肝动脉内持续输注5-氟尿嘧啶治疗原发性肝癌

目的 观察5-氟尿嘧啶(5-Fu)肝动脉内持续输注联合低剂量顺铂(DDP)(肝动脉内FP方案化疗)治疗原发性弥漫型肝癌的近期疗效和生存质量。方法 治疗组31例接受肝动脉内持续输注5-Fu 500mg／d,连用3～4周,DDP5mg／(m^2.d),静脉输注,每周用5天,连用3～4周为一疗程。共用2疗程。对照组接受常规介入治疗。结果 治疗组有效率54．83％,进展率19．36％,卡氏评分提高率54．84％。结论 肝动脉内FP方案是姑息治疗原发性弥漫型肝癌的有效方案。     

大肠癌细胞体外药敏试验结果与临床疗效的相关性

目的 研究肿瘤体外药敏试验对大肠癌个体化治疗的应用价值及与临床近期疗效的相关性.方法 采用组织块培养-MTT终点染色-计算机图像分析法(TECIA),体外测定大肠癌细胞对氟脲嘧啶(5-Fu)、顺铂(DDP)、阿霉素(ADM)、丝裂霉素(MMC)、奥沙利伯(OXA)及联用化疗药物的敏感性.结果 42例大肠癌细胞对试验化疗药物的敏感性有高到低依次为OXA＞ DDP＞ 5-Fu＞ MMC＞ ADM＞ CBP＞MTX.联合用药试验中,5-Fu+ DDP、5-Fu+ MMC的敏感率及抑制率高于单用;临床随访中,CF敏感组和CF不敏感组采用CF方案的临床有效率分别为68.6％( 24/35)和28.6％( 2/7),差异有统计学意义(x2=3.96,P＜0.05).结论 以组织块培养为基础的MTT体外药敏试验,与临床相关性较好.筛选药物后进行针对性的个体化治疗,能预测化疗疗效,提高大肠癌患者的生存率.     

健脾消癌汤配合化疗治疗老年胃癌晚期的疗效

目的观察探讨健脾消癌汤配合化疗治疗老年胃癌晚期的临床疗效,总结其临床治疗经验和临床意义。方法选取我院2009年11月至2012年6月老年胃癌晚期的患者46例,按照数字表随机抽取法分为观察组与对照组,各有23例,观察组使用健脾消癌汤配合化疗(DDP+CF+5-Fu)治疗,对照组单纯使用化疗(DDP+CF+5-Fu)治疗,观察对比两组疗效、副反应、生活质量改善(Karnofsky,KS)评分。结果观察组总有效率为69.6%(16/23),对照组总有效率为43.5%(10/23),两组治疗总有效率比较有明显差异(P<0.05),具有统计学意义。结论健脾消癌汤配合化疗治疗老年胃癌晚期的临床疗效显著,明显优于单纯使用化疗治疗。     

原发性肝癌的体外化疗药物敏感性探析

目的探究原发性肝癌对体外化疗药物的敏感性。方法选取我院2005年1月至2010年12月间确诊的原发性肝癌患者50例,选用MTT比色法,分别测定原发性肝癌对7种化疗药物的体外敏感性,包括阿霉素(ADM)、5-氟脲嘧啶(5-Fu)、顺铂(DDP)、丝裂霉素(MMC)、长春新碱(VCR)、羟基喜树碱、甲氨蝶呤(MTX)。结果肝癌患者对化疗药物的敏感率由高到低的顺序为羟基喜树碱>5-氟脲嘧啶>丝裂霉素>顺铂>阿霉素>甲氨蝶呤>长春新碱,各组敏感性具有明显的差异(P<0.05)。结论原发性肝癌对化疗药物的敏感性不同,临床治疗应该根据药敏试验的结果进行个体化综合治疗。     

大肠癌的药物敏感试验及临床意义

目的:通过测定59例大肠癌患者对阿霉素(ADM)、5-氟脲嘧啶(5-Fu)、丝裂霉素(MMC)、卡铂(CBP)、顺铂(DDP)、氨甲喋呤(MTX)6种化疗药物的体外敏感性试验,探讨肿瘤药敏试验对大肠癌患者个体化化疗的应用价值。方法:采用组织块培养-终点染色-计算机图像分析法(TECIA)。结果:59例大肠癌对肿瘤组织的的平均抑制率由高到低依次为5-Fu>MMC>ADM>MTX>DDP,联合用药的抑制率为MMC+DDP+5-Fu>MMC+5-Fu>DDP+5-Fu。结论:大肠癌是对化疗药物敏感性较好的肿瘤,且存在着明显的异质性。体外肿瘤药敏试验在指导大肠癌的临床用药及个体化化疗方面具有重要的指导意义。     

表阿霉素联合顺铂5-氟脲嘧啶治疗晚期胃癌

目的观察表阿霉素(EPI)、甲酰四氢叶酸(CF)、5氟-尿嘧啶(5-Fu)和顺铂(DDP)联合化疗治疗晚期胃癌的疗效和不良反应。方法应用EPI、CF、5-Fu和DDP(ECF)联合化疗治疗晚期胃癌36例,其中术后辅助性化疗14例,可评价疗效的有25例,全部病例均治疗2~6周期,观察评价疗效。结果完全缓解2例,部分缓解11例,总有效率52%。主要不良反应有骨髓抑制,脱发和厌食、恶心、呕吐等消化道反应,但患者可耐受。结论ECF方案仍是治疗晚期胃癌较为有效的方案,不良反应可以耐受。     

