Exploring Turkish biodiversity: A rich source of chemical diversity for drug leads discovery

Abstract

Bioresources offer tremendous potential by having excellent chemical diversity for drug discovery programs and by serving as templates for synthetic drugs. There are wellknown examples of clinically important drugs derived from natural sources. The development of pharmaceutical, nutraceutical, agricultural, and industrial products from bioresources can be used to promote incentives for conservation by providing an economic return to innovative use. Of those sources, medicinal plants have a virtually untapped reserve of original drug molecules, which await determination and chemical and biological investigation. Marine organisms have also gained increasing attention from researchers worldwide due to their chemically diverse secondary metabolites with desirable biological activities.There is still a great need for novel compounds with unique mechanisms of action to treat diseases such as cancer, Alzheimer's, arthritis, and diabetes. Besides, multiresistance development by the parasites to the present drugs also constitutes another problem for the treatment of parasitic diseases as well as tuberculosis.In this article, 209 plant species belonging to 11 plant families were investigated for cholinesterase inhibitory activity by in vitro Ellman method at 10 μg/ml and 1 mg/ml doses. Among them, Salvia, Rosmarinus, and Fumaria species were found to have the most significant cholinesterase inhibitory activity.

Biological Activities of Some Isoquinoline Alkaloids from Fumaria schleicheri Soy. Will.

“…The results obtained for the acetylcholinesterase (AchE) inhibitory activity can be explained based on the different distribution of each individual alkaloid in the analyzed samples. In a previous study focused on the evaluation of anti-cholinesterase potential of several Fumaria species from Turkey, Sener et al [36] noticed that this activity varied in a dependent manner by the content in three main alkaloids, the most important being protopine. The most recent studies showed also that the anticholinesterase potential of isoquinolinic alkaloid-rich fractions can be influenced both by the type and amount of each individual compound through a synergistic effect.…”

“…Inhibitory potential of alkaloid fractions or individual alkaloids isolated from different Fumaria species on acetyl-and butyrylcholinesterase was indicated by several studies [14,26,36]. In this regard, dry extracts of F. schleicheri were tested in vitro for their ability to inhibit acetylcholinesterase using Ellman colorimetric assay adapted to a microplate reader method.…”

In-silico identification of the binding mode of synthesized adamantyl derivatives inside cholinesterase enzymes

“…In addition, it has been demonstrated that both acetylcholinesterase and butyrylcholinesterase (BChE) play an important role in Aβ-aggregation during plaque formation [3] . Many research papers published in the last decade have indicated that the structures of compounds that exhibit cholinesterase inhibitory activity are diverse [4,5] .…”