In this work the DBL3x domain of the erythrocyte membrane protein from Plasmodium Falciparum (PfEMP1), was revisited as a potential molecular target for the development of new drugs against malaria. This protein interacts with chondroitin sulfate A (CSA), a glycosaminoglycan present in the substance fundamental for connective tissues of vertebrates and is implicated in malaria complications in pregnant women. We performed molecular docking and molecular dynamic studies of DBL3x complexed with CSA and five analogues, where the sulfate group was replaced by phosphate, in order to evaluate if the better electrostatic interactions provided by phosphate groups could afford better binders capable of preventing the binding of CSA to DBL3x. Results suggest that all proposed compounds have high affinity towards DBL3x and could bind better to the DBL3x domain of PfEMP1 than CSA, qualifying as potential inhibitors of this protein and, therefore, new potential leads for the drug design against malaria.Communicated by Ramaswamy H. Sarma.
- MeSH
- antigeny protozoální chemie MeSH
- chondroitin sulfáty chemie metabolismus farmakologie MeSH
- erytrocyty metabolismus MeSH
- fosfáty MeSH
- glykosaminoglykany metabolismus MeSH
- lidé MeSH
- malárie * komplikace metabolismus MeSH
- membránové proteiny metabolismus MeSH
- parazitární komplikace těhotenství * metabolismus MeSH
- placenta metabolismus MeSH
- Plasmodium falciparum chemie MeSH
- protozoální proteiny chemie MeSH
- simulace molekulární dynamiky MeSH
- simulace molekulového dockingu MeSH
- sírany metabolismus MeSH
- těhotenství MeSH
- tropická malárie * farmakoterapie MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- těhotenství MeSH
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
Polymeric biomaterials are widely used in medical applications owing to their low cost, processability and sufficient toughness. Surface modification by creating a thin film of bioactive agents is promising technique to enhance cellular interactions, regulate the protein adsorption and/or avoid bacterial infections. Polyethylene is one of the most used polymeric biomaterial but its hydrophobic nature impedes its further chemical modifications. Plasma treatment is unique method to increase its hydrophilicity by incorporating hydrophilic oxidative functional groups and tailoring the surface by physical etching. Furthermore, grafting of polymer brushes of amine group containing monomers onto the functionalized surface lead to strongly immobilized bioactive agents at the final step. Chondroitin sulphate is natural polysaccharide mainly found in connective cartilage tissue which used as a bioactive agent to immobilize onto polyethylene surface by multistep method in this study.
- MeSH
- chondroitin sulfáty chemie farmakologie MeSH
- fibroblasty cytologie účinky léků MeSH
- fotoelektronová spektroskopie MeSH
- mikroskopie atomárních sil MeSH
- myši MeSH
- proliferace buněk účinky léků MeSH
- skot MeSH
- smáčivost MeSH
- spektroskopie infračervená s Fourierovou transformací MeSH
- tvar buňky účinky léků MeSH
- voda chemie MeSH
- zvířata MeSH
- Check Tag
- myši MeSH
- skot MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
Poly-(lactide-co-glycolide) (PLGA) is an FDA-approved biodegradable polymer which has been widely used as a scaffold for tissue engineering applications. Collagen has been used as a coating material for bone contact materials, but relatively little interest has focused on biomimetic coating of PLGA with extracellular matrix components such as collagen and the glycosaminoglycan chondroitin sulfate (CS). In this study, PLGA films were coated with collagen type I or collagen I with CS (collagen I/CS) to investigate the effect of CS on the behaviour of the osteoblastic cell line MG 63. Collagen I/CS coatings promoted a significant increase in cell number after 3 days (in comparison to PLGA) and after 7 days (in comparison to PLGA and collagencoated PLGA). No influence of collagen I or collagen I/CS coatings on the spreading area after 1 day of culture was observed. However, the cells on collagen I/CS formed numerous filopodia and displayed well developed vinculin-containing focal adhesion plaques. Moreover, these cells contained a significantly higher concentration of osteocalcin, measured per mg of protein, than the cells on the pure collagen coating. Thus, it can be concluded that collagen I/CS coatings promote MG 63 cell proliferation, improve cell adhesion and enhance osteogenic cell differentiation.
- MeSH
- biokompatibilní potahované materiály farmakologie chemie MeSH
- buněčné inženýrství metody MeSH
- buněčné linie MeSH
- chondroitin sulfáty farmakologie chemie MeSH
- kolagen typu I farmakologie chemie MeSH
- kultivované buňky MeSH
- kyselina mléčná chemie MeSH
- kyselina polyglykolová chemie MeSH
- lidé MeSH
- osteoblasty cytologie fyziologie účinky léků MeSH
- osteogeneze fyziologie účinky léků MeSH
- proliferace buněk účinky léků MeSH
- testování materiálů MeSH
- tkáňové podpůrné struktury MeSH
- viabilita buněk účinky léků MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- práce podpořená grantem MeSH
- MeSH
- anthrachinony terapeutické užití MeSH
- antiflogistika nesteroidní terapeutické užití MeSH
- chondroitin sulfáty farmakologie chemie terapeutické užití MeSH
- farmakoterapie metody MeSH
- fixní kombinace léků MeSH
- glukosamin farmakologie terapeutické užití MeSH
- Glycine max MeSH
- hodnocení léčiv MeSH
- klinické zkoušky jako téma MeSH
- kolenní kloub patofyziologie patologie MeSH
- kyselina hyaluronová farmakologie chemie terapeutické užití MeSH
- léky s prodlouženým účinkem farmakologie terapeutické užití MeSH
- lidé MeSH
- nemoci kloubů farmakoterapie klasifikace MeSH
- patela patofyziologie patologie MeSH
- Persea MeSH
- sporty MeSH
- Check Tag
- lidé MeSH
- Klíčová slova
- Condrosulf 400, Condrosulf 800,
- MeSH
- chondroitin sulfáty farmakologie chemie terapeutické užití MeSH
- epidemiologické studie MeSH
- hodnocení léčiv MeSH
- léčivé přípravky MeSH
- lidé MeSH
- osteoartróza farmakoterapie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- metaanalýza MeSH
This review summarizes recent knowledge on the efficacy of glucosamine (GS) and/or chondroitin sulfate (CS) in the therapy of mild to moderate osteoarthritis (OA). OA, the most common joint disease is a significant source of disability, quality of life impairment and a considerable burden to any health care system. In the Czech Republic, glucosamine sulfate (GS) and chondroitin sulfate (CS) are available both as prescription drugs and as food supplements. Based on available data both are useful in the earlier stages of OA when combined with other modalities such as weight loss and exercises. They appear to relieve pain and improve range of the joint motion. In addition, they also display mild anti-inflammatory effects. However, controversy still exists over their ability to change significantly the natural history of the osteoarthritic joint. This effect is not easy to demonstrate for any other treatment modalities apart from joint replacement. Monitoring the cure efficacy by X-ray has been recently criticised and hence future techniques are anticipated for this reason. Further, long-term oral administration is required to obtain slightly increased levels of GS and/or CS in human blood. Both reviewed saccharides are well tolerated with negligible adverse reactions. In conclusion, the authors suggest that GS and CS should be classified as food supplements only.
- MeSH
- chondroitin sulfáty chemie metabolismus terapeutické užití MeSH
- glukosamin chemie metabolismus terapeutické užití MeSH
- lidé MeSH
- osteoartróza farmakoterapie metabolismus MeSH
- potravní doplňky MeSH
- výsledek terapie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- přehledy MeSH
