• The Korean Journal of Nuclear Medicine
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• v.36 no.2
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• pp.102-109
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• 2002

Purpose : In gene therapy, tumor cells expressing the herpes simplex virus thymidine kinase are sensitive to prodrugs. Potential prodrugs IVDU and IVFRU were synthesized and radiolabeled with radioiodine for noninvasive imaging of herpes simplex virus type 1 gene expression. Material and Methods : 5-(2-trimethysilyl) vinyl-2'-deoxyuridine and 5-(2-trimethylsilyl)vinyl-2'-fluoro-2'-deoxyuridine, precursors of 5-(2--iodo)viny l-2'-deoxy uridine(IVDU) and 5-(2-iodo)-2'-vinyl-2'-deoxy-2'-fluororibofuranosyl uracil(IVFRU), were synthesized from reaction of trans-1-trimethylsillyl-2-tri-n-butylstannylethylene with 5-iodo-2'-deoxyuridine and 5-iodo-2'-fluoro-2'-deoxyuridine, respectively, on the condition of Pd catalyst. These precursors were separated from reaction mixture by silica gel column chromatography method. Each precursor was radioiodinated with radioiodine by mixing with ICI oxidizing agent. These radioiodinated compounds were purified with HPLC. Radiohalogen exchange has been shown to be effective for the synthesis of products with lower specific activity. Similarly, carrier-added and high specific activity products have been isolated in respectable radiochemical yields using ICI method. Results : Synthetic yield of precursors, IVDU and IVFRU were 43% and 18%, respectively. Radiochemical purity of both compunds was over 98%. Conclusion : We synthesized precursors of IVDU and IVFRU for monitoring of HSV1-tk gene expression. Radiotracers were radioiodinated with high radiolabeling yield by ICI method.

• Journal of Nutrition and Health
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• v.36 no.2
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• pp.125-132
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• 2003

The present study was attempted to investigate and compare the antioxidant potency of several well-know flavonoids, antioxidant vitamin and commercially available popular beverages. The antioxidant potency was assessed by the effect on reducing oxidative DNA damage of human lymphocytes. Cellular oxidative DNA damage was measured by SCGE (single-cell gel electrophoresis), also known as comet assay. Lymphocytes were pre-treated for 30 minutes with wide ranges of doses of apigenin, kaempferol, luteolin, myricetin, rutin, quercetin, $\alpha$-tocopherol (10,25,50,100,200,500,1000 $\mu$M) ,green tea extract or grape juice (10,50,100,250,500,1000 $\mu$g/mL) followed by a $H_2O$$_2$(100 $\mu$M) treatment for 5 min as an oxidative stimulus. The physiological function of each antioxidant substance on oxidative DNA damage was analyzed as tail moment (tail length $\times$ percentage migrated DNA in tail) and expressed as relative DNA damage score after adjusting by the level of control treatment. Cells treated with $H_2O$$_2$alone (positive control) had an extensive DNA damage compared with cells treated with phosphate buffered saline (PBS, negative control) or pre-treated with all the tested samples. Of all the six flavonoids, quercetin was the most potent antioxidant showing the lowest $ED_{50}$/ of 8.5 $\mu$g/mL (concentration to produce 50% protection of relative DNA damage). The antoxidant potency of individual flavonoids were ranked as follows in a decreasing order; luteolin (18.4 $\mu$g/mL), myricetin (19.0 $\mu$g/mL) , rutin (22.2 $\mu$g/mL) , apigenin (24,3 $\mu$g/mL) , kaempferol (25.5 $\mu$g/mL). The protective effect of $\alpha$-tocopherol was substantially lower (highest $ED_{50}$value of 55.0 $\mu$g/mL) than all the other flavonoids, while the protective effect was highest in green tea and grape juice with low ED5O value of 7.6 and 5.3, respectively. These results suggest that flavonoids, especially quercetin, and natural compounds from food product, green tea and grape juice, produced powerful anti-oxidative activities, even stronger than $\alpha$-tocopherol. Taken together, supplementation of antioxidants to lymphocytes followed by oxidative stimulus inhibited damage to cellular DNA, supporting a protective effect against oxidative damage induced by reactive oxygen species.

• Applied Biological Chemistry
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• v.42 no.2
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• pp.99-104
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• 1999

Soil actinomycetes of 703 strains were isolated from 25 sampling points in Cheju Island using 4 different media. Arginine glycerol salts agar containing soil extract was found to be the best medium for the isolation of soil actinomycetes. Soil samples from pasture land showed higher population and diversity of the actinomycetes than those from citrus field, forest, island, hill or valley. When the antibacterial activity of the 526 isolates was tested against three bacterial strains, Escherichia coli, Staphylococcus aureus and Pseudomonas solanacearum the frequency of the isolates with antibacterial activity varied much depending upon the media used for isolation and cultivation. BL106Ba, one of the 10 isolates that showed antibacterial activity against all the above 3 test strains, was chosen based upon the pH and heat stability of its antibacterial metabolites, and was identified as Streptomyces sp. based upon its cultural, morphological and physiological characteristics. The partially purified white crystalline substance obtained from the culture supematant of BL1063a through cation exchange chromatography(AG MP-50) and three times consecutive gel filtration(Sephadex G-10) showed high antimicrobial activity against gram positive and negative bacteria, but low activity against yeasts. The partially purified substance was found to contain at least four different compounds with antibacterial activity by both thin layer chromatography and high performance liquid chromatography.

