title: Identification of lead chemotherapeutic agents from medicinal plants against blood flukes and whipworms.
abstract: Schistosomiasis and trichuriasis are two of the most common neglected tropical diseases (NTD) that affect almost a billion people worldwide. There is only a limited number of effective drugs to combat these NTD. Medicinal plants are a viable source of parasiticides. In this study, we have investigated six of the 19 phytochemicals isolated from two Bhutanese medicinal plants, Corydalis crispa and Pleurospermum amabile, for their anthelmintic properties. We used the xWORM technique and Scanning Electron Microscope-based imaging to determine the activity of the compounds. Of the six compounds tested, isomyristicin and bergapten showed significant anthelmintic activity against Schistosoma mansoni and Trichuris muris with bergapten being the most efficacious compound one against both parasites (S. mansoni IC50 = 8.6 μg/mL and T. muris IC50 = 10.6 μg/mL) and also against the schistosomulum stage of S. mansoni. These two compounds induced tegumental damage to S. mansoni and affected the cuticle, bacillary bands and bacillary glands of T. muris. The efficacy against multiple phylogenetically distinct parasites and different life stages, especially the schistosomulum where praziquantel is ineffective, makes isomyristicin and bergapten novel scaffolds for broad-spectrum anthelmintic drug development that could be used for the control of helminths infecting humans and animals.
authors: Centre for Biodiscovery and Molecular Development of Therapeutics, Australian Institute of Tropical Health and Medicine, James Cook University, Cairns, QLD, Australia.
authors: Phurpa
authors: P
authors: Wangchuk
authors: Centre for Biodiscovery and Molecular Development of Therapeutics, Australian Institute of Tropical Health and Medicine, James Cook University, Cairns, QLD, Australia.
authors: Paul R
authors: PR
authors: Giacomin
authors: Centre for Biodiscovery and Molecular Development of Therapeutics, Australian Institute of Tropical Health and Medicine, James Cook University, Cairns, QLD, Australia.
authors: Mark S
authors: MS
authors: Pearson
authors: Centre for Biodiscovery and Molecular Development of Therapeutics, Australian Institute of Tropical Health and Medicine, James Cook University, Cairns, QLD, Australia.
authors: Michael J
authors: MJ
authors: Smout
authors: Centre for Biodiscovery and Molecular Development of Therapeutics, Australian Institute of Tropical Health and Medicine, James Cook University, Cairns, QLD, Australia.
authors: Alex
authors: A
authors: Loukas
mesh_terms: D000470:Alkaloids / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D000818:Animals; D000871:Anthelmintics / Q000302:isolation & purification* / Q000494:pharmacology; D001631:Bhutan; D031311:Corydalis / Q000737:chemistry*; D055808:Drug Discovery; D005260:Female; D007546:Isoquinolines / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D019684:Magnoliopsida / Q000737:chemistry*; D008297:Male; D008519:Medicine, Traditional; D051379:Mice; D008855:Microscopy, Electron, Scanning; D015394:Molecular Structure; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D010946:Plants, Medicinal / Q000737:chemistry*; D012550:Schistosoma mansoni / Q000187:drug effects* / Q000254:growth & development / Q000648:ultrastructure; D014258:Trichuris / Q000187:drug effects* / Q000254:growth & development
chemical_list: D000470:Alkaloids; D000871:Anthelmintics; D007546:Isoquinolines; D010936:Plant Extracts