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Berberine
Journal of Natural Medicines · 2017 ·Vol. 72 ·期 2 ·390-398 · IF 1.982

Berberine protects HK-2 cells from hypoxia/reoxygenation induced apoptosis via inhibiting SPHK1 expression

Lu Jianrao,Yi Yang,Pan Ronghua,Zhang Chuanfu,Han Haiyan,Chen Jie,Liu Wenrui

Renal ischemia reperfusion injury (RIRI) refers to the irreversible damage for renal function when blood perfusion is recovered after ischemia for an extended period, which is common in clinical surgeries and has been regarded as a major risk for acute renal failures (ARF) that is accompanied with unimaginably high morbidity and mortality. Hypoxia during ischemia followed by reoxygenation via reperfusion serves as a major event contributing to cell apoptosis, which has been widely accepted as the vital pathogenesis in RIRI. Preventing apoptosis in renal tubular epithelial cell has been considered as effective method for blocking RIRI. In this paper, we established a hypoxia/reoxygenation (H/R) injury model in human proximal tubular epithelial HK-2 cells. Here, we found increased SPHK1 levels in H/R injured HK-2 cells, which could be significantly down regulated after berberine treatment. Berberine has been reported to exert a protective effect on H/R-induced apoptosis of HK-2 cells. So, in our present study, we planned to investigate whether SPHK1 participated in the anti-apoptosis process of berberine in H/R injured HK-2 cells. Our study confirmed the protective effect of berberine against H/R-induced apoptosis in HK-2 cells through promoting cells viability, inhibiting cells apoptosis, and down-regulating p-P38, caspase-3, caspase-9 as well as SPHK1, while up regulating the ratio of Bcl-2/Bax. However, SPHK1 overexpression in HK-2 cells induced severe apoptosis, which can be significantly ameliorated with additional berberine treatment. We concluded that berberine could remarkably prevent H/R-induced apoptosis in HK-2 cells through down-regulating SPHK1 expression levels, and the mechanisms included the suppression of p38 MAPK activation and mitochondrial stress pathways.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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Frontiers in Chemistry · 2024 · IF 3.8

Comprehensive plasma metabolomics analysis of berberine treatment in ulcerative colitis rats by LC-MS/MS

Baodong Feng,Linqi Su,Yang Yang,Renyan Liu,Yu Zhang,Lingyi Xin,Li Wang,Zhiming Yang,Xuemei Wei,Qinhua Chen

Background: Ulcerative colitis (UC) is a chronic inflammatory bowel disease (IBD) influenced by multiple factors. Berberine, an isoquinoline alkaloid derived from the root and bark of Coptis chinensis Franch., has shown promise in managing UC, but its underlying mechanisms remain unclear.Methods: To elucidate the relationship between berberine, ulcerative colitis (UC), and the organism’s metabolome, we established a dextran sulfate sodium (DSS)-induced UC model in rats. Colonic tissue was collected for histopathological examination, while plasma samples were analyzed using liquid chromatography-tandem mass spectrometry (LC-MS/MS) with dynamic Multiple Reaction Monitoring (dMRM). This approach, characterized by its short analysis time of 20 min per sample, excellent reproducibility, and straightforward data processing, allowed for the comprehensive detection of a wide array of metabolites, including amino acids, lipids, and organic acids, many of which are implicated in the pathophysiology of UC.Results: Our results showed that berberine modulated the metabolic disturbances of 33 compounds in the plasma of UC rats, primarily including amino acids, pyrimidines, organic phosphoric acids, fatty acyls, and organonitrogen compounds. These altered metabolites were associated with various pathways, such as amino acid metabolism, glutathione metabolism, nicotinate and nicotinamide metabolism, taurine and hypotaurine metabolism, pyrimidine metabolism, glyoxylate and dicarboxylate metabolism, and the citrate cycle (TCA cycle). Notably, 3-hydroxyproline, homocysteic acid, L-threonine, L-lysine, carbamoyl phosphate, O-phosphoethanolamine, taurine, leucine, and phosphorylcholine exhibited significant differences between the Treatment and Model groups, with levels reverting to those of the Control group (p < 0.001). These findings suggested that these compounds may serve as potential plasma biomarkers for UC.Conclusion: This study provided valuable insights into the mechanism by which berberine exerted its therapeutic effects on UC through metabolomics. Our results highlighted berberine’s potential to modulate key metabolic pathways and restore the levels of several metabolites, suggesting its utility as a therapeutic agent for UC. These findings underscored the importance of metabolomics in understanding the pathophysiology and treatment of UC.

