Forskolin

• Colforsin ( INN)
• Coleonol
• (3R,4aR,5S,6S,6aS,10S,10aR,10bS)-dodecahydro-5,6,10,10b-tetrahydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-3-vinyl-1H-naphtho[2,1-b]pyran-5-yl acetate ( IUPAC)

Colorless to yellow solid

Fixed

230-232 ° C

Insoluble in ethanol, chloroform, and DMSO

Attention

Template: Infobox chemical / molecular formula search available

Forskolin (also Colforsin ( INN), Coleonol ) is a shrub occurring in the harp Plectranthus barbatus chemical compound belonging to the group of diterpenes. In the human and animal organism forskolin has a direct stimulator of the enzyme adenylyl cyclase various effects. Therefore, it is experimentally used in biochemistry and pharmacology.

Occurrence

Diterpenes are widely used in the genre of harp shrubs. Forskolin, however, has so far only in a significant amount of Plectranthus barbatus ( Coleus forskohlii ) are isolated.

Pharmacology

Forskolin is a non-selective stimulator of isoenzymes of group of adenylyl cyclases. It activates with the exception of adenylyl cyclase IX all isoenzymes in low micromolar concentration. Forskolin binds it using hydrophobic interactions within a binding pocket between the C1 and the C2 domain of adenylyl cyclase.

As a result, the enzyme activation, the conversion of adenosine triphosphate ( ATP) to the signal substance cyclic adenosine monophosphate ( cAMP) is catalyzed in the cell. In this way, forskolin engages centrally in the signal transduction of many G protein- coupled receptors. Therefore, an increase in the cAMP level within the cell by forskolin has numerous biological reactions. On the heart it has a positive inotropic effect. In the blood vessels forskolin acts as a vasodilator as a vasodilator. In addition, it acts under experimental conditions coagulant inflammatory, lipolytic and spasmolytic.

Use

The forskolin -containing Plectranthus barbatus plant has an ethnopharmacological importance in Ayurvedic medicine as well as in the folk medicines of Brazil, Africa and China. You will find here, including the treatment of gastrointestinal disorders, respiratory disorders as well as heart and nerve diseases an application. At least a portion of its effects is attributed to the ingredient forskolin.

Forskolin is primarily used experimentally as a model substance for increasing cellular cAMP levels in biochemical and medical research. Due to its diverse effects that a possible use in the treatment of heart disease, asthma, thrombosis and of overweight was discussed. In the world of bodybuilding forskolinhaltige plant extracts are used as a fat burner. The effectiveness of forskolin for these claimed areas of application is not sufficiently proven. His risk-benefit ratio is not sufficiently studied.

A good water-soluble derivative of Colforsins is the Colforsindaropathydrochlorid.