Identification of benzothiazole derived monosaccharides as potent, selective, and orally bioavailable inhibitors of human and mouse galectin-3; a rare example of using a S···O binding interaction for drug design.

As a result of our continued efforts to pursue Gal-3 inhibitors that could be used to fully evaluate the potential of Gal-3 as a therapeutic target, two novel series of benzothiazole derived monosaccharides as potent (against both human and mouse Gal-3) and orally bioavailable Gal-3 inhibitors, represented by 4 and 5, respectively, were identified. These discoveries were made based on proposals that the benzothiazole sulfur atom could interact with the carbonyl oxygen of G182/G196 in h/mGal-3, and that the anomeric triazole moiety could be modified into an N-methyl carboxamide functionality. The interaction between the benzothiazole sulfur and the carbonyl oxygen of G196 in mGal-3 was confirmed by an X-ray co-crystal structure of early lead 9, providing a rare example of using a S···O binding interaction for drug design. It was found that for both the series, methylation of 3-OH in the monosaccharides caused no loss in h & mGal-3 potencies but significantly improved permeability of the molecules.

Antimicrobial activity and structure-activity relationships of molecules containing mono- or di- or oligosaccharides: An update.

Bacterial infections are the second leading cause of death worldwide, and the evolution and widespread distribution of antibiotic-resistance elements in bacterial pathogens exacerbate the threat crisis. Carbohydrates participate in bacterial infection, drug resistance and the process of host immune regulation. Numerous antimicrobials derived from carbohydrates or contained carbohydrate scaffolds that are conducive to an increase in pathogenic bacteria targeting, the physicochemical properties and druggability profiles. In the paper, according to the type and number of sugar residues contained in antimicrobial molecules collected from the literatures ranging from 2014 to 2024, the antimicrobial activities, action mechanisms and structure-activity relationships were delineated and summarized, for purpose to provide the guiding template to select the type and size of sugars in the design of oligosaccharide-based antimicrobials to fight the looming antibiotic resistance crisis.

Advances in the regulation of radiation-induced apoptosis by polysaccharides: A review.

Polysaccharides are biomolecules composed of monosaccharides that are widely found in animals, plants and microorganisms and are of interest for their various health benefits. Cumulative studies have shown that the modulation of radiation-induced apoptosis by polysaccharides can be effective in preventing and treating a wide range of radiation injuries with safety and few side effects. Therefore, this paper summarizes the monosaccharide compositions, molecular weights, and structure-activity relationships of natural polysaccharides that regulate radiation-induced apoptosis, and also reviews the molecular mechanisms by which these polysaccharides modulate radiation-induced apoptosis, primarily focusing on promoting cancer cell apoptosis to enhance radiotherapy efficacy, reducing radiation damage to normal tissues, and inhibiting apoptosis in normal cells. Additionally, the role of gut microbiota in mediating the interaction between polysaccharides and radiation is discussed, providing innovative ideas for various radiation injuries, including hematopoiesis, immunity, and organ damage. This review will contribute to a better understanding of the value of natural polysaccharides in the field of radiation and provide guidance for the development of natural radioprotective agents and radiosensitizers.

Glaucoma de ángulo cerrado secundario a topiramato / Angle-closure glaucoma secondary to topiramate use

Caso clínico: Se presenta el caso de una mujer de 42 años que desarrolló un cuadro de miopía aguda y glaucoma de ángulo cerrado bilateral una semana después del inicio del tratamiento con topiramato. La biomicroscopía ultrasónica (BMU) reveló que la paciente presentaba un ángulo cerrado y una efusión coroidea bilateral. Con la retirada del fármaco se resolvió el cuadro. Discusión: El topiramato puede desencadenar miopía aguda y glaucoma de ángulo cerrado en algunos pacientes debido a una efusión coroidea. La realización de la BMU parece ser una herramienta útil para observar la evolución del cuadro y su resolución tras la suspensión del fármaco(AU)

Case report: We describe a 42 year-old patient who developed acute myopia and closed-angle glaucoma one week after beginning treatment with topiramate. Ultrasound biomicroscopy revealed a bilateral angle closure and choroidal effusion. The clinical findings resolved with withdrawal of the topiramate. Discussion: Topiramate may cause acute myopia and closure angle glaucoma in some patients due to a choroidal effusion. Ultrasound biomicroscopy seems to be a useful tool for monitoring the progression of the clinical lesions and their resolution when the drug is withdrawn(AU)

Sugar inhibition of the lectin jacalin: comparison of three assays

1. Three assays were used to test nine sugars for inhibition of jacalin activity prepared from Artocarpus intefrifolia. Rat spleen proliferation was unssuitable since the measurement of the effects of sugars against jacalin binding was complicated by their simultaneous metavolic effects on the cells. 2. Based partly on a sheep red blood cell hemagglutination assay and mainly on human serum protein preciptation, the following potencies in relation to D(+)-galactose (taken as 1) were obtained: 1-0-methyl-alfa-D-galactopyranoside, 40; methyl-alfa-D-mannopyranoside and D(+)-mannose, 0.12; ß-Dd-(-)-fructose, 0.08; alfa - D(+)-glucose and 1 - 0-methyl-ß-D-glucopyranoside, <0.04