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1.
Eur Radiol ; 34(1): 715-723, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-37581653

RESUMO

OBJECTIVES: Microwave ablation (MWA) has achieved excellent long-term efficacy in treating unifocal papillary thyroid microcarcinoma (UPTMC). The therapeutic effect of this treatment on multifocal papillary thyroid microcarcinoma (MPTMC) is unknown. Therefore, we evaluated the long-term efficacy of MWA for low-risk MPTMC and to provide evidence-based medicine for the revision of clinical guidelines. METHODS: This study included 66 MPTMC patients with a total of 158 lesions, all of whom received MWA. We collected and retrospectively analyzed the patients' follow-up data before MWA, at 1, 3, 6, and 12 months posttreatment and every 6 months thereafter until 5 years posttreatment. We evaluated the MWA complication rate, technical success rate (TSR), lesion volume reduction rate (VRR), and complete disappearance rate (CDR) during follow-up and in those patients with tumor progression and delayed surgery. RESULTS: After 60 months of follow-up, all 158 lesions disappeared in 66 patients, and the volume was reduced from 43.82 mm3 to 0.00 mm3. The TSR and VRR were both 100%. The CDRs at 1 year, 2 years, and 3 years were 57.59%, 93.67%, and 100%, respectively. The complication rate was 3.03% (2/66), and the incidence of tumor progression was 3.03% (2/66), including one new intrathyroidal lesion and one cervical lymph node metastasis (LNM). These lesions were retreated with MWA, and the lesions disappeared during the follow-up period. CONCLUSIONS: Ultrasound-guided MWA for low-risk MPTMC is safe and effective and may serve as an alternative option for patients who refuse surgery or active surveillance (AS). CLINICAL RELEVANCE STATEMENT: This study concludes that ultrasound-guided microwave ablation for low-risk multifocal papillary thyroid microcarcinoma is safe and effective and may serve as an alternative option for patients who refuse surgery or active surveillance. KEY POINTS: • Ultrasound-guided microwave ablation for low-risk multifocal papillary thyroid microcarcinoma is safe and effective. • During 5 years of follow-up, multifocal papillary thyroid microcarcinoma patients treated with microwave ablation had a favorable prognosis. • To provide evidence-based medicine for the revision of clinical guidelines.


Assuntos
Carcinoma Papilar , Micro-Ondas , Neoplasias da Glândula Tireoide , Humanos , Seguimentos , Micro-Ondas/uso terapêutico , Estudos Retrospectivos , Neoplasias da Glândula Tireoide/diagnóstico por imagem , Neoplasias da Glândula Tireoide/cirurgia , Neoplasias da Glândula Tireoide/patologia , Resultado do Tratamento , Ultrassonografia de Intervenção
2.
Chem Pharm Bull (Tokyo) ; 72(2): 186-189, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38346722

RESUMO

As a part of our continuing exploration to discover new potential promising fungicide candidates, eighteen sulfonate derivatives (3a-3r) containing a kakuol moiety were designed and synthesized. Synthetic sulfonate derivatives were tested comprehensively for antifungal activities against four plant pathogenic fungi (Botrytis (B.) cinerea, Valsa (V.) mali, Fusarium (F.) graminearum, Sclerotinia (S.) sclerotiorum), and their structure activity relationships were summarized. Especially, derivatives 3i and 3j exhibited remarkable activity against V. mali, with the inhibition rates of 99.8 and 100%, which were slightly superior to that of carbendazim (98.9%), a reference fungicide. Moreover, derivatives 3a, 3k and 3q possess the broader antifungal spectrum against three tested plant pathogenic fungi with inhibition rates over 60%. Structure-activity relationship (SAR) analysis indicated that the introduction of 2-F or 3-F into the benzene ring would give rise to a remarkable increase of the antifungal activity against V. mali.


Assuntos
Ascomicetos , Benzodioxóis , Fungicidas Industriais , Propiofenonas , Antifúngicos/química , Fungicidas Industriais/farmacologia , Estrutura Molecular , Relação Estrutura-Atividade , Plantas
3.
Eur Radiol ; 33(4): 2407-2414, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-36472698

