Bioassay-guided isolation of three anthelmintic compounds from Warburgia ugandensis Sprague subspecies ugandensis, and the mechanism of action of polygodial

Liu, Maoxuan; Kipanga, Purity N.; Hung, Anh; Dhondt, Ineke; Braeckman, Bart P.; Borggraeve, Wim M. De; Luyten, Walter

doi:10.1016/j.ijpara.2017.11.009

Cited by 23 publications

(27 citation statements)

References 72 publications

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“…Trichostrongylus colubriformis in vitro (Lorimer et al, 1996). In our recent study, we found polygodial to exhibit potent anthelmintic activity against C. elegans with an EC 50 of 13.1 ± 5.3 μM, and its α,β-unsaturated 1,4-dialdehyde moiety is essential for that activity (Liu et al, 2018). Considering that miogadial has a similar structure to polygodial and possesses an α,β-unsaturated 1,4-dialdehyde moiety as well, its anthelmintic activity is consistent with our previous findings.…”

Section: Bioassay-guided Purification and Structure Elucidation Of Acmentioning

confidence: 95%

Bioassay-guided isolation of active substances from Semen Torreyae identifies two new anthelmintic compounds with novel mechanism of action

Liu

Veryser

et al. 2018

Journal of Ethnopharmacology

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We identified the bioactive compounds from Semen Torreyae responsible for its anthelmintic activity: galangal acetate and miogadial. The two anthelmintic compounds demonstrated a synergistic effect against C. elegans. Galangal acetate and miogadial are unlikely to act on the targets of currently-used anthelmintics (ivermectin, levamisole, benomyl and aldicarb), and an action on TRP channels appears to be ruled out as well. In summary, galangal acetate and miogadial are promising anthelmintic hits worth further investigation.

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Section: Bioassay-guided Purification and Structure Elucidation Of Acmentioning

confidence: 95%

Bioassay-guided isolation of active substances from Semen Torreyae identifies two new anthelmintic compounds with novel mechanism of action

Liu

Veryser

et al. 2018

Journal of Ethnopharmacology

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“…Liu et al [98] A checkerboard assay suggested that warburganal and polygodial both act synergistically with alpha-linolenic acid. A study of the structure-activity relationship for polygodial showed that the α,β-unsaturated 1,4-dialdehyde structural motif is essential for the anthelmintic activity.…”

Section: Natural Products Active Against C Elegansmentioning

confidence: 99%

“…In a few cases, synergy was reported between bioactive compounds isolated from the same plant [98,99,109]. Such synergies appear common in medicinal plants and may explain the relatively low potency of individual phytoconstituents [110].…”

Section: Synergymentioning

confidence: 99%

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Plant-Based Natural Products for the Discovery and Development of Novel Anthelmintics against Nematodes

2020

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Intestinal parasitic nematodes infect approximately two billion people worldwide. In the absence of vaccines for human intestinal nematodes, control of infections currently relies mainly on chemotherapy, but resistance is an increasing problem. Thus, there is an urgent need for the discovery and development of new anthelmintic drugs, especially ones with novel mechanisms of action. Medicinal plants hold great promise as a source of effective treatments, including anthelmintic therapy. They have been used traditionally for centuries and are mostly safe (if not, their toxicity is well-known). However, in most medicinal plants the compounds active against nematodes have not been identified thus far. The free-living nematode C. elegans was demonstrated to be an excellent model system for the discovery of new anthelmintics and for characterizing their mechanism of action or resistance. The compounds discussed in this review are of botanical origin and were published since 2002. Most of them need further studies of their toxicity, mechanisms and structure-activity relationship to assess more fully their potential as drugs.

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“…The antiparasitic mechanisms of linoleic acid are not clear. "It has been suggested that the nematicidal activity of fatty acids is due to adverse interference with the nematode cuticle or hypodermis via a detergent (solubilization) effect, or through direct interaction of the fatty acids with the lipophilic regions of target plasma membranes" [40,41]. Linoleic acid can affect ionotropic neurotransmitter receptors, like gamma-aminobutyric acid (GABA) and N-methyl-D-aspartate (NMDA) receptors [42], which are targets of some common anthelmintics.…”

Section: Mechanism Of Action Of Linoleic Acidmentioning

confidence: 99%

Nematicidal Activity of Holigarna caustica (Dennst.) Oken Fruit Is Due to Linoleic Acid

et al. 2020

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Holigarna caustica (Dennst.) Oken is used by the tribes of Northeast India for the treatment of intestinal problems. Therefore, the present study was undertaken to investigate the active principles of this plant responsible for its anthelmintic activity, using bioassay-guided fractionation. An ethanol extract of H. caustica fruit was fractionated on a silica gel column, followed by HPLC, while nematicidal activity was followed throughout on Caenorhabditis (C.) elegans as a model organism. Our study constitutes the first nematicidal report for this plant. Bioassay-guided purification led to the isolation of one compound (IC50 = 0.4 µM) as the only active constituent in the most active fraction. The compound was identified as linoleic acid based on spectroscopic data (1H and 13C NMR and ESI-MS). No cytotoxicity was observed in the crude extract or in linoleic acid (up to 356 µM). The results support the use of H. caustica for the treatment of intestinal problems by traditional healers in India.

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Bioassay-guided isolation of three anthelmintic compounds from Warburgia ugandensis Sprague subspecies ugandensis, and the mechanism of action of polygodial

Cited by 23 publications

References 72 publications

Bioassay-guided isolation of active substances from Semen Torreyae identifies two new anthelmintic compounds with novel mechanism of action

Bioassay-guided isolation of active substances from Semen Torreyae identifies two new anthelmintic compounds with novel mechanism of action

Plant-Based Natural Products for the Discovery and Development of Novel Anthelmintics against Nematodes

Nematicidal Activity of Holigarna caustica (Dennst.) Oken Fruit Is Due to Linoleic Acid

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