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Berberine
ANALYTICAL AND BIOANALYTICAL CHEMISTRY · 2019 ·Vol. 411 ·期 23 ·5963-5973 · IF 3.286

A highly fluorescent lanthanide metal-organic framework as dual-mode visual sensor for berberine hydrochloride and tetracycline

Xiong Jie,Yang Lu,Gao Li Xia,Zhu Pan Pan,Chen Qian,Tan Ke Jun

A microscale highly fluorescent Eu metal-organic framework (Eu-MOF) was synthesized with terephthalic acid and 1H-1,2,4-triazole-3,5-diamine by one-pot hydrothermal method. And it was characterized by scanning electron microscope, Fourier transform infrared spectroscopy, powder X-ray diffraction, fluorescence spectroscopy, thermogravimetric analysis, and energy dispersive X-ray mapping. The prepared Eu-MOF has high quantum yield of 30.99%, excellent water dispersibility, good fluorescence stability, and favorable thermal stability. Based on the distinctly different fluorescence responses of different emission, the prepared Eu-MOF was used as dual-mode visual sensor for the sensitive detection of berberine hydrochloride and tetracycline. The limits of detection are 78 nM and 17 nM, respectively. The sensing mechanism was also discussed. Moreover, a filter paper sensor has been designed for sensing tetracycline with a notable fluorescence color change from blue to red. The prepared Eu-MOF is promising to be developed as a multi-mode luminescent sensor for visual detection in biochemical analysis. Illustration of the synthesis of Eu-MOF and its sensing applications for berberine hydrochloride and tetracycline

✓ 已验证 产品关联 DOI PubMed 高影响因子
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Biomaterials Advances · 2025 · IF 6

Fire cupping inspired negative-pressure microneedle syringes loaded with herb berberine-based nano composite for psoriasis therapy

Dan Deng,Runfu Chen,Suai Lin,Yanxin Tao,Gaojin Pei,Bofei Cheng,Mengzhen Zhao,Haoxin Cheng,Junze Yan,Xiaolei Wang

Psoriasis, an immune-mediated chronic inflammatory skin disorder, poses challenges for topical treatment due to the thickening of the stratum corneum, hindering drug penetration. Furthermore, long-term use of chemical drugs may lead to immunosuppression and abnormal hepatic or renal dysfunction. Inspired by traditional Chinese fire cupping (Ba Huo Guan), a negative-pressure microneedle syringe therapy has been proposed here for psoriasis treatment. This microneedle syringe demonstrated an enhanced transepidermal drug delivery efficiency. Additionally, the microneedles contain nanoparticles self-assembled from Chinese herbal monomers berberine (BBR) and ferulic acid (FA), which play vital roles in psoriasis treatment, including inhibiting abnormal proliferation of local microbial communities, scavenging excess reactive oxygen species, suppressing keratinocyte proliferation locally, and modulating macrophage polarization to mitigate inflammation.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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TOXICOLOGY AND APPLIED PHARMACOLOGY · 2024 · IF 3.3

Berberine alleviated contrast-induced acute kidney injury by mitophagy-mediated NLRP3 inflammasome inactivation in a mice model

