title: Antiallergic activity of hesperidin is activated by intestinal microflora.
abstract: When hesperidin isolated from pericarpium of Citrus unshiu (family Rutaceae) was incubated with human intestinal microflora, its main metabolite was hesperetin, which was a main metabolite in urine of orally hesperidin-administered rats. The antiallergic activity of hesperidin and its metabolite hesperetin were investigated. Hesperidin did not inhibit the histamine release from RBL-2H3 cells induced by IgE. However, its metabolite hesperetin potently inhibited the histamine release from RBL-2H3 cells induced by IgE and the PCA reaction. The inhibitory activity of hesperetin was found to be comparable with azelastine, a commercially available antiallergic drug, and to potently inhibit prostaglandin E2 production in lipopolysaccharide-stimulated RAW 264.7 cells. Hesperetin weakly inhibits cyclooxygenase 2 enzyme activities. These results suggest that hesperidin may be a prodrug, which is metabolized to hesperetin by intestinal bacteria.
authors.affiliation: School of Oriental Medicine, Kyung Hee University, Seoul, Korea.
authors.forename: Neung-Kee
authors.initials: NK
authors.lastname: Lee
authors.forename: Seung-Hoon
authors.initials: SH
authors.lastname: Choi
authors.forename: Sung-Hwan
authors.initials: SH
authors.lastname: Park
authors.forename: Eun-Kyung
authors.initials: EK
authors.lastname: Park
authors.forename: Dong-Hyun
authors.initials: DH
authors.lastname: Kim
mesh_terms: D000818:Animals; D018926:Anti-Allergic Agents / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology*; D002460:Cell Line; D002957:Citrus; D015232:Dinoprostone / Q000096:biosynthesis; D016166:Free Radical Scavengers / Q000494:pharmacology; D006168:Guinea Pigs; D006569:Hesperidin / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology*; D006636:Histamine Release / Q000187:drug effects; D006801:Humans; D006821:Hyaluronoglucosaminidase / Q000037:antagonists & inhibitors; D066298:In Vitro Techniques; D007413:Intestinal Mucosa / Q000378:metabolism*; D007422:Intestines / Q000382:microbiology*; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D009569:Nitric Oxide / Q000096:biosynthesis; D010323:Passive Cutaneous Anaphylaxis / Q000187:drug effects; D001619:beta-N-Acetylhexosaminidases / Q000037:antagonists & inhibitors
chemical_list: D018926:Anti-Allergic Agents; D016166:Free Radical Scavengers; D009569:Nitric Oxide; D006569:Hesperidin; D006821:Hyaluronoglucosaminidase; D001619:beta-N-Acetylhexosaminidases; D015232:Dinoprostone; C013015:hesperetin