This study is focused on the encapsulation of polyphenols from Lycium barbarum leaves into liposomes as a strategy to improve their delivery. Liposomes loaded with Lycium barbarum leaves extract were obtained and characterized for particle size, polydispersity, entrapment efficiency, and stability. Liposomes presented entrapment efficiency higher than 75%, nanometric particle size, narrow polydispersity, and good stability over three months at 4 °C. The liposomes containing Lycium barbarum offered a slower release of polyphenols with attenuated burst effect compared with the dissolution of free Lycium barbarum extract in phosphate buffer solution at pH 7.4. Moreover, an in vitro pretreatment of 24 h with loaded liposomes showed a cytoprotective effect against H2O2-induced cytotoxicity on L-929 mouse fibroblasts cells. These preliminary findings imply that liposomes could be successfully employed as carriers for polyphenols in pharmaceutical applications.

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This study evaluates in vitro cytotoxic and antiproliferative activity on human colon tumor cell line Caco-2 (ATCC-HTB-37) of a standardized (5 mg GAE/mL) ethanolic extract from Stokesia laevis (Slae26), of five polyphenols compounds (reference substances, ref.), namely luteolin-7-O-glucoside, luteolin-8-C-glucoside, caffeic acid, gentisic acid, and p-aminobenzoic acid (PABA), as well as of Slae26 combinations with the five reference substances, 1:1 mass rate (GAE, ref.). Cell viability studies (MTS test) have revealed IC50 values of 36 μg GAE/mL in the case of Slae26 ethanolic extract, while Slae26 combinations with the five phenolics indicated IC50 values around 5 μg GAE/mL. In silico docking studies on the molecular targets human tankyrase 1 (TNKS1) and human tankyrase 2 (TNKS2) in complex with their native ligands, Co-crystallized 3J5A and Co-crystallized FLN, indicated score values of −104.15 and −76.97, respectively; in the series of the reference compounds studied, luteolin-7-O-glucoside was revealed with the best score values on both molecular targets (−80.49 and −85.17), together signifying real antiproliferative potential against human colon cancer of Slae26, of luteolin-7-O-glucoside, and of Slae26 combinations with all food-related bioactive compounds tested.

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The aim of this study was to develop a delivery system for polyphenols from an extract of Echinacea purpurea leaves, based on liposomes. Liposomes loaded with Echinacea purpurea were prepared and characterized in terms of entrapment efficiency, size, polydispersity index, stability and release behavior. Results showed good entrapment efficiency, small sizes, low polydispersity index and good stability over 90 days at 4oC. Also, the liposomal formulations presented reduced burst release and slow release of polyphenols compared with free extract. Therefore, liposomes offer a great potential in the development of drug delivery systems for polyphenols.

Eupatorium cannabinum L. (Asteraceae) has been used for a long time for medicinal purposes due to its various pharmacological effects and richness in active compounds such as phenolics, sesquiterpenes, pyrrolizidine alkaloids, and polysaccharides. Despite the high content of compounds that have important roles in medicinal plants, there are still limited literature data regarding this valuable species. The plant was fractioned using chloroform (EC) and distilled water (EA) and HPLC analysis revealed the presence of eupatorin, eupatilin, and quercetin in EC and caffeic acid and rutin in EA. The antiproliferative potential on BT-20, HepG2, Caco-2, and Jurkat cancer cell lines was assessed by MTS test. Jurkat cells were more sensitive to both extracts (IC 50 of 7.35 ± 0.35 for EC and 13.77 ± 2.16 µg/mL for EA), while the other lines were susceptible only to EC (IC 50 88.27 ± 1.34 on Caco-2 cells and over 100 µg/mL on BT-20 and HepG2 cells) after 24 h of exposure. In an LPS-induced damage mouse model of endotoxemia, we showed that preventive administration increases the survival times of mice and leads to inhibition of proinflammatory cytokines. Both polar and nonpolar compounds are involved in exerting these effects, but further analytical studies are needed to identify the key responsible compounds and their biochemical pathways.

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Oncoimmunology is a rapidly growing field, focusing both on studying of the interaction of immune factors with tumor cells and also on the development of new therapies. In this regard, immunotherapy is increasingly used clinically. Although tumorigenesis is generally seen as an autonomous process involving genetically transformed cancer cells, it is increasingly recognized that tumor environment is an essential factor that modulates both tumor progression and resistance to therapy. Tumor-associated immune cells, and in particular macrophages, are of particular importance in all stages of the tumorigenesis process and are also a clinical prognostic marker. From quantification of a single analyte in a given sample to complex platforms comprising multiple techniques, several methods for investigation of the dynamic balance and interaction between tumor-associated macrophages (TAMs) and tumor cells are available. This review presents the techniques carried out currently for investigation of TAMs functions, interactions, and modulation both at translational and transcriptional levels - ELISA and Multiplex assays, flow-cytometry, immunohistochemistry, DNA microarray - as essential steps not only for research purposes but also for predicting the therapeutic efficiency and patient survival.