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1.
Cell Biochem Funct ; 42(3): e4018, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-38644608

RESUMEN

Long noncoding RNAs (lncRNAs) are a category of noncoding RNAs characterized by their length, often exceeding 200 nucleotides. There is a growing body of data that indicate the significant involvement of lncRNAs in a wide range of disorders, including cancer. lncRNA H19 was among the initial lncRNAs to be identified and is transcribed from the H19 gene. The H19 lncRNA exhibits significant upregulation in a diverse range of human malignancies, such as breast, colorectal, pancreatic, glioma, and gastric cancer. Moreover, the overexpression of H19 is frequently associated with a worse prognosis among individuals diagnosed with cancer. H19 has been shown to have a role in facilitating several cellular processes, including cell proliferation, invasion, migration, epithelial-mesenchymal transition, metastasis, and apoptosis. This article summarizes the aberrant upregulation of H19 in human malignancies, indicating promising avenues for future investigations on cancer diagnostics and therapeutic interventions.


Asunto(s)
Neoplasias , ARN Largo no Codificante , ARN Largo no Codificante/genética , ARN Largo no Codificante/metabolismo , Humanos , Neoplasias/genética , Neoplasias/patología , Neoplasias/metabolismo , Transición Epitelial-Mesenquimal/genética , Proliferación Celular , Apoptosis , Regulación Neoplásica de la Expresión Génica , Movimiento Celular
2.
Cell Biochem Funct ; 42(2): e3934, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38379261

RESUMEN

Immunometabolism, which studies cellular metabolism and immune cell function, is a possible cancer treatment. Metabolic pathways regulate immune cell activation, differentiation, and effector functions, crucial to tumor identification and elimination. Immune evasion and tumor growth can result from tumor microenvironment metabolic dysregulation. These metabolic pathways can boost antitumor immunity. This overview discusses immune cell metabolism, including glycolysis, oxidative phosphorylation, amino acid, and lipid metabolism. Amino acid and lipid metabolic manipulations may improve immune cell activity and antitumor immunity. Combination therapy using immunometabolism-based strategies may enhance therapeutic efficacy. The complexity of the metabolic network, biomarker development, challenges, and future approaches are all covered, along with a summary of case studies demonstrating the effectiveness of immunometabolism-based therapy. Metabolomics, stable isotope tracing, single-cell analysis, and computational modeling are also reviewed for immunometabolism research. Personalized and combination treatments are considered. This review adds to immunometabolism expertise and sheds light on metabolic treatments' ability to boost cancer treatment immunological response. Also, in this review, we discussed the immune response in cancer treatment and altering metabolic pathways to increase the immune response against malignancies.


Asunto(s)
Redes y Vías Metabólicas , Neoplasias , Humanos , Glucólisis , Neoplasias/metabolismo , Inmunidad , Aminoácidos/metabolismo , Microambiente Tumoral
3.
Cell Biochem Funct ; 42(1): e3921, 2024 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-38269511

RESUMEN

This comprehensive article explores the complex field of glioma treatment, with a focus on the important roles of non-coding RNAsRNAs (ncRNAs) and exosomes, as well as the potential synergies of immunotherapy. The investigation begins by examining the various functions of ncRNAs and their involvement in glioma pathogenesis, progression, and as potential diagnostic biomarkers. Special attention is given to exosomes as carriers of ncRNAs and their intricate dynamics within the tumor microenvironment. The exploration extends to immunotherapy methods, analyzing their mechanisms and clinical implications in the treatment of glioma. By synthesizing these components, the article aims to provide a comprehensive understanding of how ncRNAs, exosomes, and immunotherapy interact, offering valuable insights into the evolving landscape of glioma research and therapeutic strategies.


