Activation of NRF2 by epiberberine improves oxidative stress and insulin resistance in T2DM mice and IR-HepG2 cells in an AMPK dependent manner.

ETHNOPHARMACOLOGICAL RELEVANCE: Phytochemical compounds offer a distinctive edge in diabetes management, attributed to their multifaceted target mechanisms and minimal toxicological profiles. Epiberberine (EPI), an alkaloid derived from plants of the Rhizoma Coptidis, has been reported to have antidiabetic effects. However, the underlying molecular mechanism of EPI are not fully elucidated. AIM OF THE STUDY: This study explored the anti-diabetic effects of EPI and the role of the NRF2/AMPK signaling pathway in improving insulin resistance. MATERIALS AND METHODS: We utilized two distinct models: in vivo, we employed mice with type 2 diabetes mellitus (T2DM) induced by high-fat diet (HFD) and streptozotocin (STZ) to conduct a range of assessments including measuring physical parameters, conducting biochemical analyses, examining histopathology, and performing Western blot tests. In parallel, in vitro experiments were carried out using insulin resistance (IR)-HepG2 cells, through which we conducted a CCK8 assay, glucose uptake tests, Western blot analyses, and flow cytometry studies. RESULTS: In the EPI-treated group of T2DM mice, there was a significant reduction in hyperglycemia, IR, and hyperlipidemia, accompanied by beneficial changes in the liver and pancreas, as well as enhanced glucose uptake in IR-HepG2 cells. Herein, our finding also provided evidence that EPI could increase the expression of GLUT4 and activated the IRS-1/PI3K/AKT insulin signaling pathway to improve IR in vitro and in vivo. Moreover, EPI alleviated oxidative stress by enhancing SOD and GPX-px activity, decreasing reactive oxygen species (ROS) and malondialdehyde (MDA) content, and promoting nuclear factor (erythroid-derived 2)-like 2 (NRF2), total NRF2, NAD(P)H-quinone oxidoreductase (NQO1) and heme oxygenase-1 (HO-1) expression in the liver tissue of T2DM mice and IR-HepG2 cells. Furthermore, EPI decreased oxidative stress and improved IR, but these benefits were nullified by siNRF2 transfection. In particular, AMP-activated protein kinase (AMPK) deficiency by short-hairpin RNA (shRNA) partially reversed the effects of EPI on nuclear transcription, oxidative stress, and IR of NRF2 in IR-HepG2 cells. CONCLUSIONS: Taken together, EPI activated NRF2-dependent AMPK cascade to protect T2DM from oxidative stress, thereby alleviating IR.

A new C19-diterpenoid alkaloid in Aconitum georgei Comber.

Nine diterpenoid alkaloids were isolated from Aconitum georgei Comber belonging to the genus Aconitum in Ranunculaceae family. Their structures were determinated by using HR-ESI-MS and 1 D/2D NMR spectra as geordine (1), yunaconitine (2), chasmanine (3), crassicauline A (4), forestine (5), pseudaconine (6), 14-acetylalatisamine (7), austroconitine B (8), and talatisamine (9). Among them, compound 1 is a previously undescribed aconitine-type C19-diterpenoid alkaloid, and compounds 3, and 5-9 have not previously been isolated from this species. The results of in vitro experiments indicated that new compound 1 possesses mild anti-inflammatory activity, which inhibited the production of NO in LPS-activated RAW 264.7 cells with an inhibition ratio of 29.75% at 50 µM.

Multi-target meridians classification based on the topological structure of anti-cancer phytochemicals using deep learning.

ETHNOPHARMACOLOGICAL RELEVANCE: Traditional Chinese medicine (TCM) meridian is the key theoretical guidance of prescription against tumor in clinical practice. However, there is no scientific and systematic verification of therapeutic action of herbs under meridians context. Several studies have determined the Chinese herbal medicine (CHM) phytochemicals for intrinsic attribute or meridians classification based on artificial intelligence (AI) tools. However, it is challenging to represent the complex molecular structures with large heterogeneity through the current technologies. In addition, the multiple correspondence between herbs and meridians has not been paid much attention. AIM OF THE STUDY: We aim to develop an AI framework to classify multi-target meridians through the topological structure of phytochemicals. MATERIALS AND METHODS: A total of 354 anti-cancer herbs, their corresponding TCM meridians and 5471 ingredient compounds were collected from public databases of CancerHSP, ETCM, and Hit 2.0. The statistical analysis of herbal and compound datasets, clustering analysis of the associated cancers, and correlational analysis of meridian tropism were preliminary conducted. Then a deep learning (DL) hybrid model named GRMC consisting of graph convolutional network (GCN) and recurrent neural network (RNN) was employed to generate the meridian multi-label sequences based on molecular graph. RESULTS: The curing herbs against tumors have tight relationships to lung, liver, stomach, and spleen meridians. These herbs behave different properties in curing certain cancer. Certain cancer types have co-occurrence such as ovarian, bladder and cervical cancer. Compounds have multitarget meridians with characteristics of higher-order correlations. Compared with the other state-of-the-art algorithms on the datasets and previous methods dealing with conventional fixed fingerprints of herbal compounds, the proposed GRMC has superior overall performance on testing dataset with the one error of 0.183, hamming loss of 0.112, mean averaged accuracy (MAA) of 0.855, mean averaged precision (MAP) of 0.891, mean averaged recall (MAR) of 0.812, and mean averaged F1 score (MAF) of 0.849. CONCLUSIONS: The proposed method can predict multi-targeted meridians through neural graph features in herbal compounds and outperforms several comparison methods. It could provide a basis for understanding the molecular scientific evidence of TCM meridians.

Improved eutrophication model with flow velocity-influence function and application for algal bloom control in a reservoir in East China.

Improving hydrodynamic conditions is considered an effective method for facilitating the eutrophication management. However, the effect of hydrodynamic conditions on algal growth has rarely been quantified. In this work, a eutrophication model was developed and flow velocity was introduced into the algae growth kinetic formula to simulate the dynamics of algae growth in a drinking water source reservoir in East China. Based on the previous research and model calibration, the flow velocity-influence function f(v) and its parameters were determined. Accordingly, the optimal flow velocity for the dominant algae growth and critical flow velocity for algal growth inhibition were presented to be 0.055 m/s and 0.200 m/s for the study reservoir. Modeled results considering f(v) agreed with better with observations and reproduced the algal overgrowth process more accurately. The spatial-temporal differences in chlorophyll a (Chl a) concentration distribution during the algal proliferation period were analyzed on the basis of simulation results, which corroborated the significant influence of flow velocity on algal growth. The established model was applied to investigate the effect of improvement in hydrodynamic conditions on algal bloom control in the reservoir, and the scenario simulation of the additional sluice was conducted. Results showed that the additional sluice operation inhibited algal overgrowth effectively, resulting in an average decrease of 24.8%, 3.3%, 43.0%, and 37.5% in modeled Chl a concentration upstream north, upstream south, midstream and downstream, respectively. The established model might serve as a practical tool for eutrophication management in the study reservoir and other water bodies with similar hydrological characteristics and geographical features.

[Cost-effectiveness analysis of Chaiyin Granules in treatment of influenza].

This study aimed to evaluate the cost-effectiveness of Chaiyin Granules compared with Oseltamivir Phosphate Capsules in the treatment of influenza(exogenous wind-heat syndrome). Based on a randomized, double-blind, positive drug parallel control clinical trial, this study evaluated the pharmacoeconomics of Chaiyin Granules with cost-effectiveness analysis method. A total of 116 patients with influenza from eight hospitals(grade Ⅱ level A above) in 6 cities were selected in this study, including 78 cases in the experimental group with Chaiyin Granules and Oseltamivir Phosphate Capsules placebo, and 38 cases in the control group with Oseltamivir Phosphate Capsules and Chaiyin Granules placebo. The total cost of this study included direct medical cost, direct non-medical cost, and indirect cost. The remission time of clinical symptoms, cure time/cure rate, antipyretic onset time/complete antipyretic time, viral nucleic acid negative rate, and traditional Chinese medicine(TCM) syndrome curative effect were selected as the effect indicators for cost-effectiveness analysis. Four-quadrant diagram was used to estimate the incremental cost-effectiveness ratio. The results showed that Chaiyin Granules were not inferior to Oseltamivir Phosphate Capsules in the remission time of clinical symptoms of influenza(3.1 d vs 2.9 d, P=0.360, non-inferiority margin was 0.5 d). Compared with Oseltamivir Phosphate Capsules, Chaiyin Granules would delay the remission time of clinic symptoms of influenza for 1 d, but could save 213.9 yuan. 1 d delay in cure time could save 149.3 yuan; 1% reduction in the cure rate could save 8.2 yuan; 1 d delay in antipyretic onset time could save 295.4 yuan; 1 d delay in complete antipyretic time could save 114.3 yuan; 1% reduction in the 5-day cure rate of TCM syndrome could save 19.2 yuan. Different from other indicators, there was no statistically significant difference between two groups in the effect of negative conversion rate of viral nucleic acid, but the cost was lower and the effect was superior, and the pharmacoeconomics was not different from that of Oseltamivir Phosphate Capsules in the field of influenza treatment.

