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1.
Biomater Adv ; 160: 213832, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38547763

RESUMEN

Triple negative breast cancer (TNBC) is an aggressive form of tumor, more prevalent in younger women resulting in poor survival rate (2nd in cancer deaths) because of its asymptomatic existence. The most popular and convenient approach for the treatment of TNBC is chemotherapy which is associated with several limitations. Considering the importance of nanotechnology in health care system, in the present manuscript, we have designed and developed a simple, efficient, cost effective, and ecofriendly method for the synthesis of copper nitroprusside analogue nanoparticles (Cu[Fe(CN)5NO] which is abbreviated as CuNPANP that may be the potential anti-cancer nanomedicine for the treatment of TNBC. Copper (present in CuNPANP) is used because of its affordability, nutritional value and various biomedical applications. The CuNPANP are thoroughly characterized using several analytical techniques. The in vitro cell viability (in normal cells) and the ex vivo hemolysis assay reveal the biocompatible nature of CuNPANP. The anti-cancer activity of the CuNPANP is established in TNBC cells (MDA-MB-231 and 4T1) through several in vitro assays along with plausible mechanisms. The intraperitoneal administration of CuNPANP in orthotopic breast tumor model by transplanting 4T1 cells into the mammary fat pad of BALB/c mouse significantly inhibits the growth of breast carcinoma as well as increases the survival time of tumor-bearing mice. These results altogether potentiate the anti-cancer efficacy of CuNPANP as a smart therapeutic nanomedicine for treating TNBC in near future after bio-safety evaluation in large animals.


Asunto(s)
Cobre , Especies Reactivas de Oxígeno , Neoplasias de la Mama Triple Negativas , Animales , Neoplasias de la Mama Triple Negativas/tratamiento farmacológico , Neoplasias de la Mama Triple Negativas/patología , Femenino , Ratones , Cobre/química , Cobre/farmacología , Cobre/administración & dosificación , Humanos , Línea Celular Tumoral , Especies Reactivas de Oxígeno/metabolismo , Antineoplásicos/farmacología , Antineoplásicos/uso terapéutico , Antineoplásicos/química , Antineoplásicos/administración & dosificación , Ratones Endogámicos BALB C , Nanopartículas del Metal/uso terapéutico , Nanopartículas del Metal/química , Supervivencia Celular/efectos de los fármacos , Modelos Animales de Enfermedad
2.
Nanoscale ; 12(14): 7604-7621, 2020 Apr 14.
Artículo en Inglés | MEDLINE | ID: mdl-32232245

RESUMEN

In recent days, vanadium complexes and nanoparticles have received sustainable attention owing to their vast applications in different fields. In the present study, we report a facile approach for the synthesis of irregular dumbbell shaped vanadium pentoxide nanoparticles (V2O5 NPs: 30-60 nm) via the polyol-induced microwave irradiation process along with calcination. The as-synthesized nanoparticles were characterized using various physico-chemical techniques (e.g. XRD, TEM, FT-IR, DLS and XPS). The cell viability assay showed that V2O5 NPs could efficiently inhibit the proliferation of different cancer cells (B16F10, A549, and PANC1), depicting their anti-proliferative activity. However, V2O5 NPs did not exert significant cytotoxicity to the normal cells (CHO, HEK-293 and NRK-49F), suggesting their biocompatible nature. Interestingly, these nanoparticles inhibited the proliferation and migration of the endothelial cells (HUVECs and EA.hy926) and disrupted the blood vasculature in a chick embryo model, indicating their anti-angiogenic properties. The mechanistic study revealed that the effective internalization of V2O5 NPs generated intracellular reactive oxygen species (ROS) which in turn up-regulated p53 protein and down-regulated survivin protein in cancer cells, leading to the apoptosis process. Furthermore, the administration of V2O5 NPs to melanoma bearing C57BL6/J mice significantly increased their survivability as compared to the control untreated tumor bearing mice, exhibiting the therapeutic potential of the nanoparticles against melanoma. Additionally, the in vivo toxicity study demonstrated no toxic effect in mice upon sub-chronic exposure to V2O5 NPs. Altogether, we strongly believe that V2O5 NPs could intrinsically provide a new direction for alternative therapeutic treatment strategies for melanoma and other cancers by employing their anti-angiogenic properties in the future.


