期刊
JOURNAL OF BIOCHEMISTRY
卷 135, 期 1, 页码 85-91出版社
OXFORD UNIV PRESS
DOI: 10.1093/jb/mvh010
关键词
FAS; flavonoid; inhibition; inhibitor; morin
The inhibitory effects of 15 flavonoids on animal fatty acid synthase (FAS, EC 2.3.1.85) were investigated, and 9 of them were found to inhibit FAS with IC50 (the inhibitor concentration inhibiting 50% of the activity of FAS) values ranging from 2 to 112 muM. A structure-activity relationship study showed that the flavonoids containing two hydroxyl groups in the B ring and 5,7-hydroxyl groups in the A ring in combination with a C-2, 3 double bond were the most inhibitory. Morin (IC50 = 2.33 +/- 0.09 muM) was further investigated kinetically to detail the inhibitory mechanism. The results showed that morin inhibited the overall reaction of FAS competitively with Ac-CoA, noncompetitively with Mal-CoA and in a mixed manner with NADPH. The study indicated that morin bound reversibly to the beta-ketoacyl synthase domain of FAS to inhibit the elongation of the saturated acyl groups in fatty acids synthesis.
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