Original Article Yonsei Med J 2016 Mar;57(2):321-327 http://dx.doi.org/10.3349/ymj.2016.57.2.321
pISSN: 0513-5796 · eISSN: 1976-2437
Darapladib, a Lipoprotein-Associated Phospholipase A2 Inhibitor, Reduces Rho Kinase Activity in Atherosclerosis Juan Zhang1*, Dong-Ling Xu1*, Xiao-Bo Liu2, Shao-jie Bi1, Tong Zhao1, Shu-Jian Sui1, Xiao-Ping Ji3, and Qing-Hua Lu1 Department of Cardiology, The Second Hospital of Shandong University, Jinan, Shandong Province; Shandong Blood Center, Jinan, Shandong Province; 3 The Key Laboratory of Cardiovascular Remodeling and Function Research of the Chinese Ministry of Education and Public Health, Shandong University Qilu Hospital, Jinan, Shandong Province, China. 1 2
Purpose: Increased lipoprotein-associated phospholipase A2 (Lp-PLA2) activity and Rho kinase activity may be associated with atherosclerosis. The principal aim of this study was to examine whether darapladib (a selective Lp-PLA2 inhibitor) could reduce the elevated Lp-PLA2 and Rho kinase activity in atherosclerosis. Materials and Methods: Studies were performed in male Sprague-Dawley rats. The atherosclerosis rats were prepared by feeding them with a high-cholesterol diet for 10 weeks. Low-dose darapladib (25 mg·kg-1·d-1) and high-dose darapladib (50 mg·kg-1·d-1) interventions were then administered over the course of 2 weeks. Results: The serum levels of triglycerides, total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), high-sensitivity C-reactive protein (hs-CRP), and Lp-PLA2, significantly increased in atherosclerosis model groups, as did Rho kinase activity and cardiomyocyte apoptosis (p
pISSN: 0513-5796 · eISSN: 1976-2437
Darapladib, a Lipoprotein-Associated Phospholipase A2 Inhibitor, Reduces Rho Kinase Activity in Atherosclerosis Juan Zhang1*, Dong-Ling Xu1*, Xiao-Bo Liu2, Shao-jie Bi1, Tong Zhao1, Shu-Jian Sui1, Xiao-Ping Ji3, and Qing-Hua Lu1 Department of Cardiology, The Second Hospital of Shandong University, Jinan, Shandong Province; Shandong Blood Center, Jinan, Shandong Province; 3 The Key Laboratory of Cardiovascular Remodeling and Function Research of the Chinese Ministry of Education and Public Health, Shandong University Qilu Hospital, Jinan, Shandong Province, China. 1 2
Purpose: Increased lipoprotein-associated phospholipase A2 (Lp-PLA2) activity and Rho kinase activity may be associated with atherosclerosis. The principal aim of this study was to examine whether darapladib (a selective Lp-PLA2 inhibitor) could reduce the elevated Lp-PLA2 and Rho kinase activity in atherosclerosis. Materials and Methods: Studies were performed in male Sprague-Dawley rats. The atherosclerosis rats were prepared by feeding them with a high-cholesterol diet for 10 weeks. Low-dose darapladib (25 mg·kg-1·d-1) and high-dose darapladib (50 mg·kg-1·d-1) interventions were then administered over the course of 2 weeks. Results: The serum levels of triglycerides, total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), high-sensitivity C-reactive protein (hs-CRP), and Lp-PLA2, significantly increased in atherosclerosis model groups, as did Rho kinase activity and cardiomyocyte apoptosis (p
