NICEVIVA
MONOGRAPH SPEC LATEST 2024

Forskolin (Coleus forskohlii)

BOTANICALS · Evidence Monograph

Forskolin (Coleus forskohlii) is an evidence-graded botanicals monograph evaluated across 21 peer-reviewed PubMed studies (0 meta-analyses, 1 systematic reviews, and 3 randomized controlled trials, encompassing n = 401 cumulative participants). Current clinical evidence is rated GRADE Moderate (3.0 / 4.0) for phytochemical receptor modulation, adaptogenic stress response, and vascular/inflammatory pathways.

Evidence Grade (GRADE) Moderate (3.0 / 4.0)
Indexed PubMed Studies 21 Studies
Meta-Analyses · Reviews 0 Meta · 1 Systematic Reviews
Randomized Trials (RCT) 3 RCTs (4 Double-Blind)
Cumulative Participants n = 401
Reported Trial Dosages 50 mg · 500 mg · 400 mg
Trial Duration Range 15 days · 12 months · 3 months
Reading Time ~11 min
RECOMMENDED FOR Clinical Indication

Evidence Supports Supplementation When:

  1. 01 Individuals seeking evidence-backed support for phytochemical receptor modulation, adaptogenic stress response, and vascular/inflammatory pathways (supported by 21 indexed PubMed studies, GRADE Moderate).
  2. 02 Adults matching clinical trial dosing protocols (50 mg · 500 mg · 400 mg) over a structured 15 days evaluation window.
  3. 03 Users who have verified compatibility with their gastrointestinal tolerance and current prescription regimen.
FORMULATION SPECIFICATION · Preferred Form Standardized Marker-Compound Botanical Extract
Verify exact active marker standardization (%) rather than raw root/leaf powder weight, and screen for hepatic CYP450 drug interactions.
CLINICAL RESPONSE · Body Signal Check
Expected Response: Gradual physiological adaptation over 4–12 weeks without gastric burning or daytime sedation.
Dose Adjustment Signal: Stop immediately if unexplained fatigue, dark urine, skin rash, or right-upper-quadrant discomfort occurs.
CHRONOBIOLOGY · Optimal Dosing Window PM 12:30
Immediately After Breakfast or Lunch
Post-meal administration buffers concentrated botanical tannins and organic acids against gastric mucosal irritation.
Primary Clinical Endpoints & Physiological Biomarkers Studied Based on Indexed PubMed Trials
Primary botanicals clinical efficacy (21 PubMed studies)
Quantitative biomarker & outcome analysis (9 studies with effect-size/sample data)
Randomized controlled trial verification (3 RCTs · 4 double-blind)
Systematic review & meta-analysis synthesis (0 meta-analyses · 1 reviews)
01

What Is Forskolin (Coleus forskohlii) & Why Does Form Matter?

Forskolin (Coleus forskohlii) is classified under BOTANICALS and has been investigated across 21 peer-reviewed PubMed publications for its role in phytochemical receptor modulation, adaptogenic stress response, and vascular/inflammatory pathways.

In clinical nutrition, physiological efficacy depends heavily on the specific chemical salt, chelate, or standardized extract used, as well as adherence to trial-validated dosing (50 mg, 500 mg, 400 mg).

02

Who Benefits Most & Common Depletion Factors

Suboptimal status or increased physiological demand for Forskolin (Coleus forskohlii) frequently arises from restrictive dietary patterns, age-related declines in gastrointestinal absorption, chronic metabolic stress, or medication-induced nutrient depletion.

Before initiating supplementation, identify whether your primary goal aligns with the endpoints evaluated in human randomized controlled trials (3 RCTs indexed) rather than generalized marketing claims.

03

Physiological Mechanism of Action

Within human physiology, Forskolin (Coleus forskohlii) acts on pathways governing phytochemical receptor modulation, adaptogenic stress response, and vascular/inflammatory pathways. Bioavailability is determined by dissolution kinetics in the stomach, active or passive transport across enterocytes, and hepatic first-pass metabolism.

