Angiotensin(1-7)-Stearic Acid Conjugate: Synthesis and Characterization

The novel coronavirus, SARS-CoV-2, broken out as the COVID-19 epidemic, is transported into cytoplasm by angiotensin-converting enzyme-2 (ACE2), a key protein of renin-angiotensin-system (RAS). ACE2 protective that reduces angiotensin (Ang) II, bioactive component RAS, converting it to its potent antagonist, Ang-(1-7) peptide, in order provide pathophysiological response stimuli. Although ACE-2 upregulated especially pulmonary endothelial cells and alveolar epithelial cells, downregulation lung owing loss regulatory factors explains enzyme-dependent lethality SARS-CoV-2. N-terminal domain (NTD) S1, one subunits coronaviruses, known recognize acetylated sialic acids on glycosylated cell surface receptors. In this study, stearic acid-peptide conjugate mimicking acid structure was synthesized, which will be able balance uncontrolled inflammatory excessive cytokine production, depending these suppress pneumonia acute respiratory distress syndrome (ARDS), against It expected fatty acylation would greatly enhance cellular internalization cytosolic distribution peptide through membrane. Thus, we synthesized acyl derivative N-Ac-Gly4-Ang (1-7) peptide. using Fmoc/tBu solid-phase chemistry characterized FT-IR, Zetasizer, LC-ESI-MS. This study provided more detailed insights understanding meeting basic structural requirements for optimal delivery formulation stearyl Ang (1-7)-peptide conjugate.