Euanorasetr Jirayut, Junhom Mayura, Tantimavanich Srisurang, Vorasin Onanong, Munyoo Bamroong, Tuchinda Patoomratana, Panbangred Watanalai
a Department of Biotechnology, Faculty of Science , Mahidol University , Bangkok 10400 , Thailand.
b Mahidol University-Osaka University Collaborative Research Center for Bioscience and Biotechnology, Faculty of Science , Mahidol University , Bangkok 10400 , Thailand.
J Asian Nat Prod Res. 2016 May;18(5):462-74. doi: 10.1080/10286020.2015.1133611. Epub 2016 Jan 14.
Altholactone exhibited the anti-fungal activity with a high MIC value of 128 μg ml(-1) against Cryptococcus neoformans and Saccharomyces cerevisiae. Fifteen ester derivatives of altholactone 1-15 were modified by esterification and their structures were confirmed by spectroscopic methods. Most of the ester derivatives exhibited stronger anti-fungal activities than that of the precursor altholactone. 3-Bromo- and 2,4-dichlorobenzoates (7 and 15) exhibited the lowest minimal inhibitory concentration (MIC) values against C. neoformans at 16 μg ml(-1), while the 4-bromo-, 4-iodo-, and 1-bromo-3-chlorobenzoates (11-13) displayed potent activity against S. cerevisiae with MIC values of 1 μg ml(-1). In conclusion, this analysis indicates that the anti-fungal activity of altholactone is enhanced by addition of halogenated benzoyl group to the 3-OH group.
阿尔托内酯对新型隐球菌和酿酒酵母具有抗真菌活性，其最低抑菌浓度（MIC）值高达128μg/ml。通过酯化反应对阿尔托内酯的15种酯衍生物1 - 15进行了修饰，并通过光谱方法确认了它们的结构。大多数酯衍生物表现出比前体阿尔托内酯更强的抗真菌活性。3 - 溴苯甲酸酯和2,4 - 二氯苯甲酸酯（7和15）对新型隐球菌的最低抑菌浓度（MIC）值最低，为16μg/ml，而4 - 溴苯甲酸酯、4 - 碘苯甲酸酯和1 - 溴 - 3 - 氯苯甲酸酯（11 - 13）对酿酒酵母具有强效活性，MIC值为1μg/ml。总之，该分析表明，在3 - OH基团上添加卤代苯甲酰基可增强阿尔托内酯的抗真菌活性。
