bluuebunny/crossref_metadata_2025 huggingface dataset:
Alteration of Substrate Specificity and Transglucosylation Activity of GH13_31 α-Glucosidase from Bacillus sp. AHU2216 through Site-Directed Mutagenesis of Asn258 on β→α Loop 5
Authors: Auiewiriyanukul Waraporn , Saburi Wataru , Ota Tomoya , Yu Jian , Kato Koji , Yao Min , Mori Haruhide
Published: March 2023

α-Glucosidase catalyzes the hydrolysis of α-d-glucosides and transglucosylation. Bacillus sp. AHU2216 α-glucosidase (BspAG13_31A), belonging to the glycoside hydrolase family 13 subfamily 31, specifically cleaves α-(1→4)-glucosidic linkages and shows high disaccharide specificity. We showed previously that the maltose moiety of maltotriose (G3) and maltotetraose (G4), covering subsites +1 and +2 of BspAG13_31A, adopts a less stable conformation than the global minimum energy conformation. This unstable d-glucosyl conformation likely arises from steric hindrance by Asn258 on β→α loop 5 of the catalytic (β/α)8-barrel. In this study, Asn258 mutants of BspAG13_31A were enzymatically and structurally analyzed. N258G/P mutations significantly enhanced trisaccharide specificity. The N258P mutation also enhanced the activity toward sucrose and produced erlose from sucrose through transglucosylation. N258G showed a higher specificity to transglucosylation with p-nitrophenyl α-d-glucopyranoside and maltose than the wild type. E256Q/N258G and E258Q/N258P structures in complex with G3 revealed that the maltose moiety of G3 bound at subsites +1 and +2 adopted a relaxed conformation, whereas a less stable conformation was taken in E256Q. This structural difference suggests that stabilizing the G3 conformation enhances trisaccharide specificity. The E256Q/N258G-G3 complex formed an additional hydrogen bond between Met229 and the d-glucose residue of G3 in subsite +2, and this interaction may enhance transglucosylation.
Polysaccharides from Discarded Stems of Trollius chinensis Bunge Elicit Promising Potential in Cosmetic Industry: Characterization, Moisture Retention and Antioxidant Activity
Authors: Liu Yang , Guo Qiwei , Zhang Saimin , Bao Yilin , Chen Mengling , Gao Lin , Zhang Yang , Zhou Hongli
Published: March 2023

Unconventional polysaccharides as representative active substances from stems of Trollius chinensis Bunge (TC) were studied. Crude polysaccharides from the stems of TC (TCSP) and the petals of TC (TCPP) were extracted, and the moisture retention and antioxidation activities of both TCSP and TCPP in vitro were studied. The weight-average molar masses (Mw) of TCSP (6.07 × 105 Da) were lower than those of TCPP (9.72 × 105 Da). Glucuronic acid and xylose only existed in TCSP, and the molar ratio of galacturonic acid and mannose in TCSP was significantly higher than that in TCPP. No significant differences in moisture retention ability were found between TCSP and TCPP. The reducing capacity and dphenyl picryl hydrazinyl (DPPH) radical scavenging capacity of TCSP were slightly weaker than those of TCPP. The 2,2-azino-bis (3-ethylbenzothiazoline–6-sulfonic acid) (ABTS) radical scavenging capacity of TCSP can be equivalent to that of TCPP. The moisture retention ability was not different between TCSP and TCPP, which are both highly homologous with traditional humectants. The antioxidation assays in vitro demonstrated that the antioxidant activity of TCSP is stronger compared to that of some plant-derived polysaccharides. The stems of TC can be a promising source of unconventional polysaccharides, which possess moisture retention and antioxidation capacities for the cosmetics industry.
Spin-Space-Encoding Magnetic Resonance Imaging: A New Application for Rapid and Sensitive Monitoring of Dynamic Swelling of Confined Hydrogels
Authors: Wang Rui , Xin Jiaxiang , Ji Zhengxiao , Zhu Mengni , Yu Yihua , Xu Min
Published: March 2023

An NMR method based on the gradient-based broadening fingerprint using line shape enhancement (PROFILE) is put forward to precisely and sensitively study hydrogel swelling under restricted conditions. This approach achieves a match between the resonance frequency and spatial position of the sample. A three-component hydrogel with salt ions was designed and synthesized to show the monitoring more clearly. The relationship between the hydrogel swelling and the frequency signal is revealed through the one-dimensional imaging. This method enables real-time monitoring and avoids changing the swelling environment of the hydrogel during contact. The accuracy of this method may reach the micron order. This finding provides an approach to the rapid and non-destructive detection of swelling, especially one-dimensional swelling, and may show the material exchange between the hydrogel and swelling medium.
Potential Therapeutic Value of the STING Inhibitors
Authors: Zhang Shangran , Zheng Runan , Pan Yanhong , Sun Hongbin
Published: March 2023

The stimulator of interferon genes (STING) is a critical protein in the activation of the immune system in response to DNA. It can participate the inflammatory response process by modulating the inflammation-preferred translation program through the STING-PKR-like endoplasmic reticulum kinase (PERK)-eIF2α pathway or by inducing the secretion of type I interferons (IFNs) and a variety of proinflammatory factors through the recruitment of TANK-binding kinase 1 (TBK1) and interferon regulatory factor 3 (IRF3) or the regulation of the nuclear factor kappa-B (NF-κB) pathway. Based on the structure, location, function, genotype, and regulatory mechanism of STING, this review summarizes the potential value of STING inhibitors in the prevention and treatment of infectious diseases, psoriasis, systemic lupus erythematosus, non-alcoholic fatty liver disease, and other inflammatory and autoimmune diseases.
One-Pot Synthesis and Evaluation of Antioxidative Stress and Anticancer Properties of an Active Chromone Derivative
Authors: Maicheen Chirattikan , Churnthammakarn Chokchaloemwat , Pongsroypech Nichapat , Khamkhenshorngphanuch Thitiphong , Ungwitayatorn Jiraporn , Rungsardthong Kanin , Asasutjarit Rathapon , Theeramunkong Sewan
Published: March 2023

