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1.
Molecules ; 24(9)2019 May 02.
Artigo em Inglês | MEDLINE | ID: mdl-31052610

RESUMO

BACKGROUND: The aim of this study was to simplify and identify the contents of the herbal formula, HBX-5. This study was carried out to evaluate the therapeutic effects of HBX-6 in a mouse model of benign prostatic hyperplasia (BPH). Based on in vitro, we selected a candidate, reconstituted an experimental agent and investigated the effects on testosterone-induced BPH rats. Cell viability was determined by MTT assay in RWPE-1 and WPMY-1 cells. The expression of androgen receptor (AR) was measured in dihydrotestosterone-stimulated RWPE-1 and WPMY-1 cells. BPH was induced in mice by a subcutaneous injection of testosterone propionate for four weeks. Animals were divided into six groups: Group 1, control mice; Group 2, mice with BPH; Group 3, mice with BPH treated with finasteride; Group 4, mice with BPH treated with 200 mg/kg HBX-5; Group 5, mice with BPH treated with 100 mg/kg HBX-6; and Group 6, mice with BPH treated with 200 mg/kg HBX-6. Changes in prostate weight were measured after treatments, and the thickness of the epithelium was evaluated. The expression levels of proteins associated with prostatic cell proliferation and cell cycle-related proteins were determined. Based on previous reports and in vitro results, we selected Cornus officinalis and Psoralea corylifolia among HBX-5 components and reconstituted the experimental agent, and named it HBX-6. The result represented a new herbal formula, HBX-6 that suppressed the pathological alterations in BPH and showed a marked reduction in proliferation-related protein expression compared to mice with BPH. Our results indicate that HBX-6 has a better therapeutic effect in the BPH murine model than those of HBX-5 and finasteride, suggesting the role of HBX-6 as a new BPH remedial agent.


Assuntos
Cornus/química , Fator de Transcrição E2F1/antagonistas & inibidores , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Hiperplasia Prostática/metabolismo , Psoralea/química , Animais , Ciclo Celular , Linhagem Celular , Proliferação de Células , Sobrevivência Celular/efeitos dos fármacos , Modelos Animais de Doenças , Regulação da Expressão Gênica/efeitos dos fármacos , Humanos , Masculino , Camundongos , Hiperplasia Prostática/tratamento farmacológico , Hiperplasia Prostática/patologia , Receptores Androgênicos/genética , Receptores Androgênicos/metabolismo
2.
Molecules ; 23(10)2018 Oct 14.
Artigo em Inglês | MEDLINE | ID: mdl-30322186

RESUMO

Benign prostatic hyperplasia (BPH), an age-dependent disorder with a prevalence percentage of 60% in the 60s, has been found to involve an androgenic hormone imbalance that causes confusion between cell apoptosis and proliferation. Because general medications for BPH treatment have undesirable side effects, the development of effective alternative medicines has been considered. HBX-5 is a newly developed formula with the aim of improving BPH, and is composed of nine medicinal herbs. BPH was induced in the rats by intramuscular injection of testosterone propionate after castration. Rats were divided into six groups, and the efficacy of HBX-5 on testosterone-induced BPH in rats was estimated. In addition, RWPE-1 and WPMY-1 cells were used to demonstrate the effect of HBX-5 on BPH in vitro model. Compared with the control group, HBX-5 administration group suppressed BPH manifestations, such as excessive development of prostate, and increase of serum dihydrotestosterone and 5α-reductase concentrations. Furthermore, immunohistochemistry analysis revealed that HBX-5 significantly decreased the expression of androgen receptor (AR) and proliferating cell nuclear antigen (PCNA). In addition, results of RWPE-1 and WPMY-1 cells showed that HBX-5 inhibited the over-expression of AR and PSA in DHT-induced prostate hyperplastic microenvironments.


