1. What is it and where does it come from?

A plant used since antiquity in Hindu and Ayurvedic traditional medicine is the source of an amazing compound of unique biological importance. The plant, Coleus forskohlii, is where the compound forskolin comes from.

Forskolin has started showing up in many of the most advanced thermogenics and fat burners on the market due to it natural fat-loss-enhancing properties. Forskolin has also shown positive effects on the heart, lungs, and blood pressure.

Forskolin has been shown to increase thyroid hormone production as well as stimulate thyroid hormone release. As we know, the thyroid is responsible for metabolic rate via the hormones it releases. Therefore, increasing production of the thyroid results in an increase in metabolism. But, that's not all forskolin is good for!

Over the centuries, Coleus has been used for a wide range of conditions. It turns out that the active ingredient in this herb, Forskolin, is capable of beneficial action against a wide range of conditions. This is because it affects one of the most basic and important cell regulating compounds in the body: cyclic adenosine monophosphate (cAMP.)

Cyclic AMP is perhaps the most important cell-regulating compound. Once formed it activates many other enzymes involved in diverse cellular functions. Under normal situations cAMP is formed when a stimulatory hormone (e.g., epinephrine) binds to a receptor site on the cell membrane and stimulates the activation of adenylate cyclase. This enzyme is incorporated into all cellular membranes and only the specificity of the receptor determines which hormone will activate it in a particular cell. In the case of forskolin, it can aide in a number of biological processes, explained in further detail below.

Forskolin appears to bypass this need for direct hormonal activation of adenylate cyclase via transmembrane activation. As a result of this activation of adenylate cyclase intracellular cAMP levels rise. The physiological and biochemical effects of a raised intracellular cAMP level include: inhibition of platelet activation and degranulation; inhibition of mast cell degranulation and histamine release; increased force of contraction of heart muscle; relaxation of the arteries and other smooth muscles; increased insulin secretion; increased thyroid function; and increased lipolysis (fat destruction). Recent studies have found forskolin to possess additional mechanisms of action independent of its ability to directly stimulate adenylate cyclase and cAMP dependent physiological responses. Specifically forskolin has been shown to inhibit a number of membrane transport proteins and channel proteins through a mechanism that does not involve the production of cAMP. The result is again a transmembrane signaling that results in activation of other cellular enzymes.

By raising cAMP, forskolin is responsible for:

• Inhibition of mast cell degranulation and histamine release.
• Increased force of contraction of heart muscle.
• Relaxation of the arteries and other smooth muscle.
• Increased insulin secretion.
• Increased thyroid function.
• Increased lipolysis (breakdown of fat)

The therapeutic ramifications of c. forskohlii based on the pharmacology of forskolin are immense. Forskolin works well as a fat-loss-aide stacked with ephedra because it counteracts the age-related decrease in response of fat cells to thermogenic (heat producing and calorie burning) agents like ephedrine.

The ancient medicinal plant Coleus forskohlii is the source of the compound forskolin which possesses unique biological activity. While clinical results are thought to be better obtained using the whole plant versus the isolated constituent forskolin, research on forskolin is upholding the traditional uses of the plant. Due to the unique pharmacology of forskolin, C. forskohlii may prove to be useful in a wide range of clinical conditions.

The forskolin content of Coleus root is typically 0.2% to 0.3%, therefore the forskolin content of crude Coleus products may not be sufficient to produce a pharmacological effect. It is best to use standardized extracts which have concentrated the forskolin content. The recommended dosage should be based upon the level of forskolin. Future studies will undoubtedly produce more precise dosage recommendations of a Coleus forskohlii. The current recommendation for Coleus forskohlii extract, standardized to contain 185 forskolin, is 50 mg (9 mg of forskolin) two to three times daily. The animal studies on forskolin indicate an extremely low order of toxicity for forskolin. Based on the pharmacology of forskolin, it may be wise to restrict the use of C. forskohlii preparations in cases of low blood pressure and peptic ulcers. Furthermore, C. forskohlii preparations should be used with caution in patients on presription medications especially anti-asthmatics and anti-hypertensives due to its ability to possibly potentiate the drug's effect.