Chromones are the structural building blocks of several natural flavonoids. The synthesis of chromones, which contain a hydroxy group on the ring, presents some challenges. We used the one-pot method to synthesize ten chromone derivatives and two related compounds using modified Baker-Venkataraman reactions. The structures were confirmed using FT-IR, 1H NMR, 13C NMR, and HRMS. The in vitro antioxidant assay revealed that compounds 2e, 2f, 2j, and 3i had potent antioxidant activity and that all these synthesized compounds, except those containing nitro groups, were harmless to normal cells. In addition, compounds 2b, 2d, 2e, 2f, 2g, 2i, and 2j had anticancer activity. Compounds 2f and 2j were used to investigate the mechanism of anticancer activity. Both 2f and 2j induced a slightly early apoptotic effect but significantly impacted the S phase in the cell cycle. The effect on cell invasion indicates that both compounds significantly inhibited the growth of cervical cancer cells. A chromone scaffold possesses effective chemoprotective and antioxidant properties, making it a promising candidate for antioxidant and future cancer treatments.
Preparation of Sulfonated Poly(arylene ether)/SiO2 Composite Membranes with Enhanced Proton Selectivity for Vanadium Redox Flow Batteries
Authors: Ye Zhoulin , Chen Nanjie , Zheng Zigui , Xiong Lei , Chen Dongyang
Published: March 2023

Proton exchange membranes (PEMs) are an important type of vanadium redox flow battery (VRFB) separator that play the key role of separating positive and negative electrolytes while transporting protons. In order to lower the vanadium ion permeability and improve the proton selectivity of PEMs for enhancing the Coulombic efficiency of VRFBs, herein, various amounts of nano-sized SiO2 particles were introduced into a previously optimized sulfonated poly(arylene ether) (SPAE) PEMs through the acid-catalyzed sol-gel reaction of tetraethyl orthosilicate (TEOS). The successful incorporation of SiO2 was confirmed by FT-IR spectra. The scanning electron microscopy (SEM) images revealed that the SiO2 particles were well distributed in the SPAE membrane. The ion exchange capacity, water uptake, and swelling ratio of the PEMs were decreased with the increasing amount of SiO2, while the mechanical properties and thermal stability were improved significantly. The proton conductivity was reduced gradually from 93.4 to 76.9 mS cm−1 at room temperature as the loading amount of SiO2 was increased from 0 to 16 wt.%; however, the VO2+ permeability was decreased dramatically after the incorporation of SiO2 and reached a minimum value of 2.57 × 10−12 m2 s−1 at 12 wt.% of SiO2. As a result, the H+/VO2+ selectivity achieved a maximum value of 51.82 S min cm−3 for the composite PEM containing 12 wt.% of SiO2. This study demonstrates that the properties of PEMs can be largely tuned by the introduction of SiO2 with low cost for VRFB applications.
The Progress of Hard Carbon as an Anode Material in Sodium-Ion Batteries
Authors: Tan Suchong , Yang Han , Zhang Zhen , Xu Xiangyu , Xu Yuanyuan , Zhou Jian , Zhou Xinchi , Pan Zhengdao , Rao Xingyou , Gu Yudong , Wang Zhoulu , Wu Yutong , Liu Xiang , Zhang Yi
Published: March 2023

When compared to expensive lithium metal, the metal sodium resources on Earth are abundant and evenly distributed. Therefore, low-cost sodium-ion batteries are expected to replace lithium-ion batteries and become the most likely energy storage system for large-scale applications. Among the many anode materials for sodium-ion batteries, hard carbon has obvious advantages and great commercial potential. In this review, the adsorption behavior of sodium ions at the active sites on the surface of hard carbon, the process of entering the graphite lamellar, and their sequence in the discharge process are analyzed. The controversial storage mechanism of sodium ions is discussed, and four storage mechanisms for sodium ions are summarized. Not only is the storage mechanism of sodium ions (in hard carbon) analyzed in depth, but also the relationships between their morphology and structure regulation and between heteroatom doping and electrolyte optimization are further discussed, as well as the electrochemical performance of hard carbon anodes in sodium-ion batteries. It is expected that the sodium-ion batteries with hard carbon anodes will have excellent electrochemical performance, and lower costs will be required for large-scale energy storage systems.
Pharmacological Characters and Toxicity Evaluation of Coumarin Derivative LP4C as Lead Compound against Biofilm Formation of Pseudomonas aeruginosa
Authors: Yu Moxi , Xin Jiajia , Liu Yongsheng , Chen Yamiao , Zhao Hui , Li Yaoyao , Hou Yachen , Jia Min , Wang Bin , Li Mingkai
Published: March 2023

