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1.
Int Immunopharmacol ; 132: 111945, 2024 May 10.
Artículo en Inglés | MEDLINE | ID: mdl-38555816

RESUMEN

BACKGROUND: Emodin, a natural anthraquinone derivative isolated from the roots of Rheum officinale Baill, has many pharmacological effects including anti-inflammatory, antioxidant, antiviral, antibacterial and anti-cancer. However, little is known about the effect of emodin on acute radiation proctitis (ARP). The present study was conducted to determine its effects and elucidate its mechanisms involving AKT/MAPK/NF-κB/VEGF pathways in ARP mice. METHODS: Total 60 C57BL/6 mice were divided randomly into control group, ARP group, AKT inhibitor MK-2206 group, and different doses of emodin groups. ARP mice were induced by 27 Gy of 6 MV X-ray pelvic local irradiation. MK-2206 was given orally for 2 weeks on alternate days. Emodin was administered daily by oral gavage for 2 weeks. Subsequently, all mice were sacrificed on day 15. The rectal tissues were obtained for further tests. The general signs score and the pathological grade were used to evaluate the severity of ARP. The expression of NF-κB, VEGF and AQP1 were determined by immunohistochemistry and western blot. The expression of p-AKT, p-ERK, p-JNK, p-p38, Bcl-2 and Bax were assessed using western blot. RESULTS: The worse general signs and damaged tissue structure of ARP mice were profoundly ameliorated by emodin. The expression of p-AKT, p-ERK, NF-κB, VEGF and AQP1 were significantly increased, resulting in the inflammation-induced angiogenesis in ARP mice. However, the expression of p-JNK and p-p38 were decreased, leading to the reduction of apoptosis in ARP mice. Excitedly, emodin reversed these changes, not only inhibited inflammation-induced angiogenesis, but also promoted apoptosis. Notably, the effects of emodin were similar to that of AKT inhibitor MK-2206, suggesting the involvement of AKT signaling in the effect of emodin. CONCLUSION: These results suggest that emodin attenuates ARP in mice, and the underlying mechanism might involve inhibition of the AKT/ERK/NF-κB/VEGF pathways and the induction of apoptosis mediated by JNK and p38.


Asunto(s)
Emodina , Ratones Endogámicos C57BL , FN-kappa B , Proctitis , Proteínas Proto-Oncogénicas c-akt , Transducción de Señal , Factor A de Crecimiento Endotelial Vascular , Animales , Emodina/farmacología , Emodina/uso terapéutico , FN-kappa B/metabolismo , Proteínas Proto-Oncogénicas c-akt/metabolismo , Proctitis/tratamiento farmacológico , Proctitis/etiología , Factor A de Crecimiento Endotelial Vascular/metabolismo , Ratones , Transducción de Señal/efectos de los fármacos , Traumatismos por Radiación/tratamiento farmacológico , Traumatismos por Radiación/patología , Masculino , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Compuestos Heterocíclicos con 3 Anillos/farmacología , Compuestos Heterocíclicos con 3 Anillos/uso terapéutico , Traumatismos Experimentales por Radiación/tratamiento farmacológico , Traumatismos Experimentales por Radiación/patología , Traumatismos Experimentales por Radiación/metabolismo , Recto/patología , Recto/efectos de los fármacos
2.
Pest Manag Sci ; 79(11): 4140-4152, 2023 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-37547967

RESUMEN

Pesticide creation is related to the development of sustainable agricultural and ecological safety, and molecular docking technology can effectively help in pesticide innovation. This paper introduces the basic theory behind molecular docking, pesticide databases, and docking software. It also summarizes the application of molecular docking in the pesticide field, including the virtual screening of lead compounds, detection of pesticides and their metabolites in the environment, reverse screening of pesticide targets, and the study of resistance mechanisms. Finally, problems with the use of molecular docking technology in pesticide creation are discussed, and prospects for the future use of molecular docking technology in new pesticide development are discussed. © 2023 Society of Chemical Industry.

