Antitumor Efficacy of Two Novel Non-Thiazolidinedione Compounds as Peroxisome Proliferator-Activated Receptor-gamma Agonists in Human Osteosarcoma Cells in vitro
文献类型：期刊论文
| 作者 | Fu, Lili3; Xiong, Xishan1; Wang, Li3; Gao, Xiang3; Ye, Yangliang2 ; Jia, Jieshuang3; Hu, Huimin3; Li, Lin3; Shen, Jianhua2; Mei, Changlin3
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| 刊名 | CHEMOTHERAPY
 |
| 出版日期 | 2009 |
| 卷号 | 55期号:6页码:468-476 |
| 关键词 | Cytotoxicity alpha-Aryloxy-alpha-methylhydrocinnamic acid derivative IC50 Osteosarcoma Peroxisome proliferator-activated receptor gamma |
| ISSN号 | 0009-3157 |
| DOI | 10.1159/000265529 |
| 文献子类 | Article |
| 英文摘要 | Background: Due to chemotherapy resistance in osteosarcoma subgroups, the prognosis of these patients is still poor, and the development of new agents is of utmost importance. The aim of our study was to test the antitumor effects of two novel alpha-aryloxy-alpha-methylhydrocinnamic acid derivatives as peroxisome proliferator-activated receptor (PPAR) gamma agonists, together with rosiglitazone, a well-known thiazolidinedione (TZD) acting on several osteosarcoma cell lines. Methods/Results: The MTT assay revealed that cell viability was inhibited in a dose-dependent manner with IC50 6.2-15.8 mu M for the two novel compounds and rosiglitazone (48.4-83.5 mu M). Exposure to DG8 and DH9 at low micromolar concentrations induced a dose-dependent block of DNA synthesis and colony formation. In these antitumor assays, DG8 and DH9 were more effective than rosiglitazone, although the PPAR gamma agonistic activity of rosiglitazone is much higher. The SiRNA approach to downregulate specifically PPAR gamma in U-2OS cells did not affect the cytotoxic efficiency of either the two novel compounds or rosiglitazone. Conclusion: These observations suggest that non-TZDs with less PPAR gamma agonistic activity might show more potent antitumor efficacy independent of PPAR gamma in human osteosarcoma cells, which supports the possibility that they could be beneficial in the treatment of osteosarcoma patients. Copyright (C) 2009 S. Karger AG, Basel |
| WOS关键词 | HUMAN BREAST-CANCER ; PPAR-GAMMA ; PHASE-I ; DIFFERENTIATION ; APOPTOSIS ; LIGANDS ; DESIGN ; AGENTS ; BEXAROTENE ; GROWTH |
| 资助项目 | National 863 Plan in High Technology Progress[2002AA2Z3130] ; National 863 Plan in High Technology Progress[2007AA02Z3Z1] ; Shanghai Leading Academic Discipline Project[B902] |
| WOS研究方向 | Oncology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000272605600012 |
| 出版者 | KARGER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279363]  |
| 专题 | 药物发现与设计中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Mei, Changlin |
| 作者单位 | 1.Acad Mil Med Sci, Dept Nephrol, Affiliated Hosp, Beijing, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, State Key Lab Drug Res,Grad Sch, Shanghai 200031, Peoples R China; 3.Second Mil Med Univ, Div Nephrol, Dept Internal Med, Nephrol Inst PLA,Changzheng Hosp, Shanghai 200003, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Fu, Lili,Xiong, Xishan,Wang, Li,et al. Antitumor Efficacy of Two Novel Non-Thiazolidinedione Compounds as Peroxisome Proliferator-Activated Receptor-gamma Agonists in Human Osteosarcoma Cells in vitro[J]. CHEMOTHERAPY,2009,55(6):468-476. |
| APA | Fu, Lili.,Xiong, Xishan.,Wang, Li.,Gao, Xiang.,Ye, Yangliang.,...&Mei, Changlin.(2009).Antitumor Efficacy of Two Novel Non-Thiazolidinedione Compounds as Peroxisome Proliferator-Activated Receptor-gamma Agonists in Human Osteosarcoma Cells in vitro.CHEMOTHERAPY,55(6),468-476. |
| MLA | Fu, Lili,et al."Antitumor Efficacy of Two Novel Non-Thiazolidinedione Compounds as Peroxisome Proliferator-Activated Receptor-gamma Agonists in Human Osteosarcoma Cells in vitro".CHEMOTHERAPY 55.6(2009):468-476. |
入库方式： OAI收割
来源：上海药物研究所
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