RESUMO

OBJECTIVES: To investigate the value of contrast-enhanced ultrasound (CEUS) combined with feeding artery ablation in the microwave ablation (MWA) of large solid benign thyroid nodules (LSBTNs) with a diameter ≥ 4 cm. METHODS: We retrospectively analyzed 122 patients with LSBTN ≥ 4 cm in diameter treated with MWA. During evaluations before and after MWA, 53 patients who underwent conventional ultrasound examination were classified as the routine group, and 69 patients who underwent CEUS combined with feeding artery ablation were classified as the union group. The differences in ablation energy required per milliliter (AERPM), complication rate, regrowth rate, and volume reduction rate (VRR) were compared between the two groups. RESULTS: The AERPM of the union group was significantly less than that of the routine group (956.3 ± 38.5 J/mL vs. 1025.9 ± 121.5 J/mL, p < 0.001). The complication rate of the routine group was significantly higher than that of the union group (13.2% vs. 2.9%, p = 0.031). The regrowth rate of the routine group (22.6%, 12/53) was significantly higher than that of the union group (7.2%, 5/69) (p = 0.015). At the 1st, 3rd, 6th, 12th, 18th, and 24th month after ablation, the mean VRRs of the routine group were significantly less than those of the union group, with p values of < 0.001, < 0.001, 0.002, 0.007, 0.013, and < 0.001, respectively. CONCLUSIONS: The application of CEUS combined with feeding artery ablation in the MWA of LSBTNs is helpful to reduce the regrowth rate, improve the ablation efficiency, and reduce bleeding. KEY POINTS: • CEUS combined with feeding artery ablation in MWA of LSBTNs is helpful to reduce regrowth rate. • CEUS combined with feeding artery ablation can help improve ablation efficiency than conventional ultrasound in LSBTNs. • CEUS combined with feeding artery ablation helps reduce the incidence of bleeding during MWA.


Assuntos
Ablação por Cateter , Nódulo da Glândula Tireoide , Humanos , Nódulo da Glândula Tireoide/diagnóstico por imagem , Nódulo da Glândula Tireoide/cirurgia , Micro-Ondas/uso terapêutico , Estudos Retrospectivos , Resultado do Tratamento , Artérias
4.
J Minim Invasive Gynecol ; 30(4): 290-299, 2023 04.
Artigo em Inglês | MEDLINE | ID: mdl-36563871

RESUMO

STUDY OBJECTIVE: To evaluate the effectiveness and safety of ultrasound-guided percutaneous microwave ablation (MWA) for a single uterine fibroid greater than 300 cm3. DESIGN: Retrospective observational study. SETTING: China-Japan Union Hospital of Jilin University, China. PATIENTS: Thirty-seven patients each with a single fibroid greater than 300 cm3 diagnosed by ultrasound and core needle biopsy. INTERVENTIONS: Ultrasound-guided percutaneous MWA. MEASUREMENTS AND MAIN RESULTS: All patients were followed up for 12 months postoperatively to assess the postoperative lesion volume reduction rate, degree of symptomatic relief, improvements in quality of life, and occurrence of adverse events. All 37 patients met the criteria for complete ablation, and the lesion volume significantly decreased from 334.28 cm3 (95% confidence interval [CI] 326.75-366.73) preoperatively to 52.01 cm3 (95% CI, 46.95-74.69) at the 12-month follow-up (difference: 280.15 cm3; 95% CI, 267.92-294.65; p <.001). The lesion volume reduction rates at 1, 3, 6, and 12 months postoperatively were 27.30% (95% CI, 24.12-31.45), 52.90% (95% CI, 47.95-55.80), 67.90% (95% CI, 63.03-70.77), and 84.00% (95% CI, 80.22-85.94), respectively. The differences in the preoperative and postoperative Uterine Fibroid Symptom and Health-Related Quality of Life Questionnaire scores were significant (p <.01). The hemoglobin levels of the anemic patients were significantly elevated after the procedure (p <.001). Of the 37 patients in this study, 29 patients (78.38%) had a highly significant treatment effect, and 8 patients (21.62%) had a significant treatment effect. Seventeen patients (45.95%) had Society of Interventional Radiology grade A to B adverse effects that required no clinical intervention or only simple clinical intervention. CONCLUSION: Ultrasound-guided percutaneous MWA has good clinical efficacy and high safety in the treatment of a single uterine fibroid greater than 300 cm3.


Assuntos
Técnicas de Ablação Endometrial , Ablação por Ultrassom Focalizado de Alta Intensidade , Leiomioma , Neoplasias Uterinas , Feminino , Humanos , Ablação por Ultrassom Focalizado de Alta Intensidade/métodos , Leiomioma/diagnóstico por imagem , Leiomioma/cirurgia , Leiomioma/patologia , Micro-Ondas/uso terapêutico , Qualidade de Vida , Resultado do Tratamento , Ultrassonografia de Intervenção , Neoplasias Uterinas/diagnóstico por imagem , Neoplasias Uterinas/cirurgia , Neoplasias Uterinas/patologia , Estudos Retrospectivos
5.
Entropy (Basel) ; 25(5)2023 May 17.
Artigo em Inglês | MEDLINE | ID: mdl-37238564

RESUMO

Deep learning methods, especially convolutional neural networks (CNNs), have achieved good results in the partial discharge (PD) diagnosis of gas-insulated switchgear (GIS) in the laboratory. However, the relationship of features ignored in CNNs and the heavy dependance on the amount of sample data make it difficult for the model developed in the laboratory to achieve high-precision, robust diagnosis of PD in the field. To solve these problems, a subdomain adaptation capsule network (SACN) is adopted for PD diagnosis in GIS. First, the feature information is effectively extracted by using a capsule network, which improves feature representation. Then, subdomain adaptation transfer learning is used to accomplish high diagnosis performance on the field data, which alleviates the confusion of different subdomains and matches the local distribution at the subdomain level. Experimental results demonstrate that the accuracy of the SACN in this study reaches 93.75% on the field data. The SACN has better performance than traditional deep learning methods, indicating that the SACN has potential application value in PD diagnosis of GIS.

6.
Bioorg Med Chem ; 29: 115895, 2021 01 01.
Artigo em Inglês | MEDLINE | ID: mdl-33271454

RESUMO

Aurones are naturally occurring structural isomerides of flavones that have diverse bioactivities including antiviral, antibacterial, antifungal, anti-inflammatory, antitumor, antimalarial, antioxidant, neuropharmacological activities and so on. They constitute an important class of pharmacologically active scaffolds that exhibit multiple biological activities via diverse mechanisms. This review article provides an update on the recent advances (2013-2020.4) in the synthesis and biological activities of these derivatives. In the cases where sufficient information is available, some important structure-activity relationships (SAR) of their biological activities were presented, and on the strength of our expertise in medicinal chemistry and careful analysis of the recent literature, for the potential of aurones as medicinal drugs is proposed.


Assuntos
Anti-Infecciosos/síntese química , Anti-Inflamatórios/síntese química , Antinematódeos/síntese química , Antineoplásicos/síntese química , Antioxidantes/síntese química , Benzofuranos/síntese química , Hipoglicemiantes/síntese química , Doença de Alzheimer/tratamento farmacológico , Animais , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/farmacologia , Antinematódeos/farmacologia , Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Benzofuranos/farmacologia , Catálise , Avaliação Pré-Clínica de Medicamentos , Flavonas/química , Humanos , Hipoglicemiantes/farmacologia , Metais/química , Relação Estrutura-Atividade
7.
J Cell Physiol ; 235(10): 6615-6624, 2020 10.
Artigo em Inglês | MEDLINE | ID: mdl-32048306

RESUMO

Small nucleolar RNA host gene 3 (SNHG3) is a long noncoding RNA (lncRNA), which is known to promote oncogenesis in many cancers but its role in human papillary thyroid carcinoma (PTC) remains poorly understood. We therefore assessed SNHG3 expression in PTC tissues via quantitative reverse transcription polymerase chain reaction. We additionally knocked down SNHG3 in PTC cells using short-hairpin RNAs (shRNAs) to explore its functional roles in PTC. The ability of SNHG3 to bind to specific microRNAs (miRNAs) was predicted using a bioinformatics tool, and this binding was confirmed via dual-luciferase reporter and RNA immunoprecipitation (RIP) assays. We then used a tumor xenograft model to assess the relevance of SNHG3 in vivo. We determined SNHG3 expression to be elevated in PTC tissues relative to controls, with advanced tumor-node-metastasis stage and lymph node metastasis being associated with this expression. Knocking down SNHG3 significantly reduced in vitro PTC cell migration, invasion, proliferation, and colony formation, and it further slowed the growth of tumors in vivo. We found that SNHG3 could bind to miR-214-3p as a competing endogenous RNA (ceRNA) for this miRNA, thereby regulating proteasome 26S subunit non-ATPase 10 (PSMD10) expression, a miR-214-3p target. These results thus indicate that SNHG3 is an oncogenic lncRNA in PTC, acting at least in part via the miR-214-3p/PSMD10 axis.


