Active Transport of Hepatotoxic Pyrrolizidine Alkaloids in HepaRG Cells

1,2-unsaturated pyrrolizidine alkaloids (PAs) are secondary plant metabolites occurring as food contaminants that can cause severe liver damage upon metabolic activation in hepatocytes. However, it is yet unknown how these contaminants enter the cells. The role of hepatic transporters is only at the beginning of being recognized as a key determinant of PA toxicity. Therefore, this study concentrated on assessing the general mode of action of PA transport in the human hepatoma cell line HepaRG using seven structurally different PAs. Furthermore, several hepatic uptake and efflux transporters were targeted with pharmacological inhibitors to identify their role in the uptake of the PAs retrorsine and senecionine and in the disposition of their N-oxides (PANO). For this purpose, PA and PANO content was measured in the supernatant using LC-MS/MS. Also, PA-mediated cytotoxicity was analyzed after transport inhibition. It was found that PAs are taken up into HepaRG cells in a predominantly active and structure-dependent manner. This pattern correlates with other experimental endpoints such as cytotoxicity. Pharmacological inhibition of the influx transporters Na⁺/taurocholate co-transporting polypeptide (SLC10A1) and organic cation transporter 1 (SLC22A1) led to a reduced uptake of retrorsine and senecionine into HepaRG cells, emphasizing the relevance of these transporters for PA toxicokinetics.     

Increasing Volumetric CO2 Uptake of Hypercrosslinked Polymers through Composite Formation

To overcome the drawbacks of solid microporous materials for CO₂ capture, this proof‐of‐concept study demonstrates a low‐cost and rapid method for producing composites consisting of hypercrosslinked polymers (HCP) with a polyethyleneimine (PEI) binder. The resulting materials capture CO₂ through physical and chemical absorption simultaneously. Compared with HCP, the composites exhibit higher CO₂ uptake, higher volumetric density, and improved tolerance to water which is attributed to the PEI binder.     

Ocular conditions and dry eye due to traditional and new forms of smoking: A review

Addiction to cigarette smoking has high prevalence rates recorded worldwide. Smoking has been linked to several life-threatening systemic conditions such as cancer, heart attack and stroke, in addition to a range of ocular pathologies. In recent years, electronic cigarettes (EC) have emerged as alternatives to smoking. ECs are nicotine delivery devices which produce an aerosol by heating, rather than combusting, a liquid which contains nicotine, flavours and preservatives. This review focuses on the association of traditional and new forms of smoking with dry eye disease, contact lens wear and four other common ocular diseases: cataract, age-related macular degeneration, glaucoma and Graves’ ophthalmopathy. It is concluded that smoking and vaping appear as a risk factor for the aforementioned ocular conditions. An evidence-based, clear link between cigarette smoking, or EC vaping and ocular problems is yet to be discovered.     

Characteristics of tiger nut milk: effects of milling

A standard method for the extraction of tiger nut milk has been introduced. It has been shown that, although milling duration improves the yield of tiger nut milk solids and its nutrient composition, there is a quantifiable loss of nutrient in the pressing residue during milk extraction. Milling duration improved the colloidal stability of the milk against creaming during 16 h of storage. A higher milling intensity resulted in the aggregation of biological polymers which resulted in colloidal destabilisation. Milling improved the lightness and stability and reduced browning rate of the tiger nut milk during storage. This report is important for the production of tiger nut milk of consistent and comparable characteristics. Milling has been introduced as a processing method for the qualitative and quantitative modulation of the properties of tiger nut milk. It is recommended to develop further strategies to improve the colloidal stability of tiger nut milk as a beverage.     

N-Substituted Nipecotic Acids as (S)-SNAP-5114 Analogues with Modified Lipophilic Domains

Potential mGAT4 inhibitors derived from the lead substance (S)-SNAP-5114 have been synthesized and characterized for their inhibitory potency. Variations from the parent compound included the substitution of one of its aromatic 4-methoxy and 4-methoxyphenyl groups, respectively, with a more polar moiety, including a carboxylic acid, alcohol, nitrile, carboxamide, sulfonamide, aldehyde or ketone function, or amino acid partial structures. Furthermore, it was investigated how the substitution of more than one of the aromatic 4-methoxy groups affects the potency and selectivity of the resulting compounds. Among the synthesized test substances (S)-1-{2-[(4-formylphenyl)bis(4-methoxyphenyl)-methoxy]ethyl}piperidine-3-carboxylic acid, that features a carbaldehyde function in place of one of the aromatic 4-methoxy moieties of (S)-SNAP-5114, was found to have a pIC₅₀ value of 5.89±0.07, hence constituting a slightly more potent mGAT4 inhibitor than the parent substance while showing comparable subtype selectivity.     

