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  1. Ana Sayfa
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Yazar "Doğan, Murat" seçeneğine göre listele

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  • Küçük Resim Yok
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    ANTROPOMETRİK ÖLÇÜMLERİN POLİS ADAYLARININ SİLAH ATIŞ PERFORMANSLARI ÜSTÜNDE ETKİSİ
    (Hitit Üniversitesi, 2017) Özgün Başıbüyük, Gülüşan; Acar, Sercan; Doğan, Murat
    Antropometri, bireyin beden şeklini sayısal olarak ifade edebilen bir tekniktir. Özellikle ergonomik tasarımların oluşturulmasında bireylerden alınan antropometrik ölçümler, üreticilerin ve tasarımcıların kişiye özgü ürünler üretmesini sağlar. Bu çalışmanın amacı alınan antopometrik ölçümler ile polis adaylarının silah atış performansı arasındaki ilişkiyi belirlemek ve etkisini tespit etmektir. Çankırı ili Polis Meslek Eğitim Merkezi’nde öğrenim gören 14. dönem 244 polis aday bu araştırmanın materyalidir. Bireylerden antropometrik ölçümler alınarak beden kitle indeksleri hesaplanmıştır. Daha sonra silah atışları gerçekleştirilerek performansları değerlendirilmiştir. Sonuç olarak silah kullanma performansı atış puanlarını etkilemiştir ve polis adayı olmak için BKE değerinin 18-27 arası olması gerekmektedir.
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    Characterization of Nanoparticles Containing Achillea Phrygia and Their Antioxidant and Antiproliferative Properties
    (2022) Doğan, Murat; Taşkın, Duygu; Ermanoğlu, Mizgin; Arabacı, Turan
    In this study, antioxidant and antiproliferative properties of ‘‘Achillea phrygia’’ were investigated. Since the antioxidant and antiproliferative activity of B sub-extract from plant’s chloroform extract is higher than other extracts, B sub-extract of Achillea phrygia was used in the preparation of nanoparticles. Characterization of nanoparticles was made, antiproliferative activities and IC50 values of nanoparticles and only chloroform extract was calculated by cell culture studies and XTT cell viability test. According to the results, it was observed that the extract-loaded chitosan nanoparticles had a strong antiproliferative activity in both MCF 7 and HT29 cells. The results of this study support that bioactive extract of the Achillea phrygia plant can be prepared as an herbal medicine candidate by preparing formulations with biopolymers and being investigated in cancer studies.
  • Küçük Resim Yok
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    Determination of biological studies and molecular docking calculations of isatin-thiosemicarbazone hybrid compounds
    (Elsevier, 2022/09/15) Koçyiğit,Ümit M.; Doğan, Murat; Muğlu, Halit; Taslimi, Parham; Tüzün,Burak; Yakan,Hasan; Bal, Halil; Güzel,Emre; Gülçin,İlhami
    Design, synthesis, structural elucidation, and investigation of cytotoxic and antimicrobial activity, butyrylcholinesterase (BChE), and acetylcholinesterase (AChE) enzyme inhibition effects of isatinthiosemicarbazone hybrid compounds (1–15) are reported in this study. Hybrid compounds (14 and 15) were synthesized, isolated, and characterized for the first time. FT-IR, 1H NMR, and 13C NMR spectroscopic methods and elemental analysis were used to characterize the structures of the compounds. In the enzymatic evaluation, hybrid compound 13 was observed as the most potent inhibitor of AChE with a K˙ I value of 0.94 ± 0.13 μM (all compound K˙ I values between 0.94 ± 0.13 and 4.47 ± 0.92), also this compound was observed as the most potent inhibitor of BChE with a K˙ I value of 0.82 ± 0.11 μM (all compounds had K˙ I values between of 0.82 ± 0.11 and 3.48 ± 0.92). Almost all compounds were shown better inhibition profile than standard compound. In the theoretical calculations, the comparison of the biological activities of isatin-thiosemicarbazone hybrid derivatives against enzymes was studied. The enzymes studied in docking calculations are AChE and BChE. Then, ADME/T analysis was conducted to examine the drug properties of these derivatives. Besides, the antimicrobial activity of these molecules was investigated by the microdilution method according to Clinical Laboratory Standards Institute (CLSI) criteria in the study. Cytotoxic activity of isatin-thiosemicarbazone hybrids was determined by the XTT cell viability assay on human breast cancer cell lines MCF-7 and MDA-MB-231. Among the hybrid compounds, compound 8 exhibited the most potent cytotoxic activity with IC50 values of 23.42 ± 0.21 μg/mL and 19.68 ± 0.23 μg/mL on MCF-7 and MDA-MB-231 cell lines, respectively. Overall, the hybridization of isatin and thiose
