Effect of dietary factors and environmental chemicals on intestinal drug metabolizing enzymes

The liver is the major site of metabolism of foreign chemicals, but contribution from intestinal biotransformation can influence the overall disposition of chemicals. The intestinal drug‐metabolizing enzymes are located in the endoplasmic reticulum and they possess biochemical properties similar to those of the hepatic system. In general, the rate of in vitro metabolism of drug substrates in intestines is lower than in the liver. There seem to be differences in regulation and induction of hepatic and intestinal drug‐metabolizing enzymes. The in vitro intestinal metabolism of foreign chemicals is affected by several factors including the nutritional status of the animal. Dietary components such as vitamins, lipids and vegetables can modify the activities of intestinal drug‐metabolizing enzymes. Phenobarbital or 3‐methyl‐cholanthrene (3‐MC) pre‐treatment induces the hepatic metabolism of a wide variety of drug substrates in a number of species, while the stimulation of intestinal enzymes is both substrate and species specific. Rabbit intestinal drug‐metabolizing enzymes seem to be resistant to induction by foreign chemicals.     

PFOS潜在替代品全氟丁基磺酸钾对不同营养水平水生生物的毒性

全氟丁基磺酸钾(PFBSK)作为全氟辛基磺酸(PFOS)潜在的替代品,极易溶于水,主要存在于水体中,因而其水生毒性的研究十分重要。采用OECD 201、OECD 202、OECD 203和OECD 211标准试验方法,研究了PFBSK对羊角月牙藻(Pseudokirchneriella subcapitata)、大型溞(Daphnia magna)和中国本土鱼种稀有鮈鲫(Gobiocypris rarus)的急性毒性效应以及对大型溞繁殖的影响。组合多终点急慢性水生生物毒性结果：PFBSK的急性毒性终点均大于100 mg·L^-1,大型溞繁殖试验的无观察效应浓度(NOEC)为571 mg·L^-1,最低可观察效应浓度(LOEC)为981 mg·L^-1。按GHS分类导则,PFBSK未表现出急性毒性和慢性毒性。与之相比,PFOS则对水生生物表现出毒性,黑头软口鲦(Pimephales promelas)为最敏感物种,其96 h-LC₅₀为4.7 mg·L^-1;大型溞繁殖试验的NOEC为12 mg·L^-1。按GHS分类导则,属于中等毒性物质。可见,PFBSK较PFOS水生毒性明显降低。     

三氯生对青海弧菌Q67和人乳腺癌细胞MCF-7的时间毒性

三氯生(triclosan,TCS)是一种广谱性抗菌剂,2005年欧盟水框架指令将TCS列为一种新型污染物。目前对TCS的研究局限于急性毒性实验,关于TCS毒性随时间的变化以及不同溶解状态下TCS的毒性差异的研究却鲜有报道。应用以96孔微板为暴露反应载体的微板毒性分析法,添加氢氧化钠(NaOH)或使用二甲亚砜(DMSO)作为助溶剂溶解TCS,分别测定其对青海弧菌Q67的相对发光抑制毒性(15min急性毒性和时间毒性)和对人乳腺癌细胞MCF-7在不同暴露时间(24、48和72h)内的细胞增殖抑制毒性。Q67的急性毒性实验结果表明,碱性条件下TCS的毒性(EC50=3.97(10-8mol.L-1)大于DMSO作为助溶剂时的毒性(EC50=1.68(10-4mol.L-1)。无论碱性条件还是DMSO助溶,TCS在不同暴露时间内对Q67的时间毒性没有明显差异。在不同暴露时间下MCF-7增殖抑制率实验中,DMSO作为助溶剂时,TCS的最高实验浓度为1.46(10-3mol.L-1,随着暴露时间的延长,抑制率在24、48和72h时分别为27.8%、44.2%和62.4%;碱性环境时TCS的最高实验浓度为1.39(10-6mol.L-1,随着暴露时间的延长,抑制率在24、48和72h时分别为20.2%、55.8%和73.9%。研究表明,在DMSO和NaOH作为助溶剂的条件下,TCS对MCF-7均存在时间毒性差异,并且NaOH碱性溶液中TCS对MCF-7的毒性远大于DMSO作为助溶剂时的毒性。     

Influence of some parameters on adsorption rate and toxicity of cadmium in activated sludge

The influence of pH, competitor ions (NaNO₃) and aerobic and anaerobic stabilization of activated sludge on the cadmium uptake by activated sludge solids was investigated. Above 0.08 mg L^‐1 cadmium in solution, biosorption was found to follow the Freundlich isotherm. Active cellular uptake of soluble cadmium does not appear to be a significant mechanism of the biosorption. In addition, the cadmium uptake is not completely reversible. The adsorption of cadmium by activated sludge seems to involve a physico‐chemical mechanism with especially weak electrostatic interactions with ion‐exchange reaction. The optimum adsorption pH was 7.5. Adsorption is influenced by sodium ion concentrations up to an equivalent conductivity of 10 000 μS cm^‐1. Aerobic and anaerobic stabilization of activated sludge increase systematically the initial adsorption capacities. Respirometric measurements were done to evaluate the inhibitive effects of cadmium on activated sludge. Monod's equation and the equation of non‐competitive inhibition were used to describe the toxicity related to cadmium uptake. These two equations appear to be complementary.     

