天然产物研究与开发 ›› 2016, Vol. 28 ›› Issue (1): 5-10.doi: 10.16333/j.1001-6880.2016.1.002

• 研究论文 • 上一篇    下一篇

西藏芽孢杆菌XZ7中Amicoumacin类抗生素的分离鉴定与生物活性研究

刘少伟1,夏曼2,高强1,蒋忠科1,胡辛欣1,何琪杨1,游雪甫1,张玉彬2,孙承航1*   

  1. 1 中国医学科学院&北京协和医学院医药生物技术研究所,北京 100050;2 中国药科大学生命科学与技术学院,南京 210009
  • 出版日期:2016-01-29 发布日期:2016-02-01

Isolation,Identification and Bioactivity of Amicoumacin Group Antibiotics Produced by Bacillus Strain XZ7 Isolated from Tibet

LIU Shao-wei1,XIA Man2,GAO Qiang1,JIANG Zhong-ke1,HU Xin-xin1,HE Qi-yang1,YOU Xue-fu1,ZHANG Yu-bin2,SUN Cheng-hang1*   

  1. 1 Institute of Medicinal Biotechnology,Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050,China; 2 College of Life Science and Technology,China Pharmaceutical University,Nanjing 210009,China
  • Online:2016-01-29 Published:2016-02-01

摘要: 采用UPLC-DAD-MS分析发现西藏当雄土壤来源芽孢杆菌XZ7发酵液中的Amicoumacin类化合物,并利用反相柱层析和高效液相色谱对发现的3个Amicoumacin类化合物进行分离纯化;根据紫外光谱、高分辨质谱和核磁共振波谱数据及文献比对,鉴定3个化合物分别为:Bacilosarcin A(1)、Bacilosarcin B(2)和Bacilosarcin C(3)。抑菌实验结果表明化合物2对表皮葡萄球菌和金黄色葡萄球菌具有较强的抑制活性(MIC=4~16 μg/mL);细胞毒性测试结果表明化合物1和2对HepG2肿瘤细胞具有较高的抑制作用,其中化合物2抑制作用最强,IC50值为2.8 μM。同时,化合物2对MCF-7和HeLa肿瘤细胞也有较强的细胞毒作用,IC50值分别为6.2 μM和4.0 μM。

关键词: Amicoumacin, 芽孢杆菌, Bacilosarcin, 葡萄球菌, 细胞毒活性

Abstract: Three Amicoumacin group compounds 1-3 were discovered by UPLC-DAD-MS analysis from the fermentation broth of strain XZ7,a Bacillus sp. isolated from soil of Damxung County in Tibet. The three compounds were isolated by reversed-phase column chromatography and further purified by high performance liquid chromatography. Their chemical structures were elucidated as Bacilosarcin A (1),Bacilosarcin B (2) and Bacilosarcin C (3) by combinational analysis of spectral data including UV,HR-ESI-MS,NMR and comparison with those of literature. Antimicrobial assay showed compound 2 had the strongest antibacterial activity against Staphylococcus epidermidis and Staphylococcus aureus with MIC values of 4-16 μg/mL. Both compound 1 and 2 exhibited cytotoxicity against HepG2 cell line,but compound 2 showed stronger cytotoxic activity with IC50 value of 2.8 μM. Meanwhile,IC50 values of compound 2 against MCF-7 and HeLa cell lines were 6.2 μM and 4.0 μM,respectively.

Key words: Amicoumacin, Bacillus, Bacilosarcin, Staphylococcus, cytotoxicity

中图分类号: 

Q939.92