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抗疟药物概述:发现、作用模式和耐药性。

An Overview of Available Antimalarials: Discovery, Mode of Action and Drug Resistance.

机构信息

School of pharmaceutical sciences, Nanjing Tech University, No. 30 South Puzhu Road, Nanjing 211816, China.

College of Biotechnology and pharmaceutical Engineering, Nanjing Tech University, No. 30 South Puzhu Road, Nanjing 211816, China.

出版信息

Curr Mol Med. 2020;20(8):583-592. doi: 10.2174/1566524020666200207123253.

Abstract

Malaria is one of the three most deadly infectious diseases in the world and seriously endangers human health and life. To reduce the public health burden of this disease, scientists have focused on the discovery and development of effective antimalarial drugs, from quinine and chloroquine to antifolates and artemisinin and its derivatives, which all play a profound role in the treatment of malaria. However, drugresistant strains of Plasmodium falciparum have emerged due to frequent use of antimalarials and have become increasingly resistant to existing antimalarial drugs, causing disastrous consequences in the world. In particular, artemisinin resistance is of greatest concern which was reported in 2008. Resistance to artenisinins has been a major obstacle for malaria control, and current efforts to curb artemisinin resistance have not been successful. Based on the current situation, it is urgent to develop more effective new antimalarials with distinct targets from conventional antimalarials in the world, which could facilitate to minimize the phenomenon of drug resistance. This review aims to summarize different kinds of antimalarial therapeutic efficacy, mechanisms of action and resistance, and proposes new solutions aiming towards further improvement of malaria elimination.

摘要

疟疾是世界上三大最致命的传染病之一,严重威胁人类健康和生命。为了降低这种疾病对公众健康的负担,科学家们一直致力于发现和开发有效的抗疟药物,从奎宁和氯喹到抗叶酸类药物和青蒿素及其衍生物,这些药物在治疗疟疾方面都发挥了深远的作用。然而,由于抗疟药物的频繁使用,恶性疟原虫的耐药株已经出现,并且对现有抗疟药物的耐药性越来越强,在世界范围内造成了灾难性的后果。特别是,青蒿素耐药性是最令人担忧的,这在 2008 年就有报道。抗青蒿素药物的耐药性一直是疟疾控制的主要障碍,目前遏制青蒿素耐药性的努力并没有成功。基于目前的情况,迫切需要开发出比世界上传统抗疟药物更有效的新抗疟药物,以减少耐药性现象。本综述旨在总结不同类型的抗疟药物的治疗效果、作用机制和耐药性,并提出新的解决方案,以进一步改善疟疾的消除。

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