Studies of medicinal plants and their therapeutically significant substances

The topic of Secondary metabolites of plants as potential drugs research group (head of the group: prof. Lucie Cahlíková) is the study of secondary metabolites of plants, which is focused on the search for substances potentially usable in the therapy of chronic diseases such as Alzheimer´s disease, and substances with anti-tumor activity. In collaboration with other national and international institutions antimalaric, antibacterial, antituberculotic and antifugal activity are also studied.

In recent years, extensive screening studies of different plant taxa, which contain various structural types of alkaloids, have been done. Based on the obtained results, plants for phytochemical studies were selected for isolation of alkaloids in pure form. All isolated alkaloids are studied for different biological activities. Selected alkaloids are used for the preparation of their derivatives, to study the structure-activity relationship (SAR). To date, more than 130 isoquinoline alkaloids, 50 Amaryllidaceae and 10 indole alkaloids have been isolated (Cahlikova et al., 2013, Chlebek et al., 2015, Vaneckova et al., 2016, Safratova et al., 2018). Furthermore, 40 pilot derivatives of lycorine, haemathamine, ambelline and scoulerine were prepared. Isolation work currently proceeds from other plants (eg Vinca minor, Narcissus sp., Peschiera fuchsiaefolia, Zephyranthes citrina, Papaver rhoeas, Centaurea sp.). Substances isolated or prepared in sufficient amounts are screened for wide range of biological activities.

In connection to Alzheimer's disease are tested inhibition of acetylcholinesterase, butyrylcholinesterases, prolyloligopeptidases (cooperation with the Faculty of Military Health, University of Defense), BACE-1 (collaboration with the Faculty of Pharmacy, University of Bologna), GSK-3b and the crossing of substances through the blood-brain membrane -test, collaboration with Centro de Investigaciones Biologicas, Madrid).
In cooperation with the Faculty of Medicine in Hradec Králové, is studied cytotoxic activity of substances on the panel of cancerous and noncancerous cells.

Active compounds are further studied in more detail. Biological studies involve the determination of the mechanism of action of these compounds on cell viability, proliferation, cellular distribution in individual phases of the cell cycle, induction of double stranded or single-stranded nuclear DNA breakages and apoptosis (Havelek et al. ).

Last year has been established new collaboration in the field of testing the antimalarial activity of Amaryllidaceae alkaloids and their derivatives with Faculdade de Medicina da Universidade de Lisboa. First alkaloids and derivatives are under testing.

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