Combination of Catechin, Epicatechin, and Rutin: Optimization of a novel complete antidiabetic formulation using a mixture design approach

Mechchate, Hamza; Es-safi, Imane; Haddad, Hassan; Bekkari, Hicham; Grafov, Andriy; Bousta, Dalila

doi:10.1016/j.jnutbio.2020.108520

Cited by 51 publications

(36 citation statements)

References 31 publications

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“…The flavonoid catechin is known to be a powerful antioxidant and anti-inflammatory molecule that is found in a variety of plants. A combination of catechin, epicatechin and rutin was successfully tested in alloxan-induced diabetic mice as an antidiabetic drug alternative [ 45 ]. Polyphenolic acid chlorogenic acid has been described as having beneficial metabolic effects on glucose homeostasis.…”

Section: Resultsmentioning

confidence: 99%

“…Scopoletin, chlorogenic acid, caffeic acid, quercetin, myricetin, typhaneoside, catechin, gracillin, oleanolic acid and gitogenin (for the last two compounds, only aglycons were commercially available) were applied at concentrations ranging from 10 nM to 10 µM. Similar concentrations have been described in the literature to be relevant for putative antidiabetic properties [ 42 , 43 , 44 , 45 , 48 ]. The results are shown in Figure 6 A–T and suggest that only one of the identified bioactive compounds had an influence on the stimulation of insulin secretion when used as a single compound.…”

Section: Resultsmentioning

confidence: 99%

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A High-Content Screen for the Identification of Plant Extracts with Insulin Secretion-Modulating Activity

et al. 2021

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Bioactive plant compounds and extracts are of special interest for the development of pharmaceuticals. Here, we describe the screening of more than 1100 aqueous plant extracts and synthetic reference compounds for their ability to stimulate or inhibit insulin secretion. To quantify insulin secretion in living MIN6 β cells, an insulin–Gaussia luciferase (Ins-GLuc) biosensor was used. Positive hits included extracts from Quillaja saponaria, Anagallis arvensis, Sapindus mukorossi, Gleditsia sinensis and Albizia julibrissin, which were identified as insulin secretion stimulators, whereas extracts of Acacia catechu, Myrtus communis, Actaea spicata L., Vaccinium vitis-idaea and Calendula officinalis were found to exhibit insulin secretion inhibitory properties. Gas chromatography-mass spectrometry (GC-MS) and liquid chromatography-mass spectrometry (LC-MS) were used to characterize several bioactive compounds in the selected plant extracts, and these bioactives were retested for their insulin-modulating properties. Overall, we identified several plant extracts and some of their bioactive compounds that may be used to manipulate pancreatic insulin secretion.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

A High-Content Screen for the Identification of Plant Extracts with Insulin Secretion-Modulating Activity

et al. 2021

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“…Plants are an inexhaustible source of different classes of biologically active compounds [ 11 ]. Among those are polyphenols, which possess anticancer, antimicrobial, antiviral, anti-inflammatory, and tumor suppression properties and are cytotoxic [ 12 , 13 ].…”

Section: Introductionmentioning

confidence: 99%

“…Rutin (quercetin-3- O -rutinoside) is a glycoside composed of the flavonol quercetin and a disaccharide rutinose found in asparagus, buckwheat, apricots, apples, cherries, tomatoes, grapefruit, plums, bananas, and tea [ 31 ]. It has a wide range of biological activity: antioxidant, anti-inflammatory, antiangiogenic, pro-apoptotic, and antiproliferative [ 11 , 32 ]. Its activity was demonstrated in a variety of cell models: adenocarcinoma, glioblastoma, leukemia, and cancer (breast, prostate, lung, stomach, liver, and colon) [ 33 ].…”

Section: Introductionmentioning

confidence: 99%

Antileukemic Activity and Molecular Docking Study of a Polyphenolic Extract from Coriander Seeds

et al. 2021

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Leukemia is a group of hematological neoplastic disorders linked to high mortality rates worldwide, but increasing resistance has led to the therapeutic failure of conventional chemotherapy. This study aimed to evaluate in vitro the antileukemic activity and potential mechanism of action of a polyphenolic extract obtained from the seeds of Coriandrum sativum L. (CSP). A methylthiazoletetrazolium assay was performed to assess the CSP cytotoxicity on chronic (K562) and acute (HL60) myeloid leukemia cell lines and on normal Vero cell line. CSP toxicity was also evaluated in vivo using the OECD 423 acute toxicity model on Swiss albino mice. The results demonstrated a remarkable antitumoral activity against K562 and HL60 cell lines (IC50 = 16.86 µM and 11.75 µM, respectively) although no cytotoxicity was observed for the Vero cells or mice. A silico study was performed on the following receptors that are highly implicated in the development of leukemia: ABL kinase, ABL1, BCL2, and FLT3. The molecular docking demonstrated a high affinity interaction between the principal CSP components and the receptors. Our findings demonstrated that CSP extract has remarkable antileukemic activity, which is mainly mediated by the flavonoids, catechins, and rutin, all of which showed the highest binding affinity for the targeted receptors. This study revealed a promising active compound alternative research-oriented biopharmacists to explore.

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“…The scientific community developed during the years many chemical and synthetic antidiabetic drugs to help manage the diabetic state and to prevent the complications [4]. Still, the adverse effect of their prolonged administration (such as gastrointestinal disorders, hypoglycemia, obesity) have changed the attention of many people and researchers for new safer alternatives [5]. Many diabetic people have changed their medication into medicinal plants as effective, safe, and present little or almost no side effect [6].…”

Section: Introductionmentioning

confidence: 99%

In-Vivo Antidiabetic Activity and In-Silico Mode of Action of LC/MS-MS Identified Flavonoids in Oleaster Leaves

et al. 2020

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Background: Olea europea L. subsp. europaea var. sylvestris (Mill) Lehr (Oleaster) is a wild endemic olive tree indigenous to the Mediterranean region. Olea europea leaves represent a natural reservoir of bioactive molecules that can be used for therapeutic purposes. Aim of the study: This work was conducted to study antidiabetic and antihyperglycemic activities of flavonoids from oleaster leaves using alloxan-induced diabetic mice. The mode of action of flavonoids against eight receptors that have a high impact on diabetes management and complication was also investigated using molecular docking. Results: During 28 days of mice treatment with doses 25 and 50 mg/kg b.w, the studied flavonoids managed a severe diabetic state (<450 mg/dL), exhibiting a spectacular antidiabetic and antihyperglycemic activity, and improved mice health status compared to diabetic control. The in-silico mode of action of oleaster flavonoids revealed the inhibition of protein tyrosine phosphatase 1B (PTP1B), Dipeptidyl-peptidase 4 (DPP4), α-Amylase (AAM), α-Glucosidase inhibition, Aldose reductase (AldR), Glycogen phosphorylase (GP), and the activation of free fatty acid receptor 1 (FFAR1). Conclusion: The findings obtained in the present work indicate that the flavonoids from the oleaster may constitute a safe multi-target remedy to treat diabetes.

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Combination of Catechin, Epicatechin, and Rutin: Optimization of a novel complete antidiabetic formulation using a mixture design approach

Cited by 51 publications

References 31 publications

A High-Content Screen for the Identification of Plant Extracts with Insulin Secretion-Modulating Activity

A High-Content Screen for the Identification of Plant Extracts with Insulin Secretion-Modulating Activity

Antileukemic Activity and Molecular Docking Study of a Polyphenolic Extract from Coriander Seeds

In-Vivo Antidiabetic Activity and In-Silico Mode of Action of LC/MS-MS Identified Flavonoids in Oleaster Leaves

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