• Title/Summary/Keyword: Inhibitory Activity

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Antioxidant and Alpha-Glucosidase Inhibitory Activity of Strychnos nux-vomica Extracts (마전자 추출물의 항산화 및 Alpha-Glucosidase 저해 활성)

  • Lee, Jeung-Min;Park, Jae-Hee;Park, Hae-Ryong;Park, Eun-Ju
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.39 no.9
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    • pp.1243-1248
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    • 2010
  • The physiological activities of Strychnos nux-vomica extracts were investigated through the total phenolic contents (TPC), 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity (RSA), comet assay, and $\alpha$-glucosidase inhibitory activity. S. nux-vomica extracts were prepared with methanol, ethanol, and acetone. The methanol extract showed the highest phenolic content (71 mg/100 g gallic acid equivalents). Pretreatment with S. nux-vomica extracts resulted in significant reductions in oxidative DNA damage at all of the concentrations tested ($1{\sim}50\;{\mu}g/mL$). The $\alpha$-glucosidase inhibitory activity of a methanol extract was 12.8% at the concentration of 1 mg/mL. Therefore, these results indicate that S. nux-vomica might be a noble potential candidate exhibiting antioxidant and $\alpha$-glucosidase inhibitory activity.

Purification and Characterization of Serine Protease Inhibitors from Dolichos lablab Seeds; Prevention Effects on Pseudomonal Elastase-Induced Septic Hypotension

  • Koo, Sun-Hyang;Choi, Yun-Lim;Choi, Su-Kyung;Shin, Young-Hee;Kim, Byeong-Gee;Lee, Bok-Luel
    • BMB Reports
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    • v.33 no.2
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    • pp.112-119
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    • 2000
  • Three kinds of serine protease inhibitors, members of the Bowman-Birk trypsin inhibitor, were purified from Dolichos lablab seeds and named Dolichos protease inhibitor 1, 2 and 3 (DI-1, DI-2 and DI-3), respectively. Each inhibitor showed a single band with gel mobility at around 15.9, 12.1 and 14.6 kDa on 20% SDS-PAGE under reducing conditions. To characterize inhibitory specificity, the inhibition constant (Ki) for these inhibitors was measured against several known serine proteases. All three Dolichos protease inhibitors (DI-1, DI-2 and DI-3) inhibited the activity of trypsin and plasmin, but had no effect on thrombin and kallikrein (either for human plasma kallikrein or for porcine pancreas kallikrein). DI-1 inhibited chymotrypsin most effectively (Ki = $3.6{\times}10^{-9}\;M$), while DI-2 displayed inhibitory activity for porcine pancreatic elastase (Ki = $6.2{\times}10^{-8}\;M$). Pre-treatment of the 33 mg/kg of DI-mixture (active fractions from $C_{18}$ open column chromatography that included DI-1, DI-2 and DI-3) inhibited the induction of pseudomonal elastase-induced septic hypotension and prevented an increase in bradykinin generation in pseudomonal elastase-treated guinea pig plasma. Also, the increase of kallikrein activity, by injection of pseudomonal elastase, was inhibited by the pretreatment of the DI-mixture in a guinea pig. Since the DI-mixture had no inhibitory effect on kallikrein activity when Z-Phe-Arg-MCA was used as a substrate in vitro, its inhibitory activity in the pseudomonal elastase-induced septic hypotension model might not be due to a direct inhibition of plasma kallikrein in the activation cascade of the Hageman factor and prekallikrein system. These results suggest that the Dolichos DI-mixture might be used as an inhibitor in pathogenic bacterial protease-induced septic shock.

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The antiproliferative activity of cannabidiol ethyl ethers against human ora epitheloid carcinoma cells

