CAJ | 학술논문

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.
조직단백매B시목과단백매류반광안산단백매가족적중요성원,타여인류다충질병상관,우기시재악성종류적침습전이과정중분연료중요각색.통과수궤사선,발현료오개대조직단백매B구유교호억제활성적천연화합물prodelphinidin B-23'-O-gallate(1),prodelphinidin B-2(2),ImJcyarddin B-2(3),puexin A(4)화(-)epigallocatechin-3-O-gallate(5),기IC50치분별위0.58,0.44,0.76,2.07화0.96umol/L.저오개억제제위황완순류화합물,균위조직단백매B적신형천연억제제.
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.