Activated carbon adsorption,activated sludge and ozonation treatments evaluated by impact intensity based on acute toxicity test

A Toxicity Reduction Evaluation (TRE) conducted on various water treatments was successful in optimizing the acute toxicity of the final effluent. In particular, we found that the acute toxicity of the sample water treated by a water treatment process should not be correlated with the concentrations of the parent compounds still remaining in the water. Therefore, it was concluded that an acute toxicity test based on a bioassay must be performed in order to evaluate the efficiency of the water treatment process for various effluents containing environmental pollutants. In addition, the treatability and the resultant toxicity was evaluated as a simple scoring system. The scoring system ranked the treated water in three classes of toxicity with the calculation of several factors for the concerned toxicity. Using an impact evaluation based on the score of the characteristics, different water treatment processes could be directly compared. The new methodology presented here is specifically effective in listing possible unit operations for a water treatment process based on the impact, and thereby enables targeted and cost-effective water treatment.     

Study on increase in toxicity of Schiff bases on microorganism on chelation with metal

New heterochelates of the type [M(L)(SB)(H₂O)] (where M?=?Mn(II), Co(II), Ni(II), Cu(II), Zn(II), and Cd(II), KHL?=?potassium salt of salicylideneglycine and SB?=?thiophene- O -carboxaldeneaniline) have been synthesized. The heterochelates have been characterized on the basis of elemental analyses, electronic spectra, and magnetic measurement analyses. The structural and geometrical conformation has been discussed on the basis of IR spectral data. A thermal study of the complexes has been carried out to ascertain their thermal stability. Magnetic susceptibility measurements and electronic spectral data suggest a six-coordinated octahedral structure for these complexes. The increase in toxicity of the investigated heterochelate metal compounds was tested against three gram-negative bacteria, S. typhi, E. coli, and Serratia marcescens by the disc diffusion method. It is observed that the heterochelates show higher toxicity when compared to the Schiff bases, metal salts, and control (DMSO) due to chelation. The toxicity is also compared to the standard drug tetracycline.     

Quantal response of Paleomonetes africanus in locally formulated drilling mud lubricants

The toxic potency of three locally formulated drilling mud lubricants against Paleomonetes africanus, a brackish water crustacean commonly found in the oil producing Niger Delta (Nigeria), was evaluated. A 96?h exposure to quantal (lethal) doses of the mud lubricants gave LC₅₀ (median lethal concentration) of 350, 620 and 210?mg?L^?1, respectively. The mud lubricant with the highest molecular weight of 40,000?g?mol^?1 (lubricant 2) had the least toxicity on the organisms, attributable to the reduced rate of diffusion into the vital cells of the test organism. The higher toxicity of lubricant 3 over lubricant 1, despite its higher molecular weight, might be as a result of its higher acid value of 21.60?mg?KOH?g^?1. The results show that the test lubricants would be environmentally friendly within the baseline concentrations and lethal times (LT₅₀) measured.     

Uptake and toxicity of some pesticides on three freshwater fishes (Oreochromis niloticus,Clarias gariepinus and Chrysicthys nigrodigitatus)

Studies were carried out to determine the toxicity of some selected pesticides on fresh water fish in a tropical environment. The uptake of the pesticides lindane, pentachlorophenol (PCP), and propoxur, which are frequently used by farmers and industrialists were studied in concrete ponds at the University of Cape Coast, in Ghana. The fishes used for the study were Oreochromis niloticus, Clarias gariepinus, and Chrysicthys nigrodigitatus, and were obtained from cultured ponds in the Cape Coast District and Mankessim in the Central Region and Weija Dam, in the Greater Accra region of Ghana. Single high lethal concentration (SD) or acute treatment and cumulative/chronic (or multiple minor) lethal concentration (CD) treatment were employed in administering the pesticides to the fishes via water. Gas chromatograph (GC) Electron Capture Detector (ECD) analysis was done on the dead fishes to see the extent of ingestion. The LC₅₀ values obtained for lindane on the three fish samples were as follows: Chrysicthys?–?0.38?mg?L^?1; Oreochromis?–?0.42?mg?L^?1, and Clarias?–?1.2?mg?L^?1. Mortalities occurred in fish within 3–5 days of application. For the PCP on Chrysicthys, Oreochromis, and Clarias species the LC₅₀ values were 0.42, 0.32 and 0.64?mg?L^?1, respectively for over a 2–3 day period. For a three-time influx period of propoxur the LC₅₀ for Chrysicthys, Oreochromis, and Clarias, were 22.0, 30.40, and 45.04 (all in mg?L^?1), respectively. The results obtained indicated that the pesticides had adverse effects on the general growth and reproduction of fishes. Gonadosomatic indices also showed that the pesticides affected the development of the body, the gonads, and their reproduction.     

In vitro genotoxicity of extracellular extract from Nostoc piscinale

The extracellular extract obtained from 3 weeks incubation of the soil isolate cyanobacterium strain Nostoc piscinale GT-319 in BG-11 broth medium showed cytotoxic activity against Chinese Hamster Ovary (CHO) cells. Based on comet assay, a concentration of 333 µg mL^?1 (IC₅₀) produced DNA breakages in CHO cells. The concentration of 481 mg kg^?1 (LD₅₀) produced acute toxicity in mice at 48 h.     

Differential toxic response of Chironomus travalensis kieffer ( Chironomidae : Diptera ) to some industrial effluents

Acute toxicity testing of some industrial effluents (rubber (Rr), brewery (Br), and bottling (Bt)) on Chironomus travalensis (Diptera larvae) was determined at 96-h using a static bioassay technique. Effluent quality characterization revealed acidic pH values of 4.5 for Rr, 5.64 for Br, and 4.32 for Bt effluents. Tests were carried out in replicates between 10 and 100% effluent concentrations. Mortality rate rose progressively with increasing concentrations. Bt effluent was the most toxic with 96-h LC₅₀ of 61.5%, closely followed by Rr effluent with 96-h LC₅₀ of 87% and the least toxic was Br effluent with 96-h LC₅₀ of 90%.