• Title/Summary/Keyword: Cortex-M3

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Inhibition of Drug-metabolizing Enzyme and Drug Transporter by Major Components of Phellodendri cortex (황백의 주요 구성 화합물에 의한 약물대사효소 및 약물수송단백 저해능 평가)

  • Ku, Hei-Young;Kim, Hyunmi;Shon, Ji-Hong;Liu, Kwang-Hyeon
    • Journal of Marine Bioscience and Biotechnology
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    • v.1 no.3
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    • pp.213-217
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    • 2006
  • We evaluated the potential of major components of Phellodendri cortex to inhibit the activities of CYP2D6 and p-glycoprotein. The abilities of berberine, palmatine, limonin, and rutaecarpine to inhibit CYP2D6-mediated dextromethorphan O-demethylation and calcein AM accumulation were tested using human liver microsomes and L-MDR1 cell, respectively. Berberine strongly inhibited CYP2D6 isoform activity, whereas limonin and reuaecarpine did not. The $IC_{50}$ value of berberine was reduced after preincubation with microsomes in the presence of NADPH generating system, suggesting that berberine is a mechanism based inhibitor. In addition, all chemicals tested, didn't show inhibitory effect on p-glycoprotein activity. These results suggest that berberine has potential to inhibit CYP2D6 activity in vitro. Therefore, in vivo studies investigating the interactions between berberine and CYP2D6 substrates are necessary to determine whether inhibition of CYP2D6 activity by berberine is clinically relevant.

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Insulin-like and Insulin Sensitizing Effects of Modified Anti-diabetic Remedies in 3T3-L1 Fibroblasts (소갈 치료 처방 가감이 3T3-L1 Adipocytes에서 인슐린 유사성과 인슐린 민감성에 미치는 영향)

  • Park Sun Min;Choi Mi Kyung;Jun Dong Wha;Choi Soo Bong;Park Seong Kyu;Lee Mi Young;Kim Ho Kyoung;Hwang Young Hee;Ko Byoung-Seob
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.18 no.2
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    • pp.451-456
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    • 2004
  • Based on the data from our previous studies, four new diabetic remedies were composed with the addition of Coicis Semen into Okchun-san (OCH), Commelinae Herba into Gangsim-tang (GST) , Scrophulariae Radix into Sunki-san (SKS), and Erythrinae Cortex into Yukmijihuang-hwan (YMG). The water extracts of these new remedies were treated in 3T3-L1 fibroblasts and adipocytes in order to investigate insulin-like substances and insulin sensitizers, respectively. With and without differentiation inducers, unmodified SKS (SKS-O) treatment induced 3T3-L1 fibroblasts into adipocytes more than the control. However, without inducers, YMG treatment, but not SKS, induced the differentiation more than the control among modified remedies. Without inducers, SKS, OCH as well as YMG increased the induction of differentiation from 3T3-L1 fibroblasts into adipocytes, compared to the control. The treatment of OCH and YMG with 1 ng/mL insulin increased glucose uptake much more than only insulin 1 ng/mL treatment. Thus, OCH and YMG contained increased insulin actions. In conclusions, the modified remedies, OCH and YMG, contained insulin-like substances and insulin sensitizers, and they can be improved the hypoglycemic effects.

Protection by Paeonol on Cytotoxicity of Cultured Rat Hepatocytes Exposed to Br-A23187

  • Bae, Ki-Hwan;Kim, Young-Ho;Oh, Ki-Wan
    • Biomolecules & Therapeutics
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    • v.11 no.3
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    • pp.174-177
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    • 2003
  • The present experiment was performed to investigate the protective effects of paeonol isolated from Moutan Cortex Radicis on primary cultured rat hepatocytes exposed to Br-A23187 ($Ca^{2+}$ ionophore). Br-A23187 is frequently used as a model of cell killing as inducing both necrotic and apoptotic cell death. Hepatocytes were isolated by collagenase perfusion from livers of fasted male Sprague Dawley rats and cultured overnight. Cell viability was determined by propidium iodide using fluorocytometry in Krebs-Ringer-HEPES buffer at pH 7.4. In addition, intracellular calcium was measured by excitation at 340 and 380 nm and emission at 505 nm using a luminescence spectrophotometer. Paeonol (20-100 ${\mu}M$) inhibited cell killing induced by 10 ${\mu}M$ Br-A23187, in a dose-dependent manner. Paeonol also reduced increased intracellular calcium level when hepatocytes were exposed to Br-A23187. Therefore, the present results suggest that paeonol protects the hepatocytotoxicity induced by Br-A23187, via inhibiting the influx of calcium into into rat hepatocytes.

