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

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Antidiabetic Activity of an Ayurvedic Formulation Chaturmukha Rasa: A Mechanism Based Study

  • Sharma, Akansha;Tiwari, Raj K;Sharma, Vikas;Pandey, Ravindra K;Shukla, Shiv Shnakar
    • Journal of Pharmacopuncture
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    • v.22 no.2
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    • pp.115-121
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    • 2019
  • Objectives: The objective of this study was to evaluate antidiabetic activity of Chaturmukha rasa based on streptozotocin induced diabetes model, alpha amylase inhibitory activity, alpha Glucosidase inhibitory activity and inhibition of sucrase. Methods: Chaturmukha rasa was prepared as per Ayurvedic formulary. Antidiabetic activity was measured in experimentally streptozotocin induced rats. The dose was taken as 45 mg/kg, i.p. The antidiabetic activity of Chaturmukha rasa was compared Triphala Kwatha, a marketed formulation. Further In vitro $\acute{\alpha}$- Amylase Inhibitory Assay, In vitro salivary amylase Inhibitory Assay, In vitro ${\alpha}-Glucosidase$ Inhibitory Assay and In vitro Sucrase Inhibitory Assay was performed with respect to Chaturmukha rasa. The IC50 value was calculated for all the above activity. Results: Streptozotocin with Acarbose showed significant decrease in blood glucose level whereas streptozotocin with Triphala kwatha showed more decrease in blood glucose level than Streptozotocin with Acarbose. The combination of Streptozotocin + Triphala kwatha + Chaturmukha rasa showed a significant decrease in blood glucose level on 21st day. In vitro $\acute{\alpha}$- Amylase Inhibitory Assay the Chaturmukha rasa showed IC50 value $495.94{\mu}l$ when compared with Acarbose $427.33{\mu}l$, respectively. In the ${\alpha}-Glucosidase$ Inhibitory Assay Chaturmukha rasa showed IC50 value $70.93{\mu}l$ when compared with Acarbose $102.28{\mu}l$, respectively. In vitro Sucrase Inhibitory Assay Chaturmukha rasa showed IC50 value $415.4{\mu}l$ when compared with Acarbose $371.43{\mu}l$, respectively. Conclusion: This study supports that Chaturmukha rasa may inhibit diabetes by inhibition of salivary amylase or alpha Glucosidase or sucrase. This may be the mechanism by which Chaturmukha rasa inhibits diabetes. Further this study supports the usage of Chaturmukha rasa for the management of diabetes.

In vitro Antioxidant Activity and α-Glucosidase and Pancreatic Lipase Inhibitory Activities of Several Korean Sanchae (우리나라 일부 산채의 in vitro 산화 방지 활성, 알파-글루코시데이스와 췌장 라이페이스 저해 활성)

  • Ahn, Haecheon;Chung, Lana;Choe, Eunok
    • Korean Journal of Food Science and Technology
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    • v.47 no.2
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    • pp.164-169
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    • 2015
  • This study evaluated in vitro antioxidant activity, antioxidant content, and ${\alpha}$-glucosidase and pancreatic lipase inhibitory activities of ethanol extracts of samnamul (shoot of Aruncus dioicus), miyeokchwi (Solidago virgaurea), daraesoon (shoot of Actinidia arguta Planchon), and bangpungnamul (leaves of Ledebouriella seseloides), as muknamul, and fresh chamnamul (Pimpinella brachycarpa). Tocopherol content (4.8-78.3 mg/100 g) of sanchae was lower than polyphenols (4.4-12.2 g/100 g). Daraesoon with high tocopherol contents showed high antioxidant activity and ${\alpha}$-glucosidase and pancreatic lipase inhibitory activities. Samnamul had the highest levels of polyphenols and flavonoids, the highest antioxidant activity, and ${\alpha}$-glucosidase inhibition. Antioxidant activity was correlated with flavonoid content ($r^2=0.8895$), but was not correlated with the levels of other antioxidants tested, suggesting that polyphenol content in samnamul, miyeokchwi, daraesoon, bangpung, and chamnamul might not be critical determinant of antioxidant activity. Our results strongly suggest that samnamul and daraesoon could be useful in the treatment of diabetes and obesity.

Inhibition of $\alpha$-Glucosidase Activity by Quercetin (Quercetin에 의한 $\alpha$-glucosidase 활성 저해)

  • Lee, Dong-Sun;Kim, Jong-Guk;Lee, Sang-Han
    • Microbiology and Biotechnology Letters
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    • v.34 no.4
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    • pp.368-372
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    • 2006
  • Quercetin is a flavonoid molecule that is known to tie in various sources of natural products such as vegetables and fruits. It has been proven that quercetin plays a crucial role in the prevention of colon cancer as well as homeostasis as radical scavenger in human body. It is also well-known that glycosidases, including $\alpha$-glucosidase, are involved in a variety of degenerative metabolic disorders. In the course of screening useful $\alpha$-glucosidase inhibitors, we screened out quercetin as a $\alpha$-glucosidase inhibitor from chemical libraries. Quercetin was shown to be a reversible, slow-binding, and noncompetitive inhibitor of yeast a-glucosidase with a K$_i$ value of $6.3\times10^{-8}$ M when it was included with an enzyme mixture. Together, these results show that quercetin has potential in treating disorders including diabetes, although the further mechanistic study is needed.

