Your browser doesn't support javascript.
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 1.680
Filtrar
1.
Chem Commun (Camb) ; 55(66): 9829-9832, 2019 Aug 13.
Artigo em Inglês | MEDLINE | ID: mdl-31363730

RESUMO

Polyethylene glycol grafted pyrrole-based conjugated polymers are synthesized through a one-pot multicomponent methodology, the self-assemblies of which enable nanoparticle size-selective encapsulation of drug molecules and their sustained release. Efficient loading of curcumin through drug-nanoparticle core interactions is probed using FRET, and the inherently fluorescent nature of polypyrrole could be used to detect these nanocarriers intracellularly.


Assuntos
Portadores de Fármacos , Nanopartículas/química , Polietilenoglicóis/química , Polímeros/química , Pirróis/química , Linhagem Celular Tumoral , Curcumina/administração & dosagem , Transferência Ressonante de Energia de Fluorescência , Humanos , Interações Hidrofóbicas e Hidrofílicas , Concentração Inibidora 50 , Microscopia Eletrônica de Transmissão , Espectrofotometria Ultravioleta
2.
Food Chem ; 299: 125097, 2019 Nov 30.
Artigo em Inglês | MEDLINE | ID: mdl-31284242

RESUMO

The low solubility, instability, and low bioavailability of food bioactive compounds such as polyphenols and flavonoids, restrict their applications in the fields of food science and nutrition. Ferritin protein has received more and more attention in encapsulation and delivery of the bioactive compounds due to its nanosized shell-like structure and its reversible self-assembly character. After encapsulation, bioactive compounds can be functionalized by the ferritin vehicle to achieve stabilization, solubilization, and targeted delivery. In addition, the outer interfaces and the porous structure of ferritin are also artfully harnessed for encapsulation. This review focuses on the newest advances in the fabrication, characterization, and application of ferritin-based nano-carriers for bioactive compounds by the reversible self-assembly, outer-interface decoration methods, and the channel-directed approach. The functional improvements of food bioactive compounds, including their solubility, stability, and cellular uptake, are emphasized. The limitations that affect ferritin encapsulation are also examined.


Assuntos
Ferritinas/química , Ferritinas/farmacocinética , Alimentos , Nanoestruturas/química , Antocianinas/administração & dosagem , Antocianinas/química , Antocianinas/farmacocinética , Disponibilidade Biológica , Catequina/análogos & derivados , Catequina/química , Quitosana/química , Curcumina/administração & dosagem , Curcumina/química , Curcumina/farmacocinética , Humanos , Polifenóis/administração & dosagem , Polifenóis/química , Polifenóis/farmacocinética , Proantocianidinas/administração & dosagem , Proantocianidinas/química , Proantocianidinas/farmacocinética , Solubilidade , beta Caroteno/administração & dosagem , beta Caroteno/química , beta Caroteno/farmacocinética
3.
Food Chem ; 298: 125091, 2019 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-31272049

RESUMO

The complexation of Lepidium sativum protein hydrolysate (LSPH) with a lipophilic molecule, curcumin (CUR), and its effect on curcumin in vitro bioaccessibility/stability, functional and antioxidant activity were investigated. Fluorescence spectroscopy of the LSPH/CUR complex confirmed the presence of hydrophobic interactions that led to the complex formation. The LSPH (10-30 kDa) fraction showed a compact complexation with curcumin at pH 3.0 with excellent aqueous solubility, stability, and bioaccessibility. Further, complexation enhanced the aqueous solubility of curcumin more than 856-fold. In vitro sequential simulated gastric and intestinal digestion indicated that the bioaccessibility of curcumin was increased from 67% to 95% post complexation. The functional attributes suggest that the LSPH/CUR complex has good foam-forming capacity and emulsion stability, which are crucial for food product formulations. The results indicate that, since LSPH is a dietary protein, it might possibly be formulated as a functional food and as an excellent lipophilic bioactive molecule delivery vehicle in food formulations.


Assuntos
Curcumina/administração & dosagem , Curcumina/química , Sistemas de Liberação de Medicamentos/métodos , Lepidium sativum/química , Hidrolisados de Proteína/química , Disponibilidade Biológica , Curcumina/farmacocinética , Digestão , Portadores de Fármacos/química , Emulsões/química , Humanos , Concentração de Íons de Hidrogênio , Interações Hidrofóbicas e Hidrofílicas , Solubilidade , Espectrometria de Fluorescência
4.
Biomater Sci ; 7(9): 3866-3875, 2019 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-31309204

RESUMO

Photothermal therapy (PTT) is emerging as a promising treatment for skin cancer. Plasmon-resonant gold-coated liposome nanoparticles (Au Lipos NPs) specifically absorb Near Infra-Red (NIR) light resulting in localized hyperthermia (PTT). In the current study, curcumin (a hydrophobic anticancer agent) was entrapped in Au Lipos NPs as nanocrystals to act as an adjuvant for the PTT of melanoma. NIR light irradiation on Au Lipos Cur NPs triggered the release of curcumin nanocrystals which coalesce to form curcumin microcrystals (CMCs). An in situ"nano to micro" transition in the crystal state of curcumin was observed. This in situ transition leads to the formation of CMCs. These CMCs exhibited sustained release of curcumin for a prolonged duration (>10 days). The localized availability of curcumin aids in enhancing PTT by inhibiting the growth and mobility of cancer cells that escape PTT. In the in vitro modified scratch assay, the Au Lipos Cur NP + Laser group showed >1.5 fold enhanced therapeutic coverage when compared with the Au Lipos NP + Laser group. In vivo PTT studies performed in a B16 tumor model using Au Lipos Cur NPs showed a significant reduction of the tumor volume along with the localized release of curcumin in the tumor environment. It was observed that the localized release of curcumin enables an immediate adjuvant effect resulting in the enhancement of PTT.


