• Korean Journal of Food Science and Technology
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• v.36 no.6
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• pp.1001-1007
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• 2004

Chloroform layer from methanol extract of Corni fructus (Cornaceae) showed strong antiproliferation effect on human cancer cell lines by SRB assay. Anticarcinogenic-active compound was isolated and purified by silica gel column and thin layer chromatograpies, and identified as ursolic acid ($3{\beta}$-hydroxyrus-12-ene-28-oic acid, MW:456) by mass and IR spectrophotometries, and $^1H-and\;^{13}C-NMRs$. The compound inhibited proliferation of A549 (human lung cancer cell line) and MCF-7 (human breast cancer cell line) cells in dose-dependant manner when treated for 48 hr. Inhibition rates of both cells were over 40% and 90% compared with control cells at the $30\;{\mu}g/mL\;and\;100\;{\mu}g/mL$, respectively. Morphology of cells treated with the compound for 15 hr at $10\;{\mu}g/mL$ was distorted with shrinked cell mass, and cell number was lower than that of control cells. Cell cycle analysis showed sub-G1 phase arrest in both cell lines following 15 hr exposure to the compound; % of cell phase increased to 11.7 and 11.2% compared to the control of 4.0% and 2.1% in A549 and MCP-7 cells, respectively.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.41 no.4
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• pp.375-382
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• 2015

Ginsenosides (ginseng saponin) as the one of important pharmaceutical compounds of ginseng and is responsible for the pharmacological and biological activities. These ginsenoside produces diverse small molecules ginsenoside which have more pharmacological activities including anti-wrinkle, anti-cancer and anti-oxidant effects. In the present study, we isolated bacteria using esculin agar, to produce ${\beta}$-glucosidase, and we focused on the bio-transformation of ginsenoside. Phylogenetic tree analysis was performed by comparing the 16S rRNA sequences; we identified the strain as Stenotrophomonas rhizopilae strain GFC09. In order to determine the optimal conditions for enzyme activity, the crude enzyme was incubated with 1 mM ginsenoside $Rb_1$. Bioconversion of ginsenoside $Rb_1$ were analyzed using TLC and HPLC. The crude enzyme hydrolyzed the ginsenoside $Rb_1$ along the following pathway: LB: $Rb_1{\rightarrow}Rd{\rightarrow}F_2$ into compound K, TSB: $Rb_1{\rightarrow}Rd{\rightarrow}F_2$. The structure of the hydrolyzed metabolites were identified by NMR. The activity screening tests showed that the conversion product induced the production of type I procollagen in a dose-dependent manner. These results suggested that hydrolyzed ginseng product containing the ginsenoside $F_2$ and compound K could be useful as an active ingredient for wrinkle-care cosmetics.

• Journal of the Korea Knowledge Information Technology Society
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• v.13 no.5
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• pp.607-614
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• 2018

Oryeong-san is a prescription widely used for diseases where water is stagnant because it has the effect of circulating the water in the body and releasing it into the urine. In order to investigate the mechanisms of oryeong-san, we in this paper construct and analysis the compound-target network of medicinal materials constituting oryeong-san based on a systems pharmacology approach. First, the targets related to the 475 chemical compounds of oryeong-san were searched in the STITCH database, and the search results for the interactions between compounds and targets were downloaded as XML files. The compound-target network of oryeong-san is visualized and explored using Gephi 0.8.2, which is an open-source software for graphs and networks. In the network, nodes are compounds and targets, and edges are interactions between the nodes. The edge is weighted according to the reliability of the interaction. In order to analysis the compound-target network, it is clustered using MCL algorithm, which is able to cluster the weighted network. A total of 130 clusters were created, and the number of nodes in the cluster with the largest number of nodes was 32. In the clustered network, it was revealed that the active compounds of medicinal materials were associated with the targets for regulating the blood pressure in the kidney. In the future, we will clarify the mechanisms of oryeong-san by linking the information on disease databases and the network of this research.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.15
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• pp.6581-6589
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• 2015

