<p>The natural flavonoid glycoside vitexin displays preclinical antitumor activity by suppressing NF-κB signaling in nasopharyngeal carcinoma</p>

Abstract

Background and objectives: Vitexin is a natural flavonoid glycoside mainly extracted from the leaves of vitex, which has a variety of physiological activities. For example, vitexin has antitumor and anti-inflammation activities, and it can also promote blood circulation in the body. However, the function and mechanism of vitexin in nasopharyngeal carcinoma (NPC) are still unclear. Materials and methods: Cell Counting Kit-8 assay and cell cycle analysis were performed to examine cell survival in response to vitexin. Immunoblotting was used to analyze relative proteins’ expression. NPC xenograft models were established to assess the effect of vitexin in vivo. The luciferase activity of pNFκB-Luc was analyzed by using Dual-Luciferase Reporter Assay System. Quantitative real-time polymerase chain reaction was performed to detect relative genes’ expression. Kinase activity of IKKβ was analyzed in a cell-free system. Results: In this study, vitexin was found to display significant antitumor activity in NPC in vitro and in vivo. In NPC cells, vitexin inhibited cell cycle progression in NPC cells and induced the cleavages of PARP and inhibited antiapoptotic proteins’ expression, including Bcl-2 and Mcl1. Further studies indicated that vitexin significantly suppressed the luciferase activity of pNF-κB-Luc and inhibited the activation of NF-κB key regulators, including p65, IκBα and IKKs in NPC cells. Moreover, the kinase activity of IKKβ could be suppressed by vitexin in a cell-free system, and overexpression of CA-IKKβ could attenuate the inhibitory effect of vitexin on p65 phosphorylation. Conclusion: These results indicated that vitexin displayed antitumor activity by suppressing NF-κB signaling in NPC, which suggested that vitexin could be as a potential drug for the treatment of NPC in the future.

Advances in targeted therapy mainly based on signal pathways for nasopharyngeal carcinoma

“…110 The natural flavonoid glycoside vitexin can inhibit the activity of IKK thereby inhibiting the activation of the NF-κB signal pathway and inducing NPC cell apoptosis. 111 BST2, also known as CD317 or HM1.24, is found to be highly expressed in cisplatin-resistant NPC cells. It can activate the NF-κB signal pathway and increase the expression of downstream anti-apoptotic proteins.…”

Effects of Vitexin, a Natural Flavonoid Glycoside, on the Proliferation, Invasion, and Apoptosis of Human U251 Glioblastoma Cells

“…Vitexin was found to abrogate hepatocellular carcinoma invasion and angiogenesis and induce hepatocellular carcinoma cell apoptosis through suppressing AKT/STAT3 signaling or activating JNK signaling [34][35][36], and it has been reported that vitexin inhibits proliferation and triggers apoptosis of glioblastoma, non-small-cell lung cancer, and renal cell carcinoma cells through suppressing the PI3K/Akt/mTOR signaling pathway [14,37,38]. In addition, vitexin has shown inhibition against nasopharyngeal carcinoma, colorectal carcinoma, epithelial ovarian cancer, and leukemia by targeting NF-κB, JNK, ERK, and RAS/RAF pathways, respectively [39][40][41][42]. In the current study, vitexin was found to suppress glioblastoma U251 cell proliferation and invasion and promote cell apoptosis, which was similar to the previous report [14].…”

Biochemical Constituent of Ginkgo biloba (Seed) 80% Methanol Extract Inhibits Cholinesterase Enzymes in Javanese Medaka (Oryzias javanicus) Model

“…It has been reported that vitexin (50 μ M) was able to prevent the formation of ROS and NRS which are the markers of protein and lipid oxidation, carbonyl protein, and malondialdehyde [ 45 ]. It also reduced loss of membrane potential by a mechanism of increased mitochondrial biogenesis, such as induction of the expression of antioxidant genes nuclei factor 2 (Nrf-2) and heme oxygenase-1 (HO-1) with increased GSH level [ 46 ].…”