Antitrypanosomal Activity of a Semi-Purified Subfraction Rich in Labdane Sesquiterpenes, Obtained from Flowers of Anthemis Tinctoria, Against Trypanosoma Cruzi

Abstract

In Brazil and several other Latin American countries, Chagas' disease still constitutes a serious medical and social problem, and there is a need to develop new, more-potent drugs with fewer side effects to effectively treat this disease. We investigated the antitrypanosomal effect of a crude extract, fractions, and a semi-purified subfraction rich in a mix- ture of isomeric labdane sesquiterpenes, obtained from flowers of Anthemis tinctoria, against Trypanosoma cruzi. In epimastigote forms, the aqueous crude extract, dichloromethane fraction, and semi-purified subfraction showed a dose-dependent inhibitory activity, with IC50 of 2.3 μg/ml, 1.8 μg/ml, and 0.2 μg/ml, respectively. In the interaction in- dex, the semi-purified subfraction showed a reduction in both the percentage of infected LLCMK2 cells and the mean number of amastigotes per infected cell. The cytotoxicity evaluation demonstrated that the cytotoxic concentrations of the semi-purified subfraction were higher for LLCMK2 cells than for the protozoans, with a selectivity index of 35.0. Epimastigote forms treated with the semi-purified subfraction showed ultrastructural and morphological alterations such as rounding of the cells and bleb formation in the flagellum and cytoplasmic membrane. These results show that the flowers from A. tinctoria may be a source of new drugs with antiprotozoal activity. However, additional in vitro and in vivo studies are needed to validate the use of A. tinctoria in the treatment of Chagas’ disease

The Effectiveness of Natural Diarylheptanoids against Trypanosoma cruzi: Cytotoxicity, Ultrastructural Alterations and Molecular Modeling Studies

“…In this regard CUR was reported to produce microtubules disorganization in cancer cells [ 31 – 33 ] and in Plasmodium falciparum [ 34 ]. Similar flagellar membrane detachment was reported after parasite incubation with semi-purified subfraction obtained of Anthemis tinctoria [ 35 ]. The blebbing and shedding of parasite membranes must also be kept in mind since these microsomes or vesicles may bind to non-infected cells, which are recognized by anti- T .…”

An ethnobotanical survey of traditionally used plants on Suva planina mountain (south-eastern Serbia)

“…In the Suva planina region, A. tinctoria is mentioned in the treatment of liver complaints. Pharmacological data on this species reveals that extracts of its aerial parts exhibit bactericidal activity against Staphylococcus aureus, Pseudomonas aeruginosa, and Enterococcus faecalis (Akgul and Saglikoglu, 2005), as well as demonstrating antiproliferative activity in vitro against Trypanosoma cruzi, thanks to high sesquiterpene levels (Bittencourt et al, 2011). Mogosan et al (2005) mentioned that tincture of A. tinctoria promotes potassium retention and also that the saponins of this species increase urinary excretion of uric acid.…”