bluuebunny/crossref_metadata_2025 huggingface dataset:
Case of Eagle Fern (Pteridium Aquilinum) Poisoning on a Pig Farm
Authors: Waret-Szkuta Agnès , Jégou Laura , Lucas Marie Noelle , Gaide Nicolas , Morvan Hervé , Martineau Guy-Pierre
Published: October 2020

Background: Free-range pig farming represents a minor proportion of pig production in France but attracts an increasing number of farmers because of societal expectations and the opportunity to use fodder consumed in the meadow. However, this type of farming faces several sanitary challenges, including biosecurity, parasitic management, and contact with wild fauna and pathogenic flora. Case presentation: Two Gascon pigs raised on an outdoor fattening farm in the Hautes-Pyrenees department of France were submitted after sudden death for necropsy at the National Veterinary School of Toulouse. The pigs were of two different breeds but from the same batch of 85 animals that had grazed on a 4-hectare plot of land being used for the first time. The combination of an in-depth interview with the breeder, the epidemiological information available, and the necropsy and histology examinations enabled the hypothesis of great eagle fern intoxication. Despite the small sample of animals available for diagnosis, the success of the administered therapy helped to confirm our diagnosis. In the short term, it was recommended that the animals be prevented access to the eagle fern by changing their pasture or by removing the plants. Vitamin B1 was administered in the feed in the amount of 1 mL per 10 kg body weight for two days (Ultra B®: 4.46 mg thiamine and 2.06 mg pyridoxine (vitamin B6) per kg body weight per day). A remarkable remission was observed, allowing 6 of 12 intoxicated animals with symptoms to survive (therapeutic success rate: 50%), but without compensating for the loss of the initial body condition. In total, out of the 85 animals in the batch after this intoxication, 6 animals died and 6 recovered.Conclusion: The interest of this report lies in the scarcity of eagle fern intoxication cases reported in the literature, although it may become a significant problem along with the development of outdoor rearing. In this context, it should be included in the differential diagnosis of nervous system symptoms in swine. The case also underlines the importance of anamnesis and discussions with the farmer to guide the diagnosis and reminds us that this step is essential in the clinical process.
The loss of DLG2 isoform 7/8, but not isoform 2, is critical in advanced staged neuroblastoma
Authors: Keane Simon , Martinsson Tommy , Kogner Per , Ejeskar Katarina
Published: October 2020

BACKGROUNDNeuroblastoma is a childhood neural crest tumor showing large clinical and genetic heterogeneity, one form displaying 11q-deletion is very aggressive. It has been shown that 11q-deletion results in decreased expression of DLG2, a gene residing in the deleted region. DLG2 has a number of different isoforms with the main difference is the presence or absence of a L27 domain. The L27 domain containing DLG proteins can form complexes with CASK/MPP and LIN7 protein family members, which will control cell polarity and signaling. METHODSWe evaluated the DLG gene family and the LIN7 gene family for their expression in differently INSS staged neuroblastoma from publically available neuroblastoma data and primary tumors, we included two distinct DLG1 and DLG2 N-terminal transcript isoforms encoding L27 domains for their expression. Functionality of DLG2 isoforms and of LIN7A were evaluated in the 11q-deleted neuroblastoma cell line SKNAS.RESULTSIn neuroblastoma only two DLG2 isoforms were expressed: isoform 2 and isoform 7/8. Using the array data we could determine that higher expression of DLG members that contain L27 domains correlated to better survival and prognosis. Whilst DLG1 showed a decrease in both isoforms with increased INSS stage, only the full length L27 containing DLG2 transcripts DLG2-isoform 7/8 showed a decrease in expression in high stage neuroblastoma. We could show that the protein encoded by DLG2-isoform 7 could bind to LIN7A, and increased DLG2-isoform 7 gene expression increased the expression of LIN7A, this reduced neuroblastoma cell proliferation and viability.CONCLUSIONWe have provided evidence that gene expression of the L27 domain containing DLG2-isoform 7/8 but not L27 domain lacking DLG2-isoform 2 is disrupted in neuroblastoma, in particular in the aggressive subsets of tumors. The presence of the complete L27 domain allows for the binding to LIN7A, which will control cell polarity and signaling, thus affecting cancer cell viability.
Associations of Total Serum IgE and Peripheral Blood Eosinophils with Childhood Asthma: a Longitudinal Retrospective Study
Authors: LEE JYH-HONG , Chu Ai-Lin , Hsiao Shu-Ya , Chang Kuei-Ying , Yang Yao-Hsu , Lin Yu-Tsan , Wang Li-Chieh , Yu Hsin-Hui , Hu Ya-Chiao , Chiang Bor-Luen
Published: October 2020

