Falcone Giuseppe, Di Matteo Giacomo, Mannina Luisa, Cellini Francesco, Menghini Luigi, Carradori Simone, Al-Samydai Ali, Chiavaroli Annalisa, Di Simone Simonetta Cristina, Ferrante Claudio
Department of Pharmacy, "G. d'Annunzio" University of Chieti-Pescara, via dei Vestini 31, 66100 Chieti, Italy.
Department of Chemistry and Technology of Drugs, Food Chemistry Lab, Sapienza Università di Roma, Piazzale Aldo Moro 5, 00185 Rome, Italy; NMR-Based Metabolomics Laboratory (NMLab), Sapienza University of Rome, Piazzale Aldo Moro 5, 00185 Rome, Italy.
J Ethnopharmacol. 2025 Aug 14:120430. doi: 10.1016/j.jep.2025.120430.
Gentiana lutea L. is a mountain herb with a long-standing use in traditional European medicine, especially for digestive disorders and for its antiseptic and anti-inflammatory properties. Its roots are also traditionally used in the preparation of regional liqueurs, particularly in Central Italy.
This study aimed to characterize the phytochemical composition of Gentiana lutea roots from the Pollino National Park and assess the potential intestinal anti-inflammatory effects, using an ex vivo model, of an hydroalcoholic extract mimicking the traditional Italian Gentiana liqueur.
Roots were collected from the Pollino National Park, extracted and subjected to HPLC-DAD and NMR-based metabolomic analysis for complete phytochemical characterization. A Gentiana hydroalcoholic liqueur analogue was prepared, chemically characterized and its anti-inflammatory activity was evaluated ex vivo on LPS-stimulated murine colon tissue.
Phytochemical analyses revealed high levels of bioactive secoiridoids (gentiopicroside, swertiamarin, amarogentin, sweroside), iridoids (loganic acid), and xanthones (isogentisin). NMR metabolomics further identified sugars (sucrose predominant), organic acids (notably malate), amino acids (asparagine, glutamine, tyrosine, aspartate as major ones), and lipid components including β-sitosterol and various fatty acids. The Gentiana hydroalcoholic liqueur analogue retained relevant concentrations of swertiamarin, loganic acid, sweroside, and isogentisin, despite its milder extraction conditions. The hydroalcoholic extract significantly reduced LPS-induced expression of pro-inflammatory cytokines IL-6 and TNF-α, while upregulating IL-10 expression in colon tissues, suggesting a potent immunomodulatory effect.
These findings provide scientific support for the traditional use of Gentiana lutea roots in digestive health and highlight their potential as sources of functional phytocompounds for complementary strategies in gut inflammation management.
黄龙胆是一种生长在山区的草本植物，在传统欧洲医学中有着悠久的使用历史，尤其用于治疗消化系统疾病，因其具有抗菌和抗炎特性。其根部在传统上也用于制备当地的利口酒，特别是在意大利中部地区。
本研究旨在对来自波利诺国家公园的黄龙胆根的植物化学成分进行表征，并使用体外模型评估模拟传统意大利黄龙胆利口酒的水醇提取物的潜在肠道抗炎作用。
从波利诺国家公园采集根部，进行提取，并通过HPLC-DAD和基于NMR的代谢组学分析进行完整的植物化学表征。制备了一种黄龙胆水醇利口酒类似物，对其进行化学表征，并在体外对脂多糖刺激的小鼠结肠组织评估其抗炎活性。
植物化学分析显示含有高水平的生物活性裂环环烯醚萜类（龙胆苦苷、獐牙菜苦苷、苦味质、獐牙菜苷）、环烯醚萜类（马钱子酸）和呫吨酮类（异秦皮素）。NMR代谢组学进一步鉴定出糖类（以蔗糖为主）、有机酸（特别是苹果酸）、氨基酸（主要是天冬酰胺、谷氨酰胺、酪氨酸、天冬氨酸）以及脂质成分，包括β-谷甾醇和各种脂肪酸。尽管提取条件较为温和，但黄龙胆水醇利口酒类似物仍保留了獐牙菜苦苷、马钱子酸、獐牙菜苷和异秦皮素的相关浓度。水醇提取物显著降低了脂多糖诱导的促炎细胞因子IL-6和TNF-α的表达，同时上调了结肠组织中IL-10的表达，表明其具有强大的免疫调节作用。
这些发现为黄龙胆根在消化健康方面的传统用途提供了科学支持，并突出了其作为功能性植物化合物来源在肠道炎症管理补充策略中的潜力。
