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Pel, Pisey,Chae, Hee-Sung,Nhoek, Piseth,Kim, Young-Mi,Chin, Young-Won American Chemical Society, Books and Journals Divi 2017 Journal of agricultural and food chemistry Vol.65 No.26
<P>Phytochemical investigation for a chloroform-soluble extract of dried Morus alba fruits, selected by proprotein convertase subtilisin-kexin type 9 (PCSK9) mRNA expression monitoring assay in HepG2 cells, led to the isolation of a new benzofuran, isomoracin D (1), and a naturally occurring compound, N-(N-benzoyl-L-phenylalanyl)-L-phenylalanol (2), along with 13 known compounds (3-15). All of the structures were established by NMR spectroscopic data as well as MS analysis. Of the isolates, moracin C (7) was found to inhibit PCSK9 mRNA expression with an IC50 value of 16.8 mu M in the HepG2 cells.</P>
Pel, Pisey,Chae, Hee-Sung,Nhoek, Piseth,Yeo, Woojin,Kim, Young-Mi,Chin, Young-Won Elsevier 2017 Phytochemistry Vol.136 No.-
<P><B>Abstract</B></P> <P>Bioactivity-guided fractionation of the fruits of <I>Schisandra chinensis</I>, using the proprotein convertase subtilisin-kexin type 9 (PCSK9) mRNA expression screening assay, led to isolation of two previously unknown lignans, 14-tigloylschinlignan D and <I>rel-</I>(7<I>R,</I> 8<I>R</I>, 7′<I>R</I>, 8′<I>R</I>)-manglisin E, along with 28 known compounds. All structures were established by NMR spectroscopic data as well as CD and MS analysis. All isolates were tested for their inhibitory activities on the mRNA expression of PCSK9. Of the tested compounds, four of the compounds <I>rel-</I>(7<I>R</I>, 8<I>R</I>, 7′<I>R</I>, 8′<I>R</I>)-manglisin E, (−)<B>-</B>schisandrin C, schinlignan D, and (+)-schisandrol B potently inhibited PCSK9 mRNA expression with IC<SUB>50</SUB> values of 3.15, 3.85, 0.36, and 1.10 μM, respectively. Furthermore, schinlignan D and (+)-schisandrol B were found to suppress PCSK9 protein expressions and schinlignan D deemed to increase low density lipoprotein receptor expression.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Fruits of <I>Schisandra chinensis</I> inhibited PCSK9 mRNA expression. </LI> <LI> 14-tigloylschinlignan D and <I>rel-</I>(7<I>R,</I> 8<I>R</I>, 7′<I>R</I>, 8′<I>R</I>)-manglisin E were identified. </LI> <LI> Four lignans potently inhibited PCSK9 mRNA expression. </LI> <LI> Schinlignan D suppressed PCSK9 protein and increased LDLR expression. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>Two lignans along with 28 known compounds were isolated and four lignans potently inhibited PCSK9 mRNA expression.</P> <P>[DISPLAY OMISSION]</P>
Lignans with NADPH Oxidase 2 (NOX2)-inhibitory Activity from the Fruits of Schisandra chinensis
박정민,Pisey Pel,진영원,이무열 한국생약학회 2018 Natural Product Sciences Vol.24 No.1
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 mM, 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.
Piseth Nhoek,채희성,안채영,Pisey Pel,김영미,진영원 한국생약학회 2021 Natural Product Sciences Vol.27 No.4
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 LPS-induced 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.