Preparation of pH-sensitive carboxymethyl chitosan nanoparticles loaded with ginsenoside Rb1 and evaluation of drug release in vitro.

Oral absorption of ginsenoside Rb1 (Rb1) is often hindered by the gastrointestinal tract. Carboxymethyl chitosan deoxycholic acid loaded with ginsenoside Rb1 nanoparticles (CMDA@Rb1-NPs), were prepared as a delivery system using a self-assembly technique with amphipathic deoxycholic acid grafted carboxymethyl chitosan as the carrier, which improved the stability and embedding rate of Rb1. In addition, the CMDA@Rb1-NPs was encapsulated with sodium alginate by ion crosslinking method with additional layer (CMDAlg@Rb1-NPs). Scanning electron microscopy showed that the nanoparticles were spherical, evenly distributed, smooth and without obvious adhesion. By evaluating drug loading, entrapment efficiency, the encapsulation efficiency of Rb1 increased from 60.07 % to 72.14 % after grafting deoxycholic acid improvement and optimization. In vitro release results showed that the cumulative release of Rb1 by CMDAlg-NPs showed a pH dependent effect, which was <10 % in simulated gastric juice with pH 1.2, completely released with pH 7.4 for about 48 h. In addition, Rb1 and CMDAlg@Rb1-NPs had inhibitory effects on A549 cells, and the inhibitory effect of CMDAlg@Rb1-NPs was better. Therefore, all results indicated that CMDA/Alg@Rb1 nanoparticles might be a novel drug delivery system to improve the stability and embedding rate of Rb1, and has the potential to be applied in oral pharmaceutical preparations.

Mangiferin for the Management of Liver Diseases: A Review.

The liver is a digestive and metabolic organ, and several factors can induce liver damage, which is a severe threat to human health. As a natural polyphenolic compound, mangiferin belongs to xanthone glucoside and mainly exists in many plants, such as mango. It is notorious that mangiferin has remarkable pharmacological activities such as anti-inflammatory, anti-tumor, antioxidative stress, antiviral and so on. Emerging evidence indicates the therapeutic benefits of mangiferin against liver disease, including liver injury, nonalcoholic fatty liver disease, alcoholic liver disease, liver fibrosis, and hepatocellular carcinoma. This review aims to summarize the possible underlying signaling mediated by mangiferin in liver disease treatment and the available findings of mangiferin, which can be used to treat different liver diseases and may contribute to mangiferin as a therapeutic agent for liver disease in humans.

Electrowetting of a Soft Elastic Gel.

A liquid drop may change its wettability on a surface with an applied voltage, known as electrowetting. Herein, we report an electrowetting phenomenon of a soft elastic gel, where gel elasticity plays an important role. We have designed experiments to measure the voltage-dependent adhesion energy between the gel and a metal electrode and proposed an electromechanical model for the electrowetting behavior of the gel. Our experiments have revealed that the voltage-dependent adhesion energy is an intrinsic material property of the polyvinyl chloride (PVC) gel, not affected by the electrode size, geometry, and the stressed state of the gel. Finally, we demonstrate that the predeformation of the gel can be used to tailor its electrowetting behavior.

Preparation of pH-sensitive chitosan-deoxycholic acid-sodium alginate nanoparticles loaded with ginsenoside Rb1 and its controlled release mechanism.

Ginsenoside is a natural extract of the genus ginseng, which has tumor preventive and inhibiting effects. In this study, ginsenoside loaded nanoparticles were prepared by an ionic cross-linking method with sodium alginate to enable a sustained slow release effect of ginsenoside Rb1 in the intestinal fluid through an intelligent response. Chitosan grafted hydrophobic group deoxycholic acid was used to synthesize CS-DA, providing loading space for hydrophobic Rb1. Scanning electron microscopy (SEM) showed that the nanoparticles was spherical with smooth surfaces. The encapsulation rate of Rb1 enhanced with the increase of sodium alginate concentration and could reach to 76.62 ± 1.78 % when concentration was 3.6 mg/mL. It was found that the release process of CDA-NPs was most consistent with the primary kinetic model which is a diffusion-controlled release mechanism. CDA-NPs exhibited good pH sensitivity and controlled release properties in buffer solutions of different pH's at 1.2 and 6.8. The cumulative release of Rb1from CDA-NPs in simulated gastric fluid was <20 % within 2 h, while could release completely around 24 h in the simulated gastrointestinal fluid release system. It was demonstrated that CDA3.6-NPs can effectively control release and intelligently deliver ginsenoside Rb1, which is a promising alternative way for oral delivery.

Syntheses, Characterizations, and Inhibition Activities Against Coxsackievirus B3 of Iodobenzoic Hydrazide Functionalized Hexamolybdates.

A class of iodobenzoyldiazenido-functionalized POMs (TBA)3 [Mo6O18(=N=NCOAr)] (Ar = Ph-o-I (1); Ph-m-I (2); Ph-p-I (3); Ph-3,4-I2 (4); Ph-2,3,5-I3 (5) (TBA = tetrabutylammonium) were prepared via the refluxing reaction of α-octamolybdates, DCC, and corresponding hydrazides in dry acetonitrile. Their structures were determined by Fourier-transform infrared spectroscopy, ultraviolet-visible spectra, X-ray photoelectron spectroscopy, hydrogen-1 nuclear magnetic resonance, and high-resolution mass spectrometry. Research on the biological activity of title compounds shows that L3, L5, 3, and 5 demonstrate potent inhibitory activity against coxsackievirus B3 and low in vitro cytotoxic activity against Hep-2 cell lines. The covalent linkage between the iodobenzoyldiazenido components and POMs can enhance the molecular inhibitory efficiency of iodobenzohydrazides.

