Abstract
Lipoxygenase (LOX) plays an important role in inflammatory processes and Arrabidaea brachypoda (DC.) Bureau (Bignoniaceae) has been described as presenting anti-inflammatory activity. Therefore, the objective of this study was to develop a high-performance liquid chromatography (HPLC) procedure to directly recognize LOX inhibitor compounds in A. brachypoda crude extract, facilitating the isolation, characterization of bioactive compounds, evaluation of natural compounds using an in vitro 15-LOX assay and prediction of the most probable binding modes of their main constituent through molecular docking simulations. The chemical analysis was performed by ethanol crude extract microfractionation using HPLC-DAD (diode array detector) associated to a fraction collector. The bioactive chromatogram displayed a peak with 50.9% LOX inhibition at 13.6 min retention time. The extract was purified and conandroside was isolated, presenting a LOX inhibitory activity with an inhibitory concentration (IC50) of 7.8 ± 1.1 µM, close to standard quercetin (IC50 7.6 ± 0.3 µM). Additionally, conandroside was not cytotoxic to normal cells (GM07492A). The LOX-conandroside complex displayed a slightly higher docking score (92.7) than quercetin (71.5). These results together suggest that conandroside could be explored as lipoxygenase inhibitor.
Highlights
Arrabidaea brachypoda (DC.) Bureau, synonym Fridericia platyphylla (Cham.) L.G
The bioactive ethanol crude extract (10.1 mg mL-1) was dissolved in methanol-water (5:95 v/v) and 1 mL was subjected to high-performance liquid chromatography (HPLC) on a semi-preparative C18 column in a
The analyses indicated that the conandroside is water-soluble, has low gastrointestinal absorption and is not BBB permeant
Summary
Lohmann, is found in the region of Brazilian Cerrado and is known as “cipó-una” and “cervejinha-do-campo” This species is commonly used in traditional medicine for treatment of kidney stones and painful joints.[1,2,3,4] Arrabidaea genus belongs to the Bignoniaceae family, which includes 800 species distributed from the south of United States of America to the north of Chile and Argentina.[5,6,7] Countless biological activities have been described for this genus, such as antiviral against human herpes virus 1 and Dengue virus 2, as well as healing, antimicrobial, anti-inflammatory, Lipoxygenases (LOXs) are dioxygenases that metabolize arachidonic acid during the inflammatory process, producing lipid mediators which are known as eicosanoids. Lipoxygenases have shown to possess specific roles in various human pathologies due to its central participation in leukotriene biosynthesis. Lipoxygenases and leukotrienes are involved in the pathogenesis of inflammatory diseases, such as asthma, rhinitis, rheumatoid arthritis, psoriasis, dermatitis, nephritis, atherosclerosis and cancer.[18]
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