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Objective To discover new-structure active molecules in order to provide candidate compounds for anti-radiation drug research.Methods Conformational fixation and functional group conversion strategies were used to modify the structure of Ex-RAD before substituted 2H-benzopyran-3-formylaniline compounds were designed and synthesized.The anti-radiation activities of the synthesized compounds were screened via irradiated cell survival models and the cytotoxicity of the active compounds was examined.Western blotting assay was used to investigate the effects of the optimal compound on the expressions of apoptosis related proteins in irradiated cells.The anti-radiation activity of the optimal compound was evaluated through irradiated mice models.Results Twenty-one target compounds were synthesized,eight of which were found to significantly improve the survival of irradiated cells.Four compounds were selected for re-screening and cytotoxicity evaluation.Compound D19 was determined as the optimal compound that could affect the expressions of apoptosis related proteins in irradiated AHH-1 cells by Western blotting assay.Compared with the radiation group,the 30-day survival rate of D19 treated mice irradiated with 8.6 Gy of whole-body radiation increased by 70%.D19 showed protective effect on the blood system of non-lethal dose irradiated mice.Conclusion The novel compound D19 has shown strong anti-radiation activity and deserves more research.
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SUMMARY Introduction: biofilm-related infections caused by Staphylococcus aureus, Klebsiella pneumoniae and Pseudomonas aeruginosa are difficult to treat and few effective pharmacological options are currently available for this purpose. In this context, coumarin (2H-1-Benzopyran-2-one) has been reported to have antibacterial and antibiofilm activity, but this potential remains poorly understood. Aim: to investigate the action of coumarin on planktonic and biofilm forms of S. aureus, K. pneumoniae and P. aeruginosa. Results: a minimum inhibitory concentration (MIC) of coumarin ranging from 256 to 1024 fig/mL was observed, with a remarkable ability to inhibit the formation of biofilms and to act on mature biofilms in concentrations close to MIC. Conclusion: coumarin has strong activity against planktonic and biofilm forms on the three species of great relevance in the clinical scenario. These results are interesting to enable a pharmacological alternative for the treatment of these infections.
Introducción: las infecciones relacionadas con la biopelícula causadas por Staphylococcus aureus, Klebsiella pneumoniae y Pseudomonas aeruginosa son difíciles de tratar y actualmente existen pocas opciones farmacológicas eficaces para este propósito. En este contexto, se ha informado que la cumarina (2H-1-Benzopiran-2-ona) tiene actividad antibacteriana y antibiofilm, pero este potencial sigue siendo poco conocido. Objetivo: investigar la acción de la cumarina sobre formas planctónicas y de biopelículas de S. aureus, K. pneumoniae y P. aeruginosa. Resultados: se observó una concentración inhibitoria mínima (CMI) de cumarina en el rango de 256 a 1024 µg/mL, con una notable capacidad para inhibir la formación de biofilms y actuar sobre biofilms maduros en concentraciones cercanas a la CMI. Conclusión: la cumarina tiene una fuerte actividad contra las formas planctónicas y biofilm sobre las tres especies de gran relevancia en el escenario clínico. Estos resultados son interesantes para habilitar una alternativa farmacológica para el tratamiento de estas infecciones.
Introdução: as infecções relacionadas ao biofilme causadas por Staphylococcus aureus, Klebsiella pneumoniae e Pseudomonas aeruginosa são difíceis de tratar e poucas opções farmacológicas eficazes estão disponíveis atualmente para esse propósito. Nesse contexto, foi relatado que a cumarina (2H-1-benzopirano-2-ona) tem atividade antibacteriana e antibiofilme, mas esse potencial permanece pouco conhecido. Objetivo: investigar a ação da cumarina sobre as formas planctónicas e de biofilme de S. aureus, K. pneumoniae e P. aeruginosa. Resultados: observou-se uma concentração inibitória mínima (CIM) de cumarina variando de 256 a 1024 µg/mL, com notável capacidade de inibir a formação de biofilmes e de atuar sobre biofilmes maduros em concentrações próximas à CIM. Conclusão: a cumarina possui forte atividade contra as formas planctónicas e de biofilme sobre as três espécies de grande relevância no cenário clínico. Esses resultados são interessantes para possibilitar uma alternativa farmacológica para o tratamento dessas infecções.
