Effects of some nonsteroidal antiinflammatory drugs on proteoglycan metabolism and organization in canine articular cartilage.
Effects of some nonsteroidal antiinflammatory drugs on proteoglycan metabolism and organization in canine articular cartilage.
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一些非甾体抗炎药对犬关节软骨蛋白多糖代谢和组织的影响。
DOI：
10.1002/art.1780230908
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发表时间：
1980
影响因子：
--
通讯作者：
Brandt,KD
中科院分区：
文献类型：
--
作者：
Palmoski,MJ;Brandt,KD
在正常犬关节软骨培养上观察了几种治疗关节炎常用的非甾体抗炎药对蛋白多糖代谢和聚集的影响。非诺洛芬和布洛芬以浓度依赖的方式抑制净蛋白多糖的合成。在培养液中的浓度与患者口服给药后的血浆浓度相当时，在这些药物存在的情况下，净原多糖合成分别平均为控制值的72%和86%(P<；0.01)。相反，吲哚美辛和舒林酸亚砜对蛋白多糖的合成没有影响，而舒林酸硫化物以非浓度依赖的方式刺激蛋白多糖的合成(平均为13%)。在布洛芬或舒林酸硫化物存在下，硫酸氨基葡聚糖的分解代谢与对照组相同，而非诺洛芬则略有降低。布洛芬、消炎痛、硫化舒林酸或亚硫化舒林酸均不影响新合成的聚合态蛋白多糖的比例和降解蛋白多糖的平均流体力学尺寸。另一方面，非诺洛芬干扰了软骨透明质酸与蛋白多糖相互作用形成聚集体的能力，而它对蛋白多糖与脐带透明质酸的体外结合没有影响。
The effects on proteoglycan metabolism and aggregation of several nonsteroidal antiinflammatory drugs commonly used in the treatment of arthritis were examined in cultures of normal canine articular cartilage. Fenoprofen and ibuprofen inhibited net proteoglycan synthesis in a concentration‐dependent fashion. At concentrations in the culture medium comparable to plasma concentrations seen in patients after oral administration in humans, net protcoglycan synthesis in the presence of these drugs averaged 72% and 86% of the control values, respectively (P< 0.01). In contrast, indomethacin and sulindac sulfoxide had no effect on proteoglycan synthesis, while sulindac sulfide stimulated synthesis in a non‐concentration dependent fashion (average, 13%). In the presence of ibuprofen or sulindac sulfide, catabolism of sulfated glycosaminoglycans was the same as that in control cartilage, while fenoprofen decreased the rate of degradation slightly. The proportion of newly synthesized proteoglycans existing as aggregates and the average hydrodynamic size of disaggregated proteoglycans were unaffected by ibuprofen, indomethacin, sulindac sulfide, or sulindac sulfoxide. Fenoprofen, on the other hand, interfered with the ability of the cartilage hyaluronic acid to interact with proteoglycans to form aggregates, whereas it has no effect on the in vitro association of proteoglycans with hyaluronic acid from umbilical cord.