对苯二甲酸接触工人尿酶及微球蛋白的变化

选择１２７名ＴＰＡ作业工人进行动式个体采样,并留取１２７名ＴＰＡ作业工人当日工前工后尿样和７０名对照工人的工前尿。对尿样中γ谷氨酰转肽酶（ＧＧＴ）、碱性磷酸酶（ＡＬＰ）、乳酸脱氢酶（ＬＤＨ）、Ｎ乙酰βＤ氨基葡糖苷酶（ＮＡＧ）活性以及尿ＴＰＡ、α１微球蛋白（α１ＭＧ）、β２微球蛋白（β２ＭＧ）水平进行分析。结果显示,ＴＰＡ接触组尿ＧＧＴ、ＡＬＰ、ＬＤＨ、ＮＡＧ活性以及尿α１ＭＧ、β２ＭＧ水平与对照组相比无显著差别,而５～ｍｍｏｌ／ｍｏｌ．Ｃｒ尿ＴＰＡ负荷组工人尿β２ＭＧ与对照组相比有明显升高（Ｐ＜００５）,尿β２ＭＧ与尿ＴＰＡ负荷量呈现一定的剂量依赖关系。尿ＴＰＡ水平对尿酶活性、α１ＭＧ均未产生明显影响。不同累积接尘量和不同工龄的工人尿酶和微球蛋白无明显差异。提示ＴＰＡ对肾实质可造成一过性可逆性影响,尚不能说明肾实质受到器质性损伤。     

二硫化碳接触者肾功能损伤早期监测指标评价

通过对某化纤厂７１名二硫化碳作业工人调查发现，二硫化碳接触工人尿β２－ＭＧ和ＬＤＨ显著高于对照组，且随暴露二硫化碳浓度增高，工龄延长而升高，呈剂量－反应关系。ＡＫＰ和ＡＬｂ则在高浓度组和高工龄段显著高于对照组。表明尿β２－ＭＧ和ＬＤＨ可作为慢性二硫化碳接触者肾功能损伤的早期监测指标。     

低浓度苯乙烯对作业工人健康危害的调查

本文对１２２名苯乙烯接触工人和３５名对照组医务人员进行了流行病学调查。结果表明，两作业车间中苯乙烯浓度分别为１３．８２ｍｇ／ｍ＾３和４５．９８ｍｇ／ｍ＾３。在此浓度下，两接触组工人主要表为神经衰弱，其症状检出率显著高于对照组；两接触组血ＲＢＣ、ＷＢＣ、Ｈｂ均降低，Ｎ和Ｌ绝对值均增高，且Ｌ绝对值有显著差异；尿β２－Ｍ、γ－ＧＴ、ＬＤＨ均显著增高；班后尿ＭＡ含量和班前和对照组均显著增高。提示长期接触低     

长期接触铅作业工人肾功能损害探讨

［目的］探讨长期接触铅作业工人肾功能损害。［方法］选择三组接触铅作业工人（第一组为长期接铅仍在岗位的工人;第二组为长期接铅但已脱离岗位退休的工人;第三组为短期接铅的工人）和对照组同样测定血铅（Ｂ－Ｐｂ）、尿β２ －微球蛋白（Ｕ－β２－ＭＧ）、尿δ－氨基酮戊酸（Ｕ－δ－ＡＬＡ）内生肌酐清除率（ＣＣｒ）等指标。［结果］三组接铅工人的血铅浓度平均值均与对照组之间存在明显差异,第一组工人的Ｕ－β２－ＭＧ和Ｕ－δ－ＡＬＡ 浓度最高并与其他各组之间有显著性差异,而第二组与第三组此两项指标与对照组之间没有显著性差异。临床体检各组人员中均未发现有异常症状和体征。［结论］长期接触铅作业工人肾功能将受到损害,但早期的肾功能损害是可恢复的,Ｕ－β２ －ＭＧ作为肾小球早期损害指标是较为敏感的,建议将其作为接铅工人肾损控制的监护指标。     