Assuntos
MicroRNAs/genética , Complexo de Endopeptidases do Proteassoma/genética , Proteínas Proto-Oncogênicas/genética , RNA Longo não Codificante/genética , Câncer Papilífero da Tireoide/genética , Neoplasias da Glândula Tireoide/genética , Animais , Carcinogênese/genética , Linhagem Celular , Movimento Celular/genética , Proliferação de Células/genética , Progressão da Doença , Feminino , Regulação Neoplásica da Expressão Gênica/genética , Humanos , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Pessoa de Meia-Idade , RNA Interferente Pequeno/genética , Câncer Papilífero da Tireoide/patologia , Neoplasias da Glândula Tireoide/patologia
8.
Bioorg Med Chem Lett ; 30(1): 126774, 2020 01 01.
Artigo em Inglês | MEDLINE | ID: mdl-31685339

RESUMO

In continuation of our program to discover new potential antifungal agents, a series of amide and imine derivatives containing a kakuol moiety were synthesized and characterized by the spectroscopic analysis. By using the mycelium growth rate method, the target compounds were evaluated systematically for antifungal activities in vitro against four plant pathogenic fungi, and structure-activity relationships (SAR) were derived. Compounds 7d, 7e, 7h, 7i and 7r showed obvious inhibitory activity against the corresponding tested fungi at 50 µg/mL. Especially, compounds 7e and 7r displayed more potent antifungal activity against B. cinerea than that of thiabendazole (a positive control). Moreover, compound 7e also exhibited good activity against A. alternata with EC50 values of 11.0 µg/mL, and the value was slightly superior to that of thiabendazole (EC50 = 14.9 µg/mL). SAR analysis showed that the ether group was a highly sensitive structural moiety to the activity and the type as well as position of substituents on benzene ring could make some effects on the activity.


Assuntos
Amidas/síntese química , Antifúngicos/uso terapêutico , Benzodioxóis/síntese química , Iminas/síntese química , Propiofenonas/síntese química , Amidas/uso terapêutico , Antifúngicos/farmacologia , Benzodioxóis/uso terapêutico , Humanos , Iminas/uso terapêutico , Estrutura Molecular , Propiofenonas/uso terapêutico , Relação Estrutura-Atividade
9.
J Cell Mol Med ; 23(9): 5907-5919, 2019 09.
Artigo em Inglês | MEDLINE | ID: mdl-31304680

RESUMO

Thyroid cancer (TC) is a prevalent endocrine malignant cancer whose pathogenic mechanism remains unclear. The aim of the study was to investigate the roles of long non-coding RNA (lncRNA) NR2F1-AS1/miRNA-338-3P/CCND1 axis in TC progression. Differentially expressed lncRNAs and mRNAs in TC tissues were screened out and visualized by R program. Relative expression of NR2F1-AS1, miRNA-338-3p and cyclin D1 (CCND1) was determined by quantitative real time polymerase chain reaction. In addition, Western blot analysis was adopted for evaluation of protein expression of CCND1. Targeted relationships between NR2F1-AS1 and miRNA-338-3p, as well as miRNA-338-3p and CCND1 were predicted using bioinformatics analysis and validated by dual-luciferase reporter gene assay. Besides, tumour xenograft assay was adopted for verification of the role of NR2F1-AS1 in TC in vivo. NR2F1-AS1 and CCND1 were overexpressed, whereas miRNA-338-3p was down-regulated in TC tissues and cell lines. Down-regulation of NR2F1-AS1 and CCND1 suppressed proliferation and migration of TC cells yet greatly enhanced cell apoptotic rate. Silence of NR2F1-AS1 significantly suppressed TC tumorigenesis in vivo. NR2F1-AS1 sponged miRNA-338-3p to up-regulate CCND1 expression to promote TC progression. Our study demonstrated that up-regulation of NR2F1-AS1 accelerated TC progression through regulating miRNA-338-3P/CCND1 axis.


Assuntos
Ciclina D1/metabolismo , MicroRNAs/genética , RNA Longo não Codificante/genética , Neoplasias da Glândula Tireoide/genética , Neoplasias da Glândula Tireoide/patologia , Animais , Apoptose/genética , Linhagem Celular Tumoral , Movimento Celular/genética , Proliferação de Células/genética , Progressão da Doença , Regulação Neoplásica da Expressão Gênica/genética , Humanos , Camundongos , Camundongos Nus , Transplante de Neoplasias , Interferência de RNA , RNA Interferente Pequeno/genética , Glândula Tireoide/patologia , Transplante Heterólogo
10.
J Cell Mol Med ; 23(3): 1865-1872, 2019 03.
Artigo em Inglês | MEDLINE | ID: mdl-30565392

RESUMO

The long intergenic non-protein coding RNA regulator of reprogramming (lncRNA-ROR) has been reported to play crucial regulatory roles in the pathogenesis and progression of multiple cancers. However, whether ROR is associated with the initiation and development of osteosarcoma (OS) remains unclear. Here, we found that ROR expression level was significantly up-regulated in OS tissue samples compared to adjacent normal tissues, and the elevated ROR was closely correlated with advanced tumour-node-metastasis (TNM) stage and lymph node metastasis and poor overall survival rate. Functional assays showed that ROR knockdown suppressed the OS cell proliferation, colony formation, migration and invasion in vitro, and retarded tumour growth in vivo. In addition, miR-206 was verified to be a target miRNA of ROR using bioinformatics online program and luciferase report assay. miR-206 inhibition partially rescued the inhibitory effects on OS cells induced by ROR knockdown. In conclusion, these results suggested that ROR function as an oncogene in OS by sponging miR-206 and might be a potential therapeutic target for patients with OS.


