Chondroitin sulfate Dotaz Zobrazit nápovědu
Cartilaginous extract, chondroitin sulfate C as well as dextran sulfate in gelatin pellets have an inhibitory effect on the development of fine capillaries, in contrast to pure gelatin pellets or pellets with sucrose. These results suggest an unspecific inhibitory effect of anionic saccharidic polymers on the development of chorioallantoic membrane vessels, because the chemical structure of dextran sulfate is (except anionic groups) different from chondroitin sulfate in the pure form or in the form of proteoglycans (in cartilaginous extract).
- MeSH
- alantois krevní zásobení účinky léků MeSH
- chondroitin sulfáty farmakologie MeSH
- chrupavka metabolismus MeSH
- gely MeSH
- kuřecí embryo MeSH
- proteoglykany izolace a purifikace farmakologie MeSH
- síran dextranu farmakologie MeSH
- želatina MeSH
- zvířata MeSH
- Check Tag
- kuřecí embryo MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- chondroitin sulfáty MeSH
- gely MeSH
- proteoglykany MeSH
- síran dextranu MeSH
- želatina MeSH
Chondroitin sulfate (CS) was chemoselectively oxidized by Tempo/NaClO to C-6 aldehyde of a D-galactosamine subunit (GalNAc). The subsequent, spontaneous desulfatation of oxidized CS gave rise to α,β-unsaturated aldehyde. A new derivative of CS was fully characterized and a degree of oxidation was determined by spectroscopic analysis. The optimization of reaction conditions showed a proportional degree of oxidation to an amount of sodium hypochlorite. The utility of α,β-unsaturated aldehyde for crosslinking and conjugation was demonstrated by a seamless condensation with various N-nucleophiles. We also demonstrated pH-dependent release of biologically active agents from oxidized CS. A live-dead assay in the presence of α,β-unsaturated aldehyde revealed unaffected viability of NIH 3T3 fibroblasts, which made this precursor promising for several biomedical applications including drug delivery and tissue engineering.
- Klíčová slova
- Chondroitin sulfate, Crosslinking, Hydrogel, Oxidation, Tissue engineering,
- MeSH
- aldehydy chemie MeSH
- biokompatibilní materiály škodlivé účinky chemická syntéza chemie MeSH
- buňky 3T3 MeSH
- chondroitin sulfáty chemie MeSH
- fibroblasty účinky léků MeSH
- myši MeSH
- reagencia zkříženě vázaná chemie MeSH
- viabilita buněk MeSH
- zvířata MeSH
- Check Tag
- myši MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- aldehydy MeSH
- biokompatibilní materiály MeSH
- chondroitin sulfáty MeSH
- reagencia zkříženě vázaná MeSH
Chondroitin sulfate (CS) was regio-specifically modified to an unsaturated derivative (ΔCS) with a double bond in positions 4 and 5 of N-acetyl-d-galactosamine. The structure of ΔCS was elucidated in detail by two dimensional nuclear magnetic resonance, ultraviolet spectroscopy and mass spectrometry. The introduction of a nucleophilic CC double bond into a polymer backbone had no influence on biocompatibility of CS, which was demonstrated by MTT live-dead assay and enzymatic degradation in vitro. On the other hand the chemical modification significantly enhanced the reactivity of ΔCS towards numerous oxidizing agents, which might be promising for a variety of biomedical and cosmetic applications.