Assuntos
Extratos Vegetais/administração & dosagem , Plantas Medicinais/química , Hiperplasia Prostática/tratamento farmacológico , Propionato de Testosterona/efeitos adversos , 3-Oxo-5-alfa-Esteroide 4-Desidrogenase/sangue , Animais , Linhagem Celular , Di-Hidrotestosterona/sangue , Modelos Animais de Doenças , Progressão da Doença , Regulação da Expressão Gênica/efeitos dos fármacos , Humanos , Injeções Intramusculares , Masculino , Extratos Vegetais/farmacologia , Antígeno Nuclear de Célula em Proliferação/metabolismo , Hiperplasia Prostática/sangue , Hiperplasia Prostática/induzido quimicamente , Ratos , Receptores Androgênicos/metabolismo
3.
Nat Prod Res ; 30(6): 705-9, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-25942587

RESUMO

Allergic contact dermatitis (ACD) is a prototypic T-cell-mediated cutaneous inflammatory response. In the present study we describe the anti-allergic effect of topically applied Scutellaria bacalensis aqueous extract (WSBE) in suppressing 2,4-dinitrochlorobenzene (DNCB)-induced ACD in BALB/c mice. Topically applied WSBE attenuated the epidermal thickness and mast cell infiltration into the skin in DNCB-induced contact dermatitis. Furthermore, WSBE suppressed DNCB-induced production of serum IgE as well as IL-4, IFN-γ, and TNF-α in the skin. Topical application of WSBE also ameliorated the significant decrease in dermal glutathione and superoxide dismutase levels. Moreover, present results demonstrated that the baicalin, bioactive compound of WSBE, was able to penetrate into the skin following topical application, which was confirmed by the HPLC analysis using rat model. Taken together, topical application of WSBE exerts beneficial effects in contact dermatitis model, suggesting that WSBE might be a candidate for the treatment of contact dermatitis.


Assuntos
Antialérgicos/farmacologia , Dermatite de Contato/tratamento farmacológico , Extratos Vegetais/farmacologia , Scutellaria baicalensis/química , Pele/efeitos dos fármacos , Administração Cutânea , Animais , Dinitroclorobenzeno , Feminino , Flavonoides/farmacologia , Imunoglobulina E/sangue , Interferon gama/metabolismo , Interleucina-4/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Ratos , Ratos Sprague-Dawley , Fator de Necrose Tumoral alfa/metabolismo
4.
Planta Med ; 79(11): 959-62, 2013 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-23818268

RESUMO

Scutellaria baicalensis has been used as a traditional herbal medicine for bronchitis, hepatitis, and allergic diseases. The root of Scutellaria baicalensis contains active flavonoid components, including baicalin, baicalein, wogonoside, and wogonin, which have pharmaceutical properties. In the present study, the antiallergic properties of a standardized aqueous extract of S. baicalensis were evaluated, and the skin toxicity of its dermal application was also determined. The in vivo and in vitro assays were performed by using the ß-hexosaminidase assay in rat basophilic leukemia cells (RBL-2H3) and cutaneous skin reaction in BALB/c mice, respectively. In addition, the acute dermal irritation/corrosion test was carried out in New Zealand white rabbits, and the skin sensitization test was conducted by Buhler's method in Hartley guinea pigs to estimate the safety of the standardized aqueous extract of S. baicalensis for topical application. ß-Hexosaminidase release in RBL-2H3 was markedly decreased following treatment with the standardized aqueous extract of S. baicalensis. It also ameliorated antigen-induced ear swelling compared with the control group in BALB/c mice. In the toxicological studies, it did not induce any dermal irritation/corrosion in rabbits or skin sensitization in guinea pigs. Although still limited, these results concerning the toxicological effects of S. baicalensis could be an initial step toward the topical application of S. baicalensis extracts on hypersensitive skin.


Assuntos
Antialérgicos/farmacologia , Flavonoides/farmacologia , Hipersensibilidade , Extratos Vegetais/farmacologia , Administração Tópica , Animais , Antialérgicos/química , Antialérgicos/isolamento & purificação , Linhagem Celular Tumoral , Flavanonas/química , Flavanonas/isolamento & purificação , Flavanonas/farmacologia , Flavonoides/química , Flavonoides/isolamento & purificação , Glucosídeos/química , Glucosídeos/isolamento & purificação , Glucosídeos/farmacologia , Cobaias , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Raízes de Plantas/química , Plantas Medicinais , Coelhos , Ratos , Scutellaria baicalensis/química , Pele/efeitos dos fármacos , beta-N-Acetil-Hexosaminidases/análise
5.
J Vet Med Sci ; 75(1): 89-92, 2013 Jan 31.
Artigo em Inglês | MEDLINE | ID: mdl-22878539