Asunto(s)
Nanopartículas del Metal/química , Neovascularización Fisiológica , Compuestos de Vanadio/química , Animales , Apoptosis/efectos de los fármacos , Materiales Biocompatibles/química , Materiales Biocompatibles/farmacología , Materiales Biocompatibles/uso terapéutico , Puntos de Control del Ciclo Celular/efectos de los fármacos , Línea Celular , Movimiento Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Embrión de Pollo , Eritrocitos/citología , Eritrocitos/efectos de los fármacos , Eritrocitos/metabolismo , Femenino , Hemólisis/efectos de los fármacos , Humanos , Melanoma Experimental/tratamiento farmacológico , Melanoma Experimental/patología , Nanopartículas del Metal/uso terapéutico , Nanopartículas del Metal/toxicidad , Ratones , Ratones Endogámicos C57BL , Neovascularización Fisiológica/efectos de los fármacos , Especies Reactivas de Oxígeno/metabolismo , Trasplante Homólogo
3.
Mater Sci Eng C Mater Biol Appl ; 105: 110079, 2019 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-31546406

RESUMEN

In the present paper, we synthesized and characterized four N-donor polypyridyl copper(II) complexes (C1-C4); [Cu(mono-CN-PIP)2]2+ (C1), [Cu(tri-OMe-PIP)2]2+ (C2), [Cu(di-CF3-PIP)2]2+ (C3) and [Cu(DPPZ)2]2+ (C4). The (Calf-Thymus) CT-DNA binding studies depicted that the complexes could interact with DNA via intercalative mode. All the complexes, particularly C3 and C4 attenuated the proliferation as well as migration of various cancer cells, indicating their anti-cancer and anti-metastatic activity. Additionally, chick embryo angiogenesis (CEA) assay exhibited the inhibition of vascular sprouting in presence of C3 and C4, suggesting their potential in inhibiting the blood vessel growth. Mechanistic studies revealed that the complexes induced the excessive production of cellular reactive oxygen species (ROS) leading to apoptosis through up regulation of p53 and downregulation of Bcl-xL, which might be the plausible mechanisms underlying their anti-cancer properties. To understand the feasibility of practical application of anti-cancer copper complexes C3 and C4, in vivo sub-chronic toxicity study (4 weeks) was performed in C57BL6 mice and the results exhibited almost non-toxic effects induced by these complexes in terms of haematology and serum biochemical analyses, suggesting their biocompatible nature. The current study provides the basis for future advancement of other novel biocompatible metal complexes that could be employed for the therapy of different cancers.


Asunto(s)
Complejos de Coordinación , Cobre , Sustancias Intercalantes , Melanoma Experimental , Animales , Antineoplásicos/síntesis química , Antineoplásicos/química , Antineoplásicos/farmacocinética , Línea Celular Tumoral , Embrión de Pollo , Complejos de Coordinación/síntesis química , Complejos de Coordinación/química , Complejos de Coordinación/farmacología , Cobre/química , Cobre/farmacología , Humanos , Sustancias Intercalantes/síntesis química , Sustancias Intercalantes/química , Sustancias Intercalantes/farmacología , Melanoma Experimental/tratamiento farmacológico , Melanoma Experimental/metabolismo , Melanoma Experimental/patología , Ratones , Proteína p53 Supresora de Tumor/metabolismo , Proteína bcl-X/metabolismo
4.
ACS Biomater Sci Eng ; 4(9): 3434-3449, 2018 Sep 10.
Artículo en Inglés | MEDLINE | ID: mdl-33435077

RESUMEN

Therapeutic agents harboring both wound healing and antibacterial activities have much demand in biomedical applications. Development of such candidates with clinically approved materials adds more advantages toward these applications. Recently, silver metal complex nanomaterials have been playing a major role in medical uses especially for antibacterial activity and wound healing. In this report, we designed and synthesized silver nitroprusside complex nanoparticles (abbreviated as AgNNPs) using sodium nitroprusside and silver nitrate (both are FDA approved precursors). The nanoparticles (AgNNPs) were thoroughly characterized by various physicochemical techniques such as XRD, FTIR, TGA, DLS, EDAX, Raman, ICP-OES, HRTEM, and FESEM. The cell viability assay in normal cells (EA.hy 926 cells, NIH 3T3) using MTT reagents and CEA assay (CEA: Chick embryo angiogenesis assay) in fertilized eggs demonstrate the biocompatibility of AgNNPs. These nanoparticles show effective antibacterial activity against both Gram positive and Gram negative bacteria through membrane and DNA damage. Additionally, AgNNPs accelerate the wound healing in C57BL6 mice by altering the macrophages from M1 to M2. Considering the results together, the current study may offer the development of new silver nanocomplex nanomaterials that shows synergistic effect on antibacterial activity and wound healing (2-in-1-system). To the best of our knowledge, this is the first report for the synthesis, characterization, and biomedical applications of silver nitroprusside nanoparticles.

