Provincial Key Laboratory of Pharmaceutics in Guizhou Province

Guiyang, China

Provincial Key Laboratory of Pharmaceutics in Guizhou Province

Guiyang, China
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Chen Y.,Guizhou University | Zheng Zhang W.,Guizhou University | Li J.,Guizhou University | Xiao T.,Guizhou University | And 9 more authors.
Medicinal Chemistry Research | Year: 2017

A series of adefovir mono L-amino acid ester, mono bile acid ester derivatives was designed and synthesized. The newly designed compounds have potent anti-anti-hepatitis B activity, especially compound 6c, which has more potent antiviral activity and a higher selectivity index (EC50 0.65 μmol/L, SI 582.24) than adefovir dipivoxil. Uptake of compounds 6a–f into rat primary hepatocytes was 71.56, 63.92, 142.88, 104.25, 67.84, and 39.95-fold, respectively, higher than that of adefovir dipivoxil. In the presence of Na+, uptake of compounds 6a–c by Na+/taurocholate co-transporting polypeptide-Human embryonic kidney 293 cells was 128.5, 137.2 and 121.7-fold higher than that of adefovir dipivoxil. Potential binding modes of compounds 6a and 6c to human apical Na+-dependent bile acid transporter were also investigated. © 2017 Springer Science+Business Media New York


Lu Y.,Provincial Key Laboratory of Pharmaceutics in Guizhou Province | Lu Y.,Guizhou University | Gong Z.,Provincial Key Laboratory of Pharmaceutics in Guizhou Province | Gong Z.,Guizhou University | And 13 more authors.
Evidence-based Complementary and Alternative Medicine | Year: 2016

Relinqing granule (RLQ) is the best-selling Chinese patent drug for treatment of urinary system diseases. In this study, the effects of RLQ on the pharmacokinetics of ciprofloxacin, sulfamethoxazole, and trimethoprim in SD rats were investigated. Rats were randomly divided into control group 1, control group 2, RLQ group 1, and RLQ group 2. RLQ group 1 and RLQ group 2 were treated orally with RLQ for 7 days, and rats were treated with the same volume of water in control group 1 and control group 2. Then, RLQ group 1 and control group 1 were given intragastrically ciprofloxacin on day 8, while RLQ group 2 and control group 2 were given intragastrically sulfamethoxazole and trimethoprim on day 8. Blood samples were collected and determined. There was no significant influence of pharmacokinetic parameters of trimethoprim on two groups. But some pharmacokinetic parameters of ciprofloxacin and sulfamethoxazole in RLQ pretreated rats were evidently altered (P < 0.05), which indicated that absorption of ciprofloxacin and sulfamethoxazole in RLQ pretreated rats was significantly affected. It indicated the coadministration of RLQ would have an influence on the efficacy of ciprofloxacin and sulfamethoxazole, and the doses of ciprofloxacin tablet and compound sulfamethoxazole tablet need adjustment. © 2016 Yuan Lu et al.


He F.,Guiyang Medical College | He F.,Provincial Key Laboratory of Pharmaceutics in Guizhou Province | Mou J.-L.,Guiyang Medical College | Zheng L.,Guiyang Medical College | And 5 more authors.
Chinese Pharmacological Bulletin | Year: 2014

Aim: To compare the pharmacokinetics of gallic acid and albiflorin in Radix Paeoniae Rubra and compound Xinshao through UPLC-MS in rats respectively, and to investigate the effect of combination in physiological disposition. Methods: Two compounds were simultameously determined by UPLC with Waters Acquity UPLC BEH C18 column. The mobile phase, consisting of acetonitrile and 0.1% aqueous formic acid, was programmed as a linear gradient. The compounds were ionized in the electrospray ionization ion source of the mass spectrometer and detected in the SIR model. The pharmacokinetic parameters describing disposition after oral administration of Radix Paeoniae Rubra extract and compound Xinshao to rats were calculated by DAS2.0. Results: The relationship, precisions, accuracy and stability of the two compounds met the requirements. Both plasma concentration-time curves were comformed to two compartment models. In the two experiment groups each albiflorin pharmacokinetic parameter had significant difference. In addition to Tmax, T1/2z had no significant difference of gallic acid. Conclusion: There is significant difference between Radix Paeoniae Rubra and compound Xinshaoon pharmacokinetics of gallic acid and albiflorin, which may be related to the intercompatibility, modeling technique and composition of compound recipe.


