• Title/Summary/Keyword: Chemical-induced inhibition

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The Interaction of Volatile Chemicals and Phytohormones on Seed Germination and Seedling Growth of Lettuce (상치의 발아와 유묘생장에 미치는 휘발성 화학물질과 식물호르몬의 상호작용)

  • 윤경원;길봉섭
    • The Korean Journal of Ecology
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    • v.20 no.4
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    • pp.233-238
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    • 1997
  • To evaluate allelopathic effect of volatile chemicals and phytohormones, seed germination and seedling growth test of Lactuca sativa have performed in laboratory experiments. Among used chemicals terpienen-4-ol was the most inhibitory to seed germination of lettuce. ABA and GA inhibited seed germination at $5{\times}10^{-6}M$ concentration but promoted germination at $2.5{\times}10^{-5}M$ and $5{\times}10^{-5}M$. ABA and GA alleviated volatile chemical-induced inhibition of seed germination and seedling elongation of lettuce.

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Poly(ADP-ribosyl)ation of p53 Contributes to TPEN-Induced Neuronal Apoptosis

  • Kim, Hyun-Lim;Ra, Hana;Kim, Ki-Ryeong;Lee, Jeong-Min;Im, Hana;Kim, Yang-Hee
    • Molecules and Cells
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    • v.38 no.4
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    • pp.312-317
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    • 2015
  • Depletion of intracellular zinc by N,N,N,N-tetrakis(2-pyridylmethyl) ethylenediamine (TPEN) induces p53-mediated protein synthesis-dependent apoptosis of mouse cortical neurons. Here, we examined the requirement for poly(ADP-ribose) polymerase (PARP)-1 as an upstream regulator of p53 in zinc depletion-induced neuronal apoptosis. First, we found that chemical inhibition or genetic deletion of PARP-1 markedly attenuated TPEN-induced apoptosis of cultured mouse cortical neurons. Poly(ADP-ribosyl)ation of p53 occurred starting 1 h after TPEN treatment. Suggesting the critical role of PARP-1, the TPEN-induced increase of stability and activity of p53 as well as poly(ADP-ribosyl)ation of p53 was almost completely blocked by PARP inhibition. Consistent with this, the induction of downstream pro-apoptotic proteins PUMA and NOXA was noticeably reduced by chemical inhibitors or genetic deletion of PARP-1. TPEN-induced cytochrome C release into the cytosol and caspase-3 activation were also blocked by inhibition of PARP-1. Taken together, these findings indicate that PARP-1 is essential for TPEN-induced neuronal apoptosis.

Molecular Mechanisms of Inhibitory Activities of Tanshinones on Lipopolysaccharide-Induced Nitric Oxide Generation in RAW 264.7 Cells

  • Choi, Hong-Seok;Cho, Dong-Im;Choi, Hoo-Kyun;Im, Suhn-Yong;Ryu, Shi-Yong;Kim , Kyeong-Man
    • Archives of Pharmacal Research
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    • v.27 no.12
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    • pp.1233-1237
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    • 2004
  • The effects of four tanshinones isolated from Tanshen (the root of Salvia miltiorrhiza Bunge, Labiatae) were tested for their inhibition of nitric oxide production in macrophage cells, and the underlying molecular mechanisms studied. Of the four tanshinones used, 15, 16-dihydrotanshinone- I, tanshinone-IIA and cryptotanshinone, but not tanshinone I, demonstrated significant inhibition of the LPS-induced nitric oxide production in RAW 264.7 cells, with calculated $IC_{50}$ values of 5, 8, and 1.5 ${\mu}M$ , respectively. Tanshinones exerted inhibitory activities on the LPS-induced nitric oxide production only when applied concurrently with LPS, and tanshinone- IIA and cryptotanshinone were found to inhibit LPS-induced NF-$_KB$ mobilization and extracellular- regulated kinase (ERK) activation, respectively. These results suggest that tanshinones inhibit LPS-induced nitric oxide generation by interfering with the initial stage of LPS-induced expression of certain genes. NF-$_KB$ and ERK could be the molecular targets for tanshinones for the inhibition of LPS-induced nitric oxide production in macrophage cells.

