Eczacılık Teknolojisi Bölümü Koleksiyonu

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https://hdl.handle.net/20.500.12418/13812

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BİYOLOJİK VERİTABANLARI KULLANILARAK BAKTERİYEL TOPOİZOMERAZ I HEDEFLİ TERAPÖTİK DNA APTAMERİ GELİŞTİRİLMESİ
(TÜSEB, 16.05.2023) Canturk, Pakize; Kılıçkaya, Ozan; Demir Dora, Devrim; Ensari, Yunus; Özalp, Veli Cengiz
DNA topoizomerazlar DNA topolojisini değiştirerek replikasyon ve transkripsiyon gibi canlılığı doğrudan ilgilendiren metabolik olaylarda görev alırlar. Bu nedenle kontrolsüz hücre bölünmesi/kanser ve patojenler ile savaşta kullanılabilecek en etkin ilaç hedeflerinden birini oluşturmaktadır. Ancak hem ilaç hedefinde oluşacak ifade azalması hem de ABC taşıyıcı proteinlerin ilacı terapötik dozunda hücre içerisinde tutmamasından kaynaklı ilaç direnci nedeniyle tedavide zorluklar oluşmaktadır. Ayrıca bugüne kadar birçok topoizomeraz inhibitörü geliştirilmiş olsa da bu moleküllerin tedavi süresince etkinlik kayıpları nedeniyle yeni yapıların araştırılmasına devam edilmektedir. Ancak geliştirilecek yapılar yine kimyasal madde tabanlı olacağı için tedavi süresince problemlerin oluşması sürdürülebilir bir Ar-Ge yöntemi değildir. Dahası hatalı antibiyotik kullanımı sonucu oluşan ilaç direnci nedeniyle süper bakterilerin gelişmesi de kimyasal ilaç tabanlı tedavilerin yenilenmesi ihtiyacını göstermektedir. Diğer taraftan günümüzde artan bir ivme ile hem Ar-Ge’si yapılan hem de piyasada mevcut olarak kullanılan biyofarmasötik tabanlı tedaviler düşük/olmayan toksik etkiler ve dolayısıyla biyolojik uyumları nedeniyle tedavide tercih edilmesi gereken etkin madde sınıflarını oluşturmuş bulunmaktadır. Bu biyofarmasötik grupları içerisinde bulunan aptamerler, antikorlar gibi hedeflerine yüksek özgüllükte bağlanabilen yüksek seçiciliğe sahip moleküllerdir. Günümüzde piyasada FDA tarafından onaylanmış tek bir terapötik aptamer bulunmaktadır ve bu alanda yeni moleküllerin geliştirilmesi önem arz etmektedir. Buradan hareketle projede biyolojik veritabanları kullanılarak bakteriyel topoizomeraz I hedefleyen bir DNA aptamerlerinin in-silico araçlar ile geliştirilmesi hedeflenmektedir. Veritabanları ve modellemeler kullanılarak yapılacak analiz aptamer seçiliminde kullanılan SELEX basamağını elimine edeceği için etkin maddenin tanımlanma süresi de kısalmış olacaktır.
Evaluation of the Anticancer and Biological Activities of Istaroxime via Ex Vivo Analyses, Molecular Docking and Conceptual Density Functional Theory Computations
(MDPI, 7 November 2023) Canturk, Pakize; Gok, Ege; Unal, Naz; Gungor, Burcin; Karakus, Gulderen; Kaya, Savas; Katin, Konstantin P.
Cancer is a disease that occurs as a result of abnormal or uncontrolled growth of cells due to DNA damage, among many other causes. Certain cancer treatments aim to increase the excess of DNA breaks to such an extent that they cannot escape from the general mechanism of cell checkpoints, leading to the apoptosis of mutant cells. In this study, one of the Sarco-endoplasmic reticulum Ca2+ATPase (SERCA2a) inhibitors, Istaroxime, was investigated. There has been very limited number of articles so far reporting Istaroxime’s anticancer activity; thus, we aimed to evaluate the anticancer effects of Istaroxime by cell proliferation assay and revealed the cytotoxic activity of the compound. We further determined the interaction of Istaroxime with topoisomerase enzymes through enzyme activity tests and detailed molecular modeling analysis. Istaroxime exhibited an antiproliferative effect on A549, MCF7, and PC3 cell lines and inhibited Topoisomerase I, suggesting that Istaroxime can act as a Topoisomerase I inhibitor under in vitro conditions. Molecular docking analysis supported the experimental observations. A chemical reactivity analysis of the Istaroxime molecule was made in the light of Density Functional Theory computations. For this aim, important chemical reactivity descriptors such as hardness, electronegativity, and electrophilicity were computed and discussed as detailed.
Poli[Maleik Anhidrit-Ko-Vinil Asetat] Kopolimerinin Doksorubisin/Doksorubisin Türevi Antikanser İlaçlarla Doğrusal Rasyonel Konjugatlarının Sentezi, Yapısal Karakterizasyonları Ve Çeşitli Kanser Hücreleri Üzerinde Sitotoksik/Antikanser Aktiviteleri
(20.01.2022) CANTÜRK, PAKİZE; Karakuş, Gülderen
Nanotoksik özellikli poli[Maleik Anhidrit-Ko-Vinil Asetat] kopolimerinin sentezlenmesinden sonra ilaçlar tr için iyi bir taşıyıcı olduğu çeşitli deneysel veri ve analizlerle kanıtlanmıştır. Doksorubisin/Doksorubisin türevi antikanser İlaçlar klinikte özellikle meme kanseri tedavisinden yaygın kullanıma sahiptir. Doksoru‐ bisin ve Doksorubisin türevi ilaçlarla anhidrit içerikli kopolimerin doğrusal rasyonel konjugatlarının sen‐ tezi, yapısal karakterizasyonları ve çeşitli kanser hücreleri üzerinde sitotoksik/antikanser aktiviteleri in‐ celenmiş ve meme kanserinde anlamlı akktivite tespit edilmiştir.
