Synthesis, crystal structure, DNA interaction and cleavage activities of mononuclear and trinuclear copper(II) complexes

Mono- and trinuclear copper(II) complexes with 2-1-(2-dimethylamino-ethylamino)-ethyl]-phenol (HL) have been synthesized and structurally characterized. The mononuclear complex Cu(L)(H2O)(ONO2)] (1) crystallizes in monoclinic space group P2(1) /n with a square pyramidal Cu(II) center coordinated by the tridentate Schiff base (L) and a water ligand in the equatorial plane and an oxygen atom from nitrate in the axial position. The trinuclear complex (CuL)(3)(mu(3)-OH)](ClO4)(2)center dot H2O (2) crystallizes in hexagonal space group P6(3); all three copper atoms are five-coordinate with square pyramidal geometries. The interactions of these complexes with calf-thymus DNA have been investigated using absorption spectrophotometry. The mononuclear complex binds more strongly than the trinuclear complex. The DNA cleavage activity of these complexes has been studied on double-stranded pBR 322 plasmid DNA by gel electrophoresis experiments in the absence and in the presence of added oxidant (H2O2). The trinuclear complex cleaves DNA more efficiently than the mononuclear complex in the presence of H2O2.

Synthesis, antimicrobial and cytotoxic activities of pyrimidinyl benzoxazole, benzothiazole and benzimidazole

A variety of pyrimidinyl benzoxazoles, benzothiazoles and benzimidazoles linked by thio, methylthio and amino moieties were prepared and studied their antimicrobial and cytotoxic activities. The compound pyrimidinyl bis methylthio benzimidazole 22 was a potent antimicrobial agent particularly against Staphylococcus aureus (29 mm, MIC 12.5 mu g/mL) and Penicillium chrysogenum (38 mm, MIC 12.5 mu g/mL). The amino linked pyrimidinyl bis benzothiazole 24 exhibited cytotoxic activity on A549 cells with IC50 value of 10.5 mu M. (C) 2014 Elsevier Masson SAS. All rights reserved.

Synthesis and Antioxidant Activities of Novel Chiral Ebselen Analogues

Novel chiral analogues of the antioxidant, anti-inflammatory organoselenium drug ebselen were synthesized. The reaction proceeded readily from 2-(chloroseleno)benzoyl chloride with chiral amino compounds. The chiral substituent on the nitrogen atom did not provide a substantial increase in activities and the newly synthesized compounds showed similar activities to ebselen.

Synthesis, antioxidant, and cytotoxic activities of bis(oxazolyl/thiazolyl/imidazolyl)amidomethanesulfonyl Acetamides

A new class of bis(oxazolyl/thiazolyl/imidazolyl)amidomethanesulfonyl acetamides was prepared from the respective (oxazolyl/thiazolyl/imidazolyl)carbamoyl-methylthio acetic acid and studied their antioxidant activity and cytotoxic activitity against A549 lung adenocarcinoma cells. The methyl-substituted sulfonyl bisoxazoles exhibited excellent radical scavenging activity. On the other hand, the chloro-substituted sulfonyl bisthiazoles (IC50 = 49 A mu M) and sulfonyl bisimidazoles (IC50 = 24 A mu M) showed noticeable cytotoxic activity on A549 cells.

Evaluation of anti-obesity activities of ethanolic extract of Terminalia paniculata bark on high fat diet-induced obese rats

