Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (9): 2420-2426.DOI: 10.6023/cjoc201805045 Previous Articles     Next Articles

Special Issue: 合成科学

Articles

通过保罗酸的加成提高保罗霉素的稳定性

唐越a,b, 王敏a, 丁勇a,b, 李金娥a, 陈义华a,b   

  1. a 中国科学院微生物研究所 微生物资源前期开发国家重点实验室 北京 100101;
    b 中国科学院大学 北京 100049
  • 收稿日期:2018-05-28 修回日期:2018-06-22 出版日期:2018-09-25 发布日期:2018-07-05
  • 通讯作者: 陈义华 E-mail:chenyihua@im.ac.cn
  • 基金资助:

    国家自然科学基金(No.31670032和31522001)资助项目.

Improvement of Paulomycin Stability by Addition of Paulic Acid

Tang Yuea,b, Wang Mina, Ding Yonga,b, Li Jinea, Chen Yihuaa,b   

  1. a State Key Laboratory of Microbial Resources, Institute of Microbiology, Chinese Academy of Sciences, Beijing 100101;
    b University of Chinese Academy of Sciences, Beijing 100049
  • Received:2018-05-28 Revised:2018-06-22 Online:2018-09-25 Published:2018-07-05
  • Contact: 10.6023/cjoc201805045 E-mail:chenyihua@im.ac.cn
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 31670032 & 31522001).

Paulomycins are a group glycoside antibiotics produced by Streptomyces, which not only show excellent antibacterial activities against gram-positive bacteria, but also display good antitumor activities. The paulic acid moiety is one of the structures that cause the instability of paulomycin. This study aimed to improve the stability of paulomycins. When small molecule thiol compound N-acetylcysteamine (SNAC) was added to the fermentation broth of paulmycin producing strain, four new paulomycin derivatives of palsimycins A, B, C, and D were obtained. The antibacterial activity evaluation showed that the minimal inhibit concentrations (MICs) of palsimycin A and palsimycin B against the tested strains were at the same level as those of paulomycin A and paulomycin B. The stability test revealed that under the same conditions, palsimycin A, B, C, and D were all more stable than paulomycin A and paulomycin B. In conclusion, without scarifying the antibacterial activity, this study increased the stability of paulomycin by the addition of paulic acid with SNAC, which laid a foundation for further research and application of paulomycins.

Key words: paulomycin, structure identification, stability, antibacterial activity