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dc.contributor.authorFayyaz, Sharmeen
dc.contributor.authorShaikh, Muniza
dc.contributor.authorGasperini, Danila
dc.contributor.authorNolan, Steven Patrick
dc.contributor.authorSmith, Andrew David
dc.contributor.authorChoudhary, M. Iqbal
dc.date.accessioned2022-05-11T23:50:50Z
dc.date.available2022-05-11T23:50:50Z
dc.date.issued2021-05-12
dc.identifier274298466
dc.identifier2fdb838f-de5e-4f33-bce3-56131b8968da
dc.identifier85107162819
dc.identifier000674454000007
dc.identifier.citationFayyaz , S , Shaikh , M , Gasperini , D , Nolan , S P , Smith , A D & Choudhary , M I 2021 , ' In vitro and in cellulo anti-diabetic activity of Au I - and Au III -isothiourea complexes ' , Inorganic Chemistry Communications , vol. In press , 108666 . https://doi.org/10.1016/j.inoche.2021.108666en
dc.identifier.issn1387-7003
dc.identifier.otherORCID: /0000-0002-2104-7313/work/94669170
dc.identifier.urihttps://hdl.handle.net/10023/25345
dc.descriptionAuthors are grateful to the Higher Education Commission (HEC), Pakistan, for providing financial support under the Indigenous Ph. D. Fellowship for 5000 Scholars Phase-II program for providing financial support.en
dc.description.abstractAbout 100 million people worldwide have type II diabetes (T2D), making it one of the most common metabolic disease. DPP-IV inhibitors are new class of anti-diabetic drug. Gold complexes are known for diverse biological activities. Considering these precedents, and growing interest in developing metal-based enzyme inhibitors, we report here the dipeptidyl peptidase-IV (DPP-IV) inhibitory potential of cationic, and neutral chiral gold (I), and gold (III) isothiourea complexes. Colorimetric assay with recombinant DPP-IV enzyme was employed for initial screening. Kinetic based mechanistic studies were also performed for most active complexes. Efficiency of identified inhibitors in biological environment was assessed in in cellulo assay, using Caco-2 cell line. These complexes showed a good to moderate inhibition of DPP-IV with IC50 values in the range of 22.0 – 99.0 µM, as compared to standard inhibitor, sitagliptin (IC50 = 0.033 ± 0.04 µM). It was observed that steric, and electronic properties of the isothiourea ligands have profound effect on the DPP-IV inhibitory activity of these complexes. To the best of our knowledge this study reports for the first time isothiourea based gold complexes as inhibitors of DPP-IV enzyme. These results thus provide an approach for exploring new insights into the development of effective agents against diabetes using incretin-based therapy.
dc.format.extent898269
dc.language.isoeng
dc.relation.ispartofInorganic Chemistry Communicationsen
dc.subjectGold complexesen
dc.subjectDipeptidyl peptdase-IVen
dc.subjectDiabetes type 2en
dc.subjectCaco-2 cellsen
dc.subjectIsothioureaen
dc.subjectBioinorganic chemistryen
dc.subjectQD Chemistryen
dc.subjectE-NDASen
dc.subjectSDG 3 - Good Health and Well-beingen
dc.subject.lccQDen
dc.titleIn vitro and in cellulo anti-diabetic activity of AuI- and AuIII-isothiourea complexesen
dc.typeJournal articleen
dc.contributor.institutionUniversity of St Andrews. School of Chemistryen
dc.identifier.doi10.1016/j.inoche.2021.108666
dc.description.statusPeer revieweden
dc.date.embargoedUntil2022-05-12


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