• Title/Summary/Keyword: ${\beta}$-ME

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Inhibitory Effect of Rosmarinic acid Extrcted from Euonymus Alatus on Cyclooxygenase-2

  • Ryu, Jung-Man
    • The Journal of Korean Medicine
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    • v.29 no.5
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    • pp.111-117
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    • 2008
  • Objectives and methods : Previous mechanistic studies suggest the cyclooxygenase-2 (COX-2) inhibitors represent the good candidates against tumor progression. MeOH extract of the stem barks of Euonymus alatus induced the strong inhibition of COX-2. A phenolic compound responsible for the anti- COX-2 known to involve in tumor adhesion and invasion has been studied through the methanol extracts. The compound, rosmarinic acid (ROS-A) was an ester of caffeic acid and 3,4-dihydroxyphenyllactic acid. ROS-A showed a strong inhibitory effect of COX-2 activity in a concentration-dependent manner. Then we have measured the IL-1${\beta}$, IL-6 and TNF-${\alpha}$ production related the immune regulation, induction of inflammatory related genes. Results and Conclusions :Hep3B cells produce proinflammatory cytokines of IL-1${\beta}$, IL-6 and TNF-${\alpha}$ while ROS A inhibited the cytokines production. Since IL-1${\beta}$, IL-6 and TNF-${\alpha}$ need the transcription factors such as nuclear factor- ${\kappa}$B (NF-${\kappa}$B) and activated protein-1 (AP-1), we measured the transcription factors. ROS-A inhibited the activation of p65, p50, c-Rel subunits of NF-${\kappa}$B and AP-1 transcription factors. These findings indicate that ROS A from the stem bark of E. alatus inhibits proliferation in metastatic cancer cells. It was suggested that stem barks of E. alatus could be suitable for anti-cancer drugs.

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Chemical Constituents of Lathyrus davidii

  • Park, Su-Yeon;Kim, Ju-Sun;Lee, So-Young;Bae, Ki-Hwan;Kang, Sam-Sik
    • Natural Product Sciences
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    • v.14 no.4
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    • pp.281-288
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    • 2008
  • From the MeOH extract of the whole plants of Lathyrus davidii (Fabaceae), thirteen constituents were isolated and identified as the flavonoids astragalin, isoquercitrin, nicotiflorin, and rutin, as the saponins soyasapogenol B 3-O-${\beta}$-D-glucuronopyranoside, azukisaponins II and V, soyasaponins II and V and as 4-O-${\beta}$-Dglucopyranosyl syringic acid, uracil and n-hexacosanol. Five saponins and 4-O-${\beta}$-D-glucopyranosyl syringic acid were isolated from the BuOH fraction as their methyl esters. Ombuoside (rutin 7,4'-di-O-methyl ether) was also isolated from the methylated BuOH-soluble fraction. However, no ombuoside was detected in the HPLC analysis of the nonmethylated BuOH fraction. Therefore, ombuoside is an artifact derived from methylation of rutin. All of these compounds were isolated for the first time from this plant.

HIF-1-Dependent Induction of Jumonji Domain-Containing Protein (JMJD) 3 under Hypoxic Conditions

  • Lee, Ho-Youl;Choi, Kang;Oh, Hookeun;Park, Young-Kwon;Park, Hyunsung
    • Molecules and Cells
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    • v.37 no.1
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    • pp.43-50
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    • 2014
  • Jumonji domain-containing proteins (JMJD) catalyze the oxidative demethylation of a methylated lysine residue of histones by using $O_2$, ${\alpha}$-ketoglutarate, vitamin C, and Fe(II). Several JMJDs are induced by hypoxic stress to compensate their presumed reduction in catalytic activity under hypoxia. In this study, we showed that an H3K27me3 specific histone demethylase, JMJD3 was induced by hypoxia-inducible factor (HIF)-$1{\alpha}/{\beta}$ under hypoxia and that treatment with Clioquinol, a HIF-$1{\alpha}$ activator, increased JMJD3 expression even under normoxia. Chromatin immunoprecipitation (ChIP) analyses showed that both HIF-$1{\alpha}$ and its dimerization partner HIF-$1{\beta}$/Arnt occupied the first intron region of the mouse JMJD3 gene, whereas the HIF-$1{\alpha}/{\beta}$ heterodimer bound to the upstream region of the human JMJD3, indicating that human and mouse JMJD3 have hypoxia-responsive regulatory regions in different locations. This study shows that both mouse and human JMJD3 are induced by HIF-1.

