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1.
Food Chem Toxicol ; 119: 445-456, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-29203196

RESUMO

An-Gong-Niu-Huang Wan (AGNH) is a famous traditional Chinese medicine prescription that contains cinnabar (HgS) and realgar (As2S2); the clinical practice of AGNH is hindered because both mercury and arsenic are hepatorenal toxic metalloids. It is noted that the cinnabar and realgar in AGNH are not used alone, but rather combined with different kinds of medicinal herbs as a formula to use. In this study, we evaluated the hepatorenal protective effects of the medicinal herbs in AGNH after co-exposure to cinnabar and realgar for 4 weeks in mice. The combination of the herbs in AGNH alleviated cinnabar and realgar-induced histopathological alterations and oxidative stress in the liver and kidneys. Furthermore, in cinnabar and realgar-treated mice, the increased expression levels of inducible enzymes (COX-2 and iNOS) and proinflammatory mediators (IL-1ß, TNF-α, PGE2 and NO) in the liver and kidneys were consistently down-regulated when medicinal herbs were combined as a formula. We also found that the herbs could reduce the inflammatory response by the inactivation of the MAPK and PI3K/Akt signaling pathway and the resulting blockade of NF-κB activation. Overall, our data indicates that the herbal medicines in AGNH attenuate cinnabar and realgar-induced hepatorenal toxicity by improving antioxidant competence and suppressing inflammatory injury.


Assuntos
Medicamentos de Ervas Chinesas/farmacologia , Medicina Herbária , Inflamação/prevenção & controle , Compostos de Mercúrio/toxicidade , Estresse Oxidativo/efeitos dos fármacos , Sulfetos/toxicidade , Animais , Antioxidantes/farmacologia , Arsenicais , Citocinas/metabolismo , Feminino , Inativação Metabólica , Mediadores da Inflamação/metabolismo , Rim/efeitos dos fármacos , Rim/metabolismo , Rim/patologia , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Sistema de Sinalização das MAP Quinases , Masculino , Camundongos , NF-kappa B/metabolismo , Fosfatidilinositol 3-Quinases/metabolismo , Fosforilação , Proteínas Proto-Oncogênicas c-akt/metabolismo , Transdução de Sinais/efeitos dos fármacos
2.
Sci Rep ; 7: 45155, 2017 03 23.
Artigo em Inglês | MEDLINE | ID: mdl-28332601

RESUMO

Transient Receptor Potential Melastatin-8 (TRPM8) reportedly plays a fundamental role in a variety of processes including cold sensation, thermoregulation, pain transduction and tumorigenesis. However, the role of TRPM8 in inflammation under cold conditions is not well known. Since cooling allows the convergence of primary injury and injury-induced inflammation, we hypothesized that the mechanism of the protective effects of cooling might be related to TRPM8. We therefore investigated the involvement of TRPM8 activation in the regulation of inflammatory cytokines. The results showed that TRPM8 expression in the mouse hypothalamus was upregulated when the ambient temperature decreased; simultaneously, tumor necrosis factor-alpha (TNFα) was downregulated. The inhibitory effect of TRPM8 on TNFα was mediated by nuclear factor kappa B (NFκB). Specifically, cold stress stimulated the expression of TRPM8, which promoted the interaction of TRPM8 and NFκB, thereby suppressing NFκB nuclear localization. This suppression consequently led to the inhibition of TNFα gene transcription. The present data suggest a possible theoretical foundation for the anti-inflammatory role of TRPM8 activation, providing an experimental basis that could contribute to the advancement of cooling therapy for trauma patients.


