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Special Issue "Discovery and Development of Antidiabetic Agents from Natural Products"

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (30 September 2019).

Special Issue Editor

Prof. Dr. Guglielmina Froldi
E-Mail Website
Guest Editor
Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Italy
Interests: hyperglycemia; aging; pharmacological studies; advanced glycation end products (AGEs); free-radical scavenging, cell proliferation, natural compounds; medicinal plants; new drugs

Special Issue Information

Dear Colleagues,

Type 2 diabetes mellitus (T2DM) is a multifactorial chronic disease, characterized by a prolonged increase in blood glucose levels, which causes macrovascular and microvascular complications. T2DM is characterized by beta-cell dysfunction, insulin resistance, and chronic inflammation, which also cause accelerated age-related damage. To explain how hyperglycemia can induce diabetic complications, a key mechanism is the accumulation of non-enzymatic glycosylation (or glycation) products of proteins and lipids, with the formation of advanced glycation end products (AGEs). These are triggered by endogenous processes related to hyperglycemia and oxidative stress. In relation to these observations, the recognition of natural products, isolated compounds, or new synthetic compounds capable to reduce glycaemia and AGEs formation represents a great challenge in medicine. 

Prof. Dr. Guglielmina Froldi
Guest Editor

Manuscript Submission Information

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Keywords

  • Hypoglycemic agents
  • Medicinal plants
  • Plant biologically active compounds
  • Dietary phytochemicals
  • Advanced glycation end products (AGEs)
  • Free radical scavengers
  • Cell proliferation

Published Papers (4 papers)