The Effect of Final Heat Treatment and Welding on Irradiation Growth of Zircaloy-4 (최종열처리와 용접Zircaloy-4의 방사선조사 성장에 미치는 영향)

  • Im, Gap-Sun;Han, Jeong-Ho;Jeong, Yong-Hwan;Lee, Deok-Hyeon;Park, Gi-Seong;Kim, Yeong-Seok;Kim, Seon-Jin
    • Korean Journal of Materials Research
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    • v.3 no.1
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    • pp.65-71
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    • 1993
  • Abstract The effect of final heat treatment and welding on the irradiation growth of Zircaloy-4 was investigated. As a simulation for neurtron irradiation, accelerated proton beam with the energy of 3.5MeV was used up to the proton fluence of 9.8 ${\times}{10^{21}}$p/$m^2$ in the present study. It was found that irradiation growth of the annealed specimen was the highest and that of the ${\beta}$-quenched specimen was the samllest among the present specimens. The magnitude of irradiation growth of the present specimens decreased by welding. The difference in the magnitude of irradiation growth of the present specimens with different final heat treatment and the effect of welding on it were quantitatively analyzed in terms of crystallographic texture by using Kearns number, f, which was calculated from the x-ray diffraction data.

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Hepatitis E Virus Methyltransferase Inhibits Type I Interferon Induction by Targeting RIG-I

  • Kang, Sangmin;Choi, Changsun;Choi, Insoo;Han, Kwi-Nam;Roh, Seong Woon;Choi, Jongsun;Kwon, Joseph;Park, Mi-Kyung;Kim, Seong-Jun;Myoung, Jinjong
    • Journal of Microbiology and Biotechnology
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    • v.28 no.9
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    • pp.1554-1562
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    • 2018
  • The type I interferons (IFNs) play a vital role in activation of innate immunity in response to viral infection. Accordingly, viruses have evolved to employ various survival strategies to evade innate immune responses induced by type I IFNs. For example, hepatitis E virus (HEV) encoded papain-like cysteine protease (PCP) has been shown to inhibit IFN activation signaling by suppressing K63-linked de-ubiquitination of retinoic acid-inducible gene I (RIG-I) and TANK-binding kinase 1 (TBK1), thus effectively inhibiting down-stream activation of IFN signaling. In the present study, we demonstrated that HEV inhibits polyinosinic-polycytidylic acid (poly(I:C))-induced $IFN-{\beta}$ transcriptional induction. Moreover, by using reporter assay with individual HEV-encoded gene, we showed that HEV methyltransferase (MeT), a non-structural protein, significantly decreases RIG-I-induced $IFN-{\beta}$ induction and $NF-{\kappa}B$ signaling activities in a dose-dependent manner. Taken together, we report here that MeT, along with PCP, is responsible for the inhibition of RIG-I-induced activation of type I IFNs, expanding the list of HEV-encoded antagonists of the host innate immunity.

Safety and Antioxydative effects of Cuscuta chinensis Lam. in PC12 Cell (PC12 Cell에 대한 토사자(?絲子)의 안정성 및 항산화작용에 대한 연구)

  • Do, Yong-Ho;Kim, Dong-Il
    • The Journal of Korean Obstetrics and Gynecology
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    • v.19 no.3
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    • pp.121-134
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    • 2006
  • Purpose : Cuscuta chinensis Lam. is utilized extensively as important medicines for threatened abortion habitual abortion. However, objective data related to an embryo is not existed until now. Therefore, this study is focused to find out stability of Cuscuta chinensis Lam. about an embryo during pregnancy based on data related to stability of nerve cell and antioxydative effect by using neural cell line, PC 12 cell. Methods : Experimentation concerns cytotoxic effects and antioxydative effect through methods such as MTT ssay, western botting after abstracting an undiluted solution from domestic Cuscuta chinensis Lam. Results : 1. As a result of experimentation on MTT assay according to each magnification from Cuscuta chinensis Lam. extraction solution with different abstraction methods, cytotoxic effect is not observed to all extract except an undiluted solution which is abstracted from MeOH stiring. Also, an undiluted solution in stiring with MeOH could not confirm whether come from Cuscuta chinensis Lam. or not. 2. As a result of revelation of Bax and GSK-3${\beta}$ which is responsive to the first stage from general stress in order to observe antioxydative effects of Cuscuta chinensis Lam. revelation of Bax by Cuscuta chinensis Lam. appeared to decrease. Conclusion : Cytotoxic effects with Cuscuta chinensis Lam. about PC12 cell is not discovered and it assume that it would be anti apoptotic effect by ROS as Bax and GSK-3${\beta}$ inviable effect. In the future, this study could be used as basic data for additional research on Cuscuta chinensis Lam. and effect and stability of complicated prescriptions for keeping pregnancy.