Assuntos
Adjuvantes Farmacêuticos/química , Antineoplásicos/química , Curcumina/química , Ouro/química , Lipossomos/química , Nanopartículas Metálicas/química , Adjuvantes Farmacêuticos/administração & dosagem , Animais , Antineoplásicos/administração & dosagem , Linhagem Celular Tumoral , Movimento Celular , Quimioterapia Adjuvante , Cristalização , Curcumina/administração & dosagem , Feminino , Humanos , Interações Hidrofóbicas e Hidrofílicas , Hipertermia Induzida , Raios Infravermelhos , Melanoma/terapia , Nanopartículas Metálicas/administração & dosagem , Camundongos Endogâmicos C57BL , Tamanho da Partícula , Fototerapia/métodos , Neoplasias Cutâneas/terapia , Microambiente Tumoral
5.
AAPS PharmSciTech ; 20(6): 250, 2019 Jul 11.
Artigo em Inglês | MEDLINE | ID: mdl-31297635

RESUMO

Melanoma is regarded as the fifth and sixth most common cancer in men and women, respectively, and it is estimated that one person dies from melanoma every hour in the USA. Unfortunately, the treatment of melanoma is difficult because of its aggressive metastasis and resistance to treatment. The treatment of melanoma continues to be a challenging issue due to the limitations of available treatments such as a low response rate, severe adverse reactions, and significant toxicity. Natural polyphenols have attracted considerable attention from the scientific community due to their chemopreventive and chemotherapeutic efficacy. It has been suggested that poorly soluble polyphenols such as curcumin, resveratrol, quercetin, coumarin, and epigallocatechin-3-gallate may have significant benefits in the treatment of melanoma due to their antioxidant, anti-inflammatory, antiproliferative, and chemoprotective efficacies. The major obstacles for the use of polyphenolic compounds are low stability and poor bioavailability. Numerous nanoformulations, including solid lipid nanoparticles, polymeric nanoparticles, micelles, and liposomes, have been formulated to enhance the bioavailability and stability, as well as the therapeutic efficacy of polyphenols. This review will provide an overview of poorly soluble polyphenols that have been reported to have antimetastatic efficacy in melanomas.


Assuntos
Sistemas de Liberação de Medicamentos/métodos , Melanoma/tratamento farmacológico , Polifenóis/administração & dosagem , Polifenóis/química , Neoplasias Cutâneas/tratamento farmacológico , Animais , Antioxidantes/administração & dosagem , Antioxidantes/química , Antioxidantes/metabolismo , Disponibilidade Biológica , Catequina/administração & dosagem , Catequina/análogos & derivados , Catequina/química , Catequina/metabolismo , Curcumina/administração & dosagem , Curcumina/química , Curcumina/metabolismo , Humanos , Melanoma/metabolismo , Melanoma/prevenção & controle , Nanopartículas/administração & dosagem , Nanopartículas/química , Nanopartículas/metabolismo , Polifenóis/metabolismo , Quercetina/administração & dosagem , Quercetina/química , Quercetina/metabolismo , Resveratrol/administração & dosagem , Resveratrol/química , Resveratrol/metabolismo , Neoplasias Cutâneas/metabolismo , Solubilidade
6.
BMC Complement Altern Med ; 19(1): 129, 2019 Jun 13.
Artigo em Inglês | MEDLINE | ID: mdl-31196040

RESUMO

BACKGROUND: Green tea has polyphenols like flavonoids and catechins; mainly epigallocatechin-3-gallate (EGCG), epicatechin gallate (ECG), epigallocatechin (EGC) and epicatechin (EC), out of which EGCG is of higher abundance. EGCG has shown preventive role in hypercholesterolemia. However, due to low oral bioavailability, a need arises to improve its membrane permeability and transporter-mediated intestinal efflux. Therefore, an attempt was made to enhance permeability and bioavailability of EGCG using curcumin to treat hyperlipidemia. Further, it was formulated in herbal tea bags to achieve patient compliance. METHODS: EGCG extracted from green tea leaves was confirmed by High Performance Thin Layer Chromatography. Green tea extract (GTE), curcumin and their mixtures were subjected to Fourier Transform Infra-Red spectroscopy and Differential Scanning Calorimetry for compatibility studies. Powder formulation was prepared comprising GTE, curcumin, sucralose and cardamom. RESULTS: Ex-vivo study was performed on everted goat intestine, analyzed by HPLC and demonstrated highest permeation of GTE:curcumin (220:50) (53.15%) than GTE (20.57%). Antihyperlipidemic activity was performed in rats for 15 days. Blood sample analysis of rats of test groups (formulation and GTE solution) fed on high fat diet showed (mg/dl):cholesterol 80 and 90, triglycerides 73.25 and 85.5, HDL 50.75 and 46, LDL 43.9 and 46, VLDL 14.65 and 17.1 respectively with significant lipid regulating effect. CONCLUSION: Curcumin enhanced permeability of EGCG. Therefore, P-glycoprotein pump inside intestine can be potential mechanism to enhance permeability of EGCG. Thus, EGCG-curcumin herbal tea bag is promising nutraceutical to treat hyperlipidemia in day-to-day life achieving patient compliance.


