Essid Rym, Kefi Sarra, Damergi Bilel, Abid Ghassen, Fares Nadia, Jallouli Selim, Tabbene Olfa, Limam Ferid
Laboratory of Bioactive Substances, Biotechnology Center in Borj-Cedria Technopole, BP 901, 2050, Hammam-Lif, Tunisia.
University of Tunis-El Manar, Campus Universitaire Farhat Hached, BP-94 Rommana, 1068, Tunis, Tunisia.
Int Microbiol. 2025 Apr;28(4):837-849. doi: 10.1007/s10123-024-00567-x. Epub 2024 Aug 31.
In the present study, we assessed the antioxidant and antileishmanial potential from fresh leaves of Ballota (B.) hirsuta essential oil (EO). The GC-MS analysis of B. hirsuta EO revealed that spathulenol and germacrene D were the main components accounting for 26.03% and 19.64% of the total EO, respectively. B. hirsuta EO possesses moderate antioxidant activity, both in neutralizing DPPH radicals and in inhibiting β-carotene bleaching. In addition, it exhibits both high antileishmanial activity and selectivity towards the promastigote and amastigote forms. Specifically, B. hirsuta EO showed an IC value of 20.78 µg/mL and 23.62 µg/mL, against the promastigote and amastigote forms of L. infantum, respectively. It also demonstrated an IC value of 22.39 and 25.76 µg/mL, against the promastigote and amastigote forms of L. major, respectively. However, it exhibited moderate cytotoxicity, with a selectivity index below 10. The investigation of the molecular mechanism of action revealed that B. hirsuta EO inhibited only the sterol pathway, including CYP51 gene expression. Additionally, in silico analysis indicated that the main compounds of B. hirsuta EO, germacrene and spathulenol, exhibited excellent affinity energy against Leishmania enzymes trypanothione reductase (TryR) and trypanothione synthase (TryS). This denotes the potential of these compounds as promising agents to control leishmaniasis.
在本研究中，我们评估了绵毛水苏（Ballota (B.) hirsuta）新鲜叶片精油（EO）的抗氧化和抗利什曼原虫潜力。绵毛水苏EO的气相色谱 - 质谱分析表明，匙叶桉油烯醇和杜松烯D是主要成分，分别占总EO的26.03%和19.64%。绵毛水苏EO在中和DPPH自由基和抑制β - 胡萝卜素漂白方面均具有中等抗氧化活性。此外，它对前鞭毛体和无鞭毛体形式均表现出高抗利什曼原虫活性和选择性。具体而言，绵毛水苏EO对婴儿利什曼原虫的前鞭毛体和无鞭毛体形式的IC值分别为20.78μg/mL和23.62μg/mL。它对硕大利什曼原虫的前鞭毛体和无鞭毛体形式的IC值分别为22.39和25.76μg/mL。然而，它表现出中等细胞毒性，选择性指数低于10。作用分子机制的研究表明，绵毛水苏EO仅抑制固醇途径，包括CYP51基因表达。此外，计算机模拟分析表明，绵毛水苏EO的主要化合物杜松烯和匙叶桉油烯醇对利什曼原虫酶硫氧还蛋白还原酶（TryR）和硫氧还蛋白合酶（TryS）表现出优异的亲和能。这表明这些化合物作为控制利什曼病的有前景药物的潜力。
