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。     

人体血清二噁英化合物检测方法的建立

目的建立人体血清二噁英(polychlorinated dibenzo-p-dioxins and polychlorinated dibenzofurans,PCDD/Fs)化合物测定方法,为开展二噁英人体健康风险评估提供检测技术手段。方法基于国际二噁英的测定方法—同位素稀释的高分辨气相色谱/高分辨质谱联用法,血清样品经C18柱固相萃取、酸性硅胶柱和活性炭柱净化的前处理方法,用DB-5MS毛细管柱(60 m×0.25 mm×0.25μm)分离,高分辨质谱检测分析。结果本方法的检出限为0.35~3.26 pg/g脂肪计,采用血清国际标准参考物质(SRM 1958)进行方法验证,与SRM 1958给出的参考质量分数值范围对比,17个PCDD/Fs单体浓度测定值均在参考质量分数值范围内,相对标准偏差为2%~19%(n=3)。该方法进一步应用于实际人体血清分析,同位素标记的17个二噁英单体回收率为61%~135%。结论本方法灵敏度和准确度高、方法性能稳定,满足人体血清二噁英检测方法的要求。     

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。     

Effects of polychlorinated biphenyls on liver ultrastructure, hepatic monooxygenases, and reproductive success in the barbel

Polychlorinated biphenyls (PCBs) are organochlorinated micropollutants ubiquitously distributed in the environment. They are known to be strong inducers of hepatic monooxygenases in fish. This can adversely affect reproduction by increasing steroid metabolism. In this work, adult barbels were contaminated with food containing Aroclor 1260, a commercial PCB mixture from Monsanto, at environmentally relevant concentrations. A significant increase in cytochrome P450 was observed, and two particularly sensitive enzymes, ethoxyresorufin o-deethylase (EROD) and ethoxycoumarin o-deethylase (ECOD), were strongly induced. Electron microscopy revealed alterations in liver ultrastructure in contaminated fish, principally an increase in the number of cisternae of the rough endoplasmic reticulum, drastic glycogen depletion, dissolution of mitochondrial contents, and appearance of myelin figures. Contamination was also studied in relation to reproductive success in a hatchery. Contaminated males displayed no alteration in milt quality, but PCBs did alter female reproductive parameters. Total mortality of eggs and larvae increased significantly with the level of PCBs in the eggs. The most highly contaminated fish did not even spawn. All the adverse effects recorded here tended to be reversible when the intoxication ended, sometimes after only a 1-year detoxication period.     

Coplanar PCB congeners increase uterine weight and frontal cortical dopamine in the developing rat: implications for developmental neurotoxicity.

We show that developmental exposure of the laboratory rat to the coplanar polychlorinated biphenyl (PCB) congener 3,4,3',4'-tetrachlorobiphenyl (TCB) and the structurally similar congener 3,4,5,3',4'-pentachlorobiphenyl (PtCB) elevates dopamine (DA) concentrations in the prefrontal cortex (PFC). To determine whether these coplanar congeners are estrogenic, and may thus contribute to the elevations in PFC DA, we measured uterine wet weight (UWW) in prepubertal rats exposed to TCB or PtCB. For comparison, additional animals were exposed to either the ortho-substituted congener 2,4,2',4'-tetrachlorobiphenyl (o-TCB) or 3,4,5,3',4',5'-hexachlorobiphenyl (HCB), a coplanar congener highly resistant to metabolism. Both TCB and PtCB increased UWW, but this effect was blocked after exposure to the anti-estrogen ICI 182,780. Neither o-TCB nor HCB altered UWW. These results demonstrate that certain coplanar PCB congeners and/or their metabolites, are estrogenic, and suggest that exposure during critical periods of neuronal development may increase central DA concentrations, and by inference, alter behavior.     

Differential expression of CYP1A, 2B, and 3A genes in the F344 rat following exposure to a polybrominated diphenyl ether mixture or individual components.

Polybrominated diphenyl ethers (PBDEs), used as flame retardants, have been detected in the environment and in mammalian tissues and fluids. Evidence indicates that PBDE mixtures induce CYPs through aryl hydrocarbon receptor (AhR)-dependent and -independent pathways. The present work has investigated the effects of individual components of a commercial PBDE mixture (DE71) on expression of CYP1A1, a biomarker for activation of the AhR (dioxin-like), and CYP2B and CYP3A, biomarkers for activation of the constitutive androstane and pregnanexreceptors (CAR and PXR), respectively, in the rat. Male F344 rats were dosed orally on three consecutive days with either DE71, PBDE components, 2,2',4,4'-tetraBDE (BDE47), 2,2',4,4',5-pentaBDE (BDE99), 2,2',4,4',5,5'-hexaBDE (BDE153), representative polybrominated dibenzofurans (PBDFs) present in DE71, or reference PCBs. Differential expression of target genes was determined in liver 24 h after the last dose. Quantitative PCR analysis indicated up-regulation of CYP1A1 by DE71; however, the response was weak compared to that for dioxin-like PCB126. Individual PBDE components of DE71 up-regulated CYP1A1 only at the highest administered dose (100 micromol/kg/day). Representative PBDFs efficiently up-regulated CYP1A1; therefore, they, along with other PBDFs and polybrominated dibenzodioxins detected in DE71 and individual PBDE components, may be responsible for most, if not all, dioxin-like properties previously observed for PBDEs. Conversely, PBDEs appear capable of up-regulating CYP2B and CYP3A in rats at doses similar to that for non-dioxin-like PCB153. These results indicate that in vivo PBDE-mediated toxicity would be better categorized by AhR-independent mechanisms, rather than the well-characterized AhR-dependent mechanism associated with exposure to dioxin-like chemicals.     

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。     

Highly Chlorinated Toxic Contaminants in Pesticide-Treated Wooden Art Objects

Although the contamination of wooden art objects with pesticides is well known, to the authors' knowledge no attempt has yet been made to investigate the eventual presence of other toxic compounds that have been produced during the degradation of pesticides or that may be present in the technical formulations. Here, the authors report on the presence of polychlorinated biphenyls (PCBs) and polychlorinated terphenyls (PCTs) in scrapings from wooden antique art objects, namely printing blocks, sculptures, and masks. These antiques belong to 2 fine art museums in Belgium—Antwerp's Ethnographic Museum and the Plantin-Moretus Museum. It is documented that these art objects were treated with pesticides in the 1950s. In addition, 2-heptachlorodibenzo-p-dioxin (HpCDD) isomers and octachlorodibenzo-p-dioxin (OCDD) were also identified. The presence of these toxic compounds in these antiques requires a better understanding of safety for the persons (conservators, museum employees, restorers, and visitors) coming in contact with these objects.