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Anti-inflammtory effects of the MeOH extract of Petiolus Nelumbinis (LPS로 활성화된 RAW 264.7 cell에서 하경(荷梗)의 염증매개물질 억제효과)

  • Lee, Won-Uk;Jo, Mi-Jeong;Park, Sang-Mi;Jung, Ji-Yun;Kim, Sang-Chan
    • Herbal Formula Science
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    • v.17 no.1
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    • pp.175-185
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    • 2009
  • Petiolus Nelumbinis, branches of lotus leaf or lotus flower is a traditional oriental herbal medicine widely used for treating a superheat or disorder of qi flow. Although there are many clinical results and literature study, it has been rarely conducted to evaluate the immuno-biological activity. The present study was conducted to examine the anti-inflammatory effects of PNM (Petiolus Nelumbinis MeOH extract) in vitro. To determine cytotoxic concentration of PNM, the cells were treated with PNM for 24 h after LPS addition, and the cell viability was tested by MTT assay. Both of dosages (30 and 100 ${\mu}g/ml$) of PNM had no cytotoxicity. In these concentrations, PNM significantly reduced the elevated levels of NO and $PGE_2$ by LPS. These inhibitory effects of PNM were due to the reduced expressions of iNOS and COX-2 protein. TNF-$\alpha$, IL-1$\beta$ and IL-6 are frequently encountered pro-inflammatory cytokines, and LPS plays a key role in inducing to the massive production of these cytokines. Thus, we next determined the levels of these cytokines. Although PNM had no significant inhibitory effect on the production of TNF-$\alpha$, the elevated levels of IL-1$\beta$ and IL-6 by LPS were dose-dependently reduced in PNM-treated groups. These results demonstrate that PNM has anti-inflammatory effects by inhibiting the production of proinflammatory cytokines, NO and $PGE_2$ in LPS-activated macrophage. Moreover, the reduction of NO and $PGE_2$ levels was due to the inhibition of iNOS and COX-2 protein expression by PNM.

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Seed extracts of a Bangladeshi medicinal plant Abrus precatorius L. show antifertility activity in female rats

  • Hannan, M.A.;Hossain, M.A.;Islam, M.T.
    • Advances in Traditional Medicine
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    • v.10 no.2
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    • pp.103-110
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    • 2010
  • The seed powder of Abrus precatorius L. has traditionally been used as oral contraceptive agent by the women in some rural areas in Bangladesh. The present study aimed to examine the antifertility activity of A. precatorius seed extracts in experimental female rats. Finely ground seeds were extracted with aqueous acetone followed by successive partitioning with n-hexane, ethyl acetate (EtOAc), methanol (MeOH) and water. Water suspended crude seed powder, organic fractions of acetone extract and a standard contraceptive drug ($Nordette^{(R)}28$) were separately administered orally to the female rats for 30 days. n-Hexane, EtOAc and MeOH solubles at the doses of 2, 4 and 6 mg/rat/day, respectively and crude seed powder at 100 mg/rat/day exhibited 100% antifertility activity with lowest levels of serum luteinizing hormone (LH), follicle stimulating hormone (FSH) and $17{\beta}$-estradiol. Histological study of ovary and uterus of these rats exhibited reduced number of developing follicles and increased number of atretic follicles in the ovary, and fewer uterine glands with shrunken morphology, reduced endometrial height, poor vascularity and compact stroma in uterus. However, the activities of serum glutamate oxaloacetate transaminase and serum glutamate pyruvate transaminase and the body weight of the rats remained almost unaffected in all the seed extract treated rats compared to control. These results suggest that A. precatorius seed extracts reduced the levels of serum FSH, LH and $17{\beta}$-estradiol probably by affecting hypothalamic-pituitary-gonadal axis. The reduced levels of these hormones might have affected the oestrous cycle, follicular development, and subsequently the establishment of pregnancy in treated rats.

