Analytical Methods
·
2024
·
IF 2.7
Wenjuan Zhang,Mingwan Luo,Juan Chen,Zhengxing Li,Xian Wei,Miqi Wu,Shengli Yang,Yuanju He,Xiaoping Wang,Zhiyou Xiao
The intrinsic fluorescence of berberine is very weak, which can be enhanced by its interaction with specific aptamers. A simple and sensitive DNA sensor for visual detection of berberine has here been established. When using this sensor, there was a good linear relationship between the change in fluorescence intensity of berberine and the concentration of berberine in the range of 16–2000 nM, with a detection limit of 5.1 nM. The change in fluorescence intensity was caused by the addition of aptamers. A detection limit of 170.1 nM was acquired by reading the RGB values of fluorescent images with a smartphone for the quantification of berberine. Common antibiotics did not interfere with the measurement of the berberine concentration. The molecular ion peaks of the complexes formed by the aptamer and berberine could be clearly observed by electrospray ionization mass spectrometry. The UV-vis absorption spectra, circular dichroism spectra, and fluorescence spectra indicated a strong interaction between berberine and the aptamer. The dissociation constant (Kd) between berberine and the aptamer was 1.91 μM. This sensor was both simple and sensitive, requiring only a 21-base oligonucleotide. It realized a visual quantitative analysis with a smartphone. This method could also be used for similar fluorescence visualization determination of aptamer-based drug molecules.
研究领域:
分析化学
·
生物医学工程
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高影响因子
MOLECULES
·
2024
·Vol. 29
·期 1
·273
·
IF 4.2
Jinsheng Li,Xueli Hou,Jinlong Xiao,Li Zhu,Yujie Deng,Ziyi Li,Zijian Zhao,Zhenghong Luo,Hao Wei
The isoquinoline alkaloid berberine, derived from Coptidis rhizoma, exhibits antibacterial, hypoglycemic, and anti-inflammatory properties. Canagliflozin is a sodium–glucose cotransporter 2 (SGLT2) inhibitor. We synthesized compounds B9OC and B9OBU by conjugating canagliflozin and n-butane at the C9 position of berberine, aiming to develop antimicrobial agents for combating bacterial infections worldwide. We utilized clinically prevalent pathogenic bacteria, namelyStaphylococcus aureus,Escherichia coli, andPseudomonas aeruginosa, to investigate the antibacterial efficacy of B9OC. This was accomplished through the determination of the MIC80values, analysis of bacterial growth curves, evaluation of biofilm formation using crystal violet staining, assessment of impact on bacterial proteins via SDS-PAGE analysis, and observation of alterations in bacterial morphology utilizing field emission scanning electron microscopy. Meanwhile, the ADMET of compound B9OC was predicted using a computer-aided method. The findings revealed that B9OC exhibited lower minimal inhibitory concentrations against all three bacteria compared to berberine alone or in combination with canagliflozin. The minimal inhibitory concentrations (MICs) of B9OC against the three experimental strains were determined to be 0.035, 0.258, and 0.331 mM. However, B9OBu exhibited a lower level of antimicrobial activity compared to berberine. The compound B9OC exhibits a broad spectrum of antibacterial activity by disrupting the integrity of bacterial cell walls, leading to cellular rupture and the subsequent degradation of intracellular proteins.
