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Therapeutic actions of allylmercaptocaptopril (BL‐2040) in the SHROB rat model of metabolic syndrome and glomerulosclerosis
Author(s) -
Ernsberger Paul,
Rosenthal T,
Mirelman D,
Koletsky R J
Publication year - 2007
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.21.6.a1196-a
Subject(s) - captopril , endocrinology , medicine , blood pressure , creatinine , pharmacology
The spontaneously hypertensive obese (SHROB) rat is a model of obese hypertension which spontaneously develops end stage renal disease. BL‐2040 is a conjugate of the ACE inhibitor captopril with allicin, an antioxidant in garlic. We compared BL‐2040 (53.5 mg/kg/d orally for 60d) to an equimolar dose of captopril (40 mg/kg/d). Both agents lowered blood pressure, but BL‐2040 was more effective. Triglycerides were decreased by both captopril and BL‐2040. Total and non‐HDL cholesterol were reduced by captopril but not BL‐2040. BL‐2040 showed significant nephroprotection, as indicated by reductions in urinary protein loss (control: 179±26; captopril: 134±29; BL‐2040: 86±17mg/d), urinary protein/creatinine, and plasma creatinine. Finally, both BL‐2040 and captopril reduced the basal level of lipolysis in isolated abdominal adipocytes and restored the response to catecholamine stimulation. Both captopril and BL‐2040 are effective in attenuating metabolic syndrome. BL‐2040 may have additional effectiveness on improving glucose tolerance, lowering blood pressure, reversing cardiac hypertrophy and retarding renal disease.