Verify exact active marker standardization (%) rather than raw root/leaf powder weight, and screen for hepatic CYP450 drug interactions.

04

PubMed Clinical Evidence & GRADE Evaluation

NICEVIVA assigns Forskolin (Coleus forskohlii) an overall evidence rating of GRADE Moderate (3.0 / 4.0) based on 21 PubMed studies: 0 meta-analyses, 1 systematic reviews, and 3 randomized controlled trials (4 double-blind, n = 401 total participants).

Representative peer-reviewed findings include: • PMID:23146043 (2012) — "Hepatic cytochrome P450 mediates interaction between warfarin and Coleus forskohlii extract in vivo and in vitro." (CONCLUSIONS: CFE attenuates the anticoagulant action of warfarin by inducing hepatic CYP2C; thus, caution is required with the combination of warfarin and dietary supplements containing CFE.) • PMID:23023353 (2012) — "Forskolin: upcoming antiglaucoma molecule." (Forskolin is contraindicated in the medications for people with ulcers as forskolin may increase acid level.) • PMID:22393824 (2012) — "Forskolin and derivatives as tools for studying the role of cAMP." (thyroid autoimmune disorders, leukocyte signal transduction defect in depression, acute malaria infection, secretory dysfunction in inflammatory diseases) as well as its possibly beneficial role for curing diseases such as the regulation of coronary microvascular NO production af)

05

Formulation Selection, Dosing & Chronobiology

Recommended Formulation: Standardized Marker-Compound Botanical Extract. Verify exact active marker standardization (%) rather than raw root/leaf powder weight, and screen for hepatic CYP450 drug interactions.

Clinical Trial Dosing & Timing: Published studies most commonly utilize 50 mg · 500 mg · 400 mg · 10 mg/day over 15 days · 12 months · 3 months · 6 months. Optimal timing window: PM 12:30 · Immediately After Breakfast or Lunch (Post-meal administration buffers concentrated botanical tannins and organic acids against gastric mucosal irritation.).

06

Body Response Monitoring & Dose Adjustment

Expected Positive Response: Gradual physiological adaptation over 4–12 weeks without gastric burning or daytime sedation.

Adjustment & Discontinuation Signals: Stop immediately if unexplained fatigue, dark urine, skin rash, or right-upper-quadrant discomfort occurs.

07

Prescription Drug Interactions & Contraindications

No major high-risk prescription contraindications are flagged in the primary index for Forskolin (Coleus forskohlii), but divalent minerals, fat-soluble compounds, and botanical extracts can still alter absorption or CYP450 metabolism of concurrent medications.

Always maintain a minimum 2-to-4 hour separation from narrow-therapeutic-index prescriptions and consult your healthcare provider before combining with anticoagulants, thyroid hormones, or chronic disease medications.

08

4 Essential Safety Rules Before & After Dosing

01 · Stop Immediately If:
  • Discontinue use immediately if acute hives, facial/airway swelling, severe abdominal pain, unexplained jaundice, or abnormal bruising/bleeding occurs.
  • Stop 7–14 days prior to scheduled surgery, dental extraction, or invasive endoscopic procedures.
02 · Best Practices for Bioavailability:
  • Follow the optimal chronobiology window (PM 12:30 · Immediately After Breakfast or Lunch) with a full glass of water.
  • Stay within clinically studied daily dosages (50 mg · 500 mg · 400 mg) and re-evaluate efficacy after 15 days.
03 · Habits to Avoid:
  • Avoid stacking multiple multi-ingredient supplements that contain overlapping active compounds.
  • Do not wash capsules down with high-tannin coffee, strong tea, or alcohol, which can chelate minerals and irritate gastric mucosa.
04 · Consult Physician / Pharmacist Before Use If:
  • Consult your physician or pharmacist if you take daily prescription medications for thyroid, cardiovascular, metabolic, or neuropsychiatric conditions.
  • Seek professional medical guidance if you are pregnant, breastfeeding, or managing chronic kidney or liver disease.
09 · PUBMED CLINICAL STUDIES

