Forskolin (Colforsin)

Forskolin increases cAMP levels in preparations of membranes, cells, or tissues. Forskolin not only activates AC but also interacts with certain other proteins, including glucose transporters and ion channels. Forskolin is able to promote activation of nine different transmembrane iso-forms of AC, albeit with somewhat less efficacy for AC9, which could be used to provides a means to identify and quantify high-affinity binding sites, i.e., G-proteins (G_s)–AC complexes. Activation of _s by GPCRs contributes to Forskolin-stimulated cAMP generation in cells because of _s-Forskolin potentiation of AC activity. ^[1] Forskolin stimulates adenylate cyclase activity without interacting with cell surface receptors. Forskolin's potentiation of cAMP in turn inhibits basophil and mast cell degranulation and histamine release, lowers blood pressure and intraocular pressure, inhibits platelet aggregation, promotes vasodilation, bronchodilation, and thyroid hormone secretion, and stimulates lipolysis in fat cells. Forskolin inhibits the binding of platelet-activating factor (PAF), independently of cAMP formation, which may be a result of Forskolin's direct effect on PAF or via interference with PAF binding to receptor sites. Forskolin also appears to have an effect on several membrane transport proteins, and inhibits glucose transport in erythrocytes, adipocytes, platelets, and other cells. Forskolin is used to treat with glaucoma. ^[2]

Colforsin (Forskolin, HL 362, Coleonol) is a ubiquitous activator of eukaryotic adenylyl cyclase (AC) in a wide variety of cell types, commonly used to raise levels of cAMP. It also activates PXR and FXR activity and stimulates autophagy.^[4]

• Cell lines

  hMPCs or cynMPCs

• Concentrations

  20 μM

• Incubation Time

  2 h

• Method

  Cells were treated with 20 μM forskolin (S2449, Selleck) for 2 h for synchronization.

• Animal Models

  Male Sprague-Dawley rats

• Dosages

  10 mg/kg

• Administration

  i.p.