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

10.1016/j.jtcme.2021.08.008

Aboagye Kwarteng Dofuor；Georgina Isabella Djameh；Michael Amoa-Bosompem；Samuel Kwain；Enoch Osei；Gilbert Mawuli Tetevi；Frederick Ayertey；Peter Bolah；Laud Kenneth Okine；Kwaku Kyeremeh；Theresa Manful Gwira；Mitsuko Ohashi

Asteraceae ； Cell cycle ； Apoptosis ； Necrosis ； Trypanosomatidae ； African trypanosomiasis ； Tryptophan esters

Journal of Traditional and Complementary Medicine

12卷3期（2022 / 05 / 01）

260 - 268

英文

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 (IC_(50)s) of 3.29 mg/ml and 5.86 mg/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 IC_(50) values of 0.66 and 1.46 mg/ml. At the IC_(50) 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.

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