• Journal of Life Science
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• v.25 no.6
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• pp.673-679
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• 2015

The culture conditions needed to maximize the production of laccase from Pholiota highlandensis mycelia were investigated. Among the tested media for laccase production, Coriolus versicolor medium (CVM; 2% dextrose, 0.4% peptone, 0.6% yeast extract, 0.046% KH₂PO₄, 0.1% K₂HPO₄, 0.05% MgSO₄·7H₂O) showed the highest activity for the enzyme. Then, to optimize culture conditions for laccase activity, the influences of various carbon, nitrogen, phosphorus, and inorganic salt sources in CVM were investigated. The optimum culture medium was 2% fructose, 0.4% peptone with 0.6% yeast extract, 0.05% NaH₂PO₄, and 0.05% MgSO₄·7H₂O as carbon, nitrogen, phosphorus, and inorganic salt sources, respectively. Several aromatic compounds in the medium enhanced laccase activity to varying degrees. Guaiacol induced maximum laccase production, yielding 114.1 U/ml laccase activity after cultivation for 11 days at 25℃. The optimum pH and temperature for laccase production were 8.0 and 35℃, respectively. Native polyacrylamide-gel electrophoresis (PAGE) followed by laccase-activity staining with 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) as the substrate was performed to identify the presence of laccase under the optimum conditions studied. Zymogram analysis of the supernatant culture showed an enzymatic band with a molecular mass of about 90 kDa.

• Journal of Life Science
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• v.25 no.2
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• pp.249-255
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• 2015

Schisandrae fructus [Schizandra chinensis (Turcz.) Baillon] is a medicinal herb widely used for treating various inflammatory and immune diseases in East Asian countries. The Schisandrae Semen essential oil (SSeo) from this plant has pharmacological activities, including antioxidant, antimicrobial, and antitumoral activities. Nevertheless, the biological activities and underlying molecular mechanisms of the potential anti-cancer effects of this oil remain unclear. In the present study, we investigated the potential inhibition of apoptosis signaling pathways by SSeo in human leukemia U937 cells and evaluated the underlying molecular mechanism. Exposure to SSeo resulted in a concentration-dependent growth inhibition due to apoptosis, which was verified by DNA fragmentation, the presence of apoptotic bodies, and an increase in the sub-G1 ratio. Induction of apoptotic cell death by SSeo was correlated with the down-regulation of members of the inhibitor of apoptosis protein (IAP) family (including X-linked inhibitor of apoptosis protein (XIAP), cIAP-1, and surviving) and anti-apoptotic Bcl-2, and with up-regulation of death receptor (DR) 4 and DR5, depending on dosage. SSeo treatment also induced Bid truncation, mitochondrial dysfunction, proteolytic activation of caspase-3, -8 and -9, and concomitant degradation of activated caspase-3 target proteins such as poly (ADP-ribose) polymerase. Taken together, these findings suggest that SSeo may be a potential chemotherapeutic agent for use in the control of human leukemia cells. Further studies are needed to identify its active compounds.

• Journal of Life Science
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• v.24 no.3
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• pp.234-241
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• 2014

To identify and isolate anticancer active compounds from Solanum nigrum, S. nigrum was extracted with MeOH and then fractionated with various organic solvents ($CH_2Cl_2$, EtOAc, n-BuOH, and $H_2O$). The cytotoxic effects of the MeOH extracts from S. nigrum and its organic solvent-soluble fractions were also tested in HT29 cells. All the MeOH extracts of S. nigrum and its organic-solvent extracts induced cytotoxicity in the HT29 cells. Among the extracts, $H_2O$ was the most effective. The $H_2O$ extract was purified further by repeated silica gel, Sephadex LH-20, Diaion HP- 20, and RP-18 column chromatography. An active anticancer compound, Des-N-26-methylene-dihydrotomatidine, was isolated with a molecular weight of 416 and a molecular formula of $C_{28}H_{48}O_2$. Analysis of the cytotoxic effects of Des-N-26-methylene-dihydrotomatidine on the HT29 cells compared to those of tomatine and tomatidine are similar in its structure, is higher than tomatidine above the 40 ${\mu}g/ml$ concentration, but lower than tomatine. This is the first study to describe the anticancer activity of Des-N-26-methylene-dihydrotomatidin, isolated from S. nigrum. Des-N-26- methylene-dihydrotomatidine seems to have potential as a natural bioactive compound.

