scholarly journals In Vitro Studies on Alpha-amylase Inhibitory Activities of Zanthoxylum armatum of Mid-Western Regions of Nepal

2021 ◽  
Vol 2 (01) ◽  
pp. 28-36
Author(s):  
Deepak Dahal ◽  
Anup Subedee ◽  
Kalpana Khanal ◽  
Ram Chandra Basnyat

The alpha-amylase inhibitors are used as a drug to control hyperglycemia in type II diabetes mellitus. The plant extract is a natural source to minimize toxicity and other side effects. The alpha-amylase inhibition assay shows that the methanol extracts of fruits, seeds, leaves, and barks of Z. armatum exhibit 50% alpha-amylase inhibition activity at concentration 47.73 μg/mL, 50.25 μg/mL, 67.25 μg/mL, 152.6 μg/mL respectively, and hexane extracts of fruits, seeds, leaves and barks of Z. armatum exhibits 50% alpha-amylase inhibition activity at concentration 86.24 μg/mL, 84.02 μg/mL, 98.8 μg/mL, 138.81 μg/mL respectively, whereas the 50% alpha-amylase inhibition activity of Acarbose (standard) was found to be 33.66 μg/mL. Therefore, methanol and hexane extracts of fruits, seeds, and leaves show potential alpha-amylase inhibition activity and can be used as anti-diabetes.

Author(s):  
Jirawat Riyaphan ◽  
Chien-Hung Jhong ◽  
May-Jwan Tsai ◽  
Der-Nan Lee ◽  
Max K. Leong ◽  
...  

The inhibition of alpha-glucosidase and alpha-amylase is one of clinic strategies for remedy the type II diabetes. Herbal medicines are reported to alleviate hyperglycemia. However, the constituents from those sources whether are targeted to the alpha-glucosidase and alpha-amylase still unexplored. This study attempted to select the compounds for efficacy of hypoglycemia via cellular and mouse levels. The results illustrated that the cytotoxicity in all tested compounds at various concentrations except the concentration of 16-hydroxy-cleroda-3,13-dine-16,15-olide (HCD) at 30 µM were not significant difference (p > 0.05) when compared with the untreated control. Acarbose (reference drug), Antroquinonol, Catechin, Quercetin, Actinodaphnine, Curcumin, HCD, Docosanol, Tetracosanol, Berberine, and Rutin could effectively inhibit the alpha-glucosidase activity of Caco-2 cells when compared with the control (maltose). The compounds (Curcumin, HCD, Tetracosanol, Antroquinonol, Berberine, Catechin, Actinodaphnine, and Rutin) could reduce blood sugar level at 30 min in tested mice. The effects of tested compounds on area under curve (AUC) were significant (p < 0.05) among Acarbose, Tetracosanol, Antroquinonol, Catechin, Actinodaphnine, and Rutin along with Berberine and Quercetin. In in vitro (alpha-glucosidase) with in vivo (alpha-amylase) experiments suggest that bioactive compounds can be a potential inhibitor candidate of alpha-glucosidase and alpha-amylase for the alleviation of type II diabetes.


2000 ◽  
Vol 18 ◽  
pp. S144
Author(s):  
R. García-Robles ◽  
F. Villalba-Díaz ◽  
O. González-Albarrán ◽  
S. Calvo ◽  
O. Gómez ◽  
...  

2020 ◽  
pp. 266-272
Author(s):  
Dian Resti Setyaningrum ◽  
Rumiyati ◽  
Yekti Asih Purwestri ◽  
Satrijo Saloko ◽  
Agung Endro Nugroho ◽  
...  

Diabetes is a metabolic syndrome characterized by high blood sugar levels or hyperglycemia.Alpha-amylase inhibitors can be used as an antidiabetic that controls postprandial hyperglycemia.Alpha-amylase inhibitors are found in plants as protein and non-protein bioactive content such as in lebuiseed. The purpose of this study was to determine the activity of alpha-amylase inhibition of the fraction ofethanol extract of lebui seed. This research was carried out by extraction of lebui seed and then fractionatedlebui extract to obtain n-hexane fraction (HF), ethyl acetate fraction (EAF), and water fraction (WF). Thefractions then tested to alpha-amylase inhibition activity in vitro by measuring the reducing sugar using3.5-dinitrosalicylic (DNS) reagent. Furthermore, the identification of the bioactive content of each fraction wascarried out using thin layer chromatography. The results of alpha-amylase inhibition activity test showed thatall fractions had the ability to inhibit alpha-amylase. The IC50 value of the n-hexane fraction, ethyl acetatefraction, and water fraction were 173.05 mg/ml, 9.98 mg/ml, and 137.19 mg/ml, respectively. Ethyl acetatefraction has the smallest IC50 value compared to other fractions. Based on the identification of the bioactivecontent, bioactive content that is only found in the ethyl acetate fraction but not in other fractions are tannins.Therefore, the chemical content in lebui seed which acts as an alpha-amylase inhibitor might be tannins.


Biomolecules ◽  
2021 ◽  
Vol 11 (12) ◽  
pp. 1877
Author(s):  
Jirawat Riyaphan ◽  
Dinh-Chuong Pham ◽  
Max K. Leong ◽  
Ching-Feng Weng

Type-II diabetes mellitus (T2DM) results from a combination of genetic and lifestyle factors, and the prevalence of T2DM is increasing worldwide. Clinically, both α-glucosidase and α-amylase enzymes inhibitors can suppress peaks of postprandial glucose with surplus adverse effects, leading to efforts devoted to urgently seeking new anti-diabetes drugs from natural sources for delayed starch digestion. This review attempts to explore 10 families e.g., Bignoniaceae, Ericaceae, Dryopteridaceae, Campanulaceae, Geraniaceae, Euphorbiaceae, Rubiaceae, Acanthaceae, Rutaceae, and Moraceae as medicinal plants, and folk and herb medicines for lowering blood glucose level, or alternative anti-diabetic natural products. Many natural products have been studied in silico, in vitro, and in vivo assays to restrain hyperglycemia. In addition, natural products, and particularly polyphenols, possess diverse structures for exploring them as inhibitors of α-glucosidase and α-amylase. Interestingly, an in silico discovery approach using natural compounds via virtual screening could directly target α-glucosidase and α-amylase enzymes through Monte Carto molecular modeling. Autodock, MOE-Dock, Biovia Discovery Studio, PyMOL, and Accelrys have been used to discover new candidates as inhibitors or activators. While docking score, binding energy (Kcal/mol), the number of hydrogen bonds, or interactions with critical amino acid residues have been taken into concerning the reliability of software for validation of enzymatic analysis, in vitro cell assay and in vivo animal tests are required to obtain leads, hits, and candidates in drug discovery and development.


2019 ◽  
Vol 2019 ◽  
pp. 1-14 ◽  
Author(s):  
Fauze Camargo Maluf ◽  
David Feder ◽  
Alzira Alves de Siqueira Carvalho

In the early sixties, a discussion started regarding the association between Parkinson’s disease (PD) and type II diabetes mellitus (T2DM). Today, this potential relationship is still a matter of debate. This review aims to analyze both diseases concerning causal relationships and treatments. A total of 104 articles were found, and studies on animal and “in vitro” models showed that T2DM causes neurological alterations that may be associated with PD, such as deregulation of the dopaminergic system, a decrease in the expression of peroxisome proliferator-activated receptor-gamma coactivator-1α (PGC-1α), an increase in the expression of phosphoprotein enriched in diabetes/phosphoprotein enriched in astrocytes 15 (PED/PEA-15), and neuroinflammation, as well as acceleration of the formation of alpha-synuclein amyloid fibrils. In addition, clinical studies described that Parkinson’s symptoms were notably worse after the onset of T2DM, and seven deregulated genes were identified in the DNA of T2DM and PD patients. Regarding treatment, the action of antidiabetic drugs, especially incretin mimetic agents, seems to confer certain degree of neuroprotection to PD patients. In conclusion, the available evidence on the interaction between T2DM and PD justifies more robust clinical trials exploring this interaction especially the clinical management of patients with both conditions.


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