Frontiers in Pharmacology
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2021
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IF 5.811
Lu Yulin,Huang Jingjing,Zhang Yao,Huang Zitong,Yan Weiming,Zhou Tianran,Wang Zhesheng,Liao Lu,Cao Hongying,Tan Bo
The etiology of diarrhea-predominant irritable bowel syndrome (IBS-D) is complicated and closely related to neurotransmission in the gastrointestinal (GI) tract. Developing new strategies for treating this disease is a major challenge for IBS-D research. Berberine hydrochloride (BBH), the derivative of berberine, is a herbal constituent used to treat IBS. Previous studies have shown that BBH has potential anti-inflammatory, antibacterial, analgesic, and antidiarrheal effects and a wide range of biological activities, especially in regulating the release of some neurotransmitters. A modified IBS-D rat model induced by chronic restraint stress was used in all experiments to study the effects of BBH on the GI tract. This study measured the abdominal withdrawal reflex (AWR) response to graded colorectal distention (CRD; 20, 40, 60, and 80 mmHg) and observed the fecal areas of stress-induced IBS-D model. Experiments were conducted using organ bath techniques, which were performed in vitro using strips of colonic longitudinal smooth muscle. Inhibitory and excitatory neurotransmitter agents were added to each organ bath to observe contractile responses on the strips and the treatment effect exerted by BBH. The IBS-D rat model was successfully induced by chronic restraint stress, which resulted in an increased defecation frequency and visceral hypersensitivity similar to that of humans. BBH could reduce 4-h fecal areas and AWR response to CRD in IBS-D. The stress-induced IBS-D model showed upregulated colonic mRNA expression levels of 5-hydroxytryptamine-3A receptor and downregulated expression levels of neuronal nitric oxide synthase. Meanwhile, BBH could reverse this outcome. The responses of substances that regulate the contraction induced by related neurotransmission in the longitudinal smooth muscle of IBS-D colon (including the agonist of acetylcholine, carbachol; NOS inhibitor, L-NAME; and P2Y1 receptor antagonist, MRS2500) can be inhibited by BBH. In summary, BBH promotes defecation frequency and visceral hypersensitivity in IBS-D and exerts inhibitory effects on contractile responses in colonic longitudinal smooth muscle. Thus, BBH may represent a new therapeutic approach for treating IBS-D.
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PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY
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2013
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IF 3.552
Siyuan Sun,Kai Wang,Hongmei Lei,Liping Li,Meijuan Tu,Su Zeng,Hui Zhou,Huidi Jiang
Organic cation transporter 2 (OCT2) and 3 (OCT3) are low-affinity, high-capacity transporters (uptake-2) expressed in the central nervous system (CNS) and other major organs. Proven to be essential components in the CNS functions , OCT2 and OCT3 are suggested as potential targets of antidepressant therapeutics recently. Berberine , an active constituent derived from many medicinal plants , such as Coptis chinensis , has been reported to possess antidepressant-like action in the tail suspension test and forced swim test with elevated serotonin/norepinephrine/dopamine (5-HT/NE/DA) level in mouse brain ; however the mechanism has not been elucidated. In consideration of the relation between OCT2/3 and antidepressant action, and the characteristic of berberine as an organic cation, we investigated the potential involvement of OCT2 and OCT3 in the antidepressant-like action of berberine in the present study. The results in mouse brain synaptosomes demonstrated that uptake-2 inhibition might play a notable role in enhanced serotonergic and noradrenergic effects induced by berberine. The inhibitory study in transfected MDCK cells displayed that berberine is a potent inhibitor of human OCT2 and OCT3, and its IC 50 values for inhibition of transporter-mediated 5-HT/NE uptake are between 0.1 and 1 μM. In addition, berberine was identified as a substrate of hOCT2 and hOCT3. In conclusion, berberine is a substrate and an inhibitor of hOCT2 and hOCT3, and its inhibition on OCT2- and OCT3-mediated 5-HT and NE uptake may contribute to the enhanced monoamine neurotransmission in mouse brain. It was deduced that the inhibition of OCT2 and OCT3 probably be implicated in the mechanism of antidepressant-like action.