Pseudomonas aeruginosa-induced biofilm infection is difficult to treat and poses a significant threat to public health. Our previous study found a new coumarin derivative LP4C which exerted potent in vitro and in vivo anti-biofilm activity against Pseudomonas aeruginosa; however, the underlying molecular mechanism and drug-likeness of LP4C is unclear. In this study, we confirmed that LP4C could inhibit the biofilm in dose-dependent manner without bactericidal activity. The transcriptomic profiling and RT-PCR result revealed that bacterial pyrimidine mediated the inhibitory activity of LP4C. The cell viability was not affected in LP4C treatment groups with the concentration under 200 μg/mL, and no death or toxicity sign was observed in mice treated by 20, 40 and 80 mg/kg LP4C during the three-week test period. Ames test presented that LP4C had no effect on the bacterial reverse mutation. In additional, pharmacokinetic results showed that LP4C was likely to have the orally bioavailable properties. Our data indicate that LP4C is a possible lead compound for the development of new anti-biofilm infection agents against Pseudomonas aeruginosa.
A Brief Review of Transparent Conducting Oxides (TCO): The Influence of Different Deposition Techniques on the Efficiency of Solar Cells
Authors: Chavan Ganesh T. , Kim Youngkuk , Khokhar Muhammad Quddamah , Hussain Shahzada Qamar , Cho Eun-Chel , Yi Junsin , Ahmad Zubair , Rosaiah Pitcheri , Jeon Chan-Wook
Published: March 2023

Global-warming-induced climate changes and socioeconomic issues increasingly stimulate reviews of renewable energy. Among energy-generation devices, solar cells are often considered as renewable sources of energy. Lately, transparent conducting oxides (TCOs) are playing a significant role as back/front contact electrodes in silicon heterojunction solar cells (SHJ SCs). In particular, the optimized Sn-doped In2O3 (ITO) has served as a capable TCO material to improve the efficiency of SHJ SCs, due to excellent physicochemical properties such as high transmittance, electrical conductivity, mobility, bandgap, and a low refractive index. The doped-ITO thin films had promising characteristics and helped in promoting the efficiency of SHJ SCs. Further, SHJ technology, together with an interdigitated back contact structure, achieved an outstanding efficiency of 26.7%. The present article discusses the deposition of TCO films by various techniques, parameters affecting TCO properties, characteristics of doped and undoped TCO materials, and their influence on SHJ SC efficiency, based on a review of ongoing research and development activities.
Biopolymer Chitosan Surface Engineering with Magnesium Oxide-Pluronic-F127-Escin Nanoparticles on Human Breast Carcinoma Cell Line and Microbial Strains
Authors: Mickymaray Suresh , Al Aboody Mohammed Saleh , Eraqi Mostafa M. , Alhoqail Wardah. A. , Alothaim Abdulaziz S. , Suresh Kaviya
Published: March 2023

Nanotechnology has been recognized as a highly interdisciplinary field of the twenty-first century, with diverse applications in biotechnology, healthcare, and material science. One of the most commonly employed non-toxic nanoparticles, magnesium oxide nanoparticles (MgO NPs), is simple, inexpensive, biocompatible, and biodegradable. Several researchers are interested in the biosynthesis process of MgO NPs through chemical and physical approaches. This is because of their simplicity, affordability, and environmental safety. In the current study, green MgO-Chitosan-Pluronic F127-Escin (MCsPFE) NPs have been synthesized and characterized via various techniques like UV-visible, Fourier-transform infrared spectroscopy, Energy dispersive X-ray composition analysis, Transmission electron microscopy, field emission scanning electron microscopy, X-ray Diffraction, Photoluminescence, and Dynamic light scattering analyses. The average crystallite size of MCsPFE NPs was 46 nm, and a face-centered cubic crystalline structure was observed. Further, the antimicrobial effectiveness of NPs against diverse pathogens has been assessed. The cytotoxic potential of the nanoparticles against MDA-MB-231 cell lines was evaluated using the MTT test, dual AO/EB, JC-1, DCFH–DA, and DAPI staining procedures. High antimicrobial efficacy of MCsPFE NPs against Gram-positive and Gram-negative bacterial strains as well as Candida albicans was observed. The findings concluded that the NPs augmented the ROS levels in the cells and altered the Δψm, leading to the initiation of the intrinsic apoptotic cell death pathway. Thus, green MCsPFE NPs possess immense potential to be employed as an effective antimicrobial and anticancer treatment option.
Nitrogen-Doped Graphene Oxide as Efficient Metal-Free Electrocatalyst in PEM Fuel Cells
Authors: Marinoiu Adriana , Raceanu Mircea , Carcadea Elena , Varlam Mihai
Published: March 2023

Nitrogen-doped graphene is currently recognized as one of the most promising catalysts for the oxygen reduction reaction (ORR). It has been demonstrated to act as a metal-free electrode with good electrocatalytic activity and long-term operation stability, excellent for the ORR in proton exchange membrane fuel cells (PEMFCs). As a consequence, intensive research has been dedicated to the investigation of this catalyst through varying the methodologies for the synthesis, characterization, and technologies improvement. A simple, scalable, single-step synthesis method for nitrogen-doped graphene oxide preparation was adopted in this paper. The physical and chemical properties of various materials obtained from different precursors have been evaluated and compared, leading to the conclusion that ammonia allows for a higher resulting nitrogen concentration, due to its high vapor pressure, which facilitates the functionalization reaction of graphene oxide. Electrochemical measurements indicated that the presence of nitrogen-doped oxide can effectively enhance the electrocatalytic activity and stability for ORR, making it a viable candidate for practical application as a PEMFC cathode electrode.
Bionic Plasmonic Nanoarrays Excited by Radially Polarized Vector Beam for Metal-Enhanced Fluorescence
Authors: Liu Min , Yu Lan , Li Yanru , Ma Ying , An Sha , Zheng Juanjuan , Liu Lixin , Lin Ke , Gao Peng
Published: March 2023

