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New strategies combining sensitive pathogenic bacterial detection and high antimicrobial efficacy are urgently desirable. Here, we report smart triple-functional Au-Ag-stuffed nanopancakes (AAS-NPs) exhibiting (1) controllably oxidative Ag-etching thickness for simultaneously obtaining the best surface-enhanced Raman scattering (SERS) enhancement and high Ag-loading antibacterial drug delivery, (2) expressive Ag

Hepatocellular carcinoma (HCC) accounts for ∼90 % of all liver cancer cases, which was the third most common cause of cancer death worldwide in 2020. Glypican-3 (GPC3) is highly and specifically expressed in HCC, which makes it a promising therapeutic target. We discovered novel antibody sequences against GPC3 from a phage display library and ranked the candidates by their binding affinity and epitope bins. Candidates with single- to double-digit nanomolar affinity were selected and expressed in Fab format and linked to a deimmunized bacterial exotoxin moiety via an intein trans-splicing reaction. The resulting immunotoxins were evaluated for their in vitro binding specificity and affinity, cell surface binding on the HepG2 or Huh7, rate of internalization, and potency of cytotoxicity. The immunotoxin called GT5 exhibited strong antigen binding and cell surface binding, as well as high internalization efficiency. The molecule GT5 was further evaluated for cytotoxicity in HepG2 and Huh7 cell-based assay and assessed for its pharmacokinetics and antitumor activity in a murine tumor xenograft model. GT5 significantly inhibited tumor growth and showed stronger potency than the chemotherapeutic drug sorafenib. In conclusion, GT5, a novel GPC3 targeting immunotoxin, was shown to have a high affinity towards GPC3 and effectively inhibit hepatocellular tumor growth in vitro and in vivo, thus providing the basis for further development of GT5 immunotoxin as a novel therapeutic modality for the treatment of liver cancer.

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) variants of concern (VOCs) continue to wreak havoc across the globe. Higher transmissibility and immunologic resistance of VOCs bring unprecedented challenges to epidemic extinguishment. Here we describe a monoclonal antibody, 2G1, that neutralizes all current VOCs and has surprising tolerance to mutations adjacent to or within its interaction epitope. Cryo-electron microscopy structure showed that 2G1 bound to the tip of receptor binding domain (RBD) of spike protein with small contact interface but strong hydrophobic effect, which resulted in nanomolar to sub-nanomolar affinities to spike proteins. The epitope of 2G1 on RBD partially overlaps with angiotensin converting enzyme 2 (ACE2) interface, which enables 2G1 to block interaction between RBD and ACE2. The narrow binding epitope but high affinity bestow outstanding therapeutic efficacy upon 2G1 that neutralized VOCs with sub-nanomolar half maximal inhibitory concentration in vitro. In SARS-CoV-2, Beta or Delta variant-challenged transgenic mice and rhesus macaque models, 2G1 protected animals from clinical illness and eliminated viral burden, without serious impact to animal safety. Mutagenesis experiments suggest that 2G1 is potentially capable of dealing with emerging SARS-CoV-2 variants in the future. This report characterized the therapeutic antibodies specific to the tip of spike against SARS-CoV-2 variants and highlights the potential clinical applications as well as for developing vaccine and cocktail therapy.

Hot-water and ethanol extracts of Chrysanthemum morifolium cv. Fubaiju were investigated for their chemical compositions, effects on gut microbiota, anti-inflammatory, and free radical scavenging capacities. UPLC-IMS-QTOF-MS analysis detected tuberonic acid glucoside and tasumatrol B in the Fubaiju for the first time. The hot-water extract had greater anti-inflammation and free radical scavenging activities than its counterpart ethanol extract under the experimental conditions. The total phenolic content, relative ABTS +, DPPH and oxygen radical scavenging capacities of the hot-water extract were 33.48 mg gallic acid equivalents/g, and 121.57, 110.11 and 1638.99 µmol Trolox equivalents/g, respectively. In addition, the hot-water extract enhanced the abundance of Bacteroidetes, Firmicutes, Bifidobacteria and Precotella, suggesting that drinking chrysanthemum tea may modulate gut microbiota. The results from this research could be used to improve the production and consumption of C. morifolium cv. Fubaiju as a functional food ingredient and promote local agricultural economics.

