Reactive oxygen species activated by mitochondria-specific camptothecin prodrug for enhanced chemotherapy
| Title: | Reactive oxygen species activated by mitochondria-specific camptothecin prodrug for enhanced chemotherapy |
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| Authors: | Zhaopei Guo, Zian Wang, Ruifeng Liang, Huayu Tian, Xuesi Chen, Meiwan Chen |
| Source: | Biomolecules & Biomedicine, Vol 22, Iss 6 (2022) |
| Publisher Information: | Association of Basic Medical Sciences of Federation of Bosnia and Herzegovina, 2022. |
| Publication Year: | 2022 |
| Collection: | LCC:Biology (General) |
| Subject Terms: | Camptothecin prodrug, reactive oxygen species, antitumor therapy, Biology (General), QH301-705.5 |
| More Details: | Camptothecin (CPT) has attracted much attention due to its potent antitumor activities. However, the undesirable physicochemical properties, including poor water-solubility, unstable lactone ring and severe adverse effects limit its further application. In this study, two water-soluble prodrugs, CPT-lysine (CPTK) and CPT-arginine (CPTR), were designed and synthesized by conjugating lysine or arginine with CPT, improving its solubility, pharmacokinetic properties and tumor penetration. Importantly, the introduction of arginine into CPTR contributed to the mitochondria-specific delivery, which increased mitochondrial reactive oxygen species (ROS) generation, induced mitochondria dysfunction and enhanced cell apoptosis and in vivo anti-cancer effect. This strategy is believed to hold great potential for organelle-specific synergistic anti-tumor therapy. |
| Document Type: | article |
| File Description: | electronic resource |
| Language: | English |
| ISSN: | 2831-0896 2831-090X |
| Relation: | https://www.bjbms.org/ojs/index.php/bjbms/article/view/7194; https://doaj.org/toc/2831-0896; https://doaj.org/toc/2831-090X |
| DOI: | 10.17305/bjbms.2022.7194 |
| Access URL: | https://doaj.org/article/f7b8cad552b34e1d814313e7cc55d505 |
| Accession Number: | edsdoj.f7b8cad552b34e1d814313e7cc55d505 |
| Database: | Directory of Open Access Journals |
| ISSN: | 28310896 2831090X |
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| DOI: | 10.17305/bjbms.2022.7194 |
| Published in: | Biomolecules & Biomedicine |
| Language: | English |