Apocynum venetum extract does not induce CYP3A and P-glycoprotein in rats.
We investigated the effect of Apocynum venetum L. extract (AV) on the activity of cytochrome P450 (CYP) 3A and P-glycoprotein (P-gp). The plasma concentration of nifedipine (NF), which is a substrate for CYP3A, did not change after oral administration with AV (3.3 mg/kg). Also, AV (3.3 and 33 mg/kg) did not affect the intestinal absorption of NF. In the rats treated with multiple administrations (15 mg/kg/d) of St. John's wort extract (SJW) for 2 weeks, the plasma concentration of NF after oral administration was significantly decreased. On the other hand, there was no significant differences in the pharmacokinetic parameters of NF between AV-treated (3.3 mg/kg/d) and none-treated rats. Furthermore, the intestinal absorption of methylprednisolone, which is a substrate for P-gp, was not affected by AV treatment for 2 weeks. These results suggest that, unlike SJW, the recommended dose of AV (3.3 mg/kg/d) would not influence hepatic CYP3A and intestinal P-gp in rats.
Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido, Ishikari-Tobetsu, Japan.
Michiya
M
Kobayashi
Hiroshi
H
Saitoh
Shujiro
S
Seo
Veronika
V
Butterweck
Sansei
S
Nishibe
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000096:biosynthesis*; D000818:Animals; D030010:Apocynum; D001189:Aryl Hydrocarbon Hydroxylases / Q000096:biosynthesis*; D051544:Cytochrome P-450 CYP3A; D041743:Herb-Drug Interactions; D020902:Hypericum; D066298:In Vitro Techniques; D007408:Intestinal Absorption; D008297:Male; D008775:Methylprednisolone / Q000493:pharmacokinetics; D009543:Nifedipine / Q000493:pharmacokinetics; D010089:Oxidoreductases, N-Demethylating / Q000096:biosynthesis*; D010936:Plant Extracts / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D010936:Plant Extracts; D001189:Aryl Hydrocarbon Hydroxylases; D051544:Cytochrome P-450 CYP3A; D010089:Oxidoreductases, N-Demethylating; D009543:Nifedipine; D008775:Methylprednisolone