Frontiers in Pharmacology
·
2024
·
IF 4.4
Wang Yun,Li Zhongrui,Li Renshi,Han Chao,Wang Lei
Tumors are still a major threat to people worldwide. Nanodrug delivery and targeting systems can significantly improve the therapeutic efficacy of chemotherapeutic drugs for antitumor purposes. However, many nanocarriers are likely to exhibit drawbacks such as a complex preparation process, limited drug-loading capacity, untargeted drug release, and toxicity associated with nanocarriers. Therefore, new therapeutic alternatives are urgently needed to develop antitumor drugs. Natural products with abundant scaffold diversity and structural complexity, which are derived from medicinal plants, are important sources of new antitumor drugs. Here, two carrier-free berberine (BBR)-based nanoparticles (NPs) were established to increase the synergistic efficacy of tumor treatment. BBR can interact with glycyrrhetinic acid (GA) and artesunate (ART) to self-assemble BBR-GA and BBR-ART NPs without any nanocarriers, respectively, the formation of which is dominated by electrostatic and hydrophobic interactions. Moreover, BBR-GA NPs could lead to mitochondria-mediated cell apoptosis by regulating mitochondrial fission and dysfunction, while BBR-ART NPs induced ferroptosis in tumor cells. BBR-based NPs have been demonstrated to possess significant tumor targeting and enhanced antitumor properties compared with those of simple monomer mixes both in vitro and in vivo. These carrier-free self-assemblies based on natural products provide a strategy for synergistic drug delivery and thus offer broad prospects for developing enhanced antitumor drugs.
研究领域:
药学
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纳米技术
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肿瘤学
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天然产物化学
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DOI
PubMed
高影响因子
Drug Design Development and Therapy
·
2015
·
IF 3.028
Meng Yan,Kaiping Zhang,Yanhui Shi,Lifang Feng,Lin Lv,Baoxin Li
Berberine (BBR), an isoquinoline alkaloid mainly isolated from plants of Berberidaceae family, is extensively used to treat gastrointestinal infections in clinics. It has been reported that BBR can block human ether-a-go-go-related gene ( hERG ) potassium channel and inhibit its membrane expression. The hERG channel plays crucial role in cardiac repolarization and is the target of diverse proarrhythmic drugs. Dysfunction of hERG channel can cause long QT syndrome. However, the regulatory mechanisms of BBR effects on hERG at cell membrane level remain unknown. This study was designed to investigate in detail how BBR decreased hERG expression on cell surface and further explore its pharmacological rescue strategies. In this study, BBR decreases caveolin-1 expression in a concentration-dependent manner in human embryonic kidney 293 (HEK293) cells stably expressing hERG channel. Knocking down the basal expression of caveolin-1 alleviates BBR-induced hERG reduction. In addition, we found that aromatic tyrosine (Tyr652) and phenylalanine (Phe656) in S6 domain mediate the long-term effect of BBR on hERG by using mutation techniques. Considering both our previous and present work, we propose that BBR reduces hERG membrane stability with multiple mechanisms. Furthermore, we found that fexofenadine and resveratrol shorten action potential duration prolongated by BBR, thus having the potential effects of alleviating the cardiotoxicity of BBR.
研究领域:
药理学
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心脏病学
·
分子生物学
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DOI
PubMed
高影响因子
Chemical Biology & Drug Design
·
2026
·Vol. 107
·期 3
·e70264
·
IF 3.3
Yichao Zhao,Qi Li,Huihui Zhu,Cheng Jiang,Min Chen,Xiaoling Ye,Shixuan Hou,Sihao Cui,Xinmei Huang,Mengshu Cao
Idiopathic pulmonary fibrosis (IPF) is a chronic, progressive fibrosing interstitial lung disease without any effective treatment. Berberine (BBR), a botanical alkaloid, possesses extensive biological activities and has significant therapeutic value in various diseases. However, the effect and potential mechanisms of BBR on pulmonary fibrosis remain elusive. In vivo, BBR was administered by gavage following intratracheal instillation of bleomycin (BLM) in a mouse model from Day 1 to Day 20. In vitro, Human Lung Fibroblast (HLF) and A549 cell lines were used to explore the effects of BBR on transforming growth factor β1 (TGF-β1) treated cells. Both cell lines were transfected with a lentivirus carrying TGF-β receptor 2 (TGFBR2) knockdown genes, and the autophagy inhibitor chloroquine (CQ) and PI3K inhibitor LY294002 were employed to investigate the underlying effects of BBR on TGF-β signaling and autophagy in pulmonary fibrosis. BBR administration attenuates pulmonary inflammation and fibrosis of BLM-induced mice in vivo. Analogously, BBR treatment significantly alleviates matrix collagen deposition and reduces the expression of fibrotic markers in TGF-β1-treated human lung fibroblasts (HLF) and alveolar epithelial cell (A549) in vitro. Mechanistically, we found that BBR downregulates the expression of TGFBR2 and suppresses TGF-β/Smad2/3 signaling in vivo and in vitro. Furthermore, BBR inhibits the activation of the PI3K/AKT/mTOR pathway and autophagy, then downregulates the expression of pro-fibrotic genes. The effect of BBR on pulmonary fibrosis was further verified using both TGF-β1-treated HLF and A549 cells with the addition of the inhibitors of PI3K, LY294002, and autophagy, CQ in vitro, respectively. Our study suggests that BBR can inhibit pulmonary fibrosis by down-regulating the expression of TGFBR2, attenuating TGF-β/Smad2/3 signal, and activating autophagy through phosphorylation of PI3K/AKT/mTOR.