Asunto(s)
Exosomas , Vesículas Extracelulares , Glioma , Humanos , Inmunoterapia , Glioma/terapia , Microambiente Tumoral
4.
BMC Ophthalmol ; 24(1): 138, 2024 Mar 27.
Artículo en Inglés | MEDLINE | ID: mdl-38539111

RESUMEN

PURPOSE: To assess the level of agreement and evaluate the reliability of measurements between two Scheimpflug imaging modalities, Scansys (MediWorks, China) and Sirius (CSO, Italy), in quantifying the anterior segment parameters in healthy eyes. METHODS: In a cross-sectional study, the right eyes of 38 healthy participants without any ocular or systemic diseases were examined. A range of anterior segment parameters including anterior and posterior flat and steep keratometry, central corneal thickness (CCT), thinnest corneal thickness (TCT), anterior chamber depth (ACD), anterior chamber angle (ACA), corneal volume, anterior chamber volume, and horizontal white to white diameter, derived from the sagittal curvature maps were measured. To evaluate the reliability of the measurements, intraclass correlation coefficient (ICC) and correlation coefficient were measured. Additionally, Bland-Altman plots were employed to examine the agreement in mean (bias line) and 95% limits of agreement between the two devices. RESULTS: The mean age was 31.5 ± 6.9 (range: 19-47) years. The ICC indicated that the majority of anterior segment parameters had an excellent or good level of reliability, surpassing the threshold of 0.9. Nevertheless, CCT and ACA exhibited a moderate level of reliability, with ICC values of 0.794 and 0.728, respectively. The correlation analysis showed a strong correlation for all the variables tested. The Bland-Altman plots revealed that the bias line was near zero and the 95% limits of agreement were narrow for most variables, except for the anterior flat and steep keratometry, which were found to range from - 0.57 to 0.84 D and - 0.68 to 0.87 D, respectively. CONCLUSION: Scansys and Sirius devices can be effectively used interchangeably for the evaluation of most anterior segment parameters; however, for anterior corneal curvatures, CCT and ACA, their alternative use is not recommended.


Asunto(s)
Córnea , Tomografía , Humanos , Adulto Joven , Adulto , Reproducibilidad de los Resultados , Estudios Transversales , Estudios Prospectivos , Córnea/diagnóstico por imagen , Topografía de la Córnea/métodos , Tomografía de Coherencia Óptica
5.
Phytother Res ; 38(3): 1358-1366, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38200617

RESUMEN

Findings on the effect of walnut consumption on endothelial function are conflicting. Therefore, the present systematic review and meta-analysis summarized available trials in this regard. A systematic search was performed in online databases including PubMed-Medline, Scopus, and ISI Web of Science up to October 2023. Articles that reported the effect of walnut intake on flow-mediated dilation (FMD), intercellular adhesion molecule-1 (ICAM-1), vascular cell adhesion molecule-1 (VCAM-1), and stimulus-adjusted response measure (SARM) were included. Random effects models for a weighted mean difference (WMD) or standardized mean difference (SMD) were used to test for the overall effect. Six eligible trials were analyzed (250 participants). Walnut intake significantly increased FMD (WMD: 0.94%, 95% CI: 0.12 to 1.75; p = 0.02). However, meta-analysis could not show any beneficial effect of walnut intake on ICAM-1 (SMD: -0.23, 95% CI: -0.68 to 0.22; p = 0.31), VCAM-1 (SMD: -0.02, 95% CI: -1.38 to 1.34; p = 0.97), and SARM (WMD: 0.01%, 95% CI: -0.01 to 0.04; p = 0.28). In conclusion, the present meta-analysis suggests that walnuts may reduce cardiovascular disease risk by improving FMD. However, further studies should be performed on adults to determine the effect of walnut intake on endothelial function.


Asunto(s)
Juglans , Adulto , Humanos , Molécula 1 de Adhesión Intercelular , Nueces , Ensayos Clínicos Controlados Aleatorios como Asunto , Molécula 1 de Adhesión Celular Vascular
6.
Bioorg Chem ; 86: 473-481, 2019 05.
Artículo en Inglés | MEDLINE | ID: mdl-30772648

