Chitosan-Gelatin-EGCG Nanoparticle-Meditated LncRNA TMEM44-AS1 Silencing to Activate the P53 Signaling Pathway for the Synergistic Reversal of 5-FU Resistance in Gastric Cancer.

Chemoresistance is one of the leading causes of therapeutic failure in gastric cancer (GC) treatment. Recent studies have shown lncRNAs play pivotal roles in regulating GC chemoresistance. Nanocarriers delivery of small interfering RNAs (siRNAs) to silence cancer-related genes has become a novel approach to cancer treatment research. However, finding target genes and developing nanosystems capable of selectively delivering siRNAs for disease treatment remains a challenge. In this study, a novel lncRNA TMEM44-AS1 that is related to 5-FU resistance is identified. TMEM44-AS1 has the ability to bind to and sponge miR-2355-5p, resulting in the upregulated PPP1R13L expression and P53 pathway inhibition. Next, a new nanocarrier called chitosan-gelatin-EGCG (CGE) is developed, which has a higher gene silencing efficiency than lipo2000, to aid in the delivery of a si-TMEM44-AS1 can efficiently silence TMEM44-AS1 expression to synergistically reverse 5-FU resistance in GC, leading to a markedly enhanced 5-FU therapeutic effect in a xenograft mouse model of GC. These findings indicate that TMEM44-AS1 may estimate 5-FU therapy outcome among GC cases, and that systemic si-TMEM44-AS1 delivery combined with 5-FU therapy is significant in the treatment of patients with recurrent GC.

A practical and fast isolation of 12 cyclolinopeptides (linusorbs) from flaxseed oil via preparative HPLC with phenyl-hexyl column.

Linusorbs, known as cyclolinopeptides, are a group of cyclic hydrophobic peptides derived from flaxseed oil with various health benefits. However, the current research efforts on both the biological activities and antioxidant capacities of linusorbs are limited because of existing issues with their purification and characterization. A practical method based on preparative HPLC for isolating 12 linusorbs simultaneously was developed and factors such as the solvent selection, gradient elution program, flow rate, loaded mass, and loading concentration, were optimized. The optimum conditions were an initial acetonitrile (ACN) to water ratio of 40%, final ACN ratio of 80%, eluting time of 21 min, a flow rate of 16 mL/min, sample load of 12.5 mg, and concentration of 80 mg/mL (in methanol). The 12 linusorbs obtained were verified using off-line MS/MS, recording purities of above 95.5%. The method could serve as a practical and fast isolation method enabling further investigation of minor linusorbs.

Structuring of sunflower oil by stearic acid derivatives: Experimental and molecular modelling studies.

Structuring of vegetable oils has potential application in food, pharmaceutical and cosmetic products. In this study, structuring effects of stearic acid derivatives on sunflower seed oil were systematically investigated by experimental and molecular simulation methods. Stearic acid (SA), 12-hydroxy stearic acid (HSA) and 2-hydroxyethyl stearate (HES) were able to structure sunflower seed oil, among which the structuring ability of HES was reported for the first time. The oleogel formed with HSA exhibited good mechanical properties (such as hardness, fracturability, adhesiveness, chewiness and storage modulus), which coincided with its highest solid fat content and degree of crystallinity. Oleogels containing SA and HES showed similar mechanical properties. Both the molecular dynamics (MD) simulation and independent gradient model (IGM) confirmed that the HSA dimer possessed the strongest interaction during the self-assembly process while the dimers of HES and SA had similar interactions, which could explain their structuring performance.

Evaluation of Oral Bioaccessibility of Aged Citrus Peel Extracts Encapsulated in Different Lipid-Based Systems: A Comparison Study Using Different in Vitro Digestion Models.