研究领域: 药理学 · 代谢组学 · 炎症性肠病研究
✓ 已验证 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

Berberine‑calcium alginate-coated macrophage membrane-derived nanovesicles for the oral treatment of ulcerative colitis

Huilin Ma,Yunmei Li,Huan Shi,Biaobiao Wang,He Tian,Xifan Mei,Chao Wu

In this study, we developed calcium alginate-coated nanovesicles derived from macrophage membranes loaded with berberine (Ber@MVs-CA) for the oral treatment of ulcerative colitis (UC). Ber@MVs-CA demonstrates resistance to gastric acid and controlled drug release in the colonic pH environment, while actively targeting sites of ulcerative colitis injury. pH-responsive release of Ber in Ber@MVs-CA was confirmed through in vitro release experiments. The results indicated a total of 19.35 ± 1.61 % of Ber was cumulatively released from Ber@MVs-CA in SGF and SIF at 4 h, and approximately 87.14 ± 2.33 % release in simulated colonic fluid (pH 7.4) after 24 h. The targeting ability of Ber@MVs-CA was confirmed using laser confocal microscopy (CLSM), Transwell™ system, and in vivo imaging. Results demonstrated effective targeting of inflammatory macrophages and sustained retention in the colon. In vitro and in vivo (mice) assessments via immunofluorescence, ELISA kit, and reactive oxygen species (ROS) assays demonstrated that Ber@MVs-CA effectively attenuated inflammatory responses, modulated macrophage polarization, and inhibited oxidative stress. Additionally, we evaluated the therapeutic efficacy of Ber@MVs-CA in a Clostridium perfringens -induced enteritis model in chickens, demonstrating its effectiveness in alleviating enteritis. Consequently, Ber@MVs-CA exhibits great potential as an oral nano-formulation for the treatment of enteritis. Thus, Ber@MVs-CA shows great potential as an oral nano-formulation for the treatment of enteritis.

CAS / MDL: 39562-70-4
研究领域: 药剂学 · 炎症研究 · 生物材料科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF HAZARDOUS MATERIALS · 2024 · IF 12.2

Berberine and chlorogenic acid-assembled nanoparticles for highly efficient inhibition of multidrug-resistant Staphylococcus aureus

Siyuan Fu,Xuan Yi,Yi Li,Yuanhui Li,Xiaolin Qu,Peng Miao,Yuanyuan Xu

Due to the bacteria resistant to various first-line antibiotics, it is urgent to develop efficient antibiotic alternatives and formulate multidimensional strategies. Herein, supramolecular Chinese medicine nanoparticles are synthesized by self-assembly of berberine (BBR) and chlorogenic acid (CGA), which exhibit higher inhibitory effect against S taphylococcus aureus and multidrug-resistant S taphylococcus aureus (MRSA) than ampicillin, oxacillin, BBR, CGA, as well as mixture of BBR and CGA (minimum inhibitory concentration, MIC = 1.5 µM). The inhibition by BBR/CGA nanoparticles (2.5 µM) reaches 99.06 % for MRSA, which is significantly higher than ampicillin (29.03 %). The nanoparticles with 1/2 MIC can also synergistically restore the antimicrobial activity of ampicillin against MRSA. Moreover, in vivo therapeutic outcome in the murine skin wound infection model suggests that the nanoparticles are able to promote wound healing. This study provides new insights in the application of Chinese medicines self-assembly for MRSA inhibition, as well as solutions for potential persistent clinical infections and drug deficiencies.