Assuntos
Resposta ao Choque Frio/genética , Regulação da Expressão Gênica , Canais de Cátion TRPM/metabolismo , Fator de Necrose Tumoral alfa/genética , Fator de Necrose Tumoral alfa/metabolismo , Animais , Biomarcadores , Encéfalo/metabolismo , Isquemia Encefálica/metabolismo , Cálcio/metabolismo , Linhagem Celular , Humanos , Masculino , Camundongos , Camundongos Knockout , NF-kappa B/metabolismo , Transporte Proteico , RNA Interferente Pequeno/genética , Canal de Cátion TRPA1/metabolismo
3.
J Ethnopharmacol ; 195: 118-126, 2017 Jan 04.
Artigo em Inglês | MEDLINE | ID: mdl-27880884

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: The Angong Niuhuang Pill (ANP) is a well known Chinese traditional therapeutic for the treatment for diseases affecting the Central Nervous System (CNS). Components of the ANP formulation, including Bovis Calculus Sativus, Pulvis Bubali Comus Concentratus, Moschus, Margarita, Cinnabaris, Realgar, Coptidis Rhizoma, Scutellariae Radix, Gardeniae Fructus, Curcumae Radix, and Bomeolum Syntheticum, have been used for the treatment of stroke, encephalitis and emergency meningitis across Asia, especially in China for hundreds of years. OBJECTIVE: The goal of this study was to investigate the anti-atherosclerosis and cardio-protective effects of ANP administration using a rodent model of atherosclerosis induced by a high fat and vitamin D3. METHODS: Specific Pathogen-Free (SPF) 78 male SD rats were randomly divided into a control group and 5 atherosclerotic model groups. The atherosclerotic groups were divided to receive either Simvastatin (SVTT, 0.005g/kg), Low-dose ANP (0.125g/kg), Medium-dose ANP (0.25g/kg), and High-dose ANP (0.5g/kg). Following adaptive feeding for one week, atherosclerosis was induced and the atherosclerosis model was established. Experimental drugs (either simvastatin or ANP) or normal saline were administered intragastrically once daily for 9 weeks starting from the 8th week. A carotid artery ultrasound was performed at the 17th week to determine whether atherosclerosis had been induced. After the atherosclerosis model was successfully established, platelet aggregation rates, serum biochemical indices, apoptosis-related Bcl-2, Bax proteins levels in the heart were assayed. Pathological and histological analysis was completed using artery tissue from different experimental different groups to assess the effects of ANP. RESULTS: ANP significantly decreased aortic membrane thickness, the maximum platelet aggregation rates, and the ratio of low density lipoprotein cholesterol (LDL) to high density lipoprotein cholesterol (HDL). In addition, ANP significantly reduced serum contents of total cholesterol, low density lipoprotein, malondialdehyde, troponin I, high-sensitivity C-reactive protein, and lactate dehydrogenase. ANP markedly improved abnormal pathological conditions of the aorta and heart, and helped to prevent myocardial apoptosis. CONCLUSIONS: We have demonstrated that ANP has robust ant-atherosclerosis and cardio-protective effects on a high-fat and vitamin D3 - induced rodent model of atherosclerosis due to its antiplatelet aggregation, lipid regulatory, antioxidant, anti-inflammatory and anti-apoptotic properties.


Assuntos
Doenças da Aorta/prevenção & controle , Aterosclerose/prevenção & controle , Doenças das Artérias Carótidas/prevenção & controle , Colecalciferol , Dieta Hiperlipídica , Medicamentos de Ervas Chinesas/farmacologia , Hipolipemiantes/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Aorta Torácica/efeitos dos fármacos , Aorta Torácica/metabolismo , Aorta Torácica/ultraestrutura , Doenças da Aorta/sangue , Doenças da Aorta/induzido quimicamente , Doenças da Aorta/diagnóstico por imagem , Apoptose/efeitos dos fármacos , Aterosclerose/sangue , Aterosclerose/induzido quimicamente , Aterosclerose/diagnóstico por imagem , Biomarcadores/sangue , Doenças das Artérias Carótidas/sangue , Doenças das Artérias Carótidas/induzido quimicamente , Doenças das Artérias Carótidas/diagnóstico por imagem , Modelos Animais de Doenças , Enzimas/sangue , Inibidores de Hidroximetilglutaril-CoA Redutases/farmacologia , Mediadores da Inflamação/sangue , Lipídeos/sangue , Masculino , Miocárdio/patologia , Agregação Plaquetária/efeitos dos fármacos , Inibidores da Agregação de Plaquetas/farmacologia , Ratos Sprague-Dawley , Sinvastatina/farmacologia , Comprimidos , Fatores de Tempo
4.
Chin J Nat Med ; 14(5): 354-62, 2016 May.
Artigo em Inglês | MEDLINE | ID: mdl-27478098

