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[PMID]:28455256
[Au] Autor:Kim JH; Cho CW; Kim HY; Kim KT; Choi GS; Kim HH; Cho IS; Kwon SJ; Choi SK; Yoon JY; Yang SY; Kang JS; Kim YH
[Ad] Endereço:College of Pharmacy, Chungnam National University, Daejeon 34134, Republic of Korea; Department of Horticultural and Crop Environment, National Institute of Horticultural and Herbal Science, RDA, Wanju, 55365, Republic of Korea; Advanced Radiation Technology Institute, Korea Atomic Energy Research I
[Ti] Título:α-Glucosidase inhibition by prenylated and lavandulyl compounds from Sophora flavescens roots and in silico analysis.
[So] Source:Int J Biol Macromol;102:960-969, 2017 Sep.
[Is] ISSN:1879-0003
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The enzyme α-glucosidase is a good drug target for the treatment of diabetes mellitus. Four minor flavonoids (1-4) from roots of Sophora flavescens showed the inhibitory activity, with IC values ranging from 11.0±0.3 to 50.6±1.3µM, toward α-glucosidase. An enzyme kinetics analysis of them revealed that the compounds 1 and 4 were non-competitive, and compounds 2 and 3 were un-competitive inhibitors. For molecular docking, 3-dimensional structure of α-glucosidase was built by homology modeling. As the result, four compounds 1-4 were confirmed to interact into common binding site of α-glucosidase. In addition, all of the four prenylated and lavandulyl compounds (1-4) were abundant in an ethyl acetate fraction separated from a methanol extract, and the potential inhibitor (3) was extracted best using tetrahydrofuran.
[Mh] Termos MeSH primário: Simulação por Computador
Extratos Vegetais/farmacologia
Raízes de Plantas/química
Prenilação
Sophora/química
Terpenos/química
alfa-Glucosidases/metabolismo
[Mh] Termos MeSH secundário: Sequência de Aminoácidos
Inibidores de Glicosídeo Hidrolases/química
Inibidores de Glicosídeo Hidrolases/metabolismo
Inibidores de Glicosídeo Hidrolases/farmacologia
Simulação de Acoplamento Molecular
Extratos Vegetais/química
Extratos Vegetais/metabolismo
Conformação Proteica
alfa-Glucosidases/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Glycoside Hydrolase Inhibitors); 0 (Plant Extracts); 0 (Terpenes); EC 3.2.1.20 (alpha-Glucosidases)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170430
[St] Status:MEDLINE


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[PMID]:28521570
[Au] Autor:Li M; Wu X; Wang X; Shen T; Ren D
[Ad] Endereço:a Department of Natural Product Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences , Shandong University , Jinan , P. R. China.
[Ti] Título:Two novel compounds from the root bark of Morus alba L.
[So] Source:Nat Prod Res;32(1):36-42, 2018 Jan.
[Is] ISSN:1478-6427
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Chemical investigation of the root bark of Morus alba led to the isolation of a new flavone, dioxycudraflavone A (1) and a new 2-arylbenzofuran, 5-hydroxyethyl moracin M (2), together with seven known compounds namely sanggenon V (3), morusin (4), morusignin L (5), licoflavone C (6), moracin C (7), alfafuran (8) and mulberrofuran G (9). The structure elucidation of these compounds was based on analyses of spectroscopic data including 1D, 2D NMR and HR-ESI-MS. All compounds were evaluated for the α-glucosidase inhibitory and cytotoxic activities. Compounds 2-4, 8 and 9 exhibited strong α-glucosidase inhibitory activities with IC less than 10 µM, while only 4 and 9 showed moderate cytotoxic effects against lung cancer cells.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Benzofuranos/farmacologia
Flavonas/farmacologia
Inibidores de Glicosídeo Hidrolases/farmacologia
Morus/química
[Mh] Termos MeSH secundário: Células A549
Antineoplásicos/química
Benzofuranos/química
Flavonas/química
Flavonoides/química
Flavonoides/farmacologia
Inibidores de Glicosídeo Hidrolases/química
Seres Humanos
Espectroscopia de Ressonância Magnética
Estrutura Molecular
Casca de Planta/química
Espectrometria de Massas por Ionização por Electrospray
Estilbenos/química
Estilbenos/farmacologia
Terpenos/química
Terpenos/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Benzofurans); 0 (Flavones); 0 (Flavonoids); 0 (Glycoside Hydrolase Inhibitors); 0 (Stilbenes); 0 (Terpenes); 0 (licoflavone C); 0 (moracin C); 62596-29-6 (morusin); 87085-00-5 (mulberrofuran G)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180301
[Lr] Data última revisão:
180301
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170520
[St] Status:MEDLINE
[do] DOI:10.1080/14786419.2017.1327862


  3 / 2143 MEDLINE  
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[PMID]:29295712
[Au] Autor:Ovais M; Ayaz M; Khalil AT; Shah SA; Jan MS; Raza A; Shahid M; Shinwari ZK
[Ad] Endereço:Department of Biotechnology, Quaid-i-Azam University, Islamabad, 44000, Pakistan.
