五种药用石斛内生真菌抑制HIV-1整合酶活性研究

目的 评价5种药用石斛内生真菌发酵产物抑制HIV-1整合酶的活性.方法 将分离自石斛的202株内生真菌提取物共404个采用高通量ELISA法评价其抑制HIV-l整合酶活性；对抑制活性大于100％的样品进行量效关系考察并进行体外抑制肿瘤细胞活性筛选.结果 筛选得到19个对HIV-l整合酶抑制活性大于80％的样品,其中样品5119F、5297F、5097F、5140J和5211F的抑制率分别达到117.96％、113.53％、108.62％、103.74％和109.02％,其对应的IC50值分别为0.02024、0.003125、0.00862、0.01007 和 0.01192 mg/ml.结论石斛属药用植物内生真菌是一个潜在的、丰富的用于筛选HIV-1整合酶抑制剂的资源库,值得进一步研究和开发.

HIV-1 integrase inhibitory activity of endophytic fungi from five species of medicinal Dendrobium

Objective To evaluate the HIV integrase inhibitory activity of endophvtic fungi in five species of medicinal Dendrobium. Methods The HIV-1 integrase inhibitory activity was detected with high-throughput ELISA. The samples that displayed more than100% inhibitory effect for HIV-1 integrase were selected for dose-response experiments and anticancer activity screening. Results Among all the tested samples, 19 samples inhibited the HIV-1 integrase activity by more than 80%. Specially, the samples 5119F, 5297F, 5097F, 5140J and 5211F inhibited the enzyme activity by 117.96%, 113.53%, 108.62%, 103.74% and 109.02% respectively. The IC50 of the five samples was 0.02024, 0.003125, 0.00862, 0.01007 and 0.01192 mg/ml respectively. Conclusion Endophytic fungi of medicinal Dendrobium are potential and abundant reservoir for the screening of HIV-1 integrase inhibitors and are worthy of further study.