A large-scale transcriptional analysis reveals herb-derived ginsenoside F2 suppressing hepatocellular carcinoma via inhibiting STAT3

Tan, Xue; Ma, Xiaofang; Dai, Yifei; An, Jun; Yu, Xiankuo; Li, Shengrong; Liao, Yile; Pei, Tianli; Tang, Yuqin; Gui, Yu; Zhou, Shiyi; Guo, Dale; Deng, Yun; Hu, Kaifeng; Wang, Dong

doi:10.1016/j.phymed.2023.155031

Cited by 6 publications

(1 citation statement)

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“…The cells were treated with GCs for another 24 h, and then the activities of firefly luciferase as well as Renilla luciferase were determined by a Dual-Glo® Luciferase Assay System. [26][27][28] Each assay was performed in triplicate on a microplate reader (Molecular Devices, Sunnyvale, CA). DMSO was used as a negative control.…”

Section: Reporter Gene Assaymentioning

confidence: 99%

Comparison of the Glucocorticoid Receptor Binding and Agonist Activities of Typical Glucocorticoids: Insights into Their Endocrine Disrupting Effects

Liang,

Li,

Zhang

et al. 2024

Chemistry & Biodiversity

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Over the past decades, the synthetic glucocorticoids (GCs) have been widely used in clinical practice and animal husbandry. Given the health hazard of these toxic residues in food, it is necessary to explore the detailed interaction mechanisms of typical GCs and their main target glucocorticoid receptor (GR). Hence, this work compared the GR binding and agonist activities of typical GCs. Fluorescence polarization assay showed that these GCs were potent ligands of GR. Their GR binding affinities were in the order of methylprednisolone > betamethasone ≈ prednisolone > dexamethasone, with IC50 values of 1.67, 2.94, 2.95, and 5.58 nM. Additionally, the limits of detection of dexamethasone, betamethasone, prednisolone, and methylprednisolone were 0.32, 0.14, 0.19, and 0.09 μg/kg in fluorescence polarization assay. Reporter gene assay showed that these GCs induced GR transactivation in a dose‐dependent manner, confirming their GR agonist activities. Among which, dexamethasone at the concentration of 100 nM produced a maximal induction of more than 11‐fold over the blank control. Molecular docking and molecular dynamics simulations suggested that hydrogen‐bonding and hydrophobic interactions played an important role in stabilizing the GC‐GR‐LBD complexes. In summary, this work might help to understand the GR‐mediated endocrine disrupting effects of typical GCs.

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Section: Reporter Gene Assaymentioning

confidence: 99%