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@article{2384408,
author = {Travnicek, Zdenek and Vanco, Jan and Belza, Jan and Hosek, Jan and Dvorak, Zdenek and Lenobel, Rene and Popa, Igor and Šmejkal, Karel and Uhrin, Pavel},
article_location = {Basel},
article_number = {3},
doi = {http://dx.doi.org/10.3390/ijms24032293},
keywords = {gold(I) complex; kinetin; anticancer; anti-inflammatory; in vitro; PPAR; cell cycle; apoptosis; ROS},
language = {eng},
issn = {1661-6596},
journal = {International Journal of Molecular Sciences},
title = {The Gold(I) Complex with Plant Hormone Kinetin Shows Promising In Vitro Anticancer and PPARγ Properties},
url = {https://www.mdpi.com/1422-0067/24/3/2293},
volume = {24},
year = {2023}
}
TY - JOUR
ID - 2384408
AU - Travnicek, Zdenek - Vanco, Jan - Belza, Jan - Hosek, Jan - Dvorak, Zdenek - Lenobel, Rene - Popa, Igor - Šmejkal, Karel - Uhrin, Pavel
PY - 2023
TI - The Gold(I) Complex with Plant Hormone Kinetin Shows Promising In Vitro Anticancer and PPARγ Properties
JF - International Journal of Molecular Sciences
VL - 24
IS - 3
SP - 2293
EP - 2293
PB - Multidisciplinary Digital Publishing Institute
SN - 16616596
KW - gold(I) complex
KW - kinetin
KW - anticancer
KW - anti-inflammatory
KW - in vitro
KW - PPAR
KW - cell cycle
KW - apoptosis
KW - ROS
UR - https://www.mdpi.com/1422-0067/24/3/2293
N2 - 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 approximate to 1-5 mu M, 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-kappa B activity did not exceed the comparative drug Auranofin, it has been found that it is able to positively influence peroxisome-proliferator-activated receptor-gamma (PPAR gamma), 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.
ER -
TRAVNICEK, Zdenek, Jan VANCO, Jan BELZA, Jan HOSEK, Zdenek DVORAK, Rene LENOBEL, Igor POPA, Karel ŠMEJKAL and Pavel UHRIN. The Gold(I) Complex with Plant Hormone Kinetin Shows Promising In Vitro Anticancer and PPARγ Properties. \textit{International Journal of Molecular Sciences}. Basel: Multidisciplinary Digital Publishing Institute, 2023, vol.~24, No~3, p.~2293-2313. ISSN~1661-6596. Available from: https://dx.doi.org/10.3390/ijms24032293.
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