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Detection of N-Acetyltranylcypromine and Glucuronide of Phenyl-Hydroxylated N-Acetyltranlcypromine from Tranylcypromine-Dosed Rat Urine : Pharmacological Implications

  • Kang, Gun-Il;Choi, Hee-Kyung
    • Archives of Pharmacal Research
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    • v.9 no.2
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    • pp.99-110
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    • 1986
  • In order to use for metabolic studies of tranylcypromine (TCP), TCP-phenyl-$d_{5}$ was synthesized via the intermediates, 3-benzoylpropionic acid-$d_{5}$ and trans-2-phenylcyclopropanecarboxylic acid-$d_{5}$ -TCP(0.22 mmole/kg) and its deuterated analog were administered s. c. to the rats and GC/MS analyses of the urines led to the detection of N-acetyltranylcypromine (ATCP) and glucuronide conjugate of phenyl-hydroxylated ATCP. MAO activities in rat brain were measured using serotonin as the substrate. In vitro $IC_{50}$ of ATCP was determined to be $10^{-3}M$. The inhibitions by ATCP were not dependent on the preincubation time and were reversed by washing sedimented mitochondrial pellets after the preincubation. In vivo MAO inhibitions at various times of 0.5, 1.5, 3, 6, 12, and 23 hr after the administration of 0.4 mmole/kg (i. p. ) of ATCP were found to be 0.13, 73, 90, 89, and 74 %, respectively. Similarly, the inhibition percents by 0.015 mmole/kg (i. p. ) of TCP were 94, 99, 95, 91, 71 and 49%. The results strongly suggest that deacetylated product of ATCP may account for its in vivo MAO inhibition. The relationship between the metabolism via phenyl-hydroxylation and the in vivo potency of TCP was examined by QSAR study and it was found that groupings discriminating between the compounds with p-substituents and those without them only ensure high correlations, suggesting that ring-hydroxylation which occurs at the para position in most of the compounds is a determining factor to the potency of TCP.

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Antitumor Effects of Kluyveromyces marxianus TFM-7 Isolated from Kefir

  • Lee, Hyun-Jung;Nam, Bo-Ra;Kim, Jin-Man;Kim, Ji-Yeon;Paik, Hyun-Dong;Kim, Chang-Han
    • Food Science and Biotechnology
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    • v.16 no.1
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    • pp.133-137
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    • 2007
  • The Strain TFM-7, Which has an antitumor effect, was isolated from Kefir and identified based on analysis using the API 50 CHL kit and 265 rDNA sequencing. Strain TFM-7 was confirmed to belong to the genus Kluyveromyces. Analysis of the 265 rDNA nucleotide sequences found strain TFM-7 to be related to Kluyveromyces marxianus. NRRL Y-828IT. K. marxianus. TFM-7 was cultured with potato dektrose broth medium at $27^{\circ}C$ for 72 hr, and its inhibition effects on the proliferation of seven tumor cell lines and a normal cell line were assessed using the MTT assay. The antitumor effects and growth characteristics of K. marxianus TFM-7 were investigated during a culture period of 7 days. By the $3^{rd}\;day$, K. marxianus TFM-7 showed a dry cell weight 2.39 g/L, a pH of 4.39, an ethanol content of 0.89%, and an inhibition effect on the proliferation of seven tumor cell lines above 50%, except for A-549 tumor cell line. K. marxianus TFM-7 was the most effective at inhibiting the growth of Hep-2 cell line among all tumor cell lines tested. Growth inhibition of a normal cell line, NIH/3T3, was less than 35%, suggesting a decreased level of cytotoxicity toward normal cells. These results indicate that K. marxianus TFM-7 may have used as a yeast strain with antitumor activity.

Survey on Fibromyalgia Syndrome (섬유조직염 환자에 대한 기초 조사연구)

  • Han, Sang-Sook;Kang, Hyun-Sook
    • Journal of muscle and joint health
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    • v.4 no.1
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    • pp.74-86
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    • 1997
  • This investigation has been conducted based on the medical chart of 344 patients who have been diagnosed of fibromyalgia syndrome during Oct. 9, 1996 through Nov. 20 at the Rheumatism Hospital of H. University located in Seoul. 280 which have been included in the analysis. 1. Only one patient was male in 280 patients, age distribution was from 28 to 76, in which the average age was 52.4. 2. Percentage of treatment duration was 6 months in 46.1%, 3 years in 22.1% and 2 years in 12.5%. Considering these results, it can be predicted that the number of patients might be increased and accumulated in the future. 3. Percentage of patients having primary fibromyalgia syndrome was 39.3%, having combination with osteoarthritis was 36.7% and the rest case have combination with rheumatoid arthritis at the same time. 4. The percentage of cases having patients 10-12 tender points was 37.1%, while the most of cases have pain at 12-19 tender points. The common locations of the tender point were at lateral epicondyle of elbow in 92.0%, at midpoint of upper border Trapezius in 84.8%, at upper part of scapula Supraspinatus in 82.9%, at medial fat pad proximal to the joint line knee in 81.85%, at intertransverse of $C_{5-7}$ Low cervical in 73.4% and at 2nd distal costochondral Junction 2nd rib in 72.0%. And most of the patients had joint functional disability at all in 47.1% with average 2.41 joint functional disability. 5. Age was not a variable influencing the number of tender points and the number of joint functional disability.

