• Title/Summary/Keyword: [$^3H$]DHA

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Binding Studies of Cardiovascular Drug on ${\beta}$ Adrenoceptors in Rat Left Ventricle using $(-)-[^3H]-DHA$, $Non-{\beta}_1/{\beta}_2-selective$ Radioligand (${\beta}_1/{\beta}_2$ 비선택적 Radioligand $(-)-[^3H]-DHA$를 사용한 Rat 좌심실 ${\beta}-adrenoceptor$에 대한 심장순환계 약물의 Binding)

  • Kwon, Kwang-Il;Lee, Sun-Kyung;Yoo, Sung-Eun
    • The Korean Journal of Pharmacology
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    • v.27 no.2
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    • pp.119-123
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    • 1991
  • ${\beta}-Adrenoceptor$ binding study of ${\beta}-agonist$ ((-)NE), ${\beta}-antagonists$ $(({\pm})\;propranolol,\;labetalol)$ and PDE inhibitors (imazodan, KR-30045, KR-30075 etc.) was performed using $(-)-[^3H]-DHA$, as a $non-{\beta}_1/{\beta}_2$ selective radioligand. In saturation studies, $K_d$ and $B_{max}$ of $(-)-[^3H]-DHA$ to ${\beta}-adrenoceptors$ in rat left ventricle in which both ${\beta}_1$ and ${\beta}_2$ receptors coexist were determined to be $1.5{\pm}0.43\;nM$ and $22.0{\pm}0.9\;fmol/mg$ protein, respectively. $({\pm})Propranolol$, labetalol and (-)NE competed for $(-)-[^3H]-DHA$ binding sites in an essentialy monophasic manner with $Ki=17.0{\pm}0.40\;nM,\;57.3{\pm}1.30\;nM,\;and\;1.57{\pm}0.95\;{\mu}M$, respectively. All of PDE inhibitors inhibited the $(-)-[^3H]-DHA$ binding by only below 10% even at the high concentration of $10^{-3}M$. The present results suggest that propranolol, labetalol and NE are $non-{\beta}_1/{\beta}_2$ selective antagonists and agonist, respectively. Additionally, this study shows that imazodan and new synthesized PDE inhibitors may hardly have the affinities to ${\beta}-adrenoceptors$ in cardiac muscle.

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고수율 DHA생산을 위한 Thraustochytrium aureum의 배지조성과 발효조건에 관한 연구

  • Park, Gyeong-Won;Kim, Jun-Sik;Heo, Byeong-Gi
    • 한국생물공학회:학술대회논문집
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    • 2000.04a
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    • pp.291-294
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    • 2000
  • Marine fungus, Thraustochytrium aureum ATCC 34034, was incubated in artificial sea water media in order to produce docosahexaenoic acid(DHA). Cultures were performed at $24^{\circ}C$ in light for 3 days with orbital shaker at 200rpm. Maximum cell productivity of 1.34g/L and DHA yield of 41.4 mg/L were obtained by using this method, which is almost the twice level of DHA yield obtained for the strains reported previously. This strain did not produce DHA in YM media and YPG media. The results indicate that salinity influenced cell growth and production of DHA.

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Effect of Calcium Antagonists on the Cardiac ${\beta}$-Adrenergic Receptors (칼슘 길항제가 심장 ${\beta}$-Adrenergic Receptors에 미치는 영향)