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产品关联
DOI
PubMed
高影响因子
Chinese Journal of Natural Medicines
·
2018
·
IF 1.991
Ling YAO,Ling-Ling WU,Qian LI,Qin-Mei HU,Shu-Yuan ZHANG,Kang LIU,Jian-Qin JIANG
A series of berberine derivatives were synthesized by introducing substituted benzyl groups at C-9. All these synthesized compounds ( 4a – 4m ) were screened for their in vitro antibacterial activity against four Gram-positive bacteria and four Gram-negative bacteria and evaluated for their antifungal activity against three pathogenic fungal strains. All these compounds displayed good antibacterial and antifungal activities, compared to reference drugs including Ciprofloxacin and Fluconazole; Compounds 4f, 4g , and 4l showed the highest antibacterial and antifungal activities. Moreover, all the synthesized compounds were docked into topoisomerase II-DNA complex, which is a crucial drug target for the treatment of microbial infections. Docking results showed that H-bond, π-π stacked, π-cationic, and π-anionic interactions were responsible for the strong binding of the compounds with the target protein-DNA complex.
研究领域:
药理学
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药物化学
·
微生物学
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DOI
PubMed
高影响因子
OPTICS AND LASER TECHNOLOGY
·
2025
·
IF 5
Hongxin Zhang,Xue Zhou,Yanan Zhang,Xuegang Li,Yong Zhao
The development of sensitive and reusable sensors for berberine hydrochloride (BH) detection remains a challenge. To address this, this paper proposes a simple, label-free, reusable, and stable optical fiber sensor using molecular imprinting polymer (MIP) for quantitative detection of berberine hydrochloride. Using BH as a template, sodium 4-styrene sulfonate (SSS) as a functional monomer, a BH molecular imprinting optical fiber sensor (BH-SSS@CS-MIP/OFS) based on surface plasmon resonance was successfully constructed. The sensor’s performance was meticulously characterized using spectral analysis, high-resolution scanning electron microscopy. The research results show that the sensor can significantly enhance the ability of recognizing BH compared to the unimprinted sensor and is not interfered with by other antibiotics. It achieves a wide detection range of 0.5–1000 μM, with a detection limit as low as 0.47 μM, and follows the Langmuir isotherm model. BH-SSS@CS-MIP/OFS can be desorbed by sodium hydroxide for multiple uses without changing its performance. The sensing response of the same sensor to a standard solution was measured over a period of 14 days (at 0, 7, and 14 days). The relative standard deviation (RSD) was 2.3 %. The prepared sensor was used to detect BH in water samples and found that the recovery rate ranged from 98 % to 108 %. After a series of tests, the novel BH molecular imprinting sensor has been proven to be an effective tool for monitoring BH. The unique advantages of MIP-based sensors, such as repeatability, simplicity, and reusability, make it a promising method for berberine hydrochloride detection and can be extended to detect other antibiotic molecules.
研究领域:
分析化学
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生物传感器
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环境监测
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药物检测
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分子识别
·
光学传感
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产品关联
DOI
高影响因子
Acta Crystallographica Section B-Structural Science Crystal Engineering and Materials
·
2026
·Vol. 82
·期 2
·
IF 2.5
Liang J.-F.,Wang Y.-T.,Xie M.,Li D.
