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Evaluation of the potassium channel activator levcromakalim (BRL38227) on the lipid profile, electrolytes and blood glucose levels of streptozotocin-diabetic rats ((BRL38227)-、).
MedLine Citation:
PMID:  23374501     Owner:  NLM     Status:  In-Data-Review    
BACKGROUND: Levcromakalim is a vasorelaxant used in the management of hypertension in diabetes mellitus. Thus, the effects of levcromakalim were investigated in streptozotocin (STZ)-diabetic rats.
METHODS: Diabetes was induced in Wistar albino rats with a single injection of STZ (60 mg/kg, i.p.) following chronic (4 weeks) treatment with levcromakalim (75 μg/kg per day). Rats were then divided into the following groups (n = 5 in each group): (i) a normal saline (2 mL/kg)-treated group; (ii) a 5 mg/kg glibenclamide-treated group; (iii) 350 mg/kg metformin-treated group; and (iv) 5, 10, 20 and 40 IU/kg insulin-treated groups. Rats were transferred to metabolic cages and the lipid profile, plasma and urine electrolytes and blood glucose levels were determined 24 h after drug administration.
RESULTS: Levcromakalim treatment significantly reduced total cholesterol, low-density lipoprotein (LDL), and triglyceride levels in diabetic rats (all P < 0.05 compared with untreated diabetic rats). In addition, levcromakalim reduced plasma sodium, bicarbonate, and chloride levels, but increased urinary bicarbonate and chloride levels, in diabetic rats (all P < 0.05 compared with untreated diabetic rats). Levcromakalim significantly inhibited the effects of glibenclamide, metformin, and low-dose (20 IU/kg) insulin treatment in diabetic rats (all P < 0.05). Only 40 IU/kg insulin produced significant reductions in hyperglycemia in levcromakalim-treated diabetic rats.
CONCLUSION: Levcromakalim induced resistance to glibenclamide, metformin, and low-dose insulin treatment in diabetic rats, leading to persistent hyperglycemia. However, reductions in LDL, total cholesterol and triglyceride levels following chronic levcromokalim treatment may decrease the risk of cardiovascular disease in diabetic rats.
Omonkhelin J Owolabi; Eric K I Omogbai
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of diabetes     Volume:  5     ISSN:  1753-0407     ISO Abbreviation:  J Diabetes     Publication Date:  2013 Mar 
Date Detail:
Created Date:  2013-02-05     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101504326     Medline TA:  J Diabetes     Country:  Australia    
Other Details:
Languages:  eng     Pagination:  88-94     Citation Subset:  IM    
Copyright Information:
© 2012 Ruijin Hospital, Shanghai Jiaotong University School of Medicine and Wiley Publishing Asia Pty Ltd.
Department of Pharmacology and Toxicology, Faculty of Pharmacy, University of Benin, Benin, Nigeria.
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