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1.
目的:获得抗炎活性强、胃肠道副作用小的新型非甾体抗炎药。方法:以间羟基苯甲醛为原料,经还原、溴代和硝氧化,最后与双氯芬酸进行酯化反应,制备2-(2,6-二氯苯胺基)苯乙酸(3-硝氧甲基)苯酯(ZLR-9);观察ZLR-9对二甲苯致炎小鼠和角叉菜胶致炎大鼠的抗炎活性,对热板法实验和扭体实验小鼠的镇痛活性及致大鼠胃肠道反应,研究体内外ZLR-9的NO释放。结果:ZLR-9结构经MS、IR、^1HNMR确证,它的抗炎镇痛活性强于DC-Na,胃肠道副作用显著小于DC-Na,并小于文献报道的硝酸酯类DO-DC,体内有明显的NO释放。结论:ZLR-9值得深入研究。  相似文献   

2.
α—取代的对甲磺酰基苯丙烯酸的合成及抗炎活性   总被引:4,自引:0,他引:4       下载免费PDF全文
目的寻找高效低毒的非甾体抗炎药.方法以COX-2选择性抑制剂罗非昔布为先导化合物,合成其开环衍生物,应用二甲苯致小鼠耳肿胀模型和角叉菜胶致大鼠足跖肿胀模型评价其抗炎活性,并考察连续经口给药对大鼠胃肠道的影响.结果合成了17个目标化合物(I1-17),I1-15未见文献报道,其结构经IR、1HNMR、MS和元素分析确证.I1,3,7,9,10,13,15,16对小鼠耳肿胀模型表现显著的抗炎活性,I1,13,15对大鼠角叉菜胶致足跖肿胀模型显示较强的抗炎活性,在致炎后3 h I15的抗炎活性与双氯芬酸相当(P>0.05),I13,15与罗非昔布相当(P>0.05).上述活性化合物的胃肠道副作用小于双氯芬酸,但略大于罗非昔布.结论 I13,15值得深入研究.  相似文献   

3.
目的合成一氧化氮(NO)供体型阿司匹林和水杨酸甲酯,并检测其体外释放NO的能力和抗炎活性。方法通过酯键和醚键将阿司匹林和水杨酸甲酯分别与NO供体结构偶联,利用Griess试剂检测其释放NO的活性,并用二甲苯致小鼠耳肿胀模型初步研究其抗炎活性。结果合成了6种化合物,其中4种在体外具有良好的NO释放能力,6种化合物均保持有抗炎活性。结论所有化合物的结构均经MS、^1H-NMR确证,呋咱环型化合物体外能有效释放NO,NO供体结构的引入对其母体化合物的抗炎活性影响甚微。  相似文献   

4.
目的: 研究对氨磺酰基苯亚甲基环酮类化合物的合成及其抗炎活性。方法: 将三环类选择性COX-2抑制剂的药效团对氨磺酰基苯基与五元含氮杂环酮拼合,合成对氨磺酰基苯亚甲基环酮类化合物,采用二甲苯致小鼠耳肿胀及角叉菜胶致大鼠足跖肿胀两种模型评价其抗炎活性,并考察其连续7 d灌胃给药对大鼠胃肠道的影响。结果: 合成了12个目标化合物(LHZ-101~LHZ-112),结构经质谱、红外光谱、核磁共振氢谱和元素分析确证。小鼠耳肿胀模型显示LHZ-105,LHZ-106,LHZ-111具有明显的抗炎活性;角叉菜胶致大鼠足跖肿胀模型显示LHZ-106,LHZ-111具有较强的抗炎活性;LHZ-105,LHZ-106,LHZ-111的胃肠道副作用小于阳性药双氯芬酸钠和CI-1004。结论: 对氨磺酰基苯亚甲基环酮类化合物具有一定的抗炎活性,胃肠道副作用较小,值得进一步研究。  相似文献   

5.
双氯芬酸锌的含量测定及稳定性考察   总被引:3,自引:0,他引:3       下载免费PDF全文
双氯芬酸钠 (DiclofenacSodium ,双氯灭痛 )是第三代邻氨基苯甲酸类非甾体抗炎药 ,具有很好的消炎、镇痛作用 ,临床应用日趋广泛 ,但此药刺激性较大 ,长期服用有致溃疡的作用 ,胃肠道不良反应较为多见。锌具有抗溃疡活性 ,同时亦有抗炎效果[1 ] ,国外曾有过双氯芬酸锌的报道 ,药理实验表明双氯芬酸锌具有明显的抗胃溃疡活性[2 ,3] 。为此作者合成了双氯芬酸锌 ,并对其结构进行了鉴定 ,本文介绍了双氯芬酸锌的含量测定方法和稳定性考察的实验结果。1 实验材料1 .1 试药与试剂双氯芬酸锌 (自制 ) ;无水乙醇 (AR) ;95 %乙…  相似文献   