RESUMEN

The increasing resistance of pathogens to common antibiotics, as well as the need to control urease activity to improve the yield of soil nitrogen fertilization in agricultural applications, has stimulated the development of novel classes of molecules that target urease as an enzyme. In this context, the newly developed compounds on the basis of 1-heptanoyl-3-arylthiourea family were evaluated for Jack bean urease enzyme inhibition activity to validate their role as potent inhibitors of this enzyme. 1-Heptanoyl-3-arylthioureas were obtained in excellent yield and characterized through spectral and elemental analysis. All the compounds displayed remarkable potency against urease inhibition as compared to thiourea standard. It was found that novel compounds fulfill the criteria of drug-likeness by obeying Lipinski's rule of five. Particularly compound 4a and 4c can serve as lead molecules in 4D (drug designing discovery and development). Kinetic mechanism and molecular docking studies also carried out to delineate the mode of inhibition and binding affinity of the molecules.


Asunto(s)
Canavalia/enzimología , Inhibidores Enzimáticos/farmacología , Simulación del Acoplamiento Molecular , Tiourea/farmacología , Ureasa/antagonistas & inhibidores , Relación Dosis-Respuesta a Droga , Inhibidores Enzimáticos/química , Cinética , Estructura Molecular , Relación Estructura-Actividad , Tiourea/química , Ureasa/metabolismo
7.
Talanta ; 273: 125896, 2024 Jun 01.
Artículo en Inglés | MEDLINE | ID: mdl-38479027

RESUMEN

Bioanalysis faces challenges in achieving fast, reliable, and point-of-care (POC) determination methods for timely diagnosis and prognosis of diseases. POC devices often display lower sensitivity compared to laboratory-based methods, limiting their ability to quantify low concentrations of target analytes. To enhance sensitivity, the synthesis of new materials and improvement of the efficiency of the analytical strategies are necessary. Enzyme-mimicking materials have revolutionized the field of the fabrication of new high-throughput sensing devices. The integration of microfluidic chips with analytical techniques offers several benefits, such as easy miniaturization, need for low biological sample volume, etc., while also enhancing the sensitivity of the probe. The use enzyme-like nanomaterials in microfluidic systems can offer portable strategies for real-time and reliable detection of biological agents. Colorimetry and electrochemical methods are commonly utilized in the fabrication of nanozyme-based microfluidic systems. The review summarizes recent developments in enzyme-mimicking materials-integrated microfluidic analytical methods in biomedical analysis and discusses the current challenges, advantages, and potential future directions.


Asunto(s)
Técnicas Biosensibles , Técnicas Analíticas Microfluídicas , Nanoestructuras , Microfluídica/métodos , Sistemas de Atención de Punto , Miniaturización , Técnicas Biosensibles/métodos , Dispositivos Laboratorio en un Chip
8.
Pathol Res Pract ; 254: 155123, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-38277740

RESUMEN

Having been involved in complex cellular regulatory networks and cell-to-cell communications, non-coding RNAs (lncRNAs) have become functional carriers that transmit information between cells and tissues, modulate tumor microenvironments, encourage angiogenesis and invasion, and make tumor cells more resistant to drugs. Immune cells' exosomal lncRNAs may be introduced into tumor cells to influence the tumor's course and the treatment's effectiveness. Research has focused on determining if non-coding RNAs affect many target genes to mediate regulating recipient cells. The tumor microenvironment's immune and cancer cells are influenced by lncRNAs, which may impact a treatment's efficacy. The lncRNA-mediated interaction between cancer cells and immune cells invading the tumor microenvironment has been the subject of numerous recent studies. On the other hand, tumor-derived lncRNAs' control over the immune system has not gotten much attention and is still a relatively new area of study. Tumor-derived lncRNAs are recognized to contribute to tumor immunity, while the exact mechanism is unclear.


