MaxiTherm SD - Cayenne [Capsicum sp.] 2% Capsaicinoids [enteric coated beadlets]

MaxiTherm Key Facts

• MaxiTherm is enteric coated capsicum extract standardised to 2.0% capsaicinoids
• MaxiTherm delivers capsaicinoids safely and effectively to the target organ for optimum benefits

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Background

Capsicum annum is a pungent spice, more commonly known as chilli pepper or red pepper. Capsaicinoids are responsible for the pungency of the fruits. Capsicum has a steep history of use in cooking, as a natural colourant as well as in traditional medicine (Hernandez-Perez et al., 2020). Traditionally capsicum species have been known for their thermogenic properties, as well as being commonly used in traditional medicine practices (Zheng et al., 2017).

Microencapsulation Technology

MaxiTherm is encapsulated to deliver capsaicinoids, eliminating the pungency of capsicum. This Pungency of chili peppers is described by Scoville Heat Units (SHU), with Capsaicin, one of the Capsaicinoids, being responsible for the spicy taste of chilli peppers, as it activates specific receptors on the tongue (Snitker et al., 2009), as well as being an irritant (Srinvasan, 2015). MaxiTherm is perfectly encapsulated form of Capsaicin to avoid any spicy taste or irritation to be caused by the extract, it encapsules capsicum extract using food grade FDA and EFSA approved matrix. It allows improved stability to various bioactive constituents of capsicum extract responsible for the numerous health and pharmacological benefits, as well as improving the absorption and bioavailability of capsaicinoids in human system.

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At present, we have two variantions of MaxiTherm

MaxiTherm Solid Dosage - Cayenne [Capsicum sp.] 2% Capsaicinoids [enteric coated beadlets]

MaxiTherm Beverage Grade - Cayenne [Capsicum sp.] 2% Capsaicinoids [enteric coated beadlets]

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Chemistry

There are three different Capsaicinoids present in Capsicum annum, these are Capsaicin, Dihydrocapsaicin and Nordihydrocapsaicin. MaxiTherm contains 2.0% to 2.3% total capsaicinoids, tested by HPLC.

Brief Identification of Capsaicinoids in MaxiTherm

Capsaicin

CAS – 404-86-4
Molecular Formula – C18H27NO3
Molecular Weight – 3.5.4 g/mol
IUPAC – (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl]-8-methylnon-6-enamide

Dihydrocapsaicin

CAS – 19408-84-5
Molecular Formula – C18H29NO3
Molecular Weight – 307.4 g/mol
IUPAC – N-[(4-hydroxy-3-methoxyphenyl)methyl]-8-methylnonanamide

Nordihydrocapsaicin

CAS – 28789-35-7
Molecular Formula – C17H27NO3
Molecular Weight – 293.4 g/mol
IUPAC – N-[(4-hydroxy-3-methoxyphenyl)methyl]-7-methyloctanamide

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Capsicum and Health

Capsicum extracts are used both orally and topically. Orally, capsaicin has been identified as possessing weight-reducing, thermogenic, hypolipidemic, chemo preventative, antioxidant and anti-inflammatory effects (Srinivasan, 2015). Many of the benefits of capsaicin are due to, but not limited to, its modulation of transient receptor potential vanilloid (TRPV) receptors (Sharma et al., 2013). Topical use focuses on the treatment of pain as well as visceral fat reduction and psoriasis (Srinivasan, 2015; Lee et al., 2013; Reuter et al., 2010).

