Leoligin, the major lignan from Edelweiss, activates cholesteryl ester transfer protein.

ABSTRACT:

Objective

Cholesteryl ester transfer protein (CETP) plays a central role in the metabolism of high-density lipoprotein particles. Therefore, we searched for new drugs that bind to CETP and modulate its activity.

Methods

A preliminary pharmacophore-based parallel screening approach indicated that leoligin, a major lignan of Edelweiss (Leontopodium alpinum Cass.), might bind to CETP. Therefore we incubated leoligin ex vivo at different concentrations with human (n=20) and rabbit plasma (n=3), and quantified the CETP activity by fluorimeter. Probucol served as positive control. Furthermore, we dosed CETP transgenic mice with leoligin and vehicle control by oral gavage for 7 days and measured subsequently the in vivo modulation of CETP activity (n=5 for each treatment group).

SUBMITTER: Duwensee K 

PROVIDER: S-EPMC3212649 | biostudies-literature | 2011 Nov

REPOSITORIES: biostudies-literature