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Frontiers in Nutrition
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2025
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IF 5.1
Min Du,Xinran Liu,Xu Ji,Yue Wang,Xiaodan Liu,Chunfang Zhao,Erhui Jin,Youfang Gu,Hongyu Wang,Feng Zhang
Introduction: Enterotoxic Escherichia coli (ETEC) is the main pathogen that causes diarrhea, especially in young children. This disease can lead to substantial morbidity and mortality and is a major global health concern. Managing ETEC infections is challenging owing to the increasing prevalence of antibiotic resistance. Berberine, categorized as a substance with similarities in “medicine and food,” has been used in China for hundreds of years to treat gastrointestinal disorders and bacteria-induced diarrhea. This study investigated the preventive effect of dietary berberine on the intestinal mucosal barrier induced by ETEC and the microbial community within the intestines of weaned piglets.Methods: Twenty-four piglets were randomly divided into four groups. Piglets were administered either a standard diet or a standard diet supplemented with berberine at concentrations of 0.05 and 0.1%. and orally administered ETEC or saline.Results: Dietary supplementation with berberine reduced diamine oxidase, d-lactate, and endotoxin levels in piglets infected with ETEC (P < 0.05). Berberine increased jejunal villus height, villus/crypt ratio, mucosal thickness (P < 0.05), and goblet cell numbers in the villi and crypts (P < 0.05). Furthermore, berberine increased the optical density of mucin 2 and the mucin 2, P-glycoprotein, and CYP3A4 mRNA expression levels (P < 0.05). Berberine increased the expressions of zonula occludins-1 (ZO-1), zonula occludins-2 (ZO-2), Claudin-1, Occludin, and E-cadherin in the ileum (P < 0.05). Moreover, berberine increased the expression of BCL2, reduced intestinal epithelial cell apoptosis (P < 0.05) and decreased the expression of BAX and BAK in the duodenum and jejunum, as well as that of CASP3 and CASP9 in the duodenum and ileum (P < 0.05). Berberine decreased the expression of IL-1β, IL-6, IL-8, TNF-α, and IFN-γ (P < 0.05) and elevated total volatile fatty acids, acetic acid, propionic acid, valeric acid, and isovaleric acid concentrations (P < 0.05). Notably, berberine enhanced the abundance of beneficial bacteria including Enterococcus, Holdemanella, Weissella, Pediococcus, Muribaculum, Colidextribacter, Agathobacter, Roseburia, Clostridium, Fusicatenibacter, and Bifidobacterium. Simultaneously, the relative abundance of harmful and pathogenic bacteria, such as Prevotella, Paraprevotella, Corynebacterium, Catenisphaera, Streptococcus, Enterobacter, and Collinsella, decreased (P < 0.05).Discussion: Berberine alleviated ETEC-induced intestinal mucosal barrier damage in weaned piglets models. This is associated with enhancement of the physical, chemical, and immune barrier functions of piglets by enhancing intestinal microbiota homeostasis.
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TALANTA
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2024
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IF 5.6
Kai Hu,Zhiyu Zhang,Di Zhao,Lixin Li,Cheng Yang,Huahui Zeng,Shusheng Zhang,Zhenqiang Zhang
In this study, a novel berberine based anion-exchanged hypercrosslinked polymer (BBR-HCPs) was synthesized via Friedel-Crafts alkylation using dimethoxymethane as a cross-linking agent. The proposed BBR-HCPs polymer exhibited excellent adsorption capacities for aristolochic acids (AAs). Moreover, there are various interactions such as hydrophobic, π-π stacking, hydrogen bonding, and electrostatic interactions between BBR-HCPs and AAs. A solid phase microextraction (SPME) coating, prepared with BBR-HCPs as the sorbent and polyacrylonitrile (PAN) as the binder, was applied for the determination of AAs in herbal plants using a 24-well plate for high-throughput, with instrumental analysis carried out via high performance liquid chromatography with diode array detector (HPLC-DAD). The optimized and validated BBR-HCPs-SPME/HPLC-DAD method exhibited excellent linearity over range of 5–400 ng mL −1 with R 2 > 0.9974. Detection limits (S/N = 3) for AAs were found to be 0.03–0.150 ng mL −1 , with recoveries ranging from 82.6 to 117.8 % and relative standard deviations (RSDs) less than 10.49 %. This study underscores the potential of BBR-HCPs as a promising adsorbent for selective extraction and enrichment of AAs while introducing a reliable novel strategy for monitoring trace amounts of AAs in water and herbal plant samples.
