Intestinal absorptive transport of Genkwanin from Flos genkwa using a single-pass intestinal perfusion rat model.
To investigate the absorptive transport behavior of genkwanin and the beneficial effects of monoterpene enhancers with different functional groups, the single-pass intestinal perfusion (SPIP) of rats was used. The results showed that genkwanin was segmentally-dependent and the best absorptive site was the duodenum. The effective permeability coefficient (P eff ) was 1.97 × 10(-4) cm/s and the absorption rate constant (Ka) was 0.62 × 10(-2) s(-1). Transepithelial transportation descended with increasing concentrations of genkwanin. This was a 1.4-fold increase in P eff by probenecid, whereas a 1.4-fold or 1.6-fold decrease was observed by verapamil and pantoprazole, respectively. Furthermore, among the absorption enhancers, the enhancement with carbonyl (camphor and menthone) was higher than that with hydroxyl (borneol and menthol). The concentration-independent permeability and enhancement by coperfusion of probenecid indicated that genkwanin was transported by both passive diffusion and multidrug resistance protein (MDR)-mediated efflux mechanisms.
State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China.
Cui-Ping
CP
Jiang
Xin
X
He
Xiao-Lin
XL
Yang
Su-Li
SL
Zhang
Hui
H
Li
Zi-Jing
ZJ
Song
Chun-Feng
CF
Zhang
Zhong-Lin
ZL
Yang
Ping
P
Li
D053799:2-Pyridinylmethylsulfinylbenzimidazoles / Q000494:pharmacology; D018435:ATP Binding Cassette Transporter, Subfamily B / Q000378:metabolism; D000818:Animals; D001692:Biological Transport; D004305:Dose-Response Relationship, Drug; D004386:Duodenum / Q000378:metabolism*; D047309:Flavones / Q000378:metabolism*; D007408:Intestinal Absorption; D007413:Intestinal Mucosa / Q000378:metabolism; D008297:Male; D023421:Models, Animal; D000077402:Pantoprazole; D010477:Perfusion / Q000379:methods*; D011339:Probenecid / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D014700:Verapamil / Q000494:pharmacology
D053799:2-Pyridinylmethylsulfinylbenzimidazoles; D018435:ATP Binding Cassette Transporter, Subfamily B; D047309:Flavones; C014568:genkwanin; D014700:Verapamil; D000077402:Pantoprazole; D011339:Probenecid