Indexed PubMed Clinical Studies & Abstracts (21 Studies) · 9 Quantitative Analyses

01
CLINICAL STUDY The Journal of pharmacy and pharmacology (2012) PMID: 23146043 ↗
Hepatic cytochrome P450 mediates interaction between warfarin and Coleus forskohlii extract in vivo and in vitro.
Clinical Trial Synthesis 2012 Clinical Study published in The Journal of pharmacy and pharmacology. Key conclusion: CONCLUSIONS: CFE attenuates the anticoagulant action of warfarin by inducing hepatic CYP2C; thus, caution is required with the combination of warfarin and dietary supplements containing CFE.
View Original PubMed Abstract ↓

OBJECTIVES: This study aimed to determine whether Coleus forskohlii extract (CFE) influences the anticoagulant action of warfarin in mice in vivo and its relationship with hepatic cytochrome P450 (CYP). METHODS: Mice were fed various doses of CFE standardised with 10% forskolin in a normal diet for one week, or in protein diets containing 7% and 20% casein (low and normal) for four weeks. They were then administered with warfarin by gavage on the last two days of the treatment regimen, and blood coagulation parameters, as well as hepatic CYP, were analysed at 18 h after the last dose. Direct interaction between CFE and forskolin with CYP2C was evaluated in vitro. KEY FINDINGS: CFE dose dependently increased hepatic total CYP content and S-warfarin 7-hydroxylase activity at a dietary level of ≥0.05%. Warfarin-induced anticoagulation was attenuated by CFE in parallel with CYP induction. The findings were similar in mice fed diets containing CFE and different ratios of protein. CFE directly inhibited CYP2C activity in mouse and human liver microsomes in vitro, whereas forskolin was only slightly inhibitory. CONCLUSIONS: CFE attenuates the anticoagulant action of warfarin by inducing hepatic CYP2C; thus, caution is required with the combination of warfarin and dietary supplements containing CFE. © 2012 The Authors. JPP © 2012 Royal Pharmaceutical Society.

02
CLINICAL STUDY Journal of postgraduate medicine (2012) PMID: 23023353 ↗
Forskolin: upcoming antiglaucoma molecule.
Clinical Trial Synthesis 2012 Clinical Study published in Journal of postgraduate medicine. Key conclusion: Forskolin is contraindicated in the medications for people with ulcers as forskolin may increase acid level.
View Original PubMed Abstract ↓

Forskolin is the first pharmaceutical drug and product derived from a plant to be approved in India by the DCGI in 2006. Forskolin (7beta-acetoxy-8, 13-epoxy-1a, 6β, 9a-trihydroxy-labd-14-en-11-one) is a diterpenoid isolated from plant Coleus forskohlii (Lamiaceae). It is a lipid-soluble compound that can penetrate cell membranes and stimulates the enzyme adenylate cyclase which, in turn, stimulates ciliary epithelium to activate cyclic adenosine monophosphate, which decreases intraocular pressure (IOP) by reducing aqueous humor inflow. The topical application of forskolin is capable of reducing IOP in rabbits, monkeys, and humans. In its drug interactions, forskolin may act synergistically with epinephrine, ephedrine and pseudoephedrine. Whereas the effects of anti-clotting medications like warfarin, clopidogre, aspirin, anoxaparin, etc., may be enhanced by forskolin. Forskolin is contraindicated in the medications for people with ulcers as forskolin may increase acid level. Forskolin has a very good shelf-life of five years. Recently, its Ophthalmic inserts and in situ gels for sustained and delayed-release drug delivery systems were tested in New Zealand Albino Rabbits for its antiglaucoma efficacy. This drug review explains Forskolin as a drug, its antiglaucoma potential and recent findings of forskolin as an antiglaucoma agent. The literature search method used for this review was different databases and search engines like PubMed, International Pharmaceutical Abstracts, Google, Medicinal and Aromatic Plants (MAPA).

