Inhibitory activity of diacylglycerol acyltransferase by tanshinones from the root of Salvia miltiorrhiza.
The inhibitory activity of tanshinones from Salvia miltiorrhiza was tested on rat liver diacylglycerol acyltransferase (DGAT). Cryptotanshinone (1) and 15,16-dihydrotanshinone I (3) exhibited potent DGAT inhibitory activities dose-dependently with IC50 values of 10.5 microg/ml and 11.1 microg/ml. However, tanshinone IIA (2) and tanshinone I (4) showed very weak inhibition (IC50 value: > 250 microg/ml). A dihydrofuran moiety was seemed to be responsible for the stronger inhibitory activity.
Ko
Jeong Suk
JS
Cardiovascular Research Laboratory, Korea Research Institute of Bioscience and Biotechnology, Yusong, Taejon.
Ryu
Shi Young
SY
Kim
Young Sup
YS
Chung
Mi Yeon
MY
Kang
Jong Seong
JS
Rho
Mun-Chual
MC
Lee
Hyun Sun
HS
Kim
Young Kook
YK
D045784:Abietanes; D000217:Acyltransferases / Q000037:antagonists & inhibitors*; D000818:Animals; D051048:Diacylglycerol O-Acyltransferase; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*; D066298:In Vitro Techniques; D008099:Liver / Q000187:drug effects / Q000201:enzymology; D008297:Male; D010616:Phenanthrenes / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*; D018517:Plant Roots / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D027544:Salvia / Q000737:chemistry*; D013624:Taiwan
D045784:Abietanes; D004791:Enzyme Inhibitors; D010616:Phenanthrenes; C021751:tanshinone; D000217:Acyltransferases; D051048:Diacylglycerol O-Acyltransferase