Cardioprotective activity of synthetic guggulsterone (E and Z-isomers) in isoproterenol induced myocardial ischemia in rats: A comparative study |
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| Authors: | Ramesh Chander Farhan Rizvi A K Khanna Ram Pratap |
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| Institution: | (1) Division of Biochemistry, Central Drug Research Institute, 226001 Lucknow, India;(2) Medicinal Chemistry, Central Drug Research Institute, 226001 Lucknow, India |
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| Abstract: | Guggulsterone, a mixture of cis (E) and trans (Z) isomers (7∶3 w/w) was synthesized from 16-DPA. The isomers were separated
by column chromatography and evaluated for cardioprotective and antioxidant activities. Myocardial necrosis induced by isoproterenol
in rats caused marked increase in serum creatine phosphokinase and glutamate pyruvate transaminase. Simultaneously in ischemic
heart, phospholipase, xanthine oxidase and lipid peroxides were enhanced following depletion of glycogen, phospholipids and
cholesterol. Treatment with guggulsterone and its both isomers at the dose of 50 mg/kg po., significantly protected cardiac
damage as assessed by the reversal of blood and heart biochemical parameters in ischemic rats. The cardioprotective activity
of guggulsterone and of both the isomers were compared with that of gemfibrozil at the same doses. Guggulsterone and both
the isomers at tested concentrations (5–20mM) inhibited oxidative degradation of lipids in human low-density lipoprotein and
rat liver microsomes induced by metal ionsin vitro. The drug counteracted against the generation of superoxide anions (O2) and hydroxyl radicals (OH−) in non-enzymic test systems. It is suggested that cardioprotective and antioxidant activities of synthetic guggulsterone
and guggulsterone obtained from gum resinCommiphora mukul that contains isomers E & Z in the ratio of 46∶54w/w are the same. |
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| Keywords: | Cis and trans-guggulsterone cardiprotective activity antioxidant property Isoproterenol cardiac |
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