  • Baek, Seung-Hwa;Kang, Kil-Ung;Chung, Soon-Ryang;Kim, Hyung-Min;Chung, Woo-Young;Han, Du-Seok
    • Advances in Traditional Medicine
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    • v.1 no.1
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    • pp.45-54
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    • 2000
  • Cannabidiol derivatives (1, 2 and 3), and 5-fluorouracil (4, 5-FU) were tested for their growth inhibitory effects against human oral epitheloid carcinoma cell lines (KB) using two different 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay and sulforhodamine B protein (SRB) assay. These compounds showed a potent inhibitory activity in vitro in the micromolar range against KB cell lines. In general, the antitumor activity of these compounds (1, 2, 3 and 4) was in a dose-dependent over the micromolar concentration ranges from $1\;{\mu}M\;to\;100\;{\mu}M$. The comparison of $IC_{50}$ values of these compounds in tumor cell lines shows that their susceptibility to these compounds decreases in the following order: CBD > 5-FU > CBDME > CBDDE by the MTT assay and SRB assay. Cannabidiol derivatives (1, 2 and 3), and 5-FU were tested for their cytotoxic effects on NIH 3T3 fibroblasts using two different MTT assay and SRB assay. These compounds exhibited potent cytotoxic activities in vitro in the micromolar range against NIH 3T3 fibroblasts. In general, the cytotoxic activities of these compounds (1, 2, 3 and 4) were in a dose-dependent over the micromolar concentration range $1\;{\mu}M\;to\;100\;{\mu}M$. The comparison of $CD_{50}$ values of these compounds on NIH 3T3 fibroblasts shows that their susceptibility to these compounds decreases in the following order; CBD > 5-FU > CBDDE > CBDME by MTT assay, CBD > 5-FU > CBDME > CBDDE by SRB assay. These results suggest that cannabidiol (1, CBD) retains the most growth-inhibitory activity against KB cell lines.

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Protective Effect against Neuronal Cell and Inhibitory Activity against Bacteria of Mulberry Fruit Extracts (오디 추출물의 신경세포 보호활성 및 항균활성)

  • Kim Hyun-Bok;Kim Sun-Yeou;Lee Hang-Young;Kim Sun-Lim;Kang Seok-Woo
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.50 no.spc1
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    • pp.220-223
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    • 2005
  • As functional evaluation of mulberry fruits extracts, the protective effect on cerebral cell and antibacterial activities were carried. $1\%$ HCl-MeOH extract showed $37\%$ cytoprotective effect on hydrogen peroxide, also C3G identified mulberry fruits and cyanidin showed $52\%,\;76\%$, respectively, protective effects on oxygen-glucose deprivation (OGD). In the antibacterial activity of mulberry fruit extracts, MeOB-Cheongil extract showed the highest inhibitory activity. Salmonella typhimurium was shown inhibitory rate more than $70\%$ in all treatment groups. Also Klebsiella pneumoniae was shown inhibitory activity in all treatment groups.

Antioxidant Property and Inhibitory Effects of an Water Extract of Hwang-Ryun-Chung-Sim-Um on the Acetylcholinesterase (황련청심음(黃連淸心飮)의 항산화 및 AChE 억제 효과에 관한 연구)

  • Yoo, Jong-Ho;Lee, Sang-Taek;Han, Yun-Seung;Kim, Geun-Woo;Koo, Byung-Soo;Kim, Hun-Il
    • Journal of Oriental Neuropsychiatry
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    • v.17 no.1
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    • pp.1-16
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    • 2006
  • Objective: An water extract of the Hwang-Ryun-Chung-Sim-Um (HRC) was assessed to determine the mechanisms of its antioxidant activity. In addition, the HRC was examined in vitro for the inhibitory effect on the acetylcholinesterse (AChE). Methods: The HRC exhibited a concentration-treatment; scavenging ${\alpha},{\alpha}-diphenyl-{\beta}-picrylhydrazyl$ (DPPH) radical, linoleic acid oxidation in a thiocyanate assay system, hydroxyl radical-induced DNA nicking. We investigated mRNA levels such as catalase activity, superoxide-dismutase and glutathione peroxidase. The water extract of HRC showed inhibitory effect on AChE activity. Result: The HRC extract showed dose-dependent free radical scavenging activity, including DPPH radicals and hydroxyl radicals, using different system. The HRC was also found to be effective in protecting plasmid DNA against the strand breakage induced by Hydroxyl radicals in Fenton's reaction mixture. Futhermore, catalase mRNA expression levels increased, but SOD1 and MnSOD was not expressed. HRC in a various concentration-dependent decreased AChE mRNA levels and inhibitory effect showed AChE. Conclusion: According to the above results, it is supposed that HRC is applicable to the Dementia-type of Alzheimer clinically.

