Forskolin
extract
supplements
by Ray Sahelian, M.D.
Health benefit of
forskolin extract supplement
Coleus forskohlii is an important traditional Ayurvedic herb that has been a
part of Indian medicine for centuries. In the 1970s, researchers isolated a chemically
active ingredient in the herb and called it forskolin. Now available in supplement form,
forskolin extract has been tested in a number of conditions. Forskolin extract is now found
in Diet Rx appetite suppressant and Passion Rx sexual enhancer.
Buy Forskolin extract supplement - Coleus Forskohlii
extract, 60 Capsules
Forskolin extract is produced from the root of coleus forskohlii, an
ancient Ayurvedic plant. Coleus is the source of a unique substance known as
forskolin. Modern extraction and analytical techniques are used to produce the
highest quality forskolin extract available. Each batch of coleus forskohlii extract is
analyzed and guaranteed to contain a minimum of 18% forskolin.
Forskolin supplement facts
Coleus Forskohlii root extract - 125 mg
Standardized to contain 10% forskolin (12.5 mg per
capsule)
Suggested use: One capsule
forskolin extract once
daily before breakfast.
Forskolin daily values are not established
Diet Rx natural appetite
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Benefits of Diet Rx with coleus forskohlii extract forskolin
All
natural appetite suppressant, decreases appetite so you eat less
Helps you maintain healthy blood sugar levels
Helps you maintain healthy cholesterol and lipid levels
Provides a variety of antioxidant from two dozen herbs and nutrients
Provides healthy fiber
Improves energy
Balances mood
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Improves will power and choice of food selection
Forskolin supplements and
weight loss
Body composition and hormonal adaptations associated with forskolin
consumption in overweight and obese men.
Obesity Research. 2005 Aug;13(8):1335-43. Godard MP, Johnson BA,
Richmond SR. University of Kansas, Department of Health, Sport and
Exercise Sciences, Applied Physiology Laboratory, Lawrence, KS 66045, USA.
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 forskolin group compared with the placebo group.
Oral ingestion of forskolin (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. The results indicate that forskolin is a
possible therapeutic agent for the management and treatment of obesity.
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 of forskolin
in psychiatry, researchers gave intravenous forskolin 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.
Forskolin has been found to benefit asthma
patients.
Forskolin ocular drops have been used to decrease intraocular pressure due to
glaucoma
Forskolin may be beneficial as a bronchodilator and anti-allergy agent.
Forskolin may reduce blood pressure.
Forskolin 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.
Forskolin may be helpful in urinary tract infections.
Forskolin 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 with 12.5 mg forskolin.
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 forskolin content of crude coleus products may not be sufficient to produce a
pharmacological effect. It is best to use standardized extracts which have
concentrated the forskolin content.
Coleus forskohlii
is available in various extract potencies, for instance 10 percent forskolin, 18
percent forskolin, and 20 percent forskolin. 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 Jan 1;36(1):13-20.
Forskolin
activates adenylate cyclase in membranes from a variety of mammalian tissues. We
found that forskolin 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 forskolin modulates the release of mediators
of immediate hypersensitivity reactions via the activation of adenylate cyclase
in human basophils and mast cells.
Forskolin for asthma
Forskolin versus sodium cromoglycate for prevention of asthma attacks: a
single-blinded clinical trial.
J Int Med Res. 2006 Mar-Apr. González-Sánchez R, Trujillo X, Trujillo-Hernández
B, Vásquez C, Huerta M, Elizalde A.
Servicio de Pediatría, Hospital del Instituto Mexicano del Seguro Social,
Manzanillo, Colima, México.
To determine the efficacy of forskolin in preventing asthma attacks, we
performed a single-blinded clinical study in children and adult out-patients at
a public hospital in Mexico. 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;165(4):225-37.
We investigated the relaxant effects of forskolin on guinea pig
airway smooth muscle. 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 of forskolin on tracheal smooth muscle
did not change, whereas with the same pretreatment the relaxant effect of
isoproterenol diminished. These
results suggest that forskolin 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.
