Arctigenin from Arctium lappa inhibits interleukin-2 and interferon gene expression in primary human T lymphocytes

<p>Abstract</p> <p>Background</p> <p><it>Arctium lappa </it>(<it>Niubang</it>), a Chinese herbal medicine, is used to treat tissue inflammation. This study investigates the effects of arctigenin (AC), isolated from <it>A. lappa</it>, on anti-CD3/CD28 Ab-stimulated cell proliferation and cytokine gene expression in primary human T lymphocytes.</p> <p>Methods</p> <p>Cell proliferation was determined with enzyme immunoassays and the tritiated thymidine uptake method. Cytokine production and gene expression were analyzed with reverse transcription-polymerase chain reaction.</p> <p>Results</p> <p>AC inhibited primary human T lymphocytes proliferation activated by anti-CD3/CD28 Ab. Cell viability test indicated that the inhibitory effects of AC on primary human T lymphocyte proliferation were not due to direct cytotoxicity. AC suppressed interleukin-2 (IL-2) and interferon-γ (IFN-γ) production in a concentration-dependent manner. Furthermore, AC decreased the IL-2 and IFN-γ gene expression in primary human T lymphocytes induced by anti-CD3/CD28 Ab. Reporter gene analyses revealed that AC decreased NF-AT-mediated reporter gene expression.</p> <p>Conclusion</p> <p>AC inhibited T lymphocyte proliferation and decreased the gene expression of IL-2, IFN-γ and NF-AT.</p

Assessing the skin-whitening property of plant extracts from taiwanese species using zebrafish as a rapid screening platform

Zebrafish can be used as a phenotype-based fast-screening platform for the discovery of skin-whitening products by observing the formation of melanin in vivo through a dissecting microscope. In this study, we first evaluated commercial whitening ingredients to confirm the potency of the zebrafish model. The zebrafish screening system verified that verbascoside and 5 other commonly used commercial skin-whitening compounds– including sodium ascorbate, azelaic acid, transamin, kojic acid, and PTU- significantly reduce melanin content in a dose-dependent manner. We subsequently conducted preliminary screening of 123 natural sources to identify those with whitening property. Through a two-step screening process, anti-melanogenesis effects of 4 and 9 candidates at low and high concentration were verified respectively. The toxicity, mortality, and malformation of zebrafish embryo were also evaluated. We further investigated the components of C. manghas L. and found 6 major compounds, one of which was manghaslin, a compound known for its melanin-suppressing effect on zebrafish without cytotoxicity. With these properties, manghaslin is a promising candidate as a skin lightening agent or a treatment for melanoma

Melanogenesis Inhibitors from the Rhizoma of <i>Ligusticum Sinense</i> in B16-F10 Melanoma Cells In Vitro and Zebrafish In Vivo

The rhizoma of Ligusticum sinense, a Chinese medicinal plant, has long been used as a cosmetic for the whitening and hydrating of the skin in ancient China. In order to investigate the antimelanogenic components of the rhizoma of L. sinense, we performed an antimelanogenesis assay-guided purification using semi-preparative HPLC accompanied with spectroscopic analysis to determine the active components. Based on the bioassay-guided method, 24 compounds were isolated and identified from the ethyl acetate layer of methanolic extracts of L. sinense, and among these, 5-[3-(4-hydroxy-3-methoxyphenyl)allyl]ferulic acid (1) and cis-4-pentylcyclohex-3-ene-1,2-diol (2) were new compounds. All the pure isolates were subjected to antimelanogenesis assay using murine melanoma B16-F10 cells. Compound 1 and (3S,3aR)-neocnidilide (8) exhibited antimelanogenesis activities with IC50 values of 78.9 and 31.1 &#956;M, respectively, without obvious cytotoxicity. Further investigation showed that compound 8 demonstrated significant anti-pigmentation activity on zebrafish embryos (10‒20 &#956;M) compared to arbutin (20 &#956;M), and without any cytotoxicity against normal human epidermal keratinocytes. These findings suggest that (3S,3aR)-neocnidilide (8) is a potent antimelanogenic and non-cytotoxic natural compound and may be developed potentially as a skin-whitening agent for cosmetic uses

