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In VitroEffects of the Dicyclohexylammonium Salt of Hyperforin on Interleukin-6 Release in Different Experimental Models
- Source :
- Planta Medica. 70:680-682
- Publication Year :
- 2004
- Publisher :
- Georg Thieme Verlag KG, 2004.
-
Abstract
- Cytokine hypersecretion might be involved in the onset and maintenance of depressive disorders and it has been suggested that St. John's wort extracts (Hypericum perforatum, SJW) might exert their antidepressant-like effects by affecting peripheral interleukin-6 (IL6) expression. We found that hyperforin, one putative active principle of SJW, and its dicyclohexylammonium salt (hyperforin-DCHA), inhibited the substance P (SP)-induced [L6 release inhuman astrocytoma cells (U373MG) with an Cs50 of 1.6 pM, indicating that hyperforin is likely to account for the inhibitory effect previously found in the same experimental model with SJW ex-tracts. [3H]SP binding experiments in parallel on the same intact cells indicate that hyperforin-DCHA does not interact with neuro-kinin-I receptors but very likely interacts with some intracellular steps leading to the synthesis and/or release of IL6. Hyperforin-DCHA also inhibited, with a similar IC50, the IL6 release induced in U373MG cells by two other classic proinflammatory stimuli,ILl and lipopolysaccharide (LPS), as well as the LPS-induced IL6 release in whole rat blood. Hyperforin-DCHA was less active in whole human blood. The concentrations required in vitro to inhibit LPS-induced IL6 release from rat and human whole blood are about one order of magnitude higher than the hyperforin levels measured in the plasma of rats or humans treated with pharmaco-logically active doses of SJW or hyperforin-DCHA.
- Subjects :
- Male
medicine.medical_treatment
Pharmaceutical Science
Phloroglucinol
Biology
Pharmacology
Models, Biological
Analytical Chemistry
Proinflammatory cytokine
Bridged Bicyclo Compounds
Inhibitory Concentration 50
chemistry.chemical_compound
Drug Discovery
medicine
Animals
Humans
Receptor
Whole blood
Cyclohexylamines
Interleukin-6
Plant Extracts
Terpenes
Organic Chemistry
Hypericum perforatum
Rats, Inbred Strains
Antidepressive Agents
In vitro
Rats
Hyperforin
Cytokine
Complementary and alternative medicine
Mechanism of action
chemistry
Models, Animal
Molecular Medicine
Female
medicine.symptom
Hypericum
Phytotherapy
Subjects
Details
- ISSN :
- 14390221 and 00320943
- Volume :
- 70
- Database :
- OpenAIRE
- Journal :
- Planta Medica
- Accession number :
- edsair.doi.dedup.....67c1d088a98d3461fea2164a972937ed