LB30057 Inhibits Platelet Aggregation and Vascular Relaxation Induced by Thrombin

  • Jung, Byoung-In;Kang, a-Kyu-Tae;Bae, Ok-Nam;Lee, Moo-Yeol;Chung, Seung-Min;Lee, Sang-Koo;Kim, In-Chul;Chung, Jin-Ho
    • Archives of Pharmacal Research
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    • v.25 no.6
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    • pp.879-884
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    • 2002
  • Previous study showed that an amidrazonophenylalanine derivative, LB30057, which has high water solubility, inhibited the catalytic activity of thrombin potently by interaction with the active site of thrombin. In the current investigation, we examined whether LB30057 inhibited platelet aggregation and vascular relaxation induced by thrombin. Treatment with LB30057 to plateletrich plasma (PRP) isolated from human blood resulted in a concentration-dependent inhibition of thrombin-induced aggregation. Values for $IC_{50}$ and $IC_{100}$ were $54{\pm}4$ nM and $96{\pm}3$ nM, respectively. This inhibition was agonist (thrombin) specific, since $IC_{50}$ values for collagen and ADP were \much greater than those for thrombin. In addition, concentration-dependent inhibitory effects were observed on the serotonin secretion induced by thrombin in PRP. Consistent with these findings, thrombin-induced increase in cytosolic calcium levels was inhibited in a concentration-dependent manner. When LB30057 was treated with aortic rings isolated from rats, LB30057 resulted in a concentration-dependent inhibition of thrombin-induced vascular relaxation. All these results suggest that LB30057 is a potent inhibitor of platelet aggregation and blood vessel relaxation induced by thrombin.

Inhibition of Benzo(a)pyrene-Induced Mutagenicity and Lipid Peroxidation by d-Limonene and Cineole (Benzo(a)pyrene에 의한 돌연변미월성과 지질과산화에 미치는 d-Limonene과 Cineole의 엑제 효과에 대한 비교연구)

  • 강은미;박성배;김상건;정기화
    • Biomolecules & Therapeutics
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    • v.1 no.1
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    • pp.71-76
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    • 1993
  • It has been reported that d-limonene inhibits chemical-induced rat mammary cancer by the mechanism of increases in detoxification enzymes such as glutathione S-transferases and that cineole fails to exhibit significant suppressive effect on chemical-induced carcinogenesis. The present study was designed to compare the effects of d-limonene and cineole on the benzo(a)pyrene (BP)-induced mutagenicity, BP metabolism and lipid peroxidation. Modified Ames assay was employed to evaluate the inhibitory effect of d-limonene and cineole on the BP-induced mutagenicity. The number of revertant-bearing wells was decreased by 44~77% in the presence of both BP and d-limonene compared with that of BP alone whereas cineole decreased the number of revertant-bearing wells by 28~45% at the concentrations between $2{\mu}m$m.TEX> and 2 mM. d-Limonene suppressed BP metabolism by 16, 54 and 67% at 1, 10 and 100 mM, respectively while cineole inhibited the metabolism by 16, 26 and 55% at the same concentrations. The $EC_{50}$ values for d-limonene and cineole in inhibiting lipid peroxidation were 2.0 mM and 16 mM respectively, as assayed by thiobarbituric acid method. The present study showed that d-limonene and cineole have common antimutagenic effects although d-limonone appeared to be more effective than cineole in suppressing mutation and lipid peroxidation. The results suggest that the antimutagenic effects of d-limonene and cineole may be associated with alternation in enzyme activities and with inhibition of lipid peroxidation.

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Cytoprotective Effects of Platycodon grandiflorus (Jacq.) A.DC on C6 Glioma Cell Apoptosis by Oxidative Stress (산화스트레스로 인한 C6 Glioma Cell Apoptosis에 대한 길경의 세포보호효과)

  • Jo, Jae Joon;Shin, Min Gu;Kim, Eui Su;Lee, Young Su;Shin, Yong Jin;Jeon, Sang Yun
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.28 no.4
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    • pp.396-402
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    • 2014
  • This study is designed to investigate cytoprotective effects of Platycodon grandiflorus (Jacq.) A.DC on C6 glioma cell apoptosis by oxidative stress. Experimental C6 glioma cells were classified into four groups as follows: normal group, PGE group, chemical groups, PGE+chemical groups. Oxidative stress that caused by chemicals in the C6 glioma cell, check the impact to Chemical group was administered normal group. Apoptotic effect protecting in order to observe the chemical group was administered PGE. We to observe effects of PGE on SOD inhibition, total glutathione production in C6 glioma cells were administered PGE. In case of administration PGE, apoptosis induced by Paraquat was significantly decreased. In case of administration PGE, apoptosis induced by SNP was significantly decreased. In case of administration PGE, apoptosis induced by $H_2O_2$ was significantly decreased. In case of administration PGE, apoptosis induced by Rotenone was decreased, but the statistical significance was not. In case of administration PGE, SOD inhibition activities significantly decreased. In case of administration PGE, Total glutathione did not affect the content. These results suggest that PGE is able to treat a disease caused by oxidative stress and prevent a aging. These results suggest that PGE is a disease caused by oxidative stress and aging, the prevention and treatment of food shall be able to be applied.

