dc.contributor.author |
Adewusi, Emmanuel Adekanmi
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dc.contributor.author |
Fouche, Gerda
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dc.contributor.author |
Steenkamp, Vanessa
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dc.date.accessioned |
2012-11-23T10:03:51Z |
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dc.date.available |
2012-11-23T10:03:51Z |
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dc.date.issued |
2012-09-28 |
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dc.description.abstract |
ETHNOPHARMACOLOGICAL RELEVANCE: Boophane disticha of the family Amaryllidaceae is used traditionally in southern Africa in the treatement of several neurological disorders.
AIM OF THE STUDY: Although acetylcholinesterase (AChE) inhibitory activity has been reported for this plant, the aim of the study was to identify and characterise the compound responsible for this activity using bioassay guided fractionation. Toxicity of the isolated compound was also assessed.
MATERIALS AND METHODS: Bioassay guided isolation of the active compound from the methanol extract was carried out using column chromatography, TLC and preparative thin layer chromatography. Structural elucidation was carried out using high field 1D and 2D NMR and mass spectroscopy. AChE inhibitory activity was determined using the Ellman’s colorimetric method. Cytotoxicity assessment was determined in human neuroblastoma (SH-SY5Y) cells using the MTT and neutral red uptake assays.
RESULTS: The data obtained from the integration of the 1H spectra confirmed the compound to be a 3:1 mixture of two epimers, with epimer A, 6α-hydroxycrinamine as the major epimer. The IC50 value for AChE inhibitory activity of the compound was 445 µM. The compound was observed to be cytotoxic in both the MTT and neutral red assays with IC50 values of 54.5 and 61.7 µM, respectively.
CONCLUSION: The present study describes for the first time, the isolation of 6-hydroxycrinamine, a crinine alkaloid, from the methanol extract of the bulbs of B. disticha. Although this compound possessed AChE inhibitory activity, it was found to be toxic to the neuroblastoma cells. Quantitative structure-activity relationship studies could be carried out to modify the structure in order to make it less toxic and improve its activity. |
en_US |
dc.description.sponsorship |
The Department of Pharmacology, University of Pretoria |
en_US |
dc.description.uri |
http://www.elsevier.com/locate/jep |
en_US |
dc.identifier.citation |
Emmaneul Adekanmi Adewusi, Gerda Fouche & Vanessa Steenkamp, Cytotoxicity and acetylcholinesterase inhibitory activity of an isolated crinine alkaloid from Boophane disticha (Amaryllidaceae), Journal of Ethnopharmacology, vol. 143, no. 2, pp. 572-578 (2012), doi: 10.1016/j.jep.2012.07.011. |
en_US |
dc.identifier.issn |
0378-8741 (print) |
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dc.identifier.issn |
1872-7573 (online) |
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dc.identifier.other |
10.1016/j.jep.2012.07.011 |
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dc.identifier.uri |
http://hdl.handle.net/2263/20470 |
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dc.language.iso |
en |
en_US |
dc.publisher |
Elsevier |
en_US |
dc.rights |
© 2012 Elsevier. All rights reserved. Notice : this is the author’s version of a work that was accepted for publication in Journal of Ethnopharmacology. Changes resulting from the publishing process, such as peer review, editing, corrections, structural formatting and other quality control mechanisms may not be reflected in this document. Changes may have been made to this work since it was submitted for publication. A definitive version was subsequently published in Journal of Ethnopharmacology, vol 143, issue 2, September 2012, doi:10.1016/j.jep.2012.07.011. |
en_US |
dc.subject |
Acetylcholinesterase |
en_US |
dc.subject |
Amaryllidaceae |
en_US |
dc.subject |
Boophane disticha |
en_US |
dc.subject |
Cytotoxicity |
en_US |
dc.subject |
SH-SY5Y cells |
en_US |
dc.subject |
6-Hydroxycrinamine |
en_US |
dc.subject.lcsh |
Medicinal plants -- Africa, Southern |
en |
dc.title |
Cytotoxicity and acetylcholinesterase inhibitory activity of an isolated crinine alkaloid from Boophane disticha (Amaryllidaceae) |
en_US |
dc.type |
Postprint Article |
en_US |