CAS / MDL: 7758-02-3
研究领域: 药学 · 纳米技术 · 微生物学 · 中药
✓ 已验证 产品关联 DOI PubMed 高影响因子
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BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS · 2024 · IF 2.5

Berberine alleviates cholesterol and bile acid metabolism disorders induced by high cholesterol diet in mice

Qihan Wang,Weiyi Shen,Wentao Shao,Hai Hu

Berberine (BBR) is a traditional Chinese herb with broad antimicrobial activity . Gut microbiota plays an important role in the metabolism of bile acids and cholesterol. Our study investigated the effects of BBR on alleviating cholesterol and bile acid metabolism disorders induced by high cholesterol diet in mice. Adult male C57BL/6J mice fed with high cholesterol diet (HC) containing 1.25 % cholesterol (HC group) or fed with chow diet containing 0.02 % cholesterol (Chow group) served as controls. BBR50 and BBR100 group mice were fed with HC, and oral BBR daily at doses of 50 or 100 mg/kg respectively for 8 weeks. The results showed that BBR could reshape the homeostasis and composition of gut microbiota. The abundance of Clostridium genera was significantly inhibited by BBR, which resulted in a significant reduction of secondary bile acids within the enterohepatic circulation and a significant lower hydrophobic index of bile acids . The absorption of cholesterol in intestine, the deposition of cholesterol in liver and the excretion of cholesterol in biliary tract were significantly inhibited by BBR, which promoted the unsaturation of cholesterol in bile. These findings suggest the potential utility of BBR as a functional food to alleviate the negative effects of high cholesterol diet.

CAS / MDL: 2086-83-1
研究领域: 营养学 · 微生物学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF ALLOYS AND COMPOUNDS · 2024 · IF 5.8

CoFe2O4/BiFeO3 Z-scheme heterojunction under rotating magnetic field: Enhanced photocatalytic degradation of berberine hydrochloride

Tianjiao Zhai,Jinyi Wang,Rui Min,Xu Su,Kai Ma,Guozhen Zhang,Tianhong Zhou

The cooperation of heterojunction and magnetic field can effectively improve the efficiency of photocatalytic degradation of pollutants. Herein, CoFe 2 O 4 /BiFeO 3 Z-scheme heterojunctions (CFO/BFO) were applied in the magnetic field-assisted photocatalytic reaction generated by a rotating permanent magnet for the degradation of berberine hydrochloride, which achieved a degradation rate of 96.49% and showed good stability and recoverability. The active substances controlling the reaction were holes and superoxide radicals . The excellent magneto-photocatalytic performances of CoFe 2 O 4 /BiFeO 3 can be attributed to the construction of the Z-scheme heterojunction, the magnetoelectric effect produced by the synergistic combination in the magnetic field, and the driving force of the Lorentz force for photocatalysis .

研究领域: 环境科学 · 材料科学 · 化学
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MOLECULES · 2024 ·Vol. 29 ·期 1 ·273 · IF 4.2

Synthesis of New Derivatives of Berberine Canagliflozin and Study of Their Antibacterial Activity and Mechanism

Jinsheng Li,Xueli Hou,Jinlong Xiao,Li Zhu,Yujie Deng,Ziyi Li,Zijian Zhao,Zhenghong Luo,Hao Wei

The isoquinoline alkaloid berberine, derived from Coptidis rhizoma, exhibits antibacterial, hypoglycemic, and anti-inflammatory properties. Canagliflozin is a sodium–glucose cotransporter 2 (SGLT2) inhibitor. We synthesized compounds B9OC and B9OBU by conjugating canagliflozin and n-butane at the C9 position of berberine, aiming to develop antimicrobial agents for combating bacterial infections worldwide. We utilized clinically prevalent pathogenic bacteria, namelyStaphylococcus aureus,Escherichia coli, andPseudomonas aeruginosa, to investigate the antibacterial efficacy of B9OC. This was accomplished through the determination of the MIC80values, analysis of bacterial growth curves, evaluation of biofilm formation using crystal violet staining, assessment of impact on bacterial proteins via SDS-PAGE analysis, and observation of alterations in bacterial morphology utilizing field emission scanning electron microscopy. Meanwhile, the ADMET of compound B9OC was predicted using a computer-aided method. The findings revealed that B9OC exhibited lower minimal inhibitory concentrations against all three bacteria compared to berberine alone or in combination with canagliflozin. The minimal inhibitory concentrations (MICs) of B9OC against the three experimental strains were determined to be 0.035, 0.258, and 0.331 mM. However, B9OBu exhibited a lower level of antimicrobial activity compared to berberine. The compound B9OC exhibits a broad spectrum of antibacterial activity by disrupting the integrity of bacterial cell walls, leading to cellular rupture and the subsequent degradation of intracellular proteins.

