Extracellular signal-regulated kinases (ERK) inhibitors from Aristolochia yunnanensis.
Extracellular signal-regulated kinases (ERK) inhibitors from Aristolochia yunnanensis.
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DOI：
10.1021/np300887d
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发表时间：
2013-04
影响因子：
5.1
通讯作者：
Zhong-bin Cheng;Weiyan Shao;Yena Liu;Qiong Liao;Ting-ting Lin;Xiao-yan Shen;Sheng Yin
中科院分区：
文献类型：
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作者：
Zhong-bin Cheng;Weiyan Shao;Yena Liu;Qiong Liao;Ting-ting Lin;Xiao-yan Shen;Sheng Yin
从云南马兜铃的茎中分离出六种新的倍半萜类化合物，马兜铃酸 A-F (1-6)、分离产物 [7-O-乙基马多林 W (7)] 和 12 种已知类似物。通过化学和光谱相结合的方法确定了结构，并通过改进的Mosher方法和CD分析确定了化合物2、3、5-7、9、14和17的绝对构型。使用生物测定系统筛选化合物 1-19，该系统旨在评估对丝裂原激活蛋白激酶 (MAPK) 信号通路的影响。在三种 MAPK（ERK1/2、JNK 和 p38）中，化合物 1、4、10-13、16、18 和 19 表现出对 ERK1/2 磷酸化的选择性抑制。化合物 16 和 19 比阳性对照 PD98059（一种已知的 ERK1/2 信号通路抑制剂）活性更高。
Six new sesquiterpenoids, aristoyunnolins A-F (1-6), an artifact of isolation [7-O-ethyl madolin W (7)], and 12 known analogues were isolated from stems of Aristolochia yunnanensis. The structures were determined by combined chemical and spectral methods, and the absolute configurations of compounds 2, 3, 5-7, 9, 14, and 17 were determined by the modified Mosher's method and CD analysis. Compounds 1-19 were screened using a bioassay system designed to evaluate the effect on mitogen-activated protein kinases (MAPKs) signaling pathways. Among three MAPKs (ERK1/2, JNK, and p38), compounds 1, 4, 10-13, 16, 18, and 19 exhibited selective inhibition of the phosphorylation of ERK1/2. Compounds 16 and 19 were more active than the positive control PD98059, a known inhibitor of the ERK1/2 signaling pathway.