Assuntos
Biomarcadores Tumorais/genética , Neoplasias Ósseas/patologia , Regulação Neoplásica da Expressão Gênica , MicroRNAs/genética , Osteossarcoma/patologia , RNA Longo não Codificante/genética , Adulto , Animais , Apoptose , Neoplasias Ósseas/genética , Neoplasias Ósseas/metabolismo , Movimento Celular , Proliferação de Células , Progressão da Doença , Feminino , Humanos , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Osteossarcoma/genética , Osteossarcoma/metabolismo , Prognóstico , Taxa de Sobrevida , Células Tumorais Cultivadas , Ensaios Antitumorais Modelo de Xenoenxerto , Adulto Jovem
11.
Clin Exp Pharmacol Physiol ; 46(2): 144-152, 2019 02.
Artigo em Inglês | MEDLINE | ID: mdl-30353914

RESUMO

YWHAZ (14-3-3ζ) plays crucial roles in regulating proliferation, apoptosis, migration, and invasion of gastric cancer (GC) cells. However, its extensive roles and potential mechanisms in GC cells remain unknown, and need to be researched deeply. In this study, we focus on the role of miR-375/YWHAZ axis in migration, invasion and epithelial-to-mesenchymal transition (EMT) of GC cells. YWHAZ level was assessed by western blot and qPCR assays in GC cells. Scratch and transwell assays were used to determine the migration and invasion of GC cells. The protein levels of correlative molecules were detected by western blot. The regulation of miR-375 on the expression of its target gene YWHAZ was verified by dual-luciferase report system. According to the results, knockdown of YWHAZ inhibited the migration, invasion and EMT of GC cells. Moreover, silencing of YWHAZ restrained the activation of wnt/ß-catenin signalling pathway. YWHAZ was confirmed to be a target gene of miR-375, and its expression was regulated by miR-375 in GC cells. Transfection of miR-375 inhibitor promoted the migration, invasion, EMT and activation of wnt/ß-catenin pathway in GC cells, which was suppressed by inhibition of YWHAZ. Taken together, this study suggests that miR-375/YWHAZ axis may be served as a novel therapeutic target for GC patients.


Assuntos
Proteínas 14-3-3/metabolismo , Movimento Celular/genética , Transição Epitelial-Mesenquimal/genética , MicroRNAs/genética , Neoplasias Gástricas/patologia , beta Catenina/metabolismo , Proteínas 14-3-3/deficiência , Proteínas 14-3-3/genética , Linhagem Celular Tumoral , Técnicas de Silenciamento de Genes , Inativação Gênica , Humanos , Invasividade Neoplásica , Via de Sinalização Wnt/genética
12.
Int J Hyperthermia ; 35(1): 450-462, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30354777

RESUMO

PURPOSE: It is unclear which kind of interventional therapies is the best when treating early-stage hepatocellular carcinoma (HCC). We conducted Bayesian network meta-analyses to compare local tumor progression (LTP), total tumor recurrence and survival rates and to rank the best intervention arm. MATERIALS AND METHODS: A literature search of Pubmed, Embase, Cochrane library and Clinicaltrials.gov was conducted and randomized controlled trials (RCTs) comparing the outcomes of interventional therapies on early-stage HCC were enrolled. The quality assessment was conducted using Cochrane Collaboration's tool, while the outcome synthesis of the network meta-analysis was conducted using R-3.3.4 software. RESULTS: A total of 35 RCTs were enrolled for further analysis. Using network meta-analysis, it was demonstrated that radiofrequency ablation (RFA) plus adjuvant therapies achieved the best performance in decreasing the LTP rate in early-stage HCC, while hepatic resection ranked as the best arm among all the interventional techniques for LTP at 3 years. Meanwhile, hepatic resection and RFA plus adjuvant therapies were the top two best arms in decreasing total recurrence. Furthermore, RFA plus adjuvant therapeutics ranked the best in achieving overall survival outcome, followed by hepatic resection. For disease-free survival, hepatic resection was the best, while for LTP-free survival, the difference among the included treatments was not significant. CONCLUSIONS: Our network meta-analysis showed that RFA-based adjuvant therapies might be the most effective interventions in achieving the best outcomes, while hepatic resection exhibited the best performance in several situations in treating early-stage HCC. More RCTs are needed to draw more solid conclusions.