RESUMO

The aim of the present study was to investigate the influence of different injection sites, i.e., the neck area and thigh muscle, on the pharmacokinetics of cefquinome in piglets following intramuscular (i.m.) injection. Cross-bred (Landrace × Duroc × Yorkshire) piglets were administered the same dose of cefquinome (2 mg/kg body weight) via intravenous injection and intramuscular injection into the neck area or thigh. The mean maximum concentrations (C(max)) of cefquinome following i.m. injection into neck or thigh area were 4.62 ± 0.31 µg/ml at 0.38 ± 0.14 hr and 4.39 ± 0.53 µg/ml at 0.42 ± 0.13 hr, respectively. The absolute bioavailabilities (F) of cefquinome after i.m. injection into the neck or thigh area were 103.04 ± 13.01 and 97.56 ± 16.14%, respectively (P>0.05). There were no differences noted between the two different injection sites for the pharmacokinetic properties of cefquinome after i.m. injection in piglets. Further studies will be needed to determine the incidence or severity of injection site reactions following repeated administrations of cefquinome into both injection sites.


Assuntos
Cefalosporinas/farmacocinética , Injeções Intramusculares/métodos , Injeções Intramusculares/veterinária , Sus scrofa/metabolismo , Análise de Variância , Animais , Disponibilidade Biológica , Cefalosporinas/administração & dosagem , Cromatografia Líquida/veterinária , Estudos Cross-Over , Cruzamentos Genéticos , Espectrometria de Massas/veterinária , Pescoço , Coxa da Perna
6.
Pharm Biol ; 50(12): 1473-8, 2012 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-23035893

RESUMO

CONTEXT: The root of Platycodon grandiflorum (Jacq.) A. DC. (Campanulaceae) has been widely studied for its hepatoprotective effects against various hepatotoxicants. OBJECTIVE: The present study evaluated the protective effect of the standardized aqueous extract of P. grandiflorum (BC703) on cholestasis-induced hepatic injury in mice. MATERIALS AND METHODS: BC703 is a standardized aqueous extract of P. grandiflorum in reference to platycodin D (at least 0.8%). The mice were allocated into five groups as follows: Sham-operated, bile duct ligation (BDL) alone, and BDL with BC703 (1, 5, and 10 mg/kg BW) treated group. BC703 was given for 3 consecutive days before BDL operation. The animals were sacrificed by CO2 anesthesia post-24 h of BDL operations. RESULTS AND DISCUSSION: Serum alanine aminotransferase and serum aspartate aminotransferase increased to 395.2 ± 90.0 and 266.0 ± 45.6 Unit/L in the BDL alone group and decreased with BC703 in a dose-dependent manner. Especially the 10 mg/kg of BC703-treated mice showed a 77% decrease of serum alanine aminotransferase and 56% of aspartate aminotransferase as compared with BDL alone. Decreased antioxidant enzyme levels in BDL alone group were elevated in BC703-treated groups ranging from 7 to 29% for glutathione and from 13 to 25% for superoxide dismutase. BC703 treatment also attenuated malondialdehyde (from 3 to 32%) and nitric oxide levels (from 32 to 50%) as compared with BDL alone. Histopathological studies further confirmed the hepatoprotective effect of BC703 in BDL-induced cholestesis. CONCLUSION: BC703 could attenuate liver injury by BDL in mice, and test results indicate that BC703 might be useful in cholestatic liver injury.


