Quercetin and Its Fermented Extract as a Potential Inhibitor of Bisphenol A-Exposed HT-29 Colon Cancer Cells’ Viability

Abstract

Bisphenol A (BPA) promotes colon cancer by altering the physiological functions of hormones. Quercetin (Q) can regulate signaling pathways through hormone receptors, inhibiting cancer cells. The antiproliferative effects of Q and its fermented extract (FEQ, obtained by Q gastrointestinal digestion and in vitro colonic fermentation) were analyzed in HT-29 cells exposed to BPA. Polyphenols were quantified in FEQ by HPLC and their antioxidant capacity by DPPH and ORAC. Q and 3,4-dihydroxyphenylacetic acid (DOPAC) were quantified in FEQ. Q and FEQ exhibited antioxidant capacity. Cell viability with Q+BPA and FEQ+BPA was 60% and 50%, respectively; less than 20% of dead cells were associated with the necrosis process (LDH). Treatments with Q and Q+BPA induced cell cycle arrest in the G0/G1 phase, and FEQ and FEQ+BPA in the S phase. Compared with other treatments, Q positively modulated ESR2 and GPR30 genes. Using a gene microarray of the p53 pathway, Q, Q+BPA, FEQ and FEQ+BPA positively modulated genes involved in apoptosis and cell cycle arrest; bisphenol inhibited the expression of pro-apoptotic and cell cycle repressor genes. In silico analyses demonstrated the binding affinity of Q > BPA > DOPAC molecules for ERα and ERβ. Further studies are needed to understand the role of disruptors in colon cancer.

Mechanism of Astragalus membranaceus (Huangqi, HQ) for treatment of heart failure based on network pharmacology and molecular docking

“…Previously, García‐Gutiérrez et al. demonstrated that Quercetin significantly increased the expression of ESR1 in HT‐29 colon cancer cells 59 . Calycosin promoted the expression of ER‐α36, which is the main oestrogen receptor of ESR1, in macrophages 60 .…”

“…demonstrated that Quercetin significantly increased the expression of ESR1 in HT‐29 colon cancer cells. 59 Calycosin promoted the expression of ER‐α36, which is the main oestrogen receptor of ESR1, in macrophages. 60 Kaempferol notably promoted ESR1 expression in the ovaries tissue of rats with premature ovarian failure.…”

Role of natural products in tumor therapy from basic research and clinical perspectives

“…Similarly, recent studies have reported that bisphenol A (BPA) may have toxic effects on the body and colon. Quercetin and its fermented extract exhibited excellent inhibitory effect on the viability of BPA-exposed HT29 colon cancer cells [33]. Additionally, quercetin enhanced the chemotherapeutic impact of oxaliplatin in HCT116 cells by increasing intracellular ROS through its suppressive action on glutathione levels [34].…”