• Title/Summary/Keyword: ${\alpha}-glucosidase$ inhibition

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Antiviral activity of methanol extract from Ephedra sinica Stapf (마황 추출물의 항바이러스 활성)

  • Lee, Doseung;Lee, Dong-Sun
    • Food Science and Preservation
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    • v.21 no.5
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    • pp.735-739
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    • 2014
  • Ephedra sinica Stapf, known as a medicinal plant, inhibited not only syncytium formation, but also trafficking of viral glycoprotein, hemagglutinin-neuramidase (HN) to the cell-surface. Trafficking of viral glycoprotein to the surface of infected-cells results in syncytium formation in Newcastle disease virus (NDV)-infected baby hamster kidney (BHK) cells. Viral glycoprotein in the infected-cell is processed within the endoplasmic reticulum during routing into surface. The processing of viral glycoprotein like a N-linked oligosaccharide trimming by ${\alpha}$-glucosidase in cell is necessary for virus infection. Methanol extracts showed inhibitory activities ($IC_{50}$ $15{\mu}g/mL$) against ${\alpha}$-glucosidase. This suggested that E. sinica extracts inhibited the cell-surface expression of NDV-HN glycoprotein without significantly affecting HN glycoprotein synthesis in NDV-infected BHK cells.

Anti-diabetic and Hypoglycemic Effect of Eleutherococcus spp. (오갈피나무 속(屬) 식물의 항당뇨 및 혈당강하 효과)

  • Lim, Sang-Hyun;Park, Yu-Hwa;Kwon, Chang-Ju;Ham, Hun-Ju;Jeong, Haet-Nim;Kim, Kyung-Hee;Ahn, Young-Sup
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.39 no.12
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    • pp.1761-1768
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    • 2010
  • Hypoglycemic effect through activity inhibition of $\alpha$-glucosidase and $\alpha$-amylase was evaluated using leaves of Eleutherococcus senticosu, Eleutherococcus gracilistylus, Eleutherococcus sieboldianus and Eleutherococcus sessiliflorus which belong to Acanthopanax sessiliflorus genus. As a result of measuring $\alpha$-glucosidase activity inhibition, extract of Eleutherococcus gracilistylus showed around 43.38% of activity inhibition compared with acarbose and extract of Eleutherococcus senticosu showed 41.24% inhibitory effect. As a result of measuring $\alpha$-amylase activity inhibition, acarbose showed 73.25% of activity inhibition in 10 mg/mL concentration, and the extract of Eleutherococcus senticosu leaves showed 91.90% higher activity inhibition compared with acarbose. Also, after subjects in a model were induced diabetes with streptozotocin (STZ) intake plant extract from Acanthopanax sessiliflorus for 2 weeks, effect of improving blood glucose level and fat was examined. In all groups with specimen, Eleutherococcus senticosu (T1), Eleutherococcus gracilistylus (T2), Eleutherococcus sieboldianus (T3) and Eleutherococcus sessiliflorus (T4), blood glucose level was significantly decreased compared with that in control group (C). In an experiment of examining changes in fat concentration in blood, total cholesterol content increased in a control group compared with a normal, while in T1, T3 and T4, it decreased significantly compared with the control group. As for HDL-cholesterol, it significantly increased in all diabetes induced groups compared with the normal group, and in T3, it increased the most significantly by 55.61% compared with the control group. In case of LDL-cholesterol, specific difference between the normal group and the control group was not found; however, significant increase was detected in T2 and T3, whereas in T1 and T4, it decreased significantly compared with the control group. As for triglyceride, its concentration increased in the control group like total cholesterol. It decreased 60.16% in T3, 60.80% in T4 and 50.16% in T1 compared with the control group. As a result of measuring the concentration of triglyceride in extracted liver, the control group showed significant increase compared with the normal group, whereas T1 and T2 showed significant decrease compared with the normal group. The above results show that extracts from Acanthopanax sessiliflorus genus are effective for hypoglycemic and improving fat metabolism due to diabetes.

