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The Gold(I) Complex with Plant Hormone Kinetin Shows Promising In Vitro Anticancer and PPARγ Properties
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SYSNO ASEP 0571095 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title The Gold(I) Complex with Plant Hormone Kinetin Shows Promising In Vitro Anticancer and PPARγ Properties Author(s) Trávníček, Z. (CZ)
Vančo, J. (CZ)
Belza, J. (CZ)
Hošek, J. (CZ)
Dvořák, Z. (CZ)
Lenobel, René (UEB-Q) ORCID
Popa, I. (CZ)
Šmejkal, K. (CZ)
Uhrin, P. (AT)Number of authors 9 Article number 2293 Source Title International Journal of Molecular Sciences. - : MDPI
Roč. 24, č. 3 (2023)Number of pages 21 s. Language eng - English Country CH - Switzerland Keywords anti-inflammatory ; anticancer ; apoptosis ; cell cycle ; gold(I) complex ; in vitro ; kinetin ; ppar ; ros OECD category Physical chemistry Method of publishing Open access Institutional support UEB-Q - RVO:61389030 UT WOS 000930771000001 EID SCOPUS 85148045447 DOI 10.3390/ijms24032293 Annotation 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. Workplace Institute of Experimental Botany Contact David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Year of Publishing 2024 Electronic address https://doi.org/10.3390/ijms24032293
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