Brachyantheraoside A(8), a new natural nor-oleanane triterpenoid as a kidney-type glutaminase inhibitor from Stauntonia brachyanthera
Brachyantheraoside A(8), a new natural nor-oleanane triterpenoid as a kidney-type glutaminase inhibitor from Stauntonia brachyanthera
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Brachyantheraoside A(8)，一种来自野木瓜的新型天然正齐墩果烷三萜类化合物，作为肾型谷氨酰胺酶抑制剂
DOI：
10.1039/c7ra11270j
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发表时间：
2017
期刊：
影响因子：
3.9
通讯作者：
Meng Dali
中科院分区：
文献类型：
--
作者：
Li Rong;Wei Peifeng;Wang Yue;Liu Ying;Liu Xuanli;Meng Dali
为寻找具有潜在抗癌活性的肾型谷胱甘肽转移酶（KGA）抑制剂，从短花野木瓜（Stauntonia brachyanthera）中筛选出18个去甲齐墩果烷型三萜类化合物，其中包括2个新化合物。基于结构的虚拟配体筛选鉴定了8个化合物，这些化合物可能更有机会成为低结合能的KGA抑制剂。谷氨酰胺酶抑制实验和一系列细胞水平的测定，包括细胞毒性、伤口愈合、transwell侵袭、western blot和细胞凋亡，进一步证实了5（短蕊菊苷A8）的抑制作用。这为5成为抑制剂提供了可能。
With the aim of finding a better kidney-type glutaminase (KGA) inhibitor with potential anti-cancer properties, 18 nor-oleanane triterpenoids from Stauntonia brachyanthera, including 2 new ones, were screened against KGA. The structure-based virtual ligand screening identified 8 compounds, which might have more chance to become inhibitors of KGA with low binding energy. Glutaminase inhibition experiments and a series of cellular level assays, including cytotoxicity, wound healing, transwell invasion, western blot, and cell apoptosis, further confirmed the inhibitory effect of 5 (brachyantheraoside A8). These provided the possibility for 5 to become an inhibitor.