Yalin Yang,Shuang Jiang,Yu Mu,Chilu Liu,Yanxing Han,Jiandong Jiang,Yuhong Wang

The incidence of contrast-induced acute kidney injury (CI-AKI) has escalated to become the third most prevalent cause of hospital-acquired AKI, with a lack of efficacious interventions. Berberine (BBR) possesses diverse pharmacological effects and exhibits renoprotective properties; however, limited knowledge exists regarding its impact on CI-AKI. Therefore, our study aimed to investigate the protective effects and underlying mechanisms of BBR on CI-AKI in a mice model, focusing on the nucleotide-binding oligomerization domain-like pyrin domain-containing protein 3 (NLRP3) inflammasome and mitophagy. The CI-AKI mice model was established by administering L-NAME, indomethacin (10 mg/kg), and iohexol (11 g/kg) following water deprivation. A pretreatment of 100 mg/kg of BBR was orally administered to the mice for two weeks. Renal injury markers, damage-associated molecular patterns (DAMPs), renal histopathology, mitochondrial morphology, autophagosomes, and potential mechanisms were investigated. BBR effectively reduced levels of renal injury biomarkers such as serum cystatin C, urea nitrogen, and creatinine, downregulated the protein levels of kidney injury molecule 1 (KIM1), and mitigated renal histomorphological damage. Moreover, BBR reduced DAMPs, including high mobility group box 1 (HMGB1), heat shock protein 70 (HSP70), and uric acid (UA). It also alleviated oxidative stress and inflammatory factors such as monocyte chemotactic protein 1 (MCP-1), tumor necrosis factor-alpha (TNF-α), interleukin 6 (IL-6), and interleukin 1 beta (IL-1β). Furthermore, the activation of NLRP3 inflammasome was attenuated in the BBR pretreatment group, as evidenced by both mRNA and protein levels. Electron microscopy and Western blotting examination revealed that BBR mitigated mitochondrial damage and enhanced mitophagy. Additionally, BBR increased the P-AMPK/AMPK ratio. These findings indicate that BBR exerts a protective effect against CI-AKI by suppressing NLRP3 inflammasome activation and modulating mitophagy, providing a potential therapeutic strategy for its prevention.

CAS / MDL: 66108-95-0
✓ 已验证 产品关联 DOI PubMed 高影响因子
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International Journal of Nanomedicine · 2024 · IF 6.6

Nanocarrier-Assisted Delivery of Berberine Promotes Diabetic Alveolar Bone Regeneration by Scavenging ROS and Improving Mitochondrial Dysfunction

Ye Ming,Xinyi He,Zhenxing Zhao,Xuehuan Meng,Ye Zhu,Hao Tan,Guoyin Yang,Yun Hu,Leilei Zheng

Purpose Oxidative stress and mitochondrial dysfunction are potential contributors to the compromised tissue regeneration capacity of alveolar bone in diabetic patients. Berberine, an active plant alkaloid, exhibits multiple pharmacological effects including antioxidation, blood glucose- and blood lipid-lowering properties. However, it remains uncertain whether berberine can improve impaired osteogenesis in type 2 diabetes mellitus (T2DM), and its poor solubility and oral bioavailability also constrain its applications in bone regeneration. Thus, our study aimed to probe the effects of berberine on bone marrow stem cells (BMSCs) in a diabetic microenvironment, with a greater emphasis on developing a suitable nano-delivery system for berberine and assessing its capability to repair diabetic alveolar bone defects.Methods Firstly, BMSCs were exposed to berberine within a high glucose and palmitate (HG+PA) environment. Reactive oxygen species levels, mitochondrial membrane potential, ATP generation, cell apoptosis, and osteogenic potential were subsequently assessed. Next, we explored the regulatory mechanism of autophagy flux in the positive effects of berberine. Furthermore, a nanocarrier based on emulsion electrospinning for sustained local delivery of berberine (Ber@SF/PCL) was established. We assessed its capacity to enhance bone healing in the alveolar bone defect of T2DM rats through micro-computed tomography and histology analysis.Results Berberine treatment could inhibit reactive oxygen species overproduction, mitochondrial dysfunction, apoptosis, and improve osteogenesis differentiation by restoring autophagy flux under HG+PA conditions. Notably, Ber@SF/PCL electrospun nanofibrous membrane with excellent physicochemical properties and good biological safety had the potential to promote alveolar bone remodeling in T2DM rats.Conclusion Our study shed new lights into the protective role of berberine on BMSCs under T2DM microenvironment. Furthermore, berberine-loaded composite electrospun membrane may serve as a promising approach for regenerating alveolar bone in diabetic patients.

