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CARAJURIN: A ANTHOCYANIDIN FROM ARRABIDAEA CHICA AS A POTENTIAL BIOLOGICAL MARKER OF ANTILEISHMANIAL ACTIVITY
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Abstract
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 in teractions 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 μg/mL for ACCE and 4.976 ± 1.09 μg/mL for ACAF. Anthocyanidins
carajurin, 3′
-hydroxy-carajurone, and carajurone had IC50 values of 3.66 ± 1.16, 22.70 ± 1.20, and 28.28 ± 0.07
μg/mL, respectively. The cytotoxicity assay after 72 h showed results ranging from 9.640 to 66.74 µg/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.
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