Anti-proliferative effects of indomethacin, acemetacin and their tromethamine salts in HCT116 human colon cancer cells
| العنوان: | Anti-proliferative effects of indomethacin, acemetacin and their tromethamine salts in HCT116 human colon cancer cells |
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| المؤلفون: | Gökçe Cihan Üstündağ, Meltem Muftuoglu, Nilgün Karalı, Berna Somuncu |
| المساهمون: | Acibadem University Dspace |
| المصدر: | Volume: 51, Issue: 2 161-166 İstanbul Journal of Pharmacy |
| بيانات النشر: | İstanbul Üniversitesi, 2021. |
| سنة النشر: | 2021 |
| مصطلحات موضوعية: | Drug, acemetacin, Chemistry, Tromethamine, Cell growth, Farmakoloji ve Eczacılık, media_common.quotation_subject, Indomethacin, Acemetacin, Pharmacology, HCT116, In vitro, tromethamine, chemistry.chemical_compound, In vivo, indomethacin,acemetacin,tromethamine,HCT116,anti-cancer, medicine, Cytotoxic T cell, Pharmacology and Pharmacy, anti-cancer, Glycolic acid, media_common, medicine.drug |
| الوصف: | Background and Aims: Since 1980's, several preclinical studies have been published on the anti-colorectal cancer activity of the nonsteroidal anti-inflammatory drug indomethacin. The direct anti-proliferative effect of indomethacin seems to occur via a variety of reported COX-independent mechanisms. Acemetacin is a glycolic acid ester derivative of indomethacin and contrary to indomethacin, there is not much published research on anti-cancer effects of acemetacin. Herein, we compared the in vitro anti-proliferative properties of indomethacin, acemetacin, and their tromethamine salts in HCT116 colon cancer cells. Methods: The tromethamine salts of indomethacin and acemetacin were synthesized and the structures were established by microanalysis, IR, 1H-NMR, 13C-NMR (APT) and 2D-NMR (HSQC and HMBC) spectrometry. Cell proliferation assays were performed using xCELLigence real-time cell analysis system. Results: Indomethacin exhibited profound inhibitory effects with IC50 values at low micromolar ranges. Acemetacin exhibited far lower cytotoxic activity as compared to that of indomethacin. Surprisingly, indomethacin-tromethamine salt was 2-fold and 4.4-fold more potent than indomethacin at 48 and 72 h, respectively, while maintaining its activity at 24 h. The tromethamine salt of acemetacin was more potent than acemetacin at 24 h and 48 h post-treatment. Conclusion: The anti-proliferative effect of indomethacin in HCT116 cells was found to be at low micro-molar levels. The esterification of indomethacin with glycolic acid caused a strong decrease in anti-proliferative effect. The salt formation caused a positive effect on the anti-proliferative activity of indomethacin and indomethacin-tromethamine salt may be a promising candidate for additional in vivo studies. |
| وصف الملف: | application/pdf |
| اللغة: | English |
| تدمد: | 2587-2087 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::535dc0841ba4c2545ac0d5c004e26235 https://dergipark.org.tr/tr/pub/iujp/issue/63480/876788 |
| حقوق: | OPEN |
| رقم الأكسشن: | edsair.doi.dedup.....535dc0841ba4c2545ac0d5c004e26235 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 25872087 |
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