Detailed Information on Publication Record
2023
The Gold(I) Complex with Plant Hormone Kinetin Shows Promising In Vitro Anticancer and PPARγ Properties
TRAVNICEK, Zdenek, Jan VANCO, Jan BELZA, Jan HOSEK, Zdenek DVORAK et. al.Basic information
Original name
The Gold(I) Complex with Plant Hormone Kinetin Shows Promising In Vitro Anticancer and PPARγ Properties
Authors
TRAVNICEK, Zdenek (203 Czech Republic), Jan VANCO (203 Czech Republic), Jan BELZA (203 Czech Republic), Jan HOSEK (203 Czech Republic), Zdenek DVORAK (203 Czech Republic), Rene LENOBEL (203 Czech Republic), Igor POPA (203 Czech Republic), Karel ŠMEJKAL (203 Czech Republic, belonging to the institution) and Pavel UHRIN (40 Austria)
Edition
International Journal of Molecular Sciences, Basel, Multidisciplinary Digital Publishing Institute, 2023, 1661-6596
Other information
Language
English
Type of outcome
Článek v odborném periodiku
Field of Study
30104 Pharmacology and pharmacy
Country of publisher
Switzerland
Confidentiality degree
není předmětem státního či obchodního tajemství
References:
Impact factor
Impact factor: 5.600 in 2022
RIV identification code
RIV/00216224:14160/23:00133785
Organization unit
Faculty of Pharmacy
UT WoS
000930771000001
Keywords in English
gold(I) complex; kinetin; anticancer; anti-inflammatory; in vitro; PPAR; cell cycle; apoptosis; ROS
Tags
International impact, Reviewed
Změněno: 4/4/2024 19:10, Mgr. Daniela Černá
Abstract
V originále
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.
Links
GF21-38204L, research and development project |
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