Cytochrome P450 CYP1 metabolism of hydroxylated flavones and flavonols: Selective bioactivation of luteolin in breast cancer cells

Nobiletin bioactivation in MDA-MB-468 breast cancer cells by cytochrome P450 CYP1 enzymes

“…In the current analysis, the metabolite NP1 was evident in the MDA-MB-468 cellular samples. However, in contrast to MCF7 cells that are inducible in the presence of a CYP1 inducer, MDA-MB-468 cells express constitutively active CYP1 enzymes (Androutsopoulos et al, 2009a;Androutsopoulos et al, 2009c;Surichan et al, 2012;Androutsopoulos and Tsatsakis, 2014;Androutsopoulos et al, 2008, Wilsher et al, 2017. Therefore the metabolism of nobiletin in MDA-MB-468 cells was evident at shorter time points compared with that in the MCF7 cell line that requires induction of cytochrome CYP1 enzymes by the activation of the AhR (Surichan et al, 2012).…”

“…The previous study conducted by our research group investigated the metabolism of nobiletin in MCF7 cells and/or MCF7 cells that were pre-induced with the potent CYP1 inducer TCDD (Surichan et al, 2012). In the present study, the investigation of nobiletin was carried out in MDA-MB-468 cells that express constitutively CYP1 enzymes in the absence of an inducer (Androutsopoulos et al, 2008, Wilsher et al, 2017). Incubation of nobiletin for 24 h with MDA-MB-468 cells resulted in an apparent decrease in the concentration of this compound, while a main metabolite denoted NP1 was present (Fig.…”

“…Previous studies have demonstrated that MDA-MB-468 cell constitutively express CYP1 enzymes compared with MCF10A cells that express little or no CYP1 protein (Androutsopoulos et al, 2008;Wilsher et al, 2017). The cytotoxicity of nobiletin was tested in the aforementioned 2 cell lines.…”

Polyphenols of Chinese skullcap roots: from chemical profiles to anticancer effects

“…87 Scutellarin is a metabolite of scutellarein and has been reported to have stronger anticancer activity than scutellarein. 88 Scutellarin can be developed as a promising anti-tumor drug to treat colon cancer since it shows anti-proliferative and proapoptotic effects on human colon cancer HCT-116 cells. The exposure of HCT-116 cells to scutellarin decreased cell viability in a dose-and time-dependent manner and also induced apoptotic transformation of the cancer cells via the potential regulation of p53 and Bcl-2/Bax expressions.…”

Scandenolone from Cudrania tricuspidata fruit extract suppresses the viability of breast cancer cells (MCF-7) in vitro and in vivo

“…Furthermore, some recent studies have shown that ordinary chemotherapy might enhance tumor vascularization, which further leads to resistance of tumor removal (Zhang et al, 2016). Scientist have been continuously searching for the new ideal anticancer drugs with high efficacy, low toxicity and side effects, and phytochemicals from plant food are under active consideration (Wilsher et al, 2017).…”