Comparison of RETREAT and CCFSS Scoring Systems for Risk Estimation of Hepatocellular Carcinoma Recurrence After Radical Resection.

Objective: RETREAT and CCFSS are two scoring systems specifically designed to predict postoperative recurrence in hepatocellular carcinoma (HCC). RETREAT and CCFSS are scoring systems designed to predict postoperative recurrence in hepatocellular carcinoma (HCC). This study aims to evaluate and compare the prognostic performance of two scoring systems, RETREAT and CCFSS, for predicting tumor recurrence after radical resection in patients with hepatocellular carcinoma (HCC). Methods: In this retrospective study, we analyzed the clinical data of 124 patients with HCC who underwent radical resection at our hospital between March 2017 and February 2020. The patients were categorized into a recurrence group (n = 41) and a non-recurrence group (n = 83) based on whether they experienced recurrence within 3 years of follow-up. Logistic regression analysis was conducted to compare the clinical characteristics between the two groups and identify factors associated with HCC recurrence. Additionally, we generated receiver operating characteristic (ROC) curves to evaluate the predictive value of the RETREAT and CCFSS scoring systems for predicting HCC recurrence after surgery. Results: Significant differences (P < .05) were found in the postoperative relapse-free survival time, HBsAg positivity, preoperative ALT≥ 40 U/L, preoperative Alb < 40 g/L, pericardial invasion, RETREAT score, and CCFSS score between the two groups. A multi-factor logistic regression analysis was performed between postoperative relapse in HCC patients and HBsAg positivity, preoperative ALT ≥ 40U/L, preoperative Alb<40g/L, pericardial invasion, RETREAT score, and CCFSS score grading as independent variables. The analysis revealed that HBsAg positivity (OR = 6.039, 95%CI: 2.994~12.182), preoperative ALT ≥ 40 U/L (OR = 3.738, 95%CI: 2.016-6.931), preoperative Alb< 40g/L (OR = 3.655, 95%CI: 2.083-6.415), envelope invasion (OR = 3.119, 95%CI: 1.922-5.061), RETREAT score (OR = 6.867, 95%CI: 3.204-14.719), and CCFSS score (OR = 3.228, 95%CI: 1.951-5.342) were significant factors influencing postoperative recurrence in HCC patients (P < .05). The RETREAT score had an area under the curve (AUC) of 0.853, with a sensitivity of 89.23% and a specificity of 93.87% (95%CI: 0.7567-0.950), while the AUC of the CCFSS score for predicting postoperative recurrence in HCC patients was 0.741, with a sensitivity of 78.57% and a specificity of 60.71% (95%CI: 0.609-0.873). Among the factors analyzed, including postoperative relapse-free survival time, HBsAg positivity, preoperative ALT≥ 40 U/L, preoperative Alb < 40 g/L, pericardial invasion, RETREAT score, and CCFSS score, statistically significant differences were observed between the recurrence and non-recurrence groups (P < .05). Conclusion: The RETREAT score demonstrates higher efficacy compared to the CCFSS score in predicting postoperative recurrence in hepatocellular carcinoma (HCC) patients and can serve as a valuable tool for the prognostic evaluation of HCC patients who undergo radical resection. The RETREAT score's superiority can be attributed to its higher area under the curve (AUC) and improved sensitivity and specificity, which allow for better discrimination between positive and negative cases. This enhanced accuracy enables clinicians to make more informed decisions towards post-surgical management and treatment strategies, ultimately improving patient outcomes. Thus, the RETREAT score serves as a vital tool for personalized and targeted care towards HCC patients undergoing radical resection.

Advances in the Application of Traditional Chinese Medicine Using Artificial Intelligence: A Review.

