scholarly journals Effect of Avarai Kudineer on α- Amylase and α- Glucosidase Inhibition: A Preclinical Antidiabetic Study

2021 ◽  
pp. 818-825
Author(s):  
K. Rajalakshmi ◽  
P. Shanmugapriya ◽  
G. J. Christian ◽  
R. Jeeva Gladys
Keyword(s):  
Diabetes Mellitus ◽  
Preparation Method ◽  
Maximum Activity ◽  
Alpha Amylase ◽  
Test Drug ◽  
Standard Drug ◽  
Polyherbal Formulation ◽  
Alpha Glucosidase

In recent years there has been a mounting interest towards the traditional medicine globally for the treatment of type 2 diabetes. Avarai Kudineer (AK) is a Siddha classical polyherbal formulation that has been indicated for the management of Diabetes mellitus in Siddha literature. The goal of the present study is to provide an in-vitro evidence for the  antidiabetic potential of Avarai Kudineer in terms of  inhibiting the carbohydrate digesting enzymes alpha amylase and alpha glucosidase. Aavirai Kudineer (1/4) was prepared by boiling the ingredients weighed 20g in 80ml and reduced to 20ml and filtered according to the decoction preparation method as indicted in the Siddha literature. The filtrate was dissolved in DMSO to make stock solution and serially diluted to make different concentrations ranging from 10,20,40,80 and 100 µg/ml. The triplicates (n=3) were maintained. The invitro alpha amylase and alpha glucosidase enzyme inhibition of AK sample was compared with standard drug acarbose and the IC 50 value was calculated.The data was statistically analysed and expressed as Mean ± SD (n=3). The results showed that AK had maximum activity towards the inhibition of the enzyme alpha amylase (59.83± 7.10) and alpha glucosidase (71.94 ± 1.22) when compared with the standard acarbose81.42± 5.51 and 91.59 ±12.79respectively. The results reveal that the test drug AK has appreciable alpha amylase and alpha glucosidase inhibitory activity.

scholarly journals Phenolics Profiling of Carpobrotus edulis (L.) N.E.Br. and Insights into Molecular Dynamics of Their Significance in Type 2 Diabetes Therapy and Its Retinopathy Complication

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4867
Author(s):  
Saheed Sabiu ◽  
Fatai O. Balogun ◽  
Stephen O. Amoo
Keyword(s):  
Type 2 Diabetes ◽  
Phenolic Compounds ◽  
Aldose Reductase ◽  
Alpha Amylase ◽  
Diabetes Therapy ◽  
Carpobrotus Edulis ◽  
Phenolic Extract ◽  
Alpha Glucosidase

Adverse effects associated with synthetic drugs in diabetes therapy has prompted the search for novel natural lead compounds with little or no side effects. Effects of phenolic compounds from Carpobrotus edulis on carbohydrate-metabolizing enzymes through in vitro and in silico methods were assessed. Based on the half-maximal inhibitory concentrations (IC50), the phenolic extract of the plant had significant (p < 0.05) in vitro inhibitory effect on the specific activity of alpha-amylase (0.51 mg/mL), alpha-glucosidase (0.062 mg/mL) and aldose reductase (0.75 mg/mL), compared with the reference standards (0.55, 0.72 and 7.05 mg/mL, respectively). Molecular interactions established between the 11 phenolic compounds identifiable from the HPLC chromatogram of the extract and active site residues of the enzymes revealed higher binding affinity and more structural compactness with procyanidin (−69.834 ± 6.574 kcal/mol) and 1,3-dicaffeoxyl quinic acid (−42.630 ± 4.076 kcal/mol) as potential inhibitors of alpha-amylase and alpha-glucosidase, respectively, while isorhamnetin-3-O-rutinoside (−45.398 ± 4.568 kcal/mol) and luteolin-7-O-beta-d-glucoside (−45.102 ± 4.024 kcal/mol) for aldose reductase relative to respective reference standards. Put together, the findings are suggestive of the compounds as potential constituents of C. edulis phenolic extract responsible for the significant hypoglycemic effect in vitro; hence, they could be exploited in the development of novel therapeutic agents for type-2 diabetes and its retinopathy complication.

scholarly journals BIOASSAY-GUIDED EVALUATION OF FICUS SEMICORDATA FOR ANTIDIABETIC ACTIVITY

2017 ◽  
Vol 9 (3) ◽  
pp. 71 ◽  
Author(s):  
Virender Kaur ◽  
Kumud Upadhyaya ◽  
Milind Pande
Keyword(s):  
Diabetes Mellitus ◽  
Early Stage ◽  
Ethanol Extract ◽  
Postprandial Hyperglycemia ◽  
Alpha Amylase ◽  
Antidiabetic Activity ◽  
Biological Studies

