五种药用石斛内生真菌抑制HIV-1整合酶活性研究  

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

作　　者：祁婧[1] 张大为[1] 陈娟[1] 康永[2] 郭顺星[1] 

机构地区：[1]中国医学科学院北京协和医学院药用植物研究所,北京100193 [2]山西省中医药研究院,太原030012

出　　处：《中国医药生物技术》2013年第1期36-40,共5页Chinese Medicinal Biotechnology

基　　金：国家自然科学基金(31170016)

摘　　要：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-1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-1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0.01192mg/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。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.

关 键 词：石斛属 HIV整合酶抑制剂 药物评价 临床前 内生真菌 

分 类 号：R285[医药卫生—中药学]