RESUMO

Brazilein is reported to have immunosuppressive effect on cardiovascular and cerebral-vascular diseases. The essential roles of innate immunity in cerebral ischemia are increasingly identified, but no studies concerning the influence of brazilein on the innate immunity receptors have been reported. The present study was designed to investigate the regulation of NOD2 (Nucleotide-binding oligomerization domain-containing protein 2) by brazilein for its protection of neuron in cerebral ischemia in vivo and oxygen-glucose deprivation in vitro. The results showed that brazilein could reverse the elevated expression of NOD2 and TNFα (tumor necrosis factor alpha) elicited by cerebral ischemia and reperfusion. This reduction could also be detected in normal mice and C17.2 cells, indicating that this suppressive effect of brazilein was correlated with NOD2. The results from GFP reporter plasmid assay suggested brazilein inhibited NOD2 gene transcription. In conclusion, brazilein could attenuate NOD2 and TNFα expression in cerebral ischemia and NOD2 may be one possible target of brazilein for its immune suppressive effect in neuro-inflammation.


Assuntos
Benzopiranos/administração & dosagem , Isquemia Encefálica/tratamento farmacológico , Isquemia Encefálica/imunologia , Medicamentos de Ervas Chinesas/administração & dosagem , Indenos/administração & dosagem , Neurônios/efeitos dos fármacos , Proteína Adaptadora de Sinalização NOD2/genética , Proteína Adaptadora de Sinalização NOD2/metabolismo , Animais , Isquemia Encefálica/genética , Isquemia Encefálica/metabolismo , Células Cultivadas , Glucose/metabolismo , Humanos , Masculino , Camundongos , Camundongos Endogâmicos ICR , Neurônios/imunologia , Oxigênio/metabolismo , Fator de Necrose Tumoral alfa/genética , Fator de Necrose Tumoral alfa/imunologia
5.
Chin J Nat Med ; 14(6): 441-8, 2016 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-27473962

RESUMO

Brazilein is an active small molecular compound extracted from Caesalpinia sappan L. with favorable pharmacological properties on immune system, cardiovascular system, and nervous system. C. sappan has been used as a traditional medicine in China for hundreds of years for various diseases. However, the general reproductive toxicity of brazilein is still unknown. The purpose of the present study was to thoroughly evaluate the general reproductive toxicity of brazilein in ICR mice to support the future drug development and modernization of this potent traditional Chinese medicine. The results showed that, although no apparent toxicity on the reproducibility of the male was observed, brazilein might cause considerable risks to the fetuses and females as indicated by the ratios of dead fetuses and reabsorptions. In conclusion, our results from the present study provided some useful insights about the safety profile of brazilein, suggesting that brazilein should be used with caution in pregnant women.


Assuntos
Benzopiranos/toxicidade , Caesalpinia/toxicidade , Medicamentos de Ervas Chinesas/toxicidade , Indenos/toxicidade , Reprodução/efeitos dos fármacos , Animais , Feminino , Masculino , Camundongos , Camundongos Endogâmicos ICR , Gravidez
6.
Zhongguo Zhong Yao Za Zhi ; 41(12): 2362-2370, 2016 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-28901086

RESUMO

A variety of pharmacological effects of berberine (BBR) are constantly being discovered with the deepening of BBR research. What followed is how to rationally use the drug according to these new pharmacological effects. Because of some cardiac toxicity and poor oral absorption, conflicts may arise between improving the bioavailability and controlling the toxicity of BBR. Meanwhile some new therapeutic uses of BBR, such as hypolipidemia, hypoglycemia as well as prevention and treatment of neurodegenerative diseases, need long-termoral administration, thereby may lead to alteration of intestinal flora and potentially affect body's other physiological functions. Based on the stated targets of BBR and related pharmaceutical properties, comprehensive analysis of these issues was conducted in this study. Some suggestions were presented below:the effect of long-term oral administration on body function, especially the intestinal flora, needs to be further investigated; risks shall be considered in changing the composition of the formulation to improve the absorption rate of oral administration; for the medication with higher concentration demand (such as anti-cancer), targeted drug-delivery is worthy to be considered.


