Ephedrannin A: A potent dual inhibitor of FAK and Src with anticancer effects

Authors
Ong, Hien Thi MyAtes, EdaKang, Min-Jung
Issue Date
2025-03
Publisher
대한화학회
Citation
Bulletin of the Korean Chemical Society, v.46, no.3, pp.317 - 325
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 mu M 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.
Keywords
SIGNALING PATHWAYS; ADHESION; PHOSPHORYLATION; RESVERATROL; ACTIVATION; EXPRESSION; CONFERONE; APOPTOSIS; MIGRATION; CURCUMIN; ephedrannin A; inhibition of FAK and Src; natural product; anticancer compound; colon cancer cells
ISSN
0253-2964
URI
https://pubs.kist.re.kr/handle/201004/152087
DOI
10.1002/bkcs.70002
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KIST Article > Others
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