Neocryptolepine: A Promising Indoloisoquinoline Alkaloid with Interesting Biological Activity. Evaluation of the Drug and its Most Relevant Analogs

Plants are one of the most important resources for the discovery of new drugs. The potential of natural compounds as new drug leads is clearly illustrated by the discovery and development of many modern medicines. This is an encouraging factor that drives natural products research in the vegetable k...

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Autores: Larghi, Enrique Leandro, Bracca, Andrea Beatriz Juana, Arrollo Aguilar, Abel A., Heredia, Daniel Alejandro, Pergomet, Jorgelina Leonor, Simonetti, Sebastián Osvaldo, Kaufman, Teodoro Saul
Formato: artículo
Estado:Versión publicada
Fecha de publicación:2015
País:Argentina
Recursos:Consejo Nacional de Investigaciones Científicas y Técnicas
Repositorio:CONICET Digital (CONICET)
Idioma:inglés
OAI Identifier:oai:ri.conicet.gov.ar:11336/6054
Acesso em linha:http://hdl.handle.net/11336/6054
Access Level:acceso abierto
Palavra-chave:Antimalarial Activity
Bioactive Natural Product Derivatives
Cytotoxicity
Dna Binding Compounds
Neocryptolepine (Cryptotakieine)
https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
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dc.title.none.fl_str_mv Neocryptolepine: A Promising Indoloisoquinoline Alkaloid with Interesting Biological Activity. Evaluation of the Drug and its Most Relevant Analogs
title Neocryptolepine: A Promising Indoloisoquinoline Alkaloid with Interesting Biological Activity. Evaluation of the Drug and its Most Relevant Analogs
spellingShingle Neocryptolepine: A Promising Indoloisoquinoline Alkaloid with Interesting Biological Activity. Evaluation of the Drug and its Most Relevant Analogs
Larghi, Enrique Leandro
Antimalarial Activity
Bioactive Natural Product Derivatives
Cytotoxicity
Dna Binding Compounds
Neocryptolepine (Cryptotakieine)
https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
title_short Neocryptolepine: A Promising Indoloisoquinoline Alkaloid with Interesting Biological Activity. Evaluation of the Drug and its Most Relevant Analogs
title_full Neocryptolepine: A Promising Indoloisoquinoline Alkaloid with Interesting Biological Activity. Evaluation of the Drug and its Most Relevant Analogs
title_fullStr Neocryptolepine: A Promising Indoloisoquinoline Alkaloid with Interesting Biological Activity. Evaluation of the Drug and its Most Relevant Analogs
title_full_unstemmed Neocryptolepine: A Promising Indoloisoquinoline Alkaloid with Interesting Biological Activity. Evaluation of the Drug and its Most Relevant Analogs
title_sort Neocryptolepine: A Promising Indoloisoquinoline Alkaloid with Interesting Biological Activity. Evaluation of the Drug and its Most Relevant Analogs
dc.creator.none.fl_str_mv Larghi, Enrique Leandro
Bracca, Andrea Beatriz Juana
Arrollo Aguilar, Abel A.
Heredia, Daniel Alejandro
Pergomet, Jorgelina Leonor
Simonetti, Sebastián Osvaldo
Kaufman, Teodoro Saul
author Larghi, Enrique Leandro
author_facet Larghi, Enrique Leandro
Bracca, Andrea Beatriz Juana
Arrollo Aguilar, Abel A.
Heredia, Daniel Alejandro
Pergomet, Jorgelina Leonor
Simonetti, Sebastián Osvaldo
Kaufman, Teodoro Saul
author_role author
author2 Bracca, Andrea Beatriz Juana
Arrollo Aguilar, Abel A.
Heredia, Daniel Alejandro
Pergomet, Jorgelina Leonor
Simonetti, Sebastián Osvaldo
Kaufman, Teodoro Saul
author2_role author
author
author
author
author
author
dc.subject.none.fl_str_mv Antimalarial Activity
Bioactive Natural Product Derivatives
Cytotoxicity
Dna Binding Compounds
Neocryptolepine (Cryptotakieine)
https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
topic Antimalarial Activity
Bioactive Natural Product Derivatives
Cytotoxicity
Dna Binding Compounds
Neocryptolepine (Cryptotakieine)
https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
description Plants are one of the most important resources for the discovery of new drugs. The potential of natural compounds as new drug leads is clearly illustrated by the discovery and development of many modern medicines. This is an encouraging factor that drives natural products research in the vegetable kingdom. Neocryptolepine is a tetracyclic nitrogen heterocycle isolated from the African climber Cryptolepis sanguinolenta, which is widely used in traditional African medicine in many countries of Central and West Africa. The natural product is one of the representative examples of the small family of indolo[2,3-b]quinoline alkaloids, being endowed of multiple biological activities, including DNA-binding and inhibition of the enzyme topoisomerase II. It is also cytotoxic, antibacterial, antifungal and molluscicidal, also displaying antiprotozoal activity, particularly as antitrypanosomal, antileishmanial, antischistosomal and antiplasmodial. Some of these activities have been related to the product’s ability to bind to DNA and to inhibit topoisomerase II; however, the exact mechanisms behind all of the observed bioactivities have not been comprehensively clarified. Major research activities regarding neocryptolepine have been focused into two seemingly opposite fields, related to its cytotoxic and antimalarial properties. Optimization of the natural product as a cytotoxic agent implied improvements in its bioavailability and activity, while the need of non-cytotoxic compounds guided the design and optimization of antimalarial agents. Therefore, the aim of the present article is to systematically review the current knowledge about the diversity of the biological activities related to neocryptolepine, its analogs and derivatives.
