Isolation of quinic acid derivatives and flavonoids from the aerial parts of Lactuca indica L. and their hepatoprotective activity in vitro

In our continuing study of biologically active compounds from Korean medicinal plants, we investigated the hepatoprotective constituents of the aerial parts of Lactuca indica L. (Compositae), since the methanolic extract of L. indica has hepatoprotective activity against hepatitis B virus (HBV) production. The bioactivity-guided separation of the methanolic extract of the aerial parts of L. indica resulted in the isolation of seven quinic acid derivatives (1, 3–4, 6, and 10–12), along with five flavonoids (2, 5, and 7–9). All the isolated compounds were evaluated for hepatoprotective activity by the HBV assay in vitro. In the human HBV-transfected liver cell line HepG2.2.15, all the compounds except 2 and 5 effectively reduced HBV DNA level in the release of mature HBV particles from HepG2.2.15 cultivation. Of the ten active compounds, treatment with 1, 3, and 12 led to significant reduction in the extracellular HBV DNA level, suggesting that they could be potent phytochemical agents against hepatitis B virus.

Graphical abstractBioactivity-guided column chromatographic separation of methanolic extract led to the isolation of three hepatoprotective quinic acids, 3,4-di-O-caffeoylquinic acid (1), 3,5-di-O-caffeoyl-muco-quinic acid (3), and 5-O-(E)-p-coumaroylquinic acid (12), along with four quinic acids and three flavonoids.Figure optionsDownload full-size imageDownload as PowerPoint slide