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1.
PLoS One ; 19(8): e0308669, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-39116140

RESUMEN

BACKGROUND: The significance of problem-solving ability has been confirmed in numerous studies worldwide, highlighting its role in enhancing the skills of nursing interns and reducing psychological pressure. However, existing research indicates that the problem-solving ability of nursing interns urgently needs to be further improved. Limited research has been conducted on the problem-solving ability of nursing interns, and the correlations among problem-solving ability, future time perspective, and future work self of Chinese nursing interns are unclear. OBJECTIVES: To investigate problem-solving ability, future time perspective, and future work self among the Chinese nursing interns, and to examine the relationships among these variables. Additionally, the study aims to explore the mediating role of future work self between problem-solving ability and future time perspective. METHODS: A cross-sectional and correlational design was employed, adhering to the quality reporting conformed to the STROBE Checklist. From May 8, 2023, to February 15, 2024, 1,251 nursing interns were recruited from 15 tertiary grade-A hospitals across six cities in China. The Demographic Characteristics Questionnaire, Social Problem-Solving Inventory, Future Time Perspective Inventory, and Future Work Self Scale were used. The data was analyzed using descriptive statistics, univariate, correlation, and process plug-in mediation effect analyses. RESULTS: The total scores for problem-solving ability, future time perspective, and future work self were 64.39 ± 18.55, 45.08 ± 11.37, and 16.92 ± 5.28, respectively. Problem-solving ability was positively correlated with future time perspective (r = 0.638, p < 0.001) and future work self (r = 0.625, p < 0.001). Additionally, future work self partially mediated mediating role between problem-solving ability and future time perspective, accounting for 39.7% of the total effect. CONCLUSION: The problem-solving ability, future time perspective, and future work self among the Chinese nursing interns were relatively moderate, indicating a need for improvement. It is suggested that nursing managers and educators should actively implement career management and planning programs. By enhancing the future time perspective and future work self of nursing interns, their problem-solving ability can be improved. This, in turn, will facilitate their adaptation to clinical work, enhance the quality of nursing care, and promote the development of their nursing profession.


Asunto(s)
Solución de Problemas , Humanos , Femenino , Masculino , China , Estudios Transversales , Adulto , Encuestas y Cuestionarios , Internado y Residencia , Estudiantes de Enfermería/psicología , Adulto Joven , Pueblos del Este de Asia
2.
Inorg Chem ; 63(1): 677-688, 2024 Jan 08.
Artículo en Inglés | MEDLINE | ID: mdl-38109074

RESUMEN

The abuse of antibiotics leads to an increasing emergence of drug-resistant bacteria, which not only causes a waste of medical resources but also seriously endangers people's health and life safety. Therefore, it is highly desirable to develop an efficient antibacterial strategy to reduce the reliance on traditional antibiotics. Antibacterial photodynamic therapy (aPDT) is regarded as an intriguing antimicrobial method that is less likely to generate drug resistance, but its efficiency still needs to be further improved. Herein, a robust titanium-based metal-organic framework ACM-1 was adopted to support Ag nanoparticles (NPs) to obtain Ag NPs@ACM-1 for boosting antibacterial efficiency via synergistic chemical-photodynamic therapy. Apart from the intrinsic antibacterial nature, Ag NPs largely boost ROS production and thus improve aPDT efficacy. As a consequence, Ag NPs@ACM-1 shows excellent antibacterial activity under visible light illumination, and its minimum bactericidal concentrations (MBCs) against E. coli, S. aureus, and MRSA are as low as 39.1, 39.1, and 62.5 µg mL-1, respectively. Moreover, to expand the practicability of Ag NPs@ACM-1, two (a dense and a loose) Ag NPs@ACM-1 films were readily fabricated by simply dispersing Ag NPs@ACM-1 into heated aqueous solutions of edible agar and sequentially cooling through heating or freeze-drying, respectively. Notably, these two films are mechanically flexible and exhibit excellent antibacterial activities, and their antimicrobial performances can be well retained in their recyclable and remade films. As agar is nontoxic, degradable, inexpensive, and ecosustainable, the dense and loose Ag NPs@ACM-1 films are potent to serve as recyclable and degradable antibacterial plastics and antibacterial dressings, respectively.