研究领域:
药理学
·
微生物学
·
药物化学
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高影响因子
NEW JOURNAL OF CHEMISTRY
·
2024
·Vol. 48
·期 36
·15884-15893
·
IF 2.7
Dong Ju Zhou,Wei Ming Liu,Su Ping Dai,Shuai Qiang Jiang,Yin Wang,Jia Jia Yang,Ya Wei Chen,Jun Liang Chen,Hyun Jin Park,Hui Yun Zhou
In our work, serine-modified β-cyclodextrin (Ser-β-CD) was synthesized and a berberine hydrochloride (BBH)/Ser-β-CD inclusion complex (IC) was prepared using the freeze-drying method. Phase solubility studies showed that BBH and Ser-β-CD formed stable inclusion complexes in a stoichiometric ratio of 1 : 1. The IC was characterized using SEM and FT-IR analyses. The results of molecular docking showed that BBH was completely contained in the Ser-β-CD cavity and the binding energy was −7.87 kcal mol−1. The results of in vitro release studies indicated that BBH could be released slowly from the IC. In addition, the prepared Ser-β-CD and IC had good biocompatibility. The IC demonstrated excellent antibacterial activity against Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus). Therefore, the BBH/Ser-β-CD IC has potential application prospects in biomedicine and food industry.
研究领域:
药学
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材料科学
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生物技术
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微生物学
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NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
·
2023
·
IF 1.3
Zizhen Huang,Jie Wang,Hui Chen,Ruofei Feng,Chunxia Tan
Four organic-polyoxometalate hybrids BR4[SiW12O40] (BR–SiW), BR3[PMo12O40] (BR–PMo), BR4K[EuSiW11O40]·2H2O (BR–EuSiW) and BR6Na3[EuW10O36] (BR–EuW) were fabricated by the polyoxometalates (POMs) anions and berberine cations (BR) noted for the alkaloids in traditional Chinese herbal medicine. These hybrids have been characterized and confirmed. The interaction between hybrids and human serum albumin (HSA) was investigated in a buffer solution (pH 7.4) using ultraviolet–visible light absorption and fluorescence techniques. The classical Stern–Volmer equation was used to analyze the fluorescence quenching at three temperatures (296, 303 and 310 K), and the static quenching mechanism for interaction was proposed. The Thermodynamic parameters, enthalpy, entropy change, and Gibbs free energy of hybrids interacting on HSA were calculated by Scatchard equation. The results indicated that therewas one binding site on the protein and BR–POMs all showed stronger binding force than that of raw materials. Synchronous fluorescence results showed that the binding sites of BR–POMs and HSA were not effectively affected the surrounding microenvironment. The following antibacterial experiments implied that inhibitory effect of hybrids were synergistic effect from organic active ingredient and POMs but the simple combination. All these data were prepared for further research on biology.
研究领域:
生物化学
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药理学
·
分子生物学
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高影响因子
MOLECULES
·
2023
·Vol. 28
·期 23
·7725
·
IF 4.6
Jingqi Li,Qi Zhang,Yutong Chen,Chengyu Lu,Yongbin Tong
Demethyleneberberine is an active component extracted from the Chinese herbal drug Cortex Phellodendri. It is also a metabolite of berberine in animals and humans. However, the pharmacokinetics, tissue distribution and excretion of demethyleneberberine have not been reported. The present study aimed to investigate the pharmacokinetic parameters of demethyleneberberine by applying high-performance liquid chromatography-tandem mass spectrometry (LC-MS/MS). After intragastric administration of demethyleneberberine in rats and mice, the pharmacokinetics, tissue distribution and excretion of demethyleneberberine were comparatively studied for the first time. The plasma concentration of demethyleneberberine reached its peak within 5 min after intragastric administration in both rats and mice. Furthermore, its bioavailability was comparable, ranging from 4.47% to 5.94%, higher than that of berberine. The total excretion of demethyleneberberine in the urine, feces and bile was 7.28~9.77%. These findings provide valuable insights into the pharmacological and clinical research on demethyleneberberine.Keywords:demethyleneberberine;pharmacokinetics;tissue distribution;excretion;rats and mice
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INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2025
·Vol. 26
·期 5
·2193
·
IF 4.9
Yangyang Cheng,Haoyang Yu,Sitong Yang,Xiaolian Tian,Mengyu Zhao,Ling Ren,Xiuping Guo,Chujuan Hu,Jiandong Jiang,Lulu Wang
