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Diterpene Forskolin (Coleus forskohlii, Benth.): A possible new compound for reduction of body weight by increasing lean body mass

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Abstract

Maintaining or increasing lean body mass should be one of the important considerations of any weight loss strategy for the following reasons: 1. increase in lean body mass is proportionate to an increase in the body’s thermogenic response to food and the basic metabolic rate (BMR); 2. food induced thermogenesis controls body weight by an increase in catabolism of body fat (thermogenesis is preferentially fueled by fatty acids derived from body fat and/or from food); and 3. enhanced thermogenesis contributes to a buildup of lean body mass.
NUTRACEUTICALS
MARCH/APRIL 2002
6
Maintaining or increasing
lean body mass should
be one of the important
considerations of any
weight loss strategy for the following
reasons:
1. increase in lean body mass is
proportionate to an increase in the
body’s thermogenic response to
food and the basic metabolic rate
(BMR);
2. food induced thermogenesis
controls body weight by an increase
in catabolism of body fat
(thermogenesis is preferentially
fueled by fatty acids derived from
body fat and/or from food); and
3. enhanced thermogenesis contributes
to a buildup of lean body mass.
An extract of Coleus forskohlii root, Benth.
(Fam. Labiatae) standardized for diterpene
forskolin was tested in an open-field study
for weight loss and lean body mass
increase. The study’s hypothesis was based
on the recognized role of diterpene
forskolin as the plant derived compound
which stimulates enzyme adenylate cyclase
and subsequently cyclic AMP
(3’5’adenosine monophosphate) (1,2).
Cyclic AMP may release fatty acids from the
adipose tissue depots which may result in
enhanced thermogenesis (3), loss of body
fat, and theoretically increased lean body
mass.
Six overweight, but otherwise healthy,
women were selected for the trial. Each
participant was informed about the
purpose of the study and was asked to
sign an informed consent before
entering the study. Each participant was
examined by a physician at the inception
and after 4 and 8 weeks of the study.
The body composition was determined
by bioelectrical impedance analysis. The
forskolin formula was prepared in the
form of two piece hard shell capsules.
Each capsule contained 250 mg of the
extract standardized for 10% forskolin,
and each bottle contained 60 capsules.
Participants were instructed to take one
capsule in the morning and one in the
evening, half an hour before a meal.
Each participant was asked to maintain
their previous daily physical exercise
habits and eating habits. In addition,
physical activity was monitored based on
a questionnaire before and during the
trial. The study was performed in an
outpatient bariatric clinic at Hilton Head,
S.C. and supervised by a physician
specializing in bariatric medicine for over
30 years.
During the eight week trial the mean
values for body weight, and fat content
were significantly decreased, whereas
lean body mass was significantly
increased as compared to the baseline
(Wilcoxon matched pairs test). Weight
loss was statistically significant (p<0.05)
after 4 and 8 weeks, and the mean
amounted to 4.3 and 9.17 lbs
respectively. The body fat values
expressed as % body fat were: 0 weeks
33.63 ±3.02, 4 weeks 30.10 ±4.34
(statistically not significant or n.s.), and
8 weeks 25.88 ±4.77 (p<0.05). The
lean body mass values expressed as % lean
body mass were: 0 weeks 67.07 ±3.02,
4 weeks 69.90 ±4.34 (n.s.), and
8 weeks 74.13 ±4.77 (p<0.05).
The eight week therapy with 50 mg of
forskolin per day did not adversely affect
the systolic/diastolic blood pressure nor
the pulse rate. A trend has been
observed to lower the systolic/diastolic
pressure in the course of treatment.
Systolic pressure (mm Hg) was
0 weeks 113.67 ±14.50,
4 weeks 110.00 ±18.93(n.s.), and
8 weeks 104.50 ±17.54(n.s.). Diastolic
NUTRACEUTICALS
Diterpene Forskolin
(
Coleus forskohlii, Benth.
):
A possible new compound
for reduction of body
weight by increasing
lean body mass
VLADIMIR BADMAEV 1
MUHAMMED MAJEED
ANTHONY A. CONTE
JOHN E. PARKER
Sabinsa Corporation
121 Ethel Road West, Unit 6
Piscataway, NJ 08854, USA
1. Tel +1 732 777-1111
Fax +1 732 777-1443
E-mail vebadmaev@attglobal.net
NNutraCCos
MARCH/APRIL 2002 7
pressure (mmHg) was 0 weeks
71.00 ±12.76, 4 weeks 69.33 ±9.93
(n.s.), and 8 weeks 66.00 ±8.49(n.s.).
Pulse rate (beats/min) was 0 weeks
66.33 ±8.02, 4 weeks 69.00 ±7.97(n.s.),
and 8 weeks 74.67 ±11.55(n.s.).
