Capsaicin

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Capsaicin (Cap-say-uh-sin) is the primary active ingredient in Hot (Chili) pepper extract. It is the compound that gives peppers the hot 'kick' to their taste when eaten. Capsaicin is actually one of a few compounds called 'Capsaicinoids', but it is the most common and well-known one.

When ingested, it does increase the Metabolic Rate slightly. It does this in part by increasing adrenaline levels (the fight-or-flight hormone) but also can act directly on fat cells to induce fat loss.

It is found in hot peppers, and due to it being the compound causing the heat of the peppers when eaten there is a direct correlation between the two. The hotter the pepper, the more capsaicin it contains. The beneficial effects can be found in foods, or also when superloaded through supplements.

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Doses of 6mg/kg bodyweight capsaicin have been shown to be able to increase the metabolic rate somewhat.

Edit1. Overview, sources, and structure

Chilis belong to the Capsicum subfamily of the plants referred to as Solanaceae, with the extract in question, capsaicin. Capsaicin is the primary pungent alkaloid of the 'Capsaicinoids' found in chili and hot pepper extracts^[1], of which the 6 most common capsaicinoids include capsaicin, dihydrocapsaicin, nordihydrocapsaicin, homodihydrocapsaicin, homocapsaicin, and nonivamide^[2][3] All 6 main analogues share the same effects on the capsaicin receptor (to be discussed) but with varying potencies. Nonivamide and Capsaicin are the most potent agonists, followed by Dihydrocapsaicin, and then the final three analogues.^[4]

Edit2. Pharmacology and ingestion

After ingestion, capsaicin is taken up through both the stomach walls and the small intestine. In the stomach, it may exert protective effects against ulcers by inducing secretion of gastric fluids.^[5][6]

Capsaicin is metabolized extensively by the liver CYP450 enzymes and Carboxyesterase class enzymes^[7] and yeild numerous byproducts via akly, aromatic, and amide metabolic pathways.^[8] Due to metabolic changes to the vanilloid ring and capsaicin's hydrophobic alkyl sidechain, the metabolites possess less potential at the VR1 receptor.^[9] Capsaicin also possess numerous 'electrophile' metabolites, that can bind to liver enzymes and proteins via a reactive arene oxide or quinone methide group.^[4][10]

In systemic circulation, capsaicin is known as a Vanilloid Receptor 1 (VR1, or TRPV1) agonist. Agonism of this receptor (known as the Capsaicin receptor) causes cell apoptosis of tumor cells^[11][12] and normal cells.^[13] It may do these effects via stimulating the catalytic units of protein kinase CKII, a protein involved in cell death regulation.^[14]

An analog of capsaicin, dihydrocapsaicin, is more potent than capsaicin in regards to cell death.^[15]

Edit3. Topical application

Edit4. Fat burning implications

Capsaicin has been shown to induce catecholamine (adrenaline-like compounds) secretion^[16][17] which exerts beta-adrenergic like effects.^[18] These effects were seen at approximately 6mg/kg bodyweight. These effects have been replicated in humans with red pepper added to meals.^[19][20][21]

In addition to slightly increasing the metabolic rate via beta-adrenergic stimulation, capsaicin can also change more systemic energy metabolism towards utilizing fat rather than carbohydrate^[19][22] and exerts an appetite suppressing effects.^[23][24][25]

Capsaicin can also induce heat production via neuronal stimulation^[26], possibly by neurons expressing the VR1 receptors.^[27] These increases in heat seem to be vicariously through beta-adrenergic stimulation.^[18][28]

These effects have also been noted with Capsiate, a non-pungent capsaicinoid compound.^[29][30]

Edit5. Capsaicin and Pain

Capsaicin works on pain primarily via agonism (activation) of the capsaicin receptor, known as the vanilloid receptor 1 (VR1, or TRPV1).^[31]

Edit6. Capsaicin and its Metabolites in regards to Cancer

Edit7. Pro-carcinogenic

One of the mechanisms by which capsaicin can promote cancer and tumor growth is via inhibition of the CYP450-2E1 enzyme, which typically prevents select carcinogencs (vinyl carbamate, dimethyl nitrosamine) from being metabolized to their toxic metabolites.^[32][33] Although this same mechanism may be protective against some carcinogens which are bio-activated by P450 enzymes.^[34][35]

It seems to have more pro-carcinogenic effects when paired with certain carcinogens, and in doses found in supplementation.^[36][37]

