Rice bran arabinoxylan compound as a natural product for cancer treatment - an evidence-based assessment of the effects and mechanisms.

CONTEXT: Rice bran arabinoxylan compound (RBAC) is a natural immunomodulator with anticancer properties. OBJECTIVE: This study critically evaluates the available evidence on the biological pathways of RBAC and its effects on cancer treatment. METHODS: This secondary analysis of a scoping review includes studies evaluating the mechanisms of RBAC on healthy or malignant cells, animal models, or humans for cancer prevention or treatment. Data from randomized controlled trials on survival and quality of life outcomes were subjectd to meta analysis. RESULTS: The evidence synthesis was based on 38 articles. RBAC exhibited antitumor properties by promoting apoptosis and restoring immune function in cancer patients to enhance inflammatory and cytotoxic responses to block tumorigenesis. RBAC works synergistically with chemotherapeutic agents by upregulating drug transport. In a clinical trial, combining RBAC with chemoembolization in treating liver cancer showed improved response, reduced recurrence rates, and prolonged survival. RBAC also augments the endogenous antioxidant system to prevent oxidative stress and protect against radiation side effects. In addition, RBAC has chemoprotective effects. Animals and humans have exhibited reduced toxicity and side effects from chemotherapy. Meta analysis indicates that RBAC treatment increases the survival odds by 4.02-times (95% CI: 1.67, 9.69) in the first year and 2.89-times (95% CI: 1.56, 5.35) in the second year. CONCLUSION: RBAC is a natural product with immense potential in cancer treatment. Additional research is needed to characterize, quantify, and standardize the active ingredients in RBAC responsible for the anticancer effects. More well-designed, large-scale clinical trials are required to substantiate the treatment efficacies further.

Understanding Antidiabetic Potential of Oligosaccharides from Red Alga Dulse Devaleraea inkyuleei Xylan by Investigating α-Amylase and α-Glucosidase Inhibition.

In this study, the α-glucosidase (maltase-glucoamylase: MGAM) and α-amylase inhibitory properties elicited by xylooligosaccharides (XOSs) prepared from dulse xylan were analysed as a potential mechanism to control postprandial hyperglycaemia for type-2 diabetes prevention and treatment. Xylan was purified from red alga dulse powder and used for enzymatic hydrolysis using Sucrase X to produce XOSs. Fractionation of XOSs produced xylobiose (X2), ß-(1→3)-xylosyl xylobiose (DX3), xylotriose (X3), ß-(1→3)-xylosyl-xylotriose (DX4), and a dulse XOS mixture with n ≥ 4 xylose units (DXM). The different fractions exhibited moderate MGAM (IC50 = 11.41-23.44 mg/mL) and α-amylase (IC50 = 18.07-53.04 mg/mL) inhibitory activity, which was lower than that of acarbose. Kinetics studies revealed that XOSs bound to the active site of carbohydrate digestive enzymes, limiting access to the substrate by competitive inhibition. A molecular docking analysis of XOSs with MGAM and α-amylase clearly showed moderate strength of interactions, both hydrogen bonds and non-bonded contacts, at the active site of the enzymes. Overall, XOSs from dulse could prevent postprandial hyperglycaemia as functional food by a usual and continuous consumption.

Dietary Intake of Yeast-Derived ß-Glucan and Rice-Derived Arabinoxylan Induces Dose-Dependent Innate Immune Priming in Mice.

Beta-glucans and arabinoxylans are known for their immunostimulatory properties. However, in vivo these have been documented almost exclusively following parenteral administration, underemphasizing oral intake. C57BL/6 mice are fed either a control diet or a diet supplemented with yeast-derived whole ß-glucan particle (yWGP) or with rice-derived arabinoxylan (rice bran-1) at a concentration of 1%, 2.5%, or 5% weight/weight (w/w) for 2 weeks. Thereafter, cells from blood, bone marrow, and spleen are collected for ex vivo stimulation with various microbial stimuli. Dietary intake of yWGP for 2 weeks at concentrations of 1% and 2.5% w/w increases ex vivo cytokine production in mouse blood and bone marrow, whereas 5% w/w yWGP shows no effect. In the spleen, cytokine production remains unaffected by yWGP. At a concentration of 1% w/w, rice bran-1 increases ex vivo cytokine production by whole blood, but 2.5% and 5% w/w cause inhibitory effects in bone marrow and spleen. This study demonstrates that dietary yWGP and rice bran-1 induce immune priming in mouse blood and bone marrow, with the strongest effects observed at 1% w/w. Future human trials should substantiate the efficacy of dietary ß-glucans and arabinoxylans to bolster host immunity, focusing on dose optimization.

