• Title/Summary/Keyword: Microsomal fraction

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THE MUTAGENIC ACTIVITY OF SOME MEDICINAL PLANT EXTRACTS IN STRAINS TA98 AMD TA100 OF SALMONELLA TYPHIMURIUM (Salmonella typhimurium에 의한 생약추출물의 돌연변이성 연구 (I))

  • 김숙영;문자영;이동욱;박기현
    • Journal of the Korean Society of Tobacco Science
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    • v.9 no.2
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    • pp.87-93
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    • 1987
  • The mutagenic activities of the pyrolyzates (300, 600, 750 and 85$0^{\circ}C$ ) of extracts from three saponeous expectorants (Platicodi Radix, Polygalae Radix and Asiasari Radix) and two nonalkaloidal antitussives (Lirionis Tuber and Codonopsis lanceolata Radix), medicinal plants, were studied in the Ames Salmonella/microsomes test system. The pyrolysates of Codonopsis lanceolata Radix and Asiasari Radix extracts at 85$0^{\circ}C$ were slightly mutagenic to tester strain TA98( frame shift ) and TA100(base-pair substitution) of Salmonella typhimurium, and the mutagens in these pyrolyzates required the metabolic activation by a liver microsomal fraction However, the extracts and pyrolyzates of all medicinal plants tasted except the above two results dud not show the significant increase in revertant colonies.

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Hepatic Drug Metabolism Modifier from Arils of Myristica fragrans

  • Shin, Kuk-Hyun;Woo, Won-Sick
    • Korean Journal of Pharmacognosy
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    • v.17 no.1
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    • pp.91-99
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    • 1986
  • The single treatment of mice with steam distillate, non-volatile ether extract and methanol extract from mace (Arils of Myristica fragrans) caused a significant prolongation of hexobarbital-induced narcosis and increase in strychnine toxicity as well as a significant decrease in hepatic microsomal drug metabolizing enzyme activities. On 7 consecutive daily administrations, however, the duration of hypnosis was markedly shortened and significant increases in the hepatic enzyme activities were shown. With systematic fractionation by $SiO_2$ column chromatography of non-volatile ether fraction monitoring by animal tests a new lignan (mp $70{\sim}72^{\circ}$, MW 328, $[{\alpha}]^{20}_D+5.28$) was isolated as an active principle and its structure was elucidated as (2R, 3S)-1-(3,4-methylendioxyphenyl)-2,3 dimethyl-4-(4-hydroxy-3-methoxyphenyl) butane.

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A Study on the Antilipidperoxidative Effects of Brazilin(II) (천연색소 Brazilin의 항지질 과산화 활성에 관한 연구(II))

  • 문창규;하배진
    • Journal of Food Hygiene and Safety
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    • v.3 no.1
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    • pp.37-40
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    • 1988
  • A great deal of attention has been directed recently at the roles played by lipidperoxides in the mediation of pathogenesis and complications of various disease. In view of the strong inhibitory activity of Brazilin on the lipidperoxidation, we examined the effect of Brazilin on the lipidperoxidation in diabetic states. Brazilin inhibited the lipidperoxidation of liver mitochondrial and microsomal fraction in alloxan-induced diabetic ICR mice in the dose and time dependent manner. In the light of the present results, further elucidation of the inhibitory activities of Brazilin on the liver and blood plasma is warrented.

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Biological Evaluation of Mace for Drug Metabolism Modifying Activity

  • Shin, Kuk-Hyun;Woo, Won-Sick
    • Korean Journal of Pharmacognosy
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    • v.17 no.3
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    • pp.189-194
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    • 1986
  • The single acute treatment of mice with the steam distillate, non-volatile ether extract and methanol extract from mace, arils of Myristica fragrans(Myristicaceae) caused a significant prolongation of hexobarbital-induced narcosis, an increase in strychnine toxicity as well as a significant decrease in hepatic microsomal drug metabolizing enzyme activities. On seven daily consecutive administrations, however, the duration of narcosis was markedly shortened and significant increases in the hepatic enzyme activities were shown. From the non-volatile ether fraction, macelignan, a new lignan, mp $70{\sim}72^{\circ}$ was isolated as an active principle.

