In vitro Antiplasmodial Activities of Alkaloids Isolated from Roots of Worsleya procera (Lem.) Traub (Amaryllidaceae)

A combined phytochemical, crystallographic and biological study of Worsleya procera roots was performed. Fifteen alkaloids were identified by gas chromatography mass spectrometry (GC-MS) and seven of them were isolated. The structures of the alkaloids were elucidated by spectroscopic methods, and a detailed crystallographic study of tazettine was carried out. The isolated alkaloids and the obtained extracts were tested in vitro against Plasmodium falciparum (3D7 and K1 strains) and human hepatocarcinoma cells (HepG2) to assess their antiplasmodial and cytotoxic effects, respectively. One of the isolated alkaloid derivatives, lycorine, exhibited antiplasmodial activity against both sensitive (3D7) and resistant (K1) parasite strains in the low micromolar range (half-maximal sample inhibitory concentration (IC50) values of 2.5 and 3.1 µM, respectively) and displayed a low cytotoxicity profile, with a selectivity index greater than 100. Our findings indicate that lycorine is a hit for antimalarial drug discovery.

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Main Authors: Gonring-Salarini,Karla L., Conti,Raphael, Andrade,Jean Paulo de, Borges,Bárbara Juliana P., Aguiar,Anna Caroline C., Souza,Juliana O. de, Zanini,Camila L., Oliva,Glaucius, Tenorio,Juan Carlos, Ellena,Javier, Bastida,Jaume, Guido,Rafael V. C., Borges,Warley de S.
Format: Digital revista
Language:English
Published: Sociedade Brasileira de Química 2019
Online Access:http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532019000801624
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spelling oai:scielo:S0103-505320190008016242019-08-08In vitro Antiplasmodial Activities of Alkaloids Isolated from Roots of Worsleya procera (Lem.) Traub (Amaryllidaceae)Gonring-Salarini,Karla L.Conti,RaphaelAndrade,Jean Paulo deBorges,Bárbara Juliana P.Aguiar,Anna Caroline C.Souza,Juliana O. deZanini,Camila L.Oliva,GlauciusTenorio,Juan CarlosEllena,JavierBastida,JaumeGuido,Rafael V. C.Borges,Warley de S. isoquinolinic alkaloids Amaryllidaceae Plasmodium falciparum lycorine tazettine A combined phytochemical, crystallographic and biological study of Worsleya procera roots was performed. Fifteen alkaloids were identified by gas chromatography mass spectrometry (GC-MS) and seven of them were isolated. The structures of the alkaloids were elucidated by spectroscopic methods, and a detailed crystallographic study of tazettine was carried out. The isolated alkaloids and the obtained extracts were tested in vitro against Plasmodium falciparum (3D7 and K1 strains) and human hepatocarcinoma cells (HepG2) to assess their antiplasmodial and cytotoxic effects, respectively. One of the isolated alkaloid derivatives, lycorine, exhibited antiplasmodial activity against both sensitive (3D7) and resistant (K1) parasite strains in the low micromolar range (half-maximal sample inhibitory concentration (IC50) values of 2.5 and 3.1 µM, respectively) and displayed a low cytotoxicity profile, with a selectivity index greater than 100. Our findings indicate that lycorine is a hit for antimalarial drug discovery.info:eu-repo/semantics/openAccessSociedade Brasileira de QuímicaJournal of the Brazilian Chemical Society v.30 n.8 20192019-08-01info:eu-repo/semantics/articletext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532019000801624en10.21577/0103-5053.20190061
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language English
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author Gonring-Salarini,Karla L.
Conti,Raphael
Andrade,Jean Paulo de
Borges,Bárbara Juliana P.
Aguiar,Anna Caroline C.
Souza,Juliana O. de
Zanini,Camila L.
Oliva,Glaucius
Tenorio,Juan Carlos
Ellena,Javier
Bastida,Jaume
Guido,Rafael V. C.
Borges,Warley de S.
spellingShingle Gonring-Salarini,Karla L.
Conti,Raphael
Andrade,Jean Paulo de
Borges,Bárbara Juliana P.
Aguiar,Anna Caroline C.
Souza,Juliana O. de
Zanini,Camila L.
Oliva,Glaucius
Tenorio,Juan Carlos
Ellena,Javier
Bastida,Jaume
Guido,Rafael V. C.
Borges,Warley de S.
In vitro Antiplasmodial Activities of Alkaloids Isolated from Roots of Worsleya procera (Lem.) Traub (Amaryllidaceae)
author_facet Gonring-Salarini,Karla L.
Conti,Raphael
Andrade,Jean Paulo de
Borges,Bárbara Juliana P.
Aguiar,Anna Caroline C.
Souza,Juliana O. de
Zanini,Camila L.
Oliva,Glaucius
Tenorio,Juan Carlos
Ellena,Javier
Bastida,Jaume
Guido,Rafael V. C.
Borges,Warley de S.
author_sort Gonring-Salarini,Karla L.
title In vitro Antiplasmodial Activities of Alkaloids Isolated from Roots of Worsleya procera (Lem.) Traub (Amaryllidaceae)
title_short In vitro Antiplasmodial Activities of Alkaloids Isolated from Roots of Worsleya procera (Lem.) Traub (Amaryllidaceae)
title_full In vitro Antiplasmodial Activities of Alkaloids Isolated from Roots of Worsleya procera (Lem.) Traub (Amaryllidaceae)
title_fullStr In vitro Antiplasmodial Activities of Alkaloids Isolated from Roots of Worsleya procera (Lem.) Traub (Amaryllidaceae)
title_full_unstemmed In vitro Antiplasmodial Activities of Alkaloids Isolated from Roots of Worsleya procera (Lem.) Traub (Amaryllidaceae)
title_sort in vitro antiplasmodial activities of alkaloids isolated from roots of worsleya procera (lem.) traub (amaryllidaceae)
description A combined phytochemical, crystallographic and biological study of Worsleya procera roots was performed. Fifteen alkaloids were identified by gas chromatography mass spectrometry (GC-MS) and seven of them were isolated. The structures of the alkaloids were elucidated by spectroscopic methods, and a detailed crystallographic study of tazettine was carried out. The isolated alkaloids and the obtained extracts were tested in vitro against Plasmodium falciparum (3D7 and K1 strains) and human hepatocarcinoma cells (HepG2) to assess their antiplasmodial and cytotoxic effects, respectively. One of the isolated alkaloid derivatives, lycorine, exhibited antiplasmodial activity against both sensitive (3D7) and resistant (K1) parasite strains in the low micromolar range (half-maximal sample inhibitory concentration (IC50) values of 2.5 and 3.1 µM, respectively) and displayed a low cytotoxicity profile, with a selectivity index greater than 100. Our findings indicate that lycorine is a hit for antimalarial drug discovery.
publisher Sociedade Brasileira de Química
publishDate 2019
url http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532019000801624
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