Injectable nanoparticle-crosslinked xyloglucan/ε-poly-l-lysine composite hydrogel with hemostatic, antimicrobial, and angiogenic properties for infected wound healing.

Skin wounds are susceptible to infection, leading to severe inflammatory reactions that can progress to chronic wounds, ultimately causing significant physical and mental distress to the patient. In this study, we propose an injectable composite hydrogel achieved through one-pot gelation of oxidized xyloglucan (OXG), cationic polyamide ε-poly-l-lysine (EPL), and surface amino-rich silicon nanoparticles (SiNPs). OXG exhibits commendable anti-inflammatory properties and provides crosslinking sites. SiNPs serve as mechanically reinforced crosslinkers, facilitating the construction of a dynamic Schiff base network. SiNPs significantly reduced the gelation time to 3 s and tripled the storage modulus of the hydrogels. Additionally, the combination of EPL and SiNPs demonstrated synergistic antimicrobial activity against both S. aureus and E. coli. Notably, the hydrogel effectively halted liver bleeding within 30 s. The hydrogel demonstrated outstanding shear-thinning and self-healing properties, crucial considerations for the design of injectable hydrogels. Furthermore, its efficacy was evaluated as a wound dressing in a mouse model with S. aureus infection. The results indicated that, compared to commercial products, the hydrogel exhibited a shorter wound healing time, decreased inflammation, thinner epithelium, increased hair follicles, enhanced neovascularization, and more substantial collagen deposition. These findings strongly suggest the promising potential of the proposed hydrogel as an effective wound dressing for the treatment of infected wounds.

Caffeic acid combined with arabinoxylan or ß-glucan attenuates diet-induced obesity in mice via modulation of gut microbiota and metabolites.

Polyphenols and dietary fibers in whole grains are important bioactive compounds to reduce risks for obesity. However, whether the combination of the two components exhibits a stronger anti-obesity effect remains unclear. Caffeic acid is a major phenolic acid in cereals, and arabinoxylan and ß-glucan are biological macromolecules with numerous health benefits. Here, we investigated the effect of caffeic acid combined with arabinoxylan or ß-glucan on glucose and lipid metabolism, gut microbiota, and metabolites in mice fed a high-fat diet (HFD). Caffeic acid combined with arabinoxylan or ß-glucan significantly reduced the body weight, blood glucose, and serum free fatty acid concentrations. Caffeic acid combined with ß-glucan effectively decreased serum total cholesterol levels and hepatic lipid accumulation, modulated oxidative and inflammatory stress, and improved gut barrier function. Compared with arabinoxylan, ß-glucan, and caffeic acid alone, caffeic acid combined with arabinoxylan or ß-glucan exhibited a better capacity to modulate gut microbiota, including increased microbial diversity, reduced Firmicutes/Bacteroidetes ratio, and increased abundance of beneficial bacteria such as Bifidobacterium. Furthermore, caffeic acid combined with ß-glucan reversed HFD-induced changes in microbiota-derived metabolites involving tryptophan, purine, and bile acid metabolism. Thus, caffeic acid and ß-glucan had a synergistic anti-obesity effect by regulating specific gut microbiota and metabolites.

Injectable plant-derived polysaccharide hydrogels with intrinsic antioxidant bioactivity accelerate wound healing by promoting epithelialization and angiogenesis.