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FOOD HYDROCOLLOIDS
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2024
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IF 11
Yuping Ning,Shuaimin Liu,Zihao Ren,Dongmei Yang,Jian Li,Lijuan Wang
Some chemicals used as preservatives may be found to be harmful to human health as a result of clinical studies conducted over time, or their limits may be updated. Natural, safe and antibacterial food packaging can simultaneously maintain the food quality , reduce preservative usage and prevent foodborne diseases . In this work, an edible, green and fluorescent packaging film with photodynamic inhibition of Staphylococcus aureus and Escherichia coli was prepared through incorporating the salt of berberine and citric acid (CA) into a composite film of carboxylated cellulose nanofibrils (CCNF) and κ-carrageenan (κC). The berberine/citric acid salt (BCA) was successfully synthesized via simple metathesis reaction, which endowed the blended film with improved thermal stability , ultraviolet shielding, water vapor barrier and mechanical properties. Among the prepared films, the film prepared from 0.6 g of CCNF and 8% of BCA (κC–CCNF–BCA8) showed the strongest fluorescence, the highest ROS production capacity and antimicrobial rate of 100% against both E. coli and S. aureus under white light. The total number of bacterial colonies in cooked chicken packaged in κC–CCNF–BCA8 film was 2.36 Log CFU/mL, which was lower than that packaged in κC-CCNF film (3.00 Log CFU/mL). The sustainable and fluorescent film could kill microorganisms in cooked chicken with only adequate sunlight and has a promising application in antibacterial packaging.
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TALANTA
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2012
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IF 3.794
Wenpeng Zhang,Zilin Chen
A novel berberine-imprinted polymer (MIP) monolith was prepared for extraction of berberine in aqueous medium. The MIP monolith was prepared inside a polypropylene micropipette tip by using dimethylsulfoxide as porogen , acrylamide (AA) as functional monomer and ethyleneglyol dimethacrylate (EGDMA) as cross-linker. Polymerization conditions were optimized and good permeability and selectivity was obtained when the ratio of berberine/AA/EGDMA was 1:5:30. Cross-reaction was also studied by three compounds (palmatine, coptisine , and jatrorrhizine) with similar structure. A molecularly imprinted micro solid-phase extraction (MI-μ-SPE) method was developed for selective extraction of berberine in aqueous solutions. Extraction parameters were investigated, such as sample pH value, sample flow rate , sample volume and elution solvent. By combining with HPLC/UV, MI-μ-SPE method showed a good linear range of 3–800 ng/mL with a low limit of detection limit of 1.0 ng/mL. The method was also applied for the pretreatment of berberbine in human plasma and urine samples. The result showed that proteins and other biological matrix were successfully eliminated and berberine was selectively enriched. Recoveries were tested in plasma and urine samples, and calculated to be 90.6–103.2% with relative standard deviations less than 4.7%.
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JOURNAL OF CHROMATOGRAPHY A
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2025
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IF 4
Hui Wang,Mingyu Wang,Jinku Zhang,Di Wu,Zhezhe Qi,Xinbei Dong,Xing Zhang,Hongyuan Yan,Yehong Han
A urea-melamine-hexamethylenetetramine resin (UMHR) was synthesized using water as the reaction medium, with hexamethylenetetramine serving as an environmentally friendly crosslinking agent in place of traditional formaldehyde. The resin was optimized as an efficient solid-phase extraction (SPE) adsorbent through optimization of synthetic parameters. A precise detection method for berberine hydrochloride in Pudilan antiphlogistic oral liquid was established by optimizing extraction parameters. The method exhibited excellent linearity, with a correlation coefficient ( r ≥ 0.9998) over a concentration range of 0.40–100.0 μg/mL. The limits of detection (LOD) and quantitation (LOQ) were 0.094 μg/mL and 0.314 μg/ mL, respectively. Recoveries ranged from 87.9 % to 97.3 %, with relative standard deviations (RSDs) below 3.2 %. This study presents a novel and environmentally friendly analytical approach for the quality control of traditional Chinese medicine preparations.