Metabolic Syndrome

Metabolic Syndrome is a clinical condition, characterised by hyper abdominal adiposity, hypertension, dyslipidemia and insulin resistance (McCracken et al., 2018), and is the main risk factor for cardiovascular disease and type II diabetes (Ford, 2005). Multiple studies have demonstrated that capsaicin has the ability to alter blood lipid profile in a positive manner, reducing plasma total cholesterol, triglycerides and phospholipids (Srinvasan, 2015). Capsaicin has also demonstrated a positive effect on blood glucose levels through decreasing fasting glucose levels and reducing obesity-induced glucose intolerance (Sharma et al., 2013). Capsaicin also appears to reduce insulin resistance through increasing fatty acid oxidation in adipose tissue and the liver (Kang et al, 2010). Capsaicin also exerts cardioprotective effects, due to its interaction with a specific TRPV receptor, TRPV1. TRPV1 is distributed in the vascular system and capsaicin has demonstrated potential vasodilatory, anti-platelet aggregation and hypotensive effects (Chen & Kang, 2013).

Weight Management

The activation of the TRPV1 receptors by capsaicin has been attributed to its weight modifying effects (Baskaran et al., 2017). Capsaicin has been found to promote negative energy balance through increasing satiety, supressing hunger, and increasing energy expenditure (Jang et al., 2020; Josse et al.,2010; Lee et al., 2010; Lejeune et al.,2003; Ludy & Mattes, 2011). Capsaicin also increases metabolic rate by acting on TRPV1 receptors in the adrenal glands to release adrenaline which acts upon beta-adrenergic receptors in fat cells (Yoshioka et al., 1995). Another method by which capsicum can benefit weight reduction is by decreasing adiposity through interactions with the central nervous system. Capsaicin stimulates the secretion of catecholamines from the adrenal medulla via sympathetic activation of the central nervous system, ultimately increasing lipid metabolism (Zhang et al., 2007). Topically, capsaicin is capable of increasing insulin sensitivity, reducing visceral fat and suppressing tissue inflammation through the alteration of adipocyte function (Lee et al., 2013).

Cancer

The actions of capsaicin and the modulation of TRPV receptors is not limited to just that of TRPV1, and in fact capsaicin modulates the TRPV superfamily. Capsaicin has been found to play a positive role in lung cancer as it has been shown to down-regulate the TRPV6 receptor in human small cell lung cancer cells (Lau et al., 2014). Capsaicin has also demonstrated a potential to supress the proliferation of breast cancer cells, gastric cancer cells and cholangiocarcinoma cells (cancer in the bile ducts) (Kim et al., 2014; Park et al., 2014; Wutka et al., 2014). Not only this, but capsaicin has also been found to exhibit an apoptotic effect on certain cancer cells, as well as having beneficial effects in pancreatic cancer, colorectal cancer and bladder cancer (Zheng et al., 2016).

Antioxidant

Capsaicin has been found to prevent lipid peroxidation, protein oxidation as well as preventing antioxidant activity loss induced by gamma radiation (Hernandez-Perez et al., 2020). Lipid peroxidation can result in cell damage and is a process that plays a role in many different diseases as well as the aging process (Spiteller, 2001). Multiple studies have found that capsaicin can act as an antioxidant and inhibit this lipid peroxidation (Srinvasan, 2015).

Anti-inflammatory

Lipid peroxides also play a role in the development of arthritis and other inflammatory diseases and therefore capsaicin can exhibit an anti-inflammatory effect through the inhibition of lipid peroxidation (Srinvasan, 2015). In addition, capsaicin has demonstrated anti-inflammatory effects in individuals with arthritis through its interaction TRPV1 (Fernandes et al., 2016). It has also been found that capsaicin can act as an anti-inflammatory agent by enhancing the expression of interleukin-10 (an anti-inflammatory cytokine) and suppressing the expression of interleukin-8 (a pro-inflammatory cytokine) in certain cells which contributes to the chemo-preventative effects of capsaicin (Lu et al., 2020).

Pain Relief

Capsaicin is a TRPV1 (also known as the capsaicin receptor) agonist, and it is through the activation of this receptor that capsaicin exerts some of its pain-relieving effects (Sharma et al., 2013). However, capsaicin also appears to provide analgesia through a cascade of events (Anand & Bley, 2011). Topical application of capsaicin has proven to alleviate pain in ostearthritis as well as neuropathy (Lee et al., 2013).

