• Title/Summary/Keyword: glucosidase inhibitor

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Purification and Characterization of Beta-Glucosidase from Weissella cibaria 37

  • Lee, Kang Wook;Han, Nam Soo;Kim, Jeong Hwan
    • Journal of Microbiology and Biotechnology
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    • v.22 no.12
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    • pp.1705-1713
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    • 2012
  • A gene encoding ${\beta}$-glucosidase was cloned from Weissella cibaria 37, an isolate from human feces. Sequence analysis showed that the gene could encode a protein of 415 amino acids in length, and the translated amino acid sequence showed homology (34-31%) with glycosyl hydrolase family 1 ${\beta}$-glucosidases. The gene was overexpressed in E. coli BL21(DE3) using pET26b(+) and a 50 kDa protein was overproduced, which matched well with the calculated size of the enzyme, 49,950.87 Da. Recombinant ${\beta}$-glucosidase was purified by using a his-tag affinity column. The purified ${\beta}$-glucosidase had an optimum pH and a temperature of 5.5 and $45^{\circ}C$, respectively. Among the metal ions (5mM concentration), $Ca^{2+}$ slightly increased the activity (108.2%) whereas $Cu^{2+}$ (46.1%) and $Zn^{2+}$ (56.7%) reduced the activity. Among the enzyme inhibitors (1 mM concentration), SDS was the strongest inhibitor (16.9%), followed by pepstatin A (45.2%). The $K_m$ and $V_{max}$ values of purified enzyme were 4.04 mM and 0.92 ${\mu}mol/min$, respectively, when assayed using pNPG (p-nitrophenyl-${\beta}$-D-glucopyranoside) as the substrate. The enzyme liberated reducing sugars from carboxymethyl cellulose (CMC).

Synthesis and Conformational Study of Ser and Cys Derivatives of N-Hydroxy Diketopiperazine

  • You, Sang-Woo;Park, Won-Choul;Lee, Hyoung-Tae;Ueom, Jeong-Hoon;Jang, Soon-Min;Lee, Kyung-Hee;Lim, Dong-Yeol
    • Bulletin of the Korean Chemical Society
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    • v.28 no.12
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    • pp.2414-2418
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    • 2007
  • N-Hydroxy diketopiperazine derivatives from L- and D-forms of Ser and Cys were synthesized for the first time and the ring conformation of both analogues in water was determined to be close to flat via NMR and ab initio calculations. However, the side chain of the Ser analogue was oriented toward a pseudo-equatorial position while that of the Cys analogue was slightly oriented toward a pseudo-axial direction, with a slightly distorted boat-shaped ring conformation. Among them, the D-Cys analogue was found to be a weak inhibitor of α- glucosidase.

Inhibitory Effects of Crude Drugs on $\alpha$-Glucosidase

  • Choi, Hyuck-Jai;Kim, Nam-Jae;Kim, Dong-Hyun
    • Archives of Pharmacal Research
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    • v.23 no.3
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    • pp.261-266
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    • 2000
  • The inhibitory activity of several crude drugs on $\alpha$-glucosidases, which are the key enzymes for carbohydrate digestion and the prevention of diabetic complications, was investigated. Several crude drugs including Terminaliae Fructus, Mori Cortex Radicis, Caesalpiniae Lignum and Cyrophora esculenta potently inhibited maltase and sucrase isolated from rat intestine, while Arecae Semen and Corni Fructus remarkably inhibited $\alpha$-amylase. Caesalpiniae Lignum and Gyrophora esculenta exhibited significant reductions of blood glucose elevation in mice loaded with maltose and sucrose.

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Anti-diabetic Effects of Mixed Extracts from Lycium chinense, Cordyceps militaris, and Acanthopanax senticosus (지골피, 동충하초, 가시오가피 혼합 추출물의 항당뇨 작용)

  • Kim, Dae-Jung;Kim, Jeong-Mi;Kim, Tae-Hyuck;Baek, Jong-Mi;Kim, Hyun-Sook;Choe, Myeon
    • Korean Journal of Plant Resources
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    • v.23 no.5
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    • pp.423-429
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    • 2010
  • In this study, we examined the anti-diabetic activity in vitro by the mixed Korean herb water extracts(JDG) composed of Lycium chinense, Cordyceps militaris, and Acanthopanax senticosus on hepatic glucose-regulating enzyme activities such as glucokinase(GK), acetyl-CoA carboxylase(ACC), and inhibition activity of $\alpha$-glucosidase. The hepatic cytosol fraction of a type II diabetic animal(Goto-Kakizaki rat) was used in GK and ACC activity assays. JDG mixed water extracts significantly increased the hepatic GK and ACC activity. The highest anti-$\alpha$-glucosidase activity was observed in JDG 5 water extract when compared to the acarbose control, inhibitor of $\alpha$-glucosidase. We suggest that Lycium chinense, Cordyceps militaris, and Acanthopanax senticosus mixed water extracts may exert an anti-diabetic activity by enhancing the glucose metabolism and may be used as natural $\alpha$-glucosidase inhibitors in type 2 diabetic conditions.

