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Abstract Circadian clock serves as a regulator of gastrointestinal health, and the disruption of circadian rhythm may trigger the dysregulation of the intestinal barrier functions. This study investigated the effectiveness of capsaicin (CAP) in mitigating intestinal barrier dysfunction induced by circadian disruption in male SPF C57BL/6J mice. Our findings indicated that CAP supplementation attenuated abnormal weight gain, alterations in serum lipid levels, and misalignment in hepatic and colonic circadian clock gene expressions in mice caused by constant darkness (CD) treatment. The restoration of the intestinal barrier integrity was also observed through the increase in mucosal thickness and goblet cell numbers. Both the diversity and the circadian rhythm of gut microbiota were improved in CAP‐treated group. Correlation analysis indicated that CAP could modulate the gut microbiota by affecting intestinal barrier function and systemic metabolism in CD‐treated mice. These results highlight the potential of CAP as a functional food component in maintaining the intestinal barrier homeostasis through regulating gut microbiota.

Abstract Background Diet and gut microbiota contribute to non-alcoholic steatohepatitis (NASH) progression. High-fat diets (HFDs) change gut microbiota compositions, induce gut dysbiosis, and intestinal barrier leakage, which facilitates portal influx of pathogen-associated molecular patterns including lipopolysaccharides (LPS) to the liver and triggers inflammation in NASH. Current therapeutic drugs for NASH have adverse side effects; however, several foods and herbs that exhibit hepatoprotection could be an alternative method to prevent NASH. Methods We investigated ginger essential oil (GEO) against palm oil-containing HFDs in LPS-injected murine NASH model. Results GEO reduced plasma alanine aminotransferase levels and hepatic pro-inflammatory cytokine levels; and increased antioxidant catalase, glutathione reductase, and glutathione levels to prevent NASH. GEO alleviated hepatic inflammation through mediated NLR family pyrin domain-containing 3 (NLRP3) inflammasome and LPS/Toll-like receptor four (TLR4) signaling pathways. GEO further increased beneficial bacterial abundance and reduced NASH-associated bacterial abundance. Conclusion This study demonstrated that GEO prevents NASH progression which is probably associated with the alterations of gut microbiota and inhibition of the LPS/TLR4/NF-κB pathway. Hence, GEO may offer a promising application as a dietary supplement for the prevention of NASH.

Abstract Dietary emulsifiers are linked to various diseases. The recent discovery of the role of gut microbiota–host interactions on health and disease warrants the safety reassessment of dietary emulsifiers through the lens of gut microbiota. Lecithin, sucrose fatty acid esters, carboxymethylcellulose (CMC), and mono- and diglycerides (MDG) emulsifiers are common dietary emulsifiers with high exposure levels in the population. This study demonstrates that sucrose fatty acid esters and carboxymethylcellulose induce hyperglycemia and hyperinsulinemia in a mouse model. Lecithin, sucrose fatty acid esters, and CMC disrupt glucose homeostasis in the in vitro insulin-resistance model. MDG impairs circulating lipid and glucose metabolism. All emulsifiers change the intestinal microbiota diversity and induce gut microbiota dysbiosis. Lecithin, sucrose fatty acid esters, and CMC do not impact mucus–bacterial interactions, whereas MDG tends to cause bacterial encroachment into the inner mucus layer and enhance inflammation potential by raising circulating lipopolysaccharide. Our findings demonstrate the safety concerns associated with using dietary emulsifiers, suggesting that they could lead to metabolic syndromes.

To expand the application of nobiletin (NOB) in semi-solid functional foods, bovine serum albumin (BSA)/carboxymethyl inulin (CMI) complexes-stabilized Pickering emulsion (BCPE) (φoil = 60%, v/v) was fabricated, and the swallowing index and bioavailability of the NOB-loaded Pickering emulsion was evaluated. Confocal laser scanning microscope (CLSM) and cryo-scanning electron microscopy (cryo-SEM) images revealed that BSA/CMI complexes attached to the oil–water interface. NOB-loaded BCPE exhibited a viscoelastic and shear-thinning behavior. Fork drip test results suggested that the textural value of unloaded and NOB-loaded emulsions was International Dysphagia Diet Standardisation Initiative Level 4, which could be swallowed directly without chewing. The in vitro lipolysis model suggested that NOB had a faster digestive profile and a higher bioaccessibility in the BCPE than in the oil suspension. The in vivo rat model revealed that the oral bioavailability of NOB was increased by 2.07 folds in BCPE compared to its bioavailability in unformulated oil. Moreover, BCPE led to a higher plasma concentration of the major demethylated metabolite of NOB (4′-demethylnobiletin) than the unformulated oil. Accordingly, BCPE enhanced the oral bioavailability of NOB by improving bioaccessibility, absorption, and biotransformation.

ABSTRACT Gut microbiota dysbiosis is causally related to inflammatory bowel disease (IBD), and increased levels of the gut metabolite ammonia have been proposed to contribute to IBD development. In this study, we aimed to clarify the anti-colitis mechanism of gallic acid (GA) based on its ability to trap the deleterious metabolite ammonia and improve gut microbiota. Aminated product was detected in the fecal samples of mice after oral gavage of gallic acid (GA) and identified as 4-amino-substituted gallic acid (4-NH2-GA), thus confirming the ability of GA to trap ammonia in vivo. Then, we compared the beneficial effects of GA and 4-NH2-GA on dextran sulfate sodium (DSS)-induced colitis mouse and found that both compounds managed to alleviate colitis phenotypes, indicating ammonia trapping had no adverse effect on the original anti-colitis activity of GA. In addition, both GA and 4-NH2-GA improved the gut microbiota dysbiosis induced by DSS, and fecal microbiota transplantation was subsequently performed, which further revealed that the gut microbiota mediated the anti-colitis activity of both GA and 4-NH2-GA. In summary, this study clarified that GA alleviated colitis by targeting both the symptoms and root causes: it directly reduced the deleterious metabolite ammonia by forming aminated metabolites without compromising the original anti-colitis activity, and it also improved gut microbiota dysbiosis, which in turn contributed to the alleviation of colitis. Since the GA structure is presented in various polyphenols as a common building block, the novel anti-colitis mechanism obtained from GA may also apply to other complex polyphenols.IMPORTANCEThe dysbiosis of the gut microbiota and its metabolism directly cause the emergence of IBD. In this study, we aimed to clarify the anti-colitis mechanism of GA in sight of gut microbiota and its metabolite ammonia. We discovered that GA directly captured and reduced the harmful metabolite ammonia in vivo to produce the aminated metabolite 4-NH2-GA, while the amination of GA had no adverse effect on its initial anti-colitis activity. In addition, both GA and its aminated metabolite improved the gut microbiota in colitis mice, and the modified gut microbiota, in turn, helped to relieve colitis. Since the GA structure is presented in diverse polyphenols as a common building block, the novel anti-colitis mechanism targeting the symptoms and root causes might also apply to other complex polyphenols.

