Synthesis of 86 species of 1,5-diaryl-3-oxo-1,4-pentadienes analogs of curcumin can yield a good lead in vivo

Chieko Kudo, Hiroyuki Yamakoshi, Atsuko Sato, Hiroshi Nanjo, Hisatsugu Ohori, Chikashi Ishioka, Yoshiharu Iwabuchi, Hiroyuki Shibata

Research output: Contribution to journalArticle

30 Citations (Scopus)

Abstract

Background: Curcumin is known to possess many anti-tumor properties such as inhibition of tumor growth and induction of apotosis. However, limited bioavailability of curcumin prevents its clinical application. A synthesized curcumin analog, 1,5-diaryl-3-oxo-1,4-pentadiene such as GO-Y030, has the improved anti-tumor potential in vitro as well as in mouse model of colorectal carcinogenesis.Results: These compounds were divided into two groups; one is the higher anti-proliferative group, in which 79.7% of 1,5-diaryl-3-oxo-1,4-pentadienes were clustered. One of the 1,5-diaryl-3-oxo-1,4-pentadiene analogs, GO-Y078 has the most enhanced growth inhibition, and its solubility was improved, compared with curcumin. GO-Y078 inhibits NF-κB transactivation, as well as expression of TP53 and DR5 more effectively than curcumin. In a mouse model, GO-Y078 presented 1.4 fold more survival elongation that was not achieved by curcumin and GO-Y030.Conclusions: The 1,5-diaryl-3-oxo-1,4-pentadiene analogs can yield good lead compounds for cancer chemotherapy, to overcome low bioavailability of curcumin.

Original languageEnglish
Article number4
JournalBMC Pharmacology
Volume11
DOIs
Publication statusPublished - 2011 May 28

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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