Paper presents the interactive computer program "POTENCY" written in BASIC program language, based on the algorithm for classifying biological assays using the assays: "2 + 2" doses, "3 + 3" doses, twin cross-over assay and probit analysis ("2 + 2" doses) described in Yugoslav Pharmacopeia (Ph. Jug. IV). The program execution is presented by assay examples of biological potency calculation described in European Pharmacopeia (Eur. Ph. 1997). The assay-examples have simultaneously been the measure of program execution correctness.
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PvHCt, a 23-amino acid long, histidine-rich peptide derived from shrimp, becomes strongly antimicrobial upon Cu(ii) ion binding. We describe Zn(ii) and Cu(ii) complexes of this peptide, aiming to understand how metal binding and structure correlates to biological activity. Using NMR, UV-vis, CD and FTIR spectroscopies, along with cyclic voltammetry, potentiometry, and DFT calculations, we demonstrate that Cu(ii) binds to the central and C-terminal regions of the peptide, inducing significant structural changes.
View Article and Find Full Text PDFRSC Med Chem
January 2025
Institute of Pharmaceutical Science, King's College London Stamford Street London SE1 9NH UK +44 (0) 20 7848 9532.
-Formyl peptide receptors (FPRs) are membrane receptors that are abundantly expressed in innate immune cells, including neutrophils and platelets, demonstrating potential new targets for immune system regulation and the treatment of inflammatory conditions. We report here the development and bio-physical validation of new FPR imaging agents as effective tools to track FPR distribution, localisation and functions, ultimately helping to establish FPR exact roles and functions in pathological and physiological conditions. The new series of probes feature a small molecule-based FPR address system conjugated to suitable fluorophores, resulting in highly specific FPR agents, including a partial agonist endowed with high affinity ( low/sub-nanomolar potency) on FPR-transfected cells and human neutrophils.
View Article and Find Full Text PDFBMJ Oncol
September 2024
Department of Biochemistry, Southern University of Science and Technology, Shenzhen, Guangdong, China.
Circulating tumour cells (CTCs) and CTC clusters are considered metastatic precursors due to their ability to seed distant metastasis. However, navigating the bloodstream presents a significant challenge for CTCs, as they must endure fluid shear forces and resist detachment-induced anoikis. Consequently, while a large number of cells from the primary tumour may enter the circulation, only a tiny fraction will result in metastasis.
View Article and Find Full Text PDFPLoS One
January 2025
Department of Dental Materials Science, Academic Center for Dentistry (ACTA), University of Amsterdam, Amsterdam, The Netherlands.
Purpose: This study aimed to determine the cytotoxicity (irritant potency) of toothpaste ingredients, of which some had known to have sensitizing properties.
Materials: From the wide variety of toothpaste ingredients, Xylitol, Propylene glycol (PEG), Sodium metaphosphate (SMP), Lemon, Peppermint, Fluoride, Cinnamon, and Triclosan and Sodium dodecyl sulphate (SDS) have been selected for evaluation of their cytotoxic properties.
Methods: Reconstructed human gingiva (RHG) were topically exposed to toothpaste ingredients at different concentrations.
Future Med Chem
January 2025
Department of Chemistry, University of Malakand, Dir Lower, Khyber Pakhtunkhwa, Pakistan.
Background: Due to the divers biological applications of Cu(II) complexes, we in this study reports the various Cu(II) complexes. The study aims to synthesize and assess new Cu(II) complexes as powerful β-glucuronidase inhibitors.
Methods: Five Schiff base ligands and their complexes were synthesized, characterized, and screened against β-glucuronidase inhibitory activity.
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