Forskolin and 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, online April 8,
2007.
Comments: Whether forskolin supplements taken orally help
individuals with bladder infections is not clear until human trials are done.
Forskolin and cancer
Forskolin: a potential antimetastatic agent.
Int J Cancer. 1983 Dec 15;32(6):801-4.
Forskolin, a diterpene from the roots of an Indian plant, Coleus forskohlii,
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 of forskolin 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%. Similar results were obtained in
three separate experiments. 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 Nov;158(5):1752-8; discussion 1758-9.
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. Dose-dependent hemodynamic responses to intracavernosal
forskolin were evaluated in a New Zealand White rabbit model. In vitro forskolin and prostaglandin E1 alone caused
concentration dependent relaxation. When the 2 agents were combined, the concentration response
curve for relaxation shifted to the left. cAMP production was highest in cells
treated with prostaglandin E1 and forskolin and was unaffected by papaverine or
phentolamine. 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.
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Forskolin and gastric tissue
Isolated gastric glands were used to investigate the action of forskolin,
a novel diterpene extracted from the Indian plant Coleus forskohlii. Forskolin
was found to stimulate both acid formation and pepsinogen secretion. The
stimulation was rapid, reversible and dose dependent. The efficacy of forskolin
was similar to that of more commonly used secretagogues, e.g. histamine,
carbachol, cyclic AMP derivatives. Forskolin was found to be more effective in
activating adenyl cyclase than histamine, isoproterenol or NaF. Treatment of
gastric glands with forskolin resulted in a 100-fold increase in tissue cAMP
levels, supporting the idea that forskolin activates adenyl cyclase in the
intact cell. The results are interpreted to show that forskolin stimulation of
gastric secretions is due to activation of adenyl cyclase with a consequent
increase in tissue cAMP.
Forskolin for glaucoma
Forskolin lowers intraocular pressure by reducing
aqueous inflow.
Invest Ophthalmol Vis Sci. 1984 Mar;25(3):268-77.
Forskolin lowers the intraocular pressure of rabbits, monkeys, and
humans. In rabbits, net aqueous humor inflow decreases, outflow facility remains
unchanged, and ciliary blood flow increases. Tolerance to the intraocular
pressure lowering effect did not occur in rabbits after topical doses given
every 6 hr for 15 days. In vitro forskolin activates adenylate cyclase of crude
particulate homogenates prepared from cultured human ciliary epithelia or from
dissected ciliary epithelial processes of rabbit or human eyes. This activation
is not blocked by timolol. The stimulation of adenylate cyclase by isoproterenol
in vitro is potentiated in the presence of forskolin. Forskolin represents a
potentially useful class of antiglaucoma agents differing in molecular mechanism
of action from previously used drugs.
Forskolin and heart muscle
Forskolin exerts its actions on cells by directly activating the catalytic subunit of adenylatecyclases. The primary effect on heart muscles is the positive inotropic
one, at higher forskolin concentrations, an acceleration of the pacemaker
activity can be observed. External calcium is required for this augmentation of
contraction. Verapamil, prenylamine and tetrodotoxin depress these effects.
Forskolin mechanism of action
Forskolin is a diterpene from the roots of the Indian plant Coleus forskohli which
directly activates the adenylate cyclase and raises cyclic AMP levels in a variety of
tissues.
Cyclic AMP is an important cell regulating compound. Once formed it activates
many other enzymes involved in diverse cellular functions. Under normal
situations cAMP is formed when a stimulatory hormone (e.g., epinephrine) binds
to a receptor site on the cell membrane and stimulates the activation of
adenylate cyclase. This enzyme is incorporated into all cellular membranes and
only the specificity of the receptor determines which hormone will activate it
in a particular cell. Forskolin appears to bypass this need for direct hormonal
activation of adenylate cyclase. As a result of this direct activation of
adenylate cyclase, intracellular cAMP levels rise. The physiological and
biochemical effects of a raised intracellular cAMP level include: inhibition of
platelet activation; inhibition of mast cell degranulation and histamine
release; increased force of contraction of heart muscle; relaxation of the
arteries and other smooth muscles; increased insulin secretion; and increased
thyroid function.
