LLDT-288, a novel triptolide analogue exhibits potent antitumor activity in vitro and in vivo
文献类型：期刊论文
| 作者 | Xu, Hongtao1,3; Fan, Xiaoting2,3; Zhang, Guanjun4; Liu, Xiaoyu3; Li, Zhihong3; Li, Yuanchao1; Jiang, Biao3 |
| 刊名 | BIOMEDICINE & PHARMACOTHERAPY
 |
| 出版日期 | 2017-09 |
| 卷号 | 93页码:1004-1009 |
| 关键词 | Triptolide Natural products Drug-resistance CYP |
| ISSN号 | 0753-3322 |
| DOI | 10.1016/j.biopha.2017.06.041 |
| 文献子类 | Article |
| 英文摘要 | (14S)-14 beta-(1-(2-morpholinoethyl)-1H-indazol-5-ylamino) mthylepitriptolide (LLDT-288) was a novel C14 beta-heterocycle aminomethyl substituent triptolide analogue, which showed comparable cytotoxicity to triptolide. Here we demonstrated that LLDT-288 displayed broad-spectrum, potent antitumor activity, effectively against drug-resistance cancer cells, and induced apoptosis in vitro, but exerted low toxicity. Moreover, it exhibited a remarkable microsomal stability, and showed no inhibitory effects on different cytochrome P450 isoforms. In vivo, orally administration of LLDT-288 exhibits promising efficacy in human prostate (PC-3) xenograft mice model with obviously low toxicity. Further, the in vivo metabolic studies suggested that LLDT-288 was extensively metabolized in rats and mainly excreted in the form of metabolites in the feces. (C) 2017 Published by Elsevier Masson SAS. |
| WOS关键词 | PANCREATIC-CANCER CELLS ; ANTICANCER ACTIVITY ; TRIPTERYGIUM-WILFORDII ; SIGNALING PATHWAY ; RESISTANCE ; TRIPDIOLIDE ; TRIPTONIDE ; INHIBITION ; ACTIVATION ; APOPTOSIS |
| 资助项目 | National Natural Science Foundation of NFSC, China[21502114] ; China Postdoctoral Science Foundation, China[2015M581677] ; Open Foundation of the State Key Laboratory of Drug Research, China[SIMM1601KF-05] |
| WOS研究方向 | Research & Experimental Medicine ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000407923000109 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272510]  |
| 专题 | 药物化学研究室 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 | Li, Yuanchao; Jiang, Biao |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Biochem & Cell Biol, Shanghai 200031, Peoples R China 3.ShanghaiTech Univ, Shanghai Inst Adv Immunochem Studies, Shanghai 201210, Peoples R China; 4.Tianjin Univ Sci & Technol, Coll Chem Engn & Mat Sci, Tianjin 300457, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Xu, Hongtao,Fan, Xiaoting,Zhang, Guanjun,et al. LLDT-288, a novel triptolide analogue exhibits potent antitumor activity in vitro and in vivo[J]. BIOMEDICINE & PHARMACOTHERAPY,2017,93:1004-1009. |
| APA | Xu, Hongtao.,Fan, Xiaoting.,Zhang, Guanjun.,Liu, Xiaoyu.,Li, Zhihong.,...&Jiang, Biao.(2017).LLDT-288, a novel triptolide analogue exhibits potent antitumor activity in vitro and in vivo.BIOMEDICINE & PHARMACOTHERAPY,93,1004-1009. |
| MLA | Xu, Hongtao,et al."LLDT-288, a novel triptolide analogue exhibits potent antitumor activity in vitro and in vivo".BIOMEDICINE & PHARMACOTHERAPY 93(2017):1004-1009. |
入库方式： OAI收割
来源：上海药物研究所
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