Description
Forskolin is a labdane diterpene found in Coleus that exhibits vasodilatory, immunomodulatory, antihypertensive, anti-inflammatory, and anticancer chemotherapeutic activities. Forskolin activates adenylyl cyclase, increasing levels of cAMP and activating PKA. Forskolin decreases intraocular pressure in animal models of glaucoma. Additionally, forskolin inhibits IL-2-induced phosphorylation of STAT5 and activation of JAK3, decreasing T cell proliferation in vivo. This compound also decreases levels of Gli1 mRNA and inhibits Smo activity, suppressing sonic hedgehog (Shh) signaling; this inhibits basal cell carcinoma tumor growth in animal models. Forskolin also activates protein phosphatase 2A (PP2A) and enhances proteasome activity. In airway smooth muscle cells, forskolin inhibits IL-1β-induced expression of IL-8.
References
Rodriguez G, Ross JA, Nagy ZS, et al. Forskolin-inducible cAMP pathway negatively regulates T-cell proliferation by uncoupling the interleukin-2 receptor complex. J Biol Chem. 2013 Mar 8;288(10):7137-46. PMID: 23341462.
Makinodan E, Marneros AG. Protein kinase A activation inhibits oncogenic Sonic hedgehog signalling and suppresses basal cell carcinoma of the skin. Exp Dermatol. 2012 Nov;21(11):847-52. PMID: 23163650.
Alasbahi RH, Melzig MF. Forskolin and derivatives as tools for studying the role of cAMP. Pharmazie. 2012 Jan;67(1):5-13. PMID: 22393824.
Cristóbal I, Garcia-Orti L, Cirauqui C, et al. PP2A impaired activity is a common event in acute myeloid leukemia and its activation by forskolin has a potent anti-leukemic effect. Leukemia. 2011 Apr;25(4):606-14. PMID: 21233840.
Asai M, Tsukamoto O, Minamino T, et al. PKA rapidly enhances proteasome assembly and activity in in vivo canine hearts. J Mol Cell Cardiol. 2009 Apr;46(4):452-62. PMID: 19059265.
Kaur M, Holden NS, Wilson SM, et al. Effect of beta2-adrenoceptor agonists and other cAMP-elevating agents on inflammatory gene expression in human ASM cells: a role for protein kinase A. Am J Physiol Lung Cell Mol Physiol. 2008 Sep;295(3):L505-14. PMID: 18586957.
Zeng S, Shen B, Wen L, et al. Experimental studies of the effect of Forskolin on the lowering of intraocular pressure. Yan Ke Xue Bao. 1995 Sep;11(3):173-6. PMID: 8758848.
