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1.
PLoS One ; 15(6): e0228524, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32497041

RESUMEN

Nester abundance is a key measure of the performance of the world's largest green turtle rookery at Raine Island, Australia, and has been estimated by mark-resight counts since 1984. Nesters are first marked by painting their carapace with a longitudinal white stripe. Painted and unpainted turtles are then counted by a surface observer on a small boat in waters adjacent to the reef. Unmanned aerial vehicles (UAV) and underwater video may provide more cost-effective and less biased alternatives to this approach, but estimates must be comparable with historical estimates. Here we compare and evaluate the three methods. We found comparatively little variation in resighting probabilities between consecutive days of sampling or time of day, which supports an underlying assumption of the method (i.e. demographic closure during sampling). This lack of bias in the location availability for detection of painted versus unpainted turtles and further supported by a parallel satellite tracking study of 40 turtles at Raine Island. Our results demonstrated that surface observers consistently reported higher proportions of marked turtles than either the UAV or underwater video method. This in turn yielded higher population estimates with UAV or underwater video compared to the historical surface observer method, which suggested correction factors of 1.53 and 1.73 respectively. We attributed this to observer search error because a white marked turtle is easier to spot than the non-marked turtle. In contrast, the UAV and underwater video methods allowed subsequent frame-by-frame review, thus reducing observer search error. UAVs were the most efficient in terms of survey time, personnel commitment and weather tolerance compared to the other methods. However, underwater video may also be a useful alternative for in-water mark-resight surveys of turtles.


Asunto(s)
Monitoreo del Ambiente/instrumentación , Islas , Comportamiento de Nidificación , Tortugas , Animales , Automatización , Femenino , Inmersión , Densidad de Población , Queensland , Grabación en Video
2.
PLoS One ; 13(4): e0195462, 2018.
Artículo en Inglés | MEDLINE | ID: mdl-29694365

RESUMEN

Raine Island hosts the largest nesting aggregation of green turtles in the world, but nest emergence success and hence recruitment of hatchlings off the beach appear to have significantly declined since the 1990s. Nests destroyed by subsequent nesting turtles, and nest failure due to flooding account for most of the nest failure, but many nests still have poor hatch success even when undisturbed and flood-free. In undisturbed, flood-free nests that experience high mortality, embryos typically die at a very early stage of development, a phenomenon we term early embryo death syndrome (EEDS). Previous research indicates that EEDS is correlated with the number of females nesting at Raine Island during a nesting season. Here, we monitor nest temperature and oxygen (PO2) and carbon dioxide (PCO2) partial pressures during the first week after nest construction to discover if they are associated with EEDS. Our investigation found that the proportion of early embryo death was greatest in two nests that experienced the highest nest temperature, lowest PO2 and highest PCO2 during the first week of incubation suggesting that these variables either by themselves or in combination may be the underlying cause of EEDS. These two nests were located adjacent to maturing nests, so the high temperature and more extreme PO2s and PCO2s are most likely to be caused by the combined metabolism of embryos in the mature nests. Although this conclusion is based on just two nests and needs to be substantiated in future studies, it would appear that the laying of new nests in the close location to mature nests could be a significant cause of hatch failure at high density nesting sea turtle rookeries around the world.


Asunto(s)
Embrión no Mamífero/fisiología , Tortugas/embriología , Animales , Dióxido de Carbono/análisis , Comportamiento de Nidificación , Oxígeno/análisis , Reproducción , Temperatura , Factores de Tiempo
3.
PLoS One ; 9(6): e100799, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-24956107

RESUMEN

The extant species of Nautilus and Allonautilus (Cephalopoda) inhabit fore-reef slope environments across a large geographic area of the tropical western Pacific and eastern Indian Oceans. While many aspects of their biology and behavior are now well-documented, uncertainties concerning their current populations and ecological role in the deeper, fore-reef slope environments remain. Given the historical to current day presence of nautilus fisheries at various locales across the Pacific and Indian Oceans, a comparative assessment of the current state of nautilus populations is critical to determine whether conservation measures are warranted. We used baited remote underwater video systems (BRUVS) to make quantitative photographic records as a means of estimating population abundance of Nautilus sp. at sites in the Philippine Islands, American Samoa, Fiji, and along an approximately 125 km transect on the fore reef slope of the Great Barrier Reef from east of Cairns to east of Lizard Island, Australia. Each site was selected based on its geography, historical abundance, and the presence (Philippines) or absence (other sites) of Nautilus fisheries The results from these observations indicate that there are significantly fewer nautiluses observable with this method in the Philippine Islands site. While there may be multiple possibilities for this difference, the most parsimonious is that the Philippine Islands population has been reduced due to fishing. When compared to historical trap records from the same site the data suggest there have been far more nautiluses at this site in the past. The BRUVS proved to be a valuable tool to measure Nautilus abundance in the deep sea (300-400 m) while reducing our overall footprint on the environment.


