Nathielle Miranda1, Adriana Passarella Gerola2, Cláudio Roberto Novello3, Tânia Ueda-Nakamura4, Sueli de Oliveira Silva5, Benedito Prado Dias-Filho6, Noboru Hioka7, João Carlos Palazzo de Mello8, Celso Vataru Nakamura9. 1. Post-Graduate Program in Pharmaceutical Sciences, Laboratory of Technological Innovation in the Development of Drugs and Cosmetics, State University of Maringá, Maringá, Paraná, Brazil. Electronic address: nathielle.miranda@gmail.com. 2. Department of Chemistry, State University of Maringá, Maringá, Paraná, Brazil. Electronic address: adrianapassarella@yahoo.com.br. 3. Department of Pharmacy, State University of Maringá, Maringá, Paraná, Brazil. Electronic address: crnovello@gmail.com. 4. Post-Graduate Program in Pharmaceutical Sciences, Laboratory of Technological Innovation in the Development of Drugs and Cosmetics, State University of Maringá, Maringá, Paraná, Brazil; Department of Basic Sciences of Health, State University of Maringá, Maringá, Paraná, Brazil. Electronic address: tunakamura@uem.br. 5. Post-Graduate Program in Pharmaceutical Sciences, Laboratory of Technological Innovation in the Development of Drugs and Cosmetics, State University of Maringá, Maringá, Paraná, Brazil; Department of Basic Sciences of Health, State University of Maringá, Maringá, Paraná, Brazil. Electronic address: lautenschlager@uem.br. 6. Post-Graduate Program in Pharmaceutical Sciences, Laboratory of Technological Innovation in the Development of Drugs and Cosmetics, State University of Maringá, Maringá, Paraná, Brazil; Department of Basic Sciences of Health, State University of Maringá, Maringá, Paraná, Brazil. Electronic address: bpdfilho@uem.br. 7. Department of Chemistry, State University of Maringá, Maringá, Paraná, Brazil. Electronic address: nhioka@uem.br. 8. Post-Graduate Program in Pharmaceutical Sciences, Laboratory of Technological Innovation in the Development of Drugs and Cosmetics, State University of Maringá, Maringá, Paraná, Brazil. Electronic address: mello@uem.br. 9. Post-Graduate Program in Pharmaceutical Sciences, Laboratory of Technological Innovation in the Development of Drugs and Cosmetics, State University of Maringá, Maringá, Paraná, Brazil; Department of Basic Sciences of Health, State University of Maringá, Maringá, Paraná, Brazil. Electronic address: cvnakamura@gmail.com.
Abstract
BACKGROUND: Approximately 6-7 million people are infected with Trypanosoma cruzi, the etiological agent of Chagas' disease. Only two therapeutic compounds have been found to be useful against this disease: nifurtimox and benznidazole. These drugs have been effective in the acute phase of the disease but less effective in the chronic phase; they also have many side effects. Thus, the search for new compounds with trypanocidal action is necessary. Natural products can be the source of many important substances for the development of drugs to treat this infection. The present study evaluated the biological activity of an extract and fractions of Arrabidaea chica against T. cruzi and observed morphological and ultrastructural characteristics of parasites exposed to the isolated compound pheophorbide a. METHODS: The crude hydroethanolic extract of A. chica was prepared. Fractions were obtained by partition and separated by liquid chromatography. RESULTS: We observed a progressive increase in activity against epimastigote, trypomastigote, and amastigote forms of the parasite over the course of the fractionation process. Interestingly, we isolated a compound known as a photosensitizer that is used in photodynamic therapy. This method of treatment involving a photosensitizer, activation light and molecular oxygen is of great importance due to its selectivity. Pheophorbide a had activity against the protozoan in the presence of light and caused morphological and ultrastructural changes, demonstrating its potential in photodynamic therapy. CONCLUSIONS: Based on the ability of pheophorbide a to eliminate bloodstream forms of T. cruzi, we suggest its use in blood banks for hemoprophylaxis.
BACKGROUND: Approximately 6-7 million people are infected with Trypanosoma cruzi, the etiological agent of Chagas' disease. Only two therapeutic compounds have been found to be useful against this disease: nifurtimox and benznidazole. These drugs have been effective in the acute phase of the disease but less effective in the chronic phase; they also have many side effects. Thus, the search for new compounds with trypanocidal action is necessary. Natural products can be the source of many important substances for the development of drugs to treat this infection. The present study evaluated the biological activity of an extract and fractions of Arrabidaea chica against T. cruzi and observed morphological and ultrastructural characteristics of parasites exposed to the isolated compound pheophorbide a. METHODS: The crude hydroethanolic extract of A. chica was prepared. Fractions were obtained by partition and separated by liquid chromatography. RESULTS: We observed a progressive increase in activity against epimastigote, trypomastigote, and amastigote forms of the parasite over the course of the fractionation process. Interestingly, we isolated a compound known as a photosensitizer that is used in photodynamic therapy. This method of treatment involving a photosensitizer, activation light and molecular oxygen is of great importance due to its selectivity. Pheophorbide a had activity against the protozoan in the presence of light and caused morphological and ultrastructural changes, demonstrating its potential in photodynamic therapy. CONCLUSIONS: Based on the ability of pheophorbide a to eliminate bloodstream forms of T. cruzi, we suggest its use in blood banks for hemoprophylaxis.
Authors: Cleydlenne Costa Vasconcelos; Alberto Jorge Oliveira Lopes; Emerson Lucas Frazão Sousa; Darleno Sousa Camelo; Fernando César Vilhena Moreira Lima; Cláudia Quintino da Rocha; Gyl Eanes Barros Silva; João Batista Santos Garcia; Maria do Socorro de Sousa Cartágenes Journal: Int J Mol Sci Date: 2019-09-23 Impact factor: 5.923
Authors: João Victor Silva-Silva; Carla J Moragas-Tellis; Maria S S Chagas; Paulo Victor R Souza; Davyson L Moreira; Daiana J Hardoim; Noemi N Taniwaki; Vanessa F A Costa; Alvaro L Bertho; Daniela Brondani; Eduardo Zapp; Aldo Sena de Oliveira; Kátia S Calabrese; Maria D Behrens; Fernando Almeida-Souza Journal: Pharmaceuticals (Basel) Date: 2022-03-09
Authors: Douglas C Brandão; Paula M A P Lima; Isabella C Martins; Carina S Cordeiro; Antonielle O Cordeiro; Lara Vecchi; Joyce F C Guerra; Priscila C Orsolin; Matheus C Gazolla; Danilo S Costa; Ademar A da Silva Filho; Thaise G Araújo Journal: BMC Complement Med Ther Date: 2022-01-20