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1.
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
2.
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
3.
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
4.
Int J Nanomedicine ; 18: 6667-6687, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38026520

RESUMO

Purpose: Sonodynamic therapy (SDT), with its high tissue penetration and noninvasive advantages, represents an emerging approach to eradicating solid tumors. However, the outcomes of SDT are typically hampered by the low oxygen content and immunosuppression in the tumor microenvironment (TME). Accordingly, we constructed a cascade nanoplatform to regulate the TME and improve the anti-tumor efficiency of SDT. Methods: In this study, we rationally design cascade nanoplatform by incorporating immunostimulant hyaluronic acid (HA) and sonosensitizer chlorin e6 (Ce6) on the polydopamine nanocarrier that is pre-doped with platinum nanozymes (designated Ce6/Pt@PDA-HA, PPCH). Results: The cascade reactions of PPCH are evidenced by the results that HA exhibits reversing immunosuppressive that converts M2 macrophages into M1 macrophages in situ, while producing H2O2, and then platinum nanozymes further catalyze the H2O2 to produce O2, and O2 produces abundant singlet oxygen (1O2) under the action of Ce6 and low-intensity focused ultrasound (LIFU), resulting in a domino effect and further amplifying the efficacy of SDT. Due to its pH responsiveness and mitochondrial targeting, PPCH effectively accumulates in tumor cells. Under LIFU irradiation, PPCH effectively reverses immunosuppression, alleviates hypoxia in the TME, enhances reactive oxygen species (ROS) generation, and enhances SDT efficacy for eliminating tumor cells in vivo and in vitro. Meanwhile, an in vivo dual-modal imaging including fluorescence and photoacoustic imaging achieves precise tumor diagnosis. Conclusion: This cascade nanoplatform will provide a promising strategy for enhancing SDT eradication against tumors by modulating immunosuppression and relieving hypoxia.


Assuntos
Nanopartículas , Porfirinas , Terapia por Ultrassom , Humanos , Terapia por Ultrassom/métodos , Peróxido de Hidrogênio , Platina , Linhagem Celular Tumoral , Porfirinas/farmacologia , Porfirinas/química , Espécies Reativas de Oxigênio , Hipóxia , Nanopartículas/química , Microambiente Tumoral
5.
Front Endocrinol (Lausanne) ; 14: 1140360, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37305060

RESUMO

Aim: Accurate preoperative prediction of cervical lymph node metastasis (LNM) in patients with mPTMC provides a basis for surgical decision making and the extent of tumor resection. This study aimed to develop and validate an ultrasound radiomics nomogram for the preoperative assessment of LN status. Methods: A total of 450 patients pathologically diagnosed with mPTMC were enrolled, including 348 patients in the modeling group and 102 patients in the validation group. Univariate and multivariate logistic regression analyses were performed on the basic information, ultrasound characteristics, and American College of Radiology Thyroid Imaging Reporting and Data System (ACR TI-RADS) scores of the patients in the modeling group to identify independent risk factors for LNM in mPTMC and to construct a logistic regression equation and nomogram to predict the risk of LNM. The validation group data were used to evaluate the predictive performance of the nomogram. Results: Male sex, age <40 years, a single lesion with a maximum diameter >0.5 cm, capsular invasion, a maximum ACR score >9 points, and a total ACR score >19 points were independent risk factors for the development of cervical LNM in mPTMC. Both the area under the curve (AUC) and concordance index (C-index) of the prediction model constructed from the above six factors were 0.838. The calibration curve of the nomogram was close to the ideal diagonal line. Furthermore, decision curve analysis (DCA) demonstrated a significantly greater net benefit of the model. The external validation demonstrated the reliability of the prediction nomogram. Conclusions: The presented radiomics nomogram, which is based on ACR TI-RADS scores, shows favorable predictive value for the preoperative assessment of LNs in patients with mPTMC. These findings may provide a basis for surgical decision making and the extent of tumor resection.


Assuntos
Nomogramas , Nódulo da Glândula Tireoide , Humanos , Masculino , Adulto , Metástase Linfática , Reprodutibilidade dos Testes
6.
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
7.
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.

8.
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
9.
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
10.
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
11.
Cancer Manag Res ; 14: 2861-2868, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36171864

