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Potential of Triterpenic Natural Compound Betulinic Acid for Neglected Tropical Diseases New Treatments

Neglected tropical diseases are one of the most important public health problems in many countries around the world. Among them are leishmaniasis, Chagas disease, and malaria, which contribute to more than 250 million infections worldwide. There is no validated vaccine to prevent these infections an...

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Autores principales: Rocha, Vinícius, Quadros, Helenita, Meira, Cássio, Silva, Laís, Carvalho, Dahara, Hodel, Katharine, Moreira, Diogo, Soares, Milena
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9027248/
https://www.ncbi.nlm.nih.gov/pubmed/35453582
http://dx.doi.org/10.3390/biomedicines10040831
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author Rocha, Vinícius
Quadros, Helenita
Meira, Cássio
Silva, Laís
Carvalho, Dahara
Hodel, Katharine
Moreira, Diogo
Soares, Milena
author_facet Rocha, Vinícius
Quadros, Helenita
Meira, Cássio
Silva, Laís
Carvalho, Dahara
Hodel, Katharine
Moreira, Diogo
Soares, Milena
author_sort Rocha, Vinícius
collection PubMed
description Neglected tropical diseases are one of the most important public health problems in many countries around the world. Among them are leishmaniasis, Chagas disease, and malaria, which contribute to more than 250 million infections worldwide. There is no validated vaccine to prevent these infections and the treatments available are obsolete, highly toxic, and non-effective due to parasitic drug resistance. Additionally, there is a high incidence of these diseases, and they may require hospitalization, which is expensive to the public health systems. Therefore, there is an urgent need to develop new treatments to improve the management of infected people, control the spread of resistant strains, and reduce health costs. Betulinic acid (BA) is a triterpene natural product which has shown antiparasitic activity against Leishmania, Trypanosoma cruzi, and Plasmodium. Here, we review the main results regarding the in vitro and in vivo pharmacological activity of BA and its derivatives against these parasites. Some chemical modifications of BA have been shown to improve its activities against the parasites. Further improvement on studies of drug-derived, as well as structure–activity relationship, are necessary for the development of new betulinic acid-based treatments.
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spelling pubmed-90272482022-04-23 Potential of Triterpenic Natural Compound Betulinic Acid for Neglected Tropical Diseases New Treatments Rocha, Vinícius Quadros, Helenita Meira, Cássio Silva, Laís Carvalho, Dahara Hodel, Katharine Moreira, Diogo Soares, Milena Biomedicines Review Neglected tropical diseases are one of the most important public health problems in many countries around the world. Among them are leishmaniasis, Chagas disease, and malaria, which contribute to more than 250 million infections worldwide. There is no validated vaccine to prevent these infections and the treatments available are obsolete, highly toxic, and non-effective due to parasitic drug resistance. Additionally, there is a high incidence of these diseases, and they may require hospitalization, which is expensive to the public health systems. Therefore, there is an urgent need to develop new treatments to improve the management of infected people, control the spread of resistant strains, and reduce health costs. Betulinic acid (BA) is a triterpene natural product which has shown antiparasitic activity against Leishmania, Trypanosoma cruzi, and Plasmodium. Here, we review the main results regarding the in vitro and in vivo pharmacological activity of BA and its derivatives against these parasites. Some chemical modifications of BA have been shown to improve its activities against the parasites. Further improvement on studies of drug-derived, as well as structure–activity relationship, are necessary for the development of new betulinic acid-based treatments. MDPI 2022-04-01 /pmc/articles/PMC9027248/ /pubmed/35453582 http://dx.doi.org/10.3390/biomedicines10040831 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Rocha, Vinícius
Quadros, Helenita
Meira, Cássio
Silva, Laís
Carvalho, Dahara
Hodel, Katharine
Moreira, Diogo
Soares, Milena
Potential of Triterpenic Natural Compound Betulinic Acid for Neglected Tropical Diseases New Treatments
title Potential of Triterpenic Natural Compound Betulinic Acid for Neglected Tropical Diseases New Treatments
title_full Potential of Triterpenic Natural Compound Betulinic Acid for Neglected Tropical Diseases New Treatments
title_fullStr Potential of Triterpenic Natural Compound Betulinic Acid for Neglected Tropical Diseases New Treatments
title_full_unstemmed Potential of Triterpenic Natural Compound Betulinic Acid for Neglected Tropical Diseases New Treatments
title_short Potential of Triterpenic Natural Compound Betulinic Acid for Neglected Tropical Diseases New Treatments
title_sort potential of triterpenic natural compound betulinic acid for neglected tropical diseases new treatments
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9027248/
https://www.ncbi.nlm.nih.gov/pubmed/35453582
http://dx.doi.org/10.3390/biomedicines10040831
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