Biomedical Optics Express
·
2019
·Vol. 10
·期 4
·1581-1600
·
IF 3.91
Ping Tang,Wendai Cheng,Xuanmeng He,Qinnan Zhang,Jing Zhong,Xiaoxu Lu,Shengde Liu,Liyun Zhong
Berberine (BBR), a traditional Chinese herb extract medicine, reveals some anticancer effects in leukemia, but it remains controversial about the molecular mechanism of BBR-induced leukemia cell apoptosis. In this study, combining Raman spectrum and spectral imaging, both the biochemical changes of BBR-induced Jurkat cell apoptosis and the precise distribution of BBR in single cell are presented. In contrast, we also show the corresponding results of Jatrorrhizine (JTZ) and Palmatine (PMT), two structural analogues of BBR. It is found that all three structural analogues can induce cell apoptosis by breaking DNA and the main action sites are located in phosphate backbone and base pair groups, but their action on cell cycle are different, in which BBR leads to the S phase arrest while JTZ and PMT are on the G2 phase arrest. Moreover, from the Raman spectra of DNA treated with different drugs, we find that the content of phosphate backbone and base pair groups in BBR-treated DNA are larger than those in JTZ or PMT. And this result reflects the strong capability of BBR breaking DNA backbone relative to JTZ or PMT, suggesting that the existence of methylene-dioxy on the 2, 3 units of A ring on the quinoline ring can greatly enhance the capability of BBR breaking DNA backbone, so the action effect of BBR-induced Jurkat cell apoptosis is better than those of PMT or JTZ. Further, by using Raman spectral imaging approach, we achieve the precise distribution of BBR in single cell, it is found that the receptor-mediated BBR targeting delivery based single-wall carbon nanotube and folic acid (SWNT/FA) reveals excellent performance in BBR targeting delivery relative to the conventional BBR diffusion approach. Importantly, these results demonstrate that Raman spectrum and spectral imaging should be a powerful tool to study the molecular mechanism of drug-induced cell apoptosis and evaluate the efficiency of drug delivery system.
研究领域:
生物医学
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药理学
·
分子生物学
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DOI
PubMed
高影响因子
MOLECULAR PHARMACEUTICS
·
2018
·
IF 4.556
Yi Feng,Ning-xi Li,Huan-li Yin,Tian-yu Chen,Qian Yang,Min Wu
Evodiamine (EVO) and Berberine (BBR), from Euodiae Fructus and Coptidis rhizoma, have been used as an herbal medicine pair in traditional Chinese medicine to exert synergistic antitumor effects against various types of tumor cells. However, their clinical use is limited by their poor solubility and adverse toxic side effects. Mesoporous silica nanoparticles (MSNs) possess excellent properties such as a readily functionalized surface, prominent biocompatibility, and huge specific surface area for loading with hydrophobic and hydrophilic drug. On this basis, a novel temperature- and pH-responsive dual drug delivery platform has been developed, in which lipid-coated MSN@p(NIPAM-co-MA) codelivers EVO and BBR. The results indicate that the nanocarrier improves the efficacy and biocompatibility of the drug pair and maintain desirable drug profiles at the low pH and higher temperature of the tumor microenvironment. The dual drug-loaded MSNs showed excellent synergistic therapy effects in vitro (cytotoxicity, cell migration and invasion, angiogenesis) and in vivo (growth of tumor grafts in mice). Meanwhile, the dual drug-loaded nanoparticles showed lower systemic toxicity than either drug alone, the free drug combination, or Taxol. These results suggest that the temperature- and pH-sensitive lipid-coated MSNs are a promising novel carrier for both hydrophobic and hydrophilic drugs.
