bluuebunny/crossref_metadata_2025 huggingface dataset:
Oral Administration of Recombinant Lactoferrin-Expressing Probiotics Ameliorates Diet-Induced Lipid Accumulation and Inflammation in Non-Alcoholic Fatty Liver Disease in Mice
Authors: Liu Zhen-Shu , Li Pei-Lin , Ku Yu-We , Chen Po-Wen
Published: November 2022

We have recently developed probiotics that can express bovine, human, or porcine lactoferrin (LF), and the present study evaluated the effect of these probiotics in improving non-alcoholic fatty liver disease (NAFLD). Three kinds of probiotic supplements, including lactic acid bacteria (LAB), LAB/LF, and inactivated LAB/LF, were prepared. The LAB supplement was prepared from 10 viable LAB without recombinant LF-expression, the LAB/LF supplement was prepared from 10 viable probiotics expressing LF, and the inactivated LAB/LF supplement was prepared from 10 inactivated probiotics expressing LF. A model of obese/NAFLD mice induced by a high-fat diet was established, and the mice were randomly divided into four groups and fed with a placebo, LAB, LAB/LF, or inactivated LAB daily for four weeks via oral gavage. The body weight, food intake, organ weight, biochemistry, and hepatic histopathological alterations and severity scoring were measured. The results revealed that the obese mice fed with any one of the three probiotic mixtures prepared from recombinant probiotics for four weeks exhibited considerably improved hepatic steatosis. These findings confirmed the assumption that specific probiotic strains or LF supplements could help to control NAFLD, as suggested in previous reports. Our data also suggest that the probiotics and LFs in probiotic mixtures contribute differently to improving the efficacy against NAFLD, and the expressed LF content in probiotics may help to boost their efficacy in comparison with the original probiotic mixtures. Moreover, when these LF-expressing probiotics were further inactivated by sonication, they displayed better efficacies than the viable probiotics against NAFLD. This study has provided intriguing data supporting the potential of recombinant probiotics in improving hepatic steatosis.
Single-Cell-Based High-Throughput Cultivation and Functional Characterization of Biosurfactant-Producing Bacteria from Soil and Oilfield-Produced Water
Authors: Xu Ying , Jing Yali , Zhang Yaqian , Liu Qingjie , Xiu Jianlong , Zhang Ke , Jia Ninghong , Zhou Minghui , Zhou Xinyu , Huang Jia , Nie Yong , Wu Xiao-Lei
Published: November 2022

Biosurfactants are a group of surface-active compounds that can be produced by diverse microorganisms. They have been widely used in various industrial fields. Reducing production costs, improving efficiency, and collecting more diverse producing strains have become major challenges in the biosurfactant industry. These challenges could be overcome by screening for more diverse and efficient biosurfactant-producing strains. The conventional methods for the isolation and functional characterization of microorganisms are laborious and biased toward fast-growing or strongly competitive microorganisms. Here, we established a high-throughput approach of single-cell-based cultivation and functional characterization of biosurfactant-producing bacteria (SCCBB). This approach combines single-cell cultivation with the detection of optical distortions. Using this approach, we isolated 431 strains with biosurfactant production potential from petroleum-contaminated soil and oilfield-produced water. The surfactant production capabilities of the strains were subsequently validated using surface tension measurements, TLC, and CMC measurements. To investigate the industrial production potential, we optimized the production conditions of a representative glycolipids-producing strain, Pseudomonas sp. L01, using response surface methodology (RSM). Optimal conditions yielded a crude biosurfactant yield of 8.43 g/L in a flask. Our work provides a high-throughput approach to the isolation and screening of biosurfactant-producing bacteria, as well as other functional bacteria in a wide range of fields.
Parthenium hysterophorus’s Endophytes: The Second Layer of Defense against Biotic and Abiotic Stresses
Authors: Khan Asif , Ali Sajid , Khan Murtaza , Hamayun Muhammad , Moon Yong-Sun
Published: November 2022

Parthenium hysterophorus L. is considered an obnoxious weed due to its rapid dispersal, fast multiplications, and agricultural and health hazards. In addition to its physio-molecular and phytotoxic allelochemical usage, this weed most probably uses endophytic flora as an additional line of defense to deal with stressful conditions and tolerate both biotic and abiotic stresses. The aim of this article is to report the diversity of endophytic flora (fungi and bacteria) in P. hysterophorus and their role in the stress mitigation (biotic and abiotic) of other important crops. Various endophytes were reported from P. hysterophorus and their roles in crops evaluated under biotic and abiotic stressed conditions. These endophytes have the potential to alleviate different stresses by improving crops/plants growth, development, biomass, and photosynthetic and other physiological traits. The beneficial role of the endophytes may be attributed to stress-modulating enzymes such as the antioxidants SOD, POD and APX and ACC deaminases. Additionally, the higher production of different classes of bioactive secondary metabolites, i.e., flavonoids, proline, and glutathione may also overcome tissue damage to plants under stressed conditions. Interestingly, a number of medicinally important phytochemicals such as anhydropseudo-phlegmcin-9, 10-quinone-3-amino-8-O methyl ether ‘anhydropseudophlegmacin-9, 10-quinone-3-amino-8-O methyl ether were reported from the endophytic flora of P. hysterophorus. Moreover, various reports revealed that fungal and bacterial endophytes of P. hysterophorus enhance plant growth-promoting attributes and could be added to the consortium of biofertilizers.
Safety Evaluation by Phenotypic and Genomic Characterization of Four Lactobacilli Strains with Probiotic Properties
Authors: Lee Ye-Rim , Bang Won Yeong , Baek Kwang-Rim , Kim Geun-Hyung , Kang Min-Ji , Yang Jungwoo , Seo Seung-Oh
Published: November 2022