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ACS Sustainable Chemistry & Engineering
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2020
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IF 7.632
Yuwei Wu,Qiaojuan Zhang,Yiwen Zhao,Kangyuan Zhuang,Yiling Fan,Shuo Zhang,Xiaohan Zhang,Kunlun Huang,Zhiyi Yao
Developing a rapid and simple method for the detection of berberine chloride (BBC), one kind of natural antibiotic, is significant to ensure reasonable control and administration of antibiotic residues in food and other feed. In this report, a sensitive and selective fluorescent probe based on a water-soluble perylene diimide derivative (PDI-Asp) has been screened for the detection of berberine chloride (BBC). The sensing performance and mechanism of this probe were systematically investigated by using UV–vis and fluorescence spectroscopic techniques. Meanwhile, the influencing factors of probe structures on the sensing performance were also addressed. It was identified that the formation of supramolecular complex between BBC and PDI-Asp through synergy of electrostatic and π–π interactions promoted a rapid and fluorometric assay for BBC in 100% aqueous systems. The detection limit for BBC was found to be as low as 28 nmol/L. Finally, PDI-Asp was a highly promising fluorometric probe for the direct determination of BBC in practical samples. To the best of our knowledge, this is the first report of PDI-based probe for detecting small biomolecules in pure aqueous solution. We believe that this approach will not only extend the sensing scope of PDIs but also contribute to understanding the mechanism of the interaction between BBC and PDIs, and it will provide some useful information for the design of PDI-based probes for other small biomolecules.
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FEBS Open Bio
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2025
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IF 2.3
Wenheng Gao,Yunlong Li,Lihua Chen,Wenshuo Yang,Yong He,Ye Yang,Dengke Yin,Song Tan
Hyperlipidemia is a common chronic disease characterized by elevated levels of lipids in the blood. There is some evidence that suggests that berberine (BBR) might be beneficial for the treatment of hyperlipidemia. However, its low intestinal bioavailability limits its potential therapeutic action. In the present study, we explored the effect and the underlying mechanism of berberine–cinnamic acid co-crystal (BBR-CA), which is self-assembled from CA and BBR and displays a high intestinal bioavailability. In mice, BBR-CA showed the ability to decrease body weight gain and hepatic lipid accumulation in animals fed a high-fat diet. To further characterize the molecular basis of this effect, we established a hyperlipidemia cell model by treating human hepatocellular carcinoma cells (HepG2) with free fatty acids. Similarly to our in vivo experiments, lipid accumulation in free fatty acids-induced HepG2 cells was also reduced by BBR-CA. We hypothesized that BBR-CA might act through the regulation of sterol regulatory element-binding proteins-1 (SREBP-1), a key factor regulating lipid synthesis, and, indeed, SREBP-1 protein expression was inhibited by BBR-CA treatment, resulting in the decreased expression of its downstream proteins stearoyl-CoA desaturase 1 and acetyl-CoA carboxylase. Furthermore, the phosphorylation of phosphatidylinositol 3-kinase (PI3K), AKT and mammalian target of rapamycin (mTOR) was inhibited by BBR-CA, contributing to decreased active SREBP-1 in the nucleus, and was reversed and enhanced by the PI3K agonist recilisib and inhibitor LY294002, respectively. Taken together, our results suggest that BBR-CA could function by modulating the PI3K/AKT/mTOR signaling pathway, resulting in decreased nuclear expression of SREBP-1, as well as reduced expression of stearoyl-CoA desaturase 1 and acetyl-CoA carboxylase, thus alleviating hyperlipidemia. Further experimental validation is required to confirm these results.
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Current Medical Science
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2026
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IF 2
Liu Xiao-cui,Liu Ya-ge,Lv Yong-ning,Deng Bin
Objective This study aimed to investigate the protective effects of berberine (BBR) on pancreatic β-cells and explore its underlying molecular mechanisms via a proteomics-based approach. Methods Using db/db mice as a diabetes model, BBR was administered at doses of 100 mg/kg and 200 mg/kg for 8 weeks. The protective effects were assessed through fasting blood glucose (FBG), oral glucose tolerance test (OGTT), insulin tolerance test (ITT), pancreatic histopathological analysis, and TUNEL staining. Proteomic analysis employing the data-independent acquisition (DIA) method identified differentially expressed proteins (DEPs), whereas Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analyses were conducted to identify potential pathways. Molecular docking, surface plasmon resonance (SPR), and immunohistochemistry (IHC) were performed to validate key target proteins. Results BBR significantly reduced blood glucose levels, improved insulin resistance, enhanced insulin secretion, and reversed pathological changes in pancreatic tissue, thereby alleviating β-cell damage. Proteomic analysis identified 171 DEPs, implicating the AGE/RAGE signaling pathway as a key mechanism through which BBR exerts its protective effects. The results of molecular docking, SPR and IHC confirmed that BBR markedly inhibited the activation of the AGE/RAGE pathway. Conclusions These findings suggest that BBR alleviates pancreatic β-cell damage, potentially through regulation of the AGE/RAGE pathway, providing insights into its therapeutic potential for diabetes management.
