Atherosclerosis 191 (2007) 54–62 Role of lipoprotein-associated phospholipase A 2 in leukocyte activation and inflammatory responses Yi Shi a, , Ping Zhang a , LiFeng Zhang a , Hashim Osman b , Emile R. Mohler III b , Colin Macphee c , Andrew Zalewski a,c , Anthony Postle d , Robert L. Wilensky b a Thomas Jefferson University, Philadelphia, PA, United States b University of Pennsylvania, Philadelphia, PA, United States c GlaxoSmithKline Pharmaceuticals, King of Prussia, PA, United States d University of Southampton, UK Received 21 November 2005; received in revised form 4 April 2006; accepted 1 May 2006 Available online 9 June 2006 Abstract Background: Lipoprotein-associated phospholipase A 2 (Lp-PLA 2 ) is an emerging cardiovascular risk marker. To explore the biologic role of Lp-PLA 2 in atherosclerosis, we examined its expression and contribution to leukocyte activation under proatherogenic conditions. Methods and results: Following the induction of diabetes and hypercholesterolemia in a porcine model, a rapid increase in plasma Lp-PLA 2 activity was observed at 1 month. This was accompanied by upregulated Lp-PLA 2 mRNA expression by peripheral blood mononuclear cells (PBMC) at 3 months, and elevated Lp-PLA 2 mRNA expression in coronary arteries at 6 months. These changes were paralleled by increased inflammatory responses by circulating PBMC (ICAM-1, IL-6), in coronary tissues (ICAM-1, VCAM-1), and the subsequent accumulation of inflammatory cells. In human PBMC, proinflammatory mediators augmented the synthesis and release of functional Lp-PLA 2 . Furthermore, lysophosphatidylcholine (lysoPC), a product of Lp-PLA 2 activity, induced an increase in several inflammatory cytokines (IL-1, IL-6, TNF-) in a concentration-dependent manner. In contrast, Lp-PLA 2 inhibition (SB677116; 1 M) abrogated the inflammatory response elicited by oxidized LDL. Conclusions: In an experimental model of diabetes and hypercholesterolemia, leukocyte activation was associated with augmented Lp-PLA 2 expression. In vitro, Lp-PLA 2 activity mediated leukocyte activation and inflammatory responses, whereas Lp-PLA 2 inhibition abolished inflammatory responses induced by oxidized LDL. Collectively, these observations support a proatherogenic role for Lp-PLA 2 . © 2006 Elsevier Ireland Ltd. All rights reserved. Keywords: Atherosclerosis; Hypercholesterolemia; Diabetes; Inflammation; Lipoprotein-associated phospholipase A 2 1. Introduction Lipoprotein-associated phospholipase A 2 (Lp-PLA 2 ), also known as platelet activating factor acetylhydrolase, belongs to the large family of phospholipases that liberate bioactive molecules through the hydrolysis of a wide range of phospholipids [1]. Lp-PLA 2 is unique among members of phospholipase A 2 superfamily due to its origin (secreted from Correspondence to: Department of Surgery, Thomas Jefferson Univer- sity, Suite 623, 1025 Walnut Street, Philadelphia, PA 19107, United States. Tel.: +1 215 955 2693; fax: +1 215 955 2878. E-mail address: yi.shi@jefferson.edu (Y. Shi). bone marrow-derived cells, mainly leukocytes), its associa- tion with circulating lipoproteins, and its substrate preference for polar phospholipids including those generated during the oxidation of LDL [2]. Several studies have demonstrated higher levels of circulating Lp-PLA 2 (mass or activity) in individuals who subsequently develop cardiovascular events [3–8]. In most studies, Lp-PLA 2 remained an independent predictor of future events even after adjustment for several conventional risk factors. Furthermore, higher levels of circu- lating Lp-PLA 2 appear to be associated with atherosclerotic burden, as assessed by extent of coronary artery calcifications or the angiographic extent of coronary artery disease [9,10]. Although the emerging epidemiologic data provide evidence 0021-9150/$ – see front matter © 2006 Elsevier Ireland Ltd. All rights reserved. doi:10.1016/j.atherosclerosis.2006.05.001