Diterpene Glycosides and Polyketides from Xylotumulus gibbisporus

[[abstract]]Four new tetracyclic diterpene glycosides, namely, sordarins C-F (1-4), and three new γ-lactone polyketides, namely, xylogiblactones A-C (5-7), along with sordarin were isolated from the ethyl acetate extracts of the fermented broths of Xylotumulus gibbisporus YMJ863. The structures of 1-7 were elucidated on the basis of spectroscopic data analyses. The configurations of 1-4 were deduced by NOESY, molecular modeling, and comparison with the literature. The relative configurations of 5-7 were deduced by X-ray crystallographic analysis of 5. Compounds 1-5 and sordarin were evaluated in an antifungal assay using Candida albicans ATCC 18804, C. albicans ATCC MYA-2876, and Saccharomyces cerevisiae ATCC 2345, and only sordarin exhibited significant antifungal activities against these fungal strains, with MIC values of 64.0, 32.0, and 32.0 μg/mL, respectively. The effect of compounds 1-7 and sordarin on the inhibition of NO production in lipopolysaccharide-activated murine macrophages was also evaluated. Compounds 2 and sordarin inhibited NO production with IC50 values of 327.2±46.6 and 157.1±24.1 μM, respectively

New Coumarins and Anti-Inflammatory Constituents from the Fruits of Cnidium monnieri

The fruit of Cnidium monnieri is commercially used as healthcare products for the improvement of impotence and skin diseases. Three new coumarins, 3'-O-methylmurraol (1), rel-(1'S,2'S)-1'-O-methylphlojodicarpin (2), and (1'S,2'S)-1'-O-methylvaginol (3), have been isolated from the fruits of C. monnieri, together with 14 known compounds (4–17). The structures of these new compounds were determined through spectroscopic and MS analyses. Compounds 1, 4–12, and 14–17 exhibited inhibition (IC50 ≤ 7.31 µg/mL) of superoxide anion generation by human neutrophils in response to formyl-l-methionyl-l-leucyl-l-phenylalanine/cytochalasin B (fMLP/CB). Compounds 7, 9–11, 15, and 17 inhibited fMLP/CB-induced elastase release with IC50 values ≤7.83 µg/mL. This investigation reveals that bioactive isolates (especially 6, 7, 14, and 17) could be further developed as potential candidates for the treatment or prevention of various inflammatory diseases

Angiogenesis Inhibitors and Anti-Inflammatory Agents from <i>Phoma</i> sp. NTOU4195

Seven new polyketides, phomaketides A–E (<b>1</b>–<b>5</b>) and pseurotins A₃ (<b>6</b>) and G (<b>7</b>), along with the known compounds FR-111142, pseurotins A, A₁, A₂, D, and F₂, 14-norpseurotin A, α-carbonylcarbene, tyrosol, cyclo­(-l-Pro-l-Leu), and cyclo­(-l-Pro-l-Phe), were purified from the fermentation broth and mycelium of the endophytic fungal strain <i>Phoma</i> sp. NTOU4195 isolated from the marine red alga <i>Pterocladiella capillacea</i>. The structures were established through interpretation of spectroscopic data. The antiangiogenic and anti-inflammatory effects of <b>1</b>–<b>7</b> and related analogues were evaluated using human endothelial progenitor cells (EPCs) and lipopolysaccharide (LPS)-activated murine macrophage RAW264.7 cells, respectively. Of the compounds tested, compound <b>1</b> exhibited the most potent antiangiogenic activity by suppressing the tube formation of EPCs with an IC₅₀ of 8.1 μM, and compound <b>3</b> showed the most selective inhibitory activity of LPS-induced NO production in RAW264.7 macrophages with an IC₅₀ value of 8.8 μM