Chemical Papers最新文献

Poly(2-Hydroxyethyl Methacrylate) (pHEMA) is a cheap biocompatible polymer. It is used in many studies as drug carrier systems, including nanoparticle hydrogels and cryogels. Naringenin (Nar) is a natural bioactive compound and has antibacterial, anticancer, antioxidant activities. Its use in treatment is limited due to its low water solubility and bioavailability. In this study, Nar was successfully loaded into pHEMA membranes and inhibited bacterial colonies. Nar-loaded/unloaded pHEMA membranes were characterized by FTIR and SEM. Additionally, the biocompatibility of the membranes was tested on human dermal fibroblasts (HDFa) cells, and their antibacterial properties were tested against Staphylococcus aureus bacteria. Nar was successfully loaded into the membranes. It was determined that after loading Nar, the pores of the membranes became smaller (average 5.7 µm) and more regular. It was determined that the prepared Nar-loaded pHEMA membranes completely inhibited bacteria and showed biocompatibility against HDFa cells. The binding affinity of the Nar to various Staphylococcus aureus proteins (PDB ID:3U2D, PDB ID:4H8E, PDB ID:3VSL, PDB ID:5YHG, PDB ID:6U3Y, and PDB ID:1JIJ) was found to be highest for PDB IDs 1JIJ and 5YHG at − 8.3 and − 8.5 kcal/mol, respectively, while the lowest binding affinity was observed for PDB ID:4H8E at − 5.2 kcal/mol.

An in situ shipborne detection device was developed and applied to the detection of manganese ion (Mn²⁺) in the offshore seawater. A sealed chamber design was used for insulating against the seawater corrosion. And under the control of computer, the device would be run without any manual intervention. The waste would be collected and follow further treatment. The sensitivity of the device was investigated with a limit of detection (3σ/S) of 1.0 ppb between the concentration 0 and 200 ppb. The stability of the device also examined with a RSD of 4.6% (n = 10), and the device worked well last a month with the same electrode. Finally, the in situ shipborne detection device has been successfully applied for the determination of Mn²⁺ in seawater around Xiamen Island. A series of optimizations would be carried out so that the shipborne detection device will be more suitably applied to the determination of heavy metal ions in seawater in the future.

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Bacitracin is among a group of antibiotic growth promoters banned in the European Union since the 1999 Council. In this study, two novel spectrofluorimetric methods were designed, developed, and validated for determining bacitracin by turning on its fluorescence activity. The turning on strategies are based on the condensation of its 1ry amine moiety either with acetylacetone and formaldehyde (Ac-Fr method), or with ninhydrin and phenylacetaldehyde (Nin-Ph method). The produced fluorescence intensity was measured at an emission of 482.5 nm (excitation = 421.5 nm) for Ac-Fr method and measured at an emission of 479.5 nm (excitation = 383.5 nm) for Nin-Ph method. A thorough investigation and optimization of the reaction conditions for both strategies was carried out. The selectivity of the established methodologies towards bacitracin was studied. The established linear ranges were 0.1–1.0 and 1.0–5.0 µg/mL for Ac-Fr method and Nin-Ph method, respectively. The LOD values were 31.2 and 163 ng/mL for Ac-Fr method and Nin-Ph method, respectively. Furthermore, the established methods were applied to determine bacitracin in water samples successfully. The recommended process for comprehensive greenness evaluations was implemented using Modified NEMI, AGREEprep, ComplexGAPI, and the newest SPMS tools. Moreover, the most recently introduced RGB12 and BAGI algorithms were employed in the concepts of “whiteness” and “blueness” inspection. This emphasizes the significance of doing a holistic sustainability assessment that takes into account greenness, analytical excellence, and practicality while creating new techniques. The suggested technique provides sensitive, cost-effective, and sustainable substitutes for traditional analysis methods.

Globally, cancer is the second leading cause of mortality, surpassed only by cardiovascular disorders. Among its various types, Non-Small Cell Lung Cancer (NSCLC) poses a significant global health risk. Chemotherapy is the most common therapeutic approach for treating cancer. However, chemotherapeutic drugs can cause serious toxicity by reducing the survival of both tumor and normal cells, thereby diminishing the survival chances of patients. Natural products extracted from medicinal plants serve as effective anticancer agents with minimal side effects. Among natural compounds, flavonoids have been reported as effective anticancer agents. In this study, two flavonoids, viscosine and quercetin 7-rutinoside, were evaluated for their antitumor potential using in silico models. These flavonoids were tested for their inhibitory activity against DEAD-box RNA helicase DDX3X (referred to as DDX3) and B-cell lymphoma-extra-large (Bcl-XL) enzymes through molecular docking and dynamic simulation analyses. The docking analysis revealed low docking scores and binding energies for both viscosine and quercetin 7-rutinoside. The overall docking results revealed that the selected flavonoids exhibited a favorable binding affinity for DDX3 and Bcl-X_L. They bind firmly to the key active sites and remain stably within the pocket regions of DDX3 and Bcl-X_L, thereby inhibiting their activity. This data was further supported by the RMSF and RMSD analyses. The preliminary molecular docking and simulation analyses confirm the promising inhibitory effects of viscosine and quercetin 7-rutinoside against DDX3 and Bcl-X_L. Therefore, these flavonoids could serve as potential antitumor drug candidates in the future. However, further experimental studies are needed to validate their potential for clinical trials.