4.
Sci Rep ; 12(1): 14116, 2022 08 18.
Artículo en Inglés | MEDLINE | ID: mdl-35982137

RESUMEN

Acute radiation proctitis (ARP) is one of the most common complications of pelvic radiotherapy attributed to radiation exposure. The mechanisms of ARP are related to inflammation, angiogenesis, and so on. In this study we evaluated the effect of dexamethasone (DXM) combined with gentamicin (GM) enema on ARP mice, and explored its possible mechanisms by transcriptome sequencing, western blot and immunohistochemistry. C57BL/6 mice were randomly divided into 3 groups: healthy control group, ARP model group, and DXM + GM enema treatment group. ARP mice were established by using a single 6 MV X-ray dose of 27 Gy pelvic local irradiation. Transcriptome sequencing results showed that 979 genes were co-upregulated and 445 genes were co-downregulated in ARP mice compared to healthy mice. According to gene ontology (GO) and kyoto encyclopedia of genes and genomes (KEGG) pathway enrichment analysis, we firstly found that PI3K/AKT/NF-κB/VEGF pathways were mostly correlated with the inflammation-induced angiogenesis in ARP mice. PI3K/AKT pathway leads to the activation of NF-κB, which promotes the transcription of VEGF and Bcl-2. Interestingly, symptoms and pathological changes of ARP mice were ameliorated by DXM + GM enema treatment. DXM + GM enema inhibited inflammation by downregulating NF-κB and upregulating AQP3, as well as inhibited angiogenesis by downregulating VEGF and AQP1 in ARP mice. Moreover, DXM + GM enema induced apoptosis by increasing Bax and suppressing Bcl-2. The novel mechanisms may be related to the downregulation of PI3K/AKT/NF-κB/VEGF pathways.


Asunto(s)
Gastritis , Proctitis , Animales , Dexametasona/farmacología , Gentamicinas/farmacología , Inflamación , Ratones , Ratones Endogámicos C57BL , FN-kappa B/metabolismo , Neovascularización Patológica , Fosfatidilinositol 3-Quinasas/metabolismo , Proteínas Proto-Oncogénicas c-akt/metabolismo , Proteínas Proto-Oncogénicas c-bcl-2/metabolismo , Transducción de Señal , Factor A de Crecimiento Endotelial Vascular/metabolismo
5.
J Environ Manage ; 310: 114584, 2022 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-35192982

RESUMEN

Gasification is an attractive method for tannery sludge (TS) disposal because of its advantages: volume reduction, stabilisation, harmlessness, and energy recovery. TS reduction ash (AR) and TS oxidation ash (AO), simulated from a downdraft fixed bed gasifier (DFBG) and an updraft fixed bed gasifier (UFBG), were investigated on their physicochemical characteristics, solidification behaviour, and value-added utilisation. Results showed that the main mineral matters in AR and AO consisted of Fe-oxids and Fe-Cr compounds, and the DFBG was more suitable for TS gasification than the UFBG because of the lower content of Cr(Ⅵ) in AR. With the addition of waste glass bottles (WGB), the ash fusion temperatures (AFTs) and leaching concentrations of heavy metals in AR and AO decreased significantly, and the heavy metals in AR and AO were successfully immobilised by the wrapping effect of the molten WGB. Moreover, gasification ash, as an auxiliary material for rock wool, reduced the AFTs and viscosity coefficient of the main chemical compositions in rock wool. With the addition of AR, the occurrence of Fe-containing compounds and the extremely low risk of leaching toxicity of heavy metals were observed. The maximum addition proportion of gasification ash was dependent on the maximum content of Fe2O3 allowed in the raw materials of rock wool, and its addition ratio must be below 15%.


Asunto(s)
Metales Pesados , Aguas del Alcantarillado , Ceniza del Carbón , Incineración , Aguas del Alcantarillado/química , Temperatura
6.
Spectrochim Acta A Mol Biomol Spectrosc ; 273: 121038, 2022 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-35189491

RESUMEN

To predict drug acute toxicity using the binding information with human serum albumin, our research group established a new method (Carrier protein binding information-toxicity relationship, CPBITR). Unfortunately, the previous model had too few data sets which may affect the accuracy and credibility of the model. In this paper, therefore, we measured the binding modes of three carbamate pesticides, Bendiocarb, Butocarboxim and Dioxacarb with human serum albumin (HSA) to supplement the previously modeled training set. Multispectral methods and molecular docking were used to study their binding modes. We built and optimized the previous models with the combined information of three different toxicity pesticides and HSA in order to find better prediction method. The results showed that Back-propagation Artificial Neural Network model has the best fitting effect among these models. In conclusion, the proposed model effectively improves the accuracy and credibility of the existing model. It results in significant predict drug acute toxicity using the binding information with carrier protein and contribute to drug development and research.


