Counteracting Estrogen as Breast Cancer Prevention

Synthesis of Casimiroin and Optimization of Its Quinone Reductase 2 and Aromatase Inhibitory Activities

“…Aromatase inhibitors decrease bioavailable estrogen and have been shown to have considerable antitumor activity in certain breast cancers 15. Such compounds ultimately reduce estradiol receptor stimulation and reduce formation of genotoxic estrogen metabolites 16. Certain nonsteroidal aromatase inhibitors are already in clinical use for the treatment of breast cancer, and several naturally occurring nonsteroidal aromatase inhibitors have shown promising chemopreventive activity 17…”

Neoflavonoids and Tetrahydroquinolones as Possible Cancer Chemopreventive Agents

“…The detailed experimental procedure is described by Singh et al (12). The selective physical data of final compounds (7)(8)(9)(10)(11)19, and 20) have been given in Table 1. Neoflavonoids (7-11) and tetrahydroquinolones (19 and 20) were evaluated using cell and molecular target-based in vitro bioassays.…”

“…Thus, aromatase inhibitors have been shown to have considerable antitumor activity in certain types of breast cancers by decreasing estrogen levels (7). Such compounds ultimately reduce estradiol receptor stimulation and reduce formation of genotoxic estrogen metabolites (8). The aromatase complex is associated with the endoplasmic reticulum and consists of a specific cytochrome P450 heme protein (CYP19) and the flavoprotein NADPH cytochrome P450 reductase (9).…”

Evaluation of selected indigenous medicinal plants from the western Himalayas for cytotoxicity and as potential cancer chemopreventive agents

“…The in vitro assays included nuclear factor-kappaB (NF-B) (Homhual et al, 2006;Dorai & Aggarwal, 2004), quinone reductase (QR) (Cuendet et al, 2006), aromatase (Strasser-Weippl & Goss, 2005), retinoic X receptor alpha (RXR) (Wu et al, 2002), and assessment of cytotoxicity (Mi et al, 2001). Cytotoxicity was assessed with four different human cancer cell lines, namely, hepatocellular carcinoma ATCC number HB-8065 (HepG2), mammary adenocarcinoma ATCC number HTB-22 (MCF-7), prostate lymph node carcinoma ATCC number CRL-1740, (LNCaP) and lung carcinoma cells (LU) established at the Department of Surgical Oncology, University of Illinois at Chicago.…”