Scorpions trapped in amber: a remarkable window on their evolution over time from the Mesozoic period to present days

This synoptic review aims to bring some general information on fossil scorpions, namely those trapped in amber - fossilized resin - ranging from Lower Cretaceous through the Palaeocene and up to the Miocene. The question to be addressed is how the study of these fossils can be connected with possible present scorpionism problems. A precise knowledge of these ancient lineages provides information about the evolution of extant lineages, including the buthoids, which contain most known noxious species. Among the Arthropods found trapped in amber, scorpions are considered rare. A limited number of elements have been described from the Late Tertiary Dominican and Mexican amber, while the most ancient Tertiary amber from the Baltic region produced more consistent results in the last 30 years, primarily focusing on a single limited lineage. Contrarily, the Cretaceous amber from Myanmar, also called Burmite, has yielded and continues to yield a significant number of results represented by several distinct lineages, which attest to the considerable degree of diversity that existed in the Burmese amber-producing forests. As in my previous similar contributions to this journal, the content of this note is primarily addressed to non-specialists whose research embraces scorpions in various fields such as venom toxins and public health. An overview knowledge of at least some fossil lineages can eventually help to clarify why some extant elements associated with the buthoids represent dangerous species while others are not noxious.(AU)

Identification of potential AChE inhibitors through combined machine-learning and structure-based design approaches-Supplementary data

Alzheimer’s disease (AD) is an irreversible, progressive neurodegenerative disease characterised by dementia.The depletion of acetylcholine (ACh) is involved the synaptic cleft is responsible for dementia due to neuronal loss. The acetylcholinesterase (AChE) enzyme isinvolved in the hydrolytic degradation of ACh and its inhibition is therapeutically beneficial for the treatment in memory loss.The use of machine learning (ML) for the identification of enzyme inhibitors has recently become popular. It identifies important patterns in the reported inhibitors to predict the new molecules. Hence, in this study, a set of support vector classifier-based ML models were developed,validated and employed to predict AChE inhibitors. Further, 247 predicted compounds obtained through PAINS and molecular property filters were docked on the AChE enzyme. The docking study identified compounds AAM132011183, ART21232619 and LMG16204648 as AChE inhibitors with suitable ADME properties. The selected compounds produced stable interactions with enzymes in molecular dynamics studies. The novel inhibitors obtained from the study may be proposed as active leads for AChE inhibition.

Identification of potential AChE inhibitors through combined machine-learning and structure-based design approaches-Supplementary data

Alzheimer’s disease (AD) is an irreversible, progressive neurodegenerative disease characterised by dementia.The depletion of acetylcholine (ACh) is involved the synaptic cleft is responsible for dementia due to neuronal loss. The acetylcholinesterase (AChE) enzyme isinvolved in the hydrolytic degradation of ACh and its inhibition is therapeutically beneficial for the treatment in memory loss.The use of machine learning (ML) for the identification of enzyme inhibitors has recently become popular. It identifies important patterns in the reported inhibitors to predict the new molecules. Hence, in this study, a set of support vector classifier-based ML models were developed,validated and employed to predict AChE inhibitors. Further, 247 predicted compounds obtained through PAINS and molecular property filters were docked on the AChE enzyme. The docking study identified compounds AAM132011183, ART21232619 and LMG16204648 as AChE inhibitors with suitable ADME properties. The selected compounds produced stable interactions with enzymes in molecular dynamics studies. The novel inhibitors obtained from the study may be proposed as active leads for AChE inhibition.

Identification of potential AChE inhibitors through combined machine-learning and structure-based design approaches

Alzheimer’s disease (AD) is an irreversible, progressive neurodegenerative disease characterised by dementia.The depletion of acetylcholine (ACh) is involved the synaptic cleft is responsible for dementia due to neuronal loss. The acetylcholinesterase (AChE) enzyme isinvolved in the hydrolytic degradation of ACh and its inhibition is therapeutically beneficial for the treatment in memory loss.The use of machine learning (ML) for the identification of enzyme inhibitors has recently become popular. It identifies important patterns in the reported inhibitors to predict the new molecules. Hence, in this study, a set of support vector classifier-based ML models were developed,validated and employed to predict AChE inhibitors. Further, 247 predicted compounds obtained through PAINS and molecular property filters were docked on the AChE enzyme. The docking study identified compounds AAM132011183, ART21232619 and LMG16204648 as AChE inhibitors with suitable ADME properties. The selected compounds produced stable interactions with enzymes in molecular dynamics studies. The novel inhibitors obtained from the study may be proposed as active leads for AChE inhibition.

