Molecules, Vol. 29, Pages 1724: New Findings on the Crystal Polymorphism of Imepitoin
Renato Molteni
Scientific and industrial reasons dictate the study of the solid state of imepitoin, a highly safe and tolerable anticonvulsant drug used in the therapy of epileptic dogs that was approved in the Europe Union in 2013. Our investigations allowed us to discover the existence of a new polymorph of imepitoin, which finds itself in a monotropic relationship with the crystalline form (polymorph I) already known and present on the market. This form (polymorph II), obtained by crystallization from xylene, remains metastable under ambient conditions for at least 1 year. Both solid forms were characterized by the...
Source: Molecules - April 11, 2024 Category: Chemistry Authors: Giovanna Bruni Doretta Capsoni Anna Pellegrini Angela Altomare Mauro Coduri Chiara Ferrara Pietro Galinetto Renato Molteni Tags: Article Source Type: research
Molecules, Vol. 29, Pages 1725: Study on the Synthesis, Surface Activity, and Self-Assembly Behavior of Anionic Non-Ionic Gemini Surfactants
This article proposes a simple and effective synthesis method, using 3-aminopropane sulfonic acid, fatty alcohol polyoxyethylene ether, and epichlorohydrin as raw materials, to insert EO into hydrophobic alkyl chains and synthesize a series of new anionic non-ionic Gemini surfactants (CnEO-5, n = 8, 12, 16). The surface activity, thermodynamic properties, and self-assembly behavior of these surfactants were systematically studied through surface tension, conductivity, steady-state fluorescence probes, transmission electron microscopy, and molecular dynamics simulations. The surface tension test results show that CnEO-5 has...
Source: Molecules - April 11, 2024 Category: Chemistry Authors: Zhiqiang Man Wenxiang Wu Tags: Article Source Type: research
Molecules, Vol. 29, Pages 1720: Rapid Apta-Chromogenic Detection Method for Nitrofuran Metabolite Determination
Unajak
Nitrofuran (NF) contamination in food products is a global problem resulting in the banned utilization and importation of nitrofuran contaminated products. A novel chromogenic detection method using a specific DNA aptamer with high affinity and specificity to nitrofurans was developed. Single-stranded DNA aptamers specific to nitrofuran metabolites, including 3-amino-2-oxazolidinone (AOZ), 3-amino-5-methylmorpholino-2-oxazolidinone (AMOZ), and 1-aminohydantoin (AHD), were isolated using magnetic bead-SELEX. The colorimetric detection of nitrofurans using gold nanoparticles (AuNPs) exhibited an AOZ detection ran...
Source: Molecules - April 10, 2024 Category: Chemistry Authors: Navarat Chaisri Chutikarn Jaengphop Ikuo Hirono Sasimanas Unajak Tags: Article Source Type: research
Molecules, Vol. 29, Pages 1719: The Piezocatalytic Degradation of Sulfadiazine by Lanthanum-Doped Barium Titanate
Shiyang Li
Piezocatalysis, a heterogeneous catalytic technique, leverages the periodic electric field changes generated by piezoelectric materials under external forces to drive carriers for the advanced oxidation of organic pollutants. Antibiotics, as emerging trace organic pollutants in water sources, pose a potential threat to animals and drinking water safety. Thus, piezoelectric catalysis can be used to degrade trace organic pollutants in water. In this work, BaTiO3 and La-doped BaTiO3 were synthesized using an improved sol–gel–hydrothermal method and used as piezocatalytic materials t...
Source: Molecules - April 10, 2024 Category: Chemistry Authors: Daijun Meng Yuqi Xiang Ziwei Yang Hao Yuan Liang Tang Shiyang Li Tags: Article Source Type: research
Molecules, Vol. 29, Pages 1704: Impact of Backbone Substitution on Organocatalytic Activity of Sterically Encumbered NHC in Benzoin Condensation
In this study, we provide a theoretical explanation for the experimentally observed decrease in the organocatalytic activity of N-aryl imidazolylidenes methylated at the C4/5-H positions in the benzoin condensation of aromatic aldehydes. A comparative quantum chemical study of energy profiles for the NHC-mediated benzoin condensation of furfural has revealed a high energy barrier to the formation of the IPrMe-based furanic Breslow intermediate that can be attributed to the negative steric interactions between the imidazole backbone methyl groups and N-aryl substituents. (Source: Molecules)
Source: Molecules - April 10, 2024 Category: Chemistry Authors: Rinat R. Aysin Konstantin I. Galkin Tags: Communication Source Type: research
Molecules, Vol. 29, Pages 1705: Injectable Hydrogels Based on Hyaluronic Acid and Gelatin Combined with Salvianolic Acid B and Vascular Endothelial Growth Factor for Treatment of Traumatic Brain Injury in Mice
Haitong Wan
Traumatic brain injury (TBI) leads to structural damage in the brain, and is one of the major causes of disability and death in the world. Herein, we developed a composite injectable hydrogel (HA/Gel) composed of hyaluronic acid (HA) and gelatin (Gel), loaded with vascular endothelial growth factor (VEGF) and salvianolic acid B (SAB) for treatment of TBI. The HA/Gel hydrogels were formed by the coupling of phenol-rich tyramine-modified HA (HA-TA) and tyramine-modified Gel (Gel-TA) catalyzed by horseradish peroxidase (HRP) in the presence of hydrogen peroxide (H2O2). SEM results showed that HA/Gel hydrogel...
