Anthelmintic

Forage chicory is grown as a bioactive anti-parasitic pasture crop, and bio-guided fractionation across five cultivars against Ascaris suum identified 8-DOL as the compound most strongly associated with anti-parasitic activity, with confirmation against Teladorsagia circumcincta and Cooperia oncophora.

The same paper concluded that it acts in synergistic combination with the other lactones rather than alone ^{4Reference 4Valente AH et al. · 2021Identification of compounds responsible for the anthelmintic effects of chicory (Cichorium intybus) by molecular networking and bio-guided fractionationView study →}.

Cultivar comparisons agree on the ranking: a DOL-dominant extract inhibited Hemonchus contortus egg hatch at EC₅₀ 2.6 mg/mL against 6.4 mg/mL for a lactucin-dominant one, with the authors noting “LAC has minimal effect” ^{5Reference 5Foster JG et al. · 2011In vitroIn vitro analysis of the anthelmintic activity of forage chicory (Cichorium intybus L.) sesquiterpene lactones against a predominantly Haemonchus contortus egg populationView study →}, and the cultivar richer in 11,13-dihydro-8-deoxylactucin was more potent against Ostertagia ostertagi in larval-feeding and adult-motility assays ^{2Reference 2Peña-Espinoza M et al. · 2015In vitroSesquiterpene lactone containing extracts from two cultivars of forage chicory (Cichorium intybus) show distinctive chemical profiles and activity against Ostertagia ostertagi — in vitroView study →}.

Every potency figure belongs to a whole extract quantified by lactone content.

No EC₅₀ has been published for the purified compound against any nematode, and the synergy finding means the isolate may underperform the extract.

No mechanism is established beyond presumed thiol alkylation, and electron microscopy found no cuticular damage ^{2Reference 2Peña-Espinoza M et al. · 2015In vitroSesquiterpene lactone containing extracts from two cultivars of forage chicory (Cichorium intybus) show distinctive chemical profiles and activity against Ostertagia ostertagi — in vitroView study →}.

No in-vivo anthelmintic study of the pure compound in any host.

Reported from —.

Asparagamine A is the chemical marker used to standardise the Stemona collinsiae root extract that a Mahidol University group is developing for human gnathostomiasis.

The standardized extract damaged advanced third-stage Gnathostoma spinigerum larvae in vitro, reduced larval burden in infected Wistar rats, and provoked less inflammatory reaction than albendazole ^{6Reference 6Arlee N et al. · 2024Assessing the efficacy of Stemona collinsiae roots extract against third-stage larvae of Gnathostoma spinigerum and its safety profilesView study →}.

No isolate has been run against a helminth.

The molecule serves as a certificate-of-analysis number rather than a demonstrated active, and the extract also contains stemofoline and other alkaloids.

The molecular target is unassigned — the Stemona insecticidal alkaloids are presumed to act on invertebrate nicotinic acetylcholine receptors by analogy with the butenolide insecticide flupyradifurone ^{7Reference 7Nauen R et al. · 2015Flupyradifurone: a brief profile of a new butenolide insecticideView study →}, but that has never been shown for a nematode or for this compound.

It does reach plasma: rat oral PK gives Tmax 1.75 h, Cmax ~1,153 ng/mL, t½ 1.86 h ^{8Reference 8Arlee N et al. · 2024AnimalLC-MS/MS analysis of didehydrostemofoline from Stemona collinsiae roots extracts in rats plasma and pharmacokinetics profile after oral administrationView study →}, so systemic exposure is at least achievable, unlike most large plant anthelmintic candidates.

Repandusinic acid A killed nematode larvae in a Phyllanthus urinaria isolate screen, with an IC₅₀ of 6.4 µM against Trichuris suis L1, the most sensitive of the parasites tested ^{11Reference 11Jato J et al. · 2023Anthelmintic activities of extract and ellagitannins from Phyllanthus urinaria against Caenorhabditis elegans and zoonotic or animal parasitic nematodesView study →}.

The molecular target is unknown; the plausible mechanism is the generic ellagitannin one, non-specific binding to cuticular and gut-surface proteins of the worm.

Like the α-glucosidase action, this is compartment-compatible — gut-dwelling helminths and an unabsorbed luminal tannin occupy the same space, so a low-µM larval IC₅₀ is at least physically reachable by an oral dose.

It was less active than geraniin from the same plant in the same assay, so on current evidence it contributes to a tannin-fraction effect rather than driving it ^{11Reference 11Jato J et al. · 2023Anthelmintic activities of extract and ellagitannins from Phyllanthus urinaria against Caenorhabditis elegans and zoonotic or animal parasitic nematodesView study →}.

Reported from chanca-piedra.

