• Title/Summary/Keyword: glycosidases

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Isolation and Characterization of $\alpha$-Glucosidase Inhibitor from the Fungus Ganoderma lucidum

  • Kim, Shin-Duk;Nho, Hong Joon
    • Journal of Microbiology
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    • v.42 no.3
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    • pp.223-227
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    • 2004
  • An ${\alpha}$-glucosidase inhibitor, SKG-3, was isolated from the fruiting bodies of Ganoderma lucidum and its physico-chemical properties were characterized. It was a highly specific and effective reversible inhibitor of ${\alpha}$-glucosidase. It showed very potent inhibitory activity against a-glucosidase with an IC$\sub$50/ value of 4.6$\mu\textrm{g}$/$m\ell$, but no activity for any other glycosidases tested. Enzyme activity could be recovered upon dialysis, thus providing evidence for the reversibility of the inhibition. A Lineweaver-Burk plot indicated that the SKG-3 inhibition of ${\alpha}$-glucosidase was competitive.

Asymmetric Total Synthesis of the Glycosidase Inhibitor, 1,4-dideoxy-l,4-imino-D-arabinitol(DAB1)

  • Kim, In-Su;Hoon, Jung-Young
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2003.11a
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    • pp.115-115
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    • 2003
  • Naturally occurring sugar mimics with a nitrogen in the ring are classified into five structural classes: polyhydroxylated pyrrolidines, piperidines, indolizidines. pyrrolizidine, and nortropanes. Glycosidase are involved in a wide range of important biological processes, such as intestinal digestion, post-translational processing of glycoproteins and the lysosomal catabolism of glycoconjugate. The realization that alkaloidal sugar mimics might have enormous therapeutic potential in many diseases such as viral infection, cancer and diabetes has led to increasing interest and demand for these compounds. Most of these effects can be shown to result from the direct or indrect inhibition of glycosidases.

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Characteristics of Invertase from Korean ginseng (Panax ginseng C.A. Meyer) Leaf (고려인삼(Panax ginseng C.A. Meyer) 잎 Invertase의 생화학적 특성)

  • 김용환;심우만
    • The Korean Journal of Food And Nutrition
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    • v.5 no.2
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    • pp.144-149
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    • 1992
  • Invertase was extracted from Korean ginseng(Panax ginseng C. A. Meyer) leaf with deionized water, and then prepared by ammonium sulfate(0.4~0.6 Sat.) fractionation, the enzymological properties of the invertase were investigated, and the results obtained were as follows. The optimum pH and temperature of the enzyme were pH 6.0 and 4$0^{\circ}C$ respectively. The enzyme was stable in the pH range of pH 6.0 to 8.0, and at the temperature below 4$0^{\circ}C$. The enzyme was inactivated completely by the treatment with some proteases(pepsin, trypsin, papain and ficin) and protein denaturants(8M urea and 6M guanidine-HCI), but not with glycosidases (a-amylase, $\beta$-amylase and glucoamylase). The enzyme catalyzed specifically the hydrolization of the $\beta$-fructofuranosides such as sucrose and inulin.

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Ovum-Membrane Denudation Activities of the Purified Acrosomal Glycosidases and Sulfatase (정제된 아크로솜의 글라이코시데이스들과 썰파테이스들의 난자막 침투의 활성도)

  • Yang, Chul-Hak
    • Clinical and Experimental Reproductive Medicine
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    • v.8 no.1
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    • pp.19-22
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    • 1981
  • 정자 아크로좀이나 정액중에서 고순도로 정제된 탄수화물 분해효소들 및 썰파테이스를 개별적으로 또는 여러 조합으로 사용하여 난자막의 용해를 조사하였다. 베타 굴룩유로니데이스와 베타-엔-에시틸글루코사미니데이스가 전혀 없이 정제된 황소 정자의 하이얄유로니데이스는 토끼의 난자막중 큐믈러스층을 쉽게 분해시켰다. 토끼의 정자에서 얻은 아릴썰파테이스와 위의 하이얄유로니데이스는 더욱 빨리 토끼난자의 큐믈러스층을 용해시켰다. 한편 아릴썰파테이스는 하이얄유로니데이스나 베타-엔-에시틸 글루코사미니데이스들도 하이얄 유로니데이스들과 아릴썰파테이스들처럼 큐믈러스츨을 용해시켰으나 모든 경우에 난자의 코로나층이나 조나펠루시다층에는 아무런 변화를 주지 않고 있다.

