Research Update:Puerarin:8-beta-D-Glucopyranosyl-7-hydroxy-3-(4-hydroxyphenyl)-4H-1-.:Introduction and Its Benefit Applications.C-glycoside,Anti-Cancer,Antioxidant.Serie No.:Pure07.Pure Phytochemical Series.MDidea Extracts Professional.

Puerarin:8-beta-D-Glucopyranosyl-7-hydroxy-3-(4-hydroxyphenyl)-4H-1-;C-glycoside,Anti-Cancer,Antioxidant photo picture image img

Phytochemical info of Puerarin:8-beta-D-Glucopyranosyl-7-hydroxy-3-(4-hydroxyphenyl)-4H-1-:

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Definition: from Pueraria root Extract are majorly composed of .
Chemical information disclosed as following table:

Research and findings of Pueraria root.kudzu root and Pueraria root extract.:

High-performance liquid chromatography-tandem mass spectrometry for identification of isoflavones and description of the biotransformation of kudzu root.:

Anal Bioanal Chem. 2005; 383(5):787-96 (ISSN: 1618-2642).Zhang Y; Xu Q; Zhang X; Chen J; Liang X; Kettrup A.Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian, 116023, PR China.
High-performance liquid chromatography-tandem mass spectrometry has been used to identify isoflavone aglycones and glycosides in kudzu root. Fourteen isoflavones were detected. Among these, six were identified by comparison with authentic standards. Tentative identifications of the other isoflavones are based on UV spectra, mass spectra of protonated and deprotonated molecules, and MS-MS data. Several are reported for the first time in kudzu root. The bioactivity and bioavailability of isoflavone aglycones are usually greater than those of their glycosides. To improve the bioavailability of kudzu root isoflavones, crude beta-glycosidases prepared from microbes were used to hydrolyze the isoflavone glycosides. Several MS modes are combined not only to identify the isoflavones in kudzu root, but also to describe the biotransformation of kudzu root isoflavone glycosides. It is also proved that crude beta-glycosidases have high selectivity toward the O-glycosides of isoflavones.

Possible developmental and reproductive toxicity of isoflavones in soybean and Kudzu root.:

Asia Pac J Clin Nutr. 2005; 14 Suppl:S105 (ISSN: 0964-7058).Guan L; Chen ZY.Food and Nutritional Sciences, Chinese University of Hong Kong, Shatin, N.T., Hong Kong.
Background - Numbers of researches over the last decades have suggested protective effects of soybean compounds against some chronic diseases, the root of Kudzu had been used to treat coronary heart disease, heart failure, and hypertension in Asian countries. It is found that the major effective component of the two plants is isoflavones, which possess both estrogenic and anti-estrogenic activity. However, a number of side effects have been also postulated, as well as mechanisms by which such effects may be mediated. Objective - To investigate the possible developmental and reproductive toxicity of isoflavones in soybean and the root of Kudzu. Design - SD rats (4 weeks of age) were used as an animal model to study the potential developmental and reproductive toxicity of isoflavones to immature animals. Both male and female rats were gastrogavaged daily with different doses of isoflavone extracts from soybean and kudzu root (30, 150, 300, and 600 mg/kg body weight), respectively, for three months. Outcome - Feeding for 3 months led to reduced body weight gain compared with the control group in both genders with dose-related relationship. Administration of soybean and kudzu root isoflavones also caused an increased relative weight of main reproductive organs in both genders. The two kinds of isoflavones could decrease both estrodial and progesterone concentrations statistically in female rats with the increasing dosage. For soybean isoflavones, both estrodial and progesterone levels in high dose group (600 mg/kg body weight) would be reduced by 72% and 45%, respectively, compared with the controls. Male rats had not only total testosterone levels but also sperm count significantly decreased by 64% and 50%, respectively, in high dose group compared with the control group administered with the soybean isoflavones. Conclusions - High dose of isoflavones affected not only growth but also development of reproductive system at least in rats.

Analysis of the estrogenic components in kudzu root by bioassay and high performance liquid chromatography.:

J Steroid Biochem Mol Biol. 2005; 94(4):375-81 (ISSN: 0960-0760).Zhang Y; Chen J; Zhang C; Wu W; Liang X.Dalian Institute of Chemical Physics, Chinese Academy of Sciences, 161 Zhongshan Road, Dalian 116011, PR China.
The estrogenic activity of the Chinese herb kudzu root was investigated by a recombinant yeast screening assay (YES). Isoflavones are the main components in the plant, of which puerarin is the most abundant one. The kudzu root extract was separated into four fractions according to the polarity. The crude extract and its sub-fractions, except the water fraction, showed clear estrogenic activity and the potencies were in the range of 10(-3) to 10(-1)g/l. The ligand potency was used to compare the estrogenic activity of these fractions. The crude extract and its sub-fractions were further analyzed by high performance liquid chromatography (HPLC) to correlate the activity and the active components. Bioassay and chemical analysis showed that theoretical estrogenic activity expressed as equivalent 17beta-estradiol concentration or the cumulative effects are comparable to that experimentally determined by YES. The results showed that the high content of isoflavones as well as the high estrogenic activity could make kudzu root extract an interesting candidate for hormone replacement therapy.