Inhibitory Effects on Dopamine Biosynthsis and Protective Effect on L-DOPA-induced Neurotoxicity of liriodenine in PC12 cells

  • Jin, Chun-Mei;Lee, Jae-Joon;Yin, Shou-Yu;Kim, Yu-Mi;Yang, You-Jong;Ryu, Si-Yong;Lee, Myung-Koo
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.139.1-139.1
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    • 2003
  • The effects of liriodenine, an aporphine isoquinoline alkaloid, on dopamine biosynthesis and L-DOPA-induced neurotoxicity in PC12 cells were investigated. Treatment of PC12 cells with liriodenine at 10 $\mu\textrm{M}$ showed 33.6% inhibition of dopamine content decreased at 3 h and reached a minimal level at 12 h after the exposure to liriodenine at 10 $\mu\textrm{M}$. (omitted)

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Thieny/Furanyl-hydroxyphenylpropenones as Inhibitors of LPS-induced ROS and NO Production in RAW 264.7 Macrophages, and Their Structure-Activity Relationship Study

  • Kadayat, Tara Man;Kim, Mi Jin;Nam, Tae-Gyu;Park, Pil-Hoon;Lee, Eung-Seok
    • Bulletin of the Korean Chemical Society
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    • v.35 no.8
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    • pp.2481-2486
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    • 2014
  • Twelve thienyl/furanyl-hydroxyphenylpropenones were systematically designed and synthesized, and evaluated for their inhibitory effect on LPS-induced ROS and NO production in RAW 264.7 macrophages. Compound 11 displayed the most significant inhibitory activity of LPS-induced ROS and NO production in RAW 264.7 macrophages. Structure-activity relationship study indicated that para-hydroxyphenyl moiety plays an important role for inhibitory activities on both LPS-induced ROS and NO production as well as 3-thienyl moiety on molecule.

Action Characteristics of EK3143 and EK3150, New Cyclohexanedione Herbicides, and Their Effects on Acetyl CoA Carboxylase Activity (신규 cyclohexanedione계 화합물 EK3143과 EK3150의 제초작용 발현특성과 Acetyl CoA Carboxylase 활성에 미치는 효과)

  • Kim, J.S.;Song, J.H.;Cho, K.Y.
    • Korean Journal of Weed Science
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    • v.18 no.4
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    • pp.314-324
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    • 1998
  • This study was carried out to investigate the herbicidal action characteristics of EK3143 and EK3150, newly synthesized cyclohexanedione analogues, and their inhibitory effects on the acetyl-CoA carboxylase activity isolated from various plants. Sethoxydim, a typical cyclohexanedione herbicide, had a high herbicidal activity against only grasses with growth inhibition, leaf chlorosis and necrosis. EK3143 and EK3150 had a lower effect against grasses but a higher effect against broadleaf plants such as black nightshade and velvetleaf than sethoxydim had. Low rate application of EK3143 induced leaf bleaching(whitening), while high rate application induced the same symptoms as those of sethoxydim. EK3150 induced more significant whitening, additionally accompanying a curling of meristem part in broadleaf plants. A consistant tendency was observed between the growth inhibition against grasses and the senstivity of grass ACCase to these compounds, but not between herbicidal activities against broadleaf plants and the senstivity of dicotyledonous ACCase; i.e. EK3150, which had higher herbicidal activity against black nightshade and velvetleaf than EK3143 had in greenhouse, rather showed lower ACCase inhibition. In EK3150-treated barnyardgrass, growth inhibition occurred prior to decrease of photosynthetic pigments, in contrast to that of norflurazon and EK3140. These results suggest that EK3143 and EK3150 may have two target sites, ACCase and an unknown site on fatty acid synthesis related to growth inhibition and bleaching respectively, and their symptoms would be appeared in different degree by a differential binding affinity between two action sites.

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