1378214

Isolation and identification from Salvia officinalis of two diterpenes which inhibit t-butylbicyclophosphoro[35S]thionate binding to chloride channel of rat cerebrocortical membranes in vitro.

Article date: 1992/2/3

PubMed ID: 1378214

Journal name: Neuroscience letters (ISSN: 0304-3940)

ABSTRACT

Ethanolic extracts from dried leaves of sage (Salvia officinalis) showed inhibition of [35S]tertiary-butylbicyclophosphorothionate ([35S]TBPS) binding to rat brain membranes in vitro. This ligand is considered to bind to the chloride channel of the GABA/benzodiazepine receptor complex in brain tissue. Substances having inhibitory activity were purified and their chemical structure identified as the diterpenes carnosic acid and carnosol (IC50 values of 33 +/- 3 microM and 57 +/- 4 microM, respectively). The two compounds did not affect binding of the ligands [3H]muscimol and [3H]diazepam to the GABA/benzodiazepine complex in vitro. Saturation experiments of [35S]TBPS binding indicated that carnosic acid decreases the binding affinity.

Author List: Rutherford D M, Nielsen M P, Hansen S K, Witt M R, Bergendorff O, Sterner O

Publication Types: Journal Article; Research Support, Non-U.S. Gov't

Substances mentioned in the article: Bridged Bicyclo Compounds; Bridged Bicyclo Compounds, Heterocyclic; Chlorides; Diterpenes; Diterpenes, Abietane; Ion Channels; Phenanthrenes; Plant Extracts; Receptors, GABA-A; carnosol; tert-butylbicyclophosphorothionate;

Mesh terms: Animals; Bridged Bicyclo Compounds/metabolism; Bridged Bicyclo Compounds, Heterocyclic; Cerebral Cortex/drug effects; Chlorides/metabolism; Diterpenes/chemistry; Diterpenes, Abietane; Ion Channels/drug effects; Kinetics; Magnetic Resonance Spectroscopy; Male; Mass Spectrometry; Phenanthrenes/pharmacology; Plant Extracts/chemistry; Plants, Medicinal/chemistry; Radioligand Assay; Rats; Rats, Inbred Strains; Receptors, GABA-A/drug effects;

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