  • Küçük Resim Yok
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    Effect of captopril on the oxidative damage caused by pentylenetetrazole in the SHSY-5Y human neuroblastoma cell line
    (Sivas Cumhuriyet University, 2020) Doğan, Murat; Karademir, Mustafa
    Objective: Epilepsy is a crucial brain disorder that seizures could cause a neuronal loss in the hippocampus. Oxidative stress has an important role in the pathology of this way. The aim of this study was to investigate the neuroprotective effect of captopril, on pentylenetetrazole (PTZ) induced epileptic seizures in SH-SY5Y cell line. Method: In this XTT cell viability assay, captopril was performed in vitro SH-SY5Y cell culture to evaluate PTZ-induced neurotoxicity. Tissue TOS concentrations at the cell supernatants were quantified with the automated assay method. Hydrogen peroxide was used for the calibration of the assay.Results: When XTT cell viability results were evaluated, captopril did not affect neuronal viability in SH-SY5Y cell line. Moreover, captopril did not have significant effect on TOS levels (***P>0. 001)Conclusions: Results showed that, captopril did not have neuroprotective properties in SH-SY5Y cell line after PTZ-induced neurotoxicity.
  • Küçük Resim Yok
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    Evaluation of the knowledge and opinions of university students in rational drug use
    (Sivas Cumhuriyet University, 2020) Doğan, Murat; Saraç, Bülent
    Objective: The aim of this study is to evaluate the knowledge and opinions of students at Sivas Cumhuriyet University on rational drug use.Method: In this study, 400 students at different faculties at Sivas Cumhuriyet University constituted the universe of this study. All students who agreed to participate in the study were included. A questionnaire consisting of 17 questions about rational drug use was prepared and students were allowed to participate in the survey with their own consent.Results: In our study, the responses of the participants to the questions in the questionnaire study were evaluated. According to the results, it was observed that the participants do not have sufficient information about rational drug utilization. It was observed 230 women participants and 170 men participants included in our study.Conclusions: As a result of the survey, the opinions of the participants were evaluated. According to the results obtained, the majority of the participants should be informed about rational drug use.
  • Küçük Resim Yok
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    In vitro bioactivity and gene silencing effect of shRNA-VEGF loaded chitosan nanoparticles
    (Ümit Muhammet KOÇYİĞİT, 2022) Doğan, Murat
    Purpose: In this study, it is aimed to prepare chitosan nanoparticles containing shRNA-VEGF and evaluate their bioactivity by in vitro cell culture studies and to perform mechanical characterization of nanoparticles. Material and Methods: Ionic chelation method was used to prepare nanoparticles. The XTT assay was used to assess the cytotoxic activity of shRNA-VEGF and shRNA-VEGF loaded NP on the HeLa and NIH 3T3 cells. Results: According to the results IC50 values of shRNA-VEGF and NP including shRNA-VEGF were calculated. IC50 values of shRNA-VEGF and NP including shRNA-VEGF were 0.89±0.010 µg/mL and 0.52±0.004 µg/mL on HeLa cell line. Bax quantities of control, shRNA-VEGF, and shRNA-VEGF loaded NP was measured as 23.70±0.27 ng/mg protein, 34.64±0.36 ng/mg protein, and 39.46±0.54 ng/mg protein, respectively. According to the results, cleaved caspase 3 quantities of control, shRNA-VEGF, and shRNA-VEGF loaded NP was measured as 711.70±4.40 pg/mg protein, 767.23±3.82 pg/mg protein, and 825.32±5.06 pg/mg protein, respectively. Conclusion: shRNA-VEGF and shRNA-VEGF loaded NP significantly reduced HeLa cell reproduction in a concentration-dependent manner while generating no cytotoxicity in NIH 3T3 cells. The expression of pro-apoptotic Bax and cleaved caspase 3 proteins was significantly increased by shRNA-VEGF and shRNA-VEGF loaded NP.
