Synthesis and Evaluation of the Fungal Activity of New Pyrazole-Carboxamides against Colletotrichum gloeosporioides

The pyrazole core has been recognized by their biological properties and included in the synthesis of modern agrochemicals. Part of these studies consists of making structural modifications to pesticides for commercial purposes to increase efficacy. In this article, we present the synthesis of four new pyrazol-4-carboxamide 8a-8d derivatives (PCD), through a four-step synthetic protocol, starting with edaravone 1 and primary amines like benzo-fused, aliphatic, and hydrazines, through a process of low environmental impact. Synthesized derivatives were evaluated against one fungal strain of Colletotrichum gloeosporioides BA3, fungus that causes several losses to farmers around the world, through in vitro sensitivity tests. The compound 8c showed better inhibiting behavior against Colletotrichum gloeosporioides BA3, inducing a lag phase of almost 2.77 days. These results were obtained via Gompertz modeling, for the first time reported for biological evaluation of pyrazole-carboxamide derivatives against Colletotrichum gloeosporioides.Fil: Gonzalez Lopez, Edwin Javier. Universidad del Atlántico; Colombia. Universidad Nacional de Río Cuarto. Facultad de Ciencias Exactas Fisicoquímicas y Naturales. Departamento de Química; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba; ArgentinaFil: León Jaramillo, Jhair Carlhino. Universidad del Atlántico; ColombiaFil: Trilleras Vásquez, Jorge Enrique. Universidad del Atlántico; ColombiaFil: Grande Tovar, Carlos D.. Universidad del Atlántico; ColombiaFil: Peralta Ruiz, Yeimmy. Universidad del Atlántico; Colombia. University Of Teramo. Faculty Of Bioscience And Technology For Food, Agriculture And Environment.; ItaliaFil: Quiroga, Jairo. Universidad del Valle; Colombi

Bioactive micro-constituents of ackee arilli (Blighia sapida K.D. Koenig)

Abstract: Ackee (Blighia sapida K. D. Koenig) is an exotic fruit widely consumed in the Caribbean countries. While there is extensive research on the presence of hypoglycin A, other bioactive compounds have not been studied. We identified and quantified the changes in bioactive molecules (total phenol, ascorbic acid, hypoglycin A, squalene, D: A-Friedooleanan-7-ol, (7.alpha.), and oleic acid), antioxidant potential, and volatile compounds during two stages of ripe. A clear reduction in hypoglycin A, ascorbic acid, and total polyphenols during the maturation process were observed. On the contrary, oleic acid, squalene, and D: A-Friedooleanan-7-ol, (7.alpha.) contents increased about 12, 12, and 13 times, respectively with advancing maturity. These bioactive molecules were positively correlated with radical scavenging (DDPH and ABTS). Solid phase microextraction (SPME) and gas chromatography coupled mass spectrometry (GC/MS) analysis revealed more than 50 compounds with 3-penten-2-one and hexanal as the major compounds in the fully ripe stage. The results suggested that ripe ackee arilli could serve as an appreciable source of natural bioactive micro-constituents

Why Are Outcomes Different for Registry Patients Enrolled Prospectively and Retrospectively? Insights from the Global Anticoagulant Registry in the FIELD-Atrial Fibrillation (GARFIELD-AF).

Background: Retrospective and prospective observational studies are designed to reflect real-world evidence on clinical practice, but can yield conflicting results. The GARFIELD-AF Registry includes both methods of enrolment and allows analysis of differences in patient characteristics and outcomes that may result. Methods and Results: Patients with atrial fibrillation (AF) and ≥1 risk factor for stroke at diagnosis of AF were recruited either retrospectively (n = 5069) or prospectively (n = 5501) from 19 countries and then followed prospectively. The retrospectively enrolled cohort comprised patients with established AF (for a least 6, and up to 24 months before enrolment), who were identified retrospectively (and baseline and partial follow-up data were collected from the emedical records) and then followed prospectively between 0-18 months (such that the total time of follow-up was 24 months; data collection Dec-2009 and Oct-2010). In the prospectively enrolled cohort, patients with newly diagnosed AF (≤6 weeks after diagnosis) were recruited between Mar-2010 and Oct-2011 and were followed for 24 months after enrolment. Differences between the cohorts were observed in clinical characteristics, including type of AF, stroke prevention strategies, and event rates. More patients in the retrospectively identified cohort received vitamin K antagonists (62.1% vs. 53.2%) and fewer received non-vitamin K oral anticoagulants (1.8% vs . 4.2%). All-cause mortality rates per 100 person-years during the prospective follow-up (starting the first study visit up to 1 year) were significantly lower in the retrospective than prospectively identified cohort (3.04 [95% CI 2.51 to 3.67] vs . 4.05 [95% CI 3.53 to 4.63]; p = 0.016). Conclusions: Interpretations of data from registries that aim to evaluate the characteristics and outcomes of patients with AF must take account of differences in registry design and the impact of recall bias and survivorship bias that is incurred with retrospective enrolment. Clinical Trial Registration: - URL: http://www.clinicaltrials.gov . Unique identifier for GARFIELD-AF (NCT01090362)

