Instituto de Química, Universidade Federal da Bahia, Salvador-BA, Brazil.
Pharm Biol. 2013 Jul;51(7):936-9. doi: 10.3109/13880209.2013.770536. Epub 2013 Apr 9.
Cratylia mollis Martius ex Benth. and Cenostigma macrophyllum Tul. (Leguminosae) are both endemic Brazilian plants and they are used by the natives as medicinal plants, and the leaves of C. mollis are also employed as forage for cattle during the dry season of region.
Isolation of the compounds responsible for the acetylcholinesterase (AChE) inhibition from the CHCl3 active extract.
Two peptidic compounds were isolated by chromatographic techniques from the CHCl3 extract of the leaves of C. mollis and C. macrophyllum. They were identified by spectrometric data analysis (MS and NMR) and they were subjected to AChE inhibition employing Ellman's test.
The peptides were identified as N-benzoylphenylalaninoyl-phenlyalaninolacetate (aurentiamide acetate) (1) and N-benzoylphenylalaninyl-N-benzoylphenylalaninate (2). Both peptides 1 and 2 exhibit AChE inhibition, with IC50 values equal to 111.34 µM and 137.6 µM, respectively.
Compound 1 (aurentiamide acetate) has rarely been isolated from the Leguminosae family, and N-benzoylphenylalaninyl-N-benzoylphenylalaninate (2) is a compound that has never previously been isolated from this family. Compound 1 is shown to be a potent inhibitor of AChE, with IC50 values similar to the physostigmine control (141.51 µM).
Cratylia mollis Martius ex Benth. 和 Cenostigma macrophyllum Tul.（豆科）都是巴西特有的植物，被当地人用作药用植物，而 C. mollis 的叶子在该地区的旱季也被用作牛的饲料。
从 CHCl3 活性提取物中分离出负责乙酰胆碱酯酶（AChE）抑制的化合物。
通过色谱技术从 C. mollis 和 C. macrophyllum 的叶子的 CHCl3 提取物中分离出两种肽类化合物。通过光谱数据分析（MS 和 NMR）对它们进行鉴定，并通过 Ellman 试验对它们进行 AChE 抑制测试。
鉴定出的肽类化合物为 N-苯甲酰基苯丙氨酰-苯丙氨醇乙酸酯（奥伦蒂酰胺乙酸酯）（1）和 N-苯甲酰基苯丙氨酰-N-苯甲酰基苯丙氨酸（2）。两种肽 1 和 2 都表现出 AChE 抑制作用，IC50 值分别为 111.34 µM 和 137.6 µM。
化合物 1（奥伦蒂酰胺乙酸酯）很少从豆科植物中分离出来，而 N-苯甲酰基苯丙氨酰-N-苯甲酰基苯丙氨酸（2）是从未从该科分离出来的化合物。化合物 1 是一种有效的 AChE 抑制剂，IC50 值与毒扁豆碱对照物（141.51 µM）相似。
