Anti-inflammatory effects in muscle injury by transdermal application of gel with Lychnophora pinaster aerial parts using phonophoresis in rats.

BACKGROUND: Lycnophora pinaster is used by the traditional Brazilian medicine for the treatment of inflammations. Anti-inflammatory activity of Lycnophora pinaster was investigated for extracts, fractions, and isolated compounds of their aerial parts. The hexane extract (HE) provided α-amyrin, lupeol, mixture of α-amyrin and lupeol, mixture of 3-O-acetyl-lupeol and 3-O-acetyl-pseudotaraxasterol, and mixture of the steroids stigmasterol and sitosterol. The aqueous extract (WE) provided a fraction containing alkaloids (AF) and another one containing phenolic compounds (PF). METHODS: The crude hexane extract obtained from aerial parts of L. pinaster was submitted to chromatographic fractionation. The fractionation of PF was performed by preparative HPLC analysis, providing the flavonoid quercetin. The extracts, fractions, and compounds isolated from L. pinaster were tested to evaluate the anti-inflammatory activity by experimental model of impact injury, followed by transdermal application of gels with these samples. The application of the gels was performed using phonophoresis in rat paws after induction of muscle injury. Histological analysis was based on scores assigned by the capacity of decreasing the lesion. RESULTS: HE and WE exhibited anti-inflammatory activity. Some fractions, triterpenes, and steroids also reduced the inflammatory infiltrates caused by muscle injury. Lupeol promoted a significant reduction of inflammation. Quercetin also provided significant results, promoting the greatest decreases in muscle injury. CONCLUSION: The results of this work suggest that topical application of triterpenes, steroids and flavonoid significantly decreases the inflammatory process generated by muscle injury. The transdermal application using phonophoresis in rat paws of gel with lupeol and quercetin attenuates the inflammation.

Evaluation of the bactericidal and trypanocidal activities of triterpenes isolated from the leaves, stems, and flowers of Lychnophora pinaster

The phytochemical investigation on the aereal parts of Lychnophora pinaster Mart., Asteraceae, was carried to isolation of triterpenes. 3-O-Acetyl-lupeol (1), 3-O-acetyl-pseudotaraxasterol (2), and 3-O-acetyl-α-amyrin (3) were isolated from hexanic extract and 4,4-dimethyl-cholesta-22,24-dien-5-ol (4), α-amyrin (5), and lupeol (6) were isolated from hexanic/dichlorometanic extract of the leaves. Compounds Δ7-bauerenyl acetate (7), friedelin (8), stigmasterol (9), and sitosterol (10) were isolated from the hexanic/dichlorometanic extract of the stems. The steroids 9 and 10 were also isolated from the hexanic/dichlorometanic extract of the flowers. Triterpenes 1, 3, 4, and 7 are described for the first time in the genus Lychnophora. The apolar fractions of the leaf and stem extracts and some isolated triterpenes showed low trypanocidal activity. Moreover, apolar fractions of the leaf and stem extracts and 5 showed antibacterial action against Staphylococcus aureus.