Selected ginsenosides of the protopanaxdiol series are novel positive allosteric modulators of P2X7 receptors.

ABSTRACT:

Background and purpose

The P2X7 receptor is an ATP-gated ion channel predominantly expressed in immune cells and plays a key role in inflammatory processes. Ginseng is a well-known Chinese herb with both pro- and anti-inflammatory properties and many of its actions have been ascribed to constituent ginsenosides. We screened a number of ginsenoside compounds for pharmacological activity at P2X7 receptors, that might contribute to the reported immunomodulatory actions of ginseng.

Experimental approach

We used several assays to measure responses of P2X7 receptors, ATP-mediated dye uptake, intracellular calcium measurement and whole-cell patch-clamp recordings. HEK-293 cells stably expressing human P2X7 receptors were used in addition to mouse macrophages endogenously expressing

SUBMITTER: Helliwell RM 

PROVIDER: S-EPMC4500369 | biostudies-literature | 2015 Jul

REPOSITORIES: biostudies-literature