scholarly journals Phytochemical screening and in vitro evaluation of alpha amylase, alpha glucosidase and beta galactosidase inhibition by aqueous and organic Atractylis gummifera L. extracts

2018 ◽  
Vol 5 (3) ◽  
pp. 103-112 ◽  
Author(s):  
Khadija Bouabid ◽  
Fatima Lamchouri ◽  
Hamid Toufik ◽  
Karima Sayah ◽  
Yahia Cherrah ◽  
...  

Diabetes is a chronic condition which is increasingly progressing throughout the world. To treat it, several methods are used, among which is medicinal plants that still have an unknown mechanism of action. The objective of this work is to evaluate the in vitro hypoglycemic effect of the extracts of the underground part of Atractylis gummifera, a member of Asteraceae used in traditional Moroccan medicine. A phytochemical study of the aqueous extracts (decocted, infused and macerated) and organic extracts (methanol, methanol macerate, chloroformic, ethyl acetate and petroleum ether), and a phytochemical screening of the different secondary metabolites was done. The antidiabetic power of the extracts of A. gummifera by testing the inhibitory activity of ?-amylase, ?-glucosidase and ?-galactosidase, which are enzymes responsible for the digestion of polysaccharides was determined. The extracts of A. gummifera are very rich in flavonoids and tannins, and are inhibitory to?-amylase and ?-glucosidase, mainly the macerate of methanol with IC50 values of 0.557 ± 0.013 and 0.743 ± 0.017 mg / mL respectively. Higher ?-galactosidase inhibitory potential than quercetin was observed for aqueous macerates and methanol with IC50 values of 2.23 ± 0.012 and 2.443 ± 0.071 mg / mL respectively. The extracts of A. gummifera possess a significant inhibitory activity of the alpha amylase and alpha glucosidase and beta-galactosidase enzymes, in particular the macerate of methanol followed by the aqueous macerate, among the eight extracts tested.

Author(s):  
Kushagra Dubey ◽  
Raghvendra Dubey ◽  
Revathi Gupta ◽  
Arun Gupta

Background: Diosmin is a flavonoid obtained from the citrus fruits of the plants. Diosmin has blood lipid lowering activities, antioxidant activity, enhances venous tone and microcirculation, protects capillaries, mainly by reducing systemic oxidative stress. Objective: The present study demonstrates the potential of Diosmin against the enzymes aldose reductase, α-glucosidase, and α-amylase involved in diabetes and its complications by in vitro evaluation and reverse molecular docking studies. Method: The assay of aldose reductase was performed by using NADPH as starting material and DL-Glyceraldehyde as a substrate. DNS method was used for alpha amylase inhibition and in alpha glucosidase inhibitory activity p-nitrophenyl glucopyranoside (pNPG) was used as substrate. The reverse molecular docking studies was performed by using Molegro software (MVD) with grid resolution of 30 Å. Result: Diosmin shows potent inhibitory effect against aldose reductase (IC50:333.88±0.04 µg/mL), α-glucosidase (IC50:410.3±0.01 µg/mL) and α-amylase (IC50: 404.22±0.02 µg/mL) respectively. The standard drugs shows moderate inhibitory activity for enzymes. The MolDock Score of Diosmin was -224.127 against aldose reductase, -168.17 against α-glucosidase and -176.013 against α-amylase respectively, which was much higher than standard drugs. Conclusion: From the result it was concluded that diosmin was a potentially inhibitor of aldose reductase, alpha amylase and alpha glucosidase enzymes then the standard drugs and it will be helpful in the management of diabetes and its complications. This will also be benevolent to decrease the socio economical burden on the middle class family of the society.