The simultaneous, precise, and quantitative detection of multi-components inflammatory markers (IMs) in sepsis serum by surface-enhanced Raman scattering (SERS) remains a challenging problem. A novel, multifunctional biosensor with dual enrichment and enhancement was designed for the ultrasensitive and quantitative analysis of multi-components IMs. The biosensor contains SERS tags-unique urchin core/porous shell (CPS) structure modified with Raman reporters (RaRs), magnetic assist-Ag coated Fe

LNCaP athymic xenograft model has been widely used to allow researchers to examine the effects and mechanisms of experimental treatments such as diet and diet-derived cancer preventive and therapeutic compounds on prostate cancer. However, the biological characteristics of human LNCaP cells before/after implanting in athymic mouse and its relevance to clinical human prostate outcomes remain unclear and may dictate interpretation of biological efficacies/mechanisms of diet/diet-derived experimental treatments. In this study, transcriptome profiles and pathways of human prostate LNCaP cells before (in vitro) and after (in vivo) implanting into xenograft mouse were compared using RNA-sequencing technology (RNA-seq) followed by bioinformatic analysis. A shift from androgen-responsive to androgen nonresponsive status was observed when comparing LNCaP xenograft tumor to culture cells. Androgen receptor and aryl-hydrocarbon pathway were found to be inhibited and interleukin-1 (IL-1) mediated pathways contributed to these changes. Coupled with in vitro experiments modeling for androgen exposure, cell-matrix interaction, inflammation, and hypoxia, we identified specific mechanisms that may contribute to the observed changes in genes and pathways. Our results provide critical baseline transcriptomic information for a tumor xenograft model and the tumor environments that might be associated with regulating the progression of the xenograft tumor, which may influence interpretation of diet/diet-derived experimental treatments.

Dietary microRNAs (miRNAs) are thought to regulate a wide range of biological processes, including the gut microbiota. However, it is difficult to separate specific effect(s) of miRNA from that of the food matrix. This study aims to elucidate the specific effect(s) of dietary corn miRNAs, ingested as a whole food, on the gut microbiota. We developed an autoclave procedure to remove 98% of miRNA from corn. A mouse feeding study was conducted comparing autoclaved corn to nonautoclaved corn and purified corn miRNA. Compared to nonspecific nucleotides and corn devoid of miRNAs, feeding purified corn miRNAs or corn to C57BL/6 mice via gavage or diet supplementation for two weeks lead to a decrease in total bacteria in the cecum. The effect appeared to be due to changes in Firmicutes. Additionally, corn matrix minus miRNA and processing also affected gut bacteria. In silico analysis identified corn miRNAs that aligned to Firmicutes genome sequences lending further support to the interaction between corn miRNAs and this bacterium. These data support interactions between plant food miRNA, as well as matrix, and the gut microbiota exist but complex. However, it provides additional support for mechanism by which bioactive dietary components interact with the gut microbiota., We developed a method to remove miRNA from food (corn) and use it to elucidate the effect of miRNA on gut microbiome in‐vivo. We found corn miRNA specifically decrease abundance of Firmicutes, while the matrix devoid of miRNA appeared to modulate Lactobacillus and Akkermansia muciniphila. Also, processing may affect bacteria such as Ruminococcus, Enterobacteriaceae. Hence, interactions between plant food miRNA, food matrix, and the gut microbiota exist but may be complex.

Accumulated evidence suggests that the cruciferous vegetables-derived compound indole-3-carbinol (I3C) may protect against prostate cancer, but the precise mechanisms underlying its action remain unclear. This study aimed to verify the hypothesis that the beneficial effect of dietary I3C may be due to its modulatory effect on the gut microbiome of mice. Athymic nude mice (5&ndash, 7 weeks old, male, Balb c/c nu/nu) with established tumor xenografts were fed a basal diet (AIN-93) with or without 1 &micro, moles I3C/g for 9 weeks. The effects of dietary I3C on gut microbial composition and microbial species interactions were then examined by 16s rRNA gene-based sequencing and co-occurrence network analysis. I3C supplementation significantly inhibited tumor growth (p &lt, 0.0001) and altered the structure of gut microbiome. The abundance of the phylum Deferribacteres, more specifically, Mucispirillum schaedleri, was significantly increased by dietary I3C. Additionally, I3C consumption also changed gut microbial co-occurrence patterns. One of the network modules in the control group, consisting of seven bacteria in family S-27, was positively correlated with tumor size (p &lt, 0.009). Moreover, dietary I3C disrupted microbial interactions and altered this association between specific microbial network and tumor development. Our results unraveled complex relationships among I3C ingestion, gut microbiota, and prostate tumor development and may provide a novel insight into the mechanism for the chemopreventive effect of dietary I3C on prostate cancer.

