• Title/Summary/Keyword: inhibitory

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The Isolation of the Inhibitory Constitutents on Melanin Polymer Formation from the Leaves of Cercis chinensis (박태기나무의 잎으로부터 피부멜라닌 색소생성 억제성분의 분리)

  • Kim, So-Young;Kim, Jin-Joon;Jang, Tae-Soo;Chung, See-Ryun;Lee, Seung-Ho
    • Korean Journal of Pharmacognosy
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    • v.30 no.4
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    • pp.397-403
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    • 1999
  • Tyrosinase plays an important role in the process of melanin polymer biosynthesis. Therefore, the enzyme inhibitors have been of great concern as cosmetics to have skin-whitening effects on the local hyperpigmentation. During the search for new inhibitory compounds on melanin polymer biosynthesis from natural sources, MeOH extracts of 589 higher plants were tested for the inhibitory effect on tyrosinase activity by the muschroom tyrosinase assay in vitro. Among plants tested, the leaves of Cercis chinensis exhibited potent inhibitory effect on mushroom tyrosinase activity. Subsequently seven active compounds were isolated from the ethyl acetate soluble part of acetone extract of the leaves of C. chinensis by the activity guided fractionation monitoring the inhibitory effect on tyrosinase activity. Their chemical structures were identified as $kaempferol-3-0-{\alpha}-L-rhamnoside$, quercitrin, $myricetin-3-0-{\alpha}-L-rhamnoside$, myricetin-3-0-(2'-O-galloyl)- ${\alpha}$ -L-rhamopyranoside (desmanthin), (-)-epicatechin-3-0-gallate, (-)-epigallocatechin-3-0-gallate, and methyl gallate on the basis of the speculation of spectral data and chemical reaction. Among the flavonol rhamnosides, myricetin-3-0-(2'-O-galloyl)- -L-rhamnoside(desmanthin) showed most potent inhibitory effect on tyrosinase activity and the structure of B-ring in flavonol moiety was related to the activity. (-)-Epigallocatechin-3-O-gallate having pyrogallol group in flavan-3-ol moiety exhibited more potent inhibitory effect than (-)-epicatechin-3-0-gallate having catechol group in flavan-3-ol moiety on mushroom tyrosinase activity.

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Antioxidant and angiotensin I-converting enzyme inhibitory activities of northern shrimp (Pandalus borealis) by-products hydrolysate by enzymatic hydrolysis

  • Kim, Sang-Bo;Yoon, Na Young;Shim, Kil-Bo;Lim, Chi-Won
    • Fisheries and Aquatic Sciences
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    • v.19 no.7
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    • pp.29.1-29.6
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    • 2016
  • In the present study, we investigated to the antioxidant and angiotensin I-converting enzyme (ACE) inhibitory activities of the northern shrimp (Pandalus borealis) by-products (PBB) hydrolysates prepared by enzymatic hydrolysis. The antioxidant and ACE inhibitory activities of five enzymatic hydrolysates (alcalase, protamex, flavourzyme, papain, and trypsin) of PBB were evaluated by the 2, 2'-azino-bis [3-ethylbenzothiazoline-6-sulfonic acid] ($ABTS^+$) radical scavenging and superoxide dismutase (SOD)-like activities, reducing power and Li's method for ACE inhibitory activity. Of these PBB hydrolysates, the protamex hydrolysate exhibited the most potent ACE inhibitory activity with $IC_{50}$ value of $0.08{\pm}0.00mg/mL$. The PBB protamex hydrolysate was fractionated by two ultrafiltration membranes with 3 and 10 kDa (below 3 kDa, between 3 and 10 kDa, and above 10 kDa). These three fractions were evaluated for the total amino acids composition, antioxidant, and ACE inhibitory activities. Among these fractions, the < 3 kDa and 3-10 kDa fractions showed more potent $ABTS^+$ radical scavenging activity than that of > 10 kDa fraction, while the > 10 kDa fraction exhibited the significant reducing power than others. In addition, 3-10 kDa and > 10 kDa fractions showed the significant ACE inhibitory activity. These results suggested that the high molecular weight enzymatic hydrolysate derived from PBB could be used for control oxidative stress and prevent hypertension.

The Inhibitory Effects of Bangpuangtongseoung-san on the Obese gene and Obese Inhibitory about Obese-mouse induced by High Fat Diet (방풍통성산(防風通聖散)이 고지방사료(高脂肪飼料) 식이(食餌)로 유발(誘發)된 비만(肥滿)생쥐에서 비만유전자(肥滿遺傳子) 및 관련인자(關聯因子)에 미치는 영향(影響))

  • Hwang Sang-Jun;Song Tae-Won;Oh Min-Suck
    • The Journal of Korean Medicine
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    • v.27 no.1 s.65
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    • pp.11-22
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    • 2006
  • Objectives : In this study, the aim was to investigate the inhibitory effects of Bangpungtong-seoung-san on the obese gene and obese inhibitory about obese-mouse induced by high fat diet. Methods : In order to investigate the effects of Bangpuangtongseoung-san(BPTS) on the obese gene and obese inhibitory, C57BL/6 mice were induced by high fat diet. C57BL/6 mice were divided into three groups(normal, high fat diet with control, high fat diet with BPTS extract) and fed for 13weeks. Results : 1. The change of body weight and the final increase of body weight were decreased significantly. 2. The amount of the adipocyte in body weight was decreased significantly. 3. In primary adipocytes, ${\beta}3AR$ gene expression was increased significantly and leptin gene expression was decreased in $100{\mu}g/ml$ density significantly. 4. In primary adipocytes, the amount of TNF-${\alpha}$ was decreased in $100{\mu}g/ml$ density significantly and the amount of leptin was decreased but did not show significance. 5. In adipocytes tissue, the expression of leptin was decreased and the expression of ${\beta}3AR$ was increased. Conclusions : These results suggest that BPTS may inhibit the expression of the obese gene mad obese inhibitory about obese-mouse induced by high fat diet.

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Effect of Injin Fraction on Hepatic Fibrosis induced by $TGF-{\beta}1$ (인진이 $TGF-{\beta}1$ 유도성 간섬유화에 미치는 영향)

  • 신성만;김영철;이장훈;우흥정
    • The Journal of Korean Medicine
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    • v.22 no.3
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    • pp.141-155
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    • 2001
  • Objective : The aim of this study is to investigate the effect of Injin fractions on hepatic fibrosis induced by $TGF-{\beta}1$. Method : $TGF-{\beta}1$ mRNA, protein, $TGF-{\beta}1$ receptor, Smad family and PAI-I mRNA were studied in HepG2 cell, and the proliferation, connective tissue growth factor, fibronectin and collagen type I mRNA in T3891 fibroblast by quantitative RT-PCR, ELISA and thymidine incorporation assay. Results : On $TGF-{\beta}1$ mRNA and protein synthesis in HepG2, $H_2O$, butanol and hexane fractions of Injin showed inhibitory effect in a dose-dependent way. In the study on $TGF-{\beta}1$ receptor, Smad family and PAI-1 mRNA in HepG2, $H_2O$, butanol and hexane fraction of Injin showed inhibitory effect on the expression of PAI-1 in a dose-dependent way. On the proliferation of T3891 fibroblast induced by $TGF-{\beta}1$, $H_2O$, ethylacetate and butanol fractions of Injin showed inhibitory effect. In the study on the factors affected by $TGF-{\beta}1$, $H_2O$, ethylacetate and butanol fractions of Injin showed inhibitory effect on CTGF, and $H_2O$, butanol, chloroform and hexane fractions showed inhibitory effect on the expression of collagen type I, whereas no fraction showed inhibitory effect on the expression of fibronectin Conclusion : These results show that each fraction of Injin acts as a fibrosis inhibitory factor by itself or in combination, ultimately inhibiting liver cirrhosis.

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ACE and α-glucosidase Inhibitory Activity of the Glucosinolates in Dolsan Leaf Mustard Pickle during Storage (저장기간 중 돌산갓피클에서 Glucosinolates의 ACE 및 α-glucosidase 저해활성)

  • Son, Hae-Reon;Oh, Sun-Kyung;Tsukamoto, Chigen;Choi, Myeong-Rak
    • KSBB Journal
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    • v.31 no.3
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    • pp.165-170
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    • 2016
  • This study was carried out for investigate that physiological activity, quantification and qualitative were sinigrin of Dolsan leaf mustard pickle (DLMP) during storage. sinigrin contains high amounts of nutritional and medicinal compounds, which are important for maintaining optimum health. ACE inhibitory activity was ranged between 43.2 and 79.4%. DLMP methanol extracts demonstrated highest ACE inhibitory activity at 79.4% on day 14, whereas DLMP ethanol extracts demonstrated highest Angiotensin I-converting Enzyme (ACE) inhibitory activity of 43.2% at day 0. The ${\alpha}-glucosidase$ inhibitory activity of positive control 0.02% (v/v) acarbose was 78%. The DLMP methanol extracts had the highest ${\alpha}-glucosidase$ inhibitory activity at 64.0% on day 14, whereas DLMP ethanol extracts had the lowest ${\alpha}-glucosidase$ inhibitory activity of 42.8% at day 28. Sinigrin was high in DLMP methanol extracts at $49.55{\mu}g/ml$ on day 14 of storage. Sinigrin standard was eluted at 2.73 min and MS analysis was m/z 283.03 along with fragment ions at m/z 204 and 149.06. These data show that sinigrin formed desulfo-glucosinolates $[M-SO_3-2H_2O+K+2H]^+$. Sinigrin concentration increased until day 14 and then decreased after that. DLMP methanol extracts had consistently higher sinigrin concentration than DLMP acetonitrile extracts during 28 days of storage.

THE INHIBITORY EFFECT OF STREPTOCOCCAL CELL WALL EXTRACTS ON STIMULATION OF LYMPHOCYTES (연쇄구균의 세포벽 단백질 추출물이 림프구 활성의 억제에 미치는 영향)

  • Sang, Hyoung-Sook;Jeong, Hee-Il;Oh, Se-Hong;Im, Mi-Kyung
    • Restorative Dentistry and Endodontics
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    • v.20 no.1
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    • pp.275-288
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    • 1995
  • The inhibitory effect of cell wall extracts of streptococci, have been investigated to know host-parasite relationship or pathogenesis of abscess formation. Streptococci isolated from the infected root canals were sonicated to get cell wall extracts which have been known as one of the factors of pyogenesis. Lymphocytes separated by density gradient were stimulated with phytohemagglutinin and exposed to cell wall extracts of Streptococcus sanguis, S. mitis, S. uberis, S. mutans (ATCC 10449), and S. faecalis (ATCC 19433). [$^3H$]-thymidine uptake of lymphocytes was analyzed with scintillation counter and lactate dehyrogenase (LD) activity was measured with autochemistry analyzer. S. faeealis had the strongest inhibitory effect. beginning at $100\;{\mu}g/ml$ concentration of sonic extracts. S. sanguis and S. mitis had inhibitory effect at $300\;{\mu}g/ml$, while S. uberis and S. mutans showed no inhibitory, effect on DNA syntheis even at $300\;{\mu}g/ml$. Each streptococci showed different inhibitory effect on the DNA synthesis of lymphocytes, which finding indicated wide spectrum of susceptibility of lymphocytes according to streptococcus spp. There were no significant difference of LD activities between control and each streptococcal extracts. Streptococcal sonic extracts did not affect the morphological findings or number of colonies activated lymphocytes. These finding suggested the inhibitory effect of sonic extract of streptococci to lymphocytes could be detected by DNA synthesis inhibition, not by cellular membrane damage.

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Evaluation of Cytotoxicity, Carbohydrate, and Lipid Inhibitory Activity of Codonopsis lanceolata using Different Solvent Fractions

  • Boo, Hee-Ock;Park, Jeong-Hun;Kim, Seung-Mi;Woo, Sun-Hee;Park, Hyeon-Yong
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.60 no.4
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    • pp.498-503
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    • 2015
  • This study was conducted to evaluate the cytotoxicity and ${\alpha}-Amylase$, ${\alpha}-Glucosidase$, pancreatic lipase inhibition in vitro by different solvent fractions from the roots of Codonopsis lanceolata. The values of $IC_{50}$ against Calu-6 cell showed a high effect in n-hexane fraction ($10.13{\mu}g/mL$) whereas DW fraction exhibited the weakest inhibition on cell viability, having an $IC_{50}$ value of over $1,000{\mu}g/mL$. The values of $IC_{50}$ against HCT-116 cell showed the highest activity in n-BuOH fraction ($102.01{\mu}g/mL$), followed by n-hexane fraction ($145.85{\mu}g/mL$), methylene chloride fraction ($332.02{\mu}g/mL$), ethyl acetate fraction ($462.93{\mu}g/mL$) and DW fracion ($>1,000{\mu}g/mL$). ${\alpha}-Amylase$ inhibitory activity in methylene chloride fraction and ethyl acetate fraction was found to have a higher inhibitory effect with 24.5% and 25.6% than the other fractions. The highest ${\alpha}-Glucosidase$ inhibitory activity was observed from the ethyl acetate fraction extract, while the extract of DW fraction showed the lowest level of inhibitory activity at given experiment concentration. The pancreatic lipase inhibitory activity of C. lanceolata was found to have a higher the effect in ethyl acetate fraction. Inhibition of lipase activity of the ethyl acetate fraction and n-hexane fraction showed a relatively high, while the extract of DW fraction showed the lowest level at given experiment concentration. These results suggested that the roots of C. lanceolata may assist in the potential biological activity on carbohydrate, lipid Inhibitory activity and anticancer activity.

Optimization of Enzymatic Hydrolysis Conditions for Production of Angiotensin-I Converting Enzyme Inhibitory Peptide from Casein

  • Do, Jeong-Ryong;Kim, Ki-Ju;Kim, Hyun-Ku;Kim, Young-Myoung;Park, Yeung-Beom;Lee, Yang-Bong;Kim, Seon-Bong
    • Food Science and Biotechnology
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    • v.16 no.4
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    • pp.565-571
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    • 2007
  • This study was carried out to investigate an optimum condition for the high angiotensin-l converting enzyme (ACE) inhibitory activity and the yield on enzyme concentration, casein concentration, and hydrolysis time. The optimum condition was performed by response surface methodology for acquirement of casein hydrolysate of milk which shows high ACE inhibitory activity, Among 8 tested enzymes, Protamex showed the highest activation degree with 77.03 unit/g from casein. Their hydrolysis degrees of flovourzyme 500MG, protamex, mixture from 1% casein were 85.5, 88.5, and 93.5%, respectively. The ranges of enzyme concentration (0.25-1.25%), casein concentration (2.5-12.5%), and hydrolysis time (20-100 min) as 3 independent variables through preliminary experiments of the yield of casein hydrolysate and ACE inhibitory activity, and it shows optimum response surface at a saddle point. It shows enzyme concentration (0.64%), casein concentration (8.38%), and hydrolysis time (55.81 min) in the yield aspect and showed the highest activity at enzyme concentration (0.86%), casein concentration (5.97%), and hydrolysis time (63.86 min) in ACE inhibitory aspect. The $R^2$ value of a fitted optimum formula on the hydrolysis yield was 0.9751 as the significant level of 1%. The $R^2$ value of a fitted optimum formula on ACE inhibitory activity is 0.8398, and the significance is recognized in the range of 5%.

Inhibitory Effects of Brown Algae Extracts on Histamine Production in Mackerel Muscle via Inhibition of Growth and Histidine Decarboxylase Activity of Morganella morganii

  • Kim, Dong Hyun;Kim, Koth Bong Woo Ri;Cho, Ji Young;Ahn, Dong Hyun
    • Journal of Microbiology and Biotechnology
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    • v.24 no.4
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    • pp.465-474
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    • 2014
  • This study was performed to investigate the inhibitory effects of brown algae extracts on histamine production in mackerel muscle. First, antimicrobial activities of brown algae extracts against Morganella morganii were investigated using a disk diffusion method. An ethanol extract of Ecklonia cava (ECEE) exhibited strong antimicrobial activity. The minimum inhibitory concentration (MIC) of ECEE was 2 mg/ml. Furthermore, the brown algae extracts were examined for their ability to inhibit crude histidine decarboxylase (HDC) of M. morganii. The ethanol extract of Eisenia bicyclis (EBEE) and ECEE exhibited significant inhibitory activities (19.82% and 33.79%, respectively) at a concentration of 1 mg/ml. To obtain the phlorotannin dieckol, ECEE and EBEE were subjected to liquid-liquid extraction, silica gel column chromatography, and HPLC. Dieckol exhibited substantial inhibitory activity with an $IC_{50}$ value of 0.61 mg/ml, and exhibited competitive inhibition. These extracts were also tested on mackerel muscle. The viable cell counts and histamine production in mackerel muscle inoculated with M. morganii treated with ${\geq}2.5 $ MIC of ECEE (weight basis) were highly inhibited compared with the untreated sample. Furthermore, treatment of crude HD-Cinoculated mackerel muscle with 0.5% ECEE and 0.5% EBEE (weight basis), which exhibited excellent inhibitory activities against crude HDC, reduced the overall histamine production by 46.29% and 56.89%, respectively, compared with the untreated sample. Thus, these inhibitory effects of ECEE and EBEE should be helpful in enhancing the safety of mackerel by suppressing histamine production in this fish species.

Inhibitory Effects of Cinnamic Acid Analogs on fMLP-Induced Chemotaxis of Rat Polymorphonuclear Leukocytes (흰쥐 다형핵백혈구의 fMLP로 유도한 유주현상에 대한 신나믹산 유사체의 억제효과)

  • Min, Kyung-Rak;Kim, Jin-Jun;Park, Sun-Gyoo;Lee, Jeong-Rai;Kang, Seh-Hoon;Kim, Young-Soo
    • YAKHAK HOEJI
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    • v.42 no.2
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    • pp.165-169
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    • 1998
  • Inhibitory effects of 16 cinnamic acid analogs on formyl-Met-Leu-Phe(fMLP)-induced chemotaxis of rat polymorphonuclear leukocytes were determined by using a microchemotaxis appa ratus. 3,4-Dlhydrocinnamic acid called as caffeic acid exhibited the highest inhibitory effect on the chemotaxis among cinnamic acid analogs tested in this study. Hydroxycinnamic acids exhibited stronger inhibitory effects on the chemotaxis than cinnnamic acid. Hydroxycinnamic acids with one hydroxy group at ortho, meta or para position exhibited similar inhibitory effects on the chemotaxis with corresponding methoxy cinnamic acids, but 3,4-dihydroxycinnamic acid did stronger inhibitory effects than 3,4-dimethoxycinnamic acid. 3,4-Dimethoxycinnamic acid exhibited weaker inhibitory effects on the chemotaxis than 1,2-dimethoxy-4-propenylbenzene and 3,4-dimethoxy cinnamonitrile with -CH=CHCN or -CH=$CHCH_3$, group instead of -CH=CHCOOH group. 4-Hydroxy cinnamic acid and 3,4-dihydroxycinnamic acid exhibited stronger exhibitory effects on the chemotaxis than 3-(4-hydroxyphenyl) propionic acid and 3,4-dihydroxyhydrocinnamic acid with -$CH_2CH_2$COOH group instead of -CH=CHCOOH group.

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