RESUMO

Background: In recent years, papillary thyroid microcarcinoma (PTMC) has been a main cause of the high incidence of thyroid carcinoma. No existing study has reported whether microwave ablation (MWA) affects patients' immunity. Therefore, this study explored the effects of MWA treatment on the immune functions of patients with PTMC. Methods: This study included 50 patients diagnosed with PTMC who received MWA treatment under ultrasound guidance at the ultrasound department of our hospital from January 2019 to October 2020. Changes in immune function after MWA treatment in PTMC patients were detected by T lymphocyte subsets and cytokines secreted by T helper cells. Results: At 1 day and 2 weeks after MWA treatment, the proportions of CD3+, CD4+ and CD4+/CD8+ T lymphocyte subsets and the levels of the cytokines interleukin (IL)-2 and interferon (IFN)-γ in the peripheral blood of the patients were significantly higher than those before MWA treatment (P<0.05). The levels of CD8+ T lymphocytes, tumour necrosis factor (TNF)-α, IL-4, IL-6, IL-10 and IL-17A were not significantly different from those before MWA treatment (P>0.05). One month after MWA treatment, the proportions of CD3+, CD4+, CD8+ and CD4+/CD8+ T lymphocytes and the levels of the cytokines IL-2, IL-4, IL-6, IL-10, IFN-γ, TNF-α and IL-17A were not significantly different from those before MWA treatment (P>0.05). Conclusion: The immune functions of patients with PTMC are temporarily enhanced after MWA treatment, which has important clinical significance for patients' anti-PTMC ability.

13.
Mol Ther Nucleic Acids ; 24: 591-609, 2021 Jun 04.
Artigo em Inglês | MEDLINE | ID: mdl-33898108

RESUMO

We identified a novel interactome, circ_0001018/miR-338-3p/SOX4, in papillary thyroid cancer (PTC), and we intended to confirm the regulatory relationship between the three and to study the effects of the three in PTC. The bioinformatics method was used to screen out the circular RNA and mRNA of interest. A cellular fractionation assay and fluorescence in situ hybridization (FISH) assay were conducted to prove that circ_0001018 and CCT4 (the host gene of circ_0001018) mRNA primarily localized in the cytoplasm of PTC cell lines. By qRT-PCR analysis, the expression of circ_0001018 and SOX4 mRNA was found upregulated while the expression of miR-338-3p was found downregulated in PTC tissues and cells. circ_0001018 silence significantly inhibited the tumor growth in xenografted nude mice. A series of cytological experiments such as a Cell Counting Kit-8 (CCK-8) assay, a 5-ethynyl-2'-deoxyuridine (EdU) assay, cell cycle profiling, wound healing, a transwell assay, and cell apoptosis were conducted and showed that circ_0001018 and SOX4 promoted cell proliferation, migration, and invasion, inhibited cell apoptosis, and reduced the cell cycle arrest at the G1 phase in PTC cells. Compared with circ_0001018 and SOX4, miR-338-3p held the opposite function. The regulatory relationship between circ_0001018 and miR-338-3p, and between miR-338-3p and SOX4 mRNA, was validated using a luciferase reporter gene assay and/or RNA immunoprecipitation (RIP assay). Our findings showed that circ_0001018 acted as the tumor promoter via sponging miR-338-3p to elevate SOX4 expression level in PTC. Importantly, this novel circ_0001018/miR-338-3p/SOX4 axis has the potential to be considered as a therapy target for PTC.

14.
Endocrine ; 71(1): 113-121, 2021 01.
Artigo em Inglês | MEDLINE | ID: mdl-32419083

RESUMO

PURPOSE: To evaluate the safety and effectiveness of microwave ablation (MWA) versus lobectomy for the treatment of benign thyroid nodules > 4 cm. METHODS: We retrospectively analyzed the data of 48 patients who underwent MWA and 53 patients who underwent lobectomy to treat benign thyroid nodules > 4 cm. The patients were followed up for 12 months. The volume reduction ratio (VRR) was calculated. The operation time, incision length, hospitalization time, complications, thyroid function, symptoms, and cosmetic improvement were analyzed and compared between the two groups. RESULTS: During the 12-month follow-up, the mean nodule volume in the MWA group was reduced from 36.1 ± 23.1 to 4.0 ± 4.1 ml, and the mean VRR of the nodules was 90 ± 5% in the MWA group, which was comparable with that in the surgery group. No significant postoperative change in thyroid function was observed in the MWA group. Compared with the surgery group, the incidence of complications and postoperative pain in the MWA group were lower, the operation time, incision length, and hospitalization time in the MWA group were shorter, and satisfaction with the esthetic results in the MWA group was greater. CONCLUSION: MWA is safe and effective for the treatment of benign thyroid nodules > 4 cm. Moreover, MWA is associated with a faster recovery, fewer complications, better protection of thyroid function, and superior esthetic results relative to thyroid lobectomy.


Assuntos
Ablação por Cateter , Ablação por Radiofrequência , Nódulo da Glândula Tireoide , Humanos , Micro-Ondas/uso terapêutico , Estudos Retrospectivos , Nódulo da Glândula Tireoide/cirurgia , Resultado do Tratamento
15.
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
16.
Int J Biol Macromol ; 165(Pt A): 683-690, 2020 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-32961189

RESUMO

Three novel polysaccharides (PCPW, PCPS1 and PCPS2) were isolated from Potentilla chinensis and subjected to structural analysis by using spectral and physicochemical methods. The molecular weights of PCPW, PCPS1 and PCPS2 were calculated to be 4.45 × 103 Da, 1.18 × 104 Da and 4.23 × 104 Da, respectively. Analysis of monosaccharides composition confirmed that PCPW was composed of mannose, rhamnose, glucose, galactose and arabinose, while the two acidic polysaccharides PCPS1 and PCPS2 were consisted of six monosaccharides, including mannose, rhamnose, galacturonic acid, glucose, galactose and arabinose respectively. In addition, the main linkages of glycosidic bonds of PCPS2 were 1, 4-linked-rha, 1, 4-linked-man,1, 4-linked-galA and 1, 6-linked-man. Immunological tests indicated that both PCPW and PCPS2 could increase NO production of RAW264.7 cells, and promote splenocyte proliferation. All three polysaccharides proved to be activators of NF-κB. Overall, three polysaccharides showed a good immunological activity and pose great potential as a novel food or drug additive.