  • Küçük Resim Yok
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    Investigation of the effect of paracetamol against glutamate-induced cytotoxicity in C6 glia cells
    (2021) Doğan, Murat; Yıldızhan, Kenan
    Paracetamol is an active metabolite with analgesic and antipyretic properties of phenacetin, which is sold without a prescription in our country and in many countries. However, the effect of paracetamol on oxidative stress due to glutamate-induced cytotoxicity remains unclear. This study aims to investigate the effect of an appropriate dose of paracetamol on nitric oxide and increased oxidative stress as a result of glutamate-induced cytotoxicity in C6 cells. The cells were divided into 4 groups as Control group, Glutamate group, Paracetamol group, and Paracetamol+Glutamate group. Cell viability rate between groups was measured by XTT assay. Oxidative stress and antioxidant levels were measured with TOS and TAS elisa kits. Paracetamol at all concentrations significantly increased cell viability in C6 cells (p < 0.001). Paracetamol also increased TAS levels (p <0.01) while significantly decreased TOS levels (p < 0.001). In addition, paracetamol was observed to decrease TNF-? and NO levels (p <0.001). In conclusion, paracetamol has protective feature on glutamate-induced cytotoxicity in C6 glial cells by suppressing oxidative stress. The results of this study show that when the appropriate dose of paracetamol is used, it can be a crucial promoter agent in glutamate toxicity-induced neurodegeneration.
  • Küçük Resim Yok
    Öğe
    Investigation of the effect of paracetamol against glutamate-induced cytotoxicity in C6 glia cells
    (Sivas Cumhuriyet Üniversitesi, 2021) Doğan, Murat; Yıldızhan, Kenan
    Paracetamol is an active metabolite with analgesic and antipyretic properties of phenacetin, which is sold without a prescription in our country and in many countries. However, the effect of paracetamol on oxidative stress due to glutamate-induced cytotoxicity remains unclear. This study aims to investigate the effect of an appropriate dose of paracetamol on nitric oxide and increased oxidative stress as a result of glutamate-induced cytotoxicity in C6 cells. The cells were divided into 4 groups as Control group, Glutamate group, Paracetamol group, and Paracetamol+Glutamate group. Cell viability rate between groups was measured by XTT assay. Oxidative stress and antioxidant levels were measured with TOS and TAS elisa kits. Paracetamol at all concentrations significantly increased cell viability in C6 cells (p < 0.001). Paracetamol also increased TAS levels (p <0.01) while significantly decreased TOS levels (p < 0.001). In addition, paracetamol was observed to decrease TNF-α and NO levels (p <0.001). In conclusion, paracetamol has protective feature on glutamate-induced cytotoxicity in C6 glial cells by suppressing oxidative stress. The results of this study show that when the appropriate dose of paracetamol is used, it can be a crucial promoter agent in glutamate toxicity-induced neurodegeneration.
