bluuebunny/crossref_metadata_2025 huggingface dataset:
Pushing the Limit of Photo-Controlled Polymerization: Hyperchromic and Bathochromic Effects
Authors: Wang Zhilei , Zhang Zipeng , Wu Chenyu , Wang Zikuan , Liu Wenjian
Published: May 2024

The photocatalyst (PC) zinc tetraphenylporphyrin (ZnTPP) is highly efficient for photoinduced electron/energy transfer reversible addition-fragmentation chain transfer (PET-RAFT) polymerization. However, ZnTPP suffers from poor absorbance of orange light by the so-called Q-band of the absorption spectrum (maximum absorption wavelength λmax = 600 nm, at which molar extinction coefficient εmax = 1.0×104 L/(mol·cm)), hindering photo-curing applications that entail long light penetration paths. Over the past decade, there has not been any competing candidate in terms of efficiency, despite a myriad of efforts in PC design. By theoretical evaluation, here we rationally introduce a peripheral benzo moiety on each of the pyrrole rings of ZnTPP, giving zinc tetraphenyl tetrabenzoporphyrin (ZnTPTBP). This modification not only enlarges the conjugation length of the system, but also alters the a1u occupied π molecular orbital energy level and breaks the accidental degeneracy between the a1u and a2u orbitals, which is responsible for the low absorption intensity of the Q-band. As a consequence, not only is there a pronounced hyperchromic and bathochromic effect (λmax = 655 nm and εmax = 5.2×104 L/(mol·cm)) of the Q-band, but the hyperchromic effect is achieved without increasing the intensity of the less useful, low wavelength absorption peaks of the PC. Remarkably, this strong 655 nm absorption takes advantage of deep-red (650–700 nm) light, a major component of solar light exhibiting good atmosphere penetration, exploited by the natural PC chlorophyll a as well. Compared with ZnTPP, ZnTPTBP displayed a 49% increase in PET-RAFT polymerization rate with good control, marking a significant leap in the area of photo-controlled polymerization.
Progress on the Synthesis of the Aromathecin Family of Compounds: An Overview
Authors: Nishiyama Takashi , Mizuno Shota , Hieda Yuhzo , Choshi Tominari
Published: May 2024

We present a systematic review of the methods developed for the synthesis of the aromathecin family of compounds (benz[6,7]indolizino[1,2-b]quinolin-11(13H)-ones) and their derivatives. These methods can be broadly classified into four categories based on the construction of pentacyclic structures: Category 1: by constructing a pyridone moiety (D-ring) on the pyrroloquinoline ring (A/B/C-ring), Category 2: by constructing a pyridine moiety (B-ring) on the pyrroloisoquinolone ring (C/D/E-ring), Category 3: by constructing an indolizidinone moiety (C/D-ring) in a tandem reaction, and Category 4: by constructing a pyrrolidine moiety (C-ring) on the isoquinolone ring (D/E-ring).
Sequestration of an Azo Dye by a Potential Biosorbent: Characterization of Biosorbent, Adsorption Isotherm and Adsorption Kinetic Studies
Authors: Gaur Bharti , Mittal Jyoti , Shah Syed Ansar Ali , Mittal Alok , Baker Richard T.
Published: May 2024

This study explores the detailed characterization of a biosorbent (Hen Feather) and its efficient use in eradicating the azo dye Metanil Yellow (MY) from its aqueous solutions. Effects of a range of experimental parameters, including pH, initial dye concentration, biosorbent dosage and contact time on the adsorption, were studied. A detailed physical and chemical characterization of the biosorbent was made using SEM, XRD, XPS and FTIR. During the optimization of adsorption parameters, the highest dye uptake of almost 99% was recorded at pH 2, dye concentration 2 × 10−5 M, 0.05 g of biosorbent and a contact period of 75 min. Various adsorption isotherm models were studied to gather different adsorption and thermodynamic parameters. The linearity of the Langmuir, Freundlich and D-R adsorption isotherms indicate homogeneous, multilayer chemisorption with high adsorption affinity between the dye and biosorbent. Values of the changes in the Gibbs free energy (ΔG°) and the enthalpy (ΔH°) of the adsorption process have been calculated, these values indicate that it is a spontaneous and endothermic process. Kinetics of the adsorption were also measured, and it was established that the adsorption of MY over Hen Feather follows a pseudo-second-order kinetic model at temperatures 30, 40 and 50 °C. The findings of this investigation clearly indicate that the studied biosorbent exhibits a high affinity towards the dye (MY), and it can be effectively, economically and efficiently used to sequestrate and eradicate MY from its aqueous solutions.
Synthesis of Fluorinated Nucleosides/Nucleotides and Their Antiviral Properties
Authors: Kothapalli Yugandhar , Jones Ransom A. , Chu Chung K. , Singh Uma S.
Published: May 2024

The FDA has approved several drugs based on the fluorinated nucleoside pharmacophore, and numerous drugs are currently in clinical trials. Fluorine-containing nucleos(t)ides offer significant antiviral and anticancer activity. The insertion of a fluorine atom, either in the base or sugar of nucleos(t)ides, alters its electronic and steric parameters and transforms the lipophilicity, pharmacodynamic, and pharmacokinetic properties of these moieties. The fluorine atom restricts the oxidative metabolism of drugs and provides enzymatic metabolic stability towards the glycosidic bond of the nucleos(t)ide. The incorporation of fluorine also demonstrates additional hydrogen bonding interactions in receptors with enhanced biological profiles. The present article discusses the synthetic methodology and antiviral activities of FDA-approved drugs and ongoing fluoro-containing nucleos(t)ide drug candidates in clinical trials.
Recent Advancements in Metallic Au- and Ag-Based Chitosan Nanocomposite Derivatives for Enhanced Anticancer Drug Delivery
Authors: El-Meligy Mahmoud A. , Abd El-Monaem Eman M. , Eltaweil Abdelazeem S. , Mohy-Eldin Mohamed S. , Ziora Zyta M. , Heydari Abolfazl , Omer Ahmed M.
Published: May 2024

