ADC TAKÁČ, Peter [30 %] - KELLO, Martin [30 %] - BAGO PILÁTOVÁ, Martina [10 %] - KUDLIČKOVÁ, Zuzana [6 %] - VILKOVÁ, Mária [6 %] - SLEPČÍKOVÁ, Paulína [3 %] - PETIK, Peter [1 %] - MOJŽIŠ, Ján [14 %]. New chalcone derivative exhibits antiproliferative potential by inducing G2/M cell cycle arrest, mitochondrial-mediated apoptosis and modulation of MAPK signalling pathway. In Chemico-Biological Interactions. ISSN 0009-2797, 2018, vol. 292, no., p. 37-49. (2018: 3.407 - IF, 3.299 - IF 5y, 115 - H-index, 0.923 - SJR, Q1 - SJR Best Q, Q2 - JCR Best Q). (2018 - Current Contents).
| Basic data | |
|---|---|
| OCA1. Surname awarded to the assessed person | Takáč |
| OCA2. Name awarded to the assessed person | Peter |
| OCA3. Degrees awarded to the assessed person | Assoc. prof. , Pharm.D., PhD |
| OCA4. Hyperlink to the entry of the person in the Register of university staff | https://www.portalvs.sk/regzam/detail/27235 |
| OCA5. Area of assessment | study programme pharmacy (joint study programme) · I. + II. degree |
| OCA6. Category of the research/artistic/other output | scientific output |
| OCA7. Year of publication of the research/artistic/other output | 2018 |
| OCA8. ID of the record in the Central Registry of Publication Activity (CRPA) or the Central Registry of Artistic Activity (CRAA) | ID: 65428 |
| OCA9. Hyperlink to the record in CRPA or CRAA | https://app.crepc.sk/?fn=detailBiblioForm&sid=F1F5C144CE18DF6CBE1E4304 |
| Characteristics of the output that is not registered in CRPA or CRAA | |
| OCA10. Hyperlink to the record in another publicly accessible register, catalogue of research/ artistic/other outputs | |
| OCA11. Characteristics of the output in the format of the CRPA or the CRAA bibliographic record, if the output is not available in a publicly accessible register or catalogue of outputs | ADC TAKÁČ, Peter [30 %] - KELLO, Martin [30 %] - BAGO PILÁTOVÁ, Martina [10 %] - KUDLIČKOVÁ, Zuzana [6 %] - VILKOVÁ, Mária [6 %] - SLEPČÍKOVÁ, Paulína [3 %] - PETIK, Peter [1 %] - MOJŽIŠ, Ján [14 %]. New chalcone derivative exhibits antiproliferative potential by inducing G2/M cell cycle arrest, mitochondrial-mediated apoptosis and modulation of MAPK signalling pathway. In Chemico-Biological Interactions. ISSN 0009-2797, 2018, vol. 292, no., p. 37-49. (2018: 3.407 - IF, 3.299 - IF 5y, 115 - H-index, 0.923 - SJR, Q1 - SJR Best Q, Q2 - JCR Best Q). (2018 - Current Contents). |
| OCA12. Type of the output (if the output is not registered in CRPA or CRAA) | |
| OCA13. Hyperlink to the webpage where the output is available (full text, other documentation, etc.) | |
| OCA14. Characteristics of the author's contribution | |
| OCA15. Annotation of the output with contextual information concerning the description of creative process and the content of the research/artistic/other activity, etc. | |
| Other data | |
| OCA16. Annotation of the output in English | In the present study, we investigated antiproliferative activity of seven newly synthesized chalcone derivatives. Among tested compounds, (2 E)-3-(acridin-9-yl)-1-(2,6-dimethoxyphenyl)prop-2-en-1-one (1C) was the most potent with IC50 = 4.1 μmol/L in human colorectal HCT116 cells and was selected for further studies. Inhibition of cell proliferation was associated with cell cycle arrest in G2/M phase and dysregulation of α, α1 and β5 tubulins. Moreover, 1C caused disruption of the mitochondrial membrane potential and increased number of cells with sub G0/G1 DNA content which is considered as marker of apoptosis. Apoptosis was confirmed by annexin V/PI and AO/PI staining. Furthermore, we found increased concentration of cytochrome c, Smac/Diablo and increased caspase-3 and caspase-9 activity, cleavage of PARP as well as activation of DNA repair mechanisms in 1C-treated HCT116 cancer cells. Moreover this chalcone derivative up-regulated proapoptotic Bax expression and down-regulated antiapoptotic Bcl-2 and Bcl-xL expression. Additionally, 1C treatment led to modulation of MAPKs and Akt signalling pathways. In conclusion, our data showed ability of 1C to suppress cancel cell growth and provide the rationale for further in vivo study. |
