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Berberine
SCIENCE OF THE TOTAL ENVIRONMENT · 2020 · IF 6.551

Synergetic suppression effects upon the combination of UV-C irradiation and berberine on Microcystis aeruginosa and Scenedesmus obliquus in reclaimed water: Effectiveness and mechanisms

Shang Li,Yi Tao,Guo-Hua Dao,Hong-Ying Hu

The risk of harmful algal blooms (HABs) in the water recharged with reclaimed water is a bottleneck for water reuse . The suppression effects and mechanisms of the combination of UV-C and berberine on Microcystis aeruginosa and Scenedesmus obliquus in reclaimed water were investigated. Mono UV-C irradiation at 75 mJ cm −2 could suppress the growth of M. aeruginosa for 7 d and that at 90 mJ cm −2 could suppress the growth of S. obliquus for 5 d. UV-C irradiation combined with 0.2–2 mg L −1 berberine lengthened the inhibition period of M. aeruginosa to 10- > 22 d and that of S. obliquus to 7- > 22 d and induced more rapid lethal effects on the harmful microalgal cells, in significant synergetic patterns. The combination of UV-C and berberine suppressed total, intracellular and extracellular microcystin-LR (MC-LR) more effectively and decreased the MC-LR quota significantly, which further reduced the risks of microcystin production and release. Furthermore, synergetic mechanisms of the combined treatments were systematically investigated from the aspects of photosynthetic system (photosynthetic activity and pigments), metabolic activity (ATP and membrane potential), oxidation stress (reactive oxygen species (ROS) and glutathione (GSH)), and apoptosis-like cell death (phosphatidylserine (PS) ectropion, caspase-3 activity and terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) positive rate). The combination treatment provided a joint attack of UV-C and berberine on photosynthetic transport chain of photosynthetic system II (PS II), and a synergetic pathway to achieve more severe disruptions in energy metabolism as well as aggravated oxidative stress . The accumulated ROS enhanced increases in programmed cell death (PCD) indicators of both microalgal species, which contributed to the enhancement effects on growth suppression. The results showed that the combination treatment achieved lower dose requirements of both UV-C irradiation and berberine for inducing the same inhibition effects on microalgal cells, which was promising to be applied in the HABs control of reclaimed water.

CAS / MDL: 64-18-6
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ENVIRONMENTAL POLLUTION · 2021 · IF 8.071

Berberine improves intestinal barrier function and reduces inflammation, immunosuppression, and oxidative stress by regulating the NF-κB/MAPK signaling pathway in deoxynivalenol-challenged piglets

Min Tang,Daixiu Yuan,Peng Liao

The aim of this study was to evaluate the effect of berberine (BBR) on the intestinal health of piglets exposed to deoxynivalenol (DON). A total of 180 weaned piglets were randomly allotted to 1 of 3 treatment groups with 10 replication pens per treatment and 6 piglets per pen. The treatments were basal diet, basal diet +4 mg/kg DON, and basal diet +4 mg/kg DON +40 mg/kg BBR. The experiment lasted for 21 d. BBR improved the growth performance of DON-challenged piglets. BBR could inhibit DON-induced intestinal injury by increasing the expression of serum antioxidant enzymes and T cell surface antigens and reducing the release of proinflammatory cytokines in the small intestine. BBR significantly increased the protein expression levels of zonula occludens 1 (ZO-1), Occludin and Claudin-1 in the ileal and jejunal mucosa and increased the morphological parameters of the jejunum. Moreover, we found that BBR significantly reduced the DON-induced gene and protein expression levels of ERK, JNK, and NF- κ B in the jejunum and ileum. In conclusion, BBR can regulate DON-induced intestinal injury, immunosuppression and oxidative stress by regulating the NF- κ B and MAPK signaling pathways and ultimately maintain the intestinal health of piglets.

