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Öğe ACA, an inhibitor phospholipases A2 and transient receptor potential melastatin-2 channels, attenuates okadaic acid induced neurodegeneration in rats(Pergamon-Elsevier Science Ltd, 2017) Cakir, Murat; Duzova, Halil; Tekin, Suat; Taslidere, Elif; Kaya, Gul Busra; Cigremis, Yilmaz; Ozgocer, TubaAim: In recent studies, it has been shown that the Transient Receptor Potential Melastatin-2 Channels (TRPM2) and Phospholipases A2 (PLA(2)) inhibitors may have a protective effect on neurons. This study was aimed to investigate the protective effect of TRPM2 and PLA(2) inhibitor N-(p-amylcinnamoyl) Anthranilic Acid (ACA) in a neurodegenerative model induced by Okadaic Acid (OKA). Main methods: OKA (200 ng/10 mu l) was administered bilateral intracerebroventricularly as a single injection. Key findings: OKA-treated rats showed significant impairments of spatial memory in Morris Water Maze Test. OKA-induced memory-impaired rats showed increased numbers of degenerated neurons and Caspase-3, tau phosphorylated ser396, beta-amyloid positive cells in the hippocampus and cerebral cortex. Furthermore, OKA-treated rats exhibited significantly increased MDA, TNF-alpha levels, and decreased SOD, GSH-PX enzyme activates and GSH levels of the tissues. ACA administration ameliorated OKA-induced memory impairment in rats. The ACA treatment also increased SOD and GSH-PX enzyme activation and GSH levels, and conversely decreased the levels of MDA, TNF-alpha. It was found that the numbers of the degenerated neurons and Caspase-3 positive cells of cortex and hippocampus regions were significantly reduced. Significance: ACA administration attenuates the oxidative stress and neuroinflammation of OKA-induced neurodegeneration; and ameliorates the cognitive decline and neurodegeneration. (C) 2017 Elsevier Inc. All rights reserved.Öğe Adipoz dokudan salgılanan bir hormon: apelin(İnönü Üniversitesi Sağlık Bilimleri Dergisi, 2013) Sandal, Süleyman; Tekin, SuatYağ doku pasif enerji deposu ve aktif metabolik bir endokrin organ olarak görev yapar. Özellikle beyaz yağ dokusu büyük ölçüde protein sinyallerini ve adipokin adı verilen faktörleri salgılayan önemli bir endokrin organdır. Apelin adipokin ailesine yeni katılmış peptid yapıda bir hormondur. Birçok fizyolojik rol üstlenen apelin, G protein kenetli orfan apelin reseptörünün (APJ) endojen ligandıdır. Bu derlemenin amacı apelin ve reseptörü olan APJ’nin olası fizyolojik rollerini açıklamaktır.Öğe Administration of Acute Agomelatine Reduces Increased Oxidative Stress Due to Experimental Renal Ischemia / Reperfusion Damage in Rats(Wiley, 2019) Aykora, Damla; Ozturk, Dilara Altay; Tanbek, Keyser; Bahar, Mehmet Refik; Tekin, Suat; Sandal, Suleyman[Abstract Not Available]Öğe Agomelatine alleviates pain-related behaviour in ovariectomized rats(2024) Korkmaz, Engin; Beytur, Asiye; Tekin, SuatAim: Menopause is a physiological process that results in the cessation of ovarian follicle activity. Research suggests that postmenopausal women may experience changes in pain sensitivity. Ovariectomized (Ovx) rats are commonly used to mimic postmenopausal pain symptoms in research. Agomelatine is a unique antidepressant that acts as both a melatonergic receptor agonist and a 5-HT2C receptor antagonist. Preclinical studies have suggested potential analgesic effects associated with agomelatine. This study aims to investigate the influence of agomelatine on pain behavior in Ovx rats. Materials and Methods: Forty female Sprague Dawley rats were divided into four groups: Sham, Ovx, Ago20 and Ago40. The Ovx, Ago20 and Ago40 groups underwent bilateral ovariectomy, while the Sham group underwent all surgical procedures except ovarian ligation. After four months, the Sham and Ovx groups received vehicle, while the Ago20 (20mg/kg) and Ago40 (40mg/kg) groups received agomelatine by oral gavage for two months. Pain sensitivity assessments were conducted using electronic von Frey, hot plate, tail flick, and tail immersion methods after the final drug administration. Results: In the Ovx group, there was an increase in pain sensitivity observed in the hot plate, electronic von Frey, tail flick, and tail immersion tests (p < 0.05). Agomelatine treatment significantly reduced the heightened nociceptive response (p < 0.05). Conclusion: Agomelatine effectively attenuates the increased sensitivity to pain observed in Ovx rats.Öğe Agomelatine pretreatment prevents development of hyperglycemia and hypoinsulinemia in streptozotocin-induced diabetes in mice(Wiley, 2019) Ozcan, Mete; Canpolat, Sinan; Bulmus, Ozgur; Ulker, Nazife; Tektemur, Ahmet; Tekin, Suat; Ozcan, SibelThe main objective of this study was to investigate potential effectiveness of agomelatine pretreatment in the prevention of diabetes itself and encephalopathy, with a focus on brain tissue oxidative stress and inflammatory processes in streptozotocin (STZ)-induced diabetic mice. Interleukine-1 beta (IL-1 beta) and TACR1 (NK1), which is a tachykinine receptor, were used for the investigation of inflammation in the brain regions including raphe nucleus, periaqueductal gyrus (PAG), amygdala, and nucleus accumbens. The effects of agomelatine on total antioxidant capacity were also evaluated. In the in vitro part of the study, the effects of agomelatine on cell viability were investigated in dorsal root ganglion (DRG) neurons. Fasting blood glucose levels were measured 72 h after STZ injection to determine the diabetic condition. Agomelatine pretreatment prevented both hyperglycemia and hypoinsulinemia in STZ-treated mice. When STZ was injected to induce diabetes in mice, neither hyperglycemia nor hypoinsulinemia was developed in agomelatine pretreated mice and 6 weeks after development of diabetes, agomelatine treatment significantly decreased levels of IL-1 beta mRNA in raphe nucleus and nucleus accumbens. TACR1 mRNA levels were lower in raphe nucleus, PAG, and amygdala of agomelatine-treated diabetic mice. The increase in total antioxidant capacity after agomelatine administration may responsible for its beneficial effect in the prevention of diabetes. We showed that agomelatine reversed high glucose-induced cell viability decreases in DRG neurons. Both the antihyperglycemic and antioxidant effects of agomelatine might have contributed to the DRG neuron viability improvement. In conclusion, agomelatine seems to both prevent development of diabetes and reverse the encephalopathic changes caused by diabetes.Öğe Alkyl sulfonic acide hydrazides: Synthesis, characterization, computational studies and anticancer, antibacterial, anticarbonic anhydrase II (hCA II) activities(Elsevier, 2015) Ozdemir, Ummuhan O.; Ilbiz, Firdevs; Gunduzalp, Ayla Balaban; Ozbek, Neslihan; Genc, Zuhal Karagoz; Hamurcu, Fatma; Tekin, SuatMethane sulfonic acide hydrazide, CH3SO2NHNH2 (1), ethane sulfonic acide hydrazide, CH3CH2SO2NHNH2 (2), propane sulfonic acide hydrazide, CH3CH2CH2SO2NHNH2 (3) and butane sulfonic acide hydrazide, CH3CH2CH2CH2SO2NHNH2 (4) have been synthesized as homologous series and characterized by using elemental analysis, spectrophotometric methods (H-1-C-13 NMR, FT-IR, LC-MS). In order to gain insight into the structure of the compounds, we have performed computational studies by using 6 311G(d, p) functional in which B3LYP functional were implemented. The geometry of the sulfonic acide hydrazides were optimized at the DFT method with Gaussian 09 program package. A conformational analysis of compounds were performed by using NMR theoretical calculations with DFT/B3LYP/6 311++G(2d, 2p) level of theory by applying the (GIAO) approach. The anticancer activities of these compounds on MCF-7 human breast cancer cell line investigated by comparing IC50 values. The antibacterial activities of synthesized compounds were studied against Gram positive bacteria; Staphylococcus aureus ATCC 6538, Bacillus subtilis ATCC 6633, Bacillus cereus NRRL-B-3711, Enterococcus faecalis ATCC 29212 and Gram negative bacteria; Estherichia coli ATCC 11230, Pseudomonas aeruginosa ATCC 15442, Klebsiella pneumonia ATCC 70063 by using the disc diffusion method. The inhibition activities of these compounds on carbonic anhydrase II enzyme (hCA II) have been investigated by comparing IC50 and Ki values. The biological activity screening shows that butane sulfonic acide hydrazide (4) has more activity than the others against tested breast cancer cell lines MCF-7, Gram negative/Gram positive bacteria and carbonic anhydrase II (hCA II) isoenzyme. (C) 2015 Elsevier B.V. All rights reserved.Öğe The alterations in serum ghrelin and leptin levels after intracerebroventricularly irisin infusion in rats(Wiley-Blackwell, 2015) Tekin, Suat; Erden, Yavuz; Sandal, Suleyman; Ozyalin, Fatma; Colak, Cemil[Abstract Not Available]Öğe The ameliorating effect of cannabinoid type 2 receptor activation on brain, lung, liver and heart damage in cecal ligation and puncture-induced sepsis model in rats(Elsevier, 2020) Cakir, Murat; Tekin, Suat; Okan, Asli; Cakan, Pinar; Doganyigit, ZuleyhaUncontrolled infection and increased inflammatory mediators might cause systemic inflammatory response. It is already known that Cannabinoid Type 2 (CB2) receptors, which are commonly expressed in immune cells and in many other tissues, have an effect on the regulation of immune response. In the present study of ours, the effects of CB2 receptor agonist JWH-133 was investigated on cecal ligation and puncture (CLP)-induced polymicrobial sepsis model in rats. In the present study, Sprague-Dawley rats were divided into 5 groups (i.e. the Sham, CLP, JWH-133 0.2 mg/kg, JWH-133 1 mg/kg, and JWH-133 5 mg/kg Groups). Except for the Sham Group, the CLP-induced sepsis model was applied to all groups. The histopathological damage in brain, lung, liver and, heart was examined and the caspase-3, p-NF-kappa B, TNF-alpha, IL-1 beta and IL-6 levels were determined immunohistochemically. The serum TNF-alpha, IL-1 beta, IL-6, IL-10 levels were examined with the ELISA Method. The JWH-133 treatment decreased the histopathological damage in brain, heart, lung, and liver and reduced the caspase-3, p-NF-kappa B, TNF alpha, IL-1 beta, IL-6 levels in these tissues. In addition to this, JWH-133 treatment also decreased the serum TNF-alpha, IL-1 beta, IL-6 levels, which were increased due to CLP, and increased the anti-inflammatory cytokine IL-10 levels. In the present study, it was determined that the CB2 receptor agonist JWH-133 decreases the CLP-induced inflammation, and reduces the damage in brain, lung, liver and heart. Our findings show the therapeutic potential of the activation of CB2 receptors with JWH-133 in sepsis.Öğe Anti-tumor properties of microwave-assisted synthesized 6,7-dihydroxycoumarins: An in vitro study(Wiley-Blackwell, 2015) Tekin, Suat; Koran, Kenan; Ozen, Furkan; Gorgulu, Ahmet Orhan; Sandal, Suleyman[Abstract Not Available]Öğe Antioxidant and cytotoxic properties of some new dipeptide-indole conjugates(Wiley, 2023) Gonul, Zeynep; Ozturk, Dilara Altay; Kucukbay, Fatumetuzzehra; Tekin, Suat; Tekin, Zehra; Kucukbay, HasanIn this study, 10 new indole-dipeptide conjugates were synthesized, and their anticancer activity was determined against on A2780 (ovarian cancer cell line) and MCF-7 (breast cancer cell line) cells. Among compounds, 5 and 10 showed better activity against A2780 cell lines than the standard drug docatexel at 0.1 and 1 mu M concentrations, while only compound 5 showed better activity than docatexel, the MCF-7 cell line at 0.1 and 1 mu M concentrations. The antioxidant potencies of the compounds were low in both the DPPH and iron reducing power methods tested when compared to standard antioxidants used in this work.Öğe Antioxidant, Antimicrobial and Anticancer Activities of the Aspergillin PZ and Terphenyllin Secondary Metabolites: An in vitro Study(Gazi University Journal of Science, 2019) Erden, Yavuz; Tekin, Suat; Ceylan, Kevser Betül; Tekin, Çiğdem; Kırbağ, SevdaÖz: The importance of secondary metabolites obtained from fungi is increasing day by day in terms of human health. Many physiological and pharmacological effects, mainly antimicrobial, anticancer and antioxidant properties of these compounds have been reported. Aim of this study is to determine the anticancer, antioxidant and antimicrobial effects of aspergillin PZ and terphenyllin compounds, which are isolated from Aspergillus and also subjected to limited number of studies. The antimicrobial activity of aspergillin PZ and terphenyllin compounds was determined by using disc diffusion method using different bacteria. The antioxidant property of the compounds was determined by measuring the level of DPPH free radical scavenging. Cytotoxic activity was determined by experiments on human prostate cancer cell lines (PC3 and LNCaP) and over cancer cell line (A2780). Both compounds showed low antimicrobial activity on test bacteria (approximately 2-3 mm zone). High concentrations of applied compounds showed apparent DPPH free radical scavenging activity, while % scavenging activity was quite low at low concentrations. Both compounds showed significant anticancer activity on cancer cell lines (p <0.05). Our results suggest that these two compounds have important biological properties due to their antioxidant and anticancer activities.Öğe Asprosin Takes a Protective Role in Mice Established Experimental Acute Kidney(Wiley, 2023) Korkmaz, Engin; Keskin, Tuba; Yildiz, Azibe; Tekin, Cigdem; Tekin, Suat; Beytur, Ali[Abstract Not Available]Öğe Bazı önemli tıbbi bitkilerin antioksidan ve antikanser etkilerinin araştırılması(2019) Top, Rabia; Erden, Yavuz; Tekin, Yavuz; Tekin, SuatÖz: Tıbbi açıdan önemli bitkiler binlerce yıldır birçok hastalığın tedavisi amacıyla kullanılmaktadır. Buna ek olarakmodern eczacılıkta birçok bitki bileşiği ilaç ham maddesi veya yeni ilaçların yapımında önemli bir yere sahiptir.Bu çalışmada tıbbi öneme sahip kudret narı (Momordica charantia), pepino (Solanum muricatum) ve altın çilek(Physalis peruviana) bitkilerinin meyvelerinden elde edilen özütlerin biyolojik etkinliklerinin ortaya konulmasıamaçlanmıştır. Bitkilerin meyve özütleri %80’lik etanolde hazırlandıktan sonra toplam polifenol içeriği FolinCiocalteu reaktifi kullanılarak spektrofotometrik olarak ölçüldü. Bitki örneklerinin serbest radikal giderme etkisiDPPH serbest radikali kullanılarak belirlendi. Özütlerin insan over ve meme kanseri hücre hatları (sıyasıyla A2780 ve MCF-7) üzerine sitotoksik etkileri MTT yöntemi kullanılarak belirlendi. Bitki örneklerindeki toplampolifenolik düzeyin en düşük 138,14±12,15 ve en yüksek 415,71±36,89 µg/gr gallik asit düzeyinde olduğubelirlendi. Bütün özütlerin düşük seviyede antioksidan etki sergilediği saptandı. Son olarak over ve meme kanserihücre serilerine uygulanan özütlerin güçlü sitotoksik etki gösterdiği belirlendi (p<0.05). Sonuçta her üç bitkiörneğinin de antioksidan etkilerinden ziyade yüksek antikanser etkiye sahip olduğunu bizlere göstermektedir. Herüç örneğinde söz konusu kanser türleri üzerine etkilerini aydınlatmak için ileriki çalışmalara ihtiyaç vardır.Öğe Benzimidazole based a new therapeutic agent effective on ovarian cancer cells(Wiley-Blackwell, 2015) Tekin, Suat; Mumcu, Akin; Kucukbay, Hasan; Sandal, Suleyman[Abstract Not Available]Öğe Beslenmenin hipotalamik kontrolünde irisin hormonunun etkilerinin araştırılması(2015) Tekedereli, İbrahim; Özyalın, Fatma; Çolak, Cemil; Bozkır, Çiğdem; Tekin, Suat; Çiğremiş, Yılmaz[Abstract Not Available]Öğe Beslenmenin hipotalamik kontrolünde irisin hormonunun etkilerinin araştırılması(İnönü Üniversitesi, 2015) Tekin, SuatHipotalamus, beslenmenin kontrolünde roller üstlenmiş bir merkezdir ve bu merkezde beslenme davranışını kontrol eden leptin, ghrelin, nöropeptid Y (NPY) ve proopiomelanokortin (POMC) başta olmak üzere birçok peptidin aktif rol aldığı bilinmektedir. İrisin 2012 yılında Boström vd., tarafından peptid yapılı bir miyokin olarak tanımlanmıştır. Bu çalışma ile irisinin, beslenme davranışı üzerine etkileri NPY, POMC ve UCP2 mRNA ifadeleri ile bu genlere ait protein düzeyleri ilişkilendirilerek açıklanması amaçlanmıştır. Materyal ve Metot: Çalışmada ağırlıkları 240-325 gr olan 40 adet Wistar-Albino cinsi erkek sıçan kullanıldı. Sıçanlar eşit olarak 4 gruba ayrıldı (n=10): Kontrol grubuna herhangi bir uygulama yapılmadı, sham kontrol grubuna ozmotik mini pompa implante edildi ve 10µl/saat hacminde 7 gün süresince yapay beyin omurilik sıvısının (irisinin çözücüsü) infüzyonu gerçekleştirildi. Uygulama gruplarına ise 7 gün süreyle irisinin, fizyolojik (10 nM) ve farmakolojik (100 nM) dozları 10 µl/saat hacminde infüze edildi. Çalışma süresince hayvanlar kafeslerde bireysel olarak tutuldu, hayvanların günlük yem ve su tüketimleri ile vücut ağırlıkları takip edildi. Yedi günlük infüzyon sonunda hayvanlara ötanazi uygulanarak beyin dokusu ve kan örnekleri toplandı. Toplanan kan örneklerinden ELISA yöntemiyle grupların serum leptin ve ghrelin seviyeleri, fotometrik yöntem ile grupların metabolik parametreleri (glukoz, kolestrol, trigliserit, HDL, LDL) ölçüldü. Alınan beyin dokularından (hipotalamus) RT-PCR yöntemiyle grupların UCP2, POMC ve NPY mRNA düzeyleri, Western blot yöntemiyle de bu genlere ait protein miktarları belirlendi. Bulgular: Uygulanan irisinin her iki konsantrasyonu (10 ve 100 nM) sıçanların günlük yem tüketimini arttırdı (p<0.05) ancak vücut ağırlığında ve su tüketiminde anlamlı bir değişime neden olmadı. İrisinin serum leptin seviyesini azalttığı (p<0.05), ghrelin seviyesini ise arttırdığı gözlendi (p<0.05). Uygulanan irisin NPY ve UCP2 seviyelerini arttırırken, POMC seviyesinde azalmaya neden oldu (p<0.05). Ayrıca irisinin serum glukoz ve HDL seviyesini azalttığı buna karşın LDL, kolestrol ve TG seviyelerinde ise artışa sebep olduğu görüldü (p<0.05). Sonuç: Tüm bu bulgular irisinin iştahı arttırdığını ancak artan yem tüketimine rağmen vücut ağırlığını değiştirmediğini göstermektedir.Öğe Bioactive contents, In vitro antiradical, antimicrobial and cytotoxic properties of rhubarb (Rheum ribes L.) extracts(Taylor & Francis Ltd, 2020) Keser, Serhat; Keser, Fatma; Karatepe, Mustafa; Kaygili, Omer; Tekin, Suat; Turkoglu, Ismail; Demir, ErsinRheum ribes L. (rhubarb) is belonging to Polygonaceae, and its roots and fresh shoots are consumed as vegetable in Turkey. This plant is considered to be one of the most important pharmaceutical raw materials in Middle East. In this study, the antiradical, antimicrobial, cytotoxic and bioactive properties of water, ethanol, and methanol extracts of R. ribes stems were determined. R. ribes stems water, ethanol and methanol extracts are better scavenged ABTS(center dot+) (99.27, 99.91, and 99.88%), DPPH center dot (83.11, 81.42, and 83.26%), and OH center dot radicals (93.49, 94.21, 95.86%) than standard antioxidant BHA (95.32, 80.49, and 93.78%). Stems of R. ribes abundantly include bioactive compounds, dominated by rutin, catechin, caffeic acid, ferulic acid, alpha-tocopherol and vitamin D. These extracts show effective cytotoxic properties against PC-3, A2780, HCT-116 and MCF-7 cancer cell lines at 24h. It is found that R. ribes contain high amount important bioactive contents, and has effective antiradical and cytotoxic properties.Öğe Cannabinoid Type 2 Receptor Activation Reduces Inflammation and Apoptosis in the Lung in Model of Sepsis Induced by Cecal Ligation Puncture(Wiley, 2019) Cakir, Murat; Tekin, Suat; Doganyigit, Zuleyha; Oflamaz, Asli Okan[Abstract Not Available]Öğe Cannabinoid type 2 receptor agonist JWH-133, attenuates Okadaic acid induced spatial memory impairment and neurodegeneration in rats(Pergamon-Elsevier Science Ltd, 2019) Cakir, Murat; Tekin, Suat; Doganyigit, Zuleyha; Erden, Yavuz; Soyturk, Merve; Cigremis, Yilmaz; Sandal, SuleymanAim: Cannabinoid system has various physiological roles such as neurogenesis, synaptic plasticity and emotional state regulation in the body. The presence of cannabinoid type 2 receptor (CB2), a member of the cannabinoid system, was detected in different regions of the brain. CB2 receptor plays a role in neuroinflammatory and neurodegenerative processes. We aimed to determine the possible effect of CB2 agonist JWH-133 in Okadaic acid (OKA)-induced neurodegeneration model mimicking Alzheimer's Disease (AD) through tau pathology. Materials and methods: In this study, 40 Sprague Dawley male rats were divided into 4 groups (Control, Sham, OKA, OKA + JWH-133). Bilateral intracerebroventricular (icv) injection of 200 ng OKA was performed in the OKA group. In the OKA + JWH-133 group, injection of JWH-133 (0.2 mg/kg) was performed intraperitoneally for 13 days different from the group of OKA. Morris water maze test was used to evaluate the spatial memory. Levels of caspase-3, phosphorylated tau (ser396), amyloid beta (A beta), tumor necrosis factor-alpha (TNF-alpha) and interleukin-1 beta (IL-1 beta) levels in brain cortex; and the hippocampus regions were examined by immunohistochemical methods. Key findings: In the OKA group, caspase-3, phosphorylated tau (ser396), A beta, IL-1 beta levels were higher in the cortex and hippocampus than in the other groups. The implementation of the JWH-133 reversed the increments in these parameters, and also prevented spatial memory impairment.Öğe Cannabinoid Type 2 Receptors Activation Improves Cognitive Dysfunction in a Okadaic Acid Induced Alzheimer Rat Model(Karger, 2018) Cakir, Murat; Tekin, Suat[Abstract Not Available]
