An popular isoflavan, vestitol in some Fabaceae plants – was isolated from the aerial part of Excoecaria cochinchinensis Lour. Var cochinchinensis. Its structure was elucidated on the basis of spectral analysis including 1H-NMR, 13C-NMR, EIMS.
Isoflavones ; Plants, Medicinal ; Medicine, Traditional

This study was mainly based on the compatibility of Puerariae Lobatae Radix and Chuanxiong Rhizoma to prepare submicron emulsion and evaluated its physical and pharmaceutical properties. Firstly, pseudo-ternary phase diagrams were drawn by dripping method which took Chuanxiong oil as the oil phase and the area of microemulsion region as the index. On this basis, suitable emulsifier and co-emulsifier were screened for the preparation of Chuanxiong oil submicron emulsion. Then, the formula realizing the largest oil loading was selected. Finally, puerarin substituted part of emulsifier and co-emulsifier to lower their content, so as to form puerarin-Chuanxiong oil submicron emulsion featuring the combination of medicine and adjuvant. Its particle size, zeta potential, centrifugal stability and storage stability were determined, and the in vitro drug release behavior was investigated by dialysis bag method, based on which the quality of the as-prepared submicron emulsion was evaluated comprehensively. The proposed method was proved feasible for the preparation of Chuanxiong oil submicron emulsion, which adopted polyoxyethylene castor oil(EL-40) as the emulsifier and was free from co-emulsifier. The formula of the maximum oil loading was found as Chuanxiong oil∶EL-40∶water 3∶7∶90. Further, puera-rin successfully replaced up to 10% of the emulsifier in submicron emulsion. Eventually, the optimal drug-loading formula was determined as puerarin∶Chuanxiong oil∶EL-40∶water 7∶30∶63∶900. The quality evaluation results of the as-prepared submicron emulsion demonstrated that the average emulsion droplet size was 333.9 nm, the PDI 0.26, and the zeta potential-10.12 mV. The submicron emulsion had a good centrifugal stability and did not present any instable phenomena such as delamination and precipitation during its standing still for 50 days. The evaluation of in vitro drug release behavior indicated that the submicron emulsion was capable of releasing the drug completely. The puerarin-chuanxiong oil submicron emulsion prepared in this study possessed a stable quality and to some extent increased the solubility of puerarin along with a sustained-release effect. This study provided ideas for the clinical application of puerarin.
Emulsions ; Isoflavones ; Particle Size ; Solubility

Puerarin is a naturally occurring isoflavone C-glycoside,isolated from the root of Pueraria lobata,which has attracted extensive attention in the medical circles because of its various pharmacological effects,such as vasodilation,cardioprotection,neuroprotection,antioxidant,anticancer,anti-inflammation,alleviating pain,promoting bone formation,inhibiting alcohol intake,and attenuating insulin resistance. However,its low oral bioavailability has limited its clinical application. This review gives a comprehensive summary of the researches on physicochemical properties,pharmacokinetics( absorption,distribution,metabolism and excretion,pharmacokinetic parameters) in oral administration,and pharmaceutics research strategies of puerarin in recent years,and the in vivo behavior difference between multicomponent and single component environment was also summarized. The reasons( low water solubility,poor membrane permeability,short half-life,inhibition of P-gp efflux and first-pass metabolic effects of intestinal enzymes,etc.) for low bioavailability were concluded and the idea that multicomponent enviroment would affect the bioavailability was clarified. The aim of this review is to provide literature basis for the development of new dosage forms and new technologies for multivariate compound drug delivery system to improve the bioavailability of oral puerarin,and to propose ways to improve the bioavailability of BCS Ⅳ drugs derived from traditional Chinese medicine by fully enlarging the synergistic effect of multi-components or reasonably using the inhibitory effect between components.
Administration, Oral ; Biopharmaceutics ; Isoflavones ; Pueraria

