Microfluidics-enabled core/shell nanostructure assembly: Understanding encapsulation processes via particle characterization and molecular dynamics.

In the realm of hybrid nanomaterials, the construction of core/shell nanoparticles offer an effective strategy for encompassing a particle by a polymeric or other suitable material, leading to a nanocomposite with distinct features within its structure. The polymer shell can be formed via nanoprecipitation, optimized by manipulating fluid flow, fluid mixing, modulating device features in microfluidics. In addition to the process optimization, success of polymer assembly in encapsulation strongly lies upon the favorable molecular interactions originating from the diverse chemical environment shared between core and shell materials facilitating formation of core/shell nanostructure.

Synthesis of Unprotected Racemic Tryptophan Derivatives Using Gramine via Nickel(II) Complex.

A chemical method for the preparation of nonprotected tryptophan via nickel(II) complexes under simple operating conditions was established. The carefully designed nickel(II) glycinates are inexpensive and can be quantitatively recovered releasing the target tryptophans in high yield. The method has a wide range of synthesis generality, allowing the preparation of various substituted tryptophans.

Enhancement of Transdermal Drug Delivery: Integrating Microneedles with Biodegradable Microparticles.

This investigation aimed to enhance transdermal methotrexate delivery through human skin by employing Dr. Pen microneedles and poly(d,l-lactide--glycolide) acid microparticles formulated from eight polymer grades (Expansorb DLG 95-4A, DLG 75-5A, DLG 50-2A, DLG 50-5A, DLG 50-8A, DLG 50-6P, DLG 50-7P, and DLL 10-15A). A comprehensive characterization of the microparticles was performed, encompassing various parameters such as size, charge, morphology, microencapsulation efficiency, yield, release kinetics, and chemical composition.

Design, synthesis, and studies of new quinazolinones tagged thiophene, thienopyrimidine, and thienopyridine scaffolds as antiproliferative agents with potential p38α MAPK kinase inhibitory effects.

The current work focuses on the creation of novel derivatives of the quinazolinone ring system, with various substituted thiophene, thienopyrimidine, and thienopyridine scaffolds 3a,b-11. Employing the standard MTT assay, every target compound's antiproliferative efficacy was evaluated in comparison with doxorubicin against both normal WI-38 cells and various cancer cell lines. Derivatives 6, 8a, and 8b demonstrated the most potent activity, alongside their safety profiles against WI-38.

Drug-Loaded Hydrogel Microneedles for Sustainable Transdermal Delivery of Macromolecular Proteins.

Introduction: Poly(methyl vinyl ether co-maleic acid) (PMVE/MA) hydrogel microneedles (HMN) are investigated for transdermal delivery of macromolecular drugs owing to their biocompatibility and super-swelling properties. However, the drug delivery efficacy reduces with increasing molecular weight due to the entrapment within the HMN matrices. Furthermore, integrating external drug reservoirs extends the drug diffusion path and reduces the efficiency of drug permeation.

Stabilizing effect of HP-β-CD on infliximab in liquid formulations and a solid formulation produced by electrospinning.

The development of stable biopharmaceutical formulations, such as monoclonal antibodies, poses a great challenge in the pharmaceutical industry. This study investigated the stabilizing effect of 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) in liquid and solid formulations of infliximab during processing and storage. The solid formulation was produced by a scaled-up high-speed electrospinning method, resulting in a product suitable for reconstitution with excellent dissolution properties.

and antimalarial activities of the ethanol extract of stem bark used for the treatment of malaria in the Western Region of Cameroon.

Background: Malaria is one of the leading causes of morbidity and/or mortality in tropical Africa. The spread and development of resistance to chemical antimalarial drugs and the relatively high cost of the latter are problems associated with malaria control and are reasons to promote the use of plants to meet healthcare needs to treat malaria. The aim of this study was to evaluate antiplasmodial activities of extracts of (Mah quat), which is traditionally used for the treatment of malaria in the western region of Cameroon.

Comparison of physico-chemical properties of different types of orthopedic acrylic cement.

Analyzing the chemical composition of different kinds of acrylic cement is necessary to understand their properties and suitability for curing bone defects. Conducting various chemical tests can give valuable insight into the composition, viscosity, and performance characteristics of each kind of cement, Therefore, our study aimed to find safety standards and the effectiveness of these products for medical applications. The polymeric characterization was determined by Nuclear Magnetic Resonance (H-NMR) spectroscopy and Fourier-transform infrared spectroscopy (FTIR).

