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Pharmacokinetics of a New Antigastritic Agent, Eupatilin, an Active Component of StillenE®, in Rats

  • Jang, Ji-Myun;Park, Kyung-Jin;Kim, Dong-Goo;Shim, Hyun-Joo;Ahn, Byung-Ok;Kim, Soon-Hoe;Kim, Won-Bae
    • Biomolecules & Therapeutics
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    • v.11 no.3
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    • pp.163-168
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    • 2003
  • Pharmacokinetics of eupatilin (an active components of $Stillen^{\circledR}$, a new antigastritic agent) were investigated after both intravenous and oral administration at a dose of 30mg/kg to rats. After intravenous administration, the plasma concentrations of unchanged eupatilin declined rapidly with a mean terminal half-life of 0.101 h. Eupatilin was eliminated fast in rats; the total body clearance was 121 mL/min/kg. Eupatilin was mainly metabolized in rats; the percentage of intravenous dose of eupatilin excreted in 24 h urine and feces as unchanged eupatilin was only 2.5 and 0.919%, respectively. Eupatilin was mainly metabolized to form its glucuronide conjugate; after intravenous administration, 15.9 and 51.7% of intravenous dose was excreted in 24 h urine and feces, respectively, as eupatilin plus its glucuronide. After oral administration, the absolute bioavailability was only 3.86% based on $AUC_{0-24h}$ of eupatilin plus its glucuronide. Approximately 68.5% of oral dose was not absorbed from the entire gastrointestinal tract. Therefore, it could be concluded that the superior effect of eupatilin in experimental animal models of gastric ulcer and inflammatory bowel disease after oral administration could be due to the local action of eupatilin. Further pharmacokinetic studies to elucidate the local action of eupatilin are required.

Anti-Obesity Effects of Water Extracts from Different Organs of Cirsium japonicum var. ussuriense (엉겅퀴 부위별 열수 추출물의 항비만 효과)

  • Yin, Hong Hua;Cho, Byoung Ok;Fang, Chong Zhou;Shim, Jae-Suk;Jang, Seon Il
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.29 no.4
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    • pp.322-329
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    • 2015
  • Cirsium japonicum var. ussuriense are often used in treatment of human diseases such as hemorrhage, blood congestion and inflammation in Korea. However, there was not report on the anti-obesity efficacy of water extracts from different organs of C. japonicum var. ussuriense. Here, we investigated the antioxidant effects of water extracts of flowers, leaves and roots from C. japonicum var. ussuriense. Total polyphenol amounts of the flower extract showed higher than those of leaf and root extract. Flower extract also showed the high antioxidant activities such as DPPH radical scavenging activity and reducing power. We also investigated the anti-obesity effects of water extracts of flowers, leaves and roots from C. japonicum var. ussuriense in 3T3-L1 cells and high fat diet-induced obesity mice. The mice were divided into four groups [high fat diet (HFD) control, HFD + leaf extract, HFD + flower extract and root extract] and administered with each extract (200 mg/kg) for 12 weeks. The flower and leaf extract significantly suppressed the levels of oil red O and triglyceride content. The flower and leaf extract also significantly reduced the triglyceride, total cholesterol and lower density lipoprotein levels of plasma as well as body and abdominal fat weight. Furthermore, oral glucose tolerance in the flower and leaf extract groups were significantly ameliorated in comparison to the high fat diet group. Therefore, these results indicate that the flower and leaf extract could ameliorate obesity and attenuate blood glucose level in high fat diet-induced obesity mice. We conclude that this study may provide positive insights into water extracts of flowers and leaves from C. japonicum var. ussuriense as a functional food ingredient for treatment of obesity.

