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Planta Med 2021; 87(06): 480-488
DOI: 10.1055/a-1373-6074
Natural Product Chemistry and Analytical Studies
Original Papers

Optimization of Coumarins Extraction from Pterocaulon balansae by Box-Behnken Design and Anti-Trichomonas vaginalis Activity

Nathalya Tesch Brazil
1   Faculdade de Farmácia, Programa de Pós Graduação em Ciências Farmacêuticas (PPGCF), Universidade Federal do Rio Grande do Sul (UFRGS), Santana, Porto Alegre, RS, Brazil
,
Bruna Medeiros-Neves
1   Faculdade de Farmácia, Programa de Pós Graduação em Ciências Farmacêuticas (PPGCF), Universidade Federal do Rio Grande do Sul (UFRGS), Santana, Porto Alegre, RS, Brazil
,
Flávia Nathiely Silveira Fachel
1   Faculdade de Farmácia, Programa de Pós Graduação em Ciências Farmacêuticas (PPGCF), Universidade Federal do Rio Grande do Sul (UFRGS), Santana, Porto Alegre, RS, Brazil
,
Vanessa Pittol 
1   Faculdade de Farmácia, Programa de Pós Graduação em Ciências Farmacêuticas (PPGCF), Universidade Federal do Rio Grande do Sul (UFRGS), Santana, Porto Alegre, RS, Brazil
,
Roselena Silvestri Schuh
1   Faculdade de Farmácia, Programa de Pós Graduação em Ciências Farmacêuticas (PPGCF), Universidade Federal do Rio Grande do Sul (UFRGS), Santana, Porto Alegre, RS, Brazil
2   Centro de Pesquisa Experimental, Laboratório Células, Tecidos e Genes, Hospital de Clínicas de Porto Alegre (HCPA), Santa Cecília, Porto Alegre, RS, Brazil
,
Graziela Vargas Rigo
1   Faculdade de Farmácia, Programa de Pós Graduação em Ciências Farmacêuticas (PPGCF), Universidade Federal do Rio Grande do Sul (UFRGS), Santana, Porto Alegre, RS, Brazil
,
Tiana Tasca
1   Faculdade de Farmácia, Programa de Pós Graduação em Ciências Farmacêuticas (PPGCF), Universidade Federal do Rio Grande do Sul (UFRGS), Santana, Porto Alegre, RS, Brazil
,
Gilsane Lino von Poser
1   Faculdade de Farmácia, Programa de Pós Graduação em Ciências Farmacêuticas (PPGCF), Universidade Federal do Rio Grande do Sul (UFRGS), Santana, Porto Alegre, RS, Brazil
,
Helder Ferreira Teixeira
1   Faculdade de Farmácia, Programa de Pós Graduação em Ciências Farmacêuticas (PPGCF), Universidade Federal do Rio Grande do Sul (UFRGS), Santana, Porto Alegre, RS, Brazil
› Author AffiliationsSupported by: Coordenação de Aperfeiçoamento de Pessoal de Nível Superior Finance code 001
Supported by: Conselho Nacional de Desenvolvimento Científico e Tecnológico 459619/2014-4
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Abstract

Trichomonas vaginalis causes trichomoniasis, a nonviral sexually transmitted infection with a high prevalence worldwide. Oral metronidazole is the drug of choice for the treatment of this disease, although high levels of T. vaginalis resistance to this agent are well documented in the literature. This study describes the anti-T. vaginalis activity of an optimized coumarin-rich extract from Pterocaulon balansae. Optimization was performed to maximize extraction of total coumarins by means of a 3-level Box-Behnken design, evaluating the effect of three factors: extraction time, plant : solvent ratio, and ethanol concentration. Optimum conditions were found to be 5 h extraction time and a plant : solvent ratio of 1% (w/v) and 60% (v/v) ethanol, which resulted in approximately 30 mg of total coumarins/g of dry plant. The coumarin-enriched extract exhibited a minimum inhibitory concentration of 30 µg/mL and an IC50 of 3.2 µg/mL against T. vaginalis, a low cytotoxicity, and a high selectivity index (18 for vaginal epithelial cells and 16 for erythrocytes). The coumarins permeation/retention profile through porcine vaginal mucosa was evaluated in Franz-type diffusion cells. After 8 h of kinetics, coumarins were detected in the tissue (4.93 µg/g) without detecting them in the receptor compartment. A significant increase of coumarins in the mucosa layers (8.18 µg/g) and receptor compartment (0.26 µg/g) was detected when a T. vaginalis suspension (2 × 105 trophozoites/mL) was previously added onto the mucosa. No alterations were visualized in the stratified squamous non-keratinized epithelium of the porcine vaginal mucosa after contact with the extract. Overall, these results suggest that the P. balansae coumarin-rich extract may have potential as a treatment for trichomoniasis.

Key words

Pterocaulon balansae - Asteraceae - coumarins - Box-Behnken design - Trichomonas vaginalis - vaginal mucosa

Supporting Information

    The chromatographic profile of HEE of P. balansae (Fig. 1S), BBD arrangement and experimental values (Table 1S), linearity, precision, and accuracy (Table 2S), and recovery of P. balansae coumarins from porcine vaginal mucosa (Table 3S) are available as Supporting Information.

  • Supporting Information


Publication History

Received: 25 May 2020

Accepted after revision: 19 January 2021

Article published online:
12 February 2021

© 2021. Thieme. All rights reserved.

Georg Thieme Verlag KG
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