Abstract
In the current study, two new flavones, 4′-O-geranyltricin (1) and 3′-O-geranylpolloin (2), and a new 2-(2-phenylethyl)-4H-chromen-4-one derivative, 7-hydroxyl-6-methoxy-2-(2-phenylethyl)chromone (3), have been isolated from the stem barks of A. sinensis, together with 21 known compounds 4–24. The structures of new compounds 1–3 were determined through spectroscopic and MS analyses. Compounds 2, 3, 5, 6, and 8–10 exhibited inhibition (IC50 ≤ 12.51 μM) of superoxide anion generation by human neutrophils in response to formyl-l-methionyl-l-leucyl-l-phenylalanine/cytochalasin B (fMLP/CB). Compounds 3, 6, 8, 10, and 19 inhibited fMLP/CB-induced elastase release with IC50 values ≤ 15.25 μM. This investigation reveals bioactive isolates (especially 2, 3, 5, 6, 8, 9, 10, and 19) could be further developed as potential candidates for the treatment or prevention of various inflammatory diseases.
Highlights
Aquilaria sinensis (Lour.) Gilg. (Thymelaeaceae) is an evergreen tree, distributed in southern China [1]
The effects on neutrophil pro-inflammatory responses of compounds isolated from the stem barks of A. sinensis were evaluated by suppressing fMet-Leu-Phe/ cytochalasin B-induced superoxide anion (O2‚ ́) generation and elastase release by human neutrophils
Granule proteases and reactive oxygen species (ROS) e.g., superoxide anion (O2‚ ́), hydrogen peroxide] and produced by human neutrophils contribute to the pathogenesis of inflammatory diseases
Summary
Aquilaria sinensis (Lour.) Gilg. (Thymelaeaceae) is an evergreen tree, distributed in southern China [1]. The effects on neutrophil pro-inflammatory responses of compounds isolated from the stem barks of A. sinensis were evaluated by suppressing fMet-Leu-Phe/ cytochalasin B (fMLP/CB)-induced superoxide anion (O2‚ ́) generation and elastase release by human neutrophils. From the results of our biological tests, the following conclusions can be drawn: (a) 31-O-Geranylpolloin (2), 7-hydroxy-6methoxy-2-(2-phenylethyl)chromone (3), 5-hydroxy-7,31,41-trimethoxyflavone (5), velutin (6), 31-hydroxygenkwanin (8), sakuranetin (9), and 6,7-dimethoxy-2-(2-phenylethyl)chromone (10) exhibited potent inhibition (IC50 ď 12.51 μM) of superoxide anion (O2‚ ́) generation by human neutrophils in response to fMLP/CB; (b) 7-hydroxy-6-methoxy-2-(2-phenylethyl)chromone (3), velutin (6), sakuranetin (9), 6,7-dimethoxy-2-(2-phenylethyl)chromone (10), and ergosta-4,6,8(14)-. Velutin (6) were the most effective among the isolated compounds, with IC50 values of 1.74 ̆ 0.17 and 1.78 ̆ 0.35 μM, against fMLP-induced superoxide anion generation; (g) 7-hydroxy6-methoxy-2-(2-phenylethyl)chromone (3), velutin (6), and 31-hydroxygenkwanin (8) were the most effective among the isolated compounds, with IC50 value of 3.91 ̆ 0.87, 4.26 ̆ 0.12, and 4.56 ̆ 0.63 μM, against fMLP-induced elastase release
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