Wound healing activity of Tropaeolum tuberosum-based topical formulations in mice.

Background and Aim: Tropaeolum tuberosum Ruiz and Pavón, a tuber native to South America, is characterized by its antioxidant, antimicrobial, and anti-inflammatory properties that contribute to wound healing. This study aimed to evaluate the healing effect of the topical T. tuberosum formulations (gel and cream) on induced wounds in mice. Materials and Methods: Here, an acidic ethanolic extract (1.5 N hydrochloric acid and 96% ethanol at the ratio of 15:85, v/v) was prepared with the tubers of T. tuberosum ecotype black and incorporated into topical cream and gel formulations at 1%. Thirty-twoBalb/c mice were divided into four experimental groups receiving daily topical treatments for 14 days: Group I (control; no treatment), Group II (a commercial ointment of neomycin, polymyxin B, and bacitracin), Group III (1% T. tuberosum gel), and Group IV (1% T. tuberosum cream). The wound closure in the mice was determined during the treatment; then, they were euthanized to obtain skin samples for histopathological analysis. Results: Groups III and IV showed a higher percentage of wound closure from the 6th day of the treatment. From the 8th day, the effect was greater in Group III. The healing effect was confirmed by the histopathological changes. Conclusion: This study concludes that the topical formulations of T. tuberosum demonstrate wound-healing activity in mice, and the most effective treatment is the 1% gel formulation.

[Identification and structural determination of a sesquiterpene of Tessaria integrifolia Ruiz & Pav. leaves and evaluation of its leishmanicidal activity]. / Identificación y determinación estructural de un sesquiterpeno de las hojas de Tessaria integrifolia Ruiz & Pav. y evaluación de su actividad leishmanicida.

OBJECTIVE.: To identify and determine the phytoconstituent structure of Tessaria integrifolia Ruiz & Pav. leaves with leishmanicidal activity. MATERIALS AND METHODS.: Fluid extract of leaves was prepared, concentrated to soft extract, and used to evaluate leishmanicidal activity in Mesocricetus auratus with experimental leishmaniasis, at the dose of 250 mg/kg of soft extract by intramuscular route for 15 days. Extract was fractionated in 45 cm column chromatography with a 2.5 cm diameter, containing G-60 silica gel, and 70-230 mesh (Sigma-Aldrich®). Nine fractions were obtained and assessed on macrophages infected with Leishmania sp to determine the active fraction and isolate the active compound, by separation, purification, and crystallization, analyzed by nuclear magnetic resonance (NMR) of 1H, 13C, and liquid chromatography coupled to mass spectroscopy (LC/ MS). RESULTS.: Fluid extract from the leaves of T. integrifolia presents leishmanicidal activity in M. auratus. Fraction F8 is active on infected macrophages at a dose of 14 µg/mL. An eudesman type sesquiterpene ((4aS, 5R, 6R, 8aR) -6-hydroxy-5, 8a-dimethyl-3- (1-methylethylidene) octahydronaphthalen-2 (1H) -one) was identified, by RMN 1 H, 13C, and LC / MS analysis. CONCLUSIONS.: Fluid extract of leaves of Tessaria integrifolia Ruiz & Pav. presents leishmanicidal activity on Mesocricetus auratus with experimental leishmaniasis. Fraction F8 presents leishmanicidal activity on infected macrophages at a dose of 14 µg/mL. An eudesman type sesquiterpene was identified, according to 1 H, 13C, and LC / MS NMR analysis.

OBJETIVOS.: Identificar y determinar la estructura del fitoconstituyente de hojas de Tessaria integrifolia Ruiz & Pav con efecto leishmanicida. MATERIALES Y MÉTODOS.: Se preparó un extracto fluido de hojas de Tessaria integrifolia Ruiz & Pav. que fue concentrado a extracto blando y se utilizó para evaluar la actividad leishmanicida en Mesocricetus auratus con leishmaniasis experimental, administrando vía intramuscular la dosis de 250 mg/kg del extracto blando por 15 días. El extracto fue fraccionado en columna cromatográfica de 45 cm, con un diámetro de 2,5 cm que contiene silicagel G-60, de 70-230 mesh (Sigma-Aldrich®), las nueve fracciones obtenidas fueron evaluadas sobre macrófagos infectados con Leishmania sp para determinar la fracción activa y aislar el compuesto activo, mediante separación, purificación y cristalización, siendo analizado por resonancia magnética nuclear (RMN) de 1H, 13C, y cromatografía líquida acoplada a espectroscopía de masas (LC/MS). RESULTADOS.: El extracto fluido de las hojas de Tessaria integrifolia Ruiz & Pav. presenta actividad leishmanicida en Mesocricetus auratus y la fracción F8 es activa sobre macrófagos infectados a dosis de 14 µg/mL. Se elucidó en esa fracción un sesquiterpeno tipo eudesmano ((4aS, 5R,6R,8aR)-6-hidroxi-5,8a-dimetil-3-(1-metiletiliden) octahidronaftalen-2(1H)-ona), según análisis de RMN 1H, 13C, y LC/MS. CONCLUSIONES.: El extracto fluido de hojas de Tessaria integrifolia Ruiz & Pav. presenta actividad leishmanicida sobre Mesocricetus auratus. La fracción F8 presenta actividad leishmanicida sobre macrófagos infectados a dosis de 14 µg/mL. Se elucidó en la fracción activa un sesquiterpeno tipo eudesmano según los análisis de RMN 1H, 13C, y LC/MS.

