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1.
BMC Cancer ; 24(1): 564, 2024 May 06.
Artigo em Inglês | MEDLINE | ID: mdl-38711026

RESUMO

BACKGROUND: 5-Fluorouracil (5FU) is a primary chemotherapeutic agent used to treat oral squamous cell carcinoma (OSCC). However, the development of drug resistance has significantly limited its clinical application. Therefore, there is an urgent need to determine the mechanisms underlying drug resistance and identify effective targets. In recent years, the Wingless and Int-1 (WNT) signaling pathway has been increasingly studied in cancer drug resistance; however, the role of WNT3, a ligand of the canonical WNT signaling pathway, in OSCC 5FU-resistance is not clear. This study delved into this potential connection. METHODS: 5FU-resistant cell lines were established by gradually elevating the drug concentration in the culture medium. Differential gene expressions between parental and resistant cells underwent RNA sequencing analysis, which was then substantiated via Real-time quantitative PCR (RT-qPCR) and western blot tests. The influence of the WNT signaling on OSCC chemoresistance was ascertained through WNT3 knockdown or overexpression. The WNT inhibitor methyl 3-benzoate (MSAB) was probed for its capacity to boost 5FU efficacy. RESULTS: In this study, the WNT/ß-catenin signaling pathway was notably activated in 5FU-resistant OSCC cell lines, which was confirmed through transcriptome sequencing analysis, RT-qPCR, and western blot verification. Additionally, the key ligand responsible for pathway activation, WNT3, was identified. By knocking down WNT3 in resistant cells or overexpressing WNT3 in parental cells, we found that WNT3 promoted 5FU-resistance in OSCC. In addition, the WNT inhibitor MSAB reversed 5FU-resistance in OSCC cells. CONCLUSIONS: These data underscored the activation of the WNT/ß-catenin signaling pathway in resistant cells and identified the promoting effect of WNT3 upregulation on 5FU-resistance in oral squamous carcinoma. This may provide a new therapeutic strategy for reversing 5FU-resistance in OSCC cells.


Assuntos
Resistencia a Medicamentos Antineoplásicos , Fluoruracila , Neoplasias Bucais , Via de Sinalização Wnt , Proteína Wnt3 , Humanos , Fluoruracila/farmacologia , Fluoruracila/uso terapêutico , Resistencia a Medicamentos Antineoplásicos/genética , Neoplasias Bucais/tratamento farmacológico , Neoplasias Bucais/metabolismo , Neoplasias Bucais/genética , Neoplasias Bucais/patologia , Via de Sinalização Wnt/efeitos dos fármacos , Linhagem Celular Tumoral , Proteína Wnt3/metabolismo , Proteína Wnt3/genética , beta Catenina/metabolismo , beta Catenina/genética , Carcinoma de Células Escamosas/tratamento farmacológico , Carcinoma de Células Escamosas/metabolismo , Carcinoma de Células Escamosas/genética , Carcinoma de Células Escamosas/patologia , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Antimetabólitos Antineoplásicos/farmacologia , Carcinoma de Células Escamosas de Cabeça e Pescoço/tratamento farmacológico , Carcinoma de Células Escamosas de Cabeça e Pescoço/genética , Carcinoma de Células Escamosas de Cabeça e Pescoço/metabolismo , Carcinoma de Células Escamosas de Cabeça e Pescoço/patologia
2.
J Nanobiotechnology ; 22(1): 269, 2024 May 19.
Artigo em Inglês | MEDLINE | ID: mdl-38764018

RESUMO

Symbiotic microbial communities are crucial for human health, and dysbiosis is associated with various diseases. Plant-derived nanovesicles (PDNVs) have a lipid bilayer structure and contain lipids, metabolites, proteins, and RNA. They offer unique advantages in regulating microbial community homeostasis and treating diseases related to dysbiosis compared to traditional drugs. On the one hand, lipids on PDNVs serve as the primary substances that mediate specific recognition and uptake by bacteria. On the other hand, due to the multifactorial nature of PDNVs, they have the potential to enhance growth and survival of beneficial bacterial while simultaneously reducing the pathogenicity of harmful bacteria. In addition, PDNVs have the capacity to modulate bacterial metabolism, thus facilitating the establishment of a harmonious microbial equilibrium and promoting stability within the microbiota. These remarkable attributes make PDNVs a promising therapeutic approach for various conditions, including periodontitis, inflammatory bowel disease, and skin infection diseases. However, challenges such as consistency, isolation methods, and storage need to be addressed before clinical application. This review aims to explore the value of PDNVs in regulating microbial community homeostasis and provide recommendations for their use as novel therapeutic agents for health protection.