3-monochloro-1, 2-propanediol fatty acid esters (3-MCPDEs) comprise a group of food toxicants formed during food processing. 3-MCPDEs have received increasing attention concerning their potential negative effects on human health. However, reports on the toxicity of 3-MCPD esters are still limited. To determine the effects of fatty acid substitutions on the toxicity of their esters, 1-stearic, 1-oleic, 1-linoleic, 1-linoleic-2-palmitic and 1-palmitic-2-linoleic acid esters of 3-MCPD were synthesized and evaluated with respect to their acute oral toxicities in Swiss mice.; Results: 3-MCPDEs were obtained through the reaction of 3-MCPD and fatty acid chlorides, and their purities and structures were characterized by ultraperformance liquid chromatography-quadrupole-time of flight-mass spectrometry (UPLC-Q-TOF-MS), infrared, 1 H and 13 C spectroscopic analyses. Medial lethal doses of 1-stearic, 1-oleic, 1-linoleic, 1-linoleic-2-palmitic and 1-palmitic-2-linoleic acid esters were 2973.8, 2081.4, 2016.3, 5000 and > 5000 mg kg-1 body weight. For the first time, 3-MCPDEs were observed for their toxic effects in the thymus and lung. In addition, major histopathological changes, as well as blood urea nitrogen and creatinine, were examined for mice fed the five 3-MCPDEs.; Conclusion: The results from the present study suggest that the degree of unsaturation, chain length, number of substitution and relative substitution locations of fatty acids might alter the toxicity of 3-MCPDEs. © 2016 Society of Chemical Industry.; © 2016 Society of Chemical Industry.

MicroRNAs (miRNAs) ubiquitously exist in microorganisms, plants, and animals, and appear to modulate a wide range of critical biological processes. However, no definitive conclusion has been reached regarding the uptake of exogenous dietary small RNAs into mammalian circulation and organs and cross-kingdom regulation. One of the critical issues is our ability to assess and distinguish the origin of miRNAs. Although periodate oxidation has been used to differentiate mammalian and plant miRNAs, validation of treatment efficiency and the inclusion of proper controls for this method were lacking in previous studies. This study aimed to address: 1) the efficiency of periodate treatment in a plant or mammalian RNA matrix, and 2) the necessity of inclusion of internal controls. We designed and tested spike-in synthetic miRNAs in various plant and mammalian matrices and showed that they can be used as a control for the completion of periodate oxidation. We found that overloading the reaction system with high concentration of RNA resulted in incomplete oxidation of unmethylated miRNA. The abundant miRNAs from soy and corn were analyzed in the plasma, liver, and fecal samples of C57BL/6 mice fed a corn and soy-based chow diet using our improved methodology. The improvement resulted in the elimination of the false positive detection in the liver, and we did not detect plant miRNAs in the mouse plasma or liver samples. In summary, an improved methodology was developed for plant miRNA detection that appears to work well in different sample matrices.

Cardiovascular disease (CVD) is the leading cause of death in the United States, and hypercholesterolemia is a major risk factor. Population studies, as well as animal and intervention studies, support the consumption of a variety of vegetables as a means to reduce CVD risk through modulation of hypercholesterolemia. Microgreens of a variety of vegetables and herbs have been reported to be more nutrient dense compared to their mature counterparts. However, little is known about the effectiveness of microgreens in affecting lipid and cholesterol levels. The present study used a rodent diet-induced obesity (DIO) model to address this question. C57BL/6NCr mice (n = 60, male, 5 weeks old) were randomly assigned to six feeding groups: (1) low-fat diet; (2) high-fat diet; (3) low-fat diet + 1.09% red cabbage microgreens; (4) low-fat diet + 1.66% mature red cabbage; (5) high-fat diet + 1.09% red cabbage microgreens; (6) high-fat diet + 1.66% mature red cabbage. The animals were on their respective diets for 8 weeks. We found microgreen supplementation attenuated high-fat diet induced weight gain. Moreover, supplementation with microgreens significantly lowered circulating LDL levels in animals fed the high-fat diet and reduced hepatic cholesterol ester, triacylglycerol levels, and expression of inflammatory cytokines in the liver. These data suggest that microgreens can modulate weight gain and cholesterol metabolism and may protect against CVD by preventing hypercholesterolemia.

