TITLE:
Antioxidant and Cytotoxicity Potential of Six Synthesized Chalcones
AUTHORS:
S. L. Kouakou, M. Ouattara, J. P. N’Guessan, S. Coulibaly, A. G. Irié-N’Guessan, G. Kouakou-Siransy
KEYWORDS:
Chalcones, Antioxidant, Cytotoxic, HEP-2, A549, ABTS
JOURNAL NAME:
Pharmacology & Pharmacy,
Vol.9 No.12,
December
26,
2018
ABSTRACT: Background: Chalcones are
open-chain flavonoids which display a large number of pharmacological
activities such as cytotoxic, anti-inflammatory including antioxidant. The objective of this study was to assess antioxidant and cytotoxic
activity of six synthesized chalcones. Methodology: For the current experiments, 1,3-diphenylpropenone (compound R) was used as molecular model to
synthetize six compounds, namely three
benzyl-benzimidazolyl-chalcones (U1, U2, WAC1) and three imidazopyridinyl-chalcones (V1, V2,
V3). All the compounds were evaluated for their ability to scavenge the stable
free ABTS.+ radical cation, according to the
method develop by Choong et al. In addition, the cytotoxicity test described by Price et al., was performed using healthy human cell line, then in human malignant cell lines (HEP-2, A549). Results: All synthesized chalcones reduced the ABTS.+ radical cation.
Indeed, benzyl benzimidazolyl compounds WAC1, U1, U2, by developing
respectively 39.61%, 66.09%, and 84.20% percentages of reduction, showed an
antioxidant effect 6, 11 and 14 times greater than the compound R (6.14%). As
a result, imidazopyridinyl-chalcones compounds, namely V1, V2 and V3 reduced
the ABTS.+ radical cation at 91.62%, 99.84% and 97.45% respectively, being 15 and 16 times more active than the
compound R. About cytotoxicity, V2 inhibited not significantly HEP-2 malignant cells
growth at 48.64%, compared to the standard product, i.e. doxorubicin that inhibited the
growth of the same cells at 42.37%. WAC1 inhibited significantly the growth of
A549 malignant cells at 89.53%, more than doxorubicin which percentage of
growth inhibition was 71.58%. Conclusion: The presence of the α, β-unsaturated carbonyl system (or 1,3-diphenylpropenone) along with a
benzimidazole or imidazopyridine heterocyclic ring is likely to contribute to both cytotoxic and antioxidant activities of
these compounds.