5.
Anc Sci Life ; 36(4): 207-214, 2017.
Artículo en Inglés | MEDLINE | ID: mdl-29269973

RESUMEN

BACKGROUND: Herbo-mineral formulations of Ayurveda contain specified metals or minerals as composition, which have their beneficial effects on biological systems. These metals or minerals are transformed into non-toxic forms through meticulous procedures explained in Ayurveda. Though literature is available on quality aspects of such herbo-mineral formulations; contemporary science is raising concerns at regular intervals on such formulations. Thus, it becomes mandate to develop quality profiles of all formulations that contain metals or minerals in their composition. Considering this, it is planned to evaluate analytical profile of Vasantakusumakara Rasa. OBJECTIVE: To prepare Vasantakusumakara Rasa as per Standard operating Procedures (SoP) mentioned in classical text and to characterize it chemically using modern analytical techniques. MATERIALS AND METHODS: The drug (Vasantakusumakara Rasa) in three batches was prepared in GMP certified pharmacy. Physico-chemical analysis, Assay of elements and HPTLC were carried out as per API. XRD was conducted using Rigaku Ultima-IV X-ray diffractometer. RESULTS: The analysis shown the presence of Mercury, Tin, Gold, Silver, Iron, Zinc and Calcium etc., and HPTLC revealed presence of organic constituents from plant material. The XRD indicated the presence of cinnabar (mercury sulphide from Rasa Sindhura), cassiterite (tin oxide from Vanga Bhasma), massicot (lead oxide from Naga bhasma) and Magnetite (di-iron oxide from Loha bhasma). CONCLUSION: The physico chemical analysis reveals that VKR prepared by following classical guidelines is very effective in converting the macro elements into therapeutically effective medicines in micro form. Well prepared herbo-mineral drugs offer many advantages over plant medicines due to their longer shelf life, lesser doses, easy storing facilities, better palatability etc. The inferences and the standards laid down in this study certainly can be utilized as baseline data of standardization and QC.

6.
Nanomedicine (Lond) ; 11(19): 2529-46, 2016 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-27622735

RESUMEN

AIM: To explore the potential of glucocorticoid receptor-targeted nano-gold formulation as antitumor drug sensitizing agent. MATERIALS & METHODS: Simultaneous conjugation of gold nanoparticle with thiol-modified dexamethasone, a synthetic glucocorticoid and anticancer drug withaferin A afforded stable gold nanoparticle-modifed dexamethasone-withaferin A nanoconjugate. RESULTS: This metallic nanoparticle formulation showed glucocorticoid receptor-dependent cancer cell selective cytotoxicity, inhibited growth of aggressive mouse melanoma tumor, reduced mice mortality, while reversing epithelial-to-mesenchymal transition in tumor cells. Same treatment also leads to near-complete downregulation of ABCG2 drug transporter in tumor-associated cells thus attributing it to its drug sensitizing ability. CONCLUSION: The presently synthesized nanoconjugate holds a great promise to sensitize cancer cells to chemotherapeutics and induce epithelial-to-mesenchymal transition reversal in tumor cells preventing metastasis.


Asunto(s)
Antineoplásicos/farmacología , Dexametasona/química , Transición Epitelial-Mesenquimal/efectos de los fármacos , Nanoconjugados/química , Receptores de Glucocorticoides/metabolismo , Witanólidos/química , Animales , Antineoplásicos/química , Antineoplásicos/uso terapéutico , Apoptosis/efectos de los fármacos , Células CHO , Supervivencia Celular/efectos de los fármacos , Cricetulus , Dexametasona/farmacología , Dexametasona/uso terapéutico , Portadores de Fármacos , Femenino , Oro/química , Humanos , Ratones , Ratones Endogámicos C57BL , Células 3T3 NIH , Tamaño de la Partícula , Propiedades de Superficie , Distribución Tisular , Witanólidos/farmacología , Witanólidos/uso terapéutico
7.
J Biomed Nanotechnol ; 12(1): 165-81, 2016 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-27301182

RESUMEN

In the present article, we report the in vitro and in vivo delivery of doxorubicin using biosynthesized gold nanoparticles (b-Au-PP). Gold nanoparticles were synthesized by a simple, fast, efficient, environmentally friendly and economical green chemistry approach using an extract of Peltophorum pterocarpum (PP) leaves. Because the biosynthesized b-Au-PP was highly stable in various physiological buffers for several weeks and biocompatible in both in vitro and in vivo systems, we designed and developed a biosynthesized gold nanoparticle (b-Au-PP)-based drug-delivery system (DDS) using doxorubicin (Dox) (b-Au-PP-Dox). Both b-Au-PP and b-Au-PP-Dox were thoroughly characterized using several analytical tools. Administration of doxorubicin-loaded DDS (b-Au-PP-Dox) resulted in a significant inhibition of the proliferation of cancer cells (A549, B16F10) in vitro and of tumor growth in an in vivo model compared to doxorubicin alone. Furthermore, we found that the cellular uptake and release of Dox in the nanoconjugated form (b-Au-PP-Dox) were faster than the uptake and release of unconjugated Dox. The in vivo toxicity study did not show any significant changes in the hematology, serum clinical biochemistry or histopathology in the C57BL6/J female mice after consecutive intraperitoneal (IP) injections over a period of seven days. To the best of our knowledge, our study is the first to report the application of a biosynthesized gold nanoparticle-based DDS for cancer therapy in an animal model, in addition to a detailed in vivo toxicity study. Together, the results demonstrate that a biosynthesized gold nanoparticle-based drug-delivery system (b-Au-PP-Dox) could be used in the near future as an alternative cost-effective treatment strategy for cancer therapy.


