Abstract

Tylogenin, a steroidal aglycone generated by acid hydrolysis from two seasonal glycosides occurring in Tylophora sylvatica, inhibits IgE-induced basophil mediator release for allergic reactions. In the rabbit basophil-dependent serotonin release (BDSR) assay system, the inhibitory activity of tylogenin (geom mean IC 50 = 39 μM) was significantly ( P<0.05) greater than that of its parent glycosides, tylophoroside (geom mean IC 50 253 μM) and acetyltylophoroside (geom mean IC 50 331 μM), and that of dexamethasone (geom mean IC 50 = 912 μM). The activity of tylogenin was found to increase with the incubation time. In the human leukocyte-dependent histamine release (LDHR) test model, the glycosides had only a minimal activity. In contrast, tylogenin, with a geom mean IC 50 = 49 μM, exerted a significantly ( P<0.05) greater potency than dexamethasone (IC 50 = 257 μM). These results suggest that tylogenin could represent a new class of antiallergic agents.

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