Asunto(s)
Antiinfecciosos , Nanopartículas del Metal , Estructuras Metalorgánicas , Fotoquimioterapia , Humanos , Plata/farmacología , Titanio/farmacología , Estructuras Metalorgánicas/farmacología , Staphylococcus aureus , Escherichia coli , Agar , Antibacterianos/farmacología , Pruebas de Sensibilidad Microbiana
3.
J Cardiovasc Dev Dis ; 10(2)2023 Feb 06.
Artículo en Inglés | MEDLINE | ID: mdl-36826567

RESUMEN

BACKGROUND: The superior cervical ganglion (SCG) plays a key role in cardiovascular diseases. The aim of this study was to determine the changes in the ion channel characteristics of the SCG following myocardial infarction (MI) and the role of pretreatment with the P2Y12 receptor antagonist ticagrelor (TIC). METHODS: A total of 18 male rabbits were randomly divided into a control group, MI group, and P2Y12 receptor antagonist (TIC) group (abbreviated as the TIC group). Rabbit MI was performed via two abdominal subcutaneous injections of 150 mg·kg-1·d-1 of isoproterenol (ISO) with an interval of 24 h. TIC pretreatment at 20 mg·kg-1·d-1 was administered via gavage for two consecutive days. The cardiac function of each group was evaluated with echocardiography. ADP receptor P2Y12 expressions in SCGs were determined using RT-PCR and immunofluorescence staining. Ion channel characteristics of SCG neurons were measured using a whole-cell patch clamp. Intracellular calcium concentrations for SCG neurons were measured using confocal microscopy. RESULTS: Cardiac function was reduced in the rabbits of the MI group, the sympathetic nerve activity of SCGs was increased, and the current amplitude of the neuron ion channel was increased. MI led to alterations in the activation and inactivation characteristics of INa channels accompanied by increased expression of P2Y12 in SCGs. Most of these abnormalities were prevented by TIC pretreatment in the TIC group. CONCLUSIONS: TIC pretreatment could attenuate the increase in P2Y12 expression in SCGs and the changes to the ion channel characteristics of SCG neurons after MI. This may be the mechanism underlying the cardiac protective effects of TIC.

4.
Front Cardiovasc Med ; 9: 908037, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36148071

RESUMEN

Purpose: The mechanism of sodium-glucose cotransporter-2 inhibitor (SGLT-2i) reducing the incidence of atrial fibrillation remains unclear. We hypothesize that sodium-glucose cotransporter-2 inhibitor alleviated atrial remodeling in STZ-induced diabetic rats by targeting TLR4 pathway. Methods: A total of 42 rats were randomly assigned into three groups: control group (CON group); diabetes group (DM group): diabetes mellitus rats were established by 65 mg/kg streptozotocin (STZ) intraperitoneal injection; and diabetes + dapagliflozin group (DM + DAPA group): diabetic rats were given DAPA gavage administration (DAPA 2mg/kg/d for 4 weeks by gavage administration), 14 rats in each group. Epicardial multiple-lead recording and intracardiac electrophysiology studies were performed to investigate the electrical remodeling in the heart and the atrial fibrillation inducibility in each group. Western blot analysis and real-time PCR were used to determine the protein and mRNA expression of toll-like receptor 4 (TLR4), interleukin receptor-associated kinase 1 (IRAK1), tumor necrosis factor receptor-associated factor 6 (TRAF6), nuclear factor-kappa B (NF-κB), and type I collagen (collagen I). Results: Compared with rats in CON group, rats in DM group showed marked myocardial fibrosis, ectopic pacing excitement, reduced conduction velocity, decreased cardiac function. TLR4/IRAK1/TRAF6/NF-κB, collagen I proteins expressions and incidence of atrial fibrillation (27.3%) were increased in DM group. Parts of these changes were reversed by treatment of DAPA. Incidence of atrial fibrillation was decreased in DM + DAPA group (2.8%). Conclusions: SGLT-2i dapagliflozin may prevent diabetic rats' atrial remodeling and reduce the inducibility of atrial fibrillation partly by targeting TLR4/IRAK1/TRAF6/NF-κB inflammatory pathway.

5.
ACS Appl Mater Interfaces ; 14(18): 21098-21105, 2022 May 11.
Artículo en Inglés | MEDLINE | ID: mdl-35482947

RESUMEN

Although tremendous progress has been achieved in the field of hydrogen-bonded organic frameworks (HOFs), the low stability, small/none pores, and difficult functionality severely obstruct their development. Herein, a novel robust mesoporous HOF (HOF-FAFU-1) decorated with a high density of free hydroxy moieties has been designed and readily synthesized in the de novo synthesis. In HOF-FAFU-1, the planar building blocks are connected to each other by typical intermolecular carboxylate dimers to form two-dimensional (2D) layers with sql topology, which are further connected to their adjacent layers by face-to-face π-π interactions to obtain a three-dimensional (3D) open mesoporous framework. Owing to the high density of intermolecular hydrogen bonding and strong π-π interactions, HOF-FAFU-1 is very stable, allowing it to retain its structure in aqueous solutions with a pH range of 1-9. Benefiting from the decorated hydroxy moieties, HOF-FAFU-1 was exploited as a fluorescent sensor for hypochlorite detection in water media by a turn-off mode, which cannot be realized by its nonhydroxy groups anchoring counterpart (HOF-TCBP). The proposed sensing system is highly efficient, validated by a very broad linear range (0-0.45 mM), fast response (15 s), and small limit of detection (LOD) (1.32 µM). The fluorescent quenching of HOF-FAFU-1 toward hypochlorite was also investigated, mainly being ascribed to the transformation of building blocks from the fluorescent reduced state to the nonfluorescent oxidative state. This work not only demonstrates that HOFs integrated with high stability and large pores as well as high density of functional groups can be simultaneously realized by judicious design of building blocks but also conceptually elucidates that such HOFs can effectively extend the application fields of HOFs.

