• Title/Summary/Keyword: Mode of action

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Changes of Glutamate and Polyamine Levels of Hippocampal Microdialysates in Response to Occlusion of Both Carotid Arteries in Mongolian Gerbils (뇌허혈 손상에 있어서 해마-세포외액내 Glutamate와 Polyamine 농도의 변동에 관한 연구)

  • Shin, Kyung-Ho;Kim, Hyung-Gun;Choi, Sang-Hyun;Cho, So-Hyun;Chun, Yeon-Sook;Chun, Boe-Gwun
    • The Korean Journal of Pharmacology
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    • v.30 no.3
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    • pp.273-289
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    • 1994
  • Reversible brain ischemia was produced by occluding both common carotid arteries for 5 min, and the effects of aminoguanidine (AG), $DL-{\alpha}-difluoromethylornithine$ (DFMO), MK-801, and nimodipine (NM) on the ischemia induced changes of the polyamine, glutamate and acetylcholine levels in the hippocampus CA1 subfield and the specific $[^3H]\;MK-801$ binding to the hippocampus synaptosomal membranes were studied with a histological reference of the cresyl violet stained hippocampus. The basal putrescine level $(PT:\;74.4{\pm}8.8\;nM)$ showed a rapid increase (up to 1.7 fold) for 5 min of ischemia, remained significantly increased for 6 h, and then resumed the further increase to amount gradually up to about 3 fold 96 h after recirculation. However, the level of spermidine was little changed, and the spermine level showed a transient increase during ischemia followed by a sustained decrease to about 40% of the preischemic level after recirculation. The increase of PT level induced by brain ischemia was enhanced with AG or MK-801, but it was reduced by DFMO or NM. The basal glutamate level $(GT:\;0.90{\pm}0.l4\;{\mu}M)$ rapidly increased to a peak level of $8.19{\pm}1.14\;{\mu}M$ within 5 min after onset of the ischemia and then decreased to the preischemic level in about 25 min after recirculation. And NM reduced the ischemia induced increase of GT level by about 25%, but AG, DFMO and MK-801 did not affect the GT increase. The basal acetylcholine level $(ACh:\;118.0{\pm}10.5\;{\mu}M)$ did little change during/after brain ischemia and was little affected by AG or NM. But DFMO and MK-801, respectively, produced the moderate decrease of ACh level. The specific $[^3H]\;MK-801$ binding to the hippocampus synaptosomal membrane was little affected by brain ischemia for 5 min. The control value (78.9 fmole/mg protein) was moderately decreased by AG and MK-801, respectively but was little changed by DFMO or NM. The microscopic findings of the brains extirpated on day 7 after ischemia showed severe neuronal damage of the hippocampus, particularly CA1 subfield. NM and AG moderately attenuated the delayed neuronal damage, and DFMO, on the contrary, aggravated the ischemia induced damage. However, MK-801 did not protect the hippocampus from ischemic damage. These results suggest that unlike to the mode of anti-ischemic action of NM, AG might protect the hippocampus from ischemic injury as being negatively regulatory on the N-methyl-D-aspartate (NMDA) receptor function in the hippocampus.

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A Social Economic Comparative Study on Appearance Background of Design -for Native Settlement of Design in Korea - (우리 나라 디자인 도입에 관한 사회경제사적 고찰 - 디자인의 한국적 개념의 정착을 위한 시론 -)

