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1.
Org Biomol Chem ; 2022 Jun 13.
Artigo em Inglês | MEDLINE | ID: mdl-35695281

RESUMO

Herein, we report a Rh(III)-catalyzed C4-selective activation of indoles by using iodonium ylides as carbene precursors. This protocol proceeded under redox neutral reaction conditions and provided important coupling products with good tolerance of functional groups and high yields. In addition, one-pot synthesis and scale-up and mechanistic studies were also conducted.

2.
Sci Rep ; 12(1): 6377, 2022 04 16.
Artigo em Inglês | MEDLINE | ID: mdl-35430598

RESUMO

Metabolic syndrome (MS) is a clinical syndrome with multiple metabolic disorders. As the diagnostic criteria for MS still lacking of imaging laboratory method, this study aimed to explore the differences between healthy people and MS patients through infrared thermography (IRT). However, the observation region of the IRT image is uncertain, and the research tried to solve this problem with the help of knowledge mining technology. 43 MS participants were randomly included through a cross-sectional method, and 43 healthy participants were recruited through number matching. The IRT image of each participant was segmented into the region of interest (ROI) through the preprocessing method proposed in this research, and then the ROI features were granulated by the K-means algorithm to generate the formal background, and finally, the two formal background were separately built into a knowledge graph through the knowledge mining method based on the attribute partial order structure. The baseline data shows that there is no difference in age, gender, and height between the two groups (P > 0.05). The image preprocessing method can segment the IRT image into 18 ROI. Through the K-means method, each group of data can be separately established with a 43 × 36 formal background and generated a knowledge graph. It can be found through knowledge mining and independent-samples T test that the average temperature and maximum temperature difference between the chest and face of the two groups are statistically different (P < 0.01). IRT could reflect the difference between healthy people and MS people. The measurement regions were found by the method of knowledge mining on the premise of unknown. The method proposed in this paper may add a new imaging method for MS laboratory examinations, and at the same time, through knowledge mining, it can also expand a new idea for clinical research of IRT.


Assuntos
Síndrome Metabólica , Termografia , Temperatura Corporal , Estudos Transversais , Humanos , Raios Infravermelhos , Síndrome Metabólica/diagnóstico por imagem , Temperatura , Termografia/métodos
3.
Org Biomol Chem ; 20(3): 565-569, 2022 01 19.
Artigo em Inglês | MEDLINE | ID: mdl-34985096

RESUMO

A thioether directed acyloxylation of arenes has been realized via Cp*Rh(III)-catalyzed C-H activation and subsequent coupling with carboxylic acids. This new method showed high functional group compatibility and broad substrate scope. Primary mechanistic studies have been conducted and a tentative reaction mechanism was proposed. It represents the first example of a thioether-directed Cp*Rh(III)-catalyzed C(sp2)-H acyloxylation reaction.

4.
Org Lett ; 23(15): 5719-5723, 2021 08 06.
Artigo em Inglês | MEDLINE | ID: mdl-34286981

RESUMO

A rhodium(III)-catalyzed C-H allylation of (hetero)arenes by using 2-methylidenetrimethylene carbonate as an efficient allylic source has been developed for the first time. Five different directing groups including oxime, N-nitroso, purine, pyridine, and pyrimidine were compatible, delivering various branched allylarenes bearing an allylic hydroxyl group in moderate to excellent yields.