Assessing the effect of sunlight exposure and reuse of polyethylene terephthalate bottles on phthalate migration.

Nowadays, polyethylene terephthalate (PET) bottles are widely used for packaging drinks and food. However, concerns have been raised about the possible migration of harmful chemicals, particularly phthalates, from these containers into their contents. Therefore, this study investigates the effects of sunlight exposure and PET bottle reuse on phthalate migration, focusing on three common phthalates: bis(2-ethylhexyl) phthalate (DEHP), dibutyl phthalate (DBP), and benzyl butyl phthalate (BBP).

Asiatic acid methyl ester, a new asiaticoside derivative, induces osteogenic differentiation of hPDLCs.

Objective: Asiaticoside has the capacity to induce osteogenic differentiation of human periodontal ligament cells (hPDLCs) through Wnt (Wingless-related integration site) signaling. A modified chemical structure (by removing glycoside side chain), referred to as asiatic acid methyl ester (AA1), has been constructed and evaluated for its capacity to induce osteogenic differentiation.

Design: hPDLCs viability was determined by MTT assay.

Design, Synthesis, and Unprecedented Interactions of Covalent Dipeptide-Based Inhibitors of SARS-CoV-2 Main Protease and Its Variants Displaying Potent Antiviral Activity.

The main protease (M) of SARS-CoV-2 is a key drug target for the development of antiviral therapeutics. Here, we designed and synthesized a series of small-molecule peptidomimetics with various cysteine-reactive electrophiles. Several compounds were identified as potent SARS-CoV-2 M inhibitors, including compounds (IC = 0.

Safety Assessment of Graphene-Based Materials.

Graphene is the first 2D atomic crystal, and its isolation heralded a new era in materials science with the emergence of several other atomically thin materials displaying multifunctional properties. The safety assessment of new materials is often something of an afterthought, but in the case of graphene, the initial isolation and characterization of the material was soon followed by the assessment of its potential impact on living systems. The Graphene Flagship project addressed the health and environmental aspects of graphene and other 2D materials, providing an instructive lesson in interdisciplinarity - from materials science to biology.

Melatonin induces drought stress tolerance by regulating the physiological mechanisms, antioxidant enzymes, and leaf structural modifications in L.

Melatonin is considered an effective bio-stimulant that is crucial in managing several abiotic stresses including drought. However, its potential mechanisms against drought stress in fragrant roses are not well understood. Here, we aim to investigate the role of melatonin on plants cultivated under drought stress (40 % field capacity) and normal irrigation (80 % field capacity).

Complexed hyaluronic acid-based nanoparticles in cancer therapy and diagnosis: Research trends by natural language processing.

Hyaluronic acid (HA) is a popular surface modifier in targeted cancer delivery due to its receptor-binding abilities. However, HA alone faces limitations in lipid solubility, biocompatibility, and cell internalization, making it less effective as a standalone delivery system. This comprehensive study aimed to explore a dynamic landscape of complexation in HA-based nanoparticles in cancer therapy, examining diverse aspects from influential modifiers to emerging trends in cancer diagnostics.

Expanding the Chemical Space of Reverse Fosmidomycin Analogs.

Multidrug-resistant pathogens pose a major threat to human health, necessitating the identification of new drug targets and lead compounds that are not susceptible to cross-resistance. This study demonstrates that novel reverse thia analogs of the phosphonohydroxamic acid antibiotic fosmidomycin inhibit 1-deoxy-d-xylulose 5-phosphate reductoisomerase (DXR), an essential enzyme for , , and that is absent in humans. Some novel analogs with large α-phenyl substituents exhibited strong inhibition across these three DXR orthologues, surpassing the inhibitory activity of fosmidomycin.

A versatile entry to unnatural, disulfide-linked amino acids and peptides through the disulfuration of azlactones.

Despite the evident demand and promising potential of disulfide-functionalized amino acids and peptides in linker chemistry and peptide drug discovery, those disulfurated specifically at the α-position constitute a unique yet rather highly underexplored chemical space. In this study, we have developed a method for preparing -linked amino acid/peptide derivatives through a base-catalyzed disulfuration reaction of azlactones, followed by the ring-opening functionalization. The disulfuration reaction proceeds under mild conditions, yielding disulfurated azlactones in excellent yields across a variety of -dithiophthalimides and diverse azlactones derived from various amino acids and peptides.

