Smartphones, smartwatches, fitness trackers, and ad-hoc wearable devices are being increasingly used to monitor human activities. Data acquired by the hosted sensors are usually processed by ...machine-learning-based algorithms to classify human activities. The success of those algorithms mostly depends on the availability of training (labeled) data that, if made publicly available, would allow researchers to make objective comparisons between techniques. Nowadays, there are only a few publicly available data sets, which often contain samples from subjects with too similar characteristics, and very often lack specific information so that is not possible to select subsets of samples according to specific criteria. In this article, we present a new dataset of acceleration samples acquired with an Android smartphone designed for human activity recognition and fall detection. The dataset includes 11,771 samples of both human activities and falls performed by 30 subjects of ages ranging from 18 to 60 years. Samples are divided in 17 fine grained classes grouped in two coarse grained classes: one containing samples of 9 types of activities of daily living (ADL) and the other containing samples of 8 types of falls. The dataset has been stored to include all the information useful to select samples according to different criteria, such as the type of ADL performed, the age, the gender, and so on. Finally, the dataset has been benchmarked with four different classifiers and with two different feature vectors. We evaluated four different classification tasks: fall vs. no fall, 9 activities, 8 falls, 17 activities and falls. For each classification task, we performed a 5-fold cross-validation (i.e., including samples from all the subjects in both the training and the test dataset) and a leave-one-subject-out cross-validation (i.e., the test data include the samples of a subject only, and the training data, the samples of all the other subjects). Regarding the classification tasks, the major findings can be summarized as follows: (i) it is quite easy to distinguish between falls and ADLs, regardless of the classifier and the feature vector selected. Indeed, these classes of activities present quite different acceleration shapes that simplify the recognition task; (ii) on average, it is more difficult to distinguish between types of falls than between types of activities, regardless of the classifier and the feature vector selected. This is due to the similarity between the acceleration shapes of different kinds of falls. On the contrary, ADLs acceleration shapes present differences except for a small group. Finally, the evaluation shows that the presence of samples of the same subject both in the training and in the test datasets, increases the performance of the classifiers regardless of the feature vector used. This happens because each human subject differs from other subjects in performing activities even if she shares with them the same physical characteristics.
The ethanolic extract of the leaves of
Piper carpunya was subjected to column chromatography and 16 pure compounds were isolated and identified. Among these, the terpenoids sitosterol, stigmasterol ...and phytol as well as the flavonoids vitexin, isovitexin, rhamnopyranosylvitexin and isoembigenin probably contribute to the significant myeloperoxidase,
Helicobater pylori and H
+, K
+-ATPase inhibitory activity observed with many of the fractions. Furthermore, neolignan, which is a DNA polymerase β lyase inhibitor, and (6S, 9S)-roseoside, that shows strong anti-bacterial activity, were isolated, for the first time, from the genus
Piper.
The leaves of
Piper carpunya Ruiz & Pav. (syn
Piper lenticellosum C.D.C.) (Piperaceae), are widely used in folk medicine in tropical and subtropical countries of South America as an anti-inflammatory, anti-ulcer, anti-diarrheal and anti-parasitical remedy as well as an ailment for skin irritations.
To study the anti-inflammatory, anti-secretory and anti-
Helicobacter pylori activities of different fractions isolated from an ethanolic extract of the leaves of
Piper carpunya, in order to provide evidence for the use of this plant as an anti-ulcer remedy. Moreover, to isolate the main compounds of the extract and relate their biological activity to the experimental results obtained with the fractions.
Sixteen fractions were obtained from the ethanolic extract (F I–XVI) and 16 pure compounds were isolated and identified from these fractions. We studied the effects of the fractions (0.1–400
μg/mL) on the release of myeloperoxidase (MPO) enzyme from rat peritoneal leukocytes, on rabbit gastric microsomal H
+, K
+-ATPase activity and anti-
Helicobacter pylori anti-microbial activity using the microdilution method (MM). The main compounds contained in the fractions were isolated and identified by
1H- and
13C NMR spectra analysis and comparison with the literature data.
