In this section, you can access to the latest technical information related to the FUTURE project topic.

Clarify the potential cholestatic hepatotoxicity components from Chinese Herb Medicine and metabolism?s role via hBSEP vesicles and S9/hBSEP vesicles

In this study, the inhibitory effect of components from Chinese Herb Medicine (CHMs) with potential hepatotoxicity was assessed by human bile salt export pump (hBSEP) vesicles with and without S9 metabolism. Sixty-three compounds from 22 hepatoxicity CHMs were selected as the test articles. In hBSEP vesicles, eighteen of them were found to have moderate or strong inhibitory effect towards BSEP. Further studies were performed to determine the IC50 values of strong inhibitors. For the compounds belong to CHMs reported to cause cholestasis and strong inhibitors defined in hBSEP vesicles, their relative transport activities of Taurocholic acid (TCA) were evaluated in hBSEP vesicles as well as hBSEP vesicles with S9 system (S9/hBSEP vesicles). The differences of their relative transport activities of TCA between the above two system were compared to reveal the net effect of metabolism on BSEP's activity. It was found that the inhibitory effect of Saikogenin A (SGA), Saikogenin D (SGD), Diosbulbin B (DB) and rhein were significantly increased; while the inhibitory effect of isobavachalcone, saikosaponin d and saikosaponin b2 were significantly decreased after S9 metabolizing. Identification of metabolic pathways suggested that CYP3A4 was responsible for aggravating inhibitory effect of SGA and SGD against BSEP.

» Author: Yue Li, Dongming Yan, Jingyi Jin, Bo Tan, Xi Chen, Bin Zou, Guochao Song, Fengyi Weng, Chenghai Liu, Furong Qiu

» Publication Date: 01/04/2022

» More Information

« Go to Technological Watch



AIMPLAS Instituto Tecnológico del Plástico

C/ Gustave Eiffel, 4
(València Parc Tecnològic) - 46980
PATERNA (Valencia) - SPAIN

PHONE

(+34) 96 136 60 40

EMAIL

Project Management department - Sustainability and Industrial Recovery
life-future-project@aimplas.es