Forskolin, alone or in combination with a PDE4 inhibitor, stimulates lipolysis and reduces fat

  • Forskolin is a well-known natural chemical from the Coleus Forkohlii plant,  used in hundreds of studies because of it's lipolytic (fat reducing) properties. Forskolin stimulates the release of cAMP which is the most important step towards lipolysis.
  • In this study forskolin was used on it's own and also in combination with rolipram, a PDE4 inhibitor.  PDE4 is an enzyme that inhibits the lipolytic process, by blocking the release of cAMP. As forskolin stimulates cAMP release / lipolysis, it makes sense to combine it with a PDE4 (phosphodiesterase-4) inhibitor, to ensure that cAMP release / lipolysis is maximised.
  • In regard to PDE4 inhibition, rolipram is similar to caffeine, a natural, widely consumed PDE4 inhibitor, which does not have the side-effects of drugs such as rolipram.
  • At the end of the study it was shown that forskolin and rolipram on their own were effective in reducing fat levels. As expected, the synergistic combination of forskolin and rolipram yielded better results than the two chemicals alone.
  • This study shows that when cAMP stimulation is combined with PDE4 inhibition, lipolysis is maximised. 
  • Although rolipram is only used experimentaly (due to it's narrow therapeutic window), caffeine, it's PDE4 inhibiting analog, is used widely and makes an excellent partner with forskolin for maximum cAMP release, lipolysis and fat reduction.
  • Due to it's lipolytic action, forskolin is an ideal anti-cellulite cream active ingredient, especially if combined with caffeine, raspberry ketone or other cAMP-boosting / lipolytic actives.
  • Source: The effects of forskolin and rolipram on cAMP, cGMP and free fatty acid levels in diet induced obesity
  • Abstract: Obesity is a major health problem. We investigated the effects of forskolin and rolipram in the diet of animals in which obesity had been induced. We used 50 female albino Wistar rats that were assigned randomly into five groups as follows: group 1, control; group 2, high fat diet; group 3, high fat diet + forskolin; group 4, high fat diet + rolipram; and group 5, high fat diet + rolipram + forskolin. The rats were fed for 10 weeks and rolipram and forskolin were administered during last two weeks. The animals were sacrificed and blood samples were obtained. Serum cAMP, cGMP and free fatty acids (FFA) levels were measured using ELISA assays. We also measured weight gain during the 10 week period. cAMP and FFA levels of groups 3, 4 and 5 were significantly higher than those of groups 1 and 2. We found no significant differences in serum cGMP levels among the groups. The weight gain in groups 3, 4 and 5 was significantly less than for group 2. We also found that the weight gain in group 5 was significantly less than in groups 3 and 4. We found that both forskolin and rolipram stimulated lipolysis and inhibited body weight increase by increasing cAMP levels. Also, combination therapy using the two agents may be more effective in preventing diet induced obesity than either agent alone. We found also that these agents did not effect cellular cGMP levels in diet induced obesity.

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