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|標題:||Epoxy type inhibitors of cholesterol esterase, acetylcholinesterase, and butyrylcholinesterase||作者:||Lin, G.L.
|關鍵字:||epoxy inhibitors;cholesterol esterase;acetylcholinesterase;butyrylcholinesterase;human-serum cholinesterase;para-nitrophenyl;lipase;binding;site;acid;rat;inactivation;purification;hydrolysis||Project:||Journal of the Chinese Chemical Society||期刊/報告no：:||Journal of the Chinese Chemical Society, Volume 47, Issue 2, Page(s) 397-404.||摘要:||
Epoxy type inhibitors, 3-t-butylphenyl 3-1,2-epoxybutyl ether (1), 3-t-butylphenyl 3-1,2-epoxyhexyl ether (2), and 2-naphthyl 3-1,2-epoxyhexyl ether (3) are synthesized as the active site-directed inhibitors of cholesterol esterase, acetylcholinesterase, and butyrylcholinesterase. All epoxy compounds are characterized as the time-independent inhibitors for all three enzymes from the stopped-time assay. Further, all epoxy compounds are characterized as the competitive inhibitors for all three enzymes from the Lineweavcr-Burk plots. The inhibition constants (K-i) of cholesterol esterase for compounds 1-3 are 320 +/- 40, 190 +/- 20, 130 +/- 20 mu M, respectively. The K-i values of acetylcholinesterase for compounds 1-3 are 490 +/- 20, 141 +/- 5, 200 +/- 30 mu M, respectively. Values of K-i of butyrylcholinesterase for compounds 1-3 are 250 +/- 30, 26 +/- 4, 120 +/- 20 mu M, respectively. Compound 2 is the most potent inhibitor for butyrylcholinesterase probably because the compound mimics most the natural substrate, butyrylcholine.
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