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钩藤内生放线菌Streptomyces sp.IMW-B19化学成分研究

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目的 研究钩藤内生放线菌Streptomyces sp.IMW-B19发酵产物的次生代谢产物及部分化合物的生物活性.方法 该菌株的发酵产物采用ODS、Sephadex LH-20、半制备HPLC等色谱技术进行分离纯化,并采用ESI-MS和NMR鉴定化合物的化学结构.使用人肝癌HepG2 细胞评价化合物1 对 11β-羟类固醇脱氢酶 1 活性的影响.结果 共分离得到 11 个化合物,经多种波谱数据分析和文献对比,分别鉴定为actiphenol(1)、苯甲酸薄荷酯A(2)、cyclo(L-Pro-L-Phe)(3)、胸苷(4)、11-hydroxy-4-amorphen-15-oic acid(5)、3-吲哚甲酸甲酯(6)、苯乙酸(7)、1-(3-ethylphenyl)-ethane-1,2-diol(8)、亚油酸(9)、亚油酸甲酯(10)和2-氨基-4-甲氧基苯甲酸(11).化合物1对11β-羟类固醇脱氢酶1具有明显的抑制作用,在20 μmol·L-1时,抑制率达到86.01%.结论 从钩藤内生放线菌Streptomyces sp.IMW-B19发酵产物中共分离得到 11 个化合物,其中化合物4、5、8 为首次从链霉菌属的放线菌中分离得到.化合物1对11β-羟类固醇脱氢酶1具有明显的抑制作用.
Chemical components of endophytic actinomycetes Streptomyces sp.IMW-B19 from Uncaria rhynchophylla
Objective To determine the chemical components and their bioactivity of secondary metabolites from fermentation products of Streptomyces sp.IMW-B19 from Uncaria rhynchophylla.Methods The fermentation products of this strain were separated and purified by ODS,Sephadex LH-20,semi-prepartic HPLC and other chromatographic techniques,and the chemical structures of the compounds were identified by ESI-MS and NMR.Human liver cancer(HepG2)cells were used to evaluate the effect of compound 1 on the activity of 11β-hydroxysteroid dehydrogenase 1(11β-HSD1).Results Totally 11 compounds were obtained and identified as actiphenol(1),menthyl phenatate A(2),cyclo(L-Pro-L-Phe)(3),thymidine(4),11-hydroxy-4-amorphen-15-oic acid(5),methyl indole-3-carboxylate(6),phenylacetic acid(7),1-(3-ethylphenyl)-ethane-1,2-diol(8),linoleic acid(9),methyl linoleate(10)and 2-amino-4-methoxybenzoic acid(11).Compound 1 greatly inhibited 11β-HSD1,and the inhibition rate reached 86.01%at the concentration of 20 μmol·L-1.Conclusion Totally 11 compounds have been obtained,and compounds 4,5 and 8 are isolated from actinomycetes of the genus Streptomyces for the first time.Compound 1 shows obvious inhibion on 11β-HSD1.

Uncaria rhynchophyllaendophytic actinomycetechemical constituentsecondary metabolite11β-hydroxysteroid dehydrogenases 1

郭永华、赵中振、徐畅、刘莹、张媛、王贵阳、张薇、魏胜利

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北京中医药大学 中药学院,北京 102488

中国医学科学院医药生物技术研究所,北京 100050

钩藤 内生放线菌 化学成分 次生代谢产物 11β-羟类固醇脱氢酶1

国家自然科学基金

81803687

2024

中南药学
湖南省药学会

中南药学

CSTPCD
影响因子:0.736
ISSN:1672-2981
年,卷(期):2024.22(6)
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