The in vitro transport mechanism of bentysrepinine:a novel anti-hepatitis B virus drug candidate
10.16438/j.0513-4870.2016-0009
- VernacularTitle:抗乙肝候选新药替芬泰的体外转运机制研究
- Author:
Hui-rong FAN
1
;
Xiao-yan CI
2
;
Wei LI
2
;
Yong ZENG
2
;
Xiu-lin YI
2
;
Duan-yun SI
2
;
Chang-xiao LIU
2
;
Guang-yi LIANG
3
Author Information
1. Tianjin Key Laboratory of Radiation Medicine and Molecular Nuclear Medicine, Institute of Radiation Medicine, Chinese Academy of Medical Sciences and Peking Union Medical College, Tianjin 300192, China
2. State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China
3. The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, Guiyang 550002, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
bentysrepinine;
in vitro transport mechanism;
gene-transfected cell;
MDCK-MDR1;
HEK293-hOATP1B1;
HEK293-hOATP2B1;
CHO-PEPT
- From:
Acta Pharmaceutica Sinica
2016;51(8):1233-
- CountryChina
- Language:Chinese
-
Abstract:
Bentysrepinine (Y101), a derivative of phenylalanine dipeptide, is a novel drug candidate for the treatment of hepatitis B virus (HBV) infection. Our previous preclinical pharmacokinetic study showed that its in vivo absorption and distribution characteristics were probably related to transmembrane transport after Y101 was administered intragastically in rats. In this study, Caco-2 and MDCK-MDR1 cell models were used to investigate interactions between Y101 and P-gp through the apparent permeation coefficient (Papp) and efflux ratio (RE); the results showed that Y101 was a substrate of P-gp. In addition, gene-transfected cell models, HEK293-hOATP1B1, HEK293-hOATP2B1 and CHO-PEPT1 were used to evaluate the affinity to OATP1B1,
