Forskolin is a diterpene produced by members of the mint family. Apart from widely being used as a weight loss supplement, it has many benefits like lowering blood pressure, stimulating cyclic AMP and preventing blood vessel blockage. The following article will discuss the health benefits and other potential uses of forskolin and forskolin derivatives.
What is Forskolin?
Forskolin is a popular supplement and research tool that entered medical practice from Ayurvedic medicine. It is obtained from the dried root of an Indian plant known as Plectranthus barbatus or Coleus forskohlii [1, 2].
- colforsin daropate
How Does Forskolin Work?
Why Is cAMP So Important?
Cyclic adenosine monophosphate or cAMP is a molecule derived from adenosine – a nucleotide that is also a part of DNA and RNA .
It activates several proteins, including protein kinase A, exchange protein activated by cAMP (Epac) and AMP-activated protein kinase (AMPKA). Through these proteins, cAMP determines the reaction of the cells to hormones and maintains energy balance [13, 14].
Health Benefits, Potential Uses of Forskolin & Side Effects
1) Weight Loss
In one clinical trial Coleus forskohlii together with the low-calorie diet was counteracted weight-gain associated with metabolic issues. Patients that had a low-calorie diet and took the forskolin had lower weight and improved insulin resistance .
It was also shown that forskolin along with rolipram induced fat destruction and prevented weight gain .
cAMP also influences fat storage .
2) May Decrease Risk For Diabetes
Though there is no data that directly shows that forskolin helps in diabetic conditions, it was proposed as a drug to help treat one of the complications of diabetes – diabetic retinopathy .
Diabetic retinopathy is caused by high levels of sugar that damage small eye vessels and cause blood to leak into the eye and damage vision.
It is also good for suppressing inflammation, which often worsens diabetes.
3) May Improve Immunity
It was recently found that forskolin helps killer immune cell development .
Forskolin does not act by blocking IL-2 directly, as cAMP is actually increasing the level of this protein. It is known to destroy the relationship between proteins that carry information into the cell and activate the development of appropriate changes .
It is also known that cAMP can reduce inflammation by suppressing RAGE protein, which initiates the development of inflammation .
There is also a report showing that cAMP-elevating drugs, including forskolin, are able to block the production of potentially inflammatory protein GM-CSF .
There is also evidence that forskolin induces immune cell production of a number of substances beneficial in treating chronic inflammation .
It should be noted that while the immune cells produce some useful proteins, their activity is partly blocked by forskolin .
The dual effect of forskolin may be explained by the fact that cAMP selectively drives the development of immune cells in favor of certain types, blocking other types of cells and reactions .
4) May Kill Cancer Cells
Forskolin can influence cancer cells through a number of mechanisms and is now viewed as a promising assisting drug in cancer therapy.
First of all, forskolin activates protein phosphatase 2A (PP2A), that is blocked in some cancers especially leukemias – cancers of blood cells. PP2A is an important protein that activates many enzymes in the cell .
Restoration of PP2A activity with forskolin blocks cancer cell development and induces cancer cell death. It can also enhance the effect of standard anti-cancer drugs such as Idarubicin and Ara-c .
Activation of PP2A also causes cell death in cancer of the prostate .
In addition, forskolin enhances the action of chemotherapy drugs 5-fluorouracil and oxaliplatin when treating colon cancer and causes cancer cell death due to the same mechanism. This drug also increases the benefits of dexamethasone [39, 40].
Forskolin is also known to block Hedgehog – a protein crucially important in early development, as it determines the fate of all the organs in the newly formed embryo. In a grown organism Hedgehog can help cancer cells move to other locations and form metastases. By inhibiting hedgehog forskolin prevents the development of new cancer cells and tumor growth .
It also prevents the invasion of cancer cells into other organs. It was also shown that by increasing the level of cAMP and activating PKA forskolin blocks a gene called gli1 besides Hedgehog. Through this mechanism cancer growth in the brain can be prevented [42, 43, 43, 44].
Research on brain cancer cell lines also shows that forskolin block editing of gene products thus preventing the development of new cancer cells from brain cells .
Forskolin can also cause changes in cancer cells of leukemia and myeloma that make them sensitive to glucocorticoids. This makes glucocorticoid cancer therapy more effective .