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Mutagenicity of Chinese Herbal Anti-cancer Drugs and Their Antimutagenic Activity to Base-pair Substitution Mutagen (치암중초약의 돌연변이유발 및 돌연변이유발 억제효과)

  • Lee, Hyun-Chul
    • The Journal of the Korean Society for Microbiology
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    • v.22 no.2
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    • pp.185-193
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    • 1987
  • Ten species of herbae, which have been used to treat cancers in Chinese medicine, were tested to investigate their mutagenicity or antimutagenicity in S. typhimurium TA97, TA98, TA100, TA1535, and TA1538. Scolopendra centipede was weakly active in reversion of the frameshift mutation in S. typhimurium TA97 strain and the base-pair substitution in TA100 and TA1535 strains. Other herbae such as Coix lachryma, Dianthus superbus, Tricanthoshse kirilowii, Eupatorium formosanum, Lithospermum erythrorhizon, Ansaema japonicum, Curcuma zedoaria, Helicteres angustifolia, and Euonymus sieboldianus did not show any of the mutagenic potential, regardless of the metabolic activation with rat hepatic microsomal fraction. Dianthus superbus, Eupatorium formosanum, and Euonymus sieboldianus exhibited suppressive activities on microbial mutagenesis of N-methyl-N'-nitrosoguanidine, a base-pair substitution mutagen, in TA1535 and TA100 tester strains. The antimutagenic activities of Dianthus superbus and Euonymus sieboldianus appeared to be dose-dependant.

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Antioidants of Theae Folium and Moutan Cortex (녹차와 목단피의 항산화 성분)

  • Boo, Yong-Chool;Jeon, Che-Ok
    • Applied Biological Chemistry
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    • v.36 no.5
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    • pp.326-331
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    • 1993
  • Three antioxidants were isolated: (-)-epigallocatechin and (-)-epigallo catechin gallate from Theae Folium generally called green tea, and gallic acid from Moutan Cortex. They inhibited $Fe^{3+}-ADP/ascorbate-induced$ lipid peroxidation in rat liver microsomal fraction, showing $IC_{50}$, the concentration of antioxidants which is required to inhibit 50% of the peroxidation for microsomal membranes at 1 mg protein/ml, to be $0.2\;{\mu}g/ml$, $0.4\;{\mu}g/ml$ and $2.5\;{\mu}g/ml$, respectively.

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Changes of the blood chemistry, lipid and protein components in blood and liver tissue according to the time lapsed of the rat after oral administration of caffeine (Rat에 caffeine 경구투여후 시간경과별로 혈액과 간조직에서 혈액화학성분, 지질 및 단백질 구성성분의 변화)

