24,111 results match your criteria: "Faculty of Chemical and Pharmaceutical Sciences; University of Chile[Affiliation]"

An overview of additive manufacturing strategies of enzyme-immobilized nanomaterials with application incatalysis and biomedicine.

Int J Biol Macromol

December 2024

School of Chemical Engineering, Yeungnam University, 280 Daehak-ro, Gyeongsan 38541, South Korea; Research Institute of Cell Culture, Yeungnam University, 280 Daehak-ro, Gyeongsan 38541, South Korea. Electronic address:

Meticulous and bespoke fabrication of structural materials with simple yet innovative outlines along with on-demand availability is the imperative aspiration for numerous fields. The alliance between nanotechnology and enzymes has led to the establishment of an inimitable and proficient class of materials. With the advancement in the field of additive manufacturing, the fabrication of some complex biological architects is achievable with similitude to the instinctive microenvironment of the biological tissue.

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Sesamolin possesses limited aqueous solubility, a drawback for biological activity study in cancer cell models. This study aimed to enhance sesamolin's ability to fight cancer, as it is a bioactive compound with low water solubility found in sesame. We developed different Pickering emulsion delivery systems and tested their anticancer effects on various cancer cell types.

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Quinoline-thiosemicarbazone-1,2,3-triazole-acetamide derivatives as new potent α-glucosidase inhibitors.

Sci Rep

December 2024

Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran.

In this work, a novel series of quinoline-thiosemicarbazone-1,2,3-triazole-aceamide derivatives 10a-n as new potent α-glucosidase inhibitors was designed, synthesized, and evaluated. All the synthesized derivatives 10a-n were more potent than acarbose (positive control). Representatively, (E)-2-(4-(((3-((2-Carbamothioylhydrazineylidene)methyl)quinolin-2-yl)thio)methyl)-1H-1,2,3-triazol-1-yl)-N-phenethylacetamide (10n), as the most potent entry, with IC = 48.

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Luliconazole (LCZ) is a topical imidazole antifungal agent with broad-spectrum activity. However, LCZ encounters challenges such as low aqueous solubility, skin retention, and penetration, which reduce its dermal bioavailability and hinder its efficacy in drug delivery. The aim of the present study was to formulate, characterize, and evaluate the in vitro antifungal efficacy of luliconazole-loaded nanostructured lipid carriers (LCZ-NLCs) against a panel of resistant fungal strains.

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Citric acid is more effective than sodium thiosulfate in chelating calcium in a dissolution model of calcinosis.

Sci Rep

December 2024

Division of Musculoskeletal and Dermatological Sciences, School of Biological Sciences, Faculty of Biology, Medicine and Health, The University of Manchester and Northern Care Alliance NHS Foundation Trust, Manchester Academic Health Science Centre, Manchester, M13 9PT, UK.

Calcinosis cutis affects 20-40% of patients with systemic sclerosis. This study tests the hypothesis that calcium-chelating polycarboxylic acids can induce calcium dissolution without skin toxicity or irritancy. We compared citric acid (CA) and ethylenediaminetetraacetic acid (EDTA) to sodium thiosulfate (STS) for their ability to chelate calcium in vitro using a pharmaceutical dissolution model of calcinosis (hydroxyapatite (HAp) tablet), prior to evaluation of toxicity and irritancy in 2D in vitro skin models.

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Development and Discovery of a Selective Degrader of Casein Kinases 1 δ/ε.

J Med Chem

January 2025

Institute of Pharmaceutical Chemistry, Goethe University, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.

Members of the casein kinase 1 (CK1) family have emerged as key regulators of cellular signaling and as potential drug targets. Functional annotation of the 7 human isoforms would benefit from isoform-selective inhibitors, allowing studies on the role of these enzymes in normal physiology and disease pathogenesis. However, due to significant sequence homology within the catalytic domain, isoform selectivity is difficult to achieve with conventional small molecules.

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A new antioxidant lipid (AL) was synthesized from rainbow trout () belly oil and cold-pressed maqui (CPM) ( (Mol.) Stuntz) seed oil via enzymatic interesterification using in supercritical CO medium. A Box-Behnken design with 15 experiments was employed, with the independent variables being the following: belly oil/CPM oil ratio (10/90, 50/50, and 90/10, /), supercritical CO temperature (40.

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Hepatocellular carcinoma (HCC) is the most common form of liver cancer in humans, with an increasing incidence worldwide. The current study aimed to explore the molecular mechanisms that inhibit the proliferation of HepG2 cells, a hepatoblastoma-derived cell line. MSC-derived exosomes (UC-MSCs) were prepared with a median particle size (N50) of 135.

