Abstract
Tabernaemontana catharinensis (Apocynaceae) has been popularly used by folk medicine because of its anti-inflammatory, analgesic, and antiophidic properties. This study aims to analyze the flavonoids composition of the hydroethanolic extract and of the ethyl acetate (EtOAc) and butanol (BuOH) fractions of T. catharinensis leaves, as well as to evaluate their anti-inflammatory activity using in vivo models. The phytochemical profile, determined by High-Performance Liquid Chromatography–High-Resolution Electrospray Ionization-Mass Spectrometry (HPLC–HRESI-MS), showed the presence of flavonoids mainly having an isorhamnetin nucleus. The anti-inflammatory activity was evaluated in carrageenan-induced paw edema (pre- and post-treatment) with oral administration of a T. catharinensis hydroethanolic extract (50, 100, and 150 mg/kg) and of organic fractions (50 mg/kg). The extract and fractions showed antiedematogenic activity by decreasing myeloperoxidase (MPO) production. In the zymosan-air-pouch model, the extract and fractions inhibited leukocyte migration and significantly decreased the levels of various proteins, such as MPO, interleukin (IL)-1β, and tumor necrosis factor (TNF)-α. The cytotoxicity was evaluated by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, which revealed no cytotoxicity of the extract and the fractions. These results suggest that the hydroethanolic extract and organic fractions of T. catharinensis leaves have sufficient anti-inflammatory activity to support the popular use of this plant in the treatment of inflammatory disorders.
Highlights
Inflammation is a complex biological process that involves several vascular and cellular mechanisms
Thin-layer chromatography (TLC) analysis of the hydroethanolic extract and fractions of T. catharinensis leaves showed a wide variety of flavonoids
Since there are several reports in the literature describing the anti-inflammatory activity of flavonoids [22], and considering that our Thin-Layer Chromatography (TLC) analysis indicated the presence of flavonoids in the hydroethanolic extract of T. catharinensis
Summary
Inflammation is a complex biological process that involves several vascular and cellular mechanisms. The treatment of inflammatory disorders usually consists of administering nonsteroidal anti-inflammatory drugs (NSAIDs) and, in specific cases, anti-inflammatory steroids. The chronic use of steroids and NSAIDs is associated with severe side effects, such as gastric or intestinal ulceration, kidney disorders, edema, sodium retention, and arterial hypertension [5,6]. Several anti-inflammatory drugs were derived from the secondary metabolites of phenolic compounds, such as flavonoids [9]. The anti-inflammatory mechanism of action of phenolic compounds and flavonoids involves the inhibition of inflammatory mediators, such as inducible nitric oxide synthase (iNOS), cyclooxygenase (COX-2), and the cytokines IL-1β, TNF-α, and IL-10 [10]
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