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1.
J Ethnopharmacol ; 300: 115671, 2023 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-36055476

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Kalyanaka ghrita (KG) is an Ayurvedic formulation traditionally used in the treatment of Daurbalya (debility) and Smritidaurbalya (impairment of intellectual activities). Clinical studies have reported the effect of KG in the treatment of Manasmandata or Buddhimandyata which is associated with impaired learning, social adjustment and maturation. AIM OF THE STUDY: The present study aims to standardization of KG and validation of its use in experimental models of neurodegeneration. MATERIALS AND METHODS: KG was Standardized for biomarkers curcumin, gallic acid, tannic acid, chebulagic acid, and berberine. In male wistar rats, neurodegeneration was induced by administration of intracerebroventricular Amyloid ß (Aß1-42). The effect of KG (oral and intranasal treatment) was evaluated through behavioral parameters such as Morris water maze, social recognition test, novel object recognition, locomotor activity, and molecular parameters, brain acetylcholinesterase, brain-derived neurotrophic factor (BDNF), inflammatory cytokines, oxidative stress markers, and antioxidants. Brain histopathology was performed for studying the architecture of the brain and plaque formation. RESULTS AND DISCUSSION: A novel HPLC method has been developed for the standardization of KG. Treatment with KG significantly improved cognition and memory and increased brain BDNF and antioxidant status in Aß1-42 induced rats. It also reduced brain acetylcholinesterase, oxidative stress, and inflammatory cytokines and prevented neuronal damage. There were more marked effects with intra-nasal administration compared to oral treatment. CONCLUSION: The findings suggest that KG has neuroprotective potential and along with its nootropic property could be a promising therapy for neurodegenerative diseases like Alzheimer's disease.


Assuntos
Doença de Alzheimer , Berberina , Curcumina , Fármacos Neuroprotetores , Nootrópicos , Acetilcolinesterase , Doença de Alzheimer/tratamento farmacológico , Peptídeos beta-Amiloides/toxicidade , Animais , Antioxidantes , Berberina/farmacologia , Fator Neurotrófico Derivado do Encéfalo , Curcumina/farmacologia , Citocinas/farmacologia , Modelos Animais de Doenças , Masculino , Aprendizagem em Labirinto , Transtornos da Memória/induzido quimicamente , Transtornos da Memória/tratamento farmacológico , Nootrópicos/farmacologia , Ratos , Ratos Wistar , Taninos/farmacologia
2.
J Pharm Biomed Anal ; 223: 115161, 2023 Jan 20.
Artigo em Inglês | MEDLINE | ID: mdl-36402125

RESUMO

Due to their health benefits, including regulating blood sugar and lowering cholesterol, berberine food supplements (FS) are widely used by consumers. This study aims to evaluate the quality of such products by proposing a new analytical methodology based on low-field NMR. Eighteen berberine FS were analyzed with both conventional (500 MHz) and benchtop (60 MHz) NMR spectrometers. Three quantitative 60 MHz 1H NMR methodologies were performed to determine berberine contents that were compared to those obtained at 500 MHz considered as reference measurements. To make the recording time of the spectra acquired at low field compatible with the requirements of a routine control, the quantification was carried out using a calibration curve established under conditions of incomplete relaxation of BrB protons. This methodology, applied to a test sample of 15 mg of FS, allowed to accurately measure a minimum quantity of berberine of ≈ 10 mg/capsule or tablet in 15 min. Regarding the FS, their labels are often unclear and/or incomplete for the consumer. Moreover, only 56 % of the FS analyzed actually contain the claimed quantity of berberine. The amounts of active they supply per day are extremely variable with only 39 % of the FS delivering a sufficient dose to achieve a hypoglycemic or hypolipidemic effect (1000-1500 mg/day based on literature data). These results show that health authorities should institute much stricter control and regulation over the production, labeling and marketing of berberine-based FS.


Assuntos
Berberina , Prótons , Espectroscopia de Prótons por Ressonância Magnética , Imageamento por Ressonância Magnética , Suplementos Nutricionais
3.
Phytomedicine ; 108: 154521, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36334387

