AIM: To evaluate the effect of thienorphine on small intestinal transit in vivo and on guinea-pig ileum (GPI) contraction in vitro . METHODS: The effects of thienorphine on intestinal transit were examined in mice and...AIM: To evaluate the effect of thienorphine on small intestinal transit in vivo and on guinea-pig ileum (GPI) contraction in vitro . METHODS: The effects of thienorphine on intestinal transit were examined in mice and in isolated GPI. Buprenorphine and morphine served as controls. The distance traveled by the head of the charchol and the total length of the intestine were measured in vivo . Gastrointestinal transit was expressed as a percentage of the distance traveled by the head of the marker relative to the total length of the small intestine. The isolated GPI preparations were connected to an isotonic force transducer and equilibrated for at least 1 h before exposure to drugs. Acetylcholine was used for muscle stimulation. RESULTS: Thienorphine (0.005-1.0 mg/kg, ig ) or bu-prenorphine (0.005-1.0 mg/kg, sc ) dose-dependently significantly inhibited gut transit compared with saline. Thienorphine inhibited gut transit less than buprenorphine. The maximum inhibition by thienorphine on the intestinal transit was 50%-60%, whereas the maximum inhibition by morphine on gut transit was about 100%. Thienorphine also exhibited less inhibition on acetylcholine-induced contraction of GPI, with a maximum inhibition of 65%, compared with 93% inhibition by buprenorphine and 100% inhibition by morphine. Thienorphine induced a concentration-dependent decrease in the basal tonus of spontaneous movement of the GPI, the effect of which was weaker than that with buprenorphine. The duration of the effect of thienorphine on the GPI was longer than that with buprenorphine. CONCLUSION: Thienorphine had less influence, but a longer duration of action on GPI contraction and moderately inhibited intestinal transit.展开更多
Objective The present in vivo study was undertaken to determine whether matrine,a kind of traditional Chinese medicinal alkaloid,would relax the isolated guinea pig aortic smooth muscles,if so,to investigate the mecha...Objective The present in vivo study was undertaken to determine whether matrine,a kind of traditional Chinese medicinal alkaloid,would relax the isolated guinea pig aortic smooth muscles,if so,to investigate the mechanism involved.Methods The concentration-dependent relaxation response to matrine was studied in phenylephrine or potassium chloride precontracted guinea pig aortic rings.Results Matrine(1×10-4 M-3.3×10-3 M)relaxed the endothelium denuded aortic rings precontracted submaximally with phenylephrine,in a concentration-dependent manner,and it's preincubation(3.3×10-3 M)produced a significant rightward shift in the phenylephrine dose-response curve,but had no effects on the potassium chloride-induced contraction.The anticontractile effect of matrine was not reduced by the highly selective ATP-dependent K+ channel blocker glibenclamide(10-5 M),the non-selective K+ channel blocker tetraethylammonium(10-3 M),as well as the β-antagonist propranolol(10-5 M).In either "normal" or "Ca2+-free" bathing medium,the phenylephrine-induced contraction was attenuated by matrine(3.3×10-3 M),indicating the vasorelaxation was due to inhibit of intracellular and extracellular Ca2+ mobilization.Conclusions The results obtained clearly demonstrated that matrine inhibits phenylephrine-induced contractions by inhibiting activation of α-adrenoceptor and interfering with both the release of intracellular Ca2+ and the influx of extracellular Ca2+.展开更多
Immunocytochemical localization of 5-hydroxytryptamine (5-HT) containing cells of the guinea-pig pancreas was studied by means of PAP-glucose oxidase-DAB-nickel (PAP-GDN) and PAPstaining methods on paraffin sections. ...Immunocytochemical localization of 5-hydroxytryptamine (5-HT) containing cells of the guinea-pig pancreas was studied by means of PAP-glucose oxidase-DAB-nickel (PAP-GDN) and PAPstaining methods on paraffin sections. In this study we demonstrated the presence of 5-HTimmunoreactive cells in the endocrine (islets) and exocrine pancreas of the guinea-ping. Cells exhib-iting 54-HT immunoreactivity were found in the center and the periphery of the pancreatic islets. The5-HT immunoreactive granules were evenly distributed throughout the cytoplasm, but was faint inthe nuclei. Cells of this type were also distributed in the exocrine pancreas. Grouped or single or single cellsoccurred intercalatedly between acinar cells, as well as in the epithlium of ducts and in the connectivetissues near the ducts or acini.展开更多
