2nd International Conference on Chemo and Bioinformatics ICCBIKG 2023 (503-506)
АУТОР(И) / AUTHOR(S): Otilija Keta, Jelena Bošković, Vladana Petković, Neda Đorđević, Vladimir Dobričić, Olivera Čudina, Snežana B. Pajović
Е-АДРЕСА / E-MAIL: otilijak@vin.bg.ac.rs
DOI: 10.46793/ICCBI23.503K
САЖЕТАК / ABSTRACT:
Among novel cancer chemotherapy approaches, the use of cyclooxygenases (COXs) and lipoxygenases (LOXs) inhibitors represents a promising mean for cancer treatment showing lesser toxicity comparing to the currently used cytotoxic drugs. This study detailed the synthesis of three novel compounds: 1ME, BHTK-AA, and IBU-Ac, each with the capability to concurrently inhibit both COX-2 and 5-LOX. Subsequently, we assessed their effectiveness in inhibiting the proliferation of HeLa cervical and MIA PaCa-2 pancreatic cancer cells. The IC50 values for both examined cell lines were approximately 40 μM, indicating the promising inhibitory potential of the IBU-Ac compound in both types of cancer cells. This finding is positioned to stimulate further investigation into the potential application of IBU-Ac against these particular types of cancers, while also advocating its use in combination with standard anti-cancer protocols, i.e., chemoterapeutics or radiation therapy. The results of this work are also advocating the development and refinement of dual COX-2 and 5-LOX inhibitors, thus improving their efficacy and safety.
КЉУЧНЕ РЕЧИ / KEYWORDS:
cancer, dual COX-2 and 5-LOX inhibitors, cytotoxicity
ЛИТЕРАТУРА / REFERENCES:
- E.R. Greene, S. Huang, C.N. Serhan, D. Panigrahy., Regulation of inflammation in cancer by eicosanoids, Prostaglandins and other lipid mediators, 96 (2011) 27-36.
- L. Goossens, N. Pommery, J.P. Hénichart., COX-2/5-LOX dual acting anti-inflammatory drugs in cancer chemotherapy, Current topics in medicinal chemistry, 7 (2007) 283-296.
- X.H. Che, C.L. Chen, X.L. Ye, G.B. Weng, X.Z. Guo, W.Y. Yu, J. Tao, Y.C. Chen, X. Chen., Dual inhibition of COX-2/5-LOX blocks colon cancer proliferation, migration and invasion in vitro, Oncology reports, 35 (2016) 1680-1688.
- M. Rudrapal, W.A. Eltayeb, G. Rakshit, A.A. El-Arabey, J. Khan, S.M. Aldosari, B. Alshehri, M. Abdalla., Dual synergistic inhibition of COX and LOX by potential chemicals from Indian daily spices investigated through detailed computational studies, Scientific reports, 13 (2023) 8656.
- J. Bošković, V. Dobričić, M. Mihajlović, J. Kotur-Stevuljević, O. Čudina., Synthesis, Evaluation of Enzyme Inhibition and Redox Properties of Potential Dual COX-2 and 5-LOX Inhibitors, Pharmaceuticals (Basel). 16 (2023) 549.
- M. Ghasemi, T. Turnbull, S. Sebastian, I. Kempson., The MTT Assay: Utility, Limitations, Pitfalls, and Interpretation in Bulk and Single-Cell Analysis, International journal of molecular sciences. 22 (2021) 12827.