Diabetes mellitus is a multifactorial global health disorder that is rising at an alarming rate. Cardiovascular diseases, kidney damage and neuropathy are the main cause of high mortality rates among individuals with diabetes. One effective therapeutic approach for controlling hyperglycemia associated with type-2 diabetes is to target alpha-amylase and alpha-glucosidase, enzymes that catalyzes starch hydrolysis in the intestine. At present, approved inhibitors for these enzymes are restricted to acarbose, miglitol and voglibose. Although these inhibitors retard glucose absorption, undesirable gastrointestinal side effects impede their application. Therefore, research efforts continue to seek novel inhibitors with improved efficacy and minimal side effects. Natural products of plant origin have been a valuable source of therapeutic agents with lesser toxicity and side effects. The anti-diabetic potential through alpha-glucosidase inhibition of plant-derived molecules are summarized in this review. Eight molecules (Taxumariene F, Akebonoic acid, Morusin, Rhaponticin, Procyanidin A2, Alaternin, Mulberrofuran K and Psoralidin) were selected as promising drug candidates and their pharmacokinetic properties and toxicity were discussed where available.

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A review of alpha-glucosidase inhibitors from plants as potential candidates for the treatment of type-2 diabetes.

Polygonum multiflorum Thunb. and its processed products have been used in China for centuries due to their multiple beneficial effects to human body. Currently, liver injuries caused by taking P. multiflorum have been reported worldwide, but the potential toxic components and possible mechanism that caused hepatotoxicity remain unclear. It is worth noting that the processing procedure could significantly decrease the toxicity of raw P. multiflorum and the processed products of P. multiflorum are considered to be relatively safe. However, the processing mechanism is still ambiguous, and there is the lack of a scientific approach to control the quality of P. multiflorum praeparata. This study is the first review that summarizes the recently advances (from 2007 to 2017) in the chemical analysis of P. multiflorum, and provides comprehensive information on the quantitative and qualitative analysis of P. multiflorum as well as its related species. In addition, the processing mechanism and quality evaluation of processed P. multiflorum are discussed. Moreover, the toxicity of P. multiflorum is analyzed from the perspectives of exploration of the proposed toxic ingredients, metabolite identification, metabolomics studies, and exogenous contaminant determination. Furthermore, trends and perspectives for future research of this medicine are discussed.

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Polygonum multiflorum Thunb.: A Review on Chemical Analysis, Processing Mechanism, Quality Evaluation, and Hepatotoxicity.

Apigenin ameliorates streptozotocin induced diabetic nephropathy in rats

Acute toxicity screening of different extractions, components and constituents of Polygonum multiflorum Thunb. on zebrafish (Danio rerio) embryos in vivo.

Popular functional foods and herbs for the management of type-2-diabetes mellitus: A comprehensive review with special reference to clinical trials and its proposed mechanism

a-Glucosidase inhibitors extracted from the roots of Polygonum multiflorum Thunb

Diabetes is a complex metabolic disease characterized by hyperglycemia, plaguing the whole world. However, the action mode of multi-component and multi-target for traditional Chinese medicine (TCM) could be a promising treatment of diabetes mellitus. According to the previous research, the TCM of Polygonum multiflorum (PM) showed noteworthy hypoglycemic effect. Up to now, its hypoglycemic active ingredients and mechanism of action are not yet clear. In this study, network pharmacology was employed to elucidate the potential bioactive compounds and hypoglycemic mechanism of PM. First, the compounds with good pharmacokinetic properties were screened from the self-established library of PM, and the targets of these compounds were predicted and collected through database. Relevant targets of diabetes were summarized by searching database. The intersection targets of compound-targets and disease-targets were obtained soon. Secondly, the interaction net between the compounds and the filtered targets was established. These key targets were enriched and analyzed by protein–protein interactions (PPI) analysis, molecular docking verification. Thirdly, the key genes were used to find the biologic pathway and explain the therapeutic mechanism by genome ontology (GO) and kyoto encyclopedia of genes and genomes (KEGG) analysis. Lastly, the part of potential bioactive compounds were under enzyme activity inhibition tests. In this study, 29 hypoglycemic components and 63 hypoglycemic targets of PM were filtrated based on online network database. Then the component-target interaction network was constructed and five key components resveratrol, apigenin, kaempferol, quercetin and luteolin were further obtained. Sequential studies turned out, AKT1, EGFR, ESR1, PTGS2, MMP9, MAPK14, and KDR were the common key targets. Docking studies indicated that the bioactive compounds could stably bind the pockets of target proteins. There were 38 metabolic pathways, including regulation of lipolysis in adipocytes, prolactin signaling pathway, TNF signaling pathway, VEGF signaling pathway, FoxO signaling pathway, estrogen signaling pathway, linoleic acid metabolism, Rap1 signaling pathway, arachidonic acid metabolism, and osteoclast differentiation closely connected with the hypoglycemic mechanism of PM. And the enzyme activity inhibition tests showed the bioactive ingredients have great hypoglycemic activity. In summary, the study used systems pharmacology to elucidate the main hypoglycemic components and mechanism of PM. The work provided a scientific basis for the further hypoglycemic effect research of PM and its monomer components, but also provided a reference for the secondary development of PM.

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Systemic elucidation on the potential bioactive compounds and hypoglycemic mechanism of Polygonum multiflorum based on network pharmacology

The invention discloses hypericum L and the extraction and the preparation method of the extraction; the drug combination containing hypericum L and/or the extraction of the hypericum L; the usage of hypericum L and/or the extraction of the hypericum L used as drugs and health care product, in particular to the usage used for preparing drugs and health care products treating and preventing metabolic disorders relative to insulin resistance, diabetes and complicating disease and other diseases

Hypericum extract, its making method and medicinal composition and use for treating diabetes

The invention discloses long-chain fatty acid compounds which are extracted, separated and obtained from plants (comprising coriander and Balanophora plants) and shown as a formula (1). The long-chain fatty acid compounds have a preparation method that a medicine combination containing the long-chain fatty acid compounds is proved that the medicine combination has trypsin sensitizing effect on a whole living mode of exosomatic PTP1b inhibitory activity and insulin resistance through the pharmacological activity screening, thereby explaining that the long-chain fatty acid compounds can be used as insulin sensitizing agent and used for preparing medicines and health products, and more particularly used for preparing the medicines and the health products for treating and preventing correlative metabolic diseases such as the insulin resistance, diabetes mellitus and complications thereof.

Fei Ye

Papers

a-Glucosidase inhibitors extracted from the roots of Polygonum multiflorum Thunb

Systemic elucidation on the potential bioactive compounds and hypoglycemic mechanism of Polygonum multiflorum based on network pharmacology

Hypericum extract, its making method and medicinal composition and use for treating diabetes

Petroselinic acid compounds