Kinetics and mechanisms of cholesterol esterase inhibition by cardiovascular drugs in vitro.
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.
Chiou
Shyh-Ying
SY
Institute of Medicine and Department of Neurosurgery, Chung Shan Medical University, Taichung, Taiwan.
Lai
Gin-Win
GW
Lin
Long-Yau
LY
Lin
Gialih
G
D017311:Amlodipine / Q000494:pharmacology; D002317:Cardiovascular Agents / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006830:Hydralazine / Q000494:pharmacology; D007700:Kinetics; D009543:Nifedipine / Q000494:pharmacology; D017830:Octoxynol; D019821:Simvastatin / Q000494:pharmacology; D002787:Sterol Esterase / Q000037:antagonists & inhibitors*; D013656:Taurocholic Acid
D002317:Cardiovascular Agents; D004791:Enzyme Inhibitors; D017311:Amlodipine; D006830:Hydralazine; D013656:Taurocholic Acid; D017830:Octoxynol; D019821:Simvastatin; D002787:Sterol Esterase; D009543:Nifedipine