Abstract
Anthocyanins, plant pigments in fruits and berries, have been shown to delay cancer development in rodent models of carcinogenesis, especially those of the colorectal tract. Anthocyanins and anthocyanidins, their aglycons, especially cyanidin and delphinidin, have been subjected to extensive mechanistic studies. In cells in vitro, both glycosides and aglycons engage an array of anti-oncogenic mechanisms including anti-proliferation, induction of apoptosis and inhibition of activities of oncogenic transcription factors and protein tyrosine kinases. Anthocyanins and anthocyanidins exist as four isomers, interconversion between which depends on pH, temperature and access to light. Anthocyanidins are much more prone to avid chemical decomposition than the glycosides, and they only survive for minutes in the biophase. These pharmaceutical issues are very important determinants of the suitability of these flavonoids for potential development as cancer chemopreventive drugs, and they have hitherto not received adequate attention. In the light of their robust cancer chemopreventive efficacy in experimental models and their superior stability as compared to that of the aglycons, the anthocyanins seem much more suitable for further drug development than their anthocyanidin counterparts.
Highlights
Epidemiological studies suggest that consumption of certain diets, for example fruits, vegetables and fibre, can reduce the risk of developing cancer
This study identified anthocyanin concentrations in the blood and gastrointestinal tract associated with efficacy
Existence as a mixture of isomers and propensity to undergo extensive metabolism are two properties which militate against the suitability of either anthocyanidins or anthocyanins for development as drugs
Summary
Epidemiological studies suggest that consumption of certain diets, for example fruits, vegetables and fibre, can reduce the risk of developing cancer. Carried away by the enthusiasm generated by a intriguing biochemical property in cells in vitro of the dietary component under study, they often conclude articles describing the novel mechanism to propose that the intervention in question ”...could be developed as agent for the management of cancer...” Such statements are often premature, if not out of place, because pharmacological and pharmaceutical issues including stability, bioavailability and formulatability of the dietary constituent need to be taken into account before it can - even remotely - be considered for further drug development. The present review illustrates these issues focusing on anthocyanins, water-soluble pigments which occur abundantly in fruits and berries, and anthocyanidins, their aglycons It summarizes the evidence for their cancer chemopreventive efficacy and juxtaposes it with their clinical pharmacology and pharmaceutical properties. The objective of the review is to highlight properties of this class of flavonoids which may define generic criteria applicable to the development of dietary agents
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