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1.
Front Med (Lausanne) ; 10: 1218720, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38034536

RESUMO

Pelvic fractures mostly result from high-energy injuries in life; the longitudinal fracture of the sacrum is the most common type of sacrum fracture. This study was designed to evaluate the accuracy, safety, and efficacy of percutaneous sacroiliac joint screw placement in the treatment of longitudinal sacrum fractures with the assistance of unobstructed orthopaedic surgery robots. According to different surgical methods, 32 patients were divided into robot group and free hand group, with 16 patients in each group. The operation time, intra-operative blood loss, intra-operative fluoroscopy times, screw placement angle deviation were collected. There were statistically significant differences in terms of angle deviation of screw placement (1.96 ± 0.75° vs. 2.87 ± 1.03°; p = 0.0145), deviation of the guide needle (1.92 ± 0.93 mm vs. 2.91 ± 1.22 mm; p = 0.0209), intra-operative fluoroscopy time (7.25 ± 1.72 s vs. 20.93 ± 5.64 s; p = 0.0000), insertion time of each sacroiliac joint screw (14.72 ± 2.66 min vs. 29.21 ± 5.18 min; p = 0.0000). There was no statistically significant difference in terms of blood loss (100.21 ± 7.37 mL vs. 102.52 ± 8.15 mL; p = 0.4136). These results suggest that orthopaedic surgery robot for the treatment of longitudinal sacrum fracture is safer and provides less irradiation than the traditional freehand methods.

2.
Eur J Med Chem ; 102: 26-38, 2015 Sep 18.
Artigo em Inglês | MEDLINE | ID: mdl-26241875

RESUMO

Three series of resveratrol oligomer derivatives were synthesized, including the indenone-type, indene-type and octahydropentalene-type derivatives, among which ten derivatives were novel compounds. Compounds 2, 14f, and 4d were confirmed as ERß agonists by yeast two-hybrid assay, and compound 2 (isopaucifloral F) was further chosen to evaluate its anti-osteoporosis activity in vivo. Compared with the sham-operated and the positive control groups, isopaucifloral F (10 µg/kg) showed a notable anti-osteoporosis effect in the ovariectomized (OVX) female rats based on a micro-CT analysis and the following measurements: bone mineral density, bone volume/tissue volume, trabecular thickness, trabecular separation/spacing, and the serum biochemical parameters. LD50 of isopaucifloral F was found to be greater than 5 mg/kg and its effective dose (ED) was found to be about 10 µg/kg. Therefore, isopaucifloral F may be a promising lead compound for the treatment of postmenopausal osteoporosis.


Assuntos
Receptor beta de Estrogênio/agonistas , Estrogênios/farmacologia , Osteoporose/tratamento farmacológico , Ovariectomia , Estilbenos/química , Estilbenos/farmacologia , Animais , Modelos Animais de Doenças , Estrogênios/síntese química , Feminino , Osteoporose/cirurgia , Ratos , Ratos Sprague-Dawley , Resveratrol , Estilbenos/síntese química
3.
Dalton Trans ; 43(18): 6667-76, 2014 May 14.
Artigo em Inglês | MEDLINE | ID: mdl-24626563

RESUMO

MnO(x) modified ZnAl layered double oxides (M-LDO) nanocomposites were prepared through an intercalation/reduction/calcination process. The morphology and crystal structure of M-LDO were characterized by powder X-ray diffraction (XRD), transmission electron microscopy (TEM), Thermogravimetric analysis (TGA) and Fourier transform infrared spectroscopy (FT-IR) analysis methods. The results confirmed that the manganese oxide nanoparticles were well distributed on the LDO support. Methyl orange (MO) was chosen as a common water-soluble azo dye probe to evaluate the adsorption performance of M-LDO. The effects of MO initial concentration, agitation time, and temperature on MO adsorption were investigated. It was found that adsorption equilibrium data were best represented by the Langmuir and Redlich-Peterson isotherms and the maximum adsorption capacity was 617.28 mg g(-1) obtained from the Langmuir isotherm, which was much larger than some reported adsorbents. Besides, the adsorption process was spontaneous and endothermic in nature and followed a pseudo-second-order kinetic model. The mechanism of the adsorption process was elaborated by an intraparticle diffusion model. Moreover, the regeneration test of M-LDO was carried out and it showed that the used M-LDO was feasible for at least five times. In principle, this adsorbent with a high adsorption capacity and great reutilization performance could be a very promising adsorbent for wastewater treatment.


