[Metabolism of cholesterol esters in cultured macrophages under the action of the calcium antagonists verapamil and nifedipine].
Using mouse macrophage cultures, the effects of verapamil and nifedipine on cholesterol ester metabolism were studied with special reference to the following parameters: i) incorporation of 14C-oleate into cholesterol esters (ChE), ii) contents of common and free cholesterol (FCh), iii) removal of 14C-oleate from ChE and incorporation of 3H-FCh into ChE and, iiii) excretion of 3H-Ch from the cells. Verapamil and nifedipine (10-100 microM) decreased the incorporation of 14C-oleate into ChE, increased the concentration of FCh but had no appreciable effect on the concentration of common Ch in macrophages cultured in the presence of acetylated low density lipoproteins. The drugs stimulated the removal of 14C-oleate from cellular ChE. The pharmacological concentrations (25-75 microM) of verapamil and nifedipine increased the excretion of 3H-Ch from ChE of macrophages in the presence of serum and high density lipoproteins. The results obtained suggest that verapamil and nifedipine mediate the antiatherosclerotic effect via reduction of intracellular synthesis of ChE, stimulation of ChE hydrolysis and cholesterol excretion from the cells.
Dushkin
M I
MI
Ivanova
M V
MV
D000818:Animals; D002784:Cholesterol / Q000378:metabolism; D002788:Cholesterol Esters / Q000378:metabolism*; D006868:Hydrolysis; D008077:Lipoproteins, LDL / Q000378:metabolism; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism*; D051379:Mice; D008810:Mice, Inbred C57BL; D009543:Nifedipine / Q000494:pharmacology*; D014700:Verapamil / Q000494:pharmacology*
D002788:Cholesterol Esters; D008077:Lipoproteins, LDL; D002784:Cholesterol; D014700:Verapamil; D009543:Nifedipine
Metabolizm éfirov kholesterina v kul'tiviruemykh makrofagakh pri vozdeĭstvii antagonistov kal'tsiia verapamila i nifedipina.