Artichoke Extract and Forskolin

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Artichoke Extract and Forskolin

Boost Energy
Cognitive
Improve Focus
Improve Memory
Longevity
Mental Health
Nootropics
Mood Support

Description

Summary

Forskolin, which is the active ingredient found from the roots and stems of Coleus forskohlii [1] has been widely used in many studies; particularly in its role in lean body mass [2]. In addition, forskolin has been attributed to treating heart diseases, glaucoma, asthma and some cancers [1]. Other reports have suggested forskolin can treat cardiovascular disorders and even lower blood pressure [3].

Mechanisms of action 

Forskolin works induces the enzyme adenylate cyclase, along with marked increases in cyclic adenosine monophosphate (cAMP) concentrations [3; 4]. cAMP is an extremely important signal necessary for the proper response of cells to other molecules such as hormones [5]. Downstream effects of an increased cAMP concentration in cells involve a broad range of biochemical and physiological outcomes. What forskolin does is re-sensitize cell receptors via the activation of adenylyl cyclase, increasing intracellular cAMP levels [5]. Adding to this, cAMP is suggested to be involved in the regulation of memory; with forskolin even be considered as a good candidate for Alzheimer’s Disease (AD) [6].

Figure 1. Forskolin acts on increasing cAMP, an important secondary messenger that cells use for transferring the signalling the effects of hormones into cells. Inflammation and inflammatory diseases is triggered through the nuclear factor (NF-kB) pathway. Forskolin may indirectly impact this pathway and its signalling [7]. Image Source: [8].

Structure and function  

Forskolin is a labdane diterpene which these types of diterpenes make up a class of natural products, all with a unique biological activity that works to provide algal, bacterial, fungal, anti-inflammatory, modulating immune cell functions and anti-tumour functioning [5; 9]. Forskolin cAMP production is linked to PDE4. PDE4 inhibitors increase the levels of cAMP, exhibiting anti-inflammatory effects [32]. Selective inhibitors of PDE4 have been reported as important in controlling depression and cognitive function [33]. The expression of PDEs (phosphodiesterases) play a role in regulating cAMP-mediated signalling [34].

 

Figure 2. Coleus forskohii is found in India and Thailand, and is a member of the mint family [10]. It is considered an active secondary metabolite since it can activate the enzyme adenylate cyclase [10]. Its classification is that of ditepene (left) which switches on a cascade of cAMP that stimulates a range of beneficial effects [11]. Image source: [11].

Benefits and Effects

Along with its ability to treat cardiovascular disorders and blood pressure [3], forskolin can also be used for health benefits to those suffering from hypertension, asthma, and Alzheimer’s Disease [12]. What’s more, forskolin can treat mood disorders, promote lean body mass, along with possessing anti-cancer properties [12]. Recently, a pure forskolin has been shown to exhibit neuroprotective and positive behavioural effects in mice with cerebral amyloidosis [6]. This pure forskolin treatment was orally given to mice over 10 days [6]. Forskolin also possess the ability to kill multiple myeloma (MM) cells in vitro and in vivo [13]. Multiple myeloma (MM) cells is considered a cell malignancy, which is characterised by the presence of malignant cells in the bone marrow – leading to bone pain, fractures and infections [13].

Forskolin and hair loss

Forskolin induces the production of cAMP [3], and this promotion of cAMP has been investigated as an activator of hair follicle activity [14], in the context of age-related hair loss. Additonally, forskolin has been suggested to be used in conjunction with other medicines to prevent hair greying, to the restoration of normal hair colour [15].

Forskolin and asthma

In a single-blind clinical study evaluating the efficacy of forskolin on preventing asthma attacks [16], a 10mg capsule forskolin dose, delivered orally over 6 months showed effectiveness in preventing asthma attacks [16].