6.
李程 《求医问药》2011,(3):40-40
非甾体类抗炎药包括阿司匹林、双氯芬酸、布洛芬、塞来昔布等,是当今人类应用最多的抗炎止痛药。这类药物具有良好的抗炎和镇痛效果,被广泛应用于治疗骨关节炎、类风湿关节炎、急性疼痛、运动损伤和软组织疾病。目前,全世界每天约有3000万人在使用非甾体类抗炎药。然而,许多非甾体类抗炎药都有可能导致胃肠出现溃疡、穿孔和出血等副作用。  相似文献   

7.
双氯芬酸钠滴眼液治疗虹膜睫状体炎宋兰英张华马青云(茌平县医院眼科,252100)双氯芬酸钠滴眼液是国内一种新型的非甾体眼科抗炎药,作用强,副作用小,对各种非感染性眼炎有极其优异的抗炎作用。我科应用双氯芬酸钠治疗虹膜睫状体炎50例,效果良好,现报告如下...  相似文献   

8.
目的研究一氧化氮(NO)供体型氢化可的松衍生物Ⅱ5的抗炎活性及对大鼠主动脉环的松弛作用.方法采用小鼠耳二甲苯致炎模型对硝酸酯类和呋咱氮氧化物类一氧化氮供体型氢化可的松衍生物进行抗炎活性筛选,用角叉菜胶致大鼠足跖肿胀模型、棉球肉芽肿模型进一步研究活性化合物Ⅱ5的抗炎作用,Greiss法检测化合物Ⅱ5体外NO的释放情况,大鼠胸主动脉环收缩性实验检测化合物Ⅱ5对血管紧张性的影响.结果化合物Ⅱ5对二甲苯诱导的小鼠耳肿胀和角叉菜胶诱导的大鼠足跖肿胀的急性炎症,以及对棉球诱导的大鼠慢性肉芽组织增生都有明显的抑制作用,并具有一定的剂量相关性.体外释放NO约在3 h时接近最大释放值(0.905 μg/mL),在其后的3 h内较稳定(维持在0.905~0.957 μg/mL).对大鼠胸主动脉具有显著的舒张作用,其IG50为(139±57)nmol/L.结论NO供体型氢化可的松衍生物Ⅱ5具有较强的抗炎活性,在体外能平稳释放低水平的NO,对大鼠胸主动脉具有明显的舒张作用.  相似文献   

9.
目的:研究一氧化氮供体型α-取代的对甲磺酰基苯丙烯酸酯的合成及其抗炎活性.方法:将一氧化氮供体硝酸酯和呋咱氮氧化物通过酯键与α-取代的对甲磺酰基苯丙烯酸偶联,评价偶联化合物的抗炎活性,并考察连续经口给药对大鼠胃肠道(GI)的影响.结果:合成了10个新化合物(III1-10),其结构经IR、1HNMR和MS确证.4个化合物(III1,4,5,9) 对小鼠耳肿胀表现显著的抗炎活性,其中 III1对角叉菜胶致大鼠足跖肿胀模型抗炎活性与双氯芬酸(DC)和罗非昔布(RC)相当 (P>0.05);III5,9的GI副作用均显著小于DC(P<0.01),与RC和CMC-Na无明显差别(P>0.05).结论:一氧化氮供体型α-取代的对甲磺酰基苯丙烯酸酯的抗炎活性较强,GI不良反应较低.  相似文献   

10.
非甾体类抗炎药临床上用于治疗风湿性关节炎及其它胶原性疾病。国内外正不断地寻找新的化合物。我们曾发现氨甲基酚类化合物有较好的抗炎活性。一些含有4芳杂环苯  相似文献   

11.
Objective To observe blood pressure change with age in salt-sensitive teenagers whose salt sensitivity were determined by repeated testing.Methods Salt sensitivity was determined through intravenous infusion of normal saline combined with volume-depletion by oral diuretic furosemide in 55 teenagers. After five years, salt sensitivity was re-examined and subject blood pressure was followed up. Blood pressure changes in salt-sensitive teenagers were compared to that of non-salt sensitive teenagers over five years.Results After 5 years, the repetition rate of salt sensitivity determined by intravenous saline loading is 92.7%. In teenagers with salt sensitivity on the baseline, both the systolic blood pressure increments and increment rates were much higher than non-salt sensitive teenagers (12.7±12.1 mmHg vs. 2.8±5.2 mmHg, P< 0.01; 12.2%± 12.0% vs. 2.5% ±4.4%, P< 0.001,respectively). There was a similar trend for diastolic blood pressure (8.4 ± 6.4 mmHg vs. 3.7 ± 6.4 mmHg, P = 0.052; 13.2% ±10.6 % vs. 6.8%± 10.1%, P = 0.053, respectively).Conclusions Salt sensitivity determined by intravenous saline loading showed good reproducibility. Blood pressure increments with age were much higher in salt-sensitive teenagers than non-salt sensitive teenagers, especially in terms of systolic blood pressure.  相似文献   

