Isolation and biological evaluation of roseofungin and its cyclodextrin inclusion complexes

2020

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DOI 10.31489/2020ch4/35-44
Data confidence 70 medium
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Abstract

Roseofungin belongs to polyene antibiotics which is more active and less toxic comparing other polyenes of this group. Roseofungin was isolated from Actinomyces roseoflavus var. Roseofungini using different chro-matographic techniques and for the first time, the complexation of roseofungin with α-, β- and γ-cyclodextrin derivatives was performed. The binding patterns of the resulted complexes were studied in silico using mo-lecular docking techniques. The best binding mode was for roseofungin against γ-CD with an affinity value of ˗42.98 kcal/mol. The proposed binding mode of roseofungin against α-CD showed unusual interaction with an affinity value of ˗41.80 kcal/mol. Also, roseofungin bonded to β-CD with a binding affinity value of ˗35.03 kcal/mol. The antiradical and cytotoxic activities of roseofungin and its obtained α-, β- and γ-cyclo-dextrin complexes were determined. The antiradical activity was performed using butylhydroxyanisole as a reference, while the cytotoxic activity was determined using Artemia salina crustaceans. As a result of the biological activity study, it was found that roseofungin and some of its complexes have weak antiradical activities.