Reference - Detail
| RRC ID | 38620 |
|---|---|
| Author | Kudo C, Yamakoshi H, Sato A, Nanjo H, Ohori H, Ishioka C, Iwabuchi Y, Shibata H. |
| Title | Synthesis of 86 species of 1,5-diaryl-3-oxo-1,4-pentadienes analogs of curcumin can yield a good lead in vivo. |
| Journal | BMC Pharmacol |
| 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. |
| Volume | 11 |
| Pages | 4 |
| Published | 2011-5-28 |
| DOI | 10.1186/1471-2210-11-4 |
| PII | 1471-2210-11-4 |
| PMID | 21619659 |
| PMC | PMC3115866 |
| MeSH | Alkadienes / chemical synthesis* Alkadienes / pharmacology Alkadienes / therapeutic use Animals Antineoplastic Agents / chemical synthesis* Antineoplastic Agents / pharmacology Antineoplastic Agents / therapeutic use Apoptosis / drug effects Cell Line, Tumor Curcumin / analogs & derivatives* Curcumin / chemical synthesis Curcumin / pharmacology Curcumin / therapeutic use Drug Evaluation, Preclinical Humans Mice Mice, Inbred C57BL Solubility |
| IF | 1.771 |
| Resource | |
| Human and Animal Cells | HuCCT1(RCB1960) SH-10-TC(RCB1940) A431 |