6.
Front Cardiovasc Med ; 9: 1087287, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36620612

RESUMEN

Background: Early detection of subclinical cardiotoxicity of immune checkpoint inhibitor (ICI) therapy can be challenging. Objective: To evaluate subclinical cardiac dysfunction using two-dimensional speckle tracking imaging (2D-STI) and three-dimensional echocardiography in Chinese patients. Methods: Fifty-five consecutive patients with malignant tumors treated by immunotherapy were included. They were examined by echocardiography before immunotherapy and after immunotherapy. Left ventricular ejection fraction (LVEF) was calculated in three-dimensional imaging. Moreover, left ventricular global longitudinal peak systolic strain (LVGLS), left ventricular global circumferential peak systolic strain (LVGCS), right ventricular global longitudinal systolic strain (RVGLS), right ventricular free wall longitudinal peak systolic strain (RVFWLS), and tricuspid annular plane systolic excursion (TAPSE) were evaluated. Clinical and laboratory parameters were recorded. Cardiac toxicity events were defined as the presence of heart failure symptoms, LVEF reduction, and increase in troponin. Subclinical cardiac toxicity was defined as cardiac dysfunction associated with ICI treatment, with absent or delayed ICI-associated cardiotoxicity clinical symptoms. Results: Compared with baseline, the LVGLS, TAPSE, and RVGLS significantly deteriorated after ICI treatment [(-18.63 ± 2.53)% vs. (-17.35 ± 2.58)%, P = 0.000; 18.29 ± 6.23 vs. 14.57 ± 3.81, P = 0.0001; and (-18.45 ± 4.65)% vs. (-14.98 ± 3.85)%, P = 0.0001, respectively]. LVGLS (-17.35 ± 2.58, P = 0.000), TAPSE (14.57 ± 3.81, P = 0.0001), and RVGLS [(-14.98 ± 3.85)%, P = 0.0001] were decreased after ICI immunotherapy. Kaplan-Meier curve analysis showed that LVGLS was more sensitive than the cardiac toxicity events to assess ICI-related subclinical cardiac dysfunction (log-rank P = 0.205). The ROC curve showed that the cutoff value of ΔLVGLS was -13%. Conclusion: Subclinical cardiac dysfunction can be detected using two-dimensional speckle-tracking imaging. LVGLS, RVGLS, and TAPSE are more sensitive indices for detection. Clinical trial registration: [https://www.chictr.org.cn/showprojen.aspx?proj=27498], identifier [ChiCTR1800016216].

7.
Chem Biodivers ; 15(3): e1700513, 2018 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-29333734

RESUMEN

A series of novel quinazolinone derivatives containing a substituted amino moiety were synthesized, evaluated for their cytotoxic and antibacterial activities. The results of MTT assay showed that all synthesized target compounds 5A - 5O showed potent cytotoxicity against SGC-7901 (IC50 , 0.72 - 1.41 µm). Moreover, the compounds 5D, 5I, and 5K showed better selectivity as compared with positive controls pemetrexed and MTX due to weak cytotoxicity against normal tissue cell line HUVSMC. Among synthesized compounds, the compounds 5E, 5J, 5L, and 5N showed broad-spectrum cytotoxic activities against at least four cancer cell lines at a micromolar level. The results of antibacteria evaluation revealed that all synthesized compounds showed good to moderate antibacterial activities against Gram-negative bacteria Escherichia coli. Among them, the MIC values of the compounds 5C, 5F, and 5M were 0.31 µg/mL.


