Investigator

Karel Šmejkal

Head of Department · Masaryk University Faculty of Pharmacy, Department of Natural Drugs

KŠKarel Šmejkal
Papers(1)
The Gold(I) Complex w…
Collaborators(5)
Pavel UhrinZdeněk DvořákZdeněk TrávníčekJan HošekJán Vančo
Institutions(4)
Masaryk UniversityMedical University of…Palacký University Ol…Regional Centre Of Ad…

Papers

The Gold(I) Complex with Plant Hormone Kinetin Shows Promising In Vitro Anticancer and PPARγ Properties

Motivated by the clinical success of gold(I) metallotherapeutic Auranofin in the effective treatment of both inflammatory and cancer diseases, we decided to prepare, characterize, and further study the [Au(kin)(PPh3)] complex (1), where Hkin = kinetin, 6-furfuryladenine, for its in vitro anti-cancer and anti-inflammatory activities. The results revealed that the complex (1) had significant in vitro cytotoxicity against human cancer cell lines (A2780, A2780R, PC-3, 22Rv1, and THP-1), with IC50 ≈ 1–5 μM, which was even significantly better than that for the conventional platinum-based drug Cisplatin while comparable with Auranofin. Although its ability to inhibit transcription factor NF-κB activity did not exceed the comparative drug Auranofin, it has been found that it is able to positively influence peroxisome-proliferator-activated receptor-gamma (PPARγ), and as a consequence of this to have the impact of moderating/reducing inflammation. The cellular effects of the complex (1) in A2780 cancer cells were also investigated by cell cycle analysis, induction of apoptosis, intracellular ROS production, activation of caspases 3/7 and disruption of mitochondrial membrane potential, and shotgun proteomic analysis. Proteomic analysis of R2780 cells treated with complex (1) and starting compounds revealed possible different places of the effect of the studied compounds. Moreover, the time-dependent cellular accumulation of copper was studied by means of the mass spectrometry study with the aim of exploring the possible mechanisms responsible for its biological effects.

80Works
1Papers
5Collaborators
Cell Line, TumorApoptosisBreast NeoplasmsNeoplasmsOvarian NeoplasmsBiomarkers, TumorTumor Cells, Cultured

Positions

2020–

Head of Department

Masaryk University Faculty of Pharmacy · Department of Natural Drugs

2013–

Associated Professor

University of Veterinary and Pharmacutical Sciences Brno · Department of Natural Drugs

2005–

Research Assistant

University of Veterinary and Pharmaceutical Sciences Brno · Department of Natural Frugs

Education

2005

PhD

University of Veterinary and Pharmaceutical Sciences Brno · Department of Natural Drugs

Country

CZ