Steinetz B G, Lust G
New York University Medical Center Laboratory for Experimental Medicine and Surgery in Primates LEMSIP, Tuxedo.
Agents Actions. 1994 Aug;42(1-2):74-80. doi: 10.1007/BF02014304.
There are similarities between the actions of estrogen and relaxin on the connective tissues of the pubic symphysis and those of neutral proteases on cartilage in osteoarthritis, including cartilage hydration, proteoglycan loss, and dissolution of collagen fibers. We hypothesized that compounds known to inhibit cartilage breakdown in animal models of osteoarthritis, such as polysulfated GAGs, would also antagonize the actions of estrogen and relaxin that increase the laxity and mobility of the pubic symphyses of guinea pigs. Estrogen-primed guinea pigs were injected with relaxin or with relaxin and the test compound. The pubic symphyses were manually palpated 6 h later and the degree of mobility scored. Glycosaminoglycan polysulfates and pentosan polysulfate inhibited relaxin-induced pubic symphyseal relaxation, whereas other types of agents were without effect. The guinea pig pubic symphysis assay for relaxin may thus provide a novel rapid screening test for compounds with potential chondroprotective activity.
雌激素和松弛素对耻骨联合结缔组织的作用，与中性蛋白酶对骨关节炎中软骨的作用存在相似之处，包括软骨水合作用、蛋白聚糖损失以及胶原纤维溶解。我们推测，已知在骨关节炎动物模型中能抑制软骨破坏的化合物，如多硫酸化糖胺聚糖，也会拮抗雌激素和松弛素增加豚鼠耻骨联合松弛度和活动度的作用。用雌激素预处理的豚鼠注射松弛素或松弛素与受试化合物。6小时后手动触诊耻骨联合并对活动度进行评分。多硫酸化糖胺聚糖和聚硫酸戊聚糖可抑制松弛素诱导的耻骨联合松弛，而其他类型的药物则无此作用。因此，用于检测松弛素的豚鼠耻骨联合试验可能为具有潜在软骨保护活性的化合物提供一种新型快速筛选试验。
