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Berberine
Frontiers in Pharmacology · 2020 · IF 4.225

Berberine-Incorporated Shape Memory Fiber Applied as a Novel Surgical Suture

Zhou Wen-cheng,Tan Peng-fei,Chen Xing-han,Cen Ying,You Chao,Tan Lin,Li Hao,Tian Meng

The surgical suture has long been used to reconnect the injured tissues to restore their structure and function. However, its utility remains challenging in many areas, such as surgical site infections and minimally invasive surgeries. Herein, we report a novel surgical suture that possesses both antibacterial activity and shape memory effect to address these issues. In detail, natural antibacterial berberine was incorporated directly into the spinning solution of shape memory polyurethane with a near body transition temperature, and then berberine-containing polyurethane (BP) fibers were prepared by a facile one-step wet-spinning method for surgical suture. The prepared BP fibers were micro-sized and characterized by their transition temperature, morphology, water contact angles, mechanical properties, in vitro shape memory effect, drug release, and antibacterial activity. The results showed that with the increasing amount of the incorporated berberine, the transition temperatures of the fibers were not significantly affected, remains at near body temperature, while the contact angles of the fibers were significantly decreased and the mechanical properties of the fibers were significantly weakened. The optimized fiber was selected to evaluate the cytotoxicity and in vivo biocompatibility before in vivo shape memory effect and wound healing capacity in a mouse skin suture–wound model was tested. Besides the shape memory effect, it was demonstrated that the fiber is capable of antibacterial activity and anti-inflammatory effect, and promoting wound healing. The mechanism of the antibacterial activity and anti-inflammatory effect of the fiber was discussed. Overall, it is expected that by the berberine added to the fiber for surgical suture, it will be more popular and extend the utility of the sutures in a wide range of clinical applications.

CAS / MDL: 633-65-8
研究领域: 材料科学 · 生物医学工程 · 外科手术 · 药剂学
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International Journal of Nanomedicine · 2023 · IF 8

Berberine-Loaded Nanostructured Lipid Carriers Enhance the Treatment of Ulcerative Colitis

Jianping Deng,Zicong Wu,Zhenling Zhao,Chaoxi Wu,Min Yuan,Zhengquan Su,Yifei Wang,Zhiping Wang

Purpose Berberine (BBR), a major ingredient extracted from Coptis chinensis, is a natural drug with limited oral bioavailability. We developed nanostructured lipid carriers (NLCs) as a delivery system for enhanced anti-inflammatory activity of BBR against ulcerative colitis (UC).Methods BBR-loaded nanostructured lipid carriers (BBR-NLCs) prepared via high-pressure homogenization were evaluated for particle size, zeta potential, drug entrapment efficiency, drug loading, drug release, toxicity, and cellular uptake. The anti-UC activities of free and encapsulated BBR were evaluated in a DSS-induced acute model of UC in mice.Results Spherical BBR-NLCs were prepared with a particle size of 63.96± 0.31 nm, a zeta potential of +3.16 ± 0.05 mV, an entrapment efficiency of 101.97±6.34%, and a drug loading of 6.00±0.09%. BBR-NLCs showed excellent biocompatibility in vivo. Cellular uptake experiments showed that BBR-NLCs improved uptake of BBR by RAW 264.7 cells and Caco-2 cells. Oral administration of BBR-NLCs significantly alleviated colitis symptoms (DAI, colon length, spleen swelling, MPO activity) through inhibition of NF-κB nuclear translocation, decreased expression of pro-inflammatory cytokines (IL-1β, IL-6, MMP-9, CX3CR1, COX-2, TERT), and increased expression of the tight junction protein ZO-1.Conclusion BBR-loaded NLCs improved colitis symptoms, which suggested that this may be a novel formulation for treatment of UC.

