新型非锌结合型基质金属蛋白酶-2和基质金属蛋白酶-9抑制剂（I-3，II-3）-双金合欢素的合成与发现
Synthesis and discovery of (I-3,II-3)-biacacetin as a novel non-zinc binding inhibitor of MMP-2 and MMP-9.
作者信息
Nanjan Pandurangan, Nambiar Jyotsna, Nair Bipin G, Banerji Asoke
机构信息
Amrita School of Biotechnology, Amrita Vishwa Vidyapeetham, Amrita University, Kollam, Kerala 690525, India.
Amrita School of Biotechnology, Amrita Vishwa Vidyapeetham, Amrita University, Kollam, Kerala 690525, India.
出版信息
Bioorg Med Chem. 2015 Jul 1;23(13):3781-7. doi: 10.1016/j.bmc.2015.03.084. Epub 2015 Apr 9.
Eleven biflavones (7a-b and 9a-i) were synthesised by a simple and efficient protocol and screened for MMP-2 and MMP-9 inhibitory activities. Amongst them, a natural product-like analog, (I-3,II-3)-biacacetin (9h) was found to be the most potent inhibitor. Molecular docking studies suggest that unlike most of the known inhibitors, 9h inhibits MMP-2 and MMP-9 through non-zinc binding interactions.
通过一种简单有效的方法合成了11种双黄酮（7a - b和9a - i），并对其进行了基质金属蛋白酶-2（MMP - 2）和基质金属蛋白酶-9（MMP - 9）抑制活性的筛选。其中，一种类似天然产物的类似物，（I - 3，II - 3）-双金合欢素（9h）被发现是最有效的抑制剂。分子对接研究表明，与大多数已知抑制剂不同，9h通过非锌结合相互作用抑制MMP - 2和MMP - 9。
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