INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2021
·Vol. 22
·期 21
·11466
·
IF 5.924
Miaomiao Qi,Xiang Liu,Ying Zhou,Haoyu Wang,Ying Zhao,Jing Ren,Jin Xiang
G protein-coupled estrogen receptor 1 (GPER1) is a potential therapeutic target for treating triple-negative breast cancers (TNBC). However, modulators for GPER1 that can be used to treat TNBC have not appeared. Berberine (BBR) is a bioactive isoquinoline alkaloid with high oral safety. In recent years, BBR has shown an inhibitory effect on TNBC tumors such as MDA-MB-231, but the molecular target remains unclear, which hinders related clinical research. Our work proved that BBR is a modulator of GPER1 that can inhibit cell viability, migration, and autophagy of MDA-MB-231 cells. The inhibitory effect of BBR on MDA-MB-231 cells has a dependence on estrogen levels. Although BBR promoted the proteasome, which is a major factor in the degradation of GPER1, it could still induce the protein level of GPER1. Correspondingly, the transcription of cellular communication network factor 2 (CCN2) was promoted. BBR could bind to GPER1 directly and change the secondary structure of GPER1, as in the case of 17β-estradiol (E2). In addition, BBR induced not only a high degree of co-localization of GPER1 and microtubule-associated protein 1 light chain 3 (MAP1LC3), but also the accumulation of sequestosome 1 (SQSTM1/p62) by the inhibition of the nuclear translocation of the nuclear factor-kappa B (NF-κB) subunit (RELA/p65), which indicates NF-κB inhibition and anti-cancer effects. This result proved that the promotional effect of BBR on the GPER1/NF-κB pathway was closely related to its inhibitory effect on autophagy, which may serve as a new mechanism by which to explain the inhibitory effect of BBR on MDA-MB-231 cells and expand our understanding of the function of both BBR and GPER1.Keywords:berberine;binding;co-localization;GPER1;MAP1LC3;NF-κB
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高影响因子
NEUROIMMUNOMODULATION
·
2021
·Vol. 29
·期 4
·317-326
·
IF 2.492
Wu Xiuwen,Liu Xiaopeng,Yang Liang,Wang Yuanyu
Background: Elevation of AMP-activated protein kinase (AMPK)/peroxisome proliferator-activated receptor-γ coactivator-1α (PGC1α) signaling can suppress intracerebral hemorrhage (ICH)-induced neurological impairments. As an isoquinoline alkaloid, Berberine exerts neuroprotective effects in neurological disease models with activated AMPK/PGC1α signaling. Aim: We aim to study the effect of Berberine on ICH-induced brain injury and explore the potential molecular mechanism. Methods: ICH model was established in mice through intracerebral injection of autologous whole blood, followed by treatment with Berberine. Neurological impairments were assessed by the modified neurological severity score and behavioral assays. Brain edema and blood-brain barrier (BBB) integrity were assessed by water content in the brain, amount of extravasated Evans blue, and BBB tight junction components. Neuroinflammatory responses were assessed by inflammatory cytokine levels. AMPK/PGC1α signaling was examined by AMPK mRNA expression and phosphorylated AMPK and PGC1α protein levels. Results: Berberine (200 mg/kg) attenuated ICH-induced neurological deficits, motor and cognitive impairment, and BBB disruption. Berberine also suppressed ICH-induced inflammatory responses indicated by reduced production of inflammatory cytokines. Finally, Berberine drastically elevated AMPK/PGC1α signaling in the hemisphere of ICH mice. Conclusion: Our findings suggest that Berberine plays an important neuroprotective role against ICH-induced neurological impairments and BBB injury, probably by inhibition of inflammation and activation of AMPK/PGC1α signaling
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JOURNAL OF THE ELECTROCHEMICAL SOCIETY
·
2021
·Vol. 168
·期 5
·056523
·
IF 4.316
Xiansen He,Xiaokun Li,Suxiang Feng,Xueying Li,Cuijie Nong
In this study, a novel photoelectrochemical (PEC) sensor based on FeMoSe2 was developed for the detection of berberine hydrochloride (BRH). The photosensitive material Fe-doped MoSe2 (FeMoSe2) was prepared by a simple hydrothermal method. Compared with MoSe2, FeMoSe2 shows superior PEC performance for the sensitive detection of BRH under blue light. Under the best experimental conditions, the PEC sensor presented a wide detection range of 0.025–15.0 μM with a detection limit of 8.4 nM. Therefore, the PEC sensor is considered an effective analytical method for detecting BRH. Moreover, the PEC sensor has good reporducibility and stability. Eventually, the proposed sensor was successfully applied to detect two different types of BRH tablets. This project provides a new pathway for detecting BRH.
