{"title":"Ephedrannin A: A potent dual inhibitor of FAK and Src with anticancer effects","authors":"Hien Thi My Ong, Eda Ates, Min-Jung Kang","doi":"10.1002/bkcs.70002","DOIUrl":null,"url":null,"abstract":"<p>Cancer is the leading cause of death worldwide, and the development of effective treatments remains an important challenge. Here, we present ephedrannin A, a compound that exhibits strong anticancer activity against various types of cancer including lung, liver, colon, and kidney cancer. The compound has demonstrated its remarkable ability to inhibit cell proliferation and invasion similar to conferone and Y15, known focal adhesion kinase (FAK) inhibitors. Treatment with 10 μM ephedrannin A significantly reduced the expression of FAK, and phosphorylated FAK and proto-oncogene tyrosine-protein kinase Src, two major signaling proteins involved in cancer progression in colon, kidney, and lung cancer cell lines. Furthermore, knockdown experiments targeting Src found no effect on FAK expression and phosphorylation, suggesting that FAK/Src complex inhibition is the main mechanism of action of ephedrannin A. Co-targeting of FAK and Src is a promising therapeutic strategy because these proteins play important roles in promoting cell proliferation, migration, and invasion. By disrupting these pathways, ephedrannin A could effectively inhibit the growth and metastasis of cancer cells. Further investigation is necessary to elucidate the exact molecular mechanisms underlying the anticancer effects of ephedrannin A and to explore the possibility of clinical development.</p>","PeriodicalId":54252,"journal":{"name":"Bulletin of the Korean Chemical Society","volume":"46 3","pages":"317-325"},"PeriodicalIF":1.7000,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Bulletin of the Korean Chemical Society","FirstCategoryId":"92","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1002/bkcs.70002","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0
Abstract
Cancer is the leading cause of death worldwide, and the development of effective treatments remains an important challenge. Here, we present ephedrannin A, a compound that exhibits strong anticancer activity against various types of cancer including lung, liver, colon, and kidney cancer. The compound has demonstrated its remarkable ability to inhibit cell proliferation and invasion similar to conferone and Y15, known focal adhesion kinase (FAK) inhibitors. Treatment with 10 μM ephedrannin A significantly reduced the expression of FAK, and phosphorylated FAK and proto-oncogene tyrosine-protein kinase Src, two major signaling proteins involved in cancer progression in colon, kidney, and lung cancer cell lines. Furthermore, knockdown experiments targeting Src found no effect on FAK expression and phosphorylation, suggesting that FAK/Src complex inhibition is the main mechanism of action of ephedrannin A. Co-targeting of FAK and Src is a promising therapeutic strategy because these proteins play important roles in promoting cell proliferation, migration, and invasion. By disrupting these pathways, ephedrannin A could effectively inhibit the growth and metastasis of cancer cells. Further investigation is necessary to elucidate the exact molecular mechanisms underlying the anticancer effects of ephedrannin A and to explore the possibility of clinical development.
期刊介绍:
The Bulletin of the Korean Chemical Society is an official research journal of the Korean Chemical Society. It was founded in 1980 and reaches out to the chemical community worldwide. It is strictly peer-reviewed and welcomes Accounts, Communications, Articles, and Notes written in English. The scope of the journal covers all major areas of chemistry: analytical chemistry, electrochemistry, industrial chemistry, inorganic chemistry, life-science chemistry, macromolecular chemistry, organic synthesis, non-synthetic organic chemistry, physical chemistry, and materials chemistry.