Identificación y determinación estructural de un sesquiterpeno de las hojas de Tessaria integrifolia Ruiz & Pav. y evaluación de su actividad leishmanicida / Identification and structural determination of a sesquiterpene of Tessaria integrifolia Ruiz & Pav. leaves and evaluation of its leishmanicidal activity

RESUMEN Objetivos. Identificar y determinar la estructura del fitoconstituyente de hojas de Tessaria integrifolia Ruiz & Pav con efecto leishmanicida. Materiales y métodos. Se preparó un extracto fluido de hojas de Tessaria integrifolia Ruiz & Pav. que fue concentrado a extracto blando y se utilizó para evaluar la actividad leishmanicida en Mesocricetus auratus con leishmaniasis experimental, administrando vía intramuscular la dosis de 250 mg/kg del extracto blando por 15 días. El extracto fue fraccionado en columna cromatográfica de 45 cm, con un diámetro de 2,5 cm que contiene silicagel G-60, de 70-230 mesh (Sigma-Aldrich®), las nueve fracciones obtenidas fueron evaluadas sobre macrófagos infectados con Leishmania sp para determinar la fracción activa y aislar el compuesto activo, mediante separación, purificación y cristalización, siendo analizado por resonancia magnética nuclear (RMN) de 1H, 13C, y cromatografía líquida acoplada a espectroscopía de masas (LC/MS). Resultados. El extracto fluido de las hojas de Tessaria integrifolia Ruiz & Pav. presenta actividad leishmanicida en Mesocricetus auratus y la fracción F8 es activa sobre macrófagos infectados a dosis de 14 µg/mL. Se elucidó en esa fracción un sesquiterpeno tipo eudesmano ((4aS, 5R,6R,8aR)-6-hidroxi-5,8a-dimetil-3-(1-metiletiliden) octahidronaftalen-2(1H)-ona), según análisis de RMN 1H, 13C, y LC/MS. Conclusiones. El extracto fluido de hojas de Tessaria integrifolia Ruiz & Pav. presenta actividad leishmanicida sobre Mesocricetus auratus. La fracción F8 presenta actividad leishmanicida sobre macrófagos infectados a dosis de 14 µg/mL. Se elucidó en la fracción activa un sesquiterpeno tipo eudesmano según los análisis de RMN 1H, 13C, y LC/MS.

ABSTRACT Objective. To identify and determine the phytoconstituent structure of Tessaria integrifolia Ruiz & Pav. leaves with leishmanicidal activity. Materials and Methods. Fluid extract of leaves was prepared, concentrated to soft extract, and used to evaluate leishmanicidal activity in Mesocricetus auratus with experimental leishmaniasis, at the dose of 250 mg/kg of soft extract by intramuscular route for 15 days. Extract was fractionated in 45 cm column chromatography with a 2.5 cm diameter, containing G-60 silica gel, and 70-230 mesh (Sigma-Aldrich®). Nine fractions were obtained and assessed on macrophages infected with Leishmania sp to determine the active fraction and isolate the active compound, by separation, purification, and crystallization, analyzed by nuclear magnetic resonance (NMR) of 1H, 13C, and liquid chromatography coupled to mass spectroscopy (LC/ MS). Results. Fluid extract from the leaves of T. integrifolia presents leishmanicidal activity in M. auratus. Fraction F8 is active on infected macrophages at a dose of 14 μg/mL. An eudesman type sesquiterpene ((4aS, 5R, 6R, 8aR) -6-hydroxy-5, 8a-dimethyl-3- (1-methylethylidene) octahydronaphthalen-2 (1H) -one) was identified, by RMN 1 H, 13C, and LC / MS analysis. Conclusions. Fluid extract of leaves of Tessaria integrifolia Ruiz & Pav. presents leishmanicidal activity on Mesocricetus auratus with experimental leishmaniasis. Fraction F8 presents leishmanicidal activity on infected macrophages at a dose of 14 μg/mL. An eudesman type sesquiterpene was identified, according to 1 H, 13C, and LC / MS NMR analysis.