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

• Published in: Bioorganic & medicinal chemistry letters 2004-08, Vol.14 (16), p.4277-4280
• Main Authors: Xu, Ming-Zhe, Lee, Woo Song, Kim, Mi Jeong, Park, Doo-Sang, Yu, Hana, Tian, Guan-Rong, Jeong, Tae-Sook, Park, Ho-Yong
• Format: Article
• Language: English
• Subjects: ACAT inhibitors; Amides - chemistry; Amides - isolation & purification; Amides - pharmacology; Animals; Biological and medical sciences; Fatty Acids - chemistry; Fatty Acids - isolation & purification; Fatty Acids - pharmacology; General pharmacology; Medical sciences; Microsomes, Liver - enzymology; Mylabris phalerate Pallas; Pharmacognosy. Homeopathy. Health food; Pharmacology. Drug treatments; Rats; Spectrometry, Mass, Electrospray Ionization; Sterol O-Acyltransferase - antagonists & inhibitors; Sterol O-Acyltransferase - metabolism; Tenebrio - chemistry; The insect
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2004.05.086

Unsaturated fatty acid amides 2 and 4, isolated from Mylabris phalerate Pallas, inhibited rat liver microsomal ACAT, hACAT-1, and -2 activities. 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 μM for 2 and of 151, 53, and 45 μM for 4, respectively.