对苯二甲酸作业人群尿液生化反应的研究

目的　探讨对苯二甲酸（ＴＰＡ） 作业人群尿酶和尿液离子水平的变化。方法　对１０７ 名工人进行个体采样并测定空气和尿中ＴＰＡ 浓度。留取１２７ 名ＴＰＡ 作业工人当日工前、工后尿样和７１ 名对照尿样,对尿样中γ谷氨酰转肽酶（γＧＧＴ） 、碱性磷酸酶（ＡＬＰ） 、乳酸脱氢酶（ＬＤＨ） 、Ｎ乙酰βＤ氨基葡糖苷酶（ＮＡＧ） 活力和尿ｐＨ 值、Ｎａ ＋ 、Ｋ＋ 、Ｃｌ－ 、Ｃａ２ ＋ 、ＮＨ４ ＋ 、ＰＯ４３ － 和ＳＯ４２ － 离子浓度进行分析。结果尿ＴＰＡ 水平与空气ＴＰＡ 浓度存在相关关系。接触组尿Ｎａ ＋ 、Ｃｌ－ 、Ｃａ２ ＋ 、ＮＨ４ ＋ 和ＳＯ４２ － 离子浓度显著高于对照组（ Ｐ＜ ０ ．０５） ;指标聚类统计分析结果显示：尿ＴＰＡ 与尿ＮＨ４ ＋ 相关系数最大（ ｒ ＝ ０ ．２１２ ５ ,Ｐ＝ ０ ．０１９ ８） ,两者之间存在剂量依赖关系;对接触组和对照组作逐步判别分析,筛选出Ｃａ２ ＋ 、ＮＨ４ ＋ 和ＮＡＧ３ 项最有价值的指标。结论　ＮＨ４ ＋ 排泄增多可引起机体负氮平衡,以尿ＮＨ４ ＋ 水平作为接触ＴＰＡ的生物学效应指标,并辅以Ｃａ２ ＋ 和ＮＡＧ 两项指标可监测ＴＰＡ 对接触人群肾功能的早期影响     

二氧化硅粉尘作业工人肾功能损害的调查研究

对１５３名二氧化硅粉尘作业工人（接尘组）和８４名年龄相当但不接尘及其它毒物者（对照组）肾功能进行调查。结果发现接尘工人尿ＮＡＧ活性及尿α１－ＭＧ、β２－ＭＧ、Ａｌｂ含量较对照组显著升高，且随接尘工龄延长而明显升高，呈剂量－反应关系。若以超过对照组９５％单侧上限值为阳性标准，则尿α１－ＭＧ、β２－ＭＧ、Ａｌｂ、ＮＡＧ阳性率增高有显著意义，且尿酶与尿蛋白各指标之间呈正相关关系。表明长期接触含游离二氧化     

苯,甲苯,二甲苯暴露人群遗传毒性生物标志物的研究

为研究苯系物职业接触人群的生物标志物，应用高效液相色谱－电化学检测系统（ＨＰＬＣ－ＥＣ）分析８７名苯接触工人及３０名对照人群外周血淋巴细胞８－羟基－２－脱氧鸟苷（８－ＯＨｄＧ），同时检测工人个体接触空气苯浓度及尿粘康酸（ＴＴＭＡ）、外周血淋巴细胞微核（ＭＮ）及白细胞（ＷＢＣ）值。结果显示：外周血淋巴细胞８－ＯＨｄＧ、ＭＮ、尿ＴＴＭＡ在苯接触人群增高显著，８－ＯＨｄＧ与空气苯、尿ＴＴＭＡ存在良好相关，且８－ＯＨｄＧ与ＭＮ之间存在一定相关性。结果提示：苯可诱导职业接触人群ＤＮＡ氧化损伤，苯的遗传毒性机理可能是通过多位点、多作用机理、多遗传后果所致。８－ＯＨｄＧ可作为苯系物职业接触人群的生物标志物，影响苯接触人群外周血淋巴细胞８－ＯＨｄＧ形成的因素有性别和甲苯。     

CS对生产工人血三酯影响的观察

本文对７８名ＣＳ２生产工人和５５例对照组工人的血三酯进行了测定。结果表明：甘油三酯的异常率和平均值与对照组相比，有非常显著性差异（Ｐ〈０．０１）。接触ＣＳ２的不同工龄组工人，甘油三酯的均值随工龄的延长而增高，异常率也相应增高，且与生产环境中ＣＳ２浓度呈正相关（ｒ＝０．７７３ Ｐ〈０．０５）。提示；ＣＳ２可引起生产工人血甘油三酯的改变，血甘不同三酯的测定可作为其健康监护的指标之一。     

