bluuebunny/crossref_metadata_2025 huggingface dataset:
Facile Solution-Refluxing Synthesis and Photocatalytic Dye Degradation of a Dynamic Covalent Organic Framework
Authors: Wang Xiao-Lian , Sun Yi-Ying , Xiao Yonghong , Chen Xiao-Xian , Huang Xiao-Chun , Zhou Hao-Long
Published: November 2022

Covalent organic frameworks (COFs), as a novel crystalline porous adsorbent, have been attracting significant attention for their synthesis and application exploration due to the advantages of designability, stability, and functionalization. Herein, through increasing the concentration of the acid catalyst, a facile solution-refluxing synthesis method was developed for the preparation of a three-dimensional dynamic COF material, COF-300, with high yields (>90%) and high space–time yields (>28 kg m–3 day–1). This synthesis method not only permits gram-scale synthesis, but also yields products that well maintain porosity and unique guest-dependent dynamic behavior. Moreover, the catalytic activity of COF-300 as a metal-free photocatalyst was explored for the first time. Under 365 nm ultra-violet light irradiation, COF-300 can effectively catalyze the dye degradation (>99%) in wastewater with good recyclability. By adding magnetic Fe3O4 nanoparticles into the solution-refluxing synthesis of COF-300, Fe3O4/COF-300 nanocomposites can be obtained and used as magnetically recyclable photocatalysts, demonstrating the superiority of this facile synthesis procedure. Our study provides new insights for the preparation of COF materials and a constructive exploration for their water treatment application.
Triptonoterpene, a Natural Product from Celastrus orbiculatus Thunb, Has Biological Activity against the Metastasis of Gastric Cancer Cells
Authors: Wang Haibo , Luo Yuanyuan , Hu Yaqi , Feng Xinyi , Feng Jun , Chu Zewen , Ou Shiya , Dai Xiaojun , Wang Xiaoqing , Liu Yanqing
Published: November 2022

Cancer is one of the greatest threats to human health. Gastric cancer (GC) is the fifth most common malignant tumor in the world. Invasion and metastasis are the major difficulties in the treatment of GC. Herbal medicines and their extracts have a lengthy history of being used to treat tumors in China. The anti-tumoral effects of the natural products derived from herbs have received a great deal of attention. Our previous studies have shown that the traditional Chinese herb Celastrus orbiculatus Thunb extract (COE) can inhibit the invasion and metastasis of GC cells, but the specific anti-cancer components of COE are still unclear. Dozens of natural products from COE have been isolated and identified by HPLC spectroscopy in our previous experiments. Triptonoterpene is one of the active ingredients in COE. In this study, we focused on revealing whether Triptonoterpene has an excellent anti-GC effect and can be used as an effective component of Celastrus orbiculatus Thunb in the treatment of tumors. We first observed that Triptonoterpene reduces GC cell proliferation through CCK-8 assays and colony formation experiments. The cell adhesion assays have shown that Triptonoterpene inhibits adhesion between cells and the cell matrix during tumor invasion. In addition, the cell migration assay has shown that Triptonoterpene inhibits the invasion and migration of GC cells. The high-connotation cell dynamic tracking experiment has also shown the same results. The effects of Triptonoterpene on epidermal mesenchymal transition (EMT)-related and matrix metalloproteinases (MMPs)-related proteins in gastric cancer cells were detected by Western blots. We found that Triptonoterpene could significantly inhibit the changes in EMT-related and invasion and metastasis-related proteins. Altogether, these results suggest that Triptonoterpene is capable of inhibiting the migration and invasion of GC cells. Triptonoterpene, as a natural product from Celastrus orbiculatus Thunb, has significant anti-gastric cancer effects, and is likely to be one of the major equivalent components of Celastrus orbiculatus Thunb.
Physicochemical Properties and Antioxidant Activity of Portuguese Craft Beers and Raw Materials
Authors: Silva Sara , Oliveira Ana Isabel , Cruz Agostinho , Oliveira Rita Ferraz , Almeida Rubim , Pinho Cláudia
Published: November 2022

There is an increase in the popularity of craft beer, which is produced by small, independent, and traditional breweries. Since craft beer popularity is rising in Portugal this research focused on assessing physicochemical parameters, total phenolic content (TPC) and the antioxidant capacity of Portuguese craft beers and raw materials used in beer production. In this experimental study, 19 beer samples were analyzed. Parameters such as pH, Total Acidity, Reducing Sugar Content and TPC were evaluated. For the determination of antioxidant activity, DPPH scavenging activity and metal chelating activity (MCA) were analyzed in all samples. Craft beers demonstrated a high phenolic content (ranging from 343.78 mg GAE/L to 2172.49 mg GAE/L), significantly different from industrial beers. Craft beers demonstrated a higher inhibition of DPPH radicals and higher MCA than the raw materials. DPPH inhibition ranged from 36.5% to 96.0% for malt and 64.7% to 79.6% in hops samples. MCA also varied between the different samples, with results of 12.0% to 24.8% in malt samples and 3.8% to 23.5% in hops. Raw materials can potentially influence the antioxidant activity of the resulting beer. Positive correlations between TPC and physicochemical properties can be useful to help consumers choose beers with added value for health.
Influence of Organic Matter on the Sorption of Cefdinir, Memantine and Praziquantel on Different Soil and Sediment Samples
Authors: Mutavdžić Pavlović Dragana , Tolić Čop Kristina , Prskalo Helena , Runje Mislav
Published: November 2022

