Sardi Janaina de Cássia Orlandi, Freires Irlan Almeida, Lazarini Josy Goldoni, Infante Juliana, de Alencar Severino Matias, Rosalen Pedro Luiz
Department of Physiological Sciences, Piracicaba Dental School, University of Campinas, Piracicaba, SP, Brazil.
Department of Agri-Food Industry, Food and Nutrition, "Luiz de Queiroz" College of Agriculture, University of São Paulo, Piracicaba, SP, Brazil.
Microb Pathog. 2017 Apr;105:280-287. doi: 10.1016/j.micpath.2017.02.044. Epub 2017 Mar 1.
Brazilian endemic fruit species have aroused attention due to their highly valuable, yet unexplored, agro-industrial, food and therapeutic potential. Herein, we describe the antifungal activity of four Eugenia spp. against Candida albicans biofilms, and further demonstrate insights into their potential mode(s) of action and toxicity in vitro and in vivo. Extracts from different parts (seeds, pulps, leaves) of E. leitonii (EL), E. brasiliensis (EB), E. myrcianthes (EM) and E. involucrata (EI) were obtained (S23°23',W45°39') and chemically characterized by GC/MS. The active extracts were tested against C. albicans biofilm viability and architecture, as well as mode of action, and toxicology using RAW 264.7 macrophages and Galleria mellonella larvae. The MIC values ranged from 15.62 to >2000 μg/mL. The most active extracts were EL (seed, 15.62 μg/mL) and EB (leaf and seeds, 31.25 and 15.62 μg/mL, respectively). Treatment with these extracts at 10xMIC reduced biofilm viability by 54-55% (P < 0.0001) as compared to 42% by nystatin. At 10xMIC, all extracts caused damages to biofilm architecture and integrity, and fewer hyphae remained attached to treated biofilms. None of them was found to interfere with cell wall biosynthesis or complexation with ergosterol. The extracts had low toxicity against macrophages in vitro (P > 0.05) and G. mellonella larvae, with mean in vivo LD of 1500 mg/kg (EL, seeds); 2500 mg/kg (EB, seeds); and 1250 mg/kg (EB, leaf). The phenolic compounds epicatechin and gallic acid were the major constituents in the extracts. Our findings may open avenues for the application of these yet unexplored native fruits in the food and pharmaceutical industry.
巴西本土水果物种因其具有高度价值但尚未得到充分探索的农业产业、食品和治疗潜力而引起了关注。在此，我们描述了四种番樱桃属植物对白色念珠菌生物膜的抗真菌活性，并进一步展示了它们在体外和体内潜在的作用方式及毒性的相关见解。从雷东氏番樱桃（EL）、巴西番樱桃（EB）、密花番樱桃（EM）和总苞番樱桃（EI）的不同部位（种子、果肉、叶子）提取（南纬23°23'，西经45°39'），并通过气相色谱/质谱联用仪进行化学表征。对活性提取物进行了针对白色念珠菌生物膜活力和结构、作用方式以及使用RAW 264.7巨噬细胞和大蜡螟幼虫进行毒理学测试。最低抑菌浓度值范围为15.62至>2000μg/mL。活性最强的提取物是雷东氏番樱桃种子提取物（15.62μg/mL）和巴西番樱桃叶提取物及种子提取物（分别为31.25和15.62μg/mL）。与制霉菌素使生物膜活力降低42%相比，用这些提取物以10倍最低抑菌浓度处理可使生物膜活力降低54 - 55%（P < 0.0001）。在10倍最低抑菌浓度下，所有提取物均对生物膜结构和完整性造成破坏，且处理后的生物膜上附着的菌丝较少。未发现它们中的任何一种会干扰细胞壁生物合成或与麦角固醇络合。这些提取物在体外对巨噬细胞（P > 0.05）和大蜡螟幼虫毒性较低，体内平均半数致死剂量分别为：雷东氏番樱桃种子提取物1500mg/kg；巴西番樱桃种子提取物2500mg/kg；巴西番樱桃叶提取物1250mg/kg。酚类化合物表儿茶素和没食子酸是提取物中的主要成分。我们的研究结果可能为这些尚未得到充分探索的本土水果在食品和制药行业的应用开辟道路。