Source: Molecules - April 10, 2024 Category: Chemistry Authors: Guoying Zhou Yajie Cao Yujia Yan Haibo Xu Xiao Zhang Tingzi Yan Haitong Wan Tags: Article Source Type: research
Molecules, Vol. 29, Pages 1706: Temperature-Controlled Divergent Synthesis of Pyrazoles and 1-Tosyl-1H-pyrazoles under Transition-Metal-Catalyst- and Oxidant-Free Conditions
ing Cao
Herein, a general and practical temperature-controlled approach for the divergent synthesis of pyrazoles and 1-tosyl-1H-pyrazoles via electrophilic cyclization in the absence of transition-metal catalysts and oxidants was developed. The desired products were obtained in moderate to excellent yields from common starting materials in both ionic liquids and ethanol by simply tuning the reaction temperature. This strategy employs easily synthesized substrates, mild reaction conditions, and excellent functional-group tolerance. (Source: Molecules)
Source: Molecules - April 10, 2024 Category: Chemistry Authors: Kai Wang Wenjing Xu Chengcai Xia Xianting Cao Tags: Article Source Type: research
Molecules, Vol. 29, Pages 1707: Starch from Unripe Apples (Malus domestica Borkh) as an Alternative for Application in the Food Industry
This study investigated the properties of starch isolated from the unripe fruit of two apple cultivars (Malus domestica Borkh) grown in southern Poland (Central Europe). The chemical composition of both starches, molecular mass, their granulation, thermal characteristics, swelling characteristics, and rheological characteristics were studied. The starches differed significantly in ash, phosphorus, and protein content. The water-binding capacity at temperatures of 25–65 °C was similar, while differences of 20% appeared at higher temperatures. In contrast, a significant difference was found in the s...
Source: Molecules - April 10, 2024 Category: Chemistry Authors: Dorota Gumul Jaros ław Korus Magdalena Orczykowska Justyna Rosicka-Kaczmarek Joanna Oracz Anna Areczuk Tags: Article Source Type: research
Molecules, Vol. 29, Pages 1708: Antitumoral Activity of the Universal Methyl Donor S-Adenosylmethionine in Glioblastoma Cells
We report here for the first time that AdoMet selectively inhibited the viability and proliferation of U87MG, U343MG, and U251MG GBM cells. In these cell lines, AdoMet induced S and G2/M cell cycle arrest and apoptosis and downregulated the expression and activation of proteins involved in homologous recombination DNA repair, including RAD51, BRCA1, and Chk1. Furthermore, AdoMet was able to maintain DNA in a damaged state, as indicated by the increased γH2AX/H2AX ratio. AdoMet promoted mitotic catastrophe through inhibiting Aurora B kinase expression, phosphorylation, and localization causing GBM cells to und...
Source: Molecules - April 10, 2024 Category: Chemistry Authors: Laura Mosca Cristina Pagano Roberta Veglia Tranchese Roberta Grillo Francesca Cadoni Giovanna Navarra Laura Coppola Martina Pagano Luigi Mele Giovanna Cacciapuoti Chiara Laezza Marina Porcelli Tags: Article Source Type: research
Molecules, Vol. 29, Pages 1710: A Novel Cocrystal of Daidzein with Piperazine to Optimize the Solubility, Permeability and Bioavailability of Daidzein
uanhua Du
Yang Lu
It is well known that daidzein has various significant medicinal values and health benefits, such as anti-oxidant, anti-inflammatory, anti-cancer, anti-diabetic, cholesterol lowering, neuroprotective, cardioprotective and so on. To our disappointment, poor solubility, low permeability and inferior bioavailability seriously limit its clinical application and market development. To optimize the solubility, permeability and bioavailability of daidzein, the cocrystal of daidzein and piperazine was prepared through a scientific and reasonable design, which was thoroughly characterized by single-crystal X...
