Forskolin
[CAS# 66575-29-9]

Identification

• Classification: Biochemical >> Plant extracts
• Name: Forskolin
• Synonyms: Colforsin; ForsLean; Coleonol; HL 362; L 75-1362B; NSC 357088; NSC 375489; (3R,4aR,5S,6S,6aS,10S,10aR,10bS)-5-(Acetyloxy)-3-ethenyldodecahydro-6,10,10b-trihydroxy-3,4a,7,7,10a-pentamethyl-1H-naphtho[2,1-b]pyran-1-one
• Molecular Formula: C₂₂H₃₄O₇
• Molecular Weight: 410.50
• CAS Registry Number: 66575-29-9
• EC Number: 266-410-9
• SMILES: CC(=O)O[C@H]1[C@H]([C@@H]2[C@]([C@H](CCC2(C)C)O)([C@@]3([C@@]1(O[C@@](CC3=O)(C)C=C)C)O)C)O

Properties

• Density: 1.2±0.1 g/cm³ Calc.^*
• Boiling point: 519.9±50.0 °C 760 mmHg (Calc.)^*
• Flash point: 171.8±23.6 °C (Calc.)^*
• Solubility: ethyl acetate:10mg/mL, DMSO: 5mg/mL, ethanol 6mg/mL (Expl.)
• Index of refraction: 1.552 (Calc.)^*

^* Calculated using Advanced Chemistry Development (ACD/Labs) Software.

Safety Data

• Hazard Symbols: GHS07 Warning
• Risk Statements: H312
• Safety Statements: P280-P302+P352-P317-P321-P362+P364-P501

Hazard Classification

Hazard	Class	Category Code	Hazard Statement
Acute toxicity	Acute Tox.	4	H312

Discovery and Applications

Forskolin is a natural compound derived from the root of the *Coleus forskohlii* plant, which is a member of the mint family. This plant has been traditionally used in Ayurvedic medicine for various health conditions, including heart disease, respiratory issues, and digestive problems. Forskolin is a diterpene compound and is known for its ability to activate the enzyme adenylate cyclase, which in turn increases the levels of cyclic adenosine monophosphate (cAMP) within cells.

The discovery of forskolin's effects on cAMP levels has made it a subject of significant interest in the fields of biochemistry and pharmacology. By increasing cAMP concentrations, forskolin influences a wide range of physiological processes, as cAMP is a critical signaling molecule involved in cellular communication and regulation. Specifically, forskolin activates adenylate cyclase, leading to an increase in cAMP, which can then activate protein kinase A (PKA) and trigger various downstream signaling pathways.

One of the most well-known applications of forskolin is in the field of cardiovascular health. Forskolin's ability to increase cAMP levels in heart muscle cells has led to its exploration as a potential treatment for heart conditions. It has been shown to have positive inotropic effects, meaning it can increase the force of contraction in the heart. This makes forskolin of interest for conditions such as heart failure, where improving the heart's contractility could be beneficial. Forskolin's effects on cAMP signaling also suggest that it may help in the regulation of blood pressure, as increased cAMP can promote vasodilation, or the relaxation of blood vessels.

In addition to its cardiovascular applications, forskolin has been studied for its potential in weight management and fat loss. The compound is believed to influence fat metabolism by increasing cAMP levels, which can enhance lipolysis—the breakdown of fat cells. As a result, forskolin has been marketed as a supplement for weight loss, though more rigorous clinical studies are required to confirm its effectiveness and safety for this purpose.

Forskolin also shows promise in the treatment of asthma and other respiratory conditions. By increasing cAMP levels, forskolin can help relax the smooth muscles in the airways, making it easier for patients with asthma or chronic obstructive pulmonary disease (COPD) to breathe. Forskolin’s bronchodilatory effects have made it a potential adjunct therapy for managing asthma symptoms.

Beyond these applications, forskolin has been investigated for its potential therapeutic effects in a variety of other conditions, including glaucoma, where its ability to increase cAMP may help reduce intraocular pressure, and in the treatment of certain types of cancer, where cAMP modulation could influence tumor growth and metastasis.

While forskolin has demonstrated therapeutic potential in several areas, its use is not without limitations. The compound's effects on cAMP are not tissue-specific, meaning that it can influence multiple systems in the body, some of which may lead to undesirable side effects. As a result, more research is needed to fully understand its mechanisms of action and to determine the optimal dosages and delivery methods for different therapeutic applications.

In summary, forskolin is a naturally occurring compound with a wide range of biological effects, particularly through its modulation of cAMP signaling. Its applications in cardiovascular health, respiratory conditions, and weight management make it a subject of ongoing research. However, further studies are needed to establish its safety and efficacy for these uses, and to develop more targeted therapies based on its molecular action.

References

1989. Minor diterpenoids of Coleus forskohlii. Phytochemistry, 28(1).
DOI: 10.1016/0031-9422(89)80130-x

2003. Aberrant Regulation of Human Intestinal Proglucagon Gene Expression in the NCI-H716 Cell Line. Endocrinology, 144(5).
DOI: 10.1210/en.2002-0049

2003. cAMP-induced changes of apical membrane potentials of confluent H441 monolayers. American Journal of Physiology. Lung Cellular and Molecular Physiology, 285(2).
DOI: 10.1152/ajplung.00412.2002