• Journal of the Korean Society of Food Science and Nutrition
• /
• v.34 no.9
• /
• pp.1336-1343
• /
• 2005

In the present study, we screened candidates for enhancing insulin action and secretion from Cinnamomum camphora (CC) fractions, in 3T3-L1 adipocytes and Min6 cells by investigating insulin- stimulated glucose uptake and glucose-stimulated insulin secretion, respectively. CC were extracted by $70\%$ ethanol followed by XAD-4 column chromatography with serial mixture solvents of methanol and water, and the fractional extractions were utilized for determining insulin action and secretion, and $\alpha$-glucoamylase suppressing activity, A significant insulin-stimulated glucose uptake was observed in 3T3-L1 adipocytes, giving 0.5 or $5{\mu}g/mL$ of $40\%\;and\;60\%$ methanol fractions plus 0.2 nM insulin, compared to the treatment of DMSO plus 0.2 nM insulin. The treatments of $40\%\;and\;60\%$ methanol fractions plus 0.2 nM insulin reached the glucose uptake of 10 nM insulin treatment. The $40\%$ methanol fraction increased triglyceride accumulation by stimulating differentiation and triglyceride synthesis similar to pioglitazone, PPAR-$\gamma$ agonist. No inhibition of $\alpha$-glucoamylase activity of CC fractions was observed. They did not modulate the insulin secretion capacity In either low or high glucose media. These results suggest that $40\%$ methanol fraction contains a potential insulin sensitizer to have a similar function of PPAR-$\gamma$ agonist. Crude CC extract may improve glucose utilization by enhancing insulin-stimulated glucose uptake without elevating glucose stimulated insulin secretion.

• The Korean Journal of Nuclear Medicine
• /
• v.32 no.4
• /
• pp.374-381
• /
• 1998

Purpose: I-131 labeled (2'-deoxy-2'-iodo-${\beta}$-D-arabinofuranosyl) adenine (IAD) may be involved in DNA synthesis during active proliferation of tumor cells. We conducted this study to find out the biodistribution of IAD and it's feasibility for scintigraphic tumor imaging. Materials and Methods: Tosyl acetyl-adenosine was dissolved in acetonitrile, and I-131-NaI was added and heated to synthesize IAD. Female Fisher 344 rats innoculated with breast tumor cells were injected with 0.27 MBq of IAD. Rats were sacrificed at 0.5, 1, 2, 4, 24h and the % of injected dose per gram of tissue (%ID/g) was determined. For scintigraphy, rats bearing breast cancer were administered with 1.11 MBq of IAD and imaging was performed after 2 and 24h. Then, rat body was fixed and microtomized slice was placed on radiographic film for autoradiography. Results: %ID/g of tumor was 0.74 (0.5h),0.73 (1h), 0.55 (2h), 0.38 (4h), and 0.05 (24h), respectively. At 1h after injection, %ID/g of tumor was higher than that of heart (0.34), liver (0.42), spleen (0.47), kidney (0.69), muscle (0.14), bone (0.33) and intestine (0.51). However, %ID/g of tumor was lower than blood (1.06), lung (0.77), and thyroid (177.71). At 4h, %ID/g of tumor in comparison with other tissue did not change. Tumor contrast expressed by tumor to blood ratio was 0.69 and tumor to muscle ratio was 5.11 at 1h. However, these ratios did not improve through 24h. On autoradiogram and scintigraphy at 2 and 24 hour, the tumor was well visualized. Conclusion: This results suggest that IAD may have a potential for tumor scintigraphy. However, further work is needed to improve localization in tumor tissue.