Author(s):  
May A El-manawaty ◽  
Lamiaa Gohar

Objective: Diabetes mellitus is a highly prevalent chronic disease in Egypt leading to high socioeconomic problems, especially in the cities due to the unhealthy life style. Although many drugs are available, they have many side effects. Furthermore, the body arouses resistance after a while for the drug so it should be changed every once in a while. Plants could be a good source for drugs. In Egypt, we have a rich flora which has not been subjected to systematic screening for antidiabetic activity.Methods: The aim of this work was to screen 264 plant extracts for their in vitro α-glucosidase inhibitory activity. Those extracts which gave more than 70% inhibition were screened on different concentrations and their inhibitory concentrations giving 50% activity (IC50) were calculated.Results: Out of all the tested extracts, 63 gave more than or equal 70% inhibition on α-glucosidase at the tested concentration (25 ppm). After the calculation of the IC50 values, 10 extracts were chosen for further study having 5 ppm and less IC50.Conclusion: The most active plant extract is Pinus roxburghii Sarg. branches (IC50 is 2.47 ppm).


2021 ◽  
Vol 16 (1) ◽  
pp. 211-118
Author(s):  
Venkatesh S ◽  
Aswani K ◽  
Asheena Asharaf V V ◽  
Anjitha P ◽  
Suresh A ◽  
...  

The present study has been undertaken to evaluate the in-vitro, in-vivo and ex-vivo anti-diabetic activity of leaves of chloroform extract Clerodendrum paniculatum (CECP). The extract was prepared by soxhlet extraction. Phytochemical screening indicates the presence of flavonoids, phenols, carbohydrates etc. The anti-diabetic activity of extract was studied by in-vitro (alpha amylase inhibition and alpha glucosidase inhibition assay), in-vivo (streptozotocin induced diabetes) and ex-vivo (glucose uptake by rat hemi - diaphragm method). For in-vitro studies, the inhibitory action of CECP was compared with standard drug Acarbose. The IC50 values of CECP for alpha amylase and alpha glucosidase was found to be 158.396 µg/ml and 113.122 µg/ml respectively and the extract shows significant anti-diabetic activity. For in-vivo and ex-vivo studies Glibenclamide was used as a standard drug to compare the blood glucose level and uptake of glucose was calculated. The results obtained from the study indicate that both 200 mg/kg and 400 mg/kg of CECP showed significant anti-diabetic activity. The 400 mg/kg of CECP showed better activity when compared to 200 mg/kg of the extract. The glucose uptake study was performed by isolated rat hemidiaphragm method. The hemi diaphragm obtained from the rats treated with both the doses of CECP showed significant glucose uptake.


Author(s):  
Gejalakshmi S. ◽  
Harikrishnan N. ◽  
Anas S. Mohameid

Background: Diabetes mellitus is a metabolic condition characterized by elevated blood glucose levels in the bloodstream. It occurs due to the inadequate amount of insulin secreted in the body or resistance of insulin receptors. Objective: In the present study, for its effect on alpha-amylase and alpha-glucosidase enzymes, Oroxylum indicuma flavone glycoside was assessed using in-vitro assays by removing the respective enzymes from whole wheat and barley in conjunction with in-silico analysis. Method: in-vitro alpha amylase inhibitory activity and in-vitro alpha glucosidase inhibitory activity was performed using acarbose as a standard drug. The molecular docking study was performed using Schrodinger (Maestro V 11.5) software. The parameters glide score, Lipinski rule for drug likeliness, bioactive scoring and ADME properties were assessed in the docking study. In addition, baicalein's antioxidant function was assessed using DPPH assay, nitric oxide scavenging activity. The cytotoxicity of Oroxylum indicumwas evaluated using the Brine shrimp lethality assay. Results: The alpha-amylase assay performed showed IC50 value of 48.40 µg/ml for Oroxylum indicumwhereas alpha-glucosidase assay showed an IC50 value of 16.03 µg/ml. Oroxylum indicumshows the glide score of-5.565 with 5EOF and glide score of -5.339 with 5NN8 in the molecular docking study. The highest percentage of DPPH radical scavenging activity and nitrous oxide scavenging activity were found to be.27% at160 µg/ml and 50.02% at the concentrations of 160 µg/ml respectively. Conclusion: Based on further in vivo and clinical trials, Oroxylum indicummay be used for the management of hyperglycaemia.