The rapid advancements in nanotechnology in the field of nanomedicine have the potential to significantly enhance therapeutic strategies for cancer treatment. There is considerable promise for enhancing the efficacy of cancer therapy through the manufacture of innovative nanocomposite materials. Metallic nanoparticles have been found to enhance the release of anticancer medications that are loaded onto them, resulting in a sustained release, hence reducing the dosage required for drug administration and preventing their buildup in healthy cells. The combination of nanotechnology with biocompatible materials offers new prospects for the development of advanced therapies that exhibit enhanced selectivity, reduced adverse effects, and improved patient outcomes. Chitosan (CS), a polysaccharide possessing distinct physicochemical properties, exhibits favorable attributes for controlled drug delivery due to its biocompatibility and biodegradability. Chitosan nanocomposites exhibit heightened stability, improved biocompatibility, and prolonged release characteristics for anticancer medicines. The incorporation of gold (Au) nanoparticles into the chitosan nanocomposite results in the manifestation of photothermal characteristics, whereas the inclusion of silver (Ag) nanoparticles boosts the antibacterial capabilities of the synthesized nanocomposite. The objective of this review is to investigate the recent progress in the utilization of Ag and Au nanoparticles, or a combination thereof, within a chitosan matrix or its modified derivatives for the purpose of anticancer drug delivery. The research findings for the potential of a chitosan nanocomposite to deliver various anticancer drugs, such as doxorubicin, 5-Fluroacil, curcumin, paclitaxel, and 6-mercaptopurine, were investigated. Moreover, various modifications carried out on the chitosan matrix phase and the nanocomposite surfaces to enhance targeting selectivity, loading efficiency, and pH sensitivity were highlighted. In addition, challenges and perspectives that could motivate further research related to the applications of chitosan nanocomposites in cancer therapy were summarized.
Antiproliferative and Pro-Apoptotic Activity and Tubulin Dynamics Modulation of 1H-Benzimidazol-2-yl Hydrazones in Human Breast Cancer Cell Line MDA-MB-231
Authors: Yancheva Denitsa , Argirova Maria , Georgieva Irina , Milanova Vanya , Guncheva Maya , Rangelov Miroslav , Todorova Nadezhda , Tzoneva Rumiana
Published: May 2024

(1) Background: The aim of the work is the evaluation of in vitro antiproliferative and pro-apoptotic activity of four benzimidazole derivatives containing colchicine-like and catechol-like moieties with methyl group substitution in the benzimidazole ring against highly invasive breast cancer cell line MDA-MB-231 and their related impairment of tubulin dynamics. (2) Methods: The antiproliferative activity was assessed with the MTT assay. Alterations in tubulin polymerization were evaluated with an in vitro tubulin polymerization assay and a docking analysis. (3) Results: All derivatives showed time-dependent cytotoxicity with IC50 varying from 40 to 60 μM after 48 h and between 13 and 20 μM after 72 h. Immunofluorescent and DAPI staining revealed the pro-apoptotic potential of benzimidazole derivatives and their effect on tubulin dynamics in living cells. Compound 5d prevented tubulin aggregation and blocked mitosis, highlighting the importance of the methyl group and the colchicine-like fragment. (4) Conclusions: The benzimidazole derivatives demonstrated moderate cytotoxicity towards MDA-MB-231 by retarding the initial phase of tubulin polymerization. The derivative 5d containing a colchicine-like moiety and methyl group substitution in the benzimidazole ring showed potential as an antiproliferative agent and microtubule destabilizer by facilitating faster microtubule aggregation and disrupting cellular and nuclear integrity.
Indulging Curiosity: Preliminary Evidence of an Anxiolytic-like Effect of Castor Oil and Ricinoleic Acid
Authors: Nisbett Khalin E. , Vendruscolo Leandro F. , Koob George F.
Published: May 2024

In the process of validating the elevated zero maze, a common test of anxiety-like behavior, in our laboratory, we demonstrated an anxiolytic-like effect of castor oil and its primary component, ricinoleic acid. We tested the effects of vehicle and chlordiazepoxide in male mice in the elevated zero maze following a 30-min pretreatment time. Chlordiazepoxide is a United States Food and Drug Administration-approved drug that was previously shown to exert anxiolytic-like effects in both the elevated zero maze and elevated plus maze. Chlordiazepoxide was administered at doses of 5 or 10 mg/kg. We used 5% polyoxyl 35 castor oil (Kolliphor® EL) and saline as treatment vehicles and found that the effect of chlordiazepoxide on open zone occupancy and open zone entries was blunted when 5% Kolliphor was used as the vehicle. These tests demonstrated that chlordiazepoxide increased open zone occupancy and entries in the elevated zero maze more effectively when saline was used as the treatment vehicle and that Kolliphor dampened the anxiolytic-like effect of chlordiazepoxide when it was used as the treatment vehicle. Notably, 5% Kolliphor alone slightly increased baseline open zone occupancy and entries. Given that Kolliphor is a derivative of castor oil, we next tested the effect of 5% castor oil and 5% ricinoleic acid, which is a major component of castor oil. We found that both castor oil and ricinoleic acid increased open zone occupancy but not entries compared with saline. Altogether, our findings demonstrate that Kolliphor, castor oil, and ricinoleic acid may exert anxiolytic-like effects in male mice in the elevated zero maze. This potential anxiolytic-like effect of castor oil is consistent with its well-established beneficial effects, including anti-inflammatory, antioxidant, antifungal, and pain-relieving properties.
Exploring the Immunomodulatory Potential of Human Milk: Aryl Hydrocarbon Receptor Activation and Its Impact on Neonatal Gut Health
Authors: Wieser Naomi V. , Ghiboub Mohammed , Verseijden Caroline , van Goudoever Johannes B. , Schoonderwoerd Anne , de Meij Tim G. J. , Niemarkt Hendrik J. , Davids Mark , Lefèvre Antoine , Emond Patrick , Derikx Joep P. M. , Jonge Wouter J. de , Sovran Bruno
Published: May 2024

Several metabolites of the essential amino acid tryptophan have emerged as key players in gut homeostasis through different cellular pathways, particularly through metabolites which can activate the aryl hydrocarbon receptor (AHR). This study aimed to map the metabolism of tryptophan in early life and investigate the effects of specific metabolites on epithelial cells and barrier integrity. Twenty-one tryptophan metabolites were measured in the feces of full-term and preterm neonates as well as in human milk and formula. The ability of specific AHR metabolites to regulate cytokine-induced IL8 expression and maintain barrier integrity was assessed in Caco2 cells and human fetal organoids (HFOs). Overall, higher concentrations of tryptophan metabolites were measured in the feces of full-term neonates compared to those of preterm ones. Within AHR metabolites, indole-3-lactic acid (ILA) was significantly higher in the feces of full-term neonates. Human milk contained different levels of several tryptophan metabolites compared to formula. Particularly, within the AHR metabolites, indole-3-sulfate (I3S) and indole-3-acetic acid (IAA) were significantly higher compared to formula. Fecal-derived ILA and milk-derived IAA were capable of reducing TNFα-induced IL8 expression in Caco2 cells and HFOs in an AHR-dependent manner. Furthermore, fecal-derived ILA and milk-derived IAA significantly reduced TNFα-induced barrier disruption in HFOs.
Understanding Health-Related Motivations for Urban Food Self-Production in the Light of Semantic Fields Analysis
Authors: Duda Ewa
Published: May 2024

One of the contemporary challenges facing urban areas is the necessity to identify novel approaches to resident involvement in solution creation, with a particular focus on ensuring the best possible nutrition. By investigating the process of co-participation of city dwellers in a unique education project, this paper aims to gain a deeper understanding of the health-related motivations that underpin the decision of early adopters of the implemented technological innovations to join the social experiment. The qualitative study employed purposive sampling and in-depth interviews conducted in two waves, the first between October and November 2022 and the second between September 2023 and January 2024. The study comprised 42 participants drawn from two communities of residents in Łódź and Warsaw, Poland. Transcriptions of the interviews were carried out using semantic field analysis, employing a quantitative approach that counts the frequency of keyword occurrences. Three categories of semantic fields were identified: associations, oppositions, and actions toward the subject, including positive, neutral, and negative temperatures. The findings demonstrate that the health concerns of residents are a pivotal factor in their decision to participate in urban food self-production initiatives, given their limited access to nutritious and healthy vegetables. This is related to several factors, including restrictions related to urbanization and the displacement of local suppliers, lifestyle, and the fast pace of urban life. The dissemination of innovative solutions for growing food in urban environments could, therefore, facilitate awareness-raising and motivation to alter the dietary habits of inhabitants.
Associations of Flavonoid Intakes with Mortality among Populations with Hypertension: A Prospective Cohort Study
Authors: Wang Kang , Lu Taotao , Yang Rukai , Zhou Shenghua
Published: May 2024

Background: The effect of flavonoid consumption on all-cause and special-cause mortality remains unclear among populations with hypertension. Methods: A total of 6110 people with hypertension from three NHANES survey cycles (2007–2008, 2009–2010, and 2017–2018) were enrolled in this study. Cox proportional hazard models were conducted to estimate the association between the intake of total flavonoids and flavonoid subclasses and all-cause, cancer-related, and cardiovascular disease (CVD)-related mortality. Nonlinear relationships were identified using restricted cubic splines (RCS). Results: During 43,977 person-years of follow-up, 1155 participants died from any cause, 282 participants died from CVD, and 265 participants died from cancer. After adjusting for relevant confounders, including demographic, lifestyle, and dietary intake, a higher intake of total flavonoids was significantly associated with lower all-cause mortality but not CVD-related and cancer-related mortality among the population with hypertension. Compared with extreme quartiles, the hazard ratio (HR) and 95% confidence interval (CI) were 0.74 (0.56–0.97) for all-cause mortality, 0.77 (0.40–1.46) for CVD-related mortality, and 0.62 (0.35–1.08) for cancer-related mortality. In terms of all-cause mortality, this inverse association was optimized at total flavonoid consumption of approximately 375 mg/day. In addition, the negative association between total flavonoid consumption and all-cause mortality was more pronounced in non-obese (BMI < 30 kg/m2) compared to obese (BMI ≥ 30 kg/m2) populations. Higher intakes of anthocyanidin, flavan-3-ol, flavonol, and isoflavone were significantly associated with lower all-cause mortality (HR (95%CI): 0.70 (0.55–0.89); 0.76 (0.59–0.96); 0.66 (0.46–0.94); 0.79 (0.67–0.93), respectively). Higher intakes of anthocyanidin, flavan-3-ol, and flavonol were significantly associated with lower cancer-related mortality (HR (95%CI): 0.55 (0.32–0.93); 0.51 (0.31–0.82); 0.52 (0.28–0.96), respectively). Conclusion: This study suggests that a heightened consumption of total flavonoids and some flavonoid subclasses was linked to lower mortality, which supports the proposal of increasing flavonoid intake as part of healthy diets in patients with hypertension.
Differences in the Evaluation of Malnutrition and Body Composition Using Bioelectrical Impedance Analysis, Nutritional Ultrasound, and Dual-Energy X-ray Absorptiometry in Patients with Heart Failure
Authors: Benitez-Velasco Ana , Alzas-Teomiro Carlos , Zurera Gómez Carmen , Muñoz Jiménez Concepción , López Aguilera José , Crespin Manuel , Vallejo-Casas Juan Antonio , Gálvez-Moreno María Ángeles , Molina Puerta María José , Herrera-Martínez Aura D.
Published: May 2024

Background: Although malnutrition is frequently observed in patients with heart failure (HF), this diagnosis should be performed carefully since HF itself is associated with increased inflammatory activity, which affects body weight, functionality, and some nutritional parameters; thus, its isolated interpretation can erroneously identify surrogate markers of severity as markers of malnutrition. In this context, we aimed to evaluate the prevalence of malnutrition using different classification systems and perform a comprehensive nutritional evaluation to determine the reliability of different diagnostic techniques. Patients and methods: Eighty-three patients with a recent hospital admission due to HF were evaluated. GLIM diagnosis criteria and subjective global assessment (SGA) were performed; a comprehensive anthropometric, functional, and biochemical nutritional evaluation was performed, in which bioelectrical impedance analysis (BIA), nutritional ultrasound, and dual-energy X-ray absorptiometry (DXA) were performed. Additionally, mortality and additional admissions due to HF were determined after a mean follow up of 18 months. Results: Malnutrition according to the GLIM criteria (54%) accurately distinguished patients with impaired functionality, lower lean mass, skeletal mass index, and appendicular muscle mass (BIA), as well as lower trunk fat mass, trunk lean mass, fat-free mass (DXA), and decreased albumin and increased C-reactive protein serum levels. According to SGA, there were significant changes in body composition parameters determined by BIA, muscle ultrasound, and functional tests between well-nourished patients and patients with risk of malnutrition (53.7%) or who had malnutrition (7.1%), but not when the last two groups were compared. BIA and DXA showed strong correlations when evaluating muscle and fat mass in HF patients, but correlations with nutritional ultrasound were limited, as well as functional tests. A multivariate analysis showed that no significant association was observed between body composition and mortality, but preperitoneal fat was associated with an increased risk of new hospital admissions (OR: 0.73). Conclusions: GLIM criteria identified a lower percentage of patients with HF and malnutrition compared with SGA; thus, SGA could have a role in preventing malnutrition in HF patients. Nutritional evaluation with BIA and DXA in patients with HF showed reliable results of body composition parameters in HF, and both help with the diagnosis of malnutrition according to the GLIM or SGA criteria and could provide complementary information in some specific cases.
Functional Gastrointestinal Symptoms in Children with Autism and ADHD: Profiles of Hair and Salivary Cortisol, Serum Leptin Concentrations and Externalizing/Internalizing Problems
Authors: Petropoulos Andreas , Anesiadou Sophia , Michou Maria , Lymperatou Aikaterini , Roma Eleftheria , Chrousos George , Pervanidou Panagiota
Published: May 2024

Background: Functional Gastrointestinal Disorders (FGIDs) present a higher prevalence in individuals with Neurodevelopmental Disorders (NDDs). The Stress System and the Gut–Brain axis (GBA) may mediate these relations. We aimed to assess the prevalence and profile of FGIDs in a clinical sample of children with Autism Spectrum Disorder (ASD) and Attention Deficit/Hyperactivity Disorder (ADHD) compared to typically developing children (TD) as well as to investigate possible relations between stress-related biomarkers and internalizing/externalizing problems in children with NDDS. Methods: In total, 120 children, aged between 4 and 12 years old, formed three groups (N = 40, each): ADHD, ASD and TD. Salivary cortisol, hair cortisol and serum leptin were measured. Results: The ASD group had more FGID problems than the TD group (p = 0.001). The ADHD and ASD groups had higher total internalizing/externalizing problems than the TD group (p < 0.0001, p < 0.0001, p = 0.005, respectively). Children with FGIDs showed more total, internalizing and externalizing problems compared to children without FGIDs (p < 0.0001, p < 0.0001, p = 0.041, respectively). The ADHD group showed lower AUCg values (p < 0.0001), while the hair cortisol was higher for the TD group (p < 0.0001). Conclusion: In conclusion, children with NDDs had more FGID symptoms and present higher internalizing and externalizing problems. Children with ADHD and FGIDs had more internalizing problems compared to those without FGIDs. No differences in stress-related biomarkers were shown to differentiate children with NDDs with and without FGIDs. Future prospective studies including a greater number of children may elucidate the biological pathways linking these comorbidities.
Genetic Diversity of Mycobacterium tuberculosis Strains Isolated from HIV-Infected Patients in Mexico
Authors: Valencia-Trujillo Daniel , Avila-Trejo Amanda Marineth , García-Reyes Rocío Liliana , Narváez-Díaz Luis , Segura del Pilar Mariela , Mújica-Sánchez Mario Alberto , Becerril-Vargas Eduardo , León-Juárez Moises , Mata-Miranda Mónica Maribel , Rivera-Gutiérrez Sandra , Cerna-Cortés Jorge Francisco
Published: May 2024

There has been very limited investigation regarding the genetic diversity of Mycobacterium tuberculosis (MTb) strains isolated from human immunodeficiency virus (HIV)-infected patients in Mexico. In this study, we isolated 93 MTb strains from pulmonary and extrapulmonary samples of HIV-infected patients treated in a public hospital in Mexico City to evaluate the genetic diversity using spoligotyping and mycobacterial interspersed repetitive unit-variable-number tandem-repeat (MIRU-VNTR) typing (based on 24 loci). The cohort comprised 80 male and 13 female individuals. There was a positive correlation between a high HIV viral load (>100,000 copies) and extrapulmonary tuberculosis (TB) (r = 0.306, p = 0.008). Lineage 4 was the most frequent lineage (79 strains). In this lineage, we found the H clade (n = 24), including the Haarlem, H3, and H1 families; the T clade (n = 22), including T1 and T2; the X clade (n = 15), including X1 and X3; the LAM clade (n = 14), including LAM1, LAM2, LAM3, LAM6, and LAM9; the S clade (n = 2); Uganda (n = 1); and Ghana (n = 1). We also found 12 strains in the EAI clade belonging to lineage 1, including the EAI2-Manila and EAI5 families. Interestingly, we identified one strain belonging to the Beijing family, which is part of lineage 2. One strain could not be identified. This study reports high genetic diversity among MTb strains, highlighting the need for a molecular epidemiological surveillance system that can help to monitor the spread of these strains, leading to more appropriate measures for TB control in HIV-infected patients.
Effects of Smallanthus sonchifolius Flour on Metabolic Parameters: A Systematic Review
Authors: Silva Isabela Frazão da , Bragante Wesley Rossi , Junior Renato Cesar Moretti , Laurindo Lucas Fornari , Guiguer Elen Landgraf , Araújo Adriano Cressoni , Fiorini Adriana M. R. , Nicolau Claudia C. T. , Oshiiwa Marie , Lima Enzo Pereira de , Barbalho Sandra Maria , Silva Luís R.
Published: May 2024

Smallanthus sonchifolius, popularly known as yacon, is a member of the Asteraceae family. Due to its medicinal and edible value, yacon is consumed by different populations. Yacon is unique due to its high fructo-oligosaccharide and inulin content, as well as flavonoids, sesquiterpene lactones, and phenolic acids. Roots can be used to produce flour, which is less perishable and can be applied in various industrial products. This systematic review focuses on the effects of yacon flour on metabolic parameters. PubMed, Cochrane, Embase, Science Direct, Scopus, Web of Science, and Google Scholar databases were consulted, and PRISMA guidelines were followed in the selection of the studies. In total, 526 articles were found in the databases, and of these, only 28 full texts were eligible for inclusion. After applying the inclusion and exclusion criteria, seven studies were finally included. The results showed that the use of yacon flour can reduce glycemia, HbA1c, advanced glycation ends, plasma lipids, body fat mass, body weight, and waist circumference and improve intestinal microbiota and the antioxidant status. Further exploration of the effects of yacon flour is warranted, and additional clinical trials are necessary to determine the optimal daily consumption levels required to assist in improving metabolic parameters.
Discovery and Anticancer Screening of Novel Oxindole-Based Derivative Bearing Pyridyl Group as Potent and Selective Dual FLT3/CDK2 Kinase Inhibitor
Authors: Soudi Aya , Bender Onur , Celik Ismail , El-Hafeez Amer Ali Abd , Dogan Rumeysa , Atalay Arzu , Elkaeed Eslam B. , Alsfouk Aisha A. , Abdelhafez Elshimaa M. N. , Aly Omar M. , Sippl Wolfgang , Ali Taha F. S.
Published: May 2024

Protein kinases regulate cellular activities and make up over 60% of oncoproteins and proto-oncoproteins. Among these kinases, FLT3 is a member of class III receptor tyrosine kinase family which is abundantly expressed in individuals with acute leukemia. Our previous oxindole-based hit has a particular affinity toward FLT3 (IC50 = 2.49 μM) and has demonstrated selectivity towards FLT3 ITD-mutated MV4-11 AML cells, with an IC50 of 4.3 μM. By utilizing the scaffold of the previous hit, sixteen new compounds were synthesized and screened against NCI-60 human cancer cell lines. This leads to the discovery of a potent antiproliferative compound, namely 5l, with an average GI50 value against leukemia and colon cancer subpanels equalling 3.39 and 5.97 µM, respectively. Screening against a specific set of 10 kinases that are associated with carcinogenesis indicates that compound 5l has a potent FLT3 inhibition (IC50 = 36.21 ± 1.07 nM). Remarkably, compound 5l was three times more effective as a CDK2 inhibitor (IC50 = 8.17 ± 0.32 nM) compared to sunitinib (IC50 = 27.90 ± 1.80 nM). Compound 5l was further analyzed by means of docking and molecular dynamics simulation for CDK2 and FLT3 active sites which provided a rational for the observed strong inhibition of kinases. These results suggest a novel structural scaffold candidate that simultaneously inhibits CDK2 and FLT3 and gives encouragement for further development as a potential therapeutic for leukemia and colon cancer.
An International Data-Based Systems Agency IDA: Striving for a Peaceful, Sustainable, and Human Rights-Based Future
Authors: Kirchschlaeger Peter G.
Published: May 2024

Digital transformation and “artificial intelligence (AI)”—which can more adequately be called “data-based systems (DS)”—comprise ethical opportunities and risks. Therefore, it is necessary to identify precisely ethical opportunities and risks in order to be able to benefit sustainably from the opportunities and to master the risks. The UN General Assembly has recently adopted a resolution aiming for ‘safe, secure and trustworthy artificial intelligence systems’. It is now urgent to implement and build on the UN General Assembly Resolution. Allowing humans and the planet to flourish sustainably in peace and guaranteeing globally that human dignity is respected not only offline but also online, in the digital sphere, and in the domain of DS, requires two policy measures: (1) human rights-based data-based systems (HRBDS): HRBDS means that human rights serve as the basis of digital transformation and DS. (2) International Data-Based Systems Agency (IDA): IDA should be established at the UN as a platform for cooperation in the field of digital transformation and DS, fostering human rights, security, and peaceful uses of DS, as well as a global supervisory institution and regulatory authority in digital transformation and DS. The establishment of IDA is realistic because humanity has already shown in its past that we are able to not always “blindly” pursue the technically possible but also to limit ourselves to what is technically feasible when humanity and the planet are at stake. For instance, humans researched the field of nuclear technology, developed the atomic bomb, and detonated it several times. Nonetheless, the same humans limited research and development in the field of nuclear technology to prevent even worse consequences by establishing the International Atomic Energy Agency (IAEA) at the UN.
Growth, Productivity, Yield Components and Seasonality of Different Genotypes of Forage Clover Lotus corniculatus L. under Varied Soil Moisture Contents
Authors: Xolocotzi-Acoltzi Sahara , Pedroza-Sandoval Aurelio , García-De los Santos Gabino , Álvarez-Vázquez Perpetuo , Gramillo-Ávila Isaac
Published: May 2024

This study aimed to evaluate the response to water deficit of different ecotypes and a variety of Lotus corniculatus on growth, productivity, and yield components, through seasonal times. A randomized block experimental design in a 2 × 5 factorial arrangement with three replicates was used. The first variation factor was soil moisture contents: field capacity (FC) was 26.5% ± 1.5, and water deficit (WD) was 85% of FC (22.5% ± 1.5); the second variation factor was the ecotypes identified with the codes 255301, 255305, 202700 and 226792 and of the variety Estanzuela Ganador. The best responses in plant cover and weight of accumulated fresh biomass were obtained in the ecotype 202700 under WD, with values of 1649.0 cm2 and 583.7 g plant−1, and 1661.2 cm2 and 740.1 g plant−1 in ecotype 255305 under FC. The leaf clover was the main component of yield during the summer and autumn seasons. Ecotype 226792 was tolerant to low temperatures during the winter season with better leaf development. Ecotype 202700 is the best option for forage clover production when water is limited, and ecotype 255305 when water is not resource-limited, but these preliminary conclusions need to be confirmed in field studies.
Antibacterial and Antibiofilm Potential of Ethanolic Extracts of Duguetia vallicola (Annonaceae) against in-Hospital Isolates of Pseudomonas aeruginosa
Authors: Contreras-Martínez Orfa Inés , Sierra-Quiroz Daniela , Angulo-Ortíz Alberto
Published: May 2024

Pseudomonas aeruginosa is an opportunistic pathogen that is especially dominant in people with cystic fibrosis; the drug resistance expressed by this pathogen and its capacity for adaptation poses a significant challenge to its treatment and control, thereby increasing morbidity and mortality rates globally. In this sense, the search for new treatment alternatives is imminent today, with products of plant origin being an excellent alternative for use. The objective of this research was to evaluate the antibacterial and antibiofilm potential and to explore the possible effect of ethanolic extracts from the wood and bark of Duguetia vallicola on the cell membrane. Microdilution assays showed the inhibition of bacterial growth by more than 50%, with the lowest concentration (62.5 μg/mL) of both extracts evaluated. Furthermore, we report the ability of both extracts to inhibit mature biofilms, with inhibition percentages between 48.4% and 93.7%. Intracellular material leakage experiments (260/280 nm), extracellular pH measurements, and fluorescence microscopy with acridine orange (AO) and ethidium bromide (EB) showed cell membrane damage. This indicates that the antibacterial action of ethanolic extracts of D. vallicola is associated with damage to the integrity of the cell membrane and consequent death of these pathogens. These results serve as a reference for future studies in establishing the mechanisms of action of these extracts.
Osmophore Structure and Labellum Micromorphology in Ophrys speculum (Orchidaceae): New Interpretations of Floral Features and Implications for a Specific Sexually Deceptive Pollination Interaction
Authors: Francisco Ana , Ascensão Lia
Published: May 2024

Pollination by sexual deception specifically attracts male insects, through the floral scent and particular morphological features of the flower that serve as visual and tactile stimuli. The unique bond between the Ophrys speculum orchid and the male Dasyscolia ciliata wasp primarily stems from a few distinctive semiochemicals that mimic the female wasp’s sex pheromone, although the floral scent comprises a variety of compounds. An osmophore producing highly volatile compounds has been documented in four close relatives of O. speculum and is now being also investigated in this species. Given the existing debates regarding the structure of the labellum and stigmatic cavity in O. speculum, this study details their micromorphology. Additionally, comparisons of O. speculum flowers and female D. ciliata wasps under stereomicroscopy and scanning electron microscopy are conducted to seek new evidence of visual and tactile mimicry. The findings confirm that (i) an osmophore is present at the apical margin of the labellum in O. speculum flowers; (ii) the labellum features a distinct basal field homologous to those found in other Ophrys species; and (iii) the basal labellum region closely mimics the female wasp’s thorax and wings. The implications of these novel floral features are discussed within an evolutionary context.
Enhancing Salt Stress Tolerance in Tomato (Solanum lycopersicum L.) through Silicon Application in Roots
Authors: Ferrández-Gómez Borja , Jordá Juana D. , Cerdán Mar , Sánchez-Sánchez Antonio
Published: May 2024

Soil salinization poses a significant threat to agricultural productivity, necessitating innovative agronomic strategies to mitigate its impact. This study focuses on improving salt stress resistance in tomato plants through the application of silicon (Si) in roots. A greenhouse experiment was carried out under normal conditions (control, and 1 and 4 mM Si) and under salinity stress (salt control, and 1 and 4 mM Si). Various parameters were analyzed in leaves and roots. Under normal conditions, tomato plants grown in non-saline conditions exhibited some toxicity when exposed to Na2SiO3. As for the experiments under salt stress conditions, Si mitigated oxidative damage, preserving root cell membrane integrity. The concentration of malondialdehyde was reduced by 69.5%, that of proline was reduced by 56.4% and there was a 57.6% decrease in catalase activity for tomato plants treated with 1 mM Si under salt stress. Furthermore, Fe uptake and distribution, under salt conditions, increased from 91 to 123 mg kg−1, the same concentration as that obtained for the normal control. In all cases, the lower dose produced better results under normal conditions than the 4 mM dose. In summary, this research provides a potential application of Si in non-fertigated crop systems through a radicular pathway.
Infraspecific Variation in Silene Seed Tubercles
Authors: Martín-Gómez José , Rodríguez-Lorenzo José , Juan Ana , Tocino Ángel , Cervantes Emilio
Published: May 2024

The seeds of many species in the order Caryophyllales exhibit surface protuberances called tubercles. While tubercle shape and distribution have often been proposed as taxonomic criteria, paradoxically, their description has primarily relied on adjectives, with quantitative data on tubercle width, height, and other measurements lacking in the literature. Recently, a quantitative analysis of seed surface tubercles based on tubercle width, height, and curvature values (maximum and average curvature, and maximum to average curvature ratio) was proposed and applied to individual populations of a total of 31 species, with 12 belonging to Silene subg. Behenantha and 19 to S. subg. Silene. Tubercles were classified into two categories: echinate and rugose. Echinate tubercles exhibited higher values of height and curvature, and lower width, and were more prevalent in species of S. subg. Behenantha, while the rugose type was more abundant in S. subg. Silene. This work explored infraspecific differences in tubercle size and shape. For this, measurements of tubercle width, height and curvature were applied to 31 populations of eight species of Silene. Significant differences between populations were observed for most of the species examined. A particular tubercle type, previously described as umbonate or mammillate, was identified in S. nocturna seeds, characterized by high curvature values.
Changes in the Aroma Profile and Phenolic Compound Contents of Different Strawberry Cultivars during Ripening
Authors: Simkova Kristyna , Veberic Robert , Grohar Mariana Cecilia , Pelacci Massimiliano , Smrke Tina , Ivancic Tea , Medic Aljaz , Cvelbar Weber Nika , Jakopic Jerneja
Published: May 2024

Secondary metabolites, namely, phenolic and volatile organic compounds, contribute to the nutritional and organoleptic quality of the strawberry fruit. This study focuses on the changes in the content of phenolic compounds and volatile organic compounds during the ripening, from green to overripe fruit, of five strawberry cultivars (‘Asia’, ‘CIVN 766’, ‘Aprica’, ‘Clery’, and ‘Malwina’). Additionally, these changes are compared with the colour of the fruit and peroxidase and polyphenol oxidase activity. Our results show that the accumulation of secondary metabolites (phenolic and volatile organic compounds) significantly changed during the ripening process for all of the studied cultivars. As for phenolic compounds, flavanols and hydroxybenzoic acid derivatives comprised between 87 and 95% of the total phenolic compound content in unripe green fruit. In contrast, anthocyanins and hydroxycinnamic acid derivatives comprised between 64 and 77% of the total phenolic compound content in overripe fruit, except in the fruit of the cultivar ‘CIVN766’. When it comes to the aroma profile, the content of aldehydes decreased by 24–49% as the fruit ripened, and the accumulation of esters increased. Our study also shows that the ripening process differs among cultivars, and it is therefore necessary to define ripening indicators separately for each cultivar.
Research Progress on Plant Shaker K+ Channels
Authors: Yuan Guang , Nong Tongjia , Hunpatin Oluwaseyi Setonji , Shi Chuhan , Su Xiaoqing , Wang Qian , Liu Haobao , Dai Peigang , Ning Yang
Published: May 2024

Plant growth and development are driven by intricate processes, with the cell membrane serving as a crucial interface between cells and their external environment. Maintaining balance and signal transduction across the cell membrane is essential for cellular stability and a host of life processes. Ion channels play a critical role in regulating intracellular ion concentrations and potentials. Among these, K+ channels on plant cell membranes are of paramount importance. The research of Shaker K+ channels has become a paradigm in the study of plant ion channels. This study offers a comprehensive overview of advancements in Shaker K+ channels, including insights into protein structure, function, regulatory mechanisms, and research techniques. Investigating Shaker K+ channels has enhanced our understanding of the regulatory mechanisms governing ion absorption and transport in plant cells. This knowledge offers invaluable guidance for enhancing crop yields and improving resistance to environmental stressors. Moreover, an extensive review of research methodologies in Shaker K+ channel studies provides essential reference solutions for researchers, promoting further advancements in ion channel research.
Artificial Intelligence and an Anthropological Ethics of Work: Implications on the Social Teaching of the Church
Authors: Onyeukaziri Justin Nnaemeka
Published: May 2024

It is the contention of this paper that ethics of work ought to be anthropological, and artificial intelligence (AI) research and development, which is the focus of work today, should be anthropological, that is, human-centered. This paper discusses the philosophical and theological implications of the development of AI research on the intrinsic nature of work and the nature of the human person. AI research and the implications of its development and advancement, being a relatively new phenomenon, have not been comprehensively interrogated in the social and ethical teachings of the Catholic Church. This paper, therefore, proposes a path for this interrogation by expounding a discourse which is believed to be epistemically helpful in the developing discourse of AI in the ethical and social teachings of the Church. The advancement in the research on AI is not only redefining the meaning of work, but, even more so, it is questioning the metaphysical notion of the human person and the theological notion of work as an intrinsic part in the selfhood and dignity of the human person.
Compilation of Dictionaries and Scientific and Technological Translations by Western Protestant Missionaries in China in the Nineteenth Century
Authors: Tao Jin , Wan Lixin
Published: May 2024

The 19th century saw the important transformation of modern Western concepts into Chinese lexical resources. The missionaries were the initiators and important driving force for the translation of Western books into Chinese in modern China. They promoted ‘translating terms’ and ‘coining terms’ in their translations of Western books and the compilation of dictionaries with the cooperation of Chinese intellectuals. Their work provided a tangible ‘word’ carrier of ‘concepts’ for disseminating modern knowledge from the West to the East. Compiled by missionaries, the English–Chinese bilingual dictionaries introduced a brand-new concept of dictionary compilation and changed China’s history of having zidian (字典, character dictionaries) but no cidian (辞典, specialized dictionaries). In particular, John Fryer applied the translation method of creating new words or characters in the translation of chemical terminology. Members of the School and Textbook Series Committee, including John Fryer and Calvin Wilson Mateer, made great contributions to theories and strategies for translation, which keep inspiring Chinese–English translation of terminology and its theoretical construction.
DDFNet-A: Attention-Based Dual-Branch Feature Decomposition Fusion Network for Infrared and Visible Image Fusion
Authors: Wei Qiancheng , Liu Ying , Jiang Xiaoping , Zhang Ben , Su Qiya , Yu Muyao
Published: May 2024

The fusion of infrared and visible images aims to leverage the strengths of both modalities, thereby generating fused images with enhanced visible perception and discrimination capabilities. However, current image fusion methods frequently treat common features between modalities (modality-commonality) and unique features from each modality (modality-distinctiveness) equally during processing, neglecting their distinct characteristics. Therefore, we propose a DDFNet-A for infrared and visible image fusion. DDFNet-A addresses this limitation by decomposing infrared and visible input images into low-frequency features depicting modality-commonality and high-frequency features representing modality-distinctiveness. The extracted low and high features were then fused using distinct methods. In particular, we propose a hybrid attention block (HAB) to improve high-frequency feature extraction ability and a base feature fusion (BFF) module to enhance low-frequency feature fusion ability. Experiments were conducted on public infrared and visible image fusion datasets MSRS, TNO, and VIFB to validate the performance of the proposed network. DDFNet-A achieved competitive results on three datasets, with EN, MI, VIFF, QAB/F, FMI, and Qs metrics reaching the best performance on the TNO dataset, achieving 7.1217, 2.1620, 0.7739, 0.5426, 0.8129, and 0.9079, respectively. These values are 2.06%, 11.95%, 21.04%, 21.52%, 1.04%, and 0.09% higher than those of the second-best methods, respectively. The experimental results confirm that our DDFNet-A achieves better fusion performance than state-of-the-art (SOTA) methods.
GGMNet: Pavement-Crack Detection Based on Global Context Awareness and Multi-Scale Fusion
Authors: Wang Yong , He Zhenglong , Zeng Xiangqiang , Zeng Juncheng , Cen Zongxi , Qiu Luyang , Xu Xiaowei , Zhuo Qunxiong
Published: May 2024

Accurate and comprehensive detection of pavement cracks is important for maintaining road quality and ensuring traffic safety. However, the complexity of road surfaces and the diversity of cracks make it difficult for existing methods to accomplish this challenging task. This paper proposes a novel network named the global graph multiscale network (GGMNet) for automated pixel-level detection of pavement cracks. The GGMNet network has several innovations compared with the mainstream road crack detection network: (1) a global contextual Res-block (GC-Resblock) is proposed to guide the network to emphasize the identities of cracks while suppressing background noises; (2) a graph pyramid pooling module (GPPM) is designed to aggregate the multi-scale features and capture the long-range dependencies of cracks; (3) a multi-scale features fusion module (MFF) is established to efficiently represent and deeply fuse multi-scale features. We carried out extensive experiments on three pavement crack datasets. These were DeepCrack dataset, with complex background noises; the CrackTree260 dataset, with various crack structures; and the Aerial Track Detection dataset, with a drone’s perspective. The experimental results demonstrate that GGMNet has excellent performance, high accuracy, and strong robustness. In conclusion, this paper provides support for accurate and timely road maintenance and has important reference values and enlightening implications for further linear feature extraction research.