Leandre van der Merwe, Catherine H. Kaschula, Prinessa Chellan
{"title":"青蒿琥酯的有机金属缀合物:抗癌潜力的合成与评价","authors":"Leandre van der Merwe, Catherine H. Kaschula, Prinessa Chellan","doi":"10.1016/j.jorganchem.2025.123804","DOIUrl":null,"url":null,"abstract":"<div><div>New organometallic Ru(II), Rh(III) and Ir(III) complexes containing artesunate were synthesised to ascertain the anticancer effect of combining artesunate with different platinum group metal centres. The synthetic approach involved the preparation of two ligands, di(2-pyridyl) methyl amine (<strong>L1</strong>) and the dipyridyl-artesunate hybrid (<strong>L2</strong>), followed by complexation with the metal dimers to produce six complexes, <strong>C1</strong>-<strong>C6</strong>. All complexes were evaluated for their anticancer activity against two breast cancer cell lines, MCF-7 and MDA-MB-231, in which they showed moderate to low activity. The complexes containing the artesunate moiety, <strong>C4</strong>-<strong>C6</strong>, showed higher activity. All complexes had low to no cytotoxicity against the normal breast cell line, MCF-12A, showing potential selectivity for cancerous cells over normal cells. A potential mode of action, through reactive oxygen species generation, was evaluated, and all complexes were found to lead to an increase in ROS levels in the MDA-MB-231 cells.</div></div>","PeriodicalId":374,"journal":{"name":"Journal of Organometallic Chemistry","volume":"1039 ","pages":"Article 123804"},"PeriodicalIF":2.1000,"publicationDate":"2025-08-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Organometallic conjugates of artesunate: synthesis and evaluation of anticancer potential\",\"authors\":\"Leandre van der Merwe, Catherine H. Kaschula, Prinessa Chellan\",\"doi\":\"10.1016/j.jorganchem.2025.123804\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>New organometallic Ru(II), Rh(III) and Ir(III) complexes containing artesunate were synthesised to ascertain the anticancer effect of combining artesunate with different platinum group metal centres. The synthetic approach involved the preparation of two ligands, di(2-pyridyl) methyl amine (<strong>L1</strong>) and the dipyridyl-artesunate hybrid (<strong>L2</strong>), followed by complexation with the metal dimers to produce six complexes, <strong>C1</strong>-<strong>C6</strong>. All complexes were evaluated for their anticancer activity against two breast cancer cell lines, MCF-7 and MDA-MB-231, in which they showed moderate to low activity. The complexes containing the artesunate moiety, <strong>C4</strong>-<strong>C6</strong>, showed higher activity. All complexes had low to no cytotoxicity against the normal breast cell line, MCF-12A, showing potential selectivity for cancerous cells over normal cells. A potential mode of action, through reactive oxygen species generation, was evaluated, and all complexes were found to lead to an increase in ROS levels in the MDA-MB-231 cells.</div></div>\",\"PeriodicalId\":374,\"journal\":{\"name\":\"Journal of Organometallic Chemistry\",\"volume\":\"1039 \",\"pages\":\"Article 123804\"},\"PeriodicalIF\":2.1000,\"publicationDate\":\"2025-08-07\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Organometallic Chemistry\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0022328X25002979\",\"RegionNum\":3,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, INORGANIC & NUCLEAR\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Organometallic Chemistry","FirstCategoryId":"92","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0022328X25002979","RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, INORGANIC & NUCLEAR","Score":null,"Total":0}
Organometallic conjugates of artesunate: synthesis and evaluation of anticancer potential
New organometallic Ru(II), Rh(III) and Ir(III) complexes containing artesunate were synthesised to ascertain the anticancer effect of combining artesunate with different platinum group metal centres. The synthetic approach involved the preparation of two ligands, di(2-pyridyl) methyl amine (L1) and the dipyridyl-artesunate hybrid (L2), followed by complexation with the metal dimers to produce six complexes, C1-C6. All complexes were evaluated for their anticancer activity against two breast cancer cell lines, MCF-7 and MDA-MB-231, in which they showed moderate to low activity. The complexes containing the artesunate moiety, C4-C6, showed higher activity. All complexes had low to no cytotoxicity against the normal breast cell line, MCF-12A, showing potential selectivity for cancerous cells over normal cells. A potential mode of action, through reactive oxygen species generation, was evaluated, and all complexes were found to lead to an increase in ROS levels in the MDA-MB-231 cells.
期刊介绍:
The Journal of Organometallic Chemistry targets original papers dealing with theoretical aspects, structural chemistry, synthesis, physical and chemical properties (including reaction mechanisms), and practical applications of organometallic compounds.
Organometallic compounds are defined as compounds that contain metal - carbon bonds. The term metal includes all alkali and alkaline earth metals, all transition metals and the lanthanides and actinides in the Periodic Table. Metalloids including the elements in Group 13 and the heavier members of the Groups 14 - 16 are also included. The term chemistry includes syntheses, characterizations and reaction chemistry of all such compounds. Research reports based on use of organometallic complexes in bioorganometallic chemistry, medicine, material sciences, homogeneous catalysis and energy conversion are also welcome.
The scope of the journal has been enlarged to encompass important research on organometallic complexes in bioorganometallic chemistry and material sciences, and of heavier main group elements in organometallic chemistry. The journal also publishes review articles, short communications and notes.