• Title/Summary/Keyword: Relative potency

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Importance of the Degree of Antigen Polymerization by Detoxification in Modulating the Immunogenicity of Acellular Pertussis Vaccine

  • Bae Cheon-Soon;Hong Sung-Sang;Ahn Sang-Jeom;Jang Yang-Suk;Hur Byung-Ki
    • Biotechnology and Bioprocess Engineering:BBE
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    • v.10 no.3
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    • pp.230-235
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    • 2005
  • For the acellular pertussis vaccine with a high immunogenicity, the concentration, composition and characteristics of acellular pertussis antigens are the crucial points to be considered. Nevertheless, it has not been proved yet whether or not the polymerization degree, one of the characteristics of formalin-detoxified acellular pertussis antigens, has an influence on vaccine potency. Thus, in the present study, the correlations among detoxification conditions of acellular pertussis bulks, their polymerization degrees and their immunogenicities were examined. In addition, the relative importance of pertussis toxoid in vaccine immunogenicity was also investigated. Results show that a lower lysine concentration during detoxification induces highly-polymerized antigens, the immunogenicity has a great dependency on the polymerization degree of antigens, and also pertussis toxoid has a relatively stronger influence on the immunogenicity than other antigens. Accordingly, in the aspect of the potency of detoxified acellular pertussis vaccine, it can be demonstrated that the polymerization of antigens and its degree are the major factors affecting the immunogenicity along with a relatively high content of pertussis toxoid

Protective Effect of Flavonoids on Lymphocyte DNA Damage Using Comet Assay (Comet Assay를 이용한 Flavonoids와 항산화 비타민의 인체임파구 세포 DNA 손상 보호 효과)

  • 박유경;전은재;강명희
    • 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.

Influence of catecholamines on the free fatty acid metabolism in the tortoise (자라에 있어서 Catecholamine이 유리지산대사(遊離脂酸代謝)에 미치는 영향(影響))

  • Kim Byong-Joo
    • The Korean Journal of Pharmacology
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    • v.1 no.1 s.1
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    • pp.37-46
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    • 1965
  • 1. In the tortoise, Amyda japonica, a cold-blooded animal readily available in this country, the role of catecholamines in the regulation of free fatty acids(FFA) metabolism was investigated in both in vivo and in vitro studies. 2. Norepinephrine elevated both FFA and glucose levels in plasma. 3. When $50{\mu}g/kg$ of Epinephrine, Norepinephrine and Isopropylarterenol were administered intravenously, the relative effectiveness of mobilizing FFA was in the descending order of potency-Epinephrine, Norepinephrine and Isopropylarterenol. 4. In order to exclude the 'tonic influence of the endogenous catecholamines', reserpine was given to some animals. Two days after the reserpine-treatment, glucose showed a significant increase over the solely vehicle treated controls, FFA but an insignificant one. Excised auricles from those animals showed a diminished response to tyramine. Seven days after the treatment, however, when the depletion of catecholamines from the tissue stores seemed to be complete, judged from the absence of the response of isolated auricles to tyramine, both FFA and glucose levels were definitely lowered. 5. In in vitro experiments Epinephrine enhanced the FFA-release from the adipose tissue. The effect increased proportionately with the concentration until a maximal effect was attained at a concentration of 1x $10^5$ g/ml. 6. The order of potency in releasing FFA from adipose tissue in vitro was the same as in vitro, i.e., Epinephrine, Norepinephrine and Isopropylarterenol, but the differences were much less marked. 7. Ergotamine exerted no lipolytic action, but inhibited the lipolytic effect ef Epinephrine significantly. 8. Nethalide showed a slight lipolytic effect per se but inhibited the Epinephrine-induced lipolysis significantly. 9. Catecholamines play an important role in regulating FFA metabolism in the cold-blooded animal, just as in the warm-blooded animals, and the tortoise, Amyda japonica, may be used in the studies of fat metabolism as well as the rat.

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Bronchodilatory Effects of Coptidis Rhizomas in Isolated Rat Trachea (흰쥐 기관지평활근에 대한 황련류의 이완효능)