Asunto(s)
Proteínas Portadoras , Plaguicidas , Sitios de Unión , Carbamatos/toxicidad , Humanos , Simulación del Acoplamiento Molecular , Plaguicidas/química , Plaguicidas/toxicidad , Unión Proteica , Espectrometría de Fluorescencia
7.
Zhongguo Fei Ai Za Zhi ; 25(2): 86-91, 2022 Feb 20.
Artículo en Chino | MEDLINE | ID: mdl-35224961

RESUMEN

BACKGROUND: Dabrafenib+Trametinib/Dabrafenib targeted therapy has been approved for V-RAF murine sarcoma viral oncogene homolog B1 with amino acid substitution for valine at position 600 (BRAF V600E) in lung cancer patients, however, the targeted therapy strategy for lung cancer patients with BRAF non-V600E mutations has not been determined yet. This study intends to explore the efficacy of targeted therapy for BRAF non-V600E mutant lung cancer, and provide a reference for clinical treatment. METHODS: Computer search of PubMed, Cochrane Library, Embase, Web of Science, Clinicaltrials.gov, CBM, CNKI, Wanfang database. Collect the relevant literature relevant on the targeted therapy of BRAF non-V600E mutant lung cancer, and conduct a descriptive analysis of the included literature. RESULTS: There were 10 articles that met the inclusion criteria, including 3 cohort studies and 7 case reports. 18 patients with BRAF non-V600E mutant lung cancer were ineffective to vermurafenib; 1 patient obtained partial response (PR) after applying vermurafenib, 5 patients did not respond to BRAF inhibitors; 9 patients showed a potential clinical benefit rate of 34% after monotherapy with trametinib; 7 patients have different degrees of benefit from dabrafenib and trametinib on progression-free survival (PFS); 1 patient is effective to sorafenib. CONCLUSIONS: At present, there is no standard treatment specification for BRAF non-V600E mutation targeted therapy. The challenge lies in the heterogeneous mutation of BRAF gene. Different mutation types respond differently to targeted therapy. In addtion, real-world research evidence is scarce, so it is necessary to carry out further large-sample high-quality research to provide reference for clinical practice.


Asunto(s)
Carcinoma de Pulmón de Células no Pequeñas , Neoplasias Pulmonares , Animales , Protocolos de Quimioterapia Combinada Antineoplásica/uso terapéutico , Carcinoma de Pulmón de Células no Pequeñas/tratamiento farmacológico , Humanos , Neoplasias Pulmonares/tratamiento farmacológico , Neoplasias Pulmonares/genética , Ratones , Mutación , Inhibidores de Proteínas Quinasas/uso terapéutico , Proteínas Proto-Oncogénicas B-raf/genética
8.
Spectrochim Acta A Mol Biomol Spectrosc ; 264: 120188, 2022 Jan 05.
Artículo en Inglés | MEDLINE | ID: mdl-34358782

RESUMEN

Toxicity is one of the most important factors limiting the success of new drug development. In this paper, we built a fast and convenient new method (Carrier protein binding information-toxicity relationship, CPBITR) for predicting drug acute toxicity based on the perspective of binding information with carrier protein. First, we studied the binding information between carbamate pesticides and human serum albumin (HSA) through various spectroscopic methods and molecular docking. Then a total of 16 models were established to clarify the relationship between binding information with HSA and drug toxicity. The results showed that the binding information was related to toxicity. Finally we obtained the effective toxicity prediction model for carbamate pesticides. And the "Platform for Predicting Drug Toxicity Based on the Information of Binding with Carrier Protein" was established with the Back-propagation neural network model. We proposed and proved that it was feasible to predict drug toxicity from this new perspective: binding with carrier protein. According to this new perspective, toxicity prediction model of other drugs can also be established. This new method has the advantages of convenience and fast, and can be used to screen out low-toxic drugs quickly in the early stage. It is helpful for drug research and development.


Asunto(s)
Proteínas Portadoras , Plaguicidas , Sitios de Unión , Carbamatos/toxicidad , Humanos , Simulación del Acoplamiento Molecular , Plaguicidas/toxicidad , Unión Proteica , Espectrometría de Fluorescencia
9.
Oral Oncol ; 122: 105563, 2021 11.
Artículo en Inglés | MEDLINE | ID: mdl-34656055

RESUMEN

Indocyanine green (ICG) fluorescence-based sentinel lymph node (SLN) biopsy has been promoted to detect early metastasis of oral/oropharyngeal carcinoma, but its diagnostic value still remains unclear. In this letter, we identified 6 studies on ICG fluorescence based SLN in the detection of lymph node metastasis in oral/oropharyngeal carcinoma. For detection of metastatic lymph node, the overall sensitivity and specificity of the studies were 0.86 and 0.91, respectively. SROC curve was determined according to the combined sensitivity and specificity, and the overall area under the curve AUC was 0.93. On the whole, ICG fluorescence-based SLN biopsy showed promising effect for earlier detection and staging.