- Klíčová slova
- Antioxidant activity, Chondroitin sulfate, Cosmetics, Oxidation, Reduction,
- MeSH
- bifenylové sloučeniny chemie MeSH
- buňky 3T3 MeSH
- chondroitin sulfáty chemická syntéza chemie toxicita MeSH
- myši MeSH
- oxidace-redukce MeSH
- pikráty chemie MeSH
- scavengery volných radikálů chemická syntéza chemie toxicita MeSH
- techniky syntetické chemie MeSH
- testování materiálů MeSH
- zvířata MeSH
- Check Tag
- myši MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- 1,1-diphenyl-2-picrylhydrazyl MeSH Prohlížeč
- bifenylové sloučeniny MeSH
- chondroitin sulfáty MeSH
- pikráty MeSH
- scavengery volných radikálů 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
- Názvy látek
- chondroitin sulfáty MeSH
- glukosamin MeSH
OBJECTIVES: Chondroitin sulfate 800 mg/day (CS) pharmaceutical-grade in the management of symptomatic knee osteoarthritis consistent with the European Medicines Agency guideline. METHODS: A prospective, randomised, 6-month, 3-arm, double-blind, double-dummy, placebo and celecoxib (200 mg/day)-controlled trial assessing changes in pain on a Visual Analogue Scale (VAS) and in the Lequesne Index (LI) as coprimary endpoints. Minimal-Clinically Important Improvement (MCII), Patient-Acceptable Symptoms State (PASS) were used as secondary endpoints. RESULTS: 604 patients (knee osteoarthritis) diagnosed according to American College of Rheumalogy (ACR) criteria, recruited in five European countries and followed for 182 days. CS and celecoxib showed a greater significant reduction in pain and LI than placebo. In the intention-to-treat (ITT) population, pain reduction in VAS at day 182 in the CS group (-42.6 mm) and in celecoxib group (-39.5 mm) was significantly greater than the placebo group (-33.3 mm) (p=0.001 for CS and p=0.009 for celecoxib), while no difference observed between CS and celecoxib. Similar trend for the LI, as reduction in this metric in the CS group (-4.7) and celecoxib group (-4.6) was significantly greater than the placebo group (-3.7) (p=0.023 for CS and p=0.015 for celecoxib), no difference was observed between CS and celecoxib. Both secondary endpoints (MCII and PASS) at day 182 improved significantly in the CS and celecoxib groups. All treatments demonstrated excellent safety profiles. CONCLUSION: A 800 mg/day pharmaceutical-grade CS is superior to placebo and similar to celecoxib in reducing pain and improving function over 6 months in symptomatic knee osteoarthritis (OA) patients. This formulation of CS should be considered a first-line treatment in the medical management of knee OA.
- Klíčová slova
- chondroitin sulfate, function, knee osteoarthritis, pain, treatment,
- MeSH
- artróza kolenních kloubů farmakoterapie patofyziologie MeSH
- celekoxib terapeutické užití MeSH
- chondroitin sulfáty terapeutické užití MeSH
- dvojitá slepá metoda MeSH
- inhibitory cyklooxygenasy 2 terapeutické užití MeSH
- lidé středního věku MeSH
- lidé MeSH
- měření bolesti MeSH
- senioři MeSH
- výsledek terapie MeSH
- Check Tag
- lidé středního věku MeSH
- lidé MeSH
- mužské pohlaví MeSH
- senioři MeSH
- ženské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
- multicentrická studie MeSH
- randomizované kontrolované studie MeSH
- Názvy látek
- celekoxib MeSH
- chondroitin sulfáty MeSH
- inhibitory cyklooxygenasy 2 MeSH
INTRODUCTION: In a previously published randomised, placebo-controlled trial, 800 mg/day of pharmaceutical-grade chondroitin sulfate (CS) was shown to be superior to placebo in reducing pain and improving function over 6 months in patients with symptomatic knee osteoarthritis (OA). The aim of the current post hoc analyses was to evaluate the cost-effectiveness of CS compared with placebo in a European perspective using individual patient data from this clinical trial. METHODS: Patients with knee OA randomised to CS or placebo were followed up at 1, 3 and 6 months. The algo-functional Lequesne index was used to derive the EuroQol Five-Dimension Five-Level (EQ-5D-5L) score based on a validated formula. The EQ-5D-5L scores at each time point were used to calculate the changes in quality-adjusted life years (QALYs) with the area under the curve method. Costs were assessed using the average price of CS in the countries where the original study took place and where CS is currently marketed. The costs of CS in three countries were then used (i.e. the Czech Republic, Italy and Switzerland). The incremental cost-effectiveness ratio (ICER) threshold for CS to be considered cost-effective was set at 91,870 EUR per QALY (equivalent to the usually recommended threshold of US $100,000). The study used an intention-to-treat population, i.e. patients who received one dose of the study drug, and imputed missing values using the basal observation carried forward method. RESULTS: No significant differences in baseline characteristics were observed between the CS group (N = 199) and the placebo group (N = 205). The mean cost of CS for 6 months of treatment was 194.74 EUR. After 6 months of treatment, CS showed a mean ICER of 33,462 (95% CI 5130-61,794) EUR per QALY gained, indicating cost-effectiveness compared with placebo. The acceptability curve for cost-effectiveness shows that the CS treatment is likely to be cost-effective compared with placebo, with a 93% probability when the ceiling ratio is set at 91,870 EUR per QALY gained. CONCLUSIONS: These results highlight the role of CS as a cost-effective therapeutic option in the management of OA. However, further studies taking into account the use of other healthcare resources are warranted for a more complete understanding.