Traditional Chinese medicine (TCM), as one of the crystallizations of Chinese wisdom, emphasizes the balance of Yin and Yang to keep the body healthy. Under the theoretical guidance of a holistic view, the diagnostic process in TCM has characteristics of subjectivity, fuzziness, and complexity. Therefore, realizing standardization and achieving objective quantitative analysis are the bottlenecks of the development of TCM. The emergence of artificial intelligence (AI) technology has brought unprecedented challenges and opportunities to traditional medicine, which is expected to provide objective measurements and improve the clinical efficacy. However, the combination of TCM and AI is still in its infancy and currently faces many challenges. Therefore, this review provides a comprehensive discussion of the existing advances, problems, and prospects of the applications of AI technologies in TCM with the hope of promoting a better understanding of the TCM modernization and intellectualization.

Vitexin ameliorated diabetic nephropathy via suppressing GPX4-mediated ferroptosis.

Diabetic nephropathy (DN) is common complication of diabetes. Ferroptosis is an atypical form of iron-dependent modulated necrosis and have been proven to contribute to the progress of diabetic nephropathy. Vitexin, a flavonoid monomer derived from medicinal plants that has various biological activities including anti-inflammatory and anticancer effects, has not been investigated in diabetic nephropathy studies. However, whether vitexin has a protective effect on diabetic nephropathy remains unclear. In this study, the roles and mechanism of vitexin on alleviating DN were explored in vivo and in vitro. The protective effect of vitexin in diabetic nephropathy were evaluated by in vitro and in vivo experiment. In this research, we validated that vitexin protect HK-2 against HG-induced damage. Besides, vitexin pretreatment also reduced fibrosis (Collagen type I Col I, TGF-ß1). Furthermore, vitexin inhibited ferroptosis induced by HG, accompanied by changes of morphological, decrease of ROS, Fe2+ and MDA, and increased GSH levels. Meanwhile, vitexin up-regulated the protein expression of GPX4 and SLC7A11 in HG-induced HK-2 cells. Moreover, knockdown of GPX4 by shRNA migrated the protective effect of vitexin on HG-challenged HK-2 and reversed the ferroptosis induced by vitexin. Consistent with in vitro, vitexin alleviated renal fibrosis, damage and ferroptosis in DN rat. In conclusion, our findings revealed that vitexin could alleviate diabetic nephropathy by attenuated ferroptosis via activating GPX4.

A comprehensive review of polyphenol oxidase in tea (Camellia sinensis): Physiological characteristics, oxidation manufacturing, and biosynthesis of functional constituents.

Polyphenol oxidase (PPO) is a metalloenzyme with a type III copper core that is abundant in nature. As one of the most essential enzymes in the tea plant (Camellia sinensis), the further regulation of PPO is critical for enhancing defensive responses, cultivating high-quality germplasm resources of tea plants, and producing tea products that are both functional and sensory qualities. Due to their physiological and pharmacological values, the constituents from the oxidative polymerization of PPO in tea manufacturing may serve as functional foods to prevent and treat chronic non-communicable diseases. However, current knowledge of the utilization of PPO in the tea industry is only available from scattered sources, and a more comprehensive study is required to reveal the relationship between PPO and tea obviously. A more comprehensive review of the role of PPO in tea was reported for the first time, as its classification, catalytic mechanism, and utilization in modulating tea flavors, compositions, and nutrition, along with the relationships between PPO-mediated enzymatic reactions and the formation of functional constituents in tea, and the techniques for the modification and application of PPO based on modern enzymology and synthetic biology are summarized and suggested in this article.

Dietary intake of household cadmium-contaminated rice caused genome-wide DNA methylation changes on gene/hubs related to metabolic disorders and cancers.

Cadmium (Cd) contamination in food has raised broad concerns in food safety and human health. The toxicity of Cd to animals/humans have been widely reported, yet little is known about the health risk of dietary Cd intake at the epigenetic level. Here, we investigated the effect of a household Cd-contaminated rice (Cd-rice) on genome-wide DNA methylation (DNAm) changes in the model mouse. Feeding Cd-rice increased kidney Cd and urinary Cd concentrations compared with the Control rice (low-Cd rice), whereas supplementation of ethylenediamine tetraacetic acid iron sodium salt (NaFeEDTA) in the diet significantly increased urinary Cd and consequently decreased kidney Cd concentrations. Genome-wide DNAm sequencing revealed that dietary Cd-rice exposure caused the differentially methylated sites (DMSs), which were mainly located in the promoter (32.5%), downstream (32.5%), and intron (26.1%) regions of genes. Notably, Cd-rice exposure induced hypermethylation at the promoter sites of genes Caspase-8 and interleukin-1ß (Il-1ß), and consequently, their expressions were down-regulated. The two genes are critical in apoptosis and inflammation, respectively. In contrast, Cd-rice induced hypomethylation of the gene midline 1 (Mid1), which is vital to neurodevelopment. Furthermore, 'pathways in cancer' was significantly enriched as the leading canonical pathway. Supplementation of NaFeEDTA partly alleviated the toxic symptoms and DNAm alternations induced by Cd-rice exposure. These results highlight the broad effects of elevated dietary Cd intake on the level of DNAm, providing epigenetic evidence on the specific endpoints of health risks induced by Cd-rice exposure.

[Data mining in traditional Chinese medicine product quality review].

The traditional Chinese medicine(TCM) enterprises have accumulated a large amount of product quality review(PQR) data. Mining these data can reveal the hidden knowledge in production and helps improve pharmaceutical manufacturing technology. However, there are few studies involving the mining of PQR data and thus enterprises lack the guidance to analyze the data. This study proposed a method to mine the PQR data, which consisted of 4 functional modules: data collection and preprocessing, risk classification of variables, risk evaluation by batches, and the regression analysis of quality. Further, we carried out a case study of the formulation process of a TCM product to illustrate the method. In the case study, the data of 398 batches of products during 2019-2021 were collected, which contained 65 process variables. The risks of variables were classified according to the process performance index. The risk of each batch was analyzed through short-term and long-term evaluation, and the critical variables with the strongest impact on the product quality were identified by partial least square regression. The results showed that 1 variable and 13 batches were of high risk, and the critical process variable was the quality of the intermediates. The proposed method enables enterprises to comprehensively mine the PQR data and helps to enhance the process understanding and improve the quality control.

Dietary protocatechuic acid ameliorates ileal mucosal barrier injury and inflammatory response and improves intestinal microbiota composition in Yellow chickens challenged with Salmonella typhimurium.

Salmonella typhimurium (ST) is a common foodborne pathogen that severely affects the health of humans and livestock. Protocatechuic acid (PCA) has been shown to possess anti-inflammatory and anti-bacterial functions. Chickens were used to investigate the effect of PCA on the gut health infected with ST. A total of one hundred eighty, 1-d-old birds were randomly allocated into 3 treatments, each with 6 replicates per treatment and 10 chicks per replicate. Broiler chicks in the control and ST treatment were fed a basal diet, and birds in the PCA+ST treatment received the basal diet with 600 mg/kg PCA. On d 14 and 16 of the trial, broilers in ST and PCA+ST treatments received an oral dose of ST, while broilers in CON received an equal amount of PBS. The data were analyzed by the one-way ANOVA. Dietary PCA increased (P < 0.05) final body weight, average daily gain, and feed to gain ratio in ST-challenged Yellow broilers. Protocatechuic acid significantly alleviated ST-induced intestinal mucosal injury reflected in the decreased (P < 0.05) plasma activity of diamine oxidase and ileal apoptosis, with increased (P < 0.05) ileal villus height and villus height/crypt depth. Protocatechuic acid treatment significantly decreased (P < 0.05) ST-induced proinflammatory cytokine (Interleukin-1ß, Interleukin-6, Tumor necrosis factor-α, and Interferon-ß) content in ileum. Meanwhile, PCA treatment significantly increased (P < 0.05) the transcript abundances of claudin 1 (CLDN1), zonula occludens-1 (ZO-1), and mucin 2 (MUC2) in ileum, all related to the intestinal barrier in ST-challenged Yellow broilers. Additionally, PCA also increased (P < 0.05) the diversity and richness of the cecal microflora as reflected by reduced (P < 0.05) abundance of Bacteroidota, Proteobacteria and Escherichia-Shigella, and increased (P < 0.05) abundance of Firmicutes and Lactobacillus in ST-challenged Yellow broilers. These findings indicate that PCA relieves ST-induced loss weight, intestinal barrier injury, inflammatory response, and improves intestinal microbiota composition in Yellow broilers.

Feeding Aquilaria sinensis Leaves Modulates Lipid Metabolism and Improves the Meat Quality of Goats.