RESUMO

BACKGROUND: Berberrubine (BRB), one of the major metabolites of berberine (BBR), exerts an anti-hyperuricemic effect even superior to BBR. Liver is an important location for drug transformation. Nevertheless, there are few studies on the bioactivities and metabolites of BRB. PURPOSE: We investigated whether oxyberberrubine (OBR), a liver metabolite of BRB, exerted urate-lowering and reno-protective effects in hyperuricemic mice. METHODS: Liver microsomes were used to incubate BRB for studying its biotransformation. We isolated and identified its new metabolite OBR, and investigated its anti-hyperuricemic and reno-protective effects. In this work, the hyperuricemic mice model was established by receiving potassium oxonate (PO) and hypoxanthine (HX) for 7 consecutive days. 1 h after modeling, different dosages of OBR (5, 10 and 20 mg/kg), BRB (20 mg/kg) or febuxostat (Fex, 5 mg/kg) were given mice by gavage. RESULTS: Results showed that OBR possessed potent anti-hyperuricemic and reno-protective effects in hyperuricemic mice. Serum uric acid (UA) level was lowered, and the activities of xanthine oxidase (XOD) as well as adenosine deaminase (ADA) in the liver were suppressed after treatment with OBR. Hepatic expressions of XOD were remarkably decreased at mRNA and protein levels by OBR treatment. In addition, OBR prominently alleviated renal injury, embodied in markedly reduced serum creatinine and blood urea nitrogen (BUN) levels, decreased inflammatory mediators (TNF-α, IL-1ß, IL-6 and IL-18) levels, mRNA expression of CYP27B1 and repairment of renal tissues damage. Besides, OBR down-regulated renal expression of urate transporter 1 (URAT1), glucose transporter 9 (GLUT9), NOD-like receptor 3 (NLRP3), apoptosis-associated speck-like protein containing CARD (ASC), and caspase-1 at mRNA and protein levels. CONCLUSIONS: In short, our study indicated that OBR possessed superior anti-hyperuricemic and reno-protective effects, at least in part, through the inhibition of XOD, URAT1, GLUT9 and NLRP3 inflammasome signaling pathway in the kidney.


Assuntos
Berberina , Hiperuricemia , Camundongos , Animais , Ácido Úrico , Berberina/farmacologia , Berberina/uso terapêutico , Microssomos Hepáticos/metabolismo , Proteína 3 que Contém Domínio de Pirina da Família NLR/metabolismo , Hiperuricemia/tratamento farmacológico , Hiperuricemia/metabolismo , Xantina Oxidase/metabolismo , Rim , Ácido Oxônico , RNA Mensageiro/metabolismo
4.
Front Endocrinol (Lausanne) ; 13: 1074348, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36465656

RESUMO

Type 2 diabetes mellitus (T2DM) and its complications are major public health problems that seriously affect the quality of human life. The modification of intestinal microbiota has been widely recognized for the management of diabetes. The relationship between T2DM, intestinal microbiota, and active ingredient berberine (BBR) in intestinal microbiota was reviewed in this paper. First of all, the richness and functional changes of intestinal microbiota disrupt the intestinal environment through the destruction of the intestinal barrier and fermentation/degradation of pathogenic/protective metabolites, targeting the liver, pancreas, visceral adipose tissue (VAT), etc., to affect intestinal health, blood glucose, and lipids, insulin resistance and inflammation. Then, we focus on BBR, which protects the composition of intestinal microbiota, the changes of intestinal metabolites, and immune regulation disorder of the intestinal environment as the therapeutic mechanism as well as its current clinical trials. Further research can analyze the mechanism network of BBR to exert its therapeutic effect according to its multi-target compound action, to provide a theoretical basis for the use of different phytochemical components alone or in combination to prevent and treat T2DM or other metabolic diseases by regulating intestinal microbiota.


Assuntos
Berberina , Diabetes Mellitus Tipo 2 , Microbioma Gastrointestinal , Resistência à Insulina , Humanos , Berberina/farmacologia , Berberina/uso terapêutico , Diabetes Mellitus Tipo 2/tratamento farmacológico , Glicemia
5.
Biomed Res Int ; 2022: 7978258, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36452059

RESUMO

Objective: This study systematically explored the mechanism of Rhizoma Coptidis-Eupatorium fortunei in treating type 2 diabetes mellitus (T2DM) by using network pharmacology and molecular docking methods. Methods: The TCMSP database was used to screen out the active ingredients and related targets of Rhizoma Coptidis-Eupatorium fortunei (R-E) drug pair. GeneCards, OMIM, DrugBank, and other databases were used to screen the related targets of T2DM, and then, the UniProt database was used to standardize the relevant targets of T2DM. Then, the Venn analysis was performed on the active ingredient-related targets and disease-related targets of R-E drugs to find the intersection targets. Using the STRING database and Cytoscape software, the PPI network and "drug-active ingredient-target-disease" network are constructed by intersecting targets and corresponding active ingredients. Through the cluster profiler package in the R software, GO function enrichment analysis and KEGG pathway enrichment analysis were carried out on the intersection targets and the screened core targets, and the prediction results were verified by molecular docking. Results: Taking OB ≥ 30% and DL ≥ 0.18 as the standard, a total of 25 effective active ingredients of R-E drug pairs were screened, including berberine, palmatine, coptisine, and so on. After corresponding, 19 effective chemical components and 284 targets of the R-E drug pair were obtained. After searching multiple disease databases, 1289 T2DM-related targets were screened. After the summary, 159 common targets were obtained in this study. Finally, in the bioinformatics analysis, this study concluded that quercetin, luteolin, berberine, palmatine, and coptisine are the main chemical components of the R-E drug pair. ESR1, MAPK1, AKT1, TP53, IL6, and JUN are the important core targets. GO and KEGG enrichment analyses showed that Rhizoma Coptidis-Eupatorium fortunei could improve T2DM by regulating multiple biological processes and pathways. Molecular docking results showed that berberine, palmatine, and coptisine had higher binding to the core target, and MAPK1, AKT1, and IL6 could stably bind to the active ingredients of Rhizoma Coptidis-Eupatorium fortunei. Conclusion: Rhizoma Coptidis-Eupatorium fortunei may have therapeutic effects on T2DM such as anti-inflammatory and regulating glucose and lipid metabolism through multiple components, multiple targets, and multiple signaling pathways, which provides a scientific basis for further research on the hypoglycemic effect of Rhizoma Coptidis-Eupatorium fortunei drug pair.


