Mustafa Karatepe

6-Phenyl-3-(4-pyridyl)-1,2,4-triazolo-[3,4-b][1,3,4]thiadiazole: synthesis, experimental, theoretical characterization and biological activities.

The molecular geometry, vibrational frequencies, and gauge including atomic orbital (GIAO) (1)H and (13)C NMR chemical shift values of the title compound in the ground state have been calculated using the Hartree-Fock (HF) and density functional theory (DFT) methods with 6-31G(d) basis sets, and compared with the experimental data. The calculated results show that the optimized geometries can well reproduce the crystal structural parameters and the theoretical vibrational frequencies, and (1)H and (13)C NMR chemical shift values show good agreement with experimental data. To determine conformational flexibility, molecular energy profile of the title compound was obtained by HF/6-31G(d) and (DFT/B3LYP) calculations with respect to selected degree of torsional freedom, which was varied from -180° to +180° in steps of 10°. The energetic behavior of the title compound in solvent media was examined using the B3LYP method with the 6-31G(d) basis set by applying the Onsager and the polarizable continuum model (PCM). The results obtained with these methods reveal that the PCM method provided more stable structure than Onsagers method. The title compound has been tested in vitro for biological effects.

Pro-oxidant and antiproliferative effects of the 1,3,4-thiadiazole–based Schiff base and its metal complexes

Adverse biological activities of Schiff base (SB) derivatives are well known. In this study, the ligand and its metal complexes have been synthesized and characterized by IR, 1H-NMR spectra, elemental analyses, magnetic susceptibility, UV-Vis spectra, and thermogravimetry/differential thermal analysis. From the elemental analyses data, the complexes were proposed to have the general formula [Mn(L)2(H2O)2], [Co(L)2(H2O)2], and [Ni2(L)(H2O)4(Cl)3]. From the magnetic moment and UV-Vis spectra data, it was found that the geometrical structures of these complexes are octahedral. In the in vivo experiment, adult male rats were injected subcutaneously with a new SB (L) and its [Mn(L)2(H2O)2], [Co(L)2(H2O)2], and [Ni2(L)(H2O)4(Cl)3] complexes (25 mg/kg body weight) and were then sacrificed 16 days later. Effects of these compounds on serum antioxidant vitamins (i.e., vitamins A, E, and C) and malondialdehyde (MDA) levels were measured in blood serum, liver, and kidney tissues. In an in vitro experiment, antiproliferative effects of these compounds were assessed on the human breast carcinoma MCF-7 and murine leukemia L1210 cell lines. Serum MDA and vitamins A, E, and C levels did not change by the treatments. However, in the kidney and liver tissues, MDA levels were higher, whereas vitamin levels were lower in treatment groups, compared to the control group. All compounds inhibited cell proliferation of MCF-7 and L1210 cancer cell lines in a dose- and time-dependent manner. In conclusion, SB derivatives tested in the current study induced oxidative stress in vivo and exhibited anti-proliferative effects in an in vitro culture system.

[Synthesis of two new acetanilide derivatives and their effect on the serum antioxidant vitamins (A, E, and C) and the MDA level in rats].

Acetanilide derivatives, 2,2′-thiobis[N-(4-nitrophenyl)acetamide] and 2,2′-thiobis[N-(4-chlorophenyl)acetamide], were synthesized and characterized. They were shown to cause a considerable oxidative stress in rats.

