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Curcumin Analogues with Enhanced Antitumor Activities


Enhanced Antitumor Activities
Strong Multi-Target Inhibitory Activities
Increased Bioavailability
Improved Water Solubility (GO-Y078; H1525)

Curcumin, a dietary constituent of turmeric, has chemopreventive and chemotherapeutic potentials against various types of cancers, but low bioavailability prevents its use in chemotherapeutic applications. GO-Y030 [B4823] and GO-Y078 [H1525] are new synthetic analogues of curcumin, developed by Shibata, Iwabuchi et al. to increase its potential and circumvent its low bioavailability.
According to their reports, B4823 shows a 30-fold greater suppression of tumor cell growth compared with curcumin.1) B4823 inhibits signal transducers and activators of transcription 3 (STAT3)2,3) and IKKβ kinase4), and suppresses tumor growth of cancer stem cells.3) B4823 and H1525 suppress the growth of myeloma cells, and are 7 to 12 times more effective than curcumin.5) B4823 and H1525 are also 6- to 15-fold stronger multi-target inhibitors of NF-κB, PI3K/AKT, JAK/STAT3 and IRF4 pathways than curcumin.5) H1525 also potently inhibits interleukin 6 (IL-6) production 14-fold more than curcumin5), and inhibits tumor angiogenesis through actin disorganization.6) In addition, H1525 has the additional characteristics of improved water solubility (H1525: 1.07 mg/L, curcumin: 0.54 mg/L) and effectiveness in a mouse model of gastric cancer.7) Furthermore, the structure activity relationships of these compounds have been reported.8)