EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
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2022
·
IF 5.589
Zhe Wang,Xin Chen,Duanxiu Li,Enhe Bai,Hailu Zhang,Yanwen Duan,Yong Huang
Co-amorphous technology is an emerging approach for pharmaceutical engineering of drugs and drug leads with improved physicochemical properties and bioavailability. Platensimycin (PTM) is a promising natural antibiotic lead that acts on bacterial fatty acid synthase and exhibits excellent antibacterial activity . Despite great strides to improve its poor pharmacokinetics by medicinal chemistry and nanotechnology, there are no convenient oral delivery systems developed. Here, a co-amorphous system of PTM and berberine chloride (BCL) was developed for oral delivery of PTM. Co-amorphous PTM-BCL was prepared by rotary vacuum evaporation method, and systematically characterized by powder X-ray diffraction, temperature modulated differential scanning calorimetry , Fourier transform infrared spectroscopy (FTIR), and X-ray photoelectron spectroscopy (XPS). Compared with PTM or BCL alone, the equilibrium solubility and dissolution rate of both of them in the co-amorphous systems decreased significantly, showing the characteristics of sustained release . The molecular interactions between PTM and BCL were mediated by strong charged-mediated hydrogen bonds , based on FTIR, XPS, and NMR-based techniques. The co-amorphous PTM-BCL system showed excellent physiochemical stability at room and elevated (40 °C) temperature under dry conditions. The combination of PTM and BCL showed increased killing of a clinical isolated methicillin-resistant Staphylococcus aureus strain in killing checkerboard assays. Finally, co-amorphous PTM-BCL exhibited 2- or 3-fold longer half-life in rats than that of crystalline and amorphous PTM upon oral administration, respectively. Our study suggests a rational approach to realize the full potential of potent antibiotic PTM, which may be conveniently adapted for engineering of other important pharmaceutics.
研究领域:
药学
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生物医学工程
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DOI
PubMed
高影响因子
BMC BIOLOGY
·
2024
·Vol. 22
·期 1
·1-17
·
IF 4.4
Yang Yuxuan,Li Wenqing,Sun Kaineng,Sun Siyu,Zhang Yong,Chen Lin,Ni Yangyue,Hou Min,Xu Zhipeng,Chen Lu,Ji Minjun
Background Inflammatory bowel disease (IBD), a persistent gastrointestinal disease, is featured with impaired gut immunity. Previous studies have demonstrated that tuft cells can regulate the intestinal type 2 immune response by activating downstream ILC2 and Th2 cells and repair gut barrier upon invasion of parasitic helminths, bacteria, protozoans, and enteritis through different chemo-sensing receptors, such as bitter taste receptors. Berberine is a widely used in the treatment of diarrhea in clinic, however the mechanism underlying this effect is not clear. In this study, we aim to explore the relationship between berberine and tuft cells in dextran sulfate sodium (DSS) -induced colitis.Results Our data showed that berberine significantly ameliorated DSS-induced colitis and regulating type 2 innate immune lymphocytes (ILC2) and Th2 immune cells via tuft cells in the gut. Furthermore, the effect of berberine on colitis was partially abolished by U73122, a bitter taste receptor inhibitor, suggesting that bitter taste signalling pathway played an important role in the effect of berberine on relieving colitis.Conclusion sBerberine ameliorates dextran sulfate sodium -induced colitis through tuft cells and bitter taste signalling. Our study reveals the unique pharmacological mechanisms of berberine in the context of colitis, laying the foundation for further clinical applications of this compound.