Vitamin and fatty acid composition of P. eryngii var. eryngii

In this study, fatty acid and vitamin contents of P. eryngii var. eryngii grown on various agro-residue were determined. The distribution of oil acid in 100 g lipid extracted from samples were found to be 0.00-0.59 g C14:0, 0.00-1.68 g C15:0, 13.56-20.09 g C16:0, 0.00-4.98 g C16:1, 0.00-0.22 g C17:1, 1.35-5.41 g C18:0, 10.77-34.80 g C18:1, 33.06-70.39 g C18:2, 0.00-1.17 g C18:3, 0.00-0.53 g C20:0, 0.00-0.59 g C20:2, 0.00-0.25 g C20:1, 0.00-4.14 g C20:3, 0.00-0.51 g C20:5, 0.00-1.15 g C22:0, 0.00-0.30 g C22:1, 0.00-3.54 g C22:2, 0.00-0.33 g C22:4, 0.00-1.15 g C22:5, 0.00-3.93 g C22:6 and 0.00-2.07 g C24:0, of wet weight. The contents of vitamin were 0.014-0.064 A, 0.869-3.565 E, 55.980-473.405 C and 0.087-5.619 MDA mg/kg of wet weight. It has been determined that P. eryngii var. eryngii is rich from the point of view of unsaturated fatty acids such as linoleic acid, oleic acid and palmitic acid, and especially vitamins C, also antioxidants vitamins such as vitamin A, E and MDA.

In vitro cytotoxic and in vivo antitumoral activities of some aminomethyl derivatives of 2,4-dihydro-3H-1,2,4-triazole-3-thiones-Evaluation of their acetylcholinesterase and carbonic anhydrase enzymes inhibition profiles: TİMUR et al.

The 1,2,4‐triazole and its derivatives were reported to exhibit various pharmacological activities such as antimicrobial, analgesic, anti‐inflammatory, antitumoural, cytotoxic, and antioxidant properties. In this study, a series of triazole compounds (M1‐M10) were evaluated for some biological activities. In vitro qualifications of these compounds on acetylcholinesterase (AChE) and human carbonic anhydrase enzyme activities were performed. Also, their antitumoral activities in human colon cancer (HT29) cell line cultures were examined. In addition, colon cancer experimentation was induced in rats by an in vivo method, and the in vivo anticancer effects of triazole derivatives were investigated. Also, the effects of these derivatives in levels of antioxidant vitamin A, vitamin E, and MDA were studied in rat liver and blood samples. Most of the compounds were found to exhibit significant antioxidant and antitumoral activities. All the compounds had cytotoxic activities on HT29 cell lines with their IC50 values lower than 10 µM concentrations. The low IC 50 values of the compounds are M1 (3.88 µM), M2 (2.18 µM), M3 (4.2 µM), M4 (2.58 µM), M5 (2.88 µM), M6 (2.37 µM), M7 (3.49 µM), M8 (4.01 µM), M9 (8.90 µM), and M10 (3.12 µM).

The determination of the effect of some 1,3,4 thiadiazole derivatives on biochemical content (Fatty Acids, Sterols, Lipophilic Vitamins) in rat liver

Thiadiazole derivatives and its metal compounds have antibacterial, antifungal, antitumoral, antiproliferative and antioxidant properties. In the study, the effects caused by thiadiazole ligand and its metal complexes upon the fatty acids and lipophilic vitamins in livers of rats were examined. The fatty acids in liver were specified by GC while the lipophilic vitamins were specified by HPLC. It was observed that the amounts of oleic acids (18:1, n-9) and monounsaturated fatty acids (MUFA) notably increased in the Mn complex group while the amounts of arachidonic acid (20:4, n-6) notably increased in the ligand group, compared to control group. The amounts of vitamin K2, vitamin D3 and α-tocopherol considerably increased in all groups compared to control group. It was noted that the amounts of α-tocopherol were elevated in both the Mn and Cr complex groups compared to control group. However, this elevation was matching with the amount in the same groups. Nevertheless, the amount of retinol was determined to be lower in the Mn complex group compared to other groups. Accordingly, it can be considered that thanks to the utilization of toxic metals such as manganese, cadmium and chrome, unsaturated fatty acids influenced the activities of the enzymes in liver tissue, which are in charge of fatty acid chain elongation.