Aim: The present study was designed to investigate the in vitro inhibitory potential of Euphorbia hirta root extract on alpha-amylase and alpha glucosidase enzymes. Materials and Methods: Alcoholic extract of Euphorbia hirta was subjected to inhibitory effect of alpha-amylase and alpha-glucosidase using specific standard in vitro procedure. Results: The results revealed that extract successfully inhibited the activity of both enzymes in an in vitro model. The alcoholic root extract of Euphorbia hirta inhibited the alpha amylase and alpha glucosidase enzymes as 79.73 ± 0.18% and 81.35 ± 0.12% respectively. Conclusion: The present study showed that, the alcoholic extract showed a significant inhibitory effect on alpha amylase and alpha glucosidase enzymes, thus validating the traditional use of the plant.


Antioxidants ◽  
2020 ◽  
Vol 9 (11) ◽  
pp. 1149
Author(s):  
Ninon G. E. R. Etsassala ◽  
Jelili A. Badmus ◽  
Jeanine L. Marnewick ◽  
Emmanuel I. Iwuoha ◽  
Felix Nchu ◽  
...  

Diabetes mellitus (DM) is one of the most dangerous metabolic diseases with a high rate of mortality worldwide. It is well known that insulin resistance and deficiency in insulin production from pancreatic β-cells are the main characteristics of DM. Due to the detrimental side effects of the current treatment, there is a considerable need to develop new effective antidiabetic drugs, especially alpha-glucosidase and alpha-amylase inhibitors with lesser adverse effects. These inhibitors are known to be directly involved in the delay of carbohydrate digestion, resulting in a reduction of glucose absorption rate and, consequently, reducing the postprandial rise of plasma glucose, which can reduce the risk of long-term diabetes complications. Furthermore, natural products are well-known sources for the discovery of new bioactive compounds that can serve as scaffolds for drug discovery, including that of new antidiabetic drugs. The phytochemical investigation of Salvia aurita collected from Hogobach Pass, Eastern Cape Province, South Africa (SA), yielded four known abietane diterpenes namely carnosol (1), rosmanol (2), 7-methoxyrosmanol (3), 12-methoxycarnosic acid (4), and one flavonoid named 4,7-dimethylapigenin (5). Structural characterization of these isolated compounds was conducted using 1 and 2D NMR, in comparison with reported spectroscopic data. These compounds are reported for the first time from S. aurita. The biological evaluation of the isolated compound against alpha-glucosidase exhibited strong inhibitory activities for 3 and 2 with the half maximal inhibitory concentration (IC50) values of 4.2 ± 0.7 and 16.4 ± 1.1 µg/mL respectively, while 4 and 1 demonstrated strong alpha-amylase inhibitory activity amongst the isolated compounds with IC50 values of 16.2 ± 0.3 and 19.8 ± 1.4 µg/mL. Molecular docking analysis confirms the strong inhibitory activity of 3 against alpha-glucosidase. Additionally, excellent antioxidant capacities were displayed by 2, 1, and 3, respectively, with oxygen radical absorbance capacity (ORAC) (25.79 ± 0.01; 23.96 ± 0.01; 23.94 ± 0.02) mM Trolox equivalent (TE)/g; 1 and 2 as ferric-ion reducing antioxidant power (FRAP) (3.92 ± 0.002; 1.52 ± 0.002) mM ascorbic acid equivalent (AAE)/g; 5 and 2 as Trolox equivalent absorbance capacity (TEAC) (3.19 ± 0.003; 2.06 ± 0.003) mM TE/g. The methanolic extract of S. aurita is a rich source of abietane diterpenes with excellent antioxidant and antidiabetic activities that can be useful to modulate oxidative stress and might possibly be excellent candidates for the management of diabetes. This is the first scientific report on the phytochemical isolation and biological evaluation of the alpha-glucosidase and alpha-amylase inhibitory activities of Salvia aurita.


2019 ◽  
Vol 9 (6) ◽  
pp. 102-109 ◽  
Author(s):  
Durgeshnandani Sinha ◽  
Trilochan Satapathy ◽  
Parag Jain ◽  
Jhakeshwar Prasad Chandel ◽  
Divya Sahu ◽  
...  

