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无瓣海桑内生真菌Aspergillus sp.ZJ-S4生物碱类次级代谢产物的分离鉴定及抗炎活性

Study on the isolation, identification and anti-inflammatory activity of the secondary metabolites of alkaloids produced by S. apetala-derived fungi Aspergillus sp. ZJ-S4

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【作者】 刘红菊闫冲佘志刚

【Author】 LIU Hongju;YAN Chong;SHE Zhigang;School of Pharmacy, Guangdong Medical University;School of Chemistry, Sun Yat-Sen University;

【机构】 广东医科大学药学院中山大学化学院

【摘要】 目的无瓣海桑内生真菌Aspergillus sp. ZJ-S4生物碱类次级代谢产物的分离鉴定与抗炎活性测定。方法无瓣海桑内生曲霉属真菌(Aspergillus sp.)用大米培养基培养,用多种色谱方法纯化,根据理化数据和波谱数据分别鉴定结构,并考察了部分化合物对LPS诱导RAW 264.7小鼠巨噬细胞产生NO的抑制作用。结果共分离得到11个吲哚生物碱类化合物,分别鉴定为epi-fiscalin E(1),quinadoline D(2),quinadoline A(3),quinadoline B(4),tryptoquivaline L(5),quinadoline E(6),nortryptoquivaline(7),tryptoquivaline(8),27-epi-tryptoquivalin(9),prelapatin B(10),glyantrypine(11)。化合物2、6、7、10对LPS诱导RAW 264.7产生的NO具有一定的抑制作用,IC50在30.2~53.7μmol/L范围内。结论共分离得到11个吲哚生物碱类化合物,其中化合物2和6为新的天然产物,部分化合物显示了较好的体外抗炎活性。

【Abstract】 Objective To study the isolation, identification and anti-inflammatory activity of the secondary metabolites produced by S. apetala-derived fungi Aspergillus sp. ZJ-S4. Methods Endophytic Aspergillus sp. from S. apetala was fermented in solid culture of rice. The secondary metabolites were separated by a combination of chromatographic purification methods and identified by MS, UV, IR and NMR. The inhibitory effects of some compounds on LPS-induced NO production in RAW 264.7 cells were evaluated. Results Eleven indole alkaloids were isolated as epi-fiscalin E(1), quinadoline D(2), quinadoline A(3), quinadoline B(4), tryptoquivaline L(5),quinadoline E(6), nortryptoquivaline(7), tryptoquivaline(8), 27-epi-tryptoquivalin(9), prelapatin B(10),glyantrypine(11). Compounds 2,6,7 and 10 had inhibitory effects on LPS-induced NO production in RAW 264.7 cells, IC50 was in the range of 30.2~53.7 μmol/L. Conclusion Eleven indole alkaloids have been isolated and identified, among which two compounds 2 and 6 are new natural products, some of the compounds show moderate anti-inflammatory activity in vitro.

【基金】 国家自然科学基金项目(41906033);广东省自然科学基金项目(2019A1515012084);广东省自然科学基金重点项目(2016A030311026)
  • 【文献出处】 广东药科大学学报 ,Journal of Guangdong Pharmaceutical University , 编辑部邮箱 ,2021年03期
  • 【分类号】R915
  • 【被引频次】2
  • 【下载频次】265
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