Tags

Type your tag names separated by a space and hit enter

Psilostachyin C: a natural compound with trypanocidal activity.
Int J Antimicrob Agents. 2011 Jun; 37(6):536-43.IJ

Abstract

In this study, the antiprotozoal activity of the sesquiterpene lactone psilostachyin C was investigated. This natural compound was isolated from Ambrosia scabra by bioassay-guided fractionation and was identified by spectroscopic techniques. Psilostachyin C exerted in vitro trypanocidal activity against Trypanosoma cruzi epimastigotes, trypomastigotes and amastigotes, with 50% inhibitory concentration (IC(50)) values of 0.6, 3.5 and 0.9 μg/mL, respectively, and displayed less cytotoxicity against mammalian cells, with a 50% cytotoxic concentration (CC(50)) of 87.5 μg/mL. Interestingly, this compound induced ultrastructural alterations, as seen by transmission electron microscopy, in which vacuolisation and a structural appearance resembling multivesicular bodies were observed even at a concentration as low as 0.2 μg/mL. In an in vivo assay, a significant reduction in the number of circulating parasites was found in T. cruzi-infected mice treated with psilostachyin C for 5 days compared with untreated mice (7.4 ± 1.2 × 10(5)parasites/mL vs. 12.8 ± 2.0 × 10(5)parasites/mL) at the peak of parasitaemia. According to these results, psilostachyin C may be considered a promising template for the design of novel trypanocidal agents. In addition, psilostachyin C inhibited the growth of Leishmania mexicana and Leishmania amazonensis promastigotes (IC(50)=1.2 μg/mL and 1.5 μg/mL, respectively).

Authors+Show Affiliations

Cátedra de Farmacognosia, IQUIMEFA (UBA-CONICET), Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Junín 956 (1113), Buenos Aires, Argentina.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

21497061

Citation

Sülsen, Valeria P., et al. "Psilostachyin C: a Natural Compound With Trypanocidal Activity." International Journal of Antimicrobial Agents, vol. 37, no. 6, 2011, pp. 536-43.
Sülsen VP, Frank FM, Cazorla SI, et al. Psilostachyin C: a natural compound with trypanocidal activity. Int J Antimicrob Agents. 2011;37(6):536-43.
Sülsen, V. P., Frank, F. M., Cazorla, S. I., Barrera, P., Freixa, B., Vila, R., Sosa, M. A., Malchiodi, E. L., Muschietti, L. V., & Martino, V. S. (2011). Psilostachyin C: a natural compound with trypanocidal activity. International Journal of Antimicrobial Agents, 37(6), 536-43. https://doi.org/10.1016/j.ijantimicag.2011.02.003
Sülsen VP, et al. Psilostachyin C: a Natural Compound With Trypanocidal Activity. Int J Antimicrob Agents. 2011;37(6):536-43. PubMed PMID: 21497061.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Psilostachyin C: a natural compound with trypanocidal activity. AU - Sülsen,Valeria P, AU - Frank,Fernanda M, AU - Cazorla,Silvia I, AU - Barrera,Patricia, AU - Freixa,Blanca, AU - Vila,Roser, AU - Sosa,Miguel A, AU - Malchiodi,Emilio L, AU - Muschietti,Liliana V, AU - Martino,Virginia S, Y1 - 2011/04/15/ PY - 2010/09/30/received PY - 2011/01/27/revised PY - 2011/02/02/accepted PY - 2011/4/19/entrez PY - 2011/4/19/pubmed PY - 2011/8/4/medline SP - 536 EP - 43 JF - International journal of antimicrobial agents JO - Int. J. Antimicrob. Agents VL - 37 IS - 6 N2 - In this study, the antiprotozoal activity of the sesquiterpene lactone psilostachyin C was investigated. This natural compound was isolated from Ambrosia scabra by bioassay-guided fractionation and was identified by spectroscopic techniques. Psilostachyin C exerted in vitro trypanocidal activity against Trypanosoma cruzi epimastigotes, trypomastigotes and amastigotes, with 50% inhibitory concentration (IC(50)) values of 0.6, 3.5 and 0.9 μg/mL, respectively, and displayed less cytotoxicity against mammalian cells, with a 50% cytotoxic concentration (CC(50)) of 87.5 μg/mL. Interestingly, this compound induced ultrastructural alterations, as seen by transmission electron microscopy, in which vacuolisation and a structural appearance resembling multivesicular bodies were observed even at a concentration as low as 0.2 μg/mL. In an in vivo assay, a significant reduction in the number of circulating parasites was found in T. cruzi-infected mice treated with psilostachyin C for 5 days compared with untreated mice (7.4 ± 1.2 × 10(5)parasites/mL vs. 12.8 ± 2.0 × 10(5)parasites/mL) at the peak of parasitaemia. According to these results, psilostachyin C may be considered a promising template for the design of novel trypanocidal agents. In addition, psilostachyin C inhibited the growth of Leishmania mexicana and Leishmania amazonensis promastigotes (IC(50)=1.2 μg/mL and 1.5 μg/mL, respectively). SN - 1872-7913 UR - https://www.unboundmedicine.com/medline/citation/21497061/Psilostachyin_C:_a_natural_compound_with_trypanocidal_activity_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0924-8579(11)00099-9 DB - PRIME DP - Unbound Medicine ER -