Assuntos
Antineoplásicos , Berberina , Diabetes Mellitus Tipo 2 , Medicamentos de Ervas Chinesas , Eupatorium , Simulação de Acoplamento Molecular , Medicamentos de Ervas Chinesas/farmacologia , Diabetes Mellitus Tipo 2/tratamento farmacológico , Farmacologia em Rede , Interleucina-6
6.
Life Sci ; 311(Pt A): 121141, 2022 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-36341914

RESUMO

BACKGROUND AND AIMS: Although oral berberine, a natural compound extracted from the Chinese herbal medicine curcumin, has low bioavailability, it is still effective in suppressing obesity; however, the underlying mechanism is unclear. Berberine can bind to bitter-taste receptors (TAS2Rs) in intestinal endocrine secretin tumor (STC-1) cells to promote glucagon-like peptide-1 (GLP-1) secretion. Notably, TAS2Rs also exist in the tuft cells of the gut. Therefore, this study aimed to explore whether the beneficial effect of oral berberine on obesity is dependent on bitter-taste signaling in the tuft cells of the gut. METHODS AND RESULTS: Standard chow diet (SCD) or high-fat diet (HFD) was administered to C57BL/6 mice, with or without berberine (100 mg/kg, 200 mg/kg, p. o.). The PLCß2 inhibitor U73122 was used to verify whether the anti-obesity effect of berberine was dependent on the bitter-taste signaling pathway. In this study, we observed that the oral administration of berberine alleviated HFD-induced obesity in mice that U73122 partially inhibited. Both in vivo and ex vivo, berberine upregulated the release of GLP-1, promoted the proliferation of tuft cells and secretion of IL-25 in obesity via the TAS2R signaling pathway. CONCLUSIONS: Oral berberine ameliorated HFD-induced obesity through the TAS2R-IL-25 signaling pathway in tuft cells in the gut. SIGNIFICANCE: We identified and functionally characterized the TAS2Rs and Gα-gustducin/Gß1γ13 signaling pathway utilized by tuft cells in response to oral berberine in obese mice and proposed a new mechanism underlying the anti-obesity effect of berberine.


Assuntos
Berberina , Células Endócrinas , Animais , Camundongos , Berberina/farmacologia , Dieta Hiperlipídica , Células Endócrinas/metabolismo , Peptídeo 1 Semelhante ao Glucagon/metabolismo , Camundongos Endogâmicos C57BL , Camundongos Obesos , Obesidade/tratamento farmacológico , Obesidade/metabolismo , Receptores Acoplados a Proteínas G/metabolismo
7.
Cells ; 11(21)2022 Oct 31.
Artigo em Inglês | MEDLINE | ID: mdl-36359829

RESUMO

Despite therapeutic advancements, lung cancer remains the principal cause of cancer mortality in a global scenario. The increased incidence of tumor reoccurrence and progression and the highly metastatic nature of lung cancer are of great concern and hence require the investigation of novel therapies and/or medications. Naturally occurring compounds from plants serve as important resources for novel drugs for cancer therapy. Amongst these phytochemicals, Berberine, an alkaloid, has been extensively explored as a potential natural anticancer therapeutic agent. Several studies have shown the effectiveness of Berberine in inhibiting cancer growth and progression mediated via several different mechanisms, which include cell cycle arrest, inducing cell death by apoptosis and autophagy, inhibiting cell proliferation and invasion, as well as regulating the expression of microRNA, telomerase activity, and the tumor microenvironment, which usually varies for different cancer types. In this review, we aim to provide a better understanding of molecular insights of Berberine and its various derivative-induced antiproliferative and antimetastatic effects against lung cancer. In conclusion, the Berberine imparts its anticancer efficacy against lung cancers via modulation of several signaling pathways involved in cancer cell viability and proliferation, as well as migration, invasion, and metastasis.


