bluuebunny/crossref_metadata_2025 huggingface dataset:
IoT based smart home automation using blockchain and deep learning models
Authors: Umer Muhammad , Sadiq Saima , Alhebshi Reemah M. , Sabir Maha Farouk , Alsubai Shtwai , Al Hejaili Abdullah , Khayyat Mashael M. , Eshmawi Ala’ Abdulmajid , Mohamed Abdullah
Published: May 2023

For the past few years, the concept of the smart house has gained popularity. The major challenges concerning a smart home include data security, privacy issues, authentication, secure identification, and automated decision-making of Internet of Things (IoT) devices. Currently, existing home automation systems address either of these challenges, however, home automation that also involves automated decision-making systems and systematic features apart from being reliable and safe is an absolute necessity. The current study proposes a deep learning-driven smart home system that integrates a Convolutional neural network (CNN) for automated decision-making such as classifying the device as “ON” and “OFF” based on its utilization at home. Additionally, to provide a decentralized, secure, and reliable mechanism to assure the authentication and identification of the IoT devices we integrated the emerging blockchain technology into this study. The proposed system is fundamentally comprised of a variety of sensors, a 5 V relay circuit, and Raspberry Pi which operates as a server and maintains the database of each device being used. Moreover, an android application is developed which communicates with the Raspberry Pi interface using the Apache server and HTTP web interface. The practicality of the proposed system for home automation is tested and evaluated in the lab and in real-time to ensure its efficacy. The current study also assures that the technology and hardware utilized in the proposed smart house system are inexpensive, widely available, and scalable. Furthermore, the need for a more comprehensive security and privacy model to be incorporated into the design phase of smart homes is highlighted by a discussion of the risks analysis’ implications including cyber threats, hardware security, and cyber attacks. The experimental results emphasize the significance of the proposed system and validate its usability in the real world.
Unusual Presentation of Bladder Tumour: Haematuria only after Administration of Anti-Platelet Drugs
Authors: Sailo Stephen Lalfak Zuala , Sailo Laltanpuii , Wann Veracious Cornerstone
Published: May 2023

Anti-thrombotic agents are used for the treatment and prevention of cardiovascular diseases. Bleeding is the most important side-effect of these agents. The common causes of haematuria after anti-thrombotic administration are benign prostatic hyperplasia, haemorrhagic cystitis, renal calculi, renal infarction, infection, and adult polycystic kidney disease. Haematuria only after anti-thrombotic administration can be the presentation of a bladder tumour. Here, 71 years old male patient, with a bladder tumour was reported, who presented with haematuria only after he took dual anti-platelet drugs (tablet Ecosprin and tablet Clopidogrel). He took these drugs after he underwent the insertion of cardiac stents. He never had any previous history of haematuria. After the complaint, ultrasonography was performed and it reported a normal urinary system. So, the anti-platelet drugs were suspected to be the cause of haematuria. Tablet Clopidogrel was stopped and patient was sent home on Tablet Ecosprin. However, one month later, he again developed haematuria. Repeat imaging studies (ultrasonography and computed tomography) detected a urinary bladder mass. Transurethral resection of the mass was performed and a biopsy reported high-grade, muscle-invasive transitional cell carcinoma. This case highlights the fact that all cases of haematuria, irrespective of anti-thrombotic agents’ administration, should be suspected to be due to urological malignancy and the patients should undergo complete urological investigations, including cystoscopy.
Structured Pulmonary Rehabilitation in a Patient with Post Tuberculosis Bronchiectasis and Endobronchial Carcinoid
Authors: Gulrandhe Purva , Tayade Vishakha , Vardhan Vishnu
Published: May 2023

Pulmonary Tuberculosis (TB) has the potential to harm the lungs over long-term owing to complication such as bronchiectasis. However, authors hereby reported a case of endobronchial carcinoid, for which there was a need for a tailored and planned physiotherapy intervention to address such a challenging condition. Loss of lung functions, a decline in exercise tolerance, and/or chronic respiratory symptoms due to TB-related interstitial and structural alterations have been identified as sequelae to pulmonary TB. A 52-year-old female presented with the chief complain of breathlessness of Grade 3 on the Modified Medical Research Council (MMRC) scale, chest pain over left-side radiating to the neck, and cough with expectoration. She had loss of appetite and highgrade fever and was diagnosed with endobronchial carcinoid with upper and middle lobe consolidation with cystic bronchiectasis. The patient received pharmacological treatment with bronchodialators, mucolytics, antibiotics, and non-opoid analgesics. The goals of physiotherapeutic management included secretion removal, relieving dyspnea, providing relaxation, enhancing exercise capacity through impacts on aerobic capacity and, management of disease, and Quality of Life (QoL) improvement. The structured rehabilitation program was found to be effective at the end of eight weeks. Clinical improvement was observed in the patient but complete rehabilitation was not able to achieve due to the patient’s socioeconomic condition.
Radiological Overview of Tubercular Arthritis of Wrist Joint: A Case Report
Authors: Ghosh Susmita Rani , Dasar Ramachandra , Debnath Soumyabrata , Chakma Ashu , Asim DE
Published: May 2023

Musculoskeletal Tuberculosis (TB) worldwide with wrist involvement is very rare. Maximum cases of tuberculous arthritis arise in patients born in and migrated from endemic regions, particularly in patients who are co-infected with Human Immunodeficiency Virus (HIV). Authors present a rare case of tuberculous arthritis of the wrist joint in a 64-year-old male having pain, swelling, and decreased range of motion in the left wrist for six months. X-ray and Computed Tomography (CT) showed erosion of carpal bones, reduced joint space, and soft tissue oedema and abscess. On Ultrasonography (USG) joint effusion and soft tissue oedema, were seen around the wrist joint, and on Magnetic Resonance Imaging (MRI) along with this marrow oedema were also noted. Aspirated fluid culture from abscess suggested Mycobacterium positive culture and Ziehl–Neelsen (Z-N) staining showed acid-fast bacilli. Antitubercular therapy was the mainstay of treatment. A high level of suspicion should be kept for TB in every infection of the wrist joint.
Kinetics Approach on the Evolution of the Nutritive Properties, Antinutritonal Factors and Free Radical Scavenging Capacity of DPPH during Germination of Two Local Legume Varieties (Phaseolus vulgaris and Vigna unguiculata)
Authors: Cissé Mariame , Doué Ginette G. , Yao Wilfried K. , Zoué Thierry L.
Published: May 2023

Aims: To improve the processes of pre-treatment of legumes for their nutritional valorization.