Background: The prevalence and severity of obesity and associated co-morbidities are rapidly increasing across the world. Natural products-based drug intervention has been proposed as one of the crucial strategies for management of obesity ailments. This study was designed to investigate the anti-obesity activities of ethanolic extract of Terminalia paniculata bark (TPEE) on high fat diet-induced obese rats. Methods: LC-MS/MS analysis was done for ethanolic extract of T. paniculata bark. Male Sprague-Dawley (SD) rats were randomly divided into six groups of six each, normal diet fed (NC), high fat diet-fed (HFD), HFD+ orlistat (standard drug control) administered, and remaining three groups were fed with HFD + TPEE in different doses (100,150 and 200 mg/kg b. wt). For induction of obesity rats were initially fed with HFD for 9 weeks, then, (TPEE) was supplemented along with HFD for 42 days. Changes in body weight, body composition, blood glucose, insulin, tissue and serum lipid profiles, atherogenic index, liver markers, and expression of adipogenesis-related genes such as leptin, adiponectin, FAS, PPARgamma, AMPK-1alpha and SREBP-1c, were studied in experimental rats. Also, histopathological examination of adipose tissue was carried out. Results: Supplementation of TPEE reduced significantly (P < 0.05) body weight, total fat, fat percentage, atherogenic index, blood glucose, insulin, lipid profiles and liver markers in HFD-fed groups, in a dose-dependent manner. The expression of adipogenesis-related genes such as Leptin, FAS, PPARgamma, and SREBP-1c were down regulated while Adiponectin and AMPK-1alpha were up regulated in TPEE + HFD-fed rats. Furthermore, histopathological examination of adipose tissue revealed the alleviating effect of TPEE which is evident by reduced size of adipocytes. Conclusions: Together, the biochemical, histological and molecular studies unambiguously demonstrate the potential anti adipogenic and anti obesity activities of TPEE promoting it as a formidable candidate to develop anti obesity drug.

The nuclease activities of both the Smr domain and an additional LDLK motif are required for an efficient anti-recombination function of Helicobacter pyloriMutS2

Helicobacter pylori, a human pathogen, is a naturally and constitutively competent bacteria, displaying a high rate of intergenomic recombination. While recombination events are essential for evolution and adaptation of H.pylori to dynamic gastric niches and new hosts, such events should be regulated tightly to maintain genomic integrity. Here, we analyze the role of the nuclease activity of MutS2, a protein that limits recombination during transformation in H.pylori. In previously studied MutS2 proteins, the C-terminal Smr domain was mapped as the region responsible for its nuclease activity. We report here that deletion of Smr domain does not completely abolish the nuclease activity of HpMutS2. Using bioinformatics analysis and mutagenesis, we identified an additional and novel nuclease motif (LDLK) at the N-terminus of HpMutS2 unique to Helicobacter and related epsilon-proteobacterial species. A single point mutation (D30A) in the LDLK motif and the deletion of Smr domain resulted in approximate to 5-10-fold loss of DNA cleavage ability of HpMutS2. Interestingly, the mutant forms of HpMutS2 wherein the LDLK motif was mutated or the Smr domain was deleted were unable to complement the hyper-recombination phenotype of a mutS2(-) strain, suggesting that both nuclease sites are indispensable for an efficient anti-recombinase activity of HpMutS2.

Structural characterization and in vitro biomedical activities of sulfated chitosan from Sepia pharaonis

A low molecular weight sulfated chitosan (SP-LMWSC) was isolated from the cuttlebone of Sepia pharaonis. Elemental analysis established the presence of C, H and N. The sulfation of SP-LMWSC was confirmed by the presence of characteristic peaks in FT-IR and FT-Raman spectra. The thermal properties of SP-LMWSC were studied by thermogravimetric analysis and differential scanning calorimetry. Electrolytic conductivity of SP-LMWSC was measured by cyclic voltammetry and the molecular weight was determined by MALDI-TOF/MS. The molecular structure and sulfation sites of SP-LMWSC were unambiguously confirmed using H-1,C-13, 2D COSY and 2D HSQC NMR spectroscopy. SP-LMWSC exhibited increased anticoagulant activity in avian blood by delaying coagulation parameters and displayed cytostatic activity by inhibiting the migration of avian leucocytes. SP-LMWSC demonstrated avian antiviral activity by binding to Newcastle disease virus receptors at a low titer value of 1/64. These findings suggested that SP-LMWSC isolated from an industrial discard holds immense potentials as carbohydrate based pharmaceuticals in future. (C) 2015 Elsevier B.V. All rights reserved.

