thiobarbituric-acid and Neoplasms

Cancer is one of the most important reasons for mortality worldwide. Several synthetic products have shown valuable efficiency as an anticancer medicines. Chromene derivatives have long been used as the promising compounds which are potent in inhibition of the growth of tumors.. In this study, we investigate an anticancer activity of barbituric/thiobarbituric acid-based chromene derivates. For this purpose, viability, antioxidant and apoptotic assays were conducted using three different cancer cell lines (A2780, MCF7, and A549). In most cases, the antiproliferative activity of barbituric acid-based derivatives was higher than that of thiobarbituric acid-based compounds. Among 14 compounds, compound 4g was the most potent one, which showed the highest effect on cells by increasing the accumulation of ROS (up to 540% increase), increasing the level of caspase-3 and caspase-9 (~ 35% increase), and decreasing the mitochondrial membrane potential (2.5 folds reduction). To characterize the type of cell death involved into our experiment Annexin V/PI double staining of compound 4g was performed. The results showed that the number of late apoptotic and/or necrotic cells (Ann V + /PI +) increased fourfold upon treatment with IC. Overall, the anti-proliferative activity of barbituric acid-based derivatives was higher than that of thiobarbituric acid compounds, and compound 4g can be introduced as a potential candidate to prevent various cancers.

Topics: Antioxidants; Apoptosis; Barbiturates; Benzopyrans; Caspase 3; Caspase 9; Cell Death; Cell Line, Tumor; Cell Proliferation; Cell Survival; Drug Screening Assays, Antitumor; Humans; Neoplasms; Reactive Oxygen Species; Structure-Activity Relationship; Thiobarbiturates

Two thiobarbituric acid-functionalized pyrene derivatives (P1, P2) have been synthesized to explore the photophysical properties and photodynamic activity of dyes of this type. Both compounds exhibit an intense intramolecular charge transfer (ICT) band at ca. 470 nm, which is absent in the spectra of the precursor. P1 and P2 exhibit singlet oxygen generation on irradiation with light with moderate singlet oxygen yields of 0.36 and 0.32, respectively, in DMSO. P1 showed better photodynamic activity against MCF-7 cells with an IC

Topics: Humans; MCF-7 Cells; Neoplasms; Photochemotherapy; Photosensitizing Agents; Pyrenes; Singlet Oxygen; Thiobarbiturates

Topics: Antineoplastic Agents; Cell Line, Tumor; Cisplatin; DNA-Directed DNA Polymerase; Enzyme Inhibitors; Humans; Indoles; Molecular Docking Simulation; Neoplasms; Pyrimidines; Small Molecule Libraries; Thiobarbiturates

Since raised oxidative stress (OS) or weak antioxidant defence or both are considered to be important players in multimechanistic pathogenesis of cancer, the present study was undertaken to evaluate their possible involvement in the pathogenesis of this disease in the local population. Levels of plasma vitamin C, vitamin E, total antioxidant activity (TAA) and thiobarbituric acid reacting substances (TBARS) as a marker of OS were measured in 20 cancer patients (Mean age 63.1 + 9.3 yr.) and 20 age, sex and socioeconomically matched healthy subjects (Mean age 63.7+7.8 yr.). Significantly low level of vitamin C (p <0.001), vitamin E (p <0.001) and TAA (p <0.003) were observed in cancer patients, whereas OS was significantly increased in patients as compared to control (p <0.003). Smokers had significantly lowered TAA and significantly raised OS than non-smokers, in both case and control groups. Tobacco chewer patients had raised OS as compared to control. This study supports the thesis that OS is a risk factor in carcinogenesis and that smoking, an established risk factor in cancer, at least partly appears through it.

Topics: Aged; Ascorbic Acid; Case-Control Studies; Female; Humans; Male; Middle Aged; Neoplasms; Oxidative Stress; Risk Assessment; Risk Factors; Thiobarbiturates; Vitamin E

Assay of free and total malondialdehyde (MDA) in human serum and plasma from healthy subjects and from patients with high risk of lipoperoxidation was performed as follows: (a) acidic (HClO4, pH 1, at 20 degrees C) or basic (NaOH, pH 13, at 60 degrees C) treatments for 30 min; (b) reaction of the protein-free extract (obtained by acid precipitation) with thiobarbituric acid (TBA); (c) HPLC separation on C18 columns with an eluting solution of methanol/phosphate buffer, 10 mmol/L, pH 5.8 (40/60, by vol), at a flow rate of 1.5 mL/min. Free MDA averaged 0.042 (SEM 0.008) and 0.043 (SEM 0.007) mumol/L, respectively, in serum and plasma from healthy subjects. Free (+/- SEM) MDA increased significantly in the plasma from cancer patients (0.270 +/- 0.047 mumol/L) and from hemodialyzed patients (0.214 +/- 0.035 mumol/L). In serum of hemodialyzed patients, analyses for total MDA were unsuitable because of interfering peaks. MDA bound to NH2 groups constituted 83.2% and 83.5% of total MDA in serum and plasma of healthy subjects, respectively, and only 58% in plasma of hemodialyzed patients.

Topics: Adolescent; Adult; Aged; Aged, 80 and over; Chromatography, High Pressure Liquid; Chromatography, Thin Layer; Female; Humans; Lipid Peroxidation; Male; Malondialdehyde; Middle Aged; Neoplasms; Renal Dialysis; Thiobarbiturates

Topics: Administration, Oral; Administration, Topical; Animal Feed; Beverages; Blood Platelets; Carcinogens; Chemical Phenomena; Chemistry; Female; Lethal Dose 50; Lipid Peroxides; Male; Malonates; Malondialdehyde; Mutagenicity Tests; Neoplasms; Plants; Thiobarbiturates

Topics: Animals; Carbohydrates; Cyclohexanes; Cyclohexanones; Deoxyribose; Drug Contamination; Humans; Hydrogen-Ion Concentration; Mice; Neoplasms; Pentanols; Sialic Acids; Thiobarbiturates