Evaluation of chemopreventive effects in colitis-associated colon tumourigenesis and oral toxicity of the lipophilic epigallocatechin gallate-docosahexaenoic acid

• EGCG-DHA (50 m/kg) appears to be a more potent chemopreventive agent than EGCG.
• EGCG-DHA shows less toxicity than EGCG in a 28-day subchronic study in mice.
• Structurally modified EGCG may render additional or synergistic health benefits.

The present study aimed to investigate and compare the anti-cancer effects and toxicity of epigallocatechin-3-gallate (EGCG) and epigallocatechin-3-gallate-docosahexaenoic acid (EGCG-DHA). Our results indicate that dietary oral administration of EGCG-DHA was more effective than EGCG and epigallocatechin-3-gallate-stearic acid (EGCG-SA) in reducing the colon weight to colon length (W/L) ratio and tumour multiplicity. In subchronic toxicity study, the mortality was 0, 40, 100, 0 and 40% in the control, EGCG 0.5 g/kg, EGCG 1 g/kg, EGCG-DHA 0.5 g/kg or EGCG-DHA 1 g/kg treatment groups, respectively. Oral administration of EGCG or EGCG-DHA resulted in changes to organ weight, body weight, and haematological parameters. However, histological tissue sections revealed no abnormal pathological changes in major organs. Overall, our findings suggest that low concentrations of EGCG-DHA (50 mg/kg) provide a safe and potent health-promoting dietary supplement than EGCG itself for further development of a chemopreventive agent. However, clinical trials are suggested to verify this study.

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