Antitumor activity of a novel series of alpha-aryloxy-alpha-methylhydrocinnamic acid derivatives as PPAR gamma agonists against a panel of human cancer cell lines
文献类型：期刊论文
| 作者 | Xiong, Xishan2; Ye, Yangliang1 ; Fu, Lili2; Dai, Bing2; Liu, Jieqiong2; Jia, Jieshuang2; Tang, Jing1; Li, Lin2; Wang, Li2; Shen, Jianhua1
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| 刊名 | INVESTIGATIONAL NEW DRUGS
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| 出版日期 | 2009-06 |
| 卷号 | 27期号:3页码:223-232 |
| 关键词 | Peroxisome proliferator-activated receptor gamma alpha-aryloxy-alpha-methylhydrocinnamic acid derivative A549 IC50 Apoptosis Cell cycle |
| ISSN号 | 0167-6997 |
| DOI | 10.1007/s10637-008-9161-0 |
| 文献子类 | Article |
| 英文摘要 | Peroxisome proliferator-activated receptor gamma (PPAR gamma) agonists have shown benefit in treating diabetes mellitus, atherosclerosis and cancer. However, widespread use of thiazolidinediones (TZDs), the clinically used synthetic PPAR gamma agonists, has been limited by adverse cardiovascular effects. Consequently, numerous novel non-TZD compounds were synthesized and antidiabetic efficacy was evaluated to identify PPAR gamma agonists for potential clinical use. On the other hand, many studies have documented that the antitumor activity of PPAR gamma agonists is PPAR gamma independent. Here we hypothesized that there might exist some compounds with less PPAR gamma agonistic activity or antidiabetic efficacy but potent antitumor activity. In this study, we evaluated the PPAR gamma agonistic and antitumor activity of several newly synthesized alpha-aryloxy-alpha-methylhydrocinnamic acid derivatives as PPAR gamma agonists in a panel of human cancer cell lines, which showed promising antitumor activity without appreciable PPAR gamma agonistic activity. The results of MTT assay revealed that cell viability was inhibited in a dose dependent manner with IC50 17.1-55.1 mu M for all the novel compounds and rosiglitazone (17.2-165 mu M). They induced cell cycle arrest and apoptosis tested by Flow Cytometry. In conclusion, our findings demonstrate that these compounds have potent in vitro cytotoxicity, the possible mechanism of which is through induction of apoptosis and cell cycle arrest. |
| WOS关键词 | ACTIVATED-RECEPTOR-GAMMA ; DIFFERENTIATED THYROID-CANCER ; HUMAN PROSTATE-CANCER ; PHASE-II TRIAL ; MYOCARDIAL-INFARCTION ; LUNG-CANCER ; ROSIGLITAZONE ; APOPTOSIS ; PROLIFERATION ; PIOGLITAZONE |
| 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:000265040900004 |
| 出版者 | SPRINGER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279227]  |
| 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.Chinese Acad Sci, Drug Discovery & Design Ctr, State Key Lab Drug Res, Shanghai Inst Mat Med,Grad Sch Chinese Acad Sci, Shanghai 201203, Peoples R China 2.Second Mil Med Univ, Changzheng Hosp, Nephrol Inst PLA, Dept Internal Med, Shanghai 200003, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Xiong, Xishan,Ye, Yangliang,Fu, Lili,et al. Antitumor activity of a novel series of alpha-aryloxy-alpha-methylhydrocinnamic acid derivatives as PPAR gamma agonists against a panel of human cancer cell lines[J]. INVESTIGATIONAL NEW DRUGS,2009,27(3):223-232. |
| APA | Xiong, Xishan.,Ye, Yangliang.,Fu, Lili.,Dai, Bing.,Liu, Jieqiong.,...&Mei, Changlin.(2009).Antitumor activity of a novel series of alpha-aryloxy-alpha-methylhydrocinnamic acid derivatives as PPAR gamma agonists against a panel of human cancer cell lines.INVESTIGATIONAL NEW DRUGS,27(3),223-232. |
| MLA | Xiong, Xishan,et al."Antitumor activity of a novel series of alpha-aryloxy-alpha-methylhydrocinnamic acid derivatives as PPAR gamma agonists against a panel of human cancer cell lines".INVESTIGATIONAL NEW DRUGS 27.3(2009):223-232. |
入库方式： OAI收割
来源：上海药物研究所
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