• Title/Summary/Keyword: EH-1

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Development of Soluble Epoxide Hydrolase Inhibitor Screening Methods for Discovery of Drug Candidate in Cardiovascular Diseases (심혈관계 질환 치료제 후보물질 발굴을 위한 Soluble Epoxide Hydrolase 억제평가 방법 개발)

  • Lee, Gwan-Ho;Kim, Bong-Hee;Kim, Sang-Kyum
    • YAKHAK HOEJI
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    • v.56 no.1
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    • pp.42-47
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    • 2012
  • Soluble epoxide hydrolase (sEH) is a metabolic regulator of epoxyeicosatrienoic acids (EETs). EETs have many beneficial effects, vasodilation, anti-diabetes, anti-inflammation, cardiovascular protection, renal protection. Therefore, selective sEH inhibitors have a potential for treating these diseases. In the present study, screening methods for sEH inhibitors using PHOME ((3-phenyl-oxiranyl)-acetic acid cyano-(6-methoxynaphthalen-2-yl)-methyl ester) and 14-15-EET as substrates were established. To determine selectivity, microsomal epoxide hydrolase (mEH) inhibition assay was also developed using styrene oxide as a substrate of microsomal epoxide hydrolase. Our results obtained from 12-[[(tricyclo[3.3.1.13,7]dec-1-ylamino)carbonyl]amino]-dodecanoic acid (AUDA) used as a positive sEH inhibitor and valpromide used as a positive mEH inhibitor showed that these methods are useful for discovery of drug candidates.

Study of Eh-jang (Korean Fermented Aquatic Products) Culture in Asia (아시아속의 한국어장문화(韓國魚醬文化)에 관한 연구(硏究))

  • Lee, Sung-Woo
    • Journal of the Korean Society of Food Culture
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    • v.1 no.4
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    • pp.371-382
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    • 1986
  • Eh-jang (fermented aquatic products) of Asia can be classified 4 groups, those are Chot-kal (salted fish guts), Chot-kal Paste, Eh-ganjang (fish sauce) and Shic-hae (lactic acid fermented fish products). The native place of Eh-jang and rice culture is almost same and Eh-jang had been spread out all the area of Asia along with rice culture. Korea has variety of Chot-gal and consumes much Chot-gal that Korea is the culture area of both soybean sauce and Chot-gal. Eh-ganjang had been edible all area of Korea during Chosun Dynasty, but it remains only Southern part of Korea. Korean Chot-gal paste is produced as a form of Kon-chang-yi-chot. Korean Shic-hae had been edible all area of Korea during Chosun Dynasty, but remains at the east coast and some area of Hwang-hae Do and Kyung-sang-nam-do.

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Molecular Engineering of Epoxide Hydrolases for Production of Enantiopure Epoxides (분자공학 기반의 광학활성 에폭사이드 제조용 epoxide hydrolase 생촉매 개발)

  • Kim, Hee-Sook;Lee, Eun-Yeol
    • Journal of Life Science
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    • v.16 no.1
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    • pp.168-174
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    • 2006
  • Enantiopure epoxides are valuable intermediates for the asymmetric synthesis of enantiopure bioactive compounds. Microbial epoxide hydrolases (EHs) are versatile biocatalysts for the preparation of enantiopure epoxides by enantioselective hydrolysis of cheap and easily available racemic epoxide substrates. EHs are commercially potential biocatalysts due to their characteristics such as high enantioselectivity, cofactor-independent catalysis, and easy-to-prepare catalysts. In this paper, recent progresses In molecular engineering of EHs are reviewed to evaluate the commercial feasibility of EH-catalyzed hydrolytic kinetic resolution for the production of enantiopure epoxides.

