College of Pharmacy, Seoul National University, Seoul, Korea.
Arch Pharm Res. 2011 Feb;34(2):217-22. doi: 10.1007/s12272-011-0206-0. Epub 2011 Mar 6.
A series of flavonoids (1-14) was isolated from the roots of Sophora flavescens. We evaluated their ability to inhibit both microbial growth and sortase A, an enzyme that plays a key role in cell wall protein anchoring and virulence in Staphylococcus aureus. Most prenylated flavonoids (7-13) displayed potent inhibitory activity against gram-positive and gram-negative bacteria except E. coli, with minimum inhibitory concentrations values ranging from 4.40 to 27.7 μM, and weak or no activity against fungal strains tested. Kurarinol (6) was a potent inhibitor of sortase A, with an IC(50) value of 107.7 ± 6.6 μM. A preliminary structure-activity relationship, including essential structural requirements, is described.
从苦参的根部分离得到一系列黄酮类化合物（1-14）。我们评估了它们抑制微生物生长和 Sortase A 的能力，Sortase A 是一种在金黄色葡萄球菌细胞壁蛋白锚定和毒力中起关键作用的酶。大多数prenylated 黄酮类化合物（7-13）对革兰氏阳性和革兰氏阴性细菌均显示出强大的抑制活性，除大肠杆菌外，最小抑菌浓度值范围从 4.40 到 27.7 μM，对测试的真菌菌株几乎没有活性或没有活性。苦参醇（6）是 Sortase A 的有效抑制剂，IC50 值为 107.7 ± 6.6 μM。描述了初步的结构-活性关系，包括必要的结构要求。