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Peptic Hydrolysate of Porcine Crude Myosin Has Many Active Fractions Inhibiting Angiotensin I-converting Enzyme

  • Katayama, Kazunori;Fuchu, Hidetaka;Sugiyama, Masaaki;Kawahara, Satoshi;Yamauchi, Kiyoshi;Kawamura, Yukio;Muguruma, Michio
    • Asian-Australasian Journal of Animal Sciences
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    • v.16 no.9
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    • pp.1384-1389
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    • 2003
  • In order to clarify one of the biological functions of pork, we investigated whether a peptic hydrolysate of denatured porcine crude myosin showed inhibitory activity against angiotensin I-converting enzyme (ACE), which contributed to hypertension. Our results indicated that this hydrolysate showed relatively strong activity, and we therefore attempted to separate the involved peptides, which were considered to be active substances. To isolate these active peptides, the hydrolysate was separated using a solidphase separation, gel filtration high-performance liquid chromatography (HPLC), and two kinds of reverse phase HPLC. In each stage of separation, many fractions were detected, almost all of which showed ACE inhibitory activity. Thus, we suggested that the activity of the hydrolysate as a whole was a result of the activities of the many individual peptides. Six peaks were distinguished, with yields from 34 to 596 ppm of original crude myosin. In addition to the six peaks, many other active fractions were found throughout the separation steps, strongly suggesting that whole porcine crude myosin itself had ACE inhibitory activity. Moreover, pork as food was considered to function as an ACE inhibitory material in vivo, because pork proteins consist primarily of crude myosin, which included almost all the myofibrillar structural proteins.

Angiotensin I Converting Enzyme Inhibitory Effect of Doenjang Fermented by B. subtilis SCB-3 Isolated from JeJu, Korean Traditional Food (메주 유래의 B. subtilis SCB-3으로 제조된 된장의 Angiotensin I Converting Enzyme 저해효과)

  • 황종현
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.26 no.5
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    • pp.775-783
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    • 1997
  • Morphologically different 18 strains were isolated and examined for their abilities to inhibit ACE. Those strains were cultured in the medium containing 10% of soybean extract at 37$^{\circ}C$ for 48hr or fermented with boiled soybean at 3$0^{\circ}C$ for 60 days. The concentration of inhibitors to inhibit 50% of ACE activity, $IC_{50}$ was measured on the culture broth of each strain and also on the hot-water extract from 20, 40 and 60 day fermented Doenjang by each strain. As a result, SCB-3 which is isolated from Meju showed the highest ACE inhibitoryactivity on the cultured broth and 40 day matured Doenjang. Then, $IC_{50}$ of SCB-3 was 0.02 mg/ml and 0.26mg/ml respectively. SCB-3 was identified as a Bacillus subtilis based upon its morphological, biochemical and physiological properties. Changes in general components and ACE inhibitory activity of Doenjang fermented by SCB-3 were examined during 90 days. Total acidity of Doenjang was increased from 1.39% to 1.66% and pH was decreased from 6.02 to 5.79 after 90 days fermentation. Total sugar contents were decreased from 16.4% to 15.1% and reducing sugar contents was also decreased from 2.45% to 1.62%. Total nitrogen contents were nearly not changed, but amino nitrogen contents were drastically increased from 196mg% to 541mg%. The numbers of total microorganism were increased to 1.1$\times$$10^{8}$ cells/g after 45 days. Protease activity was increased to 622.1U/g after 75 days. The highest ACE inhibitory activity was shown in 60 day fermented Doenjang and $IC_{50}$ of the hot-water extract was 0.31mg/ml.

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Fermentation of purple Jerusalem artichoke extract to improve the α-glucosidase inhibitory effect in vitro and ameliorate blood glucose in db/db mice

