New 5,22E-cholestadienol derivatives with broad-spectrum bactericide activity and mechanism of targeted molecule

【作者】 吕碧玉； 高嘉宇； 刘坤； 杨强强； 尹卫平；

【Author】 Biyu Lv;Jiayu Gao;Kun Liu;Qiangqiang Yang;Weiping Yin;School of Chemical Engineering and Pharmaceutics,Henan University of Science and Technology;School of pharmaceutical engineering,Harbin university of commerce;

【机构】 河南科技大学化工与制药学院； 哈尔滨商业大学；

【摘要】 This study mainly focuses on compound 1 and 2 of a new class of 5, 22 E-cholestadienol derivatives from Buthus martensi kirsch with broad-spectrum bactericide activity related to insect secondary metabolites. A powerful weapon against bacteria maybe from the insects and animals living in polluted environments has been reported. A preliminary study on the mechanism of action was carried on evaluating the inhibition of target protein D inhibitor(PDB ID: 2 XRL) for the 5, 22 E-cholestadienol derivatives. Result showed that the compound 2 has strong bactericide activity resistance to pathogen against S. aureus ATCC25923 and P. aeruginosa ATCC27853 with MICs of 16 μg/mL and MBCs of 32 μg/mL and 48 μg/mL, respectively. Structures of compound 1-3 were established by comprehensive spectroscopic analysis including 2 D-NMR and HSESI-MS studies.更多还原

【Abstract】 This study mainly focuses on compound 1 and 2 of a new class of 5, 22 E-cholestadienol derivatives from Buthus martensi kirsch with broad-spectrum bactericide activity related to insect secondary metabolites. A powerful weapon against bacteria maybe from the insects and animals living in polluted environments has been reported. A preliminary study on the mechanism of action was carried on evaluating the inhibition of target protein D inhibitor(PDB ID: 2 XRL) for the 5, 22 E-cholestadienol derivatives. Result showed that the compound 2 has strong bactericide activity resistance to pathogen against S. aureus ATCC25923 and P. aeruginosa ATCC27853 with MICs of 16 μg/mL and MBCs of 32 μg/mL and 48 μg/mL, respectively. Structures of compound 1-3 were established by comprehensive spectroscopic analysis including 2 D-NMR and HSESI-MS studies.更多还原