Probiotic Lactobacillus species are known to exert health benefits in hosts when administered in adequate quantities. A systematic safety assessment of the strains must be performed before the Lactobacillus strains can be designated as probiotics for human consumption. In this study, we selected Lactobacillus fermentum IDCC 3901, L. gasseri IDCC 3101, L. helveticus IDCC 3801, and L. salivarius IDCC 3551 as representative Lactobacilli probiotic strains and investigated their probiotic properties and potential risks through phenotypic and genomic characterization. Various assays including antimicrobial resistance, biogenic amine production, L-/D-lactate production, acute oral toxicity, and antipathogenic effect were performed to evaluate the safety of the four Lactobacillus strains. Genomic analysis using whole genome sequencing was performed to investigate virulence and antibiotic resistance genes in the genomes of the selected probiotic strains. The phenotypes of the strains such as enzymatic activity and carbohydrate utilization were also investigated. As a result, antibiotic resistances of the four Lactobacillus species were detected; however, neither antibiotic resistance-related genes nor virulence genes were found by genomic analysis. Moreover, the four Lactobacillus species did not exhibit hemolytic activity or β-glucuronidase activity. The biogenic amine production and oral acute toxicity were not shown in the four Lactobacillus species, whereas they produced D-lactate with minor ratio. The four Lactobacillus species exhibited antipathogenic effect to five pathogenic microorganisms. This study provides a way to assess the potential risks of four different Lactobacillus species and validates the safety of all four strains as probiotics for human consumption.
Higher-Quality Pumpkin Cultivars Need to Recruit More Abundant Soil Microbes in Rhizospheres
Authors: Sun Yan , Huang Ziyue , Chen Siyu , Yang Da , Lin Xinru , Liu Wenjun , Yang Shangdong
Published: November 2022

Two different qualities of pumpkin, cultivars G1519 and G1511, were grown in the same environment under identical management. However, their qualities, such as the contents of total soluble solids, starch, protein, and vitamin C, were significantly different. Do rhizospheric microbes contribute to pumpkin quality? To answer this question, this study investigated the soil microbial compositions in the rhizospheres of different quality pumpkin cultivars to determine the differences in these soil microbial compositions and thus determine how soil microbes may affect pumpkin quality. Firstly, a randomized complete block design with two pumpkin cultivars and three replications was performed in this study. The soil microbial compositions and structures in the rhizospheres of the two pumpkin cultivars were analyzed using a high-throughput sequencing technique. In comparison with the low-quality pumpkin cultivar (G1519), higher microbial diversity and richness could be found in the rhizospheres of the high-quality pumpkin cultivar (G1511). The results showed that there were significant differences in the soil bacterial and fungal community compositions in the rhizospheres of the high- and low-quality pumpkin cultivars. Although the compositions and proportions of microorganisms were similar in the rhizospheres of the two pumpkin cultivars, the proportions of Basidiomycota and Micropsalliota in the G1519 rhizosphere were much higher than those in the G1511 rhizosphere. Furthermore, the fungal phylum and genus Rozellomycota and Unclassified_p__Rozellomycota were unique in the rhizosphere of the high-quality pumpkin cultivar (G1511). All the above results indicate that soil microbes were enriched differentially in the rhizospheres of the low- and high-quality pumpkin cultivars. In other words, more abundant soil microbes were recruited in the rhizosphere of the high-quality pumpkin cultivar as compared to that of the low-quality cultivar. Rozellomycota and Unclassified_p__Rozellomycota may be functional microorganisms relating to pumpkin quality.
Variations in Antioxidant Capacity, Oxidative Stability, and Physicochemical Quality Parameters of Walnut (Juglans regia) Oil with Roasting and Accelerated Storage Conditions
Authors: Elouafy Youssef , El Idrissi Zineb , El Yadini Adil , Harhar Hicham , Alshahrani Mohammed , AL Awadh Ahmed , Goh Khang , Ming Long , Bouyahya Abdelhakim , Tabyaoui Mohamed
Published: November 2022

Walnut oil, like all vegetable oils, is chemically unstable because of the sensitivity of its unsaturated fatty acids to the oxidation phenomenon. This phenomenon is based on a succession of chemical reactions, under the influence of temperature or storage conditions, that always lead to a considerable change in the quality of the oil by promoting the oxidation of unsaturated fatty acids through the degradation of their C–C double bonds, leading to the formation of secondary oxidation products that reduce the nutritional values of the oil. This research examines the oxidative stability of roasted and unroasted cold-pressed walnut oils under accelerated storage conditions. The oxidative stability of both oils was evaluated using physicochemical parameters: chemical composition (fatty acids, phytosterols, and tocopherols), pigment content (chlorophyll and carotenoids), specific extinction coefficients (K232 and K270), and quality indicators (acid and peroxide value) as well as the evaluation of radical scavenging activity by the DPPH method. The changes in these parameters were evaluated within 60 days at 60 ± 2 °C. The results showed that the levels of total phytosterols, the parameters of the acid and peroxide value, K232 and K270, increased slightly for both oils as well as the total tocopherol content and the antioxidant activity affected by the roasting process. In contrast, the fatty acid profiles did not change considerably during the 60 days of our study. After two months of oil treatment at 60 °C, the studied oils still showed an excellent physicochemical profile, which allows us to conclude that these oils are stable and can withstand such conditions. This may be due to the considerable content of tocopherols (vitamin E), which acts as an antioxidant.
Natural Hemp-Ginger Extract and Its Biological and Therapeutic Efficacy
Authors: Žitek Taja , Bjelić Dragana , Kotnik Petra , Golle Andrej , Jurgec Staša , Potočnik Uroš , Knez Željko , Finšgar Matjaž , Krajnc Ivan , Krajnc Igor , Marevci Maša Knez
Published: November 2022