Ten commercial mung bean samples (MB1–10) were investigated and compared for their chemical composition, and anti-oxidant and anti-inflammatory properties. Mung beans had a low oil content of 0.32–0.75 g/100 g, and differed in their total phenolic, total flavonoid, and vitexin and isovitexin contents. The acetone–water (1:1, v/v) extract of MB6 exhibited the highest total phenolic content of 5.07 mg gallic acid equivalents (GAE)/g, and the greatest total flavonoid concentration of 5.97 mg rutin equivalents (RE)/g. The acetone–water extracts differed in their RDSC, FRAP, HOSC and ORAC values, and showed significant anti-inflammatory effects in LPS-stimulated RAW 264.7 mouse macrophage cells at 100 μg/mL concentration. Furthermore, the results indicated that compounds other than vitexin and isovitexin might also significantly contribute to the overall anti-inflammatory effect of mung beans. This study indicated the potential utilization of mung beans in health promoting functional food or supplemental products.

Soy (Glycine max) is a major commodity in the United States, and soy foods are gaining popularity due to their reported health-promoting effects. In the past two decades, soy and soy bioactive components have been studied for their health-promoting/disease-preventing activities and potential mechanisms of action. Recent studies have identified gut microbiota as an important component in the human body ecosystem and possibly a critical modulator of human health. Soy foods' interaction with the gut microbiota may critically influence many aspects of human development, physiology, immunity, and nutrition at different stages of life. This review summarizes current knowledge on the effects of soy foods and soy components on gut microbiota population and composition. It was found, although results vary in different studies, in general, both animal and human studies have shown that consumption of soy foods can increase the levels of bifidobacteria and lactobacilli and alter the ratio between Firmicutes and Bacteroidetes. These changes in microbiota are consistent with reported reductions in pathogenic bacteria populations in the gut, thereby lowering the risk of diseases and leading to beneficial effects on human health.

Dietary supplements are widely used in the United States, but the safety issue remains unresolved. Immuno-deficient or immuno-compromised patients, estimated to exceed 10 million in the United States, are known to use dietary supplements. This population potentially may be susceptible to supplements' adverse effects. The cruciferous vegetable-derived indole-3-carbinol (I3C) is known for its possible protective effects against a number of chronic diseases and is commercially available as a dietary supplement. However, the safety of orally consumed I3C in the general population and particularly in immuno-compromised individuals remains unknown. In this study, rodent model of immune-deficient male BALB/c nu/nu athymic mice were given diets supplemented with 0-100 μmoles I3C/g diet for 4 weeks. We found that BALB/c nu/nu mice were not viable after three days on a 100 μmoles I3C/g supplemented diet. Switching to the control diet (without I3C) after first detection of stress resulted in a 75% recovery of mice. Mice fed with 10-50 μmoles I3C/g supplemented diet survived but showed concentration-dependent adverse effects. More importantly, the intestine appeared to be the target of I3C toxicity. Number and width of intestinal villi were significantly altered by I3C, which associated with a dose-dependent reduction in cell proliferation and increase in apoptosis. Other molecular effects observed for I3C include activation of multiple xenobiotic metabolism pathways. This is the first study to report hazardous effects of I3C supplementation that are specific to the gastrointestinal tract in an immuno-compromised model and should serve as a caution in using I3C as dietary supplements.

Hypercholesterolaemia is a risk factor for CVD, which is a leading cause of death in industrialised societies. The biosynthetic pathways for cholesterol metabolism are well understood; however, the regulation of circulating cholesterol by diet is still not fully elucidated. The present study aimed to gain more comprehensive understanding of the relationship between circulating cholesterol levels and molecular effects in target tissues using the hamster model. Male golden Syrian hamsters were fed with chow or diets containing 36 % energy from fat with or without 1 % cholesteyramine (CA) as a modulator of circulating cholesterol levels for 35 d. It was revealed that the expression of lanosterol 14α-demethylase (CYP51) instead of 3-hydroxy-3-methyl-glutaryl (HMG)-CoA reductase mRNA expression was responsive to circulating cholesterol in hamsters fed hypercholesterolaemic diets. The high-fat diet increased circulating cholesterol and down-regulatedCYP51, but not HMG-CoA reductase. The CA diet decreased cholesterol and increasedCYP51expression, but HMG-CoA reductase expression was not affected. The high-fat diet and CA diet altered the expression level of cholesterol, bile acids and lipid metabolism-associated genes (LDL receptor, cholesterol 7α-hydroxylase (CYP7A1), liver X receptor (LXR) α, and ATP-binding cassette subfamily G member 5/8 (ABCG5/8)) in the liver, which were significantly correlated with circulating cholesterol levels. Correlation analysis also showed that circulating cholesterol levels were regulated by LXR/retinoid X receptor and PPAR pathways in the liver. Using the hamster model, the present study provided additional molecular insights into the influence of circulating cholesterol on hepatic cholesterol metabolism pathways during hypercholesterolaemia.