CAS / MDL: 497-19-8
✓ 已验证 产品关联 DOI PubMed 高影响因子
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CHEMICAL ENGINEERING JOURNAL · 2025 · IF 13.2

Mitigating the Coffee-Ring effect exhibited by pesticide solutions on pepper leaves using amphiphilic berberine sulfate microgels

Shuangli Zhang,Jingmei Li,Lihao Lei,Lan Li,Rongyu Li,Xianhui Yin,Zhuo Chen,Yue Ma,Fengpei Du

Nonuniform deposition of pesticide droplets on crops and their runoff create excessive pesticide waste, posing a major threat to public health and the environment. Microgels are a class of soft colloids that combine the properties of solid particles and polymers to regulate the resistance of pesticides to rainwater runoff and mitigate the coffee-ring effect (CRE). In this study, we developed amphiphilic calcium alginate microgels (UAMs) capable of enhancing the pesticide evaporation uniformity and the deposition of berberine sulfate (BS) on a target crop, as well as its surface adhesion. A BS-loaded UAM (UAM–BS) solution was sprayed onto the surface of pepper leaves. The gel coating contained flexible and complex networks, which are easily entangled with the microstructures on the leaf surface. This ultimately resulted in the removal of the interface void and the improvement of the BS deposition uniformity at multiple scales. In addition, the surfactivity of the microgels was regulated through grafting, which affected the uniformity of the liquid film deposition. Furthermore, the effect of UAM–BS on pepper anthracnose was investigated, and its control efficacy was found to be over 80%. Additionally, it could improve the BS deposition uniformity and adhesion while mitigating the CRE. This study establishes the use of alginate-based gel coatings as a promising strategy for improving pesticide utilization while addressing the issues of easy runoff and nonuniform deposition. The findings will prove valuable in the fields of bionic materials science, bio-macromolecular chemistry, and agricultural science.

CAS / MDL: 9005-38-3 7647-01-0
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BRITISH JOURNAL OF PHARMACOLOGY · 2025 · IF 7.7

Berberine partially ameliorates cardiolipotoxicity in diabetic cardiomyopathy by modulating SIRT3-mediated lipophagy to remodel lipid droplets homeostasis

Wenxian Chen,Tongzhu Jin,Yilin Xie,Changsheng Zhong,Huiying Gao,Lei Zhang,Jin Ju,Ting Cheng,Mengyang Li,Huifang Wang,Zhenbo Yang,Qin Deng,Zhimin Du,Haihai Liang

Background and Purpose Emerging evidence indicated that the excessive lipid droplets (LDs) accumulation and lipotoxicity play a significant role in the development of diabetic cardiomyopathy (DCM), yet the regulatory mechanisms governing the function of cardiac LDs are still unknown. Lipophagy has been shown to be involved in the maintenance of LDs homeostasis. The objective of this study was to explore the mechanism of lipophagy in cardiomyocytes and investigate whether berberine could mitigate DCM by modulating this pathway. Experimental Approach Bioinformatics analysis identified disorders of lipid metabolism and autophagy in DCM. To carry out further research, db/db mice were utilized. Furthermore, H9C2 cells treated with palmitic acid were employed as a model to explore the molecular mechanisms involved in myocardial lipotoxicity. Key Results The results showed that lipophagy was impaired in DCM. Mechanistically, sirtuin 3 (SIRT3) was demonstrated to regulate lipophagy in cardiomyocytes. SIRT3 was down-regulated in DCM. Conversely, activation of SIRT3 by the activator nicotinamide riboside (NR) could promote lipophagy to alleviate PA-induced lipotoxicity in H9C2 cells. Moreover, berberine administration markedly mitigated diabetes-induced cardiac dysfunction and hypertrophy in db/db mice, which dependent on SIRT3-mediated lipophagy. Conclusion and Implications Collectively, SIRT3 could moderate cardiac lipotoxicity in DCM by promoting lipophagy, suggesting that the regulation of SIRT3-mediated lipophagy may be a promising strategy for treating DCM. The findings indicate that the therapeutic potential of berberine for DCM is associated with lipophagy.

CAS / MDL: 1115-70-4 141433-60-5
✓ 已验证 产品关联 DOI PubMed 高影响因子
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CHEMICAL ENGINEERING JOURNAL · 2025 · IF 13.2

An injectable phosphocreatine-grafted gelatin hydrogel incorporating berberine-loaded copper-carbon dot nanozymes for osteoporotic bone regeneration

