<i>In vitro</i> anti-trypanosomal potential of kaurane and pimarane semi-synthetic derivatives

Rocha, Ana Carolina Ferreira Soares; Morais, Gustavo Oliveira; Silva, Marcela M da; Kovatch, Pedro Y.; Ferreira, Daniela; Esperandim, Viviane Rodrigues; Pagotti, Mariana Cintra; Magalhães, Lizandra Guidi; Heleno, Vladimir Constantino Gomes

doi:10.1080/14786419.2020.1837824

Cited by 3 publications

(2 citation statements)

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“…A trypanocidal activity research of pimarane diterpenes isolated from Aldama arenaria described the activity of the ent- 15-pimarene-8ß,19-diol (131) with IC 50 of 116.5 ± 1.21 µM while that of the positive control, gentian violet, was 76 µM (Ambrosio et al 2008). In other study ent-pimaradienoic acid (127) showed in-vitro trypanocidal activity with IC 50 of 68.7 µM (reference compound: benznidazole, IC 50 = 9.8 ± 0.68 µM), and the activity improved by esterification (Rocha et al 2022). In vitro studies against T. cruzi identified the activity of compounds 151, 171, and 187 isolated from Aldama aspilioides (Da Costa et al 1996a).…”

Section: Resultsmentioning

confidence: 90%

Secondary metabolites in Viguiera (Compositae, Heliantheae, Helianthinae) and segregated genera. A review of their biological activities with chemotaxonomic observations

et al. 2022

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Background: The first monograph of the genus Viguiera was published in 1918 by Blake, including about 141 species. Schilling & Panero based on studies of molecular sequences of nuclear Internal Transcribed Spacer and External Transcribed Spacer, as well as cpDNA, proposed to reclassify the genus, relocating its species in at least other nine genera. Question: Is it possible to identify distinctive patterns between the species of the new classification of Viguiera s. l. and the results of the chemical studies reported? Species considered: Sixty-seven species within the wide Viguiera circumscription with chemical studies and biological activities reported. Results: The species of the genus Viguiera synthesize terpenoids represented mainly by sesquiterpene lactones and diterpenes, with triterpenes, polyacetylenes, volatile terpenoids and flavonoids also present. The main types of secondary metabolites were present in the studied species, although some compounds were more frequent than others in some clades. Conclusion: Germacrolides, heliangolides, furanoheliangolides, tetracyclic diterpenes and flavonoids are the main constituents of Viguiera and segregated genera. Some interesting chemotaxonomic relationships are noted. Nevertheless, nondistinctive clear patterns were observed between clades and chemical groups. These results may be a consequence of the reported chemical studies of the species of Viguiera s. l., which have not agreed on objetives or methodologies.

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Section: Resultsmentioning

confidence: 90%

Secondary metabolites in Viguiera (Compositae, Heliantheae, Helianthinae) and segregated genera. A review of their biological activities with chemotaxonomic observations

et al. 2022

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“…Regarding the ent-pimaradienoic acid ( 91 , IC 50 68.7 μM) set, compound 94 (IC 50 3.8 μM) was the most active against trypomastigotes forms of T. cruzi . However, due to the lack of cytotoxicity data it is not possible to determine the selectivity index of these compounds [ 85 ].…”

Section: Terpenic Compounds With Antitrypanosomal Activitymentioning

confidence: 99%

Plant Terpenoids as Hit Compounds against Trypanosomiasis

et al. 2022

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Human African trypanosomiasis (sleeping sickness) and American trypanosomiasis (Chagas disease) are vector-borne neglected tropical diseases, caused by the protozoan parasites Trypanosoma brucei and Trypanosoma cruzi, respectively. These diseases were circumscribed to South American and African countries in the past. However, human migration, military interventions, and climate changes have had an important effect on their worldwide propagation, particularly Chagas disease. Currently, the treatment of trypanosomiasis is not ideal, becoming a challenge in poor populations with limited resources. Exploring natural products from higher plants remains a valuable approach to find new hits and enlarge the pipeline of new drugs against protozoal human infections. This review covers the recent studies (2016–2021) on plant terpenoids, and their semi-synthetic derivatives, which have shown promising in vitro and in vivo activities against Trypanosoma parasites.

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The Potential of Secondary Metabolites from Plants as Drugs or Leads against Trypanosoma cruzi-An Update from 2012 to 2021

Lago

Barbosa

Thevenard

et al. 2023

CTMC

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Background: Chagas disease (American Trypanosomiasis) is classified by the World Health Organization (WHO) as one of the seventeen neglected tropical diseases (NTD), affecting, mainly, several regions of Latin America. Introduction: However, immigration has expanded the range of this disease to other continents. Thousands of patients with Chagas disease die annually, yet no new therapeutics for Chagas disease have been approved, with only nifurtimox and benznidazole available. Treatment with these drugs presents several challenges, including protozoan resistance, toxicity, and low efficacy. Natural products, including the secondary metabolites found in plants, offer a myriad of complex structures that can be sourced directly or optimized for drug discovery. Method: Therefore, this review aims to assess the literature from the last 10 years (2011 – 2021) and present the anti-T. cruzi compounds isolated from plants in this period, as well as briefly discuss computational approaches and challenges in natural product drug discovery. Using this approach, more than 350 different metabolites were divided based on their biosynthetic pathway – alkaloids, terpenoids, flavonoids, polyketides, and phenylpropanoids which displayed activity against different forms of this parasite – epimastigote, trypomastigote and more important, the intracellular form, amastigote. Conclusion: In this aspect, there are several compounds with high potential which could be considered as a scaffold for the development of new drugs for the treatment of Chagas disease – for this, more advanced studies must be performed including pharmacokinetics (PK) and pharmacodynamics (PD) analysis as well as conduction of in vivo assays, these being important limitations in the discovery of new anti-T. cruzi compounds.

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In vitro anti-trypanosomal potential of kaurane and pimarane semi-synthetic derivatives

Cited by 3 publications

References 40 publications

Secondary metabolites in Viguiera (Compositae, Heliantheae, Helianthinae) and segregated genera. A review of their biological activities with chemotaxonomic observations

Secondary metabolites in Viguiera (Compositae, Heliantheae, Helianthinae) and segregated genera. A review of their biological activities with chemotaxonomic observations

Plant Terpenoids as Hit Compounds against Trypanosomiasis

The Potential of Secondary Metabolites from Plants as Drugs or Leads against Trypanosoma cruzi-An Update from 2012 to 2021

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