香豆素类化合物的血管紧张素转换酶抑制活性研究
Angiotensin-I-Converting Enzyme Inhibitory Activity of Coumarins from .
机构信息
Department of Food and Life Science, Pukyong National University, Busan 48513, Korea.
Department of Chemistry and Biochemistry, Concordia University, Montreal, QC H4B 1R6, Canada.
出版信息
Molecules. 2019 Oct 31;24(21):3937. doi: 10.3390/molecules24213937.
The bioactivity of ten traditional Korean species were screened by angiotensin-converting enzyme (ACE) assay in vitro. Among the crude extracts, the methanol extract of whole plants exhibited potent inhibitory effects against ACE. In addition, the ACE inhibitory activity of coumarins -, - was evaluated, along with two phenolic acids (, ) obtained from . . Among profound coumarins, - were determined to manifest marked inhibitory activity against ACE with IC values of 4.68-20.04 µM. Compounds , , and displayed competitive inhibition against ACE. Molecular docking studies confirmed that coumarins inhibited ACE via many hydrogen bond and hydrophobic interactions with catalytic residues and zinc ion of C- and N-domain ACE that blocked the catalytic activity of ACE. The results derived from these computational and in vitro experiments give additional scientific support to the anecdotal use of in traditional medicine to treat cardiovascular diseases such as hypertension.
十种传统韩国植物的生物活性通过体外血管紧张素转化酶（ACE）测定法进行了筛选。在粗提物中，全植物甲醇提取物对 ACE 表现出很强的抑制作用。此外，还评估了香豆素 - 和 - 的 ACE 抑制活性，以及从 中得到的两种酚酸（、）。在深刻的香豆素中，- 被证明对 ACE 表现出显著的抑制活性，IC 值为 4.68-20.04 µM。化合物 - 、- 和 - 对 ACE 表现出竞争性抑制作用。分子对接研究证实，香豆素通过与 ACE 的 C-和 N-域的催化残基和锌离子的许多氢键和疏水相互作用抑制 ACE，从而阻断 ACE 的催化活性。这些计算和体外实验的结果为传统医学中使用 治疗心血管疾病（如高血压）的轶事提供了额外的科学支持。
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