TY - JOUR
T1 - 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)
AU - Ncapayi, Vuyelwa
AU - Famutimi, Oladoyin
AU - Lebepe, Thabang Calvin
AU - Maluleke, Rodney
AU - Masha, Sam
AU - Mgedle, Nande
AU - Parani, Sundararajan
AU - Kodama, Tetsuya
AU - Adewale, Isaac Olusanjo
AU - Oluwafemi, Oluwatobi Samuel
N1 - Publisher Copyright:
© 2023
PY - 2023/9
Y1 - 2023/9
N2 - 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.
AB - 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.
KW - Enzyme inhibitor
KW - Furin
KW - Quantum dots
UR - http://www.scopus.com/inward/record.url?scp=85166522443&partnerID=8YFLogxK
U2 - 10.1016/j.colcom.2023.100737
DO - 10.1016/j.colcom.2023.100737
M3 - Article
AN - SCOPUS:85166522443
SN - 2215-0382
VL - 56
JO - Colloids and Interface Science Communications
JF - Colloids and Interface Science Communications
M1 - 100737
ER -