• The Korean Journal of Nuclear Medicine
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• v.33 no.6
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• pp.527-536
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• 1999

Purpose: Radiotracers that bind to the central benzodiazepine receptor are useful for the investigation of various neurological and psychiatric diseases. [C-11]Flumazenil, a benzodiazepine antagonist, is the most widely used radioligand for central benzodiazepine receptor imaging by PET. We synthesized 3-(2-[F-18]fluoro)flumazenil, a new fluorine-18 ($t_{1/2}$= 110 min) labeled analogue of benzodiazepine receptor imaging agent, and evaluated in vivo for biodistribution in mice. Materials and Methods: Flumazenil (Ro 15-1788) was synthesized by a modification of the reported method. Precursor of 3-(2-[F-18]fluoro)flumazenil, the tosylated flumazenil derivative was prepared by the tosylation of the ethyl ester by ditosylethane. [F-18] labeling of tosyl substitued flumazenil precursor was performed by adding F-18 ion at $85^{\circ}C$ in the hot ceil for 20 min. The reaction mixture was trapped by C18 cartridge, washed with 10% ethanol, and eluted by 40% ethanol. Bidistribution in mice was determined after intravenous injection. Results: The total chemical yield of tosylated flumazenil derivative was ${\sim}40%$. The efficiency of labeling 3-(2-[F-18]fluoro)flumazenil was 66% with a total synthesis time of 50 min. Brain uptakes of 3-(2-[F-18]fluoro)flumazenil at 10, 30, 60 min after injection, were $2.5{\pm}0.37,\;2.2{\pm}0.26,\;2.1{\pm}0.11$ and blood activities were $3.7{\pm}0.43,\;3.3{\pm}0.07,\;3.3{\pm}0.09%ID/g$, respectively. Conclusion: We synthesized a tosylated flumazenil derivative which was successfully labeled with no-carrier-added F-18 by nucleophilic substitution.

• Journal of the Korean Society of Food Science and Nutrition
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• v.42 no.2
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• pp.175-181
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• 2013

This study investigated the ability of extracts from Lentinus edodes (LE) and rice with Lentinus edodes mycelium (LEM) to inhibit diabetes and obesity. Lipid accumulation significantly decreased by 78% and 74% upon treatment with 300 ${\mu}g/mL$ of LE and LEM, respectively (p<0.01). Cholesteryl ester transfer protein (CETP) inhibition activity increased by 94% and 99% upon treatment with 300 ${\mu}g/mL$ of LE and LEM, respectively. In order to investigate the effect of LE and LEM on diabetes, the inhibition of protein tyrosine phosphate 1B (PTP1B) activity from the LE and LEM extracts at various concentrations (1, 3, 10, 30, 100, 300 ${\mu}g/mL$) was assessed. PTP1B activity by treatment with 10, 30, and 100 ${\mu}g/mL$ of LE, was inhibited at a rate of 7, 9, and 7% respectively. Also, PTP1B activity from treatment with increasing concentration of LEM led to a significant concentration-dependent inhibition of PTP1B activity (p<0.01). LE and LEM were orally administered for 28 days after a high fat diet (HFD). LE and LEM significantly reduced triglyceride, cholesterol, HDL-cholesterol and LDL-cholesterol levels. GOT and GPT were not significantly effected. These results indicate that extracts of LE and rice with LEM have potent activities useful in the treatment of obesity and diabetes mellitus.

• Journal of Oral Medicine and Pain
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• v.38 no.3
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• pp.221-233
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• 2013

Bile acids are polar derivatives of cholesterol essential for the absorption of dietary lipids and regulate the transcription of genes that control cholesterol homeostasis. Recently it have been identified the synthetic chenodeoxycholic acid (CDCA) derivatives HS-1200 and cisplatin showed apoptisis-inducing activity on various cancer cells in vivo and in vitro. This study was undertaken to investigate the synergistic apoptotic effect of co-treatment with HS-1200 and cisplatin on human tongue squamous cell carcinoma cells (SCC25 cells). To investigate whether the co-treatment with HS-1200 and cisplatin compared to each single treatment efficiently reduces the viability of SCC25 cells, MTT assay was conducted. The induction and augmentation of apoptosis were confirmed by DNA electrophoresis, Hoechst staining and an analysis DNA hypoploidy. Westen blot analysis and immunofluorescent staining were also performed to evaluate the expression levels and the translocation of apoptosis-related proteins following this co-treatment. Furthermore, proteasome activity and mitochondrial membrane potential (MMP) change were also assayed. In this study, co-treatment with HS-1200 and cisplatin on SCC25 cells showed several lines of apoptotic manifestation such as nuclear condensations, DNA fragmentation, reduction of MMP and proteasome activity, the increase of Bax and the decrease of Bcl-2, decrease of DNA content, the release of cytochrome c into cytosol, translocation of AIF and DFF40 (CAD) onto nuclei, and activation of caspase-9, caspase-7, caspase-3, PARP and DFF45 (ICAD) whereas each single treated SCC25 cells did not show these patterns. Although the single treatment of $25{\mu}M$ HS-1200 and $4{\mu}g/ml$ cisplatin for 24 h did not induce apoptosis, the co-treatment of these reagents prominently induced apoptosis. Therefore our data provide the possibility that the combination therapy with HS-1200 and cisplatin could be considered as a novel therapeutic strategy for human squamous cell carcinoma.

• Journal of the Korean Society of Food Science and Nutrition
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• v.43 no.10
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• pp.1519-1526
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• 2014

This study investigated the biological activities and effects of Korean Zingiber mioga R. (flower buds and rhizome) on memory. The general composition, minerals, anti-oxidative activities, and AChE inhibitory effects were analyzed, and NORT (Novel object recognition test) and Y-Maze test in vivo were performed. The general contents (moisture, crude fat, crude protein, and crude ash; wet basis) of ZB (flower buds) were 91.96%, 0.15%, 1.99%, and 11.90%, respectively. The general contents (moisture, crude fat, crude protein, and crude ash; wet basis) of ZR (rhizome) were 75.21%, 0.53%, 2.20%, and 9.50%, respectively. The macro mineral contents (Ca, P, Na, and K) of ZB were 31.70 mg%, 15.20 mg%, 8.20 mg%, and 258.60 mg%, respectively. Inhibitory effects (IC50 value) of DPPH and ABTS radicals were higher with ZBD (flower buds water extract) than with ZBE (flower buds EtOH extract), ZRD (rhizome water extract) or ZRE (rhizome EtOH extract). AChE inhibitory effect of ZBD was higher and that of ZRD. NORT and Y-Maze test were performed with scopolamine-induced mice treated with ZBD and ZBE. In NORT, effects of ZBD and ZBE were similar to that of donepezil. In the Y-maze test, performances of ZBD and ZBE-treated mice were similar to that of the normal group. These results suggest that Korean Zingiber mioga R. has potential to be developed into a new functional food for cognition enhancement in the global food market.

• Tuberculosis and Respiratory Diseases
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• v.51 no.2
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• pp.135-146
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• 2001

Background : One of the important mechanisms responsible for a tumor escaping the immune response is an absence of the tumor associated antigen (TAA) on the cancer cell surface. To overcome this, combination gene therapy using a herpes simplex thymidine kinase (HSTK) gene, prototype of drug sensitizing gene, was conducted to enhance T AA release by cell destruction, as well as the cytokine genes for immune cell attraction. Methods : We investigated whether or not transduction with the adenovirus-HSTK (Ad-HSTK) enhanced the sensitivity of Lewis lung carcinoma (LLC) to ganciclovir (GCV) and induced a bystander effect. A Tumor vaccine trial was performed using LLC with ad-HSTK$\pm$ad-GM-CSF$\pm$ad-IL-2 to determine if they exhibit some antitumor effect on established lung cancer xenografts. Results : LLC with ad-HSTK revealed a much higher sensitivity to ganciclovir (GCV). LLC transduced with ad-HSTK and/or ad-IL-2, ad-GM-CSF showed a lower in vivo tumorigenicity. In the treatment experiment, vaccination with LLC transduced with ad-HSTK, ad-IL-2, or ad-GM-CSF alone modestly suppressed the growth of an established tumor. Combined transduction with HSTK and GM-CSF induced stronger growth suppression of a established lung cancer, while HSTK and IL-2 combination transduction did not have any antitumor effect on individual transduction. Vaccination with LLC-HSTK-GM-CSF increased the infiltration of dendritic cells in the spleen. Conclusion : It was concluded that a tumor vaccine transduced with HSTK and GM-CSF induces strong antitumor immunity by activating the dendritic cells.

