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1.
Article in Chinese | WPRIM | ID: wpr-879146

ABSTRACT

Malignant tumor, an important factor threatening human life and health, brings huge economic burden to patients. At present, chemoradiotherapy is still the main treatment method for tumor diseases, but there are also great side effects when it plays a therapeutic role. Traditional Chinese medicine in the prevention and treatment of tumor diseases has many advantages such as few side effects, improving the physiological state of patients, and slowing down the side effects of radiotherapy and chemotherapy. Berberine is an effective component of rhizoma coptidis, with a very good antitumor effect. It can inhibit tumor cell proliferation, promote tumor cell apoptosis, inhibit tumor metastasis and angiogenesis, regulate tumor autophagy, reverse multi-drug resistance of tumor, regulate the body immunity, and affect tumor metabolic reprogramming to play its role. Compared with chemical preparations, berberine has a wide range of sources, with high safety and easy access, and has great potential in the prevention and treatment of malignant tumors. In this article, we would mainly review the research progress on the antitumor mechanism of berberine in recent years.


Subject(s)
Berberine/pharmacology , Cell Proliferation , Drugs, Chinese Herbal , Humans , Medicine, Chinese Traditional , Neoplasms/drug therapy
2.
Article in Chinese | WPRIM | ID: wpr-878924

ABSTRACT

The aim of this paper was to investigate the effect of berberine hydrochloride on the cell wall integrity of Candida albicans hypha. The minimal inhibitory concentration(MIC) of berberine hydrochloride against clinical and standard C. albicans strains was detected by micro liquid-based dilution method; the effect of berberine hydrochloride on the colony formation of C. albicans SC5314 was investigated by spot assay; the effect of berberine hydrochloride on the metabolism of C. albicans SC5314 hypha was checked by XTT reduction assay, and the viability of C. albicans SC5314 hypha was tested by fluorescent staining assay. The effect of berberine hydrochloride on the morphology of C. albicans SC5314 hypha was examined by scanning electron microscope. The changes in the cell wall of C. albicans SC5314 hypha after berberine hydrochloride treatment were detected by transmission electron microscopy. The effect of berberine hydrochloride on β-glucan from C. albicans SC5314 was detected by flow cytometry. The effect of berberine hydrochloride on hypha-specific gene ECE1 and β-glucan synthase genes FKS1 and FKS2 in C. albicans was examined by qRT-PCR. The results showed that berberine hydrochloride showed a strong inhibitory effect on both clinical and standard strains of C. albicans, and the MIC was 64-128 μg·mL~(-1). Spot assay, XTT redunction assay and fluorescent staining assay showed that with the increase of berberine hydrochloride concentration, the viability of C. albicans SC5314 gradually decreased. The transmission electron microscopy scanning assay showed that this compound could cause cell wall damage of C. albicans. The flow cytometry analysis showed the exposure degree of C. albicans β-glucan. The qRT-PCR further showed that berberine hydrochloride could significantly down-regulate hypha-specific gene ECE1 and β-glucan synthase-related gene FKS1 and FKS2. In conclusion, this compound can down-regulate C. albicans and β-glucan synthase-related gene expressions, so as to destroy the cell wall structure of C. albicans, expose β-glucan and damage the integrity of the wall.


Subject(s)
Antifungal Agents/pharmacology , Berberine/pharmacology , Candida albicans/genetics , Cell Wall , Hyphae , Microbial Sensitivity Tests
3.
Article in Chinese | WPRIM | ID: wpr-878907

ABSTRACT

Berberine is the main extract of Coptis chinensis, and its anti-inflammatory, antioxidant, antibacterial and immunomodulatory effects have been confirmed by modern studies. Ulcerative colitis(UC) is a chronic, idiopathic inflammatory bowel disease with unknown etiology. Its causes involve genetics, intestinal microecology and mucosal immune system disorders. In this paper, literatures on relevant pathways and mechanism of berberine on ulcerative colitis in recent years were consulted and summarized to provide me-thods and ideas for developing berberine in the treatment of UC and exploring the mechanisms. The results showed that berberine protects the intestinal mucosal barrier, restores the body's normal immune response, and improves oxidative stress by regulating multiple signaling pathways, such as JAK-STAT, NK-κB, PI3 K-AKT, MAPK, Nrf2, ERS, and MLCK-MLC, so as to treat UC.