publishDate 2015
dc.date.none.fl_str_mv 2015-02
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/6054
Larghi, Enrique Leandro; Bracca, Andrea Beatriz Juana; Arrollo Aguilar, Abel A.; Heredia, Daniel Alejandro; Pergomet, Jorgelina Leonor; et al.; Neocryptolepine: A Promising Indoloisoquinoline Alkaloid with Interesting Biological Activity. Evaluation of the Drug and its Most Relevant Analogs; Bentham Science Publishers; Current Topics In Medicinal Chemistry; 15; 17; 2-2015; 1683-1707
1568-0266
url http://hdl.handle.net/11336/6054
identifier_str_mv Larghi, Enrique Leandro; Bracca, Andrea Beatriz Juana; Arrollo Aguilar, Abel A.; Heredia, Daniel Alejandro; Pergomet, Jorgelina Leonor; et al.; Neocryptolepine: A Promising Indoloisoquinoline Alkaloid with Interesting Biological Activity. Evaluation of the Drug and its Most Relevant Analogs; Bentham Science Publishers; Current Topics In Medicinal Chemistry; 15; 17; 2-2015; 1683-1707
1568-0266
dc.language.none.fl_str_mv eng
language eng
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info:eu-repo/semantics/altIdentifier/doi/10.2174/1568026615666150427113937
info:eu-repo/semantics/altIdentifier/doi/
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
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eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
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dc.publisher.none.fl_str_mv Bentham Science Publishers
publisher.none.fl_str_mv Bentham Science Publishers
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
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spelling Neocryptolepine: A Promising Indoloisoquinoline Alkaloid with Interesting Biological Activity. Evaluation of the Drug and its Most Relevant AnalogsLarghi, Enrique LeandroBracca, Andrea Beatriz JuanaArrollo Aguilar, Abel A.Heredia, Daniel AlejandroPergomet, Jorgelina LeonorSimonetti, Sebastián OsvaldoKaufman, Teodoro SaulAntimalarial ActivityBioactive Natural Product DerivativesCytotoxicityDna Binding CompoundsNeocryptolepine (Cryptotakieine)https://purl.org/becyt/ford/1.4https://purl.org/becyt/ford/1Plants are one of the most important resources for the discovery of new drugs. The potential of natural compounds as new drug leads is clearly illustrated by the discovery and development of many modern medicines. This is an encouraging factor that drives natural products research in the vegetable kingdom. Neocryptolepine is a tetracyclic nitrogen heterocycle isolated from the African climber Cryptolepis sanguinolenta, which is widely used in traditional African medicine in many countries of Central and West Africa. The natural product is one of the representative examples of the small family of indolo[2,3-b]quinoline alkaloids, being endowed of multiple biological activities, including DNA-binding and inhibition of the enzyme topoisomerase II. It is also cytotoxic, antibacterial, antifungal and molluscicidal, also displaying antiprotozoal activity, particularly as antitrypanosomal, antileishmanial, antischistosomal and antiplasmodial. Some of these activities have been related to the product’s ability to bind to DNA and to inhibit topoisomerase II; however, the exact mechanisms behind all of the observed bioactivities have not been comprehensively clarified. Major research activities regarding neocryptolepine have been focused into two seemingly opposite fields, related to its cytotoxic and antimalarial properties. Optimization of the natural product as a cytotoxic agent implied improvements in its bioavailability and activity, while the need of non-cytotoxic compounds guided the design and optimization of antimalarial agents. Therefore, the aim of the present article is to systematically review the current knowledge about the diversity of the biological activities related to neocryptolepine, its analogs and derivatives.Fil: Larghi, Enrique Leandro. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Rosario. Instituto de Química Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas; ArgentinaFil: Bracca, Andrea Beatriz Juana. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Rosario. Instituto de Química Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas; ArgentinaFil: Arrollo Aguilar, Abel A.. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Rosario. Instituto de Química Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas; ArgentinaFil: Heredia, Daniel Alejandro. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Rosario. Instituto de Química Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas; ArgentinaFil: Pergomet, Jorgelina Leonor. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Rosario. Instituto de Química Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas; ArgentinaFil: Simonetti, Sebastián Osvaldo. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Rosario. Instituto de Química Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas; ArgentinaFil: Kaufman, Teodoro Saul. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Rosario. Instituto de Química Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas; ArgentinaBentham Science Publishers2015-02info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/6054Larghi, Enrique Leandro; Bracca, Andrea Beatriz Juana; Arrollo Aguilar, Abel A.; Heredia, Daniel Alejandro; Pergomet, Jorgelina Leonor; et al.; Neocryptolepine: A Promising Indoloisoquinoline Alkaloid with Interesting Biological Activity. Evaluation of the Drug and its Most Relevant Analogs; Bentham Science Publishers; Current Topics In Medicinal Chemistry; 15; 17; 2-2015; 1683-17071568-0266enginfo:eu-repo/semantics/altIdentifier/url/http://www.eurekaselect.com/130653/articleinfo:eu-repo/semantics/altIdentifier/doi/10.2174/1568026615666150427113937info:eu-repo/semantics/altIdentifier/doi/info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2024-05-08T14:22:31Zoai:ri.conicet.gov.ar:11336/6054instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982024-05-08 14:22:31.7CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
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