Quantitative analysis of phytoestrogens in kudzu-root, soy and spiked serum samples by high-pressure liquid chromatography.:

Biomed Chromatogr. 2004; 18(6):367-80 (ISSN: 0269-3879).Benlhabib E; Baker JI; Keyler DE; Singh AK.Department of Veterinary Diagnostic Medicine, College of Veterinary Medicine, University of Minnesota, St Paul Campus, 1333 Gortner Ave, St Paul, MN 55108, USA.
A sensitive and reliable HPLC method that allows simultaneous quantification of phytoestrogens extracted from kudzu-root and soy preparations, and serum samples has been developed. Kudzu-root and soy preparations were mixed with 5 microg flavone and 15 microg rutin (internal standards) and the phytoestrogens were extracted by using solid-phase (C18) extraction cartridges. Blank or spiked serum samples were extracted by using either C18 cartridges or trichloroacetic acid-methanol extraction. The extracts were analyzed by the HPLC equipped with a reverse-phase (250 x 4 mm, C18) column and UV, diode-array or MS detector. A linear gradient of acetic acid and acetonitrile provided excellent separation of glycoside and aglycone-phytoestrogens from kudzu root and soy preparations. The C18 cartridge extraction of serum yielded excellent recovery of both glycoside- and aglycone-phytoestrogens, while the trichloroacetic acid-methanol extraction yielded excellent recovery of glycoside but poor recovery of aglycone compounds. UV and MS detectors were suitable for phytoestrogen analysis in plant and serum samples, while the diode-array detector was suitable for generating the UV absorbance curve for phytoestrogens.

Optimization of high performance liquid chromatographic method for analysis of kudzu root crude extract.:

Se Pu. 2006; 24(4):354-8 (ISSN: 1000-8713).Zhang Y; Xue X; Xu Q; Zhang F; Liang X.Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, China. zhangyanzy@dicp.ac.cn
Kudzu root is an important traditional Chinese herb. Its crude extract has been used in the treatment of hypertension and angina pectoris in China. Several parameters for high performance liquid chromatography (HPLC) analytical method for kudzu root extract, including HPLC model, mobile phase, additive and gradient conditions have been optimized. The HPLC retention parameters a and c, and the peak shape parameters sigma and tau of 25 chromatographic peaks were obtained accurately and rapidly using five linear gradients and were calculated using CSASS software. The CSASS software was then used to simulate the gradient conditions in the experiments, and the optimized condition was obtained. The comparison of the simulated and real chromatogram profiles showed that the potential of simulation using the CSSASS software as compared to that of the real experimental conditions was precise. Reversed-phase HPLC model and the mobile phase of (A) acetonitrile containing 0.1% (v/v) acetic acid and (B) water containing 0.1% (v/v) acetic acid were used. The optimized gradient profile showed a linear increase as follows: from 5% A to 35% A at 0 - 33 min; from 35% A to 100% A at 33 - 50 min, and then the HPLC system was held for 5 min. The reproducibility and precision of the method were investigated. The relative standard deviations (RSDs) of retention time, peak height, and peak area were less than 0.25%, 11%, and 4.9%, respectively, which showed that the method was stable, reliable, and reproducible.

* Kudzu root extract suppresses voluntary alcohol intake and alcohol withdrawal symptoms in P rats receiving free access to water and alcohol.:

J Med Food. 2004; 7(2):168-79 (ISSN: 1096-620X).Benlhabib E; Baker JI; Keyler DE; Singh AK.Department of Veterinary Diagnostic Medicine, College of Veterinary Medicine, University of Minnesota, 1333 Gortner Avenue, St. Paul, MN 55108, USA.
Alcohol-preferring (P) rats, given free choice to drink water or 15% alcohol, drank 7-10 g of alcohol/kg/day, giving blood alcohol values ranging from 16 to 24 mg/dL. Body weight and food and total fluid intake values in control and alcohol-drinking P rats did not differ significantly, while water intake was inversely related to the amount of alcohol consumed. Alcohol withdrawal after 50 days of alcohol drinking caused withdrawal symptoms such as hypersensitivity, poor landing coordination, and tremors. A daily 0.5, 0.75, and 1.0 g/kg dose of kudzu root (KdR) did not affect body weight and food and water intake values in control (no alcohol) P rats. Subchronic feeding of relatively higher KdR doses (0.75 and 1.0 g/kg) caused a 25-30% reduction in weight gain. The 0.5 g/kg KdR dose caused a 50-60% reduction in alcohol consumption, abolished the development of alcohol withdrawal symptoms, but did not affect blood alcohol levels. The higher KdR doses did not further reduce alcohol consumption. Alcohol suppressed the weight-reducing effects of KdR. The KdR extract used in this study contained 150 mg/g of puerarin, 13 mg/g of daidzin, 4 mg/g of daidzein, 3 mg/g of genistin, 0.2 mg/g of genistein, and 1 mg/g of glycetin. Blood and liver samples contained mostly puerarin and a trace amount of daidzein that may have been formed by the hydrolysis of daidzin by liver enzymes. An important observation was that brain samples obtained from KdR-fed or alcohol + KdR-fed rats did not contain any of the KdR isoflavones. Thus, KdR isoflavones suppressed alcohol drinking and withdrawal symptoms without entering the brain.

Composition, red blood cell uptake, and serum protein binding of phytoestrogens extracted from commercial kudzu-root and soy preparations.:

