Role of P-glycoproteins in the transepithelial transport of indoline alkaloids isolated from Vinca herbaceae.

Autor: Tsiklauri, L., Hoyer, H., Chkhikvadze, G., Vachnadze, V., Tsagareishvili, G., Bakuridze, A., Bernkop-Schnurch, A.
Předmět:
Zdroj: Pharmaceutical Chemistry Journal; Dec2008, Vol. 42 Issue 12, p693-695, 3p, 2 Graphs
Abstrakt: The permeability of anti-arrhythmic crude alkaloids (Vingerbine preparation) from Vinca herbaceae W. et Kit. across rat intestine has been demonstrated for the first time. The results suggest that P-glycoproteins (P-gps) are involved in the preferential transport of vincarine and herbadine, compounds bearing a hydrogen atom on a secondary N (N―H), in the basolateral to apical direction. However, P-gp/MDR1 play a minor role in the intestinal transport of herbamine and vincamajine, compounds with substituted N (N―CH3). In order to improve peroral bioavailability and achieve maximum therapeutic efficiency of Vingerbine, further research will be focused on finding a strategy to overcome the P-gp barrier and developing suitable delivery systems. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index