Forskolin | apollo +9191 46 950 950

Forskolin | apollo +9191 46 950 950

Forskolin

CAS Number : 64657-11-0

Molecular Formula : C22H34O7

Molecular Weight : 410.50 g/mol

Systematic (IUPAC) : (3R,4aR,5S,6S,6aS,10S,10aR,10bS)-3-ethenyl-6,10,10b-

trihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-dodecahydro-1H-naphtho[2,1-b]pyran-5-yl acetate

What is Forskolin?

C. barbatus is a perennial herb in a large genus of mints. The plant is native to subtropical and tropical regions of

India and east Africa.

What is Forskolin used for?

Traditional/Ethnobotanical uses-

This species and other related species were used in many traditional medical systems. Traditional medical uses

include the treatment of digestive disorders (stomachache, gastric and intestinal spasm, nausea, as a purgative), skin (burns, wounds, insect bites, allergies), infections (eg, syphilis, ringworm), and other conditions, including neck stiffness, and rheumatism, and to induce menstruation and as an oral contraceptive. Forskolin

has also been used to treat heart, blood, and circulation conditions, and cancers. In the 1970s, the plant's

cardiovascular activity was investigated.

General uses-

Forskolin has multiple sites of action and should be used with caution. Forskolin derivatives have been developed for use in heart/blood vessel conditions. Quality clinical trials are lacking to support claims made of the weight

loss properties of forskolin, and clinical studies conducted with oral and inhaled forskolin in patients

with asthma are limited.

What is the dosage of Forskolin?

Asthma: Oral forskolin has been studied using 10 mg daily over 2 to 6 months. Obesity: 250 mg of a 10%

forskolin extract twice daily for 12 weeks has been studied.

Is Forskolin safe?

Contraindications-

Case reports are lacking.

Pregnancy/nursing-

Information regarding safety and efficacy in pregnancy and lactation is lacking. P. barbatus has been

traditionally used to induce menstruation and as an oral contraceptive.

Side Effects

Clinical trial data are generally lacking. Adverse events reported with the use of colforsin (a forskolin derivative) include rapid or irregular heart rate. Forskolin should be

avoided in patients with polycystic kidney disease.

Toxicities

Information is limited. Embryo-related toxicity has been reported.

Forskolin supplements and weight loss

Body composition and hormonal adaptations associated with forskolin consumption in overweight and obese

men.

Obesity Research. 2005.

This study examined the effect of forskolin on body composition, testosterone, metabolic rate, and blood pressure in overweight and obese men. Thirty subjects

were studied in a randomized, double-blind, placebo-controlled study for 12 weeks. Forskolin was shown to

elicit favorable changes in body composition by significantly decreasing body fat percentage and fat

mass. There was a trend toward a significant increase for lean body mass in the treatment group compared with

the placebo group. Oral ingestion (250 mg of 10% forskolin extract twice a day) for a 12-week period was

shown to favorably alter body composition while concurrently increasing bone mass and serum free testosterone levels in overweight and obese men.

Forskolin benefits

Over the years studies have shown that forskolin is a platelet aggregation inhibitor, relaxes vascular smooth muscle, decreases intraocular pressure due to glaucoma,

and has anti-allergy potential since it inhibits IgE-mediated release of histamine and peptide leukotriene from human basophils and mast cells. Forskolin has

been shown to be a potent inhibitor of cancer metastasis in mice injected with malignant cells. In a study in psychiatry, researchers gave it intravenous to four depressed and five schizophrenic patients. All four

depressed patients showed a transient mood elevation or stimulation, as did two of the five schizophrenic

patients.

This substance may be beneficial as a bronchodilator and anti-allergy agent.

May reduce blood pressure.

It is a United States Food and Drug Administration non-approved vasoactive agent that acts in synergism with prostaglandin E1 to induce smooth muscle relaxation.

In combination with other vasoactive agents, forskolin has demonstrated preliminary safety and efficacy in

patients with vascular impotence. See Passion Rx below for a product that has libido boosting properties.

Dosage

Forskolin is available over the counter in pills and liquid in a variety of dosages — most commonly 50 mg coleus forskohlii herbal extract providing 9 mg forskolin and 125 mg coleus forskohlii extract providing 12.5 mg. Research is limited on the appropriate dosages for

different conditions. The forskolin content of coleus root is typically 0.2% to 0.3%, therefore the content of crude

coleus products may not be sufficient to produce a pharmacological effect. It is best to use standardized

extracts which have it concentrated.

Coleus forskohlii is available in various extract potencies, for instance 10 percent forskolin, 18 percent, and 20 percent. We are not aware of any research that has tested various extract potencies to determine which

is best to use.

Forskolin for allergy

Inhibition of IgE-mediated release of histamine and peptide leukotriene from human basophils and mast

cells by forskolin.

Biochem Pharmacol. 1987.

We found that it caused a concentration-related inhibition of IgE-mediated release of histamine and peptide leukotriene C4 (LTC4) from human basophils and lung mast cells. Our data suggest that it modulates the release of mediators of immediate hypersensitivity

reactions via the activation of adenylate cyclase in human basophils and mast cells.

Forskolin for asthma

It is still not very clear to me whether this natural extract is effective for asthma. Results of studies have not been

very convincing.

J Int Med Res. 2010.

Forskolin compared with beclomethasone for prevention of asthma attacks: a single-blind clinical trial.

Patients with mild or moderately persistent adult asthma were randomly assigned to receive forskolin

(one 10-mg capsule orally per day) or beclomethasone (two 50 microg inhalations every 12 h) for 2 months. No statistically significant improvement occurred in any lung function parameter in the forskolin-treated

patients. There was no statistically significant difference between both treatment groups for any lung function parameter at baseline or after treatment. None of the beclomethasone-treated patients had an asthma attack and one forskolin-treated patient had a mild asthma

attack during the 2-month study period.

Forskolin versus sodium cromoglycate for prevention of asthma attacks: a single-blinded clinical trial.

J Int Med Res. 2006.

Forty patients of either sex with mild persistent or moderate persistent asthma were assigned randomly to 6 months of treatment with forskolin at 10 mg a day orally (capsules) or with two inhalations of sodium cromoglycate every 8 h, i.e. three times a day. The

number of patients who had asthma attacks during the treatment period was significantly lower among those receiving forskolin (40%) than among those receiving

sodium cromoglycate (85%). We conclude that forskolin is more effective than sodium cromoglycate in preventing asthma attacks in patients with mild

persistent or moderate persistent asthma.

Relaxant effects of forskolin on guinea pig tracheal smooth muscle.

Lung. 1987.

Forskolin caused dose-dependent relaxant effects on resting tone and on leukotriene C4, leukotriene D4, and

carbachol-induced contraction of tracheal smooth muscle. Moreover, with propranolol pretreatment the relaxant effect on tracheal smooth muscle did not change, whereas with the same pretreatment the relaxant effect of isoproterenol diminished. These

results suggest that it relaxes airway smooth muscle in guinea pigs in vitro and in vivo by raising tissue cyclic

AMP levels and that its actions are independent of beta-adrenoceptors.

Bladder, urinary tract infections

Forskolin may boost the ability of antibiotics to kill E. coli -- the bacteria responsible for 90 percent of bladder infections. In studies in mice, Duke microbiologist Dr. Soman N. Abraham found that E. coli bacteria hide in cells lining the bladder, out of reach of antibiotics. However, when the researchers injected forskolin

directly into the bladder or administered it intravenously, it appeared to expel more than 75 percent of "hiding" E. coli, rendering it susceptible to antibiotics.

While customary antibiotic treatment kills the vast majority of the bacteria, according to Dr. Soman

Abraham, small numbers of bacteria may survive the antibiotic bath by sneaking into the lining of the bladder.

There they lie there until the opportune moment, after antibiotic treatment, to come out and start multiplying again. By revving up cellular activity, forskolin helps flush out bacteria from their niches and into the urine,

where they can be killed by antibiotics. Nature Medicine, 2007.

Cancer

Forskolin: a potential antimetastatic agent.

Int J Cancer. 1983.

Forskolin is a potent platelet aggregation inhibitor and has been examined for its effects on (a) tumor-induced human platelet aggregation and (b) pulmonary tumor colonization in mice. These studies employed a subline of B16 murine melanoma, B16-F10 (highly metastatic to lungs). Forskolin strongly inhibits the melanoma cell-induced human platelet aggregation. A single dose

administered intraperitoneally 30 or 60 min prior to tail vein injection of cultured B16-F10 cells reduced tumor colonization in the lungs by more than 70%. These

findings raise the possibility that forskolin could prove of value in the clinic for the prevention of cancer

metastasis.

Forskolin extract and impotence

One study evaluated the role of forskolin as an injection into the corpus cavernosum of the penis. In many cases there was improvement in rigidity and/or erection.

Intracavernosal forskolin: role in management of vasculogenic impotence resistant to standard 3-agent

pharmacotherapy.

J Urol 1997.

We investigated forskolin, a direct adenylate cyclase activator, as an intracavernosal vasoactive agent in

management of vasculogenic impotence. Concentration responses for forskolin and prostaglandin E1 induced relaxation of phenylephrine precontracted strips of human corpus cavernosum smooth muscle were

constructed in vitro. Cyclic adenosine monophosphate (cAMP) synthesis was determined with papaverine,

phentolamine, prostaglandin E1 and forskolin in human corpus cavernosum smooth muscle cell cultures. In vitro

forskolin and prostaglandin E1 alone caused concentration dependent relaxation. Clinical

investigation in 31 patients showed no adverse events. Overall 61% reported improvement in rigidity and/or erection duration using intracavernosal forskolin, papaverine, phentolamine and prostaglandin E1.

Forskolin acts in synergism with prostaglandin E1 to induce smooth muscle relaxation. In combination with other vasoactive agents, forskolin has demonstrated

preliminary safety and efficacy in patients with vasculogenic impotence resistant to standard 3-agent

pharmacotherapy.

Overview

Forskolin is a chemical found in the roots of the plant Plectranthus barbatus (Coleus forskohlii). This plant has been used since ancient times to treat heart disorders such as high blood pressure and chest pain (angina), as

well as respiratory disorders such as asthma.

When taken by mouth, forskolin is also used to treat allergies, skin conditions such as eczema and psoriasis,

obesity, painful menstrual periods, irritable bowel syndrome (IBS), urinary tract infections (UTI), bladder

infections, advanced cancer, blood clots, sexual problems in men, trouble sleeping (insomnia), and

convulsions.

Healthcare providers sometimes give forskolin intravenously (by IV) for heart failure.

Some people breathe in (inhale) forskolin powder for asthma.

Forskolin drops are used in the eyes to treat glaucoma.

Herbal product manufacturers are now producing Coleus forskohlii extracts that contain high levels of

forskolin. These preparations are being promoted for the same conditions for which forskolin has been

traditionally used. However, currently there is no reliable scientific information that shows Coleus forskohlii extracts taken by mouth are effective.

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