Bioavailability of phosphorus in agriculturally loaded rivers in southern Finland

The potential bioavailability of phosphorus in agriculturally loaded rivers of southern Finland was determined by an algal bioassay and the release of the potentially bioavailable particulate P was estimated by sorption studies. According to the bioassay 0 to 13.2 per cent (mean 5.1%) of the particulate P in river water samples was potentially bioavailable. Dissolved reactive P (DRP) in river waters appeared to be totally bioavailable whereas the dissolved unreactive P appeared not to be utilized by algae. In addition to river waters two lake sediment samples were also assayed. In these samples 0 and 2.6% of the P was bioavailable. The potential bioavailability of particulate P in agriculturally loaded rivers obtained in this study was lower than that reported in studies from other countries. The difference was assumed to arise partly from methodological factors and partly from the nature of the Finnish soils. The EPC (equilibrium phosphate concentration) values indicated that during the period when most of the agricultural loading enters the lakes in Finland, potentially bioavailable P is not released from the particles because of the relatively high DRP concentration in the receiving waters. However, during the algal production period the DRP concentration in lakes decreases below the EPC and potentially bioavailable particulate P is desorbed. The increase in pH during this period may further enhance the desorption of P.     

Bioisosteric replacement of anilide with benzoxazole: potent and orally bioavailable antagonists of VLA-4

We have designed and synthesized a series of heterocyclic bioisosteres for an anilide based on molecular modeling. Excellent potency was retained in the benzoxazole and the benzimidazole derivatives, where a hydrogen bond acceptor is appropriately positioned to mimic the amide bond oxygen. The deletion of the hydrogen bond donor (N-H) led to improved lipophilicity and bioavailability. In the process, 9a was identified as a potent, specific, and bioavailable VLA-4 antagonist, while 9c was found to be a potent and bioavailable dual antagonist of VLA-4 and alpha(4)beta(7).     

Biofortification and Bioavailability of Rice Grain Zinc as Affected by Different Forms of Foliar Zinc Fertilization

Background

Zinc (Zn) biofortification through foliar Zn application is an attractive strategy to reduce human Zn deficiency. However, little is known about the biofortification efficiency and bioavailability of rice grain from different forms of foliar Zn fertilizers.

Methodology/Principal Findings

Four different Zn forms were applied as a foliar treatment among three rice cultivars under field trial. Zinc bioavailability was assessed by in vitro digestion/Caco-2 cell model. Foliar Zn fertilization was an effective agronomic practice to promote grain Zn concentration and Zn bioavailability among three rice cultivars, especially, in case of Zn-amino acid and ZnSO₄. On average, Zn-amino acid and ZnSO₄ increased Zn concentration in polished rice up to 24.04% and 22.47%, respectively. On average, Zn-amino acid and ZnSO₄ increased Zn bioavailability in polished rice up to 68.37% and 64.43%, respectively. The effectiveness of foliar applied Zn-amino acid and ZnSO₄ were higher than Zn-EDTA and Zn-Citrate on improvement of Zn concentration, and reduction of phytic acid, as a results higher accumulation of bioavailable Zn in polished rice. Moreover, foliar Zn application could maintain grain yield, the protein and minerals (Fe and Ca) quality of the polished rice.

Conclusions

Foliar application of Zn in rice offers a practical and useful approach to improve bioavailable Zn in polished rice. According to current study, Zn-amino acid and ZnSO₄ are recommended as excellent foliar Zn forms to ongoing agronomic biofortification.     

Synthesis and SAR of benzyl and phenoxymethylene oxadiazole benzenesulfonamides as selective beta3 adrenergic receptor agonist antiobesity agents

Benzyl and phenoxymethylene substituted oxadiazoles are potent and orally bioavailable beta3 adrenergic receptor (AR) agonists. The 4-trifluormethoxy substituted 5-benzyl oxadiazole 5f has an EC50 of 8 nM in the beta3 AR agonist assay with 100-fold selectivity over beta1 and beta2 AR binding inhibition activity. Its oral bioavailability in dogs is 30 +/- 4%, with a half-life of 3.8 +/- 0.4 h. In the anesthetized rhesus, 5f evoked a dose-dependent glycerolemia (ED50Gly = 0.15 mg/kg). Under these conditions a heart rate increase of 15% was observed at a dose level of 10 mg/kg.     

