bluuebunny/crossref_metadata_2025 huggingface dataset:
Effects of Side Chain and Peptide Bond Modifications on the Targeting Properties of Stabilized Minigastrin Analogs
Authors: Zavvar Taraneh Sadat , Hörmann Anton Amadeus , Klingler Maximilian , Summer Dominik , Rangger Christine , Desrues Laurence , Castel Hélène , Gandolfo Pierrick , von Guggenberg Elisabeth
Published: February 2023

Different attempts have been made in the past two decades to develop radiolabeled peptide conjugates with enhanced pharmacokinetic properties in order to improve the application for tumor imaging and peptide receptor radionuclide therapy (PRRT), which targets the cholecystokinin-2 receptor (CCK2R). In this paper, the influence of different side chain and peptide bond modifications has been explored for the minigastrin analog DOTA-DGlu-Ala-Tyr-Gly-Trp-(N-Me)Nle-Asp-1Nal-NH2 (DOTA-MGS5). Based on this lead structure, five new derivatives were synthesized for radiolabeling with trivalent radiometals. Different chemical and biological properties of the new derivatives were analyzed. Receptor interaction of the peptide derivatives and cell internalization of the radiolabeled peptides were studied in A431-CCK2R cells. The stability of the radiolabeled peptides in vivo was investigated using BALB/c mice. Tumor targeting of all 111In-labeled peptide conjugates, and of a selected compound radiolabeled with gallium-68 and lutetium-177, was evaluated in BALB/c nude mice xenografted with A431-CCK2R and A431-mock cells. All 111In-labeled conjugates, except [111In]In-DOTA-[Phe8]MGS5, showed a high resistance against enzymatic degradation. A high receptor affinity with IC50 values in the low nanomolar range was confirmed for most of the peptide derivatives. The specific cell internalization over time was 35.3–47.3% for all radiopeptides 4 h after incubation. Only [111In]In-DOTA-MGS5[NHCH3] exhibited a lower cell internalization of 6.6 ± 2.8%. An overall improved resistance against enzymatic degradation was confirmed in vivo. Of the radiopeptides studied, [111In]In-DOTA-[(N-Me)1Nal8]MGS5 showed the most promising targeting properties, with significantly increased accumulation of radioactivity in A431-CCK2R xenografts (48.1 ± 9.2% IA/g) and reduced accumulation of radioactivity in stomach (4.2 ± 0.5% IA/g). However, in comparison with DOTA-MGS5, a higher influence on the targeting properties was observed for the change of radiometal, resulting in a tumor uptake of 15.67 ± 2.21% IA/g for [68Ga]Ga-DOTA-[(N-Me)1Nal8]MGS5 and 35.13 ± 6.32% IA/g for [177Lu]Lu-DOTA-[(N-Me)1Nal8]MGS5.
A Multifunctional Hybrid Nanocarrier for Non-Invasive siRNA Delivery to the Retina
Authors: Nishida Shogo , Takashima Yuuki , Udagawa Ryotaro , Ibaraki Hisako , Seta Yasuo , Ishihara Hiroshi
Published: February 2023

Drug therapy for retinal diseases (e.g., age-related macular degeneration, the leading cause of blindness) is generally performed by invasive intravitreal injection because of poor drug delivery caused by the blood–retinal barrier (BRB). This study aimed to develop a nanocarrier for the non-invasive delivery of small interfering RNA (siRNA) to the posterior segment of the eye (i.e., the retina) by eyedrops. To this end, we prepared a hybrid nanocarrier based on a multifunctional peptide and liposomes, and the composition was optimized. A cytoplasm-responsive stearylated peptide (STR-CH2R4H2C) was used as the multifunctional peptide because of its superior ability to enhance the complexation, cell permeation, and intracellular dynamics of siRNA. By adding STR-CH2R4H2C to the surface of liposomes, intracellular uptake increased regardless of the liposome surface charge. The STR-CH2R4H2C-modified cationic nanocarrier demonstrated significant siRNA transfection efficiency with no cytotoxicity, enhanced siRNA release from endosomes, and effectively suppressed vascular endothelial growth factor expression in rat retinal pigment epithelium cells. The 2.0 mol% STR-CH2R4H2C-modified cationic nanocarrier enhanced intraocular migration into the retina after instillation into rat eyes.
Dual Effect of Chemo-PDT with Tumor Targeting Nanoparticles Containing iRGD Peptide
Authors: Kim Gye Lim , Park Byeongmin , Jang Eun Hyang , Gu Jaeun , Seo Seo Ra , Cheung Hyein , Lee Hyo Jung , Lee Sangmin , Kim Jong-Ho
Published: February 2023

Nanotechnology, including self-aggregated nanoparticles, has shown high effectiveness in the treatment of solid tumors. To overcome the limitations of conventional cancer therapies and promote therapeutic efficacy, a combination of PDT and chemotherapy can be considered an effective strategy for cancer treatment. This study presents the development of tumor-targeting polysialic acid (PSA) nanoparticles for chemo-PDT to increase the cellular uptake and cytotoxic effect in cancer cells. Chlorin e6 (Ce6), a photosensitizer, and the iRGD peptide (sequence; cCRGDKGPDC) were conjugated to the amine of N-deacetylated PSA. They generate reactive oxygen species (ROS), especially singlet oxygen (1O2), and target integrin αvβ3 on the cancer cell surface. To offer a chemotherapeutic effect, doxorubicin (Dox) was assembled into the core of hydrophobically modified PSA by connecting it with Ce6; this was followed by its sustained release from the nanoparticles. These nanoparticles are able to generate ROS under 633 nm visible-light irradiation, resulting in the strong cytotoxicity of Dox with anticancer effects in HCT116 cells. PSA nanoparticles with the dual effect of chemo-PDT improve conventional PDT, which has a poor ability to deliver photosensitizers to cancer cells. Using their combination with Dox chemotherapy, rapid removal of cancer cells can be expected.
Quality by Design as a Tool in the Optimisation of Nanoparticle Preparation—A Case Study of PLGA Nanoparticles
Authors: Struzek Anna-Maria , Scherließ Regina
Published: February 2023

