| 摘要: |
| 目的：考察20种四氢萘类化合物体外抗真菌活性。方法：采用NCCLS的M27-A方案,以不同氟康唑敏感性的念珠菌及非念珠菌为供试菌进行体外药敏试验。对化合物22-1、31-1及其盐酸盐22、31,还有化合物34-1、26-1及其溴酸盐34、26进行时间生长曲线实验以及与其他结构抗真菌药进行体外联合药敏试验。结果：该类化合物均具一定抗真菌活性,尤其是化合物31-1对氟康唑敏感白念珠菌的抑菌活性明显强于氟康唑,持续抑菌时间超过54 h;化合物22和22-1对氟康唑耐药白念珠菌及近平滑念珠菌和红色毛癣菌作用强大,MIC50值均〈0.125μg/ml,对于氟康唑耐药的白念珠菌抑菌活性强于酮康唑。此类药物与小檗碱或特比萘芬联用可产生协同作用。结论：四氢萘类化合物结构新颖,体外抗真菌活性显著,值得进一步研究开发 |
| 关键词: 四氢萘类 抗真菌药 微生物敏感性试验 |
| DOI：10.3724/SP.J.1008.2007.00286 |
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| 基金项目:国家自然科学基金（30672626,30572257）. |
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| Detection of in vitro anti-fungal activity of 20 tetralin compounds |
| LIANG Rong-mei, CAO Yong-bing, ZHOU You-jun, WANG Tao, LU Jia, YAO Bin, JIANG Yuan-ying |
| (Department of Pharmacology, School of Pharmacy, Second Military Medical University, Shanghai 200433, China) |
| Abstract: |
| Objective：To investigate the anti-fungal activities of 20 tetralin compounds in vitro. Methods： We adopted the M27-A project recommended by the National Committee for Clinical Laboratory Standard （NCCLS）. Tetralin compounds were tested and selected with several candidal strains and non-candidal strains with different susceptibilities to fluconazole. After obtaining the susceptibility results, we plotted the time-growth curves of several typical tetralin compounds, including compound 22-1, 31-1 and their muriate 22,31, as well as compound 34-1,26-1 and their bromate 34,26. The combination effects of compound 22, 26, 34, 31-1 with other anti-fungal agents （with different structures） were also determined. Results： The 20 tetralin compounds were proven to have different degrees of anti-fungal activities. Compound 31-1 had a stronger anti-fungal activity to FLC-susceptible strains than fluconazole did, and its effect lasted for over 54 h at the concentration of 6 μg/ml. Compounds 22-1 and 22 markedly suppressed the growth of Candida albicans, Candida parapsilosis, and Trichophyton rubrum, with all the MIC50 values less than 0. 125μg/ml. Time-growth curves indicated that the anti-fungal activity of 22-1 on fluconazole-resistant strain was more powerful than that of ketoconazole. Furthermore, tetralin compounds had a synergistic effect with terbinafine and berberine on fluconazole-resistant strains. Conclusion： Tetralin compounds have powerful anti-fungal activities and their structures are different from those of other anti-fungal agents currently used, which provide a basis for developing new anti-fungal agents.[ |
| Key words: tetrahydronaphthalenes anti-fungal agents microbial sensitivity tests |
