吴茱萸碱
酮康唑
抗真菌
白色念珠菌
化学
铅化合物
红色毛癣菌
微生物学
药理学
体外
生物
生物化学
色谱法
作者
Yan Liang,Honghua Zhang,Xi Zhang,Ying Peng,Jiedan Deng,Yuqing Wang,Ranhui Li,Linyi Liu,Zhen Wang
标识
DOI:10.1016/j.bioorg.2022.105981
摘要
Mycosis, especially superficial fungal infections (SFIs), has been a serious threat to humans in recent years. Evodiamine (EVO), as an effective component of the Traditional Chinese Medicine Evodia rutaecarpa, has good antibacterial effects and low toxicity. In order to find out the potential therapeutic agents against SFIs, a series of EVO derivatives were synthesized and systematic evaluations of antifungal activity were carried out. Among them, compound A7 exhibited great antifungal activity with the values of MIC100 were 38, 38 and 2 μg/mL, respectively, against T. rubrum, T. mentagrophytes and C. albicans, and even stronger than that of ketoconazole (KCZ) with the values of MIC100 were 106, 106 and 3 μg/mL, respectively. Further antifungal evaluations in vitro verified that compound A7 indeed had favorable antifungal activity. Moreover, compound A7 could exert excellent antifungal effect on T. rubrum-infected guinea pigs, suggesting that A7 was an attractive molecule and could be a potential lead compound for the development of anti-fungal agents, and providing a great promising therapeutic strategy for fungal disease.
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