Synthesis and Anthelmintic Activity of 7-Hydroxy- 5-oxo-5H-thieno[3,2-b]pyran-6-carboxanilides and -6-thiocarboxanilides

7-Hydroxy-5-oxo-5H-thieno[3,2-b]pyran-6-carboxanilides and -6-thio-carboxanilides represent a novel series of anthelmintic compounds, with broad-spectrum activity against important parasitic nematodes in sheep and dogs. In particular, an improved efficacy against Trichostrongylus colubriformis in sheep over the related 3-carbamoyl-4-hydroxycoumarins has been noted. New synthetic routes to the key intermediate, 7-hydroxythieno[3,2-b]pyran-5-one, have been developed.     

Anthelmintic Actions of the Cyclic Depsipeptide PF1022A and its Electrophysiological Effects on Muscle Cells of Ascaris suum

The cyclic depsipeptide PF1022A, given orally to mice, showed very good anthelmintic activity against Heligmosomoides polygyrus and Heterakis spumosa at 50 mg kg⁻¹. In vitro, PF1022A was very active against Trichinella spiralis and had good activity against Nippostrongylus brasiliensis at 1 μg ml⁻¹. An 18-membered enniatin analogue, JES 1798, showed good activity only against N. brasiliensis at 10 μg ml⁻¹. The optical antipode of PF1022A had poor activity even at 100 μg ml⁻¹. The effects of PF1022A on the membrane potential and input conductance of somatic muscle of Ascaris suum were examined using a two-microelectrode current-clamp technique. PF1022A did not antagonize the effects of the selective nicotinic agonist levamisole. PF1022A and an analogue, JES 1798, but not the PF1022A antipode, produced a small time-dependent increase in input conductance associated with no potential change. The increase in input conductance did not occur in the Cl⁻-free bathing solution, suggesting that the increase in input conductance was mediated by Cl⁻ ions. The addition of high concentrations of Ca²⁺ to the preparation after the addition of PF1022A did not lead to production of Ca²⁺-activated Cl⁻ channels, suggesting that its mode of action was not that of a Ca²⁺ ionophore. The mechanism by which the cyclic depsipeptide might increase the Cl⁻ conductance is discussed.     

Application of sperm cryopreservation in selective breeding of the Pacific oyster,Crassostrea gigas (Thunberg)

The robustness of Pacific oyster, Crassostrea gigas (Thunberg), sperm cryopreservation in the context of selective breeding based on family lines was investigated. Irrespective of egg density, high fertilization success was achieved with cryopreserved sperm when sperm:egg ratios of 1000:1 to 10 000:1 were used. Variation among replicate runs on the same oyster batches was minimal, indicating that cryopreservation and larval rearing procedures were repeatable. Twenty independent single male–female crosses were made to assess the utility of cryopreserved sperm in selective breeding. The fertility of unfrozen sperm was generally a poor predictor of cryopreserved sperm fertility. Based on D‐larval yields, 17 of the 20 crosses were likely to yield adequate spat for selective breeding (>10⁵ D‐larvae from 1 million eggs), two were marginal (5 × 10⁴ D‐larvae) and one was inadequate (4 × 10³ D‐larvae). An alternative fertilization strategy to improve D‐yield from a given number of sperm was then tested. Fertilizing 10 million eggs at a sperm:egg ratio of 200:1 increased the total D‐yield when compared with fertilizing 1 million eggs at a sperm:egg ratio of 2000:1 for the same male–female pair. We conclude that, despite wide variation in fertility, cryopreserved sperm is useful for family production.     

Schmeißfliegen (Calliphoridae) und vakuumverpackter Schinken

Blowflies (Calliphoridae) and vacuum-packed ham In a few cases blowfly maggots have been reported from vacuum-packed ham. The possibility of egg-hatching and larval development in the product was analysed. In experiments no hatching of blowfly eggs on vacuum-packed, boiled, sliced ham occurred. However, the eggs are not killed immediately; 1–4 days after the packing, they are still viable and when the wrapping is broken, hatching may occur. After a stay of 7–10 days on vacuum-packed ham, the viability of the eggs seems lost. In the actual case the risk of oviposition by blowflies on ham in the cannery and succeeding larval development in the product is considered to be very low.     