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Total synthesis of deoxy-azasugars

  • Pyun, Sung-Jae;Oh, Chang-Young;Lee, Kee-Young;Kim, Yong-Hyun;Lee, Yiu-Suk;Pharm, Van-Thoai;Ham, Won-Hun
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.233.1-233.1
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    • 2002
  • Azasugars, which have been called the "sugar-shaped" alkaloids from plants. are reversible. competitive inhibitors of glycosidases. The purpose of these natural products is possibly to inhibit the carbohydrate metabolism and consequently the growth of plant consuming pests. Since selective glycosidase inhibitors have a large number of interesting potential applications including treatment of AIDS, diabetes. and tumor metastasis. they have received a considerable attentions. (omitted)

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Electrophoretic analysis of the major proteins of ruminant erythrocyte membrane: Their relation to slow erythrocyte sedimentation rate (반추동물 적혈구막 단백의 전기영동법에 의한 분석 -낮은 적혈구침강속도와의 관계-)

  • Lee, Bang-whan;Bahk, Young-woo
    • Korean Journal of Veterinary Research
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    • v.29 no.4
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    • pp.445-455
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    • 1989
  • The proteins of the ruminant erythrocyte membranes were analysed by polyacrylamide gel electrophoresis in sodium dodecyl sulfate, and their relations to the slow erythrocyte sedimentation rate(ESR) of the ruminants were investigated by treating the erythrocytes with proteinases such as trypsin, chymotrypsin and pronase, and glycosidases such as neuraminidase and galactosidase. Protein content in the erythrocyte membrane was $2.85{\pm}0.28$ in human, $3.60{\pm}0.41$ in Korean cattle, $3.71{\pm}0.36$ in Holstein, $4.13{\pm}0.83$ in Korean native goat and $3.94{\pm}0.56mg/ml$ in sheep, showing higher in ruminant animals than in human(p<0.01). Although the general protein profiles of the ruminant erythrocyte membranes were almost similar to that of human, all the ruminant erythrocyte membranes showed one additional protein band, called band-Q in the previous report on proteins of bovine erythrocyte membrane, which migrated electrophoretically to the mid position between band-2 and band-3 in human erythrocyte membranes. The glycoprotein profiles of ruminant erythrocyte membranes revealed by periodic acid Schiff(PAS) stain showed a marked difference from that of human. The PAS-1(glycophorin) and PAS-2(sialoglycogrotein) present in human erythrocyte membranes were almost absent from the ruminant animals. Instead, a strong PAS-positive band near the origin of the electrophorograms, which was named as PAS-B in the previous report on proteins of bovine erythrocyte membranes, was shown in the ruminant animals except sheep. In addition, the erythrocyte membranes of Korean native goat and sheep showed a moderate PAS-negative band near the tracking dye of the electrophorograms, which was named as PAS-G in this study. In the erythrocyte treated with the enzymes, the migration of each protein fracture of erythrocyte membranes in response to each enzyme was diverse according to different species or breed of ruminant animals. Among others, band-Q present in ruminants was slightly or moderately decreased by trypsin-, chymotrypsin-, and pronase- treatments of the erythrocytes, but not only in sheep. It was particularly noticeable that PAS-B, a fraction of glycoprotein, present in ruminants except sheep, was better digested by proteinases than by glycosidases, showing remarkable increase(p<0.01) of the ESR in accord with complete digestion(disappearance) of the PAS-B band by pronase, trypsin or chymotrypsin treatment of erythrocytes. In sheep, there was almost no any response to the various enzymes in general protein and glycoprotein profiles of the erythrocyte membranes except PAS-G, which was markedly decreased by pronase treatment of the erythrocytes. Nevertheless, the ESRs were accelerated in erythrocytes treated with pronase, trypsin, chymotrypsin and neuraminidase. Erythrocyte osmotic fragility was increased in erythrocytes treated with only pronase among five enzymes in all the human and ruminant animals used in this study.

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Purification of a major protein with physiological activities from Panax ginseng C. A. Meyer (고려인삼(Panax ginseng C. A. Meyer)에서 생리활성을 보이는 25 kDa 주요단백질 (GMP)의 분리정제)

  • Kwon, Taek-H.;Oh, Sei-R.;Park, H.;Kim, Kyung-H.
    • Applied Biological Chemistry
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    • v.41 no.6
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    • pp.410-413
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    • 1998
  • The major protein (GMP) from the roots of Panax ginseng C. A. Meyer was purified, using gel filtration and ion exchange chromatography followed by reversed-phase and ion exchange FPLC. Staining analysis indicated that the protein has a carbohydrate moiety, which was also shown by band shift experiments using various glycosidases. Electrophoretic and gel permeation studies showed that GMP has an apparent molecular weight of 63 kDa composed of possibly two subunits of 25 kDa containing carbohydrate moiety. GMP showed an anticomplementary activity on the hemolysis of red blood cells, which is a screening tool for inflammation mediator search.

