• Journal of Integrative Natural Science
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• 제8권1호
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• pp.40-47
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• 2015

Glycogen synthase kinase 3 (GSK-3) is a serine/threonine protein kinase that has recently emerged as a promising target in drug discovery. It is involved in multiple cellular processes and associated with the pathogenesis of several diseases. A three-dimensional quantitative structure-activity relationship (3D-QSAR) analysis was performed on a series of GSK-3 inhibitors to understand the structural basis for inhibitory activity. Comparative molecular field analysis (CoMFA) method was used to derive 3D-QSAR models. A reliable CoMFA model was developed using ligand-based alignment scheme. The model produced statistically acceptable results with a cross-validated correlation coefficient ($q^2$) of 0.594 and a non-cross-validated correlation coefficient ($r^2$) of 0.943. Robustness of the model was checked by bootstrapping and progressive scrambling analysis. This study could assist in the design of novel compounds with enhanced GSK-3 inhibitory activity.

• Journal of Microbiology and Biotechnology
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• 제4권2호
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• pp.119-125
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• 1994

Steroid $\Delta^1$-dehydrogenase purified from hydrocortisone-induced cells of Arthrobacter simplex converted various 3-ketosteroids into their corresponding $\Delta^1$-dehydrogenated products. The transformation efficiencies depend upon the chemical structure of the steroids, especially length of the side chain at 17 position and hydroxyl groups at 11 and 17 positions. The Km values for androstenedione, the most favorable substrate examined, and hydrocortisone were 74 ${\mu}M$ and 294 ${\mu}M$, respectively. The optimum temperature and pH of the enzyme reaction were 35$^{\circ}C$ and pH 9, respectively, and the enzyme was relatively stable at the range from 20 to 35$^{\circ}C$ and from pH 5 to 10 after one hour of incubation. The enzyme activity was markedly inhibited in the presence of $Cu^{2+},\;Fe^{3+},\;Hg^{2+},\;Mo^{6+}$ ions, and somewhat inhibited by $Zn^{2+}$ and $Fe^{2+}$. $\alpha,\alpha'$-Dipyridyl that inhibits 9$\alpha$-hydroxylase and accumulates 1,4-androstadiene-3,17-dione from sterols revealed no inhibitory effect on this enzyme. EGTA showed inhibitory effect. $\beta$-Estradiol competitively inhibited the enzyme activity. Chemical modifications of the enzyme were attempted with several reagents. p-Hydroxymer-curibenzoate showed inhibition of the enzyme activity and protection of the substrate. This suggests that cysteine residue may be involved in the active site of the enzyme.

• KSBB Journal
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• 제7권4호
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• pp.302-307
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• 1992

Protein phosphatase 2A was obtained from a cytosolic fraction of bovine brain homogenate. The phosphatase activity using phosphorylated histone Hl as substrate was suppressed in the presence of liposomes composed of dipalmitoylphosphatidylcholine(DPPC) or the mixture of phosphatidylserine and DPPC. The binding of protein phosphatase to liposome was indicated by the facts that the phosphatase activity of the supernatant of protein phosphatase/multilayer vesicle mixture was decreased with increasing amount of liposome, and that [$^{125}I$]-labeled protein phosphatase was coeluted with liposome. However, the affinity of the protein for phospholipid membrane was not so high. On the other hand, okadaic acid and liposome reduced the phosphatase activity synergistically, which means that okadaic acid binds neither to lipid membrane nor to the membrane-associated phosphatase, The inhibitory effect of liposome was, therefore, ascribed to association of the protein phosphatase 2A with the lipid bilayer membrane.

• Journal of Life Science
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• 제14권3호
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• pp.509-513
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• 2004

Inhibitory activities of 58 methanol extracts, which were prepared from different parts of 55 kinds of edible and medicinal plants, against human thrombin were evaluated. Analysis of the anti-coagulation activity determined by thrombin time enabled us to select 8 herb extracts as possible sources of anti-thrombosis agent. Further analysis of anti-thrombosis activity determined by activated partial thromboplastin time and fibrinolytic activity, and heat stability and inhibition against other proteolytic digestive enzymes provided new information that Pimpinella brachycarpa, Lysimachia clethroides, and Salix gracilistyla could be used as a potential anti-thrombosis agent. Our results suggest that edible and medicinal plants could be the potential source of thrombin inhibitor.

• Korean Journal of Pharmacognosy
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• 제37권4호
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• pp.253-257
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• 2006

We examined anti-angiogenic effects of water extracts from 32 plant materials (20 Korean medicinal plants and 12 western herbs) using cell-based anti-angiogenic assay, HUVEC tube formation assay, and then we found that 7 plant extracts inhibited HUVEC tube formation strongly. The plant materials which showed anti-angiogenic effects are Cinnamomi Ramulus, Atractylodis Rhizoma alba, Polygalae Radix, Myristicae Semen, Artemisiae Iwayomogii Herba, leaves of Rosmarinus officinalis, and leaves of Melissa officinalis. We also investigated inhibitory effects of these anti-angiogenic herbal extracts on MMP (matrix metalloproteinase) activity which has important roles in angiogenesis. Among extracts tested in this study, water extract of Melissa officinalis showed the most potent anti-angiogenic and MMP inhibitory activity.

