Bioactive heterocyclic derivatives

  • doc. Mgr. Lucie Plíhalová, Ph.D.
    • prof. PharmDr. Josef Jampílek, Ph.D.
    • Mgr. Martin Hönig, Ph.D.
    • Mgr. Magdaléna Bryksová, Ph.D.
    • Mgr. Dardan Klos 
    • Bc. Magdaléna Zvonková
    • Bc. Pavlína Cochlarová
    • Bc. Anna Malíšková
    • Bc. Beáta Kubaláková
    • Klára Vojtášková
    • Michal Pernička

The group led by Lucie Plíhalová is dedicated to the design, preparation and research of new small heterocyclic, especially purine, molecules, most often derived from plant regulators. These substances have, in miniature concentrations, an unprecedented biological activity in plants, which can be better mapped by using their fluorescent or isotopically labelled derivatives. Controlled derivatization or slight modification of these plant molecules can also effectively modulate the biological effects on plant cells and tissues and thus prepare, for example, modern substances for the treatment of plants without significant burden on the environment. Inspired by plant substances, new heterocyclic bioactive substances with an effect on human cells and tissues, with potential use in cosmetics or hygiene, are also being prepared and investigated. The feedback obtained by the study between the structure and the activity of the prepared substances leads to a more specific targeting of the newly prepared derivatives. Many acquired patents and utility models for these compounds allow the transfer of new technologies and knowledge into practice.

Natural product synthesis

  • doc. RNDr. Jiří Pospíšil, Ph.D.
    • Mgr. Tomáš Pospíšil, Ph.D.
    • Dr. Roman Iakovenko (postdoc, LRR)
    • Mgr. Daniel Chrenko
    • Mgr. Markéta Fuksová
    • Kristýna Malíková
    • Anna Chesnoková
    • Silvie Lévayová
    • Barbora Dopitová (Badatel)

Research projects within Pospisil2ab focus on the (semi) synthetic preparation of natural substances, and on the development of new environmentally friendly synthetic procedures suitable for their preparation. In the field of natural substances, we focus mainly on (1) phenylpropanoid based plant secondary metabolites - lignans and neolignans, and on (2) plant growth regulators - gibberellins. This type of substances are prepared by (3) new synthetic procedures that are based on new synthetic methods and (pluripotent) reagents designed and developed within the group. The goal of such protocols is to create new structurally and stereo diverse chemical libraries of (potentially) biologically active substances. Substances that are subsequently used in the study of (bio)chemical transformations. The aim of the research is to find new molecular targets in studied biological targets. Our bioactivity studies focus mainly on substances with leishmanicidal and anthelmitic effects. (more info at www.pospisilab.com)

Organic synthesis and scale up lab

  • RNDr. Marek Zatloukal, Ph.D.
    • František Škařupa
    • Mgr. Jan Walla
    • Mgr. Jana Kočířová
       

The group led by Marek Zatloukal focuses mainly on the chemistry of heterocyclic compounds, especially the synthesis and study of the biological activity of nucleobases, especially purines and its bioisosteres. Newly prepared "small" molecules are subjected to a wide range of biological tests (cytokinin, antitumor, antisenescence, antioxidant and other activities). The study of neuroprotective activity with a focus on antiparkinsonian effects has also recently started on selected derivatives in cooperation with the Department of Experimental Biology, UP. The group is also interested in the synthesis of selected isotopically labelled bioactive molecules as standards for mass spectrometry. Another important area of the group's activity is the synthesis of selected biologically active candidates in a larger scale and the solution of the subsequent transfer of technology from laboratory to semi-pilot and pilot scale. Cooperation with the commercial sphere is also very important, especially in the development of new technologies. The great result of the group's work is, among other things, a number of granted international patents.

Synthesis and analysis of cytokinins

  • Dr. Karel Doležal
    • Mgr. Vladimíra Nožková, Ph.D.
    • Mgr. Hana Vylíčilová, Ph.D.
    • Mgr. Jakub Hrdlička, Ph.D.
    • Mgr. Šárka Slamencová
    • Mgr. Karolína Wojewodová
    • Mgr. Hana Omámiková
    • Jarmila Balonová
       

Our group focusses on preparation of different groups of di-and tri-substituted purines by classical organic synthesis as well as using modern methods (microwave-assisted synthesis etc.). Identity and purity of new compounds is evaluated by different physico-chemical methods (for example CHN analysis, melting point, liquid as well as solid state nuclear magnetic resonance spektrometry (NMR), high-resolution TOF mass spektrometry(HR TOF MS). Subsequently, biological activity as well as unique metabolic properties of prepared derivatives is evaluated in different bioassays, receptor assays, field experiments on various crops (corn, barley, wheat, rape seed, poppy seed) as well as different in vitro tissue-systems of various plat species, including ornamental, medicinal and endangered ones (in collaboration with different labs around the world, e.g. in South Africa or Belgium). New derivatives cross-talk with endogenous plant hormones (cytokinins, auxins, jasmonates, salicilates, abscisic acic…) is determined in the plant extracts using UHPLC-MS/MS as well as in situ by mass spectrometry imaging.

Application-oriented organic synthesis

  • Dr. Asta Žukauskaite
    • Mgr. Kristýna Bieleszová
    • Mgr. Radim Simerský, Ph.D.
       

Asta Žukauskaitė research group is interested in synthesis and application potential of indoles and their bioisosteres. Her team members devote synthetic efforts towards naturally occurring, putative and nature inspired indolic compounds. They adapt and, if necessary, develop synthetic methodologies to prepare isotopically labelled internal standards of naturally occurring indoles (i.e., auxins, tryptophan metabolites, etc.), enabling their identification and quantification in plant and/or animal tissues, which is essential for physiological studies investigating their mode of action. Fluorescently labelled auxins are being developed for visualization of auxin transport, as well as tissue-specific and subcellular localization in planta, without the use of marker or reporter lines. Other research projects are dedicated to the synthesis of biologically relevant compounds with anthelmintic, anticancer, plant growth regulating activities, etc., which are being investigated in close collaboration with local and foreign partners.  

Field oriented research

  • Ing. Radoslav Koprna, Ph.D.
    • Mgr. Zdeněk Špíšek, Ph.D.
    • Mgr. Jan Humplík, Ph.D. (LRR)
    • Mgr. Ivan Filipský
       

Radek Koprna´s group is interested in testing of biological activity of phytohormonal derivatives, growth regulators, stimulators and fertilizers on the field. Next activity of the group is the development of preparation based on plant growth regulators and combined fertilizers. Further tasks of the group are breeding, application and maintenance of breeding of field crops, research and verification of the effectiveness of plant protection products, including the extension of marketing authorizations to so-called "minority indications", development of plant growing technologies as well as phenotyping of root and shoot biomass using advanced measurement methods. The domain of the group is cooperation with commercial companies on the development of preparations and fertilizers, stability studies and studies of the effectiveness of preparations. The department also conducts contract research focusing on the above issues.

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