The prevention and treatment of skin diseases remains a major challenge in medicine. The search for natural active ingredients that can be used to prevent the development of the disease and complement treatment is on the rise. Natural extracts of ginger and hemp offer a wide range of bioactive compounds with potential health benefits. This study evaluates the effectiveness of hemp and ginger extract as a supportive treatment for skin diseases. It reports a synergistic effect of hemp and ginger extract. The contents of cannabinoids and components of ginger are determined, with the highest being CBD (587.17 ± 8.32 µg/g) and 6-gingerol (60.07 ± 0.40 µg/g). The minimum inhibitory concentration for Staphylococcus aureus (156.5 µg/mL), Escherichia coli (625.2 µg/mL) and Candida albicans (78.3 µg/mL) was also analyzed. Analysis of WM-266-4 cells revealed the greatest decrease in metabolic activity in cells exposed to the extract at a concentration of 1.00 µg/mL. Regarding the expression of genes associated with cellular processes, melanoma aggressiveness, resistance and cell survival, a significant difference was found in the expression of ABCB5, CAV1 and S100A9 compared with the control (cells not exposed to the extract).
Simultaneous Enantiodivergent Synthesis of Diverse Lactones and Lactams via Sequential One-Pot Enzymatic Kinetic Resolution–Ring-Closing Metathesis Reactions
Authors: Brodzka Anna , Koszelewski Dominik , Ostaszewski Ryszard
Published: November 2022

One of the goals of diversity-oriented synthesis is to achieve the structural diversity of obtained compounds. As most biologically active compounds are chiral, it is important to develop enantioselective methods of their synthesis. The application of kinetic resolution in DOS is problematic because of low efficiency (max. 50% yield) and many purification steps. The further derivatization of kinetic resolution products in DOS leads to the formation of a narrow library of compounds of the same stereochemistry. To overcome these limitations, we present a new concept in which the kinetic resolution is combined, the subsequent reaction of which in a one-pot protocol leads to the simultaneous formation of two skeletally and enantiomerically diverse platform molecules for DOS. Their further derivatization can gain access to a double-sized library of products in respect to a classical approach. The validity of our concept was evidenced in enzymatic kinetic resolution followed by a ring-closing metathesis cascade. From racemic carboxylic acid ester, a simultaneous formation of enantiopure lactones and lactams was achieved. These compounds are important building blocks in organic and medicinal chemistry and until now were synthesized in separate procedures.
Double Perovskite Mn4+-Doped La2CaSnO6/La2MgSnO6 Phosphor for Near-Ultraviolet Light Excited W-LEDs and Plant Growth
Authors: Lu Zheng , Sun Dashuai , Lyu Zeyu , Shen Sida , Wang Jianhui , Zhao Hanwei , Wang Lixuan , You Hongpeng
Published: November 2022

Non-rare earth doped oxide phosphors with far-red emission have become one of the hot spots of current research due to their low price and excellent physicochemical stability as the red component in white light-emitting diodes (W-LEDs) and plant growth. Herein, we report novel Mn4+-doped La2CaSnO6 and La2MgSnO6 phosphors by high-temperature solid-phase synthesis and analyzed their crystal structures by XRD and Rietveld refinement. Their excitation spectra consist of two distinct excitation bands with the dominant excitation range from 250 to 450 nm, indicating that they possess strong absorption of near-ultraviolet light. Their emission is located around 693 and 708 nm, respectively, and can be absorbed by the photosensitive pigments Pr and Pfr, proving their great potential for plant growth. Finally, the prepared samples were coated with 365 nm UV chips to fabricate far-red LEDs and W-LEDs with low correlation color temperature (CCT = 4958 K/5275 K) and high color rendering index (Ra = 96.4/96.6). Our results indicate that La2CaSnO6:Mn4+ and La2MgSnO6:Mn4+ red phosphors could be used as candidate materials for W-LED lighting and plant growth.
Applications of Deep Eutectic Solvents in Sample Preparation and Extraction of Organic Molecules
Authors: Plastiras Orfeas-Evangelos , Samanidou Victoria
Published: November 2022

The use of deep eutectic solvents (DES) is on the rise worldwide because of the astounding properties they offer, such as simplicity of synthesis and utilization, low-cost, and environmental friendliness, which can, without a doubt, replace conventional solvents used in heaps. In this review, the focus will be on the usage of DES in extracting a substantial variety of organic compounds from different sample matrices, which not only exhibit great results but surpass the analytical performance of conventional solvents. Moreover, the properties of the most commonly used DES will be summarized.
Effect of Structured Phenolic Lipids with EPA/DHA and Gallic Acid against Metabolic-Associated Fatty Liver Disease (MAFLD) in Mice
Authors: Dovale-Rosabal Gretel , Espinosa Alejandra , Rodríguez Alicia , Barriga Andrés , Palomino-Calderón Alan , Romero Nalda , Troncoso Rodrigo Hernán , Aubourg Santiago Pedro
Published: November 2022