Subject(s)
Berberine/pharmacology , Colitis , Colitis, Ulcerative/genetics , Humans , Intestinal Mucosa , Signal Transduction
4.
Article in English | WPRIM | ID: wpr-828960

ABSTRACT

Once pulp necrosis or apical periodontitis occurs on immature teeth, the weak root and open root apex are challenging to clinicians. Berberine (BBR) is a potential medicine for bone disorders, therefore, we proposed to apply BBR in root canals to enhance root repair in immature teeth. An in vivo model of immature teeth with apical periodontitis was established in rats, and root canals were filled with BBR, calcium hydroxide or sterilized saline for 3 weeks. The shape of the roots was analyzed by micro-computed tomography and histological staining. In vitro, BBR was introduced into stem cells from apical papilla (SCAPs). Osteogenic differentiation of stem cells from apical papilla was investigated by alkaline phosphatase activity, mineralization ability, and gene expression of osteogenic makers. The signaling pathway, which regulated the osteogenesis of SCAPs was evaluated by quantitative real time PCR, Western blot analysis, and immunofluorescence. In rats treated with BBR, more tissue was formed, with longer roots, thicker root walls, and smaller apex diameters. In addition, we found that BBR promoted SCAPs osteogenesis in a time-dependent and concentration-dependent manner. BBR induced the expression of β-catenin and enhanced β-catenin entering into the nucleus, to up-regulate more runt-related nuclear factor 2 downstream. BBR enhanced root repair in immature teeth with apical periodontitis by activating the canonical Wnt/β-catenin pathway in SCAPs.


Subject(s)
Animals , Berberine , Pharmacology , Cell Differentiation , Dental Papilla , Male , Osteogenesis , Periapical Periodontitis , Therapeutics , Rats , Stem Cells , Cell Biology , Metabolism , Wnt Signaling Pathway , Wnt3A Protein , Genetics , Metabolism , X-Ray Microtomography
5.
Article in Chinese | WPRIM | ID: wpr-878850

ABSTRACT

Protoberberine alkaloids belong to the quaternary ammonium isoquinoline alkaloids, and are the main active ingredients in traditional Chinese herbal medicines, like Coptis chinensis. They have been widely used to treat such diseases as gastroenteritis, intestinal infections, and conjunctivitis. Studies have shown that structural modification of the protoberberine alkaloids could produce derivative compounds with new pharmacological effects and biological activities, but the transformation mechanism is not clear yet. This article mainly summarizes the researches on the biotransformation and structure modification of protoberberine alkaloids mainly based on berberine, so as to provide background basis and new ideas for studies relating to the mechanism of protoberberine alkaloids and the pharmacological activity and application of new compounds.


Subject(s)
Alkaloids , Berberine , Berberine Alkaloids , Biotransformation , Coptis
6.
Article in Chinese | WPRIM | ID: wpr-777530

ABSTRACT

In order to clarify the characteristic components of Berberidis Cortex,the preparative liquid chromatography and spectral analysis methods were used to separate and identify the unknown components in the water extract of Berberidis Cortex. Two compounds were isolated and identified as bufotenidine and ferulic acid 4-O-β-D-glucopyranoside. They were both isolated for the first time from Berberidis Cortex and Berberis. In addition,an HPLC method was successfully established for simultaneously determination of six compounds in Berberidis Cortex,and chemometric methods were used to study the chemical differences among three main species of Berberidis Cortex. The results suggested that jatrorrhizine and bufotenidine are the main difference compounds among the three species.Compared with B. kansuensis and B. diaphana,B. vernae contains significantly more jatrorrhizine(P<0. 01),and the content of bufotenidine in B. vernae was significantly higher than that in B. kansuensis(P<0. 05). Considering these results,further research is necessary to reveal the pharmacological activities of bufotenidine and the pharmacodynamic differences between the three species. The results could provide a reference for quality control,the basic research on effective substances,and development of Berberidis Cortex.


Subject(s)
Berberine , Berberis , Chemistry , Classification , Chromatography, High Pressure Liquid , Phytochemicals , Plant Extracts
7.
Article in Chinese | WPRIM | ID: wpr-776497

ABSTRACT

OBJECTIVE@#To investigate the effects of berberine on learning and memory ability in vascular cognitive impairment rats.@*METHODS@#Sixty-eight Wistar rats were randomly divided into control group (n=10), sham operated group (n=10) and the modeling group of vascular cognitive impairment rat (n=48), then the rats in modeling group were randomly divided into four groups (n=10): vehicle group, berberine low dose group (20 mg/kg), medium dose group (40 mg/kg) and high dose group (60 mg/kg). Bilateral common carotid arteries were occluded in rats to establish vascular cognitive impairment (VCI) model. Different doses of berberine were intraperitoneally injected into the treatment group and normal saline was intraperitoneally injected into the other groups once a day for a total of 34 days. After 28 days of administration, Morris water maze was used to test the learning and memory ability of rats. After the water maze experiment, the levels of superoxide dismutase (SOD) activity, glutathione (GSH), malondialdehyde (MDA), tumor necrosis factor alpha(TNF-α), interleukin-1 beta (IL-1β), 5-hydroxytryptamine (5-HT) and monoamine oxidase (MAO) in the forebrain cortex were detected.@*RESULTS@#Compared to sham group, the escape latency in VCI group was significantly extended (P<0.01) and the times of passing through the platform were decreased remarkably (P<0.01). The levels of SOD, GSH and 5-HT in the hippocampus or anterior cortex were decreased significantly (P<0.01), while the contents of MDA, TNF-α, IL-1β and MAO were increased remarkably (P<0.01). Compared with VCI group, the escape latency in berberine-treated groups was shortened significantly (P<0.01, P<0.05) and the times of passing through the platform were increased remarkably (P<0.01, P<0.05), the levels of SOD, GSH and 5-HT were increased significantly (P<0.01), while the contents of TNF-α, IL-1β and MAO were decreased remarkably (P<0.01).@*CONCLUSION@#Berberine could significantly improve the spatial learning and memory abilities of rats with vascular cognitive impairment. The mechanism may be related to the effects of berberine on the hippocampal antioxidant stress, anti-inflammatory response and the monoamine neurotransmitter system in the forebrain cortex. Berberine 60 mg/kg dose group had better effect.


Subject(s)
Animals , Berberine , Pharmacology , Cognitive Dysfunction , Drug Therapy , Hippocampus , Inflammation , Maze Learning , Memory , Oxidative Stress , Random Allocation , Rats , Rats, Sprague-Dawley , Rats, Wistar
8.
Article in English | WPRIM | ID: wpr-713701

ABSTRACT

PURPOSE: The exact mechanism regulating fibronectin (FN) expression in breast cancer cells has not been fully elucidated. In this study, we investigated the pharmacological mechanism of berberine (BBR) with respect to FN expression in triple-negative breast cancer (TNBC) cells. METHODS: The clinical significance of FN mRNA expression was analyzed using the Kaplan-Meier plotter database (http://kmplot.com/breast). FN mRNA and protein expression levels were analyzed by real-time polymerase chain reaction and western blotting, respectively. RESULTS: Using publicly available clinical data, we observed that high FN expression was associated with poor prognosis in patients with breast cancer. FN mRNA and protein expression was increased in TNBC cells compared with non-TNBC cells. As expected, recombinant human FN significantly induced cell spreading and adhesion in MDA-MB231 TNBC cells. We also investigated the regulatory mechanism underlying FN expression. Basal levels of FN mRNA and protein expression were downregulated by a specific activator protein-1 (AP-1) inhibitor, SR11302. Interestingly, FN expression in TNBC cells was dose-dependently decreased by BBR treatment. The level of c-Jun phosphorylation was also decreased by BBR treatment. CONCLUSION: Our findings demonstrate that FN expression is regulated via an AP-1–dependent mechanism, and that BBR suppresses FN expression in TNBC cells through inhibition of AP-1 activity.


Subject(s)
Berberine , Blotting, Western , Breast Neoplasms , Breast , Cell Adhesion , Fibronectins , Humans , Phosphorylation , Prognosis , Real-Time Polymerase Chain Reaction , RNA, Messenger , Transcription Factor AP-1 , Triple Negative Breast Neoplasms
9.
Article in Chinese | WPRIM | ID: wpr-775372

