Scopus İndeksli Yayınlar Koleksiyonu
Permanent URI for this collectionhttps://hdl.handle.net/20.500.14627/7
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Article Citation - Scopus: 2Synthesis and Biological Evaluation of Novel Paracetamol-Triazole Conjugates(Society of Pharmaceutical Sciences of Ankara (FABAD), 2023) Kulabaş, Necla; Gurboga, Merve; Özakpınar, Özlem Bingöl; Liu, Jianyang; Jakobson, Per-johan; Danış, Özkan; Küçükgüzel, İlkay; Jakobsson, Per-Johan; Ogan, AyseBaşlangıç maddesi olarak parasetamol kullanılarak bazı yeni triazol içeren asetamid türevleri 9-20 sentezlendi ve yapıları FTIR, NMR (1H and 13C) ve kütle spektral verileri ile karakterize edildi. Beş insan kanser hücre hattına (akciğer kanseri A549, kronik miyelojenöz lösemi K562, meme kanseri MCF-7, prostat kanseri PC-3, nöroblastoma SH-SY5Y hücre hatları) karşı sentezlenen tüm moleküllerin in vitro sitotoksik aktiviteleri incelendi ve ayrıca seçiciliği tanımlamak için fare embriyonik fibroblast hücreleri (NIH/3T3) üzerinde sitotoksik etkileri MTT yöntemiyle test edildi. Ek olarak, on iki hedef bileşik 9-20, mPGES-1 ve COX-1/2 inhibe edici etkileri açısından tarandı. Sentezlenen bileşiklerin hiçbiri hem kanser hücrelerine hem de mPGES-1 ve COX-1/2 enzimlerine karşı anlamlı bir inhibisyon göstermezken, sağlıklı hücrelere karşı da sitotoksik olmadıkları belirlendi. Son olarak yeni sentezlenen bileşiklerin ADMET özellikleri in siliko yöntemler kullanılarak tahmin edildi.Article Citation - Scopus: 3Therapeutic Effects of Momordica Charantia L. Ethanolic Extract on Acetic Acid-Induced Ulcerative Colitis in Rats(Istanbul University Press, 2021) Ozbeyli, D.; Sen, A.; Aykac, A.; Terali, K.; Cilingir-Kaya, O.T.; Senkardes, I.; Sener, G.Objective: This study aims to investigate the effect of Momordica charantia L. (MoC) ethanolic extract on ulcerative colitis (UC) and was explored in vitro and in vivo. Materials and Methods: The rats were divided into control (C), saline-treated colitis (AA), MoC extract-treated colitis (AA+MoC), and sulfasalazine (SS)-treated colitis (AA+SS) groups. Colitis was induced by acetic acid. MoC extract, SS or saline were given to the related groups for 3 days. Interleukine-1β, malondialdehyde, glutathione levels, myeloperoxidase activity, bax/bcl-2 ratio, caspase-9 and caspase-3 levels were measured in colon and macroscopic and histopathologic examinations were done. Total phenolic/flavonoid content and biological activity of MoC were evaluated by in vitro analysis. Results: Compared to the control group, with acetic acid application interleukin-1β levels, myeloperoxidase activity, malondialdehyde levels, bax/bcl-2 ratio, caspase-9 and caspase-3 levels were significantly upregulated, while glutathione levels were significantly decreased in the AA group. In contrast, MoC and SS treatments reduced interleukin-1β, malondialdehyde levels, myeloperoxidase activity, bax/bcl-2 ratio, and caspase-9 and caspase-3 levels. Glutathione levels increased upon MoC or SS treatment. Increased macroscopic and microscopic scoring with AA improved with MoC or SS treatment, but the MoC or SS treated groups had higher score values than the control. Also, in vitro results showed that MoC exhibited 2,2-diphenyl-1- picrylhydrazyl and 2,2'-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid radical scavenging activity as well as significant antilipoxygenase activity. In addition, MoC extract showed a potent anti-inflammatory activity compared to standard indomethacin. Conclusion: Our biochemical, in vitro and histopathologic analysis indicate that MoC is likely to prove beneficial in UC therapy. © 2021 European Journal of Biology. All rights reserved.