• Title/Summary/Keyword: Inhibitory Activity

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Optimization of Whey-Based Medium for Growth and ACE-Inhibitory Activity of Lactobacillus brevis

  • Ahn, Jae-Eun;Park, Seung-Yong;Lee, Byong-H.
    • Journal of Dairy Science and Biotechnology
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    • v.25 no.1
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    • pp.1-7
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    • 2007
  • A Whey-based medium was formulated with Lactobacillus brevis to investigate whether any functional peptides could derive from whey protein. The optimal concentrations of the ingredients of the medium for the growth of Lactobacillus were determined as 2% whey protein concentrate and 1% glucose and 0.5% yeast extracts. The growth of Lb. brevis was improved with the supplementation of yeast extracts than glucose. The viable cells counts of Lb. brevis reached to 2.0 × 10$^8$CFU/mL in the whey-based medium. The whey protein hydrolysates recovered from the supernatant after centrifugation at 10,000 x g for 10min induced strong inhibitory activity against ACE. When the whey protein hydrolysate were partially purified by a membrane tubing below 8,000Da, the partially purified fraction remained 64.7 ${\pm}$ 3.6% of the ACE inhibition activity of the whey protein hydrolysates and IC$_{50}$ was 38.8 ${\pm}$ 2.2mg/mL. The whey-based medium was proved to be effective in producing ACE inhibitory peptides by lactic bacteria fermented whey protein.

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Chromatographic Fractionation of Protease Inhibitors from Fish Eggs (어류 알로부터 Protease Inhibitors의 크로마토그래피법에 의한 분획)

  • Kim, Jin-Soo;Kim, Ki Hyun;Kim, Hyeon Jeong;Kim, Min Ji;Park, Sung Hwan;Lee, Hyun Ji;Heu, Min Soo
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.46 no.4
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    • pp.351-358
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    • 2013
  • A protease inhibitor from fish eggs was fractionated using chromatographic methods. The fractionation efficiency was evaluated in terms of specific inhibitory activity (SIA, U/mg), purity (fold), total inhibitory activity (TIA, U), and recovery (%). The protease inhibitor (PI) from egg extracts of skipjack tuna (ST Katsuwonus pelamis), yellowfin tuna (YT Thunnus albacares) and Alaska pollock (AP Theragra chalcogramma) was fractionated using Sephadex G-50 gel filtration and DEAE-Sepharose CL-6B anion exchange chromatography based on protein size exclusion and net charge, respectively. Fractions exhibiting strong inhibitory activity were contained in the 30-50 kDa fraction on gel filtration and in the range of 0.4-0.7 M NaCl gradient fraction on anion exchange chromatography. The respective TIA and percent recovery of the fraction obtained with gel filtration toward trypsin and $N{\alpha}$-benzoyl-L-arginine-p-nitroanilide (BAPNA) were 2,758.7 U and 29.6% for ST, 1,005.5 U and 25.6% for YT, and 1,267.5 U and 26.0% for AP. Gel filtration chromatography was more effective at fractionating PI than using ion exchange chromatography. These results suggest that fish eggs act as serine protease inhibitors and might be useful for protease inhibition in foodstuffs.

Lipoxygenase Inhibitory Activity of Korean Indigenous Mushroom Extracts and Isolation of an Active Compound from Phellinus baumii

  • Lee, Seung Woong;Song, Ja-Gyeong;Hwang, Byung Soon;Kim, Dae-Won;Lee, Yoon-Ju;Woo, E-Eum;Kim, Ji-Yul;Lee, In-Kyoung;Yun, Bong-Sik
    • Mycobiology
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    • v.42 no.2
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    • pp.185-188
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    • 2014
  • We investigated a total of 335 samples of Korean native mushroom extracts as part of our lipoxygenase (LOX) inhibitor screening program. Among the mushroom-methanolic extracts we investigated, 35 exhibited an inhibitory activity greater than 30% against LOX at a concentration of 100 ${\mu}g/mL$. Especially, Collybia maculata, Tylopilus neofelleus, Strobilomyces confusus, Phellinus gilvus, P. linteus, P. baumii, and Inonotus mikadoi exhibited relatively potent LOX inhibitory activities of 73.3%, 51.6%, 52.4%, 66.7%, 59.5%, 100.0%, and 85.2%, respectively. Bioassay-guided fractionation led to the isolation of inoscavin A from the methanolic extract of P. baumii, which showed the most potent activity and was identified by spectroscopic methods. Specifically, inoscavin A exhibited potent LOX inhibitory activity with an $IC_{50}$ value of $6.8{\mu}M$.