ABSTRACT

To investigate the hypoglycemic effects of baicalin, berberine, puerarin and liquiritin on the insulin resistance (IR) cells. The IR model of HepG2 cells was established by treatment with insulin and dexamethasone for 48 h. Glucose uptake, glycogen content and cell viability were detected with different concentrations of baicalin, berberine, puerarin, liquiritin in IR-HepG2 cells. Compared with IR model group, all of intervened groups significantly increased the glucose consumption, except for liquiritin groups and 1 μmol·L⁻¹ baicalin group. Moreover, 10, 20, 50 μmol·L⁻¹ baicalin, 5, 10, 20, 50 μmol·L⁻¹ berberine and 40, 80, 160 μmol·L⁻¹ puerarin significantly elevated glycogen content in IR-HepG2 cells. Liquiritin did not show obvious hypoglycemic effect. Compared with normal group, the mRNA expression levels of GLUT1 and GLUT4 were decreased in IR-HepG2 cells according to qPCR results. 5, 20 μmol·L⁻¹ berberine decreased the mRNA expression level of GLUT1 in IR-HepG2 cells, whereas 20, 40, 80 μmol·L⁻¹ puerarin significantly elevated the mRNA expression level of GLUT1. Moreover, 10, 20, 50 μmol·L⁻¹ baicalin and 20 μmol·L⁻¹ berberine increased the mRNA expression level of GLUT4. Whereas, 40, 80 μmol·L⁻¹ puerarin decreased the mRNA expression level of GLUT4. Western blot results suggested that 10, 20, 50 μmol·L⁻¹ baicalin significantly increased the protein expressions of GLUT2 and GLUT4, whereas 20, 40, 80 μmol·L⁻¹ puerarin significantly up-regulated GLUT1 and GLUT2 proteins. In addition, 20 μmol·L⁻¹ berberine increased the protein expressions of GLUT2 and GLUT4, whereas 10 μmol·L⁻¹ berberine up-regulated GLUT4 expression. The results preliminarily suggested that baicalin, berberine and puerarin have differentiated hypoglycemic effects, which accelerate glucose transport, increase glycogen synthesis, regulate glucose metabolism and improve hepatic IR.


Subject(s)
Berberine , Pharmacology , Flavonoids , Pharmacology , Glucose , Hep G2 Cells , Humans , Hypoglycemic Agents , Pharmacology , Insulin , Insulin Resistance , Isoflavones , Pharmacology
10.
Article in English | WPRIM | ID: wpr-773562

ABSTRACT

A series of berberine derivatives were synthesized by introducing substituted benzyl groups at C-9. All these synthesized compounds (4a-4m) were screened for their in vitro antibacterial activity against four Gram-positive bacteria and four Gram-negative bacteria and evaluated for their antifungal activity against three pathogenic fungal strains. All these compounds displayed good antibacterial and antifungal activities, compared to reference drugs including Ciprofloxacin and Fluconazole; Compounds 4f, 4g, and 4l showed the highest antibacterial and antifungal activities. Moreover, all the synthesized compounds were docked into topoisomerase II-DNA complex, which is a crucial drug target for the treatment of microbial infections. Docking results showed that H-bond, π-π stacked, π-cationic, and π-anionic interactions were responsible for the strong binding of the compounds with the target protein-DNA complex.


Subject(s)
Anti-Bacterial Agents , Chemistry , Pharmacology , Antifungal Agents , Chemistry , Pharmacology , Bacteria , Berberine , Chemistry , Pharmacology , Drug Design , Fungi , Molecular Docking Simulation , Structure-Activity Relationship
11.
Article in English | WPRIM | ID: wpr-758866

ABSTRACT

Bacterial biofilms have been demonstrated to be closely related to clinical infections and contribute to drug resistance. Berberine, which is the main component of Coptis chinensis, has been reported to have efficient antibacterial activity. This study aimed to investigate the potential effect of a combination of berberine with ciprofloxacin (CIP) to inhibit Salmonella biofilm formation and its effect on expressions of related genes (rpoE, luxS, and ompR). The fractional inhibitory concentration (FIC) index of the combination of berberine with CIP is 0.75 showing a synergistic antibacterial effect. The biofilm's adhesion rate and growth curve showed that the multi-resistant Salmonella strain had the potential to form a biofilm relative to that of strain CVCC528, and the antibiofilm effects were in a dose-dependent manner. Biofilm microstructures were rarely observed at 1/2 × MIC/FIC concentrations (MIC, minimal inhibition concentration), and the combination had a stronger antibiofilm effect than each of the antimicrobial agents used alone at 1/4 × FIC concentration. LuxS, rpoE, and ompR mRNA expressions were significantly repressed (p < 0.01) at 1/2 × MIC/FIC concentrations, and the berberine and CIP combination repressed mRNA expressions more strongly at the 1/4 × FIC concentration. The results indicate that the combination of berberine and CIP has a synergistic effect and is effective in inhibiting Salmonella biofilm formation via repression of luxS, rpoE, and ompR mRNA expressions.


