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米氏补血草的植物化学特征及血管紧张素I转换酶(ACE)抑制活性

Phytochemical profile and angiotensin I converting enzyme (ACE) inhibitory activity of Limonium michelsonii Lincz.

作者信息

Jenis Janar, Kim Jeong Yoon, Uddin Zia, Song Yeong Hun, Lee Hyeong-Hwan, Park Ki Hun

机构信息

Division of Applied Life Science (BK21 Plus), IALS, Gyeongsang National University, Jinju, 52828, Republic of Korea.

Faculty of Chemistry and Chemical Technology, Al-Farabi Kazakh National University, Almaty, Republic of Kazakhstan.

出版信息

J Nat Med. 2017 Oct;71(4):650-658. doi: 10.1007/s11418-017-1095-4. Epub 2017 May 26.

Abstract

Members of the genus Limonium are widely used as medicinal herbs due to their health-promoting effects, such as an ability to improve blood circulation by inhibiting angiotensin I converting enzyme (ACE). While the potential of L. michelsonii Lincz. (a medicinal plant endemic to Kazakhstan) to inhibit ACE has been demonstrated, the inhibitory activities of its secondary metabolites have not been explored. In this work, the principal phenolic compounds (1-20) among these metabolites were isolated to determine the components responsible for ACE inhibition. The natural abundances of the active constituents within the target plant were characterized by UPLC-Q-TOF/MS analysis. All of the isolated compounds except for gallates 10-12 were found to significantly inhibit ACE, with IC values of between 7.1 and 138.4 μM. Unexpectedly, the flavonol glycosides 16-20 were observed to be more potent than the corresponding aglycones 4 and 5. For example, quercetin (4) had IC = 30.3 μM, whereas its glycosides (16, 17) had IC = 10.2 and 14.5 μM, respectively. A similar trend was observed for myricetin (5) and its glycosides (18-20). In a kinetic study, the flavonols 3-5 and 16-20 and the dihydroflavonols 8 and 9 behaved as competitive inhibitors, whereas other flavones (1, 2, 13-15) and flavanones (6, 7) performed noncompetitive inhibition.

摘要

补血草属植物因其促进健康的功效而被广泛用作草药,例如具有通过抑制血管紧张素I转换酶(ACE)来改善血液循环的能力。虽然已证实哈萨克斯坦特有的药用植物米氏补血草(Limonium michelsonii Lincz.)具有抑制ACE的潜力,但其次生代谢产物的抑制活性尚未得到研究。在这项研究中,分离出了这些代谢产物中的主要酚类化合物(1-20),以确定负责抑制ACE的成分。通过超高效液相色谱-四极杆飞行时间质谱(UPLC-Q-TOF/MS)分析对目标植物中活性成分的天然丰度进行了表征。发现除没食子酸盐10-12外,所有分离出的化合物均能显著抑制ACE,IC值在7.1至138.4 μM之间。出乎意料的是,观察到黄酮醇苷16-20比相应的苷元4和5更具活性。例如,槲皮素(4)的IC = 30.3 μM,而其糖苷(16, 17)的IC分别为10.2和14.5 μM。杨梅素(5)及其糖苷(18-20)也观察到类似趋势。在动力学研究中,黄酮醇3-5和16-20以及二氢黄酮醇8和9表现为竞争性抑制剂,而其他黄酮(1, 2, 13-15)和黄烷酮(6, 7)表现为非竞争性抑制。

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