Division of Biochemical and Musculoskeletal Medicine, Section of Human Metabolism and Clinical Biochemistry, University of Sheffield Medical School, S10 2RX, Sheffield, UK.
Inflammopharmacology. 1999;7(4):387-400. doi: 10.1007/s10787-999-0032-x.
Suramin is an anti-neoplastic drug. Its actions include the inhibition of binding of urokinase-type plasminogen activator (uPA) to its receptor, an event which may prevent cartilage breakdown. The aim of this work was to determine the effect of suramin on cartilage resorption. Cartilage expiants, stimulated with interleukin-1alpha, tumour necrosis factor-alpha or retinoic acid were incubated with suramin. Release of incorporated (35)S-sulphate from pre-labelled expiants was used as a measure of proteoglycan breakdown and toluidine blue staining was used to visualise proteoglycan loss.Suramin inhibited the resorption of cytokine and retinoic acid-stimulated bovine nasal cartilage at concentrations between 100-1000 microM. These findings were confirmed by histochemistry. Though reversibility studies indicated that suramin toxicity could not be excluded above 100 muM, retention of suramin in the expiants may have contributed to this. There was no significant effect on lactate production up to 500 muM. The observed inhibition of cartilage resorption may reflect actions of suramin on the PA/plasmin system or on cytokine action.
苏拉明是一种抗肿瘤药物。其作用包括抑制尿激酶型纤溶酶原激活物（uPA）与其受体的结合，这一事件可能阻止软骨分解。本工作旨在确定苏拉明对软骨吸收的影响。用白细胞介素-1α、肿瘤坏死因子-α或维甲酸刺激的软骨外植体与苏拉明孵育。用掺入的（35）S-硫酸盐从预先标记的外植体中释放来测量蛋白聚糖的分解，并用甲苯胺蓝染色来观察蛋白聚糖的损失。苏拉明抑制浓度在 100-1000μM 之间的细胞因子和维甲酸刺激的牛鼻软骨的吸收。组织化学证实了这一发现。虽然可逆性研究表明，苏拉明的毒性不能排除在 100μM 以上，但外植体中苏拉明的保留可能对此有贡献。在 500μM 以下，对乳酸生成没有显著影响。观察到的软骨吸收抑制可能反映了苏拉明对 PA/纤溶系统或细胞因子作用的作用。
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