Objective: The early stage of diabetes mellitus type 2 is associated with postprandial hyperglycemia. The therapeutic approach involved in the treatment of type 2 diabetes mellitus is the use of agents that can decrease postprandial hyperglycemia by inhibiting carbohydrate digesting enzymes. In an effort of identifying herbal drugs which may become useful in the prevention or mitigation of diabetes, the antidiabetic activity of Ficus semicordata (FS) and its constituents were studied. The present study was undertaken in part to identify the potent antihyperglycemic fraction from the ethanol extract of the plant, using bioassay guided evaluation.Methods: The ethanol extract of Ficus semicordata were fractionated to obtain chloroform, ethyl acetate, n-butanol and ethanol extracts which were tested for alpha-amylase, alpha-glucosidase inhibitory, properties. Further fractionation of the more active ethanol fraction yielded isolates FS-1 and FS-2 which were tested for in vivo antidiabetic activity using Streptozotocin (STZ)-induced diabetic rats.Results: Ethanol extract from leaves of the plant showed notable alpha-amylase (IC50 = 3.352µg/ml and alpha-glycosidase inhibitory activity (IC50= 3.448µg/ml) as compared to standard acarbose (IC50 = 3.175µg/ml. Subfraction FS-1 and FS-2 which were tested for in vivo antidiabetic activity using acute STZ-induced diabetic rats significantly (*p<0.05, **p<0.01, *** p<0.001) reduced blood glucose level.Conclusion: The Ficus semicordata plant extracts and the fractionated components could be used as a natural antidiabetic after comprehensive in vitro and in vivo biological studies.

scholarly journals Anti-diabetic activity of Clerodendrum paniculatum leaves by In-vitro, In-vivo and Ex-vivo methods

2021 ◽  
Vol 16 (1) ◽  
pp. 211-118
Author(s):  
Venkatesh S ◽  
Aswani K ◽  
Asheena Asharaf V V ◽  
Anjitha P ◽  
Suresh A ◽  
...  
Keyword(s):  
Glucose Uptake ◽  
Ex Vivo ◽  
Soxhlet Extraction ◽  
Chloroform Extract ◽  
Alpha Amylase ◽  
Standard Drug ◽  
Ic50 Values ◽  
Alpha Glucosidase

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.

scholarly journals Inhibitory effects of Launaea taraxacifolia and Strychnos spinosa leaves extract on an isolated digestive enzyme linked to type -2 -diabetes mellitus

2018 ◽  
Vol 9 (2) ◽  
pp. 52 ◽  
Author(s):  
Michael Buenor Adinortey ◽  
Justice Kwabena Sarfo ◽  
Cynthia Ayefoumi Adinortey ◽  
Eric Gyamerah Ofori ◽  
Jeffrey Kwarteng ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Digestive Enzyme ◽  
Inhibitory Effect ◽  
Leaf Extracts ◽  
Standard Drug ◽  
Soxhlet Apparatus ◽  
Inhibitory Potential ◽  
Strychnos Spinosa

Background: The most prevalent type of diabetes mellitus (Type-2), is managed using many approaches, including the lowering of postprandial hyperglycaemia. Inhibition of key enzymes involved in carbohydrate breakdown such as α-glucosidase and α-amylase has been reported as a novel strategy to delay the absorption of glucose after meals. This study sought to determine the in vitro inhibitory potential of Launaea taraxacifolia and Strychnos spinosa leaf extracts on α-glucosidase enzyme and also determine their modes of inhibiting the enzyme.Materials and Methods: Plant extracts were prepared using soxhlet apparatus. Inhibitory effect of extracts at different concentrations and mode of inhibition were carried out using α-glucosidase enzyme isolated from the small intestine of a guinea pig. Results: Extracts of Launaea taraxacifolia (LTE) and Strychnos spinosa (SSE) leaves showed α-glucosidase inhibitory potential of approximately 69 % and 79 % respectively as compared to 73 % for standard drug-acarbose at a maximum concentration of 1000 μg/mL. The IC50 values recorded were 205.2±0.044 μg/mL, 129.4±0.094 μg/mL and 196.9±0.036 μg/mL for LTE, SSE and acarbose respectively. The Lineweaver Burk plot showed an uncompetitive mode of inhibition for both LTE and SSE as depicted by the lower Km and Vmax of enzyme inhibited by extracts compared to control. Conclusion: Extracts of Launaea taraxacifolia and Strychnos spinosa leaves showed significant inhibitory effect on an isolated intestinal α-glucosidase enzyme in an uncompetitive mode

scholarly journals Teucrium polium: Potential Drug Source for Type 2 Diabetes Mellitus

