In vitro solubility, stability and permeability of novel quercetin-amino acid conjugates.
In order to discover a quercetin prodrug with improved bioavailability, we synthesized nine quercetin-amion acid conjugates and estimated their pharmacokinetic properties including water solubility, stability against chemical or enzymatic hydrolysis, and cell permeability. Among the synthesized quercetin prodrugs, quercetin-glutamic acid conjugate Qu-E (4g/5g) showed remarkable increases in water solubility, stability, and cell permeability compared with quercetin, which warrants further development as a quercetin prodrug.
Kim
Mi Kyoung
MK
Department of Bioscience and Biotechnology, Konkuk University, Seoul 143-701, Republic of Korea.
Park
Kwang-su
KS
Yeo
Woon-seok
WS
Choo
Hyunah
H
Chong
Youhoon
Y
D000596:Amino Acids / Q000138:chemical synthesis / Q000737:chemistry; D000818:Animals; D002460:Cell Line; D004285:Dogs; D006207:Half-Life; D010539:Permeability; D011355:Prodrugs / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D011794:Quercetin / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D012995:Solubility
D000596:Amino Acids; D011355:Prodrugs; D011794:Quercetin