Assuntos
Microbiota , Humanos , Plantas , Bactérias/metabolismo , Disbiose/microbiologia , Animais , Nanopartículas/química , Nanoestruturas/química , Periodontite/microbiologia
3.
BMC Musculoskelet Disord ; 25(1): 591, 2024 Jul 27.
Artigo em Inglês | MEDLINE | ID: mdl-39068403

RESUMO

OBJECTIVE: With the development of surgical technology, the level of digital medicine is constantly improving. The birth of new technologies has a certain impact on traditional methods. At present, robot-assisted technology has been applied to patients with calcaneal fractures, which poses a challenge to traditional surgery. We aimed to assess whether robot-assisted internal fixation confers certain surgical advantages through a literature review. DESIGN: The databases PubMed, EMBASE, the Cochrane Library, the China National Knowledge Infrastructure (CNKI), and the Wanfang Data Knowledge Service Platform were systematically searched for both randomized and nonrandomized studies involving patients with calcaneal fractures. MAIN RESULTS: Five studies were identified that compared clinical indexes. For the clinical indexes, robot-assisted surgery is generally feasible because of intraoperative fluoroscopy, complications, the Gissane angle, the calcaneal width, and the American Orthopedic Foot and Ankle Society (AOFAS) Ankle-Hindfoot score 3 and 6 months after the operation (P < 0.05). However, on the operation time, Böhler's angle at 3 and 6 months, Gissane angle and calcaneal width at 6 months after the operation did not show good efficacy compared with those of the traditional group (P > 0.05). CONCLUSIONS: Based on the current evidence, the advantages of robot-assisted fixation over traditional fixation are clear. The long-term clinical effects of the two methods are also good, and the short-term effect of robot assistance is better. However, the quality of some studies is low, and more high-quality randomized controlled trials (RCTs) are needed for further verification.


Assuntos
Calcâneo , Fixação Interna de Fraturas , Fraturas Ósseas , Procedimentos Cirúrgicos Robóticos , Humanos , Calcâneo/lesões , Calcâneo/cirurgia , Calcâneo/diagnóstico por imagem , Fixação Interna de Fraturas/métodos , Fixação Interna de Fraturas/instrumentação , Fraturas Ósseas/cirurgia , Fraturas Ósseas/diagnóstico por imagem , Ensaios Clínicos Controlados Aleatórios como Assunto/métodos , Procedimentos Cirúrgicos Robóticos/métodos , Procedimentos Cirúrgicos Robóticos/efeitos adversos , Resultado do Tratamento
4.
Brief Bioinform ; 22(5)2021 09 02.
Artigo em Inglês | MEDLINE | ID: mdl-33594424

RESUMO

m6A RNA methylation is an emerging epigenetic modification, and its potential role in immunity and stemness remains unknown. Based on 17 widely recognized m6A regulators, the m6A modification patterns and corresponding characteristics of immune infiltration and stemness of 1152 low-grade glioma samples were comprehensively analyzed. Machine-learning strategies for constructing m6AScores were trained to quantify the m6A modification patterns of individual samples. Here, we reveal a significant correlation between the multi-omics data of regulators and clinicopathological parameters. We identified two distinct m6A modification patterns (an immune-activated differentiation pattern and an immune-desert dedifferentiation pattern) and four regulatory patterns of m6A methylation on immunity and stemness. We show that the m6AScores can predict the molecular subtype of low-grade glioma, the abundance of immune infiltration, the enrichment of signaling pathways, gene variation and prognosis. The concentration of high immunogenicity and clinical benefits in the low-m6AScore group confirmed the sensitive response to radio-chemotherapy and immunotherapy in patients with high-m6AScore. The results of the pan-cancer analyses illustrate the significant correlation between m6AScore and clinical outcome, the burden of neoepitope, immune infiltration and stemness. The assessment of individual tumor m6A modification patterns will guide us in improving treatment strategies and developing objective diagnostic tools.


