• Title/Summary/Keyword: Inhibiting Effect

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Inhibition of Dicarboxylate Transport by p-chloromercuribenzoic Acid (PCMB) in Plasma Membrane Vesicles of Rabbit Proximal Tubule

  • Kim, Yong-Keun;Kim, Tae-In;Jung, Jin-Sup;Lee, Sang-Ho
    • The Korean Journal of Physiology
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    • v.25 no.2
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    • pp.179-188
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    • 1991
  • Effect of a sulfhydryl reagent, p-chloromercuribenzoic acid (PCMB), on the transport of succinate was studied in brush border (BBMV) and basolateral (BLMV) membrane vesicles isolated from rabbit renal cortex. PCMB induced an irreversible inhibition of the $Na^+-dependent$ succinate uptake in a dose-dependent manner with $IC_{50}$ of 55 and $65\;{\mu}M$ in BBMV and BLMV, respectively. The inhibitory effect of PCMB was prevented by a pretreatment of vesicles with dithiothreitol. PCMB did not increase $Na^+$ permeability at concentrations inhibiting succinate uptake. The PCMB inhibition of succinate uptake was due to a change in Vmax, but not in Km. When membrane vesicles were pretreated with PCMB in the presence of unlabelled succinate, the inhibitory effect was significantly reduced. In both BBMV and BLMV, succinate uptake was inhibited by various sulfhydryl reagents with the inhibitory potency of following order: $HgCl_2$>DTNB>PCMBS>PCMB. These results suggest that sulfhydryl groups are essential for dicarboxylate transport and that they may be located at or near substrate binding sites of the transporters in renal brush border and basolateral membranes.

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Effects of Flavonoids and a-Tocopherol on the Oxidation of n-3 Polyunsaturated Fatty Acids -1. Inhibition of Fish Oil Oxidation by Heating and During Storage- (n-3고도 불포화 지방산의 산화억제에 미치는 플라보노이드와 a-토코페롤의 효과 -1. 정제어유의 가열 및 저장 중 산화억제 효과-)

  • JUNG Dong-Yun;KWON Mi-Na;HONG Jeong-Hwa;BYUN Dae-Seok
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.27 no.2
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    • pp.155-165
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    • 1994
  • To evaluate the antioxidant effect of flavonoids and a-tocopherol on purified fish oil(up to $40\%$ of n-3 polyunsaturated fatty acids), lipid peroxidation, and fatty acids content during storage and upon heating were determined. The potential of these compounds for inhibiting and delaying both oxidation and lipoxygenase processes was also evaluated. The oxidation of fish oil was effectively inhibited by flavonoids and a-tocopherol. The antioxidizing effect of these compounds increased in proportion to their concentration. The addition of a-tocopherol and catechin-a-tocopherol mixture were prolonged induction period of lipid oxidation by 3.5 to 4 times. All other flavonoids also shown more than twice the prolonging effect. Lipoxygenase activity was decreased by catechin and a-tocopherol effectively.

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Effects of Atractylodis Rhizoma Alba extract on collagen-induced arthritis in mice (백출(白朮)의 콜라겐 유도 관절염 마우스에서의 관절염 개선 효과 연구)

  • Kim, Song-Hee;Park, Yong-Ki
    • The Korea Journal of Herbology
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    • v.27 no.3
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    • pp.1-6
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    • 2012
  • Objectives : The present study was undertaken to evaluate whether Atractylodis Rhizoma Alba ethanol (ARA-E) extract, which is the pericarp of $Atractylodes$ $japonica$ Koidz. has an effect on collagen-induced arthritis (CIA) in mice. Methods : Male DBA/1J mice were induced by intradermal injection of bovine collagen-II in Freund's incomplete adjuvant (IFA). The CIA mice in the onset of arthritis were treated daily with oral administration of ARA-E extract at dose of 50 mg/kg/bw for 28 days. Arthritis index, histopathological changes and the levels of anti-type II collagen (CII) IgG and inflammatory cytokine, TNF-${\alpha}$ in sera of mice were measured to evaluate the antiarthritic effect of ARA-E. Results : ARA-E extract significantly decreased the arthritic scores and inhibited pathological changes of knee joint tissues in CIA mice. ARA-E extract also significantly decreased the serum levels of anti-CII IgG and TNF-${\alpha}$ in CIA mice. These results indicate that ARA-E extract may effectively prevent arthritic damages in CIA mice, at least partially, by inhibiting the production of autoantibodies and inflammatory cytokine. Conclusions : This studies suggest that ARA-E has a therapeutic potential in inflammatory joint diseases such as rheumatoid arthritis.

