• Title/Summary/Keyword: inhibitory

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Inhibitory Effects of Quinoline Isolated from Ruta chalepensis and Its Structurally Related Derivatives against α-Amylase or α-Glucosidase

  • Park, Jun-Hwan;Lee, Hoi-Seon
    • Journal of Applied Biological Chemistry
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    • v.58 no.1
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    • pp.5-8
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    • 2015
  • This study was to isolate an active component of the chloroform fraction from the methanol extract of Ruta chalepensis leaves and to measure inhibitory effects against ${\alpha}$-glucosidase or ${\alpha}$-amylase. The inhibitory compound of R. chalepensis leaves was isolated using chromatographic methods and identified as quinoline. Quinoline and its structurally related derivatives were tested for their inhibitory activities by evaluating the $IC_{50}$ values against ${\alpha}$-amylase or ${\alpha}$-glucosidase and were compared with that of acarbose. Based on the $IC_{50}$ values, quinazoline exhibited the greatest inhibitory activity ($20.5{\mu}g/mL$), followed by acarbose ($66.5{\mu}g/mL$), and quinoline ($80.3{\mu}g/mL$) against ${\alpha}$-glucosidase. In case of ${\alpha}$-amylase, quinazoline had potent inhibitory activity, followed by quinoline ($179.5{\mu}g/mL$) and acarbose ($180.6{\mu}g/mL$). These results indicate that R. chalepensis extract, quinoline, and quinazoline could be useful for inhibiting ${\alpha}$-glucosidase or ${\alpha}$-amylase.

Physiological Functionalities of Solvent Fractions Isolated from Crataegi Fructus

  • Oh, Hae-Sook;Kim, Jun-Ho
    • Biomedical Science Letters
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    • v.14 no.4
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    • pp.249-255
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    • 2008
  • In this study we investigated the biological activities of Crataegi Fructus, including antioxidative, fibrinolytic, $\alpha$-glucosidase inhibitory, and thrombin inhibitory activities. Crataegi Fructus, hot water extract was fractionated into hexane, $CHCLl_3$, ethyl acetate, butanol, and water fractions, and each of these was assayed individually. The water fraction showed the highest extraction yield at 4.08% (w/w). The antioxidative activities of the water, ethyl acetate, and butanol fractions were 31.07%, 45.87%, 50.28%, and 91.74%, respectively. Assays for fibrinolytic activity indicated that only the butanol fraction has significant efficacy at 1.93 plasmin units/ml. Thrombin inhibitory assays indicated that the 10-fold dilutions of the $CHCLl_3$, ethyl acetate, and butanol fractions had inhibitory activities of 34.97%, 41.43%, and 58.10%, respectively. The 10-fold dilutions of the only ethyl acetate fraction demonstrated $\alpha$-glucosidase inhibitory activities of 75.07%. From the above results, we propose that extracts of Crataegi Fructus can be used as a material for the development of biofunctional foods.

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Experimental Study on the Effects of Jungchuntang (정천탕(定喘湯)의 효능(效能)에 관한 실험적(實驗的) 연구(硏究))

  • Park, Cheon-Su;Han, Sang-Whan
    • The Journal of Internal Korean Medicine
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    • v.17 no.1
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    • pp.175-192
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    • 1996
  • These studies were carried out to investigate the effect of Jungchuntang water extract on the inhibitory contractile action of acetylcholine in rat. The results of these studies were as follows; 1. Contractile force of acetylcholine from trachea smooth muscle in rat was significantly inhibited by Jungchuntang. 2. Dose-response of acetylcholine pretreated Jungchuntang in rat was not significantly changed. 3. Inhibitory contractile action of acetylcholine pretreated propranolol in rat was decreased. 4. Inhibitory contractile action of acetylcholine pretreated indomethacin was not significantly changed by Jungchuntang. 5. Inhibitory contractile action of acetylcholine pretreated methylene blue was significantly changed by Jungchuntang. 6. Contractile force of acetylcholine from trachea smooth muscle in rat was significantly inhibited by Jungchuntang. 7. Dose-response of acetylcholine pretreated Jungchuntang in rat was not significantly changed. 8. Inhibitory contractile action of acetylcholine pretreated propranolol in rat was decreased. 9. Inhibitory contractile action of acetylcholine pretreated indomethacin was not significantly changed by Jungchuntang. 10. Inhibitory contractile action of acetylcholine pretreated methylene blue was significantly changed by Jungchuntang.

