Faculty of Chemistry, University of Białystok, Ciołkowskiego 1K, 15-245 Białystok, Poland.
Department of Clinical Genetics, Medical University of Białystok, Waszyngtona 13, 15-089 Białystok, Poland.
Molecules. 2023 Nov 10;28(22):7528. doi: 10.3390/molecules28227528.
Cytostatic and pro-apoptotic effects of selenium steroid derivatives against HeLa cells were determined. The highest cytostatic activity was shown by derivative (GI 25.0 µM, almost complete growth inhibition after three days of culture, and over 97% of apoptotic and dead cells at 200 µM). The results of our study (cell number measurements, apoptosis profile, relative expression of apoptosis-related , , and mevalonate pathway-involved , , , and genes, and computational chemistry data) support the hypothesis that tested selenosteroids induce the extrinsic pathway of apoptosis by affecting the cell membrane as cholesterol antimetabolites. An additional mechanism of action is possible through a direct action of derivative to inhibit expression in a way similar to steroid hormones.
我们研究了硒甾体衍生物对 HeLa 细胞的细胞抑制和促凋亡作用。衍生物 （GI25.0μM，培养三天后几乎完全抑制生长，200μM 时凋亡和死亡细胞超过 97%）显示出最高的细胞抑制活性。我们的研究结果（细胞数量测量、凋亡谱、凋亡相关基因 、 、 和 以及甲羟戊酸途径相关基因 、 、 、 和 的相对表达，以及计算化学数据）支持了以下假设：测试的硒甾体通过作为胆固醇抗代谢物影响细胞膜来诱导细胞凋亡的外在途径。通过衍生物 以类似于甾体激素的方式直接抑制 表达，可能存在另一种作用机制。
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