[Ti] Título:HPLC-DAD finger printing, antioxidant, cholinesterase, and α-glucosidase inhibitory potentials of a novel plant Olax nana.
[So] Source:BMC Complement Altern Med;18(1):1, 2018 Jan 03.
[Is] ISSN:1472-6882
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The medicinal importance of a novel plant Olax nana Wall. ex Benth. (family: Olacaceae) was revealed for the first time via HPLC-DAD finger printing, qualitative phytochemical analysis, antioxidant, cholinesterase, and α-glucosidase inhibitory assays. METHODS: The crude methanolic extract of O. nana (ON-Cr) was subjected to qualitative phytochemical analysis and HPLC-DAD finger printing. The antioxidant potential of ON-Cr was assessed via 1,1-diphenyl,2-picrylhydrazyl (DPPH), 2,2-azinobis[3-ethylbenzthiazoline]-6-sulfonic acid (ABTS) and hydrogen peroxide (H O ) free radical scavenging assays. Furthermore, acetylcholinesterase (AChE) & butyrylcholinesterase (BChE) inhibitory activities were performed using Ellman's assay, while α- glucosidase inhibitory assay was carried out using a standard protocol. RESULTS: The qualitative phytochemical analysis of ON-Cr revealed the presence of secondary metabolites like alkaloids, flavonoids, tannins, sterols, saponins and terpenoids. The HPLC-DAD finger printing revealed the presence of 40 potential compounds in ON-Cr. Considerable anti-radical activities was revealed by ON-Cr in the DPPH, ABTS and H O free radical scavenging assays with IC values of 71.46, 72.55 and 92.33 µg/mL, respectively. Furthermore, ON-Cr showed potent AChE and BChE inhibitory potentials as indicated by their IC values of 33.2 and 55.36 µg/mL, respectively. In the α-glucosidase inhibition assay, ON-Cr exhibited moderate inhibitory propensity with an IC value of 639.89 µg/mL. CONCLUSIONS: This study investigated Olax nana for the first time for detailed qualitative phytochemical tests, HPLC-DAD finger printing analysis, antioxidant, anticholinesterase and α-glucosidase inhibition assays. The antioxidant and cholinesterase inhibitory results were considerable and can provide scientific basis for further studies on the neuroprotective and anti-Alzheimer's potentials of this plant. ON-Cr may further be subjected to fractionation and polarity guided fractionation to narrow down the search for isolation of bioactive compounds.