• Journal of Life Science
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• v.27 no.2
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• pp.247-266
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• 2017

Cordyceps is a traditional Chinese medicinal herb well-known in China, Korea and Japan since B.C. 2,000. The original entomopathogenic fungus, Cordyceps sinensis belonging to the genus Cordyceps could not be found inside Korean peninsula due to the absence of the host insect for the corresponding entomogenous fungus. The development of artificial production methods of Korean type Cordyceps using the silkworm Bombyx mori as in vivo culture medium for the the entomopathogenic fungus Paecilomyces tenuipes is the first, and wonderful occasion in the research history of insect industry of this global world. The aim of this article is to review the historical research background, mass-production methods, and pharmacological effects of the silkworm-dongchunghacho (Paecilomyces tenuipes) which is a newly developed Korean medicinal insect-borne mushroom, and another non-insect-borne medicinal mushroom (Cordyceps militaris and Cordyceps pruinosa). Their biological actions include anti-tumor, immunostimulating, anti-fatigue, anti-stress, anti-oxidant, anti-aging, anti-diabetic, anti-inflammatory, anti-thrombosis, hypolipidaemic and insecticidal effects. The bioactive principles are protein-bound polysaccharides (hexose, hexosamin), cordycepin, D-manitol, acidic polysaccharide etc. Protein-bound polysaccharides and n-butanol fractions were demonstrated to show a significant anti-tumor activities but did not show a cytotoxicities. D-mannitol exhibited a significant prolongation of the life span in tumor bearing mice. Ergosterol did not show an efficient anti-tumor activity, but showed a significant phagocytosis enhancing activity. Anti-tumor activity of silkworm-dongchunghacho might be attributed to immuno-stimulating activities rather than cytotoxic effects [164]. Also this review comprises the breeding of Dongchunghacho varieties, optimization of culture conditions, improvement of learning and memory by Dongchunghacho, application of them as foods and chemical constituents.

• The Journal of Korean Obstetrics and Gynecology
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• v.31 no.4
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• pp.16-38
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• 2018

Objectives: The objective of this in vivo study is to observe the anti-osteoporotic activities of Gojineumja aqueous extracts (GJEJ) on the ovariectomized (OVX) mice as compared to those of risedronate sodium (RES). Methods: Thirty five days after bilateral OVX, GJEJ was orally administered, for 35 days once a day and then the changes on the body weight and gain during experimental periods, femur weights, bone mineral density (BMD), bone strength (failure load), mineral contents - calcium (Ca) and inorganic phosphorus (IP), histological profiles and histomorphometrical analyses at sacrifice were conducted with serum biochemistry - osteocalcin contents and bone specific alkaline phosphatase (BALP) activities. And the results of GJEJ were compared with RES orally administered OVX mice. Results: As a result of OVX, noticeable increase of body weight and gains and serum osteocalcin levels, decrease of serum BALP activities, femur weights, femur Ca and IP contents, BMD and strength were observed as compared to those of sham control mice, respectively. Also, the decrease of all histomorphometrical indices indicating the bone mass and structure, and the increase of indices about resorption were also detected in the femur of OVX control. However, these estrogen-deficient osteoporotic signs were significantly and dose-dependently inhibited by 35 days of continuous oral treatment of GJEJ, at dose levels of 500, 250 and 125 mg/kg, respectively. Especially, GJEJ 500 mg/kg showed favorable inhibitory activities against estrogen-deficient osteoporosis symptoms induced by OVX as comparable to those of RES 2.5 mg/kg. Conclusions: The results in this study suggest that oral administrations of GJEJ have clear dose-dependent favorable anti-osteoporotic activities in OVX mice.

