scholarly journals Intestinal α-Glucosidase Inhibitors in Achillea millefolium

2017 ◽  
Vol 12 (8) ◽  
pp. 1934578X1701200
Author(s):  
Kota Noda ◽  
Eisuke Kato ◽  
Jun Kawabata
Keyword(s):  
Enzyme Activity ◽  
Bioactive Compounds ◽  
Inhibitory Activity ◽  
Achillea Millefolium ◽  
Major Contributor ◽  
Caffeoylquinic Acids ◽  
Glucosidase Inhibitor ◽  
Glucosidase Inhibitors ◽  
Prevention And Treatment ◽  
Treatment Of Diabetes

Achillea millefolium is a plant used as a component of anti-diabetic preparation but the bioactive compounds responsible for its use are not known. Inhibition of intestinal α-glucosidase is a preferable effect for prevention and treatment of diabetes, and A. millefolium extract showed inhibitory activity against the enzyme. Activity-guided separation of the extract gave four mono- or di-caffeoylquinic acids as the isolate. Quantitation of these four caffeoylquinic acids and the activity of the isolates suggested that these are the major contributor for the α-glucosidase inhibitory activity in the extract. However also, the presence of unidentified, minor, but potent α-glucosidase inhibitor in the isolate was also suggested.

scholarly journals α-Glucosidase Inhibitory Activity of Cycloartane-Type Triterpenes Isolated from Indonesian Stingless Bee Propolis and Their Structure–Activity Relationship

2019 ◽  
Vol 12 (3) ◽  
pp. 102 ◽  
Author(s):  
Niken Pujirahayu ◽  
Debu Kumar Bhattacharjya ◽  
Toshisada Suzuki ◽  
Takeshi Katayama
Keyword(s):  
Inhibitory Activity ◽  
Antioxidant Activities ◽  
Stingless Bee ◽  
Structure Activity Relationships ◽  
Glucosidase Inhibitor ◽  
Structure Activity ◽  
Glucosidase Inhibitors ◽  
Ic50 Values ◽  
New Type ◽  
Treatment Of Diabetes

This study reports on the antioxidant activity and α-glucosidase inhibitory activity of five cycloartane-type triterpenes isolated from Indonesian stingless bee (Tetragonula sapiens Cockerell) propolis and their structure–activity relationships. The structure of the triterpenes was determined to include mangiferolic acid (1), Cycloartenol (2), ambonic acid (3), mangiferonic acid (4), and ambolic acid (5). The inhibitory test results of all isolated triterpenes against α-glucosidase showed a high potential for inhibitory activity with an IC50 range between 2.46 and 10.72 µM. Among the compounds tested, mangiferonic acid (4) was the strongest α-glucosidase inhibitor with IC50 2.46 µM compared to the standard (–)-epicatechin (1991.1 µM), and also had antioxidant activities with IC50 values of 37.74 ± 6.55 µM. The study on the structure–activity relationships among the compounds showed that the ketone group at C-3 and the double bonds at C-24 and C-25 are needed to increase the α-glucosidase inhibitory activity. The carboxylic group at C-26 is also more important for increasing the inhibitory activity compared with the methyl group. This study provides an approach to help consider the structural requirements of cycloartane-type triterpenes from propolis as α-glucosidase inhibitors. An understanding of these requirements is deemed necessary to find a new type of α-glucosidase inhibitor from the cycloartane-type triterpenes or to improve those inhibitors that are known to help in the treatment of diabetes.

scholarly journals α-Glucosidase Inhibitor Isolated from Blechum pyramidatum

2018 ◽  
Vol 13 (4) ◽  
pp. 1934578X1801300 ◽  
Author(s):  
Lilia Cherigo ◽  
Sergio Martínez-Luis
Keyword(s):  
Palmitic Acid ◽  
Inhibitory Activity ◽  
Competitive Inhibitor ◽  
Positive Control ◽  
Spectrometric Analysis ◽  
Docking Analysis ◽  
Glucosidase Inhibitor ◽  
Glucosidase Inhibitors ◽  
Medicinal Use ◽  
Bioassay Guided Fractionation