尿中2—硫代噻唑烷—4—羧酸排泄规律初探

对１５名二硫化碳（ＣＳ２）作业工人与１４名非接触者进行了尿２硫代噻唑烷４羧酸（ＴＴＣＡ）排泄规律研究。结果表明，随ＣＳ２接触时间与接触量的增加，ＴＴＣＡ水平逐渐增高（班前、班中、班末ＴＴＣＡ几何均数分别为１．２５７４、１．６１２０、２．１８０５／ｇｃｒ），呈剂量效应关系。停止接触后ＴＴＣＡ排泄较快，１６ｈ后基本降至前一天班前水平。班末尿ＴＴＣＡ能灵敏地反映个体近期ＣＳ２接触量。４２个非接触者尿样中有３２个检出微量ＴＴＣＡ（７６．２％），其ＴＴＣＡ排泄无明显特征，但摄入白酒可影响尿ＴＴＣＡ的排泄     

长期接触低浓度二硫化碳对工人健康的影响

目的探讨长期接触低浓度二硫化碳（ ＣＳ２）对工人健康的影响。方法对 １５０名接触ＣＳ２粘胶车间工人和８７名对照者健康状况作了调查,同时监测了１０年来车间空气中ＣＳ２浓度。结果 １０年来车间空气中ＣＳ２浓度基本低于卫生标准;接毒者工龄长于１０年的工人记忆减退、失眠和视觉症状等自觉症状发生显著增加（ＯＲ值分别为１９．６９、１５．４３、８．０７）。接触ＣＳ２工人眼底、视野、心电图、Ｂ超的异常率均高于对照组（Ｐ＜０．０５）。结论长期接触低浓度ＣＳ２对工人健康有影响。     

An evaluation of methods for the stratified analysis of clustered binary data in community intervention trials

A simulation study is conducted in a community intervention setting. Several methods of stratified analysis of clustered binary data are compared in terms of empirical significance and empirical power levels. They are the Mantel-Haenszel test statistic (chi(2) (MH)), the adjusted Mantel-Haenszel test statistic of Donald-Donner (chi(2) (DD)), Rao-Scott (chi(2) (RSN) and chi(2) (RSP)), and Zhang-Boos (chi(2) (ZBN) and chi(2) (ZBP)), Wald (chi(2) (W)), robust Wald (chi(2) (RW)), score (chi(2) (S)), robust score (chi(2) (RS)), and the test statistic based on generalized linear mixed model (GLMM) (chi(2) (GLMM)). When rho not equal 0, chi(2) (MH) has inflated type I error, and it should not be used when observations are correlated. The results also warn of the use of chi(2) (RSN) and chi(2) (RW) due to their poor performance in terms of empirical significance level. chi(2) (ZBP) and chi(2) (GLMM) have better empirical significance levels as compared to other statistics; however, chi(2) (ZBP) tends to have lower empirical powers than other statistics when the number of clusters (N) is less than 24. chi(2) (RSP) provides the highest empirical powers when rho > or = 0.1 and N < or = 12. When rho < or = 0.01, we recommend the use of chi(2) (RS) and chi(2) (GLMM) since they have better overall performance in terms of empirical significance levels and empirical power levels.     

New transition metal ion complexes with benzimidazole-5-carboxylic acid hydrazides with antitumor activity

