Kujigamberol is the norlabdane compound isolated from Kuji amber and has recently been shown to prevent Ca2+-signal transduction and exert anti-allergy effects in vitro and in vivo. However, the anti-inflammatory activities of kujigamberol remain unclear. In the present study, we investigated the biological activities of kujigamberol on cell adhesion molecules expressed on human umbilical vein endothelial cells (HUVEC) in response to pro-inflammatory cytokines. Kujigamberol decreased the molecular weight of intercellular adhesion molecule-1 (ICAM-1) by altering N-glycan modifications. In contrast to ICAM-1, kujigamberol reduced the interleukin-1α- or tumor necrosis factor α-induced expression of vascular cell adhesion molecule-1 (VCAM-1) and E-selectin at the mRNA and protein levels. Kujigamberol B, but not kujiol A, decreased the molecular weight of the ICAM-1 protein. Kujigamberol moderately inhibited yeast α-glucosidases, whereas it was only weakly inhibited by kujigamberol B and more weakly by kujiol A. Three compounds did not inhibit Jack bean α-mannosidases. The present results reveal new biological activities of kujigamberol, which interfere with the pro-inflammatory cytokine-induced expression of and N-glycan modifications to cell adhesion molecules in HUVEC.