Liver fibrosis, caused by chronic hepatic injury, is a major threat to human health worldwide, as there are no specific drugs available for its treatment. Natural compounds, such as berberine (BBR) and quercetin (QR), have shown the ability to regulate energy metabolism and protect the liver without significant adverse effects. Additionally, combination therapy (the cocktail therapy approach), using multiple drugs, has shown promise in treating complicated conditions, including liver injury. In this study, we prepared a salt formulation of BBR and QR (BQS) to enhance their combined effect on liver fibrosis. The formation of BQS was confirmed using various analytical techniques, including nuclear magnetic resonance spectroscopy (NMR), differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR), powder X-ray diffractometry (PXRD), and scanning electron microscopy (SEM). The results demonstrated that the dissolution efficiency and bioavailability of QR significantly increased in the BQS form, aligning with that of BBR, compared to the physically mixed (BQP) form. Moreover, BQS exhibited a superior inhibitory effect on fibrosis compared to BQP in the human hepatic stellate cell line LX-2 by modulating lipid accumulation, inflammation, apoptosis, and the cell cycle. Furthermore, in a mouse model of hepatic fibrosis induced by methionine and choline-deficient (MCD) diets, BQS demonstrated enhanced anti-fibrotic activities compared to BQP. These findings suggest that BQS holds promise as a potential alternative treatment for liver fibrosis. Importantly, this study provides novel insights into achieving a cocktail effect through the salt formation of two or more drugs. The results highlight the potential of salt formulations in enhancing the therapeutic efficacy and consistent biological processes of drug combinations.
研究领域:
药理学
·
肝病学
·
药物开发
·
分子生物学
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JOURNAL OF ETHNOPHARMACOLOGY
·
2014
·
IF 2.939
Han-Ming Cui,Qiu-Yan Zhang,Jia-Long Wang,Jian-Long Chen,Yu-Ling Zhang,Xiao-Lin Tong
Ethnopharmacological relevance Berberine (BER) and BER-original herbal medicines have a variety of pharmacological functions and have been widely used in clinical. However, its effect of enzyme induction on cytochrome P450 (CYP) in human hepatocytes is unknown. Material and method Metabolism of berberine and its effect on main metabolic enzymes in HepG2 cell in vitro was investigated. Cocktail probe drugs, mRNA expression and protein expression were used to evaluate the metabolism potency. Meanwhile, an UPLC–MS/MS method was validated for the analysis of BER and four probe drugs in HepG2 cell. Result BER significantly increased the metabolism of midazolam, phenacetin and tolbutamide by inducing the CYP1A2 and 3A4 enzyme in a dose-dependent manner, the mRNA and protein expression of CYP1A2 and 3A4 were increased by berberine at 1000 ng·mL −1 . The activity of CYP1A2 and 3A4 could be induced by BER more than 500 ng·mL −1 in HepG2 cell, which was confirmed by the increase of its mRNA and protein expression. Conclusion BER increases the metabolism of cocktail drugs such as midazolam, phenacetin and tolbutamide by increasing the mRNA and protein expression of CYP1A2 and 3A4.
研究领域:
药理学
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生物化学
·
临床医学
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高影响因子
Frontiers in Pharmacology
·
2023
·
IF 5.6
Peng Xiong,Yang Yuping,Guo Chenqi,He Qin,Li Yan,Gong Tao,Li Jia
Berberine (BBR) has a long history of use in the treatment of Rheumatoid arthritis (RA) and is considered one of the most promising natural product for the treatment of RA. However, oral administration of berberine has low bioavailability and requires frequent administration, resulting in poor patient compliance. In this study, we developed a BBR-loaded phospholipid-based phase separation gel (BBR-PPSG) to achieve sustained drug release and long-term therapeutic effect. The stability of BBR-PPSG was verified and it was found that it can be stored for a long time. The pharmacokinetic study on rats and rabbits showed that BBR-PPSG not only achieved 1-month of sustained release, but also significantly increased the area under the curve (AUC) by nearly 9-fold and prolonged the half-life (t1/2) by 10-fold. By constructing rat and rabbit models of RA, we also proved that BBR-PPSG administration once a month effectively alleviated joint swelling, and significantly reduce TNF-α levels in AIA rats and OIA rabbits. Histopathological analysis of rabbit joint sections revealed that after intra-articular injection of BBR-PPSG, the synovial cell layer remained intact, while in the model group, the synovial cells were significantly reduced and exhibited necrosis. MicroCT data analysis showed that the values of Tb.N and Tb. Sp in the BBR-PPSG group were significantly better than those in the model group (p < 0.05). This study addressed the limitations of frequent administration of BBR by developing a phospholipid-based phase separation gel system for berberine delivery, achieving long-term sustained release. The BBR-PPSG demonstrated good biocompatibility, simple preparation and excellent stability, thus holding potential as a novel pharmaceutical formulation for RA treatment.