BackgroundChildhood asthma is a heterogeneous disease. The relationship of total serum IgE and peripheral blood eosinophil with childhood asthma are controversial. To determine whether total serum IgE and peripheral blood eosinophil are associated with long-term lung function, asthma severity and asthma control in children.MethodsWe conducted a longitudinal retrospective study in 383 childhood asthma patients with total serum IgE and peripheral blood eosinophil obtained at baseline. Peak expiratory flow (PEF) variability, predicted PEF percentage, asthma severity, asthma control test (ACT) score, and asthma control from each follow-up visit were recorded as phenotype outcomes. We correlated serum IgE and blood eosinophil with phenotype outcomes using generalized estimating equations. Additionally, we compared expression of microRNA in peripheral blood cells from nonallergic versus allergic patients.ResultsTotal serum IgE was positively associated with asthma severity (OR = 1.0014, P = 0.0071). Peripheral blood eosinophil was positively related to PEF variability (OR = 1.0052, P = 0.0002). Association of inhaled corticosteroids (ICS) dose with phenotype outcomes were not significant. Compared with allergic patients, children with nonallergic asthma had higher asthma severity. We identified six interaction pathways specific to IgE from eight top differentially expressed microRNAs. ConclusionsBeside asthma control, total serum IgE is predictive of long-term asthma severity and peripheral blood eosinophil is closely related to PEF variability. We suggest that total serum IgE might be involved in modulating disease severity of both allergic and nonallergic asthma while peripheral blood eosinophilia reflects the status of longitudinal lung function.
DEVELOPMENT OF THE EMULGE LFOR THE ANDROGENIC ALOPECIA TREATMENT
Authors: Yarema Inna , Fedorovska Marianа , Polovko Natalia
Published: October 2020

Androgenic alopecia (AGA) is the most common alopecia that is heritable, androgen-dependent and occurs in both sexes with defined patterns such as Male pattern hair loss in men and Female pattern hair loss in women. AGA affects at least 50 % of men by the age of 50 years, and up to 70 % of all males in later life.

The aim.The research was aimed to substantiate the optimal concentration of excipients and active pharmaceutical ingredients (APIs) of the emulgel intended for the topical treatment of androgenic alopecia.

Materials and methods. In this study the samples of the emulgel bases containing different carbomer Ultrez10 concentrationsin the range of 0.3–0.6 % and its neutralizers (0.1 % of potassium sorbate and 0 % or 0.2 % of triethanolamine) were used. Colloidal and thermal stability, pH, rheological properties (structural viscosity, mechanical stability, degree of thixotropy) of these samples were determined. The emulgel samples with different percentages of the Serenoa repens dry extract and the Sophora japonica tincture were used in the biopharmaceutical studies. The samples of the emulgel with the antioxidant butylhydroxytoluene different concentrations (0 %, 0.01 %, 0.02 %, 0.03 %) were used to determine acid value during 1 year of the emulgel storage.

Results and discussion. It was experimentally substantiated the optimal ratio of the emulgel ingredients that provide good APIs release and necessary consumer properties of the semi-solid remedy like application compliance, safety and storage stability.

Conclusions. Physicochemical, rheological and biopharmaceutical properties of emulgel bases have been studied. It was found that the base №2 (in which the concentrations of Carbomer Ultraz 10, potassium sorbate and triethanolamine are 0.3 %, 0.1 %, 0.2 % respectively) possessed the optimal properties. Considering the results of the complete range of experimental research it was developed the final formulation of the emulgel intended for AGA treatment which included the concentration of the APIs, neutralizers, preservatives, antioxidant and fragrance.
Reply to “Comment on Geodesic Cycle Length Distributions in Delusional and Other Social Networks”
Authors: Stivala Alex
Published: October 2020

Martin (2020) describes a misinterpretation of exponential random graph (ERGM) parameters in my contribution (Stivala 2020), with the use of this parametric model obscuring, rather than illuminating, the data. He suggests that this is symptomatic of a trend in the social networks community towards a methodological monoculture focussed on the use of ERGMs. In this Reply I try to clarify how this situation arose in this specific case, and address some more general issues Martin raises, including the use of nodal covariates, what we can learn from ERGMs, and methodological monoculturalism in social network research.
The Unobserved Economy – Invisible Production in Households. The Household Production Satellite Account and the National Time Transfer Account
Authors: Marszałek Marta
Published: October 2020

Standard measures of economic activity relate to goods and services offered by the market. Stiglitz’s report, however, suggests that not only monetary value or economic products create welfare, but non-monetary components should also be included in the System of National Accounts. Although household production is registered in official statistics, the main part of it, i.e. nearly 75-80% of the total home production remains outside of the GDP. The Household Production Satellite Account (HHSA) is a macroeconomic analysis covering both market and non-market home production. The National Time Transfer Accounts (NTTA) is, next to HHSA, an analysis aimed to register and observe the directions of transfers and to present the recipients and givers of home production. Regular estimations provided by the HHSA and NTTA may prove a valuable supporting tool to national accounts, pension systems, or social policy as they provide a great deal of macroeconomic information regarding households, their economic and living conditions, social changes, and welfare.
Ferropyrosmalite-bearing fluid inclusions in the North Patagonian Andes metasedimentary basement, Argentina: A record of regional metasomatism
Authors: Sosa Graciela , Oriolo Sebastián , van den Kerkhof Alfons , González Pablo Diego , Olaizola Ezequiel , Bechis Florencia
Published: October 2020

Quartz segregations in paragneisses from the Paleozoic basement of the North Patagonian Andes contain highly saline multiphase fluid inclusions with the rare daughter mineral ferropyrosmalite detected by Raman analysis, besides halite, sylvite, hematite, and/or magnetite. During heating experiments, L-V homogenization occurs (256–515 °C), followed by halite dissolution (287–556 °C) and the dissolution of ferropyrosmalite at 550–581 °C. The latter phase transition triggers the growth of clinoamphibole crystals according to the following idealized reactions, written for potential end-members:

4 F e 8 S i 6 O 15 [ ( O H ) 6 C l 4 ] + 6 C a 2 + ( a q ) Ferropyrosmalite ↔ 3 C a 2 F e 5 S i 8 ↔ O 22 ( O H ) 2 + 17 F e 2 + ( a q ) + 16 C l − ( a q ) + 12 O H − + 3 H 2 Ferro-actinolite F e 8 S i 6 O 15 [ ( O H ) 6 C l 4 ] + 2 C a 2 + ( a q ) Ferropyrosmalite + Fe 3 + ( aq ) + 2Al 3 + ( aq ) + Na + ( aq ) + H 2 O ↔ Na C a 2 ( Fe 4 2 + F e 3 + ) ( Al 2 Si 6 ) ↔ O 22 Cl 2 + 4 F e 2 + ( a q ) + 2 C l − ( a q ) + 4 H 2 Chloro-hastingsite

Ferropyrosmalite ↔ Chloro-hastingsite The amphibole resembles the composition of ferro-actinolite but also has striking similarities with chloro-hastingsite, as indicated by Raman spectroscopy. During the heating experiment, hematite (when present) transforms to magnetite by the uptake of H2, whereas inclusions without Fe-oxides contain traces of H2 after the reaction. This mineral transformation shows that ferropyrosmalite might result from the retrograde re-equilibration of amphibole with the brine, implying the uptake of Fe2+, Cl–, and H2O and the enrichment of Ca2+ in the brine. Pervasive fluid flow and fluid-assisted diffusion are recorded by channel way microstructures, healed microfractures, and dissolution-reprecipitation phenomena, as demonstrated by cathodoluminescence microscopy. These alkali- and FeCl2-rich brines, derived from magmatic sources and of possible Mesozoic age, were related to regional metasomatism, coeval with widespread granitoid activity.
Cultural embeddedness of family businesses succession planning: a comparative study of Poland and Indonesia
Authors: Bąkiewicz Anna
Published: October 2020

The research investigates the bases of succession planning in family businesses (FB), especially the cultural background of the phenomenon. The significance of the issue under study comes from the importance of family business in every economy and the delicate matter of succession as an important business development element. The research is based on the observation that the succession determinants are still outside the mainstream of the research. In this study, it is hypothesized that succession planning is influenced by cultural background. The investigation is done by performing a comparative analysis of family businesses’ potential successors from the culturally distant countries: Poland and Indonesia. An empirical survey-based method is applied to investigate the younger generation’s involvement in preparations for the transfer of the family business. The differences in the approach to the younger generation’s succession identified in the survey are not related to such factors as age, size, or succession experience of the business. Instead, there are premises to say that the differences come from the family and business culture based on national specificity. First-hand support for the cultural embeddedness of FB succession planning was found. Furthermore, the results also reaffirm the doubts concerning the importance of post-communist countries’ economic transformation for succession planning. The empirical study confirms the expectations that the specificity of cultural background in Poland could be especially harmful to succession planning in the family business.
Kaynaştırma Öğrencilerinin Fen Bilimleri Dersi STEM Çalışmalarının Değerlendirilmesi
Authors: BALÇIN Muhammed Doğukan , YILDIRIM Mehtap
Published: October 2020

Günümüzde, özel gereksinimli öğrencilerin sosyal anlamda sınıf ortamında akranları ile kaynaştırılabildikleri ancak yeterli akademik eğitime ulaşamadıkları görülmektedir. Bu nedenle kaynaştırma öğrencilerinin akademik düzeylerinin yükseltilmesi için destek eğitim odaları kullanılmaktadır. Bu araştırmada destek eğitim odalarında verilen fen bilimleri dersi kapsamında özel gereksinimli öğrencilerin STEM çalışmalarındaki yeterliklerinin değerlendirilmesi amaçlanmıştır. Araştırma bir durum çalışmasıdır. Çalışma grubunu bir devlet ortaokulunun yedinci sınıfında öğrenim gören tam zamanlı kaynaştırma eğitimi alan üç özel gereksinimli birey oluşturmaktadır. Veri toplama aracı olarak; bilgi testi, kontrol listesi, materyal değerlendirme formu, STEM becerileri dereceli puanlama anahtarı, öz değerlendirme formu ve yarı yapılandırılmış görüşme formu kullanılmıştır. Veri analizinde içerik ve betimsel analizden yararlanılmıştır. Araştırma sonucunda; öğrencilerin fen bilgilerini gerçekleştirdikleri materyallerine yansıtabildikleri fakat matematik, teknoloji ve mühendislikle bağdaştıramadıkları belirlenmiştir. Ayrıca öğrencilerin tasarımlarını planlayabildikleri, zihinlerinde oluşturabildikleri ancak çizime dökemedikleri görülmüştür. Buna rağmen tasarıma dönüştürmede başarı sağlayabildikleri belirlenmiştir. Çalışmanın sonucunda, kaynaştırma öğrencilerinin STEM çalışmalarına dâhil edilmeleri önerilmektedir.
Penyusunan Petunjuk Praktikum Kimia Berorientasi Chemo-Entrepreneurship pada Larutan Penyangga
Authors: Najib Ainun , Misrochah Nana
Published: October 2020