Biology ◽  
2022 ◽  
Vol 11 (1) ◽  
pp. 128
Author(s):  
Yaser Albadr ◽  
Andrew Crowe ◽  
Rima Caccetta
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Insulin Secretion ◽  
Β Cells ◽  
Pancreatic Β Cells ◽  
Glucose Levels ◽  
Teucrium Polium

The prevalence of type 2 diabetes mellitus is rising globally and this disease is proposed to be the next pandemic after COVID-19. Although the cause of type 2 diabetes mellitus is unknown, it is believed to involve a complex array of genetic defects that affect metabolic pathways which eventually lead to hyperglycaemia. This hyperglycaemia arises from an inability of the insulin-sensitive cells to sufficiently respond to the secreted insulin, which eventually results in the inadequate secretion of insulin from pancreatic β-cells. Several treatments, utilising a variety of mechanisms, are available for type 2 diabetes mellitus. However, more medications are needed to assist with the optimal management of the different stages of the disease in patients of varying ages with the diverse combinations of other medications co-administered. Throughout modern history, some lead constituents from ancient medicinal plants have been investigated extensively and helped in developing synthetic antidiabetic drugs, such as metformin. Teucrium polium L. (Tp) is a herb that has a folk reputation for its antidiabetic potential. Previous studies indicate that Tp extracts significantly decrease blood glucose levels r and induce insulin secretion from pancreatic β-cells in vitro. Nonetheless, the constituent/s responsible for this action have not yet been elucidated. The effects appear to be, at least in part, attributable to the presence of selected flavonoids (apigenin, quercetin, and rutin). This review aims to examine the reported glucose-lowering effect of the herb, with a keen focus on insulin secretion, specifically related to type 2 diabetes mellitus. An analysis of the contribution of the key constituent flavonoids of Tp extracts will also be discussed.

scholarly journals Potent Natural Inhibitors of Alpha-Glucosidase and Alpha-Amylase against Hyperglycemia in Vitro and in Vivo

2017 ◽  
Author(s):  
Jirawat Riyaphan ◽  
Chien-Hung Jhong ◽  
May-Jwan Tsai ◽  
Der-Nan Lee ◽  
Max K. Leong ◽  
...  
Keyword(s):  
Type Ii Diabetes ◽  
Herbal Medicines ◽  
Alpha Amylase ◽  
Type Ii ◽  
Reference Drug ◽  
Significant Difference ◽  
Natural Inhibitors ◽  
Alpha Glucosidase

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 &micro;M were not significant difference (p &gt; 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 &lt; 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.

scholarly journals In Vitro Antioxidant and Anti-Diabetic Potential of Gymnema Sylvestre Methanol Leaf Extract

2017 ◽  
Vol 13 (36) ◽  
pp. 218 ◽  
Author(s):  
Ibrahim A. ◽  
Babandi A. ◽  
Tijjani A.A. ◽  
Murtala Y. ◽  
Yakasai H.M. ◽  
...  
Keyword(s):  
Normal Control ◽  
Leaf Extract ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Significant Inhibition ◽  
Alpha Amylase ◽  
Gymnema Sylvestre ◽  
Total Flavonoids Content

Some medicinal plants and their purified derivatives have demonstrated beneficial therapeutic potentials for many centuries. They have been reported to exhibit antioxidant activity, reducing the oxidative stress in cells and are therefore useful in the treatment of many human diseases, including diabetes and other non-communicable diseases. This study evaluated antioxidative activity and enzymatic (alpha-amylase and alphaglucosidase) inhibitory potentials of Gymnema sylvestre methanolic leaf extract (GSMLE) using standard methods. Phytochemical screening revealed the presence of alkaloids, tannins, saponins, steroids, terpenoids and flavonoids. The total phenolics and total flavonoids content in the extract were found to be 6.629±0.745 (µg/ml of catechol equivalent) and 0.004±0.0012 (µg/ml of quercetin equivalent) respectively. GSMLE was shown to have radical scavenging activity against DPPH (290.54 ± 39.72 %), hydroxyl radical (86.507 ± 23.55 %) and hydrogen peroxide (45.25 ± 25.23 %). The level of SOD was significantly decreased in H2O2 induced and H2O2+extract induced when compared with normal control (p<0.05); the level of GSH was significantly increased in H2O2 induced control and significantly decreased in H2O2+extract induced test when compared to normal control. GSH was also decreased significantly in H2O2+extract induced when compared to H2O2 induced control (p<0.05). The extract also demonstrated significant inhibition of alpha-glucosidase (IC50 182.26 ±1.05μg/ml) when compared with standard acarbose (IC50 189.52±0.46) and was more potent than the arcarbose on alpha-amylase inhibition with IC50 of 195.3±4.40 and 200.05±7.16 respectively. These findings may therefore, stress the potentiality of using Gymnema sylvestre as a natural remedy for the management of type 2 diabetes.

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