酚类化合物对白色念珠菌的抗真菌活性及其构效关系(英文)  

Antifungal activities of phenolic compounds against Candida albicans and their structure- activityr elationship

作　　者：孙淑娟[1] 郭怀芳[1,2] 娄红祥[1] 葛蔚颖[1] 李宏建[3] 苏乐群[3] 马斌[1] 凌霄[1] 范培红[1] 

机构地区：[1]山东大学药学院植化教研室 [2]山东省科技厅,山东济南250011 [3]山东省千佛山医院药剂科

出　　处：《食品与药品》2006年第03A期30-36,共7页Food and Drug

基　　金：founded by National Natural Science Foundation of China(No.30271537);Teaching Foundation of China Educational Administration.

摘　　要：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 identify active compounds with fluconazole on Candida albicans. Methods The which have antifungal activity or can work synergistically antifungal activities of 8 phenolic compounds isolated from natural resources and 6 semi-synthetic phenolic derivatives against 18 strains of new clinical isolated Candida albicans were evaluated according to NCCLS M27-A broth microdilution protocol. The combination antifungal effects of some active tested compounds with fluconazole were also investigated. Results Compound albicanyl caffeate displayed strong antifungal property with MIC 4 μg/ml, while moderate antifungal effects （MIC16μg/ml） were observed with compounds emodin, resveratrol, 3,4＇-difluorostilbene, 2,2＇-difluorostilbene and 2,3＇,5＇- trifluorostilbene. Pakyonol, catechin, ampelopsin A, 3,4,4＇-trihydroxyl- bibenzyl, 2,4＇-difluorostilbene, 4-fluorostilbene, 2-methyloxy-4＇-fluorostilbene showed lower activity with MIC 32 μg/ml. Synergetic antifungal effects were observed in the combination of albicanyl caffeate or 3,4＇-difluorostilbene and fluconazole, whereas additive antifungal effects were revealed when catechin or resveratrol combined with fluconazole. Conclusion The tested phenolic compounds possess potent anti-candidal activities, and some of them work synergistically or additively with fluconazole. They may play an important role in the treatment of Candida albicans infections.

关 键 词：酚类化合物 白色念珠菌 抗真菌活性 构效关系 联合作用 氟康唑 

分 类 号：R949.751.1[医药卫生—药剂学]