Penelitian penyusunan petunjuk praktikum berorientasi chemo-entrepreneurship (CEP) pada materi larutan penyangga berdasarkan karakteristik peserta didik yang lebih menyukai metode praktikum sebagai proses pembelajaran, namun hasil observasi di sekolah belum mempunyai petunjuk praktikum yang baku dan valid agar praktikum yang dilaksanakan dapat terarah dan tersetruktur sehingga tujuan pembelajaran dapat tercapai dengan maksimal. Metode penyusunan mengadopsi metode ADDIE yang terdiri dari tahap Analyze, Desaign, Development, Implementation, and Evaluations Akan tetapi merujuk pada surat edaran Menteri Pendidikan dan kebudayaan nomor 4 tahun 2020 tentang pelaksanaan Pendidikan dalam masa darurat penyebaran COVID-19 maka peneliti hanya sampai pada tahap Development (Pengembangan). Produk divalidasi oleh dua dosen ahli materi dan satu dosen ahli media dengan hasil validasi ahli materi satu memperoleh persentase sebesar 91,11%, validator ahli materi dua dengan persentase sebesar 75,55%, dan validator ahli media sebesar 90%. Hasil persentase rata-rata dari ketiga validator sebesar 85,53%.
Respon Mahasiswa terhadap Pembelajaran Interaktif dengan Animasi 3D melalui Powerpoint
Authors: Marpaung Dewi Natalia , Pongkendek Jesi Jecsen
Published: October 2020

Pembelajaran harus di dukung oleh dosen yang kreatif untuk menciptakan media pembelajaran interaktif agar mahasiswa lebih aktif, kreatif dan inovatif selama proses pembelajaran berlangsung. Tujuan dari penelitian ini adalah untuk mengetahui respon mahasiswa terhadap  mediapembelajaran interaktif  yang digunakan oleh dosen dengan menerapkan animasi 3D melalui Powerpoint, penelitian ini adalah penelitian deskriptif, penelitian ini dilakukan di universitas musamus jurusan pendidikan kimia. Sampel dalam penelitian ini terdiri dari 20 orang mahasiswa. Pengumpulan data dilakukan melalui google form yang dapat diakses oleh masing-masing mahasiswa.  Berdasarkan hasil penelitian yang dilakukan mahasiswa memberikan respon yang positif terhadap animasi 3D yang digunakan oleh dosen dengan nilai  4,5 dari 5.0 dan dikategorikan sangat baik. Sehingga media pembelajaran interaktif dengan menggunakan animasi 3D melalui powerpoint  dapat digunakan untuk menjadikan mahasiswa termotivasi untuk belajar di dalam kelas dan membantu pemahaman mahasiswa terhadap materi yang diajarkan oleh dosen.
Islamic architectural ecological philosophy in contemporary Egyptian residence
Authors: Albasyoni Marwa Elsayed Mohamed
Published: October 2020

The research discusses the relation between the modern ecological design trends and the preservation of the identity taking advantage of the ecological Islamic design in contemporary Egyptian residence, where the research aims to avoid interior designs that help to drain energy and resources, polluting the environment and adverse impact on human health, also it aims to philosophy preservation of Islamic content in interior design re-using Islamic vocabulary environmental substances in the contemporary Egyptian residence. Finding the formulation of the contemporary Egyptian residence design by Islamic heritage vocabulary with its environmental content.
Lateralization of vigilance in geese: influence of flock size and distance to the source of disturbance
Authors: Zaynagutdinova Elmira , Karenina Karina , Giljov Andrey
Published: October 2020

Left-eye preference, implicating right hemisphere advantage, is typical for vigilant behaviour of many vertebrates. Nevertheless, lateralization of vigilance may be manifested in other ways, such as different reactions to the danger viewed with the right and left eye. Here, we studied one-side biases in the orientation of white-fronted geese Anser albifrons feeding in flocks at different distances to the source of anthropogenic disturbance (a road with traffic) and in flocks of different sizes. The birds which used the left eye to monitor the road were at shorter distances to the road than the birds which used the right eye. The tendency to monitor the road with the right eye decreased with increasing flock size. Trade-offs between feeding, social and vigilant behaviour could explain these tendencies.
Accumulation of milk increases the width of tight junctions in the epithelium of mouse mammary alveoli
Authors: Kruglova Natalia , Razgovorova Irina , Amasheh Salah , Markov Alexander
Published: October 2020

The study of the molecular mechanisms of maintaining the integrity of the epithelium during mechanical stress remains a relevant problem in the physiology of tissue barriers. A methodical approach has been applied which makes it possible to reproduce mechanical pressure on the apical region of cells in vivo and to study the participation and role of tight junctions in maintaining the integrity of the epithelial structure. Mammary gland tissue specimens from lactating control mice and animals after a 20-h interruption of suckling were prepared and the width of the tight junction of the secretory epithelium was analyzed. At the ultrastructural level, it was shown that accumulation of milk caused a significant increase in the width of the tight junction between epithelial cells. In the control group, the width of this structure was 2.1 ± 0.1 µm; in the experimental group — 4.2 ± 0.1 μm. The marked increase in the width of tight junctions between epithelial cells is in accordance with an observed increase in the level of claudin-1 and -3 in the secretory epithelium and can be interpreted as adaptive changes aimed at maintaining the structure of the alveoli.
Degradation of hydroxypropyl guar gum at wide pH range by a heterogeneous Fenton-like process using bentonite-supported Cu(0)
Authors: Zhou Ling , Xu Zhongying , Zhang Jie , Zhang Zhifang , Tang Ying
Published: October 2020

