Antileishmanial activity and ultrastructural changes of sesquiterpene lactones isolated from Calea pinnatifida (Asteraceae) |
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| Institution: | 1. Laboratory of Experimental Protozoology, Department of Pathological Sciences, Center of Biological Sciences, State University of Londrina, PR, Brazil;2. Laboratory of Biotransformation and Phytochemistry, Department of Chemistry, Center of Exact Sciences, State University of Londrina, PR, Brazil;3. Laboratory of Research on Bioactive Molecules, Department of Chemistry, Center of Exact Sciences, State University of Londrina, PR, Brazil;4. Laboratory of Applied Immunology Research, Department of Pathology Science, Clinical Analysis and Toxicology, Health Sciences Center, State University of Londrina, Londrina, PR, Brazil;1. Instituto de Física, Universidade Federal de Goiás, Goiânia, GO, Brazil;2. Departamento de Farmácia e Farmacologia, Universidade Estadual de Maringá, Maringá, PR, Brazil;3. Instituto Federal Goiano, Trindade, GO, Brazil;4. Instituto de Patologia Tropical e Saúde Publica, Departamento de Imunologia e Patologia Geral, Universidade Federal de Goiás, Goiânia, GO, Brazil;1. Instituto de Química y Metabolismo del Fármaco (IQUIMEFA), CONICET- Universidad de Buenos Aires, Junín 956 2°piso, Buenos Aires 1113, Argentina;2. Cátedra de Farmacognosia, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Junín 956 2°piso, Buenos Aires 1113, Argentina;3. Centro de Investigaciones sobre Porfirinas y Porfirias (CIPYP), CONICET- Universidad de Buenos Aires Hospital de Clínicas José de San Martín, Córdoba 2351, Buenos Aires 1120, Argentina;4. Facultad de Ciencias Médicas, Instituto de Histología y Embriología \"Dr. Mario H. Burgos\" (IHEM), Universidad Nacional de Cuyo-CONICET, CC 56 (5500), Mendoza, Argentina;5. Departamento de Química Biológica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Intendente Güiraldes 2160, Buenos Aires 1428, Argentina |
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| Abstract: | Bioactivity-guided fractionation of antileishmanial active CH2Cl2 phase of MeOH extract from leaves of Calea pinnatifida led to isolation of two sesquiterpene lactones calein C (1) and calealactone C (2), which structures were stablished on the basis of spectroscopic analysis. Compounds 1 and 2 displayed potent activity against Leishmania amazonensis promastigotes with EC50 of 1.7 and 4.6 µg mL−1, respectively. Compound 2 presented low cytotoxicity for J774 macrophages and displayed activity against amastigote forms of L. amazonensis similar to miltefosine with CC50 values of 31.73 and 27.18 µg mL−1, respectively. Additionally, compounds 1 and 2 caused ultrastructural changes in promastigotes leading to a loss of their classical structural morphology, as evidenced by electron microscopy. Also compound 2 decreased the mitochondria membrane potential. To the best of our knowledge, this is the first occurrence of 1 and 2 in C. pinnatifida. The results obtained highlighted the importance of studying sesquiterpene lactones isolated from Calea pinnatifida in terms of antileishmanial activity, in order to understand the mechanism of action of the isolated compounds in promastigotes forms of L. amazonensis. |
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| Keywords: | Sesquiterpene lactones Antileishmanial activity Ultrastructural changes Mitochondrial membrane potential |
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