Biological activity and analysis of α-glucosidase inhibitor from mulberry (Morus alba L.) wine (오디와인의 생리활성 및 α-glucosidase 저해제의 분석)

  • Son, Woo-Rim;Choi, Sang-Won
    • Food Science and Preservation
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    • v.20 no.6
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    • pp.877-885
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    • 2013
  • Wine extracts of four different berry fruits, such as mulberry, blueberry, strawberry, and raspberry, were investigated for antioxidant, anti-tyrosinase, and ${\alpha}$-glucosidase activities by using in vitro assays. Additionally, quantitative changes of ${\alpha}$-glucosidase inhibitor in mulberry wine were determined by HPLC according to mulberry cultivars and fermentation process. Among four berry wines examined, mulberry wine showed the most potent ${\alpha}$-glucosidase inhibitory activity with 69.37% at 0.23 mg/mL, while blueberry and strawberry wines exhibited the strongest inhibition against DPPH radical and tyrosinase activity, respectively. Four compounds were isolated and purified from mulberry wine by a series of isolation procedures, such as solvent fractionation, and Diaion HP-20, ODS-A, and Sephadex LH-20 column chromatographies. Among them, Comp. 4 exerted the strongest ${\alpha}$-glucosidase inhibitory activity ($I_C_{50}=31.57{\mu}M$), and its chemical structure was identified as quercetin by UV and NMR spectral analysis. Finally, the "Daeseongppong" (16.83 ppm) muberry wine had larger amount of quercetin than the "Iksuppong" (14.85 ppm) and "Cheongilppong" (8.92 ppm) mulberry wines, but their contents of three mulberry wines decreased considerably with aging process. These results suggest that mulberry wine containing quercetin acted as ${\alpha}$-glucosidase inhibitor may be useful as a potential functional wine for improving diabetic disorder.

Antioxidant and α-Glucosidase Inhibitory Activities of the Extract from Sparganium stoloniferum Buch.-Ham. Root and Its Constituent Compounds

  • Xu, Ming Lu;Wang, Lan;Hu, Jian He;Wang, Myeong-Hyeon
    • Preventive Nutrition and Food Science
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    • v.14 no.4
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    • pp.354-357
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    • 2009
  • Three compounds, vanillic acid, p-hydroxylcinnamic acid, p-hydroxybenzaldehyde have been isolated from the ethylacetate extract of Sparganium stoloniferum Buch.-Ham roots using silica gel open column chromatography, preparative thin-layer chromatography (pTLC) and reverse phase high performance liquid chromatography. The structures of the compounds were established on the basis of IR, extensive 1D NMR, and MS analyses. The ethylacetate (EtOAc) extract, vanillic acid, and p-hydroxybenzaldehyde showed $\alpha$-glucosidase inhibition activity of 72.71%, 20.13%, and 30.42%, at the concentration of 10 ${\mu}g/mL$, respectively. The EtOAc extract exhibited strong antioxidant activity with an $IC_50$ value of 24.37 ${\mu}g/mL$ against DPPH radical scavenging activity, the vanillic acid, p-hydroxylcinnamic acid, and p-hydroxybenzaldehyde with an $IC_50$ value of 2.10 ${\mu}M$, 1.59 ${\mu}M$, and 2.72 ${\mu}M$ against DPPH, respectively.

ISOLATION OF A NEW $\alpha$-GLUCOSIDASE INHIBITOR FROM A FUNGUS, PENICILLIUM SP. F70614

  • Kwon, Oh-Sung;Park, Sang-Ho;Lee, Sang-Hwa;Park, Dong-Jin;Yun, Bong-Sik;Kim, Chang-Jin
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1998.11a
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    • pp.134-134
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    • 1998
  • The modulation of glycosidase activity by inhibitors is of great interest. Such compounds have been shown to be important tools in mechanistic studies on glycohydrolase as well as having promising therapeutic application. An ${\alpha}$-glucosidase inhibitor was isolated from culture filterates of Penicillium sp. The inhibitor was active against ${\alpha}$-glucosidase isolated from yeast and porcine small intestine. However, it showed no inhibition to Aspergillus ${\alpha}$-galactosidase, Escherichia coli ${\beta}$-galactosidase, and jack bean ${\alpha}$-mannosidase. The inhibitor was highly soluble in ether, methanol and chloroform. The inhibitor was purified using silica gel, Sephadex LH-20 column chromatography and reverse-phase HPLC. The inhibitory compound designated PA-7(IC$\sub$50/=35$\mu\textrm{g}$) was obtained as white powder. The structure of PA-7 was determined with spectroscopic data of EI-MS, FAB-MS, $^1$H, and $\^$13/C NMR. The inhibitor has a diketopiperazine moiety.

