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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

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. Source

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

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. Source

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

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. Source

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

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. Source

Fu X.-Z.,Pharmacy Development | Fu X.-Z.,Provincial Key Laboratory of Pharmaceutics in Guizhou Province | Jiang F.-J.,Pharmacy Development | Ou Y.,Guiyang Women And Childrens Hospital And Health Institute | And 10 more authors.
Chinese Chemical Letters

A series of mono l-amino acid ester, mono non-steroid anti-inflammation drug (NSAID), carboxylic ester derivatives of acyclonucleoside phosphonates were prepared by using a "one pot synthesis" method and their in vitro anti-HBV activity were evaluated in HepG 2.2.15 cells. Compound 9a exhibited more potent anti-HBV activity and lower cytotoxicity than those of adefovir dipivoxil with IC50 and selective index (SI) values of 0.48 μmol/L and 763.72, respectively. © 2013 Xiao-Zhong Fu and Yong-Lin Wang. Source

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