Eight fractions showed inhibition of MPO enzyme (F I–IV, X, XII, XIV and XV). The highest inhibition was observed with F XIV (50
μg/mL, 60.9%,
p
<
0.001). F X and XII were the most active ones, inhibiting the gastric H
+, K
+-ATPase activity with IC
50 values equal to 22.3
μg/mL and 28.1
μg/mL, respectively. All fractions, except F XV, presented detectable anti-
Helicobacter pylori activity, with a diameter of inhibition zones ranging from 11
mm up to 50
mm. The best anti-
Helicobacter pylori activity was obtained with F III and V. Both fractions killed
Helicobacter pylori with lowest concentration values, about 6.25
μg/mL. Sixteen pure compounds were isolated, five of them are flavonoids that possess strong anti-oxidant and free radical scavenging activity, e.g. vitexin, isovitexin, and rhamnopyranosylvitexin. Terpenoids like sitosterol, stigmasterol and phytol, which have shown gastroprotective activity, and dihydrochalcones, like asebogenin, with anti-bacterial activity, were also isolated. Furthermore, the rare neolignan
1, that is a DNA polymerase β lyase inhibitor, and (6S, 9S)-roseoside, that shows strong anti-bacterial activity, were isolated, for the first time, from the genus Piper.
We suggest that the flavonoids isolated from F I and II (vitexin, isovitexin, rhamnopyranosylvitexin and isoembigenin) contribute to the anti-MPO activity, as well as to their anti-
Helicobacter pylori activity. These flavonoids may also be responsible for the important inhibition of H
+, K
+-ATPase activity. Also the phytosterols and phytol obtained from F XIV and XV could be involved in these gastroprotective activities. These results encourage us to continue phytochemical studies on these fractions in order to obtain full scientific validation for this species.
This book is conceived to promote synergy between research and industrial activities in the design and development of new drugs and, therefore, is not limited to any specific aspect of development. ...It covers the entire process from the identification of a molecular target, studies of drug–protein interactions, the modeling and optimization of the functional activity, design and chemical synthesis, biological evaluation, and the development of new pharmaceutical carriers.The original articles and reviews are focused on the design and development of new anticancer treatments, new anticancer low-molecular-weight agents as potential drug substances, and the elucidation of their mechanisms of action. The book also includes studies on novel modulators of the serotonergic system used to treat central nervous system disorders, novel agents against infectious diseases, and the development of anti-plasmodial and anti-inflammatory agents. The successful identification of new compounds for development as drug substances comes from rich sources of medicinal plants and medicinal chemistry approaches.
This book was devoted to the latest advances achieved in the antibacterial field, with a focus on the recent efforts made to develop new antimicrobial agents with novel modes of action, and a ...perspective on future directions of this line of research. Antimicrobial resistance has become a major threat to global health, and the twenty-two published articles here reported put in evidence that the discovery and development of new antibiotics are extremely challenging. The antimicrobial research covers a wide area, spanning from the design of new compounds, also supported by molecular modeling techniques, their synthesis and characterization, and biological tests.In this context, the current crisis caused by the COVID-19 pandemic, but also older threats, such as the human immunodeficiency virus or the hepatitis C virus, require greater attention than ever.The research works described in this book provide an extremely useful example of the results achieved in the field of antibacterial drug development. The search for new chemical entities was approached starting from both natural and synthetic compounds and addressing different targets. In addition, recent findings were presented and discussed highlighting the strategies to fight bacterial resistance. Detailed references to the state-of-the-art can be found in this book.We strongly encourage the wide group of readers to explore the book that we are presenting, to get inspired to develop new approaches for the diagnosis and treatment of antibacterial diseases, and to circumvent resistance issues.
Calcitonin gene-related peptide (CGRP) is a widely expressed neuropeptide that has a major role in sensory neurotransmission. The CGRP receptor is a heterodimer of the calcitonin receptor-like ...receptor (CLR) class B G-protein-coupled receptor and a type 1 transmembrane domain protein, receptor activity-modifying protein 1 (RAMP1). Here we report the structure of the human CGRP receptor in complex with CGRP and the G
-protein heterotrimer at 3.3 Å global resolution, determined by Volta phase-plate cryo-electron microscopy. The receptor activity-modifying protein transmembrane domain sits at the interface between transmembrane domains 3, 4 and 5 of CLR, and stabilizes CLR extracellular loop 2. RAMP1 makes only limited direct contact with CGRP, consistent with its function in allosteric modulation of CLR. Molecular dynamics simulations indicate that RAMP1 provides stability to the receptor complex, particularly in the positioning of the extracellular domain of CLR. This work provides insights into the control of G-protein-coupled receptor function.
