• Title/Summary/Keyword: enzyme inhibitors

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Evaluation of Factors Affecting Glomerular Filtration Rate by Contrast Media in Patients with Coronary Angiography (심혈관 조영술 시행 환자의 조영제 사용 시 사구체여과율 변화에 영향을 미치는 인자들 평가)

  • Kim, Eun-Young;Lee, Ok-Sang;Lim, Sung-Cil
    • Korean Journal of Clinical Pharmacy
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    • v.22 no.2
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    • pp.103-112
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    • 2012
  • Performance of coronary angiography for exact diagnosis and treatments of cardiovascular disease have been increased recently and it also brings increase of the contrast-induced nephropathy (CIN) referred from increasing use of radiological contrast agents. The variation of estimated glomerular filtration rate (eGFR) is an indicator of CIN, which is known to increase when renal function is decreased. Therefore, this study was to evaluate the affecting factors including concomitant drug on variation of eGFR of patients who underwent coronary angiography according to the conditions of renal function. Medical records of 66 patients were evaluated retrospectively and the patients underwent coronary angiography or angioplasty with nonionic and isotonic contrast media (iodixanol) at Chungnam national university hospital from 1 Jan 2008 to 30 Jul 2010. Patients group was divided into 2 groups; the patients in stages 3-4 chronic kidney disease (CKD) and the patients in stage 2 CKD. Each group was researched about the effect of concomitant drug and clinical characteristics on eGFR variation. The change of eGFR was compared among baseline and 2 or 3 day after coronary angiography. In results, the eGFR variation in group over age 75 was significantly decreased after radiological contrast agents exposure (p $$\leq_-$$ 0.05). The eGFR variation in anemia was significantly decreased after radiological contrast agents exposure in stage 2 CKD (p > 0.05). The eGFR variation in group under $HbA_{1c}$ 6.5% was significantly decreased after radiological contrast agents exposure in stages 3-4 CKD (p $$\leq_-$$ 0.05). The eGFR variation by taking statins, angiotensin converting enzyme inhibitors, calcium channel blockers and nitroglycerin was increased after radiological contrast agents exposure in stage 2 CKD (p $$\leq_-$$ 0.05). The eGFR variation by using of diuretics was significantly decreased after radiological contrast agents exposure in stages 3-4 CKD (p $$\leq_-$$ 0.05). The eGFR variation by taking statins, nitroglylcerin was increased after radiological contrast agents exposure in stages 3-4 CKD(p > 0.05). The eGFR variation in group over contrast dosage 150 ml was significantly decreased after radiological contrast agents exposure in stages 3-4 CKD (p $$\leq_-$$ 0.05). Therefore, when undergoing coronary angiography, contrast dosage should be minimized less than 150 ml, and diuretics should be restricted as possible in stages 3-4 CKD. Patients over age 75 require special attention to prevent CIN, and if patients undergo coronary angiography in stages 3-4 CKD, $HbA_{1c}$ is also requried to maintain below 6.5% to prevent CIN.

Studies on Screening and Iolation of ${\alpha}-Amylase$ Inhibitors of Soil Microorganisms( II ) -Isolation and Activities of the Inhibitor of Streptomyces Strain DMC-72- (토양균의 ${\alpha}-Amylase$ 저해제 검색 및 분리에 관한 연주(제2보) -스트렙토마이세스속 DMC-72 균주의 저해 성분의 분리 및 작용-)

