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1.
Shanghai Kou Qiang Yi Xue ; 30(3): 258-262, 2021 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-34476441

RESUMO

PURPOSE: This study aimed at exploring the effect of berberine (C20H18NO4) on osteogenic differentiation of rat adipose-derived stem cells(ADSCs) and clarifying the related mechanism. METHODS: ADSCs were subjected to 5, 10, 20 µmol/L berberine culture solution. The untreated ADSCs were set as the control group. Cell proliferation activity was determined by MTT method. Alkaline phosphatase (ALP) staining, semi-quantitative assay and alizarin red staining (ARS) were applied to analyze the effect of berberine on osteogenic differentiation of ADSCs. The phosphorylation level of c-Jun amino terminal kinase (JNK) protein was tested by Western blot. Runx2, OCN were tested by Western blot before and after application of JNK pathway inhibitor SP600125. SPSS 22.0 software package was used for statistical analysis. RESULTS: There was no significant difference on cell proliferation activity of ADSCs treated with 5, 10 and 20 µmol/L berberine at 1, 3 and 7 day(P>0.05). ALP staining and ARS staining in groups treated by berberine were significantly darker than those of the control group, and ALP protein secretion in the experimental group was significantly up-regulated (P<0.05). The phosphorylation level of JNK was increased after treated with 10 µmol/L berberine culture medium. The expression of osteogenic related proteins Runx2 and OCN was up-regulated in the experimental group. After inhibition of JNK signaling pathway, the expression of Runx2 and OCN was down-regulated. CONCLUSIONS: Berberine has no effect on cell proliferation of ADSCs, and can up-regulate osteogenic differentiation of ADSCs through activation of JNK signaling pathway.


Assuntos
Berberina , Osteogênese , Animais , Berberina/farmacologia , Diferenciação Celular , Células Cultivadas , Sistema de Sinalização das MAP Quinases , Ratos , Células-Tronco
2.
Zhongguo Zhong Yao Za Zhi ; 46(16): 4201-4207, 2021 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-34467733

RESUMO

The present study aims to investigate the effects of the main components(aesculin, berberine hydrochloride, and anemoside B4) in the butyl alcohol extract of Baitouweng Decoction(BAEB) on the chemotaxis of neutrophils induced by dimethyl sulfoxide(DMSO). HL60 cells were cultivated in RPMI-1640 complete medium, and transferred into a 6-well plate(2 × 10~5 per mL) with 4 mL in each well, followed by incubation with DMSO at 1.3% for five days. The morphologic changes of cells were observed under an inverted microscope. The CD11 b expression after DMSO induction was analyzed by flow cytometry. The effects of aesculin, berberine hydrochloride, and anemoside B4 on the cell proliferation and migration were detected by CCK8 assay and Transwell assay, respectively. The effects of the main components on the production and polarization of F-actin protein were also examined by flow cytometry and laser confocal microscopy. PI3 K/Akt signaling pathway was checked by Western blot. As revealed by the results, neutrophil-like HL60 cells were observed after DMSO induction. The CD11 b expression in these cells increased significantly as indicated by the flow cytometry. Additionally, 100 µg·mL~(-1) aesculin, 8 µg·mL~(-1) berberine hydrochloride, and 80 µg·mL~(-1) anemoside B4 were potent in inhibiting the migration of neutrophils and reducing F-actin expression. Berberine hydrochloride was verified to be capable of diminishing phosphorylated PI3 K/Akt protein expression. The findings indicate that aesculin, anemoside B4, and especially berberine hydrochloride in the BAEB can inhibit the chemotaxis of neutrophils, which is possibly achieved by the inhibition of F-actin and PI3 K/Akt signaling pathway.


Assuntos
Berberina , Medicamentos de Ervas Chinesas , 1-Butanol , Berberina/farmacologia , Quimiotaxia , Medicamentos de Ervas Chinesas/farmacologia , Neutrófilos
3.
Gynecol Obstet Invest ; 86(4): 388-397, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34515131

RESUMO

OBJECTIVES: The aim of this study was to investigate the effects of berberine on polycystic ovary syndrome (PCOS) with insulin resistance (IR). DESIGN: This study performed 16S rRNA sequencing and metabolomic analysis on dehydroepiandrosterone (DHEA)-induced PCOS rats treated with berberine, focusing on the improvement of PCOS-IR by modifying gut microbiota and metabolism. METHODS: Forty-two female Sprague Dawley rats were randomly divided into 4 experimental groups of 8 rats each (PCOS + HFD, PCOS + HFD + BBR, NCD + PCOS, and NCD + PCOS + BBR groups). Homeostasis model assessment of insulin resistance (HOMA-IR) index-related indicators and hormone level in serum were analyzed. 16S rRNA sequencing and metabolomic analysis were performed on DHEA-induced PCOS rats treated with berberine. In addition, the differential microbiotas and metabolites were screened. Also, enrichment analysis was carried out on the differential metabolites. Finally, we constructed a correlation network to analyze the correlation between differential microbiotas and metabolites. RESULTS: Firmicutes and Bacteroidetes were changed at the phylum level, and Romboutsia, Bacteroides, and Clostridium_sensu_stricto_1 were changed at the genus level after berberine treatment. In addition, a total of 26 differential operational taxonomic units and 3 metabolites (glutamine, unsaturated acids [CH = CH], and glucose) between 2 groups were obtained. Moreover, these metabolites were mainly involved in type 2 diabetes mellitus, 2-component system, and ABC transporter Kyoto Encyclopedia of Genes and Genomes pathways. And, 3 microbiotas (Lachnospiraceae_NC2004_group, Flavonifractor, and Parasutterella) were regulated by glucose and glutamine. LIMITATIONS: The sample size involved in this study is relatively small. In addition, relevant experiments need to be performed to verify the obtained results from this study, and in-depth functional studies are needed. CONCLUSIONS: Berberine is effective in improving the pathological condition in PCOS by regulating the gut microbiotas and metabolites. This study will provide evidence for therapeutic efforts to treat PCOS-IR using berberine.


