Abstract
In this paper, the selective interactions of synthetic derivatives of two natural compounds, berberine and palmatine, with DNA G-quadruplex structures were reported. In particular, the previous works on this subject concerning berberine were further presented and discussed, whereas the results concerning palmatine are presented here for the first time. In detail, these palmatine derivatives were developed by inserting seven different small peptide basic chains, giving several new compounds that have never been reported before. The preliminary studies of the interactions of these compounds with various G-quadruplex-forming sequences were carried out by means of various structural and biochemical techniques, which showed that the presence of suitable side chains is very useful for improving the interaction of the ligands with G-quadruplex structures. Thus, these new palmatine derivatives might act as potential anticancer drugs.
Highlights
A G-quadruplex is a helical tertiary structure of DNA and RNA that is formed by sequences that are rich in guanine through the stacking of at least two guanine tetrad subunits
This particular, this selectivity is much higher if short oligonucleotides are used, because they can favor selectivity is much higher if short oligonucleotides are used, because they can favor the linkage to the the linkage to the complementary DNA bases that become accessible after the formation of complementary DNA bases that become accessible after the formation of G-quadruplex structures [26]
4d, 4e, 4f, 4g, which presented a further amino acid residue on the peptide chains. This observation allowed us to establish, from an experimental point of view, that the side chains with more than two amino acids on palmatine derivatives did not increase the ability of the compound to stabilize G-quadruplex structures (GqS), but rather had the opposite effect
Summary
A G-quadruplex is a helical tertiary structure of DNA and RNA that is formed by sequences that are rich in guanine through the stacking of at least two guanine tetrad subunits. Structures of of berberine berberine and Previous interaction studies of these compounds have clearly revealed their weak interaction Previous interaction studies of these compounds have clearly revealed their weak interaction with DNA as well as their low selectivity and thermodynamic stability with GqS [20,21]. In binding scaffolds greatly increases their selectivity towards GqS versus duplex DNA. This particular, this selectivity is much higher if short oligonucleotides are used, because they can favor selectivity is much higher if short oligonucleotides are used, because they can favor the linkage to the the linkage to the complementary DNA bases that become accessible after the formation of complementary DNA bases that become accessible after the formation of G-quadruplex structures [26]. PAGE analysis, using the telomeric single-stranded DNA TSG4, showed that this to increase the stability of GqS more than berberine alone [23]. Sources that might show potential antitumoral activities by acting on GqS
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