• Title/Summary/Keyword: n uptake inhibition

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Inhibition of yeast Candida growth by protein antibiotic produced from Pseudomonas fluorescens BB2 (Pseudomonas fluorescens BB2 균주가 생산하는 단백질성 항생물질에 의한 효모 Candida 생육 억제)

  • Ahn, Kyung-Joon
    • Korean Journal of Microbiology
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    • v.51 no.4
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    • pp.448-452
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    • 2015
  • The bacterial strain that was isolated from chinese cabbage rhizosphere, showed inhibition of yeast growth. This strain was identified as Pseudomonas fluorescens BB2 by API 20NE test and 16S rRNA gene sequence analysis. P. fluorescens BB2 strain produced antibiotics against yeast as a secondary metabolite effectively when the culture was carried out in YM medium with 3% glucose at $20^{\circ}C$. The protein antibiotic of BB2 strain which was concentrated by ammonium sulfate precipitation and n-butanol extraction inhibited the growth of yeast with the minimal inhibitory concentration of $10{\mu}g/ml$ against Candida albicans KCTC 7965, and the growth of yeast was completely inhibited at $80{\mu}g/ml$. The hydrophilic fraction of n-butanol extraction inhibited the growth of Bacillus cereus ATCC 21366, showed orange halo on chrome azurol S plate, which means the fraction contained iron chelating siderophore. The results of crystal violet uptake through the cell membrane showed that membrane permeability was increased about 9% than control, when the concentration of hydrophobic antibiotic against yeast C. albicans was $60{\mu}g/ml$. As a result, the antibiotic produced by P. fluorescens BB2 against yeast Candida is considered antimicrobial peptide, and this is the first report in the genus Pseudomonas.

Effect of ${\gamma}$-mangostin through the inhibition of 5-hydroxytryptamine$_{2A}$ receptors in 5-fluoro-${\alpha}$-methyltryptamine-induced head-twitch responses of mice

  • Nattaya Chairungsrie;Furukawa, Ken-Ichi;Takeshi Tadano;Kensuke Kisara;Yasushi Ohizumi
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1998.11a
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    • pp.170-170
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    • 1998
  • In order to discover new types of 5-hydroxytryptamine antagonists, we have devoted our attention to investigating naturally occurring compounds having anti-5HT activity in vitro. Recently, ${\gamma}$-mangostin [1,3,6,7-tetrahydroxy-2,8-bis(3-methyl-2-bytenyl)-9H-xanthen-9-one] from the fruit hull of Garcinia mangostana Linn has been shown to be a selective antagonist for 5-hydroxytryptamine$_{2A}$ receptors in smooth muscle and platelets. It is of interesting that y-mangostin which does not have a nitrogen atom, possesses marked 5-$HT_{2A}$ receptor blocking activity. The present study was undertaken to investigate the effects of ${\gamma}$-mangostin on central 5-HT receptors by using animal behavioural models. Intracerebronventricular injection of ${\gamma}$-mangostin (10-40n mol/mouse) inhibited 5-fluoro-${\alpha}$-methyltryptamin (5-FMT) (45 mg kg$^{-1}$, i.p.)-induced head-twitch response in mice in the presence or absence of citalopram (5-HT-uptake inhibitor). Neither the 5-FMT- nor the 8-hydroxy-2-( di-n-propylamino )tetralin (5-HT$_{1A}$-agonist)-induced 5-HT syndrome (head weaving and hindlimb abduction) was affected by ${\gamma}$-mangostin. The locomotor activity stimulated by 5-FMT through the activation of at-adrenoceptors did not alter in the presence of ${\gamma}$-mangostin. 5-HT-induced inositol phosphates accumulation in mouse brain slices was abolished by ketanserin. ${\gamma}$-Mangostin caused a concentration-dependent inhibition of the inositol phosphates accumulation and the binding of [$^3H$]-spiperone, a specific 5-$HT_{2A}$ receptor antagonist, to mouse brain membranes. Kinetic analysis of the [$^H3$]-spiperone binding revealed that ${\gamma}$-mangostin increased the $_{d}$ value without affecting the $B_{max}$ value, indicating the mode of the competitive nature of the inhibition by ${\gamma}$-mangostin. These results suggest that ${\gamma}$-mangostin inhibits 5-FMT-induced head-twitch response in mice by blocking 5-$HT_{2A}$ receptors not by blocking the release of 5-HT from the central neurone. ${\gamma}$-Mangostin is a promising 5-$HT_{2A}$ receptors antagonist in the central nervous system.m.