  • 이신웅;김정구
    • Biomolecules & Therapeutics
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    • v.1 no.1
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    • pp.1-8
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    • 1993
  • It has been known that calcium antagonists also inhibit the radioligand binding to muscarinic and $\alpha$-adrenergic receptors and, in case of verapamil, these inhibitions may play a role in the effects of verapamil on the heart. In this study, the effects of nicardipine, nifedipine, nimodipine, diltiazem and verapamil on the binding of [$^3H$]dihydroalprenolol (DHA) to dog cardiac ${\beta}$-adrenergic receptors were examined. A single uniform [$^3H$]DHA binding site ($K_D/= 5nM\;and\;B_{max}=2600$ fmol/mg protein) was identified in dog cardiac sarcolemma. [$^3H$]DHA binding was not affected by the usual therapeutic concentrations of these calcium antagonists (nanomolar range) but in the "nonspecific"concentration ranges ($28-180{\mu}m$) these drugs inhibited [$^3H$]DHA binding to $\beta$-adrenergic receptors. Nicardipine, nifedipine, nimodipine and diltiazem competed for [$^3H$]DHA binding to ${\beta}$-adrenergic receptors with dissociation constants ($K_i$) of $28{\mu}m,\' 74{\mu}m, 39{\mu}m \;and \;35{\mu}m,$ respectively. Verapamil ($K_i=176.5 {\mu}m$) was less potent inhibitor than other drugs and this inhibition was noncompetitive; the maximal binding capacity ($B_{max}$) $300 {\mu}m$ verapamil without change in the apparent dissociation constant (4K_D$) for DHA. These results indicate that the inhibitory action of calcium antagonists at high concentrations on ${\beta}$-adrenergic receptors is not involved in the therapeutic effects of these drugs by the calcium channel blocking action.

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Effects of Dietary Algal Docosahexaenoic Acid Oil Supplementation on Fatty Acid Deposition and Gene Expression in Laying Tsaiya Ducks

  • Cheng, C.H.;Ou, B.R.;Shen, T.F.;Ding, Shih-Torng
    • Asian-Australasian Journal of Animal Sciences
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    • v.19 no.7
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    • pp.1047-1053
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    • 2006
  • The current study was designed to determine the effects of dietary docosahexaenoic acid (DHA) on fatty acid deposition in egg yolk and various tissues of laying Tsaiya ducks, and on the mRNA concentrations of hepatic lipogenesis-related transcription factors. Thirty laying ducks were randomly assigned to three treatments with diets based on corn-soybean meal (ME: 2803 kcal/kg; CP: 17.1%; Ca: 3.4%) supplemented with 0% (control diet), 0.5% or 2% algal DHA oil. The DHA content in egg yolks of the ducks was elevated significantly (p<0.01) with the supplementation of dietary DHA. The DHA percentage of the total fatty acids in the egg yolk of laying ducks was 0.5%, 1.3% and 3.4% for 0%, 0.5% and 2% algal DHA oil treatments, respectively, for the $1^{st}$ week, and 0.5%, 1.5% and 3.3% for the $2^{nd}$ week. Therefore, algal DHA oil can be utilized by laying Tsaiya ducks to enhance the egg-yolk DHA content. The concentrations of triacylglycerol (TG) and cholesterol in plasma of laying Tsaiya ducks were not affected by dietary DHA treatments (p>0.05). The DHA concentration in plasma, liver, and skeletal muscle was increased with the addition of dietary algal DHA oil (p<0.05). The mRNA abundance of sterol regulatory element binding protein 1 (SREBP1) and SREBP2 in the livers of laying Tsaiya ducks was not affected by dietary DHA, suggesting that the expression of these transcription factors is tightly controlled and not sensitive to DHA treatments.

Neural Adaptation of Beta Adrenergic Receptor Subtypes after Chronic Imipramine Treatment: A Quantitative Autoradiographic Study

  • Park, Hae-Young;Hong, Young-Sook;Park, Chan-Woong
    • The Korean Journal of Physiology and Pharmacology
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    • v.1 no.2
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    • pp.161-167
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    • 1997
  • This study compares the subtypes of central beta adrenergic receptors (ARs) of brains of untreated rats with those of imipramine-treated rats. Beta adrenergic receptors were measured by quantitative autoradiography of the binding of $^3H$-dihydroalprenolol ($^3H$-DHA) in coronal sections of rat brain. Repeated treatment of rats with imipramine significantly reduced the binding of $^3H$-DHA to beta-1 AR in many brain areas, especially throughout the cerebral cortex, hippocampus, thalamus, and amygdala. Significant reductions of the binding of $^3H$-DHA to beta-2 AR were not found in any area of the brain. These data suggests that a selective down-regulation of beta-1 AR may be involved in the adaptive changes occurring after prolonged imipramine treatment.