| OCA17. List of maximum 5 most significant citations corresponding to the output | [1]/[1] EL-ATAWY, Mohamed A. - HANNA, Demiana H. - BASHAL, Ali H. - AHMED, Hoda A. - ALSHAMMARI, Eida M. - HAMED, Ezzat A. - ALJOHANI, Abdullah R. - OMAR, Alaa Z. Synthesis, Characterization, Antioxidant, and Anticancer Activity against Colon Cancer Cells of Some Cinnamaldehyde-Based Chalcone Derivatives. In Biomolecules, 2024-02-01, 14, 2, pp. Dostupné na: https://doi.org/10.3390/biom14020216., Registrované v: WOS, SCOPUS [1]/[1] KAYA-SEZGINER, Ecem - OZ BEDIR, Beyza Ecem - TERZI, Emine - OZDEMIR SANCI, Tuba - MARYAM, Zahra - ACAR ÇEVIK, Ulviye. Design, Synthesis, and Biological Evaluation of New Benzimidazole-1,2,4-Triazole Derivatives as Potential Anticancer Agents. In Chemical Biology and Drug Design, 2024-12-01, 104, 6, pp. ISSN 17470277. Dostupné na: https://doi.org/10.1111/cbdd.70033., Registrované v: SCOPUS [1]/[1] GHANNAM, Iman A.Y. - ALI, Islam H. - BATRAN, Rasha Z. - ABO-ELFADL, Mahmoud T. - ALLAM, Rasha M. - IBRAHIM, Ibrahim M. - FAROUK, Faten. Investigating novel tubulin polymerization inhibitors: design, synthesis, LC/MS cellular permeability, in silico studies, and in vitro assessment. In Medicinal Chemistry Research, 2025-01-01, 34, 1, pp. 183-204. ISSN 10542523. Dostupné na: https://doi.org/10.1007/s00044-024-03327-8., Registrované v: WOS, SCOPUS [1]/[1] YANG, Jiayan - WANG, Ting - WANG, Pengchao - GAO, Chuanzhu - YANG, Jing. A Pair of Deep Red Phosphorescent Responsive Emissive Cyclometalated Iridium (III) Complexes as Carbonic Anhydrase Inhibitor and Effective Theranostic Photosensitizer. In Applied Organometallic Chemistry, 2025-03-01, 39, 3, pp. ISSN 02682605. Dostupné na: https://doi.org/10.1002/aoc.7882., Registrované v: WOS, SCOPUS [1]/[1] STRINGHETTA, Giulia Rodrigues - MASS, Eduardo Bustos - FARIA GOMES, Izabela Natalia - FONSECA PEIXOTO, Maria Clara - TEJADA, Amanda Helena - SUSUCCHI, Luciane - ALVES BEZERRA, Aryel José - SILVA RESENDE, Pedro Victor - VENDRÚSCULO, Vinicius - REIS, Rui Manuel - RUSSOWSKY, Dennis - OLIVEIRA, Renato José Da Silva. Design, synthesis and evaluation of quinazoline-chalcone hybrids as inducers of cell-cycle arrest and apoptosis in breast cancer via DNA damage and CDK2/ATR inhibition. In European Journal of Medicinal Chemistry Reports, 2025-04-01, 13, pp. Dostupné na: https://doi.org/10.1016/j.ejmcr.2025.100250., Registrované v: WOS, SCOPUS |
| OCA18. Characteristics of the output's impact on socio-economic practice | The output brings a significant contribution to socio-economic practice by presenting a new synthetic chalcone derivative (1C) with strong antiproliferative effects on colorectal cancer cells. Its ability to induce apoptosis through modulation of key signaling pathways and mitochondrial damage indicates potential for the development of more effective anticancer drugs. This discovery could improve colorectal cancer treatment, one of the most common and challenging cancer types. Successful application of such drugs may increase therapy success rates, reduce the burden on healthcare systems, and improve patients’ quality of life. Moreover, supporting further development and clinical testing of this derivative can stimulate investment and innovation in the biotechnology sector, contributing to economic growth and societal benefit. |
| OCA19. Characteristics of the output and related activities' impact on the educational process | The output and related activities significantly enrich the educational process in molecular biology, pharmacy, and oncology. Students gain insights into the antiproliferative mechanisms of new chalcone derivatives like 1C, including apoptosis and signaling pathway regulation. This research fosters critical thinking, analytical skills, and an interdisciplinary approach combining chemistry, biochemistry, and medicine. Involvement in projects on similar topics enhances students’ practical skills and motivation for research. Additionally, it familiarizes them with current trends in cancer treatment, contributing to the preparation of future professionals capable of developing innovative therapeutic approaches. |