  • Lee, Dong-Ung;Chang, Ki-Churl
    • YAKHAK HOEJI
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    • v.41 no.6
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    • pp.797-801
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    • 1997
  • Recently we reported that water extracts of Coptidis Rhizomas showed calcium antagonistic action and alpha-adrenoceptor inhibitory action in the vascular smooth muscle. Since ca lcium antagonistic properties are important in the treatment of various diseases including asthma. In the present study, the bronchodilatory effects of crude extract of three kinds of Coptidis Rhizoma (Coptidis chinensis, Coptis japonica and root hair of Coptis japonica) was investigated using rat isolated trachea. The result showed that all extracts relaxed carbachol-contracted tracheal smooth muscle. Concentration-dependently, in which the root hair of Coptis japonica was the least potent. The inhibitory potency expressed in terms of $IC_{50}$ against carbachol contraction was 1.8${\mu}$g/ml and 2.7${\mu}$g/ml for Coptidis chinensis and Coptis japonica, respectively. These extracts also inhibited KCI-contracted tracheal smooth muscle. But the relative potency ($IC_{50}$) was 3.5 and 4.1 folds weaker than carbachol-induced contraction for Coptidics chinenesis and Coptis japonica, respectively. Pretreatment of crude extracts also inhibited carbachol- or KCI-induced contraction, non-competitively. These findings indicate that the extracts have muscarinic blocking as well as $Ca^{2+}$ channel blocking action. When provoked intracellular stored $Ca^{2+}$ release by carbachol in $Ca^{2+}$-free conditions, initial phasic contraction due to $Ca^{2+}$ release was significantly inhibited by the extracts. As taken together, we conclude that water extracts of Coptidis Rhizoma may be beneficial in bronchospasm or other broncheal tube narrowing conditions such as asthma.

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Bioassays of Plant Hormones and Plant Growth Regulating Substances II. Abscisic Acid and Brassinolide (식물홀몬 및 생장조절물질의 생물검정기술 II. Abscisic Acid 및 Brassinolide)

  • 최충돈
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.34 no.s01
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    • pp.16-25
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    • 1989
  • A bioassay is a test system using a living organism (in whole or in part) to determine the presence or relative potency of chemical substances. The development and uses of bioassay are intimately linked to the discovery and characterization of the major classes of plant hormones. An application of this relationship is helpful for understanding the concept of plant hormones as well as the use of bioassay. And plant bioassay have been development and employed not only for the discovery and characterization of the biological activity of plant growth regulators but also have served several important secondary roles. The ideal bioassay should possess the characteristic of high specificity. great sensitivity. short response time, low cost and ease of obtaining plant material. acceptable ease of manipulation, and minimal space and equipment requirements.

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Annomocherin, Annonacin and Annomontacin: A Novel and Two Known Bioactive Mono-Tetrahydrofuran Annonaceous Acetogenins from Annona cherimolia Seeds

  • Kim, Dal-Hwan;Son, Jong-Keun;Woo, Mi-Hee
    • Archives of Pharmacal Research
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    • v.24 no.4
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    • pp.300-306
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    • 2001
  • A novel and two known bioactive mono-tetrahydrofuran (THF) annonaceous acetogenins, annomocherin (1), annonacin (2) and annomontacin (3), have been isolated from the fractionated ethanolic extracts of the seeds of Annona cherimolia, guided by the brine shrimp lethality test (BST). Their structures were elucidated on the basis of spectroscopic and chemical methods. All compounds have a relative stereochemistry of threo/trans/threo for the mono-THF ring with two flanking hydroxyls. Compound 1 has a double bond at C-23/ 24 of aliphatic chain. Compound 1 was isolated from natural sources for the first time, and was named annomocherin. Two known Compounds 2 and 3 which have never been isolated from this species before, were obtained. Compound 1 exhibited potent and selective cytotoxicities against the breast carcinoma (MCF-7) and kidney carcinoma (A-498) cell lines with 100 to 1,000 times the potency of adriamycin. In brine shrimp lethality test (BST), 1-3 exhibited cytotoxicity.

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In Vitro Effect of Aspalatone on Platelet Aggregation and Thromboxane Production in Human Platelet Rich Plasma

  • Suh, Dae-Yeon;Han, Byung-Hoon
    • Biomolecules & Therapeutics
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    • v.4 no.2
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    • pp.122-126
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    • 1996
  • In vitro inhibitory effect of aspalatone ((3-(2-methyl-4-pyronyl)]-2-acetyloxybenzoate) on collagen-, ADP-, and epinephrine-induced platelet aggregation in human platelet rich plasma (PRP) was compared with the effects of reference drugs (acetylsalicylic acid, cilostazol and ticlopidine). Aspalatone inhibited time and dose dependently human platelet aggregation induced by collagen; relative potency was in the order of cilostazol>acetylsalicylic acid>aspalatone>ticlopidine. Aspalatone, like acetylsalicylic acid, potently inhibited only the secondary phase of ADP-and epinephrine-induced aggregation. Thromboxane $B^2$ production evoked by collagen in human PRP was inhibited significantly and concentration-dependently by aspalatone and acetylsalicylic acid. These results were in agreement with the earlier studies in which the antiplatelet action of aspalatone was indicated to be due to the inhibition of platelet cyclooxygenase activity (Han et al., Arzneim. Forsch./Drug Res. 44(II), 1122, 1994; Suh and Han, Yakhak Hoeji 39, 565, 1995). In addition, the inhibitory activity of aspalatone on the platelet aggregation appears to be inversely related to the rate of nonspecific deacetylation of the drug in plasma.

