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中国真菌学杂志 2022, Vol. 17  Issue (4): 289-293.

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小G蛋白抑制剂CASIN的体外抗真菌活性研究

巢雯1, 邓忠宇1, 郭士槿1, 郭熠凡1, 阎澜2, 邱丽娟1, 吕权真2   

  1. 1. 海军军医大学基础医学院, 上海 200433;
    2. 海军军医大学药学院, 上海 200433
  • 收稿日期:2021-09-29 出版日期:2022-08-28 发布日期:2022-08-31
  • 通讯作者: 吕权真,E-mail:Lvquanzhen2011@163.com;邱丽娟,E-mail:253867468@qq.com E-mail:Lvquanzhen2011@163.com;253867468@qq.com
  • 作者简介:巢雯,女(汉族),硕士,助教.E-mail:894721254@qq.com
  • 基金资助:
    国家自然科学基金(81902039)

Study on the antifungal activity of small G protein inhibitor CASIN in vitro

CHAO Wen1, DENG Zhongyu1, GUO Shijin1, GUO Yifan1, YAN Lan2, QIU Lijuan1, LV Quanzhen2   

  1. 1. Basic Medicine School of Naval Medical University, Shanghai 200433, China;
    2. School of Pharmacy of Naval Medical University, Shanghai 200433, China
  • Received:2021-09-29 Online:2022-08-28 Published:2022-08-31

摘要: 目的 通过对小G蛋白抑制剂体外抗真菌活性的测定,筛选具有新结构类型的抗真菌活性化合物。方法 采用微量液基稀释法考察不同小G蛋白抑制剂对于念珠菌的最低抑菌浓度(MIC),并从中筛选活性较强的化合物进一步进行抗真菌谱测定;采用时间-生长曲线和时间-杀菌曲线考察CASIN对于白念珠菌生长增殖的影响;采用菌丝诱导实验考察化合物CASIN对于白念珠菌菌丝形成的抑制效果;采用甲基四氮盐(XTT)法考察化合物CASIN对于白念珠菌生物被膜形成的抑制作用。结果 在考察的小G蛋白抑制剂中,CASIN的体外抗真菌活性最强,对于近平滑念珠菌、克柔念珠菌、热带念珠菌、光滑念珠菌中均有较好的抑制作用,MIC为8~16 μg/mL。16 μg/mL CASIN可以有效抑制YPD培养基中白念珠菌的生长增殖,也在RPMI1640培养基中展现出对白念珠菌的杀菌活性;当培养基中CASIN浓度高于8 μg/mL时,白念珠菌菌丝受到明显抑制;此外,8 μg/mL的CASIN浓度对于白念珠菌的被膜生成具有80%以上的抑制率。结论 小G蛋白抑制剂CASIN具有较强的体外抗念珠菌活性。

关键词: 小G蛋白, CASIN, 抗真菌活性

Abstract: Objective In order to find antifungal compounds with new structure, the antifungal activity of small G protein inhibitors were tested in vitro. Methods Micro-dilution method was used to investigate the minimum inhibitory concentration (MIC) of different small G protein inhibitors against Candida. After that, the more active compounds were selected for the further antifungal spectrum determination. Time-growth curves and time-kill curves were used to investigate the effect of CASIN on the growth and proliferation of Candida albicans. Hyphae formation experiment was used to investigate the inhibitory effect of compound CASIN on the formation of Candida albicans hyphae. XTT was used to investigate the inhibitory effect of compound CASIN on the formation of Candida albicans biofilms. Results Among the investigated small G protein inhibitors, CASIN had the strongest in vitro antifungal activity. It also had a good inhibitory effect on Candida parapsilosis, Candida krusei, Candida tropicalis, and Candida glabrata with the MIC of 8-16 μg/mL. 16 μg/mL of CASIN could effectively inhibit the growth and proliferation of Candida albicans in YPD medium, and also exhibited fungicidal activity against Candida albicans in RPMI1640 medium. The hyphae formation of Candida albicans was significantly inhibited by 8 μg/mL of CASIN. 8 μg/mL of CASIN had an inhibition rate of more than 80% for the biofilms formation of Candida albicans. Conclusion CASIN, a small G protein inhibitor, has strong antifungal activity in vitro.

Key words: small G protein, CASIN, antifungal

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