Home
Resources
Publications
Comparative Pharmacokinetics of Arctigenin in Normal and Type 2 Diabetic Rats After Oral and Intravenous Administration

Comparative Pharmacokinetics of Arctigenin in Normal and Type 2 Diabetic Rats After Oral and Intravenous Administration

Xiao-yan Zeng, Shu Dong, Nan-nan He, Chun-jie Jiang, Yue Dai, Yu-feng Xia

Fitoterapia. 2015 Sep;105:119-26.

PMID: 26102179

Abstract:

Arctigenin is the main active ingredient of Fructus Arctii for the treatment of type 2 diabetes. In this study, the pharmacokinetics of arctigenin in normal and type 2 diabetic rats following oral and intravenous administration was investigated. As compared to normal rats, Cmax and AUC(0-10h) values of oral arctigenin in diabetic rats increased by 356.8% and 223.4%, respectively. In contrast, after intravenous injection, the Cmax and AUC(0-10h) values of arctigenin showed no significant difference between diabetic and normal rats. In order to explore how the bioavailability of oral arctigenin increased under diabetic condition, the absorption behavior of arctigenin was evaluated by in situ single-pass intestinal perfusion (SPIP). The results indicated that arctigenin was a substrate of P-glycoprotein (P-gp). The absorption difference of arctigenin in the normal and diabetic rats could be eliminated by the pretreatment of classic P-gp inhibitor verapamil, suggesting that P-gp might be the key factor causing the absorption enhancement of arctigenin in diabetic rats. Further studies revealed that the uptake of rhodamine 123 (Rho123) in diabetic rats was significantly higher, indicating that diabetes mellitus might impair P-gp function. Consistently, a lower mRNA level of P-gp in the intestine of diabetic rats was found. In conclusion, the absorption of arctigenin after oral administration was promoted in diabetic rats, which might be partially attribute to the decreased expression and impaired function of P-gp in intestines.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
ALP461054933	Ko143 hydrate		461054-93-3 (anhydrous)	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: