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Trypanocidal and leishmanicidal activities of sesquiterpene lactones from Ambrosia tenuifolia Sprengel (Asteraceae).
Antimicrob Agents Chemother. 2008 Jul; 52(7):2415-9.AA

Abstract

Bioassay-guided fractionation of the organic extract of Ambrosia tenuifolia Sprengel (Asteraceae) led to the isolation of two bioactive sesquiterpene lactones with significant trypanocidal and leishmanicidal activities. By spectroscopic methods ((1)H- and (13)C-nuclear magnetic resonance, distortionless enhancement by polarization transfer, correlated spectroscopy, heteronuclear multiple-quantum coherence, electron impact-mass spectrometry, and infrared spectroscopy), these compounds were identified as psilostachyin and peruvin. Both compounds showed a marked in vitro trypanocidal activity against Trypanosoma cruzi epimastigotes with 50% inhibitory concentration (IC(50)) values of less than 2 microg/ml. Psilostachyin exerted a significant in vitro activity against the trypomastigote forms of T. cruzi (IC(50), 0.76 microg/ml) and was selected for in vivo testing. Psilostachyin-treated mice had a survival of 100% and lower parasitemia values than control mice. Both compounds were also tested on Leishmania sp. promastigotes: psilostachyin (IC(50), 0.12 microg/ml) and peruvin (IC(50), 0.39 microg/ml) exerted significant leishmanicidal activities. This is the first time that the trypanocidal and leishmanicidal activities of these compounds have been reported. The selectivity index (SI) was employed to evaluate the cytotoxic effect of lactones on T lymphocytes. Although the SIs of both compounds were high for T. cruzi epimastigotes, psilostachyin was more selective against trypomastigotes (SI, 33.8) while peruvin showed no specificity for this parasite. Both compounds presented high selectivity for Leishmania spp. The results shown herein suggest that psilostachyin and peruvin could be considered potential candidates for the development of new antiprotozoal agents against Chagas' disease and leishmaniasis.

Authors+Show Affiliations

Cátedra de Farmacognosia, IQUIMEFA (UBA-CONICET), 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 available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

18443111

Citation

Sülsen, Valeria P., et al. "Trypanocidal and Leishmanicidal Activities of Sesquiterpene Lactones From Ambrosia Tenuifolia Sprengel (Asteraceae)." Antimicrobial Agents and Chemotherapy, vol. 52, no. 7, 2008, pp. 2415-9.
Sülsen VP, Frank FM, Cazorla SI, et al. Trypanocidal and leishmanicidal activities of sesquiterpene lactones from Ambrosia tenuifolia Sprengel (Asteraceae). Antimicrob Agents Chemother. 2008;52(7):2415-9.
Sülsen, V. P., Frank, F. M., Cazorla, S. I., Anesini, C. A., Malchiodi, E. L., Freixa, B., Vila, R., Muschietti, L. V., & Martino, V. S. (2008). Trypanocidal and leishmanicidal activities of sesquiterpene lactones from Ambrosia tenuifolia Sprengel (Asteraceae). Antimicrobial Agents and Chemotherapy, 52(7), 2415-9. https://doi.org/10.1128/AAC.01630-07
Sülsen VP, et al. Trypanocidal and Leishmanicidal Activities of Sesquiterpene Lactones From Ambrosia Tenuifolia Sprengel (Asteraceae). Antimicrob Agents Chemother. 2008;52(7):2415-9. PubMed PMID: 18443111.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Trypanocidal and leishmanicidal activities of sesquiterpene lactones from Ambrosia tenuifolia Sprengel (Asteraceae). AU - Sülsen,Valeria P, AU - Frank,Fernanda M, AU - Cazorla,Silvia I, AU - Anesini,Claudia A, AU - Malchiodi,Emilio L, AU - Freixa,Blanca, AU - Vila,Roser, AU - Muschietti,Liliana V, AU - Martino,Virginia S, Y1 - 2008/04/28/ PY - 2008/4/30/pubmed PY - 2008/9/16/medline PY - 2008/4/30/entrez SP - 2415 EP - 9 JF - Antimicrobial agents and chemotherapy JO - Antimicrob. Agents Chemother. VL - 52 IS - 7 N2 - Bioassay-guided fractionation of the organic extract of Ambrosia tenuifolia Sprengel (Asteraceae) led to the isolation of two bioactive sesquiterpene lactones with significant trypanocidal and leishmanicidal activities. By spectroscopic methods ((1)H- and (13)C-nuclear magnetic resonance, distortionless enhancement by polarization transfer, correlated spectroscopy, heteronuclear multiple-quantum coherence, electron impact-mass spectrometry, and infrared spectroscopy), these compounds were identified as psilostachyin and peruvin. Both compounds showed a marked in vitro trypanocidal activity against Trypanosoma cruzi epimastigotes with 50% inhibitory concentration (IC(50)) values of less than 2 microg/ml. Psilostachyin exerted a significant in vitro activity against the trypomastigote forms of T. cruzi (IC(50), 0.76 microg/ml) and was selected for in vivo testing. Psilostachyin-treated mice had a survival of 100% and lower parasitemia values than control mice. Both compounds were also tested on Leishmania sp. promastigotes: psilostachyin (IC(50), 0.12 microg/ml) and peruvin (IC(50), 0.39 microg/ml) exerted significant leishmanicidal activities. This is the first time that the trypanocidal and leishmanicidal activities of these compounds have been reported. The selectivity index (SI) was employed to evaluate the cytotoxic effect of lactones on T lymphocytes. Although the SIs of both compounds were high for T. cruzi epimastigotes, psilostachyin was more selective against trypomastigotes (SI, 33.8) while peruvin showed no specificity for this parasite. Both compounds presented high selectivity for Leishmania spp. The results shown herein suggest that psilostachyin and peruvin could be considered potential candidates for the development of new antiprotozoal agents against Chagas' disease and leishmaniasis. SN - 1098-6596 UR - https://www.unboundmedicine.com/medline/citation/18443111/Trypanocidal_and_leishmanicidal_activities_of_sesquiterpene_lactones_from_Ambrosia_tenuifolia_Sprengel__Asteraceae__ L2 - http://aac.asm.org/cgi/pmidlookup?view=long&pmid=18443111 DB - PRIME DP - Unbound Medicine ER -