Synthesis of B-ring substituted flavones and evaluation of their antitumor and antioxidant activities

Synthesis, Biological Evaluation and Docking Studies of Chalcone and Flavone Analogs as Antioxidants and Acetylcholinesterase Inhibitors

“…The influence of electron-donor groups, like methoxyl, can be analyzed with the 2e (p-OMe), 2f (m-OMe), and 2g (p,m-OMe) analogs; the presence of these groups did not favor the activity, getting concentrations of 100, 170, and 5 × 10 4 µg/mL, respectively, in DPPH assay, having a similar behavior of the flavones 3e-g, with EC 50 of 30, 39, and 410 µg/mL. These results may appear to contrast with the reported by many authors where methoxyl groups are considered an important factor for the antioxidant activity [42,43], however, this is the case where methoxyl groups help with the lipophilicity of the molecule, for example, when the antioxidant activity is measured by the lipid peroxidation activity assay [39]. When employing DPPH test, the transfer of acid protons is required; this implies that just as in the case of the chalcones, we consider indispensable the presence of at least one hydroxyl group, explaining the lack of scavenging activity for the synthesized compounds with only methoxyl groups (3e-g).…”

“…The high double bond conjugation of chalcone and flavonoid systems, just as the presence of a C2-C3 double bond and a carbonyl in C-4 position, have been reported as structural characteristics for the antioxidant activity [39], being these incorporated in the basic skeleton of all the synthesized compounds.…”

“…The EC 50 values of compounds, quercetin and α-tocopherol obtained are shown in Table 1 and Figure 2. lipophilicity of the molecule, for example, when the antioxidant activity is measured by the lipid peroxidation activity assay [39]. When employing DPPH test, the transfer of acid protons is required; this implies that just as in the case of the chalcones, we consider indispensable the presence of at least one hydroxyl group, explaining the lack of scavenging activity for the synthesized compounds with only methoxyl groups (3e-g).…”

Bioactive molecules as authenticity markers of Italian Chinotto (Citrus×myrtifolia) fruits and beverages

“…The collected results showed that Citrus × myrtifolia fruit contains all nine active compounds and that those present in greater amounts are caffeic acid, ferulic acid and vanillin, which are present both in the exocarp and in the endocarp in very similar M a n u s c r i p t 13 concentrations. Moreover, significantly higher concentrations of quercetin were found in the peel of the fruit when compared to the pulp and the whole fruit; lower concentrations of myricetin were determined in the endocarp and in the exocarp.…”

“…It is known how citrus fruits are rich in different phytochemicals, which all contribute to determine a high nutraceutical potential: several studies have shown that these compounds possess biological properties such as antioxidant, anti-inflammatory and analgesic effects, anti-viral and anti-bacterial activities, up to anti-thrombotic, neuroprotective and anti-tumoral properties [2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17].…”