Scientific Name: Coleus forskohlii
- Diterpenoids (labdane type: forskolin/coleanol & deoxyforskolin)
- Triterpenoids: lupeol, coleolic acid, oleanolic acid
- Phytosterols (beta-sitosterol)
- Volatile oils
- Thermogenic agent (lipolysis stimulator & thyroid hormone release stimulator)
Mechanism of Action & Pharmacology:
- Forskolin is responsible for virtually all pharmacological activities. Its primary mode of action is to increase cyclic adenosine monophosphate (cAMP) and cAMP-mediated functions, via activation of the enzyme adenylate cyclase.
- The physiological and biochemical effects of raised intracellular cAMP are many and include inhibition of platelet activation, increased force of contraction of heart muscle, relaxation of smooth muscle, increased insulin secretion, increased ACTH release by the pituitary, increased thyroid function and increased lipolysis in adipocytes.
- Forskolin increases the rate of lipolysis via cyclic adenosine monophosphate (cAMP) accumulation by mechanisms independent of hormonal stimulation both in vitro and in animal models. Forskolin also directly activates hormone sensitive lipase by phosphorylation of protein kinase A, resulting in further lipolysis and release of free fatty acids.
- Forskolin antagonizes the action of platelet-activating factor (PAF) by interfering with PAF binding to receptor sites, playing a central role in many inflammatory and allergic processes including neutrophil activation, increasing vascular permeability, smooth muscles contraction including bronchoconstriction, and reduction in coronary blood flow.
- Forskolin also appears to have an effect on several membrane transport proteins, and inhibits glucose transport in erythrocytes, adipocytes, platelets, and other cells.
Safety & Toxicity Concerns:
- May cause gastrointestinal upset.
- Use caution with active peptic ulcer, hypotension, bleeding disorders.
- Avoid in pregnancy & lactation due to unknown effects.
- Theoretical potentiating effects with anticoagulant and antihypertensive agents.
- May potentiate effects of a variety of medications due to theoretical concern based on ability of forskolin to activate increased intracellular cyclic AMP in vitro.