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1.
Artigo em Inglês | MEDLINE | ID: mdl-35682411

RESUMO

The novel coronavirus, termed severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), is responsible for the disease called coronavirus disease 2019 (COVID-19). Besides the important rates of mortality and morbidity directly attributed to the infection itself, many studies detected an important shift towards mostly unhealthy lifestyle patterns in previously healthy non-infected populations all around the world. Although most of the changes in lifestyle had or will have a negative impact on general population health status, some findings are encouraging. Notwithstanding that there was an obvious necessity for governments to apply national lockdowns, it is also necessary to identify and comprehend the consequences they have caused. A narrative literature review was performed, based on scientific articles and previous reviews. An accurate description of changes in eating habits and alcohol consumption, physical activity, mental health, daily routines, economic impacts, and broader effects on society is provided for each continent and different age groups through this review. The volume of selected scientific surveys encompasses approximately 400,000 persons.


Assuntos
COVID-19 , COVID-19/epidemiologia , Controle de Doenças Transmissíveis , Dieta , Exercício Físico , Humanos , Estilo de Vida , SARS-CoV-2
2.
Nutrients ; 12(11)2020 Nov 16.
Artigo em Inglês | MEDLINE | ID: mdl-33207743

RESUMO

Intravenous administration of pure soybean oil emulsions high in linoleic acid may lead to inflammation and lipid peroxidation in preterm neonates. We aimed to investigate the effects of a medium-chain triglyceride (MCT)/ω-3 polyunsaturated fatty acid (PUFA)-enriched intravenous fat emulsion (IVFE) on plasma fatty acid (FA) profile and serum interleukin-6 (IL-6) in preterm neonates. In this double-blind randomized study, 92 preterm neonates (gestational age < 32 weeks, birth weight < 1500 g) were assigned to receive either MCT/ω-3 PUFA-enriched IVFE (Intervention Group) or soybean oil-based IVFE (Control Group). Levels of FAs were measured at baseline (day 0) and day 15 of parenteral nutrition with gas-chromatography mass-spectrometry. Serum IL-6 was measured with sandwich ELISA in 59 neonates. Plasma FAs changed significantly over time; the MCT/ω-3 PUFA-IVFE group showed higher ω-3 PUFAs (p = 0.031), eicosapentaenoic acid (p = 0.000), and oleic acid (p = 0.003), and lower ω-6/ω-3 PUFAs ratio (p = 0.001) and ω-6 PUFAs (p = 0.023) compared to control group. Linoleic acid was higher in the soybean oil (SO)-based IVFE arm compared to the MCT/ω-3 PUFAs-IVFE arm (p = 0.006). Both fat emulsion types decreased IL-6 compared to baseline, but changes were insignificant between groups. Administration of MCT/ω-3 PUFA-enriched IVFE in preterm neonates is beneficial in changing the FA profile consistent with attenuated inflammatory response.


Assuntos
Emulsões Gordurosas Intravenosas/administração & dosagem , Ácidos Graxos Ômega-3/administração & dosagem , Recém-Nascido Prematuro/crescimento & desenvolvimento , Nutrição Parenteral , Triglicerídeos/administração & dosagem , Método Duplo-Cego , Ácido Eicosapentaenoico/sangue , Emulsões Gordurosas Intravenosas/química , Ácidos Graxos Ômega-3/sangue , Ácidos Graxos Ômega-6/sangue , Feminino , Humanos , Recém-Nascido , Interleucina-6/sangue , Ácido Linoleico/sangue , Masculino , Ácido Oleico/sangue , Óleo de Soja/administração & dosagem
3.
Chem Biol Drug Des ; 96(1): 668-683, 2020 07.
Artigo em Inglês | MEDLINE | ID: mdl-32691965

RESUMO

Irbesartan (IRB) exerts beneficial effects either alone or in combination with other drugs on numerous diseases, such as cancer, diabetes, and hypertension. However, due to its high lipophilicity, IRB does not possess the optimum pharmacological efficiency. To circumvent this problem, a drug delivery system with 2-hydroxypropyl-ß-cyclodextrin (2-HP-ß-CD) was explored. The 1:1 complex between IRB and 2-HP-ß-CD was identified through ESI QTF HRMS. Dissolution studies showed a higher dissolution rate of the lyophilized IRB-2-HP-ß-CD complex than the tablet containing IRB at pH = 1.2. DSC results revealed the differences of the thermal properties between the complex and various mixtures consisting of the two components, namely IRB and 2-HP-ß-CD. Interestingly, depending on the way the mixture preparation was conducted, different association between the two components was observed. Molecular dynamics (MD) simulations predicted the favorable formation of the above complex and identified the dominant interactions between IRB and 2-HP-ß-CD. In vitro pharmacological results verified that the inclusion complex not only preserves the binding affinity of IRB for AT1R receptor, but also it slightly increases it. As the complex formulation lacks the problems of the tablet, our approach is a promising new way to improve the efficiency of IRB.