• The Korean Journal of Nuclear Medicine
• /
• v.28 no.3
• /
• pp.364-370
• /
• 1994

The purpose of this study is to evaluate the clinical application of the no carrier added $[^{51}Cr]Cr(III)$-EDTA complexes, produced at Korea Cancer Center Hospital. The $[^{51}Cr]Cr(III)$-EDTA complexes, usefut for measurement of GFR were prepared at room temperature in the presence of bicarbonate catalysts. The radiochemical purity of $[^{51}Cr]Cr(III)$-EDTA was over 99% by paper electrophoresis. The time activity curves were obtained by counting the blood samples from 5 volunteers and counting the head and neck regions with whole body counter after injection of the $^{51}Cr$-EDTA, respectively. After the nonlinear regression, the area under curve was obtained. The plasma clearance of the $^{51}Cr$-EDTA was calculated with injected dose/AUC. The clearance rate calculated with the head and neck counting data was in good agreement with the result from the plasma sample radioactivity at 1-3 hrs after injection. From this result, the counting of head and neck region and the nonlinear regression by 2-compartment model could be applied for the measurement of the clearance rate. Using MIRD system, the absorbed radiation dose was calculated by residence $time{\times}S$. The absorbed whole body radiation dose was negligibly small.

• Journal of the Korean Chemical Society
• /
• v.45 no.3
• /
• pp.242-246
• /
• 2001

The quaternary thiophosphates, $A_2NiP_2S_6$ (A=Rb, Cs), have been synthesized with halide fluxes and structurally characterized by single-crystal X-ray diffraction technique. These compounds crystallize in the space group $C_{2h}^5-P2_1/n$ of the monoclinic system with two formula units in a cell of dimensions a=5.960(2), b=12.323(4), $c=7.491(3)\AA$, $\beta=97.05(3)^{\circ}$, and $V=546.0(3)\AA^3$ for Rb2NiP2S6 and a=5.957(4), b=12.696(7), $c=7.679(4)\AA$, $b=93.60(5)^{\circ}$, and $V=579.7(5)\AA^3$ for $Cs_2NiP_2S_6.$ These compounds are isostructural. The structure of $Cs_2NiP_2S_6$ is made up of one-dimensional $_\infty^1[NiP_2S_6^{2-}]$ chains along the a axis and these chains are isolated by $Cs^+$ ions. The Ni atom is octahedrally coordinated by six S atoms. These Ni$S_6$ octahedral units are linked by sharing three m-S atoms of the $[P_2S_6^{4-}]$ anions to form the infinite one-dimensional $_\infty^1[NiP_2S_6^{2-}]$ chain. For $Cs_2NiP_2S_6$, the magnetic susceptibility reveals an antiferromagnetic exchange interaction below 8K,which corresponds to the Neel temperature ($T_N$). Above $T_N$, this compound obeys Curie-Weiss law. The magnetic moment, C, and ${\theta}forCs_2NiP_2S_6$ are 2.77 B.M., 0.9593 K, and -19.02 K, respectively. The effective magnetic moment obtained from the magnetic data is agreed with the spin-only value of $Ni^{2+}d^8$(2.83 B.M.) system.

• Journal of Ginseng Research
• /
• v.31 no.4
• /
• pp.196-202
• /
• 2007

Skin wrinkles are associated with collagen synthesis and matrix metalloproteinase-I (MMP-1) activity. This study was carried out to select optimum ratio of 3 herbs in skin health food for anti-wrinkle. Human dermal fibroblast cell was incubated with experimental samples, which were Korean red ginseng ethanol extracts (ER), Torilis fructus water extracts (WT), Corni fructus water extracts (WC) and their mixtures (WM1, WM3). And then we determined effects on collagen biosynthesis, MMP-1 activity and SOD activity in human dermal fibroblast cell. In control group, collagen biosynthesis was amounted at 474.8 ng/ml and 533.9 ng/ml, 539.3 ng/ml, 514.1 ng/ml in ER, WT and WC respectively. Furthermore, WM3 (KTNG0345) was increased to 561.45 ng/ml. MMP-1 activity of ER, WT, WC, WM1 were determined to 31.9 ng/ml, 32.85 ng/ml, 32.0 ng/ml, 31.3 ng/ml and WM3 (KTNG0345) was decreased to 28.85 ng/ml. In addition, the experimental samples showed a antioxidative activities. From this results, we conclude that Korean red ginseng ethanol extracts, Torilis fructus water extracts, Corni fructus water extracts and their mixtures have a anti-wrinkle effect and WM3 (KTNG0345) may be regarded as an optimum composition for synergic effect producing. The standardized components of KTNG0345, ginsenoside-$Rb_1$, torilin and loganin were identified at 10.85 mg/g, 0.128 mg/g and 3.92 mg/g respectively.

