Bioactive triterpenoids from the leaves of Eriobotrya japonica as the natural PDE4 inhibitors
Bioactive triterpenoids from the leaves of Eriobotrya japonica as the natural PDE4 inhibitors
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枇杷叶中的生物活性三萜类化合物作为天然 PDE4 抑制剂
DOI：
10.1080/14786419.2017.1300796
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发表时间：
2017-01-01
影响因子：
2.2
通讯作者：
He, Xi-Xin
中科院分区：
文献类型：
--
作者：
Tan, Bing-Xin;Yang, Lu;He, Xi-Xin
摘要枇杷叶乙醇提取物对炎症性疾病的治疗靶点磷酸二酯酶- 4d （PDE4D）具有抑制活性。随后的生物测定引导分离分离了一个新的三萜(1)，以及七个已知的三萜：corcorsolate甲酯(2)、熊果酸(3)、齐墩果酸(4)、maslinate甲酯(5)、α-氨基(6)、3β、19α、23-三羟基脲-12-烯(7)和uvaol(8)。通过对化合物1的1D、2D NMR和HR-ESI-MS数据的分析，确定化合物1的结构为3β-羟基-21β-乙酰氧基-urs-12-en-28-羧酸盐。生物实验结果表明，化合物2、3和8对PDE4D2具有抑制作用，IC50值分别为3.06、2.18和5.17 μM，这可能为粳稻叶片抗炎活性提供了新的机制。
Abstract The ethanolic extract of the leaves of Eriobotrya japonica exhibited inhibitory activity against phosphodiesterase-4D (PDE4D), which is a therapeutic target of inflammatory disease. Subsequent bioassay-guided fractionation led to the isolation of a new triterpene (1), together with seven known triterpenoids, methyl corosolate (2), ursolic acid (3), oleanolic acid (4), methyl maslinate (5), α-amyin (6), 3β,19α,23-trihydroxy-urs-12-ene (7) and uvaol (8). The structure of compound 1 was established as 3β-hydroxyl-21β-acetoxyl-urs-12-en-28-carboxylate on the basis of interpretation of its 1D and 2D NMR and HR-ESI-MS spectroscopic data. The bioassay results verified compounds 2, 3 and 8 inhibited PDE4D2 effectively with the IC50 values of 3.06, 2.18 and 5.17 μM, respectively, which may provide a novel mechanism for the anti-inflammatory activity of the leaves of E. japonica.