ignorant and complacent. 

As you will find by reading through this library, these remarkable works of nature not only heal, but by their function in supplementing components for immune, endocrine, circulatory, neural, hematopoietic, gastrointestinal function, they are truly nutritional in the fullest sense, and are also preventive of disease induction through the replenishment of dietary deficiency and/or imbalances created by the high concentration of processed foods consumed in today’s society.
 

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