Assuntos
Berberina/farmacologia , Administração Oral , Berberina/administração & dosagem , Disponibilidade Biológica , Microbioma Gastrointestinal/efeitos dos fármacos , Humanos
7.
Sci Rep ; 5: 18326, 2015 Dec 16.
Artigo em Inglês | MEDLINE | ID: mdl-26671652

RESUMO

Berberine (BBR) is a natural compound with variable pharmacological effects and a broad panel of target genes. We investigated berberine's pharmacological activities from the perspective of its nucleotide-binding ability and discovered that BBR directly regulates gene expression by targeting TATA boxes in transcriptional regulatory regions as well as the poly adenine (poly (A)) tail at the mRNA terminus. BBR inhibits gene transcription by binding the TATA boxes in the transcriptional regulatory region, but it promotes higher levels of expression by targeting the poly (A) tails of mRNAs. The present study demonstrates that TATA boxes and poly (A) tails are the first and second primary targets by which BBR regulates gene expression. The final outcome of gene regulation by BBR depends on the structure of the individual gene. This is the first study to reveal that TATA boxes and poly (A) tails are direct targets for BBR in its regulation of gene expression. Our findings provide a novel explanation for the complex activities of a small molecule compound in a biological system and a novel horizon for small molecule-compound pharmacological studies.


Assuntos
Regiões 3' não Traduzidas , Berberina/farmacocinética , Regulação da Expressão Gênica/efeitos dos fármacos , Poli A , Estabilidade de RNA/efeitos dos fármacos , TATA Box , Transcrição Genética/efeitos dos fármacos , Animais , Masculino , Camundongos , Camundongos Endogâmicos ICR
8.
PLoS One ; 10(7): e0134044, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26226164

RESUMO

The purpose of the present study is to confirm the protective effect of berberine (BBR) on gastrointestinal injury caused by acute heavy alcohol exposure, an effect that has not been reported previously. Our research details how BBR protects against gastrointestinal injuries from acute alcohol exposure using both in vivo and in vitro experiments. Acute high alcohol concentrations lead to obvious damage to the gastrointestinal mucosa, resulting in necrosis of the intestinal mucosa. Oral administration of BBR was able to significantly reduce this alcohol-induced damage, inhibit increases of alcohol-induced TNFα and IL-1ß expression in gastrointestinal mucosa as well as their upstream signals TLR2 and TLR4, and regulate cytokines that modulate tight junctions. Alcohol consumption is a popular human social behavior worldwide, and the present study reports a comprehensive mechanism by which BBR protects against gastrointestinal injuries from alcohol stress, providing people with a novel application of BBR.


Assuntos
Alcoolismo/complicações , Berberina/uso terapêutico , Mucosa Gástrica/efeitos dos fármacos , Interleucina-1beta/fisiologia , Mucosa Intestinal/efeitos dos fármacos , Transdução de Sinais/efeitos dos fármacos , Receptor 2 Toll-Like/fisiologia , Fator de Necrose Tumoral alfa/fisiologia , Animais , Western Blotting , Células CACO-2/efeitos dos fármacos , Mucosa Gástrica/patologia , Células HEK293/efeitos dos fármacos , Humanos , Interleucina-1beta/efeitos dos fármacos , Mucosa Intestinal/patologia , Masculino , Camundongos , Camundongos Endogâmicos ICR , Reação em Cadeia da Polimerase em Tempo Real , Receptor 2 Toll-Like/efeitos dos fármacos , Fator de Necrose Tumoral alfa/efeitos dos fármacos
9.
Zhongguo Zhong Yao Za Zhi ; 39(16): 3142-7, 2014 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-25509303