• Journal of Life Science
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• v.23 no.3
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• pp.361-367
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• 2013

Hizikia fusiformis has been widely used in Oriental herbal medicine and health food. To identify antioxidation properties that contain natural bioactive substances, we investigated the distribution of active compounds existing in batches of organic solvent fractionation. A dried form of H. fusiformis was subjected to sequential fractionation using n-hexane, ethyl acetate, n-BuOH, and aqueous n-BuOH. The results showed that among the four isolated fractions, the n-BuOH fraction showed the highest antioxidation activities. The n-BuOH fraction was applied to reserve-phase silica gel column chromatography, which produced three fractions: BA, BB, and BC. Among these fractions, BB showed the highest antioxidation activities, which increased in a concentration-dependent manner. At a concentration of 1.0 mg/ml n-BuOH fraction, the activities of DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging and reducing power were approximately $45{\pm}0.14%$ and $1.34{\pm}0.23$, respectively. In addition, the activities of ${\beta}$-carotene-linoleic acid, hydrogen peroxide scavenging, and ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid)) radical scavenging were $76{\pm}0.12%$, $82{\pm}0.06%$, and $65{\pm}0.17%$, respectively. These findings suggest that the BB fraction contains potent antioxidation properties and that it could be used in the production of natural and functional foods.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.35 no.1
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• pp.11-17
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• 2009

Betamethasone propionate, an anti-inflammatory glucocorticosteroid, was detected in cosmetics with no indication on the label of this compound as an ingredient. The product was formulated as a topical spray or shampoo and labeled to contain zinc pyrithione as the active ingredient. A thin-layer chromatographic analysis was carried out on silica gel plates to provide a first indication about the presence of a compound with steroid structure and reactivity; then high-performance liquid chromatography (HPLC) separation allowed the identification of the corticosteroid agent and its quantification. To identify the corticosteroid agent from these commercial samples we collected the fractions suspected to have ketol steroids by prep HPLC and identified the compound as betamethasone propionate by NMR and MS spectrometry. Then we synthesized the standard for the betamethasone 17-propionate and 21-propionate and quantitate the corticosteroids from the sample by HPLC with that standards. By this method we identified the corticosteroid compounds from some commercial cosmetics such as zinc pyrithione sprays. The finding of betamethasone propionate in the products was shown by comparison to an authenticated standard of betamethasone propionate by retention time on reverse-phase HPLC. Two of the tested products contained betamethasone propionate at the levels of 0.005 ${\sim}$ 0.02% and the others were free of betamethasone propionate.

• Journal of the Korea Concrete Institute
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• v.24 no.3
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• pp.315-322
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• 2012

Alkali-activated slag (AAS) is the most obvious alternative materials that can replace OPC. But, AAS industrial usage as a structural material should be evaluated for its durability. Carbonation resistance is one of the most important factors in durability evaluation. Test results for 18 slag-based mortars activated by sodium silicate and 6 OPC mortars were obtained in this study to verify the carbonation property. Main variables considered in the study were flow, compressive strength before and after carbonation, and carbonation depth. Mineralogical and micro-structural analysis of OPC and AAS specimens prior to and after carbonation was conducted using XRD, TGA, FTIR FE-SEM. Test results showed that CHS was major hydration products of AAS and, unlike OPC, no other hydration products were found. After carbonation, CSH of hydration product in AAS turned into an amorphous silica gel, and alumina compounds was not detected. From the analysis of the results, it was estimated that the micro-structures of CSH in AAS easily collapsed during carbonation. Also, the results showed that this collapse of chemical chain of CSH lowered the compressive strength of concrete after carbonation. By increasing the dosage of activators, carbonation resistance and compressive strength were effectively improved.

• Journal of the Korean Society of Food Science and Nutrition
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• v.34 no.2
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• pp.162-166
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• 2005

Two flavonoids, 7-O-methyl-3',4'-didehydroxy quercetin (MDQ) and quercetin, isolated from Chinese propolis, which is the generic name for the resinous substance collected by honeybees from various plant sources, were tested for their antioxidant activity and protective effect against radiation-induced DNA damage in mouse lymphocytes. In antioxidant test, both compounds provided a dose-dependent scavenging effect on DPPH radical and a dose-dependent inhibitory effect on lipid peroxidation in mouse liver. Quercetin showed stronger scavenging and inhibitory effect than MDQ, and it also provided strong inhibition on superoxide anion radical generated in xanthine-xanthine oxidase system, but there was no inhibitory ability for MDQ. In comet assay using single cell gel electrophoresis, MDQ and quercetin showed a protective effect against DNA damage caused by gamma irradiation. They reduced DNA damage to 54% (p<0.01) and 53% (p<0.01) at 25 $\mu$mol, respectively. These results suggest that free radical scavenging seems to be associated with their catechol form on the B ring, and radioprotection appears to be a likely mechanism of antioxidant activity by these flavonoids.