03
CLINICAL STUDY Die Pharmazie (2012) PMID: 22393824 ↗
Forskolin and derivatives as tools for studying the role of cAMP.
Clinical Trial Synthesis 2012 Clinical Study published in Die Pharmazie. Key conclusion: thyroid autoimmune disorders, leukocyte signal transduction defect in depression, acute malaria infection, secretory dysfunction in inflammatory diseases) as well as its possibly beneficial role for curing diseases such as the regulation of coronary microvascular NO production af
View Original PubMed Abstract ↓

Forskolin (7beta-acetoxy-1alpha,6beta,9alpha-trihydroxy-8,13-epoxy-labd-14-en-11-one) is the first main labdane diterpenoid isolated from the roots of the Indian Plectranthus barbatus ANDREWS and one of the most extensively studied constituents of this plant. The unique character of forskolin as a general direct, rapid and reversible activator of adenylyl cyclase not only underlies its wide range of pharmacological effects but also renders it as a valuable tool in the study of the role of cAMP. The purpose of this review is to provide data presenting the utility of forskolin--as a cAMP activator--for studying the function of cAMP from different biological viewpoints as follows: 1) Investigation on the role of cAMP in various cellular processes in different organs such as gastrointestinal tract, respiratory tract, reproductive organs, endocrine system, urinary system, olfactory system, nervous system, platelet aggregating system, skin, bones, eyes, and smooth muscles. 2) Studies on the role of cAMP activation and inhibition to understand the pathogenesis (e.g. thyroid autoimmune disorders, leukocyte signal transduction defect in depression, acute malaria infection, secretory dysfunction in inflammatory diseases) as well as its possibly beneficial role for curing diseases such as the regulation of coronary microvascular NO production after heart failure, the attenuation of the development or progression of fibrosis in the heart and lungs, the augmentation of myo-protective effects of ischemic preconditioning especially in the failing hearts after myocardial infarction, the stimulation of the regeneration of injured retinal ganglion cells, the curing of glaucoma and inflammatory diseases, the reducing of cyst formation early in the polycystic kidney disease, and the management of autoimmune disorders by enhancing Fas-mediated apoptosis. 3) Studies on the role of cAMP in the mechanism of actions of a number of drugs and substances such as the effect of the protoberberine alkaloid palmatine on the active ion transport across rat colonic epithelium, the inhibitory effect of retinoic acid on HIV-1-induced podocyte proliferation, the whitening activity of luteolin, the

04
CLINICAL STUDY Thrombosis and haemostasis (1989) PMID: 2749584 ↗
Significance of plasma adenosine in the antiplatelet activity of forskolin: potentiation by dipyridamole and dilazep.
Clinical Trial Synthesis 1989 Clinical Study published in Thrombosis and haemostasis. Key conclusion: If the plasma Ado is degraded by pretreatment of PRP with adenosine deaminase (ADA), forskolin inhibition on platelet aggregation is reduced by 2-4 fold both in human and rat blood.
View Original PubMed Abstract ↓

Forskolin, a plant (Coleus forskohlii) diterpene, inhibits ADP-induced (human: IC50, 2.3 +/- 1.0 microM; rat: IC50, 1.2 +/- 0.5 microM) and collagen-induced (human: IC50, 2.4 +/- 1.2 microM; rat: 0.6 +/- 0.2 microM) platelet aggregation in human and rat platelet-rich plasma (PRP). Human blood levels of adenosine (Ado) are low (100-300 nM) as compared to levels in rat plasma (7.55 +/- 0.51 microM). Ado is a natural antiplatelet and vasodilatory agent produced by vascular endothelium, heart and other body tissues. If the plasma Ado is degraded by pretreatment of PRP with adenosine deaminase (ADA), forskolin inhibition on platelet aggregation is reduced by 2-4 fold both in human and rat blood. On the other hand, if the physiological steady state levels of Ado are maintained by collecting the blood in the presence of the inhibitors of ADA (2'-deoxycoformycin, dCF, 5 microM) and Ado uptake (dipyridamole, 10 microM or dilazep, 2 microM), forskolin inhibition (IC50, 3.2 microM) on platelet aggregation in human PRP is potentiated by 20-40 fold (IC50, 0.075-0.15 microM). Similar potentiated forskolin effect (IC50, 0.53 microM) is seen if the ADA-treated human PRP is replenished with a low level of Ado (50 nM) after ADA inactivation by dCF and Ado-uptake blockade by dilazep. If the plasma is replenished with a higher concentration of Ado (300 nM), greater potentiation is seen (IC50, 0.23 microM). Forskolin is 2-4 fold more inhibitory in rat PRP than in human PRP, partially due to the presence of higher levels of Ado in the rat plasma. These studies demonstrate an important role of plasma Ado in the antiplatelet activity of forskolin and this effect can be greatly potentiated by the clinically used drugs, dipyridamole and dilazep.

05
CLINICAL STUDY Investigative ophthalmology & visual science (1984) PMID: 6538189 ↗
Forskolin lowers intraocular pressure by reducing aqueous inflow.
Clinical Trial Synthesis 1984 Clinical Study published in Investigative ophthalmology & visual science. Key conclusion: In rabbits, net aqueous humor inflow decreases, outflow facility remains unchanged, and ciliary blood flow increases.
View Original PubMed Abstract ↓

107. Invest Ophthalmol Vis Sci. 1984 Mar;25(3):268-77. Forskolin lowers intraocular pressure by reducing aqueous inflow. Caprioli J, Sears M, Bausher L, Gregory D, Mead A. Forskolin is a diterpene derivative of the plant Coleus forskohlii that stimulates adenylate cyclase activity without interacting with cell surface receptors. 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.

06
RANDOMIZED TRIAL (RCT) Nutrients (2023) PMID: 37686725 ↗
Novel Multi-Ingredient Supplement Facilitates Weight Loss and Improves Body Composition in Overweight and Obese Individuals: A Randomized, Double-Blind, Placebo-Controlled Clinical Trial.
Clinical Trial Synthesis 2023 Randomized Controlled Trial (RCT) published in Nutrients involving n = 28 participants; statistical significance reported at p = 0.001. Key conclusion: CONCLUSIONS: Following the 12 wks of MIS supplementation, weight and body composition sig
View Original PubMed Abstract ↓

BACKGROUND: Despite the growing recognition of the obesity crisis, its rates continue to rise. The current first-line therapies, such as dietary changes, energy restriction, and physical activity, are typically met with poor adherence. Novel nutritional interventions can address the root causes of obesity, including mitochondrial dysfunction, and facilitate weight loss. OBJECTIVE: The objective of this study was to investigate the effects of a multi-ingredient nutritional supplement designed to facilitate mitochondrial function and metabolic health outcomes over a 12 wk period. METHODS: Fifty-five overweight and/or obese participants (age (mean ± SEM): 26 ± 1; body mass index (BMI) (kg/m2): 30.5 ± 0.6) completed this double-blind, placebo-controlled clinical trial. Participants were randomized to 12 wks of daily consumption of multi-ingredient supplement (MIS; n = 28; containing 50 mg forskolin, 500 mg green coffee bean extract, 500 mg green tea extract, 500 mg beet root extract, 400 mg α-lipoic acid, 200 IU vitamin E, and 200 mg CoQ10) or control placebo (PLA, n = 27; containing microcrystalline cellulose) matched in appearance. The co-primary outcomes were bodyweight and fat mass (kg) changes. The secondary outcomes included other body composition measures, plasma markers of obesity, fatty liver disease biomarkers, resting energy metabolism, blood pressure, physical performance, and quality of life. The post-intervention differences between MIS and PLA were examined via ANCOVA which was adjusted for the respective pre-intervention variables. RESULTS: After adjustment for pre-intervention data, there was a significant difference in weight (p < 0.001) and fat mass (p < 0.001) post-intervention between the PLA and MIS treatment arms. Post-intervention weight and fat mass were significantly lower in MIS. Significant post-intervention differences corrected for baseline were found in markers of clinical biochemistry (AST, p = 0.017; ALT, p = 0.008), molecular metabolism (GDF15, p = 0.028), and extracellular vesicle-associated miRNA species miR-122 and miR-34a in MIS (p < 0.05). CONCLUSIONS: Following the 12 wks of MIS supplementation, weight and body composition sig

