Effect of scopoletin on lipoprotein lipase activity in 3T3-L1 adipocytes.

Hypertriglyceridemia is an independent risk factor of cardiovascular diseases. It is caused by the imbalance between hepatic triglyceride production and peripheral removal. Lipoprotein lipase (LPL) plays a central role in the removal of plasma triglyceride. During the screening of possible anti-dyslipidemic drugs, we observed that scopoletin (6-methoxy-7-hydroxycoumarin) significantly increased LPL activity in adipocytes. Scopoletin increased LPL activity in culture medium of 3T3-L1 adipocytes in dose- and time-dependent manners. It did not release LPL from the adipocyte membrane and, instead, increased the LPL mRNA level, suggesting transcriptional control. Scopoletin also partially reversed tumor necrosis factor-alpha-induced suppression of LPL activity. These results suggest the possible action of scopoletin as a facilitator of plasma triglyceride clearance.