OBJECTIVETo study the chemical constituents in the roots of Pueraria lobata.

METHODVarious chromatographic methods were employed to separate of chemical constituents and the spectroscopic methods were used to elucidate the structure.

RESULTTwenty-two compounds were isolated and characterized as beta-sitosterol palmitate (1), beta-sitosterol (2), lupeol (3), lupeone (4) , puerarol (5), diisobutyl phthalate (6), bis(2-ethylhexyl) phthalate (7), sophoracoumestan A (8), coumestrol (9), allantion (10), dadzein (11), formononetin (12), 3'-methoxy daidzein (13), ononin (14), 3'-hydroxy dadzein (15), genistin (16), dadzin (17), 8-methoxy ononin (18), sissotorin (19), (-)-puerol B 2-O-glucopyranoside (20), (6S,9R)-roseoside (21) and sucrose (22), respectively.

CONCLUSIONCompounds 1, 5-8, 15, 18, 21 and 22 were isolated from P. lobata for the first time, and componds 1, 5-7, 15, 18, 21 and 22 were isolated from the genus Pueraria for the first time.

Plant Extracts ; analysis ; isolation & purification ; Plant Roots ; chemistry ; Pueraria ; chemistry

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.

Electrophoresis, Capillary ; methods ; Isoflavones ; analysis ; Pueraria ; chemistry ; Reproducibility of Results

Pueraria thomsonii has long been used in traditional Chinese medicine. Isoflavonoids are the principle pharmacologically active components, which are primarily observed as glycosyl-conjugates and accumulate in P. thomsonii roots. However, the molecular mechanisms underlying the glycosylation processes in (iso)flavonoid biosynthesis have not been thoroughly elucidated. In the current study, an O-glucosyltransferase (PtUGT8) was identified in the medicinal plant P. thomsonii from RNA-seq database. Biochemical assays of the recombinant PtUGT8 showed that it was able to glycosylate chalcone (isoliquiritigenin) at the 4-OH position and glycosylate isoflavones (daidzein, formononetin, and genistein) at the 7-OH or 4'-OH position, exhibiting no enzyme activity to flavonones (liquiritigenin and narigenin) in vitro. The identification of PtUGT8 may provide a useful enzyme catalyst for efficient biotransformation of isoflavones and other natural products for food or pharmacological applications.
Cloning, Molecular ; Genistein ; Glucosyltransferases/metabolism* ; Isoflavones/pharmacology* ; Pueraria/chemistry*

OBJECTIVETo investigate the isoflavones from the vines of Pueraria lobata.

METHODThe compounds were isolated by column chromatography over silica gel and RP-C18, and purified by Sephadex LH-20 column chromatography and preparative TLC. The structures were elucidated on the basis of physico-chemical properties and spectral data.

RESULTTwelve compounds were isolated and identified as: 3'-methoxydaidzein (1), formononetin (2), genistein (3), daidzein (4), daidzin (5), genistin (6), ononin (7), 5-hydroxyl ononin (8), calycosin (9), 6"-O-acetyl genistein (10), 6"-O-acetyl daidzin (11), puerarin (12).

CONCLUSIONFor the first time, compounds 9-11 were isolated from the genus Pueraria plant, and compounds 1, 3, 6-8 were obtained from the vines of this plant.

Genistein ; chemistry ; Glucosides ; chemistry ; Isoflavones ; chemistry ; Magnetic Resonance Spectroscopy ; Plant Stems ; chemistry ; Pueraria ; chemistry

To establish an appropriate experimental and data processing method on the basis of the general kinetic model for extraction of traditional Chinese medicines, in order to study the effect of total flavonoids in water extracts from Puerariae Radix on the adaptability of the model, with total flavonoids of Puerariae Radix as the determination indicator. The results showed that the natural logarithm of mass concentration of total flavonoids showed a good linearity with the changes in extraction time and solvent volume. Through calculating and fitting, we successfully established the kinetic model for water extraction of total flavonoids from Puerariae Radix, and verified its accuracy. Its good fitting degree and controllable deviation within the range of industrial production requirements indicated a good adaptability of the model. However, its equation correction factors require further studies.
Chemistry, Pharmaceutical ; methods ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Flavonoids ; chemistry ; isolation & purification ; Kinetics ; Plant Roots ; chemistry ; Pueraria ; chemistry

The effective components of flavonoids in the "Pueraria lobata-Hovenia dulcis" drug pair have low bioavailability in vivo due to their unstable characteristics. This study used microemulsions with amphoteric carrier properties to solve this problem. The study drew pseudo-ternary phase diagrams through titration compatibility experiments of the oil phase with emulsifiers and co-emulsifiers and screened the prescription composition of blank microemulsions. The study used average particle size and PDI as evaluation indicators, and the central composite design-response surface method(CCD-RSM) was used to optimize the prescription; high-dosage drug-loaded microemulsions were obtained, and their physicochemical properties, appearance, and stability were evaluated. The results showed that when ethyl butyrate was used as the oil phase, polysorbate 80(tween 80) as the surfactant, and anhydrous ethanol as the cosurfactant, the maximum microemulsion area was obtained. When the difference in results was small, K_(m )of 1∶4 was chosen to ensure the safety of the prescription. The prescription composition optimized by the CCD-RSM was ethyl butyrate(16.28%), tween 80(9.59%), and anhydrous ethanol(38.34%). When the dosage reached 3% of the system mass, the total flavonoid microemulsion prepared had a clear and transparent appearance, with average particle size, PDI, and potential of(74.25±1.58)nm, 0.277±0.043, and(-0.08±0.07) mV, respectively. The microemulsion was spherical and evenly distributed under transmission electron microscopy. The centrifugal stability and temperature stability were good, and there was no layering or demulsification phenomenon, which significantly improved the in vitro dissolution of total flavonoids.
Polysorbates/chemistry* ; Flavonoids ; Pueraria ; Surface-Active Agents/chemistry* ; Ethanol ; Emulsions ; Particle Size ; Solubility