Asunto(s)
Nautilus/crecimiento & desarrollo , Tecnología de Sensores Remotos/métodos , Grabación en Video , Agua , Samoa Americana , Animales , Australia , Arrecifes de Coral , Fiji , Filipinas , Fotograbar , Dinámica Poblacional
4.
Bioorg Med Chem Lett ; 21(21): 6249-52, 2011 Nov 01.
Artículo en Inglés | MEDLINE | ID: mdl-21940167

RESUMEN

A library of chemokine antagonists has been synthesized using a combination of solid and solution-phase chemistry. Structures of known chemokine antagonists were used to produce a pharmacophore which served to guide monomer selection. Several combinations of monomers have resulted in providing novel chemokine antagonists which in some cases display dual chemokine receptor antagonism.


Asunto(s)
Quimiocinas/antagonistas & inhibidores , Diseño de Fármacos , Bibliotecas de Moléculas Pequeñas , Animales , Línea Celular , Cricetinae , Cricetulus
5.
PLoS One ; 6(2): e16311, 2011 Feb 22.
Artículo en Inglés | MEDLINE | ID: mdl-21364981

RESUMEN

Vertical depth migrations into shallower waters at night by the chambered cephalopod Nautilus were first hypothesized early in the early 20(th) Century. Subsequent studies have supported the hypothesis that Nautilus spend daytime hours at depth and only ascend to around 200 m at night. Here we challenge this idea of a universal Nautilus behavior. Ultrasonic telemetry techniques were employed to track eleven specimens of Nautilus pompilius for variable times ranging from one to 78 days at Osprey Reef, Coral Sea, Australia. To supplement these observations, six remotely operated vehicle (ROV) dives were conducted at the same location to provide 29 hours of observations from 100 to 800 meter depths which sighted an additional 48 individuals, including five juveniles, all deeper than 489 m. The resulting data suggest virtually continuous, nightly movement between depths of 130 to 700 m, with daytime behavior split between either virtual stasis in the relatively shallow 160-225 m depths or active foraging in depths between 489 to 700 m. The findings also extend the known habitable depth range of Nautilus to 700 m, demonstrate juvenile distribution within the same habitat as adults and document daytime feeding behavior. These data support a hypothesis that, contrary to previously observed diurnal patterns of shallower at night than day, more complex vertical movement patterns may exist in at least this, and perhaps all other Nautilus populations. These are most likely dictated by optimal feeding substrate, avoidance of daytime visual predators, requirements for resting periods at 200 m to regain neutral buoyancy, upper temperature limits of around 25°C and implosion depths of 800 m. The slope, terrain and biological community of the various geographically separated Nautilus populations may provide different permutations and combinations of the above factors resulting in preferred vertical movement strategies most suited for each population.


Asunto(s)
Migración Animal/fisiología , Nautilus/fisiología , Animales , Australia , Biota , Ritmo Circadiano/fisiología , Arrecifes de Coral , Ecosistema , Conducta Alimentaria/fisiología , Océanos y Mares , Orientación/fisiología , Fotoperiodo , Dinámica Poblacional , Temperatura
6.
PLoS One ; 6(2): e16312, 2011 Feb 10.
Artículo en Inglés | MEDLINE | ID: mdl-21347356

RESUMEN

Nautiloids are the subject of speculation as to their threatened status arising from the impacts of targeted fishing for the ornamental shell market. Life history knowledge is essential to understand the susceptibility of this group to overfishing and to the instigation of management frameworks. This study provides a comprehensive insight into the life of Nautilus in the wild. At Osprey Reef from 1998-2008, trapping for Nautilus was conducted on 354 occasions, with 2460 individuals of one species, Nautilus pompilius, captured and 247 individuals recaptured. Baited remote underwater video systems (BRUVS) were deployed on 15 occasions and six remotely operated vehicle (ROV) dives from 100-800 m were conducted to record Nautilus presence and behavior. Maturity, sex and size data were recorded, while measurements of recaptured individuals allowed estimation of growth rates to maturity, and longevity beyond maturity. We found sexual dimorphism in size at maturity (males: 131.9±SD = 2.6 mm; females: 118.9±7.5 mm shell diameter) in a population dominated by mature individuals (58%). Mean growth rates of 15 immature recaptured animals were 0.061±0.023 mm day(-1) resulting in an estimate of around 15.5 years to maturation. Recaptures of mature animals after five years provide evidence of a lifespan exceeding 20 years. Juvenile Nautilus pompilius feeding behavior was recorded for the first time within the same depth range (200-610 m) as adults. Our results provide strong evidence of a K-selected life history for Nautilus from a detailed study of a 'closed' wild population. In conjunction with population size and density estimates established for the Osprey Reef Nautilus, this work allows calculations for sustainable catch and provides mechanisms to extrapolate these findings to other extant nautiloid populations (Nautilus and Allonautilus spp.) throughout the Indo-Pacific.