Study Design:  Original research.

Place and Duration of Study: This study took place at the Laboratory of Biotechnology, Agriculture and Valorization of Biological Resources, Félix Houphouët-Boigny University between February and July 2022.

Methodology: Red beans and cowpeas purchased on the local market of Adjamé were subjected, after unitary operation of sorting and washing, to a two-factor design of experiment:  seed/water ratio and the soaking time, in order to identify the ideal ratio and soaking time to well reduce phytates. Seeds resulting from this pre-treatment were germinated for 72 h and some key nutrient and functional parameters were evaluated.

Results: The ratio 8/9 and soaking time of 18 hours allowed a maximum reduction of 62 and 66.6% of phytate and 72.83 and 67.48% of tanins in cowpea and red beans, respectively. Protein content of these 72 hours germinated pre-treated seeds decreased very slightly and finally remained at high level of 22.02 and 23.13 g/100 g for cowpea and red bean, while reducing sugar levels increased significantly throughout germination to a maximum of 8.19 and 8.13 mg/100 g. Regarding functional and antioxidant properties, a maximum increase in total polyphenols (49.08  and 68.314 mg/100 g) and total flavonoids (13.75 and 39.67 mg/100 g) was observed after 48 h of germination for cowpea and red beans, respectively. Furthermore, this improvement in phenolic content led to a significant improvement in the free radical scavenging capacity of DPPH of 24.50 and 46.38 %. It should also be noted that the germinated red bean showed better nutritional value than the germinated cowpea. Conclusion: This approach of pre-processing germinated legumes at seed-to-water ratio of 8/9 soaked for 18 hours, providing functional foods with guaranteed nutritional value, appears to be a way to improve local diets.
O MODELO DE CINCO FATORES DE FAMA E FRENCH E O FATOR MOMENTO: UMA APLICAÇÃO AO MERCADO BRASILEIRO
Authors: Bortoluzzo Adriana Bruscato , Porto Gabriel Iseppe , Bortoluzzo Maurício Mesquita
Published: May 2023

Nos últimos 10 anos, uma carteira formada pela estratégia de momento teve uma rentabilidade superior a 528% enquanto o retorno de mercado foi de -16,32% (NEFIN, 2020). Mesmo assim, um dos modelos mais utilizados atualmente na literatura para explicar o retorno de carteiras, o modelo de cinco fatores de Fama e French (2015), não inclui o fator momento. Ao avaliar empiricamente o modelo de cinco fatores no mercado brasileiro entre 1997 e 2016, encontramos evidências de retorno não explicado pelo modelo e investigamos a viabilidade da inclusão do fator momento, conforme sugerido por Asness (2016). Embora os resultados obtidos com a adição do fator momento não tenham reduzido o número de interceptos com significância estatística quando comparado ao modelo de cinco fatores, houve um aumento no R2 ajustado para 16 das 22 carteiras analisadas.
Autorregulação da Aprendizagem no Ensino Remoto Estudo com Discentes de Ciências Contábeis Durante a Pandemia da Covid-19
Authors: Ruanderson Ferreira da Silva Levy , Meireles de Souza Jocykleber , Paulino de Oliveira Sabrina , De Melo Ramalho Keliane , Araújo Amaral Duarte Camilla
Published: May 2023

Esta pesquisa tem por objetivo investigar as estratégias de aprendizagem autorregulada utilizadas por discentes de Ciências Contábeis no ensino remoto durante a pandemia da Covid-19. Para tanto, foi adoto um survey, aplicando-se um questionário estruturado dividido em três blocos, o primeiro é composto por sete questões acerca do perfil socioeconômico e acadêmico dos participantes, já o segundo bloco, refere-se as dez estratégias de autorregulação do modelo proposto por Zimmerman e Pons (1986), e por fim, quatro perguntas analisando as vantagens e desvantagens do ensino remoto. Como técnica de análise, adotou-se a estatística descritiva para o bloco um e dois do questionário, já o bloco três, foi realizado uma codificação aberta no software ATLAS.ti®. Em síntese, os resultados evidenciam que em relação aos fatores determinantes da aprendizagem durante o ensino remoto, os mais indicados pelos discentes são: a) os esforços próprios para compreender; b) os professores e; c) trabalho em grupo.
Governança Pública e Eficiência Municipal: Um Estudo a Partir das Decisões do Tribunal de Contas dos Municípios da Bahia no período 2009-2015
Authors: Silva Lindomar , Ferreira Monica , Castro Miguel , Almeida Denise , Gonzalez José Ernesto
Published: May 2023