Inside the biological milieu, nanoparticles with photocatalytic activity have potential to trigger cell death non‐specifically due to production of reactive oxygen species (ROS) upon reacting with ...biological entities. Silver nanoparticle (AgNP) possessing narrow band gap energy can exhibit high light absorption property and significant photocatalytic activity. This study intends to explore the effects of ROS generated due to photocatalytic activity of AgNP on antimicrobial and cytotoxic propensities. To this end, AgNP was synthesized using the principle of green chemistry from the peel extract of Punica granatum L., and was characterized using UV–Vis spectroscope, transmission electron microscope and x‐ray diffraction, and so forth. The antimicrobial activity of AgNP against studied bacteria indicated that, ROS generated at AgNP interface develop stress on bacterial membrane leading to bacterial cell death, whereas Alamar Blue dye reduction assay indicated that increased cytotoxic activity with increasing concentrations of AgNP. The γH2AX activity assay revealed that increasing the concentrations of AgNP increased DNA damaging activity. The results altogether demonstrated that both antimicrobial and cytotoxic propensities are triggered primarily due interfacial ROS generation by photocatalytic AgNP, which caused membrane deformation in bacteria and DNA damage in HT1080 cells resulting in cell death.
Seafood comprising of both vertebrate and invertebrate aquatic organisms are nutritious, rich in omega-3 fatty acids, essential vitamins, proteins, minerals and form part of healthy diet. However, ...despite the health and nutritional benefits, seafood is highly perishable. Spoilage of seafood could be as a result of microbial activity, autolysis or chemical oxidation. Microbial activity constitutes more spoilage than others. Spoilage bacteria are commonly Gram negative and produce off odours and flavours in seafood as a result of their metabolic activities. Storage temperature, handling and packaging conditions affect microbial growth and thus the shelf-life of seafood. Due to the complexity of the microbial communities in seafood, culture dependent methods of detection may not be useful, hence the need for culture independent methods are necessary to understand the diversity of microbiota and spoilage process. Similarly, the volatile organic compounds released by spoilage bacteria are not fully understood in some seafood. This review therefore highlights current knowledge and understanding of seafood spoilage microbiota, volatile organic compounds, effects of storage temperature and packaging conditions on quality of seafood.
•Spoilage microbiota in seafood•Complexity of spoilage microbial communities in seafood•Effects of storage temperature and packaging conditions on quality of seafood•Diversity of volatile organic compounds produced by seafood spoilage bacteria
Aim
To evaluate the antifungal activity of extracts of Chamaecostus cuspidatus against Candida and Trichophyton species.
Methods and Results
Crude ethanol extracts of leaves, stems and rhizomes were ...prepared and evaluated for antimicrobial activity. Only the rhizomes extract (RE) showed antifungal activity but had no inhibitory effect against bacteria (Staphylococcus aureus and Escherichia coli). The RE was then submitted to liquid‐liquid partition with hexane (Hex), dichloromethane, chloroform, ethyl acetate and water. The Hex fraction (Hex Fr) from the RE was found to have the best antifungal effect. Three known saponins were isolated from the Hex Fr, of which two (dioscin and aferoside A) showed good antifungal activity. In addition, Hex Fr and the two bioactive compounds had no antibacterial effect, but exhibited fungicidal activity, caused significant changes in the morphology of the fungal cells and showed anti‐Candida albicans biofilm activity. Finally, the bioactive plant products presented greater selectivity for fungal cells over normal human cells.
Conclusions
The rhizomes of C. cuspidatus have bioactive saponins that function as effective antifungals against Candida and Trichophyton species, and have antibiofilm activity against C. albicans.
Significance and Impact of the Study
Chamaecostus cuspidatus REs may have potential clinical application towards the management of superficial mycoses caused by Candida and Trichophyton species.
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