Kim Jang Hoon, Morgan Abubaker M A, Tai Bui Huu, Van Doan Thi, Cuong Nguyen Manh, Kim Young Ho
a College of Pharmacy, Chungnam National University , Daejeon , Republic of Korea .
b Virology Unit, Department of Horticultural Environment , National Institute of Horticultural and Herbal Science, RDA , Jeollabuk-Do , Republic of Korea .
J Enzyme Inhib Med Chem. 2016 Aug;31(4):640-4. doi: 10.3109/14756366.2015.1057719. Epub 2015 Oct 7.
The aim of this study is to search for soluble epoxide hydrolase (sEH) inhibitors from natural plants, bioassay-guided fractionation of lipophilic n-hexane and chloroform layers of an extract of the aerial parts of Glycosmis stenocarpa led to the isolation of 12 compounds (1-12) including murrayafoline-A (1), isomahanine (2), bisisomahanine (3), saropeptate (4), (24 S)-ergost-4-en-3,6-dione (5), stigmasta-4-en-3,6-dion (6), stigmast-4-en-3-one (7), β-sitosterol (8), 24-methylpollinastanol (9), trans-phytol (10), neosarmentol III (11) and (+)-epiloliolide (12). Their structures were elucidated on the basis of spectroscopic data. Among them, neosarmentol III (11) was isolated from nature for the first time. All the isolated compounds were evaluated for their inhibitory activity against sEH. Among isolated carbazole-type compounds, isomahanine (2) and bisisomahanine (3) were identified as a potent inhibitor of sEH, with IC50 values of 22.5 ± 1.7 and 7.7 ± 1.2 µM, respectively. Moreover, the inhibitory action of 2 and 3 represented mixed-type enzyme inhibition.
本研究旨在从天然植物中寻找可溶性环氧化物水解酶(sEH)抑制剂,通过生物活性导向的方法对狭果山小橘地上部分提取物的亲脂性正己烷层和氯仿层进行分离,得到了12种化合物(1 - 12),包括默里叶碱 - A(1)、异马汉宁(2)、双异马汉宁(3)、蛇根肽(4)、(24 S)-麦角甾 - 4 - 烯 - 3,6 - 二酮(5)、豆甾 - 4 - 烯 - 3,6 - 二酮(6)、豆甾 - 4 - 烯 - 3 - 酮(7)、β - 谷甾醇(8)、24 - 甲基花粉甾醇(9)、反式叶绿醇(10)、新萨门托醇III(11)和(+)-表罗勒内酯(12)。根据光谱数据阐明了它们的结构。其中,新萨门托醇III(11)是首次从自然界中分离得到。对所有分离得到的化合物进行了sEH抑制活性评估。在分离得到的咔唑类化合物中,异马汉宁(2)和双异马汉宁(3)被鉴定为sEH的有效抑制剂,IC50值分别为22.5 ± 1.7和7.7 ± 1.2 µM。此外,2和3的抑制作用表现为混合型酶抑制。