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The Influence of DHA Supplementation in Maternal Diets on Fatty Acid Compositions of Plasma Lipids and Human Milk (수유기에 식이와 함께 섭취한 DHA가 산모의 혈액과 모유의 지질조성에 미치는 영향)

  • 조여원
    • Journal of Nutrition and Health
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    • v.29 no.2
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    • pp.213-222
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    • 1996
  • The most abundant long-chain polyunsaturated fatty acid in brain lipids is docosahexaenoic acid(C22 : 6 N-3, DHA). It is incorporated into nerve tissues mostly in utero and during the first year of life. DHA in brain is derived from either pre-formed DHA in human milk or by infant hepatic synthesis from linolenic acid in milk. This study was designed to investigate the effects of DHA supplementation on fatty acid profiles in maternal plasma lipid and breast milk. Twenty lactating women participated in the study. Seven women took 3g of fish oil per day and vitamin E for 28 days starting from the day of giving birth. Five women consumed 1.5g of fish oil as well as tivamin E, and the rest took vitamin E supplements for the same period of time. Dietary questionnaires and 3 consecutive 24-h recalls were collected to evaluate theri nutritional status and food habits. Finding that DHA intake from fish was not significantly different among three experimental groups, the partcipants were instructed to continue eating their usual home diets. Milk samples were taken on the day of giving birth, as well as the 7th, 14th and 28th day being the supplement phase, and finally 2 weeks after the cessating of DHA supplements. The amounts of the fish oil supplements produced significant dose-dependent increased in the DHA content of milk and plasma, but to a lesser degree. Base-line for 28 days raised the level to 2.05$\pm$0.43% and 1.5g/day supplement produced DHA levels of 1.02$\pm$0.19%. The results of this study indicated that relatively small amount of dietary DHA supplementation significantly elevats DHA content in milk. This would clearly elevate the infant's DHA intake which in turn may have implications for the infant's brain development.

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Dihydroartemisinin inhibits HepG2.2.15 proliferation by inducing cellular senescence and autophagy

  • Zou, Jiang;Ma, Qiang;Sun, Ru;Cai, Jiajing;Liao, Hebin;Xu, Lei;Xia, Jingruo;Huang, Guangcheng;Yao, Lihua;Cai, Yan;Zhong, Xiaowu;Guo, Xiaolan
    • BMB Reports
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    • v.52 no.8
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    • pp.520-525
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    • 2019
  • Dihydroartemisinin (DHA) has been reported to possess anti-cancer activity against many cancers. However, the pharmacologic effect of DHA on HBV-positive hepatocellular carcinoma (HCC) remains unknown. Thus, the objective of the present study was to determine whether DHA could inhibit the proliferation of HepG2.2.15 cells and uncover the underlying mechanisms involved in the effect of DHA on HepG2.2.15 cells. We found that DHA effectively inhibited HepG2.2.15 HCC cell proliferation both in vivo and in vitro. DHA also reduced the migration and tumorigenicity capacity of HepG2.2.15 cells. Regarding the underlying mechanisms, results showed that DHA induced cellular senescence by up-regulating expression levels of proteins such as p-ATM, p-ATR, ${\gamma}-H_2AX$, P53, and P21 involved in DNA damage response. DHA also induced autophagy (green LC3 puncta gathered together and LC3II/LC3I ratio increased through AKT-mTOR pathway suppression). Results also revealed that DHA-induced autophagy was not linked to senescence or cell death. TPP1 (telomere shelterin) overexpression could not rescue DHA-induced anticancer activity (cell proliferation). Moreover, DHA down-regulated TPP1 expression. Gene knockdown of TPP1 caused similar phenotypes and mechanisms as DHA induced phenotypes and mechanisms in HepG2.2.15 cells. These results demonstrate that DHA might inhibit HepG2.2.15 cells proliferation through inducing cellular senescence and autophagy.

