PAPRSB Institute of Health Sciences, Universiti Brunei Darussalam, Jalan Tungku Link, Gadong BE1410, Brunei.
Molecules. 2022 Mar 14;27(6):1875. doi: 10.3390/molecules27061875.
Helminth infections continue to be a neglected global threat in tropical regions, and there have been growing cases of anthelmintic resistance reported towards the existing anthelmintic drugs. Thus, the search for a novel anthelmintic agent has been increasing, especially those derived from plants. (LL) is a leguminous plant that is known to have several pharmacological activities, including anthelmintic activity. It is widely known to contain a toxic compound called mimosine, which we believed could be a potential lead candidate that could exert a potent anthelmintic effect. Hence, this study aimed to validate the presence of mimosine in LL extract and to investigate the anthelmintic effect of LL extract and mimosine on head thrashing, egg-laying, and pharyngeal pumping activities using the animal model Mimosine content in LL extract was confirmed through an HPLC analysis of spiking LL extract with different mimosine concentrations, whereby an increasing trend in peak heights was observed at a retention time of 0.9 min. LL extract and mimosine caused a significant dose-dependent increase in the percentage of worm mortality, which produced LC50s of 73 mg/mL and 6.39 mg/mL, respectively. Exposure of to different concentrations of LL extract and mimosine significantly decreased the head thrashing, egg-laying, and mean pump amplitude of pharyngeal pumping activity. We speculated that these behavioral changes are due to the inhibitory effect of LL extract and mimosine on an L-type calcium channel called EGL-19. Our findings provide evidential support for the potential of LL extract and its active compound, mimosine, as novel anthelmintic candidates. However, the underlying mechanism of the anthelmintic action has yet to be elucidated.
寄生虫感染仍然是热带地区被忽视的全球威胁，并且已经有越来越多的驱虫药耐药报告。因此，人们对新型驱虫药的需求不断增加，尤其是来自植物的驱虫药。（LL）是一种豆科植物，已知具有多种药理活性，包括驱虫活性。它被广泛认为含有一种叫做含羞草素的有毒化合物，我们认为它可能是一种有潜力的先导候选药物，可以发挥强大的驱虫作用。因此，本研究旨在验证 LL 提取物中含羞草素的存在，并通过动物模型研究 LL 提取物和含羞草素对头摆动、产卵和咽部抽吸活动的驱虫作用。通过用不同浓度的含羞草素对 LL 提取物进行 HPLC 分析，证实了 LL 提取物中含羞草素的存在，观察到在保留时间为 0.9 分钟时，峰高呈上升趋势。LL 提取物和含羞草素导致虫体死亡率呈显著的剂量依赖性增加，分别产生 LC50 值为 73 mg/mL 和 6.39 mg/mL。暴露于不同浓度的 LL 提取物和含羞草素显著降低了头摆动、产卵和咽部抽吸活动的平均泵幅度。我们推测这些行为变化是由于 LL 提取物和含羞草素对称为 EGL-19 的 L 型钙通道的抑制作用所致。我们的研究结果为 LL 提取物及其活性化合物含羞草素作为新型驱虫候选药物提供了证据支持。然而，驱虫作用的潜在机制仍有待阐明。
