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1.
Chin J Traumatol ; 22(1): 1-11, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30850324

RESUMO

Vacuum sealing drainage (VSD) is frequently used in abdominal surgeries. However, relevant guidelines are rare. Chinese Trauma Surgeon Association organized a committee composed of 28 experts across China in July 2017, aiming to provide an evidence-based recommendation for the application of VSD in abdominal surgeries. Eleven questions regarding the use of VSD in abdominal surgeries were addressed: (1) which type of materials should be respectively chosen for the intraperitoneal cavity, retroperitoneal cavity and superficial incisions? (2) Can VSD be preventively used for a high-risk abdominal incision with primary suture? (3) Can VSD be used in severely contaminated/infected abdominal surgical sites? (4) Can VSD be used for temporary abdominal cavity closure under some special conditions such as severe abdominal trauma, infection, liver transplantation and intra-abdominal volume increment in abdominal compartment syndrome? (5) Can VSD be used in abdominal organ inflammation, injury, or postoperative drainage? (6) Can VSD be used in the treatment of intestinal fistula and pancreatic fistula? (7) Can VSD be used in the treatment of intra-abdominal and extra-peritoneal abscess? (8) Can VSD be used in the treatment of abdominal wall wounds, wound cavity, and defects? (9) Does VSD increase the risk of bleeding? (10) Does VSD increase the risk of intestinal wall injury? (11) Does VSD increase the risk of peritoneal adhesion? Focusing on these questions, evidence-based recommendations were given accordingly. VSD was strongly recommended regarding the questions 2-4. Weak recommendations were made regarding questions 1 and 5-11. Proper use of VSD in abdominal surgeries can lower the risk of infection in abdominal incisions with primary suture, treat severely contaminated/infected surgical sites and facilitate temporary abdominal cavity closure.


Assuntos
Abdome/cirurgia , Drenagem/métodos , Medicina Baseada em Evidências , Guias de Prática Clínica como Assunto , Sociedades Médicas/organização & administração , Infecção da Ferida Cirúrgica/prevenção & controle , Traumatologia/organização & administração , Vácuo , China , Humanos
2.
Int J Mol Med ; 41(3): 1447-1454, 2018 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29328398

RESUMO

Colorectal cancer (CRC) is a common and life­threatening type of malignant cancer, which is associated with a high mortality rate. Cisplatin (CDDP) is a commonly used chemotherapy drug with significant side effects. Brusatol (BR) is one of the principal chemical compounds isolated from the Chinese herb Bruceae Fructus, which has been reported to markedly inhibit the proliferation of numerous cancer cell lines. The present study aimed to investigate the possible synergistic anticancer effects of CDDP combined with BR on CT­26 cells, and to evaluate the underlying mechanisms of action. The growth inhibitory effects of BR, CDDP, and BR and CDDP cotreatment on CT­26 cells were assessed by MTT assay. Cell apoptosis were determined by flow cytometry and western blot analysis. The results indicated that compared with single­agent treatment, cotreatment of CT­26 cells with CDDP and BR synergistically inhibited cell proliferation and increased cellular apoptosis. Furthermore, treatment of CT­26 cells with CDDP and BR resulted in a marked increase in the release of cytosolic cytochrome c, decreased expression of procaspase­3 and procaspase­9, and upregulation of the B­cell lymphoma 2 (Bcl­2)­associated X protein/Bcl­2 ratio compared with treatment with BR or CDDP alone. These results strongly suggested that the combination of CDDP and BR was able to produce a synergistic antitumor effect in CRC cells, thus providing a solid foundation for further development of this combination regimen into an effective therapeutic method for CRC.


Assuntos
Protocolos de Quimioterapia Combinada Antineoplásica/farmacologia , Cisplatino/farmacologia , Neoplasias Colorretais/patologia , Quassinas/farmacologia , Animais , Apoptose/efeitos dos fármacos , Apoptose/genética , Caspases/metabolismo , Linhagem Celular Tumoral , Forma Celular/efeitos dos fármacos , Neoplasias Colorretais/genética , Citocromos c/metabolismo , Sinergismo Farmacológico , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Concentração Inibidora 50 , Camundongos , Quassinas/química , Proteína X Associada a bcl-2/metabolismo
3.
Oncotarget ; 8(33): 55176-55186, 2017 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-28903411

RESUMO

OBJECTIVE: To assess the efficacy and safety of RDNI in the treatment of seasonal influenza. RESULTS: 1575 participants were screened and 229 completed the study and had a RT-PCR laboratory confirmation of influenza virus infection. Fever alleviation time was 2 and 6 hours, and fever clearance time was 27 and 47 in RDNI and oseltamivir, with significant difference between two groups. Total scores of influenza symptoms descended more in RDNI than oseltamivir on day 2 and day 3. Single symptom such as fever, aversion to cold, sore throat and nasal obstruction score descended more in RDNI than oseltamivir on different days. 20 subjects used aspirin during the trial, and there was no significant difference between two groups. MATERIALS AND METHODS: We conducted a randomized, double-blind, double-dummy, oseltamivir controlled clinical trial. Patients with a positive influenza rapid test diagnosis were enrolled and randomized to receive RDNI or oseltamivir. Primary outcome was the median fever alleviation and clearance time. Secondary outcomes were total 8 influenza symptom scores, the single influenza symptom score, and the frequency of aspirin usage. CONCLUSIONS: The effect of RDNI was not worse than oseltamivir on the alleviation of influenza symptoms. RDNI was well tolerated, with no serious adverse events noted during the study period.