Protective Effect of N-Acetylcysteine on Progression of Adriamycin-induced Nephyopathy

  • Han, Sang-Woong;Kim, Ho-Jung;Paik, Seung-Sam;Lee, Jong-Un
    • The Korean Journal of Physiology and Pharmacology
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    • v.9 no.3
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    • pp.159-164
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    • 2005
  • Effects of antioxidants on the established nephropathy were investigated. The experimental nephropathy was induced in rats by intravenous injection of adriamycin (2 mg/kg). Six weeks later, when proteinuria was apparent, the rats were supplemented with N-acetylcysteine (NAC, 1 g/kg/day) in drinking water for additional 6 weeks. Glomerulosclerosis score and tubulointerstitial injury index were determined by light microscopy. Expression of transforming growth factor (TGF) ${\beta}1$ and laminin ${\beta}1$ was determined in the renal cortex by reverse transcription-polymerase chain reaction, Western blotting, immunohistochemistry, and immunogold electron microscopy. The adriamycin-induced proteinuria as well as the glomerulosclerosis and tubulointerstitial injury was ameliorated by the treatment with NAC. Adriamycin increased the expression of TGF ${\beta}1$ mRNA and protein, which was ameliorated by NAC. Although the expression of laminin ${\beta}1$ mRNA was increased, adriamycin did not significantly alter that of its protein. These results indicate that antioxidants ameliorate the established nephropathy in association with normalization of overexpressed TGF ${\beta}1$.

Eugenol suppresses inducible cyclooxygenase-2(COX-2) expressionin lipopolysaccharide-stimulated mouse macrophage cells.

  • Kim, Sun-Suk;Oh, O-Jin;Min, Hye-Young;Lee, Youngm-Kim;Lee, Sang-Kook
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2001.11a
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    • pp.86-86
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    • 2001
  • Based on the potential inhibitors of cyclooxygenase-2 (COX-2) as anti-inflammatory or cancer chemopreventive agents, we have evaluated the active principles of COX-2 inhibition from natural products. The methanol extract of the cortex of Eugenia caryoplyllata (Myrtaceae) showed the potent inhibition of prostaglandin E$_2$(PGE$_2$) production in lipopolysaccharide (LPS)-activated RAW 264.7 cells (98.3% inhibition at the test concentration of 10 $\mu\textrm{g}$/$m\ell$) Further, hexane-soluble layer was the most active partition compared to ethyl acetate, n-butanol, and water -soluble parts. By bioassay-guided fractionation of hexane-soluble layer, eugenol was isolated and exhibited a significant suppression of PGE$_2$ production (IC$\_$50/=0.06$\mu\textrm{g}$/$m\ell$). In addition, eugenol suppressed the COX-2 gene expression in LPS-stimulated mouse macrop-hage cells. Therfore, eugenol might be a plausible lead candidate for further developing the COX-2 inhibitor as an anti-inflammatory or cancer chemopreventive agent.

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Effect of Dietary Fatty Acid and Vitamin E Supplementation in Antioxidant Systmes of the Second Generation Rat Brain Sections (식이지방산 조성 및 비타민 E의 보충이 제 2 세대 흰 쥐 뇌조직의 항산화 체계에 미치는 영향)