Subject(s)
Anti-Infective Agents , Berberine , Biofilms , Ciprofloxacin , Coptis , Drug Combinations , Drug Resistance , Drug Resistance, Multiple , Repression, Psychology , RNA, Messenger , Salmonella
12.
Article in English | WPRIM | ID: wpr-812351

ABSTRACT

A series of berberine derivatives were synthesized by introducing substituted benzyl groups at C-9. All these synthesized compounds (4a-4m) were screened for their in vitro antibacterial activity against four Gram-positive bacteria and four Gram-negative bacteria and evaluated for their antifungal activity against three pathogenic fungal strains. All these compounds displayed good antibacterial and antifungal activities, compared to reference drugs including Ciprofloxacin and Fluconazole; Compounds 4f, 4g, and 4l showed the highest antibacterial and antifungal activities. Moreover, all the synthesized compounds were docked into topoisomerase II-DNA complex, which is a crucial drug target for the treatment of microbial infections. Docking results showed that H-bond, π-π stacked, π-cationic, and π-anionic interactions were responsible for the strong binding of the compounds with the target protein-DNA complex.


Subject(s)
Anti-Bacterial Agents , Chemistry , Pharmacology , Antifungal Agents , Chemistry , Pharmacology , Bacteria , Berberine , Chemistry , Pharmacology , Drug Design , Fungi , Molecular Docking Simulation , Structure-Activity Relationship
13.
Biol. Res ; 51: 9, 2018. graf
Article in English | LILACS | ID: biblio-950895

ABSTRACT

BACKGROUND: Diabetic nephropathy (DN) is the leading cause of end-stage renal failure, contributing to severe morbidity and mortality in diabetic patients. Berberine (BBR) has been well characterized to exert renoprotective effects in DN progression. However, the action mechanism of BBR in DN remains to be fully understood. METHODS: The DN rat model was generated by intraperitoneal injection of streptozotocin (STZ, 65 mg/kg body weight) while 30 mM high glucose (HG)-treated podocytes were used as an in vitro DN model. The fasting blood glucose level and ratio of kidney weight to body weight were measured after BBR treatment (50, 100, or 200 mg/kg) in STZ-induced DN rats. The renal injury parameters including 24-h urinary protein, blood urea nitrogen and serum creatinine were assessed. qRT-PCR was performed to detect the transcript amounts of inflammatory factors. The concentrations of inflammatory factors were evaluated by ELISA kits. Western blot analysis was conducted to measure the amounts of TLR4/NF-κB-related proteins. The apoptotic rate of podocytes was analyzed by flow cytometry using Annexin V/propidium iodide. RESULTS: Berberine reduced renal injury in STZ-induced DN rat model, as evidenced by the decrease in fasting blood glucose, ratio of kidney weight to body weight, 24-h urinary protein, serum creatinine, and blood urine nitrogen. BBR attenuated the systemic and renal cortex inflammatory response and inhibited TLR4/NF-κB pathway in STZ-induced DN rats and HG-induced podocytes. Also, HG-induced apoptosis of podocytes was lowered by BBR administration. Furthermore, blockade of TLR4/NF-κB pathway by resatorvid (TAK-242) or pyrrolidine dithiocarbamate aggravated the inhibitory effect of BBR on HG-induced inflammatory response and apoptosis in podocytes. CONCLUSIONS: Berberine ameliorated DN through relieving STZ-induced renal injury, inflammatory response, and podocyte HG-induced apoptosis via inactivating TLR4/NF-κB pathway.


Subject(s)
Animals , Male , Rats , Berberine/pharmacology , Signal Transduction/drug effects , NF-kappa B/antagonists & inhibitors , Diabetes Mellitus, Experimental/drug therapy , Diabetic Nephropathies/drug therapy , Toll-Like Receptor 4/antagonists & inhibitors , Rats, Sprague-Dawley
14.
Article in English | WPRIM | ID: wpr-728623

