{"title":"A Comprehensive Review on the Antimicrobial Activity of the Genus Artemisia, Artemisinin, and its Derivatives.","authors":"Kiran Sharma","doi":"10.2174/0115680266343676250122062731","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.9000,"publicationDate":"2025-02-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current topics in medicinal chemistry","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.2174/0115680266343676250122062731","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
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.
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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