Spectroscopic characterization and in vitro studies of biological activity of bradykinin derivatives

• Published in: Scientific reports Vol. 12; no. 1; pp. 19015 - 10
• Main Authors: Proniewicz, Edyta, Burnat, Grzegorz, Domin, Helena, Iłowska, Emilia, Roman, Adam, Prahl, Adam
• Format: Journal Article
• Language: English
• Published: England Nature Publishing Group 08.11.2022; Nature Publishing Group UK; Nature Portfolio
• Subjects: Adsorption; Amino acids; Astrocytoma; Biological activity; Biological properties; Bradykinin; Brain tumors; Drug dosages; Gene expression; Glioma; Gold; Humans; Lung cancer; Lysine carboxypeptidase; Metal Nanoparticles; Nanoparticles; Neurosciences; Peptides; Physiology; Receptor, Bradykinin B1 - genetics; Receptor, Bradykinin B2 - genetics; Small cell lung carcinoma; Transcription Factors; Tumor cell lines; Vibrations
• ISSN: 2045-2322; 2045-2322
• DOI: 10.1038/s41598-022-23448-7

Eleven multiple analogs of bradykinin-a peptide that is a natural ligand of B1 and B2 receptors but does not bind or activate the B1 receptor unless Arg is removed from the sequence by the action of carboxypeptidase N-were synthesized. Their biological activity was examined on T-REx cell lines expressing B1 or B2 receptors using the intracellular IP1 assay. The mRNA expression of B1R and B2R in the lysate of tumor cell lines, e.g., U87-MG (human astrocytoma), SHP-77 (human small cell lung cancer), and H4 (human brain glioma), was determined. For five B1R antagonists, adsorption at the liquid/solid interface (Au nanoparticles (AuNPs) served as the solid surface) was discussed in terms of the vibrations of molecular fragments (structural factors) responsible for the biological properties of these analogs.