Assuntos
Antioxidantes/farmacocinética , Catequina/análogos & derivados , Curcumina/administração & dosagem , Hiperlipidemias/tratamento farmacológico , Animais , Antioxidantes/administração & dosagem , Disponibilidade Biológica , Catequina/administração & dosagem , Catequina/farmacocinética , Avaliação Pré-Clínica de Medicamentos , Sinergismo Farmacológico , Feminino , Masculino , Permeabilidade , Fitoterapia , Ratos Sprague-Dawley , Chá
7.
Int J Nanomedicine ; 14: 3311-3330, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31190795

RESUMO

Background: Oral route of administration is preferred for treating breast cancer, especially when continued disease management with good tolerability is required; however, orally administered chemotherapeutics combined with near-infrared (NIR) dyes are hindered by the low bioavailability, insufficient for the desired therapeutic efficacy. In this study, we developed a hybrid self-microemulsifying drug delivery system for co-loading curcumin-phospholipid complex and NIR dye IR780 (CUR/IR780@SMEDDS), to achieve combined phototherapeutic and chemotherapeutic effects against lung metastasis of breast cancer. Methods: CUR/IR780@SMEDDS were characterized. The efficacy against breast cancer metastasis was evaluated by photothermal and photodynamic assessment, cytotoxicity, invasion, and migration in metastatic 4T1 breast cancer cells in vitro, and in vivo oral bioavailability study in rats and pharmacodynamics studies in tumor-bearing nude mice. Results: CUR/IR780@SMEDDS improved oral bioavailability of curcumin and IR780 in rats compared with curcumin and IR780 suspensions. CUR/IR780@SMEDDS exhibited remarkable photothermal and photodynamic effects in vitro. In metastatic 4T1 breast cancer cells, CUR/IR780@SMEDDS combined with localized NIR laser irradiation induced significant cytotoxicity and inhibited invasion and migration of 4T1 cells, an outcome attributable to cumulative effects of IR780-induced hyperthermia and pharmacological effects of curcumin. In orthotopic 4T1 tumor-bearing nude mice, combination of oral administration of CUR/IR780@SMEDDS with local NIR laser irradiation inhibited tumor progression and suppressed lung metastasis.


Assuntos
Neoplasias da Mama/patologia , Corantes/administração & dosagem , Curcumina/administração & dosagem , Curcumina/uso terapêutico , Sistemas de Liberação de Medicamentos , Indóis/administração & dosagem , Neoplasias Pulmonares/secundário , Fosfolipídeos/química , Administração Oral , Animais , Linhagem Celular Tumoral , Curcumina/farmacologia , Feminino , Humanos , Hipertermia Induzida , Camundongos Nus , Ratos Sprague-Dawley
8.
Pharm Res ; 36(8): 116, 2019 Jun 03.
Artigo em Inglês | MEDLINE | ID: mdl-31161340

RESUMO

PURPOSE: Study on curcumin dissolved in natural deep eutectic solvents (NADES) was aimed at exploiting their beneficial properties as drug carriers. METHODS: The concentration of dissolved curcumin in NADES was measured. Simulated gastrointestinal fluids were used to determine the concentration of curcumin and quantum chemistry computations were performed for clarifying the origin of curcumin solubility enhancement in NADES. RESULTS: NADES comprising choline chloride and glycerol had the highest potential for curcumin dissolution. This system was also successfully applied as an extraction medium for obtaining curcuminoids from natural sources, as well as an effective stabilizer preventing curcumin degradation from sunlight. The solubility of curcumin in simulated gastrointestinal fluids revealed that the significant increase of bioavailability takes place in the small intestinal fluid. CONCLUSIONS: Suspension of curcumin in NADES offers beneficial properties of this new liquid drug formulation starting from excreting from natural sources, through safe storage and ending on the final administration route. Therefore, there is a possibility of using a one-step process with this medium. The performed quantum chemistry computations clearly indicated the origin of the enhanced solubility of curcumin in NADES in the presence of intestinal fluids. Direct intermolecular contacts leading to hetero-molecular pairs with choline chloride and glycerol are responsible for elevating the bulk concentration of curcumin. Choline chloride plays a dominant role in the system and the complexes formed with curcumin are the most stable among all possible homo- and hetero-molecular pairs that can be found in NADES-curcumin systems.