Asunto(s)
Neoplasias , ARN Largo no Codificante , Humanos , ARN Largo no Codificante/genética , Neoplasias/genética , Neoplasias/patología , Sistema Inmunológico/patología , Microambiente Tumoral/genética
9.
Front Chem ; 11: 1331933, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-38274894

RESUMEN

Recently, nanoscience, especially metal-organic frameworks (MOFs), has been used to increase the effectiveness and properties of drugs. In this study, by using microwave irradiation; penicillin, which is a known antibiotic; and copper metal-organic frameworks (Cu-MOFs), a new penicillinoate@copper metal-organic framework (penicillinoate@Cu-MOF) was synthesized. The structure and characterization of the newly synthesized compound were determined using FT-IR spectrums, EDAX analysis, elemental analysis, XRD patterns, SEM images, nitrogen adsorption/desorption curves, and TGA curve. Then, its antimicrobial effects were evaluated on numerous Gram-positive and Gram-negative bacterial strains and were compared with those of penicillin and gentamicin. In continuation of the biological activities, antioxidant tests were performed on the compounds using the DPPH method. For biological activities, the synthesized penicillinoate@Cu-MOF is much more effective than penicillin and Cu-MOF. The loading of penicillin on the nanostructure and the presence of copper in the final composition can be attributed to the high antibiotic properties of the synthesized composition.

10.
Ann Med Surg (Lond) ; 85(6): 2628-2634, 2023 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-37363492

RESUMEN

B-Raf proto-oncogene has been found in a variety of neoplasms. BRAF stimulation can promote tumour proliferation through the activation of the MAP/ERK kinase pathway. This study aimed to determine the germline spectra of BRAF and the association with pathological criteria of prostate tumours. Methods: Fifty blood samples from men treated with prostate cancer were analyzed for BRAF germline mutations and confirmed by Sanger sequencing, in addition, to establishing the frequencies and clinical correlations of frequent mutations in the BRAF gene for both exon 11 and exon 15. The frequency and distribution of high-frequency mutations were analyzed according to the pathological criteria of the patients. Results: Frameshift mutations: c.1628_1629insA and c.1624_1625insT with a frequency of (46%) and (18%), respectively, Nonsense mutations: c.1181C>A (p.Ser394Ter) was detected in one patient, missense mutations: c.1226A>G (p.Gln409Arg), c.1270T>C (p.Trp424Arg), c.1270_1271delins2 (p.Trp424Leu), with a frequency of (4%) were detected. There was no significant difference between mutation carriers and non-carriers regarding medical and surgical history, but prostate-specific antigen concentration was significantly different between the two groups. Conclusion: The results of this study elucidate the presence and involvement of germline mutations in prostate cancer, which could serve as a potential indicator for the diagnosis and therapeutic management of prostate cancer in the population studied.

11.
RSC Adv ; 13(48): 34122-34135, 2023 Nov 16.
Artículo en Inglés | MEDLINE | ID: mdl-38019984

RESUMEN

Researchers are increasingly focusing on using biomass waste for green synthesis of nanostructured materials since green reducing, capping, stabilizing and orientation agents play a significant role in final application. Wheat peel extract contains a rich source of reducing and structure orienting agents that are not utilized for morphological transformation of NiO nanostructures. Our study focuses on the role of wheat peel extract in morphological transformation during the synthesis of NiO nanostructures as well as in non-enzymatic electrochemical urea sensing. It was observed that the morphological transformation of NiO flakes into nanoplatelets took place in the presence of wheat peel extract during the preparation of NiO nanostructures and that both the lateral size and thickness of the nanostructures were significantly reduced. Wheat peel extract was also found to reduce the optical band gap of NiO. A NiO nanostructure prepared with 5 mL of wheat peel extract (sample 2) was highly efficient for the detection of urea without the use of urease enzyme. It has been demonstrated that the induced modification of NiO nanoplatelets through the use of structure-orienting agents in the wheat peel has enhanced their electrochemical performance. A linear range of 0.1 mM to 13 mM was achieved with a detection limit of 0.003 mM in the proposed urea sensor. The performance of the presented non-enzymatic urea sensor was evaluated in terms of selectivity, stability, reproducibility, and practical application, and the results were highly satisfactory. As a result of the high surface active sites on sample 2, the low charge transfer resistance, as well as the high exposure to the surface active sites of wheat peel extract, sample 2 demonstrated enhanced performance. The wheat peel extract could be used for the green synthesis of a wide range of nanostructured materials, particularly metal/metal oxides for various electrochemical applications.