Source: Molecules - April 10, 2024 Category: Chemistry Authors: Zhipeng Wang Shuang Li Qi Li Wenwen Wang Meiru Liu Shiying Yang Li Zhang Dezhi Yang Guanhua Du Yang Lu Tags: Article Source Type: research
Molecules, Vol. 29, Pages 1709: Diselenide-Bridged Doxorubicin Dimeric Prodrug: Synthesis and Redox-Triggered Drug Release
Liu
The diselenide bond has attracted intense interest in redox-responsive drug delivery systems (DDSs) in tumor chemotherapy, due to its higher sensitivity than the most investigated bond, namely the disulfide bond. Here, a diselenide-bridged doxorubicin dimeric prodrug (D-DOXSeSe) was designed by coupling two doxorubicin molecules with a diselenodiacetic acid (DSeDAA) molecule via α-amidation, as a redox-triggered drug self-delivery system (DSDS) for tumor-specific chemotherapy. The drug release profiles indicated that the D-DOXSeSe could be cleaved to release the derivatives selenol (DOX-SeH) and selen...
Source: Molecules - April 10, 2024 Category: Chemistry Authors: Yanru Hu Peng Liu Tags: Article Source Type: research
Molecules, Vol. 29, Pages 1712: Genistein Prevents Apoptosis and Oxidative Stress Induced by Methylglyoxal in Endothelial Cells
In this study, the effect of genistein, a natural soybean isoflavone, has been evaluated on MG-induced cytotoxicity in human endothelial cells. Our results show that genistein is able to counteract the MG-induced apoptosis by restraining ROS production, thus inhibiting the MAPK signaling pathways and caspase-3 activation. These findings identify a beneficial role for genistein, providing new insights for its potential clinical applications in preserving endothelial function in diabetic vascular complications. (Source: Molecules)
Source: Molecules - April 10, 2024 Category: Chemistry Authors: Liccardo Sapio Perrella Sirangelo Iannuzzi Tags: Article Source Type: research
Molecules, Vol. 29, Pages 1711: Synthesis, Anti-Inflammatory Activities, and Molecular Docking Study of Novel Pyxinol Derivatives as Inhibitors of NF- & kappa;B Activation
Molecules, Vol. 29, Pages 1711: Synthesis, Anti-Inflammatory Activities, and Molecular Docking Study of Novel Pyxinol Derivatives as Inhibitors of NF-κB Activation
Molecules doi: 10.3390/molecules29081711
Authors:
Shuai Tan
Zongji Zou
Xuwen Luan
Cheng Chen
Shuang Li
Zhen Zhang
Mengran Quan
Xiang Li
Wei Zhu
Gangqiang Yang
Pyxinol, an active metabolite of ginsenosides in human hepatocytes, exhibits various pharmacological activities. Here, a series of C-3 modified pyxinol derivatives was designed and virtually screened by molecular docking with the key inflammation-related proteins of the ...
Source: Molecules - April 10, 2024 Category: Chemistry Authors: Shuai Tan Zongji Zou Xuwen Luan Cheng Chen Shuang Li Zhen Zhang Mengran Quan Xiang Li Wei Zhu Gangqiang Yang Tags: Article Source Type: research
Molecules, Vol. 29, Pages 1714: Electronic Effects in a Green Protocol for (Hetero)Aryl-S Coupling
Pace
Pisano
Aryl and heteroaryl iodides have been efficiently converted into the corresponding thioacetates in cyclopentyl methyl ether (CPME), a green solvent, under Cu catalysis. The chemoselectivity of the reaction is mainly controlled by electronic factors, enabling the conversion of both electron-rich and electron-deficient substrates into the corresponding thioacetates in good to excellent yields. The products can be easily deprotected to the corresponding thiolates to carry out additional synthetic transformations in situ. Surprisingly, despite CPME’s relatively low dielectric constant, the ...
Source: Molecules - April 10, 2024 Category: Chemistry Authors: Carraro Are Azzena De Luca Gaspa Satta Holzer Pace Pisano Tags: Article Source Type: research
Molecules, Vol. 29, Pages 1715: Total Synthesis of 4-epi-Bengamide E
Rocca
Lisa Moni
Bengamide E is a bioactive natural product that was isolated from Jaspidae sponges by Crews and co-workers in 1989. It displays a wide range of biological activities, including antitumor, antibiotic, and anthelmintic properties. With the aim of investigating the structural feature essential for their activity, several total syntheses of Bengamide E and its analogues have been reported in the literature. Nevertheless, no synthesis of the stereoisomer with modification of its configuration at C-4 carbon has been reported so far. Here, we report the first total synthesis of the 4-epi-Bengamide E. Key rea...
Source: Molecules - April 10, 2024 Category: Chemistry Authors: Gabriella Vitali Forconesi Andrea Basso Luca Banfi Davide Gugliotta Chiara Lambruschini Marta Nola Renata Riva Valeria Rocca Lisa Moni Tags: Article Source Type: research