Nanoparticles can be used as drug carriers in various applications (e.g., in pulmonary drug delivery and mucosal vaccination). For further investigations, such as drug release studies, as well as for cell and tissue targeting, particles with defined properties are needed. The purpose of the study was to show a multi-step systematic method utilising quality by design to ensure the quality of ovalbumin loaded polylactic-co-glycolic acid nanoparticles (OVA-PLGA-NP), which can be delivered to the lung, and to gain knowledge of the preparation method (double-emulsion solvent evaporation method) in an early development process. Within a definitive screening design, several process parameters (OVA, PLGA and stabiliser concentrations, stirring time and stirring speed of inner emulsion and stirring time and stirring speed of double emulsion) were varied to analyse their impact on resulting properties (z-average, PDI, loading efficiency and loading capacity). The results showed that the preparation of the inner emulsion mainly influenced the drug loading, while the parameters of the second emulsifying step controlled the size. Then a central composite response surface design was used to achieve a predictable OVA-PLGA-NP with an average particle size of 700 nm and high drug-loading. This also enabled the demonstration of curvature and interaction of the stabiliser and the PLGA concentration.
Intranasal Delivery of a Silymarin Loaded Microemulsion for the Effective Treatment of Parkinson’s Disease in Rats: Formulation, Optimization, Characterization, and In Vivo Evaluation
Authors: Imran Mohd , Almehmadi Mazen , Alsaiari Ahad Amer , Kamal Mehnaz , Alshammari Mohammed Kanan , Alzahrani Mohammed Omar , Almaysari Faisal Khaled , Alzahrani Abdulrahman Omar , Elkerdasy Ahmed Faraj , Singh Sachin Kumar
Published: February 2023

A mucoadhesive microemulsion of lipophilic silymarin (SLMMME) was developed to treat Parkinson’s disease (PD). Optimization of the SLM microemulsion (ME) was performed using Central Composite Design (CCD). The composition of oil, surfactant, co-surfactant, and water was varied, as per the design, to optimize their ratio and achieve desirable droplet size, zeta potential, and drug loading. The droplet size, zeta potential, and drug loading of optimized SLMME were 61.26 ± 3.65 nm, −24.26 ± 0.2 mV, and 97.28 ± 4.87%, respectively. With the addition of chitosan, the droplet size and zeta potential of the developed ME were both improved considerably. In vitro cell toxicity investigations on a neuroblastoma cell line confirmed that SLMMME was non-toxic and harmless. In comparison to ME and drug solution, mucoadhesive ME had the most flow through sheep nasal mucosa. Further, the in vitro release showed significantly higher drug release, and diffusion of the SLM loaded in MEs than that of the silymarin solution (SLMS). The assessment of behavioral and biochemical parameters, as well as inflammatory markers, showed significant (p < 0.05) amelioration in their level, confirming the significant improvement in neuroprotection in rats treated with SLMMME compared to rats treated with naïve SLM.
HS 3D-SeboSkin Model Enables the Preclinical Exploration of Therapeutic Candidates for Hidradenitis Suppurativa/Acne Inversa
Authors: Zouboulis Christos C. , Hou Xiaoxiao , von Waldthausen Henriette , Zouboulis Konstantin C. , Hossini Amir M.
Published: February 2023

Despite the rapid development in hidradenitis suppurativa (HS) research, the immediate introduction of potent therapeutic compounds in clinical trials and the lack of definitive outcome measures have led to the discontinuation of potential therapeutic compound studies. HS is a solely human disease, and therefore, the search for preclinical human models has been given priority. The 3D-SeboSkin model, a co-culture of human skin explants with human SZ95 sebocytes as a feeder layer, has been shown to prevent the rapid degeneration of human skin in culture and has been validated for HS preclinical studies. In this work, the HS 3D-SeboSkin model has been employed to characterize cellular and molecular effects of the EMA- and FDA-approved biologic adalimumab. Adalimumab, a tumor necrosis factor-α inhibitor, was shown to target inflammatory cells present in HS lesions, inducing a prominent anti-inflammatory response and contributing to tissue regeneration through a wound healing mechanism. Adalimumab inhibited the lesional tissue expression of TNF-α, IL-3, IL-15, and MCP-3 and downregulated the secretion of IL-1α, IL-5, RANTES, MCP-2, TNF-α, TNF-β, TGF-β, and IFN-γ. In contrast, IL-6 was stimulated. The compound failed to modify abnormal epithelial cell differentiation present in the HS lesions. Patients with Hurley stage II lesions exhibited stronger expression of autophagy proteins in perilesional than in lesional skin. Adalimumab modified the levels of the pro-apoptotic proteins LC3A, LC3B, and p62 in an individual, patient-dependent manner. Finally, adalimumab did not modify the NFκB signal proteins in SZ95 sebocytes and NHK-19 keratinocytes, used to study this specific pathway. The administration of the validated HS 3D-SeboSkin model in ex vivo studies prior to clinical trials could elucidate the individual pathogenetic targets of therapeutic candidates and, therefore, increase the success rates of clinical studies, minimizing HS drug development costs.
Cell-Membrane-Coated Nanoparticles for Targeted Drug Delivery to the Brain for the Treatment of Neurological Diseases
Authors: Li Jianzhuang , Wei Yanhao , Zhang Chunlin , Bi Rentang , Qiu Yanmei , Li Yanan , Hu Bo
Published: February 2023

