• Title/Summary/Keyword: 9-dihydroxy-2

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Renal Action of SKF 81297, Dopamine $D_1$ Receptor Agonist, in Dogs (Dopamine $D_1$ Receptor 효능제인 SKF 81297의 신장작용)

  • 고석태;정경희
    • Biomolecules & Therapeutics
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    • v.9 no.3
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    • pp.209-217
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    • 2001
  • This study was attempted to investigate on renal effect of ($\pm$)6-chloro-7,8-dihydroxy-1-phenol 2,3,4,5-tetrahydro-lH-3 benzazepine (SKF 81297), dopamine $D_1$ receptor agonist, in dog. SKF 81297, when gluten intravenously, produced diuretic action along with the increases of renal plasma flow (RPF), glomerular filtration rate (GFR), amounts of N $a^{+}$ and $K^{+}$ excreted into urine ( $E_{Na}$ , $E_{K}$) and osmolar clearance ( $C_{osm}$). It also decreased the reabsorption rates of N $a^{+}$ and $K^{+}$ in renal tubule ( $R_{Na}$ , $R_{K}$) and free water clearance ( $C_{H2O}$), whereas ratios of $K^{+}$ agonist N $a^{+}$ in urine and filtration fraction (FF) was not changed. SKF 81297, when administered into a renal artery, elicited diuresis both in experimental kidney given the SKF 81297 and control kidney not given, while the effect was more remarkable in experimental kidney than those exhibited in control kidney. SKF 81297 given into carotid artery also exhibited diuresis, the potency at this time, compared to those induced by intravenous SKF 81297, was magnusgreat. Above results suggest that SKF 81297 produces diuresis by both indirect action through changes of central function and direct action being induced in kidney. Central diuretic action is mediated by improvement of renal hemodynamics, but direct action by inhibition of electrolytes reabsorption in renal tubule.enal tubule. tubule.

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Identification of Carotenoids from Green Alga Haematococcus pluvialis by HPLC and LC-MS (APCI) and Their Antioxidant Properties

  • Ranga, Rao;Sarada, A.R.;Baskaran, V.;Ravishankar, G.A.
    • Journal of Microbiology and Biotechnology
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    • v.19 no.11
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    • pp.1333-1341
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    • 2009
  • Haematococcus pluvial is, a green alga, accumulates astaxanthin (3,3'-dihydroxy-$\beta$,$\beta$'-carotene-4,4'-dione) upto 2-3% on a dry weight basis. In the present study, identification of carotenoids from Haematococcus cyst cell extract by HPLC and LC-MS (APCI) and their antioxidant properties were evaluated in in vitro model systems. The extract exhibited 89% and 78% antioxidant activities in the $\beta$-carotene linoleate model and the hydroxyl radical scavenging model, at 9 ppm of total carotenoid, respectively. The extract also showed 80%, 85%, and 79% antioxidant activities against lipid peroxidation in the kidney, brain, and liver of rats. Low-density lipoprotein oxidation induced by $Cu^{2+}$ ions was also protected (45%, 64%, and 75%) by the extract in a dose-dependent manner with different carotenoid levels. Thiobarbituric acid reactive substances concentration in the blood, liver, and kidney of rats were also significantly (p<0.005) decreased in H. pluvialis-treated rats. The potent antioxidant activity is attributable to various carotenoids present in the extract.

Analysis and Comparison of Cerebroside Components from Soybean Fermented Foods (대두발효식품 Cerebroside의 구성성분 분석 및 비교)