Metal complexes of 2-methyl-1H-benzimidazole-5-carboxylic acid hydrazide (4a; L(1)) and its Schiff base 2-methyl-N-(propan-2-ylidene)-1H-benzimidazole-5-carbohydrazide (5a; L(2)) with transition metal ions e.g., copper, silver, nickel, iron and manganese were prepared. The complexes formed were 1:1 or 1:2 M:L complexes and have the structural formulae [Cu(L(1))Cl(H(2)O)]Cl x 3 H(2)O (6), [Ag(L(1))NO(3)(H(2)O)] (7), [Ni(L(1))Cl(2)(H(2)O)(2)] x H(2)O (8), [Fe(L(1))Cl(3)(H(2)O)] x 3 H(2)O (9) and [Mn(L(1))(2)Cl(H(2)O)]Cl x 3 H(2)O (10) for ligand L(1), and [Cu(L(2))Cl(2)(H(2)O)(2)] x H(2)O (11), [Ag(L(2))(2)]NO(3) x H(2)O (12), [Ni(L(2))(2)Cl(2)] x 5 H(2)O (13), [Fe(L(2))(2)Cl(2)]Cl x 2 H(2)O (14) and [Mn(L(2))Cl(2)(H(2)O)(2)] x H(2)O (15) for ligand L(2). The antitumor activity of the synthesized compounds has been studied. The silver complex 7 was found to display cytotoxicity (IC(50)=2 microM) against both human lung cancer cell line A549 and human breast cancer cell line MCF-7.     

Organotin(IV) complexes of 2-pyridineformamide-derived thiosemicarbazones: antimicrobial and cytotoxic effects

Reaction of n-butyltin trichloride [(n-Bu)SnCl(3)] with 2-pyridineformamide thiosemicarbazone (H2Am4DH) and its N(4)-methyl (H2Am4Me) and N(4)-ethyl (H2Am4Et) derivatives gave [(n-Bu)Sn(2Am4DH)Cl(2)] (1), [(n-Bu)Sn(2Am4Me)Cl(2)] (2), and [(n-Bu)Sn(2Am4Et)Cl(2)] (3). Thiosemicarbazones as well as their tin complexes are active as antimicrobials against the growth of Candida albicans and Salmonella typhimurium and were highly active against malignant glioblastoma. The cytotoxic activity of complexes 1-3 is similar. Among the studied compounds [(n-Bu)Sn(2Am4DH)Cl(2)] (1) was the most active as antiproliferative (cytostatic) agent. Thiosemicarbazones and their tin(IV) complexes proved to be more potent as cytotoxic agents than cisplatin. All the compounds were able to induce apoptosis.     

重铬酸钾和氧化还原物质反应致质粒DNA断链

目的　在体外研究六价铬化合物诱导质粒ＤＮＡ 链断裂的作用。方法　采用质粒松弛法。结果　重铬酸钾（０ ．５ ｍｍｏｌ／Ｌ） 、抗坏血酸（１ ｍｍｏｌ／Ｌ） 、谷胱甘肽（５ ｍｍｏｌ／Ｌ） 或过氧化氢（１７ｍｍｏｌ／Ｌ） 单独作用都不能诱导明显的ＤＮＡ 单链断裂。然而,将重铬酸钾和具有氧化还原功能的物质与ＤＮＡ 共同温浴,发现重铬酸钾和抗坏血酸、谷胱甘肽或过氧化氢反应后可明显诱导质粒ＤＮＡ 单链断裂。重铬酸钾和过氧化氢（１７ ｍｍｏｌ／Ｌ） 还诱导质粒ＤＮＡ 双链断裂。结论　抗坏血酸、谷胱甘肽和过氧化氢可能在重铬酸钾的致癌过程中起重要作用。     

New perfluoroalkylated amphiphilic methacrylates bearing sulfinyl group as monomers for biomedical applications: water content and oxygen permeability of their copolymers with DEGMA

Perfluoroalkylated methacrylates 7a-c bearing sulfinyl group within a straight-chain ester group, i.e. CH(2)=C(CH(3))CO(2)CH(2)CH(2)S(O)-CH(2)CH(2)CF(2)(CF(2)CF(2))(n)CF(3) (n=1-3) were prepared by two alternative synthetic sequences from 2-[(polyfluoroalkyl)sulfanyl]ethanols HOCH(2)CH(2)SCH(2)CH(2)CF(2)(CF(2)CF(2))(n)CF(3) (n=1-3) in overall yields of 88-91%. Copolymers of 7a-c with diethylene glycol methacrylate (DEGMA) prepared in bulk under radical conditions display high transparency, increased water content and good oxygen permeability properties, which are advantageous for their application in ophthalmology and as prosthetic materials.     