Neurological diseases (NDs) are a significant cause of disability and death in the global population. However, effective treatments still need to be improved for most NDs. In recent years, cell-membrane-coated nanoparticles (CMCNPs) as drug-targeting delivery systems have become a research hotspot. Such a membrane-derived, nano drug-delivery system not only contributes to avoiding immune clearance but also endows nanoparticles (NPs) with various cellular and functional mimicries. This review article first provides an overview of the function and mechanism of single/hybrid cell-membrane-derived NPs. Then, we highlight the application and safety of CMCNPs in NDs. Finally, we discuss the challenges and opportunities in the field.
The Effect of Curcumin-Loaded Glucan Nanoparticles on Immune Cells: Size as a Critical Quality Attribute
Authors: Colaço Mariana , Roquito Tiago , Costa João Panão , Cruz Maria Teresa , Borges Olga
Published: February 2023

Curcumin is known for its multiple health benefits, largely due to its antioxidant and anti-inflammatory properties. It has been extensively studied as a therapeutic agent, however, it does not have good clinical efficacy due to its poor water solubility and bioavailability. Despite accepting the encapsulation of this compound in polymeric particles as one of the most promising strategies to increase its therapeutic value, these nanoparticles have fallen short of expectations due to a lack of assessment of their possible adverse effects on the immune system. Therefore, in this work, we report on a new method to encapsulate curcumin into glucan nanoparticles and their effects on cells of the immune system were evaluated. Two different-sized curcumin-loaded glucan NPs (GluCur 100 and GluCur 380) were produced, each with an encapsulation efficiency close to 100%, and were characterized regarding their size distribution, surface properties, and morphology. The results revealed the greatest hemolytic effect and cytotoxicity for the smallest particles (100 nm) tested in human PBMCs and RAW 264.7 cells. Although GluCur 380 NPs showed a weaker ROS production, they were able to inhibit the production of NO by macrophages. Furthermore, we found that the coagulation time was not affected by both sized-particles as well as platelet function. Additionally, both nanoparticles induced lymphocyte proliferation and TNF-α secretion by Mo-DCs. In conclusion, this report emphasizes the importance of the immunotoxicity assessment and how this is dependent on the intrinsic properties of nanomaterials, hopefully contributing to increasing the safety of nanomedicines.
A Gelatin Methacrylate-Based Hydrogel as a Potential Bioink for 3D Bioprinting and Neuronal Differentiation
Authors: Cruz Elisa Marozzi , Machado Lucas Simões , Zamproni Laura Nicoleti , Bim Larissa Valdemarin , Ferreira Paula Scanavez , Pinto Leonardo Alves , Pessan Luiz Antonio , Backes Eduardo Henrique , Porcionatto Marimélia Aparecida
Published: February 2023

Neuronal loss is the ultimate pathophysiologic event in central nervous system (CNS) diseases and replacing these neurons is one of the most significant challenges in regenerative medicine. Providing a suitable microenvironment for new neuron engraftment, proliferation, and synapse formation is a primary goal for 3D bioprinting. Among the various biomaterials, gelatin methacrylate (GelMA) stands out due to its Arg-Gly-Asp (RGD) domains, which assure its biocompatibility and degradation under physiological conditions. This work aimed to produce different GelMA-based bioink compositions, verify their mechanical and biological properties, and evaluate their ability to support neurogenesis. We evaluated four different GelMA-based bioink compositions; however, when it came to their biological properties, incorporating extracellular matrix components, such as GeltrexTM, was essential to ensure human neuroprogenitor cell viability. Finally, GeltrexTM: 8% GelMA (1:1) bioink efficiently maintained human neuroprogenitor cell stemness and supported neuronal differentiation. Interestingly, this bioink composition provides a suitable environment for murine astrocytes to de-differentiate into neural stem cells and give rise to MAP2-positive cells.
Ball-Milling Preparation of the Drug–Drug Solid Form of Pioglitazone-Rosuvastatin at Different Molar Ratios: Characterization and Intrinsic Dissolution Rates Evaluation
Authors: Muñoz Tecocoatzi M. Fernanda , Páez-Franco José C. , Rubio-Carrasco Kenneth , Núñez-Pineda Alejandra , Dorazco-González Alejandro , Fuentes-Noriega Inés , Vilchis-Néstor Alfredo R. , Olvera Lilian I. , Morales-Morales David , Germán-Acacio Juan Manuel
Published: February 2023

Ball-milling using neat grinding (NG) or liquid-assisted grinding (LAG) by varying the polarity of the solvents allowed access to various drug–drug solid forms of pioglitazone hydrochloride (PGZ·HCl) and rosuvastatin calcium (RSV). Using NG, the coamorphous form was formed from the reaction of pioglitazone hydrochloride (PGZ·HCl) and rosuvastatin calcium (RSV) in a 2:1 molar ratio. The formation of the expected coamorphous salt could not be corroborated by FT-IR, but DSC data showed that it was indeed a single-phase amorphous mixture. By varying the molar ratios of the reactants, either keeping PGZ·HCl constant and varying RSV or vice versa, another coamorphous form was obtained when a 1:1 molar ratio was employed. In the case of the other outcomes, it was observed that they were a mixture of solid forms coexisting simultaneously with the coamorphous forms (1:1 or 2:1) together with the drug that was in excess. When RSV was in excess, it was in an amorphous form. In the case of PGZ·HCl, it was found in a semicrystalline form. The intrinsic dissolution rates (IDRs) of the solid forms of PGZ·HCl-RSV in stoichiometric ratios (1:1, 2:1, 1:4, 6:1, and 1:10) were evaluated. Interestingly, a synchronized release of both drugs in the dissolution medium was observed. In the case of the release of RSV, there were no improvements in the dissolution profiles, because the acidic media caused the formation of degradation products, limiting any probable modification in the dissolution processes. However, the coamorphous 2:1 form exhibited an improvement of 1.03 times with respect to pure PGZ·HCl. It is proposed that the modification of the dissolution process of the coamorphous 2:1 form was limited by changes in the pH of the media as RSV consumes protons from the media due to degradation processes.
Curcumin-Loaded Platelet Membrane Bioinspired Chitosan-Modified Liposome for Effective Cancer Therapy
Authors: Wan Shengli , Fan Qingze , Wu Yuesong , Zhang Jingqing , Qiao Gan , Jiang Nan , Yang Jie , Liu Yuanzhi , Li Jingyan , Chiampanichayakul Sawitree , Tima Singkome , Tong Fei , Anuchapreeda Songyot , Wu Jianming
Published: February 2023