4.
Int Immunopharmacol ; 46: 146-155, 2017 May.
Artigo em Inglês | MEDLINE | ID: mdl-28284148

RESUMO

Usnic acid (UA) can be found in certain lichen species. Growing evidence suggests that UA possesses antitumoral, antioxidative and anti-inflammatory activities. Bleomycin (BLM) is widely used in the treatment of malignant ascites, however, it unexpectedly causes pulmonary fibrosis (PF). Researches show that excessive inflammatory response and oxidative stress in lung tissue is conspicuous causes of BLM-induced PF. Here we investigated mechanism underlying the effect-enhancing and toxicity-reducing activity of UA on H22-bearing mice treated with BLM. UA combined with BLM was significantly more effective than BLM alone in inhibiting the tumor growth, arresting the cell cycle at G0/G1 phase, and promoting the cleaved caspase-3 and cleaved caspase-8 activities to induce cancer cellular apoptosis. The mechanism may be associated with the transcriptional regulation of p53/p21/Cyclin pathway. Furthermore, UA effectively moderated the histopathological changes, reduced the content of MDA, HYP, TNF-α, IL-1ß, IL-6 and TGF-ß1, and increased the level of SOD when combined with BLM in lung tissues of H22-bearing mice, which was believed to be related to the inhibition on the protein level of p-Smad2/3 and enhancement of Smad7 expression. These findings suggested that UA might be a potential effect-enhancing and toxicity-reducing candidate for BLM in the treatment of malignant ascites.


Assuntos
Antineoplásicos/uso terapêutico , Ascite/tratamento farmacológico , Benzofuranos/uso terapêutico , Carcinoma Hepatocelular/tratamento farmacológico , Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos/prevenção & controle , Neoplasias Hepáticas/tratamento farmacológico , Fibrose Pulmonar/prevenção & controle , Adjuvantes Farmacêuticos , Animais , Apoptose/efeitos dos fármacos , Ascite/complicações , Bleomicina/efeitos adversos , Bleomicina/uso terapêutico , Carcinoma Hepatocelular/complicações , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Humanos , Líquens/imunologia , Neoplasias Hepáticas/complicações , Masculino , Camundongos , Camundongos Endogâmicos , Neoplasias Experimentais , Fibrose Pulmonar/etiologia , Proteínas Smad/metabolismo
5.
Surg Endosc ; 31(7): 3004-3013, 2017 07.
Artigo em Inglês | MEDLINE | ID: mdl-28205028

RESUMO

BACKGROUND AND STUDY AIM: The commonly used minimally invasive methods for patients with infected pancreatic necrosis (IPN) are initial endoscopic transluminal drainage (ETD) and percutaneous catheter drainage (PCD), which are followed, if necessary, by endoscopic or surgical necrosectomy. This study intends to explore which of the two minimally invasive treatments leads to a better prognosis. PATIENTS AND METHODS: Patients with IPN and an indication for intervention were prospectively enrolled and underwent either initial ETD or PCD followed, if necessary, by endoscopic or surgical necrosectomy. RESULTS: Initial treatment success occurred in 8 of 11 patients after ETD (72.7%) and in 3 of 13 patients after PCD (30.8%) (risk ratio [RR] with ETD, 2.36; 95% CI 0.97-5.77; P = 0.04). After 1 year of follow-up, 72.7% of patients survived with ETD, and 69.2% survived with PCD (RR 1.05; 95% CI 0.63-1.75; P = 0.85). Intestinal fistula seems to have occurred less in the patients who received initial ETD rather than PCD therapy (9.1 vs. 38.5%; RR 0.24; 95% CI 0.03-1.73; P = 0.098). Fewer patients who underwent an initial ETD were transferred to surgery (9.1 vs. 46.2%; RR 0.20; 95% CI 0.03-1.40; P = 0.047). A higher rate of new-onset diabetes (3 cases) or impaired glucose tolerance (1 case) occurred in initial PCD compared to ETD (40 vs. 0%, P = 0.042). CONCLUSION: The outcomes of initial endoscopic transluminal drainage are superior to percutaneous drainage for patients with infected pancreatic necrosis (ChiCTR-ONRC-13003653).


