Abstract
Herbal medicinal products are commonly used in alternative treatment of
menopausal hot flushes. In a recent clinical study, Salvia
officinalis tincture was found to reduce hot flush frequency and
intensity. The aim of the current study was the investigation of the
mechanism(s) responsible for the anti-hot flush activity of S.
officinalis and determination of its active principle(s). The 66 %
ethanolic tincture, as well as the n-hexane, CHCl3, and
aqueous ethanolic subextracts obtained from the tincture were studied in
vitro for two of the most relevant activities, estrogenicity and
selective serotonin reuptake inhibition. Because of an increased risk of
menopausal women to suffer from Alzheimerʼs disease, an in vitro
acetylcholinesterase inhibition assay was also employed. No activity was
observed in the selective serotonin reuptake inhibition or the
acetylcholinesterase inhibition assays at the highest test concentrations.
The tincture showed no estrogenic effects whereas the aqueous ethanolic
subextract exhibited estrogenicity in the ERLUX assay with an
EC50 value of 64 µg/mL. Estrogenic activity-guided
fractionation of the aqueous ethanolic subextract by a combination of
reverse-phase vacuum liquid chromatography and gel chromatography identified
luteolin-7-O-glucuronide (EC50 129 µg/mL) as the
active component of the vacuum liquid chromatography fraction 4
(EC50 69 µg/mL). Luteolin-7-O-glucoside was identified
as the putative estrogenic principle of the most potent minor fraction
(7.6.7.6, EC50 0.7 µg/mL) obtained from the initial vacuum liquid
chromatography fraction 7 (EC50 3 µg/mL). This study suggests the
involvement of common and ubiquitous estrogenic flavonoids in the anti-hot
flush effect of Salvia officinalis, a safe and commonly used herbal
medicinal product during the menopause.
Key words
estrogenicity - hot flush - luteolin-7-
O-glucoside - menopause -
Salvia officinalis
- Lamiaceae