Anti-inflammatory Effect of Red Ginseng through Regulation of MAPK in Lipopolysaccharide-stimulated RAW264.7 (Lipopolysaccharide로 유도된 RAW264.7 세포에서 MAPK에 의한 홍삼추출물의 항염증 효과)

  • Shin, Ji-Su;Kim, Jong-Myoung;An, Won-Gun
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.26 no.3
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    • pp.293-300
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    • 2012
  • Inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) are important inflammatory mediators implicated in pathogenesis of inflammation and certain types of human cancers. The present study was designed to determine whether Red Ginseng (RG) could modulate $I{\kappa}B$-kinase, iNOS and COX-2 gene expression and immune responses in RAW 264.7 macrophages stimulated with lipopolysaccharide (LPS). RG extract suppressed the expression of LPS-induced $I{\kappa}B$, iNOS, COX-2, and immune responses in a dose-dependent manner. It also showed an anti-inflammatory effect by inhibiting NF-${\kappa}B$ immune response induced by LPS treatment. Inhibitory effect of RG on LPS-induced inflammation was mediated by suppressed phosphorylation of ERK, JNK and p38 through the regulation of the mitogen-activated protein kinase (MAPK) pathway leading to a decreased production of NO, iNOS, COX-2 and NF-${\kappa}B$. The results implied the role of RG as an inflammation regulator and its possible application for curing inflammatory diseases.

Anti-oxidative Effect of Ginsenoside $Rb_1$ on the HCI.Ethanol-Induced Gastric Tissue in Rats (흰쥐의 염산.에탄올 유발 위염 위조직에서 ginsenoside $Rb_1$의 항산화 효과)

  • Hyun, Jin-Ee;Kim, Yeong-Shik;Jeong, Choon-Sik
    • Korean Journal of Pharmacognosy
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    • v.33 no.3 s.130
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    • pp.252-256
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    • 2002
  • In the previous study, we demonstrated that ginsenoside $Rb_1$ isolated from the butanol fraction of the head of Panax ginseng had significant gastroprotective activity on gastritis and gastric ulcer models in rats. It has been well established that drugs to have capacity of scavenging or inhibiting the generation of reactive oxygen radicals prevent the gastric mucosal injury. Ginsenoside $Rb_1$ was tested on HCl ethanol-induced gastritis in rats, DPPH-induced free radical scavenging effect, MDA assay, GSH activity, and SOD activity in gastric tissue. It showed significant inhibition in HCl ethanol-induced gastritis, and al~o significantly increase of GSH activated SOD. We speculate that the protective effect of ginsenoside $Rb_1$ against HCl ethanol-induced gastric mucosal damage is originated from the increase of GSH and the activation of SOD.

Anti-inflammatory effect of various solvent extract from Atractylodes japonica on Lipopolysaccharide-induced Inflammation in BV2 cells. (창출 추출물의 BV2 cell 소염작용에 관한 실험적 연구)

  • Hur, Inn-Hee;Sim, Sung-Yong;Kim, Kyung-Jun
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.20 no.2 s.33
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    • pp.36-46
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    • 2007
  • Objective : In this study, the effect of Atractylodes japonica against LPS induced inflammation in mouse microglia BV2 cells was investigated. Method : Microglia BV2 Cells viability was determined using the MTT assay. We used water, ethanol extract from Atractylodes japonica and studied on the anti-inflammatory effect of lipopolysaccharide-induced inflammation using reverse transcription polymerase chain reaction (RT-PCR), western blot, and nitric oxide detection on mouse microglia BV2 cells. Result : The MTT assay revealed that it's extract has no significant cytotoxicity in the microglia BV2 cell. Various solvent extract from Atractylodes japonica inhibited nitrite production, iNOS protein and mRNA expression levels. And also it's extracts significantly reduced lipopolysaccharide-induced COX-2 activation in RT-PCR and western blot in lipopolysaccharide-induced microglia BV2 cells Conclusion : In this study, it's extracts was shown to suppress NO production by inhibiting iNOS expression and COX-2 activity. With this effects of anti-inflammation, we suggests that, it's extracts may be a useful candidate for the development of a drug on the related inflammatory diseases in brain.

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강원도산 참당귀와 일본산 일당귀의 생리 활성 성분 탐색

  • Ham, Moon-Sun;Kim, Seung-Su;Hong, Jong-Su;Lee, Jin-Ha;Chung, Eul-Kwon;Park, Young-Shik;Lee, Hyeon-Yong
    • Microbiology and Biotechnology Letters
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    • v.24 no.5
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    • pp.624-629
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    • 1996
  • The ethanol extracts from Angelica gigas Nakai and Angelica acutiloba Kitagawa were fractionated to diethyl ether and aqueous partitions. Both partitions had strong antimutagenic effect on the MNNG (N-methyl-N-nitro-N-nitrosoguanidine) by Ames mutagenicity test. Diethyl ether fractions exhibited the greatest antimutagenic effect suppressing the mutagenicity of MNNG with inhibition of 78-80%. The ethanol extracts from both species showed the inhibitory effect on the growth of several human cancer cell lines. Especially, the diethyl ether fraction from ethanol extracts was most effective on human hepatocellular carcinoma cells, inhibiting 90-95% of cell growth. However, the aqueous fractions had least inhibition activity on many cancer cells. There was little cytotoxicity on human normal liver cell by ethanol extracts. Diethyl ether fraction from Angelica gigas Nakai ethanol extract had cytotoxicity less than 20% on human normal liver cells, compared with that from Angelica acutiloba Kitagawa ethanol exract. The adding of 0.5 (g/l) of diethyl ether fractions of Angelica gigas Nakai or Angelica acutiloba Kitagawa increased immune activity by enhacing human B and T cells up to three to four times. It was proven that diethyl ether fraction (0.7 g/1) from Angelica gigas Nakai could control blood pressure by suppressing angiotensin converting enzyme activity up to 98%. From TLC, it was appeared that both of diethyl ether partitions had umbelliferon, known to one of active substances from Angelica gigas Nakai and Angelica acutiloba Kitagawa.