ABSTRACT Diet and gut microbiota impact the progression of non-alcoholic steatohepatitis (NASH). An unhealthy diet, rich in fat and sugar, promotes gut microbiota dysbiosis, leading to the translocation of lipopolysaccharides (LPS) and other harmful pathogen-associated molecular patterns to the liver, triggering hepatic inflammation and aggravating NASH. Currently, there are no approved pharmacological treatments for NASH, although novel drugs, such as obeticholic acid (OCA), have demonstrated beneficial effects. Healthy dietary modifications have been proposed to prevent and treat NASH. However, the therapeutic effect of the combined implementation of a healthy dietary intervention with pharmaceutical agents or dietary supplements for NASH treatment and how it interplays with the gut microbiota and associated pathways remains poorly understood. This study aims to investigate the therapeutic efficacy of a healthy dietary modification, either alone or in combination with a dietary supplement [ginger essential oil (GEO)] or drug (OCA), in a Gubra-Amylin diet-induced NASH mouse model. NASH was induced for 12 weeks, after which the interventions were administered for a subsequent 3-week period. Our findings revealed that healthy dietary intervention primarily restores obesity, lipidemia, and NASH. In contrast, GEO and OCA have additional benefits by suppressing pro-inflammatory cytokines by partially modulating the NLRP3/ASC/caspase-1 pathways. Moreover, healthy dietary intervention restores gut microbiota composition and function from dysbiosis, while GEO and OCA partially mediate the gut-derived LPS/toll-like receptor 4/nuclear factor kappa B pathway. Therefore, adherence to healthy dietary patterns plays a primary role in NASH reversion, and additional supplementation of GEO or OCA could offer extra benefits in suppressing hepatic inflammation and preventing disease progression. IMPORTANCE The link between gut microbiota and diet is crucial in the development of non-alcoholic steatohepatitis (NASH). This study underscores the essential role of a healthy diet in preventing and treating NASH by reversing obesity, lipidemia, and gut microbiota dysbiosis. Moreover, the supplementation of functional food or drug to the diet can provide additional advantages by inhibiting hepatic inflammation through the modulation of the hepatic inflammasome signaling pathway and partially mediating the gut microbiota and lipopolysaccharide signaling pathway. This study highlights the importance of adopting healthy dietary habits in treating NASH and proposes that supplementing with ginger essential oil or obeticholic acid may offer additional benefits. Nonetheless, further clinical studies are necessary to validate these findings.

Abstract Recently, the role of the gut microbiota in diseases, including cardiovascular disease (CVD), has gained considerable research attention. Trimethylamine-N-oxide (TMAO), which is formed during ʟ-carnitine metabolism, promotes the formation of atherosclerotic plaques, causing thrombosis. Here, we elucidated the anti-atherosclerotic effect and mechanism of ginger (Zingiber officinale Roscoe) essential oil (GEO) and its bioactive compound citral in Gubra Amylin NASH (GAN) diet with ʟ-carnitine-induced atherosclerosis female ApoE−/− mice. Treatment with GEO at both low and high doses and citral inhibited the formation of aortic atherosclerotic lesions, improved plasma lipid profile, reduced blood sugar, improved insulin resistance, decreased plasma TMAO levels, and inhibited plasma inflammatory cytokines, especially interleukin-1β. Additionally, GEO and citral treatment modulated gut microbiota diversity and composition by increasing the abundance of beneficial microbes and decreasing the abundance of CVD-related microbes. Overall, these results showed that GEO and citral may serve as potential dietary supplements for CVD prevention by improving gut microbiota dysbiosis.

Considerable evidence indicates the important role of gut microbiota in human health. Through the interaction with the host and diet, it secretes a myriad of metabolites to modulate biological processes essential for health. Cognitive impairment is a common feature of psychiatric and neurological disorders, which may seriously damage the quality of patients' life. Studies have found that cognitive impairment has a close relationship with gut microbiota, and plant polysaccharides intervention to maintain intestinal micro-ecological balance has a great impact on ameliorating cognitive impairment. This review introduced the interaction between gut microbiota and plant polysaccharides, and focused on signaling pathogenesis of gut microbiota in cognitive impairment. The effect of plant polysaccharides intervention on regulation of gut microbiota was also discussed, so as to provide a promising strategy for ameliorating cognitive impairment.

Background and aim: Obesity is one of the complications of sedentary lifestyle and high-calorie food intake which become a global problem. Thermogenesis is a novel way to promote anti-obesity by consuming energy as heat rather than storing it as triacylglycerols. Over the last decade, growing evidence has identified the gut microbiota as a potential factor in the pathophysiology of obesity. Calebin A is a non-curcuminoid novel compound derived from the rhizome of medicinal turmeric with putative anti-obesity effects. However, its ability on promoting thermogenesis and modulating gut microbiota remain unclear. Experimental procedure: C57BL/6J mice were fed either normal diet or high-fat diet (HFD) supplement with calebin A (0.1 and 0.5%) diet for 12 weeks. The composition of the gut microbiota was assessed by analyzing 16S rRNA gene sequences. Results and conclusion: Mice treated with calebin A shows a remarkable alteration in microbiota composition compared with that of normal diet-fed or HFD-fed mice and is characterized by an enrichment of Akkermansia, Butyricicoccus, Ruminiclostridium_9, and unidentified_Ruminococcaceae. We also explored that calebin A reduce the weight and blood sugar of mice that are induced by HFD, and show a dose-dependent reaction. Moreover, calebin A decreases the weight of white, beige, and brown adipose tissue, and also restores liver weight. In cold exposure experiments, calebin A can better maintain rectal temperature through thermogenesis. In summary, calebin A has a good thermogenesis function and is effective in anti-obesity. It can be used as a novel gut microbiota modulator to prevent HFD-induced obesity.

Dietary nutrients are associated with the development of cardiovascular disease (CVD) both through traditional pathways (inducing hyperlipidemia and chronic inflammation) and through the emergence of a metaorganism-pathogenesis pathway (through the gut microbiota, its metabolites, and host). Several molecules from food play an important role as CVD risk-factor precursors either themselves or through the metabolism of the gut microbiome. Animal-based dietary proteins are the primary source of CVD risk-factor precursors; however, some plants also possess these precursors, though at relatively low levels compared with animal-source food products. Various medications have been developed to treat CVD through the gut-microbiota–circulation axis, and they exhibit potent effects in CVD treatment. Nevertheless, such medicines are still being improved, and there are many research gaps that need to be addressed. Furthermore, some medications have unpleasant or adverse effects. Numerous foods and herbs impart beneficial effects upon health and disease. In the past decade, many studies have focused on treating and preventing CVD by modulating the gut microbiota and their metabolites. This review provides an overview of the available information, summarizes current research related to the gut-microbiota–heart axis, enumerates the foods and herbs that are CVD-risk precursors, and illustrates how metabolites become CVD risk factors through the metabolism of gut microbiota. Moreover, we present perspectives on the application of foods and herbs—including prebiotics, probiotics, synbiotics, postbiotics, and antibiotic-like substances—as CVD prevention agents to modulate gut microbiota by inhibiting gut-derived CVD risk factors. Taxonomy (classification by EVISE): Cardiovascular disease, gut microbiota, herbal medicine, preventive medicine, dietary therapy, nutrition supplements.

The objective of our study was to analyze and identify enzymatic peptides from straw mushrooms that can enhance salty taste with the aim of developing saltiness enhancement peptides to reduce salt intake and promote dietary health. We isolated taste-related peptides from the straw mushroom extract using ultrafiltration and identified them using UPLC-Q-TOF-MS/MS. The study found that the ultrafiltration fraction (500–2000 Da) of straw mushroom peptides had a saltiness enhancement effect, as revealed via subsequent E-tongue and sensory analyses. The ultrafiltration fractions (500–2000 Da) were found to contain 220 peptides, which were identified through UPLC-Q-TOF-MS/MS analysis. The interaction of these peptides with the T1R1/T1R3 receptor was also assessed. The investigation highlighted the significant involvement of Asp223, Gln243, Leu232, Asp251, and Pro254 in binding peptides from triple-enzymatically hydrolyzed straw mushrooms to T1R1/T1R3. Based on the binding energy and active site analysis, three peptides were selected for synthesis: DFNALPFK (−9.2 kcal/mol), YNEDNGIVK (−8.8 kcal/mol), and VPGGQEIKDR (−8.9 kcal/mol). Importantly, 3.2 mmol of VPGGQEIKDR increased the saltiness level of a 0.05% NaCl solution to that of a 0.15% NaCl solution. Additionally, the addition of 0.8 mmol of YNEDNGIVK to a 0.05% NaCl solution resulted in the same level of saltiness as a 0.1% NaCl solution.

Background and aim: Cannabis sativa L. is a medicinal plant with a long history. Phyto-cannabinoids are a class of compounds from C. sativa L. with varieties of structures. Endocannabinoids exist in the human body. This article provides an overview of natural cannabinoids (phyto-cannabinoids and endocannabinoids) with an emphasis on their pharmacology activities. Experimental procedure: The keywords “Cannabis sativa L″, “cannabinoids”, and “central nervous system (CNS) diseases” were used for searching and collecting pieces of literature from PubMed, ScienceDirect, Web of Science, and Google Scholar. The data were extracted and analyzed to explore the effects of cannabinoids on CNS diseases. Result and conclusion: In this paper, schematic diagrams are used to intuitively show the phyto-cannabinoids skeletons’ mutual conversion and pharmacological activities, with special emphasis on their relevant pharmacological activities on central nervous system (CNS) diseases. It was found that the endocannabinoid system and microglia play a crucial role in the treatment of CNS diseases. In the past few years, pharmacological studies focused on Δ9-THC, CBD, and the endocannabinoids system. It is expected to encourage new studies on a more deep exploration of other types of cannabinoids and the mechanism of their pharmacological activities in the future.

ABSTRACT: In 2021, there are approximately 537 million adults ageing 2079 years affected by diabetes worldwide and the number is rising rapidly, hence it is important to manage and control diabetes mellitus and its associated complications. Food is one of the key factors in preventing and combating diseases such as diabetes. Both as a food and an herbal medicine, Polygonum multiflorum (PM) has been used as an anti-aging tonic, for hair darkening in traditional Chinese medicine for several centuries. The recent research effort of PM has been focused on antioxidant, anti-ageing and anti-tumor properties. In the present study, we utilized the traditional processing of harvested raw PM, and identified several stilbene components and then evaluated the potential anti-diabetic effects of the processed PM extract (PME). PME (0.075 %) was given to diabetic mice (KK CgAy/J) in drinking water and after 7 weeks, PME-treated mice had significantly lower glucose levels than mice in the diabetic control group (P < 0.01). The mechanism was explored with ELISA and Western blotting and results suggested that the effect was through maintaining β-cell function.

5-Demethylnobiletin (5-DMN), a hydroxylated polymethoxyflavone (OH-PMF) identified in aged citrus peels, has demonstrated health benefiting effects in previous studies. 5-DMN undergoes biotransformation in vivo, yielding 5,3'-didemethylnobiletin (5,3'-DDMN), 5,4'-didemethylnobiletin (5,4'-DDMN) and 5,3',4'-tridemethylnobiletin (5,3',4'-TDMN). However, the anti-cancer effects of 5-DMN and its in vivo metabolites against HepG2 cells remain unclear. In this study, an efficient chemical synthetic method was developed to obtain 5-DMN and its 3 metabolites, and their molecular structures were confirmed by 1H NMR and LC-MS. Cytotoxicity, cell cycle arrestment, apoptosis and caspase-3 expression were investigated to evaluate the anti-liver cancer effects of these OH-PMFs on HepG2 cells. The results showed that all 4 compounds inhibited the proliferation of HepG2 cells in a concentration-dependent manner. Their anti-proliferative activity was exerted through inducing G2/M phase arrestment, cell apoptosis and promoting expression of a key apoptotic protein called cleaved caspase-3. Our results indicated that 5,3'-DDMN and 5,3',4'-TDMN showed a stronger inhibitory activity on cell proliferation than 5-DMN, followed by 5,4'-DDMN. The expression of cleaved caspase-3 was the highest in cells treated with 5,4'-DDMN, implying that the apoptosis induced by other OH-PMFs might be mediated by other apoptotic execution proteins. Our research reveals the application potential and scientific evidence for the production and functionality of OH-PMFs.

ABSTRACT: Alzheimer’s disease (AD) is the most common neurodegenerative disease characterized by cognitive decline and memory impairment. Many lines of evidence indicate that excessive β-amyloid peptide (Aβ) generation and aggregation play pivotal roles in the initiation of AD, leading to various biochemical alteration including oxidative damage, mitochondrial dysfunction, neuroinflammation, signaling pathway and finally resulting in neuronal death. AD has a complex pathogenic mechanism, and a single-target approach for anti-AD strategy is thus full of challenges. To overcome these limitations, the present study focused to review on one of multiple target-compounds, (–)-epigallocatechin-3-gallate (EGCG) for the prevention and treatment of AD. EGCG is a main bioactive polyphenol in green tea and has been reported to exert potent neuroprotective properties in a wide array of both cellular and animal models in AD. This review demonstrated multiple neuroprotective efficacies of EGCG by focusing on the involvement of Aβ-evoked damage and its Aβ regulation. Furthermore, to understand its mechanism of action on the brain, the permeability of the blood-brain barrier was also discussed.

Tea is a widespread functional plant resource. Phytochemicals such as tea polyphenols (TP) can interact with the intestinal flora and participate in regulating the expression and rhythm of biological clock genes. Circadian rhythm controls a variety of behaviors and physiological processes, and circadian misalignment has been found to be closely related to multiple metabolic diseases. Interestingly, the gut microbiota also has diurnal fluctuations, which can be affected by diet composition and feeding rhythm, and play a role in maintaining the host’s circadian rhythm. The two-way relationship between the host’s circadian rhythm and intestinal microbiota confirms the possibility that prebiotics or probiotic can be used to adjust the intestinal environment and microbiome composition to improve the host health. This article reviews the relationship between the host’s circadian rhythm and microbiota and its influence on metabolic diseases. The beneficial effects of the interaction between TP and gut microbiota on diseases related to rhythm disorders are emphasized to improve the theories of disease prevention and treatment.

Tea as the most consumed beverage in the world has received enormous attention for its promoting health benefits. The deleterious effect of α-dicarbonyls and AGEs formed in Maillard reaction is also a long-term challenge. The connection between the two topics was the main aim of this review, to address and update the antiglycation effect and mechanism of tea and tea polyphenols. By analyzing recent publications, we have covered across chemistry models, cell lines and animal studies. Tea polyphenols, particularly catechins, showed outstanding antiglycation effect by trapping α-dicarbonyl compounds and impeding AGEs formation. Reduction of carbonyl stress brought alleviation to aging, diabetes, and collagen related diseases or complications through regulation of RAGE expression and subsequent MAPK and TGF-β pathway. Therefore, tea polyphenols can serve as promising natural candidates in the treatment and/or prevention of nephropathy, retinopathy, hepatopathy, hyperglycemia and obesity among others, by their potent antiglycation effect. Further studies need to address on aspects like exact mechanisms, solution of detection obstacles, balance of practical usage and harmful effects such as potential flavor damage and toxicity in food, to gain a comprehensive understanding of antiglycation activities of tea polyphenols and its actual application.

ABSTRACT: Tea polyphenols (TPPs) have attracted significant research interest due to their health benefits. However, TPPs are sensitive to certain environmental and gastrointestinal conditions and their oral bioavailability was found to be very low. Delivery systems made of food-grade materials have been reported to improve the shelf-life, bioavailability and bioefficacy of TPPs. This review discusses the chemistry of TPPs; the setbacks of TPPs for application; and the strategies to counteract application limitations by rationally designing delivery systems. An overview of different formulations used to encapsulate TPPs is provided in this study, such as emulsion-based systems (liposome, nanoemulsion, double emulsion, and Pickering emulsion) and nano/microparticles-based systems (protein-based, carbohydrate-based, and bi-polymer based). In addition, the stability, bioavailability and bioactivities of encapsulated TPPs are evaluated by various in vitro and in vivo models. The current findings provide scientific insights in encapsulation approaches for the delivery of TPPs, which can be of great value to TPPs-fortified food products. Further explorations are needed for the encapsulated TPPs in terms of their applications in the real food industry as well as their biological fate and functional pathways in vivo.

Larger-leaf yellow tea (LYT) is a characteristic type of Chinese tea produced in Huoshan County, Anhui Province, which is made by mature leaves with stems. According to recent report, LYT showed competitive effects in anti-hyperglycemia in comparison to other teas such as green or black tea. However, the bioactive compounds of LYT are still undiscovered so far. For this purpose, 5 fractions of LYT were prepared by sequential extraction. The in vitro bioassay results indicated that the ethyl acetate fraction of LYT had the strongest inhibitory effects on α-glucosidase and α-amylase. Fluorescence-quenching analysis and protein-binding test revealed that the compounds of ethyl acetate fraction could inhibit α-glucosidase and α-amylase activities through binding to enzymes or other mechanisms. All chromatographic peaks of high-performance liquid chromatography (HPLC) of ethyl acetate fraction were separated and collected. The purified compounds were identified by liquid chromatography-mass spectrometry (LC-MS), and subsequently screened by calculating their inhibition ratio on α-glucosidase at the real concentration in LYT infusion. The results showed that (–)-epigallocatechin gallate, (–)-gallocatechin gallate, caffeine, N-ethyl-2-pyrrolidone-substituted flavan-3-ols were effective inhibitors for α-glucosidase.

ABSTRACT: Oolong tea, partially fermented from Camellia sinensis leaves, exhibits significant antioxidative, anti-inflammatory, and anti-cancer activities as indicated in several in vitro and in vivo studies. However, studies on health promoting effects of oolong tea and its characteristic compounds are limited. The potential efficacy of bioactives derived from oolong tea and their roles as promising anticancer agents, their cardio-protective benefits during hypoxic conditions, effects in treating allergic disorders, potential prebiotic activities, improvement of blood lipid status in human beings, effectivity as oral hypoglycemic agent in the treatment of type 2 diabetes, and their potentials to reduce the risk of obesity have been discussed in this review. These promising studies mainly gained from animal studies might broaden the consumption and usage of the phenolic-enriched oolong tea and its products in food and pharmaceutical industries. However, potential health beneficial effects of oolong tea in humans should be further complemented by large-sized, randomized double-blind and placebo-controlled trials to consolidate potential therapeutic applications.

ABSTRACT: Both tea polyphenols and selenium (Se) have been suggested to exert the health benefits via the regulatory capacities of chronic inflammation, which make Se-enriched oolong tea a promising beverage as an anti-inflammatory diet. The aim of this study is to investigate the anti-inflammatory effects of Se-enriched oolong tea extract (Se-TE) and underlying mechanism in lipopolysaccharide (LPS)-induced RAW264.7 cells. Se-TE treatments (50 and 150 μg/mL) significantly suppressed the over-production of nitric oxide (NO) and prostaglandin E2 (PGE2) in LPS-stimulated macrophages via downregulating the expression of nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Moreover, Se-TEs also effectively inhibited the productions of inflammatory cytokines, such as tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-1β (IL-1β). Furthermore, Se-TE could block mitogen-activated protein kinase (MAPK) and nuclear factor-kappa B (NF-κB) signaling pathways through the inhibition of the phosphorylation of key proteins (IκB-α, p65, p38, ERK, and JNK) and the translocation of the p65 subunit into the nucleus. Collectively, our results indicated that Se-TE may have the potential to be used as a novel food ingredient for the development of various anti-inflammatory foods and the treatment and prevention of chronic inflammation-related diseases.

Roasting is a common manufacture technology for processing various teas. It is not only used in decreasing the water content of finished tea, but also improving the flavor of teas. In the present study, the roasted and non-roasted teas were compared by liquid-chromatography mass spectrometry and sensory evaluation. The roasted tea tasted less bitter and astringent. The content of main galloylated and simple catechins, caffeine and theobromine in roasted were significantly lower than non-roasted teas. Targeted taste-compounds metabolomics revealed that (–)-epigallocatechin gallate, kaempferol-glucose-rhamnose-glucose and (–)-epicatechin gallate were main contributors tightly correlated to astringent intensity. Flavonol glycosides including kaempferol-glucose, quercetin-glucose, kaempferol-glucose-rhamnose-glucose, and quercetin-glucose-rhamnose-glucose in roasted teas were also significantly less than non-roasted teas. To study the chemical changes during roasting, tea with a strong astringency was roasted under 80, 100, 120, 140, and 160 °C. With the increase of roasting temperature, the bitter and astringent intensity of tea was gradually decreased, but the main astringent compounds including (–)-epigallocatechin, (–)-epigallocatechin gallate and kaempferol/quercetin glycosides were irregularly varied with temperature. The Pearson correlation coefficient analysis suggested procyanidin B2, coumaroylquinic acids and gallotannins were tightly correlated to the astringent and bitter perceptions, while N-ethyl-2-pyrrolidone-substituted flavan-3-ols were negatively correlated.

Pu-erh ripen tea becomes popular worldwide owing to its unique taste and aroma. In the present study, volatile compounds from Pu-erh ripen tea were extracted using a solvent assisted flavor evaporation (SAFE) and analyzed with a gas chromatography-mass spectrometry (GC-MS) and a gas chromatography olfactometry (GC-O). Results demonstrated that 58 major volatile compounds and 24 aroma active substances of Pu-erh ripen tea were identified by GC-MS and GC-O analysis. Among volatile compounds identified, methoxyphenyl compounds were considered as the dominate compounds in the aroma of Pu-erh ripen tea. Further investigation showed that 6 methoxybenzenes were responsible for the aging aroma in Pu-erh ripen tea; α-ionone, 3,4-dimethoxytoluene, 1,3-dimethoxybenzene, etc. were responsible for the wood-like aroma. Linalool, α-terpineol, α-ionone, β-ionone, and benzeneacetaldehyde were responsible for the floral odor. Compared the odor detection threshold (ODT) among the 8 methoxyphenyl compounds in water, 1,2,3-trimethoxybenzene showed the highest ODT, followed by 3,4-dimethoxyphenol. 1,3-Dimethoxybenzene (105 μg/L) and 1,2,3-trimethoxy-5-methylbenzene (100 μg/L) were present at relatively low odor threshold values. The result indicated that methoxyphenyl compounds play a vital role in the unique flavor of Pu-erh ripen tea.

Tea polysaccharides (TPSs), one of the major bioactive ingredients in tea, have been widely studied due to their variety of biological activities, including antioxidant, cancer prevention, hypoglycemia, anti-fatigue, anti-coagulant, anti-obesity and immunomodulatory effect. The biological effectiveness of TPSs has direct relation with their structures such as monosaccharide composition, molecular weight, glycosidic linkages, conformation and others, which can be influenced by tea materials, processing methods, extraction and purification procedures among others. Comparing to the study of tea polyphenols, the exploration of TPSs in structural elucidation and biofunctionality is very preliminary. Yet several factors affecting the structural change of TPSs have been studied and identified. Consequently, the variation of some TPS biological activity brought by the change of TPS structures has been evaluated and preliminary correlation of structure activity relationship of TPSs has been performed. Therefore, this review aims to serve as a summary research report regarding the influencing factors on TPSs structures and consequential effects on the biological activities of TPSs. We hope to provide updated information and systematic references for future study and functional food development of TPSs.

ABSTRACT: Myriad evidence attests to the health-promoting benefits of tea drinking. While there are multiple factors of tea influencing the effective biological properties, tea polyphenols are the most significant and valuable components. The chemical characterization and physical characteristics of tea polyphenols have been comprehensively studied over the previous years. Still the emergence of new chemistry in tea, particularly the property of scavenging reactive carbonyl species (RCS) and the newly discovered flavoalkaloid compounds, has drawn increasing attention. In this review, we summarize recent findings of a new class of compounds in tea - flavonoid alkaloids (flavoalkaloids), which exist in fresh tea leaves and can be generated during the process of post-harvesting, and also postulate the formation mechanism of flavoalkaloids between catechins and theanine-derived Strecker aldehyde. Additionally, we detail the up-to-date research results of tea polyphenols regarding their ability to trap RCS and their in vivo aminated metabolites to suppress advanced glycation ends products (AGEs). We further raise questions to be addressed in the near future, including the synthetic pathways for the generation of flavoalkaloids and AGEs in fresh tea leaves before processing and the concentrations of tea polyphenols that affect their RCS scavenging capability due to their pro-oxidant nature. More intensive research is warranted to elucidate the mechanisms of action underlying the biological activity of flavoalkaloids and the pharmacological application of tea polyphenols in scavenging RCS and impeding detrimental AGEs.

Marine polyphenols, including eckol(EK), dieckol(DK), and 8,8’-bieckol(BK), have attracted attention as bioactive ingredients for preventing Alzheimer’s disease (AD). Since AD is a multifactorial disorder, the present study aims to provide an unbiased elucidation of unexplored targets of AD mechanisms and a systematic prediction of effective preventive combinations of marine polyphenols. Based on the omics data between each compound and AD, a protein–protein interaction (PPI) network was constructed to predict potential hub genes. Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analyses were performed to provide further biological insights. In the PPI network of the top 10 hub genes, AKT1, SRC, EGFR, and ESR1 were common targets of EK and BK, whereas PTGS2 was a common target of DK and BK. GO and KEGG pathway analysis revealed that the overlapped genes between each compound and AD were mainly enriched in EGFR tyrosine kinase inhibitor resistance, the MAPK pathway, and the Rap1 and Ras pathways. Finally, docking validation showed stable binding between marine polyphenols and their top hub gene via the lowest binding energy and multiple interactions. The results expanded potential mechanisms and novel targets for AD, and also provided a system-level insight into the molecular targets of marine polyphenols against AD.

Actinidia arguta leaves (AAL) are an excellent source of bioactive components for the food industry and possess many functional properties. However, the hypoglycemic effect and mechanism of AAL remain unclear. The aim of this work was to investigate the potential hypoglycemic effect of AAL and explore its possible mechanism using 16S rRNA sequencing and serum metabolomics in diabetic mice induced by high-fat feeding in combination with streptozotocin injection. A total of 25 flavonoids from AAL were isolated and characterized, and the contents of the extract from the AAL ranged from 0.14 mg/g DW to 8.97 mg/g DW. The compound quercetin (2) had the highest content of 8.97 ± 0.09 mg/g DW, and the compound kaempferol-3-O-(2′-O-D-glucopyl)-β-D-rutinoside (12) had the lowest content of 0.14 ± 0.01 mg/g DW. In vivo experimental studies showed that AAL reduced blood glucose and cholesterol levels, improved insulin sensitivity, and ameliorated oxidative stress and liver and kidney pathological damage. In addition, gut microbiota analysis found that AAL significantly reduced the F/B ratio, enriched the beneficial bacteria Bacteroides and Bifidobacterium, and inhibited the harmful bacteria Lactobacillus and Desulfovibrio, thereby playing an active role in intestinal imbalance. In addition, metabolomics analysis showed that AAL could improve amino acid metabolism and arachidonic acid metabolism, thereby exerting a hypoglycemic effect. This study confirmed that AAL can alleviate type 2 diabetes mellitus (T2DM) by regulating intestinal flora and interfering with related metabolic pathways, providing a scientific basis for its use as a dietary supplement and for further exploration of the mechanism of AAL against T2DM.

Abstract Cardiovascular disease (CVD) is strongly associated with the gut microbiota and its metabolites, including trimethylamine-N-oxide (TMAO), formed from metaorganismal metabolism of ʟ-carnitine. Raw garlic juice, with allicin as its primary compound, exhibits considerable effects on the gut microbiota. This study validated the benefits of raw garlic juice against CVD risk via modulation of the gut microbiota and its metabolites. Allicin supplementation significantly decreased serum TMAO in ʟ-carnitine-fed C57BL/6 J mice, reduced aortic lesions, and altered the fecal microbiota in carnitine-induced, atherosclerosis-prone, apolipoprotein E-deficient (ApoE−/−) mice. In human subjects exhibiting high-TMAO production, raw garlic juice intake for a week reduced TMAO formation, improved gut microbial diversity, and increased the relative abundances of beneficial bacteria. In in vitro and ex vivo studies, raw garlic juice and allicin inhibited γ-butyrobetaine (γBB) and trimethylamine production by the gut microbiota. Thus, raw garlic juice and allicin can potentially prevent cardiovascular disease by decreasing TMAO production via gut microbiota modulation.

ABSTRACT: Increasing interest in attaining an optimal health have longstanding and are imperative for consumers, medical and health researchers and functional food scientists and producers among others. Functional food is defined as foods that have a biological function with a very broad range of coverage including natural and conventional foods with reported bioactivities, dietary supplements and medical foods. Its concept is inclusively broad and ambiguous. Medical food is a specific class of functional foods with clear definition and limited coverage to guarantee its integrity. This review introduced the definition of medical food by the US Food and Drug Administration, intended to clarify the differences among medical food, dietary supplements and conventional foods, and listed some examples of medical food products developed in the US.

In thermally processed foods, several heat-induced toxicants are potentially formed due to the Maillard reaction, such as α-dicarbonyls and advanced glycation end products (AGEs). In the present work, we found that the methylglyoxal (MGO)-trapping and antiglycative activities of the herbal tea samples correlated strongly with their total phenolic and flavonoid contents. Among the tested herbal tea samples, rooibos exhibited the strongest MGO-trapping and antiglycative activities against AGEs formation. Aspalathin, orientin and isoorientin were further identified as the major bioactive compounds of rooibos that scavenged MGO to form the corresponding mono-MGO adducts. Moreover, the contents of dicarbonyls and AGEs in the cookie were remarkably reduced by fortification with rooibos. Altogether, our current findings suggested that rooibos might serve as a functional ingredient to reduce intake of dietary reactive carbonyl species (RCS) and AGEs from thermally processed foods, especially bakery products.

Selenium nanoparticles (SeNPs) have gained extensive attention for their excellent biological activity and low toxicity. However, SeNPs are extremely liable to aggregate into non-bioactive or gray elemental selenium, which limits their application in the biomedicine field. This study aimed to prepare stable SeNPs by using lentinan (LNT) as a template and evaluate its anti-colon cancer activity. The average particle diameter of obtained lentinan-selenium nanoparticles (LNT-SeNPs) was approximately 59 nm and presented zero-valent, amorphous, and spherical structures. The monodisperse SeNPs were stabilized by LNT through hydrogen bonding interactions. LNT-SeNPs solution remained highly stable at 4°C for at least 8 weeks. The stability of LNT-SeNPs solution sharply decreased under high temperature and strong acidic conditions. LNT-SeNPs showed no obvious cytotoxic effect on normal cells (IEC-6) but significantly inhibited the proliferation of five colon cancer cells (HCT-116, HT-29, Caco-2, SW620, and CT26). Among them, LNT-SeNPs exhibited the highest sensitivity toward HCT-116 cells with an IC50 value of 7.65 μM. Also, LNT-SeNPs displayed better cancer cell selectivity than sodium selenite and selenomethionine. Moreover, LNT-SeNPs promoted apoptosis of HCT-116 cells through activating mitochondria-mediated apoptotic pathway. Meanwhile, LNT-SeNPs induced cell cycle arrest at G0/G1 phase in HCT-116 cells via modulation of cell cycle regulatory proteins. The results of this study indicated that LNT-SeNPs possessed strong potential application in the treatment of colorectal cancer (CRC).

ABSTRACT Antibiotics used as growth promoters in livestock and animal husbandry can be detected in animal-derived food. Epidemiological studies have indicated that exposure to these antibiotic residues in food may be associated with childhood obesity. Herein, the effect of exposure to a residual dose of tylosin—an antibiotic growth promoter—on host metabolism and gut microbiota was explored in vivo. Theoretical maximal daily intake (TMDI) doses of tylosin were found to facilitate high-fat-diet-induced obesity, induce insulin resistance, and perturb gut microbiota composition in mice. The obesity-related phenotypes were transferrable to germfree recipient mice, indicating that the effects of a TMDI dose of tylosin on obesity and insulin resistance occurred mainly via alteration of the gut microbiota. Tylosin TMDI exposure restricted to early life, the critical period of gut microbiota development, altered the abundance of specific bacteria related to host metabolic homeostasis later in life. Moreover, early-life exposure to tylosin TMDI doses was sufficient to modify the ratio of primary to secondary bile acids, thereby inducing lasting metabolic consequences via the downstream FGF15 signaling pathway. Altogether, these findings demonstrate that exposure to very low doses of antibiotic residues, whether continuously or in early life, could exert long-lasting effects on host metabolism by altering the gut microbiota and its metabolites. IMPORTANCE This study demonstrates that even with limited exposure in early life, a residual dose of tylosin might cause long-lasting metabolic disturbances by altering the gut microbiota and its metabolites. Our findings reveal that the gut microbiota is susceptible to previously ignored environmental factors.

The chemical structure of GLP-1, a novel water-soluble heteropolysaccharide purified Ganoderma leucocontextum fruiting bodies, has been characterized in our previous study. This study aimed to investigate the immunostimulatory activity of GLP-1 in vitro and in vivo by using RAW264.7 macrophages and cyclophosphamide-induced immunosuppressed mice model. Results showed that GLP-1 was able to enhance phagocytic activity and promote the production of reactive oxygen species, nitric oxide, tumor necrosis factor-α, interleukin-6, and monocyte chemoattractant protein-1 in RAW264.7 macrophages. Moreover, GLP-1 could activate mitogen-activated protein kinase, phosphatidylinositol-3-kinase/protein kinase B, and nuclear factor-kappa B signaling pathways through toll-like receptor 2 and dectin-1 receptors. Furthermore, GLP-1 increased the thymus index, serum immunoglobulin levels, and percentage of CD3+ T lymphocytes in cyclophosphamide-induced immunosuppressed mice. These results demonstrated that GLP-1 possessed significant immunostimulatory effects in vivo and in vitro and could be developed as an effective immunomodulator for application in functional foods.

To objectively classify and evaluate the strong aroma base liquors (SABLs) of different grades, solid-phase microextraction-mass spectrometry (SPME-MS) combined with chemometrics were used. Results showed that SPME-MS combined with a back-propagation artificial neural network (BPANN) method yielded almost the same recognition performance compared to linear discriminant analysis (LDA) in distinguishing different grades of SABL, with 84% recognition rate for the test set. Partial least squares (PLS), successive projection algorithm partial least squares (SPA-PLS) model, and competitive adaptive reweighed sampling-partial least squares (CARS-PLS) were established for the prediction of the four esters in the SABL. CARS-PLS model showed a greater advantage in the quantitative analysis of ethyl acetate, ethyl butyrate, ethyl caproate, and ethyl lactate. These results corroborated the hypothesis that SPME-MS combined with chemometrics can effectively achieve an accurate determination of different grades of SABL and prediction performance of esters.

Crude rice bran oils from different rice cultivars and extraction methods bear different contents of nutraceuticals. The health benefits of lowering cholesterol activity of rice bran oil being confirmed by many reports are partly attributed to non-nutrient nutraceuticals, especially γ-oryzanol, phytosterols, and policosanols. As the world has been facing the global warming crisis, green extraction technology is gaining attention from many sectors. The current study aims to compare the nutraceutical composition with respect to γ-oryzanol, phytosterol, and policosanol content as well as the antioxidant properties of crude rice bran oils extracted from white and red rice bran using three green technologies, comparing with conventional hexane extraction. The data show that the traditional solvent extraction gave the highest oil yield percentage (26%), but it was not significantly different from subcritical liquefied dimethyl ether extraction (24.6%). Subcritical liquefied dimethyl ether extraction gave higher oil yield than supercritical CO2 extraction (15.5–16.2%). The crude rice bran oil extracted using subcritical liquefied dimethyl ether extraction produced the highest total phenolic contents and antioxidant activities. The highest γ-oryzanol content of the crude rice bran oil was found in oil extracted by conventional cold press (1370.43 mg/100 g). The γ-oryzanol content of the oil obtained via subcritical liquefied dimethyl ether extraction was high (1213.64 mg/100 g) compared with supercritical CO2 extraction. The red rice bran yielded the crude rice bran oil with the highest total phytosterol content compared with the white bran, and the oil from red rice bran extracted with subcritical liquefied dimethyl ether generated the highest total phytosterol content (1784.17 mg/100 g). The highest policosanol content (274.40 mg/100 g) was also found in oil obtained via subcritical liquefied dimethyl ether extraction.

Oxyresveratrol (ORes, trans-2,4,3′,5′-tetrahydroxy stilbene) naturally exists in mulberry, grapes, peanuts and other plants. It belongs to stilbene polyphenolic family and has an extra hydroxyl group at 2-position comparing with resveratrol (Res). Hence, ORes has stronger antioxidant activity than resveratrol. In present study, we employed a rat hepatic fibrosis model induced by carbon tetrachloride (CCl4) and administrated ORes via gavage feeding to study the protective effects and potential mechanisms of ORes against hepatic fibrosis. We demonstrated that rat liver oxidative damage induced by CCl4 was significantly alleviated after ORes feeding. Furthermore, the mRNA transcription levels of α-smooth muscle actinn (α-SMA), desmin, and two MMPs (MMP2 and MMP9) were reduced and the expression levels of transforming growth factor β1 (TGF-β1), p- small mother against decapen-taplegic protein (Smad)1/2 and p-extracellular signal-regulated kinases (ERK)1/2 in the liver tissue down-regulated dramatically. In a parallel study with Res, ORes showed more efficacious protective effect than Res against rat liver fibrosis, which is attributed to extended conjugation system due to the extra hydroxyl group at 2-position on ORes making it more electron-rich and susceptible to oxidation than Res. Therefore, dietary consumption of mulberry and other fruits containing ORes may be beneficial in the prevention of liver fibrosis.

Coronavirus disease 2019 (COVID-19) disrupts the intestinal micro-ecological balance, and patients often develop the intestinal disease. The gut is the largest immune organ in the human body; intestinal microbes can affect the immune function of the lungs through the gut-lung axis. It has been reported that tea polyphenols (TPs) have antiviral and prebiotic activity. In this review, we discussed TPs reduced lung-related diseases through gut-lung axis by inhibiting dysbiosis. In addition, we also highlighted the preventive and therapeutic effects of TPs on COVID-19 complications, further demonstrating the importance of research on TPs for the prevention and treatment of COVID-19 in humans. Based on this understanding, we recommend using TPs to regulate the gut microbiota to prevent or alleviate COVID-19 through the gut-lung axis.

