• Title/Summary/Keyword: Oral activity

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Studies on the Mutagenicity and Hepatotoxicity of Antaeum (안태음의 변이원성 및 간독성에 관한 연구)

  • Lee, Dong-Nyung;Moon, Jin-Young;Oh, Gue-Suc;Lee, Tae-Kyun;Choi, Mi-Jung;Lee, Dong-Mok;Nam, Kyung-Soo
    • Korean Journal of Pharmacognosy
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    • v.28 no.3
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    • pp.149-155
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    • 1997
  • Antaeum(ATE) has been used as a prescription for threatened abortion, associated with pregnancy in traditional medicine. Because gravida could be administered ATE for a long period, its administration might cause a harmful effect on fetus and gravida during the pregnancy. This study aimed to determine whether exposure to ATE caused mutagenicity or hepatotoxicity during the pregnant period. For mutagenicity test of ATE, Salmonella typhimurium and Bacillus subtilis were used as indications for DNA damage. In the Ames test, Samonella typhimurium TA98 and TA100 were used for mutagenicity testing, and the number of histidine revertants was measured. In Rec-assay, Bacillus subtilis H $17(Rec^+)$ and $M-45(Rec^-)$ strains were used to clarify the DNA damage property. In the SOS umu test, Salmonella typhimurium TA15335 containing plasmid pSK1002 was used as a tester strain, and we monitored the levels of umu operon expression by measuring the ${\beta}-galactosidase$ activity. From the tested results, ATE did not show DNA damage and mutagenicity. On the other hand, hepatotoxicity of ATE to female ICR mice was monitored by the measurements of s-GOT, s-GPT and LDH activities after oral feeding for 15 days. ATE did not show significant change of s-GOT, s-GPT and LDH activities in mice sera.

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Effect of Myadis Stigma Water Extract on Adipogenesis and Blood Glucose in 3T3-L1 Adipocytes and db/db Mice (3T3-L1 지방세포와 db/db 마우스에서 옥수수수염 물 추출물의 지방생성 억제 및 혈당 저하효과)

  • Min, Oh-Jin;Sharma, Bhesh Raj;Park, Chul-Min;Rhyu, Dong-Young
    • Korean Journal of Pharmacognosy
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    • v.42 no.2
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    • pp.201-208
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    • 2011
  • Obesity occur from the imbalance between energy intake and energy expenditure. Obesity is a complex chronic disease that is suggested to cause other metabolic disorders such as type 2 diabetes, hyperlipidemia, hypertension, and arteriosclerosis. In this study, our purpose is to investigate the anti-hyperglycemic and anti-obesitic effects of Maydis stigma water extract in 3T3-L1 adipocytes and db/db mice. Maydis stigma water extract at dose of 100 and 500 ${\mu}g/ml$ slowly inhibited cell viability as compared to that of control in mature adipocytes. Also, the additions of 50 and 250 ${\mu}g/ml$ of Maydis stigma water extract significantly inhibited the lipid accumulations and CCAAT/enhancer-binding protein(C/EBP) ${\alpha}$ and peroxisome proliferator-activated receptor(PPAR) ${\gamma}$ expressions with dose-dependent manner in 3T3-L1 adipocytes. Maydis stigma water extract at 250, 500, and 1000 ${\mu}g/ml$ only showed the increasing pattern on lipolysis activity. The oral treatment of Maydis stigma water extract (100 or 400 mg/kg body weight) in db/db mice only showed tendency to decrease body weight, food efficiency ratio (FER), HbA1c, blood glucose, total cholesterol, triglyceride, and the adipocyte size of in db/db mice. However, Maydis stigma water extract increased the insulin level in a dose dependent manner. Thus these results indicate that Maydis stigma water extracxt inhibits adipogenesis through regulation of C/EBP${\alpha}$ and PPAR${\gamma}$ expressions in 3T3-L1 adipocytes and shows anti-hyperglycemic effect through increase of insulin secretion in db/db mice.

