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1.
Aging (Albany NY) ; 13(5): 6702-6711, 2021 02 17.
Artigo em Inglês | MEDLINE | ID: mdl-33675295

RESUMO

OBJECTIVE: Obesity has gained attention among patients with inflammatory bowel disease (IBD). The impact of visceral obesity on chronic constipation, inflammation, immune function and cognition after diagnosis of IBD is still unknown. METHODS: This is a cross-sectional study of 150 IBD patients. Patients' visceral adipose tissue (VAT) and subcutaneous adipose tissue (SAT) were measured and were grouped according to visceral obesity. The potential impact of visceral obesity on cognitive function were evaluated using Mini-Mental State Examination. We evaluated patients' incidence of chronic constipation, levels of interleukin-6 (IL-6), T cells and body mass index in two groups. RESULTS: The prevalence of visceral obesity was 51% (37 out of 72) for Crohn's disease (CD) patients and 26% for UC patients (20 out of 78 patients). CD patients with visceral obesity has higher incidence of chronic constipation (81% vs. 57%, P = 0.028), higher IL-6 levels (15.28 pg/ml vs. 9.429 pg/ml, P = 0.007) and lower CD4+ T cells (32.7% vs. 44.0%, P < 0.001). VAT/SAT ratio is associated with BMI (P < 0.001). CONCLUSIONS: IBD patients had high risks of visceral obesity. CD Patients with visceral obesity had higher prevalence of chronic constipation, higher inflammation levels, decreased immune function.


Assuntos
Doenças Inflamatórias Intestinais/complicações , Obesidade Abdominal/complicações , Adulto , Idoso , Índice de Massa Corporal , Linfócitos T CD4-Positivos/metabolismo , Doença Crônica , Disfunção Cognitiva/diagnóstico , Constipação Intestinal/complicações , Estudos Transversais , Feminino , Humanos , Interleucina-6/sangue , Masculino , Testes de Estado Mental e Demência , Pessoa de Meia-Idade , Adulto Jovem
2.
Molecules ; 21(7)2016 Jul 04.
Artigo em Inglês | MEDLINE | ID: mdl-27384553

RESUMO

A series of bedaquiline analogs containing H-bond donors were designed as anti-Mycobacterium tuberculosis drugs. A pair of diastereoisomers (R/S- and S/S-isomers) was selected from these designed compounds for synthetic and stereochemical research. The title compounds were synthesized from chiral precursors for the first time and the absolute configurations (ACs) were determined by electronic circular dichroism (ECD) with quantum chemical calculations. Moreover, a single crystal of the S/S compound was obtained for X-ray diffraction analysis, and the crystal structure showed high consistency with the geometry, confirming the reliability of ACs obtained by ECD analyses and theoretical simulation. Furthermore, the effect of stereochemistry on the anti-tuberculosis activity was investigated. The MICs of the R/S- and S/S-isomers against Mycobacterium phlei 1180 are 9.6 and 32.1 µg·mL(-1), respectively. Finally, molecular docking was carried out to evaluate the inhibitory nature and binding mode differences between diastereoisomers.


Assuntos
Antituberculosos/química , Antituberculosos/farmacologia , Diarilquinolinas/química , Diarilquinolinas/farmacologia , Desenho de Fármacos , Modelos Moleculares , Conformação Molecular , Adenosina Trifosfatases/química , Adenosina Trifosfatases/metabolismo , Antituberculosos/síntese química , Sítios de Ligação , Cristalografia por Raios X , Diarilquinolinas/síntese química , Ligação de Hidrogênio , Simulação de Acoplamento Molecular , Ligação Proteica , Estereoisomerismo , Relação Estrutura-Atividade , Difração de Raios X
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