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The effect of trichlorfon and other organophosphates on prenatal brain development in the guinea pig
The organophosphates trichlorfon, dichlorvos, dimethoate, soman, triortho-cresyl phosphate (TOCP), and the diethoxy-analogue of trichlorfon (O,O-diethyl 2,2,2-trichloro-1-hydroxyethylphosphonate, ethyl-trichlorfon), were administrated to guinea pigs between day 42 and 46 of gestation. When the offsprings were examined at birth, there was a severe reduction in brain weight in the case of trichlorfon and dichlorvos, but not after treatment with the other organophosphates. The reduction in weight was most pronounced for cerebellum, medulla oblongata, thalamus/hypothalamus and quadrigemina. The effect was less marked for cerebral cortex and hippocampus. Since soman, a potent anticholinesterase, and TOCP, an inhibitor of neuropathy target esterase, did not show any effects, this excludes that the brain hypoplasia can be caused by inhibition of these two enzymes. Further, the lack of effect with ethyl-trichlorfon has shed some light on the part of the trichlorfon molecule which could be involved in the formation of the hypoplasia. It is suggested that alkylation of DNA may be involved in the development of the lesion. The possible consequences for a teratogenic effect of trichlorfon and dichlorvos on humans are discussed.Special issue dedicated to Dr. Bernard W. Agranoff. 相似文献
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D. Christopher Braddock Jared S. Marklew Kevin M. Foote Andrew J. P. White 《Chirality》2013,25(11):692-700
Dimethylaluminum triflate‐mediated activation of tetrafluorobenzoates of enantiomerically pure bromohydrins results in enantiospecific polyene cyclizations. The initiation of cyclization by enantiomerically pure bromonium ions and subsequent propagation is not subject to catastrophic erosion of enantiomeric purity by any intramolecular or intermolecular bromonium ion‐to‐alkene transfer. Chirality 25:692–700, 2013. © 2013 Wiley Periodicals, Inc. 相似文献
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8‐Prenylnaringenin (8PN) is a naturally occurring bioactive chiral prenylflavonoid found most commonly in the female flowers of hops (Humulus lupulus L.). A stereospecific method of analysis for 8PN in biological fluids is necessary to study the pharmacokinetic disposition of each enantiomer. A novel and simple liquid chromatographic‐electrospray ionization‐mass spectrometry (LC‐ESI‐MS) method was developed for the simultaneous determination of R‐ and S‐8PN in rat serum and urine. Carbamazepine was used as the internal standard (IS). Enantiomeric resolution of 8PN was achieved on a Chiralpak® AD‐RH column with an isocratic mobile phase consisting of 2‐propanol and 10 mM ammonium formate (pH 8.5) (40:60, v/v) and a flow rate of 0.7 mL/min. Detection was achieved using negative selective ion monitoring (SIM) of 8PN at m/z 339.15 for both enantiomers and positive SIM m/z at 237.15 for the IS. The calibration curves for urine were linear over a range of 0.01–75 µg/mL and 0.05–75 µg/mL for serum with a limit of quantification of 0.05 µg/mL in serum and 0.01 µg/mL in urine. The method was successfully validated showing that it was sensitive, reproducible, and accurate for enantiospecific quantification of 8PN in biological matrices. The assay was successfully applied to a preliminary study of 8PN enantiomers in rat. Chirality 26:419–426, 2014. © 2014 Wiley Periodicals, Inc. 相似文献
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Marc‐André Dubois Alain Grandbois Shawn K. Collins Andreea R. Schmitzer 《Journal of molecular recognition : JMR》2011,24(2):288-294
Dimerization of a hydroxycarbazole produces an axially chiral biaryl, BICOL ( 2 ). One enantiomer (R)‐ 2 , is capable of enantioselective binding to different polymorphs of DNA. The biaryl (R)‐ 2 was shown by fluorescence and circular dichroism to induce a shift of Z‐DNA to B‐DNA. The opposite enantiomer (S)‐ 2 shows no specific binding. The significant difference in behaviour between the two enantiomers (S)‐ 2 and (R)‐ 2 is in line with molecular modelling studies which show two very different binding geometries between the enantiomers with each polymorph of DNA. Copyright © 2010 John Wiley & Sons, Ltd. 相似文献
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The effects of three organophosphate pesticides, i.e. monocrotophos, dichlorvos, and phosphamidon on respiration in rat brain and liver tissue slices have been studied. Among these pesticides dichlorvos causes significant inhibition of respiration both in brain and liver. 相似文献
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This study investigated the anaerobic degradation of tetrachlorobisphenol-A (TCBPA) in sediment samples collected at three sites along the Erren River in southern Taiwan. TCBPA anaerobic degradation half-lives (t1/2) in the sediment were 12.6, 16.9 and 21.7 d at concentrations of 50, 100, and 250 ??g g−1, respectively. TCBPA (50 ??g g−1) anaerobic degradation half-lives (t1/2) in the sediment were 10.1, 11.8, 11.0, 11.6, 10.8, 9.1, 8.5, 18.2, 19.3, and 16.1 d by the addition of yeast extract (5 mg l−1), cellulose (0.96 mg l−1), sodium chloride (1%), brij 30 (130 mg l−1), brij 35 (43 mg l−1), rhamnolipid (55 ??M), surfactin (91 ??M), phthalic esters (2 mg l−1), nonylphenol (2 mg l−1), and heavy metals (2 mg l−1), respectively. The degradation rate of TCBPA was enhanced by the addition of yeast extract, cellulose, sodium chloride, brij 30, brij 35, rhamnolipid, or surfactin. However, it was inhibited by the addition of phthalic esters, nonylphenol, or heavy metals. Also noted was the presence of dichlorobisphenol-A and bisphenol-A, two intermediate products resulting from the anaerobic degradation of TCBPA accumulated in the sediments. 相似文献
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This study presents data collected over a 6 year period on the effects of extremely low‐frequency magnetic fields (MFs) (1·4–1·6 µT, 500 Hz and 1·4–1·6 µT, 72·5 Hz) and MFs in combination with other environmental stressors (elevated temperature, 0·01 mg l?1 trichlorfon, 0·01 mg l?1 copper sulphate pentahydrate) on roach Rutilus rutilus embryos. Effects were studied during different stages of early development. Rutilus rutilus were raised in ponds for 4 months after exposure to MFs. The mass, standard length (LS) and morphological characteristics of underyearlings which were exposed as embryos were recorded. An increase in embryo mortality and a decrease in LS and mass indices in underyearlings were noted after they had been exposed to a combination of MFs and different adverse environmental factors. In addition, exposure to MFs led to changes in the total number of vertebrae and the number of seismosensory system openings in the mandibular bones of underyearlings. MFs of different frequency caused both increases (500 Hz) and decreases (72·5 Hz) in morphological diversity. The stressors used in this study, however, did not increase the fluctuating asymmetry of bilateral morphological characteristics. The possible microevolutionary effects of exposure to MFs alone and in combination with other adverse environmental factors upon natural fish populations are discussed. 相似文献
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A synthesis of diastereomeric bicyclic dibenzoyl esters derived from enantiomerically pure (1S,5S)‐bicyclo[3.3.1]nonane‐2,6‐dione was accomplished. Molecules containing two benzoyl chromophores with different configuration in the bicyclic framework were obtained. Chiroptical properties of the synthesized enantiomerically pure molecules were studied. Diastereomeric esters exhibited exciton couplets in the circular dichroism (CD) spectra because of transannular interaction between non‐conjugated benzoate chromophores. The conformational effects and solvent impact on the exciton coupling were examined by CD spectroscopy. Theoretical computation of the CD spectra of diastereomers correctly reproduced the sign of the exciton couplets in the studied molecules, however, no major solvent dielectric constant influence and conformational effects per se on the exciton coupling was observed. Chirality 24:810–816, 2012. © 2012 Wiley Periodicals, Inc. 相似文献
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Rodrigo Gouvêa Taketani Henrique Fragoso dos Santos Jan Dirk van Elsas Alexandre Soares Rosado 《Antonie van Leeuwenhoek》2009,96(3):343-354
An analysis of the effect of an oil spill on mangrove sediments was carried out by contamination of mesocosms derived from
