Forskolin stimulates fat release from fat cells (but is inhibited by alpha-2 adrenoreceptor activation)

  • Forskolin is the strongest natural lipolytic chemical known today
  • In this paper forskolin was shown to increase glycerol release from adipocytes by 600% than without, proving the lipolytic effects of forskolin
  • Adenylate cyclase, a kew enzyme in the lipolytic process was increased by 100x times (10,000%), showing that forskolin needs to release a lot of adenylate cyclase in order to produce lipolysis, in comparison to adrenaline.
  • The lipolytic effect of forskolin has been enhanced by adrenaline, which is normally produced when we exercise. This practically means that combining forskolin application in combination with exercise (as in applying a forskolin-rich anti-cellulite cream before and after exercise when adrenaline levels are high) will offer maximum results.
  • On the other hand, alpha-2 adrenoreceptor activation reduced the lipolytic response of forskolin. This practically means that we need to combine forskolin with an alpha-2 antagonist (such as golden chamomile extract or yohimbine), for maximum results.
  • Forskolin is ideal as an anti-cellulite / topical fat loss active in cellulite / contouring creams, especially if combined with golden chamomile, caffeine and other synergistic actives.
  • Source: Alpha-2 adrenergic activation inhibits forskolin-stimulated adenylate cyclase activity and lipolysis in human adipocytes,
  • Abstract: Forskolin at 10 muM caused a 100-fold increase in the intracellular concentration of cyclic AMP and a 6-fold increase in glycerol release in the human adipocyte. These responses are comparable to those prompted by 10 muM isoproterenol. The effects of forskolin on cyclic AMP and lipolysis were dose-dependent. Alpha-2 adrenergic activation, achieved with 10 muM epinephrine and 30 muM propranolol, significantly inhibited forskolin-stimulated cyclic AMP accumulation and glycerol release, shifting the dose-response curves to the right. Forskolin at 10 muM caused a 4.5-fold increase in the adenylate cyclase activity of human adipocyte membranes. When either isoproterenol or epinephrine (0.1 mM) was combined with forskolin, the magnitude of response was substantially greater than the sum of responses achieved by each agent incubated alone.

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