Forskolin and weight loss

The ability of forskolin to increase intracellular levels of cAMP leads to the stimulation of lipolysis, which promotes the breakdown of stored fats [17]. Moreover, cAMP increases the use of stored body fat; along with increases metabolic rate and regulating the body’s temperatures in response to food [18; 19]. Obese individuals have lower cAMP production, so, theoretically, forskolin could be trigger weight loss [15]. Forskolin induces weight loss and fat loss through its interaction with producing lipolysis [17; 20]. A 250mg dose of forskolin extract was shown to induce weight loss – fat percentage and mass – over a 12-week period in obese males [17]. Other work has suggested that forskolin does not promote weight loss; however, in fact mitigates weight gain in overweight women with no clinical side effects [20]. This work used a forskolin extract dose of 500mg per day over 12 weeks [21]. Pure forskolin extract – fed to male mice for 2-3 weeks – showed little increase in relative liver weight; along with increasing hepatic cytochrome P450 and glutathione S-transferase activity [17]. It has been suggested that differences in response to forskolin extract in men and women requires further investigation [21]. It is currently unclear whether forskolin works for weight loss.

Forskolin Vs Garcinia cambogia

In a study evaluating the efficacy of Garcinia cambogia in body weight and fat mass loss in obese humans, results showed that G. cambogia failed to produce significant weight loss compared to the placebo control [22]. This study involved 135 subjects, in which a 1500mg dose of hydroxycitric acid – the active herbal compound – was administered over a 12-wek period [22]. In comparison, a double-blind placebo-controlled clinical trial showed that a 10% forskolin extract – given to 15 obese men at 500mg per day – significantly decreased their body fat and increased lean body mass [21]. Another study assessing garcinia cambogia’ effects on body weight and weight loss failed to produce any significant results [23]. Overall, there have been inconsistent results from the assessment of garcinia cambogia and weight loss [21]. In particular, experiments have found the active ingredient of G. cambogia, hydroxycitric acid, to elicit adverse effects such as hepatotoxicity. There is still little evidence to conclude a long-term benefit of taking G. cambogia, and its role in weight loss [21].

Forskolin in depressed patients

In a study that aimed to determine the before and after effects of forskolin in depressed and schizophrenic patients, forskolin – administered intravenously at a dose between 0.5 – 2 micrograms per kg – results demonstrated that forskolin had a positive impact [24]. Interestingly, some patients showed improvement in mood anxiety, fatigue and confusion, after forskolin had been given. Other work has documented forskolin’s antidepressant activity in a forced swimming test in mice [6].

Forskolin extract 

Forskolin is generally extracted using a range of organic solvents and purified using a series of separation techniques [15]. One particular study used an extract of forskolin to assess the skin diffusion properties of forskolin [25]. These results found that the forskolin extract could be effectively delivered through the outermost layer of the skin [25]. Forskolin extraction from the Coleus roots involves extraction using alcohol and a range of different solvents followed by the use of laboratory-based chromatography equipment [26].

Forskolin and testosterone

In the investigation of how forskolin might impact testosterone and other physiological parameters in obese men results found that a 250mg forskolin extract raised serum free testosterone levels [27]. One particular research looking to assess the effects of forskolin on a steroid-producing cell line found that a low dose of forskolin could induce higher hormone production [28]. In addition, forskolin was able to increase gene expression in this cell line, and induce steroidogenesis [28]. The importance of having steroid-producing machinery within a cell is crucial for the synthesis of testosterone [29]. An increase in steroidogenesis indicates the presence of the required machinery necessary to producing testosterone.

Dosage 

Forskolin has been documented as being well tolerated at doses of 50-100mg/kg body weight [3]. Other academic sources report that oral administration of 50mg per day does not produce significant side effects in patients [13].

Side effects and safety

Side effects and dangers associated with forskolin have yet to be fully evaluated [15]. In addition, a safe forskolin dose has yet to be determined; however, no adverse effects from been reported from its use [10]. Forskolin’s safety has also been assessed in a 3-month topical, cream, treatment in animals [Spry et al., 2008]. Researchers of this study found that forskolin topically administered to animal skin in a low dose caused no toxic reactions [30]. Other cosmetically relevant applications of forskolin-based cream are, apparently, currently in laboratory testing stages [15]. Clinical trials that investigate the effectiveness of forskolin as a therapy is currently limited [31]. Although forskolin might be considered safe, there is potential for herb-drug interactions in patients who might be on combination therapy [31].

