β-Zearalenol

β-Zearalenol is a zearalenone metabolite and Estrogen receptor binder (K_d = 0.406 nM) that induces apoptosis through activation of p53, JNK, and p38 kinases and the mitochondrial apoptosis pathway, while inhibiting CYP19A1 and inducing autophagy via SIRT1. β-Zearalenol is used in research on cardiotoxicity, mycotoxin-induced reproductive toxicity, and breast cancer^{[1][2][3][4][5][6][7][8][9][10]}. In Vitro:β-Zearalenol (β-ZOL) (0-50 μM; 24 h) reduces the viability of RAW264.7 macrophages, YD-38, and Detroit 551 cells in a dose-dependent manner^[1].
β-Zearalenol (10-50 μM; 24 h) induces apoptosis in RAW264.7 macrophages, manifested as a dose-dependent increase in the sub-G₁ cell population^[1].
β-Zearalenol (50 μM; 24 h) primarily induces apoptosis, rather than necrosis, in RAW264.7 macrophages^[1].
β-Zearalenol (50 μM; 24 h) induces caspase-independent cell death in RAW264.7 macrophages^[1].
β-Zearalenol (300 μM; 24 h) induces caspase-3 activation in HCT116 cells^[8].
β-Zearalenol (300 μM; 24 h) induces HCT116 cell death mediated by Bax and Bak^[8].
β-Zearalenol (30-120 μM; 24 h) activates caspase-3 in human Caco-2 cells^[9].
β-Zearalenol (10-50 μM; 12 h) induces a significant loss of mitochondrial membrane potential in RAW264.7 macrophages^[1].
β-Zearalenol (10-50 μM; 24 h) induces mitochondrial stress and alters the Bcl-2/Bax signaling pathway in RAW264.7 macrophages, leading to the release of cytochrome c into the cytoplasm^[1].
β-Zearalenol (300 μM; 24 h) increases mitochondrial superoxide anion production in HCT116 cells^[8].
β-Zearalenol (10-50 μM; 24 h) induces nuclear translocation of AIF in RAW264.7 macrophages^[1].
β-Zearalenol (10-50 μM; 3 h) activates JNK but not p38 MAPK in RAW264.7 macrophages^[1].
β-Zearalenol (20-100 μM; 24 h) is cytotoxic to H9c2 cells, with an LD₅₀ of 80 μM after 24 h of treatment^[2].
β-Zearalenol (5-200 μM) inhibits the proliferation of primary bovine ovarian granulosa cells in a dose-dependent manner, with an IC₅₀ of 25 μM^[3].
β-Zearalenol (β-Zol) (0-130 μM; 24 h) reduces Vero cell viability in a dose-dependent manner, with an IC₅₀ of approximately 50 μM^[4].
β-Zearalenol (37-150 μM; 24 h) inhibits DNA synthesis in Vero cells with an IC₅₀ of 90 μM, exhibiting a non-linear dose-response between 37 and 75 μM^[4].
β-Zearalenol (10% loss of cell viability-50% loss of cell viability; 24 h) induces Hsp 27 and Hsp 70 expression in Vero cells in a concentration-dependent manner^[4].
β-Zearalenol (β-ZEL) (0-10 μmol/L) forms stable complexes with HSA, BSA, PSA, and RSA, with the highest affinity for RSA (logK = 5.43) and the lowest affinity for PSA (logK = 4.05), exhibiting significant species-dependent binding^[5].
β-Zearalenol (0-10 μmol/L) reduces the total fluorescence intensity of Warfarin (HY-B0687) in a concentration-dependent manner, supporting the hypothesis that its binding site or location on HSA differs from that of ZEN and α-ZEL^[5].
β-Zearalenol (7.5-30 μM; 48 h) reduces the viability of primary cultured porcine endometrial cells in a dose-dependent manner, with significant cytotoxicity observed at 30 μM^[6].
β-Zearalenol (30 μM; 48 h) induces necrotic ultrastructural changes in primary cultured porcine endometrial cells^[6].
β-Zearalenol (7.5-30 μM; 24-48 h) significantly decreases the expression of the proliferation marker PCNA in primary cultured porcine endometrial cells in a time- and dose-dependent manner^[6].
β-Zearalenol (1 nM-1 μM; 1 h) binds to porcine uterine cytosolic estrogen receptors^[6].
β-Zearalenol (1-100 μM; 24 h) inhibits E2 secretion in human BeWo cells at concentrations of 1 μM and above^[7].
β-Zearalenol (300 μM; 24 h) promotes a significant decrease in Δψ_m in HCT116 cells and does not induce necrosis in HCT116 cells^[8].
β-Zearalenol (0-100 μM; 48 h) reduces the viability of human Caco-2 cells with an IC₅₀ of approximately 60 μM^[9].
β-Zearalenol (30-120 μM; 24 h) induces DNA damage and fragmentation in human Caco-2 cells^[9].
β-Zearalenol (60 μM; 24 h) induces PARP cleavage in human Caco-2 cells^[9].
β-Zearalenol (50 μM) induces intracellular ROS generation in RAW264.7 macrophages^[1].
β-Zearalenol (50 μM) increases cellular ROS levels, whereas catalase and superoxide dismutase both decrease ROS levels in RAW264.7 macrophages^[1].
β-Zearalenol (80 μM; 6-24 h) induces oxidative stress in H9c2 cardiomyocytes by generating intracellular and mitochondrial ROS^[2].
β-Zearalenol (IC₅₀/4-IC₅₀; 24 h) induces lipid peroxidation in Vero cells in a concentration-dependent manner, increasing MDA levels to 18 times those of the control group^[4].
β-Zearalenol (300 μM; 24 h) induces oxidative stress by increasing ROS generation in HCT116 cells^[8].
β-Zearalenol (80 μM; 24 h) does not induce significant necrosis after 24 h treatment in H9c2 cells, induces loss of mitochondrial membrane potential, induces caspase-3 activation, and increases BAX protein expression in H9c2 cells^[2].
β-Zearalenol (80 μM; 6-24 h) induces autophagy in H9c2 cardiomyocytes, with increased LC3-II and Beclin-1 levels observed at 6 h but not at 24 h^[2].
β-Zearalenol (37-150 μM; 24 h) inhibits protein synthesis in Vero cells with an IC₅₀ of approximately 60 μM and an inhibition rate of nearly 80% at 150 μM^[4].
β-Zearalenol (60 μM; 24 h) decreases Bcl-2 protein levels in human Caco-2 cells^[9].
β-Zearalenol (7.5-30 μM; 24-48 h) inhibits the proliferation of primary cultured porcine endometrial cells by reducing the S phase cell population and arresting cells in the G₀/G₁ phase of the cell cycle^[6].
β-Zearalenol (100-400 μM; 24 h) reduces HCT116 cell viability with an IC₅₀ of approximately 300 μM^[8].
β-Zearalenol (6.25-25 µM; 144 h) exhibits estrogenic activity in MCF-7 cells, with a maximum relative proliferative effect of 87.70% at 12.5 µM, classifying it as a partial agonist at low concentrations and a full agonist at 12.5 µM^[10].
β-Zearalenol (30-120 μM; 24 h) induces lipid peroxidation in human Caco-2 cells in a concentration-dependent manner^[9].