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Neuraminidase Inhibitors from Mushroom Microphorus affinis

  • Kim, Kyung-Bum;Kim, Sang-In;Song, Kyung-Sik
    • Journal of Microbiology and Biotechnology
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    • v.13 no.5
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    • pp.778-782
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    • 2003
  • In the course of screening anti-influenza agents from natural products, four neuraminidase inhibitors were isolated from the methanol extract of mushroom Microphorus affinis by purification using solvent partition, silica gel column chromatography, Sephadex LH-20, and semi-preparative HPLC. The chemical structures of these compounds were identified as ${\alpha}-lupeol$, methyl linoleate, methyl palmitate, and methyl oleate by means of spectral data including GC-MS, $^1H-,\;and\;^{13}C-NMR\;with\;IC_{50}$ values of 5.65, 7.07, 7.12, and $7.52\;\mu\textrm{M}$, respectively. They did not inhibit other glycosidases such as glucosidase, mannosidase, and galactosidase, indicating that they were relatively specific inhibitors of neuraminidase. The relationship between the fatty acid structure and inhibitory activity was investigated. The result showed that, in the case of an aliphatic linear hydrocarbon skeleton, at least one carboxyl (presumably any carbonyl) moiety and sixteen carbons were the necessary requirements for potent inhibition, whereas saturated, unsaturated, free, and ester forms did not have any significant effect on the activity.

Picomolar Scale Determination of Carbohydrates Covalently Immobilized on Activated Beads Using Hydroxyl Functionality

  • Yu, Jae-Hoon;Chun, Sung-Min;Park, Ho-Koon;Park, Yong-Keun;Jeong, Sun-Joo
    • BMB Reports
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    • v.32 no.1
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    • pp.98-102
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    • 1999
  • Since carbohydrates are major mediators in cell-to-cell adhesion and communication, the development of specific and strong binders against them could generate promising therapeutics. As the first step towards that goal, sugar molecules have to be immobilized to be used as an affinity matrix. The amino functionality in sugar is the most active nucleophile for the immobilization, if the amino group is available. An alternative and general method is to use the hydroxyl group as a direct nucleophile, but the quantitation of immobilized hydroxyl groups is not easily done. To overcome this limitation, we have developed a method to immobilize various isomers of monosaccharides with p-nitrophenyl groups to the beads by using their hydroxyl groups. It was found that the amount of immobilized sugar was independent of the structure of the sugar, but was dependent on the number of hydroxyl groups. We also developed a sensitive method to quantify the amount of immobilized sugar at the picomolar scale by utilizing commercially available glycosidases to release a sensitive reporter molecule, p-nitrophenol, and detect it by HPLC. This new technique would allow a facile quantitation method for immobilized sugar molecules, which could be used as the affinity matrix to develop strong binders against biologically important sugars.

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Role of Curcuma longa, a traditional ayurvedic medicinal plant, in diabetes

  • Ponnusamy, Sudha;Zinjarde, Smita;Bhargava, Shobha;Kumara, Ameeta Ravi
    • CELLMED
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    • v.2 no.4
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    • pp.31.1-31.7
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    • 2012
  • Curcuma longa belongs to the family Zingiberaceae and can be found in the tropical and subtropical regions of the world. It is widely used in Asiatic countries, especially India and South East Asia where it is cultivated commercially as a condiment. Its rhizomes exhibit anti-inflammatory, anti-human immunodeficiency virus, anti-bacterial, antioxidant effects, nematocidal activities, antiproliferative and antiangiogenic activities and are of pharmaceutical importance. Another relevant medicinal property exhibited by it is antidiabetic property which is reviewed here. Studies on the efficacy of crude C.longa extracts against type 2 diabetes in murine models reveal that it demonstrates a hypoglycemic effect by lowering the blood glucose levels under in vivo conditions. Clinical studies have revealed the safety of curucmin (major principle component exhibiting pharmaceutical properties from C.longa) on humans but with very low bioavailability. In view of its effective hypoglycemic effect and its low bioavailability, further studies are needed for the characterization of the bioactive principles and formulating the development of C.longa extracts as a novel anti-diabetic therapeutic agent.