Assuntos
Colestase Extra-Hepática/tratamento farmacológico , Hepatopatias/prevenção & controle , Fígado/efeitos dos fármacos , Extratos Vegetais/farmacologia , Platycodon , Substâncias Protetoras/farmacologia , Alanina Transaminase/sangue , Animais , Aspartato Aminotransferases/sangue , Biomarcadores/sangue , Colestase Extra-Hepática/sangue , Colestase Extra-Hepática/etiologia , Colestase Extra-Hepática/patologia , Cromatografia Líquida de Alta Pressão , Ducto Colédoco/cirurgia , Citoproteção , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Glutationa/metabolismo , Ligadura , Fígado/enzimologia , Fígado/patologia , Hepatopatias/sangue , Hepatopatias/etiologia , Hepatopatias/patologia , Masculino , Malondialdeído/metabolismo , Camundongos , Camundongos Endogâmicos ICR , Óxido Nítrico/metabolismo , Extratos Vegetais/análise , Extratos Vegetais/isolamento & purificação , Raízes de Plantas , Plantas Medicinais , Platycodon/química , Substâncias Protetoras/análise , Substâncias Protetoras/isolamento & purificação , Superóxido Dismutase/metabolismo , Substâncias Reativas com Ácido Tiobarbitúrico/metabolismo , Fatores de Tempo
7.
J Nutr Sci Vitaminol (Tokyo) ; 58(3): 187-94, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-22878389

RESUMO

The present study aims to evaluate the anti-HCV activity of hotwater extract from Platycodon grandiflorum (BC703) with HCV genotype 1b subgenomic replicon system and investigate its hepatoprotective activity on carbon tetrachloride (CCl(4))-induced acute liver damage in mice. BC703 produced significant hepatoprotective effects against CCl(4)-induced acute hepatic injury by decreasing the activities of serum enzymes, nitric oxide and lipid peroxidation. Histopathological studies further substantiated the protective effect of BC703. Furthermore, BC703 inhibited the HCV RNA replication with an EC(50) value and selective index (CC(50)/EC(50)) of 2.82 µg/mL and above 35.46, respectively. However, digested BC703 using a simulated gastric juice showed poor protective effect against CCl(4)-induced hepatotoxicity in mice and decreased anti-HCV activity as compared to the intact BC703. Although further studies are necessary, BC703 may be a beneficial agent for the management of acute hepatic injury and chronic HCV infection.


Assuntos
Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Hepacivirus/efeitos dos fármacos , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Platycodon/química , Animais , Hepatite C/prevenção & controle , Masculino , Camundongos , Camundongos Endogâmicos ICR , Fitoterapia , Extratos Vegetais/química
8.
Exp Anim ; 61(1): 71-5, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-22293675

RESUMO

This study was conducted to evaluate the oral absorption of enrofloxacin (ENFX) in rats when administered with orange oil or its main component, limonene. Compared with the group administered ENFX alone, the ENFX + limonene group did not show any significant difference in the absorption of ENFX, whereas the extent and rate of absorption of ENFX were significantly decreased in the ENFX + orange oil group (C(max), -43%; T(max), 129%). In addition, t(1/2λz) and MRT of ENFX were prolonged by the concomitant administration of orange oil. The AUCs of ENFX were not affected in the ENFX + orange oil group. These results suggest that decreased oral absorption could reduce the efficacy of ENFX therapy in animals.


Assuntos
Antibacterianos/farmacocinética , Cicloexenos/farmacocinética , Fluoroquinolonas/farmacocinética , Óleos Vegetais/farmacocinética , Terpenos/farmacocinética , Absorção/efeitos dos fármacos , Administração Oral , Animais , Antibacterianos/administração & dosagem , Antibacterianos/sangue , Cicloexenos/administração & dosagem , Cicloexenos/sangue , Combinação de Medicamentos , Interações Medicamentosas , Enrofloxacina , Fluoroquinolonas/administração & dosagem , Fluoroquinolonas/sangue , Limoneno , Masculino , Óleos Vegetais/administração & dosagem , Ratos , Ratos Sprague-Dawley , Terpenos/administração & dosagem , Terpenos/sangue
9.
Toxicol Res ; 28(4): 263-8, 2012 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-24278619

RESUMO

The aim of this study was to investigate the acute oral toxicity of fermented Scutellariae Radix (JKTMHGu- 100) in rats and dogs. JKTM-HGu-100 was orally administered at a dose of 2,000 mg/kg in Sprague-Dawley rats. An escalating single-dose oral toxicity test in beagle dogs was performed at doses of 500, 1000, and 2000 mg/kg with 4-day intervals. Clinical signs, changes in body weight, mortality, and necropsy findings were examined for 2 weeks following oral administration. No toxicological changes related to the test substance nor mortality was observed after administration of a single oral dose of JKTM-HGu-100 in rats or dogs. Therefore, the approximate lethal dose (LD) for oral administration of JKTMHGu-100 in rats was considered to be over 2,000 mg/kg, and the maximum tolerance doses (MTDs) in rats and dogs were also estimated to be over 2,000 mg/kg. These results indicate that JKTM-HGu-100 shows no toxicity in rodents or non-rodents at doses of 2,000 mg/kg or less.

