Forskolin boosts fat release, especially if used in high concentrations and if combined with caffeine, exercise and dieting

  • In this study it was found that:
    • forskolin boosts fat release due to adrenergic stimulation (this suggests that combining exercise and forskolin would produce maximum results)
    • that adrenergic stimulation is stronger than forskolin in stimulating lipolysis (this means that higher concentrations of forskolin are needed than adrenergic stimulation, in order to produce the same lipolytic result)
    • that insulin and adenosine inhibit the effect of forskolin (thus suggests that caffeine should boost the effect of forskolin)
  • Taken together, these three results practically mean that as an active ingredient in anti-cellulite creams, forskolin can boost both cAMP and fat release from fat cells, especially if combined with exercise (adrenergic response), dieting (insulin inhibition) and caffeine (PDE inhibition) and if used in high concentrations.
  • Source: Forskolin as an activator of cyclic AMP accumulation and lipolysis in rat adipocytes
  • Abstract: Forskolin increased cyclic AMP accumulation in isolated adipocytes and markedly potentiated the elevation of cyclic AMP due to isoproterenol. In adipocyte membranes, forskolin stimulated adenylate cyclase activity at concentrations of 0.1 microM or greater. Forskolin did not affect the EC50 for activation of adenylate cyclase but did increase the maximal effect of isoproterenol. Neither the soluble nor particulate low-Km cyclic AMP phosphodiesterase activity was affected by forskolin. Low concentrations of forskolin (0.1-1.0 microM), which significantly elevated cyclic AMP levels, did not increase lipolysis, whereas similar increases in cyclic AMP levels due to isoproterenol elevated lipolysis. Forskolin did not inhibit the activation of triacylglycerol lipase by cyclic AMP-dependent protein kinase or the subsequent hydrolysis of triacylglycerol. Higher concentrations of forskolin (10-100 microM) did increase lipolysis. Both the increased cyclic AMP production and lipolysis due to forskolin were inhibited by the antilipolytic agents insulin and N6-(phenylisopropyl)adenosine. Hypothyroidism reduced the ability of forskolin to stimulate cyclic AMP production and lipolysis. These results indicate that forskolin increases cyclic AMP production in adipocytes through an activation of adenylate cyclase. Lipolysis is activated by forskolin but at higher concentrations of total cyclic AMP than for catecholamines.

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