研究领域:
药理学
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免疫学
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胃肠病学
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DOI
PubMed
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2025
·
IF 4.9
Menglan Wang,Lewei Li,Lifang Tang,Zuowei Xiao,Hong Yang,Qian Luo,Shiyang Fu,Zehui Fan,Xiaojun Tao,Chunlian He,Xiong Wu
Chemoresistance remains a major barrier to the effective treatment of triple-negative breast cancer (TNBC). To enhance the targeting and chemosensitivity of paclitaxel (PTX) for TNBC treatment, we developed a dual-drug-loaded nanodelivery system (BBR@PTX NPs) using BI-PEG-PTX polymer as the carrier, with berberine (BBR) loaded at an optimal ratio (PTX:BBR =1:10) determined by synergistic toxicity assays. The BBR@PTX NPs in this study demonstrated loading efficiencies of 9.5% for PTX and 28.06% for BBR, with an average particle size of 130-150 nm and a uniform distribution. In in vitro cellular assays, BBR potentiates PTX, achieving synergistic anti-tumor efficacy. The BBR@PTX NP co-delivery system enhances bioavailability by evading macrophage phagocytosis and lysosomal capture. The ability to inhibit cell growth, metastasis, and induce apoptosis was significantly enhanced after the NPs were taken up by tumor cells. In vivo experiments demonstrated that the BBR@PTX NP nanomicellar system enhanced tumor targeting, anti-tumor activity, and biosafety compared to single-agent formulations. These findings establish an effective approach to develop high-performance, selective, and low-toxicity nanocellular aggregates for combined therapy of solid triple-negative breast cancer.
研究领域:
肿瘤学
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药剂学
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纳米医学
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DOI
高影响因子
JOURNAL OF BIOMATERIALS APPLICATIONS
·
2023
·
IF 2.9
Chen Chen,Maomei Xie,Yueling Yan,Yongyuan Li,Zhiyao Li,Tong Zhang,Zanyan Gao,Liyi Deng,Haixia Wang
In recent years, Ag nanoparticle (Ag NP)-loaded antibacterial dressings have attracted much attention in high-level medical dressings. However, the high cytotoxicity of Ag NP has always been a problem. In this paper, we examined the improvement of antibacterial activity of berberine hydrochloride (BBR) with Ag NP, the results showed that the combined use of BBR and Ag NP can effectively reduce the dosage of Ag NP while ensuring the inhibition of bacterial growth, thus an intermediate layer dressing containing combined drugs were prepared. At the same time, the top dressing of polyvinyl alcohol (PVA) solid film and the PVA bottom dressings with three kinds of leakage structures were prepared by 3D printing technology. Three kinds of PVA bottom dressings showed high quality consistency, and the greater the number of leak holes, the higher the porosity value of the dressing, while the swelling ratio value of the bottom layer dressing with three holes was the lowest. Finally, three types of BBR-Ag NP composite antibacterial dressings (3D-BBR-Ag NP) can be obtained by self-assembling of the top dressing, the intermediate layer dressing, and the bottom dressings with three kinds of leakage structures. The cumulative drug release results showed that dressing with more holes had a faster drug release rate compared to the other two ones with fewer leakage holes. Besides, five drug release kinetic models were used to investigate the cumulative BBR release profiles for three types of 3D-BBR-Ag NP. And the three types of composite dressings showed strong antibacterial activity after 6 h of cultivation with staphylococcus aureus. The study showed that the antibacterial activity of the self-assembled dressing prepared by combination of BBR with Ag NP can be improved, and the drug release rate of the hydrogel dressing can be flexibly controlled through 3D printing technology.
研究领域:
药学
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纳米技术
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生物医学工程
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DOI
PubMed
高影响因子
LUMINESCENCE
·
2019
·Vol. 34
·期 6
·558-562
·
IF 1.691
Mingwei Guo,Weijie Li,Yanan Sun,Huimin Xu,Yiling Fan,Liyan Ma,Kunlun Huang,Zhiyi Yao
In this study, a rapid method for the detection of berberine hydrochloride (BRH) was developed based on a water-soluble pyrenyl probe, 8-hydroxypyrene-1,3,6-trisulfonic acid (HPTS). This method features low cost, good selectivity, high sensitivity and a fast response. The sensing mechanism of this probe is attributed to the formation of a complex between HPTS and BRH induced by electrostatic interaction and π–π stacking. To the best of our knowledge, this is the first fluorescent sensor for BRH based on organic materials that has low cost and a visual response. The detection limit of this method was as low as 1.24 μM and the linear response range is 2–50 μM. This method also allowed rapid detection of BRH real samples.
