Abstract

A convenient method for the synthesis of the first generation PAMAM dendrimers based on the thiacalix[4]arene has been developed for the first time. Three new PAMAM-calix-dendrimers with the macrocyclic core in cone, partial cone, and 1,3-alternate conformations were obtained with high yields. The interaction of the obtained compounds with salmon sperm DNA resulted in the formation of the associates of the size up to 200 nm, as shown by the UV-Vis spectroscopy, DLS, and TEM. It was demonstrated by the CD method that the structure of the DNA did not undergo significant changes upon binding. The PAMAM-calix-dendrimer based on the macrocycle in cone conformation stabilized DNA and prevented its degradation.

Highlights

  • In recent years, research aimed at developing DNA vaccines has shown great potential [1]

  • Synthesis of the poly(amidoamine) (PAMAM) dendrimers is well described in the literature [28,29]

  • The obtained precursor is involved in the reaction with an excess of the diamine. This leads to the formation of a full generation of the PAMAM dendrimer

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Summary

Introduction

Research aimed at developing DNA vaccines has shown great potential [1]. These medicinal products are already successfully used in veterinary medicine [2]. Inovio Pharmaceuticals Corporation (Plymouth Meeting, PA) proposed a DNA vaccine for the prevention of SARS COVID-19 [3]. A significant increase in research on the use of DNA-based drugs for the treatment of other diseases has been noted in recent years [4]. Jazz Pharmaceuticals proposed the drug Defitelio®® (defibrotide sodium), which is the oligonucleotide obtained by depolymerization of porcine intestinal mucosal DNA for the treatment of hepatic venoocclusive disease [5]. Polynucleotides obtained from marine fish exert a wide therapeutic use [6,7,8]

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