Background: Previously, stingless bee (Trigona spp.) products from East Kalimantan, Indonesia, were successfully screened for in vitro antiproliferative activity against human cancer derived cell lines. It was established that propolis from T. incisa presented the highest in vitro cytotoxicity against the SW620 colon cancer cell line (6% cell survival in $20{\mu}g/mL$). Materials and Methods: Propolis from T. incisa was extracted with methanol and further partitioned with n-hexane, ethyl acetate and methanol. The in vitro cytotoxicity of the extracts was assessed by the MTT assay against human colon (SW620), liver (Hep-G2), gastric (KATO-III), lung (Chago) and breast (BT474) cancer derived cell lines. The active fractions were further enriched by silica gel quick column, absorption and size exclusion chromatography. The purity of each fraction was checked by thin layer chromatography. Cytotoxicity in BT-474 cells induced by cardanol compared to doxorubicin were evaluated by MTT assay, induction of cell cycle arrest and cell death by flow cytometric analysis of propidium iodide and annexin-V stained cells. Results: A cardol isomer was found to be the major compound in one active fraction (F45) of T. incisa propolis, with a cytotoxicity against the SW620 ($IC_{50}$ of $4.51{\pm}0.76{\mu}g/mL$), KATO-III (IC50 of $6.06{\pm}0.39{\mu}g/mL$), Hep-G2 ($IC_{50}$ of $0.71{\pm}0.22{\mu}g/mL$), Chago I ($IC_{50}$ of $0.81{\pm}0.18{\mu}g/mL$) and BT474 (IC50 of $4.28{\pm}0.14{\mu}g/mL$) cell lines. Early apoptosis (programmed cell death) of SW620 cells was induced by the cardol containing F45 fraction at the $IC_{50}$ and $IC_{80}$ concentrations, respectively, within 2-6 h of incubation. In addition, the F45 fraction induced cell cycle arrest at the G1 subphase. Conclusions: Indonesian stingless bee (T. incisa) propolis had moderately potent in vitro anticancer activity on human cancer derived cell lines. Cardol or 5-pentadecyl resorcinol was identified as a major active compound and induced apoptosis in SW620 cells in an early period (${\leq}6h$) and cell cycle arrest at the G1 subphase. Thus, cardol is a potential candidate for cancer chemotherapy.

• Journal of Periodontal and Implant Science
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• v.35 no.1
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• pp.87-98
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• 2005

The purpose of present study was to investigate the effects of physiologically active compound (SD62-122) from Phlomidis Radix on the cell cycle progression and its molecular mechanism in human gingival fibroblasts(HGFs). For this purpose, fibroblasts were isolated and cultured from excisioned gingiva during crown lengthening procedure in healthy adult. The following parameter were evaluated that there are cell number counting, MIT assay, cell cycle progression, western blot analysis. The cell number and MIT assay of primary cultured fibroblast was not increased at 2 days but significant increased compare to negative control at 3days(p<0.05). S phase was increased and G1 phase decreased in both $10^{-8}M$ and $10^{-9}M$ of SD62-122 in cell cycle analysis. The cell cycle regulation protein levels of Cyclin $D_1$, Cyclin E, cdk 2, cdk 4 and cdk 6 were increased compare to control in both $10^{-8}M$ and $10^{-9}M$ of SD62-122. The protein levels of p21 and p53 were decreased compare to control, but the level of pRb was not changed compare to control in $10^{-9}M$ of SD2-122. These results suggested that physiologically active compound (SD62-122) isolated from Phlomidis Radix increases the cell proliferation and cell cycle progression in HGFs, which is linked to increased cell cycle regulation protein levels of Cyclin $D_1$, Cyclin E, cdk 2, cdk 4 and cdk 6, and decreased the levels of p21, p53.

• Korean Journal of Food Science and Technology
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• v.50 no.2
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• pp.123-131
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• 2018

The objective of this study was to evaluate the effect of roasting degree of barley on aroma characteristics of boricha (barley tea) using solvent-assisted flavor evaporation-gas chromatography-mass spectrometry and gas chromatography-olfactometry. Fifteen volatile compounds including pyrazine, ethylpyrazine, butyrolactone, and guaiacol were considered important volatile compounds, which are generated by roasting barley, because concentrations of those volatiles were significantly increased (p<0.05) as roasting degree of barley was darker. Guaiacol (smoky), furfuryl alcohol (burnt sugar), and furfural (caramel) were detected as aroma-active compounds of boricha with high intensity. Aroma intensity of aroma-active compounds in boricha increased with increase in roasting degree of barley. However, one unknown compound with burnt smell was detected as off-flavor in dark roasted barley. Therefore, it is implied that medium roasting of barley is desirable during boricha manufacturing. Furthermore, boricha manufactured with steamed barley contained more abundant volatile flavor compounds, which may lead to better aroma quality of boricha.

