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

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 (AC...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2004-08, Vol.14 (16), p.4277-4280
Hauptverfasser:	Xu, Ming-Zhe, Lee, Woo Song, Kim, Mi Jeong, Park, Doo-Sang, Yu, Hana, Tian, Guan-Rong, Jeong, Tae-Sook, Park, Ho-Yong
Format:	Artikel
Sprache:	eng
Schlagworte:	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
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2004.05.086