Assuntos
Colina/química , Curcumina/química , Portadores de Fármacos/química , Glicerol/química , Extratos Vegetais/química , Curcumina/administração & dosagem , Estabilidade de Medicamentos , Modelos Químicos , Teoria Quântica , Solubilidade , Solventes , Termodinâmica
9.
Phys Chem Chem Phys ; 21(20): 10377-10390, 2019 May 22.
Artigo em Inglês | MEDLINE | ID: mdl-31065651

RESUMO

Herein, novel dehydropeptide-based magnetogels, based on the hydrogelators Npx-l-Phe-Z-ΔAbu-OH, Npx-l-Trp-Z-ΔPhe-OH and Npx-l-Ala-Z-ΔPhe-Gly-l-Arg-Gly-l-Asp-Gly-OH and containing manganese ferrite nanoparticles (diameters around 20 nm), were prepared and characterized. TEM and FTIR measurements showed that the magnetogels maintained the fibrous structure of neat hydrogels, with fibres of ca. 20 nm average width (generally in the range 10-30 nm) and a few conformational changes relative to the neat hydrogels. The magnetogels were tested as nanocarriers for two potential fluorescent antitumor drugs: a thienopyridine derivative and the natural compound curcumin. FRET (Förster resonance energy transfer) from the aromatic moieties (energy donors) of gels to the fluorescent drugs (energy acceptors) and fluorescence anisotropy measurements confirmed the incorporation of both drugs into the magnetogel matrices. The transport of both drugs loaded into the magnetogels to membrane models (small unilamellar vesicles) was assessed by FRET between the fluorescent drugs and the dye Nile Red. The magnetogel possessing the RGD sequence was most promising for the delivery of the thienopyridine derivative, whereas three magnetogels were found to be suitable for the delivery of curcumin.


Assuntos
Portadores de Fármacos/química , Compostos Férricos/química , Compostos de Manganês/química , Nanopartículas/química , Animais , Antineoplásicos/administração & dosagem , Antineoplásicos/química , Linhagem Celular , Curcumina/administração & dosagem , Transferência Ressonante de Energia de Fluorescência , Hidrogéis/química , Magnetismo
10.
Molecules ; 24(6)2019 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-30934561

RESUMO

Curcumin, which is a potential antineuroinflammatory and neuroprotective compound, exhibits poor bioavailability in brain cells due to its difficulty in crossing the blood⁻brain barrier and its rapid metabolism during circulation, which decreases its efficacy in treating chronic neuroinflammatory diseases in the central nervous system. The bioavailability and potential of curcumin can be improved by using a nanodelivery system, which includes solid lipid nanoparticles. Curcumin-loaded solid lipid nanoparticles (SLCN) were efficiently developed to have a particle size of about 86 nm and do not exhibit any toxicity in the endothelial brain cells. Furthermore, the curcumin-loaded solid lipid nanoparticles (SLCN) were studied to assess their efficacy in BV-2 microglial cells against LPS-induced neuroinflammation. The SLCN showed a higher inhibition of nitric oxide (NO) production compared to conventional curcumin in a dose-dependent manner. Similarly, the mRNA and proinflammatory cytokine levels were also reduced in a dose-dependent manner when compared to those with free curcumin. Thus, SLCN could be a potential delivery system for curcumin to treat microglia-mediated neuroinflammation.


Assuntos
Anti-Inflamatórios não Esteroides/administração & dosagem , Curcumina/administração & dosagem , Lipídeos , Lipopolissacarídeos/imunologia , Microglia/efeitos dos fármacos , Microglia/fisiologia , Nanopartículas , Animais , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Lipídeos/química , Camundongos , Nanopartículas/química , Óxido Nítrico
11.
Pharm Biol ; 57(1): 250-254, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30957612

RESUMO

CONTEXT: In vitro and in vivo research has shown that curcumin can alleviate diabetes and the relevant complications. OBJECTIVE: To investigate the effect of curcumin on gestational diabetes (GD). MATERIALS AND METHODS: C57 BL/KsJdb/+(db/+) mice and C57 BL/KsJ+/+ mice (10-12 weeks old) were divided into four groups (n = 15): normal pregnancy (C57 BL/KsJ+/+), GD (C57 BL/KsJdb/+), GD plus low dose curcumin (50 mg/kg, orally gavage every day) and GD plus high dose curcumin (100 mg/kg, orally gavage every day). The tolerance of glucose and insulin were measured on gestation day 10. Body weight at birth and litter size of offspring were investigated, and the expression of oxidative stress factors [thiobarbituric acid reactive substance (TBARS), glutathione (GSH), superoxide dismutase (SOD) and catalase (CAT)] and AMP-activated protein kinase (AMPK), phospho-AMPK, histone deacetylases 4 (HDAC4), pHDAC4 and glucose-6-phosphatase (G6Pase) in the livers were analyzed by ELISA and Western blot on gestation day 20. RESULTS: High dose curcumin could partly ameliorate the intolerance of glucose and insulin, and completely restore the litter size and the body weight of GD mice through decreased TBARS expression (p < 0.05) and increased GSH, SOD and CAT expression (p < 0.05). Enhanced AMPK activation, accompanied with decreased HDAC4 and G6Pase expression (p < 0.05) were partly contributed to the alleviation of GD mediated by curcumin. CONCLUSIONS: Although further detailed mechanism needs to be deciphered, curcumin can be considered as an alternative treatment for gestational diabetes.