  • 이인자
    • Archives of design research
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    • v.11
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    • pp.130-139
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    • 1995
  • The dictionary defines the word 'Design' as planning and designing. Though this is a meaning confined to decorative function, the conception of modern design in this capitalist society of mass production and mass consumption can be said to have reached a new stage of the meeting of industry and the arts. This means the two sides of design' the side of beauty and usefulness The side of beauty should be understood in view of the sense of beauty, and usefulness should also be considered from the viewpoint of consumer's taste and preference This is thought to be the natural problems of design The origin of design can be understood from the background of capitalism. But the capitalism can be said to be the mode of Western thought and action developed based on Western thinking. The capitalism is an economic system derived from the society of industrial capitalism through commercial capitalism. but this economic thinking has been resulted from a mature social system of democracy and civic society. The civic society and democracy are derived from polis of ancient Greece and Rome. and the ancient Greek and Roman society was a society developed from the social system of the nobility and slaves. Polis continued to develop based on the positive territorial expansionism centering around the Mediterranean on the basis of Hellenism. and European countries achieved the intergration of religion. society and politics based on this. thus accomplishing the spirit of capitalism Our design is believed to have been derived from the direct import of Western capitalism. Accordingly. as the original form of Western capitalism has become our economic system. so our design copied that of th West. And our traditional culture and sensitivity which are different in the original form and root of racial disposition seem to breed discord between them. It is. therefore. very important and meaningful for us to exert all possible efforts to seek the root of our disposition and tradition and grope for the appropriate thought and style of design.

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Inhibitory Effects of ${\gamma}$-Aminobutyric Acid on the Contractility of Isolated Rat Vas Deferens (흰쥐의 적출 정관 수축성에 대한 ${\gamma}$-Aminobutyric Acid의 억제작용)

  • Ahn, Ki-Young;Kwon, Oh-Cheol;Ha, Jeoung-Hee;Lee, Kwang-Youn;Kim, Won-Joon
    • Journal of Yeungnam Medical Science
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    • v.9 no.2
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    • pp.382-395
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    • 1992
  • GABA is an inhibitory neurotransmitter in central nervous system and produce sedative, antianxiety and muscle reaxing effects via $GABA_A$ receptor or $GABA_B$ receptor. Recently it is known that GABA is widely distributed throughout peripheral organs and may playa physiological role in certain organ. The vas deferens is innervated by species-difference. These study, therefore, was performed to investigate the mode and the mechanism of action of GABA on the norepiniphrine-, ATP- and electric stimulation-induced contraction of vas deferens of rat. Sprague-Dawley rats were sacrificed by cervical dislocation. The smooth muscle strips were isolated from the prostastic portion and were mounted in the isolated muscle bath. PSS in the bath was aerated with 95/5%-$O_2/CO_2$ at $33^{\circ}C$. Muscle tensions were measured by isometric tension transducer and were recorded by biological recording system. 1. GABA, muscimol, a $GAB_A$ agonist, and baclofen, a $GABA_B$ agonist inhibited the electric field stimulation(EFS, 0.2Hz, 1mSec, 80 V, monophasic square wave)-induced contraction with a rank order of potency of GABA greater than baclofen greater than muscimol. 2. The inhibitory effect of GABA was antagonized by delta aminovaleric acid(DAVA), a $GABA_B$ antagonist, but not by bicuculline, a $GABA_A$ mtagonist. 3. The inhibitory effect of baclofen was antagonized by DAVA, but the effect of muscimol was not antagonized by bicuculline. 4. Exogenous norepinephrine(NE) and ATP contracted muscle strip concentration dependently, but the effect of acetylcholine was negligible : and GABA did not affect the NE-and ATP-induced contractions. 5. GABA, baclofen and muscimol did not affect basal tone, and GABA did not affect the NE-and ATP-induced contractionsm 6. EFS-induced contraction was including 2 distinctable components. The first phasic component was inhibited by beta gamma-methylene ATP(mATP), a desensitizing agent of APT receptor and the second tonic component was reduced by pretreatment of reserpine(3 mg/Kg, IP). 7. GABA inhibited the EFS-induced contraction of reserpinized strips, but not the mATP-treated strips. These results suggest that in the prostatic portion of the rat vas deferens, adrenergic and purinergic neurotransmissions are exist, and GABA inhibits the release of ATP via presynaptic $GABA_B$ receptor on the excitatory neurons.

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Effects of Sinetrol-XPur on Leptin-Deficient Obese Mice and Activation of cAMP-Dependent UCP-2 (Leptin 유전자 결핍 동물모델을 이용한 시네트롤(Sinetrol-XPur)의 항비만 효과와 cAMP를 통한 UCP-2 활성화 기전 연구)

  • Yoo, Jae Myeong;Lee, Minhee;Kwon, Han Ol;Choi, Sei Gyu;Bae, Mun Hyoung;Kim, Ok-Kyung
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.45 no.4
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    • pp.484-491
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    • 2016
  • The present study investigated the effect of Sinetrol-XPur (polyphenolic Citrus spp. and Paullinia cupana Kunth dry extract) and defined the action mode for cyclic adenosine monophosphate (cAMP)-dependent uncoupling protein (UCP)-2 activation. Leptin-deficient obese mice were treated with two different doses, 100 mg/kg body weight (BW) and 300 mg/kg BW of each AIN93G supplement, for 7 weeks. Treatment of obese mice with both low and high doses of Sinetrol-XPur significantly reduced body weight gain compared to control obese mice. White adipose tissue weight of mice was reduced by 30.96% in high dose-supplemented groups. Serum total cholesterol and triglyceride were reduced by a high dose of Sinetrol-XPur by 20.02% and 30.96%, respectively. Serum level of high density lipoprotein (HDL) was significantly increased by treatment with both doses, as the ratio of HDL to low density lipoprotein increased by 138.78% and 171.49%, respectively. Regarding expression of biochemical factors related to lipid metabolism, fatty acid synthase significantly decreased and UCP-2 increased upon treatment with a high dose of Sinetrol-XPur, but there was no significant difference in lipoprotein lipase and hormone-sensitive lipase. To define cellular mechanism, intracellular cAMP levels in 3T3-L1 adipocytes significantly increased in a dose-dependent manner over the range of $50{\sim}250{\mu}m/mL$. The phosphodiesterase (PDE) inhibitor 3-isobutyl-1-methylxanthine clearly blocked cAMP, suggesting that Sinetrol-XPur promotes lipolysis of adipocytes through inhibition of cAMP-dependent PDE, resulting in induction of cAMP response element binding protein and UCP-2. These results suggest that Sinetrol-XPur supplementation is a viable option for reducing body weight and fat by improving serum lipid profiles and genetic expression of lipid metabolic factors, especially activation of cAMP-dependent UCP-2.

Effects of Non-Steroidal Anti-Inflammatory Drugs on the FMLP-Induced Migration of Neutrophil (비스테로이드성 항염증제가 FMLP에 의한 사람 중성구의 이동에 미치는 영향)

  • Kim, Woo-Mi;Kang, Koo-Il
    • The Korean Journal of Pharmacology
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    • v.30 no.1
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    • pp.137-143
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    • 1994
  • Enhancement or diminution of leukocyte migration to the specific site might be important factors for the development of inflammatory diseases. To investigate the effects of non-steroidal anti-inflammatory drugs (NSAIDs) on chemotaxis of neutrophil, we obtained neutrophils by Hypaque-Ficoll step gradient centrifugation and tested the effects of seven drugs on the n-formyl-leucyl-phenylalanine (FMLP)-induced migration of neutrophil using a 48-well micro chemotaxis assembly. Oxyphenbutazone, phenylbutazone, sulindac, zomepirac, and ibuprofen suppressed the migration of neutrophil at the therapeutic concentrations, however, indomethacin showed stimulation effect. IC50s for inhibition of neutrophil migration by these drugs are less than 100uM. When drugs were preincubated with FMLP, no inhibition on migration of neutrophil was observed. These results indicated that inhibitory effects of these drugs on migration of neutrophil might be related to the receptor sites of neutrophil rather than molecular inactivation of chemoattractant (FMLP). In conclusion, we suggested that the property of inhibition effects on neutrophil migration of several NSAIDs might be another mode of pharmacological action for anti-iflammatory effect, which showed significant effects at concentrations below therapeutic levels, in addition to cyclooxygenase inhibition.

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Inhibitory Effects of Chios Mastic Gum on Gastric Acid Secretion by Histamine-Related Pathway in a Rat Model and Primary Parietal Cells (위염 동물모델과 위 벽세포에서 히스타민 경로를 통한 매스틱검(Chios Mastic Gum)의 위산 분비 억제효과 및 기전 연구)

  • Nam, Da-Eun;Kim, Ok Kyung;Shim, Tae Jin;Lee, Jum Kyun;Hwang, Kwon-Tack
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.43 no.10
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    • pp.1500-1509
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    • 2014
  • The object of this study was to investigate the inhibitory effects of chios mastic gum (MG) on gastric acid secretion in an ethanol-induced SD rat model and primary parietal cells. Rats were randomly divided into four groups: Vehicle (normal group), Control (treated with ethanol), MG50 (treated with ethanol and mastic gum at 50 mg/kg b.w), MG100 (treated with ethanol and mastic gum at 100 mg/kg b.w). Groups treated with both MG50 and MG100 showed attenuation of gastric mucosal injury, sub-epithelial loss, hemorrhaging, and gastric juice secretion. We also examined the acidity of gastric juice during gastric injury. Oral administration of both MG50 and MG100 significantly decreased acidity of gastric juice by % and %, respectively. To examine the stimulatory factors related to gastric acid secretion, mRNA expression levels of H2r, M3r, CCK2r, and $H^+/K^+$ ATPase were measured by real-time PCR. Compared with a vehicle group, mRNA expression levels of H2r, CCK2r, and $H^+/K^+$ ATPase clearly increased in the control group. However, levels of H2r, CCK2r, and $H^+/K^+$ ATPase slightly but significantly decreased in MG-treated groups compared with control. Blood level of histamine significantly decreased in MG-treated groups, which indicates the involvement of MG on in histamine-related acid secretion. To identify the mode of action of MG in regulating histamine-related pathways, intracellular level of cAMP and mRNA levels of H2r, M3r, CCK2r, and $H^+/K^+$ ATPase were measured in primary parietal cells. While mRNA levels of M3r and CCK2r remained unchanged, levels of H2r and $H^+/K^+$ ATPase significantly decreased upon MG treatment. Subsequently, intracellular levels of cAMP decreased. These results suggest that mastic gum has the ability to inhibit gastric acid secretion by regulating a histamine-related pathway.

Inhibitory Effect on Infection of Plant Viruses by Filtrate Powder from Culture Broth of Acinetobacter sp. and Its Mode of Action (Acinetobacter sp. 배양여과액 분말제제의 식물바이러스에 대한 감염억제 효과 및 작용)

  • Kim Mi-Soon;Jung Min-Young;Kim Yun-Sung;Jang Cheol;Hwang In-Cheon;Ryu Ki-Hyun;Choi Jang-Kyung
    • Research in Plant Disease
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    • v.12 no.2
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    • pp.91-98
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    • 2006
  • A filtrate powder, designated as KNF2022, produced from culture broth of Acinetobacter sp. KTB3 was tested for their inhibitory effects on Pepper mild mottle virus (PMMoV) infection to Nicotiana glutinosa or N. tabacum cv. Xanthi nc. When 1/100 dilution with distilled water was treated to the plants and PMMoV was inoculated, the inhibition was estimated to be 94.3 and 95.6%, respectively. The same concentrations of KNF2022 inhibited infections of Pepper mottle virus (PepMoV) and Cucumber mosaic virus (CMV) on Chenopodium amaranticolor by 97.1 and 92.5%, respectively. Duration of inhibitory activity of the filtrate powder from Acinetobacter sp. culture broth against PMMoV infection on N. glutinosa was maintained for 2 days at 80% inhibition level, however, the inhibitory effect was diminished from 4 days after treatment to 50% levels. To evaluate inhibitory effects on systemic host plants of the antiviral agent, symptom developments of PMMoV, PepMoV and CMV on KNF2022-treated pepper plants were investigated. Delayed symptom developments until 10 days after inoculation (DAI) were observed for all the three viruses when the viruses were inoculated individually, and these delayed symptom development effects were maintained until 30 DAI in case of PepMoV. Moreover, PepMoV was not detected by RT-PCR and ELISA until 30 DAI. These delayed symptom development effects were diminished in all combinations of three virus co-inoculations due to synergism of three viruses on symptom developments. Inhibitory effect of KNF2022 was verified under electron microscopic examinations using purified virus preparations. Particles of PMMoV and PepMoV were observed on specimens from 5 min after KNF2022 treatment, and the particle sizes were reached in the range of 200-250 nm and 400-600 nm, respectively. Furthermore, the viral particles were destructed and particle sizes were reached in the range of 100-150 nm and 300-500 nm, respectively, on 60 min after treatments. Reduction of local lesion numbers on N. tabacum cv. Xanthi nc and C. amaranticolor were accompanied with reduction of virus particle sizes. In the case of CMV destructed particle numbers were also increased according to incubation period after KNF2022 treatment and local lesions on C. amaranticolor were reduced.

Inhibitory Effects of PLM-WE1 Formulated from Extract of Phellinus linteus Mycelium against Plant Viruses Infection and Identification of Active Compound (목질진흙버섯(Phellinus linteus) 균사체 추출물 제제 PLM-WE1의 식물 바이러스에 대한 감염억제 효과 및 활성성분의 동정)

  • Kwon, Soon-Bae;Bae, Seon-Hwa;Choi, Jang-Kyung;Lee, Sang-Yong;Kim, Byung-Sup;Kwon, Yong-Soo
    • Research in Plant Disease
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    • v.16 no.3
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    • pp.259-265
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    • 2010
  • Pepper mild mosaic virus(PMMoV) and Cucumber mosaic virus (CMV) are important pathogens in various vegetable crops worldwide. We have found that hot water extract of Phellinus linteus mycelium strongly inhibit PMMoV and CMV infection. Based on these results, the inhibitor named as 'PLM-WE1' formulated from extract of Phellinus linteus mycelium was tested for its inhibitory effects on PMMoV and CMV infection to each local lesion host plant (Nicotiana glutinosa: PMMoV, Chenopodium amaranticolor: CMV). Pretreatment effect of PLM-WE1 against infections of each virus (PMMoV and CMV) to local host plant was measured to be 99.2% to PMMoV and 80.3% to CMV, and its permeability effect was measured to be 45.0% to PMMoV and 41.9% to CMV. Duration of inhibitory activity of PLM-WE1 against PMMoV infection on N. glutinosa was maintained for 3 days at 75% inhibition level and CMV infection on C. amaranticolor maintained for 3 days at 62% inhibition level. Inhibitory effects on systemic host plants of PLM-WE1 were measured to be 75~85% to PMMoV and 75% to CMV. Under electron microscope, PMMoV particles were not denatured or aggregated by mixing PLM-WE1. It is suggested that the mode of action of PLM-WE1 differ from that of inactivation due to the aggregation of viruses. The methanol extract of P. linteus mycelium was sequentially partitioned with haxane, ethyl acetate, BuOH and $H_2O$. The $H_2O$ fraction was showed high activity than the other fractions. The active compound was isolated with a partial acid hydrolysis, fractional precipitation with ethanol. The inhibitory effect of the precipitate isolated from 70% ethanol fraction was 99.1% to PMMoV and 88.0% to CMV. The structure of isolated compound was determined by $^1H$-NMR and $^{13}C$-NMR. This compound was identified as a polysaccharide consisting alpha or beta-glucan.

Effects of Insoluble Dietary Fiber Supplementation on Performance and Nutrient Digestibility of Weanling Pigs (난용성 식이섬유의 첨가가 이유자돈의 생산성 및 영양소 소화율에 미치는 영향)

  • Han, Y.K.;Han, K.Y.;Lee, J.H.
    • Journal of Animal Science and Technology
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    • v.47 no.4
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    • pp.565-572
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    • 2005
  • An experiment was conducted to determine the effect of supplementation of insoluble dietary fiber (Vitacel®) on growth performance and nutrient digestibility in weanling pigs. A total of 96 pigs that averaged 6.49$\pm$0.52kg BW and 23$\pm$2.1d age were allocated in a randomized block design with two pigs per pen and 12 pens per treatment. Pigs and feeders were weighed 10-days interval for the 40-d trials to determine ADG, ADFI and feed:gain ratio(F:G). Pigs were fed one of four diets:1) Control diet (C) 2) C+0.3% insoluble dietary fiber(IDF) 3) C+0.6% IDF and 4) c+0.9% IDF. For the determination of fecal nutrients digestibility, pigs were fed diets(diet 2) with 1% Celite-545(Fluka) as a marker and feces were collected on $9^{th}$ day and $18^{th}$ day after feeding diet 2. During the whole experimental period, pigs fed diet with 0.3% IDF have significantly higher ADG than other dietary treatment groups(P<0.05). ADG of pigs fed diet with 0.6% IDF was higher than that of pigs fed control diet(P<0.05). However, there was no significant difference in ADG between control group and 0.9% IDF group(P>0.05). ADFI of pigs fed diet with 0.3% IDF was significantly higher than any other dietary treatment groups(P<0.05). There was no significant difference in ADFI among control group, 0.6% and 0.9% IDF supplementation groups (P>0.05). Digestibilities of organic matter, crude protein, crude fiber and energy were significantly higher in 0.3% IDF supplementation group than any other dietary groups. However, there was no difference in over all nutrient digestibilities between 0.6% and 0.9% IDF group. Feeding diets more than 0.6% IDF did not affect the rest of the nutrients digestibilities except for ADF digestibility compared to control diet. Dietary supplementation level of IDF showed a significant quadratic effect on performance improvement of piglets. This response of growth performance to IDF supplementation is, as expected, in agreement with that of nutrient digestibility. Our results showed that IDF supplementation to diet for weaned piglets might be beneficial in terms of growth and nutrient digestibility. However, there should be more study on the relationship between level of IDF supplementation and piglet response as well as the exact mode of action of IDF in weaned piglets.

A Study of Mode of Action of Fluazifop-butyl- II. Fluazifop-butyl Effect on Cell Division, Cell Enlargement, and Protein Synthesis in Oat(Avena sativa L.) Roots (Fluazifop-butyl의 제초기구(除草機構)에 관한 연구(硏究)- 제2보(第II報) Fluazifop-butyl이 귀리뿌리의 세포분열(細胞分裂), 세포신장(細胞伸張) 및 단백질합성(蛋白質合成)에 미치는 영향(影響))

  • Kim, Jae-Cheol
    • Korean Journal of Weed Science
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    • v.6 no.2
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    • pp.168-173
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    • 1986
  • The effects of varying concentrations and duration of fluazifop-butyl [(${\pm}$)-butyl [2- [4- [(5-(trifluoro methyl)-2-pyridinyl] oxy] phenoxy] propanate] treatment on cell division, cell enlargement, and protein synthesis were studied. Oat (Avena staiva L.) were treated from 0 to 48 hr with concentration ranging from $1{\times}10^{-6}M$ to $1{\times}10^{-3}M$ of fluazifop-butyl in the cell division study. There was a significant reduction in the mitotic indices of oat roots treated with $1{\times}10^{-4}M$ after 6 hr. After 18 hr treatment, All herbicide treatment inhibited cell division significantly. After 24 hr treatment almost 100% inhibition of cell division occurred at $1{\times}10^{-4}M$ to $1{\times}10^{-3}M$ while 20% inhibition of cell division occurred at $1{\times}10^{-6}M$ concentration at same exposure period. The greatest inhibition of cell division occurred between 0 to 18 hr. The avena coleoptile straight- growth test were used to determine the influence of fluazifop-butyl on eoleoptile growth. Significant inhibition of elongation of oat coleoptiles were observed at $1{\times}10^{-7}M$ to $1{\times}10^{-3}M$ after 24 hr incubation. Protein incorporation study showed that the $1{\times}10^{-4}M$ of fluazifop-butyl caused 60% inhibition of protein synthesis. It was concluded that the growth of inhibition of plants caused by fluazifop-butyl results from inhibition of cell division, cell enlargement, and protein synthesis.

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