Asunto(s)
Carcinoma , Neoplasias de la Boca , Neoplasias Orofaríngeas , Ganglio Linfático Centinela , Carcinoma/diagnóstico por imagen , Colorantes , Humanos , Verde de Indocianina , Ganglios Linfáticos/diagnóstico por imagen , Metástasis Linfática , Neoplasias de la Boca/diagnóstico por imagen , Estadificación de Neoplasias , Neoplasias Orofaríngeas/diagnóstico por imagen , Ganglio Linfático Centinela/diagnóstico por imagen , Biopsia del Ganglio Linfático Centinela
10.
J Med Internet Res ; 23(4): e25817, 2021 04 15.
Artículo en Inglés | MEDLINE | ID: mdl-33729985

RESUMEN

BACKGROUND: Internet hospitals in China are in great demand due to limited and unevenly distributed health care resources, lack of family doctors, increased burdens of chronic diseases, and rapid growth of the aged population. The COVID-19 epidemic catalyzed the expansion of online health care services. In recent years, internet hospitals have been rapidly developed. Ping An Good Doctor is the largest, national online medical entry point in China and is a widely used platform providing online health care services. OBJECTIVE: This study aims to give a comprehensive description of the characteristics of the online consultations and inquisitions in Ping An Good Doctor. The analyses tried to answer the following questions: (1) What are the characteristics of the consultations in Ping An Good Doctor in terms of department and disease profiles? (2) Who uses the online health services most frequently? and (3) How is the user experience of the online consultations of Ping An Good Doctor? METHODS: A total of 35.3 million consultations and inquisitions over the course of 1 year were analyzed with respect to the distributions of departments and diseases, user profiles, and consulting behaviors. RESULTS: The geographical distribution of the usage of Ping An Good Doctor showed that Shandong (18.4%), Yunnan (15.6%), Shaanxi (7.2%), and Guangdong (5.5%) were the provinces that used it the most; they accounted for 46.6% of the total consultations and inquisitions. In terms of department distribution, we found that gynecology and obstetrics (19.2%), dermatology (17.0%), and pediatrics (14.4%) were the top three departments in Ping An Good Doctor. The disease distribution analysis showed that, except for nondisease-specific consultations, acute upper respiratory infection (AURI) (4.1%), pregnancy (2.8%), and dermatitis (2.4%) were the most frequently consulted diseases. In terms of user profiles, females (60.4%) from 19 to 35 years of age were most likely to seek consultations online, in general. The user behavior analyses showed that the peak times of day for online consultations occurred at 10 AM, 3 PM, and 9 PM. Regarding user experience, 93.0% of users gave full marks following their consultations. For some disease-related health problems, such as AURI, dermatitis, and eczema, the feedback scores were above average. CONCLUSIONS: The prevalence of internet hospitals, such as Ping An Good Doctor, illustrated the great demand for online health care services that can go beyond geographical limitations. Our analyses showed that nondisease-specific issues and moderate health problems were much more frequently consulted about than severe clinical conditions. This indicated that internet hospitals played the role of the family doctor, which helped to relieve the stress placed on offline hospitals and facilitated people's lives. In addition, good user experiences, especially regarding disease-related inquisitions, suggested that online health services can help solve health problems. With support from the government and acceptance by the public, online health care services could develop at a fast pace and greatly benefit people's daily lives.


Asunto(s)
COVID-19/epidemiología , Atención a la Salud/métodos , Telemedicina/métodos , Adulto , China/epidemiología , Estudios Transversales , Femenino , Humanos , Masculino , SARS-CoV-2/aislamiento & purificación , Encuestas y Cuestionarios , Adulto Joven
11.
Mol Med Rep ; 23(3)2021 03.
Artículo en Inglés | MEDLINE | ID: mdl-33495815