Asunto(s)
Arrecifes de Coral , Nautilus/crecimiento & desarrollo , Distribución por Edad , Animales , Australia , Conservación de los Recursos Naturales , Toma de Decisiones , Buceo , Femenino , Explotaciones Pesqueras/estadística & datos numéricos , Longevidad , Masculino , Nautilus/fisiología , Oviposición , Estaciones del Año , Caracteres Sexuales , Distribución por Sexo
7.
PLoS One ; 6(2): e16716, 2011 Feb 10.
Artículo en Inglés | MEDLINE | ID: mdl-21347360

RESUMEN

The low fecundity, late maturity, long gestation and long life span of Nautilus suggest that this species is vulnerable to over-exploitation. Demand from the ornamental shell trade has contributed to their rapid decline in localized populations. More data from wild populations are needed to design management plans which ensure Nautilus persistence. We used a variety of techniques including capture-mark-recapture, baited remote underwater video systems, ultrasonic telemetry and remotely operated vehicles to estimate population size, growth rates, distribution and demographic characteristics of an unexploited Nautilus pompilius population at Osprey Reef (Coral Sea, Australia). We estimated a small and dispersed population of between 844 and 4467 individuals (14.6-77.4 km(-2)) dominated by males (83:17 male:female) and comprised of few juveniles (<10%).These results provide the first Nautilid population and density estimates which are essential elements for long-term management of populations via sustainable catch models. Results from baited remote underwater video systems provide confidence for their more widespread use to assess efficiently the size and density of exploited and unexploited Nautilus populations worldwide.


Asunto(s)
Especies en Peligro de Extinción/estadística & datos numéricos , Nautilus , Migración Animal , Animales , Conservación de los Recursos Naturales , Femenino , Inmersión , Masculino , Modelos Estadísticos , Movimiento , Nautilus/fisiología , Densidad de Población , Factores de Tiempo , Grabación en Video
8.
Bioorg Med Chem Lett ; 17(8): 2376-9, 2007 Apr 15.
Artículo en Inglés | MEDLINE | ID: mdl-17337182

RESUMEN

Inhibitors of PDE5 are useful therapeutic agents for treatment of erectile dysfunction. A series of novel xanthine derivatives has been identified as potent inhibitors of PDE5, with good levels of selectivity against other PDE isoforms, including PDE6. Studies in the dog indicate excellent oral bioavailability for compound 21.


Asunto(s)
3',5'-GMP Cíclico Fosfodiesterasas/antagonistas & inhibidores , Xantinas/farmacología , Animales , Disponibilidad Biológica , Bovinos , Fosfodiesterasas de Nucleótidos Cíclicos Tipo 5 , Perros , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/farmacología , Inhibidores Enzimáticos/uso terapéutico , Disfunción Eréctil/tratamiento farmacológico , Humanos , Concentración 50 Inhibidora , Masculino , Farmacocinética , Isoformas de Proteínas/efectos de los fármacos , Relación Estructura-Actividad , Xantinas/química
9.
J Med Chem ; 47(19): 4642-4, 2004 Sep 09.
Artículo en Inglés | MEDLINE | ID: mdl-15341478

RESUMEN

The bradykinin B(1) receptor is rapidly induced after inflammation or tissue trauma and appears to play an important role in the maintenance of hyperalgesia in inflammatory conditions. Here, we describe the optimization process to identify novel, potent non-peptide human B(1) receptor antagonists based on a 2-alkylamino-5-sulfamoylbenzamide core. Optimized derivatives are selective, functional B(1) antagonists with low nanomolar affinity and exhibit oral bioavailability in animals.


Asunto(s)
Antagonistas del Receptor de Bradiquinina B1 , ortoaminobenzoatos/química , ortoaminobenzoatos/farmacocinética , Administración Oral , Aminas/química , Aminoácidos/química , Disponibilidad Biológica , Ácidos Carboxílicos/química , Humanos , Estructura Molecular , Péptidos/administración & dosificación , Péptidos/síntesis química , Péptidos/química , Péptidos/farmacología , ortoaminobenzoatos/administración & dosificación , ortoaminobenzoatos/farmacología
11.
Bioorg Med Chem Lett ; 12(18): 2587-90, 2002 Sep 16.
Artículo en Inglés | MEDLINE | ID: mdl-12182866

RESUMEN

In clinical studies, several inhibitors of phosphodiesterase 5 (PDE5) have demonstrated utility in the treatment of erectile dysfunction. We describe herein a series of 8-aryl xanthine derivatives which function as potent PDE5 inhibitors with, in many cases, high levels of selectivity versus other PDE isoforms.