Non-benzodiazepine sedative-hypnotic zaleplon has showed potential in reducing symptoms of HIV infection in people who suffer from sleeplessness. It interacts with Gamma-aminobutyric acid (GABA) receptors and enhances sleep quality. Insomnia is associated with metabolic difficulties; zaleplon’s effects on metabolic alterations and branched-chain amino acid (BCAA) metabolism indicate it may be useful in treating these concerns. It also helps with secondary depression, demonstrating its therapeutic value. To evaluate the oral bioavailability and subjective sleep quality and duration of the newly designed Zaleplon nanoemulsifying drug delivery system (SNEDDS). This study developed a solution of optimised Zaleplon self-nanoemulsifying medication delivery devices and then pharmacokinetics and pharmacodynamics characteristics were compared with that of the market-available similar drug on psychiatric patients. Multiple components were obtained, and response surface design reduced tests. The UV–Vis spectrophotometry assessed optical clarity after dilution. Comparing Zal-SNEDDS to control capsules in simulated stomach fluid for dissolution examined medication concentration. High-performance liquid chromatography was used to measure serum Zaleplon concentration before and after administration. The study demonstrated significant improvements in subjective sleep quality for the Zaleplon-SNEDDS group, which scored lower (0.69 ± 0.066) compared to the usual Zaleplon group (1.25 ± 0.085) with a p-value of 0.0026. Sleep latency showed no significant difference between the groups. Both groups had low sleep disturbance scores, with no significant difference observed. Daytime dysfunction significantly improved in the Zaleplon-SNEDDS group (p = 0.0012). Sleep duration was significantly better in the Zaleplon-SNEDDS group (p = 0.045). Total PSQI scores showed a trend towards improvement in the Zaleplon-SNEDDS group, though not statistically significant (p = 0.065). The study concluded that Zaleplon-SNEDDS is highly effective in increasing subjective sleep quality, daytime dysfunction and sleep duration as compared to the Zaleplon available in the market.

Chitosan and heparin are two biopolymers with different properties that can be combined to develop biomaterials with unique and desirable characteristics. Chitosan is a cationic polymer with antimicrobial, hemostatic, and wound-healing properties. Heparin is an anionic polymer with anticoagulant properties. The combination of chitosan and heparin can be used to develop biomaterials with a variety of applications, including drug delivery, wound dressing, and tissue engineering. These biomaterials can be fabricated into various forms, such as films, membranes, sponges, hydrogels, nanoparticles, and scaffolds. Chitosan is a natural polysaccharide, present in the form of copolymers of N-acetyl-D-glucosamine as repeating units. Heparin is a natural glycosaminoglycan; a linear sulfated molecule consisting of repetitive units of disaccharide containing uronic acid and N-acetyl glucosamine. Heparin binds and activates the vascular endothelial growth factor (VEGF), which in turn promotes proliferation and migration and thus results in angiogenesis and the formation of new blood vessels. These advantages make chitosan- and heparin-based biomaterials promising candidates for a variety of biomedical applications. However, there are still some challenges that need to be addressed before these biomaterials can be widely used in clinical practices. For example, the degradation rate of chitosan- and heparin-based biomaterials need to be better controlled, and the mechanical properties of these biomaterials need to be improved. Despite these challenges, chitosan- and heparin-based biomaterials have the potential to revolutionize the field of biomedicine. These biomaterials offer several advantages over traditional materials, and they have the potential to be used in a variety of innovative applications. The purpose of this review is to provide a comprehensive overview of the current state of research and applications in this field. It aims to summarize the key findings and advancements in the development and use of chitosan- and heparin-based hydrogels for various biomedical applications.

The health crisis induced by the COVID-19 pandemic has accelerated the quest for innovative antiviral drugs. One such advancement is the authorization of favipiravir (FAR) as an antiviral medication for COVID-19 management. As a result, it is essential to develop precise and cost-effective methodologies for quantifying FAR levels in plasma samples and tablets. In this research, we describe the creation of novel, thermostable (25–80 °C) and pH (3–11) stable amine-doped carbon dots (N@CQDs using green source) produced via a single-step synthesis approach for the assessment of FAR with high quantum yield 33.84% for reduction in the consumed organic solvents. Carbon quantum dots (CQDs) have garnered significant attention in recent times due to their effectiveness as probes. Their affordability, environmentally friendly nature, and exceptional photocatalytic properties have positioned them as noteworthy substitutes for traditional luminescent methods such as fluorescent dyes and luminous derivatization. The addition of FAR significantly reduced the luminescence response of the synthesized green and stable carbon quantum dots at 515 nm. The linear graph for detection was quantified to be 5.0–200.0 ng mL⁻¹, with a lower limit of quantitation (LOQ) of 3.85 ng mL⁻¹. The method’s high sensitivity, thermostable, and selectivity make it suitable for use in clinical laboratories. Besides, the reusability and stability of the N@CQDs were conducted effectively for analysis of FAR.

TMP195 is a highly profiled clinical candidate demonstrating class IIa histone deacetylase (HDAC) selective inhibition. Current preparation of TMP195 is limited to subgram-scale due to the requirement of tedious (post-)experimental procedures and the uses of hazardous reagents. To fulfill the unmet need for the bulky synthesis of TMP195 for the future clinical study, we have carried out its synthetic research. The present study provides a novel synthetic process suitable for the multigram-scale synthesis of TMP195. Its overall yield has increased significantly from the literature to the present, with respective values of 9% and 45%. Notably, the proposed process is more efficient and facile, characterized by accelerated reaction rates from 40 h to within 19 h and a streamlined post-reaction column chromatography purification from five reactions to just one. Additionally, the proposed process is more environmentally friendly, featured by the solvent-free synthesis of key intermediate 4-(chloromethyl)-2-phenyloxazole and replacement of non-toxic cyanide source. This newly proposed synthetic process is highly stable and repeatable under 10 gramme scale counted by benzamide as starting material.

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