Tenulin and isotenulin inhibit P-glycoprotein function and overcome multidrug resistance in cancer cells.

ABSTRACT:

Background

Multidrug resistance (MDR) in cancer is one of the main obstacles in treatment with chemotherapy. Drug efflux through P-glycoprotein is the major mechanism involved in MDR. A potential strategy to provide the best possible clinical outcomes is to develop P-glycoprotein (P-gp) inhibitors from natural products.

Purpose

The present study investigated the effects of the natural sesquiterpene lactone tenulin and its derivative isotenulin on human P-gp; the mechanisms of kinetic interactions were also explored.

Methods

The human P-gp (ABCB1/Flp-In™-293) stable expression cells were established by using the Flp-In™ system. The effects of tenulin and isotenulin on cell viability were evaluated by SRB assays in established cell lines, sensitive cancer cell line (HeL

SUBMITTER: Chang YT 

PROVIDER: S-EPMC6421864 | biostudies-literature | 2019 Feb

REPOSITORIES: biostudies-literature