Asunto(s)
Antibacterianos/farmacología , Escherichia coli/efectos de los fármacos , Quinazolinonas/farmacología , Staphylococcus aureus/efectos de los fármacos , Animales , Antibacterianos/síntesis química , Antibacterianos/química , Línea Celular , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Humanos , Ratones , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Quinazolinonas/síntesis química , Quinazolinonas/química , Relación Estructura-Actividad
8.
Int J Pharm ; 528(1-2): 47-54, 2017 Aug 07.
Artículo en Inglés | MEDLINE | ID: mdl-28559216

RESUMEN

A novel ultrasound-responsive liposomal system for tumor targeting was prepared in order to increase the antitumor efficacy and decrease serious side effects. In this paper, PLGA nanoparticles were used ultrasound-responsive agents instead of conventional microbubbles. The PLGA-nanoparticles were prepared by an emulsion solvent evaporation method. The liposomes were prepared by a lipid film hydration method. Particle size, zeta potential, encapsulation efficiency and drug loading capacity of the liposomes were studied by light scattering analysis and dialysis. Transmission electron microscopy (TEM) and atomic force microscope (AFM) were used to investigate the morphology of liposomes. The release in vitro was carried out in the pH 7.4 phosphate buffer solutions, as a result, liposome L3 encapsulating PLGA-nanoparticles displayed good stability under simulative physiological conditions and quickly responsive release under the ultrasound. The release in vivo was carried out on the rats, as a result, liposome L3 showed higher bioavailability than traditional intravenous injectable administration, and liposome L3 showed higher elimination ratio after stimulation by ultrasound than L3 without stimulation. Thus, the novel ultrasound-responsive liposome encapsulating PLGA-nanoparticles has a potential to be developed as a new drug delivery system for anti-tumor drug.


Asunto(s)
Portadores de Fármacos/química , Ácido Láctico/química , Liposomas/química , Mitoxantrona/administración & dosificación , Nanopartículas/química , Ácido Poliglicólico/química , Animales , Antineoplásicos/administración & dosificación , Antineoplásicos/farmacocinética , Disponibilidad Biológica , Portadores de Fármacos/farmacocinética , Mitoxantrona/farmacocinética , Tamaño de la Partícula , Copolímero de Ácido Poliláctico-Ácido Poliglicólico , Ratas , Ratas Sprague-Dawley
9.
Chem Biodivers ; 14(2)2017 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-27696660

RESUMEN

A series of 3-(substituted aroyl)-4-(3,4,5-trimethoxyphenyl)-1H-pyrrole derivatives were synthesized and determined for their anticancer activity against eleven cancer cell lines and two normal tissue cell lines using MTT assay. Among the synthesized compounds, compound 3f was the most potent compound against A375, CT-26, HeLa, MGC80-3, NCI-H460 and SGC-7901 cells (IC50  = 8.2 - 31.7 µm); 3g, 3n and 3a were the most potent compounds against CHO (IC50  = 8.2 µm), HCT-15 (IC50  = 21 µm) and MCF-7 cells (IC50  = 18.7 µm), respectively. Importantly, all the target compounds showed no cytotoxicity towards the normal tissue cell (IC50  > 100 µm). Thus, these compounds with the potent anticancer activity and low toxicity have potential for the development of new anticancer chemotherapy agents.


Asunto(s)
Antineoplásicos/farmacología , Proliferación Celular/efectos de los fármacos , Diseño de Fármacos , Neoplasias/tratamiento farmacológico , Pirroles/síntesis química , Pirroles/farmacología , Antineoplásicos/química , Células Cultivadas , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Células Endoteliales de la Vena Umbilical Humana , Humanos , Estructura Molecular , Neoplasias/patología , Relación Estructura-Actividad
10.
Anticancer Agents Med Chem ; 17(6): 821-831, 2017.
Artículo en Inglés | MEDLINE | ID: mdl-27671311

RESUMEN

BACKGROUND: Cancer is considered a major public health problem worldwide. OBJECTIVE: The aim of this paper is to design and synthesis of novel anticancer agents with potent anticancer activity and minimum side effects. METHOD: A series of pyrrole derivatives were synthesized, their anti-cancer activity against nine cancer cell lines and two non-cancer cell lines were evaluated by MTT assay, and their cell cycle progression were determined by flow cytometry analysis. RESULTS: The study of the structure-activity relationships revealed that the introduction of the electron-donation groups at the 4th position of the pyrrole ring increased the anti-cancer activity. Among the synthesized compounds, specially the compounds bearing 3,4-dimethoxy phenyl at the 4th position of the pyrrole ring showed potent anti-cancer activity, cpd 19 was the most potent against MGC 80-3, HCT-116 and CHO cell lines (IC50s = 1.0-1.7 µM), cpd 21 was the most potent against HepG2, DU145 and CT-26 cell lines (IC50s = 0.5-0.9 µM), and cpd 15 was the most potent against A549 (IC50 = 3.6 µM). Moreover, these potent compounds showed weak cytotoxicity against HUVEC and NIH/3T3. Thus, the cpds 15, 19 and 21 show potential anti-cancer for further investigation. Furthermore, the flow cytometry analysis revealed that cpd 21 arrested the CT-26 cells at S phase, and induced the cell apoptosis. CONCLUSION: Thus, these compounds with the potent anticancer activity and low toxicity have potential for the development of new anticancer chemotherapy agents.


