Current and future approaches for in vitro hit discovery in diabetes mellitus

Zhang, Xin; Kupczyk, Erwin; Schmitt‐Kopplin, Philippe; Mueller, Constanze

doi:10.1016/j.drudis.2022.07.016

Cited by 5 publications

(1 citation statement)

References 94 publications

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“…As a negative regulator of insulin receptor signaling, PTP1B inhibition may lead to improved insulin sensitivity and/or increased glucose uptake ( Elchebly et al, 1999 ; Klaman et al, 2000 ; Nandi and Saxena, 2020 ). A recently published review provides a comprehensive overview of additional molecular targets and in-vitro methods ( Zhang et al, 2022 ). However, greater emphasis should be placed on validating in-vitro results in-vivo .…”

Section: Summary and Perspectivesmentioning

confidence: 99%

A comprehensive in-vitro/in-vivo screening toolbox for the elucidation of glucose homeostasis modulating properties of plant extracts (from roots) and its bioactives

Bauer,

Rimbach,

Cordeiro

et al. 2024

Front. Pharmacol.

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Plant extracts are increasingly recognized for their potential in modulating (postprandial) blood glucose levels. In this context, root extracts are of particular interest due to their high concentrations and often unique spectrum of plant bioactives. To identify new plant species with potential glucose-lowering activity, simple and robust methodologies are often required. For this narrative review, literature was sourced from scientific databases (primarily PubMed) in the period from June 2022 to January 2024. The regulatory targets of glucose homeostasis that could be modulated by bioactive plant compounds were used as search terms, either alone or in combination with the keyword “root extract”. As a result, we present a comprehensive methodological toolbox for studying the glucose homeostasis modulating properties of plant extracts and its constituents. The described assays encompass in-vitro investigations involving enzyme inhibition (α-amylase, α-glucosidase, dipeptidyl peptidase 4), assessment of sodium-dependent glucose transporter 1 activity, and evaluation of glucose transporter 4 translocation. Furthermore, we describe a patch-clamp technique to assess the impact of extracts on KATP channels. While validating in-vitro findings in living organisms is imperative, we introduce two screenable in-vivo models (the hen’s egg test and Drosophila melanogaster). Given that evaluation of the bioactivity of plant extracts in rodents and humans represents the current gold standard, we include approaches addressing this aspect. In summary, this review offers a systematic guide for screening plant extracts regarding their influence on key regulatory elements of glucose homeostasis, culminating in the assessment of their potential efficacy in-vivo. Moreover, application of the presented toolbox might contribute to further close the knowledge gap on the precise mechanisms of action of plant-derived compounds.

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Section: Summary and Perspectivesmentioning

confidence: 99%

A comprehensive in-vitro/in-vivo screening toolbox for the elucidation of glucose homeostasis modulating properties of plant extracts (from roots) and its bioactives

Bauer,

Rimbach,

Cordeiro

et al. 2024

Front. Pharmacol.

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Changes in toxicity after mixing imidacloprid and cadmium: enhanced, diminished, or both? From a perspective of oxidative stress, lipid metabolism, and amino acid metabolism in mice

Wang,

Agarry

et al. 2023

Environ Sci Pollut Res

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Characteristics and Biological Properties of Imeglimin Hydrochlo ride, A Novel Antidiabetic Agent: A Systematic Review

Sultan,

Agarwal,

Sharma

2024

CDR

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Background: WHO indicates that diabetes will become the 7th leading reason for death by 2030. The physiopathology of dysfunctioning is associated with obesity, weight gain and predominantly insulin resistance in insulin-sensitive cells and continuous deterioration of pancreatic beta cell function. Imeglimin is an investigational novel oral anti-diabetic drug. Objectives: The motive of the review is to comprehensively explore the chemistry, biological and analytical analysis of the Imeglimin hydrochloride Methods: To enhance the understanding, a systematic review was conducted by forming a database of relevant existing studies from electronic resources like Web of Science, ScienceDirect and PubMed. The methodology is reflected in the PRISMA design. Result: The drug was approved in the year 2021 for therapeutic purposes in Japan. It is the novel and first approved drug for this type of Anti-diabetic treatment. It is a small molecular drug whose molecular weight is 191.6 grams per mole utilized for oral administration. Imeglimin is thought to have both activities, as the amount of glucose is dependent on insulin secretory impact and insulin sensitivity is increased. Conclusion: Therapeutic, pharmacological, and analytical considerations for the novel drug Imeglimin hydrochloride are discussed in this review.

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Current and future approaches for in vitro hit discovery in diabetes mellitus

Cited by 5 publications

References 94 publications

A comprehensive in-vitro/in-vivo screening toolbox for the elucidation of glucose homeostasis modulating properties of plant extracts (from roots) and its bioactives

A comprehensive in-vitro/in-vivo screening toolbox for the elucidation of glucose homeostasis modulating properties of plant extracts (from roots) and its bioactives

Changes in toxicity after mixing imidacloprid and cadmium: enhanced, diminished, or both? From a perspective of oxidative stress, lipid metabolism, and amino acid metabolism in mice

Characteristics and Biological Properties of Imeglimin Hydrochlo ride, A Novel Antidiabetic Agent: A Systematic Review

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