The present study describes the use of the traditional species Copaifera for treating wounds, such as ulcers scarring and antileishmanial wounds. It also relates phytochemical studies, evaluation of the leishmanicidal activity, and toxicity. The species of Copaifera with a higher incidence in the Amazon region are Copaifera officinalis, Copaifera reticulata, Copaifera multijuga Hayne. The copaiba oil is used in the Amazon's traditional medicine, especially as anti-inflammatory ingredient, in ulcers healing, and in scarring and for leishmaniasis. Chemical studies have shown that these oils contain diterpenes and sesquiterpenes. The copaiba oil and terpenes isolated have antiparasitic activity, more promising in the amastigote form of L. amazonensis. This activity is probably related to changes in the cell membrane and mitochondria. The oil showed low cytotoxicity and genotoxicity. Furthermore, it may interfere with immune response to infection and also has a healing effect. In summary, the copaiba oil is promising as leishmanicidal agent.

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Leishmaniasis treatment is often carried out with drugs of high toxic potential and high cost, and satisfactory therapeutic response is not usually observed. In this context, searching for therapeutic alternatives is urgent. This study seeks to evaluate the antileishmanial potential of alkaloids from plants. The search for scientific papers occurred at Pubmed, CAPES Journal Portal (PPC), Virtual Health Library (VHL) and COCHRANE using the descriptors: alkaloid and antileishmanial. The inclusion criteria were studies about alkaloids isolated from plants and tested against Leishmania parasite. A total of 805 publications were found in Pubmed, 825 in PPC, 4 in VHL and none in COCRHANE. After reading the titles and abstracts, articles containing other biological evaluations (350), chemical studies such as docking and material characterizations (388), evaluation of extracts and fractions activities (406) which did not fit in this research or were in duplicate (377) were excluded. Acridone and all the naphthylisoquinolinic and tetrahydroisoquinolinic alkaloids were active or moderately active against Leishmania promastigotes or amastigotes, and indolizidine was active against both forms. The β-carbolines were inactive or moderately active against Leishmania promastigotes, with the exception of flavopereirine. The indolizidine alkaloid was the most promising as a future drug candidate, since it was very active against both forms of Leishmania.

This study evaluated the morphological changes caused by fractions and subfractions, obtained from barks of Aspidosperna nitidum, against L. (L.) amazonensis promastigotes. The ethanolic extract (EE) obtained through the maceration of trunk barks was subjected to an acid–base partition, resulting the neutral (FN) and the alkaloid (FA) fractions, and fractionation under reflux, yielded hexane (FrHEX), dichloromethane (FrDCL), ethyl acetate (FrACoET), and methanol (FrMEOH) fractions. The FA was fractionated and three subfractions (SF5-6, SF8, and SF9) were obtained and analyzed by HPLC–DAD and 1H NMR. The antipromastigote activity of all samples was evaluated by MTT, after that, scanning electron microscopy (SEM) and transmission electron microscopy (TEM) for the active fractions were performed. Chromatographic analyzes suggest the presence of alkaloids in EE, FN, FA, and FrDCL. The fractionation of FA led to the isolation of the indole alkaloid dihydrocorynantheol (SF8 fractions). The SF5-6, dihydrocorynantheol and SF-9 samples were active against promastigotes, while FrDCL was moderately active. The SEM analysis revealed cell rounding and changes in the flagellum of the parasites. In the TEM analysis, the treated promastigotes showed changes in flagellar pocket and kinetoplast, and presence of lipid inclusions. These results suggest that alkaloids isolated from A. nitidum are promising as leishmanicidal.

O tratamento medicamentoso da leishmaniose pode acarretar várias reações adversas e já foram encontrados isolados de Leishmania resistentes a terapêutica. Neste cenário, torna-se imprescindível a busca de alternativas terapêuticas e alcaloides, isolados de plantas pertencentes ao gênero Aspidosperma, têm se mostrado promissores como antiparasitário. O presente estudo avaliou a atividade antipromastigota, amastigota e citotoxicidade do extrato e frações pertencentes a A. nitidum. O extrato etanólico das cascas (EE) foi obtido por maceração e submetido a partição ácido:base, sendo obtidas as frações FN e FA. Além disso, o EE foi submetido ao fracionamento sob refluxo, obtendo-se as frações FrHEX, FrDCL, FrAcOEt e FrMeOH. A atividade antipromastigota em L. amazonensis e citotoxicidade para macrófagos foram avaliadas através do ensaio de viabilidade (MTT). Após a invasão dos macrófagos pelo parasito, realizou-se o tratamento com diferentes concentrações das amostras por 72 h, seguida de fixação e coloração das amostras e leitura em microscópio óptico. Somente a FrDCL mostrou-se moderadamente ativa contra promastigota (CI50= 105,7±1,12 µg/mL). No entanto, o EE (CI50= 23,87 ±0,87 µg/mL) e FA (CI50= 18,5 ±0,94 µg/mL) mostraram-se ativos contra amastigota, enquanto que na FrDCL (CI50= 204,5 ± 0,71 µg/mL) e FrHEX (CI50= 143,0 ±0,82 µg/mL) observou-se atividade moderada. Quando se relaciona a citotoxicidade das amostras a atividade antiamastigota, observa-se que o EE (CC50= 491,8 + 1,86 µg/mL; IS= 21) parece ser mais promissor que a FA (CC50= 209,1 + 1,7 µg/mL; IS=11). Em síntese, a A. nitidum mostrou-se promissora como leishmanicida.