An Experimental Study on the Effect of Chengsimyeonjatang-gagam Extracts on the ADHD Animal Model (ADHD 동물모델에서 가감청심연자탕의 효과에 관한 실험연구)

  • Oh, Young-je;Liu, Quan Feng;Kim, Man-gi;Hong, Min-ho;Kim, Geun-woo;Koo, Byung-soo
    • Journal of Oriental Neuropsychiatry
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    • v.31 no.3
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    • pp.149-156
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    • 2020
  • Objectives: The purpose of this study was to experimentally assess the effects of Chengsimyeonjatanggagam extracts in the animal model regarding ADHD related symptoms and indicators. Methods: The experimental group was classified into the normal group (WKY rat) in 7, the control group (SHR rat) in 7, the low-concentration group of herbal medicines (SHR rat) in 7, and the high-concentration group of herbal medicines (SHR rat) in 7 by random sampling. The open field test was conducted three times on the 7th, 14th, and 21st days during the oral medication. After that, Y-maze test, intestinal permeability verification (L/M ratio), and Western blotting (CDK expression in the cerebral cortex) were performed in sequence. Results: The Chengsimyeonjatang-gagam extracts reduced the activity distance in the SHR rat at 21 days in the low and high concentration groups by the open field test. It also reduced the cross-action rate in the low and high concentration groups by the Y-maze test. And the low concentration group showed 52.3% decrease in the L/M ratio compared to the SHR group. Finally, the CDK5 protein significantly increased in the low and high concentration groups. Conclusions: This study suggests that the Chengsimyeonjatang-gagam extracts have potential to be used for the treatment of ADHD.

Effects of 8-Fluorociprofloxacin And Ciprofloxacin on the Central Nervous System

  • Kim, Young-Hoon;Kim, Dal-Hyun;Choi, Kyung-Eob
    • Toxicological Research
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    • v.8 no.2
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    • pp.161-170
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    • 1992
  • The objectives of this sutdy were to investigate the effects of 8-fluorociprofloxacin(8-FCP) on the central nervous system (CNS) and to compare with those of ciprofloxacin(CP). The $LD_{50}$ values of intravenous 8-FCP were similar or slightly lower in rat (M;203.6mg/kg, F;186.1mg/kg)and markedly lower in mice (M;126.5mg/kg, F;163.1mg/kg), as compared to those of CP. However, no recognizable differences in the clinical signs and recovery were found between 8-FCP and CP in both species. In combination with fenbufen, the convulsive liability of 8-FCP was higher than that of CP. At an intravenous dose of 10mg/kg, 8-FCP provoked convulsive signs and subsequent death in mice, whereas CP produced convulsion at a dose of 40mg/kg. The hexobabital -induced sleeping time was markedly lengthened by the oral administration of 8-FCP, but slightly increased by CP. In addition, the two quinolone derivatives had analgesic effects. The analgesic activity of 8-FCP was approximately two times higher than that at CP. However, both 8-FCP and CP had little effects of pentylenetetrazole-or strychnine-induced convulsion and muscle relaxation. Our finding that 8-FCP had more remarkable CNS effects than CP strongly suggests that there should be differences in the pharmacokinetic characteristics and/or in the binding affinity for specific biologic targets, or receptors, in the CNS.

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Pharmacokinetics and Tissue Distribution of a New Fluoroquinolone Containing C7-Bicyclic Structure in Rats (C7-이환체 구조를 갖는 새로운 플루오로퀴놀론계 항생물질의 흰쥐 체내동태와 조직분포)

  • 조재열;한승희;김병오;남권호;손호정;이재욱;유영효;박명환
    • Biomolecules & Therapeutics
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    • v.5 no.4
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    • pp.419-425
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    • 1997
  • The pharmacokinetics of DWP20364 (1-cyclopropyl -5-amino-6,8-difluoro-7-(2,7-diazabiclo [3,3,0] oct-4-ene-7-yl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid), a novel fluoroquinolone containing C7-bicyc-talc structure, were compared with those of ciprofloxacin (CPFX) after single intravenous (i.v.) and oral (p.o.) administration to rats using microbiological assay (bioassay). After i.v. administration to rats, the plasma concentrations of the two drugs declined biexponentially. The terminal half-lives (t$_{1}$2$\beta$/) of DWP20364 were 110$\pm$ 13.2 min and 117$\pm$3.09 min after i.v. and p.o. administration, respectively, and they were significantly higher than those of CPFX (45.5$\pm$9.52 min and 48.3$\pm$ 12.1 min, respectively). Similar results were also obtained from plasma concentrations and area under the plasma concentration-time curves. The total body clearance of DWP20364, 7.82$\pm$0.37 ml/min/kg was significantly slower than that of CPFX, 27.3 $\pm$ 11.1 m1/ min/kg. Above data suggested that the antimicrobial activity of DWP20364 could be longer than that of CPFX. The urinary recovery after i.v. and p.o. administration of DWP20364 was significantly lower than those of CPFX suggesting that the effect of DWP20364 on urinary tract infection could be lower than that of CPFX. The serum protein binding values of DWP20364 at 2$\mu$g/ml were apparently 91.5~93.1% in rats and human. DWP20364 was distributed by the order of liver, lung, kidney, sf)leon, heart, muscle and brain collected at 30 min after orally administered.