• Archives of Pharmacal Research
• /
• v.21 no.4
• /
• pp.458-464
• /
• 1998

Search for a new $\alpha$-methylene-$\gamma$-butyrolactone-bearing 6-substituted purine as a potental antitumor agent has led to synthesize seven, hitherto unreported, $5^1$-Methyl-$5^1$-[(6-substituted-9H-purin-9-yl)methyl]-$2^1$-oxo-$3^1$- methylenetetrahydrofurans (H, Cl, l, $CH_3$, $NH_2$, SH, >C=O) (6a-g). These include $5^1$-Methyl-$5^1$-[(9H-purin-9-yl)methyll-$2^1$-oxo-$3^1$ -methylenetetrahydrofurans (6a), $5^1$-Methyl-$5^1$-[(6-chloro-9H-purin-9-yl)methyl]-$2^1$-oxo-$3^1$-methylenetetrahydr ofurans (6b), $5^1$-Methyl-$5^1$-[(6-chloro-9H-purin-9-yl) methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6c), $5^1$-Methyl-$5^1$-[(6-methyl-9H-purin-9-yl) methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6d), $5^1$-Methyl-$5^1$-[(9H-adenin-9-yl)methyll-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6e), $5^1$-Methyl-$5^1$-[(6-mercapto-9H-purin-9-yl) methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6f) and $5^1$-Methyl-$5^1$-[(9H-hypoxanthin-9-yl)methyll-$2^1$-oxo-$3^1$-methylenetetrahydrof urans (6g) which were made by the Reformatsky-type reaction of ethyl $\alpha$-(bromomethyl) acrylate with the corresponding (6-substituted-9H-purin-9-yl)-2-propanone intermediates (5a-g). These ketone intermediates 5a-g, 1-(9H-purin-9-yl)-2-propanone (5a), 1-(6-chloro-9H-purin-9-yl)-2-propanone (5b), 1-(6-iodo-9H-purin-9-yi)-2-propanone (5c), 1-(6-methyl-9H-purin-9-yl)-2-propanone (5d), 1-(9H-adenin-9-yl)-2-propanone (Se), 1-(6-mercapto-9H-purin-9-yl)-2-propanone (5f), and 1-(9H-hypoxanthin-9-yl)-2-propanone (5g) were directly obtained by the alkylation of the 6-substituted purine bases with the chloroacetone in the presence of $K_2$$CO_3$ (or NaH) under DMF (or DMSO). The preliminary in vitro cytotoxcity assay for the synthetic .alpha.-methylene-y-butyro-lactone compounds (6a-g) were determined against three cell lines (PM-3A, P-388, and K-562) and showed the moderate antitumor activity ($IC_50$ ranged from 1.4 to 4.3 $\mu\textrm{g}$/ml) with the compound $5^1$-methyl-$5^1$ -[(9H-hypoxanthin-9-yl)methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofuran (6g) showing the least antitumor activity.

• Korean Journal of Food Science and Technology
• /
• v.38 no.1
• /
• pp.114-120
• /
• 2006