Assuntos
Adenosina/análogos & derivados , Dioxigenase FTO Dependente de alfa-Cetoglutarato/genética , Neoplasias Encefálicas/genética , Neoplasias Encefálicas/imunologia , Metilação de DNA/genética , Regulação Neoplásica da Expressão Gênica/imunologia , Glioma/genética , Glioma/imunologia , Imunidade Inata , Metiltransferases/genética , Proteínas de Ligação a RNA/genética , Adenosina/genética , Biomarcadores Tumorais/genética , Neoplasias Encefálicas/patologia , Variações do Número de Cópias de DNA , Epigênese Genética , Glioma/patologia , Humanos , Linfócitos do Interstício Tumoral/imunologia , Aprendizado de Máquina , Taxa de Mutação , Fenótipo , Prognóstico , Microambiente Tumoral/genética , Microambiente Tumoral/imunologia
5.
Biochem Biophys Res Commun ; 625: 38-45, 2022 10 15.
Artigo em Inglês | MEDLINE | ID: mdl-35944362

RESUMO

Glioma is a clinically heterogeneous disease with a poor prognosis. Berberine (BBR), as a multi-target anti-tumor alkaloid, has the ability to penetrate the blood-brain barrier and shows cytotoxicity to glioma cells. In previous studies, we demonstrated that berberine inhibits glioma cell proliferation by inhibiting mutant p53 protein and promoting mitochondrial damage. In addition, berberine has been shown to reduce collagen accumulation in pulmonary fibrosis, diabetic nephropathy and arthritis. However, its effect on collagen in cancer needs to be further elucidated. In this study, we proved that the collagen XI alpha 1 chain (COL11A1) is highly expressed in glioma cell lines and associated with migration and invasion of glioma cells. Knocking down COL11A1 caused decreased expression of MMPs. Berberine could inhibit the migration and invasion of glioma cells by suppressing the TGF-ß1/COL11A1 pathway and changes actin cytoskeleton arrangement. Nude mouse subcutaneous xenografts model also showed that berberine inhibited the expression of COL11A1 in vivo. Collectively, berberine that targets COL11A1 to inhibit glioma migration and invasion, may serve as a promising candidate for the development of anti-glioma drugs in the future.


Assuntos
Berberina , Glioma , Animais , Berberina/farmacologia , Linhagem Celular Tumoral , Movimento Celular , Proliferação de Células , Colágeno/farmacologia , Colágeno Tipo XI , Glioma/tratamento farmacológico , Glioma/patologia , Humanos , Camundongos , Camundongos Nus , Fator de Crescimento Transformador beta1/metabolismo
6.
Appl Opt ; 61(8): 1898-1905, 2022 Mar 10.
Artigo em Inglês | MEDLINE | ID: mdl-35297879

RESUMO

A compact digital control system based on an all-programmable system-on-chip iodine-stabilized laser is presented for realization of the meter. The system is composed of ZYNQ7000, peripheral circuits, and human-computer interaction, which can operate independently. An nth-harmonic extraction algorithm with less resource consumption is used in this system. The digital system overcomes the problems of complex debugging, large volume, and manual locking. Additionally, customers can set up, calibrate, and upgrade the system by themselves. Its stability is similar to that of the current analog system, with long-term stability of up to 10-13. The repeatability of the two lasers with the digital system is approximately 1.5×10-11, and the absolute frequencies satisfy the international recommendation.

