Forskolin
From Coleus forskohlii , a cardiovascular tonic
Uses
Allergies
Asthma
Cancer treatment
Congestive heart failure
Glaucoma
Hypertension
Weight loss
Clinical Summary
Forskolin is a diterpene derived from the root of Coleus forskohlii. It is used for a variety of conditions, including cancer, obesity, glaucoma, asthma, and heart failure. Forskolin was shown in animal studies to promote the activation of adenylate cyclase and increase intracellular concentrations of cyclic adenosine monophosphate (cAMP) . Small clinical studies suggest that forskolin can benefit obese men in weight management . Forskolin eye drops may reduce intra-ocular pressure and oral forskolin capsules help reduce asthma attacks . When administered intravenously or inhaled, forskolin has bronchodilation effect . Forskolin also benefits cardiovascular health due to its inotropic , anti-inflammatory and antiplatelet properties . One study found intra-arterial forskolin daropate to be an effective treatment for cerebral vasospasm in patients with aneurysmal subarachnoid hemorrhage . Treatment of uropathogenic E.coli-infected mice with forskolin resulted in reduced number of bacteria via cyclic AMP-regulated exocytosis.
The anticancer effects of forskolin and its derivatives have also been studied in vitro and in animal models . When applied on the skin of mice, forskolin can stimulate the production of melanin in the absence of ultraviolet light . It has been proposed for use in sunless tanning lotions to reduce the risk of skin cancer by decreasing exposure to sun. In an in vitro study, an extract of forskolin was found to significantly reduce viral production in human lymphoid CEM-GFP cells infected with human immunodeficiency virus (HIV- 1NL4) . These effects have yet to be confirmed in human studies.
Cases of acute poisoning after the consumption of Coleus forskohlii products, possibly from contaminants, have been reported in Europe.
Mechanism of Action
Forskolin activates adenylate cyclase through direct stimulation of enzyme and by modulating enzyme activities. These lead to increase in intracellular concentrations of cyclic adenosine monophosphate (cAMP) . This may explain the bronchodilation , inotropic , vasodilatory and antiplatelet effects of Forskolin. Forskolin has also been reported to increase cellular acetylcholinesterase and protect neuronal cells from organophosphate toxicity . It is thought to reduce body fat and has been studied as a weight loss agent.
In vitro and animals studies have shown forskolin and its derivative can inhibit cell proliferation, and induce cell cycle arrest and apoptosis in human gastric cancer cells . Forskolin was also found to inhibit melanoma cell-induced platelet aggregation and reduce lung metastasis . Forskolin upregulates the expression of cytochrome P450 3A (CYP3A) family through the pregnane-Xreceptor that regulates the CYP3A genes.
Study:
The present study was designed to investigate the potential of Coleus forskohlii plant extract- ‘forskolin’ in experimental dementia in Wistar rats. Dementia was induced by the administration of High Fat Diet (HFD) for 90 days. The effects on learning and memory were assessed using Morris Water Maze (MWM) test. A battery of biochemical tests such as brain Thiobarbituric Acid Reactive Species (TBARS), reduced Glutathione (GSH), Superoxide Dismutase (SOD), brain Acetylcholinesterase (AChE) activity, Myeloperoxidase (MPO) activity and total serum cholesterol levels were measured. Administration of high fat diet significantly impaired the learning and memory and also deleteriously affected the biochemical parameters. Administration of forskolin (20 mg/kg, p.o.) for 14 days significantly attenuated high fat diet induced memory deficits and the biochemical alterations. Combined administration of forskolin and Pregnane X Receptor (PXR) antagonist, ketoconazole (25 mg/kg, p.o.) significantly reduced the beneficial effects of forskolin in HFD treated rats. This study demonstrates that improvement of memory by forskolin administration may occur as an outcome of its antioxidative, anticholinergic, anti-inflammatory, hypolipidemic and amyloid lowering potential. The study also proposes the possible involvement of pregnane X receptors in the pathophysiology of experimental dementia.
No other species of Coleus contains forskolin and not even all varieties of C. forskohlii....
In 1981 it was first demonstrated that forskolin possessed a special property: it could activate in a unique way the enzyme involved in the production of cyclic AMP (cAMP, adenylate cyclase).