槐花提取化合物K3体外抗HIV-1活性的研究

Anti-HIV-1 Effect of Compound K3 from Flower of Japanese pagoda Tree in Vitro

目的:研究槐花提取化合物K3的体外抗H IV-1活性,并对其抗H IV-1机制进行初步探讨。方法:采用MTT比色法检测化合物对各种细胞的毒性。用合胞体形成计数法,p24抗原捕获ELISA法及RT-PCR等多种方法研究化合物体外抗H IV-1活性。结论:槐花提取化合物K3体外有较好的抗H IV-1活性,能够抑制病毒实验株(H IV-1ⅢB,耐药株(H IV-174V)和临床分离株(H IV-1KM018)等多种病毒株的复制,且其作用机制是多靶点的,不仅可以抑制病毒的进入,还可以抑制H IV-1逆转录酶活性。

Objective ： To investigate the anti-HIV properties of compound K3 purified from Japanese pagoda tree flower as well as its anti-HIV mechanism in vitro. Methods： The cytotoxicity of compound K3 was detected by MTT assay. The anti-HIV activities was measured by syncytium reduction, p24 antigen production and protection for HIV-1 induced cytopathic effects in various HIV-1 strains acute or chronically infected cells system. The mechanism of action of the compound K3 was determined by inhibiting HIV-1 RT activity, cell-to-cell fusion, virus binding and entry into cells. Conclusion： Compound K3 is found to be a potent inhibitor of HIV-1 replication against a various viruses in different cells including laboratory strain （HIV-1 ⅢB ）, drug-resistant （HIV-174v ） and clinical isolates （HIV-1KgMO18） of HIV-1. It indicats that K3 act through at least two clarified antiviral mechanisms： inhibition of HIV-1 entry into cell and inhibition of HIV-1 RT activity.