To study chemical constituents of Polygonatum odoratum (Mill.) Druce, the compounds were separated with column chromatography and HPLC. On the basis of physicochemical properties and spectral data, their structures were confirmed. Nine compounds were isolated and identified as 5,7-dihydroxy-6-methoxyl-8-methyl-3-(2',4'-dihydroxybenzyl)chroman-4-one (1), 5,7-dihydroxy-6-methyl-3-(2',4'-dihydroxybenzyl)chroman-4-one (2), 5,7-dihydroxy-6-methoxyl-8-methyl-3-(4'-methoxybenzyl)chroman-4-one (3), disporopsin (4), chrysoeriol (5), 5,4'-dihydroxy-7-methoxy-6-methylflavone (6), N-trans-feruloyltyramine (7), N-trans-feruloyloctopamine (8), and (+)-syringaresinol (9). Compounds 1-3 are new homoisoflavanones. Compounds 4-9 are isolated from this plant for the first time.
Isoflavones ; isolation & purification ; Molecular Structure ; Polygonatum ; chemistry

To decrease the hemolysis side effect of puerarin, the basic formula and preparation of puerarin submicron emulsion were optimized and the physicochemical properties were evaluated. Puerarin submicron emulsions were prepared by phase inversion-ultrasound combining with phospholipids complexes technology. The effects of preparative parameters, such as emulsification time, stirring velocity and ultrasound time, on mean diameter, span of dispersity, entrapment efficiency and overall desirability were investigated. The three dimensional response surface graphs were produced by second-order polynomial and liner equation, which predict the optimal experiment conditions. All response variables were found to be greatly dependent on three independent variables. Second-order polynomial equations were fitter than liner equations for this study. The optimal emulsification time, stirring velocity and ultrasound time was 15 min, 2 000 r x min(-1), 30 min, respectively. The mean diameter, span of dispersity, entrapment efficiency, drug content and zeta potential of emulsions prepared by the method were 228.23 nm, 0.628 4, 84. 32%, 9.98 mg x mL(-1), - 29.03 mV, respectively. Puerarin submicron emulsion was prepared by the optimized preparation method. The narrow particle diameter distribution, high envelopment efficacy and good stability were obtained. The physicochemical properties were suitable for the requirement of the intravenous emulsion.
Emulsions ; Isoflavones ; administration & dosage ; chemistry ; Particle Size

OBJECTIVE: To observe the effects of blocking and activating chloride channels on hemolysis induced by puerarin injection in rabbits and to investigate the roles of chloride channels in hemolytic reaction induced by puerarin injection. METHODS: Rabbit erythrocyte suspension was incubated with different concentrations of puerarin injection(0.75, 1.5, 3, 6, 12 mg/ml) at 37C for 6 hours. The cell imaging system was employed to observe whether puerarin injection induced hemolysis. The hemolysis rate was detected by microplate reader and flow cytometry. Effects of activating and closing chloride channels on the hemolysis induced by puerarin injection were explored. RESULTS: Puerarin injection could induce the hemolysis of rabbit erythrocytes . In the range of 1.5 mg/ml~12 mg/ml, puerarin injection could induce hemolysis in a concentration-dependent manner (=3, <0.01). The chloride channel blockers tamoxifen (20 μmol/L) and ATP (10 mmol/L) significantly inhibited the hemolysis induced by puerarin injection (=3~5, <0.01). Application of low concentration ATP (50 μmol/L) to activate the chloride channel significantly increased puerarin injection induced hemolysis (=4, <0.01). CONCLUSIONS The hemolytic effect of puerarin injection is dose-dependent , and the activation of chloride channel is closely related to the hemolysis induced by puerarin injection.
Animals ; Chloride Channels ; Erythrocytes ; Hemolysis ; Isoflavones ; Rabbits