Metal-enhanced fluorescence (MEF) is an important fluorescence technology due to its ability to significantly improve the fluorescence intensity. Here, we present a new MEF configuration of the bionic nanorod array illuminated by radially polarized vector beam (RVB). The bionic nanorod array is fabricated via a nanoimprinting method by using the wings of the Chinese cicada “meimuna mongolica” as bio-templates, and later coating gold film by ion sputtering deposition method. The MEF performance of the prepared substrate is tested by a home-made optical system. The experiment results show that, in the case of RVB excitation, the intensity of fluorescence is more than 10 times stronger with the nano-imprinted substrate than that with glass. Using the bionic nanoarray as a substrate, the intensity of fluorescence is ~2 times stronger via RVB than that by the linearly polarized beam. In addition, the prepared substrate is verified to have good uniformity.
Piezoelectric Enhancement of Piezoceramic Nanoparticle-Doped PVDF/PCL Core-Sheath Fibers
Authors: Feng Zhangbin , Wang Ke , Liu Yukang , Han Biao , Yu Deng-Guang
Published: March 2023

Electrospinning is considered to be an efficient method to prepare piezoelectric thin films because of its ability to transform the phase of the polymers. A core-sheath structure can endow fibers with more functions and properties. In this study, fibers with a core-sheath structure were prepared using polyvinylidene fluoride (PVDF) included with nanoparticles (NPs) as the shell layer and polycaprolactone (PCL) as the core layer. Their mechanical and piezoelectric properties were studied in detail. During the course of the electrospinning process, PVDF was demonstrated to increase the amount of its polar phase, with the help of nanoparticles acting as a nucleating agent to facilitate the change. PCL was chosen as a core material because of its good mechanical properties and its compatibility with PVDF. Transmission electron microscope (TEM) assessments revealed that the fibers have a core-sheath structure, and shell layers were loaded with nanoparticles. Mechanical testing showed that the core layer can significantly improve mechanical properties. The XRD patterns of the core-sheath structure fibers indicated the β phase domain the main component. Piezoelectric testing showed that the doped nanoparticles were able to enhance piezoelectric performances. The increases of mechanical and piezoelectric properties of core-sheath structure fibers provide a feasible application for wearable electronics, which require flexibility and good mechanical properties.
Exploring Solar Cells Based on Lead- and Iodide-Deficient Halide Perovskite (d-HP) Thin Films
Authors: Gollino Liam , Mercier Nicolas , Pauporté Thierry
Published: March 2023

Perovskite solar cells have become more and more attractive and competitive. However, their toxicity induced by the presence of lead and their rather low stability hinders their potential and future commercialization. Reducing lead content while improving stability then appears as a major axis of development. In the last years, we have reported a new family of perovskite presenting PbI+ unit vacancies inside the lattice caused by the insertion of big organic cations that do not respect the Goldschmidt tolerance factor: hydroxyethylammonium HO-(CH2)2-NH3+ (HEA+) and thioethylammonium HS-(CH2)2-NH3+ (TEA+). These perovskites, named d-HPs for lead and halide-deficient perovskites, present a 3D perovskite corner-shared Pb1−xI3−x network that can be assimilated to a lead-iodide-deficient MAPbI3 or FAPbI3 network. Here, we propose the chemical engineering of both systems for solar cell optimization. For d-MAPbI3-HEA, the power conversion efficiency (PCE) reached 11.47% while displaying enhanced stability and reduced lead content of 13% compared to MAPbI3. On the other hand, d-FAPbI3-TEA delivered a PCE of 8.33% with astounding perovskite film stability compared to classic α-FAPI. The presence of TEA+ within the lattice impedes α-FAPI degradation into yellow δ-FAPbI3 by direct degradation into inactive Pb(OH)I, thus dramatically slowing the aging of d-FAPbI3-TEA perovskite.
Nanotechnology-Based Diagnostics for Diseases Prevalent in Developing Countries: Current Advances in Point-of-Care Tests
Authors: Thwala Lungile Nomcebo , Ndlovu Sphumelele Colin , Mpofu Kelvin Tafadzwa , Lugongolo Masixole Yvonne , Mthunzi-Kufa Patience
Published: March 2023

The introduction of point-of-care testing (POCT) has revolutionized medical testing by allowing for simple tests to be conducted near the patient’s care point, rather than being confined to a medical laboratory. This has been especially beneficial for developing countries with limited infrastructure, where testing often involves sending specimens off-site and waiting for hours or days for results. However, the development of POCT devices has been challenging, with simplicity, accuracy, and cost-effectiveness being key factors in making these tests feasible. Nanotechnology has played a crucial role in achieving this goal, by not only making the tests possible but also masking their complexity. In this article, recent developments in POCT devices that benefit from nanotechnology are discussed. Microfluidics and lab-on-a-chip technologies are highlighted as major drivers of point-of-care testing, particularly in infectious disease diagnosis. These technologies enable various bioassays to be used at the point of care. The article also addresses the challenges faced by these technological advances and interesting future trends. The benefits of point-of-care testing are significant, especially in developing countries where medical care is shifting towards prevention, early detection, and managing chronic conditions. Infectious disease tests at the point of care in low-income countries can lead to prompt treatment, preventing infections from spreading.
Reaction of Cornu aspersum Immune System against Different Aelurostrongylus abstrusus Developmental Stages
Authors: Napoli Ettore , Sfacteria Alessandra , Rifici Claudia , Mazzullo Giuseppe , Gaglio Gabriella , Brianti Emanuele
Published: March 2023