Obesity is the leading risk factor for developing metabolic (dysfunction)-associated fatty liver disease (MAFLD). The food industry has an essential role in searching for new strategies to improve primary food sources to revert some of the metabolic alterations induced by obesity. There is consistent evidence that long-chain polyunsaturated fatty acids (n-3 LCPUFA) belonging to the n-3 series, i.e., eicosapentaenoic (20:5n-3, EPA) and docosahexaenoic (22:6n-3, DHA) acids, could revert some alterations associated with obesity-induced metabolic diseases. A relevant tool is the synthesis of structured acylglycerols (sAG), which include EPA or DHA at the sn-2 position. On the other hand, it has been reported that a crucial role of antioxidants is the reversion of MAFLD. In this work, we studied the effects of new molecules incorporating gallic acid (GA) into EPA/DHA-rich structured lipids. Mice were fed with a high-fat diet (60%) for three months and were then divided into five groups for supplementation with sAG and sAG structured with gallic acid (structured phenolic acylglycerols, sPAG). sPAG synthesis was optimized using a 2²-screening factorial design based on the response surface methodology (RSM). Our results show that treatment of sPAG was effective in decreasing visceral fat, fasting glycemia, fasting insulin, suggesting that this new molecule has a potential use in the reversal of MAFLD-associated alterations.
Carbonic Anhydrase Inhibition Activities of Schiff’s Bases Based on Quinazoline-Linked Benzenesulfonamide
Authors: El-Azab Adel S. , Abdel-Aziz Alaa A.-M. , Ghabbour Hazem A. , Bua Silvia , Nocentini Alessio , Alkahtani Hamad M. , Alsaif Nawaf A. , Al-Agamy Mohamed H. M. , Supuran Claudiu T.
Published: November 2022

Human carbonic anhydrase (CA, EC 4.2.1.1) (hCA) isoforms I, II, IX, and XII were investigated for their inhibitory activity with a series of new Schiff’s bases based on quinazoline scaffold 4–27. The hCA I isoform was efficiently inhibited by Schiff’s bases 4–6, 10–19, 22–27 and had an inhibition constant (Ki) value of 52.8–991.7 nM compared with AAZ (Ki, 250 nM). Amongst the quinazoline derivatives, the compounds 2, 3, 4, 10, 11, 16, 18, 24, 26, and 27 were proven to be effective hCA II inhibitors, with Ki values of 10.8–52.6 nM, measuring up to AAZ (Ki, 12 nM). Compounds 2–27 revealed compelling hCA IX inhibitory interest with Ki values of 10.5–99.6 nM, rivaling AAZ (Ki, 25.0 nM). Quinazoline derivatives 3, 10, 11, 13, 15–19, and 24 possessed potent hCA XII inhibitory activities with KI values of 5.4–25.5 nM vs. 5.7 nM of AAZ. Schiff’s bases 7, 8, 9, and 21 represented attractive antitumor hCA IX carbonic anhydrase inhibitors (CAIs) with KI rates (22.0, 34.8, 49.2, and 45.3 nM, respectively). Compounds 5, 7, 8, 9, 14, 18, 19, and 21 showed hCA I inhibitors on hCA IX with a selectivity index of 22.46–107, while derivatives 12, 14, and 18 showed selective hCA I inhibitors on hCA XII with a selectivity profile of 45.04–58.58, in contrast to AAZ (SI, 10.0 and 43.86). Compounds 2, 5, 7–14, 19–23, and 25 showed a selectivity profile for hCA II inhibitors over hCA IX with a selectivity index of 2.02–19.67, whereas derivatives 5, 7, 8, 13, 14, 15, 17, 20, 21, and 22 showed selective hCA II inhibitors on hCA XII with a selectivity profile of 4.84–26.60 balanced to AAZ (SI, 0.48 and 2.10).
Synthesis and Characterisation of Novel Bis(diphenylphosphane oxide)methanidoytterbium(III) Complexes
Authors: Rangarajan Shalini , Beaumont Owen A. , Balakrishna Maravanji S. , Deacon Glen B. , Blair Victoria L.
Published: November 2022

Reaction of [YbCp2(dme)] (Cp = cyclopentadienyl, dme = 1,2 dimethoxyethane) with bis(diphenylphosphano)methane dioxide (H2dppmO2) leads to deprotonation of the ligand H2dppmO2 and oxidation of ytterbium, forming an extremely air-sensitive product, [YbIII(HdppmO2)3] (1), a six-coordinate complex with three chelating (OPCHPO) HdppmO2 ligands. Complex 1 was also obtained by a redox transmetallation/protolysis synthesis from metallic ytterbium, Hg(C6F5)2, and H2dppmO2. In a further preparation, the reaction of [Yb(C6F5)2] with H2dppmO2, not only yielded compound 1, but also gave a remarkable tetranuclear cage, [Yb4(µ-HdppmO2)6(µ-F)6] (2) containing two [Yb(µ-F)]2 rhombic units linked by two fluoride ligands and the tetranuclear unit is encapsulated by six bridging HdppmO2 donors. The fluoride ligands of the cage result from C-F activation of pentafluorobenzene and concomitant formation of p-H2C6F4 and m-H2C6F4, the last being an unexpected product.
Intrafibrillar Dispersion of Cuprous Oxide (Cu2O) Nanoflowers within Cotton Cellulose Fabrics for Permanent Antibacterial, Antifungal and Antiviral Activity
Authors: Hillyer Matthew B. , Nam Sunghyun , Condon Brian D.
Published: November 2022