J Med Food. 2002; 5(3):109-23 (ISSN: 1096-620X).Benlhabib E; Baker JI; Keyler DE; Singh AK.Department of Veterinary Diagnostic Medicine, College of Veterinary Medicine, University of Minnesota, St. Paul Campus, 1333 Gortner Avenue, St. Paul, MN 55108, USA.
Kudzu-root and soy phytoestrogens have been associated with anti-cancer and anti-intoxication activities. Sales of capsules containing kudzu-root and soy extracts through health food stores and the Internet are unregulated. To compare efficacy, the amount of phytoestrogens present in commercial preparations and their fate in biological samples must be determined. In this study, the levels and composition of phytoestrogens in kudzu-root and soy extracts were studied using high-performance liquid chromatography with ultraviolet light detection. The bioavailability of phytoestrogens was studied by measuring red blood cell (RBC) uptake and serum protein binding ability. Phytoestrogen levels in acidified kudzu-root samples were 5- to 10-fold greater than those in nonacidified samples. Puerarin accounted for 80% of total phytoestrogens in kudzu-root. In soy extract, puerarin was absent while genistin, glycetein, and daidzin or daidzein were the major phytoestrogens. The RBC uptake depended on the phytoestrogen's polarity and molecular length. When serum was dialyzed with phytoestrogen standards in a buffer, the protein binding of phytoestrogens correlated negatively with their polarity. However, when serum was dialyzed with kudzu-root or soy extract, almost all of the phytoestrogens present in the extract bound to serum protein. Therefore, this study suggests differences in the bioavailability of phytoestrogens when they are ingested as purified compounds compared with crude plant extract. The differential composition of phytoestrogens in kudzu-root and soy may account for the differences in their therapeutic activities.

Effects of extracts of root of kudzu vine on mammary gland and uterus development in rats.:

Zhongguo Zhong Yao Za Zhi. 2003; 28(6):560-2 (ISSN: 1001-5302).Xue XO; Jin H; Niu JZ; Wang JF.Beijing University of Chinese Traditional Medicine, Beijing 100029, China. xxo123@163.net
OBJECTIVE: To study the effects of extracts of root of kudzu vine on mammary gland and uterus development in rats. METHOD: 40 Wistar rats weighting 65-85 g were randomly divided into 4 groups: control group, estrogen group, extracts of root of kudzu vine group of high dose, extracts of root of kudzu vine group of low dose. (10 rats in each group). After having been treated for 7 days, the rats were killed; mammary glands and uterus were removed and weighed. Serum was isolated and kept at 4 degrees C for determination of hormones. RESULT: 1. Administration of the root of kudzu vine significantly increased the weigh of mammary gland and uterus in rats. 2. Administration of the root of kudzu vine increased serum FSH, LH, E2 and decreased PRL. CONCLUSION: Extracts of root of kudzu vine could enhance the weight of mammary gland and uterus growth in rats, which may provide experimental evidence for the development of new drug used for promoting mammary gland and uterus.

A pilot study exploring the effect of kudzu root on the drinking habits of patients with chronic alcoholism.:

J Altern Complement Med. 2000; 6(1):45-8 (ISSN: 1075-5535).Shebek J; Rindone JP.Veteran Affairs Medical Center 316, Prescott, Arizona 86313, USA.
PURPOSE: The objective of this study was to assess if kudzu root extract influences the drinking habits of veterans who entered a substance abuse treatment program. DESIGN: Prospective, randomized double-blind controlled clinical trial. SETTING: A nonacademic Veteran Affairs Medical Center. METHODS: Patients with the diagnosis of alcoholism were randomly assigned to receive either kudzu root extract 1.2 g twice daily or a matching placebo. Patients completed questionnaires that focused on craving for alcohol and sobriety status on a monthly basis. OUTCOME MEASURES: Sobriety level and craving for ethanol were assessed on a visual analogue scale from 0 to 10. RESULTS: Thirty-eight patients completed 1 month of the study; 21 randomly assigned kudzu, 17 to placebo. No statistically significance difference in craving and sobriety scores were noted after 1 month between kudzu and placebo, or at later stages with smaller numbers (15-19) of patients. CONCLUSION: In this small patient population, kudzu root appeared to be no better than placebo in reducing the craving for alcohol or promoting sobriety.

Kudzu root: an ancient Chinese source of modern antidipsotropic agents.:

Phytochemistry. 1998; 47(4):499-506 (ISSN: 0031-9422).Keung WM; Vallee BL.Center for Biochemical and Biophysical Sciences and Medicine, Harvard Medical School, Boston, MA 02115 USA.
Kudzu (Pueraria lobata) is one of the earliest medicinal plants used in traditional Chinese medicine. It has many profound pharmacological actions including antidipsotropic (antialcohol abuse) activity. Although both the roots and flowers of kudzu, Radix and Flos puerariae, respectively, have been used to treat alcohol abuse safely and effectively in China for more than a millennium, their true efficacy, active constituents, sites and mechanisms of action have never been critically examined. Recently, we have demonstrated that a crude extract of Radix puerariae suppresses the free-choice ethanol intake of ethanol-preferring golden Syrian hamsters and have identified two of its isoflavones, daidzin and daidzein, that account for this effect. Since then, we and other investigators have confirmed these findings in rats that were either trained or genetically bred to prefer and consume large amounts of ethanol. This article summarizes recent progress on the pharmacological and biochemical studies of the antidipsotropic isoflavones isolated from Radix puerariae.

An extract of the Chinese herbal root kudzu reduces alcohol drinking by heavy drinkers in a naturalistic setting.:

Alcohol Clin Exp Res. 2005; 29(5):756-62 (ISSN: 0145-6008).Lukas SE; Penetar D; Berko J; Vicens L; Palmer C; Mallya G; Macklin EA; Lee DY.Behavioral Psychopharmacology Research Laboratory, McLean Hospital, Belmont, Massachusetts 02478, USA. lukas@mclean.harvard.edu
BACKGROUND: Of the available medications for treating alcohol-related problems, none are universally effective, and all have side effects that may limit their use. Extracts of kudzu containing a variety of isoflavones have been shown to reduce alcohol drinking in rats and hamsters. METHODS: The present study was designed to test the efficacy of a kudzu extract in a clinical population. Male and female "heavy" alcohol drinkers were treated with either placebo or a kudzu extract for 7 days and then given an opportunity to drink their preferred brand of beer while in a naturalistic laboratory setting. Participants served as their own controls, and order of treatment exposure was counterbalanced. Drinking behavior was monitored by a digital scale that was located in the top of an end table. RESULTS: Kudzu treatment resulted in significant reduction in the number of beers consumed that was paralleled by an increase in the number of sips and the time to consume each beer and a decrease in the volume of each sip. These changes occurred in the absence of a significant effect on the urge to drink alcohol. There were no reported side effects of kudzu treatment. CONCLUSION: These data suggest that an extract of this leguminous plant may be a useful adjunct in reducing alcohol intake in a naturalistic setting.

