VII Simposio Internacional de Ciencias Farmacéuticas 2019 "VII SICF" -IV Simposio Internacional "Química de los productos naturales"

VII Simposio Internacional de Ciencias Farmacéuticas 2019

VII SICF

IV Simposio Internacional "Química de los productos naturales"

BIOASSAY-FRACTIONATION EVALUATION OF ANTIPROTOZOAL ACTIVITY OF THE LEAVES OF CROTON LINEARIS JACQ.

Resumen [ES]

Leaves of Croton linearis, known as “rosemary”, are widely used in folk medicine in Caribbean countries to treat fever and colds (associated to infections), that’s why in the present work we accomplish to evaluate the in vitro antimicrobial activity of extracts and fractions derived from C. linearis leaves. Bioassay-guided fractionation and isolation of compounds from an ethanolic extract of C. linearis, using flash chromatography and semi-preparative HPLC-DAD-MS (High Performance Liquid Chromatography – Diode Array Detection – Mass Spectrometry). Isolated compounds were characterized by MS and 1D and 2D NMR (Nuclear Magnetic Resonance) spectroscopy. The microdilution method with resazurin, as well as direct counting in optical microscopes, were used to determine the in vitro antimicrobial activity against bacteria, fungi and parasites. Moreover, the cytotoxicity on three cell lines (human fetal lung fibroblasts (MRC-5), RAW 264.7 (murine macrophages) and Vero cells) was evaluated. The total extract and chloroform fraction (Cl-F) showed high activity against protozoa with IC50 values ranging from 1 to 26 µg/mL. Seven compounds were isolated and characterized for first time in this medicinal plant: the alkaloids laudanidine, laudanosine, reticuline, corydine, glaucine and cularine and the flavonoid glycoside isorhamnetin-3-O-(6''-O-p-trans-coumaroyl)-β-glucopyranoside. Reticuline showed a weak activity against L. infantum (IC50=148.0 ± 1.2 µM), while the flavonoid was active against T. cruzi (IC50=35.6 ± 2.3 µM). This study is a first pharmacological exploration on the leaves of C. linearis. The results show the antiprotozoal potential of the extract and some isolated constituents, which supports the use of this species in Caribbean folk medicine.

Resumen [EN]

Leaves of Croton linearis, known as “rosemary”, are widely used in folk medicine in Caribbean countries to treat fever and colds (associated to infections), that’s why in the present work we accomplish to evaluate the in vitro antimicrobial activity of extracts and fractions derived from C. linearis leaves. Bioassay-guided fractionation and isolation of compounds from an ethanolic extract of C. linearis, using flash chromatography and semi-preparative HPLC-DAD-MS (High Performance Liquid Chromatography – Diode Array Detection – Mass Spectrometry). Isolated compounds were characterized by MS and 1D and 2D NMR (Nuclear Magnetic Resonance) spectroscopy. The microdilution method with resazurin, as well as direct counting in optical microscopes, were used to determine the in vitro antimicrobial activity against bacteria, fungi and parasites. Moreover, the cytotoxicity on three cell lines (human fetal lung fibroblasts (MRC-5), RAW 264.7 (murine macrophages) and Vero cells) was evaluated. The total extract and chloroform fraction (Cl-F) showed high activity against protozoa with IC50 values ranging from 1 to 26 µg/mL. Seven compounds were isolated and characterized for first time in this medicinal plant: the alkaloids laudanidine, laudanosine, reticuline, corydine, glaucine and cularine and the flavonoid glycoside isorhamnetin-3-O-(6''-O-p-trans-coumaroyl)-β-glucopyranoside. Reticuline showed a weak activity against L. infantum (IC50=148.0 ± 1.2 µM), while the flavonoid was active against T. cruzi (IC50=35.6 ± 2.3 µM). This study is a first pharmacological exploration on the leaves of C. linearis. The results show the antiprotozoal potential of the extract and some isolated constituents, which supports the use of this species in Caribbean folk medicine.

Sobre el ponente

Jesús García Díaz

Dr. Jesús García Díaz

University of Oriente Flag of Cuba

Profesor de la Universidad de Oriente

Información Práctica
Ponencia
English (US)
junio 26, 2019 10:40 a. m.
20 minutos
Restaurante "El Tesico"
Autores
Emmy Tuenter
Gabriel Llauradó
Luc Pieters
Dr. Jesús García Díaz
Paul Cos
Julio Cesar Escalona
Palabras clave
antimicrobial
bioassay-guided isolation
croton linearis
cytotoxicity
isoquinoline alkaloids