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EVALUATION OF ANTIOXIDANT POTENTIAL OF PYRAZOLONE DERIVATIVES

Mariappan G, Saha BP, Bhuyan NR, Bharti PR, Kumar D - J Adv Pharm Technol Res (2010)

Bottom Line: Among synthesized derivatives PYZ2, PYZ3, PYZ7, PYZ8, PYZ9, and PYZ10 were found to have potent antioxidant effect against MDA marker.In case of 4-HNE, PYZ4, PYZ5, PYZ6, PYZ7, PYZ8, PYZ9 and PYZ10 were found to have effective antioxidant activity and the rest of the compounds are moderately active.All the experimental data were statistically significant at p< 0.05 level.

Affiliation: Department of Pharmaceutical Chemistry, Himalayan Pharmacy Institute, E. Sikkim, (India).

ABSTRACT

In this article the antioxidant property of pyrazolones derivatives (PYZ1 to PYZ10) are reported. It was assessed by estimation of Malonaldehyde (MDA) and 4-Hydroxyl-2-noneal (4-HNE) as lipid peroxidation markers in myocardial ischemic reperfusion injury. The inhibition of lipid peroxidation was compared with the standard ascorbic acid. Among synthesized derivatives PYZ2, PYZ3, PYZ7, PYZ8, PYZ9, and PYZ10 were found to have potent antioxidant effect against MDA marker. In case of 4-HNE, PYZ4, PYZ5, PYZ6, PYZ7, PYZ8, PYZ9 and PYZ10 were found to have effective antioxidant activity and the rest of the compounds are moderately active. Comparatively PYZ7, PYZ8, PYZ9 and PYZ10 are having effective role to control both MDA and 4-HNE generation. All the experimental data were statistically significant at p< 0.05 level. Interestingly, beyond its NSAID property, this study explores the protective role of pyrazolone derivatives in ischemic heart injury.

Standard calibration curve of MDA estimation
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Figure 1: Standard calibration curve of MDA estimation

Mentions: TBARS activity in the myocardium was determined by a modified version of the method described by Okhawa et.al. 1979. Hearts were homogenized in 10% trichloroacetic acid at 4°C. 0.2 ml homogenate was pippeted in to a test tube followed by the addition of 0.2 ml of 8.1% sodiumdodecyl sulphate (SDS), 1.5 ml of 20% acetic acid (pH 3.5) and 1.5 ml of 0.8% TBA. All tubes were boiled for 60min at 90°C and then cooled on ice. 1.0 ml double distilled water and Sml of n-Butanol: pyridine (15:1v/v) mixture was added to the tubes and centrifuged at 4000 rpm for 10 minute. The absorbance of developed colour in organic layer was measured at 532nm. TBARS activity was determined, from the standard curve of TBA adduct formation when various concentration of commercially available 1, 1, 3, 3--tetramethoxypropane was subjected to the above procedure (Fig. 1 and 2). The concentration of MDA was expressed in nM.

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EVALUATION OF ANTIOXIDANT POTENTIAL OF PYRAZOLONE DERIVATIVES

Mariappan G, Saha BP, Bhuyan NR, Bharti PR, Kumar D - J Adv Pharm Technol Res (2010)

Standard calibration curve of MDA estimation
© Copyright Policy
Figure 1: Standard calibration curve of MDA estimation
Mentions: TBARS activity in the myocardium was determined by a modified version of the method described by Okhawa et.al. 1979. Hearts were homogenized in 10% trichloroacetic acid at 4°C. 0.2 ml homogenate was pippeted in to a test tube followed by the addition of 0.2 ml of 8.1% sodiumdodecyl sulphate (SDS), 1.5 ml of 20% acetic acid (pH 3.5) and 1.5 ml of 0.8% TBA. All tubes were boiled for 60min at 90°C and then cooled on ice. 1.0 ml double distilled water and Sml of n-Butanol: pyridine (15:1v/v) mixture was added to the tubes and centrifuged at 4000 rpm for 10 minute. The absorbance of developed colour in organic layer was measured at 532nm. TBARS activity was determined, from the standard curve of TBA adduct formation when various concentration of commercially available 1, 1, 3, 3--tetramethoxypropane was subjected to the above procedure (Fig. 1 and 2). The concentration of MDA was expressed in nM.

Bottom Line: Among synthesized derivatives PYZ2, PYZ3, PYZ7, PYZ8, PYZ9, and PYZ10 were found to have potent antioxidant effect against MDA marker.In case of 4-HNE, PYZ4, PYZ5, PYZ6, PYZ7, PYZ8, PYZ9 and PYZ10 were found to have effective antioxidant activity and the rest of the compounds are moderately active.All the experimental data were statistically significant at p< 0.05 level.

Affiliation: Department of Pharmaceutical Chemistry, Himalayan Pharmacy Institute, E. Sikkim, (India).

ABSTRACT

Background: In this article the antioxidant property of pyrazolones derivatives (PYZ1 to PYZ10) are reported. It was assessed by estimation of Malonaldehyde (MDA) and 4-Hydroxyl-2-noneal (4-HNE) as lipid peroxidation markers in myocardial ischemic reperfusion injury. The inhibition of lipid peroxidation was compared with the standard ascorbic acid. Among synthesized derivatives PYZ2, PYZ3, PYZ7, PYZ8, PYZ9, and PYZ10 were found to have potent antioxidant effect against MDA marker. In case of 4-HNE, PYZ4, PYZ5, PYZ6, PYZ7, PYZ8, PYZ9 and PYZ10 were found to have effective antioxidant activity and the rest of the compounds are moderately active. Comparatively PYZ7, PYZ8, PYZ9 and PYZ10 are having effective role to control both MDA and 4-HNE generation. All the experimental data were statistically significant at p< 0.05 level. Interestingly, beyond its NSAID property, this study explores the protective role of pyrazolone derivatives in ischemic heart injury.

View Similar Images In: Results  - Collection
View Article: Pubmed Central -  PubMed
Show All Figures - Show MeSH
getmorefigures.php?pmc=3255439&rFormat=json&query=null&req=5