7.
J Plant Res ; 135(6): 723-737, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-36260182

RESUMO

We sequenced and analyzed the complete chloroplast genomes of Lilium amoenum, Lilium souliei, and Nomocharis forrestii in detail, including the first sequence and structural comparison of Nomocharis forrestii. We found that the lengths and nucleotide composition of the three chloroplast genes showed little variation. The chloroplast genomes of the three Lilium species contain 87 protein coding genes (PCGs), 38 tRNAs, and 8 rRNA genes. The only difference is that Nomocharis forrestii had an additional infA pseudogene. In the sequence analysis of the Lilium chloroplast genomes, 216 SSRs, 143 pairs of long repeats, 571 SNPs, and 202 indels were detected. In addition, we identified seven hypervariable regions that can be used as potential molecular markers and DNA barcodes of Lilium through complete sequence alignment. The phylogenetic tree was constructed from the three chloroplast genome sequences of Lilium obtained here and 40 chloroplast genome sequences from the NCBI database (including 35 Lilium species, 4 Fritillaria species, and one species of Smilax). The analysis showed that the species clustering of the genus Lilium essentially conformed to the classical morphological classification system of Comber, but differences in the classification of individual species remained. In our report, we support the reclassification of Lilium henryi and Lilium rosthorniiy in the genus Lilium. In general, this study not only provides genome data for three Lilium species, but also provides a comparative analysis of the Lilium chloroplast genomes. These advances will help to identify Lilium species, clarify the phylogenetic analysis of the Lilium genus, and help to solve and improve the disputes and deficiencies in the traditional morphological classification.


Assuntos
Genoma de Cloroplastos , Lilium , Genoma de Cloroplastos/genética , Filogenia , Lilium/genética , Genômica , Alinhamento de Sequência
8.
Angew Chem Int Ed Engl ; 61(34): e202208143, 2022 08 22.
Artigo em Inglês | MEDLINE | ID: mdl-35730106

RESUMO

A cobalt porphyrin complex with a pendant imidazole base ([(L1 )CoII ]) is an efficient catalyst for the homogeneous catalytic two-electron reduction of dioxygen by 1,1'-dimethylferrocene (Me2 Fc) in the presence of triflic acid (HOTf), as compared with a cobalt porphyrin complex without a pendant imidazole base ([(L2 )CoII ]). The pendant imidazole ligand plays a crucial role not only to provide an imidazolinium proton for proton-coupled electron transfer (PCET) from [(L1 )CoII ] to O2 in the presence of HOTf but also to facilitate electron transfer (ET) from [(L1 )CoII ] to O2 in the absence of HOTf. The kinetics analysis and the detection of intermediates in the stoichiometric and catalytic reduction of O2 have provided clues to clarify the crucial roles of the pendant imidazole ligand of [(L1 )CoII ] for the first time.


Assuntos
Cobalto , Porfirinas , Imidazóis , Ligantes , Oxirredução , Oxigênio , Prótons
9.
Cancer Cell Int ; 21(1): 492, 2021 Sep 16.
Artigo em Inglês | MEDLINE | ID: mdl-34530814

RESUMO

BACKGROUND: Toosendanin (TSN) is a triterpenoid compound mainly used as an ascaris repellant. Recent studies have shown that it possesses antitumor effects in many types of tumor cells. However, the effects of TSN on glioma cells have rarely been reported. METHODS: Different assays were performed to investigate the effects of TSN on the different glioma cell lines including U87MG and LN18. The assays included colony formation, wound healing, and transwell assays. Furthermore, Hoechst 33342 staining, flow cytometry, and western blotting analysis were performed to investigate the apoptotic activities of TSN. Finally, the results were confirmed using a xenograft tumor model that comprised of nude mice. RESULTS: In vitro, the CCK-8 and colony formation assays showed that TSN effectively inhibited glioma cell proliferation. Moreover, the inhibitory effects on glioma cell migration and invasion were demonstrated through the wound healing and transwell assays, respectively. Hoechst 33342 staining, flow cytometry, and western blotting assays demonstrated the significant effect of TSN in the apoptosis induction of glioma cells. Furthermore, the anti-glioma effect of TSN was exerted through the inhibition of the PI3K/Akt/mTOR signaling pathways as demonstrated by western blotting analysis. In addition, the effects of TSN on glioma cell viability, apoptosis, cell cycle arrest, migration, and invasion were reversed by 740Y-P, a PI3K activator. Finally, the mouse xenograft model confirmed the suppressive effect of TSN on tumor growth in vivo. CONCLUSION: Our results suggest that TSN is a promising chemotherapeutic drug for patients with glioma.

