[Transport mechanism of danshensu across Caco-2 monolayer model].
OBJECTIVE
To study the absorption mechanism of Danshensu by using Caco-2 monolayer model .


METHODS
Caco-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.


RESULTS
Transport 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 .


CONCLUSIONS
The absorption of Danshensu in Caco-2 cell model may be an active transportation mediated by P-glycoprotein transporter.
Zhu
Di-Feng
DF
Pharmaceutical Informatics Institute, Zhejiang University, Hangzhou 310027, China.
Zhao
Xiao-Ping
XP
Cheng
Yi-Yu
YY
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors; D018938:Caco-2 Cells; D002463:Cell Membrane Permeability / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006801:Humans; D007773:Lactates / Q000008:administration & dosage / Q000493:pharmacokinetics*; D010946:Plants, Medicinal / Q000737:chemistry; D027561:Salvia miltiorrhiza / Q000737:chemistry; D014700:Verapamil / Q000494:pharmacology
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D004365:Drugs, Chinese Herbal; D007773:Lactates; C035055:3,4-dihydroxyphenyllactic acid; D014700:Verapamil