RESUMEN

Autosomal dominant polycystic kidney disease (ADPKD), a common disease with a high incidence ratio of between 1/400 and 1/1,000 individuals, often results in kidney failure and even mortality. However, there are relatively few effective treatments available, and treatment is limited to lifelong hemodialysis or kidney transplant. Our previous studies have reported that curcumin (Cur) and ginkgolide B (GB) inhibited cystogenesis by regulating the Ras/ERK MAPK signaling pathway. In the present study, it was hypothesized that Cur and GB may have a synergistic effect on the inhibition of cystogenesis, and their synergistic effect may be the result of regulation of multiple signaling pathways. To assess this hypothesis, an in vitro Madin­Darby canine kidney (MDCK) cyst model and an in vivo kidney­specific polycystin 1 transient receptor potential channel interacting (Pkd1) knockout mouse model were established to observe the effects of the combination of Cur and GB. The cysts exposed to Cur, GB and Cur combined with GB became small thick­walled cysts, small thin­walled cysts and round shaped cell colonies, respectively. The combination of Cur and GB was more effective compared with either treatment alone in inhibiting cystogenesis. Additionally, to the best of our knowledge, the present study was the first to demonstrate the synergistic effect of Cur and GB on the inhibition of cystogenesis in Pkd1 knockout mice. Cur may have mediated its anti­cyst effects by blocking EGFR/ERK1/2, JNK and PI3K/mTOR signaling pathways, while GB may have inhibited cystogenesis via the downregulation of the EGFR/ERK1/2, JNK and p38 signaling pathways. These results provide a proof­of­concept for application of the combination of Cur and GB in inhibiting cystogenesis in ADPKD.


Asunto(s)
Curcumina/farmacología , Ginkgólidos/farmacología , Lactonas/farmacología , Sistema de Señalización de MAP Quinasas/efectos de los fármacos , Riñón Poliquístico Autosómico Dominante/tratamiento farmacológico , Animales , Perros , Quinasas MAP Reguladas por Señal Extracelular/genética , Quinasas MAP Reguladas por Señal Extracelular/metabolismo , Sistema de Señalización de MAP Quinasas/genética , Células de Riñón Canino Madin Darby , Ratones , Ratones Noqueados , Riñón Poliquístico Autosómico Dominante/genética , Riñón Poliquístico Autosómico Dominante/metabolismo , Riñón Poliquístico Autosómico Dominante/patología , Proteína Quinasa C/genética , Proteína Quinasa C/metabolismo
12.
Metab Brain Dis ; 35(8): 1385-1394, 2020 12.
Artículo en Inglés | MEDLINE | ID: mdl-32860609

RESUMEN

Aß aggregation is one of the pathological biomarkers of Alzheimer's disease (AD). However, the possible mechanism related to Aß-induced pathological signaling pathway is still unknown. In the present study, Aß1-42-induced time-dependent memory impairment and its possible relationship to hypothalamic-pituitary-adrenal (HPA) axis hyperactivity were examined. Aß1-42-treated mice significantly impaired acquisition activity in the learning curve at 10 days, 1 and 4 months in the Morris water-maze (MWM) task. This learning activity was back to normal at 8 months after Aß1-42 treatment. In the probe trial test, Aß1-42-treated mice needed longer latencies to touch the precious platform location and fewer numbers of crossing from 10 days to 4 months after microinjection. This Aß1-42 induced memory loss was consistent with the results of the step-down passive avoidance test. The HPA axis related parameters, such as corticosterone (CORT) level in the serum, glucocorticoid receptor (GR) and corticotropin-releasing factor receptor (CRF-R) expression in the frontal cortex and hippocampus increased in Aß1-42-treated mice from 10 days to 4 months. While the downstream molecules phosphorylation of cyclic AMP response element binding (pCREB) and brain-derived neurotrophic factor (BDNF) expression decreased during this time. These effects were back to normal 8 months after treatment with Aß1-42. Altogether, our results suggested that Aß1-42 induced significant learning and memory impairment, which is involved in HPA axis dysfunction.


Asunto(s)
Péptidos beta-Amiloides/toxicidad , Sistema Hipotálamo-Hipofisario/metabolismo , Aprendizaje por Laberinto/fisiología , Trastornos de la Memoria/inducido químicamente , Trastornos de la Memoria/metabolismo , Fragmentos de Péptidos/toxicidad , Sistema Hipófiso-Suprarrenal/metabolismo , Péptidos beta-Amiloides/administración & dosificación , Animales , Reacción de Prevención/efectos de los fármacos , Reacción de Prevención/fisiología , Sistema Hipotálamo-Hipofisario/efectos de los fármacos , Inyecciones Intraventriculares , Masculino , Aprendizaje por Laberinto/efectos de los fármacos , Ratones , Ratones Endogámicos ICR , Fragmentos de Péptidos/administración & dosificación , Sistema Hipófiso-Suprarrenal/efectos de los fármacos , Factores de Tiempo
13.
Acta Cir Bras ; 35(5): e202000502, 2020 Jul 06.
Artículo en Inglés | MEDLINE | ID: mdl-32638843

