Abstract
A collection of both commercial and non-commercial galloyl derivatives (either isolated from plants or synthesized) was examined for an in vitro structure-activity relationship (SAR) screening of their anti-yeast activity. Most of the compounds exhibited an antimycotic activity when used together with amphotericin B (AMB) and none when used alone. The SAR study indicated the presence of two galloyl moieties in adjacent position as an important structural characteristic. In fact, among the compounds tested, 2,3-O-digalloyl-O-methylglucose and 2,3-O-digalloyl-Omethylmannose exhibited a synergistic interaction with AMB against a set of Candida albicans, Candida glabrata and Pichia kudriavzevii strains. A similar biological activity has also been observed for epigallocatechin gallate (EGCG). The high structural similarity between the two digalloyl derivatives and EGCG was advocated as possible rationale to explain their synergy with AMB.
Keywords: Anti-yeast activity, FIC, gallic acid, glucogalloy derivatives, MIC, SAR, synergy.
The Natural Products Journal
Title:In Vitro Synergistic Anti-yeast Activity between Galloyl Derivatives and Amphotericin B
Volume: 3 Issue: 2
Author(s): Panagiotis Arapitsas, Benedetta Turchetti, Fabrizio Melani, Daniela Tacconi, Cristina Nativi, Annalisa Romani, Stefano Menichetti and Pietro Buzzini
Affiliation:
Keywords: Anti-yeast activity, FIC, gallic acid, glucogalloy derivatives, MIC, SAR, synergy.
Abstract: A collection of both commercial and non-commercial galloyl derivatives (either isolated from plants or synthesized) was examined for an in vitro structure-activity relationship (SAR) screening of their anti-yeast activity. Most of the compounds exhibited an antimycotic activity when used together with amphotericin B (AMB) and none when used alone. The SAR study indicated the presence of two galloyl moieties in adjacent position as an important structural characteristic. In fact, among the compounds tested, 2,3-O-digalloyl-O-methylglucose and 2,3-O-digalloyl-Omethylmannose exhibited a synergistic interaction with AMB against a set of Candida albicans, Candida glabrata and Pichia kudriavzevii strains. A similar biological activity has also been observed for epigallocatechin gallate (EGCG). The high structural similarity between the two digalloyl derivatives and EGCG was advocated as possible rationale to explain their synergy with AMB.
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Arapitsas Panagiotis, Turchetti Benedetta, Melani Fabrizio, Tacconi Daniela, Nativi Cristina, Romani Annalisa, Menichetti Stefano and Buzzini Pietro, In Vitro Synergistic Anti-yeast Activity between Galloyl Derivatives and Amphotericin B, The Natural Products Journal 2013; 3 (2) . https://dx.doi.org/10.2174/2210315511303020008
DOI https://dx.doi.org/10.2174/2210315511303020008 |
Print ISSN 2210-3155 |
Publisher Name Bentham Science Publisher |
Online ISSN 2210-3163 |
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