Chalcones are the simple chemical backbone of many natural compounds and are widely distributed in vegetables, fruits, teas and other plants. This class of compounds is the main secondary metabolite of plants and serves as a defense mechanism for plants to resist reactive oxygen species and prevent damage to themselves by microorganisms, insects or herbivores, etc. In addition, chalcones and their derivatives have a wide range of biological activities due to their unique structures, such as antibacterial, antidiabetic, antitubercular, antioxidant, and antimalarial.
The cellular microtubule system, which is established by the balance between polymerization and depolymerization of α- and β-microtubulin heterodimers, is widely found in the structures of various types of cells, including tumor cells. Its structure is long and hollow, and has the role of maintaining cell shape, regulating cell transport and cell division. Based on the important role of microtubules in the cell cycle. By inhibiting or interfering with the kinetics of microtubule protein polymerization and depolymerization, mitotic arrest and apoptosis can be caused.
The process of tumor vascular growth is a complex biochemical reaction involving the reception and transduction of many signals from vascular growth stimuli. Among them, the main pro-angiogenic factors are epidermal growth factor (EGF), vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF), which mainly promote the growth of tumor neovascularization through mediating signal transduction pathways.
1. PI3K/AKT signaling pathway
Phosphatidylinositol 3 kinase (PI3K) is an important transduction signal downstream of RTK family EGFR/VEGFR-2, and its activation converts phosphorylated phosphatidylinositol-4,5-bisphosphate to phosphatidylinositol-3,4,5-trisphosphate [PI(3,4,5)P3], which binds to and activates the serine protein kinase AKT, and subsequently regulates a variety of transcription factors (such as phosphorylation regulates various transcription factors (e.g. NF-κB) and thus suppresses apoptotic gene expression.
2. Ntoch signaling pathway
Notch signaling is a short-range intercellular communication system that regulates many biological processes, such as self-renewal of embryonic and adult stem cells, as well as cell differentiation and proliferation. Activation of this signal induces numerous protein hydrolysis, such as ADAM metalloproteinase cleavage and γ-secretase (GS) complex cleavage, which leads to the release of membrane-activated NICD and promotes transcription of Notch downstream target genes with the DNA-binding protein CSL.
Cytotoxicity is the effect of chemicals on basic cellular structures or physiological processes, such as cytoskeletal structure, cellular metabolic processes, ion regulation, cell division and other processes, resulting in disruption of cell survival, proliferation or function. Chalcones have a wide range of cytotoxic effects on tumor cells. This section focuses on chalcones and their derivatives that have no specific anti-cancer mechanism in recent years but have anti-malignant proliferative activity on tumor cells.
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