Background: The plant origin capsaicinoids (capsaicin, dihydrocapsaicin, norcapsaicin, dihydrocapsaicin, homocapsaicin, homodihydrocapsaicin) are well known and used as nutritional additive agents in the every day nutritional practice from the last 9,500 years; however, we had have a very little scientifically based knowledge on their chemistry, physiology and pharmacology in animal observations, and in humans up to the mid-twentieth century. Our knowledge about their chemistry, physiology, pharmacology entered to be scientifically based evidence from the year 1980, dominantly in animal observations. The human observations with capsaicin (capsaicinoids), in terms of good clinical practice, have been started only in the last 10-year period (from 1997) in randomized, prospective, multiclinical studies. The name of "capsaicin" used only in the physiological and pharmacological research both in animal experiments and in human observation. The "capsaicin" (as a "chemically" used natural compound) modifies the so-called capsaicin-sensitive afferent nerves depending on their applied doses.
Aims: The specific action of capsaicin (capsaicinoids) on sensory afferent nerves modifying gastrointestinal (GI) function (under very specific conditions) offers a possibility for the production of an orally applicable drug or for other drug combinations, which can be used in the human medical therapy. The production of new drug is based on the critical interdisciplinary review of the results obtained with capsaicinoids.
Materials and methods: This paper gives an interdisciplinary and critical overview on the chemical, physiological, pharmacological and toxicological actions of the natural origin capsaicinoids (from the point of drug production) under conditions of acute, subacute and chronic administration in animal experiments and human observations, toxicology, pharmacokinetics). This interdisciplinary review covers the following main chapters: (1) physiological and pharmacological research tool by capsaicin in the animals and human beings, (2) capsaicin research in animals (including the acute, subacute toxicology and chronic toxicology metabolism, genotoxicology), (3) capsaicin observation with capsaicin in human beings.
Conclusion: (1) The capsaicin used in the physiological and pharmacological observations (in animals and human beings) chemically represents different chemical compounds, which can be obtained from the plants (paprika, chilli, etc.), (2) capsaicinoids are able to modify the capsaicin-sensitive afferent nerves, which have principle roles in the defence of different organs (including the gastrointestinal tract [against the different chemicals, heat, strech, chemical millieu-induced damage], (3) the application of capsaicin (capsaicinoids) can be repeated for the beneficial effects on the gastrointestinal tract as those in animal experiments. After this interdisciplinary and critical review, this paper demonstrates the well-planned research pathways of the discoveries of capsaicinoids from plant chemistry, via physiology, pharmacology and toxicology in animal experiments and human observations.