Effect of consumption of organically and conventionally produced apples on antioxidant activity and DNA damage in humans

The present study was performed to compare the effects on antioxidant activity and on DNA damage of organic and conventionally produced apples grown under controlled conditions in human peripheral blood lymphocytes. Six healthy volunteers consumed either organically or conventionally grown apples (Golden Delicious, 1000 g) from two neighboring commercial farms in a double-blinded, randomized, cross-over study. The average content of total identified and quantified polyphenols in the organically and conventionally produced apples was 308 and 321 microg/g fresh weight, respectively. No statistically significant differences in the sum of phenolic compounds or in either of the polyphenol classes were found between the agricultural methods. Consumption of neither organically nor conventionally grown apples caused any changes in antioxidant capacity of low-density lipoproteins (lag time test), endogenous DNA strand breaks, Fpg protein-sensitive sites, or capacity to protect DNA against damage caused by hydrogen peroxide. However, a statistically significant decrease in the levels of endonuclease III sensitive sites and an increased capacity to protect DNA against damage induced by iron chloride were determined 24 h after consumption in both groups of either organic or conventionally grown apples, indicating the similar antigenotoxic potential of both organically and conventionally grown apples.     

Der Bulk-Stomata-Widerstand von Ackerbohnen und seine Abhängigkeit vom Bodenwassergehalt

Bulk stomatal resistance of Vicia faba and its dependence on soil water content Bulk stomatal resistance of beans (Vicia faba L.,) as a function of soil water content was estimated for 41 days by comparison of potential transpiration, determined from meteorological data, and actual transpiration, determined from soil water losses. The resistance of beans is about 46 s/m if soil water content is above 70 % of available field capacity and increases strongly in dryer situations. This behaviour can be described by an exponential function.     

Bodenmechanische Eigenschaften als Kriterium für die Klassifizierung von Andepts aus Südchile

Mechanical soil properties as criteria for the classification of Andepts The shear strenght in the upper layer of seven different Andepts from southern Chile was examined. The samples were taken from sites of a middle slope position, in one of the Andepts from five positions of catena. The intention was to determine the variation of shear strenght properties, within and between the soil series. Moreover, some physical and chemical properties of the soils were determined. The evaluation includes multiple regressions, principal component analyses (PCA) and cluster analyses, in order to check the interrelation of soil properties for grouping the samples. The variables of the first two components between the series which show the greatest variability of the soil properties are consistency characteristics and shear strenght parameters. The PCA permit conclusion that the shear strenght parameters are useful criteria for grouping the analysed Andepts. However, they contribute only moderately to the total variation between the samples of the studied catena. The groups of soil samples formed by the series from the same topographic position are closely related to their distance from the Andes and their particle size distribution. The groups formed by the samples from the catena, show the humidity of the site as a common influence factor.     

LC-MS/MS quantification of sulforaphane and indole-3-carbinol metabolites in human plasma and urine after dietary intake of selenium-fortified broccoli

This study aimed at developing a sensitive LC-MS/MS method for the quantification of sulforaphane (SFN) and indole-3-carbinol metabolites in plasma and urine after dietary intake of regular and selenium-fertilized broccoli using stable isotope dilution analysis. In a three-armed, placebo-controlled, randomized human intervention study with 76 healthy volunteers, 200 g of regular (485 μg of total glucosinolates and <0.01 μg of selenium per gram fresh weight) or selenium-fertilized broccoli (589 μg of total glucosinolates and 0.25 μg of selenium per gram fresh weight) was administered daily for 4 weeks. Glucoraphanin and glucobrassicin metabolites quantified in plasma and urine were SFN-glutathione, SFN-cysteine, SFN-cysteinylglycine, SFN-acetylcysteine, and indole-3-carboxaldehyde, indole-3-carboxylic acid, and ascorbigen, respectively. Dietary intake of selenium-fertilized broccoli increased serum selenium concentration analyzed by means of atomic absorption spectroscopy by up to 25% (p < 0.001), but affected neither glucosinolate concentrations in broccoli nor their metabolite concentrations in plasma and urine compared to regular broccoli.     

LC-MS/MS quantification of bioactive angiotensin I-converting enzyme inhibitory peptides in rye malt sourdoughs

This study quantified antiotensin I-converting enzyme (ACE) inhibitory peptides in rye malt sourdoughs supplemented with gluten proteins and fermented with six strains of Lactobacillus spp. Bioinformatic analysis of prolamins from barley, rye, and wheat demonstrated that the ACE inhibitory peptides LQP, LLP, VPP, and IPP are frequently encrypted in their primary sequence. These tripeptides were quantified by liquid chromatography-tandem mass spectrometry. Tripeptide levels in sourdoughs were generally higher as compared to the chemically acidified controls. Sourdoughs fermented with different strains showed different concentrations of LQP and LLP. These differences corresponded to strain-specific differences in PepO and PepN activities. The highest levels of peptides VPP, IPP, LQP, and LLP, 0.23, 0.71, 1.09, and 0.09 mmol (kg DM)(-1), respectively, were observed in rye malt: gluten sourdoughs fermented with Lactobacillus reuteri TMW 1.106 and added protease. These concentrations were 6-7 times higher as compared to sourdough without fungal protease and exceed the IC(50) by 100-1000-fold.