Anticancer Activity of Centaurea babylonica L.

Today, new agents are required to protect from cancer due to the side effects and some deficiencies in the medical drugs used to treat cancer. Because of this reason, active substances used in drugs which is herbal origin of the treatment of tumors as an alternative agent studies continues to increase. It has been determined that some species belonging to the genus Centaurea have cytotoxic effect. Centaurea babylonica plant has not been performed on cytotoxicity before. Plant was collected from Çamlıyayla district of Mersin province. Methanol extract was prepared from the plant and cytotoxicity tests of the extracts were performed. In vitro cytotoxic effects of extraneous material obtained from the supernatant were determined by MTT assay using C6 (Glioma), A549 (human lung adenocarcinoma) and MCF-7 (human breast cancer) cell lines. Cytotoxic effect was found high in methanol extract. In the DNA synthesis inhibition test of extract, the extract was found to show a high inhibition from the cisplatin used as a control. The 3T3 test, in which the methanol extract showed no toxic effect on healthy fibroblast cells, was supported

Cytotoxic, antiproliferative and apoptotic effects of new benzimidazole derivatives on A549 lung carcinoma and C6 glioma cell lines

Benzimidazole ring is a versatile structure which has been extensively utilized in medicinal chemistry. Since we are working on 1,2-disubstutited benzimidazoles, we have reported new antitumor active derivatives. As a continuation to our previous work, we have synthesized a new series of 1-(2-aryl-2-oxoethyl)-2-[(N,N- dimethylamino/pyrrolidinyl/piperidinyl)thiocarbamoyl] benzimidazole derivatives. Anticancer activity of the compounds was evaluated using MTT assay, BrdU assay and flow cytometric analysis on A549 human lung carcinoma and C6 rat glioma cell lines. Compounds bearing dimethylamino moiety exhibited higher antitumor activity

TİTANYUM DİOKSİTİN A549 HÜCRELERİ ÜZERİNDEKİ APOPTOTİK ETKİLERİ

Metal temelli bileşikler potansiyel etkilerinden ve az toksisiteye neden olduklarından dolayı uzun zamandır kullanılmaktadır. Metal bileşik sisplatin çeşitli kanser türlerine karşı tıbbi olarak kullanılmış ve yan etkiler göstermiştir. Biz bu çalışmada sisplatine alternatif ajan olarak düşündüğümüz titanyum dioksitin A549 hücreleri üzerindeki etkilerini ve apoptotik mekanizmasını araştırdık. Titanyum dioksitin 24, 48 ve 72 saatlik sürelerdeki zamana ve konsantrasyon aralığına bağlı olarak antiproliferatif etkilerini MTT canlılık analizini kullanarak belirledik. Titanyum dioksitin apoptozisi tetiklediğini saptadık. Titanyum dioksitin IC30 konsantrasyonu, 72 saat süresince A549 hücreleri üzerinde uygulandığında erken ve geç apoptozisi tetiklediği belirlendi. Titanyum dioksitin IC30 konsantrasyonu, 72 saat süresince A549 hücreleri üzerine uygulandığında mitokondriyal membran potansiyelini azaltarak apoptozisi tetikledi. Buna rağmen kaspaz-3 aktivitesi gözlenmedi. Titanyum dioksit kaspazdan bağımsız bir yol izleyerek apoptozisi tetiklemiştir diyebiliriz. Titanyum dioksitin IC30 konsantrasyonun 72 saatlik süre sonundaki hematoksilen ve eozin, TUNEL, BrdU, Bcl-2 ve Bax immünositokimyasal analizleri sonucunda  apoptotik indekslerinde artış belirlendi. Titanyum dioksitin IC30 konsantrasyonun uygulandığı A549 hücrelerinde 72 saatlik süre sonunda konfokal ve TEM mikrokobisi kullanılarak çeşitli apoptotik yapılar gözlendi. Bu sonuçlar titanyum dioksitin A549 hücreleri üzerinde antiproliferatif ve apoptotik etkilerini ve sisplatine eş potansiyel kemoterapötik bir ajan olabileceğini göstermektedir

Novel benzothiazole based imidazole derivatives as new cytotoxic agents against glioma (C6) and liver (HepG2) cancer cell lines