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The Effects of Gooboeum on the Airway Smooth Muscle in the Sensitized Rats (구보음(九寶飮)이 Sensitized Rat의 기관지평골근(氣管支平滑筋)에 미치는 영향(影響))

  • Lee, Seung-Woo
    • The Journal of Internal Korean Medicine
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    • v.14 no.2
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    • pp.1-19
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    • 1993
  • This study was carried out to investigate the effects of Gooboeum extract on the inhibitory contractile action of acetylcholine in the control and sensitized rat. The results were obtained as follows: 1. The acetylcholine contractile force of the trachea smooth muscle with epithelium was significantly relaxed by Gooboeum. 2. Dose-response of acetylcholine from the trachea smooth muscle pretreated Gooboeum was not changed. 3. Effect of Gooboeum on the inhibitory contractile action of trachea smooth muscle pretreated propranolol was not significantly inhibited. 4. The inhibitory contractile action of acetylcholine of trachea smooth muscle pretreated indomethacin was not significantly changed by Gooboeum. 5. Effects of Gooboeum extract on the inhibitory contractile action of acetylcholine of trachea smooth muscle pretreated methylene blue was not significant. 6. The contractile force of acetylcholine of the trachea smooth muscle without epithelium was significantly inhibited by Gooboeum. 7. Dose-response of acetylcholine of the trachea smooth muscle pretreated Gooboeum was not significant. 8. Effects of Gooboeum extract on the inhibitory contractile action of acetylcholine of the trachea smooth muscle pretreated propranolol was significantly inhibited. 9. Effects of Gooboeum extract on the inhibitory contractile action of acetylcholine of the trachea smooth muscle pretreated indomethacin decreased. 10. Effects of Gooboeum extract on the inhibitory contractile action of acetylcholine of the trachea smooth muscle pretreated methylene blue was not significant.

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Purification and characterization of β-secretase inhibitory peptide from sea hare (Aplysia kurodai) by enzymatic hydrolysis

  • Lee, Jung Kwon;Kim, Sung Rae;Byun, Hee-Guk
    • Fisheries and Aquatic Sciences
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    • v.21 no.5
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    • pp.13.1-13.8
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    • 2018
  • Amyloid plaque, also called senile plaque, the product of aggregation of ${\beta}$-amyloid peptides ($A{\beta}$), is observed in brains of the patients with Alzheimer's disease (AD) and is one of the key factors in etiology of the disease. In this study, hydrolysates obtained from the sea hare (Aplysia kurodai) were investigated for ${\beta}$-secretase inhibitory peptide. The sea hare's muscle protein was hydrolyzed using six enzymes in a batch reactor. Trypsin hydrolysate had highest ${\beta}$-secretase inhibitory activity compared to the other hydrolysates. ${\beta}$-secretase inhibitory peptide was separated using Sephadex G-25 column chromatography and high-performance liquid chromatography on a C18 column. ${\beta}$-secretase inhibitory peptide was identified as eight amino acid residues of Val-Ala-Ala-Leu-Met-Leu-Phe-Asn by N-terminal amino acid sequence analysis. $IC_{50}$ value of purified ${\beta}$-secretase inhibitory peptide was $74.25{\mu}M$, and Lineweaver-Burk plots suggested that the peptide purified from sea hare muscle protein acts as a competitive inhibitor against ${\beta}$-secretase. Results of this study suggest that peptides derived from sea hare muscle may be beneficial as anti-dementia compounds in functional foods or as pharmaceuticals.

Isolation of 1',3'-Dilinolenoyl-2'-Linoleoylglycerol with Tyrosinase Inhibitory Activity from Flammulina velutipes

  • Jang, Se-Gul;Jeon, Kyung-Su;Lee, Eun-Hee;Kong, Won-Sik;Cho, Jae-Yong
    • Journal of Microbiology and Biotechnology
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    • v.19 no.7
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    • pp.681-684
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    • 2009
  • This study was carried out to evaluate the inhibitory effect of Flammulina velutipes extracts on tyrosinase activity and to identify its biologically active component. The ethyl acetate and n-butanol extracts showed potent tyrosinase inhibitory activities. Subsequently, fractions of the n-butanol extract showed only a partial tyrosinase inhibitory activity. The most active compound of tyrosinase inhibitory activity was identified from the ethyl acetate extract as 1',3'-dilinolenoyl-2'-linoleoylglycerol (LnLLn) by comparing its mass, $^1H-$, and $^{13}C-NMR$spectral data with those previously reported in the literature. LnLLn showed tyrosinase inhibitory activity with an $IC_{50}$value of 16.1 ${\mu}g/ml$. These results suggest that the ethyl acetate extract of F. velutipes could be applicable for the development of a new whitening agent.

Inhibitory Effects of Doen-jang(Korean Fermented Soybean Paste) and Soybean Extracts on the Growth of KB Cells (한국 전통 된장 및 콩 추출물의 KB 세포에 대한 증식 억제효과)

  • Lee, Sung-Lim;Kim, Jong-Gyu
    • Journal of Environmental Health Sciences
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    • v.31 no.5 s.86
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    • pp.444-450
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    • 2005
  • The present study was designed to investigate whether traditional Korean fermented soybean paste(doen-jang) and soybean extracts have inhibitory effects on the growth of KB cell, an oral epithelioid cancer cell. When KB cell ATCC CCL-17 was cultivated for 48 flours with the addition of 0.5% of the five types or doen-jang extract, the growth of KB cell was inhibited by all types of extract, and ethyl acetate extract showed the highest inhibitory effect. In case of soybean extract, all types of extract also showed KB cell inhibitory effects, however, generally less than those of doen-jang extract. When ethyl acetate extract of doen-jang was added in different concentrations and KB cell was cultivated for 24 hours and 45 hours, strong inhibitory effect began to appear from the concentration of 1.25 mg/ml. Although soybean extract showed such a tendency, its effect was lower than that of doen-jang extract. These results indicate that doen-jang extract has inhibitory effect against KB cell, and particularly ethyl acetate extract has the highest effect. The effect of doen-jang extract might be possibly enhanced by the fermentation of soybeans. It is assumed that doen-jang extract may be used to develop nontoxic medicines for preventing and treating oral diseases.

