INSERM U1132, Hôpital Lariboisière, Paris, France.
Rheumatology Department, University Paris Diderot, Hôpital Lariboisière, Paris, France.
Ann Rheum Dis. 2017 Apr;76(4):748-755. doi: 10.1136/annrheumdis-2016-209757. Epub 2016 Oct 27.
To investigate the impact of systemic inhibition of interleukin 6 (IL-6) or signal transducer and activator of transcription (Stat3) in an experimental model of osteoarthritis (OA).
Expression of major catabolic and anabolic factors of cartilage was determined in IL-6-treated mouse chondrocytes and cartilage explants. The anti-IL-6-receptor neutralising antibody MR16-1 was used in the destabilisation of the medial meniscus (DMM) mouse model of OA. Stat3 blockade was investigated by the small molecule Stattic ex vivo and in the DMM model.
In chondrocytes and cartilage explants, IL-6 treatment reduced proteoglycan content with increased production of matrix metalloproteinase (MMP-3 and MMP-13) and a disintegrin and metalloproteinase with thrombospondin motifs (ADAMTS-4 and ADAMTS-5). IL-6 induced Stat3 and extracellular signal-regulated kinase (ERK) 1/2 signalling but not p38, c-Jun N-terminal kinase or Akt. In the DMM model, Stat3 was activated in cartilage, but neither in the synovium nor in the subchondral bone. Systemic blockade of IL-6 by MR16-1 alleviated DMM-induced OA cartilage lesions, impaired the osteophyte formation and the extent of synovitis. In the same model, Stattic had similar beneficial effects on cartilage and osteophyte formation. Stattic, but not an ERK1/2 inhibitor, significantly counteracted the catabolic effects of IL-6 on cartilage explants and suppressed the IL-6-induced chondrocytes apoptosis.
IL-6 induces chondrocyte catabolism mainly via Stat3 signalling, a pathway activated in cartilage from joint subjected to DMM. Systemic blockade of IL-6 or STAT-3 can alleviate DMM-induced OA in mice.
研究在骨关节炎(OA)的实验模型中,全身性抑制白细胞介素 6(IL-6)或信号转导和转录激活因子 3(Stat3)的影响。
在 IL-6 处理的小鼠软骨细胞和软骨外植体中确定软骨主要分解代谢和合成代谢因子的表达。在 OA 的内侧半月板不稳定(DMM)小鼠模型中使用抗 IL-6 受体中和抗体 MR16-1。通过小分子 Stattic 进行体外和 DMM 模型中的 Stat3 阻断研究。
在软骨细胞和软骨外植体中,IL-6 处理降低了蛋白聚糖含量,同时增加了基质金属蛋白酶(MMP-3 和 MMP-13)和具有解整合素和金属蛋白酶基序的金属蛋白酶(ADAMTS-4 和 ADAMTS-5)的产生。IL-6 诱导 Stat3 和细胞外信号调节激酶(ERK)1/2 信号,但不诱导 p38、c-Jun N-末端激酶或 Akt。在 DMM 模型中,Stat3 在软骨中被激活,但在滑膜中和软骨下骨中均未被激活。MR16-1 对 IL-6 的全身性阻断通过减轻 DMM 诱导的 OA 软骨病变、损害骨赘形成和滑膜炎程度来缓解 DMM 诱导的 OA。在相同的模型中,Stattic 对软骨和骨赘形成具有类似的有益作用。Stattic,但不是 ERK1/2 抑制剂,显著抵消了 IL-6 对软骨外植体的分解代谢作用,并抑制了 IL-6 诱导的软骨细胞凋亡。
IL-6 主要通过 Stat3 信号通路诱导软骨细胞分解代谢,该通路在 DMM 处理的关节软骨中被激活。全身性阻断 IL-6 或 STAT-3 可以减轻 DMM 诱导的小鼠 OA。