O artigo avalia a relação entre governança pública e eficiência municipal, no período 2009- 2015. Coletaram-se dados nos sites do Instituto Nacional de Estudos e Pesquisas Educacionais Anísio Teixeira (Inep), Instituto Brasileiro de Geografia e Estatísticas (Ibge), Tribunal Superior Eleitoral (Tse) e Tribunal de Contas dos Municípios do Estado da Bahia (Tcm-BA). Realizou-se a análise quantitativa, utilizando-se a regressão logística em painel, tendo como variável explicada da dimensão da eficiência pública, a decisão nos pareceres prévios do TCM-BA. Os resultados indicam que as variáveis “índice de renovação na câmara de vereadores”, “parecer do conselho de educação”, “parecer do conselho de saúde” e “Ideb (Prova Brasil)” influenciam a eficiência pública municipal, e as variáveis “percentual de vereadores da oposição”, “escolaridade dos vereadores”, “existência de conselho municipal de educação”, “tipo de conselho de educação”, “existência de conselho municipal de saúde”, “quantidade de denúncias”, “eleitores com nível superior completo” e “percentual de votos nominais”, não influenciam a eficiência municipal. Os resultados enriquecem as discussões sobre o papel dos atores da governança pública, identificando a relevância de algumas variáveis na melhora da eficiência municipal, especialmente o papel dos conselhos municipais e da sociedade civil.
Chronic Obstructive Pulmonary Disease Exacerbations and Pneumonia Hospitalizations Among New Users of Combination Maintenance Inhalers
Authors: Feldman William B. , Avorn Jerry , Kesselheim Aaron S. , Gagne Joshua J.
Published: May 2023

Importance

Clinical guidelines on chronic obstructive pulmonary disease (COPD) recommend inhalers containing long-acting muscarinic antagonists (LAMAs) and long-acting β-agonists (LABAs) over inhalers containing inhaled corticosteroids (ICSs) and LABAs. However, data from randomized clinical trials comparing these combination inhalers (LAMA-LABAs vs ICS-LABAs) have been conflicting and raised concerns of generalizability.

Objective

To assess whether LAMA-LABA therapy is associated with reduced COPD exacerbations and pneumonia hospitalizations compared with ICS-LABA therapy in routine clinical practice.

Design, Setting, and Participants

This was a 1:1 propensity score–matched cohort study using Optum’s Clinformatics Data Mart, a large commercial insurance–claims database. Patients must have had a diagnosis of COPD and filled a new prescription for a combination LAMA-LABA or ICS-LABA inhaler between January 1, 2014, and December 31, 2019. Patients younger than 40 years were excluded, as were those with a prior diagnosis of asthma. The current analysis was performed from February 2021 to March 2023.

Exposures

Combination LAMA-LABA inhalers (aclidinium-formoterol, glycopyrronium-formoterol, glycopyrronium-indacaterol, tiotropium-olodaterol, or umeclidinium-vilanterol) and combination ICS-LABA inhalers (budesonide-formoterol, fluticasone-salmeterol, fluticasone-vilanterol, or mometasone-formoterol).

Main Outcome

The primary effectiveness outcome was first moderate or severe COPD exacerbation, and the primary safety outcome was first pneumonia hospitalization. Propensity score matching was used to control for confounding between the 2 groups. Logistic regression analysis was used to estimate propensity scores. Hazard ratios (HRs) and 95% CIs were estimated using Cox proportional hazards models stratified on matched pairs.

Results

Among 137 833 patients (mean [SD] age, 70.2 [9.9] years; 69 530 [50.4%] female) (107 004 new ICS-LABA users and 30 829 new LAMA-LABA users), 30 216 matched pairs were identified for the primary analysis. Compared with ICS-LABA use, LAMA-LABA use was associated with an 8% reduction in the rate of first moderate or severe COPD exacerbation (HR, 0.92; 95% CI, 0.89-0.96) and a 20% reduction in the rate of first pneumonia hospitalization (HR, 0.80; 95% CI, 0.75-0.86). These findings were robust across a range of prespecified subgroup and sensitivity analyses.

Conclusion

In this cohort study, LAMA-LABA therapy was associated with improved clinical outcomes compared with ICS-LABA therapy, suggesting that LAMA-LABA therapy should be preferred for patients with COPD.
Record High Power Factor and Low Thermal Conductivity in Amorphous/PbTe/Amorphous Multiple Quantum Wells
Authors: Ning Xingkun , Dong Yaolong , Jian Weixiong , Wang Jinrong , Guo Wenbo , Wang Shufang
Published: May 2023

Quantum well (QW) superlattice is one of the proposals to improve the thermoelectric properties and provide a rich platform for the next generation of thermoelectric device. Previous QW have two main challenges that need to be addressed: i) decrease the electron tunneling across the layers in the semiconductor‐based multiple QWs (MQW), and ii) decrease the thermal conductivity in the oxide‐based MQW. Herein, the study demonstrates amorphous based PbTe/amorphous‐STO MQWs with ultrahigh power factor of 40.9 µW cm−1 K−2and record low thermal conductivity of ≈0.49 W m−1 K−1at room temperature. The high performance of PbTe/amorphous‐STO MQWs is attributed to strong quantum confine effect and its intrinsic low thermal conductivity of amorphous superlattice structure. The results open up a new avenue toward modulating thermoelectric properties beyond traditional MQWs of thermoelectric materials.
Construction of 2‐Azabicyclo[2.2.1]heptenes via Selenium‐Catalyzed Intramolecular Oxidative Amination of Cyclopentenes
Authors: Ma Jiao , Dong Liuli , Yao Jiarong , Lin Aijun , Yao Hequan
Published: May 2023

A selenium‐catalyzed intramolecular oxidative amination of cyclopentenes has been described. A variety of 2‐azabicyclo[2.2.1]heptenes were obtained with 58%–96% yields. This protocol was featured with mild reaction conditions and broad substrate scope. The subsequent modification of the bicyclic backbone and amino group further demonstrated the application value of this aza‐bridged ring.
Synthesis of 3‐Aminopiperidines via I(III)‐Mediated Olefin Diamination with (Hetero)aryl Nucleophiles
Authors: Vazquez‐Lopez Andres , Allen James E. , Wengryniuk Sarah E.
Published: May 2023

