Effects of ellagic acid on arylamine N‐acetyltransferase activity in human colon tumor cells

The inhibition of arylamine N‐acetyltransferase (NAT) activity by ellagic acid was determined in a human colon tumor (adenocarcinoma) cell line. Two assay systems were performed, one with cellular cytosols (9000g supernatant), the other with intact colon tumor cell suspensions. The NAT activity in a human colon tumor cell line was inhibited by ellagic acid in a dose‐dependent manner in both types of examined systems: i.e. the greater the concentration of ellagic acid in the reaction, the greater the inhibition of NAT activities in both systems. The data also indicated that ellagic acid decreased the apparent K _m and V _max of NAT enzymes from human colon tumor cells in both the systems examined. This report is the first demonstration which showed ellagic acid affect human colon tumor cell NAT activity.     

Alkylation of metals and the activity of metal‐alkyls†

The biochemical basis for resistance to metal ion toxicity is emerging though it is complicated by the different resistance mechanisms. Several strategies for resistance to toxic metal ions have been identified:

1. The development of energy driven efflux pumps which keep toxic element levels low in the interior of the cell. Such mechanisms have been described for Cd(II) and As(V).

2. Oxidation (e.g. AsO^2‐ to AsO₄ ^3‐) or reduction (e.g. Hg²⁺ to Hg⁰) can enzymatically and intracellularly convert a more toxic form of an element to a less toxic form.

3. The biosynthesis of intracellular polymers which serve as traps for the removal of metal ions from solution such as traps have been described for cadmium, calcium, nickel and copper.

4. The binding of metal ions to cell surfaces.

5. The precipitation of insoluble metal complexes (e.g. metal sulfides and metal oxides) at cell surfaces.

6. Biomethylation and transport through cell‐membranes by diffusion controlled processes.

In this short review I shall discuss the implications of biomethylation as a detoxification mechanism for microorganisms as well as for certain higher organisms.     

Effects of cucl2 on UV‐mutagenesis and on DNA damage in a restriction fragment of E. Coli gpt∗

CuCl₂ does not cause Trp⁺ reversion in E. coli WP2. However, when the bacteria are exposed to CuCl₂ and UV‐irradiated, a greater than 3‐fold enhancement of mutagenesis (compared to UV alone) is seen at 30 μMCuCl₂, and significant enhancement is seen even at 3 μM. The mechanism for this comutagenic effect was studied using a restriction fragment of the E. coli gpt gene. Whereas UV or CuCl₂ alone caused few strand breaks, UV + CuCl₂ induced breaks at every site. This reaction was blocked by KI, a free radical scavenger. While UV alone induced alkali‐labile sites, UV+ CuCl₂ induced many more such sites and altered the sequence specificity. We suggest that at least some of the comutagenic effect might be due to hydroxyl radical formed via a Fenton reaction.     

Investigation of the hemolytic effects of various organophosphoric acid triesters (OPEs) and their structure‐activity relationship

The hemolytic effects of various organophosphonc acid triesters (OPEs) were investigated and they showed strong hemolyic toxicity except triethyl phosphate and tris(chloroethyl)phosphate. 2‐Ethylhexyl diphenyl phosphate (EHDP) showed the strongest toxicity. By quantitative structure‐activity relationship (QSAR) study, one‐parameter regression equation to estimate hemolysis was not obtained. But, two‐parameter regression equations were obtained which were enought to estimate EC₅₀ and EC₂₀. The correlation coefficients with the two‐parameter regression equations were 0.939 for log(l/EC₅₀) and 0.946 for log(l/EC₂₀).     

The synergistic effects of increasing temperature and CO2 levels on activity capacity and acid–base balance in the spider crab, Hyas araneus