Physicochemical Characteristics of Salted Jellyfish Processed in Southeast Asia (동남아시아산 염장해파리의 이화학적 성분 특성 비교)

  • Choi, Ji Il;Shim, Kil Bo;Yoon, Na Young;Kim, Min A;Park, Jae Sung;Lim, Chi Won
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.47 no.5
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    • pp.482-488
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    • 2014
  • The study investigated the chemical composition, pH, and texture of salted jellyfish processed in Indonesia, Thailand, and China as a pilot study for processing the jellyfish Nemopilema nomurai, which occurs in Korean coastal waters. The 14 samples of salted jellyfish included processed umbrella and oral arms and consisted of 68.4-78.3 g/100 g moisture, 1.79-4.37 g/100 g crude protein, and 0.07-0.41 g/100 g crude lipid. The total amino acid content was 2.30-4.69 g/100 g and glycine accounted for 20.07-37.37% of the total amino acids. Salting jellyfish reduces the possibility of microbial growth and enhances the shelf life because the samples have a pH of 3.77-4.35, salinity of 18.53-24.02%, and lower water activity of 0.77-0.80. The lightness (L), redness (a), and yellowness (b) of the samples were 53.98-61.32, 1.76-6.26, and 14.08-29.0, respectively. The springiness, strength, and hardness of the salted jellyfish differed significantly among the products. The sample processed in Indonesia had the highest springiness. While the chemical composition, pH, water activity, and color differed significantly among the products, there were no significant effects of the country of manufacture. These results will enable the determination of quality index parameters for salted processed Nemopilema nomurai caught in Korean coastal.

Characterization of an O-Methyltransferase from Streptomyces avermitilis MA-4680

  • Yoon, Young-Dae;Park, Young-Hee;Yi, Yong-Sub;Lee, Young-Shim;Jo, Geun-Hyeong;Park, Jun-Cheol;Ahn, Joong-Hoon;Lim, Yoong-Ho
    • Journal of Microbiology and Biotechnology
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    • v.20 no.9
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    • pp.1359-1366
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    • 2010
  • A search of the Streptomyces avermitilis genome reveals that its closest homologs are several O-methyltransferases. Among them, one gene (viz., saomt5) was cloned into the pET-15b expression vector by polymerase chain reaction using sequence-specific oligonucleotide primers. Biochemical characterization with the recombinant protein showed that SaOMT5 was S-adenosyl-L-methionine-dependent Omethyltransferase. Several compounds were tested as substrates of SaOMT5. As a result, SaOMT5 catalyzed O-methylation of flavonoids such as 6,7-dihydroxyflavone, 2',3'-dihydroxyflavone, 3',4'-dihydroxyflavone, quercetin, and 7,8-dihydroxyflavone, and phenolic compounds such as caffeic acid and caffeoyl Co-A. These reaction products were analyzed by TLC, HPLC, LC/MS, and NMR spectroscopy. In addition, SaOMT5 could convert phenolic compounds containing ortho-dihydroxy groups into O-methylated compounds, and 6,7-dihydroxyflavone was known to be the best substrate. SaOMT5 converted 6,7-dihydroxyflavone into 6-hydroxy-7-methoxyflavone and 7-hydroxy-6-methoxyflavone, and caffeic acid into ferulic acid and isoferulic acid, respectively. Moreover, SaOMT5 turned out to be a $Mg^{2+}$-dependent OMT, and the effect of $Mg^{2+}$ ion on its activity was five times greater than those of $Ca^{2+}$, $Fe^{2+}$, and $Cu^{2+}$ ions, EDTA, and metal-free medium.

Caffeine Induces High Expression of cyp-35A Family Genes and Inhibits the Early Larval Development in Caenorhabditis elegans

  • Min, Hyemin;Kawasaki, Ichiro;Gong, Joomi;Shim, Yhong-Hee
    • Molecules and Cells
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    • v.38 no.3
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    • pp.236-242
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    • 2015
  • Intake of caffeine during pregnancy can cause retardation of fetal development. Although the significant influence of caffeine on animal development is widely recognized, much remains unknown about its mode of action because of its pleiotropic effects on living organisms. In the present study, by using Caenorhabditis elegans as a model organism, the effects of caffeine on development were examined. Brood size, embryonic lethality, and percent larval development were investigated, and caffeine was found to inhibit the development of C. elegans at most of the stages in a dosage-dependent fashion. Upon treatment with 30 mM caffeine, the majority ($86.1{\pm}3.4%$) of the L1 larvae were irreversibly arrested without further development. In contrast, many of the late-stage larvae survived and grew to adults when exposed to the same 30 mM caffeine. These results suggest that early-stage larvae are more susceptible to caffeine than later-stage larvae. To understand the metabolic responses to caffeine treatment, the levels of expression of cytochrome P450 (cyp) genes were examined with or without caffeine treatment using comparative microarray, and it was found that the expression of 24 cyp genes was increased by more than 2-fold (p < 0.05). Among them, induction of the cyp-35A gene family was the most prominent. Interestingly, depletion of the cyp-35A family genes one-by-one or in combination through RNA interference resulted in partial rescue from early larval developmental arrest caused by caffeine treatment, suggesting that the high-level induction of cyp-35A family genes can be fatal to the development of early-stage larvae.

Sclerotium Rot of Onion Caused by Sclerotium rolfsii (Sclerotium rolfsii에 의한 양파 흰비단병)

  • Kwon, Jin-Hyeuk;Kim, Hee-Dae;Choi, Ok-Hee;Kwak, Youn-Sig;Lee, Yong-Hwan;Shim, Hong-Sik
    • Research in Plant Disease
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    • v.17 no.2
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    • pp.222-224
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    • 2011
  • The sclerotium rot of onion (Allium cepa L.) was occurred sporadically in the farmer's fields at Daehap, Changnyeong in Korea. The typical symptom was water-soaking on the bulb, stem and leaves and then rotting, wilting, blighting and the infected plants eventually were rotted and died. The sclerotia were globoid, 1-3 mm, and white to brown. The optimum temperature for mycelial growth and sclerotial formation on PDA was $30^{\circ}C$. The hyphal width was 4-9 ${\mu}m$. The typical clamp connections were observed in the hyphae of the fungus grown on PDA. On the basis of mycological characteristics, ITS rDNA sequence analysis, and pathogenicity, this fungus was identified as Sclerotium rolfsii Saccardo. To our knowledges, this is the first report of sclerotium rot on onion caused by S. rolfsii in Korea.

Kinetic Analysis about the Bidirectional Transport of 1-Anilino-8-naphthalene Sulfonate (ANS) by Isolated Rat Hepatocytes

  • Lee, Pung-Sok;Song, Im-Sook;Shin, Tae-Ha;Chung, Suk-Jae;Shim, Chang-Koo;Song, Sukgil;Chung, Youn-Bok
    • Archives of Pharmacal Research
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    • v.26 no.4
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    • pp.338-343
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    • 2003
  • The purpose of the present study was to investigate the bidirectional transport of 1-anilino-8-naphthalene sulfonate (ANS) using isolated rat hepatocytes. The initial uptake rate of ANS by isolated hepatocytes was determined. The uptake process of ANS was saturable, with a $K_m of 29.1\pm3.2 \mu M and V_{max} of 2.9\pm0.1$ mmol/min/mg protein. Subsequently, the initial efflux rate of ANS from isolated hepatocytes was determined by resuspending preloaded cells to 3.0% (w/v) BSA buffer. The efflux process for total ANS revealed a little saturability. The mean value of the efflux clearance was $2.2\pm0.1 \mu$ L/min/mg protein. The efflux rate of ANS from hepatocytes was markedly decreased at $4^{\circ}C$, indicating that the apparent efflux of ANS might not be attributed to the release of ANS bound to the cell surface, but to the efflux of ANS from intracellular space. The efflux clearance was furthermore corrected for the unbound intracellular ANS concentration on the basis of its binding parameters to cytosol. The relation between efflux rate and unbound ANS concentration was fitted well to the Michaelis-Menten equation with a saturable and a nonsaturable components. The $V_{max} and K_m$ values were 0.54 mmol/min/mg protein, and 10.0 $\mu$ M, respectively. Based on the comparison of the ratios of $V_{max} to K_m (V_{max}/K_m)$ corresponding to the transport clearance, the influx clearance was two times higher than the efflux clearance. Together with our preliminary studies that ATP suppression in hepatocytes substantially inhibited ANS influx rate, we concluded that the hepatic uptake of ANS is actively taken up into hepatocytes via the carrier mediated transport system.

