Kumarasingha Rasika, Karpe Avinash V, Preston Sarah, Yeo Tiong-Chia, Lim Diana S L, Tu Chu-Lee, Luu Jennii, Simpson Kaylene J, Shaw Jillian M, Gasser Robin B, Beale David J, Morrison Paul D, Palombo Enzo A, Boag Peter R
Development and Stem Cells Program, Monash Biomedicine Discovery Institute and Department of Biochemistry and Molecular Biology, Monash University, Melbourne, Victoria, 3800, Australia.
Department of Chemistry and Biotechnology, Faculty of Science, Engineering and Technology, Swinburne University of Technology, Hawthorn, 3122, Victoria, Australia; Land and Water, Commonwealth Scientific and Industrial Research Organization (CSIRO), Ecosciences Precinct, Dutton Park, 4102, Queensland, Australia.
Int J Parasitol Drugs Drug Resist. 2016 Dec;6(3):171-178. doi: 10.1016/j.ijpddr.2016.08.002. Epub 2016 Aug 26.
Anthelmintic resistance is widespread in gastrointestinal nematode populations, such that there is a consistent need to search for new anthelmintics. However, the cost of screening for new compounds is high and has a very low success rate. Using the knowledge of traditional healers from Borneo Rainforests (Sarawak, Malaysia), we have previously shown that some traditional medicinal plants are a rich source of potential new anthelmintic drug candidates. In this study, Picria fel-terrae Lour. plant extract, which has previously shown promising anthelmintic activities, was fractionated via the use of a solid phase extraction cartridge and each isolated fraction was then tested on free-living nematode Caenorhabditis elegans and the parasitic nematode Haemonchus contortus. We found that a single fraction was enriched for nematocidal activity, killing ≥90% of C. elegans adults and inhibiting the motility of exsheathed L3 of H. contortus, while having minimal cytotoxic activity in mammalian cell culture. Metabolic profiling and chemometric analysis of the effective fraction indicated medium chained fatty acids and phenolic acids were highly represented.
抗蠕虫药耐药性在胃肠道线虫种群中广泛存在，因此一直需要寻找新的抗蠕虫药。然而，新化合物的筛选成本很高，且成功率极低。利用来自婆罗洲雨林（马来西亚砂拉越）传统治疗师的知识，我们之前已表明一些传统药用植物是潜在新抗蠕虫药候选物的丰富来源。在本研究中，先前已显示出有前景的抗蠕虫活性的地锦苗（Picria fel-terrae Lour.）植物提取物，通过使用固相萃取柱进行分离，然后对每个分离的组分在自由生活线虫秀丽隐杆线虫和寄生线虫捻转血矛线虫上进行测试。我们发现有一个单一的组分富含杀线虫活性，能杀死≥90%的秀丽隐杆线虫成虫，并抑制捻转血矛线虫脱鞘L3的运动，同时在哺乳动物细胞培养中具有最小的细胞毒性活性。有效组分的代谢谱分析和化学计量分析表明，中链脂肪酸和酚酸高度富集。
