• Asian Pacific Journal of Cancer Prevention
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• v.13 no.12
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• pp.6211-6216
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• 2012

Objective: To investigate the effects of gambogic acid (GA) on the growth of human malignant glioma cells. Methods: U251MG and U87MG human glioma cell lines were treated with GA and growth and proliferation were investigated by MTT and colony formation assays. Cell apoptosis was analyzed by annexin V FITC/PI flow cytometry, mitochondrial membrane potential assays and DAPI nuclear staining. Monodansylcadaverine (MDC) staining and GFP-LC3 localisation were used to detect autophagy. Western blotting was used to investigate the molecular changes that occurred in the course of GA treatment. Results: GA treatment significantly suppressed cell proliferation and colony formation, induced apoptosis in U251 and U87MG glioblastoma cells in a time- and dose-dependent manner. GA treatment also lead to the accumulation of monodansylcadaverine (MDC) in autophagic vacuoles, upregulated expressions of Atg5, Beclin 1 and LC3-II, and the increase of punctate fluorescent signals in glioblastoma cells pre-transfected with GFP-tagged LC3 plasmid. After the combination treatment of autophagy inhitors and GA, GA mediated growth inhibition and apoptotic cell death was further potentiated. Conclusion: Our results suggested that autophagic responses play roles as a self-protective mechanism in GA-treated glioblastoma cells, and autophagy inhibition could be a novel adjunctive strategy for enhancing chemotherapeutic effect of GA as an anti-malignant glioma agent.

• Bulletin of the Korean Chemical Society
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• v.35 no.9
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• pp.2733-2737
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• 2014

A series of pyrazolyl thiosemicarbazone derivatives were synthesized and evaluated for their anticonvulsant activity using the maximal electroshock (MES) method. Interestingly, all compounds prepared showed long duration of protection effect in the MES screens. Among them, compound 5b was considered as the most promising one with an $ED_{50}$ value of 47.3 mg/kg, and a PI value of 4.8, which was superior to phenobarbital and valproate in the aspect of safety. Furthermore, compound 5b showed protection against seizures induced by pentylenetetrazole suggesting that compound 5b may exert anticonvulsant activity through GABA-mediated mechanisms.

• Journal of Korean Medical Ki-Gong Academy
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• v.18 no.1
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• pp.27-51
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• 2018

Objective : The purpose of this study is to examine the relationship between the brain and the pelvis. Methods : The relationship between the pelvis and the brain was searched in PubMed, and these searching studies were reviewed. Conclusions : 1. Urinary disorder is influenced by brain. 2. Brain is influenced by luteinizing hormone. 3. Pelvic floor muscles are influenced by brain. 4. Urological Chronic Pelvic Pain Syndrome(UCPPS) is influenced by brain. 5. Brain is influenced by the low intensity laser acupuncture stimulating thirteen ghost acupoints(includes CV1).

• The Journal of Korean Society of Virology
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• v.29 no.3
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• pp.165-174
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• 1999

To investigate viral pathogenesis and in vivo efficacy of acyclovir (ACV) in mouse HSV-1 encephalitis models, female BALB/c mice aged 5 weeks were inoculated with strain F either intranasally (IN) or intracerebrally (IC). ACV-treatment by intraperitomeal injection with 0, 5, 10 and 25 mg/kg b.i.d. for 6 days was commenced 1 h after infection. Body weight and signs of clinical disease were noted daily up to 2 weeks. $ED_{50}$ of ACV in IN infection was <5 mg/kg and 14.1 mg/kg in IC infection. Tissues of central nervous system were collected from 2 mice per group everyday up to 5 day p.i. and the virus titers were measured. In IN infection model, high titers in eyes and trigeminal nerves were observed. ACV-treatment showed significant reduction of the titers in all the isolated. In IC infection model, cerebrum, cerebellum and brain stem showed high virus titers. ACV-treatment showed less significant reduction of virus titers than that in IN infection model. Reactivation of explanted trigeminal nerves from mice 30 day p.i. was monitored. In all of ACV treated mice reactivation was observed, i.e. even the highest dose of ACV did not inhibit the establishment of viral latency.

