Cycloartane-Type Sapogenol Derivatives Inhibit Nf Kappa B Activation As Chemopreventive Strategy For Inflammation-Induced Prostate Carcinogenesis
| العنوان: | Cycloartane-Type Sapogenol Derivatives Inhibit Nf Kappa B Activation As Chemopreventive Strategy For Inflammation-Induced Prostate Carcinogenesis |
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| المؤلفون: | Kemal Sami Korkmaz, Ismail Hakki Akgun, Erdal Bedir, Ozgur Tag, Mert Burak Ozturk, Bilge Debelec-Butuner, Gunay Yetik-Anacak |
| المساهمون: | Izmir Institute of Technology, Bedir, Erdal, Izmir Institute of Technology. Biotechnology and Bioengineering |
| بيانات النشر: | Aperta, 2018. |
| سنة النشر: | 2018 |
| مصطلحات موضوعية: | 0301 basic medicine, Male, Sapogenins, Transcription, Genetic, Carcinogenesis, Clinical Biochemistry, Apoptosis, Astragenol, medicine.disease_cause, Biochemistry, Chemoprevention, Dinoprostone, 03 medical and health sciences, chemistry.chemical_compound, NF?B, 0302 clinical medicine, Endocrinology, Cell Line, Tumor, LNCaP, medicine, Humans, Cycloastragenol, NF kappa B, Viability assay, Molecular Biology, Inflammation-induced carcinogenesis, Cell Proliferation, Pharmacology, Inflammation, Chemistry, Cell growth, Semi-synthesis, Organic Chemistry, NF-kappa B, Cancer, Prostatic Neoplasms, medicine.disease, In vitro, Triterpenes, 3. Good health, 030104 developmental biology, 030220 oncology & carcinogenesis, Prostate cancer chemoprevention, Cancer research, Signal transduction, NFκB, Signal Transduction |
| الوصف: | PubMed: 29678446 2-s2.0-85046477155 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 NF?B 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 NF?B signaling leading the repression of NF?B transcriptional activation and suppressed cell proliferation. The results suggested that these molecules might have significant potential for chemoprevention of prostate carcinogenesis induced by inflammatory NF?B signaling pathway. © 2018 Elsevier Inc. 113Z078 Consejo Nacional para Investigaciones Científicas y Tecnológicas, CONICIT This work was supported by Turkish Scientific and Technological Research Council (TUBITAK) with the project number 113Z078 to BDB. |
| وصف الملف: | application/pdf |
| تدمد: | 8504-6477 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6f62d90af317fc4d453f24ad20e07b5c https://aperta.ulakbim.gov.tr/record/33299 |
| حقوق: | OPEN |
| رقم الأكسشن: | edsair.doi.dedup.....6f62d90af317fc4d453f24ad20e07b5c |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 85046477 |
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