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Research

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Open AccessArticle
Formulation of a Mixture of Plant Extracts for Attenuating Postprandial Glycemia and Diet-Induced Disorders in Rats
Molecules 2019, 24(20), 3669; https://doi.org/10.3390/molecules24203669 - 11 Oct 2019
Abstract
The aim of this study was to design a mixture consisting of plant-derived preparations containing inhibitors of carbohydrate digestion and/or glucose absorption that could lower postprandial glycemia and attenuate dietary-induced disorders. The following standardized preparations were tested: white mulberry leaf extract, green coffee [...] Read more.
The aim of this study was to design a mixture consisting of plant-derived preparations containing inhibitors of carbohydrate digestion and/or glucose absorption that could lower postprandial glycemia and attenuate dietary-induced disorders. The following standardized preparations were tested: white mulberry leaf extract, green coffee bean extract, white kidney bean extract, pomelo fruit extract, bitter melon fruit extract, and purified l-arabinose. The study design was composed of oral sucrose and starch tolerance tests in Wistar rats preceded by a single ingestion of the preparations or their mixtures. Then, a 20 week-long experiment was conducted on rats that were fed a high-fat diet and supplemented with the most effective mixture. Based on the results of the oral sucrose and starch tolerance tests, the mulberry leaf extract, l-arabinose, kidney bean extract, and coffee bean extract were selected for composing three mixtures. The most effective inhibition of postprandial glycemia in the oral tolerance tests was observed after the ingestion of a mixture of mulberry leaf, kidney bean, and coffee bean extract. The glucose-lowering effect of the mixture and its effective dosage was confirmed in the feeding experiment. Full article
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Open AccessArticle
Optimization of Hyperglycemic Induction in Zebrafish and Evaluation of Its Blood Glucose Level and Metabolite Fingerprint Treated with Psychotria malayana Jack Leaf Extract
Molecules 2019, 24(8), 1506; https://doi.org/10.3390/molecules24081506 - 17 Apr 2019
Abstract
A standard protocol to develop type 1 diabetes in zebrafish is still uncertain due to unpredictable factors. In this study, an optimized protocol was developed and used to evaluate the anti-diabetic activity of Psychotria malayana leaf. The aims of this study were to [...] Read more.
A standard protocol to develop type 1 diabetes in zebrafish is still uncertain due to unpredictable factors. In this study, an optimized protocol was developed and used to evaluate the anti-diabetic activity of Psychotria malayana leaf. The aims of this study were to develop a type 1 diabetic adult zebrafish model and to evaluate the anti-diabetic activity of the plant extract on the developed model. The ability of streptozotocin and alloxan at a different dose to elevate the blood glucose levels in zebrafish was evaluated. While the anti-diabetic activity of P. malayana aqueous extract was evaluated through analysis of blood glucose and LC-MS analysis fingerprinting. The results indicated that a single intraperitoneal injection of 300 mg/kg alloxan was the optimal dose to elevate the fasting blood glucose in zebrafish. Furthermore, the plant extract at 1, 2, and 3 g/kg significantly reduced blood glucose levels in the diabetic zebrafish. In addition, LC-MS-based fingerprinting indicated that 3 g/kg plant extract more effective than other doses. Phytosterols, sugar alcohols, sugar acid, free fatty acids, cyclitols, phenolics, and alkaloid were detected in the extract using GC-MS. In conclusion, P. malayana leaf aqueous extract showed anti-diabetic activity on the developed type 1 diabetic zebrafish model. Full article
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Open AccessFeature PaperReview
Catalpol in Diabetes and its Complications: A Review of Pharmacology, Pharmacokinetics, and Safety
Molecules 2019, 24(18), 3302; https://doi.org/10.3390/molecules24183302 - 11 Sep 2019
Abstract
This review aimed to provide a general view of catalpol in protection against diabetes and diabetic complications, as well as its pharmacokinetics and safety concerns. The following databases were consulted with the retrieval of more than 100 publications through June 2019: PubMed, Chinese [...] Read more.
This review aimed to provide a general view of catalpol in protection against diabetes and diabetic complications, as well as its pharmacokinetics and safety concerns. The following databases were consulted with the retrieval of more than 100 publications through June 2019: PubMed, Chinese National Knowledge Infrastructure, WanFang Data, and web of science. Catalpol exerts an anti-diabetic effect in different animal models with an oral dosage ranging from 2.5 to 200 mg/kg in rats and 10 to 200 mg/kg in mice. Besides, catalpol may prevent the development of diabetic complications in kidney, heart, central nervous system, and bone. The underlying mechanism may be associated with an inhibition of inflammation, oxidative stress, and apoptosis through modulation of various cellular signaling, such as AMPK/PI3K/Akt, PPAR/ACC, JNK/NF-κB, and AGE/RAGE/NOX4 signaling pathways, as well as PKCγ and Cav-1 expression. The pharmacokinetic profile reveals that catalpol could pass the blood-brain barrier and has a potential to be orally administrated. Taken together, catalpol is a well-tolerated natural compound with promising pharmacological actions in protection against diabetes and diabetic complications via multi-targets, offering a novel scaffold for the development of anti-diabetic drug candidate. Further prospective and well-designed clinical trials will shed light on the potential of clinical usage of catalpol. Full article
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Open AccessReview
Anti-Diabetic Effects and Mechanisms of Dietary Polysaccharides
Molecules 2019, 24(14), 2556; https://doi.org/10.3390/molecules24142556 - 13 Jul 2019
Abstract
Diabetes mellitus is a multifactorial, heterogeneous metabolic disorder, causing various health complications and economic issues, which apparently impacts the human’s life. Currently, commercial diabetic drugs are clinically managed for diabetic treatment that has definite side effects. Dietary polysaccharides mainly derive from natural sources, [...] Read more.
Diabetes mellitus is a multifactorial, heterogeneous metabolic disorder, causing various health complications and economic issues, which apparently impacts the human’s life. Currently, commercial diabetic drugs are clinically managed for diabetic treatment that has definite side effects. Dietary polysaccharides mainly derive from natural sources, including medicinal plants, grains, fruits, vegetables, edible mushroom, and medicinal foods, and possess anti-diabetic potential. Hence, this review summarizes the effects of dietary polysaccharides on diabetes and underlying molecular mechanisms related to inflammatory factors, oxidative stress, and diabetes in various animal models. The analysis of literature and appropriate data on anti-diabetic polysaccharide from electronic databases was conducted. In vivo and in vitro trials have revealed that treatment of these polysaccharides has hypoglycemic, hypolipidemic, antioxidant, and anti-inflammatory effects, which enhance pancreatic β-cell mass and alleviates β-cell dysfunction. It enhances insulin signaling pathways through insulin receptors and activates the PI3K/Akt pathway, and eventually modulates ERK/JNK/MAPK pathway. In conclusion, dietary polysaccharides can effectively ameliorate hyperglycemia, hyperlipidemia, low-grade inflammation, and oxidative stress in type 2 diabetes mellitus (T2DM), and, thus, consumption of polysaccharides can be a valuable choice for diabetic control. Full article
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