Processing and Characteristics of Pearl Oyster (Pinctada fucata) Extracts (진주조개(Pinctada fucata) 추출물의 가공 및 품질특성)

  • Kang, Jeong-Goo;Kang, Su-Tae;Kang, Jin-Yeong;Nam, Gi-Ho;Lee, Sung-Man;Oh, Kwang-Soo
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.40 no.6
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    • pp.343-349
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    • 2007
  • This study examined the effective utilization of pearl processing by-products. Three extracts of hot-water extract (WE), hydro-cooked extract (HE), and two-step enzymatic hydrolysate (EH) were prepared from pearl oyster muscle, and their characteristics were examined. The moisture, crude protein, volatile basic nitrogen (VBN), and amino-N contents were 97.5-98.0%, 0.5-1.3%, 2.1-4.9 g/100 mL, and 35.0-74.5 g/100 mL, respectively. EH had the lowest VBN and highest amino-N contents. In addition, EH had the highest yields. In terms of its functional properties, EH inhibited angiotensin-I converting enzyme ($IC_{50}$, 1.39 mg/mL) more strongly than the other extracts ($IC_{50}$, 4.17-7.95 mg/mL). The free amino acid contents of WE, HE, and EH were 661, 470 and 1,150 mg/100 mL, respectively. Major amino acids were taurine and glutamic acid. Major inorganic ions were Na, Mg, and Ca. Contents of taste compounds, such as free amino acids, inorganic ions, and quaternary ammonium bases, differed significantly according to the extract methods. Based on the results of chemical experiments and sensory evaluation, the quality of EH was superior to the other extracts, and EH is suitable for use in natural flavoring materials.

Sensory Characteristics of Granular Tea and the Components of Mulberry Fruit Extracts by Different Extraction Process (오디의 추출 공정에 따른 성분 변화 및 분말 과립차의 관능 특성)

  • Ryu, Il-Hwan;Kwon, Tae-Oh
    • Korean Journal of Medicinal Crop Science
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    • v.20 no.5
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    • pp.331-338
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    • 2012
  • In the present work, mulberry fruit extracts by four extraction processes, namely wet pressing extraction (WPE), hot-water extraction (HWE), enzymatic hydrolysis (EH), and lactic-acid bacteria fermentation (LBF) by Lactobacillus plantarum TO-2100, were analyzed for nutrients and functional compounds. The sugar contents of extracts by WPE, HWE, EH, and LBF were 12.0, 10.9, 14.5, and 14.3 brix, respectively, and the extraction yields by EH and LBF were 1.65 and 1.50 times higher than those by WPE. Among the organic acids, tartaric acid and malic acid contents were the highest in the extracts by WPE. Acetic acid was best extracted by LBF, and citric acid was best extracted by EH. Lactic acid was detected only in LBF. The extracts by EH showed the highest contents of all vitamins with an exception that the extracts by LBF showed the highest contents of the folic acid, vitamin B12, and vitamin C. We also noted that vitamin B group was not detected in the extracts by LBF. The extracts by EH showed the highest contents of all the amino acids, whereas LBF showed the lowest. Polyphenol contents of extracts by EH and LBF were 3.05 and 2.51 times more than those by WPE respectively. Anthocyanin contents were 7.66, 7.14 times higher for EH and LBF compare to WPE. We manufactured mulberry fruit granular teas with different compositions and tested them for their sensory characteristics. We found that 15% mulberry fruit extracts by enzymatic hydrolysis and 85% dextrin composition gave the most satisfactory result.

Energy Harvester on a Ship Propulsion Shaft for Wireless Sensor System Applications (무선센서 시스템 응용을 위한 선박 추진 축계용 에너지 하베스터)

  • Van Ai Hoang;Young Chul Lee
    • Journal of Advanced Navigation Technology
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    • v.27 no.1
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    • pp.96-101
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    • 2023
  • In this work, an energy harvester (EH) on the rotating shaft has been proposed for a wireless sensor system (WSS) applications. The EH was designed and implemented to the shaft with a diameter of 20 cm to continuously power a wireless sensor system (WSS). The rotor has coils wound in pairs on seven U-shaped cores attached to the shaft. The stator consists of eight pairs of magnets attached to eight I-cores and they are fixed to an outer fixture. The generated power of the EH was investigated as function of the air gap between the rotor and stator, the number of turn of coils, and shaft speed. The fabricated EH produced power up to 2.87 W at 300 rpm and the 3 mm air gap.