Stacks

Forskolin and artichoke extract

Artichoke leaf extract (ALE) has been noted as being able to increase bile flow, exert hepatoprotective and antioxidant effects [35]. Artichoke (Cynara scolymus) showed significant inhibition activity on PDE activity [34]. The weight loss potential of artichoke is initiated via the constituent cynarin (artichoke extract) has been investigated through the assessment of artichoke on non-alcoholic fatty acid liver disease (NAFLD) [37]. 60 patients suffering a form of NAFLD, after given a 2700mg artichoke extract showed improvement in liver enzymes [37].

The stacking of artichoke with forskolin has gained recent attention. Although scientific literature has not confirmed the safety profile, dosing or side effects of stacking artichoke with forskolin, reviews have spoken of the CILTEP stack – a stack used to improve mental performance and induce Long-term potentiation (LTP). Long-term potentiation is important in the formation and retrieval of some forms of memory [36]; the long-lasting increase in strengthening synapses [36].

 

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[1] Gracy L. SAILO and Davis J. BAGYARAJ, 2005. Influence of different AM-fungi on the growth, nutrition and forskolin content of Coleus forskohlii. The British Mycological Society, 7: 795-798.

[2] A.M. Saleem, P.B. Dhasan, M.R.M. Rafiullah, 2006. Simple and rapid method for the isolation of forskolin from Coleus forskohlii by charcoal column chromatography. Journal of Chromatography, 313-314.

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[3] Khalid Pasha Mohammed, Archana Aarey, Shayesta Tamkeen, Parveen Jahan, 2015. Forskolin: Genotoxicity assessment in Allium cepa. Mutation Research/Genetic Toxicology and Environmental Mutagenesis, 777: 29-32.

[4] Irini Pateraki, Johan Andersen-Ranberg, Britta Hamberger, Allison Maree Heskes, Helle Juel Martens, Philipp Zerbe, Søren Spanner Bach, Birger Lindberg Møller, Jörg Bohlmann, and Björn Hamberger, 2014.

Manoyl Oxide (13R), the Biosynthetic Precursor of Forskolin, Is Synthesized in Specialized Root Cork Cells in Coleus forskohlii. Plant Physiology, 164: 1222-1236.

[5] Srinivasa Rao Vattikonda, Nageswara Rao Amanchi and Sabita Raja S. 2014. Antifeedant activity of forskolin, an extract of Coleus forskohlii, against Papilio demoleus L. (Lepidoptera: Papilionidae) larvae. Pelaiga Research Library, 4:1, 237-241.

[6] Brice Ayissi Owona, PhD, Caroline Zug, MSc, Hermann J. Schluesener, PhD, MD, and Zhi-Yuan Zhang, PhD, 2016. Protective Effects of Forskolin on Behavioral Deficits and Neuropathological Changes in a Mouse Model of Cerebral Amyloidosis. Journal of Neuropathology and Experimental Neurology, 75:7.

[7] A. Salminen, M. Lehtonen, T. Suuronen, K. Kaarniranta and J. Huuskonen, 2008. Terpenoids: natural inhibitors of NF-kB signaling with anti-inflammatory and anticancer potential. Cellular and Molecular Life Sciences, 65: 2979-2999.

[8] M. B. Patel, 2010. Forskolin: A Successful Therapeutic Phytomolecule. East and Central African Journal of Pharmaceutical Sciences, 13: 25-32.

[9] Sharad Kumar Srivastava, Manjoosha Chaubey, S. Khatoon, A.K.S. Rawat and Shanta Mehrotra, 2002. Pharmacognostic Evaluation of Coleus forskohlii. Pharmaceutical Biology, 40:2, 129-134.

[10] BRIAN T. SCHANEBERG and IKHLAS A. Khan, 2003. Quantitative Analysis of Forskolin in Coleus forskohlii (Lamiaceae) by Reversed-Phase Liquid Chromatography. Dietary supplements, 86:3.