Assuntos
Antineoplásicos , Berberina , Neoplasias Pulmonares , Humanos , Berberina/farmacologia , Berberina/uso terapêutico , Berberina/química , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Antineoplásicos/química , Neoplasias Pulmonares/tratamento farmacológico , Neoplasias Pulmonares/patologia , Apoptose , Proliferação de Células , Microambiente Tumoral
8.
Food Funct ; 13(23): 12135-12143, 2022 Nov 28.
Artigo em Inglês | MEDLINE | ID: mdl-36321951

RESUMO

Berberine is widely used for the prevention of cancers and diabetes. However, the absorption rate of berberine is less than 1% in humans. The objective of this research was to determine whether emulsification improves the absorption and affects the metabolism of orally ingested berberine. Twelve healthy subjects, both men and women, received 800 mg berberine in a powder or emulsified form by vitamin E TPGS or Quillaja extract using a randomized crossover design. Blood samples were collected 12 hours after a dose. Berberine and its metabolites in plasma were analyzed with and without hydrolysis by glucuronidase and sulfatase on UHPLC-MS/MS. The area under the curve (AUC0-12 h) and peak plasma concentration (Cmax) of berberine was 6.7 nM h and 0.9 nM in participants who received berberine powder. They were increased to 12.6 nM h and 2.0 nM by TPGS emulsification and 28.0 nM h and 5.1 nM by Quillaja extract emulsification, respectively. Berberrubine and demethyleneberberine were detected as major phase-1 metabolites of berberine. The AUC0-12 of both free and total berberrubine was significantly increased by TPGS and Quillaja extract. Emulsification by Quillaja extract was more effective than TPGS to increase the plasma concentrations of free and total demethyleneberberine. However, the ratios of phase-1 metabolites and ratios of phase-2 conjugates were not affected by emulsification. Absorption increases of berberine by TPGS or Quillaja extract emulsification may lead to enhanced bioactivity in humans.


Assuntos
Berberina , Quillaja , Masculino , Humanos , Feminino , Espectrometria de Massas em Tandem , Pós , Vitamina E , Extratos Vegetais
9.
Int J Nanomedicine ; 17: 5303-5314, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36406639

RESUMO

Aim: This study focuses on constructing of an anti-inflammatory drug delivery system by encapsulation of berberine in the ß-glucan nanoparticles and evaluates its effect on treating ulcerative colitis. Methods: ß-Glucan and the anti-inflammatory drug berberine (BER) are self-assembled into nanoparticles to construct a drug delivery system (GLC/BER). The interaction between the drug and the carrier was characterized by circular dichroism, ultraviolet-visible spectroscopy, and dynamic light scattering. The anti-inflammatory effect of the GLC/BER was evaluated through a lipopolysaccharide (LPS)-induced RAW264.7 macrophage inflammation model and a sodium sulfate (DSS)-induced C57BL/6 mouse ulcerative colitis model. Results: The GLC/BER nanoparticles have a particle size of 80-120 nm and a high encapsulation efficiency of 37.8±4.21%. In the LPS-induced RAW264.7 macrophage inflammation model, GLC/BER significantly promoted the uptake of BER by RAW264.7 cells. RT-PCR and ELISA assay showed that it could significantly inhibit the inflammatory factors including IL-1ß, IL-6 and COX-2. Furthermore, GLC/BER shows inhibiting effect on the secretion of pro-inflammatory factors such as IL-1ß and IL-6, down-regulating the production of nitrite oxide; in animal studies, GLC/BER was found to exert a relieving effect on mice colitis. Conclusion: The study found that GLC/BER has an anti-inflammatory effect in vitro and in vivo, and the GLC carrier improves the potency and bioavailability of BER, providing a new type of nanomedicine for the treatment of colitis.


Assuntos
Berberina , Colite Ulcerativa , Colite , Nanopartículas , beta-Glucanas , Camundongos , Animais , Berberina/farmacologia , Berberina/uso terapêutico , Colite Ulcerativa/induzido quimicamente , Colite Ulcerativa/tratamento farmacológico , Lipopolissacarídeos , Interleucina-6 , Camundongos Endogâmicos C57BL , Macrófagos , Colite/induzido quimicamente , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Inflamação/tratamento farmacológico
10.
Int J Mol Sci ; 23(22)2022 Nov 14.
Artigo em Inglês | MEDLINE | ID: mdl-36430540

