scholarly journals Chemical Composition, Antioxidant, and α-Glucosidase-Inhibiting Activity of Aqueous and Hydroethanolic Extracts of Traditional Antidiabetics from Croatian Ethnomedicine

Horticulturae ◽  
2021 ◽  
Vol 7 (2) ◽  
pp. 15
Author(s):  
Kristina Bljajić ◽  
Andrea Brajković ◽  
Ana Čačić ◽  
Lovorka Vujić ◽  
Jasna Jablan ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Inhibiting Activity ◽  
Bioactive Constituents ◽  
Artemisia Absinthium ◽  
Glucosidase Inhibitors ◽  
Phenolic Constituents ◽  
Phenolic Substances ◽  
Extraction Solvents ◽  
Centaurium Erythraea

Type 2 diabetes (T2D) is a chronic disease with a growing prevalence worldwide. In addition to the conventional therapy, many T2D patients use phytotherapeutic preparations. In the present study, chemical composition, antioxidant, and α-glucosidase inhibiting activity of traditional antidiabetics from Croatian ethnomedicine (Achillea millefolium, Artemisia absinthium, Centaurium erythraea, Morusalba, Phaseolus vulgaris, Sambucus nigra, and Salvia officinalis) were assessed. The efficacy of water and 80% ethanol as extraction solvents for bioactive constituents was compared. HPLC analysis revealed that the prepared extracts were rich in phenols, especially rutin, ferulic, and chlorogenic acid. Antiradical (against DPPH and ABTS radicals), reducing (towards Mo6+ and Fe3+ ions), and enzyme inhibiting properties were in linear correlation with the content of phenolic constituents. Ethanolic extracts, richer in phenolic substances, showed dominant efficacy in those assays. Aqueous extracts, on the other hand, were better Fe2+ ion chelators and more active in the β-carotene linoleic acid assay. Extracts from S. officinalis and A. millefolium were particularly active antioxidants and α-glucosidase inhibitors. A. absinthium, another potent α-glucosidase inhibitor, contained chromium, a mineral that promotes insulin action. The investigated plants contained significant amounts of minerals useful in management of T2D, with negligible amounts of heavy metals deeming them safe for human use.

Recent Developments in Alpha-Glucosidase Inhibitors for Management of Type-2 Diabetes: An Update

2019 ◽  
Vol 25 (23) ◽  
pp. 2510-2525 ◽  
Author(s):  
Bashir Usman ◽  
Neha Sharma ◽  
Saurabh Satija ◽  
Meenu Mehta ◽  
Manish Vyas ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Patient Compliance ◽  
Postprandial Hyperglycemia ◽  
Diabetic Patients ◽  
Poor Patient ◽  
Glucosidase Inhibitors ◽  
Poor Patient Compliance ◽  
Recent Developments ◽  
Alpha Glucosidase

The incidence of diabetes has increased globally in recent years and figures of diabetic patients were estimated to rise up to 642 million by 2040. The disorder is accompanied with various complications if not managed at the early stages, and interlinked high mortality rate and morbidity with time. Different classes of drugs are available for the management of type 2 diabetes but were having certain limitations of their safety. Alphaglucosidase is a family of enzyme originated from the pancreas which plays a role in the anabolism of 80-90% of carbohydrate consumed into glucose. This glucose is absorbed into the blood and results in frank postprandial hyperglycemia and worsens the conditions of diabetic patients which precipitate complications. Inhibition of these enzymes helps to prevent postprandial hyperglycemia and the formation of glycated end products. Alphaglucosidase inhibitors are reported to be more important in adequate control of type 2, but marketed drugs have various side effects, such as poor patient compliance and also expensive. This proves the needs for other class of drugs with better efficacy, safety, patient compliance and economic. In this review, we have emphasized the recent advances in the field of new alpha-glucosidase inhibitors with improved safety and pharmacological profile.

