Non-alcoholic fatty liver disease (NAFLD) is considered one of the most serious public health problems affecting liver. The reported beneficial impact of raspberries on obesity and associated metabolic disorder makes it a suitable candidate against NAFLD. In the current study, the chemical profile of raspberry seed oil (RO) was characterized by analysis of fatty acid and tocopherol contents using high-performance liquid chromatography (HPLC) in addition to the determination of total phenolic and flavonoids. High levels of unsaturated fatty acids, linoleic acid (49.9%), α-linolenic acid (25.98%), and oleic acid (17.6%), along with high total tocopherol content (184 mg/100 gm) were detected in oil. The total phenolic and flavonoid contents in RO were estimated to be 22.40 ± 0.25 mg gallic acid equivalent (GAE)/100 mg oil and 1.34 ± 0.15 mg quercetin (QU)/100 mg, respectively. Anti-NAFLD efficacy of RO at different doses (0.4 and 0.8 mL) in a model of a high-fat diet (HFD) fed rats was assessed by estimating lipid profile, liver enzyme activity, glucose and insulin levels as well as adipokines and inflammatory marker. Peroxisome proliferator-activated receptor γ (PPARγ), which is a molecular target for NAFLD was also tested. Liver histopathology was carried out and its homogenate was used to estimate oxidative stress markers. Consumption of RO significantly improved lipid parameters and hepatic enzyme activities, reduced insulin resistance and glucose levels, significantly ameliorated inflammatory and oxidative stress markers. Furthermore, RO treatment significantly modulated adipokines activities and elevated PPARγ levels. Raspberry seed oil administration significantly improved these HFD induced histopathological alterations. Moreover, a molecular docking study was performed on the identified fatty acids and tocopherols. Among the identified compounds, oleic acid, α-linolenic acid and γ-tocopherol exhibited the highest docking score as PPARγ activator posing them as a potential anti-NAFLD drug leads. Study findings suggest RO as an effective therapeutic candidate for ameliorating NAFLD.
Luteolin is a natural drug used as an antioxidant and anti-inflammatory, but unfortunately, it possesses low water solubility, which hinders its delivery via the skin. The main objective of this study was to prepare a luteolin-loaded nanosuspension by the antisolvent precipitation/sonication technique and study the effects of four stabilizers (two nonionic stabilizers, Pluronic F127 and Tween 80, and two polymeric stabilizers, HPMC and alginate) on the physicochemical properties of the prepared formulations. The selected formulations were incorporated into a gel base to evaluate their skin permeability and anti-inflammatory efficacy. The particle size was in the nanosize range (in the range from 468.1 ± 18.6 nm to 1024.8 ± 15.9 nm), while the zeta potential was negative and in the range from −41.7 ± 6.3 mV to −15.3 ± 1.9 mV. In particular, alginate-stabilized nanosuspensions showed the smallest particle size, the highest zeta potential value, and excellent stability due to the dual stabilizing effects (electrostatic and steric effects). The DSC results revealed a less crystalline structure of luteolin in lyophilized NS2 and NS12. Formulations stabilized by 1% Pluronic (NS2) and 2% alginate (NS12) were incorporated into a carbopol 940 gel base and showed good organoleptic character (homogenous with no evidenced phase separation or grittiness). In vitro dissolution studies showed that NS12 enhanced luteolin release rates, indicating the effect of particle size on the drug release pattern. On the other hand, NS2 showed enhanced skin permeability and anti-inflammatory effect in a carrageenan-induced paw edema model, revealing the surface activity role of the stabilizers. In conclusion, while alginate increased the nanosuspension stability by means of dual stabilizing effects, Pluronic F127 improved the skin delivery and pharmacodynamic efficacy of luteolin.
Solid tumors are fairly common and face many clinical di culties since they are hardly surgically resectable and broadly do not respond to radiation and chemotherapy. The current study aimed to fabricate ginsenoside Rg3 nanoparticles (Rg3-NPs) and evaluate their antitumor effect against Ehrlich solid tumors (EST) in mice. Rg3-NPs were fabricated using whey protein isolates (WPI), maltodextrin (MD), and gum Arabic (GA). EST was developed by the injection of mice with Ehrlich ascites cells (2.5 x 10 6 ). The mice were divided into a control group, EST group, and the EST groups that were treated orally 2 weeks for with normal Rg3 (3 mg/kg b.w), Rg3-NPs at a low dose (3 mg/kg b.w), and Rg3-NPs at a high dose (6 mg/kg b.w). Serum and solid tumors were collected for different assays. The results revealed that synthesized Rg3-NPs showed a spherical shape with an average particle size of 20 nm and zeta potential of -5.58 mV. The in vivo study revealed that EST mice showed a signi cant increase in AFP, Casp3, TNF-α, MMP-9, VEGF, MDA DNA damage accompanied by a signi cant decrease in SOD and GPx. Treatment with Rg3 or Rg3-NPs decreased the tumor weight and size and induced a signi cant improvement in all the biochemical parameters. Rg3-NPs were more effective than Rg3 and the improvement was dosedependent. It could be concluded that fabrication of Rg3-NPs enhanced the protective effect against EST development which may be due to the synergistic effect of Rg3 and MD, GA, and WPI.
Plant materials and Preparation of ginsenoside Rg3 nanoparticles (Rg3-NPs)Phoenix ginseng (the standardized Panax ginseng extract) containing 3.6% ginsenoside Rg3 (Rg3) was supplied by LOTTE Group R & D Center (Seoul, Korea). MD, GA, and WPI (1:1:1 w/w) were dissolved in 800 ml of distilled water with stirring. Solutions were left overnight at room temperature before emulsi cation for full hydration. Rg3 was dissolved in deionized water (10 g/100 ml) and the solution was progressively added to the polymer solution with homogenization at 20000 rpm for 10 min. The concentration of polymer was 20%, and Rg3 was 10% of the polymer mass concentration. The emulsion was encapsulated using a spray drier (B-290, Buchi) equipped with a pressure air atomizing nozzle at 2.5 bar, inlet, and outlet temperatures were 160 ± 5 and 85 ± 5 o C, respectively. The dried Rg3-NPs powder was collected and stored at 4 o C until analysis (Jinapong et al. 2008).
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