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    In-Vitro Anticancer and Antibacterial Activities of Brominated Indeno[1,2-b]qinoline Amines Supported with Molecular Docking and MCDM**
    (Wiley-V C H Verlag Gmbh, 2021) Aydin, Ali; Okten, Salih; Erkan, Sultan; Bulut, Merve; Ozcan, Evrencan; Tutar, Ahmet; Eren, Tamer
    The present study describes mono substituted indeno[1,2-b]quinolines (3 a-c and 5) have much more antiproliferative potentials than positive controls against A549, HeLa, MCF7 and Hep3B cell lines (IC50 values 1.1-29.6 mu g/mL) and show similar cytotoxicity (14.3 % to 19.8 %) to cells such as controls. Moreover, the mono substituted indeno[1,2-b]quinoline amines (3 a-c and 5) exhibit significant antimicrobial activity with MIC values between 15.62 mu g/mL and 250 mu g/mL. The compounds can also bind to DNA in the groove binding mode with a binding constant range of 1.1x10(3)-1.1x10(5) M-1. The anticancer and antibacterial properties of compounds were confirmed with the molecular docking simulation for their pharmacokinetic. As a result, the preliminary experimental data and a multi-criteria decision-making methodology (MCDM) indicated that the mono substituted indeno[1,2-b]quinoline amine derivatives, especially 3 a and 5, exhibit effective pharmacological properties. parameters and their interaction with related cells at the molecular level.
  • Küçük Resim
    Öğe
    What is the role of bosentan in healing of femur fractures in a rat model?
    (Springer Japan Kk, 2015) Aydin, Ali; Halici, Zekai; Akpinar, Erol; Aksakal, A. Murat; Saritemur, Murat; Yayla, Muhammed; Karcioglu, S. Sena
    The purpose of this study was to examine the effects bosentan (which is a strong vasoconstrictor) on bone fracture pathophysiology, and investigate the roles of the nonselective endothelin 1 receptor blocker bosentan on the bone fractures formed in rats through radiographic, histopathologic, and immunohistochemical methods. The rats were divided into three groups (six rats in each group): a femoral fracture control group, a femoral fracture plus bosentan at 50 mg/kg group, and a femoral fracture plus bosentan at 100 mg/kg group. The femoral fracture model was established by transversely cutting the femur at the midsection. After manual reduction, the fractured femur was fixed with intramedullary Kirschner wires. The radiographic healing scores of the bosentan 100 and 50 mg/kg groups were significantly better that those of the fracture control group. The fracture callus percent of new bone in the bosentan 100 mg/kg group was significantly greater than that in the control group. Also, semiquantitative analysis showed higher positive vascular endothelial growth factor and osteocalcin staining and lower positive endothelin receptor type A staining in the treatment groups than in the control group. Bosentan treatment also decreased tissue endothelin 1 expression relative to that in the fracture control group. As a result of our study, the protective effect of bosentan was shown in experimental femoral fracture healing in rats by radiographic, histopathologic, and molecular analyses.