Abstract
Background and Purpose: Diabetic nephropathy is one of the most common
complications that is related to high morbidity and mortality in type 2
diabetic patients. We investigated ability of a novel dual modulator,
PTUPB that concurrently acts as a soluble epoxide hydrolase inhibitor
and as a cyclooxygenase-2 inhibitor against diabetic nephropathy.
Experimental Approach: Sixteen-week-old type 2 diabetic and proteinuric
obese ZSF1 rats were orally treated with vehicle, PTUPB, or enalapril
for 8 weeks. Key Results: PTUPB alleviated diabetic nephropathy in obese
ZSF1 rats by reducing albuminuria by 50%, renal tubular cast formation
by 60-70%, renal fibrosis by 40-50%, glomerular injury by 55% and
preserved glomerular nephrin expression. Enalapril demonstrated
comparable effects and alleviated diabetic nephropathy in obese ZSF1
rats by reducing all kidney injury parameters by 30 to 50%. Diabetic
renal injury in obese ZSF1 rats was accompanied by renal inflammation
with 6-7-fold higher urinary MCP-1 level and renal infiltration of CD-68
positive cells. PTUPB and enalapril reduced renal inflammation but PTUPB
demonstrated superior anti-inflammatory actions than enalapril. Obese
ZSF1 rats were also hypertensive, hyperlipidemic, and exhibited liver
injury. Interestingly, PTUPB but not enalapril decreased hyperlipidemia
and liver injury in Obese ZSF1 rats. Conclusion and Implication:
Overall, we demonstrate that a dual modulator PTUPB does not treat
hyperglycemia, but can effectively alleviate hypertension, diabetic
nephropathy, hyperlipidemia, and liver injury in type 2 diabetic rats.
Therefore, we suggest that PTUPB has promising potential to be developed
as a novel therapy for type 2 diabetic nephropathy and other
complications.