Baicalein inhibits adipocyte differentiation by enhancing COX-2 expression.

Baicalein, one of the major flavonoids in Scutellaria baicalensis (Chinese Skullcap), is well known for its effects on cell proliferation, apoptosis, and inflammation. Here we show that baicalein also inhibits the adipogenesis of 3T3-L1 preadipocytes. Baicalein inhibited triglyceride accumulation during adipogenesis and significantly decreased the mRNA expression of fatty acid-binding protein (FABP), a marker of adipogenesis. Microarray analysis revealed that several genes, which are differentially expressed during adipogenesis, were modulated by baicalein treatment in 3T-L1 cells. The expression of FABP, apolipoprotein D, and insulin-like growth factor 2, which was markedly up-regulated during adipogenesis, was down-regulated by baicalein. Cyclooxygenase (COX)-2 mRNA expression, which was decreased during adipogenesis, was up-regulated by baicalein. These COX-2 mRNA expression patterns were mirrored by the expression of COX-2 protein and its enzymatic activity. NS-398, a COX-2 inhibitor, partially abrogated the baicalein-induced inhibition of adipogenensis. Thus, the anti-adipogenic effect of baicalein may be mediated by its ability to enhance the expression of COX-2, which is normally down-regulated during adipogenesis.