Potent α-Glucosidase Inhibitors Isolated from Ginkgo biloba 
 Leaves

Sukito, Agus; Tachibana, Sanro

doi:10.3923/pjbs.2014.1170.1178

Cited by 7 publications

(5 citation statements)

References 17 publications

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“…Various mechanisms have been reported, regarding the cytotoxic and anticancer activities of GA. They activate protein phosphatase 2C (PP2C) [4] and inhibit fatty acid synthase (FAS) [29], and α-glucosidase [30]. In addition, GA inhibited de novo lipogenesis in cancer cells by activating AMPK signaling and lowering the expression of enzymes involved in lipogenesis, including acetyl-CoA carboxylase (ACC), fatty acid synthase (FASN) [14].…”

Section: Discussionmentioning

confidence: 99%

Ginkgolic acids inhibit migration in breast cancer cells by inhibition of NEMO sumoylation and NF-κB activity

Hamdoun

Efferth

2017

Oncotarget

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Ginkgolic acids (GA), a group of alkyl phenols found in crude extracts of Ginkgo biloba leaves, are known to have anticancer activity, but their mode of action is not well understood. Our aim in this study was to investigate the anti-migratory activity of seven GA against breast cancer cells and to determine the molecular mechanism behind this activity. All seven GA and their mixture inhibited wound healing in MCF-7 and MDA-MB 231 breast cancer cells. None of the compounds nor the mixture showed cytotoxicity towards the two cell lines, if tested by the resazurin assay. C13:0 inhibited NF-κB activity in the HEK Blue Null 1 reporter cell line. Furthermore, C13:0 inhibited degradation of nuclear factor of κ-light polypeptide gene enhancer in B-cells inhibitor α (IκBα). Sumoylation assay revealed that GA inhibited sumoylation of NF-κB essential modulator (NEMO). Molecular docking on SUMO-activating enzyme E1 showed that the seven GA bound to the active adenylation site with high calculated affinities ranging from -10.28 to -12.27 kcal/mol. Quantitative RT-PCR using C15:0, C13:0 and the mixture showed a significant down-regulation of urokinase plasminogen activator (uPA), plasminogen activator inhibitor-1 (PAI-1), C-X-C chemokine receptor type 4 (CXCR4) and matrix metalloproteinase 9 (MMP-9). We conclude that GA revealed considerable anti-migratory activity at non-cytotoxic concentrations, indicating anti-metastatic activity with low toxicity. This effect can be explained by the inhibition of NEMO sumoylation leading to inhibition of IκBα degradation and consequently a reduction of NF-κB activity, leading to the down-regulation of metastasis related genes including uPA, PAI-1, CXCR4, and MMP-9.

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Section: Discussionmentioning

confidence: 99%

Ginkgolic acids inhibit migration in breast cancer cells by inhibition of NEMO sumoylation and NF-κB activity

Hamdoun

Efferth

2017

Oncotarget

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“…α-Glucosidase inhibitors reduce the rate of carbohydrate digestion and delay carbohydrate absorption in the digestive tract. Therefore, α-glucosidase inhibitors have the potential to prevent the development of type 2 diabetes by lowering after-meal glucose levels 11 . Plants and microorganisms are known as rich sources of α-glucosidase inhibitors 11 .…”

Section: Introductionmentioning

confidence: 99%

Development of novel Meju starter culture using plant extracts with reduced Bacillus cereus counts and enhanced functional properties

Shukla̽

Park

et al. 2017

Sci Rep

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We developed a novel type of Meju starter culture using single and combined extracts of Allium sativum (garlic clove), Nelumbo nucifera (lotus leaves), and Ginkgo biloba (ginkgo leaves) to improve the quality and functionality of Meju-based fermented products. Meju samples fermented with plant extracts (10 mg/ml) showed phenolic contents of 11.4–31.6 mg/g (gallic acid equivalents). Samples of extracts (garlic clove, lotus leaves, ginkgo leaves and their combination) fermented with Meju strongly inhibited tyrosinase, α-glucosidase, and elastase activities by 36.43–64.34%, 45.08–48.02%, and 4.52–10.90%, respectively. Specifically, ginkgo leaves extract added to fermented Meju samples at different concentrations (1% and 10%) strongly inhibited tyrosinase, α-glucosidase, and elastase activities and exhibited a potent antibacterial effect against Bacillus cereus with a significant reduction in bacterial counts compared with the effects observed for garlic clove and lotus leaf added to Meju samples. Scanning electron microscopy revealed severe morphological alterations of the B. cereus cell wall in response to ginkgo leaf extracts. Gas chromatographic mass spectroscopic analysis of plant extract-supplemented Meju samples and control Meju samples identified 113 bioactive compounds representing 98.44–99.98% total extract. The proposed approach may be useful for the development of various fermented functional foods at traditional and commercial levels.

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“…(2020) , carnosol (44) displayed a competitive inhibition (Ki =5.57 μg/mL) on α-glucosidase with IC 50 value of 12.0 ± 0.8 μg/mL, and showed much stronger inhibitory effect than acarbose (IC 50 = 412 ± 26 μg/mL). Ginkgolic acid (C13:0) (62) revealed higher α-glucosidase inhibitory activity (IC 50 = 3.5 ± 0.13 μg/mL) than the positive control quercetin (IC 50 = 3.8 ± 0.12 μg/mL) ( Sukito and Tachibana, 2014 ).…”

Section: Resultsmentioning

confidence: 99%

Phytochemical Analysis, Antioxidant, Antibacterial, Cytotoxic, and Enzyme Inhibitory Activities of Hedychium flavum Rhizome

Tian

et al. 2020

Front. Pharmacol.

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Potent α-Glucosidase Inhibitors Isolated from Ginkgo biloba Leaves

Cited by 7 publications

References 17 publications

Ginkgolic acids inhibit migration in breast cancer cells by inhibition of NEMO sumoylation and NF-κB activity

Ginkgolic acids inhibit migration in breast cancer cells by inhibition of NEMO sumoylation and NF-κB activity

Development of novel Meju starter culture using plant extracts with reduced Bacillus cereus counts and enhanced functional properties

Phytochemical Analysis, Antioxidant, Antibacterial, Cytotoxic, and Enzyme Inhibitory Activities of Hedychium flavum Rhizome

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