Assuntos
Carcinoma Hepatocelular/terapia , Neoplasias Hepáticas/terapia , Idoso , Carcinoma Hepatocelular/patologia , Feminino , Humanos , Neoplasias Hepáticas/patologia , Masculino , Pessoa de Meia-Idade , Estadiamento de Neoplasias , Metanálise em Rede , Prognóstico , Resultado do Tratamento
13.
Chem Pharm Bull (Tokyo) ; 65(1): 82-89, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28049918

RESUMO

As a part of our continuing research on amine derivative antifungal agents, 19 novel target compounds containing 1,2,4-triazole and tertiary amine moieties were designed and synthesized, and their in vitro antifungal activities against six phytopathogenic fungi (Magnaporthe grisea, Alternaria solani, Fusarium solani, Curvularia lunata, A. alternata, F. graminearum) were assayed. All target compounds were elucidated by means of 1H-NMR, 13C-NMR, high resolution (HR)-MS, and IR analysis. The results showed that most of the derivatives exhibited obvious activity against each of the fungi at 50 µg/mL. Among them, compounds 7f, l, and o displayed excellent activity against A. solani with median effective concentration values (EC50) of 2.88, 8.20, and 1.92 µg/mL. 7o in particular was superior to tebuconazole (EC50=2.03 µg/mL), a commercial fungicide. Furthermore, compounds 7j, k, and m also showed good activity against F. graminearum with EC50 values of 11.60, 5.14, and 16.24 µg/mL, and the value of 7k was extremely close to that of tebuconazole (EC50=3.13 µg/mL). The preliminary analysis of the structure-activity relationship (SAR) demonstrated that combination of the active structure of 1,2,4-triazole with the tertiary amine group containing benzene rings effectively increased the antifungal activities. Generally, introducing halogen atoms obviously improved activities against most of the test fungi to varying degrees, while the presence of OMe decreased the activities. Thus, the results strongly indicate that the newly synthesized derivatives should be lead compounds for the development of novel antifungal agents for the effective control of phytopathogenic fungi.


Assuntos
Aminas/farmacologia , Antifúngicos/farmacologia , Desenho de Fármacos , Ergosterol/biossíntese , Triazóis/farmacologia , Aminas/síntese química , Aminas/química , Antifúngicos/síntese química , Antifúngicos/química , Relação Dose-Resposta a Droga , Fungos/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade , Triazóis/química
14.
Chem Pharm Bull (Tokyo) ; 64(6): 616-24, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27250796

RESUMO

The study reported the synthesis and antifungal activities in vitro against six phytopathogenic fungi of 17 novel N-[2-hydroxy-3,3-dimethyl-2-[(1H-1,2,4-triazol-1-yl)methyl]butyl]benzamide derivatives. All the target compounds were synthesized and elucidated by means of MS, high resolution (HR)-MS, IR, (1)H- and (13)C-NMR analysis. The results showed that almost all the derivatives exhibited good activities against each of the tested fungi at the concentration of 50 µg/mL. Among them, 6h displayed excellent activity against Alternaria alternata with the median effective concentration value (EC50) of 1.77 µg/mL, superior to myclobutanil (EC50=6.23 µg/mL), a commercial fungicide with broad-spectrum bioactivities for plant protection and high-efficiency. Compound 6k showed the broadest antifungal spectrum, demonstrating positive activities against the corresponding fungi with EC50 values ranging from 0.98 to 6.71 µg/mL. Furthermore, 6e to 6i revealed good activities against Alternaria solani with EC50 values of 1.90, 4.51, 7.07, 2.00 and 5.44 µg/mL, respectively. The preliminary analysis of structure-activity relationship (SAR) demonstrated that the presence of F or Cl on the benzene ring remarkably improved the activity, while the introduction of 4-OMe or CF3 group decreased the activity in varying degrees. Thus, the present results strongly suggest that N-[2-hydroxy-3,3-dimethyl-2-[(1H-1,2,4-triazol-1-yl)methyl]butyl]benzamide derivatives should be promising candidates for the development of novel antifungal agents in the effective control of phytopathogenic fungi.