Histone lysine-specific demethylase 1(LSD1) has become a promising molecular target for lung cancer therapy. Upon the screening platform for LSD1 activity, some Chinese herbal extracts were screened for LSD1 activity inhibition, and the underlying mechanism was preliminarily investigated at both molecular and cellular levels. The results of LSD1 inhibition showed that Puerariae Lobatae Radix extract can effectively reduce LSD1 expression to elevate the expression of H3 K4 me2 and H3 K9 me2 substrates in H1975 and H1299 cells. Furthermore, Puerariae Lobatae Radix was evaluated for its anti-lung cancer activity. It had a potent inhibitory ability against the proliferation and colony formation of both H1975 and H1299 cells. Flow cytometry and DAPI staining assays indicated that Puerariae Lobatae Radix can induce the apoptosis of lung cancer cells. In addition, it can significantly suppress the migration and reverse the epithelial-mesenchymal transition(EMT) process of lung cancer cells by activating E-cadherin and suppressing the expression of N-cadherin, slug and vimentin. To sum up, Puerariae Lobatae Radix displayed a robust inhibitory activity against lung cancer, and the mechanism may be related to the down-regulation of LSD1 expression to induce the cell apoptosis and suppress the cell migration and EMT process. These findings will provide new insights into the action of Puerariae Lobatae Radix as an anti-lung cancer agent and offer new ideas for the study on the anti-cancer action of Chinese medicine based on the epigenetic modification.
Pueraria/chemistry* ; Histone Demethylases/analysis* ; Plant Roots/chemistry* ; Epithelial-Mesenchymal Transition ; Neoplasms

Puerariae Lobatae Radix is a traditional Chinese medicine,which was first recorded in Shennong Classic of Materia Medica,and was recorded in many ancient books. Its main effect is to relieve muscles to expel heat,produce saliva and promote eruption,invigorate splenic yang and stop diarrhea. CNKI and Wanfang Data were searched in this paper with the words " Pueraria", " puerarin usage" and " puerarin application" as the key words,and it was found that the puerarin usage characteristics were rarely reported.Therefore,the application characteristics of fresh use,crude use and processed use of Puerariae Lobatae Radix in ancient books were summarized in this paper,in order to provide a reference for the modern development of Puerariae Lobatae Radix.
Drugs, Chinese Herbal ; therapeutic use ; Humans ; Medicine, Chinese Traditional ; Plant Roots ; chemistry ; Pueraria ; chemistry

Near-infrared (NIR) was used as rapid analysis method to identify the sulfur fumigated Puerariae Lobatae Radix. NIR spectra of the cross-sectional and longitudinal selection of samples were acquired. Principal component analysis was conducted. The samples were randomly selected. The different pretreatment methods were compared. Discriminant models were established for every type of spectra to calculate the recognition rate. The orthogonal test and nonparametric test were used to test data normality. The result showed that absorbance values of different sections were different due to the different structure, and the raw spectra were analyzed by PCA method. The result founded that the cumulative contribution rate was arrived at 99.2% while the PC numbers were arrived at 3. The pretreatment method based on the MSC + 1D + Savitzky-Golay was the best to establish the model. For the 50 models constructed with cross-section and longitudinal spectra and total spectra, the recognition rate were (94.4 ± 0.66)%, (94.4 ± 0.66)%, (95.3 ± 0.65)%, respectively, and no difference was observed. The NIR method could be used to identify the sulfur fumigated Puerariae Lobatae Radix.
Chemistry, Pharmaceutical ; methods ; Discriminant Analysis ; Drugs, Chinese Herbal ; chemistry ; Fumigation ; Pueraria ; chemistry ; Spectroscopy, Near-Infrared ; Sulfur ; chemistry

OBJECTIVETo study the pharmacokinetics and biodistribution of pur derivative nanopaticles 4ac in mice.

METHODAfter intravenous administration of 15 mg x kg(-1) of pur derivative 4ac, the plasma and tissue concentration was detected by HPLC. The pharmacokinetics parameters were calculated by the method of 3p97.

RESULTThe concentration time curves were conformed to two compartment model. The Re of 4ac nanopaticles was 21.18 times higher than suspension.

CONCLUSIONOur present study demonstrates that, compared to nanopaticles and suspension, nanopaticles significantly alter the pharmacokinetics in plasma and tissues targeting. Biodistribution of pur derivative 4ac nanopaticles in heart of mice was better than 4ac suspension. It will become a new drug for cardiovascular disease therapy.

Animals ; Female ; Isoflavones ; chemistry ; pharmacokinetics ; Male ; Mice ; Nanoparticles ; chemistry ; Plant Extracts ; chemistry ; pharmacokinetics ; Pueraria ; chemistry ; Random Allocation ; Tissue Distribution