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Phytomedicine. 2013 Aug 15;20(11):1030-8. doi: 10.1016/j.phymed.2013.04.005. Epub 2013 Jun 2.

In vitro to in vivo evidence of the inhibitor characteristics of Schisandra lignans toward P-glycoprotein.

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State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China.


Concomitant administration of herbal medicines with drugs that are P-glycoprotein (P-gp) substrates may produce significant herb-drug interactions. The purpose of this study was to evaluate the effects of Schisandra lignans extract (SLE) on P-gp thoroughly in vitro and in vivo, and to investigate the possible P-gp-based herb-drug interactions. In the in vitro experiments, the effect of SLE on the uptake and transport for P-gp substrates in Caco-2, LLC-PK1 and L-MDR1 cells were carefully investigated. Verapamil, a known P-gp inhibitor, was used as a positive control drug. Results shown that, 10 μM verapamil and SLE (0.5, 2.0, and 10.0 μg/ml) were observed to significantly enhance the uptake and inhibit the efflux ratio of P-gp substrates in Caco-2 and L-MDR1 cells. In vivo experiments showed that single-dose SLE at 500 mg/kg could increase the area under the plasma concentration time curve of digoxin and vincrisine significantly without affecting terminal elimination half-time. Long-term treatment with SLE for continuous 10 days could also increase the absorption of P-gp substrates with greatly down regulation of P-gp expression in rat intestinal and brain tissues. In conclusion, SLE was a strong P-gp inhibitor, which indicated a potential herb-drug interaction when SLE was co-administered with P-gp substrate drugs.


AP; AUC; BL; C(max); CL; CMC-Na; DDI; DGX; HBSS; HMs; HPLC; Hank's balanced salt solution; Herb–drug interaction; Inhibitor; LC/MS; LC–IT-TOF/MS; P-glycoprotein; P-gp; SLE; Schisandra lignans extract; TBS-T; Tris-buffered saline-Tween 20; VCR; apical; basolateral; clearance; digoxin; drug–drug interaction; half-life time; herbal medicines; high-performance liquid chromatography; liquid chromatography combined hybrid ion trap time-of-flight mass spectrometry; liquid chromatography combined mass spectrometry; maximum plasma concentration; sodium carboxymethyl cellulose; t(1/2); the area under the concentration–time curve; vincrisine

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