A total of 13 commercial soybean samples were investigated and compared for their tocopherol and carotenoid compositions, fatty acid profile, total phenolic content (TPC), isoflavone and sterol compositions, and free radical scavenging properties. Free radical scavenging activities were estimated against peroxyl, hydroxyl, and ABTS(•) (+) radicals. The commercial soybean samples differed in their chemical compositions and health properties. Among the tested samples, CN-DB soybean showed the highest TPC and antioxidant activities and the greatest amount of total isoflavones and lutein and tocopherol contents. In addition, four of the soybean samples were further tested for their potential anti-inflammatory activity. The four samples behaved differently in suppressing the IL-1β, IL-6, and COX-2 mRNA expressions, suggesting their different potential of anti-inflammatory activities. The results from this study suggested a need of improved quality control and measurement system to better reflect the health properties of commercial soybeans for general consumers and food manufacturers to improve the use of this important food ingredient.

Five new glycerol esters including 2-acetyl-1-coumaroyl-3-cinnamoylglycerol (13), (+)-2-acetyl-1-feruloyl-3-cinnamoylglycerol (14), (-)-2-acetyl-1-feruloyl-3-cinnamoylglycerol (15), 2-acetyl-1,3-dicinnamoylglycerol (16), and (-)-2-acetyl-1-(E)-feruloyl-3-(3″(ζ),16″)-dihydroxy-palmitoylglycerol (17) were isolated from methanolic extract of Wuhan propolis. The chemical structures of the five new compounds were confirmed by (1)H and (13)C NMR and HR-MS spectra. Twelve minor constituents in the Wuhan propolis extract were tentatively identified by UPLC-Q-TOF-MS, according to their characteristic UV spectrum, retention times, and accurate MS data. The anti-inflammatory activities of the five new compounds were studied in lipopolysaccharide (LPS)-stimulated RAW 264.7 mouse macrophage cells. All five compounds exhibited remarkable inhibitory effects on interleukin (IL)-1β, IL-6, and cyclooxygenase (COX)-2 mRNA expressions at 10 and 100 μM, suggesting that Wuhan propolis may serve as a potential anti-inflammatory functional food ingredient or nutraceutical.

In vitro cell culture models are widely used in inflammation research; however, information regarding the time- and dose-dependency of inflammatory responses toward LPS in these cell lines is scattered in the literature. J774A.1 mouse macrophage and THP-1 human monocyte cell lines. J774A.1 and THP-1 cells were treated with 0–500 ng/mL lipopolysaccharide for 0–24 h. SRB and BCA tests were used to measure total protein. Real-time PCR was used to determine gene expression levels, and ELISA was used to assess the protein levels. One-way ANOVA and Tukey’s Honestly Significant Difference test were used to test the significance levels. In J774A.1 and THP-1 cells, cytokines responded in distinct patterns upon LPS stimulation in a time- and dose-dependent manner, and the differential regulation of the response to LPS between J774A.1 and THP-1 cells appeared to correlate with the differential regulation of TLR4 at the mRNA level. In summary, this study indicated that temporal and dose-dependent responses to LPS need to be controlled for and that extrapolation of data on mechanisms may differ between cell lines of different origin.

The ethyl acetate fraction of the leaves of Engelhardia roxburghiana Wall exhibited strong anti-inflammatory, anti-proliferative, and antioxidant activities. From this fraction, three new flavanonol glycosides: (2 R , 3 R )-3,5,7,4′-tetrahydroxyflavanonol-3- O -(3″- O -galloyl)-α- l -rhamnopyranoside ( 1 ), (2 R , 3 R )-3,5,7,3′,4′-pentahydroxyflavanonol-3- O -(3″- O -galloyl)-α- l -rhamnopyranoside ( 2 ), (2 R , 3 R )-3,5,7,3′,4′-pentahydroxyflavanonol-3- O -(3″- O - p -( E )-coumaroyl)-α- l -rhamnopyranoside ( 3 ), were isolated. The structures of these compounds were elucidated based on spectroscopic, and chemical analyses. The anti-inflammatory activities of 1 – 3 were examined as their inhibitory abilities on the expression of IL-1β, TNF-α, MCP-1, and COX-2 mRNA, in lipopolysaccharide-stimulated mouse J774A.1 macrophage cells. At the concentration of 50 μM, 2 and 3 significantly reduced the IL-1β expression, while 1 induced its expression contrarily. Meanwhile, 1 and 3 exhibited significant inhibition of TNF-α expression at the concentration of 10 μM, while 2 could achieve weak but significant inhibition at 50 μM. Furthermore, 1 – 3 did not suppress the mRNA expression of MCP-1 and COX-2. Compounds 1 – 3 showed significant anti-proliferative effect in Hep G2 cells. 3 showed the most potent anti-proliferative effect in HT-29 human colon cancer cells, while 1 and 2 had no inhibition. In addition, 1 and 2 exhibited antioxidant activities. The ORAC values of 1 and 2 were 12.8 and 17.0 mmol TE/g and the HOSC values of 1 and 2 were 14.4 and 16.0 mmol TE/g, respectively.