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The In Vitro and In Vivo Effect of Lipoxygenase Pathway Inhibitors Nordihydroguaiaretic Acid and Its Derivative Tetra-O-methyl Nordihydroguaiaretic Acid against Brucella abortus 544

  • Reyes, Alisha Wehdnesday Bernardo;Kim, Heejin;Huy, Tran Xuan Ngoc;Nguyen, Trang Thi;Min, Wongi;Lee, Dongho;Hur, Jin;Lee, John Hwa;Kim, Suk
    • Journal of Microbiology and Biotechnology
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    • v.32 no.9
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    • pp.1126-1133
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    • 2022
  • This study investigated the contribution of lipoxygenase (LOX) inhibitors, nordihydroguaiaretic acid (NDGA), tetra-O-methyl nordihydroguaiaretic acid (M4N) and zileuton (ZIL), and thromboxane A2 (TXA2) inhibitor 4,5-diphenylimidazole (DPI) in the proliferation of Brucella abortus infection. None of the compounds affected the uptake of Brucella into the macrophages. We determined the effect of neutralizing leukotriene B4 (LTB4) receptor and showed that the uptake of the bacteria was inhibited at 30 min post-infection. M4N treatment attenuated intracellular survival of Brucella at 2 h post-incubation but it was not observed in the succeeding time points. DPI treatment showed reduced survival of Brucella at 24 h post-incubation while blocking LTB4 receptor was observed to have a lower intracellular growth at 48 h post-incubation suggesting different action of the inhibitors in the course of the survival of Brucella within the cells. Reduced proliferation of the bacteria in the spleens of mice was observed in animals treated with ZIL or DPI. Increased serum cytokine level of TNF-α and MCP-1 was observed in mice treated with M4N or ZIL while a lower IFN-γ level in ZIL-treated mice and a higher IL-12 serum level in DPI-treated mice were observed at 7 d post-infection. At 14 d post-infection, ZIL-treated mice displayed reduced serum level of IL-12 and IL-10. Overall, inhibition of 5-LOX or TXA2 or a combination therapy promises a potential alternative therapy against B. abortus infection. Furthermore, strong ligands for LTB4 receptor could also be a good candidate for the control of Brucella infection.

Naltrexone Inhibits Catecholamine Secretion Evoked by Nicotinic Receptor Stimulation in the Perfused Rat Adrenal Medulla

  • Yu, Byung-Sik;Min, Seon-Young;Seo, Yoo-Seok;Choi, Cheol-Hee;Lee, Eun-Hwa;Lim, Dong-Yoon
    • The Korean Journal of Physiology and Pharmacology
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    • v.9 no.4
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    • pp.223-230
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    • 2005
  • The purpose of the present study was to examine the effect of naltrexone, an opioid antagonist, on secretion of catecholamines (CA) evoked by cholinergic nicotinic stimulation and membrane-depolarization from the isolated perfused rat adrenal gland and to establish the mechanism of its action. Naltrexone $(3{\times}10^{-6}M)$ perfused into an adrenal vein for 60 min produced time-dependent inhibition in CA secretory responses evoked by ACh $(5.32{\times}10^{-3}M)$ , high $K^+$ $(5.6{\times}10^{-2}M)$ , DMPP ($10^{-4}$ M) and McN-A-343 $(10^{-4}M)$ . Naltrexone itself did also fail to affect basal CA output. In adrenal glands loaded with naltrexone $(3{\times}10^{-6}M)$ , the CA secretory responses evoked by Bay-K-8644, an activator of L-type $Ca^{2+}$ channels and cyclopiazonic acid, an inhibitor of cytoplasmic $Ca^{2+}-ATPase$, were also inhibited. However, in the presence of met-enkephalin $(5{\times}10^{-6}M)$ , a well-known opioid agonist, the CA secretory responses evoked by ACh, high $K^+$, DMPP, McN-A-343, Bay-K-8644 and cyclopiazonic acid were also significantly inhibited. Collectively, these experimental results demonstrate that naltrexone inhibits greatly CA secretion evoked by stimulation of cholinergic (both nicotinic and muscarinic) receptors as well as that by membrane depolarization. It seems that this inhibitory effect of naltrexone does not involve opioid receptors, but might be mediated by blocking both the calcium influx into the rat adrenal medullary chromaffin cells and the uptake of $Ca^{2+}$ into the cytoplasmic calcium store, which are at least partly relevant to the direct interaction with the nicotinic receptor itself.

