In vitro intestinal absorption of capsaicin

Monsereenusorn, Yongyot

doi:10.1016/0041-008x(80)90390-7

Cited by 16 publications

(5 citation statements)

References 8 publications

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“…Results indicated regional differences in the absorption of capsaicin from the gastrointestinal tract. The findings reported by Kawada et al 300 are in agreement with the in vitro results reported by Monsereenusorn 301 regarding the in vitro intestinal absorption of capsaicin. The degree and processes of absorption of capsaicin and capsaicinoids in the respiratory tract have not been elucidated.…”

Section: Uptake Distribution Metabolism and Excretionsupporting

confidence: 91%

Riot control agents: pharmacology, toxicology, biochemistry and chemistry

Olajos¹,

Salem²

2001

J of Applied Toxicology

121

116

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The desired effect of all riot control agents is the temporary disablement of individuals by way of intense irritation of the mucous membranes and skin. Generally, riot control agents can produce acute site-specific toxicity where sensory irritation occurs. Early riot control agents, namely, chloroacetophenone (CN) and chlorodihydrophenarsazine (DM), have been replaced with 'safer' agents such as o-chlorobenzylidene malononitrile (CS) and oleoresin of capsicum (OC). Riot control agents are safe when used as intended: however, the widespread use of riot control agents raises questions and concerns regarding their health effects and safety. A large margin exists between dosages that produce harassment and dosages likely to cause adverse health effects for modern riot control agents such as CS and dibenz[b,f]1 : 4-oxazepine (CR). Yet, despite the low toxicity of modern riot control agents, these compounds are not entirely without risk. The risk of toxicity increases with higher exposure levels and prolonged exposure durations. Ocular, pulmonary and dermal injury may occur on exposure to high levels of these substances, and exposure to riot control agents in enclosed spaces may produce significant toxic effects. Reported deaths are few involving riot control agents, and then only under conditions of prolonged exposure and high concentrations. Recently, concern has focused on the deaths resulting from law enforcement use of OC, a riot control agent generally regarded as safe because it is a natural product. As with other xenobiotics, not enough is known concerning the long-term/chronic effects of riot control agents. Clearly, there is considerable need for additional research to define and delineate the biological and toxicological actions of riot control agents and to illuminate the full health consequences of these compounds as riot control agents.

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Section: Uptake Distribution Metabolism and Excretionsupporting

confidence: 91%

Riot control agents: pharmacology, toxicology, biochemistry and chemistry

Olajos¹,

Salem²

2001

J of Applied Toxicology

121

116

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“…There are no published data on the oral bioavailability of capsaicin. However, evidence from a rat intestinal ex vivo study predicts that the molecule will be readily absorbed from the intestinal tract (Monsereenusorn, 1980). Therefore, capsaicin ingested from food is probably well absorbed and subjected to significant first-pass hepatic metabolism.…”

Section: Discussionmentioning

confidence: 99%

In Vitro Hepatic and Skin Metabolism of Capsaicin

Chanda¹,

Musa²,

Babbar³

et al. 2008

Drug Metab Dispos

110

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ABSTRACT:On the basis of the ability of capsaicin to activate the transient receptor potential vanilloid 1 receptor (TRPV1) expressed in nociceptive sensory neurons, topical and injectable high-concentration formulations are being developed as potential treatments for various pain syndromes. As much of the published literature on capsaicin is based on pepper extracts, which are typically a mixture of capsaicin and other capsaicinoids (including norhydrocapsaicin, dihydrocapsaicin, homocapsaicin and homodihydrocapsaicin), the purpose of this investigation was to study the in vitro metabolism of pure capsaicin. The metabolism of capsaicin was similar in human, rat, and dog microsomes and S9 fractions.In these assays, three major metabolites were detected and identified as 16-hydroxycapsaicin, 17-hydroxycapsaicin, and 16,17-dehydrocapsaicin. In addition to these three metabolites, rat microsomes and S9 fractions also produced vanillylamine and vanillin. Biotransformation of capsaicin was slow in human skin in vitro, with the majority of the applied capsaicin remaining unchanged and a small fraction being metabolized to vanillylamine and vanillic acid. These data suggest that the metabolism of capsaicin by cytochrome P450 enzymes in skin is minimal, relative to hepatic metabolism.Capsaicin is the most abundant pungent molecule produced by pepper plants and thereby represents an important ingredient in spicy foods consumed throughout the world. The capsaicin content of peppers ranges from 0.1 to 2.5 mg/g (Parrish, 1996), and the resulting average human capsaicin consumption is on the order of 0.5 to 4 mg/kg/day (EC Scientific Committee on Food, 2002, http://ec.europa.eu/food/fs/sc/scf/out120_en.pdf). In addition to its extensive role as a food additive, there is also substantial human exposure to capsaicin in the form of nonprescription (in the United States) or prescription (in the European Union) topical analgesics, self-defense products (e.g., pepper spray), and oral herbal supplements.Capsaicin is a highly selective agonist for the TRPV1 [formerly known as the vanilloid receptor 1 (VR1)]. TRPV1 is a ligand-gated, nonselective cation channel preferentially expressed on small-diameter sensory neurons, especially those nociceptors that specialize in the detection of painful or noxious sensations (C-fibers and to a lesser extent A␦-fibers) (Caterina et al., 1997;Szallasi and Blumberg, 1999). The initial effect of capsaicin is the activation of TRPV1-expressing nociceptors, resulting in a burning sensation, hyperalgesia, allodynia, and erythema (Szallasi and Blumberg, 1999); these events are followed by a reversible defunctionalization of nociceptive sensory axons (Bley, 2004). Defunctionalization of hyperactive nociceptors is thought to underlie the pain relief that follows topical application or intra-articular injections of capsaicin (Bley, 2004).Much of the published literature on capsaicin relates to extracts of capsaicin derived from peppers; these extracts are typically a mixture of capsaicin, norhydrocapsaicin...

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“…The intestinal absorption of capsaicin in vitro was done using everted intestinal sacs isolated from rats [32]. It was observed that capsaicin was robustly absorbed both into intestinal tissues, jejunum and serosal fluid.…”

Section: Biotransformation Of Capsaicin In Vitromentioning

confidence: 99%

Bioavailability of capsaicin and its implications for drug delivery

Rollyson

Stover

Brown

et al. 2014

Journal of Controlled Release

210

160

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The dietary compound capsaicin is responsible for the “hot and spicy” taste of chili peppers and pepper extracts. It is a valuable pharmacological agent with several therapeutic applications in controlling pain and inflammation. Emerging studies show that it displays potent anti-tumor activity in several human cancers. On a more basic research level, capsaicin has been used as a ligand to activate several types of ion-channel receptors. The pharmacological activity of capsaicin-like compounds is dependent on several factors like the dose, the route of administration and most importantly on its concentration at target tissues. The present review describes the current knowledge involving the metabolism and bioavailability of capsaicinoids in rodents and humans. Novel drug delivery strategies used to improve the bioavailability and therapeutic index of capsaicin are discussed in detail. The generation of novel capsaicin-mimetics and improved drug delivery methods will foster the hope of innovative applications of capsaicin in human disease.

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In vitro intestinal absorption of capsaicin

Cited by 16 publications

References 8 publications

Riot control agents: pharmacology, toxicology, biochemistry and chemistry

Riot control agents: pharmacology, toxicology, biochemistry and chemistry

In Vitro Hepatic and Skin Metabolism of Capsaicin

Bioavailability of capsaicin and its implications for drug delivery

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