| Author | Soares, Marilia Amável Gomes | |
| Author | Aquino, Paloma Anorita de | |
| Author | Costa, Telma | |
| Author | Serpa, Carlos | |
| Author | Chaves, Otávio Augusto | |
| Access date | 2024-10-10T15:59:54Z | |
| Available date | 2024-10-10T15:59:54Z | |
| Document date | 2024 | |
| Citation | SOARES, Marilia Amável Gomes et al. Insights into the effect of glucose on the binding between human serum albumin and the nonsteroidal anti-inflammatory drug nimesulide. International Journal of Biological Macromolecules, v. 265, n. 2, p. 1-10, Apr. 2024. | |
| ISSN | 0141-8130 | |
| URI | https://www.arca.fiocruz.br/handle/icict/66444 | |
| Description | Produção científica do Laboratório de Imunofarmacologia. | pt_BR |
| Sponsorship | The authors acknowledge the Brazilian financing agencies: Fundação de Amparo à Pesquisa do Estado do Rio de Janeiro (FAPERJ), Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq), and Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) for fellowships and research grants. Additionally, the authors also acknowledge the Coimbra Chemistry Centre which is supported by the Fundação para a Ciência e a Tecnologia (FCT - Portuguese Agency for Scientific Research) through the projects UIDB/00313/2020 and UIDP/00313/2020. Otávio Augusto Chaves thanks FCT for his PhD fellowship 2020.07504.BD. | |
| Language | eng | en_US |
| Publisher | Elsevier | |
| Rights | restricted access | |
| Title | Insights into the effect of glucose on the binding between human serum albumin and the nonsteroidal anti-inflammatory drug nimesulide | en_US |
| Type | Article | |
| DOI | 10.1016/j.ijbiomac.2024.131148 | |
| Abstract | Glucose interacts with human serum albumin (HSA, the main protein responsible for the biodistribution of drugs in the bloodstream) and consequently affects the binding capacity of exogenous compounds. Thus, in this work, the interactive profile between HSA and the anti-inflammatory drug nimesulide (NMD, used mainly by patients with diabetic neuropathy to relieve acute or chronic pains) was characterized in nonglycemic, normoglycemic (80 mg/dL), and hyperglycemic (320 mg/dL) conditions by biophysics techniques. There is a spontaneous and ground-state association HSA:NMD under physiological conditions. Therefore, the Stern-Volmer constant (Kₛᵥ) can also be used to estimate the binding affinity. The Kₛᵥ values for nonglycemic, normoglycemic, and hyperglycemic conditions are around 10⁴ Mˉ¹, indicating a moderate affinity of NMD to albumin that was slightly improved by glucose levels. Additionally, the binding is enthalpically and entropically driven mainly into subdomains IIA or IIIA. The binding perturbs weakly the α-helix content of albumin, however, glucose potentially stabilizes the tertiary structure, decreasing the structural perturbation upon NMD binding and improves the complex HSA:NMD stability. Overall, the biophysical characterization indicated that glucose levels might slightly positively impact the pharmacokinetic profile of NMD, allowing NMD to achieve its therapeutical potential without affecting drastically its effective dosages. | en_US |
| Affilliation | Comissão Brasileira de Energia Nuclear. Instituto de Engenharia Nuclear. Laboratório de Nanoradiofármacos e Síntese de Novos Radiofármacos. Rio de Janeiro, RJ, Brasil. | |
| Affilliation | Universidade Federal Rural do Rio de Janeiro. Instituto de Ciências Biológicas e da Saúde. Departamento de Ciências Farmacêuticas. Seropédica, RJ, Brasil. | |
| Affilliation | Universidade de Coimbra. Faculdade de Ciências e Tecnologia. Centro de Química de Coimbra. Institute of Molecular Sciences. Departamento de Química. Coimbra, Portugal. | |
| Affilliation | Universidade de Coimbra. Faculdade de Ciências e Tecnologia. Centro de Química de Coimbra. Institute of Molecular Sciences. Departamento de Química. Coimbra, Portugal. | |
| Affilliation | Universidade de Coimbra. Faculdade de Ciências e Tecnologia. Centro de Química de Coimbra. Institute of Molecular Sciences. Departamento de Química. Coimbra, Portugal / Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Imunofarmacologia. Rio de Janeiro, RJ, Brasil / Fundação Oswaldo Cruz. Presidência. Diretoria Executiva. Centro de Pesquisa, Inovação e Vigilância em Covid-19 e Emergências Sanitárias. Rio de Janeiro, RJ, Brasil. | |
| Subject | Diabetes mellitus | en_US |
| Subject | Human serum albumin | en_US |
| Subject | Protein-drug interactions | en_US |
| e-ISSN | 1879-0003 | |
| xmlui.metadata.dc.subject.ods | 03 Saúde e Bem-Estar | |
| xmlui.metadata.dc.subject.ods | 09 Indústria, inovação e infraestrutura | |