ABSTRACT

Post-traumatic stress disorder (PTSD) is a trauma-induced psychiatric disorder characterized by impaired fear extermination, hyperarousal, anxiety, depression, and amnesic symptoms that may involve the release of monoamines in the fear circuit. The present study measured several anxiety-related behavioral responses to examine the effects of berberine (BER) on symptoms of anxiety in rats after single prolonged stress (SPS) exposure, and to determine if BER reversed the dopamine (DA) dysfunction. Rats received BER (10, 20, or 30 mg/kg, intraperitoneally, once daily) for 14 days after SPS exposure. BER administration significantly increased the time spent in the open arms and reduced grooming behavior during the elevated plus maze test, and increased the time spent in the central zone and the number of central zone crossings in the open field test. BER restored neurochemical abnormalities and the SPS-induced decrease in DA tissue levels in the hippocampus and striatum. The increased DA concentration during BER treatment may partly be attributed to mRNA expression of tyrosine hydroxylase and the DA transporter in the hippocampus, while BER exerted no significant effects on vesicular monoamine transporter mRNA expression in the hippocampus of rats with PTSD. These results suggest that BER had anxiolytic-like effects on behavioral and biochemical measures associated with anxiety. These findings support a role for reduced anxiety altered DAergic transmission and reduced anxiety in rats with PTSD. Thus, BER may be a useful agent to treat or alleviate psychiatric disorders like those observed in patients with PTSD.


Subject(s)
Animals , Anxiety , Arm , Berberine , Depression , Dopamine , Grooming , Hippocampus , Humans , Rats , RNA, Messenger , Stress Disorders, Post-Traumatic , Tyrosine 3-Monooxygenase , Vesicular Monoamine Transport Proteins
15.
Article in English | WPRIM | ID: wpr-812125

ABSTRACT

Heat stress can stimulate an increase in body temperature, which is correlated with increased expression of heat shock protein 70 (HSP70) and tumor necrosis factor α (TNFα). The exact mechanism underlying the HSP70 and TNFα induction is unclear. Berberine (BBR) can significantly inhibit the temperature rise caused by heat stress, but the mechanism responsible for the BBR effect on HSP70 and TNFα signaling has not been investigated. The aim of the present study was to explore the relationship between the expression of HSP70 and TNFα and the effects of BBR under heat conditions, using in vivo and in vitro models. The expression levels of HSP70 and TNFα were determined using RT-PCR and Western blotting analyses. The results showed that the levels of HSP70 and TNFα were up-regulated under heat conditions (40 °C). HSP70 acted as a chaperone to maintain TNFα homeostasis with rising the temperature, but knockdown of HSP70 could not down-regulate the level of TNFα. Furthermore, TNFα could not influence the expression of HSP70 under normal and heat conditions. BBR targeted both HSP70 and TNFα by suppressing their gene transcription, thereby decreasing body temperature under heat conditions. In conclusion, BBR has a potential to be developed as a therapeutic strategy for suppressing the thermal effects in hot environments.


Subject(s)
Animals , Berberine , Pharmacology , HSP70 Heat-Shock Proteins , Genetics , Metabolism , Heat Stress Disorders , Drug Therapy , Genetics , Metabolism , Hot Temperature , Humans , Male , Mice , Mice, Inbred ICR , TATA Box , Tumor Necrosis Factor-alpha , Genetics , Metabolism
16.
AJMB-Avicenna Journal of Medical Biotechnology. 2017; 9 (1): 2-7
in English | IMEMR | ID: emr-185805

ABSTRACT

Background: Related Multidrug Resistance [MDR] to efflux pumps is a significant problem in treating infections caused by Pseudomonas aeruginosa [P. aeruginosa]. Plant compounds have been identified as Pump Inhibitors [EPIs]. In the current study, the potential effect of Berberine and Palmatine as EPIs were investigated on efflux pump inhibition through focusing on different gene patterns in P. aeruginosa isolated from burn infections


Methods: All isolates were collected and identified using the standard biochemical tests. Antimicrobial sensitivity was performed based on disk agar diffusion method for 12 antibiotics. MIC-MBC tests were also performed based on the broth microdilution method to detect synergistic relationship between ciprofloxacin, Berberine and Palmatine. Detection of mexA, mexB, mexC, mexD, mexE, mexF and mexX was conducted by PCR assay. Fisher's Exact test and Logistic Regression were used as statistical tools


Results: A total of 60 P. aeruginosa isolates were collected. The highest and lowest levels of resistance were found to be respectively against clindamycin and tigecycline. Comparing the MIC with MBC distribution, it was found that Berberine and Palmatine lower the MIC-MBC level of ciprofloxacin. The PCR results indicated that the highest frequency is about MexAB-OprM operon. The statistical analysis among different gene patterns of efflux pumps showed that there were no significant relationships between the effectiveness of Berberine and Palmatine [p>0.05]