12.
Micromachines (Basel) ; 14(3)2023 Mar 19.
Artículo en Inglés | MEDLINE | ID: mdl-36985084

RESUMEN

To determine urea accurately in clinical samples, food samples, dairy products, and agricultural samples, a new analytical method is required, and non-enzymatic methods are preferred due to their low cost and ease of use. In this study, bitter gourd peel biomass waste is utilized to modify and structurally transform nickel oxide (NiO) nanostructures during the low-temperature aqueous chemical growth method. As a result of the high concentration of phytochemicals, the surface was highly sensitive to urea oxidation under alkaline conditions of 0.1 M NaOH. We investigated the structure and shape of NiO nanostructures using powder X-ray diffraction (XRD) and scanning electron microscopy (SEM). In spite of their flake-like morphology and excellent crystal quality, NiO nanostructures exhibited cubic phases. An investigation of the effects of bitter gourd juice demonstrated that a large volume of juice produced thin flakes measuring 100 to 200 nanometers in diameter. We are able to detect urea concentrations between 1-9 mM with a detection limit of 0.02 mM using our urea sensor. Additionally, the stability, reproducibility, repeatability, and selectivity of the sensor were examined. A variety of real samples, including milk, blood, urine, wheat flour, and curd, were used to test the non-enzymatic urea sensors. These real samples demonstrated the potential of the electrode device for measuring urea in a routine manner. It is noteworthy that bitter gourd contains phytochemicals that are capable of altering surfaces and activating catalytic reactions. In this way, new materials can be developed for a wide range of applications, including biomedicine, energy production, and environmental protection.

13.
Biosensors (Basel) ; 13(4)2023 Mar 31.
Artículo en Inglés | MEDLINE | ID: mdl-37185519

RESUMEN

The electrochemical performance of NiCo2O4 with urea precursors was evaluated in order to develop a non-enzymatic urea sensor. In this study, NiCo2O4 nanostructures were synthesized hydrothermally at different concentrations of urea and characterized using scanning electron microscopy and X-ray diffraction. Nanostructures of NiCo2O4 exhibit a nanorod-like morphology and a cubic phase crystal structure. Urea can be detected with high sensitivity through NiCo2O4 nanostructures driven by urea precursors under alkaline conditions. A low limit of detection of 0.05 and an analytical range of 0.1 mM to 10 mM urea are provided. The concentration of 006 mM was determined by cyclic voltammetry. Chronoamperometry was used to determine the linear range in the range of 0.1 mM to 8 mM. Several analytical parameters were assessed, including selectivity, stability, and repeatability. NiCo2O4 nanostructures can also be used to detect urea in various biological samples in a practical manner.


Asunto(s)
Glucosa , Nanoestructuras , Animales , Glucosa/química , Urea , Leche , Óxidos/química , Níquel , Cobalto/química , Nanoestructuras/química , Técnicas Electroquímicas
14.
Phytother Res ; 26(4): 552-6, 2012 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-21953729

RESUMEN

A study was conducted to identify constituents that might be responsible for analgesic and antiinflammatory conditions. Tasumatrol B, 1,13-diacetyl-10-deacetylbaccatin III (10-DAD) and 4-deacetylbaccatin III (4-DAB) were isolated from the bark extract of Taxus wallichiana Zucc. All the compounds were assessed for analgesic and antiinflammatory activities using an acetic acid-induced writhing model, a hot-plate test, a carrageenan-induced paw oedema model, a cotton-pellet oedema model and in vitro lipoxygenase inhibitory assay. All the compounds, especially tasumatrol B, revealed significant analgesic activity in comparison to a saline group based on an acetic acid-induced model. Similarly all of the test compounds, particularly tasumatrol B, showed significant antiinflammatory activity. However, all the compounds failed to exhibit any considerable activity in of the hot-plate test and the in vitro lipoxygenase inhibitory assay. This study has highlighted the potential of tasumatrol B to be further explored as a new lead compound for the management of pain and inflammation, one that has been discovered by scientific validation of the traditional medicinal use of T. wallichiana Zucc.