Risk profiles and one-year outcomes of patients with newly diagnosed atrial fibrillation in India: Insights from the GARFIELD-AF Registry.

BACKGROUND: The Global Anticoagulant Registry in the FIELD-Atrial Fibrillation (GARFIELD-AF) is an ongoing prospective noninterventional registry, which is providing important information on the baseline characteristics, treatment patterns, and 1-year outcomes in patients with newly diagnosed non-valvular atrial fibrillation (NVAF). This report describes data from Indian patients recruited in this registry. METHODS AND RESULTS: A total of 52,014 patients with newly diagnosed AF were enrolled globally; of these, 1388 patients were recruited from 26 sites within India (2012-2016). In India, the mean age was 65.8 years at diagnosis of NVAF. Hypertension was the most prevalent risk factor for AF, present in 68.5% of patients from India and in 76.3% of patients globally (P < 0.001). Diabetes and coronary artery disease (CAD) were prevalent in 36.2% and 28.1% of patients as compared with global prevalence of 22.2% and 21.6%, respectively (P < 0.001 for both). Antiplatelet therapy was the most common antithrombotic treatment in India. With increasing stroke risk, however, patients were more likely to receive oral anticoagulant therapy [mainly vitamin K antagonist (VKA)], but average international normalized ratio (INR) was lower among Indian patients [median INR value 1.6 (interquartile range {IQR}: 1.3-2.3) versus 2.3 (IQR 1.8-2.8) (P < 0.001)]. Compared with other countries, patients from India had markedly higher rates of all-cause mortality [7.68 per 100 person-years (95% confidence interval 6.32-9.35) vs 4.34 (4.16-4.53), P < 0.0001], while rates of stroke/systemic embolism and major bleeding were lower after 1 year of follow-up. CONCLUSION: Compared to previously published registries from India, the GARFIELD-AF registry describes clinical profiles and outcomes in Indian patients with AF of a different etiology. The registry data show that compared to the rest of the world, Indian AF patients are younger in age and have more diabetes and CAD. Patients with a higher stroke risk are more likely to receive anticoagulation therapy with VKA but are underdosed compared with the global average in the GARFIELD-AF. CLINICAL TRIAL REGISTRATION-URL: http://www.clinicaltrials.gov. Unique identifier: NCT01090362

Large expert-curated database for benchmarking document similarity detection in biomedical literature search

Document recommendation systems for locating relevant literature have mostly relied on methods developed a decade ago. This is largely due to the lack of a large offline gold-standard benchmark of relevant documents that cover a variety of research fields such that newly developed literature search techniques can be compared, improved and translated into practice. To overcome this bottleneck, we have established the RElevant LIterature SearcH consortium consisting of more than 1500 scientists from 84 countries, who have collectively annotated the relevance of over 180 000 PubMed-listed articles with regard to their respective seed (input) article/s. The majority of annotations were contributed by highly experienced, original authors of the seed articles. The collected data cover 76% of all unique PubMed Medical Subject Headings descriptors. No systematic biases were observed across different experience levels, research fields or time spent on annotations. More importantly, annotations of the same document pairs contributed by different scientists were highly concordant. We further show that the three representative baseline methods used to generate recommended articles for evaluation (Okapi Best Matching 25, Term Frequency-Inverse Document Frequency and PubMed Related Articles) had similar overall performances. Additionally, we found that these methods each tend to produce distinct collections of recommended articles, suggesting that a hybrid method may be required to completely capture all relevant articles. The established database server located at https://relishdb.ict.griffith.edu.au is freely available for the downloading of annotation data and the blind testing of new methods. We expect that this benchmark will be useful for stimulating the development of new powerful techniques for title and title/abstract-based search engines for relevant articles in biomedical research.Peer reviewe

Exploring the bacterial microbiota of colombian fermented maize dough "Masa agria" (Maiz añejo)