Pharmaceuticals are known for their great effects and applications in the treatment and suppression of various diseases in human and veterinary medicine. The development and modernization of science and technologies have led to a constant increase in the production and consumption of various classes of pharmaceuticals, so they pose a threat to the environment, which can be subjected to the sorption process on the solid phase. The efficiency of sorption is determined by various parameters, of which the physicochemical properties of the compound and the sorbent are very important. One of these parameters that determine pharmaceutical mobility in soil or sediment is the soil–water partition coefficient normalized to organic carbon (Koc), whose determination was the purpose of this study. The influence of organic matter, suspended in an aqueous solution of pharmaceutical (more precisely: cefdinir, memantine, and praziquantel), was studied for five different types of soil and sediment samples from Croatia. The linear, Freundlich, and Dubinin–Raduskevich sorption isotherms were used to determine specific constants such as the partition coefficient Kd, which directly describes the strength of sorbate and sorbent binding. The linear model proved to be the best with the highest correlation coefficients, R2 > 0.99. For all three pharmaceuticals, a positive correlation between sorption affinity described by Kd and Koc and the amount of organic matter was demonstrated.
Future Prospective of Radiopharmaceuticals from Natural Compounds Using Iodine Radioisotopes as Theranostic Agents
Authors: Nurhidayah Wiwit , Setyawati Luthfi Utami , Daruwati Isti , Gazzali Amirah Mohd , Subroto Toto , Muchtaridi Muchtaridi
Published: November 2022

Natural compounds provide precursors with various pharmacological activities and play an important role in discovering new chemical entities, including radiopharmaceuticals. In the development of new radiopharmaceuticals, iodine radioisotopes are widely used and interact with complex compounds including natural products. However, the development of radiopharmaceuticals from natural compounds with iodine radioisotopes has not been widely explored. This review summarizes the development of radiopharmaceuticals from natural compounds using iodine radioisotopes in the last 10 years, as well as discusses the challenges and strategies to improve future discovery of radiopharmaceuticals from natural resources. Literature research was conducted via PubMed, from which 32 research articles related to the development of natural compounds labeled with iodine radioisotopes were reported. From the literature, the challenges in developing radiopharmaceuticals from natural compounds were the purity and biodistribution. Despite the challenges, the development of radiopharmaceuticals from natural compounds is a golden opportunity for nuclear medicine advancement.
In Silico ADME and Toxicity Prediction of Benzimidazole Derivatives and Its Cobalt Coordination Compounds. Synthesis, Characterization and Crystal Structure
Authors: Raducka Anita , Świątkowski Marcin , Gobis Katarzyna , Szymański Paweł , Czylkowska Agnieszka
Published: November 2022

As a result of the synthesis, three new solids, cobalt (II) coordination compounds with benzimidazole derivatives, and chlorides were obtained. The ligands that were used in the synthesis were specially synthesized and were commercially unavailable. During the synthesis, a single crystal of the complex with the L1 ligand was obtained and the crystal structure was refined. All coordination compounds were characterized by elemental analysis, infrared spectroscopy, and thermogravimetric analysis. All the obtained data allowed one to determine the formulas of the new compounds, as well as to determine the method of metal–ligand coordination. Thermal analysis allowed to know the temperature stability of the compounds, solids intermediate and final products of pyrolysis. Additionally, volatile decomposition and fragmentation products have been identified. The toxicity of the compounds and their bioavailability were determined using in silico methods. By predicting activity on cell lines, the potential use of compounds as chemotherapeutic agents has been specified. The blood-brain barrier crossing and the gastrointestinal absorption were defined. Pharmaceutical biodistribution was also simulated.
One-Step Theory View on Photoelectron Diffraction: Application to Graphene
Authors: Krasovskii Eugene
Published: November 2022

Diffraction of photoelectrons emitted from the core 1s and valence band of monolayer and bilayer graphene is studied within the one-step theory of photoemission. The energy-dependent angular distribution of the photoelectrons is compared to the simulated electron reflection pattern of a low-energy electron diffraction experiment in the kinetic energy range up to about 55 eV, and the implications for the structure determination are discussed. Constant energy contours due to scattering resonances are well visible in photoelectron diffraction, and their experimental shape is well reproduced. The example of the bilayer graphene is used to reveal the effect of the scattering by the subsurface layer. The photoemission and LEED patterns are shown to contain essentially the same information about the long-range order. The diffraction patterns of C 1s and valence band photoelectrons bear similar anisotropy and are equally suitable for diffraction analysis.
Omnidirectional Triboelectric Nanogenerator for Wide-Speed-Range Wind Energy Harvesting
Authors: Wang Qiman , Li Wenhao , Wang Kun , Liao Yitao , Zheng Junjie , Zhou Xiongtu , Lin Jianpu , Zhang Yongai , Wu Chaoxing
Published: November 2022

The environmentally friendly harvesting of wind energy is an effective technique for achieving carbon neutrality and a green economy. In this work, a core–shell triboelectric nanogenerator (CS-TENG) for harvesting wind energy is demonstrated and the device structure parameters are optimized. The core–shell structure enables the CS-TENG to respond sensitively to wind from any direction and generate electrical output on the basis of the vertical contact–separation mode. A single device can generate a maximum power density of 0.14 W/m3 and can power 124 light-emitting diodes. In addition, wind energy can be harvested even at a wind speed as low as 2.3 m/s by paralleling CS-TENGs of different sizes. Finally, a self-powered water quality testing system that uses the CS-TENG as its power supply is built. The CS-TENG exhibits the advantages of a simple structure, environmentally friendly materials, low cost, and simple fabrication process. These features are of considerable significance for the development of green energy harvesting devices.
Plasmon-Enhanced Ultraviolet Luminescence in Colloid Solutions and Nanostructures Based on Aluminum and ZnO Nanoparticles
Authors: Lizunova Anna A. , Malo Dana , Guzatov Dmitry V. , Vlasov Ivan S. , Kameneva Ekaterina I. , Shuklov Ivan A. , Urazov Maxim N. , Ramanenka Andrei A. , Ivanov Victor V.
Published: November 2022

Aluminum nanoparticles attract scientific interest as a promising low-cost material with strong plasmon resonance in the ultraviolet region, which can be used in various fields of photonics. In this paper, for the first time, ultraviolet luminescence of zinc oxide nanoparticles in colloid solutions and nanostructure films in the presence of plasmonic aluminum nanoparticles 60 nm in size with a metal core and an aluminum oxide shell were studied. Mixture colloids of ZnO and Al nanoparticles in isopropyl alcohol solution with concentrations from 0.022 to 0.44 g/L and 0.057 to 0.00285 g/L, correspondingly, were investigated. The enhancement of up to 300% of ZnO emission at 377 nm in colloids mixtures with metal nanoparticles due to formation of Al-ZnO complex agglomerates was achieved. Plasmon nanostructures with different configurations of layers, such as Al on the surface of ZnO, ZnO on Al, sandwich-like structure and samples prepared from a colloidal mixture of ZnO and Al nanoparticles, were fabricated by microplotter printing. We demonstrated that photoluminescence can be boosted 2.4-fold in nanostructures prepared from a colloidal mixture of ZnO and Al nanoparticles, whereas the sandwich-like structure gave only 1.1 times the amplification of luminescence. Calculated theoretical models of photoluminescence enhancement of ideal and weak emitters near aluminum nanoparticles of different sizes showed comparable results with the obtained experimental data.
Eco-Friendly Green Synthesis of Rubropunctatin Functionalized Silver Nanoparticles and Evaluation of Antibacterial Activity
Authors: Lin Guibin , Zhao Chenhui , Liao Wenqiang , Yang Jianmin , Zheng Yunquan
Published: November 2022

In order to solve the problems of rubropunctatin insoluble in water and its low bioavailability, and explore the synthesis method of green silver nanoparticles, rubropunctatin was used as reducing agent and blocking agent, rubropunctatin-functionalized silver nanoparticles (R-AgNPs) were successfully synthesized. The distinctive absorption peak at 410 nm confirmed the formation of R-AgNPs. Zeta potential measurement showed excellent stability of R-AgNPs with negative values of −29.81 ± 0.37 mV. The results of TEM and XRD showed that the prepared R-AgNPs were round, well dispersed and crystallized with average particle size of 13.54 ± 0.42 nm. FT-IR and XPS studies show that functional groups are involved in R-AgNPs synthesis. The antibacterial activity of R-AgNPs was compared with commercial silver nanoparticles (AgNPs) by microdilution method. The results showed that R-AgNPs (MIC 7.81 μg/mL) has stronger antibacterial activity than commercial AgNPs. The bacteria morphology was observed by the live and dead (SYTO 9/PI) staining assay and SEM showed that the antibacterial effect of R-AgNPs was caused by the destruction of the bacterial cell membrane. Cytotoxicity of rubropunctatin-functionalized silver nanoparticles and commercial silver nanoparticles on mouse fibroblast 3T3 cells was assessed by CCK-8 assay. The results showed that the toxicity of rubropunctatin-functionalized silver nanoparticles to 3T3 cells was lower than that of commercial silver nanoparticles. In summary, synthesis of silver nanoparticles using rubropunctatin is a green synthesis method, and R-AgNPs is a potential antibacterial agent.
A Review on the Application of Cobalt-Based Nanomaterials in Supercapacitors
Authors: Yang Lin , Zhu Qinghan , Yang Ke , Xu Xinkai , Huang Jingchun , Chen Hongfeng , Wang Haiwang
Published: November 2022

Among many electrode materials, cobalt-based nanomaterials are widely used in supercapacitors because of their high natural abundance, good electrical conductivity, and high specific capacitance. However, there are still some difficulties to overcome, including poor structural stability and low power density. This paper summarizes the research progress of cobalt-based nanomaterials (cobalt oxide, cobalt hydroxide, cobalt-containing ternary metal oxides, etc.) as electrode materials for supercapacitors in recent years and discusses the preparation methods and properties of the materials. Notably, the focus of this paper is on the strategies to improve the electrochemical properties of these materials. We show that the performance of cobalt-based nanomaterials can be improved by designing their morphologies and, among the many morphologies, the mesoporous structure plays a major role. This is because mesoporous structures can mitigate volume changes and improve the performance of pseudo capacitance. This review is dedicated to the study of several cobalt-based nanomaterials in supercapacitors, and we hope that future scholars will make new breakthroughs in morphology design.
Coal-Based Semicoke-Derived Carbon Anode Materials with Tunable Microcrystalline Structure for Fast Lithium-Ion Storage
Authors: Liu Yaxiong , Guo Xing , Tian Xiaodong , Liu Zhanjun
Published: November 2022

Fast charging capability is highly desired for new generation lithium-ion batteries used in consumer-grade electronic devices and electric vehicles. However, currently used anodes suffer from sluggish ion kinetics due to limited interlayer distance. Herein, the coal-based semicoke was chosen as precursor to prepare cost-effective carbon anodes with high-rate performance through a facile pyrolytic strategy. The evolution of microstructure and its effect on electrochemical performance are entirely studied. The results show that large number of short-ordered defective structures are generated due to the occurrence of turbostatic-like structures when pyrolyzed at 900 °C, which are propitious to large interlayer distance and developed porous structure. High accessible surface area and large interlayer spacing with short-ordered defective domains endow the sample treated at 900 °C under argon (A900) with accelerated ion dynamics and enhanced ion adsorption dominated surface-induced capacitive processes. As a result, A900 delivers high capacity (331.1 mAh g−1 at 0.1 A g−1) and long life expectancy (94.8% after 1000 cycles at 1 A g−1) as well as good rate capability (153.2 mAh g−1 at 5 A g−1). This work opens a scalable avenue to fabricating cost-effective, high-rate, and long cycling life carbon anodes.
The Clinical Utility of Leukoaraiosis as a Prognostic Indicator in Ischemic Stroke Patients
Authors: Christidi Foteini , Tsiptsios Dimitrios , Sousanidou Anastasia , Karamanidis Stefanos , Kitmeridou Sofia , Karatzetzou Stella , Aitsidou Souzana , Tsamakis Konstantinos , Psatha Evlampia A. , Karavasilis Efstratios , Kokkotis Christos , Aggelousis Nikolaos , Vadikolias Konstantinos
Published: November 2022

Stroke constitutes a major cause of functional disability with increasing prevalence among adult individuals. Thus, it is of great importance for both clinicians and stroke survivors to be provided with a timely and accurate prognostication of functional outcome. A great number of biomarkers capable of yielding useful information regarding stroke patients’ recovery propensity have been evaluated so far with leukoaraiosis being among them. Literature research of two databases (MEDLINE and Scopus) was conducted to identify all relevant studies published between 1 January 2012 and 25 June 2022 that dealt with the clinical utility of a current leukoaraiosis as a prognostic indicator following stroke. Only full-text articles published in English language were included. Forty-nine articles have been traced and are included in the present review. Our findings highlight the prognostic value of leukoaraiosis in an acute stroke setting. The assessment of leukoaraiosis with visual rating scales in CT/MRI imaging appears to be able to reliably provide important insight into the recovery potential of stroke survivors, thus significantly enhancing stroke management. Yielding additional information regarding both short- and long-term functional outcome, motor recovery capacity, hemorrhagic transformation, as well as early neurological deterioration following stroke, leukoaraiosis may serve as a valuable prognostic marker poststroke. Thus, leukoaraiosis represents a powerful prognostic tool, the clinical implementation of which is expected to significantly facilitate the individualized management of stroke patients.
Age-Related Sex Differences in Glucose Tolerance by 75 g Oral Glucose Tolerance Test in Japanese
Authors: Yoshida Akihiro , Kimura Takao , Tsunekawa Katsuhiko , Shoho Yoshifumi , Yanagawa Yoshimaro , Araki Osamu , Aoki Tomoyuki , Ogiwara Takayuki , Murakami Masami
Published: November 2022

To elucidate the age-related sex difference in glucose tolerance, we conducted 75 g oral glucose tolerance tests in 1156 participants. Participants were divided into four groups, namely, young (22–29) males, young females, middle-aged (>50) males, and middle-aged females. According to the Japanese Clinical Practice Guideline for Diabetes 2019, the prevalence of normal glucose tolerance (NGT) was significantly lower in middle-aged than in young participants. The prevalence of high-normal fasting plasma glucose (FPG) was higher, and NGT was lower in young males (high-normal FPG 15.2%, NGT 82.0%) than young females (high-FPG 3.9%, NGT 94.3%). Combined glucose intolerance (CGI) was higher and NGT was lower in middle-aged males (CGI 10.2%, NGT 25.2%) than in middle-aged females (CGI 3.3%, NGT 39.8%). FPG and body mass index (BMI) were the lowest and Homeostatic model assessment beta cell function (HOMA-β) was the highest in young females, followed by young males, middle-aged females, and middle-aged males. Multiple linear regression analysis revealed that BMI weakly correlated with HOMA-β and Matsuda index in all subjects except young females. The superior glucose tolerance in females was apparent in young, but attenuated in middle-aged females. The differences are due to the higher insulin secretion potential and lower BMI in young females.
Reducing Liver Cancer Risk through Dietary Change: Positive Results from a Community-Based Educational Initiative in Three Racial/Ethnic Groups
Authors: Zhu Lin , Kim Ellen Jaeseon , González Evelyn , Fraser Marilyn A. , Zhu Steven , Rubio-Torio Nathaly , Ma Grace X. , Yeh Ming-Chin , Tan Yin
Published: November 2022

Dietary behaviors and alcohol consumption have been linked to liver disease and liver cancer. So far, most of the liver cancer awareness campaigns and behavioral interventions have focused on preventive behaviors such as screening and vaccination uptake, while few incorporated dietary aspects of liver cancer prevention. We implemented a community-based education initiative for liver cancer prevention among the African, Asian, and Hispanic populations within the Greater Philadelphia and metropolitan New York City areas. Data from the baseline and the 6-month follow-up surveys were used for the assessment of changes in dietary behaviors and alcohol consumption among participants. In total, we recruited 578 participants through community-/faith-based organizations to participate in the educational workshops. The study sample included 344 participants who completed both baseline and follow-up survey. The Hispanic subgroup was the only one that saw an overall significant change in dietary behaviors, with the Mediterranean dietary score increasing significantly from 30.000 at baseline survey to 31.187 at 6-month follow-up assessment (p < 0.05), indicating a trend towards healthier dietary habit. In the African Americans participants, the consumption scores of fruits and poultry increased significantly, while vegetables and red meats decreased. In Asian Americans, the consumption of non-refined cereals, red meats, and dairy products decreased. Alcohol consumption decreased significantly among Hispanics while it did not change significantly among the other two communities. This community-based educational initiative generated different impacts in the three populations, further highlighting the needs for more targeted, culturally tailored efforts in health promotion among these underprivileged communities.
Modulatory Effect of Chlorogenic Acid and Coffee Extracts on Wnt/β-Catenin Pathway in Colorectal Cancer Cells
Authors: Villota Hernán , Santa-González Gloria A. , Uribe Diego , Henao Isabel Cristina , Arroyave-Ospina Johanna C. , Barrera-Causil Carlos J. , Pedroza-Díaz Johanna
Published: November 2022

The Wnt/β-Catenin pathway alterations present in colorectal cancer (CRC) are of special interest in the development of new therapeutic strategies to impact carcinogenesis and the progression of CRC. In this context, different polyphenols present in natural products have been reported to have modulatory effects against the Wnt pathway in CRC. In this study, we evaluate the effect of two polyphenol-rich coffee extracts and chlorogenic acid (CGA) against SW480 and HT-29 CRC cells. This involved the use of MTT and SRB techniques for cell viability; wound healing and invasion assay for the evaluation of the migration and invasion process; T cell factor (TCF) reporter plasmid for the evaluation of transciption factor (TCF) transcriptional activity; polymerase chain reaction (PCR) of target genes and confocal fluorescence microscopy for β-Catenin and E-Cadherin protein fluorescence levels; and subcellular localization. Our results showed a potential modulatory effect of the Wnt pathway on CRC cells, and we observed a reduction in the transcriptional activity of β-catenin. All the results were prominent in SW480 cells, where the Wnt pathway deregulation has more relevance and implies a constitutive activation of the signaling pathway. These results establish a starting point for the discovery of a mechanism of action associated with these effects and corroborate the anticancer potential of polyphenols present in coffee, which could be explored as chemopreventive molecules or as adjunctive therapy in CRC.
Dietary Intake and the Neighbourhood Environment in the BC Generations Project
Authors: Murphy Rachel A. , Kuczynski Gabriela , Bhatti Parveen , Dummer Trevor J. B.
Published: November 2022

Poor diet is a major risk factor for many chronic diseases including cancer. Understanding broader contextual factors that influence dietary intake is important for making tangible progress towards improving diet at the population level. This study investigated neighbourhood social and built environment factors and fruit and vegetable intake among ~28,000 adults aged 35–69 years within the BC Generations Project. Daily fruit and vegetable intake was categorized according to guidelines (≥5 servings/day vs. <5 servings/day). Geospatial characteristics included walkability, greenness, marginalization, and material and social deprivation, reflecting access to goods and amenities and social relationships. Generalized, linear mixed-effect models adjusted for sociodemographic factors and lifestyle variables were used to estimate the odds ratios (ORs). Participants living in neighbourhoods with greater material deprivation (e.g., OR = 0.77; 95% CI: 0.70–0.86 for very high material deprivation) and very high social deprivation (OR = 0.90; 95% CI: 0.82–0.99) were less likely to meet recommendations for fruit and vegetable consumption relative to those living in areas with very low material deprivation and very low social deprivation, respectively. Relative to participants living in areas with very low greenness, participants living in neighbourhoods with high (OR = 1.10, 95% CI 1.01–1.20) to very high (OR = 1.11, 95% CI 1.01–1.21) greenness were more likely to meet recommendations for fruits and vegetables. These findings highlight the complexity of dietary intake which may be shaped by multiple neighbourhood characteristics.
Trypanosoma cruzi Antigenic Proteins Shared with Acute Lymphoblastic Leukemia and Neuroblastoma
Authors: Eligio García Leticia , Crisóstomo Vázquez María del Pilar , Maravelez Acosta Víctor Alberto , Soria Guerrero Mariana , Cortés Campos Adrián , Jiménez Cardoso Enedina
Published: November 2022

Background. Research studies indicate that immunization with protein extracts of Trypanosoma cruzi, the protozoan parasite that causes Chagas disease, prevents the appearance of tumors in 60% of mice injected with the murine lung carcinoma tumor line. The molecular basis of this process is unknown, although the presence of specific antigens in tumor cells and on the surface of T. cruzi suggests an antiparasitic immune response, with an effective cross-reaction against cancer cells, hence the importance to identify the antigens involved and determine their potential as target cells in anticancer therapy. Aim. This study aimed to determine the presence of antigenic proteins of T. cruzi shared with acute lymphoblastic leukemia and neuroblastoma cells. Material and methods. To achieve this, polyclonal antibodies against T. cruzi were developed in rabbits, and reactivity was determined with protein extracts of acute lymphoblastic leukemia cells and neuroblastoma. The immunodetection of five different strains of T. cruzi against anti-T. cruzi polyclonal antibodies was also performed. Conclusion. The study allows the knowledge of the immunological interactions between cancer and parasites to be expanded and, therefore, contributes to the design of more and better projects that improve the therapeutic strategies applied in oncology.
A Shape-Adaptive Gallic Acid Driven Multifunctional Adhesive Hydrogel Loaded with Scolopin2 for Wound Repair
Authors: Chen Huan , Zheng Tingting , Wu Chenyang , Wang Jinrui , Ye Fan , Cui Mengyao , Sun Shuhui , Zhang Yun , Li Ying , Dong Zhengqi
Published: November 2022

Wound healing is one of the major challenges in the biomedical fields. The conventional single drug treatment has unsatisfactory efficacy, and the drug delivery effectiveness is restricted by the short retention on the wound. Herein, we develop a multifunctional adhesive hydrogel that can realize robust adhesion, transdermal delivery, and combination therapy for wound healing. Multifunctional hydrogels (CS-GA-S) are mixed with chitosan-gallic acid (CS-GA), sodium periodate, and centipede peptide-scolopin2, which slowly releases scolopin2 in the layer of the dermis. The released scolopin2 induces the pro-angiogenesis of skin wounds and enables excellent antibacterial effects. Separately, GA as a natural reactive-oxygen-species-scavenger promotes antioxidation, and further enables excellent antibacterial effects and wet tissue adhesion due to a Schiff base and Michael addition reaction for accelerating wound healing. Once adhered to the wound, the precursor solution becomes both a physically and covalently cross-linked network hydrogel, which has potential advantages for wound healing with ease of use, external environment-isolating, and minimal tissue damage. The therapeutic effects of CS-GA-S on wound healing are demonstrated with the full thickness cutaneous wounds of a mouse model. The significant improvement of wound healing is achieved for mice treated with CS-GA-S. This preparation reduces wound system exposure, prolongs local drug residence time, and improves efficacy. Accordingly, with the incorporation of scolopin2 into the shape-adaptive CS-GA hydrogel, the composite hydrogel possesses multi-functions of mechanical adhesion, drug therapy, and skin wound healing. Overall, such an injectable or sprayable hydrogel plays an effective role in emergency wound treatment with the advantage of convenience and portability.
Recent Synthesis, Characterization, and Pharmacological Evaluation of Multifunctional Hemorphins Containing Non-Natural Amino Acids with Potential Biological Importance
Authors: Todorov Petar , Georgieva Stela , Tchekalarova Jana
Published: November 2022

The endogenous hemorphins are bioactive peptides with activity on opioid receptors. They are extensively studied and summarized in numerous reviews. During the last decade, several research teams have synthesized, characterized, and pharmacologically evaluated synthetic hemorphin analogs containing unusual amino acids, D-amino acids, α-aminophosphonic acids, and their derivatives. The present review summarizes the current studies on short-chain synthetic hemorphin peptide derivates containing non-natural amino acids. This review focuses on the structure–activity relationship analysis, details on specific methods for their characterization, and the advantage of synthetic hemorphin analogs compared to endogenous peptides as potent biologically active compounds with a complex mechanism of action.
Development and Characterisation of a Topical Methyl Salicylate Patch: Effect of Solvents on Adhesion and Skin Permeation
Authors: Yeoh Soo Chin , Loh Poh Lee , Murugaiyah Vikneswaran , Goh Choon Fu
Published: November 2022

The advent of skin patch formulation design and technology has enabled the commercialisation of methyl salicylate (MS) as a topical patch. However, the most fundamental aspect of skin permeation is unknown at present. The study aims to investigate the effect of solvent choice on the skin permeation of MS in a neat solvent system and patch formulation with an emphasis on patch adhesion. MS in six selected solvents (propylene glycol (PG), Transcutol®, isopropyl myristate, Labrasol®, Plurol® oleique CC 497 and Maisine® CC) was characterised and in vitro permeation studies were also performed. An ATR-FTIR analysis on solvent-treated skin was conudcted. Patch formulation was prepared and characterised for adhesion, in vitro drug release and skin permeation studies. The highest MS permeation was found in neat PG over 24 h (~90 μg/cm2) due to its strong skin protein conformation effect. Transcutol® and isopropyl myristate showed better skin deposition and formulation retention, respectively. Nevertheless, PG enhanced the patch adhesion despite having a lower cumulative amount of MS permeated (~80 μg/cm2) as compared with Transcutol® and Maisine® (~110–150 μg/cm2). These two solvents, however, demonstrated better skin deposition and formulation retention but a lower patch adhesion. The unpredictable influence of the solvent on patch adhesion highlights the importance of the trade-off between patch adhesion and skin permeation during formulation design.
Involvement of Transporters in Intestinal Drug–Drug Interactions of Oral Targeted Anticancer Drugs Assessed by Changes in Drug Absorption Time
Authors: Malnoë David , Fardel Olivier , Le Corre Pascal
Published: November 2022

(1) Background: Oral targeted anticancer drugs are victims of presystemic pharmacokinetic drug–drug interactions (DDI). Identification of the nature of these DDIs, i.e., enzyme-based or/and transporter-based, is challenging, since most of these drugs are substrates of intestinal and/or hepatic cytochrome P-450 enzymes and of intestinal membrane transporters. (2) Methods: Variations in mean absorption time (MAT) between DDIs and control period (MAT ratios < 0.77 or >1.30) have been proposed to implicate transporters in DDIs at the intestinal level. This methodology has been applied to a large set of oral targeted anticancer drugs (n = 54, involved in 77 DDI studies), from DDI studies available either in the international literature and/or in publicly accessible FDA files. (3) Results: Significant variations in MAT were evidenced in 33 DDI studies, 12 of which could be explained by modulation of an efflux transporter. In 21 DDI studies, modulation of efflux transporters could not explain the MAT variation, suggesting a possible relevant role of influx transporters in the intestinal absorption. (4) Conclusions: This methodology allows one to suggest the involvement of intestinal transporters in DDIs, and should be used in conjunction with in vitro methodologies to help understanding the origin of DDIs.
Galactosylated Polymer/Gold Nanorods Nanocomposites for Sustained and Pulsed Chemo-Photothermal Treatments of Hepatocarcinoma
Authors: Giammona Gaetano , Drago Salvatore Emanuele , Calabrese Giovanna , Varvarà Paola , Rizzo Maria Giovanna , Mauro Nicolò , Nicotra Giuseppe , Conoci Sabrina , Pitarresi Giovanna
Published: November 2022

In this paper, we propose a rational design of a hybrid nanosystem capable of locally delivering a high amount of hydrophobic anticancer drugs (sorafenib or lenvatinib) and heat (hyperthermia) in a remote-controlled manner. We combined in a unique nanosystem the excellent NIR photothermal conversion of gold nanorods (AuNRs) with the ability of a specially designed galactosylated amphiphilic graft copolymer (PHEA-g-BIB-pButMA-g-PEG-GAL) able to recognize hepatic cells overexpressing the asialoglycoprotein receptor (ASGPR) on their membranes, thus giving rise to a smart composite nanosystem for the NIR-triggered chemo-phototherapy of hepatocarcinoma. In order to allow the internalization of AuNRs in the hydrophobic core of polymeric nanoparticles, AuNRs were coated with a thiolated fatty acid (12-mercaptododecanoic acid). The drug-loaded hybrid nanoparticles were prepared by the nanoprecipitation method, obtaining nanoparticles of about 200 nm and drug loadings of 9.0 and 5.4% w/w for sorafenib and lenvatinib, respectively. These multifunctional nanosystems have shown to convert NIR radiation into heat and release charged drugs in a remote-controlled manner. Then, the biocompatibility and synergistic effects of a chemo-phototherapy combination, as well the receptor-mediated internalization, were evaluated by an in vitro test on HepG2, HuH7, and NHDF. The results indicate that the proposed nanoparticles can be considered to be virtuous candidates for an efficient and selective dual-mode therapy of hepatocarcinoma.
The Synthesis and Preclinical Investigation of Lactosamine-Based Radiopharmaceuticals for the Detection of Galectin-3-Expressing Melanoma Cells
Authors: Gyuricza Barbara , Szűcs Ágnes , Szabó Judit P. , Arató Viktória , Képes Zita , Szücs Dániel , Szikra Dezső , Trencsényi György , Fekete Anikó
Published: November 2022

Given that galectin-3 (Gal-3) is a β-galactoside-binding lectin promoting tumor growth and metastatis, it could be a valuable target for the treatment of Gal-3-expressing neoplasms. An aromatic group introduced to the C-3′ position of lactosamine increased its affinity for Gal-3. Herein, we aimed at developing a radiopharmaceutical for the detection of Gal-3 positive malignancies. To enhance tumor specificity, a heterodimeric radiotracer capable of binding to both Gal-3 and αvβ3 integrin was also synthetized. Arginine-glycine-asparagine (RGD) peptide is the ligand of angiogenesis- and metastasis-associated αvβ3 integrin. Following the synthesis of the chelator-conjugated (2-naphthyl)methylated lactosamine, the obtained compound was applied as a precursor for radiolabeling and was conjugated to the RGD peptide by click reaction as well. Both synthetized precursors were radiolabeled with 68Ga, resulting in high labeling yield (>97). The biological studies were carried out using B16F10 melanoma tumor-bearing C57BL6 mice. High tumor accumulation of both labeled lactosamine derivatives—detected by in vivo PET and ex vivo biodistribution studies—indicated their potential for melanoma detection. However, the heterodimer radiotracer showed high hepatic uptake, while low liver accumulation characterized chelator-conjugated lactosamine, resulting in PET images with excellent contrast. Therefore, this novel carbohydrate-based radiotracer is suitable for the highly selective determination of Gal-3-expressing melanoma cells.
Drug Physicochemical Properties and Capsule Fill Determine Extent of Premature Gastric Release from Enteric Capsules
Authors: Moghrabi Fouad S. , Fadda Hala M.
Published: November 2022

Intrinsically, enteric capsule shells offer several advantages compared to coating of dosage forms with enteric polymers. We undertook a systematic investigation to elucidate capsule-fill parameters that may result in premature gastric drug release from Vcaps® Enteric capsules (Lonza CHI, Morristown, NJ, USA). Four model drugs with different ionization and solubility profiles were investigated: acetaminophen, ketoprofen, trimethoprim and atenolol. Different fill loads, diluents and drug-to-diluent ratios were explored. Enteric capsules were filled with drug or drug and diluent powder mix and underwent USP II dissolution testing using mini-vessels and paddles. Capsules were tested in pH 2 (0.01 M HCl) or pH 4.5 (3.2 × 10−5 M HCl) 200 mL acid media to simulate normal, fasted or hypochlorhydric gastric pH, respectively. Acetaminophen, trimethoprim and atenolol displayed premature gastric drug release from enteric capsules. The extent of premature release was dependent on drug solubility, ionization profile and capsule-fill level. At 100 mg drug-fill level, acetaminophen, trimethoprim and atenolol gave rise to 10.6, 12.2 and 83.1% drug release, respectively, in normal, fasted, gastric fluids. Diffusion layer pH of trimethoprim and atenolol in pH 2 media was determined to be pH 6.3 and 10.3, respectively. Upon increasing capsule-fill load using microcrystalline cellulose as a diluent, a significant reduction in premature gastric release was observed. However, including mannitol as a diluent was only effective at decreasing premature drug release at a low drug-to-diluent ratio. Systematic in vitro screening of enteric capsule fills needs to be conducted to ensure that drug product performance is not compromised.
Bacterial Response to the Surface Aging of PLA Matrices Loaded with Active Compounds
Authors: Fernández-Grajera María , Gallardo-Moreno Amparo María , Luque-Agudo Verónica , González-Martín María Luisa , Hierro-Oliva Margarita
Published: November 2022

The use of active components in biomaterials improves the properties of existing ones and makes it possible to obtain new devices with antibacterial properties that prevent infections after implantation, thus guaranteeing the success of the implant. In this work, cetyltrimethylammonium bromide (CTAB) and magnesium particles were incorporated into polylactic acid (PLA) films to assess the extent to which progressive aging of the new surfaces resists bacterial colonization processes. For this purpose, the films’ surface was characterized by contact angle measurements, ToF-SIMS and AFM, and adhesion, viability and biofilm growth of Staphylococcus epidermidis bacteria on these films were also evaluated. The results show that the inclusion of Mg and CTAB in PLA films changes their surface properties both before and after aging and also modifies bacterial adhesion on the polymer. Complete bactericidal activity is exhibited on non-degraded films and films with CTAB. This antibacterial behavior is maintained after degradation for three months in the case of films containing a higher amount of CTAB.
Scaling-Up an Aqueous Self-Degassing Electrochemically Mediated ATRP in Dispersion for the Preparation of Cellulose–Polymer Composites and Films
Authors: De Bon Francesco , Azevedo Inês M. , Ribeiro Diana C. M. , Rebelo Rafael C. , Coelho Jorge F. J. , Serra Arménio C.
Published: November 2022

Electrochemically mediated atom transfer radical polymerization (eATRP) is developed in dispersion conditions to assist the preparation of cellulose-based films. Self-degassing conditions are achieved by the addition of sodium pyruvate (SP) as a ROS scavenger, while an aluminum counter electrode provides a simplified and more cost-effective electrochemical setup. Different polyacrylamides were grown on a model cellulose substrate which was previously esterified with 2-bromoisobutyrate (-BriB), serving as initiator groups. Small-scale polymerizations (15 mL) provided optimized conditions to pursue the scale-up up to 1000 mL (scale-up factor ~67). Cellulose-poly(N-isopropylacrylamide) was then chosen to prepare the tunable, thermoresponsive, solvent-free, and flexible films through a dissolution/regeneration method. The produced films were characterized by Fourier-transform infrared (FTIR), scanning electron microscopy (SEM), dynamic scanning calorimetry (DSC), and thermogravimetric analysis (TGA).
Influence of Initiator Concentration on the Polymerization Course of Methacrylate Bone Cement
Authors: Przesławski Grzegorz , Szcześniak Katarzyna , Gajewski Piotr , Marcinkowska Agnieszka
Published: November 2022

Background: The amount of oxidant (initiator) and reductant (co-initiator) and their ratio have a significant effect on the properties of polymethacrylate bone cement, such as maximum temperature (Tmax), setting time (tset) and compressive strength (σ). The increase in the initiating system concentration causes an increase in the number of generated radicals and a faster polymerization rate, which shortens the setting time. The influence of the redox-initiating composition on the course of polymerization (rate of polymerization and degree of double bond conversion) and the mechanical properties of bone cement will be analyzed. Methods: Bone cements were synthesized by mixing a powder phase composed of two commercially available methacrylate copolymers (Evonic) and a liquid phase containing 2-hydroxyethyl methacrylate (HEMA), methyl methacrylate (MMA), and triethylene glycol dimethacrylate (D3). As an initiating system, the benzoyl peroxide (BPO) as an oxidant (initiator) in combination with a reducing agent (co-initiator), N,N-dimethylaniline (DMA), was used. Samples were prepared with various amounts of peroxide BPO (0.05%, 0.1%, 0.2%, 0.3%, 0.5% and 0.7% by weight) with a constant amount of reducing agent DMA (0.5 wt.%), and various amounts of DMA (0.25%, 0.35% and 0.5% by weight) with a constant amount of BPO (0.3 wt.%). The polymerization kinetics were studied by differential scanning calorimetry (DSC). Doughing time and compressive strength tests were carried out according to the requirements of the ISO 5833:2002 standard. Results: The increase in polymerization rate was due to the increase in the amount of BPO. In addition, the curing time was shortened, as well as the time needed to achieve the maximum polymerization rate. The final conversion of the double bonds in the studied compositions was in the range 74–100%, and the highest value of this parameter was obtained by the system with 0.3 wt.% of BPO. The doughing times for each BPO concentration were in the range of 90–140 s. The best mechanical properties were obtained for the cement following the initiating system concentrations: 0.3 wt.% of BPO and 0.5 wt.% of DMA. Nevertheless, all tested cements met the requirements of the ISO 5833:2002 standard. Conclusions: Based on the conducted polymerization kinetic studies, the best reaction conditions are provided by an initiating system containing 0.3 wt.% of BPO oxidant (initiator) and 0.5 wt.% of DMA reductant (co-initiator). A decrease in the DMA amount caused a decrease in the polymerization rate and the amount of heat released during the reaction. The change in BPO and DMA concentrations in the composition had little effect on the doughing time of the studied bone cement. The cements showed similar doughing times, ranging from 90–225 s, which is comparable to the bone cement available on the market.