• Title/Summary/Keyword: enzyme inhibitors

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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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Effect of ACE Inhibitor on Nephrotic Proteinuria in the Children (ACE inhibitor가 소아 신증후군에서 단백뇨 소실에 미치는 영향)

  • Park, Eun-Hye;Kim, Ji-Hong;Kim, Pyung-Kil
    • Childhood Kidney Diseases
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    • v.3 no.1
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    • pp.42-47
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    • 1999
  • Angiotensin-converting enzyme inhibitors lower urinary protein excretion in hypertensive and normotensive patients with renal disease. Most children with nephrotic syndrome have minimal change histology and the great majority of these patients respond to the treatment with oral prednisone. Here we have studied the effects of combination of Inhibace and oral prednisone in pediatric patients with nephrotic syndrome. 45 patients with nephrotic syndrome were selected. Of these, 29 patients were treated with prednisone(2mg/kg/day) and 16 children were treated with prednisone and Inhibace(2.5mg/day). Urinary protein, blood pressure, creatinine clearance, serum creatinine, serum albumin and serum cholesterol were measured in both control and Inhibace group. Also the duration to remission after treatment was compared in both groups. The amounts of proteinuria before and after treatment were not significantly different in both group. The duration to remission of proteinuria was significantly shorter in Inhibace group compared to that in control group. The changes of blood pressure and creatinine clearance were not significant in Inhibace group. In conclusion, the combination therapy of oral prednisone and ACE inhibitor have shortened the duration to remission of proteinuria in nephrotic syndrome of children.

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Immunomodulatory effect of captopril and local irradiation on myeloid-derived suppressor cells

  • Cho, Won Kyung;Shin, Sung-Won;Kim, Shin-Yeong;Hong, Chang-Won;Choi, Changhoon;Park, Won;Noh, Jae Myoung
    • Radiation Oncology Journal
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    • v.34 no.3
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    • pp.223-229
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    • 2016
  • Purpose: This study is to investigate the effect of captopril when combined with irradiation. Materials and Methods: 4T1 (mouse mammary carcinoma) cells were injected in the right hind leg of Balb/c mice. Mice were randomized to four groups; control (group 1), captopril-treated (group 2), irradiated (group 3), irradiated and captopril-treated concurrently (group 4). Captopril was administered by intraperitoneal injection (10 mg/kg) daily and irradiation was delivered on the tumor-bearing leg for 15 Gy in 3 fractions. Surface markers of splenic neutrophils (G-MDSCs) and intratumoral neutrophils (tumor-associated neutrophils [TANs]) were assessed using flow cytometry and expression of vascular endothelial growth factor (VEGF) and hypoxia-inducible factor 1 alpha ($HIF-1{\alpha}$) of tumor was evaluated by immunohistochemical (IHC) staining. Results: The mean tumor volumes (${\pm}$standard error) at the 15th day after randomization were $1,382.0({\pm}201.2)mm^3$ (group 1), $559.9({\pm}67.8)mm^3$ (group 3), and $370.5({\pm}48.1)mm^3$ (group 4), respectively. For G-MDSCs, irradiation reversed decreased expression of CD101 from tumor-bearing mice, and additional increase of CD101 expression was induced by captopril administration. Similar tendency was observed in TANs. The expression of tumor-necrosis factor-associated molecules, CD120 and CD137, are increased by irradiation in both G-MDSCs and TANs. Further increment was observed by captopril except CD120 in TANs. For IHC staining, VEGF and $HIF-1{\alpha}$ positivity in tumor cells were decreased when treated with captopril. Conclusion: Captopril is suggested to have additional effect when combined to irradiation in a murine tumor model by modulation of MDSCs and angiogenesis.

Inhibitory Effects of Fucoidan on Melanin Synthesis and Tyrosinase Activity (Fucoidan의 멜라닌 합성과 tyrosinase 활성도 억제 효과)

  • Jung, Sook-Hee;Ku, Mi-Jung;Moon, Hee-Jung;Yu, Byeng-Chul;Jeon, Man-Joong;Lee, Yong-Hwan
    • Journal of Life Science
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    • v.19 no.1
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    • pp.75-80
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    • 2009
  • Melanogenesis is a physiological process that results in the synthesis of melanin pigments. Tyrosinase is a key enzyme for melanin biosynthesis, and hyperpigmentation disorders are associated with abnormal accumulation of melanin pigments, which can be improved by treatment with depigmenting agents. Among the possible melanin-reducing compounds, tyrosinase inhibitors are most promising for preventing and treating pigmentation disorder and are used as skin-whitening agents in the cosmetic industry. In the present study, the effects of fucoidan on melanogenesis and tyrosinase activity of B16F10 melanoma cells were investigated. Melanin synthesis and tyrosinase activity in B16F10 melanoma cells were decreased in a dose-dependent manner by fucoidan. Melanin production and tyrosinase activity in B16F10 melanoma cells stimulated by a-melanocyte stimulating hormone (a-MSH) were inhibited by fucoidan with a dose-dependent manner compared to control. Fucoidan inhibited tyrosinase activity of B16F10 melanoma cells with a dose-dependent manner as assessed by 3,4-dihydroxyphenylalanine (DOPA) staining. In conclusion, these findings indicate that fucoidan, which inhibit melanin synthesis and tyrosinase activity, is an effective skin-whitening agent.