12.
Objective: To evaluatel the value of D-dimers in patients with acute aortic dissection (AAD). Methods: This study consisted of 16 patients with AAD and 27 non-AAD patients. Serum D-dimets were measured by Sta-Liatest D-DI immunoturbidimetric assay. Results: D-dimer level was higher (P < 0.001) in patients with AAD(7.91 ± 5.52 μg/ml) than that in non- AAD group(1.57±1.24 μg/ml). D-dimer was positive (>0.4 μg/ml) in all patients with AAD and in 10 control group patients (37%). Among patients with acute AAD, D-dimers tended to be higher in Stanford A than in Stanford B (8.67 ± 4.31 μg/ml vs. 3.24±1.27 μg/ml, P <0.01). D-dimer values tended to be higher in more extended disease(3.84 ± 1.65 μg/ml, 8.57 ± 3.58 μg/ml and 11.87 ± 5.69 μg/ml in thoracic aorta, thoracic and abdominal aorta, thoracic and abdominal aorta and iliacal arteries, respectively, P < 0.05 for both 8.57 ± 3.58 and 11.87 ± 5.69 vs. 3.84 ± 1.65 ). Including the control group into the analysis, we found a sensitivity of 100%, a negative predictive value of 100%, and a specificity of 66% and a positive predictive value of 64% for D-dimer in diagnosis of AAD in our patients with suspected AAD. Conclusion: D-dimer was elevated in patients with AAD. A negative D-dimer test result could be useful in excluding AAD.  相似文献   

13.
Objective: To set up a simple and reliable rat model of combined liver-kidney transplantation. Methods: SD rats served as both donors and recipients. 4℃ sodium lactate Ringer's was infused from portal veins to donated livers,and from abdominal aorta to donated kidneys, respectively. Anastomosis of the portal vein and the inferior vena cava (IVC) inferior to the right kidney between the graft and the recipient was performed by a double cuff method, then the superior hepatic vena cava with suture. A patch of donated renal artery was anastomosed to the recipient abdominal aorta. The urethra and bile duct were reconstructed with a simple inside bracket. Results: Among 65 cases of combined liver-kidney transplantation, the success rate in the late 40 cases was 77.5%. The function of the grafted liver and kidney remained normal. Conclusion: This rat model of combined liver-kidney transplantation can be established in common laboratory conditions with high success rate and meet the needs of renal transplantation experiment.  相似文献   

14.
Increasing maternal age is the only etiological factor unequivocally linked to Down's syndrome in humans. The occurrence rate of newborns with Down's syndrome is about 1/220 in women over 35 years old. However, the occurrence rate in embryos fertilized in vitro, of the elder woman is unclear. Using FISH we screened the number of chromosome 21 in preimplanted embryos of 5 elderly women (average age, 38.4 years) to study the feasibility and necessity of screening trisomy 21 in embryos in patients over 35 years old at the in vitro fertilization (IVF) center.  相似文献   

15.
Real-time three-dimensional echocardiography (RT3DE)is a new ultrasound technique that enables dynamic threedimensional visualization and quantification of the heart in real time. Investigation of feasibility and methodology of RT3DE in determining left ventricular (LV) and right ventricular (RV) volumes, RT3DE was performed in 35 normal adults using Philips SONOS 7500 system with a 2-4 MHz matrix array transducer. The 60°×60° "pyramid" volume database was obtained and analyzed on a TomTec echo workstation. Both LV and RV volumes were calculated with four 3DE methods (i.e. apical 2, 4, 8, and 16-plane) through manually tracing ventricular endocardial borders in end diastole and end systole. Stroke volumes were then calculated. LV volume was also measured by 2DE Simpson's rule using GE VIVID 7 ultrasound machine.  相似文献   