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Purification and Characterization of an Intracellular NADH: Quinone Reductase from Trametes versicolor

  • Lee, Sang-Soo;Moon, Dong-Soo;Choi, Hyoung-T.;Song, Hong-Gyu
    • Journal of Microbiology
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    • v.45 no.4
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    • pp.333-338
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    • 2007
  • Intracellular NADH:quinone reductase involved in degradation of aromatic compounds including lignin was purified and characterized from white rot fungus Trametes versicolor. The activity of quinone reductase was maximal after 3 days of incubation in fungal culture, and the enzyme was purified to homogeneity using ion-exchange, hydrophobic interaction, and gel filtration chromatographies. The purified enzyme has a molecular mass of 41kDa as determined by SDS-PAGE, and exhibits a broad temperature optimum between $20-40^{\circ}C$, with a pH optimum of 6.0. The enzyme preferred FAD as a cofactor and NADH rather than NADPH as an electron donor. Among quinone compounds tested as substrate, menadione showed the highest enzyme activity followed by 1,4-benzoquinone. The enzyme activity was inhibited by $CuSO_4,\;HgCl_2,\;MgSO_4,\;MnSO_4,\;AgNO_3$, dicumarol, KCN, $NaN_3$, and EDTA. Its $K_m\;and\;V_{max}$ with NADH as an electron donor were $23{\mu}M\;and\;101mM/mg$ per min, respectively, and showed a high substrate affinity. Purified quinone reductase could reduce 1,4-benzoquinone to hydroquinone, and induction of this enzyme was higher by 1,4-benzoquinone than those of other quinone compounds.

Vascular Plants of Major Sites in Bukhansan National Park -A Case Study on Bukhansan Dulegil, Jingwan-dong Wetland, Bukhan-dong Cheolgeoji- (북한산국립공원 주요지역의 관속식물상 -북한산 둘레길, 진관내동 습지, 북한동 철거지를 대상으로-)

  • Oh, Hyun-Kyung;Han, Yun-Hee;Cho, Woo
    • Journal of the Korean Society of Environmental Restoration Technology
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    • v.15 no.1
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    • pp.35-51
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    • 2012
  • The vascular plants in Bukhansan Dulegil, Jingwan-dong Wetland and Bukhan-dong Cheolgeoji were listed 432 taxa (8.9% of all 4,881 taxa of vascular plants); 95 families, 274 genera, 345 species, 2 subspecies, 69 varieties and 16 forms. Divided into woody plants were 145 taxa (33.6%) and herbaceous plants were 287 taxa (66.4%). The Bukhansan Dulegil were listed (Myeongsang-gil 159 taxa, Huingureum-gil 227 taxa, Wooyiryeong-gil 216 taxa, Banghakdong-gil 139 taxa, Boru-gil 199 taxa), Jingwan-dong Wetland were listed 147 taxa and Bukhan-dong Cheolgeoji were listed 129 taxa. Based on the list of rare plants by Korea Forest Service and Korea National Arboretum were Viola albida Palibin (Violaceae), Iris minutiaurea Makino (Iridaceae) and Korea National Arboretum were endemic plants, Philadelphus schrenkii Rupr. var. schrenkii (Saxifragaceae), Weigela subsessilis L.H. Bailey (Caprifoliaceae). Based on the list of floristic regional indicator plants by Korean Ministry of Environment were total 22 taxa; Wisteria floribunda DC. for. floribunda in class IV, 3 taxa (Betula davurica Pall., Mukdenia rossii Koidz., Glechoma grandis Kuprian., etc.) in class III, 5 taxa (Acer triflorum Kom., Viola orientalis W. Becker, Heloniopsis koreana Fuse & Al., etc.) in class II and 13 taxa (Camptosorus sibiricus Rupr., Clematis patens C. Morren & Decne., Cirsium pendulum Fisch. ex DC., etc.) in class I. Based on the list of naturalized plants, 16 families, 35 genera, 37 species, 3 varieties, 1 form, total 41 taxa (Rumex crispus L., Abutilon theophrasti Medicus, Panicum dichotomiflorum Michx. etc.), naturalization rate was 9.5% of all 432 taxa of vascular plants and urbanization index was 13.3% of all 309 taxa of naturalized plants. Ecosystem disturbing wild plants were 5 taxa; Rumex acetocella L., Ambrosia artemisiifolia L., Ambrosia trifida L. var. trifida, Eupatorium rugosum Houtt., Aster pilosus Willd.

