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Six compounds were isolated from an ethanol extract of Swertia mussotii and identified as 2-phenylethyl-β-D-glucoside (1), amaroswerin (2), 1,3,7,8-tetrahydroxyxanthone (3), swertiamarine (4), 1,3,8-trihydroxy-5-methoxyxanthone (5) and methylswertianin (6). Compounds 1, 2 and 6 were isolated from S. mussotii for the first time. The anti-inflammatory activities of the compounds were evaluated by determining their effect on the production of NO by LPS-stimulated RAW264.7 cells. Amaroswerin was the most potent inhibitor of NO release, with an IC50 value of 5.42 μg/mL. Treatment with amaroswerin inhibited expression of iNOS at both protein and mRNA levels. Amaroswerin also dose-dependently suppressed production of TNF-α, IL-6 and IL-1β and reduced expression of mRNA for these LPS-stimulated pro-inflammatory mediators. Amaroswerin thus inhibits the expression of iNOS, TNF-α, IL-6 and IL-1β by downregulating transcription in LPS-induced RAW264.7 macrophage cells, indicating that amaroswerin may be a valuable therapeutic agent for the treatment of inflammatory diseases.

Antioxidant potencies of an ethanolic extract and its components from Lepidium latifolium were investigated. In this study, we found that the ethyl acetate soluble fraction of L. latifolium was a rich source of antioxidant, resulting from its high total phenolic content. To determine the antioxidant components of the ethyl acetate fraction, a bioassay-guided fractionation approach using 1,1-diphenyl-2-picrylhydrazyl, 2,2′-azinobis-(3-ethylbenzthiazoline-6-sulfonate), and ferric reducing antioxidant power assays were conducted. Nine compounds were isolated and their structures were identified by MS and NMR spectral data and comparison to reported data. They are Quercetin-3-O-β-d-sophoroside-7-O-α-l-rhamnoside (1), Apetalumoside B6 (2), Kaempferol-3-O-β-d-glucopyranosyl-(1-2)-β-d-glucopyranoside-7-O-β-d-glucopyranoside (3), Kaempferol-7-O-α-l-rhamnopyranoside (4), Kaempferol-3-O-β-d-glucopyranoside-7-O-α-l-rhamnopyranoside (5), Kaempferol-3-O-(2-O-feruloyl-β-d-glucopyranosyl-(1-2)-β-d-glucopyranoside)-7-O-glucopyranoside (6), Kaempferol-3-O-β-d-sophoroside-7-O-α-l-rhamnoside (7), Kaempferol-3-O-robinoside-7-O-(2″″-(E)-feruloyl)-sophoroside (8), Quercetin-3-O-(2,6-di-O-β-d-glucopyranosyl)-β-d-glucopyranoside-7-O-α-l-rhamnopyranoside (9), compounds 1, 2, 4, and 8 had potent free radical scavenging activity. The IC50 values of these compounds were 9.8–12.3 and 7.4–31.4 μg/mL in DPPH and ABTS assays, respectively. The results indicate that L. latifolium is a potential natural source of antioxidants to treat several diseases related to oxidant by-products of human metabolism.

The aim of the present study was to evaluate the antiproliferative effect of phenylpropanoids isolated from the n-BuOH-soluble fraction of an ethanolic extract of Lagotis brevituba Maxim. The phenylpropanoids were identified as echinacoside, lagotioside, glucopyranosyl(1-6)martynoside, plantamoside, and verbascoside. Three of the compounds, lagotioside, glucopyranosyl(1-6)martynoside, and plantamoside, were isolated from L. brevituba for the first time. The antiproliferative activity of the isolates was evaluated in human gastric carcinoma (MGC-803), human colorectal carcinoma (HCT116), human hepatocellar carcinoma (HepG2), and human lung cancer (HCT116) cells using an 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Plantamoside showed promising activity against MGC-803 cells, with a half maximal inhibitory concentration value of 37.09 μM. The mechanism of the pro-apoptosis effect of plantamoside was then evaluated in MGC-803 cells. Changes in cell morphology, including disorganization of the architecture of actin microfilaments and formation of apoptotic bodies, together with cell cycle arrest in G2/M phases, were observed after treatment of plantamoside. The antiproliferative and pro-apoptotic effects were associated with a decrease in the ratio of Bcl-2/Bax and reduced mitochondrial membrane potential, which was accompanied by the release of reactive oxygen species and Ca2+ into the cytoplasm. Taken together, the results indicated that plantamoside promotes apoptosis via a mitochondria-dependent mechanism. Copyright © 2017 John Wiley & Sons, Ltd.