This preliminary data obtained with
250 mg bid of a 10% extract of Coleus
forskohlii indicate that this botanical
bears promise as a safe and effective
weight loss regimen. The effect of
Coleus forskohlii is particularly valid in
the absence of change in frequency and
intensity of physical exercise and without
diet restrictions during the course of the
trial. This study warrants a double-blind
clinical trial evaluating effects of forskolin
on body composition and its possible
thermogenic mechanism.
REFERENCES
1) LEAMON, KB; PADGETT, W; DALY, JW.
“Forskolin: Unique diterpene activator of
adenylate cyclase in membrane and intact cells”
Proc. Natl. Acad. Sci. USA 1981,78,
3363-67
2) DE SOUZA, NJ; DOHADWALLA, AN; REDEN,J;
Forskolin, A. “Labdane Diterpenoid with
Antihypertensive, Positive Inotropic, Platelet
Aggregation Inhibitory, and Adenylate Cyclase
Activating Properties” Medicinal Research
Reviews 1983, 3(2), 201-219
3) GIRARDIER, L. “Brown Fat: An Energy
Dissipating Tissue”; In: Mammalian
Thermogenesis; Girardier, L.; Sock M.J. Eds.;
Chapman and Hall Ltd.:London New York,
1983, pp.50-98
NUTRACEUTICALS
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Coleus (Coleus forskohlii) is a cardiovascular, respiratory, and metabolic herb. It is a plant from the mint family that grows in tropical regions. It is traditionally used in Ayurvedic medicine to treat skin rashes, asthma, bronchitis, insomnia, epilepsy, and angina pectoris. Organic extracts of coleus have demonstrated antiinflammatory, antimicrobial, antioxidant, cytotoxic, hypotensive, spasmolytic, hepatoprotective, antifeedant (preventing infestation), and antitumor properties. Clinical research indicates that coleus may be beneficial for glaucoma, asthma, congestive heart failure, obesity, subarachnoid hemorrhage, and psoriasis. This chapter examines some of the scientific research conducted on coleus, both alone and in combination formulas, for treating numerous health conditions. It summarizes results from several human studies of the herb’s use in treating ophthalmological, pulmonary, cardiovascular, cardiometabolic, neurological, and dermatological disorders. Finally, the chapter presents a list of coleus’ Active Constituents, different Commonly Used Preparations and Dosage, and a Section on “Safety and Precaution” that examines side effects, toxicity, and disease and drug interactions.
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The diterpene, forskolin [half-maximal effective concentration (EC50), 5-10 microM] activates adenylate cyclase [ATP pyrophosphate-lyase (cyclizing), EC 4.6.1.1] in rat cerebral cortical membranes in a rapid and reversible manner. Activation is not dependent on exogenous guanyl nucleotides and is not inhibited by guanosine 5'-O-(2-thiodiphosphate) when assayed with adenosine 5'-[beta, gamma-imido]triphosphate as substrate. GTP and GDP potentiate responses to forskolin. The activations of adenylate cyclase by forskolin and guanosine 5'-[beta, gamma-imido]triphosphate p[NH]ppG are not additive, whereas activations by forskolin and fluoride are additive or partially additive. The responses of adenylate cyclase to forskolin or fluoride are not inhibited by manganese ions, whereas the response to p[NH]ppG is completely blocked. Activation of adenylate cyclase by forskolin is considerably greater than the activation by fluoride in membranes from rat cerebellum, striatum, heart, and liver, while being about equal or less than the activation by fluoride in other tissues. Forskolin (EC50, 25 microM) causes a rapid and readily reversible 35-fold elevation of cyclic AMP in rat cerebral cortical slices that is not blocked by a variety of neurotransmitter antagonists. Low concentrations of forskolin (1 microM) augment the response of cyclic AMP-generating systems in brain slices to norepinephrine, isoproterenol, histamine, adenosine, prostaglandin E2, and vasoactive intestinal peptide. Forskolin would appear to activate adenylate cyclase through a unique mechanism involving both direct activation of the enzyme and facilitation or potentiation of the modulation of enzyme activity by receptors or the guanyl nucleotide-binding subunit, or both.
Brown Fat: An Energy Dissipating Tissue"; In: Mammalian Thermogenesis; Girardier, L.; Sock M
GIRARDIER, L. "Brown Fat: An Energy Dissipating Tissue"; In: Mammalian Thermogenesis; Girardier, L.; Sock M.J. Eds.; Chapman and Hall Ltd.:London New York, 1983, pp.50-98
s.), and 8 weeks 74.67 ± 11.55(n.s.). REFERENCES 1)Forskolin: Unique diterpene activator of adenylate cyclase in membrane and intact cells
  • Kb Padgett
  • W Daly
Pulse rate (beats/min) was 0 weeks 66.33 ± 8.02, 4 weeks 69.00 ± 7.97(n.s.), and 8 weeks 74.67 ± 11.55(n.s.). REFERENCES 1) LEAMON, KB; PADGETT, W; DALY, JW. "Forskolin: Unique diterpene activator of adenylate cyclase in membrane and intact cells" Proc. Natl. Acad. Sci. USA 1981,78, 3363-67