Darapladib, a Lipoprotein-Associated Phospholipase A2 Inhibitor, Reduces Rho Kinase Activity in Atherosclerosis
Yonsei Medical Journal
;
: 321-327, 2016.
Article
in English
| WPRIM
| ID: wpr-147359
ABSTRACT
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 ANDMETHODS:
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 (p0.05).CONCLUSION:
Darapladib, a Lp-PLA2 inhibitor, leads to cardiovascular protection that might be mediated by its inhibition of both Rho kinase and Lp-PLA2 in atherosclerosis.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Oximes
/
Triglycerides
/
Benzaldehydes
/
C-Reactive Protein
/
Cholesterol
/
Rats, Sprague-Dawley
/
1-Alkyl-2-acetylglycerophosphocholine Esterase
/
Dose-Response Relationship, Drug
/
Atherosclerosis
/
Rho-Associated Kinases
Type of study:
Prognostic study
Limits:
Animals
Language:
English
Journal:
Yonsei Medical Journal
Year:
2016
Type:
Article
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