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1.
Front Microbiol ; 15: 1358467, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38468852

RESUMEN

Introduction: Evaluating the anticancer property of Padina boergesenii mediated bimetallic nanoparticles. Methods: The present study focuses on synthesizing Se-ZnO bimetallic nanoparticles from an aqueous algal extract of brown algae Padina boergesenii.Synthesized Se-ZnO NPs were characterized by UV, FTIR, SEM-EDS and HRTEM for confirmation along with the anticancer activity by MTT assay. Results: The UV gave an absorbance peak at 342 and 370 nm, and the FTIR showed functional groups involved in synthesizing Se-ZnO NPs. The TEM micrographs indicated the crystalline nature and confirmed the size of the Se-ZnO NPs to be at an average size of 26.14 nm. Anticancer efficacy against the MCF-7 breast and HepG2 (hepatoblastoma) cell lines were also demonstrated, attaining an IC50 value of 67.9 µg and 74.9 µg/ml respectively, which caused 50% cell death. Discussion: This work aims to highlight an effective method for delivering bioactive compounds extracted from brown algae and emphasize its future therapeutic prospects. The potential of Selenium-Zinc oxide nanoparticles is of great interest due to the biocompatibility and low toxicity aspects of selenium combined with the cost-effectiveness and sustainability of zinc metal. The presence of bioactive compounds contributed to the stability of the nanoparticles and acted as capping properties.

2.
Sci Rep ; 14(1): 2204, 2024 01 25.
Artículo en Inglés | MEDLINE | ID: mdl-38273022

RESUMEN

In the present study, ZnO nanoparticles have been synthesized using an aqueous extract of shilajit. The nanoparticles were characterized using different techniques such as UV (ultraviolet-visible spectrophotometer), FTIR (Fourier transform infrared), XRD (X-ray diffraction), particle size analysis, SEM (scanning electron microscope) and EDAX (Energy-dispersive X-ray) analysis. The UV absorption peak at 422.40 nm was observed for ZnO nanoparticles. SEM analysis showed the shape of nanoparticles to be spherical, FTIR spectrum confirmed the presence of zinc atoms, particle size analysis showed the nanoparticle size, EDAX confirmed the purity of ZnO nanoparticles whereas XRD pattern similar to that of JCPDS card for ZnO confirmed the presence of pure ZnO nanoparticles. The in vitro anticancer activity of ZnO nanoparticles against the HeLa cell line showed the IC50 value of 38.60 µg/mL compared to reference standard cisplatin. This finding confirms that ZnO nanoparticles from shilajit extract have potent cytotoxic effect on human cervical cancer cell lines.


Asunto(s)
Nanopartículas del Metal , Minerales , Nanopartículas , Resinas de Plantas , Óxido de Zinc , Humanos , Óxido de Zinc/farmacología , Óxido de Zinc/metabolismo , Células HeLa , Antibacterianos/farmacología , Extractos Vegetales/farmacología , Difracción de Rayos X , Espectroscopía Infrarroja por Transformada de Fourier , Pruebas de Sensibilidad Microbiana
3.
J Enzyme Inhib Med Chem ; 29(4): 555-62, 2014 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-25019596

RESUMEN

HDAC inhibitors emerged as promising drug candidates in combating wide variety of cancers. At present, two of the compounds SAHA and Romidepsin were approved by FDA for cutaneous T-cell lymphoma and many are in various clinical phases. A new quinolone cap structure was explored with hydroxamic acid as zinc-binding group (ZBG). The pan HDAC inhibitory and antiproliferative activities against three human cancer cell lines HCT-116 (colon), NCI-H460 (lung) and U251 (glioblastoma) of the compounds (4a-4w) were evaluated. Introduction of heterocyclic amines in CAP region increased the enzyme inhibitory and antiproliferative activities and few of the compounds tested are metabolically stable in both MLM and HLM.