Effect of Thyroid Hormones and Albinism during Metamorphosis of Flounder, Paralichthys olivaceus under Low Temperature Stress (넙치 변태기에 있어 저수온 스트레스가 갑상선 호르몬과 백화현상에 미치는 영향)

  • YOO Jin Hyung;TAKEUCHI Toshio;JEONG Kwan Sik
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.36 no.1
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    • pp.65-67
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    • 2003
  • Flounder (Paralichthys olivaceus) fish goes through metamorphosis in the larvae phase. In this phase, it secretes much thyroid hormone to control metamorphosis. Sharp change in the environment and nutrition deficiency may cause stress in the metamorphosis phase. It leads to interfering with the development of thyroid hormone and finally inhibits the normal growth of larvae. In this study, the correlation between the change in thyroid hormones and the albinism appearance was examined by growing them with low temperature ($13^{\circ}C$) stress over the premetamorphosis stages (stage $D\~F$) of flounder metamorphosis. Albinism rate was $15\%$ in the low temperature group and $25\%$ in the control goup. $T_{4}\;and\;T_{3}$ of the control group tended to increase from stage F as larvae grew. $T_{4}$ increased 2 times compared to the control group as 72 ng/g at stage H, the increasing phae of water temperature, in the low temperature group. $T_{3}$ increased 8 times compared to the control group as 2.9 ng/g at stage E, the decreasing phase of water temperature. Therefore, it is judged that the albinism appearance of flouner is caused from the sharp increase in $T_{3}$ by the inappropriate secretion of thyroid hormone.

Nitrongen and Phosphorus Removal using Elutriated Acids of Food Waste as an External Carbon Source in SBR (음식물쓰레기 세정산발효액을 외부탄소원으로 주입한 SBR 공정에서 질소 및 인 제거)

  • Kwon, Koo-ho;Kim, Si-won;Lee, Min-jae;Min, Kyung-sok
    • Journal of Korean Society on Water Environment
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    • v.22 no.3
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    • pp.462-467
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    • 2006
  • An improvement of nitrogen and phosphorus removal in SBR using the elutriated acids from the food waste as an external carbon source was investigated in this study. The food waste was elutriated at $35^{\circ}C$ and pH 9 to produce the external carbon source. The elutriate of food waste were continuously collected. The elutriated liquid contained VFAs of 39,180 mg/L representing soluble COD of 44,700 mg/L. The SBR showed poor denitrification and EBPR (enhanced biological phosphorus removal) without elutriated VFAs addition. An average denitrification rate was 0.4 mg NOx-N/g MLVSS/day. In turn, EBPR was also inhibited by this poor denitrification because the remaining nitrate in anaerobic phase resulting a poor denitrification. On the other hand, the denitrification in anoxic phase significantly improved with an elutriated VFAs addition. Nitrate removal was 82% while the denitrification rate was 2.9 mg NOx-N/g MLVSS/day with 18.4 mL/cycle of elutriated VFAs. With the enhanced denitrification, nitrate concentration in anaerobic phase could effectively be controlled to a very low level. The elimination of nitrate inhibition in anaerobic phase resulted enhancement of EBPR. The specific phosphate release rate was $1.9mg\;PO_4^{3-}-P/g\; MLVSS/day$ with less than 0.5 mg/L of $PO_4^{3-}-P$ concentration.

Mosquito Species Composition and Plasmodium vivax Infection Rates on Baengnyeong-do (Island), Republic of Korea