RESUMEN

PURPOSE: Changrui enema, a traditional Chinese medicine prescription, is used as a supplementary treatment for acute radiation proctitis (ARP). Herein we explored the inhibition effects of Changrui enema on NF-κB and VEGF in ARP mice. METHODS: A total of 120 C57BL/6 mice were divided randomly into normal mice group, ARP mice group, western medicine enema group (dexamethasone combined with gentamicin), and Changrui enema group. ARP mice were established by pelvic local irradiation. The expression of IL-1ß, NF-κB, VEGF, AQP1, AQP3, p-ERK1/2 and p-JNK was determined by immunohistochemistry or western blot. RESULTS: The study firstly found that Changrui enema alleviated ARP mice. The expression of IL-1ß, NF-κB, VEGF, AQP1 and p-ERK1/2 was increased in ARP mice, and was reserved by Changrui enema. However, the expression of AQP3 and p-JNK was decreased in ARP mice, and was up-regulated by Changrui enema. CONCLUSIONS: Changrui enema is an effective treatment with fewer side effects for ARP. The mechanism of Changrui enema may be related to the inhibition of inflammation-induced angiogenesis. Changrui enema inhibits IL-1ß and NF-κB expression as well as VEGF expression. Interestingly, AQP1 promotes angiogenesis, while AQP3 inhibits inflammation. Changrui enema probably inhibits AQP1 expression by down-regulating p-ERK1/2, and improves AQP3 expression by up-regulating p-JNK.


Asunto(s)
Medicamentos Herbarios Chinos , FN-kappa B , Proctitis , Traumatismos por Radiación , Factor A de Crecimiento Endotelial Vascular , Animales , Medicamentos Herbarios Chinos/farmacología , Enema , Inflamación , Ratones , Ratones Endogámicos C57BL , FN-kappa B/efectos de los fármacos , Proctitis/tratamiento farmacológico , Proctitis/etiología , Traumatismos por Radiación/tratamiento farmacológico , Traumatismos por Radiación/metabolismo , Factor A de Crecimiento Endotelial Vascular/efectos de los fármacos
14.
RSC Adv ; 10(16): 9476-9485, 2020 Mar 02.
Artículo en Inglés | MEDLINE | ID: mdl-35497211

RESUMEN

Three couples of coordination polymers (CPs), namely, [Co((R/S)-Hcna)2] n (1-D/L), [Cd6((1R,2R/1S,2S)-cpba)4(phen)6(H2O)3] n (2-D/L) and [Cd2((1R,2R/1S,2S)-Hcpba)2(phen)2] n (3-D/L) {(R/S)-H2cna = (R/S)-6-(1-carboxyethoxy)-2-naphthoic acid, (1R,2R/1S,2S)-H3cpba = (1R,2R/1S,2S)-2,2'-((5-carboxy-1,3-phenylene)bis(oxy))dipropionic acid, phen = 1,10-phenanthroline} are successfully synthesized under hydrothermal conditions. Structural analysis shows that CP 1 has a 3D 3,6-c net structure with a point symbol of (4·62)2(42·610·83). CPs 2 and 3 are obtained under very similar reaction conditions except using different solvent ratios. The presence of the planar chelating ligand phen in CPs 2 and 3 limited the spatial growth of the structure, resulting in the formation of different 1D structures. All CPs crystallized in the chiral space group P21, CPs 1-3 are all SHG active. Their luminescence sensing activities for organics such as antibiotics, pesticides and nitro aromatics are also investigated. The results showed that CP 1 can effectively identify trace amounts of nitrofurans (NFs) and CP 3 has obvious recognition ability toward nitrofurans (NFs) and nitroimidazoles (NMs). Both CPs 1 and 3 could selectively detect 2,6-dichloro-4-nitroaniline (DCN). The luminescence of CPs 1 and 3 can also be quenched by (D/L)-4-nitrophenylalanine ((D/L)-NPA) and (1R,2R/1S,2S)-2-amino-1-(4-nitrophenyl)propane-1,3-diol ((1R,2R/1S,2S)-ANPO).