3‐Aminopiperidines are a valuable motif present in small molecule pharmaceuticals and bioactive natural products. Synthesis of these moieties via olefin diamination would be an attractive approach, however significant challenges remain with regards to both regioselectivity and exogenous nucleophile scope. Herein, we report a metal‐free olefin diamination via a “heterocyclic group transfer“ (HGT) reaction of I(III) N‐HVI reagents, giving rise to 3‐aminopiperidines with high selectivity. The HGT strategy leverages heteroarenes as oxidatively masked amine nucleophiles, giving rise to (hetero)arylonium salt products which are isolated via simple trituration and provide a versatile handle for downstream diversification. This represents only the second 6‐endo selective I(III)‐mediated diamination reaction and mechanistic studies indicate ring opening of an intermediate aziridinium ion is responsible for the 6‐endo selectivity.
Achieving Diamond‐Like Wear in Ta‐Rich Metallic Glasses
Authors: Li Fucheng , Li Mingxing , Hu Liwei , Cao Jiashu , Wang Chao , Sun Yitao , Wang Weihua , Liu Yanhui
Published: May 2023

Most metals and alloys suffer from high friction and wear due to their low hardness and lack of self‐lubrication. Although plenty of strategies have been proposed, it is still a long‐standing challenge to achieve diamond‐like wear in metals. Metallic glasses (MGs) are supposed to possess low coefficient of friction (COF) because of their high hardness and fast surface mobility. However, their wear rate is larger than that of diamond‐like materials. Here, this work reports the discovery of Ta‐rich MGs that exhibit diamond‐like wear. This work develops an indentation approach for high‐throughput characterization of crack resistance. By employing deep indentation loading, this work is able to efficiently identify the alloys that exhibit better plasticity and crack resistance according to the differences of indent morphology. With high temperature stability, high hardness, improved plasticity, and crack resistance, the discovered Ta‐based MGs exhibit diamond‐like tribological properties, featured by COF as low as ≈0.05 for diamond ball test and ≈0.15 for steel ball test, and specific wear rate of only ≈10−7 mm3 N−1m−1. The discovery approach and the discovered MGs exemplifie the promise to substantially reduce friction and wear of metals and may unleash the potential of MGs in tribological applications.
Single‐Cell RNA Sequencing and Spatial Transcriptomics Reveal Pathogenesis of Meningeal Lymphatic Dysfunction after Experimental Subarachnoid Hemorrhage
Authors: Wang Xiaoyu , Zhang Anke , Yu Qian , Wang Zelin , Wang Junjie , Xu Penglei , Liu Yibo , Lu Jianan , Zheng Jingwei , Li Huaming , Qi Yangjian , Zhang Jiahao , Fang Yuanjian , Xu Shenbin , Zhou Jingyi , Wang Kaikai , Chen Sheng , Zhang Jianmin
Published: May 2023

Subarachnoid hemorrhage (SAH) is a devastating subtype of stroke with high mortality and disability rate. Meningeal lymphatic vessels (mLVs) are a newly discovered intracranial fluid transport system and are proven to drain extravasated erythrocytes from cerebrospinal fluid into deep cervical lymph nodes after SAH. However, many studies have reported that the structure and function of mLVs are injured in several central nervous system diseases. Whether SAH can cause mLVs injury and the underlying mechanism remain unclear. Herein, single‐cell RNA sequencing and spatial transcriptomics are applied, along with in vivo/vitro experiments, to investigate the alteration of the cellular, molecular, and spatial pattern of mLVs after SAH. First, it is demonstrated that SAH induces mLVs impairment. Then, through bioinformatic analysis of sequencing data, it is discovered that thrombospondin 1 (THBS1) and S100A6 are strongly associated with SAH outcome. Furthermore, the THBS1‐CD47 ligand‐receptor pair is found to function as a key role in meningeal lymphatic endothelial cell apoptosis via regulating STAT3/Bcl‐2 signaling. The results illustrate a landscape of injured mLVs after SAH for the first time and provide a potential therapeutic strategy for SAH based on mLVs protection by disrupting THBS1 and CD47 interaction.
Hofmeister Effects Shine in Nanoscience
Authors: Wei Weichen
Published: May 2023

Hofmeister effects play a crucial role in nanoscience by affecting the physicochemical and biochemical processes. Thus far, numerous wonderful applications from various aspects of nanoscience have been developed based on the mechanism of Hofmeister effects, such as hydrogel/aerogel engineering, battery design, nanosynthesis, nanomotors, ion sensors, supramolecular chemistry, colloid and interface science, nanomedicine, and transport behaviors, etc. In this review, for the first time, the progress of applying Hofmeister effects is systematically introduced and summarized in nanoscience. It is aimed to provide a comprehensive guideline for future researchers to design more useful Hofmeister effects‐based nanosystems.
Impact of type 2 diabetes on mortality, cause of death, and treatment in chronic lymphocytic leukemia
Authors: Rotbain Emelie Curovic , Allmer Cristine , Rostgaard Klaus , Andersen Michael Asger , Vainer Noomi , da Cunha‐Bang Caspar , Parikh Sameer A. , Rabe Kari G. , Hjalgrim Henrik , Frederiksen Henrik , Slager Susan L. , Niemann Carsten Utoft
Published: May 2023

Age‐related comorbid conditions are exceedingly common in patients with chronic lymphocytic leukemia (CLL). As the prevalence of type 2 diabetes (T2D) is predicted to double during the next two decades, a better understanding of the interplay between CLL and T2D is of increasing importance. In this study, analyses were performed in parallel in two separate cohorts, based on Danish national registers and the Mayo Clinic CLL Resource. The primary outcomes were overall survival (OS) from time of CLL diagnosis, OS from time of treatment, and time to first treatment (TTFT), studied using Cox proportional hazard regression analysis and Fine‐Gray regression analysis. In the Danish CLL cohort, the prevalence of T2D was 11%, in the Mayo CLL cohort, it was 12%. Patients with CLL and T2D had shorter OS both from time of diagnosis and from first‐line treatment for were less likely to receive treatment for CLL compared with patients with CLL and without T2D. The increased mortality was largely driven by an increased risk of death due to infections, especially in the Danish cohort. The findings of this study emphasize a substantial subgroup of CLL patients with co‐occurring T2D with an inferior prognosis and a possible unmet treatment need requiring additional interventions and further research.
Integrated Soft Porosity and Electrical Properties of Conductive‐on‐Insulating Metal‐Organic Framework Nanocrystals
Authors: Yao Ming‐Shui , Otake Ken‐ichi , Zheng Jiajia , Tsujimoto Masahiko , Gu Yi‐Fan , Zheng Lu , Wang Ping , Mohana Shivanna , Bonneau Mickaele , Koganezawa Tomoyuki , Honma Tetsuo , Ashitani Hirotaka , Kawaguchi Shogo , Kubota Yoshiki , Kitagawa Susumu
Published: May 2023

