In vitro basal and metabolism-mediated cytotoxicity of flavonoids.
The purpose of this study was to compare the basal cytotoxicity and metabolism-mediated cytotoxicity of kaempferol, quercetin and rutin. McCoy cells were exposed to various concentrations of the flavonols with and without the S9 system. The neutral red uptake assay was used to determine viability after 24 h at 35-37 degrees C. Dose-response curves were established for each flavonol in the presence and absence of external metabolizing systems. Kaempferol and quercetin were cytotoxic and provoked a dose-dependent decrease in cell viability, without the S9 system. The hepatic S9 microsomal fraction metabolized these compounds to less cytotoxic metabolites. In contrast, rutin at 500 microg/ml failed to produce any overt signs of toxicity in either assay.
Soares
V C G
VC
UNESP-Universidade Estadual Paulista, Instituto de Química de Araraquara, CEP 14801-902, Araraquara, SP, Brazil.
Varanda
E A
EA
Raddi
M S G
MS
D000818:Animals; D016923:Cell Death / Q000187:drug effects*; D002460:Cell Line; D020111:Chlorodiphenyl (54% Chlorine) / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D005347:Fibroblasts; D005419:Flavonoids / Q000008:administration & dosage / Q000378:metabolism / Q000633:toxicity*; D044949:Kaempferols / Q000008:administration & dosage / Q000378:metabolism / Q000633:toxicity; D051379:Mice; D008862:Microsomes, Liver / Q000187:drug effects / Q000378:metabolism*; D011794:Quercetin / Q000008:administration & dosage / Q000378:metabolism / Q000633:toxicity; D051381:Rats; D017207:Rats, Sprague-Dawley; D012431:Rutin / Q000008:administration & dosage / Q000378:metabolism / Q000633:toxicity
D005419:Flavonoids; D044949:Kaempferols; D020111:Chlorodiphenyl (54% Chlorine); D012431:Rutin; C006552:kaempferol; D011794:Quercetin