Dataset Information

In vitro effects and mechanisms of action of Bidens pilosa in Trypanosoma brucei.

ABSTRACT:

Background and aim

African trypanosomiasis poses serious health and economic concerns to humans and livestock in several sub-Saharan African countries. The aim of the present study was to identify the antitrypanosomal compounds from B. pilosa (whole plant) through a bioactivity-guided isolation and investigate the in vitro effects and mechanisms of action against Trypanosoma brucei (T. brucei).

Experimental procedure

Crude extracts and fractions were prepared from air-dried pulverized plant material of B. pilosa using the modified Kupchan method of solvent partitioning. The antitrypanosomal activities of the fractions were determined through cell viability analysis. Effects of fractions on cell death and cell cycle of T. brucei were determined using flow cytometry, while fluorescence microscopy was used to investigate alterations in cell morphology and distribution.

Results and conclusion

The solvent partitioning dichloromethane (BPFD) and methanol (BPFM) fractions of B. pilosa exhibited significant activities against T. brucei with respective half-maximal inhibitory concentrations (IC₅₀s) of 3.29 μg/ml and 5.86 μg/ml and resulted in the formation of clumpy subpopulation of T. brucei cells. Butyl (compound 1) and propyl (compound 2) esters of tryptophan were identified as the major antitrypanosomal compounds of B. pilosa. Compounds 1 and 2 exhibited significant antitrypanosomal effects with respective IC₅₀ values of 0.66 and 1.46 μg/ml. At the IC₅₀ values, both compounds significantly inhibited the cell cycle of T. brucei at the G0-G1 phase while causing an increase in G2-M phase. The results suggest that tryptophan esters may possess useful chemotherapeutic properties for the control of African trypanosomiasis.

SUBMITTER: Dofuor AK

PROVIDER: S-EPMC9039108 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature

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Publications

In vitro effects and mechanisms of action of <i>Bidens pilosa</i> in <i>Trypanosoma brucei</i>.

Dofuor Aboagye Kwarteng AK Djameh Georgina Isabella GI Amoa-Bosompem Michael M Kwain Samuel S Osei Enoch E Tetevi Gilbert Mawuli GM Ayertey Frederick F Bolah Peter P Okine Laud Kenneth LK Kyeremeh Kwaku K Gwira Theresa Manful TM Ohashi Mitsuko M

Journal of traditional and complementary medicine 20210811 3

<h4>Background and aim</h4>African trypanosomiasis poses serious health and economic concerns to humans and livestock in several sub-Saharan African countries. The aim of the present study was to identify the antitrypanosomal compounds from <i>B. pilosa</i> (whole plant) through a bioactivity-guided isolation and investigate the <i>in vitro</i> effects and mechanisms of action against <i>Trypanosoma brucei</i> (<i>T. brucei</i>).<h4>Experimental procedure</h4>Crude extracts and fractions were pr ...[more]

PMID: 35493314

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Project description:African trypanosomiasis is a major neglected tropical disease with significant health and economic concerns in sub-Saharan Africa. In the absence of vaccines for African trypanosomiasis, there is a consideration for alternative sources of chemotherapy. Acanthospermum hispidum DC (A. hispidum) is a herbal species of the Asteraceae family that is endowed with rich phytochemicals with unknown mechanisms of antitrypanosomal effects. This study aimed to investigate the cellular mechanisms of antitrypanosomal and antioxidant activities of A. hispidum against Trypanosoma brucei (T. brucei), a causative protozoan species of African trypanosomiasis. Fractions were prepared from the whole plant of A. hispidum through solvent partitioning by employing solvents of varying polarities (hexane, HEX; dichloromethane, DCM; ethyl acetate, EA; aqueous, AQ). The in vitro efficacies and mechanisms of antitrypanosomal activities of A. hispidum were investigated using a panel of cell biological approaches. GC-MS analysis was used to identify the major compounds with a possible contribution to the trypanocidal effects of A. hispidum. A. hispidum fractions displayed significant antitrypanosomal activities in terms of half-maximal effective concentrations (EC50) and selectivity indices (SI) (AH-HEX, EC50 = 2.4 μg/mL, SI = 35.1; AH-DCM, EC50 = 2.2 μg/mL, SI = 38.3; AH-EA, EC50 = 1.0 μg/mL, SI = 92.8; AH-AQ, EC50 = 2.0 μg/mL, SI = 43.8). Fluorescence microscopic analysis showed that at their EC50 values, the fractions of A. hispidum altered the cell morphology as well as the organization of the mitochondria, nucleus, and kinetoplast in T. brucei. At their maximum tested concentrations, the prepared fractions exhibited antioxidant absorbance intensities comparable to the reference antioxidant, Trolox, in contrast to the oxidant intensity of an animal antitrypanosomal drug, diminazene (Trolox, 0.11 A; diminazene, 0.65 A; AH-HEX, 0.20 A, AH-DCM, 0.20 A, AH-EA, 0.13 A, AH-AQ, 0.22 A). GC-MS analysis of the various fractions identified major compounds assignable to the group of alkaloids and esters or amides of aliphatic acids. The results provide useful pharmacological insights into the chemotherapeutic potential of A. hispidum toward drug discovery for African trypanosomiasis.