Leaf and whole-plant samples of the diploid and tetraploid Gynostemma pentaphyllum (GP) were investigated and compared for their chemical compositions, and their potential anti-proliferative and anti-inflammatory effects. The highest levels of total flavonoids and phenolics were observed in the diploid leaf botanical (2L3) at 36.84mg rutin equiv/g and 41.15mg gallic acid equiv/g, respectively. The diploid leaf sample (2L2) had the highest amount of rutin and quercetin contents of 77.7μmol quercetin equiv/g. The tetraploid whole-plant botanical (4L3) had the highest total saponin content of 227.1mg gypenoside equiv/g. Extracts from all tested GP samples showed time- and dose-dependent antiproliferative effects in HT-29 cells, and the diploid leaf samples had the overall highest inhibitory activity. These extracts had different order of antiproliferative properties in the LNCaP cells, suggesting the potential selective inhibition of GP extracts against different types of cancer cells and the effect of the cell model in screening and evaluation of antiproliferative components. In addition, the diploid leaf extracts showed the strongest inhibitory effects on the expression of TNF-α, IL-6 and COX-2 mRNA at final concentrations of 0.2 and 1mg botanical equiv/ml media. The results from this study will be used to develop new nutraceutical products from G. pentaphyllum.

Whole wheat flour from five wheat cultivars was evaluated for phenolic, carotenoid, and tocopherol compositions as well as anti-inflammatory and antiproliferative activities against HT-29 cells. The total ferulic acid content ranged from 452 to 731 μg/g among the five cultivars and was primarily present in the insoluble-bound form. Lutein was the only carotenoid detected and ranged from 1.5 to 4.0 μg/g, and α-tocopherol levels ranged from 12 to 61 μg/g. Extracts of four cultivars demonstrated significant anti-inflammatory activity, measured as inhibition of interleukin-1β (IL-1β) mRNA expression; however, none of the extracts inhibited tumor necrosis factor-α (TNF-α) mRNA expression, a second indicator of anti-inflammatory activity. Proliferation of HT-29 adenocarcinoma cells was inhibited by extracts from all cultivars at the dose of 100 mg botanical equivalent/mL. The cultivar WestBred 936 had the greatest antiproliferative activity at lower concentrations (20 and 50 mg botanical equivalent/mL), had the greatest anti-inflammatory effect against IL-1β, and also had the highest levels of ferulic acid and α-tocopherol. This research shows that whole wheat flours of these five cultivars varied significantly in their contents of phenolics, carotenoids, and α-tocopherol as well as in their anti-inflammatory and antiproliferative potentials, suggesting the possibility that wheat varieties can be selected based on potential health benefits.

Five Gynostemma pentaphyllum (GP) samples were investigated and compared for their chemical compositions and their antioxidant, antiproliferative, and anti-inflammatory effects. Extracts (50% acetone, 75% ethanol, and 100% ethanol) of the five GP samples (GP1-5) differed in their total phenolic, saponin, and flavonoid contents and in their rutin and quercetin concentrations. The highest level of total flavonoids was 63.5 mg of rutin equiv/g in GP4, and the greatest total phenolic content was 44.3 mg of gallic acid equiv/g in GP1 with 50% acetone as the extraction solvent. GP2 had the highest total saponin content of 132.6 mg/g with 100% ethanol as the extraction solvent. These extracts also differed in their scavenging capacity against DPPH and hydroxyl radicals, although they all showed significant radical scavenging capacity. The 100% ethanol extracts also showed dose-dependently strong inhibition on IL-6 and Ptgs2 mRNA expression and weak inhibition on TNF-α mRNA expression. In addition, GP1 had the highest antiproliferative activity at 3.2 mg equiv/mL concentration in HT-29 human colon cancer cells. The results from this study will be used to promote the application of G. pentaphyllum for improving human health.

