Coleus forskolii
Common name: Coleus
Family: Lamiaceae
Part used: Root
Constituents: Diterpenoids (labdane; forskolin/coleanol)
Actions: Hypotensive, bronchodilator, inflammation modulating, positive inotropic, lipolysis stimulator, thyroid hormone release stimulator, mood elevator, platelet aggregation inhibitor
Pharmacology:
- Hypotensive and spasmolytic component appears to be coleanol/forskolin.
- An adenylate cyclase enzyme activator (stimulates the formation of ATP) which increases cyclic adenosine monophosphate (cAMP) in cells. Appears to bypass the need for direct hormonal activation of adenylate cyclase via transmembrane activation. 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 muscle, increased insulin secretion, increased thyroid function, and increased lipolysis.
- 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.
- 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.
Medical uses: Hypertension, allergies, asthma, dilated cardiomyopathy, glaucoma, hypothyroidism, obesity. Appears to be well indicated in conditions such as eczema (atopic dermatitis), asthma, psoriasis, angina, and hypertension.
Pharmacy:
- Capsules: 100-250 mg BID (standardized to 10 %forskolin)
Contraindications: Caution with active peptic ulcer
Toxicity: Overall very safe; GI stimulating, possibly vasodilating
Interactions: Theoretical concern it may potentiate warfarin and digoxin.