研究领域:
分析化学
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药物分析
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有机化学
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DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACOLOGY
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2021
·
IF 4.432
Yuling Tong,Xu Zhao,Ruilin Wang,Ruisheng Li,Wenjun Zou,Yanling Zhao
The purpose of this study was to investigate the therapeutic effect of berberine (BBR) on chronic atrophic gastritis (CAG) and its potential mechanism. The effects of BBR on gastric histopathology , serum biochemical indexes and inflammatory factors in CAG rats were assessed. Moreover, plasma and urine metabolomics based on ultra high performance liquid chromatography-quadrupole-time-of-flight mass spectrometer (UHPLC-Q-TOF/MS) were used to identify potential metabolic markers and possible pathways of BBR in the treatment of CAG. The results showed that BBR could significantly improve the pathological characteristics of gastric tissue, alleviate the serum biochemical indexes and reduce the mRNA expression of nuclear factor-κB, tumor necrosis factor-α, Cyclooxygenase-2, monocyte chemoattractant protein-1, Interleukin-17A and I interferon-γ. The results of metabolomic analysis show that the therapeutic effect of BBR on CAG may be related to the regulation of 15 metabolic markers and 12 metabolic pathways, which may be the potential mechanism for the treatment of CAG. This study provides new insights for elucidating the mechanism of BBR improving CAG.
研究领域:
药理学
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胃肠病学
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代谢组学
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病理学
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DOI
PubMed
高影响因子
Food & Function
·
2021
·Vol. 12
·期 23
·12115-12126
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IF 5.396
Lele Yang,Jiliang Cao,Jinchao Wei,Jiagang Deng,Xiaotao Hou,Erwei Hao,Zhengcai Du,Liang Zou,Peng Li
The therapeutic targets of berberine for hepatocellular carcinoma (HCC) and its detailed mechanisms remain unexplored. Here, an integration of network pharmacology, proteomic, bioinformatic and in vitro biochemical approach was proposed to reveal therapeutic targets and pathways underlying the antiproliferative activity of berberine against HepG2 cells. Results indicated that berberine caused the cytotoxicity and inhibited the growth of HepG2 cells with IC50 values ranging from 92 μM to 118 μM. Network pharmacology analysis revealed that targeting apoptosis and cell cycle pathways by berberine contributed to its antitumor efficacy against HCC. Proteomic analysis demonstrated that mitochondria-related apoptosis pathways were involved in the cytotoxic action of berberine, as evidenced by the expression of mitochondrial dysfunction-mediated proteins. Moreover, a total of 160 significantly altered proteins were screened, among which AKAP12 presented significantly increased levels under berberine treatment. Bioinformatic analysis of various public datasets showed that expression of AKAP12 in HCC liver tissues was downregulated, emphasizing its role as a tumor suppressor. Immunoblotting validated the increased levels of AKAP12, while co-immunoprecipitation identified its interaction with Cyclin D1. These data, together with flow cytometry analysis, suggested that AKAP12 mediated cell cycle arrest, thereby suppressing cell proliferation. Altogether, the antiproliferative action of berberine in HepG2 cells involves both apoptosis and cell cycle arrest. Regulating AKAP12 signalling by berberine might provide a promising strategy for HCC treatment.
