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|標題:||Kinetics and mechanisms of cholesterol esterase inhibition by cardiovascular drugs in vitro||作者:||Chiou, S.Y.
|關鍵字:||cholesterol esterase inhibition;enzyme kinetics;cardiovascular drugs;salt-activated lipase||Project:||Indian Journal of Biochemistry & Biophysics||期刊/報告no：:||Indian Journal of Biochemistry & Biophysics, Volume 43, Issue 1, Page(s) 52-55.||摘要:||
Cardiovascular drugs such as lovastatin, simvastatin, amlodipine besylate, nifedipine, and hydralazine hydrochloride inhibit,cholesterol esterase (CEase) in vitro. In the present paper, an attempt was made to determine kinetically the reaction mechanism for CEase inhibition by these drugs. The inhibition constant, K-i, for the mixed-type inhibition of CEase by these drugs in the presence of triton-X-100 or taurochloate were measured. Moreover, the pK(i) values were correlated with the molecular weights of these drugs. In conclusion, the fact that these drugs lower cholesterol levels in the plasma low-density lipoprotein may be partially due to the CEase inhibition by these drugs.
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