Assuntos
Berberina , Diabetes Mellitus Tipo 2 , Microbioma Gastrointestinal , Resistência à Insulina , Síndrome do Ovário Policístico , Animais , Berberina/farmacologia , Desidroepiandrosterona , Feminino , Humanos , Síndrome do Ovário Policístico/induzido quimicamente , Síndrome do Ovário Policístico/tratamento farmacológico , RNA Ribossômico 16S/genética , Ratos , Ratos Sprague-Dawley
4.
Life Sci ; 284: 119928, 2021 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-34480937

RESUMO

AIMS: Berberine is effective for type 2 diabetes mellitus (T2DM), but has limited use in clinic. This study aims to evaluate the effect of berberine combined with stachyose on glycolipid metabolism and gut microbiota and to explore the underlying mechanisms in diabetic rats. MAIN METHODS: Zucker diabetic fatty (ZDF) rats were orally administered berberine, stachyose and berberine combined with stachyose once daily for 69 days. The oral glucose tolerance and levels of blood glucose, insulin, triglyceride and total cholesterol were determined. The gut microbial profile, colonic miRNA and gene expression were assayed using Illumina sequencing. The quantitative polymerase chain reaction was used to verify the expression of differentially expressed miRNAs and genes. KEY FINDINGS: Repeated treatments with berberine alone and combined with stachyose significantly reduced the blood glucose, improved the impaired glucose tolerance, and increased the abundance of beneficial Akkermansiaceae, decreased that of pathogenic Enterobacteriaceae in ZDF rats. Furthermore, combined treatment remarkably decreased the abundances of Desulfovibrionaceae and Proteobacteria in comparison to berberine. Combined treatment evidently decreased the expression of intestinal early growth response protein 1 (Egr1) and heparin-binding EGF-like growth factor (Hbegf), and significantly increased the expression of miR-10a-5p, but berberine alone not. SIGNIFICANCE: Berberine combined with stachyose significantly improved glucose metabolism and reshaped gut microbiota in ZDF rats, especially decreased the abundance of pathogenic Desulfovibrionaceae and Proteobacteria compared to berberine alone, providing a novel strategy for treating T2DM. The underlying mechanisms may be associated with regulating the expression of intestinal Egr1, Hbegf and miR-10a-5p, but remains further elucidation.


Assuntos
Berberina/farmacologia , Colo/metabolismo , Diabetes Mellitus Experimental/genética , Microbioma Gastrointestinal , Regulação da Expressão Gênica , Glucose/metabolismo , MicroRNAs/genética , Oligossacarídeos/farmacologia , Animais , Colo/efeitos dos fármacos , Colo/microbiologia , Diabetes Mellitus Experimental/microbiologia , Diabetes Mellitus Tipo 2/sangue , Diabetes Mellitus Tipo 2/genética , Microbioma Gastrointestinal/efeitos dos fármacos , Microbioma Gastrointestinal/genética , Perfilação da Expressão Gênica , Regulação da Expressão Gênica/efeitos dos fármacos , Masculino , MicroRNAs/metabolismo , Análise de Componente Principal , Ratos Zucker , Reprodutibilidade dos Testes , Transcriptoma/genética
5.
Nat Commun ; 12(1): 5503, 2021 09 17.
Artigo em Inglês | MEDLINE | ID: mdl-34535644

RESUMO

Non-alcoholic steatohepatitis is frequently associated with diabetes and may cause progressive liver disease. Current treatment options are limited. Here we report on a prospective, randomised, double-blind, placebo-controlled trial of two doses of HTD1801 (berberine ursodeoxycholate, an ionic salt of berberine and ursodeoxycholic acid), versus placebo that was conducted in 100 subjects with fatty liver disease and diabetes (NCT03656744). Treatment was for 18 weeks with a primary endpoint of reduction in liver fat content measured by magnetic resonance imaging proton density fat fraction. Key secondary endpoints included improvement in glycemic control, liver-associated enzymes and safety. The pre-specified primary endpoint was met. Thus, subjects receiving 1000 mg twice a day of berberine ursodeoxycholate had significantly greater reduction in liver fat content than in placebo recipients (mean absolute decrease -4.8% vs. -2.0% (p = 0.011). Compared to placebo, subjects receiving this dose also experienced significant improvement in glycemic control as well as reductions in liver-associated enzymes and significant weight loss. Diarrhea and abdominal discomfort were the most frequently reported adverse events. We conclude that berberine ursodeoxycholate has a broad spectrum of metabolic activity in patients with presumed NASH and diabetes. It is relatively well tolerated and merits further development as a treatment for NASH with diabetes.


