Antiobesity, antioxidant and cytotoxicity activities of newly synthesized chalcone derivatives and their metal complexes (original) (raw)

Synthesis and biological activities of some chalcone derivatives

2014

A series of chalcone derivatives were synthesized in order to obtain multipotent antioxidant and antimicrobial agents. These compounds were characterized by IR, and 1H-NMR. All the compounds were screened for in vitro antioxidant activity using DPPH, total reducing power activity (FRAP) based on the ability of compounds to reduce the Fe 3+-TPTZ complex to the Fe 2+ /ferrous, NO scavenging activity, and H2O2 scavenging activity methods. The present results showed that chalcone containing a hydroxyl group attached to one of the aromatic rings showed relatively high ability to reduce the danger of free radicals either directly (DPPH, NO scavenging activity, and FRAP) or indirectly (H2O2 scavenging activity). However, the highest activity was obtained when two hydroxyl groups attached to the two aromatic rings in chalcones. In addition, these compounds have been screened for their antibacterial and antifungal activities against strains of St. aureus, B. subtillis, E. coli, P. auriginose...

Antioxidant and Cytotoxicity Potential of Six Synthesized Chalcones

Pharmacology & Pharmacy, 2018

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.

A Green Synthesis of Chalcones As an Antioxidant and Anticancer

IOP Conference Series: Materials Science and Engineering

Three chalcones (4'-amino-4-methoxy chalcone, 4'-amino-3,4-dimethoxy chalcone and 4'-amino-3,4,5-trimethoxy chalcone) has been synthesized by a green chemistry approach using grinding technique. Antioxidant activity of the chalcones were assessed using 1,1biphenyl-2-picrylhydrazyl (DPPH) radical scavenging method. Cytotoxicity of chalcones sythesized was evaluated using a tetrazolium (MTT) colorimetric assay against cervical cancer cell line, HeLa. The antioxidant activity test showed that 4'-amino-4-methoxy chalcone had a stronger activity than the 4'-amino-3,4-dimethoxy chalcone and 4'-amino-3,4,5-trimethoxy chalcone, respectively with IC 50 58.85, 64.79 and 210.3 µg/mL. These results indicate that there is a relationship between the structure of chalcone with antioxidant activity, the more methoxy groups in the ring B of the chalcone, antioxidant activity is getting smaller. The chalcone synthesized showed cytotoxicity against HeLa cell line with IC 50 value of 31.75, 36.65, 49.04 µg/mL, respectively. It was observed that the highest cytotoxic activity was found at 4'-amino-4-methoxy chalcone (IC 50 31.75 µg/mL). Lower activity was showed by 4'amino-3,4,5-trimethoxy chalcone with IC 50 value of 49,04 µg/mL. There is a relationship cytotoxicity with chalcone structure, the more the number of methoxy groups in ring B chalcone, will decrease the activity of cytotoxicity.