5.
Vascul Pharmacol ; 138: 106860, 2021 06.
Artigo em Inglês | MEDLINE | ID: mdl-33794383

RESUMO

5-Hydroxytryptamine (5-HT)-dependent signaling mediated through its transporters and receptors plays important roles in chronic hypoxic pulmonary hypertension (CHPH), which is associated with aberrant reactive oxygen species (ROS) production. NADPH oxidase 4 (NOX4) is one of the major sources of ROS in pulmonary vasculature, and has been implicated in the development of PH. NOX4 generates H2O2, which can activate the transient receptor potential melastatin 2 (TRPM2) channels, providing Ca2+ signals for cell proliferation and migration. However, the connection between 5-HT, NOX4, ROS and TRPM2 in the context of PH has not been established. Here we examined the level of 5-HT and expression of NOX4 and TRPM2, and their roles in pulmonary arterial smooth muscle cells (PASMCs) proliferation and migration. NOX4 and TRPM2 were upregulated in pulmonary arteries of CHPH rats, which were associated with elevated levels of 5-HT and ROS, and enhanced proliferation and migration in PASMCs. The increase in ROS, and the enhanced proliferation and migration of PASMCs from CHPH rats were mimicked by treating normoxic PASMCs with 5-HT. 5-HT; and CH-induced ROS production were reversed by catalase, the NOX1/NOX4 inhibitor GKT137831, and Nox4 siRNA. 5-HT and H2O2 elicited Ca2+ responses were significantly augmented in CHPH PASMCs; and the augmented Ca2+ responses were obliterated by the 2-Aminoethoxydiphenyl borate (2-APB) and Trpm2-specific siRNA. Moreover, 5-HT and CH-induced proliferation and migration were suppressed by Nox4 or Trpm2 siRNA; and simultaneous transfection of both siRNA did not cause further inhibition. These results suggest that the 5-HT and CH-induced PASMC proliferation and migration were mediated, at least in part, by TRPM2 via activation of NOX4-dependent ROS production; and revealed a novel NOX4-ROS-TRPM2 signaling pathway for the pathogenesis of CHPH.


Assuntos
Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Músculo Liso Vascular/efeitos dos fármacos , Miócitos de Músculo Liso/efeitos dos fármacos , NADPH Oxidase 4/metabolismo , Hipertensão Arterial Pulmonar/enzimologia , Serotonina/farmacologia , Canais de Cátion TRPM/metabolismo , Animais , Sinalização do Cálcio , Células Cultivadas , Doença Crônica , Modelos Animais de Doenças , Hipóxia/complicações , Masculino , Músculo Liso Vascular/enzimologia , Músculo Liso Vascular/patologia , Músculo Liso Vascular/fisiopatologia , Miócitos de Músculo Liso/enzimologia , Miócitos de Músculo Liso/patologia , NADPH Oxidase 4/genética , Hipertensão Arterial Pulmonar/etiologia , Hipertensão Arterial Pulmonar/patologia , Hipertensão Arterial Pulmonar/fisiopatologia , Artéria Pulmonar/efeitos dos fármacos , Artéria Pulmonar/enzimologia , Artéria Pulmonar/patologia , Artéria Pulmonar/fisiopatologia , Ratos Sprague-Dawley , Espécies Reativas de Oxigênio/metabolismo , Serotonina/metabolismo , Canais de Cátion TRPM/genética , Remodelação Vascular/efeitos dos fármacos
6.
Mol Med Rep ; 18(1): 571-579, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-29750304

RESUMO

Vascular endothelial growth factor (VEGF) is expressed in articular cartilage and increases in expression levels have been associated with the progression of osteoarthritis (OA). Thalidomide is a drug that has been reported to inhibit angiogenesis and reduce VEGF production by downregulating VEGF expression. The objective of the present study was to determine whether intraperitoneal administration of thalidomide may attenuate early OA development in mice. Male C57BL/6 mice (10­weeks­old) were randomly assigned into the destabilization of the medial meniscus (Dmm) with thalidomide treatment (Dmm+Th), Dmm and Sham groups equally. An OA model was induced surgically in Dmm+Th and Dmm groups, and mice of the Dmm+Th group were subsequently treated with an intraperitoneal injection of thalidomide (200 mg/kg/day). At 2 and 4 weeks following surgery, the pathological alterations in cartilage samples were assessed qualitatively by hematoxylin and eosin staining and Safranin O/Fast green staining, and quantitatively by the Osteoarthritis Research Society International scoring system. The mRNA expression levels of matrix metalloproteinase­13 (MMP­13) and VEGF were measured by reverse transcription­quantitative polymerase chain reaction. The protein expression levels of MMP­13 and VEGF were detected by immunofluorescence and immunohistochemistry, respectively. The production of VEGF in serum was evaluated via an ELISA assay. Pathological scores were significantly higher in the Dmm and the Dmm+Th groups than those in the Sham group; however, the Dmm+Th group exhibited markedly less severe pathological changes compared with the Dmm group. Compared with the Sham group, the mRNA and protein expression levels of VEGF and MMP­13 in the Dmm and the Dmm+Th groups were significantly increased. The Dmm+Th group exhibited significantly decreased expression levels of VEGF and MMP­13, as well as significantly decreased serum VEGF concentration compared with the Dmm group. Thus, the results of the present study demonstrated that intraperitoneal administration of thalidomide may alleviate the development of early OA by suppressing VEGF expression in mice and may have potential as a novel therapy for the treatment of OA.