Assuntos
Berberina/uso terapêutico , Diabetes Mellitus Tipo 2/complicações , Diabetes Mellitus Tipo 2/tratamento farmacológico , Hepatopatia Gordurosa não Alcoólica/complicações , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Estudo de Prova de Conceito , Adiposidade/efeitos dos fármacos , Adulto , Idoso , Berberina/efeitos adversos , Berberina/farmacologia , Feminino , Hemoglobina A Glicada/análise , Humanos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Masculino , Pessoa de Meia-Idade
6.
Int J Mol Sci ; 22(18)2021 Sep 13.
Artigo em Inglês | MEDLINE | ID: mdl-34576028

RESUMO

Lung cancer is one of the most common cancers and the leading cause of death in humans worldwide. Non-small-cell lung cancer (NSCLC) accounts for approximately 85% of lung cancer cases and is often diagnosed at a late stage. Among patients with NSCLC, 50% die within 1 year after diagnosis. Even with clinical intervention, the 5-year survival rate is only approximately 20%. Therefore, the development of an advanced therapeutic strategy or novel agent is urgently required for treating NSCLC. Berberine exerts therapeutic activity toward NSCLC; therefore, its activity as an antitumor agent needs to be explored further. In this study, three terpenylated-bromide derivatives of berberrubine were synthesized and their anti-NSCLC activities were evaluated. Each derivative had higher anti-NSCLCs activity than berberrubine and berberine. Among them, 9-O-gernylberberrubine bromide (B4) and 9-O-farnesylberberrubine bromide (B5) showed greater growth inhibition, cell-cycle regulation, in vitro tumorigenesis suppression, and tumor migration reduction. In addition, some degree of apoptosis and autophagic flux blocking was noted in the cells under B4 and B5 treatments. Our study demonstrates that the berberrubine derivatives, B4 and B5, exhibit impressive anti-NSCLC activities and have potential for use as chemotherapeutic agents against NSCLC.


Assuntos
Berberina/análogos & derivados , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Células A549 , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Berberina/síntese química , Berberina/química , Berberina/farmacologia , Brometos/química , Carcinogênese/efeitos dos fármacos , Carcinoma Pulmonar de Células não Pequenas/patologia , Humanos , Terpenos/síntese química , Terpenos/farmacologia
7.
Molecules ; 26(16)2021 Aug 05.
Artigo em Inglês | MEDLINE | ID: mdl-34443321

RESUMO

Berberine (BBR), a plant alkaloid, is known for its therapeutic properties of anticancer, cardioprotective, antidiabetic, hypolipidemic, neuroprotective, and hepatoprotective activities. The present study was to determine the molecular mechanism of BBR's pharmacological activity in human monocytic (THP-1) cells induced by arachidonic acid (AA) or lipopolysaccharide (LPS). The effect of BBR on AA/LPS activated proinflammatory markers including TNF-α, MCP-1, IL-8 and COX-2 was measured by ELISA or quantitative real-time PCR. Furthermore, the effect of BBR on LPS-induced NF-κB translocation was determined by immunoblotting and confocal microscopy. AA/ LPS-induced TNF-α, MCP-1, IL-6, IL-8, and COX-2 markers were markedly attenuated by BBR treatment in THP-1 cells by inhibiting NF-κB translocation into the nucleus. Molecular modeling studies suggested the direct interaction of BBR to IKKα at its ligand binding site, which led to the inhibition of the LPS-induced NF-κB translocation to the nucleus. Thus, the present study demonstrated the anti-inflammatory potential of BBR via NF-κB in activated monocytes, whose interplay is key in health and in the pathophysiology of atherosclerotic development in blood vessel walls. The present study findings suggest that BBR has the potential for treating various chronic inflammatory disorders.


Assuntos
Anti-Inflamatórios/farmacologia , Berberina/farmacologia , Quinase I-kappa B/metabolismo , Lipopolissacarídeos/farmacologia , NF-kappa B/metabolismo , Linhagem Celular , Quimiocina CCL2/metabolismo , Ciclo-Oxigenase 2/metabolismo , Humanos , Interleucina-8/metabolismo , Transdução de Sinais/efeitos dos fármacos , Fator de Necrose Tumoral alfa/metabolismo
8.
Reprod Health ; 18(1): 171, 2021 Aug 18.
Artigo em Inglês | MEDLINE | ID: mdl-34407851

