Cytotoxic activity and influence on acetylcholinesterase of series dinuclear platinum(II) complexes with aromatic nitrogen-containing heterocyclic bridging ligands: Insights in the mechanisms of action
Samo za registrovane korisnike
2021
Autori
Bondžić, Aleksandra M.![](/themes/MirageVinar/images/orcid.png)
Žakula, Jelena
![](/themes/MirageVinar/images/orcid.png)
Korićanac, Lela B.
Keta, Otilija D.
![](/themes/MirageVinar/images/orcid.png)
Janjić, Goran V.
![](/themes/MirageVinar/images/orcid.png)
Đorđević, Ivana S.
Rajković, Snežana U.
Članak u časopisu (Objavljena verzija)
![](/themes/MirageVinar//images/creativecommons/arr.png)
Metapodaci
Prikaz svih podataka o dokumentuApstrakt
Herein, the stability, lipophilicity, in vitro cytotoxicity, and influence on acetylcholinesterase of five dinuclear platinum(II) complexes with the general formula [{Pt(en)Cl}2(μ-L)]2+ (L is a different aromatic nitrogen-containing heterocyclic bridging ligands pyrazine (pz, Pt1), pyridazine (pydz, Pt2), quinoxaline (qx, Pt3), phthalazine (phtz, Pt4) and quinazoline (qz, Pt5), while en is bidentate coordinated ethylenediamine) were evaluated. The most active analyzed platinum complexes induced time-dependent growth inhibition of A375, HeLa, PANC-1, and MRC-5 cells. The best efficiency was achieved on HeLa and PANC-1 cells for Pt1, Pt2, and Pt3 at the highest concentration, while Pt1 was significantly more potent than cisplatin at a lower concentration. Additionally, a lower effect on normal cells was observed compared to cisplatin, which may indicate potentially fewer side effects of these complexes. Selected complexes induce reactive oxygen species and apoptosis on tumor cell lines. ...The most potent reversible acetylcholinesterase (AChE) inhibitors were Pt2, Pt4, and Pt5. Pt1 showed similar inhibitory potential toward AChE as cisplatin, but a different type of inhibition, which could contribute to lower neurotoxicity. Docking studies revealed that Pt2 and Pt4 were bound to the active gorge above the catalytic triad. In contrast, the other complexes were bound to the edge of the active gorge without impeding the approach to the catalytic triad. According to this, Pt1 represents a promising compound with potent anticancer properties, high selectivity, and low neurotoxicity.
Ključne reči:
Acetylcholinesterase / Cytotoxicity / Docking studies / Neurotoxicity / Platinum(II) complexesIzvor:
Chemico-Biological Interactions, 2021, 109708-Finansiranje / projekti:
- Ministarstvo nauke, tehnološkog razvoja i inovacija Republike Srbije, institucionalno finansiranje - 200017 (Univerzitet u Beogradu, Institut za nuklearne nauke Vinča, Beograd-Vinča) (RS-MESTD-inst-2020-200017)
- info:eu-repo/grantAgreement/MESTD/inst-2020/200026/RS/ (-)
- Ministarstvo nauke, tehnološkog razvoja i inovacija Republike Srbije, institucionalno finansiranje - 200122 (Univerzitet u Kragujevcu, Prirodno-matematički fakultet) (RS-MESTD-inst-2020-200122)
DOI: 10.1016/j.cbi.2021.109708
ISSN: 0009-2797
WoS: 00082047000000
Scopus: 2-s2.0-85118274093
Kolekcije
Institucija/grupa
VinčaTY - JOUR AU - Bondžić, Aleksandra M. AU - Žakula, Jelena AU - Korićanac, Lela B. AU - Keta, Otilija D. AU - Janjić, Goran V. AU - Đorđević, Ivana S. AU - Rajković, Snežana U. PY - 2021 UR - https://vinar.vin.bg.ac.rs/handle/123456789/10015 AB - Herein, the stability, lipophilicity, in vitro cytotoxicity, and influence on acetylcholinesterase of five dinuclear platinum(II) complexes with the general formula [{Pt(en)Cl}2(μ-L)]2+ (L is a different aromatic nitrogen-containing heterocyclic bridging ligands pyrazine (pz, Pt1), pyridazine (pydz, Pt2), quinoxaline (qx, Pt3), phthalazine (phtz, Pt4) and quinazoline (qz, Pt5), while en is bidentate coordinated ethylenediamine) were evaluated. The most active analyzed platinum complexes induced time-dependent growth inhibition of A375, HeLa, PANC-1, and MRC-5 cells. The best efficiency was achieved on HeLa and PANC-1 cells for Pt1, Pt2, and Pt3 at the highest concentration, while Pt1 was significantly more potent than cisplatin at a lower concentration. Additionally, a lower effect on normal cells was observed compared to cisplatin, which may indicate potentially fewer side effects of these complexes. Selected complexes induce reactive