Carajurin: a anthocyanidin from Arrabidaea chica as a potential biological marker of antileishmanial activity

Autor(es):Mostrar menos -

Silva-Silva, Joao Victor ^[1] ; Moragas-Tellis, Carla J. ^[2] ; Chagas, Maria S. S. ^[2] ; Souza, Paulo Victor R. ^{[2, 3]} ; Moreira, Davyson L. ^{[2, 4]} ; de Souza, Celeste S. F. ^[1] ; Teixeira, Kerolain F. ^[5] ; Cenci, Arthur R. ^[5] ; de Oliveira, Aldo S. ^[5] ; Almeida-Souza, Fernando ^{[1, 6]} ; Behrens, Maria D. ^[2] ; Calabrese, Katia S. ^[1]

Afiliação do(s) autor(es)

^[1] Fundacao Oswaldo Cruz, Oswaldo Cruz Inst, Lab Immunomodulat & Protozool, Rio De Janeiro, RJ - Brazil

^[2] Fundacao Oswaldo Cruz, Pharmaceut Technol Inst Farmanguinhos, Lab Nat Prod Publ Hlth, Rio De Janeiro, RJ - Brazil

^[3] Fundacao Oswaldo Cruz, Postgrad Program Translat Res Drugs & Med, Farmanguinhos, Rio De Janeiro, RJ - Brazil

^[4] Rio de Janeiro Bot Garden Res Inst, BR-22460030 Rio De Janeiro, RJ - Brazil

^[5] Univ Fed Santa Catarina, Dept Exact Sci & Educ, Blumenau, SC - Brazil

^[6] Univ Estadual Maranhao, Postgrad Program Anim Sci, Sao Luis, Maranhao - Brazil

• Tipo de documento: Artigo Científico
• Fonte: BIOMEDICINE & PHARMACOTHERAPY; v. 141, SEP 2021.
• Citações Web of Science: 0

Resumo

Leishmaniasis is a group of neglected tropical diseases whose treatment with antimonials bears limitations and has changed little in over 80 years. Medicinal plants have been evaluated as a therapeutic alternative for leishmaniasis. Arrabidaea chica is popularly used as a wound healing and antiparasitic agent, especially as leishmanicidal agent. This study examined the leishmanicidal activity of a crude extract (ACCE), an anthocyanidin-rich fraction (ACAF), and three isolated anthocyanidins from A. chica: carajurin, 3'-hydroxy-carajurone, and carajurone. We evaluated the antileishmanial activity against promastigote and intracellular amastigote forms of Leishmania amazonensis and determined cytotoxicity in BALB/c peritoneal macrophages, as well as nitrite quantification, using the Griess method. Molecular docking was carried out to evaluate interactions of carajurin at the nitric oxide synthase enzyme. All compounds were active against promastigotes after 72 h, with IC50 values of 101.5 +/- 0.06 mu g/mL for ACCE and 4.976 +/- 1.09 mu g/mL for ACAF. Anthocyanidins carajurin, 3'-hydroxy-carajumne, and carajumne had IC50 values of 3.66 +/- 1.16, 22.70 +/- 1.20, and 28.28 +/- 0.07 mu g/mL, respectively. The cytotoxicity assay after 72 h showed results ranging from 9.640 to 66.74 mu g/mL for anthocyanidins. ACAF and carajurin showed selectivity against intracellular amastigote forms (SI> 10), with low cytotoxicity within 24 h, a statistically significant reduction in all infection parameters, and induced nitrite production. Molecular docking studies were developed to understand a possible mechanism of activation of the nitric oxide synthase enzyme, which leads to an increase in the production of nitric oxide observed in the other experiments reported. These results encourage us to suggest carajurin as a biological marker of A. chica. (AU)

• Processo FAPESP: 13/07600-3 - CIBFar - Centro de Inovação em Biodiversidade e Fármacos
• Beneficiário: Glaucius Oliva
• Modalidade de apoio: Auxílio à Pesquisa - Centros de Pesquisa, Inovação e Difusão - CEPIDs
• Processo FAPESP: 20/12904-5 - Descoberta de inibidores de Plasmodium falciparum a partir de plantas do Cerrado como candidatos a compostos líderes para a malária: estudos integrados de cromatografia de ultra eficiência, espectroscopia e ensaios biológicos
• Beneficiário: Rafael Victorio Carvalho Guido
• Modalidade de apoio: Auxílio à Pesquisa - Programa BIOTA - Regular