Abstract

In this study, we isolated from the aerial parts of Baccharis conferta Kunth (i) a new neoclerodane, denominated “bacchofertone”; (ii) four known terpenes: schensianol A, bacchofertin, kingidiol and oleanolic acid; and (iii) two flavonoids: cirsimaritin and hispidulin. All structures were identified by an exhaustive analysis of nuclear magnetic resonance (NMR) and mass spectroscopy (MS). Extracts from aerial parts were screened for anti-inflammatory activity in the mice ear edema model of 12-O-tetradecanoylforbol-13-acetate mice. Dichloromethane extract (BcD) exhibited 78.5 ± 0.72% inhibition of edema, followed by the BcD2 and BcD3 fractions of 71.4% and 82.9% respectively, at a dose of 1 mg/ear. Kingidiol and cirsimaritin were the most potent compounds identified, with a median effective dose of 0.12 and 0.16 mg/ear, respectively. A histological analysis showed that the topical application of TPA promoted intense cell infiltration, and this inflammatory parameter was reduced with the topical application of isolated compounds.

Highlights

  • Baccharis L. (Asteraceae) includes approximately 400 species that are distributed from USA to Argentina

  • Mouse ear edema induced by TPA has been used to test anti-inflammatory activity

  • (PKC) pathway, which results in elevated levels of eicosanoids such as prostaglandin E2 (PGE2 ) and leukotriene B4 (LTB4 )

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Summary

Introduction

Baccharis L. (Asteraceae) includes approximately 400 species that are distributed from USA to Argentina. (Asteraceae) includes approximately 400 species that are distributed from USA to Argentina. This genus is very relevant in folk medicine because many of these species have been used medicinally (e.g., to reduce phlegm, relieve cough, improve blood circulation, reduce pain, induce diuresis, as anthelmintic, anti-inflammatory and stomachic agents). 27 species of the genus Baccharis have been chemically investigated, and 139 compounds corresponding to flavonoids, triterpenes, cinnamic acids and diterpenoids have been isolated. Twenty-four diterpenoids have been reported, and 16 new terpenoids have been isolated, including seven neoclerodanes [1,2,3,4,5,6,7]. Hautriwaic acid, a neoclerodane diterpene, showed anti-inflammatory activity on two murine models: ear edema induced with

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