http://jcps.bjmu.edu.cn

中国药学(英文版) ›› 2019, Vol. 28 ›› Issue (8): 527-536.DOI: 10.5246/jcps.2019.08.050

• 【研究论文】 •    下一篇

Bacillus sp. PKU-TA00001中发现的色胺类天然产物

耿彤彤, 王贵阳, 马学洋, 张中义, 刘谈, 葛元洁, 金晶, 孙晓旭, 张英涛, 杨东辉*, 马明*   

  1. 北京大学药学院 天然药物及仿生药物国家重点实验室, 北京 100191
  • 收稿日期:2019-04-19 修回日期:2019-05-12 出版日期:2019-09-02 发布日期:2019-05-26
  • 通讯作者: Tel.: +86-10-82801559; +86-10-82805794, E-mail: mma@bjmu.edu.cn
  • 基金资助:

    National Natural Science Foundation of China (Grant No. 81673332, 81573326, 81741148).

Discovery of tryptamine derivatives from Bacillus sp. PKU-TA00001

Tongtong Geng, Guiyang Wang, Xueyang Ma, Zhongyi Zhang, Tan Liu, Yuanjie Ge, Jing Jin, Xiaoxu Sun, Yingtao Zhang, Donghui Yang*, Ming Ma*   

  1. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
  • Received:2019-04-19 Revised:2019-05-12 Online:2019-09-02 Published:2019-05-26
  • Contact: Tel.: +86-10-82801559; +86-10-82805794, E-mail: mma@bjmu.edu.cn
  • Supported by:

    National Natural Science Foundation of China (Grant No. 81673332, 81573326, 81741148).

摘要:

色胺类天然产物已经在动物、植物和微生物中得到分离并且具有多种生物活性。然而, 相对于大量化学合成的色胺类化合物, 只有有限数量的色胺类天然产物被发现。我们从菌株Bacillus sp. PKU-TA00001中发现了五个色胺类天然产物(15), 其中化合物12是新化合物, 化合物4是新天然产物, 化合物34的核磁共振波谱数据首次被提供。生物活性筛选结果显示, 所有化合物对几株革兰氏阳性菌和阴性菌的最低抑制浓度(MIC)均在50 µM以上, 对人肿瘤细胞株A549, HCT-8MCF-7100 µM下未显示细胞毒活性。化合物14的发现扩展了色胺类天然产物的结构多样性, 并为将来的生物合成和更多生物活性研究打下了基础。

关键词: Bacillus, 菌株优选, 色胺类天然产物

Abstract:

Tryptamine-derived natural products have been discovered from different sources including animals, plants and bacteria,and they show various biological activities. However, they are not discovered widely compared with the large amounts of tryptaminederivatives generated by chemical synthesis. We here report the discovery of five tryptamine-derived natural products (15) and one known polyketide 6 from Bacillus sp. PKU-TA00001. Compounds 1 and 2are new compounds featuring methyl-hexanamide moieties, compound 4is first discovered as a natural product, and 3 and 4’s NMR data are first provided. All compounds showed MIC (minimum inhibitory concentration) values higher than 50 µM against several Gram-positive and negative strains, and showed no cytotoxicity at the concentration of 100 µM against the human cancer cell lines A549, HCT-8 and MCF-7. The discovery of 14expands the structural diversity of tryptamine-derived natural products, and sets the stage for revealing their biosynthetic mechanisms and biological activities in the future.

Key words: Bacillus, Strain prioritization, Tryptamine-derived natural products

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