Aquilaria (A.) sinensis is a medicinal plant widely grown in tropical South China. Given the abundant pruning waste of its leaves, the use of A. sinensis leaves is valuable. In this study, goats were fed a diet containing 20% A. sinensis leaves. Compared with the basal diet, feeding A. sinensis leaves to goats did not affect growth performance but considerably reduced the feeding cost. Strikingly, feeding A. sinensis leaves resulted in a significant decrease in the blood cholesterol levels (2.11 vs. 1.49 mmol/L, p = 0.01) along with a significant increase in the high-density lipoprotein levels (1.42 vs. 1.82 mmol/L, p = 0.01). There was also a tendency to lower the content of low-density lipoprotein levels in goats (0.78 vs. 0.45 mmol/L, p = 0.09). Furthermore, metabolomics analysis demonstrated that the reduction in cholesterol levels occurred in both the serum (0.387-fold change) and muscle (0.382-fold change) of goats during A. sinensis leaf feeding. The metabolic responses to feeding A. sinensis leaves suggest that the activation of lipolysis metabolism might happen in goats. These observed changes would be conducive to improving animal health and meat quality, ultimately benefiting human health.

Targeted photothermal release of antibiotics by a graphene nanoribbon-based supramolecular glycomaterial.

Here, we report the simple construction of a supramolecular glycomaterial for the targeted delivery of antibiotics to P. aeruginosa in a photothermally-controlled manner. A galactose-pyrene conjugate (Gal-pyr) was developed to self-assemble with graphene nanoribbon-based nanowires via π-π stacking to produce a supramolecular glycomaterial, which exhibits a 1250-fold enhanced binding avidity toward a galactose-selective lectin when compared to Gal-pyr. The as-prepared glycomaterial when loaded with an antibiotic that acts as an inhibitor of the bacterial folic acid biosynthetic pathway eradicated P. aeruginosa-derived biofilms under near-infrared light irradiation due to the strong photothermal effect of the nanowires accelerating antibiotic release.

Theaflavins in Black Tea Mitigate Aging-Associated Cognitive Dysfunction via the Microbiota-Gut-Brain Axis.

Aging-associated cognitive dysfunction has a great influence on the lifespan and healthspan of the elderly. Theaflavins (TFs), a mixture of ingredients formed from enzymatic oxidation of catechins during the manufacture of tea, have a positive contribution to the qualities and antiaging activities of black tea. However, the role of TFs in mitigating aging-induced cognitive dysfunction and the underlying mechanism remains largely unknown. Here, we find that TFs effectively improve behavioral impairment via the microbiota-gut-brain axis: TFs maintain gut homeostasis by improving antioxidant ability, strengthening the immune response, increasing the expression of tight junction proteins, restructuring the gut microbiota, and altering core microbiota metabolites, i.e., short-chain fatty acids and essential amino acids (SCFAs and AAs), and upregulating brain neurotrophic factors. Removing the gut microbiota with antibiotics partly abolishes the neuroprotective effects of TFs. Besides, correlation analysis indicates that the decrease in gut microbiota, such as Bacteroidetes and Lachnospiraceae, and the increase in microbiota metabolites' levels are positively correlated with behavioral improvements. Taken together, our findings reveal a potential role of TFs in mitigating aging-driven cognitive dysfunction via the microbiota-gut-brain axis. The intake of TFs can be translated into a novel dietary intervention approach against aging-induced cognitive decline.

Macrostines A and B: Tetracyclic fisicoccane from the fungus Periconia macrospinosa WTG-10.

Two previous unreported fusicoccane diterpenoids macrostines A and B, together with seven known compounds were isolated from an extract of the fungus Periconia macrospinosa WTG-10. Their structures were elucidated by detailed analysis of spectroscopic data, NMR calculations with DP4+, and their absolute configurations were further determined by quantum chemical calculations of ECD spectra or X-crystallography. Macrostines A and B showed no cytotoxicity, antimicrobial activity and inhibitory effect on nitric oxide production in LPS-activated RAW264.7 macrophages. Compound 9 showed moderate activity against Bacillus subtilis.

Dietary supplementation with anthocyanin attenuates lipopolysaccharide-induced intestinal damage through antioxidant effects in yellow-feathered broiler chicks.

