Antidiabetic activity, alpha-amylase, and alpha-glucosidase inhibitory effect of Tradescantia spathacea Swartz extract

Tradescantia spathacea Swartz belongs to the genus Commelinaceae, a tropical tree used in many countries as an herbal drug for the care of diabetic patients. The aim of this study was to examine anti-diabetic activity of the Tradescantia spathacea Swartz methanolic extract (METSW) and the in-vitro activity of α-amylase, and α-glucosidase was carried out. METSW compared with acarbose inhibition of the α-amylase and α-glucosidase enzyme, METSW exhibited IC50 less than 100μg/mL would be considered as healthy. The METSW showed IC50 66.22 ± 0.52μg/mL α-amylase activity, acarbose revealed an IC50 of 83.25 ± 1.28μg/mL. METSW demonstrated IC50 levels of 85.37 ± 0.72 μg/mL (y= 0.095x+41.89) inhibition of the α-Glucosidase enzymes. METSW at 400 mg/kg greatly decreased the region under the blood glucose level curve in a typical rat test for oral glucose tolerance. The single dose of the extract decreased dramatically from 211 mg/dl to 89.22 mg/dl at 400 mg/kg METSW in the alloxan induced diabetic model. METSW possesses strong antidiabetic activity in vivo and in vitro. Besides, the extract has also been shown to have a significant inhibitory activity of α-amylase and α-glucosidase which may lead to its anti-hyperglycemic function when used in diabetic patients.

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Assessment of In Vitro Antidiabetic Potential of Purified Anthocyanin Extract from Floral Petals of Wild Balsam Species

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v10i3.4050 ◽

2020 ◽

Vol 10 (3) ◽

pp. 31-35

Author(s):

R ARATHY ◽

K MURUGAN ◽

KV DINESH BABU ◽

GS MANOJ

Keyword(s):

International Diabetes Federation ◽

Inhibitory Effect ◽

Alpha Amylase ◽

Herbal Remedies ◽

Antidiabetic Activity ◽

Public Health Issue ◽

Impatiens Balsamina ◽

Alpha Glucosidase

Diabetes is a notorious and growing clinical and public health issue. The International Diabetes Federation assumes that 592 million had diabetes by 2035 and that by 2040 the number will increase to 642 million. Cardiovascular corollary accounts for four million deaths annually attributable to diabetes. Evidence reveals that certain glucose-lowering phytochemicals can improve vascular outcomes with type 2 diabetes, which, together with better understanding of using multiple therapies concurrently, offers opportunities for beneficial personalization of medication regimens. Anthocyanins are coloured pigments and are natural antioxidants. Keeping this in focus, this study was undertaken to evaluate the in vitro antidiabetic activity in the petals of wild Impatiens balsamina L. The anthocyanin was extracted from floral petals of wild balsam species and purified to homogeneity using chromatographic techniques. Evaluation of in vitro antidiabetic properties of anthocyanin extract revealed a dose-dependent increase in the inhibitory effect on the alpha-glucosidase (200 μg/ml) and alpha-amylase enzymes (500 μg/ml) and was comparable with the standard acarbose drug (189 μg/ml and 50 μg/ml). These results indicated that anthocyanin could be used as a source of functional food and nutraceuticals. This information from wild species will be useful in finding more potent antidiabetic principle from the natural resources for the clinical development of antidiabetic therapeutics. Future studies are planned to substantiate the antidiabetic power of anthocyanin using in vivo animal models. Keywords: Alpha amylase, alpha glucosidase, diabetes, herbal remedies, Impatiens balsamina L.

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Preliminary Analysis of the Antidiabetic Activity of Indonesian Polyherbal Formulation

Journal of Natural Remedies ◽

10.18311/jnr/2021/25960 ◽

2021 ◽

Vol 21 (3) ◽

pp. 219

Author(s):

Syamsudin Abdillah ◽

Apriala Gita Lestari ◽

Priskila Monika ◽

Wahono Sumaryono ◽

Kartiningsih Hisyam

Keyword(s):

Stevia Rebaudiana ◽

Inhibitory Effect ◽

Antidiabetic Activity ◽

Smallanthus Sonchifolius ◽

Polyherbal Formulation ◽

Diabetes In Mice ◽

Ethanol Extracts ◽

Alpha Glucosidase

This study aims to prepare polyherbal formulations and also analyze the antidiabetic potentials of the prepared polyherbal in animals. The ethanol extracts of the leaves of Smallanthus sonchifolius, Stevia rebaudiana, Syzygium polyanthum, and Camellia sinensis were used in this study. The extracts of the aforementioned plants were prepared in the ratio of 2:1:1:1. The formulation was tested for antidiabetic activity in vitro through the inhibition of alpha-glucosidase and in vivo using alloxan-induced diabetes in mice. The polyherbal has an inhibitory effect with the IC50 value of 26.23 μg/mL compared to acarbose (control) was 17.02 μg/mL. The diabetic animals were observed to show an obvious decline in glucose level when compared with control (P< 0.001) after treatment.

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Inhibition of α-Glucosidase, Intestinal Glucose Absorption, and Antidiabetic Properties by Caralluma europaea

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2018/9589472 ◽

2018 ◽

Vol 2018 ◽

pp. 1-8 ◽

Cited By ~ 5

Author(s):

Hayat Ouassou ◽

Touda Zahidi ◽

Saliha Bouknana ◽

Mohamed Bouhrim ◽

Hassane Mekhfi ◽

...

Keyword(s):

Ethyl Acetate Fraction ◽

Inhibitory Effect ◽

Tolerance Test ◽

Glucose Absorption ◽

Significant Inhibition ◽

Oral Glucose ◽

Glucosidase Activity ◽

Intestinal Glucose Absorption

Many medicinal plants around the world are used for therapeutic purposes against several diseases, including diabetes mellitus. Due to their composition of natural substances that are effective and do not represent side effects for users, unlike synthetic drugs, in this study, we investigated the inhibitory effect of Caralluma europaea (CE) on α-glucosidase activity in vitro; then the kinetics of the enzyme were studied with increasing concentrations of sucrose in order to determine the inhibition type of the enzyme. In addition, this effect of Caralluma europaea (CE) was confirmed in vivo using rats as an experimental animal model. Among the five fractions of CE, only the ethyl acetate fraction of C. europaea (EACe) induced a significant inhibition of α-glucosidase and its inhibition mode was competitive. The in vivo studies were conducted on mice and rats using glucose and sucrose as a substrate, respectively, to determine the oral glucose tolerance test (OGTT). The results obtained showed that the EACe and the aqueous extract of C. europaea (AECe) have significantly reduced the postprandial hyperglycemia after sucrose and glucose loading in normal and diabetic rats. AECe, also, significantly decreased intestinal glucose absorption, in situ. The results obtained showed that Caralluma europaea has a significant antihyperglycemic activity, which could be due to the inhibition of α-glucosidase activity and enteric absorption of glucose.

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Morphometric Measurements to Quantify the Cerulein Induced Hyperstimulatory Pancreatitis of Rats under the Protective Effect of Lectins

Analytical Cellular Pathology ◽

10.1155/1998/618913 ◽

1998 ◽

Vol 17 (4) ◽

pp. 219-230 ◽

Cited By ~ 6

Author(s):

Ludwig Jonas ◽

Ulrike Mikkat ◽

Anke Witte ◽

Uta Beckmann ◽

Katrin Dölker ◽

...