two different mangroves, one with a history of contamination and one pristine. The association between N2 fixers and hydrocarbon degradation was assessed using quantitative PCR (qPCR) for the genes rrs and nifH, nifH clone library sequencing and total petroleum hydrocarbon (TPH) quantification using gas chromatography. TPH showed that the
microbial communities of both mangroves were able to degrade the hydrocarbons added; however, whereas the majority of oil
added to the mesocosm derived from the polluted mangrove was degraded in the 75 days of the experiment, there was only partially
degradation in the mesocosm derived from the pristine mangrove. qPCR showed that the addition of oil led to an increase in
rrs gene copy numbers in both mesocosms, having almost no effect on the nifH copy numbers in the pristine mangrove. Sequencing of nifH clones indicated that the changes promoted by the oil in the polluted mangrove were greater than those observed in the pristine
mesocosm. The main effect observed in the polluted mesocosm was the selection of a single phylotype which is probably adapted
to the presence of petroleum. These results, together with previous reports, give hints about the relationship between N2 fixation and hydrocarbon degradation in natural ecosystems. 相似文献
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Giuseppe Cannazza Marina M. Carrozzo Umberto Battisti Daniela Braghiroli Carlo Parenti Alessandro Troisi Luigino Troisi 《Chirality》2010,22(9):789-797
Benzothiadiazines differently substituted at the sulfonamidic nitrogen atom, at the stereogenic carbon atom and at the anilinic nitrogen atom have been synthesized and fully characterized. Enantioseparation of these compounds has revealed rapid on‐column enantiomerization. The recently developed software DCXplorer has been successfully applied to calculate enantiomerization kinetic parameters. Enantiomerization barriers of 3‐phenyl substituted benzothiadiazines, calculated in this work, have indicated a higher enantiomerization rate suggesting that the aromatic substituent exerts a strong effect on the enantiomerization process. Methyl substitution on N2 position led to higher free energy barriers of enantiomerization, suggesting negative influence of methyl in the N2 position on enantiomerization kinetics. However, methylation on N4 position increases the enantiomerization rates significantly. The results obtained have been employed to postulate an enantiomerization mechanism for chiral benzothiadiazine type compounds. Chirality 2010. © 2010 Wiley‐Liss, Inc. 相似文献
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Mutagenicity of dichlorvos and methyl methanesulphonate for Escherichia coli WP2 and some derivatives deficient in DNA repair 总被引:2,自引:0,他引:2
The mutagenic and lethal action of methyl methanesulphonate (MMS) and dichlorvos (DDVP) has been studied on Escherichia coli WP2 and some derivatives deficient in DNA repair genes. The exrA+ and recA+ alleles were necessary for significant mutagenesis by either compound, and the uvrA gene affected neither the lethal nor mutagenic responses. Increased sensitivity to both compounds was shown by the exrA and uvrAexrA strains and in a more pronounced way by the uvrApolA, recA, and uvrAexrApolA strains.Bacteria deficient at the polA locus were 2 and 3 times more mutable by DDVP and MMS respectively, consistent with the hypothesis that the absence of the polA system for the repair of single-strand gaps results in a greater proportion of the total repair being channelled through the error-prone exrA+/recA+-dependent system. Single-strand breaks were detectable by alkaline sucrose gradient centrifugation after both MMS and DDVP treatment of polA bacteria. Thus in all the tests carried out, both compounds showed similar patterns of activity, and the results are consistent with their known ability to alkylate DNA. The chief differences were quantitative; sensitivity increases were far more pronounced with MMS which was also a far more potent mutagen than DDVP. 相似文献