α-Glucosidase Inhibitory Effect of Vicine and α-Eleostearic Acid from the Seeds of Momordica charantia (여주씨에서 분리한 Vicine과 α-Eleostearic Acid의 α-glucosidase 저해효과)

  • Yuk, Heung Joo;Noh, Geon Min;Choe, Jeong Sook;Kwon, Oh Kyung;Hong, Su Young;Kang, Sang Soo;Cho, Kye Man;Park, Dong Sik
    • Korean Journal of Environmental Agriculture
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    • v.34 no.1
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    • pp.57-63
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    • 2015
  • BACKGROUND: Momordica charantia (MC) have been used in various parts of the world to treat diabetes. Despite the highest effects of phytochemicals than any other part of the plant, the main components of seed of MC grown in Korea and their properties have not been studied extensively. METHODS AND RESULTS: The seeds of MC were extracted into five different polarity solvents: 30%, 50%, 70%, 95% ethanol and distilled water. The 95% ethanol extract showed the most potent inhibition ($IC_{50}=88.7{\mu}g/mL$) against ${\alpha}$-glucosidase. To investigate the compounds responsible for this effect, activity guided fractionation of MC seeds by chromatography yielded two phytochemicals which were confirmed as vicine (1) and ${\alpha}$-eleostearic acid (2) based on their NMR and ESI-MS spectroscopic data. Among them, ${\alpha}$-eleostearic acid (2) possessed potent ${\alpha}$-glucosidase inhibitory activities with $IC_{50}$ values from $32.4{\mu}g/mL$. CONCLUSION: Collectively, the results from this present study strongly suggest that both extract and ${\alpha}$-eleostearic acid (2) have potent ${\alpha}$-glucosidase inhibitory activity. Furthermore, ${\alpha}$-eleostearic acid (2) as the most active ${\alpha}$-glucosidase inhibitor was proven to be present in high quantities in the MC seeds by a HPLC chromatogram.

Downregulatory Effect of AGI-1120 $({\alpha}-Glucosidase Inhibitor)$ and Chaga Mushroom (Inonotus obliquus) on Cellular $NF-{\kappa}B$ Activation and Their Antioxidant Activity (AGI-1120과 차가버섯의 $NF-{\kappa}B$ 활성화 억제 및 항산화 효과)

  • Song, Hee-Sun;Lee, Young-Jong;Kim, Seung-Kyoon;Moon, Won-Kuk;Kim, Dong-Woo;Kim, Yeong-Shik;Moon, Ki-Young
    • Korean Journal of Pharmacognosy
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    • v.35 no.1 s.136
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    • pp.92-97
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    • 2004
  • Effect of AGI $({\alpha}-Glucosidase\;Inhibitor)-1120$, pine (Pinus densiflora) bark extract and Chaga mushroom (Inonotus obliquus) - and Chaga mushroom mycelium extracts on cellular $NF-{\kappa}B$ activation in malignant human keratinocytes (SCC-13) were evaluated to elucidate the possible correlation of $NF-{\kappa}B$ with antioxidant activity. The antioxidant activities of these natural products were examined in three different evaluation methods, i.e., lipid peroxidation value (POV) evaluation test, and 1,1diphenyl-2-picrylhydrazyl radical (DPPH) and nitric oxide (NO) scavenging test. In a cell-based $NF-{\kappa}B$ monitoring assay systern, all samples revealed the downregulatory profiles on the cellular $NF-{\kappa}B$ activity. AGI -1120 (1, 2 mg) and Chaga mushroom extract (0.05, 0.1 mg) downregulated the $NF-{\kappa}B$ activity in a dose-dependent manner. Chaga mushroom mycelium extract (5 mg) significantly inhibited the $NF-{\kappa}B$ activity (p<0.05). Although AGI-1120 and Chaga mushroom mycelium extract exhibited no antioxidant activities evaluated in pay, Chaga mushroom extract showed antioxidant in a dose-dependent manner at concentrations of $0.05{\sim}1$ mg. While AGI-1120 and Chaga mushroom extract possessed a relatively potential DPPH radical scavenging activity, the NO scavenging activity of Chaga mushroom extract $(SC_{50}:47\;{mu}g)$ was higher than the known antioxidant, vitamin C $(SC_{50}:77\;{mu}g)$. These results suggest that AGI-1120 and Chaga mushroom- and Chaga mushroom mycelium extracts may serve as an useful radical scavenging antioxidant agents with $NF-{\kappa}B$ inhibitory effect in human skin.