Masa Agria is a naturally fermented maize dough produced in Colombia, very common in the traditional gastronomy. In this study we used culture-dependent and RNA-based pyrosequencing to investigate the bacterial community structure of Masa Agria samples produced in the south west of Colombia. The mean value of cell density was 7.6 log CFU/g of presumptive lactic acid bacteria, 5.4 log cfu/g for presumptive acetic bacteria and 5.6 og CFU/g for yeasts. The abundance of these microorganisms is also responsible for the low pH (3.1-3.7) registered. Although the 16S rRNA pyrosequencing revealed that the analyzed samples were different in bacteria richness and diversity, the genera Lactobacillus, Weissella, and Acetobacter were predominant. In particular, the most common species were Lactobacillus plantarum and Acetobacter fabarum, followed by L. fermentum, L. vaccinostercus, and Pediococcus argentinicus. Several microorganisms of environmental origin, such as Dechloromonas and most of all Sphingobium spp., revealed in each sample, were detected, and also bacteria related to maize, such as Phytoplasma. In conclusion, our results elucidated for the first time the structures of the bacterial communities of Masa Agria samples obtained from different producers, identifying the specific dominant species and revealing a complete picture of the bacterial consortium in this specific niche. The selective pressure of tropical environments may favor microbial biodiversity characterized by a useful technological potential

Synthesis and Evaluation of the Fungal Activity of New Pyrazole-Carboxamides Aagainst Colletotrichum gloeosporioides

The pyrazole core has been recognized by their biological properties and included in the synthesis of modern agrochemicals. Part of these studies consists of making structural modifications to pesticides for commercial purposes to increase efficacy. In this article, we present the synthesis of four new pyrazol-4-carboxamide 8a-8d derivatives (PCD), through a four-step synthetic protocol, starting with edaravone 1 and primary amines like benzo-fused, aliphatic, and hydrazines, through a process of low environmental impact. Synthesized derivatives were evaluated against one fungal strain of Colletotrichum gloeosporioides BA3, fungus that causes several losses to farmers around the world, through in vitro sensitivity tests. The compound 8c showed better inhibiting behavior againts Colletotrichum gloeosporioides BA3, inducing a lag phase of almost 2.77 days. These results were obtained via Gompertz modeling, for the first time reported for biological evaluation of pyrazole-carboxamide derivatives against Colletotrichum gloeosporioides

Fundamentals and Applications of Chitosan

International audienceChitosan is a biopolymer obtained from chitin, one of the most abundant and renewable material on Earth. Chitin is a primary component of cell walls in fungi, the exoskeletons of arthropods, such as crustaceans, e.g. crabs, lobsters and shrimps, and insects, the radulae of molluscs, cephalopod beaks, and the scales of fish and lissamphibians. The discovery of chitin in 1811 is attributed to Henri Braconnot while the history of chitosan dates back to 1859 with the work of Charles Rouget. The name of chitosan was, however, introduced in 1894 by Felix Hoppe-Seyler. Because of its particular macromolecular structure, biocompatibility, biode-gradability and other intrinsic functional properties, chitosan has attracted major scientific and industrial interests from the late 1970s. Chitosan and its derivatives have practical applications in food industry, agriculture, pharmacy, medicine, cos-metology, textile and paper industries, and chemistry. In the last two decades, chito-san has also received much attention in numerous other fields such as dentistry, ophthalmology, biomedicine and bio-imaging, hygiene and personal care, veterinary medicine, packaging industry, agrochemistry, aquaculture, functional textiles and cosmetotextiles, catalysis, chromatography, beverage industry, photography, wastewater treatment and sludge dewatering, and biotechnology. Nutraceuticals and cosmeceuticals are actually growing markets, and therapeutic and biomedical products should be the next markets in the development of chitosan. Chitosan is also the N. Morin-Crini (*) · Laboratoire Chrono-environnement, UMR 6249, UFR Sciences et Techniques

Vitamin K antagonist control in patients with atrial fibrillation in Asia compared with other regions of the world: Real-world data from the GARFIELD-AF registry

Objective: To compare the distribution of international normalized ratios (INRs) in patients receiving vitamin K antagonist (VKA) for newly diagnosed atrial fibrillation in Eastern and Southeastern Asia and in other regions of the world (ORW) represented in the ongoing, global observational study GARFIELD-AF

Evolving antithrombotic treatment patterns for patients with newly diagnosed atrial fibrillation

Objective We studied evolving antithrombotic therapy patterns in patients with newly diagnosed non-valvular atrial fibrillation (AF) and >= 1 additional stroke risk factor between 2010 and 2015