Understanding the interacting factors that determine ecological effectiveness of terrestrial protected areas

Protected areas are recognized as an essential tool to safeguard habitat integrity and biodiversity in the Anthropocene. Substantial efforts have been made to clarify the conditions under which they deliver conservation outcomes effectively. Location, spatial design, management strategy and threats, have commonly been identified as key factors. The impacts of these factors have, however, often been evaluated independently, and there is limited information on how their combined and interactive effects can improve or hinder protected area effectiveness. Here we develop a framework for understanding the combined effects of these factors. This has important implications for how protected areas are established and maintained.     

Leucoflavonine,a new bioactive racemic flavoalkaloid from the leaves of Leucosceptrum canum

A new flavoalkaloid racemate, leucoflavonine (1), together with its flavonoid precursor pectolinarigenin (2), was isolated from the leaves of Leucosceptrum canum collected from Tibet. Its structure was established by comprehensive spectroscopic analysis. Chrial separation of the enantiomers of 1 was achieved, and their absolute configurations were determined as S-(+)- and R-(?)-leucoflavonines ((+)-1a and (?)-1b) by comparison of their computational and experimental optical rotations. Biological assays indicated that both (+)-1a and (?)-1b exhibited inhibitory activity against acetylchlorinesterase (AChE) in vitro (IC₅₀?=?68.0?±?8.6 and 18.3?±?1.8?μM, respectively). Moreover, (?)-1b displayed cytotoxicity against human hepatoma cells HepG2 (IC₅₀?=?52.9?±?3.6?μM), and inhibited the production of interleukelin-2 (IL-2) in Jurkat cells (IC₅₀?=?16.5?±?0.9?μM), while (+)-1a showed no obvious activity in these assays.     

Synthesis and urease inhibitory potential of benzophenone sulfonamide hybrid in vitro and in silico

This study deals with the synthesis of benzophenone sulfonamides hybrids (1–31) and screening against urease enzyme in vitro. Studies showed that several synthetic compounds were found to have good urease enzyme inhibitory activity. Compounds 1 (N′-((4′-hydroxyphenyl)(phenyl)methylene)-4′′-nitrobenzenesulfonohydrazide), 2 (N′-((4′-hydroxyphenyl)(phenyl)methylene)-3′′-nitrobenzenesulfonohydrazide), 3 (N′-((4′-hydroxyphenyl)(phenyl)methylene)-4′′-methoxybenzenesulfonohydrazide), 4 (3′′,5′′-dichloro-2′′-hydroxy-N′-((4′-hydroxyphenyl)(phenyl)methylene)benzenesulfonohydrazide), 6 (2′′,4′′-dichloro-N′-((4′-hydroxyphenyl)(phenyl)methylene)benzenesulfonohydrazide), 8 (5-(dimethylamino)-N′-((4-hydroxyphenyl)(phenyl)methylene)naphthalene-1-sulfono hydrazide), 10 (2′′-chloro-N′-((4′-hydroxyphenyl)(phenyl)methylene)benzenesulfonohydrazide), 12 (N′-((4′-hydroxyphenyl)(phenyl)methylene)benzenesulfonohydrazide) have found to be potently active having an IC₅₀ value in the range of 3.90–17.99?µM. These compounds showed superior activity than standard acetohydroxamic acid (IC₅₀?=?29.20?±?1.01?µM). Moreover, in silico studies on most active compounds were also performed to understand the binding interaction of most active compounds with active sites of urease enzyme. Structures of all the synthetic compounds were elucidated by ¹H NMR, ¹³C NMR, EI-MS and FAB-MS spectroscopic techniques.     

Solid state fermentation,storage and viability of Streptomyces similanensis 9X166 using agro-industrial substrates against Phytophthora palmivora-induced black rot disease in orchids

Streptomyces similanensis 9X166 is known to be an antagonist of the black rot pathogen of orchids, Phytophthora palmivora. In this study, we investigated the production of highly viable S. similanensis 9X166 cells by solid state fermentation using agro-industrial substrates, and the shelf life of a S. similanensis 9X166 dried solid. Rice bran was found to be the most appropriate raw material for production of both viable cells and β-1,3-glucanase. A medium containing 12?g of rice bran and coconut husks at a ratio of 10:2, supplemented with 10?mL of mineral salts produced the highest number of viable cells and greatest level of β-1,3-glucanase. Ammonium sulfate was the most suitable nitrogen source, and an initial moisture content of 65% and a temperature of 30°C were found to be optimal conditions for the production of viable cells and β-1,3-glucanase. Storing the dried fermented solid under non-vacuum conditions resulted in the highest cell viability. The specific rate of degradation on viability increased as the temperature increased to 37°C, according to the Arrhenius equation. There was no difference between the storage time estimated by the Arrhenius equation from the specific rate of degradation compared to the validated storage time of S. similanensis 9X166 dried solids when maintained at the ambient temperature in Thailand. At 60 days, the product retained 10⁶ CFU/g of S. similanensis 9X166 in dried solid, which was the minimal effective amount for 100% inhibition of P. palmivora in living orchids.     

