尼卡地平与硝苯地平可抑制大鼠肝脏微粒体中的脂肪酸去饱和酶。

Nicardipine and nifedipine inhibit fatty acid desaturases in rat liver microsomes.

作者信息

Kawashima H, Akimoto K, Jareonkitmongkol S, Shirasaka N, Shimizu S

机构信息

Department of Agricultural Chemistry, Faculty of Agriculture, Kyoto University, Japan.

出版信息

Biosci Biotechnol Biochem. 1996 Oct;60(10):1672-6. doi: 10.1271/bbb.60.1672.

DOI:10.1271/bbb.60.1672

PMID:8987667

Abstract

Nicardipine and nifedipine, Ca channel blockers, inhibited rat liver microsomal desaturases, though verapamil, methoxyverapamil, cinnarizine, flunarizine, and diltiazem did not. However, nicardipine and nefidipine apparently did not inhibit the fungal desaturation in Mortierella alpina 1S-4. Nicardipine inhibited rat liver microsomal delta 5 desaturase specifically (50% inhibitory concentration. 170 microM), and nifedipine inhibited delta 6 desaturase specifically (78 microM). The inhibition by nicardipine and nifedipine is uncompetitive, the Ki values for delta 5 and delta 6 desaturases being 62 and 44 microM, respectively.

摘要

钙通道阻滞剂尼卡地平与硝苯地平可抑制大鼠肝脏微粒体去饱和酶，但维拉帕米、甲氧基维拉帕米、桂利嗪、氟桂利嗪及地尔硫䓬则无此作用。然而，尼卡地平与尼非地平显然并不抑制高山被孢霉1S - 4中的真菌去饱和作用。尼卡地平特异性抑制大鼠肝脏微粒体δ5去饱和酶（50%抑制浓度为170微摩尔），而硝苯地平则特异性抑制δ6去饱和酶（78微摩尔）。尼卡地平和硝苯地平的抑制作用为非竞争性，δ5和δ6去饱和酶的Ki值分别为62和44微摩尔。