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.

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 mu g/mL for EA), while the other lines were susceptible only to EC (IC50 88.27 +/- 1.34 on Caco-2 cells and over 100 mu g/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.

Luteolin derivates are plant compounds with multiple benefits for human health. Stability to heat and acid hydrolysis and high resistance to (auto)oxidation are other arguments for the laden interest in luteolin derivates today. The present study was designed to compare the in silico and in vitro anti-proliferative potential of two luteolin derivates, luteolin-7-O-glucoside/cynaroside (7-Lut) and luteolin-8-C-glucoside/orientin (8-Lut). In silico investigations were carried out on the molecular target, namely, the human dual specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2) in association with its natural ligand, curcumin (PDB ID: 5ZTN), by CLC Drug Discovery Workbench v. 1.5.1. software and Molegro Virtual Docker (MVD) v. MVD 2019.7.0. software. In vitro studies were performed on two human tumor cell lines, glioblastoma (U87) and colon carcinoma (Caco-2), respectively. Altogether, docking studies have revealed 7-Lut and 8-Lut as effective inhibitors of DYRK2, even stronger than the native ligand curcumin; in vitro studies indicated the ability of both luteolin glucosides to inhibit the viability of both human tumor cell lines, up to 85% at 50 and 100 µg/mL, respectively; the most augmented cytotoxic and anti-proliferative effects were obtained for U87 exposed to 7-Lut (IC₅₀ = 26.34 µg/mL). The results support further studies on cynaroside and orientin to create drug formulas targeting glioblastoma and colon carcinoma in humans.

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.

Neuroblastoma can be accessed with compounds of larger sizes and wider polarities, which do not usually cross the blood–brain barrier. Clinical data indicate cases of spontaneous regression of neuroblastoma, suggesting a reversible point in the course of cell brain tumorigenesis. Dual specificity tyrosine-phosphorylation-regulated kinase2 (DYRK2) is a major molecular target in tumorigenesis, while curcumin was revealed to be a strong inhibitor of DYRK2 (PBD ID: 5ZTN). Methods: in silico studies by CLC Drug Discovery Workbench (CLC) and Molegro Virtual Docker (MVD) Software on 20 vegetal compounds from the human diet tested on 5ZTN against the native ligand curcumin, in comparison with anemonin. In vitro studies were conducted on two ethanolic extracts from Anemone nemorosa tested on normal and tumor human brain cell lines NHA and U87, compared with four phenolic acids (caffeic, ferulic, gentisic, and para-aminobenzoic/PABA). Conclusions: in silico studies revealed five dietary compounds (verbascoside, lariciresinol, pinoresinol, medioresinol, matairesinol) acting as stronger inhibitors of 5ZTN compared to the native ligand curcumin. In vitro studies indicated that caffeic acid has certain anti-proliferative effects on U87 and small benefits on NHA viability. A. nemorosa extracts indicated potential benefits on NHA viability, and likely dangerous effects on U87.

Introduction: Romania has the highest incidence and mortality rate of cervical cancer in Europe. The objective was to estimate the prevalence of high-risk human papillomavirus (hrHPV) genotypes and to evaluate the role of certain socio-behavioral factors in acquiring viral infection, in a cohort of Romanian women with negative Pap. Methodology: In a prevalence study 611 women (aged 17-58 years) with negative Pap, with no known history of atypical cytology and valid HPV test were included. Each participant completed a questionnaire containing data on socio-behavioral factors. From 344 women aged between 30-58 years, 63 were randomly selected for a second examination (conventional cytology and HPV detection and genotyping) after twelve months. Results: Of the 611 women, 19.80% were HPV positive, 14.73% infected with hrHPV. Differences in the prevalence of hrHPV (17.60% versus 12.50%) as single (13.01% vs 9.01%) and multiple infections (9.71% vs 3.49%) were noted between women under the age of 30 and above. Among socio-behavioral factors, marital status and multiple sexual partners correlate with HPV and hrHPV infection. At follow-up, from 34 HPV negative cases, 10 changed to positive (5 hrHPV), while 2 developed abnormal cytology. Out of the 29 HPV positive cases, 12 cleared the HPV infection and 17 retested positive of which 4 worsened their cytology. Conclusions: In Romania, HPV infection is common in women with negative cytology. HPV genotyping is of epidemiological importance because the distribution of hrHPV types can determine the impact of prophylactic vaccines and the necessity of HPV testing as screening method.