  • Küçük Resim Yok
    Öğe
    Lomber spondilozlu hastalarda fizik tedavi ile birlikte balneoterapinin etkinliğinin değerlendirilmesi
    (Cumhuriyet Üniversitesi, 2008) Doğan, Murat; Elden, Hasan
    Amaç: Balneoterapi lomer spondilozlu hastaların tedavisinde yaygın olarak kullanılmaktadır fakat balneoterapinin yararlı etkileri ve etki mekanizmaları hala tartışmalıdır ve bu konuda sınırlı sayıda çalışma bulunmaktadır. Biz bu çalışmada lomber spondilozlu hastalarda, kombine balneoterapi ve fizik tedavi ajanlarının ağrıya, lomber mobiliteye, fonksiyonel duruma ve yaşam kalitesine etkilerini değerlendirmeyi amaçladıkYöntem: Lomber spondiloz tanısı alan 60 hasta, 35 ve 25 kişilik 2 gruba ayrıldı. Birinci gruba 3 hafta süreyle balneoterapi, fizik tedavi ajanları [ ultrason (1 Mhz frekansında, 1.5 w/cm2 dozunda,6 dakika), TENS (50-100 frekansında, 20 dakika), hotpack (20 dakika) ], medikal tedavi (NSAİİ ve myorelaksan) ve egzersiz programı uygulandı. İkinci gruba ise, balneoterapi haricinde aynı protokol uygulandı. Hastalar ağrı değerlendirilmesi için visuel analog skala (VAS), mobilite değerlendirilmesi için bel hareketleri ( el parmak zemin mesafesi (EPZM), lomber schober (LS) testi, ekstansiyon ve lateral fleksiyon dereceleri ), fonksiyonel yetersizlik için Modifiye Oswestry İndeksi ( MOI ) izlem parametreleri kullanılarak klinik iyileşme açısından değerlendirildi.Sonuçlar: 3 hafta süren tedavi sonunda her iki grupta da anlamlı iyileşmeler olurken, özellikle balneoterapi uygulanan grupta balneoterapi uygulanmayan gruba göre anlamlı ağrı azalması, lomber mobilite artışı (sağ ve sol lateral fleksiyon hariç) ve fonksiyonel iyileşme gözlendi.Yorum: Balneoterapi ve fizik tedavi ajanlarının kombine kullanımı lomber spondilozlu hastaların ağrısında azalma, mobilitelerinde artış, fonksiyonel durumlarında iyileşme ve yaşam kalitelerinde artış ile sonuçlanmaktadır.Anahtar Kelimeler: Balneoterapi, Fizik Tedavi Ajanları, Lomber Spondiloz, Fonksiyonel Yetmezlik
  • Küçük Resim Yok
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    Plasmid DNA isolation and characterization studies
    (Sivas Cumhuriyet University, 2021) Doğan, Murat
    Objective: The use of gene therapy for targeted therapy in various genetic diseases has become more and more popular day by day. Various carrier vectors are used in gene therapy. The plasmid we are interested in in this study is used as a gene delivery vector. In this study, it was aimed to perform the isolation and characterization studies of the peGFP-N1 plasmid. In addition, necessary properties were investigated to make it a suitable gene carrier vector.Method: In this study, isolation was performed using the plasmid peGFP-N1 via classical method. Escherichia coli was used as expression medium in the isolation process. In order to calculate the amount of plasmid DNA in the studies, the spectral curve value of the plasmid DNA was calculated. Spectrophotometric methods were used to determine the amount and impurity of the isolated bacterial DNA.Results: In plasmid DNA isolation studies, it was observed that the yield was quite high and the contamination from protein or RNA was very low. In fact, the ratio of absorbance values (A1/A2) is very close to 1.8 as a result of the isolation III study shows that there is no contamination.Conclusions: The isolation and spectrophotometric study results of the peGFP-N1 plasmid showed that this plasmid is suitable and usable in terms of impurity and contamination risk. By making use of the results of this study, it will support the studies in which this plasmid can be used in an appropriate gene carrier system.