Cornu aspersum, the land snail, is recognized as a suitable intermediate host of Aelurostrongylus abstrusus; however, there is little information both on larval development as well as on the intermediate host’s immune system reaction to the parasite. The aim of the study was to assess the histological reaction of C. aspersum’s immune system against A. abstrusus. Sixty-five snails were provided by a snail farm. Five of them were digested to assess the absence of natural parasitic infections. The remaining sixty were divided into five groups. Three groups of snails were infected with A. abstrusus using by-contact or injection methods; one group was injected only with saline solution and one group was left untreated as the control. The snails of group A were sacrificed and digested on study days 2, 10, and 18; snails of the other groups were collected and examined for histopathological analysis on study days 2, 10, and 18. On study day 2, in the infected snails, several free L1s were observed along with the absence of immune system reactions. On day 10, the L2s elicited an intense reaction in the internal layer of the muscular foot. On day 18, all L3s partially encapsulated by the snail’s immune system were observed in the outermost part of the muscular foot, which is near and among the goblet cells. This last finding suggests that L3s could be shed with the snail’s mucus and spread in the environment, representing an alternative route of transmission for this feline lungworm.
Synthesis, Anticancer, Antimicrobial and Antioxidant Potential of Novel 4-(Substituted phenyl-1,3,4-oxadiazol/thiadiazol-2-yl)-4-(4-substituted phenyl) Azetidin-2-One Derivatives
Authors: Kumar Davinder , Aggarwal Navidha , Kumar Virender , Kumar Harsh , Deep Aakash , Bibi Shabana , Chopra Hitesh , Kumar Marwaha Rakesh , Alshammari Abdulrahman , Alharbi Metab , Hayee Abdul
Published: March 2023

By exploiting the ample biological potential of 1,3,4-oxadiazole/thiadiazole ring, 4-substitutedphenyl-1,3,4-oxadiazol/Thiadiazol-2-yl)-4-(4-substitutedphenyl) azetidin-2-one derivatives were prepared. Various substituted azetidin-2-one derivatives have been identified as immunostimulating and antimicrobial, as well as their antioxidant activity. 2-amino 1,3,4 oxadiazole/thiadiazole conjugates were synthesized by mixing semi/thio carbazides and sodium acetate with water and stirring well, followed by adding aldehydes in methanol at room temperature. Acetate (glacial) was used as the catalyst to produce Schiff’s bases (intermediates) by treating substituted aldehydes with 2-amino 1,3,4 oxadiazole/thiadiazole(s). Using the mixture of triethylamine (dropwise) and chloroacetylchloride with vigorous stirring, 4-substitutedphenyl-1,3,4-oxadiazol/Thiadiazol-2-yl)-4-(4-substitutedphenyl) azetidin-2-one derivatives were prepared. The newly synthesized conjugates were evaluated for their anticancer potential using MCF-7 cell lines. Amoxicillin and fluconazole were used as reference drugs to determine their antimicrobial activity. Synthesized derivatives were evaluated for their antioxidant properties using 2-diphenyl-1-picrylhydrazyl (DPPH). In vitro cytotoxicity screening (MTTS assay) revealed that derivatives AZ-5, 9, 10, 14 and 19 demonstrated high efficacy with the percentage of inhibition at different concentration ranges (0.1 μM, 0.5 μM, 1 μM, 2 μM) of 89% to 94% μM as compared to doxorubicin as standard drug. The antimicrobial study indicated that compounds AZ-10, 19, and AZ-20 were found to have significant antimicrobial potential with MIC ranges of 3.34 µM to 3.71 µM in comparison to reference drugs having 4.29 µM to 5.10 µM. Based on antioxidant screening, most of the synthetic derivatives showed greater stability and effectiveness than the standard drug. According to the antioxidant screening, compounds AZ-5 and AZ-15 (IC50 = 45.02 μg/mL and 42.88 μg/mL, respectively) showed the greatest potency, as compared to ascorbic acid (IC50 = 78.63 μg/mL). Structure-activity relationship (SAR) studies of synthesized novel derivatives revealed that para-substituted halogen and nitro derivatives have remarkable potential against MCF-7 cancer cell lines and different microbial strains. Current evidence indicates that the synthesized derivatives may be promising candidates for use in the prevention and treatment of these infections. These synthesized compounds require further mechanism-based research to understand how they interact with the cells.
Modulatory Effect of Medicinal Plants and Their Active Constituents on ATP-Sensitive Potassium Channels (KATP) in Diabetes
Authors: Al Kury Lina T.
Published: March 2023

Hyperglycemia, which is a chronic metabolic condition caused by either a defect in insulin secretion or insulin resistance, is a hallmark of diabetes mellitus (DM). Sustained hyperglycemia leads to the onset and development of many health complications. Despite the number of available antidiabetic medications on the market, there is still a need for novel treatment agents with increased efficacy and fewer adverse effects. Many medicinal plants offer a rich supply of bioactive compounds that have remarkable pharmacological effects with less toxicity and side effects. According to published evidence, natural antidiabetic substances influence pancreatic β-cell development and proliferation, inhibit pancreatic β-cell death, and directly increase insulin output. Pancreatic ATP-sensitive potassium channels play an essential role in coupling glucose metabolism to the secretion of insulin. Although much of the literature is available on the antidiabetic effects of medicinal plants, very limited studies discuss their direct action on pancreatic KATP. The aim of this review is to focus on the modulatory effects of antidiabetic medicinal plants and their active constituents on pancreatic KATP. The KATP channel should be regarded as a key therapeutic milestone in the treatment of diabetes. Therefore, continuous research into the interaction of medicinal plants with the KATP channel is crucial.
Glycoconjugates of Mucochloric Acid—Synthesis and Biological Activity
Authors: Żurawska Katarzyna , Burdalska Daria , Skonieczna Magdalena , Byczek-Wyrostek Anna , Dawicka Anahit , Kasprzycka Anna , Walczak Krzysztof
Published: March 2023

