Curcumin Analogs with Enhanced Antitumor Activities

Turmeric containing curcumin, a yellow dye, has been used as a South Asian traditional medicine for hepatobiliary disorders, inflammation, and wound healing. Curcumin has anti-proliferative, cancer-chemopreventive, anti-angiogenic, and anti-oxidant effects. However, its low bioavailability causes limitations of its application to chemotherapy.
GO-Y030 and GO-Y078 are synthetic analogs of curcumin, develoa hped by Shibata, Iwabuchi et al. to increase the antitumor potential and improve the bioavailability.^2,3) The assays on various cancer cell lines revealed that GO-Y030 and GO-Y078 suppress tumor cell growth and control the growth-related molecules such as NF-κB, β-catenin, STAT3, c-Myc and IRF-4.^4,5) It has been reported that they inhibit in vivo cancer cell growth in a mouse model of gastric cancer and GO-Y078 having a twice higher water-solubility than curcumin is even more effective.⁵⁾