Anti-diabetic effects of extracts and fractions of Sasa borealis (SB), white lotus roots (LR) and leaves (LL), and their mixture were determined in 3T3-L1 adipocytes and Min6 cells by investigating insulin-sensitizing activity and glucose-stimulated insulin secretion, respectively. SB, LR, LL, and mixture of SB, LR, and LL (3 : 2 : 3) were extracted using 70% ethanol, and m mixture extract was fractionated by XAD-4 column chromatography with serial mixture solvents of methanol and water. Fractional extractions were utilized for anti-diabetic effect assay. SB and LR extracts increased insulin-stimulated glucose uptake, but not as much as mixture of SB, LR, and LL. Significant insulin-sensitizing activities of 20 and 80% methanol fractions of SB, LR, and LL mixture extract were observed in 3T3-L1 adipocytes, giving 0.5 or $5\;{\mu}g/mL$ each fraction with 0.2 nM insulin to attain glucose uptake level similar to that attained by 10 nM insulin alone. Similar to pioglitazone, peroxisome proliferators-activated $receptor-{\gamma}\;(PPAR-{\gamma})$ agonist, 20 and 80% methanol fractions increased adipocytes by stimulating differentiation from fibroblasts and triglyceride synthesis. LL extract and 20, 60, and 80% methanol fractions of the mixture suppressed ${\alpha}-amylase$ activity, but did not modulate insulin secretion capacity of Min6 cells in both low and high glucose media. These data suggest 20 and 80% methanol tractions contain potential insulin sensitizers with functions similar to that of $PPAR-{\gamma}$ agonist. Crude extract of SB, LR, and LL mixture possibly improves glucose utilization by enhancing insulin-stimulated glucose uptake and inhibiting carbohydrate digestion without affecting insulin secretion in vivo.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.41 no.4
• /
• pp.341-350
• /
• 2015

Skin carrys out protective role against harmful outer environment assaults including ultraviolet radiation, heavy metals and oxides. Especially, ultraviolet-B (UVB) light causes inflammatory reactions in skin such as sun burn and erythma and stimulates melanin pigmentation. Furthermore, the influx of UVB into skin cells causes DNA damage in keratinocytes and dermal fibroblasts, inhibition of extracellular matrix (ECM) synthesis which leads to a decrease in elasticity of skin and wrinkle formation. It also damages dermal connective tissue and disrupts the skin barrier function. Prolonged exposure of human skin to UVB light is well known to trigger severe skin lesions such as cell death and carcinogenesis. Haloarcula vallismortis is a halophilic microorganism isolated from the Dead Sea, Its growth characteristics have not been studied in detail yet. It generally grows at salinity more than 10%, but the actual growth salinity usually ranges between 20 to 25%. Because H. vallismortis is found mainly in saltern or salt lakes, there could exist defense mechanisms against strong sunlight. One of them is generation of additional ATP using halorhodopsin which absorbs photons and produces energy by potential difference formed by opening the chloride ion channel. It often shows a color of pink or red because of their high content of carotenoid pigments and it is considered to act as a defense mechanism against intense UV irradiation. In this study, the anti-inflammatory effect of the halophilic microorganism, H. vallismortis, extract was investigated. It was found that H. vallismortis extract had protective effect on DNA damage induced by UV irradiation. These results suggest that the extract of halophilic bacterium, H. vallismortis could be used as a bio-sunscreen or natural sunscreen which ameliorate the harmful effects of UV light with its anti-inflammatory and DNA protective properties.

• Nuclear Medicine and Molecular Imaging
• /
• v.41 no.3
• /
• pp.241-246
• /
• 2007