5) May Improve Heart Health
According to recent research, forskolin can be used to treat heart disease.
Forskolin blocks the movement of Ca2+ into muscle cells, thus preventing contraction of muscle cells in the heart and blood vessels. Muscle relaxation is very important in preventing heart attacks .
It was also proposed that new forskolin derivative, NKH477, can reverse damage to the heart in rats with heart attack .
NKH477 at present is viewed as a promising drug that can make the heart to work at a proper pace .
It was also shown in experiments on heart cells that forskolin reverses some defects associated with a type of heart failure called mitral deficiency, which may improve outcomes after heart operations for this type of problem .
NKH477 can be also used as a preventive measure during surgery as it prevents heart failure by narcotic drugs used in anaesthesiology .
Forskolin derivatives NKH77 and DMAPD increase the level of cAMP in heart cells better than forskolin itself and are more effective for heart therapy .
6) May Lower Blood Pressure
It was known since the 80s that forskolin helps muscles in blood vessels relax, thus helping the blood flow .
The same effect was observed a decade later for the forskolin derivative, NKH477 .
Coleus forskohlii extract is shown to lower blood pressure in older patients due to forskolin ability to relax muscle cells in blood vessels .
7) May Prevent Surgical Complications
Drugs used during surgery can cause problems with the heart, breathing, and kidney. Using forskolin before operations can prevent such complications, as is shown below.
As it was said earlier, NKH477 reverses the heart failure caused by narcotic drugs used in surgery such as pentobarbital, propranolol or verapamil, thus preventing heart arrest .
Pretreatment of sheep before surgery with forskolin prevents the blockage of blood vessels and relaxes vessel muscles, thus improving blood flow .
Another forskolin derivative, colforsin daropate, prevents complications by improving blood flow when taken before undergoing surgery for blood vessel transplants .
Also, synthetic blood vessel grafts coated with forskolin are better accepted into patients organism as there is no immune cell attachment on their surface and they do not get rejected by the patient’s immune system .
8) May Help Breathing
Forskolin also relaxes muscles in the lung, helping to breathe. Injection or inhalation of forskolin derivative NKH477 prevents the constriction of lungs during surgery and may be also used for asthma.
It also lowers blood pressure during surgery, which may prevent bleeding .
Colforsin daropate, a forskolin derivative, prevents tightening of the lungs in humans, which is useful for asthma attacks .
It was found to be more effective than sodium cromoglycate .
As for beclomethasone, no significant differences were found .
It should be noted, that cAMP alone actually can cause asthma attacks .
9) Used For Skin Treatment
Forskolin and C. forskohlii extract are often used for skin treatments. For example, it was shown that forskolin can induce migration of skin cells to the place of the wound helping its healing .
Certain types of ultraviolet rays emitted by the sun are actually dangerous, damaging the genetic information in the skin cells.
Application of forskolin to skin cell culture repairs such damage and prevents skin cell death .
Also, forskolin treatment makes the skin thicker and resistant to UV light .
It was shown in the lab setting that in animals that do not possess an active melanin gene, forskolin increases the production of a protein similar to melanin-eumelanin, thus activating an alternative mechanism of protection .
Forskolin can also prevent aging by counteracting damage to the genes and eliminating destructive types of oxygen .
Comparison of skin treatment with forskolin and C. forskohlii extract has shown that forskolin gets into the skin faster if it a part of the plant extract .
10) May Influence Egg Cells And Sperm
Forskolin can also influence reproductive cells both in men and women.
In the case for women, forskolin in combination with cilostamide improved the development of human egg cells .
Even without the presence of other drugs forskolin increases the rate of egg cell division and makes them more likely to be fertilized and develop into an embryo .
In course of laboratory research on pig egg cells, it was found that forskolin is able to control the development of pig oocytes and increases the production of progesterone, a protein important for the development of the embryo .
Forskolin can also play a role in male reproduction. Forskolin in low doses can increase testosterone production by testes cells as well as the production of cAMP, but in high doses, it can block the same processes [73, 10].
Also, forskolin is able to increase the level of cAMP in an appropriate part of the sperm cell and make the cell more likely to get inside the egg cell .
11) May Be Good For Nerve Cells
There is a number of research reports that show the influence of forskolin and P. barbatus/C. forskohlii extract on nerve cells in different conditions.