RESUMO

The interaction between the series of berberine derivatives 1-5 (NAX071, NAX120, NAX075, NAX077 and NAX079) and human telomeric G-quadruplexes (G4), which are able to inhibit the Telomerase enzyme's activity in malignant cells, was investigated. The derivatives bear a pyridine moiety connected by a hydrocarbon linker of varying length (n = 1-5, with n number of aliphatic carbon atoms) to the C13 position of the parent berberine. As for the G4s, both bimolecular 5'-TAGGGTTAGGGT-3' (Tel12) and monomolecular 5'-TAGGGTTAGGGTTAGGGTTAGGG-3' (Tel23) DNA oligonucleotides were considered. Spectrophotometric titrations, melting tests, X-ray diffraction solid state analysis and in silico molecular dynamics (MD) simulations were used to describe the different systems. The results were compared in search of structure-activity relationships. The analysis pointed out the formation of 1:1 complexes between Tel12 and all ligands, whereas both 1:1 and 2:1 ligand/G4 stoichiometries were found for the adduct formed by NAX071 (n = 1). Tel12, with tetrads free from the hindrance by the loop, showed a higher affinity. The details of the different binding geometries were discussed, highlighting the importance of H-bonds given by the berberine benzodioxole group and a correlation between the strength of binding and the hydrocarbon linker length. Theoretical (MD) and experimental (X-ray) structural studies evidence the possibility for the berberine core to interact with one or both G4 strands, depending on the constraints given by the linker length, thus affecting the G4 stabilization effect.


Assuntos
Berberina , Quadruplex G , Humanos , Análise Espectral , Telômero , Espectrofotometria
11.
Nutrients ; 14(22)2022 Nov 11.
Artigo em Inglês | MEDLINE | ID: mdl-36432457

RESUMO

Currently, the nutraceutical approach to treat dyslipidaemia is increasing in use, and in many cases is used by physicians as the first choice in the treatment of patients with borderline values. Nutraceuticals represent an excellent opportunity to treat the preliminary conditions not yet showing the pathological signs of dyslipidaemia. Their general safety, the patient's confidence, the convincing proof of efficacy and the reasonable costs prompted the market of new preparations. Despite this premise, many nutraceutical products are poorly formulated and do not meet the minimum requirements to ensure efficacy in normalizing blood lipid profiles, promoting cardiovascular protection, and normalizing disorders of glycemic metabolism. In this context, bioaccessibility and bioavailability of the active compounds is a crucial issue. Little attention is paid to the proper formulations needed to improve the overall bioavailability of the active molecules. According to these data, many products prove to be insufficient to ensure full enteric absorption. The present review analysed the literature in the field of nutraceuticals for the treatment of dyslipidemia, focusing on resveratrol, red yeast rice, berberine, and plant sterols, which are among the nutraceuticals with the greatest formulation problems, highlighting bioavailability and the most suitable formulations.


Assuntos
Berberina , Dislipidemias , Fitosteróis , Humanos , Dislipidemias/prevenção & controle , Suplementos Nutricionais , Lipídeos
12.
Am J Gastroenterol ; 117(11): 1805-1815, 2022 11 01.
Artigo em Inglês | MEDLINE | ID: mdl-36327436

RESUMO

INTRODUCTION: Primary sclerosing cholangitis (PSC) is a fibroinflammatory disease of the bile ducts leading to cirrhosis and hepatic decompensation. There are no approved pharmaceutical therapies for PSC. Berberine ursodeoxycholate (HTD1801) is an ionic salt of berberine and ursodeoxycholic acid with pleiotropic mechanisms of action. METHODS: An 18-week proof-of-concept study was conducted to assess the safety and efficacy of HTD1801 in PSC. This study had three 6-week periods: (i) a placebo-controlled period, (ii) a treatment extension period, and (iii) a randomized treatment withdrawal period. The primary end point was change from baseline in alkaline phosphatase (ALP) at week 6. RESULTS: Fifty-five patients were randomized and treated; 35 (64%) had inflammatory bowel disease and 22 (40%) had previously received ursodeoxycholic acid. Patients were initially randomized to placebo (n = 16), HTD1801 500 mg BID (n = 15), or HTD1801 1000 mg BID (n = 24). At baseline, mean (range) ALP values were 414 U/L (138-1,048), 397 U/L (237-773), and 335 U/L (122-882) for the placebo, HTD1801 500 mg BID, and HTD1801 1,000 mg BID groups, respectively. At week 6, a significant decrease in ALP was observed with HTD1801 (least square mean; HTD1801 500 mg BID = -53 U/L, P = 0.016; HTD1801 1000 mg BID = -37 U/L, P = 0.019) compared with placebo (98 U/L). ALP reductions were sustained through week 18 in those who remained on therapy, whereas ALP increased in those who crossed over to placebo during period 3. HTD1801 was generally well tolerated; 4 patients experienced serious adverse events, none attributed to HTD1801. DISCUSSION: HTD1801 is associated with significant improvement in ALP and warrants further study as a treatment for PSC.