Objective: The present study was performed to determine in vitro antidiabetic effect of neohesperidin. To evaluate inhibitory effect of neohesperidin on α-amylase and α-glucosidase diabetes causing enzyme. Methods and Materials: Invitro carbohydrate metabolizing enzyme based inhibitory methods were used to determine antidiabetic effect of neohesperidin. Alpha (α)-amylase inhibitory assay was performed using different sources i.e. wheat alpha (α)-amylase enzyme, salivary alpha (α)-amylase and fungal alpha (α)-amylase assay. Alpha (α)-glucosidase inhibitory assay was performed using alpha (α)-glucosidase (B. stearothermophil), alpha (α)-glucosidase rat intestine and alpha (α)-glucosidase from baker’s yeast. Sucrase inhibitory assay from rat small intestine. Result: Neohesperidin possess a potent anti-diabetic by significantly inhibiting alpha amylase activity. Conclusion: It was concluded that enzyme inhibitory activity of neohesperidin shown a significantly higher inhibitory activity on alpha-amylase in comparision to alpha-glucosidase & Sucrase enzymes. Keywords: Neohespiridin, acarbose, alpha-amylase, alpha-glucosidase


2008 ◽  
Vol 55 (2) ◽  
pp. 391-398 ◽  
Author(s):  
Rammohan Subramanian ◽  
M Zaini Asmawi ◽  
Amirin Sadikun

There has been an enormous interest in the development of alternative medicines for type 2 diabetes, specifically screening for phytochemicals with the ability to delay or prevent glucose absorption. The goal of the present study was to provide in vitro evidence for potential inhibition of alpha-glucosidase and alpha-amylase enzymes, followed by a confirmatory in vivo study on rats to generate a stronger biochemical rationale for further studies on the ethanolic extract of Andrographis paniculata and andrographolide. The extract showed appreciable alpha-glucosidase inhibitory effect in a concentration-dependent manner (IC(50)=17.2+/-0.15 mg/ml) and a weak alpha-amylase inhibitory activity (IC(50)=50.9+/-0.17 mg/ml). Andrographolide demonstrated a similar (IC(50)=11.0+/-0.28 mg/ml) alpha-glucosidase and alpha-amylase inhibitory activity (IC(50)=11.3+/-0.29 mg/ml). The positive in vitro enzyme inhibition tests paved way for confirmatory in vivo studies. The in vivo studies demonstrated that A. paniculata extract significantly (P


2018 ◽  
Vol 40 (3) ◽  
Author(s):  
Tran Duc Tuong ◽  
Duong Xuan Chu ◽  
Bui Thi Minh Dieu

ABSTRACT Alpha-amylase and α-glucosidase are two main enzymes involved in carbohydrate metabolism. Inhibition of α-amylase and α-glucosidase can be said as an effective treatment for delaying the absorption of glucose after meals in people with diabetes mellitus. The objective of the present study is to provide an in vitro evidence for the potential hypoglycemic activity via inhibitory activity of the ethanolic and aqueous extracts from fruiting bodies of Pycnoporus sanguineus mushroom on α-amylase and α-glucosidase enzymes. Alpha-amylase and α-glucosidase inhibitory activities of aqueous and ethanolic extracts of P. sanguineus fruiting body were examined in a dose-response manner. Acarbose was used as a positive control. The results showed that the ethanolic extract of P. sanguineus possessed strong inhibitory activity on α-amylase and α-glucosidase with IC50 values of 97.08 and 92.60 μg/mL, respectively. The aqueous extract also exhibited moderate activity against α-amylase and α-glucosidase with IC50 values of 150.15 and 102.29 μg/mL, respectively. Which was significantly lower than that of acarbose with IC50 values of 85.12 and 68.36 μg/mL, respectively. The degree of α-amylase and α-glucosidase inhibition was correlated with the dose of inhibitors. From these results Pycnoporus sanguineus (Trametes sanguinea) possesses high potential in lowering blood glucose level, reduced insulin resistance and the risk of diabetic-related complications.


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