Antihelminthic activity of some newly synthesized 5(6)-(un)substituted-1H-benzimidazol-2-ylthioacetylpiperazine derivatives

Piperazine derivatives of 5(6)-substituted-(1H-benzimidazol-2-ylthio)acetic acids were synthesized by using two methods and studied for antihelminthic activity. The antiparasitic screening showed that compounds 18-24 exhibited higher activity against Trichinella spiralis in vitro in comparison to methyl 5-(propylthio)-1H-benzimidazol-2-yl-carbamate (albendazole). Most active were compounds 2-({2-[4-(4-chlorophenyl)piperazin-1-yl]-2-oxoethyl}thio)-1H-benzimidazole 21 and 2-{[2-oxo-2-(4-benzhydrylpiperazin-1-yl)ethyl]thio}-5(6)-methyl-1(H)-benzimidazole 19 as well as 2-({2-[4-(4-chlorophenyl)piperazin-1-yl]-2-oxoethyl}thio)-5(6)-methyl-1(H)-benzimidazole 23 with efficacy of 96.0%, 98.4% and 100%, respectively. The tested derivatives 15-19 and 20-23 were less active against Syphacia obvelata in vivo than albendazole and exhibited the same efficacy as piperazine, but in twice lower concentration.Compounds 2-({2-[4-(4-chlorophenyl)piperazin-1-yl]-2-oxoethyl}thio)-1H-benzimidazole 21, 1,4-bis[(5(6)-methyl-1(H)-benzimidazol-2-ylthio)acetyl]piperazine 17 and 2-({2-[4-(4-chlorophenyl)piperazin-1-yl]-2-oxoethyl}thio)-5(6)-methyl-1(H)-benzimidazole 23 had higher efficacies of 73%, 76%, and 77%, respectively.     

Synthesis and studies on antidepressant and anticonvulsant activities of some 3-(2-furyl)-pyrazoline derivatives

Twelve 1-phenyl-, 1-thiocarbamoyl- and 1-N-substituted thiocarbamoyl-3-(2-furyl)-5-phenyl/(2-furyl)-2-pyrazoline derivatives were synthesized. The chemical structures of the compounds were proved by IR, (1)H NMR, Mass spectrometric data and microanalyses. The antidepressant activities of the compounds were investigated by Porsolt's behavioural despair (forced swimming) test on albino mice. 1-N-Ethylthiocarbamoyl-3-(2-furyl)-5-phenyl-2-pyrazoline (6) and 1-N-allylthiocarbamoyl-3,5-di(2-furyl)-2-pyrazoline (11) reduced 33.80-31.42% duration of immobility times at 10 mg kg(-1) dose level. Anticonvulsant activities of the compounds were determined by maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (metrazol) (scMet.) tests, neurotoxicities were determined by rotarod toxicity test on albino mice. 1,5-Diphenyl-3-(2-furyl)-2-pyrazoline (2), 1-N-allylthiocarbamoyl-3-(2-furyl)-5-phenyl-2-pyrazoline (7), 1-N-allylthiocarbamoyl-3,5-di(2-furyl)-2-pyrazoline (11) and 1-N-phenylthiocarbamoyl-3,5-di(2-furyl)-2-pyrazoline (12) were active at 100-300 mg kg(-1) dose levels. 1-Thiocarbamoyl-3,5-di(2-furyl)-2-pyrazoline (4), 1-N-methylthiocarbamoyl-3,5-di(2-furyl)-2-pyrazoline (9) and 1-N-ethylthiocarbamoyl-3,5-di(2-furyl)-2-pyrazoline (10) were found protective against MES and scMet. at 30-300 mg kg(-1) dose levels.     