Assuntos
Drenagem/métodos , Endoscopia do Sistema Digestório/métodos , Pancreatite Necrosante Aguda/cirurgia , Adolescente , Adulto , Idoso , China , Estudos de Coortes , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Procedimentos Cirúrgicos Minimamente Invasivos/métodos , Estudos Prospectivos , Resultado do Tratamento , Adulto Jovem
6.
Food Chem ; 218: 116-121, 2017 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-27719886

RESUMO

The aim of this study was to synthesize and characterize the octenyl succinic-ß-cyclodextrin (OS-ß-CD) and assess its application as a potential emulsion stabilizer. OS-ß-CD was prepared by esterifying ß-CD with OSA under alkaline conditions. The properties of OS-ß-CD were characterized by Fourier transform infrared, 13C and 1H NMR spectroscopy, X-ray diffraction (XRD), which demonstrated that OS groups had been introduced into the ß-CD molecules and most of OS substitution occurred at the C-6 hydroxyl group of glycosyl units. The properties of emulsions stabilized by ß-CD and OS-ß-CD were evaluated via surface and interface tensiometry, determination of the creaming index and droplet size. The results showed that emulsions stabilized by ß-CD broke just after 24h storage at 25°C. The emulsions prepared by OS-ß-CD with all degree of substitution (DS) possessed a smaller oil droplet size and improved storage stability compared with that of the emulsion generated using ß-CD.


Assuntos
Emulsões/química , Succinatos/síntese química , beta-Ciclodextrinas/síntese química , Espectroscopia de Ressonância Magnética , Amido/química , Succinatos/análise , Difração de Raios X , beta-Ciclodextrinas/análise
7.
Oncotarget ; 8(3): 5498-5507, 2017 Jan 17.
Artigo em Inglês | MEDLINE | ID: mdl-27729619

RESUMO

BACKGROUND: Specific profile of microRNAs (miRNAs, miR) expressed in psoriasis has been identified in the past few years, while the studies on roles and molecular mechanisms of these miRNAs are still on the way. In our previous study, four specific miRNAs (miR-31, miR-203, hsa-miR-99a and miR-125b) were found to be specifically altered in psoriatic lesions.We therefore conducted a systematic literature review in this study to reveal the role of these miRNAs in the pathogenesis of psoriasis in order to inform future research. METHODS: The related articles indexed in PubMed (MEDLINE) database were searched and analyzed. We identified eligible studies related to the mechanism research of miR-31, miR-203, hsa-miR-99a and miR-125b in psoriasis or psoriatic lesional skin from inception up to July 2016. The experts in the field of miRNAs and Psoriasis were involved in analysis process. RESULTS: Both miR-31 and miR-203 are dramatically upregulated in psoriatic lesions. The former plays the pro-proliferative, pro-differentiative and pro-inflammatory roles and the latter holds the potentials for anti-proliferation, pro-inflammation and pro-differentiation in psoriatic keratinocytes. Conversely, both hsa-miR-99a and miR-125b are significantly downregulated in psoriatic skin. These two miRNAs are able to inhibit proliferation while promote differentiation of psoriatic keratinocytes, and miR-125b can also suppress inflammation in psoriatic lesions. By analyzing the contexts related to these miRNAs, we found that each of them does not act alone but rather work in concert with other miRNAs. The imbalance between miR-31/miR-203and hsa-miR-99a/miR-125b may contribute to the intense proliferation and abnormal differentiation of psoriatic keratinocytes, which is a characteristic of pathogenesis of psoriasis. CONCLUSION: An imbalanced miRNAs axis was for the first time outlined. Apparently, upregulation of miR-31/miR-203 and downregulation of hsa-miR-99a/miR-125b work together in concert to facilitate the development of psoriasis pathogenesis. Further work in this field holds the potentials to open a new way to study psoriasis.


Assuntos
MicroRNAs/genética , Psoríase/genética , Humanos
8.
Springerplus ; 5(1): 1101, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27468402

RESUMO

BACKGROUND: Spontaneous rupture is one of the most fatal complications of HCC. The incidence of HCC still remains a significant health problem in Eastern Asia. Many studies have shown that the in-hospital or 30-day mortality rates are as high as 25-100 %. It is often difficult to stratify these patients based on clinical manifestations and biochemical data, for deciding on an appropriate treatment strategy, especially when the patient's hemodynamic status is unstable. This study aimed to explore the clinical outcomes of treatment of spontaneously ruptured hepatocellular carcinoma with hemorrhagic shock. METHODS: One hundred and sixty two patients with hemorrhagic shock secondary to spontaneous rupture of hepatocellular carcinoma were included in this retrospective study. The therapeutic methods included conservative treatment, transcatheter arterial embolization (TAE) and hepatectomy. The outcomes in terms of 30 day and 1 year survival were analyzed. RESULTS: Thirty five (21.6 %) received only conservative management, TAE was performed in 48 (29.6 %) and partial hepatectomy (emergency and staged) in 106 (65.4 %) patients. The 30-day survival rate was lower in patients receiving conservative treatment (8.6 %) than in those receiving either hepatectomy or TAE (88.2 %; P < 0.001). Conservative treatment was associated with poorer long-term survival (0 % at 1 year) when compared to those receiving either hepatectomy or TAE (54.3 % at 1 year; P < 0.001). The survival rates at 30 days and 1 year were 92.5 % and 59.4 % for the patients who underwent hepatectomy, which were significantly higher (66.7 and 28.6 % respectively) than those receiving TAE alone (P = 0.003 and P = 0.009, respectively). Multivariate Cox-regression analysis showed that hepatectomy and TAE were significant protective factors for survival as compared with conservative treatment (all P < 0.01). CONCLUSIONS: Partial hepatectomy, tended to provide better survival than transcatheter arterial embolization alone or conservative treatment in the management of patients with hemorrhagic shock secondary to spontaneous rupture of hepatocellular carcinoma.

