白木香内生真菌发酵产物抑制HIV-1整合酶活性筛选

梁寒峭,温欣,张大为,王春兰,郭顺星

中国药学杂志 ›› 2013, Vol. 48 ›› Issue (16) : 1352-1358.

中国药学杂志 ›› 2013, Vol. 48 ›› Issue (16) : 1352-1358. DOI: 10.11669/cpj.2013.16.007
论著

白木香内生真菌发酵产物抑制HIV-1整合酶活性筛选

  • 梁寒峭,温欣,张大为,王春兰,郭顺星
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HIV-1 Integrase Inhibitory Activity of Endophytic fungi from Aquilaria sinensis (Lour.) Gilg

  • LIANG Han-qiao,WEN Xin,ZHANG Da-wei,WANG Chun-lan,GUO Shun-xing
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摘要

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。

Abstract

OBJECTIVE To investigate the HIV-1 integrase inhibitory activity of endophytic fungi from medicinal plant Aquilaria sinensis (Lour.) Gilg. METHODS HIV-1 integrase inhibitory activity of the isolated endophytic fungi was determined by HIV-1 integrase strand transfer inhibitory activity assay,and the active metabolites of the endophytic fungi with the greatest potential were studied by activity tracking. RESULTS Among 78 strains of endophytic fungi isolated from A. sinensis,nine strains(11.54%) showed strong inhibitory activity against HIV-1 integrase. Three compounds were obtained from the fermentation of strain HN-AS-8 which was identified to be Chaetomium globosum by HIV-1 integrase strand reaction. Compound 1 inhibited HIV-1 integrase with IC50 value of 35.4 μmol·L-1,and compounds 1 and 3 were for the first time isolated from Chaetomium sp. CONCLUSION Potential anti-HIV-1 metabolites exist in the endophytic fungi from A.sinensis,which can be new resources for new anti-AIDS drugs.

关键词

内生真菌 / 抗人类免疫缺陷病毒活性 / 白木香 / 球毛壳菌

Key words

endophytic fungi / anti-HIV-1 activity / Aquilaria sinensis / Chaetomium globosum

引用本文

导出引用
梁寒峭,温欣,张大为,王春兰,郭顺星. 白木香内生真菌发酵产物抑制HIV-1整合酶活性筛选[J]. 中国药学杂志, 2013, 48(16): 1352-1358 https://doi.org/10.11669/cpj.2013.16.007
LIANG Han-qiao,WEN Xin,ZHANG Da-wei,WANG Chun-lan,GUO Shun-xing. HIV-1 Integrase Inhibitory Activity of Endophytic fungi from Aquilaria sinensis (Lour.) Gilg[J]. Chinese Pharmaceutical Journal, 2013, 48(16): 1352-1358 https://doi.org/10.11669/cpj.2013.16.007
中图分类号: R284.1   

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国家自然科学基金资助项目(31170016)

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