Assuntos
Proliferação de Células/efeitos dos fármacos , Polissacarídeos , Potentilla/química , Baço/imunologia , Animais , Configuração de Carboidratos , Camundongos , Polissacarídeos/química , Polissacarídeos/farmacologia , Células RAW 264.7 , Baço/citologia
17.
Biomater Sci ; 8(11): 3116-3129, 2020 Jun 07.
Artigo em Inglês | MEDLINE | ID: mdl-32352102

RESUMO

To enhance the specificity and efficiency of anti-tumor therapies, we have designed a multifunctional nanoparticle platform for photochemotherapy using fluorescence (FL) and photoacoustic (PA) imaging guidance. Nanoparticles (NPs) composed of a eutectic mixture of natural fatty acids that undergo a solid-liquid phase transition at 39 °C were used to encapsulate materials for the rapid and uniform release of the hypoxia-activated prodrug tirapazamine (TPZ) and the photosensitizer IR780, which targets the mitochondria of tumor cells and can be used to induce hypoxic cell death via photodynamic therapy and photothermal therapy. In vitro, the NPs containing TPZ and IR7890 exhibited appreciable cell uptake and triggered drug release when irradiated with a NIR laser. In vivo, photochemotherapy of the NPs achieved the best anti-tumor efficacy under PA and FL imaging guidance and monitoring. By combining IR780 mitochondria-targeting phototherapy with TPZ, we observed improved anti-tumor effectiveness and this has the potential to reduce the side effects of traditional chemotherapy. Herein, we demonstrate a new intracellular photochemotherapy nanosystem that co-encapsulates photosensitizers and hypoxia-activated drugs to enhance the overall anti-tumor effect precisely and efficiently.


Assuntos
Antineoplásicos/administração & dosagem , Indóis/administração & dosagem , Nanopartículas/administração & dosagem , Neoplasias/tratamento farmacológico , Fotoquimioterapia , Fármacos Fotossensibilizantes/administração & dosagem , Pró-Fármacos/administração & dosagem , Tirapazamina/administração & dosagem , Animais , Antineoplásicos/química , Antineoplásicos/efeitos da radiação , Hipóxia Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Liberação Controlada de Fármacos , Feminino , Indóis/química , Indóis/efeitos da radiação , Lasers , Camundongos Endogâmicos BALB C , Nanopartículas/química , Nanopartículas/efeitos da radiação , Neoplasias/metabolismo , Neoplasias/patologia , Imagem Óptica , Técnicas Fotoacústicas , Fármacos Fotossensibilizantes/química , Fármacos Fotossensibilizantes/efeitos da radiação , Pró-Fármacos/química , Pró-Fármacos/efeitos da radiação , Espécies Reativas de Oxigênio/metabolismo , Tirapazamina/química , Tirapazamina/efeitos da radiação
18.
Int J Biol Macromol ; 156: 640-647, 2020 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-32304789

RESUMO

Biofilms and intracellular bacteria often cause a series of overwhelming public health issues due to their strong drug resistance. Hence, chitosan nanoparticles (CS NPs), phosphatidylcholine and gentamicin were used to synthesize a novel nanodrug delivery system (GPC NPs). Dynamic light scattering (DLS) demonstrated that the surface zeta-potential of GPC NPs was -19.5 mV. The morphology of GPC NPs was observed by scanning electron microscopy (SEM). The gentamicin adsorption and release behaviors of GPC NPs were also investigated. The GPC NPs could effectively damage and remove the biofilm formed by pathogens through permeation of the antibiotic into the biofilm. In addition, the nanoparticles were readily engulfed by macrophages which facilitated the killing of intracellular bacteria and had neglectable cytotoxicity. Our study indicated that GPC NPs could be used as a promising nanoantibacterial agent against biofilms and intracellular bacteria.


Assuntos
Quitosana/química , Portadores de Fármacos/química , Gentamicinas/administração & dosagem , Nanopartículas/química , Fosfatidilcolinas/química , Bactérias/efeitos dos fármacos , Biofilmes/efeitos dos fármacos , Sistemas de Liberação de Medicamentos , Estabilidade de Medicamentos , Gentamicinas/química , Gentamicinas/farmacologia , Testes de Sensibilidade Microbiana
19.
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
20.
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
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