Asunto(s)
Analgésicos/uso terapéutico , Antiinflamatorios/uso terapéutico , Fitoterapia , Taxoides/uso terapéutico , Taxus/química , Ácido Acético/efectos adversos , Analgésicos/aislamiento & purificación , Animales , Antiinflamatorios/aislamiento & purificación , Carragenina/efectos adversos , Evaluación Preclínica de Medicamentos , Edema/inducido químicamente , Edema/tratamiento farmacológico , Femenino , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Inhibidores de la Lipooxigenasa/aislamiento & purificación , Inhibidores de la Lipooxigenasa/uso terapéutico , Masculino , Dolor/inducido químicamente , Dolor/tratamiento farmacológico , Corteza de la Planta/química , Ratas , Ratas Wistar , Taxoides/aislamiento & purificación , Taxoides/farmacología
15.
J Enzyme Inhib Med Chem ; 24(1): 224-9, 2009 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-18825532

RESUMEN

The antibacterial, antifungal, acute cytotoxicity, phytotoxicity and insecticidal profile of the crude extract and various fractions of Indigofera gerardiana have been studied. Six bacterial and fungal strains were used, of which Samonella typhi and Microsporum canis were the most susceptible strains with MICs 0.37 mg/mL and 0.09 mg/mL, respectively. The crude extract and the fractions showed low insecticidal activity against Sitophilus oryzae, Rhyzopertha dominica and Callosbruchus analis but no activity against Tribolium castaneum. The brine shrimp lethality assay showed absence of any measurable cytotoxicity of the crude extract and fractions, showing a good safety profile at a preliminary level. All the fractions except crude extract revealed profound and highly significant herbicidal activity against Lemna minor at the concentration of 1000 microg/mL. Indigofera gerardiana was shown by in-vitro assays to be a potential source for natural antifungal, antibacterial and herbicidal agents.


Asunto(s)
Antibacterianos/farmacología , Antifúngicos/farmacología , Citotoxinas/farmacología , Herbicidas/farmacología , Indigofera/química , Insecticidas/farmacología , Extractos Vegetales/farmacología , Animales , Antibacterianos/aislamiento & purificación , Antifúngicos/aislamiento & purificación , Citotoxinas/aislamiento & purificación , Herbicidas/aislamiento & purificación , Insecticidas/aislamiento & purificación , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/aislamiento & purificación
16.
J Ayub Med Coll Abbottabad ; 17(2): 23-5, 2005.
Artículo en Inglés | MEDLINE | ID: mdl-16092644

RESUMEN

BACKGROUND: A review of the literature shows that refugees in different parts of the world have high rates of psychological and emotional problems. However, psychiatric morbidity among Afghan refugees in Pakistan has been poorly studied. Most of the studies of psychiatric disorders come from western countries. However, these studies may not be representative of the Afghan refugees in Pakistan. This study was carried out to measure psychiatric morbidity among a group of Afghan refugees attending a psychiatric clinic in Peshawar, Pakistan. METHODS: This is a cross sectional study, to measure prevalence of psychiatric morbidity among the residents of Afghan refugee camps in Peshawar, Pakistan, who attended a psychiatric clinic between November 2003 and February 2004. Data were collected using Mini International neuropsychiatry Interview Schedule (MINI), and a form specifically developed for the study. RESULTS: Nearly 80% of our patients had a diagnosis of Post Traumatic Stress Disorder. Nearly half (47.9%) reported family history of mental illness, while almost a quarter (23.3%) had a physical disability or long term illness. Only 13.7% (106) had contacted health services prior to seeking help for their psychiatric illness. CONCLUSIONS: A high number of patients presenting with PTSD is not an unusual finding when one considers the traumatic experiences faced by the general population of Afghanistan. Only a small number of the patients had been in contact with the health services prior to their contact with the psychiatric service. This study highlights the importance of health education among Afghan refugees and to establish the mental health services for them.