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Brown adipocytes are characterized by a high abundance of mitochondria, allowing them to consume fatty acids for heat production. Increasing the number of brown adipocytes is considered a promising strategy for combating obesity. However, the molecular mechanisms underlying their differentiation remain poorly understood.

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Background: Immunotherapy, including the use of immune checkpoint inhibitors such as nivolumab, is increasingly common in cancer treatment and can lead to various immune-related adverse effects, including rare cases of diabetic ketoacidosis. This case report highlights an unique instance of nivolumab-induced diabetic ketoacidosis in a patient without prior history of diabetes, emphasizing the importance of careful monitoring even in those without traditional risk factors.

Case Presentation: We report a case of a 70-year-old Caucasian male with metastatic esophageal adenocarcinoma who developed diabetic ketoacidosis 3 weeks after stopping nivolumab therapy.

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Article Synopsis
  • The study analyzed 76 sediment samples from the Persian Gulf and Oman Sea, focusing on the concentrations of 18 PCB congeners.
  • The highest concentration was PCB-52 at 636.1 pg/g dw in the Oman Sea, while PCB-28 reached 139.0 pg/g dw in the Persian Gulf.
  • Overall, both regions showed PCB levels within acceptable limits, though the T11S3-2 station in the Oman Sea presented a medium risk due to elevated PCB concentrations, still remaining lower than global urban and industrial levels.
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Objectives: To examine the association between maternal plasma cotinine concentrations during pregnancy and attention-deficit/hyperactivity disorder (ADHD) related characteristics in children.

Design: Prospective birth cohort study from the Hokkaido Study on Environment and Children's Health.

Setting: Hokkaido, Japan.

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Poly(lactide-co-glycolide) (PLG) nanoparticles loaded with doxorubicin have reached phase-I clinical trials for treating advanced solid tumors. This study explores cell hitchhiking, where nanoparticles associate with blood cells and investigates the impact on pharmacokinetics and tumor migration. Previous findings highlighted the early post-injection phase dominated by nonspecific nanoparticle-cell interactions and burst release.

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Mushrooms have proven to be a valuable source of diverse bioactive compounds that can hold substantial potential for preventing and managing various diseases. This research focused on examining the numerous bioactive compounds found in () (Cooke & Massee) Priest mushrooms, particularly those obtained from ethyl acetate and dichloromethane extracts. Polyphenols, flavonoids, tannins, and alkaloids were also evaluated by chemical analysis.

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TKK130 is a 3-Hydroxy-Propanamidine (HPA) with Potent Antimalarial Activity and a High Barrier to Resistance.

J Med Chem

January 2025

Heinrich Heine University Düsseldorf, Faculty of Mathematics and Natural Sciences, Institute of Pharmaceutical and Medicinal Chemistry, Universitätsstr. 1, 40225 Düsseldorf, Germany.

Malaria continues to pose a significant burden on populations in endemic areas and requires innovative treatment options. Here, we report the synthesis and preclinical evaluation of the novel 3-hydroxypropanamidine (HPA) , which shows excellent antiplasmodial activity against drug-sensitive and -resistant strains. Moreover, in various human cell lines, the compound shows no cytotoxicity and excellent parasite selectivity.

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Isolation, Structure Elucidation, and Bioactivity Evaluation of Two Alkaloids From H. Stem: A Traditional Medicinal Spice and Its Chemico-Pharmacological Aspects.

Food Sci Nutr

December 2024

Key Laboratory of Joint Diagnosis and Treatment of Chronic Liver Disease and Liver Cancer of Lishui, Central Laboratory of The Lishui Hospital of Wenzhou Medical University The First Affiliated Hospital of Lishui University, Lishui People's Hospital Lishui Zhejiang China.

Bangladesh is endowed with an abundance of excellent medicinal plant resources. A well-known traditional medicinal plant H. from the Piperaceae family is rich in bioactive phytochemicals that have antidiarrheal, antimicrobial, analgesic, antioxidant, anticancer, and cytotoxic effects.

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The biosynthesis of nanomaterials is a vast and expanding field of study due to their applications in a variety of fields, particularly the pharmaceutical and biomedical fields. Various synthetic routes, including physical and chemical methods, have been developed in order to generate metal nanoparticles (NPs) with definite shapes and sizes. In this review, focused on the recent advancements in the green synthetic methods for the generation of silver, zinc and copper NPs with simple and eco-friendly approaches and the potential of the biosynthesized metal and metal oxide NPs as alternative and therapeutic agent for the treatment of inflammatory diseases.

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Background: The utilization of PD1 and CTLA4 inhibitors has revolutionized the treatment of malignant melanoma (MM). However, resistance to targeted and immune-checkpoint-based therapies still poses a significant problem.