Assuntos
Meniscos Tibiais/efeitos dos fármacos , Osteoartrite/tratamento farmacológico , Talidomida/farmacologia , Fator A de Crescimento do Endotélio Vascular/genética , Animais , Modelos Animais de Doenças , Progressão da Doença , Regulação da Expressão Gênica , Injeções Intraperitoneais , Masculino , Metaloproteinase 13 da Matriz/genética , Meniscos Tibiais/metabolismo , Camundongos , Camundongos Endogâmicos C57BL , Osteoartrite/metabolismo , Talidomida/administração & dosagem , Talidomida/uso terapêutico
7.
Exp Mol Med ; 49(5): e332, 2017 05 19.
Artigo em Inglês | MEDLINE | ID: mdl-28524176

RESUMO

Our study aims to explore the effects of lentivirus-mediated microRNA-124 (miR-124) gene-modified bone marrow mesenchymal stem cell (BMSC) transplantation on the repair of spinal cord injury (SCI) in rats. BMSCs were isolated from the bone marrow of rats. The target gene miR-124 was identified using a luciferase-reporter gene assay. Seventy-two rats were selected for construction of the SCI model, and the rats were randomly divided into the blank group, sham group, SCI group, negative control (NC) group, overexpressed miR-124 group and si-PDXK group. The mRNA expression of miR-124 and the mRNA and protein expression of pyridoxal kinase (PDXK) were detected by quantitative real-time polymerase chain reaction and western blotting. The locomotor capacity of the rats was evaluated using the Basso, Beattie and Bresnahan (BBB) scale. Brdu, neuron-specific enolase (NSE), neurofilament (NF) and microtubule-associated protein 2 (MAP2) were detected using immunohistochemistry. The expression levels of thyrotropin-releasing hormone (TRH), prostacyclin (PGI2) and gangliosides (GM) were measured using an enzyme-linked immunosorbent assay. PDXK was identified as the target gene of miR-124. The overexpressed miR-124 group exhibited higher miR-124 expression than the SCI, NC and si-PDXK groups. Compared with the SCI and NC groups, the PDXK expression was downregulated in the overexpressed miR-124 and si-PDXK groups, and the BBB scores were significantly increased 7, 21 and 35 days after transplantation. The double-labeled positive cell densities (Brdu+NSE/NF/MAP2) and the expression levels of TRH, PGI2 and GM in the overexpressed miR-124 group were significantly higher than those in the NC and SCI groups. These results indicated that miR-124 targeted PDXK to accelerate the differentiation of BMSCs into neurocytes and promote SCI repair.


Assuntos
Transplante de Células-Tronco Mesenquimais/métodos , Células-Tronco Mesenquimais/metabolismo , MicroRNAs/genética , Terapêutica com RNAi , Traumatismos da Medula Espinal/terapia , Regeneração da Medula Espinal , Animais , Células Cultivadas , Epoprostenol/metabolismo , Gangliosídeos/metabolismo , Filamentos Intermediários/genética , Filamentos Intermediários/metabolismo , Lentivirus/genética , MicroRNAs/metabolismo , Proteínas Associadas aos Microtúbulos/genética , Proteínas Associadas aos Microtúbulos/metabolismo , Fosfopiruvato Hidratase/genética , Fosfopiruvato Hidratase/metabolismo , Piridoxal Quinase/genética , Piridoxal Quinase/metabolismo , Ratos , Ratos Sprague-Dawley , Hormônio Liberador de Tireotropina/metabolismo
8.
Sensors (Basel) ; 17(1)2017 Jan 13.
Artigo em Inglês | MEDLINE | ID: mdl-28098774

RESUMO

This paper proposes a computer-aided cirrhosis diagnosis system to diagnose cirrhosis based on ultrasound images. We first propose a method to extract a liver capsule on an ultrasound image, then, based on the extracted liver capsule, we fine-tune a deep convolutional neural network (CNN) model to extract features from the image patches cropped around the liver capsules. Finally, a trained support vector machine (SVM) classifier is applied to classify the sample into normal or abnormal cases. Experimental results show that the proposed method can effectively extract the liver capsules and accurately classify the ultrasound images.