Assuntos
Berberina , Colangite Esclerosante , Humanos , Ácido Ursodesoxicólico/uso terapêutico , Colangite Esclerosante/tratamento farmacológico , Berberina/uso terapêutico , Resultado do Tratamento , Ácidos e Sais Biliares , Fosfatase Alcalina
13.
Am J Gastroenterol ; 117(11): 1762-1763, 2022 11 01.
Artigo em Inglês | MEDLINE | ID: mdl-36327435

RESUMO

ABSTRACT: Effective pharmacologic treatment of primary sclerosing cholangitis (PSC) remains elusive. Ursodeoxycholic acid (UDCA) is known to improve liver biochemistry, specifically serum alkaline phosphatase, in patients with PSC but has not been shown to favourably alter the natural history. Similarly, many immunomodulatory medications have been studied for the treatment of PSC, but none has been demonstrated to be of unequivocal benefit. In this issue of the Journal, a pilot study of a ursodeoxycholate berberine salt vs placebo is reported. Although improvement in serum alkaline phosphatase is reported, without a control arm with UDCA monotherapy, it is not possible to determine whether this study drug is beneficial over UDCA by itself. More study in the PSC therapeutic arena is needed.


Assuntos
Berberina , Colangite Esclerosante , Humanos , Fosfatase Alcalina , Berberina/uso terapêutico , Ácidos e Sais Biliares , Colagogos e Coleréticos/uso terapêutico , Colangite Esclerosante/tratamento farmacológico , Projetos Piloto , Ácido Ursodesoxicólico/uso terapêutico
14.
Biol Pharm Bull ; 45(11): 1669-1677, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36328503

RESUMO

Although paliperidone-related hyperglycemia has been extensively examined, the underlying mechanisms have not yet been elucidated. We investigated the effects of a single intravenous injection of paliperidone (0.2, 0.4, or 0.6 mg/kg) on serum concentrations of glucose and other endogenous metabolites in rats. We also examined the effects of a single intravenous injection of paliperidone (0.4 mg/kg) on AMP-activated protein kinase (AMPK) activity in the hypothalamus and liver. To clarify the relationship between AMPK activity and adrenaline secretion, the effects of berberine, which inhibits hypothalamic AMPK, on paliperidone-induced hyperglycemia were assessed. Significant increases were observed in serum glucose, adrenaline, and insulin concentrations following intravenous injections of paliperidone at doses of 0.4 and 0.6 mg/kg. A propranolol pretreatment attenuated paliperidone-induced increases in serum concentrations of glucose, but not adrenaline. Significant increases were also noted in phosphorylated AMPK concentrations in the hypothalamus following the administration of paliperidone at a dose of 0.4 mg/kg. A berberine pretreatment attenuated paliperidone-induced increases in blood concentrations of glucose, adrenaline, and insulin and phosphorylated AMPK concentrations in the hypothalamus. Collectively, the present results demonstrated that an acute treatment with paliperidone induced hyperglycemia, which was associated with the effects of hypothalamic AMPK activation on the secretion of adrenaline.


Assuntos
Berberina , Hiperglicemia , Ratos , Animais , Proteínas Quinases Ativadas por AMP/metabolismo , Palmitato de Paliperidona/farmacologia , Berberina/farmacologia , Berberina/uso terapêutico , Hiperglicemia/induzido quimicamente , Hiperglicemia/metabolismo , Hipotálamo/metabolismo , Insulina , Glucose/metabolismo
15.
Inflammopharmacology ; 30(6): 2003-2016, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36183284

RESUMO

Coronavirus disease 2019 (Covid-19) is a global diastrophic disease caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Covid-19 leads to inflammatory, immunological, and oxidative changes, by which SARS-CoV-2 leads to endothelial dysfunction (ED), acute lung injury (ALI), acute respiratory distress syndrome (ARDS), and multi-organ failure (MOF). Despite evidence illustrating that some drugs and vaccines effectively manage and prevent Covid-19, complementary herbal medicines are urgently needed to control this pandemic disease. One of the most used herbal medicines is berberine (BBR), which has anti-inflammatory, antioxidant, antiviral, and immune-regulatory effects; thus, BBR may be a prospective candidate against SARS-CoV-2 infection. This review found that BBR has anti-SARS-CoV-2 effects with mitigation of associated inflammatory changes. BBR also reduces the risk of ALI/ARDS in Covid-19 patients by inhibiting the release of pro-inflammatory cytokines and inflammatory signaling pathways. In conclusion, BBR has potent anti-inflammatory, antioxidant, and antiviral effects. Therefore, it can be utilized as a possible anti-SARS-CoV-2 agent. BBR inhibits the proliferation of SARS-CoV-2 and attenuates the associated inflammatory disorders linked by the activation of inflammatory signaling pathways. Indeed, BBR can alleviate ALI/ARDS in patients with severe Covid-19. In this sense, clinical trials and prospective studies are suggested to illustrate the potential role of BBR in treating Covid-19.


