2-(4--(methylamino)phenyl)-6-hydroxybenzothiazole and ferulic-acid

Many researchers argue that Alzheimer's disease is at least partly caused by deposition of amyloid beta (Aβ) in the brain. Ferulic acid (FA) and Angelica archangelica (AA) are candidate agents for reducing Aβ and improving cognitive function. Feru-guard 100M is a supplement containing FA and AA extract. Using this supplement, we planned to assess the effect of FA and AA on Aβ deposition in the human brain.. This was an open-label, interventional multi-institutional joint study of Kobe University and the Institute of Biomedical Research and Innovation (Kobe, Japan). Seventeen subjects diagnosed with mild cognitive impairment were divided into two groups: the intervention group (n = 10) and the control group (n = 7). The subjects in the intervention group used Feru-guard 100M every day for 48 weeks, whereas the subjects in the control group did not use the supplement. We assessed the differences between the two groups by examining Aβ deposition and brain atrophy at 48 weeks and cognitive function every 24 weeks. We used carbon-11-labelled Pittsburgh compound B (PiB) positron emission tomography to evaluate Aβ deposition.. There were no significant differences in Aβ deposition, brain atrophy, and cognitive function between the two groups. Specifically, differences in Aβ deposition change in seven regions of interest examined with PiB positron emission tomography, brain atrophy change in four indicators of voxel-based morphometry, and cognitive impairment measured by five psychological tests were not significantly between the two groups.. Treatment with Feru-guard 100M, a supplement containing FA and AA extract, for 48 weeks did not reduce cortical PiB retention, which reflects Aβ deposition. It also did not suppress the aggravation of brain atrophy or decline in cognitive function.

Topics: Aged; Alzheimer Disease; Amyloid beta-Peptides; Angelica archangelica; Aniline Compounds; Atrophy; Brain; Carbon Radioisotopes; Cognitive Dysfunction; Coumaric Acids; Disease Progression; Female; Humans; Japan; Male; Positron-Emission Tomography; Radiopharmaceuticals; Thiazoles

New ferulic acid and benzothiazole dimer derivatives were synthesized and evaluated by in vitro competition assay using [(125)I]TZDM for their specific binding affinities to Abeta fibrils. In particular, 4a showed the most excellent binding affinity (K(i)=0.53 nM), compared to PIB (K(i)=0.77 nM), for benzothiazole binding sites of Abeta(1-42) fibrils. This result suggests a possibility of a potential AD diagnostic probe for detection of Abeta fibrils.

Topics: Amyloid beta-Peptides; Benzothiazoles; Coumaric Acids; Dimerization; Structure-Activity Relationship