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Coumarins belong to a diverse group of naturally occurring non-nutrient phytochemicals known as benzo-α-pyrones.In this study,esculetin,a 6,7-dihydroxy derivative of coumarin with pleiotropic biological activities,wasfound to have no significant cytotoxic effect on normal murine macrophages,but it could increase the in vivomigration of the thioglycollate-elicited macrophages in a dose-dependent manner.Moreover,esculetin significantlyincreased the endocytic activity,and augmented the nitric oxide production and iNOS gene expression inLPS-treated macrophages.In addition,in vivo administration of esculetin into mice was shown to increase themitogenesis of splenic lymphocytes towards Con A and LPS stimulations,and induced the LAK activity of spleniclymphocytes.Collectively,our results indicate that esculetin could exert immunomodulatory effects on murinemacrophages and lymphocytes,both in vitro and in vivo,and this might be one of the possible mechanisms bywhich coumarins can exert their chemopreventive and anti-tumor activities in vivo.Cellular & MolecularImmunology.2005;2(3):181-188.
Coumarins belong to a diverse group of naturally occurring non-nutrient phytochemicals known as benzo-α-pyrones. In this study, esculetin, a 6,7-dihydroxy derivative of coumarin with pleiotropic biological activities, wasfound to have no significant cytotoxic effect on normal murine macrophages, but it could increase the in vivomigration of the thioglycollate-elicited macrophages in a dose-dependent manner. Moreover, esculetin significantly increased the endocytic activity, and augmented the nitric oxide production and iNOS gene expression in LPS-treated macrophages. In addition, in vivo administration of esculetin into mice was shown to increase the mitogenesis of splenic lymphocytes towards Con A and LPS stimulations, and induced the LAK activity of spleniclymphocytes. Collectively, our results indicate that esculetin could exert immunomodulatory effects on murinema corophages and lymphocytes, both in vitro and in vivo, and this might be one of the possible mechanisms bywhich coumarins can exert their chemopreventive and anti-tumor activities in vivo. Cellular & Molecular Immunology. 2005; 2 (3): 181-188.