研究领域:
药理学
·
纳米技术
·
肿瘤学
·
中医药
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产品关联
DOI
PubMed
高影响因子
BIOFOULING
·
2026
·
IF 2.5
Ming Lu,Ze Yao,Chunshuang Li,Xiang Li,Hui Shang,Songtao Bie
Berberine, a naturally occurring isoquinoline alkaloid, has demonstrated strong antibiofilm properties against Staphylococcus aureus. However, the molecular mechanisms underlying this activity remain poorly understood. Here, we report that berberine effectively inhibits S. aureus biofilm formation with a minimum biofilm inhibitory concentration (MBIC) of 32 µg ml–1. XTT assays demonstrated a marked reduction in biofilm metabolic activity, while high-content screening (HCS) combined with three-dimensional reconstruction revealed significant decreases in biofilm biomass and thickness. Mechanistically, berberine selectively suppressed the production of key extracellular polymeric substance (EPS) components, particularly polysaccharide intercellular adhesin (PIA) and proteins, without significantly affecting extracellular DNA (eDNA) levels. Transcriptomic profiling integrated with protein–protein interaction (PPI) network modeling suggested that srrA, a response regulator within the two-component system, may serve as a central hub gene downregulated by berberine. Quantitative PCR (qPCR) further corroborated the altered expression of srrA and associated genes (walR, atpB, luxS, icaR). Collectively, these findings provide mechanistic insights into berberine’s antibiofilm activity and point to srrA-mediated EPS regulation as a candidate pathway warranting further investigation.
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DOI
PubMed
高影响因子
JOURNAL OF PHARMACY AND PHARMACOLOGY
·
2013
·Vol. 65
·期 5
·734-744
·
IF 2.033
Chen Da-Peng,Xiong Yong-Jian,Lv Bo-Chao,Liu Fang-Fei,Wang Li,Tang Ze-Yao,Lin Yuan
ObjectivesThe aim of the study was to evaluate berberine-induced bidirectional regulation on the contractility of jejunum.MethodsDifferent low and high contractile states of isolated jejunal segment from rat were established to investigate the effects of berberine.Key findingsStimulatory effects on jejunal segment were exerted by berberine in six low contractile states and inhibitory effects were produced on jejunal segment in six high contractile states. The effects of berberine on myosin light chain kinase (MLCK) mRNA expression, MLCK protein content, and myosin phosphorylation in jejunum were also bidirectional. Bidirectional regulation was not observed in the presence of tetrodotoxin. No regulatory effects of berberine on jejunal contractility were observed in the presence of verapamil. The stimulatory effects of berberine on jejunal contractility were blocked by atropine. The inhibitory effects of berberine on jejunal contractility were abolished by phentolamine, propranolol and L-NG-nitro-arginine, respectively.ConclusionsBerberine-induced bidirectional regulation needed the presence of the enteric nervous system, and depended on the influx of extracellular Ca2+, related to the cholinergic system while jejunum was in low contractile states, and related to the adrenergic system and nitric oxide relaxing mechanism while jejunum was in high contractile states. The results suggested the potential clinical implication of berberine for alternating-type irritable bowel syndrome.
研究领域:
药理学
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胃肠病学
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神经科学
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DOI
PubMed
高影响因子
ARCHIVES OF GYNECOLOGY AND OBSTETRICS
·
2022
·Vol. 306
·期 1
·115-125
·
IF 2.493
Zhu Bo,Chen Yumei,Guo Min,zhang Chenhui,Huang Lingxiao,Pan Qiangwei,Lin Tao,Lu Yiyi,Shen Xiaolu,Zhang Hongping
Purpose Adenomyosis is a common gynecological disease, but its pathogenesis and treatment options are not yet completely clear. This study aimed to investigate the analgesic effect of berberine on tamoxifen-induced neonatal mouse adenomyosis and its curative effects on the disease. Methods The mouse adenomyosis model was established in neonatal female mice via oral administration of tamoxifen suspended solution. Adenomyosis mice were given berberine by intraperitoneal injection with the dosage of 5, 10, and 20 mg/kg body weight, respectively, at 17 weeks after birth. The pain sensation of the mice was evaluated by hotplate and tail-flick tests. The mRNA levels of gene expression were detected by RT-qPCR. The protein expression was analyzed by ELISA and Western blot. Results Berberine reduced the uterine weight, suppressed the myometrial infiltration of ectopic endometrium, improved the hotplate and tail-flick latency of the adenomyosis mice. Mechanistically, berberine downregulated the expression of genes related to pain and inflammation, such as TRPV1, COX-2, VEGF and OTR, impaired the inflammatory response at the DRG site, and inhibited the expression of TLR4 in DRG and uterine tissues. Conclusions Berberine attenuates hyperalgesia and exhibits analgesic and therapeutic effects on adenomyosis mice.
