Bioactive Isoquinoline Alkaloids from Corydalis saxicola
Bioactive Isoquinoline Alkaloids from Corydalis saxicola
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紫堇中的生物活性异喹啉生物碱
DOI：
10.1055/s-0031-1280126
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发表时间：
2012-01-01
期刊：
影响因子：
2.7
通讯作者：
Yin, Ge-Fen
中科院分区：
文献类型：
--
作者：
Huang, Qiao-Qin;Bi, Jun-Long;Yin, Ge-Fen
从岩黄连全草中分得12个异喹啉生物碱，其中包括两个新的含硝基四氢原小檗碱类化合物：（-）2，9-二羟基-3，11-二甲氧基-1，10-二硝基四氢原小檗碱（1）和（+）-4-硝基异阿朴卡维定（2）。新化合物的结构经光谱分析和化学确证。对这些分离物的抑制活性对胆碱酯酶和犬细小病毒进行了评价。化合物1和1a、（+）-1-硝基阿朴卡维啶（5）、小檗碱（8）、巴马汀（9）、脱氢卡维啶（10）和血根碱（11）显示出对乙酰胆碱酯酶的有效抑制活性，IC 50值小于10 μ M，而只有化合物1对犬细小病毒具有弱活性。构效关系研究表明，四氢原小檗碱A环上的硝基取代基导致抗乙酰胆碱酯酶活性的增加。
Twelve isoquinoline alkaloids including two new nitro-containing tetrahydroprotoberberines, (-)2,-9- dihydroxyl-3,11-dimethoxy-1,10-dinitrotetrahydroprotoberberine (1) and (+)-4-nitroisoapocavidine (2), were isolated from the whole plant of Corydalis saxicola Bunting. The structures of the new compounds were established by spectroscopic analysis and chemical evidence. The inhibitory activity of these isolates against cholinesterase and canine parvovirus were evaluated. Compounds 1 and 1a, (+)-1-nitroapocavidine (5), berberine (8), palmatine (9), dehydrocavidine (10), and sanguinarine (11) showed potent inhibitory activity against acetylcholinesterase with IC50 values of less than 10 mu M, while only compound 1 possessed weak activity against canine parvovirus. Structure-activity studies demonstrated that the nitro substituents at ring A in the tetrahydroprotoberberines led to an increase in the anti-acetylcholinesterase activity.