20(S)-Protopanaxadiol (PPD) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs
文献类型：期刊论文
| 作者 | Liu, Junhua1; Wang, Xu2; Liu, Peng1; Deng, Rongxin2; Lei, Min1 ; Chen, Wantao2; Hu, Lihong1
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2013-07-15 |
| 卷号 | 21期号:14页码:4279-4287 |
| 关键词 | 20(S)-Protopanoxadiol Multidrug resistant P-glycoprotein Chemosensitizer Structure-activity relationship |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2013.04.067 |
| 文献子类 | Article |
| 英文摘要 | Novel 20(S)-protopanoxadiol (PPD) analogues were designed, synthesized, and evaluated for the chemosensitizing activity against a multidrug resistant (MDR) cell line (KBvcr) overexpressing P-glycoprotein (P-gp). Structure-activity relationship analysis showed that aromatic substituted aliphatic amine at the 24-positions (groups V) effectively and significantly sensitized P-gp overexpressing multidrug resistant (MDR) cells to anticancer drugs, such as docetaxel (DOC), vincristine (VCR), and adriamycin (ADM). PPD derivatives 12 and 18 showed 1.3-2.6 times more effective reversal ability than verapamil (VER) for DOC and VCR. Importantly, no cytotoxicity was observed by the active PPD analogues (5 mu M) against both non-MDR and MDR cells, suggesting that PPD analogues serve as novel lead compounds toward a potent and safe resistance modulator. Moreover, a preliminary mechanism study demonstrated that the chemosensitizing activity of PPD analogues results from inhibition of P-glycoprotein (P-gp) overexpressed in MDR cancer cells. (C) 2013 The Authors. Published by Elsevier Ltd. All rights reserved. |
| WOS关键词 | GINSENG ; TRANSPORTER ; INHIBITOR ; REVERSAL ; EXTRACT ; BINDING ; MODEL |
| 资助项目 | National Natural Science Foundation of China[30925040] ; National Natural Science Foundation of China[81102329] ; National Natural Science Foundation of China[81273397] ; Chinese National Science Technology Major Project 'Key New Drug Creation and Manufacturing Program'[2013ZX09508104] ; Chinese National Science Technology Major Project 'Key New Drug Creation and Manufacturing Program'[2012ZX09301001-001] ; Chinese National Science Technology Major Project 'Key New Drug Creation and Manufacturing Program'[2011ZX09307-002-03] ; Science Foundation of Shanghai[12XD1405700] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000320838200034 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277539]  |
| 专题 | 上海中药现代化研究中心 |
| 通讯作者 | Chen, Wantao |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Res Ctr Modernizat Tradit Chinese Med, Shanghai 201203, Peoples R China; 2.Shanghai Jiao Tong Univ, Sch Med, Peoples Hosp 9, Dept Oral & Maxillofacial Head & Neck Oncol, Shanghai 200011, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu, Junhua,Wang, Xu,Liu, Peng,et al. 20(S)-Protopanaxadiol (PPD) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2013,21(14):4279-4287. |
| APA | Liu, Junhua.,Wang, Xu.,Liu, Peng.,Deng, Rongxin.,Lei, Min.,...&Hu, Lihong.(2013).20(S)-Protopanaxadiol (PPD) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs.BIOORGANIC & MEDICINAL CHEMISTRY,21(14),4279-4287. |
| MLA | Liu, Junhua,et al."20(S)-Protopanaxadiol (PPD) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs".BIOORGANIC & MEDICINAL CHEMISTRY 21.14(2013):4279-4287. |
入库方式： OAI收割
来源：上海药物研究所
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