1.Lignans with NADPH Oxidase 2 (NOX2)-inhibitory Activity from the Fruits of Schisandra chinensis
Jung Min PARK ; Pisey PEL ; Young Won CHIN ; Moo Yeol LEE
Natural Product Sciences 2018;24(1):59-65
An isoform of NADPH oxidase (NOX), NOX2 is a superoxide-generating enzyme involved in diverse pathophysiological events. Although its potential as a therapeutic target has been validated, there is no clinically available inhibitor. Herein, NOX2-inhibitory activity was screened with the constituents isolated from Schisandra chinensis, which has been reported to have antioxidant and reactive oxygen species (ROS)-scavenging effects. Among the partitions prepared from crude methanolic extract, a chloroform-soluble partition showed the highest NOX2-inhibitory activity in PLB-985 cell-based NOX2 assay. A total of twenty nine compounds (1 – 29) were identified from the chloroform fraction, including two first isolated compounds; dimethyl-malate (25) and 2-(2-hydroxyacetyl) furan (27) from this plants. Of these constituents, two compounds (gomisin T, and pregomisin) exhibited an NOX2-inhibitory effect with the IC₅₀ of 9.4 ± 3.6, and 62.9 ± 11.3 µM, respectively. They are confirmed not to be nonspecific superoxide scavengers in a counter assay using a xanthine-xanthine oxidase system. These findings suggest the potential application of gomisin T (6) and other constituents of S. chinensis to inhibit NOX2.
Chloroform
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Fruit
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Lignans
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Methanol
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NADP
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NADPH Oxidase
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Oxidoreductases
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Reactive Oxygen Species
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Schisandra
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Superoxides
2.Chemical Constituents from Agrimonia pilosa with Inhibitory Activity against Interleukin 1β Production via NLRP3 and NLRC4 Inflammasomes
Piseth NHOEK ; Hee-Sung CHAE ; Chae-Yeong AN ; Pisey PEL ; Young-Mi KIM ; Young-Won CHIN
Natural Product Sciences 2021;27(4):228-233
Bioactivity-guided fractionation by preliminary screening using interleukin-1β production in lipopolysaccharides (LPS)-induced J774A.1 cell line led to the isolation of fourteen structures including chromone, isocoumarins, flavanoids, and triterpenes from the aerial part of Agrimonia pilosa Ledeb. All structures were determined by measuring their spectroscopic data and comparing their spectroscopic data with the literatures. All the isolates were tested for their inhibitory activities against interleukin-1β production in LPSinduced J774A.1 cell. Of the tested compounds, (S)-(+)-5,7-dihydroxy-2-(1-methylpropyl)chromone (1), agrimonolide-6-O-β-D-glucopyranoside (5), agrimonolide-6-O-α-L-arabinofuranosyl-(1→6)-β-D-glucopyranoside (6), and catechin (10) were found to be active. Furthermore, compound 1 suppressed the protein expressions of NLRP3 and NLRC4 in murine macrophage.
3.Benzoquinone Derivatives with Neuroprotective Activities from Lysimachia vulgaris L.
Chan-Woong PARK ; Jeonghoon LEE ; Pisey PEL ; Seung-Eun LEE ; Young-Won CHIN
Natural Product Sciences 2024;30(1):1-7
The ethyl acetate-soluble fraction of Lysimachia vulgaris , which was found to suppress β-amyloid production in Aβ-treated PC12 cells, was purified using various column chromatographies, resulting in the isolation of four known compounds, 2,4,6-triphenylhex-1-ene (1), pinoresinol (2), monomethyl embelin (3), and 2-hydroxy-5-methoxy-3-tridecyclohexa-2,5-diene-1,4-dione (4). The isolated compounds 3 and 4 downregulated P-tau production in Aβ-treated SH-SY5Y cells and demonstrated the inhibitory activities against NO production in lipopolysaccharide (LPS)-treated BV2 cells.