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Comparative analysis of Bombyx batryticatus and Bombyx mori on α-glucosidase inhibition and their bioactive compositions

  • Hwa Lee;Jong-Hoon Kim
    • International Journal of Industrial Entomology and Biomaterials
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    • v.48 no.3
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    • pp.156-162
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    • 2024
  • This study aimed to evaluate and compare the inhibitory effects of extracts from Bombyx batryticatus (BBE) and Bombyx mori (BME) on α-glucosidase, DPP-4, and LDL oxidation activities, focusing on their potential applications in managing postprandial hyperglycemia and metabolic syndrome. The results demonstrated that both BBE and BME effectively inhibited α-glucosidase and LDL oxidation, with BBE exhibiting higher inhibitory activity than BME. HPLC analysis identified linolenic acid, linoleic acid, linolenic acid ethyl ester, pheophorbide a, and pyropheophorbide a as key compounds contributing to these effects. Notably, the identified unsaturated fatty acids and pheophorbides showed strong α-glucosidase inhibitory activity, surpassing that of acarbose, a standard diabetic drug. These results suggest that, in addition to the previously reported 1-DNJ and fibroin proteins, unsaturated fatty acids and chlorophyll-derived pheophorbides may play significant roles in glycemic control. Compounds, particularly those from BBE, present promising opportunities for the development of natural therapeutic agents for diabetes management. The study concludes that BBE and BME have strong potential as functional ingredients in future diabetes treatment strategies, possibly offering enhanced efficacy over conventional inhibitors.

Antioxidant and Anti-diabetes Activities of Methanolic Extract and Fractions of Astragalus membranaceus Roots

  • Park, Jae-Hyo;Yin, Yu;Wang, Myeong-Hyeon
    • Preventive Nutrition and Food Science
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    • v.15 no.1
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    • pp.30-35
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    • 2010
  • The potential biological activities of methanol extract and 5 fractions (hexane, $CH_2Cl_2$, EtOAc, BuOH and water) from roots of Astragalus membranaceus were examined by 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, hydroxyl radical (${\cdot}OH$) scavenging activity, reducing power assays, lipid peroxidation inhibitory activity, $\alpha$-amylase and $\alpha$-glucosidase inhibition assays. The EtOAc fraction showed high DPPH free radical scavenging activity ($EC_{50}=170.34\;{\mu}g/mL$), hydroxyl radical scavenging activity ($EC_{50}=32.14\;{\mu}g/mL$), lipid peroxidation inhibitory activity ($EC_{50}=52.46\;{\mu}g/mL$) and a concentration dependence, with OD value ranging from 0.234 to 0.345 (0.1 to 0.5 mg/mL), for reducing power. The EtOAc fraction has the highest total phenolic content ($142.13\;Gal\;{\mu}g/mg$) and the $CH_2Cl_2$ fraction has the highest flavonoid content ($71.63\;Que\;{\mu}g/mg$). Meanwhile, hexane and EtOAc showed certain $\alpha$-amylase and $\alpha$-glucosidase inhibition activities. These results suggest that the methanol extract and fractions from Astragalus membranaceus root have significant antioxidant and anti-diabetes activities, which could be used as a potential source of pharmaceutical materials.