Based on the fact that glycyrrhizic acid can form micelles in aqueous solution and play a role in solubilization, the optimal compatibility ratio between puerarin and glycyrrhizic acid was screened to prepare puerarin-glycyrrhizic acid dispersible tablets and investigate the dissolution of puerarin. The particle size, Zate potential and puerarin dissolution were compared among the micellar solutions with mass ratio of 7∶1, 6∶1, 5∶1, 4∶1, 3∶1 and 2∶1(puerarin to glycyrrhizic acid), and it was found that when the mass ratio of puerarin and glycyrrhizic acid was 5∶1, the micelle showed smallest particle size, uniform distribution, and largest puerarin dissolution, so mass ratio of 5∶1 was determined as the optimal condition. The formulation of puerarin-glycyrrhizic acid dispersible tablets was optimized by single factor and orthogonal test: puerarin 100.0 mg, glycyrrhizin 20.0 mg, polyvinylpolypyrrolidone 24.0 mg as disintegrating agent, microcrystalline cellulose 135.0 mg as stuffing bulking agent, hydroxypropyl methyl cellulose 18.0 mg as adhesive agent, magnesium stearate 2.7 mg as lubricant, and tablet weight of 300.0 mg. High-performance liquid chromatography(HPLC) method was used to determine the content of puerarin in dispersible tablets. Puerarin showed a good linear relationship(r=0.999 8) in the range of 15.5-248 g·L~(-1), with high precision(RSD<2.0%) and good repeatability(RSD<2.0%), and the recovery rate was 101.1%, RSD 0.89%. There was no significant difference in the quantity of puerarin in different batches of puerarin-glycyrrhizic acid dispersible tablets. When the artificial gastric juice was used as the dissolution medium, the dissolution of puerarin in puerarin-glycyrrhizic acid dispersible tablets could reach over 85% within 15 min. When phosphate buffer(pH 6.8) was used as the dissolution medium, the dissolution of puerarin in the puerarin-glycyrrhizic acid dispersible tablets had a faster dissolution rate in vitro, 99.8% in 30 min. Therefore, puerarin-glycyrrhizic acid dispersible tablets could improve the dissolution of puerarin in vitro due to the solubilization effect of glycyrrhizic acid.
Glycyrrhizic Acid ; chemistry ; Isoflavones ; chemistry ; Solubility ; Tablets

Phytoestrogen is an estrogenic compound that occurs naturally in plants. The most common sources of phytoestrogen are soybean products, which contain high levels of isoflavones. This compound, which has structural similarity with estrogen, can act as an estrogen receptor agonist or antagonist. Animal studies provide evidence of the significant effects of phytoestrogen on sexual development, including altered pubertal timing, impaired estrous cycling and ovarian function, and altered hypothalamus and pituitary functions. Although human studies examining the effects of phytoestrogen on sexual development are extremely limited, the results of some studies agree with those of the animal studies. In this paper, we review the possible mechanism of phytoestrogen action and the evidence showing the effects of phytoestrogen on sexual development in animal and human studies.
Animals ; Estrogens ; Humans ; Hypothalamus ; Isoflavones ; Phytoestrogens ; Puberty ; Sexual Development ; Soybeans

OBJECTIVETo develop a method for analyzing the chemical compositions of Gegen and Fenge extracts using high-performance capillary electrophoresis (HPCE).

METHODSUsing HPCE/DAD, the chemical composition of the extracts was analyzed with the buffer solution of 40 mmol/L borax containing 16.7% methanol, with injection pressure at 137.9 kPa for 5 s, separation voltage at 25 kV in 0-5 min time range and at 22 kV in 5-25 min time range, and the temperature of the capillary of 20 degrees celsius.

RESULTS AND CONCLUSIONThe method for analysis of Gegen and Fenge extracts was established, which identified puerarin and daidzein as the two major components. This simple and rapid analysis method can be used for Gegen and Fenge extract fingerprinting.

We studied the effects of soy isoflavones supplementation with exercise on bone mineral density and the urinary excretion of deoxypyridinoline as an index of bone resorption rates in postmenopausal women. A total of 67 postmenopausal women were assigned to Isoflavone (90 mg/day) or placebo groups. These groups were further divided into groups that undergone a regular exercise or a rather sedentary state performing daily activity only. Four groups were Placebo-control group (n = 16), Placebo-exercise group (n = 16), Isoflavone-sedentary group (n = 19) and Isoflavone-exercise group (n = 16). After the intervention, we compared anthropometric mesurement, dietary recall, bone mineral density (femoral neck, lumbar spine), urinary deoxypyridinoline between the groups and between the pre and post studies. There were no significant differences between the four groups in terms of average age, height, weight, period after menopause at the baseline. The average age of the subjects were 55.2 yrs, average height, weight, period after menopause were 154.7 cm, 59.3 kg, 5.58 yrs, respectively. After eight week intervention period, there were no significant differences between the four groups in bone mineral density, but urinary deoxypyridinoline excretion was significantly decreased both in Isoflavone-sedentary and Isoflavone-Exercise groups. These results suggest that Isoflavone supplementation alone or with exercise may be preventive measures through the decrease of bone reabsorption rate in post-menopausal subjects. Whereas exercise alone did not appear to be an effective measure in bone loss with these subjects.
Bone Density* ; Bone Resorption ; Female ; Humans ; Isoflavones ; Menopause ; Neck