[Mh] Termos MeSH primário: Antioxidantes/análise
Inibidores da Colinesterase/análise
Cromatografia Líquida de Alta Pressão/métodos
Inibidores de Glicosídeo Hidrolases/análise
Olacaceae/química
Extratos Vegetais/análise
[Mh] Termos MeSH secundário: Antioxidantes/química
Antioxidantes/metabolismo
Benzotiazóis/análise
Benzotiazóis/metabolismo
Compostos de Bifenilo/análise
Compostos de Bifenilo/metabolismo
Inibidores da Colinesterase/química
Inibidores da Colinesterase/metabolismo
Inibidores de Glicosídeo Hidrolases/química
Inibidores de Glicosídeo Hidrolases/metabolismo
Peróxido de Hidrogênio/análise
Peróxido de Hidrogênio/metabolismo
Picratos/análise
Picratos/metabolismo
Extratos Vegetais/química
Extratos Vegetais/metabolismo
Ácidos Sulfônicos/análise
Ácidos Sulfônicos/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Benzothiazoles); 0 (Biphenyl Compounds); 0 (Cholinesterase Inhibitors); 0 (Glycoside Hydrolase Inhibitors); 0 (Picrates); 0 (Plant Extracts); 0 (Sulfonic Acids); 28752-68-3 (2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid); BBX060AN9V (Hydrogen Peroxide); DFD3H4VGDH (1,1-diphenyl-2-picrylhydrazyl)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180216
[Lr] Data última revisão:
180216
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180104
[St] Status:MEDLINE
[do] DOI:10.1186/s12906-017-2057-9


  4 / 2143 MEDLINE  
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[PMID]:29208524
[Au] Autor:Wang G; Chen M; Qiu J; Xie Z; Cao A
[Ad] Endereço:Provincial Key Laboratory of Pharmaceutics in Guizhou Province, Guizhou Medical University, 4 Beijing Road, Guiyang 550004, China; School of Pharmacy, Guizhou Medical University, 4 Beijing Road, Guiyang 550004, China; National Engineering Research Center of Miao's Medicines, 4 Beijing Road, Guiyang
[Ti] Título:Synthesis, in vitro α-glucosidase inhibitory activity and docking studies of novel chromone-isatin derivatives.
[So] Source:Bioorg Med Chem Lett;28(2):113-116, 2018 01 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A novel series of chromone-isatin derivatives 6a-6p were designed, synthesized and characterized by H NMR, C NMR and HRMS. These novel synthetic compounds were evaluated for inhibitory activity against yeast α-glucosidase enzyme. The results of biological test have shown that all tested compounds exhibited excellent to potent inhibitory activity in the range of IC = 3.18 ±â€¯0.12-16.59 ±â€¯0.17 µM as compared to the standard drug acarbose (IC = 817.38 ±â€¯6.27 µM). Compound 6j (IC = 3.18 ±â€¯0.12 µM) with a hydroxyl group at the 7-position of chromone and a 4-bromobenzyl group at the N1-positions of isatin, was found to be the most active compound among the series. Furthermore, molecular docking study was performed to help understand binding interactions of the most active analogs with α-glucosidase enzyme. These results indicated that this class of compounds had potential for the development of anti-diabetic agents.
[Mh] Termos MeSH primário: Cromonas/farmacologia
Inibidores de Glicosídeo Hidrolases/farmacologia
Isatina/farmacologia
Simulação de Acoplamento Molecular
alfa-Glucosidases/metabolismo
[Mh] Termos MeSH secundário: Cromonas/química
Relação Dose-Resposta a Droga
Inibidores de Glicosídeo Hidrolases/síntese química
Inibidores de Glicosídeo Hidrolases/química
Isatina/química
Estrutura Molecular
Saccharomyces cerevisiae/enzimologia
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Chromones); 0 (Glycoside Hydrolase Inhibitors); 82X95S7M06 (Isatin); EC 3.2.1.20 (alpha-Glucosidases)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180216
[Lr] Data última revisão:
180216
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171207
[St] Status:MEDLINE


  5 / 2143 MEDLINE  
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[PMID]:29210296
[Au] Autor:Zhu LJ; Yi S; Li X; Chen HF; Ming M; Zhang X; Yao XS
[Ad] Endereço:a Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, School of Traditional Chinese Materia Medica , Shenyang Pharmaceutical University , Shenyang 110016 , China.
[Ti] Título:C-glycosides from the stems of Calophyllum membranaceum.
[So] Source:J Asian Nat Prod Res;20(1):49-54, 2018 Jan.
[Is] ISSN:1477-2213
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Three new C-glycosides, calophymembransides D-F (1-3), were isolated from the stems of Calophyllum membranaceum Gardn. et Champ.. The structures were assigned on the basis of spectroscopic data. RXRα transcriptional inhibition and α-glucosidase inhibition assays indicated that all the isolates were inactive.
