Bioactivity-guided isolation of antioxidant and anti-hepatocarcinoma constituents from Veronica ciliata Iridoid glycosides, Bioactivity-guided screening

Background: Veronica ciliata Fisch., widely distributed in western China, has been traditionally used in Tibetan Medicine as a treatment for hepatitis, cholecystitis, rheumatism, and urticaria. However, V. ciliata Fisch. has not been subjected to detailed chemical constitution analysis and the bioactive studies were restricted to its crude extracts. It is necessary to investigate the active chemical components of these extracts and identify their biological effects. Results: Four iridoid glycosides, (veronicoside, cataposide, amphicoside, and verminoside) were isolated from the ethyl acetate fraction. Among these compounds, veronicoside and verminoside were isolated for the first time from this plant. These compounds exhibited strong antioxidant activity and inhibitory activity on HepG2 cell proliferation. The antioxidant activity of verminoside was equal to Vc. Cataposide, amphicoside and verminoside had stronger antihepatocarcinoma activity than 5-fluorouracil. Conclusions: Four iridoid glycosides,(veronicoside, cataposide, amphicoside and verminoside) were isolated from the extract of V. ciliata Fisch. using bioassay-guided screening.Among these compounds, veronicoside and verminoside were isolated for the first time from this plant. The above results indicated that these compounds were the active chemical components responsible for the antioxidant and anti-hepatocarcinoma properties of V. ciliata Fisch. The underlying mechanism of their bioactivity is worthy of further investigation.