• Title/Summary/Keyword: Asa1

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Synthesis and Properties of 5-Aminosalicyl-L-Aspartic Acid and 5-Aminosalicyl-L-glutamic Acid as Colon-Specific Prodrugs of 5-Aminosalicylic Acid (5-아미노살리실산의 결장표적성 프로드럭 : 5-아미노살리실-L-글루타민산과 5-아미노살리실-L-아스파틸산의 합성 및 성상)

  • Jung, Yun-Jin;Lee, Jeoung-Soo;Kim, Hak-Hyun;Kim, Young-Mi;Kim, Dae-Duk;Han, Suk-Kyu
    • YAKHAK HOEJI
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    • v.42 no.1
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    • pp.5-11
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    • 1998
  • 5-Aminosalicyl-L-aspartic acid (5-ASA-Asp) and 5-aminosalicyl-L-glutamic acid (5-ASA-Glu) were synthesized as new colon-specific prodrugs of 5-aminosalicylic acid (5-ASA), their apparent partition coefficients, and the extent of conversion in the homogenates of tissue and contents of various G.I. Tract segments of rats were evaluated. These prodrugs were stable in the homogenate of tissue and contents of stomach, proximal small intestine (PSI) or distal small intestine (DSI). Release of 5-ASA from 5-ASA-Asp after incubation with the cecal and colonic contents for 8hrs at $37^{\circ}C$ was 18%, and 8%, respectively. No significant conversion of prodrug was observed in the cecal and colonic contents of rats pretreated with kanamycin sulfate, which indicated that microbial enzymes were responsible for the cleavage of these prodrugs.

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Optimization of Modified Starches on Retrogradation of Korean Rice Cake(Garaeduk) (가래떡의 노화 억제에 관한 변형 전분의 최적화)

  • Park, Hyun-Jeong;Song, Jae-Chul;Shin, Wan-Chul
    • The Korean Journal of Food And Nutrition
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    • v.19 no.3
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    • pp.279-287
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    • 2006
  • This study was carried out to investigate the influences of modified starches on suppression of retrogradation in Korean rice cake for their optimization, Garaeduk. Based upon studying Avrami equation, the Avrami exponent n value of all the experiment samples was found to be 1.03 ${\sim}$ 1.37 in the influence of modified starches on retrogradation of the rice cake. This means that the retrogradation of the Korean rice cake occurred instantly after the crystallization of starch particles in the Korean rice cake formulated by modified starches. The highest Avrami exponent n value was indicated in the control sample. The rate constant k of retrogradation in the Korean rice cake formulated by modified starches showed comparatively low and appeared to be the lowest in the Korean rice cake formulated by SHPP. This tendency was shown well in the time constant(1/k) of retrogradation velocity. According to the DSC analysis, the onset temperature of gelatinization in thermal characteristics showed somewhat high in case of addition of modified starch into the Korean rice cake on storage time and the SHPP was slowly gone up. In peak temperature of gelatinization in thermal characteristics of the DSC analysis, SSOS and ASA were increased a little in comparison with the control. The control was comparatively high increase. Melting enthalphy of all samples added with modified starches (SSOS: 21.1${\rightarrow}$23.7${\rightarrow}$24.1, ASA: 21.1${\rightarrow}$24.8${\rightarrow}$25.4) appeared to be lower than that of the Korean rice cake without modified starches(21.2${\rightarrow}$26.1${\rightarrow}$27.1). The Korean rice cake added with SHPP was shown to be the lowest in the increasing rate of melting enthalpy(20.9${\rightarrow}$21.4${\rightarrow}$22.1). Heat spreadability of all the samples in Martin melting diameter was revealed to be good in order of control, ASA, SSOS, SHPP and especially the Korean rice cake added with SHPP was shown to be the best in heat spreadability. In color, sensory examination and textural characteristic of the Korean rice cake added with modified starches, the L$^*$value was not changed practically with the storage time and seemed to be stable. The a$^*$ value of the samples was followed by control(2.21${\rightarrow}$5.34: 141.6%), ASA (2.01${\rightarrow}$4.22: 110.0%), SSOS (2.78${\rightarrow}$4.87: 75.2%) and SHPP (2.12${\rightarrow}$3.40: 60.4%) in order of color change. Also the b$^*$ value of the samples was followed by control(4.32${\rightarrow}$6.35: 47.0%), ASA (4.66${\rightarrow}$5.73: 23.0%), SSOS (4.90${\rightarrow}$5.89: 20.2%) and SHPP (4.89${\rightarrow}$5.12: 4.7%) and there was the least (or no) color change with the SHPP. Textural characteristics of samples was shown to be the highest in case of modified starch addition and especially SHPP appeared to be the best in texture.

