Evaluation of the amine derivatives of Monascus pigment with anti-obesity activities

Forty-seven amine derivatives of Monascus pigment were produced via a series of fermentation and chemical derivation. Their anti-obesity activities were determined using cellular and mice tests. Among the derivatives, 16 derivatives showed an inhibitory activity against adipogenic differentiation in 3T3-L1 cells. Both the number and droplet size of fatty cells was reduced by treatment with the inhibitory derivatives. The derivatives of 4-phenylbutylamine (PBA) (2.5 mu M) and 2-(p-toyly) ethylamine (TEA) (12.5 mu M) caused approximately 40% inhibition. The transcription factors PPAR gamma and C/EBP alpha were down-regulated by the PBA derivative and the TEA derivative at 10 MM. When a high fat diet (HFD) supplemented with either 0.1 mg PBA derivative/g-mouse/day (PBA 0.1) or 0.4 mg TEA derivative/g-mouse/day (TEA 0.4) was fed to C57BL/6 mice, weight gain was reduced by 47.7% and 59.5%, respectively, compared to the HFD group. The smallest epididymal adipose tissue (EAT) size was obtained for the TEA 0.2 (HFD supplemented with 0.2 mg TEA/g-mouse/day) group and confirmed by micro-CT images. Supplementation of TEA derivative reduced the total cholesterol content in mice serum, especially LDL. Thus, HTR values increased and Al values decreased, indicating that the supplement has an anti-obesity effect. (C) 2012 Elsevier Ltd. All rights reserved.