  • Do, Jae-cheul;Huh, Rhin-sou
    • Korean Journal of Veterinary Research
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    • v.36 no.4
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    • pp.795-807
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    • 1996
  • This study was conducted to identify the effects of caffeine on the lipid and protein components or blood chemistry levels of the serum as well as the total homogenate, mitochondrial and microsomal fraction of the rat(Sprague-Dawley, female) liver. Acute test were conducted to determine those effects. The acute test was conducted by dividing rats into 7 groups according to the time lapsed after a single oral administration of 100mg/kg caffeine(that is control, 2hrs, 4hrs, 8hrs, 24hrs, 48hrs and 72hrs lapsed group). The concentrations of glucose, urea nitrogen, uric acid, creatinine, total protein, albumin, A/G ratio, triglyceride, total cholesterol, HDL-cholesterol, free fatty acid, phospholipid as well as the activities of alanine aminotransferase(ALT), aspartate aminotransferase(AST) and alkaline phosphatase(ALP) were measured in the serum of each experimental groups. The concentrations of the carbonyl group, malondialdehyde(MDA) and the patterns of the SDS-PAGE(Sodium Dodecyl Sulfate-Polyacrylamide Gel Electrophoresis) were analyzed to determine the oxidative damages and metabolic changes on the lipid and protein components in the serum, and total homogenate, mitochondrial and microsomal fractions of the rat liver. The results obtained from this study were summarized as follows; 1. The concentrations of serum glucose were significantly higher(p<0.01) between 4(143.0mg/dl) and 8hrs(138.0mg/dl) in comparison to that of the control(101.1mg/dl) after a single oral administration of caffeine(100mg/kg). While on the other, there were no significant differences in the concentrations of urea nitrogen, uric acid, creatinine, total protein, albumin and albumin/globulin(A/G) ratio in comparison to those of the control. 2. The concentrations of total cholesterol and HDL-cholesterol in serum were significantly higher(p<0.01) between 4(77.4mg/dl, total cholesterol) and 8hrs(64.7mg/dl, HDL-cholesterol) in comparison to those of the control(62.8, 46.7mg/dl) after a single oral administration of caffeine(100mg/kg). On the other hand, the concentrations of triglyceride in serum were significantly lower(p<0.01) after 8hrs(38.8mg/dl) in comparison to that of the control(66.5mg/dl). 3. The activities of AST in serum was significantly higher(p<0.05) from 2hrs(149U/L) to 8hrs(178U/L) in comparison to the control(112U/L) after a single oral administration of caffeine(100mg/kg). The activities of ALT in serum were significantly higher(p<0.01) at 4(45.5U/L), 24(49.3U/L), 48(46.8U/L) and 72 hrs(42.3U/L) in comparison to that of the control(39.7U/L) after a single oral administration of caffeine(100mg/kg). On the other hand, there were no significant differences in the activities of ALP in comparison to that of the control. 4. The concentrations of free fatty acid in serum were significantly higher(p<0.01) at 8hrs(65.0mg/dl) in comparison to that of the control(37.6mg/dl) after a single oral administration of caffeine(100mg/kg). However, there were no significant differences in the concentrations of carbonyl group and malondialdehyde within serum, and liver homogenate, mitochondrial and microsomal fractions in comparison to that of the control. 5. The patterns of SDS-PAGE in serum, mitochondrial and microsomal fraction of the liver showed no significant differences.

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Farnesylcysteine Methyltransferase Activity and Ras Protein Expression in Human Stomach Tumor Tissue

  • Han, Eui-Sik;Oh, Hye-Young;Ha, Kwang-Won;Han, Beom-Seok;Hong, Seok-Min;Han, Jung-Whwan;Hong, Sung-Youl;Noh, Sung-Hun;Lee, Hyang-Woo
    • Archives of Pharmacal Research
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    • v.21 no.4
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    • pp.378-384
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    • 1998
  • The processing pathway of G-proteins and Ras family proteins includes the isoprenylation of the cysteine residue, followed by proteolysis of three terminal residues and .alpha.-carboxyl methyl esterification of the cysteine residue. Farnesylcysteine methyltransferase (FCMT) activity is responsible for the methylation reaction which play a role in the membrane attachment of a variety of cellular proteins. Four kinds of Ras protein (c-Ha-ras, c-N-Ras, c-Ki-Ras, pan-Ras) expression were detected in adenocarcinoma of human tissue by immunohistochemical method, and hematoxylin and eosin staining. The level of Ras protein in human stomach tumor tissues was much higher than in normal and peritumoral regions of the same biopsy samples. The FCMT activities of each cellular fractions were high in mitochondrial fraction followed by microsomal fraction, whole homogenate and cytosolic fraction. The inhibitory effect on FCMT activity on stomach tumor tissue was determined after treatment with 0.25 $\mu\textrm{M}$ of S-adenosyl-$_L$-homocysteine. S-adenosyl-$_L$-homocysteine inhibited FCMT activity from 11.2% to 30.5%. These results suggested that FCMT might be involved in Ras proteins activity.

