Transport properties of puerarin and effect of extract of Radix Angelicae dahuricae on puerarin intestinal absorption using in situ and in vitro models.
The root of Angelica dahurica (Radix Angelicae Dahuricae, RAD), which contains coumarins and volatile oil as its main classes of active components, is often given in conjunction with Pueraria root (Radix Puerariae, RP), which contains the phytoestrogen puerarin. The two herbs are considered to be compatible 'herb-pairs' in traditional Chinese medicine. The present investigation investigates the absorption of puerarin from RP and the effect of the total coumarins and volatile oil from RAD on its absorption. The everted gut sac and single-pass intestinal perfusion methods were used, respectively. The results showed that the absorption of puerarin in the jejunum was significantly increased in the presence of the coumarins and/or volatile oil. The absorption rate constant (K(a)) of puerarin increased gradually until the concentration reached 160 µg · mL(-1), after which its absorption became saturated and the apparent permeability (P(app)) values significantly decreased. The results showed that the intestinal absorption mechanisms of puerarin involved active transportation processes and that puerarin is likely to be a substrate of P-gp because verapamil significantly affected its P(app) and K(a). The absorption of puerarin significantly increased (p < 0.01) when combined with RAD extracts, as shown by the increase in concentration of puerarin in blood from the hepatic portal vein, supporting the concept of RAD and RP as a compatible herb-pair.
Key Laboratory of Modern Preparation of TCM of Ministry of Education, Jiangxi University of TCM, Nanchang, 330004, China.
Zheng-Gen
ZG
Liao
Xin-Li
XL
Liang
Jing-Yun
JY
Zhu
Guo-Wei
GW
Zhao
Yong-Mei
YM
Guan
Yun-Chao
YC
Cao
Li-Jun
LJ
Zhao
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism; D029969:Angelica / Q000737:chemistry; D000818:Animals; D003374:Coumarins / Q000494:pharmacology*; D004357:Drug Synergism; D004365:Drugs, Chinese Herbal / Q000493:pharmacokinetics*; D066298:In Vitro Techniques; D007408:Intestinal Absorption / Q000187:drug effects*; D007529:Isoflavones / Q000493:pharmacokinetics*; D007583:Jejunum / Q000378:metabolism; D008297:Male; D009822:Oils, Volatile / Q000494:pharmacology*; D018517:Plant Roots / Q000737:chemistry; D029908:Pueraria / Q000737:chemistry; D017207:Rats, Sprague-Dawley
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D003374:Coumarins; D004365:Drugs, Chinese Herbal; D007529:Isoflavones; D009822:Oils, Volatile; C033607:puerarin
Radix Angelicae dahurica extracts; everted rat gut sacs; in situ single-pass intestinal perfusion; intestinal absorption; puerarin; synergistic effects