Assuntos
Antifúngicos/farmacologia , Benzamidas/farmacologia , Fungos/efeitos dos fármacos , Triazóis/farmacologia , Antifúngicos/síntese química , Antifúngicos/química , Benzamidas/síntese química , Benzamidas/química , Relação Dose-Resposta a Droga , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade , Triazóis/química
15.
Pak J Med Sci ; 31(5): 1152-5, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26649004

RESUMO

OBJECTIVE: The aim of this study was to explore the diagnostic value of ultrasound-guided (US-guided) fine-needle aspiration cytology (FNAC), thyroglobulin measurement on fine-needle aspiration (FNA-Tg), combined US-guided FNAC, and the ratio between FNA-Tg and serum Tg (FNA-Tg/serum Tg) for patients with cervical lymph node (CLN) metastases from thyroid carcinoma. METHODS: We selected 148 patients with thyroid cancer with suspicious CLN metastases who met the inclusion criteria. FNAC findings, FNA-Tg levels, and serum Tg levels were evaluated before surgical treatment. The results of FNAC and FNA-Tg from CLNs were analyzed retrospectively. RESULTS: Ninety-four of 148 cases were metastatic and 54 were benign. The sensitivity, specificity, and accuracy of FNAC were 68.1%, 100.0%, and 79.7%, respectively. The sensitivity, specificity, and accuracy of FNA-Tg/serum Tg were 91.5%, 88.9%, and 90.5%, respectively. The sensitivity, specificity, and accuracy of FNA-Tg [10 ng/mL] were 98.9%, 68.5%, and 87.8%, respectively. The sensitivity, specificity, and accuracy of combined US-guided FNAC and FNA-Tg/serum Tg were 95.7%, 96.3%, and 95.9%, respectively. There was a statistically significant difference between FNAC and combined US-guided FNAC and FNA-Tg/serum Tg for sensitivity, specificity, and accuracy (P < 0.05). CONCLUSION: The method of FNA-Tg/serum Tg is sensitive enough for diagnosing CLN metastases from thyroid cancer. The combined application of US-guided FNAC and FNA-Tg/serum Tg contributes to improving the accuracy of diagnosing CLN metastases in patients with thyroid cancer.

16.
J Sep Sci ; 37(23): 3443-50, 2014 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-25215879

RESUMO

Recycling high-speed counter-current chromatography was successfully applied to the preparative separation of oxybutynin enantiomers. The two-phase solvent system consisted of n-hexane, methyl tert-butyl ether, and 0.1 mol/L phosphate buffer solution (pH = 5.0) with the volume ratio of 6:4:10. Hydroxypropyl-ß-cyclodextrin was employed as the chiral selector. The influence of factors on the chiral separation process, including the concentration of chiral selector, the equilibrium temperature, the pH value of the aqueous phase were investigated. Under optimum separation conditions, 15 mg of oxybutynin racemate was separated with the purities of both the enantiomers over 96.5% determined by high-performance liquid chromatography. Recovery for the target compounds reached 80-82% yielding 6.00 mg of (R)-oxybutynin and 6.15 mg of (S)-oxybutynin. Technical details for recycling elution mode were discussed.


Assuntos
Ácidos Mandélicos/química , Ácidos Mandélicos/isolamento & purificação , beta-Ciclodextrinas/química , 2-Hidroxipropil-beta-Ciclodextrina , Distribuição Contracorrente/instrumentação , Distribuição Contracorrente/métodos , Estereoisomerismo
17.
J Sep Sci ; 37(14): 1736-41, 2014 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-24788958

RESUMO

High-speed countercurrent chromatography (HSCCC) combined with biphasic chiral recognition was successfully applied to the resolution of phenylsuccinic acid enantiomers. D-Isobutyl tartrate and hydroxypropyl-ß-cyclodextrin were employed as lipophilic and hydrophilic selectors dissolved in the organic stationary phase and aqueous mobile phase, respectively. The two-phase solvent system was made up of n-hexane/methyl tert-butyl ether/water (0.5:1.5:2, v/v/v). Impacts of the type and concentration of chiral selectors, the pH value of the aqueous phase solution as well as the temperature on the separation efficiency were investigated. By means of preparative HSCCC, pure enantiomer was obtained by separating 810 mg of racemate with a purity >99.5% and a recovery rate between 82 and 85%. The experimental results indicate that biphasic recognition HSCCC provide a promising means for efficient separation of racemates.

