Coleus Forskohlii and Forskolin Mechanism of action.

Coleus Forskohlii Research.

Coleus Forskohlii Extract CAS 66575-29-9 66428-89-5 photo picture image Effects of Coleus forskohlii on Fat Storage in Ovariectomized Rats.

The antiobesity effects of Coleus forskohlii were investigated in ovariectomized (ovx) rats. Eight-week-old female Wistar rats were assigned to four groups: a sham-operated group fed the control diet (MF, sham-m) ; an ovx-m group fed the control diet; a sham-operated group fed the control diet containing 50 g/kg of Coleus forskohlii extract (sham-c) ; and an ovx-c group fed the control diet containing 50 g/kg of Coleus forskohlii extract. The body weight, adipose tissues, and cell diameter were investigated in ovx rats after Coleus forskohlii extract treatment. Administration of Coleus forskohlii extracts reduced body weight, food intake, and fat accumulation in ovx rats. Our results suggest that Coleus forskohlii may be useful in the treatment of obesity.

Induction of Drug Metabolism by Forskolin, the Role of The Pregnane X Receptor and the PKA Signal Transduction Pathway.

An extract of the plant Coleus forskohlii has been used for centuries in Ayurvedic medicine to treat various diseases such as hypothyroidism, heart disease and respiratory disorders. Additionally, complex herbal mixtures containing this extract are gaining popularity in United States for their putative 'fat-burning' properties. The active ingredient in Coleus forskohlii extract is the diterpene compound forskolin. Forskolin is a widely used biochemical tool that activates adenyl cyclase, thereby increasing intracellular concentration of cAMP, and thus activating the PKA signal transduction pathway. We show here that both forskolin induces CYP3A gene expression in primary hepatocytes by functioning as agonists of the pregnane X receptor. Our data provide important insights into the molecular mechanism of both the PKA-dependent and the PKA-independent effects of forskolin on the expression of drug-metabolizing enzymes in liver. Finally, our data suggest that herbal therapy with Coleus forskohlii extract should be approached cautiously due to the potential for herb-drug interactions in patients on combination therapy.

Quantitative analysis of forskolin in Coleus forskohlii (Lamiaceae) by reversed-phase liquid chromatography.

A rapid method was developed for the evaluation of forskolin in Coleus forskohlii Briq. (Lamiaceae). Forskolin was quantitated in the root and stem of dried C. forskohlii and in 17 market products by reversed-phase liquid chromatography (LC) with a photodiode array detector at 210 nm. The temperature was held constant at 30 degrees C, and the retention time of forskolin was approximately 6.8 min. The samples were extracted with acetonitrile by sonication. The precision of the method was confirmed by a standard deviation less than 5.0% (n = 3), and forskolin recovery was 99.1%. Limit of detection was 1.5 microg/mL, and the response was linear through zero from 6.3 to 630 microg/mL with a correlation coefficient (R2) of 0.9998. Identity of the marker compound was confirmed by an LC/mass spectrometry experiment. The method was successful in the qualitative and quantitative evaluation of the marker compound in C. forskohlii plant material and in market products claiming to contain C. forskohlii.

Relaxant effects of forskolin on guinea pig tracheal smooth muscle:

Some Research investigated the relaxant effects of forskolin, a diterpene derivative isolated from the roots of Coleus forskohlii, on guinea pig airway smooth muscle. Forskolin caused dose-dependent relaxant effects on resting tone and on leukotriene C4, leukotriene D4, and carbachol-induced contraction of tracheal smooth muscle. Moreover, with propranolol pretreatment the relaxant effect of forskolin on tracheal smooth muscle did not change, whereas with the same pretreatment the relaxant effect of isoproterenol diminished. These results suggest that forskolin relaxes airway smooth muscle in guinea pigs in vitro and in vivo by raising tissue cyclic AMP levels and that its actions are independent of beta-adrenoceptors. coleus Forskohlii.

Pharmacological studies on coleonol, a hypotensive diterpene from Coleus forskohlii:

Coleus species have been used in Ayurvedic medicine for heart diseases, spasmodic pain, painful micturition and convulsions. The pharmacological properties of coleonol, a diterpene, isolated from Coleus forskohlii were investigated. Its predominant effect is to lower the blood pressure of anaesthetised cat and rat as well as of the spontaneously hypertensive rat due to relaxation of the vascular smooth muscle. In small doses it has a positive inotropic effect on isolated rabbit heart as well as on cat heart in vivo. Coleonol also exhibits nonspecific spasmolytic activity on smooth muscle of the gastrointestinal tract in various species but not on bronchial musculature of guinea pig. Large doses of coleonol have a depressant action on the central nervous system. These results provide the rationale for the use of this plant in Aurvedic medicine.

Additional potential properties of Coleus Forskohlii

Some marketers are promoting the extract forskolin from coleus forskohlii as a way to maintain lean body mass. They call this extract Forslean. coleus forskohlii