To seek for efficient Fenton-like oxidation processing for treatment of waste fracturing fluid containing hydroxypropyl guar gum (HPGG), in heterogeneous reaction, five bentonite-supported zero-valent metal catalysts were prepared by liquid-phase reduction. The results showed that the bentonite-supported zero-valent copper exhibited best catalytic performance, attributed to the high dispersion of active sites of zero-valent copper. The effects of the most relevant operating factors (H2O2 concentration, catalyst dosage, temperature and pH) were evaluated in detail. Moreover, the chemical oxygen demand removal rate of HPGG can achieve 76% when the reaction time was selected at 45 min under optimal experimental conditions. The stability evaluation showed that the catalytic performance was almost unaffected after the catalyst was recycled and used once more showing the good stability of the bentonite-supported zero-valent copper in the application process.
Assessment of Phytochemicals and Herbal Formula for the Treatment of Depression through Metabolomics
Authors: Wang Xu , Lu Guanyu , Liu Xuan , Li Jinhui , Zhao Fei , Li Kefeng
Published: October 2020

Depression is a widespread and persistent psychiatric disease. Due to various side effects and no curative
treatments of conventional antidepressant drugs, botanical medicines have attracted considerable attention
as a complementary and alternative approach. The pathogenesis of depression is quite complicated and unclear.
Metabolomics is a promising new technique for the discovery of novel biomarkers for exploring the potential
mechanisms of diverse diseases and assessing the therapeutic effects of drugs. In this article, we systematically
reviewed the study of botanical medicine for the treatment of depression using metabolomics over a period
from 2010 to 2019. Additionally, we summarized the potential biomarkers and metabolic pathways associated
with herbal medicine treatment for depression. Through a comprehensive evaluation of herbal medicine as
novel antidepressants and understanding of their pharmacomechanisms, a new perspective on expanding the application
of botanical medicines for the treatment of depression is provided.
Ferrocene and Organotin (IV) Conjugates Containing Amino Acids and Peptides: A Promising Strategy for Searching New Therapeutic and Diagnostic Tools
Authors: Román Tatiana , Ramirez David , Fierro-Medina Ricardo , Santillan Rosa , Farfán Norberto
Published: October 2020

Organometallic complexes are an important class of synthetic reagents and are of
great interest due to their versatility and wide biological application. The cationic nature of the
coordination nucleus facilitates its interaction with biological molecules such as amino acids,
proteins, and nucleic acids. The functionalization of peptides or amino acids with organometallic
motifs is a novel strategy for the design and development of molecules with greater biological
activity, stability in biological environments, and selectivity for specific targets, which
make them valuable tools for designing and obtaining molecules with therapeutic applications.
The physicochemical properties of ferrocene make it ideal for drug development, due to its
structure, stability in aqueous solutions, redox properties, and low toxicity. In the same way,
organotin (IV) derivatives have great potential for drug development because of their multiple
biological activities, wide structural versatility, high degree of stability, and low toxicity.
However, the synthesis of these drugs based on organometallic molecules containing ferrocene or organotin (IV) is
quite complex and represents a challenge nowadays; for this reason, it is necessary to design and implement procedures
to obtain molecules with a high degree of purity, in sufficient quantities, and at low cost. This review describes
the strategies of synthesis used up to now for the preparation of organometallic amino acids and peptides
containing ferrocene or organotin (IV) derivates, as well as their impact on the development of therapeutic agents.
Genetic Engineering of AAV Capsid Gene for Gene Therapy Application
Authors: Liu Yunbo , Zhang Xu , Yang Lin
Published: October 2020

Adeno-associated virus (AAV) is a promising vector for in vivo gene therapy because of
its excellent safety profile and ability to mediate stable gene expression in human subjects. However,
there are still numerous challenges that need to be resolved before this gene delivery vehicle is
used in clinical applications, such as the inability of AAV to effectively target specific tissues, preexisting
neutralizing antibodies in human populations, and a limited AAV packaging capacity.
Over the past two decades, much genetic modification work has been performed with the AAV capsid
gene, resulting in a large number of variants with modified characteristics, rendering AAV a
versatile vector for more efficient gene therapy applications for different genetic diseases.
1,2,4-triazoles Clubbed Pyrimidine Compounds with Synthesis, Antimicrobial, Antituberculosis, Antimalarial, and Anti-protozoal Studies
Authors: Patel Navin B. , Soni Hetal I. , Parmar Rahul B. , Chan-Bacab Manuel J. , Rivera Gildardo
Published: October 2020

:

Triazoles are famous as an antifungal agent. Itraconazole and fluconazole are the best examples of antifungal drugs available in the market, which consist an active triazole moiety. Pyrimidines are also bioactive molecules which shows multiple bioactivity. It’s an effort to synthesize pyrimidine clubbed triazole to enhance bioactivity. To synthesize new active pyrimidine clubbed triazole biomolecule and to evaluate these new products for better drug potential as antimicrobial, an-tituberculosis, antimalarial, and anti-protozoal. N-[4-(substituted phenyl)-6-(substituted aryl) pyrimidine-2-yl]-2-[(4H-1,2,4-triazol-4-yl)amino]acetamide(3A-J) were synthesized by different method as cyclization, condensation, purification and crystallization. The newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR and mass spectral analysis and screened for antibacterial, antifungal, anti-tuberculosis, antimalarial, and anti-protozoal activities. These com-pounds satisfied the bioactive response and simple way for the synthesis.
New Chalcone Derivatives with Pyrazole and Sulfonamide Pharmacophores as Carbonic Anhydrase Inhibitors
Authors: Tugrak Mehtap , Gul Halise Inci , Akincioglu Hulya , Gulcin Ilhami
Published: October 2020

Background:

Compound containing sulfonamide, pyrazole and chalcone groups are
important in medicinal chemistry. They have a wide range of biological activities, including carbonic
anhydrase (CA) inhibitory activities.