STUDY ON THE STABILITY OF O/W AND MLV EMULSION CONTAINING DIHYDROXYACETONE

  • Joo, Yong-Joon;Han, Yeoung-Jun;Joo, Yong-Ho;Jeon, Young-Hwan
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.24 no.3
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    • pp.123-128
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    • 1998
  • Dihydroxyacetone (DHA) has been used as a self tanning agent and many emulsion formulations containing DHA have been studied. In an emulsion, many factors which have negative effect on DHP and the resultant DHA decomposition can destabilize the emulsion base. In this study, two kinds of emulsion with 5% DHA were prepared, O/W type emulsion and Multilamellavesicle (MLV) type emulsion to compare the stabilization effects of both emulsions on the DHA. The OHA concentration was analyzed quantitatively by high performance liquid Chromatography (HPLC), also the pH and viscosity of both emulsions were measured for stability. This process was carried out over 4 months. For HPLC, a bondaclone $C_{18}$ column with a mobile phase of distilled water and UV detector were used. The results of these experiment showed that DHA is more stable in an MLV emulsion than it is in an O/W type emulsion.

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Development of Hydrophobically Modified Casein Derivative-Based Delivery System for Docosahexaenoic Acids by an Acid-Induced Gelation

  • Ho-Kyung Ha;Dan-Bi Woo;Mee-Ryung Lee;Won-Jae Lee
    • Food Science of Animal Resources
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    • v.43 no.2
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    • pp.220-231
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    • 2023
  • Although omega-3 fatty acids including docosahexaenoic acid (DHA) contain various health-promoting effects, their poor aqueous solubility and stability make them difficult to be induced in dairy foods. The aims of this research were to manufacture casein derivative-based delivery system using acid-induced gelation method with glucono-σ-lactone and to investigate the effects of production variables, such as pH and charged amount of linoleic acid, on the physicochemical properties of delivery systems and oxidative stability of DHA during storage in model milk. Covalent modification with linoleic acid resulted in the production of casein derivatives with varying degrees of modification. As pH was reduced from 5.0 to 4.8 and the charged amount of linoleic acid was increased from 0% to 30%, an increase in particle size of casein derivative-based delivery systems was observed. The encapsulation efficiency of DHA was increased with decreased pH and increased charged amount of linoleic acid. The use of delivery system for DHA resulted in a decrease in the development of primary and secondary oxidation products. An increase in the degree of modification of casein derivatives with linoleic acid resulted in a decrease in the formation of primary and secondary oxidation products than of free DHA indicating that delivery systems could enhance the oxidative stability of DHA during storage in model milk. In conclusions, casein derivatives can be an effective delivery system for DHA and charged amount of linoleic acid played a key role determining the physicochemical characteristics of delivery system and oxidative stability of DHA.

Production of 1,3-Dihydroxyacetone from Glycerol by Gluconobacter oxydans ZJB09112

  • Hu, Zhong-Ce;Liu, Zhi-Qiang;Zheng, Yu-Guo;Shen, Yin-Chu
    • Journal of Microbiology and Biotechnology
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    • v.20 no.2
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    • pp.340-345
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    • 2010
  • The culture variables were optimized to increase 1,3-dihydroxyacetone (DHA) production by Gluconohacter oxydans ZJB09112 in shake flasks and bubble column bioreactors. After fermentation in the optimized medium (g/l: yeast extract 5, glycerol 2.5, mannitol 22.5, $K_2HPO_4$ 0.5, $KH_2PO_4$ 0.5, $MgSO_4{\cdot}7H_2O$ 0.1, $CaCO_3$ 2.0, pH 5.0), when five times of glycerol feeding were applied, $161.9{\pm}5.9\;g/l$ of DHA was attained at a $88.7{\pm}3.2%$ conversion rate of glycerol to DHA.