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SEPARATION AND PURIFICATION TECHNOLOGY · 2018 · IF 3.927

Visible-light photocatalytic fuel cell with Z-scheme g-C3N4/Fe0/TiO2 anode and WO3 cathode efficiently degrades berberine chloride and stably generates electricity

Kané Rabé,Lifen Liu,Noor Ahmed Nahyoon,Yizhen Zhang,Ahmed Mahmoud Idris

A visible-light Z-scheme g-C 3 N 4 /Fe 0 /TiO 2 anodic catalyst was tested with cathodic WO 3 in photocatalytic Fuel Cell (PFC) that efficiently degrades berberine chloride and simultaneously generate electricity at pH 2,5,7 and 13. The Stainless-steel mesh electrodes loaded with prepared catalyst were irradiated by visible-light in single chamber PFC. The highest removal of berberine Chloride, cell voltage, and power density were 91%, 0.8 V, and 16.4 W/m 2 at a current density of 2.02 mA/cm 2 , respectively after 90 min irradiation in 0.05 M Na 2 SO 4 electrolyte, with 10 Ω external resistance. The impacts of pH and initial concentration of BEC on photocatalytic degradation and cell voltage were evaluated. The cell current density is enhanced while the photocatalyst activity increased. The constructed PFC maintained high-performance after 5 uses. Its use in degrading wide spectrum refractory pollutants and generate electricity is expected for the proved catalyst design, paired electrodes and high PFC performance for practical wastewater treatment.

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PHARMACOLOGICAL RESEARCH · 2025 · IF 10.5

Ginsenoside Rb1 and berberine synergistically protect against type 2 diabetes mellitus via GDF15/HAMP pathway throughout the liver lobules: Insights from spatial transcriptomics analysis

Rongfang Guo,Shuying Zhang,Anyao Li,Ping Zhang,Xin Peng,Xiaoyan Lu,Xiaohui Fan

Type 2 diabetes mellitus (T2DM) is a significant public health issue with high morbidity and mortality. Ginsenoside Rb1 (Rb1) and berberine (BBR), the main bioactive compounds of Panax ginseng and Coptis chinensis , respectively, are known for their hypoglycemic effects. Nevertheless, the synergistic effects and underlying mechanism of Rb1 and BBR on T2DM remain unclear. In this study, we utilized a leptin receptor-deficient (db/db) mouse model to investigate the protective effects of their combination treatment. Our findings demonstrated that the combined use of Rb1 and BBR at a 1:4 ratio had more pronounced effects than the first-line anti-diabetic drug metformin on reducing the weight ratio of white adipose tissue, ameliorating insulin resistance, and improving glucose and lipid metabolism. Using spatial transcriptomics, we revealed that metformin treatment improved gluconeogenesis and lipogenesis only in the periportal zone, while the combination treatment induced improvements throughout the liver lobule, with distinct key targets across different zones, thus underscoring a more comprehensive modulation of hepatic metabolism. This may be the key reason why this combination therapy demonstrated superior protective effects against T2DM. Additionally, the reversed expression of the key callback gene hepcidin (HAMP) and its regulator growth differentiation factor 15 (GDF15) following the combination therapy across all zones, along with validation experiments, further suggested that GDF15/HAMP pathway might be a key mechanism underlying the beneficial effects of Rb1 and BBR against T2DM. This study also indicates a path toward innovative drug cocktails for treating T2DM, offering a holistic approach to regulate the entire liver lobule metabolism.

CAS / MDL: 492-62-6
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MOLECULES · 2020 ·Vol. 25 ·期 8 ·1957 · IF 3.267

Development and In Vitro and In Vivo Evaluation of Microspheres Containing Sodium N-[8-(2-hydroxybenzoyl)amino]caprylate for the Oral Delivery of Berberine Hydrochloride

Ying Li,Chunyan Zhu

Microspheres containing absorption enhancer (sodiumN-[8-(2-hydroxybenzoyl)amino]caprylate, SNAC) were developed to enhance the oral bioavailability of berberine hydrochloride (BER) with poor intestinal membrane permeability. Microspheres were prepared and characterized by particle size measurements, scanning electron microscopy, differential scanning calorimetry, BER payload and release, Caco-2 cell monolayer transport, and rat pharmacokinetics. The microspheres were spherical and had uniform size, high encapsulation efficiency and high loading capacity. In vitro release studies showed that BER-loaded microspheres had good sustained release characteristics. The Caco-2 cell monolayer transport study proved that SNAC could significantly enhance permeability of BER 2–3-fold. Pharmacokinetic studies demonstrated a 9.87-fold increase in area under the curve (AUC) of BER mixed with SNAC and a 14.14-fold increase in AUC of microspheres compared with BER alone. These findings indicate that SNAC is a promising absorption enhancer for oral delivery of BER in the form of both solution and microspheres.Keywords:sodiumN-[8-(2-hydroxybenzoyl)amino]caprylate;permeation enhancement;berberine hydrochloride;microspheres;oral bioavailability