Introduction:

Carbonic anhydrase I and II inhibitors are used for the treatment of diseases, such as
retinal and cerebral edema (CA I), epilepsy, and glaucoma (CA II). However, the currently available
drugs have some limitations or side effects. Thus, there is a need for new drug candidates to
overcome these issues. In this study, a series of compounds, (E)-4-(4-(3-aryl)-3-oxoprop-1-en-1-yl)-
3-phenyl-1H-pyrazol-1-yl) benzenesulfonamides MS4-MS10, were designed to discover new CA
inhibitors using a hybrid approach.

Methods:

Compounds MS4-MS10 were synthesized as shown in Scheme 1, and their chemical
structures were confirmed by 1H NMR, 13C NMR, and HRMS spectra. The CAs (E.C.4.2.1.1) inhibitory
effects of MS4-MS10 were tested on the hCA I and II isoenzymes using previously reported
procedures.

Results:

The CA inhibitors MS4–MS10 gave IC50 values (nM) of 27.8–87.3 towards hCA I and
24.4–54.8 towards hCA II while the IC50 values for reference drug acetazolamide were 384.2 (hCA I)
and 36.9 (hCA II). MS7 and MS9 exhibited 13.8 (hCA I) and 1.5 (hCA II) times more potent CA
inhibition than the reference compound acetazolamide, respectively.

Conclusion:

MS7 (Ar: 2,4,5-trimethoxy phenyl) and MS9 (Ar: 3,4-dimethoxy phenyl) were the
most promising compounds of our series with the lowest IC50 values towards hCA I and hCA II,
respectively, and can be considered for further studies.
Virtual Screening of Chinese Medicine Small Molecule Compounds Targeting SARS-CoV-2 3CL Protease (3CL pro)
Authors: He Qingxiu , Chen Xin , Yang Xi , Li Guangpin , Guo Haiqiong , Chu Han , Lin Zhihua , Wang Yuanqiang
Published: October 2020

Background:

The outbreak of coronavirus disease 2019 (COVID-19) caused by severe
acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has attracted worldwide attention due to
its high infectivity and pathogenicity.

Objective:

The purpose of this study is to develop drugs with therapeutic potentials for COVID-19.

Methods:

we selected the crystal structure of 3CL pro to perform virtual screening against natural
products in the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform
(TCMSP). Then, molecular dynamics (MD) simulation was carried out to explore the binding
mode between compounds and 3CL pro.

Results and Discussion:

A total of 6 candidates with good theoretical binding affinity to 3CL pro were
identified. The binding mode after MD shows that hydrogen bonding and hydrophobic interaction play
an important role in the binding process. Finally, based on the free binding energy analysis, the candidate
natural product Gypenoside LXXV may bind to 3CL pro with high binding affinity.

Conclusion:

The natural product Gypenoside LXXV may have good potential anti-SARS-COV-2
activity.
Synthesis, Characterization and Biological Studies of Organoselenium trans-Palladium(II) Complexes
Authors: Raković Ivana , Bogojeski Jovana , Mladenović Katarina , Petrović Angelina , Divac Vera , Mihailović Kristina , Jovicić Biljana Popovska , Kostić Marina , Canović Predrag , Milivojević Nevena , Zivanović Marko , Radojević Ivana
Published: October 2020

Background:

Over the years, transition metal complexes have exhibited significant antimicrobial
and antitumor activity. It all started with cisplatin discovery, but due to the large number of
side effects it shows, there is a growing need to find a new metal-based compound with higher selectivity
and activity on more tumors.

Objectives:

Two novel trans-palladium(II) complexes with organoselenium compounds as ligands,
[Pd(L1)2Cl2] (L1 = 5-(phenylselanylmethyl)-dihydrofuran-2(3H)-one) and [Pd(L2)2Cl2] (L2 = 2-
methyl-5-(phenylselanylmethyl)- tetrahydrofuran) were synthesized, in the text referred to as Pd-Se1
and Pd-Se2. Also, a structurally similar trans-palladium(II) complex, [Pd(L3)2Cl2] (L3= 2,2-
dimethyl-3-(phenylselanylmethyl)-tetrahydro-2H-pyran) was synthesized according to an already
published work and is referred to as Pd-Se3. The interaction of synthesized complexes with DNA and
bovine serum albumin was observed. Also, antimicrobial activity and in vitro testing, cell viability,
and cytotoxic effects of synthesized ligands and complexes on human epithelial colorectal cancer cell
line HCT-116 were studied. Molecular docking simulations were performed to understand better the
binding modes of the complexes reported in this paper with DNA and BSA, as well as to comprehend
their antimicrobial activity.

Methods:

The interactions of the synthesized complexes with DNA and bovine serum albumin were
done using UV-Vis and emission spectral studies as well as docking studies. Antimicrobial activity
was tested by determining the minimum inhibitory concentrations (MIC) and minimum microbicidal
concentration (MMC) using the resazurin microdilution plate method. Cytotoxic activity on cancer
cells was studied by MTT test.