Clustered regularly interspaced short palindromic repeats (CRISPR) was discovered in the 1980s in E. coli and its function was elucidated in 2007 in S. thermophilus . Coupled with the CRISPR-associated protein nuclease (Cas), CRISPR/Cas forms a defense system enabling the organisms to respond to and eliminate invading exogenous organisms and foreign nucleic acids. The discovery and development of CRISPR/ CRISPR-associated protein-9 nuclease (Cas9) system offered superior precision and simplicity in genome editing, which can greatly bene t and has enormous potential in both biological and medical science research. Artificial intelligence (AI) was conceptualized in the 1950s and the recent resurgence of machine learning research assisted a rapid advancement in AI capability and functionality. Combining these two technologies, equipped with the machine learning and pattern recognition capability, AI has the potential to lift the biological and medical science research to a new level by (I) improving CRISPR ef cacy and precision with AI-assisted analysis and design of targets; (II) performing more ef cient analysis of molecular pathways and deepening understanding of their interactions through pattern recognition, and (III) incorporating CRISPR and AI to better understand multifactorial disorders, identify critical mutations, and design therapeutic targets.

Cholestyramine (CA) is a bile acid sequestrant widely used as a cholesterol-lowering drug to treat hypercholesterolemia, one of the major risk factors for cardiovascular disease. Despite the wide u...

3-monochloro-1, 2-propanediol fatty acid esters (3-MCPDEs) comprise a group of food toxicants formed during food processing. 3-MCPDEs have received increasing attention concerning their potential negative effects on human health. However, reports on the toxicity of 3-MCPD esters are still limited. To determine the effects of fatty acid substitutions on the toxicity of their esters, 1-stearic, 1-oleic, 1-linoleic, 1-linoleic-2-palmitic and 1-palmitic-2-linoleic acid esters of 3-MCPD were synthesized and evaluated with respect to their acute oral toxicities in Swiss mice.3-MCPDEs were obtained through the reaction of 3-MCPD and fatty acid chlorides, and their purities and structures were characterized by ultraperformance liquid chromatography-quadrupole-time of flight-mass spectrometry (UPLC-Q-TOF-MS), infrared,The results from the present study suggest that the degree of unsaturation, chain length, number of substitution and relative substitution locations of fatty acids might alter the toxicity of 3-MCPDEs. © 2016 Society of Chemical Industry.

Soy is an important commodity and a long-time staple food in eastern Asian countries. Recent research and clinical studies have provided ample evidence for the health benefits of soy and soy foods, which have also contributed to an increase in soy consumption among the Western population. The current mini-review aims to summarize the current knowledge of the health benefits of soy and soy phytochemicals, and their reported effects in preventing (I) cardiovascular disease, (II) obesity-related metabolic syndrome, (III) certain types of cancers, and (IV) other chronic diseases. In addition to the widely reported soy isoflavones, namely, genistein, daidzein, and glycitein, a novel group of soy phytoalexins, glyceollins, have also shown promising biological activities, such as insulinotropic, antiestrogenic, antiproliferative, antioxidation, anti-inflammation, and cholesterol-lowering effects. The elucidation of soy’s health benefits is an important part of promoting the consumption of soy as a functional food and the understanding of the mechanism of actions of soy and soy phytochemicals’ biological activities will provide further evidence for the optimized use for health promotion.

Food-derived phytochemicals, many known for their health beneficial effects, often exist in conjugated forms containing sugar moieties such as glucose or rhamnose in foods. The uptake of these compounds requires colonic bacterial cleavage of sugar moieties. However, most studies involved in screening extracts for biological activities do not take this process into account. This study seeks to determine the utility of commercially available hesperidinase to mimic colonic digestion and to test the effects of this treatment on the biological properties of extracts. Using hesperidinase resulted in efficient hydrolysis of Engelhardia roxburghiana Wall. extract containing rhamnose conjugates. Enzymatic digestion enhanced the extract's cellular antioxidant ability by 2-fold in HepG2/C3A and the anti-inflammatory effect on lipopolysaccharide-induced interleukin (IL)-1β and IL-6 expression in mouse macrophage J774A.1 and human monocyte THP-1 cells. Enzymatic digestion also efficiently processed extracts with mixed rhamnose and glucose conjugates and altered their biological activities. Results of the present study supported the importance of considering enzymatic digestion during the biological activity studies of botanicals.

Diet-derived flavonoids quercetin (Q), kaempferol (K) and taxifolin (T) were studied for their anti-inflammatory property in J774A.1 mouse macrophage, undifferentiated- (u-) and differentiated- (d-) human THP-1 cells. Cells were pre-incubated with respective compound for 48 h followed by stimulation with bacterial lipopolysaccharide (LPS) to induce inflammatory response. All test compounds inhibited LPS induction of the pro-inflammatory cytokines IL-6 mRNA expressions in J774A.1 cells with EC50 at 6 µM for Q, 5 µM for K, and 16 µM for T, respectively. Interestingly, all compounds at concentration up to 10 µM exerted no inhibitory effect on LPS induction of IL-6 mRNA expression in u-THP-1 cells. In d-THP-1 cells, Q and K significantly inhibited LPS stimulation of IL-6 mRNA expression, while T showed no inhibitory effect. This differential effect in different cell lines appeared to be associated with differential ability of the compounds to inhibit expression of the xenobiotic metabolizing enzyme, cytochrom...

