Evaluation Of The Anti-Inflammatory And Antioxidant Pharmcodynamic Compoents Of Naoxintong Capsules As A Basis Of Broad Spectrum Effects

PHARMACEUTICAL BIOLOGY(2021)

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摘要
ContextNaoxintong capsule (NXT) is one of the most prevalent Traditional Chinese Medicine formulations in the treatment of coronary heart disease (CHD), yet the action of pharmacodynamic components remains unclear.ObjectiveTo determine the basis by which pharmacodynamic components of NXT may be effective in the treatment of CHD.Materials and methodsThe protective effect of NXT (0.01-100 mu g/mL) on 293 T and hy926 cells was determined by MTT assay for 24 h. Afterwards, to investigate the pharmacodynamic material basis of NXT in anti-inflammatory and antioxidant effects, based on previous UPLC/Q-TOF analysis, 293 T and hy926 cells were divided into control (treated with solvent), model (incubated with TNF-alpha, LPS or H2O2), intervention (treated with UPLC components) and positive groups. After 24 h of treatment, all cells were tested to verify the screening results. MOE software was applied to dock bioactive compounds with phosphoinositide 3-kinase (PI3K), then the protein expression and phosphate levels were determined by western blotting.ResultsNXT could significantly inhibit the expression of NF-kappa B, MMP-9 and NO in cells with IC50 values of 0.1178, 0.1182 and 0.1094 mu g/mL. Based on the screening results, six components of NXT were identified (calycosin, ferulic acid, salvianolic acid B, ononin, salvianolic acid E, and salvianolic acid F) which can inhibit NF-kappa B, MMP-9, and NO simultaneously, while exerting cytoprotective effects by inhibiting the activation of the PI3K/AKT pathway under different conditions by virtue of their advantageous interaction with PI3K.ConclusionsThese ingredients have outstanding therapeutic potential and may provide a scientific basis for the future application and research of NXT.
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关键词
High-throughput screening, PI3K, AKT pathway, biological activity ingredients
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