Dermal Bioavailability of Toluene Aged in Soil

When organic chemicals age in soil, they can become more sequestered with time and less bioavailable. The impact of aging in soil was assessed on the dermal bioavailability of toluene. Comparisons were made between the dermal bioavailability of toluene aged in two soils (Atsion and Keyport) for 3 months, toluene in freshly spiked soil, and toluene without soil (pure chemical). In vitro flow-through diffusion cell methodology measured the amount of radioactive chemical that penetrated dermatomed male pig skin into receptor fluid, and that was detected in skin following soap and water decontamination. Volatilization reduced the amount of toluene that was available for skin penetration. Therefore, relative to the available dose, the total penetration of pure toluene (sum of the dose in the receptor fluid and skin) was 93%. The majority of pure toluene was found in skin (82%). The dermal bioavailability of non-aged and aged toluene was decreased to 4–6% and 3–4% of the available dose, respectively. The data suggest that there would be a lower potential risk to human health from dermal exposure to toluene in soil. However, lower soil loading and longer aging time are needed to quantitate the risk.     

Bioavailability of Vanadium Extracted by EDTA, HCl, HOAC, and NaNO3 in Topsoil in the Panzhihua Urban Park, Located in Southwest China

Bioavailable vanadium was evaluated on the basis of soil vanadium single-extraction with ethylenediaminetetraacetic acid (EDTA), hydrochloric acid (HCl), acetic acid (HOAc), and sodium nitrate (NaNO(3)) in Panzhihua urban park. The soil vanadium concentration extracted by HOAc was 0.01-2.07?mg?kg(-1), by EDTA 0.28-7.03?mg?kg(-1), by NaNO(3) 0.07-0.53?mg?kg(-1), and by HCl 0.19-1.36?mg?kg(-1). The bioavailable vanadium (bioavailable fraction) obtained with HOAc was 0.01-1.33%, with EDTA 0.27-4.09%, with NaNO(3) 0.13-0.72%, and with HCl 0.06-0.28%. In addition, the impact of soil properties, soil nutrients, and soil enzyme activities on bioavailability of vanadium is discussed in this study. Based on the characteristics of bioavailable vanadium in the soil, ecological and health risks should have been given more attention in the studied area.     

Substituted oxazole benzenesulfonamides as potent human beta3 adrenergic receptor agonists

As a part of our investigation into the development of orally bioavailable beta3 adrenergic receptor agonists, we have identified a series of substituted oxazole derivatives that are potent beta3 agonists with excellent selectivity against other beta receptors. Several of these compounds showed excellent oral bioavailability in dogs. One example, cyclopentylethyloxazole 5f is a potent beta3 agonist (EC50 = 14 nM, 84% activation) with 340-fold and 160-fold selectivity over beta1 and beta2 receptors, respectively, and has 38% oral bioavailability in dogs.     

Assessing bioavailability of the solubilization of organic compound in nonionic surfactant micelles by dose–response analysis

It is uncertain in some extent that organic compounds solubilized in micelles of a nonionic surfactant aqueous solution are bioavailable directly by the microbes in an extractive microbial transformation or biodegradation process. In this work, a dose–response method, where a bioequivalence concept is introduced to evaluate the synergic toxicity of the nonionic surfactants and the organic compounds, was applied to analyze the inhibition effect of organic compounds (naphthalene, phenyl ether, 2-phenylethanol, and 1-butanol) in nonionic surfactant Triton X-100 micelle aqueous solutions and Triton X-114 in aqueous solutions forming cloud point systems. Based on the result, a mole solubilization ratio of organic compounds in micelle was also determined, which consisted very well with those of classic semi-equilibrium dialysis experiments. The results exhibit that bioavailability of organic compounds solubilized in micelles to microbial cells is negligible, which provides a guideline for application of nonionic surfactant micelle aqueous solutions or cloud point systems as novel media for microbial transformations or biodegradations.     

Studies on bioavailability of some bulk and trace elements in mexican tortilla using an in vitro model

An in vitro gut model was used to investigate the bioavailability of calcium, magnesium, cadmium, chromium, iron, manganese, and lead in the Mexican (maize) tortilla. The samples (4 g) were digested in quartz tubes using concentrated nitric acid (12 mL) at 65‡C (2 h) and then at 120‡C (4 h). Total element concentration was determined by atomic absorption spectrometry. Enzymatic hydrolysis was carried out in two steps: first, with pepsin in a hydrochloric acid medium (pH 1.8) and then after neutralization with sodium bicarbonate (pH 6.0), with the mixture of pancreatine, amylase, and bile salts extract. Elements under study were determined in the supernatant by atomic absorption spectrometry. The bioavailable fraction of each element in tortilla was evaluated as the percentage of total element content found in the solution after enzymolysis. The obtained results showed relatively low bioavailability of the selected elements (from 2% to 32%), which possibly may be ascribed to the presence of dietary fiber in tortilla.     