Assuntos
Compostos de Alumínio/química , Compostos Azo/isolamento & purificação , Compostos de Manganês/química , Nanocompostos/química , Nitratos/química , Óxidos/química , Compostos de Zinco/química , Adsorção , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Difração de Raios X
4.
Bioorg Med Chem Lett ; 23(24): 6834-7, 2013 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-24269481

RESUMO

By-product 9a exhibited potent cytotoxicity against both SK-OV-3 and A549 cell lines. The structure of 9a was characterized using 1D and 2D NMR experiments and confirmed by synthesis to afford a diastereomeric mixture (16a) that was identical to 9a, as well as a pair of diastereomers (R)-16b and (S)-16c. The preliminary SAR study demonstrated that analogs with an (R)-configuration were slightly more potent than analogs with an (S)-configuration. In addition, α,α-gem-dimethyl analogs 16 g-i were the most potent analogs in this series, exhibiting similar potency to docetaxel and greater potency than Taxol against the SK-OV-3 cell line. For the A549 cell line, analogs 16 g-i were more potent (>65-fold) than both docetaxel and Taxol.


Assuntos
Antineoplásicos/síntese química , Desenho de Fármacos , Taxoides/química , Antineoplásicos/química , Antineoplásicos/toxicidade , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Docetaxel , Humanos , Paclitaxel/química , Paclitaxel/toxicidade , Estereoisomerismo , Relação Estrutura-Atividade , Taxoides/síntese química , Taxoides/toxicidade
5.
Nanoscale Res Lett ; 8(1): 436, 2013 Oct 22.
Artigo em Inglês | MEDLINE | ID: mdl-24144325

RESUMO

In this work, we explored the formation processes of interfacial polygonal patterning via surfactant-mediated self-assembly of gold nanoparticles (AuNPs). We found that a balance between DDT-capped AuNPs and PVP-passivated AuNPs is a key to making these inorganic-organic thin films. The interfacial polygonal patterning possesses many processing advantages and flexibilities, such as controllable interfacial shape and inter-AuNP distance, tuning of particle sizes, thiol population, chain lengths, and other new properties by introducing functional groups to thiol chains. In principle, self-assembly of AuNPs via well-designed interfaces may be useful for fabrications of other complex architectures.

6.
Molecules ; 18(9): 10189-212, 2013 Aug 22.
Artigo em Inglês | MEDLINE | ID: mdl-23973993

RESUMO

Nine new 3'-N-phenylsulfonyl docetaxel analogs were synthesized in good yields from the key intermediate N-phenylsulfonyl oxazolidine via a six-step route. These analogs were tested for anti-hepatitis B virus (HBV) activity in vitro. Compounds 3e, 3g and 3j showed more potent inhibitory activity against HBeAg secretion than the positive control lamivudine. Further extensive SAR and mechanistic studies will be reported in due course.


Assuntos
Antivirais/síntese química , Vírus da Hepatite B/efeitos dos fármacos , Sulfonas/síntese química , Taxoides/síntese química , Antivirais/farmacologia , Docetaxel , Avaliação Pré-Clínica de Medicamentos , Células Hep G2 , Humanos , Paclitaxel/farmacologia , Relação Estrutura-Atividade , Sulfonas/farmacologia , Taxoides/farmacologia
7.
Eur J Pharm Biopharm ; 85(3 Pt A): 541-9, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-23791719