Asunto(s)
Inhibidores de Fosfodiesterasa/farmacología , Hidrolasas Diéster Fosfóricas/efectos de los fármacos , Xantinas/farmacología , Modelos Moleculares , Estructura Molecular , Inhibidores de Fosfodiesterasa/química , Xantinas/química
12.
Bioorg Med Chem Lett ; 12(15): 1973-6, 2002 Aug 05.
Artículo en Inglés | MEDLINE | ID: mdl-12113821

RESUMEN

PDE5 inhibitors based upon the xanthine scaffold 8 have been expediently synthesized using a solid-phase route. Attachment of the xanthine scaffold 8 using the Rink chloride linker 4 and N-1 functionalization using Mitsunobu chemistry is described. A library of compounds was produced in multi-milligram quantities with excellent purities and acceptable yields. The compounds were tested for their PDE5 inhibitory activity.


Asunto(s)
Inhibidores de Fosfodiesterasa/síntesis química , Hidrolasas Diéster Fosfóricas/metabolismo , Xantina/química , 3',5'-GMP Cíclico Fosfodiesterasas , Técnicas Químicas Combinatorias , Fosfodiesterasas de Nucleótidos Cíclicos Tipo 5 , Bases de Datos Factuales , Indicadores y Reactivos/química , Resonancia Magnética Nuclear Biomolecular , Inhibidores de Fosfodiesterasa/farmacología , Relación Estructura-Actividad
13.
J Med Chem ; 45(11): 2160-72, 2002 May 23.
Artículo en Inglés | MEDLINE | ID: mdl-12014954

RESUMEN

The 1-(2-nitrophenyl)thiosemicarbazide (TSC) derivative, (S)-1-[4-(4-benzhydrylthiosemicarbazido)-3-nitrobenzenesulfonyl]pyrrolidine-2-carboxylic acid [2-[(2-dimethylaminoethyl)methylamino]ethyl]amide (bradyzide; (S)-4), was recently disclosed as a novel, potent, orally active nonpeptide bradykinin (BK) B2 receptor antagonist. The compound inhibited the specific binding of [3H]BK to NG108-15 cell membrane preparations (rodent neuroblastoma-glioma) expressing B2 receptors with a K(i) of 0.5 +/- 0.2 nM. Compound (S)-4 also demonstrated oral efficacy against Freund's complete adjuvant (FCA)-induced mechanical hyperalgesia in rats with an ED50 value of 0.84 micromol/kg. After we optimized the terminal binding determinants projecting from the TSC framework, we found that it was possible to replace the potentially toxicophoric nitro and divalent sulfur moieties with only a 15-fold loss in binding affinity ((S)-14a). However, bradyzide and its congeners were found to have much lower affinities for cloned human B2 receptors, expressed in Cos-7 cells. The hitherto synthesized TSC series was screened against the human B2 receptor, and the dibenzosuberane (DBS) pharmacophore emerged as the key structural requirement for potency. Incorporation of this group resulted in a series of derivatives ((S)-14d,e and 19b-d) with K(i) ranges of 10.7-176 nM in NG108-15 cells (expressing the rodent B2 receptor) and 0.79-253 nM in Cos-7 cells (expressing the human B2 receptor). There was no evidence of agonist activity with any of the nonpeptides in any of the cell lines tested. In vivo, oral administration of compound 19c reversed FCA-induced and turpentine-induced mechanical hyperalgesia in rodents with ED50 values of 0.027 and 0.32 micromol/kg, respectively. The selectivity profiles of compounds (S)-14f and (S)-14g were also assessed to determine the conformational and/or steric preferences of the double-ring arrangement. The affinity of (S)-14 g for the human B2 receptor suggested that it may be a hydrophobic interaction with the ethane bridge of the DBS moiety that accounts for the increased potency of compounds (S)-14d,e and 19b,c at this receptor, by favoring a binding mode inaccessible to the unsubstituted diphenylmethyl derivative, (S)-4.


Asunto(s)
Antiinflamatorios no Esteroideos/síntesis química , Antagonistas de los Receptores de Bradiquinina , Pirrolidinas/síntesis química , Tiosemicarbazonas/síntesis química , Administración Oral , Animales , Antiinflamatorios no Esteroideos/química , Antiinflamatorios no Esteroideos/farmacología , Artritis Experimental/tratamiento farmacológico , Línea Celular , Femenino , Humanos , Hiperalgesia/inducido químicamente , Hiperalgesia/tratamiento farmacológico , Modelos Moleculares , Estimulación Física , Pirrolidinas/química , Pirrolidinas/farmacología , Ensayo de Unión Radioligante , Ratas , Ratas Sprague-Dawley , Receptor de Bradiquinina B2 , Especificidad de la Especie , Relación Estructura-Actividad , Tiosemicarbazonas/química , Tiosemicarbazonas/farmacología , Trementina
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