The simplified nutrient profiling system (SENS) adequately ranks foods in relation to the overall nutritional quality of diets: a validation study.

Background/objectives: We aimed to validate the simplified nutrient profiling system (SENS) algorithm based on its ability to rank foods across the four SENS classes in relation to overall nutritional quality of both observed diets and nutritionally optimized diets.

Subjects/methods: Foods and beverages from the French nutritional composition database were classified according to SENS. Diets consumed by French adults in the latest national dietary survey (>19 years, n = 1719) were divided into four nutritional quality levels, and average daily frequencies (number of portions per day) of foods from the four SENS classes were compared between the four levels.

The SENS algorithm-a new nutrient profiling system for food labelling in Europe.

Background/objectives: In response to the European regulation on nutrition and health claims, France proposed in 2008 the SAIN,LIM profiling system that classifies foods into four classes based on a nutrient density score called 'SAIN', a score of nutrients to limit called 'LIM', and one primary threshold on each score. We present here the SENS algorithm, a new nutrient profiling system adapted from the SAIN,LIM to be operational for simplified nutrition labelling in line with the European regulation on food information to consumers.

Subjects/methods: The main changes made to SAIN,LIM to get SENS were to introduce food categories and sub-categories ('Beverages', 'Added Fats' and 'Other Solid Foods' sub-categorised into 'cereals', 'cheese', 'other dairy products', 'eggs', 'fish' and 'others'), reduce the number of nutrients, introduce category-specific nutrients and category-specific weighting for some nutrients, replace French recommendations with European reference intakes, and add secondary thresholds.

Drinking Water Intake Is Associated with Higher Diet Quality among French Adults.

This study aimed to examine the association between drinking water intake and diet quality, and to analyse the adherence of French men and women to the European Food Safety Authority 2010 Adequate Intake (EFSA AI). A representative sample of French adults (≥18) from the Individual and National Survey on Food Consumption (INCA2) was classified, by sex, into small, medium, and large drinking water consumers. Diet quality was assessed with several nutritional indices (mean adequacy ratio (MAR), mean excess ratio (MER), probability of adequate intakes (PANDiet), and solid energy density (SED)).

Fully Synthetic Granulocyte Colony-Stimulating Factor Enabled by Isonitrile-Mediated Coupling of Large, Side-Chain-Unprotected Peptides.

Human granulocyte colony-stimulating factor (G-CSF) is an endogenous glycoprotein involved in hematopoiesis. Natively glycosylated and nonglycosylated recombinant forms, lenograstim and filgrastim, respectively, are used clinically to manage neutropenia in patients undergoing chemotherapeutic treatment. Despite their comparable therapeutic potential, the purpose of O-linked glycosylation at Thr133 remains a subject of controversy.

3-substituted thieno[2,3-b][1,4]thiazine-6-sulfonamides. A novel class of topically active carbonic anhydrase inhibitors.

3-Aminoalkyl derivatives of thieno[2,3-b][1,4]thiazine-6-sulfonamide were prepared for evaluation as topically active ocular hypotensive agents. The compounds described were found to be excellent in vitro inhibitors of carbonic anhydrase II and in vivo to lower intraocular pressure in three rabbit models of ocular hypertension. Compounds 20A, 20B, and 20C met the requirement of formulation as a 1% solution at pH 5.

Sulfonylmethanesulfonamide inhibitors of carbonic anhydrase.

A series of sulfonylmethanesulfonamide derivatives is described, which are inhibitors of carbonic anhydrase (CA). The most potent of these is the racemic fluoro sulfone 9, which inhibits carbon dioxide hydration catalyzed by human CA II (CA-II) with an IC50 of 3 nM. Binding competition studies versus dansylamide indicate that the enantiomers of 9 have different affinities for CA-II, with equilibrium dissociation constants of 3.

4-substituted thiophene- and furan-2-sulfonamides as topical carbonic anhydrase inhibitors.

A series of 4-substituted thiophene- and furan-2-sulfonamides was prepared and was found to possess nanomolar-level potency for inhibition of human carbonic anhydrase II in vitro. Selected examples from this group were further evaluated for their potential to act as topically effective ocular hypotensive agents in the ocular normotensive albino rabbit and the ocular alpha-chymotrypsinized rabbit. Solubility studies in water and pH 7.

Thieno[2,3-b]furan-2-sulfonamides as topical carbonic anhydrase inhibitors.

Novel 5-[(alkylamino)methyl]thieno[2,3-b]furan-2-sulfonamides were prepared and evaluated in vitro for inhibition of human carbonic anhydrase II (CA II) and ex vivo for their ability to inhibit Ca II in the albino rabbit eye after topical administration. Compound 11a was found to lower intraocular pressure (IOP) in both the alpha-CT ocular hypertensive albino rabbit and the normal albino rabbit, but was ineffective at lowering IOP in a hypertensive, pigmented monkey model. Since 11a was highly bound to ocular pigment, a series of less basic analogs was prepared.

Topically active carbonic anhydrase inhibitors. 4. [(Hydroxyalkyl)sulfonyl]benzene and [(hydroxyalkyl)sulfonyl]thiophenesulfonamides.

For several decades a tantalizing goal for the treatment of primary open-angle glaucoma has been the development of a topically active carbonic anhydrase inhibitor. Recent results from several research groups indicate that considerable progress has been made toward this objective. In this report, we present the design and synthesis of (hydroxyalkyl)sulfonyl-substituted benzene- and thiophenesulfonamides.

New isomeric classes of topically active ocular hypotensive carbonic anhydrase inhibitors: 5-substituted thieno[2,3-b]thiophene-2-sulfonamides and 5-substituted thieno[3,2-b]thiophene-2-sulfonamides.

A series of 5-substituted thieno[2,3-b]- and thieno[3,2-b)- and thieno[3,2-b)thiophene-2-sulfonamides was prepared and evaluated for topical ocular hypotensive activity in glaucoma models. The 5-substituents were varied to maximize both inhibitory potency against carbonic anhydrase and water solubility. At the same time, these substituents were varied in order to obtain compounds with the appropriate pKa to minimize pigment binding in the iris.

Topically active carbonic anhydrase inhibitors. 3. Benzofuran- and indole-2-sulfonamides.

Derivatives of benzofuran- and indole-2-sulfonamide were prepared for evaluation as topically active ocular hypotensive agents. These compounds were found to be excellent inhibitors of carbonic anhydrase and to lower intraocular pressure in a rabbit model of ocular hypertension. However, the development of these compounds for clinical use was precluded by the observation that they cause dermal sensitization in guinea pigs.

Dihydrofolate reductase: the amino acid sequence of the enzyme from a methotrexate-resistant mutant of Escherichia coli.

The determination of the amino acid sequence of the enzyme dihydrofolate reductase (5,6,7,8-tetrahydrofolate:NADP+ oxidoreductase, EC 1.5.1.