This study explores the bioactive potential of young shoots from blackcurrant, European blueberry, and mountain cranberry, widely employed in gemmotherapy and phytotherapy, as rich sources of antioxidants, antimicrobial agents, and anti-inflammatory components. The primary aims of this study were to enhance the extraction conditions for bioactive compounds from blackcurrant young shoots using Modde software for experimental design, to conduct a comprehensive phytochemical analysis of blackcurrant, European blueberry, and mountain cranberry young shoot extracts through LC–MS analysis, and to evaluate the in vitro biological activities of these optimized extracts. The experimental design comprised multiple variables: extraction techniques, solvent type, extraction time, apparent pH, and the solvent-to-vegetal product ratio. The responses included total phenolic content, total flavonoid content, condensed tannin content, and total antioxidant activity determined through the DPPH assay. Furthermore, the antioxidant potential of the extracts was validated through in vitro cell culture experiments, in addition to the cytotoxicity assessments conducted on both normal and cancer cell lines. Extracts obtained through Ultra-Turrax extraction using 70% acetone displayed high levels of polyphenolic compounds and enhanced antioxidant potential, regardless of young shoots origin. LC–MS analysis revealed the predominant occurrence of chlorogenic acid, hyperoside, and isoquercitrin in all examined samples. The optimized extracts also displayed significant biological potential when evaluated in vitro on cell lines. These results provide valuable insights into the potent bioactive components present in these young shoot extracts, paving the way for further exploration in therapeutic applications.

A series of thiazolyl–catechol compounds with antioxidant and cytotoxic activities were synthesized by a Hantzsch heterocyclization, using diverse thioamides as the thiocarbonyl component and 4-chloroacetyl-catechol as haloketone. These compounds were characterized by MS, IR spectroscopy, and NMR. Their antioxidant potential was evaluated by antiradical, electron transfer, and ferrous ion chelation assays using ascorbic acid, Trolox, and EDTA-Na₂ as references. The cytotoxicity of the synthesized compounds was evaluated on two different cell types, normal human foreskin fibroblasts (BJ) and human pulmonary malignant cells (A549), using gefitinib as a reference anticancer drug. The results obtained from the tests highlighted compounds 3g and 3h with significant antioxidant activities. The highest cytotoxic potency against A549 cells was exhibited by compounds 3i and 3j, while compound 3g demonstrated exceptional selectivity on malignant cells compared to gefitinib. These promising results encourage further investigation into targeted modifications on position 2 of the thiazole ring, in order to develop novel therapeutic agents.

Background/Objectives: Magnetic hyperthermia (MH) has emerged as a promising alternative to conventional cancer treatments, offering targeted tumor destruction with minimal damage to healthy tissues. In this study, we synthesized manganese-doped magnetic nanoflowers (Mn-NFs) using a polyol-mediated approach to enhance heating efficiency and biocompatibility for MH applications. Our objective was to evaluate their structural, magnetic, and in vitro hyperthermic properties to determine their potential for lung cancer therapy. Methods: Mn-NFs, with the general formula MnxFe₃-xO₄ (x = 0, 0.3, 0.5, 0.7), were synthesized via a one-step polyol method and characterized using transmission electron microscopy (TEM), X-ray diffraction (XRD), and vibrating sample magnetometry (VSM). Their heating efficiency was assessed through specific absorption rate (SAR) measurements in aqueous and solid environments under an alternating magnetic field (AMF). Cytocompatibility was evaluated using the Alamar Blue assay on A549 lung carcinoma cells. Cellular uptake was quantified via a colorimetric iron determination method, while in vitro MH efficacy was tested by subjecting Mn-NF-loaded A549 cells to AMF exposure at different field strengths and nanoparticle concentrations. Results: Mn-NFs exhibited a flower-like morphology with enhanced magnetic properties, achieving high SAR values, particularly in immobilized conditions. Cytotoxicity assays confirmed high biocompatibility at relevant doses, with Mn-NFs of x = 0.3 showing optimal cellular uptake. MH studies demonstrated significant cancer cell death at AMF intensities of around 30 kA/m, with increased effectiveness following static magnetic field pre-alignment. Conclusions: The results highlight Mn-NFs, particularly those with a Mn content of x = 0.3, as promising candidates for MH-based lung cancer therapy, combining high heating efficiency, biocompatibility, and effective intracellular uptake. Further studies are needed to validate their therapeutic potential in vivo.