AIM: To evaluate the intestinal motility changes evoked by 8 bacterial strains belonging to Bifidobacterium , Lactobacillus and Streptococcus genera within the probiotic preparation VSL#3. METHODS: Ileum and proximal ...AIM: To evaluate the intestinal motility changes evoked by 8 bacterial strains belonging to Bifidobacterium , Lactobacillus and Streptococcus genera within the probiotic preparation VSL#3. METHODS: Ileum and proximal colon segments isolated from guinea-pigs were used as a study model. Entire cells and cell fractions (cell debris, cell wall fraction, cytoplasmatic fraction, proteinaceous and non- proteinaceous cytoplasmatic components) of VSL#3 strains and, as controls, Escherichia coli, Salmonella aboni and Bacillus licheniformis were tested in this in vitro model. RESULTS: Among the bacterial cell fractions tested, only the cytoplasmatic fraction modified intestinal motility. Lactobacillus strains stimulated the contraction of ileum segment, whereas all probiotic strains tested induced proximal colon relaxation response. The non-proteinaceous cytoplasmatic components were responsible for the colon relaxation. CONCLUSION: The results obtained in this study suggest that the proximal colon relaxation activity showed by the probiotic bacteria could be one of the possible mechanisms of action by which probiotics exert their positive effects in regulating intestinal motility.展开更多
The present study was carried out to evaluate the effect of different rates of dried cassava leafs in diet as replacement of protein sources on the weight gain and carcass yield of guinea-pigs, as well as on the physi...The present study was carried out to evaluate the effect of different rates of dried cassava leafs in diet as replacement of protein sources on the weight gain and carcass yield of guinea-pigs, as well as on the physico-chemical and technological properties of guinea-pigs’ meat. A total of forty-eight (48) eight-week-old guinea-pigs were divided in a completely randomized experimental design, in four groups and fed with the experimental foods. These experimental foods were formulated as follows: cassava-leaf (Manihot esculenta) powder was incorporated at concentrations of 0%, 8%, 10% and 12% respectively in replacement of protein sources for R0, R1, R2 and R3. Each treatment consisted of a group of 12 guinea pigs per paddock (6 males and 6 females). The initial weight (IW), final weight (FW), daily weight gain (DWG) and total gain (TG) were evaluated. At the 22nd week, animals of each group were sacrificed by bleeding, then skinned and eviscerated. Carcasses were cut, and some parts (loin, thigh and shoulder) were collected, deboned and analysed. The highest FW and carcass yield (CY) were obtained with the use of 10% cassava leafs (R2): 556 g (FW), 42.65% (CY) for males and 529.17 g (FW), 37.39% (CY) for females. The incorporation of 8% (R1) and 12% (R3) cassava leafs led to a significant increase (P < 0.05) in protein levels in the loins (22.89%) and shoulders (22.43%) of females and the thighs (21.68%) and shoulders (21.09%) of males. However, protein levels of male fed with R3 in the various parts studied were higher than females fed with the same diet. The study of the technological parameters of guinea-pig’s meat showed that the incorporation of 8% and 12% cassava leafs in the diet resulted in a significant decrease in the water holding capacity and technological yield in the different parts studied. These results show that, the incorporation of cassava leafs in guinea-pigs’ diet made it possible to obtain good growth (R2) and meat of good technological quality.展开更多
The unsatisfactory results of clinical trials with class-Ⅰ antiarrhythmic drugs have prompted a renaissance of interest in compounds with class-Ⅲ antiarrhythmic action. In the present, we have reevaluated the class-...The unsatisfactory results of clinical trials with class-Ⅰ antiarrhythmic drugs have prompted a renaissance of interest in compounds with class-Ⅲ antiarrhythmic action. In the present, we have reevaluated the class-Ⅲ antiarrhythmic ef-展开更多
基金Supported by National New Drugs Foundation of China, No.2011ZX09101-005-01"Integrated Drug Discovery Technology Plat form" of National Science and Technology Major Projects for "Major New Drugs Innovation and Development", No.2012ZX09301003-001
文摘AIM: To evaluate the effect of thienorphine on small intestinal transit in vivo and on guinea-pig ileum (GPI) contraction in vitro . METHODS: The effects of thienorphine on intestinal transit were examined in mice and in isolated GPI. Buprenorphine and morphine served as controls. The distance traveled by the head of the charchol and the total length of the intestine were measured in vivo . Gastrointestinal transit was expressed as a percentage of the distance traveled by the head of the marker relative to the total length of the small intestine. The isolated GPI preparations were connected to an isotonic force transducer and equilibrated for at least 1 h before exposure to drugs. Acetylcholine was used for muscle stimulation. RESULTS: Thienorphine (0.005-1.0 mg/kg, ig ) or bu-prenorphine (0.005-1.0 mg/kg, sc ) dose-dependently significantly inhibited gut transit compared with saline. Thienorphine inhibited gut transit less than buprenorphine. The maximum inhibition by thienorphine on the intestinal transit was 50%-60%, whereas the maximum inhibition by morphine on gut transit was about 100%. Thienorphine also exhibited less inhibition on acetylcholine-induced contraction of GPI, with a maximum inhibition of 65%, compared with 93% inhibition by buprenorphine and 100% inhibition by morphine. Thienorphine induced a concentration-dependent decrease in the basal tonus of spontaneous movement of the GPI, the effect of which was weaker than that with buprenorphine. The duration of the effect of thienorphine on the GPI was longer than that with buprenorphine. CONCLUSION: Thienorphine had less influence, but a longer duration of action on GPI contraction and moderately inhibited intestinal transit.
