Cross-Linking of Thiolated Paclitaxel-Oligo(p-phenylene vinylene) Conjugates Aggregates inside Tumor Cells Leads to "Chemical Locks" That Increase Drug Efficacy
文献类型：期刊论文
| 作者 | Zhou, Lingyun1,2; Lv, Fengting1,2; Liu, Libing1,2; Shen, Guizhi3; Yan, Xuehai3; Bazan, Guillermo C.4,5; Wang, Shu1,2 |
| 刊名 | ADVANCED MATERIALS
 |
| 出版日期 | 2018-03-08 |
| 卷号 | 30期号:10 |
| 关键词 | Antitumor Assembly Inside Cells Chemical Locks Drug Resistance Supramolecular Paclitaxel |
| ISSN号 | 0935-9648 |
| DOI | 10.1002/adma.201704888 |
| 英文摘要 | How to reduce the resistance of certain tumor cells to paclitaxel (PTX) and related taxoid anticancer drugs is a major challenge for improving cure rates. An oligo(p-phenylenevinylene) unit with thiol groups and a PTX unit (OPV-S-PTX), which enhances drug efficacy and reverses resistance is thus designed. The mechanism involves diffusion of OPV-S-PTX into the cell, where pi-pi interactions lead to aggregation. Cross-linking of the aggregates via oxidation of thiol groups is favored in tumor cells because of the higher reactive oxygen species (ROS) concentration. Cross-linked aggregates "chemically lock" the multichromophore particle for a more persistent effect. The IC50 of OPV-S-PTX for tumor cell line A549 is reduced down to 0.33 x 10(-9) M from that observed for PTX itself (41 x 10(-9) M). Enhanced efficacy by OPV-S-PTX is proposed to proceed via acceleration of microtubule bundle formation. A549/T-inoculated xenograft mice experiments reveal suppression of tumor growth upon OPV-S-PTX treatment. Altogether, these results show that the internal cross-linking of OPV-S-PTX through ROS provides a means to discriminate between tumor and healthy cells and the formation of the chemically locked particles enhances drug efficacy and helps in reducing resistance. |
| 语种 | 英语 |
| WOS记录号 | WOS:000426720400007 |
| 出版者 | WILEY-V C H VERLAG GMBH |
| 源URL | [http://ir.iccas.ac.cn/handle/121111/45769]  |
| 专题 | 中国科学院化学研究所 |
| 通讯作者 | Yan, Xuehai; Bazan, Guillermo C.; Wang, Shu |
| 作者单位 | 1.Chinese Acad Sci, Beijing Natl Lab Mol Sci, Key Lab Organ Solids, Inst Chem, Beijing 100190, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 3.Chinese Acad Sci, State Key Lab Biochem Engn, Inst Proc Engn, Beijing 100190, Peoples R China 4.Univ Calif Santa Barbara, Dept Chem & Biochem, Ctr Polymers & Organ Solids, Santa Barbara, CA 93106 USA 5.Univ Calif Santa Barbara, Dept Mat, Ctr Polymers & Organ Solids, Santa Barbara, CA 93106 USA |
| 推荐引用方式 GB/T 7714 | Zhou, Lingyun,Lv, Fengting,Liu, Libing,et al. Cross-Linking of Thiolated Paclitaxel-Oligo(p-phenylene vinylene) Conjugates Aggregates inside Tumor Cells Leads to "Chemical Locks" That Increase Drug Efficacy[J]. ADVANCED MATERIALS,2018,30(10). |
| APA | Zhou, Lingyun.,Lv, Fengting.,Liu, Libing.,Shen, Guizhi.,Yan, Xuehai.,...&Wang, Shu.(2018).Cross-Linking of Thiolated Paclitaxel-Oligo(p-phenylene vinylene) Conjugates Aggregates inside Tumor Cells Leads to "Chemical Locks" That Increase Drug Efficacy.ADVANCED MATERIALS,30(10). |
| MLA | Zhou, Lingyun,et al."Cross-Linking of Thiolated Paclitaxel-Oligo(p-phenylene vinylene) Conjugates Aggregates inside Tumor Cells Leads to "Chemical Locks" That Increase Drug Efficacy".ADVANCED MATERIALS 30.10(2018). |
入库方式： OAI收割
来源：化学研究所
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