Edit8. Anti-carcinogenic

Capsaicins have been shown to be protective against lung cancers that are promoted by polycyclic aromatic hydrocarbons, such as Naphthalene and NNK (the major nitrosamine in cigarette smoke^[38]).^[39][40] This may be due to the reduction in P450 activity, and that these carcinogens are actually bioactivated by these compounds rather than properly detoxified.^[41]

Edit9. Toxicity and safety - Potential complications

Capsaicin holds a Generally Recognized as Safe (GRAS) title for usage in foods.^[42]

Oral LD50 values as low as 161.2 mg/kg (rats) and 118.8 mg/kg (mice) have been reported for Capsaicin in acute oral toxicity studies.^[42] Much lower amounts are needed (0.58 and 1.6mg/kg) when injected.^[43] Only one report of death by capsaicin ingestion has been noted^[44], although there have been multiple deaths linked to pepper spray usage.^[45][46]

Capsaicin in topical products have been sometimes found to be contaminated with aflatoxin and N-nitroso compounds.^[42]

References

1. Surh Y. Molecular mechanisms of chemopreventive effects of selected dietary and medicinal phenolic substances. Mutat Res. (1999)
2. Reilly CA, et al. Determination of capsaicin, dihydrocapsaicin, and nonivamide in self-defense weapons by liquid chromatography-mass spectrometry and liquid chromatography-tandem mass spectrometry. J Chromatogr A. (2001)
3. Luo XJ, Peng J, Li YJ. Recent advances in the study on capsaicinoids and capsinoids. Eur J Pharmacol. (2011)
4. Reilly CA, Yost GS. Metabolism of capsaicinoids by P450 enzymes: a review of recent findings on reaction mechanisms, bio-activation, and detoxification processes. Drug Metab Rev. (2006)
5. Holzer P, Sametz W. Gastric mucosal protection against ulcerogenic factors in the rat mediated by capsaicin-sensitive afferent neurons. Gastroenterology. (1986)
6. Oyagbemi AA, Saba AB, Azeez OI. Capsaicin: a novel chemopreventive molecule and its underlying molecular mechanisms of action. Indian J Cancer. (2010)
7. Surh YJ, Lee SS. Capsaicin, a double-edged sword: toxicity, metabolism, and chemopreventive potential. Life Sci. (1995)
8. Reilly CA, et al. Metabolism of capsaicin by cytochrome P450 produces novel dehydrogenated metabolites and decreases cytotoxicity to lung and liver cells. Chem Res Toxicol. (2003)
9. Jordt SE, Julius D. Molecular basis for species-specific sensitivity to "hot" chili peppers. Cell. (2002)
10. The mechanism of inhibition of cytochrome P450IIE1 by dihydrocapsaicin
11. Lee YS, Nam DH, Kim JA. Induction of apoptosis by capsaicin in A172 human glioblastoma cells. Cancer Lett. (2000)
12. Surh YJ. More than spice: capsaicin in hot chili peppers makes tumor cells commit suicide. J Natl Cancer Inst. (2002)
13. Reilly CA, et al. Calcium-dependent and independent mechanisms of capsaicin receptor (TRPV1)-mediated cytokine production and cell death in human bronchial epithelial cells. J Biochem Mol Toxicol. (2005)
14. Rho YW, Bae YS. Capsaicin, a component of red peppers, stimulates protein kinase CKII activity. BMB Rep. (2010)
15. Oh SH, et al. Dihydrocapsaicin (DHC), a saturated structural analog of capsaicin, induces autophagy in human cancer cells in a catalase-regulated manner. Autophagy. (2008)
16. Kawada T, et al. Some pungent principles of spices cause the adrenal medulla to secrete catecholamine in anesthetized rats. Proc Soc Exp Biol Med. (1988)
17. Watanabe T, et al. Capsaicin, a pungent principle of hot red pepper, evokes catecholamine secretion from the adrenal medulla of anesthetized rats. Biochem Biophys Res Commun. (1987)
18. Kawada T, et al. Capsaicin-induced beta-adrenergic action on energy metabolism in rats: influence of capsaicin on oxygen consumption, the respiratory quotient, and substrate utilization. Proc Soc Exp Biol Med. (1986)
19. Yoshioka M, et al. Effects of red-pepper diet on the energy metabolism in men. J Nutr Sci Vitaminol (Tokyo). (1995)
20. Henry CJ, Emery B. Effect of spiced food on metabolic rate. Hum Nutr Clin Nutr. (1986)