文摘Objective The present in vivo study was undertaken to determine whether matrine,a kind of traditional Chinese medicinal alkaloid,would relax the isolated guinea pig aortic smooth muscles,if so,to investigate the mechanism involved.Methods The concentration-dependent relaxation response to matrine was studied in phenylephrine or potassium chloride precontracted guinea pig aortic rings.Results Matrine(1×10-4 M-3.3×10-3 M)relaxed the endothelium denuded aortic rings precontracted submaximally with phenylephrine,in a concentration-dependent manner,and it's preincubation(3.3×10-3 M)produced a significant rightward shift in the phenylephrine dose-response curve,but had no effects on the potassium chloride-induced contraction.The anticontractile effect of matrine was not reduced by the highly selective ATP-dependent K+ channel blocker glibenclamide(10-5 M),the non-selective K+ channel blocker tetraethylammonium(10-3 M),as well as the β-antagonist propranolol(10-5 M).In either "normal" or "Ca2+-free" bathing medium,the phenylephrine-induced contraction was attenuated by matrine(3.3×10-3 M),indicating the vasorelaxation was due to inhibit of intracellular and extracellular Ca2+ mobilization.Conclusions The results obtained clearly demonstrated that matrine inhibits phenylephrine-induced contractions by inhibiting activation of α-adrenoceptor and interfering with both the release of intracellular Ca2+ and the influx of extracellular Ca2+.
文摘Immunocytochemical localization of 5-hydroxytryptamine (5-HT) containing cells of the guinea-pig pancreas was studied by means of PAP-glucose oxidase-DAB-nickel (PAP-GDN) and PAPstaining methods on paraffin sections. In this study we demonstrated the presence of 5-HTimmunoreactive cells in the endocrine (islets) and exocrine pancreas of the guinea-ping. Cells exhib-iting 54-HT immunoreactivity were found in the center and the periphery of the pancreatic islets. The5-HT immunoreactive granules were evenly distributed throughout the cytoplasm, but was faint inthe nuclei. Cells of this type were also distributed in the exocrine pancreas. Grouped or single or single cellsoccurred intercalatedly between acinar cells, as well as in the epithlium of ducts and in the connectivetissues near the ducts or acini.
文摘AIM: To evaluate the intestinal motility changes evoked by 8 bacterial strains belonging to Bifidobacterium , Lactobacillus and Streptococcus genera within the probiotic preparation VSL#3. METHODS: Ileum and proximal colon segments isolated from guinea-pigs were used as a study model. Entire cells and cell fractions (cell debris, cell wall fraction, cytoplasmatic fraction, proteinaceous and non- proteinaceous cytoplasmatic components) of VSL#3 strains and, as controls, Escherichia coli, Salmonella aboni and Bacillus licheniformis were tested in this in vitro model. RESULTS: Among the bacterial cell fractions tested, only the cytoplasmatic fraction modified intestinal motility. Lactobacillus strains stimulated the contraction of ileum segment, whereas all probiotic strains tested induced proximal colon relaxation response. The non-proteinaceous cytoplasmatic components were responsible for the colon relaxation. CONCLUSION: The results obtained in this study suggest that the proximal colon relaxation activity showed by the probiotic bacteria could be one of the possible mechanisms of action by which probiotics exert their positive effects in regulating intestinal motility.
文摘The present study was carried out to evaluate the effect of different rates of dried cassava leafs in diet as replacement of protein sources on the weight gain and carcass yield of guinea-pigs, as well as on the physico-chemical and technological properties of guinea-pigs’ meat. A total of forty-eight (48) eight-week-old guinea-pigs were divided in a completely randomized experimental design, in four groups and fed with the experimental foods. These experimental foods were formulated as follows: cassava-leaf (Manihot esculenta) powder was incorporated at concentrations of 0%, 8%, 10% and 12% respectively in replacement of protein sources for R0, R1, R2 and R3. Each treatment consisted of a group of 12 guinea pigs per paddock (6 males and 6 females). The initial weight (IW), final weight (FW), daily weight gain (DWG) and total gain (TG) were evaluated. At the 22nd week, animals of each group were sacrificed by bleeding, then skinned and eviscerated. Carcasses were cut, and some parts (loin, thigh and shoulder) were collected, deboned and analysed. The highest FW and carcass yield (CY) were obtained with the use of 10% cassava leafs (R2): 556 g (FW), 42.65% (CY) for males and 529.17 g (FW), 37.39% (CY) for females. The incorporation of 8% (R1) and 12% (R3) cassava leafs led to a significant increase (P < 0.05) in protein levels in the loins (22.89%) and shoulders (22.43%) of females and the thighs (21.68%) and shoulders (21.09%) of males. However, protein levels of male fed with R3 in the various parts studied were higher than females fed with the same diet. The study of the technological parameters of guinea-pig’s meat showed that the incorporation of 8% and 12% cassava leafs in the diet resulted in a significant decrease in the water holding capacity and technological yield in the different parts studied. These results show that, the incorporation of cassava leafs in guinea-pigs’ diet made it possible to obtain good growth (R2) and meat of good technological quality.
文摘The unsatisfactory results of clinical trials with class-Ⅰ antiarrhythmic drugs have prompted a renaissance of interest in compounds with class-Ⅲ antiarrhythmic action. In the present, we have reevaluated the class-Ⅲ antiarrhythmic ef-
