Natural products are the important source for the discovery of more potent anti-HIV agents.In this study,six daphnane diterpenoids including three unreported structures were isolated from Trigonostemon lii,which showe...Natural products are the important source for the discovery of more potent anti-HIV agents.In this study,six daphnane diterpenoids including three unreported structures were isolated from Trigonostemon lii,which showed signifcant activities against HIV-1 strains replication in the nanomolar/picomolar range.Meanwhile,these diterpenoids signifcantly inhibited the fusion of H9/HIV-1 IIIB cells with uninfected C8166 cells,with the EC50s from 1.06 to 8.73 ng/mL,and did not show any inhibition activities against HIV-1 reverse transcriptase.Moreover,all of the diterpenoids shows signifcant inhibitions against T20-resistan HIV-1 strains,PNL4-3gp41(36G)V38E,N42S and pNL4-3gp41(36G)V38A,N42T.The results revealed that the six diterpenoids could be a new type of potential lead candidate as an HIV entry inhibitor,particularly for those infected by T20-resistant variants.展开更多
基金supported financially by grants from the National Science Foundation of China(21432010 and 81660612)Technological leading talent project of Yunnan(2015HA020)+1 种基金Yunnan Applied Basic Research Project-Kunming Medical University Union Foundation(2017FE467(-127),Scientific Research Fund Projects from the Department of Education of Yunnan(2016ZDX042)the Hundred-Talent Program of Kunming Medical University(60117190441).
文摘Natural products are the important source for the discovery of more potent anti-HIV agents.In this study,six daphnane diterpenoids including three unreported structures were isolated from Trigonostemon lii,which showed signifcant activities against HIV-1 strains replication in the nanomolar/picomolar range.Meanwhile,these diterpenoids signifcantly inhibited the fusion of H9/HIV-1 IIIB cells with uninfected C8166 cells,with the EC50s from 1.06 to 8.73 ng/mL,and did not show any inhibition activities against HIV-1 reverse transcriptase.Moreover,all of the diterpenoids shows signifcant inhibitions against T20-resistan HIV-1 strains,PNL4-3gp41(36G)V38E,N42S and pNL4-3gp41(36G)V38A,N42T.The results revealed that the six diterpenoids could be a new type of potential lead candidate as an HIV entry inhibitor,particularly for those infected by T20-resistant variants.