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高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR MEDICINE
·
2023
·Vol. 51
·期 6
·1-13
·
IF 5.4
Lin Yang,Chun-Feng Cheng,Zhi-Fang Li,Xiao-Jing Huang,Shao-Qing Cai,Shan-Yu Ye,Li-Jun Zhao,Yi Xiong,Dong-Feng Chen,He-Lu Liu,Zhen-Xing Ren,Hong-Cheng Fang
Diabetic cardiomyopathy (DCM) is a cardiovascular disease which has been reported as a major cause of mortality worldwide for several years. Berberine (BBR) is a natural compound extracted from a Chinese herb, with a clinically reported anti‑DCM effect; however, its molecular mechanisms have not yet been fully elucidated. The present study indicated that BBR markedly alleviated DCM by inhibiting IL‑1β secretion and the expression of gasdermin D (Gsdmd) at the post‑transcriptional level. Considering the importance of microRNAs (miRNAs/miRs) in the regulation of the post‑transcriptional process of specific genes, the ability of BBR to upregulate the expression levels of miR‑18a‑3p by activating its promoter (‑1,000/‑500) was examined. Notably, miR‑18a‑3p targeted Gsdmd and abated pyroptosis in high glucose‑treated H9C2 cells. Moreover, miR‑18a‑3p overexpression inhibited Gsdmd expression and improved biomarkers of cardiac function in a rat model of DCM. On the whole, the findings of the present study indicate that BBR alleviates DCM by inhibiting miR‑18a‑3p‑mediated Gsdmd activation; thus, BBR may be considered a potential therapeutic agent for the treatment of DCM.
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高影响因子
MOLECULES
·
2018
·Vol. 24
·期 1
·103
·
IF 3.098
Hong-Xin Cui,Ya-Nan Hu,Jing-Wan Li,Ke Yuan,Ying Guo
Berberine has many pharmacological effects, such as antidiabetic, antimicrobial, anti-inflammatory, and antioxidant, but the question remains on how its low oral bioavailability has greatly limited its clinical application. As a safer hypoglycemic agent, we must evaluate the bioavailability of berberine organic acid salts (BOAs) to ensure that the bioavailability of berberine is not negatively affected. It has been proven that the bioavailability of BOAs is higher than that of BH (berberine hydrochloride); especially BF (berberine fumarate) and BS (berberine succinate), which are improved by 1.278-fold and 1.313-fold, respectively. After 1 h of oral administration, berberine mainly acted on the stomach of mice, it also influenced the liver, kidney, lungs, and intestines after 4 h. The accumulation of BF in the lung is more evident than BH. Our analysis shows that these results are closely related to the regulation of organic acids and berberine in the intestinal tract, they also indicate the influence of intestinal flora on berberine metabolism.Keywords:berberine organic acid salts;type 2 diabetes;pharmacokinetics;in-vivo imaging;intestinal flora
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Experimental and Therapeutic Medicine
·
2019
·Vol. 18
·期 4
·2385-2392
·
IF 1.448
Li Li,Qiuhong Li,Lei Wei,Zhongfu Wang,Wei Ma,Fangying Liu,Yanhua Shen,Shanfang Zhang,Xiulian Zhang,Huiping Li,Yechang Qian
