高等学校化学学报 ›› 2018, Vol. 39 ›› Issue (8): 1668-1675.doi: 10.7503/cjcu20180007

• 有机化学 • 上一篇    下一篇

漆斑菌中单端孢霉烯化合物及衍生物的细胞毒活性

贾云静1, 史文思1, 胡飞柳1, 朱华结1(), 刘莉2(), 马正月1   

  1. 1. 河北大学药学院, 2. 医学院, 保定 071000
  • 收稿日期:2018-01-03 出版日期:2018-08-10 发布日期:2018-05-15
  • 作者简介:联系人简介: 朱华结, 男, 博士, 教授, 博士生导师, 主要从事手性计算、 合成及新药研发筛选方面的研究. E-mail: hjzhu2017@163.com;刘 莉, 女, 博士, 讲师, 主要从事化合物药理活性方面的研究. E-mail: ll1113-work@163.com
  • 基金资助:
    河北省教育厅重点项目(批准号: ZD2017004)、 河北省教育厅资助科研项目(批准号: QN2017021)和河北大学“一省一校”资助项目(批准号: 2017030)资助.

Cytotoxic Activity of Trichothecene Compounds and Derivatives from Myrothecium sp.

JIA Yunjing1, SHI Wensi1, HU Feiliu1, ZHU Huajie1,*(), LIU Li2,*(), MA Zhengyue1   

  1. 1. College of Pharmaceutical Sciences,2. College of Medicine, Hebei University, Baoding 071000, China
  • Received:2018-01-03 Online:2018-08-10 Published:2018-05-15
  • Contact: ZHU Huajie,LIU Li E-mail:hjzhu2017@163.com;ll1113-work@163.com
  • Supported by:
    † Supported by the Scientific Research Foundation of Hebei Educational Committee, China(No.ZD2017004), the Scientific Research Foundation of Hebei Educational Committee, China(No.QN2017021) and the Financial Support from “One Province and One School Special Project”of Hebei University, China(No.20170030).

摘要:

从漆斑菌中分离得到了5个单端孢霉烯族化合物, 并确定了其平面结构; 选取其中获得量比较大的化合物进行结构改造, 得到4个新化合物; 分别对这9个化合物进行了抗菌和细胞毒活性测试. 结果表明, 化合物1结构中C12和C13位的环氧环打开后, 重新与C2位形成新的四元环氧环或对C2'位的羟基进行酰基保护后, 化合物的细胞毒活性下降.

关键词: 漆斑菌, 结构改造, 抗菌活性, 细胞毒活性

Abstract:

Five trichothecene compounds were obtained from Myrothecium sp. KX136897 and their structures were confirmed by means of 1H NMR, 13C NMR and HRMS. Compound 1 was used for the further structural modifications and four new derivatives were synthesized. The structure of compound 6 was different from those of the other derivatives, which was identified via comparing its 13C NMR with the reported structure. Furthermore, compound 6 was confirmed by comparing the calculated data with the experimental data of 13C NMR. Compounds 1—9 were used for antibacterial and cytotoxic activity study, respectively. It was found that if the epoxy ring at positions C12 and C13 was opened and then reformed a new four-membered epoxy ring, the cytotoxic activity of compound 1 would decrease. Besides, the protection of hydroxyl at position C2' by acyl would also cause the decrease of cytotoxic activity.

Key words: Myrothecium sp., Structural modification, Antibacterial activity, Cytotoxic activity

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