TY - JOUR
T1 - In vitro effects and mechanisms of action of Bidens pilosa in Trypanosoma brucei
AU - Dofuor, Aboagye Kwarteng
AU - Djameh, Georgina Isabella
AU - Amoa-Bosompem, Michael
AU - Kwain, Samuel
AU - Osei, Enoch
AU - Tetevi, Gilbert Mawuli
AU - Ayertey, Frederick
AU - Bolah, Peter
AU - Okine, Laud Kenneth
AU - Kyeremeh, Kwaku
AU - Gwira, Theresa Manful
AU - Ohashi, Mitsuko
N1 - Publisher Copyright:
© 2021 Center for Food and Biomolecules, National Taiwan University
PY - 2022/5
Y1 - 2022/5
N2 - 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.
AB - 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.
KW - African trypanosomiasis
KW - Apoptosis
KW - Asteraceae
KW - Cell cycle
KW - Necrosis
KW - Trypanosomatidae
KW - Tryptophan esters
UR - http://www.scopus.com/inward/record.url?scp=85112506576&partnerID=8YFLogxK
U2 - 10.1016/j.jtcme.2021.08.008
DO - 10.1016/j.jtcme.2021.08.008
M3 - Article
AN - SCOPUS:85112506576
SN - 2225-4110
VL - 12
SP - 260
EP - 268
JO - Journal of Traditional and Complementary Medicine
JF - Journal of Traditional and Complementary Medicine
IS - 3
ER -