Skin wound healing is a complex and dynamic process involving hemostasis, inflammatory response, cell proliferation and migration, and angiogenesis. Currently used wound dressings remain unsatisfactory in the clinic due to the lack of adjustable mechanical property for injection operation and bioactivity for accelerating wound healing. In this work, an "all-sugar" hydrogel dressing is developed based on dynamic borate bonding network between the hydroxyl groups of okra polysaccharide (OP) and xyloglucan (XG). Benefiting from the reversible crosslinking network, the resulting composite XG/OP hydrogels exhibited good shear-thinning and fast self-healing properties, which is suitable to be injected at wound beds and filled into irregular injured site. Besides, the proposed XG/OP hydrogels showed efficient antioxidant capacity by scavenging DPPH activity of 73.9 %. In vivo experiments demonstrated that XG/OP hydrogels performed hemostasis and accelerated wound healing with reduced inflammation, enhanced collagen deposition and angiogenesis. This plant-derived dynamic hydrogel offers a facile and effective approach for wound management and has great potential for clinical translation in feature.

A water-soluble arabinoxylan from Chinese liquor distillers' grains: Structural characterization and anti-colitic properties.

Chinese liquor distillers' grain (CLDG) is a valuable and abundant by-product from traditional Chinese baijiu production, containing a diverse array of bioactive components that have attracted significant interest. Herein, a water-soluble polysaccharide, DGPS-2B, with a weight-average molecular weight of 37.3 kDa, was isolated from the alkali-extract fraction of CLDG. Methylation and NMR analysis identified that the primary constituents of DGPS-2B are arabinoxylans, with an arabinose-to-xylose ratio of 0.66. In an animal model of colitis, DGPS-2B treatment significantly altered the gut microbiota composition by increasing the SCFA-producing bacteria (e.g., Butyricicoccus) and reducing the mucin-degrading bacteria such as Muribaculaceae. This microbial shift resulted in elevated production of butyrate, acetate, and propionate, which subsequently suppressed NF-κB signaling, decreased the levels of IL-1ß, IL-6, and TNFα, and potentially inactivated Notch signaling. These multifaceted effects stimulated mucin 2 production, reduced inflammation and apoptosis in the gut epithelium, and ultimately alleviated colitis symptoms. Collectively, this study not only elucidates the purification and characterization of DGPS-2B from CLDG but also illuminates its anti-colitic properties and the underlying molecular mechanisms. These findings underscore the potential of DGPS-2B as a therapeutic intervention for managing inflammatory bowel disease and emphasize CLDG as a promising source for developing value-added products.

Toward Enhanced Antioxidant and Protective Potential: Conjugation of Corn Cob Xylan with Gallic Acid as a Novel Approach.

Maize ranks as the second most widely produced crop globally, yielding approximately 1.2 billion tons, with corn cob being its primary byproduct, constituting 18 kg per 100 kg of corn. Agricultural corn production generates bioactive polysaccharide-rich byproducts, including xylan (Xyl). In this study, we used the redox method to modify corn cob xylan with gallic acid, aiming to enhance its antioxidant and protective capacity against oxidative stress. The conjugation process resulted in a new molecule termed conjugated xylan-gallic acid (Xyl-GA), exhibiting notable improvements in various antioxidant parameters, including total antioxidant capacity (1.4-fold increase), reducing power (1.2-fold increase), hydroxyl radical scavenging (1.6-fold increase), and cupric chelation (27.5-fold increase) when compared with unmodified Xyl. At a concentration of 1 mg/mL, Xyl-GA demonstrated no cytotoxicity, significantly increased fibroblast cell viability (approximately 80%), and effectively mitigated intracellular ROS levels (reduced by 100%) following oxidative damage induced by H2O2. Furthermore, Xyl-GA exhibited non-toxicity toward zebrafish embryos, offered protection against H2O2-induced stress, and reduced the rate of cells undergoing apoptosis resulting from H2O2 exposure. In conclusion, our findings suggest that Xyl-GA possesses potential therapeutic value in addressing oxidative stress-related disturbances. Further investigations are warranted to elucidate the molecular structure of this novel compound and establish correlations with its pharmacological activities.

In vitro evaluation of the application of an optimized xylanase cocktail for improved monogastric feed digestibility.

