Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0344307 (analgesia)
 28,200 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Resiniferatoxin is an extremely irritant diterpene present in the latex of several members of the genus Euphorbia. Its mechanism of action has been shown to be clearly distinct from that of the structurally related phorbol esters. Since resiniferatoxin possesses a 4-hydroxy-3-methoxyphenyl substituent, a key feature of capsaicin, the major pungent ingredient of plants of the genus Capsicum, we examined the ability of resiniferatoxin to induce typical capsaicin responses. We report here that treatment of rats with resiniferatoxin, like treatment with capsaicin, caused hypothermia, neurogenic inflammation, and pain. These responses were followed by loss of thermoregulation, by desensitization to neurogenic inflammation, and by chemical and thermal analgesia, with cross-tolerance between resiniferatoxin and capsaicin. Resiniferatoxin was 3 4 orders of magnitude more potent than capsaicin for the effects on thermoregulation and neurogenic inflammation. Resiniferatoxin was only comparable in potency to capsaicin, however, in the assay for induction of acute pain, and the desensitization to acute pain appeared to require less resiniferatoxin than did desensitization for the other responses. We conclude that resiniferatoxin acts as an ultrapotent capsaicin analog and hypothesize that it may distinguish between subclasses of capsaicin response.
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PMID:Resiniferatoxin, a phorbol-related diterpene, acts as an ultrapotent analog of capsaicin, the irritant constituent in red pepper. 274 24

Capsaicin, the pungent alkaloid of red pepper (Capsicum annuum) has been extensively studied for its biological effects which are of pharmacological relevance. These include: cardio protective influence, antilithogenic effect, antiinflammatory, and analgesia, thermogenic influence, and beneficial effects on gastrointestinal system. Therefore, capsaicinoids may have the potential clinical value for pain relief, cancer prevention and weight loss. It has been shown that capsaicinoids are potential agonists of capsaicin receptor (TRPV1). They could exert the effects not only through the receptor-dependent pathway but also through the receptor-independent one. The involvement of neuropeptide Substance P, serotonin, and somatostatin in the pharmacological actions of capsaicin has been extensively investigated. Topical application of capsaicin is proved to alleviate pain in arthritis, postoperative neuralgia, diabetic neuropathy, psoriasis, etc. Toxicological studies on capsaicin administered by different routes are documented. Capsaicin inhibits acid secretion, stimulates alkali and mucus secretion and particularly gastric mucosal blood flow which helps in prevention and healing of gastric ulcers. Antioxidant and antiinflammatory properties of capsaicin are established in a number of studies. Chemopreventive potential of capsaicin is evidenced in cell line studies. The health beneficial hypocholesterolemic influence of capsaicin besides being cardio protective has other implications, viz., prevention of cholesterol gallstones and protection of the structural integrity of erythrocytes under conditions of hypercholesterolemia. Beneficial influences of capsaicin on gastrointestinal system include digestive stimulant action and modulation of intestinal ultrastructure so as to enhance permeability to micronutrients.
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PMID:Biological Activities of Red Pepper (Capsicum annuum) and Its Pungent Principle Capsaicin: A Review. 2567 68

Capsaicinoids are acid amides of C9-C11 branched-chain fatty acids and vanillylamine and constitute important chemical compounds of Capsicum annuum together with their non-pungent analogs (capsinoids) which have an impressive list of health benefit properties (i.e., analgesia, anti-obesity, thermogenic, cardiovascular, gastrointestinal, antioxidant, anti-bacterial, anti-virulence, anti-inflamatory, anti-diabetic, inhibits angiogenesis, and improves glucose metabolism) . In this review, the state of art on how capsaicinoids are affected by different pre- and postharvest factors is discussed together with their biological activity. For instance, high light intensity and heat treatments may reduce capsaicinoid content in fruits probably due to the loss of activity of capsaicin synthase (CS) and phenylalanine ammonia lyase (PAL). The pungency in peppers varies also with environment, genotype or cultivar, node position, fruiting and maturity stages, nitrogen and potassium contents. As the fruit mature, capsaicinoid levels increase. Fruits from the second node tend to have higher accumulation of pungency than those of other positions and the pungency decreases linearly as the node position increase. Sodium hydroxide treatment reduces the pungency of pepper fruit as it hydrolyzes and modifies one of the features (vanillyl group, the acid-amide linkage and alkyl side chain) of capsaicin molecule. Salt and water stress increase PAL and capsaicin synthase activity and increase the capsaicinoid accumulation in fruit, by negatively regulating peroxidase activity at appropriate levels. Future research must be directed in better understanding the changes of capsinoids during pre and post-harvest management, the causal drivers of the loss of activity of the aminotransferase gene (pAMT) and if possible, studies with genetically modified sweet peppers with functional pAMT. Available data provided in this review can be used in different agricultural programs related to developing new cultivars with specific pungency levels. The contents of capsaicinoids and capsinoids in both fresh fruits and marketed products are also of remarkable importance considering the preferences of certain niches in market where higher added-value products might be commercialized.
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PMID:Factors affecting the capsaicinoid profile of hot peppers and biological activity of their non-pungent analogs (Capsinoids) present in sweet peppers. 3221 28