論文 - 詳細
| RRC ID | 63029 |
|---|---|
| 著者 | Hiromi I, Nakata S, Uenishi J. |
| タイトル | Up-regulation of Death Receptor 5/TRAIL-R2 Mediates Apoptosis Induced by N,N'-[(3,4-dimethoxyphenyl)methylene] Biscinnamide in Cancer Cells. |
| ジャーナル | Anticancer Res |
| Abstract |
BACKGROUND/AIM:Based on the cytotoxic agent (-)-zampanolide, N,N'-(arylmethylene)bisamides were designed and synthesized as candidate anti-cancer agents. Among them, N,N'-[(3,4-dimethoxyphenyl)methylene]biscinnamide (DPMBC) was identified as the most potent cytotoxic analog against cancer cells. In this study, we investigated the mechanisms underlying DPMBC-induced cell death in HL-60 human promyelocytic leukemia and PC-3 human prostate cancer cells. MATERIALS AND METHODS:Cell growth was assessed by the WST-8 assay. Induction of apoptosis was assessed by nuclear morphology, DNA ladder formation, and flow cytometry using Annexin V staining. Activation of factors in the apoptotic signaling pathway was assessed by western blot analyses. Knockdown of death receptor 5 (DR5) was performed using siRNA. RESULTS:DPMBC up-regulated expression levels of DR5 protein and induced apoptosis through the extrinsic apoptotic pathway mediated by DR5 and caspases. CONCLUSION:DPMBC is an extrinsic apoptosis inducer, which has potential as a therapeutic agent for cancer therapy. |
| 巻・号 | 40(9) |
| ページ | 5035-5041 |
| 公開日 | 2020-9-1 |
| DOI | 10.21873/anticanres.14506 |
| PII | 40/9/5035 |
| PMID | 32878791 |
| MeSH | Antineoplastic Agents / chemistry Antineoplastic Agents / pharmacology* Apoptosis / drug effects* Apoptosis / genetics* Caspases / metabolism Cell Line, Tumor Cell Proliferation / drug effects DNA Fragmentation Dose-Response Relationship, Drug Gene Expression Regulation, Neoplastic / drug effects* Humans Macrolides / chemistry Macrolides / pharmacology* Molecular Structure RNA, Small Interfering / genetics Receptors, TNF-Related Apoptosis-Inducing Ligand / genetics* Receptors, TNF-Related Apoptosis-Inducing Ligand / metabolism |
| IF | 1.994 |
| リソース情報 | |
| ヒト・動物細胞 | HL-60(RCB3683) PC-3(RCB2145) |