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Antifungal Activity in Compounds from the Australian Desert Plant Eremophila alternifolia with Potency Against Cryptococcus spp.

机译:来自澳大利亚沙漠植物互花米草的化合物中的抗真菌活性对隐球菌具有潜在作用。

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摘要

Plant metabolites that have shown activity against bacteria and/or environmental fungi represent valuable leads for the identification and development of novel drugs against clinically important human pathogenic fungi. Plants from the genus Eremophila were highly valued in traditional Australian Aboriginal medicinal practices, and E. alternifolia was the most prized among them. As antibacterial activity of extracts from E. alternifolia has been documented, this study addresses the question whether there is also activity against infectious fungal human pathogens. Compounds from leaf-extracts were purified and identified by 1- and 2-D NMR. These were then tested by disk diffusion and broth microdilution assays against ten clinically and environmentally relevant yeast and mould species. The most potent activity was observed with the diterpene compound, 8,19-dihydroxyserrulat-14-ene against Cryptococcus gattii and Cryptococcus neoformans, with minimum inhibition concentrations (MIC) comparable to those of Amphotericin B. This compound also exhibited activity against six Candida species. Combined with previous studies showing an antibacterial effect, this finding could explain a broad antimicrobial effect from Eremophila extracts in their traditional medicinal usage. The discovery of potent antifungal compounds from Eremophila extracts is a promising development in the search for desperately needed antifungal compounds particularly for Cryptococcus infections.
机译:已显示出对细菌和/或环境真菌具有活性的植物代谢产物,是鉴定和开发针对临床上重要的人类致病性真菌的新药的宝贵线索。来自Ermophila属的植物在澳大利亚的传统土著医学实践中享有很高的价值,而E. alternifolia在其中尤为珍贵。由于已经记录了互花米草的提取物的抗菌活性,因此本研究解决了是否还具有针对人的传染性真菌病原体的活性的问题。纯化叶提取物中的化合物,并通过一维和二维NMR进行鉴定。然后通过圆盘扩散法和肉汤微量稀释法对10种临床和环境相关的酵母和霉菌进行测试。观察到最有效的活性是二萜化合物8,19-dihydroxyserrulat-14-ene对加氏隐球菌和新隐隐球菌的抑制作用,其最小抑菌浓度(MIC)与两性霉素B相当。该化合物还对六种念珠菌具有活性。 。结合先前的研究显示抗菌作用,该发现可以解释传统方法将血友病提取物的广泛抗菌作用。从嗜血杆菌提取物中发现有效的抗真菌化合物,对于寻找急需的抗真菌化合物,尤其是对于隐球菌感染的抗真菌化合物而言,是一个有前途的发展。

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