P. barbatus herbal tea can protect nerve cells enzyme acetylcholinesterase. This protein can be toxic to the organism, so P. barbatus tea is a potential antidote against this type of poisoning .
It was also discovered in rats with a brain injury that forskolin derivative NKH477 prevents complications in affected animals by elevating cAMP .
cAMP is involved in many other processes of nerve cell development and protection. For example, cAMP can be used to protect nerve cells from toxic proteins in some diseases that involve nerve cells destruction by initiating ubiquitin protein production .
cAMP is also important for the activity of pituitary gland, which is a part of the brain. The pituitary gland controls a wide array of processes, mainly those controlled by hormones. The ability of pituitary gland cells to react to the changes in the organism and in the surrounding depends on cyclic nucleotides, including cAMP .
By increasing cAMP level, forskolin makes nerve cells of pituitary gland produce electrical impulses and regulatory chemical substances.
Among other necessary substances, cAMP increases the production of prolactin by certain specialized cells in the pituitary gland. Prolactin is mainly known as a hormone that stimulates the production of milk for feeding in mothers but also controls many other processes that are crucial for well being and even mood .
cAMP can be also used in therapy after nerve injuries. For instance, a combination of drugs promoting cell growth together with cAMP injections promotes nerve cell growth and regeneration after injury .
cAMP is so crucial in nerve development, that normal development of the eye retina depends on the regulation of cAMP level inside the cell .
Forskolin is also found to be influencing the activity of the nerve cells responsible for hearing in the brain .
Forskolin can be also used indirectly for treating nerve disorders such as autism, epilepsy, and schizophrenia, as it is used together with a protein Ascl1 to reprogram connective tissue cells into a certain type of neurons .
12) May Improve Glaucoma
Forskolin and cAMP influence on the eye nerve cells is so profound that forskolin – containing substances are actively reviewed for treatment of glaucoma and other eye diseases.
Here it was already mentioned that forskolin can be used for the treatment of diabetic retinopathy .
cAMP is also known to be very important in retinal development .
It is known that soluble adenylyl cyclase, an enzyme directly making cAMP, active in different parts of the eye and plays an important role in their function .
Food supplements containing forskolin and other useful substances have improved the condition of patients with glaucoma .
In case of injuries to the eye blood vessels, complex injections into the eye with forskolin, homotaurine, and L-carnosine prevents nerve cell death in the eye after elevating of the intraocular blood pressure .
13) May Improve X-Adrenoleukodystrophy
x-ALD or x-adrenoleukodystrophy is a disease caused by the faulty transformation of molecules called long-chain fatty acids. cAMP helps lower the level of such acids and also blocks a number of cytokines driving the disease progress .
14) May Help With HIV Infection
There is one experimental report indicating that P. barbatus extract blocks the activity of proteins derived from the HIV virus .
Unfortunately, there are no more reports that corroborate or refute this statement.
Forskolin Can Be Toxic And Can Interfere With Other Drugs
Here is the review of the literature concerning this topic.
- Forskohlii extract can potentially damage the liver. It was shown in laboratory animals that Coleus forskohlii extract increases the level of a number of proteins in the liver which may result in damage to the organ .
- It should be noted that the diet of the patient is of importance. C. forskohlii extract was shown to be most toxic in cases where the animals were fed products with a high level of starch (is present in high quantities in grain and potatoes) .
- Forskohlii extract also interacts badly with tolbutamide that lowers the level of sugar in the blood. The plant extract increases the level of a protein called cytochrome P450 and prevents tolbutamide from lowering blood sugar levels .
The same cytochrome P450, increased by C. forskohlii extract, blocks the action of warfarin, a drug preventing blood flow blockages .
Besides activating potentially damaging proteins in the liver, C.forskohlii also leads to the increase in the size of the liver and quantity of fat it contains .
There Are Novel Ways Of Forskolin Synthesis
Due to wide use of the compound, difficulties inherent to terpene synthesis and potential hepatotoxicity of natural sources, there is a demand for new methods of production .
One method uses genetically engineered yeast to make 11β-hydroxy-manoyl oxide, a similar compound which can be used to make forskolin .
Another biosynthetic method introduces C. forskohlii genetic material to E.coli in order to produce manoyl oxide, another forskolin precursor .
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