Asunto(s)
Doxorrubicina/administración & dosificación , Doxorrubicina/farmacocinética , Fabaceae/química , Nanocápsulas/química , Neoplasias Experimentales/tratamiento farmacológico , Neoplasias Experimentales/metabolismo , Animales , Antibióticos Antineoplásicos/administración & dosificación , Supervivencia Celular/efectos de los fármacos , Femenino , Oro/química , Tecnología Química Verde/métodos , Tasa de Depuración Metabólica , Nanopartículas del Metal/química , Nanopartículas del Metal/ultraestructura , Ratones , Ratones Endogámicos C57BL , Nanocápsulas/ultraestructura , Neoplasias Experimentales/patología , Especificidad de Órganos , Extractos Vegetales/química , Distribución Tisular , Resultado del Tratamiento
8.
J Nanosci Nanotechnol ; 15(2): 1714-24, 2015 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-26353720

RESUMEN

Gold nanoparticles supported on SBA-15 are prepared by homogenous deposition-precipitation method (HDP) using urea as the precipitating agent. The structural features of the synthesized catalysts were characterized by various techniques such as X-ray diffraction (XRD), transmission electron microscopy (TEM), nitrogen adsorption-desorption (BET), pore size distribution (PSD), CO chemisorption and X-ray photoelectron spectroscopy (XPS). The catalytic activity and stability of the Au/SBA-15 catalysts are investigated during the vapor phase aerobic oxidation of benzyl alcohol. The BJH pore size distribution results of SBA-15 support and Au/SBA-15 catalysts reveals that the formation of mesoporous structure in all the samples. TEM results suggest that Au nanoparticles are highly dispersed over SBA-15 and long range order of hexagonal mesopores of SBA-15 is well retained even after the deposition of Au metallic nanoparticles. XPS study reveals the formation of Au (0) after chemical reduction by NaBH4. The particle size measured from CO-chemisorption and TEM analysis are well correlated with the TOF values of the reaction. Au/SBA-1 5 catalysts are found to show higher activity compare to Au/TiO2 and Au/MgO catalysts during the vapor phase oxidation of benzyl alcohol. The catalytic functionality are well substantiated with particle size measured from TEM. The crystallite size of Au in both fresh and spent catalysts were measured from X-ray diffraction.


Asunto(s)
Benzaldehídos/química , Alcohol Bencilo/química , Oro/química , Nanopartículas del Metal/química , Dióxido de Silicio/química , Adsorción , Aerobiosis , Catálisis , Coloides/química , Gases/química , Ensayo de Materiales , Tamaño de la Partícula , Transición de Fase , Porosidad , Propiedades de Superficie
9.
Mater Sci Eng C Mater Biol Appl ; 53: 298-309, 2015 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-26042718

RESUMEN

In the present article, we demonstrate the delivery of anti-cancer drug to the cancer cells using biosynthesized gold and silver nanoparticles (b-AuNP & b-AgNP). The nanoparticles synthesized by using Butea monosperma (BM) leaf extract are thoroughly characterized by various analytical techniques. Both b-AuNP and b-AgNP are stable in biological buffers and biocompatible towards normal endothelial cells (HUVEC, ECV-304) as well as cancer cell lines (B16F10, MCF-7, HNGC2 & A549). Administration of nanoparticle based drug delivery systems (DDSs) using doxorubicin (DOX) [b-Au-500-DOX and b-Ag-750-DOX] shows significant inhibition of cancer cell proliferation (B16F10, MCF-7) compared to pristine drug. Therefore, we strongly believe that biosynthesized nanoparticles will be useful for the development of cancer therapy using nanomedicine approach in near future.


