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1.
Dalton Trans ; 53(1): 65-73, 2023 Dec 19.
Artículo en Inglés | MEDLINE | ID: mdl-37955357

RESUMEN

A tridentate ligand LH3 ((2-hydroxy-3-methoxybenzylidene)-2-(hydroxyimino)propanehydrazide) comprising o-vanillin, hydrazone and oxime donor groups has been employed to prepare a series of tetranuclear Ln(III) complexes. The reaction of ligand LH3 with Ln(NO3)3 [Ln = Sm, Eu, Gd, Tb, Dy, Ho, Er] in MeOH yielded Ln4(LH)6(MeOH)2 (Ln = Sm(1), Eu(2), Gd(3), Tb(4), Ho (6) and Er (7))] whereas the corresponding reaction with Dy(NO3)3 afforded Dy4(LH)4(LH2)2(OH)2 (5). All complexes were characterized by various analytical techniques including single crystal X-ray diffraction, IR spectroscopy, UV-Vis spectroscopy, and elemental analysis. To investigate the potential of these lanthanide complexes for wound healing applications, their effects on fibroblast viability, migration, and M2 macrophage polarization were evaluated. The cytotoxicity assessment revealed that complexes 2(Eu), 4(Tb), 5(Dy), and 7(Er) significantly enhanced fibroblast viability compared to the negative control (NC). In vitro wound healing assay demonstrated that complexes 2(Eu) and 7(Eu) substantially promoted fibroblast migration compared to the NC. Moreover, complex 2(Eu) exhibited significant anti-inflammatory effects by reducing the phagocytic ability of lipopolysaccharide (LPS)-stimulated macrophage cells and attenuating nitric oxide (NO) production. In conclusion, among the series of complexes tested, complex 2(Eu) displayed the most potent anti-inflammatory effect on macrophage cells, while simultaneously promoting fibroblast viability and migration. This unique combination of properties renders complex 2 (Eu) highly promising for wound healing applications.


Asunto(s)
Elementos de la Serie de los Lantanoides , Elementos de la Serie de los Lantanoides/farmacología , Elementos de la Serie de los Lantanoides/química , Ligandos , Fibroblastos , Macrófagos , Antiinflamatorios
2.
Methods Appl Fluoresc ; 10(4)2022 Jul 28.
Artículo en Inglés | MEDLINE | ID: mdl-35856854

RESUMEN

Thein vitropanel of technologies to address biomolecular interactions are in play, however microscale thermophoresis is continuously increasing in use to represent a key player in this arena. This review highlights the usefulness of microscale thermophoresis in the determination of molecular and biomolecular affinity interactions. This work reviews the literature from January 2016 to January 2022 about microscale thermophoresis. It gives a summarized overview about both the state-of the art and the development in the field of microscale thermophoresis. The principle of microscale thermophoresis is also described supported with self-created illustrations. Moreover, some recent advances are mentioned that showing application of the technique in investigating biomolecular interactions in different fields. Finally, advantages as well as drawbacks of the technique in comparison with other competing techniques are summarized.

3.
J Tradit Complement Med ; 12(4): 367-374, 2022 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-35747348

RESUMEN

Background: and purpose: The formation of postoperative intra-abdominal adhesion band formation may lead to severe complications. This study aimed to evaluate the preventive effect of local administration of frankincense n-hexane extract (FHE) on the formation of postsurgical adhesion bands. Materials and methods: FHE was extracted from the resin of a Boswellia sacra tree and its components were identified by gas chromatography-mass spectrometry (GC-MS). In an animal model, the expression levels of TNF-α and TGF-ß1 cytokines after application of FHE were assessed to check the inflammatory and fibrotic cues, respectively. Results: Following FHE compound analysis, in vivo experiments demonstrated that intraoperative local administration of FHE resulted in the prevention of adhesion band formation. The adhesion grades in the FHE-treated group were significantly lower than those in the negative control (NC) and the positive control (Interceed). The infiltration of inflammatory cells observed by histopathology revealed a significant anti-inflammatory potential of FHE. Furthermore, the gene expression results proved that significant suppression of TNF-α and TGF-ß1 was responsible for its antiadhesion properties. Conclusions: The study reported the potential of FHE as an ointment for the prevention of adhesion bands.

4.
Carbohydr Polym ; 262: 117921, 2021 Jun 15.
Artículo en Inglés | MEDLINE | ID: mdl-33838800

RESUMEN

The aim of this study was to evaluate a bioactive multilayer wound dressing, based on chitosan and alginate. To enhance healing potential, Dracaena Cinnabari and Aloe Vera were loaded as separate layers into the scaffold. The bare and bioactive multilayered scaffolds were fabricated by an iterative layering freeze-drying technique. Following of topographical, chemical, and physical assessment, the performance of the scaffolds was evaluated in vitro and in vivo. The results revealed adequate attachment, and proliferation of human foreskin fibroblasts, indicating excellent biocompatibility of the bioactive scaffold. In vivo, the performance of the multi-layered scaffold loaded with the bioactive materials was comparable with Comfeel plus®. The wounds treated with the bioactive scaffold exhibited superior hypergranulation, fibroblast maturation, epithelization, and collagen deposition, with minimal inflammation, and crust formation. It is concluded that the synergism of extracellular matrix-mimicking multi-layered scaffolding with Aloe Vera and Dracaena Cinnabari could be considered as a supportive wound dressing.


