Please use this identifier to cite or link to this item: https://hdl.handle.net/11147/7602
Title: Cycloartane-type sapogenol derivatives inhibit NF?B activation as chemopreventive strategy for inflammation-induced prostate carcinogenesis
Authors: Debeleç Bütüner, Bilge
Öztürk, Mert Burak
Tağ, Özgür
Akgün, İsmail Hakkı
Yetik Anacak, Günay
Bedir, Erdal
Korkmaz, Kemal Sami
Bedir, Erdal
Izmir Institute of Technology. Biotechnology and Bioengineering
Keywords: Astragenol
Cycloastragenol
NFκB
Prostate cancer chemoprevention
Issue Date: Jul-2018
Publisher: Elsevier Ltd.
Source: Debeleç Bütüner, B., Öztürk, M. B., Tağ, Ö., Akgün, İ. H., Yetik Anacak, G., Bedir, E., and Korkmaz, K. S. (2018). Cycloartane-type sapogenol derivatives inhibit NFκB activation as chemopreventive strategy for inflammation-induced prostate carcinogenesis. Steroids, 135, 9-20. doi:10.1016/j.steroids.2018.04.005
Abstract: Chronic inflammation is associated to 25% of cancer cases according to epidemiological data. Therefore, inhibition of inflammation-induced carcinogenesis can be an efficient therapeutic approach for cancer chemoprevention in drug development studies. It is also determined that anti-inflammatory drugs reduce cancer incidence. Cell culture-based in vitro screening methods are used as a fast and efficient method to investigate the biological activities of the biomolecules. In addition, saponins are molecules that are isolated from natural sources and are known to have potential for tumor inhibition. Studies on the preparation of analogues of cycloartane-type sapogenols (9,19-cyclolanostanes) have so far been limited. Therefore we have decided to direct our efforts toward the exploration of new anti-tumor agents prepared from cycloastragenol and its production artifact astragenol. The semi-synthetic derivatives were prepared mainly by oxidation, condensation, alkylation, acylation, and elimination reactions. After preliminary studies, five sapogenol analogues, two of which were new compounds (2 and 3), were selected and screened for their inhibitory activity on cell viability and NFκB signaling pathway activity in LNCaP prostate cancer cells. We found that the astragenol derivatives 1 and 2 as well as cycloastragenol derivatives 3, 4, and 5 exhibited strong inhibitory activity on NFκB signaling leading the repression of NFκB transcriptional activation and suppressed cell proliferation. The results suggested that these molecules might have significant potential for chemoprevention of prostate carcinogenesis induced by inflammatory NFκB signaling pathway.
URI: https://doi.org/10.1016/j.steroids.2018.04.005
https://hdl.handle.net/11147/7602
ISSN: 0039-128X
0039-128X
Appears in Collections:Bioengineering / Biyomühendislik
PubMed İndeksli Yayınlar Koleksiyonu / PubMed Indexed Publications Collection
Scopus İndeksli Yayınlar Koleksiyonu / Scopus Indexed Publications Collection
WoS İndeksli Yayınlar Koleksiyonu / WoS Indexed Publications Collection

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