摘要
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。
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 20μmol·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.
作者
郭永华
赵中振
徐畅
刘莹
张媛
王贵阳
张薇
魏胜利
GUO Yong-hua;ZHAO Zhong-zhen;XU Chang;LIU Ying;ZHANG Yuan;WANG Gui-yang;ZHANG Wei;WEI Sheng-li(School of Chinese Materia Medica,Beijing University of Chinese Medicine,Beijing 102488;Institute of Pharmaceutical Biotechnology,Chinese Academy of Medical Sciences,Beijing 100050)
出处
《中南药学》
CAS
2024年第6期1412-1417,共6页
Central South Pharmacy
基金
国家自然科学基金项目(No.81803687)。
关键词
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
Uncaria rhynchophylla
endophytic actinomycete
chemical constituent
secondary metabolite
11β-hydroxysteroid dehydrogenases 1