21. Diepvens K, Westerterp KR, Westerterp-Plantenga MS. Obesity and thermogenesis related to the consumption of caffeine, ephedrine, capsaicin, and green tea. Am J Physiol Regul Integr Comp Physiol. (2007)
22. Yoshioka M, et al. Effects of red pepper added to high-fat and high-carbohydrate meals on energy metabolism and substrate utilization in Japanese women. Br J Nutr. (1998)
23. Yoshioka M, et al. Effects of red pepper on appetite and energy intake. Br J Nutr. (1999)
24. Yoshioka M, et al. Combined effects of red pepper and caffeine consumption on 24 h energy balance in subjects given free access to foods. Br J Nutr. (2001)
25. Westerterp-Plantenga MS, Smeets A, Lejeune MP. Sensory and gastrointestinal satiety effects of capsaicin on food intake. Int J Obes (Lond). (2005)
26. Osaka T, et al. Thermogenesis mediated by a capsaicin-sensitive area in the ventrolateral medulla. Neuroreport. (2000)
27. Adrenal sympathetic efferent nerve and catecholamine secretion excitation caused by capsaicin in rats
28. Hursel R, Westerterp-Plantenga MS. Thermogenic ingredients and body weight regulation. Int J Obes (Lond). (2010)
29. Ohnuki K, et al. Administration of capsiate, a non-pungent capsaicin analog, promotes energy metabolism and suppresses body fat accumulation in mice. Biosci Biotechnol Biochem. (2001)
30. Ohnuki K, et al. CH-19 sweet, a non-pungent cultivar of red pepper, increased body temperature and oxygen consumption in humans. Biosci Biotechnol Biochem. (2001)
31. Wong GY, Gavva NR. Therapeutic potential of vanilloid receptor TRPV1 agonists and antagonists as analgesics: Recent advances and setbacks. Brain Res Rev. (2009)
32. Effect of capsaicin and chilli on ethanol induced gastric mucosal injury in the rat
33. Capsaicin can alter the expression of tumor forming-related genes which might be followed by induction of apoptosis of a Korean stomach cancer cell line, SNU-1
34. Tanaka T, et al. Modifying effects of dietary capsaicin and rotenone on 4-nitroquinoline 1-oxide-induced rat tongue carcinogenesis. Carcinogenesis. (2002)
35. Zhang Z, Huynh H, Teel RW. Effects of orally administered capsaicin, the principal component of capsicum fruits, on the in vitro metabolism of the tobacco-specific nitrosamine NNK in hamster lung and liver microsomes. Anticancer Res. (1997)
36. Surh YJ, Lee SS. Capsaicin in hot chili pepper: carcinogen, co-carcinogen or anticarcinogen. Food Chem Toxicol. (1996)
37. Bode AM, Dong Z. The two faces of capsaicin. Cancer Res. (2011)
38. Hecht SS, Hoffmann D. Tobacco-specific nitrosamines, an important group of carcinogens in tobacco and tobacco smoke. Carcinogenesis. (1988)
39. Jang JJ, Kim SH, Yun TK. Inhibitory effect of capsaicin on mouse lung tumor development. In Vivo. (1989)
40. Miller CH, et al. Effects of capsaicin on liver microsomal metabolism of the tobacco-specific nitrosamine NNK. Cancer Lett. (1993)
41. Zhang Z, et al. Inhibition of liver microsomal cytochrome P450 activity and metabolism of the tobacco-specific nitrosamine NNK by capsaicin and ellagic acid. Anticancer Res. (1993)
42. [No authors listed. Final report on the safety assessment of capsicum annuum extract, capsicum annuum fruit extract, capsicum annuum resin, capsicum annuum fruit powder, capsicum frutescens fruit, capsicum frutescens fruit extract, capsicum frutescens resin, and capsaicin. Int J Toxicol. (2007)
43. Glinsukon T, et al. Acute toxicity of capsaicin in several animal species. Toxicon. (1980)
44. Snyman T, Stewart MJ, Steenkamp V. A fatal case of pepper poisoning. Forensic Sci Int. (2001)
45. Steffee CH, et al. Oleoresin capsicum (pepper) spray and "in-custody deaths". Am J Forensic Med Pathol. (1995)
46. Billmire DF, et al. Pepper-spray-induced respiratory failure treated with extracorporeal membrane oxygenation. Pediatrics. (1996)
47. Chaiyasit K, Khovidhunkit W, Wittayalertpanya S. Pharmacokinetic and the effect of capsaicin in Capsicum frutescens on decreasing plasma glucose level. J Med Assoc Thai. (2009)

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