作者
Magda F Mohamed, Farid M Sroor, Nada S Ibrahim, Ghada S Salem, Hadeer H El-Sayed, Marwa M Mahmoud, Menna-Allah M Wagdy, Amina M Ahmed, Aya-Allah T Mahmoud, Somia S Ibrahim, Mariam M Ismail, Sanaa Mohy Eldin, Fatma M Saleh, Hamdi M Hassaneen, Ismail A Abdelhamid
发表日期
2021/2
期刊
Investigational New Drugs
卷号
39
页码范围
98-110
出版商
Springer US
简介
Two novel chemotherapeutic chalcones were synthesized and their structures were confirmed by different spectral tools. Theoretical studies such as molecular modeling were done to detect the mechanism of action of these compounds. In vitro cytotoxicity showed a strong effect against all tested cell lines (MCF7, A459, HepG2, and HCT116), and low toxic effect against normal human melanocytes (HFB4). The lung carcinoma cell line was chosen for further molecular studies. Real-time PCR demonstrated that the two compounds upregulated gene expression of (BAX, p53, casp-3, casp-8, casp-9) genes and decreased the expression of anti-apoptotic genes bcl2, CDK4, and MMP1. Flow-cytometry indicated that cell cycle arrest of A459 was induced at the G2/M phase and the apoptotic percentage increased significantly compared to the control sample. Cytochrome c oxidase and VEGF enzyme activity were …
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