α-Glucosidase inhibitory effect of rhinacanthins-rich extract from Rhinacanthus nasutus leaf and synergistic effect in combination with acarbose

Shah, Muhammad Ajmal; Khalil, Ruqaiya; Ul-Haq, Zaheer; Panichayupakaranant, Pharkphoom

doi:10.1016/j.jff.2017.07.021

Cited by 47 publications

(15 citation statements)

References 28 publications

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“…Synergistic effect between two different α‐glucosidase inhibitors has been previously recognized as a prominent therapeutic approach in lowering postprandial hyperglycemia [32] . To further evaluate the synergistic inhibitory effect of the three compounds on α‐glucosidase, an isobologram was conducted at three different concentrations at 1 / 4 IC 50 , 1 / 2 IC 50 and IC 50 .…”

Section: Resultsmentioning

confidence: 99%

α‐Glucosidase Inhibition Action of Major Flavonoids Identified from Hypericum Attenuatum Choisy and Their Synergistic Effects

Jin

Zhang

et al. 2021

Chemistry & Biodiversity

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Hypericum attenuatum Choisy is a traditional Chinese herbal plant with multiple therapeutic effects. In this study, bioactivity‐guided fractionation of Hypericum attenuatum Choisy extracts afforded three major flavonoids (including astragalin, guaijaverin and quercetin), which possessed α‐Glucosidase inhibitory activity with IC50 values of 33.90±0.68 μM, 17.23±0.75 μM and 31.90±0.34 μM, respectively. Circular dichroism analysis revealed that all the three compounds could interact with α‐glucosidase by inducing conformational changes of the enzyme. Molecular docking results indicated that they could bind to the active site in α‐glucosidase, and the binding force was driven mainly by hydrogen bond. Additionally, isobolographic analysis of the interactions between two compounds showed that all the combinations presented a synergistic α‐glucosidase inhibitory effect at lower concentrations, and the combination between quercetin and guaijaverin or astragalin exhibited the best synergistic effect. This research might provide a theoretical basis for the application of Hypericum attenuatum Choisy in treating hyperglycemia.

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Section: Resultsmentioning

confidence: 99%

α‐Glucosidase Inhibition Action of Major Flavonoids Identified from Hypericum Attenuatum Choisy and Their Synergistic Effects

Jin

Zhang

et al. 2021

Chemistry & Biodiversity

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“…The quantitative measurement of difference in the cartesian coordinates of simulated pose and experimental pose (RMSD) serve as gold standard to evaluate the reliability of a docking experiment. 43 For a satisfactory redocking experiment, the RMSD value between the cartesian coordinates of simulated and crystal pose should be less than 3 Å.…”

Section: Methodsmentioning

confidence: 99%

Exploring Novel N-Myristoyltransferase Inhibitors: A Molecular Dynamics Simulation Approach

et al. 2019

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N -Myristoyltransferase (NMT) is a cytosolic monomeric enzyme involved in the allocation of the myristoyl group to the aminoterminal of glycine in several viral and eukaryotic cellular proteins. NMT has been validated as a potential drug target against kinetoplastid for parasitic protozoa. A multistep virtual screening protocol based on the pharmacophore modeling, molecular docking, and molecular dynamics simulation was carried out. Initially, Maybridge database was virtually screened via a validated pharmacophore model. The effective pharmacophore models were accompanied with exclusion volumes to improve their receiver operating characteristic curve to identify potential NMT inhibitors. The hits identified as actives based on the 3D-pharmacophore model were evaluated by molecular docking studies. In stepwise screening, six compounds were shortlisted for the dynamic simulation to get insights into their binding mode. In conclusion, this study provides fundamental information about the architecture of the binding site and some crucial residues that may provide insights into the development of new antiparasitic agents.

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“…All experiments were performed in triplicates, and the inhibitory percentage of α-amylase activity was calculated through the following formula (Shah et al, 2017): After incubation for 10 min at 37°C, 0.5 ml of 0.01 M iodine-potassium iodide solution was added to start the reaction.…”

Section: Effect Of Three Flavonoids On α-Amylase Activitymentioning

confidence: 99%

“…However, it has been reported to cause some gastrointestinal side effects, such as diarrhea, flatulence, and abdominal pain (Shah, Khalil, Ul-Haq, & Panichayupakaranant, 2017;Yang, He, & Lu, 2014). However, it has been reported to cause some gastrointestinal side effects, such as diarrhea, flatulence, and abdominal pain (Shah, Khalil, Ul-Haq, & Panichayupakaranant, 2017;Yang, He, & Lu, 2014).…”

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confidence: 99%

An assessment of the interaction for three Chrysanthemum indicum flavonoids and α‐amylase by surface plasmon resonance

Huang

Yin

et al. 2019

Food Science & Nutrition

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This study evaluated the interaction of Chrysanthemum indicum (CI) flavonoids (luteolin, acacetin, and buddleoside) with α‐amylase. Surface plasmon resonance (SPR) assay showed their equilibrium dissociation constants (KD) are 1.9695 ± 0.12, 2.9240 ± 0.20, and 3.2966 ± 0.08 mM at pH 6.0, respectively. Furthermore, their binding affinities were influenced by KCl, MgCl2, and CaCl2. Enzymatic kinetic studies revealed that three flavonoids exhibited noncompetitive α‐amylase inhibitory activity. The inhibitory sequence is luteolin > acacetin > buddleoside, which was in accordance with the results of binding affinity from SPR. 1,1‐diphenyl‐2‐picryl hydrazyl radical assay demonstrated that antioxidant activities of three flavonoids were inhibited significantly with α‐amylase. Meanwhile, the study reveals that hydroxyl on C′‐4, C′‐5, and C‐7 of flavonoids play an important role on the interaction of three flavonoids with α‐amylase. Also, SPR could be used as sensor for rapid screening inhibitors of α‐amylase and provide useful information for the application of C. indicum flavonoids in food and pharmaceutical area.

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α-Glucosidase inhibitory effect of rhinacanthins-rich extract from Rhinacanthus nasutus leaf and synergistic effect in combination with acarbose

Cited by 47 publications

References 28 publications

α‐Glucosidase Inhibition Action of Major Flavonoids Identified from Hypericum Attenuatum Choisy and Their Synergistic Effects

α‐Glucosidase Inhibition Action of Major Flavonoids Identified from Hypericum Attenuatum Choisy and Their Synergistic Effects

Exploring Novel N-Myristoyltransferase Inhibitors: A Molecular Dynamics Simulation Approach

An assessment of the interaction for three Chrysanthemum indicum flavonoids and α‐amylase by surface plasmon resonance

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