天然产物研究与开发 ›› 2018, Vol. 30 ›› Issue (5): 725-730.doi: 10.16333/j.1001-6880.2018.5.001

• 研究论文 •    下一篇

青蒿素衍生物抗菌机理研究

徐杰1, 邓龙兴1, 胡国元1*, 杨春雷2, 余君2, 杨锦鹏2   

  1. 1绿色化工过程教育部重点实验室 武汉工程大学化工与制药学院,武汉 430205;2湖北省烟草科学研究院,武汉 430030
  • 出版日期:2018-06-04 发布日期:2018-06-04
  • 基金资助:

    中国烟草总公司重点科技项目(110201302015)

Study on Antibacterial Mechanism of Artemisinin Derivatives

XU Jie1, DENG Long-xing1, HU Guo-yuan1*, YANG Chun-lei2, YU Jun2, YANG Jin-peng2   

  1. 1Key Laboratory for Green Chemical Process of Ministry of Education,School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology,Wuhan 430205;2Tobacco Research Institute of Hubei Province, Wuhan 430030,China
  • Online:2018-06-04 Published:2018-06-04

摘要: 前期研究从臭蒿中提取分离出臭蒿抗菌流分Fr.5.2主要成分为青蒿素衍生物。为了研究青蒿素衍生物的抗菌机理,测试Fr.5.2和双氢青蒿素(Dihydroartemisinin ,DHA)对烟草链格孢菌的抗菌活性、细胞膜完整度、胞内物质的泄露、菌体和孢子的影响。结果发现:Fr.5.2对烟草链格孢菌最小抑菌浓度(minimum inhibitory concentration,MIC)为1.25 mg/mL,最小杀菌浓度(minimum bactericidal concentration,MBC)为2.5 mg/mL,DHA对烟草链格孢菌的MIC为10 mg/mL,MBC为10 mg/mL。0.625 mg/mL Fr.5.2和2.5 mg/mL DHA作用于烟草链格孢菌,在0~3 h,细胞膜完整度不断下降,胞内核酸大分子不断流失;SEM观察发现菌丝体细胞膜细小、有空洞,孢子表面也有凹陷;Fr.5.2和DHA还可以抑制麦角甾醇的合成,与空白组相比,麦角甾醇的含量分别降低29.77%,28.99%,孢子平均密度提高,但是萌发率降低。这些实验结果表明,青蒿素衍生物能够抑制真菌麦角甾醇的合成,破坏细胞膜,阻碍真菌细胞的新陈代谢,破坏真菌孢子,能有效的抑制、杀死真菌。

关键词: 臭蒿, 青蒿素衍生物, 双氢青蒿素, 抗菌机理

Abstract: The main ingredient of antibacterial compound Fr.5.2 isolated by Artemisia hedinii (A.hedinii) was Artemisinin Derivatives.The antibacterial activity,the integrity of cell membrane,the leakage of intracellular substances,Scanning Electron Microscopy (SEM) observation of bacteria and their spores were determinated to study the antibacterial mechanism of Fr.5.2 and DHA against A.alternate,.The results showed that the minimum bactericidal concentration(MIC) and minimum bactericidal concentration (MBC) of aganist A.alternate were 1.25 mg/mL and 2.5 mg/mL,respectively,while the MIC and MBC was the same 10 mg/mL of DHA aganist A.alternate.The cell integrity of A.alternate decreased and the intracellular nucleic acid macromolecules losed with the time in 0-3 h as the Fr.5.2 and DHA concentration of 1/2 MIC.SEM observation shows that the cell membrane of mycelium was small,concave and hollow and the surface of the spores was also sunken;The Fr.5.2 and DHA can inhibit the synthesis of ergosterol and lead to its content decreasing by 29.77%,28.99%,respectively,comparing to the control group.The number of spores increased,however,the germination rate decreased.These results indicate that Artemisinin Derivatives show antibacterial effect on fungi,and can cause the inhibition of fungal ergosterol synthesis,the cell membrane destroyed,the metabolism of fungal cells hindered and fungal spores germinated.

Key words: Artemisia hedinii, artemisinin derivatives, dihydroartemisinin, antibacterial mechanism

中图分类号: 

Q946.887 R961