IF 2.9 4区 医学 Q3 CHEMISTRY, MEDICINAL Current topics in medicinal chemistry Pub Date : 2025-02-27 DOI:10.2174/0115680266343676250122062731
Kiran Sharma
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引用次数: 0

摘要

青蒿素及其半合成衍生物是一组生物活性化学物质,主要从青蒿物种的提取物中获得,具有显著的抗疟活性,同时相对安全、可耐受。不过,它们的功效并不局限于疟疾,还可用于多种人类传染病。青蒿素类药物的作用模式主要是通过打破其分子结构中的内过氧化物链节产生自由基,从而有利于消灭微生物物种。青蒿素类药物可抑制细菌、病毒、原生动物、蠕虫和真菌感染。青蒿素类药物的衍生物,如青蒿酮,是一种可逆抑制剂,以病毒复制周期为目标,青蒿琥酯通过抑制早期 EBV 蛋白的产生来抑制 EBV 感染。研究还发现,它们通过产生过氧化物的时间和浓度对幽门螺旋杆菌和结核分枝杆菌非常有效。其他衍生物,如蒿琥酯、蒿甲醚和蒿乙醚,也显示出抗菌活性,可口服、直肠给药、肌肉注射或静脉注射。本综述旨在全面介绍青蒿素及其半合成衍生物以及衍生二聚体/三聚体的最新抗菌应用情况。论文反映了发现新型青蒿素药物的巨大潜力,这些药物可用作各种疾病的辅助治疗。不过,还需要进一步开展转化和实验研究,以优化和建立药代动力学特征。此外,卫生当局还需要对现有的青蒿素类药物和新发现的衍生物进行监管,以确保它们在全球抗击抗生素耐药性的斗争中长期有效。
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A Comprehensive Review on the Antimicrobial Activity of the Genus Artemisia, Artemisinin, and its Derivatives.

Artemisinin and its semisynthetic derivatives are a group of bioactive chemicals obtained mostly from the extracts of Artemisia species that exert a significant amount of antimalarial activity while remaining relatively safe and tolerable. However, their effectiveness is not limited to malaria; it extends to a variety of human infectious diseases. Mostly the mode of action includes the generation of free radicals by breaking the endoperoxide link in its molecular structure, which facilitates the eradication of microbial species. Artemisinins are found to inhibit bacterial, viral, protozoal, helminth, and fungal infections. Their derivatives, like artemisone, a reversible inhibitor, target the viral replication cycle, and artesunate suppresses EBV infection by inhibiting the production of early EBV proteins. They were also found to be highly effective against Helicobacter pylori and Mycobacterium tuberculosis by generating peroxides in a time and concentrationdependent way. Other derivatives, such as artesunate, artemether, and arteether, have also shown antimicrobial activity that can be administered orally, rectally, intramuscularly, or intravenously. This review aims to provide a complete update on the antimicrobial applications of Artemisinin and its semi-synthetic derivatives, as well as derived dimers/trimers. The paper reflects a significant potential for the discovery of novel Artemisinin medications that can be used as supplementary treatments for various diseases. However, further translational and experimental research is required for optimization and the establishment of pharmacokinetic profiles. In addition, health authorities are also required to regulate the present Artemisinins and newly discovered derivatives to ensure their long-term effectiveness in the worldwide fight against antibiotic resistance.

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来源期刊
CiteScore
6.40
自引率
2.90%
发文量
186
审稿时长
3-8 weeks
期刊介绍: Current Topics in Medicinal Chemistry is a forum for the review of areas of keen and topical interest to medicinal chemists and others in the allied disciplines. Each issue is solely devoted to a specific topic, containing six to nine reviews, which provide the reader a comprehensive survey of that area. A Guest Editor who is an expert in the topic under review, will assemble each issue. The scope of Current Topics in Medicinal Chemistry will cover all areas of medicinal chemistry, including current developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, compound diversity measurements, drug absorption, drug distribution, metabolism, new and emerging drug targets, natural products, pharmacogenomics, and structure-activity relationships. Medicinal chemistry is a rapidly maturing discipline. The study of how structure and function are related is absolutely essential to understanding the molecular basis of life. Current Topics in Medicinal Chemistry aims to contribute to the growth of scientific knowledge and insight, and facilitate the discovery and development of new therapeutic agents to treat debilitating human disorders. The journal is essential for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important advances.
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