Asunto(s)
Antineoplásicos/química , Sistemas de Liberación de Medicamentos , Oro/química , Nanopartículas del Metal/química , Plata/química , Animales , Antineoplásicos/farmacocinética , Antineoplásicos/farmacología , Butea , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Doxorrubicina/química , Doxorrubicina/farmacocinética , Doxorrubicina/farmacología , Oro/farmacocinética , Tecnología Química Verde , Humanos , Ratones , Extractos Vegetales/metabolismo , Plata/farmacocinética
10.
J Med Chem ; 58(13): 5226-41, 2015 Jul 09.
Artículo en Inglés | MEDLINE | ID: mdl-26068145

RESUMEN

A series of four new mononuclear copper(II) polypyridyl complexes (1-4) have been designed, developed, and thoroughly characterized by several physicochemical techniques. The CT-DNA binding properties of 1-4 have been investigated by absorption, emission spectroscopy, and viscosity measurements. All the complexes especially 1 and 4 exhibit cytotoxicity toward several cancer cell lines, suggesting their anticancer properties as observed by several in vitro assays. Additionally, the complexes show inhibition of endothelial cell (HUVECs) proliferation, indicating their antiangiogenic nature. In vivo chick embryo angiogenesis assay again confirms the antiangiogenic properties of 1 and 4. The formation of excessive intracellular ROS (H2O2 and O2(•-)) and upregulation of BAX induced by copper(II) complexes may be the plausible mechanisms behind their anticancer activities. The present study may offer a basis for the development of new transition metal complexes through suitable choice of ligands for cancer therapeutics by controlling tumor angiogenesis.


Asunto(s)
Inhibidores de la Angiogénesis/farmacología , Antineoplásicos/farmacología , Complejos de Coordinación/farmacología , Cobre/química , Neoplasias/tratamiento farmacológico , Neovascularización Fisiológica/efectos de los fármacos , Piridinas/química , Inhibidores de la Angiogénesis/síntesis química , Animales , Antineoplásicos/síntesis química , Apoptosis/efectos de los fármacos , Western Blotting , Ciclo Celular/efectos de los fármacos , Movimiento Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Células Cultivadas , Embrión de Pollo , Complejos de Coordinación/síntesis química , ADN/metabolismo , División del ADN/efectos de los fármacos , Citometría de Flujo , Células Endoteliales de la Vena Umbilical Humana/efectos de los fármacos , Humanos , Modelos Moleculares , Estructura Molecular , Neoplasias/patología , Unión Proteica , Especies Reactivas de Oxígeno/metabolismo , Relación Estructura-Actividad
11.
Chem Commun (Camb) ; 51(34): 7325-8, 2015 Apr 30.
Artículo en Inglés | MEDLINE | ID: mdl-25820667

RESUMEN

We have designed and developed stable and biocompatible copper analogues of a Prussian blue (PB) nanoparticle based drug delivery system containing doxorubicin that show selective quenching of fluorescence of doxorubicin compared to PB analogues with other metals and inhibition of cancer cell proliferation, suggesting future potential multifunctional applications in biomedical sciences.


Asunto(s)
Cobre/química , Portadores de Fármacos/química , Ferrocianuros/química , Línea Celular , Portadores de Fármacos/síntesis química , Tecnología Química Verde , Humanos , Nanopartículas/química
12.
ACS Biomater Sci Eng ; 1(8): 646-655, 2015 Aug 10.
Artículo en Inglés | MEDLINE | ID: mdl-33435088

RESUMEN

Herein we report on the unexpected cancer cell selective cytotoxicities of the liposomal formulations of aspartic and glutamic acid backbone-based four novel lipids with endosomal pH-sensitive head-groups and aliphatic n-hexadecyl & n-octadecyl hydrophobic tails. Surprisingly, although the formulations killed cancer cells efficiently, they were significantly less cytotoxic in non-cancerous healthy cells. Importantly, intratumoral administration of the liposomal formulations efficiently inhibited growth of melanoma in a syngeneic C57BL/6J mouse tumor model. Western Blotting experiments with the lysates of liposomes treated cancer cells revealed that liposomes of lipids 1-4 induce apoptosis selectively in cancer cells presumably by releasing cytochrome c from depolarized mitochondria and subsequent activation of caspases 3 & 9, upregulation of Bax and down regulation of Bcl-2. In summary, the present report describes for the first time tumor growth inhibition properties of the liposomal formulations of endosomal pH-sensitive histidinylated cationic lipids under both in vitro and systemic settings.

13.
Org Biomol Chem ; 12(34): 6725-9, 2014 Sep 14.
Artículo en Inglés | MEDLINE | ID: mdl-25047719

RESUMEN

Propargylamines are synthesized via metal-free activation of the C-halogen bond of dihalomethanes and the C-H bond of terminal alkynes in a three-component coupling without catalyst or additional base and under mild reaction conditions. The dihalomethanes are used both as solvents as well as precursors for the methylene fragment (C1) in the final product. The scope of the reaction and the influence of various reaction variables has been investigated. A plausible reaction mechanism is proposed and the involvement of various intermediates that can be generated in situ in the process is discussed. The metal-free conditions also make this protocol environmentally benign and atom economical.