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CHEMICAL ENGINEERING JOURNAL
·
2020
·
IF 10.652
Yan-Yan Xie,Yan-Wen Zhang,Xiao-Zhi Liu,Xiao-Fang Ma,Xiao-Tong Qin,Shi-Ru Jia,Cheng Zhong
Bacterial infections are a great threat to public health. The development of materials which prevent biofilm formation, and exhibit antibacterial properties, but are otherwise biocompatible, is a major research goal. In this study, a novel hybrid hydrogel with aggregation-induced emission (AIE) behavior was prepared through the self-assembly of commercial N -(9-fluorenylmethoxycarbonyl)- L -phenylalanine (Fmoc-F) and berberine chloride (BBR). BBR self-assembled into nanoparticles which dispersed throughout the gel network, and endowed the hydrogel with AIE functionality. Fmoc-F/BBR hydrogel displayed enhanced antibacterial and anti-biofilm activity against both Gram-negative ( Escherichia coli ) and Gram-positive ( Staphylococcus aureus ) bacteria when used as the active agent in the photodynamic therapy (PDT) process. Additionally, negligible cytotoxicity and low hemolytic activity were displayed. In vivo infection studies showed that Fmoc-F/BBR hydrogel facilitated the repair of wounds in rats infected with S. aureus . Therefore, Fmoc-F/BBR hydrogel provides potential applications in biomedicines, and especially in wound healing.
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ACS Applied Materials & Interfaces
·
2021
·
IF 9.229
Zeqi Zhao,Zhengzhong Han,Konduru Naveena,Guanxiong Lei,Shiwei Qiu,Xuanyi Li,Ting Li,Xi Shi,Wei Zhuang,Yalan Li,Yuehua Qiao,Hongmei Liu
Overproduction of reactive oxygen species (ROS) and inflammation are two key pathogeneses of noise-induced hearing loss (NIHL), which leads to outer hair cell (OHC) damage and hearing loss. In this work, we successfully developed ROS-responsive nanoparticles as berberine (BBR) carriers (PL-PPS/BBR) for OHC-targeted therapy of NIHL: Prestin-targeting peptide 2 (PrTP2)-modified nanoparticles (PL-PPS/BBR), which effectively accumulated in OHC areas, and poly(propylene sulfide)120 (PPS120), which scavenged ROS and converted to poly(propylene sulfoxide)120 in a ROS environment to disintegrate and provoke the rapid release of BBR with anti-inflammatory and antioxidant effects. In this study, satisfactory anti-inflammatory and antioxidant effects of PL-PPS/BBR were confirmed. Immunofluorescence and scanning electron microscopy (SEM) images showed that PL-PPS/BBR effectively accumulated in OHCs and protected the morphological integrity of OHCs. The auditory brainstem response (ABR) results demonstrated that PL-PPS/BBR significantly improved hearing in NIHL guinea pigs after noise exposure. This work suggested that PL-PPS/BBR may be a new potential treatment for noise-associated injury with clinical application.
