α-Glucosidase inhibition by luteolin: Kinetics, interaction and molecular docking

Yan, Jiakai; Zhang, Guowen; Pan, Junhui; Wang, Yajie

doi:10.1016/j.ijbiomac.2013.12.007

Cited by 264 publications

(182 citation statements)

References 47 publications

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“…Compounds 16, 17, and 19 have all previously been reported as α-glucosidase inhibitors [42,43], but this is the first report of the α-glucosidase inhibitory activity of 20, 26, and 29. Compounds 16, 19, 20, 26, and 29 all showed higher α-glucosidase inhibitory activity than the clinically approved antidiabetic drug acarbose (Table 1), which supports the use of Eremanthus as an antidiabetic herbal medicine.…”

Section: Isolation and Pharmacological Evaluation Of The α-Glucosidasmentioning

confidence: 83%

High-Resolution α-Glucosidase Inhibition Profiling Combined with HPLC-HRMS-SPE-NMR for Identification of Antidiabetic Compounds in Eremanthus crotonoides (Asteraceae)

et al. 2016

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α-Glucosidase inhibitors decrease the cleavage-and absorption rate of monosaccharides from complex dietary carbohydrates, and represent therefore an important class of drugs for management of type 2 diabetes. In this study, a defatted ethyl acetate extract of Eremanthus crotonoides leaves with an inhibitory concentration (IC 50 ) of 34.5 µg/mL towards α-glucosidase was investigated by high-resolution α-glucosidase inhibition profiling combined with HPLC-HRMS-SPE-NMR. This led to identification of six α-glucosidase inhibitors, namely quercetin (16), trans-tiliroside (17), luteolin (19), quercetin-3-methyl ether (20), 3,5-di-O-caffeoylquinic acid n-butyl ester (26) and 4,5-di-O-caffeoylquinic acid n-butyl ester (29). In addition, nineteen other metabolites were identified. The most active compounds were the two regioisomeric di-O-caffeoylquinic acid derivatives 26 and 29, with IC 50 values of 5.93 and 5.20 µM, respectively. This is the first report of the α-glucosidase inhibitory activity of compounds 20, 26, and 29, and the findings support the important role of Eremanthus species as novel sources of new drugs and/or herbal remedies for treatment of type 2 diabetes.

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Section: Isolation and Pharmacological Evaluation Of The α-Glucosidasmentioning

confidence: 83%

High-Resolution α-Glucosidase Inhibition Profiling Combined with HPLC-HRMS-SPE-NMR for Identification of Antidiabetic Compounds in Eremanthus crotonoides (Asteraceae)

et al. 2016

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“…The results also show that the K SV values increased with increasing temperature, suggesting that quenching proceeded mainly through a dynamic mechanism of collisions between OA and tryptophans. This relationship may also be described by the equation log (Yan et al, 2014), where K A is the binding constant, and n the number of binding sites on the protein (Figure 6). It can be observed that both K A and n rose with the increase in temperature, showing again that the OA/α-glucosidase interaction was favored under warmer conditions.…”

Section: Fluorescence Quenching Of α-Glucosidase By Oleanolic Acidmentioning

confidence: 99%

Free radical scavenging and α-glucosidase inhibition, two potential mechanisms involved in the anti-diabetic activity of oleanolic acid

et al. 2016

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SUMMARY:This work investigates the role of oleanolic acid (OA), isolated from the olive (Olea europaea L.) leaf, as a radical scavenger and inhibitor of the hydrolyzing enzymes of dietary carbohydrates. New evidence is provided showing that OA may capture 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) and peroxyl radicals, and also exert a strong and non-competitive inhibition of α-glucosidase (IC 50 10.11 ± 0.30 µM). The kinetic and spectrometric analyses performed indicate that OA interacts with this enzyme inside a hydrophobic pocket, through an endothermic and non spontaneous process of a hydrophobic nature. These are two possible mechanisms by which OA may facilitate a better control of post-prandial hyperglycaemia and oxidative stress, so contributing to preserving insulin signalling. Obesity, insulin resistance and Type 2 Diabetes Mellitus are considered the first pandemics of the 21st century. In this sense, OA might be used in future preventive and therapeutic strategies, as an ingredient in new drugs and functional foods.KEYWORDS: Anti-diabetic activity; Antioxidant; α-glucosidase inhibitor; Olea europaea; Oleanolic acid RESUMEN: La Captación de radicales libres y la inhibición de α-glucosidasa, dos posibles mecanismos involucrados en la actividad antidiabética del ácido oleanólico. Este trabajo estudia el papel del ácido oleanólico (OA), aislado de la hoja de olivo, como secuestrador de radicales libres e inhibidor de enzimas implicados en la hidrolisis de los carbohidratos de la dieta, dos mecanismos por los que el triterpeno podría mitigar la hiperglicemia postprandial y el estrés oxidativo. Se aportan nuevas evidencias que muestran que el OA puede capturar radicales ácido 2,2'-azino-bis-(3-etilbenzotiazolín)-6-sulfónico y peroxilo, y que ejerce una potente inhibición nocompetitiva de α-glucosidasa (IC 50 10.11±0.30 µM). El análisis cinético y espectrométrico llevado a cabo indica que OA interacciona con este enzima en el interior de un bolsillo hidrofóbico, mediante un proceso endotér-mico no espontáneo, de naturaleza hidrofóbica. Estos son dos posibles mecanismos por los cuales el OA puede facilitar un mejor control de la hiperglucemia postprandial y el estrés oxidativo, lo que contribuye a preservar la señalización de la insulina. La obesidad, la resistencia a la insulina y la diabetes mellitus tipo 2 se consideran la primera pandemia del siglo XXI. En este sentido, el OA podría ser utilizado en futuras estrategias preventivas y terapéuticas, como ingrediente de nuevos fármacos y alimentos funcionales. Free radical scavenging and α-glucosidase inhibition, two potential mechanisms involved in the anti-diabetic activity of oleanolic acid. Grasas Aceites 67 (3): e142. doi: http://dx

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“…Assay of XO activity was carried out by ultraviolet-visible (UV-vis) spectroscopy as reported earlier [18] with minor modifications by using a UV-2450 spectrophotometer (Shimadzu, Japan) with a 1.0 cm quartz cell. Briefly, a series of assay solutions prepared in Tris-HCl buffer (0.05 mol L −1 , pH 7.4) consisting of a constant concentration of XO (7.5 × 10 −8 mol L −1 ) and various amounts of inhibitor solutions were incubated for 3 h at 37 • C. Then the assay was initiated by adding the substrate xanthine (final concentration was 5.0 × 10 -5 mol L −1 ) to the 2.0 mL reaction mixture.…”

Section: Enzyme Activity Assaymentioning

confidence: 99%

Inhibition of chrysin on xanthine oxidase activity and its inhibition mechanism

Lin

Zhang

Liao

et al. 2015

International Journal of Biological Macromolecules

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α-Glucosidase inhibition by luteolin: Kinetics, interaction and molecular docking

Cited by 264 publications

References 47 publications

High-Resolution α-Glucosidase Inhibition Profiling Combined with HPLC-HRMS-SPE-NMR for Identification of Antidiabetic Compounds in Eremanthus crotonoides (Asteraceae)

High-Resolution α-Glucosidase Inhibition Profiling Combined with HPLC-HRMS-SPE-NMR for Identification of Antidiabetic Compounds in Eremanthus crotonoides (Asteraceae)

Free radical scavenging and α-glucosidase inhibition, two potential mechanisms involved in the anti-diabetic activity of oleanolic acid

Inhibition of chrysin on xanthine oxidase activity and its inhibition mechanism

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