Asunto(s)
Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Pirroles/síntesis química , Pirroles/farmacología , Animales , Antineoplásicos/química , Células CHO , Espectroscopía de Resonancia Magnética con Carbono-13 , Línea Celular Tumoral , Cricetinae , Cricetulus , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Espectroscopía de Protones por Resonancia Magnética , Pirroles/química , Espectrometría de Masa por Ionización de Electrospray , Relación Estructura-Actividad
11.
Braz. j. pharm. sci ; 51(2): 373-382, Apr.-June 2015. tab, ilus
Artículo en Inglés | LILACS | ID: lil-755048

RESUMEN

The purpose of this study was to develop a reservoir-type transdermal delivery system for isosorbide dinitrate (ISDN). The developed patch consisted of five layers from bottom to top, namely, a temporary liner, an adhesive layer, a rate-controlling membrane, a reservoir and a backing. The effects of chemical penetration enhancers, reservoir materials and rate-controlling membranes on the release behaviour of ISDN from the transdermal patch were studied, and the in vitro release of ISDN from the developed patch was studied and compared with the commercially available ISDN patch. The results showed that there was no significant difference in permeation rates between the developed reservoir-type patch and the commercially available ISDN patch (p> 0.05). Moreover, the cumulative release ratio of the commercially available ISDN patch in 48 h was up to 89.8%, whereas the developed patch was only 34.9%, which meant the sustained release time of the developed patch was much longer than the commercially available ISDN patch, and would promote the satisfaction of the patient...


O objetivo do presente estudo foi desenvolver um sistema de liberação transdérmico do tipo reservatório para o dinitrato de isossorbida (ISDN, abrevitura em Inglês). A formulação transdérmica desenvolvida constou de cinco camadas de baixo para cima, ou seja, um revestimento temporário, uma camada adesiva, uma membrana controladora da taxa de liberação, um reservatório e um reforço. Estudaram-se os efeitos dos potenciadores de penetração química, materiais do reservatório e membranas de controle da taxa de liberação no comportamento da formulação transdérmica de dinitrato de isossorbida. A liberação in vitro da formulação transdérmica de dinitrato de isossorbida desenvolvida foi estudada em comparação com a formulação de dinitrato de isossorbida disponível comercialmente. Os resultados mostraram que não existem diferenças significativa nas taxas de permeação entre o tipo de reservatório desenvolvido e o de dinitrato de isossorbida desenvolvido comercialmente (p>0,05). Ademais, a taxa de liberação cumulativa da formulação de dinitrato de isossorbida disponível comercialmente em 48 horas foi de até 89,8% e a da formulação desenvolvida, de apenas de 34,9%, o que provou que a liberação sustentada da formulação desenvolvida foi muito maior do que a de dinitrato de isossorbida desenvolvida comercialmente, o que promoveria a satisfação do paciente...


Asunto(s)
Humanos , Dinitrato de Isosorbide/administración & dosificación , Dinitrato de Isosorbide/análisis , Dinitrato de Isosorbide/farmacocinética , Dinitrato de Isosorbide/farmacología , Administración Cutánea , Angina de Pecho/tratamiento farmacológico , Química Farmacéutica , Permeabilidad
12.
Eur J Med Chem ; 86: 165-74, 2014 Oct 30.
Artículo en Inglés | MEDLINE | ID: mdl-25151579

RESUMEN

A series of N-alkyl or aryl substituted isoindigo derivatives have been synthesized and their anti-proliferative activity was evaluated by Sulforhodamine B (SRB) assay. Some of the target compounds exhibited significant antitumor activity, including compounds 6h and 6k (against K562 cells), 6i (against HeLa cells) and 6j (against A549 cells). N-(p-methoxy-phenyl)-isoindigo (6k) exhibited a high and selective anti-proliferative activity against K562 cells (IC50 7.8 µM) and induced the apoptosis of K562 cells in a dose-dependent manner. Compound 6k arrested the cell cycle at S phase in K562 cells by decreasing the expression of cyclin A and CDK2, which played critical roles in DNA replication and passage through G2 phase. Moreover, compound 6k down-regulated the expression of p-GSK-3ß (Ser9), ß-catenin and c-myc proteins, up-regulated the expression of GSK-3ß, consequently, suppressed Wnt/ß-catenin signaling pathway and induced the apoptosis of K562 cells. The binding mode of compound 6k with GSK-3ß was simulated using molecular docking tools. All of these studies gave a better understanding to the molecular mechanisms of this class of agents and clues to develop dual CDK2/GSK-3ß (Ser9) phosphorylation inhibitors applied in cancer chemotherapy.