  • Kim, Kyung-Jae;Lee, Shung-Hee;Kim, Jung-Woo;Kim, Ha-Won;Shim, Mi-Ja;Choi, Eung-Chil;Kim, Byong-Kak
    • The Korean Journal of Mycology
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    • v.13 no.4
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    • pp.203-212
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    • 1985
  • Of 450 strains isolated from the soil microbes collected in various locations in Korea, a strain had a strong inhibitory activity against bacterial ${\alpha}-amylase$ and was named strain DMC-72 of the genus Streptomyces. The amylase inhibitory metabolite produced by this strain was purified by means of acetone precipitation, adsorption on Amberlite IRC-50 and SP-Sephadex C-25. The inhibitor was found to be a derivative of oligosaccharides by spectral and chemical data. The inhibitor was stable at the pH range of $1{\sim}13$ and at $100^{\circ}C$ for half an hour, also inhibited other amylases such as salivary ${\alpha}-amylase$, pancreatic ${\alpha}-amylase$, fungal ${\alpha}-amylase$ and glucoamylase. However, it showed no inhibitory activity against ${\alpha}-glucosidase$, ${\beta}-glucosidase$, dextranase, and ${\beta}-amylase$. The kinetic studies of the inhibitor showed that its inhibitory effects on starch hydrolysis by ${\alpha}-amylase$ were noncompetitive.

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Enhanced Radiosensitivity of Tumor Cells Treated with Vanadate in Vitro (Vanadate 처리가 종양세포의 방사선 감수성에 미치는 영향)

  • Lee, Myung-Za;Lee, Won-Young
    • Radiation Oncology Journal
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    • v.12 no.2
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    • pp.129-141
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    • 1994
  • Intracellular ions which have a major role in cellular function have been reported to affect repair of radiation damage. Recently it has been reported that ouabain sensitizes A549 tumor cellls but not CCL-120 normal cells to radiation. Ouabain inhibits the $Na^+-K^+$-pump rapidly thus it increases intracellular Na concentration, Vanadate which is distributed extensively in almost all living organisms is known to be a $Na^+-K^+$-ATPase inhibitors, This study was performed to see any change in radiosensitivity of tumor cell by vanadate and any role of $Na^+-K^+$ATPase in radiosensitization. Experiments have been carried out by pretreatment with vanadate in human cell line(A549, JMG) and mouse cell line(L1210, spleen). For the cell survival MTT assay was performed for A549 and JMC cells and frypan blue dye exclusion test for L120, and spleen cells. Measurements of $Na^+-K^+$-ATPase activity in control, vanadate treated cell, radiation treated cell (9 Gy for A549 and JMG, 2 Gy for L1201, spleen), and combined $10^{-6}M$ vanadate and radiation treated cells were done. The results were summerized as fellows. 1. L1210 cell was most radiosensitive, and spleen cell and JMG cell were intermediate, and A549 cell was least radiosensitive. 2. Mininum or no cytotoxicity was seen with vanadate below concentration of $10^{-6}M$. 3. In A549 cells there was a little change in radiosensitivity with treatment of vanadate. However radiation sensitization was shown in low dose level of radiation i. e. 2- Gy. In JMG cells no change in radiosensitivity was noted. Both L1210 and spleen cell had radiosensitization but change was greater in tumor cell. 4. $Na^+-K^+$-ATPase activity was inhibited significantly in tumor cell by treatment of vanadate. 5. Radiaiton itself inhibited $Na^+-K^+$-ATPase activity of tumor cell with high $Na^+-K^+$-ATPase concention. Increase in radiosensitivity by vanadate was closely associated with orginal $Na^+-K^+$-ATPase contents. From the above results vanadate had little cytotoxicity and it sensitized tumor cells to radiation. Inhibitory effect of vanadate on $Na^+-K^+$-ATPase activity might be one of the contributing factors for radiosensitization to tumor cells which has greater enzyme activity than that of normal cell. It was suggested vanadate could be used as a potential radiosensitizer for tumor cells.

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Microbiological Studies on the Rice Makkulli (Part 2) Nucleic Acid Degrading Enzymes and Their Related Substances during Rice Makkulli Koji Making (쌀막걸리의 미생물학적 연구 (제2보)쌀막걸리 제국중 핵산분해효소 및 핵산관련물질)

  • 정덕화;성낙계
    • Microbiology and Biotechnology Letters
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    • v.8 no.1
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    • pp.1-8
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    • 1980
  • Changes of nucleic acid related substances and their enzymes during rice makkulli koji making were observed and enzymological properties of crude enzymes were examined. The results obtained were as follows : (1) The amounst of acid soluble phosphorus were increased, while no remarkable changes were observed in the component of total phosphorus during koji making. (2) AMP and IMP were increased, while ADP and ATP were decreased gradually in the course of process. (3) Activities of nucleic acid degrading enzymes were increased with the lapse of time. (4) In the crude enzyme solution extracted from rice makkulli koji, the optimal pH of RNase was 4.0~5.0 and those of PDase PNase were 5.0. (5) RNase and PMase were stable at the range of pH 4.0~5.0 and PDase was stable at the pH 4.0. (6) The optimal temperature of RNase was 55$^{\circ}C$, and that of PDase was at the range of 50~55$^{\circ}C$, and 5$0^{\circ}C$ for PMase. (7) Among the three enzymes, the heat stability was in order RNase, PDase and PMase, and especially PMase was so heat labile that it was almost inactivated at 7$0^{\circ}C$ for 10 min. (8) Inhibition by metal ions and other inhibitors was disclosed : C $u^{++}$ and Z $n^{++}$ inhibited the activity of RNase, and C $u^{++}$, NaF and N $a_2$HP $O_4$ inhibited that of PDase, while C $u^{++}$ and NaF inhibited the PMase activity.ctivity.

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Associations of matrix metalloproteinase (MMP)-8, MMP-9, and their inhibitor, tissue inhibitor of metalloproteinase-1, with obesity-related biomarkers in apparently healthy adolescent boys

  • Shin, Youn Ho;Kim, Ki Eun;Lee, Yong-Jae;Nam, Jae-Hwan;Hong, Young Mi;Shin, Hye-Jung
    • Clinical and Experimental Pediatrics
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    • v.57 no.12
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    • pp.526-532
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    • 2014
  • Purpose: Matrix metalloproteinases (MMPs) have been implicated in atherosclerosis, and therefore, are considered risk factors for metabolic dysfunction in adults. However, there is little data on circulating levels of MMPs and tissue inhibitors of MMPs (TIMPs) with regard to obesity-related biomarkers in the general adolescent population. In the present study, we determined the associations of MMP-8, MMP-9, and TIMP-1 levels and MMP-8/TIMP-1 and MMP-9/TIMP-1 ratios with obesity-related biomarkers in apparently healthy adolescent boys. Methods: We measured MMP and TIMP concentrations in plasma samples using the enzyme-linked immunosorbent assay and analyzed their associations with obesity-related biomarkers, such as liver enzymes and lipid profiles, in a sample of 91 Korean boys aged 13-14 years who participated in a general health check-up. Results: The mean age of the boys was $13.8{\pm}0.3years$; 72 boys were normal weight and 19 were overweight/obese. The Pearson correlation coefficients revealed a significant correlation between MMP-8 and aspartate aminotransferase (r=0.217, P=0.039) and alanine aminotransferase (r=0.250, P=0.017) and between TIMP-1 and aspartate aminotransferase (r=0.267, P=0.011). In a multivariate linear regression analysis, serum alanine aminotransferase was positively associated with the MMP-8 level. There were no significant differences in the MMP-8, MMP-9, and TIMP-1 levels or MMP-8/TIMP-1 and MMP-9/TIMP-1 ratios between control and overweight/obese subjects. Conclusion: We found a significant association between the MMP-8 level and alanine aminotransferase in the apparently healthy adolescent boys. These findings indicate that there may be a pathophysiological mechanism underlying the relationship between MMP-8 and liver enzymes in young adolescents.

Polyphenol Compounds and Biochemical Characteristics of Polyphenol Oxidase in Chinese Chestnut (밤의 Polyphenol물질과 Polyphenol Oxidase의 생화학적 특성)

