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1.
Bioorg Chem ; 57: 99-107, 2014 Dec.
Article in English | MEDLINE | ID: mdl-25305720

ABSTRACT

Chondrocyte based therapy is promising to treat symptomatic chondral and osteochondral lesions. Growth factors to accelerate the proliferation and retain the phenotype of chondrocytes in vitro are imperative. However, the high cost and rapid degradation of growth factors limited their further application. Therefore, it is significant to find substitutes that can preserve chondrocytes phenotype and ensure sufficient cells for cytotherapy. Antioxidant and anti-inflammatory agents or their derivatives that have effect on arthritis may be an alternative. In this study, we synthesized sulfonamido-based gallate - LDQN-C and investigated its effect on rat articular chondrocytes through examination of the cell proliferation, morphology, viability, glycosaminoglycans (GAGs) synthesis and cartilage specific gene expression. Results showed that LDQN-C could enhance secretion and synthesis of cartilage extracellular matrix (ECM) by up-regulating expression levels of aggrecan, collagen II and Sox9 genes compared to the GA treated group and control group. Expression of collagen type II was effectively up-regulated while collagen I was down-regulated, which demonstrated that the inhibition of chondrocytes dedifferentiation by LDQN-C. Range of 1.36×10(-9)M to 1.36×10(-7)M is recommended dose of LDQN-C, among which the most profound response was observed with 1.36×10(-8)M. GA at concentration of 0.125µg/mL was compared. This study might provide a basis for the development of a novel agent for the treatment of articular cartilage defect.


Subject(s)
Chondrocytes/drug effects , Chondrogenesis/drug effects , Gallic Acid/chemistry , Gallic Acid/pharmacology , Sulfonamides/chemistry , Sulfonamides/pharmacology , Animals , Cartilage, Articular/cytology , Cartilage, Articular/drug effects , Cartilage, Articular/physiology , Cell Proliferation/drug effects , Cell Survival/drug effects , Cells, Cultured , Chondrocytes/cytology , Chondrocytes/metabolism , Gallic Acid/chemical synthesis , Rats , Rats, Sprague-Dawley , Sulfonamides/chemical synthesis
2.
Asian Pac J Trop Biomed ; 2(1): 70-5, 2012 Jan.
Article in English | MEDLINE | ID: mdl-23569838

ABSTRACT

OBJECTIVE: To identify more effective and less toxic drugs to treat animal toxoplasmosis. METHODS: Efficacy of seven kinds of sulfonamides against Toxoplasma gondii (T. gondii) in an acute murine model was evaluated. The mice used throughout the study were randomly assigned to many groups (10 mice each), which either remained uninfected or were infected intraperitoneally with tachyzoites of T. gondii (strains RH and CN). All groups were then treated with different sulfonamides and the optimal treatment protocol was determined candidates. Sulfadiazine-sodium (SD) was used for comparison. RESULTS: The optimal therapy involved gavaging mice twice per day with 250 mg/kg bw of sulfachloropyrazine-sodium (SPZ) for five days. Using this protocol, the average survival time and the time-point of 50% fatalities were prolonged significantly compared with SD treatment. Treatment with SPZ protected 40% of mice from death, and the heart and kidney tissue of these animals was parasite-free, as determined by nested-PCR. SPZ showed excellent therapeutic effects in the treatment of T. gondii in an acute murine model and is therefore a promising drug candidate for the treatment and prevention of T. gondii in animals. CONCLUSIONS: It can be concluded that the effective drug sulfachloropyrazine may be the new therapeutic options against animal toxoplasmosis.


Subject(s)
Antiprotozoal Agents/administration & dosage , Sulfanilamides/administration & dosage , Toxoplasma/drug effects , Toxoplasmosis/drug therapy , Administration, Oral , Animals , DNA, Protozoan/analysis , DNA, Protozoan/isolation & purification , Disease Models, Animal , Female , Heart/parasitology , Kidney/parasitology , Mice , Polymerase Chain Reaction , Survival Analysis , Toxoplasma/genetics , Toxoplasma/isolation & purification , Treatment Outcome
3.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-499684

ABSTRACT

Objective: To identify more effective and less toxic drugs to treat animal toxoplasmosis.Methods:Efficacy of seven kinds of sulfonamides against Toxoplasma gondii (T. gondii) in an acute murine model was evaluated. The mice used throughout the study were randomly assigned to many groups (10 mice each), which either remained uninfected or were infected intraperitoneally with tachyzoites of T. gondii (strains RH and CN). All groups were then treated with different sulfonamides and the optimal treatment protocol was determined candidates. Sulfadiazine-sodium (SD) was used for comparison. Results: The optimal therapy involved gavaging mice twice per day with 250 mg/kg bw of sulfachloropyrazine-sodium (SPZ) for five days. Using this protocol, the average survival time and the time-point of 50% fatalities were prolonged significantly compared with SD treatment. Treatment with SPZ protected 40% of mice from death, and the heart and kidney tissue of these animals was parasite-free, as determined by nested-PCR. SPZ showed excellent therapeutic effects in the treatment of T. gondii in an acute murine model and is therefore a promising drug candidate for the treatment and prevention of T. gondii in animals. Conclusions: It can be concluded that the effective drug sulfachloropyrazine may be the new therapeutic options against animal toxoplasmosis.

4.
Article in English | WPRIM (Western Pacific) | ID: wpr-303622

ABSTRACT

<p><b>OBJECTIVE</b>To identify more effective and less toxic drugs to treat animal toxoplasmosis.</p><p><b>METHODS</b>Efficacy of seven kinds of sulfonamides against Toxoplasma gondii (T. gondii) in an acute murine model was evaluated. The mice used throughout the study were randomly assigned to many groups (10 mice each), which either remained uninfected or were infected intraperitoneally with tachyzoites of T. gondii (strains RH and CN). All groups were then treated with different sulfonamides and the optimal treatment protocol was determined candidates. Sulfadiazine-sodium (SD) was used for comparison.</p><p><b>RESULTS</b>The optimal therapy involved gavaging mice twice per day with 250 mg/kg bw of sulfachloropyrazine-sodium (SPZ) for five days. Using this protocol, the average survival time and the time-point of 50% fatalities were prolonged significantly compared with SD treatment. Treatment with SPZ protected 40% of mice from death, and the heart and kidney tissue of these animals was parasite-free, as determined by nested-PCR. SPZ showed excellent therapeutic effects in the treatment of T. gondii in an acute murine model and is therefore a promising drug candidate for the treatment and prevention of T. gondii in animals.</p><p><b>CONCLUSIONS</b>It can be concluded that the effective drug sulfachloropyrazine may be the new therapeutic options against animal toxoplasmosis.</p>


Subject(s)
Animals , Female , Mice , Administration, Oral , Antiprotozoal Agents , DNA, Protozoan , Disease Models, Animal , Heart , Parasitology , Kidney , Parasitology , Polymerase Chain Reaction , Sulfanilamides , Survival Analysis , Toxoplasma , Genetics , Toxoplasmosis , Drug Therapy , Treatment Outcome
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