Cancer is a serious threat to human health, and chemotherapy for cancer is limited by severe side effects. Curcumin (CUR) is a commonly used natural product for antitumor treatment without safety concerns. However, low bioavailability and poor tumor accumulation are great obstacles for its clinical application. Our previous research has demonstrated that platelet membrane-camouflaged nanoparticles can efficiently ameliorate the in vivo kinetic characteristics and enhance the tumor affinity of payloads. Nevertheless, the antitumor efficiency of this formulation still needs to be thoroughly investigated, and its drug release behavior is limited. Herein, CUR-loaded platelet membrane bioinspired chitosan-modified liposome (PCLP-CUR) was constructed to improve CUR release. PCLP-CUR was shown to have long retention time, improved bioavailability, strong tumor targeting capacity and effective cellular uptake. The incorporation of chitosan enabled PCLP-CUR to release cargoes quickly under mild acidic tumor conditions, leading to more complete drug release and favoring subsequent treatment. Both in vitro and in vivo investigations showed that PCLP-CUR could significantly enhance the anticancer efficacy of CUR with minimal side effects through biomimetic membrane and chitosan modification. In summary, this developed delivery system can provide a promising strategy for tumor-targeting therapy and phytochemical delivery.
Lensless Imaging via Blind Ptychography Modulation and Wavefront Separation
Authors: Xu Cheng , Pang Hui , Cao Axiu , Deng Qiling , Hu Song , Yang Huajun
Published: February 2023

A novel lensless imaging approach based on ptychography and wavefront separation is proposed in this paper, which was characterized by rapid convergence and high-quality imaging. In this method, an amplitude modulator was inserted between the light source and the sample for light wave modulation. By laterally translating this unknown modulator to different positions, we acquired a sequence of modulated intensity images for quantitative object recovery. In addition, to effectively separate the object and modulator wavefront, a couple of diffraction patterns without modulation were recorded. Optical experiments were performed to verify the feasibility of our approach by testing a resolution plate, a phase object, and an agaricus cell.
CuO Nanoparticle-Mediated Seed Priming Improves Physio-Biochemical and Enzymatic Activities of Brassica juncea
Authors: Faraz Ahmad , Faizan Mohammad , D. Rajput Vishnu , Minkina Tatiana , Hayat Shamsul , Faisal Mohammad , Alatar Abdulrahman A. , Abdel-Salam Eslam M.
Published: February 2023

The use of nanoparticles (NPs) in agricultural fields has risen to a level where people are considering NPs as an alternative to commercial fertilizers. The input of copper oxide NPs (CuO NPs) as seed primers was investigated in this study, and the growth indices of Brassica juncea such as phenotypic parameters, photosynthetic attributes, and biochemical parameters were measured during maximum vegetative growth stage, i.e., at 45 days after sowing. Surface sterilized seeds were soaked in varying concentrations (0, 2, 4, 8 and 16 mg/L) of CuO NPs for 15, 30, and/or 45 min. After those priming periods, the seeds were planted in pots and allowed to grow naturally. Among the different tested concentrations of CuO NPs, 4 mg/L of CuO NPs for 30 min seed priming proved to be best, and considerably increased the, shoot length (30%), root length (27%), net photosynthetic rate (30%), internal CO2 concentration (28%), and proline content (41%). Besides, the performance of the antioxidant enzymes, viz, superoxide dismutase, catalase, peroxidase, and biochemical parameters such as nitrate reductase and carbonic anhydrase were also increased by several folds after the application of CuO NPs in B. juncea. The present study suggests that CuO NPs can be effectively used to increase the performance of B. juncea and may also be suitable for testing on other crop species.
Cytogenetic Characterization and Metabolomic Differences of Full-Sib Progenies of Saccharum spp.
Authors: Wang Yi , Li Ru , Chen Baoshan
Published: February 2023