  • Yun, Ki Yun;Moon, Kwang Deog;Sohn, Tae Hwa
    • Current Research on Agriculture and Life Sciences
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    • v.9
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    • pp.51-59
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    • 1991
  • This study was conducted to understand browning characteristics of Chinese Chestnut during processing and storage. For this, the isolation and identification of polyphenolic compounds and the biochemical characteristics of polyphenol oxidase(PPO) were investigated. The content of total phenol was $6.5{\mu}g/g$ and it was consisted of ferulic acid, caffeic acid, synapic acid, p-coumaric acid, gallic acid and salicylic acid in order. PPO was purified 11.7 fold through ammonium sulfate fractionation, DEAE-cellulose column chromatography and Sephadex G-200 column chromatography. Purified enzyme showed single protein and activity band by polyacrylamide gel electrophoresis. The optimum pH and temperature of PPO were 5.9 and $45^{\circ}C$, respectively. The activity of PPO was lost 93% by exposing at $80^{\circ}C$ for 15minutes. $Mg^{{+}{+}}$, $Ca^{{+}{+}}$, $Zn^{{+}{+}}$ increased the activity of PPO, but $Fe^{{+}{+}}$, $K^+$, $Hg^{{+}{+}}$ inhibited PPO at 10mM concentration. L-ascorbic acid, thiourea, sodium chloride and L-cysteine were effective inhibitors of PPO. The activity of PPO was higher for o-diphenols than other polyphenols. The Km value of PPO for catechol was 5mM.

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Effect of Vitamin C, Silicon and Iron on Collagen Synthesis and Break-Down Enzyme Expression in the Human Dermal Fibroblast Cell (HS27) (피부 섬유아세포에서 비타민 C, Silicon, 철분 처리가 콜라겐 합성 및 분해 관련 효소의 발현에 미치는 효과 비교)

  • Kim, Jeong-Eun;Lee, Jin-Ah;Kim, Hyun-Ae;Kim, Jung-Min;Cho, Yun-Hi
    • Journal of Nutrition and Health
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    • v.42 no.6
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    • pp.505-515
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    • 2009
  • Collagen is the major matrix protein in dermis and consists of proline and lysine, which are hydroxylated by prolyl hydroxylase (PH) and lysyl hydroxylase (LH) with cofactors such as vitamin C, oxygen, iron (Fe$^{2+}$), ketoglutarate and silicon. The collagen degradation is regulated by matrix metalloproteinase-1 (MMP-1), of which is the major collagen-degrading proteinase whereas tissue inhibitors of metalloproteinase-1 (TIMP-1) bind to MMP-1 thereby inhibiting MMP-1 activity. In this study, we investigated the effects of vitamin C, silicon and iron on mRNA, protein expressions of PH, LH, MMP-1 and TIMP-1. The physiological concentrations of vitamin C (0-100 $\mu$M), silicon (0-50 $\mu$M) and iron (Fe$^{2+}$:0-50 $\mu$M) were treated to human dermal fibroblast cells (HS27 cells) for 3 or 5days. The expression level of mRNA and protein was increased in not only PH but also LH when cells were incubated with vitamin C. A similar increase in LH mRNA or protein expression occurred when cells were incubated with silicon. Our results suggest that treatment of vitamin C and silicon increased mRNA and protein expression of PH and LH in human dermal fibroblast.

Screening of $\alpha$-amylase and $\alpha$-glucosidase Inhibitors from Brazilian Plant Extracts for Treatment of Rumen Acidosis (100종 브라질 식물 추출물로부터 반추동물 산독증 예방치료를 위한 $\alpha$-amylase 및 $\alpha$-glucosidase 저해제의 선별)