CAS / MDL: 8001-25-0
研究领域: 药剂学 · 药理学 · 胃肠病学 · 纳米技术
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Polymers · 2024 ·Vol. 16 ·期 16 ·2368 · IF 4.7

Oral Administration of Berberine Hydrochloride Based on Chitosan/Carboxymethyl-β-Cyclodextrin Hydrogel

Bukatuka Futila Clemence,Lin Xiao,Guang Yang

In this study, a novel oral formulation of berberine hydrochloride (BBH) hydrogel was successfully synthesized through physical cross-linking using chitosan (CS) and carboxymethyl-β-cyclodextrin (CMCD). The characterization results confirmed the successful synthesis of the CS/CMCD hydrogel and the subsequent loading of BBH into this composite (CS/CMCD/BBH) was effectively accomplished. The BBH was used as a model drug and the resulting hydrogel demonstrated a sustained drug release profile. In addition to its improved solubility and sustained release characteristics, the hydrogel exhibited excellent antibacterial activity against common pathogens such asEscherichia coli(E. coli),Staphylococcus aureus(S. aureus), andCandida albicans(C. albicans). Additionally, in vitro studies indicated that the hydrogel was not cytotoxic to NIH3T3 and HaCaT cells, suggesting its safety for biomedical applications. This lack of cytotoxic effects, combined with the mechanical strength, solubility improvements, and antibacterial properties of the hydrogel, positions the CS/CMCD/BBH hydrogel as a promising candidate for the effective oral delivery of BBH. By addressing the solubility and delivery challenges of BBH, this hydrogel offers a viable solution for the oral administration of BBH, with potential applications in various biomedical fields.

CAS / MDL: 64-19-7 9012-76-4
研究领域: 药剂学 · 生物材料学 · 微生物学
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Advanced Science · 2024 · IF 14.3

Berberine Protects against Hepatocellular Carcinoma Progression by Regulating Intrahepatic T Cell Heterogeneity

Jiaxiang Hu,Qingmiao Shi,Chen Xue,Qingqing Wang

Accumulating evidence suggests that berberine (BBR) exhibits anti-cancer effects in hepatocellular carcinoma (HCC). However, the mechanisms by which BBR regulates the immunological microenvironment in HCC has not been fully elucidated. In this study, a mouse model of orthotopic HCC is established and treated with varying doses of BBR. BBR showed effectiveness in reducing tumor burden in mice with HCC. Cytometry by time-of-flight depicted the alterations in the tumor immune landscape following BBR treatment, revealing the enhancement in the T lymphocytes effector function. In particular, BBR decreased the proportion of TCRb hi PD-1 hi CD69 + CD27 + effector CD8 + T lymphocytes and increased the proportion of Ly6C hi TCRb + CD69 + CD27 + CD62L + central memory CD8 + T lymphocytes. Single-cell RNA sequencing further elucidates the effects of BBR on transcriptional profiles of liver immune cells and confirms the phenotypical heterogeneity of T lymphocytes in HCC immune microenvironment. Additionally, it is found that BBR potentially regulated the antitumor immunity in HCC by modulating the receptor-ligand interaction among immune cells mediated by cytokines. In summary, the findings improve the understanding of BBR's impact on protecting against HCC, emphasizing BBR's role in regulating intrahepatic T cell heterogeneity. BBR has the potential to be a promising therapeutic strategy to hinder the advancement of HCC.

CAS / MDL: 67-68-5
研究领域: 肿瘤学 · 免疫学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF COLLOID AND INTERFACE SCIENCE · 2024 · IF 9.4

Exosomes derived from mesenchymal stem cells containing berberine for ulcerative colitis therapy

Chao Deng,Huanxiao Zhang,Yuxuan Li,Xinyi Cheng,Youyi Liu,Shubing Huang,Jianqing Cheng,Hui Chen,Ping Shao,Bing Jiang,Xianwen Wang,Kewei Wang

Berberine (Ber), an isoquinoline alkaloid, is a potential drug therapy for ulcerative colitis (UC) because of its anti-inflammatory activity, high biological safety, and few side effects. Nevertheless, its clinical application is hindered by its limited water solubility and low bioavailability. Currently, compared to synthetic nanocarriers, exosomes as carriers possess advantages such as low toxicity, high stability, and high specificity. Human placental mesenchymal stem cell-derived exosomes (HplMSC-Exos) have emerged as a promising drug delivery system, offering intrinsic anti-inflammatory and antioxidant activities. Therefore, we engineered MSC-Exos loaded with Ber (Exos-Ber) to enhance the solubility and bioavailability of Ber and for colon targeting, revealing a novel approach for treating UC with natural compounds. Structurally and functionally, Exos-Ber closely resembled unmodified Exos. Both in vitro and in vivo investigations confirmed the antioxidant and anti-inflammatory properties of Exos-Ber. Notably, Exos-Ber exhibited reparative effects on injured epithelial cells and reduced cellular apoptosis. Furthermore, Exos-Ber concurrently demonstrated anti-inflammatory and antioxidant activities, contributing to the mitigation of UC, possibly through its modulation of the MAPK signaling pathway. Overall, our findings demonstrate the potential of Exos-Ber as a promising therapeutic option for alleviating UC, highlighting its capacity to enhance the clinical applicability of Ber.