The pharmacological effects of the presence of a sugar moiety, 1,2,3-triazole ring and silyl groups in the structure of biologically active compounds have been extensively studied in drug design and medicinal chemistry. These components can be useful tools to tailoring the bioavailability of target molecules. Herein we present the study on the impact of the sugar substituent structure and triisopropylsilyl group presence on the anticancer activity of mucochloric acid (MCA) derivatives containing the furan-2(5H)-one or 2H-pyrrol-2-one core. The obtained results clearly indicated that tested compounds caused a significant decrease in cell viability of HCT116 and MCF-7 cell lines. MCF-7 cells indicate serious resistance toward investigated compounds in comparison with HCT116 cell line, it suggests that estrogen-dependent breast cancer cells are significantly less sensitive to the tested derivatives. Depending on the structure of the sugar, the type and site of connection with the furanone or 2H-pyrrol-2-one derivative and the presence of the silyl group, the selectivity of the compound towards cancer cells can be controlled. The obtained results may have an impact on the design of new furanone-based anticancer compounds.
The Novel Artemisinin Dimer Isoniazide ELI-XXIII-98-2 Induces c-MYC Inhibition, DNA Damage, and Autophagy in Leukemia Cells
Authors: Elbadawi Mohamed , Boulos Joelle C. , Dawood Mona , Zhou Min , Gul Waseem , ElSohly Mahmoud A. , Klauck Sabine M. , Efferth Thomas
Published: March 2023

The proto-oncogenic transcription factor c-MYC plays a pivotal role in the development of tumorigenesis, cellular proliferation, and the control of cell death. Its expression is frequently altered in many cancer types, including hematological malignancies such as leukemia. The dimer isoniazide ELI-XXIII-98-2 is a derivative of the natural product artemisinin, with two artemisinin molecules and an isoniazide moiety as a linker in between them. In this study, we aimed to study the anticancer activity and the molecular mechanisms of this dimer molecule in drug-sensitive CCRF-CEM leukemia cells and their corresponding multidrug-resistant CEM/ADR5000 sub-line. The growth inhibitory activity was studied using the resazurin assay. To reveal the molecular mechanisms underlying the growth inhibitory activity, we performed in silico molecular docking, followed by several in vitro approaches such as the MYC reporter assay, microscale thermophoresis, microarray analyses, immunoblotting, qPCR, and comet assay. The artemisinin dimer isoniazide showed a potent growth inhibitory activity in CCRF-CEM but a 12-fold cross-resistance in multidrug-resistant CEM/ADR5000 cells. The molecular docking of artemisinin dimer isoniazide with c-MYC revealed a good binding (lowest binding energy of −9.84 ± 0.3 kcal/mol) and a predicted inhibition constant (pKi) of 66.46 ± 29.5 nM, which was confirmed by microscale thermophoresis and MYC reporter cell assays. Furthermore, c-MYC expression was downregulated by this compound in microarray hybridization and Western blotting analyses. Finally, the artemisinin dimer isoniazide modulated the expression of autophagy markers (LC3B and p62) and the DNA damage marker pH2AX, indicating the stimulation of both autophagy and DNA damage, respectively. Additionally, DNA double-strand breaks were observed in the alkaline comet assay. DNA damage, apoptosis, and autophagy induction could be attributed to the inhibition of c-MYC by ELI-XXIII-98-2.
Technegas, A Universal Technique for Lung Imaging in Nuclear Medicine: Technology, Physicochemical Properties, and Clinical Applications
Authors: Khatib Isra , Young Paul M.
Published: March 2023

Technegas was developed in Australia as an imaging radioaerosol in the late 1980s and is now commercialized by Cyclomedica, Pty Ltd. for diagnosing pulmonary embolism (PE). Technegas is produced by heating technetium-99m in a carbon crucible for a few seconds at high temperatures (2750 °C) to generate technetium–carbon nanoparticles with a gas-like behaviour. The submicron particulates formed allow easy diffusion to the lung periphery when inhaled. Technegas has been used for diagnosis in over 4.4 m patients across 60 countries and now offers exciting opportunities in areas outside of PE, including asthma and chronic obstructive pulmonary disease (COPD). The Technegas generation process and the physicochemical attributes of the aerosol have been studied over the past 30 years in parallel with the advancement in different analytical methodologies. Thus, it is now well established that the Technegas aerosol has a radioactivity aerodynamic diameter of <500 nm and is composed of agglomerated nanoparticles. With a plethora of literature studying different aspects of Technegas, this review focuses on a historical evaluation of the different methodologies’ findings over the years that provides insight into a scientific consensus of this technology. Also, we briefly discuss recent clinical innovations using Technegas and a brief history of Technegas patents.
Lutathera® Orphans: State of the Art and Future Application of Radioligand Therapy with 177Lu-DOTATATE
Authors: Urso Luca , Nieri Alberto , Uccelli Licia , Castello Angelo , Artioli Paolo , Cittanti Corrado , Marzola Maria Cristina , Florimonte Luigia , Castellani Massimo , Bissoli Sergio , Porto Francesca , Boschi Alessandra , Evangelista Laura , Bartolomei Mirco
Published: March 2023