Results:

The Pd(II) complexes showed a significant binding affinity for calf thymus DNA and bovine
serum albumin by UV-Vis and emission spectral studies. The intensity of antimicrobial activity varied
with the complexes Pd-Se1 and Pd-Se3, showing significantly higher activity than the corresponding
ligand. The most significant activity was shown on Pseudomonas aeruginosa. Under standardized
laboratory conditions for in vitro testing, cell viability and cytotoxic effects of synthesized
ligands and complexes were studied on human epithelial colorectal cancer cell line HCT-116, where
Pd-Se2 showed some significant cytotoxic effects.

Conclusion:

The newly synthesized complexes have the potential to be further investigated as metallodrugs.
Design and Synthesis of Novel Anti-inflammatory/Anti-ulcer Hybrid Molecules with Antioxidant Activity
Authors: Chaudhari Bhim Bahadur , Bali Alka , Balaini Ajitesh
Published: October 2020

Background:

NSAIDs are the most widely prescribed medications worldwide for their
anti-inflammatory, antipyretic, and analgesic effects. However, their chronic use can lead to several
adverse drug events including GI toxicity. The selective COX-2 inhibitors developed as gastrosparing
NSAIDs also suffer from serious adverse effects which limit their efficacy.

Objective:

Local generation of reactive oxygen species is implicated in NSAID-mediated gastric ulceration
and their combination with H2 antagonists like famotidine reduces the risk of ulcers. The
objective of this work was to design and synthesize novel methanesulphonamido isoxazole derivatives
by hybridizing the structural features of NSAIDs with those of antiulcer drugs (ranitidine, famotidine,
etc.) to utilize a dual combination of anti-inflammatory activity and reducing (antioxidant)
potential.

Method:

The designing process utilized three dimensional similarity studies and utilized an isoxazole
core having a potential for anti-inflammatory as well as radical scavenging antioxidant activity.
The compounds were assayed for their anti-inflammatory activity in established in vivo models. The
in vitro antioxidant activity was assessed in potassium ferricyanide reducing power (PFRAP) assay
employing ascorbic acid as the standard drug. Results: Compounds 5, 6, 9 and 10 showed antiinflammatory
activity comparable to the standard drugs and were also found to be non-ulcerogenic at
the test doses. Compounds 6-10 exhibited good antioxidant effect in the concentration range of 1.0-
50.0 μmol/ml. The test compounds were also found to comply with the Lipinski rule suggesting good
oral absorption.

Conclusion:

A new series of isoxazole based compounds is being reported with good antiinflammatory
activity coupled with antioxidant potential as gastro-sparing anti-inflammatory agents.
Method and Device for Production of Driving Force in Underwater Floating Vehicle
Authors: Auzins Janis , Eimanis Marcis
Published: October 2020

Background:

In this paper, we present a completely new type of propulsion system where
thrust force is created by the helicoidal shape of the hull rather than screw propellers. The method and
device have been recently patented. The inspiration comes from nature, the world of bacteria, where
some organisms have been using the drilling motion or rotating flagella to move in fluid media for several
million years. The hull of device consists of three parts – bow and stern (which create the propulsion
force) and the middle part which can serve as a cargo compartment containing all control mechanisms
and communications. The Cardan-joint mechanism that allows changing the direction of the vehicle
is actuated by bending drives. A bending drive velocity control algorithm is proposed for the automatic
control of vehicle movement direction.

Objective:

Development of a new propulsion system for underwater vehicles.

Methods:

The watercraft dynamics were simulated using multibody simulation software MSC Adams. For accurate
interaction with medium, polynomial metamodels were created on the basis of computer experiments with CFD software.
Computational Fluid Dynamics software was used for flow interaction with the prototype geometry, implementing the
same idea that is used in wind tunnel experiments.

Results and Conclusion:

The results are compared with measurements of the physical prototype, built at the Institute of
Mechanics and Mechanical Engineering of Riga Technical University. These results showed good validation with
mathematical simulation and confirmed the effectiveness and future potential of the proposed principle.
Analysis of Univariate and Multivariate Filters Towards the Early Detection of Dementia
Authors: Khanna Kavita , Bansal Deepika , Chhikara Rita , Dua Rakesh Kumar , Malhotra Rajeev
Published: October 2020

Objective:

Dementia is a progressive neurodegenerative brain disease emerging as a global
health problem in adults aged 65 years or above, resulting in the death of nerve cells. The elimination
of redundant and irrelevant features from the datasets is however necessary for accurate detection
thus timely treatment of dementia.

Methods:

For this purpose, an ensemble approach of univariate and multivariate feature selection
methods has been proposed in this study. A comparison of four univariate feature selection techniques
(t-Test, Wilcoxon, Entropy and ROC) and six multivariate feature selection approaches (ReliefF,
Bhattacharyya, CFSSubsetEval, ClassifierAttributeEval, CorrelationAttributeEval, OneRAttributeEval)
has been performed. The ensemble of best univariate & multivariate filter algorithms is
proposed which helps in acquiring a subset of features that includes only relevant and non-redundant
features. The classification is performed using Naïve Bayes, k-NN, and Random Forest algorithms.