The oral delivery efficiency of aged citrus peel extract containing polymethoxyflavones and 5-demethylated polymethoxyflavones (PMFs) in three different systems, including a pure oil phase, a Tween 80-stabilized nanoemulsion, and a milled-cellulose-particles-stabilized Pickering emulsion, was investigated using two typical in vitro digestion models. The digestion profiles and release of PMFs in these emulsions and bulk oil in the human upper gastrointestinal (GI) tract were evaluated using the pH-stat lipolysis model and TNO's gastrointestinal model (TIM-1). Compared to the bulk oil sample, the bioaccessibilities of PMFs in the nanoemulsion and Pickering emulsion were both increased by around 14 fold when the pH-stat lipolysis model was used. However, the results from the TIM-1 system indicated that the bioaccessibilities of PMFs in the nanoemulsion and Pickering emulsion were around two and four times that in bulk oil, respectively. The results from this work would provide valuable information for the rational design and evaluation of lipid-based delivery systems for lipophilic bioactive compounds.

Nano/Submicrometer Milled Red Rice Particles-Stabilized Pickering Emulsions and Their Antioxidative Properties.

Nano/submicrometer red rice particles were obtained through processing a type of red rice using media-milling. The diameters of red rice were gradually reduced as processing time increased. After 4 h of processing, the particle size of milled red rice was reduced to around 692 nm. Microscopic observation and SEM analysis confirmed the presence of nano/submicrometer particles. The phytochemical contents of milled red rice were analyzed. The total anthocyanin content of red rice increased after milling process. Its phenolic and flavonoid contents were slightly decreased after the milling process. All milled red rice exhibited good ferric reducing antioxidant property (FRAP) and DPPH (2, 2-diphenyl-1-picrylhydrazyl) radical scavenging activity. The emulsifying ability of milled red rice particles with different milling time was characterized. Milled red rice starch particles with a concentration of 0.8-3.5% were able to form stable Pickering emulsions, and milled red rice particles retarded the oil oxidation process when being used as Pickering emulsions stabilizers. This pioneer study directly modifies whole grain materials to submicrometer particles that can form stable food grade Pickering emulsions with intrinsic antioxidant properties.

pH-Responsive Emulsions with ß-Cyclodextrin/Vitamin E Assembled Shells for Controlled Delivery of Polyunsaturated Fatty Acids.

Lipid-based delivery systems (LBDSs) are widely applied in pharmaceuticals and health care because of the increased bioavailability of lipophilic components when they are coadministered with high-fat meals. However, how to accurately control their in vivo release and stability is still challenging. Here, after introducing the simple esterification and coprecipitation, we created the dual-functional composite ODS-ß-CD-VE by the coassembly of ß-cyclodextrin (ß-CD), octadecenyl succinic anhydride (ODSA), and vitamin E (VE). The resulting dual-functional particle presented a uniform sheetlike shape and nanometer size. In addition, its chemical structure was clarified in detail via nuclear magnetic resonance (NMR), Fourier transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD). Benefiting from the antioxygenation of VE, lipid oxidation in the ODS-ß-CD-VE-stabilized Pickering emulsion was effectively inhibited. Meanwhile, pH-induced protonation/deprotonation of carboxyl groups guaranteed that the emulsions kept steady at pH ≤4 but were unsteady under neutral conditions. In this way, the lipids contained in the emulsion were protected from gastric juice and then digested and accurately released as n-3 polyunsaturated fatty acids (PUFA) in the simulated intestine environment. This strategy sheds some light on the rational and efficient construction of LBDSs for nutrient supplements and even pharmaceuticals in a living digestive tract.

Structural changes of waxy and normal maize starches modified by heat moisture treatment and their relationship with starch digestibility.

In the present study, the variations in structure of waxy and normal maize starches modified by heat-moisture treatment (HMT) for different treating time (3h and 9h) were investigated. HMT caused the destruction of starch granules. The 1H NMR confirmed that glycosidic bonds were broken during HMT. The 13C NMR result suggested that HMT caused the transformation of starch granules from double and single helical components into amorphous components. Heat-moisture treated starches exhibited higher gelatinization temperature (To, Tp and Tc), narrower gelatinization temperature range (Tc-To) and lower gelatinization enthalpy (ΔH). HMT caused the rearrangement of starch molecules, degeneration of double helices and formation of new single helix. In addition, in vitro digestibility assessment indicated that the contents of rapidly digestible starch (RDS) and slowly digestible starch (SDS) were improved and resistant starch (RS) was reduced after HMT, which was related to the decrease of single and double helical components.