Assessing contrast sensitivity change in retinal diseases with use of yellow-amber NoIR glasses

Purpose: The purpose of this study was to assess change of contrast sensitivity (CS) in subjects having retinal diseases with yellow?amber no infrared (NoIR) glasses used as low vision aid (LVA). Methods: We examined CS in 82 low vision (LV) subjects having retinal diseases with Pelli Robson Chart at 1 m distance before and after wearing yellow?amber NoIR glasses. We also found type of retinal affection and macular optical coherence tomography (OCT) features. Results: The distance and near best?corrected visual acuity (BCVA) was, respectively, 0.68 ± 0.17 (median = 0.70) and 0.72 ± 0.25 (median = 0.70) logmar units. The pre?LVA CS was 0.52 ± 0.29 (median = 0.3) and post? LVA was 0.52 ± 0.28 (median = 0.45) logunits (mean reduction = ?0.002 ± 0.24; Median reduction = 0; P = 0.909). The pre?LVA and post?LVA CS showed a negative correlation with logmar distance BCVA [r = ?0.090; P = 0.317 and r = ?0.152; P = 0.090 respectively]. The pre?LVA and post?LVA CS showed a negative correlation with logmar near BCVA [r = ?0.114; P = 0.207 and r = ?0.054; P = 0.549 respectively]. The CS did not improve in subjects having macular degeneration, pathological myopia, hereditary maculopathy, and diabetic retinopathy. The macular OCT features like fluid, exudates, scars, drusens, traction, and hole did not significantly influence CS both at pre?LVA and post?LVA stage. Conclusion: This is the first study with yellow?amber NoIR glasses which blocks “both ultraviolet and infrared light.” The subjects having macular degeneration, pathological myopia, hereditary maculopathy, and diabetic retinopathy did not improve in CS with filters. The correlation values showed that filters may improve CS in subjects having good baseline BCVA.

Use of the amber teething necklace by the child population: risks versus benefits / Uso do colar de âmbar pela população infantil: riscos x benefícios

Abstract Objective: Based on scientific evidence, the objective of the present study is to report the possible risks and benefits of the amber teething necklace for children who use it. Data source: This is an integrative literature review, carried out based on the following guiding question: "Does the amber teething necklace have therapeutic properties that justify its usage during tooth eruption?". The consulted databases were LILACS (Latin American and Caribbean Health Sciences Literature) and PubMed (National Center for Biotechnology Information), with the following descriptors: "Amber," "Deciduous teeth," "Strangulation," and "Local symptoms." Data synthesis: A total of five scientific articles were selected, which indicates an insufficient basis regarding the benefits associated with the use of the amber teething necklace. Conversely, there is a convergence regarding the possibility of health risks such as strangulation, asphyxiation, and swallowing of beads. Conclusions: Health professionals should discourage the use of the amber teething necklace by children insofar more studies on the topic are carried out.

Resumo Objetivo: Com base em evidências científicas, a proposta do presente trabalho é relatar os prováveis riscos e benefícios do uso do colar de âmbar pela população infantil. Fontes de dados: Trata-se de uma revisão integrativa da literatura, realizada a partir da elaboração da questão norteadora: "O colar de âmbar apresenta propriedades que justifiquem seu uso durante a erupção dentária?''. As bases de dados utilizadas foram LILACS (Literatura Latino-americana e do Caribe em Ciências da Saúde), PubMed (National Center for Biotechnology Information), por meio dos descritores: Âmbar; Dentes decíduos; Estrangulamento; Sintomas locais. Síntese dos dados: Após a busca dos dados, foram selecionados cinco artigos, os quais apontam insuficiente embasamento científico que comprove os benefícios relacionados ao uso do colar de âmbar. Em contrapartida, existe uma convergência quanto à possibilidade de riscos à saúde, como estrangulamento, asfixia e deglutição das pedras. Conclusões: Conclui-se que os profissionais da saúde devem desencorajar o seu uso por crianças até que pesquisas clínicas bem delineadas sejam disponibilizadas.

New genus of fossil apoid wasps (Hymenoptera, Apoidea) from the Cretaceous amber of Myanmar

ABSTRACT The new genus †Burmasphex is proposed for two fossil species, †Burmasphex sulcatus sp. nov. and †Burmasphex pilosus sp. nov., described from Myanmar Cretaceous amber. It exhibits many plesiomorphic features in relation to the extant Apoidea and is here provisionally allocated in the extinct family †Angarosphecidae.

