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KMID : 0043320120350101763
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Archives of Pharmacal Research
2012 Volume.35 No. 10 p.1763 ~ p.1770
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Inhibition of LFA-1/ICAM-1-mediated cell adhesion by stilbene derivatives from Rheum undulatum
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Lee Seung-Woong
Hwang Byung-Soon
Kim Mi-Hwa
Park Chan-Sun
Lee Woo-Song
Oh Hyun-Mee
Rho Mun-Chual
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Abstract
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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 (1H-, 13C-NMR and MS), to be desoxyrhapontigenin (1), rhapontigenin (2), trans-resveratrol (3), piceatannol (4), piceatannol-3′-O-β-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 μM, 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 μM). 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.
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KEYWORD
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Rheum undulatum, Stilbenes, Anti-inflammatory agents, Lymphocyte function-associated antigen-1 (LFA-1), Intercellular adhesion molecule-1 (ICAM-1), Cell adhesion molecules
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