While various nucleoside and nucleotide analogs have been approved as anticancer and antiviral drugs, their limitations, including low bioavailability and chemotherapeutic resistance, encourage the development of novel structures. In this context, and motivated by our previous findings on bioactive 3'--substituted xylofuranosyl nucleosides and 5-guanidine xylofuranose derivatives, we present herein the synthesis and biological evaluation of 5'-guanidino furanosyl nucleosides comprising 6-chloropurine and uracil moieties and a 3--benzyl xylofuranosyl unit. The synthetic methodology was based on the glycosylation of a 5-azido 3--benzyl xylofuranosyl acetate donor with the silylated nucleobase and a subsequent one-pot sequential two-step protocol involving Staudinger reduction of the thus-obtained 5-azido uracil and N/N-linked purine nucleosides followed by guanidinylation with ,'-bis(-butoxycarbonyl)-''-triflylguanidine.
View Article and Find Full Text PDFCathinones, a class of synthetic new psychoactive substances (NPSs), continue to emerge and pose public threats. Government control efforts often lead to the emergence of new isomers, which have adverse repercussions on NPSs identification and risk prediction. This work reports on the synthesis and structural characterization of twenty chloro-cathinones, including different isomers, to create analytical data to facilitate their identification in forensic and clinical contexts.
View Article and Find Full Text PDFBackground: The mental health of women is significantly shaped by gender-related issues stemming from social and cultural disparities, which intensify female susceptibility and culminate in mental disorders. Despite a plethora of studies delineating the effects of gender on mental health, there exists a conspicuous deficiency in research investigating women's viewpoints regarding their own experiences of rehospitalization. Therefore, the principal aim of our investigation was to assess the relationship between rehospitalization and the Quality of Life (QoL) among women undergoing treatment at a psychiatric care institution.
View Article and Find Full Text PDFOphthalmol Retina
May 2025
Purpose: To correlate histopathologic findings in an eye with Jalili syndrome with clinical and imaging results available before enucleation.
Design: Case report with histopathologic analysis.
Subjects: Histopathologic analysis of an enucleated eye from a 63-year-old woman diagnosed with Jalili syndrome.
Sphaerococcenol A is a cytotoxic bromoditerpene biosynthesized by the red alga . A series of its analogues (-) was designed and semi-synthesized using thiol-Michael additions and enone reduction, and the structures of these analogues were characterized by spectroscopic methods. Cytotoxic analyses (1-100 µM; 24 h) were accomplished on A549, DU-145, and MCF-7 cells.
View Article and Find Full Text PDFWounds or chronic injuries are associated with high medical costs so, develop healing-oriented drugs is a challenge for modern medicine. The identification of new therapeutic alternatives focuses on the use of natural products. Therefore, the main goal of this study was to evaluate the healing potential and anti-inflammatory mechanism of action of extracts and the main compounds derived from Myrciaria plinioides D.
View Article and Find Full Text PDFNaturally occurring peptides, such as rubiscolins derived from spinach leaves, have been shown to possess some interesting activities. They exerted central effects, such as antinociception, memory consolidation and anxiolytic-like activity. The fact that rubiscolins are potent even when given orally makes them very promising drug candidates.
View Article and Find Full Text PDFMolecules
October 2023
The formulation of magnetic ionic liquids (MILs) or organic salts based on lanthanides as anions has been explored. In this work, a set of choline-family-based salts, and two other, different cation families, were combined with Gadolinium(III) and Terbium(III) anions. Synthetic methodologies were previously optimized, and all organic salts were obtained as solids with melting temperatures higher than 100 °C.
View Article and Find Full Text PDFThis work addresses the potential of the red seaweed as a source of bioactive ingredients for skin health and wellness in response to the growing awareness regarding the significance of sustainable strategies in developing new nature-based dermocosmetic products. Hydroalcoholic extracts from the dried biomass were subjected to sequential liquid-liquid partitions, affording five different fractions (F1-F5). Their cosmetic potential was assessed through a set of in vitro assays concerning their antioxidant, photoprotective, and healing properties.
View Article and Find Full Text PDFThe increase in the life expectancy average has led to a growing elderly population, thus leading to a prevalence of neurodegenerative disorders, such as Parkinson's disease (PD). PD is the second most common neurodegenerative disorder and is characterized by a progressive degeneration of the dopaminergic neurons in the substantia (SNpc). The marine environment has proven to be a source of unique and diverse chemical structures with great therapeutic potential to be used in the treatment of several pathologies, including neurodegenerative impairments.
View Article and Find Full Text PDFGlobal cancer incidence and death are expected to increase to 28 [...