Feprazone Displays Antiadipogenesis and Antiobesity Capacities in in Vitro 3 T3-L1 Cells and in Vivo Mice.

BACKGROUND AND PURPOSE: Excessive lipid accumulation in adipose tissues and deregulation of adipogenesis-induced obesity affect millions of people worldwide. Feprazone, a nonsteroidal anti-inflammatory drug, has a wide clinical use. However, it is unknown whether Feprazone possesses an antiadipogenic ability. The aim of this study is to investigate whether Feprazone possesses an antiadipogenic ability in 3 T3-L1 cells and an antiobesity capacity in mouse models. METHODS: An MTT assay was used to determine the optimized incubation concentrations of Feprazone in 3 T3-L1 cells. The lipid accumulation was evaluated using Oil Red O staining. The concentrations of triglyceride and glycerol release were detected to check the lipolysis during 3 T3-L1 adipogenesis. A quantitative real-time polymerase chain reaction (qRT-PCR) was used to determine the expressions of sterol regulatory element-binding protein-1C (SREBP-1C) and fatty acid binding protein 4 (FABP4) in treated cells. The expressions of peroxisome proliferator-activated receptor-γ (PPAR-γ), CCAAT/enhancer-binding protein α (C/EBP-α), adipose triglyceride lipase (ATGL), and aquaporin-7 (AQP-7) were detected using qRT-PCR and Western blot analysis. After the high-fat diet (HFD) mice were treated with Feprazone, the pathological state of adipocyte tissues was evaluated using HE staining. The adipocyte size, visceral adipocyte tissue weight, and bodyweights were recorded. RESULTS: According to the proliferation result, 30 and 60 µM Feprazone were used as the optimized concentrations of Feprazone. In the in vitro study, lipid accumulation, elevated production of triglycerides, the release of glycerol, upregulated SREBP-1C, FABP4, PPAR-γ, and C/EBP-α and downregulated ATGL and AQP-7 in the 3 T3-L1 adipocytes induced by the adipocyte differentiation cocktail medium were significantly reversed by treatment with Feprazone. In the in vivo experiment, we found that the increased adipocyte size, visceral adipocyte tissue weight, and body weights induced by HFD feeding in mice were significantly suppressed by the administration of Feprazone. CONCLUSION: Feprazone might display anti-adipogenic and antiobesity capacities in in vitro 3 T3-L1 cells and in vivo mice.

Changes in Matrix Metalloproteinase-8, Interleukin-6 and Tumor Necrosis Factor-A in Gingival Crevicular Fluid during Rapid Maxillary Expansion in Adolescent Patients.

BACKGROUND: Rapid maxillary expansion (RME) is the standard treatment for correcting lateral maxillary defects commonly used in orthodontics. It is the most effective approach to increase maxillary width in clinical practice. At present, there are few studies on the level of molecular biology of periodontal tissue remodeling during RME. We aimed to investigate changes in matrix metalloproteinase (MMP)-8, interleukin (IL)-6 and tumor necrosis factor (TNF)-αin gingival crevicular fluid during RME. METHODS: Patients admitted to Department of Stomatology, the Third Affiliated Hospital of Qiqihar Medical University, Qiqihar, Heilongjiang Province, China between Dec 2016 and Dec 2018 were enrolled, and randomly divided into the observation group (76 cases) and control group (62 cases). Periodontal clinical indicators were recorded. Gingival crevicular fluid was collected and the periodontal clinical indicators were recorded. The levels of MMP-8, IL-6 and TNF-α were determined by ELISA, and the contents of the two groups were compared. RESULTS: The plaque index of the observation group was significantly higher than that of the baseline T0 (P< 0.05) from T4, and the increase in the control group started from T5. The general clinical data of the two groups showed that the white blood cell count of the observation group was higher than that of the control group. The levels of MMP-8, IL-6 and TNF-α were the highest at T2, followed by T3, and gradually decreased at T4, and T5, and the differences were significant (P<0.05). CONCLUSION: The changes in levels of MMP-8, IL-6 and TNF-α in adolescent patients during RME were related to the remodeling of periodontal tissue after RME.

Effect of ultrasonic treatment on the physicochemical properties and antioxidant activities of polysaccharide from Cyclocarya paliurus.

The effects of ultrasonic treatment on the physicochemical properties and antioxidant activities of the polysaccharide from Cyclocarya paliurus leaves were investigated. The physicochemical properties were detected by high-performance gel permeation chromatography (HPGPC), high-performance anion exchange chromatography coupled with pulsed amperometric detection (HPAEC-PAD) and fourier transform infrared spectrometer (FT-IR) as well. The antioxidant activities were evaluated by the assay of DPPH, hydroxyl free radical, ß-carotene-linoleic acid, respectfully. Results showed that no considerable change was observed on the structure between the polysaccharide of Cyclocarya paliurus (CP) and the ultrasonic polysaccharide of Cyclocarya paliurus (UCP) by FT-IR, and no apparent differences were found on the content of sugar, uronic acid and protein after the ultrasonic treatment, but difference appeared in the ratio of monosaccharide composition of CP (1.0:4.6:3.5:4.5) and UCP (1.0:5.9:3.9:4.4), and the antioxidant activities of CP were promoted after ultrasonic treatment.