Forskolin

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Forskolin

Common Names

  • Makandi
  • Colforsin

For Patients & Caregivers

How It Works

Forskolin is used in Ayurvedic medicine for various conditions, but clinical studies that demonstrate its safety and effectiveness are lacking.

Forskolin is a root extract of the Indian plant Coleus forskohlii. It has been used for centuries in Ayurvedic medicine to treat various diseases such as underactive thyroid, heart disease, and respiratory disorders. Although anti-inflammatory and blood-pressure lowering effects have been shown in the laboratory setting, very few clinical trials have been conducted. In addition, only a few studies actually use forskolin as an oral supplement. More studies are needed to determine safety and effectiveness for various conditions in humans.

Purported Uses
  • To treat asthma
    Forskolin may cause cellular changes that stimulate the dilation of airways.
  • To treat heart disease
    Two clinical trials found positive effects with intravenous forskolin, but overall support for this use is not strong. In addition, oral forms of this herb have not been tested in humans.
  • To treat glaucoma
    Studies in humans have conflicting results.
  • To lower high blood pressure
    Forskolin is known to cause cellular changes that lead to blood vessel dilation, which should lower blood pressure, but there is no proof from clinical trials that this effect occurs in humans.
  • For weight loss
    A small clinical study suggests forskolin may have benefits in obese men.
Patient Warnings
  • Forskolin formulations that are not designed for use in the eye, such as topical creams or extracts meant to be taken by mouth, should not be placed directly in the eye.
  • Forskolin preparations should not be used by patients with polycystic kidney disease.
Do Not Take If
  • You are taking medication for high blood pressure such as beta-blockers, vasodilators, ACE inhibitors, or calcium channel blockers: Laboratory studies show that forskolin may also lower blood pressure. Therefore it may have added effects, although clinical relevance has yet to be determined.
  • You are taking warfarin or other blood thinners: Laboratory studies show that forskolin may have similar effects. Therefore, it may have added effects with these medications, increasing the risk of bleeding or bruising. However, clinical relevance has yet to be determined.
Side Effects
  • Low blood pressure
  • Slow heart rate
  • Diarrhea, gastrointestinal syptoms
Special Point
  • Although forskolin is used to reduce intraocular pressure in glaucoma, no sterile eye drop formulation is available.
  • The intravenous form of forskolin is not available in the United States.
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For Healthcare Professionals

Scientific Name
Coleus forskohlii
Clinical Summary

Forskolin is a diterpene derived from the root of Coleus forskohlii. It has been used for centuries in Ayurvedic medicine to treat a variety of conditions including heart disease, respiratory disorders, and hypothyroidism. However, studies are quite limited and only a few actually use forskolin as an oral supplement.

Laboratory studies suggest it has inotropic (7) and antiplatelet properties (9). In animal studies, forskolin promoted activation of adenylate cyclase and increased intracellular concentrations of cyclic adenosine monophosphate (1). Treatment of uropathogenic E.coli-infected mice with forskolin reduced bacteria (11).

In humans, small clinical studies suggest that forskolin may help weight management (2) or reduce asthma attacks (4). When administered intravenously or inhaled, forskolin had a bronchodilation effect (5) (6). Other small studies suggest that intraoperative infusion of forskolin may benefit cardiovascular health due to anti-inflammatory effects (8) or that intraarterial forskolin daropate may improve cerebral vasospasm in patients with aneurysmal subarachnoid hemorrhage (10).

In vitro and animal studies suggest some anticancer effects with forskolin and its derivatives (1) (23) (12). When applied on the skin of mice, forskolin stimulated production of melanin in the absence of ultraviolet light (12). It has been proposed for use in sunless tanning lotions to reduce skin cancer risk by decreasing sun exposure. In an in vitro study, a forskolin extract reduced viral production in human lymphoid CEM-GFP cells infected with human immunodeficiency virus (HIV-1NL4) (14). However, these effects have yet to be confirmed in humans.

Purported Uses
  • Asthma
  • Heart disease
  • Glaucoma
  • Hypertension
  • Weight loss
Mechanism of Action

Forskolin activates adenylate cyclase through direct stimulation and modulation of enzyme activities, leading to increased intracellular concentrations of cyclic adenosine monophosphate (cAMP) (1). This may explain bronchodilation (4) (5) (6), inotropic (7), vasodilatory (16), and antiplatelet (11) effects. Forskolin also increased cellular acetylcholinesterase and protected neuronal cells from organophosphate toxicity (17).

In vitro and animals studies suggest forskolin and derivatives may inhibit cell proliferation, and induce cell cycle arrest and apoptosis in human gastric cancer cells (18) (19). Forskolin upregulated expression of cytochrome P450 3A family via the pregnane-X-receptor that regulates CYP3A genes (20) (21).

Warnings

Forskolin may contribute to cyst enlargement in patients with polycystic kidney disease. It is therefore recommended that these patients avoid preparations containing this compound (22).

