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目的研究白木香内生真菌的抗人类免疫缺陷病毒(HIV)活性,旨在获得具有显著活性的菌株,以寻找新的抗获得性免疫缺陷综合征药物来源,降低生产成本。方法以人类免疫缺陷病毒-1整合酶为靶点,利用人类免疫缺陷病毒-1整合酶链转移反应筛选内生真菌发酵产物的抗人类免疫缺陷病毒活性,并对其中活性最好的一株内生真菌进行了活性指导下的化合物分离。结果不同时期不同地点采集的白木香材料分离所得78株内生真菌,其中有9株真菌显示出良好的活性(抑制率>80%),占总分离菌株的11.54%。其中毛壳菌属菌株球毛壳菌HN-AS-8的发酵液活性最好,IC50为9.44μg·mL-1,从其活性部位得到3个已知化合物,其中化合物1具有一定的人类免疫缺陷病毒整合酶链转移反应抑制活性,IC50为35.4μmol·L-1,化合物1和3为首次从该属真菌中分离得到的化合物。结论白木香的内生真菌具有潜在的抑制人类免疫缺陷病毒-1整合酶活性物质,这为新型抗获得性免疫缺陷综合征药物的开发提供了更丰富的资源。
Objective To study the anti-human immunodeficiency virus (HIV) activity of endophytic fungi from white wood and to obtain a significant active strain in search of a new source of anti-SARS medicine and to reduce the production cost. Methods Human immunodeficiency virus-1 integrase was used as a target to screen the anti-human immunodeficiency virus activity of endogenous fungus fermentation products by human immunodeficiency virus-1 integrase chain reaction. Raw fungi were subjected to activity-directed compound separation. Results 78 strains of endophytic fungi were isolated from different locations in different periods. Among them, 9 strains showed good activity (inhibition rate> 80%), accounting for 11.54% of the total isolates. Among them, the activity of the broth of Chaetomium globosum HN-AS-8 was the best, with an IC50 of 9.44μg · mL-1. Three known compounds were obtained from its active site, of which Compound 1 had certain human immunity Defective virus integrase chain transfer reaction inhibitory activity, IC50 of 35.4μmol·L-1, compounds 1 and 3 for the first time isolated from the genus fungi compounds. Conclusion The endophytic fungi of white wood have the potential to inhibit the activity of human immunodeficiency virus-1 integrase, which provides more abundant resources for the development of new anti-SARS medicine.