Secolignans with Antiangiogenic Activities from Peperomia dindygulensis
Secolignans with Antiangiogenic Activities from Peperomia dindygulensis
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来自 Peperomia dindygulensis 的具有抗血管生成活性的 Secolignans
DOI：
10.1002/cbdv.201000123
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发表时间：
2011-05-01
影响因子：
2.9
通讯作者：
Yang, Guo-Hong
中科院分区：
文献类型：
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作者：
Lin, Meng-Gan;Yu, De-Hong;Yang, Guo-Hong
从大花菜全株中分离得到2个新的木脂素类化合物，分别为花木脂素G和H(1和2)，以及5个已知的木脂素类化合物：花木脂素A(3)，花木脂素E(4)，花木脂素B(5)，2，3-trans-2-methyl-3-{(3-hydroxy-4，5-dimethoxyphenyl)[5-methoxy-3，4-(methylenedioxy)苯基]甲基}丁内酯(6)，2，3-cis-2-(hydroxymethyl)-3-{bis[5-methoxy-3，4-(methylenedioxy)苯基]甲基}丁内酯(7)。它们的结构和构型通过包括2D-核磁共振技术在内的波谱方法来确定。通过人脐静脉内皮细胞(HUVEC)增殖和成管实验评价所有化合物的抗血管生成作用，其中化合物4和5在生物测定中具有活性。化合物4和5对人脐静脉内皮细胞有明显的细胞毒作用，其IC(50)分别为1.64+/-0.19和8.44+/-0.4微米。化合物4和5也表现出明显的抑制HUVEC管形成的活性，其IC(50)值分别为3.13+/-0.09和6.24+/-0.12微米。
Two new secolignans, peperomins G and H (1 and 2, resp.), were isolated from the whole plant of Peperomia dindygulensis, together with five known secolignans, peperomin A (3), peperomin E (4), peperomin B (5), 2,3-trans-2-methyl-3-{(3-hydroxy-4,5-dimethoxyphenyl)[5-methoxy-3,4-(methylenedioxy) phenyl]methyl}butyrolactone (6), 2,3-cis-2-(hydroxymethyl)-3-{bis[5-methoxy-3,4-(methylenedioxy) phenyl]methyl}butyrolactone (7). Their structures and configurations were elucidated by spectroscopic methods including 2D-NMR techniques. Antiangiogenic effects of all compounds were evaluated using human umbilical vein endothelial cells (HUVEC) proliferation and tube-formation tests, with compounds 4 and 5 being active in the bioassay. Compounds 4 and 5 induced obvious cell toxicity to HUVEC with IC(50) values of 1.64 +/- 0.19 and 8.44 +/- 0.4 mu m, respectively. Compounds 4 and 5 also exhibited significant HUVEC tube formation-inhibiting activity with IC(50) values of 3.13 +/- 0.09 and 6.24 +/- 0.12 mu m, respectively.