Effects of Maturing Stage of Corn Hybrids on Silage Yield, Feeding Value for Dairy Cows and Milk Production in a Cold Region of Japan

  • Oshita, Tomoko;Takayama, Hideki;Otsuka, Hiroshi;Igarashi, Hiroaki;Nonaka, Kazuhisa;Kume, Shinichi
    • Asian-Australasian Journal of Animal Sciences
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    • v.20 no.4
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    • pp.511-516
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    • 2007
  • This experiment was conducted to evaluate the effects of differently maturing corn hybrids on silage production and milk production per unit area in the northern part of Japan, where grain development occurs under decreasing ambient temperature. Both hybrids were harvested at the same time. The stages of maturity for the early-maturing hybrids (EH; 80 d relative maturity) and the mid-maturing hybrids (MH; 93 d relative day) were early dent and late dough stage, respectively. The plant yields for MH were higher than those for EH. The dry matter (DM) content of MH was lower than that for EH, and the effluent loss for MH silage was greater than that for EH silage. Therefore, the DM yields of prepared silage per area were similar for both treatments. Twelve multiparous mid-lactation Holstein cows ($58{\pm}13$ days in milk) were fed diets based on EH or MH silage in a crossover design with two 3-week periods. Cows were fed 3 kg of hay crop silage (DM basis) and either EH or MH silage ad libitum, and concentrates were supplied to meet NRC requirement for dairy cows. Silage DM intake for EH was found to be higher (p<0.05) than that for MH (10.0 vs. 9.1 kg/day). Milk production and milk composition for EH were similar to those for MH. Feed efficiency per total feed intake was similar in both treatments, although the feed efficiency per concentrate intake tended to be higher for the EH than that for the MH diet. These results indicate that differences in maturation in corn hybrids affect the effluent production of silage and the silage intake of dairy cows. It may be advantageous to plant early hybrid corn with a reduction in effluent production of silage as well as a reduction in purchased feed costs for dairy cows under the climatic conditions of the northern part of Japan.

Anti-inflammatory effect of Equisetum hyemale via suppression of nuclear factor-κB activation in human mast cells

  • Jeon, So-Ra;Na, Ho-Jeong;Jeon, Hoon
    • Advances in Traditional Medicine
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    • v.9 no.2
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    • pp.149-156
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    • 2009
  • Equisetum hyemale Linne. (EH) (Equisetaceae) has been used for the treatment of eye and skin disease, chronic eczema, pneumoconiosis and asthma in Korea and China. Human leukemic mast cells are widely distributed in the connective tissues of mammals and other vertebrates. Phorbol 12-myristrate 13-acetate (PMA) and calcium ionophore A23187 stimulated Human leukaemic mast cell line-1 (HMC-1) can produce a variety of inflammatory mediators and several pro-inflammatory and chemotactic cytokines such as TNF-$\alpha$, IL-6 and IL-8. Since TNF-$\alpha$, IL-6 and IL-8 are major factors during the inflammatory process, we studied the effects of EH on TNF-$\alpha$, IL-6 and IL-8 release in HMC-1 stimulated with PMA and A23187. The result of this study indicate that EH inhibits TNF-$\alpha$, IL-6 and IL-8 in activated HMC-1 cells via $I{\kappa}B$/Nuclear factor-${\kappa}B$ pathway. Therefore, EH might contribute significantly to the prevention or treatment of mast-cell mediated inflammatory diseases and EH has potential use in the therapy of chronic allergic inflammation.

Induction of Microsomal Epoxide Hydrolase, rGSTA2, rGSTA3/5, and rGSTM1 by Disulfiram, but not by Diethyldithiocarbamate, a Reduced Form of Disulfiram

