Bioassay-Guided Isolation of Broad-Spectrum Fungicidal Active Compound from <i>Artemisia ordosica</i>

• Main Authors: Gaijuan Tang, Shuyu Yang, Wenqiong Hu, Jingyi Jiang, He Yan, Juntao Feng, Chao Zhang, Yonghong Wang
• Format: Article
• Language: English
• Published: MDPI AG 2021-09-01
• Series: Metabolites
• Subjects: <i>Artemisia ordosica</i>; natural products; trans-dehydromatricaria ester; broad-spectrum; botanical fungicides
• Online Access: https://www.mdpi.com/2218-1989/11/9/629

To avoid the widespread resistance of commercial fungicides, new broad-spectrum botanical fungicides need to be developed. In previous bioactive screening assays, extracts of <i>Artemisia ordosica</i> Krasch. (<i>A. ordosica</i>) had highly antifungal activities, but the responsible phytochemicals were unidentified. In this study, active compounds of <i>A. ordosica</i> extracts were identified using a bioassay-guided method, and antifungal assays were performed in vitro and in vivo. The bioactive compounds were dissolved in petroleum ether, and the best antifungal fraction contained four compounds: trans-dehydromatricaria ester (TDDE), 7, 4-demetylnringenin, capillarin, and stearic acid. Among them, TDDE exhibited the highest antifungal activity against six pathogenic fungi and five bacteria. It exhibited significant fungicidal activity against <i>Thanatephorus cucumeris</i> and <i>Botrytis cinerea</i> with EC₅₀ values of 0.464 μg/mL and 1.4 μg/mL, respectively. The living tissue bioassay results showed that the relative protection effects (RPE) of TDDE on tomato leaves, tomato fruit, and strawberry leaves infected with <i>B. cinerea</i> reached 76.78%, 86.2%, and 80.89%, respectively. In pot experiments, the RPE on tomato and strawberry plants infected with <i>B. cinerea</i> reached 84.11% and 96.37%, respectively. Morphological and physiological examination showed that TDDE had significant inhibitory effects on mycelial growth, including increased top offshoot, contorted hyphal tips, and extravasated cytochylema. Meanwhile, bactericidal activities of TDDE were significantly higher than kanamycin and streptomycin in five bacteria, and the plant tissue experiments further demonstrated that it had an 88.31% RPE on walnut leaves infected with <i>Xanthomonas campestris</i> pv. <i>jugiandis</i>, 72.18% RPE on potato infected with <i>Erwinia carotovora</i> subsp. <i>carotovora</i>, and 82.50% RPE on kiwifruit branches infected with <i>Pseudomonas syringae</i> pv. <i>actinidiae</i>. The active compounds isolated from <i>A. ordosica</i> in this study show great potential value for developing broad-spectrum fungicides, and also provide an important way to identify and isolate new bioactive products from medicinal plants.