ARCHIVES OF PHARMACAL RESEARCH
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2014
·Vol. 37
·期 12
·1617-1623
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IF 1.751
Shi Lei,Dang Xue-Liang,Liu Xin-You,Wei Hua-Mei,Yang Meng-Meng,Zhang Yan
Carbamazepine (CBZ), an antiepileptic with narrow therapeutic window, is a substrate of CYP 3A4 which metabolizes CBZ to carbamazepine-10,11-epoxide (CBZE). CBZE is an active and toxicity metabolite, and it is a substrate of MRP-2. Using CBZ for a long time can cause hepatic injury. Sophora flavescens (SF) is a medicinal herb used for the protected hepatic injury. This study investigated the acute and chronic effects of SF on the pharmacokinetics of CBZ in rats. The concentrations of CBZ and CBZE in plasma and tissues were determined by HPLC method. The results showed that SF which significantly decreased the AUC 0-t of CBZ, increased CBZE conversely. Tissue analysis showed that the concentrations of CBZ and CBZE in brain and liver were decreased by SF. In addition, the distribution of CBZE in kidney was reduced significantly, which influenced the CBZE excretion and increased the drug toxic potentially. Results in the current study suggest that patients using CBZ might be cautioned in the use of SF extract or Sophora -derived products. Meanwhile, patients receiving drugs which are substrates of CYP 3A4 and/or MRP-2 should be advised of the potential herb–drug interaction to reduce the risk of therapeutic failure or increased toxicity of conventional drug therapy.
研究领域:
药理学
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中药学
✓ 已验证
DOI
PubMed
高影响因子
RSC Advances
·
2017
·Vol. 7
·期 55
·34746-34754
·
IF 3.108
Ziwei Hu,Mingshan Xie,Danting Yang,Dong Chen,Jingyi Jian,Haibin Li,Kaisong Yuan,Zhengjin Jiang,Haibo Zhou
Berberine is an important anti-inflammatory drug widely used for the treatment of heart and intestinal disorders. The quantification of berberine is usually required in clinic medical assays. Herein, we report simple, fast and sensitive colorimetric visualization of berberine in human plasma using citrate-stabilized gold nanoparticles (AuNPs). Upon exposure to μg mL−1 levels of berberine, the AuNP solution exhibits a highly sensitive color change from red to blue and rapid aggregation kinetics within the initial 10 min, which can be directly seen with the naked eye and monitored by UV-vis absorbance spectroscopy. As confirmed by comparison with potential coexisting foreign substances, the presence of positively charged berberine induces the aggregation of the AuNPs owing to the electrostatic attraction and coordination interactions between the ring nitrogen atoms of berberine and the AuNPs, causing a color change of the AuNP suspension. Further evidence is that the sensitivity is significantly improved when NaHSO4 is added to promote the ligand exchange between citrate and berberine at the surface of the AuNPs. The NaHSO4-optimized AuNP system provides a simple colorimetric assay for the rapid detection of berberine in human plasma. The limit of detection (LOD) is 0.24 μg mL−1 by the naked eye and 0.06 μg mL−1 by UV-vis spectroscopy.
研究领域:
药理学
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分析化学
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纳米医学
✓ 已验证
DOI
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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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
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临床医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
LIFE SCIENCES
·
2019
·
IF 3.448
Jian Liu,Zhenjing Zhu,Yueyao Liu,Linlin Wei,Bai Li,Fengxia Mao,Ju Zhang,Yingchao Wang,Yufeng Liu
Aims Berberine (BBR) is reported to induce apoptosis and inhibit migration of leukemic cells, but the underlying pharmacological mechanisms have not been fully revealed. This study aims to investigate the possible mechanisms from the perspective of autophagy. Main methods P-53-null leukemic cell lines Jurkat and U937 were used for the in vitro study. MDC staining was used for observation of autophagy in leukemic cells, and Western blot analysis was for determination of the expression levels of autophagy-associated proteins. Apoptosis of the leukemic cells was detected by flow cytometry. Cellular location of MDM2 was observed with immunofluorescence staining. Ubiquitination of MDM2 was assessed by immunoprecipitation. Male 6–8-week-old NOD/SCID mice were used for evaluating the effect of BBR on chemotherapy sensitivity in vivo . Key findings BBR induced autophagy in p53-null leukemic cells, which was inhibited by autophagy inhibitors 3-methyladenine. 3-methyladenine also inhibited BBR-induced apoptosis in leukemic cells. In addition, BBR not only decreased MDM2 mRNA expression, but also enhanced MDM2 self-ubiquitination in leukemic cells. Forced overexpression of MDM2 reversed the effect of BBR on autophagy and apoptosis. Furthermore, BBR promoted doxorubicin-induced autophagy and cell death in the leukemic cells and overexpression of MDM2 suppressed these effects. In vivo , BBR combined with doxorubicin achieved better therapeutic effect than doxorubicin alone. Significance MDM2 inhibits autophagy and apoptosis in leukemic cells in a p53-independent manner. BBR induces autophagy in p53-null leukemic cells through downregulating MDM2 expression at both transcriptional and post-transcriptional levels, which may contribute to the anti-cancer effect of BBR in leukemia.
