ABSTRACT
Aim To explore the differential expression genes (DEGs) and potential therapeutic drugs of neutrophilic asthma (NA) based on bioinformatics analysis and molecular docking. Methods The gene expression profiles of NA were obtained from GEO database, and the differential expression genes were screened. The protein-protein interactions (PPI) of DEGs were obtained from STRING database, and the hub genes were screened by Cytoscape according to the degree of DEGs. The GO and KEGG pathway analysis were performed by DAVID database. Finally, molecular docking technology was used to screen the potential therapeutic drugs for the treatment of NA. Results A total of 147 DEGs were obtained from NA patients compared with healthy people in GEO database. Ten hub genes were screened from PPI network, including CXCL8, FPR2, CXCL1, TNFRSF1B, CXCR1, etc. Go enrichment analysis showed that DEGs were mostly associated with inflammation, immune response and chemotaxis, etc. KEGG pathway analysis indicated that the DEGs were mainly involved in cytokine-cytokine receptor interaction and complement and coagulation signaling pathways. Molecular docking showed that paeoniflorigenone and triptolide had good binding activity with C8B and PLAU. Conclusion Complement and coagulation cascades may become a new therapeutic target of NA. The two screened compounds paeoniflorigenone and triptolide may be potential therapeutic drugs for the treatment of NA.
ABSTRACT
<p><b>OBJECTIVE</b>To investigate the chemical constituents of Patrinia villosa.</p><p><b>METHOD</b>The chemical constituents were isolated by silica gel column chromatography and semi-preparative high-performance liquid chromatography, and identified by physicochemical properties and spectral analysis (MS, 1H-NMR and 13C-NMR).</p><p><b>RESULT</b>Seven compounds were isolated from ethyl acetate and n-butanol extract and identified as: 5-hydroxyl-7, 3', 4'-trimethoxy flavone (I), 5-hydroxyl-7, 4'-dimethoxy flavone (II), luteolin (III), quercetin (IV), isoorientin (V), isovitexin (VI) and 8-C glucosylprunetin (VII).</p><p><b>CONCLUSION</b>Compounds I , II, III, V, VI and VIII were obtained from the plant of genus Patrinia for the first time, compound IV was separated from P. villosa for the first time.</p>
Subject(s)
Apigenin , Chemistry , Luteolin , Chemistry , Patrinia , Chemistry , Plants, Medicinal , Chemistry , Quercetin , ChemistryABSTRACT
<p><b>AIM</b>To study the chemical constituents of Patrinia villosa Juss.</p><p><b>METHODS</b>Solvent extraction, silica gel column and preparative liquid chromatography were used to separate the chemical constituents, and the chemical structures were elucidated by physico-chemical properties and spectra data.</p><p><b>RESULTS</b>Eight compounds were isolated and identified as bolusanthol B (1), (2S)-5, 7, 2', 6'-tetrahydroxy-6,8-di (gamma,gamma-dimethylallyl) flavanone (2), orotinin (3), (2S)-5, 7, 2', 6'-tetrahydroxy-6-lavandulylated flavanone (4), 3'-prenyl-apigenine (5), luteolin (6), quercetin (7) and apigenin (8).</p><p><b>CONCLUSION</b>Compound 2 and 4 are new compounds, compounds 1, 3 and 5 were separated from Patrinia genius for the first time, compounds 6, 7 and 8 were isolated from Patrinia vollosa Juss for the first time.</p>
Subject(s)
Apigenin , Chemistry , Flavanones , Chemistry , Isoflavones , Chemistry , Luteolin , Chemistry , Molecular Conformation , Molecular Structure , Patrinia , Chemistry , Plants, Medicinal , Chemistry , Quercetin , ChemistryABSTRACT
<p><b>AIM</b>To investigate the stereoselective pharmacokinetic process of tetrahydropalmatine (THP) in rats.</p><p><b>METHODS</b>The concentrations of tetrahydropalmatine enantiomers in rat plasma were determined by coupled achiral and chiral HPLC method. The differences in plasma concentrations and pharmacokinetic parameters between the two enantiomers were compared by paired t-test.</p><p><b>RESULTS</b>The plasma levels of l-THP were always higher than those of d-THP in eight rats. There was significant difference between the main pharmacokinetic parameters of the two enantiomers.</p><p><b>CONCLUSION</b>Tetrahydropalmatine showed significant stereoselective pharmacokinetics in rats after an ig dose of the racemate.</p>
Subject(s)
Animals , Female , Male , Rats , Area Under Curve , Berberine Alkaloids , Chemistry , Pharmacokinetics , Chromatography, High Pressure Liquid , Methods , Corydalis , Chemistry , Molecular Structure , Plants, Medicinal , Chemistry , Rats, Sprague-Dawley , StereoisomerismABSTRACT
Objective：To evaluate bioequivalence and relative bioavailability of domestic and imported repaglinide tablets in healthy volunteers. Methods： Twenty two healthy male volunteers were randomized into A and B groups. A single dose (4 mg) of domestic and imported repaglinide tablets were given respectively according to an open 2-way crossover study design. The washout period was 1 week. Plasma concentrations of repaglinide were determined by HPLC method. Results：The pharmacokinetic parameters of domestic and imported drugs were as follows: t1/2 were(0.86±0.24) and (0.83±0.31) h；tmax were( 0.79±0.37) and (0.75±0.41) h；cmax were (52.43±20.92) and (53.32±24.94) μg/L. AUC0-t were (79.87±36.48) and (74.95±30.57) μg*h*L-1，respectively. The relative bioavailability of domestic formulation was (106.55±16.15)%. Conclusion： The results of variance analysis and two one-side t test show that 2 formulations are of bioequivalence.
ABSTRACT
Objective：To evaluate bioequivalence and relative bioavailability of domestic and imported repaglinide tablets in healthy volunteers. Methods： Twenty two healthy male volunteers were randomized into A and B groups. A single dose (4 mg) of domestic and imported repaglinide tablets were given respectively according to an open 2-way crossover study design. The washout period was 1 week. Plasma concentrations of repaglinide were determined by HPLC method. Results：The pharmacokinetic parameters of domestic and imported drugs were as follows: t1/2 were(0.86±0.24) and (0.83±0.31) h；tmax were( 0.79±0.37) and (0.75±0.41) h；cmax were (52.43±20.92) and (53.32±24.94) μg/L. AUC0-t were (79.87±36.48) and (74.95±30.57) μg*h*L-1，respectively. The relative bioavailability of domestic formulation was (106.55±16.15)%. Conclusion： The results of variance analysis and two one-side t test show that 2 formulations are of bioequivalence.