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Echinacea-induced cytosolic Ca2+ elevation in HEK293.

Lankun Wu¹, Eric W Rowe, Ksenija Jeftinija

¹Department of Genetics, Development, and Cell Biology, Iowa State University, Ames, IA, 50011, USA.

BMC Complementary and Alternative Medicine

|November 25, 2010

Summary

Unidentified Echinacea purpurea compounds elevate calcium in non-immune cells via phospholipase C and IP3 receptors, distinct from CB2 pathways. This suggests novel immune-modulating mechanisms for Echinacea beyond known alkamides.

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Area of Science:

Pharmacology
Immunology
Cell Signaling

Background:

Echinacea preparations are widely used for immune support, with alkamides targeting cannabinoid type 2 (CB2) receptors proposed as a mechanism.
This study investigates Echinacea's effects on intracellular calcium (Ca2+) in non-immune cells, exploring pathways independent of CB2 receptors.

Purpose of the Study:

To identify compounds in Echinacea purpurea root extracts that modulate intracellular Ca2+ levels in non-immune cells.
To elucidate the signaling pathway involved in Echinacea-induced Ca2+ elevation in HEK293 cells.

Main Methods:

Human embryonic kidney 293 (HEK293) cells were used to assess E. purpurea root extracts and constituents.
Intracellular Ca2+ levels were monitored using calcium imaging, with inhibitors of phospholipase C (U73122) and inositol-1,4,5-trisphosphate (IP3) receptors (2-APB) employed.
High-performance liquid chromatography (HPLC) fractionation and gas chromatography-mass spectrometry (GC-MS) were used to identify active compounds.

Main Results:

E. purpurea extracts rapidly increased cytosolic Ca2+ in HEK293 cells, dependent on phospholipase C and IP3 receptors.
CB2 receptor antagonists did not block these effects, indicating CB2 independence.
Unknown lipophilic constituents, not alkamides, were associated with the observed Ca2+ response, suggesting a novel mechanism.

Conclusions:

Echinacea constituents stimulate Ca2+ release via IP3 receptors and phospholipase C in non-immune cells.
This pathway differs from the CB2 receptor-mediated pathway observed in immune cells, highlighting distinct Echinacea actions.