A one‐stone, two‐bird method to integrate the soft porosity and electrical properties of distinct metal–organic frameworks (MOFs) into a single material involves the design of conductive‐on‐insulating MOF (cMOF‐on‐iMOF) heterostructures that allow for direct electrical control. Herein, we report the synthesis of cMOF‐on‐iMOF heterostructures using a seeded layer‐by‐layer method, in which the sorptive iMOF core is combined with chemiresistive cMOF shells. The resulting cMOF‐on‐iMOF heterostructures exhibit enhanced selective sorption of CO2 compared to the pristine iMOF (298 K, 1 bar, S
from 15.4 of ZIF‐7 to 43.2–152.8). This enhancement is attributed to the porous interface formed by the hybridization of both frameworks at the molecular level. Furthermore, owing to the flexible structure of the iMOF core, the cMOF‐on‐iMOF heterostructures with semiconductive soft porous interfaces demonstrated high flexibility in sensing and electrical “shape memory” toward acetone and CO2. This behavior was observed through the guest‐induced structural changes of the iMOF core, as revealed by the operando synchrotron grazing incidence wide‐angle X‐ray scattering measurements.
Azoheteroarene and Diazocine Molecular Photoswitches: Self‐Assembly, Responsive Materials and Photopharmacology
Authors: Mukherjee Anurag , Seyfried Maximilian D. , Ravoo Bart Jan
Published: May 2023

Aromatic units tethered with an azo (−N=N−) functionality comprise a unique class of compounds, known as molecular photoswitches, exhibiting a reversible transformation between their E‐ and Z‐isomers in response to photo‐irradiation. Photoswitches have been explored extensively in the recent past to prepare dynamic self‐assembled materials, optoelectronic devices, responsive biomaterials, and more. Most of such materials involve azobenzenes as the molecular photoswitch and to date, SciFinder lists more than 7000 articles and 1000 patents. Subsequently, a great deal of effort has been invested to improve the photo‐isomerization efficiency and related mesoscopic properties of azobenzenes. Recently, azoheteroarenes and cyclic azobenzenes, such as arylazopyrazoles, arylazoisoxazoles, arylazopyridines, and diazocines, have emerged as second generation molecular photoswitches beyond conventional azobenzenes. These photoswitches offer distinct photoswitching behavior and responsive properties which make them highly promising candidates for multifaceted applications ranging from photoresponsive materials to photopharmacophores. In this minireview, we introduce the structural refinement and photoresponsive properties of azoheteroarenes and diazocines and summarize the state‐of‐the‐art on utilizing these photoswitches as responsive building blocks in supramolecular assembly, material science and photopharmacology, highlighting their versatile photochemical behavior, enhanced functionality, and latest applications.
First report on the utility of pupal case for early determination of CRISPR/Cas9 ribonucleoprotein mediated genomic edits in the oriental fruit fly, Bactrocera dorsalis (Hendel) (Tephritidae: Diptera)
Authors: Ashok Karuppannasamy , Bhargava Chikmagalur Nagaraja , Asokan Ramasamy , Pradeep Chalapathi , Kennedy John Samuel , Rai Anil , Manamohan Maligeppagol
Published: May 2023

The Oriental fruit fly, Bactrocera dorsalis (Hendel), is a highly invasive pest of quarantine importance affecting the global fruit trade. In managing B. dorsalis, methods like cultural, biological, chemical, sterile insect technique (SIT), and semiochemical‐mediated attract‐and‐kill are in use with varying success. The SIT approach is the method of choice for a chemical‐free, long‐term suppression of B. dorsalis, followed in many countries across the globe. The nonspecific mutations caused by irradiation affect the overall fitness of flies, thus requiring a more precise method for a heritable, fitness‐not‐compromising approach. In this regard, CRISPR/Cas9‐mediated genome editing enables the creation of mutations at the precise genomic location/s through RNA‐guided dsDNA cleavage. Of late, DNA‐free editing employing ribonucleoprotein complex (RNP) is preferred to validate the target genes at G0 stage embryos in insects. It requires characterizing genomic edits from adults after completing their life cycle, which may entail a few days to months, depending on longevity. Additionally, edit characterization is required from each individual, as edits are unique. Therefore, all RNP‐microinjected individuals must be maintained until the end of their life cycle, irrespective of editing. To overcome this impediment, we predetermine the genomic edits from the shed tissues, such as pupal cases, to maintain only edited individuals. In this study, we have shown the utility of pupal cases from five males and females of B. dorsalis to predetermine the genomic edits, which corroborated the edits from the respective adults.
Current progress in the targeted therapy of breast cancer: Structure–activity correlation and docking studies (2015–2021)
Authors: Pandey Shivanshu , Mondal Sitanshu , Kajal Kumari , Kurmi Balak Das , Verma Sant Kumar , Patel Preeti
Published: May 2023