Assuntos
Cirrose Hepática , Humanos , Redes Neurais de Computação , Máquina de Vetores de Suporte , Ultrassonografia
9.
Guang Pu Xue Yu Guang Pu Fen Xi ; 32(3): 647-50, 2012 Mar.
Artigo em Chinês | MEDLINE | ID: mdl-22582624

RESUMO

The skin temperature distribution of a healthy human body exhibits a contralateral symmetry. Some lesions of facial nerve function are associated with an alteration of the thermal distribution of the human body. Since the dissipation of heat through the skin occurs for the most part in the form of infrared radiation, infrared thermography is the method of choice to capture the alteration of the infrared thermal distribution. This paper presents a new method of analysis of the thermal asymmetry named effective thermal area ratio, which is a product of two variables. The first variable is mean temperature difference between the specific facial region and its contralateral region. The second variable is a ratio, which is equal to the area of the abnormal region divided by the total area. Using this new method, we performed a controlled trial to assess the facial nerve function of the healthy subjects and the patients with Bell's palsy respectively. The results show: that the mean specificity and sensitivity of this method are 0.90 and 0.87 respectively, improved by 7% and 26% compared with conventional methods. Spearman correlation coefficient between effective thermal area ratio and the degree of facial nerve function is an average of 0.664. Hence, concerning the diagnosis and assessment of facial nerve function, infrared thermography is a powerful tool; while the effective ther mal area ratio is an efficient clinical indicator.


Assuntos
Paralisia de Bell/fisiopatologia , Nervo Facial/patologia , Espectrofotometria Infravermelho , Estudos de Casos e Controles , Paralisia Facial , Humanos , Pele
10.
Guang Pu Xue Yu Guang Pu Fen Xi ; 32(11): 2939-45, 2012 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-23387154

RESUMO

Intra-operation monitoring depth of anesthesia is an important method to insure the quality and safety of clinical anesthesia. As a noninvasive brain function monitoring technology, functional near-infrared spectroscopy can provide objective and reliable brain activity monitoring and imaging in real time. The characteristic of this technique is highly suitable for interrelated research on depth of anesthesia monitoring. The present paper briefly introduced the fundamental and instruments of functional near-infrared spectroscopy, reviewed the current situation about the application of functional near-infrared spectroscopy in research on depth of anesthesia monitoring, pointed out the possible way of using functional near-infrared spectroscopy in depth of anesthesia monitoring research, and expounded the unsolved problems and future prospects.


Assuntos
Anestesia , Encéfalo/fisiologia , Neuroimagem Funcional , Monitorização Intraoperatória/instrumentação , Espectroscopia de Luz Próxima ao Infravermelho/métodos , Algoritmos , Encéfalo/efeitos dos fármacos , Humanos , Monitorização Intraoperatória/métodos
11.
Zhongguo Zhen Jiu ; 29(1): 7-9, 2009 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-19186713

RESUMO

OBJECTIVE: To observe the influence of different frequencies of acupuncture on the therapeutic effect in patients with cerebral infarction at convalescence. METHODS: Ninety-seven cases were randomly divided into an observation group I (n = 50) and an observation group II (n = 47). They were treated with same Chinese drugs and western medicine and electroacupuncture at Jiquan (HT 1), Quchi (LI 11), Hegu (LI 4), Huantiao (GB 30), etc. The observation group I was treated twice each day and the observation group II once each day. After treatment of 30 days, their therapeutic effects were observed. RESULTS: The total effective rate of 94.0% for improvement of limb activity in the observation group I was better than 78.7% in the observation group II (P < 0.05); the therapeutic effects for choking when taking water, dysphagia, vague mind and slurred speech were similar in the two groups (P > 0.05). CONCLUSION: The therapeutic effect of acupuncture twice each day on cerebral infarction at convalescence is superior to that of once daily.


Assuntos
Terapia por Acupuntura , Infarto Cerebral/terapia , Convalescença , Terapia por Acupuntura/métodos , Adulto , Idoso , Infarto Cerebral/tratamento farmacológico , Infarto Cerebral/fisiopatologia , Terapia Combinada , Medicamentos de Ervas Chinesas/uso terapêutico , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Resultado do Tratamento
12.
Zhongguo Zhen Jiu ; 26(3): 227-9, 2006 Mar.
Artigo em Chinês | MEDLINE | ID: mdl-16570452

RESUMO

In recent years, the studies on moxibustion for treatment of cancer are increasing day by day, with some advances. In the paper, clinical and experimental studies on traditional moxibustion for treatment of cancer and the mechanisms are reviewed, and some problems and shortcomings are put forward.


Assuntos
Terapia por Acupuntura , Moxibustão , Humanos , Neoplasias
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