기니픽과 토끼에서 PDT-Hepa의 항원성 시험

  • 강경선;이영순
    • Environmental Mutagens and Carcinogens
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    • v.11 no.2
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    • pp.141-147
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    • 1991
  • 기니픽과 New Zealand White Rabbit에서 PDT-Hepa에 대한 항원성 시험을 실시하였다. 1) Active Systemic Anaphylaxis (ASA), 2) Passive Systemic Anaphylaxis (PSA), 3) Passive Custaneous Anaphylaxis (PCA) 시험을 실시한 결과 ASA, PSA 실험에서 anaphylaxis와 관련된 어떠한 특이적인 임상증상도 나타나지 않아 PDT-Hepa는 기니픽과 토끼에서 항원성이 없는 것으로 보인다. 또한 PCA 실험에서 청색반점이 관찰되지 않은 것으로 보아 PDT-Hepa specific IgE는 생성되지 않는 것으로 판단된다.

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Antigenicity test of cis-Malonato[(4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane]platinum(II)(SKI 2053R) in Guinea Pigs and Mice (기니픽 및 마우스에서 cis-Malonato[(4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane]platinum(II)(SKI 2053R)의 항원성시험)

  • Lee, Yong-Soon;Kang, Kyung-Sun;Shin, Dong-Jin;Kim, Hyoung-Ook;Cho, Jae-Jin;Kim, Bae-Hwan;Nam, Ki-Hoan;Seo, Kwang-Won
    • Toxicological Research
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    • v.8 no.2
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    • pp.255-263
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    • 1992
  • SKI 2053R and SKI 2053R-human serum albumin(HSA) mixture were examined for their antigenicity in Hartley guinea pigs as well as C57BL/6 mice in comparison with distilled water (DW), HSA and DW-HSA conjugate. Several antigenicity tests, including acitive systemic anaphylaxis(ASA), passive systemic anaphylaxis (PSA), passive cutaneous anaphylaxis (PCA) and indirect hamagglutination test (IHA), were performed according to the Established Regulations of National Institute of Safety Research. The results were as follows: 1. When guinea pigs were sensitized with SKI2053R or SKI2053R-HSA emulsified with complete Freund's adjuvant(CFA), these animals showed negative reactions in ASA and PSA. 2.No blue spot was observed on the back skin of guinea pigs in the PCA test. 3. Sera from guinea pigs revealed a negative reaction in IHA. 4.Guinea pigs were sensitized by HSA emulsified with CFA as a positive control, and these animals showed positive reactions in ASA, PSA, PCA, and IHA. As shown above, SKI2053R was considered to possess neither antigenic, nor haptenic properties, and confirmed not to have the haemagglutinating activity.

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Phenolic and Furan Type Compounds Isolated from Gastrodia elata and their Anti-Platelet Effects

  • Pyo Mi Kyung;Jin Jing Ling;Koo Yean Kyoung;Yun-Choi Hye Sook
    • Archives of Pharmacal Research
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    • v.27 no.4
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    • pp.381-385
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    • 2004
  • Nine phenolic ($1\~9$) and two furan type (10, 11) compounds, were isolated from the methanolic extract of the tuber of Gastrodia elata Blume (Orchidaceae) in the course of continuing search for platelet anit-aggregating plant components. Compound 1 was identified as 4,4'-dihy-droxybenzyl sulfone, a novel compound for the best of our knowledge. Compound 10, 5-hydroxymethyl-2-furancarboxaldehyde, was isolated for the first time from this plant. Compound 1 ($IC_{50};\;83{\mu}M$) was about four times more inhibitory to U46619 induced aggregation than ASA ($IC_{50};\340{\mu}M$). Compound 9, 4,4'-dihydroxy-dibenzylether, ($IC_{50};\;5{\mu}M$, $3{\mu}M\;and\;33{\mu}M$, respectively) was $10\~}80$ fold more potent than ASA ($IC_{50};\;420\;{\mu}M,\;53\;{\mu}M\;and\;340\;{\mu}M$ respectively) to collagen, epinephrine and U46619 induced aggregation, although it is less active than ASA to AA induced aggregation.