RESUMO

Pineapple (Ananas comosus) leaves contain mainly phenolic components with antioxidant and hypolipidemic effects. One of the principle components is p-coumaric acid. In this study, the transport behavior of p-coumaric acid, was observed after the administration of pineapple leaf phenols in vitro. Simultaneously, the effect of the phenols on glucose, total cholesterol and triglycerides transportation and metabolism in HepG2 cells was also observed. The results showed that the phenols had good transport characteristics. 5 min after the administration, p-coumaric acid of the phenols could be detected, and the content of p-coumaric acid reached the peak concentration after 60 min of the administration. p-coumaric acid of phenols have time-and dose-dependent manner. While promoting glucose transporter (GLUT4) and low density lipoprotein receptor (LDLR) expression, the phenols decreased intracellular lipid content. This reduction of intracellular lipid content was highly correlated with the promotion of lipoprotein lipase (LPL) and hepatic triglyceride lipase (HTGL) expression, while the reduction of intracellular glucose levels was correlated with glycogen synthesis in the cells.


Assuntos
Glucose/metabolismo , Metabolismo dos Lipídeos/efeitos dos fármacos , Extratos Vegetais/farmacologia , Folhas de Planta/química , Ananas/química , Transporte Biológico/efeitos dos fármacos , Colesterol/metabolismo , Células Hep G2 , Humanos
10.
PLoS One ; 9(11): e112937, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-25402492

RESUMO

The anti-cancer activities of berberine (BBR) have been reported extensively in various cancer cell lines. However, the minimal inhibitory concentrations of BBR varied greatly among different cell lines and very few studies have been devoted to elucidate this aspect. In this study, we employed three cancer cell lines, HepG2, HeLa and SY5Y, to compare the transportation and distribution of BBR. HPLC results demonstrated that BBR was capable of penetrating all the cell lines whereas the cumulative concentrations were significantly different. HepG2 cells accumulated higher level of BBR for longer duration than the other two cell lines. Molecular docking studies revealed the BBR binding site on P-glycoprotein 1 (P-gp). In addition, we elucidated that BBR regulated P-gp at both mRNA and protein levels. BBR induced the transcription and translation of P-gp in HeLa and SY5Y cells, whereas BBR inhibited P-gp expression in HepG2 cells. Further study showed that BBR regulates P-gp expression depending on different mechanisms (or affected by different factors) in different cell lines. To summarize, our study has revealed several mechanistic aspects of BBR regulation on P-gp in different cancer cell lines and might shed some useful insights into the use of BBR in the anti-cancer drug development.


Assuntos
Antineoplásicos Fitogênicos/metabolismo , Antineoplásicos Fitogênicos/farmacologia , Berberina/metabolismo , Berberina/farmacologia , Membro 1 da Subfamília B de Cassetes de Ligação de ATP/química , Membro 1 da Subfamília B de Cassetes de Ligação de ATP/metabolismo , Antineoplásicos Fitogênicos/química , Berberina/química , Transporte Biológico , Linhagem Celular Tumoral , Expressão Gênica , Células HeLa , Células Hep G2 , Humanos , Cinética , Modelos Moleculares , Conformação Molecular , Ligação Proteica
11.
PLoS One ; 9(9): e108000, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-25275506

RESUMO

Brazilein, a natural small molecule, shows a variety of pharmacological activities, especially on nervous system and immune system. As a potential multifunctional drug, we studied the distribution and the transport behavior and metabolic behavior of brazilein in vivo and in vitro. Brazilein was found to be able to distribute in the mouse brain and transport into neural cells. A metabolite was found in the brain and in the cells. Positive and negative mode-MS/MS and Q-TOF were used to identify the metabolite. MS/MS fragmentation mechanisms showed the methylation occurred at the 10-hydroxyl of brazilein (10-O-methylbrazilein). Further, catechol-O- methyltransferase (COMT) was confirmed as a crucial enzyme correlated with the methylated metabolite generation by molecular docking and pharmacological experiment.