With global climate change, ocean warming and acidification occur concomitantly. In this study, we tested the hypothesis that increasing CO₂ levels affect the acid–base balance and reduce the activity capacity of the Arctic spider crab Hyas araneus, especially at the limits of thermal tolerance. Crabs were acclimated to projected oceanic CO₂ levels for 12 days (today: 380, towards the year 2100: 750 and 1,120 and beyond: 3,000 μatm) and at two temperatures (1 and 4 °C). Effects of these treatments on the righting response (RR) were determined (1) at acclimation temperatures followed by (2) righting when exposed to an additional acute (15 min) heat stress at 12 °C. Prior to (resting) and after the consecutive stresses of combined righting activity and heat exposure, acid–base status and lactate contents were measured in the haemolymph. Under resting conditions, CO₂ caused a decrease in haemolymph pH and an increase in oxygen partial pressure. Despite some buffering via an accumulation of bicarbonate, the extracellular acidosis remained uncompensated at 1 °C, a trend exacerbated when animals were acclimated to 4 °C. The additional combined exposure to activity and heat had only a slight effect on blood gas and acid–base status. Righting activity in all crabs incubated at 1 and 4 °C was unaffected by elevated CO₂ levels or acute heat stress but was significantly reduced when both stressors acted synergistically. This impact was much stronger in the group acclimated at 1 °C where some individuals acclimated to high CO₂ levels stopped responding. Lactate only accumulated in the haemolymph after combined righting and heat stress. In the group acclimated to 1 °C, lactate content was highest under normocapnia and lowest at the highest CO₂ level in line with the finding that RR was largely reduced. In crabs acclimated to 4 °C, the RR was less affected by CO₂ such that activity caused lactate to increase with rising CO₂ levels. In line with the concept of oxygen and capacity limited thermal tolerance, all animals exposed to temperature extremes displayed a reduction in scope for performance, a trend exacerbated by increasing CO₂ levels. Additionally, the differences seen between cold- and warm-acclimated H. araneus after heat stress indicate that a small shift to higher acclimation temperatures also alleviates the response to temperature extremes, indicating a shift in the thermal tolerance window which reduces susceptibility to additional CO₂ exposure.     

Synthesis and antithyroid activity of 6‐n‐propyl‐5‐arylazo‐2‐thiouracils †

The synthesis of several 6‐n‐propyl‐5‐arylazo‐2‐thiouracil derivatives was achieved. The antithyroid activity of these derivatives has been determined using iodine‐125‐thiocyanate discharge technique in rats, and 6‐n‐propyl‐2‐thiouracil (PTU) as a standard. None of the 5‐arylazo‐2‐thiouracil analogs showed antithyroid activity as compared to PTU. The structure‐activity relationships (SAR) of position 5 in the PTU molecule and the requirements for better binding to the proposed receptor are discussed.     

Study of the levels of N‐methylcarbamate pesticides in waters of the river Huelva

A study on the levels of N‐methylcarbamate pesticides and some degradation products in waters of the river Huelva was carried out. This river constitutes the main water supply of the city of Seville at the south west of Spain with a population of almost one million inhabitants. N‐methylcarbamates were extracted from the water by using C‐18 solid phase cartridges. High performance liquid chromatography with UV detection was used to carry out the determinations. Residues of carbaryl, methiocarb sulphoxide and α‐naphthol were found in some of the analysed water samples.     

Effects of different concentrations of tetracycline and oxytetracycline on the growth and ecotoxicity in lettuce北大核心CSCD

四环素类抗生素(TCs)是目前我国应用广泛、用量最大的一类抗生素,畜禽粪便和土壤中存在TCs残留,影响蔬菜作物的生长发育. TCs因水溶性较高更容易被植物转运和积累,植物对TCs耐受性机理研究仍不足.为更全面探究土壤TCs对蔬菜的毒性作用,研究不同浓度四环素(TC)和土霉素(OTC)分别对生菜的抗生素残留、生长特征及抗氧化酶系统的影响.结果显示,在0(对照)、2、10、50、250 mg/kg 5个施用水平下,生菜叶片抗生素含量逐渐增加,且土霉素含量始终大于四环素含量.与对照相比,抗生素浓度在50 mg/kg以上时对生菜生长具有显著抑制作用,其中,株高、根长、地上部和地下部鲜重与叶片TC残留量具显著负相关.生菜叶片的脯氨酸含量随浓度增加呈先增加后降低的趋势,在10 mg/kg时达到最大.并且低浓度(2 mg/kg)促进抗氧化酶基因SOD、POD21和CAT的表达,高浓度抗生素(50、250 mg/kg)对其产生抑制作用,10 mg/kg的抗生素处理对SOD、POD21和CAT基因表达的影响在抗生素种类上存在差异.本研究表明抗生素浓度超过50 mg/kg对生菜生长产生抑制作用,脯氨酸和抗氧化酶SOD、POD、CAT的转录水平及其酶活性能快速响应抗生素胁迫,可作为生菜对抗生素抗性的辅助评价指标.(图8表3参19)     

Effects of lead and selected pyrethroids/piperonyl butoxide alone and in combination on Na,K‐ATPase

