Recio-Balsells Alejandro, Ristau Eugenia Rodriguez, Pacciaroni Adriana, Nicotra Viviana, Casero Carina, García Manuela
Instituto Multidisciplinario de Biología Vegetal (IMBIV), Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET), Córdoba, Argentina.
Facultad de Ciencias Químicas, Universidad Nacional de Córdoba (UNC), Ciudad Universitaria, X5000HUA, Córdoba, Argentina.
Nat Prod Bioprospect. 2025 May 8;15(1):28. doi: 10.1007/s13659-025-00513-y.
Antimicrobial resistance is one of the most pressing global health challenges, as many pathogens are rapidly evolving to evade existing treatments. Despite this urgent need for new solutions, natural plant-derived compounds remain relatively underexplored in the development of antimicrobial drugs. This report highlights an innovative approach to discovering potent antimicrobial agents through bioguided fractionation of numerous plant species from the rich Argentinean flora. By systematically screening 60 species (over 177 extracts) for antimicrobial activity against representative strains of gram-positive and gram-negative bacteria, we identified promising bioactive compounds within the Asteraceae family-particularly sesquiterpene lactones from the Xanthium genus. Building on this basis, we synthesized semi-synthetic derivatives by chemically modifying plant sub-extracts, focusing on structures incorporating heteroatoms and/or heterocycles containing oxygen and nitrogen (important for the bioavailability and bioactivity that they are capable of providing). These modifications were evaluated for their potential to enhance antimicrobial efficacy against bacteria and Candida species, including resistant strains. Our findings suggest that tailoring natural metabolites from Xanthium and related Asteraceae species can significantly improve their antimicrobial properties. This strategy offers a promising pathway for the development of novel therapeutic agents to combat bacterial and fungal infections in an era of rising drug resistance.
抗菌耐药性是全球最紧迫的健康挑战之一，因为许多病原体正在迅速进化以逃避现有治疗方法。尽管迫切需要新的解决方案，但在抗菌药物开发中，天然植物衍生化合物仍相对未得到充分探索。本报告重点介绍了一种创新方法，即通过对阿根廷丰富植物群中的众多植物物种进行生物导向分级分离来发现强效抗菌剂。通过系统筛选60种植物（超过177种提取物）对革兰氏阳性和革兰氏阴性细菌代表性菌株的抗菌活性，我们在菊科中鉴定出了有前景的生物活性化合物，特别是来自苍耳属的倍半萜内酯。在此基础上，我们通过化学修饰植物亚提取物合成了半合成衍生物，重点关注含有杂原子和/或含氧和氮的杂环的结构（这对它们能够提供的生物利用度和生物活性很重要）。评估了这些修饰增强对细菌和念珠菌物种（包括耐药菌株）抗菌效力的潜力。我们的研究结果表明，对苍耳属及相关菊科物种的天然代谢产物进行定制可以显著改善其抗菌性能。在耐药性不断上升的时代，这一策略为开发新型治疗剂以对抗细菌和真菌感染提供了一条有前景的途径。