• The Bulletin of The Korean Astronomical Society
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• v.42 no.1
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• pp.49.3-50
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• 2017

Metallicity is one of the most important properties in understanding galaxy evolution. However, measuring metallicity is limited to low redshift (z<3.5) due to the faintness of the metallicity indicators in normal galaxies. For high redshift universe, active galactic nuclei (AGN) can be used to constrain the host galaxy metallicity. Previous studies investigated AGN metallicity using emission line flux ratios (i.e., NV/CIV and FeII/MgII), finding no evolution up to z~6. Those results might be due to selection effect since previous studies are based on very luminous AGNs. The observed luminosity-metallicity relation of AGNs (e.g., Nagao et al. 2006) suggests that luminous AGNs may be already matured at the observed epoch. Considering the luminosity-metallicty relation, we focused on low luminosity AGNs to find young AGNs (i.e., low metallicity). Through the Gemini/GNIRS observation in 2012A and 2015A (K-GMT GN-2015A-Q-203 PI: Shin, J.), we obtained the Gemini/GNIRS data for 7 high redshift AGNs (3.0

• Archives of Pharmacal Research
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• v.21 no.6
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• pp.764-768
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• 1998

In connection with the development of new anticonvulsant agents with a broad spectrum, we reported that N-Cbz-alpha-aminoglutarimides, combining common structures of othe r anticonvulsants such as N-CO-C-N and cyclic imides in a single molecule, showed significant anticonvulsant activities in the MES (maximal electroshock seizure) and PTZ (pentylenetetrazole induced seizure) tests. In these studies, a series of (R) and (S) N-alkyloxycarbonyl-alpha-aminoglutarimides 7a-7e and 8a-8e, which were substituted with various alkyloxycarbonyl group instead of Cbz group, were prepared from the corresponding (R) and (S) N-Cbz-glutamic acid 3 and 4, and were evaluated with their anticonvulsant activities against the MES and PTZ tests, including neurotoxicity, in order to define the effect of N-alkyloxycarbonyl group on the anticonvulsant activities of N-alkyloxycarbonyl-${\alpha}$-aminoglutarimides. Among them, (S)N-4-nitrobenzyloxycarbonyl-${\alpha}$-amino-N-methylglutarimide 8e was the most active in MES ($ED_{50}$=35.6mg/kg, PI=2.7) and PTZ tests ($ED_{50}$=15.6, PI=6.1). Interestingly, (R) and (S) N-4-nitrobenzyloxycarbonyl-${\alpha}$-amino-N-methylglutarimide 7e and 8e and (R) N-phenoxycarbonyl-${\alpha}$-amino-N-methylglutrimide 7d showed significant anti-convulsant activities in both the MES and PTZ tests and other compounds showed anticonvulsant activities in only the PTZ test. In addition, it was found that their anticonvulsant activities were dependent on their stereochemistries and N-substituted alkyloxycarbonyl groups.

• Korean Journal of Fisheries and Aquatic Sciences
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• v.46 no.4
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• pp.351-358
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• 2013

A protease inhibitor from fish eggs was fractionated using chromatographic methods. The fractionation efficiency was evaluated in terms of specific inhibitory activity (SIA, U/mg), purity (fold), total inhibitory activity (TIA, U), and recovery (%). The protease inhibitor (PI) from egg extracts of skipjack tuna (ST Katsuwonus pelamis), yellowfin tuna (YT Thunnus albacares) and Alaska pollock (AP Theragra chalcogramma) was fractionated using Sephadex G-50 gel filtration and DEAE-Sepharose CL-6B anion exchange chromatography based on protein size exclusion and net charge, respectively. Fractions exhibiting strong inhibitory activity were contained in the 30-50 kDa fraction on gel filtration and in the range of 0.4-0.7 M NaCl gradient fraction on anion exchange chromatography. The respective TIA and percent recovery of the fraction obtained with gel filtration toward trypsin and $N{\alpha}$-benzoyl-L-arginine-p-nitroanilide (BAPNA) were 2,758.7 U and 29.6% for ST, 1,005.5 U and 25.6% for YT, and 1,267.5 U and 26.0% for AP. Gel filtration chromatography was more effective at fractionating PI than using ion exchange chromatography. These results suggest that fish eggs act as serine protease inhibitors and might be useful for protease inhibition in foodstuffs.

• Biomolecules & Therapeutics
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• v.21 no.2
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• pp.107-113
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• 2013

Plasminogen activator inhibitor-1 (PAI-1) is a member of serine protease inhibitor family, which regulates the activity of tissue plasminogen activator (tPA). In CNS, tPA/PAI-1 activity is involved in the regulation of a variety of cellular processes such as neuronal development, synaptic plasticity and cell survival. To gain a more insights into the regulatory mechanism modulating tPA/PAI-1 activity in brain, we investigated the effects of proteasome inhibitors on tPA/PAI-1 expression and activity in rat primary astrocytes, the major cell type expressing both tPA and PAI-1. We found that submicromolar concentration of MG132, a cell permeable peptide-aldehyde inhibitor of ubiquitin proteasome pathway selectively upregulates PAI-1 expression. Upregulation of PAI-1 mRNA as well as increased PAI-1 promoter reporter activity suggested that MG132 transcriptionally increased PAI-1 expression. The induction of PAI-1 downregulated tPA activity in rat primary astrocytes. Another proteasome inhibitor lactacystin similarly increased the expression of PAI-1 in rat primary astrocytes. MG132 activated MAPK pathways as well as PI3K/Akt pathways. Inhibitors of these signaling pathways reduced MG132-mediated upregulation of PAI-1 in varying degrees and most prominent effects were observed with SB203580, a p38 MAPK pathway inhibitor. The regulation of tPA/PAI-1 activity by proteasome inhibitor in rat primary astrocytes may underlie the observed CNS effects of MG132 such as neuroprotection.

• Biomedical Science Letters
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• v.13 no.3
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• pp.169-173
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• 2007

[ $^{31}PNMR$ ] spectroscopy revealed the adenylate kinase-like activity and the phosphotransferase activity from $F_1-ATPase$ of Escherichia coli. Incubation of $F_1-ATPase$ with ADP in the presence of $Mg^{2+}$ shows the appearance of $^{31}P$ resonances from AMP and Pi, suggesting the generation of AMP and ATP by adenylate kinase-like activity and the subsequent hydrolysis to Pi. Incubation of $F_1-ATPase$ with ADP in the presence of methanol shows additional peak from methyl phosphate, suggesting phosphotransferase activity of $F_1-ATPase$. Both adenylate kinase-like activity and the phosphotransferase activity has not been reported from $F_1-ATPase$ from Escherichia coli. $^{31}P$ NMR proved that it could be a valuable tool for the investigation of phosphorous related enzyme.

• Korean Journal of Fisheries and Aquatic Sciences
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• v.25 no.2
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• pp.73-78
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• 1992

To investigate the desirable index for evaluation of frozen surimi's grades, the relationship between indices for grading of surimi, such as ATPase activity $(Ca^{2+}-,\;Mg^{2+}-\;and\;EDTA-)4, solubility, viscosity and K-value of frozen surimi and jelly strength of kamaboko was studied. The myofibrillar $Ca^{2+}-ATPase$ activity and solubility from frozen surimi of grades SA, FA, A, RA and B gave values of $1.184\pm0.2,\;0.956\pm0.14,\;0.766\pm/0.07,\;0.453\pm0.07\;and\;0.227\pm0.08$(umoles Pi/min/mg) for $Ca^{2+}-$ATPase activity and $93.19\pm5,\;84.62\pm4,\;70.63\pm5,\;41.21\pm4\;and\;32.82\pm4(\%)$ for solubility, respectively. Therefore, the myofibrillar $Ca^{2+}-$ATPase activity and solubility of surimi were closely related to the jelly strength of kamaboko from same material, as the correlation coefficient were 0.9584 and 0.9849, respectively. K-value, the index of freshness, was related to the jelly strength of frozen surimi as the correlation coefficient 0.9053 and shown as SA $15.67\pm1.4,\;FA\;14.94\pm 3,\;A\;28.00\pm5,\;RA\;32.16\pm3\;and \;B\;48.68\pm 5(\%)$. $Mg^{2+}-$ and EDTA-ATPase activity and viscosity were not related to the jelly strength. The $Ca^{2+}-$ATPase activity and solubility were found to be useful index for evaluating the quality of frozen surimi.