• The Korean Journal of Ecology
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• 제20권4호
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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.

• Molecules and Cells
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• 제38권4호
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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.

• Bulletin of the Korean Chemical Society
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• 제20권3호
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• pp.370-372
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• 1999

• Archives of Pharmacal Research
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• 제27권12호
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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.

• Archives of Pharmacal Research
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• 제25권6호
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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.

• Biomolecules & Therapeutics
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• 제1권1호
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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.

• 동의생리병리학회지
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• 제28권4호
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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.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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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)

• Bulletin of the Korean Chemical Society
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• 제35권8호
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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.

• 한국잡초학회지
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• 제18권4호
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• pp.314-324
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• 1998

신규로 합성한 cyclohexanedione계 화합물 EK3143과 EK3150의 제초작용 발현의 특성을 기존약제와 비교조사하고, 이들이 ACCase에 대해 어떠한 저해활성을 가지는지를 알아보고자 제반실험을 수행하였다. Sethoxydim은 화본과식물에만 제초효과를 가지며 생육정지와 함께 조직의 황화, 괴사가 나타난다, 반면에 Ek3143과 EK3150은 화본과식물에 대한 활성은 상대적으로 감소되었으나 까마중, 어저귀 등의 광엽잡초에 대해서는 보다 강한 활성을 가졌다. EK3143은 저농도의 보다 폭넓은 범위에서는 백화증상이, 고농도에서는 sethoxydim과 동일한 증상을 나타내었고 EK3150은 모든 농도에서 식물체의 백화를 유기시켰으며 광엽잡초의 경우 분열조직에서 그 증상이 뚜렷하였다. 이들 화합물의 화본과식물에 대한 생육저해 활성과 옥수수 ACCase에 대한 저해정도간에는 일치된 경향을 보였으나 광엽잡초인 어저귀와 까마중에 대한 ACCase 활성과 전식물체(intact plant)에서의 제초활성간에는 일치된 경향을 보이지 않았다. 즉 EK3143과 EK3150은 어저귀와 까마중의 ACCase에 대한 저해활성이 sethoxydim보다 전반적으로 높은 특징을 보이지만, 광엽잡초에 대한 제초활성이 상대적으로 높았던 EK3150이 ACCase에 대해서는 EK3143보다 오히려 낮은 저해활성을 나타내었다. 한편 색소감소 정도가 신장저해보다 빨리 나타나는 norflurazon 및 EK3140 처리에서와는 달리, EK3143과 EK3150 처리에서는 색소감소 보다 신장저해가 보다 빠르게 나타나 다른 저해양상을 보였다. 이상의 결과로 보아 EK3143 EK3150은 ACCase 이외에 다른 작용점을 추가로 저해하는 것으로 생각되며, 약간의 구조변경에따라 제초작용점간의 결합정도에 차이가 생김으로써 생육저해 또는 백화증상이 서로 비중을 달리하여 나타나는 것으로 추정된다.