Interdisciplinary review for correlation between the plant origin capsaicinoids, non-steroidal antiinflammatory drugs, gastrointestinal mucosal damage and prevention in animals and human beings

Mózsik, Gyula; Past, T; Abdel-Salam, Omar M.E.; Kuźma, Monika; Perjési, Pál

doi:10.1007/s10787-009-0002-3

Cited by 24 publications

(12 citation statements)

References 150 publications

(203 reference statements)

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“…Therefore, approximately 94 percent of orally administered capsaicin is digested. Only a small part of capsaicin was also expelled intact in urine (0.095%) [223]. Kawada et al [224] have documented from an in vivo study in rats that the gastrointestinal absorption of capsaicin is rapid, and about 85 percent of the dose was absorbed within 3 h. Additionally, the absorbed capsaicin is willingly transported to the portal blood (about 85%) and partially metabolized during absorption to 8-methyl nonanoic acid.…”

Section: Pharmacokinetics Of Capsicum and Its Related Compound (Capsamentioning

confidence: 99%

Biological Properties, Bioactive Constituents, and Pharmacokinetics of Some Capsicum spp. and Capsaicinoids

Batiha

Alqahtani

Ojo

et al. 2020

IJMS

144

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Pepper originated from the Capsicum genus, which is recognized as one of the most predominant and globally distributed genera of the Solanaceae family. It is a diverse genus, consisting of more than 31 different species including five domesticated species, Capsicum baccatum, C. annuum, C. pubescen, C. frutescens, and C. chinense. Pepper is the most widely used spice in the world and is highly valued due to its pungency and unique flavor. Pepper is a good source of provitamin A; vitamins E and C; carotenoids; and phenolic compounds such as capsaicinoids, luteolin, and quercetin. All of these compounds are associated with their antioxidant as well as other biological activities. Interestingly, Capsicum fruits have been used as food additives in the treatment of toothache, parasitic infections, coughs, wound healing, sore throat, and rheumatism. Moreover, it possesses antimicrobial, antiseptic, anticancer, counterirritant, appetite stimulator, antioxidant, and immunomodulator activities. Capsaicin and Capsicum creams are accessible in numerous ways and have been utilized in HIV-linked neuropathy and intractable pain.

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Section: Pharmacokinetics Of Capsicum and Its Related Compound (Capsamentioning

confidence: 99%

Biological Properties, Bioactive Constituents, and Pharmacokinetics of Some Capsicum spp. and Capsaicinoids

Batiha

Alqahtani

Ojo

et al. 2020

IJMS

144

View full text Add to dashboard Cite

show abstract

“…Exposure to high doses of capsaicin (above 100 mg capsaicin per kg body weight) for a prolonged time causes peptic ulcers, accelerates the development of prostate, stomach, duodenal, and liver cancers and enhances breast cancer metastasis [5, 6]. …”

Section: Pharmacological Effects Of Capsaicinoidsmentioning

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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“…Our aim was to product a capsaicin containing drug or drug combinations with a NSAID for the treatment of above mentioned groups of patients hoping that application of these compounds will be able to prevent the NSAIDs induced GI side effects in patients (Mózsik et al, 2009a(Mózsik et al, ,b, 2010Szabo et al, 2013).…”

Section: Main Problems Of Pharmacological Treatment In Patient With Dmentioning

confidence: 99%

Capsaicin is a New Gastrointestinal Mucosal Protecting Drug Candidate in Humans — Pharmaceutical Development and Production Based on Clinical Pharmacology

Mózsik¹,

Past²,

Habon³

et al. 2014

Capsaicin - Sensitive Neural Afferentation and the Gastrointestinal Tract: From Bench to Bedside

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applications of these drugs are contraindicated from the points of gastroenterologist. 4. We earlier proved clearly that the small doses of capsaicin (given orally in doses of nanogram to microgram / kg in animal experiments and 200 to 800 µg in human observations) prevents the aspirin, indomethacin (a mixed COX-1 and COX-2 inhibitor)-induced gastrointestinal mucosal damage. Aims: 1. The development and pharmaceutically production of the planned production of new gastrointestinal mucosal protective drug (capsaicin alone and/or capsaicin in combination with different nonsteroidal anti-inflammatory drugs) for the use in human healthy beings and in patients. 2. For the development and production of a new drug, we had to respect the following aspects: a. the knowledge of the chemical composition of natural origin capsaicin(oids); b. problems of the analytical measurements of capsaicin(oids) in the biological samples (in animals and humans); c. correct and complete preclinical dossier; d. correct dossier of acute and chronic toxicological studies with capsaicin (including the different tests) in two speciments of animal experiments; e. existence of a complete drug master file (DMF); f. the exclusion of pesticides, fusariums, aflatoxin and other toxicological agents (which are used during the plant cultivation in the different countries) from the capsaicin(oids) preparations used for drug production; g. to collect the necessary permissions from the different international and national authrorities before starting of pharmaceutical production of drug alone or in combinations; h. different pharmaceutical controlling measurements and other pharmaceutical aspects of planned drug or drug combinations (such as stability, drug preparation, different pharmaceutical technologies, etc.); i. preparation of different protocols for human human phase examinations (especially for human phase I.); j. to receive the permissions from the the different national authorities to carried out the prepared protocols before starting of the classical pharmacological studies; k. to gather the necessary numbers of experts from the very different scientific fields, who are able to solve all of above mentioned scientific, pharmaceutical, research problems (in animal experiments and in human observations); l. to find accredited institutes to perform human clinical pharmacological (phase) examinations. 2. When we solved all of above scientific problems, the human phase I. examinations with capsaicin alone and with combination+aspirin and capsaicin+diclofenac, the human phase I. examinations were in the

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Interdisciplinary review for correlation between the plant origin capsaicinoids, non-steroidal antiinflammatory drugs, gastrointestinal mucosal damage and prevention in animals and human beings

Cited by 24 publications

References 150 publications

Biological Properties, Bioactive Constituents, and Pharmacokinetics of Some Capsicum spp. and Capsaicinoids

Biological Properties, Bioactive Constituents, and Pharmacokinetics of Some Capsicum spp. and Capsaicinoids

Bioavailability of capsaicin and its implications for drug delivery

Capsaicin is a New Gastrointestinal Mucosal Protecting Drug Candidate in Humans — Pharmaceutical Development and Production Based on Clinical Pharmacology

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