Novel daidzein molecules exhibited anti-prostate cancer activity through nuclear receptor ER β modulation, < em > in vitro < /em > and < em > in vivo < /em > studies

J Chemother. 2021 Jun 1:1-13. doi: 10.1080/1120009X.2021.1924935. Online ahead of print.ABSTRACTEight novel ERβ selective daidzein analogues (NCE1-8) were synthesized and their anti-cancer activity was evaluated by in vitro and in vivo methods. Cytotoxicity study, Receptor binding studies, Luciferase assay, cMYC & Cyclin D1 expression and Caspase 3, 8 & 9 activities were measured to ascertain the anticancer activity and mechanism. Uterotropic, anti-androgenic and anti-tumour activities were performed in rodents. The results revealed that NCEs produced anti-prostate cancer activity in DU145, LNCaP and PC3 cell lines and 50% more active than genistein. NCEs was significantly down-regulated cMYC & Cyclin D1 genes and elevated caspase 3 & 9 levels and did not show any difference in uterotropic, anti-androgenic activities. The tumour weight was also reduced. The NCE 1 and 2 have shown ERβ selectivity in receptor binding studies. Daidzein with methyl substitution at R or R1 position exhibited more ERβ selectivity and could be considered as lead molecules for anti-prostate cancer activity.PMID:34060437 | DOI:10.1080/1120009X.2021.1924935
Source: Journal of Chemotherapy - Category: Cancer & Oncology Authors: Source Type: research