Xylanases from glycoside hydrolase (GH) families 10 and 11 are common feed additives for broiler chicken diets due to their catalytic activity on the nonstarch polysaccharide xylan. This study investigated the potential of an optimized binary GH10 and GH11 xylanase cocktail to mitigate the antinutritional effects of xylan on the digestibility of locally sourced chicken feed. Immunofluorescence visualization of the activity of the xylanase cocktail on xylan in the yellow corn of the feed showed a substantial collapse in the morphology of cell walls. Secondly, the reduction in the viscosity of the digesta of the feed by the cocktail showed an effective degradation of the soluble fraction of xylan. Analysis of the xylan degradation products from broiler feeds by the xylanase cocktail showed that xylotriose and xylopentaose were the major xylooligosaccharides (XOS) produced. In vitro evaluation of the prebiotic potential of these XOS showed that they improved the growth of the beneficial bacteria Streptococcus thermophilus and Lactobacillus bulgaricus. The antibacterial activity of broths from XOS-supplemented probiotic cultures showed a suppressive effect on the growth of the extraintestinal infectious bacterium Klebsiella pneumoniae. Supplementing the xylanase cocktail in cereal animal feeds attenuated xylan's antinutritional effects by reducing digesta viscosity and releasing entrapped nutrients. Furthermore, the production of prebiotic XOS promoted the growth of beneficial bacteria while inhibiting the growth of pathogens. Based on these effects of the xylanase cocktail on the feed, improved growth performance and better feed conversion can potentially be achieved during poultry rearing.

Synthesis and antitumor activity of bagasse xylan derivatives modified by graft-esterification and cross-linking.

A crucial aspect in achieving sustainable development of biomass materials is the modification of renewable polysaccharides to create various high-value functional materials. In this paper, bagasse xylan (BX) was used as a raw material to introduce benzyl methacrylate (BMA) through graft copolymerization reaction to generate the intermediate product BX-g-BMA. Subsequently, the target product (CA-BX-g-BMA) was synthesized by catalytic esterification of BX-g-BMA with citric acid (CA) in AmimCl ionic liquid. Meanwhile, the characterization and bioactivity studies of CA-BX-g-BMA were carried out. The graft copolymerization and esterification reactions induced significant changes in the morphological structure of BX and obviously improved its thermal stability and crystallinity. The application of density functional theory (DFT), molecular electrostatic potential (MEP) and molecular docking has revealed that CA-BX-g-BMA possesses multiple active sites, strong biological activity and a strong binding affinity to 6RCF tumor protein with a binding energy of -32.26 kJ/mol. The in vitro antitumor activity of this novel derivative was tested by MTT assay, and the results showed that CA-BX-g-BMA was non-toxic to normal cells and inhibited MDA-MB-231 (breast cancer cells) by up to 32.16 % ± 4.89 %, which is approximately 11 times higher than that of BX. The exploration of these properties is essential to promote future multidisciplinary applications of BX derivatives.

Purification, characterization and bioactivities of a 4-O-methylglucuronoxylan from Aralia echinocaulis.

The discovery of active constituents from food plants is an important area of research in pharmaceutical sciences. Aralia echinocaulis is a medicinal food plant that is mainly used to prevent or treat rheumatoid arthritis in China. This paper reported the isolation, purification and bioactivity of a polysaccharide (HSM-1-1) from A. echinocaulis. Its structural features were analyzed according to the molecular weight distribution, monosaccharide composition, gas chromatography-mass spectrometry (GC-MS) and nuclear magnetic resonance spectra. The results indicated that HSM-1-1 was a new 4-O-methylglucuronoxylan mainly composed of xylan and 4-O-methyl glucuronic acid with the molecular weight of 1.6 × 104 Da. Furthermore, the antitumor and anti-inflammatory activities of HSM-1-1 in vitro were investigated, and the results showed that HSM-1-1 had potent proliferation inhibition activity on colon cancer cell SW480 with an inhibition rate of 17.57 ± 1.03 % at a concentration of 600 µg/mL, as measured via MTS methods. To our knowledge, this is the first report of a polysaccharide structure obtained from A. echinocaulis and its bioactivities, and its potential as an adjuvant natural product with antitumor effects is shown.