研究领域:
肿瘤学
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药理学
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细胞生物学
✓ 已验证
产品关联
DOI
PubMed
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.
研究领域:
药理学
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代谢紊乱
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分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
SCIENCE OF THE TOTAL ENVIRONMENT
·
2020
·
IF 6.551
Shang Li,Yi Tao,Guo-Hua Dao,Hong-Ying Hu
The risk of harmful algal blooms (HABs) in the water recharged with reclaimed water is a bottleneck for water reuse . The suppression effects and mechanisms of the combination of UV-C and berberine on Microcystis aeruginosa and Scenedesmus obliquus in reclaimed water were investigated. Mono UV-C irradiation at 75 mJ cm −2 could suppress the growth of M. aeruginosa for 7 d and that at 90 mJ cm −2 could suppress the growth of S. obliquus for 5 d. UV-C irradiation combined with 0.2–2 mg L −1 berberine lengthened the inhibition period of M. aeruginosa to 10- > 22 d and that of S. obliquus to 7- > 22 d and induced more rapid lethal effects on the harmful microalgal cells, in significant synergetic patterns. The combination of UV-C and berberine suppressed total, intracellular and extracellular microcystin-LR (MC-LR) more effectively and decreased the MC-LR quota significantly, which further reduced the risks of microcystin production and release. Furthermore, synergetic mechanisms of the combined treatments were systematically investigated from the aspects of photosynthetic system (photosynthetic activity and pigments), metabolic activity (ATP and membrane potential), oxidation stress (reactive oxygen species (ROS) and glutathione (GSH)), and apoptosis-like cell death (phosphatidylserine (PS) ectropion, caspase-3 activity and terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) positive rate). The combination treatment provided a joint attack of UV-C and berberine on photosynthetic transport chain of photosynthetic system II (PS II), and a synergetic pathway to achieve more severe disruptions in energy metabolism as well as aggravated oxidative stress . The accumulated ROS enhanced increases in programmed cell death (PCD) indicators of both microalgal species, which contributed to the enhancement effects on growth suppression. The results showed that the combination treatment achieved lower dose requirements of both UV-C irradiation and berberine for inducing the same inhibition effects on microalgal cells, which was promising to be applied in the HABs control of reclaimed water.
研究领域:
环境科学
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藻类学
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水处理工程
✓ 已验证
产品关联
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
✓ 已验证
DOI
PubMed
高影响因子
Biomaterials Advances
·
2025
·
IF 6
Dan Deng,Runfu Chen,Suai Lin,Yanxin Tao,Gaojin Pei,Bofei Cheng,Mengzhen Zhao,Haoxin Cheng,Junze Yan,Xiaolei Wang
Psoriasis, an immune-mediated chronic inflammatory skin disorder, poses challenges for topical treatment due to the thickening of the stratum corneum, hindering drug penetration. Furthermore, long-term use of chemical drugs may lead to immunosuppression and abnormal hepatic or renal dysfunction. Inspired by traditional Chinese fire cupping (Ba Huo Guan), a negative-pressure microneedle syringe therapy has been proposed here for psoriasis treatment. This microneedle syringe demonstrated an enhanced transepidermal drug delivery efficiency. Additionally, the microneedles contain nanoparticles self-assembled from Chinese herbal monomers berberine (BBR) and ferulic acid (FA), which play vital roles in psoriasis treatment, including inhibiting abnormal proliferation of local microbial communities, scavenging excess reactive oxygen species, suppressing keratinocyte proliferation locally, and modulating macrophage polarization to mitigate inflammation.
