Objective:To study the chemical constituents of the EtOAc extract of Armillaria gallica 012m.Methods:The chemical constituents of the EtOAc extract of A.gallica 012m were isolated and purified by various column chroma...Objective:To study the chemical constituents of the EtOAc extract of Armillaria gallica 012m.Methods:The chemical constituents of the EtOAc extract of A.gallica 012m were isolated and purified by various column chromatography and their structures were elucidated on the basis of the 1D and 2D NMR spectroscopic and HRESIMS data.Cytotoxicity of all isolates against A549,HCT-116,M231 and W256 human tumor cells was determined by the MTT method.Results:A new sesquiterpene aryl ester,armimelleolide C(1),and eight known ones including armillarivin(2),melleolide F(3),6'-chloromelleolide F(4),melleolide(5),melleolide K(6),melledonol(7),13-hydroxydihydromelleolide(8),and armillane(9),were isolated from the EtOAc extract of A.gallica 012m.All isolates showed potential cytotoxic activities against at least one of the human cancer cell lines with IC_(50) values ranging from(3.17±0.54)to(17.57±0.47)μmol/L.Compound 1 showed significant inhibitory activity against M231 with an IC_(50) value of(7.54±0.24)μmol/L compared with paclitaxel as the positive control.Compounds 2,3,and 7,9 showed obvious inhibitory activity against HCT-116 and were better than that of the positive control.Conclusion:The chemical constituents including a new sesquiterpene aryl ester armimelleolide C(1)from the EtOAc extract of A.gallica 012m have a variety of structures and potential antitumor activities.展开更多
Eleven new 1-{5-[4-（benzyloxy）phenyl]-3-methyl-4,5-dihydropyrazol-l-yl} oxime ester dcrivatives were synthesized and characterized by elemental analysis, HRMS, ^1H NMR data. All the compounds were screened for their...Eleven new 1-{5-[4-（benzyloxy）phenyl]-3-methyl-4,5-dihydropyrazol-l-yl} oxime ester dcrivatives were synthesized and characterized by elemental analysis, HRMS, ^1H NMR data. All the compounds were screened for their antibacterial potential in vitro against Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. The results indicate that compounds 8c and 8f possess potent activity with the minimum inhibitory concentrations（MIC） of 1.562--3.125 ug/mL against all the four bacteria. Compounds 8c, 8e and 8f show moderate inhibition against the DNA gyrase（IC50=1.9--2.5 ug/mL）. On the basis of the biological activities, structure-activity relationship was discussed.展开更多
A simple, efficient and low-cost methodology for the synthesis of α-aryl-α,β-unsaturated esters using paraformaldehyde as a source of carbon was developed. Factors that control reaction yields such as temperature, ...A simple, efficient and low-cost methodology for the synthesis of α-aryl-α,β-unsaturated esters using paraformaldehyde as a source of carbon was developed. Factors that control reaction yields such as temperature, concentration and reaction time were evaluated. A mechanism is proposed based on experimental structures of the intermediates.展开更多
基金This project was in part supported financially by National Natural Science Foundation of China(Nos.31960095 and 82160670)National Natural Science Foundation of Yunnan Province(Nos.202101AS070022 and 202201AT070228)Yunnan Ten thousand Talents Program to Weiguang Wang and Yanping Li.
文摘Objective:To study the chemical constituents of the EtOAc extract of Armillaria gallica 012m.Methods:The chemical constituents of the EtOAc extract of A.gallica 012m were isolated and purified by various column chromatography and their structures were elucidated on the basis of the 1D and 2D NMR spectroscopic and HRESIMS data.Cytotoxicity of all isolates against A549,HCT-116,M231 and W256 human tumor cells was determined by the MTT method.Results:A new sesquiterpene aryl ester,armimelleolide C(1),and eight known ones including armillarivin(2),melleolide F(3),6'-chloromelleolide F(4),melleolide(5),melleolide K(6),melledonol(7),13-hydroxydihydromelleolide(8),and armillane(9),were isolated from the EtOAc extract of A.gallica 012m.All isolates showed potential cytotoxic activities against at least one of the human cancer cell lines with IC_(50) values ranging from(3.17±0.54)to(17.57±0.47)μmol/L.Compound 1 showed significant inhibitory activity against M231 with an IC_(50) value of(7.54±0.24)μmol/L compared with paclitaxel as the positive control.Compounds 2,3,and 7,9 showed obvious inhibitory activity against HCT-116 and were better than that of the positive control.Conclusion:The chemical constituents including a new sesquiterpene aryl ester armimelleolide C(1)from the EtOAc extract of A.gallica 012m have a variety of structures and potential antitumor activities.
基金the Student Research Train Project of Anhui University of Technology(No.08021)
文摘Eleven new 1-{5-[4-（benzyloxy）phenyl]-3-methyl-4,5-dihydropyrazol-l-yl} oxime ester dcrivatives were synthesized and characterized by elemental analysis, HRMS, ^1H NMR data. All the compounds were screened for their antibacterial potential in vitro against Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. The results indicate that compounds 8c and 8f possess potent activity with the minimum inhibitory concentrations（MIC） of 1.562--3.125 ug/mL against all the four bacteria. Compounds 8c, 8e and 8f show moderate inhibition against the DNA gyrase（IC50=1.9--2.5 ug/mL）. On the basis of the biological activities, structure-activity relationship was discussed.
文摘A simple, efficient and low-cost methodology for the synthesis of α-aryl-α,β-unsaturated esters using paraformaldehyde as a source of carbon was developed. Factors that control reaction yields such as temperature, concentration and reaction time were evaluated. A mechanism is proposed based on experimental structures of the intermediates.
