Publication
Inhibition of pancreatic α-amylase activity by a group of hydroxyxanthones
| dc.contributor.author | Santos, Clementina M.M. | |
| dc.contributor.author | Proença, Carina | |
| dc.contributor.author | Freitas, Marisa | |
| dc.contributor.author | Araújo, Alberto N. | |
| dc.contributor.author | Silva, Artur | |
| dc.contributor.author | Fernandes, Eduarda | |
| dc.date.accessioned | 2022-08-02T14:09:15Z | |
| dc.date.available | 2022-08-02T14:09:15Z | |
| dc.date.issued | 2020 | |
| dc.description.abstract | Diabetes mellitus is a non-infectious and non-transmissible life threatening disease. It is one of the fastest growing health challenges of the current century, in which the number of adults living with diabetes have more than tripled over the past 20 years. According to the International Diabetes Federation, 1 in 11 adults (20-79 years) have diabetes (463 million people) and 2 in 3 people with diabetes live in urban areas.1 This may be closely related to genetic and lifestyle factors such as physical inactivity, unhealthy diets, obesity, raised blood cholesterol and glucose, stress, etc.2 Diabetes mellitus is an endocrine disorder that occurs when pancreas does not produce enough insulin, when the body cannot use insulin efficiently or both situations, leading to chronic hyperglycemia. Thus, the control of postprandial blood glucose level via the inhibition of digestive enzymes, such as α-glucosidase and/or α-amylase, is a relevant strategy for the management of type 2 diabetes and its complications.3 During the last two decades, in the pursuit for novel antidiabetic drugs, a wide variety of natural and synthetic xanthone derivatives have been applied in the inhibition of α-glucosidase enzyme activity, however, the effects of this class of compounds on the activity of α-amylase enzyme is scarce.4 With this ratio in mind and as part of our on-going project, the aim of the present study is to investigate the effect of a series of hydroxyxanthones 1 on pancreatic α-amylase activity to find out the relevance of this group of compounds in controlling blood glucose levels for the treatment of disorders related with the carbohydrate uptake. Different concentrations of xanthones 1 were incubated with the enzyme and the hydrolysis of the substrate 2-chloro-p-nitrophenyl-α-D-maltotriose was monitored spectrophotometrically at 405 nm. Acarbose was used as the standard inhibitor. In addition, the study of the inhibition type was carried out through nonlinear regression Michaelis-Menton enzymatic kinetics and the corresponding Lineweaver-Burk plot.5 The results pointed out that the IC50 values obtained ranged from 23 to 90 μM, considerably higher than the values obtained for the positive control acarbose (IC50 = 0.62 ± 0.07 μM). For the active compounds, two of them revealed a competitive type of inhibition while for the remaining ones a noncompetitive type of inhibition was recorded. More details concerning the structureactivity relationship will be presented and discussed in this communication. | pt_PT |
| dc.description.sponsorship | This work received financial support from the European Union (FEDER funds POCI/01/0145/FEDER/007265) and National Funds (FCT/MEC, Fundação para a Ciência e Tecnologia and Ministério da Educação e Ciência) under the Partnership Agreement PT2020 UID/AGR/00690/2019; UID/QUI/50006/2019; UID/QUI/00062/2019, and “Programa Operacional Competitividade e Internacionalização” (COMPETE) (POCI-01-0145-FEDER-029241), and under the framework of QREN (NORTE-01-0145-FEDER-000024). | pt_PT |
| dc.description.version | info:eu-repo/semantics/publishedVersion | pt_PT |
| dc.identifier.citation | Santos, Clementina M.M.; Proença, Carina; Freitas, Marisa; Araújo, Alberto N.; Silva, Artur; Fernandes, Eduarda (2020). Inhibition of pancreatic α-amylase activity by a group of hydroxyxanthones. In 13th National Organic Chemistry Meeting. Aveiro | pt_PT |
| dc.identifier.uri | http://hdl.handle.net/10198/25797 | |
| dc.language.iso | eng | pt_PT |
| dc.peerreviewed | yes | pt_PT |
| dc.publisher | Sociedade Portuguesa de Química | pt_PT |
| dc.relation | Mountain Research Centre | |
| dc.relation | Associated Laboratory for Green Chemistry - Clean Technologies and Processes | |
| dc.rights.uri | http://creativecommons.org/licenses/by/4.0/ | pt_PT |
| dc.subject | Diabetes Mellitus | pt_PT |
| dc.title | Inhibition of pancreatic α-amylase activity by a group of hydroxyxanthones | pt_PT |
| dc.type | conference object | |
| dspace.entity.type | Publication | |
| oaire.awardTitle | Mountain Research Centre | |
| oaire.awardTitle | Associated Laboratory for Green Chemistry - Clean Technologies and Processes | |
| oaire.awardURI | info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UID%2FAGR%2F00690%2F2019/PT | |
| oaire.awardURI | info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UID%2FQUI%2F50006%2F2019/PT | |
| oaire.citation.conferencePlace | Aveiro | pt_PT |
| oaire.citation.endPage | 66 | pt_PT |
| oaire.citation.startPage | 66 | pt_PT |
| oaire.citation.title | 13th National Organic Chemistry Meeting/6th National Medicinal Chemistry Meeting | pt_PT |
| oaire.fundingStream | 6817 - DCRRNI ID | |
| oaire.fundingStream | 6817 - DCRRNI ID | |
| person.familyName | Santos | |
| person.givenName | Clementina M.M. | |
| person.identifier.ciencia-id | 9018-DB9C-C590 | |
| person.identifier.orcid | 0000-0003-4380-7990 | |
| person.identifier.scopus-author-id | 7201458663 | |
| project.funder.identifier | http://doi.org/10.13039/501100001871 | |
| project.funder.identifier | http://doi.org/10.13039/501100001871 | |
| project.funder.name | Fundação para a Ciência e a Tecnologia | |
| project.funder.name | Fundação para a Ciência e a Tecnologia | |
| rcaap.rights | openAccess | pt_PT |
| rcaap.type | conferenceObject | pt_PT |
| relation.isAuthorOfPublication | 64f662b6-775d-4ea0-bfd7-f527af0ac1a0 | |
| relation.isAuthorOfPublication.latestForDiscovery | 64f662b6-775d-4ea0-bfd7-f527af0ac1a0 | |
| relation.isProjectOfPublication | d6683ba1-d253-48e4-968e-35106ce7b750 | |
| relation.isProjectOfPublication | a8b5499f-df63-4561-a825-05c4eca80d9a | |
| relation.isProjectOfPublication.latestForDiscovery | a8b5499f-df63-4561-a825-05c4eca80d9a |