  • 황혜진;엄영숙;정은정;김수연;이양자
    • Journal of Nutrition and Health
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    • v.34 no.1
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    • pp.14-22
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    • 2001
  • In this study, we examined the effects of dietary fatty acids and vitamin E supplementation on antioxidant systems in the rat brain regions. The Sprague Dawley rats were fed the experimental diets 3-4 wks prior to the conception. Experimental diet consisted of 10% fat(wt/wt) which were safflower oil(SO, poor in $\omega$3 fatty acids), mixed oil(MO, P/M/S ratio=1.03:1.45:1,$\omega$6/$\omega$3 ratio=6.3) and mixed oil supplemented with vitamin E(ME:MO+500mg vitamin E/kg diet). At 3 and 9 weeks of age of the newborn rats, frontal cortex(FC), corpus striatum(CS), hippocampus(H) cerebellum(CB) were dissected out from the whole brain. Activities of glutathione peroxidase(GSH-P(sub)x, superoxide dismutase(SOD) concentrations of malondialdehyde(MDA) were mesaured. Dietary fatty acids were not effective in antioxidative system for rat brain. However, when vitamin E was supplemented to the diet(ME), the activities of GSH-P(suh)x tended to increase in comparison to MO group. Therefore, the activites of GSH-P(suh)x of FC and H at the age of 3 weeks showed significant differences(p<0.05). The activities of Total-SOD tended to decrease in ME group compared to MO group. There were significant differences(p<0.05) in FC and CS at the age of 3 weeks. The activities of Mn-SOD tended to increase and Cu, Zn-SOD tended to decrease when vitamin E was supplemented. The activity levels of antioxidative enzymes at the age of 3 weeks and 9 weeks were similar. This suggested that the activity level of antioxidative enzymes reached to the adult level at the age of 3 weeks which is the end point of lactation period. The concentrations of MDA were not altered by experimental diets. When the activities of antioxidant enzymes were compared, the activities of antioxidant enzymes were the lowest in H and FC. In conclusion, the antioxidative system were not altered by dietary fatty acid at the age of 3 weeks and 9 weeks, but the supplementation of vitamin E altered the antioxidative systems. Therefore, these findings should be considered comprehensively in scope of the balance of various antioxidative systems and their interactions(Korean J Nutrition 34(1):14-22, 2001)

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Characterization of Ionic Currents in Human Neural Stem Cells

  • Lim, Chae-Gil;Kim, Sung-Soo;SuhKim, Hae-Young;Lee, Young-Don;Ahn, Seung-Cheol
    • The Korean Journal of Physiology and Pharmacology
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    • v.12 no.4
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    • pp.131-135
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    • 2008
  • The profile of membrane currents was investigated in differentiated neuronal cells derived from human neural stem cells (hNSCs) that were obtained from aborted fetal cortex. Whole-cell voltage clamp recording revealed at least 4 different currents: a tetrodotoxin (TTX)-sensitive $Na^+$ current, a hyperpolarization-activated inward current, and A-type and delayed rectifier-type $K^+$ outward currents. Both types of $K^+$ outward currents were blocked by either 5 mM tetraethylammonium (TEA) or 5 mM 4-aminopyridine (4-AP). The hyperpolarization-activated current resembled the classical $K^+$ inward current in that it exhibited a voltage-dependent block in the presence of external $Ba^{2+}$ (30 ${\mu}$M) or $Cs^+$ (3${\mu}$M). However, the reversal potentials did not match well with the predicted $K^+$ equilibrium potentials, suggesting that it was not a classical $K^+$ inward rectifier current. The other $Na^+$ inward current resembled the classical $Na^+$ current observed in pharmacological studies. The expression of these channels may contribute to generation and repolarization of action potential and might be regarded as functional markers for hNSCs-derived neurons.

Electron Microscopic Studies on the Morphological Differences of Ethnic Hair (인종 모발의 형태학적 차이에 관한 전자현미경적 연구)

  • Lee, Gui-Young;Chang, Byung-Soo
    • Applied Microscopy
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    • v.38 no.3
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    • pp.265-273
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    • 2008
  • We investigated the morphological differences of the ethnic hairs using scanning electron microscopy and transmission electron microscopy, sampled from African, Asian and Caucasian women. Transverse section of African hair had a highly elliptical type whereas those of Asian and Caucasian hairs had circular and elliptical types, respectively. The diameter of African hair showed wide variations from 90 to 115 ${\mu}m$. The diameter of Asian hair was 100 ${\mu}m$ and Caucasian hair had a lesser diameter of 80 ${\mu}m$ on average. African hair were much more damaged in cuticle layer compared with Asian or Caucasian hairs. In particular, endocuticle of cuticle cell had a lot of holes in it, which resulted that it tends to be easily broken. Phaeomelanin in the cortex of Caucasian hair had a concentrically helical structure in it.

