Han Yoo Kyong, Lee Ji Sun, Yang Seo Young, Lee Ki Yong, Kim Young Ho
College of Pharmacy, Korea University, Sejong 30019, Korea.
College of Pharmacy, Chungnam National University, Daejeon 34134, Korea.
Plants (Basel). 2021 Feb 13;10(2):356. doi: 10.3390/plants10020356.
Soluble epoxide hydrolase (sEH) is an enzyme that is considered a potential therapeutic target in human cardiovascular disease. Triterpenes (-) and phenylpropanoids (-) were isolated from to obtain sEH inhibitors through various chromatographic purificationtechniques. The isolated compounds were evaluated for their inhibitory activity against sEH, and methyl rosmarinate (), martynoside (), dimethyl lithospermate () and 9″ methyl lithospermate () showed remarkable inhibitory activity, with the IC values ranging from 10.6 ± 3.2 to 35.7 ± 2.1 µM. Kinetic analysis of these compounds revealed that , and were competitive inhibitors bound to the active site, and was the preferred mixed type inhibitor for allosteric sites. Additionally, molecular modeling has identified interacting catalytic residues and bindings between sEH and inhibitors. The results suggest that these compounds are potential candidates that can be used for further development in the prevention and treatment for cardiovascular risk.
可溶性环氧化物水解酶（sEH）是一种被认为在人类心血管疾病中具有潜在治疗靶点的酶。从[具体来源未提及]中分离出三萜类化合物（-）和苯丙素类化合物（-），通过各种色谱纯化技术获得sEH抑制剂。对分离出的化合物进行sEH抑制活性评估，迷迭香酸甲酯（）、紫葳苷（）、二甲基紫草素（）和9''-甲基紫草素（）表现出显著的抑制活性，IC值范围为10.6±3.2至35.7±2.1μM。对这些化合物的动力学分析表明，[此处原文有缺失信息]、[此处原文有缺失信息]和[此处原文有缺失信息]是结合到活性位点的竞争性抑制剂，而[此处原文有缺失信息]是变构位点的首选混合型抑制剂。此外，分子建模确定了sEH与抑制剂之间相互作用的催化残基和结合方式。结果表明，这些化合物是可用于心血管疾病预防和治疗进一步开发的潜在候选物。
