Screening of agonistic activities against four nuclear receptors in wastewater treatment plants in Japan using a yeast two-hybrid assay

To assess the potential endocrine disruptive effects through multiple nuclear receptors(NRs),especially non-steroidal NRs,in municipal wastewater,we examined the agonistic activities on four NRs(estrogen receptor α,thyroid hormone receptor α,retinoic acid receptor α and retinoid X receptor α) of untreated and treated wastewater from municipal wastewater treatment plants(WWTPs) in Japan using a yeast two-hybrid assay.Investigation of the influent and effluent of seven WWTPs revealed that agonistic activities...     

Estrogen-related receptor disruption of source water and drinking water treatment processes extracts

Environmental chemicals in drinking water can impact human health through nuclear receptors. Additionally, estrogen-related receptors (ERRs) are vulnerable to endocrine-disrupting e ects. To date, however, ERR disruption of drinking water potency has not been reported. We used ERR two-hybrid yeast assay to screen ERR disrupting activities in a drinking water treatment plant (DWTP) located in north China and in source water from a reservoir, focusing on agonistic, antagonistic, and inverse agonistic activity to 4-hydroxytamoxifen (4-OHT). Water treatment processes in the DWTP consisted of pre-chlorination, coagulation, coal and sand filtration, activated carbon filtration, and secondary chlorination processes. Samples were extracted by solid phase extraction. Results showed that ERR antagonistic activities were found in all sample extracts, but agonistic and inverse agonistic activity to 4-OHT was not found. When calibrated with the toxic equivalent of 4-OHT, antagonistic e uent e ects ranged from 3.4 to 33.1 g/L. In the treatment processes, secondary chlorination was e ective in removing ERR antagonists, but the coagulation process led to significantly increased ERR antagonistic activity. The drinking water treatment processes removed 73.5% of ERR antagonists. To our knowledge, the occurrence of ERR disruption activities on source and drinking water in vitro had not been reported previously. It is vital, therefore, to increase our understanding of ERR disrupting activities in drinking water.     

Microfluidic photomechanic infrared receptors in a pyrophilous flat bug

Infrared (IR) receptors are so far known only in boid and crotalid snakes and in three genera of pyrophilous beetles that seek out forest fires. Pyrophilous insects can also be found in other orders, however, so it can be hypothesised that IR receptors also occur in some of these species. We investigated the pyrophilous Australian flat bug Aradus albicornis and found a small number of dome-shaped sensilla (diameter 13 microm) on the prothorax, which have previously not been described. Ultrastructural investigations revealed that the sensilla are characterised by a fluid-filled inner compartment enclosed in a round cuticular shell. The cuticular apparatus is innervated by the dendrite of a ciliary mechanoreceptor, which is fluidically coupled to the inner compartment. Electrophysiological recordings demonstrated that the sensilla respond to brief warming by red laser light or to broadband IR radiation. Depending on the radiation intensity (4.4-549 mW/cm(2) tested, threshold measured as 11.3 mW/cm(2)), first spike latencies varied between 3.4 and 7.5 ms. Thus, our findings demonstrate that A. albicornis most probably possesses photomechanic IR sensilla resembling the metathoracic IR sensilla of buprestid beetles of the genus Melanophila. In the Melanophila sensillum, IR radiation causes thermal expansion of a fluid, which rapidly deforms the dendritic membrane of a mechanosensory cell. The existence of photomechanic IR receptors in both beetles and bugs demonstrates a remarkable convergent evolution towards this particular biophysical transduction mechanism and suggests that it provides selective advantages over other possible solutions.     

Predation and aggressiveness in host plant protection: a generalization using ants from the genus Azteca

In studying the ant genus Azteca, a Neotropical group of arboreal species, we aimed to determine the extent to which the ants use predation and/or aggressiveness to protect their host plants from defoliating insects. We compared a territorially dominant, carton-nester, Azteca chartifex, and three plant-ant species. Azteca alfari and Azteca ovaticeps are associated with the myrmecophyte Cecropia (Cecropiaceae) and their colonies shelter in its hollow branches; whereas Azteca bequaerti is associated with Tococa guianensis (Melastomataceae) and its colonies shelter in leaf pouches situated at the base of the laminas. Whereas A. bequaerti workers react to the vibrations transmitted by the lamina when an alien insect lands on a leaf making it unnecessary for them to patrol their plant, the workers of the three other species rather discover prey by contact. The workers of all four species use a predatory behaviour involving spread-eagling alien insects after recruiting nestmates at short range, and, in some cases, at long range. Because A. alfari and A. ovaticeps discard part of the insects they kill, we deduced that the workers' predatory behaviour and territorial aggressiveness combine in the biotic defence of their host tree.     

