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1.
The effects of a new anti-allergic agent, MY-5116: isoamyl 5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano [3,2-c] quinoline-2-carboxylate, on experimental animal models of type I approximately type IV allergic reactions and the formation of IgE antibody were investigated. MY-5116 administered intraperitoneally at doses of 30 and 100 mg/kg suppressed significantly the homologous PCA in guinea pigs. MY-5116 administered intraperitoneally at the dose of 100 mg/kg also suppressed significantly the heterologous PCA in guinea pigs. MY-1250, the main active metabolite of MY-5116, showed no suppression on the Schultz-Dale reaction in guinea pigs, and MY-5116 showed no inhibition on the active systemic anaphylaxis in mice (type I). MY-5116 showed no inhibition on the reversed cutaneous anaphylaxis in rats (type II), the Forssman reaction in guinea pigs (type II), the Arthus reaction in mice (type III) and the delayed type hypersensitivity in mice (type IV). MY-5116 showed no suppression on the formation of IgE antibody in C3H/He and BALB/c mice and rats. From these results, it is concluded that MY-5116 selectively suppresses the experimental models of type I allergic reaction.  相似文献   

2.
The effects of YM-13650 on experimental animal models of cell-mediated immune responses (type IV), antibody formation and type I to type III allergic reactions were investigated. YM-13650 in the dose range of 6.3 to 100 mg/kg, p.o., inhibited the picrylchloride-induced delayed type hypersensitivity (Pc-DTH) in mice when administered during the induction and the effector phases. The compound also inhibited the Pc-DTH enhanced by the pretreatment with cyclophosphamide, and even bilateral adrenalectomy failed to reduce the inhibitory effect of the compound on Pc-DTH in mice. YM-13650 in doses of 25 and 50 mg/kg, p.o., prolonged the survival time of allogenic skin grafts in mice. However, no significant effect was observed on hapten-specific IgE and HA antibody production and PFC formation in mice in doses up to 300 mg/kg, p.o. YM-13650 inhibited the passive Arthus reaction in guinea pigs and the reversed passive Arthus reaction in rats (type III). On the other hand, YM-13650 did not show any inhibitory effect on passive cutaneous anaphylaxis in rats (type I), Forssman shock in guinea pigs (type II) and carrageenin-induced paw edema in rats. These results indicate that YM-13650 suppresses not only cell-mediated immune responses but also type III allergic reactions without any influence on type I and type II allergic reactions as well as an acute inflammatory reaction.  相似文献   

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The activities of four lysosomal enzymes, β-d-glucuronidase, β-d-galactosidase, α-d-mannosidase and acid phosphatase, were determined in tissue homogenates of rats suffering from drug-induced lipidosis. The lysosomal storage disease was produced by daily oral administration of 30–40 mg chlorphentermine/kg b.wt. for 12 weeks. The enzyme activities were found either increased or unchanged. A rise of about 2.5 fold was displayed by the β-d-glucuronidase in liver and kidneys and of 1.85 fold by the α-d-mannosidase in kidneys. The activity of the acid phosphatase was only slightly enhanced in the adrenals. The finding that a drug-induced lysosomal lipid storage is accompanied by an increase of some enzyme activities, corresponds to observations made on human cases of inherited storage diseases, and to experimental results obtained by overloading lysosomes with exogeneous material.  相似文献   

5.
AIM: Fetal adrenal, which synthesizes steroid hormones, is critical to fetal growth and development. Our recent research showed that some xenobiotics could interfere with steroidogenesis and induce intrauterine growth retardation in rats. The study on the characteristics of biotransformation enzymes in fetal adrenals still seems to be important with respect to possible significance in xenobiotic-induced fetal development toxicity. In this study, the activities of several important xenobiotic-related phase I and phase II enzymes in human fetal adrenals were examined and compared with those in fetal livers. METHODS: The activity and mRNA expression were determined by enzymatic analysis and RT-PCR. RESULTS: The levels of cytochrome (CYP)2A6, CYP2E1, and CYP3A7 isozymes in fetal adrenals were 82%, 92%, and 33% of those in fetal livers, respectively. There was a good positive correlation between adrenal CYP2A6 activity and gestational time. The values of alpha glutathione S-transferase (GST), pi-GST, and microGST in adrenals were 0.5, 4.4, and 8.3-fold of those in the livers, respectively, and the activity of adrenal pi-GST was negatively correlated with gestational time. The uridine diphosphoglucuronyl transferase activities, which were measured using p-hydroxy-biphenyl and 7-hydroxy-4-methylcoumarin as substrates, were 9% and 3%, respectively, of those in the fetal livers. CONCLUSION: Our investigation suggested that adrenal could be an important xenobiotic-metabolizing organ in fetal development and may play a potential role in xenobiotic-induced fetal development toxicity.  相似文献   

