Inhibition of LFA-1/ICAM-1-mediated cell adhesion by stilbene derivatives from Rheum undulatum
Inhibition of LFA-1/ICAM-1-mediated cell adhesion by stilbene derivatives from Rheum undulatum
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DOI：
10.1007/s12272-012-1008-8
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发表时间：
2012-10-01
影响因子：
6.7
通讯作者：
Rho, Mun-Chual
中科院分区：
文献类型：
--
作者：
Lee, Seung Woong;Hwang, Byung Soon;Rho, Mun-Chual
采用生物活性导向分级法从波叶大黄根茎甲醇提取物中分离得到6个二苯乙烯类化合物。化合物的结构经波谱分析（H-1-，C-13-NMR和MS）确定为脱氧漏芦皂苷元（1），漏芦皂苷元（2），反式白藜芦醇（3），白藜芦醇（4），白藜芦醇-3 '-O-β-D-吡喃葡萄糖苷（5）和异漏芦皂苷（6）。化合物1-4以剂量依赖性方式抑制THP-1细胞的sICAM-1和LFA-1之间的直接结合，IC 50值分别为50.1、25.4、33.4和45.9 μ M。另一方面，在每个分子中具有葡萄糖部分的其它化合物5和6在细胞粘附测定中没有显示任何抑制活性（IC 50值> 100.0 μ M）。化合物2、3和4也对THP-1细胞的sVCAM-1和VLA-4之间的直接结合具有抑制作用。这表明来自波叶大黄根茎的芪类化合物是针对炎症的治疗策略的良好候选物。
Six stilbenes were isolated from the methanol extract of Rheum undulatum rhizomes by bioactivity-guided fractionation. The structures of the compounds were determined by spectroscopic analysis (H-1-, C-13-NMR and MS), to be desoxyrhapontigenin (1), rhapontigenin (2), trans-resveratrol (3), piceatannol (4), piceatannol-3'-O-beta-D-glucopyranoside (5) and isorhapontin (6). Compounds 1-4 inhibited the direct binding between sICAM-1 and LFA-1 of the THP-1 cells in a dose-dependent manner with IC50 values of 50.1, 25.4, 33.4 and 45.9 mu M, respectively. On the other hand, the other compounds 5 and 6 with a glucose moiety in each molecule did not show any inhibitory activity in the cell adhesion assay (IC50 values of > 100.0 mu M). Compounds 2, 3 and 4 also had an inhibitory effect on direct binding between sVCAM-1 and VLA-4 of THP-1 cells. This suggests that the stilbenes from Rheum undulatum rhizomes are good candidates for therapeutic strategies towards inflammation.