Transport mechanism of danshensu across Caco-2 monolayer model.
- Author:
Di-Feng ZHU
1
;
Xiao-Ping ZHAO
;
Yi-Yu CHENG
Author Information
- Publication Type:Journal Article
- MeSH: ATP-Binding Cassette, Sub-Family B, Member 1; antagonists & inhibitors; Caco-2 Cells; Cell Membrane Permeability; drug effects; Dose-Response Relationship, Drug; Drugs, Chinese Herbal; administration & dosage; pharmacokinetics; Humans; Lactates; administration & dosage; pharmacokinetics; Plants, Medicinal; chemistry; Salvia miltiorrhiza; chemistry; Verapamil; pharmacology
- From: China Journal of Chinese Materia Medica 2006;31(18):1517-1521
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVETo study the absorption mechanism of Danshensu by using Caco-2 monolayer model .
METHODCaco-2 cell monolayer model was used to study the bi-direction transport of Danshensu. An LC-MS method was developed to measure the concentration of Danshensu in cell culture medium and calculate the apparent permeability coefficients (P(app)). The effects of time, drug concentration and inhibitor on the absorption of Danshensu were studied.
RESULTTransport of Danshensu was time and concentration dependent, and it was also effected by P-glycoprotein inhibitor. P(app) increased with time increase and tended to become saturated at some point. It, however,decreased while concentration of Danshensu increased. P(ratio) is larger than 1.5 . Verapamil can cause significantly effect on transport of Danshensu: P(app,A-B) increased and P(app,B-A) decreased .
CONCLUSIONThe absorption of Danshensu in Caco-2 cell model may be an active transportation mediated by P-glycoprotein transporter.