With increasingly frequent highly infectious global pandemics, the textile industry has responded by developing commercial fabric products by incorporating antibacterial metal oxide nanoparticles, particularly copper oxide in cleaning products and personal care items including antimicrobial wipes, hospital gowns and masks. Current methods use a surface adsorption method to functionalize nanomaterials to fibers. However, this results in poor durability and decreased antimicrobial activity after consecutive launderings. In this study, cuprous oxide nanoparticles with nanoflower morphology (Cu2O nanoflowers) are synthesized in situ within the cotton fiber under mild conditions and without added chemical reducing agents from a copper (II) precursor with an average maximal Feret diameter of 72.0 ± 51.8 nm and concentration of 17,489 ± 15 mg/kg. Analysis of the Cu2O NF-infused cotton fiber cross-section by transmission electron microscopy (TEM) confirmed the internal formation, and X-ray photoelectron spectroscopy (XPS) confirmed the copper (I) reduced oxidation state. An exponential correlation (R2 = 0.9979) between the UV-vis surface plasmon resonance (SPR) intensity at 320 nm of the Cu2O NFs and the concentration of copper in cotton was determined. The laundering durability of the Cu2O NF-cotton fabric was investigated, and the superior nanoparticle-leach resistance was observed, with the fabrics releasing only 19% of copper after 50 home laundering cycles. The internally immobilized Cu2O NFs within the cotton fiber exhibited continuing antibacterial activity (≥99.995%) against K. pneumoniae, E. coli and S. aureus), complete antifungal activity (100%) against A. niger and antiviral activity (≥90%) against Human coronavirus, strain 229E, even after 50 laundering cycles.
Effects of Extraction Methods on the Bioactivities and Nutritional Value of Virginia and Valencia-Type Peanut Oil
Authors: Idrissi Zineb Lakhlifi El , El Moudden Hamza , Mghazli Najoua , Bouyahya Abdelhakim , Guezzane Chakir El , Alshahrani Mohammed Merae , Al Awadh Ahmed Abdullah , Goh Khang Wen , Ming Long Chiau , Harhar Hicham , Tabyaoui Mohamed
Published: November 2022

This study aimed to evaluate the effects of peanut varieties cultivated in Morocco (Virginia and Valencia) and extraction methods (cold press, CP; Soxhlet, Sox and maceration, and Mac) on the fatty acid profile, phytosterol, and tocopherol contents, quality characteristics, and antioxidant potential of peanut seed oil. The DPPH method was used to determine the antioxidant activity of the oils. The results revealed that fatty acid content was slightly affected by the extraction technique. However, the CP method was shown to be an excellent approach for extracting oil with desirable quality features compared to the Sox and Mac methods. Furthermore, the peanut oil extracted via CP carried a higher amount of bioactive compounds and exhibited remarkable antioxidant activities. The findings also revealed higher oleic acid levels from the Virginia oil, ranging from 56.46% to 56.99%. Besides, a higher total phytosterol and tocopherol content and DPPH scavenging capacity were obtained from the Valencia oil. Analyzing the study, it can be inferred that extraction method and variety both affect the composition of the peanut oil’s bioactive compounds and antioxidant activity. This information is relevant for extracting peanut oil with a greater level of compounds of industrial interest.
Interaction of Destruxin A with Three Silkworm Proteins: BmCRT, BmDPP3, and BmPDIA5
Authors: Yin Xuyu , Peng Haitao , Weng Qunfang , Hu Qiongbo , Wang Jingjing
Published: November 2022

Destruxin A (DA), a hexa-cyclodepsipeptidic mycotoxin produced by the entomopathogenic fungus Metarhizium anisopliae, has insecticidal activity, but its molecular mechanism of action is still not clear. Three proteins with modification-related functions, calreticulin (BmCRT), dipeptidyl peptidase Ⅲ (BmDPP3), and protein disulfide isomerase A5 (BmPDIA5), were selected to verify the interactions with DA in this study. The kinetic data of the interactions were measured by surface plasmon resonance (SPR) and bio-layer interferometry (BLI) in vitro. The KD values of DA with BmCRT, BmDPP3, and BmPDIA5 ranged from 10−4 to 10−5 mol/L, which suggested that the three proteins all had fairly strong interactions with DA. Then, it was found that DA in a dose-dependent manner affected the interactions of the three proteins with their partners in insect two-hybrid tests in SF-9 cells. Furthermore, the results of enzyme activities by ELISA indicated that DA could inhibit the activity of BmDPP3 but had no significant effect on BmPDIA5. In addition, DA induced the upregulation of BmDPP3 and the downregulation of BmCRT. The results prove that BmCRT, BmDPP3, and BmPDIA5 are all binding proteins of DA. This study might provide new insights to elucidate the molecular mechanism of DA.
Integration of Two-Dimensional Liquid Chromatography-Mass Spectrometry and Molecular Docking to Characterize and Predict Polar Active Compounds in Curcuma kwangsiensis
Authors: Xiang Kaijing , Zhou Weijia , Hou Tao , Yu Long , Zhou Han , Zhou Liangliang , Liu Yanfang , Wang Jixia , Guo Zhimou , Liang Xinmiao
Published: November 2022

Curcuma kwangsiensis, one species of Curcumae zedoaria Ros. c, is a commonly used traditional Chinese medicine (TCM) for treating cardiovascular disease, cancer, asthma and inflammation. Polar compounds are abundant in water decoction, which would be responsible for critical pharmacological effects. However, current research on polar compounds in Curcumae zedoaria Ros. c remains scarce. In this study, the polar fraction from Curcuma kwangsiensis was firstly profiled on G protein-coupled receptor 109A (GPR109A), β2-adrenergic receptor (β2-AR), neurotensin receptor (NTSR), muscarinic-3 acetylcholine receptor (M3) and G protein-coupled receptor 35 (GPR35), which were involved in its clinical indications and exhibited excellent β2-AR and GPR109A receptor activities. Then, an offline two-dimensional reversed-phase liquid chromatography (RPLC) coupled with the hydrophilic interaction chromatography (HILIC) method was developed to separate polar compounds. By the combination of a polar-copolymerized XAqua C18 column and an amide-bonded XAmide column, an orthogonality of 47.6% was achieved. As a result of coupling with the mass spectrometry (MS), a four-dimensional data plot was presented in which 373 mass peaks were detected and 22 polar compounds tentatively identified, including the GPR109A agonist niacin. Finally, molecular docking of these 22 identified compounds to β2-AR, M3, GPR35 and GPR109A receptors was performed to predict potential active ingredients, and compound 9 was predicted to have a similar interaction to the β2-AR partial agonist salmeterol. These results were supplementary to the material basis of Curcuma kwangsiensis and facilitated the bioactivity research of polar compounds. The integration of RPLC×HILIC-MS and molecular docking can be a powerful tool for characterizing and predicting polar active components in TCM.
Optimization of κ-Selenocarrageenase Production by Pseudoalteromonas sp. Xi13 and Its Immobilization
Authors: Deng Yashan , Wang Xixi , Xu Hui , Liu Cui , Li Ran , Zhang Yuanyuan , Qu Changfeng , Miao Jinlai
Published: November 2022

