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Title 

Human Acyl-CoA: cholesterol acyltransferase inhibitory activities of aliphatic acid amides from Zanthoxylum piperitum DC

Authors 

Yong-Dae ParkWoo Song LeeSo-Jin AnTae Sook Jeong

Publisher 

Pharmaceutical Society of Japan

Issue Date 

2007

Citation 

Biological & Pharmaceutical Bulletin, vol. 30, no. 1, pp. 205-207

Keywords 

aliphatic acid amideatherosclerosischolesterol acytransferase (hACAT)human acyl-CoAzanthoxylum piperitum DCacyl coenzyme Aamidebeta sanshool acetic acidcholesterol acyltransferasezanthoxylym piperitum extract

Abstract 

Acyl-CoA: cholesterol acyltransferase (ACAT) plays an important role in the esterification of cholesterol with its substrates, cholesterol and fatty acyl coenzyme A, to facilitate both intracellular storage and intercellular transport. ACAT-1 is more involved in macrophage foam cell formation and ACAT-2 plays a critical role in the cholesterol absorption process in intestinal enterocytes. Three aliphatic acid amides, β-sanshool (1), γ-sanshool (2), and hydroxy-β-sanshool (3), were isolated by bioassay-guided fractionation of the ethanolic extracts of Zanthoxylum piperitum DC. Compounds 1 and 2 inhibited human ACAT-1 and -2 activities with IC50 values of 39.0 and 79.7 μM for 1 and of 12.0 and 82.6 μM for 2, respectively. However, the hACAT-1 and -2 inhibitory activities of compound 3 having hydroxyl group were relatively less than those of compounds 1 and 2. A semi-synthetic compound 4, which has acetyl residue at 2′-OH of compound 3, exhibited the increased hACAT-1 and -2 inhibitory activities with IC50 values of 28.1 and 87.5 μM, respectively.

ISSN 

0918-6158

Link 

http://dx.doi.org/10.1248/bpb.30.205

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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