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OBJECTIVE:To virtually screen lignanoid compounds with inhibitory effect of histone deacetylase(HDAC)by vir-tual screening method. METHODS:Using“lignanoid”as keyword,requiring CNKI,VIP,PubMed and other database,lignanoid compounds were collected as ligand to establish ligand base, histone deacetylase receptor HDAC2 (PDB code:4LXZ) and HDAC8 (PDB code:1T69) were selected from PDB database,and then ligands and 3D active site of receptors were docked by SYBYL-X 2.0 software. The affinity of receptors to ligand was reflected by total score. RESULTS:345 lignanoid compounds, 4LXZ and 1T69 primary ligand were used to establish ligand base which included 347 ligands. Ligands No.275,271,110,200, 056,258,181,129,037,270,187 were demonstrated good affinity with receptors HDAC2 and HDAC8. Ligands and receptors residue were docked via hydrogen bond. CONCLUSIONS:Lignanoid compounds have inhibitory effect on HDAC;virtual screen-ing method is effective in natural product activity prediction,which can provide quick access to and theoretical guidance for new pharmacological studies of lignanoid compounds.
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OBJECTIVE: To develop a method of quantitative analysis of multi-components by single marker (QAMS) for simultaneous determining six lignanoids in Schisandra chinens(S. chinensis). METHODS: A HPLC method was set up. Lichrosphere C18 column(4.6 mm × 250 mm, 5 μn) was used. Acetonitrile-water was used as gradient mobile phase. The flow rate was 1.0 mL · min-1. The column temperature was 30°C and detection wavelength was 217 nm. A method was developed for QAMS to determine schizandrol A, schizandrol B, schisantherin A, deoxyschizandrin, schizandrin B, and schizandrin C in 5. chinensis. Schizandrol A was selected as internal standard; the relative correction factors (RCF) of schizandrol B, schisantherin A, deoxyschizandrin, schizandrin B, and schizandrin C to schizandrol A were calculated. The contents of the six lignanoids in 12 different batches of S. chinensis were determined by both external standard method and QAMS. The QAMS method was evaluated by comparison of its assay results with that of external standard method. RESULTS: The linear range of schizandrol A, schizandrol B, schisantherin A, deoxyschizandrin, schizandrin B, and schizandrin C were within 0.09-1.62 μg(r=0.9999), 0.0408-0.7344 μg (r=0.9999), 0.0208-0.3744 μg(r=0.9999), 0.0242-0.4356 μg(r=0.9999), 0.0532-0.9576 μg(r=0.9999) and 0.0258-0.4644 μg(r=0.9999), respectively. No significant differences were found between the quantitative results of external standard method and QAMS. CONCLUSION: The developed method is accurate, feasible, and can be used for quality evaluation of S. chinensis.
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Objective: To establish the UPLC fingerprint of Schisandra chinensis. Methods: The chromatographic fingerprint was obtained with Acquity UPLC HSS T3 column (100 mm × 2.1 mm, 1.8 μm) and gradient eluted with acetonitrile and water; The flow rate was 0.5 mL/min, and the column temperature was maintained at 30°C. The detection wavelength was set at 216 nm, and the injection volume was 2 μL. Results: The common mode of UPLC fingerprint of S. chinensis was set up for the first time. There were 21 common peaks in the fingerprints. Schisandrin, schisandrol B, angeloylgomisin H, schisantherin A, schisantherin B, deoxyschizandrin, γ-schisandrin, gomisin N, and schisandrin C were identified by comparing the retention time and their ultraviolet spectra. The similarities of 19 batches of S. chinensis were above 0.970. Conclusion: The method is fast and efficiency. It can be used for the quality evaluation of S. chinensis.
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Objective To investigate the protective effect of Schizandrae Lignanoid(SCL)on the apoptosis of PC12 cells induced by H2O2 and its relative mechanisms.Methods PC12 cells were divided into four groups: control group,model group,high dose SCL(SCL1) group,and low dose SCL(SCL2) group.Apoptosis of PC12 cells was induced by H2O2.The cell activity was determined by MTT,the cell apoptotic rate was determined by Annexin V-FITC/PI and ??m was detected by flow cytometry.The expressions of bcl-2 and bax were detected by immunohistochemistry.Results Compared with model group,SCL increased the survival rate of PC12 cells(P
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Objective To investigate the protective effect of Schizandrae Lignanoid (SCL) on myocardial ischemia reperfusion injury in hyperlipidemic rats and its mechanisms and provide theoretical basis and experiment foundation for treatment of myocardial ischemia complicated with hyperlipidemic disease with SCL in the future. Methods After hyperlipidemic rat models were set up by oral administration of high lipid emulsion,the rats were divided into seven groups: control group,sham group,model group,SCL 60,20,5 mg?kg-1 groups and 200 mg?kg-1 CDT group.After reperfusion,the blood samples taken from the ventricles were assayed for blood lipid;MPO activities of ischemic myocardium were measured;Infarct area of left ventricles was measured by Evens blue-TTC staining,and myocardial pathological changes were also observed.Results Compared with model group, the myocardial infarct area/ventricle area ratios and MPO activities in SCL 60,20,5 mg?kg-1 groups decreased (P