Ito Takayuki, Ikeda Uichi, Shimpo Masahisa, Ohki Ruri, Takahashi Masafumi, Yamamoto Keiji, Shimada Kazuyuki
Division of Cardiovascular Medicine, Department of Medicine, Jichi Medical School, Tochigi, Japan.
Cardiovasc Drugs Ther. 2002 Mar;16(2):121-6. doi: 10.1023/a:1015701415588.
Interleukin-6 (IL-6) is a key molecule in chronic inflammation and has been implicated in the progression of atherosclerosis. HMG-CoA reductase inhibitors (statins) may reduce the cardiovascular risk and vulnerability of atherosclerotic plaque through nonlipid as well as lipid-lowering mechanisms, but their anti-inflammatory effects on the vascular tissue have not been fully elucidated. We investigated the effects of fluvastatin on IL-6 synthesis in human vascular smooth muscle cells (VSMCs). Addition of fluvastatin decreased IL-6 synthesis in VSMCs in a time (0-24 hours)- and dose (10(-8)-10(-5) mol/L)-dependent manner. Fluvastatin also decreased IL-6 mRNA expression in VSMCs. The effects of fluvastatin on IL-6 expression were completely reversed in the presence of mevalonate or geranylgeranyl-pyrophosphate, but not squalene. Inhibition of Rho by C3 exoenzyme or Rho kinase by Y-27632 significantly decreased IL-6 expression in VSMCs. In conclusion, fluvastatin decreases IL-6 synthesis in human VSMCs through inhibition of Rho pathway. These findings suggested that reduction of IL-6 expression by statins may partially explain their therapeutic effects in patients with coronary artery disease.
白细胞介素-6(IL-6)是慢性炎症中的关键分子,与动脉粥样硬化的进展有关。羟甲基戊二酸单酰辅酶A还原酶抑制剂(他汀类药物)可通过非降脂以及降脂机制降低心血管风险和动脉粥样硬化斑块的易损性,但其对血管组织的抗炎作用尚未完全阐明。我们研究了氟伐他汀对人血管平滑肌细胞(VSMCs)中IL-6合成的影响。添加氟伐他汀以时间(0 - 24小时)和剂量(10^(-8) - 10^(-5) mol/L)依赖性方式降低VSMCs中IL-6的合成。氟伐他汀还降低了VSMCs中IL-6 mRNA的表达。在甲羟戊酸或香叶基香叶基焦磷酸存在下,氟伐他汀对IL-6表达的影响完全逆转,但在鲨烯存在下则不然。C3外切酶抑制Rho或Y-27632抑制Rho激酶可显著降低VSMCs中IL-6的表达。总之,氟伐他汀通过抑制Rho途径降低人VSMCs中IL-6的合成。这些发现表明,他汀类药物降低IL-6表达可能部分解释了它们对冠心病患者的治疗作用。