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Evaluation of antihypertensive polyphenols of barley (Hordeum vulgare L.) seedlings via their effects on angiotensin-converting enzyme (ACE) inhibition
Applied Biological Chemistry ( IF 2.3 ) Pub Date : 2020-07-14 , DOI: 10.1186/s13765-020-00519-9
Ji-Eun Ra , So-Yeun Woo , Hui Jin , Mi Ja Lee , Hyun Young Kim , Hyeonmi Ham , Ill-Min Chung , Woo Duck Seo

Angiotensin-converting enzyme (ACE) is an important therapeutic target in the regulation of high blood pressure. This study was conducted to investigate the alterations in blood pressure associated with ACE inhibition activity of the polyphenols (1–10), including 3-O-feruloylquinic acid (1), lutonarin (2), saponarin (3), isoorientin (4), orientin (5), isovitexin (6), isoorientin-7-O-[6-sinapoyl]-glucoside (7), isoorientin-7-O-[6-feruloyl]-glucoside (8), isovitexin-7-O-[6-sinapoyl]-glucoside (9), and isovitexin-7-O-[6-feruloyl]-glucoside (10), isolated from barley seedlings (BS). All the isolated polyphenols exhibited comparable IC50 values of ACE inhibition activity (7.3–43.8 µM) with quercetin (25.2 ± 0.2 µM) as a positive control, and their inhibition kinetic models were identified as noncompetitive inhibition. Especially, compound 4 was revealed to be an outstanding ACE inhibitor (IC50 = 7.3 ± 0.1 µM, Ki = 6.6 ± 0.1 µM). Based on the compound structure–activity relationships, the free hydroxyl groups of flavone-moieties and glucose connections at the A ring of the flavone moieties were important factors for inhibition of ACE. The alcohol extract of BS also demonstrated potent ACE inhibition activity (66.5% ± 2.2% at 5000 µg mL−1). The polyphenols from BS had strong inhibitory activity on ACE and this study results suggest that BS can be used as an effective blood pressure regulator through ACE inhibition.

中文翻译:

大麦的降压多酚的评价(大麦通过它们对血管紧张素转化酶(ACE)抑制效果L.)幼苗

血管紧张素转换酶(ACE)是调节高血压的重要治疗靶标。进行这项研究的目的是研究血压的变化与多酚(1-10)的ACE抑制活性有关,其中包括3-O-阿魏酰奎尼酸(1),卢托那林(2),皂苷(3),异Orientientin(4) ,Orientin(5),Isovititexin(6),isoorientin-7-O- [6-sinapoyl]-葡萄糖苷(7),Isoorientin-7-O- [6-feruloyl]-葡萄糖苷(8),Isovititexin-7-O从大麦幼苗(BS)中分离的-[[6-芥子基]-葡糖苷(9)和异石蛋白-7-O- [6-阿魏酰基]-葡糖苷(10)。以槲皮素(25.2±0.2 µM)作为阳性对照,所有分离出的多酚均显示出与ACE抑制活性相当的IC50值(7.3–43.8 µM),其抑制动力学模型被确定为非竞争性抑制。特别,化合物4被证明是出色的ACE抑制剂(IC50 = 7.3±0.1 µM,Ki = 6.6±0.1 µM)。基于化合物的结构-活性关系,黄酮部分的游离羟基和黄酮部分A环的葡萄糖连接是抑制ACE的重要因素。BS的醇提取物还显示出有效的ACE抑制活性(5000 µg mL-1时为66.5%±2.2%)。BS中的多酚对ACE具有很强的抑制活性,这项研究结果表明BS可通过ACE抑制作为有效的血压调节剂。黄酮部分的游离羟基和黄酮部分A环的葡萄糖连接是抑制ACE的重要因素。BS的醇提取物还显示出有效的ACE抑制活性(5000 µg mL-1时为66.5%±2.2%)。BS中的多酚对ACE具有很强的抑制活性,这项研究结果表明BS可通过ACE抑制作为有效的血压调节剂。黄酮部分的游离羟基和黄酮部分A环的葡萄糖连接是抑制ACE的重要因素。BS的醇提取物还显示出有效的ACE抑制活性(5000 µg mL-1时为66.5%±2.2%)。BS中的多酚对ACE具有很强的抑制活性,这项研究结果表明BS可通过ACE抑制作为有效的血压调节剂。
更新日期:2020-07-14
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