In vitro effects of Pb²⁺, the pyrethroid insecticides cypermethrin, fenvalerate and the syner‐gist piperonyl butoxide on sodium‐potassium‐activated adenosine triphosphatase (Na,K‐ATPase) from dog kidney were determined. Pb²⁺ with an estimated IC50 value of 5.2 μM was found to be a potent inhibitor of Na,K‐ATPase activity, whereas Na,K‐ATPase was less sensitive to the pyrethroids tested and piperonyl butoxide. Investigation with circular dichroism (CD) spec‐troscopy showed that inhibition occurs through conformational changes of the α‐subunit of the enzyme. The kinetic characteristics of inhibition of Na,K‐ATPase with varying substrate (ATP) concentrations as well as with varying Na⁺ concentrations exhibited a competitive type of inhibition with Pb²⁺ in the μM range. With Pb²⁺ alone in the enzyme assay no conformational changes of the protein could be observed which confirmed the assumption that Pb²⁺ can bind to the Na⁺ binding site of the α‐subunit. Uncompetitive type of inhibition occurred with varied K⁺ concentrations demonstrating that this cation binding site is not affected directly by Pb²⁺.

Complete reversal of Pb²⁺ by DTT confirms that a possible target for interaction of this heavy metal ion with Na, K‐ATPase are specific SH groups.

Synergistic effects could only be determined with higher Pb²⁺ concentrations of 3, 5 and 7 μM plus piperonyl butoxide while all other combinations with this heavy metal plus organic substances where of the additive type. With CD spectroscopy also only additive effects were observed. These results demonstrate that higher concentrations of piperonyl butoxide favor the binding of Pb²⁺ to the Na⁺ binding site by conformational changes of the protein.     

The use of the embryo‐culture techniques in the research on the Teratogenic and Mutagenic properties of metals†

Actually, embryos can be cultured from the one‐cell stage up to the blastocyst stage, and their development can be easily monitored at any time: severe effects caused by toxic compounds are traduced by rapid embryonic death, less pronounced effects can be expressed by a lowered cleavage activity or by an arrest of the development from a particular stage. The system can be improved by transferring the embryos at the blastocyst stage in another more complete medium where they can “implant”; and form an inner cell mass with differentiated ectoderm and endoderm. Since last years, it has also become possible to culture postimplantation rodent embryos for short periods involving a number of particularly critical stages of organogenesis, such as the formation and closure of the anterior neuropore. Embryo‐culture also represents a useful system to study cytogenetic effects of chemicals which are often linked to lethal or teratogenic effects. These different possibilities are illustrated by examples of studies already performed with metals, and dealing with their teratogenic and/or cytogenetic effects on pre‐ and postimplantation rodents.     

Cross‐sectional epidemiological study on the lead burden of children and workers in Greece

Exposure of the general population to lead in the environment is mainly caused by motor traffic exhaust and by industrial pollution. The aim of the study in Greece was to assess lead exposure in children living in point source impacted areas (Lavrion and Aspropyrgos‐Eleusis) using the biological monitoring parameter “blood lead concentration”;.

In addition, workers of a lead smelter, a battery plant and an oil refinery were investigated in these areas at the same time.

Five hundred and thirty‐four children and 105 workers took part in this investigation.

The highest blood lead levels (mean: 24.16 μg/100ml; range: 10.40–60.49 μg/100 ml) were found in children living in a 500m‐area around the lead smelter at Lavrion. Blood lead decreases corresponded to the increasing distance from the emitter. Nevertheless the values of children living in a 1500 m distance to the smelter are significantly higher than those of children living next to other kinds of industrial lead sources.

The mean values of the children living in the two industrial towns were manifold higher than those of the control group.

The blood lead levels of the investigated workers did not exceed the German BAT‐value (Biologischer Arbeitsstoff‐Toleranzwert) of 70 μg/100ml.     

Transport of metanil yellow in the rat plasma and interaction of its metabolite,p‐aminodiphenylamine with serum proteins

Binding affinity of metanil yellow and its breakdown product p‐aminodiphenylamine to serum proteins has been studied employing chromatographic separation on Sephadex G‐200 and by paper and polyacrylamide gel electrophoresis. Metanil yellow has more affinity towards albumin than to globulins. The complexing is presumably through electrostatic forces. p‐Aminodiphenylamine on the other hand, preferably binds to globulin fractions of serum protein. However, a stable binding with BSA alone was also observed. The binding was quite stable and was accompanied by a shift in absorbance from 430 nm to 500 nm. Aspartic acid moiety of protein was found to be one of the units involved in the binding of p‐ADPA to proteins.     