18.
Endocrine ; 83(3): 691-699, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-37889469

RESUMO

PURPOSE: To investigate the diagnostic value of contrast-enhanced ultrasound (CEUS) quantitative analysis parameters combined with shear wave elastography (SWE) quantitative parameters in the differentiation of benign and malignant ACR TI-RADS category 4 thyroid nodules and to provide a more effective reference for clinical work. METHODS: We analyzed 187 category 4 nodules, including 132 nodules in the development cohort and 55 nodules in the validation cohort, divided the development cohort into benign and malignant groups, and analyzed the differences in all CEUS and SWE quantitative parameters between the two groups. We selected the highest AUC of the two parameters, performed binary logistic regression analysis with the ACR TI-RADS score and constructed a diagnostic model. ROC curves were applied to evaluate their diagnostic efficacy. RESULTS: 1) The diagnostic model had an AUC of 0.926, sensitivity of 87.5%, specificity of 86.8%, diagnostic threshold of 3, accuracy of 87.12%, positive predictive value of 86.15%, and negative predictive value of 88.06%. 2) The diagnostic model had an AUC of 0.890 in the validation cohort, sensitivity of 81.5%, specificity of 79.6%, and accuracy of 80.00%. CONCLUSION: The combined multiparameter construction of the nodule diagnostic model can effectively improve the diagnostic efficacy of 4 types of thyroid nodules and provide a new reference index for clinical diagnostic work.


Assuntos
Técnicas de Imagem por Elasticidade , Nódulo da Glândula Tireoide , Humanos , Nódulo da Glândula Tireoide/diagnóstico por imagem , Nódulo da Glândula Tireoide/patologia , Diagnóstico Diferencial , Modelos Logísticos , Ultrassonografia , Estudos Retrospectivos
19.
J Cancer Res Clin Oncol ; 149(4): 1645-1656, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-35831762

RESUMO

Tumor immunotherapy has become an important means of tumor therapy by enhancing the immune response and triggering the activation of immune cells. However, currently, only a small number of patients respond to immunotherapy alone, and patients may experience immune-related adverse events (irAEs) during the course of treatment. Sonodynamic therapy (SDT) can produce cytotoxic substances to tumor tissue, induce apoptosis and enhance immunity. SDT combined with immunotherapy is considered a promising strategy for cancer treatment. In this mini review, we summarize the role of SDT in immunotherapy in recent years, including the application of SDT-triggered immunotherapy and the combination of SDT and immunotherapy.


Assuntos
Neoplasias , Terapia por Ultrassom , Humanos , Terapia Combinada , Apoptose , Imunoterapia/efeitos adversos , Neoplasias/terapia , Linhagem Celular Tumoral , Espécies Reativas de Oxigênio
20.
Int J Nanomedicine ; 18: 2275-2293, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37159806

RESUMO

Introduction: In order to diagnose and treat papillary thyroid carcinoma (PTC) accurately, phase-transition nanoparticles, P@IP-miRNA (PFP@IR780/PLGA-bPEI-miRNA338-3p), was engineered. The nanoparticles (NPs) can target the tumor cells, realize the multimodal imaging, and provide sonodynamic-gene therapy for PTC. Methods: P@IP-miRNA NPs were synthesized through double emulsification method, and miRNA338-3p was attached to the surface of the NPs by electrostatic adsorption. The characterization of NPs was detected to screen out qualified nanoparticles. In vitro, laser confocal microscopy and flow cytometry were used to detect the targeting and subcellular localization of NPs. Western blot, qRT-PCR, and immunofluorescence were used to detect the ability to transfect miRNA. CCK8 kit, laser confocal microscopy and flow cytometry were used to detect the inhibition on TPC-1 cells. In vivo experiments were performed based on tumor-bearing nude mice. The efficacy of combined treatment by NPs was comprehensively evaluated, and the multimodal imaging ability of NPs in vivo and in vitro was detected. Results: P@IP-miRNA NPs were successfully synthesized which have spherical shape, uniform size, good dispersion and positive potential. The encapsulation rate of IR780 was (82.58±3.92) %, the drug loading rate was (6.60±0.32) %, and the adsorption capacity of miRNA338-3p was 41.78 µg/mg. NPs have excellent tumor targeting ability, miRNA transfection ability, ROS production ability and multimodal imaging ability in vivo and in vitro. The antitumor effect of combined treatment group was the best, and the efficacy was better than that of single factor treatment group, and the difference was statistically significant. Conclusion: P@IP-miRNA NPs can realize multimodal imaging and sonodynamic-gene therapy, providing a new idea for accurate diagnosis and treatment of PTC.


Assuntos
Carcinoma Papilar , Nanopartículas , Neoplasias da Glândula Tireoide , Animais , Camundongos , Câncer Papilífero da Tireoide , Camundongos Nus , Terapia Genética , Neoplasias da Glândula Tireoide/diagnóstico por imagem , Neoplasias da Glândula Tireoide/terapia
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