Assuntos
Proteínas Quinases Ativadas por AMP/efeitos dos fármacos , Curcumina/farmacologia , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Gestacional/tratamento farmacológico , Proteínas Quinases Ativadas por AMP/metabolismo , Animais , Western Blotting , Catalase/metabolismo , Curcumina/administração & dosagem , Diabetes Mellitus Experimental/fisiopatologia , Diabetes Gestacional/fisiopatologia , Relação Dose-Resposta a Droga , Ensaio de Imunoadsorção Enzimática , Feminino , Glucose/metabolismo , Glutationa/metabolismo , Insulina/metabolismo , Tamanho da Ninhada de Vivíparos/efeitos dos fármacos , Camundongos , Camundongos Endogâmicos C57BL , Estresse Oxidativo/efeitos dos fármacos , Gravidez , Superóxido Dismutase/metabolismo
12.
Int J Mol Sci ; 20(5)2019 Mar 07.
Artigo em Inglês | MEDLINE | ID: mdl-30866573

RESUMO

Oxidative stress resulting from decreased antioxidant protection and increased reactive oxygen and nitrogen species (RONS) production may contribute to muscle mass loss and dysfunction during aging. Curcumin is a phenolic compound shown to upregulate antioxidant defenses and directly quench RONS in vivo. This study determined the impact of prolonged dietary curcumin exposure on muscle mass and function of aged rats. Thirty-two-month-old male F344xBN rats were provided a diet with or without 0.2% curcumin for 4 months. The groups included: ad libitum control (CON; n = 18); 0.2% curcumin (CUR; n = 18); and pair-fed (PAIR; n = 18) rats. CUR rats showed lower food intake compared to CON, making PAIR a suitable comparison group. CUR rats displayed larger plantaris mass and force production (vs. PAIR). Nuclear fraction levels of nuclear factor erythroid-2 related-factor-2 were greater, and oxidative macromolecule damage was lower in CUR (vs. PAIR). There were no significant differences in measures of antioxidant status between any of the groups. No difference in any measure was observed between CUR and CON rats. Thus, consumption of curcumin coupled with reduced food intake imparted beneficial effects on aged skeletal muscle. The benefit of curcumin on aging skeletal muscle should be explored further.


Assuntos
Curcumina/administração & dosagem , Músculo Esquelético/efeitos dos fármacos , Fator 2 Relacionado a NF-E2/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Envelhecimento , Animais , Curcumina/farmacologia , Suplementos Nutricionais , Ingestão de Alimentos , Peroxidação de Lipídeos/efeitos dos fármacos , Masculino , Modelos Animais , Músculo Esquelético/fisiologia , Estresse Oxidativo/efeitos dos fármacos , Ratos
13.
Int J Biol Macromol ; 131: 184-191, 2019 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-30840864

RESUMO

The study deals with the synthesis and characterization of chitosan-g-Poly (Acrylic acid-co-Acrylamide) [chit-g-Poly (AA-co-Am)] for sustained release of curcumin. The formation of chit-g-Poly (AA-co-Am) was ascertained through various spectral, thermal, microscopic methods and zeta potential. The potential of chit-g-Poly (AA-co-Am) for drug delivery applications were investigated through pH regulated kinetic models, in vitro antibacterial assay and molecular docking studies. The study reveals antibacterial activity of chit-g-Poly (AA-co-Am) against Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa along with enhanced binding with bacterial receptors. In this study, nanoparticle of curcumin drug with grafted chitosan (NpCGC) was developed as effective nano therapeutic drug delivery system. Kinetic data of NpCGC reveals that the enhanced release of curcumin from NpCGC has been occurred at pH 5.4. The present study provides an economical and eco-friendly approach towards the preparation of chit-g-Poly (AA-co-Am) for sustained drug delivery applications.


Assuntos
Quitosana/química , Curcumina/administração & dosagem , Portadores de Fármacos/química , Nanopartículas/química , Acrilamidas/química , Resinas Acrílicas/química , Antibacterianos/administração & dosagem , Antibacterianos/química , Bactérias/efeitos dos fármacos , Curcumina/química , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Concentração de Íons de Hidrogênio , Cinética , Micro-Ondas , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Nanopartículas/ultraestrutura , Análise Espectral , Temperatura Ambiente , Viscosidade
14.
Molecules ; 24(5)2019 Feb 27.
Artigo em Inglês | MEDLINE | ID: mdl-30818888

