The interaction between 13-phenylalkyl and 13-diphenylalkyl Berberine derivatives (NAX) and the human telomeric DNA G4 structures has been investigated by both spectroscopic and crystallographic methods. NAX042 and NAX053 are the best ones in improving the performance of the natural precursor Berberine. This finding is in agreement with the X-ray diffraction result for the NAX053-Tel12 adduct, showing the ligand which interacts via ?- stacking, sandwiched at the interface of two symmetry related quadruplex units with its benzhydryl group contributing to the overall stability of the adduct, by means of additional ?-stacking interactions with the DNA residues. The Berberine derivatives were also investigated for their cytotoxic activity towards a panel of human cancer cell. Compounds NAX042 and NAX053 may affect the viability of cancer cell lines in a dose-dependent manner.
Solution and solid state analysis of binding of 13-substituted Berberine analogues to human telomeric G-quadruplex.
2016
Abstract
The interaction between 13-phenylalkyl and 13-diphenylalkyl Berberine derivatives (NAX) and the human telomeric DNA G4 structures has been investigated by both spectroscopic and crystallographic methods. NAX042 and NAX053 are the best ones in improving the performance of the natural precursor Berberine. This finding is in agreement with the X-ray diffraction result for the NAX053-Tel12 adduct, showing the ligand which interacts via ?- stacking, sandwiched at the interface of two symmetry related quadruplex units with its benzhydryl group contributing to the overall stability of the adduct, by means of additional ?-stacking interactions with the DNA residues. The Berberine derivatives were also investigated for their cytotoxic activity towards a panel of human cancer cell. Compounds NAX042 and NAX053 may affect the viability of cancer cell lines in a dose-dependent manner.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