Asunto(s)
Antineoplásicos/farmacología , Inhibidores de Histona Desacetilasas/farmacología , Histona Desacetilasas/metabolismo , Quinolonas/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/química , 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 , Activación Enzimática/efectos de los fármacos , Células HCT116 , Inhibidores de Histona Desacetilasas/síntesis química , Inhibidores de Histona Desacetilasas/química , Humanos , Estructura Molecular , Quinolonas/síntesis química , Quinolonas/química , Relación Estructura-Actividad
4.
Int Immunopharmacol ; 16(1): 72-8, 2013 May.
Artículo en Inglés | MEDLINE | ID: mdl-23541634

RESUMEN

Epigenetic modifications represent a promising new approach to modulate cell functions as observed in autoimmune diseases. Emerging evidence suggests the utility of HDAC inhibitors in the treatment of chronic immune and inflammatory disorders. However, class and isoform selective inhibition of HDAC is currently favored as it limits the toxicity that has been observed with pan-HDAC inhibitors. HDAC6, a member of the HDAC family, whose major substrate is α-tubulin, is being increasingly implicated in the pathogenesis of inflammatory disorders. The present study was carried out to study the potential anti-inflammatory and anti-rheumatic effects of HDAC6 selective inhibitor Tubastatin. Tubastatin, a potent human HDAC6 inhibitor with an IC50 of 11 nM showed significant inhibition of TNF-α and IL-6 in LPS stimulated human THP-1 macrophages with an IC50 of 272 nM and 712 nM respectively. Additionally, Tubastatin inhibited nitric oxide (NO) secretion in murine Raw 264.7 macrophages dose dependently with an IC50 of 4.2 µM and induced α-tubulin hyperacetylation corresponding to HDAC6 inhibition in THP-1 cells without affecting the cell viability. Tubastatin showed significant inhibition of paw volume at 30 mg/kg i.p. in a Freund's complete adjuvant (FCA) induced animal model of inflammation. The disease modifying activity of Tubastatin was also evident in collagen induced arthritis DBA1 mouse model at 30 mg/kg i.p. The significant attenuation of clinical scores (~70%) by Tubastatin was confirmed histopathologically and was found comparable to dexamethasone (~90% inhibition of clinical scores). Tubastatin showed significant inhibition of IL-6 in paw tissues of arthritic mice. The present work has demonstrated anti-inflammatory and antirheumatic effects of a selective HDAC6 inhibitor Tubastatin.


Asunto(s)
Antiinflamatorios/uso terapéutico , Antirreumáticos/uso terapéutico , Artritis Experimental/tratamiento farmacológico , Inhibidores de Histona Desacetilasas/uso terapéutico , Ácidos Hidroxámicos/uso terapéutico , Indoles/uso terapéutico , Inflamación/tratamiento farmacológico , Animales , Antiinflamatorios/farmacología , Antirreumáticos/farmacología , Artritis Experimental/metabolismo , Artritis Experimental/patología , Línea Celular , Línea Celular Tumoral , Femenino , Adyuvante de Freund , Histona Desacetilasa 6 , Inhibidores de Histona Desacetilasas/farmacología , Histona Desacetilasas/metabolismo , Humanos , Ácidos Hidroxámicos/farmacología , Indoles/farmacología , Inflamación/inducido químicamente , Inflamación/metabolismo , Interleucina-6/metabolismo , Ratones , Ratones Endogámicos DBA , Óxido Nítrico/metabolismo , Ratas Wistar , Factor de Necrosis Tumoral alfa/metabolismo
5.
J Enzyme Inhib Med Chem ; 21(5): 501-7, 2006 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-17194018