Linoleic Acid from Bamboo (Phyllostachys Bambusoides) Displaying Potent α- Glucosidase Inhibition (대나무로부터 분리한 linoleic acid의 α-glucosidase 저해활성 연구)

  • Jung, Sun-In;Kang, Su-Tae;Choi, Cheol-Yong;Oh, Kyeong-Yeol;Cho, Jung-Keun;Rengasamy, Rajesh;Park, Ki-Hun
    • Journal of Life Science
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    • v.19 no.5
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    • pp.680-683
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    • 2009
  • Glycosidase inhibitors are major targets in the treatment of type II diabetes, cancer and viral infections. This study was carried out to investigate the glycosidase inhibitory substances from bamboo (Phyllostachys bambusoides). Bamboo was extracted with methanol and then further fractionated with n-hexane, chloroform, n-BuOH and aqueous to get an active fraction. All extracts were evaluated for ${\alpha}$-glucosidase inhibitory activities to identify the n-hexane fraction with 33.5 ${\mu}$g/ml of IC50 value. Active compound 1 in the n-hexane fraction was identified as linoleic acid, which exhibited inhibitory activity with 12.4 ${\mu}$M of IC50 value. Mechanistic analysis showed that linoleic acid exhibited noncompective inhibition. This is the first study in which bamboo is reported to show ${\alpha}$-glucosidase inhibitory activity.

Free radical scavenging and α-glucosidase inhibitory effects of a roots extract of Aruncus dioicus var. kamtschaticus (재배 삼나물 뿌리 추출물의 자유 라디칼소거 및 α-glucosidase 저해활성)

  • Jeong, Gyeong Han;Kim, Tae Hoon
    • Food Science and Preservation
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    • v.23 no.7
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    • pp.989-994
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    • 2016
  • As part of our continuing search for bioactive natural products, the antioxidant and ${\alpha}$-glucosidase inhibitory activities of an 80% methanolic extract and organic solvent soluble-portions of Aruncus dioicus var. kamtschaticus roots were investigated by using a bioassay system. The antioxidant activity of A. dioicus var. kamtschaticus roots extract and organic solvent soluble-portions were assessed by examining with 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) ($ABTS^+$) radical scavenging. In addition, anti-diabetic effects of the A. dioicus var. kamtschaticus root extract and organic solvent soluble-portions were tested via ${\alpha}$-glucosidase inhibition assay. The total phenolic contents of the products were determined by applying UV-VIS spectrophotometry. All tested samples showed dose-dependent radical scavenging and ${\alpha}$-glucosidase inhibitory properties. In particular, the ${\alpha}$-glucosidase inhibitory and radical scavenging effects of the ethyl-acetate (EtOAc)-soluble portion from the roots of A. dioicus var. kamtschaticus were greater than those from other solvent-soluble portions. These results indicate that A. dioicus var. kamtschaticus could be considered a new effective source of natural antioxidants and anti-diabetic materials. More systematic research of the constituents of the roots of this A. dioicus variety will be conducted to further develop its antioxidative and anti-diabetic properties.

Antioxidant and α-glucosidase inhibition activity of seaweed extracts (해조류 추출물의 항산화 및 α-glucosidase 저해 활성)

  • Kim, Jin-Hak;Kang, Hye-Min;Lee, Shin-Ho;Lee, Ju-Young;Park, La-Young
    • Food Science and Preservation
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    • v.22 no.2
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    • pp.290-296
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    • 2015
  • The antioxidant and ${\alpha}$-glucosidase inhibition activities of 10 kinds of seaweeds Ecklonia cava (EC), Ecklonia stolonifera (ES), Eisenia bicyclis (EB), Capsosiphon fulvescens (CF), Sargassum fulvellum (SF), Undaria pinnatifida (UP), Sargassum thunbergii (ST), Codium fragile (CFr), Hizikia fusiformis (HF), and Enteromorpha prolifera (EP) were investigated. Among all the tested seaweed extracts, the total polyphenol and flavonoid contents of the EB extract were highest 150.81 mg/g and 77.02 mg/g, respectively. The DPPH and ABTS radical scavenging abilities of the EB ethanol extract (1 mg/mL) were 86.26% and 99.71%, respectively, and its SOD-like activity and reducing power were 21.34% and 1.710 ($OD_{700}$). The ${\alpha}$-glucosidase inhibition activities of the EC, EB, and ST were above 98% at the 0.1 mg/mL concentration. These results suggest that seaweed extracts effectively prevent the what of antioxidants and decrease the blood glucose level, and may be used to develop various functional products.

