Antiviral effects of the combination of glycyrrhizin and ribavirin against influenza A H1N1 virus infection in vivo / 药学学报

Ribavirin is a broad-spectrum antiviral agent and glycyrrhizin has activities of anti-inflammation, immunoregulation and anti-viral infections. To enhance antiviral efficacy and weaken side-effects of ribavirin, antiviral effects of the combination of glycyrrhizin and ribavirin were studied in the present study. Firstly, a mouse model of viral pneumonia was established by inoculation of influenza H1N1 virus. Protective effects of glycyrrhizin and ribavirin used alone or in combination against H1N1 virus infection in mice were evaluated based on the survival rate, lung index and virus titer in lungs of mice. Results showed that the combination of glycyrrhizin and ribavirin significantly inhibited the lung consolidation with a 36% inhibition ratio on the lung swell of infected mice. The combination of the two drugs exhibited synergetic effects on survival of infected mice. The combination of 50 mg · kg(-1) · d(-1) glycyrrhizin and 40 mg · kg(-1) · d(-1) ribavirin resulted a 100% protection for infected mice with a synergetic value of 36, which was significantly higher than the control group and each drug alone. This combination also resulted a significant drop of lung virus titer (P < 0.01), as well as inhibition on the production of proinflammatory cytokines IL-6 (P < 0.01), TNF-α (P < 0.01) and IL-1β (P < 0.05) induced by virus infection compared to the control. The treatment of ribavirin plus glycyrrhizin was more effective in influenza A infection in mice than either compound used alone, which suggested a potential clinical value of the combination of the two agents.

Research on antiproliferative effect of flavones isolated from Laggera pterodonta / 中国中药杂志

<p><b>OBJECTIVE</b>To research the cytotoxicity and in vitro antiproliferative effect of the six flavone compounds extracted from Laggera pterodonta.</p><p><b>METHOD</b>The cytotoxicity on the normal cells and antiproliferative effect on tumor cells were tested by MTT assay, and then the preliminary structure-activity relationship was analysed. The phase distribution of the cell cycle and apoptosis rate were analyzed by flow cytometry.</p><p><b>RESULT</b>The results of MTT assay showed 5,7,3',4'-tetramethoxy-3-hydroxyflavone and chrysosplenetin B inhibited growth of A549 and Hela cells significantly with a dose dependent mode, while exhibited low cytotoxicity to the two normal cells, Vero and EVC304. Both compounds contain ortho-phenolic methoxyl moietys in their structures. Flow cytometry analysis revealed that Hela cells treated with increasing quantities of chrysosplenetin B increased the percentage of cells in the G2/M phase, and Hela and A549 cells treated with increasing quantites of the 5,7,3',4'-tetramethoxy-3-hydroxyflavone and chrysosplenetin B increased the apoptosis rates.</p><p><b>CONCLUSION</b>The 5,7,3',4'-tetramethoxy-3-hydroxyflavone and chrysosplenetin B extracted from L. pterodonta showed high antiproliferative effect on cancer cells with low cytotoxicity on normal cells, and took the effects on A549 and Hela cells through the hold-up of the G2/M phase of the cell cycle and induction of the apoptosis.</p>

Chemical constituents of Laggera pterodonta / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of Laggera pterodonta.</p><p><b>METHOD</b>The ethanol extract of L. pterodonta was isolated by column chromatogramphy on silica gel, ODS, and Sephadex LH-20 to afford compounds. The structures of the obtained compounds were identified by chemical reactions and spectroscopic analysis.</p><p><b>RESULT</b>Nineteen compounds were separated and identified to be pterodondiol (1), ilicic acid (2), artemitin (3), chrysosplenetin B (4), 3,5-dihydroxy-3',4',6,7-tetramethoxyflavone (5), chrysosplenol D (6), 5,6,4'-trihydroxy-3,7-dimethoxyflavone (7), quercetin (8), tamarixetin (9), patuletin (10), quercetin-3-O-beta-D-galactopyranoside (11), patuletin-3-O-beta-D-glucopyranoside (12), helichrysoside (13), 4,5,7-trihydroxy-6-methoxyflavone-3-O-beta-D-rutinoside (14), kaempferol-3-O-beta-D-glucopyranoside (15), stigmasterol (16), stigmasterol 3-O-beta-D-glucopyranoside (17), 2-hydroxy-benzoic acid (18), beta-sitosterol (19).</p><p><b>CONCLUSION</b>Compounds 5, 7, 9-15, and 17-18 were isolated from this plant for the first time. The 13C-NMR data of compound 7 is reported for the first time.</p>

Effect of 3,5-hydroxy-6,7,3',4'-tetramethoxyflavone isolated from Laggera pterodonta on apoptosis of Hep-2 cells in vitro / 中国病理生理杂志

AIM:To investigate the effect of 3,5-hydroxy-6,7,3',4'-tetramethoxyflavone (HTMF) isolated from Laggera pterodonta on Hep-2 cell apoptosis and the underlying mechanism.METHODS:The MTT assay was used to observe the cytotoxicity of HTMF to the normal cells and the inhibitory effect of HTMF on the proliferation of tumor cells.The apoptosis was determined by flow cytometry.Western blotting was used to detect the expression of caspase-3 and caspase-9.RESULTS:HTMF significantly inhibited the growth of Hep-2 cells in dose and time dependent manners.HTMF exhibited weak cytotoxicity to the two normal cell lines Vero and EVC304,while showed low effect of anti proliferation on HepG2 cells and A549 cells.The increase in apoptosis of Hep-2 cells by HTMF was observed with dose and time dependent manners.Western blotting showed that HTMF time dependently increased the expression of caspase 3 and caspase-9 in Hep-2 cells.CONCLUSION:HTMF has high inhibitory effect on the proliferation of Hep-2 cells by induction of apoptosis in the tumor cells through caspase-9 and caspase-3 activation.However,the cytotoxicity of HTMF to the normal cells is low.

Extraction,analysis of sulfated polysaccharides from Grateloupia turuturu Yamada and their antiviral activities / 中国海洋药物

Objective To extract the sulfated polysaccharides from Grateloupia turuturu Yamada and to studyits physico-chemical properties and antiviral activities.Methods The sulfated polysaccharides were extracted from Grateloupia turuturu Yamada by hot water extraction and alcohol precipitation.Two pure polysaccharides were obtained by DEAE-52 cellulose column chromatography.The physico-chemical properties including the composition of the glycoconjugate and the content of the sulfate were analyzed.The antiviral effects of the samples on HSV-1,Cox_(3) and their cytotoxicity to Vero,Hela cell were studied by cytopathic effect(CPE) reduction assay and MTT colorimetric assay.Results The results showed that the glycoconjugate was composed of Gal and slight Glc,Xyl etc.The content of the sulfate group was more than 15%.And the polysaccharides showed good antiviral activities,especially the pure polysaccharides.Their 50% inhibited concentrations(IC_(50))on HSV-1 were(7.81) and 3.91?g?mL~(-1),selectivity index(SI)values were larger than 128 and 256,respectively.Conclusion The sulfated polysaccharides from Grateloupia turuturu Yamada have good antiviral effects on HSV-1 and Cox_(3).