Asunto(s)
Antineoplásicos/farmacología , Quinasa 2 Dependiente de la Ciclina/antagonistas & inhibidores , Diseño de Fármacos , Glucógeno Sintasa Quinasa 3/antagonistas & inhibidores , Antineoplásicos/síntesis química , Antineoplásicos/química , Apoptosis/efectos de los fármacos , Ciclo Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Quinasa 2 Dependiente de la Ciclina/metabolismo , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Glucógeno Sintasa Quinasa 3/metabolismo , Glucógeno Sintasa Quinasa 3 beta , Células HCT116 , Células HeLa , Humanos , Indoles/síntesis química , Indoles/química , Indoles/farmacología , Células K562 , Modelos Moleculares , Estructura Molecular , Fosforilación/efectos de los fármacos , Relación Estructura-Actividad , Células Tumorales Cultivadas
13.
Anticancer Agents Med Chem ; 14(7): 994-1002, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-24372525

RESUMEN

A novel series of 3-substituted-4-(4-methylthio phenyl)-1H-pyrrole derivatives were synthesized via Van Leusen pyrrole synthesis. The in vitro anticancer activity against a panel of 16 cancer cell lines and 2 normal cell lines was investigated by MTT assay. It was found that some of the pyrrole compounds showed similar antiproliferative activity against cancer cells compared with Paclitaxel, but little impact on normal cell lines, which indicated that the novel pyrrole derivatives could be used as potential anticancer candidates for possessing both selectivity and good therapeutic efficacy. Structure-activity relationship analysis found that 3-phenylacetyl-4- (4-methylthio phenyl)-1H-pyrrole derivatives displayed the most strong anticancer activity, among which [4-(4-methylthio phenyl)-1H-pyrrol- 3-yl] (4-methoxy phenyl) methanone (3j) was employed to investigate the effect of these pyrrole analogues on cell cycle by propidium iodide (PI) staining on cell flow cytometry. Cell necrotic effect of 10.0 µM 3j against MGC80-3 cells were also observed under fluorescence microscope and transmission electron microscope by ultrathin sections observation.


Asunto(s)
Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Pirroles/síntesis química , Pirroles/farmacología , Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Necrosis , Relación Estructura-Actividad
14.
Zhonghua Wei Chang Wai Ke Za Zhi ; 15(12): 1282-6, 2012 Dec.
Artículo en Chino | MEDLINE | ID: mdl-23268278

RESUMEN

OBJECTIVE: To investigate the independent predictors of postoperative mortality, morbidity, and long-term survival in patients with stage IV ( colorectal cancer. METHODS: Clinical data of 189 patients with stage IV( colorectal cancer undergoing palliative resection of primary tumor in the presence of unresectable synchronous metastases were analyzed retrospectively. RESULTS: Eighty-six (45.5%)patients developed postoperative complications. Preoperative predictors of medical complications included age(≥65, P=0.039) and emergency operations (P=0.001). Preoperative predictors of surgical complications included advanced local disease (T4, P=0.022) and lymph node spread (N2, P=0.009). Seventeen (9.0%) patients died in the postoperative period. Mortality was independently associated with age(P=0.013), peritoneal dissemination(P=0.010), emergency operations(P=0.001) and medical complications(P=0.008). The survival rates at 1-, 2-, and 3- year of 172 patients admitted in survival analysis were 41.2%, 22.7% and 7.7% respectively. Independent factors associated with poor overall survival included lymph node spread(N2, P=0.015) and poor tumor differentiation(P=0.038). CONCLUSIONS: Emergency operations should be avoid when palliative resection of primary tumor is considered for stage IV( colorectal cancer patients, especially for elderly patients and those with peritoneal dissemination. The significance of palliative resection is limited for stage IV ( colorectal cancer patients with lymph node spread and poor tumor differentiation.


Asunto(s)
Neoplasias Colorrectales/cirugía , Anciano , Neoplasias Colorrectales/patología , Humanos , Ganglios Linfáticos , Estadificación de Neoplasias , Cuidados Paliativos , Complicaciones Posoperatorias , Pronóstico , Estudios Retrospectivos , Análisis de Supervivencia
15.
Chin J Integr Med ; 14(2): 137-41, 2008 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-18679606

RESUMEN

OBJECTIVE: To observe the clinical efficacy of integrative medical therapy in treating post-craniocerebral traumatic mental disorder (PCT-MD). METHODS: Sixty patients with confirmed diagnosis of PCT-MD were randomly assigned to the treated group and the control group equally. All were treated by conventional comprehensive Western medicine, but to patients in the treated group, modified Xufu Zhuyu Decoction (XFZY) was additionally given and the therapeutic course for both groups was 20 days. Changes in mental symptoms were observed and recorded on the 10th and 20th day and clinical efficacy as well as cranial CT image was estimated after termination of the treatment. RESULTS: The clinical effective rate in the treated group and the control group was 96.67% and 83.30% respectively. Comparison between them showed significant difference (P<0.05). Significant differences were also shown in the comparisons between the two groups in improving mental symptoms, either on the 10th or on the 20th day (P<0.05 and P<0.01 respectively), and in post-treatment cranial CT image (P<0.05). CONCLUSION: Better efficacy could be obtained by integrative medical therapy in treating PCT-MD.