Conclusion: It can be speculated that Berberine and Palmatine both act as EPIs and can be used as auxiliary treatments with the purpose of increasing the effect of available antibiotics as well as decreasing the emergence of MDR bacteria. The efficiency of these combinations should be studied further under in vivo conditions to have a more comprehensive conclusion regarding this issue


Subject(s)
Pseudomonas aeruginosa/genetics , Genes, MDR/drug effects , Berberine/therapeutic use , Plant Extracts/therapeutic use , Berberine Alkaloids , Iran
17.
Article in English | WPRIM | ID: wpr-812595

ABSTRACT

The present study aimed at determining whether berberine can enhance the antidiabetic effects and alleviate the adverse effects of canagliflozin in diabetes mellitus. Streptozotocin-induced diabetic mice were introduced, and the combined effects of berberine and canagliflozin on glucose metabolism and kidney functions were investigated. Our results showed that berberine combined with canagliflozin (BC) increased reduction of fasting and postprandial blood glucose, diet, and water intake compared with berberine or canagliflozin alone. Interestingly, BC showed greater decrease in blood urea nitrogen and creatinine levels and lower total urine glucose excretion than canagliflozin alone. In addition, BC showed increased phosphorylated 5' AMP-activated protein kinase (pAMPK) expression and decreased tumor necrosis factor alpha (TNFα) levels in kidneys, compared with berberine or canagliflozin alone. These results indicated that BC was a stronger antidiabetic than berberine or canagliflozin alone with less negative side effects on the kidneys in the diabetic mice. The antidiabetic effect was likely to be mediated by synergically promoting the expression of pAMPK and reducing the expression of TNFα in kidneys. The present study represented the first report that canagliflozin combined with berberine was a promising treatment for diabetes mellitus. The exact underlying mechanisms of action should be investigated in future studies.


Subject(s)
AMP-Activated Protein Kinases , Metabolism , Animals , Berberine , Blood Glucose , Metabolism , Canagliflozin , Diabetes Mellitus, Experimental , Drug Therapy , Metabolism , Drug Therapy, Combination , Drugs, Chinese Herbal , Humans , Hypoglycemic Agents , Insulin , Metabolism , Kidney , Metabolism , Male , Mice , Streptozocin
18.
Fortaleza; s.n; 2016. 67 p. ilus.
Thesis in Portuguese | LILACS | ID: biblio-971926

ABSTRACT

Atualmente, a incidência de infecções fúngicas tem aumentado significativamente,contribuindo assim para morbidade e mortalidade. Esse fato que tem como umas das principais causas o aumento da resistência antimicrobiana, estando associado à produção de biofilme que tem um elevado nível de resistência antimicrobiana juntamente com o arsenal farmacológico antifúngico limitado, quando comparado ao arsenal antibacteriano, leva a necessidade do desenvolvimento de novas estratégias terapêuticas. A berberina tem demonstrado ter ampla atividade antibacteriana e antifúngica. Dentro desse contexto, o objetivo foi avaliar o potencial antifúngico da berberina frente às cepas de Candida spp. e Cryptococcus neo formans resistentes ao fluconazol, bem como avaliar o efeito da berberina frente às cepas de Candida spp...


Currently, the incidence of fungal infections has increased significantly, contributing tomorbidity and mortality. It has as one of its main causes the increase of antibiotic resistance.Recently associated with biofilm production, which has a high level of antibiotic resistance,coupled with the limited antifungal pharmacological when compared to antibacterial, it leadsto the need for the development of new therapeutic strategies. The berberine has shown tohave broad antibacterial and antifungal activity. In this context, the objective was to evaluatethe antifungal potential of berberine against strains of Candida spp. and Cryptococcusneoformans resistant to fluconazole and evaluate the effect of berberine against strains ofCandida tropicalis in biofilm formation. The evaluation of the antifungal effect wasdetermined by microdilution in broth (M27-A3) and by flow cytometry techniques, in whichthe likely mechanism of action of that compound was evaluated. For the assessment of thebiofilm, a colorimetric assay (MTT) was used to determine the susceptibility of sessile cells.Strains of Candida spp...