9.
Huan Jing Ke Xue ; 37(3): 834-46, 2016 Mar 15.
Artigo em Chinês | MEDLINE | ID: mdl-27337873

RESUMO

Indoor dust was an important and even a major route of human exposure to polybrominated diphenyl ethers (PBDEs). However, the vacuum dust concentrations were less correlated with indoor residents' serum concentrations of PBDEs, thus inadequat for either estimation of human exposure dose or research of deposition flux and its seasonal variations. Passive sampling of indoo dustfall could offset these shortages. A total of 49 indoor sampling sites including homes, offices, computer rooms and furniture factor were selected in Xiamen, China to collect the four season dustfall samples with glass plates (walled by clean aluminum foil). Deposition flux, concentrations, congener profiles, seasonal variations, and human exposure to PBDEs in the dustfall were studied The geometric means of the yearly round deposition flux of ∑ PBDEs (sum of 16 BDE congeners including BDE-209) in homes offices, computer rooms and furniture factory were 6.1, 3.0, 1.1 and 179.8 ng · (m² · d)⁻¹, respectively. The geometric mea deposition flux of ∑ PBDEs in homes was 2 times of that in offices, but the concentration of ∑ PBDEs in the dustfall from home (445.5 ng · g⁻¹) was only slightly higher than that of offices (384.0 ng · g⁻¹). The ∑ PBDEs deposition flux in homes, offices and computer rooms in Xiamen were at lower level compared with other cities around the world. The PBDEs deposition flux in furnitur factory was much higher than that in the ordinary indoor environment. Autumn was the season with highest deposition flux of ∑ PBDEs. Geometric means of BDE- 209's proportion of the ∑ PBDEs in dustfall in all seasons in the four types of indoo environment were above 80% . The deposition flux of PBDEs was correlated to the dustfall deposition flux in homes, offices and computer rooms, but not that in furniture factory. ∑15 PBDEs in homes and offices were significantly correlated with the age of computers, but not quantities of electrical and electronic products, furniture and interior decoration, etc. Indoor dust was a key route for human exposure to ∑ PBDEs, especially for higher brominated BDEs.


Assuntos
Poluição do Ar em Ambientes Fechados/análise , Éteres Difenil Halogenados/análise , Estações do Ano , China , Poeira/análise , Exposição Ambiental , Habitação , Humanos , Local de Trabalho
10.
J Ethnopharmacol ; 183: 59-70, 2016 May 13.
Artigo em Inglês | MEDLINE | ID: mdl-26732632

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Radix Astragali (RA), Radix Angelicae Sinensis (RAS) and Folium Epimedii (FE) are three of the extensively applied herbs among traditional Chinese medicines for gynecological disorders and osteoporosis. A derivative herbal formula-RRF, consisting of the three medicines with a weight ratio of 5:1:5, is derived from a famous Chinese herbal formula-Danggui Buxue Tang (DBT). RRF has shown noteworthy perimenopause ameliorating effect in both ovariectomized rats and natural aging female rats, which might represent a promising candidate for the treatment of perimenopausal disorders. The aim of this study was to evaluate its immunological potential, chronic toxicity and reproductive effects by 26-week repeated daily administration in female rats, in order to optimize its safe use. MATERIALS AND METHODS: The effect of RRF on immunological function was studied by macrophage phagocytosis, immune organ index, serum immunoglobulin level as well as delayed type hypersensitivity (DTH) in mice. For toxicity assessment, acute toxicity study was performed according to fixed dose procedure with a single oral administration of RRF to mice. In the oral chronic toxicity, 120 female rats were administrated RRF orally in 0, 1100, 4400, or 8800mg/kg/day doses for 26 weeks. Clinical signs, mortality, body weights, feed consumption, haemato-biochemical parameters, organ weights, histopathology and reproductive hormone profiles were examined at the end of the 13- and 26-week dosing period, as well as after the 4-week recovery period. RESULTS: Oral administration of RRF at three doses (282, 564 and 1128mg/kg) significantly increased the indices of phagocytosis K, as compared with prednisone acetate (PR) group (p<0.05 or 0.01). Exposure of RRF dose-dependently boosted circulating serum IgM level (all p<0.01) in response to CRBC in PR-induced mice. Furthermore, RRF treatment elicited a significant increment (all p<0.01) in DNFB-induced DTH response and the immune organ indices in a dose-dependent manner in mice, in parellel to DNFB-induced group. In the single dose acute toxicity and repeated dose 90-day chronic toxicity investigations, no toxic signs/mortality were observed. RRF treatment did not cause any toxicologically significant changes in clinical signs, food consumption, body weight, relative organ weight, hematological parameters, clinical chemistry, gross pathology and histopathology between treatment and control groups. No treatment related gross/histopathological lesions were observed and no target organ was identified. Long-term repeated administration of RRF exerted a significant promotion on serum level of steroid hormone estradiol, progesterone and testosterone release, along with decrease of circulating pituitary follicle stimulating hormone, luteinizing hormone, and prolactin levels in female rats. The No Observed Adverse Effect Level (NOAEL) of RRF was determined to be over 8800mg/kg/day for elderly female rats, a dose that was equivalent to 50 times of human dose. CONCLUSION: The present investigation demonstrated that RRF possessed appreciable immunopotentiating activity and had a relatively wide margin of safety. Long-term treatment of RRF exhibited estrogenic properties, and retarded certain age-associated degenerations. RRF might have the potential for further development as a safe and effective alternative/complementary to conventional medication in relieving perimenopausal symptoms.