Regulation of isoflavone production in hydroponically grown Pueraria montana (kudzu) by cork pieces, XAD-4, and methyl jasmonate.:

Plant Cell Rep. 2006; 25(12):1387-91 (ISSN: 0721-7714).Kirakosyan A; Kaufman PB; Chang SC; Warber S; Bolling S; Vardapetyan H.Department of Cardiac Surgery, University of Michigan, Ann Arbor, MI 48109-0686, USA. pbk@umich.edu
A mini-hydroponic growing system was employed for seedlings of kudzu vine (Pueraria montana) and contents of isoflavones (daidzein, genistein, daidzin, genistin, and puerarin) from shoot and root parts of seedlings were analyzed quantitatively. In addition, exogenous cork pieces, polymeric adsorbent, XAD-4, and universal elicitor, methyl jasmonate (MeJA), were used to regulate the production of these isoflavones. It was shown that cork pieces up-regulate the production of daidzein and genistein up to seven- and eight-fold greater than the levels obtained for control roots. In contrast, levels of glucosyl conjugates, daidzin and genistin, decrease up to five- and eight-fold, respectively. Cork treatment also induces the excretion of the root isoflavone constituents into the growth medium. Minimal levels of isoflavones are absorbed by the cork pieces. XAD-4 stimulates the production of glucosyl conjugates, daidzin and genistin, in root parts about 1.5-fold greater than that obtained in control roots.
These are the highest amounts of daidzin and genistin that are observed (5.101 and 6.759 mg g(-1) dry weight, respectively). In contrast to these two adsorbents, MeJA increases the accumulation of isoflavones in shoot rather than in root parts of seedlings, about three- to four-fold over control levels, with the exception of genistein. These studies reveal new observations on the regulation of isoflavone production in hydroponically grown Pueraria montana plants by two adsorbents (cork pieces and XAD-4) and MeJA elicitor.

Identification of isoflavonoids in several kudzu samples by high-performance liquid chromatography coupled with electrospray ionization tandem mass spectrometry.:

J Chromatogr Sci. 2006; 44(2):57-63 (ISSN: 0021-9665).Fang C; Wan X; Tan H; Jiang C.Key Laboratory of Tea Biochemistry and Biotechnology, Ministry of Education and Ministry of Agriculture, P.R. China.
Pueraria lobata is a rich source of isoflavonoids. The detection and identification of isoflavonoid components from Pueraria radix (RP), callus and cell cultures, is very important for the safest and most effective use of kudzu as a medicinal plant, and for the studies on quantitative analysis and secondary metabolism of isoflavonoids in vitro cultures. Liquid chromatography is coupled with negative and positive electrospray ionization (ESI) tandem mass spectrometry (MS-MS), and photodiode array detection is used to characterize and detect isoflavonoids in root, callus, and cell samples of P. lobata. Characteristic product ions of aglycones, O-glucosides, and C-glucosides were obtained from the full-scan ESI-MS chromatography of the major peaks and the MS-MS spectra of the protonated ions. Five major components of puerarin, daidzin-6"-O-acetylester, genistin-6"-O-malonylester, biochanin A-7-O-glucoside-6"-O-malonylester, and daidzein are detected and identified from the methanolic extract of P. lobata callus cultures. The major isoflavonoid components of P. lobata cell suspension cultures are identified as puerarin, daidzin, daidzin-6"-O-acetylester, genistin-6"-O-malonylester, biochanin A-7-O-glucoside-6"-O-malonylester, genistein-8-C-glucoside-6"-O-malonylester, and daidzein, on the basis of ESI-MS and MS-MS spectra analysis. Likewise, puerarin, daidzin, genistein-6"-O-malonylester, 3'-methoxypuerarin, and daidzein are detected and identified from RP. Of those isoflavonoid components detected, daidzin-6"-O-acetylester is a new isoflavonoid glucoside and is for the first time detected from P. lobata cultures in vitro.

Evaluation of the estrogenic effects of legume extracts containing phytoestrogens.:

J Agric Food Chem. 2003; 51(8):2193-9 (ISSN: 0021-8561).Bou?? SM; Wiese TE; Nehls S; Burow ME; Elliott S; Carter-Wientjes CH; Shih BY; McLachlan JA; Cleveland TE.Agricultural Research Service, Southern Regional Research Center, U.S. Department of Agriculture, New Orleans, Louisiana 70179, USA. sboue@nola.srrc.usda.gov
Seven legume extracts containing phytoestrogens were analyzed for estrogenic activity. Methanol extracts were prepared from soybean (Glycine max L.), green bean (Phaseolus vulgaris L.), alfalfa sprout (Medicago sativa L.), mung bean sprout (Vigna radiata L.), kudzu root (Pueraria lobata L.), and red clover blossom and red clover sprout (Trifolium pratense L.). Extracts of kudzu root and red clover blossom showed significant competitive binding to estrogen receptor beta (ERbeta). Estrogenic activity was determined using an estrogen-dependent MCF-7 breast cancer cell proliferation assay. Kudzu root, red clover blossom and sprout, mung bean sprout, and alfalfa sprout extracts displayed increased cell proliferation above levels observed with estradiol. The pure estrogen antagonist, ICI 182,780, suppressed cell proliferation induced by the extracts, suggesting an ER-related signaling pathway was involved. The ER subtype-selective activities of legume extracts were examined using transiently transfected human embryonic kidney (HEK 293) cells. All seven of the extracts exhibited preferential agonist activity toward ERbeta. Using HPLC to collect fractions and MCF-7 cell proliferation, the active components in kudzu root extract were determined to be the isoflavones puerarin, daidzin, genistin, daidzein, and genistein. These results show that several legumes are a source of phytoestrogens with high levels of estrogenic activity.