• Tuberculosis and Respiratory Diseases
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• v.45 no.5
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• pp.992-999
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• 1998

Background: To correlate the emphysema score for quantification of the overall extent of emphysema in both lungs by CT with physiologic fingings and to get more objective and simple method to assess the extent of emphysema. Method: Thin-section CT and pulmonary function test(PFT) were performed in 17 patients with emphysema (all males, mean age, 62 years). Emphysema score was obtained as percentage of emphysematous lung area, dividing the total area of the emphysema(voxels with attenuation value less than -880, -900, -920HU, respectively) by the overall area of both lungs(voxels with attenuation value less than -400HU) with highlighting voxels using "Density mask" program. Emphysema score was calculated from whole lung(ESV) and 5 representative scans(ESR) using "Density mask", Visual emphysema score(ESV) was obtained by visual assessment from 5 representative scans. Correlation of these emphysema scores(ESW, ESR, ESV) and physiologic findings were performed, comparing the ESW with ESR and ESV. Results: ESW had correlation with DLCO(r=0.53-0.64) and $FEV_1/FVC$(r=0.42-0.57) among PFT parameters. ESR had good correlation with ESW and with PFT parameters as well. ESV did not correlate with PFT parameters except DLCO. Conclusion: CT quantification of emphysema using "density mask" correlated well with physiologic findings. To assess the severity of emphysema, both ESW and ESR are more reliable than ESV, and ESR is recommended in routine practice as it is objective, simple and reliable.

• The Journal of Korean Academy of Prosthodontics
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• v.49 no.4
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• pp.333-340
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• 2011

Purpose: The aim of this study was to study the effect of hydroxyapatite (HA) coating crystallinity on the proliferation and differentiation of human osteosarcoma cells. Materials and methods: Surface roughness of the titanium disks increased by anodizing treatment and then HA was coated using ion beam-assisted deposition (IBAD). HA coating was crystallized by heat-treated at different temperature ($100^{\circ}C$, $300^{\circ}C$, $500^{\circ}C$, $800^{\circ}C$). According to the temperature, disks were divided into four groups (HA100, HA300, HA500, HA800). With the temperature, crystallinity of the HA coating was different. Anodized disks were used as control group. The physical properties of the disk surface were evaluated by surface roughness tests, XRD tests and SEM. The effect of the crystallinity of HA coating on HOS cells was studied in proliferation and differentiation. HOS cells were cultured on the disks and evaluated after 1, 3, 5, and 7 days. Growth and differentiation kinetics were subsequently investigated by evaluating cell proliferation and alkaline phosphatase activity. Results: Regardless of the heat-treated temperature, there is no difference on the surface roughness. Crystallinity of the HA was appeared in the groups of HA500, HA800. HOS cells proliferation, ALP activity were higher in HA500 and HA800 group than HA100 and HA300. Conclusion: Within the results of this limited study, heat treatment at $500^{\circ}C$ of HA coating produced by IBAD has shown greater effect on proliferation and differentiation of HOS cells. It is considered that further in vivo study will be necessary.

• Journal of Life Science
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• v.21 no.12
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• pp.1752-1760
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• 2011

In this study, the effect of the Opuntiahumifusa extracts on proliferation, alkaline phosphatase (ALP) activity, collagen synthesis and ROS level of a cell was investigated using an osteoblast. Opuntiahumifusawas separated intoOpuntiahumifusapeel (OH-P), seed (OH-Se) and stem (OH-St).These were subjected to extraction by using hot water and ethanol. The proliferation of the MC3T3-E1 osteoblastic cells that were treated with OH-Se water extract were increased by approximately 120%. Regarding the effects of OH-Se on ALP activity, the $50{\mu}g/ml$ ethanol extract group showed the highest activity. The synthesis of collagen increased significantly in response to treatment with OH-Se water extract. The ROS scavenging effects of Opuntiahumifusawere investigated for involvement of oxidativedamage, cell culture and staining. Also, when OH-Se water extract $100{\mu}g/ml$ was added, the ROS level decreased by 54%. These results indicate that Opuntiahumifusa extracts have an anabolic effect on bone through the promotion of osteoblastic differentiation, suggesting that it could be used for the treatment of common metabolic bone diseases.