Ali Hazhmat, Rasool Shelan, Saidu Muhammad Bello, Germán Péter, Szebeni Gábor J, Szabó Enikő, Rédei Dóra, Hohmann Judit, Zupkó István
Institute of Pharmacodynamics and Biopharmacy, University of Szeged, 6720 Szeged, Hungary.
College of Medicine, University of Duhok, Duhok 42001, Kurdistan Region, Iraq.
Int J Mol Sci. 2025 May 8;26(10):4489. doi: 10.3390/ijms26104489.
The current study examined the in vitro antineoplastic potentials of centrapalus coumarin F (CCF) obtained from aerial parts of (Willd.) H.Rob. (Asteraceae). Cytotoxic activity was tested against a panel of human adherent cancer cell lines, including breast, cervical, and oropharyngeal cancer and glioblastoma. Cell cycle analyses using flow cytometry and Hoechst 33258-propidium iodide (HOPI) fluorescent double staining were used to describe the proapoptotic property of CCF. Wound healing assessment and the Boyden chamber assay were performed to characterize the antimetastatic action of the compound. The firefly luciferase assay was applied to clarify the action of CCF on estrogenic receptors. CCF demonstrated remarkable selective growth inhibition against the HPV-18-positive human cervical cancer cell line HeLa (IC = 2.28 µM). The compound elicited crucial markers of apoptosis, inhibited the migration and invasion capacity of HeLa cells, and demonstrated an antiestrogenic property. Our current data indicate that the meroterpenoid scaffold presented here displays remarkable antiproliferative and antimetastatic effects on HeLa cells and can be considered a valuable model for designing further analogs targeting cervical carcinoma.
本研究检测了从（菊科）H.Rob.的地上部分获得的centrapalus香豆素F（CCF）的体外抗肿瘤潜力。针对一组人类贴壁癌细胞系，包括乳腺癌、宫颈癌、口咽癌和胶质母细胞瘤，测试了其细胞毒性活性。使用流式细胞术和Hoechst 33258-碘化丙啶（HOPI）荧光双重染色进行细胞周期分析，以描述CCF的促凋亡特性。进行伤口愈合评估和Boyden小室试验，以表征该化合物的抗转移作用。应用萤火虫荧光素酶试验来阐明CCF对雌激素受体的作用。CCF对HPV-18阳性的人宫颈癌细胞系HeLa表现出显著的选择性生长抑制作用（IC = 2.28 µM）。该化合物引发了凋亡的关键标志物，抑制了HeLa细胞的迁移和侵袭能力，并表现出抗雌激素特性。我们目前的数据表明，此处呈现的半萜类支架对HeLa细胞显示出显著的抗增殖和抗转移作用，可被视为设计针对宫颈癌的进一步类似物的有价值模型。