This study investigated the protective effects of anthocyanin (AC) supplementation on lipopolysaccharide (LPS)-challenged yellow-feathered broiler chicks. A total of 480 1-d female broiler chicks were randomly assigned to 4 treatment groups: basal diet (CON), basal diet + LPS-challenge (LPS), supplementation with 100 or 400 mg/kg AC + LPS-challenge (AC100, AC400). On d 17 and d 19, birds in LPS, AC100 and AC400 received an intramuscular dose of LPS, while birds in CON received saline. The result showed that (1) LPS injection significantly decreased (P < 0.05) body weight on d 21 and average daily gain of broiler chicks from 1 to 21 days of age, and supplementation with 100 mg/kg AC increased (P < 0.05) those of LPS-challenged broilers. (2) There were no differences among the treatments (P > 0.05) in relative weights of immune organs. (3) Supplementation with AC (AC100 and AC400) increased (P < 0.05) the jejunal villus height and villus height/crypt depth ratio (AC100) of LPS-challenged birds. Challenge with LPS decreased the relative expression of OCLN (Occludin), ZO-1, JAM2, and MUC2 in jejunal mucosa of broilers, and supplementation with AC offset the relative expression of ZO-1, JAM2 (AC100 and AC400), and OCLN (AC400) in LPS-injected broilers. (4) LPS-induced increase in the malondialdehyde (MDA) concentration and decreases in activity of total superoxide dismutase (T-SOD), and expression of SOD1, CAT and GPX in jejunal mucosa, were attenuated by dietary AC supplementation. In conclusion, in yellow-feathered broiler chicks, dietary supplementation with AC alleviated LPS-induced declined growth performance and mucosal damage of the intestine through antioxidant effects.

Research progress on the lipid-lowering and weight loss effects of tea and the mechanism of its functional components.

Obesity caused by poor eating habits has become a great challenge faced by public health organizations worldwide. Optimizing dietary intake and ingesting special foods containing biologically active substances (such as polyphenols, alkaloids, and terpenes) is a safe and effective dietary intervention to prevent the occurrence and development of obesity. Tea contains several active dietary factors, and daily tea consumption has been shown to have various health benefits, especially in regulating human metabolic diseases. Here, we reviewed recent advances in research on tea and its functional components in improving obesity-related metabolic dysfunction, and gut microbiota homeostasis and related clinical research. Furthermore, the potential mechanisms by which the functional components of tea could promote lipid-lowering and weight-loss effects by regulating fat synthesis/metabolism, glucose metabolism, gut microbial homeostasis, and liver function were summarized. The research results showing a "positive effect" or "no effect" objectively evaluates the lipid-lowering and weight-loss effects of the functional components of tea. This review provides a new scientific basis for further research on the functional ingredients of tea for lipid lowering and weight loss and the development of lipid-lowering and weight-loss functional foods and beverages derived from tea.

Screening and characterization estrogen receptor ligands from Arnebia euchroma (Royle) Johnst. via affinity ultrafiltration LC-MS and molecular docking.

Arnebiae Radix (dried root of Arnebia euchroma (Royle) Johnst.) is a traditional Chinese medicine (TCM) used to treat macular eruptions, measles, sore throat, carbuncles, burns, skin ulcers, and inflammations. The Arnebiae Radix extract can exert anti-breast cancer effects through various mechanisms of action. This study aimed to rapidly screen potential estrogen receptor (estrogen receptor α and estrogen receptor ß) ligands from the Arnebiae Radix extract. In this study, an analytical method based on affinity ultrafiltration coupled with UHPLC-Q-Exactive Orbitrap mass spectrometry was established for rapidly screening and identifying estrogen receptor ligands. Then, bindings of the components to the active site of estrogen receptor (estrogen receptor α and estrogen receptor ß) were investigated via molecular docking. Moreover, surface plasmon resonance (SPR) experiments with six compounds were performed to verify the affinity. As a result, a total of 21 ligands were screened from Arnebiae Radix using affinity ultrafiltration. Among them, 14 and 10 compounds from Arnebiae Radix showed affinity with estrogen receptor α and estrogen receptor ß, respectively. All of those ligands could have a good affinity for the multiple amino acid residues of the estrogen receptor based on molecular docking. In addition, six compounds display the great affinity by SPR. The method established in the study could be used to rapidly screen estrogen receptor ligands in Traditional Chinese medicine. The results demonstrated that the affinity ultrafiltration-UHPLC-Q-Exactive Orbitrap mass spectrometry method not only aids in the interpretation of the potential bioactive components and possible mechanisms of action of Arnebiae Radix but also provides a further effective basis for the quality control of this valuable herb medicine.