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高影响因子
PHARMACEUTICAL BIOLOGY
·
2020
·
IF 2.971
Yucheng Li,Baoying Wang,Jiduo Shen,Ming Bai,Erping Xu
Context Berberine is an alkaloid that possesses various pharmacologic effects.Objective To explore the mechanism of berberine to improve insulin sensitivity in fructose-fed mice.Materials and methods Sixty male ICR mice were randomly divided into 6 groups (10 mice in each group): control, fructose, pioglitazone (10 mg/kg) and berberine (50, 100, and 200 mg/kg). Except for the control group, the mice received 20% fructose drinking for 10 weeks. Pioglitazone and berberine were orally administered once daily during the last 4 weeks. The insulin sensitivity was evaluated using an oral glucose tolerance test (OGTT). The serum levels of fasting glucose and insulin, blood lipids, and hormones were determined. The hepatic AMP and ATP contents were detected using high performance liquid chromatography (HPLC) analysis, and the protein expression was examined by immunoblotting.Results Berberine significantly reversed the insulin resistance induced by fructose, including lowering fasting insulin levels (from 113.9 to 67.4) and area under the curve (AUC) during OGTT (from 1310 to 1073), decreasing serum leptin (from 0.28 to 0.13) and increasing serum adiponectin levels (from 1.50 to 2.80). Moreover, berberine enhanced the phosphorylation levels of protein kinase B (PKB/AKT; 2.27-fold) and glycogen synthase kinase-3β (GSK3β; 2.56-fold), and increased hepatic glycogen content (from 0.19 to 1.65). Furthermore, berberine upregulated the protein expression of peroxisome proliferator activated receptor gamma coactivator 1α (PGC1α; 2.61-fold), phospho-AMP-activated protein kinase (p-AMPK; 1.35-fold) and phospho-liver kinase B1 (p-LKB1; 1.41-fold), whereas it decreased the AMP/ATP ratio (from 4.25 to 1.82).Conclusion The present study demonstrated the protective effects of berberine against insulin resistance induced by fructose. Our findings may provide an experimental basis for the application of berberine in the treatment of insulin resistance.
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Materials Science & Engineering C-Materials for Biological Applications
·
2019
·
IF 4.959
Xueqian Yin,Pengfei Tan,Hao Luo,Jianwu Lan,Yidong Shi,Yong Zhang,Haojun Fan,Lin Tan
Nanofibrous drug delivery systems (DDSs) recently have attracted remarkable interest, especially their potential to program dosage of the encased drug intelligently. Despite this, the exploration of efficient strategy to precisely program drug release from nanofibrous DDS still remains a significant challenge. In this study, we electrospun a near-body temperature (T trans ≈ 42 °C) sensitive shape memory polyurethane in three stages through sequential electrospinning technology, and prepared a sort of sandwich structural membrane, comprising of top, inner and bottom layers, wherein a natural antibacterial agent, berberine hydrochloride (BCH), was imbedded inside the middle layer. As demonstrated by the results obtained from tensile testing and morphology characterization, the prepared sandwich structural membrane and the nanofibrous membrane with homogenous structure exhibited not only desirable mechanical properties but also surface morphologies. In addition, the release period can be significantly prolonged in virtue of the sandwich structure. As revealed by the experiment of in vitro drug release, it took nearly 144 h to release 80 wt% BCH from sandwich structural membrane, while as little as 72 h was observed to release the same amount of BCH from that with homogenous structure. More interestingly, the encapsulated BCH is capable to be released in a controlled manner owning to the thermo-sensitive shape memory effect, and the release rate of BCH can be accelerated by stretching and fixing the nanofibrous membranes into certain ratios prior to release. Collectively, this study provides a facile strategy to design and prepare a reliable and smart DDS, i.e. sandwich structural membrane, which may enhance the availability of BCH and also intelligently avoid the bacterial infection.
