Dihydrochalcone derivatives as promising antifoulants: synthesis, bioactivity evaluation and performance in coatings.

Marine biofouling presents a major challenge for the maritime industry and marine ecosystems, traditionally managed through biocide-based antifouling (AF) coatings. However, the environmental toxicity of these biocides has intensified the search for sustainable, environmentally friendly alternatives. In this study, a novel approach using flavonoid-based compounds as environmentally safe AF agents is presented.

Unlocking the Role of Metabolic Pathways in Brain Metastatic Disease.

The dissemination of malignant cells to the brain is a late-stage complication of cancer, leading to significant morbidity and mortality. Brain metastases (BM) affect 20-30% of cancer patients, primarily originating from lung cancer, breast cancer, and melanoma. Despite advances in molecular-targeted therapies, brain metastatic disease remains incurable, with a poor median survival of ≤12 months if left untreated.

Spontaneous Intracranial Hypotension in Professional Dancers: A Case Report and Rehabilitation Strategy.

Spontaneous intracranial hypotension (SIH) is a condition caused by a cerebrospinal fluid (CSF) leak, leading to a drop in intracranial pressure. SIH typically results from a spontaneous dural tear, often linked to connective tissue disorders, minor trauma, or repetitive spinal stress. Among dancers, especially in professional ballet, the risk of SIH may be increased by repetitive spinal hyperextension and strenuous movements.

Global functional genomics reveals GRK5 as a cystic fibrosis therapeutic target synergistic with current modulators.

Cystic fibrosis (CF) is a life-shortening disease affecting >160,000 individuals worldwide predominantly with respiratory symptoms. About 80% of individuals with CF have the p.Phe508del variant that causes the CF transmembrane conductance regulator (CFTR) protein to misfold and be targeted for premature degradation by the endoplasmic reticulum (ER) quality control (ERQC), thus preventing its plasma membrane (PM) traffic.

Risk factors affecting the therapeutic effect of onabotulinum toxin a on chronic migraine.

Background: OnabotulinumtoxinA demonstrates effectiveness in chronic migraine prevention but is hindered by variable patient responses. This study aims to identify modifiable and non-modifiable risk factors influencing the response to onabotulinumtoxinA.

Methods: We conducted a retrospective cohort study at a tertiary hospital involving chronic migraine patients treated with onabotulinumtoxinA.

Retinal Capillary Ischemia Following Migraine: A Case Report.

Migraine, a neurological disorder often accompanied by symptoms such as visual disturbances, nausea, and photophobia, involves complex interactions between genetic and environmental factors, while vascular factors are also implicated, influenced by both genetic predisposition and environmental triggers. This case report discusses a 41-year-old male with a history of migraine with visual aura, presenting with sudden left-eye visual loss. Comprehensive ophthalmologic examination revealed a central scotoma, while multimodal imaging, including spectral-domain optical coherence tomography (SD-OCT), showed focal alterations in the outer plexiform layer.

Persulfated Ascorbic Acid Glycoside as a Safe and Stable Derivative of Ascorbic Acid for Skin Care Application.

The pursuit of cosmetic ingredients with proven efficacy and safety that meet consumer needs drives the advancement of new products. Ascorbic acid (AA) is utilized in cosmetic products, predominantly for its potent antioxidant properties. Nonetheless, its instability compromises its efficacy.

A Chemical Toolbox to Unveil Synthetic Nature-Inspired Antifouling (NIAF) Compounds.

The current scenario of antifouling (AF) strategies to prevent the natural process of marine biofouling is based in the use of antifouling paints containing different active ingredients, believed to be harmful to the marine environment. Compounds called booster biocides are being used with copper as an alternative to the traditionally used tributyltin (TBT); however, some of them were recently found to accumulate in coastal waters at levels that are deleterious for marine organisms. More ecological alternatives were pursued, some of them based on the marine organism mechanisms' production of specialized metabolites with AF activity.

Chalcone derivatives as promising antifoulants: Molecular optimization, bioactivity evaluation and performance in coatings.

Marine biofouling remains a huge concern for maritime industries and for environmental health. Although the current biocide-based antifouling coatings can prevent marine biofouling, their use has been associated with toxicity for the marine environment, being urgent to find sustainable alternatives. Previously, our research group has identified a prenylated chalcone (1) with promising antifouling activity against the settlement of larvae of the macrofouling species Mytilus galloprovincialis (EC = 16.

Correction: Palmeira et al. Preliminary Virtual Screening Studies to Identify GRP78 Inhibitors Which May Interfere with SARS-CoV-2 Infection. 2020, , 132.

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Antibacterial Potential of Symmetrical Twin-Drug 3,6-Diaminoxanthones.

Global health faces a significant issue with the rise of infectious diseases caused by bacteria, fungi, viruses, and parasites. The increasing number of multi-drug resistant microbial pathogens severely threatens public health worldwide. Antibiotic-resistant pathogenic bacteria, in particular, present a significant challenge.

Evaluation of Antitumor Activity of Xanthones Conjugated with Amino Acids.

Cancer is a complex disease characterized by several alterations, which confer, to the cells, the capacity to proliferate uncontrollably and to resist cellular death. Multiresistance to conventional chemotherapy drugs is often the cause of treatment failure; thus, the search for natural products or their derivatives with therapeutic action is essential. Chiral derivatives of xanthones (CDXs) have shown potential inhibitory activity against the growth of some human tumor cell lines.

The Role of Natural and Synthetic Flavonoids in the Prevention of Marine Biofouling.

Marine biofouling is a major concern for the maritime industry, environment, and human health. Biocides which are currently used in marine coatings to prevent this phenomenon are toxic to the marine environment, and therefore a search for antifoulants with environmentally safe properties is needed. A large number of scientific papers have been published showing natural and synthetic compounds with potential to prevent the attachment of macro- and microfouling marine organisms on submerged surfaces.

The Synthesis and Characterization of a Delivery System Based on Polymersomes and a Xanthone with Inhibitory Activity in Glioblastoma.

Glioblastoma (GBM) is the most common and deadly primary malignant brain tumor. Current therapies are insufficient, and survival for individuals diagnosed with GBM is limited to a few months. New GBM treatments are urgent.

Polymersomes for Sustained Delivery of a Chalcone Derivative Targeting Glioblastoma Cells.

Glioblastoma (GBM) is a primary malignant tumor of the central nervous system responsible for the most deaths among patients with primary brain tumors. Current therapies for GBM are not effective, with the average survival of GBM patients after diagnosis being limited to a few months. Chemotherapy is difficult in this case due to the heterogeneity of GBM and the high efficacy of the blood-brain barrier, which makes drug absorption into the brain extremely difficult.

Characterization of Progranulin Gene Mutations in Portuguese Patients with Frontotemporal Dementia.

In Portugal, heterozygous loss-of-function mutations in the progranulin () gene account for approximately half of the genetic mediated forms of frontotemporal dementia (FTD). mutations reported thus far cause FTD through a haploinsufficiency disease mechanism. Herein, we aim to unveil the mutation spectrum, investigated in 257 FTD patients and 19 family members from the central/north region of Portugal using sequencing methods.

Structure-Activity Relationship Studies of Chalcones and Diarylpentanoids with Antitumor Activity: Potency and Selectivity Optimization.

We previously reported that chalcone () and diarylpentanoid () induced p53-dependent growth inhibitory activity in human cancer cells. Herein, () and () analogues were designed and synthesized in order to obtain more potent and selective compounds. Compounds , , , , and - caused pronounced in vitro growth inhibitory activity in HCT116 cells (0.

Synthesis and Anti-Inflammatory Evaluation of a Library of Chiral Derivatives of Xanthones Conjugated with Proteinogenic Amino Acids.

In recent decades, the relationship between drug chirality and biological activity has been assuming enormous importance in medicinal chemistry. Particularly, chiral derivatives of xanthones (CDXs) have interesting biological activities, including enantioselective anti-inflammatory activity. Herein, the synthesis of a library of CDXs is described, by coupling a carboxyxanthone () with both enantiomers of proteinogenic amino esters as chiral building blocks (-), following the chiral pool strategy.

The Chemical Space of Marine Antibacterials: Diphenyl Ethers, Benzophenones, Xanthones, and Anthraquinones.

The emergence of multiresistant bacteria and the shortage of antibacterials in the drug pipeline creates the need to search for novel agents. Evolution drives the optimization of the structure of marine natural products to act as antibacterial agents. Polyketides are a vast and structurally diverse family of compounds that have been isolated from different marine microorganisms.

Effect of Indole-Containing Pyrazino[2,1-]quinazoline-3,6-diones in the Virulence of Resistant Bacteria.

Drug resistance is rising to alarming levels, constituting one of the major threats to global health. The overexpression of efflux pumps and the formation of biofilms constitute two of the most common resistance mechanisms, favoring the virulence of bacteria. Therefore, the research and development of effective antimicrobial agents that can also counteract resistance mechanisms are extremely important.

3,4-Dioxygenated xanthones as antifouling additives for marine coatings: in silico studies, seawater solubility, degradability, leaching, and antifouling performance.

Marine biofouling pollution is a process that impacts ecosystems and the global economy. On the other hand, traditional antifouling (AF) marine coatings release persistent and toxic biocides that accumulate in sediments and aquatic organisms. To understand the putative impact on marine ecosystems of recently described and patented AF xanthones (xanthones 1 and 2), able to inhibit mussel settlement without acting as biocides, several in silico environmental fate predictions (bioaccumulation, biodegradation, and soil absorption) were calculated in this work.

Antitumor Effect of Chalcone Derivatives against Human Prostate (LNCaP and PC-3), Cervix HPV-Positive (HeLa) and Lymphocyte (Jurkat) Cell Lines and Their Effect on Macrophage Functions.

Chalcones are synthetic and naturally occurring compounds that have been widely investigated as anticancer agents. In this work, the effect of chalcones - against the metabolic viability of cervical (HeLa) and prostate (PC-3 and LNCaP) tumor cell lines was tested, to compare the activity against solid and liquid tumor cells. Their effect was also evaluated on the Jurkat cell line.

Absolute Stereochemistry Determination of Bioactive Marine-Derived Cyclopeptides by Liquid Chromatography Methods: An Update Review (2018-2022).

Cyclopeptides are considered as one of the most important classes of compounds derived from marine sources, due to their structural diversity and a myriad of their biological and pharmacological activities. Since marine-derived cyclopeptides consist of different amino acids, many of which are non-proteinogenic, they possess various stereogenic centers. In this respect, the structure elucidation of new molecular scaffolds obtained from natural sources, including marine-derived cyclopeptides, can become a very challenging task.