Recent Progress in Natural Products as DPP-4 Inhibitors

Gao, Yuanyuan; Zhang, Yong; Zhu, Jianming; Li, Bo; Zhao, Li; Zhu, Weiliang; Shi, Jiye; Jia, Qi; Li, Yiming

doi:10.4155/fmc.15.49

Cited by 54 publications

(48 citation statements)

References 32 publications

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“…This information correlates with the obtained free-binding energy where anagliptin has the lowest binding score among other gliptin classes ( Table 3 ). While diprotin-A is a potent DPPIV inhibitor with a Ile-Pro-Ile sequence commonly used as reference compound [ 17 , 64 ].…”

Section: Discussionmentioning

confidence: 99%

“…To date, there are more than 20 types of plant compounds reported to have DPPIV inhibitory properties and that have undergone in vitro validations. This includes compounds such as resveratrol, luteolin, apigenin, flavone, and cyanidin 3,5-diglucoside, which can be found in citrus, grapes, soybeans, and aronia berries [ 15 – 17 ]. Other plants species that have DPPIV inhibitory properties that have been demonstrated through in vitro studies are Urena lobata , Fagonia cretica L., Hedera nepalensis K. Koch, Senna nigricans , Commiphora mukul , Emblica officinalis , Terminalia arjuna , and Smilax china [ 18 – 22 ].…”

Section: Introductionmentioning

confidence: 99%

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Computational Analysis of Gynura bicolor Bioactive Compounds as Dipeptidyl Peptidase-IV Inhibitor

Rozano

Abdullah‐Zawawi

Ahmad

et al. 2017

Advances in Bioinformatics

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The inhibition of dipeptidyl peptidase-IV (DPPIV) is a popular route for the treatment of type-2 diabetes. Commercially available gliptin-based drugs such as sitagliptin, anagliptin, linagliptin, saxagliptin, and alogliptin were specifically developed as DPPIV inhibitors for diabetic patients. The use of Gynura bicolor in treating diabetes had been reported in various in vitro experiments. However, an understanding of the inhibitory actions of G. bicolor bioactive compounds on DPPIV is still lacking and this may provide crucial information for the development of more potent and natural sources of DPPIV inhibitors. Evaluation of G. bicolor bioactive compounds for potent DPPIV inhibitors was computationally conducted using Lead IT and iGEMDOCK software, and the best free-binding energy scores for G. bicolor bioactive compounds were evaluated in comparison with the commercial DPPIV inhibitors, sitagliptin, anagliptin, linagliptin, saxagliptin, and alogliptin. Drug-likeness and absorption, distribution, metabolism, and excretion (ADME) analysis were also performed. Based on molecular docking analysis, four of the identified bioactive compounds in G. bicolor, 3-caffeoylquinic acid, 5-O-caffeoylquinic acid, 3,4-dicaffeoylquinic acid, and trans-5-p-coumaroylquinic acid, resulted in lower free-binding energy scores when compared with two of the commercially available gliptin inhibitors. The results revealed that bioactive compounds in G. bicolor are potential natural inhibitors of DPPIV.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Computational Analysis of Gynura bicolor Bioactive Compounds as Dipeptidyl Peptidase-IV Inhibitor

Rozano

Abdullah‐Zawawi

Ahmad

et al. 2017

Advances in Bioinformatics

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“…Therefore, the discovery of DPP-IV inhibitors with new structures, especially among the secondary metabolites of plants, with higher safety, is a reliable and proven approach for discovering new hypoglycemic drugs [8]. For example, Gao et al conducted a review and reported that 63 kinds of natural flavonoids and alkaloids that inhibit DPP-IV have been found, which proves that natural products are an important source of active drugs [9].…”