Structural analysis of adsorption processes of 5FU and imiquimod on hydrogels using AMBER/PM3 hybrid model / Análisis estructural de los procesos de adsorción de 5FU e imiquimod en hidrogeles utilizando el modelo híbrido AMBER/PM3 / Análise estrutural de procedimentos de adsorção de 5FU e imiquimod em hidrogeles usando modelo híbrido AMBER/PM3

Abstract AMBER/PM3 hybrid model allowed determining the structural properties of 5FU and imiquimod individually and after the adsorption in chitosan hydrogels crosslinked with genipin, respectively. It was observed that the Gibbs free energy (AG) decreases with the adsorption, but indicates thermodynamic stability and spontaneity in both processes; AG was verified by the increase in the dipole moments. On the one hand the partition coefficient established the hydrophilic character with respect to the water present in the hydrogel, which increases with the adsorption. The FTIR showed that there were displacements in the signals, however, the hydrogen bond bands attributed to the formation of new bonds to perform the adsorption of the drugs were observed. The adsorption was verified by the MESP and the surface analysis, where the distribution of nucleophilic and electrophilic zone was observed.

Resumen El modelo hibrido AMBER/PM3 permitió determinar las propiedades estructurales del 5FU e imiquimod individualmente y después de la adsorción en hidrogeles de quitosano entrecruzados con genipina, respectivamente. Se observó que la energía libre de Gibbs (AG) disminuye con la adsorción, sin embargo, en ambos procesos se encontró estabilidad termodinámica y espontaneidad; AG fue verificado mediante el incremento en los momentos dipolares. Por otro lado, el coeficiente de partición estableció el carácter hidrofílico con respecto al agua presente en el hidrogel, el cual aumenta con la adsorción. El FTIR evidenció que existen desplazamientos en las señales. Se observaron las bandas de puente de hidrógeno, atribuidas a la formación de enlaces, para realizar la adsorción de los fármacos. La adsorción fue verificada mediante los MESP y los análisis de superficie, en donde se apreció la distribución de zonas nucleofílicas y electrofílicas.

Resumo O modelo hibrido AMBER/PM3 permitiu determinar as propriedades estruturadas do 5FU e imiquimod individualmente e depois da adsorção em hidrogeles de quitosano entrecruzados com genipina, respectivamente. Observou-se que o poder livre de Gibbs (AG) diminui com a adsorção, sem embargo, em ambos os processos se encontró estabilidade termodinâmica e espontaneidad; AG foi verificado através do aumento nos momentos de dipolares. Por outro lado, o coeficiente de divisão estabeleceu o carácter hidrofílico em relação à água presente no hidrogel, o qual aumenta com a adsorção. El FTIR evidenció que existem deslocamentos em las señales. Se observe as bandas de puente de hidrógeno, atribuições à formação de enlaces, para realizar a adsorção dos fármacos. A adsorção foi verificada através do MESP e os análises de superfície, em donde se apreciou a distribuição de zonas nucleofílicas e eletrofílicas.

Effects of amiodarone combined with succinylmetroprolol sustained-release tablets on cardiac function in patients with atrial fibrillation and congestive heart failure / 中国生化药物杂志

Objective To investigate the clinical efficacy of amiodarone combined with succinylmetroprolol sustained-release tablets in patients with atrial fibrillation and congestive heart failure (CHF) complicated with atrial fibrillation (AF), and to observe the effect of amiodarone on heart function and ventricular rate.MethodsIn people's hospital of Anji county from June 2013 to June 2016 a total of 80 patients with atrial fibrillation and heart failure were enrolled in this study.The patients were randomly divided into control group and treatment group, 40 cases.(Ventricular rate, resting ventricular rate), cardiac function (ejection fraction-EF, stroke volume-SV, cardiac output-CO and left ventricular function) were measured before treatment and 6 months after treatment Ventricular end-diastolic early/late peak velocity ratio-VA/VE).The clinical efficacy and side effects during the treatment were statistically analyzed.ResultsThe ventricular rate and resting ventricular rate after exercise were significantly lower than those before treatment, but the ventricular rate and resting ventricular rate were significantly lower in the treatment group than those in the control group after 6 months of treatment (P<0.05).The VA/VE was significantly lower than that of the control group at 6 months after treatment, and the values of EF, SV and CO were significantly higher than those of the control group at 6 months after the treatment, SV, CO were significantly higher than the control group(P<0.05).Treatment group, the total effective rate was 92.5%, significantly higher than the control group 72.5%(χ2=7.77, P=0.02).No significant adverse reactions during treatment.ConclusionRapid ventricular rate of atrial fibrillation with congestive heart failure were treated with amiodarone combined with metoprolol succinate sustained release tablets can conducive to the ventricular rate and heart function of patients, and the effect is remarkable, safe, so it can be recommended as the drug of choice for clinical treatment of patients.