  • 이은열;김희숙
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.31 no.2
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    • pp.177-183
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    • 2002
  • Cerebroside fatty acids, sugars and long-chain sphingoid bases in raw soybean and soybean fermented foods (chongkukjang and deunjang) were analyzed using gas chromatography-mass spectrometry (GC-MS) and high-pH anion exchange chromatography with pulsed amerometric detection (HPAEC-PAD). Fatty acids of acid-hydrolyzed cerebrosides were derivatized to O-TMS methylester and analysed. The major fatty acids in raw soybean and chongkukjang cerebrosides were identified as 2-hydroxyhexadecanoic acid (16 : 0h), 2-hydroxydocosanoic acid (22 : 0h) and 2-hydroxytetracosanoic acid (24 : 0h). In the case of deunjang cerebroside, 24 : 0h (40.9%) and 22 : 0h (23.4%) were major fatty acids, but 16 : 0h, 23 : 0h, 25 : 0h and 26 : 0h were also detected. Long-chain sphingoid bases of acid-hydrolyzed cerebrosides from raw soybean, chongkukjang and deunjang consisted primarily of 4-tracts, 8-tracts-sphingadienine (dihydroxy base, d18 : 2$\Delta$$^{4trans, 8trans}$) and sis-tracts isomers of 4-hydroxy-sphingenine (trihydroxy base, tl8:1$\Delta$$^{4trans or cis}$) with much less amounts of phytosphingosine (tl8: 0) and isomers of sphingenine (d18 : 1). Although deunjang is a soybean food fermented by fungi and microorganisms for a long period, 2-hydroxyoctadec-3-enoic acid (18 : 1h) and branched 9-methyl-4,8-sphingadienine known as compositional cerebroside fatty acids in Aspergillus species were not detected. Mass spectrum for sugar derivatives in cerebrosides of soybean foods including raw soybean and fermented soybean showed that C-1 of glucose moiety was linked to ceramide backbone as like a monoglucosylceramide.

Neuroprotective Effect of Wogonin: Potential Roles of Inflammatory Cytokines

  • Piao, Hua-Zi;Jin, Shun-Ai;Chun, Hyang-Sook;Lee, Jae-Chul;Kim, Won-Ki
    • Archives of Pharmacal Research
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    • v.27 no.9
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    • pp.930-936
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    • 2004
  • Wogonin (5,7-dihydroxy-8-methoxyflavone), an active component originated from the root of Scutellaria baicalensis Georgi, has been reported to possess antioxidant and anti-inflamma-tory properties. In this study, we investigated the neuroprotective effect of wogonin in a focal cerebral ischemia rat model. Wogonin markedly reduced the infarct volume after 2 h middle cerebral artery occlusion followed by 22 h reperfusion. Wogonin decreased the production of nitric oxide and inflammatory cytokines such as TNF-$\alpha$ and IL-6 in lipopolisaccharide-stimu-lated microglial cells. While wogonin reduced the activity of NF-$textsc{k}$B, it did not change the activ-ity of mitogen-activated protein kinases family members, p38, ERK and JNK. The lipopolisaccharide-stimulated production of NO and cytokines was significantly blocked by vari-ous kinds of NF-$textsc{k}$B inhibitors such as N-acetyl cysteine, pyrrolidinedithiocarbamate and MG-132. The data may indicate that wogonin has neuroprotective effect by preventing the over-activation of microglial cells, possibly by inactivating NF-$textsc{k}$B signaling pathway

Effects of Calcium and Vitamin D Supplementation on Bone Mineral Density and Biochemical Markers in Osteoporotic Postmenopausal Women

  • Kim, Jeong, Seon;Kim, Joo-Hak
    • Nutritional Sciences
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    • v.9 no.1
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    • pp.42-47
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    • 2006
  • It has been reported that taking a proper amount of calcium and vitamin D helps to increase bone mineral density (BMD) and is effective in decreasing the risk of osteoporosis. This study investigated the supplementary effects of calcium and vitamin D on postmenopausal women who had osteoporosis and used calcium and vitamin D supplements. The study subjects consisted of osteoporotic postmenopausal women who were recruited from the Department of Orthopedics in a university-affiliated hospital. Sixty-seven study subjects were orally administrated 1,000 mg of calcium (calcium carbonate) and 2.5 mg of active vitamin D (1-$\alpha$ hydroxyvitamin D) (cholecalciferol 250 IU) twice a day for a year and a half. BMD and biochemical markers were evaluated and repeated every six months. One year after the intervention test, the bone mineral density of the lumbar spine was significantly increased as compared to the baseline. Six months after supplement administration, the level of serum alkaline phosphatase began to decrease, and afterwards a significant difference was maintained Concentration of 1, 25-dihydroxy-vitamin D at 1.5 years was higher than that of the baseline. In comparison with that of the baseline, the level of urinary hydroxyproline in the study subjects over six months was significantly decreased This study continued that effects such as BMD improvement and changes in biochemical markers appeared at least one year after administration of supplements.

