Phenolic compounds isolated from Zingiber officinale roots inhibit cell adhesion

Inhibitors of cell adhesion molecule-mediated cell adhesion might be novel therapeutic agents for the treatment of various inflammatory diseases. In this study, nine phenolic compounds were isolated from the methanol extracts of Zingiber officinale roots by bioactivity-guided fractionation. The structures of the compounds were determined by spectroscopic analysis (1H, 13C NMR and MS), to be 6-gingerol (1), 8-gingerol (2), 10-gingerol (3), 6-shogaol (4), 8-shogaol (5), 10-shogaol (6), dehydro-6-gingerdione (7), dehydro-10-gingerdione (8) and 6-paradol (9). Compounds 3, 4, 5 and 7 inhibited direct binding between sICAM-1 and LFA-1 of the THP-1 cells in a dose-dependent manner with IC50 values of 57.6, 27.1, 65.4 and 62.0 μM, respectively. Compounds 4 and 7 had an inhibitory effect on direct binding between sVCAM-1 and VLA-4 of THP-1 cells. These results suggest that the phenolic compounds from Z. officinale roots are good candidates for therapeutic strategies aimed at inflammation.

► The MeOH extract of Zingiber officinale roots inhibited the binding between sICAM-1 and THP-1 cells.
► Nine phenolic compounds were isolated from MeOH extract of the Zingiber officinale roots.
► Compound 4 showed the most potent inhibitory activity on binding assay between sICAM-1 and THP-1 cells.
► Also, 4 inhibited the direct binding between sVCAM-1 and THP-1 cells.
► These results can be used to design new cell adhesion inhibitors leading to anti-inflammatory agents.