Inhibitory potential of trilobatin from Lithocarpus polystachyus Rehd against α-glucosidase and α-amylase linked to type 2 diabetes

Dong, Hao; Li, Mei; Zhu, Feng; Liu, Fulai; Huang, Jianbo

doi:10.1016/j.foodchem.2011.07.030

Cited by 219 publications

(132 citation statements)

References 22 publications

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“…These results suggested that the rates of α-glucosidase catalyzed reactions were slowed down with the rise of quercetagetin concentration, and the K m value was not affected. Interestingly, trilobatin extracted from Lithocarpus polystachyus Rehd also exhibited a non-competitive inhibition of α-glucosidase inhibition and the K m value of trilobatin was 0.25 mM (Dong et al 2012).…”

Section: Abtsmentioning

confidence: 99%

“…Acarbose is a drug commonly applied in the management of diabetes mellitus (Dong et al 2012). As shown in Table 2, quercetagetin exhibited good α-glucosidase and α-amylase inhibitory activities.…”

Section: Abtsmentioning

confidence: 99%

“…There are many reports focused on its antioxidant activity (Gong et al 2012a, b;Xu et al 2014), antiinflammatory activity (Kang et al 2013) and copigment effect (Xu et al 2015). Some scientific researches reported that quercetin has strong inhibition of α-glucosidase, α-amylase and lipase (Dong et al 2012;You et al 2012). However, to the best of our knowledge, there were no investigation into α-glucosidase, α-amylase and pancreatic lipase inhibitory activities of quercetagetin by far.…”

Section: Introductionmentioning

confidence: 99%

“…toxicity have also been reported (Shobana et al 2009). Hence, some studies have focused on developing natural inhibitors of these enzymes from plants (Dong et al 2012;Marrelli et al 2013;You et al 2012). Recent findings indicate that inhibitory properties of the enzymes activity, in particular, correspond to the flavonoid compounds present in plants, such as quercetin and its glycoside derivatives, ellagic acid, chlorogenic acid, kaempferol, myricitrin and rutin (Marrelli et al 2013;Wang et al 2010;You et al 2012).…”

Section: Introductionmentioning

confidence: 99%

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In vitro antioxidant, anti-diabetic and antilipemic potentials of quercetagetin extracted from marigold (Tagetes erecta L.) inflorescence residues

Wang

Chen

et al. 2016

J Food Sci Technol

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Quercetagetin, the major flavonoid in marigold (Tagetes erecta L.) inflorescence residues was extracted and purified. The content of quercetagetin after the purification was 89.91 ± 0.26 %. The in vitro antioxidant activity of quercetagetin and its potential in controlling diabetes mellitus and obesity were investigated and compared to quercetin and rutin. The 50 % inhibitory concentration (IC 50 ) values of quercetagetin on scavenging 1, 1-diphenyl-2-picrylhydrazyl (DPPH), 2,2-azinobis-(3-ethylbenzothiazolin-6-sulfonic acid) (ABTS) and hydroxyl radicals were 27.12 ± 1.31 μmol/L, 12.16 ± 0.56 μmol/L and 1833.97 ± 6.66 μmol/L, respectively. The IC 50 values of quercetagetin on α-glucosidase, α-amylase and pancreatic lipase were 180.11 ± 3.68 μmol/L, 137.71 ± 3.55 μmol/L and 2327.58 ± 12.37 μmol/L, respectively. These results indicated that quercetagetin exhibited strong in vitro antioxidant, anti-diabetic and antilipemic activities. Lineweaver-Burk plots analysis elucidated that quercetagetin inhibited α-glucosidase and α-amylase non-competitively, while its inhibition against pancreatic lipase was involved in a mixed-type pattern. Moreover, strong correlations were found between ABTS ·+ /DPPH · scavenging activities and lipase inhibitory activity (R 2 > 0.90), as well as ·OH scavenging activity and α-amylase inhibitory activity (R 2 = 0.8967).

