Walley Keith R, Thain Katherine R, Russell James A, Reilly Muredach P, Meyer Nuala J, Ferguson Jane F, Christie Jason D, Nakada Taka-aki, Fjell Chris D, Thair Simone A, Cirstea Mihai S, Boyd John H
Centre for Heart Lung Innovation, University of British Columbia, Vancouver V6Z 1Y6, Canada.
Cardiovascular Institute, University of Pennsylvania Perelman School of Medicine, Philadelphia, PA 19104, USA.
Sci Transl Med. 2014 Oct 15;6(258):258ra143. doi: 10.1126/scitranslmed.3008782.
A decrease in the activity of proprotein convertase subtilisin/kexin type 9 (PCSK9) increases the amount of low-density lipoprotein (LDL) receptors on liver cells and, therefore, LDL clearance. The clearance of lipids from pathogens is related to endogenous lipid clearance; thus, PCSK9 may also regulate removal of pathogen lipids such as lipopolysaccharide (LPS). Compared to controls, Pcsk9 knockout mice displayed decreases in inflammatory cytokine production and in other physiological responses to LPS. In human liver cells, PCSK9 inhibited LPS uptake, a necessary step in systemic clearance and detoxification. Pharmacological inhibition of PCSK9 improved survival and inflammation in murine polymicrobial peritonitis. Human PCSK9 loss-of-function genetic variants were associated with improved survival in septic shock patients and a decrease in inflammatory cytokine response both in septic shock patients and in healthy volunteers after LPS administration. The PCSK9 effect was abrogated in LDL receptor (LDLR) knockout mice and in humans who are homozygous for an LDLR variant that is resistant to PCSK9. Together, our results show that reduced PCSK9 function is associated with increased pathogen lipid clearance via the LDLR, a decreased inflammatory response, and improved septic shock outcome.
前蛋白转化酶枯草溶菌素/克新9型(PCSK9)活性降低会增加肝细胞上低密度脂蛋白(LDL)受体的数量,从而增加LDL清除率。病原体脂质的清除与内源性脂质清除有关;因此,PCSK9也可能调节病原体脂质如脂多糖(LPS)的清除。与对照组相比,Pcsk9基因敲除小鼠的炎症细胞因子产生以及对LPS的其他生理反应均有所降低。在人肝细胞中,PCSK9抑制LPS摄取,这是全身清除和解毒的必要步骤。PCSK9的药理学抑制作用改善了小鼠多微生物性腹膜炎的存活率并减轻了炎症。人PCSK9功能丧失的基因变异与感染性休克患者存活率提高以及感染性休克患者和LPS给药后健康志愿者炎症细胞因子反应降低有关。在LDL受体(LDLR)基因敲除小鼠和对PCSK9有抗性的LDLR变异纯合子人类中,PCSK9的作用被消除。总之,我们的结果表明,PCSK9功能降低与通过LDLR增加病原体脂质清除、炎症反应降低以及感染性休克结局改善有关。