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⁾

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Products

B4823

GO-Y030

H1525

GO-Y078

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Advantages

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

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References

• 1) Newly synthesized curcumin analog has improved potential to prevent colorectal carcinogenesis in vivo
  • H. Shibata, H. Yamakoshi, A. Sato, H. Ohori, Y. Kakudo, C. Kudo, Y. Takahashi, M. Watanabe, H. Takano, C. Ishioka, T. Noda, Y. Iwabuchi, Cancer Sci. 2009, 100, 956.
• 2) Curcumin analogue GO-Y030 inhibits STAT3 activity and cell growth in breast and pancreatic carcinomas
  • B. Hutzen, L. Friedman, M. Sobo, L. Lin, L. Cen, S. De Angelis, H. Yamakoshi, H. Shibata, Y. Iwabuchi, J. Lin, Int. J. Oncol. 2009, 35, 867.
• 3) Targeting colon cancer stem cells using a new curcumin analogue, GO-Y030
  • L. Lin, Y. Liu, H. Li, P.-K. Li, J. Fuchs, H. Shibata, Y. Iwabuchi, J. Lin, Br. J. Cancer 2011, 105, 212.
• 4) Curcumin analog GO‐Y030 is a novel inhibitor of IKKβ that suppresses NF‐κB signaling and induces apoptosis
  • A. Sato, C. Kudo, H. Yamakoshi, Y. Uehara, H. Ohori, C. Ishioka, Y. Iwabuchi, H. Shibata, Cancer Sci. 2011, 102, 1045.
• 5) Novel Curcumin Analogs, GO-Y030 and GO-Y078, Are Multi-targeted Agents with Enhanced Abilities for Multiple Myeloma
  • C. Kudo, H. Yamakoshi, A. Sato, H. Ohori, C. Ishioka, Y. Iwabuchi, H. Shibata, Anticancer Res. 2011, 31, 3719.
• 6) A Curcumin Analog, GO-Y078, Effectively Inhibits Angiogenesis through Actin Disorganization
  • S. Sugiyama, Y. Yoshino, S. Kuriyama, M. Inoue, K. Komine, K. Otsuka, A. Kohyama, H. Yamakoshi, C. Ishioka, M. Tanaka, Y. Iwabuchi, H. Shibata, Anti-Cancer Agents Med. Chem. 2016, 16, 633.
• 7) Synthesis of 86 species of 1,5-diaryl-3-oxo-1,4-pentadienes analogs of curcumin can yield a good lead in vivo
  • C. Kudo, H. Yamakoshi, A. Sato, H. Nanjo, H. Ohori, C. Ishioka, Y. Iwabuchi, H. Shibata, BMC Pharmacol. 2011, 11, 4.
• 8) Structure-Activity Relationships of the Antitumor C5-Curcuminoid GO-Y030
  • A. Kohyama, H. Yamakoshi, S. Hongo, N. Kanoh, H. Shibata, Y. Iwabuchi, Molecules 2015, 20, 15374.

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Related Products

C0434

Curcumin (Natural)

C2302

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Related Product Category Pages

• Antitumor Ingredients (for Research and Experimental Use)
• Cancer Research

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Product Brochure

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For Laboratory Use, Research Purposes Only