title: Bioconversion of quercetin and rutin and the cytotoxicity activities of the transformed products.
abstract: Quercetin and rutin are well-know flavonoids. In spite of this, the comprehension of their metabolism is still incomplete. In this work, the cytotoxic activity of quercetin and rutin and its metabolites produced by metabolism of filamentous fungi was investigated. Flavonoids metabolism was monitored by HPLC and LC-MS. Both flavonoids were extensively metabolized. Quercetin was converted into metabolite methylquercetin (2) and quercetin glucuronide (3) and rutin into metabolite rutin sulphate (5), methylrutin (6) and rutin glucuronide (7). Cytotoxic effects of rutin, quercetin and its metabolites were measured by MTT tetrazolium reduction test and the trypan blue exclusion assay on HL-60 leukemic cells. The results showed similar concentration-dependent cytotoxic effect for rutin and rutin sulphate (5), while no cytotoxic effect was detected with the metabolites 6 and 7. In relation to the quercetin and its metabolites the results showed that all compounds have a similar concentration-dependent inhibitory effect on HL-60 cells. These findings corroborate the literature, showing that bioconversion is a useful strategy for production of biological active metabolites.
authors.affiliation: Laboratório de Bioconversão, Faculdade de Farmácia, Universidade Federal de Goiás, Postal Box 131, 74.605-220 Goiânia, GO, Brazil.
authors.forename: Kelly Carolina Frauzino
authors.initials: KC
authors.lastname: Araújo
authors.forename: Eula Maria
authors.initials: EM
authors.lastname: de M B Costa
authors.forename: Francine
authors.initials: F
authors.lastname: Pazini
authors.forename: Marize Campos
authors.initials: MC
authors.lastname: Valadares
authors.forename: Valéria
authors.initials: V
authors.lastname: de Oliveira
mesh_terms: D052982:Beauveria / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D020093:Cunninghamella / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D018922:HL-60 Cells / Q000187:drug effects; D006801:Humans; D011794:Quercetin / Q000378:metabolism* / Q000493:pharmacokinetics*; D012431:Rutin / Q000031:analogs & derivatives / Q000378:metabolism* / Q000493:pharmacokinetics*
chemical_list: C056067:rutin sulfate; D012431:Rutin; D011794:Quercetin