Synthesis and structural characterization of xylan acetate ester and its antinephritic effects in rats with experimental chronic kidney disease.

Acetic acid has been shown to be effective in chronic kidney disease (CKD). However, it is a low-molecular-weight compound that allows it to be absorbed in the upper digestive tract so that it cannot function in colon. To overcome these deficiencies, an acetate-releasing xylan derivative, xylan acetate ester (XylA), was synthesized and selected in this study for its potential in the treatment of CKD. IR, NMR and HPGPC were used to characterize the structure of XylA and its antinephritic effects was evaluated in vivo. The results showed that acetate was successfully grafted onto the C-2 and C-3 positions of xylan and with a molecular weight at 69157 Da. XylA treatments could relieve the symptoms of CKD in an adenine-induced chronic renal failure (CRF) model and an adriamycin-induced focal segmental glomerulosclerosis (FSGS) model in SD rats. Further study indicated that XylA could upregulate the short-chain fatty acids (SCFAs) in vitro and vivo. Nevertheless, the relative abundance of Phascolarctobacterium in colon was increased after XylA treatment. XylA could upregulate G-protein-coupled receptor 41 (GPR41) expression, inhibit glomerular cell apoptosis and promoting proliferation. Our study expands the application of xylan and provides a new idea for the treatment of CKD with acetic acid.

New insight into the mode of action of a GH74 xyloglucanase on tamarind seed xyloglucan: Action pattern and cleavage site.

Structural elucidation of plant cell wall xyloglucan through the analysis of enzymatically produced fragments requires detailed knowledge of enzymes hydrolytic mechanism. In this note, the mode of action and cleavage site of commercial recombinant xyloglucanases (GH74, Paenibacillus sp.) was studied on native and fluorescent-tagged tamarind xyloglucan. In complement to information provided by the manufacturer, GH74 hydrolysis was shown dual endo/exo- and exo-processive with low affinity towards labelled reducing-ends. GH74 accommodated X/G in its subsite -1 and X/L in its subsite +1. Moreover, hydrolysis kinetic indicated a GH74 activity inhibition by excess products. These results will help for application of this enzyme in xyloglucans structural analysis or for processing cell walls.

Dimethylaminoethyl Methacrylate/Diethylene Glycol Dimethacrylate Grafted onto Folate-Esterified Bagasse Xylan/Andrographolide Composite Nanoderivative: Synthesis, Molecular Docking and Biological Activity.

As a biocompatible biomaterial, bagasse xylan (BX) has been widely used in the biomedical field. The low biological activity of andrographolide (AD) restricts its development, so AD with certain anticancer activity is introduced. We use chemical modification methods such as grafting and esterification to improve the biological activity and make a novel anticancer nanomaterial. On the basis of the esterification of a mixture of BX and AD with folic acid (FA), a novel anticancer nanoderivative of bagasse xylan/andrographolide folate-g-dimethylaminoethyl methacrylate (DMAEMA)/diethylene glycol dimethacrylate (DEGDMA) nanoparticles (FA-BX/AD-g-DMAEMA/DEGDMA NPs) was synthesized by introducing DMAEMA and DEGDMA monomers through a graft copolymerization and nanoprecipitation method. The effects of reaction temperature, reaction time, the initiator concentration and the mass ratio of FA-BX/AD to mixed monomers on the grafting rate (GR) were investigated. The structure of the obtained product was characterized by FTIR, SEM, XRD and DTG. Further, molecular docking and MTT assays were performed to understand the possible docking sites with the target proteins and the anticancer activity of the product. The results showed that the GR of the obtained product was 79% under the conditions of the initiator concentration 55 mmol/L, m (FA-BX/AD):m (mixed monomer) = 1:2, reaction temperature 50 °C and reaction time 5 h. The inhibition rate of FA-BX/AD-g-DMAEMA/DEGDMA NPs on human lung cancer cells (NCI-H460) can reach 39.77 ± 5.62%, which is about 7.6 times higher than that of BX. Therefore, this material may have potential applications in the development of anticancer drug or carriers and functional materials.