Screening Test of Wild Mushroom Methanol Extracts for Fibrinolytic and $\alpha-Glucosidase$ Inhibitory Activity

  • Kim, Jun-Ho;Yoo, Kwan-Hee;Seok, Soon-Ja
    • Biomedical Science Letters
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    • v.13 no.3
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    • pp.245-249
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    • 2007
  • We investigated the fibrinolytic and ${\alpha}-glucosidase$ inhibitory activity of 55 wild mushroom methanol extracts. Among them, 14 mushrooms showed fibrinolytic activity. In particular, Amanita virgineoides showed the greatest enzyme activity (3.9 plasmin units/ml) by a fibrin plate assay. The fibrinolytic activities of Suillus pictus and Polypolellus varius were 3.8 plasmin units, and the activity of Gomphus fujisanensis was 2.8 plasmin units. Leccinum extremiorientale and Xerocomus nigromaculatus had the same activity with 2.3 plasmin units. In a ${\alpha}-glucosidase$ inhibitory activity test, Lactarius sp. showed the greatest inhibitory activity at 97.3%. The ${\alpha}-glucosidase$ inhibitory activities of Clitocybe odora, Xerocomus nigromaculatus, Melanoleuca melaleuca, Suillus pictus, and Gyroporus castaneus were 84.3%, 77.9%, 74.6%, 68.7%, and 65.4%, respectively. According to the results, because Suillus pictus and Xerocomus nigromaculatus have strong fibrinolytic and ${\alpha}-glucosidase$ inhibitory activities, the two mushrooms will be used as materials for the development of new biofunctional food.

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Inhibitory Effects of Ginseng Seed Oil on α-Glucosidase and α-Amylase Activity (인삼종자오일의 α-Glucosidase 및 α-Amylase 저해작용)

  • Ahn, Chang Ho;Nam, Yun Min;Kim, Shin Jung;Yang, Byung Wook;Kim, Hyoung Chun;Ko, Sung Kwon
    • Korean Journal of Pharmacognosy
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    • v.47 no.1
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    • pp.24-28
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    • 2016
  • This study was to evaluate the effect of ginseng (Panax ginseng) seed oil on the ${\alpha}$-glucosidase and ${\alpha}$-amylase. Each ginseng seed oils (HE, SE, EE) exhibited a significant inhibitory effect (p<0.001) at all concentrations (10 and 20 mg/ml) on ${\alpha}$-glucosidase activity. HE is the highest inhibitory activity (86.92%) at a concentration of 20 mg/ml, SE and EE showed an inhibitory effect of 77.13% and 65.83%, respectively. And also, Each ginseng seed oils (HE, SE, EE) exhibited a significant inhibitory effect (p<0.001) at all concentrations (1 and 2 mg/ml) on ${\alpha}$-amylase activity. HE is the highest inhibitory activity (89.68%) at a concentration of 2 mg/ml, SE and EE showed an inhibitory effect of 76.99% and 65.70%, respectively.

Biological Activities of the Water Extract and its Fractions from Taraxacum coreanum Nakai (흰민들레 열수 추출물 및 분획물의 피부 관련 생리활성)

  • Lee, Kyoung-In;Im, Do-Youn
    • Korean Journal of Pharmacognosy
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    • v.42 no.2
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    • pp.195-200
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    • 2011
  • In this study, we investigated on antioxidative activity, tyrosinase inhibitory activity and nitric oxide(NO) production inhibitory activity in the hot water extract of Taraxacum coreanum and its fractions. The total polyphenol and flavonoid contents of the extract were found to be 65.42 mg/g and 9.83 mg/g, respectively. And the total polyphenol and flavonoid contents of the ethyl acetate fraction were found to be 168.23 mg/g and 31.92 mg/g, respectively. In DPPH radical scavenging ability, $SC_{50}$ values of the ethyl acetate and butanol fraction were exhibited 64.65 ${\mu}g/ml$ and 277.42 ${\mu}g/ml$, respectively. Moreover, ethyl acetate fraction showed higher inhibitory activity than other samples in tyrosinase inhibitory activity. In NO production inhibitory activity, the extract and its fractions showed NO production inhibitory effect. Especially, the ethyl acetate, chloroform and butanol fraction was exhibited higher NO production inhibitory activity than other samples. As a result, the ethyl acetate and butanol fraction from the water extract of T. coreanum could be applicable to functional materials for skin-related fields.