Recent developments in the synthesis and applications of phosphinic peptide analogs

Synthetic pseudopeptides that fit well with the active site architecture allow the most effective binding to enzymes, similar to native substrates in high-energy transition states. Phosphinic acid peptide analogs that comprise the tetrahedral phosphorus moiety introduced to replace an internal amide bond exert such an isosteric or isoelectronic resemblance, combined with providing other advantageous features, for example, metal complexing properties. Accordingly, they are capable of inhibiting metal-dependent enzymes involved in biological functions in eukaryotic and prokaryotic cells. These enzymes are associated with notorious human diseases, such as cancer, e.g., matrix metalloproteinases, or are etiological factors of protozoal and bacterial infections, e.g., metalloaminopeptidases. The affinity and selectivity of these compounds can be conveniently adjusted, either by structural modification of dedicated side chains or by backbone elongation to enhance specific interactions with the corresponding binding pockets. Recent approaches to the synthesis of these compounds are illustrated by examples of the preparation of rationally designed structures of inhibitors of particular enzymes. Activity against appealing enzymatic targets is presented, along with the molecular mechanisms of action and therapeutic implications. Innovative aspects of phosphinic peptide application, e.g., as activity-based probes, and ligands of complexes of radioisotopes for nuclear medicine are also outlined.     

Synthesis and biological activities evaluation of sanjuanolide and its analogues

Sanjuanolide, psorachalcone A and its seven new analogues were synthesized via a combinatorial strategy by aldol reaction. In order to investigate the effect between electron density in π-conjugated systems and biological activities, several electron-withdrawing and electron-donating groups were introduced at C-4 and the phenolic hydroxyl groups of sanjuanolide. The two natural products and its seven new analogues were investigated for their inhibitory effects against five cancer cell lines. Moreover, the hydroxyisoprenyl group may be important to maintain the biological activities of sanjuanolide.     

Birth weight and physical stature in St. Petersburg: Living standards of women in Russia, 1980–2005

We analyze data on the height and weight of mothers and newborn babies between 1980 and 2005 in St. Petersburg, Russia. We find that women's living standards, as measured by their height, improved steadily from the end of World War II through those born in 1972, hence reached adulthood in 1990. Thereafter, heights declined. Evidence on both the length and weight of babies corroborates this pattern. Their values trace a "U" shaped curve with troughs near the mid-1990s. Thus, the anthropometric results on newborn as well as for their mother point to the strains and challenges to living standards experienced during the restructuring of the post-Soviet economy. This is a general result that has become a recurring pattern: economic transitions are almost always accompanied by biological strains.     

Discovery of Substituted Human Urocortin 1 Analogs with Improved CRF2 Receptor Selectivity and Increased Efficacy in Preventing Skeletal Muscle Atrophy

We have identified specific amino acid modifications of human Urocortin 1 (hUCN1) that lead to highly potent and selective Corticotropin Releasing Factor Receptor 2 (CRF2R) agonists that are efficacious in preventing skeletal muscle atrophy in animal models. We have demonstrated that the CRF2R versus CRF1R selectivity can be increased by modifying the 40 amino acid hUCN1 at amino acid positions 11, 12, 13, 35 and 39. Further improvement in drug properties, including reduced binding to the CRF binding protein, improved solubility, and improved in vivo potency, were achieved by modifying amino acids at positions 22, 23, 36, and 40. In vivo investigations of selected optimized hUCN1 analogs demonstrated significant anti-atrophy efficacy in a mouse casting model of hind leg muscle disuse atrophy.     

A fibre reorientation model for orthotropic multiplicative growth

The main goal of this contribution consists in the development of a remodelling framework for orthotropic continua whereby the underlying symmetry group is incorporated via two fibre families. Special emphasis is placed on the modelling of biological tissues at finite deformations. Besides the incorporation of a referential mass source, anisotropic growth is addressed by means of a multiplicative decomposition of the overall deformation gradient into an elastic and a growth distortion. Projected quantities of a configurational growth stress tensor are advocated as driving forces for time-dependent saturation–type evolution of the principal values of the growth distortion. Moreover, the reorientation of both fibre families, which directly affects the strain energy as well as the growth distortion itself, is guided by analyzing critical energy points. In particular, a time-dependent formulation is developed which aligns the fibre directions according to the principal stretch directions. Finally, the proposed framework is embedded into a finite element context so that representative numerical examples, examining growth and resorption in volume and density together with fibre reorientation, close this study.