Lu Y.,Provincial Key Laboratory of Pharmaceutics in Guizhou Province | Lu Y.,Pharmacy Development | Pan J.,Provincial Key Laboratory of Pharmaceutics in Guizhou Province | Xie Y.-M.,Provincial Key Laboratory of Pharmaceutics in Guizhou Province | And 7 more authors.
Chinese Pharmacological Bulletin | Year: 2015

Aim: To evaluate the inhibitive and inductive effects of Polygonum capitatum water extract on main cytochrome P450 isoforms in human and liver microsomes of mouse in vitro for predicting the herb-drug interactions in clinical application. Methods: The in vitro inhibitory effect was evaluated by incubating Polygonum capitatum water extract with the probe substrates of main phase I metabolic enzymes in human liver microsomes, including CYP1A2, CYP2E1, CYP2C9, CYP2C19 and CYP3A4. Mice were administered with Polygonum capitatum water extract at dosage of 0.58 g • kg-1 and 1.16 g • kg-1 by gastric lavage for successive 7 days and 14 days, then the cocktail-LC-MS/MS method was applied to assess the inductive effect of main CYP450 isoforms in mouse liver microsomes. Results: The IC50 values of Polygonum capitatum water extract on main CYP450 isoforms in human liver microsomes were from 849.6 mg • L-1 to 2 287 mg • L-1. Compared with the blank control group, the activites of CYP2C9 and CYP3A4 in 1.16 g • kg-1 7 d group were about 49.9 % and 21.1 % higher (P < 0.01, P < 0.05) respectively, the activities of CYP2C9 and CYP3A4 in 0.58 g • kg-1 7 d group were 27.6 % and 15.5 % higher (P < 0.01, P < 0.05) respectively, the activities of CYP2C9 and CYP3A4 in 1.16 g • kg-1 14 d group were 67.5 % and 32.1 % higher (P<0.01) respectively, while the activities of CYP1A2, CYP2E1 and CYP2C19 were not increased significantly in Polygonum capitatum treatment group. Conclusions Polygonum capitatum water extract do not show the inhibitory effect on main CYP450 in human liver microsomes. There is induction on CYP2C9 and CYP3A4 in mouse liver microsomes by Polygonum capitatum water extract.


Zheng L.,Pharmacy Development | Zheng L.,Provincial Key Laboratory of Pharmaceutics in Guizhou Province | Mu J.-L.,Pharmacy Development | Huang Y.,Pharmacy Development | And 6 more authors.
Chinese Journal of New Drugs | Year: 2014

Objective: To establish a UPLC-MS/MS method for simultaneous determination of gallic acid, oxypaeoniflorin, albiflorin, paeoniflorin, scutellarin, 4'-hydroxy baicalein-7-O-β-D pyrangluconat emethyl ester and benzoylpaeoniflorin in Xinshao freeze-dried powder injection. Methods: The analysis was performed on a BEH C18 column(50 mm×2.1 mm, 1.7 μm)with acetonitrile-0.1% formate acid solution as mobile phase in gradient elution mode. The column temperature was set at 45°C. The flow rate was 0.35 mL·min-1 and the injection volume was 1 μL. Multiple-reaction monitoring(MRM)scanning was employed for quantification with switching electrospray ion source polarity in positive/negative mode. Results: The linear ranges were 2.55~25.48 μg·mL-1(r=0.999 3)for gallic acid, 0.49~4.94 μg·mL-1(r=0.994 9)for oxypaeoniflorin, 2.02~20.24 μg·mL-1(r=0.998 4)for albiflorin, 6.25~62.52 μg·mL-1(r=0.999 2)for paeoniflorin, 4.17~41.68 μg·mL-1(r=0.997 8)for scutellarin, 0.17~1.67 μg·mL-1(r=0.997 7)for 4'-hydroxy baicalein-7-O-β-D pyrangluconat emethyl ester, and 0.80~8.03 μg·mL-1(r=0.996 3)for benzoylpaeoniflorin. The average recoveries were 98.56% with RSD of 2.22% for gallic acid, 96.06% with RSD of 4.06% for oxypaeoniflorin, 99.27% with RSD of 3.79% for albiflorin, 98.47% with RSD of 0.93% for paeoniflorin, 98.85% with RSD of 1.21% for scutellarin, 101.03% with RSD of 4.69% for 4'-hydroxy baicalein-7-O-β-D pyrangluconat emethyl ester, and 97.69% with RSD of 3.71% for benzoylpaeoniflorin, respectively. Conclusion: The method is simple, accurate and highly reproducible, and can be used for the quality control of Xinshao freeze-dried powder injection.