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Reduction of Estrogenic Activity by Gamma-ray Treatment (감마선 처리에 의한 에스트로겐 활성 저감 연구)

  • Kang, Sung-Wook;Seo, Jaehwan;Lee, Byoung Cheun;Kim, Suejin;Jung, Jinho
    • Journal of Korean Society on Water Environment
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    • v.26 no.6
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    • pp.948-953
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    • 2010
  • In this study, degradation of estrone (E1) and $17{\alpha}$-ethynylestradiol (EE2) by gamma-irradiation and subsequent reduction of estrogenic activity as a function of absorbed dose were conducted using the yeast two-hybrid assay. Relative potency of E1 and EE2 compared to estrogenic activity of $17{\beta}$-estradiol (E2) was found to be 0.0144 and 0.1605, respectively. More than 90% of E1 and EE2 (both $5.0{\times}10^{-6}M$) was removed at an absorbed dose of 5 kGy, but more than 40% of estrogenic activity still remained. The addition of $TiO_2$ catalyst appeared to improve the removal efficiency of E1 and decrease estrogenic activity while there was no significant effect for EE2. Additionally, the calculated estrogenic activity of E1 and EE2 based on a regression model was well correlated with the observed activity.

Health Risk of Airborne Complex Mixtures Based on their Mutagenicity (대기중 복합물질의 돌연변이원성과 인체 위해도)

  • Park, Seong-Eun;Chung, Yong
    • Journal of Korean Society for Atmospheric Environment
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    • v.12 no.3
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    • pp.269-278
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    • 1996
  • Airborne suspended particulates were collected by an Andersen high volume air sampler in a traffic area of Seoul from September 1990 to August 1991. Origanic matter extracted from particulates, their fractions, namely acidic, basic, neutral and carcinogenic subfractions (PAHs, nitroarenes) in neutral fractions were assayed for mutagenicity on TA98, TA100 and TA98NR deficient Salmonella strains, use of the pre-incubation method. The relative contribution to total mutanenicity of organic matters was highest in neutral fraction and was lowest in basic fraction. Among subfractions, that of neutral fraction was higher nitroarenes subfraction compared to PAHs subfraction. While the carcinogenic effect of benzo[a]pyrene was calculated as 0.96 persons/million persons based on unit risk estimates by extrapolation method, life time excess cancer risk estimate of EOM, neutral, PAH fraction based on their mutagenicity was calculated as 52, 42, 3.8 persons/million persons, respectively. These findings indicate that the mutagenic hazard of the partciculate, air organic complex mixture, may be dependent upon the mutagen composition in the particulate and interactions each of them. Therfore, health risk from air organic complex mixtures based on mutagenicity might be useful indicator for evaluation of actual risk.

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Effect of Caerulein on the Isolated Gall Bladder Strips of Rabbits (토끼 담낭절펼에 대한 Caerulein의 작용)

  • Cho, T.S.;Lee, W.C.;Hong, S.S.
    • The Korean Journal of Pharmacology
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    • v.10 no.1 s.15
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    • pp.47-52
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    • 1974
  • The isolated rabbit gall bladder strips were prepared according to the technique described by Amer and Becvar (1969). The strips were placed in a bath containing 100 ml of Locke-Ringer solution maintained at $38^{\circ}C$. Oxygen was continuously bubbled through the solution. The tension of the muscle strip was initially adjusted to 0.7g. The contractile response was measured isometrically by a force-displacement transducer connected to a polygraph. The effect of a number of autonomic drugs were studied for their interaction with caerulein (Prof. V. Erspamer, F.I. 6934 Caerulein, Farmitalia, Italia), a gastrin or CCK.PZ like peptide, on isolated rabbit gall bladder strips. In this preparation caerulein produced contractions of CCK-PZ type, but the relative potency on a weight basis was 40 times that of CCK-PZ. The response of caerulein was not modified by either cholinergic or alpha or beta adrenergic blockade. However, the response of caerulein and of barium on the strips were prevented by papaverine or aminophylline. Isoproterenol, papaverine or aminophylline alone relaxed the preparation whereas caerulein, CCK-PZ, acetylcholine, serotonin, histamine or barium chloride contracted the preparation. In summary, it is concluded that caerulein on the gall bladder strip seems to act independently of the autonomic nervous system and mediated via mechanisms apparently similar to those involved in the action of barium chloride.

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