Assuntos
Berberina , COVID-19 , Síndrome do Desconforto Respiratório , Humanos , COVID-19/tratamento farmacológico , SARS-CoV-2 , Berberina/farmacologia , Berberina/uso terapêutico , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Estudos Prospectivos , Antivirais/farmacologia , Antivirais/uso terapêutico , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico
16.
Curr Microbiol ; 79(12): 366, 2022 Oct 17.
Artigo em Inglês | MEDLINE | ID: mdl-36253652

RESUMO

Nowadays, with increasing resistance of microorganisms to drugs, it is necessary to look for new solutions beside antibiotic therapy. One of these effective approaches is the use of plant compounds and blue LED Irradiation. Berberine (an alkaloid compound) has several properties, including antibacterial effect. This compound destroys bacterial cells by producing reactive oxygen species (ROS). In this study, the combined effect of blue LED Irradiation and berberine on Pseudomonas aeruginosa (Gram-negatives) and Staphylococcus aureus (Gram-positive) and also their effect on human dermal fibroblast (HDF) cells were investigated. The obtained results showed that the combination of berberine and blue light irradiation had a better effect on both bacteria and this antimicrobial effect was higher in Gram-positive bacteria. These compounds also prevented the formation of biofilms and were able to destroy the created biofilms. Therefore, this method can be suggested to treat infection in chronic wounds, such as diabetic wounds.


Assuntos
Berberina , Infecções Estafilocócicas , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Berberina/farmacologia , Berberina/uso terapêutico , Biofilmes , Humanos , Pseudomonas aeruginosa , Espécies Reativas de Oxigênio , Staphylococcus aureus
17.
Comput Math Methods Med ; 2022: 7137401, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36276998

RESUMO

Berberine exhibits polytrophic medicinal roles in various diseases and is safe and effective. However, its role and the underlying mechanism in the replication of herpes simplex virus 1 (HSV-1) remain unreported. This research aimed to determine the functional mechanisms of berberine on HSV-1 infection. We determined the CC50 (405.11 ± 15.67 µM) and IC50 (45.6 ± 6.84 µM) of berberine on HEK293T cells infected with HSV-1. Berberine inhibited the transcription and translation of HSV-1 activity-related genes (gD, ICP-4, ICP-5, and ICP-8) in HSV-1-infected HEK293T cells dose-dependently. Berberine also inhibited the phosphorylation of MAPK proteins (JNK and p38) and inflammatory responses induced by HSV-1 infection in HEK293T cells dose-dependently. In conclusion, berberine attenuates HSV-1 replication through its activity, infective ability, and inflammatory response. Our research indicated that berberine may be a candidate drug for HSV-1 infection.


Assuntos
Berberina , Herpesvirus Humano 1 , Humanos , Herpesvirus Humano 1/fisiologia , Berberina/farmacologia , Células HEK293 , Replicação Viral , Antivirais/farmacologia
18.
Mikrochim Acta ; 189(11): 401, 2022 10 03.
Artigo em Inglês | MEDLINE | ID: mdl-36190563

RESUMO

In view of the limitations of existing berberine solid-phase extraction adsorbents, this paper proposes a novel carbonized π-conjugated polymer-coated porous silica (SiO2@C-π-CP) adsorbent with simple process and low cost for efficient extraction of berberine by multiple interactions. Characterization methods, including Brunner-Emmet-Teller measurement, thermogravimetric analysis, X-ray photoelectron spectroscopy, and scanning electron microscopy techniques, were used to verify the successful modification of carbonized π-conjugated polymer on the surface of porous silica. The berberine was selected as target molecule, and the adsorption mechanism and process were investigated through adsorption kinetics, adsorption isotherms, and thermodynamic studies. The fitting results show that the adsorption of berberine by SiO2@C-π-CP well conforms to the pseudo-second-order and Langmuir models. By optimizing the main SPE parameters, the SPE method based on SiO2@C-π-CP was developed. Excellent results were obtained, including low limit of detection (0.75 ng mL-1) and limit of quantification (2 ng mL-1), wide linearity (2-13,000 ng mL-1), and satisfactory relative standard deviations (RSD) of inter-day (1.5%) and intra-day (6.2%). Finally, the SiO2@C-π-CP also has been successfully used to the enrichment of berberine in real urine samples. This research makes clear that SiO2@C-π-CP has outstanding potential for trace enrichment of berberine alkaloids.


