Biological Activity of Newly synthesized Cyclotriphosphazene Derivatives


Koyunoğlu D., Cemaloğlu R., Asmafiliz N., Açık L.

13th INTERNATIONAL MOLECULAR BIOLOGY AND BIOTECHNOLOGY CONGRESS, Adana, Türkiye, 4 - 06 Kasım 2024, ss.15, (Özet Bildiri)

  • Yayın Türü: Bildiri / Özet Bildiri
  • Basıldığı Şehir: Adana
  • Basıldığı Ülke: Türkiye
  • Sayfa Sayıları: ss.15
  • Gazi Üniversitesi Adresli: Evet

Özet

Chlorocyclophosphazenes, have highly reactive P-Cl bonds, can give substitution reactions with different nucleophiles. Hexachlorocyclotriphosphazene (N 3 P 3 Cl 6 ; trimer; HCCP) is the best known starting cyclic phosphazene and is widely used in the design of new cyclotriphosphazenes. It is known that structures containing ferrocene rings are also effective in biological activity studies. In the study, monospirocyclotriphosphazenes were synthesized by combining ferrocenyldiamines with a biocompatible compound, trimeric phosphazene compound. This study focused on investigating the antimicrobial activities and DNA interactions of several phosphazenes, numerically labeled as compounds 4c and 5b. The microdilution and agar well diffusion method was used to examine the antimicrobial activity and minimum inhibitory concentration (MIC) values of the phosphazenes against 14 different strains of microorganisms, 11 of which are bacteria and 3 of which are yeasts. Additionally,

Minimum Bactericidal/Fungicidal Concentration (MBC/MFC) was also measured using the microdilution method. Compounds were interacted with pBR322 plasmid DNA and their effects on DNA were observed by agarose gel electrophoresis. This determined whether the compounds bound to DNA or not by cutting with BamHI and HindIII restriction endonuclease enzymes. This results showed that the MIC values of the compounds used in this study lie in the range of <19.5 to >2500 μM. Among them, compound 5b exhibited the highest potential as an antimicrobial agent against 7 out of the 11 tested bacteria. Also, compound 5b showed strong activity against 3 yeast strains C. albicans, C.krusei and C. tropicalis. The MBC, and MFC values of the studied compounds ranged from 19.5 to >2500 μM. All of the studied compounds partly inhibited DNA restriction, indicating that they partly bind to A/A and G/G nucleotides. In addition, as a result of the studies, it was revealed that the compound 4c used showed antimicrobial activity and also affected DNA. (4c compound: Spiro[(2- methyl-1-ferrocenylmethyl)]ethane-1,2-diamino-4-metronidazole-4,6,6 trichlorocyclotriphosphatriene; 5bcompound:Spiro[(2-ethyl-1-ferrocenylmethyl)]ethane-1,2-diamino-4,4,6,6 tetrakisbutylaminocyclotriphosphatriene.