Effects of C-Terminal-Ethyl-Esterification in a Snake-Venom-Based Peptide Against the Neurotoxicity of Acrolein in PC12 Cells

Enhancing activity of food protein‐derived peptides: An overview of pretreatment, preparation, and modification methods

“…However, esterification can be a useful modification for certain applications, such as enhancing the stability and bioavailability of peptides. There has been some research on the use of esterification modifications of peptides for drug delivery and therapeutic purposes (Bernardes et al, 2023;Li et al, 2021;Tadashi Ogawa et al, 2003;Wang, Qiu, et al, 2017). The lipophilicity of a peptide is a key determinant of its ability to penetrate cell membranes, and lipid solubility is an important factor to consider when evaluating the efficacy of a drug (Steven Ballet et al, 2008).…”

“…The lipophilicity of a peptide is a key determinant of its ability to penetrate cell membranes, and lipid solubility is an important factor to consider when evaluating the efficacy of a drug (Steven Ballet et al, 2008). Esterification can increase the lipophilicity of peptides, leading to improved cellular uptake and ultimately enhancing their bioavailability and potency as therapeutic agents (Bernardes et al, 2023). Methyl esterification of amide bonds is a crucial modification that can modulate biological functions by reducing conformational flexibility and inhibiting the action of protein hydrolases, thereby enhancing peptide stability (Li et al, 2021).…”

“…Methyl esterification of amide bonds is a crucial modification that can modulate biological functions by reducing conformational flexibility and inhibiting the action of protein hydrolases, thereby enhancing peptide stability (Li et al, 2021). In a study by Bernardes et al (2023), ethyl esterification of the Cterminus of a snake venom-based tripeptide (Glu-Val-Trp) resulted in improved neurotrophic and neuroprotective potential compared to the original unmodified peptide. Both Wang, Qiu, et al (2017) andTadashi Ogawa et al (2003) demonstrated that C-terminal esterification of morphine analogs resulted in potent systemic anti-injury effects with decreased tolerability and gastrointestinal side effects and increased bioavailability.…”