Insights into tyrosinase inhibition by compounds isolated from Greyia radlkoferi Szyszyl using biological activity, molecular docing and gene expression analysis

dc.contributor.authorLall, Namrita
dc.contributor.authorMogapi, Elizabeth
dc.contributor.authorDe Canha, Marco Nuno
dc.contributor.authorCrampton, Bridget Genevieve
dc.contributor.authorNqephe, Mabatho
dc.contributor.authorHussein, Ahmed A.
dc.contributor.authorKumar, Vivek
dc.contributor.emailnamrita.lall@up.ac.zaen
dc.date.accessioned2017-05-30T07:20:06Z
dc.date.issued2016-11en
dc.description.abstractGreyia radlkoferi ethanol extract and its five compounds were tested for their inhibitory activity against the mushroom tyrosinase enzyme and melanin production on melanocytes. The crude extract showed significant tyrosinase inhibition with IC50 of 17.96 μg/ml. This is the first report of the isolation of these 5 compounds from Greyia radlkoferi. 2',4',6'-Trihydroxydihydrochalcone showed the highest tyrosinase inhibition at 17.70 μg/ml (68.48 μM), with low toxicity when compared with crude extract. This compound is therefore, a key component in the crude extract, which is responsible for tyrosinase inhibitory activity. The RT-qPCR indicated that the mechanism of action is most likely post transcriptional. Further, the molecular docking study showed that tyrosinase inhibitory activity depends on interaction of the compound with Cu2+ ions at the active site. This is the first report of the tyrosinase inhibitory activity of the G. radlkoferi extract and molecular insights on interaction of its compounds with Cu2+ ions as the driving factor for tyrosinase inhibition. These results suggest that the extract of G. radlkoferi and the compound 2',4',6'-trihydroxydihydrochalcone have great potential to be further developed as pharmaceutical or cosmetic agents for use against dermatological disorders associated with melanin.en_ZA
dc.description.departmentPlant Scienceen
dc.description.departmentChemistryen
dc.description.embargo2017-11-30
dc.description.sponsorshipThe National Research Foundation [Grant 90355] and the Department of Science and Technology [Grant 0024/2015].en
dc.description.urihttp://www.elsevier.com/locate/bmcen
dc.identifier.citationLall, N., Mogapi, E., De Canha, M.N., Crampton, B.G., Nqephe, M., Hussein, A.A. & Kumar, V. 2016, 'Insights into tyrosinase inhibition by compounds isolated from Greyia radlkoferi Szyszyl using biological activity, molecular docing and gene expression analysis', Bioorganic and Medicinal Chemistry, vol. 24, no. 22, pp. 5953-5959.en
dc.identifier.issn1464-3391 (online)en
dc.identifier.issn0968-0896 (print)en
dc.identifier.other10.1016/j.bmc.2016.09.054en
dc.identifier.urihttp://hdl.handle.net/2263/60696
dc.language.isoEnglishen
dc.publisherElsevieren
dc.rights© 2016 Published by Elsevier Ltd. All rights reserved. Notice : this is the author's version of a work that was accepted for publication in Bioorganic and Medicinal Chemistry. 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. A definitive version was subsequently published in Bioorganic and Medicinal Chemistry, vol. 24, no. 22, pp. 5953-5959, 2016. doi : 10.1016/j.bmc.2016.09.054.en
dc.subjectGreyia radlkoferien
dc.subjectTyrosinaseen
dc.subjectHyper-pigmentationen
dc.subjectMelanin inhibitionen
dc.subjectGene expressionen
dc.subjectMolecular dockingen
dc.titleInsights into tyrosinase inhibition by compounds isolated from Greyia radlkoferi Szyszyl using biological activity, molecular docing and gene expression analysisen
dc.typePostprint Articleen

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