Sugarcane smut is a worldwide fungal disease. Disease resistance breeding is the most economical and effective measure to prevent and control sugarcane smut. The cytogenetic characteristics and metabolomic differences of sugarcane F1s are closely related to disease resistance. Zhongzhe 1 and G160 sugarcane from the same parents (ROC25 and Yunzhe89-7) were used; the plants were grown in accordance with the barrel method. When the seedlings had 4–5 leaves, genomic in situ hybridization (GISH) was performed; digoxigenin (DIG)-labeled female parental (ROC25)DNA and biotin-labeled male parental (Yunzhe89-7) DNA were used as probes, and the karyotypes of two hybrids were analyzed. The new sugarcane smut-resistant variety (Zhongzhe 1) and the susceptible variety (G160) derived from the same parent were analyzed via gas chromatography—mass spectrometry technology (GC–MS) to compare the metabolomic differences between them. GISH analysis revealed that the chromosome ploidy number of Zhongzhe 1 sugarcane and G160 sugarcane were 114 and 110, respectively. However, the two contain different numbers of chromosomes from the female (ROC25) and male (Yunzhe89-7) parents. Moreover, 258 significantly changed metabolites were identified in smut-resistant Zhongzhe 1, as compared with the smut-susceptible G160 sugarcane: 56 flavonoids, 52 phenolic acids, 30 lipids, 26 organic acids, 26 amino acids and derivatives, 19 nucleotides and derivatives, 5 alkaloids, 9 terpenoids, and 35 others. Multivariate statistical analysis revealed a distinct difference in metabolic pathways between Zhongzhe 1 sugarcane and G160, and both of these varieties had unique functional metabolites. Differences in chromosome composition may constitute the genetic basis for the difference in resistance to smut disease between Zhongzhe 1 sugarcane and G160 sugarcane, and a high accumulation of flavonoids, lipids, terpenoids and tannins may constitute the basis of resistance to smut disease for the Zhongzhe 1 variety.
Phenolic Profile and Cholinesterase Inhibitory Properties of Three Chilean Altiplano Plants: Clinopodium gilliesii (Benth.) Kuntze [Lamiaceae], Mutisia acuminata Ruiz & Pav. var. hirsuta (Meyen) Cabrera, and Tagetes multiflora (Kunth) [Asteraceae]
Authors: Fernández-Galleguillos Carlos , Jiménez-Aspee Felipe , Mieres-Castro Daniel , Rodríguez-Núñez Yeray A. , Gutiérrez Margarita , Guzmán Luis , Echeverría Javier , Sandoval-Yañez Claudia , Forero-Doria Oscar
Published: February 2023

This research aimed to identify the phenolic profile and composition of the aerial parts of three native species used in traditional medicine in the Andean Altiplano of northern Chile: Clinopodium gilliesii (Benth.) Kuntze [Lamiaceae] (commonly known as Muña-Muña), Mutisia acuminata Ruiz & Pav. var. hirsuta (Meyen) Cabrera [Asteraceae] (commonly known as Chinchircoma), and Tagetes multiflora (Kunth), [Asteraceae] (commonly known as Gracilis), as well as to evaluate their potential inhibitory effects against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Polyphenolic enriched-extracts (PEEs) of the species were prepared and analyzed and the main components were quantified using HPLC-DAD. In total, 30 phenolic compounds were identified and quantified in all species, including simple phenolics, hydroxycinnamic acids, flavan-3-ols (monomers and polymers), flavanones, and flavonols. In addition, other main phenolics from the extracts were tentatively identified by ESI-MS-MS high-resolution analysis. T. multiflora extract showed the greatest anti-AChE and BChE activity in comparison with C. gilliesii and M. acuminata extracts, being the anti-AChE and BChE activity weak in all extracts in comparison to galantamine control. To comprise to better understand the interactions between cholinesterase enzymes and the main phenolics identified in T. multiflora, molecular docking analysis was conducted.
IlAP2, an AP2/ERF Superfamily Gene, Mediates Cadmium Tolerance by Interacting with IlMT2a in Iris lactea var. chinensis
Authors: Wang Zhiquan , Ni Longjie , Liu Liangqin , Yuan Haiyan , Gu Chunsun
Published: February 2023

Cadmium (Cd) stress has a major impact on ecosystems, so it is important to find suitable Cd-tolerant plants while elucidating the responsible molecular mechanism for phytoremediation to manage Cd soil contamination. Iris lactea var. chinensis is an ornamental perennial groundcover plant with strong tolerance to Cd. Previous studies found that IlAP2, an AP2/ERF superfamily gene, may be an interacting partner of the metallothionein gene IlMT2a, which plays a key role in Cd tolerance. To study the role of IlAP2 in regulating Cd tolerance in I. lactea, we analyzed its regulation function and mechanism based on a yeast two-hybrid assay, a bimolecular fluorescence complementation test, quantitative real-time PCR, transgenics and transcriptome sequencing. The results showed that IlAP2 interacts with IlMT2a and may cooperate with other transcription factors to regulate genes involved in signal transduction and plant hormones, leading to reduced Cd toxicity by hindering Cd transport. These findings provide insights into the mechanism of IlAP2-mediated stress responses to Cd and important gene resources for improving plant stress tolerance in phytoremediation.
A Set of Highly Polymorphic Microsatellite Markers for Genetic Diversity Studies in the Genus Origanum
Authors: Alekseeva Marina , Rusanova Mila , Rusanov Krasimir , Atanassov Ivan
Published: February 2023

This study reports the development of a set of 20 highly polymorphic genomic SSR markers which can be used for both cultivar identification and genetic diversity studies in several Origanum species, including some of the most popular ones like Greek oregano (Origanum vulgare L. ssp. hirtum), common oregano (O. vulgare L. ssp. vulgare), and sweet marjoram (O. majorana L.). Analysis of the polymorphic information content (PIC) showed an average PIC value of 0.75 with a minimum of 0.41 and a maximum of 0.89, where 17 of the markers showed PIC values above 0.73. Comparative analysis of the genetic diversity of eight natural populations of Greek oregano in Bulgaria showed that six of the genomic SSR markers revealed significantly higher portions of genetic diversity in the populations, compared to 12 EST SSR markers used in our previous study. We also compared the performance of the same six genomic SSR markers with the results for eight SRAP primer combinations, which showed that SRAP markers captured more precisely the genetic structure in natural populations. The developed highly polymorphic genomic SSR markers can be successfully applied to evaluation of the genetic diversity in the genus Origanum, based on the expected and observed heterozygosity in the populations as well as for easy identification of breeding lines and cultivars based on unique SSR fingerprints.
Biological Activities of the Fruit Essential Oil, Fruit, and Root Extracts of Ferula drudeana Korovin, the Putative Anatolian Ecotype of the Silphion Plant
Authors: Tosun Fatma , Göger Fatih , İşcan Gökalp , Kürkçüoğlu Mine , Kuran Fadıl Kaan , Miski Mahmut
Published: February 2023