  • Kim, Mi-Sun;An, Seon-Mi;Jung, In-Chang;Kwon, Gi-Seok;Sohn, Ho-Yong
    • Food Science and Preservation
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    • v.17 no.2
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    • pp.290-296
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    • 2010
  • To develop anti-acidosis and anti-diabetes agentsfrom natural products, the inhibitory activities of Brazilian plant extracts against microbial $\alpha$-amylase and $\alpha$-glucosidase were evaluated. Among 100 different ethanol extracts tested, those of Acacia jurema Mart., Anacardium humile A. St.-Hil., Cedrela odorata L., and Guazuma ulmifolia Lam showed good inhibitoryactivities toward both enzymes. In addition, an extract of Plumeria drastica Mart. showed specific inhibition of $\alpha$-amylase, whereas that of Eugenia uniflora L. demonstrated strong inhibition of the enzyme. IC50 values of $\alpha$-amylase inhibition suggested that the extract of A. humile A. St.-Hil., which has been used as an anti-diabetes medicine in Brazil, had potent inhibitory activity. The IC50 for the A. humile A. St.-Hil. extract ($91.2{\mu}g/mL$) was similar to that of acarbose ($50.5{\mu}g/mL$). This activity of A. humile A. St.-Hil. was not reduced by heat or acid treatment. Moreover, treatment with HCl (0.01 M) for 1 h increased the inhibitory activity from 57.5% to 81.2%. Also, the extract did not cause hemolysis of human red blood cells at levels up to 1 mg/mL. The results indicate that the extract of A. humile A. St.-Hil. is potentially useful as an anti-acidosis and anti-diabetes agent.

Anti-diabetic Effects of Mixed Extracts from Lycium chinense, Cordyceps militaris, and Acanthopanax senticosus (지골피, 동충하초, 가시오가피 혼합 추출물의 항당뇨 작용)

  • Kim, Dae-Jung;Kim, Jeong-Mi;Kim, Tae-Hyuck;Baek, Jong-Mi;Kim, Hyun-Sook;Choe, Myeon
    • Korean Journal of Plant Resources
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    • v.23 no.5
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    • pp.423-429
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    • 2010
  • In this study, we examined the anti-diabetic activity in vitro by the mixed Korean herb water extracts(JDG) composed of Lycium chinense, Cordyceps militaris, and Acanthopanax senticosus on hepatic glucose-regulating enzyme activities such as glucokinase(GK), acetyl-CoA carboxylase(ACC), and inhibition activity of $\alpha$-glucosidase. The hepatic cytosol fraction of a type II diabetic animal(Goto-Kakizaki rat) was used in GK and ACC activity assays. JDG mixed water extracts significantly increased the hepatic GK and ACC activity. The highest anti-$\alpha$-glucosidase activity was observed in JDG 5 water extract when compared to the acarbose control, inhibitor of $\alpha$-glucosidase. We suggest that Lycium chinense, Cordyceps militaris, and Acanthopanax senticosus mixed water extracts may exert an anti-diabetic activity by enhancing the glucose metabolism and may be used as natural $\alpha$-glucosidase inhibitors in type 2 diabetic conditions.

Diagnostic Device Model for Insecticide susceptibilities of Beet Armyworm, Spodoptera exigua(Hubner) (파밤나방(Spodoptera exigua (Hiibner)) 살충제 감수성 진단장치모형)

  • 김용균;이준익;강성영;한상찬
    • Korean journal of applied entomology
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    • v.38 no.1
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    • pp.53-57
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    • 1999
  • Simple diagnostic kits for monitoring insecticide susceptibility of beet armyworm, Spodoptera exigua (Hiibner) were developed and applied to the field populations. The operation of the kits was based on the correlations between enzyme activities of esterase (EST) and acetylcholinesterase (AChE) and the insecticide susceptibilities. Four different kinds of diagnostic kits (ED, EM, AD, and AM) were designed and classified by diagnostic enzymes (E for esterases and A for acetylcholinesterase) and inhibitors (D for dichlorvos and M for monocrotophos). Diagnostic inhibitor concentrations were 1 mM for ED, 10 mM for EM, 100 mM for AD, and 100 mM for AM. Resistant larvae which were not inhibited by the diagnostic amounts of insecticides developed positive staining (red color), but susceptible~ s howed negative (no color). An insect was used for both EST and AChE diagnostic kits, but different in their samples: hemolymph for EST and the head for AChE. These four diagnostic kits were applied to 1 1 different populations which showed variations of insecticide susceptibilities. Four kits were different in the capability discriminating the insecticide susceptibilites according to insecticides: ED to bifenthrin, AD to methomyl, and ED and AM to chlorpyrifos-methyl. These diagnostic devices can be used for insecticide-resistance management program for this insect pest. It also provide a technical guide to insect pest management for farmers, directors, and researchers.

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