Combined treatment of xyloglucan derivative hydrogel and anti-C5a receptor antibody in preventing peritoneal adhesion.

Postoperative peritoneal adhesion is a common complication after surgery with high morbidity. In addition to improving surgical operations, medical therapy and physical barriers are the two main ways to prevent postoperative peritoneal adhesion. Satisfactory efficacy is not often obtained by the single antiadhesion method, and the combination of barrier therapy and antiadhesion drugs has attracted more attention. In this study, we first demonstrated that aberrant complement activation was associated with peritoneal injury and inflammatory responses. Correspondingly, blocking the C5a-C5aR axis reaction effectively reduced inflammatory reactions. Therefore, we creatively developed an integrated treatment of xyloglucan derivative (mXG) hydrogel and intravenous anti-C5a receptor antibody (anti-C5aRab) aimed at peritoneal adhesion, and then systematically evaluated the therapeutic efficacy using a sidewall defect-cecum abrasion model in mice. In vitro and in vivo experiments showed that the mXG hydrogel had good biocompatibility and degradability and could serve as a safe anti-adhesion barrier. The results showed that anti-C5aRab treatment could significantly inhibit peritoneal adhesions by reducing neutrophil infiltration and the expression of phosphorylated Smad2. Taken together, the mXG hydrogel integrated with anti-C5aRab showed superior antiadhesion performance and holds promising clinical applications in preventing peritoneal adhesion. STATEMENT OF SIGNIFICANCE: Postoperative peritoneal adhesion is an urgent problem to be solved after surgery. Previously, a biodegradable and thermoreversible xyloglucan derivative (mXG) hydrogel was developed that effectively prevented postoperative peritoneal adhesions, but obvious inflammatory responses and proliferation could still be observed. In addition, aberrant complement activation is associated with a variety of inflammatory diseases. We demonstrated that aberrant complement activation is involved in peritoneal adhesion. In this work, mXG hydrogel and intravenous anti-C5a receptor antibody (anti-C5aRab) were integrated to address peritoneal adhesions. The anti-C5aRab reduced the inflammatory responses. In addition, the mXG hydrogel was easy to use and effectively isolated the wound surface at the local injury site. Overall, this integrated treatment significantly improved the antiadhesion effect.

A xylan from the fresh leaves of Piper betle: Structural characterization and studies of bioactive properties.

A pure water soluble xylan (PS-I) with an average molecular weight ~1.1 × 105 Da was isolated from the hot water extraction of fresh leaves of Piper betle (paan). The xylan was found to be composed of xylose, galactose and methyl galacturonate in a molar ratio of nearly 3:1:1. The repeating unit was composed of a backbone containing three (1 â†’ 4)-α-D-Xylp residues, one of which was branched at O-2 position with the side chain consisting of (1 â†’ 4)-α-D-GalpA6Me and terminal ß-D-Galp residues. This xylan exhibited macrophage, splenocyte, and thymocyte stimulatory activities. In vitro antioxidant studies demonstrated that the xylan has DPPH radical scavenging potential (EC50 = 148 µg/mL), ABTS radical quenching activity (EC50 = 188 µg/mL) and ferrous ions chelating activity (EC50 = 370 µg/mL). These findings elicit the need for further exploration of the xylan as a natural antioxidant and a potent immunostimulating agent.

Dectin-1b activation by arabinoxylans induces trained immunity in human monocyte-derived macrophages.

Arabinoxylans of various structures and sources have shown to possess the ability to induce a range of immune responses in different cell types in vitro and in vivo. Although the underlying mechanisms remain to be fully established, several studies point towards the involvement of activation of pattern recognition receptors (PRRs). Activation of specific PRRs (i.e., Dectin-1 and CR3) has also been shown to play a key role in the induction of a non-specific memory response in innate immune cells, termed 'trained innate immunity'. In the current study, we assessed whether arabinoxylans are also able to induce trained innate immunity. To this end, a range of arabinoxylan preparations from different sources were tested for their physicochemical properties and their capacity to induce innate immune training and resilience. In human macrophages, rice and wheat-derived arabinoxylan preparations induced training and/or resilience effects, the extent depending on fiber particle size and solubility. Using a Dectin-1 antagonist or a CR3 antibody, it was demonstrated that arabinoxylan-induced trained immunity in macrophages is mainly dependent on Dectin-1b. These findings build on previous observations showing the immunomodulatory potential of arabinoxylans as biological response modifiers and open up promising avenues for their use as health promoting ingredients.