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ACS Applied Bio Materials
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2026
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IF 5.6
Xinyue Wu,Jinrui Hou,Shiji Liu,Jiaxiao Liang,Shujuan Zhuo,Jinyan Du
The development of multifunctional wound dressings that concurrently eradicate bacterial infections and orchestrate tissue regeneration remains a critical challenge in clinical wound management. Herein, we report the fabrication of a BBH/Ag-MOF composite, synthesized by integrating berberine hydrochloride (BBH) into a silver-based metal-organic framework (Ag-MOF). This hybrid platform synergistically combines the potent antimicrobial efficacy of Ag+ with the broad-spectrum bioactivity of BBH. In vitro investigations demonstrate that BBH/Ag-MOF exerts robust inhibitory effects against both Gram-positive (Staphylococcus aureus (S. aureus) and Methicillin-resistant Staphylococcus aureus (MRSA)) and Gram-negative (Escherichia coli (E. coli) and Multidrug-resistant Escherichia coli (MDR E. coli)) bacteria, significantly prolonging the bacterial lag phase, reducing proliferation rates, and achieving a superior bactericidal efficiency at remarkably low concentrations. Mechanistically, BBH/Ag-MOF facilitates bacterial targeting through electrostatic attraction, disrupts membrane integrity via Ag+ release, and triggers intracellular respiratory chain inhibition through the delivered BBH molecules. Furthermore, the composite effectively scavenges reactive oxygen species (ROS) and suppresses biofilm maturation, thereby rebalancing the hostile wound microenvironment into a pro-healing state. In vivo assessments in an S. aureus-infected murine wound model reveal that BBH/Ag-MOF significantly accelerates wound closure, enhances organized collagen deposition, and stimulates angiogenesis. These therapeutic outcomes are accompanied by the downregulation of pro-inflammatory cytokines (TNF-α and IL-6), with no detectable cytotoxicity or systemic toxicity. Collectively, this study establishes BBH/Ag-MOF as a biocompatible, multifunctional therapeutic agent that synergistically bridges antibacterial, antioxidant, and regenerative functions, offering a highly effective strategy for the advanced management of infected chronic wounds.
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Frontiers in Pharmacology
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2022
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IF 5.988
Sa Yang,Shijie Cao,Congyu Li,Jichao Zhang,Chang Liu,Feng Qiu,Ning Kang
Non-alcoholic fatty liver disease (NAFLD) is a major public health problem in many countries. Berberine (BBR) is an effective therapeutic agent in alleviating NAFLD. Berberrubine (BRB) is one of the main active metabolites of BBR, which shows significant anti-obesity and antihypoglycemic effects. However, whether BRB is responsible for the in vivo therapeutic effect and the underlying mechanism of BRB on NAFLD have not been elucidated. In this study, the ability of BRB to ameliorate NAFLD, together with its molecular mechanism, was investigated. The results showed that BRB treatments could significantly improve hepatic steatosis and insulin resistance in high-fat diet (HFD)-fed mice and oleic acid (OA)-treated HepG2 cells. Meanwhile, BBR and BRB treatment similarly prevented lipid accumulation by regulating the protein expression of ATGL, GK, PPARα, CPT-1, ACC1, FAS, and CD36. In addition, compared with BBR, BRB could maintain glucose homeostasis via GLUT2, GSK3β, and G6Pase in HFD-fed mice. Furthermore, the components of the gut microbiota in mice were analyzed by 16S rRNA gene sequencing. BBR and BRB treatment could greatly modify the structure and composition of gut microbiota. At the genus level, BBR and BRB treatment decreased Lactobacillus and Romboutsia , while BBR increased beneficial bacteria, such as Akkermansia and Bacteroides , and BRB increased beneficial bacteria, such as Ileibacterium and Mucispirillum . Altogether, both BRB and BBR were active in alleviating NAFLD in vivo and BRB might be used as a functional material to treat NAFLD clinically.
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