Effects of Baicalein on Neuroinflammation in Lipopolysaccharide-treated Mice (Baicalein이 Lipopolysaccharide에 의한 생쥐의 Neuroinflammation에 미치는 영향)

  • Ha, Gyung-Woon;Kim, Youn-Sub
    • The Korea Journal of Herbology
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    • v.28 no.2
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    • pp.93-101
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    • 2013
  • Objects : Baicalein is a major bioactive flavonoid component of Scutellaria baicalensis Georgi that shows a wide range of biological activities, including neuroprotections and anti-inflammatory actions. Hence it is a potential therapeutic material for the treatment of neuroinflammation. In this study, we investigated the modulatory effect of baicalein on neuroinflammation. Method : Pro-inflammatory cytokines (TNF-${\alpha}$, IL-$1{\beta}$ and IL-6 mRNA), COX-2 mRNA expression and microglial activation in the brain tissue is induced by systemic lipopolysaccharide (LPS) treatment in C57BL/6 mice. Baicalein was treated orally with 10, 20, and 30 mg/kg 1 hour prior to the LPS (3 mg/kg, i.p.) injection. TNF-${\alpha}$, IL-$1{\beta}$, IL-6 and COX-2 mRNA expression in the brain tissue was measured by the quantitative real-time polymerase chain reaction(PCR) method. Iba1 expression in the brain was measured by western blotting method. Microglia was observed with immunohistochemistry. Results : Baicalein 30 mg/kg significantly attenuated the expression of TNF-${\alpha}$, IL-$1{\beta}$, IL-6 and COX-2 mRNA in the brain tissue. Baicalein 20 mg/kg significantly attenuated the expression of IL-6 mRNA in the brain tissue. Baicalein 30 mg/kg significantly attenuated the expression of Iba1 protein expression in the brain tissue. Baicalein 30 mg/kg significantly decreased the number and cell size of microglia in the cerebral cortex and hypothalamic region and the area percentage of Iba1-expressed microglia in the hippocampus. Conclusion : These results demonstrated that baicalein attenuates LPS induced neuroinflammation in the mice via reduction of pro-inflammatory cytokines (TNF-${\alpha}$, IL-$1{\beta}$, IL-6), COX-2 mRNA expression and microglial activation.

An Experimental Study on the Effect of Chengsimyeonjatang-gagam Extracts on the ADHD Animal Model (ADHD 동물모델에서 가감청심연자탕의 효과에 관한 실험연구)

  • Oh, Young-je;Liu, Quan Feng;Kim, Man-gi;Hong, Min-ho;Kim, Geun-woo;Koo, Byung-soo
    • Journal of Oriental Neuropsychiatry
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    • v.31 no.3
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    • pp.149-156
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    • 2020
  • Objectives: The purpose of this study was to experimentally assess the effects of Chengsimyeonjatanggagam extracts in the animal model regarding ADHD related symptoms and indicators. Methods: The experimental group was classified into the normal group (WKY rat) in 7, the control group (SHR rat) in 7, the low-concentration group of herbal medicines (SHR rat) in 7, and the high-concentration group of herbal medicines (SHR rat) in 7 by random sampling. The open field test was conducted three times on the 7th, 14th, and 21st days during the oral medication. After that, Y-maze test, intestinal permeability verification (L/M ratio), and Western blotting (CDK expression in the cerebral cortex) were performed in sequence. Results: The Chengsimyeonjatang-gagam extracts reduced the activity distance in the SHR rat at 21 days in the low and high concentration groups by the open field test. It also reduced the cross-action rate in the low and high concentration groups by the Y-maze test. And the low concentration group showed 52.3% decrease in the L/M ratio compared to the SHR group. Finally, the CDK5 protein significantly increased in the low and high concentration groups. Conclusions: This study suggests that the Chengsimyeonjatang-gagam extracts have potential to be used for the treatment of ADHD.