  • Foley, Desmond H.;Klein, Terry A.;Lee, In-Yong;Kim, Myung-Soon;Wilkerson, Richard C.;Harrison, Genelle;Rueda, Leopoldo M.;Kim, Heung-Chul
    • Parasites, Hosts and Diseases
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    • v.49 no.3
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    • pp.313-316
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    • 2011
  • Vivax malaria is a significant military and civilian health threat in the north of the Republic of Korea (ROK). The island of Baengnyeong-do is the westernmost point of the ROK and is located close to the southwestern coast of the Democratic People's Republic of Korea (DPRK). Mosquitoes were collected using a black light trap on Baengnyeong-do, and Anopheles spp. were assayed by PCR, to identify the species, and screened for sporozoites of Plasmodium vivax. Of a subsample of 257 mosquitoes, Anopheles lesteri was the most frequently collected (49.8%), followed by Anopheles sinensis (22.6%), Anopheles pullus (18.7%), Anopheles kleini (7.8%), and Anopheles belenrae (1.2%). The overall sporozoite rate was 3.1%, with the highest rates observed in An. kleini (15.0%), An. sinensis (5.2%), and An. lesteri (1.6%). No sporozoite positive An. pullus or An. belenrae were observed. The results extend our knowledge of the distribution and potential role in malaria transmission of An. kleini, An. lesteri, and An. sinensis, for an area previously considered to be at a low risk for contracting vivax malaria.

Effect of Different Contents of Nuruk Extract on Fermentation Characteristics of Kwahaju (a Korean Traditional Alcoholic Beverage) (수국 첨가량이 과하주의 발효 특성에 미치는 영향)

  • Kim, In-Ho;Park, Wan-Soo;Koo, Young-Jo
    • Journal of the Korean Society of Food Culture
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    • v.11 no.5
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    • pp.711-719
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    • 1996
  • Fermentation characteristics of kwahaju (a typical Korean traditional alcoholic beverage) base were investigated during fermentation with different contents of nuruk (Korean-style bran koji) extract. The nuruk extract which was prepared by incubating the mixture of nuruk powder and water at $25^{\circ}C$ overnight and by filtering it was used to be 0.6%, 2.7%, 5% and 10% (v/v). Total and reducing sugar contents as well as acidity of the kwahaju base with 0.6% nuruk extract were higher than those with 2.7%, 5% and 10% at the fermentation end. Final pH values of all the base samples were ranged from 3.3 to 4.1. Alcohol concentrations of the base samples with 2.7%, 5% and 10% nuruk extract were higher than those with 0.6%. Microbial growth rate was great and inner temperature was high in the sample with high content of nuruk extract, but fermentation period was short. Total sugar consumption and alcohol production increased as the content of nuruk extract increased, but total acid production decreased. The base sample with 10% nuruk extract showed the most excellent fermentation efficiency. Fusel oil content of the base sample with 2.7% nuruk extract was the highest (457.3 ppm), and those wity 5% and 10% nuruk extract were 438.9 ppm and 442.6 ppm, respectively. The sample with 0.6% nuruk extract had the lowest content (409.5 ppm). Sensory evaluation of both the kwahaju base and kwahaju mix with 25% and 40% alcohol by adding soju (Korean distilled liquor) showed that the base with 2.7% nuruk extract had the highest score, and that the kwahaju mix with 25% alcohol had higher score than that with 40%. The sensory results on overall desirability were consistent to those on color and alcohol concentration, and it turned out that the two factors were important to make kwahaju.

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Changes in the Contents of Sugar, Organic Acid, Free Amino Acid and Nucleic Acid-Related Compounds during Fermentation of Leaf Mustard-Kimchi (갓김치 숙성중 당, 유기산, 유리아미노산 및 핵산관련 물질 함량의 변화)

  • 박석규;조영숙;박정로;문주석;이용수
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.24 no.1
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    • pp.48-53
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    • 1995
  • Changes in the contents of sugar, organic acid, free amino acid and uncleic acid-related compounds of leaf mustard-Kimchi during fermentation at 5~7$^{\circ}C$ were investigated. The leaf mustard-Kimchi was formulated with 4kg leaf mustard, 120g garlic, 80g ginger, 540ml salted anchovies, 1kg green onion, 200g red pepper powder, 200g ground red pepper, 60g whole sesame and 600ml glutinous rice paste. Changes in pH and acidity were relatively slow. Major free sugars were glucose(0.13%) and maltose(0.42%), and residual sugars(0.03-0.04%) were also detected after 32 days of fermentation. Major free amino acids containing more than 26.5mg% were proline, glutamic acid, alanine and histidine. Contents of total free amino acids increased from 244.8 to 397.2mg% by 24 days of fermentation. Of non-volatile organic acid, lactic acid was the most abundant(119.3mg%), and its content increased markedly after 10 days of fermentation. Other organic acids(below 53.1mg%) observed were malic, oxalic and citric acid. Contents of nucleic acid-related compounds were high in the order of hypoxanthine(22.8mg%), IMP(8.3mg%) and GMP(6.9mg%). Hypoxanthine content increased by 10 days(27.3mg%) and decreased thereafter, while the others decreased gradually during the overall period of fermentation.

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