Memorias do Instituto Oswaldo Cruz · 2026
In vitro anti-Trypanosomatid activity and chemical profile of crude extracts of Chromolaena hookeriana and Campuloclinium macrocephalum (Asteraceae).
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Fiuza Ludmila Ferreira de Almeida, da Conceição Ketlym, Nunes Krislayne, Corlatti Aldana Malen, Laurella Laura Cecilia, Mendonça Simony Carvalho, Gomes Brendo Araujo, Leitão Suzana Guimarães, Sülsen Valeria Patricia, Soeiro Maria de Nazaré Correia
Аннотация
BACKGROUND: Chagas disease (CD) and Leishmaniasis, caused by Trypanosoma cruzi and Leishmania species, are treated with outdated drugs that are toxic and have limited efficacy. New therapeutic alternatives are therefore needed. Natural products are valuable scaffolds for drug discovery, and Asteraceae species exhibit microbicidal activity.
OBJECTIVES: This study evaluated the antiparasitic activity and selectivity of two Asteraceae species, Chromolaena hookeriana and Campuloclinium macrocephalum, against trypanosomatids.
METHODS: C. hookeriana and C. macrocephalum extracts were profiled by ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS), and their cytotoxicity and antiparasitic activity were evaluated against multiple forms and strains of T. cruzi and Leishmania amazonensis (L. amazonensis) in 2D and 3D cultures.
FINDINGS: UHPLC-MS/MS revealed predominantly pentacyclic triterpenoids in C. macrocephalum, including ursolic and oleanolic acids (negative mode) and lupeol derivatives (positive mode). C. macrocephalum was more effective than Benznidazole (Bz) (EC50 = 1.17 vs 4.47 µg/mL) against epimastigotes and nine times more potent against trypomastigotes (EC50 = 0.38 vs 3.5 µg/mL). Both extracts matched Bz activity on intracellular T. cruzi but exhibited time-dependent cytotoxicity. They also showed similar effectiveness to miltefosine (Mt) against L. amazonensis amastigotes (EC50 = 0.36-0.70 µg/mL).
MAIN CONCLUSIONS: The chemical profile supports the stronger antiparasitic activity of C. macrocephalum, likely linked to triterpenoids, and highlights Asteraceae extracts as promising candidates for drug discovery against neglected tropical diseases (NTDs).
OBJECTIVES: This study evaluated the antiparasitic activity and selectivity of two Asteraceae species, Chromolaena hookeriana and Campuloclinium macrocephalum, against trypanosomatids.
METHODS: C. hookeriana and C. macrocephalum extracts were profiled by ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS), and their cytotoxicity and antiparasitic activity were evaluated against multiple forms and strains of T. cruzi and Leishmania amazonensis (L. amazonensis) in 2D and 3D cultures.
FINDINGS: UHPLC-MS/MS revealed predominantly pentacyclic triterpenoids in C. macrocephalum, including ursolic and oleanolic acids (negative mode) and lupeol derivatives (positive mode). C. macrocephalum was more effective than Benznidazole (Bz) (EC50 = 1.17 vs 4.47 µg/mL) against epimastigotes and nine times more potent against trypomastigotes (EC50 = 0.38 vs 3.5 µg/mL). Both extracts matched Bz activity on intracellular T. cruzi but exhibited time-dependent cytotoxicity. They also showed similar effectiveness to miltefosine (Mt) against L. amazonensis amastigotes (EC50 = 0.36-0.70 µg/mL).
MAIN CONCLUSIONS: The chemical profile supports the stronger antiparasitic activity of C. macrocephalum, likely linked to triterpenoids, and highlights Asteraceae extracts as promising candidates for drug discovery against neglected tropical diseases (NTDs).