Identification of puerarin and its metabolites in rats by liquid chromatography-tandem mass spectrometry.:

J Agric Food Chem. 2004; 52(12):3708-12 (ISSN: 0021-8561).Prasain JK; Jones K; Brissie N; Moore R; Wyss JM; Barnes S.Department of Pharmacology and Toxicology, University of Alabama at Birmingham, Birmingham, Alabama 35294, USA. jprasain@uab.edu
Puerarin (daidzein-8-C-glucoside) is the major bioactive isoflavone of kudzu root (the root of Pueraria lobata). Its metabolic fate, however, is not well-known. In this study, a sensitive and specific LC-ESI-MS/MS method for the determination of puerarin and its metabolites daidzein, dihydrodaidzein, and equol was developed for their analysis in biological samples. Two new metabolites of puerarin, mono- and dihydroxylated derivatives, were detected in the urine and feces of rats after oral administration. The persistence of puerarin in blood and urine as the principal metabolic form for the period of 4-72 h after oral administration suggested that puerarin is rapidly absorbed from the intestine without metabolism. Its presence in organs such as the brain suggests that this glucoside may enter tissues by specific transport pathways. Study of these metabolites may provide further understanding of the health beneficial effects of puerarin in kudzu dietary supplements.

Effects of purified puerarin on voluntary alcohol intake and alcohol withdrawal symptoms in P rats receiving free access to water and alcohol.:

J Med Food. 2004; 7(2):180-6 (ISSN: 1096-620X).Benlhabib E; Baker JI; Keyler DE; Singh AK.Department of Veterinary Diagnostic Medicine, College of Veterinary Medicine, University of Minnesota, 1333 Gortner Avenue, St. Paul, MN 55108, USA.
Alcohol preferring (P) rats, given "free choice" of water, exhibited daily intake of 60-75 g of water/kg of body weight. When given "free choice" of water and 15% ethanol, P rats consumed 7-13 g of alcohol/kg. Their water intake decreased proportionally to the alcohol intake, but total fluid intake did not differ significantly. Alcohol withdrawal after 50 days of alcohol drinking caused withdrawal symptoms such as hypersensitivity, poor coordination, and tremors. A daily 50 mg/kg dose of puerarin (PU) caused approximately 50% suppression in alcohol intake, but did not affect body weight and food and total fluid intake in P rats receiving "free choice" of water and 15% ethanol. Alcohol ingestion gradually returned to the control level despite consistent PU intake. However, alcohol intake following alcohol withdrawal was suppressed in PU-fed P rats. PU suppressed the severity of alcohol withdrawal symptoms. Thus, withdrawal symptoms do not occur in PU-fed rats even though their alcohol ingestion is comparable to that in control P rats. Brain, plasma, and liver samples were analyzed for the presence of kudzu root isoflavones, which are mostly PU (>90% of total isoflavones) and a trace amount of daidzin. Liver samples obtained from PU-fed P rats contained 20-30 microg/g of PU. An important observation was that plasma or brain samples obtained from PU-fed or alcohol + PU-fed rats did not contain PU. This study indicated that PU feeding transiently suppressed alcohol intake and abolished withdrawal symptoms at a time when alcohol intake had returned to the control level. The absence of PU in plasma and brain indicates the possibility that some nonspecific mechanism may be involved in the anti-alcoholism effects of PU in P rats.

A comparative survey of leguminous plants as sources of the isoflavones, genistein and daidzein: implications for human nutrition and health.:

J Altern Complement Med. 1997; 3(1):7-12 (ISSN: 1075-5535).Kaufman PB; Duke JA; Brielmann H; Boik J; Hoyt JE.Department of Biology, University of Michigan, Ann Arbor 48109-1048, USA.
Over 80 taxa of mostly agriculturally important legumes were surveyed as sources of the metabolites, genistein and daidzein. Remarkably high concentrations (over 2 g.kg-1 dry weight) of the anticancer metabolite, genistein, were found in the leaves of Psoralea corylifolia (Indian bread root). All other legumes, with the exception of fermented soybean miso, had genistein levels < 400 mg.kg-1 dry weight. Concentrations of over 1 g.kg-1 dry weight and 0.95 g.kg-1 dry weight of the anticancer metabolite, daidzein, were found in the stems of the fava bean (Vicia faba) and roots of kudzu vine (Pueraria lobata), respectively. From this survey, our results indicate that the legumes, lupine (Lupinus spp.), fava bean, (Vicia faba), soybeans (Glycine max), kudzu (Pueraria lobata), and psoralea (Psoralea corylifolia), are excellent food sources for both genistein and daidzein. Miso, a fermented soybean product, is also a rich source of both isoflavones.