Selection and Horticultural Characteristics Evalution of High ${\alpha}-Glucosidase$ Inhibitor in Pepper (고추의 ${\alpha}-glucosidase$ 저해제 고 활성 계통 선발 및 특성 평가)

  • Cho, Myeong-Cheoul;Park, Dong-Bok;Yang, Eun-Young;Pae, Do-Ham;Won, Se-Ra;Yu, Wang-Kyun;Rhee, Hae-Ik
    • Journal of Bio-Environment Control
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    • v.16 no.3
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    • pp.233-239
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    • 2007
  • This study was carried out to investigate the distribution of ${\alpha}-glucosidase$ inhibitor (AGI) activity and to evaluate horticultural characteristics of pepper (Capsicum spp.). AGI activities of pepper fruits and leaves were different from 1.0 to 20.5 times and 1.0 to 5.9 times, respectively. Weight, length and width of evaluated pepper fruit were distributed from 0.5 to 56.0 g, 0.8 to 15.4 cm and 0.5 to 6.3 cm per fruit respectively. Stem colors before transplanting varied from green to violet. Length and width of leaf were distributed from 3.1 to 5.0 cm and 2.1 to 3.0 cm. Immature fruit color was almost green and mature fruit color was almost red. In horticultural characteristics of selected pepper lines with high AGI activity, the fruit position was downward position. The immature fruit color was green in all lines except one and the mature fruit color was red in all lines. Fruit weight and fruit length of selected pepper lines with high AGI activity were distributed from 5.9 to 41.1 g and 5.9 to 17.0 cm and leaf width and leaf length were distributed from 5.8 to 29.7 cm and 3.9 to 8.7 cm, respectively. The AGI activities of pepper is widely variable between leaf and fruit. According to this result, it suggested the possibility of developing a new pepper line with high AGI activity.

Effects of the Biological Function of Yogurt Added with Lycium chinence Miller Extract (구기자(Lycium chinence Miller)추출액을 첨가한 요구르트의 생리활성 효과)

  • Bae, H.C.;Cho, I.S.;Nam, M.S.
    • Journal of Animal Science and Technology
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    • v.47 no.6
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    • pp.1051-1058
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    • 2005
  • This experiment was carried out to investigate the biological function of Lycium chinence Miller yogurt. Antioxidant activity was higher in methanol extract yogurt than in water extract yogurt. The antioxidant activity was shown at 83.9% in Lycii folium extract yogurt, 47.0% in Lycii fructus extract yogurt and 54.0% in Lycii cortex extract yogurt. Angiotensin converting enzyme inhibitor activity was shown highly both in water extract and methanol extracts from the Lycii folium. The $\alpha$-glucosidase inhibitor activity was shown at the 4.0% concentration of Lycii folium extract yogurt, Lycii fructus extract yogurt and Lycii cortex extract. In an orally administrated rat, normal yogurt, Lycii fructus extract yogurt and Lycii cortex extract yogurt have no effect on blood cholesterol content. IgG production in blood is more increased in Lycii cortex extract yogurt than in normal yogurt and Lycii fructus extract yogurt.

Studies on Screening and Iolation of ${\alpha}-Amylase$ Inhibitors of Soil Microorganisms( II ) -Isolation and Activities of the Inhibitor of Streptomyces Strain DMC-72- (토양균의 ${\alpha}-Amylase$ 저해제 검색 및 분리에 관한 연주(제2보) -스트렙토마이세스속 DMC-72 균주의 저해 성분의 분리 및 작용-)

  • Kim, Kyung-Jae;Lee, Shung-Hee;Kim, Jung-Woo;Kim, Ha-Won;Shim, Mi-Ja;Choi, Eung-Chil;Kim, Byong-Kak
    • The Korean Journal of Mycology
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    • v.13 no.4
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    • pp.203-212
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    • 1985
  • Of 450 strains isolated from the soil microbes collected in various locations in Korea, a strain had a strong inhibitory activity against bacterial ${\alpha}-amylase$ and was named strain DMC-72 of the genus Streptomyces. The amylase inhibitory metabolite produced by this strain was purified by means of acetone precipitation, adsorption on Amberlite IRC-50 and SP-Sephadex C-25. The inhibitor was found to be a derivative of oligosaccharides by spectral and chemical data. The inhibitor was stable at the pH range of $1{\sim}13$ and at $100^{\circ}C$ for half an hour, also inhibited other amylases such as salivary ${\alpha}-amylase$, pancreatic ${\alpha}-amylase$, fungal ${\alpha}-amylase$ and glucoamylase. However, it showed no inhibitory activity against ${\alpha}-glucosidase$, ${\beta}-glucosidase$, dextranase, and ${\beta}-amylase$. The kinetic studies of the inhibitor showed that its inhibitory effects on starch hydrolysis by ${\alpha}-amylase$ were noncompetitive.

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