青果抗人免疫缺陷病毒活性部位的筛选研究

目的:筛选青果中作用于人免疫缺陷病毒(HIV)gp41抑制HIV-1与靶细胞融合的活性部位。方法:分别用水蒸气蒸馏法、溶剂梯度萃取法获得青果挥发油、青果10%水提液的石油醚、氯仿、乙酸乙酯、正丁醇萃取部位,用酶联免疫吸附(ELISA)法检测以上各部位抑制HIV-1与靶细胞融合的活性;测定活性部位中鞣质的含量,以确定青果中非鞣质成分与活性的关系。结果:青果10%水提液的石油醚、氯仿、乙酸乙酯萃取部位均有较强的抑制HIV-1与靶细胞融合的活性,其半数抑制浓度分别为(3.97±0.38)、(26.78±0.47)、(6.80±0.10)μg.mL-1;各部位中鞣质的含量分别为8.0%、9.6%、32%。结论:青果抑制HIV与靶细胞融合的活性部位为水提液的石油醚、氯仿和乙酸乙酯萃取部位,其中石油醚萃取部位活性最强,且很可能含有非鞣质类的活性物质。

Screening of Inhibitors Targeting HIV from Extracts of Fructus Canarii

OBJECTIVE： To screen HIV - 1 fusion inhibitors targeting HIV gp41 from extracts of Chinese medicinal herb Fructus Canarii. METHODS： The essential oil of Fructus Canarii was extracted by steam - stilling. Other solvent extracts were obtained by extracting Fructus Canarii＇ s water-soluble part with petroleum ether, chloroform, ethyl acetate, and nbutanol in order. A sandwich ELISA assay was applied to screen active HIV fusion inhibitory parts. And the polyphenol content in the active parts were determined to establish the relationship between inhibitory activities and non- polyphenol components. RESULTS： The petroleum ether part, chloroform part and ethyl acetate part had remarkable inhibitory activities on HIV gp41 six-helix bundle formation with IC50 at（3.97±0.38）, （26.78±0.47） and （6.80±0.10） μg · mL^-1, respectively. The content of polyphenols in the three parts was 8.0%, 9.6% and 32%, respectively. CONCLUSION： Among essential oil and solvent extracts of Fructus Canarii＇s water- soluble parts, the petroleum ether part, chloroform part and ethyl acetate part have remarkable inhibitory activities on HIV - 1 gp41 six- helix bundle formation. The petroleum ether part has the strongest inhibitory activities and it is most likely that the non - polyphenol components contribute to the inhibitory activities on HIV - 1 gp41 six- helix bundle formation.