Antileishmanial Activity and Immunomodulatory Effects of Tricin Isolated from Leaves of Casearia arborea (Salicaceae)

Abstract

Bioactivity-guided fractionation of antileishmanial active extract from leaves of Casearia arborea led to isolation of three metabolites: tricin (1), 1',6'-di-O-β-d-vanilloyl glucopyranoside (2) and vanillic acid (3). Compound 1 demonstrated the highest activity against the intracellular amastigotes of Leishmania infantum, with an IC value of 56 μm. Tricin (1) demonstrated selectivity in mammalian cells (SI > 7) and elicited immunomodulatory effect on host cells. The present work suggests that tricin modulated the respiratory burst of macrophages to a leishmanicidal state, contributing to the parasite elimination. Therefore, the natural compound tricin could be further explored in drug design studies for leishmaniasis treatment.

Identification of flavonoid‐3‐O‐glycosides from leaves of Casearia arborea (Salicaceae) by UHPLC‐DAD‐ESI‐HRMS/MS combined with molecular networking and NMR

“…255, 352) and observed it in EP compounds (Supporting Information, Figure S1). The literature agrees that there are flavonoids in the polar phase of C. arborea 14,16,17 . The absence of UV pattern for clerodane diterpenoids excludes the presence of these compounds in the polar phase of C. arborea EP, which corresponds to a low band in λ max.…”

“…listed a small number of flavonoids (11 structures) from Casearia species. After that review, another 11 known flavonoids in Casearia appeared for the first time; also, structures of glycosylated flavonoids were identified putatively in some Casearia species as cyanindin, delphinidin, isorhamnetin, luteolin, and quercetin derivatives 13,14,16–18,33,34 . In the present work, we reported 11 compounds using molecular networking aided by dereplication using the GNPS platform, analysis using HPLC‐DAD with standard compounds to confirm the annotations from MS/MS, and isolation of compounds for structural identification using NMR.…”

“…Clerodane diterpenes are chemical markers of Casearia ; they possess highly cytotoxic activity against several cancer cell lines, as described in a review by Xia et al 12 . A diverse array of flavonoids was recently described in various Casearia species, including C. arborea , 14,16,17 C. decandra , 14 C. gossypiosperma , 13 C. grandiflora , C. javitensis , C. lasiophylla , 14 C. sylvestris var. lingua , 18 and C. ulmifolia 14 .…”

Therapeutics Activities of Amazonian Plant Himatanthus sucuuba (Spruce ex Müll. Arg.) Woodson (Apocynaceae): A Review

“…Leishmaniasis is a disease with ample clinical spectrum and epidemiological diversity and is considered a sizable public health problem [82]. Several treatments, including plant extracts, showed an effective action against Leishmania as methanolic leave extract of Casearia arborea [83], ethanolic leave extract of Ocimum sanctum [84], hexane leave extract of Croton caudatus [85], ethanolic bark extract [56], and n-butanol leave extract [50] from H. sucuuba.…”

Alternative Treatment for Leishmaniasis

“…This effect was attributed to curcumin [54]. A substance isolated of Casearia arborea, tricin, was able to modulate the respiratory burst, which favors the parasite elimination [55].…”