RESUMO

Curcumin (CC) is known to have anti-inflammatory and anti-oxidative properties and has already been tested for its efficiency in different diseases including diabetes mellitus (DM). New formulations and route administration were designed to obtain products with higher bioavailability. Our study aimed to test the effect of intraperitoneal (i.p.) administration of liposomal curcumin (lCC) as pre-treatment in streptozotocin(STZ)-induced DM in rats on oxidative stress, liver, and pancreatic functional parameters. Forty-two Wistar-Bratislava rats were randomly divided into six groups (seven animals/group): control (no diabetes), control-STZ (STZ-induced DM -60 mg/100g body weight a single dose intraperitoneal administration, and no CC pre-treatment), two groups with DM and CC pre-treatment (1mg/100g bw-STZ + CC1, 2 mg/100g bw-STZ + CC2), and two groups with DM and lCC pre-treatment (1 mg/100g bw-STZ + lCC1, 2 mg/100g bw-STZ + lCC1). Intraperitoneal administration of Curcumin in diabetic rats showed a significant reduction of nitric oxide, malondialdehyde, total oxidative stress, and catalase for both evaluated formulations (CC and lCC) compared to control group (p < 0.005), with higher efficacy of lCC formulation compared to CC solution (p < 0.002, excepting catalase for STZ + CC2vs. STZ + lCC1when p = 0.0845). The CC and lCC showed hepatoprotective and hypoglycemic effects, a decrease in oxidative stress and improvement in anti-oxidative capacity status against STZ-induced DM in rats (p < 0.002). The lCC also proved better efficacy on MMP-2, and -9 plasma levels as compared to CC (p < 0.003, excepting STZ + CC2 vs. STZ + lCC1 comparison with p = 0.0553). The lCC demonstrated significantly better efficacy as compared to curcumin solution on all serum levels of the investigated markers, sustaining its possible use as adjuvant therapy in DM.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Curcumina/farmacologia , Complicações do Diabetes/prevenção & controle , Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/farmacologia , Lipossomos/administração & dosagem , Animais , Anti-Inflamatórios não Esteroides/administração & dosagem , Antioxidantes/administração & dosagem , Antioxidantes/farmacologia , Curcumina/administração & dosagem , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Experimental/patologia , Hipoglicemiantes/administração & dosagem , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Masculino , Estresse Oxidativo , Pâncreas/efeitos dos fármacos , Pâncreas/metabolismo , Pâncreas/patologia , Ratos , Ratos Wistar
15.
Fish Shellfish Immunol ; 89: 83-90, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30898618

RESUMO

The present study was conducted to evaluate the effects of various levels of dietary curcumin on growth performance, haematological values, immunity and protection against Aeromonas salmonicida subsp. achromogenes infection in rainbow trout, Oncorhynchus mykiss. Fish were fed with diets containing different levels of curcumin; 0% (C), %1 (E1), %2 (E2) and %4 (E3), as treatment groups. After 8 weeks of feeding, the growth performance [weight gain (WG), specific growth rate (SGR) and feed conversion ratio (FCR)], haematological values [the red blood cell (RBC) count, haemoglobin (Hb) concentration, haematocrit (Ht) level and erythrocyte indices: mean corpuscular volume (MCV), mean corpuscular haemoglobin (MCH) and mean corpuscular haemoglobin concentration (MCHC)], various immune parameters [white blood cell (WBC) count, oxidative radical production (nitroblue tetrazolium (NBT) assay), phagocytic activity (PA) and phagocytic index (PI), total protein (TP) and immunoglobulin M (IgM) levels, serum bactericidal (BA), lysozyme (LYZ) and myeloperoxidase (MPO) activities] and antioxidant capacity [tissue malondialdehyde (MDA) levels and superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GSH-Px) activities] were analysed. In addition, fish were challenged by Aeromonas salmonicida subsp. achromogenes and survival rate was recorded for 14 days. The results indicated that the growth performance was significantly influenced by the dietary curcumin levels, the maximal WG and SGR occurred at fish fed the diet containing 2% curcumin. Fish fed the diet containing curcumin had lower FCR than those fed the control diet. The RBC count, Hb concentration, and Ht level increased in the groups fed with curcumin when compared with the control group. However, there were no significant differences in the MCV, MCH and MCHC values among experimental groups. All the chosen immune parameters were enhanced in the groups fed diets containing curcumin. Also, the relative percentage survivals were higher in the groups fed with curcumin, especially in the E2 group, compared to the control. The dietary curcumin stimulated the SOD, CAT and GSH-Px activities in liver, head kidney and spleen as compared to the control group; however, a reverse trend was observed in the MDA levels of tissues. The highest values for haematological, immunological (except TP level of E3 group) and antioxidant parameters were found in the E2 group. These results collectively suggest that curcumin can be used in aquaculture to improve the growth, haematological values, immune responses, antioxidant capacity and disease resistance of rainbow trout, O. mykiss.


