2-(2, 6-二氯苯胺基)苯乙酸(3-硝氧甲基)苯酯的合成及抗炎镇痛活性

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。     

α—取代的对甲磺酰基苯丙烯酸的合成及抗炎活性

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.     

一氧化氮供体型阿司匹林和水杨酸甲酯的合成及其生物活性测定

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。     

对氨磺酰基苯亚甲基环酮类化合物的合成及抗炎活性

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。     

双氯芬酸锌的含量测定及稳定性考察

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…     

副作用最小的镇痛药——塞来昔布

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。     

双氯芬酸钠滴眼液治疗虹膜睫状体炎

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...     

一氧化氮供体型氢化可的松衍生物Ⅱ_5的抗炎及血管舒张活性研究

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.     

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抗炎活性

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.     

非甾体抗炎药4（2—噻吩羰基）苯酚类化合物的抗炎活性

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     

APPLICATION OF LORNOXICAM TO PATIENT-CONTROLLED ANALGESIA IN PATIENTS UNDERGOING ABDOMINAL SURGERIES

FOR anesthesiologis s ,treatingpostoperativepainhas alwaysbeen a problem.Althoughopioidshave been provedtobe effective,theirsideeffectscouldnotbeignored.With thedevelopmentofscienceand pharmacology,many drugs with aspectsof satisfactoryanalgesicefficacyand couldbe welltoleratedby patientshave been developed.And lornoxicamisone of them, which isa non-steroidalanti-inflammatorydrug (NSAID ), with analgesic, anti-infl-ammatory,andantipyreticproperties.Itseliminationhalf-time(3 to 5 hours) isle…     

Dr.Zhang Ren''''s Experience in the Acupuncture Treatment of Different Diseases with the Same Therapeutic Principle

Dr.Zhang Ren,the chief physician,is the chairman of Shanghai Acupuncture and Moxibustion Association.Having been engaged in medicine for about 40 years,he is experienced in treating various intractable diseases.In his long years of clinical practice,he advocates taking the TCM differentiation as the basis to seek for the acupuncture method for treatment of modern intractable diseases.The author of this essay had the fortune to follow Dr.Zhang in study.The following is a summary of Dr.Zhang's experience in the acupuncture treatment for different intractable diseases with the same therapeutic principle.     

Luo Lingjie''''s Experience in Treating Chronic Nephropathy

In treating chronic nephropathy,Luo Lingjie,a chief physician,pays attention to regulating the balance between yin and yang,treating infection if present,and removing pathogenic factors.He prescribes gentle drugs and uses carefully strongly warming-tonifying ones,emphasizes the importance of persuading the patient to persist in treatment with medication and nurse one's health for recuperation,and is good at combined use of TCM and western medicine therapy and brings the merits of various therapies into full play,with obvious theraoeutic effects.     

Acupuncture Combined with Spinal Tui Na for Treatment of Primary Dysmenorrhea in 30 Cases

Objective: To observe the therapeutic effects in acupunture treatment of primary dysmenorrhea combined with spinal Tui Na, and study its mechanism. Methods: Thirty cases of the treatment group were treated by acupuncture combined with spinal Tui Na, and thirty cases in the control group were treated by routine acupuncture. Results: The total effective rate was 93.3% in the treatment group, and 73.3% in the control group, with a significant difference between the two groups (P<0.05). Conclusions: Acupuncture combined with spinal Tui Na has good prospects for treatment of primary dysmenorrhea.     

猪肺磷脂注射液联合经鼻持续气道正压通气对呼吸衰竭早产儿的临床疗效及肌酸激酶同工酶活性的影响

目的 探讨猪肺磷脂注射液联合经鼻持续气道正压通气(NCPAP)对呼吸衰竭早产儿的临床疗效及肌酸激酶同工酶活性(CK-MB)的影响.方法 选取呼吸衰竭早产儿80例,分为观察组和对照组各40例.对照组采用NCPAP给氧治疗,观察组给予NCPAP给氧联合猪肺磷脂气管内给药.观察两组患儿治疗前及治疗12h、24 h后PaO2、PaCO2、血氧饱和度(SaO2)、pH的变化情况,检测治疗前及治疗5d后血清CK-MB水平;评估两组患儿的临床治疗效果.结果 两组患儿PaO2、PaCO2、SaO2、pH比较,差异均有统计学意义(P＜0.05),其中观察组治疗后的PaO2、SaO2、pH均高于对照组,PaCO2则低于对照组.两组的PaO2、SaO2、pH均随观察时间延长而升高(P＜0.05),PaCO2均随观察时间的延长而降低(P＜0.05).观察组治疗有效率为87.5％,显著高于对照组的70.0％ (P ＜0.05).治疗5d后两组患儿血清CK-MB水平均较前降低(P＜0.05),且观察组明显低于对照组(P＜0.05).结论 猪肺磷脂注射液气管内给药联合NCPAP可以显著降低呼吸衰竭早产儿CK-MB的含量,提高治疗有效率,起到很好的呼吸循环支持作用.     

Survey and practice of reporting quality of randomized controlled clinical trials on traditional Chinese medicine

Evidence obtained from randomized controlled trials （RCTs） has been generally accepted as the gold standard in the evaluation of clinical effectiveness. Readers need to understand the trial design, implementation, results, analysis and interpretation, so as to fully Jnderstand the results of RCTs. Thus, the investigators of RCTs have to report these items in a complete, accurate and clear manner. Since 1998, we have conducted several evaluations on the reporting quality of RCTs published in Chinese journals on traditional Chinese medicine （TCM） and results have shown that there is an urgent need for higher quality RCTs on TCM.     

TCM Treatment of Ankylosing Spondylitis by Tonifying the Kidney and Strengthening the Governor Vessel

Ankylosing spondylitis is a chronic and progressive disorder with inflammation mainly involving the central axis joints. It mainly affects the cervical spine and the lumbosacral area, with the pathogenesis closely related to the kidney and the Governor Vessel (GV). TCM holds that the syndrome is deficiency in origin and excess in superficiality, which is due to insufficiency of the kidney, deficiency of GV, and blocking of the channels with the invasion of exogenous evil, leading to poor circulation of qi and blood and malnutrition of the bones, muscles and joints. The TCM method of tonifying the kidney and strengthening GV to regulate circulation of qi and blood and check the arthralgia pain should be adopted, with the Kidney-Tonifying and GV Strengthening Decoction (益肾强督汤) prescribed.     

IMPROVING P-gp EXPRESSION IN HUMAN MONONUCLEAR CELLS IN VITRO TRANSFECTED BY MULTIDRUG RESISTANCE-1 mRNA

CHEMOTHERAPY playsa greatrolein the treat- ment of malignanttumors,especiallyingynecolo- gicalones.But inanticancerchemotherapy,leuko-cytopeniaisfrequentlytheprimarydose-limitingsideeffect factor.Moreover,cancersarefrequentlychemoresistantbe-causeof overexpressionof P-glycoprotein(P-gp), which isencodedby multidrugresistancegene (MDR1 ) and detectableinup to50% ofhuman cancersand renderscellsresistancetoanticancerdrugs.The safetyand potentialtherapeuticbenefitof mdr1 gene transferredto h…