Despite cancer research and therapy, breast cancer remains a complicated health crisis in women and represents a top biomedical research priority. Nowadays, breast cancer is an extremely heterogeneous disease and is known as the leading cause of death among women worldwide. The incidence and mortality rates of breast cancer have been increasing gradually for the past decades. Nowadays, common treatments for breast cancer are chemotherapy, endocrine therapy, immunotherapy, radiotherapy, and surgery. The most common targets in breast cancer treatment are human epidermal growth factor receptor 2 (HER2) and estrogen receptors. The literature suggests that several targets/pathways are also involved in the development of breast cancer, that is, poly(ADP‐ribose) polymerase (PARP), bromodomain‐containing protein 4 (BRD4), cyclin‐dependent kinase 4/6 (CDK4/6), epidermal growth factor receptor (EGFR), vascular endothelial growth factor receptor (VEGFR), polo‐like kinase 1 (PLK1), phosphoinositide 3‐kinases/protein kinase B/mammalian target of rapamycin (PI3K/AKT/mTOR), histone deacetylase (HDAC), nuclear factor kappa B (NF‐κB), PD‐L1, and aromatase inhibitors. Meanwhile, the study of breast cancer is a hot topic in the current scenario of basic/clinical research. This review article provides information on different targets associated with breast cancer and summarizes the progress of current research on synthesized inhibitors as anti‐breast cancer agents from 2015 to 2021. The review aims to provide structure–activity relationship and docking studies for designing novel compounds for breast cancer therapy.
Tunable Luminescence of Nonaromatic Borate Esters
Authors: Yang Tianjia , Hou Wubeiwen , Yuan Wang Zhang
Published: May 2023

While the majority of nonconventional luminophores consist of electron‐rich heteroatoms, an emerging category with electron‐deficient atoms (e. g. boron) have gained much attention. In this work, we focused on one of the most common boron‐containing substances, namely bis(pinacolato)diboron (BE1) and its analogue bis(2,4‐dimethylpentane‐2,4‐glycolato)diboron (BE2), whose empty p‐orbitals of boron atoms and p‐orbitals with lone pairs of oxygens form π frameworks. Both compounds are nonemissive in dilute solutions but depict remarkable photoluminescence (PL) at aggregate states, featuring aggregation‐induced emission characteristics. Additionally, their PL can be easily tuned by various external factors, such as excitation wavelength, compression, and oxygen. These photophysical properties could well be explained by the clustering‐triggered emission (CTE) mechanism.
Coordination‐Induced Migration of Aryl Groups in the Reactions of a Dialkylsilanone with a Series of Triarylboranes
Authors: Ishida Shintaro , Sakamoto Kengo , Kobayashi Ryo , Iwamoto Takeaki
Published: May 2023

Although carbonyl compounds are activated by the coordination of a Lewis acid to the carbonyl oxygen atom, a similar activation process of R2Si=O species remains unclear. We report herein the reactions of a silanone (1, Scheme 1) with a series of triarylboranes to afford the corresponding boroxysilanes. Experimental results and computational studies indicate that the electrophilicity of the unsaturated silicon atom is enhanced by the complexation of 1 with triarylboranes, and the subsequent aryl migration from the boron atom to the electrophilic silicon atom proceeds.
Blossoming of Polyenamine Catalysis in Asymmetric Synthesis: Scope and Future Applications
Authors: Borah Biplob , Sivaprakash Murugesan , Sharma Samrita , Prasad Madavi S. , Raju Chowhan L.
Published: May 2023

After the emergence of organocatalysis, the field of asymmetric synthesis has reached an exceptional level in this century. Asymmetric aminocatalysis, among other organocatalytic strategies, proceeded through LUMO‐lowering iminium ion and HOMO‐raising enamine ion activation has appeared as a powerful synthetic approach for realizing potential chiral building blocks from unmodified carbonyl compounds. Consequently, the concept of HOMO‐raising activation strategy for a plethora of asymmetric transformations based on enamine, dienamine, and most recently trienamine, tetraenamine, and pentaenamine catalysis has been devised. In this mini‐review article, we disclosed the recent progress accomplished in asymmetric aminocatalysis through polyenamine activation strategies for the functionalization of carbonyl compounds, and we covered the reports from 2014 to till date.
Preoperative denosumab treatment in patients with giant cell bone tumors in limbs: A retrospective study using propensity score matching
Authors: Huang Yongfu , Xu Mingxian , Wang Bo , Zhao Zhiqiang , Lin Tiao , Huang Gang , Yin Junqiang , Xie Xianbiao , Shen Jingnan , Zou Changye
Published: May 2023

Background and Objectives

Denosumab is recommended for advanced giant cell tumor of bone (GCTB) that is unresectable or resectable with unacceptable morbidity. But the effect of preoperative denosumab treatment on the local control GCTB remains controversial.

Methods

We conducted a study of 49 patients with GCTB in the limbs treated with denosumab before surgery and 125 patients without in our hospital from 2010 to 2017. Propensity‐score matching (PSM) at a 1:1 ratio between the denosumab and control groups was performed to minimize possible selection bias, and compared the recurrence rate, limb function, and surgical degradation between the two groups.

Results

The 3‐year recurrence rates in the denosumab group and the control group were 20.4% and 22.9% after PSM, respectively (p = 0.702). In the denosumab group, 75.5% (n = 37/49) of patients experienced surgical downgrading. Limb joint preservation rates were 92.1% (35) for 38 patients treated with denosumab and 60.2% (71) for 118 control subjects. (p ≺ 0.001). Postoperative MSTS were higher in patients in the denosumab group than in the control group (24.1 vs. 22.6, p = 0.034).

Conclusions

Preoperative denosumab treatment did not result in an increased risk of local recurrence of GCTB. Patients with advanced GCTB may benefit from preoperative denosumab treatment for surgical downgrading and the preservation of the joint.
TRIM55 inhibits colorectal cancer development via enhancing protein degradation of c‐Myc
Authors: Lin Min , Fang Zejun , Lin Xuedan , Zhou Weihua , Wang Yizhang , Han Shanshan , Ye Ming , Zhu Fengjiao
Published: May 2023

Background

Colorectal cancer (CRC) is one of the most common and lethal malignancies which including colon and rectum cancer. Tripartite motif containing 55 (TRIM55) is an E3 ubiquitin ligase belonging to the TRIM family. Although the aberrant TRIM55 expression has been implicated in several tumors, its functional role, and molecular mechanisms in CRC remain unknown.