[Mh] Termos MeSH primário: Calophyllum/química
Inibidores de Glicosídeo Hidrolases/farmacologia
Monossacarídeos/isolamento & purificação
[Mh] Termos MeSH secundário: Inibidores de Glicosídeo Hidrolases/química
Inibidores de Glicosídeo Hidrolases/isolamento & purificação
Estrutura Molecular
Monossacarídeos/química
Caules de Planta/química
alfa-Glucosidases/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (C-glycoside); 0 (Glycoside Hydrolase Inhibitors); 0 (Monosaccharides); EC 3.2.1.20 (alpha-Glucosidases)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180202
[Lr] Data última revisão:
180202
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171207
[St] Status:MEDLINE
[do] DOI:10.1080/10286020.2017.1409734


  6 / 2143 MEDLINE  
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[PMID]:29210299
[Au] Autor:Czarnecka K; Girek M; Maciejewska K; Skibinski R; Jonczyk J; Bajda M; Kabzinski J; Solowiej P; Majsterek I; Szymanski P
[Ad] Endereço:a Department of Pharmaceutical Chemistry, Drug Analyses and Radiopharmacy, Faculty of Pharmacy , Medical University of Lodz , Lodz , Poland.
[Ti] Título:New cyclopentaquinoline hybrids with multifunctional capacities for the treatment of Alzheimer's disease.
[So] Source:J Enzyme Inhib Med Chem;33(1):158-170, 2017 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Alzheimer's disease (AD) is the most common progressive form of brain neurodegeneration and the most prevailing cause of dementia. Unfortunately, the aetiology of AD is not completely studied but different factors are associated with the development of AD such as among others low level of acetylcholine, aggregation of ß-amyloid (Aß), hyperphosphorylated tau protein, oxidative stress, and inflammation. The study encompass organic syntheses of 2,3-dihydro-1H-cyclopenta[b]quinoline with 5,6-dichloronicotinic acid and suitable linkers derivatives as multifunctional agents for AD treatment. Afterwards self-induced amyloid beta aggregation, inhibition studies of acetylcholinesterase and butyrylcholinesterase and molecular docking studies were performed. The results showed that 3b compound exhibited the best acetylcholinesterase inhibitory activity, with IC value of 0.052 µM which is lower compared to references. Besides, all synthesised compounds showed good butyrylcholinesterase inhibitory activity with IC values from 0.071 to 0.797 µM. Compound 3b exhibited strong Aß aggregation inhibitory effect with 25.7% at 5 µM to 92.8% at 100 µM as well as good anti-inflammatory effect. Thus, new compounds could create new perspectives for further development as a multi-target-directed agent for AD treatment.
[Mh] Termos MeSH primário: Acetilcolinesterase/metabolismo
Doença de Alzheimer/tratamento farmacológico
Aminoquinolinas/farmacologia
Butirilcolinesterase/metabolismo
Inibidores da Colinesterase/farmacologia
Inibidores de Glicosídeo Hidrolases/farmacologia
Hialuronoglucosaminidase/antagonistas & inibidores
Niacinamida/análogos & derivados
[Mh] Termos MeSH secundário: Doença de Alzheimer/metabolismo
Aminoquinolinas/síntese química
Aminoquinolinas/química
Peptídeos beta-Amiloides/antagonistas & inibidores
Peptídeos beta-Amiloides/metabolismo
Animais
Proliferação Celular/efeitos dos fármacos
Inibidores da Colinesterase/síntese química
Inibidores da Colinesterase/química
Relação Dose-Resposta a Droga
Enguias
Inibidores de Glicosídeo Hidrolases/síntese química
Inibidores de Glicosídeo Hidrolases/química
Cavalos
Seres Humanos
Hialuronoglucosaminidase/metabolismo
Modelos Moleculares
Estrutura Molecular
Niacinamida/síntese química
Niacinamida/química
Niacinamida/farmacologia
Fragmentos de Peptídeos/antagonistas & inibidores
Fragmentos de Peptídeos/metabolismo
Agregados Proteicos/efeitos dos fármacos
Relação Estrutura-Atividade
Células Tumorais Cultivadas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (5,6-dichloro-N-(3-(2,3-dihydro-1H-cyclopenta(b)quinolin-9-ylamino)propyl)nicotinamide); 0 (Aminoquinolines); 0 (Amyloid beta-Peptides); 0 (Cholinesterase Inhibitors); 0 (Glycoside Hydrolase Inhibitors); 0 (Peptide Fragments); 0 (Protein Aggregates); 0 (amyloid beta-protein (1-42)); 25X51I8RD4 (Niacinamide); EC 3.1.1.7 (Acetylcholinesterase); EC 3.1.1.8 (Butyrylcholinesterase); EC 3.2.1.35 (Hyaluronoglucosaminidase)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171219
[Lr] Data última revisão:
171219
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171207
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2017.1406485


  7 / 2143 MEDLINE  
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[PMID]:28745232
[Au] Autor:Khan MA; Javaid K; Wadood A; Jamal A; Batool F; Fazal-Ur-Rehman S; Basha FZ; Choudhary MI
[Ad] Endereço:H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270. Pakistan.
