高等学校化学学报 ›› 2018, Vol. 39 ›› Issue (4): 674-680.doi: 10.7503/cjcu20170636

• 有机化学 • 上一篇    下一篇

β-咔啉衍生物的抗肿瘤及抗菌活性

刘莉1, 马洋洋2, 王宽1, 贾云静2, 李婉2, 朱华结2()   

  1. 1. 河北大学医学院, 2. 药学院, 保定071000
  • 收稿日期:2017-09-21 出版日期:2018-04-10 发布日期:2018-03-18
  • 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研究. E-mail:zhuhuajie@hotmail.com
  • 基金资助:
    河北省教育厅科研项目(批准号: QN2017021)和河北大学“一省一校”专项项目(批准号: 2017030)资助

Anti-tumor and Antimicrobial Activities of β-Carbolines

LIU Li1, MA Yangyang2, WANG Kuan1, JIA Yunjing2, LI Wan2, ZHU Huajie2,*()   

  1. 1. College of Medicine, 2. College of Pharmaceutical Sciences, Hebei University, Baoding 071000, China
  • Received:2017-09-21 Online:2018-04-10 Published:2018-03-18
  • Contact: ZHU Huajie E-mail:zhuhuajie@hotmail.com
  • Supported by:
    † Supported by the Scientific Rsearch Foundation of Hebei Educational Committee, China(No.QN2017021) and the Project from “A Province and A School” of Hebei University, China(No.2017030)

摘要:

L-色氨酸为原料合成了72个不同取代基的β-咔啉化合物, 其中31个新化合物, 包括12对手性化合物. 采用噻唑蓝(MTT)法对5种肿瘤细胞株及5种菌株进行了体外抗肿瘤活性、 抗菌活性的筛选及构效关系研究. 生物活性测试结果表明, 部分目标化合物具有一定的抗肿瘤活性(化合物3b对A549细胞的IC50=3.17 μmol/L), 且具有不同程度的抑菌活性(化合物5h对鳗弧菌的MIC=0.78 μmol/L).

关键词: β-咔啉化合物, 抗菌活性, 抗肿瘤活性, 手性化合物

Abstract:

A series of β-carbolines possessing different substituents at C1, C3 and N9 positions derived from L-tryptophan was used in anti-tumour and antimicrobial activity study. Compound 3b exhibited anti-tumour activity against tumour cell line A459 with a IC50 value of 3.17 μmol/L in vitro by methyl thiazolyl tetrazolium(MTT) assay while the positive control group(cis-platin, DDP) was 1.45 μmol/L. Other eleven compounds showed relatively weak activities against the five cell-lines. Compound 5h exhibited activitiy against vibrio anguillarum with a MIC value of 0.78 μmol/L while the positive control group(ciprofloxacin) was 1.25 μmol/L. Other fourteen compounds showed relatively weak activities against five spices of bacteria. By the study of structural-activity relationship, optimizing structures is possible and necessary in the future to screen potential compounds for medicinal study.

Key words: β-Carboline, Antimicrobial activity, Anti-tumor activity, Chiral compound

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