Assuntos
Berberina , Dióxido de Silício , Limite de Detecção , Polímeros/química , Porosidade , Dióxido de Silício/química
19.
Life Sci ; 309: 121040, 2022 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-36208663

RESUMO

AIMS: Several signaling events have been identified for mediating cisplatin-induced chronic inflammation and progressive renal fibrosis, but the majority of them have not yet been established as therapeutic targets. This study investigated the modulatory effects of berberine on purinergic 2X7 receptors (P2X7R) and some potential intracellular profibrogenic signaling as molecular mechanisms that could hinder renal fibrosis associated with cisplatin administration in rats. MAIN METHODS: For induction of kidney injury, rats were injected with cisplatin (1 mg/kg, i.p.) daily for two weeks. Concurrently, the rats were treated with berberine (100 or 200 mg/kg, p.o). The gene expressions of P2X7R, dual-specificity phosphatase 6 (DUSP6), and murine double-minute 2 (MDM2) were determined. The expressions of alpha smooth-muscle actin and tumor necrosis factor alpha (TNF-α) were assessed by immunohistochemical staining. Phosphorylated extracellular signal-regulated kinase 1/2, (p-ERK1/2) was evaluated by western blotting. Sirtuin 2 (SIRT2), kidney injury molecule-1, and galectin-3 were measured by enzyme-linked immunosorbent assay. The degree of renal fibrosis was assessed by microscopic examination and picrosirius red staining. KEY FINDINGS: Berberine effectively inhibited cisplatin-induced renal histopathological changes, enhanced renal function, and markedly mitigated inflammatory and fibrotic alterations as well as TNF-α protein expression. Additionally, P2X7R, p-ERK1/2, MDM2, and SIRT2 were suppressed and DUSP6 was upregulated by berberine. SIGNIFICANCE: The nephroprotective effects of berberine were mediated in part by downregulating P2X7R and modulating DUSP6-mediated inactivation of ERK1/2 as well as by suppressing SIRT2/MDM2-triggered renal fibrosis.


Assuntos
Berberina , Nefropatias , Ratos , Camundongos , Animais , Cisplatino/toxicidade , Berberina/farmacologia , Sirtuína 2 , Fator de Necrose Tumoral alfa , Fosfatase 6 de Especificidade Dupla , Proteína Quinase 3 Ativada por Mitógeno , Sistema de Sinalização das MAP Quinases , Actinas , Galectina 3 , Nefropatias/induzido quimicamente , Nefropatias/tratamento farmacológico , Nefropatias/prevenção & controle , Fibrose
20.
Acta Crystallogr D Struct Biol ; 78(Pt 10): 1273-1282, 2022 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-36189746

RESUMO

The bacterial nitroreductases (NRs) NfsB and NfsA are conserved homodimeric FMN-dependent flavoproteins that are responsible for the reduction of nitroaromatic substrates. Berberine (BBR) is a plant-derived isoquinoline alkaloid with a large conjugated ring system that is widely used in the treatment of various diseases. It was recently found that the gut microbiota convert BBR into dihydroberberine (dhBBR, the absorbable form) mediated by bacterial NRs. The molecular basis for the transformation of BBR by the gut microbiota remains unclear. Here, kinetic studies showed that NfsB from Escherichia coli (EcNfsB), rather than EcNfsA, is responsible for the conversion of BBR to dhBBR in spite of a low reaction rate. The crystal structure of the EcNfsB-BBR complex showed that BBR binds into the active pocket at the dimer interface, and its large conjugated plane stacks above the plane of the FMN cofactor in a nearly parallel orientation. BBR is mainly stabilized by π-stacking interactions with both neighboring aromatic residues and FMN. Structure-based mutagenesis studies further revealed that the highly conserved Phe70 and Phe199 are important residues for the conversion of BBR. The structure revealed that the C6 atom of BBR (which receives the hydride) is ∼7.5 Šfrom the N5 atom of FMN (which donates the hydride), which is too distant for hydride transfer. Notably, several well ordered water molecules make hydrogen-bond/van der Waals contacts with the N1 atom of BBR in the active site, which probably donate protons in conjunction with electron transfer from FMN. The structure-function studies revealed the mechanism for the recognition and binding of BBR by bacterial NRs and may help to understand the conversion of BBR by the gut microbiota.


Assuntos
Berberina , Proteínas de Escherichia coli , Bactérias/metabolismo , Carbono-Oxigênio Ligases/metabolismo , Escherichia coli/metabolismo , Mononucleotídeo de Flavina/química , Flavoproteínas/metabolismo , Isoquinolinas , Cinética , Medicina Tradicional , Nitrorredutases/química , Nitrorredutases/metabolismo , Prótons , Água
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