The bioenzymatic production of selenium oligosaccharides addresses the problems resulting from high molecular weight and poor water solubility of κ-selenocarrageenan, and lays foundation for its application as adjuvant drugs for cancer treatment and food additive. κ-selenocarrageenase extracted from Pseudoalteromonas sp. Xi13 can degrade κ-selenocarrageenan to selenium oligosaccharides. The maximum optimized κ-selenocarrageenase activity using Response Surface Methodology (RSM) was increased by 1.4 times, reaching 8.416 U/mL. To expand applications of the κ-selenocarrageenase in industry, the preparation conditions of it in either lyophilized or immobilized form were investigated. The activity recovery rate of the lyophilized enzyme was >70%, while that of the immobilized enzyme was 62.83%. However, the immobilized κ-selenocarrageenase exhibits good stability after being reused four times, with 58.28% of residual activity. The selenium content of κ-selenocarrageenan oligosaccharides degraded by the immobilized κ-selenocarrageenase was 47.06 µg/g, 8.3% higher than that degraded by the lyophilized enzyme. The results indicate that the immobilized κ-selenocarrageenase is suitable for industrial applications and has commercial potential.
Cellular Antioxidant Properties of Ischnoderma Resinosum Polysaccharide
Authors: Liao Caiyu , Wu Liyan , Zhong Wenting , Zheng Qinhua , Tan Weijian , Feng Kexin , Feng Xiaolin , Meng Fanxin
Published: November 2022

A predominant polysaccharide isolated from Ischnoderma resinosum underwent evaluation for its capacity to scavenge free radicals and its potential antioxidant properties at a cellular-oriented level. This proved that Ischnoderma resinosum polysaccharide (IRP) remarkably curtailed AAPH-induced erythrocyte hemolysis through the inhibition of the generation of ROS (p < 0.05). Rather, it caused the restoration of intracellular antioxidant enzyme (SOD, GSH-Px, and CAT) activities at an acceptable pace and the silencing of intracellular MDA formation, as well as the rescaling of LDH leakage. Furthermore, a model of oxidative stress in HepG2 cells was established by adopting 400 μM of hydrogen peroxide, which suggested that IRP manifests promising antioxidant activity. Notably, after the intervention of IRP in the H2O2-induced HepG2 cells, there was a statistical elevation in cell survivability (p < 0.05). IRP diminished the morphological alterations in the nucleus and decreased the secretion of ROS (p < 0.05), with a dose-dependent abrogation of apoptosis (p < 0.05). Consequently, IRP, which was isolated and purified, was able to scavenge free radicals and possessed favorable antioxidant activity that could dampen the occurrence of oxidative stimulation and effectively alleviate the AAPH-induced erythrocyte hemolysis and H2O2-induced oxidative damage in HepG2 cells. This provides a basis and theoretical reference for the development and utilization of IRP as a natural antioxidant, with emphasis on the exploitation of environmentally friendly and cost-effective antioxidants.
Identification of Antiviral Compounds against Monkeypox Virus Profilin-like Protein A42R from Plantago lanceolata
Authors: Bajrai Leena H. , Alharbi Azzah S. , El-Day Mai M. , Bafaraj Abrar G. , Dwivedi Vivek Dhar , Azhar Esam I.
Published: November 2022

Infections caused by the monkeypox virus (MPXV) have continued to be transmitted significantly in recent years. However, understanding the transmission mechanism, risk factors, and consequences of infection are still limited. Structure-based drug design for MPXV is at an early stage due to the availability of protein structures that have been determined experimentally. However, the structure of the A42R profilin-like protein of MPXV has been solved and submitted to the structure database. This study illustrated an in silico structure-based approach to identify the potential hit compound against A42R of MPXV. Here, 65 Plantago lanceolata compounds were computationally screened against A42R of MPXV. Virtual screening identified top five hits (i) Luteolin 7,3′-Diglucuronide (PubChem ID: 44258091), (ii) Luteolin 7-Glucuronide-3′-Glucoside (PubChem ID: 44258090), (iii) Plantagoside (PubChem ID: 174157), (iv) Narcissoside (PubChem ID: 5481663), and (v) (AlphaE,8S,9R)-N-(3,4-Dihydroxyphenethyl)-8-[(3,4-Dihydroxyphenethyl)Carbamoyl]-9-(1,3-Benzodioxole-5-Yl)-3aalpha,7aalpha-Ethano-1,3-Benzodioxole-5-Acrylamide (PubChem ID: 101131595), with binding energy <−9.0 kcal/mol that was further validated by re-docking and molecular dynamic (MD) simulation. Interaction analysis of re-docked poses confirmed the binding of these top hits to the A42R protein as reported in the reference compound, including active residues ARG114, ARG115, and ARG119. Further, MD simulation and post-simulation analysis support Plantagoside and Narcissoside for substantial stability in the binding pocket of viral protein contributed by hydrogen and hydrophobic interactions. The compounds can be considered for further optimisation and in vitro experimental validation for anti-monkeypox drug development.
(E)-N-(3-(1-(2-(4-(2,2,2-Trifluoroacetamido)benzoyl)hydrazono)ethyl)phenyl)nicotinamide: A Novel Pyridine Derivative for Inhibiting Vascular Endothelial Growth Factor Receptor-2: Synthesis, Computational, and Anticancer Studies
Authors: Yousef Reda G. , Elkady Hazem , Elkaeed Eslam B. , Gobaara Ibraheem M. M. , Al-ghulikah Hanan A. , Husein Dalal Z. , Ibrahim Ibrahim M. , Metwaly Ahmed M. , Eissa Ibrahim H.
Published: November 2022

