Abstract
The effect of trapidil (RocornalR) and some of its newly developed derivatives on the receptor-mediated low density lipoprotein (LDL) uptake and degradation was studied in human skin fibroblasts (HSF) and human hepatoma cell line Hep G2. One compound (AR 12456) influenced this pathway in a selective way: it enhanced the uptake and degradation of 125 I-LDL by Hep G2 cells in a dose-dependent manner, but inhibited it in HSF. When AR 12456 was preincubated with Hep G2 cells and then the incubation medium was transferred to HSF, a stimulation of specific LDL pathway occurred also in this cell line. The stimulation of the LDL pathway by AR 12456 in Hep G2 was modified by preincubation of Hep G2 cells with agents known to induce drug metabolism enzymes. These findings suggest that a metabolite(s) of AR 12456 might be responsible for the enhanced expression of LDL receptors in cultured human cells.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
