生物活性

• 描述Forskolin is a strong adenylate cyclase activator with an IC50 of 41 nM. Forskolin can activate adenylyl cyclase in broken cell preparations as well as in intact tissues, thereby resulting in marked increases of intracellular cyclic adenosine phosphate (cAMP) accumulation^[1]. cAMP as a second messenger plays very important roles in biological processes. Forskolin elicits cellular responses which have been proposed to be dependent on cyclic AMP. In vitro studies have shown that forskolin significantly stimulated vasopressin (AVP) and oxytocin (OT) secretion from the rat neurohypophysis in a dose-dependent manner. Moreover, addition of forskolin to the rat hypotha-lamic SON in vitro increase cAMP accumulation, and Forskolin elicited a 3-fold greater increase in cyclic AMP in the neural lobe of the pituitary in vitro^[2].
  In human mesenchymal stromal cells (hMSCs), the use of Forskolin in different concentrations inhibits cell proliferation. At the same time, Forskolin induced alkaline phosphatase levels, bone-specific target genes, and secretion of insulin-like growth factor-1 in a manner related to concentration. The effect of forskolin on in vivo shows that bone formation ability significantly enhance after treatment of hMSCs with forskolin. In addition, 0.10mM forskolin displayed larger amounts of bone by pretreating hMSCs before implantation, compared with with 0.15 mM forskolin^[3]. Importantly, Forskolin has been shown to have a number of relevant anticancer effects, such as the induction of mesenchymal-to-epithelial transition, the inhibition of proliferation, motility, and migration in many types of cancer cells, indicating its perspectives as an effective anticancer agent^[4].
• 作用机制Forskolin is a strong adenylate cyclase activator via an interaction with the catalytic subunit of adenylate cyclase, directly activating the adenylate cyclase enzyme and raising intracellular cAMP levels.
• 细胞研究
• Cell Data

  Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
  3T3-L1	2.5/5 μM	Function Assay	24 h	significantly decreases ATGL protein expression at all doses tested	25590597
  3T3-L1 preadipocytes	10 μM	Function Assay	12 h	induces CREB phosphorylation and C/EBPβ expression	25928058
  AML-12	20 μM	Function Assay	3 h	upregulates the phosphorylation levels at Thr-411 and Ser-493	26048985

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• 动物研究
  剂量	Rat: 10 mg/kg - 30 mg/kg[5] (intragastric) Mice: 2.5 mg/kg - 10 mg/kg[6] (p.o.), 100 mg/kg[7] (p.o.)
  给药途径	Intragastric, p.o.

• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT03390985	-	-	Completed	-	-
  NCT02586883	Idiopathic Dilation of the Bro... more >>nchi Collapse <<	Not Applicable	Recruiting	April 2020	France ... more >> Necker-Enfants Malades Hospital Recruiting Paris, France, 75015 Contact: Isabelle SERMET-GAUDELUS, MD, PhD    +33144494887    isabelle.sermet@nck.aphp.fr Collapse <<
  NCT03455153	-	-	Completed	-	United Kingdom ... more >> Lindum Medical Practice Lincoln, Lincolnshire, United Kingdom, LN2 2JP Nettleham Medical Practice Lincoln, Lincolnshire, United Kingdom, LN2 2RS Birchwood Medical Practice Lincoln, Lincolnshire, United Kingdom, LN6 0QQ Collapse <<

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• 参考文献

• [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] Meeker RB, Michels KM, Hayward JN. Vasopressin and oxytocin regulation of cyclic AMP accumulation in rat hypothalamo-neurohypophysial explants in vitro. Neurosci Lett. 1990;114(2):225-30.

  [3] Doorn J, Siddappa R, et al. Forskolin enhances in vivo bone formation by human mesenchymal stromal cells. Tissue Eng Part A. 2012;18(5-6):558-67.

  [4] Sapio L, Gallo M, et al. The Natural cAMP Elevating Compound Forskolin in Cancer Therapy: Is It Time?. J Cell Physiol. 2017;232(5):922-927.