Evaluation of antioxidant, α-glucosidase inhibition and acetylcholinesterase inhibition activities of Allium hookeri root grown in Korea and Myanmar (국내 및 미얀마에서 재배된 삼채뿌리의 항산화, α-Glucosidase 저해 및 Acetylcholinesterase 저해 활성)

  • Park, Joo Young;Yoon, Kyung Young
    • Food Science and Preservation
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    • v.23 no.2
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    • pp.239-245
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    • 2016
  • This study was conducted to compare the functionality (antioxidant, anti-diabetic, and anti-dementia activities) of the methanol extract of Allium hookeri root grown in Korea (KR) and Myanmar (MR). The total polyphenol and flavonoid contents of KR and MR were 5.27 and 4.80 mg GAE/g, and 0.35 and 0.24 mg QE/g, respectively. KR contained significantly higher levels of total polyphenols and total flavonoids than those of MR (p<0.05). The IC50 values of KR and MR were 6.53 and 5.31 mg/mL, respectively, for DPPH radical scavenging activity. However, KR had a significantly higher ABTS radical scavenging activity, $Fe^{2+}$ chelating ability, and reducing power compared with those of MR (p<0.05). In the evaluation of anti-diabetic activity, KR showed significantly higher ${\alpha}-glucosidase$ inhibition activity than acarbose and MR at whole concentrations (p<0.05). KR and MR had acetylcholinesterase inhibition activities that of 51.44% and 44.33%, respectively, at a 50 mg/mL concentration. These results suggested that roots of A. hookeri, especially KR, could be useful in improving diabetic and dementia disorders due to their high antioxidant, anti-diabetic, and anti-dementia activities.

Antioxidant Properties of Water Extract from Acorn

  • Yin, Yu;Heo, Seong-Il;Jung, Mee-Jung;Wang, Myeong-Hyeon
    • Journal of Applied Biological Chemistry
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    • v.50 no.2
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    • pp.70-73
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    • 2007
  • Antioxidant and anti-diabetic activities of acorn were evaluated by its potential for scavenging stable DPPH free radical, inhibition of lipid peroxidation, reducing power, and inhibiton of ${\alpha}-glucosidase\;and\;{\alpha}-amylase$. The water extract of acorn exhibited strong antioxidant and antidiabetic related activities in the tested model systems. Solvent fractionation of the water extract revealed that the water fraction and the EtOAc fraction had strong antioxidant activity, and inhibitory activity on ${\alpha}-glucosidase\;and\;{\alpha}-amylase$. The water fraction exhibited higher DPPH radical scavenging activity ($EC_{50}=7.19{\mu}g/mL$) than that of ${\alpha}-tocopherol\;(EC_{50}=7.59{\mu}g/mL)$. It is considered that water extract of acorn has the potential for natural antioxidant and anti-diabetic products.

Isolation and Characterization of α-glucosidase Inhibitors from Euonymus alatus (화살나무(Euonymus alatus)로 부터 α-glucosidase 저해 물질의 분리 및 동정)

  • Kim, Shin-Duk
    • Microbiology and Biotechnology Letters
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    • v.45 no.4
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    • pp.311-315
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    • 2017
  • ${\alpha}$-glucosidase inhibitory compounds (1-4) in a 50% methanol extract of Euonymus alatus were isolated by activity-based fractionations and the structures determined on the basis of chemical and spectral characterization techniques such as $^1H$ and $^{13}C$ nuclear magnetic resonance spectroscopy, $^1H-^1H$ correlation spectroscopy (COSY), and heteronuclear multiple bond correlation (HMBC). The compounds 1-4 belong to flavonols and exhibited potent inhibitory activities against ${\alpha}$-glucosidase, with $IC_{50}$ values of 25.3, 17.1, 47.3, and $35.1{\mu}M$, respectively. All the isolated compounds were more potent than the positive control acarbose. This is the first report describing the potential hypoglycemic effect of Euonymus alatus through ${\alpha}$-glucosidase inhibition and identification of its active components.

Characteristics of Cellulomonas fimi $\beta$-glucosidase expressed in Escherichia coli (대장균에서 발현되는 Cellulomonas fimi $\beta$-glucosidase의 효소학적 특징)

  • Kim, Ha-Kun
    • The Journal of Natural Sciences
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    • v.8 no.2
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    • pp.57-61
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    • 1996
  • The $\beta$-glucosidase enzyme was purified from E. coli carrying Cellulomonas fimi $\beta$-glucosidase gene. SDS-PAGE and analytical gel filtration revealed that molecular weight of this enzyme was 56,000 dalton and consisted of a single polypeptide.Inhibition caused by heavy metals and activation by dithiothreitol suggest the existence of essential thiol group in the enzyme. The enzyme was not active on maltose (glucose $\alpha$-1,4-glucose) which has a $\alpha$-linkage, whereas it was active on lactose (glucose $\beta$-1,4-glucose), PNPG (p-nitrophenyl $\beta$-D-glucopyranoside) and PNPC (p-nitrophenyl $\beta$-D-cellobioside), although its reaction rates were different.

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