Adverse Reactions

Reported: Hypotension, tachycardia (1), headache (10), gastrointestinal symptoms, diarrhea (15)

Herb-Drug Interactions

Anti-hypertensives: Laboratory experiments of forskolin also suggest hypotensive effects (7). However clinical relevance has yet to be determined.
Anticoagulants: Laboratory experiments demonstrate that forskolin also inhibits platelet aggregation (9). Forskolin can also induce CYP3A gene expression and potentially increase the metabolism of drugs that are substrates of related microsomal enzymes (20) (21). Clinical relevance has yet to be determined.

References
  1. Seamon KB, Padgett W, Daly JW. Forskolin: unique diterpene activator of adenylate cyclase in membranes and in intact cells. Proc Natl Acad Sci U S A, 1981. 78(6):3363-7.
  2. Godard MP, Johnson BA, Richmond SR. Body composition and hormonal adaptations associated with forskolin consumption in overweight and obese men. Obes Res, 2005. 13(8):1335-43.
  3. Meyer BH, et al. The effects of forskolin eye drops on intra-ocular pressure. S Afr Med J, 1987. 71(9):570-1.
  4. Gonzalez-Sanchez R, et al. Forskolin versus sodium cromoglycate for prevention of asthma attacks: a single-blinded clinical trial. J Int Med Res, 2006. 34(2):200-7.
  5. Wajima Z, et al. Intravenous colforsin daropate, a water-soluble forskolin derivative, prevents thiamylal-fentanyl-induced bronchoconstriction in humans. Crit Care Med, 2002. 30(4):820-6.
  6. Bauer K, et al. Pharmacodynamic effects of inhaled dry powder formulations of fenoterol and colforsin in asthma. Clin Pharmacol Ther, 1993. 53(1):76-83.
  7. Metzger H, Lindner E. The positive inotropic-acting forskolin, a potent adenylate cyclase activator. Arzneimittelforschung, 1981. 31(8):1248-50.
  8. Hayashida N, et al. Antiinflammatory effects of colforsin daropate hydrochloride, a novel water-soluble forskolin derivative. Ann Thorac Surg, 2001. 71(6):1931-8.
  9. Christenson JT, Thulesius O, Nazzal MM. The effect of forskolin on blood flow, platelet metabolism, aggregation and ATP release. Vasa, 1995. 24(1):56-61.
  10. Suzuki S, Ito O, Sayama T, Goto K. Intra-arterial colforsin daropate for the treatment of cerebral vasospasm after aneurysmal subarachnoid hemorrhage. Neuroradiology. 2010 Sep;52(9):837-45.
  11. Bishop BL, Duncan MJ, Song J, et al. Cyclic AMP-regulated exocytosis of Escherichia coli from infected bladder epithelial cells. Nat Med. 2007;13(5):625-30.
  12. Agarwal KC, Parks RE, Jr. Forskolin: a potential antimetastatic agent. Int J Cancer, 1983. 32(6):801-4.
  13. D’Orazio JA, et al. Topical drug rescue strategy and skin protection based on the role of Mc1r in UV-induced tanning. Nature, 2006. 443(7109):340-4.
  14. Sabde S, Bodiwala HS, Karmase A, et al. Anti-HIV activity of Indian medicinal plants. J Nat Med. 2011;65(3-4):662-9.
  15. Nishijima C, Chiba T, Sato Y, et al. Nationwide Online Survey Enables the Reevaluation of the Safety of Coleus forskohlii Extract Intake Based on the Adverse Event Frequencies. Nutrients. Apr 17 2019;11(4).
  16. Baumann G, et al. Cardiovascular effects of forskolin (HL 362) in patients with idiopathic congestive cardiomyopathy—a comparative study with dobutamine and sodium nitroprusside. J Cardiovasc Pharmacol, 1990. 16(1):93-100.
  17. Curtin BF, et al. Forskolin, an inducer of cAMP, up-regulates acetylcholinesterase expression and protects against organophosphate exposure in neuro 2A cells. Mol Cell Biochem. 2006;290(1-2):23-32.
  18. Li Z, Wang J. A forskolin derivative, FSK88, induces apoptosis in human gastric cancer BGC823 cells through caspase activation involving regulation of Bcl-2 family gene expression, dissipation of mitochondrial membrane potential and cytochrome c release. Cell Biol Int, 2006.
  19. Sun B, Geng S, Huang X, et al. Coleusin factor exerts cytotoxic activity by inducing G0/G1 cell cycle arrest and apoptosis in human gastric cancer BGC-823 cells. Cancer Lett. 2011 Feb 1;301(1):95-105.
  20. Dowless MS, et al. Cyclic AMP-independent activation of CYP3A4 gene expression by forskolin. Eur J Pharmacol, 2005. 512(1):9-13.
  21. Ding X, Staudinger JL. Induction of drug metabolism by forskolin: the role of the pregnane X receptor and the protein kinase a signal transduction pathway. J Pharmacol Exp Ther, 2005. 312(2):849-56.
  22. Putnam WC, Swenson SM, Reif GA, et al. Identification of a forskolin-like molecule in human renal cysts. J Am Soc Nephrol. 2007 Mar;18(3):934-43.
  23. Follin-Arbelet V, Misund K, Hallan Naderi E, et al. The natural compound forskolin synergizes with dexamethasone to induce cell death in myeloma cells via BIM. Sci Rep. 2015 Aug 26;5:13001.
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