Evaluation of organic load related efficacy changes in antiseptic solutions used in hospitals
(TUBİTAK, 2022) Şahiner, Aslı; Halat, Ece; Alğın Yapar, Evren; Kara,Bilgen Ahsen
Abstract Background/aim: In this study, it was aimed to evaluate the change in antimicrobial efficacy related to the presence of the organic load of four different antiseptic solutions that are frequently used in hospitals. Materials and methods: Solutions of hydrogen peroxide, povidone-iodine, chlorhexidine digluconate, and ethyl alcohol were prepared, tested in terms of antimicrobial efficacy changes in the presence of organic substances, and evaluated according to EN 13727 and EN 13624 standards. Results: Among the investigated solutions ethanol 70% solution showed the best results by providing a 5-log reduction on all test organisms without affecting by the type and concentration of organic substances. Solutions of hydrogen peroxide 3%, povidone-iodine 7.5%, and chlorhexidine digluconate 0.2% performed lower antimicrobial efficacy depending on the concentration of organic load. Conclusion: It is concluded that the antimicrobial efficacy of antiseptic solutions is significantly affected by the organic substances and thus the proper use of antiseptics has become important to achieve successful disinfection and prevention of antibacterial resistance.
Design and in vitro in vivo evaluation of antioxidant bioadhesive gels for burn treatment
(TUBİTAK, 2022) Gökçe, Göksel; Karavana, Sinem Yaprak; Bağrıyanık, Hüsnü Alper; Pekçetin, Çetin; Alğın Yapar, Evren; Aybar Tural, Gülşen; Gökçe, Evren Homan.
Abstract Burn wounds are frequently encountered health problems, which need a new treatment approach especially in terms of good patient compliance. Availability of use of antioxidant agents and bio-adhesive gels in tissue healing can be an alternative as a new approach for wound healing. Antioxidant taurine containing bio-adhesive gels were prepared by using carbopol (CP) 940 and 934. Rheological and texture analyses were carried out on bio-adhesive gels for in vitro characterization. Wound model on Wistar rats was used to evaluate the in vivo evaluation of gels. Rheological and texture analyses showed that a carbopol bioadhesive gel has acceptable topically use dosage characteristics and in combination with Taurine it presented a successful wound healing effect via antioxidant parameters. In conclusion, bio-adhesive CP 940 (2%) gel containing 50 mM taurine could be promising in the treatment of burns by balancing oxidative stress.
Bioactive Loaded Novel Nano-Formulations for Targeted Drug Delivery and Their Therapeutic Potential
(MDPI, 2022) Kumari, Sapna; Goyal, Anju; Sönmez Gürer, Eda; Algın Yapar, Evren; Garg, Madhukar; Sood, Meenakshi; Sindhu, Rakesh K.
Abstract Plant-based medicines have received a lot of attention in recent years. Such medicines have been employed to treat medical conditions since ancient times, and in those times only the observed symptoms were used to determine dose accuracy, dose efficacy, and therapy. Rather than novel formulations, the current research work on plant-based medicines has mostly concentrated on medicinal active phytoconstituents. In the past recent decades, however, researchers have made significant progress in developing “new drug delivery systems” (NDDS) to enhance therapeutic efficacy and reduce unwanted effects of bioactive compounds. Nanocapsules, polymer micelles, liposomes, nanogels, phytosomes, nano-emulsions, transferosomes, microspheres, ethosomes, injectable hydrogels, polymeric nanoparticles, dendrimers, and other innovative therapeutic formulations have all been created using bioactive compounds and plant extracts. The novel formulations can improve solubility, therapeutic efficacy, bioavailability, stability, tissue distribution, protection from physical and chemical damage, and prolonged and targeted administration, to name a few. The current study summarizes existing research and the development of new formulations, with a focus on herbal bioactive components.
Herbal Bioactives for Ocular Drug Delivery Systems
(Elsevier, Academic Press, 2022) Algın Yapar, Evren; Durgun, Meltem Ezgi; Esentürk, Imren; Güngör, Sevgi; Özsoy, Yıldız.
Herbal Bioactive-Based Drug Delivery Systems: Challenges and Opportunities provides a wide-ranging, in-depth resource for herbal bioactives, including detailed discussion of standardization and regulations. The book first explores specific drug delivery systems such as gastrointestinal, ocular, pulmonary, transdermal, and vaginal and rectal. It then discusses novel applications for nano, cosmetics, nutraceuticals, wound healing and cancer treatment. Finally, there is a section focusing on standardization and regulation which includes an enhancement of properties. This book is an essential resource for pharmacologists, pharmaceutical scientists, material scientists, botanists, and all those interested in natural products and drug delivery systems developments.

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