[Ti] Título:In vitro α-Glucosidase Inhibition by Non-sugar based Triazoles of Dibenzoazepine, their Structure-Activity Relationship, and Molecular Docking.
[So] Source:Med Chem;13(7):698-704, 2017.
[Is] ISSN:1875-6638
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: α-Glucosidase inhibitors (AGIs) have been reported for their clinical potential against postprandial hyperglycemia, which is responsible for the risks associated with diabetes mellitus 2 and cardiovascular diseases (CVDs). Besides, a number of compounds have been reported as potent AGIs, several side effects are associated with them. METHODS: The aim of present work is to explore new and potent molecules as AGIs. Therefore, a library of dibenzoazepine linked triazoles (1-15) was studied for their in vitro α-glucosidase inhibitory activity. The binding modes of potent compounds in the active site of α-glucosidase enzyme were also explored through molecular docking studies. RESULTS AND CONCLUSION: Among the reported triazoles, compounds 3-9, 11, and 13 (IC50 = 6.0 ± 0.03 to 19.8 ± 0.28 µM) were found to be several fold more active than the standard drug acarbose (IC50 = 840 ± 1.73 µM). Compound 5 (IC50 = 6.0 ± 0.03 µM) was the most potent AGIs in the series, about 77- fold more active than acarbose. Therefore, dibenzoazepine linked-triazoles described here can serve as leads for further studies as new non-sugar AGIs.
[Mh] Termos MeSH primário: Dibenzazepinas/farmacologia
Inibidores de Glicosídeo Hidrolases/farmacologia
Triazóis/farmacologia
alfa-Glucosidases/metabolismo
[Mh] Termos MeSH secundário: Acarbose/farmacologia
Domínio Catalítico
Dibenzazepinas/síntese química
Inibidores de Glicosídeo Hidrolases/síntese química
Simulação de Acoplamento Molecular
Saccharomyces cerevisiae/enzimologia
Relação Estrutura-Atividade
Triazóis/síntese química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Dibenzazepines); 0 (Glycoside Hydrolase Inhibitors); 0 (Triazoles); EC 3.2.1.20 (alpha-Glucosidases); T58MSI464G (Acarbose)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171205
[Lr] Data última revisão:
171205
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170727
[St] Status:MEDLINE
[do] DOI:10.2174/1573406413666170726142949


  8 / 2143 MEDLINE  
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[PMID]:28749197
[Au] Autor:Yandrapalli S; Jolly G; Horblitt A; Sanaani A; Aronow WS
[Ad] Endereço:a Cardiology Division, Department of Medicine , Westchester Medical Center /New York Medical College , Valhalla , NY , USA.
[Ti] Título:Cardiovascular benefits and safety of non-insulin medications used in the treatment of type 2 diabetes mellitus.
[So] Source:Postgrad Med;129(8):811-821, 2017 Nov.
[Is] ISSN:1941-9260
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Diabetes mellitus is a growing in exponential proportions. If the current growth trend continues, it may result in every third adult in the United States having diabetes mellitus by 2050, and every 10 adult worldwide. Type 2 diabetes mellitus (T2DM) confers a 2- to 3-fold increased risk of cardiovascular (CV) events compared with non-diabetic patients, and CV mortality is responsible for around 80% mortality in this population. Patients with T2DM can have other features of insulin resistance-metabolic syndrome like hypertension, lipid abnormalities, and obesity which are all associated with increased CV disease and stroke risk even in the absence of T2DM. The management of a T2DM calls for employing a holistic risk factor control approach. Metformin is the first line therapy for T2DM and has been shown to have cardiovascular beneficial effects. Intense debate regarding the risk of myocardial infarction with rosiglitazone led to regulatory agencies necessitating cardiovascular outcome trials with upcoming anti-diabetic medications. Glucagon like peptide-1 agonists and sodium glucose co-transporter-2 inhibitors have shown promising CV safety and additional CV benefit in recent clinical trials. These drugs have favorable effects on traditional CV risk factors. The findings from these studies further support that fact that CV risk factor control plays an important role in reducing morbidity and mortality in T2DM patients. This review article will discuss briefly the cardiovascular safety and benefits of the oral medications which are currently being used for T2DM and will then discuss in detail about the newer medications being investigated for the treatment of T2DM.