CAS / MDL: 842133-18-0
研究领域: 药理学 · 微生物学 · 药物化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES · 2025 ·Vol. 26 ·期 5 ·2193 · IF 4.9

Enhancing the Therapeutic Efficacy of Berberine and Quercetin Through Salt Formulation for Liver Fibrosis Treatment

Yangyang Cheng,Haoyang Yu,Sitong Yang,Xiaolian Tian,Mengyu Zhao,Ling Ren,Xiuping Guo,Chujuan Hu,Jiandong Jiang,Lulu Wang

Liver fibrosis, caused by chronic hepatic injury, is a major threat to human health worldwide, as there are no specific drugs available for its treatment. Natural compounds, such as berberine (BBR) and quercetin (QR), have shown the ability to regulate energy metabolism and protect the liver without significant adverse effects. Additionally, combination therapy (the cocktail therapy approach), using multiple drugs, has shown promise in treating complicated conditions, including liver injury. In this study, we prepared a salt formulation of BBR and QR (BQS) to enhance their combined effect on liver fibrosis. The formation of BQS was confirmed using various analytical techniques, including nuclear magnetic resonance spectroscopy (NMR), differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR), powder X-ray diffractometry (PXRD), and scanning electron microscopy (SEM). The results demonstrated that the dissolution efficiency and bioavailability of QR significantly increased in the BQS form, aligning with that of BBR, compared to the physically mixed (BQP) form. Moreover, BQS exhibited a superior inhibitory effect on fibrosis compared to BQP in the human hepatic stellate cell line LX-2 by modulating lipid accumulation, inflammation, apoptosis, and the cell cycle. Furthermore, in a mouse model of hepatic fibrosis induced by methionine and choline-deficient (MCD) diets, BQS demonstrated enhanced anti-fibrotic activities compared to BQP. These findings suggest that BQS holds promise as a potential alternative treatment for liver fibrosis. Importantly, this study provides novel insights into achieving a cocktail effect through the salt formation of two or more drugs. The results highlight the potential of salt formulations in enhancing the therapeutic efficacy and consistent biological processes of drug combinations.

CAS / MDL: 117-39-5
研究领域: 药理学 · 肝病学 · 药物开发 · 分子生物学
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NEW JOURNAL OF CHEMISTRY · 2024 ·Vol. 48 ·期 36 ·15884-15893 · IF 2.7

Inclusion complex of berberine hydrochloride with serine-β-cyclodextrin: construction, characterization, inclusion mechanisms, and bioactivity

Dong Ju Zhou,Wei Ming Liu,Su Ping Dai,Shuai Qiang Jiang,Yin Wang,Jia Jia Yang,Ya Wei Chen,Jun Liang Chen,Hyun Jin Park,Hui Yun Zhou

In our work, serine-modified β-cyclodextrin (Ser-β-CD) was synthesized and a berberine hydrochloride (BBH)/Ser-β-CD inclusion complex (IC) was prepared using the freeze-drying method. Phase solubility studies showed that BBH and Ser-β-CD formed stable inclusion complexes in a stoichiometric ratio of 1 : 1. The IC was characterized using SEM and FT-IR analyses. The results of molecular docking showed that BBH was completely contained in the Ser-β-CD cavity and the binding energy was −7.87 kcal mol−1. The results of in vitro release studies indicated that BBH could be released slowly from the IC. In addition, the prepared Ser-β-CD and IC had good biocompatibility. The IC demonstrated excellent antibacterial activity against Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus). Therefore, the BBH/Ser-β-CD IC has potential application prospects in biomedicine and food industry.

CAS / MDL: 98-59-9 633-65-8
研究领域: 药学 · 材料科学 · 生物技术 · 微生物学
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ACS Applied Polymer Materials · 2026 · IF 5.2

Injectable Self-Healing Berberine-Loaded Boronate Ester Cross-Linked Chitosan/Cellulose Hydrogels for Wound Management

Yidan Zhang,Wensi Jiang,Yuqian Liu,Yang Huang,Chao Liu,Huining Xiao,Farzad Seidi

Injectable self-healing hydrogels with intrinsic antibacterial properties represent a promising advancement for wound management. This study presents a natural-based hydrogel system for full-thickness wound healing, fabricated via the hybridization of quaternary ammonium cellulose phenylboronic acid (QAC-PBA) with quaternary ammonium glycol chitosan (QGCS) and the in situ encapsulation of berberine (BBR). The quaternary ammonium groups endow intrinsic antibacterial properties, and the dynamic boronate esters confer self-healing and injectable properties to the hydrogel. Additionally, the release of BBR provides an additional antibacterial mechanism by targeting possible wound sites that are not in direct contact with the hydrogel. The hydrogel demonstrated a strong antibacterial effect (up to 94.1% against E. coli and 99.8% against S. aureus), fast self-healing, injectability, and high biocompatibility (>100% viability against NIH3T3 cells). In a full-thickness wound model, the hydrogel dressing achieved 95% wound closure in 14 days compared to 89% for the Tegaderm film control.

