Acetylated and propionated derivatives of swertiamarin have anti-adipogenic effects

OBJECTIVE: To investigate whether the acetylated and propionated derivatives (LMP-09-1 and -2) of swertiamarin have anti-adipogenic effects. MATERIALS AND METHODS: 3T3-L1 pre-adipocytes were grown in Dulbecco's Modified Eagle's Medium (DMEM) containing 10% calf serum; fully confluent cells were differentiated with insulin, dexamethasone, and 3-isobutylmethylxanthine in the presence and absence of LMP-09-1 and -2 (100 μg/mL) for 10 days. Control cells received same amount of dimethylsulfoxide (DMSO). On day ten, cells were analyzed for triglycerides accumulation and the expression of genes involved in adipogenesis, lipogenesis, and lipolysis. In another set of experiment, effects of LMP-09-1 and 2 were studied for isoproterenol induced lipolysis using fully mature adipocytes. RESULTS: LMP-09-1 and -2 caused a significant (P < 0.001) reduction in intracellular triglycerides accumulation. Both LMP-09-1 and -2 significantly (P < 0.001) decreased the mRNA expression of peroxisome proliferator activated receptor-γ and acetyl-CoA carboxylase-1, and increased isoproterenol induced lipolysis in adipocytes. LMP-09-1 induced lipolysis even in the absence of isoproterenol, and also showed a significant up-regulation of carnitine palmitoyl transferase-1α and hormone sensitive lipase (HSL) gene expression. CONCLUSIONS: These findings show that swertiamarin derivatives, LMP-09-1 and -2 have a potent anti-adipogenic effect.