• 한국약용작물학회:학술대회논문집
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• 2011.04a
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• pp.94-95
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• 2011

• Bulletin of the Korean Chemical Society
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• v.31 no.1
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• pp.199-201
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• 2010

• Bulletin of the Korean Chemical Society
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• v.32 no.1
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• pp.319-320
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• 2011

• Bulletin of the Korean Chemical Society
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• v.31 no.12
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• pp.3800-3802
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• 2010

• Journal of Microbiology and Biotechnology
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• v.15 no.2
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• pp.269-273
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• 2005

Five dibenzylbutyrolactones were isolated from a methanol extract of Arctii fructus (Arctium lappa L.) by bioassay-guided isolation, using the interleukin-l $\beta$ converting enzyme (caspase-l, ICE) production inhibitory assay in vitro. These compounds were spectroscopically identified as lappaol E (1), lappaol A (2), matairesinol (3), arctigenin (4), and arctiin (5). Among the compounds tested, arctigenin (4) showed the strongest inhibitory activity for ICE production in IL-$\beta$-induced proliferation of D 1 OS cells. Western blot analysis demonstrated that the arctigenin suppressed the expression of ICE protein in a dose-dependent manner. To estimate the biotransformation of Arctii fructus in vivo by human intestinal bacteria, we carried out an anaerobic incubation of the Arctii fructus extract with a human fecal suspension. From the HPLC analysis of metabolites, Arctiin (IC$_{50}$=74.2$\mu$g/ml), a major component of Arctii fructus, was transformed to aglycone, arctigenin (IC$_{50}$=12.5$\mu$g/ml), by human intestinal bacteria. The ICE production inhibitory activity of Arctii fructus would be much stronger in vivo than in vitro due to the biotransformation by human intestinal bacteria.

• Natural Product Sciences
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• v.18 no.4
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• pp.273-278
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• 2012

Further phytochemical investigation on the whole plant of Thyrsanthera suborbicularis, collected in Cambodia, led to kaempferol (1), vitexin (2), apigenin-7-O-neohesperidoside (3), chrysoeriol-7-O-${\beta}$-D-glucopyranoside (4), isorhamnetin 3-O-rutinoside (5), kaempferol-3-O-[${\alpha}$-L-rhamnopyranosyl-(13)-${\alpha}$-L-rhamnopyranosyl-(16)-${\beta}$-D-galactopyranoside (6), kaempferol-3-O-${\alpha}$-L-rhamnopyranosyl(12)-O-[${\alpha}$-L-rhamnopyranosyl (16)]-${\beta}$-D-glucopyranoside (7), kaempferol-3-O-[6"-O-(E)-p-coumaroyl]-${\beta}$-D-glucopyranoside (8), kaempferol-3-O-[6"-O-(E)-p-coumaroyl]-${\beta}$-D-galactopyranoside (9), and amentoflavone (10). All the structures were confirmed by the interpretation of NMR (1D and 2D) and MS data, and comparison with the published values. Of the isolated compounds 1 - 10, compounds 8 and 10 displayed the inhibitory activity against NO production in LPS-induced Raw 264.7 cells with $IC_{50}$ values, 3.56 and $15.73{\mu}M$, respectively.

• IMMUNE NETWORK
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• v.13 no.1
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• pp.1-9
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• 2013

Autophagy is a fundamental cellular process in eukaryotic cells for maintaining homeostasis by degrading cellular proteins and organelles. Recently, the roles of autophagy have been expanded to immune systems, which in turn modulate innate immune responses. More specifically, autophagy acts as a direct effector for protection against pathogens, as well as a modulator of pathogen recognition and downstream signaling in innate immune responses. In addition, autophagy controls autoimmunity and inflammatory disorders by negative regulation of immune signaling. In this review, we focus on recent advances in the role of autophagy in innate immune systems.

• Journal of Microbiology and Biotechnology
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• v.15 no.3
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• pp.532-536
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• 2005

In the course of our screening for small molecules to inhibit apoptosis of U937 human leukemia cells induced by etoposide ($10\;{\mu}g/ml$), Penicillium sp. F020150 with potent inhibitory activity was selected. The active compound was purified from ethyl acetate extract of the microorganism by Sephadex LH-20 column chromatography and HPLC, and was identified as gentisyl alcohol (2,5-dihydroxybenzyl alcohol) by spectroscopic methods. The compound inhibited caspase-3 induction with $IC_{50}$ value of $3.0\;{\mu}g/ml$ after 8 h of etoposide treatment. The expression levels of caspase-3 and PARP were dose-dependently inhibited by the compound, suggesting that gentisyl alcohol inhibits etoposide-induced apoptosis via downregulation of caspases.

• Bulletin of the Korean Chemical Society
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• v.30 no.11
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• pp.2631-2636
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• 2009

JHL45, a novel immune modulator for anti-atopic dermatitis and allergic airway disease, was synthesized from decursin isolated from Angelica gigas. In order to conduct a pharmacokinetic study of JHL45, an analytical method, ideally one that uses a minimal amount of biological sample must first be validated. In this study, a HPLC-MS/MS method was developed and validated for the quantification of JHL45 and its major metabolite, (+)-decursinol, from 10 ${\mu}L$ of rat plasma. JHL45 was stable under the analysis conditions, and intra- and inter-day accuracies exceeded 90.06%, with a precision variability ${\leq}$ 13.16% for each analyte. The mean values for Cmax, AUC8h, half-life of JHL45 in rats after intravenous administration of 5 mg/kg JHL45 were 24.59 μg/mL, 10.02 ${\mu}g{\cdot}h/mL$, and 1.88 h, respectively. The validated method herein will be useful for further pharmacokinetic studies of JHL45, as well as in preclinical and clinical phases.

• Journal of Microbiology and Biotechnology
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• v.16 no.3
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• pp.475-479
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• 2006

Gentisyl alcohol isolated from Penicillium sp. has an antioxidative activity, protecting cells from oxidative stresses. From our in vitro angiogenesis assays with bovine aortic endothelial cells (BAECs), gentisyl alcohol was newly identified as a pro-angiogenic small molecule that induces new blood vessel formation of the cells. Gentisyl alcohol stimulated the proliferation of BAECs in a dose-dependent manner. Moreover, it induced in vitro angiogenesis of BAECs such as invasiveness, migration, and tube formation of the endothelial cells. Effects of gentisyl alcohol on invasion and tube formation were also dose-dependent. These results demonstrate that gentisyl alcohol could affect the angiogenic phenotypes of endothelial cells and be developed as a new small molecule with pro-angiogenic activity.