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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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Chili extract, Hot pepper extract, trans-8-methyl-N-Vanilyl-6-nonenamide, Capsaicinoids
Piperine (Black Pepper extract)
Doses of 6mg/kg bodyweight capsaicin have been shown to be able to increase the metabolic rate somewhat.
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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, of which the 6 most common capsaicinoids include capsaicin, dihydrocapsaicin, nordihydrocapsaicin, homodihydrocapsaicin, homocapsaicin, and nonivamide 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.
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.
Capsaicin is metabolized extensively by the liver CYP450 enzymes and Carboxyesterase class enzymes and yeild numerous byproducts via akly, aromatic, and amide metabolic pathways. Due to metabolic changes to the vanilloid ring and capsaicin's hydrophobic alkyl sidechain, the metabolites possess less potential at the VR1 receptor. Capsaicin also possess numerous 'electrophile' metabolites, that can bind to liver enzymes and proteins via a reactive arene oxide or quinone methide group.
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 and normal cells. It may do these effects via stimulating the catalytic units of protein kinase CKII, a protein involved in cell death regulation.
An analog of capsaicin, dihydrocapsaicin, is more potent than capsaicin in regards to cell death.
Capsaicin has been shown to induce catecholamine (adrenaline-like compounds) secretion which exerts beta-adrenergic like effects. These effects were seen at approximately 6mg/kg bodyweight. These effects have been replicated in humans with red pepper added to meals.
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 and exerts an appetite suppressing effects.
Capsaicin can also induce heat production via neuronal stimulation, possibly by neurons expressing the VR1 receptors. These increases in heat seem to be vicariously through beta-adrenergic stimulation.
Capsaicin works on pain primarily via agonism (activation) of the capsaicin receptor, known as the vanilloid receptor 1 (VR1, or TRPV1).
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. Although this same mechanism may be protective against some carcinogens which are bio-activated by P450 enzymes.
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). This may be due to the reduction in P450 activity, and that these carcinogens are actually bioactivated by these compounds rather than properly detoxified.
Capsaicin holds a Generally Recognized as Safe (GRAS) title for usage in foods.
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. Much lower amounts are needed (0.58 and 1.6mg/kg) when injected. Only one report of death by capsaicin ingestion has been noted, although there have been multiple deaths linked to pepper spray usage.
Capsaicin in topical products have been sometimes found to be contaminated with aflatoxin and N-nitroso compounds.
(Common misspellings for Capsaicin include capsayicin, capsayisin, capsaisin, capsaysin, capsaycin, peper)
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