In vitro activities of natural products against oral Candida isolates from denture wearers

Background: Candida-associated denture stomatitis is a frequent infectious disease. Treatment of this oral condition is difficult because failures and recurrences are common. The aim of this study was to test the in vitro antifungal activity of pure constituents of essentials oils. -- Methods: Eight terpenic derivatives (carvacrol, farnesol, geraniol, linalool, menthol, menthone, terpinen-4-ol, and aterpineol), a phenylpropanoid (eugenol), a phenethyl alcohol (tyrosol) and fluconazole were evaluated against 38 Candida isolated from denture-wearers and 10 collection Candida strains by the CLSI M27-A3 broth microdilution method. -- Results: Almost all the tested compounds showed antifungal activity with MIC ranges of 0.03-0.25% for eugenol and linalool, 0.03-0.12% for geraniol, 0.06-0.5% for menthol, a-terpineol and terpinen-4-ol, 0.03-0.5% for carvacrol, and 0.06-4% for menthone. These compounds, with the exception of farnesol, menthone and tyrosol, showed important in vitro activities against the fluconazole-resistant and susceptible-dose dependent Candida isolates. -- Conclusions: Carvacrol, eugenol, geraniol, linalool and terpinen-4-ol were very active in vitro against oral Candida isolates. Their fungistatic and fungicidal activities might convert them into promising alternatives for the topic treatment of oral candidiasis and denture stomatitis.

Illustrated key to the genera of free-living marine nematodes of the Order Enoplida

A pictorial key to US genera of free-living marine nematodes in the order Enoplida is presented. Specific morphological and anatomical features are iUustrated to facilitate use of the key. The purpose of this work is to provide a single key to the genera of enoplid nematodes to facilitate identification of these organisms by nematologists and marine biologists working with meiofauna. (PDF file contains 32 pages.)

Reconstructing an 83-Year Time Series of Daily Sea Surface Temperature at Pacific Grove, California

Daily sea surface temperatures have been acquired at the Hopkins Marine Station in Pacific Grove, California since January 20, 1919.This time series is one of the longest oceanographic records along the U.S. west coast. Because of its length it is well-suited for studying climate-related and oceanic variability on interannual, decadal, and interdecadal time scales. The record, however, is not homogeneous, has numerous gaps, contains possible outliers, and the observations were not always collected at the same time each day. Because of these problems we have undertaken the task of reconstructing this long and unique series. We describe the steps that were taken and the methods that were used in this reconstruction. Although the methods employed are basic, we believe that they are consistent with the quality of the data. The reconstructed record has values at every time point, original, or estimated, and has been adjusted for time-of-day variations where this information was available. Possible outliers have also been examined and replaced where their credibility could not be established. Many of the studies that have employed the Hopkins time series have not discussed the issue of data quality and how these problems were addressed. Because of growing interest in this record, it is important that a single, well-documented version be adopted, so that the results of future analyses can be directly compared. Although additional work may be done to further improve the quality of this record, it is now available via the internet. [PDF contains 48 pages]

Validation of daily growth increments and estimation of growth rates of larval and early juvenile black skipjack, Euthynnus lineatus, using otoliths

