We report the synthesis and characterization of three new complexes of the natural flavonoid 5-hydroxyflavone (primuletin) and Al (III), Ga (III), In (III), respectively. The physico-chemical properties and structural features of these three novel compounds have been investigated by elemental and thermogravimetric analysis, molar conductance and several spectroscopic techniques, including FT-IR, UV-Vis and mass spectra. Based on the experimental data, the general chemical formula of the complexes iswhere M is the cation and n = 2 for Al (III), n = 0 for Ga (III), n = 1, for In (III); each one of the three 5-hydoxyflavone molecules acts as a monoanionic bidentate chelate ligand in the complexes. DFT calculations further sustain the proposed structures of the complexes. Cytotoxicity was studied using MTS assay on cervical, breast, colon and ovary adenocarcinoma cell lines.The central metal ions exert cytotoxic effects in a disparate manner: Al (III) enhances, while Ga (III) and In (III) decrease the cytotoxicity of the ligand.As a means to investigate the mechanism underlying the cytotoxic effects of the complexes, interactions with calf thymus DNA, human serum albumin and transferrin were also carried out.This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.

In order to develop novel chemotherapeutic agents with potent anticancer activities, a series of new 2,5-diaryl/heteroaryl-1,3,4-oxadiazoles were designed and synthesized. The structures of the new compounds were established using elemental analyses, IR and NMR spectral data. The compounds were evaluated for their anticancer potential on two standardized human cell lines, HT-29 (colon adenocarcinoma) and MDA-MB-231 (breast adenocarcinoma). Cytotoxicity was measured by MTS assay, while cell cycle arrest and apoptosis assays were conducted using a flow cytometer, the results showing that the cell line MDA-MB-231 is more sensitive to the compounds’ action. The results of the predictive studies using the PASS application and the structural similarity analysis indicated STAT3 and miR-21 as the most probable pharmacological targets for the new compounds. The promising effect of compound 3e, 2-[2-(phenylsulfanylmethyl)phenyl]-5-(4-pyridyl)-1,3,4-oxadiazole, especially on the MDA-MB-231 cell line motivates future studies to improve the anticancer profile and to reduce the toxicological risks. It is worth noting that 3e produced a low toxic effect in the D. magna 24 h assay and the predictive studies on rat acute toxicity suggest a low degree of toxic risks.

No abstract

Naringenin enhances the UV protection, photostability and cell viability of lipid based vegetable nanocarriers.