Abstract
Salvia triloba, traditionally known as Greek sage, has been used to enhance memory, as a sedative and to treat headaches. Pharmacological evaluation of purified extracts and isolated compounds of S. triloba were carried out on functional assays using two-electrode voltage clamp methods on recombinant GABA receptors expressed in Xenopus laevis oocytes. Bio-assay guided fractionation led to seven compounds being isolated from S. triloba: ursolic acid, carnosol, oleanolic acid, salvigenin, rosmanol, cirsimaritin and hispidulin. The purified extracts of S. triloba inhibited 54% of the current produced by 300 μM GABA at α1β2γ2L GABAA receptors. Ursolic acid, carnosol, oleanolic acid and rosmanol also acted as negative allosteric modulators. The flavonoids salvigenin, cirsimaritin and hispidulin acted as positive modulators when applied in the presence of low concentrations of GABA but in the presence of high concentrations of GABA acted as negative modulators, demonstrating a biphasic action. These results are consistent with the concept that Salvia triloba may have cognition enhancing properties. In most cases these activities are likely to be occurring via different modulatory sites on GABAA receptor complexes. It may be that the combination of these activities permits cognition enhancement whilst offering protection from convulsant activity.
Highlights
Salvia triloba L. (Lamiaceae), traditionally known as Greek sage, is known by several other names including Salvia fruticosa, Salvia libanotica, Salvia lobryana, and Salvia cypria due to a taxonomic confusion over the years
We have studied the effects of extracts and isolated compounds from S. triloba on functional assays using two-electrode voltage clamp methods on recombinant GABAA receptors containing α1β2γ2L subunits expressed in Xenopus laevis oocytes
Previous studies have investigated some of the chemical constituents of sage at the GABAA/benzodiazepine complex and cholinergic receptors, few studies have investigated the constituents of Salvia at GABAA receptors using a functional electrophysiological assay
Summary
Salvia triloba L. (Lamiaceae), traditionally known as Greek sage, is known by several other names including Salvia fruticosa, Salvia libanotica, Salvia lobryana, and Salvia cypria due to a taxonomic confusion over the years. (Lamiaceae), traditionally known as Greek sage, is known by several other names including Salvia fruticosa, Salvia libanotica, Salvia lobryana, and Salvia cypria due to a taxonomic confusion over the years. It is a perennial Mediterranean herb and has been used to enhance memory [1], as a sedative [2] and to treat headaches [3]. Many phytochemicals are known to interact with receptors for the major inhibitory neurotransmitter GABA [4]. Such interaction may underlie some of the pharmacological effects of S. triloba. Another study demonstrated that compounds isolated from this plant increased the hypnotic effect of hexobarbital in the rat [6] [7], suggesting a benzodiazepine like effect
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