10.
J Vet Sci ; 12(2): 115-9, 2011 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-21586869

RESUMO

The isoflavonol glycoside Talosin A, genistein (GT)-7-α-L-6-deoxy talopyranose (GT-Tal), was first isolated from the culture broth of Kitasatospora kifunensis MJM341. The aim of the present study was to evaluate the oral absorption and metabolism of the newly isolated isoflavonol glycoside, GT-Tal compared to genistin (GT-7-O-ß-D-glucopyranoside; GT-Glu). Free GT-Glu and GT-Tal could not be detected prior to enzymatic hydrolysis of the corresponding conjugates in rat plasma. Following oral administration of GT-Tal (15 min), GT-Tal was rapidly absorbed through the gastrointestinal tract and metabolized into GT-Tal conjugates with a mean C(max) of 2.74 µg/mL. GT-Tal was further metabolized to its aglycone, free GT and conjugated GT. After oral administration, GT-Glu was absorbed after being converted to its aglycone and then further metabolized into its conjugate metabolites (free GT with a mean C(max) of 0.24 mg/mL at 1.25 h; conjugated GT with a mean C(max) of 1.31 mg/mL at 2.00 h). Significant differences in absorption and metabolism of GT-Tal and GT-Glu were observed. GT-Tal was metabolized into its corresponding conjugates or underwent deglycosylation to form GT, whereas GT-Glu was metabolized into its aglycone, GT.


Assuntos
Actinobacteria/química , Glicosídeos/metabolismo , Isoflavonas/metabolismo , Administração Oral , Animais , Área Sob a Curva , Glicosídeos/administração & dosagem , Glicosídeos/farmacocinética , Hidrólise , Absorção Intestinal , Isoflavonas/administração & dosagem , Isoflavonas/farmacocinética , Masculino , Distribuição Aleatória , Ratos , Ratos Sprague-Dawley
11.
J Toxicol Pathol ; 24(4): 223-8, 2011 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-22319234

RESUMO

The aim of the present study was to evaluate the protective activity of aqueous extract from Platycodon grandiflorum (BC703) on thioacetamide (TA)-induced hepatotoxicity in mice. We found that BC703 significantly decreased mortality and the change in serum transaminase following TA administration. The group treated with BC703 at doses of 1, 5, and 10 mg/kg produced significant hepatoprotective effects against TA-induced liver damage by decreasing the activities of serum enzymes, nitric oxide and lipid peroxidation in dose-dependent manners. Histopathological studies further substantiated the protective effect of BC703. These results show the hepatoprotective activity of aqueous extract from Platycodon grandiflorum on thioacetamide-induced fulminant hepatic failure.

12.
J Vet Med Sci ; 72(8): 1085-7, 2010 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-20332592

RESUMO

Toltrazuril (TZR) is a triazine-based antiprotozoal agent. Following a single oral administration of TZR at 10 and 20 mg/kg to male pigs, the mean TZR concentration in plasma peaked at 4.24 and 8.18 microg/ml at 15.0 and 12.0 hr post-dose, respectively. TZR absorbed was rapidly converted to the short-lived intermediary metabolite toltrazuril sulfoxide (TZR-SO), and then metabolized to the reactive toltrazuril sulfone (TZR-SO2). TZR-SO2 was actually more slowly eliminated, with average half-lives of 231 and 245 hr, compared with TZR (48.7 and 68.9 hr) or TZR-SO (51.9 and 53.2 hr) in the 10 and 20 mg/kg groups, respectively. This study demonstrates that TZR metabolizes to TZR-SO2 having a long-terminal half-life, enabling the persistent clinical efficacy in the treatment of I. suis infection. In contrast, special consideration should be given to the residual of TZR-SO2.