研究领域:
药理学
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妇科学
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疼痛研究
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炎症
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF IMMUNOLOGY
·
2022
·Vol. 208
·期 10
·2309-2318
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IF 5.426
Li Min,Zhang Haifeng,Zhang Yameng,Fan Jinting,Zhu Jinhao,Gu Xinyue,Li Zhonghui,Zhang Chengyang,Liu Zhen,Li Yuebai,Zang Mingxi,Jin Ge,Li Guoping,Mi Yang
Classical activation of macrophage and monocyte differentiation induced by β-glucan is accompanied with metabolic change in glucose. However, the role of the metabolic rewiring in monocyte/macrophage activation remains elusive. In this study, we show that berberine induces aerobic glycolysis by blocking the tricarboxylic acid cycle and modulates cytokine responses in bone marrow–derived macrophages (BMDMs) from mice and human PBMC. 13-Methyberberine had activities on glucose metabolism and BMDM activation similar to those of berberine, whereas other tested derivatives lost both activities. Glucose transporter (GLUT)1 expression and total cellular hexokinase activity increased gradually in BMDMs in the presence of berberine. In the contrast, LPS upregulated GLUT1 and 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) levels in 6 h. Extracellular glucose levels and replacing glucose with galactose in culture medium affected the cytokine secretion of BMDMs. Berberine alleviated enteritis of Salmonella typhimurium infection and protected mice against endotoxic shock. In mice i.p. injected with LPS, the increase of serum TNF-α and the drop of blood glucose were attenuated by berberine treatment. These data together demonstrated that macrophage activation was closely related with glucose metabolism.
研究领域:
免疫学
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药理学
·
代谢
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产品关联
DOI
PubMed
高影响因子
AATCC Journal of Research
·
2022
·
IF 0.726
Jiliang Cao,Chunli Meng,Hong Zhao
The natural cationic colorant berberine was used to dye cationic dyeable polyester (CDP) fibers. Its dyeing properties, namely color strength (K/S) of dyed CDP and percent exhaustion (E%) of berberine, on CDP were explored at various dyeing pH levels, temperatures, time, and concentration of berberine. Furthermore, dyeing kinetic and thermodynamic studies were also carried out to evaluate the adsorption properties and mechanism. It was found that the E% of berberine on CDP fibers and the rate of adsorption increased with increasing dyeing temperature, while the influence of pH was extraordinarily small. In addition, the adsorption isotherm of berberine on CDP fibers was in line with the Langmuir model.
研究领域:
材料科学
·
染料化学
·
纺织工程
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DOI
高影响因子
MOLECULES
·
2026
·Vol. 31
·期 4
·621
·
IF 5.1
Ying Zhao,Yubo Lu,Yushan Ma,Sijia Wang,Pin Lv,Huifang Xu,Yuanyuan Li,Weisheng Feng
Breast cancer ranks among the most prevalent malignant tumors globally, underscoring the urgent need for efficient and low-toxicity treatment strategies. In this study, a novel nanomedicine (BBR-SA) was constructed based on the self-assembled of berberine (BBR) and sinapic acid (SA) for synergistic chemotherapy. Firstly, utilizing π-π stacking, hydrogen bonding, and electrostatic forces between BBR and SA, the BBR-SA achieved a well-defined nanostructure with high drug-loading capacity and favorable water dispersibility. Furthermore, BBR-SA nanomedicine effectively inhibited the proliferation of mouse mammary carcinoma cells (4T1), showing a significantly stronger inhibitory effect than either BBR or SA alone. Moreover, the remarkable anti-tumor effect was obtained after treatment with BBR-SA nanomedicine in vivo, further demonstrating a synergistic therapeutic effect. More importantly, no significant systemic toxicity was observed after 28 days of intravenous administration with BBR-SA nanomedicine. In summary, the BBR-SA nanomedicine represents a safe and effective therapeutic strategy for breast cancer, offering new perspectives on the application of the traditional chinese medicine in anti-tumor therapy.