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ACS Sustainable Chemistry & Engineering
·
2026
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IF 7.6
Zhang Hongli,Guo Yan,Li Ning,Ma Sumeng,Zhao Fanrong,Wang Kai,Jing Xu,Han Jiajun
The development of deep eutectic solvents (DESs) that can be readily and sustainably recycled is expected to reduce costs and enhance the environmental friendliness of extracting plant-derived active ingredients. Here, a novel temperature-responsive DES prepared from propylene carbonate and n -butanol was employed as the extractant for ultrasound-assisted extraction of berberine from Coptis chinensis Franch. The prepared temperature-responsive DES did not require the addition of acids, bases, or salts. Phase separation between DES and water was achieved under mild conditions simply by adjusting the temperature. At 45 ° C, DES and water formed a single phase and were used for berberine extraction. Upon decreasing the temperature to 25 ° C, the DES phase separated from the aqueous phase, enabling recovery of DES and berberine. The relatively low critical solution temperature (45 ° C) of DES enabled mild extraction conditions, minimizing the thermal degradation of active components. The recovered DES was reused for subsequent extractions; after five cycles, the yield showed no decrease, while berberine recovery remained above 80%. Moreover, the biological activity of the berberine extract was assessed, revealing its efficacy in suppressing the lipopolysaccharide-induced inflammatory response in RAW264.7 cells and inhibiting the proliferation of gastric cancer cells. Furthermore, network pharmacology analysis suggested that berberine may exert antigastric cancer activity by regulating the cell cycle. Overall, this study presents a green and sustainable strategy for berberine extraction and provides a promising basis for its potential application in gastric cancer therapy.
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JOURNAL OF SEPARATION SCIENCE
·
2026
·Vol. 49
·期 9
·e70514
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IF 3.6
Xingyun Zhao,Zhenwei Zhang,Junjie Zhang,Zhiqin Qin,Lijuan Yan,Xiaojing Yang,Weidong Wu,Liyun Zhang,Rongfang Wu
An anionic covalent organic framework (COF) was constructed using 2,5-diaminobenzenesulfonic acid as an ionic building unit. The incorporation of sulfonate functionalities endows the framework with permanent anionic sites, thereby enabling selective ion-exchange interactions with cationic species. The adsorption performance toward berberine hydrochloride (BBH) was systematically investigated by optimizing pH, ionic strength, adsorbent dosage, extraction time, and elution conditions. Rapid adsorption equilibrium was achieved within 10 min, and the kinetic data were well described by a pseudo-second-order model, indicating a chemisorption-dominated process. Under optimal conditions (pH 11, 303 K), the maximum adsorption capacity reached 1082.4 mg g −1 . The material maintained high adsorption efficiency in the presence of competing cations, demonstrating pronounced selectivity arising from electrostatic interactions. Moreover, it retained over 90% of its initial adsorption capacity after five adsorption–desorption cycles, confirming its structural stability and recyclability. These results highlight the effectiveness of introducing ionic functionalities into COF architectures to achieve high-capacity and selective adsorption of alkaloid compounds, providing a viable platform for the separation and analysis of BBH in complex herbal matrices. The design and synthesis of novel COF porous adsorption materials will play a crucial role in the separation and analysis of natural products.
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JOURNAL OF MEDICINAL CHEMISTRY
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2020
·
IF 6.205
Xiaojia Shi,Tao Zhang,Hongxiang Lou,Huina Song,Changhao Li,Peihong Fan
Mitochondrion is a favorable therapeutic target in cancer, given its regulation of bioenergetics and cell death. Honokiol exhibits antiproliferative effects through mitochondria-mediated death signaling. To enhance its anticancer potential and selectivity, we conjugated honokiol to berberine, a mitochondria-targeting carrier. All designed derivatives displayed 1 order of magnitude increased cytotoxicity compared with the parent compounds, especially with massive cytoplasmic vacuoles. Biological evaluation demonstrated the representative compound 6b localized within the mitochondria, and mitochondrial dilation resulted in vacuolization. 6b induced vacuolation-associated cell death and apoptosis with obvious mitochondrial dysfunction, as demonstrated by booming reactive oxygen species generation, opening mitochondrial permeability transition pore, and reducing mitochondrial membrane potential. The targeting property also conferred 6b with selectivity for tumor cells compared to normal cells. 6b inhibited cancer cell proliferation in the zebrafish xenograft model. These results demonstrate that berberine-linked honokiol derivatives open up a direction for novel mitochondrial-targeting antitumor agents.