Lake Chivero: A management case study

Lake Chivero in Zimbabwe was shown to be hypereutrophic. Historical data showed that the eutrophication process had been arrested in the late 1970s. However, a combination of poor planning, multiplicity of jurisdiction, mismatch between rate of urbanization and waste management investment, recent changes in the local climate and a permissive, immature political system that called for no public accountability resulted in environmental management breakdown leading to hypereutrophication of the lake. The case of Lake Chivero is presented as an example of a wider global issue regarding the status of environmental management in competition with other priorities in emerging democracies.     

Influences of land use/cover on water quality in the upper and middle reaches of River Njoro, Kenya

Data from 10 sampling sites along the River Njoro are used to examine the contribution of nutrients from upstream land uses draining each of the sampling sites. The data also are used to assess whether both the proportion of land uses and the size of the subwatersheds account for the variability in water quality in the River Njoro watershed. Geographical Information System analysis was used to determine the spatial distribution of land‐cover types and subwatersheds contributing run‐off to the sampling sites in the River Njoro. Standard Digital Elevation Model‐based routines were used to establish the watershed area contributing run‐off to each sampling site. Water and sediment samples were collected for chemical analysis, and the nutrient levels were related to the upstream land‐use types and the size of the subwatersheds. The mid‐stream portion of the River Njoro (near Egerton University) accounts for the highest nutrient contributions. The percentage contribution is magnified by additions from industrial, human settlements and agricultural land uses around the University. There is a significant decrease in nutrient levels downstream, however, indicating natural purification as the river flows through an area of large‐scale farming with intense, well‐preserved riparian and in‐stream vegetation. Steep slopes of the land upstream of Egerton University enhance erosion and nutrient losses from those subwatersheds. Mixed small‐scale agricultural and bare lands contribute over 55% of the phosphorus load to the upper and mid‐reaches of the River Njoro. The size of the subwatershed accounts for about 53% of the variability in the soluble phosphorus in the river. The land‐use subwatershed proportions are important for characterizing and modelling water quality in the River Njoro watershed. Upland land uses are as important as near‐stream land uses. We suggest that conservation of intact riparian corridor along the river and its tributaries contributes significantly to natural purification processes and recovery of the ecological integrity of the River Njoro ecosystem.     

Sorption of Acid Green 25 on chitosan: Influence of experimental parameters on uptake kinetics and sorption isotherms

Acid Green 25, which is a diazoic dye bearing two sulfonic groups, is efficiently sorbed on chitosan. The protonation of chitosan may explain the electrostatic attraction of this anionic dye and that its optimum pH is close to 3. Preliminary protonation of amine groups (obtained by contact with a sulfuric acid solution) reduced the variation of solution pH following sorbent addition but significantly reduced sorption performance: the maximum sorption capacity of raw chitosan, 525 mg dye/g (0.84 mmol dye/g), was halved by acidic preconditioning. The acidic conditioning also reduced the kinetic rate—the time necessary to reach equilibrium increased up to threefold depending on the experimental conditions. The size of sorbent particles influenced sorption kinetics and equilibrium because of resistance to intraparticle diffusion, but the sorption appeared to occur not only at the surface of the sorbent but also in the intraparticle network of the polymer. © 2003 Wiley Periodicals, Inc. J Appl Polym Sci 90: 1073–1080, 2003     

Synthetic resins: XV. Chelation ion exchange properties of 2,4- dinitrophenylhydrazone of resacetophenone-formaldehyde resin

A number of copolymers were synthesised by condensing the 2,4-dinitrophenylhydrazone of resacetophenone with substituted benzoic acids/ phenols and formaldehyde in the presence of sodium hydroxide or hydrochloric acid. The decomposition temperature, solubility and viscosity of the polymers have been determined. The ion-exchange properties have been studied by using a batch equilibrium method. The distribution of a number of metal ions between an aqueous solution and the resin have been measured. A wide range of pH and variable ionic strengths have been investigated.