酒精代谢酶基因型在日本双生子中的分布

目的为预防酒精相关性疾病发生,调查了酒精代谢酶控制基因在日本双生子中的分布。方法以饱和酚法提取ＤＮＡ,应用限制性片段长度多态性分析技术检测了９２个日本双生子的酒精脱氢酶２（ＡＤＨ２）和乙醛脱氢酶２（ＡＬＤＨ２）基因型,根据基因型差异筛选敏感个体。结果ＡＤＨ２和ＡＬＤＨ２基因分布符合Ｈａｒｄｙｗｅｉｎｂｅｒｇ等式。ＡＤＨ２基因的３种基因型分别是ＡＤＨ２１／ＡＤＨ２１（１．１％）、ＡＤＨ２１／ＡＤＨ２２（４４．６％）和ＡＤＨ２２／ＡＤＨ２２（５４．３％）。ＡＬＤＨ２的基因型分别为ＡＬＤＨ２１／ＡＬＤＨ２１（４１．３％）、ＡＬＤＨ２１／ＡＬＤＨ２２（３９．１％）和ＡＬＤＨ２２／ＡＬＤＨ２２（１９６％）。ＡＤＨ２和ＡＬＤＨ２基因频率分别为０．２５５、０．７４５和０６０９、０３９１。结论异常纯合的ＡＤＨ２基因和纯合的ＡＬＤＨ２基因占优势。个体携有ＡＤＨ２１／ＡＤＨ２２和ＡＬＤＨ２１／ＡＬＤＨ２１、ＡＤＨ２２／ＡＤＨ２２和ＡＬＤＨ２１／ＡＬＤＨ２１者可视为敏感个体。     

Regiospecific synthesis and biological evaluation of spirooxindolopyrrolizidines via [3+2] cycloaddition of azomethine ylide

Reaction of (E)-3-aryl-1-(thiophen-2-yl)prop-2-en-1-ones with azomethine ylide (generated in situ via decarboxylative condensation of isatin with l-proline) in refluxing methanol afforded 1'-(aryl)-2'-(2-thienylcarbonyl)-spiro[3H-indole-3,3'-[3H]pyrrolizin]-2-ones as the sole product in a regiospecific manner. The synthesized compounds have been characterized by their elemental, analytical and spectral studies. The synthesized compounds were screened for their antibacterial and antifungal activities against a spectrum of microbial organisms. These studies proved that compounds 1'-(p-chlorophenyl)-2'-(2-thienylcarbonyl)-spiro[3H-indole-3,3'-[3H]pyrrolizin]-2-one (4b), 1'-(p-fluorophenyl)-2'-(2-thienylcarbonyl)-spiro[3H-indole-3,3'-[3H]pyrrolizin]-2-one (4d) and 1'-(p-methoxyphenyl)-2'-(2-thienylcarbonyl)-spiro[3H-indole-3,3'-[3H]pyrrolizin]-2-one (4h) against Staphylococcus aureus, 1'-(p-chlorophenyl)-2'-(2-thienylcarbonyl)-spiro[3H-indole-3,3'-[3H]pyrrolizin]-2-one (4b), 1'-(p-methylphenyl)-2'-(2-thienylcarbonyl)-spiro[3H-indole-3,3'-[3H]pyrrolizin]-2-one (4c) and 1'-(p-fluorophenyl)-2'-(2-thienylcarbonyl)-spiro[3H-indole-3,3'-[3H]pyrrolizin]-2-one (4d) against Salmonella typhi show maximum inhibition potency at low concentration (6.25?μg/mL) whereas 4d against Candida albicans and 4b and 4d against Rhizopus sp. showed beneficial antifungal activity at minimum concentration.     

Azanonaboranes [(RNH(2))B(8)H(11)NHR] as possible new compounds for use in boron neutron capture therapy

The synthesis and biological in vitro and in vivo activities of possible new compounds for Boron Neutron Capture Therapy (BNCT) are reported. The azanonaboranes of the type [(RNH(2))B(8)H(11)NHR] are water-soluble when hydrophilic groups are introduced. The reaction of B(9)H(13)SMe(2) with primary amines yields azanonaboranes. Five compounds with different numbers of hydroxypropyl groups have been isolated: [(HO(CH(2))(3)NH(2))B(8)H(11)NHCH(3)] (4), [(HO(CH(2))(3)NH(2))B(8)H(11)NH(CH(2))(3)OH] (2), [((HO(CH(2))(3))(2)NH)B(8)H(11)NHCH(3)] (6), [((HO(CH(2))(3))(2)NH)B(8)H(11)NH(CH(2))(3)OCH(3)] (11) and [((HO(CH(2))(3))(2)NH)B(8)H(11)NH(CH(2))(3)OH] (8). In vitro experiments as judged by cloning survival tests showed that two of the synthesised compounds are not toxic. The in vivo experiments were carried out with C3H/He mice bearing SCCVII tumours and C57 mice bearing B16 tumours. Compounds 2 and 6 have no particular affinity to any tissue, but are excluded from the brain.