Blechum pyramidatum (Lam.) Urb. is a species of extensive medicinal use in the American continent. In fact, antidiabetic and anticancer preparations from this plant have been patented in Mexico, even though their active constituents are not yet known. It was recently discovered that B. pyramidatum inhibits the action of the α-glucosidase enzyme, thereby corroborating the antidiabetic properties attributed to this plant. The primary purpose of this study was to identify and characterize the α-glucosidase inhibitors from this species. Bioassay-guided fractionation of a crude extract of B. pyramidatum led to the isolation of a main α-glucosidase inhibitor, Palmitic acid (IC50 237.5). This compound was identified by both spectroscopic and spectrometric analysis. Its inhibitory activity was similar to that of the antidiabetic drug acarbose (IC50 241.6 μM), which was used as a positive control in our bioassay. Kinetic analysis established that palmitic acid acted as a competitive inhibitor. Docking analysis predicted that this compound binds to the same site as acarbose does in the human intestinal α-glucosidase (PDB: 3TOP). The presence of palmitic acid in B. pyramidatum and its potent inhibitory activity against α-glucosidase enzyme provides solid evidence to support the antidiabetic use of this plant in traditional medicine.

scholarly journals Synthesis of Pyrazolo[1,2-b]phthalazine-5,10- dione Derivatives: A New Class of α –Glucosidase Inhibitors

2021 ◽  
Author(s):  
Maryam Hosseinpoor Tehrani ◽  
Seyed Ahmad Mirshokraie ◽  
Mehdi Khoobi ◽  
Mohsen Amini
Keyword(s):  
Saccharomyces Cerevisiae ◽  
Enzyme Activity ◽  
Biological Activity ◽  
Inhibitory Activity ◽  
Diabetic Patients ◽  
New Class ◽  
Glucosidase Inhibitors ◽  
Membrane Bound ◽  
Carbohydrate Digestion ◽  
Control Post

Background: Hyperglycemia is a metabolic disorder that refers to an increase in blood sugar in diabetic patients. α-Glucosidase has been introduced as a membrane-bound enzyme, and it is the main enzyme for carbohydrate digestion in some parts of the intestine. Inhibition of α -glucosidase enzyme activity is a reliable approach to control post-prandial hyperglycemia condition. Objectives: In this study, a series of Pyrazolo[1,2-b]phthalazine-5,10-dione derivatives 5a–t were synthesized via a multicomponent reaction and evaluated as new inhibitors for α-glucosidase. Methods: The biological activity of the synthesized compounds was studied using a source of the α-glucosidase enzyme (EC3.2.1.20, Saccharomyces cerevisiae) at 20 U/mg concentration. Results: Four compounds showed higher α-glucosidase inhibitory activity in comparison to a standard, i.e., Acarbose. Compound 5q displays the most potent α-glucosidase inhibitory activity (IC50 = 155.4 ± 6.0 μM). Conclusion: In conclusion, some of the synthesized compounds, including heterocyclic core molecules, have shown remarkable activity that could be considered as subjects for the development of new, more efficient inhibitors of the α-glucosidase enzyme.

scholarly journals IN VITRO ANTIDIABETIC EFFECTS OF FERULA ASSA-FOETIDA EXTRACTS THROUGH DIPEPTIDYL PEPTIDASE IV AND α-GLUCOSIDASE INHIBITORY ACTIVITY

2017 ◽  
Vol 10 (5) ◽  
pp. 357 ◽  
Author(s):  
Adel Yarizade ◽  
Hsan Hasani Kumle ◽  
Ali Niazi
Keyword(s):  
Diabetes Mellitus ◽  
Inhibitory Activity ◽  
Postprandial Glucose ◽  
Dipeptidyl Peptidase ◽  
Dipeptidyl Peptidase Iv ◽  
Dpp Iv ◽  
Glucosidase Inhibitors ◽  
Treatment Of Diabetes ◽  
Ethanol Ethanol

Objective: Diabetes mellitus (DM) causes hyperglycemia, which is one of the most common diseases in the world. One of the strategies for the treatment of diabetes is maintaining postprandial glucose level through inhibition of dipeptidyl peptidase IV (DPP-IV) and α-glucosidase enzymes. The aim of this study was to determine in vitro antidiabetic potential of Ferula assa-foetida via DPP-IV and α-glucosidase inhibitory activities.Methods: F. assa-foetida seeds were extracted in methanol, ethanol, ethanol-methanol, and water. Inhibitory activity on DPP-IV and α-glucosidase wasperformed in vitro and measured spectrophotometrically at λ=405 nm.Results: The result showed that the F. assa-foetida seed extract is effective against both enzymes. All fractions had DPP-IV inhibitory activity, but the ethanolic fraction had the highest inhibitory activity on DPP-IV enzyme and significantly decreased DPP-IV activity (24.5%). With respect to α-glucosidase inhibitory activity, the aqueous extract has the highest inhibitory activity (28%).Conclusion: According to the results of this study, F. assa-foetida contains DPP-IV and α-glucosidase inhibitors and could be a potential source for the discovery of active constituents as α-glucosidase and DPP-IV inhibitors to treat Type 2 DM.Keywords: Diabetes mellitus, Herbal medicine, Dipeptidyl peptidase IV, α-glucosidase.

