Research article summary (published 28 Feb 2004):

Novel diterpenoid acetylcholinesterase inhibitors from Salvia miltiorhiza.

Full Abstract

Acetylcholinesterase (AChE, EC 3.1.1.7) inhibitors are the only registered drugs used to treat Alzheimer's disease (AD). New AChE inhibitors may contribute to the design of new pharmaceuticals and supply information which will facilitate the understanding of the interaction between inhibitors and the enzyme. The dried root of Salvia miltiorhiza is called 'Danshen' in China, and has been used for the treatment of cerebrovascular disease and CNS deterioration in old age for over one thousand years. In this work, a modified Ellman method was used to guide the fractionation of the active AChE inhibitory compounds from an acetone extract. Four inhibitory compounds, dihydrotanshinone, cryptotanshinone, tanshinone I and tanshinone IIA were isolated, and the structures were identified by comparison of their spectral characteristics with previous reports. The inhibitory activities of dihydrotanshinone and cryptotanshinone were dose-dependent, their IC (50) values being 1.0 microM and 7.0 microM, respectively. These two compounds were the major inhibitory compounds in the extract as judged by HPLC analysis, forming 0.054 % w/w and 0.23 % w/w in the dried root, respectively, and in mixture they appear to be less active than as isolated compounds. The clogP values of dihydrotanshinone, cryptotanshinone, tanshinone I and tanshinone IIA were calculated as 2.4, 3.4, 4.8 and 5.8, respectively, which indicate that these compounds have potential to penetrate the blood-brain barrier. This is the first example of diterpenoids as inhibitors of AChE.

Author information

Author/s: Ren, Yuhao (Y); Houghton, Peter J (PJ); Hider, Robert C (RC); Howes, Melanie-Jayne R (MJ);

Affiliation: Department of Pharmacy, King's College London, U.K.

Journal and publication information

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

Journal: Planta medica (Planta Med), published in Germany. (Language: eng)

Reference: 2004-Mar; vol 70 (issue 3) : pp 201-4

Dates: Created 2004/04/28; Completed 2004/08/09; Revised 2006/11/15;

PMID: 15114495, status: MEDLINE (last retrieval date: 2/18/2009, IMS Date: )

Sourced from the National Library of Medicine. Abstract text and other information may be subject to copyright.

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MeSH headings (categories)

This article was linked to the MESH Headings shown below.

Acetylcholinesterase - drug effects Alzheimer Disease - drug therapy Cholinesterase Inhibitors - administration & dosage; pharmacology; therapeutic use Diterpenes - administration & dosage; pharmacology; therapeutic use Dose-Response Relationship, Drug

Humans Phytotherapy Plant Extracts - administration & dosage; pharmacology; therapeutic use Plant Roots Salvia miltiorrhiza

Associated Chemicals: Cholinesterase Inhibitors (0) ; Diterpenes (0) ; Plant Extracts (0) ; Acetylcholinesterase (EC 3.1.1.7)

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