Assuntos
Antioxidantes/metabolismo , Curcumina/administração & dosagem , Resistência à Doença/efeitos dos fármacos , Doenças dos Peixes/imunologia , Oncorhynchus mykiss/imunologia , Aeromonas salmonicida , Ração Animal/análise , Animais , Análise Química do Sangue/veterinária , Dieta/veterinária , Suplementos Nutricionais/análise , Infecções por Bactérias Gram-Negativas/imunologia , Infecções por Bactérias Gram-Negativas/veterinária , Distribuição Aleatória
16.
Int J Mol Sci ; 20(6)2019 Mar 22.
Artigo em Inglês | MEDLINE | ID: mdl-30909499

RESUMO

The anti-cancer properties of curcumin in vitro have been documented. However, its clinical use is limited due to rapid metabolization. Since irradiation of curcumin has been found to increase its anti-cancer effect on several tumor types, this investigation was designed to determine whether irradiation with visible light may enhance the anti-tumor effects of low-dosed curcumin on renal cell carcinoma (RCC) cell growth and proliferation. A498, Caki1, and KTCTL-26 cells were incubated with curcumin (0.1⁻0.4 µg/mL) and irradiated with 1.65 J/cm² visible light for 5 min. Controls were exposed to curcumin or light alone or remained untreated. Curcumin plus light, but not curcumin or light exposure alone altered growth, proliferation, and apoptosis of all three RCC tumor cell lines. Cells were arrested in the G0/G1 phase of the cell cycle. Phosphorylated (p) CDK1 and pCDK2, along with their counter-receptors Cyclin B and A decreased, whereas p27 increased. Akt-mTOR-signaling was suppressed, the pro-apoptotic protein Bcl-2 became elevated, and the anti-apoptotic protein Bax diminished. H3 acetylation was elevated when cells were treated with curcumin plus light, pointing to an epigenetic mechanism. The present findings substantiate the potential of combining low curcumin concentrations and light as a new therapeutic concept to increase the efficacy of curcumin in RCC.


Assuntos
Curcumina/farmacologia , Luz , Antineoplásicos/química , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Carcinoma de Células Renais/genética , Carcinoma de Células Renais/metabolismo , Carcinoma de Células Renais/patologia , Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Proliferação de Células/efeitos da radiação , Sobrevivência Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos da radiação , Curcumina/administração & dosagem , Técnicas de Silenciamento de Genes , Humanos
17.
Carbohydr Polym ; 213: 70-78, 2019 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-30879691

RESUMO

A novel ß-cyclodextrin-based nanosponge (CDNS) was proposed as curcumin (CUR) delivery system improving pharmacokinetics and anticancer activity of CUR. The effect of molar ratio of Epiclon (EPI) as cross-linker and ß-cyclodextrin (ßCD) on the porosity, surface area, swelling ratio, CUR solubility and loading capacity, rate of drug release and selective toxicity of the CDNSs was fully investigated. The high degree of cross-linking led to the formation of mesoporous CDNS having high specific surface area and high loading capacity. All CUR-free CDNSs showed no toxicity against MCF 10A and 4T1 cells as normal and cancerous cells, respectively. While CDNSs-CUR exhibited selective toxicity against cancerous cells. In sum, high CUR aqueous solubility, significant loading and controllable release of the CUR, outstanding and selective toxicity against cancerous cells make CDNS8-CUR (EPI/ßCD = 8) as promising candidate for further study in the cancer therapy.


Assuntos
Reagentes para Ligações Cruzadas/farmacologia , Curcumina/toxicidade , Nanopartículas/química , beta-Ciclodextrinas/farmacologia , Animais , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Reagentes para Ligações Cruzadas/administração & dosagem , Reagentes para Ligações Cruzadas/química , Curcumina/administração & dosagem , Curcumina/química , Relação Dose-Resposta a Droga , Sistemas de Liberação de Medicamentos , Humanos , Camundongos , Estrutura Molecular , Tamanho da Partícula , Solubilidade , Relação Estrutura-Atividade , Propriedades de Superfície , Termodinâmica , beta-Ciclodextrinas/química
18.
Indian J Dent Res ; 30(1): 31-36, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30900653

RESUMO

Context: It is important to develop new therapeutic materials that have requisite clinical actions, are safe and economical. Aims: This study aims to histologically evaluate curcumin, an extract of turmeric (Curcuma longa) as a pulpotomy agent in rat molars and to compare it to mineral trioxide aggregate (MTA). Settings and Design: Animal study. Subjects and Methods: Twelve Wistar-Albino rats were randomly divided into two groups of 6 each. Pulpotomies were performed on caries free maxillary first and second molars on both sides of the arch, with MTA and curcumin (24 teeth each), respectively. Access cavities were sealed with resin-modified glass ionomer cement. Postoperative histological evaluation of pulpotomized teeth in both groups was done at 7, 14, and 30 days under a light microscope (×10). Statistical Analysis Used: Data were evaluated with Freidman's test and Mann-Whitney test at 0.05 level. Results: (a) There was a gradual reduction in inflammatory cell response in both groups across time periods tested (MTA P = 0.074, curcumin P = 0.039). (b) The overall architecture of pulp was maintained better in the curcumin group across all time periods tested (P = 0.368). (c) Dentinal bridge formation was consistently seen across time periods tested in MTA group (P = 0.9094) and was feeble in curcumin group (P = 0.9094) across time periods tested. Conclusions: Curcumin has been shown to have wound healing properties. It has the potential to be developed into a predictable and cost-effective vital pulp therapy medicament.