A water-soluble heteropolysaccharide (SGP2-1) was purified from Suillus granulatus fruiting bodies by anion-exchange chromatography and gel permeation chromatography. The structural characteristics were analyzed by high-performance gel permeation chromatography, high-performance liquid chromatography, Fourier transform infrared spectroscopy, gas chromatography-mass spectrometry, and nuclear magnetic resonance spectroscopy. The immunostimulatory activity was investigated using RAW 264.7 macrophages. Results showed that SGP2-1 with weight average molecular weight of 150.75 kDa was composed of mannose, glucose, and xylose. The backbone of SGP2-1 was mainly composed of → 4)-α-Glcp-(1→, and the terminal group α-d-Glcp → was linked to the main chain by O-6 position. SGP2-1 could significantly enhance pinocytic capacity, reactive oxygen species production, and cytokines secretion. SGP2-1 exerted immunomodulatory effects through interacting with toll-like receptor 2, and activating mitogen-activated protein kinase, phosphatidylinositol-3-kinase/protein kinase B, and nuclear factor-kappa B signaling pathways. These findings indicated that SGP2-1 could be explored as a potential immunomodulatory agent for application in functional foods.

Abstract Background Tea plant (Camellia sinensis) is one of the world’s most important beverage crops due to its numerous secondary metabolites conferring tea quality and health effects. However, only a small fraction of tea genes (especially for those metabolite-related genes) have been functionally characterized to date. A cohesive bioinformatics platform is thus urgently needed to aid in the functional determination of the remaining genes. Description TeaCoN, a database of gene co-expression network for tea plant, was established to provide genome-wide associations in gene co-expression to survey gene modules (i.e., co-expressed gene sets) for a function of interest. TeaCoN featured a comprehensive collection of 261 high-quality RNA-Seq experiments that covered a wide range of tea tissues as well as various treatments for tea plant. In the current version of TeaCoN, 31,968 (94% coverage of the genome) tea gene models were documented. Users can retrieve detailed co-expression information for gene(s) of interest in four aspects: 1) co-expressed genes with the corresponding Pearson correlation coefficients (PCC-values) and statistical P-values, 2) gene information (gene ID, description, symbol, alias, chromosomal location, GO and KEGG annotation), 3) expression profile heatmap of co-expressed genes across seven main tea tissues (e.g., leaf, bud, stem, root), and 4) network visualization of co-expressed genes. We also implemented a gene co-expression analysis, BLAST search function, GO and KEGG enrichment analysis, and genome browser to facilitate use of the database. Conclusion The TeaCoN project can serve as a beneficial platform for candidate gene screening and functional exploration of important agronomical traits in tea plant. TeaCoN is freely available at http://teacon.wchoda.com .

A novel coronavirus disease (COVID-19), transmitted from humans to humans, has rapidly become the pandemic responsible for the current global health crisis. COVID-19 is caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), which is said to be of zoonotic origin. This review describes the etiology and signs and symptoms as well as the current allopathic therapy for COVID-19. Additionally, findings of previous studies on the immunomodulatory effects and antiviral activities of particular foods and herbs on influenza virus and coronaviruses have been collated, with the aim of promoting the use of dietary therapy and herbal medicine as COVID-19 preventive therapies, while specific drugs and vaccines are yet to be discovered or are still under development. The volume of existing reports is irrefutable evidence that foods and herbs possess a potential antiviral ability against SARS-CoV-2 and can prevent COVID-19. Foods and herbs could be used as dietary or complementary therapy to prevent infection and strengthen immunity, as antiviral agents for masks, as disinfectants to curb aerosol transmission, or as sanitizing agents to disinfect surfaces. However, these hypotheses need to be experimentally verified for SARS-CoV-2 and COVID-19 patients.

Longan (Dimocarpus longan Lour.), as an edible fruit and traditional Chinese medicine, has been consumed for thousands of years. Longan pulp has abundant nutritional phytochemicals such as protein, carbohydrate, vitamin C, polysaccharides, polyphenols, which shows multiple biological activities including antioxidant, immunomodulatory and antitumor effects. Longan pericarp also demonstrates biological activities because of its rich content of polysaccharides and polyphenols. This review summarizes the bioactive compounds and bioactivities of longan pulp and aims to provide comprehensive information for future development of longan as a functional health food.

Stilbene compounds existing in edible berries have attracted much attention due to their efficacious health-promoting properties such as antioxidant, anti-aging, modulation of metabolic diseases and cancer prevention among others. Pterostilbene has superior pharmacokinetic profile over hydroxylated stilbenes such as resveratrol and oxyresveratrol. Hence, the current study was to evaluate the anti-hepatic fibrosis effects of pterostilbene in direct comparison to two hydroxylated stilbene compounds. In a carbon tetrachloride (CCl4) stimulated hepatic fibrosis model, rats were co-administrated with pterostilbene and hydroxystilbene via gavage feeding. Results revealed that stilbenes exerted significant efficacious protective effects against rat liver fibrosis, by reducing the expression levels of α-SMA, desmin, MMP2 and MMP9 and down-regulating the expression ofTGF-β1, phosphorylated Smad1/2 and ERK1/2 in the liver tissue, among which pterostilbene demonstrated much potent preventive activity than the hydroxylated stilbenes.

A kind of hydroxylated polymethoxyflavone (PMFs) existing in the citrus genus, 5-Demethyltangeretin (5-DTAN), has been reported to possess several bioactivities in vitro and in vivo. The aim of this study was to investigate whether acetylation could enhance the anticancer activity and oral bioavailability of 5-DTAN. PC-3 human prostate cancer cells were treated with tangeretin (TAN), 5-DTAN, and 5-acetylated TAN (5-ATAN), and the results showed that the cytotoxic effect 5-ATAN (IC50 value of 5.1 µM) on the cell viability of PC-3 cells was stronger than that of TAN (IC50 value of 17.2 µM) and 5-DTAN (IC50 value of 11.8 µM). Compared to 5-DTAN, 5-ATAN treatment caused a more pronounced DNA ladder, increased the sub-G1 phase population, and induced G2/M phase arrest in the cell cycle of PC-3 cells. We also found that 5-ATAN triggered the activation of caspase-3 and the progression of the intrinsic mitochondrial pathway in PC-3 cells, suggesting the induction of apoptosis. In a cell wound healing test, 5-ATAN dose-dependently reduced the cell migration, and the expression of matrix metalloproteinase-2 (MMP-2) and matrix metalloproteinase-9 (MMP-9) was decreased after 48 h of 5-ATAN treatment. Moreover, oral administration of 5-ATAN showed a significantly stronger inhibitory effect on tumor size and tumor weight in tumor-bearing nude mice than those of vehicle or the 5-DTAN group (p < 0.05). Furthermore, pharmacokinetic results showed that single-dose oral administration of 5-ATAN exhibited a higher maximum concentration (Cmax) and area under the curve (AUC) of 5-DTAN in plasma than that of 5-DTAN. More extensive distribution of 5-DTAN to most tissues of mice was also observed in mice treated with 5-ATAN for 7 days. In conclusion, acetylation strongly enhances the anticancer activity and oral bioavailability of 5-DTAN and could be a promising strategy to promote the potential bioactivities of natural products.

Extracting nutraceuticals with high value from bagasse, filter mud, and sugarcane leaves discarded as sugar mill by-products, is crucial for the development of a sustainable bio-economy. These by-products are important sources of policosanols and phytosterols, which have a cholesterol-lowering effect. This research focused on using a promising green technology, subcritical liquefied dimethyl ether extraction, with a low pressure of 0.8 MPa, to extract policosanols and phytosterols and on application of pretreatments to increase their contents. For direct extraction by subcritical liquefied dimethyl ether without sample pretreatment, the highest extraction yield (7.4%) and policosanol content were found in sugarcane leaves at 2888 mg/100 g, while the highest and lowest phytosterol contents were found in filter mud at 20,878.75 mg/100 g and sugarcane leaves at 10,147.75 mg/100 g, respectively. Pretreatment of filter mud by ultrasonication in hexane solution together with transesterification before the second subcritical liquefied dimethyl ether extraction successfully increased the policosanol content, with an extract purity of 60%, but failed to increase the phytosterol content.