10.
J Craniofac Surg ; 32(3): 940-943, 2021 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-33290332

RESUMO

ABSTRACT: Mixed reality (MR) merges virtual information into the real world through computer technology, in which the real environment and virtual objects can get spliced in the same image or space at real time so that it can effectively express and integrate the virtual and real worlds and allow high feedback interaction. This technology combines the many advantages of virtual realityand augmented reality, and has a promising future in the medical field. At present, MR technology is just at the beginning stage in the medical field in the world, whose application in neurosurgery is also rarely reported. Given this, the authors described the research progress of MR in neurosurgery including preoperative planning and intraoperative guidance, doctor-patient communication, teaching rounds, physician training, and so on.


Assuntos
Realidade Aumentada , Neurocirurgia , Humanos , Procedimentos Neurocirúrgicos
11.
Anal Chem ; 92(2): 2151-2158, 2020 01 21.
Artigo em Inglês | MEDLINE | ID: mdl-31869211

RESUMO

Leaf-like hollow cobalt sulfides with a sulfur-gold-cysteine (S-Au-Cys) structure on the surface have been synthesized for efficient N-glycopeptide enrichment. A two-dimensional (2D) zeolitic imidazolate framework with cobalt (ZIF-L-Co, L for leaf) was used as a self-sacrificed template. After sulfidation, the S-Au-Cys architecture was created on the surface of the leaf-like hollow cobalt sulfide to obtain a material denoted ZIF-L-Co-S-Au-Cys. Enrichment of glycopeptides from trypsin digests of immunoglobulin G (IgG) standard samples and of IgG isolated from real human plasma samples was accomplished via hydrophilic interaction liquid chromatography processes using ZIF-L-Co-S-Au-Cys. The good sensitivity and selectivity ensure the effectiveness and robustness of ZIF-L-Co-S-Au-Cys for sample preconcentration, which is comparable to a commercial HILIC product. This work provides an efficient way to produce transition metal sulfides with a low-dimensional morphology and provides a novel concept for material design for exploitation in sample preparation, especially in glycoproteomics.


Assuntos
Aminoácidos/química , Cobalto/química , Glicopeptídeos/análise , Imidazóis/química , Nanopartículas/química , Zeolitas/química , Ouro/química , Humanos , Imunoglobulina G/química , Imunoglobulina G/isolamento & purificação , Imunoglobulina G/metabolismo , Estrutura Molecular , Tamanho da Partícula , Porosidade , Propriedades de Superfície
12.
Br J Neurosurg ; 34(2): 227-228, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-29405778

RESUMO

We describe a rare case of syringomyelia with left knee Charcot arthropathy in a 35-year-old male, who presented with dissociative sensory disorder, muscle atrophy, painless knee joint swelling and limited joint mobility. Early diagnosis and appropriate treatment are essential in avoiding disease progression.


Assuntos
Artropatia Neurogênica , Siringomielia , Adulto , Malformação de Arnold-Chiari , Humanos , Joelho , Masculino
13.
Chemistry ; 25(55): 12780-12788, 2019 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-31265180

RESUMO

The development of efficient bifunctional electrocatalysts for the oxygen reduction reaction (ORR) and oxygen evolution reaction (OER) still remains a challenge in a wide range of renewable energy technologies. Herein, CuCo alloy nanoparticles encapsulated by nitrogen-doped carbonaceous nanoleaves (CuCo-NC) have been synthesized from a Cu(OH)2 /2D leaf-like zeolitic imidazolate framework (ZIF-L)-pyrolysis approach. Leaf-like Cu(OH)2 is first prepared by the ultrasound-induced self-assembly of Cu(OH)2 nanowires. The efficient encapsulation of Cu(OH)2 in ZIF-L is obtained owing to the morphology fitting between the leaf-like Cu(OH)2 and ZIF-L. CuCo-NC catalysts present superior electrocatalytic activity and stability toward ORR and OER over the commercial Pt/C and IrO2 , respectively, which are further used as bifunctional oxygen electrocatalysts in Zn-air batteries and exhibit impressive performance, with a high peak power density of 303.7 mW cm-2 , large specific capacity of up to 751.4 mAh g-1 at 20 mA cm-2 , and a superior recharge stability.