研究领域: 药理学 · 干细胞研究 · 胃肠病学 · 药物递送系统
✓ 已验证 DOI PubMed 高影响因子
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Journal of Biomedical Nanotechnology · 2018 ·Vol. 14 ·期 8 ·1486-1495 · IF 5.068

Berberine Hydrochloride-Loaded Chitosan Nanoparticles Effectively Targets and Suppresses Human Nasopharyngeal Carcinoma

Wang Yonghong,Wen Baofang,Yu Hongli,Ding Dejun,Zhang JingJing,Zhang Yunxiang,Zhao Limin,Zhang Weifen

Nasopharyngeal carcinoma (NPC) is a common epithelial malignancy that occurs in the nasopharynx and it is one of the high incidences of malignant tumors in China. As previous reports, berberine hydrochloride (BH) possesses a repressive effect on the proliferation of various cancer types. But the application of BH was hampered for a long time due to its hydrophobic properties, along with poor stability and bioavailability. In this study, folate acid modified chitosan nanoparticles loaded berberine hydrochloride (BH/FA-CTS NPs) were prepared by the ionic cross-linking technique, the physicochemical properties and the influence of BH/FA-CTS NPs on proliferation, migration and apoptosis in human nasopharyngeal carcinoma CNE-1 cells were studied in vitro and in vivo. Results of scanning electron microscopy (SEM) images showed that BH/FA-CTS NPs were sphere and the diameter was 258.2±9.1 nm. The drug loading and encapsulation efficiency were 8.17±1.12% and 87.73±4.21%, respectively. The drug release kinetics exhibited a slower and sustained release over a period of 48 h. Moreover, results of MTT assay and scratch assay displayed that BH/FA-CTS NPs inhibited proliferation and migration of CNE-1 cells remarkably. BH/FA-CTS NPs promoted apoptosis and necrosis of CNE-1 cells. And BH/FA-CTS NPs displayed distinguished higher tumor inhibition than control group, free BH and BH/CTS NPs in vivo. Therefore, as a nanocomposite, BH/FA-CTS NPs provide a new method and option for the treatment of nasopharyngeal carcinoma patients.

研究领域: 肿瘤学 · 药剂学 · 生物医学工程
✓ 已验证 DOI PubMed 高影响因子
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International Journal of Analytical Chemistry · 2020 ·Vol. 2020 ·期 1 ·8892696 · IF 1.678

A Validated Liquid Chromatographic Method for Berberine Analysis in Tissue and Application

Neng Zhou,Dangmei Liu,Xiaowang Bao

Simple and rapid high-performance liquid chromatography methods were developed for the determination of berberine (BB) in various rat tissues so as to evaluate a P-gp inhibitor, glycyrrhetinic acid (GA), on BB’s oral bioavailability. Acetonitrile was used to extract BB from tissues and showed different extraction recoveries in diverse tissues. The intra- and interday precision and accuracy were less than 10%. Long-term stability, pre (post) -preparative stability, and freeze-thaw stability were evaluated, and the results showed it could meet the need of this study. The proposed methods were subsequently applied to investigate the possible drug-drug interaction of GA and BB in vivo from the aspect of tissue distribution. The results showed that no significant difference was found between the group of low dose and high dose at the same time point. The tissue distributions show a saturated model, i.e., the content of BB in tissue tends to be constant while its dose is more than 200 mg/kg. Besides, the contents of BB ranged from high to low according to the order of the liver, kidney, and spleen. The BB content in the liver is especially high as compared to other tissues.