研究领域:
皮肤病学
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药剂学
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纳米医学
✓ 已验证
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
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环境科学
✓ 已验证
DOI
MOLECULES
·
2020
·Vol. 25
·期 8
·1957
·
IF 3.267
Ying Li,Chunyan Zhu
Microspheres containing absorption enhancer (sodiumN-[8-(2-hydroxybenzoyl)amino]caprylate, SNAC) were developed to enhance the oral bioavailability of berberine hydrochloride (BER) with poor intestinal membrane permeability. Microspheres were prepared and characterized by particle size measurements, scanning electron microscopy, differential scanning calorimetry, BER payload and release, Caco-2 cell monolayer transport, and rat pharmacokinetics. The microspheres were spherical and had uniform size, high encapsulation efficiency and high loading capacity. In vitro release studies showed that BER-loaded microspheres had good sustained release characteristics. The Caco-2 cell monolayer transport study proved that SNAC could significantly enhance permeability of BER 2–3-fold. Pharmacokinetic studies demonstrated a 9.87-fold increase in area under the curve (AUC) of BER mixed with SNAC and a 14.14-fold increase in AUC of microspheres compared with BER alone. These findings indicate that SNAC is a promising absorption enhancer for oral delivery of BER in the form of both solution and microspheres.Keywords:sodiumN-[8-(2-hydroxybenzoyl)amino]caprylate;permeation enhancement;berberine hydrochloride;microspheres;oral bioavailability
研究领域:
药剂学
·
药物代谢动力学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PHARMAZIE
·
2020
·Vol. 75
·期 10
·483-487
·
IF 1.198
Wang Lili,Liu Shuyu,Gao Ziyao
Berberine hydrochloride (BCl) is commercially used to treat diarrhea, diabetes, hyperlipidemia, and cancer. However, BCl suffers from solid state instability, low aqueous solubility, low dissolution rate, and poor bioavailability, which limit its potential application in clinical medicine.
In this work, we report a novel cocrystal hydrate of BCl with L(+)-lactic acid (BCl-LA-H2O), designed to improve its physicochemical properties, thus promoting its application in the pharmaceutical industry. As a result, the cocrystal strategy improved the solubility, dissolution,
melting point, and hygroscopicity of BCl, which indicated that the BCl-LA-H2O can be used as a better solid form.
研究领域:
药学
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材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Polymers
·
2018
·Vol. 10
·期 11
·1198
·
IF 2.935
Jingfu Jia,Kerong Zhang,Xue Zhou,Dan Zhou,Fahuan Ge
It is still controversial whether poor aqueous solubility is the most primary reason for the low oral bioavailability of insoluble drugs. Therefore, in this study, berberine-loaded solid polymeric particles (BPs) of varied dissolution profiles with β-cyclodextrin (β-CD) as carrier were fabricated using solution-enhanced dispersion by supercritical fluids (SEDS), and the relationship between dissolution and berberine (BBR) bioavailability was evaluated. Dissolution property was controlled via particle morphology manipulation, which was achieved by adjusting several key operating parameters during the SEDS process. Characterization on BP using infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction indicated that BBR was dispersed in amorphous form, while nuclear magnetic resonance spectroscopy showed that methoxy groups of BBR were included into the cavities of β-CD. In vivo pharmacokinetic studies showed that oral bioavailability increased by about 54% and 86% when the dissolution rate of BBR was increased by 51% and 83%, respectively. The entry speed of BBR into the bloodstream was also advanced with the degree of dissolution enhancement. It seemed that dissolution enhancement gave positive effect to the oral bioavailability of berberine, but this might not be the crucial point. Meanwhile, supercritical CO2technology is a promising method for pharmaceutical research due to its advantages in regulating drug-dosage properties.Keywords:berberine;polymeric particle;supercritical CO2;dissolution;bioavailability
研究领域:
药学
·
药物递送系统
✓ 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）