Asunto(s)
Alquinos/química , Cloruro de Metileno/química , Pargilina/análogos & derivados , Propilaminas/síntesis química , Butilaminas/química , Tecnología Química Verde , Estructura Molecular , Pargilina/síntesis química , Piperidinas/química , Pirrolidinas/química
14.
Nanoscale ; 6(12): 6745-54, 2014 Jun 21.
Artículo en Inglés | MEDLINE | ID: mdl-24824564

RESUMEN

Nanoparticles, such as gold nanoparticles (GNP), upon convenient modifications perform multi tasks catering to many biomedical applications. However, GNP or any other type of nanoparticles is yet to achieve the feat of intracellular regulation of endogenous genes of choice such as through manipulation of a gene-promoter in a chromosome. As for gene modulation and delivery, GNP (or other nanoparticles) showed only limited gene therapy potential, which relied on the delivery of 'exogenous' genes invoking gene knockdown or replacement. Practically, there are no instances for the nanoparticle-mediated promoter regulation of 'endogenous' genes, more so, as a cancer selective phenomenon. In this regard, we report the development of a simple, easily modifiable GNP-formulation, which promoted/up-regulated the expression of a specific category of 'endogenous' genes, the glucocorticoid responsive genes. This genetic up-regulation was induced in only cancer cells by modified GNP-mediated transcriptional activation of its cytoplasmic receptor, glucocorticoid receptor (GR). Normal cells and their GR remained primarily unperturbed by this GNP-formulation. The most potent gene up-regulating GNP-formulation down-regulated a cancer-specific proliferative signal, phospho-Akt in cancer cells, which accompanied retardation of tumor growth in the murine melanoma model. We show that GR-targeted GNPs may find potential use in the targeting and modulation of genetic information in cancer towards developing novel anticancer therapeutics.


Asunto(s)
Dexametasona/administración & dosificación , Nanopartículas del Metal/química , Neoplasias Experimentales/tratamiento farmacológico , Neoplasias Experimentales/genética , Regiones Promotoras Genéticas/genética , Receptores de Glucocorticoides/genética , Animales , Antineoplásicos Hormonales/administración & dosificación , Antineoplásicos Hormonales/química , Línea Celular Tumoral , Dexametasona/química , Difusión , Marcación de Gen/métodos , Oro/química , Humanos , Nanopartículas del Metal/administración & dosificación , Nanopartículas del Metal/ultraestructura , Ratones , Nanocápsulas/administración & dosificación , Nanocápsulas/química , Nanocápsulas/ultraestructura , Neoplasias Experimentales/patología , Resultado del Tratamiento
15.
Chemistry ; 20(20): 6154-61, 2014 May 12.
Artículo en Inglés | MEDLINE | ID: mdl-24700354

RESUMEN

New graphene oxide (GO)-tethered-Co(II) phthalocyanine complex [CoPc-GO] was synthesized by a stepwise procedure and demonstrated to be an efficient, cost-effective and recyclable photocatalyst for the reduction of carbon dioxide to produce methanol as the main product. The developed GO-immobilized CoPc was characterized by X-ray diffraction (XRD), FTIR, XPS, Raman, diffusion reflection UV/Vis spectroscopy, inductively coupled plasma atomic emission spectroscopy (ICP-AES), thermogravimetric analysis (TGA), Brunauer-Emmett-Teller (BET), scanning electron microscopy (SEM), and transmission electron microscopy (TEM). FTIR, XPS, Raman, UV/Vis and ICP-AES along with elemental analysis data showed that Co(II) -Pc complex was successfully grafted on GO. The prepared catalyst was used for the photocatalytic reduction of carbon dioxide by using water as a solvent and triethylamine as the sacrificial donor. Methanol was obtained as the major reaction product along with the formation of minor amount of CO (0.82 %). It was found that GO-grafted CoPc exhibited higher photocatalytic activity than homogeneous CoPc, as well as GO, and showed good recoverability without significant leaching during the reaction. Quantitative determination of methanol was done by GC flame-ionization detector (FID), and verification of product was done by NMR spectroscopy. The yield of methanol after 48 h of reaction by using GO-CoPc catalyst in the presence of sacrificial donor triethylamine was found to be 3781.8881 µmol g(-1) cat., and the conversion rate was found to be 78.7893 µmol g(-1) cat. h(-1). After the photoreduction experiment, the catalyst was easily recovered by filtration and reused for the subsequent recycling experiment without significant change in the catalytic efficiency.