研究领域:
肿瘤学
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药理学
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生物信息学
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细胞生物学
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DOI
PubMed
高影响因子
eFood
·
2026
·Vol. 7
·期 4
·e70184
·
IF 5.7
Qing-Qing Dong,Si-Hui Wang,Chen-Yan Wang,Ke-Da Yang,Xiao-Ling Xu,Yi Shi,Wei Chen
Sepsis often progresses to multiorgan failure through intestinal barrier disruption and bacterial translocation. Berberine (BBR) has anti-inflammatory and intestinal protective activity, but its oral use is limited by poor solubility and low bioavailability (< 1%). Here, we designed BGNP@YM, an oral colon-targeted system in which BBR-loaded gelatin nanoparticles (BGNP) are encapsulated within yeast microcapsules (YM), and tested it in a lipopolysaccharide (LPS)-induced sepsis mouse model. BGNP@YM was stable in simulated gastric and intestinal fluids and released its payload in simulated colonic fluid, confirming colon-specific delivery. In vivo, BGNP@YM outperformed free BBR, BGNP, or YM alone, improving survival, attenuating weight loss and splenomegaly, and lowering TNF-α, IL-6, and IL-1β in colonic and renal tissues. Histology showed restored intestinal barrier integrity and reduced injury in multiple organs, with no detectable hepatic or renal toxicity. 16S rRNA sequencing further revealed partial reversal of sepsis-induced dysbiosis, with increased microbial diversity, a restored Firmicutes / Bacteroidetes ratio, and enrichment of short-chain fatty acid (SCFA)-producing taxa such as Odoribacter . The associated renal protection is consistent with a gut-kidney axis effect. These findings support BGNP@YM as a promising oral candidate for the treatment of sepsis-induced intestinal injury.
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DOI
高影响因子
Polymers
·
2026
·Vol. 18
·期 8
·908
·
IF 5.8
Xinyu Zhang,Chu Gong,Yujie Liu,Jun Wang,Zhizhou Yang,Jun-Li Yang
Biopolymer-based packaging films possess outstanding performances and are being developed as the alternatives to traditional petroleum-based plastic packaging films with many non-ignorable shortcomings. In this study, chitosan, succinylated pullulan (SP), and berberine (BBR) were combined to fabricate novel biopolymer-based composite films (CSSPB) via the layer-by-layer assembly method. The effects of the incorporation of BBR on the physicochemical properties of the film were investigated. It was found that after BBR was added, the tensile strength (TS), elongation at break (EAB), hydrophobicity, and antioxidant capacities of the film were enhanced. The chemical bonding, crystalline properties, elemental composition, and thermal stability of the films were also characterized by Fourier transform infrared (FT-IR) spectroscopy, X-ray diffraction (XRD), X-ray photoelectron spectroscopy (XPS), and thermogravimetric analysis (TGA), respectively. The in vitro antifungal tests revealed the antifungal activities of the films with a relatively high BBR content againstColletotrichum gloeosporioides(CG). In the preservation experiments, the CSSPB films exhibited preservation effects on fresh-cut apples, which manifested as delaying browning, weight loss, an increase in the soluble solids content, and a decrease in hardness. The new CSSPB composite films were opined to hold application potential in the field of food packaging.
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DOI
PubMed
高影响因子
JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY B-BIOLOGY
·
2026
·
IF 4
Yumeng Xie,Yujie Sun,Xin Li,Liang Zheng,Yuguang Wang,Chen Xu,Ludan Zhang,Bingran Yu,Lilei Zhu
Superficial mucosal and skin infections caused by Candida albicans remain a clinical burden because current antifungals rarely combine high potency with host safety. Here, we report berberine (BBR)–derived aggregation-induced emission (AIE) photosensitizers for photodynamic therapy (PDT), in which alkyl-chain length is tuned to modulate molecular amphiphilicity, nanoaggregation, and fungal selectivity. A series of cationic AIE derivatives (CABs) was constructed and evaluated for antifungal activity and biocompatibility. Upon 405 nm irradiation, CABs efficiently generated reactive oxygen species through both Type I and Type II photodynamic pathways, including HO• and 1 O₂. In vitro , the medium-chain derivative CAB-8 showed a favorable balance between uptake and cytocompatibility: under 405 nm irradiation, CAB-8 achieved nearly 99.9% fungicidal killing against C. albicans and outperformed fluconazole, while displaying preferential uptake by fungal over mammalian cells, consistent with reduced host phototoxicity. Transcriptomic profiling revealed a dual intrinsic antifungal mechanism under dark conditions, involving concomitant disruption of mitochondrial oxidative phosphorylation and ribosome-dependent protein synthesis. In vivo , CAB-8–mediated PDT enhanced fungal clearance and wound healing in a skin burn infection model and prevented C. albicans colonization in an oral mucosal infection model, without evidence of systemic toxicity. These findings establish alkyl-chain engineering of BBR-based AIE photosensitizers as an effective strategy to improve the efficacy–safety profile of PDT for localized treatment and prevention of superficial C. albicans infections.
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DOI
PubMed
高影响因子
BIOMATERIALS
·
2025
·
IF 12.9
Liqiang Gu,Xintao Sun,Jian Pan,Dongming Liu,Lilan Huang,Yaru Yu,Bing Yu,Hailin Cong
The antibacterial hydrogels have attracted a significant amount of interest for preventing bacterial infection in wound healing. However, irreversible antibiotic resistance and lagging detection of wound infection are still current research pain points for hydrogel wound dressings. This study successfully prepared and characterized a novel aggregation-induced PVA/SA/BBR hydrogel. BBR confers significant antibacterial potential to PVA/SA/BBR hydrogels avoiding the use of antibiotics. The results indicate that PVA/SA/BBR hydrogels displayed antibacterial activity against S. aureus , enhanced wound healing process, negligible cytotoxicity, and low hemolytic activity (< 5%). Molecular docking analysis indicate that BBR could inhibit the activity of FabH of E. coli and S. aureus , with a respective binding energy of -9.0185 and -8.4037 kcal/mol. Moreover, the real-time in situ monitoring and quantifying of wound pH levels could be realized by RGB signals collected and transformed from the visible-fluorescent images. PVA/SA/BBR hydrogels also provided significant fluorescent signals visible to the naked eye due to the AIE effect of BBR when the hydrogel severely loses water. All of these signals suggested anti-infective therapy and hydrogel replacement. Therefore, PVA/SA/BBR hydrogels as efficient non-antibiotic-dependent wound dressings with significant therapeutic effect on skin wounds provide potential applications in wound healing, flexible wearable sensing and drug delivery.
研究领域:
生物医学工程
·
材料科学
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感染与免疫
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
·
2025
·
IF 4.7
Guangqi Guo,Zhen Zhang,Xiaoyang Xia,Zhixiong He,Nanjie Jiang,Xiang Liu,Xia Xiang,Yanan Xue
Berberine (BBR) and oleanolic acid (OA) are natural bioactive compounds with recognized anti-inflammatory properties. However, their therapeutic potential is often limited due to poor solubility and low bioavailability. Different from the traditional polymeric or lipidic-encapsulation strategies, this study successfully prepared carrier-free co-assembly BBR-OA nanoparticles (B-O NPs) using a solvent exchange method, which could achieve higher payload. Under optimal conditions, BBR and OA self-assembled to form uniform spherical nanoparticles, with an average particle size of approximately 130 nm. B-O NPs were negatively charged with a zeta potential of -42.43 mV and demonstrated improved water solubility and stability compared to the BBR and OA alone. The self-assemble mechanism of BBR and OA was further elucidated by molecular dynamics simulations and molecular docking analysis, highlighting the role of electrostatic and hydrogen bonding interactions. In vitro studies revealed that B-O NPs displayed obvious pH responsiveness and sustained BBR release capabilities in simulated gastric fluid (pH 2.0) and physiological buffer (pH 7.4) when compared to free BBR. Cellular experiments revealed that B-O NPs had enhanced cellular uptake and transmembrane transport ability. Moreover, in a lipopolysaccharide (LPS)-stimulated inflammatory model of RAW 264.7 macrophages, B-O NPs effectively reduced the intracellular reactive oxygen species (ROS) and downregulated the inflammatory mediators, including NO, TNF-α, IL-1β, and IL-6, showing significantly higher anti-inflammatory activity than free BBR, OA, or their physical mixture. These findings suggested that B-O NPs may provide a promising approach to improve the bioavailability and biological activity of small natural molecules.
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DOI
高影响因子
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