Several chalcones were synthesized and their in vitro cytotoxicity against various human cell lines, including human breast adenocarcinoma cell line MCF-7, human lung adenocarcinoma cell line A549, human prostate cancer cell line PC3, human adenocarcinoma cell line HT-29 (colorectal cancer) and humannormal liver cell line WRL-68 was evaluated. Most of the compounds being active cytotoxic agents, four of them with minimal IC50 values were chosen and studied in detail with MCF-7 cells. The compounds 1, 5, 23, and 25 were capable in eliciting apoptosis in MCF-7 cells as shown by multiparameter cytotoxicity assay and caspase-3/7, -8, and -9 activities (p < 0.05). The ROS level showed 1.3-fold increase (p < 0.05) at the low concentrations used and thus it was concluded that the compounds increased the ROS level eventually leading to apoptosis in MCF-7 cells through intrinsic as well as extrinsic pathways.
Palm date fruits have been used for nutritional and medicinal purposes in Middle Eastern countries. They are used in folk medicine for treatment of liver diseases and highly recommended to be consumed by pregnant women before and after delivery. Therefore, the present work aimed to determine the total phenolic content and total flavonoids in three syrups obtained from palm dates extracted with aqueous ethanol (80%) and to evaluate in vitro their antioxidative properties. The new findings showed that the three tested syrups contained significantly different amounts of both total phenolic content and total flavonoids. Syrups can be arranged according to the increase of total phenolic contents and total flavonoids as follows: Yemeni-Rotab > Saudi-Tamr > Iraqi-Tamr. The results of antioxidant activities of palm dates syrups obtained by using different in vitro methods were varied depending on the method used. According to the TBARS method, H2O2 scavenging ability and DPPH methods, all syrups showed to have high to very high antioxidant activities. On the other hand, syrups showed low to intermediate antioxidant activities when other methods were used, such as the scavenging ability of OH and NO and the ability to chelate Fe2+ ions. Generally, the values of antioxidant activities of Rotab-syrup have been shown to be always the highest.
Polyhydroxylated natural phenolic compounds, especially those with low molecular weights, are characterized by their ability to eliminate free radicals as they act as strong antioxidants. The various types of phenolic compounds represent the most important natural antioxidants in addition to some vitamins. The chemical structures of these compounds is discussed in details with their action mechanisms to remove free radicals and prevent many incurable and malignant diseases. In addition to these natural compounds, the last two decades have witnessed increased attempts by many scientific groups and research centers to synthesize chemical compounds in large quantities to mimic these natural compounds, but at a lower cost and greater biological effectiveness. Herein, we conduct a chemical survey of relevant synthetic compounds containing the hydroxyl groups prepared in chemical laboratories and studied for their biological efficacies, such as their effectiveness as antioxidants, as well as the mechanism of elimination of free radicals.
There has been substantial interest over the past many years in the design of novel chemical compounds containing the azomethine group (-NH-N=CH) and exhibiting various medicinal properties such as antibacterial, antiviral, antifungal, and anti-inflammatory activities. Herein, hydrazones were synthesized via the chemical reaction of substituted aromatic hydrazides with various aromatic aldehydes. The obtained products were confirmed using different physical and spectroscopic techniques, such as m.p., IR, 1H-NMR and 13C-NMR. The present study was designed to synthesize different aromatic hydrazones assembled by various combinations of aromatic hydrazides and aromatic benzaldehydes containing different substituents such as hydroxyl and polyhydroxyl groups as key structural features. Thus, incorporating such moieties and simultaneously creating highly-conjugated systems was expected to create novel species to mimic as much as possible natural phenolics, chalcones and stilbenes. Compounds of aromatic hydrazones synthesized in the present study were tested in vitro for their direct and indirect antioxidant activities using different methods such as DPPH, ABTS and FTC. The antioxidant activities of the new compounds ranged from very weak to very high activity. In addition, the inhibition of tyrosinase and cholinesterase by these compounds was tested. The new compounds containing two or three hydroxyl groups attached to aldehyde rings exhibited significantly greater inhibition effects on tyrosinase or cholinesterase activities in comparison to other compounds of the same series containing only one hydroxyl group.