Huang Y.,Provincial Key Laboratory of Pharmaceutics in Guizhou Province | Tang L.,Provincial Key Laboratory of Pharmaceutics in Guizhou Province | Liu Y.,Provincial Key Laboratory of Pharmaceutics in Guizhou Province | Lu Y.,Provincial Key Laboratory of Pharmaceutics in Guizhou Province | And 2 more authors.
Chinese Journal of New Drugs | Year: 2014

Objective: To develop a sensitive and reliable ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method for simultaneous determination of scutellarein, and to investigate the intestinal absorption kinetics of scutellarein. Methods: The absorption of scutellarein was determined at different intestine segments of rats. The influences of drug concentrations, pH values and P-gp inhibitors were evaluated. The intestinal cannulation was performed for in situ recirculation. Results: The in situ recirculation showed that the absorption of scutellarein was not influenced by pH values ranging from 5.0 to 7.4. The absorption of scutellarein significantly increased at large and moderate doses, but not at low dose. In addition, the P-gp inhibitor verapamil had no obvious effect on the intestinal absorption of scutellarein. The absorption in small intestine was more than that in colon. Conclusion: Scutellarein can be absorbed in whole intestinal segments, and the absorption is possibly independent on active transport mechanism. The low bioavailability of scutellarein may result from wide range of metabolism in intestinal tract and efflux secretion.


He X.,Pharmacy Development | Wang Z.,Pharmacy Development | Wang A.-M.,Provincial Key Laboratory of Pharmaceutics in Guizhou Province | Li Y.-J.,Pharmacy Development | And 3 more authors.
Chinese Journal of New Drugs | Year: 2015

Objective: To establish the UHPLC fingerprint for Guizhou Miao medicine Geum japonicum and a method for determining its main component ellagic acid. Methods: The chromatographic separation was performed on the Phenomenex Synergi column (2.0 mm×100 mm, 2.5 μm) with gradient elution of methanol and 0.1% aqueous formic acid at a flow rate of 0.3 mL·min-1. The column temperature was set at 40 ℃. Results: The UHPLC fingerprint with 17 common peaks was established for Geum japonicum. The method for determining ellagic acid in the same chromatographic condition was set up, which showed good linearity in the test ranges. The average recovery was 100.6% and the RSD was 1.3%. Conclusion: The methods developed are convenient, rapid, accurate and reproducible, which is applicable to the quality control of Guizhou Miao medicine Geum japonicum. ©, 2015, Chinese Journal of New Drugs Co. Ltd. All right reserved.