Paeonol promotes arylamine N‐acetyltransferase activity in human bladder tumor cells

Paeonol was used to determine effects of arylamine N‐acetyltransferase (NAT) activity in human bladder tumor cells. The NAT activity was measured by high performance liquid chromatography assaying for the amounts of N‐acetyl‐2‐aminofluorene (2‐AAF) and N‐acetyl‐p‐amino‐benzoic acid (N‐Ac‐PABA) and remaining 2‐aminofluorene (2‐AF) and p‐aminobenzoic acid (PABA). The NAT activity in human bladder tumor cells was promoted by paeonol in a dose‐dependent manner, i.e. the higher the concentration of paeonol, the higher the promotion of NAT activity. The data also indicated that paeonol increases the apparent values of K_m and K_max from human bladder tumor cells in cytosols and intact cells. This report is the first demonstration to show paeonol did promote human bladder tumor cell NAT activity.     

Effects of β-cyclodextrin on adsorption and desorption of carbofuran in soils of divergent texture

Laboratory studies were conducted to determine the adsorption/desorption equilibrium of carbofuran between four divergently textured soils and distilled water and an aqueous solution of 0.01?mol?L^?1 β-cyclodextrin using a batch equilibrium technique. The determined adsorption isotherms for silt loam soils were of L-shaped, for sandy loam soil S-shaped, in agreement with a Freundlich isotherm. In the presence of β-cyclodextrin, the adsorption of carbofuran to the four soils was lower than with distilled water. Positive hysteresis was observed in all soils with distilled water, negative hysteresis when using a solution of β-cyclodextrin as desorbent. The results indicate the potential use of β-cyclodextrin for remediation of pesticide-contaminated soils.     

Effects of glucose dehydrogenase gene knock-out in Acetobacter sp. On the metabolism of carbon sources and the synthesis of 3-hydroxypropionic acid北大核心CSCD

3-Hydroxypropionic acid (3-HP) is an emerging platform chemical with a high added-value. Resting cells of Acetobacter sp. can efficiently catalyze 1,3-propanediol (1,3-PDO) to 3-HP. Glucose is oxidized by the membrane-bound dehydrogenase, resulting in an acidic environment that inhibits cell growth and reduces the biomass. We deleted the gdh gene for glucose dehydrogenase (GDH), and investigated the effects on cell growth, carbon metabolism, and 3-HP production. The gdh gene knocked-out showed a 1.72-fold increase in biomass in the mixed medium containing glucose and glycerol. A carbon flux analysis showed that glucose was converted to gluconic acid by GDH, followed by an oxidation to 2-ketogluconic acid. In addition, a small percentage of the gluconic acid was degraded via the pentose phosphate pathway. Glycerol was phosphorylated and entered the central pathway (gluconeogenesis). Results indicate that the deletion of gdh can effectively promote higher cell densities and improve the catalytic performance for the production of 3-HP, and thus provide a theoretical reference for improving the carbon source utilization and the catalytic performance of acetic acid bacteria. © 2018 Science Press. All rights reserved.     

Study on polychlorinated dibenzo‐p‐dioxins and dibenzofurans in rivers and estuaries in Osaka Bay in Japan

In order to search the source of polychlorinated dibenzo‐p‐dioxins (PCDDs) and dibenzofurans (PCDFs) in blue mussel in Osaka bay, sediments from Osaka bay and from rivers running near an urban municipal incinerator were analysed for PCDDs, PCDFs and PCBs. The river and estuary sediments were all found to be contaminated with PCDDs at average levels of 9.8 and 12ppb on the dry basis, PCDFs of 7.8 and 5.1 ppb, and PCBs of 1600 and 1300ppb, respectively. The two sediments contained similar profiles of specific isomers and congeners of PCDDs and PCDFs with each other. In addition, there was observed positive close correlations between PCDD and PCDF levels in the two specimens as well as fly ash from urban municipal incinerators. These allow the conclusion that the main source of the two chemicals in Osaka bay is fly ash from waste incineration.     