Lutathera® is the first EMA- and FDA-approved radiopharmaceutical for radioligand therapy (RLT). Currently, on the legacy of the NETTER1 trial, only adult patients with progressive unresectable somatostatin receptor (SSTR) positive gastroenteropancreatic (GEP) neuroendocrine neoplasms (NET) can be treated with Lutathera®. Conversely, patients with SSTR-positive disease arising from outside the gastroenteric region do not currently have access to Lutathera® treatment despite several papers in the literature reporting the effectiveness and safety of RLT in these settings. Moreover, patients with well-differentiated G3 GEP-NET are also still “Lutathera orphans”, and retreatment with RLT in patients with disease relapse is currently not approved. The aim of this critical review is to summarize current literature evidence assessing the role of Lutathera® outside the approved indications. Moreover, ongoing clinical trials evaluating new possible applications of Lutathera® will be considered and discussed to provide an updated picture of future investigations.
Unleashing the Potential of Medicinal Plants in Benin: Assessing the Status of Research and the Need for Enhanced Practices
Authors: Agbodjento Eric , Lègba Boris , Dougnon Victorien Tamègnon , Klotoé Jean Robert , Déguénon Esther , Assogba Phénix , Koudokpon Hornel , Hanski Leena , Baba-Moussa Lamine , Yayi Ladékan Eléonore
Published: March 2023

Medicinal plants play a crucial role in the primary health care of the population in developing countries such as Benin. The national universities of Benin conduct research on the pharmacological, toxicological, and phytochemical properties of these plants, but the resulting knowledge often does not lead to the development of phytomedicines for the improvement of public health. This study aims to assess the current status of research on medicinal plants in Benin. A literature review was conducted using various search engines, and the collected data was analyzed. The results indicate that research on the biological properties of medicinal plants is still in its early stages, with limited and inadequate methodological approaches. These limitations highlight the urgent need to enhance research practices and facilitate the development of effective and safe phytomedicines.
Wrack Burial Limits Germination and Establishment of Yellow Flag Iris (Iris pseudacorus L.)
Authors: Castillo Jesús M. , Gallego-Tévar Blanca , Grewell Brenda J.
Published: March 2023

Seed burial under wrack, mats of water-transported plant debris, can limit recruitment of seedlings in wetlands. In a greenhouse experiment, we studied the effects of wrack burial (0, 1, 2, 4, 8 cm depths) on germination and emergence of the macrophyte Iris pseudacorus, native to Europe, Mediterranean Basin, and western Asia, that has invaded wetlands in nearly every global ecozone. We recorded the percentages of germinating, senescent, and quiescent seeds and evaluated seedling establishment and growth relative to substrate environmental variables. Seedling emergence of I. pseudacorus was reduced from >80% in controls without burial to <40% even at minimal wrack depths of 1 cm. Few I. pseudacorus seedlings were able to emerge from wrack burial of up to 8 cm in depth. We also found greater numbers of both quiescent seeds and germinated seeds that did not emerge from wrack burial. Reduced seedling emergence and increased seed quiescence with wrack burial were primarily explained by a reduction in daily temperature variation within the substrate. No senescent seedlings were observed with any depth of wrack burial. In view of our results, the management of I. pseudacorus invasion will be a long-term challenge, requiring continued control due to persistent seeds in wrack-buried seed banks.
Trends in Harnessing Plant Endophytic Microbiome for Heavy Metal Mitigation in Plants: A Perspective
Authors: Tiwari Pragya , Bae Hanhong
Published: March 2023

Plant microbiomes represent dynamic entities, influenced by the environmental stimuli and stresses in the surrounding conditions. Studies have suggested the benefits of commensal microbes in improving the overall fitness of plants, besides beneficial effects on plant adaptability and survival in challenging environmental conditions. The concept of ‘Defense biome’ has been proposed to include the plant-associated microbes that increase in response to plant stress and which need to be further explored for their role in plant fitness. Plant-associated endophytes are the emerging candidates, playing a pivotal role in plant growth, adaptability to challenging environmental conditions, and productivity, as well as showing tolerance to biotic and abiotic stresses. In this article, efforts have been made to discuss and understand the implications of stress-induced changes in plant endophytic microbiome, providing key insights into the effects of heavy metals on plant endophytic dynamics and how these beneficial microbes provide a prospective solution in the tolerance and mitigation of heavy metal in contaminated sites.
Anticancer Podophyllotoxin Recovery from Juniper Leaves at Atmospheric and High Pressure Using Eco-Friendly Solvents
Authors: Ivanova Diana , Nedialkov Paraskev , Tashev Alexander , Kokanova-Nedialkova Zlatina , Olech Marta , Nowak Renata , Boyadzhieva Stanislava , Angelov George , Yankov Dragomir
Published: March 2023

Podophyllotoxin (PPT) is a precursor for the synthesis of drugs against cancer and other diseases. The present sources of PPT (Sinopodophyllum hexandrum and Podophyllum peltatum) are endangered species, with PPT production highly dependent on their growing conditions. In connection with the identification of new sources of PPT, the present study aimed to recover PPT from Juniperus virginiana leaves via atmospheric or high pressure extraction methods with a focus on using eco-friendly solvents. PPT quantification was determined by UHPLC/HRMS/MS. A thorough study of conventional extraction was carried out to reveal the optimal conditions (solvent ethyl acetate at room temperature and a duration of 1 h) for maximizing the PPT recovery (about 30 mg/g of dry extract and 3 mg/g of dry initial plant material). Peleg’s equation was applied for process kinetics modeling. The best PPT content in the final dry extract (42–45 mg/g of dry extract) was obtained by high pressure methods under supercritical (scCO2 with ethanol or ethyl acetate, 30 MPa, 50 °C and 100 min) or accelerated solvent extraction conditions (solvent ethyl acetate, 10.35 MPa, 20 °C and 3 cycles for 15 min). Seasonal stability and storage stability of the raw material were also determined. The present results have potential applications in the pharmacy for the delivery of PPT from juniper leaves.
Melt Memory Effect in Polyethylene Random Terpolymer with Small Amount of 1-Octene and 1-Hexene Co-Units: Non-Isothermal and Isothermal Investigations
Authors: Wang Dengfei , Li Shiyan , Lu Ying , Wang Jian , Men Yongfeng
Published: March 2023