Asunto(s)
Lesiones Encefálicas/tratamiento farmacológico , Medicamentos Herbarios Chinos/uso terapéutico , Trastornos Mentales/tratamiento farmacológico , Adulto , Anciano , Quimioterapia Combinada , Medicamentos Herbarios Chinos/efectos adversos , Femenino , Humanos , Masculino , Medicina Tradicional China/efectos adversos , Persona de Mediana Edad , Tomografía Computarizada por Rayos X , Resultado del Tratamiento
16.
Eur J Pharm Biopharm ; 66(3): 429-34, 2007 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-17196806

RESUMEN

Poly(2-hydroxy-3-phenoxypropylacrylate, 4-hydroxybutyl acrylate, dibutyl maleate) membrane was synthesized by UV curing method in our laboratory for the first time. When above-mentioned monomers were in the weight ratio of 4:4:2, the membrane not only had perfect permeation property but also had excellent plasticity, so the membrane made from monomers in the ratio of 4:4:2 was chosen as an optimized membrane. The optimized membrane provided perfect linear permeation properties in clonidine transdermal drug delivery system. The permeation rate decreased in proportion to the thickness of membrane. When the concentrations of clonidine were in the range of 0.5-7.0mg/ml, the permeation rate was proportional to the square root of clonidine concentrations. The optimized membrane was characterized by FTIR, DSC and SEM.


Asunto(s)
Clonidina/administración & dosificación , Sistemas de Liberación de Medicamentos , Membranas Artificiales , Piel/metabolismo , Acrilatos/administración & dosificación , Administración Cutánea , Clonidina/química , Maleatos/administración & dosificación , Permeabilidad , Polímeros/administración & dosificación , Polímeros/síntesis química , Rayos Ultravioleta
17.
Int J Pharm ; 322(1-2): 1-5, 2006 Sep 28.
Artículo en Inglés | MEDLINE | ID: mdl-16815655

RESUMEN

A new type of copolymer membranes was prepared through photosynthesis of mixtures of three different monomers. The membranes present a linear permeation property in clonidine transdermal drug delivery system. Monomers used in the photosynthesis were 2-hydroxy-3-phenoxypropylacrylate, 4-hydroxybutyl acrylate and sec-butyl tiglate. Permeation property of the membranes with different monomer ratios and thickness were investigated. When clonidine concentrations were in 3.0 - 5.0 mg/ml range, membranes showed near zero order permeation rates. An optimized membrane was characterized by FTIR, DSC and SEM.


Asunto(s)
Clonidina/química , Sistemas de Liberación de Medicamentos , Membranas Artificiales , Polímeros/síntesis química , Acrilatos/química , Acrilatos/efectos de la radiación , Administración Cutánea , Rastreo Diferencial de Calorimetría , Clonidina/administración & dosificación , Metacrilatos/química , Metacrilatos/efectos de la radiación , Microscopía Electrónica de Rastreo , Permeabilidad , Fotoquímica , Espectroscopía Infrarroja por Transformada de Fourier , Rayos Ultravioleta
18.
Zhongguo Zhong Yao Za Zhi ; 31(5): 411-3, 2006 Mar.
Artículo en Chino | MEDLINE | ID: mdl-16711429

RESUMEN

OBJECTIVE: To evaluate the effect of decoction for invigorating the kidney and improving blood circulation to thrombosis and pathology on rabbit blood stasis model. METHOD: Thirty rabbits were ramdomly divided into normal group, model group, high dose group, low dose group and Xue Shuan Ning group. Tissue-type plasminogen activator (t-PA), plasminogen activator inhibitor (PAI), fibrinogen (Fbg) and D-dimer (DD) were investigated after those rabbits had been treated. One rot was solected randomly from each group to observe pathological changes. RESULT: There were significant differences in t-PA, PAI, Fbg and DD between normal group and other groups is very obvious (P < 0.01) . Between groups of high dose low dose Xue Shuan Ning and model, the statistical differeces were significant, as well as between groups of high dose, low dose and Xue Shuan Ning groups (P < 0.05). However, there was no statistical difference between high dose group and high dose group (P > 0.05). The pathological changes in model group were most serious, those in Xue Shuan Ning were less serious. There were slight pathological changes in high dose group and low dose group. CONCLUSION: Models ware made successfully. High dose group and low dose group have stronger effect on thrombosis than Xue Shuan Ning group.


