Large-scale synthesis of CISe/ZnS core-shell quantum dots and its effects on the enzymatic activity of recombinant human furin (an activator of SARS-COV-2 S1/S2 spike proteins)

We herein report, for the first time, the activity of copper indium selenide/zinc sulphide core-shell quantum dots (CISe/ZnS QDs) as an inhibitor against recombinant human furin, an enzyme that has been implicated in the aetiology of many diseases, including Covid-19. The cell viability of the as-sy...

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Veröffentlicht in:Colloid and interface science communications 2023-09, Vol.56, p.100737, Article 100737
Hauptverfasser: Ncapayi, Vuyelwa, Famutimi, Oladoyin, Lebepe, Thabang Calvin, Maluleke, Rodney, Masha, Sam, Mgedle, Nande, Parani, Sundararajan, Kodama, Tetsuya, Adewale, Isaac Olusanjo, Oluwafemi, Oluwatobi Samuel
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Sprache:eng
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Zusammenfassung:We herein report, for the first time, the activity of copper indium selenide/zinc sulphide core-shell quantum dots (CISe/ZnS QDs) as an inhibitor against recombinant human furin, an enzyme that has been implicated in the aetiology of many diseases, including Covid-19. The cell viability of the as-synthesised CISe/ZnS QDs was tested against mouse colon carcinoma cells (C26), while the Furin activity was measured by hydrolysis of peptide substrate Pyr-RTKR-AMC liberating the fluorogenic 7-amino-4-methyl coumarin. The result showed that the as-synthesised stable near-infrared emitting (840 nm) CISe-ZnS QDs is biocompatible against C26 and can inhibit furin with an inhibition constant, Ki, of 15.66 μM. The IC50 was 11.29 ± 0.54 μM, while the enzymatic activity was abolished at about 23 μM of the inhibitor concentration. The results indicate the chemotherapeutic potential of CISe-ZnS QDs as an enzyme inhibitor, which may find application in managing diseases whose pathogenesis involves hyperactivity of furin. [Display omitted] •Synthesis of indium selenide/zinc sulphide core-shell quantum dots (CISe/ZnS QDs).•Recombinant human furin is an activator of SARS-COV-2 S1/S2 spike proteins.•The near-infrared emitting QDs serve as inhibitor against recombinant human furin.•The CISe-ZnS QDs inhibit furin with an inhibition constant, Ki, of 15.66 μM.•The IC50 was 11.29 ± 0.54 μM, and the binding of QDs to furin was non-competitive.
ISSN:2215-0382
2215-0382
DOI:10.1016/j.colcom.2023.100737