Antibiyotik ve antioksidan yapılar içeren biyouyumlu polihedral oligomerik silseskioksan (POSS) nano konjugatların hazırlanması ve biyokimyasal aktivitelerinin incelenmesi
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Dosyalar
Tarih
2016
Yazarlar
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Yayıncı
İnönü Üniversitesi
Erişim Hakkı
info:eu-repo/semantics/embargoedAccess
Özet
Nanoboyutlu malzemeler üzerine gerçekleştirilen çalışmalar son yıllarda büyük bir gelişme göstermektedir. Bu gelişmeye dahil olmak adına tez kapsamında, antibiyotik ve antioksidanlar için çok daha etkin, biyouyumlu, nano boyutlu formülasyonların ortaya konulması amaçlanmıştır. Bu amaç doğrultusunda kolayca fonksiyonelleştirilebilir, biyouyumlu, nano boyutlu POSS (polihedral oligomerik silseskioksan) yapısı tercih edilmiştir. Bu tercih doğrultusunda POSS temelli sefotaksim, metronidazol, melatonin ve N-asetil-L-sistein (NAC) içeren yeni formülasyonlar sentezlendi. Yapıların karakterizasyonları FTIR, NMR, SEM-EDX ve termal özellikleri DTA, TGA, DSC gibi termal analiz sistemleri ile belirlendi. Antibakteriyel test sonuçlarımızda IC50 değerleri E.coli bakterisinde POSS-Sefotaksim nano konjugatı ve sefotaksim için sırasıyla 11,51±3,02 ve 62,71±14,30µg/mL olarak belirlenmiş, S.aureus bakterisinde ise POSS-Sefotaksim ve sefotaksim için IC50 değerleri sırasıyla 26,20±11,14 ve 144,17±20,90µg/mL olarak belirlenmiştir. POSS-Metronidazol nano konjugatında E.coli ve S.aureus için IC50 değerleri sırasıyla 304,17±7,2 ve 260,00±17,32µg/mL, metronidazol'de ise E.coli için IC50 1933,33±115,47µg/mL ve S.aureus için IC50 1416,67±144,33µg/mL olarak belirlenmiştir. POSS-Sefotaksim ve POSS-Metronidazol nano konjugatlarının saf sefotaksim ve metronidazol antibiyotiklerine göre IC50 değerlerindeki düşüşler istatiksel olarak anlamlı olup (p<0.05) istenilen yüksek antibakteriyel etkinlik elde edilmiştir. POSS-Melatonin ve saf melatonin ABTS radikal süpürme aktivitesi % inhibisyon olarak %41,91±0,80 ve %14,05±0,43 bulunmuştur (p<0.05). POSS-NAC konjugatında ise radikal süpürme özelliği saf NAC bileşiği ile benzer olarak belirlenmiştir. Tez kapsamında; tek bir molekülde birden fazla sayıda etkin grup bulundurularak, düşük doz uygulamalarında yüksek düzeyde antibakteriyel ve antioksidan aktiviteye sahip nano konjugat formülasyonları elde edilmiştir.
Studies carried out on nano-sized materials have been showing a great improvement in recent years. In order to contribute this development, this thesis was aimed to put forward biocompatible nano formulations for more effective antibiotics and antioxidants. For this purpose, easily functionalized, biocompatible nano POSS (polyhedral oligomeric silsesquioxane) structure that could be formulated was preferred. For this reason, the new formulations including POSS-based cefotaxime, metronidazole, melatonin and N-acetyl-L-cysteine (NAC) were synthesized. The structural characterization of materials were determined with NMR, FTIR, SEM-EDX and the thermal properties of structures were determined by thermal analysis systems like DTA, TGA and DSC. According to our antibacterial test results with E.coli bacteria, the values of IC50 was measured as 11,51±3,02 and 62,71±14,30µg/mL for POSS-Cefotaxime nano conjugate and cefotaxime, respectively. In addition, from the antibacterial test results with S.aureus bacteria, the values of IC50 was found to be 26,20±11,14 and 144,17±20,90µg/mL for POSS-Cefotaxime and cefotaxime. For POSS-Metronidazole nano conjugate, the values of IC50 was measured as 304,17±7,22 and 260,00±17,32µg/mL from the E.coli and S.aureus bacteria, respectively. Also, for metronidazole, the values of IC50 was measured as 1933,33±115,47 and 1416,67±144,33µg/mL from the E.coli and S.aureus bacteria, respectively. When compared to pure cefotaxime and metronidazole antibiotics, higher antibacterial activity has been achieved from POSS-Cefotaxime and POSS-Metronidazole nano conjugates with reduced IC50 values, which are statistically meaninful (p<0.05). POSS-Melatonin and pure melatonin ABTS radical scavenging activity was found to be %41,91±0,80 and %14,05±0,43 inhibition (p<0.05). In POSS-NAC conjugate, radical scavenging property was determined to be similar to the NAC pure compounds. In this thesis; nano-conjugated formulations were obtained by taking multiple active groups to one molecule in low dose applications offering relatively high antibacterial and antioxidant activities.
Studies carried out on nano-sized materials have been showing a great improvement in recent years. In order to contribute this development, this thesis was aimed to put forward biocompatible nano formulations for more effective antibiotics and antioxidants. For this purpose, easily functionalized, biocompatible nano POSS (polyhedral oligomeric silsesquioxane) structure that could be formulated was preferred. For this reason, the new formulations including POSS-based cefotaxime, metronidazole, melatonin and N-acetyl-L-cysteine (NAC) were synthesized. The structural characterization of materials were determined with NMR, FTIR, SEM-EDX and the thermal properties of structures were determined by thermal analysis systems like DTA, TGA and DSC. According to our antibacterial test results with E.coli bacteria, the values of IC50 was measured as 11,51±3,02 and 62,71±14,30µg/mL for POSS-Cefotaxime nano conjugate and cefotaxime, respectively. In addition, from the antibacterial test results with S.aureus bacteria, the values of IC50 was found to be 26,20±11,14 and 144,17±20,90µg/mL for POSS-Cefotaxime and cefotaxime. For POSS-Metronidazole nano conjugate, the values of IC50 was measured as 304,17±7,22 and 260,00±17,32µg/mL from the E.coli and S.aureus bacteria, respectively. Also, for metronidazole, the values of IC50 was measured as 1933,33±115,47 and 1416,67±144,33µg/mL from the E.coli and S.aureus bacteria, respectively. When compared to pure cefotaxime and metronidazole antibiotics, higher antibacterial activity has been achieved from POSS-Cefotaxime and POSS-Metronidazole nano conjugates with reduced IC50 values, which are statistically meaninful (p<0.05). POSS-Melatonin and pure melatonin ABTS radical scavenging activity was found to be %41,91±0,80 and %14,05±0,43 inhibition (p<0.05). In POSS-NAC conjugate, radical scavenging property was determined to be similar to the NAC pure compounds. In this thesis; nano-conjugated formulations were obtained by taking multiple active groups to one molecule in low dose applications offering relatively high antibacterial and antioxidant activities.
Açıklama
01.02.2019 tarihine kadar kullanımı yazar tarafından kısıtlanmıştır.
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Karaca Açarı, İ. (2016). Antibiyotik ve antioksidan yapılar içeren biyouyumlu polihedral oligomerik silseskioksan (POSS) nano konjugatların hazırlanması ve biyokimyasal aktivitelerinin incelenmesi. İnönü Üniversitesi Fen Bilimleri Enstitüsü. 1-133 ss.
