Sürdürülebilir Kalkınma Amaçları
Yayınlar
- ArticleYalnız künye2019Preliminary phytochemical analysis and evaluation of in vitro antioxidant, antiproliferative, antidiabetic, and anticholinergics effects of endemic Gypsophila taxa from Turkey
Altay, Ahmet; Tohma, Hatice; Durmaz, Lokman; Taslimi, Parham; Korkmaz, Mustafa; Gulcin, Ilhami; Koksal, Ekrem
The phenolic contents and antioxidant, anticancer, antidiabetic, and anticholinergic potentials of four endemic Gysophila taxa (G. pallida, G. arrosti, G. tuberculosa, and G. eriocalyx) were investigated. The HPLC analysis showed that methanol extracts of all the tested species were richer in phenolics than water extracts. 3,4-dihydroxybenzoic acid, p-hydroxybenzoic acid, vanillin, syringic acid, and p-coumaric acid were detected in all extracts. In parallel to the phenolic contents, methanol extracts displayed comparatively higher antioxidant activity than water extracts. Additionally, all extracts exhibited dose-dependent antiproliferative activity on the cancer cell lines with lower IC50 values changing from 0.170 to 1.805 mg/ml. Moreover, the extracts impressively inhibited the acetylcholinesterase (0.63–26.04), butyrylcholinesterase (3.66–10.73), and α-glycosidase (98.52–235.55) enzymes with very low IC50 (mg/ml) values. Together, the present results indicate that Gysophila taxa have various biological activities together with higher phenolic contents. Hence, these species hold good potential for use in the pharmaceutical industry. Practical applications: Gypsophila taxa having numerous biological activities have been used for different purpose in folk medicine as well as their use in the food industry. The obtained results of the current study indicated that the extracts of Gypsophila taxa are rich in phenolics and flavonoids with powerful antioxidant and antiproliferative activity against different type of cancer cell lines. In addition, the extracts obtained from these taxa showed notable antidiabetic and anticholinergics effects. Gypsophila taxa could be used as a natural material to develop anticancer, antidiabetic, and anticholinergic drugs.
RDL Kalıcı Kaydıİncele - ArticleAçık Erişim2019Novel silver(I) complexes bearing mefenamic acid and pyridine derivatives: Synthesis, chemical characterization and in vitro anticancer evaluation
Altay, Ahmet; Caglar, Sema; Caglar, Bulent; Sahin, Zarife Sibel
Two Ag(I) complexes [Ag2(μ-mef)2(2-pymet)2] 1, [Ag2(μ-mef)2(2-pyet)2] 2 containing mefenamic acid, 2-pyridinemethanol and 2-pyridineethanol were synthesized and characterized by using SCXRD, FT-IR, elemental and thermal analysis techniques. The complex 1 was synthesized as a single crystal whereas the complex 2 was obtained as a microcrystalline powder. The complex 1 consists of binuclear structure. The argentophilic interaction occurs among silver(I) ions due to the short Ag⋯Ag distance (2.8710(10) Å). Two Ag(I) centers are connected by carboxylato oxygen-bridge to form the binuclear metal core. The FT-IR spectra and thermal analysis studies confirmed that both complexes exhibited similar structures. In vitro antiproliferative activity of both complexes were evaluated against MCF-7, HT-29 and HepG2 cancer cell lines. The apoptotic effects and intracellular ROS generation from both complexes were investigated in MCF-7 cell line by flow cytometry analysis. The XTT and LDH assays revealed that both complexes showed strong antiproliferative activity with higher selectivity towards cancer cells compared to the normal cells. In addition, Annexin V/propidium iodide assay exhibited that apoptotic cell number was increased in MCF-7 cells with increasing concentrations of Ag(I) complexes. Furthermore, both complexes induced the ROS generation considerably in MCF-7 cells suggesting the possible pro-oxidant activity of the novel synthesized Ag(I) complexes. Taken together, these findings provide a notable support for potential utility of Ag(I) complexes as novel anticancer agents against numerous kind of carcinogenesis.
RDL Kalıcı Kaydıİncele - ArticleYalnız künye2019Measurement of anticancer, antidiabetic and anticholinergic properties of sumac (Rhus coriaria): analysis of its phenolic compounds by LC–MS/MS
Tohma, Hatice; Altay, Ahmet; Köksal, Ekrem; Gören, Ahmet Ceyhan; Gülçin, İlhami
The present study aimed to investigate Sumac (Rhus coriaria) for anticancer, antidiabetic, anticholinergic activities and total phenolic and flavonoid contents. Two solvents, water and ethanol, were used for extraction. For anticancer activity, the extracts were tested against human cancer cell lines including HT-29 and MCF-7. The cell growth inhibition rate was measured via XTT assay. The antidiabetic activity of the sumac extracts was measured by the inhibition of α-glycosidase and α-amylase enzymes, whereas the anticholinergic activity was measured via the inhibition of acetylcholinesterase and butyrylcholinesterase enzymes. The total phenolic and flavonoid contents were determined using the Folin–Ciocalteau and the aluminum chloride colorimetric methods, respectively. Liquid chromatography–mass spectrometry/mass spectrometry (LC–MS/MS) method was used for the separation, identification and quantification of phenolic compounds in the samples. The ethanolic extract had higher phenolic and phenolic contents than aqueous extract. It exhibited substantial antiproliferative, antidiabetic and anticholinergic activities. The aqueous extract of sumac showed moderate therapeutic efficiency in all the preformed assays. LC–MS/MS study revealed fumaric acid as a main compound in both the ethanolic (452.78 mg/kg) and aqueous (180.72 mg/kg) extracts. These results suggest that sumac may have health-enhancing effects and act as inhibitors of certain enzymes or interfering with some cellular pathways.
RDL Kalıcı Kaydıİncele - ArticleAçık Erişim2018HPLC Analysis of Phenolic Compounds from Gypsophila aucheri Boiss. and Investigation of Antioxidant and Cytotoxic Activity of Gypsophila aucheri Boiss. exracts
Altay, Ahmet
This study was designed to investigate the antioxidant and antiproliferative activities of Gypsophila aucheriBoiss. extracts as well as phenolic content by RP-HPLC technique. Antioxidant activity potentials of theextracts were evaluated by four different methods namely, 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging capacity tests, cupric ionreducing antioxidant capacity (CUPRAC) method, and metal chelating assay. Antiproliferative activities of theextracts were tested against breast carcinoma (MCF-7), colorectal carcinoma (HT-29), and hepatocellularcarcinoma (HepG2) cells. RP-HPLC analysis revealed the presence of eight phenolic compounds in eighteenphenolics scanned. Antioxidant activity results showed that methanol extract of Gypsophila aucheri displayedmore pronounced antioxidant activity than water extract according to DPPH and ABTS tests, whereas waterextract was superior than methanol extract for CUPRAC and metal chelating activity tests. Cytotoxicity testsdemostrated the promising antiproliferative activity of methanol extract against all the tested cancer cell lineswith its lower IC50 values. However, both extracts were observed to display moderate biological activitycompared to positive controls. The obtained data suggest that Gypsophila aucheri could be evaluated as apromising source for food and nutraceutical industries due to its striking antioxidant and moderateantiproliferative potentials together with high phytochemical profile.
RDL Kalıcı Kaydıİncele - ArticleYalnız künye2018IN VITRO ASSESSMENT OF ANTIOXIDANT AND ANTIPROLIFERATIVE ACTIVITY, AND IDENTIFICATION OF PHENOLIC PROFILE OF GYPSOPHILA LEPIDIOIDES BOISS. EXTRACTS FROM TURKEY
Altay, Ahmet
The aim of this study was to evaluate the antioxidant and anti-proliferative activities of Gypsophila lepidiodies Boiss. together with investigation of phenolic content. Antioxidant activity of water and methanol extracts were evaluated by four different methods namely, DPPH and ABTS radical scavenging activity, cupric ion reducing antioxidant capacity (CUPRAC), and Fe2+ chelating assay. Antiproliferative activities of the extracts were assessed against various human cancer cell lines namely, breast adenocarcinoma (MCF-7), colorectal adenocarcinoma (HT-29) and hepatocellular carcinoma (HepG2) cells. HPLC analysis indicated the presence of eight phenolic compounds in eighteen phenolic standards scanned. Antioxidant activity results showed the superiority of methanol extract to water extract according to DPPH, CUPRAC and Fe2+ chelating tests, while the water extract displayed more antioxidant activity by ABTS assay. Antiproliferative activity results demostrated that methanol extract displayed about 2.5-fold, 3.3-fold and 6-fold more activity against MCF-7 cells, HepG2 cells and HT-29 cells, respectively. However, both water and methanol extracts were observed to display moderate biological activity compared to positive controls. The obtained data suggest that Gypsophila lepidioides may be evaluated as a promising source for food and nutraceutical industries due to its good antioxidant and moderate antiproliferative potentials together with its rich phytochemical profile.
RDL Kalıcı Kaydıİncele - ArticleYalnız künye2018In vitro evaluation of antioxidant and anti-proliferative activities of Gypsophila sphaerocephala (Caryophyllaceae) extracts together with their phenolic profiles
Altay, Ahmet; Degirmenci, Sebnem; Korkmaz, Mustafa; Cankaya, Murat; Koksal, Ekrem
This study was designed to investigate the antioxidant and antiproliferative activities of water and methanol extracts of endemic plant Gypsophila sphaerocephala subsp cappadocica in conjuction with phenolic profiles. Individual phenolics of the extracts were identified and quantified by RP-HPLC analysis. Antioxidant potentials of the extracts were evaluated by DPPH (1,1-diphenyl-2-picrylhydrazyl) and ABTS [2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid)] radical scavenging capacity tests, cupric ion reducing antioxidant capacity (CUPRAC) method and Fe2+ chelating assay. Antiproliferative activities of the extracts were tested against MCF-7 (breast adenocarcinoma), HT-29 (colorectal adenocarcinoma) and HepG2 (hepatocellular carcinoma) cell lines. RP-HPLC analysis showed that methanol extract was richer than water extract in terms of phenolic content. In parallel to the phenolic contents, methanol extract showed higher antioxidant activity than water extract by DPPH, CUPRAC and Fe2+ chelating tests while water extract exhibited higher activity by ABTS method. Moreover, methanol extract displayed 1.8-fold, 4.3-fold and 2.6-fold more antiproliferative activity than water extract against MCF-7 cells, HepG2 cells and HT-29 cells, respectively. However, both extracts were found to show moderate antioxidant and antiproliferative activity compared to positive controls. These results suggest that Gypsophila sphaerocephala may be used as a promising source for food and nutraceutical industries due to its considerable antioxidant and antiproliferative potentials together with its rich phenolic content.
RDL Kalıcı Kaydıİncele - ArticleAçık Erişim2018Purification and selected biochemical properties of peroxidase from cress (Lepidium sativum sub sp. sativum)
Altay, Ahmet; Koktepe, Tubanur; Durmaz, Lokman; Topal, Fevzi; Gülçin, İlhami; Köksal, Ekrem
Cress (Lepidium sativum) is an annual herb from Brassicaceae family, and in some regions. It is known as peppergrass, garden cress, garden pepper-cress, pepperwort, or poor man’s pepper. Cress is an important medicinal plant in some countries including Turkey. This plant has major scientific and therapeutic significance. Peroxidase (POD, E.C.1.11.1.7) is an oxidor-eductase enzyme produced by a number of organisms. In this study, POD enzyme was purified from cress by ammonium sulphate precipitation, gel filtration, and CM-Sephadex ion-exchange chromatographies. K m and V max values were calculated from the Lineweaver-Burk graph for H 2 O 2 and guaiacol substrates and the substrate specificity of POD was investigated. The results showed that substrate specificity of H 2 O 2 is better than substrate specificity of guaiacol for this enzyme. The inhibition effects of three cations (Al 3+ , Cu 2+ , and Cr 3+ ) and one organic compound of cetyl trimethylammonium bromide were performed and their inhibition types were determined. Finally, optimum pH, optimum temperature, optimum ionic strength, and stable pH were determined.
RDL Kalıcı Kaydıİncele - ArticleAçık Erişim2018Synthesis, structural, thermal elucidation and in vitro anticancer activity of novel silver(I) complexes with non-steroidal anti-inflammatory drugs diclofenac and mefenamic acid including picoline derivatives
Altay, Ahmet; Caglar, Sema; Caglar, Bulent; Sahin, Onur
Six new Ag(I) coordination complexes, namely [Ag4(μ-dicl)4(2-pic)3] 1, [Ag2(μ-mef)2(2-pic)2] 2, [Ag2(μ-dicl)2(3-pic)2] 3, [Ag2(μ-mef)2(3-pic)2] 4, [Ag2(μ-dicl)2(4-pic)2] 5 and [Ag2(μ-mef)2(4-pic)2] 6, were synthesized and characterized by elemental analysis, FT-IR and thermal analysis techniques. The crystal structures of 1, 3, 4 and 5 were determined by X-ray diffraction analysis, whereas 2 and 6 were obtained as microcrystalline powders. X-ray diffraction analysis demonstrated that 1 occurs as a tetranuclear complex, while 3, 4 and 5 have binuclear structures. A short Ag⋯Ag distances of 2.8446 and 2.8823 Å for 1, 2.8409 Å for 3, 2.8942 Å for 4 and 2.8423 Å for 5 were found in the complexes, indicating that argentophilic interactions exist between the silver ions. In 1, the dicl ligands act as μ3-O,O′,O′ bridging ligands between three Ag(I) ions. In 3, 4 and 5, the dicl and mef ligands behave as bridging ligands and bind two Ag(I) ions together with the carboxylato oxygen atoms. The simultaneous TG/DTG and DTA techniques were applied to interpret the mass losses, decomposition temperatures and corresponding processes of the thermal behaviours of the complexes. The experimental and calculated mass losses of the proposed structures for complexes 2 and 6 are quite compatible with each other and these complexes have very similar FT-IR spectra to the other complexes, which reflect their same structural geometries and characteristics. The cytotoxic activities of the complexes (1–6) were tested against three different cancer cell lines, MCF-7, HT-29 and HepG2, and one normal cell line, 3 T3-L1. XTT assay results demonstrated that although all the silver(I) complexes showed good cytotoxic activity, depending on the cell types tested, the complexes with mefanamic acid (2, 4 and 6) were found to predominate over those with diclofenac (1, 3 and 5), as well as the superiority of 3-picoline to 4-picoline and 2-picoline. Moreover, compared with the cytotoxic potential of carboplatin, 4 especially exhibited a significant cancer cell inhibitory rate and lower cytotoxicity toward the normal cell line, with much higher selectivity indexes.
RDL Kalıcı Kaydıİncele - ArticleYalnız künye2018Modulation of cytochrome P450s and antioxidant enzymes by caffeic acid, p-coumaric acid and quercetin-rich Anatolian propolis in human adenocarcinoma HT-29 cells
Altay, Ahmet; Irtem-Kartal, Deniz; Sagdicoglu-Celep, Gulcin; Guray, Tulin; Bozoglu, Faruk
Propolis, which is a complex resinous material has diverse pharmacological and biological properties. Phase I and II enzymes are responsible for detoxication and elimination of activated carcinogens, acting as important biomarkers for chemoprevention. Among them, cytochrome P450s plays a prominent role in metabolic activation of xenobiotics. This study was designed to investigate the in vitro modulatory effects of Anatolian propolis and its phenolic contents; caffeic acid, quercetin and p-coumaric acid on the mRNA expression levels of CYP1A1, CYP1A2, CYP2E1, NQO1, GSTP1 and GPx in human colorectal adenocarcinoma HT-29 cells. Analysis results revealed that the propolis extract and its major phenolic contents; caffeic acid and quercetin suppressed the mRNA expression levels of CYP1A1, CYP1A2 and CYP2E1 between the range of 1,66 and 4,55 fold, while p-coumaric acid did not show remarkable effects on the enzymes aforementioned. On the other hand, the extract and all phenolics increased the mRNA expression levels of antioxidant enzymes; NQO1, GSTP1 and GPx between the range of 1,51 and 9,85 fold. This preliminary study demonstrates that phenolic content rich-Anatolian propolis modulates the gene expression of the enzymes involved in xenobiotics activation and detoxication pathways.
RDL Kalıcı Kaydıİncele - ArticleAçık Erişim2017Glassworts as Possible Anticancer Agents Against Human Colorectal Adenocarcinoma Cells with Their Nutritive, Antioxidant and Phytochemical Profiles
Altay, Ahmet; Celep, Gulcin Sagdicoglu; Yaprak, Ahmet E.; Baskose, Isa; Bozoglu, Faruk
In this study, the possible uses of glassworts as potential food ingredients and their antiproliferative activity against colorectal adenocarcinoma cells together with their antioxidant and phytochemical profiles were investigated for the first time. MeOH extracts of five different taxa collected from different localities were screened for their antioxidant capacities by DPPH (IC50 2.91-5.49mg/ml) and ABTS (24.4-38.5molTE/gextract) assays. Salicornia freitagii exhibited the highest DPPH radical scavenging activity. LC/MS/MS analysis displayed that vanillic acid and p-coumaric acid were two main phenolic compounds in the extract. Salicorniafreitagii extracts also exhibited high antiproliferative activity against HT-29 (IC50 1.67mg/ml) and Caco-2 (IC50 3.03mg/ml) cells for 72h. Mineral analysis indicated that all the species with different proportions of elemental components contained high amount of cations. These results indicate that investigated glassworts, with their high phenolic and mineral contents and also notable antioxidant and cytotoxic properties, may be utilized as a promising source of therapeutics.
RDL Kalıcı Kaydıİncele - ArticleAçık Erişim2017Modulation of mRNA expression and activities of xenobiotic metabolizing enzymes, CYP1A1, CYP1A2, CYP2E1, GPx and GSTP1 by the Salicornia freitagii extract in HT-29 human colon cancer cells
Altay, Ahmet; Kartal, Deniz Irtem; Sadi, Gokhan; Güray, Tulin; Yaprak, Ahmet Emre
Phase I-II detoxification and antioxidant enzymes are responsible for the detoxification and elimination of activated carcinogens, acting as important biomarkers for chemoprevention. Among them, cytochrome P450s plays a prominent role in the metabolic activation of xenobiotics. The herb Salicornia freitagii (SF) (Amaranthaceae) is known for its anticancer, antioxidant, antidiabetic and antiinflammatory activities. In this study, we determined the bioactive phenolics in the SF methanol extract and investigated its antiproliferative potential in HT-29 human colon cancer cells. We also investigated the modulation of some phase I and II enzyme (CYP 1A1, 1A2, 2E1, GSTP1 and GPx) mRNA expression and enzymatic activities by the SF extract and its major bioactive phenolic compounds. LC/MS-MS analysis showed that the main phenolic compounds of the methanolic SF extract are vanillic acid (48 mu g/100g) and p-coumaric acid (10.8 mu g/100g). SF extract, vanillic acid and p-coumaric acid exhibited high antiproliferative activities in HT-29 cells, with IC50 values of 81.79 mu g/mL, 98.8 mu M and 221.6 mu M, respectively. The mRNA expression levels of CYP1A2 and CYP2E1 were decreased, while those of GSTP1 and GPx in HT-29 cells were increased after application of either the SF extract or vanillic acid. The SF extract by itself also increased the activities of GPx and GSTP1 enzymes 1.68- and 1.49-fold, respectively. Our data indicate that the SF extract and its major bioactive compound, vanillic acid, could exert a modulatory effect on the expression of enzymes that are involved in xenobiotic activation and detoxification pathways in the gastrointestinal tract. For this reason, SF can be considered as a natural source of chemopreventive agents.
RDL Kalıcı Kaydıİncele - ArticleAçık Erişim2017Salvia fruticosa Modulates mRNA Expressions and Activity Levels of Xenobiotic Metabolizing CYP1A2, CYP2E1, NQO1, GPx, and GST Enzymes in Human Colorectal Adenocarcinoma HT-29 Cells
Altay, Ahmet; Bozoğlu, Faruk
Natural products have gained considerable interests because of their use in some industrial areas including nutrition, cosmetic, pharmacy, and medicine. Salvia fruticosa M. (Lamiaceae) is known for its antioxidant, antimicrobial, and antiproliferative activities. Phase I xenobiotic metabolizing enzymes, CYP1A2 and CYP2E1, produce reactive metabolites which are eliminated by the action of phase II enzymes, NQO1, GPx, and glutathione S-transferases (GSTs). In this study, in vitro modulatory effects of S. fruticosa and its major phenolic compound rosmarinic acid (RA) on CYP1A2, CYP2E1, NQO1, GPx, and GSTm1 mRNA expressions and enzyme activities of GPx and GSTs were investigated in HT-29 cells. An mRNA expression analysis revealed that CYP1A2 and CYP2E1 levels were decreased while those of NQO1, GPx, and GSTm1 increased after S. fruticosa and RA treatments. In parallel to gene expressions, enzyme activities of GPx and GSTs by S. fruticosa increased 1.68- and 1.48-fold, respectively. Moreover, RA increased GPx and GSTs activities 1.67- and 1.94-fold, respectively. The results of this preliminary study show that metabolism of xenobiotics may be altered due to changes in the expression and activity of the investigated enzymes by S. fruticosa.
RDL Kalıcı Kaydıİncele