(E)-N-(3-(1-(2-(4-(2,2,2-Trifluoroacetamido)benzoyl)hydrazono)ethyl)phenyl)nicotinamide (compound 10) was designed as an antiangiogenic VEGFR-2 inhibitor with the essential pharmacophoric structural properties to interact with the catalytic pocket of VEGFR-2. The designed derivative was synthesized, and its structure was confirmed through Ms, elemental, 1H, and 13C spectral data. The potentiality of the designed pyridine derivative to bind with and inhibit the vascular endothelial growth factor receptor-2 (VEGFR-2) enzyme was indicated by molecular docking assessments. In addition, six molecular dynamic (MD) experiments proved its correct binding with VEGFR-2 over 100 ns. Additionally, the molecular mechanics energies, combined with the generalized born and surface area (MM-GBSA) analysis, identified the precise binding with optimum energy. To explore the stability and reactivity of the designed pyridine derivative, density functional theory (DFT) calculations, including electrostatic potential maps and total electron density, were carried out. Additionally, the absorption, distribution, metabolism, excretion, and toxicity (ADMET) analysis demonstrated its general likeness and its safety. The designed compound was synthesized to evaluate its effects against VEGFR-2 protein, cancer, and normal cells. The in vitro results were concordant with the in silico results, because the new pyridine derivative (compound 10) displayed VEGFR-2 inhibition with an IC50 value of 65 nM and displayed potent cytotoxic properties against hepatic (HepG2) and breast (MCF-7) cancer cell lines with IC50 values of 21.00 and 26.10 μM, respectively; additionally, it exhibited high selectivity indices against the normal cell lines (W-38) of 1.55 and 1.25, respectively. The obtained results present compound 10 as a new lead VEGFR-2 inhibitor for further biological investigation and chemical modifications.
Cytotoxic and Pro-Apoptotic Effects of Leaves Extract of Antiaris africana Engler (Moraceae)
Authors: Thiam Khadidiatou , Zhao Minjie , Marchioni Eric , Muller Christian D. , Diop Yerim M. , Julien-David Diane , Emhemmed Fathi
Published: November 2022

Antiaris africana Engler leaves have been used in Senegalese folk medicine to treat breast cancer. The present study aimed to investigate the anticancer potential of Antiaris africana Engler leaves using several human cancer cell lines. The leaves of Antiaris africana Engler were extracted in parallel with water or 70% ethanol and each extract divided into three parts by successive liquid–liquid extraction with ethyl acetate and butanol. The phytochemical components of the active extract were investigated using ultra-performance liquid chromatography-diode array detector-quadrupole time-of-flight tandem mass spectrometry (UPLC-DAD-QTOF-MS/MS). The cytotoxic and cytostatic effects of each extract, as well as their fractions, were evaluated in vitro via flow and image cytometry on different human cancer phenotypes, such as breast (MCF-7), pancreas (AsPC-1), colon (SW-620) and acute monocytic leukemia (THP-1). Both hydro-alcoholic and aqueous extracts induced strong apoptosis in MCF-7 cells. The water fraction of the hydro-alcoholic extract was found to be the most active, suppressing the cell growth of MCF-7 in a dose-dependent manner. The half maximum effective concentration (EC50) of this fraction was 64.6 ± 13.7 μg/mL for MCF-7, with equivalent values for all tested phenotypes. In parallel, the apoptotic induction by this fraction resulted in a EC50 of 63.5 ± 1.8 μg/mL for MCF-7, with again equivalent values for all other cellular tested phenotypes. Analysis of this fraction by UPLC-DAD-QTOF-MS/MS led to the identification of hydroxycinnamates as major components, one rutin isomer, and three cardiac glycosides previously isolated from seeds and bark of Antiaris africana Engler and described as cytotoxic in human cancer models. These results provide supportive data for the use of Antiaris africana Engler leaves in Senegal.
Antibacterial Properties of Crotoxin from Crotalus durissus terrificus—Insight into the Mechanism of Action
Authors: Nemecz Dorota , Golińska Patrycja
Published: November 2022

The growing problem of antibiotic resistance among bacteria requires searching for new therapeutic agents with bacteriostatic and/or bactericidal properties. Crotoxin is a β-neurotoxin from the venom of the Crotalus durissus terrificus. It is composed of two subunits: CA (non-active) and CB (with phospholipase A2 activity). It has already been shown that the isolated CB, but not the CA, subunit of crotoxin exhibits an antibacterial activity towards a variety of Gram-positive and Gram-negative bacterial species. However, no studies on the whole crotoxin complex have been carried out so far. We tested the antibacterial properties of crotoxin, as well as its isolated CB subunit, towards Staphylococcus aureus ATCC 25923, Staphylococcus aureus ATCC 6535, Micrococcus luteus ATCC 10240, Escherichia coli ATCC 25922, Escherichia coli ATCC 8739, and Pseudomonas aeruginosa ATCC 10145. Both toxins exhibited antibacterial properties only against Micrococcus luteus ATCC 10240. Crotoxin showed only bacteriostatic activity with a MIC of 46 µM, while the CB subunit acted as both a bacteriostatic and bactericidal agent with a MIC = MBC = 0.21 μM. The bacteriostatic effect of the toxins was independent of the enzymatic activity of the CB subunit. Bactericidal properties, however, require phospholipase A2 activity. Both toxins reduced bacteria viability at the MIC by 72% and 85% for crotoxin- and CB-treated bacteria, respectively. The membrane permeability increased approximately three times within the first hour of incubation with toxins; afterwards, either no significant changes or a decrease of membrane permeability, compared to the control cells, were observed. We isolated a single, approximately 30 kDa bacterial wall protein which belongs to the NlpC/P60 family that interacts with crotoxin leading to the inhibition of bacterial growth. Neither crotoxin nor the CB subunit showed any cytotoxic properties to human fibroblasts at the MIC during the three-day incubation.
Effect of the Citrus Flavone Nobiletin on Circadian Rhythms and Metabolic Syndrome
Authors: Neba Ambe Gael N. N. , Breda Carlo , Bhambra Avninder Singh , Arroo Randolph R. J.
Published: November 2022