Effects of citric acid on Cu（Ⅱ） and Cd（ Ⅱ ） adsorption ＆ desorption in calcareous cinnamon soil

通过室内培养和吸附-解吸实验,研究了不同柠檬酸含量土壤对Cu2＋、Cd2＋吸附-解吸的影响.结果表明,土壤对Cu2＋的吸附量随加入柠檬酸量的增加而明显增加,达到峰值后（柠檬酸含量为0.5 mmol.kg-1）,吸附量随柠檬酸含量的增加而下降,即Cu2＋的吸附曲线呈峰型.在低柠檬酸含量时,土壤对Cu2＋的吸附量受Cd2＋浓度影响较小,但随柠檬酸含量的增加,在低铜浓度处理（Cu2＋浓度为600 mg·L-1,Cu600）下,土壤对Cu2＋的吸附量随Cd2＋浓度的增大而增大,但在高浓度铜处理（Cu2＋浓度为1000 mg·L-1,Cu1000）下,土壤对Cu2＋的吸附量随Cd2＋浓度的增加而减少.Cu2＋的解吸量随柠檬酸含量的增加而总体上降低;相同柠檬酸含量下,Cu600处理下,Cd2＋浓度为10 mg·L-1（Cd10）条件下Cu2＋解吸量明显低于无Cd2＋（Cd0）和Cd2＋浓度为1 mg·L-1（Cd1）条件下.而Cu1000处理下,Cd2＋的浓度对Cu2＋解吸量的影响较小.Cd2＋吸附量随柠檬酸含量的增加无明显变化,但随Cu2＋浓度的增加下降明显,其中无Cu2＋处理Cd2＋吸附量极显著地高于Cu600和Cu1000处理,而Cu600和Cu1000处理间差异不显著,且土壤对Cd2＋的吸附随镉添加量增加而增加;Cd2＋的解吸量随柠檬酸含量的增加先增大后保持稳定,在柠檬酸含量为0.5 mmol.kg-1时达到最大,Cu600处理的Cd2＋的解吸量显著地高于Cu1000处理.     

Effects of climate change and anthropogenic activity on ranges of vertebrate species endemic to the Qinghai–Tibet Plateau over 40 years

Over the past 40 years, the climate has been changing and human disturbance has increased in the vast Qinghai–Tibet Plateau (QTP). These 2 factors are expected to affect the distribution of a large number of endemic vertebrate species. However, quantitative relationships between range shifts and climate change and human disturbance of these species in the QTP have rarely been evaluated. We used occurrence records of 19 terrestrial vertebrate species (birds, mammals, amphibians, and reptiles) occurring in the QTP from 1980 to 2020 to quantify the effects of climate change and anthropogenic impacts on the distribution of these 4 taxonomic groups and estimated species range changes in each species. The trend in distribution changes differed among the taxonomic groups, although, generally, ranges shifted to central QTP. Climate change contributed more to range variation than human disturbance (the sum of the 4 climatic variables contributed more than the sum of the 4 human disturbance variables for all 4 taxonomic groups). Suitable geographic range increased for most mammals, amphibians, and reptiles (+27.6%, +18.4%, and +27.8% on average, respectively), whereas for birds range decreased on average by 0.9%. Quantitative evidence for climate change and human disturbance associations with range changes for endemic vertebrate species in the QTP can provide useful insights into biodiversity conservation under changing environments.     

Effect of Florasulam on soil residues and enzyme activity of wheat in drylands北大核心CSCD

Florasulam is a three azole and pyrimidine sulfonamide herbicide, mainly used for weeds prevention and control in winter wheat fields. The main purpose of this experiment was to study the effects of different doses of Florasulam on soil residues and on the enzymatic activity of wheat cultivated in drylands, and to provide the theoretical basis for a scientific use of florasulam. Five doses (0, 15, 30, 45, and 60 mL/667 m2) of Florasulam were applied in order to detect differences in soil residue content and enzymatic activities. Soil residues and enzymatic activities (catalase, phosphatase, urease, dehydrogenase) were measured and analyzed after the 5 different doses of Florasulam were processed. The residual amount of Florasulam in the soils decreased gradually with the growth phase of wheat, and was lower than that of 0.01 mg/kg. The residual amount of Florasulam in different soil layers gradually decreased with the increase of soil thickness. The enzymatic activity of soils treated with Florasulam was basically T3 > T2 > T1 > CK > T4, where T3 was the highest, whereas T4 could inhibit the enzymatic activity. Under these experimental conditions, in order to decrease soil pollution and lower Florasulam residues, it is recommended to apply Florasulam at a concentration range of 30 to 45 mL/667 m2 © 2018 Science Press. All rights reserved.