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http://ntour.ntou.edu.tw:8080/ir/handle/987654321/37531
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| Title: | Use of Cilofungin as Direct Fluorescent Probe for Monitoring Antifungal Drug-Membrane Interactions |
| Authors: | YUAN-TIH KO;BRUCE P. WASSERMAN';RICHARD D. LUDESCHER;DAVID J. FROST |
| Contributors: | 國立臺灣海洋大學:食品科學系 |
| Date: | 1994-06
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| Issue Date: | 2016-03-14T01:39:22Z
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| Publisher: | American Society for Microbiology |
| Abstract: | Abstract:Cilofungin is an antifungal cyclopeptide which inhibits cell wall (1,3)-p1-glucan biosynthesis in fungal
organisms, and its action against Candida albicans (1,3)-Il-glucan synthase has been widely studied. Since
glucan synthase inactivation is thought to partially result from perturbations of the membrane lipid
environment, the interaction of cilofungin with fungal membranes and phosphatidylcholine membrane vesicles
was studied. Cilofungin, which contains two independent aromatic groups, has an excitation maximum of 270
nm and an emission maximum of 317 nm in aqueous solution. Comparison of the fluorescence properties of
cilofungin with those of the analogs pneumocandin Bo, N-acetyl-tyrosinamide, and 4-hydroxybenzamide
indicated that the emission of cilofungin largely derived from the p-octyloxybenzamide side chain. Microsomal
membranes from Saccharomyces cerevisiae, C. albicans, and phosphatidylcholine membrane vesicles induced a
blue shift in the cilofungin emission spectrum and increased the cilofungin steady-state emission anisotropy,
providing direct evidence for a cilofungin-membrane interaction. Cilofungin interacted more strongly with
membranes of C. albicans than with those of S. cerevisiae, correlating with previous findings that C. albicans is
far more susceptible than S. cerevisiae to the action of cilofungin. These findings support the hypothesis that
drug-induced inhibition of the (1,3)-,B-glucan synthesis results from the perturbation of the membrane
environment and the interaction with the glucan synthase complex combined. The study demonstrated ways in
which the fluorescence properties of drugs can be used to directly evaluate drug-membrane interactions and
structure-activity relationships. |
| Relation: | 38(56),pp.1378-1385 |
| URI: | http://ntour.ntou.edu.tw:8080/ir/handle/987654321/37531 |
| Appears in Collections: | [食品科學系] 期刊論文
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