RESUMO

BACKGROUND: Multiple oral insulin-sensitizing agents, such as metformin, thiazolidinediones, inositols, and berberine, have been proven safe and efficacious in improving the endocrine, metabolic, and reproductive abnormalities seen in polycystic ovary syndrome (PCOS), providing more options for healthcare providers and patients. These oral insulin sensitizers are more convenient, practical, and economic than agents that need to be injected. A comparison of the clinical effectiveness of the four different classes of oral insulin sensitizers in PCOS has not been explored, leading to clinical uncertainty about the optimal treatment pathway. The present study aims to compare the effects of oral insulin sensitizers on endocrine and metabolic profiles in women with PCOS. METHODS: We identified randomized controlled trials for PCOS from a variety of databases, published from January 2005 to October 2020. Outcomes included changes in menstrual frequency, improvements in hyperandrogenism and glucolipid metabolism and adverse side effects. A random-effects network meta-analysis was performed. RESULTS: Twenty-two trials comprising 1079 patients with PCOS were included in this study. Compared with metformin, treatment with myo-inositol + D-chiro-inositol was associated with a greater improvement in menstrual frequency (odds ratio 14.70 [95% confidence interval (CI) 2.31-93.58]). Myo-inositol + D-chiro-inositol and metformin + thiazolidinediones combination therapies were superior to respective monotherapies in reducing total testosterone levels. Thiazolidinediones, metformin + thiazolidinediones, and myo-inositol + D-chiro-inositol were associated with a lower insulin resistance index (HOMA-IR) compared with that in metformin alone (mean differences: - 0.72 [95% CI (- 1.11)-(- 0.34)] to - 0.89 [95% CI (- 1.460)-(- 0.32)]). Metformin + thiazolidinediones treatment was associated with lower triglyceride levels compared with that in metformin and thiazolidinediones monotherapy, while thiazolidinediones was superior to metformin in increasing high-density lipoprotein cholesterol and decreasing fasting plasma glucose, triglycerides, low-density lipoprotein cholesterol, and gastrointestinal adverse events. CONCLUSIONS: Ours is the first study to report that for women with PCOS, myo-inositol combined with D-chiro-inositol and metformin combined with thiazolidinediones appear superior to metformin alone in improving insulin resistance and decreasing total testosterone. Myo-inositol combined with D-chiro-inositol is particularly efficacious in menstrual recovery. Thiazolidinediones and metformin combined with thiazolidinediones improve lipid metabolism better than metformin alone. Trial registration PROSPERO CRD42020211524.


Assuntos
Berberina , Resistência à Insulina , Metformina , Síndrome do Ovário Policístico , Tiazolidinedionas , Tomada de Decisão Clínica , Feminino , Humanos , Hipoglicemiantes/uso terapêutico , Inositol/uso terapêutico , Insulina , Metaboloma , Metformina/uso terapêutico , Metanálise em Rede , Síndrome do Ovário Policístico/tratamento farmacológico , Tiazolidinedionas/uso terapêutico , Incerteza
9.
Zhongguo Zhong Yao Za Zhi ; 46(14): 3504-3513, 2021 Jul.
Artigo em Chinês | MEDLINE | ID: mdl-34402272

RESUMO

Coptidis Rhizoma is a common Chinese medicinal in clinical practice,with the effects of clearing heat,drying dampness,purging fire,and removing toxin. All the medicinal plants of Coptis can be used for clinical treatment,but some species are endangered due to resource destruction and difficulty in planting. The dominant medicinal components in Coptidis Rhizoma are isoquinoline alkaloids. There are various methods for the analysis and detection of alkaloids,such as LC-MS,HPLC,and TLC,among which LC-MS is the most widely applied. Different plants of Coptis vary in the kind and content of alkaloids. C. chinensis,C. deltoidea,C. teeta,C. chinensis var. brevisepala,C. omeiensis,C. quinquefolia,and C. quinquesecta mainly contain berberine,palmatine,coptisine,jatrorrhizine,and columbamine,five effective alkaloid components. Plant isoquinoline alkaloids( PIAs) have strong pharmacological activity but are difficult to prepare. The application of synthetic biology of PIAs will be helpful for the clinical application of PIAs. This paper reviews the research progress on biological resources of Coptis species and structures of alkaloids as well as analysis methods and synthetic biology for isoquinoline alkaloids in the medicinal plants of Coptis in recent years,which will facilitate the protection of Coptis medicinal resources and the application and development of alkaloids.


Assuntos
Alcaloides , Alcaloides de Berberina , Berberina , Coptis , Medicamentos de Ervas Chinesas , Isoquinolinas , Rizoma
10.
Molecules ; 26(16)2021 Aug 13.
Artigo em Inglês | MEDLINE | ID: mdl-34443489

RESUMO

Hydrogel formulations (masks or patches, without tissue support) represent the new frontier for customizable skin beauty and health. The employment of these materials is becoming popular in wound dressing, to speed up the healing process while protecting the affected area, as well as to provide a moisturizing reservoir, control the inflammatory process and the onset of bacterial development. Most of these hydrogels are acrylic-based at present, not biodegradable and potentially toxic, due to acrylic monomers residues. In this work, we selected a new class of cellulose-derived and biodegradable hydrogel films to incorporate and convey an active compound for dermatological issues. Films were obtained from a combination of different polysaccharides and clays, and berberine hydrochloride, a polyphenolic molecule showing anti-inflammatory, immunomodulatory, antibacterial and antioxidant properties, was chosen and then embedded in the hydrogel films. These innovative hydrogel-based systems were characterized in terms of water uptake profile, in vitro cytocompatibility and skin permeation kinetics by Franz diffusion cell. Berberine permeation fitted well to Korsmeyer-Peppas kinetic model and achieved a release higher than 100 µg/cm2 within 24 h. The latter study, exploiting a reliable skin model membrane, together with the biological assessment, gained insights into the most promising formulation for future investigations.