Preparation, physicochemical and pharmacological study of 10-hydroxycamptothecin solid dispersion with complexation agent - xylan-nonanoic acid amphiphilic conjugates.

An amphiphilic conjugate of carboxymethyl xylan-nonanoic acid (CX-NA) was synthesized with molecular weight of 38.35 kDa, HLB value of 13.59, and critical micelle concentration of 23.17 µg/ml. CX-NA could efficiently encapsulate the model drug of 10-hydroxycamptothecin (HCPT). The drug loaded amphiphilic conjugate could self-assembled to micelles with an average diameter of 110 nm, zeta potential of -42.88 mV, and drug encapsulation efficiency of 79.8%. In vitro experiments confirmed that the drug-loaded micelles exhibited excellent stability and permeability in the intestinal environment. Transport pathway demonstrated that HCPT was uptake by cells through clathrin-mediated endocytosis. Intestinal in situ absorption study further confirmed CX-NA vehicle could enhance HPCT to transport across intestinal epithelial cells in colonic tissues. Furthermore, the formulation showed excellent anti-tumor activity in vitro and improved bioavailability of 3.4 times in vivo as comparing with free HCPT. These findings imply that this amphiphilic conjugate is a potential and promising vehicle for delivery anticancer drug.

Feruloylated arabinoxylan from wheat bran inhibited M1-macrophage activation and enhanced M2-macrophage polarization.

The effects of feruloylated arabinoxylan (AX) on typically activated inflammatory macrophages (M1) and alternatively anti-inflammatory macrophages (M2) and its possible mechanisms were investigated. The results revealed that feruloylated AX was composed of 37.63% arabinose and 52.23% xylose, with a weight-average molecular weight of 1.1374 × 104 Da, and bound ferulic acid content of 10.84 mg/g. Besides, feruloylated AX (50-1000 µg/mL) markedly downregulated the mRNA expressions of NO, IL-1ß, TNF-α, IL-6, and IL-23a, and reduced the phosphorylation levels of p38, ERK, and JNK in M1. In contrast, the mRNA expressions of Arg-1, Mrc-1, and CCL22 were significantly upregulated by feruloylated AX (50-1000 µg/mL), and the phosphorylation level of AKT was significantly increased in M2. Overall, our results indicated that feruloylated AX could have an inhibitory or a promoting effect on already activated macrophages, and MAPK or PI3K signaling pathways might be involved in this regulation.

Bamboo shavings derived O-acetylated xylan alleviates loperamide-induced constipation in mice.

BSH-1 is an O-acetylated xylan obtained from bamboo shavings. This study determined the protective effects of BSH-1 against loperamide (Lop)-induced constipation in mice. Mice received BSH-1 by gavage daily for 14 days. In constipated mice, BSH-1 significantly shortened the defecation time and raised the gastrointestinal (GI) transit rate, stool production, and cecal concentration of short-chain fatty acids (SCFAs). BSH-1 regulated the serum levels of gut hormones and neurotransmitters. BSH-1 also significantly altered the cecal microbiota of the constipated mice by increasing the abundance of potentially beneficial bacteria (e.g., Lactobacillus, Roseburia, and Bacteroidales_S24-7) and decreasing potentially pathogenic bacteria (e.g., Alloprevotella and Staphylococcus). Furthermore, colonic transcriptome analysis revealed that BSH-1 significantly reversed the expression changes of genes related to intestinal motility, water and ion transport, inflammation and cancer in constipated mice. Our findings indicated that BSH-1 effectively relieved Lop-induced constipation in mice and could be potentially used for constipation treatment.