In the present study, preliminary phytochemical investigations were performed on the fruit essential oil and antioxidant-rich methanolic extracts of the fruits and roots of Ferula drudeana, the putative Anatolian ecotype of the Silphion plant, to corroborate its medicinal plant potential and identify its unique characteristics amongst other Ferula species. The essential oil from the fruits of the endemic species Ferula drudeana collected from Aksaray was analyzed by GC and GC/MS. The main components of the oil were determined as shyobunone (44.2%) and 6-epishyobunone (12.6%). The essential oil of the fruits and various solvent extracts of the fruits and roots of F. drudeana were evaluated for their antibacterial and anticandidal activity using microbroth dilution methods. The essential oil of the fruits, methanol, and methylene chloride extracts of the fruits and roots showed weak to moderate inhibitory activity against all tested microorganisms with MIC values of 78–2000 µg/mL. However, the petroleum ether extract of the roots showed remarkable inhibitory activity against Candida krusei and Candida utilis with MIC values of 19.5 and 9.75 µg/mL, respectively. Furthermore, all the samples were tested for their antioxidant activities using DPPH• TLC spot testing, online HPLC–ABTS screening, and DPPH/ABTS radical scavenging activity assessment assays. Methanolic extracts of the fruits and roots showed strong antioxidant activity in both systems.
Effects of Biochar on the Fluorescence Spectra of Water-Soluble Organic Matter in Black Soil Profile after Application for Six Years
Authors: Jin Liang , Wei Dan , Li Yan , Zou Guoyuan , Wang Lei , Ding Jianli , Zhang Yitao , Sun Lei , Wang Wei , Ma Xingzhu , Shen Huibo , Wang Yuxian , Wang Junqiang , Lu Xinrui , Sun Yu , Ding Xinying , Li Dahao , Yin Dawei
Published: February 2023

At present, extracting water-soluble organic matter (WSOM) from agricultural organic waste is primarily used to evaluate soil organic matter content in farmland. However, only a few studies have focused on its vertical behavior in the soil profile. This study aims to clarify the three-dimensional fluorescence spectrum characteristics of the WSOM samples in 0–60 cm black soil profile before and after different chemical fertilizer treatments after six years of fertilization. Fluorescence spectroscopy combined with fluorescence and ultraviolet-visible (UV-Vis) spectroscopies are used to divide four different fertilization types: no fertilization (T0), nitrogen phosphorus potassium (NPK) (T1), biochar (T2), biochar + NPK (T3), and biochar + N (T4) in a typical black soil area. The vertical characteristics of WSOC are also analyzed. The results showed that after six years of nitrogen application, T2 had a significant effect on the fluorescence intensity of Zone II (decreasing by 9.6% in the 0–20 cm soil layer) and Zone V (increasing by 8.5% in the 0–20 cm soil layer). The fluorescent components identified in each treatment group include ultraviolet radiation A humic acid-like substances (C1), ultraviolet radiation C humic acid-like substances (C2), and tryptophan-like substance (C3). As compared with the land with T1, the content of C2 in the 20–60 cm soil layer with T2 was lower, while that of C2 in the surface and subsoil with T3 was higher. In addiiton, there were no significant differences in the contents of C1, C2, and C3 by comparing the soils applied with T3 and T4, respectively. The composition of soil WSOM was found to be significantly influenced by the addition of a mixture of biochar and chemical fertilizers. The addition of biochar alone exerted a positive effect on the humification process in the surface soil (0–10 cm). NPK treatment could stimulate biological activity by increasing biological index values in deeper soil layers (40–50 cm). Nitrogen is the sovereign factor that improves the synergism effect of chemical fertilizer and biochar during the humification process. According to the UV-Vis spectrum and optical index, soil WSOM originates from land and microorganisms. This study reveals the dynamics of WSOC in the 0–60 cm soil layer and the biogeochemical effect of BC fertilizer treatment on the agricultural soil ecosystem.
Design, Analysis, and 3D Printing of a Patient-Specific Polyetheretherketone Implant for the Reconstruction of Zygomatic Deformities
Authors: Moiduddin Khaja , Mian Syed Hammad , Umer Usama , Alkhalefah Hisham , Ahmed Faraz , Hashmi Faraz Hussain
Published: February 2023

The reconstruction of craniomaxillofacial deformities, especially zygomatic bone repair, can be exigent due to the complex anatomical structure and the sensitivity of the crucial organs involved. The need to reconstruct the zygomatic bone in the most precise way is of crucial importance for enhancing the patient outcomes and health care-related quality of life (HRQL). Autogenous bone grafts, despite being the gold standard, do not match bone forms, have limited donor sites and bone volume, and can induce substantial surgical site morbidity, which may lead to adverse outcomes. The goal of this study is to provide an integrated approach that includes various processes, from patient scanning to implant manufacture, for the restoration of zygomatic bone abnormalities utilizing Polyetheretherketone (PEEK) material, while retaining adequate aesthetic and facial symmetry. This study takes an integrated approach, including computer-aided implant design using the mirror reconstruction technique, investigating the biomechanical behavior of the implant under loading conditions, and carrying out a fitting accuracy analysis of the PEEK implant fabricated using state-of-the-art additive manufacturing technology. The findings of the biomechanical analysis results reveal the largest stress of approximately 0.89 MPa, which is relatively low in contrast to the material’s yield strength and tensile strength. A high degree of sturdiness in the implant design is provided by the maximum value of strain and deformation, which is also relatively low at roughly 2.2 × 10−4 and 14 µm. This emphasizes the implant’s capability for load resistance and safety under heavy loading. The 3D-printed PEEK implant observed a maximum deviation of 0.4810 mm in the outside direction, suggesting that the aesthetic result or the fitting precision is adequate. The 3D-printed PEEK implant has the potential to supplant the zygoma bone in cases of severe zygomatic reconstructive deformities, while improving the fit, stability, and strength of the implant.
Designed Synthesis of Three-Dimensional Covalent Organic Frameworks: A Mini Review
Authors: Phan Pham Thi , Ta Qui Thanh Hoai , Nguyen Phan Khanh Thinh
Published: February 2023

