Planta Medica International Open 2017; 4(S 01): S1-S202
DOI: 10.1055/s-0037-1608560
Lecture Session – Ethnopharmacology
Georg Thieme Verlag KG Stuttgart · New York

Anthelmintic activity of procyanidins from West African medicinal plants – Insights into phytochemistry and molecular targets

V Spiegler
1  University of Münster, Institute for Pharmaceutical Biology & Phytochemistry, Münster, Germany
,
E Liebau
2  University of Münster, Institute for Animal Physiology – Molecular Physiology, Münster, Germany
,
A Hensel
1  University of Münster, Institute for Pharmaceutical Biology & Phytochemistry, Münster, Germany
› Author Affiliations
Further Information

Publication History

Publication Date:
24 October 2017 (online)

 

Oligomeric procyanidins (OPC) have been identified as the major anthelmintic components in hydroethanolic extracts from Combretum mucronatum leaves [1] and Paullinia pinnata roots [2] that are used as traditional remedies against soil-transmitted helminthiasis (STH) in West Africa [3]. The traditional use was rationalized by in vitro mortality assays against Caenorhabditis elegans and selected parasitic helminths (Toxocara cati, Trichuris vulpis).

To investigate the anthelmintic activity of OPCs on a molecular level, a transcriptome analysis was performed in C. elegans after treatment with purified OPCs from C. mucronatum (0.02 to 2 mg/mL).

Highly significant changes in differential gene expression were observed mainly for proteins related to the intestine, many of which were located extracellularly or within cellular membranes. Among the up-regulated genes, several hitherto undescribed orthologues of structural proteins in humans were identified, but also genes that are potentially involved in the worms' mechanism of tannin detoxification. For example, T22D1.2, an orthologue of human Basic salivary proline-rich protein (PRB) 2 or a nuclear localized metal responsive (numr-1) were found to be strongly up-regulated. Down-regulated genes, were mainly associated with lysosomal activity, glycoside hydrolysis or the worms' innate immune response.

The current findings support previous hypotheses of OPCs interacting with intestinal surface proteins and provide the first insights into the nematode's response to OPCs on a molecular level as a base for the identification of future drug targets.

[1] Spiegler V, Sendker J, Petereit F, Liebau E, Hensel A. Molecules 2015, 20: 14810 – 14832.

[2] Spiegler V, Liebau E, Peppler C, Raue K, Werne S, Strube C, Heckendorn F, Agyare C, Stark T, Hofmann T, Hensel A. Planta Medica 2016, 82: 1173 – 1179.

[3] Agyare C, Spiegler V, Sarkodie H, Asase A, Liebau E, Hensel A. J Ethnopharmacol 2014, 158PA: 255 – 263.