Nutraceutical cranberry powder extract (CBPE) has distinct polyphenols inhibiting colon cancer growth and proliferation. However, its oral therapeutic efficacy is hindered because of its low permeability. This study aims to formulate chitosan surface-modified PLGA nanoparticles (CS-PLGA NPs) for encapsulating CBPE and modulating its release rate, permeation, cell targeting, and, therefore, its cytotoxicity. A full 2³ factorial design is employed to scrutinize the effect of lactide/glycolide ratio, PLGA weight, and stabilizer concentrations on entrapment efficiency percentage (EE%), particle size (PS), polydispersity index (PDI), and zeta potential (ZP). The optimum formula (F4) shows spherical particles with a relatively high EE% (72.30 ± 2.86%), an appropriate size of 370.10 ± 10.31 nm, PDI; 0.398 ± 0.001, and ZP; −5.40 ± 0.21 mV. Alongside the ATR-FTIR outcomes, the chitosan surface-modified formula (CS-F4) demonstrates a significant increase in particle size (417.67 ± 6.77 nm) and a shift from negative to positive zeta potential (+21.63 ± 2.46 mV), confirming the efficiency of surface modification with chitosan. The intestinal permeability of F4 and CS-F4 is significantly increased by 2.19- and 3.10-fold, respectively, compared to the CBPE solution, with the permeability coefficient (P_app) being 2.05 × 10⁻⁴ cm/min and 2.91 × 10⁻⁴ cm/min, for F4 and CS-F4, respectively, compared to the CBPE solution, 9.36 × 10⁻⁵ cm/min. Moreover, CS-F4 evidences significant caspase-3 protein level expression stimulation and significant inhibition of vascular endothelial growth factor (VEGF) and signal transducer and activator of transcription-3 (STAT-3) protein expression levels, confirming the superiority of CS-F4 for targeting HT-29 cells. Briefly, CS-PLGA NPs could be regarded as a prosperous delivery system of CBPE with enhanced permeation, cell targeting, and antitumor efficacy.

There is a trend to use nanoparticles as distinct treatments for cancer treatment because they have overcome many of the limitations of traditional drug delivery systems. Gallic acid (GA) is an effective polyphenol in the treatment of tissue injuries. In this study, GA was loaded onto niosomes to produce gallic acid nanoemulsion (GANE) using a green synthesis technique. GANE’s efficiency, morphology, UV absorption, release, and Fourier-transform infrared spectroscopy (FTIR) analysis were evaluated. An in vitro study was conducted on the A549 lung carcinoma cell line to determine the GANE cytotoxicity. Also, our study was extended to evaluate the protective effect of GANE against lipopolysaccharide (LPS)-induced pulmonary fibrosis in rats. GANE showed higher encapsulation efficiency and strong absorption at 280 nm. Transmission electron microscopy presented a spherical shape of the prepared nanoparticles, and FTIR demonstrated different spectra for the free gallic acid sample compared to GANE. GANE showed cytotoxicity for the A549 carcinoma lung cell line with a low IC₅₀ value. It was found that oral administration of GANE at 32.8 and 82 mg/kg.b.w. and dexamethasone (0.5 mg/kg) provided significant protection against LPS-induced pulmonary fibrosis. GANE enhanced production of superoxide dismutase, GPx, and GSH. It simultaneously reduced the MDA level. The GANE and dexamethasone, induced the production of IL-4, but suppressed TNF-α and IL-6. On the other hand, the lung p38MAPK, TGF-β1, and NF-κB gene expression was downregulated in rats administrated with GANE when compared with the LPS-treated rats. Histological studies confirmed the effective effect of GANE as it had a lung-protective effect against LPS-induced lung fibrosis. It was noticed that GANE can inhibit oxidative stress, lipid peroxidation, and cytokines and downregulate p38MAPK, TGF-β1, and NF-κB gene expression to suppress the proliferation and migration of lung fibrotic cells.

Context: Genus Verbascum (Scrophulariaceae) comprises about 360 species of flowering plants. Verbascum has been used in traditional medicine as an astringent, antitussive, analgesic and anti-inflammatory. Objective: Nothing was found in the available literature concerning Verbascum nubicum Murb; therefore, the study evaluates the biological activities, isolated compounds and HPLC profile. Materials and methods: Methanol extract (VME) and butanol fraction (VBF) of air-dried powdered V. nubicum were obtained. Four compounds were isolated from VBE and identified by ¹H- and ¹³C-NMR. High-performance liquid chromatography (HPLC) profile was determined for (VME). LD₅₀, in vitro antioxidant, in vivo antiulcerogenic and anti-inflammatory activities as well as hepatoprotective activity were assessed. Anti-ulcerogenic and hepatoprotective activities were supported by histopathological examinations. Results: HPLC analysis of VME revealed the presence of luteolin 7-glucoside (2215.43 mg/100 g), hesperidin (954.51 mg/100 g) and apigenin (233.15 mg/100 g) as major compounds. Four compounds were isolated and confirmed by NMR data, were identified as gentiopicroside, luteolin, aucubin and gallic acid. The LD₅₀ of VME and VBF extracts were calculated to be 8200 and 4225 mg/kg b.w., respectively. IC₅₀ values of VBE and VMF as measured by DPPH·method were 43.6 and 50 µg/mL, respectively. Also, anti-inflammatory effect of VME (400 mg/kg b.w.) and VBF (200 mg/kg b.w.) induced edema model after 120 min were 61.93 and 56.13%, respectively. Antiulcerogenic activity of VME (400 mg/kg b.w.) and VBF (200 mg/kg b.w.) in albino rats were 65.14 and 84.57%, respectively. Conclusions: The V. nubicum extracts displayed safe and promising antioxidant, anti-inflammatory and hepatoprotective properties. It can be also applied in the pharmacy industry, food industry and healthcare.