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Trademark

MaxiTherm is a trademark of Vita Actives, EU trademark number 013819727.

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References

1. Anand, P. and Bley, K., 2011. Topical capsaicin for pain management: therapeutic potential and mechanisms of action of the new high-concentration capsaicin 8% patch. British Journal of Anaesthesia, 107(4), pp.490-502.
2. Baskaran, P., Krishnan, V., Fettel, K., Gao, P., Zhu, Z., Ren, J. and Thyagarajan, B., 2017. TRPV1 activation counters diet-induced obesity through sirtuin-1 activation and PRDM-16 deacetylation in brown adipose tissue. International Journal of Obesity, 41(5), pp.739-749.
3. Chen, L. and Kang, Y., 2013. Anti-inflammatory and antioxidant activities of red pepper (Capsicum annuum L.) stalk extracts: Comparison of pericarp and placenta extracts. Journal of Functional Foods, 5(4), pp.1724-1731.
4. Fernandes, E., Cerqueira, A., Soares, A. and Costa, S., 2016. Capsaicin and Its Role in Chronic Diseases. Advances in Experimental Medicine and Biology, pp.91-125.
5. Ford, E., 2005. Risks for All-Cause Mortality, Cardiovascular Disease, and Diabetes Associated With the Metabolic Syndrome: A summary of the evidence. Diabetes Care, 28(7), pp.1769-1778.
6. Hernández‐Pérez, T., Gómez‐García, M., Valverde, M. and Paredes‐López, O., 2020. Capsicum annuum(hot pepper): An ancient Latin‐American crop with outstanding bioactive compounds and nutraceutical potential. A review. Comprehensive Reviews in Food Science and Food Safety, 19(6), pp.2972-2993.
7. Jang, H., Lee, J., Lee, S. and Lee, Y., 2020. Effects of Capsicum annuum supplementation on the components of metabolic syndrome: a systematic review and meta-analysis. Scientific Reports, 10(1).
8. Josse, A., Sherriffs, S., Holwerda, A., Andrews, R., Staples, A. and Phillips, S., 2010. Effects of capsinoid ingestion on energy expenditure and lipid oxidation at rest and during exercise. Nutrition & Metabolism, 7(1), p.65.
9. Kang, J., Tsuyoshi, G., Han, I., Kawada, T., Kim, Y. and Yu, R., 2010. Dietary Capsaicin Reduces Obesity-induced Insulin Resistance and Hepatic Steatosis in Obese Mice Fed a High-fat Diet. Obesity, 18(4), pp.780-787.
10. Kim, H., Kim, M., Kim, S. and Kim, Y., 2013. Pepper Seed Extract Suppresses Invasion and Migration of Human Breast Cancer Cells. Nutrition and Cancer, 66(1), pp.159-165.
11. Lau, J., Brown, K., Dom, A., Witte, T., Thornhill, B., Crabtree, C., Perry, H., Brown, J., Ball, J., Creel, R., Damron, C., Rollyson, W., Stevenson, C., Hardman, W., Valentovic, M., Carpenter, A. and Dasgupta, P., 2014. Capsaicin induces apoptosis in human small cell lung cancer via the TRPV6 receptor and the calpain pathway. Apoptosis, 19(8), pp.1190-1201.
12. Lee, T., Li, Z., Zerlin, A. and Heber, D., 2010. Effects of dihydrocapsiate on adaptive and diet-induced thermogenesis with a high protein very low-calorie diet: a randomized control trial. Nutrition & Metabolism, 7(1), p.78.