16.
Theranostics ; 4(3): 316-35, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-24505239

RESUMEN

In this report, we have designed a simple and efficient green chemistry approach for the synthesis of colloidal silver nanoparticles (b-AgNPs) that is formed by the reduction of silver nitrate (AgNO3) solution using Olax scandens leaf extract. The colloidal b-AgNPs, characterized by various physico-chemical techniques exhibit multifunctional biological activities (4-in-1 system). Firstly, bio-synthesized silver nanoparticles (b-AgNPs) shows enhanced antibacterial activity compared to chemically synthesize silver nanoparticles (c-AgNPs). Secondly, b-AgNPs show anti-cancer activities to different cancer cells (A549: human lung cancer cell lines, B16: mouse melanoma cell line & MCF7: human breast cancer cells) (anti-cancer). Thirdly, these nanoparticles are biocompatible to rat cardiomyoblast normal cell line (H9C2), human umbilical vein endothelial cells (HUVEC) and Chinese hamster ovary cells (CHO) which indicates the future application of b-AgNPs as drug delivery vehicle. Finally, the bio-synthesized AgNPs show bright red fluorescence inside the cells that could be utilized to detect the localization of drug molecules inside the cancer cells (a diagnostic approach). All results together demonstrate the multifunctional biological activities of bio-synthesized AgNPs (4-in-1 system) that could be applied as (i) anti-bacterial & (ii) anti-cancer agent, (iii) drug delivery vehicle, and (iv) imaging facilitator. To the best of our knowledge, there is not a single report of biosynthesized AgNPs that demonstrates the versatile applications (4-in-1 system) towards various biomedical applications. Additionally, a plausible mechanistic approach has been explored for the synthesis of b-AgNPs and its anti-bacterial as well as anti-cancer activity. We strongly believe that bio-synthesized AgNPs will open a new direction towards various biomedical applications in near future.


Asunto(s)
Nanopartículas del Metal/química , Plata , Animales , Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Células CHO , Línea Celular Tumoral , Cricetinae , Cricetulus , Tecnología Química Verde , Células Endoteliales de la Vena Umbilical Humana/efectos de los fármacos , Humanos , Nanopartículas del Metal/uso terapéutico , Ratones , Miocitos Cardíacos/efectos de los fármacos , Ratas , Plata/química , Plata/farmacología
17.
Int J Nanomedicine ; 9: 575-88, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-24531257

RESUMEN

AIM: The aim of this study was to develop poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) for delivery of a protein - tissue inhibitor of matrix metalloproteinases 1 (TIMP-1) - across the blood-brain barrier (BBB) to inhibit deleterious matrix metalloproteinases (MMPs). MATERIALS AND METHODS: The NPs were formulated by multiple-emulsion solvent-evaporation, and for enhancing BBB penetration, they were coated with polysorbate 80 (Ps80). We compared Ps80-coated and uncoated NPs for their toxicity, binding, and BBB penetration on primary rat brain capillary endothelial cell cultures and the rat brain endothelial 4 cell line. These studies were followed by in vivo studies for brain delivery of these NPs. RESULTS: Results showed that neither Ps80-coated nor uncoated NPs caused significant opening of the BBB, and essentially they were nontoxic. NPs without Ps80 coating had more binding to endothelial cells compared to Ps80-coated NPs. Penetration studies showed that TIMP-1 NPs + Ps80 had 11.21%± 1.35% penetration, whereas TIMP-1 alone and TIMP-1 NPs without Ps80 coating did not cross the endothelial monolayer. In vivo studies indicated BBB penetration of intravenously injected TIMP-1 NPs + Ps80. CONCLUSION: The study demonstrated that Ps80 coating of NPs does not cause significant toxic effects to endothelial cells and that it can be used to enhance the delivery of protein across endothelial cell barriers, both in vitro and in vivo.


Asunto(s)
Barrera Hematoencefálica/metabolismo , Sistemas de Liberación de Medicamentos , Ácido Láctico/química , Nanopartículas/administración & dosificación , Nanopartículas/química , Ácido Poliglicólico/química , Inhibidor Tisular de Metaloproteinasa-1/administración & dosificación , Animales , Barrera Hematoencefálica/efectos de los fármacos , Línea Celular , Células Cultivadas , Química Farmacéutica , Preparaciones de Acción Retardada , Células Endoteliales/efectos de los fármacos , Células Endoteliales/metabolismo , Nanomedicina , Nanopartículas/toxicidad , Nanotecnología , Copolímero de Ácido Poliláctico-Ácido Poliglicólico , Polisorbatos/química , Ratas , Tensoactivos/química , Inhibidor Tisular de Metaloproteinasa-1/farmacocinética
18.
Chemistry ; 19(46): 15759-68, 2013 Nov 11.
Artículo en Inglés | MEDLINE | ID: mdl-24123356