The importance of the circadian clock in maintaining human health is now widely acknowledged. Dysregulated and dampened clocks may be a common cause of age-related diseases and metabolic syndrome Thus, circadian clocks should be considered as therapeutic targets to mitigate disease symptoms. This review highlights a number of dietary compounds that positively affect the maintenance of the circadian clock. Notably the polymethoxyflavone nobiletin has shown some encouraging results in pre-clinical experiments. Although many more experiments are needed to fully elucidate its exact mechanism of action, it is a promising candidate with potential as a chronotherapeutic agent.
Heat-Treated Meat Origin Tracing and Authenticity through a Practical Multiplex Polymerase Chain Reaction Approach
Authors: Cheng Yan , Wang Sha , Ju Shilong , Zhou Song , Zeng Xiaoqun , Wu Zhen , Pan Daodong , Zhong Guowei , Cai Zhendong
Published: November 2022

Meat adulteration have become a global issue, which has increasingly raised concerns due to not only economic losses and religious issues, but also public safety and its negative effects on human health. Using optimal primers for seven target species, a multiplex PCR method was developed for the molecular authentication of camel, cattle, dog, pig, chicken, sheep and duck in one tube reaction. Species-specific amplification from the premixed total DNA of seven species was corroborated by DNA sequencing. The limit of detection (LOD) is as low as 0.025 ng DNA for the simultaneous identification of seven species in both raw and heat-processed meat or target meat: as little as 0.1% (w/w) of the total meat weight. This method is strongly reproducible even while exposed to intensively heat-processed meat and meat mixtures, which renders it able to trace meat origins in real-world foodstuffs based on the authenticity assessment of commercial meat samples. Therefore, this method is a powerful tool for the inspection of meat adulterants and has broad application prospects.
Optimization and Application of A Bionic System of Dynamic Co-Culture with Hepatocytes and Renal Cells Based on Microfluidic Chip Technique in Evaluating Materials of Health Food
Authors: Chen Di , Yin Jiyong , Huo Junsheng , Sun Jing , Huang Jian , Li Tiantong , Sun Chaoqun , Yang Zhuo , Qin Wen
Published: November 2022

We aimed to explore the optimization and application of a bionic system of dynamic co-culture with hepatocytes and renal cells based on the microfluidic chip technique in evaluating emodin, which might replace the conventionally cytological evaluation technique of health food. After optimal experiments, the improved bionic system was composed of human hepatocellular carcinoma cells (HepG2), human renal glomerular endothelial cells (HRGECs), rat tail collagen type I, and gelatin with optimized concentrations (1.3 mg/mL + 7.5%). The applicability of the bionic system indicated that the growth stability was appropriate (CV: 7.36%), and the cell viability of that gradually decreased with the increasing of emodin concentration from 0–100 μM, which statistic significances were at 50 and 100 μM (p < 0.05), and the stained results of dead/live cells also showed the same trend. The LDH level appeared rising trend after decline between 0 μM and 100 μM emodi, and the level of that at 100 μM emodin was significantly higher than that at 25 μM and 50 μM emodin, respectively. The BUN level continuously and significantly declined with the increasing of emodin concentration (p < 0.05). Our research realized the application of this optimized bionic system in evaluating emodin, and provided a useful platform and reference for further in vitro alternative research with regard to evaluating the efficacies of health food in the future.
Peripheral T-Cells, B-Cells, and Monocytes from Multiple Sclerosis Patients Supplemented with High-Dose Vitamin D Show Distinct Changes in Gene Expression Profiles
Authors: Kim Dohyup , Witt Emily E. , Schubert Simone , Sotirchos Elias , Bhargava Pavan , Mowry Ellen M. , Sachs Karen , Bilen Biter , Steinman Lawrence , Awani Avni , He Zihuai , Calabresi Peter A. , Van Haren Keith
Published: November 2022

Vitamin D is a steroid hormone that has been widely studied as a potential therapy for multiple sclerosis and other inflammatory disorders. Pre-clinical studies have implicated vitamin D in the transcription of thousands of genes, but its influence may vary by cell type. A handful of clinical studies have failed to identify an in vivo gene expression signature when using bulk analysis of all peripheral immune cells. We hypothesized that vitamin D’s gene signature would vary by immune cell type, requiring the analysis of distinct cell types. Multiple sclerosis patients (n = 18) were given high-dose vitamin D (10,400 IU/day) for six months as part of a prospective clinical trial (NCT01024777). We collected peripheral blood mononuclear cells from participants at baseline and again after six months of treatment. We used flow cytometry to isolate three immune cell types (CD4+ T-cells, CD19+ B-cells, CD14+ monocytes) for RNA microarray analysis and compared the expression profiles between baseline and six months. We identified distinct sets of differentially expressed genes and enriched pathways between baseline and six months for each cell type. Vitamin D’s in vivo gene expression profile in the immune system likely differs by cell type. Future clinical studies should consider techniques that allow for a similar cell-type resolution.