手性液晶的研究——Ⅸ．联苯羧酸酯类

合成了文题所述的十三个手性液晶化合物。经元素分析和红外光谱分析确证了其结构，并进行了相态、相变温度和电滞回线的测定，证实其为铁电液晶。     

Effects of individual terphenyls and polychlorinated terphenyls on rat hepatic microsomal cytochrome P-450-dependent monooxygenases: structure-activity relationships

The effects of o-, m- and p-terphenyl, 2,4-dichloro-, 2,4,6-trichloro-, 2,3,5,6-tetrachloro-, 2,3,4,6-tetrachloro-, 2,4,4'",6- tetrachloro- and 2,3,4,5-tetrachloro-p-terphenyl, 2,3,4,5-tetrachloro-m- and o-terphenyl as inducers of hepatic drug-metabolizing enzymes were determined in immature male Wistar rats. o-Terphenyl, 2,4-dichloro-, 2,4,6-trichloro-p-terphenyl and 2,3,4,5-tetrachloro-o-terphenyl induced 4,4-dimethylamino antipyrine N-demethylase at total dose levels of 300 mol/kg and the 2,3,4,5-tetrachloro-p-terphenyl induced ethoxyresorufin O-deethylase (EROD). In contrast, none of the other terphenyls or polychlorinated terphenyls (PCTs) induced these enzyme activities. Previous studies have demonstrated that 2,3,4,5-tetrachloro-p-terphenyl did not exhibit a high affinity for the 2,3,7,8-tetrachlorodibenzo-p-trachlorodibenzo-p-dioxin (TCDD) receptor protein (EC₅₀= 6.6×10^–6M). In contrast, this study showed that 2,3,4,5-tetrachloro-p-terphenyl was more active than either 2,3,4,5-tetrachloro-o- or m-terphenyl as an inducer of EROD. Moreover, the competitive receptor binding EC₅₀ values for the latter two isomers were > 10^–5 M and this result was also consistent with their lack of EROD induction activity. Previous studies showed that analysis of the data for a series of 4-substituted-2,3,4,5-tetrachlorobiphenyls indicated that the p-terphenyl structural moiety (i.e. 4-substituent = phenyl) did not interact with high affinity with the receptor protein binding site. Since the 2,3,4,5-tetrachloro o- and m-terphenyls are also poor ligands for the receptor protein, this data and results from other studies indicate that PCT congeners (and commercial mixtures) are therefore unlikely to elicit significant 2,3,7,8-TCDD-like biologic or toxic effects in target species.     

Are video display terminals a source of increased PCB concentration in the working atmosphere?

Summary In response to the question: Are datascreen terminals a source of increased PCB concentrations in the working atmosphere? a study of PCB emissions from video display terminals (VDT) was undertaken. Emissions of 2.4 to 8.1 ng PCB/h were observed from VDT located in a building (1) where the mean PCB level in the air was 46 ng PCB/m³ during the test period, whereas no PCB emissions were detected from VDT located in a building (2) where no PCB could be detected in the ambient air. However, both the air and the VDT from building 2 were found to be contaminated with polycyclic aromatic hydrocarbons. We conclude that the observed PCB emissions from VDT are the result of the vapourization of PCB deposited onto the VDT from the PCB contaminated air and do not originate from the electrical components of the VDT.     

科素亚与卡托普利治疗高血压的对比研究

目的 :对比、观察科素亚在治疗高血压中的临床疗效及不良反应。方法 :将 3 0例轻、中度高血压病人随机分为科素亚 L组及卡托普利 C组。在治疗前、后观察血压变化及不良反应并记录之。结果 :1科素亚组在治疗后 SBP下降 1 .3 3～ 2 k Pa(P<0 .0 5 ) ,DBP下降 0 .67k Pa(P>0 .0 5 )。 2科素亚组起效时间在用药后 1 0～ 1 4d,卡托普利组在治疗后 5～ 7d起效。3科素亚组未见不良反应 ,卡托普利组有 3例出现不良反应。结论 :科素亚对于轻、中度高血压有肯定的降压效果 (尤其 SBP) ;降压作用较为平和、缓慢 ,适合老年人使用 ;不良反应少 ,是一安全有效的药物。     

Body burden of polychlorinated biphenyls among persons employed in capacitor manufacturing

Summary In an effort to assess exposure among workers engaged in capitor manufacture, PCB concentration was determined in plasma (290) and adipose tissue (61). In general, males had higher concentrations of PCBs than females.The correlation of plasma concentration (1–546 ppb) of the more highly chlorinated PCBs, which had been used in the past, with total duration of employment suggested accumulation over time. The gc-ec pattern of these PCB peaks was, in most cases, characteristic of exposure to a PCB mixture with 54% chlorine.The less highly chlorinated PCBs, di-, tri-, and tetrachlorobiphenyls, were the source of current exposure, and were observed in concentrations of 6–2530 ppb in plasma. Higher exposure occurred among persons with direct contact with PCBs, in jobs such as capacitor filling.Adipose tissue concentrations, for both the more highly chlorinated PCBs (1–165 ppm) and lower chlorinated PCBs (0.6-414 ppm), were proportional to those in plasma.Abbreviations PCB polychlorinated biphenyl - p,p-DDE 2,2-bis-(4-chlorophenyl)-1,1-dich-loroethylene - DDT dichlorodiphenyltrichloroethane Presented in part, at the XIX. International Congress on Occupational Health, Dubrovnik, September, 1978     

