IngentaConnect In-vitro Inhibition of Human Erythrocyte Acetylcholinesterase by ...

Authors: Perry N.S.L.¹; Houghton P.J.¹; Theobald A.²; Jenner† P.³; Perry‡ E.K.⁴

Source: Journal of Pharmacy and Pharmacology, Volume 52, Number 7, 1 July 2000 , pp. 895-902(8)

Abstract:

Sage (Salvia spp) is reputed in European herbal encyclopaedias to enhance memory, and current memory-enhancing/anti-dementia drugs are based on enhancing cholinergic activity by inhibiting cholinesterase. In this study the effects of Salvia lavandulaefolia Vahl. (Spanish sage) essential oil and some of its constituent terpenes on human erythrocyte acetylcholinesterase were examined in-vitro. The main constituents in the essential oil batch used for analysis of cholinesterase inhibition were camphor (27%), 1,8-cineole (13%), alpha

- and

-pinene (10–15%) and bornyl acetate (10%) with other minor constituents (1% or less) including geraniol, limonene, linalool, terpineol and gamma

-terpinene.

Using the Ellman spectrophotometric method, kinetic analysis was conducted on the interaction of the essential oil and the main monoterpenoids, camphor, 1,8-cineole and alpha

-pinene. IC50 values were obtained for the essential oil, 1,8-cineole and alpha

-pinene and were 0·03

g mL^-1, 0·67 mM and 0·63 mM, respectively. Camphor and other compounds tested (geraniol, linalool and gamma

-terpinene) were less potent (camphor IC50: >10 mM). The essential oil, alpha

-pinene, 1,8-cineole and camphor were found to be uncompetitive reversible inhibitors.

These findings suggest that if the inhibitory activity of the essential oil is primarily due to the main inhibitory terpenoid constituents identified, there is a major synergistic effect among the constituents. Since no single constituent tested was particularly potent, it remains to be determined whether these in-vitro cholinesterase inhibitory activities are relevant to in-vivo effects of the ingestion of S. lavandulaefolia essential oil on brain acetylcholinesterase activity.

Document Type: Research article

DOI: 10.1211/0022357001774598

Affiliations: 1: Pharmacognosy Research Laboratories 2: Department of Pharmacy, King’s College London, Franklin-Wilkins Building, 150 Stamford Street, London SE1 8WA 3: G. K. T. Centre for Biomedical Sciences, Division of Pharmacology and Therapeutics, King’s College London, Guy’s Campus, London Bridge, London SE1 1U2 4: MRC Neurochemical Pathology Unit, Newcastle General Hospital, Westgate Road, Newcastle Upon Tyne NE4 6BE, UK, peter.houghton@kcl.ac.uk

The full text electronic article is available for purchase. You will be able to download the full text electronic article after payment.

$38.34 plus tax Refund Policy

In-vitro Inhibition of Human Erythrocyte Acetylcholinesterase by Salvia lavandulaefolia Essential Oil and Constituent Terpenes