Preventive Effects of Santalum album L. Extracts on Oxidation, Platelet Aggregation and Thrombosis (백단향추출물의 항산화, 항혈소판 응집 및 혈전 용해능에 관한 연구)

  • Sung, Yung-Wei;Lee, Ji-Hyun;Song, Kyoo-Ju;Koo, Byung-Soo;Kim, Geun-Woo
    • Journal of Oriental Neuropsychiatry
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    • v.23 no.1
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    • pp.115-128
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    • 2012
  • Objectives : To evaluate the in vitro scavenging activity, inhibitory effect of LDL oxidation of pro-oxidant reactive species, anti-platelet aggregative effects and anti-thrombosis effects in response to treatment with SA using various screening methods including biological and non-biological oxidants. Methods : The antioxidant activity concerning extract from SA was studied with 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 and the inhibitory effect on thrombin-induced platelet aggregation and thrombosis. Results : SA extracts were found to have a potent scavenging activity regarding oxidative stress as well as an inhibitory effect towards LDL oxidation, platelet aggregation, and thrombosis. Conclusions : The SA extracts have anti-oxidative and anti-atherosclerotic effects in vitro system, which can be used for developing pharmaceutical drugs against oxidative stress and atherosclerosis.

Screening of ${\alpha}$-Glucosidase Inhibitory Activity of Vietnamese Medicinal Plants : Isolation of Active Principles from Oroxylum indicum

  • Nguyen, Mai Thanh Thi;Nguyen, Nhan Trung;Nguyen, Hai Xuan;Huynh, Thuy Nghiem Ngoc;Min, Byung-Sun
    • Natural Product Sciences
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    • v.18 no.1
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    • pp.47-51
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    • 2012
  • Among 38 Vietnamese medicinal plant extracts investigated for their ${\alpha}$-glucosidase inhibitory activity, 35 extracts showed $IC_{50}$ values below $250{\mu}g/mL$. The MeOH extracts of the heartwood of Oroxylum indicum, the seeds of Caesalpinia sappan, and the fruits of Xanthium strumarium exhibited strong ${\alpha}$-glucosidase inhibitory activity with $IC_{50}$ values less than $50{\mu}g/mL$. Fractionation of the MeOH extract of the heartwood of O. indicum led to the isolation of oroxylin A (1), oroxyloside (2), hispidulin (3), apigenin (4), ficusal (5), balanophonin (6), 2- (1-hydroxymethylethyl)-4H,9H-naphtho[2,3-b]furan-4,9-dione (7), salicylic acid (8), p-hydroxybenzoic acid (9), protocatechuic acid (10), isovanillin (11), and ${\beta}$-hydroxypropiovanillon (12). Compounds 1 - 3, 5, 6, 8, 10, and 12 showed more potent activities, with $IC_{50}$ values ranging from 2.13 to $133.51{\mu}M$, than a positive control acabose ($IC_{50}$, $241.85{\mu}M$). The kinetic study indicated that oroxyloside (2) displayed mixed-type inhibition with inhibition constant (Ki) was $3.56{\mu}M$.

Analysis of Nutritional Characteristics and Physiological Functionality of Hypsizygus marmoreus (Brown cultivar) (갈색 느티만가닥버섯의 영양특성 및 생리기능성 분석)

  • Bolormaa, Zanabaatar;Kang, Min-Gu;Seo, Geon-Sik;Lee, Young-Wook;Lee, Jong-Soo
    • The Korean Journal of Mycology
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    • v.40 no.2
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    • pp.104-108
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    • 2012
  • In order to apply into functional food or medicinal industry, nutritional characteristics and physiological functionality of Hypsizygus marmoreus (brown cultivar) were investigated. Fruiting body of H. marmoreus contained 27.3% of crude protein, 55.8% of total sugar and 11,109.3 mg/100 g dry weight of malic acid. Furthermore, 66.7% of antihypertensive angiotensin I-converting enzyme (ACE) inhibitory activity and 37.3% of antigout xanthin oxidase inhibitory activity showed in the water extract from H. marmoreus. The economically ACE inhibitory activity (81.4%) was obtained when the fruiting body of Hysizygus marmoreus was extracted with distilled water of $50^{\circ}C$ for 12 h, even though maximal ACE inhibitory activity (84.4%) was showed the extracts from $70^{\circ}C$ for 12 h.

Screening of Herbal Medicines from China and Vietnam with Inhibitory Activity on Advanced Glycation End Products (AGEs) Formation (VIII) (중국.베트남 약용식물의 최종당화산물 생성저해활성 검색(VIII))

  • Choi, So-Jin;Song, Yoo Jin;Kim, Young Sook;Kim, Joo Hwan;Hang, Sun;Tran, The Bach;Kim, Jin Sook
    • Korean Journal of Pharmacognosy
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    • v.43 no.4
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    • pp.338-344
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    • 2012
  • Advanced glycation end products (AGEs) have been postulated to play a central role in the development of diabetic complications. A variety of different agents that inhibit AGEs have been under investigation. In this study, 62 herbal medicines from China and Vietnam have been investigated with an in vitro evaluation system using AGEs formation inhibitory activity. Of these, 5 herbal medicines ($IC_{50}$ < $5{\mu}g/ml$) were found to have significant AGEs formation inhibitory activity. Particularly, herbal medicines Albizia odoratissima (twigs and leaves), Rhododendron spinuliferum (twigs and leaves), Dioscorea cirrhosa (stems and leaves), Illicium verum (stems and leaves) and Aglaia perviridis (stems and leaves), showed more potent inhibitory activity (approximately 16-26 fold) than the positive control aminoguanidine ($IC_{50}=76.47{\mu}g/ml$).