Chemical Characteristics and Flavors of Bamboo-shoot Vinegar (죽순식초의 화학적 특성 및 향기분석)

  • Jang, Hyejin;Lee, Eunsil;Shim, You-Shin;Seo, Dongwon;Hwang, Jinbong;Lee, Songjin;Ha, Jaeho
    • Korean Journal of Food Science and Technology
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    • v.45 no.6
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    • pp.675-681
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    • 2013
  • We assessed the quality of a bamboo shoot vinegar produced in Damyang-gun in terms of parameters that included acidity, mineral contents, amino acids, and flavonol aglycones. The flavor compounds of the bamboo shoot vinegar were also analyzed using the stir bar sorptive extraction (SBSE) method. The acidity of the bamboo shoot vinegar was 4.49%, which was the lowest value among the commercial vinegars studied. The bamboo shoot vinegar had a lower concentration of Na (8.36 mg/100 g) than the other commercial vinegars. There was a relatively large amount of tyrosine and lysine in the bamboo shoot vinegar. The concentration of quercetin, a flavonol aglycone, was 3.29 mg/100 g. The results of the flavor analysis showed that hexanal, 2-furancarboxaldehyde, and benzaldehyde were high in the bamboo shoot vinegar. Oleamide, a compound that is known to induce sleep, was first found in bamboo shoot vinegar using the SBSE method.

Symptoms and Damages of Powdery Mildew on Leafy Lettuce Caused by Podosphaera fusca (Podosphaera fusca에 의한 상추 흰가루병의 증상과 피해)

  • Jee, Hyeong-Jin;Shim, Chang-Ki;Ryu, Kyung-Yul;Shin, Hyeon-Dong
    • Research in Plant Disease
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    • v.12 no.3
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    • pp.294-297
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    • 2006
  • Leafy lettuce(Lactuca sativa L.) is one of the most important vegetable crops in Korea, cultivated throughout the year in greenhouses. During the autumn of 2005, powdery mildew of lettuce that is a new disease caused by Podosphaera fusca occurred in several plantings grown in plastic houses near Suwon in central Korea. Further survey on commercial fields of the plant in central and southern Korea revealed its widespread occurrence and severe losses. Infections occur on upper part of mature leaves often cause leaf distortions, withering, and reduced vigor and growth. Among 184 greenhouses surveyed 121 were infested by the disease and 52 showed over 10% infection rate. Yields were greatly reduced by the disease reaching only 59% compared to healthy plants. About 60% leaves of infected plant were not marketable and fresh weight of the leaves was 73.6% compared to healthy leaves. Total yield of the greenhouses infested by the disease ranged from $100{\sim}140kg$, while it was 260 kg in a non-infested greenhouse at one time harvest. Since the disease represents a threat to safe cultivation of leafy lettuce in Korea, environmentally-friend control strategies should be urgently developed.

Efficient Authentication of Aggregation Queries for Outsourced Databases (아웃소싱 데이터베이스에서 집계 질의를 위한 효율적인 인증 기법)

  • Shin, Jongmin;Shim, Kyuseok
    • Journal of KIISE
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    • v.44 no.7
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    • pp.703-709
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    • 2017
  • Outsourcing databases is to offload storage and computationally intensive tasks to the third party server. Therefore, data owners can manage big data, and handle queries from clients, without building a costly infrastructure. However, because of the insecurity of network systems, the third-party server may be untrusted, thus the query results from the server may be tampered with. This problem has motivated significant research efforts on authenticating various queries such as range query, kNN query, function query, etc. Although aggregation queries play a key role in analyzing big data, authenticating aggregation queries has not been extensively studied, and the previous works are not efficient for data with high dimension or a large number of distinct values. In this paper, we propose the AMR-tree that is a data structure, applied to authenticate aggregation queries. We also propose an efficient proof construction method and a verification method with the AMR-tree. Furthermore, we validate the performance of the proposed algorithm by conducting various experiments through changing parameters such as the number of distinct values, the number of records, and the dimension of data.