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5-Lipoxygenase Inhibition of the Fructus of Foeniculum vulgare and Its Constituents

  • Lee, Je-Hyeong;Lee, Dong-Ung;Kim, Yeong-Shik;Kim, Hyun-Pyo
    • Biomolecules & Therapeutics
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    • v.20 no.1
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    • pp.113-117
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    • 2012
  • The fruits of Foeniculum vulgare (Foeniculi Fructus) have been widely used in Chinese medicine as an antiemetic, ameliorating stomach ailments and as an analgesic. In order to establish its potential for antiallergic use, inhibitory actions of the fruit on 5-lipoxgenase (5-LOX) and ${\beta}$-hexosaminidase release were evaluated. The 70% ethanol extract of this plant material (FR) considerably inhibited 5-LOX-catalyzed leukotriene production from A23187-induced rat basophilic leukemia (RBL)-1 cells. The $IC_{50}$ was $3.2{\mu}g/ml$. From this extract, 12 major compounds including sabinene, fenchone, ${\gamma}$-terpinene, ${\alpha}$-pinene, limonene, p-anisylacetone, panisylaldehyde, estragole (4-allylanisole), trans-anethole, scopoletin, bergapten and umbelliferone were isolated. And it was found that several terpene derivatives including ${\gamma}$-terpinene and fenchone as well as phenylpropanoid, trans-anethole, showed considerable inhibitory action of 5-LOX. In particular, the $IC_{50}$ of trans-anethole was $51.6{\mu}M$. In contrast, FR and the isolated compounds did not show considerable inhibitory activity on the degranulation reaction of ${\beta}$-hexosaminidase release from antigen-treated RBL-2H3 cells. Against arachidonic acid-induced ear edema in mice, FR and trans-anethole showed significant inhibition by oral administration at doses of 100-400 mg/kg. In conclusion, FR and several major constituents are 5-LOX inhibitors and they may have potential for treating 5-LOX-related disorders.

Purification and risk assessment of Bacillus thuringiensis Vip3Aa protein against Apis mellifera (Bacillus thuringiensis 유래 Vip3Aa 단백질 순수분리 및 꿀벌 (Apis mellifera)에 대한 위해성평가)

  • Jung, Young Jun;Yoo, Su-Hyang;Lee, Jung Ro
    • Korean Journal of Environmental Biology
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    • v.37 no.4
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    • pp.585-591
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    • 2019
  • Most insect-resistant LMOs have been produced by applying Cry and Vip3Aa proteins. Vip3Aa protein is activated during the vegetative stage of Bacillus thuringensis (Bt) and the inhibitory activity of the Vip3Aa protein against pathogenic attacks from lepidopteran insect species is well known. However, a risk assessment of the Vip3Aa protein compared to the Cry protein has not been conducted in South Korea. This study demonstrates a possible risk assessment method for Vip3Aa protein against honeybees (Apis mellifera). For the risk assessment of the protein, we purified the recombinant Vip3Aa protein in Escherichia coli. The survival rate and symptoms of general intoxication of 4 months honeybees were measured after Vip3Aa exposure. These results indicated that there was no significant difference in the survival rate and the symptom between Vip3Aa and the control buffer. In this study, we established standard methods of Vip3Aa protein purification and oral adult toxicity test using A. mellifera as an LMO risk assessment technique for preserving the natural ecosystem of South Korea.

An Electron Microscopic Radioautographic Study of the Synthesis and Migration of the Glycoproteins in the Osteoclast of the Mice Maxillary Alveolar Bone (생쥐 상악치조부에서의 파골세포의 당단백 합성 및 이동에 관한 전자현미경 자기방사법적 연구)