6.
Pulmonary and hepatic drug metabolizing enzyme activities of tuberculous guinea pigs were examined in detail. Experimental tuberculosis resulted in enlargement of liver and lung accompanied by decreased microsomal cytosolic protein. The tuberculosis infection resulted in decreased hepatic contents of cytochrome P-450 and cytochrome b5 NADPH-cytochrome C reductase in lung and liver. A parallel decrease in the microsomal mixed function oxidases (MFO) was observed in liver and lung of tuberculous guinea pigs. The hepatic and pulmonary activities of UDP-glucuronyl transferase were elevated in the infected animals. Glutathione S-transferase activity exhibited an increase in liver and decrease in the lung of tuberculous guinea pigs. Some of the changes observed in monooxygenase in tuberculosis were caused by reduced food consumption. In general, tuberculosis infection can be viewed to lower drug metabolizing capacity of the animal, probably due to the damage and disturbed membrane integrity.  相似文献   

7.
The effects of butyl 3'-(1H-tetrazol-5-yl)oxanilate (WP-833), a new antiallergic drug, on type I to type IV allergic reactions were investigated by employing various animal models. WP-833 (i.v. and p.o.) dose-dependently inhibited homologous or heterologous passive cutaneous anaphylaxis (PCA) mediated by rat or mouse immunoglobulin E (IgE) in rats. Homologous PCA caused by guinea pig IgE was also inhibited by WP-833. In addition, WP-833 had inhibitory actions upon homologous PCA induced by rat or guinea pig IgG. However, WP-833 showed no inhibition of rat skin reactions caused by histamine, serotonin and bradykinin, contrasting with the inhibition of prostaglandin E1-induced skin reaction. Furthermore, both adrenalectomy and propranolol treatment exerted no influences on the inhibition of IgE-mediated homologous PCA in rats by WP-833. In contrast to above findings demonstrating that WP-833 clearly inhibited type I allergic reaction, systemic Forssman shock in guinea pigs and reversed cutaneous anaphylaxis in rats (type II), passive Arthus reaction in rats (type III), and contact dermatitis and tuberculin reaction in mice (type IV) were unaffected by WP-833 even in higher doses than in those capable of completely inhibiting type I allergic reaction.  相似文献   

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Although there is evidence for the anti-inflammatory activity of nicotinamide, there is no evaluation of its effects in models of nociceptive and inflammatory pain. In addition, there is no information about the potential anti-inflammatory and antinociceptive activities of the nicotinamide isomers, picolinamide and isonicotinamide. Per os (p.o.) administration of nicotinamide (1000 mg/kg, −1 h) inhibited the first and second phases of the nociceptive response induced by formalin in mice. In the model of nociceptive pain, exposure of mice to a hot-plate (50 °C), nicotinamide (1000 mg/kg, −1 h) also presented antinociceptive activity. Nicotinamide (500 mg/kg, −1 and 3 h) also inhibited the mechanical allodynia induced by carrageenan in rats, a model of inflammatory pain. In addition to inhibiting the nociceptive response, nicotinamide (500 or 1000 mg/kg, −1 and 3 h) inhibited the paw edema induced by carrageenan in mice and rats. P.o. administration of picolinamide (125 mg/kg, −1 h) and isonicotinamide (500 or 1000 mg/kg, −1 h) inhibited the second phase of the nociceptive response induced by formalin in mice. The paw edema induced by carrageenan in mice was also inhibited by isonicotinamide (500 or 1000 mg/kg, −1 h) and picolinamide (125 mg/kg, −1 h and 3 h). The results represent the first demonstration of the activity of nicotinamide and its isomers in models of nociceptive and inflammatory pain and provide support to their anti-inflammatory activity. The demonstration of new activities for nicotinamide is important as it may contribute to expand its use in the treatment of other pathological conditions.  相似文献   