  • Wang, Zhiqiang;Hwang, Seung Hwan;Lee, Sun Youb;Lim, Soon Sung
    • Nutrition Research and Practice
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    • v.10 no.3
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    • pp.282-287
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    • 2016
  • BACKGROUND/OBJECTIVES: Jerusalem artichoke has inhibitory activity against ${\alpha}$-glucosidase and decreases fasting serum glucose levels, which may be related to its fructan content. The biological activity of fructan can be influenced by the degree of polymerization. Thus, in this study, the inhibitory effects of original and fermented purple Jerusalem artichoke (PJA) on ${\alpha}$-glucosidase were compared in vitro. Additionally, the anti-diabetes effect of Lactobacillus plantarum-fermented PJA (LJA) was studied in a non-insulin-dependent diabetes mellitus animal model (C57BIKsJ db/db). MATERIALS/METHODS: The water extract of PJA was fermented by L. plantarum, and two strains of Bacillus subtilis to compare their anti-${\alpha}$-glucosidase activities in vitro by ${\alpha}$-glucosidase assays. The anti-diabetes effect of LJA was studied in a non-insulin-dependent diabetes mellitus animal model (C57BIKsJ db/db) for seven weeks. During the experiment, food intake, body weight, and fasting blood glucose were measured every week. At the end of the treatment period, several diabetic parameters and the intestinal ${\alpha}$-glucosidase activity were measured. RESULTS: The LJA showed the highest ${\alpha}$-glucosidase inhibitory activity in vitro. In the in vivo study, it resulted in a significantly lower blood glucose concentration than the control. Serum insulin and HDL cholesterol levels were significantly higher and the concentrations of triglycerides, non-esterified fatty acids, and total cholesterol were significant lower in mice treated with LJA after seven weeks. In addition, the intestinal ${\alpha}$-glucosidase activity was partially inhibited. CONCLUSIONS: These results suggested that LJA regulates blood glucose and has potential use as a dietary supplement.

Effect of Temperature and pH on Trypsin Inhibitory Activity of Ethanol Extracts from Ecklonia cava (감태 에탄올 추출물의 Trypsin 저해활성에 대한 열 및 pH의 영향)

  • Jeong, Hee-Ye;Kim, Koth-Bong-Woo-Ri;Jung, Seul-A;Kim, Hyun-Jee;Jeong, Da-Hyun;Lee, Ga-Yeong;Kang, Bo-Kyeong;Bark, Si-Woo;Kim, Tae-Wan;Cho, Young-Je;Ahn, Dong-Hyun
    • KSBB Journal
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    • v.27 no.6
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    • pp.330-334
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    • 2012
  • This study was performed to investigate the inhibitory activity of ethanol extract from Ecklonia cava (EE-EC) against trypsin and the stability of this activity under various heat and pH conditions. As a results, The EE-EC showed trypsin inhibitory activity of 77, 54, and 32% at concentrations of 5, 2.5, and 1 mg/mL and was not affected by the heat treatment conditions used in this study. Whereas trypsin inhibitory activity of EE-EC was stable in the pH range of 2-8, but decreased with pH treatment of pH 10 compared with the control. Therefore, the EE-EC could be useful as a natural and functional agent.

Screening of Antioxidative, Anti-platelet Aggregation and Anti-thrombotic Effects of Clove Extracts (정향 추출물의 항산화.항혈소판 응집효과 및 혈전 용해능 탐색)

  • Yang, Young-Yi;Lee, Min-Ja;Lee, Hye-Sook;Park, Won-Hwan
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.25 no.3
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    • pp.471-481
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    • 2011
  • Clove has been frequently used as anti-diabetic, anti-microbial, anti-inflammatory, anesthetic drug and remedies for stomachache by coldness. In this study, the antioxidant activity of extract from Clove was studied in vitro methods by measuring the antioxidant activity by TEAC, measuring the scavenging effects on reactive oxygen species (ROS) [superoxide anion, hydroxyl radical] and on reactive nitrogen species (RNS) [nitric oxide and peroxynitrite] as well as measuring the inhibitory effect on $Cu^{2+}$-induced human LDL oxidation. Anti-platelet aggregation and anti-thrombotic effects of Clove extracts were studied ex vivo methods by mesuring the inhibitory effect on thrombin induced platelet aggregation and the fibrinolytic activity. The Clove extracts were found to have a potent scavenging activity, as well as an inhibitory effect on LDL oxidation in vitro. Moreover Clove extracts were exhibited remarkable inhibitory effect on platelet aggregation and fibrinolytic activity. In conclusion, the Clove extracts have anti-oxidative and anti-atherosclerotic effects in vitro and ex vivo system, which can be used for developing pharmaceutical drug against oxidative stress and atherosclerosis.