| 组织蛋白酶B的新型天然抑制剂 |
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| 引用本文： | 贾锐锐,曾广智,谭宁华,周志宏,张颖君.组织蛋白酶B的新型天然抑制剂[J].云南植物研究,2008,30(5). |
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| 作者姓名： | 贾锐锐 曾广智 谭宁华 周志宏 张颖君 |
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| 作者单位： | 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 |
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| 基金项目： | 国家自然科学基金，中国科学院"西部之光"人才培养计划 |
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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-23'-O-gallate(1),prodelphinidin B-2(2),ImJcyarddin B-2(3),puexin A(4)和(-)epigallocatechin-3-O-gallate(5),其IC50值分别为0.58,0.44,0.76,2.07和0.96umol/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.
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| 关 键 词： | 组织蛋白酶B 天然抑制剂 黄烷醇 |
New Natural Inhibitors of Human Cathepsin B |
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| JIA Rui-Rui,ZENG Guang-Zhi,TAN Ning-Hua,ZHOU Zhi-Hong,ZHANG Ying-Jun.New Natural Inhibitors of Human Cathepsin B[J].Acta Botanica Yunnanica,2008,30(5). |
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| Authors: | JIA Rui-Rui ZENG Guang-Zhi TAN Ning-Hua ZHOU Zhi-Hong ZHANG Ying-Jun |
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| Abstract: | Cathepsin B is an important member of the papain-like cysteine proteases. It has been implicated in the patholo-gy of many human diseaes, 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 shouw potent cathepsin B inhibitory activity with IC50s of 0.58,0.44,0.76,2.07and 0.96μmol/L, respectively. Inhibitors1-5 are found with chemotype of flavanols, which are new natural inhibitors of cathepsin B. |
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| Keywords: | Cathepsin B Natural inhibitors Flavaols |
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