10.
Fluoride (NaF, 50 mg/kg po) administration to rats caused an increased urinary excretion of inorganic phosphate, calcium, magnesium, potassium, and sodium associated with polyuria. The renal enzyme activities of Na+ and K+-stimulated adenosine triphosphatase [(Na+ + K+)-ATPase], Mg2+ and Ca2+-stimulated adenosine triphosphatase [(Mg2+ + Ca2+)-ATPase], acid phosphatase, and alkaline phosphatase were decreased by single oral doses of fluoride. A decrease in renal (Na+ + K+)-ATPase activity was associated with an increase in urine volume and a decrease in serum sodium concentration.  相似文献   

11.
The activities of certain enzymes in the urine and tissues of rats given 2% sodium o- phenylphenate in the diet for 20 wk were examined. Urinary gamma-glutamyl transpeptidase (gamma GTP) decreased immediately after the start of feeding of the treated diet and its activity remained low for 20 wk. The gamma GTP and alkaline phosphatase (ALP) activities in kidney homogenate decreased to about 80% of the control at 20 wk, but G6PD activity was significantly increased; Na,K-ATPase was unchanged. On the other hand, the gamma GTP activity in the liver homogenate of treated rats was increased to about eight times that of the controls, the G6PD activity showed a significant increase, but the ALP and Na, K-ATPase activities were not significantly different from the control values. The glutathione concentration in the livers of treated rats was significantly reduced.  相似文献   

12.
Riboflavin, similar to other vitamins of the B complex, presents anti-inflammatory activity but its full characterization has not yet been carried out. Therefore, we aimed to investigate the effect of this vitamin in different models of nociception, edema, fever and formation of fibrovascular tissue. Riboflavin (25, 50 or 100 mg/kg, i.p.) did not alter the motor activity of mice in the rota-rod or the open field models. The second phase of the nociceptive response induced by formalin in mice was inhibited by riboflavin (50 or 100 mg/kg). The first phase of this response and the nociceptive behavior in the hot-plate model were inhibited only by the highest dose of this vitamin. Riboflavin (25, 50 or 100 mg/kg, i.p.), administered immediately and 2 h after the injection of carrageenan, induced antiedema and antinociceptive effects. The antinociceptive effect was not inhibited by the pretreatment with cadmium sulfate (1 mg/kg), an inhibitor of flavokinase. Riboflavin (50 or 100 mg/kg, i.p., 0 and 2 h) also inhibited the fever induced by lipopolysaccharide (LPS) in rats. Moreover, the formation of fibrovascular tissue induced by s.c. implant of a cotton pellet was inhibited by riboflavin (50 or 100 mg/kg, i.p., twice a day for one week). Riboflavin (10 or 25 mg/kg, i.p.) also exacerbated the effect of morphine (2, 4 or 8 mg/kg, i.p.) in the mouse formalin test. In conclusion, the study demonstrates the antinociceptive and anti-inflammatory activities of riboflavin in different experimental models. These results, associated with the fact that riboflavin is a safe drug, is approved for clinical use and exacerbates the antinociceptive effect of morphine, may warrant clinical trials to assess its potential in the treatment of different painful or inflammatory conditions.  相似文献   