Background/Objectives: Angiogenesis plays a crucial role in tumor development and is a driving force for the aggressiveness of several types of cancer. Our team developed a novel series of thiosemicarbazone-containing quinazoline derivatives, TSC1-TSC10, as potential VEGFR2 inhibitors with proven anti-angiogenic and antiproliferative potential. Methods: The TSC1-TSC10 series was synthesized and characterized by spectral data. Extensive methodology was applied both in vitro (Alamar Blue assay, Scratch assay, CAM assay, and VEGFR2 kinase assay) and in silico (docking studies, MDs, and MM-PBSA) for the confirmation of the biological potential. Results: TSC10 emerged as the most promising compound, with a favorable cytotoxic potential across the cell panel (Ea.Hy296, HaCaT, and A375) in agreement with the in vitro VEGFR2 kinase assay (IC₅₀ = 119 nM). A comparable motility reduction in the vascular endothelial cells to that of the reference drug sorafenib was provided by TSC10, with a similar anti-angiogenic potential in the more complex in ovo model of the CAM assay. The in silico experiments confirmed the successful accommodation of the active site of the kinase domain similar to sorafenib for the entire TSC1-TSC10 series, providing valuable key insight into the complex stability driving force for the evaluated compounds. Conclusions: The in vitro evaluations of the biological potential correlated with the in silico predictions by computer-aided complex simulations provided a solid confirmation of the initial hypothesis for the TSC1-TSC10 series.

Retinal degenerative processes such as age-related macular degeneration are at the center of many ongoing research studies, as their impact on the general population is significant, with severe visual impairment and even irreversible vision loss if left untreated. Currently, there are few efficient treatments available to stop or limit its progression. In the present paper, a molecular hybridization approach was employed to develop novel compounds that address this issue. By adding either 2-butenal or a β-ionone-derived residue to the hydrazone-catechol-thiazole scaffold, two compounds were designed and synthesized: 5a and 5b. After being characterized by mass spectrometry and nuclear magnetic resonance, and proving potent antioxidant activity in the in vitro assays, the cytotoxicity evaluation using the ARPE-19, BJ, and A549 cell lines revealed a surprisingly low-dose effect of 5a and the unexpected cytotoxic activity of 5b, despite its β-ionone moiety, known for its significant therapeutic properties.

Background: Walnut (Juglans regia L.) processing generates polyphenol-rich by-products, including the septum (WS) and pellicle (WP). This study comparatively characterized the phytochemical composition of WS and WP from Romania and investigated their antioxidant and preliminary immunomodulatory properties using chemical, computational, and cell-based approaches. Methods: Extracts were characterized by targeted LC–QTOF–MS/MS, and antioxidant capacity was evaluated using ABTS, DPPH, and FRAP assays. Major phenolic compounds were docked against Kelch-like ECH-associated protein 1 (KEAP1), followed by 100 ns molecular dynamics simulations. Cytocompatibility was evaluated in Caco-2, Jurkat, and THP-1 cells, and cellular antioxidant activity was assessed in H₂O₂-stimulated Caco-2 cells using the DCFH-DA assay. Immunomodulatory potential was investigated following lipopolysaccharide (LPS) stimulation of the same cell lines. Results: WSLE contained 25 quantified compounds, with ellagic acid, catechin, procyanidins, and quercitrin among the major quantified constituents, whereas WP contained 13, with higher ellagic acid, gallic acid, and castalagin levels. WPE showed greater cell-free antioxidant capacity, while both extracts attenuated the H₂O₂-induced increase in intracellular DCF fluorescence in Caco-2 cells. Simulations suggested favorable KEAP1 interactions, with quercitrin and catechin predicted to form the most stable complexes. LPS induced an insufficient cytokine response in Caco-2 and Jurkat cells. In THP-1 cells, IL-8 was the only responsive marker, and both extracts reduced its LPS-induced secretion. Conclusions: The extracts showed distinct polyphenolic profiles and redox-related cellular activity. Their effects on IL-8 secretion in THP-1 cells and predicted KEAP1 binding are preliminary and hypothesis-generating; Nrf2 activation was not measured, and validation in physiologically relevant in vivo and clinical models is required to establish the biological relevance and potential applications of these extracts.