13. Lee, G., Shin, M., Yoon, D., Kim, A., Yu, R., Park, N. and Han, I., 2013. Topical application of capsaicin reduces visceral adipose fat by affecting adipokine levels in high-fat diet-induced obese mice. Obesity, 21(1), pp.115-122.
14. Lejeune, M., Kovacs, E. and Westerterp-Plantenga, M., 2003. Effect of capsaicin on substrate oxidation and weight maintenance after modest body-weight loss in human subjects. British Journal of Nutrition, 90(3), pp.651-659.
15. Lu, M., Chen, C., Lan, Y., Xiao, J., Li, R., Huang, J., Huang, Q., Cao, Y. and Ho, C., 2020. Capsaicin—the major bioactive ingredient of chili peppers: bio-efficacy and delivery systems. Food & Function, 11(4), pp.2848-2860.
16. Ludy, M. and Mattes, R., 2011. The effects of hedonically acceptable red pepper doses on thermogenesis and appetite. Physiology & Behaviour, 102(3-4), pp.251-258.
17. McCracken, E., Monaghan, M. and Sreenivasan, S., 2018. Pathophysiology of the metabolic syndrome. Clinics in Dermatology, 36(1), pp.14-20.
18. Park, S., Kim, J., Lee, S., Jun, C., Cho, S., Park, C., Joo, Y., Kim, H., Choi, S. and Rew, J., 2013. Capsaicin induces apoptosis and modulates MAPK signaling in human gastric cancer cells. Molecular Medicine Reports, 9(2), pp.499-502.
19. Reuter, J., Merfort, I. and Schempp, C., 2010. Botanicals in Dermatology. American Journal of Clinical Dermatology, p.1.
20. Sharma, S., Vij, A. and Sharma, M., 2013. Mechanisms and clinical uses of capsaicin. European Journal of Pharmacology, 720(1-3), pp.55-62.
21. Snitker, S., Fujishima, Y., Shen, H., Ott, S., Pi-Sunyer, X., Furuhata, Y., Sato, H. and Takahashi, M., 2008. Effects of novel capsinoid treatment on fatness and energy metabolism in humans: possible pharmacogenetic implications. The American Journal of Clinical Nutrition, 89(1), pp.45-50.
22. Spiteller, G., 2001. Lipid peroxidation in aging and age-dependent diseases. Experimental Gerontology, 36(9), pp.1425-1457.
23. Srinivasan, K., 2015. Biological Activities of Red Pepper (Capsicum annuum) and Its Pungent Principle Capsaicin: A Review. Critical Reviews in Food Science and Nutrition, 56(9), pp.1488-1500.
24. Wutka, A., Palagani, V., Barat, S., Chen, X., El Khatib, M., Götze, J., Belahmer, H., Zender, S., Bozko, P., Malek, N. and Plentz, R., 2014. Capsaicin Treatment Attenuates Cholangiocarcinoma Carcinogenesis. PLoS ONE, 9(4), p.e95605.
25. Yoshioka, M., Lim, K., Kikuzato, S., Kiyonaga, A., Tanaka, H., Shindo, M. and Suzuki, M., 1995. Effects of Red-Pepper Diet on the Energy Metabolism in Men. Journal of Nutritional Science and Vitaminology, 41(6), pp.647-656.
26. Zhang, L., Yan Liu, D., Ma, L., Luo, Z., Cao, T., Zhong, J., Yan, Z., Wang, L., Zhao, Z., Zhu, S., Schrader, M., Thilo, F., Zhu, Z. and Tepel, M., 2007. Activation of Transient Receptor Potential Vanilloid Type-1 Channel Prevents Adipogenesis and Obesity. Circulation Research, 100(7), pp.1063-1070.
27. Zheng, J., Zhou, Y., Li, Y., Xu, D., Li, S. and Li, H., 2016. Spices for Prevention and Treatment of Cancers. Nutrients, 8(8), p.495.
28. Zheng, J., Zheng, S., Feng, Q., Zhang, Q. and Xiao, X., 2017. Dietary capsaicin and its anti-obesity potency: from mechanism to clinical implications. Bioscience Reports, 37(3).