红花五味子甲素的分离纯化及其抗HIV-1活性的研究

The Isolation of Rubrifloralignan A and Its Anti-HIV-1 Activities

目的:从红花五味子果实中寻找活性代谢产物,研究其抗HIV1活性和作用机制。方法:通过合胞体抑制、HIV1感染细胞保护、HIV1p24抗原测定、融合阻断、逆转录酶和蛋白酶活性分析等实验,检测分离化合物的抗HIV1活性并探讨其作用机制。结果:红花五味子甲素能够抑制病毒诱导的合胞体形成,保护病毒感染细胞,抑制病毒在细胞内的复制。对HIV1感染细胞与正常CD+4细胞间的融合,逆转录酶活性有一定的抑制作用。但是红花五味子甲素不抑制病毒在慢性感染细胞中的复制,也不抑制蛋白酶的活性。结论:首次从天然产物中分离得到红花五味子甲素,它对HIV1病毒复制早期具有抑制作用。

AIM： To isolate bioactive secondary metabolites from the fruits of Schisandra rebriflora （Franch.） Rehd. et. Wils and study their effects on HIV-1 infectivity. METHODS： Inhibition of syncytia formation, HIV-1 reverse transcriptase （RT） and protease （PR）, protection of HIV-1 infected cells, level of HIV-1 p24 antigen,blockage of fusion were detected. RESULTS： A lignan compound, named rubrifloralignan A, was first isolated as a natural product with modest inhibition effects on syncytium formation and HIV- 1 replication and could protect HIV-1 infected cells with weak inhibition effects on fusion and RT, but it showed no effects on the replication of HIV-1 chronic H9 and PR. CONCLUSION： Rubrifloralignan A is an efficient anti-HIV-1 product with effect on early stage of HIV-1 replication.