RESUMEN

A selective N-arylation of cyclic amides and amines in DMF and water, respectively, catalysed by Cu(II) /Al2 O3 has been achieved. This protocol has been employed for the synthesis of a library of arenes bearing a cyclic amide and an amine moiety at two ends, including a few scaffolds of therapeutic importance. The mechanism has been established based on detailed electron paramagnetic resonance (EPR) spectroscopy, X-ray photoelectron spectroscopy (XPS), UV diffuse reflectance spectroscopy (DRS) and inductively coupled plasma-mass spectrometry (ICP-MS) studies of the catalyst at different stages of the reaction. The Cu(II) /Al2 O3 catalyst was recovered and recycled for subsequent reactions.


Asunto(s)
Amidas/química , Aminas/química , Cobre/química , Hidrocarburos Halogenados/química , Solventes/química , Catálisis , Cristalografía por Rayos X , Espectroscopía de Resonancia por Spin del Electrón , Estructura Molecular , Espectroscopía de Fotoelectrones
19.
Artículo en Inglés | MEDLINE | ID: mdl-23220527

RESUMEN

There are many methods to synthesise metal and metal oxide nanoparticles (NPs) using different reducing agents which are hazardous in nature. Although some researchers have used biobased materials for synthesis of these NPs, further research is needed in this area. To explore the scope of bio-extract for the synthesis of transition metal NPs, the present paper synthesises metal NPs replacing hazardous traditional reducing agents. This paper reports the synthesis of palladium and iron NPs, using aqueous extract of Terminalia chebula fruit. Reduction potential of aqueous extract of polyphenolic rich T. chebula was 0.63V vs. SCE by cyclic voltammetry study which makes it a good green reducing agent. This helps to reduce palladium and iron salts to palladium and iron NPs respectively. Powder X-ray Diffraction (XRD) and Transmission Electron Microscope (TEM) analyses revealed that amorphous iron NPs were within the size less than 80 nm and cubic palladium NPs were within the size less than 100 nm. The synthesised nanomaterials were remarkably stable for a long period and synthesis of stable metal NPs will need to be explored using biobased materials as reducing agents.


Asunto(s)
Tecnología Química Verde/métodos , Hierro/química , Nanopartículas del Metal/química , Paladio/química , Extractos Vegetales/química , Terminalia/química , Nanopartículas del Metal/ultraestructura , Agua/química
20.
Nanotechnology ; 23(45): 455103, 2012 Nov 16.
Artículo en Inglés | MEDLINE | ID: mdl-23064012

RESUMEN

The biological approach to synthesis of AuNPs is eco-friendly and an ideal method to develop environmentally sustainable nanoparticles alternative to existing methods. We have developed a simple, fast, clean, efficient, low-cost and eco-friendly single-step green chemistry approach for the synthesis of biocompatible gold nanoparticles (AuNPs) from chloroauric acid (HAuCl(4)) using a water extract of Eclipta Alba leaves at room temperature. The AuNPs using Eclipta extract have been formed in very short time, even in less than 10 min. The as-synthesized AuNPs were thoroughly characterized by several physico-chemical techniques. The in vitro stability of as-synthesized AuNPs was studied in different buffer solutions. A plausible mechanism for the synthesis of AuNPs by Eclipta extract has been discussed. The biocompatibility of AuNPs was observed by in vitro cell culture assays. Finally, we have designed and developed a AuNPs-based drug delivery system (DDS) (Au-DOX) containing doxorubicin (DOX), a FDA approved anticancer drug. Administration of this DDS to breast cancer cells (MCF-7 and MDA-MB-231) shows significant inhibition of breast cancer cell proliferation compared to pristine doxorubicin. Therefore we strongly believe that the use of Eclipta Alba offers large-scale production of biocompatible AuNPs that can be used as a delivery vehicle for the treatment of cancer diseases.


Asunto(s)
Portadores de Fármacos/química , Eclipta/química , Oro/química , Tecnología Química Verde/métodos , Nanopartículas del Metal/química , Extractos Vegetales/química , Antibióticos Antineoplásicos/administración & dosificación , Antibióticos Antineoplásicos/farmacología , Neoplasias de la Mama/tratamiento farmacológico , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Cloruros/química , Doxorrubicina/administración & dosificación , Doxorrubicina/farmacología , Portadores de Fármacos/síntesis química , Femenino , Compuestos de Oro/química , Tecnología Química Verde/economía , Humanos , Extractos Vegetales/aislamiento & purificación , Hojas de la Planta/química
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