RESUMO
Chondroitin sulfate (CS)-calcium complex (CSCa) was fabricated, and the structural characteristics of CSCa and its proliferative bioactivity to the chondrocyte were investigated in vitro. Results suggested calcium ions could bind CS chains forming polysaccharide-metal complex, and the maximum calcium holding capacity of CSCa reached 4.23 %. Characterization of CSCa was performed by EDS, AFM, FTIR, UV, XRD and 1H-NMR. It was found that calcium ions were integrated with CS by binding the sulfate or carboxyl groups. The thermal properties analysis indicated CSCa had a good thermal stability by TGA and DSC. CSCa could interact the calcium-sensing receptor increasing the intracellular calcium ions and influence the cell cycle. The TGF-ß1 secretion induced by CSCa could activate the TGF-ß/Smads pathway and change the genes associated proliferation expression ultimately leading to the chondrocyte proliferation. This research probably has an important implication for understanding the effect of CSCa on bone care as food supplements.
Assuntos
Cálcio/metabolismo , Cálcio/farmacologia , Condrócitos/efeitos dos fármacos , Condrócitos/metabolismo , Sulfatos de Condroitina/síntese química , Sulfatos de Condroitina/farmacologia , Apoptose/efeitos dos fármacos , Cálcio/química , Ciclo Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Células Cultivadas , Condrócitos/citologia , Sulfatos de Condroitina/química , Expressão Gênica , Humanos , Técnicas In Vitro , Espectroscopia de Ressonância Magnética , Modelos Biológicos , Simulação de Acoplamento Molecular , Estrutura Molecular , Tamanho da Partícula , Receptores de Detecção de Cálcio/química , Receptores de Detecção de Cálcio/genética , Receptores de Detecção de Cálcio/metabolismo , Espectroscopia de Infravermelho com Transformada de Fourier , Fator de Crescimento Transformador beta1/metabolismoRESUMO
Chondroitin sulphate is a sulphated glycosaminoglycan biopolymer composed over 100 individual sugars. Chondroitin sulphate nanoparticles (NPs) loaded with catechin were prepared by an ionic gelation method using AlCl3 and optimised for polymer and cross-linking agent concentration, curing time and stirring speed. Zeta potential, particle size, loading efficiency, and release efficiency over 24â h (RE24%) were evaluated. The surface morphology of NPs was investigated by scanning electron microscopy and their thermal behaviour by differential scanning calorimetric. Antioxidant effect of NPs was determined by chelating activity of iron ions. The cell viability of mesenchymal stem cells was determined by 3-[4, 5-dimethylthiazol-2-yl]-2, 5-diphenyl tetrazolium bromide assay and the calcification of osteoblasts was studied by Alizarin red staining. The optimised NPs showed particle size of 176â nm, zeta potential of -20.8â mV, loading efficiency of 93.3% and RE24% of 80.6%. The chatechin loaded chondroitin sulphate NPs showed 70-fold more antioxidant activity, 3-fold proliferation effect and higher calcium precipitation in osteoblasts than free catechin.
Assuntos
Alumínio/química , Sulfatos de Condroitina/síntese química , Portadores de Fármacos/síntese química , Composição de Medicamentos/métodos , Flavonoides/administração & dosagem , Nanopartículas/química , Chá/química , Calcificação Fisiológica/efeitos dos fármacos , Catequina/administração & dosagem , Catequina/isolamento & purificação , Catequina/farmacocinética , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Sulfatos de Condroitina/química , Reagentes de Ligações Cruzadas/química , Portadores de Fármacos/química , Liberação Controlada de Fármacos , Flavonoides/isolamento & purificação , Flavonoides/farmacocinética , Humanos , Íons , Células-Tronco Mesenquimais/efeitos dos fármacos , Células-Tronco Mesenquimais/fisiologia , Osteoblastos/efeitos dos fármacos , Osteoblastos/fisiologia , Tamanho da PartículaRESUMO
A novel selenium-chondroitin sulfate (SeCS) was synthesized by ultrasonic and dialysis method. With characterization by FTIR, XRD and TEM, the SeCS was found to form nanoparticles in distilled water through a self-aggregation progress. The SeCS nanoparticles had sizes between 30 and 200 nm with selenium entrapment efficiency of about 10.1%. The anti-toxin capacity of SeCS nanoparticles was demonstrated through MTT and apoptosis assays in vitro. Results indicated that the SeCS was less cytotoxic to chondrocytes than sodium selenite. In particular, the SeCS could obviously alleviate chondrocyte apoptosis induced by T-2 toxin compared to chondroitin sulfate. These results thus represent an advanced understanding of the properties of SeCS nanoparticles and demonstrate their exciting potential applications in therapy of Kashin-Beck disease (KBD) and osteoarthritis.
Assuntos
Apoptose/efeitos dos fármacos , Condrócitos/efeitos dos fármacos , Sulfatos de Condroitina/química , Sulfatos de Condroitina/farmacologia , Nanopartículas/química , Selênio/química , Selênio/farmacologia , Linhagem Celular , Condrócitos/citologia , Sulfatos de Condroitina/síntese química , Humanos , Doença de Kashin-Bek/tratamento farmacológico , Nanopartículas/ultraestrutura , Osteoartrite/tratamento farmacológicoRESUMO
The purpose of this study was to investigate the anti-arthritic effects of synthesized chondroitin sulfate E hexasaccharide (sCSE-6, CAS 866407-73-0), using a type II collagen-induced arthritis model in mice. sCSE-6 was administered subcutaneously on a daily basis to type II collagen (CII)-sensitized mice from day 0 to day 55. The severity of arthritis, as well as the immunohistological features of the arthritic mice, were analyzed. sCSE-6 inhibited the course of arthritis and restored the body weight loss of CII-immunized mice. An immunohistological analysis showed that bone/cartilage destruction in the arthritic mice was significantly attenuated by sCSE-6 treatment, with a marginal inhibition of synovial inflammation also observed. The beneficial effect of sCSE-6 on bone destruction, which is the most important factor in preventing arthritis, is particularly noteworthy. In summary, sCSE-6 inhibited arthritis and helped to prevent bone and cartilage destruction in a type II collagen-induced arthritis model in mice. The findings indicated that CSE oligosaccharides might be a novel potential therapeutic tool for rheumatoid arthritis.