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Tubeimoside-1 suppresses breast cancer metastasis through downregulation of CXCR4 chemokine receptor expression

  • Peng, Yaojin;Zhong, Yan;Li, Gao
    • BMB Reports
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    • v.49 no.9
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    • pp.502-507
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    • 2016
  • To examine the effect of TBMS1on breast cancer metastasis, and investigate the potential mechanism by which Tubeimoside-1 (TBMS1) inhibits the CXCR4 expression in breast cancer cells. The expression of CXCR4 in breast cancer cell lines was determined by immunoblotting and real-time PCR. The effect of TBMS1 on NF-κB binding activity was evaluated by EMSA assay and ChIP analysis. Cell proliferation and invasion were analyzed by MTT assay and transwell invasion assay, respectively. The effect of TBMS1 on breast cancer metastasis was further evaluated in a metastasis model of nude mice. TBMS1 suppressed the expression of CXCR4 through inhibition of NF-κB binding activity. TBMS1 inhibited CXCL12-induced invasion in breast cancer cells, while ectopic expression of CXCR4 abolished the inhibitive activity of TBMS1. TBMS1 suppressed breast cancer metastasis in the metastatic model of nude mice. TBMS1 suppressed the CXCR4-mediated metastasis of breast cancer by inhibiting NF-κB binding activity.

Antiviral Effect of Amphotericin B on Japanese Encephalitis Virus Replication

  • Kim, Hun;Kim, Seong-Jun;Park, Sue-Nie;Oh, Jong-Won
    • Journal of Microbiology and Biotechnology
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    • v.14 no.1
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    • pp.121-127
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    • 2004
  • Amphotericin B (AmB), an amphipathic polyene macrolide, is an antifungal drug produced by Streptomyces nodosus. Recently, AmB has been shown to exert antiviral activity against rubella virus and human immunodeficiency virus by different mechanisms. In this study, we evaluated the antiviral effect of AmB against Japanese encephalitis virus (JEV) and investigated which step of the viral life cycle was inhibited by AmB to understand the mechanism of antiviral action of AmB. AmB reduced both plaque size and number in the infected cells in a dose-dependent manner. In addition, a 200-fold reduction of infectious virus titer was observed by treatment of infected cells with $5\mug/ml$ of AmB. AmB acted at the post virus-infection step, but not during adsorption of virus to host cells. Western blot analysis revealed that the accumulated level of JEV envelope protein dramatically decreased in the infected cells by treatment with $5-10\mug/ml$ of AmB. Our results indicate that AmB inhibits the replication of JEV at the postinfection step by interfering with viral replication and/or by inhibiting the synthesis of viral proteins.

Polyacetylene Compound from Cirsium japonicum var. ussuriense Inhibits the LPS-Induced Inflammatory Reaction via Suppression of NF-κB Activity in RAW 264.7 Cells

  • Kang, Tae-Jin;Moon, Jung-Sun;Lee, Sook-Yeon;Yim, Dongs-Sool
    • Biomolecules & Therapeutics
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    • v.19 no.1
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    • pp.97-101
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    • 2011
  • Cirsium japonicum var. ussuriense is known to have a variety of biological activities, including anti-inflammatory, analgesic activity and antipyretic activity. In this study we investigated the role of polyacetylene compound, 1-Heptadecene-11, 13-diyne-8, 9, 10-triol (PA) from the root of Cirsium japonicum var. ussuriense as an immune-modulator. PA was evaluated as inhibitors of some macrophage functions involved in the inflammatory process. We tested the effect of PA on the production of pro-inflammatory cytokines, interleukin-1beta (IL-$1{\beta}$) and tumor necrosis factor-alpha (TNF-$\alpha$), and nitric oxide (NO) in murine macrophage cell line, RAW264.7. There was no effect on cytokine production of macrophages by PA itself. However, PA inhibited lipopolysaccharide (LPS)-induced IL-$1{\beta}$ and TNF-$\alpha$ production by macrophages at a dose dependent manner. PA also suppressed the NO production of macrophages by LPS. LPS-induced NF-${\kappa}B$ activity was decreased by treatment of PA. Therefore, these results suggest that PA has anti-inflammatory effect by inhibiting the NF-${\kappa}B$ activation.