Assuntos
2-Hidroxipropil-beta-Ciclodextrina/química , Anti-Hipertensivos/química , Irbesartana/química , Anti-Hipertensivos/farmacologia , Composição de Medicamentos , Liberação Controlada de Fármacos , Liofilização , Humanos , Conformação Molecular , Simulação de Dinâmica Molecular , Solubilidade , Espectrometria de Massas por Ionização por Electrospray
4.
Mol Pharm ; 12(3): 954-65, 2015 Mar 02.
Artigo em Inglês | MEDLINE | ID: mdl-25665128

RESUMO

Cyclodextrins (CDs) are a well-known class of supermolecules that have been widely used to protect drugs against conjugation and metabolic inactivation as well as to enhance the aqueous solubility and hence to ameliorate the oral bioavailability of sparingly soluble drug molecules. The hepatoprotectant drug silibinin can be incorporated into CDs, and here we elucidate the interaction between the drug and the host at the molecular level. The complexation product of silibinin with 2-hydroxypropyl-ß-cyclodextrin (HP-ß-CD) is characterized by Differential Scanning Calorimetry, mass spectrometry, solid and liquid high-resolution NMR spectroscopy. The chemical shift changes using (13)C CP/MAS on the complexing of the guest with the host provided significant information on the molecular interactions, and they were in agreement with the 2D NOESY results. These results point out that in both solid and liquid forms, the drug is engulfed and interacts with HP-ß-CD in identical manner. Molecular dynamics calculations have been performed to examine the thermodynamic characteristics associated with the silibinin-HP-ß-CD interactions and to study the stability of the complex. To approximate the physiological conditions, the aqueous solubility and dissolution characteristics of the complex at pH states simulating those of the upper gastrointestinal tract have been applied. To evaluate the antiproliferative activity of silibinin-HP-ß-CD complex comparatively to silibinin in MCF-7 human cancer cells, MTT assays have been performed.


Assuntos
Silimarina/administração & dosagem , Silimarina/química , beta-Ciclodextrinas/administração & dosagem , beta-Ciclodextrinas/química , 2-Hidroxipropil-beta-Ciclodextrina , Biofarmácia , Fenômenos Biofísicos , Proliferação de Células/efeitos dos fármacos , Interações Medicamentosas , Humanos , Células MCF-7 , Espectroscopia de Ressonância Magnética , Modelos Moleculares , Simulação de Dinâmica Molecular , Estrutura Molecular , Substâncias Protetoras/administração & dosagem , Substâncias Protetoras/química , Silibina , Solubilidade
5.
Comb Chem High Throughput Screen ; 17(8): 652-62, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24875271

RESUMO

The dissolution of the antihypertensive AT1 antagonist olmesartan in methanol generates in situ a new highly bioactive methyl ether analogue via SN1 mechanism involving an intramolecular proton transfer from carboxyl to hydroxyl group. Theoretical calculations confirmed the thermodynamic control preference of methyl ether versus the antagonistic product methyl ester. Α facile synthetic method for olmesartan methyl ether from olmesartan or olmesartan medoxomil is also described. Interestingly, the introduction of the methyl group to olmesartan did not alter its pharmacological properties. This observation opens new avenues in the synthesis of novel drugs, since hydroxyl and carboxylate groups have an orthogonal relationship in many drugs.


Assuntos
Antagonistas de Receptores de Angiotensina/química , Imidazóis/química , Tetrazóis/química , Antagonistas de Receptores de Angiotensina/síntese química , Anti-Hipertensivos/síntese química , Anti-Hipertensivos/química , Imidazóis/síntese química , Modelos Teóricos , Estrutura Molecular , Tetrazóis/síntese química
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