Eugenol Inhibits ATP-induced P2X Currents in Trigeminal Ganglion Neurons

  • Li, Hai Ying;Lee, Byung-Ky;Kim, Joong-Soo;Jung, Sung-Jun;Oh, Seog-Bae
    • The Korean Journal of Physiology and Pharmacology
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    • v.12 no.6
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    • pp.315-321
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    • 2008
  • Eugenol is widely used in dentistry to relieve pain. We have recently demonstrated voltage-gated $Na^+$ and $Ca^{2+}$ channels as molecular targets for its analgesic effects, and hypothesized that eugenol acts on $P2X_3$, another pain receptor expressed in trigeminal ganglion (TG), and tested the effects of eugenol by whole-cell patch clamp and $Ca^{2+}$ imaging techniques. In the present study, we investigated whether eugenol would modulate 5'-triphosphate (ATP)-induced currents in rat TG neurons and $P2X_3$-expressing human embryonic kidney (HEK) 293 cells. ATP-induced currents in TG neurons exhibited electrophysiological properties similar to those in HEK293 cells, and both ATP- and $\alpha$, $\beta$-meATP-induced currents in TG neurons were effectively blocked by TNP-ATP, suggesting that $P2X_3$ mediates the majority of ATP-induced currents in TG neurons. Eugenol inhibited ATP-induced currents in both capsaicin-sensitive and capsaicin-insensitive TG neurons with similar extent, and most ATP-responsive neurons were IB4-positive. Eugenol inhibited not only $Ca^{2+}$ transients evoked by $\alpha$, $\beta$-meATP, the selective $P2X_3$ agonist, in capsaicin-insensitive TG neurons, but also ATP-induced currents in $P2X_3$-expressing HEK293 cells without co-expression of transient receptor potential vanilloid 1 (TRPV1). We suggest, therefore, that eugenol inhibits $P2X_3$ currents in a TRPV1-independent manner, which contributes to its analgesic effect.

Effect of Ca2+ on contractile responses induced by perivascular nerve stimulation in isolated coronary artery of pig

  • Hong, Yong-geun;Shim, Cheol-soo;Kim, Joo-heon
    • Korean Journal of Veterinary Research
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    • v.39 no.4
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    • pp.702-709
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    • 1999
  • The present study was performed to elucidate the effects of extracellular $Ca^{2+}$ on contractile responses in isolated porcine coronary artery ring using by perivascular nerve stimulation (PNS). Especially, the study was focused on the source of $Ca^{2+}$ on $P_{2X}$-purinoceptor mediated muscle contraction which one of $P_2$-purinoceptor subtypes. The following results can be drawn from these studies : 1. The phasic contractions induced by PNS were inhibited with muscarinic receptor antagonist, atropine ($10^{-6}M$). 2. The phasic contractions induced by PNS were significantly inhibited by sequential treatment with atropine and adrenergic neural blocker, guanethidine ($10^{-6}M$). 3. The phasic contractions induced by PNS were inhibited with $P_{2X}$-purinoceptor desensitization by repetitive application of $\alpha$,$\beta$-Me ATP ($10^{-4}M$). 4. The phasic contractions induced by PNS were so weakened in calcium-free medium. 5. The phasic contractions induced by PNS were inhibited with calcium channel blocker, verapamil ($10^{-6}{\sim}5{\times}10^{-6}M$). 6. The phasic contractions induced by PNS on pretreated with verapamil ($10^{-6}{\sim}5{\times}10^{-6}M$) were not changed by $\alpha$,$\beta$-Me ATP ($10^{-4}M$). These results demonstrate that the neurogenic phasic contractions induced by PNS are due to adrenergic-, cholinergic- and $P_{2X}$-purinergic receptors and the origin of $Ca^{2+}$ on $P_{2X}$-purinoceptor mediated muscle contraction is extracellular $Ca^{2+}$ through plasmalemmal $Ca^{2+}$ channels.

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