Biochemical evaluation of hydroxyurea derivative schiff bases in liver of rats

In this study, it was aimed to examine the antioxidant and antihepatotoxic effects of hydroxyurea derivative Schiff bases on serum biochemical parameters (AST, ALT, LDH, urea, creatinine and total bilirubin) and antioxidant parameters (SOD, CAT, GPx, MDA). In this study, a total of 49 adult male Wistar rats was examined and they were divided into 7 equal groups. DMSO, which is diluted only with corn oil, was administered to control group. 25 mg / kg ligand, 25 mg / kg Schiff base - manganese, 25 mg / kg Schiff base-copper, 25 mg / kg Schiff base - zinc, 25 mg / kg Schiff base - nickel, 25 mg / kg Schiff base - cobalt complexes were administered to rats of experimental group subcutaneously for 15 days with three-day intervals throughout the test process. All specimens were killed by decapitation and their livers were extracted. According to the results obtained, ALT level was observed to be higher (P<0.05) in the Cu-L group compared to other groups. LDH level was observed to be higher (P<0.05) in the Cu-L and Co-L groups compared to other groups. SOD level was observed to be higher (P<0.05) in the Cu-L, Mn-L and Zn-L groups compared to other groups. MDA level was observed to be higher (P<0.05) in the Ni-L, Cu-L, Zn-L groups compared to other groups. In conclusion, it can be suggested that the determination of the pharmacological characteristics of them can be beneficial in numerous fields of application thanks to the antioxidant and hepatotoxic activities demonstrated by hydroxyurea derivative Schiff bases.

Phytochemical Compounds and Biological Activities of Celtis tournefortii Fruits

Abstract It is known that Celtis species have been used in healing wound, epilepsy crisis, and stomach pain among the people. The antiradical (DPPH, OH, ABTS) activities, phytochemical compounds (total proanthocyanidin, total flavonoid, total phenolic, flavonoids, phenolic acids, sterols, lipid soluble vitamins, fatty acids), antimicrobial, antiproliferative (MCF-7, HCT-116, A2780, PC-3) activities of water, ethanol, methanol extracts of C. tournefortii fruits were evaluated in this study. All the C. tournefortii fruit water extracts were higher scavenged OH radical than standard antioxidant BHT. It was detected that C. tournefortii includes high amount of α-tocopherol (2.65 mg/kg), vitamin D (10.05 mg/kg), ergosterol (78.70 mg/kg), stigmasterol (185.90 mg/kg), unsaturated fatty acids (74.47%). C. tournefortii extracts showed antiproliferative activity on MCF-7, HCT-116, A2780, PC-3 cancer cell lines and antimicrobial activity on some microorganisms when compared to standard antibiotics. Also, this study is the first report about phytochemical contents, antiproliferative, antimicrobial, antiradical properties of C. tournefortii fruits.

THE EFFECTS OF 5,5'-BUTANE-1,4-DIYLBIS[4-ALLYL-2-({4-[3-(TRIFLUOROMETHYL)PHENYL]PIPERAZIN-1-YL}METHYL)- 2,4-DIHYDRO-3H-1,2,4-TRIAZOLE-3-THIONE] COMPOUND ON MDA LEVEL AND VITAMINS IN SERUM, LIVER AND KIDNEY OF RATS

The 1,2,4-triazole along with its derivatives were reported to exhibit various pharmacological activities [1]. 1,2,4-triazole moieties have been incorporated into a wide variety of therapeutically interesting drug candidates, including anti-inflammatories, CNS stimulants, sedatives, anti-anxiety compounds, antimicrobial agents, as well as anti-mycotic ones such as fluconazole, intraconazole andvoriconazole [2]. As previously reported, Aminomethyl derivatives were synthesized. In this study, the effects of newly synthesized bis1,2,4-triazole containing aminomethyl derivatives on the level of malondialdehyde(MDA)and antioxidant vitamins (A,E,C) of the serum, liver and kidney of rats have been investigated. In addition, level of malondialdehyde (MDA) and vitamins (A,E,C) has been determined by HPLC [3]. Most of the compounds showed satisfactory performance when compared to the control group [4]