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Title: Kinetics and mechanisms of cholesterol esterase inhibition by cardiovascular drugs in vitro
Authors: Chiou, Shyh-Ying
Lai, Gin-Win
Lin, Long-Yau
Lin, Gialih
Keywords: Cholesterol esterase inhibition
Enzyme kinetics
Cardiovascular drugs
Issue Date: Feb-2006
Publisher: CSIR
IPC CodeC12N9/99
Abstract: 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, Ki, for the mixed-type inhibition of CEase by these drugs in the presence of triton-X-100 or taurochloate were measured. Moreover, the pKi 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.
Page(s): 52-55
ISSN: 0301-1208
Source:IJBB Vol.43(1) [February 2006]

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