The influence of trapidil and some of its derivatives (AR 12456, AR 12463, AR 12465) on the LDL receptor mediated uptake and degradation of 125 I-LDL by human skin fibroblasts (HSF) and human hepatic cells (HEP G2) was investigated. AR 12456 enhanced the uptake and degradation of 125 I-LDL in HEP G2, but inhibited this pathway in HSF. When this drug 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. Trapidil, AR 12463 and AR 12465 were inactive under the same experimental conditions. These findings suggest that a metabolite of AR 12456 might be responsible for the enhanced expression of LDL receptors in human cells.
Effect of derivatives of trapidil on the expression of LDL receptors / J. Beitz, A. Corsini, A. Granata, R. Fumagalli, H.J. Mest, R. Paoletti. - In: BIOMEDICA BIOCHIMICA ACTA. - ISSN 0232-766X. - 47:10-11(1988), pp. S153-S156.
|Titolo:||Effect of derivatives of trapidil on the expression of LDL receptors|
CORSINI, ALBERTO (Secondo)
PAOLETTI, RODOLFO (Ultimo)
|Parole Chiave:||Liver Neoplasms ; Skin ; Pyrimidines ; Receptors, LDL ; Cells, Cultured ; Carcinoma, Hepatocellular ; Kinetics ; Humans ; Trapidil ; Lipoproteins, LDL ; Antihypertensive Agents ; Cell Line|
|Settore Scientifico Disciplinare:||Settore BIO/14 - Farmacologia|
|Data di pubblicazione:||1988|
|Appare nelle tipologie:||01 - Articolo su periodico|