Naphthoquinone Analog-induced G1 Arrest is Mediated by cdc25A Inhibition and p53-independent p21 Induction in Human Hepatocarcinoma Cells

  • Kim, Won-Ho;Kim, Jung-Woong;Jang, Sang-Min;Song, Ki-Hyun;Ham, Seung-Wook;Choi, Kyung-Hee
    • Animal cells and systems
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    • v.11 no.1
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    • pp.9-15
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    • 2007
  • The naphthoquinone analog (2,3-dichloro-6,9-dihydroxy-1,4-naphtoquinone, NA) has an inhibitory effect on cdc25A protein phosphatase in vitro, which is responsible for G1/S transition during cell cycle. However, the exact mechanism inducing the growth inhibition is not understood. In this study, we investigated the regulatory mechanisms of growth arrest induced by NA, as a new potent inhibitor of cdc25A phosphatase, in human hepatocarcinoma SK-hep-1 cells. We found that NA induced the G1 arrest by perturbation of protein tyrosine dephosphorylation of Cdk2, which may be resulting from inhibition of cdc25A phosphatase. In addition, p21 was expressed in a p53-independent manner and participated in the NA-induced G1 arrest by inhibiting Cdk2 activity. Although the exact mechanism is not known, the p21 expression might be related to MAPK activation. From these results, we suggest that NA induces G1 arrest via inhibition of cdc25A and induction of p53-independent p21 expression in SK-Hep-1 cells.

The Fok1 Vitamin D Receptor Gene Polymorphism and 25(OH) D Serum Levels and Prostate Cancer among Jordanian Men

  • Atoum, Manar Fayiz;AlKateeb, Dena;Mahmoud, Sameer Ahmed AlHaj
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.6
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    • pp.2227-2230
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    • 2015
  • Background: Prostate cancer (PCa) is one of the most commonly diagnosed neoplasms and the second leading cause of cancer death in men in the Western world. Vitamin D (1,25dihydroxy vitamin D) is linked to many biological processes that influence oncogenesis but data on relations between its genetic variants and cancer risk have been inconsistent. The aim of this study was to determine associations between a vitamin D genetic polymorphism and 25-hydroxyvitamin D [25(OH)D] levels and prostate cancer. Materials and Methods: Genomic DNA was extracted from 124 Jordanian prostate cancer patients and 100 healthy volunteers. Ethical approval was granted from the ethical committee at Hashemite University and written consent was given by all patients. PCR was used to amplify the vitamin D receptor Fok1 polymorphism fragment. 25(OH)D serum levels were measured by competitive immunoassay. Results: All genotypes were in Hardy-Weinberg equilibrium. Genotype frequency for Fok1 genotypes FF, Ff and ff was 30.7%, 61.3% and 8.06%, for prostate cancer patients, while frequencies for the control group was 28.0%, 66.0% and 6.0%, respectively, with no significant differences. Vitamin D serum level was significantly lower in prostate cancer patients (mean 7.7 ng/ml) compared to the control group (21.8 ng/ml). No significant association was noted between 25(OH)D and VDR Fok1 gene polymorphism among Jordanians overall, but significant associations were evident among prostate cancer patients (FF, Ff and ff : 25(OH)D levels of 6.2, 8.2 and 9.9) and controls (19.0, 22.5 and 26.3, respectively). An inverse association was noted between 25(OH)D serum level less than 10ng/ml and prostate cancer risk (OR 35.5 and 95% CI 14.3- 88.0). Conclusions: There is strong inverse association between 25(OH)D serum level less than 10ng/ml level and prostate cancer risk.

Chemical Constituents of the Culture Broth of Panus rudis

  • Song, Ja-Gyeong;Ha, Lee Su;Ki, Dae-Won;Choi, Dae-Cheol;Lee, In-Kyoung;Yun, Bong-Sik
    • Mycobiology
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    • v.49 no.6
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    • pp.604-606
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    • 2021
  • In our ongoing search for new secondary metabolites from fungal strains, one novel compound (1) and nine known compounds (2-10) were isolated from the EtOAc-soluble layer of the culture broth of Panus rudis. The culture broth of P. rudis was extracted in acetone and fractionated by solvent partition; column chromatography using silica gel, Sephadex LH-20, and Sephadex G-10; MPLC; and HPLC. The structures of isolated compounds were elucidated by one- and two-dimensional NMR and LC-ESI-mass measurements. One new compound, panepoxydiol (1), and nine known compounds, (E)-3-(3-hydroxy-3-methylbut-1-en-1-yl)-7-oxabicyclo[4.1.0]hept-3-ene-2,5-diol (2), isopanepoxydone (3), neopanepoxydone (4), panepoxydone (5), panepophenanthrin (6), 4-hydroxy-2,2-dimethyl-6-methoxychromane (7), 6-hydroxy-2,2-dimethyl-3-chromen (8), 2,2-dimethyl-6-methoxychroman-4-one (9), 3,4-dihydroxy-2,2-dimethyl-6-methoxychromane (10), were isolated from the culture broth of P. rudis. This is the first report of isolation of a new compound panepoxydiol (1) and nine other chemical constituents (2-5, 7-10) from the culture broth of P. rudis.