Assuntos
Coccidiostáticos/farmacocinética , Triazinas/farmacocinética , Administração Oral , Animais , Coccidiostáticos/administração & dosagem , Coccidiostáticos/sangue , Absorção Intestinal , Cinética , Masculino , Sulfonas/farmacocinética , Sulfóxidos/sangue , Sulfóxidos/farmacocinética , Suínos , Triazinas/administração & dosagem , Triazinas/sangue
13.
Vet Parasitol ; 169(1-2): 51-6, 2010 Apr 19.
Artigo em Inglês | MEDLINE | ID: mdl-20083354

RESUMO

The objective of this study was to evaluate the pharmacokinetic profiles of toltrazuril (TZR), and its major metabolites toltrazuril sulfoxide (TZR x SO) and toltrazuril sulfone (TZR x SO(2)) in rabbits after oral administrations. Rabbits were dosed once with 10 and 20mg/kg TZR via stomach tube with manual restraint. The plasma concentrations of TZR, TZR x SO and TZR x SO(2) were determined by liquid chromatography/mass spectrometry. Plasma concentration-time data after single oral administration were analyzed by a non-compartmental analysis. Plasma peak concentrations of TZR, TZR x SO and TZR x SO(2) were 30.2+/-1.5microg/mL at 20.0+/-6.9h, 8.9+/-1.3microg/mL at 20.0+/-6.9h and 14.7+/-3.9microg/mL at 96.0+/-0.0h after oral administration of TZR with 10mg/kg bw, respectively. The terminal elimination half-lives for TZR, TZR x SO and TZR x SO(2) after oral dose of 10mg/kg were 52.7+/-3.6, 56.1+/-10.7 and 76.7+/-7.5h, respectively. Plasma peak concentrations of TZR, TZR x SO and TZR x SO(2) were 39.4+/-1.2microg/mL at 28.0+/-6.9h, 12.5+/-3.9microg/mL at 20.0+/-6.9h and 24.9+/-8.74microg/mL at 112.0+/-6.9h after oral administration of TZR with 20mg/kg bw, respectively. The terminal elimination half-lives for TZR, TZR x SO and TZR x SO(2) after oral dose of 20mg/kg were 56.7+/-1.9, 68.8+/-12.5 and 82.3+/-12.6h, respectively. In conclusion, TZR was very well-absorbed through the gastrointestinal tract and rapidly metabolized to TZR x SO and TZR x SO(2) in rabbits after oral administration. TZR x SO(2) was actually more slowly eliminated than TZR and TZR x SO.


Assuntos
Coccidiostáticos/farmacocinética , Triazinas/farmacocinética , Administração Oral , Animais , Área Sob a Curva , Coccidiostáticos/administração & dosagem , Coccidiostáticos/sangue , Coccidiostáticos/metabolismo , Meia-Vida , Masculino , Coelhos , Distribuição Aleatória , Triazinas/administração & dosagem , Triazinas/sangue , Triazinas/metabolismo
14.
Biotechnol Lett ; 31(6): 789-95, 2009 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-19214388

RESUMO

Aim of work To determine whether talosin A inhibits production of pro-inflammatory cytokines and nitric oxide (NO) in lipopolysaccharide (1 mug/ml)-stimulated RAW 264.7 macrophages. Talosin A (10 and 50 mug/ml) significantly reduced LPS-induced overproduction of tumor necrosis factor-alpha, interleukin IL-1beta, -6 and NO in a dose-dependent manner (P < 0.01). Talosin A had a direct NO-scavenging activity in the cell-free system. In RT-PCR analysis, gene expressions were inhibited at a transcriptional level. Moreover, the activation of nuclear factor-kappa B (NF-kappaB) was significantly suppressed by talosin A in LPS-stimulated macrophage cells (P < 0.05). Therefore, we confirmed anti-inflammatory activity of talosin A was via suppression of pro-inflammatory cytokines, NO production and NF-kappaB activation, suggesting a therapeutic candidate for inflammatory disorders.