RESUMO

The aim of this work was to track the distribution and conversion of paclitaxel based prodrug by fluorescence imaging, which would help to up-regulate the therapeutic efficacy and reduce cytotoxicity of paclitaxel and docetaxel. We developed a novel prodrug for tumor treatment, in which a fluorinated docetaxel derivative, 4FDT as a chemotherapeutic reagent and rhodamine B as an imaging reporter as well as targeting domain were conjugated via a biodegradable ester bond. In vitro image studies demonstrated the morphological changes of tubulin and chromosomal alterations of human liver cancer cells HepG2, which were similar to the phenomena observed after treatment with the active drug 4FDT. At 48 h post-treatment, the cytotoxicity of 4FDT-RhB was 18.5% of that of 4FDT. However, this value increased to 49.3% of 4FDT at 72 h post-incubation. These experimental results implied the consistent release of the active drug from the prodrug throughout the incubation period via the linear increase in the cytotoxicity observed as a function of time. It also showed good stability in both plasma and complete blood. Additionally, the specific delivery of the prodrug to mitochondria was observed by fluorescent microscopy.


Assuntos
Antineoplásicos/administração & dosagem , Sistemas de Liberação de Medicamentos , Paclitaxel/administração & dosagem , Taxoides/administração & dosagem , Antineoplásicos/farmacocinética , Antineoplásicos/farmacologia , Antineoplásicos Fitogênicos/administração & dosagem , Antineoplásicos Fitogênicos/farmacocinética , Antineoplásicos Fitogênicos/farmacologia , Carcinoma Hepatocelular/tratamento farmacológico , Carcinoma Hepatocelular/patologia , Docetaxel , Flúor/química , Células Hep G2 , Humanos , Neoplasias Hepáticas/tratamento farmacológico , Neoplasias Hepáticas/patologia , Microscopia de Fluorescência , Mitocôndrias/metabolismo , Imagem Óptica , Paclitaxel/farmacocinética , Paclitaxel/farmacologia , Pró-Fármacos , Rodaminas/química , Taxoides/farmacocinética , Taxoides/farmacologia , Fatores de Tempo
8.
Acta Crystallogr Sect E Struct Rep Online ; 69(Pt 4): o601, 2013 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-23634128

RESUMO

In the title compound, C20H19NO4, the absolute configuration (3R,4S) for the two chiral centres of the mol-ecule has been determined.

9.
Eur J Med Chem ; 62: 187-98, 2013 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-23353752

RESUMO

Three types of resveratrol analogues were designed, synthesized and evaluated in vitro against paraquat-induced apoptosis in SH-SY5Y cells. The results showed that some compounds, especially those containing an indene core, exhibit good activities. Analogue 3'a showed a potent neuroprotective effect at a low concentration (10 µM). Further investigation showed that compound 3'a could attenuate paraquat-induced nuclear morphological changes, significantly decrease paraquat-induced ROS (reactive oxygen species) generation in SH-SY5Y cells and elevate the expression of SOD (Superoxide Dismutase) and GPx (glutathione peroxidase) in a dose-dependent manner. Furthermore, analogue 3'a could decrease Bax protein levels in a concentration-dependent manner and increase Bcl-2 protein expression, which was accompanied by increasing chances of cell survival.


Assuntos
Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Fármacos Neuroprotetores/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Fármacos Neuroprotetores/síntese química , Fármacos Neuroprotetores/química , Paraquat/farmacologia , Relação Estrutura-Atividade , Células Tumorais Cultivadas
10.
Nanoscale Res Lett ; 7(1): 295, 2012 Jun 06.
Artigo em Inglês | MEDLINE | ID: mdl-22673303

RESUMO

In this work, we explored the formation processes of suspended hybrid thin films of thiol-capped Au nanoparticles (AuNPs) inside metal oxide tubular structures. We found that a balance between in-film interactions of the AuNPs and boundary interactions with metal oxides is a key in making these special organic-inorganic thin films. The hybrid films process many processing advantages and flexibilities, such as controllable film thickness, interfacial shape and inter-AuNPs distance, tuning of particle sizes, thiol population, chain lengths, and other new properties by introducing functional groups to thiol chains. Among their many unique features, the assembly-disassembly property may be useful for future on-off or store-release applications.

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