In Vitro and In Silico Anthelmintic Activity of Extracts of Lannea kerstingii and Ficus thonningii on Heligmosomoides polygyrus

Abstract

Background: The aim of this study was to assess the anthelmintic activity of Lannea kerstingii and Ficus thonningii, on a nematode model, to promote their use in the Cameroonian pharmacopoeia for the treatment of helminthiases. Methods: One nematode was used, Heligmosomoides polygyrus. First, the effect of the extracts on the eggs and larval stages (L1, L2, and L3) of H. polygyrus was evaluated, 100 μL of extract and 100 μL of parasite suspension (containing 50 eggs) were mixed in a 96-well microplate. The 96-well microplate was incubated for 20 h at 25°C in the WMicroTracker which measures the motility of the worms at various concentrations. Finally, docking studies were conducted by using the Glide module in Schrodinger Maestro. Results: The ethanolic extract of L. kerstingii with the half maximal inhibitory concentration (IC₅₀) of 0.1371 mg/mL produced a higher ovicidal effect than the effect produced by other extracts of these plants. However, with an IC₅₀ of 0.31 mg/mL, the aqueous extract of F. thonningii showed the greatest effect on the L2 stage. The aqueous and ethanolic extracts of L. kerstingii and F. thonningii inhibited the development of the L3 larvae of H. polygyrus with a better effect for the ethanolic extracts. Conclusion: The use of L. kerstingii and F. thonningii for the treatment of helminthiasis has been proved in vitro and in silico by this research. However, more research is required, especially on the acute toxicity and in vivo anthelmintic efficacy to validate this scientific investigation.

Keywords: Ficus thonningii; Heligmosomoides polygyrus; Lannea kerstingii; anthelmintics.

Figure 1

PDB ID: 1SA0. (a) The surface mode of the β-tubulin, (b) optimized β-tubulin receptor, and (c) Ramachandran plot of β-tubulin receptor. PDB ID: 4YSX. (d) The surface mode of the SDH model, (e) optimized SDH model receptor, and (f) Ramachandran plot of SDH model receptor.

Figure 2

Inhibitory concentration 50 (IC₅₀) of egg hatching treated with aqueous and ethanolic extracts of L. kerstingii and F. thonningii.

Figure 3

First larval stage and larval motility IC₅₀ of H. polygyrus when treated with aqueous and ethanolic extracts of L. kerstingii and F. thonningii.

Figure 4

Second larval stage and larval motility IC₅₀ of H. polygyrus when treated with aqueous and ethanolic extracts of L. kerstingii and F. thonningii.

Figure 5

Third larval stage and larval motility IC₅₀ of H. polygyrus when treated with aqueous and ethanolic extracts of L. kerstingii and F. thonningii.

Figure 6

Three-dimensional (3D) and two-dimensional (2D) interactions between the β-tubulin and the ligands of L. kerstingii: (a) p-coumaric acid, (b) vacciniin, (c) cianidanol, (d) 2-O-caffeoylglucarate, (e) phyllocoumarin, and (f) albendazole.

Figure 7

Three-dimensional (3D) and two-dimensional (2D) interactions between the SDH and the ligands of L. kerstingii: (a) L-tryptophane, (b) cianidanol, (c) phyllocoumarin, (d) 5-p-coumaroylquinic acid, (e) vacciniin, and (f) albendazole.

Figure 8

Three-dimensional (3D) and two-dimensional (2D) interactions between the β-tubulin and ligands of F. thonningii: (a) protocatechuic acid, (b) dihydroquercetin, (c) dihydrokaempferol, (d) thonningianin A, (e) luteone, and (f) albendazole.

Figure 9

Three-dimensional (3D) and two-dimensional (2D) interactions between the SDH and the ligands of F. thonningii: (a) luteone, (b) shuterin, (c) alpinumisoflavone, (d) gancaonin A, (e) taxifolin, and (f) albendazole.