Purpose: $[^{11}C]6-OH-BTA-1$ ([N-methyl-$^{11}C$]2-(4'-methylaminophenyl)-6-hydroxybenzothiazole, 1), a -amyloid imaging agent for the diagnosis of Alzheimer's disease in PET, can be labeled with higher yield by a simple loop method. During the synthesis of $[^{11}C]1$, we found the formation of by-products in various solvents, e.g., methylethylketone (MEK), cyclohexanone (CHO), diethylketone (DEK), and dimethylformamide (DMF). Materials and Methods: In Automated radiosynthesis module, 1 mg of 4-aminophenyl-6-hydroxybenzothiazole (4) in 100 l of each solvent was reacted with $[^{11}C]methyl$ triflate in HPLC loop at room temperature (RT). The reaction mixture was separated by semi-preparative HPLC. Aliquots eluted at 14.4, 16.3 and 17.6 min were collected and analyzed by analytical HPLC and LC/MS spectrometer. Results: The labeling efficiencies of $[^{11}C]1$ were $86.0{\pm}5.5%$, $59.7{\pm}2.4%$, $29.9{\pm}1.8%$, and $7.6{\pm}0.5%$ in MEK, CHO, DEK and DMF, respectively. The LC/MS spectra of three products eluted at 14.4, 16.3 and 17.6 mins showed m/z peaks at 257.3 (M+1), 257.3 (M+1) and 271.3 (M+1), respectively, indicating their structures as 1, 2-(4'-aminophenyl)-6-methoxybenzothiazole (2) and by-product (3), respectively. Ratios of labeling efficiencies for the three products $([^{11}C]1:[^{11}C]2:[^{11}C]3)$ were $86.0{\pm}5.5%:5.0{\pm}3.4%:1.5{\pm}1.3%$ in MEK, $59.7{\pm}2.4%:4.7{\pm}3.2%:1.3{\pm}0.5%$ in CHO, $9.9{\pm}1.8%:2.0{\pm}0.7%:0.3{\pm}0.1%$ in DEK and $7.6{\pm}0.5%:0.0%:0.0%$ in DMF, respectively. Conclusion: The labeling efficiency of $[^{11}C]1$ was the highest when MEK was used as a reaction solvent. As results of mass spectrometry, 1 and 2 were conformed. 3 was presumed.

• Journal of Periodontal and Implant Science
• /
• v.25 no.3
• /
• pp.720-732
• /
• 1995

The use of transforming growth $factor-{\beta}1$ which functions as a potent biologic mediator regulating numerous activities of wound healing has been suggested for the promotion of periodontal regeneration. The mitogenic effects of transforming growth $factor-{\beta}1$ on human periodontal ligament cells and human gingival fibroblasts were evaluated by determining the incorporation of $[^3H]-thymidine$ into DNA of the cells dose-dependently. Cells were prepared with primary cultured fibroblasts and periodontal ligament cells from humans, and used in experiments were the fourth or sixth subpassage. Cells were seeded with serum free Dulbecco's modified Eagle medium containing 0.1% bovine serum albumine. The added concentrations of transforming growth $factor-{\beta}1$ were 0.25, 0.5, 1, 2.5, 5ng/ml and transforming growth $factor-{\beta}1$ were added to the quiescent cells for 24hours, 48hours, 72hours. They were labeled with lnCi/ml $[^3H]$ thymidine for the last 24hour of the each culture. The results were presented as the mean counts per minute (CPM) per well and S.D. of four determinations. The results were as follows. : The DNA synthetic activity of human gingival fibroblasts was increased dose-dependently by transforming growth $factor-{\beta}1$ at 24 hours, 48 hours and 72 hours. The maximum mitogenic effects were at the 48 hour application of transforming growth $factor-{\beta}1$. The DNA synthetic activity was generally more decreased at the 72 hour application than at the 48 hour the application of transforming growth $factor-{\beta}1$. The DNA synthetic activity of human periodontal ligament cells was increased dose-dependently by transforming growth $factor-{\beta}1$ at 24 hours and 48 hours. But the DNA synthetic activity was decreased at 5ng/ml of the 72 hour application. The maximum mitogenic effects were also at the 48 hour application of transforming growth $factor-{\beta}1$. The DNA synthetic activity of human periodontal ligament cells was generally more decreased at the 72 hour application than at the 48 hour application of transforming growth $factor-{\beta}1$. In the comparision of DNA synthetic activity between the human gingival fibroblasts and human periodontal ligament cells, the human gingival fibroblasts had more activity than the human periodontal ligament cells at all time application with the concentration of transforming growth $factor-{\beta}1$. In conclusion, transforming growth $factor-{\beta}1$ has an important roles in the stimulation of DNA synthesis in human periodontal ligament cells and human gingival fibroblasts, which means an increase in collagen synthesizing cells and thus, may be useful for clinical application in periodontal regenerative procedures.