Single-crystal X-ray diffraction is one of the most reliable techniques for elucidating the molecular structures, while it requires high-quality single crystals. The crystalline mate (CM) strategy has recently emerged as an effective method to induce rapid and selective co-crystallization. Here, we demonstrate that this strategy can be reliably extended to ionic systems using the neutral trinuclear silver pyrazolate complex Ag3Pz3 as a crystallization mate. By regulating solvent polarity, two co-crystals of silver pyrazolate berberine hydrochloride Ag3Pz3·BCl, SF (sandwich form) and NSF (non-sandwiched form), were obtained. In SF, neutral Ag3Pz3 simultaneously engages the Cl− anion via π-acid/base contacts and the berberine cation through weak Ag⋯O coordination. Remarkably, SF can also be crystallized directly from crude Coptis chinensis extract without prior purification. In NSF, due to the influence from methanol or ethanol, Ag3Pz3 rearranges into a rare anionic Ag3Pz4 cluster that serves as the counterion to berberine. These results establish solvent polarity as a decisive factor governing CM-mediated co-crystal assembly and broaden the applicability of the crystalline-mate concept to ionic systems.
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DOI
PubMed
高影响因子
International Journal of Burns and Trauma
·
2022
·
IF 0
Zhenqiang Liu,Yanchao Liu,Ting Fang,Jianhua Xia,Ning Ma,Yanhong Wang
In recent years, the morbidity of infections in traumatic wounds has been on the increase. There are not many kinds of drugs for clinical treatment of infections, and their efficacy and safety are limited. Plant antimicrobial drugs are increasingly popular in mainstream medicine due to the challenges of traditional antibiotics abuse. Berberine has a scavenging effect on infections, however, berberine was restricted from using as a drug preparation with poor stability and bioavailability. Due to the low toxicity of nanoparticles, the green-synthetic, size-controlled approach of nanoparticles has been paid more attention. Therefore, based on the intermolecular disulfide bond network platform built earlier, we designed and developed a strategy to assemble molecular bovine serum albumin into large-sized nanostructures through the reconstructed intermolecular disulfide bond and hydrophobic interaction, and berberine with poor water solubility was encapsulated in it. Nanoassembly with bovine serum albumin increased biostability of berberine and significantly improved its activity against Staphylococcus Aureus ( S.aureus ) activity, which gives some new insights into the preparation and development of anti-infectives for Chinese medicine.
研究领域:
药学
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纳米技术
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传染病学
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产品关联
DOI
PubMed
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2019
·
IF 3.973
Hong-Yu Xu,Chang-Shun Liu,Chuan-Li Huang,Li Chen,Yu-Rong Zheng,Si-Hang Huang,Xiao-Ying Long
Berberine (BBR) is an important natural product with poor gastrointestinal behavior includes low permeability, P-glycoprotein efflux, and mass elimination in the intestine. The aim of this study was to develop a novel nanoemulsion (NE) to improve the hypoglycemic efficacy of BBR. NE was prepared and characterized by morphology and droplet size detection, stored stability, in vitro intestinal lipolysis and metabolism, Caco-2 cells transport, in situ single-pass intestinal perfusion, oral bioavailability in rats, and hypoglycemic efficacy in high-fat diet and streptozocin-induced mice. BBR-loaded NE exhibits small droplet size (30.56 ± 0.35 nm) and good stability. NE could remain intact after lipolysis and protect BBR against the intestinal metabolism mediated by CYP2D6 and CYP3A4. Cells transport and intestinal perfusion studies revealed that NE decreases the P-glycoprotein efflux of BBR by 2-fold and enhances its permeability by 5.5-fold. Consequently, NE increased the oral bioavailability of BBR in rats by 212.02%. Compared to BBR control, blood glucose level of diabetic mice by NE was decreased by 3-fold. This novel NE provides a promising carrier to improve the hypoglycemic efficacy of BBR by overcoming its gastrointestinal deficiency, which may offer a product for the therapy of diabetes.