- Klíčová slova
- Chondroitin sulfate, Health economics, Osteoarthritis, Quality-adjusted life years,
- MeSH
- analýza nákladové efektivity MeSH
- analýza nákladů a výnosů * MeSH
- artróza kolenních kloubů * farmakoterapie ekonomika MeSH
- chondroitin sulfáty * terapeutické užití ekonomika MeSH
- kvalitativně upravené roky života * MeSH
- lidé středního věku MeSH
- lidé MeSH
- senioři MeSH
- Check Tag
- lidé středního věku MeSH
- lidé MeSH
- mužské pohlaví MeSH
- senioři MeSH
- ženské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
- multicentrická studie MeSH
- randomizované kontrolované studie MeSH
- Geografické názvy
- Česká republika MeSH
- Itálie MeSH
- Švýcarsko MeSH
- Názvy látek
- chondroitin sulfáty * MeSH
Polysaccharides like hyaluronan (HA) and chondroitin sulfate (CS) are native of the brain's extracellular matrix crucial for myelination and brain maturation. Despite extensive research on HA and CS as drug delivery systems (DDS), their high water solubility limits their application as drug carriers. This study introduces an injectable DDS using aldehyde-modified hyaluronic acid (HAOX) hydrogel containing polyelectrolyte complexes (PEC) formed with calcium, gelatin, and either CS or aldehyde-modified CS (CSOX) to deliver minocycline for Multiple Sclerosis therapy. PECs with CSOX enable covalent crosslinking to HAOX, creating immobilized PECs (HAOX_PECOX), while those with CS remain unbound (HAOX_PECS). The in situ forming DDS can be administered via a 20 G needle, with rapid gelation preventing premature leakage. The system integrates into an implanted device for minocycline release through either Fickian or anomalous diffusion, depending on PEC immobilization. HAOX_PECOX reduced burst release by 88 %, with a duration of 127 h for 50 % release. The DDS exhibited an elastic modulus of 3800 Pa and a low swelling ratio (0-1 %), enabling precise control of minocycline release kinetics. Released minocycline reduced IL-6 secretion in the Whole Blood Monocytes Activation Test, suggesting that DDS formation may not alter the biological activity of the loaded drug.
- Klíčová slova
- Chondroitin sulphate, Hyaluronic acid, Hydrogel, Minocycline, Polyelectrolyte complexes,
- MeSH
- aldehydy chemie MeSH
- chondroitin sulfáty * chemie MeSH
- hydrogely * chemie farmakologie MeSH
- interleukin-6 metabolismus MeSH
- kyselina hyaluronová * chemie MeSH
- lidé MeSH
- minocyklin * chemie farmakologie aplikace a dávkování MeSH
- nosiče léků * chemie MeSH
- polyelektrolyty * chemie MeSH
- systémy cílené aplikace léků metody MeSH
- uvolňování léčiv MeSH
- želatina * chemie MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- aldehydy MeSH
- chondroitin sulfáty * MeSH
- hydrogely * MeSH
- interleukin-6 MeSH
- kyselina hyaluronová * MeSH
- minocyklin * MeSH
- nosiče léků * MeSH
- polyelektrolyty * MeSH
- želatina * MeSH
To investigate that a 6-month treatment with avocado soybean unsaponifiable (Piascledine 300 mg) once daily is as effective as with chondroitin sulfate 400 mg three times daily in femorotibial gonarthrosis, and also the carry-over effect for two more months is comparable. Patients were randomized (1:1) to the treatment groups. They received for 6 months 3 capsules chondroitin sulfate per day or one capsule of avocado soybean unsaponifiable (ASU) in a double-dummy technique. A 2-month post-treatment period followed to determine the carry-over effect. Primary efficacy criterion was the change of the WOMAC-index from study begin to end of treatment. Secondary criteria were the changes in Lequesne-index, pain on active movement and at rest, global assessment of efficacy. Three hundred sixty-four patients have been taken up into the trial. Three hundred sixty one patients were eligible for evaluation. One hundred eighty three received ASU 300 mg once daily, one hundred seventy eight chondroitin sulfate three times daily. The WOMAC-index decreased in both groups for approx. 50% to the end of therapy. During the post-treatment observation there was a further slight improvement. There was no statistical significant difference between the treatment groups during the entire observation. All other observed parameters showed the same pattern. The daily intake of rescue medication was reduced continuously. Overall efficacy has been rated excellent and good in more than 80% of the patients in both groups. Both drugs were safe and well tolerated. The first direct comparison between avocado soybean unsaponifiable 300 mg once daily and chondroitin sulfate three times daily reveiled no difference in efficacy or safety aspects between 1 capsule ASU 300 mg per day and 3 capsules chondroitin sulfate per day. It can be assumed that the once daily intake of ASU will lead to a better compliance in routine therapy.
- MeSH
- adherence pacienta MeSH
- artróza kolenních kloubů farmakoterapie MeSH
- chondroitin sulfáty škodlivé účinky terapeutické užití MeSH
- dvojitá slepá metoda MeSH
- fixní kombinace léků MeSH
- fytosteroly škodlivé účinky terapeutické užití MeSH
- lidé středního věku MeSH
- lidé MeSH
- prospektivní studie MeSH
- rostlinné extrakty škodlivé účinky terapeutické užití MeSH
- rozvrh dávkování léků MeSH
- senioři MeSH
- stupeň závažnosti nemoci MeSH
- vitamin E škodlivé účinky terapeutické užití MeSH
- výsledek terapie MeSH
- Check Tag
- lidé středního věku MeSH
- lidé MeSH
- mužské pohlaví MeSH
- senioři MeSH
- ženské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
- multicentrická studie MeSH
- práce podpořená grantem MeSH
- randomizované kontrolované studie MeSH
- srovnávací studie MeSH
- Názvy látek
- chondroitin sulfáty MeSH
- fixní kombinace léků MeSH
- fytosteroly MeSH
- piascledine MeSH Prohlížeč
- rostlinné extrakty MeSH
- vitamin E 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 collagen-coated 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 chemie farmakologie MeSH
- buněčné inženýrství metody MeSH
- buněčné linie MeSH
- chondroitin sulfáty chemie farmakologie MeSH
- kolagen typu I chemie farmakologie MeSH
- kopolymer kyseliny glykolové a mléčné MeSH
- kultivované buňky MeSH
- kyselina mléčná chemie MeSH
- kyselina polyglykolová chemie MeSH
- lidé MeSH
- osteoblasty cytologie účinky léků fyziologie MeSH
- osteogeneze účinky léků fyziologie MeSH
- proliferace buněk účinky léků MeSH
- testování materiálů MeSH
- tkáňové podpůrné struktury MeSH
- viabilita buněk účinky léků MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- biokompatibilní potahované materiály MeSH
- chondroitin sulfáty MeSH
- kolagen typu I MeSH
- kopolymer kyseliny glykolové a mléčné MeSH
- kyselina mléčná MeSH
- kyselina polyglykolová MeSH
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.
- Klíčová slova
- Chondrointin derivatives, malaria, molecular docking, molecular dynamics,
- 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
- Názvy látek
- antigeny protozoální MeSH
- chondroitin sulfáty MeSH
- fosfáty MeSH
- glykosaminoglykany MeSH
- membránové proteiny MeSH
- protozoální proteiny MeSH
- sírany MeSH