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Two growth media containing arsenobetaine [(CH3)3 As+ CH2COO–] were mixed with coastal marine sediments, the latter providing a source of microorganisms. The mixtures were kept at 25 °C in the dark and shaken for several weeks under an atmosphere of air. The disappearance of arsenobetaine and the appearance of two metabolites were followed by HPLC. The HPLC-retention time of the first metabolite agreed with that of trimethylarsine oxide [(CH3)3AsO]. The second metabolite was identified as arsenate (As(V)) using hydride generation/cold trap/GC MS analysis and thin layer chromatography. This is the first scientific evidence showing that arsenobetaine is degraded by microorganisms to inorganic arsenic via trimethylarsine oxide. The degradation of arsenobetaine to inorganic arsenic completes the marine arsenic cycle that begins with the methylation of inorganic arsenic on the way to arsenobetaine. 相似文献
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The present study was designed to investigate the possible effects of chronic dichlorvos exposure on the various aspects of calcium homeostasis in rat brain. Chronic dichlorvos administration caused significant rise in the intrasynaptosomal calcium levels. The activity of major calcium expelling enzyme i.e. Ca2+ ATPase was found to be declined. Also, the depolarization induced calcium uptake via voltage operated calcium channels increased significantly. Concomitant to the increase in intrasynaptosomal calcium, calpain activity was found to be increased. The results presented herein, indicate that the toxic effects of dichlorvos could be mediated through modifications in the intracellular calcium homeostasis which may lead to impaired neuronal function. 相似文献
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为了解农药对不同发育期蝌蚪的毒性,以多疣狭口蛙Kaloula verrucosa蝌蚪为对象,采用水生生物急性毒性试验方法,研究杀虫剂敌敌畏(DDVP)对25期、26期、35期和42期蝌蚪的急性毒性影响.结果表明,在水温19.5~22.0℃条件下,敌敌畏对各期蝌蚪96 h LC50分别为1.13、1.43、1.38和0.61 mg/L,各期蝌蚪对敌敌畏的敏感顺序为42期>25期>35期>26期.由此得出敌敌畏对25期、26期和35期蝌蚪属中等毒性,对42期蝌蚪则表现为高毒.因此建议农药施用应尽量避开蝌蚪的变态期进行.蛙类胚胎期(出膜后)随着发育对外界环境的耐受性增强,蝌蚪期随着发育对外界环境的敏感性增强.鉴于42期蝌蚪意外死亡率高的特点,认为不宜采用变态期蝌蚪进行急性毒性试验. 相似文献
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1. Habitat degradation and biological invasions are important threats to fish diversity worldwide. We experimentally examined the effects of turbidity, velocity and intra- and interspecific competition on prey capture location, reactive distance and prey capture success of native rosyside dace ( Clinostomus funduloides ) and invasive yellowfin shiners ( Notropis lutipinnis ) in Coweeta Creek, North Carolina, U.S.A.
2. Increased turbidity and velocity produced significant decreases in the number of prey captured forward of the fish's location. It is possible that this represents an increase in the amount of energy expended per prey captured.
3. We used Akaike's Information Criterion (AIC) to evaluate competing explanatory models for reactive distance (10 generalised linear models, GLM) and prey capture success (9 generalised linear mixed models, GLMM).
4. Reactive distance decreased by 12% with an increase from 2 to 4 conspecifics, whereas a 10 NTU increase in turbidity reduced reactive distance by 9%. Capture success was affected by velocity, dominance and competition, and varied among species. A 6 cm s−1 increase in velocity produced a 28% decline in capture probability; however, dominant fish were 3.2 times more likely to capture a prey item than non-dominant fish. Yellowfin shiners only were 0.62 times as likely to capture a prey item as rosyside dace. Both intra- and interspecific competition reduced capture probability, and fish in high density intraspecific or interspecific trials were 0.46 times and 0.44 times as likely to capture prey, respectively, as fish in two fish intraspecific trials.
5. These results suggest behavioural variables are as important as physical factors in determining reactive distance and capture probability by these minnows. 相似文献
2. Increased turbidity and velocity produced significant decreases in the number of prey captured forward of the fish's location. It is possible that this represents an increase in the amount of energy expended per prey captured.
3. We used Akaike's Information Criterion (AIC) to evaluate competing explanatory models for reactive distance (10 generalised linear models, GLM) and prey capture success (9 generalised linear mixed models, GLMM).
