Influence 3-formylchromone derivatives in vitro at aggregation of p-amyloid plagues and tyrosinase activity

Objectives. Alzheimer's disease is one of the most common terminal forms of dementia, characterized by a complex pathogenesis with the formation of amyloid plagues in the brain structures. At the same time, one of the new and promising areas of Alzheimer's disease therapy is the influence on the amyloidogenic cascade. Aim of the study. In vitro to evaluate the effect of ten 3-formylchromone derivatives on the formation of p-amyloid aggregates and tyrosinase activity. Materials and methods. The effect of the studied compounds on tyrosinase activity was evaluated using the Mapunyamethod, using L-tyrosine as a substrate and kojic acid as a reference. Aggregation of amyloid plagueswas studied spectrophotometrically in reaction with Congo red after three and six days of incubation. Results. Among the test-objects, the most significant antithyrosinase properties were found in the 6-acetyl substituted derivative of 3-formylchromone, whose IC50 value was comparable to kojic acid (32±1.913 pg/ml versus 30.2±1.599 pg/ml). Also, this compound most significantly inhibited the aggregation of amyloid plagues on the third day of incubation-31.0% (p<0.05) and 61% (p<0.05) - on the sixth day. It should be noted that 3-formylchromone and oxime of this compound had no significant effect on tyrosinase activity and amyloidogenesis. Conclusion. This study suggests the relevance of further study of 6-acetyl-substituted 3-formylchronome as a potential means of pathogenetic therapy of Alzheimer's disease.

Alzheimer's disease, chromone derivatives, tyrosinase, fi-amyloid