  • Küçük Resim Yok
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    Polis adaylarının bazı antropometrik ölçümleri ile silah atış performanslarının karşılaştırılması
    (Cumhuriyet Üniversitesi, 2016) Doğan, Murat; Başıbüyük, Gülüşan Özgün
    Devletin temel görevlerinden birisi de şüphesiz ki güvenlik konusudur. Güvenliği sağlarken de kamu düzenini korumak temel ilkelerindendir. Güvenlik hizmetleri ne kadar eksiksiz olursa kamu düzeni de o derece korunur. Kamu düzeni için, kendisinin ve masum insanların can ve mal güvenliğini korumak için güvenlik güçlerine silah kullanabilme yetkisi verilmiştir. Bu da kanunlarla yasal hale gelmiştir. Ölçülülük, orantılılık ilkesi doğrultusunda bu yetki kullanılmaktadır.Bu tez çalışmasında polisin; kanunlar çerçevesinde silahını kullanırken fiziksel şartlarının buna etki edip etmediği, hangi şartlarda daha iyi silah kullanabildiği araştırılmaya çalışılmıştır. Araştırma yapılırken Antropometrik değerlerin silah performanslarına etki edip etmediği araştırılmış, bununla ilgili ölçümler alınmıştır. Bu Antropometrik ölçümler, boy uzunluğu, ağırlık, işaret parmağı uzunluğu (tetik parmağı), el uzunluğu, el genişliği olmak üzere toplam (6) ölçü ve ağırlık/boy2 formülünden hesaplanan Beden Kütle Endisi (BKE)' dir. Bu araştırma yaklaşık 8 ay sürmüş, Çankırı Polis Meslek Eğitim Merkezi Polis adaylarından 244 öğrenci üzerinden kişisel bilgiler ve Antropometrik ölçüler bir bilgi formu yardımı ile alınmıştır. Ayrıca silah performans atışları da POMEM atış alanında kayıtları tutulmak üzere gözlemlenerek veriler kaydedilmiştir. Araştırmada kullanılan veriler bilgisayar ortamına aktarılarak SPSS 21.0 yardımıyla analizi yapılmıştır. Güvenilirlik çalışması yapılmış, alfa değeri 0,94 bulunmuştur ve yapılan çalışma güvenilirlik olarak pozitiftir. Araştırmamızda uyguladığımız test sonuçlarına göre (BKE) değerleri 27 ye yaklaştıkça, öğrencilerin uzun menzilli tabanca performanslarının daha iyi olduğu saptanmıştır. Ayrıca unutulmamalıdır ki polis okulu öğrencisi olmak için (BKE) değeri 18-27 arası olması gerekmektedir.Bilgi ve veri formunda bulunan daha önce silah kullanıp kullanmadığı sorusuna verilen evet cevaplarının silah performanslarını etkilediği ölçülmüştür.Yapılan araştırmanın silah performansı ölçümleri kısmında işin içine yetenek ister istemez girmiştir, yetenek konusu da sayısal verilerle ölçümlenemediği için çalışmanın silah kısmında ölçümleri, performansları az da olsa etkilemiştir. Anahtar Kelimeler: Antropometri, Silah, Silah Performansı, Polis
  • Küçük Resim Yok
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    Preparation and characterization of chitosan nanoparticles with extracts of Rheum ribes, evaluation of biological activities of extracts and extract loaded nanoparticles
    (Pamukkale University, 2024) Doğan, Murat; Koçyiğit, Ümit Muhammet; Taşkın, Duygu; Yılmaz, Beyza Nur; Taşkın, Turgut
    The biological activities of different parts of the Rheum ribes plant were evaluated comparatively. Extracts showing strong biological activity were identified and it was determined which of the extract-loaded nanoparticles showed stronger activity. Cytotoxic activity of R. ribes extracts was calculated on glial (C6) and fibroblast (NIH 3T3) cells using XTT assay. Spectrophotometry was used to evaluate the impact of these compounds on the enzyme activities of human carbonic anhydrase I and II (hCA I and hCA II). The findings showed that chitosan NPs with extracts loaded on them have a lower IC50 value and more cytotoxic activity in C6 cells than chitosan NPs with only extracts. R. ribes young shoots ultrasonic methanol extract (RYU) was shown to have the strongest antiproliferative efficacy against C6 cells. Results showed that RYU and ultrasonic methanol extract of R. ribes radix (RRU) were determined as the best carbonic anhydrase inhibitors. According to results of particle size, encapsulation efficiency, and release studies of chitosan NPs, it has been observed that they are suitable for application. At a concentration of 10 µg/mL, it was found that none of the R. ribes extracts exhibited cytotoxic action toward the NIH 3T3 cell line. According to results of particle size, encapsulation efficiency, and release studies of chitosan NPs, it has been observed that they are suitable for application. It was observed that none of the extracts of R. ribes at a concentration of 10 µg/mL showed cytotoxic activity in the NIH 3T3 cell line. © The Author(s) 2024.