Inhibitory Activity of Aralia elata Leaves on Protein Tyrosine Phosphatase 1B and α-Glucosidase (참두릅 잎의 Protein Tyrosine Phosphatase 1B와 α-Glucosidase 저해 활성)

  • Cho, Yoon Sook;Seong, Su Hui;Bhakta, Himanshu Kumar;Jung, Hee Jin;Moon, Kyung Ho;Choi, Jae Sue
    • Korean Journal of Pharmacognosy
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    • v.47 no.1
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    • pp.29-37
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    • 2016
  • Anti-diabetic potential of the leaves of A. elata through the inhibitory activity on PTP1B and ${\alpha}$-glucosidase has not been reported. In this study, the EtOAc fraction of methanolic extract from the leaves of A. elata showed potent inhibitory activity against the PTP1B and ${\alpha}$-glucosidase with $IC_{50}$ value of $96.29{\pm}0.3$ and $264.71{\pm}14.87{\mu}g/mL$, respectively. Three known triterpenoids, oleanolic acid, oleanolic acid-28-O-${\beta}$-D-glucopyranoside and oleanolic acid-3-O-${\beta}$-D-glucopyranoside were isolated from the most active EtOAc fraction. We determined the chemical structure of these triterpenoids through comparisons of published nuclear magnetic resonance (NMR) spectroscopic data. Furthermore, we screened these triterpenoids for their ability to inhibit PTP1B and ${\alpha}$-glucosidase over a range of concentrations ($12.5-50{\mu}M$). All three terpenoids significantly inhibited PTP1B in a concentration dependent manner and oleanolic acid effectively inhibited ${\alpha}$-glucosidase. In addition, these compounds revealed potent inhibitory activity with negative binding energies toward PTP1B, showing high affinity and tight binding capacity in the molecular docking studies. Therefore, the results of the present study clearly demonstrate that A. elata leaves and its triterpenoid constituents might be beneficial in the prevention or treatment of diabetic disease.

Enhancement of the Anti-hyperglycemic and Antioxidant Activities of Five Selected Beans by the Germination Process (발아에 따른 콩류의 식후 혈당 상승 억제효능과 항산화 활성)

  • Cho, Cha-Young;Choi, Hwang-Yong;Jo, Sung-Hoon;Ha, Kyoung-Soo;Chung, Ji-Sang;Jang, Hae-Dong;Kwon, Young-In
    • The Korean Journal of Food And Nutrition
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    • v.25 no.2
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    • pp.246-252
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    • 2012
  • After a mixed carbohydrate diet, inhibition of ${\alpha}$-amylase and ${\alpha}$-glucosidase involved in the digestion and absorption of carbohydrates can significantly decrease the postprandial increase of blood glucose level. In the course of screening these useful enzyme inhibitors, we selected five kinds of bean, using an in-vitro enzyme inhibition assay method. To evaluate the effect of germination process on the functionality of the bean, we investigated the inhibitory activities of the water extracts of non-germinated bean and germinated bean against ${\alpha}$-amylase and ${\alpha}$-glucosidase, relevant to postprandial hyperglycemia. We also investigated the oxygen radical absorbance capacity(ORAC), total phenolics content, and postprandial blood glucose lowering effect in rats(Sprague-Dawley rat model). Most germinated beans showed significantly higher ${\alpha}$-glucosidase inhibitory activity, compared with non-germinated beans. Among germinated beans, Glycine max had the highest ${\alpha}$-glucosidase inhibitory activity(53.3%). The water extract of germinated Phaseolus vulgaris L. had the highest ${\alpha}$-amylase inhibitory activity(95.1%), followed by Glycine max(58.7%), and Glycine max L. Merr(54.1%). Furthermore, the five germinated beans also showed high antioxidant activities in ORAC assay. Results suggested that the germination process may improve and enhance the anti-hyperglycemia potential and antioxidant activity of the bean.

3D-QSAR Analyses on the Inhibition Activity of 4-Hydroxybenzyl alcohol Analogues Against Tyrosinase (4-Hydroxybenzyl alcohol 유도체들의 Tyrosinase 활성 저해에 대한 3D-QSAR 분석)

  • Kim, Sang Jin;Sung, Nack Do
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.39 no.4
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    • pp.329-335
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    • 2013
  • Three-dimensional quantitative structure-activity relationships (3D-QSARs) models between the substituents with changing groups ($R_1$ & $R_2$) of 4-hydroxybenzyl alcohol (4-HBA) derivatives as substrate molecule and their inhibitory activities against tyrosinase were derived and discussed quantitatively. The optimized CoMSIA FF model showed the best predictability and fitness ($r^2$ = 0.858 & $q^2$ = 0.951). The contour maps of the optimized CoMSIA FF model showed that, the inhibitory activities of the analogues against tyrosinase were expected to increase when hydrophobic (Hy) favor, negative charge (E) favor, steric (S) disfavor and hydrogen bond donor (HD) disfavor groups were substituted at the $R_2$ position. When the hydrogen bond donor (HD) favor groups were substituted at the $R_1$ position, it is predicted that the substituents will be able to increase the inhibitory activity.