从大斑芫菁中分离得到的脂肪酸酰胺的酰基辅酶A：胆固醇酰基转移酶抑制活性

Acyl-CoA: cholesterol acyltransferase inhibitory activities of fatty acid amides isolated from Mylabris phalerate Pallas.

作者信息

Xu Ming-Zhe, Lee Woo Song, Kim Mi Jeong, Park Doo-Sang, Yu Hana, Tian Guan-Rong, Jeong Tae-Sook, Park Ho-Yong

机构信息

Insect Resources Laboratory, Korea Research Institute of Bioscience and Biotechnology, 52 Oun, Yusong, Daejeon 305-333, Republic of Korea.

出版信息

Bioorg Med Chem Lett. 2004 Aug 16;14(16):4277-80. doi: 10.1016/j.bmcl.2004.05.086.

DOI:10.1016/j.bmcl.2004.05.086

PMID:15261286

Abstract

Unsaturated fatty acid amides, 9(Z)-octadecenamide (2) and 9(Z),12(Z)-octadecadienamide (4) as inhibitors of acyl-CoA: cholesterol acyltransferase (ACAT) were isolated from the ethyl acetate extracts of the insect, Mylabris phalerate Pallas, and elucidated by their spectroscopic data analysis. Compounds 2 and 4 inhibited rat liver microsomal ACAT, hACAT-1, and hACAT-2 with IC(50) values of 170, 85, and 63 microM for 2 and of 151, 53, and 45 microM for 4, respectively.

摘要

从昆虫斑蝥（Mylabris phalerate Pallas）的乙酸乙酯提取物中分离出不饱和脂肪酸酰胺9(Z)-十八碳烯酰胺（2）和9(Z),12(Z)-十八碳二烯酰胺（4），它们作为酰基辅酶A：胆固醇酰基转移酶（ACAT）的抑制剂，并通过光谱数据分析对其进行了鉴定。化合物2和4对大鼠肝微粒体ACAT、hACAT-1和hACAT-2均有抑制作用，化合物2的IC(50)值分别为170、85和63 microM，化合物4的IC(50)值分别为151、53和45 microM。