Moreira Rute, Ferreres Federico, Gil-Izquierdo Ángel, Gomes Nelson G M, Araújo Luísa, Pinto Eugénia, Andrade Paula B, Videira Romeu A
REQUIMTE/LAQV, Laboratório de Farmacognosia, Departamento de Química, Faculdade de Farmácia, Universidade do Porto, 4050-313 Porto, Portugal.
Molecular Recognition and Encapsulation (REM) Group, Department of Food Technology and Nutrition, Universidad Católica de Murcia, 30107 Murcia, Spain.
Antibiotics (Basel). 2023 May 8;12(5):869. doi: 10.3390/antibiotics12050869.
Pest resistance against fungicides is a widespread and increasing problem, with impact on crop production and public health, making the development of new fungicides an urgent need. Chemical analyses of a crude methanol extract (CME) of leaves revealed the presence of sugars, phospholipids, phytosterols, guieranone A, porphyrin-containing compounds, and phenolics. To connect chemical composition with biological effects, solid-phase extraction was used to discard water-soluble compounds with low affinity for the C18 matrix and obtain an ethyl acetate fraction (EAF) that concentrates guieranone A and chlorophylls, and a methanol fraction (MF) dominated by phenolics. While the CME and MF exhibited poor antifungal activity against , and , the EAF demonstrated antifungal activity against these filamentous fungi, particularly against . Studies with yeasts revealed that the EAF has strong effectiveness against , and with MICs of 8, 8 and 16 μg/mL, respectively. A combination of in vivo and in vitro studies shows that the EAF can function as a mitochondrial toxin, compromising complexes I and II activities, and as a strong inhibitor of fungal tyrosinase (Ki = 14.40 ± 4.49 µg/mL). Thus, EAF appears to be a promising candidate for the development of new multi-target fungicides.
害虫对杀菌剂的抗性是一个普遍且日益严重的问题，对作物生产和公共卫生都有影响，这使得开发新型杀菌剂成为当务之急。对叶片粗甲醇提取物（CME）的化学分析表明，其中存在糖类、磷脂、植物甾醇、桂兰酮A、含卟啉化合物和酚类物质。为了将化学成分与生物效应联系起来，采用固相萃取法去除对C18基质亲和力低的水溶性化合物，得到富集桂兰酮A和叶绿素的乙酸乙酯馏分（EAF）以及以酚类物质为主的甲醇馏分（MF）。虽然CME和MF对[此处原文缺失真菌名称]、[此处原文缺失真菌名称]和[此处原文缺失真菌名称]的抗真菌活性较差，但EAF对这些丝状真菌表现出抗真菌活性，尤其是对[此处原文缺失真菌名称]。对酵母的研究表明，EAF对[此处原文缺失酵母名称]、[此处原文缺失酵母名称]和[此处原文缺失酵母名称]具有很强的效果，其最低抑菌浓度（MIC）分别为8、8和16μg/mL。体内和体外研究相结合表明，EAF可作为线粒体毒素，损害复合物I和II的活性，并作为真菌酪氨酸酶的强抑制剂（抑制常数Ki = 14.40 ± 4.49 µg/mL）。因此，EAF似乎是开发新型多靶点杀菌剂的一个有前景的候选物。