Influence of Naloxone on Catecholamine Release Evoked by Nicotinic Receptor Stimulation in the Isolated Rat Adrenal Gland

  • Kim Ok-Min;Lim Geon-Han;Lim Dong-Yoon
    • Archives of Pharmacal Research
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    • v.28 no.6
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    • pp.699-708
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    • 2005
  • The present study was designed to investigate the effect of naloxone, a well known opioid antagonist, on the secretion of catecholamines (CA) evoked by cholinergic stimulation and membrane-depolarization in the isolated perfused rat adrenal glands, and to establish its mechanism of action. Naloxone ($10^{-6}\~10^{-5}$ M), perfused into an adrenal vein for 60 min, produced dose- and time-dependent inhibition of CA secretory responses evoked by ACh ($5.32\times10^{-3}$ M), high K+ ($5.6\times10^{-2}$ M), DMPP ($10^{-4}$ M) and McN-A-343 ($10^{-4}$ M). Naloxone itself also failed to affect the basal CA output. In adrenal glands loaded with naloxone ($3\times10^{-6}$ M), the CA secretory responses evoked by Bay-K-8644, an activator of L-type $Ca^{2+}$ channels, and cyclopiazonic acid, an inhibitor of cytoplasmic $Ca^{2+}$-ATPase, were also inhibited. In the presence of met-enkephalin ($5\times10^{-6}$ M), a well known opioid agonist, the CA secretory responses evoked by ACh, high $K^+$, DMPP, McN-A-343, Bay-K-8644 and cyclopiazonic acid were also significantly inhibited. Taken together, these results suggest that naloxone greatly inhibits the CA secretion evoked by stimulation of cholinergic (both nicotinic and muscarinic) receptors as well as that by membrane depolarization. It seems that these inhibitory effects of naloxone does not involve opioid receptors, but might be mediated by blocking both the calcium influx into the rat adrenal medullary chromaffin cells and the uptake of $Ca^{2+}$ into the cytoplasmic calcium store, which are at least partly relevant to the direct interaction with the nicotinic receptor itself.

Effect of McN-A-343, Clonidine and Cocaine on the Contractile Response of Rat and Rabbit Vas Deferens to Field Stimulation (McN-A-343, Clonidine 및 Cocaine의 백서(白鼠)와 가토정관(家兎精管)의 자극효과(刺戟效果)에 대(對)한 영향(影響))

  • Yang, Hyo-Koo
    • The Korean Journal of Pharmacology
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    • v.17 no.2
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    • pp.23-30
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    • 1981
  • 1) Effects of McN-A-343, clonidine and cocaine on the contractile response of the rat and rabbit vas deferens to field stimulation were investigated. The action mechanisms of these drugs have shown to be associated with endogenous norepinephrine(NE). 2) The contractile response to the stimulation of 5-10 Hz was markedly inhibited by the cumulative doses of McN-A-343 (0.003, 0.03, $0.3{\mu}g/ml$), clonidine (0.003, $0.3{\mu}g/ml$) and cocaine $(0.03\;{\mu}g/ml)$. The inhibition was antagonized by yohimbine and pjperoxan. 3) The inhibitory effect of McN-A-343 $(0.03{\mu}g/ml)$ and cocaine $(0.03{\mu}g/ml)$ was markedly enhanced by the same dose of cocaine and McN-A-343, respectively. This enhanced inhibition was also antagonized by yohimbine. 4) The contractile response to the stimulation of 0.01 Hz and 5-10 Hz was markedly potentiated by comparatively large doses of McN-A-343 $(30\;{\mu}g/ml)$ and $(3\;{\mu}g/ml)$. This potentiation was not observed in the presence of thymoxamine. The potentiation by McN-A-343 also did not appear in the presence of atropine. 5) The contractile response to the above stimulation was potentiated by muscarine and the potentiation was markedly attenuated in the presence of thymoxamine and atropine.