Thyroid disruption by technical decabromodiphenyl ether （DE-83R） at low concentrations in Xenopus laevis

Decabromodiphenyl ether (decaBDE), as a flame retardant, is widely produced and used. To study the thyroid disruption by technical decaBDE at low concentrations, Xenopus laevis tadpoles were exposed to technical decaBDE mixture DE-83R (1–1000 ng/L) in water from stage 46/47 (free swimming larvae, system of Nieuwkoop and Faber) to stage 62. DE-83R at concentration of 1000 ng/L significantly delayed the time to metamorphosis (presented by forelimb emergence, FLE). Histological examination showed that DE- 83R at all tested concentrations caused histological alterations – multilayer follicular epithelial cell and markedly increased follicle size accompanied by partial colloid depletion and increase in the peripheral colloid vacuolation, in thyroid glands. All tested concentrations of DE-83R also induced a down-regulation of thyroid receptor mRNA expression. These results demonstrated that technical decaBDE disrupted the thyroid system in X. laevis tadpoles. Analysis of polybrominated diphenyl ethers (PBDEs) (sum of 39 congeners) in X. laevis indicated that mean concentrations of total PBDEs in X. laevis exposed to 1, 10, 100, 1000 ng/L were 11.0, 128.1, 412.1, 1400.2 ng/g wet weight, respectively. Considering that PBDEs burden of X. laevis tadpoles was close to PBDEs levels in amphibians as reported in previous studies, our study has raised new concerns for thyroid disruption in amphibians of technical decaBDE at environmentally relevant concentrations.     

重庆主城区春季大气PM10及PM2.5中多环芳烃来源解析

于2012年春季采集了重庆主城区和缙云山共6个环境采样点的大气PM₁₀、PM_2.5样品,同步采集了燃煤尘、机动车尾气尘、施工机械尾气尘、船舶尾气尘、餐饮油烟尘、生物质燃烧尘及土壤尘等7类污染源,采集到有效受体样品139个、有效源样品233个,使用GC-MS分析样品中18种PAHs的质量浓度(ρ),分析了PM₁₀、PM_2.5上载带PAHs的污染特征,并分别运用比值法、主成分分析法及CMB(化学质量平衡)受体模型法对PM₁₀、PM_2.5中的PAHs进行来源解析,所得源解析结果较为一致. 结果表明:重庆主城区大气PM₁₀、PM_2.5中ρ(PAHs)较低,ρ(PAHs)分别为22.03~31.71、19.02~29.92 ng/m3,其中位于工业区新山村采样点的ρ(PAHs)最高. PM₁₀载带的PAHs有86%~99%集中在PM_2.5中,说明PAHs主要富集在PM_2.5中. 重庆主城区大气PM₁₀、PM_2.5载带的PAHs主要来自机动车尾气尘和燃煤尘的贡献,这2类源对PM₁₀的贡献率分别为25.89%、32.80%;而在PM_2.5中,机动车尾气尘的贡献率较高,可达62%左右.      

Di (2-ethylhesyl)(DEHP)和Monoethylphthalate(MEHP)长期暴露对海洋青鳉(Oryzias melastigma)内分泌干扰效应的评价

为探讨邻苯二甲酸二(2-乙基己)酯(DEHP)和邻苯二甲酸单乙基己基酯(MEHP)长期暴露对海水生物的内分泌干扰效应及机制,将孵化后1周的海洋青鳉(Oryzias melastigma)分别暴露于DEHP(0.1 mg·L^-1和0.5 mg·L^-1)和MEHP(0.1 mg·L^-1和0.5 mg·L^-1)6个月。结果显示：DEHP显著增加了雌性和雄性海洋青鳉的肝指数,而MEHP只在高剂量时显著增加雄性青鳉的肝指数。对于雌性青鳉,DEHP暴露后肝脏雌激素相关基因ERα、ERβ、ERγ、VTG1、VTG2、ChgH和ChgL的表达水平显著上调,而对于雄性青鳉,DEHP暴露后,只有肝脏ERβ的表达水平显著上调。相比之下,MEHP暴露对雌性和雄性青鳉肝VTG和Chg基因表达无显著影响。DEHP激活了雌性和雄性青鳉的肝过氧化物增殖激活受体PPARα和PPARγ,而MEHP只在低剂量时上调了雄性青鳉PPARγ的表达。在雌性和雄性青鳉体内,VTG和Chg的表达与ERα和ERγ的表达显著相关,并且ER与PPAR也显著相关。研究表明,DEHP长期暴露可通过激活肝性激素受体调控肝雌激素响应基因(VTG和Chg)和过氧化物增殖激活受体(PPARα和PPARγ)的表达而对海洋青鳉产生内分泌干扰效应,并且显示出性别特异性。MEHP对海洋青鳉的内分泌干扰效应弱于DEHP。     

Synthesis and pharmacological properties of certain analogs of pilocarpine

The synthesis of 4‐(4'‐pyrimidinylmethyl)oxacyclohexan‐2‐one (2a) and 4‐(4'‐pyrimidinylmethyl)oxacycloheptan‐2‐one (3a) were achieved through the Michael addition of the anion derived from 4‐methylpyrimidine with oxacyclyo‐3‐hexen‐2‐one and oxacyclo‐3‐hepten‐2‐one respectively. These compounds 2a and 3a and their quaternary methiodide salts lack cholinomimetic activity.     

β-肾上腺受体阻滞剂的水生态毒理学研究进展

β-肾上腺受体阻滞剂是一类治疗心血管疾病的药物,其药理作用是和β-肾上腺受体结合但不使其活化。由于此类化合物在环境水体中的高检出率以及自身所具有的生物活性,近年来有关其对非靶生物的生态毒性效应日益受到关注。在概括了β-受体阻滞剂的使用现状及其在水体环境中的归趋后,重点介绍了此类化合物对鱼类以及其他水生生物的毒性效应。最后,针对目前的研究现状对今后的工作做出展望。