Asunto(s)
Alginatos/química , Vendajes , Quitosano/química , Extractos Vegetales/farmacología , Andamios del Tejido/química , Cicatrización de Heridas/efectos de los fármacos , Alginatos/farmacología , Aloe/química , Animales , Proliferación Celular/efectos de los fármacos , Quitosano/farmacología , Colágeno/metabolismo , Dracaena/química , Matriz Extracelular/metabolismo , Fibroblastos/efectos de los fármacos , Prepucio/patología , Humanos , Masculino , Microscopía Electrónica de Rastreo/métodos , Extractos Vegetales/química , Ratas , Ratas Wistar
5.
Mol Biol Rep ; 47(7): 5421-5430, 2020 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-32623616

RESUMEN

Among medicinal plants, Acridocarpus orientalis (AO) possesses a remarkable anti-cancer potential, possibly because of its anti-oxidant property. In this study, the leaf and stem extracts from AO were assessed to find the bioactive compound with selective anti-cancer properties. The MTT viability and live and dead assays revealed that around 80% and 98% of 4T1 cells survival were declined after 48 h incubation with leaf and stem extracts, respectively. The leaf extract increased stem cell proliferation by 20% whereas the stem extract inhibited around 22% of stem cells proliferation after 48 h treatment. The live and dead assay of MSCs confirmed that 40% of the MSCs died when treated with AO stem extract. On the other hand, there were no dead cells after two days of treatment with the leaf extract. Followed by the induction of cell cycle arrest in G0/G1-phase, the real-time PCR demonstrated apoptosis properties in 4T1 cells through overexpression of Bax and down-regulation of BCL2 genes. Interestingly, within the pure compounds isolated from AO leaf extract, Morin was responsible for the inhibition of 4T1 cells proliferation as well as MSCs expansion, predicting to play an essential role in the treatment of cancer. The promising in vitro anti-cancer and stem cell-inductive properties of morin isolated from AO extract may provide a great potential to produce selective herbal derived drugs.


Asunto(s)
Malpighiaceae/metabolismo , Extractos Vegetales/farmacología , Apoptosis/efectos de los fármacos , Puntos de Control del Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Humanos , Células Madre Mesenquimatosas/efectos de los fármacos , Células Madre Mesenquimatosas/metabolismo , Hojas de la Planta/metabolismo , Tallos de la Planta/metabolismo , Plantas Medicinales/metabolismo
6.
Phytochem Anal ; 29(1): 16-22, 2018 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-28741853

RESUMEN

INTRODUCTION: Citrullus colocynthis (L.) Schrad is extensively used to treat diabetes, obesity, fever, cancer, amenorrhea, jaundice, leukemia, rheumatism, and respiratory diseases. Chemical studies have indicated the presence of several cucurbitacins, flavones, and other polyphenols in this plant. These phytochemical constituents are responsible for the interesting antioxidant and other biological activities of C. colocynthis. OBJECTIVE: In the present study, for the first time, near infrared (NIR) spectroscopy coupled with partial least square (PLS) regression analysis was used to quantify the polyphenolic phytochemicals of C. colocynthis. METHODOLOGY: The fruit and aerial parts of the C. colocynthis were extracted individually in methanol followed by fractionation in n-hexane, chloroform, ethyl acetate, n-butanol, and water. Near infrared (NIR) spectra were obtained in absorption mode in the wavelength range 700-2500 nm. The PLS regression model was then built from the obtained spectral data to quantify the total polyphenol contents in the selected plant samples. RESULTS: The PLS regression model obtained had a R2 value of 99% with a 0.98 correlationship value and a good prediction with a root mean square error of prediction (RMSEP) value of 1.89% and correlation of 0.98. These results were further confirmed through UV-vis spectroscopy and it is found that the ethyl acetate fraction has the maximum value for polyphenol contents (101.7 mg/100 g; NIR, 100.4 mg/100 g; UV-vis). CONCLUSIONS: The polyphenolic phytochemicals of the fruit and aerial parts of C. colocynthis have been quantified successfully by using multivariate analysis in a non-destructive, economical, precise, and highly sensitive method, which uses very simple sample preparation. Copyright © 2017 John Wiley & Sons, Ltd.