• Natural Product Sciences
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• 제23권2호
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• pp.108-112
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• 2017

Anti-inflammatory, anti-arthritic and analgesic activity of each herbal extract, which is extracted from Bacopa monnieriis, Cassia fistula and Phyllanthus polyphyllus, respectively. The treatment of herbal extract exhibited anti-inflammatory effect as a dose-dependent manner, from 1.25 mg/kg to 12.5 mg/kg, in acute inflammatory models (carrageen and egg-albumin induced rat hind paw edema). It also elicited significant anti-inflammatory activity in chronic inflammatory models (cotton pellet granuloma and Freund's adjuvant induced polyarthritis in rat). In cotton pellet granuloma test, the extract exhibited the inhibitory effect of 23 and 57% at the dose of 6.25 and 12.5 mg/kg, respectively. In Freund's adjuvant induced model, the treatment of the extract of 1.25, 6.25 and 12.5 mg/kg showed the inhibitory effect of 23, 56 and 66% at 8 days, respectively. In the acetic acid-induced model, the extract significantly reduced abdominal writhing in mice when compared to the control group, reducing the mean number of writhing from $41{\pm}2$ in the control group to $17{\pm}3$ and $15{\pm}2$ at the dose of 6.25 and 12.5 mg/kg. From these experiments, the extract, which was extracted from the combination of Bacopa monnieriis, Cassia fistula and Phyllanthus polyphyllus, (w/w/w = 1/2/1) is surprisingly found a significant analgesic and anti-inflammatory activity.

• Journal of the Korean Wood Science and Technology
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• 제38권2호
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• pp.159-164
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• 2010

Nine compounds, caffeic acid, naringenin, apigenin, luteolin, kaempferol, verbascoside, isoverbascoside, isocampneoside II, and cistanoside F, were isolated from the EtOAc and n-BuOH fractions of P. coreana bark. The structures of these compounds (1-9) were elucidated by spectroscopic methods and literature data. All the isolates were subjected to in vitro bioassay to evaluate their inhibitory activity against rat lens aldose reductase. Among these, compounds 6 and 8 indicated the significant inhibitory activity on rat lens aldose reductase with $IC_{50}$ values of 2.67 and 5.59 ${\mu}M$, respectively. Especially, The inhibition activity of acteoside was 3.9 times better than that of quercetin as a positive control (10.6 ${\mu}M$). These results suggested that phenylethanoid glycosides are likely to be the potential compounds for the prevention and/or treatment of diabetic complications.

• IMMUNE NETWORK
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• 제9권5호
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• pp.203-207
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• 2009

Background: The FimA of Porphyromonas gingivalis is a crucial pathogenic component of the bacteria and has been implicated as a target for vaccine development against the periodontal diseases. Methods: In this study, the purified fimbriae (FimA subunit polymers) protein was used for immunization in their native form and B hybridoma clones producing antibodies specific to FimA were established. Results: The monoclonal antibodies prepared from selected two clones, designated #123 (IgG2b/ kappa) and #265 (IgG1/kappa), displayed different patterns of binding activity against the cognate antigen. Both antibodies reacted with conformational epitopes expressed by partially dissociated oligomers, but not with monomer as elucidated by Western blot analysis. Ascites fluid containing the monoclonal antibodies showed the inhibitory activity against P. gingivalis to saliva-coated hydroxyapatite beads, an in vitro model for the pellicle-coated tooth surface. Conclusion: These results suggest that the monoclonal antibodies could be used as vaccine material against the periodontal diseases through passive immunization.

• Journal of Oriental Neuropsychiatry
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• 제14권1호
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• pp.75-84
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• 2003

Object : The present experiments were designed to study on the memory enhancement of the extract of Gongjadaesungjichimjung-bang(GDJB). Methods : The water extract of GCJB has been tested for its activities on memory enhancement by passive avoidance task in vivo and for its inhibitory effect on the acetylcholine esterase activity. Results : GDJB water extract significantly enhanced the memory at a concentration of 50mg/kg, but this effect did not proportionally increased at a dose of l00mg/kg and significantly inhibited the acetylcholine esterase activity in a dose-dependent manner in in vitro assay with IC50 value of 1.57mg/ml and also in in vivo assay. Conclusion : The extract of GDJB showed a memory enhancement as well as the inhibitory effect on acetylcholine esterase activity, which suggest that this prescription may be applied for the treatment of memory impairment.

• Biomedical Science Letters
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• 제23권4호
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• pp.339-347
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• 2017

This study was performed to evaluate the cytotoxicity induced by ischemia-like condition (ILC) in cultured neuroglial cells (C6 glioma cells). The protective effect of kaempferol (KAE), flavonoid against the cytotoxicity induced by ILC induction was assessed. In addition, antioxidative effects of KAE were done by colorimetric assays. Cell viability and the antioxidative effects such as DPPH-radical scavenging activity, superoxide dismutase (SOD)-like activity and inhibitory activity of lipid peroxidation (LP) were analyzed. ILC induction decreased cell viability in a dose-dependent manner, and the $XTT_{90}$ value (low cytotoxicity value) and $XTT_{50}$ value (high cytotoxicity value) were determined during ILC induction for 15 and 40 minutes, respectively. The butylated hydroxytoluene (BHT) antioxidant significantly increased cell viability damaged by the ILC-induced cytotoxicity. In the protective effect of KAE on ILC-induced cytotoxicity, KAE protected the ILC-induced cytotoxicity by the significant increase of cell viability, and also it showed DPPH-radical scavenging ability, SOD-like ability and inhibitory ability of LP. From these results, it is suggested that ILC induction showed cytotoxicity in these cultures and the oxidative stress is involved in the ILC-induced cytotoxicity. While, KAE prevented ILC-induced cytotoxicity by antioxidative effects. In conclusion, natural products like KAE may be a putative therapeutic agent for the treatment of disease associated with oxidative stress such as ischemia.