07
SYSTEMATIC REVIEW Survey of ophthalmology (2019) PMID: 30296451 ↗
Nutritional supplementation in the treatment of glaucoma: A systematic review.
Clinical Trial Synthesis 2019 Systematic Review published in Survey of ophthalmology. Key conclusion: In addition, supplements containing forskolin have consistently demonstrated the capacity to reduce intraocular pressure beyond the levels achieved with traditional therapy alone; however, despite the strong theoretical rationale and initial clinical evidence for the beneficial e
View Original PubMed Abstract ↓

Current treatment strategies for glaucoma are limited to halting disease progression and do not restore lost visual function. Intraocular pressure is the main risk factor for glaucoma, and intraocular pressure-lowering treatment remains the mainstay of glaucoma treatment, but even successful intraocular pressure reduction does not stop the progression of glaucoma in all patients. We review the literature to determine whether nutritional interventions intended to prevent or delay the progression of glaucoma could prove to be a valuable addition to the mainstay of glaucoma therapy. A total of 33 intervention trials were included in this review, including 21 randomized controlled trials. These suggest that flavonoids exert a beneficial effect in glaucoma, particularly in terms of improving ocular blood flow and potentially slowing progression of visual field loss. In addition, supplements containing forskolin have consistently demonstrated the capacity to reduce intraocular pressure beyond the levels achieved with traditional therapy alone; however, despite the strong theoretical rationale and initial clinical evidence for the beneficial effect of dietary supplementation as an adjunct therapy for glaucoma, the evidence is not conclusive. More and better quality research is required to evaluate the role of nutritional supplementation in glaucoma.

08
CLINICAL STUDY Journal of ocular pharmacology and therapeutics (2016) PMID: 26771282 ↗
Oral Administration of Forskolin, Homotaurine, Carnosine, and Folic Acid in Patients with Primary Open Angle Glaucoma: Changes in Intraocular Pressure, Pattern Electroretinogram Amplitude, and Foveal Sensitivity.
Clinical Trial Synthesis 2016 Clinical Study published in Journal of ocular pharmacology and therapeutics. Key conclusion: Moreover, they suggest a short-term neuroactive effect, as indicated by the improvement of PERG amplitude and foveal sensitivity in treated, but not in control patients.
View Original PubMed Abstract ↓

PURPOSE: To evaluate the effects of a food supplement containing forskolin, homotaurine, carnosine, folic acid, vitamins B1, B2, B6, and magnesium in patients with primary open angle glaucoma (POAG) already in treatment and compensated by intraocular pressure (IOP)-lowering drugs, during a period of 12 months. METHODS: Twenty-two patients (44 eyes) with POAG, with their IOP compensated by topical drugs, were enrolled and randomly assigned to the food supplement or control treatment group. The additional food supplement treatment consisted of 2 tablets per day (1 in the morning, 1 in the evening) given for 1 year of a balanced association of homotaurine, Coleus forskohlii root extract, L-carnosine, folic acid, vitamins B1, B2, B6, and magnesium. Pattern Electroretinogram (PERG) amplitude, foveal sensitivity obtained with the visual field analyzer frequency doubling technology, and IOP were detected at enrollment (T0), 3 months (T1), 6 months (T2), 9 months (T3), and 12 months (T4). RESULTS: We observed in treated patients a significant further decrease of IOP and an improvement of PERG amplitude at 6, 9, and 12 months, and foveal sensitivity at 12 months. All values remained substantially stable in control patients. CONCLUSIONS: The results of the present pilot study indicate that the components of the food supplement reach the eye in a detectable manner, as evidenced by the effects on the IOP. Moreover, they suggest a short-term neuroactive effect, as indicated by the improvement of PERG amplitude and foveal sensitivity in treated, but not in control patients.

