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1.
Luminescence ; 37(1): 51-57, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34610201

RESUMO

Here, to elucidate the interaction mechanism and physicochemical properties of remimazolam and human serum albumin interactions, techniques such as fluorescence, circular dichroism (CD) spectroscopy, and isothermal titration calorimetry have been applied for study. The thermodynamic parameters at body temperature (ΔS = -207 J·mol-1 ·K-1 , ΔS = -9.76 × 104 J·mol-1 and ΔG = -3.34 × 104 J·mol-1 ; 310 K) manifests one strong binding site on the protein, which was modulated by van der Waals forces and hydrogen bonds. What is more, the results of CD, synchronous and three-dimensional fluorescence showed that remimazolam altered the microenvironment of the protein amino acid residues. A distance of 2.1 nm between the remimazolam and Trp shows the potential for resonance energy transfer. Furthermore, these results potentially provide information for illustrating the pharmacodynamics and toxicodynamics of remimazolam when it is applied clinically.


Assuntos
Benzenossulfonatos , Benzodiazepinas , Albumina Sérica Humana , Benzenossulfonatos/química , Benzodiazepinas/química , Sítios de Ligação , Dicroísmo Circular , Humanos , Ligação Proteica , Albumina Sérica Humana/química , Espectrometria de Fluorescência , Termodinâmica
2.
J Biochem Mol Toxicol ; 28(10): 433-41, 2014 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-24939449

RESUMO

Herein, we report the effect of parecoxib on the structure and function of human serum albumin (HSA) by using fluorescence, circular dichroism (CD), Fourier transforms infrared (FTIR), three-dimensional (3D) fluorescence spectroscopy, and molecular docking techniques. The Stern-Volmer quenching constants K(SV) and the corresponding thermodynamic parameters ΔH, ΔG, and ΔS have been estimated by the fluorescence quenching method. The results indicated that parecoxib binds spontaneously with HSA through van der Waals forces and hydrogen bonds with binding constant of 3.45 × 10(4) M(-1) at 298 K. It can be seen from far-UV CD spectra that the α-helical network of HSA is disrupted and its content decreases from 60.5% to 49.6% at drug:protein = 10:1. Protein tertiary structural alterations induced by parecoxib were also confirmed by FTIR and 3D fluorescence spectroscopy. The molecular docking study indicated that parecoxib is embedded into the hydrophobic pocket of HSA.


Assuntos
Isoxazóis/química , Albumina Sérica/química , Sítios de Ligação , Dicroísmo Circular , Humanos , Ligação de Hidrogênio , Interações Hidrofóbicas e Hidrofílicas , Isoxazóis/metabolismo , Simulação de Acoplamento Molecular , Ligação Proteica , Estrutura Secundária de Proteína , Estrutura Terciária de Proteína , Albumina Sérica/metabolismo , Espectrometria de Fluorescência , Espectroscopia de Infravermelho com Transformada de Fourier , Termodinâmica
3.
Neurosci Lett ; 801: 137164, 2023 03 28.
Artigo em Inglês | MEDLINE | ID: mdl-36868396

