The effects of curcumin, mangiferin, resveratrol and other natural plant products on aminopeptidase B activity

Cadel, Sandrine; Darmon, Cécile; Désert, Alexandre; Mahbouli, Mouna; Piesse, Christophe; Ghélis, Thanos; Lafont, René; Foulon, Thierry

doi:10.1016/j.bbrc.2019.02.143

Cited by 2 publications

(1 citation statement)

References 33 publications

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“…The data were further analysed to understand the inhibition mechanism by using Lineweaver–Burk plot to build the inhibition mode of curcumin against α‐glucosidases. When the inhibition mechanism was competitive inhibition, the increasing inhibition concentrations led to an increase in the K m values, whereas V max values remained mostly unchanged, while the non‐competitive inhibition reduced both K m and V max (Cadel et al ., 2019). A double‐reciprocal graph is shown in Fig.…”

Section: Resultsmentioning

confidence: 99%

Curcumin as a mild natural α‐glucosidase inhibitor: a study on its mechanism in vitro

Liu

Zhu

et al. 2021

Int J of Food Sci Tech

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Curcumin, natural dietary ingredient, is considered as mild effective inhibitors for α-glucosidase to prevent type 2 diabetes. In this work, spectroscopic techniques combined with molecular simulation were used to further understand the inhibition kinetic mechanism of curcumin on α-glucosidase. Curcumin showed a mild inhibition effect (IC 50 =20.54 AE 1.02 mg/ml) for α-glucosidases through a competitive inhibition mechanism, and it led to fluorescence quenching as well as energy transfer by binding behaviour (average binding distance, r 0 = 2.43 nm). Hydrogen bonds and steric hindrance were the main interactions between curcumin and the activity site of α-glucosidases, as revealed by molecular docking. Circular dichroism spectroscopy results also indicate that curcumin affected the denaturation temperature of α-glucosidases, which dropped from 74 °C to 68 °C, resulting in inhibition. The findings can contribute to a better understanding of the development and application of curcumin in functional dietary food.

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Section: Resultsmentioning

confidence: 99%

Curcumin as a mild natural α‐glucosidase inhibitor: a study on its mechanism in vitro

Liu

Zhu

et al. 2021

Int J of Food Sci Tech

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Multi-functional Ligands and Molecular Hybridization: Conceptual Aspects and Application in the Innovative Design of Drug Candidate Prototypes for Neurodegenerative Diseases

de Freitas Silva,

Dias Viegas,

Silva Gontijo

et al. 2023

Frontiers in Clinical Drug Research - CNS and Neurological Disorders

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The rapid increase in the incidence of dementia has enormous socio.economic impacts and costs for governmental health systems all over the world. Despite this, finding an effective treatment for the different types of neurodegenerative diseases (NDs) so far represents a challenge for science. The biggest obstacles related to NDs are their multifactorial complexity and the lack of knowledge of the different pathophysiological pathways involved in the development of each disorder. The latest advances in science, especially those related to the systems biology concepts, have given new insights for a better comprehension of such multifactorial networks related to the onset and progression of NDs, and how Medicinal Chemists could act in the search for novel disease-modifying drug candidates capable of addressing the multiple pathological factors involved in neurodegeneration. The multi-target directed ligands (MTDLs) concept has captivated and opened new windows for the creativity and rationality of researchers worldwide in seeking innovative drug candidates capable of modulating different molecular targets by a single multifunctional molecule. In fact, in the last two decades, thousands of research groups have dedicated their efforts to the use of molecular hybridization as the main tool for the rational design of novel molecular scaffolds capable of expressing multi-target biological activity. In this way, this chapter addresses the most recent pathophysiological hallmarks of the most high-impact NDs, represented by Alzheimer’s, Parkinson’s, Huntington’s diseases, and amyotrophic lateral sclerosis, as well as the state-of-art in the design of new MTDLs, inspired mostly by natural products with improved druggability properties.

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The effects of curcumin, mangiferin, resveratrol and other natural plant products on aminopeptidase B activity

Cited by 2 publications

References 33 publications

Curcumin as a mild natural α‐glucosidase inhibitor: a study on its mechanism in vitro

Curcumin as a mild natural α‐glucosidase inhibitor: a study on its mechanism in vitro

Multi-functional Ligands and Molecular Hybridization: Conceptual Aspects and Application in the Innovative Design of Drug Candidate Prototypes for Neurodegenerative Diseases

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