S‐Allyl‐Mercapto‐Captopril: A Novel Compound in the Treatment of Cohen‐Rosenthal Diabetic Hypertensive Rats

Abstract

S-allyl-mercapto-captopril (CPSSA) is a conjugate of captopril with allicin, an active principle in garlic with multiple beneficial actions on metabolic syndrome abnormalities, including weight preservation, observed by the authors in fructose-induced hypertensive hyperinsulinemic rats and in Koletsky rats. The aim of the study was to examine blood pressure (BP) and glucose levels in the Cohen-Rosenthal Diabetic Hypertensive (CRDH) model as well as to follow their weight preservation. CRDH rats (n=14) were fed the sugar-rich copper-free diet essential for the development of diabetes mellitus. Two months later BP and blood glucose levels were measured. CPSSA was diluted in drinking water and administered at a final dose of 53.5 mg/kg/d (n=8). Control rats (n=6) received no drug (vehicle group). In contrast to control group, CPSSA prevented progressive weight gain, without a detectable effect on food and water intake. CPSSA was effective in attenuating systolic and diastolic BP (P<0.01) as well as significantly reducing glucose levels (P<0.01). Control rats continued to gain weight, whereas the groups fed CPSSA did not. CPSSA was shown to have additional beneficial effects on improving BP and glucose level, as well as preserving weight gain. The authors conclude that the combined molecule CPSSA integrates the antihypertensive feature of both allicin and captopril, making it a potential antidiabetic and cardiovascular protective agent.

Spice-Derived Bioactive Ingredients: Potential Agents or Food Adjuvant in the Management of Diabetes Mellitus

“…This supports the in vitro data published by Kuo et al ( 2013 ) and further showed DATS ability to ameliorate diabetes-induced elevation of inflammatory mediators such as tumor necrosis factor-alpha (TNFα) in the muscles. Additionally, oral administration of S -allyl-mercapto-captopril (alliin and Captopril conjugate) at 53.5 mg/kg bw for 55 days reduced FBG (42%) and blood pressure in Cohen-Rosenthal diabetic hypertensive rats (Younis et al, 2010 ). Allicin (derived from hydrolysis of alliin) at 250 mg/kg bw decreased blood glucose levels and improved glucose tolerance after 4 h post-administration period in alloxan-induced diabetic rabbits (Mathew and Augusti, 1973 ).…”

Prevailing Knowledge on the Bioavailability and Biological Activities of Sulphur Compounds from Alliums: A Potential Drug Candidate

“…That evidently revealed the potential of allicin as a chemopreventive agent for the prevention of liver cancer [ 29 ]. Allicin along with a few molecules of captopril, makes them a potential antidiabetic and cardiovascular protective agent for the treatment of metabolic syndrome [ 30 ].…”

“…Day by day treatment with 600 mg of Allicor (garlic powder tablets) has proven to decrease both systolic and diastolic blood pressure. Younis, F., et al, had shown that S-allyl-mercapto-captopril (CPSSA), a conjugate of captopril with allicin, was effective in attenuating systolic and diastolic blood pressures as well as reducing blood glucose levels [ 30 ].…”

Therapeutic Role of Functional Components in Alliums for Preventive Chronic Disease in Human Being

“…Diallyl disulphide of garlic oil has the hypolipidemic effect and reducing the morbidity in diabetes [ 93 ]. The S -allyl-mercapto-captopril for a promising antidiabetic and cardiovascular protective agent integrates the antihypertensive feature between allicin and captopril [ 94 ]. Garlic plays an important role of improving metabolic syndrome containing abdominal obesity, hypertension, dyslipidemia, and hyperglycemia disorders [ 125 ], which prevents obesity by the downregulation of gene expression patterns [ 126 ].…”