Novel coumarin containing dithiocarbamate derivatives as potent α-glucosidase inhibitors for management of type 2 diabetes

2020 ◽  
Vol 16 ◽  
Author(s):  
Marjan Mollazadeh ◽  
Maryam Mohammadi-Khanaposhtani ◽  
Yousef Valizadeh ◽  
Afsaneh Zonouzi ◽  
Mohammad Ali Faramarzi ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Kinetic Study ◽  
Active Site ◽  
Docking Study ◽  
Secondary Amines ◽  
Molecular Docking Study ◽  
Glucosidase Inhibitors ◽  
Dithiocarbamate Derivatives

Background: α-Glucosidase is a hydrolyze enzyme that plays a crucial role in degradation of carbohydrates and starch to glucose. Hence, α-glucosidase is an important target in the carbohydrate mediated diseases such as diabetes mellitus. Objective: In this study, novel coumarin containing dithiocarbamate derivatives 4a-n were synthesized and evaluated against α-glucosidase in vitro and in silico. Methods: These compounds were obtained of reaction between 4-(bromomethyl)-7-methoxy-2H-chromen-2-one 1, carbon disulfide 2, and primary or secondary amines 3a-n in the presence potassium hydroxide and ethanol at room temperature. In vitro α-glucosidase inhibition and kinetic study of these compounds were performed. Furthermore, docking study of the most potent compounds was also performed by Auto Dock Tools (version 1.5.6). Results: Obtained results showed that all the synthesized compounds exhibited prominent inhibitory activities (IC50 = 85.0 ± 4.0-566.6 ± 8.6 μM) in comparison to acarbose as standard inhibitor (IC50 = 750.0 ± 9.0 µM). Among them, secondary amine derivative 4d with pendant indole group was the most potent inhibitor. Enzyme kinetic study of the compound 4d revealed that this compound compete with substrate to connect to the active site of α-glucosidase and therefore is a competitive inhibitor. Also, molecular docking study predicted that this compound as well interacted with α-glucosidase active site pocket. Conclusion: Our results suggest that the coumarin-dithiocarbamate scaffold can be a promising lead structure for design potent α-glucosidase inhibitors for treatment of type 2 diabetes.

scholarly journals Phytochemical and Psychotropic Research of Motherwort (Leonurus cardiaca L.) Modified Dry Extracts

Plants ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 230
Author(s):  
Oleh Koshovyi ◽  
Ain Raal ◽  
Igor Kireyev ◽  
Nadiya Tryshchuk ◽  
Tetiana Ilina ◽  
...  
Keyword(s):  
Amino Acids ◽  
Chemical Composition ◽  
Phenolic Compounds ◽  
Pharmacological Activity ◽  
Ellagic Acid ◽  
Hydroxycinnamic Acids ◽  
Psychotropic Activity ◽  
Phytochemical Analysis ◽  
Phenolic Substances ◽  
Leonurus Cardiaca

The prospect of creating a new medicine with psychotropic activity is shown as a result of studying the chemical composition and pharmacological activity of modified dry extracts of motherwort (Leonurus cardiaca L.) tincture. The most promising substances were the dry extracts, modified by adding small amounts of arginine, valine, phenylalanine, glycine, lysine, and alanine. A total of 15 main phenolic substances were found in the extracts, and eight of them were identified. There were also 10 hydroxycinnamic acids in these extracts, three of which were identified (chlorogenic, caffeic, and rosmarinic acids). The dominant hydroxycinnamic acids were chlorogenic and caffeic acids. Among flavonoids, catechin, hyperoside, and rutin were identified. It should be noted that the extracts had a significant content of ellagic acid. On the basis of the results of the phytochemical analysis of the extracts, it can be concluded that the composition of phenolic compounds does not differ significantly, and the main differences are related to amino acids, which obviously have an impact on the overall pharmacological effect. The results obtained indicate the presence of anxiolytic activity in the motherwort extracts studied in complex with amino acids. The extracts with glycine, valine, and arginine were more effective in reducing anxiety in animals.

scholarly journals Investigation on the potential of poplar bark from short-rotation coppices as bio-based fungicidal additives

2021 ◽  
Author(s):  
Martina Bremer ◽  
Javane Oktaee ◽  
Daniela Einer ◽  
Steffen Fischer ◽  
André Wagenführ
Keyword(s):  
Fatty Acids ◽  
Chemical Composition ◽  
Outer Bark ◽  
Chemical Substances ◽  
Adverse Conditions ◽  
Short Rotation ◽  
Poplar Clones ◽  
Phenolic Substances ◽  
Excellent Source