Assuntos
Berberina/administração & dosagem , Sistemas de Liberação de Medicamentos , Metilgalactosídeos/química , Pele/efeitos dos fármacos , Morte Celular/efeitos dos fármacos , Forma Celular/efeitos dos fármacos , Fibroblastos/efeitos dos fármacos , Células HaCaT , Humanos , Cinética , Permeabilidade , Fibras de Estresse/efeitos dos fármacos , Fibras de Estresse/metabolismo , Difração de Raios X
11.
Talanta ; 234: 122625, 2021 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-34364434

RESUMO

To investigate the strong electrochemiluminescence (ECL) of ultrathin two dimensional metal-organic frameworks (2D MOFs) is crucial. In this work, we reported the strong ECL behavior of 2D Yb-MOFs, which exhibited thickness-dependent ECL. The thinner the 2D Yb-MOFs, the stronger the ECL signals. The corresponding ECL emission mechanism was investigated in detail, which was ascribed to the thinner 2D Yb-MOF with larger specific surface area, provided more luminophores, better electronic conductivity and superior fluorescence quantum yield, which yielded a higher ECL intensity. Considering the excellent ECL performances above, the ultrathin 2D Yb-MOF-1 was selected as new ECL emitter so that a sensor could be fabricated to realize the "on-off-on" detection of picric acid (PA) and berberine chloride form (BCF). The proposed sensor strategy exhibited a good analytical performance, where the linear range for PA detection was from 0.1 µM to 1 µM with a limit of 81.3 nM, and that for BCF detection from 0.05 µM to 1 µM with a limit of 36.5 nM. This study carves out a novel avenue for exploiting excellent ECL materials.


Assuntos
Berberina , Técnicas Biossensoriais , Estruturas Metalorgânicas , Cloretos , Técnicas Eletroquímicas , Medições Luminescentes , Picratos
12.
Phytomedicine ; 91: 153654, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34333328

RESUMO

BACKGROUND: Polycystic ovary syndrome (PCOS) is a clinical syndrome with reproductive and endocrine disorders. Berberine is a monomer from Chinese herbs such as Coptis chinensis, whose effect on improving ovulation and endometrial receptivity of PCOS is uncertain. PURPOSE: To evaluate the effect of berberine on improving PCOS and explore the mechanism. METHODS: The rat model of PCOS was induced by intraperitoneal injection of testosterone propionate. Then they was divided into model (Mod) group, low-dose of berberine (BL) group, high-dose of berberine (BH) group and metformin (Met) group as well as a control (Con) group was established. Ovary morphology, hormone level, glucolipid metabolism were measured. UID-mRNA-seq of ovary tissue was conducted to seek the mechanism of berberine on improving ovulation. Three biomarkers of endometrial receptivity were also examined in endometrium by immunohistochemistry. RESULTS: The number of cystic follicles was increased while the number of corpus luteum was decreased in the rats of Mod group. These changes could be reversed by high-dose of berberine intervention. Berberine could also decrease the levels of serum luteinizing hormone (LH) and total cholesterol (TC) in PCOS rats. Meanwhile, berberine improved the impairment of abnormal oral glucose tolerance without affecting fasting insulin level and Homeostasis model assessment-insulin resistance (HOMA-IR). Luteinizing hormone/ choriogonadotropin receptor (LHCGR) and cytochrome P450 Family 19 Subfamily A Member 1 (CYP19A1) were focused via RNA-seq of ovary. Protein expression in ovary and mRNA expression in granulosa cell of LHCGR and CYP19A1 were decreased in Mod group and rescued by the intervention of berberine. A decrease of endometrial thickness and an increase of integrin αvß3 and lysophosphatidic acid receptor 3 (LPAR3) protein expression were observed in Mod group, which could be also reversed by berberbine. CONCLUSIONS: Berberine could improve ovulation in PCOS and the mechanism might be associated with up-regulating LHCGR and CYP19A1. Berberine could also improve endometrial receptivity through down-regualting αvß3 and LPAR3.


Assuntos
Berberina , Ovulação/efeitos dos fármacos , Síndrome do Ovário Policístico , Animais , Berberina/farmacologia , Endométrio/efeitos dos fármacos , Feminino , Metformina , Síndrome do Ovário Policístico/tratamento farmacológico , Ratos
13.
Nutrients ; 13(8)2021 Jul 26.
Artigo em Inglês | MEDLINE | ID: mdl-34444711