Acute Toxicity and Antigenicity of Guamerin (Guamerin의 단회투여독성 및 항원성 평가)

  • 조명행;김민영;손장원;배미옥;김정현;신민기;방명주;김경연;최승진
    • Toxicological Research
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    • v.16 no.1
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    • pp.83-87
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    • 2000
  • This study was carriet out to evaluate the acute intravenous toxicity and antigenicity of Guamerin, newly developed by Mogam Biotechnology Research Institute (MBRI). In acute intravenous toxicity test, ICR mice were administered intravenously with single dose of 1,000mg/kg, and body weights and clinical signs were observed for 14 days. No dead animal, clinical signs, body weight change and abnormal autopsy findings were found in control and Gumerin treated group. Therefore, the 50% lethoal dose (LD50) of Guamerin for ICR mice was more than 1,000mg/kg on intravenous route for male and female. And the antigenic potential of Guamerin was examined by active systemic anaphylaxis(ASA) and passive cutaneous anaphylaxis(PCA) tests. In the ASA test, low and high doses (10 and 100ug/animal, respectiwely) of Guamerin were administed subcutaneously to guinea pigs for 9 times 3 weeks. All experimental groups showed negative responses whereas the positive control group given ovalbumin plus Freunds complete adjuvant (FCA) showed severe anaphylactic responses. PCA test using rats with mice anti-serum against Guamerin, low and high doses(10 and 100 ug/animal, respectively) of Guamerin were administered to mice for 9 times in 3 weeks. The anti-serum against Guamerin was administed intradermally at the back of rats, however, any positive responses were not detected in the experimental groups. These results strongly indicate that Guamerin does not induce IgE production and is not a PCA reaction inducer under these experimental conditions.

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Antigenicity Study of CFA-001, cefazolin, a cephalosperin Derivative Produced by an :Enzymatic Semisynthesis

  • Park, Jong-Il;Jeong, Tae-Cheon;Kim, Hyoung-Chin;Han, Sang-Seop;Roh, Jung-Koo;Kim, Jeong-Hwan;Jeon, Yeong-Joong;Kim, Dal-Hyun;Kim, Je-Hak;Park, Kwan-Ha
    • Biomolecules & Therapeutics
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    • v.5 no.1
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    • pp.48-52
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    • 1997
  • The antigenic potential of CFA-001, cefazolin, a cephalosporin derivative produced by an enzy-matic semisynthesis, was determined in Hartley guinea pigs. A battery of tests employed consisted of active systemic anaphylaxis (ASA), passive cutaneous anaphylaxis (PCA), and indirect hemagglutination test (IHA). The results were as follows: 1) In ASA, no signs attributable to anaphylaxis was observed in guinea pigs sensitized with CFA-001, whereas OVA-sensitized animals induced severe anaphylactic symptoms; 2) guinea pigs did not produce antibodies against CFA-001 when sensitized with or without Freund's complete adjuvant (FCA) in homologous PCA tests. Meanwhile, antibodies against ovalbumin (OVA) were clearly detected; 3) No CFA-001-specific hemagglutination was observed in the IHA using sera obtained from CFA-001- sensitized guinea pigs. These results suggest that CFA-001 has no antigenicity potential in guinea pigs.

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A Study on Antigenicity of Recombinant Human Interferon $\beta$ (LB00013) in Mice and Guinea Pigs

  • Park, Jong-Il;Jeong, Tae-Cheon;Cha, Shin-Woo;Shin, Ho-Chul;Han, Sang-Seop
    • Toxicological Research
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    • v.12 no.1
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    • pp.81-86
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    • 1996
  • Antigenicity of recombinant human interferon $\beta$(LB00013), a newly developed drug for anti-cancer and anti-viral therapeutic use, was investigated in mice and guinea pigs. The following results were obtained: 1. Mice showed no production of antibodies against LB00013 sensitized with aluminum hydroxide gel (Alum) as an adjuvant, when judged by the heterologous passive cutaneous anaphylaxis (PCA) test in rats. Meanwhile, antibodies against ovalbumin (OVA) sensitized with Alum were clearly detected. 2. In guinea pigs, the sensitization of neither LB00013 only nor LB00013 with complete Freund's adjuvant (CFA) produced positive reactions in the homologous active systemic anaphylaxis (ASA) and the PCA tests. Meanwhile, the sensitization of OVA with CFA produced positive reactions in both PCA and ASA. 3. A LB00013-specific reaction was not observed in an indirect hemagglutination(IHA) assay using sera isolated from LB00013 sensitized mice. The present results suggested that LB00013 may have no antigenic potential in mice and guinea pigs.