AbstractBark on trees protects the plant against environmentally adverse conditions as well as fungi and insect attacks. There are different chemical substances, mostly in the outer bark of trees, which can stop fungi from developing. Bark as a by-product of wood plantations is available in high quantity and can serve as an excellent source for the production of eco-fungicides. In the presented article, bark of various poplar clones from two short-rotation coppices (SRC) in Poland and Germany was examined to determine the chemical composition, the possible extraction of potential fungicides (terpenes, aromatic and phenolic substances), and influence of their extracts on slowing the growth of mold fungi. It was proved that the content of the fungicidal substances depends strongly on the clone type. Two methods of extraction—Soxhlet and batch—were compared to obtain fungicidal extracts. Fungicidal substances were found in extracts gained with both approaches. Triterpenes, fatty acids, aldehydes, and alcohols were primarily the active fungicides in the Soxhlet extracts, whereas phenolic substances act as fungicides in the batch extracts.

scholarly journals Histochemistry and immunolocalisation of glucokinin in antidiabetic plants used in traditional Mexican medicine

2017 ◽  
Author(s):  
Guillermo Laguna-Hernández ◽  
Carlos A. Rio-Zamorano ◽  
Itzel G. Meneses-Ochoa ◽  
Alicia E. Brechú-Franco
Keyword(s):  
Medicinal Plants ◽  
Public Health Problem ◽  
Direct Application ◽  
Glucosidase Inhibitors ◽  
Naphthol Blue Black ◽  
Bauhinia Variegata ◽  
Alpha Glucosidase ◽  
Antidiabetic Plants

Mexico is a megadiverse country that has 3,600 to 4,000 species of medicinal plants, of which approximately 800 are used to treat conditions related to diabetes mellitus (DM). DM is a chronic degenerative disease of energy metabolism that exists as two types: type 1 (DM1) and type 2 (DM2). DM is considered a public health problem that affects 7% of the Mexican population older than 20 years. DM is clinically controlled with hypoglycaemic drugs, alpha-glucosidase inhibitors, insulin secretion stimulants or the direct application of insulin. The hypoglycaemic effectiveness of specific molecules has been determined only for some medicinal plants in Mexico used to treat DM2. The presence of molecules called glucokinins, wich are similar to animal insulin molecules, has been reported in some plant species; glucokinins act as both growth factors and regulators of glucose metabolism in plants. Therefore, we hypothesized that the hypoglycaemic effectiveness of some of the popularly used species for the control of DM could be due to the presence of glucokinin, as reported for Bauhinia variegata. The goal of this work was to use histochemistry to detect, the accumulation of protein that is immunocytochemically compatible with glucokinin in slide sections of hypoglycaemic species used as remedies for DM2. The top fourteen most used medicinal plants in Mexico were selected for study via microscopic sections. Proteins were histochemically detected using naphthol blue black and Johansen’s quadruple stain, and the immunocytochemical correspondence of the proteins with glucokinin was investigated using an insulin antibody. All species studied reacted positively to proteins and glucokinin in the same structures. The presence of glucokinin in these structures and the corresponding hypoglycaemic effects are discussed in the contex of the actions of other compounds.

scholarly journals Phytochemical analysis of diuretic collection

2016 ◽  
Author(s):  
O. H. Doroshenko ◽  
S. M. Marchyshyn
Keyword(s):  
Chemical Composition ◽  
Hplc Method ◽  
Hydroxycinnamic Acids ◽  
Phytochemical Analysis ◽  
Phenolic Substances ◽  
Ferulic Acids

Chemical composition of diuretic collection was studied. The presence of phenolic substances namely flavonoids, hydroxycinnamic acids and coumarines was proved. By HPLC method rutin, hiperoside, isoquercetin, luteolin, apigenin, coumarin, umbelliferon, scopoletin, chlorogenic, rosmarinic and ferulic acids were identified and their content was set.

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