Assuntos
Benzopiranos/metabolismo , Indenos/metabolismo , Neurônios/metabolismo , Animais , Benzopiranos/administração & dosagem , Benzopiranos/química , Benzopiranos/farmacologia , Transporte Biológico/efeitos dos fármacos , Encéfalo/metabolismo , Catecol O-Metiltransferase/química , Catecol O-Metiltransferase/metabolismo , Morte Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Complexo IV da Cadeia de Transporte de Elétrons/antagonistas & inibidores , Complexo IV da Cadeia de Transporte de Elétrons/metabolismo , Indenos/administração & dosagem , Indenos/química , Indenos/farmacologia , Masculino , Metilação/efeitos dos fármacos , Camundongos Endogâmicos ICR , Neurônios/efeitos dos fármacos , Células PC12 , Ratos , Reprodutibilidade dos Testes , Espectrometria de Massas em Tandem , Temperatura Ambiente , Raios Ultravioleta
12.
PLoS One ; 9(6): e90850, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24603897

RESUMO

Berberine is one kind of isoquinoline alkaloid with anti-apoptotic effects on the neurons suffering ischemia. To address the explanation for these activities, the berberine-induced cell cycle arrest during neurons suffering ischemia/reperfusion had been studied in the present study. According to the in vitro neurons with oxygen-glucose deprivation and in vivo ICR mice with cerebral ischemia/reperfusion, it was found that berberine could protect the mRNA of retinoblastoma (Rb) from degradation through its function on the poly(A) tail. The prolonged half-life of retinoblastoma 1 (gene of Rb, RB1) mRNA level secures the protein level of retinoblastoma, which facilitates cell cycle arrest of neurons in the process of ischemia/reperfusion and subsequently avoids cells entering in the apoptotic process. The poly(A) tail of RB1 mRNA, as a newly identified target of berberine, could help people focus on the interaction between berberine and mRNA to further understand the biological activities and functions of berberine.


Assuntos
Berberina/farmacologia , Isquemia Encefálica/tratamento farmacológico , Fármacos Neuroprotetores/farmacologia , Estabilidade de RNA/efeitos dos fármacos , RNA Mensageiro/metabolismo , Proteína do Retinoblastoma/genética , Animais , Apoptose , Pontos de Checagem do Ciclo Celular , Sobrevivência Celular/efeitos dos fármacos , Hipocampo/efeitos dos fármacos , Hipocampo/patologia , Masculino , Camundongos Endogâmicos ICR , Células PC12 , Fosforilação , Regiões Promotoras Genéticas , Processamento de Proteína Pós-Traducional , RNA Mensageiro/genética , Ratos , Traumatismo por Reperfusão/prevenção & controle , Proteína do Retinoblastoma/metabolismo
13.
Zhongguo Zhong Yao Za Zhi ; 38(16): 2639-44, 2013 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-24228579

RESUMO

Activation pattern recognition receptors can cause the startup of downstream signaling pathways, the expression of inflammatory factors, and finally immunological inflammatory reaction. Either exogenous pathogenic microorganisms or endogenous tissue components can activate these pattern recognition receptors as ligands at varying degrees, and then cause the immunological inflammatory reaction. Therefore, it is of great significance to inhibit relevant receptors, as well as the immunological inflammatory reaction, in order to avoid tissue injury during the course of disease. Baicalin is able to specifically inhibit the expression of TLR2/4-NOD2, inhibit the expression of inflammatory factors IL-1beta, IL-6 and TNF-alpha, and thereby reducing the injury of the tissue cells during the course of disease. This effect is non-specific with tissues, which is of great theoretical and practical significance in druggability. In addition, the drug metabolism and toxicity of baicalin are also discussed for its druggability in this article.


