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Acetylated and propionated derivatives of swertiamarin have anti-adipogenic effects.

Vaidya HB, Goyal RK, Cheema SK - J Pharmacol Pharmacother (2014)

Bottom Line: 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.These findings show that swertiamarin derivatives, LMP-09-1 and -2 have a potent anti-adipogenic effect.

View Article: PubMed Central - PubMed

Affiliation: Department of Biochemistry, Memorial University, St. John's, Canada.

ABSTRACT

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.

No MeSH data available.


Related in: MedlinePlus

Effects of LMP-09-1 and LMP-09-2 on the mRNA expression of a) PPAR-γ, b) C/EBPα; and c) ACC-1 in 10 day fully differentiated 3T3-L1 adipocytes. Values are presented as mean ± SD, n = 3. * indicates significantly (P < 0.001) different than control
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Figure 3: Effects of LMP-09-1 and LMP-09-2 on the mRNA expression of a) PPAR-γ, b) C/EBPα; and c) ACC-1 in 10 day fully differentiated 3T3-L1 adipocytes. Values are presented as mean ± SD, n = 3. * indicates significantly (P < 0.001) different than control

Mentions: PPAR-γ is a marker gene associated with adipogenesis. We measured the effects of LMP-09-1 and -2 on the mRNA expression of PPAR-γ to investigate whether a decrease in triglycerides accumulation corresponds with inhibition of PPAR-γ. Both LMP-09-1 and -2 significantly (P < 0.001) reduced the mRNA expression of PPAR-γ compared to the control cells [Figure 2a]; however there was no effect of the treatments on C/EBP-α mRNA expression [Figure 2b].


Acetylated and propionated derivatives of swertiamarin have anti-adipogenic effects.

Vaidya HB, Goyal RK, Cheema SK - J Pharmacol Pharmacother (2014)

Effects of LMP-09-1 and LMP-09-2 on the mRNA expression of a) PPAR-γ, b) C/EBPα; and c) ACC-1 in 10 day fully differentiated 3T3-L1 adipocytes. Values are presented as mean ± SD, n = 3. * indicates significantly (P < 0.001) different than control
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4231551&req=5

Figure 3: Effects of LMP-09-1 and LMP-09-2 on the mRNA expression of a) PPAR-γ, b) C/EBPα; and c) ACC-1 in 10 day fully differentiated 3T3-L1 adipocytes. Values are presented as mean ± SD, n = 3. * indicates significantly (P < 0.001) different than control
Mentions: PPAR-γ is a marker gene associated with adipogenesis. We measured the effects of LMP-09-1 and -2 on the mRNA expression of PPAR-γ to investigate whether a decrease in triglycerides accumulation corresponds with inhibition of PPAR-γ. Both LMP-09-1 and -2 significantly (P < 0.001) reduced the mRNA expression of PPAR-γ compared to the control cells [Figure 2a]; however there was no effect of the treatments on C/EBP-α mRNA expression [Figure 2b].

Bottom Line: 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.These findings show that swertiamarin derivatives, LMP-09-1 and -2 have a potent anti-adipogenic effect.

View Article: PubMed Central - PubMed

Affiliation: Department of Biochemistry, Memorial University, St. John's, Canada.

ABSTRACT

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.

No MeSH data available.


Related in: MedlinePlus