Assuntos
Medicamentos de Ervas Chinesas/efeitos adversos , Medicamentos de Ervas Chinesas/farmacologia , Hormônios/metabolismo , Administração Oral , Animais , Astrágalo (Planta)/efeitos adversos , Astrágalo (Planta)/química , Feminino , Medicina Tradicional Chinesa/efeitos adversos , Camundongos , Nível de Efeito Adverso não Observado , Perimenopausa/efeitos dos fármacos , Ratos , Ratos Sprague-Dawley
11.
Exp Biol Med (Maywood) ; 241(2): 193-204, 2016 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-26290140

RESUMO

Pogostemonis Herba, known as "Guang-Huo-Xiang" in Chinese, has been widely used in the treatment of gastrointestinal dysfunction. Pogostone is one of the major constituents of Pogostemonis Herba. The aim was to scientifically evaluate the possible gastroprotective effect and the underlying mechanisms of pogostone against indomethacin-induced gastric ulcer in rats. Rats were orally treated with vehicle, lansoprazole (30 mg/kg) or pogostone (10, 20 and 40 mg/kg) and subsequently exposed to acute gastric lesions induced by indomethacin. Gross evaluation, histological observation, gastric mucosal superoxide dismutase activity, glutathione content, catalase activity, malonaldehyde level and prostaglandin E2 production were performed. Immunohistochemistry and reverse transcription polymerase chain reaction for cyclooxygenase-1 and cyclooxygenase-2, as well as terminal deoxynucleotidyltransferase-mediated dUTP nick-end labeling assay, immunohistochemistry for heat-shock protein 70, B-cell lymphoma-2 and Bax were conducted. Results indicated that rats pretreated with pogostone showed remarkable protection from the gastric mucosa damage compared to vehicle-treated rats based on the ulcer index and inhibition percentage. Histologically, oral administration of pogostone resulted in observable improvement of gastric injury, characterized by reduction of necrotic lesion, flattening of gastric mucosa and alleviation of submucosal edema with hemorrhage. Pogostone pretreatment significantly raised the depressed activities of superoxide dismutase, glutathione and catalase, while reduced the elevated malonaldehyde level compared with indomethacin-induced group. Pogostone-pretreated group induced a significant increase in gastric mucosal prostaglandin E2 level and obvious up-regulation of protein levels and mRNA expressions of cyclooxygenase-1 and cyclooxygenase-2. Furthermore, antiapoptotic effect of pogostone was verified by terminal deoxynucleotidyltransferase-mediated dUTP nick-end labeling assay, and the apoptotic process triggered by pogostone involved the up-expression of heat-shock protein70 and B-cell lymphoma-2 protein, and suppression of Bax protein expressions in the ulcerated tissues. It is speculated that the gastroprotective effect of pogostone against indomethacin-induced gastric ulceration might be associated with its stimulation of cyclooxygenase-mediated prostaglandin E2, antioxidant and antiapoptotic effect.


Assuntos
Fármacos Gastrointestinais/administração & dosagem , Indometacina/toxicidade , Óleos Voláteis/administração & dosagem , Úlcera Gástrica/tratamento farmacológico , Úlcera Gástrica/prevenção & controle , Administração Oral , Animais , Modelos Animais de Doenças , Mucosa Gástrica/patologia , Fármacos Gastrointestinais/isolamento & purificação , Histocitoquímica , Humanos , Imuno-Histoquímica , Indometacina/administração & dosagem , Masculino , Microscopia , Óleos Voláteis/isolamento & purificação , Ratos Sprague-Dawley , Índice de Gravidade de Doença , Úlcera Gástrica/induzido quimicamente , Resultado do Tratamento
12.
BMC Complement Altern Med ; 15: 238, 2015 Jul 16.
Artigo em Inglês | MEDLINE | ID: mdl-26179287