RESUMEN

Bis(1,10-phenanthroline/2,2'-bipyridine) ruthenium(II)complexes containing TCP, TTZ OPBI, and BTSC ligands (where, TCP = 1-thiocarbamoyl-3,5-diphenyl-2-pyrazoline, TTZ = 2-(3,5-diphenyl-4,5-dihydropyrazol-1-yl)-4-phenylthiazole, OPBI = 2-hydroxyphenyl benzimidazole and BTSC = benzoin thiosemicarbazone) have been prepared and characterized. The spectral data suggested that the ligands were coordinated with the metal through nitrogen, sulfur and oxygen atoms. The target complexes were tested in vivo for anticancer activity against transplantable murine tumor cell line, Ehrlich's Ascitic Carcinoma (EAC). All these complexes increased the life span of the EAC-bearing mice, decreased their tumor volume and viable ascitic cell count as well as improved Hb, RBC and WBC counts. These results suggest that the Ru(II) complexes exhibit significant antitumor activity in EAC-bearing mice. It was also observed that the ruthenium complexes protected red blood cells from 2,2'-azo-bis(2-methylpropionamidine) dihydrochloride (AAPH)- induced hemolysis. The inhibitory effect was dose-dependent at a concentration of 20-120 microg/ml.


Asunto(s)
Antineoplásicos/síntesis química , Antineoplásicos/uso terapéutico , Compuestos de Rutenio/síntesis química , Compuestos de Rutenio/uso terapéutico , Animales , Antineoplásicos/química , Carcinoma de Ehrlich/tratamiento farmacológico , Carcinoma de Ehrlich/patología , Línea Celular Tumoral , Masculino , Ratones , Estructura Molecular , Compuestos de Rutenio/química , Relación Estructura-Actividad
6.
Bioorg Med Chem ; 13(20): 5766-73, 2005 Oct 15.
Artículo en Inglés | MEDLINE | ID: mdl-15982893

RESUMEN

A series of mononuclear Ru(II) complexes of the type [Ru(M)2(U)]2+, where M = 2,2'-bipyridine/1,10-phenanthroline and U = tpl (Ru1), 4-Cl-tpl (Ru2), 4-CH3-tpl (Ru3), 4-CH3O-tpl (Ru4), and 4-NO2-tpl (Ru5), -pai (Ru6), where tpl = thiopicolinanilide and pai = 2-phenyl-azo-imidazole, have been prepared and characterized by IR, UV-Vis, 1H NMR, 13C-NMR, FAB-Mass spectrophotometer, and elemental analysis. The complexes display metal-ligand charge transfer (MLCT) transitions in the visible region. The title complexes were subjected to in vivo anticancer activity tests against a transplantable murine tumor cell line, Ehrlich's ascitic carcinoma (EAC) and in vitro antibacterial activity against Gram positive and Gram negative microorganisms. Ru1-Ru6 were found to increase the life span of the tumor hosts by 19-52%, and decreased tumor volume and viable ascitic cell count. The results of the present study clearly demonstrated the tumor inhibitory activity of the ruthenium chelates against transplantable murine tumor cell line. The treatment with ruthenium complexes could be secondary to tumor regression or due to the action of the compounds itself. The significant antibacterial activity was observed for Ru1-Ru4 against microorganisms like Vibrio cholera 865, Staphylococcus aureus 6571, and Shigella flexneri as compared to that of standard drug chloramphenical. Ru5 showed moderate activity against S. aureus 8530. However, all the complexes fail to show significant antibacterial activity against V. cholera 14033 and Shigella sonnai.


Asunto(s)
Compuestos de Rutenio/síntesis química , Compuestos de Rutenio/farmacología , Animales , Antibacterianos/síntesis química , Antibacterianos/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Ensayos de Selección de Medicamentos Antitumorales , Ratones , Pruebas de Sensibilidad Microbiana , Análisis Espectral
7.
J Enzyme Inhib Med Chem ; 19(2): 185-92, 2004 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-15449735