Methods

Immunohistochemical studies, qRT‐PCR, and Western blot were performed to analyze the expression of TRIM55 in CRC patients and cell lines. TRIM55 expression and its relevance to clinical traits and prognosis were further explored in the TCGA database, and in our 87 clinical samples. Subsequently, we performed a series of functional assays to explore the effect of TRIM55 on CRC progression. Finally, the molecular mechanism of TRIM55 was investigated by immunoprecipitation and ubiquitination analyses.

Results

Here, we demonstrated that TRIM55 was markedly downregulated in CRC cell lines and tumors from CRC patients. Moreover, overexpression of TRIM55 could suppress CRC cell growth in vitro and inhibit CRC xenograft tumor development in vivo. Additionally, TRIM55 overexpression dampened CRC cell migration and invasion. Further bioinformatics analysis indicated that TRIM55 suppressed cyclin D1 and c‐Myc expression. Mechanistically, co‐immunoprecipitation assay revealed that TRIM55 directly interacted with c‐Myc and down‐regulated its protein expression level via protein ubiquitination. Intriguingly, c‐Myc overexpression partially antagonized the function of TRIM55 overexpression.

Conclusions

Taken together, our findings suggest that TRIM55 inhibits CRC tumor development via, at least in part, enhancing protein degradation of c‐Myc. Targeting TRIM55 could provide a new therapeutic approach for CRC patients.
Reasons for truly negative cytology reports preceding the diagnoses of invasive cervical cancer—Results of a false‐negative cytology audit in Polish Cervical Cancer Screening Programme
Authors: Macios Anna , Komerska Katarzyna , Nowakowski Andrzej
Published: May 2023

Background

False‐negative (FN) results in cervical cancer (CC) screening pose significant risk for participants and should be audited. The aim of the study was to analyse the results of audit of FN slides collected in 2010–2013 in Polish Cervical Cancer Screening Program (CCSP) and to seek for risk factors of obtaining true‐negative result (TN; not containing abnormal cells as confirmed in audit) before CC diagnosis.

Methods

Screening database was merged with National Cancer Registry to identify negative slides preceding histologically confirmed CC diagnosis up to 42 months. Two blinding slides were randomly assigned per each FN. The whole set was reassessed independently by three pathologists with 30 years of experience in cytology evaluation. Final audit result was established in the case of ≥2 coherent reports. Agreement rates and kappa (κ) coefficients were calculated. Logistic analysis of risk factors for obtaining TN result was performed.

Results

Of 374 included FNs, 204 were considered abnormal (54.6%) and 91 were confirmed negative for intraepithelial neoplasia (24.3%). Agreement between experts was moderate for FNs (κ = 0.266) and fair for blinding slides (κ = 0.142) when grouping abnormal slides. Adenocarcinoma diagnosis elevated the risk of TN result (OR = 3.83); detection of macroscopic changes on the cervix and smoking lowered the risk (OR = 0.39, OR = 0.40 respectively).

Conclusions

Misinterpretation was the main reason for FN cytology in the CCSP which indicated the need of further personnel training to increase screening quality. Rather low agreement between auditors requires further insight. A standardised process of auditors' selection should be planned to increase audit quality.
PIK3R3 is upregulated in liver cancer and activates Akt signaling to control cancer growth by regulation of CDKN1C and SMC1A
Authors: Lin Weidong , Wang Kunpeng , Mo Jinggang , Wang Liezhi , Song Zhenshun , Jiang Hao , Wang Cong , Jin Chong
Published: May 2023

Background

Liver cancer is a highly malignant disease and the third leading cause of cancer death worldwide. Abnormal activation of PI3K/Akt signaling is common in cancer, but whether phosphoinositide‐3‐kinase regulatory subunit 3 (PIK3R3) plays a role in liver cancer is largely unexplored.

Methods

We determined the expression of PIK3R3 in liver cancer by using TCGA data and our clinical samples and knocked it down by siRNA or overexpressing it by the lentivirus vector system. We also investigated the function of PIK3R3 by colony formation, 5‐Ethynyl‐2‐Deoxyuridine, flow cytometry assay, and subcutaneous xenograft model. The downstream of PIK3R3 was explored by RNA sequence and rescue assays.

Results

We found that PIK3R3 was significantly upregulated in liver cancer and correlated with prognosis. PIK3R3 promoted liver cancer growth in vitro and in vivo by controlling cell proliferation and cell cycle. RNA sequence revealed that hundreds of genes were dysregulated upon PIK3R3 knockdown in liver cancer cells. CDKN1C, a cyclin‐dependent kinase inhibitor, was significantly upregulated by PIK3R3 knockdown, and CDKN1C siRNA rescued the impaired tumor cell growth. SMC1A was partially responsible for PIK3R3 regulated function, and SMC1A overexpression rescued the impaired tumor cell growth in liver cancer cells. Immunoprecipitation demonstrated there is indirect interaction between PIK3R3 and CNKN1C or SMC1A. Importantly, we verified that PIK3R3‐activated Akt signaling determined the expression of CDKN1C and SMC1A, two downstream of PIK3R3 in liver cancer cells.

Conclusion

PIK3R3 is upregulated in liver cancer and activates Akt signaling to control cancer growth by regulation of CDNK1C and SMC1A. Targeting PIK3R3 could be a promising treatment strategy for liver cancer that deserves further investigation.
Clinical characteristics and outcomes for children, adolescents and young adults with “CIC‐fused” or “BCOR‐rearranged” soft tissue sarcomas: A multi‐institutional European retrospective analysis
Authors: Sparber‐Sauer Monika , Corradini Nadège , Affinita Maria Carmen , Milano Giuseppe Maria , Pierron Gaelle , Carton Matthieu , Tirode Franck , Pissaloux Daniel , Alaggio Rita , Vokuhl Christian , Bisogno Gianni , Berlanga Pablo , Ferrari Andrea , Orbach Daniel
Published: May 2023

Background

In certain rare undifferentiated small round cell sarcomas new specific molecular CIC‐DUX4/other partner, BCOR‐CCNB3/other partner, YWHAE fusions, or BCOR‐ITD (internal tandem duplication) were identified. These new “CIC fused” (CIC‐fused/ATXN1::NUTM1) and “BCOR rearranged” (BCOR fused/ITD/ YWHAE) soft tissue sarcomas (STS) are not well described.