[Mh] Termos MeSH primário: Doenças Cardiovasculares/etiologia
Doenças Cardiovasculares/prevenção & controle
Diabetes Mellitus Tipo 2/complicações
Diabetes Mellitus Tipo 2/tratamento farmacológico
Hipoglicemiantes/uso terapêutico
[Mh] Termos MeSH secundário: Benzamidas/uso terapêutico
Angiopatias Diabéticas/prevenção & controle
Inibidores da Dipeptidil Peptidase IV/uso terapêutico
Receptor do Peptídeo Semelhante ao Glucagon 1/agonistas
Inibidores de Glicosídeo Hidrolases/uso terapêutico
Seres Humanos
Hipoglicemiantes/administração & dosagem
Hipoglicemiantes/efeitos adversos
Metformina/uso terapêutico
Ensaios Clínicos Controlados Aleatórios como Assunto
Fatores de Risco
Transportador 2 de Glucose-Sódio/antagonistas & inibidores
Compostos de Sulfonilureia/uso terapêutico
Tiazolidinedionas/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Benzamides); 0 (Dipeptidyl-Peptidase IV Inhibitors); 0 (Glucagon-Like Peptide-1 Receptor); 0 (Glycoside Hydrolase Inhibitors); 0 (Hypoglycemic Agents); 0 (Sodium-Glucose Transporter 2); 0 (Sulfonylurea Compounds); 0 (Thiazolidinediones); 8V6OK1I088 (meglitinide); 9100L32L2N (Metformin)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171128
[Lr] Data última revisão:
171128
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170728
[St] Status:MEDLINE
[do] DOI:10.1080/00325481.2017.1358064


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[PMID]:29068991
[Au] Autor:Chu WM; Ho HE; Huang KH; Tsan YT; Liou YS; Wang YH; Lee MC; Li YC
[Ad] Endereço:aInstitute of Medicine, Chung Shan Medical University, Taichung bDepartment of Family Medicine, Taichung Veterans General Hospital, Chiayi Branch, Chiayi cSchool of Medicine, National Yang-Ming University, Taipei dDepartment of Family Medicine, Taichung Armed Force General Hospital, Taichung eSchool of Medicine, National Defense Medical Center, Taipei fDepartment of Health Service Administration, College of Public Health, China Medical University gDivision of Occupational Medicine, Department of Emergency Medicine, Taichung Veterans General Hospital hSchool of Medicine, Chung Shan Medical University, Taichung iSchool of Public Health, National Defense Medical Center, Taipei jDepartment of Family Medicine, Taichung Veterans General Hospital kDepartment of Family Medicine, Taichung Hospital, Ministry of Health and Welfare, Taichung lInstitute of Population Sciences, National Health Research Institutes, Miaoli County mCollege of Management, Chao-Yung University of Technology nDepartment of Public Health, China Medical University, Taichung oDepartment of Family Medicine, Yuan Rung Hospital, Yuanlin, Changhwa, Taiwan.
[Ti] Título:The prescribing trend of oral antidiabetic agents for type 2 diabetes in Taiwan: An 8-year population-based study.
[So] Source:Medicine (Baltimore);96(43):e8257, 2017 Oct.