RESUMEN

These ligands (L) show a bidentate behavior, forming octahedral ruthenium complexes. The title complexes were subjected to in-vivo anticancer activity tests against a transplantable murine tumor cell line, Ehrlich's Ascitic Carcinoma (EAC) and in-vitro antibacterial activity against several Gram positive and Gram negative bacterial strains. [Ru(bpy)2(ihqs)]Cl2 and [Ru(bpy)2 (hc)]Cl2 (where bpy = 2,2'-bipyridine, ihqs = 7-iodo-8hydroxy quinoline-5-sulphonic acid and hc = 3-hydroxy coumarin) showed promising antitumor activity. Treatment with these complexes prolonged the life span of EAC bearing mice as well as decreased their tumor volume and viable ascitic cell count. All the tested complexes exhibited mild to moderate antibacterial activity.


Asunto(s)
Antibacterianos/síntesis química , Antibacterianos/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Compuestos de Rutenio/síntesis química , Compuestos de Rutenio/farmacología , Animales , Carcinoma de Ehrlich , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Bacterias Gramnegativas , Bacterias Grampositivas/efectos de los fármacos , Ratones
8.
Chem Pharm Bull (Tokyo) ; 52(2): 178-85, 2004 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-14758001

RESUMEN

In search of potential anticancer drug candidates in ruthenium complexes, a series of mononuclear ruthenium complexes of the type [Ru(phen)(2)(nmit)]Cl(2) (Ru1), [Ru(bpy)(2)(nmit)]Cl(2) (Ru2), [Ru(phen)(2)(icpl)]Cl(2) (Ru3), Ru(bpy)(2)(icpl)]Cl(2) (Ru4) (phen=1,10-phenanthroline; bpy=2,2'-bipyridine; nmit=N-methyl-isatin-3-thiosemicarbazone, icpl=isatin-3-(4-Cl-phenyl)thiosemicarbazone) and [Ru(phen)(2)(aze)]Cl(2) (Ru5), [Ru(bpy)(2)(aze)]Cl(2) (Ru6) (aze=acetazolamide) and [Ru(phen)(2)(R-tsc)](ClO(4))(2) (R=methyl (Ru7), ethyl (Ru8), cyclohexyl (Ru9), 4-Cl-phenyl (10), 4-Br-phenyl (Ru11), and 4-EtO-phenyl (Ru12), tsc=thiosemicarbazone) were prepared and characterized by elemental analysis, FTIR, (1)H-NMR and FAB-MS. Effect of these complexes on the growth of a transplantable murine tumor cell line (Ehrlich Ascites Carcinoma) and their antibacterial activity were studied. In cancer study the effect of hematological profile of the tumor hosts have also been studied. In the cancer study, the complexes Ru1-Ru4, Ru10 and Ru11 have remarkably decreased the tumor volume and viable ascitic cell count as indicated by trypan blue dye exclusion test (p<0.05). Treatment with the ruthenium complexes prolonged the lifespan of Ehrlich Ascites Carcinoma (EAC) bearing mice. Tumor inhibition by the ruthenium chelates was followed by improvements in hemoglobin, RBC and WBC values. All the complexes showed antibacterial activity, except Ru5 and Ru6. Thus, the results suggest that these ruthenium complexes have significant antitumor property and antibacterial activity. The results also reflect that the drug does not adversely affect the hematological profiles as compared to that of cisplatin on the host.


Asunto(s)
Antibacterianos , Antineoplásicos , Compuestos Organometálicos , Rutenio , Animales , Antibacterianos/síntesis química , Antibacterianos/química , Antibacterianos/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/química , Antineoplásicos/uso terapéutico , Carcinoma de Ehrlich/tratamiento farmacológico , Supervivencia Celular/efectos de los fármacos , Ratones , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Compuestos Organometálicos/síntesis química , Compuestos Organometálicos/química , Compuestos Organometálicos/uso terapéutico , Rutenio/química , Rutenio/farmacología , Rutenio/uso terapéutico , Relación Estructura-Actividad , Células Tumorales Cultivadas
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