研究领域: 药理学 · 分析化学
✓ 已验证 DOI 高影响因子
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Anti-Cancer Agents in Medicinal Chemistry · 2018 ·Vol. 18 ·期 11 ·1639-1648 · IF 2.556

Synthesis and Anticancer Activity of 9-O-Pyrazole Alkyl Substituted Berberine Derivatives

Xiao Daipeng,He Fen,Peng Dongming,Zou Min,Peng Junying,Liu Pan,Liu Yanfei,Liu Zhenbao

Background: Berberine (BBR), an isoquinoline plant alkaloid isolated from plants such as Coptis chinensis and Hydrastis canadensis, own multiple pharmacological activities. Objective: In this study, seven BBR derivatives were synthesized and their anticancer activity against HeLa cervical and A549 human lung cancer cell lines were evaluated in vitro. Methods: The anti-cancer activity was measured by MTT assay, and apoptosis was demonstrated by the annexin V-FITC/PI staining assay. The intracellular oxidative stress was investigated through DCFH-DA assay. The molecular docking study was carried out in molecular operating environment (MOE). Results: Compound B3 and B5 showed enhanced anti-cancer activity compared with BBR, the IC50 for compound B3 and B5 were significantly lower than BBR, and compound B3 at the concentration of 64 or 128 μM induced apoptosis in HeLa and A549 cell lines. The reactive oxygen species (ROS) was generated in both cell lines when treated with 100 μM of all the compounds, and compound B3 and B5 induced higher activity in the generation of ROS, while compound B3 exhibited the highest activity, these results are in accordance with the cytotoxicity results, indicating the cytotoxicity were mostly generated from the oxidative stress. In addition, molecular docking analysis showed that compound B3 had the greatest affinity with Hsp90. Upon binding, the protective function of Hsp90 was lost, which might explain its higher cytotoxicity from molecular interaction aspect. Conclusion: All the results demonstrated that compound B3 and B5 showed significantly higher anti-cancer ability than BBR, and compound B3 is a promising anticancer drug candidate.

研究领域: 药理学 · 肿瘤学 · 化学 · 分子生物学
✓ 已验证 DOI PubMed 高影响因子
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Nanotechnology Reviews · 2020 ·Vol. 9 ·期 1 ·568-579 · IF 3.639

Berberine/Ag nanoparticle embedded biomimetic calcium phosphate scaffolds for enhancing antibacterial function

Cheng Hu,Lina Wu,Changchun Zhou,Huan Sun,Peng Gao,Xiujuan Xu,Chenxi Zhang,Jie Liang,Yujiang Fan,Jianxun Sun,Xuedong Zhou,Xingdong Zhang

In the past decade, biomimetic calcium phosphate (CaP) ceramics have been considered as practicable grafts and biomaterial substitutes in repairing jaw bone defect after tumor resection or traffic accident. Nowadays, increasing incidence of biomedical material-associated infection has raised a concern when applying these materials. In this work, a new porous CaP scaffold with antibacterial coating was proposed. This biomimetic scaffold was composited with berberine (BBR), Ag nanoparticles (nAg), and silk fibroin (SF). The microstructures and phase composition of the scaffolds were analyzed. The cytocompatibility and osteogenic potential of the prepared samples were evaluated in vitro . The scaffolds held hierarchical structure: the first-level porous CaP ceramic with micron pores ranged from 250 to 600 µm; the second-level spongy-like structure with abundant capillary pores ranged from 500 nm to 10 µm; and the third-level structure was achieved by filling BBR, nAg, and SF gel coatings into the above porous structures. The experimental results showed that the antimicrobial capability of single BBR coating is inconspicuous. However, the introduction of nAg could significantly promote the antibacterial effect of scaffolds. At the same time, such scaffolds showed improved osteoinductivity. This new biomimetic CaP scaffold with antibacterial and osteoinductive properties may be a promising candidate for bone tissue engineering.

研究领域: 生物医学工程 · 材料科学 · 组织工程 · 生物材料
✓ 已验证 DOI 高影响因子
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JOURNAL OF COLLOID AND INTERFACE SCIENCE · 2024 · IF 9.4

Interfacial interaction mechanism between Mn doped highly conjugated biochar and berberine hydrochloride

