Novel niclosamide-derived adjuvants elevating the efficacy of polymyxin B against MDR Pseudomonas aeruginosa DK2
文献类型：期刊论文
| 作者 | Lu, Taotao1; Zheng, Xinyu1; Mao, Fei1; Cao, Qiao2; Cao, Qin2; Zhu, Jin1; Li, Xiaokang1; Lan, Lefu2 ; Li, Baoli3; Li, Jian1,3,4,5
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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| 出版日期 | 2022-06-05 |
| 卷号 | 236页码:114318 |
| ISSN号 | 0223-5234 |
| 关键词 | Pseudomonas aeruginosa DK2 Polymyxin B Niclosamide Adjuvants Drug repurposing |
| DOI | 10.1016/j.ejmech.2022.114318 |
| 文献子类 | Article |
| 英文摘要 | Pseudomonas aeruginosa (P. aeruginosa) DK2 is a multidrug-resistant (MDR) gram-negative bacterial pathogen, being observed serious resistance to the 'last-resort' antibiotic, polymyxin B (PB). Combination therapies with adjuvants have emerged as effective strategies to reactivate the antibiotics resisted by MDR bacteria. Herein, we screened a library of approved drugs and found that niclosamide (NIC), an anthelmintic drug, could potentiate the efficacy of PB against MDR P. aeruginosa DK2. Next, a series of novel NIC-derived adjuvants were designed, synthesized, and evaluated the synergistic activity with PB. Among them, the combination of 15 with PB displayed superior elimination of P. aeruginosa DK2 in vitro and in vivo compared with the single administration. Moreover, this combination decelerated PB-resistance progress in DK2, along with lower potential toxicity. Overall, this study provides a strategy for development antibiotic adjuvants to potentiate PB against MDR P. aeruginosa infections. (C) 2022 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | RESISTANCE ; COLISTIN ; POTENTIATION ; ANTIBIOTICS ; MUTATIONS ; INFECTION ; DYNAMICS ; HYBRIDS ; AGENTS ; PMRB |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| WOS记录号 | WOS:000821147500004 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/309352]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Lan, Lefu; Li, Baoli; Li, Jian |
| 作者单位 | 1.East China Univ Sci & Technol, Shanghai Frontiers Sci Ctr Optogenet Tech Cell Me, Frontiers Sci Ctr Materiobiol & Dynam Chem,Shangh, Sch Pharm,State Key Lab Bioreactor Engn & New Dru, Shanghai 200237, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 3.Hainan Univ, Coll Pharm, Key Lab Trop Biol Resources, Minist Educ, Haikou 570228, Hainan, Peoples R China; 4.Dali Univ, Coll Pharm, Yunnan Key Lab Screening & Res Antipathogen Plant, Dali 671000, Peoples R China; 5.Tongji Univ, Clin Med Sci & Tech Innovat Ctr, Shanghai Peoples Hosp 10, Sch Med, Shanghai 200092, Peoples R China |
| 推荐引用方式 GB/T 7714 | Lu, Taotao,Zheng, Xinyu,Mao, Fei,et al. Novel niclosamide-derived adjuvants elevating the efficacy of polymyxin B against MDR Pseudomonas aeruginosa DK2[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2022,236:114318. |
| APA | Lu, Taotao.,Zheng, Xinyu.,Mao, Fei.,Cao, Qiao.,Cao, Qin.,...&Li, Jian.(2022).Novel niclosamide-derived adjuvants elevating the efficacy of polymyxin B against MDR Pseudomonas aeruginosa DK2.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,236,114318. |
| MLA | Lu, Taotao,et al."Novel niclosamide-derived adjuvants elevating the efficacy of polymyxin B against MDR Pseudomonas aeruginosa DK2".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 236(2022):114318. |
入库方式： OAI收割
来源：上海药物研究所
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