Section of Parasitology, Department of Zoology, Aligarh Muslim University, Aligarh, Uttar Pradesh, 202002, India.
College of Medicine, Gachon University, Incheon, South Korea.
Exp Parasitol. 2022 Dec;243:108421. doi: 10.1016/j.exppara.2022.108421. Epub 2022 Nov 2.
Recent research on the emergence of parasitic resistance to commonly prescribed anthelmintics has sparked a greater interest in finding novel therapeutic molecules, including those derived from plants. The use of medicinal plants and their derivatives has been viewed as an alternative source of anti-parasitic compounds and as being safe in comparison to synthetic medications due to the absence of adverse effects, ease of accessibility, and little to no expense. Consequently, in the current study, thymoquinone (TQ), an active component of Nigella sativa (Black cumin), has been tested to see their effect on the activity of some important parameters of Gigantocotyle explanatum worms, including Gamma-glutamyl Transpeptidase (GGT), glutathione (GSH), Glutathione-S-Transferase (GST), Superoxide dismutase (NO). Additionally, various other survival indicators are also used, such as assays for motility, tegument damage, and DNA fragmentation. G. explanatum adult flukes were in vitro treated to thymoquinone at various concentrations for 3 h at 37 °C. Even though all of the worms were still alive after 3 h of exposure, there was a substantial (p < 0.05) reduction in worm motility at a concentration of 90 M. There were pronounced tegumental disturbances, a loss of surface annulations, and erosion in the papillae posterior region and around the acetabulum. A significant (p < 0.05) decrease in glutathione-S-transferase and superoxide dismutase activity and reduced glutathione (GSH) level was observed. A significant inhibition of Gamma-glutamyl Transpeptidase (GGT) in thymoquinone treated worms was also evident. Thymoquinone and GGT also displayed a high interaction during in silico molecular docking, suggesting that this combination may be more effective at inhibiting the antioxidant enzymes of G. explanatum. The present findings suggest that thymoquinone would reduce the worm capacity for detoxification, while GGT inhibition would have a major impact on their ability to transport amino acids across the tegument. Thymoquinone thus seemed to be a promising anthelmintic compound for future investigations.
最近对常见驱虫药出现寄生虫耐药性的研究引起了人们对寻找新型治疗分子的更大兴趣，包括源自植物的分子。由于没有不良反应、易于获得且几乎没有费用，药用植物及其衍生物的使用被视为抗寄生虫化合物的替代来源，并且与合成药物相比是安全的。因此，在目前的研究中，测试了来自黑孜然（黑孜然）的活性成分百里醌（TQ）对巨睾吸虫（Gigantocotyle explanatum）蠕虫一些重要参数活性的影响，包括γ-谷氨酰转肽酶（GGT）、谷胱甘肽（GSH）、谷胱甘肽-S-转移酶（GST）、超氧化物歧化酶（NO）。此外，还使用了各种其他生存指标，例如运动性、外皮损伤和 DNA 片段化测定。将巨睾吸虫成虫在 37°C 下用不同浓度的百里醌处理 3 小时进行体外处理。尽管暴露 3 小时后所有蠕虫仍存活，但在 90μM 浓度下，蠕虫运动性显著降低（p<0.05）。明显的外皮干扰，表面环纹丧失，后区乳头和髋臼周围侵蚀。谷胱甘肽-S-转移酶和超氧化物歧化酶活性以及还原型谷胱甘肽（GSH）水平显著降低（p<0.05）。在百里醌处理的蠕虫中也明显抑制了γ-谷氨酰转肽酶（GGT）。百里醌和 GGT 在计算机分子对接中也表现出很高的相互作用，这表明这种组合可能更有效地抑制巨睾吸虫的抗氧化酶。本研究结果表明，百里醌会降低蠕虫的解毒能力，而 GGT 抑制会对其穿过外皮运输氨基酸的能力产生重大影响。因此，百里醌似乎是一种有前途的驱虫化合物，值得进一步研究。