Biological Activities of Water and Ethanol Extracts from Two Varieties of Rubus coreanus Miquel Fruits

  • Yin, Yu;Wang, Myeong-Hyeon
    • Preventive Nutrition and Food Science
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    • v.16 no.1
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    • pp.89-94
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    • 2011
  • The potential biological activities of water and ethanol extracts from two varieties of Rubus coreanus Miquel fruits produced in the Gochang-gun (GR) and Hoengseong-gun (HR) regions of Korea were examined. The hydroxyl radical ($\cdot$OH) scavenging activity, reducing power, lipid peroxidation inhibitory activity, and antiproliferative activity on cancer cells by these extracts were examined, and $\alpha$-amylase and $\alpha$-glucosidase inhibition assays were also performed. The EtOH extract from GR showed high hydroxyl radical scavenging activity ($EC_{50}=119.47{\pm}5.13\;{\mu}g/mL$), lipid peroxidation inhibitory activity ($EC_{50}=213.45{\pm}3.14\;{\mu}g/mL$) and a concentration dependence, with OD values ranging from 0.15 to 0.56 (50 to 200 ${\mu}g/mL$), for reducing power. The EtOH extract from GR has the highest antiproliferative activities on MDA-MB-231 and HepG2 cancer cells among four extracts. Meanwhile, all extracts showed certain $\alpha$-amylase and $\alpha$-glucosidase inhibition activities. These results indicate that extracts from two varieties of R. coreanus fruits have significant antioxidant, anti-diabetic and anti-tumorigenic activities, which suggest these extracts could be a potential source for pharmaceutical.

Antioxidant Activities and α-Glucosidase Inhibitory Effect of Water Extracts from Medicinal Plants (약용식물 물 추출물의 항산화 활성 및 α-Glucosidase 저해효과)

  • Kim, Hyun Sook;Kim, Tae Woo;Kim, Dae Jung;Lee, Jae Sung;Kim, Kyoung Kon;Choe, Myeon
    • Korean Journal of Medicinal Crop Science
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    • v.21 no.3
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    • pp.197-203
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    • 2013
  • We studied the total polyphenol content, DPPH radical scavenging activity, hydroxyl radical scavenging activity and ${\alpha}$-glucosidase inhibition of water extracts from 17 medicinal plants. Total polyphenol contents ranged from 10.0 (Coix lachryma-jobi L, CL) ~ 279.7 (Perilla sikokiana, PS)mg/g. The water extract from medicinal plants were evaluated for its free radical scavenging activities and compared with a commercial antioxidant, ascorbic acid. DPPH radical scavenging activity of Pyrus pyrifolia (PP), Chamaecyparis obtusa L. (COL), Chamaecyparis obtusa F. (COF), and PS were higher than positive control. Higher hydroxyl radical scavenging activity were shown in Acanthopanax senticosus (AS) and Cordyceps militaris (CM) than the other plants. The highest anti-${\alpha}$-glucosidase activity was observed in Cornus officinalis (CO) and Paeonia suffruticosa Andrews (PSA) water extracts. PSA showed not only the higher DPPH radical scavenging activity but also the anti-${\alpha}$-glucosidase activity. The results of our study that PP, COL, COF, PS, AS, CM, CO and PSA could be potential candidates for natural antioxidants.

Screening for Anti-diabetic Effects of Prescribed Korean Traditional Medicines

  • Shin, Seon Mi;Jeong, Yong Joon;Park, Dae Won;Ko, Heung;Kim, Gi Tae;Kim, Ee-Hwa;Kim, Taeseong;Sohn, Eun-Hwa;Kwon, Jung-Eun;Koo, Hyun Jung;Kang, Se Chan
    • Korean Journal of Plant Resources
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    • v.25 no.6
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    • pp.670-681
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    • 2012
  • Herb extracts commercially used in Korea were screened for PPAR-${\gamma}$ agonist test and ${\alpha}$-glucosidase inhibition assay. Total 16 herb plants had a PPAR-${\gamma}$ agonist activity. Specially, Alisma orientale Juz (108.41%), Ephedra sinica (98.22%), Sasa japonica Makino var. purpurascens Nakai (140.68%), Astragalus membranaceus Bunge (106.79%) and Cnidium officinale Makino (113.00%) showed high PPAR-${\gamma}$ agonist activity rate compared with rosiglitazone's (167.46%). And Cornus officinalis S. et Z. (90.3%), Cinnamomum cassia Blume (89.2%), Psoralea corylifolia L. (89.8%), Paeonia japonica (Makino) Miyabe (92.4%) and Paeonia suffruticosa Andr (93.2%), showed high ${\alpha}$-glucosidase inhibition rates. These results support previous reports of the efficacy of Oriental medicinal plants used for diabetes mellitus.