Forskolin summary
With so many interesting possibilities, forkolin will likely be continued
to be studied for a long time. Unfortunately, at this point in time, we don't
know enough about forskolin to know for certain which clinical conditions it can
be used effectively and safely.
Topical forskolin
Treatment with forskolin can promote skin pigmentation and protect
against the UV light-induced damage. Fair-skinned individuals do not tan when
exposed to UV light due to a defective melanocortin 1 receptor (MC1R) gene --
one of several genes that regulate skin, hair and eye color. The gene plays a
key role in determining if a person has red hair, light skin and sensitivity to
UV light. However, a functional MC1R is not required to achieve skin
pigmentation. Dr. David E. Fisher, from the Dana Farber Cancer Institute in
Boston, and colleagues investigated the effects of UV light in mice lacking a
working MC1R gene. UV light exposure induced melanocyte stimulating hormone
expression in keratinocytes (skin cells) of these red / blonde-haired mice, but
pigmentation did not take place. Melanocytes are a type of skin cells that
produce pigment. Topical application of forskolin, however, caused pigmentation
to occur without the need for UV light, showing that functional MC1R is, in
fact, not required. Testing in skin cancer-prone mice showed that forskolin
treatment protected the animals from UV light-induced skin DNA damage. Nature
September 21, 2006.
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Forskolin Research
Induction of Drug Metabolism by Forskolin, the Role of The Pregnane X
Receptor and the PKA Signal Transduction Pathway.
J Pharmacol Exp Ther. 2004 Sep 30
Ding X, Staudinger J. University of Kansas.
The active ingredient in Coleus forskohlii
extract is the diterpene compound forskolin. Forskolin is a widely used
biochemical tool that activates adenyl cyclase, thereby increasing intracellular
concentration of cAMP, and thus activating the PKA signal transduction pathway.
Both forskolin and its non-adenyl cyclase-activating analog
1,9 dideoxyforskolin induce CYP3A gene expression in primary hepatocytes by
functioning as agonists of the pregnane X receptor. Activation of PKA signaling potentiates PXR-mediated induction of CYP3A gene expression in
cultured hepatocytes and increases the strength of PXR-coactivator
protein-protein interaction in cell-based assays. Kinase assays show that PXR
can serve as a substrate for catalytically active PKA in vitro. Our data provide
important insights into the molecular mechanism of both the PKA-dependent and
the PKA-independent effects of forskolin on the expression of drug-metabolizing
enzymes in liver. Finally, our data suggest that herbal therapy with Coleus
forskohlii extract should be approached cautiously due to the potential for
herb-drug interactions in patients on combination therapy.
Traditional uses of coleus
forskholii extract forskolin
An extract of the plant coleus forskohlii has been used for centuries in
Ayurvedic medicine to treat various diseases such as hypothyroidism, heart
disease and respiratory disorders.
Forskolin emails
Q. Does forskolin extract supplement reduce blood pressure?
A. We have not seen any definitive research evaluating forskolin
supplements and hypertension in humans.
Q. Just want to know if there is any evidence of
tolerance in the continued administration of forskolin. It seems that there are
a number of beneficial effects, including enhanced exercise tolerance. I have
been taking Tenormin for years and forskolin definitely helps. My brother in law
is a physician and he wondered if forskolin is something that I should cycle on
and off of. Can't find mention of tolerance to forskolin on the internet.
A. The reason there is little info on forskolin is
because there is hardly any human studies published with the use of forskolin
supplements for prolonged periods, so we really don't know at this time.
This forskolin page was last updated in January 2008.