Assuntos
Flavonoides/farmacologia , Proteína Adaptadora de Sinalização NOD2/metabolismo , Receptor 2 Toll-Like/metabolismo , Receptor 4 Toll-Like/metabolismo , Animais , Humanos
14.
Chin J Nat Med ; 11(3): 231-9, 2013 May.
Artigo em Inglês | MEDLINE | ID: mdl-23725834

RESUMO

AIM: Euphorbia kansui (E. KS) is a traditional medicine used in China for thousands of years with the effect of propulsion in the gastrointestines. However, there is no reported study of E. KS on gastrointestinal motility until now. The aim of this work is to study the effect of E. KS on the propulsion of gastrointestines, and to elucidate the possible mechanism of action. METHODS: E.KS was prepared as a 30% ethanol extract and used for the experiment of small and large intestines of mice by oral administration with three different dosages (1.2, 0.6 and 0.3 g·kg(-1)). The feces were observed in vivo. The morphology was carried out to detect if there are any changes in the intestines after the extract of E. KS administration. The assays of mRNA and protein expression were employed to observe IL-1ß, TNFα and caspase 3. RESULTS: It was shown that the extract of E.KS promoted diarrhea in mouse feces after administration, inhibited the contraction of smooth muscle of mouse small intestine and caused the inflammatory exudation on the mucosa of the intestines, enhanced the expression of both mRNA and the protein levels of IL-1ß and TNFα in the small or large intestines. CONCLUSION: The results showed that the extract of E. KS acted on the intestinal smooth muscle with propulsion of feces involving the irritation of the intestines with acute inflammatory reactions.


Assuntos
Diarreia/imunologia , Medicamentos de Ervas Chinesas/efeitos adversos , Euphorbia/efeitos adversos , Animais , Diarreia/etiologia , Diarreia/genética , Diarreia/fisiopatologia , Medicamentos de Ervas Chinesas/administração & dosagem , Euphorbia/química , Feminino , Motilidade Gastrointestinal/efeitos dos fármacos , Humanos , Interleucina-1beta/genética , Interleucina-1beta/imunologia , Intestinos/efeitos dos fármacos , Intestinos/fisiopatologia , Masculino , Camundongos , Camundongos Endogâmicos ICR , Músculo Liso/efeitos dos fármacos , Músculo Liso/fisiopatologia , Raízes de Plantas/efeitos adversos , Raízes de Plantas/química , Fator de Necrose Tumoral alfa/genética , Fator de Necrose Tumoral alfa/imunologia
15.
Eur J Pharmacol ; 708(1-3): 44-55, 2013 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-23499694

RESUMO

Berberine acted as a natural medicine with multiple pharmacological activities. In the present study, we examined the effect of berberine against cerebral ischemia damage from cell cycle arrest and cell survival. Oxygen-glucose deprivation of PC12 cells and primary neurons, and carotid artery ligation in mice were used as in vitro and in vivo cerebral ischemia models. We found that the effect of berberine on cell cycle arrest during ischemia was mediated by decreased p53 and cyclin D1, increased phosphorylation of Bad (higher expression of p-Bad and higher ratio of p-Bad to Bad) and decreased cleavage of caspase 3. Meanwhile, berberine activated the PI3K/Akt pathway during the reperfusion, especially the phosphor-activation of Akt, to promote the cell survival. The neural protective effect of berberine was remained in the presence of inhibitor of mitogen-activated protein/extracellular signal-regulated kinase (MEK), but was suppressed by the inhibitors of PI3K and Akt. We demonstrated that berberine induced cell cycle arrest and cell survival to resist cerebral ischemia injury.


Assuntos
Berberina/farmacologia , Isquemia Encefálica/metabolismo , Fármacos Neuroprotetores/farmacologia , Traumatismo por Reperfusão/metabolismo , Animais , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Ciclina D1/genética , Ciclina D1/metabolismo , Hipocampo/efeitos dos fármacos , Hipocampo/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos ICR , Neurônios/efeitos dos fármacos , Neurônios/metabolismo , Células PC12 , Fosfatidilinositol 3-Quinases/genética , Fosfatidilinositol 3-Quinases/metabolismo , Proteínas Proto-Oncogênicas c-akt/genética , Proteínas Proto-Oncogênicas c-akt/metabolismo , RNA Mensageiro/metabolismo , Ratos , Ratos Wistar , Proteína Supressora de Tumor p53/genética , Proteína Supressora de Tumor p53/metabolismo
16.
PLoS One ; 8(1): e54234, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-23335996