• Archives of Pharmacal Research
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• v.19 no.4
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• pp.312-316
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• 1996

A series of N-Cbz${alpha}$-aminosucinimides (1), combining common moieties of various anticonvulsants such as N-CO-C-N and cyclic imide in a single molecule, were synthesized from the corresponding (R)- and (S)-N-Cbz-aspartic acid (2). And their in vivo anticonvulsant evaluations in MES and PTZ test were investigated. And also the rotorod test for neurotoxicity was investigated. All the tested compounds (1), except 1c and 1f, showed significant anticonvulsant activities in both MES and PTZ test. And the most active compound among them in MES test was (R)-N-Cbz-${alpha}$-amino-N-methylsuccinimide (1b) $(ED_50/=52.5 mg/kg)$ and (S)-N-Cbz-aminosuccinimide((1d) was most active in PTZ test $(ED_50/=78.1 mg/kg)$. And the $TD_50$ values of the tested compounds were above 117.5 mg/kg. These pharmacological data were comparable to those of currently available anticonvulsants. And also we found that the pharmacological effects were dependent on their N-substituted alkyl chains and their stereochemistry.

• Archives of Pharmacal Research
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• v.9 no.3
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• pp.163-167
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• 1986

Twenty six urea analogues, most of which have already been approved for human use, were tested for their antiurease activity in vitro. Cell-free extracts obtained from a clinical isolate of Proteus mirabilis was used as the source of enzyme. Acetohydroxamic acid which is a proven potent urease inhibitor but not approved for human use was again shown to be the most active compound among the tested. Phenacemide, cycloserine, and deferoxamine were demonstrated to be moderate inhibitors. Oxtetracycline, trimethoprim, and cefamandole revealed a demonstrable antiruease activity, but only at very high concentrations. The antiurease activity of cycloserine, trimethoprim, and cefamandole was pH dependent-only active at acidic pH. The inhibitory activity of acetohydroxamic acid however was independent of change in pH. The inhibitory activity of acetohydroxamic acid however was independent of change in pH. Hydrogen ion concentration plays an important role in urease activity and acidification (pH 5. 5) alone eliminates approximately 65% of the enzymic activity. Adjustment of pH therefore appears to be an important adjunct in reducing unrease activity and should always be studied to maximize the effcacy of antiurease compounds under investigation.

• Journal of the Korean Applied Science and Technology
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• v.33 no.2
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• pp.342-351
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• 2016

The bioactive compound and antioxidant property of Korean yam (Dioscorea batatas DECNE.) were studied using in vitro methods. Yam available in Korea was analyzed for lycopene, chlorophyll a, b, tannin, phytic acid and total saponin contents. 70% Methanol, 70% ethanol and chloroform-methanol mixture (CM, 2:1, v/v) were used to extract yam. Then the antioxidant activity evaluated through ferrous ion chelating activity, ${\beta}$-carotene bleaching method, lipid peroxidation inhibition and nitric oxide (NO) radical scavenging activity. 70% Methanol extract showed the highest ferrous ion chelating activity and NO radical scavenging activity. And CM extract was the most effective in inhibition of linoleic acid peroxidation evaluated by ${\beta}$-carotene bleaching assay and lipid peroxidation inhibition assay. Based on the results obtained, yam is a potential active ingredient that could be applied in antioxidation as well as bio-health functional food to take a good part in prevention of human diseases and aging.

• YAKHAK HOEJI
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• v.28 no.6
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• pp.313-319
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• 1984

Phenylurea, phenylthiourea, benzylcarbamate and toluenesulfonate of L-alanyl-L-proline(comp. $3{\sim}6$) were synthesized and their effects against angiotensin-converting enzyme (ACE) were tested. Comp. 3 showed only mild inhibitory activities against ACE while comp. $4{\sim}6$ were inert indicating that those functional groups were not suitable for interactions with ACE. Ortho-hydroxy- or ortho-carboxy-benzamide of proline (comp. 7) and phenylalanine (comp. 8 and 9) were also tested. Of the benzamides, ortho-hydroxy function was unsuitable to exert inhibitory activities against ACE. Ortho-carboxy group of 9 seemed to have mild interactions with active site of ACE possibly because of the shorter distance between the amide and ortho-carboxyl group of the compound than the corresponding two active sites of the enzyme.