Objective: Here, we mine large-scale MM proteogenomic data to identify druggable targets and forecast treatment efficacy and resistance.

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New benzimidazole-indole-amide derivatives as potent α-glucosidase and acetylcholinesterase inhibitors.

Arch Pharm (Weinheim)

January 2025

Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran.

New derivatives 6a-m with benzimidazole-indole-amide scaffold were developed, synthesized, and assessed for potential inhibitory effects on α-glucosidase and acetylcholinesterase (AChE). These compounds were synthesized by various amine derivatives. With the exception of two compounds, the α-glucosidase inhibitory activities of the title derivatives were more than that of the positive control acarbose.

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Arketamine alleviates cognitive impairments and demyelination in mice with postoperative cognitive dysfunction via TGF-β1 activation.

Prog Neuropsychopharmacol Biol Psychiatry

January 2025

Chiba University Center for Forensic Mental Health, Chiba 260-8670, Japan; Department of Anesthesiology, Pain and Perioperative Medicine, The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, China. Electronic address:

Postoperative cognitive dysfunction (POCD) is characterized by a decline in cognitive functions, including memory, attention, and executive abilities, following surgery, with no effective therapeutic drugs currently available. Arketamine, the (R)-enantiomer of ketamine, has shown promise in mitigating cognitive deficits in animal models. In this study, we investigated whether arketamine could ameliorate cognitive deficits in a mouse model of POCD, with a focus on the role of transforming growth factor (TGF)-β1 in its effects.

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The treatment of effluents from the pharmaceutical industry currently remains a major challenge due to their impact on the environment and public health along with the cost of treatments. Considering these issues, our work focused on the development of materials with effective adsorption properties to treat industrial effluents based on locally available and inexpensive clays and zeolite. Local Algerian kaolin (Djebel Debbagh), palygorskite (Ghoufi) and zeolite (Tinbdar) were treated thermally and chemically prior to synthesis into mesoporous materials of hexagonal structure using pluronic P123 as surfactant.

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Anti-inflammatory and antinociceptive effects of LQFM275 - A new multi-target drug.

Int Immunopharmacol

January 2025

Laboratory of Pharmacology of Natural and Synthetic Products, Institute of Biological Sciences, Federal University of Goiás, Campus Samambaia, Goiânia, Brazil.

Compound (4-(3,5-di-tert-butyl-4-hydroxybenzylamine)benzenesulfonamide) (LQFM275) was designed and synthesized from darbufelone and sulfanilamide as a new multi-target for the treatment of inflammatory diseases. LQFM275 showed a great range of safe cytotoxicity profile (100-400 μM) evaluated by MTT assay, preventing damage induced by lipopolysaccharide (LPS) in EA.hy926 cell line.

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Many plants are reported to enhance cognition in amnesic-animal models. The metabolite profile of fruit methanolic extract (CDFME) was characterized by LC-QTOF-MS/MS, and its total phenolics content (TPC) and total flavonoids content (TFC) were determined. In parallel, its cognitive-enhancing effect on scopolamine (SCOP)-induced AD in rats was evaluated.

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Chemical composition, antimicrobial, and antioxidant properties of essential oils from asso. and caball. from Morocco: and evaluation.

Front Chem

December 2024

Laboratory of Spectroscopy, Molecular Modelling, Materials, Nanomaterial, Water and Environment, CERNE2D, Mohammed V University in Rabat, Faculty of Science, Rabat, Morocco.

Introduction: Morocco is home to a remarkable diversity of flora, including several species from the Artemisia genus. This study aims to thoroughly examine the chemical composition of essential oils derived from Artemisia species and assess their antibacterial and antioxidant properties through in vitro experiments and in silico simulations.

Methods: Samples of Artemisia herba-alba Asso.

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Novel flame retardants (NFRs) in e-waste: Environmental burdens, health implications, and recommendations for safety assessment and sustainable management.

Toxicology

December 2024

Helmholtz Centre for Environmental Research - UFZ, Department Ecotoxicology, Leipzig, Germany; Entity of In Vitro Toxicology and Dermato-Cosmetology, Department of Pharmaceutical and Pharmacological Sciences, Faculty of Medicine and Pharmacy, Vrije Universiteit Brussel, Brussels, Belgium.

Novel flame retardants (NFRs) have emerged as chemicals of environmental health concern due to their widespread use as an alternative to polybrominated diphenyl ethers (PBDE) in electrical and electronic devices. Humans and ecosystems are under threat because of e-waste recycling procedures that may emit NFRs and other anthropogenic chemicals into the e-waste workplace and the surrounding environment. The individual toxicity of NFRs including novel brominated flame retardants (NBFRs), their combined effects and the underlying mechanisms of toxicity have remained poorly understood.

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