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Effect of Benzoyl Peroxide on the Activity of Drug-metabolizing Enzyme System and Lipid Peroxidation in Rats (Benzoyl peroxide가 흰쥐의 지질과산화현상에 미치는 영향)

  • Lee, H.W.;Rhee, K.S.;Hong, S.U.
    • The Korean Journal of Pharmacology
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    • v.18 no.1
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    • pp.55-63
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    • 1982
  • Lipid peroxidation is the reaction of oxidative deterioration of polyunsaturated lipids and this peroxidation involves the direct reaction of oxygen and lipid to form free radical intermediates, which can lead to autocatalysis. As results of the extensive studies on the lipid peroxidation by many authors, the relationship between lipid peroxidation and the drug metabolizing system as well as the actions of free radicals on the peroxidation was reasonably well known. For a long time, the mechanism of hepatotoxicity of $CCl_4$ was not clearly understood. However, it is now quite well established that $CCl_4$ is activated in vivo to a free radical which is a highly reactive molecule. Therefore, lipid peroxidation which induces the reduction of cytochrome P-450 and aminopyrine demethylase activity is known as decisive event of $CCl_4$ hepatotoxicity. On the other hand, it was also reported that singlet molecular oxygen produces lipid peroxidation in liver microsomes. In this study the effects of benzoyl peroxide on the lipid peroxidation and drug-metabolizing enzyme were examined. Benzoyl peroxide mixed with starch and phosphates etc. is usually used as a food additive for flour bleaching and maturing purpose because of its oxidative property. Albino rats were used for the experimental animals. Benzoyl peroxide was suspended in soybean oil and sesame oil and administered intraperitoneally or orally. TBA value and aminopyrine demethylase activity were determined in liver microsomal fraction and serum. The results were summerized as following. 1) Body weights of animals administered benzoyl peroxide suspension were decreased while that of oil administered group were increased. 2) The activity of aminopyrine demethylase was generally decreased in animals administered oil suspension of benzoyl peroxide. Furthermore, the marked reduction of the enzyme activity was observed in animals administered benzoyl peroxide intraperitoneally. 3) Generally, microsomal TBA values as well as serum TBA were significantly elevated in benzoyl peroxide group in comparison with the control group. However, the more remarkable increase of serum TBA than microsomal TBA was observed in animals administered orally for 6 days. 4) Specifically, the changing pattern of TBA value was notable in serum rather than in liver microsome by intraperitoneal administration of benzoyl peroxide.

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Antioxidative Properties of Artemisia princeps Pamp (약쑥(Artemisia princeps Pamp)의 항산화작용)

  • Hong, Jung-Hee;Jeon, Jeong-Lan;Lee, Ju-Hyun;Lee, In-Seon
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.36 no.6
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    • pp.657-662
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    • 2007
  • Antioxidant properties of Artemisia princeps Pamp were determined using in vitro assay systems against 1,1-diphenyl-picrylhydrazyl (DPPH) radical, superoxide ($O_2{^-}$), hydrogen peroxide ($H_2O_2$), hydroxyl radical ($HO{\cdot}$) and nitric oxide (NO) radical, as well as rat liver microsomal lipid peroxidation. Among the five solvent fractions, ethyl acetate fractions showed the highest total polyphenol and flavonoid contents at $311.35{\mu}g/mg\;and\;92.73{\mu}g/mg$, respectively. Ethyl acetate fractions, except for $H_2O_2$ scavenging activity, also showed the highest scavenging activity; the 50% inhibitory concentration ($IC_{50},\;{\mu}g/mg$) values for DPPH, superoxide, $HO{\cdot}$ and NO radical scavenging were 52.71, 26.47, 58.92 and 65.94, respectively. Additionally, the highest inhibition of rat liver microsomal lipid peroxidation was observed by ethyl a cetate fraction.