Estudios preliminares de estabilidad de un extracto lipídico de los frutos de Roystonea regia en frascos de vidrio ámbar / Preliminary studies of a lipid extract stability from the fruits of Roystonea regia in amber glass flasks

El D004 es un nuevo ingrediente activo extraído de los frutos de la palma real cubana (Roystonea regia), promisorio en el tratamiento de la hiperplasia prostática benigna. Para determinar su estabilidad en frascos de vidrio ámbar, se realizaron estudios donde las muestras se sometieron a diferentes condiciones. En condiciones de estrés se observó que el D004 es susceptible a la degradación térmica y oxidativa. En condiciones aceleradas (40 ± 2 ºC y 75 ± 5 por ciento humedad relativa) no se observaron cambios significativos en ninguno de los parámetros evaluados durante 12 meses, lo que permitió predecir un tiempo de vida útil de al menos 2 años en condiciones menos drásticas. Esto fue corroborado en las condiciones de las zonas climáticas II (25 ± 2 ºC y 60 ± 5 por ciento humedad relativa) y IV (30 ± 2 ºC y 70 ± 5 por ciento humedad relativa)

The D004 is a new active ingredient extracted from the Cuban real palm (Roystonea regia), promising in the treatment of the benign prostatic hyperplasia. To determine its stability in amber glass flasks studies were conducted where samples underwent different conditions. In stress situations D004 is sensitive to the thermal and oxidative degradation. Under accelerated conditions (40 ± 2 ºC ad 75 ± 5 percent of relative humidity) there weren't significant changes in any assessed parameters during 12 months allowing predicting a useful life time of at least 2 years under less drastic conditions. It was corroborated under climatic conditions II (25 ± 2ºC and 60± 5 percent of relative humidity and IV (30 ± 2 ºC and 70 ± 5 percent of relative humidity)

Estudio de estabilidad acelerada del ingrediente activo D-004 en diferentes envases / Accelerated stability study of D-004 active ingredient in different containers

INTRODUCCIÓN: D-004 es un nuevo ingrediente activo en fase de investigación y desarrollo, obtenido de los frutos de Roystonea regia (Kunth) O.F. Cook. OBJETIVO: precisar la estabilidad de D-004 en condiciones aceleradas en frascos de vidrio ámbar, de tereftalato de polietileno y de polietileno de alta densidad. MÉTODOS: muestras de 3 lotes se almacenaron a (40 ± 2) ºC y (75 ± 5) porciento de humedad relativa durante 12 meses. Se determinaron las características organolépticas, la densidad relativa, el índice de refracción (USP 27) y el contenido de ácidos grasos mediante cromatografía de gases. RESULTADOS: los parámetros medidos se mantuvieron dentro de las especificaciones de calidad establecidas, con excepción del contenido de ácidos grasos, que en los frascos de tereftalato y polietileno disminuyó significativamente a los 3, 6 y 4,5 meses, respectivamente. CONCLUSIONES: el vidrio ámbar protege al D-004 de la degradación más que los envases plásticos estudiados.

INTRODUCTION: D-004 is a new active ingredient under research and development stage, which is obtained from Roystonea regia (Kunth) O. F. Cook fruits. OBJECTIVE: to precise over the D-004 stability under accelerated conditions in amber glass, polyethylene terephtalate and high density polyethylene containers. METHODS: samples from three batches were stored at (40 ± 2) ºC and (75 ± 5) percent relative humidity for 12 months. Organoleptic characteristics, relative density, refractive index (USP 27) and fatty acids content by gas chromatography, were determined. RESULTS: measured parameters were within the set quality specifications , except for fatty acids content that significantly decreased in polyethylene terephtalate and high density polyethylene containers after 3, 4 and a half and 6 months, respectively. CONCLUSIONS: the amber glass protects more D-004 from degradation than the analyzed plastic containers.

Description of Pintomyia (Pifanomyia) paleotrichia, a Miocene period new species from the Dominican Republic (Diptera: Psychodidae: Phlebotominae)

A new fossil species of phlebotomine sandflies is described from Dominican amber based in one specimen. Pintomyia (Pifanomyia) paleotrichia sp. nov. is distinguished from the other extant and extinct species by aspects of paramere and the basal tuft of bristles in the gonocoxite.