Davies S R, Cole A A, Schmid T M
Department of Biochemistry, Rush Medical College, Rush-Presbyterian St. Luke's Medical Center, Chicago, Illinois 60612, USA.
J Biol Chem. 1996 Oct 18;271(42):25966-70. doi: 10.1074/jbc.271.42.25966.
Doxycycline, a member of the tetracycline family, has been shown to reduce a type X collagen epitope as detected by immunohistochemistry with a monoclonal antibody in an avian explant culture system (). It was also shown to decrease collagenase and gelatinase activities and thus matrix degradation. This study investigates the effect of doxycycline on type X collagen synthesis in monolayer cultures of hypertrophic chondrocytes. Protein synthesis was evaluated by radioisotopic labeling during doxycycline, tetracycline, or minocycline treatment. Radiolabeled proteins were analyzed by gel electrophoresis, and total collagen was quantitated by hydroxyproline analysis. Additionally, the synthesis of type X collagen was measured by immunoprecipitation. Doxycycline was found to inhibit type X production more effectively than either of the other tetracyclines at comparable dose levels. Furthermore, type X collagen was inhibited more than other collagens, non-collagenous proteins and proteoglycans, with maximal inhibition at 80 microg/ml and an IC50 of 7 microg/ml. This inhibition by doxycycline was specific for type X collagen at 10 microg/ml, and the pattern was distinct from cycloheximide, a recognized inhibitor of protein translation. This suppression of type X collagen could not be overcome by excess extracellular calcium, conditions that have been demonstrated to induce synthesis of this protein (2).
强力霉素是四环素家族的一员,在鸟类外植体培养系统中,通过单克隆抗体免疫组化检测发现,它能减少X型胶原表位()。研究还表明,它能降低胶原酶和明胶酶的活性,从而减少基质降解。本研究探讨强力霉素对肥大软骨细胞单层培养中X型胶原合成的影响。在强力霉素、四环素或米诺环素处理过程中,通过放射性同位素标记评估蛋白质合成。通过凝胶电泳分析放射性标记的蛋白质,通过羟脯氨酸分析对总胶原进行定量。此外,通过免疫沉淀法测定X型胶原的合成。结果发现,在相当的剂量水平下,强力霉素比其他任何一种四环素更有效地抑制X型胶原的产生。此外,与其他胶原、非胶原蛋白质和蛋白聚糖相比,X型胶原受到的抑制作用更强,在80微克/毫升时达到最大抑制,半数抑制浓度(IC50)为7微克/毫升。在10微克/毫升时,强力霉素对X型胶原的这种抑制具有特异性,其模式与公认的蛋白质翻译抑制剂环己酰亚胺不同。过量的细胞外钙无法克服这种对X型胶原的抑制作用,而细胞外钙已被证明能诱导该蛋白的合成(2)。