Testing for novel inhibitors of periodontitis-associated sialidases

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dc.contributor.authorGalleh, Raphael Peter
dc.contributor.authorLambert, D.W.
dc.contributor.authorStafford, G.P.
dc.date.accessioned2023-12-14T07:43:30Z
dc.date.available2023-12-14T07:43:30Z
dc.date.issued2020-07-10
dc.description.abstractThe microorganisms associated with severe periodontitis are the periodontal pathogens of the red complex: Porphyromonas gingivalis, Tannerella forsythia and Treponema denticola. These organisms cleave sialic acids found at the terminal end of host glycoconjugates by hydrolysing the glycosidic linkages with their expressed sialidases, thereby affecting the integrity of the host periodontium and promoting disease progression. Both p. gingivalis (SiaPG) and T. forsythia (NanH) sialidase enzymes were purified using HisTag affinity chromatography and a range of putative synthetic and plant-based inhibitors were tested for their ability to inhibit both enzymes using a ٨لا٨لالا ٧ cleavage assay. Investigation of sialidase inhibitory activity of these compounds revealed that the plant derived alkaloids: Epicatechin gallate (IC50 = 21.75pM and 1 20.9pM) and Berberine chloride (IC50 = 106.2pM and 1 25.5pM) were more effective inhibitors of both SiaPg and NanH enzymes than the anti-influenza drug Zanamivir, an FDA approved viral neuraminidase inhibitor. Finally, a range of newly synthesized sialic acid analogues were effective in the micromolar to nanomolar range against both SiaPg and NanH enzymes with compound 2e3aDFNeu5Ac9N3 having an IC50 of (3.846pM and . ا م) respectively. The data suggests several novel inhibitors of these enzymes that might have future use as novel drugs against diseases such as periodontitis, and which we are currently testing further in host-pathogen interaction studies.en_US
dc.identifier.citationGalleh, R.P. et al. (2020)Testing for novel inhibitors of periodontitis-associated sialidasesen_US
dc.identifier.urihttps://keffi.nsuk.edu.ng/handle/20.500.14448/5944
dc.language.isoenen_US
dc.publisherDepartment of Microbiology, Nasarawa State University Keffien_US
dc.titleTesting for novel inhibitors of periodontitis-associated sialidasesen_US
dc.typeArticleen_US

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