A new cyclic thiopeptide,berninamycin F(3),three new linear thiopeptides,berninamycins G—I(4-6),and two known berninamycin derivatives,berninamycins C and D(1 and 2)were isolated from Streptomyces sp.CPCC 203702.Thei...A new cyclic thiopeptide,berninamycin F(3),three new linear thiopeptides,berninamycins G—I(4-6),and two known berninamycin derivatives,berninamycins C and D(1 and 2)were isolated from Streptomyces sp.CPCC 203702.Their structures were elucidated through HRESIMS and one-and two-dimensional NMR data,and the absolute configurations were assigned using Marfey's method.Compounds 4-6 are the first examples of linear berninamycin analogs.Notably,compound 4 is the first example of linear thiopeptide with a 1-(oxazol-2-yl)ethan-1-one group,compound 6 is the first linear thiopeptide derivative with methylated oxoacetate moiety.Compounds 1-6 exhibited excellent anti-Zika virus activities with IC_(50) values in the range of 4.4-10.5μmol/L,which were superior to that of the positive control ribavirin(IC_(50)=49.2μmol/L).Compounds 1 and 3 showed strong anti-influenza A virus activities with the IC_(50) values of 15.6 and 3.2μmol/L,respectively.Compound 1 exhibited good antibacterial activities against methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus spp.pathogens.展开更多
基金This work was financially supported by the National Natural Science Foundation of China(Nos.82073744 and 81402835)CAMS Initiative for Innovative Medicine(Nos.2020-I2M-2-010 and CAMS-I2M-3-014)+1 种基金the National Mega-project for Innovative Drugs(Nos.2019ZX09721001-004-006 and 2018ZX09711001-007-001)the National Microbial Resource Center(No.NMRC-2020-3).
文摘A new cyclic thiopeptide,berninamycin F(3),three new linear thiopeptides,berninamycins G—I(4-6),and two known berninamycin derivatives,berninamycins C and D(1 and 2)were isolated from Streptomyces sp.CPCC 203702.Their structures were elucidated through HRESIMS and one-and two-dimensional NMR data,and the absolute configurations were assigned using Marfey's method.Compounds 4-6 are the first examples of linear berninamycin analogs.Notably,compound 4 is the first example of linear thiopeptide with a 1-(oxazol-2-yl)ethan-1-one group,compound 6 is the first linear thiopeptide derivative with methylated oxoacetate moiety.Compounds 1-6 exhibited excellent anti-Zika virus activities with IC_(50) values in the range of 4.4-10.5μmol/L,which were superior to that of the positive control ribavirin(IC_(50)=49.2μmol/L).Compounds 1 and 3 showed strong anti-influenza A virus activities with the IC_(50) values of 15.6 and 3.2μmol/L,respectively.Compound 1 exhibited good antibacterial activities against methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus spp.pathogens.