Subject(s)
Humans , Candida , Cryptococcus neoformans , Biofilms , Berberine
19.
Article in English | WPRIM | ID: wpr-310875

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the effects of berberine (BBR) and cinnamic acid (CA), the main active components in Jiaotai Pill (, JTP), on palmitic acid (PA)-induced intracellular triglyceride (TG) accumulation in NIT-1 pancreatic β cells.</p><p><b>METHODS</b>Cells were incubated in culture medium containing PA (0.25 mmol/L) for 24 h. Then treatments with BBR (10 μmol/L), CA (100 μmol/L) and the combination of BBR and CA (BBR+CA) were performed respectively. Intracellular lipid accumulation was assessed by Oil Red O staining and TG content was measured by colorimetric assay. The expression of adenosine monophosphate-activated protein kinase (AMPK) protein and its downstream lipogenic and fatty acid oxidation genes, including fatty acid synthase (FAS), acetyl-coA carboxylase (ACC), phosphorylation acetyl-coA carboxylase (pACC), carnitine acyl transferase 1 (CPT-1) and sterol regulating element binding protein 1c (SREBP-1c) were determined by Western blot or real time polymerase chain reaction.</p><p><b>RESULTS</b>PA induced an obvious lipid accumulation and a significant increase in intracellular TG content in NIT-1 cells. PA also induced a remarkable decrease in AMPK protein expression and its downstream targets such as pACC and CPT-1. Meanwhile, AMPK downstream lipogenic genes including SREBP-1c mRNA, FAS and ACC protein expressions were increased. Treatments with BBR and BBR+CA, superior to CA, significantly reversed the above genes changes in NIT-1 pancreatic β cells. However, the synergistic effect of BBR and CA on intracellular TG content was not observed in the present study.</p><p><b>CONCLUSION</b>It can be concluded that in vitro, BBR and BBR+CA could inhibit PA-induced lipid accumulation by decreasing lipogenesis and increasing lipid oxidation in NIT-1 pancreatic β cells.</p>


Subject(s)
AMP-Activated Protein Kinases , Metabolism , Animals , Berberine , Chemistry , Pharmacology , Cell Line , Cinnamates , Chemistry , Pharmacology , Fatty Acids , Metabolism , Gene Expression Regulation , Insulin-Secreting Cells , Metabolism , Intracellular Space , Metabolism , Lipogenesis , Genetics , Mice , Oxidation-Reduction , Palmitic Acid , Toxicity , Triglycerides , Metabolism
20.
Article in English | WPRIM | ID: wpr-285310

ABSTRACT

Berberine (BBR) is an isoquinoline alkaloid extracted from Rhizoma coptidis and has been used for treating type 2 diabetes mellitus (T2DM) in China. The development of T2DM is often associated with insulin resistance and impaired glucose uptake in peripheral tissues. In this study, we examined whether BBR attenuated glucose uptake dysfunction through the cholinergic anti-inflammatory pathway in HepG2 cells. Cellular glucose uptake, quantified by the 2-[N-(7-Nitrobenz-2-oxa-1,3-diazol-4-yl)-amino]-2-deoxy-D-glucose (2-NBDG), was inhibited by 21% after HepG2 cells were incubated with insulin (10(-6) mol/L) for 36 h. Meanwhile, the expression of alpha7 nicotinic acetylcholine receptor (α7nAChR) protein was reduced without the change of acetylcholinesterase (AChE) activity. The level of interleukin-6 (IL-6) in the culture supernatant, the ratio of phosphorylated I-kappa-B kinase-β (IKκβ) Ser181/IKKβ and the expression of nuclear factor-kappa B (NF-κB) p65 protein were also increased. However, the treatment with BBR enhanced the glucose uptake, increased the expression of α7nAChR protein and inhibited AChE activity. These changes were also accompanied with the decrease of the ratio of pIKKβ Ser181/IKKβ, NF-κB p65 expression and IL-6 level. Taken together, these results suggest that BBR could enhance glucose uptake, and relieve insulin resistance and inflammation in HepG2 cells. The mechanism may be related to the cholinergic anti-inflammatory pathway and the inhibition of AChE activity.


Subject(s)
Berberine , Pharmacology , Glucose , Metabolism , Hep G2 Cells , Humans , Hypoglycemic Agents , Pharmacology , I-kappa B Kinase , Metabolism , I-kappa B Proteins , Metabolism , Insulin , Metabolism , Insulin Resistance , Interleukin-6 , Metabolism , Transcription Factor RelA , Metabolism , alpha7 Nicotinic Acetylcholine Receptor , Genetics , Metabolism
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