scholarly journals UPLC-MS-Based Metabolomics Profiling for α-Glucosidase Inhibiting Property of Parkia speciosa Pods

Life ◽  
2021 ◽  
Vol 11 (2) ◽  
pp. 78
Author(s):  
Mohammed S. M. Saleh ◽  
Juriyati Jalil ◽  
Nor Hidayah Mustafa ◽  
Fitri Fareez Ramli ◽  
Ahmad Yusof Asmadi ◽  
...  
Keyword(s):  
Bioactive Compounds ◽  
Inhibitory Activity ◽  
High Performance ◽  
Peninsular Malaysia ◽  
Flight Mass Spectrometry ◽  
Glucosidase Inhibitors ◽  
Potential Applications ◽  
Inhibitory Potential ◽  
Different Levels ◽  
Inhibiting Property

Parkia speciosa is a food plant that grows indigenously in Southeast Asia. A great deal of interest has been paid to this plant due to its traditional uses in the treatment of several diseases. The pods contain many beneficial secondary metabolites with potential applications in medicine and cosmetics. However, studies on their phytochemical properties are still lacking. Therefore, the present study was undertaken to profile the bioactive compounds of P. speciosa pods collected from six different regions of Malaysia through ultra-high-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UHPLC-QTOF-MS) and α-glucosidase inhibitory potential. This study applied metabolomics to elucidate the differences between P. speciosa populations found naturally in the different locations and to characterize potential α-glucosidase inhibitors from P. speciosa pods. P. speciosa collected from different regions of Malaysia showed good α-glucosidase inhibitory activity, with a median inhibitory concentration (IC50) of 0.45–0.76 μg/mL. The samples from the northern and northeastern parts of Peninsular Malaysia showed the highest activity. Using UHPLC-QTOF-MS/MS analysis, 25 metabolites were identified in the pods of P. speciosa. The findings unveiled that the pods of P. speciosa collected from different locations exhibit different levels of α-glucosidase inhibitory activity. The pods are a natural source of potent antidiabetic bioactive compounds.

Pharmaceutical quality of yarrow (Achillea millefolium L. s.l.) – Investigation of 40 commercial drug samples by means of the bioactive compounds

Planta Medica ◽  
2007 ◽  
Vol 73 (09) ◽  
Author(s):  
B Benedek ◽  
K Rothwangl-Wiltschnigg ◽  
E Rozema ◽  
N Gjoncaj ◽  
G Reznicek ◽  
...  
Keyword(s):  
Bioactive Compounds ◽  
Achillea Millefolium ◽  
Pharmaceutical Quality

TOTAL POLYPHENOL CONTENT, FREE RADICAL SCAVENGING, ALPHA-GLUCOSIDASE INHIBITION CAPACITY, THE EFFICACY IN CONTROLLING BLOOD GLUCOSE OF DIABETIC RATS OF THE MIXTURE VOS EXTRACTED FROM THE LEAVES OF CLEISTOCALYX OPERCULATUS, PSIDIUM GUAJAVA AND NELUMBO NUCIFERA

2013 ◽  
pp. 50-55
Author(s):  
Tuyet Mai Truong ◽  
Thi Lam Nguyen ◽  
Lan Anh Pham ◽  
Hoang Kien Truong
Keyword(s):  
Body Weight ◽  
Blood Glucose ◽  
Radical Scavenging ◽  
Psidium Guajava ◽  
Free Radical Scavenging ◽  
Diabetic Mice ◽  
Cleistocalyx Operculatus ◽  
Prevention And Treatment ◽  
Treatment Of Diabetes ◽  
Alpha Glucosidase

