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Cinnamic acids have been identified as interesting compounds with antioxidant, anti-inflammatory and cytotoxic properties. In the present study, simple cinnamic acids were synthesized by Knoevenagel condensation reactions and evaluated for the above biological activities. Compound 4ii proved to be the most potent LOX inhibitor. Phenylsubstituted acids showed better inhibitory activity against soybean LOX, and it must be noted that compounds 4i and 3i with higher lipophilicity values resulted less active than compounds 2i and 1i. The compounds have shown very good activity in different antioxidant assays. The antitumor properties of these derivatives have been assessed by their 1/IC 50 inhibitory values in the proliferation of HT-29, A-549, OAW-42, MDA-MB-231, HeLa and MRC-5 normal cell lines. The compounds presented low antitumor activity considering the IC 50 values attained for the cell lines, with the exception of compound 4ii. Molecular docking studies were carried out on cinnamic acid derivative 4ii and were found to be in accordance with our experimental biological results.

Inhibitors of acetylcholine breakdown by acetylcholinesterase (AChE) constitute the main therapeutic modality for Alzheimer's disease. In the search for natural products with inhibitory action on AChE, this study investigated the activity of saffron extract and its constituents by in vitro enzymatic and molecular docking studies. Saffron has been used in traditional medicine against Alzheimer's disease. Saffron extract showed moderate AChE inhibitory activity (up to 30%), but IC(50) values of crocetin, dimethylcrocetin, and safranal were 96.33, 107.1, and 21.09 μM, respectively. Kinetic analysis showed mixed-type inhibition, which was verified by in silico docking studies. Safranal interacts only with the binding site of the AChE, but crocetin and dimethylcrocetin bind simultaneously to the catalytic and peripheral anionic sites. These results reinforce previous findings about the beneficial action of saffron against Alzheimer's disease and may be of value for the development of novel therapeutic agents based on carotenoid-based dual binding inhibitors.

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The purpose of the present in vitro study was to compare the cytotoxic effect of two commercially available brands of mineral trioxide cement (ProRoot MTA and MTA Angelus), modified zinc oxide-eugenol cement (SuperEBA) and resin-modified glass ionomer cement (Vitrebond) using rat pulp cells (RPC-C2A) and human lung fibroblasts (MRC-5). The cells were cultured in typical culture conditions and exposed to the tested materials by adaptation of insert wells. The cytotoxic effect was recorded at two observation periods (24 and 72 h) by using a colorimetric assay of tetrazolium reduction (XTT method) in reference to controls. Overall, the degree of cytotoxic effect in ascending order was ProRoot MTA - MTA Angelus < SuperEBA < Vitrebond. Both MTA materials tested exerted mild suppression of cellular mitochondrial activity and may be characterized as biologically inert materials.

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A series of aryl-acetic acids and hydroxamic acids possessing antioxidant/anti-inflammatory activities were tested for anticancer activity using different cancer cell lines. The compounds have low antitumor activity considering the 1/IC(50) values attained for the cell lines. Compound 5iv presents the best anticancer activity. Moreover, they depict the same activity pattern, suggesting similar mechanisms of action correlated to their antioxidant activities. The obtained results subjected in a QSAR analysis. It seems reasonable to conclude that the same molecular structural features are responsible for the compounds biological activity, these being the electron accepting/donating ability and the molar volume. For all cellular lines (HT-29, A-549 and OAW-42) log 1/IC(50) exhibits a reasonable correlation with a two parameters relationship in which the Esp-min and D term are present. Apart from Esp-min the other descriptor found important for anticancer activity is the molar volume (MgVol). The QSAR analyses did not indicate any role for lipophilicity Electrostatic potential, dipole moment and the bulk, primarily affect the biological response.

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