16.
A clinical guideline for the therapeutic interventions of integrative medicine may be defined as a written document which states a series of recommendations on therapeutic interventions of integrative medicine for a special disease or condition. The guideline may provide assistance to medical professionals in making clinical decisions aimed at improving the clinical outcome of patients and reducing the costs of medical care(~'4~. Recommendations issued by a guideline should be based on the best available evidence in both Western and Chinese medicine. For fulfilling this purpose, the development of clinical guidelines for therapeutic interventions in the field of integrative medicine should follow scientific principles and undergo a rigorous processes.  相似文献   

17.
Objective:To probe into the influence of changes of ovarian hormones on the pathogenesis of the specific sub-type premenstrual syndrome(PMS)and reveal partial microcosmic mechanisms of adverse flow of liver-qi.Methods:Estradiol(E2)and progesterone(P)levels in serum were determined at different phases of menstrual cycle by radioimmunoassay.Results:In the group of PMS with adverse flow of liver-qi.the secretive peak value Of E2 and P at the follicular phase significantly decreased,and the secretive peak value at the luteal phase did not come into being.Conclusions:Low E2 and P secretive peak at the follicular phase and absence of secretive peak at the luteal phase is one of the microcosmic mechanisms of PMS with adverse flow of liver-qi.One of the pathophysiologic mechanisms of specific sub-type PMS is probably the continuous low level of E2and P.  相似文献   

18.
Journal of Nanjing Medical University (English Edition) JNMU, sponsored by Nanjing Medical University, was established in 1987. It is a bimonthly comprehensive English medical journal published locally and abroad.Since 2007, Journal of Nanjing Medical University (English Edition )was granted Elsevier the full publishing and distribution rights worldwide for the Electronic Edition, excluding the People's Republic of China.  相似文献   

19.
Objective To measure Derpl and Blot5 allergen levels in asthmatics' homes in Hongkong.Methods Seventy houses were enrolled for a mite indoor environment study. Dust samples were obtained from two sites of each patients' house: bed and floor. Derpl and Blot5 levels were quantified by a two-site monoclonal antibody-based ELISA technique.Results The levels of Derpl allergens found in bed (geometric mean (GM) 3.43 μg/g of dust; 95%CI, 1.89-4.96 μg/g)and on the floor (GM 1.12 μg/g of dust; 95%CI, 0.71-1.53 μg/g) indicated significant differences (P=0.005). However, the levels of Blot5 allergens found in bed (GM 19.00 μg/g of dust; 95%CI, 0.89-38.90 μg/g) and on the floor (GM 6.14 μg/g of dust; 95%CI, 0.40-11.90 μg/g) showed no statistically significant difference. In addition, in regards to the exposure index for Derpl and Blot5 allergens found in bed and on the floor, 17.6% in bed and 8.6% on the floor had levels of Blot5 ≥ 10 μg/g of dust, higher than those obtained for Derp1 (7.2% and 0% in bed and on the floor respectively, P< 0.05); higher percentages in bed and on the floor (25.0% and 35.7%) were observed for levels of Blot5 =0 μg/g of dust as compared with Derpl in bed and on the floor (4.3% and 14.5% respectively, P< 0.05).Conclusions Derpl and Blot5 are the major allergens found in this regional study, Blot5 is a more potent allergen in Hongkong, probably reflecting the high level of exposure to Blomia tropicalis (Bt). Bt and Dermatophagoides pteronyssinus (Dp) allergens should be included for precise diagnosis and effective immuno-therapeutic treatment of mite allergy in Hongkong.  相似文献   

20.
ANTI-PROLIFERATION EFFECT OF ORIDONIN ON HL-60 CELLS AND ITS MECHANISM   总被引:4,自引:0,他引:4  
Objcetive To investigate the anti-proliferation effect of oridonin on leukemic HL-60 cells and its mechanism. Methods HL-60 cells in vitro in culture medium were given different concentrations of oridonin. The inhibitory rate of cells were measured by microculture tetrazolium (MTT) assay, cell apoptotic rate was detected by flow cytometry (FCM), morphology of cell apoptosis was observed by hoechst 33258 fluorescence staining, and the activity of telomerase was detected using telomere repeat amplification protocol (TRAP) PCR-ELISA before and after apoptosis occurred. Results Oridonin could decrease telomerase activity, inhibit growth of HL-60 cells, and cause apoptosis significantly. The suppression was both in time- and dose-dependent manner. Marked morphological changes of cell apoptosis including condensation of chromatin and nuclear fragmentation were observed clearly by hoechst 33258 fluorescence staining especially after cells were treated 48-60 hours by oridonin. Conclusions Oridonin has apparent anti-proliferation and apoptotic effects on HL-60 cells in vitro, decreasing telomerase activity of HL-60 cells may be one of its most important mechanisms. These results will provide strong laboratory evidence of oridonin for clinical treatment of acute leukemia.  相似文献   

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