Asunto(s)
Citrullus colocynthis/química , Frutas/química , Componentes Aéreos de las Plantas/química , Polifenoles/química , Análisis de los Mínimos Cuadrados , Análisis Multivariante , Fitoquímicos/química , Espectroscopía Infrarroja Corta/métodos
7.
Bioorg Chem ; 67: 95-104, 2016 08.
Artículo en Inglés | MEDLINE | ID: mdl-27299811

RESUMEN

Two new pregnane glycosides named desmiflavasides C (1) and D (2) were isolated from the sap of Desmidorchis flava (N.E.Br.) Meve & Liede and have had their structures confirmed from 1D and 2D NMR spectroscopic techniques and mass spectrometry (ESIMS). Further, the effects of desmiflavasides C (1) and D (2) on the proliferation of breast and ovarian cancer cells as well as normal breast epithelial cells in culture were examined. Interestingly, desmiflavasides C (1) and D (2) were able to cause a substantial decline in the viability of cancer cells in a concentration-dependent manner. Moreover, treatment of normal cells with compound 2 resulted in no significant growth inhibition, indicating that its cytotoxicity was selective towards cancer cells. Furthermore, the activity of compound 2 against cancer as well as normal epithelial cells was found to be similar to that of a previously reported pregnane glycoside, nizwaside (3). Molecular docking studies of desmiflavasides C (1) and D (2) and nizwaside (3) were carried out to ascertain if it was possible to predict any important binding orientations required of small molecule drug candidates with suggested protein target molecules for the purposes of being able to predict the affinity and activity to an acceptable degree by such compounds. Desmiflavaside D (2) showed a relatively good binding affinity (-22.4449kcal/mol) as compared to the other two compounds viz., nizwaside (3) (-20.0319kcal/mol), and desmiflavaside C (1) (-19.4042kcal/mol). Docking results of the three pregnane glycosides viz., 1-3 revealed that these ligand molecules can accurately interact with the target protein.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Apocynaceae/química , Glicósidos/farmacología , Simulación del Acoplamiento Molecular , Pregnanos/farmacología , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Glicósidos/química , Glicósidos/aislamiento & purificación , Humanos , Estructura Molecular , Pregnanos/química , Pregnanos/aislamiento & purificación , Relación Estructura-Actividad
8.
Arch Pharm Res ; 38(12): 2137-42, 2015 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-26335549

RESUMEN

The sap from the succulent Desmidorchis flava (N.E.Br) Meve and Liede yielded a new pregnane glycoside, named nizwaside whose structure was established using 1D and 2D NMR techniques as well as mass spectrometry (ESIMS). Nizwaside was tested for anticancer, DPPH antioxidant, urease enzyme inhibition, α-glucosidase enzyme inhibition and acetylcholinesterase inhibition activities. Interestingly, nizwaside showed significant anti-proliferative effects on MDA MB231 breast cancer cells with an IC(50) of 23.5 µg/ml. Moreover, nizwaside was more effective than Doxorubicin, a well-known clinical anticancer drug, in suppressing MDA MB231 cell proliferation even at concentrations lower than that of Doxorubicin (75 µg/ml nizwaside vs. 100 µg/ml Doxorubicin). On the other hand, nizwaside showed relatively weak antioxidant activity with 15 % inhibition.


Asunto(s)
Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Apocynaceae , Glicósidos/química , Glicósidos/aislamiento & purificación , Pregnanos/química , Pregnanos/aislamiento & purificación , Antineoplásicos Fitogénicos/farmacología , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Supervivencia Celular/fisiología , Relación Dosis-Respuesta a Droga , Femenino , Glicósidos/farmacología , Humanos , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Pregnanos/farmacología
9.
Asian Pac J Trop Med ; 7S1: S591-8, 2014 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-25312188

RESUMEN

OBJECTIVE: To assess the nutritional values and antioxidant analysis of 22 varieties of date palm (Phoenix dactylifera) fruit collected from various regions of the Sultanate of Oman. METHODS: Nutritional parameters including moisture, fats, fiber, proteins, carbohydrates, and energy value were determined using standard methods of Association of Official Analytical Chemists. The antioxidant activity was screened for their free radical scavenging properties using ascorbic acid as a standard antioxidant. Free radical scavenging activity was evaluated using 1,1-diphenyl-2-picrylhydrazyl free radical. RESULTS: The results of the date fruits (dried/tamar stage) revealed significantly higher moisture (15%-21%), dry matter (78%-86%), ash content (1.0%-2.0%), fiber (1.0%-2.5%), fat (0.1%-0.7%), protein (1.8%-3.8%), nitrogen (0.25%-0.55%), carbohydrates (74.5%-82.4%), and energy values (307-345.5 kcal/100 g). The antioxidant activity ranged between 40% and 86% depending upon the type of date and location. Overall, Khalas, Fardh and Khasab have significantly higher nutritional attributes; however, other varieties such as Barshi, Qush LuLu, Handal, and Khunaizi also have comparable nutritional values. The cluster analysis further evidenced the correlation of proximate parameters in different locations. Moreover, the nutritional and antioxidant attributes of similar date varieties collected from different locations were slightly varied. CONCLUSIONS: The present finding helps in understanding the nutritional significance of different date varieties in Oman while the lesser known varieties can be improved through sustainable horticultural practices as a valuable product. The study further reveals that the consumption of these dates' fruits would exert several beneficial effects by virtue of their antioxidant activity.

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