Curcumin is a polyphenol of the Curcuma longa plant, which can be used for various medicinal purposes, such as inflammation and cancer treatment. In this context, two symmetric curcumin derivatives (D1—(1E,6E)-1,7-bis(4-acetamidophenyl)hepta-1,6-diene-3,5-dione and D2—p,p-dihydroxy di-cinnamoyl methane) were obtained by the microwave-based method and evaluated for their antitumoral effect on human cervix cancer in comparison with toxicity on non-tumoral cells, taking into account that they were predicted to act as apoptosis agonists or anti-inflammatory agents. The HeLa cell line was incubated for 24 and 72 h with a concentration of 50 μg/mL of derivatives that killed almost half of the cells compared to the control. In contrast, these compounds did not alter the viability of MRC-5 non-tumoral lung fibroblasts until 72 h of incubation. The nitric oxide level released by HeLa cells was higher compared to MRC-5 fibroblasts after the incubation with 100 μg/mL. Both derivatives induced the decrease of catalase activity and glutathione levels in cancer cells without targeting the same effect in non-tumoral cells. Furthermore, the Western blot showed an increased protein expression of HSP70 and a decreased expression of HSP60 and MCM2 in cells incubated with D2 compared to control cells. We noticed differences regarding the intensity of cell death between the tested derivatives, suggesting that the modified structure after synthesis can modulate their function, the most prominent effect being observed for sample D2. In conclusion, the outcomes of our in vitro study revealed that these microwave-engineered curcumin derivatives targeted tumor cells, much more specifically, inducing their death.

The therapeutic effects of curcumin and its derivatives, based on research in recent years, are limited by their low bioavailability. To improve bioavailability and develop the medical field of application, different delivery systems have been developed that are adapted to certain environments or the proposed target type. This study presents some half-curcuminoids prepared by the condensation of acetylacetone with 4-hydroxybenzaldehyde (C1), 4-hydroxy-3-methoxybenzaldehyde (C2), 4-acetamidobenzaldehyde (C3), or 4-diethylaminobenzaldehyde (C4), at microwaves as a simple, solvent-free, and eco-friendly method. The four compounds obtained were characterized in terms of morphostructural and photophysical properties. Following the predictions of theoretical studies on the biological activities related to the molecular structure, in vitro tests were performed for compounds C1–C3 to evaluate the antitumor properties and for C4’s possible applications in the treatment of neurological diseases. The four compounds were encapsulated in two types of hydrogel matrices. First, the alginate–glucosamine network was generated and then the curcumin analogs were loaded (G1, G3, G5–G7, and G9). The second type of hydrogels was obtained by loading the active compound together with the generation of the hydrogel carrier matrices, by simply dissolving (G4 and G10) or by chemically binding half-curcuminoid derivatives to glucosamine (G2 and G8). Thus, two types of curcumin analog delivery systems were obtained, which could be applied in various types of medical treatments.

Anxiety and depression are two conditions that had increased incidences in the context of COVID-19. The administration of current therapies based on anxiolytic and antidepressant drugs can result in adverse reactions and even potential dangers in the case of some patients, such as older adults and elderly patients. Aiming to identify safer treatments, we used molecular docking to screen twenty natural compounds against γ-aminobutyric acid A receptor (GABAA receptor), a major drug target in anxiety, and against serotonin transporter (SERT), a major drug target in depression. The list of compounds included molecules that were previously reported as beneficial in the two conditions. In the case of all molecules, we predicted their drug-likeness, bioavailability, and pharmacokinetic profiles. Molecular docking has shown that the top five molecules in terms of affinity for the GABAA receptor are luteolin, baicalein, myricetin, chrysin, and curcumin. In the case of SERT, the top five ligands were myricetin, luteolin, curcumin, apigenin, and fisetin. According to the predictions performed here, these molecules comply with drug-likeness rules, are bioavailable and non-toxic, present a high intestinal absorption, and are distributed to the central nervous system. Our results point toward luteolin, myricetin, and curcumin as common ligands for the GABAA receptor and SERT, suggesting their beneficial effects for both anxiety and depression.