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Kinetics and mechanisms of cholesterol esterase inhibition by cardiovascular drugs in vitro

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Title Kinetics and mechanisms of cholesterol esterase inhibition by cardiovascular drugs in vitro
 
Creator Chiou, Shyh-Ying
Lai, Gin-Win
Lin, Long-Yau
Lin, Gialih
 
Subject Cholesterol esterase inhibition
Enzyme kinetics
Cardiovascular drugs
 
Description 52-55
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.
 
Date 2009-02-24T04:36:56Z
2009-02-24T04:36:56Z
2006-02
 
Type Article
 
Identifier 0301-1208
http://hdl.handle.net/123456789/3234
 
Language en_US
 
Relation C12N9/99
 
Publisher CSIR
 
Source IJBB Vol.43(1) [February 2006]