Keyword(s):

Protective Effect ◽

Amylase Activity ◽

Acinar Cells ◽

Inhibitory Effect ◽

Pancreatic Acinar Cells ◽

Amylase Secretion ◽

Ulex Europaeus ◽

Serum Amylase Activity

In preceding papers we demonstrated an inhibitory effect of wheat germ agglutinin (WGA) and Ulex europaeus agglutinin (UEA) on the cholecystokinin (CCK) binding to the CCK receptor of rat pancreatic cells and also on the CCK induced Ca2+release and α-amylase secretionin vitroas well as on pancreatic secretion of intact ratsin vivo. In the present study we show the same inhibitory effect of both lectins on the cerulein pancreatitis of rats. This acute pancreatitis was induced by supramaximal injections (5 µg/kg/h iv or 10 µg/kg/h ip) of the CCK analogue cerulein in rats every hour. To monitor the degree of pancreatitis, we measured the number and diameter of injury vacuoles in the pancreatic acinar cells as one of the most important signs of this type of pancreatitis by light microscopic morphometry with two different systems on paraffin sections. Furthermore, the serum α-amylase activity was measured biochemically. We found a correlation between the diameter of vacuoles inside the acinar cells and the serum enzyme activity up to 24 h. The simultaneous ip administration of cerulein and WGA or UEA in a dosage of 125 µg/kg/h for 8 h led to a reduction of vacuolar diameter from 13.1 ± 2.0 µm (cerulein) to 7.5 ± 1.1 µm (cerulein + WGA) or 7.2 ± 1.3 µm (cerulein + UEA). The serum amylase activity was reduced from 63.7 ± 15.8 mmol/l \times min (cerulein) to 37.7 ± 11.8 (cerulein + WGA) or 39.4; +52.9; -31.1 (cerulein + UEA-I). Both parameters allow the grading this special type of pancreatitis to demonstrate the protective effect of the lectins.

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Bronchodilatory effect of Myxopyrum serratulum in animal model

Bangladesh Journal of Pharmacology ◽

10.3329/bjp.v12i1.30257 ◽

2017 ◽

Vol 12 (1) ◽

pp. 84

Author(s):

Vijayalakshmi Maruthamuthu ◽

Ruckmani Kandasamy

Keyword(s):

Guinea Pig ◽

Methanolic Extract ◽

Relaxation Effect ◽

Inhibitory Effect ◽

Chlorpheniramine Maleate ◽

Relaxant Effect ◽

Significant Inhibitory Effect ◽

Guinea Pig Model

The plant Myxopyrum serratulum is traditionally claimed to relieve asthma and cough. The present study was undertaken to evaluate the bronchodilatory effect of the methanolic extract of M. serratulum on histamine-induced bronchospasm by in vivo and the inhibitory effect of the extract on histamine-contracted tracheal chain and ileum by in vitro guinea pig model. Additionally, the relaxant effect of four cumulative concentrations of the extract (0.25, 0.5, 0.7 and 1.0 g%) was assessed using precontracted tracheal chain under different conditions. The extract (400 mg/kg) prolonged the preconvulsive time to 102.3 ± 3.8 sec when compared to saline and standard chlorpheniramine maleate as 121.3 ± 4.5 sec (p<0.05). The extract also possessed significant inhibitory effect on histamine-contracted guinea pig ileum and tracheal chain and also exhibited significant relaxation effect on precontracted tracheal chain of guinea pig models contracted by 60 mM KCl (p<0.001) and 10 µM methacholine (p<0.001) when compared with standard theophylline.

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In vitro, acute and subchronic evaluation of the antidiabetic activity of Atractylis flava Desf n-butanol extract in alloxan-diabetic rats

Future Journal of Pharmaceutical Sciences ◽

10.1186/s43094-021-00358-5 ◽

2021 ◽

Vol 7 (1) ◽

Author(s):

Mohamed Akram Melakhessou ◽

Salah Eddine Marref ◽

Naima Benkiki ◽

Cherine Marref ◽

Imene Becheker ◽

...