In this work, some novel N-(6-substituted-benzothiazol-2-yl)-2-[[4,5-dimethyl-1-((p-tolyl/4-nitrophenyl)amino)-1H-imidazol-2-yl]thio]acetamide derivatives were synthesized and searched for their cytotoxic activities against C6 and HepG2 tumor cells. Among all compounds, the most active compound was determined as compound 7. It was calculated IC50 value about 15.67 µg/mL through C6 tumor cell lines and also compound 2, 4, 5, 6 were observed as good cytotoxic agents against HepG2 tumor cells. Findings about antiproliferative activity studies have encouraged the acquirement of new similar compounds in undergoing studies

Synthesis of novel 3, 5, 6-trisubstituted triazine derivatives and their biological activity evaluation as potential antitumor and anti-inflammatory agents

In this study, new 3, 5, 6-trisubstituted 1, 2, 4-triazine derivatives (1-9) were synthesized and their structures were determined by using NMR, IR and Mass spectroscopic methods. In vitro antitumor activities against MCF-7 breast adenocarcinoma and C6 rat glioma cell lines were evaluated via MTT colorimetric assay. Among the compounds, compound 4 (IC50=21.0 µg/mL) was found as the most active one against C6 cell line, whereas compound 5 (IC50=9.5 µg/mL) was found the most potent compound against MCF-7 cell line and both of compounds had higher activity than cisplatin in their line. Furthermore, IC50 value of compound 6 was found as 26.0 µg/mL against C6 which was very close to cisplatin potency (IC50=23.5 µg/mL). Besides, all compounds were tested to determine their lipoxygenase (LOX) inhibitory activity. Compounds 1 and 6 showed LOX inhibition with percentages of 43.35% and 38.79% at 100 µg/mL concentration, respectively. The obtained results on cell lines inspire to synthesise new and more potent molecules compounds as anticancer agents

Synthesis and biological evaluation of some 1,2-disubstituted benzimidazole derivatives as new potential anticancer agents

The synthesis of some new 1-(2-aryl-2-oxoethyl)-2-[(morpholine-4-yl)thioxomethyl]benzimidazole derivatives and investigation of their anticancer activities were the aims of this work. 2-(Chloromethyl)benzimidazole compound was reacted with sulfur and morpholine via WillgerodtKindler reaction to give 2-[(morpholine-4-yl)thioxomethyl]benzimidazole. Then, the obtained compound was reacted with appropriate -bromoacetophenone derivatives in the presence of potassium carbonate to give the final products. Structure elucidation of the final compounds was achieved by FT-IR, 1H NMR spectroscopy and MS spectrometry. The anticancer activities of the final compounds were evaluated by MTT assay, BrdU method, and flow cytometric analysis on C6, MCF-7, and A549 tumor cells. Most of the synthesized compounds exhibited considerable selectivity against the MCF-7 and C6 cell lines

Novel benzimidazole derivatives: Cytotoxic and apoptotic properties on lung cancer cell line

Background: Benzimidazole derivatives are privileged molecules known to have a wide variety of biological activities. In medicinal chemistry, due to the ring's structural similarity to nucleotides, its derivatives were investigated as new chemotherapeutic agents. Our research group have been studying 1,2-disubstituted benzimidazoles, including thiocarbamoyl group and their potential anticancer activity. Based on previous findings, we synthesized novel 1-[2-(4-substituted phenyl-2-oxoethyl)]-2-[(2/3/4-substituted phenylpiperidin-1-yl)thiocarbamoyl]benzimidazole derivatives (3a-o).Methods: The obtained fifteen derivatives were studied on A549 adenocarcinomic human alveolar basal epithelial cell line and mouse L929 fibroblastic cell line to determine their cytotoxic activity. These compounds were also investigated to identify their apoptotic properties.Results and Discussion: The structures of the compounds based on three different groups differ from each other with the phenyl substituents bonded to the piperazine ring. All of the compounds showed remarkable antitumor activity, but the first five compounds bearing non-substituted phenyl moiety exhibited selective cytotoxicity when compared in terms of potencies to the normal cell line.Conclusion: Compounds 3j, 3m and 3n were identified as the most apoptotic derivatives; however, compounds 3e and 3h provoked apoptosis with the percentages of 10.6 and 10.9% and selective cytotoxicity