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6-蔗糖单酯糖脂作为新型抗真菌剂的合成及生物学评价

Synthesis and Biological Evaluation of 6--Sucrose Monoester Glycolipids as Possible New Antifungal Agents.

作者信息

Verboni Michele, Sisti Maurizio, Campana Raffaella, Benedetti Serena, Palma Francesco, Potenza Lucia, Lucarini Simone, Duranti Andrea

机构信息

Department of Biomolecular Sciences, University of Urbino Carlo Bo, 61029 Urbino, PU, Italy.

出版信息

Pharmaceuticals (Basel). 2023 Jan 17;16(2):136. doi: 10.3390/ph16020136.

DOI:10.3390/ph16020136
PMID:37259288
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9966131/
Abstract

A small library of 6--sucrose monoester surfactants has been synthesized and tested against various microorganisms. The synthetic procedure involved a modified Mitsunobu reaction, which showed improved results compared to those present in the literature (higher yields and larger scope). The antifungal activities of most of these glycolipids were satisfactory. In particular, sucrose palmitoleate (URB1537) showed good activity against Candida albicans ATCC 10231, spp., and IDRAH01 (MIC value: 16, 32, 64 µg/mL, respectively), and was further characterized through radical scavenging, anti-inflammatory, and biocompatibility tests. URB1537 has been shown to control the inflammatory response and to have a safe profile.

摘要

已合成了一个包含6种蔗糖单酯表面活性剂的小型文库，并针对各种微生物进行了测试。合成过程涉及改良的光延反应，与文献中的结果相比，该反应显示出更好的效果（更高的产率和更大的适用范围）。这些糖脂中的大多数具有令人满意的抗真菌活性。特别是，蔗糖棕榈油酸酯（URB1537）对白色念珠菌ATCC 10231、 spp.和IDRAH01表现出良好的活性（MIC值分别为16、32、64 µg/mL），并通过自由基清除、抗炎和生物相容性测试进一步表征。URB1537已被证明可控制炎症反应并具有安全的特性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/039e/9966131/0d2e772d5221/pharmaceuticals-16-00136-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/039e/9966131/2e24d64f6b72/pharmaceuticals-16-00136-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/039e/9966131/8b3b89d24b09/pharmaceuticals-16-00136-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/039e/9966131/7285dc3890f3/pharmaceuticals-16-00136-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/039e/9966131/2c34e98d239c/pharmaceuticals-16-00136-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/039e/9966131/38271804381d/pharmaceuticals-16-00136-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/039e/9966131/1a4a2d3c9b3a/pharmaceuticals-16-00136-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/039e/9966131/0d2e772d5221/pharmaceuticals-16-00136-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/039e/9966131/2e24d64f6b72/pharmaceuticals-16-00136-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/039e/9966131/8b3b89d24b09/pharmaceuticals-16-00136-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/039e/9966131/7285dc3890f3/pharmaceuticals-16-00136-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/039e/9966131/2c34e98d239c/pharmaceuticals-16-00136-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/039e/9966131/38271804381d/pharmaceuticals-16-00136-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/039e/9966131/1a4a2d3c9b3a/pharmaceuticals-16-00136-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/039e/9966131/0d2e772d5221/pharmaceuticals-16-00136-g005.jpg

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