RESUMO

Cardiovascular disease (CVD) is a major contributor to the global burden of disease. Berberine, a long-standing, widely used, traditional Chinese medicine, is thought to have beneficial effects on CVD risk factors and in women with polycystic ovary syndrome. The mechanisms and effects, specifically in men, possibly via testosterone, have not been examined previously. To assess the effect of berberine on CVD risk factors and any potential pathway via testosterone in men, we conducted a randomized, double-blind, placebo-controlled, parallel trial in Hong Kong. In total, 84 eligible Chinese men with hyperlipidemia were randomized to berberine (500 mg orally, twice a day) or placebo for 12 weeks. CVD risk factors (lipids, thromboxane A2, blood pressure, body mass index and waist-hip ratio) and testosterone were assessed at baseline, and 8 and 12 weeks after intervention. We compared changes in CVD risk factors and testosterone after 12 weeks of intervention using analysis of variance, and after 8 and 12 weeks using generalized estimating equations (GEE). Of the 84 men randomized, 80 men completed the trial. Men randomized to berberine had larger reductions in total cholesterol (-0.39 mmol/L, 95% confidence interval (CI) -0.70 to -0.08) and high-density lipoprotein cholesterol (-0.07 mmol/L, 95% CI -0.13 to -0.01) after 12 weeks. Considering changes after 8 and 12 weeks together, berberine lowered total cholesterol and possibly low-density lipoprotein-cholesterol (LDL-c), and possibly increased testosterone. Changes in triglycerides, thromboxane A2, blood pressure, body mass index and waist-hip ratio after the intervention did not differ between the berberine and placebo groups. No serious adverse event was reported. Berberine is a promising treatment for lowering cholesterol. Berberine did not lower testosterone but instead may increase testosterone in men, suggesting sex-specific effects of berberine. Exploring other pathways and assessing sex differences would be worthwhile, with relevance to drug repositioning and healthcare.


Assuntos
Berberina/uso terapêutico , Colesterol/sangue , Fatores de Risco de Doenças Cardíacas , Adulto , Anticolesterolemiantes/administração & dosagem , Anticolesterolemiantes/efeitos adversos , Anticolesterolemiantes/uso terapêutico , Berberina/administração & dosagem , Berberina/efeitos adversos , Pressão Sanguínea/efeitos dos fármacos , Índice de Massa Corporal , HDL-Colesterol/sangue , LDL-Colesterol/sangue , Método Duplo-Cego , Humanos , Hiperlipidemias/tratamento farmacológico , Masculino , Pessoa de Meia-Idade , Testosterona/sangue , Tromboxano A2/sangue , Triglicerídeos/sangue , Relação Cintura-Quadril
14.
Environ Pollut ; 289: 117865, 2021 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-34358871

RESUMO

The aim of this study was to evaluate the effect of berberine (BBR) on the intestinal health of piglets exposed to deoxynivalenol (DON). A total of 180 weaned piglets were randomly allotted to 1 of 3 treatment groups with 10 replication pens per treatment and 6 piglets per pen. The treatments were basal diet, basal diet +4 mg/kg DON, and basal diet +4 mg/kg DON +40 mg/kg BBR. The experiment lasted for 21 d. BBR improved the growth performance of DON-challenged piglets. BBR could inhibit DON-induced intestinal injury by increasing the expression of serum antioxidant enzymes and T cell surface antigens and reducing the release of proinflammatory cytokines in the small intestine. BBR significantly increased the protein expression levels of zonula occludens 1 (ZO-1), Occludin and Claudin-1 in the ileal and jejunal mucosa and increased the morphological parameters of the jejunum. Moreover, we found that BBR significantly reduced the DON-induced gene and protein expression levels of ERK, JNK, and NF-κB in the jejunum and ileum. In conclusion, BBR can regulate DON-induced intestinal injury, immunosuppression and oxidative stress by regulating the NF-κB and MAPK signaling pathways and ultimately maintain the intestinal health of piglets.


Assuntos
Berberina , NF-kappa B , Animais , Imunossupressão , Inflamação , NF-kappa B/metabolismo , Estresse Oxidativo , Transdução de Sinais , Suínos , Tricotecenos
15.
Life Sci ; 284: 119884, 2021 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-34389401

RESUMO

BACKGROUND: Liver injury results in excessive extracellular matrix (ECM) deposition in the liver, which is mainly produced by hepatic stellate cells (HSC). Alpha-smooth muscle actin (α-SMA) and liver enzymes are the two hallmarks of liver injury. Previously, it has been confirmed that berberine (BBR) attenuates liver injury. This study aimed to investigate the protective effect of Poly Lactic-co-Glycolic Acid (PLGA) encapsulated BBR against liver injury. METHODS: Nanoprecipitation, encapsulation, and physio-chemical characterization of BBR-PLGA nanoparticles (BBR-PLGA-NP) have been done. The protective effects of BBR-PLGA-NPs and BBR against carbon tetrachloride (CCl4)-treated Wistar rats were investigated. The serum levels of alanine aminotransferase and aspartate transaminase were measured, and the expression level of α-SMA was quantified by qRT-PCR. To evaluate the liver changes, morphological and histological staining was done. RESULTS: BBR-PLGA-NPs markedly reduced serum ALT and AST in rats treated with CCl4. Although the expression level of α-SMA was downregulated in the CCl4-injected rats that were treated with BBR, α-SMA expression in this group was still remarkably higher than the control group. α-SMA mRNA was significantly under-expressed (p < 0.05) by BBR-PLGA-NPs and the hepatic histology revealed BBR-PLGA-NPs made further improvements than free BBR. CONCLUSION: The use of nanoparticle to encapsulate BBR is a worthy approach to enhance the curative effect of BBR against liver injuries, which donate a safe and effective drug delivery strategy to treat liver injuries.