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Effect of Lime Stabilized Slaughterhouse Waste on Growth of Chinese Cabbage and Soil pH (산화칼슘을 처리한 도축폐기물이 배추의 생육 및 토양산도에 미치는 영향)

  • Back, Jun-Ho;Lee, Seung-Ho;Shin, Hyun-Jin;Song, Yu-Chun;Kim, Bok-Jin
    • Korean Journal of Soil Science and Fertilizer
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    • v.36 no.2
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    • pp.80-85
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    • 2003
  • This study was conducted to find out the effect of a lime stabilized slaughterhouse waste(LSW) on the growth of chinese cabbage and soil pH. Two levels of the lime stabilized slaughterhouse waste treatment, 169 and $338kg\;10a^{-1}$, with N-P-K fertilization were tested, and treatments of N-P-K and N-P-K with slaked lime were included in the experiment as a control. Fresh weight of chinese cabbage at harvest was not significantly different among the treatments. However, in the LSW treatment of $169kg\;10a^{-1}$, fresh weight of chinese cabbage was 5% higher comparing to the N-P-K treatment. Contents of N, P, and K in chinese cabbage were higher in the LSW treatments in comparison to the control treatments. Competitive inhibition of Mg uptake by Ca in the treatments of LSW and lime was apparent. Soil pH was increased by the application of LSW, and the increase in the LSW treatment of $169kg\;10a^{-1}$ was nearly the same as the soil pH increase in the slaked lime treatment. The lime stabilized slaughterhouse waste can be considered as a potential soil amendment for amelioration of soil acidity and supply of organic matter as well.

Algae and Nutrient Removal by Vegetated Artificial Floating Island (인공식물섬에 의한 조류(Algae)및 영양염류의 제거)

  • Park, Sun-Koo;Cho, In-Ki;Kwon, Oh-Byung;Mun, Jung-Soo;Um, Han-Yong;Hwang, Soon-Jin
    • Korean Journal of Ecology and Environment
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    • v.41 no.spc
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    • pp.93-98
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    • 2008
  • We investigated the effect on the removal of BOD, SS, TN and TP and algal growth inhibition of Vegetated Artificial Floating Island (VAFI), by examining microorganism activity and nutrient uptake in the batch test of various conditions: (1) Blank (Control group), (2) VAFI of $0.25m^2$, (3) AFI of $0.25m^2$ which has no vegetation, (4) buoyant plate of $0.25m^2$, (5) buoyant plate of $0.25m^2$ with linear media. The proportion of BOD removal in the VAFI, AFI, buoyant plate and buoyant plate with media were 82.7, 80.8, 45.2% and 59.6% respectively. TN removal in the VAFI, AFI and buoyant plate with media were 51.2, 31.7% and 25.1% respectively. TP removal in the VAFI, AFI, buoyant plate and buoyant plate with media were 23.3, 16.7, 10.0% and 13.3% respectively. Chlorophyll-${\alpha}$ removal in the VAFI was 97.9%. The factors of chlorophyll-${\alpha}$ removal in the VAFI accounted for the shading effect of 35.1%, microorganisms activity of 61%, and plant root of 1.8%.

Postprandial hypoglycemic effects of mulberry twig and root bark in vivo and in vitro (In vivo와 in vitro에서 상지 및 상백피 에탄올추출물이 식후 혈당 상승 억제 조절에 미치는 영향)

  • Park, Soo Yeon;Jin, Bo Ra;Lee, Yu Rim;Kim, You Jin;Park, Jeong Bin;Jeon, Young Hee;Choi, Sang Won;Kwon, Oran
    • Journal of Nutrition and Health
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    • v.49 no.1
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    • pp.18-27
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    • 2016
  • Purpose: Our previous study demonstrated the hypoglycemic effects of mulberry (Morus alba L.) leaf and the underlying mechanisms. Here we explored the potency of mulberry twigs (TW) and root barks (RB) in postprandial hypoglycemic effects in vitro and in vivo. Methods: The major components of TW and RB were determined by high performance liquid chromatography (HPLC). Alpha-glucosidase inhibition and glucose/fructose uptake inhibition in Caco-2 cells were determined for TW, RB, and their major components, followed by an oral sugar tolerance test (OSTT) in streptozotocin-induced diabetic rats. Male Wistar rats were fed a high-fat diet for 2 weeks and then a single dose of streptozotocin (35 mg/kg B.W) was administered by intraperitoneal injection. Rats with fasting blood glucose levels above 126 mg/dL were randomly divided into 5 groups (n = 8/group) for the following treatments by gavage for 4 weeks: vehicle (normal control and diabetic control), 200 mg/kg B.W of TW or RB or 100 mg/kg B.W of oxyresveratrol (OXY). Results: OXY and mulberroside A were identified as the major components of TW and OXY, mongolicin, and kuwanon H for RB. A significant inhibitory activity on ${\alpha}-glucosidase$ was found for TW, RB, and OXY (p = 0.0099). There was a dose-dependent inhibition of TW and RB on the intestinal sugar uptakes in Caco-2 cells, showing a greater impact on fructose compared to glucose. The OSTT showed that TW and RB significantly delayed time to maximal concentration (p = 0.0088) and decreased maximal concentration (p = 0.0043) compared to the control group. Conclusion: These results suggest that TW and RB may have a postprandial hypoglycemic effect, particularly in the case of high fructose or sucrose intake. OXY was suggested as a contributor to the hypoglycemic effect of TW and RB. Further studies are needed for the systemic effect of TW and RB in circulation.

Effect of Root-Zone Temperature in Hydroponics on Plant Growth and Nutrient Uptake in Vegetable Crops (수경재배(水耕栽培)에서 양액온도(養液溫度)가 채소작물(菜蔬作物)의 생장(生長) 및 무기양분흡수(無機養分吸收)에 미치는 영향(影響))

  • Jang, Byoung-Choon;Hong, Young-Pyo;Chun, Jae-Chul
    • Korean Journal of Soil Science and Fertilizer
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    • v.25 no.3
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    • pp.242-248
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    • 1992
  • This study was carried out to investigate the effects of root-zone temperature in hydroponics on the plant growth and nutrient uptake of lettuce(Lactuca sativa L), tomato (Lycopersicon esculentum Mill), and cucumber (Cucumis sativus L). Respiration rate in roots increased with increase in root-zone temperature. At $10^{\circ}C$ of root-zone temperature, respiration rate in lettuce root was higher than those in tomato and cucumber. Increasing rate of root respiration in tomato with increase in root-zone temperature was greater than those in lettuce and cucumber. The lowest dry weight and leaf area of the crops studied were obtained at $10^{\circ}C$ of root-zone temperature, but they were not different between 20 and $30^{\circ}C$. Increase in root-zone temperature generally resulted in increase in T/R ratio and net assimilation rate. At the low root-zone temperature, root growth and leaf area of tomato and cucumber were severely affected. Relative growth rates of lettuce and cucumber were also greatly reduced by the low root-zone temperature. Contents of N, P, K, Ca, and Mg in the crops increased as root-zone temperature increased from 10 to $20^{\circ}C$, whereas only Ca content in tomato and cucumber increased with increase in root-zone temperature to $30^{\circ}C$. Remarkably low contents of P and Mg in the crops were found at the low root-zone temperature. Inhibition of plant growth and nutrient uptake due to low root-zone temperature was much greater in cucumber than in lettuce and tomato.

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