{"title":"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","authors":"Vuyelwa Ncapayi , Oladoyin Famutimi , Thabang Calvin Lebepe , Rodney Maluleke , Sam Masha , Nande Mgedle , Sundararajan Parani , Tetsuya Kodama , Isaac Olusanjo Adewale , Oluwatobi Samuel Oluwafemi","doi":"10.1016/j.colcom.2023.100737","DOIUrl":null,"url":null,"abstract":"<div><p>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, <em>K</em><sub><em>i</em></sub>, of 15.66 μM. The IC<sub>50</sub> 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.</p></div>","PeriodicalId":10483,"journal":{"name":"Colloid and Interface Science Communications","volume":null,"pages":null},"PeriodicalIF":4.7000,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"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)\",\"authors\":\"Vuyelwa Ncapayi , Oladoyin Famutimi , Thabang Calvin Lebepe , Rodney Maluleke , Sam Masha , Nande Mgedle , Sundararajan Parani , Tetsuya Kodama , Isaac Olusanjo Adewale , Oluwatobi Samuel Oluwafemi\",\"doi\":\"10.1016/j.colcom.2023.100737\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>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, <em>K</em><sub><em>i</em></sub>, of 15.66 μM. The IC<sub>50</sub> 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.</p></div>\",\"PeriodicalId\":10483,\"journal\":{\"name\":\"Colloid and Interface Science Communications\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":4.7000,\"publicationDate\":\"2023-09-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Colloid and Interface Science Communications\",\"FirstCategoryId\":\"88\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S2215038223000444\",\"RegionNum\":3,\"RegionCategory\":\"材料科学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, PHYSICAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Colloid and Interface Science Communications","FirstCategoryId":"88","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S2215038223000444","RegionNum":3,"RegionCategory":"材料科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, PHYSICAL","Score":null,"Total":0}
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-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.
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.