CAS / MDL: 9004-57-3
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

Carboxymethyl chitosan/PVA-based dynamic cross-linked dual network hydrogel loaded with berberine with self-healing, self-adaptive, sustainable release and antibacterial ability for dressing

Zhiyong Tan,Li Liu,Liting Hao,Jing Zhang,Yuhua Dai,Jianxiang Yu

Developing novel dressings with superior antibacterial properties to resist bacterial infections during wound healing remains a significant challenge. Hydrogels have emerged as prominent materials due to their excellent biocompatibility and adjustable functionality, and are widely applied in the field of wound therapy. However, the majority of hydrogels exhibit suboptimal mechanical properties, which hinder their practical application. In order to integrate dynamic function design and remarkable antibacterial activity, a dual-network (DN) hydrogel with multiple dynamic bonds was designed and constructed. Specifically, carboxymethyl chitosan (CMCS) and polyvinyl alcohol (PVA) were used as hydrogel matrix. Oxidized sodium alginate (OSA) and borax were utilized as crosslinking agents, resulting in the formation of Schiff base bonds and borate ester bonds with CMCS and PVA, respectively. Concurrently, berberine (BBR) was incorporated into the system to impart sustainable release properties and elevated antibacterial efficacy. The maximum antibacterial rates of the hydrogel against Escherichia coli (E. coli) and Staphylococcus aureus ( S. aureus ) reached 97.1 % and 99.9 %, respectively, exhibiting remarkable synergistic antibacterial activity. Furthermore, the dynamic crosslinked DN hydrogel endowed it with exceptional mechanical properties, malleability, adhesion, self-healing, and self-adaptive ability, rendering it more efficacious in actual wound sites. Moreover, the hydrogel also exhibited favorable blood and cell biocompatibility, characterized by a hemolysis rate of less than 1 % and cell viability exceeding 90 %. Overall, the multifunctional hydrogel demonstrates considerable potential in addressing the challenges associated with infectious wound healing, thus indicating its candidacy as a promising wound dressing.

CAS / MDL: 1310-73-2 7647-01-0
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JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES · 2015 · IF 2.729

Effects of berberine and pomegranate seed oil on plasma phospholipid metabolites associated with risks of type 2 diabetes mellitus by U-HPLC/Q-TOF-MS

Xia Wu,Yan Li,Qiu Wang,Weimin Li,Yifan Feng

A rapid and reliable ultra-performance liquid chromatography coupled with electrospray ionization/quadrupole-time-of-flight mass spectrometry (U-HPLC/Q-TOF-MS) has been firstly used to analyze the changes of plasma phospholipids, in type 2 diabetes mellitus (T2DM) mice after administration of berberine and pomegranate seed oil (PSO). The separation of plasma phospholipids was carried out on an Acquity U-HPLC BEH C18 column (2.1   mm   ×   50   mm, 1.7   μm, Waters) by linear gradient elution using a mobile phase consisting of 10   mM ammonium formate in water and acetonitrile: isopropanol (1:1, v/v) mixed solution added by 0.25% water and 10   mM ammonium formate. The method demonstrated a good precision and reproducibility. Linear regression analysis showed a good linearity. And potential biomarkers were discovered based on their mass spectra and chemometrics methods. The results demonstrated that the proposed U-HPLC/Q-TOF-MS method was successfully applied to analyze the dynamic changes of phospholipids components in plasma of T2DM mice after drug treatment and could provide a useful data base for meriting further study in humans and investigating pharmacological actions of drugs.