RESUMO

BACKGROUND: The inhibitory effect of andrographolide sodium bisulphite (ASB) on jack bean urease (JBU) and Helicobacter pylori urease (HPU) was performed to elucidate the inhibitory potency, kinetics and mechanism of inhibition in 20 mM phosphate buffer, pH 7.0, 2 mM EDTA, 25 °C. METHODS: The ammonia formations, indicator of urease activity, were examined using modified spectrophotometric Berthelot (phenol-hypochlorite) method. The inhibitory effect of ASB was characterized with IC50 values. Lineweaver-Burk and Dixon plots for JBU inhibition of ASB was constructed from the kinetic data. SH-blocking reagents and competitive active site Ni2+ binding inhibitors were employed for mechanism study. Molecular docking technique was used to provide some information on binding conformations as well as confirm the inhibition mode. RESULTS: The IC50 of ASB against JBU and HPU was 3.28±0.13 mM and 3.17±0.34 mM, respectively. The inhibition proved to be competitive and concentration- dependent in a slow-binding progress. The rapid formation of initial ASB-JBU complex with an inhibition constant of Ki=2.86×10(-3) mM was followed by a slow isomerization into the final complex with an overall inhibition constant of Ki*=1.33×10(-4) mM. The protective experiment proved that the urease active site is involved in the binding of ASB. Thiol reagents (L-cysteine and dithiothreithol) strongly protect the enzyme from the loss of enzymatic activity, while boric acid and fluoride show weaker protection, indicating that the active-site sulfhydryl group of JBU was potentially involved in the blocking process. Moreover, inhibition of ASB proved to be reversible since ASB-inactivated JBU could be reactivated by dithiothreitol application. Molecular docking assay suggested that ASB made contacts with the important sulfhydryl group Cys-592 residue and restricted the mobility of the active-site flap. CONCLUSIONS: ASB was a competitive inhibitor targeting thiol groups of urease in a slow-binding manner both reversibly and concentration-dependently, serving as a promising urease inhibitor for the treatment of urease-related diseases.


Assuntos
Diterpenos/farmacologia , Sulfitos/farmacologia , Urease , Canavalia/enzimologia , Cinética , Simulação de Acoplamento Molecular , Urease/química , Urease/efeitos dos fármacos , Urease/metabolismo
13.
Int Immunopharmacol ; 26(2): 384-91, 2015 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-25916678

RESUMO

Andrographolide sodium bisulfite (ASB), a water-soluble sulfonate of andrographolide has been shown to possess anti-inflammatory, antipyretic and analgesic activities. However, there is no report on the gastroprotective effect of ASB against indomethacin-induced gastric ulcer. Here we investigated the possible anti-ulcerogenic potential of ASB and the underlying mechanism against indomethacin-induced gastric ulcer in rats. The ulcer area, histopathological assessment, contents of gastric mucosal glutathione (GSH), catalase (CAT), superoxide dismutase (SOD), malonaldehyde (MDA) and prostaglandin E2 (PGE2) were examined. In addition, cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2) mRNA expression and immunohistochemical evaluation of HSP70, Bcl-2 and Bax proteins were also investigated. Results indicated that ASB pre-treatment significantly reduced the ulcer areas induced by indomethacin compared with the vehicle group. The gastric levels of GSH, CAT and SOD were markedly increased by ASB while the level of MDA was decreased. In addition, ASB pretreatment significantly promoted the gastric PGE2 levels and up-regulated the COX-1 and COX-2 mRNA expression in comparison with the vehicle group. Immunohistochemistry analysis showed obvious up-regulation of HSP70 and Bcl-2 protein expression while suppression of Bax protein in the gastric tissue of ASB-pretreated group. Taken together, these findings indicated that the gastroprotective effect of ASB might be associated with the improvement of antioxidative status, activation of COX-mediated PGE2 synthesis, down-regulation of Bax proteins and up-regulation of Bcl-2 and HSP70 proteins. ASB might have the potential for further development as a promising alternative for antiulcer treatment.


Assuntos
Antioxidantes/administração & dosagem , Diterpenos/administração & dosagem , Mucosa Gástrica/efeitos dos fármacos , Úlcera Gástrica/prevenção & controle , Sulfitos/administração & dosagem , Animais , Antioxidantes/efeitos adversos , Catalase/metabolismo , Dinoprostona/metabolismo , Diterpenos/efeitos adversos , Mucosa Gástrica/patologia , Glutationa/metabolismo , Proteínas de Choque Térmico HSP70/genética , Proteínas de Choque Térmico HSP70/metabolismo , Humanos , Indometacina/administração & dosagem , Malondialdeído/metabolismo , Prostaglandina-Endoperóxido Sintases/genética , Prostaglandina-Endoperóxido Sintases/metabolismo , Proteínas Proto-Oncogênicas c-bcl-2/genética , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Ratos , Ratos Sprague-Dawley , Úlcera Gástrica/induzido quimicamente , Sulfitos/efeitos adversos , Superóxido Dismutase/metabolismo
14.
Exp Gerontol ; 61: 147-55, 2015 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-25498537