Biodegradation of Dioxin-Related Compounds: A Review

A number of bacteria have been isolated, as well as genetically constructed, that are able to transform dioxin-related compounds including mono- and dichlorinated dibenzo-p-dioxins, dibenzofurans, and diphenyl ethers. Invariably, dioxygenases are the primary degradative enzymes involved in the transformations. In most cases, these dioxygenases operate regioselectively and attack their substrates at an ether bond-carrying carbon and an adjacent carbon (the angular position), which prompts the irreversible cleavage of otherwise recalcitrant aryl ether bonds. Arising metabolites typically are mineralized to carbon dioxide, water, and inorganic salts. Some angular dioxygenases have been studied biochemically, resulting in information that may help to expand their substrate ranges to include tri-, tetra-, and other poychlorinated dioxins. Theoretically, all toxic congeners are susceptible to biocatalysis because they all possess an unsubstituted carbon adjacent to an ether bridge. Bacteria harboring these enzymes represent a promising tool for the future bioremediation of contaminated soils. Feasibility studies have shown that hydrophobic dioxins are bioavailable and rapidly degraded in soils from concentrations of 10 ppm to levels in the low ppb range by laboratory-cultured bacteria. Even lower treatment endpoints may be achievable by using these bacteria in concert with methods to increase the bioavailability of the pollutants.     

Substituted acrylamides as factor Xa inhibitors: improving bioavailability by P1 modification

To overcome the low bioavailability of our substituted acrylamide P1 benzamidine factor Xa inhibitors reported previously, neutral and less basic groups were used to replace the benzamidine. As a result, a series of P1 aminoisoquinoline substituted acrylamide Xa inhibitors was identified to be potent, selective, and orally bioavailable. Modification of P4 moiety of these compounds further improved their pharmacokinetic properties.     

The bioavailability of colloidal and dissolved organic phosphorus to the alga Pseudokirchneriella subcapitata in relation to analytical phosphorus measurements

The speciation of phosphorus (P) in freshwater affects its bioavailability. Analytical detection methods were compared for different colloidal and dissolved organic forms of phosphorus (P) in relation to the potential P bioavailability to Pseudokirchneriella subcapitata, determined with a 14 day growth response to P. Growth on these P-forms was referenced to supplies of inorganic P (P_i) as operational definition of the relative potential bioavailability. The bioavailability of ten organic P molecules ranged 1–70% of P_i while these forms were generally not detected by colorimetric method (CM, malachite green) or ion chromatography (IC). The bioavailability of P associated with Fe- and Al oxides ranged 55–85% of P_i and these forms were completely detected by CM and partially by IC. The bioavailability of total dissolved P in the environmental samples ranged 7–85% (mean 43%) of P_i. The P detected by IC underestimates bioavailable P while CM and total dissolved P (inductively coupled plasma, ICP) overestimate P bioavailability by, on average 44% (CM) or 57% (ICP) in the environmental samples. We conclude that CM is the best index among the three tested for predicting long-term availability of environmental dissolved P in which colloidal P contributes more importantly than organic P.     

Assessment of Bioavailability after In Vitro Digestion and First Pass Metabolism of Bioactive Peptides from Collagen Hydrolysates

Collagen hydrolysates (CHs) are composed of bioactive peptides (BAPs), which possess health enhancing properties. There is a knowledge gap regarding the bioavailability of these BAPs that involves intestinal transport and hepatic first pass effects. A simulated gastrointestinal model was used to generate digesta from two CHs (CH-GL and CH-OPT), which were applied to a novel transwell co-culture of human intestinal epithelium cell line-6 (HIEC-6) and hepatic (HepG2) cells to simulate in vivo conditions of absorption and first pass metabolism. Peptide transport, hepatic first pass effects, and bioavailability were determined by measuring BAPs (Gly-Pro, Hyp-Gly, Ala-Hyp, Pro-Hyp, Gly-Pro-Hyp) using an innovative capillary electrophoresis method. All peptides were transported across the intestinal cell layer to varying degrees with both CHs; however, Gly-Pro-Hyp was transported only with CH-GL, but not CH-OPT. Notable hepatic production was observed for Ala-Hyp with both CH treatments, and for Pro-Hyp and Gly-Pro with CH-GL only. All peptides were bioavailable (>10%), except for Gly-Pro-Hyp after CH-OPT. Overall, a high degree of transport and hepatic first pass effects on CH-derived BAPs were observed. Further research is needed to explore the hepatic mechanisms related to the production of BAPs and the bifunctional effects of the bioavailable BAPs noted in this study.     

Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist

5-n-Pentyl oxadiazole substituted benzenesulfonamide 8 is a potent and selective beta3 adrenergic receptor agonist (beta3 EC50 = 23 nM, beta1 IC50 = 3000 nM, beta2 IC50 = 3000 nM). The compound has high oral bioavailability in dogs (62%) and rats (36%) and is among the most orally bioavailable beta3 adrenergic receptor agonists reported to date.     

Hepatic pyridine nucleotides content in rat--a better indicator for determining available niacin values of food.

After 10 days depletion period with niacin free diet, weanling rats were repleted with either reference diets containing niacin at four levels (2, 4, 8 and 12 mg/kg diet) or test diets containing test material at two levels as source of niacin. Gains in body weight and hepatic pyridine nucleotides content increased with increase in niacin intake. The correlation coefficient for hepatic pyridine nucleotides content and niacin intake was 0.98, whereas for weight gain and niacin intake was 0.89. Dried skim milk and pearl millet were taken as test materials. Dried skim milk with most of its niacin in free form showed 98% niacin equivalent to be bioavailable whereas in pearl millet niacin was in bound form and bioavailability equivalent was only 48 per cent.     

Phosphorus and nitrogen in a monomictic freshwater lake: employing cyanobacterial bioreporters to gain new insights into nutrient bioavailability

1. It is an uncontested paradigm that an adequate supply of the macronutrients nitrogen (N) and phosphorus (P) is critical for maintaining phytoplankton primary production in aquatic ecosystems; it has also been suggested that there is an optimal total N : total P ratio for this globally significant process. 2. This ratio, normally assessed by chemical determination of the major dissolved N and P species, poses a dilemma: do chemical measurements actually reflect the bioavailable fraction of these nutrient pools? Accurate determination of the various N and P species and their fluxes into phytoplankton cells is notoriously difficult. 3. To provide a possible solution to this difficulty, we engineered strains of the cyanobacterium Synechococcus sp. strain PCC 7942 that ‘report’ on N and P bioavailability via a bioluminescent signal. These strains were used to quantify, for the first time, bioavailable concentrations of these essential macronutrients in a freshwater lake. 4. Only a small fraction (0.01–1%) of the chemically determined P may actually be bioavailable to this unicellular cyanobacterium and, by inference, to the phytoplankton community in general. In contrast, bioavailable N comprises most of the dissolved N pool. Consequently, bioavailable N : P ratios based on these assays are higher then those based on chemical determinations, indicating that P limitation in Lake Kinneret is more extensive then previously thought.     

Bioavailability and composition of dissolved organic carbon and nitrogen in a near coastal catchment of south-western Australia

The bioavailability and composition of dissolved organic carbon (DOC) and nitrogen (DON) were examined in 10 major sub-catchments of the Swan-Canning estuary, which bisects the city of Perth, in south-western Australia. Catchments contain a mix of forest, agriculture, and urban-dominated land-use, with the degree of development increasing near the city center. We incubated water samples from the 10 sub-catchments for 14 days at 25°C, and measured changes in DOC and DON and dissolved inorganic nitrogen (DIN). A greater proportion of DON (4–44%) was decomposed compared to DOC (1–17%). Both agricultural and urban catchments had high proportions of bioavailable DOC and DON, but overall DOC and DON losses were greatest in urban catchments. Using resin isolation techniques, we found that DOC was concentrated in the hydrophobic (humic) fraction, whereas DON had both hydrophobic and hydrophilic (non-humic) fractions. Hydrophobic DOC content was positively related to DOC decomposition. In contrast, DON decomposition was highly correlated with hydrophilic DON content and inversely related to the hydrophilic DOC/DON ratio, indicating a labile fraction of DON from non-humic sources. Taken together, these relationships suggest that bioavailable DOC may be supplied in part from terrestrial plant material, but bioavailable DON is likely to be from highly labile sources, possibly autochthonous or anthropogenic. Overall, labile DON was greater than initial DIN concentration at seven of ten sites and was even dominant in highly developed catchments. This study highlights the importance of organic N in urbanizing coastal catchments that, in addition to DIN, may serve as a readily available source of N for in-stream and estuarine production.     