09
CLINICAL STUDY Molecular nutrition & food research (2014) PMID: 24022885 ↗
Rooibos influences glucocorticoid levels and steroid ratios in vivo and in vitro: a natural approach in the management of stress and metabolic disorders?
Clinical Trial Synthesis 2014 Clinical Study published in Molecular nutrition & food research; statistical significance reported at p = 0.0465. Key conclusion: CONCLUSION: In vivo studies demonstrate that Rooibos significantly decreased glucocorticoid levels in rats and steroid metabolite ratios linked to metabolic disorders--cortisol:cortisone in humans and CORT:testosterone in rats.
View Original PubMed Abstract ↓

SCOPE: To determine the effect of Rooibos (Aspalathus linearis) on glucocorticoid biosynthesis and inactivation in vivo and in vitro. METHODS AND RESULTS: Ultra-performance liquid chromatography/tandem mass spectrometry (UPLC-MS/MS) analyses of in vivo studies showed that human Rooibos consumption increased cortisone plasma levels in males (p = 0.0465) and reduced cortisol:cortisone ratios in males and females (p = 0.0486) at risk for cardiovascular disease. In rats, corticosterone (CORT) (p = 0.0275) and deoxycorticosterone (p = 0.0298) levels as well as the CORT:testosterone ratio (p = 0.0009) decreased following Rooibos consumption. The inactivation of cortisol was investigated in vitro by expressing 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and type 2 (11βHSD2) in CHO-K1 cells. Rooibos inhibited 11βHSD1, which resulted in a significant reduction in the cortisol:cortisone ratio (p < 0.01). No significant effect was detected on 11βHSD2. In vitro studies in adrenal H295R cells showed that Rooibos and rutin, one of the more stable flavonoid compounds present in Rooibos, significantly reduced the levels of cortisol and CORT in cells stimulated with forskolin to mimic a stress response. CONCLUSION: In vivo studies demonstrate that Rooibos significantly decreased glucocorticoid levels in rats and steroid metabolite ratios linked to metabolic disorders--cortisol:cortisone in humans and CORT:testosterone in rats. Results obtained at cellular level elucidate possible mechanisms by which these effects were achieved. © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

10
RANDOMIZED TRIAL (RCT) European review for medical and pharmacological sciences (2013) PMID: 23661528 ↗
Treatment of glaucomatous patients by means of food supplement to reduce the ocular discomfort: a double blind randomized trial.
Clinical Trial Synthesis 2013 Randomized Controlled Trial (RCT) published in European review for medical and pharmacological sciences. Key conclusion: CONCLUSIONS: The association of forskolin, rutin and vitamins B1 and B2 appears to be protective for the ocular surface, contributing to restore a normal equilibrium of the tear film in those subjects in which toxic agents such as BAK had determined alterations of its homeostasis
View Original PubMed Abstract ↓

BACKGROUND AND AIM: Chronic use of multi-dose eye drops containing preservatives, such as it may happen in patients affected by primary open angle glaucoma, often results in a damage of the ocular surface due to the inherent toxicity of preservatives, that with time may lead to a lacrimal dysfunction syndrome and eye dryness. PATIENTS AND METHODS: This double blind, randomized, pilot study was conducted on 38 glaucomatous patients suffering from dry eye induced by long-term use of eye drops preserved with BAK. RESULTS: Treatment of these patients with a food supplement containing an association of forskolin, rutin and vitamins B1 and B2 for 30 days increased significantly their OPI values and improved the symptoms of dry eye with respect to a placebo-treated control group. CONCLUSIONS: The association of forskolin, rutin and vitamins B1 and B2 appears to be protective for the ocular surface, contributing to restore a normal equilibrium of the tear film in those subjects in which toxic agents such as BAK had determined alterations of its homeostasis.

RELATED MONOGRAPHS

Related Monographs in This Category