View Article and Find Full Text PDFAge-related macular degeneration (AMD) is the leading cause of severe vision loss and blindness in elderly people worldwide. The damage to the retinal pigment epithelium (RPE) triggered by oxidative stress plays a central role in the onset and progression of AMD and results from the excessive accumulation of reactive oxygen species (ROS) produced mainly by mitochondria. Tumor necrosis factor receptor-associated protein 1 (TRAP1) is a mitochondrial molecular chaperone that contributes to the maintenance of mitochondrial integrity by decreasing the production and accumulation of ROS.
View Article and Find Full Text PDFPolymers (Basel)
January 2023
The marine environment presents itself as a treasure chest, full of a vast diversity of organisms yet to be explored. Among these organisms, macroalgae stand out as a major source of natural products due to their nature as primary producers and relevance in the sustainability of marine ecosystems. Sulfated polysaccharides (SPs) are a group of polymers biosynthesized by macroalgae, making up part of their cell wall composition.
View Article and Find Full Text PDFSeaweeds are a great source of compounds with cytotoxic properties with the potential to be used as anticancer agents. This study evaluated the cytotoxic and proteasome inhibitory activities of 12-hydroxy-bromosphaerol, 12-hydroxy-bromosphaerol, and bromosphaerol isolated from . The cytotoxicity was evaluated on malignant cell lines (A549, CACO-2, HCT-15, MCF-7, NCI-H226, PC-3, SH-SY5Y, and SK-MEL-28) using the MTT and LDH assays.
View Article and Find Full Text PDFThe growing knowledge about the harmful effects caused by some synthetic ingredients present in skincare products has led to an extensive search for natural bioactives. Thus, this study aimed to investigate the dermatological potential of five fractions (F1-F5), obtained by a sequential extraction procedure, from the brown seaweed . The antioxidant (DPPH, FRAP, ORAC and TPC), anti-enzymatic (collagenase, elastase, hyaluronidase and tyrosinase), antimicrobial (, and ), anti-inflammatory (nitric oxide, tumor necrosis factor-α, interleukin-6 and interleukin-10) and photoprotective (reactive oxygen species) properties of all fractions were evaluated.
View Article and Find Full Text PDFPeptides have revealed a large range of biological activities with high selectivity and efficiency for the development of new drugs, including neuroprotective agents. Therefore, this work investigates the neuroprotective properties of naturally occurring peptides, endomorphin-1 (EM-1), endomorphin-2 (EM-2), rubiscolin-5 (R-5), and rubiscolin-6 (R-6). We aimed at answering the question of whether well-known opioid peptides can counteract cell injury in a common in vitro model of Parkinson's disease (PD).
View Article and Find Full Text PDFAntioxidants (Basel)
August 2022
Neurodegenerative diseases are characterized by the progressive degeneration of the neuronal cells and their networks, hampering the function of the central or peripheral nervous system [...
View Article and Find Full Text PDFAntibiotics (Basel)
April 2022
In recent decades, seaweeds have proven to be an excellent source of bioactive molecules. Presently, the seaweed is harvested in a small area of the Portuguese coast exclusively for agar extraction. The aim of this work was to fully disclosure as a sustainable source of antimicrobial ingredients for new dermatological formulations, highlighting its potential to be explored in a circular economy context.
View Article and Find Full Text PDFJ Sci Food Agric
September 2022
Backgroud: In recent years, research on the bioactive properties of macroalgae has increased, due to the great interest in exploring new products that can contribute to improve human health and wellbeing. In the present study, the antioxidant and antimicrobial potential of six different brown algae of the Fucales order were evaluated, namely Ericaria selaginoides, Ericaria amentacea, Gongolaria baccata, Gongolaria usneoides, Cystoseira compressa and Sargassum vulgare (collected along the Mediterranean and Atlantic coasts). The antioxidant capacity was measured by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, the oxygen radical absorbent capacity (ORAC) and the ferric reducing antioxidant power (FRAP) and were related to the total phenolic content (TPC).
View Article and Find Full Text PDFNature has revealed to be a key source of innovative anticancer drugs. This study evaluated the antitumour potential of the marine bromoditerpene sphaerococcenol A on different cancer cellular models. Dose-response analyses (0.
View Article and Find Full Text PDFResulting from the growing human population and the long dependency on fossil-based energies, the planet is facing a critical rise in global temperature, which is affecting all ecosystem networks. With a growing consciousness this issue, the EU has defined several strategies towards environment sustainability, where biodiversity restoration and preservation, pollution reduction, circular economy, and energetic transition are paramount issues. To achieve the ambitious goal of becoming climate-neutral by 2050, it is vital to mitigate the environmental footprint of the energetic transition, namely heavy metal pollution resulting from mining and processing of raw materials and from electronic waste disposal.
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