  • Küçük Resim Yok
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    Preparation of chitosan nanoparticles and characterization studies
    (Sivas Cumhuriyet University, 2020) Doğan, Murat
    Objective: The aim of this study was to prepare different nanoparticles using chitosan and tripolyphosphate and to perform characterization studies of nanoparticles. In addition, FTIR spectrum measurements were aimed to determine specific chemical groups and bonds in the structures of nanoparticles and materials. Method: In this study, different nanoparticles were prepared and their zeta potential, particle size and polydispersity index were measured. Moreover, specific chemical groups of nanoparticles and materials used in nanoparticles were determined by FTIR spectrum study. Morphological properties of nanoparticles were evaluated using scanning electron microscopy. Results: According to the zeta potential measurement results, A3 (18.66 ± 0.22) and A2 (14.32 ± 0.14) formulations showed the highest and the lowest zeta potential value, respectively. It was also observed that the A3 (284.22 ± 1.60) formulation had the lowest particle size. According to FTIR absorption spectrum results, a wide aliphatic O-H tension band of chitosan was observed between 1500 cm-1 -1100 cm-1. Conclusions: According to the results, it could be said that chitosan nanoparticles have the desired particle size, charge and morphological properties in terms of application. In FTIR spectrum results, bands showing specific chemical groups of chitosan, tripolyphosphate and A3 formulation were obtained.
  • Küçük Resim Yok
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    SİVAS'TA YETİŞKİN BİREYLERDE ANTROPOMETRİK ÖLÇÜMLERİN DEĞERLENDİRİLMESİ: YAŞ VE CİNSİYET FARKLILIKLARI
    (2015) Başıbüyük, Gülüşan Özgün; Sönmez, Gamze; Aktan, Burcu Korkmaz; Doğan, Murat; Ay, Faruk; Çınar, Ziynet
    Bireylerin sağlık ve beslenme durumlarının saptanmasında antropometri tekniği yaygın kullanılan ucuz ve pratik bir yöntemdir. Tüm dünyada ve ülkemizde yetişkin bireylerin beslenme sorunları artmakta, özellikle obezite oranlarında hızla artış görülmektedir. Bunun sonucunda, beslenme sorunlarını belirleyici ve önleyici çalışmalar önem taşımaktadır. Bu amaçla; araştırma örneklemi Sivasta yaşayan 50 yaş ve üstü 180 kadın ve 173 erkek birey, 50-64 ve 65 yaş üstü kadın ve erkek birey gruplarına ayrılmış; bireylerden boy uzunluğu, ağırlık ve bel çevresi antropometrik ölçüleri alınmıştır. Çalışma verileri; SPSS programında; bağımsız gruplarda iki ortalama arasındaki farkın önemlilik testi olan t testi (students t testi) uygulanarak değerlendirilmiştir. Alınan antropometrik ölçüler ile beden kitle indeksi (kg/m2) değerleri hesaplanmıştır. Beden kitle indeksi (kg/m2) ortalama değerleri, kadın bireylerde 50-64 arası yaş grubunda 33,91 kg/m², 65 yaş ve üstü grubu 34,19 kg/m² dir. Erkek bireylerde ise 50-64 arası yaş grubunda 29,20 kg/ m² bulunmuşken, 65 yaş ve üstü grubunda 29,60 kg/m² olduğu görülmüştür. Bu verilere göre iki yaş grubu kadın ve erkek bireylerde şişmanlık ve obezite riskinin yüksek olduğu belirlenmiştir
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    Synthesis and biological evaluation of thiosemicarbazone derivatives
    (Springer US, 2022/07/21) Doğan, Murat; Koçyiğit,Ümit M.; Gürdere,Meliha B.; Ceylan,Mustafa; Budak,Yakup
    In this study, firstly, 22 thiosemicarbazone derivatives (3a-y) were synthesized. Then, ADME parameters, pharmacokinetic properties, drug-like structures, and suitability for medicinal chemistry of these molecules were studied theoretically by using SwissADME and admetSAR programs. According to the results of these theoretical studies, it can be said that the bioavailability and bioactivity of these compounds may be high. In silico molecular docking between ligands (thiosemicarbazone derivatives) and targeted proteins (protein-78 (GRP78) for C6 and quinone reductase-2 (4ZVM for MCF 7) was analyzed using Hex 8.0.0 docking software. According to the docking data, almost all molecules had higher negative E values than Imatinib (already used as a drug). For this, in vitro anticancer studies of these molecules were done. The cytotoxic activities of thiosemicarbazone derivatives (3a-y) were evaluated on C6 glioma and MCF7 breast cancer cell lines at 24 h, and Imatinib was used as the positive control. According to the results of the cytotoxicity assay, it can be said that the five compounds (3b, c, f, g, and m with IC50 = 10.59–9.08 μg/mL; Imatinib IC50 = 11.68 μg/mL) showed more potent cytotoxic activity than Imatinib on C6 cell line. Together with to these results ten compounds (3b, d, f, g, I, k, l, m, n, and r with IC50 = 7.02–9.08 μg/mL; Imatinib IC50 = 9.24 μg/mL) had a more effective cytotoxic activity against MCF7 cell line than Imatinib. Compound 3 m showed the highest antiproliferative effect against C6 and MCF7 cell lines.
