Inhibitory activity of diacylglycerol acyltransferase by glabrol isolated from the roots of licorice.
Acyl-coenzyme A: diacylglycerol acyltransferase (DGAT, EC 2.3.1.20) catalyzes triglyceride synthesis in the glycerol phosphate pathway. It has relations with the excess supply and accumulation of triglycerides. Therefore, DGAT inhibitors may act as a potential therapy for obesity and type 2 diabetes. Five flavonoids were isolated from the ethanol extracts of licorice roots, using an in vitro DGAT inhibitory assay. One isoprenyl flavonoid showed most potential inhibition of DGAT on five flavonoids (1-5). On the basis of spectral evidences, the compound was identified as glabrol (5). Compound 5 inhibited rat liver microsomal DGAT activity with an IC50 value of 8.0 microM, but the IC50 value for four flavonoids (1-4) was more than 100 microM. In addition, glabrol showed a noncompetitive type of inhibition against DGAT. These data suggest that potential therapy for the treatment in obesity and type 2 diabetes patients by licorice roots might be related with its DGAT inhibitory effect.
Choi
Jung Ho
JH
Jeonnam Institute of Natural Resources Research, Jangheung 529-851, Korea.
Choi
Ji Na
JN
Lee
Sung Yoon
SY
Lee
Sung Jae
SJ
Kim
Koanhoi
K
Kim
Young Kook
YK
D000818:Animals; D051048:Diacylglycerol O-Acyltransferase / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D005419:Flavonoids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D006035:Glycyrrhiza; D008297:Male; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology; D015394:Molecular Structure; D010936:Plant Extracts / Q000494:pharmacology*; D018517:Plant Roots / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D005419:Flavonoids; D010936:Plant Extracts; C420863:glabrol; D051048:Diacylglycerol O-Acyltransferase