RESUMO

The purpose of this study was to assess the effects of berberine (BBR) on thermoregulation in mice exposed to hot (40°C) and cold (4°C) environmental conditions. Four groups of mice were assembled with three different dosages of BBR (0.2, 0.4, and 0.8 mg/kg) and normal saline (control). In room temperature, our largest dosage of BBR (0.8 mg/kg) can reduce rectal temperatures (Tc) of normal mice. In hot conditions, BBR can antagonize the increasing core body temperature and inhibit the expression of HSP70 and TNFα in mice; conversely, in cold conditions, BBR can antagonize the decreasing core body temperature and enhance the expression of TRPM8. This study demonstrates the dual ability of BBR in maintaining thermal balance, which is of great relevance to the regulation of HSP70, TNFα and TRPM8.


Assuntos
Berberina/farmacologia , Regulação da Temperatura Corporal/efeitos dos fármacos , Regulação da Temperatura Corporal/fisiologia , Temperatura Baixa , Temperatura Alta , Animais , Berberina/administração & dosagem , Eletrocardiografia , Regulação da Expressão Gênica/efeitos dos fármacos , Proteínas de Choque Térmico HSP70/antagonistas & inibidores , Proteínas de Choque Térmico HSP70/genética , Proteínas de Choque Térmico HSP70/metabolismo , Masculino , Camundongos , Atividade Motora/efeitos dos fármacos , Atividade Motora/genética , Canais de Cátion TRPM/genética , Canais de Cátion TRPM/metabolismo , Fator de Necrose Tumoral alfa/genética , Fator de Necrose Tumoral alfa/metabolismo
17.
Chin Med J (Engl) ; 125(9): 1586-93, 2012 May.
Artigo em Inglês | MEDLINE | ID: mdl-22800826

RESUMO

BACKGROUND: Baicalin has a significant anti-inflammation effect and is widely used in the clinical treatment of stroke. Most of the studies of Toll-like receptor 2/4 (TLR2/4) during cerebral ischemia had defined their specific expressions in microglia in hippocampus tissue. To explore the targets of baicalin in stroke, we detected the expressions of TLR2/4 in vitro/vivo. METHODS: By constructing a cerebral ischemia-reperfusion model in vivo and glucose oxygen deprivation model, we successfully induced neuron damage, then added baicalin and detected expressions of TLR2/4, nuclear factor-kB (NF-kB), tumor necrosis factor-alpha (TNFα), and interleukin-1ß (IL-1ß) in mRNA level and protein level. RESULTS: We found distinct upregulations of TLR2/4 and TNFα in both mRNA level and protein level in PC12 cells and primary neurons. Moreover, TLR2/4 and TNFα expressions were significantly higher in mice hippocampus treated with cerebral ischemia-reperfusion. Baicalin could downregulate the expressions of TLR2/4 and TNFα in the damaged cells and mice hippocampus effectively. CONCLUSIONS: Neurons could respond to the damage and activate the related signal pathway directly. TLR2/4 responsed to the damage and sent the signal to downstream factor TNFα through activating NF-kB. Baicalin could inhibit the inflammatory reaction in neuron damage and TLR might be its targets, which explained why baicalin could widely be used in the clinical treatment of stroke.


Assuntos
Isquemia Encefálica/tratamento farmacológico , Isquemia Encefálica/metabolismo , Flavonoides/uso terapêutico , Traumatismo por Reperfusão/tratamento farmacológico , Traumatismo por Reperfusão/metabolismo , Receptor 2 Toll-Like/metabolismo , Receptor 4 Toll-Like/metabolismo , Animais , Isquemia Encefálica/genética , Células Cultivadas , Feminino , Interleucina-1beta/genética , Interleucina-1beta/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos ICR , NF-kappa B/genética , NF-kappa B/metabolismo , Neurônios/efeitos dos fármacos , Neurônios/metabolismo , Células PC12 , Ratos , Traumatismo por Reperfusão/genética , Receptor 2 Toll-Like/genética , Receptor 4 Toll-Like/genética , Fator de Necrose Tumoral alfa/genética , Fator de Necrose Tumoral alfa/metabolismo
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