Asunto(s)
Trastornos Mentales/epidemiología , Refugiados/psicología , Trastornos por Estrés Postraumático/epidemiología , Adolescente , Adulto , Afganistán/etnología , Estudios Transversales , Femenino , Humanos , Entrevistas como Asunto , Masculino , Persona de Mediana Edad , Pakistán/epidemiología , Prevalencia , Refugiados/estadística & datos numéricos
17.
Fitoterapia ; 82(7): 1008-11, 2011 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-21703333

RESUMEN

Zizyphus oxyphylla Edgew is used in Pakistan as a folk medicinal remedy for inflammatory conditions, pains especially rheumatic pain, fevers, allergy and diabetes. The aim of the current study was to scientifically validate the folk use of Z. oxyphylla Edgew by using the isolated compound in vitro and in vivo levels. Kushecarpin A was isolated from ethyl acetate fraction of the plant crude extract. Molecular docking simulations predicted Kushecarpin A as a potential new lipoxygenase (LOX) inhibitor. Kushecarpin A showed significant lipoxygenase inhibition (IC(50): 7.2 ± 0.02 µM) thus validated computational prediction. It also exhibited significant and highly significant inhibition (p < 0.05 and p < 0.01) of carrageenan-induced hind paw oedema at the doses of 5, 10 and 20 mg/kg. Kushecarpin A seems to be a potentially new anti-inflammatory compound responsible for anti-inflammatory activities of Z. oxyphylla Edgew. In vitro and in vivo anti-inflammatory inflammatory activities were found in good agreement with the folk medicinal use of Z. oxyphylla Edgew in inflammatory disorders.


Asunto(s)
Edema/tratamiento farmacológico , Compuestos Heterocíclicos de 4 o más Anillos/uso terapéutico , Inhibidores de la Lipooxigenasa/uso terapéutico , Lipooxigenasa/metabolismo , Fitoterapia , Extractos Vegetales/uso terapéutico , Ziziphus/química , Animales , Simulación por Computador , Edema/metabolismo , Compuestos Heterocíclicos de 4 o más Anillos/aislamiento & purificación , Compuestos Heterocíclicos de 4 o más Anillos/farmacología , Inhibidores de la Lipooxigenasa/aislamiento & purificación , Inhibidores de la Lipooxigenasa/farmacología , Pakistán , Componentes Aéreos de las Plantas , Extractos Vegetales/química , Extractos Vegetales/farmacología , Ratas
18.
Fitoterapia ; 81(8): 1020-5, 2010 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-20600681

RESUMEN

The main aim of the current study was to explore molecular insights for potentially new dual cholinesterase inhibitor(s) from Asparagus adscendens via molecular docking. This medicinal plant is traditionally used as a nerve tonic and remedy for memory impairments. Conypododiol was isolated from the chloroform fraction of methanolic extract of A. adscendens, based on bioactivity guided isolation. Conypododiol exhibited significant inhibition of both acetylcholinesterase and butyrylcholinesterase, having the IC(50) values 2.17 ± 0.1 µM and 11.21 ± 0.1 µM, respectively. IC(50) values of the standard compound Galanthamine for both the enzymes were 0.537 ± 0.018 µM and 8.6 ± 0.27 µM, respectively. Based on MTT cytotoxicity assay, Conypododiol was found safe against LCMK-2 monkey kidney epithelial cells and mice hepatocytes. Molecular docking studies revealed the hydrogen bonding interactions of Conypododiol with His440 and Ser200 at esteratic site (ES), and also with Tyr334 at peripheral anionic site (PAS) of the aromatic gorge of acetylcholinesterase. Simultaneous contacts of Conypododiol with PAS and ES shows its significance as a bivalent ligand. This preliminary study highlighted the potential of Conypododiol to be further developed and modified as new lead compound identified by its folk use.


Asunto(s)
Alquenos/química , Alquenos/farmacología , Asparagus/química , Inhibidores de la Colinesterasa/química , Inhibidores de la Colinesterasa/farmacología , Furanos/química , Furanos/farmacología , Acetilcolinesterasa/metabolismo , Alquenos/metabolismo , Animales , Butirilcolinesterasa/metabolismo , Inhibidores de la Colinesterasa/metabolismo , Furanos/metabolismo , Ratones , Estructura Molecular
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