Asunto(s)
Viscosidad Sanguínea/efectos de los fármacos , Medicamentos Herbarios Chinos/farmacología , Plantas Medicinales , Trombosis/sangre , Activador de Tejido Plasminógeno/sangre , Animales , Relación Dosis-Respuesta a Droga , Combinación de Medicamentos , Medicamentos Herbarios Chinos/administración & dosificación , Medicamentos Herbarios Chinos/aislamiento & purificación , Femenino , Productos de Degradación de Fibrina-Fibrinógeno/metabolismo , Fibrinógeno/metabolismo , Hematócrito , Masculino , Plantas Medicinales/química , Inactivadores Plasminogénicos/sangre , Conejos , Distribución Aleatoria , Trombosis/patología
19.
Zhongguo Zhong Yao Za Zhi ; 29(8): 785-8, 2004 Aug.
Artículo en Chino | MEDLINE | ID: mdl-15506295

RESUMEN

OBJECTIVE: To investigate the nephrotoxocity of Longdan Xiegan Tang in rats, and to test its safety. METHOD: Sprague-Dauley rats were given Longdan Xiegan Tang 4.5 mL x (100 mg)(-1) Bid for thirty days, and the control group was given NS. MTP, BUN, Cr, MDA, MTP/Ucr and SOD were measured on 1st, 2nd, 3rd, 4th week. The kidney tissues were viewed with light microscopy and electron microscope. RESULT: MTP and MTP/Ucr were obviously higher than controls ( P < 0.01), and the other index had no difference (P > 0.05). No remarkable structural change could been seen with light microscopy, but with electron microscope we could find that the basal membranes were thickened and some of foot process were infused. CONCLUSION: Longdan Xiegan Tang will result in injury of kidney function.


Asunto(s)
Medicamentos Herbarios Chinos/toxicidad , Riñón/ultraestructura , Magnoliopsida , Plantas Medicinales , Animales , Membrana Basal/ultraestructura , Nitrógeno de la Urea Sanguínea , Creatinina/sangre , Combinación de Medicamentos , Medicamentos Herbarios Chinos/aislamiento & purificación , Gentiana/química , Corteza Renal/metabolismo , Magnoliopsida/química , Masculino , Malondialdehído/metabolismo , Plantas Medicinales/química , Proteinuria/inducido químicamente , Ratas , Ratas Sprague-Dawley , Superóxido Dismutasa/metabolismo
20.
Zhongguo Zhong Yao Za Zhi ; 29(5): 440-3, 2004 May.
Artículo en Chino | MEDLINE | ID: mdl-15706899

RESUMEN

OBJECTIVE: To evaluate the effect of decoction for invigorating the kidney and improving blood circulation to thrombosis on rabbits blood stasis model. METHOD: Thirty rabbits were randomly divided into normal group, model group, heavy dose group, slight dose group and xue shuan ning group. Tissue-type plasminogen activator (t-PA), plasminogen activator inhibitor (PAI), fibrinogen (Fbg) and D-dimer (DD) were investigated after those rabbits had been treated. One was selected randomly from each group to observe pathological changes. RESULT: There was significant difference in t-PA, PAI, Fbg and DD between normal group and other groups (P < 0.01). Among groups of heavy dose, slight dose, xue shuan ning and model, the statistical differences were significant, as well as among groups of heavy dose, slight dose and xue shuan ning (P < 0.05). However, there was no statistical difference between heavy dose group and slight dose group (P > 0.05). The pathological changes in model group were most serious, and those in xue shuan ning were less serious. There were slight pathological change in heavy dose group and light dose group. CONCLUSION: Models were made successfully. Heavy dose group and slight dose group have stronger effect on thrombosis than xue shuan ning group.


Asunto(s)
Medicamentos Herbarios Chinos/farmacología , Medicina Tradicional China , Trombosis/patología , Activador de Tejido Plasminógeno/sangre , Animales , Relación Dosis-Respuesta a Droga , Combinación de Medicamentos , Medicamentos Herbarios Chinos/administración & dosificación , Medicamentos Herbarios Chinos/aislamiento & purificación , Femenino , Productos de Degradación de Fibrina-Fibrinógeno/metabolismo , Fibrinógeno/metabolismo , Riñón/patología , Hígado/patología , Pulmón/patología , Masculino , Plantas Medicinales/química , Inactivadores Plasminogénicos/sangre , Conejos , Distribución Aleatoria , Trombosis/sangre
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