Assuntos
Actinas/genética , Berberina/farmacologia , Regulação da Expressão Gênica , Fígado/patologia , Copolímero de Ácido Poliláctico e Ácido Poliglicólico/química , Actinas/metabolismo , Alanina Transaminase/sangue , Animais , Aspartato Aminotransferases/sangue , Tetracloreto de Carbono , Regulação da Expressão Gênica/efeitos dos fármacos , Fígado/efeitos dos fármacos , Masculino , Nanopartículas/química , Nanopartículas/ultraestrutura , Tamanho da Partícula , RNA Mensageiro/genética , RNA Mensageiro/metabolismo , Ratos Wistar , Espectroscopia de Infravermelho com Transformada de Fourier , Eletricidade Estática
16.
Phytomedicine ; 91: 153678, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34385092

RESUMO

BACKGROUND: Demethyleneberberine (DMB) is a natural active component of medicinal plant Cortex phellodendri chinensis with favorable bioactivity. However, the role of DMB in suppressing non-small cell lung cancer (NSCLC) remains unknown. PURPOSE: In this study, we aimed to examine the effect and underlying mechanism of DMB in suppressing NSCLC. METHODS: CCK8 assay and colony formation assay were utilized to assess the efficiency of DMB on the viability and colony formation capacity of NSCLC cells. Flow cytometry and ß-Galactosidase Staining Kit were utilized to determine the efficiency of DMB on the cell cycle and cellular senescence of NSCLC cells. RT-qPCR and Western blot were used to detect the effect of DMB on cell cycle and cellular senescence related gene and protein expression of NSCLC cells. In vivo tumor model was established to evaluate the anti NSCLC effect of DMB. In addition, RNA-seq analysis was performed to detect the differential gene expression after DMB treatments. RESULTS: In this study, we revealed that DMB exhibits efficient inhibitory effect on NSCLC cell proliferation and tumor xenografts growth in vivo. We also demonstrated that DMB could inhibit cell migration by suppressing epithelial-mesenchymal transition (EMT) and trigger cell cycle arrest by down-regulating the expression of cell cycle related genes in NSCLC cells. In addition, DMB treatment efficiently induces cellular senescence of NSCLC cells. From the RNA-seq analysis, we found that DMB accelerates senescence through suppressing HIF-1α expression, which was further elucidated by overexpressing HIF-1α in NSCLC to reduce the inhibitory effect of DMB. Furthermore, we also revealed that DMB decreases the expression of c-Myc, an up-stream protein of HIF-1α. CONCLUSIONS: Taken together, we first report that DMB inhibits NSCLC progress through inducing cell cycle arrest and triggering cellular senescence by downregulating c-Myc/HIF-1α pathway.


Assuntos
Berberina/análogos & derivados , Carcinoma Pulmonar de Células não Pequenas , Neoplasias Pulmonares , Animais , Berberina/farmacologia , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Senescência Celular/efeitos dos fármacos , Humanos , Subunidade alfa do Fator 1 Induzível por Hipóxia/metabolismo , Neoplasias Pulmonares/tratamento farmacológico , Proteínas Proto-Oncogênicas c-myc/metabolismo , Transdução de Sinais , Ensaios Antitumorais Modelo de Xenoenxerto
17.
ACS Biomater Sci Eng ; 7(8): 3737-3753, 2021 08 09.
Artigo em Inglês | MEDLINE | ID: mdl-34297529

RESUMO

Selective permeability of the blood-brain barrier limits effective treatment of neurodegenerative disorders. In the present study, brain-targeted lipid-coated mesoporous silica nanoparticles (MSNs) containing berberine (BBR) were synthesized for the effective treatment of Alzheimer's disease (AD). The study involved synthesis of Mobil Composition of Matter-41 (MCM-41) mesoporous silica nanoparticles (MSNs), BBR loading, and lipid coating of MSNs (MSNs-BBR-L) and in vitro and in vivo characterization of MSNs-BBR-L. The liposomes (for lipid coating) were prepared by the thin-film hydration method. Transmission electron microscopy (TEM) images indicated 5 nm thickness of the lipid coating. Dynamic light scattering (DLS) and TEM results confirmed that the size of synthesized MSNs-BBR-L was in the range of 80-100 nm. The X-ray diffraction (XRD) pattern demonstrated retention of the ordered structure of BBR after encapsulation and lipid coating. Fourier transform infrared (FTIR) spectrum confirmed the formation of a lipid coat over the MSN particles. MSNs-BBR-L displayed significantly (p < 0.05) higher acetylcholine esterase (AChE) inhibitory activity. The study confirmed significant (p < 0.05) amyloid fibrillation inhibition and decreased the malondialdehyde (MDA) level by MSNs-BBR-L. Pure BBR- and MSNs-BBR-L-treated AD animals showed a significant decrease in the BACE-1 level compared to scopolamine-intoxicated mice. Eight times higher area under the curve for MSNs-BBR-L (2400 ± 27.44 ng h/mL) was recorded compared to the pure BBR (295.5 ± 0.755 ng h/mL). Overall, these results highlight the utility of MSNs-BBR-L as promising drug delivery vehicles for brain delivery of drugs.