Homo-polymers of reasonable molecular weight relax very fast in the molten state. Starting from a semi-crystalline structure, when the homo-polymer is heated up to a temperature higher than its nominal melting temperature, it relaxes quickly into a homogenous molten state. The following crystallization temperature during cooling remains constant irrespective of the melt temperature. However, the situation is evidently different in copolymers. A phenomenon named the crystallization melt memory effect denotes an increased crystallization rate during cooling after a polymer was melted at different temperatures, which is often observed. The melt temperature can be even higher than the equilibrium melting temperature of the corresponding polymer crystals. In this work, we investigated such memory effect in a polyethylene random terpolymer with a small fraction of 1-octene and 1-hexene co-units using differential scanning calorimetry techniques. Both non-isothermal and isothermal protocols were employed. In non-isothermal tests, a purposely prepared sample with well defined thermal history (the sample has been first conditioned at 200 °C for 5 min to eliminate the thermal history and then cooled down to −50 °C) was melted at different temperatures, followed by a continuous cooling at a constant rate of 20 °C/min. Peak crystallization temperature during cooling was taken to represent the crystallization rate. Whereas, in isothermal tests, the same prepared sample with well defined thermal history was cooled to a certain crystallization temperature after being melted at different temperatures. Here, time to complete the isothermal crystallization was recorded. It was found that the results of isothermal tests allowed us to divide the melt temperature into four zones where the features of the crystallization half time change.
Research the Thermal Decomposition Processes of Copolymers Based on Polypropyleneglycolfumaratephthalate with Acrylic Acid
Authors: Sarsenbekova Akmaral Zh. , Zhumanazarova Gaziza M. , Tazhbayev Yerkeblan M. , Kudaibergen Gulshakhar K. , Kabieva Saule K. , Issina Zhannur A. , Kaldybayeva Aigul K. , Mukabylova Arailym O. , Kilybay Muslim A.
Published: March 2023

Kinetics of thermal degradation of polymeric materials is usually studied by weight loss at a constant temperature or during heating. Hence, the activation energy and other kinetic parameters of the thermal destruction process are determined. One of the fastest and most accessible methods for studying the kinetics of these processes is TGA. Weight methods of TGA do not provide an opportunity to judge the proportion of gaseous degradation products. This is especially true for processes associated with the release of hydrogen and other substances with low molecular weights, the accuracy of determining the amount of which by the weight method is low. Meanwhile, the study of the gas evolution process can provide additional information about the kinetics and mechanism of thermal destruction processes. Of great interest is also the joint study of the total weight loss and gas evolution during the polymer heating. Using mass spectrometry, IR spectroscopy combined with thermal analysis (TGA/DSC-IR and TGA/DSC-MS) we have defined product composition and thermal destruction kinetics. As a result of the TGA/DSC-MS study of gaseous products of thermolysis in nitrogen atmosphere, there were found products with 44, 45, 59, 60, 68, and 88 phr. Quite a similar pattern for p-PGFPh:AA copolymers is also observed in TGA/DSC-IR studies: the same products and the same temperature range. However, in contrast to the TGA/DSC-MS study, CO release was also recorded by this method (weak signal). Kinetic characteristics of the processes were determined based on Friedman, Ozawa-Flynn-Wall and modified NPC methods. Obtained values of the activation energy and thermodynamic characteristics make it possible to predict the composition of polymers, which make a significant contribution to the development of theoretical ideas about the features of the physicochemical properties of polymers.
Dimensionally Stable Delignified Bamboo Matrix Phase-Change Composite under Ambient Temperature for Indoor Thermal Regulation
Authors: Duan Qinchen , Zhang Xin , Lang Shuang , Liu Guowei , Wang Hui , Zhou Xiaojian , Du Guanben
Published: March 2023

Energy storage materials to modulate indoor microclimates are needed to improve energy efficiency and for human comfort. Of these, phase-change material (PCM) is considered a very useful material because of its excellent latent heat energy storage. For application, some synthetic porous materials for supporting PCM are usually not friendly enough for people and housing environments due to their non-degradation characteristics. Hence, to develop an eco-friendly porous material is needed in order to encapsulate PCM composites that are always expected in indoor applications. In this work, heat-treated bamboo bricks were delignified to provide a delignified bamboo (DB) matrix. A phase-change composite was then fabricated by impregnating DB with polyethylene glycol (PEG) polymer. Impregnation was carried out under wet conditions to ensure the regular arrangement of the DB structure so as to achieve dimensional stability. The final DB/PEG composite was investigated for dimensional stability, load rate, latent heat, and phase-change temperature. Results showed that the DB matrix could be easily impregnated with PEG polymer under wet conditions, and the DB/PEG composite was found to have high enthalpy and a large phase-change temperature interval. Moreover, the composite was found to be a good regulator of indoor temperature and a stable dimension with a snow-white appearance. In summary, this DB/PEG composite is an energy storage material with the potential to modulate ambient indoor temperature and reduce building energy consumption.