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
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
Xiong L.,State Key Laboratory Breed Base Of Systems Res Development And Utilization Of Chinese Medicine Resources |
Xiong L.,Key Laboratory of Standardization of Chinese Herbal Medicine |
Xiong L.,Chengdu University of Traditional Chinese Medicine |
Peng C.,State Key Laboratory Breed Base Of Systems Res Development And Utilization Of Chinese Medicine Resources |
And 23 more authors.
Two new alkaloids, aconicarmine (1) and aconicaramide (5), were isolated from the EtOH extract of the lateral roots of Aconitum carmichaelii, together with five known compounds: fuziline (2), neoline (3), N-ethylhokbusine B (4), 5-hydroxymethylpyrrole-2- carbaldehyde (6), and oleracein E (7). Their structures were elucidated by physical and NMR analysis. Pyrrole alkaloids were isolated from A. carmichaelii for the first time. In the in vitro assays, compounds 2 and 3 showed activity against pentobarbital sodiuminduced cardiomyocytes damage by obviously recovering beating rhythm and increasing the cell viability, while compounds 5 and 7 showed moderate antibacterial activity. Source