In this study,37 derivatives of phorbol esters were synthesized and their anti-HIV-1 activities evaluated,building upon our previous synthesis of 51 phorbol derivatives.12-Para-electron-acceptor-trans-cinnamoyl-13-dec...In this study,37 derivatives of phorbol esters were synthesized and their anti-HIV-1 activities evaluated,building upon our previous synthesis of 51 phorbol derivatives.12-Para-electron-acceptor-trans-cinnamoyl-13-decanoyl phorbol derivatives stood out,demonstrating remarkable anti-HIV-1 activities and inhibitory effects on syncytia formation.These derivatives exhibited a higher safety index compared with the positive control drug.Among them,12-(trans-4-fluorocinnamoyl)-13-decanoyl phorbol,designated as compound 3c,exhibited the most potent anti-HIV-1 activity(EC_(50)2.9 nmol·L^(−1),CC50/EC_(50)11117.24)and significantly inhibited the formation of syncytium(EC_(50)7.0 nmol·L^(−1),CC50/EC_(50)4891.43).Moreover,compound 3c is hypothesized to act both as an HIV-1 entry inhibitor and as an HIV-1 reverse transcriptase inhibitor.Isothermal titration calorimetry and molecular docking studies indicated that compound 3c may also function as a natural activator of protein kinase C(PKC).Therefore,compound 3c emerges as a potential candidate for developing new anti-HIV drugs.展开更多
The average mass concentration of the aerosols in Beijing during the dust storm in the spring of 2000 was -6000 μg · m-3, -30 times as high as that in the non-dust storm days. The enrichment factors of the pollu...The average mass concentration of the aerosols in Beijing during the dust storm in the spring of 2000 was -6000 μg · m-3, -30 times as high as that in the non-dust storm days. The enrichment factors of the pollution elements As, Sb and Se were higher than those in the non-dust storm days. This indicated that As, Sb and Se resulted from the pollution sources of those areas, through which the dust storm passed during their long-range transport, in addition to the local pollution sources in Beijing. The enrichment factors of the Pb, Zn, Cd and Cu were much less than those in the non-dust storm days, suggesting that the local pollution sources in Beijing area contributed to them mostly. The enrichment factors of elements Al, Fe, Sc, Mn, Na, Ni, Cr, V and Co were close to 1, showing that these elements originated from crust. The concentration of S in the dust storm was -10 μg · m-3,4 times as high as that in non-dust storm. S in the aerosols resulted from the adsorption of gaseous SO2 and the consequent展开更多
By Riccati transformation, we establish some oscillation theorems for a class of two-dimensional nonlinear delay differential systems. The results obtained generalize some relatively known results.
基金supported by the National Natural Science Foundation of China(Nos.81202882,82060670)Suzhou Science and Technology Planning Project in Jiangsu Province of China(No.SNG2021022)+1 种基金the Priority Academic Program Development of the Jiangsu Higher Education Institutes,China(PAPD)and the Project of Innovative Research Team of Yunnan Province(No.202005AE160005).
文摘In this study,37 derivatives of phorbol esters were synthesized and their anti-HIV-1 activities evaluated,building upon our previous synthesis of 51 phorbol derivatives.12-Para-electron-acceptor-trans-cinnamoyl-13-decanoyl phorbol derivatives stood out,demonstrating remarkable anti-HIV-1 activities and inhibitory effects on syncytia formation.These derivatives exhibited a higher safety index compared with the positive control drug.Among them,12-(trans-4-fluorocinnamoyl)-13-decanoyl phorbol,designated as compound 3c,exhibited the most potent anti-HIV-1 activity(EC_(50)2.9 nmol·L^(−1),CC50/EC_(50)11117.24)and significantly inhibited the formation of syncytium(EC_(50)7.0 nmol·L^(−1),CC50/EC_(50)4891.43).Moreover,compound 3c is hypothesized to act both as an HIV-1 entry inhibitor and as an HIV-1 reverse transcriptase inhibitor.Isothermal titration calorimetry and molecular docking studies indicated that compound 3c may also function as a natural activator of protein kinase C(PKC).Therefore,compound 3c emerges as a potential candidate for developing new anti-HIV drugs.
文摘The average mass concentration of the aerosols in Beijing during the dust storm in the spring of 2000 was -6000 μg · m-3, -30 times as high as that in the non-dust storm days. The enrichment factors of the pollution elements As, Sb and Se were higher than those in the non-dust storm days. This indicated that As, Sb and Se resulted from the pollution sources of those areas, through which the dust storm passed during their long-range transport, in addition to the local pollution sources in Beijing. The enrichment factors of the Pb, Zn, Cd and Cu were much less than those in the non-dust storm days, suggesting that the local pollution sources in Beijing area contributed to them mostly. The enrichment factors of elements Al, Fe, Sc, Mn, Na, Ni, Cr, V and Co were close to 1, showing that these elements originated from crust. The concentration of S in the dust storm was -10 μg · m-3,4 times as high as that in non-dust storm. S in the aerosols resulted from the adsorption of gaseous SO2 and the consequent
文摘By Riccati transformation, we establish some oscillation theorems for a class of two-dimensional nonlinear delay differential systems. The results obtained generalize some relatively known results.