RESUMO

AIM: We aimed to study the influence of sevoflurane on the nucleotide-binding domain and Leucine-rich repeat protein 3 (NLRP3) pathways in rats with cerebral ischemia/reperfusion (I/R) injury. METHODS: Sixty Sprague-Dawley rats were equally divided into five groups randomly: sham-operated, cerebral I/R, sevoflurane (Sevo), NLRP3 inhibitor-treated (MCC950), and sevoflurane and NLRP3 inducer-treated groups. Rats' neurological functions were assessed using Longa scoring after 24 h of reperfusion, after which they were sacrificed, and cerebral infarction area was determined by triphenyl tetrazolium chloride staining. Pathological changes in damaged portions were assessed using hematoxylin-eosin and Nissl staining, and cell apoptosis was detected by terminal-deoxynucleotidyl transferase-mediated nick end labeling staining. Interleukin 1 beta (IL-1ß), tumor necrosis factor α (TNF-α), interleukin-6 (IL-6), interleukin-18 (IL-18), malondialdehyde (MDA), and superoxide dismutase (SOD) levels in brain tissues were determined using enzyme-linked immunosorbent assay. Reactive oxygen species (ROS) levels were analyzed using a ROS assay kit. Protein levels of NLRP3, caspase-1, and IL-1ß were determined by western blot. RESULTS: Neurological function scores, cerebral infarction areas, and neuronal apoptosis index were decreased in the Sevo and MCC950 groups than in the I/R group. IL-1ß, TNF-α, IL-6, IL-18, NLRP3, caspase-1, and IL-1ß levels decreased in the Sevo and MCC950 groups (p < 0.05). ROS and MDA levels increased, but SOD levels increased in the Sevo and MCC950 groups than in the I/R group. NLPR3-inducer nigericin eliminated the protective effects of sevoflurane on cerebral I/R injury in rats. CONCLUSION: Sevoflurane could alleviate cerebral I/R-induced brain damage by inhibiting the ROS-NLRP3 pathway.


Assuntos
Isquemia Encefálica , Traumatismo por Reperfusão , Ratos , Animais , Sevoflurano/farmacologia , Ratos Sprague-Dawley , Interleucina-18 , Espécies Reativas de Oxigênio/metabolismo , Proteína 3 que Contém Domínio de Pirina da Família NLR/metabolismo , Interleucina-6 , Fator de Necrose Tumoral alfa/metabolismo , Doenças Neuroinflamatórias , Isquemia Encefálica/tratamento farmacológico , Traumatismo por Reperfusão/metabolismo , Caspase 1/metabolismo , Infarto Cerebral/tratamento farmacológico , Reperfusão , Superóxido Dismutase
4.
Exp Ther Med ; 21(5): 469, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-33767764

RESUMO

The aim of the present study was to investigate the effect of exposure to sevoflurane general anesthesia during early pregnancy on interferon-inducible protein AIM2 (AIM2) expression in the hippocampus and parietal cortex of the offspring Sprague-Dawley (SD) rats. A total of 18 SD rats at a gestational age of 5-7 days were randomly divided into three groups: i) A control group (control); ii) 2-h sevoflurane general anesthesia, group 1 (S1); and iii) 4-h sevoflurane general anesthesia, group 2 (S2). The six offspring rats in each group were maintained for 30 days and assessed by Morris water maze testing. Brain specimens were collected from offspring rats 30 days after birth. Changes in the structural morphology of neurons in the hippocampus and parietal cortex were observed using hematoxylin and eosin staining. Nissl bodies in the hippocampus and parietal cortex were observed by Nissl staining. The expression of glial fibrillary acidic protein (GFAP), AIM2, CD45 and IL-1ß was detected by immunohistochemistry and the protein levels of CD45, IL-1ß, pro-caspase-1 and caspase-1 p10 were detected by western blotting. Compared with the control group, offspring rats in the S1 and S2 groups exhibited poor long-term learning and memory ability and experienced different degrees of damage to both the hippocampus and parietal cortex. The expression levels of GFAP, AIM2, CD45, IL-1ß, caspase-1 and caspase-1 p10 in the offspring of both the S1 and the S2 groups were significantly increased (P<0.05) compared with offspring of the control group. Moreover, compared with the offspring of the S1 group, hippocampal and parietal cortex injury in the offspring of the S2 group was further aggravated, and the expression of GFAP, AIM2, CD45, IL-1ß, pro-caspase-1 and cleaved-caspase-1 was significantly increased (P<0.05). In conclusion, sevoflurane general anesthesia in SD rat early pregnancy promoted the expression of AIM2 and the inflammatory response in the hippocampus and parietal cortex of offspring rats.

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