Results:

Experimental results show that t-Test and ReliefF feature selection is capable of selecting
10 relevant features that give the same accuracy when all features are considered. In addition to it,
the accuracy obtained using k-NN with an ensemble approach is 99.96%. The statistical significance
of the method has been established using Friedman’s statistical test.

Conclusion:

The new ranking criteria computed by the ensemble method efficiently eliminate the
insignificant features and reduces the computational cost of the algorithm. The ensemble method has
been compared to the other approaches for ensuring the superiority of the proposed model.

Discussion:

The percentage gain in accuracy for all three classifiers, Naïve Bayes, k-NN, and Random
Forest shows a remarkable difference noted down for the percentage gain in the accuracies after
applying feature selection using Naïve Bayes and k-NN. Using univariate filter selection methods,
the t-test is outshining among all the methods while selecting only 10 feature subsets.
Use of Social Media to Promote Cancer Screening and Early Diagnosis: Scoping Review
Authors: Plackett Ruth , Kaushal Aradhna , Kassianos Angelos P , Cross Aaron , Lewins Douglas , Sheringham Jessica , Waller Jo , von Wagner Christian
Published: October 2020

Background

Social media is commonly used in public health interventions to promote cancer screening and early diagnosis, as it can rapidly deliver targeted public health messages to large numbers of people. However, there is currently little understanding of the breadth of social media interventions and evaluations, whether they are effective, and how they might improve outcomes.

Objective

This scoping review aimed to map the evidence for social media interventions to improve cancer screening and early diagnosis, including their impact on behavior change and how they facilitate behavior change.

Methods

Five databases and the grey literature were searched to identify qualitative and quantitative evaluations of social media interventions targeting cancer screening and early diagnosis. Two reviewers independently reviewed each abstract. Data extraction was carried out by one author and verified by a second author. Data on engagement was extracted using an adapted version of the key performance indicators and metrics related to social media use in health promotion. Insights, exposure, reach, and differing levels of engagement, including behavior change, were measured. The behavior change technique taxonomy was used to identify how interventions facilitated behavior change.

Results

Of the 23 publications and reports included, the majority (16/23, 70%) evaluated national cancer awareness campaigns (eg, breast cancer awareness month). Most interventions delivered information via Twitter (13/23, 57%), targeted breast cancer (12/23, 52%), and measured exposure, reach, and low- to medium-level user engagement, such as number of likes (9/23, 39%). There were fewer articles about colorectal and lung cancer than about breast and prostate cancer campaigns. One study found that interventions had less reach and engagement from ethnic minority groups. A small number of articles (5/23, 22%) suggested that some types of social media interventions might improve high-level engagement, such as intended and actual uptake of screening. Behavior change techniques, such as providing social support and emphasizing the consequences of cancer, were used to engage users. Many national campaigns delivered fundraising messages rather than actionable health messages.

Conclusions

The limited evidence suggests that social media interventions may improve cancer screening and early diagnosis. Use of evaluation frameworks for social media interventions could help researchers plan more robust evaluations that measure behavior change. We need a greater understanding of who engages with these interventions to know whether social media can be used to reduce some health inequalities in cancer screening and early diagnosis.

International Registered Report Identifier (IRRID)

RR2-10.1136/bmjopen-2019-033592
Social Media Surveillance in Schools: Rethinking Public Health Interventions in the Digital Age
Authors: Burke Colin , Bloss Cinnamon
Published: October 2020

Growing public concern about student safety and well-being has led schools and school districts to contract private companies to implement new technologies that target and surveil students’ activity on social media websites. Although innovative solutions for addressing student safety and health are needed, it is unclear whether the implementation of social media surveillance in schools is an effective strategy. Currently, there is no evidence to support the claims made by social media surveillance companies, as well as the schools that hire them, that these technologies can address the myriad of public health issues facing today’s students. Instead, these digital surveillance systems may only serve to exacerbate the problems that youth—especially those from historically marginalized groups—already face.
Research Participants’ Perspectives on Using an Electronic Portal for Engagement and Data Collection: Focus Group Results From a Large Epidemiologic Cohort (Preprint)
Authors: Rees-Punia Erika , Patel Alpa V , Beckwitt Asher , Leach Corinne R , Gapstur Susan M , Smith Tenbroeck G
Published: October 2020

BACKGROUND

Epidemiologic cohort studies have begun to leverage electronic research participant portals to facilitate data collection, integrate wearable technologies, lower costs, and engage participants. However, little is known about the acceptability of portal use by research participants.

OBJECTIVE

The aim of this study is to conduct focus groups among a sample of Cancer Prevention Study-3 (CPS-3) participants to better understand their preferences and concerns about research portals.

METHODS

CPS-3 participants were stratified based on sex, race and ethnicity, age, and cancer status, and randomly invited to participate. Focus groups used an exploratory case design with semistructured guides to prompt discussion. Using a constant comparison technique, transcripts were assigned codes to identify themes.

RESULTS

Participants (31/59, 52% women; 52/59, 88% White/non-Latinx) were favorably disposed toward using a research participant portal to take surveys, communicate with the study staff, and upload data. Most participants indicated that a portal would be beneficial and convenient but expressed concerns over data safety. Participants stressed the importance of an easy-to-use and trustworthy portal that is compatible with mobile devices.

CONCLUSIONS

In addition to being beneficial to researchers, portals may also benefit participants as long as the portals are secure and simple. Participants believe that portals can provide convenient ways to report data and remain connected to the study.