TY - JOUR
T1 - Pharmacokinetics of isoliquiritigenin and its metabolites in rats
T2 - Low bioavailability is primarily due to the hepatic and intestinal metabolism
AU - Lee, Yu Kyung
AU - Chin, Young Won
AU - Bae, Jin Kyung
AU - Seo, Jun Su
AU - Choi, Young Hee
PY - 2013/10/9
Y1 - 2013/10/9
N2 - Isoliquiritigenin, a chalcone found in licorice has shown a variety of biological activities including antioxidative, anti-inflammatory, estrogenic, chemopreventive and antitumor effects. Thus, pharmacokinetics of isoliquiritigenin and its metabolites [liquiritigenin, glucuronidated isoliquiritigenin (M1), and glucuronidated liquiritigenin (M2)] after intravenous and oral administration of isoliquiritigenin was evaluated in rats. The pharmacokinetics of isoliquiritigenin, liquiritigenin, M1, and M2 showed no dose dependence after both intravenous and oral administration of isoliquiritigenin. Although approximately 92.0 % of the oral isoliquiritigenin was absorbed, the extent of the absolute bioavailability value was only 11.8 % of the oral dose. The low absolute bioavailability value of isoliquiritigenin might be due to the considerable metabolism of isoliquiritigenin in the small intestine and liver. This was supported by the facts that the ratios of AUCM1/AUCisoLQ and AUCM2/AUCisoLQ were high (over 0.25), isoliquiritigenin disappeared, and M1 and M2 were formed mainly in S9 fractions of the liver and small intestine. The affinities of liquiritigenin, isoliquiritigenin, M1, and M2 were high in the liver, small intestine, large intestine, and/or kidney.
AB - Isoliquiritigenin, a chalcone found in licorice has shown a variety of biological activities including antioxidative, anti-inflammatory, estrogenic, chemopreventive and antitumor effects. Thus, pharmacokinetics of isoliquiritigenin and its metabolites [liquiritigenin, glucuronidated isoliquiritigenin (M1), and glucuronidated liquiritigenin (M2)] after intravenous and oral administration of isoliquiritigenin was evaluated in rats. The pharmacokinetics of isoliquiritigenin, liquiritigenin, M1, and M2 showed no dose dependence after both intravenous and oral administration of isoliquiritigenin. Although approximately 92.0 % of the oral isoliquiritigenin was absorbed, the extent of the absolute bioavailability value was only 11.8 % of the oral dose. The low absolute bioavailability value of isoliquiritigenin might be due to the considerable metabolism of isoliquiritigenin in the small intestine and liver. This was supported by the facts that the ratios of AUCM1/AUCisoLQ and AUCM2/AUCisoLQ were high (over 0.25), isoliquiritigenin disappeared, and M1 and M2 were formed mainly in S9 fractions of the liver and small intestine. The affinities of liquiritigenin, isoliquiritigenin, M1, and M2 were high in the liver, small intestine, large intestine, and/or kidney.
KW - Fabaceae
KW - glucuronidated metabolites
KW - Glycyrrhiza glabra
KW - isoliquiritigenin
KW - liquiritigenin
KW - pharmacokinetics
UR - http://www.scopus.com/inward/record.url?scp=84889596807&partnerID=8YFLogxK
U2 - 10.1055/s-0033-1350924
DO - 10.1055/s-0033-1350924
M3 - Article
C2 - 24108436
AN - SCOPUS:84889596807
SN - 0032-0943
VL - 79
SP - 1656
EP - 1665
JO - Planta Medica
JF - Planta Medica
IS - 17
ER -