Section: Introductionmentioning

confidence: 99%

Identification of Potential Dipeptidyl Peptidase (DPP)-IV Inhibitors among Moringa oleifera Phytochemicals by Virtual Screening, Molecular Docking Analysis, ADME/T-Based Prediction, and In Vitro Analyses

et al. 2020

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Moringa oleifera Lam. (MO) is called the “Miracle Tree” because of its extensive pharmacological activity. In addition to being an important food, it has also been used for a long time in traditional medicine in Asia for the treatment of chronic diseases such as diabetes and obesity. In this study, by constructing a library of MO phytochemical structures and using Discovery Studio software, compounds were subjected to virtual screening and molecular docking experiments related to their inhibition of dipeptidyl peptidase (DPP-IV), an important target for the treatment of type 2 diabetes. After the four-step screening process, involving screening for drug-like compounds, predicting the absorption, distribution, metabolism, excretion, and toxicity (ADME/T) of pharmacokinetic properties, LibDock heatmap matching analysis, and CDOCKER molecular docking analysis, three MO components that were candidate DPP-IV inhibitors were identified and their docking modes were analyzed. In vitro activity verification showed that all three MO components had certain DPP-IV inhibitory activities, of which O-Ethyl-4-[(α-l-rhamnosyloxy)-benzyl] carbamate (compound 1) had the highest activity (half-maximal inhibitory concentration [IC50] = 798 nM). This study provides a reference for exploring the molecular mechanisms underlying the anti-diabetic activity of MO. The obtained DPP-IV inhibitors could be used for structural optimization and in-depth in vivo evaluation.

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“…Diabetes mellitus (DM) is the fastest growing metabolic disease all over the world, identified by approximately 285 million people who have been diagnosed with DM to date, with this number predicted to increase by the year 2030. 1,2 There are some mechanisms of antidiabetic drugs and currently the category of antidiabetic drugs working on the incretin pathway is more desirable. 3 Incretin consists of a Glucose-dependent Insulinotropic Polypeptide (GIP) and Glucagon-Like Peptide-1 (GLP-1).…”

Section: Introductionmentioning

confidence: 99%

The Antidiabetic Effectivity of Indonesian Plants Extracts via DPP-IV Inhibitory Mechanism

Setyaningsih¹,

Saputri²,

Mun’im³

2019

JYP

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Background: Nature provides a rich source of antidiabetic medicines. More than 1.200 plants have been reported to have anti-diabetic activities and more than half of the drugs on the market come from natural products. Therefore, research for developing new antidiabetic drugs from natural sources is necessary to properly evaluate various mechanism of action, efficacy and safety at toxicological, physiological, pharmacological and molecular levels before these drugs applied in treatment of diabetes. This study aims to examine and determine the highest activity of 10 ethanol extracts from Indonesian plants selected for in vitro inhibitory activity of dipeptidyl peptidase-IV (DPP-IV). Materials and Methods: This research studied DPP-IV inhibitory mechanism from 10 plant extract, namely Caesalpinia sappan, Cinchona officinalis, Elephantopus scaber, Foeniculum vulgare, Morus nigra, Muntingia calabura, Phyllanthus niruri, Psidium guajava, Rheum palmatum and Vernonia amygdalina using the spectrophotometric method and Sitagliptin as a positive control. The effectiveness of inhibition was assessed by percent inhibition. Tannin removal test was performed to exclude false-positive results. Results: The ethanolic extract of Caesalpinia sappan exhibited DPP-IV inhibitory activity greater than 80%, which was not markedly different from that of Sitagliptin at 85%. Brazilin, an active compound from Caesalpinia sappan gave the inhibition at greater than 78%. Tannin removal test for Caesalpinia sappan gave the inhibition at 74.16%. The High Performance Liquid Chromatography (HPLC) analysis result displayed that brazilin content on Caesalpinia sappan extract was 91.94%. Conclusion: Based on these results, Caesalpinia sappan ethanol extract has a potential effect as a better antidiabetic agent than other extracts used in this study.

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Recent Progress in Natural Products as DPP-4 Inhibitors

Cited by 54 publications

References 32 publications

Computational Analysis of Gynura bicolor Bioactive Compounds as Dipeptidyl Peptidase-IV Inhibitor

Computational Analysis of Gynura bicolor Bioactive Compounds as Dipeptidyl Peptidase-IV Inhibitor

Identification of Potential Dipeptidyl Peptidase (DPP)-IV Inhibitors among Moringa oleifera Phytochemicals by Virtual Screening, Molecular Docking Analysis, ADME/T-Based Prediction, and In Vitro Analyses

The Antidiabetic Effectivity of Indonesian Plants Extracts via DPP-IV Inhibitory Mechanism

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