Evaluation of Lethality by Chemical Marker (Chemical Marker를 이용한 살균도 예측)

  • Choi, Yang-Mun;Kim, Hie-Joon
    • Korean Journal of Food Science and Technology
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    • v.29 no.1
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    • pp.32-37
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    • 1997
  • The rate constants and activation energies for formation of two chemical markers, M-1 and M-2 at sterilization temperatures were determined in a meatball system. Destruction rates for bacterial spores were also determined. The rate constants for M-1 and M-2 formation at $121^{\circ}C$ were 0.03 and 0.28 Abs/min, respectively. The activation energies for M-1 and M-2 were 27.9 and 24.6 Cal/mol. M-2 was formed faster than M-1 and reached a maximum and decreased. M-1 formation continued up to 30 min at $121^{\circ}C$ and 10 min at $131^{\circ}C$, which makes M-1 a more useful chemical marker for high $F_0$ values. The D-values for spores (B. stearothermophilus ATCC 12980) at 111, 114.4, 117.7 and $121^{\circ}C$ were 7.5, 4.5, 1.9 and 0.58 respectively. At temperatures between 111 and $121^{\circ}C$, there was a liner correlation between destruction of the spores and the M-1 formation. It was difficult to get accurate D-value at $126^{\circ}C\;and\;131^{\circ}C$, because almost all spores were dead before temperature at the center of the meatball reached $126^{\circ}C$. These data suggest that the chemical marker should be used to evaluate overprocessing as well as microbial lethality in aseptic processing.

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Synthetic Derivatives of Diosgenin and Their Antinociceptive and Antihypercholesterolemic Effects (Diosgenin 유도체 합성과 진통 및 항고지혈 효과)

  • Kim, Hak-Soon;Ma, Eun-Sook
    • YAKHAK HOEJI
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    • v.51 no.1
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    • pp.56-62
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    • 2007
  • Twelve epoxy and hydroxydiosgenin derivatives (DI-1${\sim}$DI-12) were synthesized from diosgenin (25(R)-5-spirosten-3${\beta}$-ol). Diosgenin was epoxidized with m-chloroperoxybenzoic acid (mCPBA) to oxidize 25(R)-4${\alpha}$,5${\alpha}$-epoxyspirostane (DI-1). Diosgenin was reacted with DDQ to form 25(R)-1,4,6-spirostatrien-3-one (DI-2), which was treated with 30% H$_2$O$_2$ to give 25(R)-1${\alpha}$,2${\alpha}$-epoxy-4,6-spirostadien-3-one (DI-3) and treated with mCPBA to form 25(R)-6${\alpha}$,7${\alpha}$-epoxy-1,4-spirostadien-3-one (DI-7), respectively. DI-3 was reduced with NaBH$_4$ to afford 25(R) -1${\alpha}$,2 ${\alpha}$-epoxy-4,6-spirostadien-3${\beta}$-ol(DI-4) and reacted with Li metal in absolute ethanol to form 25(R)-2-ethoxy-1,4,6-spirostatrien-3-one (DI-5). DI-7 was reduced with NaBH$_4$ to produce 25(R)-3${\beta}$,7${\alpha}$-dihydroxy-4-spirostene (DI-8) and treated with Li metal in liquid ammonia to produce 25(R)-7${\alpha}$-hydroxy-4-spirosten-3-one (DI-9). DI-2 was reduced with NaBH$_4$ to form 25(R) -4,6-spirestadien-3${\beta}$-ol(DI-10), which was stirred with 30% H$_2$O$_2$ to synthesize 25(R)-4,6-spirostadien-3-one (DI-11) and reacted with mCPBA to give 25(R)-4${\beta}$,5${\beta}$ -epoxy-6-spirosten-3${\beta}$-ol (DI-12), respectively. The antinociceptive effects of synthesiz ed compounds were measured by hot plate method and compound DI-7 signifcantly exhibited antinociceptive effect. DI-2 decreased the serum triglyceride and total cholesterol levels in poloxamer P-407 injected rat.