Chen Zhang,Junyu Qian,Yuanhao Wang,Binbin Wang,Deli Wang,Sheng Dai,Haotian Qin

Osteoporotic bone defects represent a multifactorial clinical challenge due to impaired osteogenesis, insufficient angiogenesis, hyperactive osteoclast activity, and high infection risk. To address these limitations, we developed an injectable phosphocreatine-grafted gelatin hydrogel (BCG) incorporating berberine-loaded copper‑carbon dot nanozymes (BBR-CuCDs). BBR-CuCDs were synthesized via a one-step hydrothermal method, enabling simultaneous drug loading and catalytic activity, while dual enzymatic and Cu 2+ coordination crosslinking endowed the hydrogel with enhanced mechanical integrity, stability, and sustained release of therapeutic payloads. In vitro, BCG hydrogels significantly promoted BMSC proliferation, adhesion, migration, and osteogenic differentiation, while enhancing HUVEC migration, tube formation, and angiogenic marker expression. The hydrogels also suppressed RANKL-induced osteoclastogenesis and exhibited strong antibacterial effects against both Staphylococcus aureus and Escherichia coli . In vivo, BCG (1.0 mg/mL) hydrogel markedly accelerated bone regeneration and neovascularization in an ovariectomized rat calvarial defect model, as demonstrated by micro-CT and histological analyses, accompanied by elevated expression of COL1A1, BMP2, RUNX2, and CD31. Importantly, transcriptomic profiling revealed that BCG hydrogel activated PI3K-Akt, Wnt/β-catenin, and HIF-1 signaling pathways, highlighting a coordinated mechanism of osteogenesis-angiogenesis coupling and immune modulation. Collectively, this multifunctional hydrogel integrates osteoinductive, proangiogenic, anti-osteoclastic, and antibacterial activities, and demonstrates excellent biosafety, offering a robust and translationally promising platform for osteoporotic bone defect repair.

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FOOD RESEARCH INTERNATIONAL · 2025 · IF 8

High oxygen barrier and synergistically enhanced photodynamic antibacterial films via Berberine/layered double hydroxide for food packaging

Jin Liang,Yanzhi Liu,Fengyi Liu,Xiaoying Zhang,Yue Su,Jun Wang,Fang Duan,Gang Wu,Kai Qiu

Microbial contamination and oxygen ingress are primary drivers of food spoilage, but advanced materials that simultaneously offer high oxygen barrier and effective antibacterial functions remain scarce. To address this dual challenge, we engineered a polyvinyl alcohol-based composite coating, incorporating the natural aggregation-induced emission photosensitizer berberine (BBR) and non-toxic layered double hydroxide nanosheets (LDH NS), on a polyethylene terephthalate substrate. The developed composite film demonstrated a low oxygen transmission rate of 0.06 cm 3  m −2  day −1  atm −1 . Furthermore, it achieved 100 % inhibition rate against both Staphylococcus aureus and Escherichia coli upon light irradiation. Crucially, we propose and elucidate a novel antimicrobial enhancement mechanism mediated by the orderly-arranged LDH NS for BBR. This mechanism involves (i) promoting BBR molecular aggregation to enhance reactive oxygen species (ROS) generation, and (ii) improving bacterial capture capacity via electrostatic interactions. These effects collectively establish a synergistic “capture–ROS enrichment–bacterial killing” pathway on the film surface. In a practical application, the composite film effectively suppressed microbial growth on packaged bread, extending its shelf life by more than 4-fold compared to conventional packaging. This work not only presents a promising multifunctional material for food preservation but also provides fundamental insights into the design of nanomaterial-enhanced, natural photosensitizer-based systems for advanced active packaging.

CAS / MDL: 2086-83-1
✓ 已验证 产品关联 DOI PubMed 高影响因子
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CARBOHYDRATE POLYMERS · 2025 · IF 12.5

Exploring the masking of berberine bitterness by natural polysaccharides based on a “net-hook” dual-effect mechanism

Min Qiu,Jiaxin Li,Huijuan Xie,Jiamin Feng,Qi Huang,Yin Tian,Haozhou Huang,Li Han,Dingkun Zhang