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PHYTOTHERAPY RESEARCH · 2026 · IF 8.1

Epi-Berberine Alleviates Ulcerative Colitis, Protects the Intestinal Mucosal Barrier, and Inhibits Colonic Inflammation via Glutaminyl-Peptide Cyclotransferase in a Mouse Model of DSS-Induced Colitis

Bingyu Chen,Ke Liu,Yaya Guo,Jingwei Zhao,Yanhua Wang

The global incidence of ulcerative colitis (UC), a chronic inflammatory bowel disease, is rising. Epi-berberine (EPI), an alkaloid from Coptidis Rhizoma , shows potential for UC treatment. This study aimed to assess EPI's effect on UC and explore the mechanism underlying its UC-alleviating effect. The therapeutic effects of EPI on UC were validated in dextran sulfate sodium (DSS)-induced colitis mice and lipopolysaccharide (LPS)-induced Caco-2 inflammatory models and further investigated the underlying mechanism. In vivo, high-dose EPI (200 mg/kg) attenuated weight loss, reduced disease activity index, increased colon length, lowered colon macroscopic/histological scores, restored intestinal mucosal barrier and inhibited colonic inflammation. EPI (25/50 μM) had similar in vitro effects. mRNA-seq identified EPI-regulated genes in UC mice, revealing six gene clusters with analogous expression patterns. The largest cluster contained genes upregulated by DSS but downregulated by EPI, potentially involved in the MAPK pathway. Key DEGs were enriched in PI3K-Akt and MAPK pathways, verified in vivo and in vitro. Literature retrieval and molecular docking predicted glutaminyl-peptide cyclotransferase (QPCT) as EPI's potential UC therapeutic target. EPI inhibited DSS/LPS-induced QPCT upregulation in vivo and in vitro; QPCT knockdown suppressed inflammation and preserved Caco-2 monolayer barrier function, while QPCT overexpression reversed EPI's therapeutic effects. QPCT mediates PI3K-Akt/MAPK activation, and its overexpression abrogated EPI's inhibitory effects. EPI alleviates murine UC by protecting the intestinal mucosal barrier and inhibiting inflammation, likely via regulating the QPCT-PI3K-Akt/MAPK pathway. It provides a preclinical basis for developing prophylactic strategies for inflammatory bowel disease.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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NEUROTOXICITY RESEARCH · 2020 ·Vol. 38 ·期 1 ·59-73 · IF 2.992

The Secretion from Bone Marrow Mesenchymal Stem Cells Pretreated with Berberine Rescues Neurons with Oxidative Damage Through Activation of the Keap1-Nrf2-HO-1 Signaling Pathway

Wen Caiyan,Huang Cuiqin,Yang Mei,Fan Chongzhu,Li Qin,Zhao Jiayi,Gan Danhui,Li An,Zhu Lihong,Lu Daxiang

Oxidative stress is a potential pathological mechanism of Alzheimer’s disease (AD). Berberine (BBR) can improve antioxidative capacity and inhibit Aβ protein aggregation and tau protein hyperphosphorylation in AD, and stem cell therapy is also increasingly recognized as a therapy for AD. Bone marrow mesenchymal stem cells (BMSCs) have many advantages, as they exhibit antioxidant and anti-inflammatory activity and secrete a variety of neurotrophic factors, and play important roles in neurodegenerative disease treatment. In this study, we investigated the antioxidant effects of secretions from BMSCs pretreated with BBR on tert -butyl hydroperoxide ( t -BHP)–damaged neurons. We demonstrated that BBR can enhance BMSC viability and the secretion of nerve growth factor (NGF) and brain-derived neurotrophic factor (BDNF), both of which are vital neurotrophic factors that maintain neuronal growth. Moreover, conditioned medium from BBR-treated BMSCs (BBR-BMSC-CM) reduced reactive oxygen species (ROS) production, attenuated a decrease in the mitochondrial membrane potential, and ameliorated neuronal apoptosis by decreasing levels of the apoptotic proteins Bax/Bcl-2, cytochrome c, and cleaved caspase-3/caspase-3. In addition, increased synaptophysin (SYP) and postsynaptic density protein 95 (PSD95) levels indicated that neuronal synaptic function was restored. Further study revealed that BBR-BMSC-CM activated the antioxidant proteins Keap1, Nrf2, and HO-1. In conclusion, our results showed that BBR-BMSC-CM attenuated apoptosis and oxidative damage in neurons by activating the Keap1-Nrf2-HO-1 signaling pathway. Taken together, these results also suggest BBR as a drug to stimulate the secretion of nutritional cytokines with the potential to treat AD.