Assuntos
Berberina , Nanopartículas , Acetilcolina , Acetilcolinesterase , Animais , Berberina/farmacologia , Lipídeos , Camundongos , Porosidade , Dióxido de Silício
18.
Molecules ; 26(14)2021 Jul 11.
Artigo em Inglês | MEDLINE | ID: mdl-34299486

RESUMO

Coptisine is the major bioactive protoberberine alkaloid found in Rhizoma Coptidis. Coptisine reduces inflammatory responses and improves glucose tolerance; nevertheless, whether coptisine has vasoprotective effect in diabetes is not fully characterized. Conduit arteries including aortas and carotid arteries were obtained from male C57BL/6J mice for ex vivo treatment with risk factors (high glucose or tunicamycin) and coptisine. Some arterial rings were obtained from diabetic mice, which were induced by high-fat diet (45% kcal% fat) feeding for 6 weeks combined with a low-dose intraperitoneal injection of streptozotocin (120 mg/kg). Functional studies showed that coptisine protected endothelium-dependent relaxation in aortas against risk factors and from diabetic mice. Coptisine increased phosphorylations of AMPK and eNOS and downregulated the endoplasmic reticulum (ER) stress markers as determined by Western blotting. Coptisine elevates NO bioavailability and decreases reactive oxygen species level. The results indicate that coptisine improves vascular function in diabetes through suppression of ER stress and oxidative stress, implying the therapeutic potential of coptisine to treat diabetic vasculopathy.


Assuntos
Berberina/análogos & derivados , Diabetes Mellitus Experimental/complicações , Estresse do Retículo Endoplasmático/efeitos dos fármacos , Endotélio Vascular/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Doenças Vasculares/tratamento farmacológico , Doenças Vasculares/etiologia , Proteínas Quinases Ativadas por AMP/metabolismo , Animais , Aorta/efeitos dos fármacos , Aorta/metabolismo , Berberina/farmacologia , Diabetes Mellitus Experimental/metabolismo , Dieta Hiperlipídica/efeitos adversos , Endotélio Vascular/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo III/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Doenças Vasculares/metabolismo
19.
ACS Appl Mater Interfaces ; 13(27): 32295-32306, 2021 Jul 14.
Artigo em Inglês | MEDLINE | ID: mdl-34196538

RESUMO

Synthetic fungicides have been widely used to protect crops from fungal diseases. However, excessive use of synthetic fungicides leads to the generation of fungicide resistance in fungal pathogens. Recently, smart cargo delivery systems have been introduced for the construction of a pesticide delivery nanoplatform, benefiting from their controlled release performance. Herein, a fungal pathogen microenvironment-responsive supramolecular fungicide nanoplatform has been designed and constructed, using quaternary ammonium salt (Q)-modified mesoporous silica nanoparticles (MSN-Q NPs) as nanocarriers loaded with berberine hydrochloride (BH) and carboxylatopillar[5]arene (CP[5]A) as nanogates to form BH-loaded CP[5]A@MSN-Q NPs for effective inhibition of Botrytis cinerea. CP[5]A as nanogates can endow the fungicide nanoplatform with pH stimuli-responsive release features for the control of fungicide release. The loaded BH, as a natural plant fungicide, provides an ecofriendly alternative to synthetic fungicides for controlling B. cinerea. Interestingly, we use oxalic acid (OA) secreted by B. cinerea as a trigger so that BH can be released from the fungicide nanoplatform on demand under pathogen microenvironments for controlling B. cinerea. The experimental results indicate that the fabricated fungicide nanoplatform could effectively inhibit the mycelial growth and spore germination, providing a new way for the management of B. cinerea in actual application.


Assuntos
Portadores de Fármacos/química , Fungicidas Industriais/química , Fungicidas Industriais/farmacologia , Nanopartículas/química , Dióxido de Silício/química , Berberina/química , Berberina/farmacologia , Botrytis/efeitos dos fármacos , Preparações de Ação Retardada , Liberação Controlada de Fármacos , Farmacorresistência Fúngica/efeitos dos fármacos , Porosidade , Compostos de Amônio Quaternário/química
20.
Med Hypotheses ; 153: 110639, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34229236

RESUMO

Huntington disease (HD) is a type of neurodegenerative disease that is characterized by presence of multiple repeats (more than 36) of cytosine-adenine-guanine (CAG) trinucleotides and mutated huntingtin (mHtt). This can further lead to oxidative stress, enhancement in level of ROS/RNS, mitochondrial dysfunction and neuroinflammations. Many clinical and preclinical trials have been conducted so far for the effective treatment of HD however, none of the drugs has shown complete relief. The regeneration of neurons is a very complicated process and associated with multiple pathological pathways. Hence, finding a unique solution using single drug that could act on multiple pathological pathways is really cumbersome. In the proposed hypothesis the use of demethyleneberberine (DMB) as a potential anti-HD agent has been explained. It is a metabolite of berberine and reported to act on multiple mechanistic pathways that are responsible for HD. Present article highlights new mechanistic insights through which DMB inhibits ROS/RNS, oxidative stress, mitochondrial dysfunctions and neuroinflammation such as NFκB, TNF-α, IL-6 and IL-8, cytokinin. Further its action on cellular apoptosis and neuronal cell death are also reported.


Assuntos
Berberina , Doença de Huntington , Doenças Neurodegenerativas , Berberina/análogos & derivados , Berberina/uso terapêutico , Humanos , Doença de Huntington/tratamento farmacológico , Estresse Oxidativo
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