Suppression of arachidonic acid metabolism and nitric oxide formation by kudzu isoflavones in murine macrophages.:

Mol Nutr Food Res. 2005; 49(12):1154-9 (ISSN: 1613-4125).Jun M; Hong J; Jeong WS; Ho CT.Department of Food Science, Rutgers University, 65 Dudley Road, New Brunswick, NJ 08901-8520, USA.
Inhibitory effect of kudzu isoflavones on arachidonic acid metabolism and nitric oxide (NO) production in lipopolysaccharide activated RAW 264.7 macrophages were investigated. Isoflavone aglycones, such as daidzein, genistein, biochanin A, and formononetin significantly suppressed arachidonic acid release (50 microM). Biochanin A, which displayed the most active inhibition on arachidonic acid release in HT-29 human colon cancer cells, exhibited its most potent suppression in RAW 264.7 cell (by 86%) without showing cytotoxicity. However, isoflavone glucosides, puerarin and daidzin, showed lower inhibitory activities on the release of arachidonic acid and its metabolites. In NO formation, biochanin A showed marked inhibition, by 62% (50 microM), followed by genistein, daidzein, formononetin, and daidzin, 56, 39, 33, and 8%, respectively. 5,7-Dihydroxyl group in the A-ring of isoflavones could be a key functional group responsible for the strong inhibitory activity of biochanin A and genistein on NO production. These activities may contribute to the antiinflammatory and anticarcinogenic properties of kudzu isoflavones.

Biochemical studies of a new class of alcohol dehydrogenase inhibitors from Radix puerariae.:

Alcohol Clin Exp Res. 1993; 17(6):1254-60 (ISSN: 0145-6008).Keung WM.Center for Biochemical and Biophysical Sciences and Medicine, Harvard Medical School, Boston, MA 02115.
Two potent, reversible inhibitors of human alcohol dehydrogenase (ADH) isozymes were isolated from Radix puerariae (RP, commonly known as kudzu root) and identified as the isoflavones diadzein and genistein. The 4'-methoxy derivatives of daidzein (trivial name, formononetin) and genistein (biochanin A), minor constituents of RP, were also shown to be ADH inhibitors. All of these isoflavones inhibit the human gamma 2 gamma 2-ADH isozyme competitively with respect to ethanol and uncompetitively with respect to NAD+. A survey of more than 40 structurally related compounds revealed one more isoflavone (prunetin) and four flavones (7-hydroxyflavone, apigenin, galangin, and kaempferol) that inhibit ADH. The isoflavone inhibitors, however, are far more potent than the flavone inhibitors. Among the isoflavones studied, genistein is the most potent with Ki = 0.1 microM toward gamma 2 gamma 2-ADH. Human ADH isozymes differ in their sensitivity to these inhibitors in the order gamma 2 gamma 2-, gamma 1 gamma 1- > alpha alpha-, pi pi- > chi chi-ADH. These inhibitors do not affect the beta 1 beta 1- and beta 2 beta 2-ADH isozymes at concentrations as high as 20 microM. Rat and rabbit class I ADHs are also inhibited by these isoflavone inhibitors. The 7-O-glucosyl derivatives of daidzein, genistein, formononetin, and biochanin A do not inhibit ADH, but are potent aldehyde dehydrogenase inhibitors.

Puerarin acts through brain serotonergic mechanisms to induce thermal effects.:

J Pharmacol Sci. 2004; 96(4):420-7 (ISSN: 1347-8613).Chueh FS; Chang CP; Chio CC; Lin MT.Department of Applied Life Science, Taichung Healthcare and Management University, Taichung, Taiwan 413.
The present study was attempted to investigate the effect of puerarin, an isoflavone compound isolated from Pueraria lobata, on both the basal body temperature and pyrogenic fever in unanesthetized, restrained rats. Intraperitoneal administration of puerarin or crude extracts of Pueraria lobata elicited hypothermia. Direct administration of a small amount of puerarin into the lateral cerebral ventricle produced the same extent of hypothermia. Systemic or central administration of puerarin causes a decrease in both colonic temperature and hypothalamic 5-HT efflux in rats. The puerarin-induced hypothermia and decreased 5-HT efflux in the hypothalamus were attenuated by selective depletion of hypothalamic 5-HT produced by intracerebroventricular injection of 5,7-dihydroxytryptamine. Furthermore, the puerarin-induced hypothermia was almost completely abolished by treatment with a 5-HT2A-receptor agonist (DOI or quipazine) or a 5-HT1A-receptor antagonist [(-)-pindolol]. A 5-HT2A-receptor antagonist (ketanserin) or a 5-HT1A-receptor agonist (8-OH-DPAT) had additive effects with puerarin. Intracerebroventricular administration of interleukin-1 caused an increase in both colonic temperature and hypothalamic 5-HT efflux. The interleukin-1-induced hyperthermia and increased 5-HT efflux in the hypothalamus were attenuated by treatment with systemic administration of puerarin. The data indicate that puerarin exerts its hypothermic and antipyretic effects by activating 5-HT1 receptor and/or antagonizing 5-HT2A receptors in the hypothalamus.

Contrasting effects of puerarin and daidzin on glucose homeostasis in mice.:

J Agric Food Chem. 2005; 53(22):8760-7 (ISSN: 0021-8561).Meezan E; Meezan EM; Jones K; Moore R; Barnes S; Prasain JK.Department of Pharmacology & Toxicology, Comprehensive Cancer Center Mass Spectrometry Shared Facility, and Purdue-UAB Botanicals Center for Age-Related Diseases, University of Alabama at Birmingham, Birmingham, AL 35294, USA.
Puerarin and daidzin are the major isoflavone glucosides found in kudzu dietary supplements. In this study, we demonstrated that puerarin significantly improves glucose tolerance in C57BL/6J-ob/ob mice, an animal model of type 2 diabetes mellitus, blunting the rise in blood glucose levels after i.p. administration of glucose. In contrast, daidzin, the O-glucoside, had a significant but opposite effect, impairing glucose tolerance as compared to saline-treated controls. When they were administered i.p. with (14)C-glucose to C57BL/6J lean mice, puerarin inhibited glucose uptake into tissues and incorporation into glycogen, while daidzin stimulated glucose uptake, showing an opposite effect to puerarin. Puerarin also antagonized the stimulatory effect of decyl-beta-D-thiomaltoside, an artificial primer of glycogen synthesis, which increases (14)C-glucose uptake and incorporation into glycogen in mouse liver and heart. A liquid chromatography-tandem mass spectrometry procedure was used to investigate the metabolism and bioavailability of puerarin and daidzin. The blood puerarin concentration-time curve by i.p. and oral administration indicated that puerarin was four times more bioavailable via i.p. injection than via the oral route of administration. This may account for the increased hypoglycemic effect seen in the i.p. glucose tolerance test vs that seen orally. Our results suggest that puerarin is rapidly absorbed from the intestine without metabolism, while daidzin is hydrolyzed to the aglycone daidzein. The opposing effects of puerarin and daidzin on glucose homeostasis may have implications for the activity of dietary supplements that contain both of these isoflavonoids.

Puerarin decreases serum total cholesterol and enhances thoracic aorta endothelial nitric oxide synthase expression in diet-induced hypercholesterolemic rats.:

Life Sci. 2006; 79(4):324-30 (ISSN: 0024-3205).Yan LP; Chan SW; Chan AS; Chen SL; Ma XJ; Xu HX.Institute of Medicinal Plant Development, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing, China.
Hypercholesterolemia is a dominant risk factor for the development and progression of atherosclerosis and cardiovascular diseases. Natural compounds have been proved to be useful in lowering serum cholesterol to slow down the progression of cardiovascular diseases. Pueraria lobata is employed clinically to treat cardiovascular diseases in China. In the present study, the atheroscleroprotective potential of the herb's major active compound, puerarin, was investigated by monitoring serum lipid profile and major enzyme expressions on cholesterol homeostasis in Sprague-Dawley rats fed with control diet, hypercholesterolmic diet or hypercholesterolmic diet plus administration of puerarin (300 mg/kg/day, p.o.) for 4 weeks. Puerarin markedly attenuated the increased total cholesterol induced by hypercholesterolmic diet in both serum and liver. It caused a significant reduction in the atherogenic index. Expression of mRNA for hepatic 7alpha-hydroxylase (CYP7A1) was significantly enhanced but not for those of 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) and lanosterol 14alpha-demethylase (CYP51). To further explore the atheroscleroprotective potential of puerarin, acetylcholine induced endothelium-dependent vasorelaxation and endothelial nitric oxide synthase (eNOS) expression on isolated thoracic aortas were analyzed. Animals administered with puerarin suppressed the hypercholesterolemic diet induced impairment of eNOS expression, whereas there was no significant difference in the endothelium-dependent vasorelaxation among various groups of animals. These data indicated that puerarin reduced the atherogenic properties of dietary cholesterol in rats. Its hypocholesterolemic function may be due to the promotion of cholesterol and bile acids excretion in liver. Whether puerarin targets directly on cholesterol homeostasis or both cholesterol homeostasis and endothelial function remains to be determined.

Determination of puerarin in human plasma by high performance liquid chromatography.:

J Chromatogr B Analyt Technol Biomed Life Sci. 2005; 823(2):108-14 (ISSN: 1570-0232).Ma Z; Wu Q; Lee DY; Tracy M; Lukas SE.Bio-organic and Natural Products Laboratory, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA.
Puerarin, an isoflavone C-glycoside, has been identified as the major active component isolated from Pueraria lobata (Kudzu) responsible for suppression of alcohol drinking. In order to conduct clinical studies of Kudzu's efficacy, a method for measuring its bioavailability and pharmacokinetic profile is needed. We have developed a gradient reversed-phase HPLC system for pharmacokinetic study of puerarin in human plasma. Solid-phase extraction was performed on an abselut Nexus cartridge (60 mg/3 ml) possessing adsorbent function with a recovery of >97% and 4-hydroxybenzoic acid was used as an internal standard. The HPLC assay was performed on a YMC ODS-A column (150 mm x 4.6mm i.d., 5 microm particle size). The HPLC mobile phase consisted of methanol/0.5% acetic acid with 20-35% methanol gradient at a flow-rate of 0.8 ml/min. The UV wavelength was set at 254 nm. Calibration of the overall analytical procedure gave a linear signal (r>0.999) over a puerarin concentration range of 5-500 ng/ml in human plasma. The lower limit of quantification was ca. at 8 ng/ml of puerarin in plasma. The detection limit (defined as signal-to-noise ratio of about 3) was approximately 3 ng/ml. The preliminary pharmacokinetic study after oral administration of the Kudzu capsules containing 400mg of puerarin to a healthy volunteer confirmed that the present method was suitable for determining puerarin in human plasma.

Intestinal bacteria activate estrogenic effect of main constituents puerarin and daidzin of Pueraria thunbergiana.:

Biol Pharm Bull. 2006; 29(12):2432-5 (ISSN: 0918-6158).Park EK; Shin J; Bae EA; Lee YC; Kim DH.College of Pharmacy, Kyung Hee University, Seoul, Korea.
To understand the relationship between the metabolites and estrogenic activity of the main isoflavones puerarin and daidzin of the rhizome of Pueraria thunbergiana (PT, family Leguminosae), PT and its isoflavones were transformed by human intestinal bacteria and their estrogenic effects were investigated. All human fecal specimens hydrolyzed puerarin and daidzin to daidzein, but their hydrolyzing activities varied depending on the individuals. All intestinal bacteria isolated from human also hydrolyzed daidzin to daidzein, but a few bacteria transformed puerarin to daidzein. When the estrogenic effect of PT, puerarin and daidzin was compared with those of their metabolites, the metabolites more potently increased proliferation of MCF-7 cells than PT, puerarin and daidzin. The metabolite daidzein also potently increased estrogen-response c-fos mRNA and PR protein expressions. These findings suggest that intestinal bacteria, which can hydrolyze puerarin and/or daidzin, may activate a potent estrogenic activity of PT.