15.
Acta cir. bras ; 35(5): e202000502, 2020. tab, graf
Artículo en Inglés | LILACS | ID: biblio-1130646

RESUMEN

Abstract Purpose Changrui enema, a traditional Chinese medicine prescription, is used as a supplementary treatment for acute radiation proctitis (ARP). Herein we explored the inhibition effects of Changrui enema on NF-κB and VEGF in ARP mice. Methods A total of 120 C57BL/6 mice were divided randomly into normal mice group, ARP mice group, western medicine enema group (dexamethasone combined with gentamicin), and Changrui enema group. ARP mice were established by pelvic local irradiation. The expression of IL-1β, NF-κB, VEGF, AQP1, AQP3, p-ERK1/2 and p-JNK was determined by immunohistochemistry or western blot. Results The study firstly found that Changrui enema alleviated ARP mice. The expression of IL-1β, NF-κB, VEGF, AQP1 and p-ERK1/2 was increased in ARP mice, and was reserved by Changrui enema. However, the expression of AQP3 and p-JNK was decreased in ARP mice, and was up-regulated by Changrui enema. Conclusions Changrui enema is an effective treatment with fewer side effects for ARP. The mechanism of Changrui enema may be related to the inhibition of inflammation-induced angiogenesis. Changrui enema inhibits IL-1β and NF-κB expression as well as VEGF expression. Interestingly, AQP1 promotes angiogenesis, while AQP3 inhibits inflammation. Changrui enema probably inhibits AQP1 expression by down-regulating p-ERK1/2, and improves AQP3 expression by up-regulating p-JNK.


Asunto(s)
Animales , Ratones , Proctitis/etiología , Proctitis/tratamiento farmacológico , Traumatismos por Radiación/metabolismo , Traumatismos por Radiación/tratamiento farmacológico , Medicamentos Herbarios Chinos/farmacología , FN-kappa B/efectos de los fármacos , Factor A de Crecimiento Endotelial Vascular/efectos de los fármacos , Enema , Inflamación , Ratones Endogámicos C57BL
16.
Cell Cycle ; 18(15): 1745-1758, 2019 08.
Artículo en Inglés | MEDLINE | ID: mdl-31213123

RESUMEN

Pancreatic cancer (PC) is one of the most aggressive and lethal malignancies worldwide. Although significant progress has been made in oncology treatment, this refractory disease is still become intractable. Natural herb product diosgenin is described to exhibit vast range of pharmacological activities in preclinical studies, including anti-cancer activities. Accumulating data demonstrated that Enhancer of zeste homolog 2 (EZH2) as an oncogenic protein is over-expressed in various human cancers, including PC. However, the underlying mechanism has not been fully understood. In this study, we aim to investigate the anti-cancer properties and molecular basis of diosgenin in PC cells. Significant inhibition of cell proliferation was observed in diosgenin treated Patu8988 and Panc-1 cells in a dose- and time-dependent manner. Apoptotic cell death and G2/M phase arrest were also induced by diosgenin treatment in PC cells. Moreover, obvious inhibition of cell migration and invasive capacities was detected in diosgenin treated PC cells. Mechanistically, the expression levels of EZH2 and its target Vimentin were reduced, and PTEN was promoted after diosgenin exposure. Our results further supported that EZH2 signaling was closely associated with the anti-tumor characteristics of diosgenin in PC cells. Therefore, inhibition of EZH2 by diosgenin could be a promising therapeutic method for PC treatment.


Asunto(s)
Antineoplásicos/farmacología , Apoptosis/efectos de los fármacos , Movimiento Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Diosgenina/farmacología , Proteína Potenciadora del Homólogo Zeste 2/metabolismo , Neoplasias Pancreáticas/metabolismo , Animales , Línea Celular Tumoral , Diosgenina/administración & dosificación , Proteína Potenciadora del Homólogo Zeste 2/genética , Puntos de Control de la Fase G2 del Ciclo Celular/efectos de los fármacos , Silenciador del Gen , Humanos , Ratones , Ratones Desnudos , Fosfohidrolasa PTEN/metabolismo , Neoplasias Pancreáticas/tratamiento farmacológico , Neoplasias Pancreáticas/patología , ARN Interferente Pequeño , Trasplante Heterólogo , Regulación hacia Arriba , Vimentina/metabolismo
17.
RSC Adv ; 9(72): 42272-42283, 2019 Dec 18.
Artículo en Inglés | MEDLINE | ID: mdl-35542844

RESUMEN

Three novel coordination polymers (CPs), namely, {[Ag2(L)2(Mo4O13)·(CH3CN)]} n (1), {[Zn(L)(1,4-bdc)2·2(1,4-H2bdc)]} n (2), {[Cd(L)(1,4-bdc)0.5]} n (3) have been synthesized under solvothermal conditions by the reaction of bis(4-(4H-1,2,4-triazol-4-yl)phenyl)methane (L) and varied metal salts. Their structures are determined by single X-ray crystal diffraction, and further characterized by elemental analysis, IR, TGA and PXRD. CP 1 with ammonium molybdate as a secondary ligand displays a 2D network with (2,3,3,3,4)-connected net topology and the point symbol of {4·82}6{4·84·10}2{8}, CP 2 and CP 3 with 1,4-H2bdc as a secondary ligand demonstrate 3D structures with different topologies. CP 2 exhibits high sensibility and low detection limit in the recognition of antibiotics (NZF, NFT and FZD) and pesticide (DCN) identification. CP 1 demonstrates good anti-tumor activity toward the tested glioma cells. The possible luminescent sensitivity and anti-tumor mechanisms are also discussed.

