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Peng F.,State Key Laboratory Breeding Base of Systematic Research | Peng F.,Sichuan University | Xiong L.,State Key Laboratory Breeding Base of Systematic Research | Xiong L.,Chengdu University of Traditional Chinese Medicine | Zhao X.-M.,Chengdu University of Traditional Chinese Medicine
Molecules | Year: 2013

A new 15,16-dinorlabdane diterpenoid 1 and a known labdane diterpenoid 2, together with three known ergosterols 3-5, were isolated from the EtOAc-soluble portion of the EtOH extract of Leonurus japonicus. Their structures were elucidated by physical and spectroscopic analysis. Compound 1 showed in vitro coagulant activity in the APTT, PT, TT, and FIB assays. © 2013 by the authors. Source


Li Y.-X.,Chengdu University of Traditional Chinese Medicine | Li Y.-X.,Ministry of Education Key Laboratory of Standardization of Chinese Herbal Medicine | Li Y.-X.,State Key Laboratory Breeding Base of Systematic Research | Zhang R.-Q.,Chengdu University of Traditional Chinese Medicine | And 5 more authors.
European Journal of Drug Metabolism and Pharmacokinetics | Year: 2012

Forsythiaside was characterized by low intestinal absorption by in situ rat experiment and Caco-2 cells. The mechanisms behind this low absorption had not yet been elucidated. The purpose of this study was to investigate the role of efflux transporters in the intestinal absorption of forsythiaside as a potential mechanism for its low small-intestinal absorption following oral administration. Polarized MDCKII cell lines stably transfected with human or murine complementary DNA encoding for various efflux transporters (P-gp/MDR1, MRP2 and Bcrp1) were used to study transepithelial transport of forsythiaside and compare results with the MDCKII-Wild type cells. The transportation inhibitors GF120918, MK571 and Ko143 were used to investigate the transport mechanism. The active transport of forsythiaside was found in MDCKII-WT cells. The MDCKII-MRP2 and MDCKII-Bcrp1 cells significantly increased forsythiaside efflux ratio compared with the parental cells due to the apically directed transport by MRP2 and Bcrp1, respectively. The efflux ratios inMRP2and Bcrp1 transfected cell lines were greatly decreased in the presence of MK-571 and Ko143, respectively, which indicated that forsythiaside efflux by MRP2 and Bcrp1 were significantly inhibited by their selective inhibitors. MDCKII-MDR1 cells did not exhibit a significant reduction in the forsythiaside efflux compared with the parental cells, indicating that it was not a good substrate for MDR1. And the results were then validated by the in situ experiment. This study presents direct evidence that forsythiaside is effluxed by both MRP2 and Bcrp1, which may contribute to its poor oral bioavailability. © Springer-Verlag France 2012. Source


Li Y.-X.,Chengdu University of Traditional Chinese Medicine | Li Y.-X.,Key Laboratory of Standardization of Chinese Herbal Medicine | Li Y.-X.,State Key Laboratory Breeding Base of Systematic Research | Ye L.-H.,Chengdu University of Traditional Chinese Medicine | And 6 more authors.
European Journal of Drug Metabolism and Pharmacokinetics | Year: 2011

The study was to investigate the absorption mechanism and transport modulation of phillyrin by P-gp in Caco-2 cells and MDR1-MDCKII cells. Three concentrations of phillyrin were tested in transport studies. The absorptive transports of phillyrin in the two cell models were not concentration-dependent which indicated passive diffusion as the dominating process in the test concentrations. The absorptive P app were 7.15, 6.39 and 10.03 × 10-6 cm s-1, respectively, for different concentrations (2.2, 4.8 and 8.4 μg ml-1) in Caco-2 cells. And the low absorptive P app was consistent with the low oral bioavailability of phillyrin observed in pharmacokinetic experiments. In transport inhibition experiment, the efflux inhibitors, verapamil and GF120918 can increase the absorption of phillyrin in Caco-2 cells which suggested the involvement of efflux transporters. In the further inhibition experiment in MDR1-MDCKII cells, the absorption was greatly increased and the efflux of phillyrin was competitively inhibited by verapamil and GF120918, which confirmed the involvement of P-gp in the efflux of phillyrin. © 2011 Springer-Verlag France. Source


Wan F.,Chengdu University of Traditional Chinese Medicine | Wan F.,State Key Laboratory Breeding Base of Systematic Research | Peng F.,Chinese University of Hong Kong | Xiong L.,Chengdu University of Traditional Chinese Medicine | And 5 more authors.
Chinese Journal of Integrative Medicine | Year: 2016

Objective: To investigate the antibacterial activity of patchouli alcohol (PA) against 127 bacteria strains, including the common bacteria and drug-resistant bacteria strains both in the in vitro and in vivo tests. Methods: For the in vitro trial, the antibacterial property of PA against 107 Gram-positive and 20 Gram-negative bacteria strains was screened by agar double dilution method. For the in vivo trial, specific pathogen free Kunming strain of both male and female white mice, were used to test the protective ability of PA after being injected with the median lethal dose of the tested strains. Results: PA possessed antibacterial activity against all the tested 127 strains. In the in vitro test, PA could inhibit both Gram-negative bacteria (25–768μg/mL) and Gram-positive bacteria (1.5–200μg/mL). Particularly, PA was active against some drug-resistant bacteria like methicillin-resistant Staphylococcus aureus (MRSA). PA also exhibited in vivo anti-MRSA activity in mice via intraperitoneal injection. PA could protect mice entirely infected with MRSA at 100 and 200 mg/kg, while 80% mice injected with MRSA could be protected at a low dose of 50μg/mL. Conclusion: PA might be a potential antibacterial drug from natural sources and might be worthy to explore its mechanism and application in further study. © 2016 Chinese Association of the Integration of Traditional and Western Medicine and Springer-Verlag Berlin Heidelberg Source


Gong X.-H.,Chengdu University of Traditional Chinese Medicine | Gong X.-H.,State Key Laboratory Breeding Base of Systematic Research | Li Y.,Chengdu University of Traditional Chinese Medicine | Li Y.,State Key Laboratory Breeding Base of Systematic Research | And 11 more authors.
Journal of Chromatographic Science | Year: 2016

A specific and sensitive UPLC-Q-TOF-MS method operated in the positive ion mode was developed and validated for the quantification of Fuziline in Beagle dog plasma. Fuziline and Neoline internal standard were separated on an Acquity UPLC BEH C18 column with the total running time of 4 min using gradient elution at the flow rate of 0.25 mL/min. The calibration curves for Fuziline showed good linearity in the concentrations ranging from 2 to 400 ng/mL with correlation coefficients (r) greater than 0.9971. The lower limit of quantification was 0.8 ng/mL. Intra- and interbatch relative standard deviations ranged from 2.11 to 3.11% and 3.12 to 3.81%, respectively. Fuziline was stable under different sample storage and processing conditions. The developed method was successfully applied to the comparative pharmacokinetic study of Fuziline in Beagle dog after intravenous and oral administration. Low absolute bioavailability of Fuziline (1.45 ± 0.76%) suggested a significant metabolism transformation extent in Beagle dog. © The Author 2015. Published by Oxford University Press. Source

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