RESUMO

It has been confirmed that repeated exposure of skin to ultraviolet (UV) radiation results in cutaneous oxidative stress and inflammation, which act in concert to cause premature skin aging, well known as photoaging. 18ß-Glycyrrhetinic acid (GA), widely used to treat various tissue inflammations, is the main active component of licorice root, and has also been shown to possess favorable anti-oxidative property and modulating immunity function. In the present study, we investigated the potential protective effect of GA on UV-induced skin photoaging in a mouse model. During the experimental period of ten consecutive weeks, the dorsal depilated skin of mice was treated with topical GA for 2 hours prior to UV irradiation. The results showed that GA pretreatment significantly alleviated the macroscopic and histopathological damages in mice skin caused by UV. Meanwhile, the data also indicated that GA markedly up-regulated the activities of the antioxidant enzymes (SOD, GSH-Px), and increased the content of skin collagen, while obviously decreased malonaldehyde level and inhibited high expressions of matrix metalloproteinase-1 (MMP-1) and -3 (MMP-3), as well as down-regulated the expression of inflammatory cytokines such as IL-6, TNF-α and IL-10. Taken together, these findings amply demonstrate that GA observably attenuates UV-induced skin photoaging mainly by virtue of its antioxidative and anti-inflammatory properties, as well as regulating the abnormal expression of MMP-1 and MMP-3.


Assuntos
Ácido Glicirretínico/análogos & derivados , Protetores contra Radiação/farmacologia , Envelhecimento da Pele/efeitos dos fármacos , Animais , Elasticidade , Feminino , Glutationa Peroxidase/metabolismo , Ácido Glicirretínico/farmacologia , Malondialdeído/análise , Metaloproteinase 3 da Matriz/metabolismo , Camundongos , Pele/metabolismo , Pele/patologia , Pele/efeitos da radiação , Superóxido Dismutase/metabolismo , Raios Ultravioleta
15.
Food Chem ; 168: 302-10, 2015 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-25172714

RESUMO

Pectin-enriched material (PEM) was extracted from sugar beet pulp using subcritical water combined with ultrasonic-assisted treatment. Optimisation of the reaction parameters for maximum extraction yield of PEM was carried out using response surface methodology. Optimum modification conditions were as follows: liquid/solid ratio 44.03, extraction temperature 120.72°C, extraction time 30.49min and extraction pressure 10.70MPa. Under optimal conditions, the maximum yield of PEM was 24.63%. The composition of the PEM was determined. The data showed that the contents of galacturonic acid and arabinose were 59.12% and 21.66%, respectively. The flow behaviours were investigated by a rheometer. The effects of PEM on the pasting and thermal properties of maize starch were also conducted. The results showed that the addition of PEM increased pasting temperature and decreased other pasting parameters. Increasing PEM concentrations resulted in increased gelatinisation temperature and enthalpy.


Assuntos
Beta vulgaris/química , Pectinas/isolamento & purificação , Pectinas/química , Termodinâmica , Ultrassom , Viscosidade , Água
16.
Int J Clin Exp Med ; 7(5): 1483-9, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24995117

RESUMO

UNLABELLED: To investigate the effects of Ulinastatin (UTI) in cerebral ischemia-reperfusion (IR) injury in rats and whether this effect might be related to Aquaporin 4 (AQP4), one hundred and eighty adult male Sprague Dawley (SD) rats, weighing 230-280 g, were randomly divided into 3 groups: sham (S) group, IR group and UTI (U) group. Every group was further divided into 3 sub-groups: 6 h group, 24 h group and 48 h group. The transient focal IR injury was induced by inserting a silicone-coater monofilament nylon suture (0.28 mm) from the right external carotid artery to the origin of the left middle cerebral artery. The suture was removed after 2 h to allow reperfusion. UTI treatment group was injected with UTI 100000 u/kg at the beginning of the reperfusion period, while S group and IR group were injected with the same volume of saline. Samples were taken according to the reperfusion time (6 h, 12 h and 24 h). Infract volume was measured by triphenyl tetrazolium chloride staining, and brain water content was determined by wet-dry weight method and neurological scores were checked with a five-point scale. Expression levels of AQP4 were checked with immunohistochemistry and Western blot. RESULTS: Compared with S group, the infarct volume, water content, neurological scores and AQP4 levels in the rat brain tissues were significantly increased in IR group. Administration of UTI significantly decreased the infarct volume, water content of the brain tissue and neurological scores. Moreover, the expression levels of AQP4 were also down-regulated by UTI treatment. CONCLUSION: UTI improves cerebral IR injury in rats potentially via decreasing the expression levels of AQP4.

17.
Artigo em Inglês | MEDLINE | ID: mdl-24991227

RESUMO

This study attempted to explore the effects of white pepper and its major component piperine on puerarin administered to rats. Pharmacokinetic parameters of puerarin in rats were determined by oral administration (400 mg/kg) or intravenous injection (40 mg/kg) of puerarin, pretreated with or without white pepper and piperine given orally. Compared to the control group given oral puerarin only, the combined use of piperine (10 or 20 mg/kg) increased the C max of puerarin by 1.30-fold or 1.64-fold and the AUC0-∞ by 133% or 157%, respectively. In contrast, coadministration of white pepper (125 or 250 mg/kg) decreased oral absorption of puerarin to 83% or 74%, respectively. On the other hand, pretreatment with piperine orally did not alter the intravenous pharmacokinetics of puerarin, while the AUC of puerarin after intravenous administration was increased by pretreatment with white pepper. The results indicate that pretreatment with piperine or pepper exerts different effects on pharmacokinetics of puerarin administrated via intragastric and intravenous routes. Therefore, it is suggested that the combined application of piperine or white pepper with puerarin should be carefully monitored for potential diet-drug interactions.