Forty compounds were isolated and characterized from A. tenuissimum flower. Among them, twelve flavonoids showed higher α−glucosidase inhibition activities in vitro than acarbose, especially kaempferol. The molecular docking results showed that the binding of kaempferol to α−glucosidase (GAA) could reduce the hydrolysis of substrates by GAA and reduce the glucose produced by hydrolysis, thus exhibiting α−glucosidase inhibition activities. The in vivo experiment results showed that flavonoids−rich A. tenuissimum flower could decrease blood glucose and reduce lipid accumulation. The protein expression levels of RAC−alpha serine/threonine−protein kinase (AKT1), peroxisome proliferator activated receptor gamma (PPARG), and prostaglandin G/H synthase 2 (PTGS2) in liver tissue were increased. In addition, the Firmicutes/Bacteroidetes (F/B) ratio was increased, the level of gut probiotics Bifidobacterium was increased, and the levels of Enterobacteriaceae and Staphylococcus were decreased. The carbohydrate metabolism, lipid metabolism, and other pathways related to type 2 diabetes mellitus were activated. This study indicating flavonoids−rich A. tenuissimum flower could improve glycolipid metabolic disorders and inflammation in diabetic mice by modulating the protein expression and gut microbiota.

Musa (ABB group) “Kluai Namwa” bananas (Musa sp.) are widely grown throughout Thailand. Mali Ong is the most popular Kluai Namwa variety used as raw material for sun-dried banana production, especially in the Bangkratum District, Phitsanulok, Thailand. The sun-dried banana product made from Nanwa Mali Ong is well recognized as the best dried banana product of the country, with optimal taste compared to one made from other Kluai Namwa varieties. However, the production of Mali Ong has fluctuated substantially in recent years, leading to shortages. Consequently, farmers have turned to using other Kluai Namwa varieties including Nuanchan. This study investigated the nutraceutical contents of two popular Namwa varieties, Mali Ong and Nuanchan, at different ripening stages. Nutraceuticals in the dried banana products made from these two Kluai Namwa varieties and four commercial dried banana products were compared. Results indicated that the content of moisture, total sugar, and total soluble solids (TSS) (°Brix) increased, while total solids and texture values decreased during the ripening stage for both Kluai Namwa varieties. Rutin was the major flavonoid found in both Namwa Mali Ong and Nuanchan varieties ranging 136.00–204.89 mg/kg and 129.15–260.38 mg/kg, respectively. Rutin, naringenin, quercetin and catechin were abundant in both Namwa varieties. All flavonoids increased with ripening except for rutin, gallocatechin and gallocatechin gallate. There were no significant differences (p < 0.05) in flavonoid contents between both varieties. Tannic acid, ellagic acid, gallic acid, chlorogenic acid and ferulic acid were the main phenolic acids found in Mali Ong and Nuanchan varieties, ranging from 274.61–339.56 mg/kg and 293.13–372.66 mg/kg, respectively. Phenolic contents of both varieties decreased, increased and then decreased again during the development stage. Dopamine contents increased from 79.26 to 111.77 mg/kg and 60.38 to 125.07 mg/kg for Mali Ong and Nuanchan, respectively, but the amounts were not significantly different (p < 0.5) between the two Namwa varieties at each ripening stage. Inulin as fructooligosaccharide (FOS) increased with ripening steps. Production stages of sun-dried banana products showed no statistically significant differences (p < 0.05) between the two Namwa varieties. Therefore, when one variety is scarce, the other could be used as a replacement in terms of total flavonoids, phenolic acid, dopamine and FOS. In both Namwa varieties, sugar contents decreased after the drying process. Sugar contents of the dried products were 48.47 and 47.21 g/100 g. The drying process caused a reduction in total flavonoid contents and phenolic acid at 63–66% and 64–70%, respectively. No significant differences (p < 0.05) were found for total flavonoid and phenolic contents between the dried banana products made from the two Namwa varieties (178.21 vs. 182.53 mg/kg and 96.06 vs. 102.19 mg/kg, respectively). Products made from Nuanchan varieties (24.52 mg/kg) contained significantly higher dopamine than that from Mali Ong (38.52 mg/kg). The data also suggest that the banana maturity stage for production of the sun dried products was also optimum in terms of high nutraceutical level.

This review summarized the composition of volatile and nonvolatile compounds, the sensory mechanism and the application of Sichuan pepper (Zanthoxylum genus) as a spice and multifunctional food, such as antibacterial, inhibition of inflammation, and antioxidant among others. The aim is to provide a better understanding and potential future in-depth research and application of Sichuan pepper. Keywords: Sichuan pepper, Zanthoxylum, Volatile flavor compounds, Pungent taste, Alkyl amides

The function of small G protein signalling modulators (SGSM1/2/3) in cancer remains unknown. Our findings demonstrated that SGSM2 is a plasma membrane protein that strongly interacted with E-cadherin/β-catenin. SGSM2 downregulation enhanced the phosphorylation of focal adhesion kinase (FAK; Y576/577), decreased the expression of epithelial markers such as E-cadherin, β-catenin, and Paxillin, and increased the expression of Snail and Twist-1, which reduced cell adhesion and promoted cancer cell migration. Oestrogen and fibronectin treatment was found to promote the colocalization of SGSM2 at the leading edge with phospho-FAK (Y397). The BioGRID database showed that SGSM2 potentially interacts with cytoskeleton remodelling and cell-cell junction proteins. These evidences suggest that SGSM2 plays a role in modulating cell adhesion and cytoskeleton dynamics during cancer migration.

Acute myeloid leukemia (AML) is characterized by the dysregulation of hematopoietic cell proliferation, resulting in the accumulation of immature myeloid cells in bone marrow. 5-Demethylnobiletin (5-demethyl NOB), a citrus 5-hydroxylated polymethoxyflavone, has been reported to exhibit various bioactivities, such as antioxidant, anti-inflammatory and anticancer properties. In this study, we investigated the antileukemic effects of 5-demethyl NOB and its underlying molecular mechanisms in human AML cells. We found that 5-demethyl NOB (20–80 μM) significantly reduced human leukemia cell viability, and the following trend of effectiveness was observed: THP-1 ≈ U-937 > HEL > HL-60 > K562 cells. 5-Demethyl NOB (20 and 40 μM) modulated the cell cycle through the regulation of p21, cyclin E1 and cyclin A1 expression and induced S phase arrest. 5-Demethyl NOB also promoted leukemia cell apoptosis and differentiation. Microarray-based transcriptome, Gene Ontology (GO) and Gene Set Enrichment Analysis (GSEA) of differentially expressed genes (DEGs) analysis showed that the expression of inhibitor of differentiation/DNA binding 1 (ID1), a gene associated with the GO biological process (BP) cell population proliferation (GO: 0008283), was most strongly suppressed by 5-demethyl NOB (40 μM) in THP-1 cells. We further demonstrated that 5-demethyl NOB-induced ID1 reduction was associated with the inhibition of leukemia cell growth. Moreover, DEGs involved in the hallmark gene set NF-κB/TNF-α signaling pathway were markedly enriched and downregulated by 5-demethyl NOB. Finally, we demonstrated that 5-demethyl NOB (20 and 40 μM), combined with cytarabine, synergistically reduced THP-1 and U-937 cell viability. Our current findings support that 5-demethyl NOB dramatically suppresses leukemia cell proliferation and may serve as a potential phytochemical for human AML chemotherapy.