14.
Org Biomol Chem ; 16(4): 645-651, 2018 01 24.
Artigo em Inglês | MEDLINE | ID: mdl-29303203

RESUMO

As a kind of biologically important reactive oxygen species (ROS), hypochlorite (ClO-) plays a crucial role in many physiological processes. As such, endogenous ClO- is a powerful antibacterial agent during pathogen invasion. Nonetheless, excessive endogenous ClO- could pose a health threat to mammalian animals including humans. However, the detection of endogenous ClO- by bioluminescence probes in vivo remains a considerable challenge. Herein, based on a caged strategy, we developed a turn-on bioluminescent probe 1 for the highly selective detection of ClO-in vitro and imaging endogenous ClO- in a mouse inflammation model. We anticipate that such a probe could help us understand the role of endogenous ClO- in a variety of physiological and pathological processes.


Assuntos
Luciferina de Vaga-Lumes/análogos & derivados , Ácido Hipocloroso/análise , Ácido Hipocloroso/metabolismo , Substâncias Luminescentes/química , Animais , Linhagem Celular Tumoral , Luciferina de Vaga-Lumes/síntese química , Luciferina de Vaga-Lumes/toxicidade , Humanos , Inflamação/induzido quimicamente , Inflamação/diagnóstico por imagem , Luciferases/química , Substâncias Luminescentes/síntese química , Substâncias Luminescentes/toxicidade , Masculino , Camundongos , Zimosan
15.
Org Biomol Chem ; 16(26): 4789-4792, 2018 07 04.
Artigo em Inglês | MEDLINE | ID: mdl-29926875

RESUMO

To develop a photoactivatable bioluminescence imaging technique, a set of high and efficient photoactivatable substrates for Renilla luciferase has been well designed and synthesized. Surprisingly, all of them could release the free luciferin that presented robust bioluminescent signals ex vivo and in living animals after UV irradiation at 365 nm.


Assuntos
Imidazóis/química , Luciferases de Renilla/análise , Substâncias Luminescentes/química , Imagem Óptica , Pirazinas/química , Animais , Imidazóis/síntese química , Luciferases de Renilla/metabolismo , Substâncias Luminescentes/síntese química , Medições Luminescentes , Camundongos , Camundongos Nus , Estrutura Molecular , Neoplasias Experimentais/diagnóstico por imagem , Processos Fotoquímicos , Pirazinas/síntese química , Especificidade por Substrato , Raios Ultravioleta
16.
Org Biomol Chem ; 15(48): 10238-10244, 2017 Dec 13.
Artigo em Inglês | MEDLINE | ID: mdl-29177293

RESUMO

The prodrug or caged-luciferin strategy affords an excellent platform for persistent bioluminescence imaging. In the current work, we designed and synthesized ten novel pro-substrates for Renilla luciferase by introducing ester protecting groups of different sizes into the carbonyl group of the free luciferin 1. Taking advantage of intracellular esterases, lipases, and nucleophilic substances, the ester protecting groups were hydrolyzed, resulting in the release of a free luciferin and a bioluminescence signal turn-on. Among the tested pro-substrates, the butyryloxymethyl luciferin 7 exhibited low cytotoxicity and a prolonged luminescence signal both in cellulo and in vivo. Therefore, the butyryloxymethyl luciferin 7 can act as a promising substrate for noninvasive extended imaging in diagnostic and therapeutic fields.


Assuntos
Luciferina de Vaga-Lumes/química , Luciferases/análise , Medições Luminescentes , Renilla/enzimologia , Animais , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Feminino , Luciferina de Vaga-Lumes/síntese química , Luciferina de Vaga-Lumes/farmacologia , Humanos , Luciferases/metabolismo , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Especificidade por Substrato
17.
Org Biomol Chem ; 14(43): 10267-10274, 2016 Nov 02.
Artigo em Inglês | MEDLINE | ID: mdl-27747358

RESUMO

The first dual bioluminescent and chemiluminescent sensor for detecting highly toxic thiophenols has been developed. Such a probe was designed by using a coelenterazine analogue as the luminophore and dinitrophenyl ether as the recognition moiety. It should be noted that this probe displayed good sensitivity and selectivity toward thiophenols, and has been effectively applied for the quantitative detection of thiophenols in aqueous media and complex biological samples.