Hypercholesterolemia is one of the major factors contributing to the risk of cardiovascular disease (CVD), which is the leading cause of death in developed countries. Consumption of soy foods has been recognized to lower the risk of CVD, and phytochemicals in soy are believed to contribute to the health benefits. Glyceollin is one of the candidate phytochemicals synthesized in stressed soy that may account for many unique biological activities. In this study, the in vivo cholesterol-lowering effect of glyceollins was investigated. Male golden Syrian hamsters were fed diets including (1) 36 kcal% fat diet, (2) 36 kcal% fat diet containing 250 mg/kg diet glyceollins, or (3) chow for 28 days. Hepatic cholesterol esters and free cholesterol, hepatic total lipid content, plasma lipoproteins, fecal bile acid, fecal total cholesterol, and cholesterol metabolism related gene expressions were measured. Glyceollin supplementation led to significant reduction of plasma VLDL, hepatic cholesterol esters, and total lipid content. Consistent with changes in circulating cholesterol, glyceollin supplementation also altered expression of the genes related to cholesterol metabolism in the liver. In contrast, no change in plasma LDL and HDL, fecal bile acid, or cholesterol content was observed. The cholesterol-lowering effect of glyceollins appeared not to go through the increase of bile excretion. These results supported glyceollins' role as novel soy-derived cholesterol-lowering phytochemicals that may contribute to soy's health effects.

Six new acylphloroglucinol derivatives, sampsonols A-F ( 1 – 6 ), were isolated from the petroleum ether extract of the aerial parts of Hypericum sampsonii . The structures and relative configurations of sampsonols A-F were elucidated by extensive spectroscopic analyses. All these compounds were tested for their in vitro cytotoxic and anti-inflammatory activities. Sampsonols A and B ( 1 and 2) showed significant cytotoxicity against four human tumor cell lines with IC 50 values in the range of 13–28 μM, whereas sampsonols C and F ( 3 and 6) showed potent inhibitory activities against LPS-induced NO production in RAW 264.7 macrophages with IC 50 values of 27.3 and 29.3 μM, respectively.

Conventional and organic cinnamon and peppermint were investigated for their phenolic profile, anti-proliferative, anti-inflammatory, and antioxidant properties. Accelerated solvent extraction with 75% acetone was used to extract samples. Caffeic acid was the most abundant phenolic acid in peppermint. Catechin, (−)-epigallocatechin gallate, syringic acid, gallic acid, vanillic acid, and p-coumaric acid were also detected in both spices. There was no significant difference between conventional and organic spices in the composition of most individual phenolics. All conventional and organic peppermint and cinnamon extracts exhibited strong anti-proliferative and anti-inflammatory properties. Cinnamon was more efficient in inhibiting IL-1β and COX-2 expression, while peppermint showed better inhibitory effect on IL-6 and MCP-1. This study indicates that cinnamon and peppermint may potentially be used as dietary sources of bioactive phytochemicals for improving health.

Engeletin, a flavonoid compound, was isolated from the leaves of Engelhardia roxburghiana for the first time, along with astilbin, another flavonoid. The chemical structures of engeletin and astilbin were confirmed by (1)H and (13)C nuclear magnetic resonance (NMR) and mass spectrometry (MS) spectra, and their anti-inflammatory activities were studied in lipopolysaccharide (LPS)-stimulated mouse J774A.1 macrophage cells. LPS induced the inflammatory state in macrophage cells and increased mRNA expressions of pro-inflammatory cytokines. Engeletin and astilbin exhibited remarkable inhibitory effects on interleukin (IL)-1β and IL-6 mRNA expression. Significant inhibition of LPS-mediated mRNA expressions were also seen in LPS binding toll-like receptor (TLR)-4, pro-inflammatory cytokine tumor necrosis factor (TNF)-α, IL-10, chemoattractant monocyte chemotactic protein (MCP)-1, and cyclooxygenase (COX)-2 genes. The reduced expression of these cytokines may alleviate immune response and reduce inflammatory activation, indicating that engeletin and astilbin may serve as potential anti-inflammatory agents.