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Section: Abtsmentioning

confidence: 99%

Section: Abtsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

In vitro antioxidant, anti-diabetic and antilipemic potentials of quercetagetin extracted from marigold (Tagetes erecta L.) inflorescence residues

Wang

Chen

et al. 2016

J Food Sci Technol

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“…The α‐glucosidase inhibition activity was performed according to the slightly modified method of Kwon, Apostolidis, and Shetty (2008) and Dong, Li, Zhu, Liu, and Huang (2012). Total volume of the reaction mixture of 100 μl contained 70 μl 50 m m phosphate buffer saline, pH 6.8, 10 μl (0.5 m m ) test compound, followed by the addition of 10 μl (0.057 units) enzyme.…”

Section: Methodsmentioning

confidence: 99%

Anticancer, antithrombotic, antityrosinase, and anti‐α‐glucosidase activities of selected wild and commercial mushrooms from Pakistan

Sharif

Atta

Huma

et al. 2018

Food Science & Nutrition

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Mushrooms have been accepted as nutraceutical foods because of their high nutritional and functional values. They have also gained interest due to their medicinal properties, economic importance, and organoleptic merit. In this study, wild Ganoderma lucidum and four commercial mushrooms, that is, Pleurotus ostreatus, Volvariella volvacea, Hericium erinaceus, and Lentinus edodes from Pakistan were screened for their biological activities such as anticancer, antityrosinase, anti‐α‐glucosidase, and antithrombotic activities from their methanol, ethanol, and water extracts. Enzyme inhibition assay showed that selected mushrooms are potent inhibitors with %age inhibition ranging from 19.00% to 80.91%, and 32.85% to 83.38% for tyrosinase and α‐glucosidase, respectively. The best tyrosinase inhibition was shown by P. ostreatus whereas L. edodes was found best as α‐glucosidase inhibitor. These mushrooms were tested against cancer cell lines including HT‐29 colon and H‐1299 lungs carcinoma cell lines. G. lucidum showed 29% and 24% viability of cells against HT‐29 and H‐1299 cell lines, respectively. This antiproliferative effect was in dose‐dependent manner, and the maximum inhibition was observed at 200 μg/ml. Mushrooms extracts were also found effective against clot lysis. The percentage of clot lysis was in the range of 27%–29%. The research would provide knowledge to the people of Pakistan about the importance of locally available commercial mushrooms and wild mushrooms for health improvement and prevention against different kinds of diseases.

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Trilobatin as an HIV‐1 entry inhibitor targeting the HIV‐1 Gp41 envelope

et al. 2018

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HIV-1 transmembrane protein gp41 plays a crucial role by forming a stable six-helix bundle during HIV entry. Due to highly conserved sequence of gp41, the development of an effective and safe small-molecule compound targeting gp41 is a good choice. Currently, natural polyanionic ingredients with anti-HIV activities have aroused concern. Here, we first discovered that a glycosylated dihydrochalcone, trilobatin, exhibited broad anti-HIV-1 activity and low cytotoxicity in vitro. Site-directed mutagenesis analysis suggested that the hydrophobic residue (I564) located in gp41 pocket-forming site is pivotal for anti-HIV activity of trilobatin. Furthermore, trilobatin displayed synergistic anti-HIV activities combined with other antiretroviral agents. Trilobatin has a good potential to be developed as a small-molecule HIV-1 entry inhibitor for clinical combination therapy.

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Inhibitory potential of trilobatin from Lithocarpus polystachyus Rehd against α-glucosidase and α-amylase linked to type 2 diabetes

Cited by 219 publications

References 22 publications

In vitro antioxidant, anti-diabetic and antilipemic potentials of quercetagetin extracted from marigold (Tagetes erecta L.) inflorescence residues

In vitro antioxidant, anti-diabetic and antilipemic potentials of quercetagetin extracted from marigold (Tagetes erecta L.) inflorescence residues

Anticancer, antithrombotic, antityrosinase, and anti‐α‐glucosidase activities of selected wild and commercial mushrooms from Pakistan

Trilobatin as an HIV‐1 entry inhibitor targeting the HIV‐1 Gp41 envelope

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