Liu Dan, Wang Dandan, Yang Wei, Meng Dali
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University), Ministry of Education, School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China.
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University), Ministry of Education, School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China.
Bioorg Med Chem. 2017 Jul 1;25(13):3562-3566. doi: 10.1016/j.bmc.2017.05.010. Epub 2017 May 6.
With the aim of finding a better xanthine oxidase inhibitor with potential anti-gout properties, the studies on the fruit of Stauntonia brachyanthera were carried out, which led to the isolation of 12 glycosides, including 4 new nor-oleanane triterpenoids. Their structures were determined by comprehensive spectroscopic (NMR and HR MS) analysis. Two compounds (4 and 11) exhibited significant inhibitory activities on xanthine oxidase with IC values of 5.22 and 1.60µM, respectively. Another five compounds (1, 2, 3, 8 and 10) showed qualified activities. The results suggested that the existences of nor-oleanane triterpenoids and flavonoids in the fruits were responsible for the inhibitory activity on xanthine oxidase that could cut off the production of uric acid. Nor-oleanane triterpenoids, a new leading XO inhibitor, is worthy of further studies on molecular biology level for its mechanisms.
为了寻找一种具有潜在抗痛风特性的更好的黄嘌呤氧化酶抑制剂，对短药野木瓜果实进行了研究，从中分离出12种糖苷，包括4种新的降齐墩果烷三萜类化合物。通过综合光谱（核磁共振和高分辨质谱）分析确定了它们的结构。两种化合物（4和11）对黄嘌呤氧化酶表现出显著的抑制活性，IC值分别为5.22和1.60μM。另外五种化合物（1、2、3、8和10）表现出一定活性。结果表明，果实中降齐墩果烷三萜类化合物和黄酮类化合物的存在是其对黄嘌呤氧化酶具有抑制活性的原因，该活性可切断尿酸的产生。降齐墩果烷三萜类化合物作为一种新的主要黄嘌呤氧化酶抑制剂，因其作用机制值得在分子生物学水平上进一步研究。
