In vitro inhibition of arterial myocyte growth and stimulation of low density lipoprotein metabolism by SIM 6080, a new calcium antagonist
Articolo
Data di Pubblicazione:
1990
Citazione:
In vitro inhibition of arterial myocyte growth and stimulation of low density lipoprotein metabolism by SIM 6080, a new calcium antagonist / F. Bernini, M. Fantoni, A. Corsini, R. Fumagalli. - In: PHARMACOLOGICAL RESEARCH. - ISSN 1043-6618. - 22:1(1990), pp. 27-35. [10.1016/1043-6618(90)90740-5]
Abstract:
We have investigated the in vitro effect of the new calcium antagonist SIM 6080 on proliferation of rat aortic smooth muscle cells and on LDL receptor-mediated catabolism in human fibroblasts. Verapamil was used as the reference compound. SIM 6080 inhibited the proliferation of rat aortic myocytes in concentrations ranging between 1 and 20 microM. The inhibition, evaluated as cell number and nuclear incorporation of [3H]thymidine, was dose and time dependent; the cell doubling time increased with drug concentrations up to 69 h versus 20 h for controls. Similar results on both LDL pathway and smooth muscle cell proliferation were achieved with verapamil, but higher concentrations were needed. The specific uptake and degradation of 125I-LDL was evaluated in human fibroblasts after 48 h incubation with SIM 6080 (1-10 microM). The compound dose dependently enhanced the receptor-mediated 125I-LDL uptake, with a fourfold increase as a maximal effect (10 microM); LDL degradation was less sensitive to the drug. The present results provide evidence that the new calcium antagonist SIM 6080 interferes in vitro with processes involved in atherogenesis.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
calcium antagonists; LDL; LDL receptor; myocyte proliferation
Elenco autori:
F. Bernini, M. Fantoni, A. Corsini, R. Fumagalli
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