Activity-guided fractionation of Cicerbita alpina assigned its most active subfraction as 11β,13-dihydrolactucin, which inhibited 58% of Ascaridia galli embryo development at 1.8 µM, within range of the flubendazole control.

Alongside luteolin it affected tubulin polymerisation at 50 µM, with in-silico docking supporting microtubule stabilisation as the target class ^{1Reference 1Horgan MJ et al. · 2025In vitroMicrotubule inhibition as a proposed mechanism for the anthelmintic effect of phytochemicals isolated from Cicerbita alpina — in vitroView study →}.

That would put it in the same mechanistic family as the benzimidazole anthelmintics, which is a substantive claim for a dietary lactone.

The plant-level data contradict that.

In forage chicory the cultivar ‘Puna II’ had significantly higher 11,13-dihydrolactucin, yet its extract was the less potent of two against Ostertagia ostertagi larvae and adults, and the more active ‘Spadona’ extract was the one richer in 11,13-dihydro-8-deoxylactucin ^{2Reference 2Peña-Espinoza M et al. · 2015In vitroSesquiterpene lactone containing extracts from two cultivars of forage chicory (Cichorium intybus) show distinctive chemical profiles and activity against Ostertagia ostertagi — in vitroView study →}.

The isolate result and the cultivar correlation point at different molecules, and the isolate finding is a single-point subfraction assignment with no purified dose–response, no EC₅₀ and no mammalian-cell selectivity index.

Reported from Cicerbita alpina (no monograph here) ^{1,3Reference 1Horgan MJ et al. · 2025In vitroMicrotubule inhibition as a proposed mechanism for the anthelmintic effect of phytochemicals isolated from Cicerbita alpina — in vitroView study →Reference 3Zheleva-Dimitrova D et al. · 2023In vitroMetabolite profiling and bioactivity of Cicerbita alpina (L.) Wallr. (Asteraceae, Cichorieae) — in vitroView study →}; chicory (Cichorium intybus, forage cultivars) ^{2Reference 2Peña-Espinoza M et al. · 2015In vitroSesquiterpene lactone containing extracts from two cultivars of forage chicory (Cichorium intybus) show distinctive chemical profiles and activity against Ostertagia ostertagi — in vitroView study →}.

Two in-vivo fish trials are the only studies on this molecule that measured host toxicity alongside efficacy.

Against the monogenean gill fluke Dactylogyrus intermedius in goldfish, gracillin isolated from Dioscorea zingiberensis gave a 48-hour EC₅₀ of 0.18 mg/L against a goldfish LD₅₀ of 1.40 mg/L, a therapeutic index of 7.78, and was about 150× more potent than the trillin tested alongside it ^{9Reference 9Wang GX et al. · 2010Anthelmintic activity of steroidal saponins from Dioscorea zingiberensis CView study →}.

Against the ciliate Ichthyophthirius multifiliis, gracillin from Costus speciosus was 100% effective at 0.8 mg/L (EC₅₀ 0.53 mg/L), killed all protomonts and encysted tomonts at 1.0 mg/L, against a grass carp LD₅₀ of 1.64 mg/L ^{10Reference 10Zheng W et al. · 2015Antiparasitic efficacy of gracillin and zingibernsis newsaponin from Costus speciosus against Ichthyophthirius multifiliisView study →}.

The mechanism is almost certainly membrane lysis rather than any receptor: a spirostanol saponin at sub-mg/L in water, killing protozoa and metazoa alike with a host margin under ten-fold, is behaving as a surfactant.

The 2015 paper reports therapeutic indices of 2.76 and 7.78, which are precisely the 2010 paper’s figures for trillin and gracillin; recomputed from its own data the values are about 3.1 and 6.5, so the 2010 pair is the reliable one.

All of this is aquaculture immersion treatment: there is no oral anthelmintic study, no mammalian parasite, and no host-selectivity data outside fish.

Reported from wild-yam.

Bioassay-guided fractionation identified tribulosin as one of the two anthelmintic principles of Tribulus terrestris, with an ED50 of 76.25 µg/mL against Caenorhabditis elegans (β-sitosterol-D- glucoside, the other, at 82.50 µg/mL) ^{12Reference 12Deepak M et al. · 2002In vitroTribulosin and β-sitosterol-D-glucoside, the anthelmintic principles of Tribulus terrestris — in vitroView study →}.

The likely target is the nematode membrane rather than a receptor, and tribulosin’s membrane activity has been measured directly rather than assumed by class: on phosphatidylcholine bilayers it substantially lowers the boundary potential and alters the dipole potential enough to change gramicidin A channel conductance and lifetime, alongside digitonin and dioscin in the same experiments ^{13Reference 13Efimova SS · 2021In vitroIs the membrane lipid matrix a key target for action of pharmacologically active plant saponins? — in vitro, model lipid bilayersView study →}.