Antifungal Indole Alkaloids from Winchia calophylla
Antifungal Indole Alkaloids from Winchia calophylla
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DOI：
10.1055/s-0042-102459
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发表时间：
2016-03
期刊：
影响因子：
2.7
通讯作者：
Mei-li Yang;Jia Chen;Meng Sun;Dong-bo Zhang;K. Gao
中科院分区：
文献类型：
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作者：
Mei-li Yang;Jia Chen;Meng Sun;Dong-bo Zhang;K. Gao
摘要从凤眼莲抗真菌提取物中分离得到10个吲哚生物碱（1-10），其中2个（2和4）为新化合物。N（4）-甲基-10-羟基-脱乙酰基拉库阿米林（2）是一种阿库阿米林型吲哚生物碱。N（1）-甲基-echitaminic酸（4）是一种不寻常的两性离子，具有基本的长春碱型骨架。这是W.美叶树所有化合物的结构都是基于光谱数据确定的，并且它们的生物活性进行了评估。化合物1显示出对植物病原真菌意大利青霉和香蕉尖孢镰刀菌的有效活性，IC 50分别为10.4和11.5 μM，化合物3抑制立枯丝核菌，IC 50为11.7 μM。化合物2和4在体外对人白血病细胞系HL-60显示出弱的细胞毒性，IC 50分别为51.4和75.3 μM。化合物1和2显示出对乙酰胆碱酯酶的弱活性，IC 50分别约为61.3和52.6 μM。
Abstract Ten indole alkaloids (1–10) were obtained from an antifungal extract of Winchia calophylla, of which two (2 and 4) were new. N(4)-Methyl-10-hydroxyl-desacetylakuammilin (2) was an akuammiline-type indole alkaloid. N(1)-Methyl-echitaminic acid (4) was an unusual zwitterion with a basic vincorine-type skeleton. This is the first report of 10 in W. calophylla. The structures of all of the compounds were determined based on spectroscopic data, and their bioactivities were assessed. Compound 1 showed potent activity against the plant pathogenic fungi of Penicillium italicum and Fusarium oxysporum f.sp cubens with IC50 s of 10.4 and 11.5 µM, respectively, and 3 inhibited Rhizoctonia solani with an IC50 of 11.7 µM. Compounds 2 and 4 showed weak cytotoxicity against the human leukemic cell line HL-60 in vitro with IC50 s of 51.4 and 75.3 µM, respectively. Compounds 1 and 2 displayed weak activity against acetylcholinesterase with IC50 s around 61.3 and 52.6 µM, respectively.