植物源酚类化合物作为胰蛋白酶抑制剂的研究。
An investigation of phenolic compounds from plant sources as trypsin inhibitors.
机构信息
Center for Natural Product Drug Development, Department of Chemistry, Government College University, Lahore, Pakistan.
出版信息
Nat Prod Res. 2012;26(12):1087-93. doi: 10.1080/14786419.2011.559637. Epub 2011 Oct 20.
In the search of new trypsin inhibitors caffeic acid (1), cinnamic acid (2), gallic acid (3) and eugenol (4) from Cinnamomum zeylanicum, ferulic acid (5) from Impatiens bicolor, vanillin (6) from Melia azedarach and catechol (7) from Allium cepa were isolated through bioassay guided fractionation of the plant extracts. IC (50) values of the compounds 1, 2 and 5 were found to be 0.35 ± 0.02 mM, 0.96 ± 0.05 mM and 1.22 ± 0.06 mM, respectively. Lineweaver-Burk and Dixon plots and their secondary replots showed that 1 was non-competitive inhibitor of this enzyme with K(i) value 0.102 ± 0.006 mM.
从肉桂（Cinnamomum zeylanicum）中分离得到了咖啡酸（1）、肉桂酸（2）、没食子酸（3）和丁香酚（4），从双色金鸡菊（Impatiens bicolor）中分离得到了阿魏酸（5），从楝树（Melia azedarach）中分离得到了香草醛（6），从洋葱（Allium cepa）中分离得到了儿茶酚（7），采用生物活性导向的分步提取法从这些植物提取物中分离得到了上述化合物。 发现化合物 1、2 和 5 的 IC50 值分别为 0.35 ± 0.02 mM、0.96 ± 0.05 mM 和 1.22 ± 0.06 mM。Lineweaver-Burk 和 Dixon 图及其二次重绘图表明，1 是该酶的非竞争性抑制剂，其 K(i) 值为 0.102 ± 0.006 mM。
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