Journals / Türk Tarım ve Doğa Bilimleri Dergisi / 2020 / Cilt: 7 - Sayı: 2

Antiproliferative Activity of α-Tomatine and Molecular Target Identification

Pages
290–300
DOI
—
🏛️Bibliographic metadata and full text access for this article are provided via DergiPark.
DergiPark Record ↗
✨

AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

The results indicated that α-tomatinehas a significant inhibition effect on both EGFR and HER2. α-tomatineformed some key interaction into ATP binding sites of EGFR and HER2.

📌 3 Key Takeaways

🎯
Objective & Hypothesis:α-tomatine is a glycoalkaloid derived from tomato varietiesthat has been reported to possess various anticancer properties.
📊
Key Findings & Data:The aim of this study is to investigate the anticancer effect of α-tomatine and its related mechanisms in lung cancer cells.Cytotoxicity and apoptosis induction of α-tomatine were determined by MTT assay and annexin V-FITC staining methods, respectively.For tyrosine kinase activity, TK-1 kinase selectivity profiling assay and molecular modelling study were performed.
💡
Conclusion & Impact:The results indicated that α-tomatinehas a significant inhibition effect on both EGFR and HER2. α-tomatineformed some key interaction into ATP binding sites of EGFR and HER2.
🔬Design:Modeling & Simulation
📍Scope:Comprehensive Sample
⚙️Variables:Domain Parameters

Özet

α-tomatine is a glycoalkaloid derived from tomato varietiesthat has been reported to possess various anticancer properties. However, its inhibitory effects on epidermal growth factor receptorisstill poorly understood. The aim of this study is to investigate the anticancer effect of α-tomatine and its related mechanisms in lung cancer cells.Cytotoxicity and apoptosis induction of α-tomatine were determined by MTT assay and annexin V-FITC staining methods, respectively.For tyrosine kinase activity, TK-1 kinase selectivity profiling assay and molecular modelling study were performed. The DNA cleavage activityof α-tomatinewas investigated using agarose gel electrophoretic method. α-tomatine proved to possess an outstanding antiproliferative activity against A549 and Jurkat cells without noticeable toxicity on PBMC. The results indicated that α-tomatinehas a significant inhibition effect on both EGFR and HER2. α-tomatineformed some key interaction into ATP binding sites of EGFR and HER2. Furthermore, α-tomatine strongly disintegrated DNA atlowconcentrations in the presence of iron(II) complexes. The current findings suggest that α-tomatine has a distinguished receptor tyrosine kinase inhibition profile from erlotinib and might be a potential drug candidate for treatment of NSCLC.

🔖

Cite This Article

CIFTCI, H. I. (2020). Antiproliferative Activity of α-Tomatine and Molecular Target Identification. Türk Tarım ve Doğa Bilimleri Dergisi, Cilt: 7 - Sayı: 2, 290–300. https://ajindex.com/articles/330647

📄 Full Text PDF Viewer

📄

PDF görüntüleyici hazırlanıyor...

References (9)

  1. Ali, T. F. S., Ciftci, H. I., Radwan, M. O., Koga, R., Ohsugi, T., Okiyama, Y., Honma, T., Nakata, A., Ito, A., Yoshida, M.,Fujita, M., Otsuka, M.2019. New SIRT2 inhibitors: Histidine-based bleomycin spin-off. Bioorgan Med Chem, 27, (9), 1767-1775.
  2. Arkhipov, A.,Shan, Y. B., Kim, E. T., Dror, R. O.,Shaw, D. E. 2013. Her2 activation mechanism reflects evolutionary preservation of asymmetric ectodomain dimers in the human EGFR family. Elife, 2. Banappagari, S., Corti, M., Pincus, S., Satyanarayanajois, S.2012. Inhibition of protein-protein interaction of HER2-EGFR and HER2-HER3 by a rationally designed peptidomimetic. J Biomol Struct Dyn, 30, (5), 594-606.
  3. Bayrak, N.,Yildirim, H., Yildiz, M., Radwan, M. O.,Otsuka, M., Fujita, M.,Tuyun, A. F.,Ciftci, H. I., 2019. Design, synthesis, and biological activity of Plastoquinone analogs as a new class of anticancer agents. Bioorg Chem, 92. Chan, B. A., Hughes, B. G. M.2015. Targeted therapy for non-small cell lung cancer: current standards and the promise of the future. Transl Lung Cancer R, 4, (1), 36-54.
  4. Chao, M. W.,Chen, C. H., Chang, Y. L., Teng, C. M.,Pan, S. L. 2012. Alpha-Tomatine-Mediated Anti-Cancer Activity In Vitro and In Vivo through Cell Cycle-and Caspase-Independent Pathways. Plos One, 7, (9), 1-13.
  5. Ciftci, H. I., Bayrak, N., Yildirim, H., Yildiz, M., Radwan, M. O., Otsuka, M., Fujita, M., Tuyun, A. F.2019. Discovery andstructure-activity relationship of plastoquinone analogs as anticancer agents against chronic myelogenous leukemia cells. Arch Pharm. Ciftci, H. I.,Ozturk, S. E., Ali, T. F. S.,Radwan, M. O., Tateishi, H., Koga, R., Ocak, Z.,Can, M., Otsuka, M.,Fujita, M. 2018. The First Pentacyclic Triterpenoid Gypsogenin Derivative Exhibiting Anti-ABL1 Kinase and Anti-chronic Myelogenous Leukemia Activities. Biol Pharm Bull, 41, (4), 570-574.
  6. Ciftci, H.I., Radwan, M. O., Ozturk, S.E., Ulusoy, N. G., Sozer, E., Ellakwa, D. E., Ocak, Z., Can, M., Ali, T. F. S., Abd-Alla,H. I., Yayli, N.,Tateishi,H., Otsuka, M., Fujita, M.2019.
  7. Design, Synthesis and Biological Evaluation of Pentacyclic Triterpene Derivatives: Optimization of Anti-ABL Kinase Activity. Molecules, 24, (19), 1-15.
  8. Citri, A., Yarden, Y.2006. EGF-ERBB signalling: towards the systems level. Nat Rev Mol Cell Bio, 7, (7), 505-516.
  9. Denisenko, T. V., Budkevich, I. N., Zhivotovsky, B.2018. Cell death-based treatment of lung adenocarcinoma. Cell Death Dis, 9. Dong, Q. J., Yu, P. F., Ye, L., Zhang, J. Z.,Wang, H. B., Zou, F. X., Tian, J. W., Kurihara,