ONO - 4817，一种口服活性基质金属蛋白酶抑制剂，可防止脂多糖诱导的豚鼠关节软骨蛋白聚糖释放。
ONO-4817, an orally active matrix metalloproteinase inhibitor, prevents lipopolysaccharide-induced proteoglycan release from the joint cartilage in guinea pigs.
作者信息
Yamada A, Uegaki A, Nakamura T, Ogawa K
机构信息
Discovery Research Laboratory II, Minase Research Institute, ONO Pharmaceutical Co., Ltd., Osaka, Japan.
出版信息
Inflamm Res. 2000 Apr;49(4):144-6. doi: 10.1007/s000110050573.
OBJECTIVE AND DESIGN
To evaluate the effect of a newly developed inhibitor of matrix metalloproteinases (MMPs), ONO-4817, on the degradation of cartilage in the guinea pig arthritis model.
MATERIALS
42 guinea pigs were used in the arthritis model.
TREATMENT
Lipopolysaccharide (LPS) was injected into guinea pig knee joints. The content of proteoglycan released in synovial cavity was measured as a marker of cartilage degradation. ONO-4817, dexamethasone or indomethacin were administered orally to the animals.
RESULTS
ONO-4817 showed a broad inhibitory activity against MMPs except MMP-1 and MMP-7. The oral administration of ONO-4817 dose-dependently suppressed the release of proteoglycan from the cartilage of the knee joints.
CONCLUSION
This study suggests the possibility that a novel MMP inhibitor, ONO-4817 may have a therapeutic utility for MMP-related diseases.
目的与设计
评估新开发的基质金属蛋白酶（MMPs）抑制剂ONO - 4817对豚鼠关节炎模型中软骨降解的影响。
材料
42只豚鼠用于关节炎模型。
处理
将脂多糖（LPS）注入豚鼠膝关节。测量滑膜腔中释放的蛋白聚糖含量作为软骨降解的标志物。对动物口服给予ONO - 4817、地塞米松或吲哚美辛。
结果
ONO - 4817对除MMP - 1和MMP - 7之外的MMPs显示出广泛的抑制活性。口服ONO - 4817剂量依赖性地抑制膝关节软骨中蛋白聚糖的释放。
结论
本研究提示新型MMP抑制剂ONO - 4817可能对MMP相关疾病具有治疗作用。
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