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

Nathalya Tesch Brazil; Bruna Medeiros-Neves; Flávia Nathiely Silveira Fachel; Vanessa Pittol; Roselena Silvestri Schuh; Graziela Vargas Rigo; Tiana Tasca; Gilsane Lino von Poser; Helder Ferreira Teixeira

doi:10.1055/a-1373-6074

Planta Medica, Inhaltsverzeichnis

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

¹Faculdade 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

¹Faculdade 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

¹Faculdade 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

¹Faculdade 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

¹Faculdade de Farmácia, Programa de Pós Graduação em Ciências Farmacêuticas (PPGCF), Universidade Federal do Rio Grande do Sul (UFRGS), Santana, Porto Alegre, RS, Brazil

²Centro de Pesquisa Experimental, Laboratório Células, Tecidos e Genes, Hospital de Clínicas de Porto Alegre (HCPA), Santa Cecília, Porto Alegre, RS, Brazil

,

Graziela Vargas Rigo

¹Faculdade 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

¹Faculdade 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

¹Faculdade 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

¹Faculdade de Farmácia, Programa de Pós Graduação em Ciências Farmacêuticas (PPGCF), Universidade Federal do Rio Grande do Sul (UFRGS), Santana, Porto Alegre, RS, Brazil

› Institutsangaben

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

Volltext

Referenzen

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