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目的寻找对白色念珠菌具有抗真菌作用或与氟康唑具有联合抗真菌作用的活性化合物。方法以美国临床标准化委员会建立的真菌敏感性测定液基稀释法(NCCLSM27-A)评价了8种天然酚类化合物和其6种半合成衍生物对18株临床新近分离的白色念珠菌的抗真菌活性。对具有抗真菌活性的实验化合物进一步进行了与氟康唑的联合抗真菌作用评价。结果化合物albicanylcaffeate对白色念珠菌表现出强的抗真菌活性,MIC为4μg/ml;而化合物大黄素、白藜芦醇、3,4’-二氟二苯乙烯、2,2’-二氟二苯乙烯及2,3’,5’-三氟二苯乙烯显示出中等程度的抗真菌活性,MIC为16μg/ml;双联苄pakyonol、多酚类儿茶素、白藜芦醇二聚体野葡萄素A、3,4,4’-三羟基联苄、2,4’-二氟二苯乙烯、4-氟二苯乙烯及2-甲氧基-4’-氟二苯乙烯显示出较弱的抗真菌活性,MIC为32μg/ml。当与氟康唑联合时,albicanylcaffeate和3,4’-二氟二苯乙烯显示出协同抗真菌活性,而儿茶素与白藜芦醇显示出相加的抗真菌活性。结论所实验的酚类化合物对白色念珠菌具有较强的抗真菌活性,其中部分活性化合物与氟康唑呈现出协同或相加的联合抗真菌作用。在未来抗念珠菌感染的治疗中可能会起到重要的作用。
Objective To find an active compound that has an antifungal activity against Candida albicans or a combination antifungal effect with fluconazole. Methods The fungal susceptibility assay established by the American Committee for Clinical Standardization (FACS) was used to evaluate the antifungal activity of eight naturally occurring phenolic compounds and six semi-synthetic derivatives against 18 clinically newly isolated C. albicans isolates active. Test compounds with antifungal activity were further evaluated for their combined antifungal effect with fluconazole. Results The compound albicanyl caffeate showed strong antifungal activity against C. albicans with a MIC of 4 μg / ml; whereas the compounds emodin, resveratrol, 3,4’-difluorostilbene, 2,2’-difluorobis Styrene and 2,3 ’, 5’-trifluorodistilbene showed moderate antifungal activity with a MIC of 16 μg / ml; dibenzyl pakyonol, polyphenolic catechin, resveratrol dimer Glucosamine A, 3,4,4’-trihydroxybibenzyl, 2,4’-difluorostilbene, 4-fluorostilbene and 2-methoxy-4’-fluorostilbene Weak antifungal activity with a MIC of 32 μg / ml. When combined with fluconazole, albicanylcaffeate and 3,4’-difluorostilbene showed synergistic antifungal activity whereas catechin and resveratrol showed additive antifungal activity. CONCLUSION The tested phenolic compounds have strong antifungal activity against Candida albicans, some of which show synergistic antifungal activity with fluconazole. In the future the treatment of anti-Candida infection may play an important role.