The dipeptidyl peptidase-4 inhibitory effect of flavonoids is hindered in protein rich environments

Proença, Carina; Freitas, Marisa; Ribeiro, Daniela; Tomé, Sara M.; Araújo, Alberto N.; Silva, Artur M. S.; Fernandes, Pedro Alexandrino; Fernandes, Eduarda

doi:10.1039/c9fo00722a

Cited by 22 publications

(23 citation statements)

References 73 publications

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“…The inhibitory activities of the compounds isolated against α-amylase and α-glucosidase were investigated in comparison with acarbose. The inhibitory activities observed in this study are consistent with recent reports on the inhibitory activities of polyphenolic compounds against α-amylase and α-glucosidase [5,17,21,23,24]. Although all the fractions showed mild inhibition against these enzymes, only PP4 and PP6 showed better activities which was evident by their IC 50 values.…”

Section: Discussionsupporting

confidence: 92%

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In Vitro Antidiabetic Activity Affecting Glucose Uptake in HepG2 Cells Following Their Exposure to Extracts of Lauridia tetragona (L.f.) R.H. Archer

Odeyemi

Dewar

2019

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The incidence of diabetes is on the rise and one of the medically active plants used for the treatment of diabetes in South Africa is Lauridia tetragona. The aim of this study is to investigate the antidiabetic property of the polyphenolics (PP) compounds isolated from the methanolic extract of Lauridia tetragona. The α-amylase, α-glucosidase, dipeptidyl peptidase IV (DPPIV), lipase inhibitory activities, and glucose uptake in HepG2 were investigated. The methanolic extract fractions of L. tetragona yielded six fractions (PP1-PP6) all of which showed weak inhibition against DPPIV and lipase compared to the standards. However, PP4 and PP6 showed the best inhibition against α-amylase (IC 50 of 359.3 ± 2.11 and 416.82 ± 2.58 µg/mL, respectively) and α-glucosidase (IC 50 of 95.93 ± 2.34 and 104.49 ± 2.21 µg/mL, respectively) and only PP4 (173.6%) resulted in enhanced glucose uptake in HepG2 cells compared to berberine (129.89%) and metformin (187.16%) used as positive controls. The previous investigation on PP4 and PP6 showed the presence of polyphenolics such as ferulic acid, coumaric acid, and caffeic acid. The results of this study suggest that L. tetragona could be suitable as an antidiabetic agent and justifies the folkloric use of the plant to treat diabetes.

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Section: Discussionsupporting

confidence: 92%

“…The inhibitory effect against DPPIV activity was based on a previously described method [17]. Briefly, about 30 µg/mL of each fraction was incubated with 0.1 mg/mL of DPPIV enzyme (D3446, Sigma Aldrich, South Africa) at 37 • C for 30 min in an incubator containing 5% CO 2 .…”

Section: Dipeptidyl Peptidase-ivmentioning

confidence: 99%

In Vitro Antidiabetic Activity Affecting Glucose Uptake in HepG2 Cells Following Their Exposure to Extracts of Lauridia tetragona (L.f.) R.H. Archer

Odeyemi

Dewar

2019

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“…Although recognized for their antioxidant activity, flavonoids have several other activities, including anti‐inflammatory, 69 vasorelaxant, 70 anticoagulant, 71 cardioprotective, 72 antidiabetic, 73–76 chemoprotective, 77 neuroprotective, 78 and antidepressant properties 79 . Furthermore, available data suggest that flavonoids from dietary and herbal plants possess potentially beneficial effects on the prevention and treatment of obesity, and its relation to metabolic disorders 80,81 .…”

Section: Flavonoid Structure and Antiobesity Mechanisms Of Flavonoidsmentioning

confidence: 99%

Flavonoids as antiobesity agents: A review

Rufino

Costa

Carvalho

et al. 2020

Medicinal Research Reviews

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117

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Obesity is a global health problem that affects all age groups in both developing and developed countries. In recent years, the prevalence of overweight and obesity has reached pandemic levels, resulting in a dramatic increase in the incidence of various comorbidities, such as cardiovascular diseases, type 2 diabetes, and cancer, consequently leading to massive health and socioeconomic burdens. Together with lifestyle changes, antiobesity pharmacotherapy is gaining momentum as an adjunctive treatment. However, the available pharmacological approaches have limited use owing to either significant adverse effects or low efficacy. Over the years, natural products have been an important source of lead compounds for drug discovery. Among these, flavonoids are associated with important biological effects and health‐promoting activities. In this review, we discuss the modulatory effects of flavonoids on obesity and their potential mechanisms of action. The literature strongly suggests that most common flavonoids demonstrate a pronounced effect on obesity as shown by their ability to lower body weight, fat mass, and plasma triglycerides/cholesterol, both in in vitro and in vivo models. The impact of flavonoids on obesity can be observed through different mechanisms: reducing food intake and fat absorption, increasing energy expenditure, modulating lipid metabolism, or regulating gut microbiota profile. A better understanding of the known antiobesity mechanisms of flavonoids will enable their potential use to treat this medical condition. Therefore, this review focuses on the putative biological mechanisms through which flavonoids may prevent or treat obesity and highlights new perspectives on future pharmacological use.

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“…DPP‐4 inhibitors have been the most recently developed agents for the treatment of T2DM. [ 5 ] Up to now, 11 DPP‐4 inhibitors have been marketed around the world, and some typical gliptins are shown in Figure 1.…”

Section: Background and Originality Contentmentioning

confidence: 99%

“…[ 7 ] These two incretins stimulate secretory of insulin in response to food ingestion by recognizing G protein‐coupled receptors on pancreatic β cells. [ 5 ] GLP‐1 could also decrease islet glucagon secretion, slow gastric emptying and increase satiety. [ 6,8 ] However, endogenous GLP‐1 has a short half‐time of 1—2 min due to being recognized and degraded by DPP‐4 enzymes.…”

Section: Background and Originality Contentmentioning

confidence: 99%

Design, Synthesis and SAR Studies of Novel and Potent Dipeptidyl Peptidase 4 Inhibitors

Luo

Fang

et al. 2020

Chin. J. Chem.

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Dipeptidyl peptidase 4 (DPP-4) is a clinically validated target for the treatment of type 2 diabetes mellitus (T2DM). To discover novel and potent DPP-4 inhibitors, three series of compounds were designed and synthesized in this study based on our previously identified novel scaffold of 2-phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine. Among the designed compounds, 41d-1 was the most potent one with an IC 50 value of 16.00 nM. Besides, 41d-1 (5 mg/kg) displayed a moderate glucose tolerance capability in ICR mice. Structure-activity-relationship (SAR) studies were discussed in detail, which is constructive for our further optimization.

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The dipeptidyl peptidase-4 inhibitory effect of flavonoids is hindered in protein rich environments

Abstract: The DPP-4 inhibition by flavonoids is hindered in human blood and plasma.

Cited by 22 publications

References 73 publications

In Vitro Antidiabetic Activity Affecting Glucose Uptake in HepG2 Cells Following Their Exposure to Extracts of Lauridia tetragona (L.f.) R.H. Archer

In Vitro Antidiabetic Activity Affecting Glucose Uptake in HepG2 Cells Following Their Exposure to Extracts of Lauridia tetragona (L.f.) R.H. Archer

Flavonoids as antiobesity agents: A review

Design, Synthesis and SAR Studies of Novel and Potent Dipeptidyl Peptidase 4 Inhibitors

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