  • Kim, Sang-Geon;Kim, Hye-Jung
    • Toxicological Research
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    • v.13 no.4
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    • pp.339-347
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    • 1997
  • Disulfiram (DSF) and diethyldithiocarbamate (DDC), a reduced form of DSF, protect the liver against toxicant-induced injury through inhibition of cytochrome P450 2E1. The effect of DSF and DDC on the levels of major hepatic microsomal epoxide hydrolase (mEH) and glutathione S-transferase (GST) expression was comparatively studied, given the view that these enzymes are involved in terminal detoxification events for high energy intermediates of xenobiotics. Treatment of rats with a single dose of DSF (20-200 mg/kg, po) resulted in 2- to 15-fold increases in the mEH mRNA level at 24 hr with the ED$_{50}$ value being noted as 60 mg/kg. The mEH mRNA level was elevated ~15-fold at 24 hr after treatment at the dose of 100 mg/kg, whereas the hepatic mRNA level was rather decreased from the maximum at the dose of 200 mg/kg, indicating that DSF might cause cytotoxicity at the dose. In contrast to the effect of DSF, DDC only minimally elevated the mEH mRNA level at the doses employed. DSF moderately increased the major GST mRNA levels in the liver as a function of dose, resulting in rGSTA2, rGSTA3/5 or rGSTM1 mRNA levels being elevated 3- to 4-fold at 24 hr post-treatment, whereas the rGSTM2 mRNA level was not altered. DDC, however, failed to stimulate the mRNA levels for major GST subunits, indicating that the reduced form of DSF was ineffective in stimulating the GST the expression. The effect of other organosulfides including aldrithiol, 2, 2'-dithiobis(benzothiazole) (DTB), tetramethylthiouram disulfide (TMTD) and allyl disulfide (ADS) on the hepatic mEH and GST mRNA expression was assessed in rats in order to further confirm the increase in the gene expression by other disulfides. Treatment of rats with aldrithiol (100 mg/kg, po) resulted in a 16-fold increase in the mEH mRNA level at 24 hr post-treatment. DTB, TMTD and ADS also caused 5-, 9- and 12-fold increases in the rnRNA level, respectively, as compared to control. Thus, all of the disulfides examined were active in stimulating the mEH gene in the liver. The organosulfides significantly increased the rGSTA2, rGSTA3, rGSTA5 and rGSTM1 mRNA levels at 24 hr after administration. In particular, aldrithiol was very efficient in stimulating the rGSTA and rGSTM genes among the disulfides examined. These results provide evidence that DSF and other sulfides effectively stimulate the mEH and major GST gene expression at early times in the liver and that DDC, a reduced form of DSF, was ineffective in stimulating the expression of the genes, supporting the conclusion that reduced form(s) of organosulfur compound(s) might be less effective in inducing the mEH and GST genes through the antioxidant responsive element(s).

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Effects of the Herbal-acupuncture with Epimedii Herba Extract on Osteoporosis in Ovariectomized ddY Mice (음양곽(淫羊藿) 약함(藥緘)이 난소적출 흰쥐의 골다공증에 미치는 영향)

  • Kang, Min-Wan;Hong, Kwon-Eui;Kim, Young-Il
    • Journal of Acupuncture Research
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    • v.26 no.2
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    • pp.1-14
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    • 2009
  • Objectives & Methods : The purpose of this study is to observe the effects of herbal-acupuncture with Epimedii Herba extract (EH-HA) at $KI_{10}$ (Eumgok) on osteoporosis in ovariectomized (OVX) ddY mice. We carried out several experimental items to analyze the changes in body weight, uterine weight, uterus index, tibial length, the ash bone weight, tibial BMD, serum ALP, serum osteocalcin, serum Ca, and the levels of Ca, P, Ca/P ratio in tibia, and we performed histological and histomorphological analysis as well. Results: 1. The tibial length and ash bone weight were insignificant, while BMD was significantly increased by in EH-HA in comparison with control group. 2. Serum ALP and serum osteocalcin were decreased and serum Ca was increased by in EH-HA in comparison with control group, But all were insignificant. 3. Ca and P level in tibia were significantly increased in EH-HA in comparison with control group, while Ca/P ratio was insignificant. 4. Osteoclast like cell in tibia was significantly decreased in EH-HA in comparison with control group. 5. In the histological study in tibia, TBV was significantly increased, TBT was insignificantly increased and GPL was significantly decreased in EH-HA in comparison with control group. Conclusions: These results suggest that EH-HA at $KI_{10}$ has a therapeutic effect on osteoporosis in OVX mice.

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