a College of Pharmacy, Chungnam National University , Daejeon , Korea.
b Immunoregulatory Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup-si , Jeonbuk , Korea.
J Enzyme Inhib Med Chem. 2019 Dec;34(1):753-760. doi: 10.1080/14756366.2019.1584621.
The aerial parts of Tetrastigma hemsleyanum (APTH) have been used as a functional tea in China. The purpose of the current study was to identify the bioactive constituents with inhibitory activity against soluble epoxide hydrolase (sEH) and inducible nitric oxide synthase (iNOS), which are jointly considered potential therapeutic targets for vascular system diseases. In the present study, 39 compounds (1-39) were isolated from the APTH. Among them, compounds 8, 10, 12, 16, 17, 19, and 32 displayed potential activities, with IC values ranging from 4.5 to 9.5 µM, respectively, and all in non-competitive inhibition mode. Compounds 5, 10, 12, 19, and 32 displayed potent iNOS inhibitory effects, with IC values ranging from 15.6 to 47.3 µM. The results obtained in this work contribute to a better understanding of the pharmacological activities of T. hemsleyanum and its potential application as a functional food.
五岭瓜馥木的地上部分在中国被用作一种功能性茶。本研究的目的是鉴定具有抑制可溶性环氧化物水解酶 (sEH) 和诱导型一氧化氮合酶 (iNOS) 活性的生物活性成分，sEH 和 iNOS 被共同认为是血管系统疾病的潜在治疗靶点。在本研究中，从五岭瓜馥木中分离得到 39 种化合物（1-39）。其中，化合物 8、10、12、16、17、19 和 32 表现出潜在的活性，IC 值范围为 4.5 到 9.5μM，均为非竞争性抑制模式。化合物 5、10、12、19 和 32 对 iNOS 表现出很强的抑制作用，IC 值范围为 15.6 到 47.3μM。本工作的结果有助于更好地理解瓜馥木的药理活性及其作为功能性食品的潜在应用。
