Ndongo_2021_Arch.Pharm.(Weinheim)__e2100150

A miniaturized microsequential injection/lab-on-valve (microSIA-LOV) system was developed and shown to be a useful alternative to perform inhibitory studies on acetylcholinesterase. These studies are essential for the evaluation of the potential therapeutic effect of drugs commonly used in the treatment of Alzheimer's disease. Donepezil, galantamine, and rivastigmine were tested, in addition to compounds based on the xanthone scaffold. Four of these xanthone derivatives were identified as having EC(50) values between 676 and 4466 micromol/l, showing a potential inhibitory effect higher than the clinical agent rivastigmine. The developed automatic system added advantages of reduction of reagents and sample consumption (around 55 microl per analysis), lower cost per analysis, and the generation of less waste (around 1.2 ml per analysis). The microSIA-LOV system is also a robust, rapid, reliable, and simple system to use. Docking studies suggested a possible mode of interaction with the target acetylcholinesterase protein.