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INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2023
·Vol. 24
·期 22
·16286
·
IF 5.6
Zhengbo Hu,Kai Zhao,Xingcan Chen,Mingyuan Zhou,Yuchi Chen,Xiaoqing Ye,Fangmei Zhou,Zhishan Ding,Bingqi Zhu
The healing process of a diabetic wound (DW) is often impeded by a series of interrelated factors, including severe infection, persistent inflammation, and excessive oxidative stress. Therefore, it is particularly crucial to develop a medical dressing that can address these issues simultaneously. To this end, different ratios ofBletilla striatapolysaccharide (BSP) and berberine (BER) were physically blended with Carbomer 940 (CBM940) to develop a composite hydrogel as a medical dressing. The BSP/BER hydrogel was characterized using SEM, FTIR, rheological testing and other techniques. The anti-inflammatory, antioxidant, and antibacterial properties of the hydrogel were evaluated using cell and bacterial models in vitro. A DW model of ICR mice was established to evaluate the effect of the hydrogel on DW healing in vivo. The hydrogel exhibited excellent biocompatibility and remarkable antibacterial, anti-inflammatory, and antioxidant properties. In addition, animal experiments showed that the BSP/BER hydrogel significantly accelerated wound healing in DW mice. Among the different formulations, the LBSP/BER hydrogel (2% BSP, mBER:mBSP= 1:40) demonstrated the most remarkable efficacy. In conclusion, the BSP/BER hydrogel developed exhibited immense properties and great potential as a medical dressing for the repair of DW, addressing a crucial need in clinical practice.Keywords:diabetic wound;Bletilla striatapolysaccharide;berberine;hydrogel
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BIOMEDICINE & PHARMACOTHERAPY
·
2023
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IF 7.5
Xiongjie Sun,Yu Zhang,Gang Cheng,Tianxiang Zhu,Zhigang Zhang,Lei Xiong,Haiming Hu,Hongtao Liu
Ulcerative colitis (UC) has been confirmed as a disease with a high incidence and low cure rate worldwide. In severe cases, UC can develop into colon cancer. Modern research has confirmed that berberine (BBR) can treat UC by inhibiting the expressions of inflammatory factors. However, the contribution of gut microbiota and flora metabolites in treating UC with BBR remains unclear. In this study, the ameliorative effects of BBR on gut microbiota dysbiosis and flora metabolites were investigated in a dextran sodium sulfate (DSS)-induced UC rodent model. We found that BBR significantly improved the pathological phenotype, attenuated intestinal barrier disruption, and mitigated colonic inflammation in DSS mice. By 16 S rDNA sequencing, BBR alleviated gut microbiota dysbiosis in UC mice. Moreover, the gut microbiota depletion experiment confirmed that the therapeutic effect of BBR was inextricably correlated with the gut microbiota. Besides, the flora metabolites ( e.g. , short-chain fatty acids, bile acids, and 5-hydroxytryptamine) were studied using HPLC-MS. The results suggested that BBR ameliorated the bile acid imbalance induced by DSS in the liver and gut. Furthermore, BBR treatment repaired gut barrier damage. The above results revealed that BBR alleviated DSS-induced UC in mice by restoring the disturbed gut microbiota, elevating unconjugated and secondary bile acids in the gastrointestinal tract, and activating the FXR and TGR5 signal pathway. This study provides novel insights into the mechanism of BBR in treating UC.
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