Isolation And Biological Evaluation Of Roseofungin And Its Cyclodextrin Inclusion Complexes
BULLETIN OF THE UNIVERSITY OF KARAGANDA-CHEMISTRY(2020)
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 chromatographic techniques and for the first time, the complexation of roseofungin with alpha-, beta- and gamma-cyclodextrin derivatives was performed. The binding patterns of the resulted complexes were studied in silico using molecular docking techniques. The best binding mode was for roseofungin against gamma-CD with an affinity value of -42.98 kcal/mol. The proposed binding mode of roseofungin against alpha-CD showed unusual interaction with an affinity value of -41.80 kcal/mol. Also, roseofungin bonded to beta-CD with a binding affinity value of -35.03 kcal/mol. The antiradical and cytotoxic activities of roseofungin and its obtained alpha-, beta- and gamma-cyclodextrin 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.
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Key words
roseofungin, cyclodextrin, in silico, molecular docking, complexation, antiradical activity, cytotoxicity
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