Assuntos
Anti-Inflamatórios/farmacologia , Glicosídeos/farmacologia , Isoflavonas/farmacologia , Macrófagos/efeitos dos fármacos , NF-kappa B/antagonistas & inibidores , Animais , Linhagem Celular , Citocinas/antagonistas & inibidores , Relação Dose-Resposta a Droga , Expressão Gênica/efeitos dos fármacos , Perfilação da Expressão Gênica , Macrófagos/imunologia , Camundongos , Óxido Nítrico/antagonistas & inibidores
15.
Res Vet Sci ; 84(1): 85-9, 2008 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-17570454

RESUMO

A study on the bioavailability and pharmacokinetics of florfenicol was conducted in six healthy dogs following a single intravenous (i.v.) or oral (p.o.) dose of 20 mg kg(-1) body weight (b.w.). Florfenicol concentrations in serum were determined by a high-performance liquid chromatography/mass spectrometry. Plasma concentration-time data after p.o. or i.v. administration were analyzed by a non-compartmental analysis. Following i.v. injection, the total body clearance was 1.03 (0.49) L kg(-1)h(-1) and the volume of distribution at steady-state was 1.45 (0.82) L kg(-1). Florfenicol was rapidly distributed and eliminated following i.v. injection with 1.11 (0.94)h of the elimination half-life. After oral administration, the calculated mean C(max) values (6.18 microg ml(-1)) were reached at 0.94 h in dogs. The elimination half-life of florfenicol was 1.24 (0.64) h and the absolute bioavailability (F) was achieved 95.43 (11.60)% after oral administration of florfenicol. Florfenicol amine, the major metabolite of florfenicol, was detected in all dogs after i.v. and p.o. administrations.


Assuntos
Antibacterianos/farmacocinética , Cães/metabolismo , Tianfenicol/análogos & derivados , Administração Oral , Animais , Antibacterianos/administração & dosagem , Antibacterianos/química , Área Sob a Curva , Disponibilidade Biológica , Estudos Cross-Over , Meia-Vida , Injeções Intravenosas , Masculino , Estrutura Molecular , Tianfenicol/administração & dosagem , Tianfenicol/química , Tianfenicol/farmacocinética
16.
Eur J Pharmacol ; 556(1-3): 166-71, 2007 Feb 05.
Artigo em Inglês | MEDLINE | ID: mdl-17126323

RESUMO

To evaluate the anti-endotoxin activity of surfactin C, we studied its lipopolysaccharide-binding activity in vitro and therapeutic efficacy in experimental models of gram-negative septic shock. The ability of surfactin C to bind LPS from Escherichia coli O111:B4 was determined using a limulus chromogenic assay. Male ICR mice and Sprague-Dawley rats were given intraperitoneal administration of 1x10(9) colony forming units of E. coli ATCC 25922. After bacterial challenge, all animals were randomized to receive intraperitoneally saline, polymyxin B or surfactin C. Surfactin C not only completely bound to the LPS (its median effective concentration being 13.75 microM) but also improved the survival and reduced of the number of inoculated bacteria in the mouse model of septic shock. Surfactin C reduced the plasma endotoxin, tumor necrosis factor-alpha and nitric oxide levels in response to septic shock in rats.


Assuntos
Lipopolissacarídeos/metabolismo , Peptídeos Cíclicos/uso terapêutico , Choque Séptico/prevenção & controle , Animais , Endotoxinas/sangue , Escherichia coli , Lipopeptídeos , Masculino , Camundongos , Camundongos Endogâmicos ICR , Óxido Nítrico/sangue , Peptídeos Cíclicos/metabolismo , Polimixina B/uso terapêutico , Ratos , Ratos Sprague-Dawley , Choque Séptico/microbiologia , Fator de Necrose Tumoral alfa/sangue
17.
Korean J Gastroenterol ; 48(4): 286-9, 2006 Oct.
Artigo em Coreano | MEDLINE | ID: mdl-17060724

RESUMO

Internal hernia is defined as the herniation of viscera through an anatomic or pathologic opening within the boundaries of peritoneal cavity. Transmesocolic hernia, a subtype of internal hernia, has a herniated sac through the transverse mesocolon. Transmesocolic hernia has been rarely described in the literature, and most of reported cases were associated with a history of operation or congenital anormaly. A 72-year-old female with chronic intermittent abdominal pain and bloating was admitted. Small bowel series showed multiple jejunal loops confined to the left upper quadrant of abdomen. Abdomen spiral computed tomography (CT) showed a cluster of mildly dilated small bowel loops with mesenteries on the same area. On the three-dimensional reconstruction CT scan, a herniated sac through the transverse mesocolon was identified. She was diagnosed as transmesocolic hernia by using the three-dimensional reconstruction CT and small bowel series, without surgical exploration. The symptoms were managed with conservative measures.