Assuntos
Compostos de Alumínio/farmacologia , Compostos de Cálcio/farmacologia , Curcumina/farmacologia , Polpa Dentária/patologia , Polpa Dentária/fisiologia , Óxidos/farmacologia , Agentes de Capeamento da Polpa Dentária e Pulpectomia/farmacologia , Pulpotomia/métodos , Silicatos/farmacologia , Cicatrização/efeitos dos fármacos , Compostos de Alumínio/administração & dosagem , Animais , Compostos de Cálcio/administração & dosagem , Curcumina/administração & dosagem , Combinação de Medicamentos , Óxidos/administração & dosagem , Ratos Wistar , Silicatos/administração & dosagem
19.
J Nanobiotechnology ; 17(1): 44, 2019 Mar 27.
Artigo em Inglês | MEDLINE | ID: mdl-30917812

RESUMO

BACKGROUND: The combination of multiple chemotherapeutics has been used in the clinic for enhanced cancer chemotherapy, however, frequent relapse, chemo-resistance and side effects remains therapeutic hurdles. Thus, the development of co-delivery system with enhanced targeting and synergistic different modal treatments has been proposed as promising strategies for intensive improvement of the therapeutic outcomes. RESULTS: We fabricated a nanocarrier based on gold nanorods (Au NRs), cRGD peptide-modified and multi-stimuli-responsive paclitaxel (PTX) and curcumin (CUR) release for synergistic anticancer effect and chemo-photothermal therapy (PTX/CUR/Au NRs@cRGD). The specific banding of cRGD to αvß3 integrin receptor on the tumor cell surfaces facilitated the endocytosis of PTX/CUR/Au NRs@cRGD, and the near-infrared ray (NIR) further enhanced the drug release and chemotherapeutical efficiency. Compared to single drug, single model treatment or undecorated-PTX/CUR/Au NRs, the PTX/CUR/Au NRs@cRGD with a mild NIR showed significantly enhanced apoptosis and S phase arrest in three cancer cell lines in vitro, and improved drug accumulation in tumor sites as well as tumor growth inhibition in vivo. CONCLUSIONS: The tumor targeted chemo-photothermal therapy with the synergistic effect of dual drugs provided a versatile strategy for precise cancer therapy.


Assuntos
Antineoplásicos/administração & dosagem , Curcumina/administração & dosagem , Portadores de Fármacos/química , Liberação Controlada de Fármacos , Ouro/química , Nanotubos/química , Paclitaxel/administração & dosagem , Células A549 , Animais , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Curcumina/química , Células Hep G2 , Humanos , Raios Infravermelhos , Integrina alfaVbeta3/metabolismo , Células KB , Camundongos Endogâmicos BALB C , Paclitaxel/química , Tamanho da Partícula , Peptídeos Cíclicos/metabolismo , Fototerapia/métodos , Propriedades de Superfície
20.
Anticancer Res ; 39(3): 1161-1168, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30842145

RESUMO

BACKGROUND/AIM: Curcumin is being widely investigated for its anticancer properties and several studies in the literature suggest that curcumin is distributed to a higher degree in cancer cells compared to normal cells. The goal of this study was to investigate the disposition of curcumin in the form of Lipocurc™ in multiple myeloma (MM)-causing plasma cell lines and B-lymphocytes from healthy individuals and compare the uptake to previously published data for red blood cells (RBCs), peripheral blood mononuclear cells (PBMCs) from healthy individuals and PBMCs from patients with chronic lymphocytic leukemia (CLL-cells). MATERIALS AND METHODS: Two MM-producing cell lines were studied: RPMI-8266, an IgG lambda cell line, and NCL-H929, an IgA kappa line. The distribution of liposomal curcumin and its metabolism to the major stable metabolite tetrahydrocurcumin (THC) were measured in vitro in the cell lines and B-lymphocytes. The cells were incubated in plasma protein-supplemented media with liposomal curcumin (Lipocurc™) for 15 min at 37°C and the levels of curcumin and THC in cells and medium were determined by liquid chromatography tandem mass spectrometry. RESULTS: Extremely intense uptake was seen in both MM lines compared to that in B-lymphocytes and previously published data in RBCs, PBMCs and CLL cells. The levels of curcumin in RPMI-8266 and NCI-H929 cells were 14,225±847 and 12,723±500 pg/106 cells compared to 19±5,587±86 and 3,122±166 pg/106 cells in RBCs, PBMCs and CLL cells, respectively. Conversion of curcumin to THC was greatest in PBMCs, considerably less in CLL cells and minimal or absent in B-lymphocytes and MM cell lines. CONCLUSION: The extremely intense uptake of curcumin (as Lipocurc™) in both MM lines further suggests that Lipocurc™ should be investigated in the treatment of patients with this disease.


Assuntos
Antineoplásicos/administração & dosagem , Linfócitos B/metabolismo , Curcumina/administração & dosagem , Eritrócitos/metabolismo , Leucemia Linfocítica Crônica de Células B/metabolismo , Mieloma Múltiplo/metabolismo , Linhagem Celular Tumoral , Humanos , Lipossomos
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA