• Title/Summary/Keyword: enzyme inhibitory

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Effects of the Deer Antler Extract on Scopolamine-induced Memory Impairment and Its Related Enzyme Activities (녹용 추출물이 치매 동물모델의 기억력 개선과 관련효소 활성에 미치는 효과)

  • Lee, Mi-Ra;Sun, Bai-Shen;Gu, Li-Juan;Wang, Chun-Yan;Fang, Zhe-Ming;Wang, Zhen;Mo, Eun-Kyoung;Ly, Sun-Young;Sung, Chang-Keun
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.38 no.4
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    • pp.409-414
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    • 2009
  • The aim of this study was to investigate the ameliorating effects of deer antler extract on the learning and memory impairments induced by the administration of scopolamine (2 mg/kg, i.p.) in rats. Tacrine was used as a positive control agent for evaluating the cognition enhancing activity of deer antler extract in scopolamine-induced amnesia models. The results showed that the deer antler extract-treated group (200 mg/kg, p.o.) and the tacrine-treated group (10 mg/kg, p.o.) significantly ameliorated scopolamine-induced amnesia based on the Morris water maze test. Although there was no statistical significance of brain ACh contents among the experimental groups, the brain ACh contents of the deer antler extract-treated group was slightly higher than that of the scopolamine-treated group. The inhibitory effect of deer antler extract on the acetylcholinesterase activity in the brain was significantly lower than that of scopolamine-treated group. The tacrine- and the deer antler-treated groups reduced the MAO-B activity compared to the scopolamine-treated group, but not significantly. These results suggest that the deer antler extract could be an effective agent for the prevention of the cognitive impairment induced by cholinergic dysfunction.

Inhibitory Effect against Helicobacter pylori and Biological Activity of Thyme (Thymus vulgaris L.) Extracts (Thyme(Thymus vulgaris L.) 추출물의 Helicobacter pylori 억제효과 및 생리활성)

  • Kim, Jeung-Hoan;Kwon, Jung-Hyo;Lee, Kyeong-Hwan;Chun, Sung-Sook;Kwon, Oh-Jun;Woo, Hi-Seob;Cho, Young-Je;Cha, Won-Seup
    • Applied Biological Chemistry
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    • v.49 no.3
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    • pp.243-247
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    • 2006
  • The biological activity of functional food source with thyme extracts were examined. Total phenol contents in the 60% ethanol extracts $(26.8{\pm}0.35\;mg/g)$ with thyme leaf was higher than water extracts $(25.7{\pm}0.20\;mg/g)$. This HPLC analysis is significant in that physiological activity is related with phenolic compound content such as rosemarinic acid, quercetin and chlorogenic acid. Electron donating ability was shown as 90.1% in the water extracts and 77.7% in the 60% ethanol extracts. Antioxidant protection factor of 60% ethanol extracts was higher than water extracts. Helicobacter pylori of the water extracts from thyme leaves did not have antimicrobial activity, but the 60% ethanol extracts revealed the high antimicrobial activity as 9 mm of clear zone in $50\;{\mu}g/ml$ of phenol content, 10 mm in $100\;{\mu}g/ml$, 13 mm in $150\;{\mu}g/ml$ and 16 mm in $200\;{\mu}g/ml$, respectively. Angiotensin converting enzyme inhibition activity showed no inhibition activity in 60% ethanol extracts but 39.9% inhibition activity in water extracts. Xanthine oxidase inhibition activity showed high inhibition activity at 73.5% in water extracts and 100% in 60% ethanol extracts. The result suggests the development of phenol compound in thyme as anti Helicobacter pylori, antioxidant and anti-gout agents.

Screening of Biologically Active Compound from Edible Plant Sources-IX. Isolation and Identification of Sesquiterpene Lactons Isolated from the Root of Ixeris dentata forma albiflora; Inhibition Effects on ACAT, DGAT and FPTase Activity (식용식물자원으로부터 활성물질의 탐색-IX. 흰씀바귀(Ixeris dentata forma albiflora)뿌리에서 Sesquiterpene Lactone 화합물의 분리 및 구조 동정; ACAT, DGAT 및 FPTase 효소 활성의 저해)

  • Bang, Myun-Ho;Jang, Tae-O;Song, Myoung-Chong;Kim, Dong-Hyun;Kwon, Byoung-Mog;Kim, Young-Kuk;Lee, Hyun-Sun;Chung, In-Sik;Kim, Dae-Keun;Kim, Sung-Hoon;Park, Mi-Hyun;Baek, Nam-In
    • Applied Biological Chemistry
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    • v.47 no.2
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    • pp.251-257
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    • 2004
  • The root of lxeris dentata forma albiflora was extracted with 80% aqueous MeOH and solvent fractionated with EtOAc, n-BuOH and water, successively. From the EtOAc and n-BuOH fractions, four sesquiterpene compounds were isolated through the repeated silica gel and ODS column chromatographies. The chemical structures were determined as zaluzanin C (1), $9{\alpha}-hydroxyguaian-4(l5),10(14),11(13)-triene-6,12-olide$ (2), $3{\beta}-O-{\beta}-D-glucopyranosyl-8{\alpha}-hydroxyguaian-4(15),10(14 )-diene-6,12-olide$ (3), and $3{\beta}-O-{\beta}- D-glucopyranosyl-8{\beta}hydroxyguaian-10(14)-ene-6,12-olide$ (4) through the interpretation of several spectral data including 2D-NMR. Some showed the inhibitory effects on DGAT (Diacylglycerol acyltransferase), ($IC_{50}$ values of 1, 2: 0.13, 0.10 mM), the catalyzing enzymes of the intracellular esterification of diacylglycerol and FPTase (Famesyl-protein transferase), ($IC_{50}$ values of 1, 2: 0.15, 0.18 mM), the farnesylation enzyme for Ras protein charge of cancer promotion.

Antihypertensive Effect of Peptide from Sardine Muscle Hydrolyzate on Mild Hypertensive Subjects (정어리 단백질 유래 펩타이드의 경중 고혈압 환자에 대한 강압효과)

  • Kawasaki, T.;Seki, E.;Osajima, K.;Yoshida, M.;Asada, K.;Matsui, T.;Osajima, Y.
    • Proceedings of the Korean Society of Food Hygiene and Safety Conference
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    • 2004.11a
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    • pp.50-58
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    • 2004
  • Valy-Tyrosine (VY) derived from alkaline pretense hydrolyzate of sardine muscles showed the in vitro Angiotensin I converting enzyme (ACE) inhibitory activity and the in vivo antihypertensive effect in SHR. We investigated the antihypertensive effect of the VY on mild hypertensive subjects including subjects with high-normal blood pressure using a randomized double-blind placebo-controlled study. (1) Nineteen subjects (Age 48.9${\pm}$4.3, M/F;18/1) took a 100ml drink either containing 125${\mu}$g of VY or placebo twice daily for 4 weeks. The reductions of the systolic (SBP) and diastolic blood pressure (DBP) were observed in mild hypertensive subjects (n=5) with averages of 17.8${\pm}$2.5 mmHg (p<0.01 vs placebo) and 11.0${\pm}$2.0 mmHg(p<0.05 vs placebo), respectively. Neither SBP nor DBP changed in the subjects of both the placebo group and the high-normal blood pressure group. (2) A randomized double-blind cross-over placebo-controlled study was carried out in 10 mild essential hypertensive subjects (Age 50.6${\pm}$4.6, M/F;10/0). They took a 100ml drink either containing 62.5${\mu}$g of VY or placebo twice daily for 4 weeks alternatively with a 6-week interval. The percent changes in SBP and DBP were -6.9 % and -5.8 % (p<0.05) one week after the VY drink administration, respectively. No adverse effects such as coughing or allergic phenomena could be observed in any of the subjects of drinking VY during the experimental period. These results suggest that the drink containing at least 125${\mu}$g/day of VY may have a significant antihypertensive effect on mild hypertensive subjects without any adverse effects.

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Variation in bioactive principles and bioactive compounds of Rosa rugosa fruit during ripening (해당화 열매 성숙단계에 따른 생리활성 및 기능성 물질 변화 분석)

  • Kwak, Minjeong;Eom, Seung Hee;Gil, Jinsu;Kim, Ju-Sung;Hyun, Tae Kyung
    • Journal of Plant Biotechnology
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    • v.46 no.3
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    • pp.236-245
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    • 2019
  • Fruit ripening is a genetically programmed process involving a number of biochemical and physiological processes assisted by variations in gene expression and enzyme activities. This process generally affects the phytochemical profile and the bioactive principles in fruits and vegetables. To appraise the variation in bioactive principles of fruits from Rosa rugosa during its ripening process, we analyzed the changes in antioxidant and anti-elastase activities and polyphenolic compounds during the four ripening stages of fruits. Overall, an extract of unripe fruits contained the highest levels of total phenolic and flavonoid contents, radical scavenging activity, reducing power, oxygen radical antioxidant capacity, and elastase inhibitory activity, compared with the extracts of fruits at other stages of ripening. Additionally, we found that the reduction of flavonoid content occurs because of decreased transcriptional levels of genes involved in flavonoid biosynthesis pathway during the ripening process. Based on HPLC analysis, we found that the extract of unripe fruits contained the highest amount of myricetin, caffeic acid, chlorogenic acid, syringic acid, and p-coumaric acid and suggested that the antioxidant and anti-elastase activities of the extract obtained from stage 1, should be mediated by the presence of these compounds. Additionally, we analyzed the interaction sites and patterns between these compounds and elastase using the structure-based molecular docking approach, and suggested that chlorogenic acid strongly interacted with elastase. Together, these findings suggest that the maturity of fruits has profound effects on the pharmaceutical value of R. rugosa.

A Novel Synthesized Tyrosinase Inhibitor, (E)-3-(4-hydroxybenzylidene) chroman-4-one (MHY1294) Inhibits α-MSH-induced Melanogenesis in B16F10 Melanoma Cells (신규 합성물질 (E)-3-(4-하이드록시벤질리딘)크로마논 유도체의 티로시나아제 효소활성 저해 및 멜라닌 생성 억제 효과)

  • Jeon, Hyeyoung;Lee, Seulah;Yang, Seonguk;Bang, EunJin;Ryu, Il Young;Park, Yujin;Jung, Hee Jin;Chung, Hae Young;Moon, Hyung Ryong;Lee, Jaewon
    • Journal of Life Science
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    • v.31 no.8
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    • pp.719-728
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    • 2021
  • Melanin pigments are abundantly distributed in mammalian skin, hair, eyes, and nervous system. Under normal physiological conditions, melanin protects the skin against various environmental stresses and acts as a physiological redox buffer to maintain homeostasis. However, abnormal melanin accumulation results in various hyperpigmentation conditions, such as chloasma, freckles, senile lentigo, and inflammatory pigmentation. Tyrosinase, a copper-containing enzyme, plays an important role in the regulation of the melanin pigment biosynthetic pathway. Although several whitening agents based on tyrosinase inhibition have been developed, their side effects, such as allergies, DNA damage, mutagenesis, and cytotoxicity of melanocytes, limit their applications. In this study, we synthesized 4-chromanone derivatives (MHY compounds) and investigated their ability to inhibit tyrosinase activity. Of these compounds, (E)-3-(4-hydroxybenzylidene)chroman-4-one (MHY1294) more potently inhibited the enzymatic activity of tyrosinase (IC50 = 5.1±0.86 μM) than kojic acid (14.3±1.43 μM), a representative tyrosinase inhibitor. In addition, MHY1294 showed competitive inhibitory action at the catalytic site of tyrosinase and had greater binding affinity at this site than kojic acid. Furthermore, MHY1294 effectively inhibited α-melanocyte stimulating hormone (α-MSH)-induced melanin synthesis and intracellular tyrosinase activity in B16F10 melanoma cells. The results of the present study indicate that MHY1294 may be considered as a candidate pharmacological agent and cosmetic whitening ingredient.

Inhibitory effect of water-soluble mulberry leaf extract on hepatic lipid accumulation in high-fat diet-fed rats via modulation of hepatic microRNA-221/222 expression and inflammation (고지방식이 급여 쥐에서 수용성 뽕나무 잎 추출물의 간 microRNA-221/222 발현 및 염증 조절을 통한 간 지질 축적억제 효과)

  • Lee, Mak-Soon;Kim, Cheamin;Ko, Hyunmi;Kim, Yangha
    • Journal of Nutrition and Health
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    • v.55 no.2
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    • pp.227-239
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    • 2022
  • Purpose: This study investigated the effects of water-soluble mulberry leaf extract (ME) on hepatic lipid accumulation in high-fat diet-fed rats via the regulation of hepatic microRNA (miR)-221/222 and inflammation. Methods: Male Sprague-Dawley rats (4 weeks old) were randomly divided into 3 groups (n = 7 each) and fed with 10 kcal% low-fat diet (LF), 45 kcal% high-fat diet (HF), or HF + 0.8% ME for 14 weeks. Lipid profiles and cytokine levels of the liver and serum were measured using commercial enzymatic colorimetric and enzyme-linked immunosorbent assay, respectively. The messenger RNA (mRNA) and miR levels in liver tissue were assayed by real-time quantitative reverse-transcription polymerase chain reaction. Results: Supplementation of ME reduces body weight and improves the liver and serum lipid profiles as compared to the HF group. The mRNA levels of hepatic peroxisome proliferator-activated receptor-gamma, sterol regulatory element binding protein-1c, fatty acid synthase, and fatty acid translocase, which are genes involved in lipid metabolism, were significantly downregulated in the ME group compared to the HF group. In contrast, the mRNA level of hepatic carnitine palmitoyl transferase-1 (involved in fatty acid oxidation) was upregulated by ME supplementation. Furthermore, administration of ME significantly downregulated the mRNA levels of inflammatory mediators such as hepatic tumor necrosis factor alpha (TNF-α), interleukin 6 (IL-6), monocyte chemoattractant protein-1, and inducible nitric oxide synthase. The serum levels of TNF-α, IL-6, and nitric oxide were also significantly reduced in ME group compared to the HF group. Expression of hepatic miR-221 and miR-222, which increase in the inflammatory state of the liver, were also significantly inhibited in the ME group compared to the HF group. Conclusion: These results indicate that ME has the potential to improve hepatic lipid accumulation in high-fat diet-fed rats via modulation of inflammatory mediators and hepatic miR-221/222 expressions.

Anti-wrinkle effects of solvent fractions from Jubak on CCD-986sk (CCD-986sk 세포 내 주박 분획물의 항주름 효능)

  • Young-Ah Jang;Hyejeong Lee
    • Journal of the Korean Applied Science and Technology
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    • v.41 no.2
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    • pp.508-519
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    • 2024
  • In this study, in order to evaluate the possibility of using Jubak as a functional cosmetic material, evaluation of antioxidant activity according to fractions and anti-wrinkle efficacy in CCD-986sk cells, a human fibroblast, were conducted. As a result of confirming the antioxidant activity by measuring ABTS+ radical scavenging ability, Jubak's Ethyl Acetate fractions was found to be 75.5% at a concentration of 1,000 ㎍/ml, showing the highest antioxidant activity among the extraction solvents. The wrinkle improvement effect was confirmed by measuring the inhibitory activity of elastase and collagenase, and in both test results, Jubak's Ethyl Acetate fractions showed the highest efficacy at a concentration of 1,000 ㎍/ml. As a result of measuring the synthesis rate of pro-collagen type I in CCD-986sk cells induced by UVB, Jubak showed the highest efficacy in the order of Ethyl Acetate, Water, Acetonitrile, and Hexan fractions at the same concentration of 20 ㎍/ml. As a result of measuring the inhibition rate of MMP-1, a collagen degrading enzyme, all four solvent fractions showed an efficacy of more than 70% at 20 ㎍/ml. As a result of measuring the mRNA expression levels of pro-collagen type I, MMP-1, and MMP-3 in a real-time PCR experiment, the protein expression level of pro-collagen type I increased when treated with Jubak fractions compared to the UVB group alone. The mRNA expression levels of MMP-1 and MMP-3 were confirmed to be decreased, and Ethyl Acetate fractions was the most effective in improving wrinkles after the control group (EGCG). As a result, it was confirmed that the Ethyl Acetate fractions among Jubak's solvent fractions has an anti-wrinkle effect against photoaging caused by UVB stimulation, and is expected to be used as a natural material for cosmetics.

Whitening activity of Ficus carica L. fruits extract through inhibition of tyrosinase and MITF expression (무화과(Ficus carica L.) 열매 추출물의 tyrosinase 및 MITF 발현 억제를 통한 미백 활성)

  • Min Ji Kim;Si Eun Park;Geun soo Lee;Jin Hwa Kim;Sunwoo Kwon;Hyung Seo Hwang
    • Journal of Applied Biological Chemistry
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    • v.66
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    • pp.204-212
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    • 2023
  • Whitening is inhibitory activity of the melanin synthesis of melanocytes. Recently, whitening materials have been developed on natural materials because of its side effects on skin. Figs (Ficus Carica L.) is a fruit belonging to the Moraceae family and whitening activity was reported in focusing on the fig's stem and leaf components, but whitening activity of the figs fruit was not known. Thus, in this study, we tried to observe its anti-melanogenesis as well as antioxidant and anti-inflammation. The radical scavenging activity of figs fruits extract (FFE) was observed as the level of 34.52±1.98%/60.71±1.26% compared to the control in the its maximum concentration in the DPPH/ABTS assay. Cytotoxicity of FFE was observed at 10% concentration by CCK8 assay, so the maximum concentration was set at 5% and applied to all experiments. FFE concentration dependently decreased NO production associated with inducible nitric oxide synthase, cyclooxygenase-2, interleukin-6 and tumor necrosis factor-α gene expression, these strongly suggesting anti-inflammatory activity. In melanin contents assay, FFE significantly down-regulated melanin production in α-MSH-stimulated B16F10 cell as well as tyrosinase inhibition in vitro. In addition, FFE decreased the Microphthalmia-associated transcription factor (MITF) mRNA expression about 94.34% compared to the α-MSH treatment group in RT-PCR. Finally, FFE significantly reduced the MITF, cAMP response element-binding protein and tyrosinase protein expression in the α-MSH stimulated B16F10 cell. Through these results, we found that FFE can not only directly inhibit tyrosinase enzyme activity but also suppress melanogenesis through regulation of MITF gene expression in α-MSH signal transduction.