19.
PLoS One ; 12(5): e0175401, 2017.
Artículo en Inglés | MEDLINE | ID: mdl-28481958

RESUMEN

PURPOSE: The aim of this study was to assess the diagnostic performance of 18F-FDG Positron Emission Tomography/Magnetic Resonance Imaging (PET/MRI) for gynecological cancers of the pelvis, based on a systematic review and meta-analysis of published data. METHODS: We performed a comprehensive literature search of Pubmed and Embase for studies that evaluated the diagnosis of 18F-FDG PET/MRI for gynecological malignancies in the pelvis. Quality Assessment for Studies of Diagnostic Accuracy 2 (QUADAS 2) tool was used to access the quality of included studies. After testing heterogeneity of the pooled studies with I^2 and H^2 (calculated using metaan in Stata12.0) we treated the data that extracted and transformation from the studies, based on DerSimonian-Laird method(Random-effects models),then back-transformation them to percentages and plotting to get the pooled sensitivity, specificity, likelihood ratios, and constructed summary receiver operating characteristics (SROC) curve. RESULTS: Eventually, 7 studies fulfilled our predefined inclusion criteria were included in our research. On patient-based assessment, the pooled sensitivity, specificity, positive likelihood ratio, negative likelihood ratio and diagnostic odds ratio of 18F-FDG PET/MRI for diagnosis of gynecological malignancies were 0.95 (95%CI 0.86-0.99), 0.95 (95% CI 0.74-1.00), 7.51 (95% CI 2.29-24.59), 0.12 (95% CI 0.05-0.29) and 116.27 (95% CI 17.07-791.74), respectively. On lesion-based assessment, the pooled sensitivity, specificity, positive likelihood ratio, negative likelihood ratio and the summary DOR were 0.89 (95%CI 0.84-0.93), 0.87 (95%CI 0.74-0.95), 6.99 (95%CI 3.30-14.79), 0.12 (95%CI 0.06-0.25) and 55.82 (95%CI 20.91-149.05), respectively. CONCLUSIONS: Our meta-analysis indicated that 18F-FDG PET/MRI, combined the advantages of MRI and PET, may be a very promising diagnostic method to assess the primary tumor and nodal staging in patients with gynecological malignancies of the pelvis.


Asunto(s)
Radioisótopos de Flúor/administración & dosificación , Neoplasias de los Genitales Femeninos/diagnóstico por imagen , Imagen Multimodal , Neoplasias Pélvicas/diagnóstico por imagen , Femenino , Humanos , Tomografía de Emisión de Positrones , Tomografía Computarizada por Rayos X
20.
Clin Chim Acta ; 450: 282-97, 2015 Oct 23.
Artículo en Inglés | MEDLINE | ID: mdl-26320853

RESUMEN

Neonatal hypoxic ischemic encephalopathy (HIE) is a common disease caused by perinatal asphyxia, a major cause of neonatal death, neurological behavior, and long-term disability. Currently, the diagnosis and prognosis of neonatal HIE are based on nervous system clinical manifestations, imaging and electrophysiological examination. These take time and late diagnosis allows brain injury to occur in newborns, so that infants of many brain injury missed the best treatment time, left with varying degrees of neurological sequelae. The use of biomarkers to monitor brain injury and evaluate neuroprotective effects might allow the early intervention and treatment of neonatal HIE to reduce mortality rates. This study reviewed the mechanism of neonatal hypoxic ischemic encephalopathy in relation to numerous brain-related biomarkers including NSE, S-100ß, GFAP, UCH-L1, Tau protein, miRNA, LDH, and CK-BB. In early diagnosis of neonatal HIE, S-100ß and activin A seems to be better biomarkers. Biomarkers with the greatest potential to predict long-term neurologic handicap of neonates with HIE are GFAP and UCH-L1 and when combined with other markers or brain imaging can increase the detection rate of HIE. Tau protein is a unique biological component of nervous tissues, and might have value for neonatal HIE diagnosis. Combination of more than two biological markers should be a future research direction.


Asunto(s)
Hipoxia-Isquemia Encefálica/sangre , Hipoxia-Isquemia Encefálica/líquido cefalorraquídeo , Animales , Biomarcadores/sangre , Biomarcadores/líquido cefalorraquídeo , Humanos , Recién Nacido
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