Isolation and characterisation of nematicidal compound, leolorin C, from Leonotis leonurus acetone leaf extract

• Published in: Journal of ethnopharmacology 2022-02, Vol.284, p.114802, Article 114802
• Main Authors: Makhubu, F.N., Nkadimeng, S.M., Fouche, G., Khosa, M.C., McGaw, L.J.
• Format: Article
• Language: English
• Subjects: Animals; Anthelmintic; Anthelmintics - chemistry; Anthelmintics - pharmacology; Anti-Bacterial Agents - chemistry; Anti-Bacterial Agents - pharmacology; Antimicrobial; Bacteria - drug effects; Caenorhabditis elegans; Caenorhabditis elegans - drug effects; Cell Survival; Chlorocebus aethiops; Cytotoxicity; Lamiaceae - chemistry; Leoleorin C; Leonotis leonurus; Molecular Structure; Plant Extracts - chemistry; Plant Extracts - pharmacology; Plant Leaves - chemistry; Tylenchoidea - drug effects; Vero Cells
• ISSN: 0378-8741; 1872-7573
• DOI: 10.1016/j.jep.2021.114802

Leonotis leonurus (L.) R.Br. (Lamiaceae) is a perennial shrub native to South Africa used to treat various diseases including digestive tract problems, intestinal worms and constipation. The aim was to isolate and characterise nematicidal compounds from leaves of L. leonurus. Bioassay-guided fractionation was carried out using the free-living nematode Caenorhabditis elegans as a model organism. Structural elucidation of the purified compound was carried out using NMR spectroscopic analyses and UPLC-QTOF-MS. The fractions and the isolated compound were tested for nematicidal activity on motility of plant-parasitic Meloidogyne incognita juveniles (J2s) and J2 hatch inhibition. Further screening was done to determine the minimum inhibitory concentration (MIC) of the fractions against bacterial phytopathogens and cytotoxicity against Vero kidney cells. Leoleorin C isolated from L. leonurus had moderate activity against C. elegans juveniles (34%) but was not active against J2 motility and J2 hatch of M. incognita. Thus, activity against the free-living C. elegans did not correspond with efficacy against plant-parasitic nematodes. Leoleorin C was not active against the tested bacterial phytopathogens, but some activity was observed in the bioautography assay against Clavibacter michiganensis subsp. michiganensis, the organism causing bacterial canker in tomatoes. The plant extract, fractions and leolorin C were relatively non-toxic to Vero cells with LC50 values greater than 0.01 mg/mL. The crude extract of L. leonurus and fractions may be useful in developing complementary treatments for controlling nematodes and phytopathogens. This study does not support the use of free-living nematodes as a model to isolate anti-parasitic compounds from plants. [Display omitted]