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Carborane-Based Analog of Rev-5901 Attenuates Growth of Colon Carcinoma In Vivo.
dc.creator | Paskaš, Svetlana | |
dc.creator | Murganić, Blagoje | |
dc.creator | Kuhnert, Robert | |
dc.creator | Hey-Hawkins, Evamarie | |
dc.creator | Mijatović, Sanja | |
dc.creator | Maksimović-Ivanić, Danijela | |
dc.date.accessioned | 2022-10-25T11:57:17Z | |
dc.date.available | 2022-10-25T11:57:17Z | |
dc.date.issued | 2022 | |
dc.identifier.issn | 1420-3049 | |
dc.identifier.uri | https://www.mdpi.com/1420-3049/27/14/4503 | |
dc.identifier.uri | http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=PMC9321230 | |
dc.identifier.uri | http://radar.ibiss.bg.ac.rs/handle/123456789/5088 | |
dc.description.abstract | Lipoxygenases convert polyunsaturated fatty acids into biologically active metabolites such as inflammatory mediators-prostaglandins and leukotrienes. The inhibition of lipoxygenases is increasingly employed in the treatment of cancer. We evaluated the anticancer potential of two novel 5-lipoxygenase inhibitors, named CarbZDNaph and CarbZDChin, which are analogues of the commercially available inhibitor Rev-5901. The in vitro segment of this study was conducted on a mouse colorectal carcinoma cell line-CT26CL25. For an in vivo model, we induced tumors in BALB/c mice by the implantation of CT26CL25 cells, and we treated the animals with potential inhibitors. A 48 h treatment resulted in diminished cell viability. Calculated IC50 values (half-maximal inhibitory concentrations) were 25 μM, 15 μM and 30 μM for CarbZDNaph, CarbZDChin and Rev-5901, respectively. The detailed analysis of mechanism revealed an induction of caspase-dependent apoptosis and autophagy. In the presence of chloroquine, an autophagy inhibitor, we observed an increased mortality of cells, implying a cytoprotective role of autophagy. Our in vivo experiment reports tumor growth attenuation in animals treated with CarbZDChin. Compounds CarbZDNaph and Rev-5901 lacked an in vivo efficacy. The results presented in this study display a strong effect of compound CarbZDChin on malignant cell growth. Having in mind the important role of inflammation in cancer development, these results have a significant impact and are worthy of further evaluation. | |
dc.publisher | Basel: MDPI | |
dc.relation | info:eu-repo/grantAgreement/MESTD/inst-2020/200007/RS// | |
dc.relation | info:eu-repo/grantAgreement/MESTD/inst-2020/200007/RS// | |
dc.rights | openAccess | |
dc.rights.uri | https://creativecommons.org/licenses/by/4.0/ | |
dc.source | Molecules (Basel, Switzerland) | |
dc.subject | 5-lipoxygenase | |
dc.subject | CT26CL25 | |
dc.subject | Rev-5901 | |
dc.subject | Carboranes | |
dc.subject | Colorectal carcinoma | |
dc.title | Carborane-Based Analog of Rev-5901 Attenuates Growth of Colon Carcinoma In Vivo. | |
dc.type | article | en |
dc.rights.license | BY | |
dc.rights.holder | © 2022 by the authors. Licensee MDPI, Basel, Switzerland. | |
dc.citation.issue | 14 | |
dc.citation.volume | 27 | |
dc.identifier.doi | 10.3390/molecules27144503 | |
dc.identifier.pmid | 35889376 | |
dc.identifier.scopus | 2-s2.0-85135623350 | |
dc.identifier.wos | 000832129900001 | |
dc.citation.apa | Paskaš, S., Murganić, B., Kuhnert, R., Hey-Hawkins, E., Mijatović, S., & Maksimović-Ivanić, D. (2022). Carborane-Based Analog of Rev-5901 Attenuates Growth of Colon Carcinoma In Vivo. Molecules (Basel, Switzerland), 27(14), 4503. | |
dc.citation.vancouver | Paskaš S, Murganić B, Kuhnert R, Hey-Hawkins E, Mijatović S, Maksimović-Ivanić D. Carborane-Based Analog of Rev-5901 Attenuates Growth of Colon Carcinoma In Vivo. Molecules. 2022;27(14):4503. | |
dc.citation.spage | 4503 | |
dc.type.version | publishedVersion | |
dc.identifier.fulltext | https://radar.ibiss.bg.ac.rs/bitstream/id/11006/molecules-27-04503.pdf | |
dc.citation.rank | M22 |