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Study on the Detection of Anti-Sperm Antibodies in Zygote Intra Fallopian Transfer (ZIFT) Patients with Fertilization Failure or Low Fertilization Rate and Retreatment of Oocyte and Sperm (접합자 난관내 이식 환자에 있어서 수정 실패와 항정자 항체와의 관계 및 난자와 정자의 재처리에 관한 연구)

  • Chung, M.K.;Ko, J.J.;Do, B.R.;Koo, J.J.;Han, S.Y.;Cha, K.Y.
    • Clinical and Experimental Reproductive Medicine
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    • v.19 no.2
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    • pp.169-174
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    • 1992
  • Previous studies have indicated that immunological factor is responsible for the infertility. We have detected sperm antibodies in ZIFT patients which grouped as fertilization failure (A; n=18) and low fertilization rate (${\leq}50%$)(B; n=20). Patients, however, had normal oocytes and sperms. We collected serum from wives and semen from husbands and donors (fertile sperm), if it was needed. We examined class, binding patterns and amounts of antisperm antibodies(ASA) by direct and indirect immunobead binding assay. In group A, 11 husbands were ASA positive showing 62.2% and 61.1% binding with IgA and IgG, respectively, and two wives were ASA positive showing 70.0% and 71.0% binding with IgA and IgG, respectively. Binding sites were mainly at the head of sperms (84%). In group B, 8 husbands were ASA positive showing 37.5% and 40.0% binding with IgA and IgG, respectively, and two wives were ASA positive showing 41.3% and 42.0% binding with IgA and IgG, respectively. Binding sites were also mainly at the head of sperms (78%). For the treatment of ZIFT patients who had fertilization failure at the first trial, we used albumin fractionation method and dilution method with 30% fetal cord serum (FCS) to reduce the titer of ASA. We used partial zona dissection (P.Z.D.) method for wives who have antisperm antibodies in their serum. According to represented method, we could inhance the fertilization rate to 60.0% by albumin fractionation and 20.0% by P.Z.D., respectively. We concluded that the use of micromanipulation like P.Z.D. or the other sperm processing methods is required to increase a chance of fertilization. This result suggested that it should be a prerequisite to test antisperm antibodies prior to entering assisted reproductive technologies (ART) programs.

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Decomposition of Acetylsalicylic Acid by Gamma Ray (감마선 조사에 의한 Acetylsalicylic Acid의 분해)

  • Ahn, Young Deok;Lee, Kyoung-hwon;Lee, O Mi;Kim, Tae-Hun;Jung, In ha;Yu, SeungHo;Lee, Myun-Joo
    • Journal of Radiation Industry
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    • v.5 no.3
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    • pp.253-258
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    • 2011
  • Acetylsalicylic acid (ASA) has been issued recently in contaminated water environments because of potential impacts on ecosystem and public health. This study was aimed at investigating the possibility of ASA degradation using gamma ray irradiation. In addition, the use of sodium persulfate, hydrogen peroxide, ferrous sulfate were tested in order to examine a synergistic effect with gamma ray. The absorbed dose was ranged from 0.2 to 10 kGy and the concentration of oxidants were from 0.1 to 10 mM in this study. The concentration of ASA was gradually decreased corresponding to the increase of the absorbed dose. When soudium persulfate was simultaneously applied, most of the parent compound was completely degraded even at a low dose of 0.8 kGy. The removal efficiency of total organic carbon was 90% even at the highest dose of 10 kGy without sodium persulfate. However, the efficiency was dramatically enhanced up to 98% at the same dose by adding 10 mM of oxidants. It was suggested that hydroxyl radical ($OH{\cdot}$) and sulfate radical ($SO{_4}^-{\cdot}$) were formed in the system and made roles in degrading ASA at the same time.