ENGLISH: Increments in otoliths (sagittae) were examined, using light and scanning electron microscopy, to determine ages and estimate growth rates of larval and early-juvenile black skipjack, Euthynnus lineatus. Larvae and juveniles were collected between 1987 and 1989 from coastal waters of Panama in the eastern Pacific Ocean. Results from a laboratory experiment indicated that immersion for 6 and 12 hours in a 200 mg/L solution of tetracycline hydrochloride adequately marks otoliths and that increments are formed daily in the sagittae of postflexion larvae and early juveniles. Further, survival rates of tetracycline-treated fish were not significantly different from those of control fish. Growth rates were derived from length-age relationships of 218 field-collected specimens ranging in size from 5.7 to 20.3 mm SL. A growth rate of 0.70 mm/d was estimated from the weighted regression of standard length on age for all specimens. This rate lies within the range reported for larvae and early juveniles of other species of subtropical and tropical scombrids. Growth rates of postflexion larvae and early juveniles were not significantly different between the rainy season in July-August 1988 and the dry, upwelling season in January-February 1989. Growth was, however, significantly more variable for older individuals in July-August than in January-February, and may correspond, in part, to seasonal patchiness of prey. The growth rates of the otoliths relative to fish length were also not significantly different between seasons; however, the otoliths were larger relative to the lengths of fish collected in the rainy season, which may reflect slower growth during earlier larval stages. SPANISH: Se examinaron incrementos en otolitos (ságitas), usando microscopia de luz y de barrido electrónico, a fin de determinar la edad y estimar las tasas de crecimiento de barriletes negros, Euthynnus lineatus, larvales y juveniles tempranos. Entre 1987 y 1989 se capturaron larvas y juveniles en las aguas costeras de Panamá en el Océano Pacífico oriental. Los resultados de un experimento de laboratorio indicaron que una inmersión de 6 a 12 horas de duración en una solución de 200 mg/L de hidrocloro de tetraciclina marca los otolitos adecuadamente y que los incrementos se forman a diario en las ságitas de larvas en postflexión y juveniles tempranos. Además, las tasas de supervivencia de los peces tratados con tetraciclina no fueron significativamente diferentes a aquellas de los peces de control. Se calcularon las tasas de crecimiento a partir de las relaciones de talla-edad de 218 especímenes de TE entre 5.7 y 20.3 mm capturados en el mar. Se estimó.una tasa de crecimiento de 0.70 mm/día a partir de la regresión ponderada de talla estándar sobre edad para todos los especímenes. Esta tasa cae dentro del rango reportado para larvas y juveniles tempranos de otras especies de escómbridos subtropicales y tropicales. Las tasas de crecimiento de larvas en postflexión y juveniles tempranos no fueron significativamente diferentes entre la temporada de lluvias en julio-agosto de 1988 y la temporada de sequía y afloramiento en enero-febrero de 1989. Sin emoargo, el crecimiento fue significativamente más variable para los individuos de mayor edad en julio-agosto que en enero-febrero, y quizás corresponda parcialmente a la irregularidad temporal de la abundancia de presas. Las tasas de crecimiento de los otolitos en relación a la talla de los peces tampoco fueron significativamente diferentes entre temporadas; sin embargo, los otolitos eran más grandes en relación a la talla en peces capturados en la temporada de lluvias, lo cual podría reflejar crecimiento más lento durante las etapas larvales más tempranas. (PDF contains 42 pages.)

Membrane activities of Dynamin-related protein 1 (DRP1) and BCL2-related Ovarian Killer (BOK)

311 p.

Island life in the Cretaceous - faunal composition, biogeography, evolution, and extinction of land-living vertebrates on the Late Cretaceous European archipelago

The Late Cretaceous was a time of tremendous global change, as the final stages of the Age of Dinosaurs were shaped by climate and sea level fluctuations and witness to marked paleogeographic and faunal changes, before the end-Cretaceous bolide impact. The terrestrial fossil record of Late Cretaceous Europe is becoming increasingly better understood, based largely on intensive fieldwork over the past two decades, promising new insights into latest Cretaceous faunal evolution. We review the terrestrial Late Cretaceous record from Europe and discuss its importance for understanding the paleogeography, ecology, evolution, and extinction of land-dwelling vertebrates. We review the major Late Cretaceous faunas from Austria, Hungary, France, Spain, Portugal, and Romania, as well as more fragmentary records from elsewhere in Europe. We discuss the paleogeographic background and history of assembly of these faunas, and argue that they are comprised of an endemic 'core' supplemented with various immigration waves. These faunas lived on an island archipelago, and we describe how this insular setting led to ecological peculiarities such as low diversity, a preponderance of primitive taxa, and marked changes in morphology (particularly body size dwarfing). We conclude by discussing the importance of the European record in understanding the end-Cretaceous extinction and show that there is no clear evidence that dinosaurs or other groups were undergoing long-term declines in Europe prior to the bolide impact.