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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Sociedade Brasileira de Química
2019
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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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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. |
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Sociedade Brasileira de Química |
publishDate |
2019 |
url |
http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532019000801624 |
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