4. Reactive distance decreased by 12% with an increase from 2 to 4 conspecifics, whereas a 10 NTU increase in turbidity reduced reactive distance by 9%. Capture success was affected by velocity, dominance and competition, and varied among species. A 6 cm s
5. These results suggest behavioural variables are as important as physical factors in determining reactive distance and capture probability by these minnows. 相似文献
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A simple and precise method for chiral separation of tryptophan enantiomers using high performance liquid chromatography with
aligand exchange mobile phase was developed. Chiral separation was performed on a conventional C18 column, using a mobile phase that consisted of a water-methanol solution (88∶12, v/v) containing 10 mmol/Ll-leucine and 5 mmol/L copper sulfate as a chiral ligand additive at a flow rate of 1.0 mL/min. This method allowed baseline
separation of two enantiomers with a resolution of 1.84 in less than 30 min. The effect of various conditions, including concentration,
type of ligand, organic modifier, pH, flow rate, and temperature, on enantioseparation were evaluated and chiral recognition
mechanisms were investigated. Thermodynamic data (ΔΔH and ΔΔS) obtained by van't Hoff plots revealed that enantioseparation is an enthalpy-controlled process. 相似文献
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目的:探讨急性重度敌敌畏中毒患者血清儿茶酚胺水平与其心脏损伤的关系。方法:选取我院2009年12月至2011年12月收治的急性重度敌敌畏中毒患者40例,接受阿托品和氯解磷定等常规治疗,检测患者入院第1、3、5天血清肌酸激酶(CK-MB)、心肌肌钙蛋(CTNI)、胆碱酯酶(AchE)、乙酰胆碱(Ach)、肾上腺素(EPI)和去甲肾上腺素(NorP)等指标,分析患者血清儿茶酚胺水平与其心脏损伤的关系。结果:40例患者中,34例存活,6例死亡;窦性心动过速35例,心电图(ECG)ST-T改变36例;血清CK-MB、CTNI入院第1、3、5天相比,先升高后降低,出院时降至正常,变化差异有统计学意义(CK-MB:H=8.782,P=0.002;CTNI:H=5.017,P=0.024)。Ach入院第1天时最高,逐渐降低,出院时恢复到正常水平,变化差异有统计学意义(H=9.235,P=0.002;AchE入院第1天时最低,逐渐升高至正常,变化差异有统计学意义(H=46.891,P=0.001)。肾上腺素(EPI)和去甲肾上腺素(NorP)代表儿茶酚胺的变化,入院当天为峰值,其后均逐渐下降,出院恢复正常,变化差异有统计学意义(EPI:H=16.031,P=0.021;NorP:H=57.913,P=0.025)。进一步分析显示EPI和与NorP水平分别与CK-MB和CTNII呈显著正相关,差异均具有统计学意义(P0.05)。结论:敌敌畏中毒时,儿茶酚胺与乙酰胆碱的释放增多,可能引起心肌损害或加重心肌缺血的严重程度。 相似文献
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PNU-103017, 4-Cyano-N-(3-(cyclopropyl(5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxo-2H-cycloocta(b) pyran-3-yl)methyl)phenyl)-benzenesulfonamide, is a selective HIV aspartyl protease inhibitor under evaluation as a potential oral treatment of Acquired Immunodeficiency Diseases. PNU-103017 is a racemic mixture of two enantiomers, designated PNU-103264 (R-) and PNU-103265 (S-). Stereoselective pharmacokinetics of the two enantiomers of PNU-103017 were observed in the dog, rat, and human after single and multiple dose administration of the racemate and were apparently species-dependent. Mean enantiomeric ratios of plasma concentrations (R-/S-) at each time point were greater than 1 in the dog, ranging from 1.22 to 3.06, but less than 1 in the rat and in the human, ranging from 0.44 to 0.80 and 0.23 to 0.73, respectively. A trend towards increased or decreased (farther from 1:1, R-/S-) enantiomeric ratio of plasma concentrations with time after each administration was also observed. The enantiomeric ratio remained unchanged after multiple dose administration in the rat, dog, and human although enzyme induction and increased plasma clearance were observed for both enantiomers. Chirality 10:210–216, 1998. © 1998 Wiley-Liss, Inc. 相似文献