顺铂联合卡培他滨治疗胃肠道肿瘤的疗效及护理

目的观察顺铂联合希罗达治疗中晚期胃肠道肿瘤的临床疗效。方法 76例入选患者按随机数字表分为对照组(38例)顺铂(DDP)、5-氟尿嘧啶(5-Fu)联合亚叶酸钙(CF)治疗,观察组(38例)顺铂(DDP)联合口服卡培他滨治疗,并观察记录两组临床疗效以及骨髓抑制、胃肠道反应。结果观察组近期治疗有效率为60.53%,对照组为57.89%,两组比较无显著性差异(P>0.05),化疗后毒副反应的比较,观察组程度轻于对照组,有显著性差异(P<0.05)。结论顺铂联合卡培他滨治疗中晚期胃肠道肿瘤,其骨髓抑制以及胃肠道反应明显少于对照组,同时配合精心的基础、治疗、肿瘤药物不良反应护理,提高了对化疗的耐受性,减轻患者痛苦,提高生存质量,值得临床应用。     

体外药敏试验指导下的结直肠癌个体化化疗的临床研究

目的 研究大肠癌体外化疗药物敏感性与临床疗效的关系,为临床肿瘤化疗个体化提供依据。方法 用改进的MTT法测定53例结、直肠癌组织的化疗药物敏感性,并依药敏结果选择化疗方案,观察临床近期疗效和远期生存率。结果 53例结、直肠癌组织对8种化疗药物的敏感顺序为5-氟脲嘧啶(5-Fu)、顺铂(DDP)、丝裂霉素(MMC)、阿糖胞苷(ARA-C)、长春新碱(VCR)、氨甲喋呤(MTX)、阿霉素(ADM)、卡氮芥(BCNU),除DDP、5-Fu、MMC的敏感率高于文献报道的单药有效率外,其余与文献报道有效的单药基本一致。体外敏感性与临床近期疗效的总符合率为91.7％(11/12),药敏试验组和按经验给药组的3年生存率无明显区别,但药敏试验组5年生存率明显高于按经验给药组(P<0.05)。结论 MTT法测定化疗药物敏感性可帮助临床医师制定合理的化疗方案,按药敏试验结果指导化疗可能会有助于提高大肠癌患者的远期存活率。     

放疗联合化疗治疗中晚期食管癌的临床分析

目的分析放疗联合化疗治疗中晚期食管癌的临床疗效。方法对符合条件的82例病例,随机分为2组,放疗 化疗(综合组)41例,放疗前用DDP、5-Fu、CF化疗,放疗后再给予4个周期化疗;单纯放疗(单放组)41例。结果综合组和单放组近期疗效CR PR分别为83%和51%(P<0.05),1、2、3年生存率分别为70.7%、51.2%、39.0%和46.3%、29.3%、19.5%(P<0.01),综合组生存率明显高于单放组(P<0.05),但不良反应综合组高于单放组(P<0.05)。结论放疗联合化疗对中晚期食管癌治疗有协同作用,可以提高疗效。     

中晚期肝癌热疗结合化疗栓塞术的疗效观察

目的观察热疗介入化疗栓塞术治疗中晚期肝癌的临床疗效。方法原发性中晚期肝癌患者48例,随机分为二组,治疗组26例,对照组22例,治疗组行介入化疗栓塞术加局部区域热疗;对照组仅行介入化疗加栓塞治疗。化疗方案采用阿霉素(ADM)50-60mg,顺帕(DDP)60- 80mg,5氟脲嘧啶(5-F)500mg,栓塞剂是超液态碘化油及明胶海绵。结果通过两组比较,治疗组从肿瘤客观疗效、疼痛缓解率及生活质量均显著高于对照组。结论中晚期肝癌,热疗结合化疗栓塞术治疗明显高于单纯介入化疗栓塞术,增加治疗有效率,缓解疼痛,提高患者生活质量。     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Lung disease and PKCs

The lung offers a rich opportunity for development of therapeutic strategies focused on isozymes of protein kinase C (PKCs). PKCs are important in many cellular responses in the lung, and existing therapies for pulmonary disorders are inadequate. The lung poses unique challenges as it interfaces with air and blood, contains a pulmonary and systemic circulation, and consists of many cell types. Key structures are bronchial and pulmonary vessels, branching airways, and distal air sacs defined by alveolar walls containing capillaries and interstitial space. The cellular composition of each vessel, airway, and alveolar wall is heterogeneous. Injurious environmental stimuli signal through PKCs and cause a variety of disorders. Edema formation and pulmonary hypertension (PHTN) result from derangements in endothelial, smooth muscle (SM), and/or adventitial fibroblast cell phenotype. Asthma, chronic obstructive pulmonary disease (COPD), and lung cancer are characterized by distinctive pathological changes in airway epithelial, SM, and mucous-generating cells. Acute and chronic pneumonitis and fibrosis occur in the alveolar space and interstitium with type 2 pneumocytes and interstitial fibroblasts/myofibroblasts playing a prominent role. At each site, inflammatory, immune, and vascular progenitor cells contribute to the injury and repair process. Many strategies have been used to investigate PKCs in lung injury. Isolated organ preparations and whole animal studies are powerful approaches especially when genetically engineered mice are used. More analysis of PKC isozymes in normal and diseased human lung tissue and cells is needed to complement this work. Since opposing or counter-regulatory effects of selected PKCs in the same cell or tissue have been found, it may be desirable to target more than one PKC isozyme and potentially in different directions. Because multiple signaling pathways contribute to the key cellular responses important in lung biology, therapeutic strategies targeting PKCs may be more effective if combined with inhibitors of other pathways for additive or synergistic effect. Mechanisms that regulate PKC activity, including phosphorylation and interaction with isozyme-specific binding proteins, are also potential therapeutic targets. Key isotypes of PKC involved in lung pathophysiology are summarized and current and evolving therapeutic approaches to target them are identified.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.