Do anthocyanins and anthocyanidins, cancer chemopreventive pigments in the diet, merit development as potential drugs?

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 of 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.

Anthocyanins as Functional Food Factors— Chemistry, Nutrition and Health Promotion —

“…Cancer The preventive and suppressive effects of anthocyanins on cancer have been demonstrated in many studies, and key findings in this area can be found in the literature (Thomasset et al, 2009;Prasad et al, 2010). In general, anthocyanins suppress inflammatory pathways associated with cancer pathogenesis.…”

Combining naturally occurring polyphenols with TNF-related apoptosis-inducing ligand: a promising approach to kill resistant cancer cells?

“…They are generally found in nature as glycosides, called anthocyanins, and are responsible for the blue, red, or purple colors of plants. Anthocyanin-rich extracts demonstrated chemopreventive activities against cancer in animal models of carcinogenesis [50]. Single agents have been tested in in vitro models and have shown interesting anti-proliferative and proapoptotic properties, acting by modulating survival pathways such as NFjB [51] or MAPK [52].…”

Antioxidant Capacity of Anthocyanin Pigments

“…Some studies specify the anticarcinogenic effect of anthocyanins [12,13,19,111,112,[133][134][135]. They inhibit the growth of carcinogenic cells that provoke colon cancer, induce the apoptosis effect, have the capacity to inhibit in vitro the growth of cells that cause tumours in humans and are even able to act as modulators of the macrophages in the immune response [89,112].…”