Browsing by Subject "Drug cytotoxicity"

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Open Access
Cytotoxic activity of resveratrol in different cell lines evaluated by MTT and NRU assays
(Turkish Pharmacists Association, 2016) Anlar, H. G.; Bacanli, M.; Kutluk, B.; Başaran, A. A.; Başaran, N.
Oxidative stress is the state of imbalance between the level of antioxidant defence system and production of reactive oxygen species (ROS) and is involded in the progression of several diseases such as inflammation, cancer, neurodegenerative disorders and cardiovascular diseases. It is suggested that plant polyphenols may act as antioxidants and therefore it has anti-cancer activities. Resveratrol (RV), is a naturally occuring polyphenolic compound which is found in many plant species including grapes, nuts, blueberries and raspberries. Data indicated that it has anti-oxidant, anti-inflamatory and anti-cancer activities. But there are also some studies reported that RV has not protective effects aganist cancer. In this study, the cytotoxicity of RV in human breast adenocarcinoma (MDA-MB 231), human cervical cancer (HeLa) and Chinese hamster lung fibroblast (V79) cells were evaluated by Neutral Red uptake assay (NRU) and MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) assays after incubation at 24 h. We obtained more or the less same results by two cytotoxicity assays. In the concentrations between 2-400 μM, RV seemed not to induce a pronounced cytotoxicity in all cell types. Even at highest concentrations, it showed almost no cytotoxic effects. So the IC50 values were not calculated at the studied concentrations.
Open Access
Phenotype-based variation as a biomarker of sensitivity to molecularly targeted therapy in melanoma
(Royal Society of Chemistry, 2017) Senses, K. M.; Ghasemi M.; Akbar, M. W.; Isbilen, M.; Fallacara, A. L.; Frankenburg, S.; Schenone, S.; Lotem, M.; Botta, M.; Gure, A. O.
Transcriptomic phenotypes defined for melanoma have been reported to correlate with sensitivity to various drugs. In this study, we aimed to define a minimal signature that could be used to distinguish melanoma sub-types in vitro, and to determine suitable drugs by which these sub-types can be targeted. By using primary melanoma cell lines, as well as commercially available melanoma cell lines, we find that the evaluation of MLANA and INHBA expression is as capable as one based on a combined analysis performed with genes for stemness, EMT and invasion/proliferation, in identifying melanoma subtypes that differ in their sensitivity to molecularly targeted drugs. Using this approach, we find that 75% of melanoma cell lines can be treated with either the MEK inhibitor AZD6244 or the HSP90 inhibitor 17AAG.
Open Access
Quinoides and VEGFR2 TKIs influence the fate of hepatocellular carcinoma and its cancer stem cells
(Royal Society of Chemistry, 2017) Kahraman, D. C.; Hanquet, G.; Jeanmart, L.; Lanners, S.; Šramel, P.; Boháč, A.; Cetin-Atalay, R.
Bioactivities of quinoides 1–5 and VEGFR2 TKIs 6–10 in hepatocellular cancer (HCC) and cancer stem cells (HCSCs) were studied. The compounds exhibited IC50 values in μM concentrations in HCC cells. Quinoide 3 was able to eradicate cancer stem cells, similar to the action of the stem cell inhibitor DAPT. However, the more cytotoxic VEFGR TKIs (IC50: 0.4–3.0 μM) including sorafenib, which is the only FDA approved drug for the treatment of HCC, enriched the hepatocellular cancer stem cell population by 2–3 fold after treatment. An aggressiveness factor (AF) was proposed to quantify the characteristics of drug candidates for their ability to eradicate the CSC subpopulation. Considering the tumour heterogeneity and marker positive cancer stem cell like subpopulation enrichment upon treatments in patients, this study emphasises the importance of the chemotherapeutic agent choice acting differentially on all the subpopulations including marker-positive CSCs.