摘要
目的考察2-壬基胺基-6-甲氧基四氢萘盐酸盐(10b)体外真菌抗菌活性。方法采用微量液体稀释法考察2-壬基胺基-6-甲氧基四氢萘盐酸盐对19株白念珠菌和15株非白念珠菌的抗菌活性。通过琼脂纸片扩散实验、时间生长曲线实验、IC50值和MFC值测定比较2-壬基胺基-6-甲氧基四氢萘盐酸盐与氟康唑对白念珠菌Y0109的体外抗真菌活性。通过薄层色谱分析(TLC)和透射电镜观察对2-壬基胺基-6-甲氧基四氢萘盐酸盐可能的作用机制进行初步探讨。结果 2-壬基胺基-6-甲氧基四氢萘盐酸盐对白念珠菌的体外抗菌活性优于氟康唑,前者IC50值和MFC值分别为5.41和64μg·mL-1,而后者为337.18和大于256μg·mL-1。2-壬基胺基-6-甲氧基四氢萘盐酸盐能显著降低白念珠菌麦角甾醇的含量,但不影响羊毛甾醇C-14α去甲基酶的活性和细胞膜结构的完整性。结论 2-壬基胺基-6-甲氧基四氢萘盐酸盐结构新颖,对白念珠菌活性强大,值得深入探讨和研究。
OBJECTIVE To investigate the in vitro antifungal activity of 2-nonylamino-6-methoxytetralin hydrochloride （10b）. METHODS The antifungal activities of 10b against 19 Candida albicans （C. albicans） strains and 15 non-C, albicans strains were assayed by microbroth dilution in 96-well plates according to the methods recommended by Clinical and Laboratory Standards Institute （CLSI）. The sensitivity of C. albicans strain Y0109 to 10b and fluconazole （FLC） was compared by agar disk diffusion test, plotting time-growth curves, and determining the values of IC5o and MFC. In addition, the potential mechanism of 10b against C. albicans strains was investigated by using thin-layer chromatography （TLC） assay and transmission electron microscope. RESULTS 10b had stronger in vitro activity than FLC against C. albicans. The values of IC50 and MFC of 10b were 5.41 and 64 μg . mL^-1 while the latter were 337. 18 μg . mL^-1 and 〉256 μg . mL^-1, respectively. 10b markedly reduced ergosterol content in C. albicans but did not affect the activity of lanosterol 146-demethylase （ CYPS1 ） and the integrality of cell membrane structure. CONCLUSION 10b deserves further exploration and investigation for its potent antifungal activity and novel chemical structure.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2014年第6期449-454,共6页
Chinese Pharmaceutical Journal