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JOURNAL OF COLLOID AND INTERFACE SCIENCE · 2025 · IF 9.7

Bovine serum albumin modified carbon dots and berberine composite promotes tumor mitochondrial dysfunction and apoptosis

He Feng,Yang-Jian Hong,Qi-Qi Zheng,Jia-Ming Ge,Hong-Wei Cheng,Yu-Peng Liu,Jie Deng,Qing-Lin Li,Song-Nan Qu

Precise delivery of antitumor drugs has become a research focus in cancer treatment. Herein, we developed a bovine serum albumin (BSA) modified carbon dots (CDs) and berberine (BBR) composite for improved intravenous BBR delivery. The surface-negatively charged CDs can associate with positively charged BBR through electrostatic interactions, resulting in CDs and BBR composite (BBR@CDs). BBR@CDs can be further stabilized by modification with BSA, resulting in enlarged composite (BSA@BBR@CDs) with much better water solubility. In vitro, with BSA modification, BSA@BBR@CDs was more readily taken up by tumor cells than BBR@CDs. After entering cells, BSA@BBR@CDs could more efficiently target mitochondria, resulting in mitochondrial dysfunction and eventually showing a stronger pro-apoptotic effect on tumor cells than BBR. In vivo, BSA@BBR@CDs can well accumulate in tumors via intravenous injection and significantly inhibit the tumor growth without significant toxicity to other organs. Therefore, BSA@BBR@CDs holds potential as a promising nanomedicine for cancer therapy.

研究领域: 癌症研究 · 纳米技术 · 药剂学 · 细胞生物学 · 生物医学工程
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ChemistrySelect · 2025 ·Vol. 10 ·期 35 ·e03533 · IF 2

Self-Assembled Synergistic Nanoparticles from Carrier-Free Berberine and Ferulic Acid for Improved Antibacterial Activity

Xiaodan Zheng,Ruolong Ma,Ziyan Song,Limeng Zhang,Chuanda Ruan,Wenzhi Yang,Yi Zhang,Xiaohui Yan,Fei Tian

With the widespread overuse of antibiotics, Staphylococcus aureus has developed multiple resistances to a variety of first-line antibiotics; therefore, it is imperative to explore novel antimicrobial strategies to solve the problem of resistance. Traditional Chinese medicines (TCM) are considered sources of chemicals with potential healing properties. In this study, berberine (BBR) and ferulic acid (FA) were used as raw materials to prepare nanoparticles with enhanced antibacterial activity by self-assembly technology. The study revealed that the self-assembly process involves non-covalent interactions. Minimum inhibitory concentration (MIC) of the FA-BBR NPs was 0.1 µmol/mL, and the antibacterial rate of FA-BBR NPs with a concentration of 0.2 µmol/mL against S. aureus was 94.56 ± 0.57%, which was significantly higher than monomers. The Bradford protein concentration assay was used to analyze the leakage of cellular contents. Scanning electron microscopy (SEM) and the fluorescent probe DiSC 3 (5) revealed that the nanoparticles can affect the integrity and permeability of bacterial biofilm, which is a key factor contributing to their superior antibacterial activity. Graphical A self-assembled carrier-free nano drug delivery system composed of ferulic acid and berberine was developed using a one-step self-assembly approach. FA-BBR NPs were found to significantly improve the solubility and antibacterial activity of the individual traditional Chinese medicine compounds. The two components primarily interact through noncovalent forces, including hydrogen bonding, ᴨ-ᴨ stacking, and electrostatic interactions. Further investigation revealed that FA-BBR NPs exerted enhanced antibacterial effects by compromising the integrity and permeability of bacterial cell membranes.

研究领域: 药剂学 · 纳米医学 · 微生物学 · 天然药物化学 · 分子药理学
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