Dai Z.-Q.,Guiyang Medical College | Su H.,Guiyang Medical College | Luo M.,Guiyang Medical College | Ou Y.,Maternal and Child Health Hospital of Guiyang City | And 6 more authors.
Bulletin of the Korean Chemical Society | Year: 2015

A series of 4′-N-substituted (aminomethyl)benzoate derivatives of scutellarein were designed and synthesized. Evaluation of their physiochemical properties showed that the designed target compounds 5a-e exhibit higher chemical stability and aqueous solubility than scutellarin and scutellarein. The permeability (Papp AP to BL) of 5c-e in Caco-2 cells were 2.8, 8.1, and 12.6 times higher than that of scutellarin and 1.3, 4.1, and 6.0 times higher than that of scutellarein; especially, 5e had the highest Papp AP to BL value (7.19 ± 0.31 × 10-6 cm/s) and the lowest ER (Papp BL to AP/Papp AP to BL) value of 0.17. In vitro antioxidative evaluation results revealed that 5e could protect against H2O2-induced PC12 cells' oxidative damage by attenuating mitochondrial membrane potential loss and decreasing H2O2-induced reactive oxygen species (ROS) production. © 2015 Korean Chemical Society & Wiley-VCH Verlag GmbH & Co. KGaA.


Zhang L.J.,Provincial Key Laboratory of Pharmaceutics in Guizhou Province
Zhong yao cai = Zhongyaocai = Journal of Chinese medicinal materials | Year: 2012

To investigate the chemical constituents of the active fraction of Polygonum capitatum. Various preparative chromatographic techniques were used for the isolation and purification of the compounds in the flavonoid-enriched fraction and their structures were determined by comparison of their physicochemical and chromatographic data with those of the authentic samples and spectral analysis. Fourteen compounds were obtained and identified as 1-O-P-D-(6'-O-galloyl)-glucopyranosyl-3-methoxy-5-hydroxybenzene (1) ,5,7-dihydroxy-4H-chromen-4-one (2), ellagic acid (3), myricetrin (4), hirsutine (5), rutin (6), quercetin-3-O-(2"-O-galloyl)-beta-D-glucopyranoside (7) , quercetin-3-O-( 3"-O-galloyl) -/3-D-glucopyranoside (8), quercitrin (9) , kaempferol-3-O-alpha-L-rhamnopyranoside (10), quercetin-3-O-(2"-O-galloyl) -alpha-L-rhamnopyranoside (11), quercetin-3-O-(3"-O-galloyl) -alpha-L-rhamnopyranoside (12), quercetin (13), kaempferol (14). The flavonoid-enriched fraction contains flavonols and their glycosides as its major components,which might be responsible for the biological effects of Polygonum capitatum. Compounds 1, 8 and 12 are isolated from the genus Polygonum for the first time; Compound 3 is isolated from Polygonum capitatum for the first time.


PubMed | Provincial Key Laboratory of Pharmaceutics in Guizhou Province
Type: Journal Article | Journal: Zhong yao cai = Zhongyaocai = Journal of Chinese medicinal materials | Year: 2013

To investigate the chemical constituents of the active fraction of Polygonum capitatum.Various preparative chromatographic techniques were used for the isolation and purification of the compounds in the flavonoid-enriched fraction and their structures were determined by comparison of their physicochemical and chromatographic data with those of the authentic samples and spectral analysis.Fourteen compounds were obtained and identified as 1-O-P-D-(6-O-galloyl)-glucopyranosyl-3-methoxy-5-hydroxybenzene (1) ,5,7-dihydroxy-4H-chromen-4-one (2), ellagic acid (3), myricetrin (4), hirsutine (5), rutin (6), quercetin-3-O-(2-O-galloyl)-beta-D-glucopyranoside (7) , quercetin-3-O-( 3-O-galloyl) -/3-D-glucopyranoside (8), quercitrin (9) , kaempferol-3-O-alpha-L-rhamnopyranoside (10), quercetin-3-O-(2-O-galloyl) -alpha-L-rhamnopyranoside (11), quercetin-3-O-(3-O-galloyl) -alpha-L-rhamnopyranoside (12), quercetin (13), kaempferol (14).The flavonoid-enriched fraction contains flavonols and their glycosides as its major components,which might be responsible for the biological effects of Polygonum capitatum. Compounds 1, 8 and 12 are isolated from the genus Polygonum for the first time; Compound 3 is isolated from Polygonum capitatum for the first time.

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