Jiangmei Zhao,Cheng Ji,Chong Peng,Yuanfei Wang,Shuyi Yang,Yun Li,E. Tao

MnSO 4 -modified biochar (Mn-BC) was synthesized to remove berberine hydrochloride (BH) from wastewater by utilizing tea waste as raw material and MnSO 4 as modifier. Brunel Emmett Taylor (BET) analysis reveals that the specific surface area (SSA) and average pore size (D ave ) of Mn-BC are 1.4 and 7 times higher than those of pristine biochar apart, attributing to the dissociation effect can promote the dispersion of MnSO 4 in the pores of the biochar. Meanwhile, the doping of Mn not only introduces additional oxygen-containing functional groups (OCFGs), but also modulates the π electron density. Furthermore, Response surface method (RSM) analysis reveals that Mn-BC dosage has the most significant effect on BH removal, followed by BH concentration and pH value. Kinetic and isothermal studies reveal that the BH adsorption process of Mn-BC was mainly dominated by chemical and monolayer adsorption. Meanwhile, density functional theory (DFT) calculations confirm the contribution of Mn doping to the conjugation effect in the adsorption system. Originally proposed Mn-BC is one potentially propitious material to eliminate BH from wastewater, meanwhile this also provides a newfangled conception over the sustainable utilization of tea waste resources.

CAS / MDL: 10034-96-5
研究领域: 环境科学 · 材料科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF NANOBIOTECHNOLOGY · 2026 · IF 15

An oral berberine nanocapsule platform orchestrates microbiota for potent gastric cancer chemotherapy

Shuai Gong,Yuxiang Zhang,Wei Du,Chong Zhang,Nai Wu,Xiuzhong Zhang,Zeqiang Ren,Yi Zhang,Pengbo Zhang,Chenyue Zhan,Xiaoyu Wu

Systemic chemotherapy for gastric cancer is frequently compromised by debilitating, dose-dependent toxicities, necessitating innovative adjunctive strategies that balance therapeutic efficacy with systemic safety. While natural products represent a promising source of candidates, their clinical translation is frequently hindered by intrinsic pharmacokinetic barriers. To address this, we developed the oral resident binary intestinal therapy (ORBIT) system, an excipient-free nanocapsule platform engineered for prolonged gut residency. Unlike conventional pharmaceutical formulations that depend on synthetic excipients, ORBIT is an excipient-free, self-assembled nanocapsule composed of a high-density dopamine-functionalized hyaluronic acid (hDAHA) shell encapsulating a berberine (BBR) core. This unique architecture provides a protective shield for BBR against premature degradation while utilizing the adhesive properties of the hDAHA shell to enhance gastrointestinal retention. ORBIT enables sustained, pH-responsive drug release, providing robust in situ shielding of the intestinal mucosa against oxaliplatin-induced injury and preserving epithelial barrier integrity. In preclinical gastric cancer models, the ORBIT regimen synergistically potentiates oxaliplatin-mediated tumor suppression while dramatically ameliorating systemic toxicity. Mechanistically, ORBIT administration profoundly remodels the microbiome-immune axis, specifically enriching beneficial commensals such as Akkermansia to drive increased intratumoral infiltration of CD8⁺ T cells. This study establishes a new oral nanotherapeutic paradigm for chemo-immunotherapy, presenting a compelling and clinically translatable strategy to optimize gastric cancer treatment outcomes.

✓ 已验证 DOI PubMed 高影响因子
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LUMINESCENCE · 2026 ·Vol. 41 ·期 3 ·e70462 · IF 2.8

Preparation of PVP-Cys CuNCs and Its Application in Determination of Berberine

Rui Tian,Yuhui Yang,Duo Li,Jiamin Chai,Rui Zhang,Hua Yang,Haoyu Li,Xuehua Sun

Polyvinylpyrrolidone (PVP) and cysteine (Cys) double-ligand–modified copper nanoclusters (PVP-Cys CuNCs) were synthesized by a one-pot method. The addition of Cys can protect copper nanoclusters (CuNCs) more effectively and enhance its fluorescence intensity, compared with the single-ligand-modified PVP CuNCs; the double-ligand-modified PVP-Cys CuNCs showed higher fluorescence intensity and sensing ability. Based on the internal filtration and dynamic quenching effect of berberine (BBR) on PVP-Cys CuNCs, a novel, simple, and sensitive method for BBR detection has been established. This method exhibits a good linear response to BBR within the linear range of 1.09 × 10 −7 –4.26 × 10 −6 mol · L −1 , and with a limit of detection (LOD) of 3.67 × 10 −8 mol · L −1 . It has been successfully applied to the determination of BBR in practical pharmaceutical samples.

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