Pulmonary fibrosis (PF) is a heterogeneous pathological process in lung tissues with a considerable mortality rate. Currently, combination therapy represents an effective approach to treat PF. Dexamethasone (Dxs) and berberine (BBR) are widely applied to inhibit the progression of PF. Dxs plus penehyclidine hydrochloride or alfacalcidol have been reported more effective in therapy compared with any single drug treatment. However, whether Dxs plus BBR induces an increased antifibrotic effect remains unknown. The current study aimed to evaluate the therapeutic effect of BBR plus Dxs in bleomycin (BLM)‑induced PF. A PF model in rats was established and rats were divided into control, BLM, BBR, Dxs and BBR plus Dxs groups (n=9/group). On days 3, 7 and 14, blood samples were collected from the eyes of the rats (n=6/group). CXC chemokine ligand 14 (CXCL14), collagen I, collagen III, matrix metalloproteinase (MMP)2 and MMP9 serum levels were measured by ELISA. On day 14, all rats were sacrificed. Hematoxylin and eosin analysis, Masson staining and hydroxyproline (Hyp) assessment were performed to observe histopathological changes and collagen deposition. mRNA and protein levels of CXCL14, CXC chemokine receptor 4 (CXCR4), collagen I/III, α‑smooth muscle actin (α‑SMA), MMP2/9 and phosphorylated‑Smad 2/3 in lung tissue were further evaluated. Similar effects in preventing lung damage were observed histopathologically for Dxs and BBR compared with the BLM group. These treatments further reduced levels of Hyp, CXCL14, CXCR4, collagen I/III, MMP2/9, α‑SMA and p‑Smad 2/3. The combination of Dxs and BBR exhibited increased effectiveness compared with the single treatments. Results further suggested that antifibrotic mechanisms were involved in inhibiting CXCL14 and MMP2/MMP9 expression, and preventing the activation of Smad2/3 and hedgehog signaling pathways. The combined use of Dxs and BBR may represent a potential therapeutic approach for PF.
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高影响因子
MICROCHIMICA ACTA
·
2022
·Vol. 189
·期 11
·1-15
·
IF 6.408
Jin Pian,Zhu Fucheng,Jiang Mi,Takafuji Makoto,Ihara Hirotaka,Nie Lei,Liu Houmei
In view of the limitations of existing berberine solid-phase extraction adsorbents, this paper proposes a novel carbonized π-conjugated polymer-coated porous silica (SiO 2 @C-π-CP) adsorbent with simple process and low cost for efficient extraction of berberine by multiple interactions. Characterization methods, including Brunner–Emmet–Teller measurement, thermogravimetric analysis, X-ray photoelectron spectroscopy, and scanning electron microscopy techniques, were used to verify the successful modification of carbonized π-conjugated polymer on the surface of porous silica. The berberine was selected as target molecule, and the adsorption mechanism and process were investigated through adsorption kinetics, adsorption isotherms, and thermodynamic studies. The fitting results show that the adsorption of berberine by SiO 2 @C-π-CP well conforms to the pseudo-second-order and Langmuir models. By optimizing the main SPE parameters, the SPE method based on SiO 2 @C-π-CP was developed. Excellent results were obtained, including low limit of detection (0.75 ng mL −1 ) and limit of quantification (2 ng mL −1 ), wide linearity (2–13,000 ng mL −1 ), and satisfactory relative standard deviations (RSD) of inter-day (1.5%) and intra-day (6.2%). Finally, the SiO 2 @C-π-CP also has been successfully used to the enrichment of berberine in real urine samples. This research makes clear that SiO 2 @C-π-CP has outstanding potential for trace enrichment of berberine alkaloids. Graphical abstract
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危险品化学品经营许可证（带存储）