Induction of hepatic drug metabolizing enzymes in mammals by pesticides: A review

Abstract

The induction of drug metabolizing enzymes in mammals is summarized including both enzymes of the cytochrome P‐450‐dependent microsomal mixed function oxidase system and glutathione S‐transferases. Particular emphasis is placed on the role of pesticides as inducers, the early work being summarized while investigations carried out at North Carolina State University are considered in greater detail. Finally, the possible significance of induction is considered.     

A device for sampling the mud‐water interface in eutrophic lakes and bogs for residue analysis

Abstract

A tubular device has been developed making it possible to obtain layered samples of loosely aggregated, flocculent material from bogs or eutrophic lakes. The samples are up to 50 cm long and 15 cm in diameter. The sampler is free from protuberances and intact, layered samples can be taken. The tubular part of the sampler is about 85 em long, the walls of the lower 25‐cm portion harbouring a pneumatic closing mechanism which is controlled from above the water surface. An extendible handle for manipulating the sampler and for guiding it into place, is fastened to the upper end of the sampling tube. The performance and the operation of the sampler in the field are described.     

Distribution and persistence of carbaryl in some terrestrial and aquatic components of a forest environment

Abstract

An oil‐based formulation of carbaryl (1‐naphthyl N‐methyl‐carbamate) (Sevin‐2‐Oil) was applied twice by a fixed‐wing aircraft at a dosage rate of 280 g of A.I./ha/application to a coniferous forest near Allardville, New Brunswick. The highest concentrations of the chemical in fir foliage, litter and forest soil 1 h after application were respectively 4.20, 1.21 and 0.59 ppm (fresh weight). The residues dissipated rapidly and the DT50 values obtained from the depletion curves were 2.3 d for foliage and 1.5 d for litter and soil samples. Very low levels (<0.1 ppm) of carbaryl persisted in foliage and litter beyond the 10 d sampling period. The maximum residue level found in stream water was 0.314 ppm and more than 50% of it had dissipated within 1 h. Low but detectable levels (0.001 ppm) of the chemical persisted in water until the end of the 10 d sampling period. Sediment samples contained a maximum level of 0.04 ppm, which dissipated below the detection limit within 5 h. Brook trout and slimy sculpins captured in the stream 1 d after the spray contained on average about 0.04 ppm of carbaryl and none of it was found in 3 d postspray samples.     

Mutagenicity of chloroaniline/lignin metabolites in the salmonella/microsome assay

Abstract

Chloroanilines are constituents of many agrochemicals and have been found to be metabolized to succinic acid conjugates, e.g., succinamides and succinimides. The mutagenic potential of five chloroanilines and their succinamides and succinimide derivatives have been tested with two strains of Salmonella typhimurium (TA98 and TA100) with and without rat hepatic micro‐somal fraction. None of the compounds produced a dose response effect with a two‐fold increase in revertants indicating that these compounds are not mutagens or promutagens in these assays.     

An improved method to study the impact of pesticide sprays on small song birds

Abstract

Four test groups of small songbirds (Zebra Finch, Poephila guttata) were sprayed in a chamber with varying concentrations of fenitrothion. Exposure levels were assessed by monitoring air concentrations, deposits of the active ingredient (AI) on glass plates and droplets/cm² on Kromekote® cards. All indices of exposure were linearly correlated and the mean AI deposit on glass plates for the four groups tested were equivalent to 38, 51, 139 and 255 g/ha or 14%, 18%, 50% and 91% of the highest permissible emitted rate for broadscale forest spraying in Canada. Significant depression in body weights and brain acetylcholinesterase levels were noted only for the highest exposure group. Fenitrothion residues in blood were detectable only at the highest exposure level, and in liver at the two higher levels. Carcass and feather residues were much higher than those in blood and liver, and were detectable at all exposure levels but the residues did not increase linearly with exposure. For one of the spray groups, we were able to compute an equivalent acute oral dose based on matching acetylcholinesterase inhibition.     

Appendix

Abstract

An atrazine‐degrading bacterial isolate (M91–3) was able to utilize simazine and cyanazine as N sources for glucose‐dependent growth. The degradation of these three 5‐triazine herbicides was also investigated in binary and ternary mixtures. The organism used atrazine and simazine indiscriminately, whereas cyanazine degradation was slow and delayed until the depletion of the two other herbicides. There was no apparent effect of other commonly used herbicides on the rate of atrazine degradation by M91–3.     

The effects of triclopyr on 2,4‐D mineralization in two soils

Abstract

The effects of the herbicide triclopyr (3,5,6‐trichloro‐2‐pyridinyloxyacetic acid) on the mineralization of 2,4‐D (2,4‐dichlorophenoyxacetic acid) in two soils which differed in their histories of prior exposure to the two herbicides were investigated. The relative effects of triclopyr on 2,4‐D mineralization and most probable numbers of 2,4‐D degraders were dependent upon the soil. Triclopyr was shown to increase 2,4‐D mineralization rates in a soil which had been exposed to both 2,4‐D and triclopyr, but decreased the mineralization rate of 2,4‐D and inhibited the increase of most probable numbers of 2,4‐D degraders in a soil that had not been directly exposed to either herbicide.     