[11] LUIGI SAPIO, MONICA GALLO, MICHELA ILLIANO, EMILIO CHIOSI, DANIELE NAVIGLIO, ANNAMARIA SPINA, AND SILVIO NAVIGLIo, 2016. The Natural cAMP Elevating Compound Forskolin in Cancer Therapy: Is It Time? Journal of Cellular Physiology. DOI: 10.1002/jcp.25650.

[12] Shirish M. Harde, Rekha S. Singhal, 2012. Extraction of forskolin from Coleus forskohlii roots using three phase partitioning. Separation and Purification Technology, 96: 20-25.

[13] Virginie Follin-Arbelet, Kristine Misund, Elin Hallan Naderi, Hege Ugland, Anders Sundan & Heidi Kiil Blomhoff, 2015. The natural compound forskolin synergizes with dexamethasone to induce cell death in myeloma cells via BIM. Scientific Reports, 5:13001.

[14] Alexandra Amaro-Ortiz, Betty Yan and John A. D’Orazio, 2014. Ultraviolet Radiation, Aging and the Skin: Prevention of Damage by Topical cAMP Manipulation. Molecules, 19.

[15] CARMEN CIOTONEA and CORINA CERNĂTESCU, 2010. BIOLOGICAL ACTIVE EFFECTS OF FORSKOLIN EXTRACT.

[16] R GONZÁLEZ-SÁNCHEZ1, X TRUJILLO2, B TRUJILLO-HERNÁNDEZ3, C VÁSQUEZ2, M HUERTA2 AND A ELIZALDE, 2006. Forskolin versus Sodium Cromoglycate for Prevention of Asthma Attacks: a Single-blinded Clinical Trial. The Journal of International Medical Research, 34: 200-207.

[17] N. Virgona, Y. Taki, K. Umegaki, 2009. A rapid HPLC with evaporative light scattering method for quantification of forskolin in multi-herbal weight-loss solid oral dosage forms. Pharmazie, 65: 322-326.

[18] Katie J. Astell & Michael L. Mathai & Xiao Q. Su, 2013. A Review on Botanical Species and Chemical Compounds with Appetite Suppressing Properties for Body Weight Control. Plant Foods Human Nutrition, 68: 213-221.

[19] Haritha Kanne, Narayan Pandurang Burte,1 V. Prasanna, and Ravi Gujjula, 2015. Extraction and elemental analysis of Coleus forskohlii extract. Pharmacognosy Research, 7:3, 237-241.

[20] C.Kavitha, K. Rajamani and E. Vadivel, 2009. Coleus forskohlii: A comprehensive review on morphology, phytochemistry and pharmacological aspects. Journal of Medicinal Plants Research, 4:4, 278-285.

[21] Alejandro Ríos-Hoyo & Gabriela Gutiérrez-Salmeán, 2016. New Dietary Supplements for Obesity: What We Currently Know. Obesity Treatment, 5: 262-270.

[22] Steven B. Heymsfield, MD; David B. Allison, PhD; Joseph R. Vasselli, PhD; Angelo Pietrobelli, MD; Debra Greenfield, MS, RD; Christopher Nunez, MEd, 1998. Garcinia cambogia (Hydroxycitric Acid) as a Potential Antiobesity Agent. American Medical Association, 280: 18.

[23] K. Hayamizu, H. Hirakawa, D. Oikawa, T. Nakanishi, T. Takagi, T. Tachibana, M. Furuse, 2003. Effect of Garcinia cambogia extract on serum leptin and insulin in mice. Fitoterapia, 74: 267-273.

[24] Y. Bersudsky, M. Kotler, M. Shifrin and R.H. Belmaker, 1996. A preliminary study of possible psychoactive effects of intravenous forskolin in depressed and schizophrenic patients. Journal of Neural Transmission, 103: 1463-1467.

[25] Jing Chen, Dana C. Hammell, Malinda Spry, John A. D’Orazio, and Audra L. Stinchcomb, 2009. In Vitro Skin Diffusion Study of Pure Forskolin versus a Forskolin-Containing Plectranthus barbatus Root Extract. Journal of Natural Products, 72:4, 769-771.