18.
Bioorg Med Chem Lett ; 25(2): 259-61, 2015 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-25499881

RESUMO

2-(Indole-3-yl)-thiochroman-4-ones were synthesized via ionic liquid and tested for in vitro antifungal activity. The contribution of ionic liquid to Michael addition reaction is significant. Structures of all compounds are elucidated by (1)H NMR, (13)C NMR and HRMS. Most of these compounds showed better antifungal activity than fluconazole. The results suggest that 2-(indole-3-yl)-thiochroman-4-ones would be efficient antifungal agents.


Assuntos
Antifúngicos/síntese química , Antifúngicos/farmacologia , Fungos/efeitos dos fármacos , Indóis/síntese química , Indóis/farmacologia , Líquidos Iônicos , Indóis/química , Estrutura Molecular , Relação Estrutura-Atividade
19.
J Robot Surg ; 18(1): 221, 2024 May 23.
Artigo em Inglês | MEDLINE | ID: mdl-38780662

RESUMO

Intramedullary nail fixation of intertrochanteric fractures assisted by orthopedic surgical robot navigation is a new surgical method, but there are few studies comparing its efficacy with traditional intramedullary nail fixation. We aimed to assess whether robot-assisted internal fixation confers certain surgical advantages through a literature review. PubMed, EMBASE, Cochrane Library, China National Knowledge Infrastructure (CNKI) and Wan fang Data Knowledge service Platform were searched to collect randomized and non-randomized studies on patients with calcaneal fractures. Five studies were identified to compare the clinical indexes. For the clinical indexes, the technology of robot-assisted is generally feasible, in time to operation, intraoperative fluoroscopy times, blood loss, pine insertion, tip apex distance (TAD), and Harris score (P < 0.05). However, on the complication and excellent and good rate after operation did not show good efficacy compared with the traditional group (P > 0.05). Based on the current evidence, For the short-term clinical index, the advantages of robot-assisted are clear. The long-term clinical effects of the two methods are also good, but the robot-assisted shows better. However, the quality of some studies is low, and more high-quality randomized controlled trials (RCTs) are needed for further verification.


Assuntos
Fixação Intramedular de Fraturas , Fraturas do Quadril , Procedimentos Cirúrgicos Robóticos , Humanos , Procedimentos Cirúrgicos Robóticos/métodos , Fraturas do Quadril/cirurgia , Fixação Intramedular de Fraturas/métodos , Resultado do Tratamento , Duração da Cirurgia , Perda Sanguínea Cirúrgica/estatística & dados numéricos , Pinos Ortopédicos
20.
Bioorg Med Chem ; 21(24): 7624-7, 2013 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-24262885

RESUMO

In an effort to develop potent anti-cancer chemopreventive agents that act on topoisomerase II, a novel series of bisindolylalkanes analogues such as 3,3'-(thiochroman-4,4-diyl)bis(1H-indole) are synthesized. Structures of all compounds are elucidated by (1)H NMR, (13)C NMR and HRMS. Anti-proliferative activities for all of these compounds are investigated by the method of MTT assay on 7 human cancer lines. Most of them showed antitumor activities in vitro, the half maximal inhibitory concentration (IC50) value is 7.798 µg/mL of 3a against MCF7. Compound 3a showed comparable topoisomerase II inhibitory activity to etoposide (VP-16) at 100 µM concentration. The rest of the compounds also showed varying degree topoisomerase II inhibitory activity.


Assuntos
DNA Topoisomerases Tipo II/metabolismo , Indóis/farmacologia , Inibidores da Topoisomerase II/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Células Hep G2 , Humanos , Indóis/síntese química , Indóis/química , Concentração Inibidora 50 , Células MCF-7 , Estrutura Molecular , Relação Estrutura-Atividade , Inibidores da Topoisomerase II/síntese química , Inibidores da Topoisomerase II/química
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