Interspecies comparison of pharmacokinetic profile and bioavailability of (±)-gossypol in male Fischer-344 rats and male B6C3F mice

The Pharmacokinetics Study of Gossypol-acetate Enantiomers in Rat

“…And the pharmacokinetics parameters of GA enantiomers were fitted to three-compartment model with intervals administration. These results were consistent with the one reported 21 years ago [9] .…”

The Pharmacokinetics Study of Gossypol-acetate Enantiomers in Rat

“…And the pharmacokinetics parameters of GA enantiomers were fitted to three-compartment model with intervals administration. These results were consistent with the one reported 21 years ago [9] .…”

Gossypol Exhibits a Strong Influence Towards UDP-Glucuronosyltransferase (UGT) 1A1, 1A9 and 2B7-Mediated Metabolism of Xenobiotics and Endogenous Substances

“…Gossypol was demonstrated to exhibit inhibitory effects on the metabolism of xenobiotic and endogenous substances catalyzed by UGT1A1, 1A9 and 2B7, with the Ki values of 34.2, 16.4 and 14 μM, respectively. Previous reports have showed that the maximum plasma concentration can reach more than 10 μg/mL (19.3 μM) after mice received a single 50 mg/kg intravenous dose [22], which is very close to Ki values and suggest the risk of metabolic disorders of some endogenous substances and alteration of metabolic behaviour of co-administered xenobiotics through inhibition of UGTs’ activity.…”

Gossypol as undesirable substance in animal feed - Scientific Opinion of the Panel on Contaminants in the Food Chain

“…Another study on mice reported half lives after a single and after multiple oral doses of 10 mg/kg b.w. to be fairly similar, 36 and 20.4 hours, respectively (Abou-Donia et al, 1989). The faeces was confirmed as the primary route for elimination of gossypol in rats by Chen et al (1987).…”

“…The terminal half-life of racemic gossypol in F-344 rats administered 10 mg/kg b.w. orally as a single dose, or as daily doses for 14 days was 4.3 and 139 hours, respectively (Abou-Donia et al, 1989). In Sprague Dawley rats, the elimination half-life, after multiple doses of gossypol racemate, has been reported to 102 hours (Othman and Abou-Donia, 1988).…”

The Pharmacokinetics Study of Gossypol-acetate Enantiomers in Rat

“…And the pharmacokinetics parameters of GA enantiomers were fitted to three-compartment model with intervals administration. These results were consistent with the one reported 21 years ago [9] .…”

Gossypol Exhibits a Strong Influence Towards UDP-Glucuronosyltransferase (UGT) 1A1, 1A9 and 2B7-Mediated Metabolism of Xenobiotics and Endogenous Substances

“…Gossypol was demonstrated to exhibit inhibitory effects on the metabolism of xenobiotic and endogenous substances catalyzed by UGT1A1, 1A9 and 2B7, with the Ki values of 34.2, 16.4 and 14 μM, respectively. Previous reports have showed that the maximum plasma concentration can reach more than 10 μg/mL (19.3 μM) after mice received a single 50 mg/kg intravenous dose [22], which is very close to Ki values and suggest the risk of metabolic disorders of some endogenous substances and alteration of metabolic behaviour of co-administered xenobiotics through inhibition of UGTs’ activity.…”

Gossypol as undesirable substance in animal feed - Scientific Opinion of the Panel on Contaminants in the Food Chain

“…Another study on mice reported half lives after a single and after multiple oral doses of 10 mg/kg b.w. to be fairly similar, 36 and 20.4 hours, respectively (Abou-Donia et al, 1989). The faeces was confirmed as the primary route for elimination of gossypol in rats by Chen et al (1987).…”

“…The terminal half-life of racemic gossypol in F-344 rats administered 10 mg/kg b.w. orally as a single dose, or as daily doses for 14 days was 4.3 and 139 hours, respectively (Abou-Donia et al, 1989). In Sprague Dawley rats, the elimination half-life, after multiple doses of gossypol racemate, has been reported to 102 hours (Othman and Abou-Donia, 1988).…”

The Pharmacokinetics Study of Gossypol-acetate Enantiomers in Rat

“…And the pharmacokinetics parameters of GA enantiomers were fitted to three-compartment model with intervals administration. These results were consistent with the one reported 21 years ago [9] .…”

Gossypol Exhibits a Strong Influence Towards UDP-Glucuronosyltransferase (UGT) 1A1, 1A9 and 2B7-Mediated Metabolism of Xenobiotics and Endogenous Substances

“…Gossypol was demonstrated to exhibit inhibitory effects on the metabolism of xenobiotic and endogenous substances catalyzed by UGT1A1, 1A9 and 2B7, with the Ki values of 34.2, 16.4 and 14 μM, respectively. Previous reports have showed that the maximum plasma concentration can reach more than 10 μg/mL (19.3 μM) after mice received a single 50 mg/kg intravenous dose [22], which is very close to Ki values and suggest the risk of metabolic disorders of some endogenous substances and alteration of metabolic behaviour of co-administered xenobiotics through inhibition of UGTs’ activity.…”

Gossypol as undesirable substance in animal feed - Scientific Opinion of the Panel on Contaminants in the Food Chain

“…Another study on mice reported half lives after a single and after multiple oral doses of 10 mg/kg b.w. to be fairly similar, 36 and 20.4 hours, respectively (Abou-Donia et al, 1989). The faeces was confirmed as the primary route for elimination of gossypol in rats by Chen et al (1987).…”

“…The terminal half-life of racemic gossypol in F-344 rats administered 10 mg/kg b.w. orally as a single dose, or as daily doses for 14 days was 4.3 and 139 hours, respectively (Abou-Donia et al, 1989). In Sprague Dawley rats, the elimination half-life, after multiple doses of gossypol racemate, has been reported to 102 hours (Othman and Abou-Donia, 1988).…”