Covalent organic frameworks are porous crystals of polymers with two categories based on their covalent linkages: layered structures with two dimensions and networks with three-dimensional structures. Three-dimensional covalent organic frameworks are porous, have large surface areas, and have highly ordered structures. Since covalent bonds are responsible for the formation of three-dimensional covalent organic frameworks, their synthesis has been a challenge and different structures are generated during the synthesis. Moreover, initially, their topologies have been limited to dia, ctn, and bor which are formed by the condensation of triangular or linear units with tetrahedral units. There are very few building units available for their synthesis. Finally, the future perspective of 3D COFs has been designated for the future development of three-dimensional covalent organic frameworks.
Influence of DNA Type on the Physicochemical and Biological Properties of Polyplexes Based on Star Polymers Bearing Different Amino Functionalities
Authors: Haladjova Emi , Panseri Silvia , Montesi Monica , Rossi Arianna , Skandalis Athanasios , Pispas Stergios , Rangelov Stanislav
Published: February 2023

The interactions of two star polymers based on poly (2-(dimethylamino)ethyl methacrylate) with different types of nucleic acids are investigated. The star polymers differ only in their functionality to bear protonable amino or permanently charged quaternary ammonium groups, while DNAs of different molar masses, lengths and topologies are used. The main physicochemical parameters of the resulting polyplexes are determined. The influence of the polymer’ functionality and length and topology of the DNA on the structure and properties of the polyelectrolyte complexes is established. The quaternized polymer is characterized by a high binding affinity to DNA and formed strongly positively charged, compact and tight polyplexes. The parent, non-quaternized polymer exhibits an enhanced buffering capacity and weakened polymer/DNA interactions, particularly upon the addition of NaCl, resulting in the formation of less compact and tight polyplexes. The cytotoxic evaluation of the systems indicates that they are sparing with respect to the cell lines studied including osteosarcoma, osteoblast and human adipose-derived mesenchymal stem cells and exhibit good biocompatibility. Transfection experiments reveal that the non-quaternized polymer is effective at transferring DNA into cells, which is attributed to its high buffering capacity, facilitating the endo-lysosomal escape of the polyplex, the loose structure of the latter one and weakened polymer/DNA interactions, benefitting the DNA release.
Dewetting-Induced Hierarchical Self-Assembly of Block Copolymers Templated by Colloidal Crystals
Authors: Kim Dong Hwan , Kwon Hong Gu , Choi Hong Kyoon
Published: February 2023

Recent advances in high-performance flexible electronic devices have increased the demand for more diverse and complex nanofabrication methods; high-resolution, high-efficiency, and low-cost patterning strategies for next-generation devices are therefore required. In this study, we demonstrate the formation of dewetting-induced hierarchical patterns using two self-assembled materials: block copolymers (BCPs) and colloidal crystals. The combination of the two self-assembly methods successfully generates multiscale hierarchical patterns because the length scales of the periodic colloidal crystal structures are suitable for templating the BCP patterns. Various concentric ring patterns were observed on the templated BCP films, and a free energy model of the polymer chain was applied to explain the formation of these patterns relative to the template width. Frequently occurring spiral-defective features were also examined and found to be promoted by Y-junction defects.
Controllable Preparation of Highly Crystalline Sulfur-Doped Π-Conjugated Polyimide Hollow Nanoshell for Enhanced Photocatalytic Performance
Authors: Zhang Duoping , Ma Chenghai , Shi Peidong , Yang Zuan , Rong Tongwei , Xiong Liurui , Liao Wenhui
Published: February 2023

In this study, a series of highly crystalline π-conjugated polyimide photocatalysts with porous nano hollow shell (HSPI) was prepared for the first time by the hard template method by adjusting the addition ratio of the template precursor. SiO2 nanospheres not only serve as template agents but also as dispersants to make precursors of SPI more uniform, and the degree of polymerization will be better, resulting in significantly enhanced crystallinity of HSPI relative to bulk SPI (BSPI). More strikingly, it is found that HSPI has a larger specific surface area, stronger visible light absorption, and higher separation efficiency of photogenerated electron and hole pairs compared with BSPI by various spectral means characterization analysis. These favorable factors significantly enhanced the photocatalytic degradation of methyl orange (MO) by HSPI. This work provides a promising approach for the preparation of cheap, efficient, environmentally friendly, and sustainable photocatalysts.
Influence of Synthetic Fibers on the Flexural Properties of Concrete: Prediction of Toughness as a Function of Volume, Slenderness Ratio and Elastic Modulus of Fibers
Authors: Del Savio Alexandre Almeida , Esquivel Darwin La Torre , de Andrade Silva Flávio , Agreda Pastor Joaquín
Published: February 2023

