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      Anticholinesterase Inhibitory Activity of Quaternary Alkaloids from Tinospora crispa

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          Abstract

          Quaternary alkaloids are the major alkaloids isolated from Tinospora species. A previous study pointed to the necessary presence of quaternary nitrogens for strong acetylcholinesterase (AChE) inhibitory activity in such alkaloids. Repeated column chromatography of the vine of Tinospora crispa extract led to the isolation of one new protoberberine alkaloid, 4,13-dihydroxy-2,8,9-trimethoxydibenzo[a,g]quinolizinium ( 1), along with six known alkaloids—dihydrodiscretamine ( 2), columbamine ( 3), magnoflorine ( 4), N-formylannonaine ( 5), N-formylnornuciferine ( 6), and N- trans-feruloyltyramine ( 7). The seven compounds were isolated and structurally elucidated by spectroscopic analysis. Two known alkaloids, namely, dihydrodiscretamine and columbamine are reported for the first time for this plant. The compounds were tested for AChE inhibitory activity using Ellman’s method. In the AChE inhibition assay, only columbamine ( 3) showed strong activity with IC 50 48.1 µM. The structure–activity relationships derived from these results suggest that the quaternary nitrogen in the skeleton has some effect, but that a high degree of methoxylation is more important for acetylcholinesterase inhibition.

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          Natural Products and Derivatives Affecting Neurotransmission Relevant to Alzheimer’s and Parkinson’s Disease

          Peter J. Houghton, Melanie-Jayne R Howes (2005)
          The two major neurodegenerative diseases Alzheimer’s disease (AD) and Parkinson’s disease (PD) are characterised by low levels in the brain of the neurotransmitters acetylcholine (ACh) and dopamine (DA), respectively. Clinical treatment of these two conditions is palliative and relies, in most cases, on improving stimulation at the relevant receptors by either increasing levels of the endogenous neurotransmitter or by the use of substances which have a similar agonist response. Natural products continue to provide useful drugs in their own right but also provide templates for the development of other compounds. The major advances in the treatment of AD have been the use of acetylcholinesterase inhibitors such as galantamine, huperzine A, physostigmine and its derivatives to increase the levels of ACh rather than the use of cholinergic compounds, although compounds with nicotinic properties have attracted some interest. In contrast, the treatment of PD has relied on the elevation of DA levels by use of L-DOPA, its precursor, and by the administration of dopaminergic agonists, especially the ergot alkaloid derivatives. The use of inhibitors of enzymes that cause breakdown of DA is an avenue which is being explored. As well as the major natural products of clinical interest, the paper discusses the chemistry, activity and usage of the constituents of plants used in traditional medicine for the treatment of diseases presenting symptoms similar to those characteristic for Alzheimer’s or Parkinson’s disease.
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            Antibacterial, anti-inflammatory, anti-cholinesterase and mutagenic effects of extracts obtained from some trees used in South African traditional medicine.

            I Eldeen, Johan van Griensven, Esam Elgorashi (2005)
            Extracts obtained from 10 trees used in South African traditional medicine were screened for antibacterial, anti-inflammatory (COX-1 and COX-2) and anti-cholinesterase activities and investigated for potential mutagenic effects using the Ames test. Antibacterial activity was detected using the disc-diffusion and micro-dilution assays. The extracts were tested against Gram-positive bacteria: Bacillus subtilis, Staphylococcus aureus, Micrococcus luteus and Gram-negative bacteria: Escherichia coli and Klebsiella pneumoniae. Of the 78 different plant extracts investigated, 80% showed activity against both Gram-positive and Gram-negative bacteria in the disc-diffusion assay. In the micro-dilution assay, 60% of the plant extracts showed minimum inhibitory concentration (MIC) values 50% and 70% for water and organic solvent extracts, respectively). An ethyl acetate leaf extract of Trichilia dregeana showed selective inhibition of COX-2 (81%). In the acetylcholinesterase inhibitory test, 21% of the plant extracts were active at a concentration < or =1 mg ml(-1) using the micro-dilution assay. The lowest IC(50) value was 0.04 mg ml(-1) obtained with an ethanol bark extract of Combretum kraussii. None of the investigated plants showed any potential mutagenic effects.
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              Qualitative and quantitative structure activity relationships for the inhibitory effects of cationic head groups, functionalised side chains and anions of ionic liquids on acetylcholinesterase

              Johannes Ranke, Jürgen Arning, Bernd Jastorff … (2008)
              Article 0 comments Cited 30 times – based on 0 reviews     Review now
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                Author and article information

                Journal
                Journal ID (nlm-ta): Molecules
                Journal ID (iso-abbrev): Molecules
                Journal ID (publisher-id): molecules
                Title: Molecules
                Publisher: MDPI
                ISSN (Electronic): 1420-3049
                Publication date (Electronic): 20 January 2014
                Publication date Collection: January 2014
                Volume: 19
                Issue: 1
                Pages: 1201-1211
                Affiliations
                [1 ]Faculty of Industrial Sciences & Technology, Universiti Malaysia Pahang, Lebuhraya Tun Razak, Gambang Kuantan, Pahang 26300, Malaysia; E-Mail: hazrulrizawati@ 123456ump.edu.my
                [2 ]Department of Pharmacy, King’s College London, Franklin-Wilkins Building, 150 Stamford Street, London SE1 8WA, UK; E-Mail: peter.houghton@ 123456kcl.ac.uk
                Author notes
                [* ]Author to whom correspondence should be addressed; E-Mail: mashitah@ 123456ump.edu.my ; Tel.: +60-9-549-2767; Fax: +60-9-549-2766.
                Article
                Publisher ID: molecules-19-01201
                DOI: 10.3390/molecules19011201
                PMC ID: 6270727
                PubMed ID: 24448061
                SO-VID: 8dd388ce-052a-461f-aef8-6273e255d9fd
                Copyright © © 2014 by the authors.
                License:

                Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license ( http://creativecommons.org/licenses/by/3.0/).

                History
                Date received : 01 December 2013
                Date revision received : 14 January 2014
                Date accepted : 15 January 2014
                Categories
                Subject: Communication

                Keywords: tinospora crispa,menispermaceae,ethnoremedy,anticholinesterase inhibitory activities,quaternary alkaloids,4,13-dihydroxy-2,8,9-trimethoxydibenzo[a,g]quinolizinium,dihydrodiscretamine,columbamine
                Data availability:
                Keywords: tinospora crispa, menispermaceae, ethnoremedy, anticholinesterase inhibitory activities, quaternary alkaloids, 4,13-dihydroxy-2,8,9-trimethoxydibenzo[a,g]quinolizinium, dihydrodiscretamine, columbamine

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