18.
Artigo em Inglês | MEDLINE | ID: mdl-24223056

RESUMO

The aim of this study was to analyze the chemical composition and investigate the anti-inflammatory property of the supercritical-carbon dioxide extract from flowers and buds of C. indicum (CISCFE). The anti-inflammatory effect was evaluated in four animal models including xylene-induced mouse ear edema, acetic acid-induced mouse vascular permeability, carrageenan-induced mouse hind paw edema, and cotton pellet-induced rat granuloma formation. The results indicated that CISCFE significantly attenuated xylene-induced ear edema, decreased acetic acid-induced capillary permeability, reduced carrageenan-induced paw, and inhibited the cotton pellet-induced granuloma formation in a dose-dependent manner. Histopathologically, CISCFE abated inflammatory response of the edema paw. Preliminary mechanistic studies demonstrated that CISCFE decreased the MDA level via increasing the activities of anti-oxidant enzymes (SOD, GPx, and GRd), attenuated the productions of NF- κ B, TNF- α , IL-1 ß , IL-6, PGE2 and NO, and suppressed the activities of iNOS and COX-2. In phytochemical study, 35 compounds were identified by GC-MS, and 5 compounds (chlorogenic acid, luteolin-7-glucoside, linarin, luteolin and acacetin) were reconfirmed and quantitatively determined by HPLC-PAD. This paper firstly analyzed the chemical composition by combining GC-MS with HPLC-PAD and explored possible mechanisms for the anti-inflammatory effect of CISCFE.

19.
Neurochem Res ; 38(9): 1871-9, 2013 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-23780673

RESUMO

Ischemic stroke is the most common type of stroke and brings about a big disease burden because of high mortality and disability in China. Tetrandrine, a bisbenzylisoquinoline alkaloid isolated from the Chinese herb Radix Stephania tetrandra, has been demonstrated to possess anti-inflammatory and free radical scavenging effects and even regulate astrocyte activation, but the possible role of tetrandrine in ameliorating cerebral ischemia/reperfusion injury of ischemic stroke remains unknown. The aim of this study was to determine the effects of tetrandrine on neurological injury and differential proteomic changes induced by transient reversible middle cerebral artery occlusion (MCAO) in mice. Male Balb/c mice were divided into sham (n = 30), MCAO + saline as control (n = 30), and MCAO + Tet as tetrandrine-treated (n = 30) groups. Mice in the control and tetrandrine-treated groups underwent 120 min of MCAO following reperfusion. Immediately and 2 h after MCAO, the mice received either normal saline (sham operated and control groups) or tetrandrine (tetrandrine-treated group) intraperitoneally. Neurological defects, brain water content, and infarct volume at 24 h after stoke were used to evaluate neurological injury extent. Treatment with tetrandrine not only mitigated cerebral neurological deficits (P < 0.05) and infarct size (P < 0.01), but also decreased brian edema in the ischemic brain (P < 0.05). Then, fluorescence two-dimensional difference in gel electrophoresis was used to detect our systematic differential profiling of proteomic changes responding to tetrandrine administration. We validated that the expression of GRP78, DJ-1 and HYOU1 was associated with neuroprotective effect of tetrandrine in MCAO model by Western blotting. These findings indicate a potential neuroprotective role of tetrandrine for ischemic stroke and yield insights into cellular and molecular mechanisms of tetrandrine taking place in ischemic stroke.


Assuntos
Benzilisoquinolinas/farmacologia , Isquemia Encefálica/metabolismo , Modelos Animais de Doenças , Eletroforese em Gel Bidimensional/métodos , Infarto da Artéria Cerebral Média/metabolismo , Proteômica , Traumatismo por Reperfusão/metabolismo , Animais , Masculino , Espectrometria de Massas , Camundongos , Camundongos Endogâmicos BALB C
20.
Acta Crystallogr Sect E Struct Rep Online ; 69(Pt 3): m172, 2013 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-23476512

RESUMO

In the title compound, [Mn(C4H3N2O2)2(H2O)2], the Mn(II) ion is located on a twofold rotation axis and displays a distorted octa-hedral coordination environment, defined by two N,O-bidentate 1H-imidazole-4-carboxyl-ate ligands in the equatorial plane and two water mol-ecules in axial positions. In the crystal, O-H⋯O and N-H⋯O hydrogen bonds link the mol-ecules into a three-dimensional supra-molecular network. π-π stacking inter-actions between the imidazole rings [centroid-centroid distances = 3.5188 (15) and 3.6687 (15) Å] further stabilize the structure.

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