Xanthohumol, a prenylated flavonoid from Hops, exerts anticancer effects against gastric cancer in�vitro

Abstract

Xanthohumol (Xn), a prenylated flavonoid isolated from Hops (Humulus lupulus L.), has demonstrated potent anticancer activity in multiple types of cancer. However, the effect of Xn on gastric cancer (GC) remains unknown. The aim of the present study was to investigate the effect of Xn on GC cell proliferation, apoptosis and metastasis. It was observed that Xn decreased the viability of GC cells, with very low or no toxicity to normal gastric epithelial cells GES-1 at a concentration of 1–100 µM. The proliferation of AGS cells was inhibited by Xn, as indicated by the decreased number of EdU-positive cells. Xn treatment increased the number of apoptotic cells, downregulated the expression of Bcl-2 and upregulated the expression of Bax, suggesting induction of apoptosis. The results from the wound healing and Transwell assays indicated that Xn suppressed AGS cell metastasis. Moreover, Xn induced reactive oxygen species (ROS) overproduction and inhibited nuclear factor (NF)-κB signaling in AGS cells, which was reversed by the ROS inhibitor N-acetylcysteine (NAC). NAC suppressed the effect of Xn on the proliferation, apoptosis and metastasis of AGS cells. Taken together, these results suggest that Xn exerts anticancer effects against GC via induction of ROS production and subsequent inhibition of NF-κB signaling. Therefore, Xn may be a promising candidate treatment against GC progression.

Antiproliferative Effect of Acridine Chalcone Is Mediated by Induction of Oxidative Stress

“…Recently, we documented excellent antiproliferative action of 1C acridine chalcone in HCT116 cells [11]. In the last decade, some articles indicated a relationship between the antiproliferative effect and induction of oxidative stress in both natural and synthetic chalcones [51][52][53][54]. This fact prompted us to evaluate the role of ROS/RNS in the antiproliferative and proapoptotic effect of chalcone 1C.…”

Antioxidant, Antiproliferative and Apoptosis-Inducing Efficacy of Fractions from Cassia fistula L. Leaves

“…Choi and coauthors [36] reported the cytotoxic and apoptogenic potential of kaempferol against the colorectal cancer HCT116 cells through the enhancement in the generation of ROS. In a report by Wei and coworkers [37], it was found that xanthohumol, a prenylated flavonoid isolated from Humulus lupulus L. exhibited its antiproliferative and apoptotic effects by the overproduction of ROS in gastric cancer AGS cells. The loss of mitochondrial membrane permeability is another important feature for the determination of apoptosis in cancer cells.…”

A bio-guided assessment of the anti-inflammatory activity of hop extracts (Humulus lupulus L. cv. Cascade) in human gastric epithelial cells

“…both were able to reduce this parameter, but not to completely inhibit the secretion even at the highest To the best of our knowledge, this is the first study demonstrating the anti-inflammatory activity of xanthohumol D in human gastric epithelial cells. Many literature studies have investigated the biological properties of xanthohumol A, which is mostly known for its anti-proliferative activity in different cancer cell lines, including gastric cells (Wei et al, 2018).…”

“…In the second study, a high molecular weight fraction from hop bract extract, rich in polymerized catechins, reduced in mice the gastric damage induced by the oral administration of VacA, a vacuolating cytotoxin produced by Helicobacter pylori (Yahiro et al, 2005) (Yahiro et al, 2005) (Yahiro et al, 2005) (Yahiro et al, 2005). As anti-inflammatory effects, a CO2 hop extract reduced the prostaglandin E2 production in adenocarcinoma gastric cells (AGS) by influencing COX-2 enzyme (Tripp et al, 2005), while xanthohumol A suppressed the proliferation, apoptosis and metastasis of AGS cells via induction of ROS production and inhibition of the NF-κB signaling (Wei et al, 2018).…”