13.
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.  相似文献   

14.
Trichloroethylene (TCE) and tetrachloroethylene (perchloroethylene; PCE) are commonly identified as environmental contaminants of groundwater. Previously, we investigated the enhancing effects of TCE and PCE on antigen-induced histamine release and inflammatory mediator production in rat mast cells. In this study, to examine the potential effect of TCE and PCE on antigen-induced histamine release from mouse mast cells, mouse bone marrow-derived mast cells (BMMC) were sensitized with anti-dinitrophenol (DNP) monoclonal IgE antibody and then stimulated with DNP-BSA containing with TCE or PCE. Both TCE and PCE significantly enhanced antigen-induced histamine release from BMMC. Next we investigated the effects of TCE and PCE on the passive cutaneous anaphylaxis (PCA) reaction in vivo using ICR mice. TCE and PCE significantly enhanced the PCA reaction in a dose-dependent manner. In addition, we examined the enhancing effects of ingesting small amount of TCE and PCE in drinking water on antigen-stimulated allergic responses. After the ICR mice had ingested TCE or PCE in their drinking water for 2 or 4 weeks, we performed the PCA reaction. Both TCE and PCE ingestion enhanced the PCA reaction in a dose-dependent manner for 4 weeks. These results suggest that exposure to TCE and PCE leads to the augmentation of type I allergic responses in many species.  相似文献   

15.
红花注射液致Ⅰ型过敏反应试验   总被引:2,自引:0,他引:2  
目的:研究红花注射液在全身主动过敏试验和被动皮肤过敏试验中是否出现过敏反应。方法:豚鼠分别腹腔注射红花注射液5 mL.kg-1,0.9%氯化钠注射液5 mL.kg-1及牛血清白蛋白生理盐水注射液5 mL(40 mg).kg-1,qod,连续3次进行致敏。末次致敏后14 d各组静脉单次注射2倍剂量的以上相应受试物进行激发,观察30 min内是否有过敏反应;SD大鼠皮内注射相应抗血清0.1 mL被动致敏48 h后,分别静脉注射红花注射液5 mL.kg-1,0.9%氯化钠注射液5 mL.kg-1和牛血清白蛋白生理盐水溶液5 mL(40 mg).kg-1及1%伊文思蓝溶液共1 mL进行激发,30 min后处死动物,观察注射点皮肤蓝斑直径。结果:红花注射液组致敏期间豚鼠未出现任何异常反应,给予激发剂量后红花注射液组其中一个批次出现异常反应,但未出现豚鼠死亡;红花注射液组和牛血清白蛋白溶液组大鼠背部皮肤内层均出现蓝斑。结论:红花注射液组全身主动过敏反应和被动皮肤过敏均为阳性,红花注射液具有一定的致敏性。  相似文献   

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17.
The present study was planned to investigate the antioxidant, antinociceptive, and anti-inflammatory activities of atorvastatin and rosuvastatin (1, 3 and 10 mg/kg, p.o.) in various animal models. The antinociceptive effect was assessed by chemically- (formalin, acetic acid) and thermally- (hot plate) induced nociception, while anti-inflammatory effect was evaluated using carrageenan-, formaldehyde-induced paw oedema and cotton pellet-induced granuloma. The effect of atorvastatin and rosuvastatin on liver antioxidant enzymes like superoxide dismutase, glutathione, LPO, CAT along with the effect on lactate dehydrogenase (LDH) and alkaline phosphatase (ALP) was evaluated in the cotton pellet-induced granuloma model. Atorvastatin and rosuvastatin showed significant decrease (p < 0.05) in carrageenan- and formaldehyde-induced rat paw oedema and reduced granuloma formation in the cotton pellet-induced granuloma method (p < 0.01) while the levels of LDH and ALP were also significantly decreased (p < 0.05). The liver antioxidant enzyme levels were found to be restored (p < 0.05). Atorvastatin and rosuvastatin also showed antinociceptive activities (p < 0.05 and p < 0.01) in the acetic acid- and formalin-induced nociception in mice, while there was no significant activity in the hot plate method. The present findings suggest that atorvastatin and rosuvastatin possess dose-dependent antioxidant, analgesic, and anti-inflammatory activities.  相似文献   

18.
齐墩果醇酸对免疫系统及I型变态反应的影响   总被引:4,自引:0,他引:4  
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Indomethacin increases the cellular levels of several lysosomal enzymes in cultures of mouse peritoneal macrophages exposed to the drug for periods of time ranging from one day to four weeks. This increase can be blocked by puromycin, an inhibitor of protein synthesis. Pretreatment of macrophages with indomethacin inhibits the selective release of lysosomal enzymes induced by a C-mucopolysaccharide peptidoglycan complex purified from the cell walls of Group A streptococci.  相似文献   

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