Our group has been studying the chemoprotective effects of flavonoids for many years.  This presentation will present an overview of our research on anthocyanin biological activity. By screening a variety of edible anthocyanin sources for chemopreventive activity, we found that anthocyanin-rich extract from plant materials with different and distinctive anthocyanin pro?les currently used or potential food  natural colorants including chokeberry, elderberry, bilberry, grape, purple carrot, purple corn, red radish, and eggplant exhibited colon cancer cell chemoprotective activity. Those anthocyanins showed an additive effect between anthocyanins with other phenolics from the same plant sources as chemoprotective agents.A comprehensive statistical comparison of anthocyanins with various structure patterns demonstrated that glycosylation and acylation pattern have important impact on their biological activity in a HT-29 cell model.Computer simulation was used to predict the bioactivity of anthocyanin or their conjugated phenolic acids based on their structure properties. A 3D-QSAR model was established to predict anthocyanins/phenolic acids with high radical scavenging activity to understand their structure-activity relationships. With aid of contour maps, the structural characteristics of anthocyanins/ phenolics acids favorable for high radical scavenging activity have been elucidated.Pure anthocyanins typically present in fruits and vegetables have been tested for their ability to inhibit gastrointestinal (GI) tumor cell growth including human mouth epidermal carcinoma (KB), esophageal adenocarcinoma cells (TE-1), and colorectal adenocarcinoma cells (HT-29 and HCT-116), and their antioxidant capacity.  We found anthocyanins exhibited selective chemopreventive action on the four GI tract cell lines and worked potent radical scavengers ex vivo via increasing of GSR expression and protecting DNA damage.Our data, combined with data from other laboratories, compiles strong evidence of the GI chemoprotective effects of anthocyanins, and they deserve close attention for in vivo systems. Incorporation of anthocyanins into the diet could be facilitated through their use as food colorants.

Anthocyanin structure-function relationships and their impact on cancer cells

246th National Meeting (2013)

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