Assuntos
Hérnia Abdominal/diagnóstico , Mesocolo , Idoso , Colo Transverso , Feminino , Hérnia Abdominal/diagnóstico por imagem , Humanos , Imageamento Tridimensional , Tomografia Computadorizada Espiral
18.
Korean J Gastroenterol ; 47(5): 389-93, 2006 May.
Artigo em Coreano | MEDLINE | ID: mdl-16714882

RESUMO

Hepatoid carcinoma is a primary extrahepatic neoplasm exhibiting features of hepatocellular carcinoma (HCC) in terms of morphology, immunohistochemistry, and behavior. In many cases, tumor cytoplasm is positive for alpha- fetoprotein (alpha-FP) with elevated serum alpha-FP level. Because not all hepatoid carcinomas are associated with alpha- FP overproduction, diagnosis should be made essentially by histological features of the tumor. We present a case of hepatoid carcinoma of the pancreas in a 21-year-old male patient. Abdominal computed tomography and magnetic resonance imaging revealed an inhomogeneously enhanced pancreatic head mass. Serum alpha-FP level was markedly elevated. He underwent pylorus-preserving Whipple's operation. The tumor showed hepatoid and neuroendocrine components simultaneously. The histopathological diagnosis was hepatoid carcinoma associated with neuroendocrine tumor of the pancreas. Seven months after the surgery, the patient is healthy without evidence of recurrence. To date, only 7 cases of hepatoid carcinoma of the pancreas have been reported in the literature, and this is the first case report in Korea.


Assuntos
Neoplasias Pancreáticas/diagnóstico , Adulto , Carcinoma Hepatocelular/patologia , Humanos , Masculino , Neoplasias Pancreáticas/patologia
19.
J Vet Sci ; 6(4): 353-5, 2005 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-16294001

RESUMO

Platelet aggregation was inhibited and the density of platelet-rich plasma (PRP) clots was decreased by the preincubation of PRP with surfactins, an acidic lipopeptide of Bacillus subtilis complex BC1212 isolated from soybean paste, in dose-dependent manner. Our findings suggest that surfactins are able to prevent a platelet aggregation leading to an inhibition of additional fibrin clot formation, and to enhance fibrinolysis with facilitated diffusion of fibrinolytic agents.


Assuntos
Fibrinolíticos/farmacologia , Peptídeos Cíclicos/farmacologia , Bacillus subtilis/metabolismo , Plaquetas/efeitos dos fármacos , Humanos , Lipopeptídeos , Peptídeos Cíclicos/isolamento & purificação , Inibidores da Agregação de Plaquetas/farmacologia
20.
Korean J Gastroenterol ; 45(4): 301-5, 2005 Apr.
Artigo em Coreano | MEDLINE | ID: mdl-15843756

RESUMO

Thromboembolic disease is a significant cause of morbidity and mortality in patients with inflammatory bowel disease. The reported incidence is 1-6%. The most common thromboembolic complications are deep venous thrombosis of legs and pulmonary thromboembolism. Cerebral thrombosis, portal vein thrombosis, retinal venous thrombosis and arterial thrombosis were also reported. We experienced a case of ulcerative colitis complicated with pulmonary thromboembolism. The patient was a 70-year-old woman who was diagnosed as ulcerative colitis on colonoscopy. We used prednisolone and sulfasalazine for the treatment of ulcerative colitis. Twenty five days later, she complained of abrupt dyspnea and chest pain. Chest CT and ventilation-perfusion scan revealed a thromboembolism in both lung. After the treatment of heparin & warfarin therapy, follow-up chest CT showed much regressed pulmonary thromboembolism. We report a 70-year-old woman with ulcerative colitis complicated with pulmonary thromboembolism and treated with heparin & warfarin therapy successfully.


Assuntos
Colite Ulcerativa/complicações , Embolia Pulmonar/complicações , Idoso , Feminino , Humanos
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