  • Kim, Myung-Kook
    • Applied Microscopy
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    • v.22 no.2
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    • pp.118-126
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    • 1992
  • The pathway and time course of fucose-containing glycoprotein synthesis and intracellular translocation in osteoclasts of the mice maxillary alveolar bone were investigated by electron microscopic radioautography. Male Balb-C mice weighing 17gm were anesthetized with Nembutal and injected via the external jugular vein with 2.5 mCi of $L-[6-^{3}H]-fucose$ (specific activity 16.8 mCi/mmol) in 0.1 ml of sterile saline solution. At 5, 10, 20, 35 minutes and 8 hours after administration of the $^{3}H-fucose$, animals were killed by intracardiac perfusion of 30ml of 2% glutaraldehyde in a modified Tyroid solution, pH 7.4. The maxillae were then removed and further fixed in Karnovsky fixative for an additional 3-4 hours. After rinsing in 0.1M cacodylate buffer for 10 minutes, the maxillae were demineralized for 2 weeks at $4^{\circ}C$ in ethylene diamine tetra acetate containing 2% glutaraldehyde. The first interdental areas were mesiodistally sectioned into slices of 1mm thickness and postfixed in osmium tetroxide. Tissues were then dehydrated and embedded in Poly Bed. To prepare electron microscopic radioautography, the dipping method of Kopriwa (1973) was employed. Thin sections were coated with a crystalline monolayer of ILford $L_4$ photographic emulsion. After exposure for 4 months at $4^{\circ}C$, the sections were developed Kodak Microdol-X and Phenidon (for compact grains), fixed in 30% sodium thiosulfate, stained with uranyl acetate and lead citrate and examined in the electron microscope (JEOL 1200 EX). At 5, 10 and 20 minutes after injection, $^{3}H-fucose$ was concentrated in Golgi cisternae of the osteoblasts. By 35 minutes the labels were observed over small vesicles in the suprannclear area of osteoclasts. At 8 hours, numerous silver grains were located on the ruffled border and cell membrane of osteoclasts. These results indicate that fucose molecules are added in the Golgi apparatus and small vesicles appear to be responsible for translocation of the glycoproteins to the marginal portion of osteoblasts. The glycoproteins are distributed on the osteoclast cell surface and especially over the ruffled border.

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The Effects of yeast $\beta$-glucan in the Diet on Immune Response of Japanese eel, Anguilla japonica, by Oral Administration (Yeast $\beta$-glucan 첨가 사료가 뱀장어의 비특이적 면역 반응에 미치는 영향)

  • Kim, Jin-Do;Woo, Sung-Ho;Kim, Yi-Cheong;Lee, Jun-Hee;Cho, Yong-Chul;Choi, Sang-Min;Park, Soo-Il
    • Journal of fish pathology
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    • v.21 no.3
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    • pp.219-228
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    • 2008
  • The effects of dietary yeast β-glucan administration on growth, nonspecific immune responses, serum lysozyme, skin mucous lysozyme, NBT (nitroblue tetrazolium) reduction by phagocytes, and disease resistance against Edwardsiella tarda in Japanese eel, Anguilla japonica were evaluated. Fish were fed the diets supplemented with 0%, 0.1% and 0.5% of yeast β-glucan to a commercial diet for 6 weeks. The body weight gain from the fish fed on the 0.5% supplemented diet for 6 weeks was significantly higher than the control. Both serum and skin mucous lysozyme were significantly higher in the all experimental groups except 2 weeks of 0.5% group. The bactericidal activity of serum was slightly increased at 6 weeks. Also, The intracellular superoxide anion production of kidney phagocytes was significantly higher in the all experimental groups. The diet supplemented with 0.1% were also found to raise the relative percent survival (RPS) of Japanese eel after an artificial challenge with 1×107 cells of Edwardsiella tarda per fish. The results suggested the potential of yeast β-glucan to activate some innate immune responses and to improve the growth in Japanese eel.

Antidiabetic Activity of Polysaccharide Extract from Tetragonia tetragonoides in Streptozotocin-induced Diabetic Mice (스트렙토조토신으로 유도한 당뇨 마우스에서 번행초 다당 추출물의 항당뇨 효과)

  • Choi, Hye Jung;Yee, Sung-Tae;Joo, Woo Hong
    • Journal of Life Science
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    • v.27 no.5
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    • pp.579-583
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    • 2017
  • Tetragonia tetragonioides seems to be a promising antiulcer medicinal plant due to the presence of water-soluble polysaccharide and cerebroside as its major constituents. There have been no previous studies using T. tetragonioides polysaccharide extract (TPE) to assess its antidiabetic effect in streptozotocin (STZ)-induced diabetes in mice. This study was designed to evaluate the antidiabetic effect of TPE in diabetic mice, which was established by one-week intraperitoneal injection of 65 mg/kg STZ. After three weeks of TPE treatment at a dose of 100 mg/kg, a maintenance of body weight, a decrement in plasma glucose, and low levels of triglyceride, lactate dehydrogenase, alkaline phosphatase, and glutamic pyruvic transaminase were observed in diabetic mice. Furthermore, the ingestion of TPE lowered the blood glucose levels during the oral glucose tolerance test (OGTT) and restored most of the tested parameters to their normal levels. Therefore, the antidiabetic potential of T. tetragonioides has been demonstrated for the first time by our research.