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

Summary, in English

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.

• Författare: Diane M Rutherford; Mogens P Nielsen; Susanne K Hansen; Michael-Robin Witt; Ola Bergendorff; Olov Sterner
• Avdelning/ar: Dermatologi och venereologi, Lund; Centrum för analys och syntes
• Publiceringsår: 1992
• Språk: Engelska
• Sidor: 224-226
• Publikation/Tidskrift/Serie: Neuroscience Letters
• Volym: 135
• Issue: 2
• Länkar: http://dx.doi.org/10.1016/0304-3940(92)90441-9
• Dokumenttyp: Artikel i tidskrift
• Förlag: Elsevier
• Ämne: Neurosciences
• Nyckelord: γ-Aminobutyric acid; Benzodiazepine receptor; [35S]TBPS binding; Salvia officinalis; Diterpenoid; Carnosol; Carnosic acid
• Status: Published
• ISBN/ISSN/Övrigt: ISSN: 0304-3940