Flavopereirine-An Alkaloid Derived from Geissospermum vellosii -Presents Leishmanicidal Activity In Vitro

Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
João Victor da Silva E SilvaMaria Fâni Dolabela

Abstract

Chemotherapy is limited in the treatment of leishmaniasis due to the toxic effects of drugs, low efficacy of alternative treatments, and resistance of the parasite. This work assesses the in vitro activity of flavopereirine on promastigote cultures of Leishmania amazonensis. In addition, an in silico evaluation of the physicochemical characteristics of this alkaloid is performed. The extract and fractions were characterized by thin-layer chromatography and HPLC-DAD, yielding an alkaloid identified by NMR. The antileishmanial activity and cytotoxicity were assayed by cell viability test (MTT). The theoretical molecular properties were calculated on the Molinspiration website. The fractionation made it possible to isolate a beta-carboline alkaloid (flavopereirine) in the alkaloid fraction. Moreover, it led to obtaining a fraction with greater antileishmanial activity, since flavopereirine is very active. Regarding the exposure time, a greater inhibitory effect of flavopereirine was observed at 24 h and 72 h (IC50 of 0.23 and 0.15 μg/mL, respectively). The extract, fractions, and flavopereirine presented low toxicity, with high selectivity for the alkaloid. Furthermore, flavopereirine showed no violation of Lipinski's rule of five...Continue Reading

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Methods Mentioned

BETA
NMR
Assay
enzyme-linked immunosorbent assay

Software Mentioned

PBSA
Antechamber
PMEMD
TLEaP
ff12SB
Amber
MM
MolDock
py
Graph Pad Prism

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