ABSTRACT
Artichoke (Cynara scolymus L.) is a perennial plant belonging to the Asteraceae family originating from the Mediterranean region. In Vietnam, there are some varieties of artichoke which are extensively cultivated and propagated in highland areas, however, there have been limited detailed scientific publications on the chemical composition and biological activity of artichoke grown in Vietnam. Therefore, this study provides a detailed description of the extraction, isolation, and structural determination of 20 natural secondary metabolites present in harvested artichoke. The antioxidant activity of the extract and the 9 isolated compounds are tested in 1,1-diphenyl-2-picrylhydrazyl radical scavenging and ex vivo malondialdehyde model. Among the selected compounds, 1-caffeoylquinic acid, 3-caffeoylquinic acid, chlorogenic acid, 4-caffeoylquinic acid, cynarin, 1,5-dicaffeoylquinic acid, 4,5-di-caffeoylquinic acid, cynaroside, and scolymoside exhibited strong radical scavenging activity with IC50 values ranging from 5.7 to 61.6 µM. In the malondialdehyde assay, 1,3-dicaffeoylquinic acid (or cynarin) showed the strongest activity with an IC50 value of 24.7 µM, followed by 1,5-di-caffeoylquinic acid (66.8 µM), and 4,5-di-caffeoylquinic acid (127.3 µM). This outcome contributes to establishing a database on the phytochemical and antioxidant activity of the Vietnamese artichoke.
ABSTRACT
In the present study, bioactivity-guided extraction and isolation of the n-hexane fraction of the fruits of Vietnamese Schisandra sphenanthera led to the isolation of five dibenzocyclooctadiene lignans as gomisin N (1), schisandrin C (2), gomisin H (3), gomisin D (4), and gomisin C (5). All the isolates were tested for their inhibition of NO production in LPS-induced RAW 264.7 cells. Among them, compounds 4 and 5 showed weak inhibition of NO production with IC 50 values of 25.0 ± 1.6 and 24.8 ± 2.0 µM, respectively. Compound 1 exhibited NO production inhibition with an IC 50 value of 15.8 ± 2.1 µM, meanwhile, schisandrin C (2) showed the most potent inhibition with an IC 50 value of 8.5 ± 0.5 µM. In addition, compound 2 had a concentrationdependent inhibitory effect on the protein expression of the inflammatory enzymes iNOS and COX-2. Their physicochemical properties and ADMET data were predicted by in silico, indicating favorable drug-like properties as well as low acute oral toxicity. The results suggest that the fruit of S. sphenanthera and its phytochemical constituents might be used as anti-inflammatory agents.