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Paudel S.,Chonnam National University | Cao Y.,Chonnam National University | Guo S.,Chonnam National University | An B.,Jeonnam Development Institute for Korean Traditional Medicine | And 2 more authors.
Bioorganic and Medicinal Chemistry | Year: 2015

A series of 4-benzylpiperidine carboxamides were designed and synthesized, and tested for their dual (serotonin and norepinephrine) reuptake inhibition. The synthesis of 4-benzylpiperidine carboxamides involved two main steps: amidation and substitution. Derivatives with 3 carbon linker displayed better activity than with 2 carbon linker. 4-Biphenyl- and 2-naphthyl-substituted derivatives 7e and 7j showed greater dual reuptake inhibition than standard drug venlafaxine HCl. © 2015 Elsevier Ltd. Source


Noh E.-M.,Chonbuk National University | Cho D.-H.,Chonbuk National University | Lee Y.-R.,Chonbuk National University | Jeong Y.-J.,Chonbuk National University | And 7 more authors.
BMB Reports | Year: 2011

Heme oxygenase-1 (HO-1), an inducible enzyme with broad tissue expression, is wel1-regulated in response to hematopoietic stress and preserves vascular homeostasis. We investigated the involvement of HO-1 in HL-60 cell differentiation. Dimethyl sulfoxide (DMSO) completely decreased HO-1 expression in a time-dependent manner, but clearly induced HL-60 cell differentiation, as evidenced by a marked increase in CD11b expression. Interestingly, zinc protoporphyrin (ZnPP), a strong inhibitor of HO-1, induced HL-60 cell differentiation. In contrast, treatment with cobalt protoporphyrin (CoPP), an activator of HO-1, decreased CD11b expression. Additionally, ZnPP downregulated HO-1 protein expression in HL-60 cells, whereas CoPP induced upregulation. These results suggest that HO-1 might have a negative function in DMSO-induced HL-60 cell differentiation. This study provides the first evidence that HO-1 plays an important role in DMSO-induced HL-60 cell differentiation. Source


Jung H.-R.,Korea University | Kim S.-J.,Korea University | Ham S.-H.,Jeonnam Development Institute for Korean Traditional Medicine | Cho J.-H.,Jeonnam Development Institute for Korean Traditional Medicine | And 2 more authors.
Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences | Year: 2014

A rapid, selective and sensitive ultra-performance liquid chromatography (UPLC)-tandem mass spectrometry method about the simultaneous determination of puerarin and its major active metabolite, daidzein, in human plasma was developed and validated in order to investigate the pharmacokinetics (PKs) of Gegen after the usual oral dose administration to human. Chromatography was carried out on a Kinetex C18 column (2.1. mm. ×. 50. mm, 1.7. μm) using 0.05% acetic acid in water and 0.05% acetic acid in methanol as mobile phase with a gradient elution. Liquid-liquid extraction with ethyl acetate in acidic condition could remove the interference and minimize the matrix effect of human plasma. The lower limit of quantification in human plasma was 0.2. ng/mL for both of compounds, puerarin and daidzein. The calibration curves for puerarin and daidzein in human plasma were linear over all the concentration range of 0.2-100. ng/mL with correlation coefficients greater than 0.998. This assay procedure was successfully applied to the PKs of puerarin and daidzein, after the usual oral dose of Gegen extract powder (2.56. g, containing 9.984. mg puerarin) in human subjects. © 2014. Source


Kim H.-L.,Kyung Hee University | Sim J.-E.,Kyung Hee University | Choi H.-M.,Kyung Hee University | Choi I.-Y.,Jeonnam Development Institute for Korean Traditional Medicine | And 11 more authors.
Food and Function | Year: 2014

Hovenia dulcis Thunb. is well known as a treatment for liver disease. Several studies have demonstrated that extracts of Hovenia dulcis Thunb. or its purified compounds can serve as detoxifying agents for alcohol poisoning. However, its anti-obesity effect has not been reported thus far. In this study, the anti-obesity effect of water extracts from the fruits or stems of Hovenia dulcis Thunb. was examined in 3T3-L1 preadipocytes. The cellular lipid contents in 3T3-L1 adipocytes were assessed by Oil Red O staining. Fruits of Hovenia dulcis Thunb. (FHD) significantly inhibit lipid accumulation during adipogenesis in a dose-dependent manner, but not stems of Hovenia dulcis Thunb. FHD (100 μg ml-1) significantly down-regulates the expression of the peroxisome proliferator-activated receptor-γ, CCAAT/enhancer-binding protein-α, adipocyte fatty acid-binding protein 2, adiponectin, and resistin, and the inhibition rates were 29.33%, 54.36%, 34.5%, 55.69%, and 60.39%, respectively. In addition, FHD (100 μg ml-1) also up-regulates the phosphorylation of AMP-activated protein kinase (AMPK)-α, liver kinase B1 as a major AMPK kinase, and the downstream substrate acetyl-CoA carboxylase, and the inhibition rates were 43.52%, 38.25%, and 20.39%, respectively. These results indicate that FHD has a significant anti-obesity effect through the modulation of the AMPK pathway, suggesting that FHD has a potential benefit in preventing obesity. © 2014 the Partner Organisations. Source


Bae G.-S.,Wonkwang University | Seo S.-W.,ChungBuk Oriental Medicine Center | Kim M.-S.,Wonkwang University | Park K.-C.,Wonkwang University | And 10 more authors.
Journal of Natural Medicines | Year: 2011

Nardostachys jatamansi (NJ) has been used in the treatment of inflammatory diseases. However, it is not clear how NJ produces anti-inflammatory effects. In the present study, using an experimental model of lipopolysaccharide (LPS)-induced endotoxin shock, the protective effects and mechanisms of action of NJ were investigated. The water extract of roots of NJ was administrated to mice orally (1, 5, and 10 mg/kg) 1 h after or before LPS challenge. The administration of NJ inhibited LPS-induced endotoxin shock and the production of inflammatory mediators, such as interleukin (IL)-1β, IL-6, tumor necrosis factor (TNF)-α, and interferon (IFN)-α/β. Murine peritoneal macrophages were used to determine the production of inflammatory mediators. In peritoneal macrophages, NJ also inhibited LPS-induced production of inflammatory mediators, such as IL-1β, IL-6, TNF-α, and IFN-α/β. In addition, NJ reduced the activation of mitogen-activated protein kinases (MAPKs) and the level of expression of interferon regulatory factor (IRF)-1 and IRF-7 mRNA. Furthermore, post-treatment with NJ reduced LPS-induced endotoxin shock and the production of inflammatory mediators. These results suggest that NJ inhibits endotoxin shock by inhibiting the production of IL-1β, IL-6, TNF-α, and IFN-α/β through the inhibition of MAPKs activation and IRF induction. © 2010 The Japanese Society of Pharmacognosy and Springer. Source

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