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产品关联
DOI
PubMed
高影响因子
Materials Letters-X
·
2021
·
IF 0
Mei Qin,Daqing Liu,Xin Meng,Zhang Dai,Shufang Zhu,Na Wang,Xu Yan
At the beginning of 2020, the whole world suffered from the new coronavirus (COVID-19). Wearing a mask was believed to reduce the spread of the virus. The core material of a mask required good air permeability and efficient filtration. Electrospun materials may match these requirements. By electrospinning, we prepared polyvinyl butyral (PVB)/berberine hydrochloride (BH) membranes onto the spunbonded nonwovens. The composite meshes showed porous structures, good air permeability (164 ± 16 mm/s) and air filtration efficiency 96.4% for PM 0.3, 100% for PM 2.5, with pressure drop (108 Pa). Moreover, with the addition of BH, the as-spun membranes showed good antibacterial property for staphylococcus aureus. Furthermore, the prepared PVB/berberine membranes had good hydrophobicity with water contact angle higher than 140°. These results indicated that the fabricated PVB/berberine membranes have potential applications in mask and air filtration.
研究领域:
材料科学
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生物医学工程
·
环境科学
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DOI
ACTA PHARMACOLOGICA SINICA
·
2020
·Vol. 42
·期 7
·1190-1194
·
IF 5.064
Shen Zhu-qing,Wang Juan,Tan Wen-fu,Huang Tao-min
Hedgehog plays an important role in a wide range of physiological and pathological conditions. Paracrine activation of Hedgehog pathway in stromal cells increases the expression of VEGF, which promotes neovascularization in colorectal cancer and ultimately the growth of colorectal cancer. Berberine (BBR) has anticancer activity. In this study we investigated whether BBR inhibited the growth of colon cancer through suppressing the paracrine sonic hedgehog (SHH) signaling in vitro and in vivo. We showed that BBR (1–10 μM) dose-dependently inhibited the secretion and expression of SHH protein in HT-29 and SW480 cells. BBR did not influence the transcription of SHH, but promoted the degradation of SHH mRNA, thus decreased the SHH mRNA expression in the colorectal cancer cells. In nude mice bearing HT-29 xenograft, oral administration of BBR (100 mg · kg − 1 · d −1 ) or a positive control drug GDC-0449 (100 mg · kg −1 · d −1 ) for 4 weeks markedly suppressed the growth of HT-29 tumor with BBR exhibiting a better antitumor efficacy. The tumor growth inhibition caused by BBR or GDC-0449 was comparable to their respective inhibitory effect on the mouse-specific Gli mRNA expression in the tumor. However, BBR (20 μM) did not affect the expression of human transcription factor Gli1 mRNA in HT-29 and SW480 cells. In conclusion, BBR promotes the degradation of SHH mRNA in colorectal cancer cells, interrupting the paracrine Hedgehog signaling pathway activity thus suppresses the colorectal cancer growth. This study reveals a novel molecular mechanism underlying the anticancer action of BBR.
研究领域:
肿瘤学
·
分子生物学
·
药理学
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产品关联
DOI
PubMed
高影响因子
CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
·
2018
·Vol. 34
·期 4
·571-577
·
IF 1.248
Han Xie,Shao Kaiyuan,Hu Wenxiang
Hyperglycemia is frequently accompanying with hyperlipidemia. To explore the potent drugs with dual-activity and dual-site effects that could reduce blood glucose and blood lipid at the same time, fibrate group with lipid-lowering effect on the 9th position of berberine(BBR) was introduced using the drug design combination principle and the multitarget collaborative treatment method. Moreover, the molecular structure of BBR was modified, and six 9-substituted derivatives of BBR were designed and synthesized, among which, five compounds have never been reported before. In addition, the molecular structures of these derivatives were identified using liquid chromatography-mass spectrometry(LC-MS), 1 H nuclear magnetic resonance( 1 H NMR) and 13 C NMR, respectively. Furthermore, the microwave irradiation experimental technique was applied in the synthesis reaction using the novel microwave synthesizer, which accelerated the reaction rate, enhanced the reaction yield, reduced the reaction by-products, and simplified the post-processing steps. In the meantime, the 9-position regioselective demethylation of BBR was explored through quantum chemical calculation during the synthesis of berberrubine. The computations were consistent with the experimental results, which contributed to deducing the mechanism of its selective methylation.
研究领域:
药物化学
·
合成化学
·
计算化学
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产品关联
DOI
高影响因子
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
·
纳米技术
·
肿瘤学
·
天然产物化学
✓ 已验证
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）