Exploration of orally available calpain inhibitors. Part 3: Dipeptidyl alpha-ketoamide derivatives containing pyridine moiety

Calpain-mediated proteolysis has been implicated as a major process in neuronal cell death including retinal neurological degeneration. The previously reported calpain inhibitor SJA6017 (1) showed oral efficacy in a retinal pharmacological model, but its oral bioavailability was low due to the metabolic lability and low water-solubility. The purpose of present study was to identify good orally bioavailable calpain inhibitors. A series of water-soluble dipeptidyl alpha-ketoamides containing a pyridine moiety at P3 were designed, synthesized, and evaluated for their oral bioavailability and retinal penetration. Introduction of a pyridineethanol moiety provided the potent alpha-ketoamide inhibitor 8 with good oral bioavailability. Compound 8 showed about 12-fold higher retinal AUC than 1.     

Rare earth elements and relation between their potential bioavailability and soil properties, Nidda catchment (Central Germany)

Rare earth elements (REEs) are widely used in industry and the entry of REEs into the pedosphere is assumed. Data about REEs in soils are scarce since only a few studies discuss their ecologically relevant behavior. Hence, we investigated total contents (aqua regia digestion) and potentially bioavailable contents (EDTA extraction) of REEs in soils from the Nidda catchment in Hesse (Central Germany). The study site covers a 1,600 km² sized area and 232 soil samples from 63 soil profiles were examined. The total REE content varied considerably, ranging from 544 mg kg^?1 to 41 mg kg^?1 (mean 201.1 mg kg^?1) with a high proportion of light REEs. Highest REE contents were found in the soilscape VB, followed by LVB, WNE, T, WSW and BF with the smallest concentrations. With respect to the parent material the contents decreased in the following order: basalt > clay slate > loess > sandstone. On average 15.9% of the total REEs belong to the potentially bioavailable fraction. They range greatly by a factor of 100, between 1.3 and 171.3 mg kg^?1 (average 33.5 mg kg^?1). Remarkably, Yttrium has a maximum available proportion of 75%. In contrast, Ce showed the highest total contents with the smallest potentially bioavailable proportion of all elements. Regression analyses established relation between soil properties and the potential bioavailability of REEs. Around 53% (range from 29.9 to 76.8%) of the REE’s potential bioavailability variations could be explained by the chosen variables (pH, clay and C_org contents and the total element concentrations). Occurrence patterns and concentrations of REEs lie within the range of the results found in the available literature. Bioavailability is linked to soil properties and varies greatly according to the individual element. In comparison with the chosen soil properties the pH value shows the least impact on bioavailability.     

The composition and bioavailability of phosphorus transport through the Changjiang (Yangtze) River during the 1998 flood

Water and suspended sediment (SS) samples were collected from the Changjiang River at the Datong Hydrological Station (DHS), five times from May 1997 through January 1999 in order to evaluate transport, composition and bioavailability of phosphorus (P) during a 1998 flood. Transport of most of the phosphorus compositions was substantially higher during the 1998 flood than at other sampling dates. Phosphorus associated with suspended sediment (TPP) accounted for more than 85% of total phosphorus (TP) transport during periods of preflood and flood. The high transport of TPP during the flood was due to unusually high concentrations of TPP and sediment discharge. The potentially bioavailable phosphorus in SS (PBAP) accounted for about 10% of TPP. PBAP with dissolved inorganic phosphorus (DIP) consisted of 15–89% of TP. For all the sampling dates, the concentrations of potential bioavailable phosphorus (BAP) ranged from 0.035–0.08 mg L^–1, significantly higher than the limiting concentration for eutrophication. Therefore, the increasing temporal trends of TP concentration and high bioavailability of TP appear to support more frequent algal blooms in receiving East China Sea coastal waters in recent years. Hence, the underestimate of TPP transport by large rivers may also underestimate the biogeochemical cycling of other associated nutrients, such as nitrogen and carbon.