Design, Synthesis, and Pharmacological Evaluation of Nonsteroidal Tricyclic Ligands as Modulators of GABA Receptors.

GABA receptors (GABARs) are the major elements of inhibitory neurotransmission in the central nervous system (CNS). They are established targets for regulation by endogenous brain neuroactive steroids (NASs) such as pregnanolone. However, the complexity of de novo synthesis of NAS derivatives has hindered attempts to circumvent the principal limitations of using endogenous NASs, including selectivity and limited oral bioavailability.

Exploring the neuroprotective benefits of phytochemicals extracted from indigenous edible fruits in Bangladesh.

The increasing incidence of neurodegenerative diseases (NDs) and the constraints of existing treatment methods have spurred a keen interest in investigating alternative therapies. Medicinal plants, renowned for their long-standing use in traditional medicine, offer a hopeful avenue for discovering new neuroprotective agents. This study emphasizes the potential neuroprotective characteristics of edible fruit plants in Bangladesh, specifically focusing on their traditional folk medicine uses for neurological disorders.

Harnessing the tumor microenvironment: targeted cancer therapies through modulation of epithelial-mesenchymal transition.

The tumor microenvironment (TME) is integral to cancer progression, impacting metastasis and treatment response. It consists of diverse cell types, extracellular matrix components, and signaling molecules that interact to promote tumor growth and therapeutic resistance. Elucidating the intricate interactions between cancer cells and the TME is crucial in understanding cancer progression and therapeutic challenges.

Preclinical and First-in-Human Study of a Compact Radionuclide Labeled Self-Assembly Nanomedicine for Chemo-Radio-Theranostics of Cancer.

The emerging combination of chemotherapy and radionuclide therapy has been actively investigated to overcome the limitations of monotherapy and augment therapeutic efficacy. However, it remains a challenge to design a single delivery vehicle that can incorporate chemotherapeutics and radionuclides into a compact structure. Here, a chelator DOTA- or NOTA-modified Evans blue conjugated camptothecin molecule (EB-CPT) nanoprodrug was synthesized, which could self-assemble into nanoparticles due to its inherent amphiphilicity.

Substituted piperazine conjugated to quinoline-thiosemicarbazide as potent α-glucosidase inhibitors to target hyperglycemia.

Diabetes mellitus, particularly type 2 diabetes, is a growing global health challenge characterized by chronic hyperglycemia due to insulin resistance. One therapeutic approach to managing this condition is the inhibition of α-glucosidase, an enzyme involved in carbohydrate digestion, to reduce postprandial blood glucose levels. In this study, a series of thiosemicarbazide-linked quinoline-piperazine derivatives were synthesized and evaluated for their α-glucosidase inhibitory activity, to identify new agents for type 2 diabetes management.

Discovery and mechanistic exploration of promiscuous xylosyltransferase based on protein engineering.

Glycosylation is an effective means to alter the structure and properties of plant compounds, influencing the pharmacological activity of natural products (NPs) to obtain highly active NPs. In nature, glucosides are the most widely distributed, while other glycosides such as xylosides are less common and present in lower quantities. This is due to the scarcity of xylosyltransferases with substrate promiscuity in nature, and the modification of their catalytic function is also quite challenging.

Identification of a Chemical Probe for BLT2 Activation by Scaffold Hopping.

The leukotriene B4 receptor 2 (BLT2) is a G-protein coupled receptor, which is endogenously activated by 12()-hydroxyheptadeca-5Z,8E,10E-trienoic acid (12-HHT). BLT2 is gaining attention as a potential therapeutic target involved in various pathologies including diabetic wound healing, ophthalmic diseases, and colitis. However, validation of BLT2 as drug target requires chemical probes and pharmacological tools which will allow for application in vivo.

Exploring the Anticancer Effect of on Colorectal Cancer: Insights From Eight Colorectal Cancer Cell Lines.

Colorectal cancer (CRC) is a prevalent and deadly disease, necessitating the exploration of novel therapeutic strategies. Traditional chemotherapy often encounters drug resistance and adverse side effects, highlighting the need for alternative approaches. , a plant rich in phytochemical constituents, was investigated for its potential as an anticancer agent against colorectal cancer (CRC).