Cranberry extract (CBE) is a major source of the antioxidant polyphenolics but suffers from limited bioavailability. The goal of this research was to encapsulate the nutraceutical (CBE), into bile salt augmented liposomes (BSALs) as a promising oral delivery system to potentiate its hepatoprotective impact against dimethylnitrosamine (DMN) induced liver injury in rats. The inclusion of bile salt in the liposomal structure can enhance their stability within the gastrointestinal tract and promote CBE permeability. CBE loaded BSALs formulations were fabricated utilizing a (2³) factorial design to explore the impact of phospholipid type (X₁), phospholipid amount (X₂), and sodium glycocholate (SGC) amount (X₃) on BSALs properties, namely; entrapment efficiency percent, (EE%); vesicle size, (VS); polydispersity index; (PDI); zeta potential, (ZP); and release efficiency percent, (RE%). The optimum formulation (F1) exhibited spherical vesicles with EE% of 71.27 ± 0.32%, VS; 148.60 ± 6.46 nm, PDI; 0.38 ± 0.02, ZP; −18.27 ± 0.67 mV and RE%; 61.96 ± 1.07%. Compared to CBE solution, F1 had attenuated DMN-induced hepatic injury, as evidenced by the significant decrease in serum level of ALT, AST, ALP, MDA, and elevation of GSH level, as well as SOD and GPX activities. Furthermore, F1 exhibited an anti-inflammatory character by suppressing TNF-α, MCP-1, and IL-6, as well as downregulation of VEGF-C, STAT-3, and IFN-γ mRNA levels. This study verified that when CBE was integrated into BSALs, F1, its hepatoprotective effect was significantly potentiated to protect the liver against DMN-induced damage. Therefore, F1 could be deliberated as an antioxidant, antiproliferative, and antifibrotic therapy to slow down the progression of hepatic damage.

Introduction: Cysteamine, a powerful endogenous antioxidant, is produced mostly by the vanin-1 with pantetheinase activity. With regard to glycemic, inflammatory, and redox factors, the current study sought to evaluate the association between the expression of the vanin-1 gene, oxidative stress, and inflammatory and iNOS signaling pathway in obese diabetic patients. Methods: We enrolled 67 male subjects with an average age of 53.5 ± 5.0 years, divided into 4 groups according to the WHO guideline. We determined their plasma levels of glucose, insulin, IRI, HbA1c, TC, TG, HDL-C, TNF- α, MCP-1, TGF-β 1, SOD, CAT, and TBARs, as well as expression of the iNOS and Vanin1 genes. Results: Overweight and obese class I and II diabetics had significantly higher levels of plasma glucose, insulin, HbA1c, TNF-α, MCP-1, TGF-β 1, CAT, and TBAR as well as iNOS and vanin-1 gene expression compared to healthy control individuals. In addition, as compared to healthy control individuals, overweight obese class I and II diabetics’ plasma HDL-C levels and blood SOD activity were significantly lower. In addition, ultrasound and computed tomography showed that the presence of a mild obscuring fatty liver with mild hepatic echogenicity appeared in overweight, class I and II obese diabetic patients. Conclusion: These findings provide important information for understanding the correlation between Vanin 1 and glycemic, inflammatory, and redox factors in obese patients. Furthermore, US and CT analysis were performed to visualize the observed images of fatty liver due to obesity. Graphical Abstract:

Parkia roxburghii belongs to the family Mimosaceae; it has been used since ancient times as a cure for different health complications; such as inflammatory and gynecological diseases and hemiplegia. In this investigation, a reversed-phase-high-performance liquid chromatography (RP-HPLC) profile was carried out for P. roxburghii; also, the isolated bioactive compounds including quercetin, catechin, and biochaninA were individually and/or in combination investigated for their inhibitory effects on scopolamine-induced memory impairments in mice, implying that they have the ability to reduce the neurodegenerative effects of scopolamine and thus could be employed as a more effective therapeutic agent in the treatment of Alzheimer’s disease (AD) in humans. The possible interactions of Parkia flavonoids with acetylcholinesterase (AChE), γ-aminobutyric acid A receptor, alpha5 (GABA_A α5), glycogen synthase kinase-3 (GSK-3), p38 mitogen-activated protein kinase (p38MAP-kinase), signal-regulated kinase (ERK), and protein-serine/threonine kinase (Akt) were then determined using molecular docking.