The construction industry requires concrete with adequate post-cracking behavior for applications such as tunnels, bridges, and pavements. For this reason, polypropylene macrofibers are used, which are synthetic fibers that fulfill the function of providing residual strength to concrete. In this study, an experimental plan is carried out to evaluate the bending behavior of concrete reinforced with polypropylene fibers using the four-point bending test according to ASTM C1609. Three fiber dosages (3.6, 7.2 and 10.8 kg/m3) and three fiber lengths (40, 50, and 60 mm) were used. The use of macro polypropylene fibers increased the post-cracking behavior of concrete. In addition, based on the experimentally obtained results and available literature data, a multivariable equation was developed to predict the concrete toughness as a function of the volume, slenderness, and modulus of elasticity of the fibers. A Pearson’s correlation coefficient, r of 0.90, showed a strong correlation between the developed equation and the experimental data. From this equation, it was possible to determine the participation of the following parameters in calculating toughness. The participation or weight of the fiber’s modulus of elasticity on the concrete’s tenacity is 26%, the volume of the fiber is 39%, the slenderness is 19%, and the reinforcement index is 16%.
Theoretical Derivation of the Effect of Bonding Current on the Bonding Interface during Anodic Bonding of PEG-Based Encapsulation Materials and Aluminum
Authors: Du Chao , Zhao Yali , Li Yong
Published: February 2023

This study analyzed the mechanism underlying the effect of the bonding current on the bonding interface during anodic bonding on the basis of the anodic bonding of PEG (polyethylene glycol)-based encapsulation materials and Al. By establishing an equivalent electrical model, the effects of various electrical parameters on the dynamic performance of the bonding current were evaluated, and the change law of the bonding current transfer function was analyzed. By examining the gap deformation model, the conditions for contact between the interface gaps and the bonding current pair were determined, and the influence law of the gap deformation of the bonding interface was derived. By assessing the effect of the bonding current on the ionic behavior, we found that the larger the bonding current, the greater the number of activated mobile ions in the bonding material and the higher the field strength in the cation depletion area. From the anodic bonding experiments, it was found that increasing the bonding voltage can increase the peak current and improve the bonding efficiency. The SEM image after bonding shows that the bonding interface had no obvious defects; the higher bonding voltage can result in a thicker bonding layer.
Self-Supported Biopolymeric Films Based on Onion Bulb (Allium cepa L.): Gamma-Radiation Effects in Sterilizing Doses
Authors: da Costa Borges Marco Antonio , Sorigotti Amanda Rinaldi , Paschoalin Rafaella Takehara , Júnior José Alberto Paris , da Silva Lucas Henrique Domingos , Dias Diógenes Santos , Ribeiro Clóvis Augusto , de Araújo Elmo Silvano , Resende Flávia Aparecida , da Silva Barud Hernane
Published: February 2023

Sterilization is a fundamental step to eliminate microorganisms prior to the application of products, especially in the food and medical industries. γ-irradiation is one of the most recommended and effective methods used for sterilization, but its effect on the properties and performance of bio-based polymers is negligible. This work is aimed at evaluating the influence of γ-radiation at doses of 5, 10, 15, 25, 30, and 40 kGy on the morphology, properties, and performance of bioplastic produced from onion bulb (Allium cepa L.), using two hydrothermal synthesis procedures. These procedures differ in whether the product is washed or not after bioplastic synthesis, and are referred to as the unwashed hydrothermally treated pulp (HTP) and washed hydrothermally treated pulp (W-HTP). The morphological analysis indicated that the film surfaces became progressively rougher and more irregular for doses above 25 kGy, which increases their hydrophobicity, especially for the W-HTP samples. In addition, the FTIR and XRD results indicated that irradiation changed the structural and chemical groups of the samples. There was an increase in the crystallinity index and a predominance of the interaction of radiation with the hydroxyl groups—more susceptible to the oxidative effect—besides the cleavage of chemical bonds depending on the γ-radiation dose. The presence of soluble carbohydrates influenced the mechanical behavior of the samples, in which HTP is more ductile than W-HTP, but γ-radiation did not cause a change in mechanical properties proportionally to the dose. For W-HTP, films there was no mutagenicity or cytotoxicity—even after γ-irradiation at higher doses. In conclusion, the properties of onion-based films varied significantly with the γ-radiation dose. The films were also affected differently by radiation, depending on their chemical composition and the change induced by washing, which influences their use in food packaging or biomedical devices.
An Adhesion Improvement of Low-Density Polyethylene to Aluminum through Modification with Functionalized Polymers
Authors: Nassr Mohamed , Krupa Igor , Ouederni Mabrouk , Krishnamoorthy Senthil Kumar , Popelka Anton
Published: February 2023

An interfacial adhesion improvement between low-density polyethylene (LDPE) and aluminum (Al) foil is an important challenge in designing multilayered packaging (TetraPak packaging type) due to insufficient inherent adhesion between both untreated materials. Therefore, extra adhesive layers are often used. The hydrophobic character of LDPE is responsible for poor adhesion to Al and can result in delamination. This study deals with the comparative study of the bulk modification of LDPE with various commercially available adhesive promoters with different chemical compositions to increase LDPE’s adhesive characteristics and ensure good adhesion in LDPE/Al laminates. A copolymer of ethylene and methacrylic acid; a terpolymer of ethylene, maleic anhydride, and acrylic ester; or maleated polyethylene (PE) were used as adhesive promoters, and their effect on adhesion improvement of LDPE to Al was investigated. The best adhesion improvement was observed in LDPE-modified samples with maleated PE, while 0.1 wt.% additive content significantly increased peel resistance (from zero to 105 N/m). An additional increase in additive content (0.5 wt.%) in LDPE led to stronger adhesion forces than the cohesion forces in Al foil. Adding 0.5 wt.% of maleated PE into LDPE improved the LDPE/Al laminates’ adhesion and can be applied in multilayered lamination applications.