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)

IF 4.7 3区 材料科学 Q2 CHEMISTRY, PHYSICAL
Vuyelwa Ncapayi , Oladoyin Famutimi , Thabang Calvin Lebepe , Rodney Maluleke , Sam Masha , Nande Mgedle , Sundararajan Parani , Tetsuya Kodama , Isaac Olusanjo Adewale , Oluwatobi Samuel Oluwafemi
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Abstract

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.

Abstract Image

CISe/ZnS核壳量子点的大规模合成及其对重组人糠蛋白(S1/S2刺突蛋白激活剂)酶活性的影响
本文首次报道了硒化铜铟/硫化锌核壳量子点(CISe/ZnS QDs)作为重组人糠蛋白抑制剂的活性,该酶与包括新冠肺炎在内的许多疾病的病因有关。针对小鼠结肠癌细胞(C26)测试合成的CISe/ZnS量子点的细胞活力,同时通过肽底物Pyr RTKR AMC的水解释放荧光7-氨基-4-甲基香豆素来测量Furin活性。结果表明,合成的稳定的近红外发射(840nm)CISe-ZnS量子点对C26具有生物相容性,并能抑制弗林蛋白酶,抑制常数Ki为15.66μM。IC50为11.29±0.54μM,而在抑制剂浓度约为23μM时酶活性消失。结果表明,CISe-ZnS-QDs作为一种酶抑制剂具有化疗潜力,可用于治疗发病机制涉及弗林过动的疾病。
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来源期刊
Colloid and Interface Science Communications
Colloid and Interface Science Communications Materials Science-Materials Chemistry
CiteScore
9.40
自引率
6.70%
发文量
125
审稿时长
43 days
期刊介绍: Colloid and Interface Science Communications provides a forum for the highest visibility and rapid publication of short initial reports on new fundamental concepts, research findings, and topical applications at the forefront of the increasingly interdisciplinary area of colloid and interface science.
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