Cytotoxic effect of thienopyridine derivatives on human ovarian cancer cells
| العنوان: | Cytotoxic effect of thienopyridine derivatives on human ovarian cancer cells |
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| المؤلفون: | Braica, Andrea |
| المساهمون: | Čikeš Čulić, Vedrana, Gujinović, Diana, Omerović, Jasminka |
| سنة النشر: | 2022 |
| مصطلحات موضوعية: | karcinom jajnika, ovarian cancer, thienopiridine derivatives, tienopiridinski derivat, cytotoxicity, citotoksičnost, BIOMEDICINA I ZDRAVSTVO. Farmacija. Medicinska biokemija, BIOMEDICINE AND HEALTHCARE. Pharmacy. Medical Biochemistry, karcinom jajnika, tienopiridinski derivat, citotoksičnost |
| الوصف: | Cilj istraživanja: Cilj ovog istraživanja utvrditi je potencijalno citotoksično djelovanje derivata tieno[2,3-b]piridina na staničnoj liniji humanog karcinoma jajnika. Materijali i metode: Citotoksičnost spojeva tieno[2,3-b]piridina, odnosno inhibitora 5, 6, 8 i 9 ispitivana je na SKOV-3 staničnoj liniji korištenjem MTT metode na temelju koje se određuje postotak metabolički aktivnih stanica. Učinak tieno[2,3-b]piridina ispitivan je u sedam različitih koncentracija nakon 4, 24, 48 i 72 sata inkubacije. Djelotvornost ispitivanih spojeva određena je spektrofotometrijski pri valjnoj duljini od 570 nm. Rezultati: Rezultati su prikazani grafički u odnosu vremena inkubacije i postotka metabolički aktivnih stanica. Svi ispitivani spojevi pokazali su citotoksičnu aktivnost ovisnu o koncentraciji i vremenu inkubacije. Citotoksična aktivnost nije u svim slučajevima proporcionalna porastu koncentracije inhibitora i vremena inkubacije. Inhibitor 6 pokazao je najmanju citotoksičnost. Inhibitor 8 pokazao je najveću citotoksičnost i to pri koncentraciji od 5 μmol/L nakon inkubacije od 72h gdje se postotak metabolički aktivnih stanica smanjio na oko 40 %. Također, vrijednosti IC50 izmjerene kod inhibitora 8 iznosile su 8,276 μmol/L nakon inkubacije od 24h, 5,68 μmol/L nakon 48h, a 4,093 μmol/L nakon 72h. Zaključak: In vitro izlaganje stanica karcinoma jajnika derivatima tieno[2,3-b]piridina dovodi do smanjenja broja živih stanica. Citotoksični učinak ispitivanih spojeva ovisi o koncentraciji i vremenu inkubacije. U nekim slučajevima citotoksični učinak nije proporcionalan povećanju koncentracije i vremena inkubacije jer dolazi do blagog porasta metabolički aktivnih stanica zbog oporavka stanica. Najslabiji citotoksični učinak pokazao je inhibitor 6, a najjači inhibitor 8. Dobivenim rezultatima potvrđena je hipoteza ovog istraživanja. Potrebna su dodatna in vitro i in vivo ispitivanja na životinjama kako bi se utvrdio mehanizam njihovog citotoksičnog učinka i potencijal za razvoj novih lijekova za liječenje karcinoma jajnika. The aim of the research: The aim of the research is to examine the potential cytotoxic effects of tieno[2,3-b]piridine derivates on human ovarian cancer cells. Materials and methods: The cytotoxicity of thieno[2,3-b]pyridine compounds, i.e. inhibitors 5, 6, 8 and 9, was tested on the SKOV-3 cell line using the MTT method, based on which the percentage of metabolically active cells is determined. The effect of thieno[2,3-b]pyridine was examined in seven different concentrations after 4, 24, 48 and 72 hours of incubation. The effectiveness of the tested compounds was determined spectrophotometrically at a wavelength of 570 nm. Results: The results are presented graphically in relation to the incubation time and the percentage of metabolically active cells. All tested compounds showed cytotoxic activity dependent on concentration and incubation time. Cytotoxic activity is not in all cases proportional to the increase in inhibitor concentration and incubation time. Inhibitor 6 showed the lowest cytotoxicity. Inhibitor 8 showed the highest cytotoxicity at a concentration of 5 μmol/L after incubation for 72 hours, where the percentage of metabolically active cells decreased to about 40 %. Also, the IC50 values measured for inhibitor 8 were 8.276 μmol/L after 24h incubation, 5.68 μmol/L after 48h, and 4.093 μmol/L after 72h. Conclusion: In vitro exposure of ovarian cancer cells to thieno[2,3-b]pyridine derivatives leads to a decrease in the number of live cells. The cytotoxic effect of the tested compounds depends on the concentration and incubation time. In some cases, the cytotoxic effect is not proportional to the increase in concentration and incubation time because there is a slight increase in metabolically active cells due to cell recovery. The weakest cytotoxic effect was shown by inhibitor 6, and the strongest by inhibitor 8. The obtained results confirmed the hypothesis of this research. Additional in vitro and in vivo animal studies are needed to determine their cytotoxic effect and the potential development of new drugs for the treatment of ovarian cancer. |
| وصف الملف: | application/pdf |
| اللغة: | Croatian |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=dedup_wf_001::d0ec617443d0cb1941e95e0b3cb5048c https://www.bib.irb.hr/1223201 |
| حقوق: | OPEN |
| رقم الأكسشن: | edsair.dedup.wf.001..d0ec617443d0cb1941e95e0b3cb5048c |
| قاعدة البيانات: | OpenAIRE |
| الوصف غير متاح. |