[The in vitro transport mechanism of bentysrepinine: a novel anti-hepatitis B virus drug candidate].
Yao Xue Xue Bao
; 51(8): 1233-9, 2016 08.
Article
in Zh
| MEDLINE
| ID: mdl-29897720
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 (P(app)) and efflux ratio (RE); the results showed that Y101 was a substrate of P-gp. In addition, gene-transfected cell models, HEK293-h OATP1B1, HEK293-h OATP2B1 and CHO-PEPT1 were used to evaluate the affinity to OATP1B1, OATP2B1 and PEPT1. The results suggest that Y101 has a weak inhibitory effect on OATP1B1 and OATP2B1, and Y101 may not be substrates of OATP1B1, OATP2B1 or PEPT1. The above results can be used to explain the in vivo absorption and distribution characteristics, and to provide a scientific basis for the further development of Y101.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Antiviral Agents
/
Benzamides
/
Hepatitis B virus
/
Dipeptides
Type of study:
Prognostic_studies
Limits:
Animals
/
Humans
Language:
Zh
Journal:
Yao Xue Xue Bao
Year:
2016
Document type:
Article