Determination of puerarin, daidzin and daidzein in root of Pueraria lobata of different origin by HPLC.:

Zhongguo Zhong Yao Za Zhi. 2003; 28(1):49-51 (ISSN: 1001-5302).Jin WS; Tan YY; Chen YG; Wang Y.Beijing Yuke Botanical Development CO., LTD., Beijing 100062, China. jinwenshan@yahoo.com.cn
OBJECTIVE: To develop an HPLC method to determine Puerarin, Daidzin and Daidzein in Pueraria lobata. METHOD: The separation was performed in a SYMMETRY C18 column with a mobile phase of methanol-1% HAC solution (gradient elution), the The detection wavelength being 250 nm. RESULT: The average recovery was respectively 101.7%, 100.7% and 101.7% (n = 3), RSD 0.43%, 0.82% and 1.50% (n = 3) for Puerarin, Daidzin and Daidzein. CONCLUSION: This method is suitable for the determination of Puerarin, Daidzin and Daidzein in Pueraria lobata and its preparation.

Estrogen-like effects of puerarin and total isoflavones from Pueraria lobata.:

Zhong Yao Cai. 2002; 25(8):566-8 (ISSN: 1001-4454).Zheng G; Zhang X; Zheng J; Meng Q; Zheng D.Institute of Metaria Medica, Zhejiang Academy of Medical Sciences, Hangzhou 210013.
OBJECTIVE: To study the estrogen-like effects of puerarin and total isoflavones from Pueraria lobata (TIP) in vivo. METHODS: Puerarin and TIP were orally administrated to ovariectomized rats, infancy or adult mice and estrogen-treated mice at the doses of 150, 300 and 600 mg/kg for 5-9 days. The estrogen-like effects were measured by viginacytology and uterus or ovary weights.
RESULTS: Puerarin and TIP significantly promoted uterus growth in ovariectomized rats and infancy mice, increased the ratios of keratocytes in vaginal smear in ovariectomized rats. The sexual cycle was partially recovered in dose-dependent manner. In E2-treated mice, puerarin and TIP obviously inhibited the growth of vigina induced by E2. No obvious effect was observed in normal adult mice.
CONCLUSION: The results showed that puerarin and TIP acted as weak estrogen-like effect on estrogen-deficiency animals, while no effect on normal-estrogen level ones, but as antiestrogen-like effect in high-estrogen-level ones. These results suggested that puerarin and TIP possessed property of partial agonist of estrogen receptor.

Improvement of ocular blood flow and retinal functions with puerarin analogs.:

J Ocul Pharmacol Ther. 1999; 15(3):207-16 (ISSN: 1080-7683).Xuan B; Zhou YH; Yang RL; Li N; Min ZD; Chiou GC.Institute of Ocular Pharmacology and Department of Medical Pharmacology and Toxicology, Texas A&M Health Science Center, College of Medicine, College Station 77843-1114, USA.
Ischemic retinopathy and, particularly, age-related macular degeneration (AMD) are difficult eye diseases to treat. Since the etiology of these diseases is inadequate blood circulation in the retina and choroid, drugs which can improve blood circulation to these tissues should be beneficial to these diseases. Since fovea is avascular, AMD is closely related to choroidal vascular abnormalities, and drugs which show strong effects to increase choroidal blood flow would be particularly useful. Puerarin and all its derivatives, except ET (puerarin disubstituted with -CH2CH2OH), showed marked increase of choroidal blood flow at various time periods. Even ET showed a tendency to increase choroidal blood flow, though it was not statistically significant. As for b wave recovery, all puerarin analogs showed strong recovery of retinal function after ischemic insult for 30 min. These results indicate that puerarin analogs could be used for the treatment of ischemic retinopathy, and AMD in particular.

  Scientific References:

  1.What is Pueraria root.kudzu root and Pueraria root extract?
  2.Research Update:Puerarin:8-beta-D-Glucopyranosyl-7-hydroxy-3-(4-hydroxyphenyl)-4H-1-.:Introduction and Its Benefit Applications.

Claims & Warning:

Claims: Information this web site presented is meant for Nutritional Benefit and as an educational starting point only, for use in maintenance and promotion good health in cooperation with a common knowledge base reference...Furthermore,it based solely on the traditional and historic use or legend of a given herb from the garden of Adonis. Although every effort has been made to ensure its accurate, please note that some info may be outdated by more recent scientific developments......

Pharmakon Warning: The order of knowledge is not the transparent order of forms and ideas,as one might be tempted retrospectively to interpret it; it is the antidote....(Dissemination,Plato's Pharmacy,II.The Ingredients:Phantasms,Festivals,and Paints;138cf. Jacques Derrida.).

And as it happens,the technique of imitation,along with the production of the simulacrum,has always been in Plato's eyes manifestly magical,thaumaturgical:......and the same things appear bent and straight to those who view them in water and out,or concave and convex,owing to similar errors of vision about colors, and there is obviously every confusion of this sort in our souls.And so scene painting (skiagraphia) in its exploitation of this weakness of four nature falls nothing short of witchcraft (thaumatopoia), and so do jugglery and many other such contrivances.(Republic X,602c-d;cf.also 607c).