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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

a) Effects of LMP-09-1 and LMP-09-2 on cell viability of 3T3-L1 cells, b) Oil Red O staining of 3T3-L1 cells on day 10; the original magnification was × 100, c) Intracellular triglycerides accumulation was measured using triglycerides assay kit after lipid extraction in 10 day fully differentiated 3T3-L1 cells as described in methods. Values are presented as mean ± SD, n = 3. * indicates significantly (P < 0.001) different than control
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Figure 2: a) Effects of LMP-09-1 and LMP-09-2 on cell viability of 3T3-L1 cells, b) Oil Red O staining of 3T3-L1 cells on day 10; the original magnification was × 100, c) Intracellular triglycerides accumulation was measured using triglycerides assay kit after lipid extraction in 10 day fully differentiated 3T3-L1 cells as described in methods. Values are presented as mean ± SD, n = 3. * indicates significantly (P < 0.001) different than control

Mentions: The viability assay was used to determine suitable dose and possible cytotoxic effect of LMP-09-1 and -2 on adipocytes. 3T3-L1 preadipocytes were incubated in the presence of different doses of LMP-09-1 and -2 (10, 50, 100 and 250 μg/ml) for 48 h. As shown in Figure 1a, treatment with LMP-09-1 and -2 at all tested concentrations did not affect cell viability.


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

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

a) Effects of LMP-09-1 and LMP-09-2 on cell viability of 3T3-L1 cells, b) Oil Red O staining of 3T3-L1 cells on day 10; the original magnification was × 100, c) Intracellular triglycerides accumulation was measured using triglycerides assay kit after lipid extraction in 10 day fully differentiated 3T3-L1 cells as described in methods. 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 2: a) Effects of LMP-09-1 and LMP-09-2 on cell viability of 3T3-L1 cells, b) Oil Red O staining of 3T3-L1 cells on day 10; the original magnification was × 100, c) Intracellular triglycerides accumulation was measured using triglycerides assay kit after lipid extraction in 10 day fully differentiated 3T3-L1 cells as described in methods. Values are presented as mean ± SD, n = 3. * indicates significantly (P < 0.001) different than control
Mentions: The viability assay was used to determine suitable dose and possible cytotoxic effect of LMP-09-1 and -2 on adipocytes. 3T3-L1 preadipocytes were incubated in the presence of different doses of LMP-09-1 and -2 (10, 50, 100 and 250 μg/ml) for 48 h. As shown in Figure 1a, treatment with LMP-09-1 and -2 at all tested concentrations did not affect cell viability.

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