天然产物白藜芦醇类似物的合成及其对HIV-1的抑制作用

Synthesis and HIV-1 inhibitory activity of natural products isolated from Gnetum parvifolium and their analogues

摘要:
合成了天然产物白藜芦醇 (12a)、异单叶大黄素 (12b)、银松素 (12c) 及其类似物 (12d～12h), 并筛选了它们的抗HIV-1作用, 部分化合物 (12d、12e、12g) 在培养细胞中显示出抑制HIV-1复制的活性, 其中活性最强的化合物为12d, 它的IC₅₀为1.84 μmol·L⁻¹。

Abstract:
Resveratrol, isorhapontigenin and pinosylvin, isolated from Gnetum parvifolium, and their analogues have been synthesized and tested for their inhibitory activity of HIV-1. Natural product 12a and analogues (12d, 12e, 12g) display significant inhibitory activity of HIV-1 replication. Among them, compound 12d (trans-3, 4, 5, 4'-tetrahydroxystilbene) exhibits the most potent anti-HIV-1 activity with an IC₅₀ value of 1.84 μmol·L⁻¹.