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1.
Artigo em Inglês | MEDLINE | ID: mdl-35911142

RESUMO

Purpose: Complete detachment of the medial collateral ligament (MCL) may occur during medial release of total knee arthroplasty (TKA) in patients with severe varus knee osteoarthritis. This study was to determine functional and stability outcomes of repaired knee with complete detachment of MCL compared to those of contralateral nondetached MCL in patients with bilateral TKA. Methods: Records of 1052 consecutive knees undergoing bilateral TKA from 2003 to 2015 were retrospectively reviewed. Of which, 45 patients were repaired for complete MCL detachment injury (2.1%) at tibial insertion in one side (repaired group). MCL was not detached in the contralateral side (control group). Clinical evaluation was performed preoperatively and at the final follow-up using KS and WOMAC scores between two groups. Similarly, stability was compared on a valgus stress radiograph between two groups. Results: Two patients had insufficient data. Hence, 43 patients were included after a minimum of 5 years follow-up. There were no significant differences in terms of alignment and clinical outcomes between the two groups either preoperatively or at the final follow-up (p > 0.05). Radiographic stability also showed no differences between repaired and control groups in extension and 30° of flexion (p=0.208 and p=0.125). Conclusions: For tibial detachment of the MCL during TKA, repair with suture anchor provided good clinical and stability results, similar to TKA without MCL injury. Therefore, repair with a suture anchor is a reliable method that provides good clinical and stability outcomes in patients with MCL injury during TKA.

2.
Bioorg Chem ; 124: 105813, 2022 07.
Artigo em Inglês | MEDLINE | ID: mdl-35447405

RESUMO

A series of dihydrotriazine derivatives bearing 5-aryloxypyrazole moieties were designed, and their anticancer activities against three human cancer cell lines (SGC-7901, HepG-2 and MCF-7) and one non-cancer cell line (LO2) were explored using the MTT assay in vitro. Most of the compounds exhibited potent antiproliferative activities against the three cancer cell lines, with compound 10e (IC50 = 2.12 µM) exhibiting the most potent antiproliferative activity against HepG-2 cells. Interestingly, autophagy was observed in the 10e-treated HepG-2 cells. Compound 10e also increased reactive oxygen species (ROS) levels and resulted in marked HepG-2 cells apoptosis. Further studies revealed that compound 10e could enhance the expression of Cl-PARP, Cl-caspase-3, and Cl-caspase-9. In addition, 10e triggered the formation of autophagosomes by promoting LC3-II and Beclin-1 expression. These results might be useful for exploring and developing dihydrotriazine derivatives as novel anticancer agents.


Assuntos
Antineoplásicos , Neoplasias , Antineoplásicos/farmacologia , Apoptose , Autofagia , Linhagem Celular Tumoral , Proliferação de Células , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espécies Reativas de Oxigênio/metabolismo , Relação Estrutura-Atividade
3.
Mol Divers ; 26(2): 1129-1139, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-34080112

RESUMO

In order to discover novel anti-inflammatory agents, three series of compounds obtained by appending 1,2,3-triazole moieties on ursolic acid were designed and synthesized. All compounds have been screened for their anti-inflammatory activity by using an ear edema model. The potent anti-inflammatory compound was subjected to in vitro cyclooxygenase COX-1/COX-2 inhibition assays. In general, the derivatives were found to be potent anti-inflammatory activity. Especially, the compound 11b exhibited the strongest activity of all of the compounds prepared, with 82.81% inhibition after intraperitoneal administration, which was better than celecoxib as a positive control. Molecular docking results unclose the rationale for the interaction of the compound 11b with COX-2 enzyme. Further studies revealed that compound 11b exhibited effective COX-2 inhibitory activity, with half-maximal inhibitor concentration (IC50) value of 1.16 µM and selectivity index (SI = 64.66) value close to that of celecoxib (IC50 = 0.93 µM, SI = 65.47). Taken together, these results could suggest a promising chemotype for development of new COX-2-targeting anti-inflammatory agent.


Assuntos
Inibidores de Ciclo-Oxigenase 2 , Triazóis , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios não Esteroides/farmacologia , Celecoxib/farmacologia , Ciclo-Oxigenase 2/metabolismo , Inibidores de Ciclo-Oxigenase 2/farmacologia , Relação Dose-Resposta a Droga , Desenho de Fármacos , Simulação de Acoplamento Molecular , Estrutura Molecular , Relação Estrutura-Atividade , Triazóis/farmacologia , Triterpenos , Ácido Ursólico
4.
Photochem Photobiol Sci ; 14(4): 853-8, 2015 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-25694154

RESUMO

Quaterthiophene is used as a fluorescent marker for biological applications, but the intrinsic excited state dynamics for its high triplet-formation yield are still under debate due to the complexity of the molecule structure and the undetermined energy level order. In this work, ultrafast geometry relaxation and intersystem crossing of quaterthiophene in 1,4-dioxane are studied by femtosecond time-resolved spectroscopy combined with quantum calculations. Transient absorption spectra at a pump wavelength of 400 nm are completely recorded up to the delay time of 1 ns. The kinetic traces of excited state absorption indicate that geometry relaxation occurs on the S1 potential energy surface with a time constant of ∼70 ps. Two triplet-triplet absorption bands centered at 563 nm and 600 nm show a direct dynamical conversion. The intersystem crossing is determined to be ∼398 ps. The high triplet yield is measured as ∼0.7 via the efficient intersystem crossing. On the basis of quantum chemical calculations, a general mechanism is proposed to describe the geometry relaxation and intersystem crossing processes.

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