研究领域:
药剂学
·
糖尿病治疗
·
药物递送系统
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产品关联
DOI
PubMed
高影响因子
BIOFACTORS
·
2021
·Vol. 47
·期 4
·587-599
·
IF 6.113
Ninghua Wu,Wu Liu,Jiawen Wang,Yanqi Han,Yu Ye,Xiufen Liu,Yuandong Yu,Qingjie Chen,Yongfen Bao,Chao Liu
IR (insulin resistance) in diabetic brain gave rise to the generation of toxic factor Aβ42 and axon collapse which were the marker of AD (Alzheimer's disease)-like lesions in the circumstance of diabetes mellitus. But the underling molecular mechanism was not clear. Chronic HGHI (high glucose and high insulin) exposure accelerates IR has been reported in type II diabetes models. Berberine has been shown to promising effect for IR in vitro and in vivo. This study demonstrates the protective effect and the underlying mechanism of berberine on HGHI-induced IR. HGHI-induced cells were used to mimic the hyperinsulinemia resulting in IR. Berberine was used to uncover the mechanisms for the treatment of hyperinsulinemia in IR model. Morris water maze (MWM), PET imaging, CCK8 assay, ELISA assay, glucose kits, microscopy, and western blot analysis were performed to evaluate the protective effects of berberine. Berberine-improved HGHI-induced IR was correlated with the increase of glucose application in neurons. Meanwhile, the expressions of Pi3K, as well as GLUT3, PKCε, and APP were downregulated in the model, while p-IRS Ser307 was upregulated compared with Normal group. Fortunately, these scenes were reversed by berberine administration. Furthermore, berberine decreased GSK3β Y216 expressions, inhibited the production of oligomer Aβ42 and extended neuronal axon. The monomeric berberine treatment improves IR that may be involved in glucose effective application, rectifying the related proteins of the aberrant insulin pathway. Additionally, it suppressed the generation of Aβ42 and ameliorated neuron axon damage. Finally, berberine improves DM (diabetes mellitus)-induced cognitive impairment.
研究领域:
药理学
·
神经科学
·
糖尿病学
·
分子生物学
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DOI
PubMed
高影响因子
JOURNAL OF FLUORESCENCE
·
2024
·
IF 2.6
Chen De Xing,Long Yun Fei
The copper nanoclusters (CuNCs) have been garnered significant attention owing to their low cost raw materials, outstanding optical properties, environmental friendliness and good biocompatibility. In this study, copper nanoclusters stabilized by Acid Chromic Blue K (ACBK-CuNCs) were synthesized. The optimal excitation wavelength of the synthesized ACBK-CuNCs is 344 nm and the optimal emission wavelength is 460 nm. Its fluorescence intensity can be retained for more than two weeks, which indicated that the antioxidant capacity of the synthesized ACBK-CuNCs is strong. It was noted that the fluorescence intensities of the synthesized ACBK-CuNCs significantly increased with the decrease of pH. There are good linear correlation between the fluorescence intensity ratio of the system to the fluorescence intensity of the original solution (F/F 0 ) and the pH of the medium. Based on this finding, a method for fluorescence analysis to detect the pH of solution was developed. Additionally, it was discovered that the fluorescence intensity of CuNCs could be quenched efficiently by Berberine hydrochloride (BH), and there is a favorable linear relationship between the change value of fluorescence intensity of CuNCs ((F 0 - F) / F 0 ) and the concentration of BH. This gave rise to the establishment of a fluorescence analysis method for determining the concentration of BH. Simultaneously, visual quantitative detection for BH and pH was achieved based on smartphones and colorimetric analysis software using ACBK-CuNCs as the fluorescent probes. Graphical
研究领域:
化学
·
生物医学工程
·
分析化学
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产品关联
DOI
PubMed
高影响因子
RSC Advances
·
2021
·Vol. 11
·期 29
·17611-17621
·
IF 3.361
Yanfei Liu,Shuo Long,Shanshan Zhang,Yifu Tan,Ting Wang,Yuwei Wu,Ting Jiang,Xiaoqin Liu,Dongming Peng,Zhenbao Liu
Although berberine (BBR) shows antioxidant activity, its activity is limited. We synthesized 9-O-benzoic acid berberine derivatives, and their antioxidant activities were screened via ABTS, DPPH, HOSC and FRAP assays. The para-position was modified with halogen elements on the benzoic acid ring, which led to an enhanced antioxidant activity and the substituent on the ortho-position was found to be better than the meta-position. Compounds 8p, 8c, 8d, 8i, 8j, 8l, and especially 8p showed significantly higher antioxidant activities, which could be attributed to the electronic donating groups. All the berberine derivatives possessed proper lipophilicities. In conclusion, compound 8p is a promising antioxidant candidate with remarkable elevated antioxidant activity and moderate lipophilicity.
研究领域:
药理学
·
有机化学
·
自由基生物学
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产品关联
DOI
PubMed
高影响因子
Frontiers in Pharmacology
·
2020
·
IF 4.225
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.
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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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）