[Is] ISSN:1536-5964
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The purpose of this study was to evaluate the prescription trend and pattern of oral antidiabetic (OAD) medications, which are extensively used worldwide for treating type 2 diabetes, in 2 age groups.In this population-based study, data obtained from the National Health Insurance Research Database, Taiwan, were analyzed to investigate the prescription trend of all types of OAD medications during 2005 to 2012. We used descriptive statistics to demonstrate the trend of prescription patterns stratified by age (aged 65 years and above or younger than 65).Sulfonylurea (SU) was once the most commonly used drug, but the proportion of its prescription had declined gradually (76.83% in 2005 to 63.70% in 2012). Consequently, biguanide (BG) became the most commonly used drug since 2010 (64.31% in 2005 to 74.41% in 2012). In addition, the prescriptions of thiazolidinedione decreased significantly (9.20% in 2005 to 2.86% in 2012), whereas the usage of DPP-4 inhibitor increased with time (3.73% in 2009 to 19.64% in 2012). The treatment choice of SU and α-glucosidase inhibitor (AGI) was higher in elderly patients compared with the younger population (SU: 62.70% in 2012, AGI: 12.78% in 2012). Two-drug combination therapies were the prevalent treatment choices for patients with type 2 diabetes (44.77% in 2012), particularly in the elderly group; however, ≥3 drug combination therapies increased gradually during the study period, particularly in the younger group.This descriptive study presents the change in the prescription of OAD medication for different age groups during 2005 to 2012.
[Mh] Termos MeSH primário: Diabetes Mellitus Tipo 2/tratamento farmacológico
Hipoglicemiantes/uso terapêutico
Padrões de Prática Médica/estatística & dados numéricos
[Mh] Termos MeSH secundário: Administração Oral
Fatores Etários
Idoso
Biguanidas/uso terapêutico
Inibidores da Dipeptidil Peptidase IV/uso terapêutico
Quimioterapia Combinada
Inibidores de Glicosídeo Hidrolases/uso terapêutico
Seres Humanos
Meia-Idade
Compostos de Sulfonilureia/uso terapêutico
Taiwan
Tiazolidinedionas/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; OBSERVATIONAL STUDY
[Nm] Nome de substância:
0 (Biguanides); 0 (Dipeptidyl-Peptidase IV Inhibitors); 0 (Glycoside Hydrolase Inhibitors); 0 (Hypoglycemic Agents); 0 (Sulfonylurea Compounds); 0 (Thiazolidinediones); AA68LXK93C (2,4-thiazolidinedione)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171123
[Lr] Data última revisão:
171123
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:171026
[St] Status:MEDLINE
[do] DOI:10.1097/MD.0000000000008257


  10 / 2143 MEDLINE  
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[PMID]:28933564
[Au] Autor:Proença C; Freitas M; Ribeiro D; Oliveira EFT; Sousa JLC; Tomé SM; Ramos MJ; Silva AMS; Fernandes PA; Fernandes E
[Ad] Endereço:a UCIBIO, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy , University of Porto , Porto , Portugal.
[Ti] Título:α-Glucosidase inhibition by flavonoids: an in vitro and in silico structure-activity relationship study.
[So] Source:J Enzyme Inhib Med Chem;32(1):1216-1228, 2017 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:α-Glucosidase inhibitors are described as the most effective in reducing post-prandial hyperglycaemia (PPHG) from all available anti-diabetic drugs used in the management of type 2 diabetes mellitus. As flavonoids are promising modulators of this enzyme's activity, a panel of 44 flavonoids, organised in five groups, was screened for their inhibitory activity of α-glucosidase, based on in vitro structure-activity relationship studies. Inhibitory kinetic analysis and molecular docking calculations were also applied for selected compounds. A flavonoid with two catechol groups in A- and B-rings, together with a 3-OH group at C-ring, was the most active, presenting an IC much lower than the one found for the most widely prescribed α-glucosidase inhibitor, acarbose. The present work suggests that several of the studied flavonoids have the potential to be used as alternatives for the regulation of PPHG.
[Mh] Termos MeSH primário: Simulação por Computador
Flavonoides/farmacologia
Inibidores de Glicosídeo Hidrolases/química
Inibidores de Glicosídeo Hidrolases/farmacologia
Simulação de Acoplamento Molecular
alfa-Glucosidases/metabolismo
[Mh] Termos MeSH secundário: Acarbose/química
Acarbose/farmacologia
Relação Dose-Resposta a Droga
Flavonoides/química
Estrutura Molecular
Saccharomyces cerevisiae/enzimologia
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Flavonoids); 0 (Glycoside Hydrolase Inhibitors); EC 3.2.1.20 (alpha-Glucosidases); T58MSI464G (Acarbose)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171010
[Lr] Data última revisão:
171010
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170922
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2017.1368503



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