We have studied the effect of acridine derivatives on the amyloid aggregation of lysozyme to investigate the acridine structure-activity relationship. The activity of the effective planar acridines was characterized by the half-maximum depolymerization concentration DC50 and half-maximal inhibition concentration IC50. For the most effective acridine derivatives we examined their interaction with DNA and their effect on cell viability in order to investigate their eventual influence on cells. We thus identified planar acridine derivatives with intensive anti-amyloid activity (IC50 and DC50 values in micromolar range), low cytotoxicity and weak ability to interfere with the processes in the cell.
Structure-activity relationship of acridine derivatives to amyloid aggregation of lysozyme
Beatrice Chelli;Eva Bystrenova;Francesco Valle;Fabio Biscarini;
2010
Abstract
We have studied the effect of acridine derivatives on the amyloid aggregation of lysozyme to investigate the acridine structure-activity relationship. The activity of the effective planar acridines was characterized by the half-maximum depolymerization concentration DC50 and half-maximal inhibition concentration IC50. For the most effective acridine derivatives we examined their interaction with DNA and their effect on cell viability in order to investigate their eventual influence on cells. We thus identified planar acridine derivatives with intensive anti-amyloid activity (IC50 and DC50 values in micromolar range), low cytotoxicity and weak ability to interfere with the processes in the cell.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.