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    Synthesis, carbonic anhydrase inhibitory activity, anticancer activity and molecular docking studies of new imidazolyl hydrazone derivatives
    (Elsevier, 2022/12/05) Tapera,Michael; Kekeçmuhammed, Hüseyin; Tüzün,Burak; Sarıpınar,Emin; Koçyiğit,Ümit M.; Yıldırım,Ebrar; Doğan, Murat; Zorlu, Yunus
    A new series of imidazolyl hydrazone derivatives IA (1-12) were prepared from a condensation reaction between indoline-2,3-dione (isatin) and 2-benzylidenehydrazinecarboximidamide derivatives. The structure of compounds was elucidated using various spectral techniques including FTIR, 1H NMR, 13C NMR, and HRMS. The proposed structure of IA-2 was determined by single-crystal X-ray analysis. Synthesized compounds were evaluated for their inhibitory action against carbonic anhydrase I and II isoenzymes (hCA I and hCA II), as well as cytotoxicity activity in a cancer cell line (HT-29) and a healthy cell line (NIH 3T3). Among them, some compounds exhibited remarkable CA inhibitory activities compared to a standard inhibitor with Ki values in the range of 13.434 ± 3.278-522.549 ± 360.720 nM for hCA I (Ki value for standard inhibitor = 271.15 ± 74.620 nM) and 41.108 ± 10.180-271.171 ± 65.293 nM for hCA II (Ki value for standard inhibitor = 113.07 ± 20.980 nM) and significant antiproliferative activity with less toxicity to a health cell line. In addition, the theoretical parameters of the bioactive molecules were calculated to establish their drug-likeness qualities and ADME/T analysis was carried out to examine the drug properties of the synthesized compounds.
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    The Role of Cisplatin Loaded Biocompatible Nanoparticles in Cancer Treatment
    (2022) Kumtepe, Tuğba; Doğan, Murat
    Chemotherapeutic treatments focusing on cisplatin, ovarian cancer, testicular cancer, breast cancer, colon cancer, lung cancer etc. seen in adults and children. Cisplatin is an antineoplastic agent frequently used in cancer types. Drug resistance to cisplatin has an effect on the success of the treatment. After cisplatin-administered treatments, patients may experience cisplatin-induced side effects of various toxic dimensions, such as nausea, nephrotoxicity, cardiotoxicity, hepatotoxicity, and neurotoxicity. As a result of the literature review, various studies have been carried out to reduce the side effects and toxic effects of cisplatin and other anticancer molecules without interfering with their activities. In this study, we planned to prepare a cisplatin-loaded chitosan nanoparticle formulation based on the ionic gelation method using chitosan and tripolyphosphate (TPP) with the information obtained from the literature. In this study, chitosan nanoparticles containing the same concentration of cisplatin were applied to MDA-MB-231 breast cancer cell lines obtained from the American Type Culture Collection (ATCC). As a result, biocompatible nanoparticles with similar cytotoxic effects cause less side effects in other cells and tissues than other nanoparticles.

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