Bitterness masking is a crucial technical hurdle in the development and application of oral liquid medicines. Small-molecule excipients, such as cyclodextrin, often provide insufficient bitterness masking, thus prompting the exploration of large-molecule excipients, especially polysaccharides. In this study, the bitterness-masking effects of 10 polysaccharides were assessed using berberine as a model. Only iota-carrageenan significantly reduced the bitterness of berberine, decreasing it from strong to slight. A comparative study of the bitterness-masking mechanisms of three polysaccharides revealed that carrageenan polymer chains formed an interwoven network, decreasing the release of berberine by 40 %. Moreover, -OSO₃ − groups on the polymer chains exhibited strong electrostatic interactions with the N + in berberine, significantly reducing the electron cloud density of N + . This combined effect traps berberine within the “net-hook” structure of the iota-carrageenan, markedly weakening the activation of bitter receptors by the berberine. Ultrasonic treatment-induced disruption of the iota-carrageenan network structure yielded a 29 % reduction in bitterness-masking efficacy, while carrageenan with a lower -OSO₃ − content achieved a 40 % reduction in efficacy. In conclusion, the “net-hook” structure of natural polysaccharides is a necessary condition for them to exert a bitterness-masking effect. This finding provides a scientific basis for expanding the applications of natural polysaccharides in taste-masking.

CAS / MDL: 83512-85-0
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

Antifungal chitosan-based lipoic acid/berberine sulfate composite film for suppressing Penicillium italicum and preserving mandarin fruit

Lihao Lei,LinFeng Yang,Lan Li,Shuangli Zhang,Shuai Wu,Rongyu Li,Xianhui Yin,Yue Ma,Zhuo Chen

Postharvest losses, specifically due to Penicillium italicum disease, pose a significant challenge to the mandarin industry. To enhance mandarin preservation efficacy, this study developed a chitosan (CS)-based berberine sulfate/alpha-lipoic acid composite film (CS@BS/ALA) and evaluated its effects on mandarin preservation. Among the various concentrations, 4 % CS demonstrated optimal wettability and adhesion. Incorporating BS/ALA into CS formed a dense double-network structure that reduced oxygen permeability. CS@BS/ALA treatment effectively inhibited weight loss, delayed fruit softening, maintained gloss, and preserved the brix acid ratio. It also enhanced antioxidant capacity by reducing malondialdehyde (MDA) content and sustaining superoxide dismutase (SOD) and phenylalanine ammonia-lyase (PAL) activities. Furthermore, antimicrobial tests revealed pronounced inhibitory effects of CS@BS/ALA against Penicillium italicum . These findings indicate that CS@BS/ALA extends mandarin shelf life by regulating respiratory metabolism, enhancing antioxidant defenses, and suppressing microbial infection, thereby providing an innovative solution for reducing postharvest losses.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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Journal of Biomedical Nanotechnology · 2019 ·Vol. 15 ·期 7 ·1432-1442 · IF 0

Programmable Release of Berberine Chloride Hydrate from Shape Memory Fibers Prepared from Core-Sheath Wet-Spinning Technology

Tang Jiamin,Zhao Ruifang,Yin Xueqian,Wen Ya,Shi Yidong,Zhu Puxin,Chen Zheng,Zeng Rong,Tan Lin

Smart wet-spun fibers for highly programmable release of therapeutic drug have been rarely reported. Herein, thermalresponsive composite fibers were successfully prepared by core-sheath wet-spinning technology in present study. They consisted of a model drug of natural antibacterial berberine chloride hydrate (BCH) and a drug carrier of temperature responsive shape memory polyurethane (SMPU). The obtained composite fibers featured with well-controlled microscopic morphologies, exhibiting significantly enhanced thermal stability and superb mechanical properties. In vitro drug release test and corresponding release kinetics study were performed for investigation of BCH's release behavior. Results demonstrated that the release behaviors of BCH from the core-sheath fibers were pH-dependent, influenced by both diffusion from pore channels and the solubility of BCH in the release mediums, and BCH imbedded only in core part showed a longer release period compared with that in both core and sheath parts of the composite fibers. More importantly, the release rate of BCH can be simply controlled by changing the initial shapes of fibers through stretching and fixation of the stretched deformations. Furthermore, the antibacterial durability of the smart composites fibers was demonstrated and tracked according to the growth inhibition against both negative E. coli and positive S. aureus bacteria strains. All these results suggest that the developed composite fibers can be promising candidates as smart drug delivery vehicles for highly adjustable doses of target drugs towards practical applications.

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