CAS / MDL: 633-65-8
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INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES · 2023 ·Vol. 24 ·期 20 ·15403 · IF 5.6

Berberine-Encapsulated Poly(lactic-co-glycolic acid)–Hydroxyapatite (PLGA/HA) Microspheres Synergistically Promote Bone Regeneration with DOPA-IGF-1 via the IGF-1R/PI3K/AKT/mTOR Pathway

Li Chen,Meng Tian,Jing Yang,Zhenxu Wu

Polymer microspheres have recently shown outstanding potential for bone tissue engineering due to their large specific surface area, good porosity, injectable property, good biocompatibility, and biodegradability. Their good load-release function and surface modifiability make them useful as a carrier of drugs or growth factors for the repair of bone defects in irregularly injured or complex microenvironments, such as skull defects. In this study, berberine (BBR)-encapsulated poly(lactic-co-glycolic acid) (PLGA)/hydroxyapatite (HA) microspheres were fabricated using electrified liquid jets and a phase-separation technique, followed by modification with the 3,4-hydroxyphenalyalanine-containing recombinant insulin-like growth–factor-1 (DOPA-IGF-1). Both the BBR and the IGF-1 exhibited sustained release from the IGF-1@PLGA/HA-BBR microspheres, and the composite microspheres exhibited good biocompatibility. The results of the alkaline phosphatase (ALP) activity assays showed that the BBR and IGF-1 in the composite microspheres synergistically promoted the osteogenic differentiation of MC3T3-E1 cells. Furthermore, it was confirmed that immobilized IGF-1 enhances the mRNA expression of an osteogenic-related extracellular matrix and that BBR accelerates the mRNA expression of IGF-1-mediated osteogenic differentiation and cell mineralization. Further cellular studies demonstrate that IGF-1 could further synergistically activate the IGF-1R/PI3K/AKT/mTOR pathway using BBR, thereby enhancing IGF-1-mediated osteogenesis. Rat calvarial defect repair experiments show that IGF-1@PLGA/HA-BBR microspheres can effectively promote the complete bony connection required to cover the defect site and enhance bone defect repair. These findings suggest that IGF-1@PLGA/HA-BBR composite microspheres show a great potential for bone regeneration.Keywords:polymer microspheres;berberine (BBR);IGF-1;bone regeneration;osteogenic differentiation

CAS / MDL: 141433-60-5
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Analytical Methods · 2014 ·Vol. 6 ·期 9 ·2998-3008 · IF 1.938

The simultaneous determination of berberine, palmatine, coptisine, epiberberine and jatrorrhizine in rat plasma by LC-MS/MS and a pharmacokinetic comparison after the oral administration of Rhizoma coptidis and Jiao-Tai-Wan extract

Guanghui Liu,Wei He,Hao Cai,Xiuman Sun,Waner Hou,Manna Lin,Zhiyong Xie,Qiongfeng Liao

A rapid and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed to simultaneously determine berberine, palmatine, coptisine, epiberberine and jatrorrhizine in rat plasma, using tetrahydropalmatine as an internal standard. The separation of the five compounds was carried out on a C18 column using a mobile phase consisting of acetonitrile and water (containing 5 mmol ammonium acetate adjusted to pH 5.0 with formic acid). The detection was performed in the multiple reaction monitoring (MRM) mode via the electrospray ionization (ESI) source operating in the positive ionization mode. Linear calibration curves were obtained over the concentration range of 0.20–200.0 ng ml−1 for berberine, and 0.20–100.0 ng ml−1 for palmatine, coptisine, epiberberine and jatrorrhizine. The accuracy, precision and extraction recovery of the five analytes were all satisfactory. The validated method was successfully applied to study the pharmacokinetic differences of the five protoberberine-type alkaloids after the oral administration of Rhizoma coptidis (RC) and Jiao-Tai-Wan (JTW) extract. It was found that the Tmax values of the five ingredients in the JTW extract were significantly increased (P < 0.05) when compared with those in RC. In addition, the AUC0–t of palmatine, coptisine and epiberberine were significantly increased (P < 0.05).

CAS / MDL: 631-61-8
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