New Steroidal Selenides as Proapoptotic Factors

Autor: Izabella Jastrzebska, Natalia Wawrusiewicz-Kurylonek, Paweł A. Grześ, Artur Ratkiewicz, Ewa Grabowska, Magdalena Czerniecka, Urszula Czyżewska, Adam Tylicki
Jazyk: angličtina
Rok vydání: 2023
Předmět:
Zdroj: Molecules, Vol 28, Iss 22, p 7528 (2023)
Druh dokumentu: article
ISSN: 1420-3049
DOI: 10.3390/molecules28227528
Popis: Cytostatic and pro-apoptotic effects of selenium steroid derivatives against HeLa cells were determined. The highest cytostatic activity was shown by derivative 4 (GI50 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 APAF1, BID, and mevalonate pathway-involved HMGCR, SQLE, CYP51A1, and PDHB 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 4 to inhibit PDHB expression in a way similar to steroid hormones.
Databáze: Directory of Open Access Journals
Nepřihlášeným uživatelům se plný text nezobrazuje