oxygen species and apoptosis on tumor cell lines. The most potent reversible acetylcholinesterase (AChE) inhibitors were Pt2, Pt4, and Pt5. Pt1 showed similar inhibitory potential toward AChE as cisplatin, but a different type of inhibition, which could contribute to lower neurotoxicity. Docking studies revealed that Pt2 and Pt4 were bound to the active gorge above the catalytic triad. In contrast, the other complexes were bound to the edge of the active gorge without impeding the approach to the catalytic triad. According to this, Pt1 represents a promising compound with potent anticancer properties, high selectivity, and low neurotoxicity. T2 - Chemico-Biological Interactions T1 - Cytotoxic activity and influence on acetylcholinesterase of series dinuclear platinum(II) complexes with aromatic nitrogen-containing heterocyclic bridging ligands: Insights in the mechanisms of action SP - 109708 DO - 10.1016/j.cbi.2021.109708 ER -
@article{ author = "Bondžić, Aleksandra M. and Žakula, Jelena and Korićanac, Lela B. and Keta, Otilija D. and Janjić, Goran V. and Đorđević, Ivana S. and Rajković, Snežana U.", year = "2021", abstract = "Herein, the stability, lipophilicity, in vitro cytotoxicity, and influence on acetylcholinesterase of five dinuclear platinum(II) complexes with the general formula [{Pt(en)Cl}2(μ-L)]2+ (L is a different aromatic nitrogen-containing heterocyclic bridging ligands pyrazine (pz, Pt1), pyridazine (pydz, Pt2), quinoxaline (qx, Pt3), phthalazine (phtz, Pt4) and quinazoline (qz, Pt5), while en is bidentate coordinated ethylenediamine) were evaluated. The most active analyzed platinum complexes induced time-dependent growth inhibition of A375, HeLa, PANC-1, and MRC-5 cells. The best efficiency was achieved on HeLa and PANC-1 cells for Pt1, Pt2, and Pt3 at the highest concentration, while Pt1 was significantly more potent than cisplatin at a lower concentration. Additionally, a lower effect on normal cells was observed compared to cisplatin, which may indicate potentially fewer side effects of these complexes. Selected complexes induce reactive oxygen species and apoptosis on tumor cell lines. The most potent reversible acetylcholinesterase (AChE) inhibitors were Pt2, Pt4, and Pt5. Pt1 showed similar inhibitory potential toward AChE as cisplatin, but a different type of inhibition, which could contribute to lower neurotoxicity. Docking studies revealed that Pt2 and Pt4 were bound to the active gorge above the catalytic triad. In contrast, the other complexes were bound to the edge of the active gorge without impeding the approach to the catalytic triad. According to this, Pt1 represents a promising compound with potent anticancer properties, high selectivity, and low neurotoxicity.", journal = "Chemico-Biological Interactions", title = "Cytotoxic activity and influence on acetylcholinesterase of series dinuclear platinum(II) complexes with aromatic nitrogen-containing heterocyclic bridging ligands: Insights in the mechanisms of action", pages = "109708", doi = "10.1016/j.cbi.2021.109708" }
Bondžić, A. M., Žakula, J., Korićanac, L. B., Keta, O. D., Janjić, G. V., Đorđević, I. S.,& Rajković, S. U.. (2021). Cytotoxic activity and influence on acetylcholinesterase of series dinuclear platinum(II) complexes with aromatic nitrogen-containing heterocyclic bridging ligands: Insights in the mechanisms of action. in Chemico-Biological Interactions, 109708. https://doi.org/10.1016/j.cbi.2021.109708
Bondžić AM, Žakula J, Korićanac LB, Keta OD, Janjić GV, Đorđević IS, Rajković SU. Cytotoxic activity and influence on acetylcholinesterase of series dinuclear platinum(II) complexes with aromatic nitrogen-containing heterocyclic bridging ligands: Insights in the mechanisms of action. in Chemico-Biological Interactions. 2021;:109708. doi:10.1016/j.cbi.2021.109708 .
Bondžić, Aleksandra M., Žakula, Jelena, Korićanac, Lela B., Keta, Otilija D., Janjić, Goran V., Đorđević, Ivana S., Rajković, Snežana U., "Cytotoxic activity and influence on acetylcholinesterase of series dinuclear platinum(II) complexes with aromatic nitrogen-containing heterocyclic bridging ligands: Insights in the mechanisms of action" in Chemico-Biological Interactions (2021):109708, https://doi.org/10.1016/j.cbi.2021.109708 . .