酯抑素：一种有效的溶酶体酸性脂肪酶抑制剂。

Esterastin: a potent inhibitor of lysosomal acid lipase.

作者信息

Imanaka T, Moriyama Y, Ecsedi G G, Aoyagi T, Amanuma-Muto K, Ohkuma S, Takano T

出版信息

J Biochem. 1983 Sep;94(3):1017-20. doi: 10.1093/oxfordjournals.jbchem.a134399.

DOI:10.1093/oxfordjournals.jbchem.a134399

Abstract

The effect of a fungal metabolite, esterastin, on lysosomal acid lipase purified from rabbit liver was studied. Esterastin inhibited the enzyme activity very strongly (IC50, about 80 nM). The inhibition of acid lipase by esterastin was competitive with respect to the substrate and the inhibition constant for esterastin was 90 nM. Esterastin was less inhibitory to other lipolytic enzymes, such as pancreatic lipase and carboxylesterase. Thus esterastin is a potent new inhibitor of lysosomal acid lipase.

摘要

研究了一种真菌代谢产物酯酶抑制素对从兔肝脏纯化的溶酶体酸性脂肪酶的作用。酯酶抑制素能非常强烈地抑制该酶的活性（IC50约为80 nM）。酯酶抑制素对酸性脂肪酶的抑制作用在底物方面具有竞争性，其对酯酶抑制素的抑制常数为90 nM。酯酶抑制素对其他脂解酶，如胰脂肪酶和羧酸酯酶的抑制作用较弱。因此，酯酶抑制素是溶酶体酸性脂肪酶的一种强效新型抑制剂。