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Plant Diversity ›› 2008, Vol. 30 ›› Issue (05): 621-623.DOI: 10.3724 SP.J.1143.2008.07305

• 研究论文 • 上一篇    下一篇

组织蛋白酶B 的新型天然抑制剂

贾锐锐, 曾广智, 谭宁华, 周志宏, 张颖君   

  1. 中国科学院昆明植物研究所植物化学与西部植物资源持续利用国家重点实验室, 云南昆明 650204
  • 收稿日期:2007-12-20 出版日期:2008-10-25 发布日期:2008-10-25
  • 通讯作者: 谭宁华

New Natural Inhibitors of Human Cathepsin B

JIA Rui-Rui, ZENG Guang-Zhi, TAN Ning-Hua, ZHOU Zhi-Hong, ZHANG Ying-Jun   

  1. State Key Laboratory of Phytochemistry and Plant Resources in West China , Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204, China
  • Received:2007-12-20 Online:2008-10-25 Published:2008-10-25
  • Contact: TAN Ning-Hua

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摘要： 组织蛋白酶B 是木瓜蛋白酶类半胱氨酸蛋白酶家族的重要成员, 它与人类多种疾病相关, 尤其是在恶性肿瘤的侵袭转移过程中扮演了重要角色。通过随机筛选, 发现了五个对组织蛋白酶B 具有较好抑制活性的天然化合物prodelphinidin B-2 3′-O-gallate (1), prodelphinidin B-2 (2) , procyanidin B-2 (3) , puerin A (4) 和(-) epigallocatechin-3-O-gallate (5) , 其IC50 值分别为0. 58 , 0 .44 , 0 .76 , 2 .07 和0 . 96μmol/L。这五个抑制剂为
黄烷醇类化合物, 均为组织蛋白酶B 的新型天然抑制剂。

关键词: 组织蛋白酶B, 天然抑制剂, 黄烷醇

Abstract: Cathepsin B is an important member of the papain-like cysteine proteases . It has been implicated in the pathology of many human diseases, especially in the invading and metastasis of most malignant tumors. With random screening, five natural compounds, prodelphinidin B-2 3′-O-gallate (1 ) , prodelphinidin B-2 ( 2), procyanidin B-2 ( 3), puerin A (4) and (- ) epigallocatechin-3-O-gallate ( 5 ) , were found to show potent cathepsin B inhibitory activity with IC50 s of 0.58, 0.44, 0.76, 2.07 and 0.96μmol/L, respectively. Inhibitors 1 - 5 are found with chemotype of flavanols, which are
new natural inhibitors of cathepsin B.

Key words: Cathepsin B

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