J. Heisig, Niels V. Heise, Sophie Hoenke, A. Al-Harrasi, R. Csuk
{"title":"In search of cytotoxic abietyl amides","authors":"J. Heisig, Niels V. Heise, Sophie Hoenke, A. Al-Harrasi, R. Csuk","doi":"10.13171/mjc02307191709csuk","DOIUrl":null,"url":null,"abstract":"<p><span lang=\"EN-US\">Based on prior research findings with pentacyclic triterpenoids, it was hypothesized that (un)-substituted benzylamides would exhibit enhanced cytotoxic activity compared to parent abietic acid. Conversely, none of these compounds was cytotoxic, but (homo)-piperazinyl amides demonstrated significant cytotoxic activity across multiple cell lines, even at concentrations as low single-digit micromolar levels. Additional staining experiments revealed that the most potent compound (with an EC<sub>50</sub> value of 2.8 </span><span lang=\"EN-US\">m</span><span lang=\"EN-US\">M for HT29 colon carcinoma cells) primarily induced apoptosis rather than necrosis. </span> </p>","PeriodicalId":18513,"journal":{"name":"Mediterranean Journal of Chemistry","volume":"80 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2023-07-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Mediterranean Journal of Chemistry","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.13171/mjc02307191709csuk","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0
Abstract
Based on prior research findings with pentacyclic triterpenoids, it was hypothesized that (un)-substituted benzylamides would exhibit enhanced cytotoxic activity compared to parent abietic acid. Conversely, none of these compounds was cytotoxic, but (homo)-piperazinyl amides demonstrated significant cytotoxic activity across multiple cell lines, even at concentrations as low single-digit micromolar levels. Additional staining experiments revealed that the most potent compound (with an EC50 value of 2.8 mM for HT29 colon carcinoma cells) primarily induced apoptosis rather than necrosis.