In our study, the binding affinities of selected natural products towards PfTrxR, PfGR, human TrxR and human GR were determined using a mass spectrometry based ligand binding assay. The in vitro antimalarial activity and cytotoxicity of these ligands were also determined. Catharanthine, 11-(OH)-coronaridine, hernagine, vobasine and hispolone displayed antiplasmodial activity against PfK1 (IC50 = 0.996–3.63 μg/mL).
FrederichM., TitsM., AngenotL. (2008) Potential antimalarial activity of indole alkaloids. Transactions of the Royal Society of Tropical Medicine and Hygiene, 102, 11–19.
ChinYW, BalunasM.J., ChaiH.B., KinghornA.D. (2006) Drug discovery from natural sources. The AAPS Journal, 8, 239–253.
4.
GuantaiE., ChibaleK. (2011) How can natural products serve as a viable source of lead compounds for the development of new/novel antimalarials?Malaria Journal, 10, S2–S8.
5.
MuniguntiR., CalderónA.I. (2012) Development of liquid chromatography/mass spectrometry based screening assay for PfTrxR inhibitors using relative quantitation of intact thioredoxin. Rapid Communications in Mass Spectrometry, 26, 1–6.
6.
RavikumarS., InbanesonS.J., SuganthiP. (2012) In vitro antiplasmodial activity of ethanolic extracts of South Indian medicinal plants against Plasmodium falciparum. Asian Pacific Journal of Tropical Disease, 180–183.
7.
MulabagalV., CalderónA.I. (2010) Development of binding assays to screen ligands for Plasmodium falciparum thioredoxin and glutathione reductases by ultrafiltration and liquid chromatography/mass spectrometry. Journal of Chromatography B, 878, 987–993.
8.
KanzokS.M., SchirmerR.H., TurbachovaI., IozefR., BeckerK. (2000) The Thioredoxin system of the malaria parasite Plasmodium falciparum. Glutathione reduction revisited. Journal of Biological Chemistry, 275, 40180–40186.
9.
FarberP.M., ArscottL.D., WilliamsC.H.Jr., BeckerK., SchirmerR.H. (1998) Recombinant Plasmodium falciparum glutathione reductase is inhibited by the antimalarial dye methylene blue. FEBS Letters, 422, 311–314.
10.
BradfordM.M. (1976) A rapid and sensitive method for the quantitation of microgram quantities of proteins utilizing the principle of protein-dye binding. Analytical Biochemistry, 72, 248–254.
11.
OrhanI., ŞenerB., KaiserM., BrunR., TasdemirD. (2010) Inhibitory activity of marine sponge-derived natural products against parasitic protozoa. Marine Drugs, 8, 47–58.
