Thiosemicarbazone modification of 3-acetyl coumarin inhibits Aβ peptide aggregation and protect against Aβ-induced cytotoxicity

Amino group of salicylic acid exhibits enhanced inhibitory potential against insulin amyloid fibrillation with protective aptitude toward amyloid induced cytotoxicity

“…For clarity of results only selected spectra were shown. However, in presence of 500 μM of 5‐ASA, utmost reduction in ANS fluorescence intensity clearly indicates that lesser number of hydrophobic patches (propensity to form aggregates) were exposed to ANS dye as show in Figure B . In addition, reduction of ANS fluorescence intensity was concentration dependent as observed in Figure C.…”

Thiosemicarbazone Moiety Assist in Interaction of Planar Aromatic Molecules with Amyloid Beta Peptide and Acetylcholinesterase

“…Further we reconfirmed the inhibitory potential of TSC analogues toward Aβ peptide aggregation using turbidity assay (Figure ). Turbidity assay is routinely employed in Aβ aggregation studies . Upon incubating the monomeric 20 μM Aβ(1–42) peptide alone, a time dependent increase in the turbidity at 400 nm was observed which reached plateau phase at 30 min (table S3).…”

“…Designing the multi‐targeted molecules capable of targeting multiple pathways are urgently needed for the development of treatments for AD. Thiosemicarbazone derivatization could provide new avenues in designing of the molecules against treatment of AD . However exact nature of the interaction between thiosemicarbazone analogues with Aβ peptide and AChE was not available.…”

“…However many of these compounds have not been studied for their AChE inhibitiory potential. In our preliminary work, we studied the effect of thiosemicarbazone modification of 3‐acetylcoumarin (AC) on the inhibition of Aβ peptide aggregation as well as Aβ‐induced cytotoxicity . Our results showed that 3‐acetylcoumarin thiosemicarbazone (ACT) profoundly inhibits the formation of higher aggregates of Aβ peptide compared to AC.…”

Biological Applications of Co(II) and Ni(II) Complexes of Semicarbazones and Thiosemicarbazones

“…Thiosemicarbazones after coordination with transition metals results in the formation of metal complex of corresponding ligand and shows better biological properties because of chelation and overtone's theory. A lot of work proving the biological importance of thiosemecarbazones and their transition metal complexes have been already reported [41][42][43][44][45][46] and still the efforts to develop more active thiosemicarbazone based drugs goes on. Due to the outstanding and diversified properties, these thiosemicarbazones are employed in pharmacological as well as in food industries [47].…”