Wang, Tong; Meng, Qian; Lin, Lan; Yang, Li; Zhao, Wenjiao; Sun, Dequn published the artcile< Self-assembled dehydropeptide nanocarrier as a delivery system for antitumor drug temozolomide>, Formula: C19H34O2, the main research area is glioblastoma cell antitumor dehydropeptide nanocarrier temozolomide; Dehydropeptide; Drug delivery; Nanocarrier; Self-assembly; Temozolomide.
Stable mol. conformation and intermol. forces are essential for peptide self-assembly. In this study, one novel dehydropeptide (DDP) monomer (Boc-(Z)Cα,b-ΔPhe-Gly-NHMe, DDP 1) was prepared; its conformation was confirmed to be more stable than the normal peptide 2 by NMR (NMR) and X-ray crystal diffraction experiments DDP 1 was self-assembled to one novel dehydropeptide nanomaterial (DDPN 1). Fourier transform IR (FTIR) spectroscopy results showed that hydrogen bonding was the main driving force of self-assembly. Electron microscope images displayed that the DDPN 1 fibers were longer and more stable than peptide 2 nanomaterials. Results of cell activity and enzyme hydrolysis proved that DDPN 1 had excellent biocompatibility and resistance to the enzymic hydrolysis of protease K. Therefore, the DDPN 1 was used to load the antitumor drug temozolomide (TMZ). Due to intermol. hydrogen bonds formed between TMZ and DDPN 1, TMZ-loaded DDPN 1 had a high percent entrapment efficiency (EE) of 83.72 ± 4.30% (n = 8) and a percent drug loading efficiency (LE) of 6.70 ± 0.34% (n = 8), and the half-life of TMZ-loaded DDPN 1 was 2.5-3 times longer than that of TMZ at pH 7. The in vitro cell viability results revealed that TMZ-loaded DDPN 1 exhibited higher antitumor activity (IC50 = 552.1 μM) against U118-MG than that of TMZ (IC50 = 1980.1 μM), possibly because that U118-MG cells uptook more TMZ from TMZ-loaded DDPN 1 than from free TMZ directly. This study is expected to inspire the design of biocompatible nanocarriers applied for anti-enzymic hydrolysis in drug delivery systems.
Bioorganic Chemistry published new progress about Antitumor agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Formula: C19H34O2.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics