The metabolism of berberine and its contribution to the pharmacological effects

Wang, Kun; Feng, Xinchi; Chai, Liwei; Cao, Shijie; Qiu, Feng

doi:10.1080/03602532.2017.1306544

Cited by 334 publications

(257 citation statements)

References 102 publications

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“…Berberine widely exists in diversified kinds of herbs, and has many pharmacological effects, especially to protect against urinary system diseases (Lu, Du, & Wang, ; Wang et al, ). Li et al () investigated the dynamic changes of metabolite profiles in cell models and Balb/c nude‐mouse model of prostate cancer, to reveal a therapeutic mechanism of berberine.…”

Section: Ms In Herbal Ingredinetsmentioning

confidence: 99%

“…With MS advantages, researchers can bring the insight into the therapeutic effect from multicomponent and multi-target of herbal medicines, as well to elucidate the mechanism of drug action. Berberine widely exists in diversified kinds of herbs, and has many pharmacological effects, especially to protect against urinary system diseases (Lu, Du, & Wang, 2015;Wang et al, 2017b). Li et al (2017b) investigated the dynamic changes of metabolite profiles in cell models and Balb/c nude-mouse model of prostate cancer, to reveal a therapeutic mechanism of berberine.…”

Section: Drug Metabolism and Mechanisms Of Actionmentioning

confidence: 99%

See 1 more Smart Citation

Novel applications of mass spectrometry‐based metabolomics in herbal medicines and its active ingredients: Current evidence

Wang

Ren

Zhang

et al. 2019

Mass Spectrometry Reviews

100

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Current evidence shows that herbal medicines could be beneficial for the treatment of various diseases. However, the complexities present in chemical compositions of herbal medicines are currently an obstacle for the progression of herbal medicines, which involve unclear bioactive compounds, mechanisms of action, undetermined targets for therapy, non‐specific features for drug metabolism, etc. To overcome those issues, metabolomics can be a great to improve and understand herbal medicines from the small‐molecule metabolism level. Metabolomics could solve scientific difficulties with herbal medicines from a metabolic perspective, and promote drug discovery and development. In recent years, mass spectrometry‐based metabolomics was widely applied for the analysis of herbal constituents in vivo and in vitro. In this review, we highlight the value of mass spectrometry‐based metabolomics and metabolism to address the complexity of herbal medicines in systems pharmacology, and to enhance their biomedical value in biomedicine, to shed light on the aid that mass spectrometry‐based metabolomics can offer to the investigation of its active ingredients, especially, to link phytochemical analysis with the assessment of pharmacological effect and therapeutic potential. © 2019 Wiley Periodicals, Inc. Mass Spec Rev

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Section: Ms In Herbal Ingredinetsmentioning

confidence: 99%

Section: Drug Metabolism and Mechanisms Of Actionmentioning

confidence: 99%

Novel applications of mass spectrometry‐based metabolomics in herbal medicines and its active ingredients: Current evidence

Wang

Ren

Zhang

et al. 2019

Mass Spectrometry Reviews

100

View full text Add to dashboard Cite

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“…Berberine (BBR), which can be isolated from a variety of plants (i.e., Coptidis chinensis Franch, Phellodendron chinense Schneid, etc. ), exhibits anti-diabetic, anti-cancer and anti-oxidant activities in treating some clinical disorders [13]. During the research of sepsis, BBR could prevent intestinal mucosal barrier damage at the early phase of disease [14].…”

Section: Survival Ratementioning

confidence: 99%

Berberine Prevents Cognitive Disorders Induced by Sepsis by Regulating the Inflammatory Cytokines, Oxidative Stress and Neuronal Apoptosis in Rat Brain

Shi¹,

Zhao²,

Ge³

et al. 2018

Neuropsychiatry

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Sepsis is a life-threatening organ dysfunction caused by a dysregulated host response to infection and can cause a huge burden to whole families and to society in terms of medical costs. Cognitive disorders induced by sepsis are still exasperating problems in clinical research. This paper examines a new measure of berberine (BBR) in sepsis induced cognitive disorders based on CLP surgery. BBR is one of many extracts from Chinese traditional herbs and exhibits antidiabetic, anticancer and antioxidant activities in treating various clinical disorders. Whether BBR shows efficacy in improving survival rates and inhibiting the extent of cognitive disorders after sepsis was explored in this paper. The result revealed that BBR treatment significantly improved the survival rate and cognitive disorders in septic rats. Increased levels of antioxidant superoxide dismutase (SOD) and reduced levels of lipid peroxidation malondialdehyde (MDA) were exhibited in the serum and brain tissue of the BBR treatment group. Moreover, the inflammatory cytokine (IL-1β, IL-4, IL-6, TNF-α) levels in the brain tissue were all decreased in the BBR treatment group compared to those in the sepsis group. BBR also largely protected the cells from apoptosis in the cerebral cortex and hippocampal CA1 region. Overall, our results indicated that BBR exhibited protective effects on survival rate and cognitive disorders after sepsis by inhibiting the release of inflammatory cytokines, oxidative stress and neuronal apoptosis in brain tissue. Therefore, BBR is a potential drug that shows efficacy in avoiding death rates and cognitive disorder after sepsis.