[26] Sanjay P. Mishra and Vilas G. Gaikar, 2009. Hydrotropic Extraction Process for Recovery of Forskolin from Coleus Forskohlii Roots. Industrial and Engineering Chemistry Research, 48:17.

[27] Michael P. Godard, Brad A. Johnson, and Scott R. Richmond, 2005. Body Composition and Hormonal Adaptations Associated with Forskolin Consumption in Overweight and Obese Men. Obesity Research, 13:8.

[28] Kristine von Krogh, Hannah Harjen, Camilla Alma , Karin E. Zimmer, Ellen Dahl, yIngrid Olsaker, zErik Taubøll, Erik Ropstad, and Steven Verhaegen, 2010. The effect of valproate and levetiracetam on steroidogenesis in forskolin-stimulated H295R cells. Epilepsia, 51:11, 2280-2288.

[29] V. Papadopoulos, 2010. How is the synthesis of testosterone regulated? American Society of Andrology.

[30] Malinda L Spry, Jillian C Vanove, Timothy Scott, Osama Abona-Ama, Kazumasa Wakamatsu, Shosuke Ito and John A. D’Orazio, 2008. Prolonged treatment of fair-skinned mice with topical forskolin causes persistent tanning and UV protection. Pigment Cell Melanoma Research, 22: 219-229.

[31] Xunshan Ding and Jeff L. Staudinger, 2005. Induction of Drug Metabolism by Forskolin: The Role of the Pregnane X Receptor and the Protein Kinase A Signal Transduction Pathway. The Journal of Pharmacology and Experimental Therapeutics, 312: 849-856.

[32] Lirlaˆndia P. Sousa, Fernando Lopes, Douglas M. Silva, Luciana P. Tavares, Ang ́elica T. Vieira, Ba ́rbara M. Rezende, Aline F. Carmo, Remo C. Russo, Cristiana C. Garcia, Cla ́udio A. Bonjardim, Ana L. Alessandri, Adriano G. Rossi, Vanessa Pinho, and Mauro M. Teixeira, 2010. PDE4 inhibition drives resolution of neutrophilic inflammation by inducing apoptosis in a PKA-PI3K/Akt-dependent and NF- B-independent manner. Journal of Leukocyte Biology, 87.

[33] Simon J. MacKenzie, George S. Baillie, Ian McPhee, Carolynn MacKenzie, Rachael Seamons, Theresa McSorley, Jenni Millen, Matthew B. Beard, Gino van Heeke & Miles D. Houslay, 2002. Long PDE4 cAMP speci®c phosphodiesterases are activated by protein kinase A-mediated phosphorylation of a single serine residue in Upstream Conserved Region 1 (UCR1).

[34] Teresa Röhrig, Olga Pacjuk, Silvia Hernández-Huguet, Johanna Körner, Katharina Scherer and Elke Richling, 2017. Inhibition of Cyclic Adenosine Monophosphate- Specific Phosphodiesterase by Various Food Plant-Derived Phytotherapeutic Agents. Medicines, 4: 80.

[35] G. HOLTMANN, B. ADAM, S. HAAG, W. COLLET, E. GRU ̈ NEWALD & T. WINDECK, 2003. Efficacy of artichoke leaf extract in the treatment of patients with functional dyspepsia: a six-week placebo-controlled, double-blind, multicentre trial. Ailment Pharmacological Therapy, 18: 1099-1105.

[36] Elizabeth C. Warburton, 2014. Long-Term Potentiation and Memory. Encyclopaedia of Psychopharmacology.

[37] Vajiheh Rangboo, Mostafa Noroozi, Roza Zavoshy, Seyed Amirmansoor Rezadoost, and Asghar Mohammadpoorasl, 2016. The Effect of Artichoke Leaf Extract on Alanine Aminotransferase and Aspartate Aminotransferase in the Patients with Nonalcoholic Steatohepatitis. International Journal of Hepatology.

 

 

Also known as:Artichoke, Cynarin
Type:Racetam
Good for: , , , , , , ,
Stacks well with: Nootropics Sampler
Typical dose:50 - 900 mg
Half Life :Coming soon...