Objective: Plant polyphenols have antioxidant capacity and alpha-glucosidase inhibition to supporting for prevention and treatment of diabetes. Materials and Method: Present study was conducted to determine the content of total polyphenols, free radical scavenging and alpha-glucosidase inhibition of the VOS mixture that extracted from leaves (Voi leaves - Cleistocalyx operculatus (V), Oi leaves - Psidium guajava (O), Sen leaves - Nelumbo nucifera (S)). Results: The efficacy of blood glucose controlling in diabetic mice was investigated. After 8 weeks of administration with 200 mg VOS/kg body weight and 400 mg VOS/kg body weight, VOS diabetic mice had significantly reduced blood glucose level as compared to control diabetic mice. VOS diabetic mice with 400 mg dosage are lower in blood glucose levels than that of the diabetic mice with 200 mg. Also, the significant reducing in HbA1c was observed in VOS diabetic mice as compared with control diabetic mice. Conclusion: VOS-product extracted from Cleistocalyx operculatus leaves, guava leaves, lotus leaves might be considered as a safe product and to be a potential product in the supporting of prevention and treatment of diabetes.

scholarly journals An Insight into Kiwiberry Leaf Valorization: Phenolic Composition, Bioactivity and Health Benefits

Molecules ◽  
2021 ◽  
Vol 26 (8) ◽  
pp. 2314
Author(s):  
Ana Margarida Silva ◽  
Diana Pinto ◽  
Iva Fernandes ◽  
Victor de Freitas ◽  
María de la Luz Cádiz-Gurrea ◽  
...  
Keyword(s):  
Bioactive Compounds ◽  
Plant Material ◽  
Dry Weight ◽  
Alcoholic Extract ◽  
Phenolic Profile ◽  
Hydroalcoholic Extract ◽  
Caffeoylquinic Acids ◽  
Solar Exposure ◽  
Assisted Extraction ◽  
Phenolic And Flavonoid

During kiwiberry production, different by-products are generated, including leaves that are removed to increase the fruit’s solar exposure. The aim of this work was to extract bioactive compounds from kiwiberry leaf by employing microwave-assisted extraction (MAE). Compatible food solvents (water and ethanol) were employed. The alcoholic extract contained the highest phenolic and flavonoid contents (629.48 mg of gallic acid equivalents (GAE) per gram of plant material on dry weight (dw) (GAE/g dw) and 136.81 mg of catechin equivalents per gram of plant material on dw (CAE/g dw), respectively). Oppositely, the hydroalcoholic extract achieved the highest antioxidant activity and scavenging activity against reactive oxygen and nitrogen species (IC50 = 29.10 μg/mL for O2•−, IC50 = 1.87 μg/mL for HOCl and IC50 = 1.18 μg/mL for •NO). The phenolic profile showed the presence of caffeoylquinic acids, proanthocyanidin, and quercetin in all samples. However, caffeoylquinic acids and quercetin were detected in higher amounts in the alcoholic extract, while proanthocyanidins were prevalent in the hydroalcoholic extract. No adverse effects were observed on Caco-2 viability, while the highest concentration (1000 µg/mL) of hydroalcoholic and alcoholic extracts conducted to a decrease of HT29-MTX viability. These results highlight the MAE potentialities to extract bioactive compounds from kiwiberry leaf.

scholarly journals Anabaenopeptins: What We Know So Far

Toxins ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 522
Author(s):  
Patrick Romano Monteiro ◽  
Samuel Cavalcante do Amaral ◽  
Andrei Santos Siqueira ◽  
Luciana Pereira Xavier ◽  
Agenor Valadares Santos
Keyword(s):  
Secondary Metabolites ◽  
Bioactive Compounds ◽  
Inhibitory Activity ◽  
Important Class ◽  
Biotechnological Applications ◽  
Peptide Synthetases ◽  
Ecological Roles ◽  
Cyclic Hexapeptides ◽  
Key Features

Cyanobacteria are microorganisms with photosynthetic mechanisms capable of colonizing several distinct environments worldwide. They can produce a vast spectrum of bioactive compounds with different properties, resulting in an improved adaptative capacity. Their richness in secondary metabolites is related to their unique and diverse metabolic apparatus, such as Non-Ribosomal Peptide Synthetases (NRPSs). One important class of peptides produced by the non-ribosomal pathway is anabaenopeptins. These cyclic hexapeptides demonstrated inhibitory activity towards phosphatases and proteases, which could be related to their toxicity and adaptiveness against zooplankters and crustaceans. Thus, this review aims to identify key features related to anabaenopeptins, including the diversity of their structure, occurrence, the biosynthetic steps for their production, ecological roles, and biotechnological applications.

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