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“…Berberine Induces CYP2J2 Expression in Human U251 Glioma Cells via of PPARα 361 Pharmacology 2020;105:360-367 DOI: 10.1159/000503884 titative characterization of many proprietary Chinese medicines [1]. Currently, there is an increasing interest in berberine due to its favorable biological activities, and there have been many studies regarding its pharmacokinetic properties [2][3][4] and pharmacological activities [5]. In clinical practice and some trials, berberine has been shown to have therapeutic effects on several clinical disorders, including neurodegenerative diseases [6][7][8], cancer [9], cardiological problems [10,11], metabolic syndrome [12], mood disorders [13], and hepatic and renal disorders [14], indicating that berberine has potential for further development as a natural drug.…”

Section: Introductionmentioning

confidence: 99%

“…CYP2J2 is the only member of the CYP2J subfamily in humans. One of its major biological functions is as an arachidonic acid (AA) epoxygenase, which breaks AA into 4 regioisomeric cis-epoxyeicosatrienoic acids (5,8,11,and 14, [19,20]. CYP2J2 encodes a 502 amino acid protein that is primarily expressed in the heart, and, to a lesser degree, in the brain, pancreas, liver, kidney, gastrointestinal tract, and skeletal muscle [14].…”

Section: Introductionmentioning

confidence: 99%

Berberine Induces <b><i>CYP2J2</i></b> Expression in Human U251 Glioma Cells via Regulation of Peroxisome Proliferator-Activated Receptor Alpha

Wang

et al. 2019

Pharmacology

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Background: Berberine is a promising natural drug that has a potential therapeutic effect on neurodegenerative diseases. Objectives: Using U251 cells in vitro, we investigated whether berberine exerts its neuroprotective effect via regulation of CYP2J2. Method: After pretreatment with increasing concentrations (1, 3, and 10 μmol/L) of berberine for 0.5 h, U251 cells were stimulated with 1 μg/mL of lipopolysaccharide (LPS). Cell viability was measured 24 h later using a CCK8 kit. mRNA and protein levels of CYP2J2 and peroxisome proliferator-activated receptor alpha (PPARα) were measured by quantitative real-time-polymerase chain reaction and western blotting, respectively, after 24 h of exposure to 1, 3, or 10 μmol/L berberine. Fluorescence immunocytochemistry was also used to evaluate PPARα protein expression after treatment of U251 cells with 10-μmol/L berberine for 24 h. Transient transfection (cotransfection with the plasmid of PPARα-and RXRα-containing) followed by luciferase and chromatin immunoprecipitation assays was used to elucidate the molecular mechanism underlying the observed effects. Results: Compared to the control, LPS-induced U251 cell death was attenuated by berberine in a dose-dependent manner. After 24 h, cell viability was found to be 52.3% (p < 0.05), 66.2% (p < 0.01), and 70.9% (p < 0.001) using 1, 3, and 10 μmol/L berberine treatment, respectively. At these concentrations, berberine increased the CYP2J2 mRNA levels by 1.31-fold (p < 0.05), 1.48-fold (p < 0.01), and 1.88-fold (p < 0.01), respectively, and increased the PPARα mRNA levels 1.17-fold (p < 0.05), 1.29-fold (p < 0.05), and 1.53-fold (p < 0.01), respectively, compared with the respective control groups. In addition, the CYP2J2 and PPARα protein level was also significantly upregulated in U251 cells by berberine (concentrations in 1, 3, and 10 μmol/L) in a dose-dependent manner, compared with the respective control groups. Further investigation indicated that berberine enhances the heterodimerization of PPARα and RXRα, which together bind to the CYP2J2 promoter to induce the expression of CYP2J2 in U251 cells. Conclusion: Upon exposure of U251 cells to berberine, CYP2J2 expression is induced as a result of PPARα stimulation, resulting in a neuroprotective effect.

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The metabolism of berberine and its contribution to the pharmacological effects

Cited by 334 publications

References 102 publications

Novel applications of mass spectrometry‐based metabolomics in herbal medicines and its active ingredients: Current evidence

Novel applications of mass spectrometry‐based metabolomics in herbal medicines and its active ingredients: Current evidence

Berberine Prevents Cognitive Disorders Induced by Sepsis by Regulating the Inflammatory Cytokines, Oxidative Stress and Neuronal Apoptosis in Rat Brain

Berberine Induces <b><i>CYP2J2</i></b> Expression in Human U251 Glioma Cells via Regulation of Peroxisome Proliferator-Activated Receptor Alpha

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