司帕沙星、联苯乙酸对大鼠海马神经元GABA-A和离子型谷氨酸受体的作用(英文)

目的 :观察司帕沙星单用和与联苯乙酸合用时 ,对γ 氨基丁酸 (GABA) ,NMDA ,AMPA和海人藻酸诱导电流的作用。方法 :应用全细胞式膜片钳技术在急性打散的新生大鼠海马锥体神经元上记录GABA ,NMDA ,AMPA和海人藻酸的诱导电流。结果 :司帕沙星 1mmol·L- 1对GABA诱导的电流有迅速可逆的抑制作用 ,抑制率为 (4 7.6±s2 .9) % ,而联苯乙酸 10 μmol·L- 1无抑制作用。但联苯乙酸 (10 μmol·L- 1)与司帕沙星 1mmol·L- 1合用时 ,稍稍增强抑制作用 ,司帕沙星单用或合用联苯乙酸 (10 μmol·L- 1)对GABA诱导电流的IC50 分别为 (2 38± 2 1) μmol·L- 1和 (89± 5 ) μmol·L- 1。司帕沙星、联苯乙酸或司帕沙星合用联苯乙酸对NM DA ,AMPA和海人藻酸诱导的电流无明显作用。结论 :提示司帕沙星 ,或与联苯乙酸合用时所产生的中枢神经毒性可能与抑制GABA诱导的电流有关 ,而与NMDA ,AMPA和海人藻酸诱导的电流无关。     

TCDD and PCBs inhibit breast cancer cell proliferation in vitro

The effects on cell proliferation of arylhydrocarbon receptor (AhR) agonists in estrogen-responsive T47D and ZR-75-1 cells were investigated. 2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD) and the non-ortho-substituted polychlorinated biphenyl (PCB) congeners, PCB 77, PCB 81, PCB 126, and PCB 169 each inhibited 17β-estradiol (E₂)-stimulated cell proliferation in a dose–responsive manner. In the absence of added E₂, TCDD, PCB 77, PCB 81, and PCB 169 had no significant effect on cell proliferation, while PCB 126 at high concentrations caused slight elevations. The order of effective inhibition of E₂-stimulated cell proliferation by the PCB congeners was: PCB 81>PCB 126PCB 169>PCB 77. In the comparative literature, mammalian TEFs for these congeners toxic potency are in the order: PCB 126>PCB 169>PCB 81PCB 77 [Organohalogen Compd. 34 (1997) 237]. Our results thus show an unexpected different pattern for the inhibitory effects of PCBs congeners on E₂-mediated cell proliferation.     

新生期大鼠化学物暴露对睾丸DNA甲基化及精子生成的影响

目的 通过新生期大鼠暴露DNA甲基转移酶抑制剂(5-Aza-CdR)、镉(Cd)和多氯联苯153(PCB153),探讨化学物新生期暴露对SD大鼠睾丸DNA甲基化变化、细胞凋亡和精子生成的影响.方法 将出生3 d(postnatal day 3,PND3)SD大鼠随机分组,每组24只动物.经口给予溶剂对照5-Aza-CdR(0.025、0.250mg/kg)、PCB153(0.025、0.250、2.500mg/kg)和Cd(1、2、4mg/kg),连续暴露5 d.最后1次暴露24 h后,解剖每组的一半动物,剩余动物在无暴露条件下继续喂养至12周龄(成鼠)解剖.检测睾丸细胞凋亡和DNA甲基化水平.结果 与对照组比较,新生期大鼠5-Aza-CdR、PCB153和Cd暴露后,在12周龄时精子计数均呈下降趋势,差异有统计学意义(P<0.05).新生期化学物暴露后,与对照组相比,基因组整体DNA甲基化水平降低,新生期细胞凋亡上升,差异均有统计学意义(P<0.05). 5-Aza-CdR使p53启动子区BstUI位点甲基化水平下降,p53基因表达上调,提示p53通路可能是DNA甲基化诱导细胞凋亡的通路之一.新生期大鼠Cd暴露可诱导整体DNA甲基化变化,细胞凋亡增加,与对照组比较,差异有统计学意义(P<0.05),但p53 mRNA表达及p53启动子区BstUI位点甲基化水平和对照组相比,差异无统计学有意义(P>0.05),提示Cd暴露诱导的细胞凋亡可能是非p53通路依赖的.PCB153的体内暴露未发现基因组整体甲基化和细胞凋亡的明显变化.结论 新生期化学物体内暴露可诱导成年精子形成障碍.DNA甲基化异常和细胞凋亡可能是其中的机制之一.     

五灵丸、五味子丸和联苯双酯治疗慢性乙型肝炎的疗效比较

作者比较了五灵丸、五味子丸和联苯双酯治疗慢性乙型肝炎的疗效.结果五灵丸对乏力、纳差的显效率显著高于五味子丸(93.8％,84.3％对40.0％,30.0％,P<0.05);对体征的改善五灵丸组治后的无效例次(4例次)明显少于另两组的14例次.实验检测示五灵丸降S-GPT,S-GOT至正常的百分率显著高于五味子丸组(90.6％,87.5％对36.6％,23.5％,P<0.05);在降S-GOT方面五灵丸还优于联苯双酯(87.5％对26.3％P<0.05).对于血清白蛋白五灵丸治后与治前比有显著提高(t=2.57,P<0.05),而另药无此差异.对黄疸指数的消退五灵丸也优于联苯双酯(t=2.67,P<0.05).提示五灵丸治疗慢性肝炎优于五味子丸和联苯双酯.