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

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

doi:10.1016/j.bmcl.2004.05.086

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

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

Authors

Ming-Zhe Xu¹, Woo Song Lee, Mi Jeong Kim, Doo-Sang Park, Hana Yu, Guan-Rong Tian, Tae-Sook Jeong, Ho-Yong Park

Affiliation

¹ Insect Resources Laboratory, Korea Research Institute of Bioscience and Biotechnology, 52 Oun, Yusong, Daejeon 305-333, Republic of Korea.

PMID: 15261286
DOI: 10.1016/j.bmcl.2004.05.086

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Amides / chemistry
Amides / isolation & purification
Amides / pharmacology*
Animals
Fatty Acids / chemistry
Fatty Acids / isolation & purification
Fatty Acids / pharmacology*
Microsomes, Liver / enzymology
Rats
Spectrometry, Mass, Electrospray Ionization
Sterol O-Acyltransferase / antagonists & inhibitors*
Sterol O-Acyltransferase / metabolism
Tenebrio / chemistry*

Substances

Amides
Fatty Acids
Sterol O-Acyltransferase