Rain‐washing of foliar deposits of Dimilin®WP‐25 formulated in four different carrier liquids

Abstract

Dimilin^® WP‐25, a wettable powder formulation of diflubenzuron (DFB) [1‐(4‐chlorophenyl)‐3‐(2,6‐difluorobenzoyl) urea], was formulated in four different carrier liquids, viz., water; a light petroleum paraffinic oil, ID 585; a heavy paraffinic oil, Sunspray^® 7N; and a 1:2 mixture of a light petroleum aromatic solvent (Cyclosol^® 63) and canola oil; to provide four end‐use mixtures, Dim‐W, Dim‐585, Dim‐7N and Dim‐Cy‐C respectively, each containing 28 g of DFB per litre. Balsam fir branch tips clipped from greenhouse‐grown seedlings, and sugar maple branch tips clipped from field‐grown young trees, were exposed to uniform‐sized droplets (ranging in diameters from 135 to 190 μm) of the four end‐use mixtures which were atomized using a monodispersed droplet generator. Droplets were collected on the fir and maple branch tips and the initial residue per g fresh weight of foliage was determined by high‐performance liquid chromatography (HPLC). The branch tips were exposed to cumulative rainfall of 3, 6 and 10 mm at an intensity of 5 mm/h and at time intervals of 1, 12, 36 and 72 h after DFB treatment, to test the influence of ‘ageing’ of foliar residues on rainfastness. Foliar samples were collected for residue determination just before the onset of rainfall, and at 0.5 h post‐rain. DFB was quantified by the HPLC method. In the case of fir foliage, the Dim‐W formulation was the most susceptible to rain‐washing and the rainfastness did not increase with the ageing period of foliar deposits. In contrast, the three oil‐based mixtures showed greater rainfastness depending upon the carrier liquid and the ageing period. Rainfastness decreased in the order of Dim‐Cy‐C > Dim‐7N > Dim‐585 > Dim‐W. In contrast, the data on maple foliage indicated that the ageing of deposits increased the rainfastness of all the 4 end‐use mixtures. Dim‐585 was the most susceptible to rain washing, and rainfastness decreased in the order of Dim‐W > Dim‐Cy‐C > Dim‐7N > Dim‐585.     

Persistence of Bacillus thuringiensis deposits in a hardwood forest,after aerial application of a commercial formulation at two dosage rates

Abstract

A commercial formulation of Bacillus thuringiensis Berliner var. kurstaki (BTK), Foray® 48B, was sprayed aerially over four blocks B13, B14, B15A and B15B in an oak forest in Wayne County, Pennsylvania during May 1990. B13 and B14 were sprayed at 75 billion international units (BIU) in 5.91 litres/ha and the other two at 50 BIU in 3.94 litres/ha. Oak foliage was collected at different intervals of time after treatment. Three types of bioassays were conducted against fourth instar gypsy moth larvae, viz., direct feeding of sprayed foliage, feeding on diet containing homogenized foliage, and force‐feeding of foliar extracts. Larval mortalities were converted into international units of BTK activity per unit area (IU/cm²) of foliage. Foliar extracts were also subjected to enzyme‐linked immunosorbent assay (ELISA) to determine the concentration of delta‐endotoxin protein. Regardless of the type of bioassay used, bioactivity of BTK persisted in foliage for about a week in all the blocks. The half‐life of inactivation, DT₅₀, ranged from ca 12 to 22 h. The immunoassay data indicated a shorter duration of persistence (i.e., about 2 d) of the delta‐endotoxin protein, with DT₅₀ values ranging from 10 to 15 h. Formulation ingredients present in Foray 48B played a role in the toxicity of BTK to gypsy moth larvae.     

The role of toxicology in the evaluation of new agrochemicals

Abstract

The use of agrochemicals like crop protecting agents, veterinary disinfectants, and wood preservatives may result in (un)intentional exposure of the environment, animals and man. This paper deals with current testing strategies to assess the potential health risks for humans exposed to these chemicals during production or application or via consumption of foods containing pesticide residues.

Principles and procedures for safety assessment of pesticide residues in food as developed by WHO/FAO are described. Different types of toxicity studies in mammalian test animal species are discussed and a strategy is outlined in order to characterize the toxicity profile of a compound and the relationship between applied doses and adverse effects. Safety testing of agrochemicals should be carried out in relation to its intended use, and in particular attention will be paid to toxicity testing of residues of pesticides in food. Extrapolation of results from animal studies to humans and the use of safety factors is discussed.

Besides the use of animal protocol studies for safety testing of agrochemicals, the potential use of in‐vitro models derived from organs and tissues of animals is discussed. Data on the in‐vitro metabolism of thiabendazole, aldicarb and alachlor are discussed in order to demonstrate that such data may complement or partly substitute whole animal experimentation.

Principles and procedures for safety testing of residues of agrochemicals in food as applied during the last three decades, constitute a ‘safety‐first’ approach, providing sufficient safety margins for the consumer of foods which may contain low levels of residues of agrochemicals.