Methods

Multi‐institutional European retrospective analysis of young patients (0–24 years) with CIC‐fused and BCOR rearranged STS.

Results

Overall, out of the 60 patients selected, the fusion status was CIC‐fused (n = 29), ATXN1::NUTM1 (n = 2), BCOR::CCNB3 (n = 18), BCOR‐ITD (n = 7), and YWHAE (n = 3), MAML::BCOR STS (n = 1). The main primaries were abdomen‐pelvic (n = 23) and limbs (n = 18). Median age was 14 years (0.9–23.8) and 0.9 (0.1–19.1) for CIC‐fused and BCOR‐rearranged groups, respectively (n = 29; p < 0.001). IRS stages were I (n = 3), II (n = 7), III (n = 35), and IV (n = 15). Overall, 42 patients had large tumors (>5 cm) but only six had lymph node involvement. Patients received mainly chemotherapy (n = 57), local surgery (n = 50), and/or radiotherapy (n = 34). After a median follow‐up of 47.1 months (range, 3.4–230), 33 (52%) patients had an event and 23 patients died. Three‐year event‐free survivals were 44.0% (95% CI 28.7–67.5) and 41.2% (95% CI 25.4–67.0) for CIC and BCOR groups (p = 0.97), respectively. Three‐year overall survivals were 46.3% (95% CI 29.6–72.4) and 67.1% (95% CI 50.4–89.3; p = 0.24), respectively.

Conclusions

Pediatric patients often present with large tumors and metastatic disease, especially CIC sarcomas. Overall outcome is dismal. New treatment options are needed.
Associations of the 2018 World Cancer Research Fund/American Institute of Cancer Research (WCRF/AICR) cancer prevention recommendations with stages of colorectal carcinogenesis
Authors: Kværner Ane Sørlie , Andersen Astrid Riseth , Henriksen Hege Berg , Knudsen Markus Dines , Johansen Anne Marte Wetting , Hjartåker Anette , Bøhn Siv Kjølsrud , Paur Ingvild , Wiedswang Gro , Smeland Sigbjørn , Rounge Trine B. , Blomhoff Rune , Berstad Paula
Published: May 2023

Background

While adherence to cancer prevention recommendations is linked to lower risk of colorectal cancer (CRC), few have studied associations across the entire spectrum of colorectal carcinogenesis. Here, we studied the relationship of the standardized 2018 World Cancer Research Fund/American Institute for Cancer Research (WCRF/AICR) Score for cancer prevention recommendations with detection of colorectal lesions in a screening setting. As a secondary objective, we examined to what extent the recommendations were being followed in an external cohort of CRC patients.

Methods

Adherence to the seven‐point 2018 WCRF/AICR Score was measured in screening participants receiving a positive fecal immunochemical test and in CRC patients participating in an intervention study. Dietary intake, body fatness and physical activity were assessed using self‐administered questionnaires. Multinomial logistic regression was used to estimate odds ratios (ORs) and 95% confidence intervals (CIs) for screen‐detected lesions.

Results

Of 1486 screening participants, 548 were free from adenomas, 524 had non‐advanced adenomas, 349 had advanced lesions and 65 had CRC. Adherence to the 2018 WCRF/AICR Score was inversely associated with advanced lesions; OR 0.82 (95% CI 0.71, 0.94) per score point, but not with CRC. Of the seven individual components included in the score, alcohol, and BMI seemed to be the most influential. Of the 430 CRC patients included in the external cohort, the greatest potential for lifestyle improvement was seen for the recommendations concerning alcohol and red and processed meat, where 10% and 2% fully adhered, respectively.

Conclusions

Adherence to the 2018 WCRF/AICR Score was associated with lower probability of screen‐detected advanced precancerous lesions, but not CRC. Although some components of the score seemed to be more influential than others (i.e., alcohol and BMI), taking a holistic approach to cancer prevention is likely the best way to prevent the occurrence of precancerous colorectal lesions.
An Efficient Approach for the Synthesis and Antitumor Evaluation of Novel Azo‐ and Anil‐Linked with 3‐Aminopyrazolo[3,4‐b]pyridine
Authors: El‐Bana Ghada G. , Hamama Wafaa S. , Zoorob Hanafi H. , Ibrahim Mona E.
Published: May 2023

In this project, an effective procedure for constructing a new combination of pyrazolo[3,4‐b]pyridine was depicted through the coupling of diazonium salt 2 of heterocyclic amine 1 with active methylene, enamine, and amidine moieties such as 3, 5, 7, and 9 at 0–5 °C in pyridine to afford hydrazinylhydrazonoyl derivatives 4, and diazenylheterocyclic derivatives 6, 8, and 10, respectively. Also, aminopyrazolo[3,4‐b]pyridine 1 condensed with different aryl or heteroaryl aldehydes in EtOH/AcOH gave the corresponding aldimine 14, 15, 16. Compound 15 was cyclized via refluxing in DMF for 6 h to afford 18, while the transformation of compound 16 with an alkyl halide afforded 19a, b. The synthesized compounds, explicated by spectral data and elemental analysis, were examined for their antitumor activities. The in vitro cytotoxic activity of new pyrazolo[3,4‐b]pyridines against the A2780CP, MCF‐7, and HepG‐2 cell lines was evaluated using the reference doxorubicin. Compounds 15 and 19a exhibited high reactivity against the A2780CP cell lines, with IC50 values of 35 and 17.9 μM, respectively. Also, compound 28 had the cytotoxic potential for A2780CP and MCF‐7 cell lines, with IC50 values of 14.5, and 27.8 μM, respectively.