Yazar "Gonul, Ilyas" seçeneğine göre listele

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    Differential Immunomodulatory Activities of Schiff Base Complexes Depending on their Metal Conjugation
    (Springer/Plenum Publishers, 2019) Ayaz, Furkan; Gonul, Ilyas; Demirbag, Burcu; Ocakoglu, Kasim
    Immunomodulatory compounds have become crucial with advances in immunotherapy. Using our own immune system cells, we can direct the immune cell function and develop desired response against a certain threat. Immunotherapy applications have been suggested against tumors, autoimmune disorders, and infectious diseases. Vaccination can be considered as one of the best known example of immunotherapy. Infectious agent's signature molecular structures are introduced to the immune cells together with the adjuvants that further activate the immune cells to mount a proper immune response and memory. Immunotherapy and vaccine formulations are in constant need of a library of immunomodulatory reagents that can be applied depending on the target. In order to expand the number of immunomodulatory reagents that can find medicinal applications, our group has been testing unique chemical structures on the immune system cells, especially macrophages. Schiff base complexes are known for their anti-inflammatory and antimicrobial activities. In this study, we used previously characterized Schiff base complexes with different metal conjugations. These molecules had differential immunostimulatory and immunomodulatory potentials on macrophages in vitro depending on the type of the conjugated metal. After light exposure, these complexes changed their characteristics and became powerful anti-inflammatory complexes. Due to their possible antimicrobial potentials, we also tested their activities against gram negative and gram positive bacteria. All of the complexes exerted antimicrobial activities which were not light responsive. Here, we present Schiff base complexes with differential immunostimulatory and immunomodulatory activities that can also efficiently eliminate gram positive and gram negative bacteria. Upon photo activation, they block the production of inflammatory TNF alpha cytokine. Therefore, together with the light, they can be used to treat bacterial infections associated with damaging inflammation.
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    Novel Copper Bearing Schiff Bases with Photodynamic Anti-Inflammatory and Anti-Microbial Activities
    (Springer, 2020) Ayaz, Furkan; Gonul, Ilyas; Demirbag, Burcu; Ocakoglu, Kasim
    Schiff bases and their copper complexes have been previously studied for their anti-inflammatory, anti-tumor as well as anti-microbial activities. Schiff bases can be derivatized to gain photoluminiscence capacity. This property of the schiff bases enables the transfer of the electrons upon absorption of the light at a specific wavelength. In this study, we exploited this attribute of novel copper bearing schiff bases and tested their photodynamic biological activities. These compounds exerted photodynamic anti-inflammatory activities on the in vitro activated mammalian macrophages. Compared with salicylic acid control groups, these novel schiff bases had stronger activity which became more prominent with photo-induction. Moreover, they also had anti-microbial activity on gram negative bacteria E.coli and gram positive bacteria S.aureus.This anti-microbial activity was stronger than that of Neomycin on both bacterial strains. Our results suggest their potential use as anti-inflammatory and anti-microbial agents both in the dark as well as after photo-induction.
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    Novel Schiff Base Sulfonate Derivatives as Carbonic Anhydrase and Acetylcholinesterase Inhibitors: Synthesis, Biological Activity, and Molecular Docking Insights
    (Wiley-V C H Verlag Gmbh, 2025) Yasar, Umit; Demir, Yeliz; Gonul, Ilyas; Ozaslan, Muhammet Serhat; Celik, Gizem Gumusgoz; Turkes, Cuneyt; Beydemir, Sukru
    Sulfonate derivatives are an essential class of compounds with diverse pharmacological applications. This study presents the synthesis and detailed characterization of six novel Schiff base sulfonate derivatives (L1-L6) through spectroscopic techniques (FT-IR and NMR). Their inhibitory potential was evaluated against human carbonic anhydrase isoenzymes (hCA I and hCA II) and acetylcholinesterase (AChE), which are crucial therapeutic targets for diseases such as glaucoma, epilepsy, and Alzheimer's disease. The KI values for the compounds concerning AChE, hCA I, and hCA II enzymes were in the ranges of 106.10 +/- 14.73 to 422.80 +/- 17.64 nM (THA: 159.61 +/- 8.41 nM), 116.90 +/- 24.40 to 268.00 +/- 35.84 nM (AAZ: 439.17 +/- 9.30 nM), and 177.00 +/- 35.03 to 435.20 +/- 75.98 nM (AAZ: 98.28 +/- 1.69 nM), respectively. Molecular docking analyses revealed key interactions within the active sites of the enzymes, including hydrogen bonding with critical residues and pi-pi stacking interactions. Notably, L3 demonstrated superior inhibition against hCA I (KI: 116.90 +/- 24.40 nM) and AChE (KI: 106.10 +/- 14.73 nM), positioning it as a promising lead compound. This comprehensive investigation contributes to the development of isoform-specific inhibitors for therapeutic use and provides valuable insights into their binding mechanisms. The findings underscore the potential of Schiff base sulfonates as scaffolds in drug discovery for neurodegenerative and metabolic disorders.
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    Öğe
    Unique photodynamic antimicrobial Schiff bases and their copper complexes exert immunomodulatory activity on mammalian macrophages
    (Taylor & Francis Ltd, 2020) Gonul, Ilyas; Demirbag, Burcu; Ocakoglu, Kasim; Ayaz, Furkan
    Antibiotic resistance has been a growing problem for the public health. Especially the hospitalized patients are at high risk due to emergence of superbugs that can evade a wide range of antibiotics in use. In order to circumvent this major problem, new candidates of antimicrobial agents should be created and tested for their efficacies. Moreover, having antimicrobial agents that could get activated with light exposure (antimicrobial PDT) would create a great advantage in terms of decreasing the required effective dose as well as controlled localized activation of the candidate drugs. Schiff base derivatives have antimicrobial, antitumor, and anti-inflammatory activities. In this study, we used a unique set of Schiff base derivatives with and without copper for antimicrobial PDT applications both on gram-negative Escherichia coli and gram-positive Staphylococcus aureus. Our compounds had strong antimicrobial PDT potential especially with the addition of copper into their structures. Moreover, these Schiff base derivatives' possible immunomodulatory activities were tested on mammalian macrophages in vitro. These compounds had photodynamic anti-inflammatory activities as well. Our results suggest that these unique Schiff bases can be utilized in antimicrobial PDT applications that can also alter the function of the immune system cells to suppress excessive inflammation.