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Objective: To establish UPLC-Q/TOF method for simultaneous qualitative and quantitative analysis of main chemical components in Sinodielsia yunnanensis. Methods: High performance liquid chromatography tandem flight time mass spectrometry was used. Chromatographic column was Agilent shell 120 Hilic, and the flow phase was acetonitrile-0.1% acid aqueous solution (gradient elution) at a flow rate of 0.3 mL/min; Qualitative and quantitative analysis adopted Q-TOF positive anion full scanning + IDA (information correlation acquisition) mode. Results: Using the established screening database, the target compounds with a mass error of less than 5×10-6, a correct isotope distribution and fragment ion are used as the target compounds. Combined with software Formula Finder, Mass Calculators and other functions, online database (Human Metabolome Database, PubChem, Chemical Book, etc.), and two stage fragmentation rule, 23 compounds were identified by qualitative identification. Ferulic acid was determined as a quantitative indicator component, and the quantitative and qualitative ions were 178 and 149, respectively; The linear range was 1.14-1 140 ng/mL (r = 1.000), and the limits of detection and quantitation respectively was 0.87 ng/mL and 2.91 ng/mL; RSDs of precision, stability, and reproducibility tests were lower than 2%; The recovery rate was 98.13%-101.25% (RSD = 1.37%, n = 5). Conclusion: This method has high sensitivity, good reproducibility, and its analysis is fast, accurate, and reliable, and it can be used for simultaneous qualitative and quantitative determination of main chemical components in the medicinal materials of S. yunnanensis; The content of ferulic acid in Yunnan is higher than that in Tibet.
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Objective: To study the chemical constituents from the fruits of Cudrania cochinchinensis. Methods: The ethanol extract from the fruits of C. cochinchinensis was separated by silica column chromatography, and the structures were elucidated based on spectroscopy and X-ray diffraction. Results Two known benzopyran isoflavones were isolated and elucidated as 4'-O-methylalpinmumisoflavone (1) and isoderrone (2). The crystal structures showed compounds 1 and 2 belonged to monoclinic system, the space group was P2 (1)/c, and the 3D-supramolecular structures were accumulated by hydrogen bond in intra-and inter-molecule, π-π deposition, and Van der Waals force. The in vitro inhibition on BEL-7404 and SGC-7901 carcinoma cell lines was investigated and the results showed compound 2 had a distinct antiproliferative activity. Conclusion: Compound 1 is isolated from this plant and compound 2 from the plants in this genus for the first time. The plane crystal structures of compounds 1 and 2 are determined by X-ray crystal diffraction, and the 3D stack structures are also reported for the first time.
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Antifungal activity of bioactive compound 2H-Furo[2,3-H]-1-benzopyran-2-one isolated from seeds of Psoralea corylifolia L. were tested against eight Fusarium species of maize seeds at 100- 1000ppm concentration. F. moniliforme, F. oxysporum, F. semitectum and F. solani were completely inhibited at 600ppm concentration. F. equiseti, F. lateritium and F. proliferatum were completely inhibited at 700ppm concentration and F. graminearum was inhibited at 800 ppm concentration. Significant inhibition was also observed from 100-500ppm concentration in all the test fungi. Compared to synthetic fungicide Thiram recorded significant antimicrobial activity than Captan tested at 2000ppm concentration. Minimum Inhibitory Concentration (MIC) was also determined for all the species of Fusarium tested. In dry mycelia weight analysis, the mycelia growth all the species of Fusarium were completely inhibited at 500-650 ppm concentration of the bioactive compound.
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Objective: To study the polyphenols from the leaves of Olea europaea. Methods: The polyphenols from ethyl acetate fraction were separated and purified by silica chromatographic method and identified by spectroscopic analysis. Results: In combination with the data from literatures, the structure of 15 polyphenols had been elucidated on the basis of various spectroscopic methods, including tyrosol (1), hydroxytyrosol (2), hydroxytyrosol acetate (3), 1H-2-benzopyran-6,7-diol (4), 3,4-dihydroxyl-benzoic acid (5), 3-methoxyl-4-hydroxyl benzoic acid (6), isorhamnetin (7), eriodictyol (8), taxifolin (9), quercetin (10), luteolin (11), ligstroside (12), oleuropein (13), apigenin-7-O-glucoside (14), and luteolin-7-O-glucoside (15). Conclusion: Compounds 4-9 are isolated from this plant for the first time.
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Aim To determine whether pranlukast (ONO-1078), a cysteinyl leukotriene receptor antagonist, possesses therapeutic effect when administered after focal cerebral ischemia in mice. Methods Persistent focal cerebral ischemia was induced by middle cerebral artery occlusion. Pranlukast and edaravone, a positive control drug, were ip injected 1, 6 and 24 h after ischemia. The neurological deficits were evaluated by neurological scores and inclined plane test 24 and 48 h after the surgery. Forty-eight h later, the brain slices were prepared for measurements of infarct volume and the ratio of ischemic/non-ischemic hemispheres. Brain sections were cut and examined for neuron densities in different regions of the brain. The effects of pranlukast and edaravone were evaluated by the changes of these variables. Results Pranlukast (0.1 and 0.2 mg?kg -1) and edaravone (3 and 10 mg?kg -1) significantly reduced the neurological deficits, infarct volume (maximally 82.3%), ratio of ischemic/non-ischemic hemispheres, and attenuated the reduction of neuron densities in hippocampal CA1 region, cortex and striatum. Conclusion Pranlukast possesses therapeutic effect on ischemic insults when administered after ischemia as effective as edravone, indicating a therapeutic potential in the treatment of ischemic stroke.