Keyword(s):

Blood Glucose ◽

Plant Extract ◽

Fasting Blood Glucose ◽

Folk Medicine ◽

Diabetic Rats ◽

Antidiabetic Activity ◽

Oral Glucose ◽

Butanol Extract

Abstract Background Diabetes mellitus is a serious complex multifactorial disorder that imposes huge health and economic burden on societies. Because the currently available medications have many drawbacks, it's important to look for alternative therapies. Medicinal plants utilized in folk medicine are ideal candidates. Therefore, this work assessed the antidiabetic action of n-butanol extract from the whole plant Atractylis flava Desf (BEAF). These ethnomedicinal properties of BEAF were scientifically validated using in vitro and in vivo assays. In vitro antidiabetic effect of the BEAF was conducted using α-Glucosidase and α-Amylase assays. While the antihyperglycemic activity was assessed using two rat models: Alloxan-induced diabetic rats and oral glucose challenged rats. Experimental diabetes was induced by a single intraperitoneal injection of alloxan at a dose of 150 mg/kg and animals with fasting blood glucose levels (BGL) > 200 mg/dL were considered diabetic. Glibenclamide (5 mg/kg) was used as a typical drug. Results The BEAF at all tested dose levels (100, 250, and 500 mg/kg) showed a significant decrease in blood glucose level in all the two animal models. Besides, the plant extract exhibited a potent inhibitory effect on α-Amylase and α-Glucosidase activity at a concentration of 1000 µg/mL with 76.17% and 89.37%, respectively. Conclusion BEAF exerts in vitro and in vivo antidiabetic effects, these results suggest that the plant extract can be a therapeutic resource in the treatment of diabetes and hyperlipidemia.

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Polyalthia Clerodane Diterpene Potentiates Hypoglycemia via Inhibition of Dipeptidyl Peptidase 4

International Journal of Molecular Sciences ◽

10.3390/ijms20030530 ◽

2019 ◽

Vol 20 (3) ◽

pp. 530 ◽

Cited By ~ 1

Author(s):

Po-Kai Huang ◽

Shian-Ren Lin ◽

Jirawat Riyaphan ◽

Yaw-Syan Fu ◽

Ching-Feng Weng

Keyword(s):

Single Dose ◽

Natural Compounds ◽

Dipeptidyl Peptidase ◽

Antidiabetic Activity ◽

Drug Candidate ◽

Diabetic Patients ◽

Dose Administration ◽

Dipeptidyl Peptidase 4

Serine protease dipeptidyl peptidase 4 (DPP-4) is involved in self/non-self-recognition and insulin sensitivity. DPP-4 inhibitors are conventional choices for diabetic treatment; however, side effects such as headache, bronchus infection, and nasopharyngitis might affect the daily lives of diabetic patients. Notably, natural compounds are believed to have a similar efficacy with lower adverse effects. This study aimed to validate the DPP-4 inhibitory activity of clerodane diterpene 16-hydroxycleroda-3,13-dien-15,16-olide (HCD) from Polyalthia longifolia, rutin, quercetin, and berberine, previously selected through molecular docking. The inhibitory potency of natural DPP-4 candidates was further determined by enzymatic, in vitro Caco-2, and ERK/PKA activation in myocyte and pancreatic cells. The hypoglycemic efficacy of the natural compounds was consecutively analyzed by single-dose and multiple-dose administration in diet-induced obese diabetic mice. All the natural-compounds could directly inhibit DPP-4 activity in enzymatic assay and Caco-2 inhibition assay, and HCD showed the highest inhibition of the compounds. HCD down-regulated LPS-induced ERK phosphorylation in myocyte but blocked GLP-1 induced PKA expression. For in vivo tests, HCD showed hypoglycemic efficacy only in single-dose administration. After 28-days administration, HCD exhibited hypolipidemic and hepatoprotective efficacy. These results revealed that HCD performed potential antidiabetic activity via inhibition of single-dose and long-term administrations, and could be a new prospective anti-diabetic drug candidate.

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Evaluation of Aqueous Extract of Alphonsea sclerocarpa for in vivo and in vitro Antidiabetic Potentials in Wistar Rats

International Journal of Pharmaceutical Sciences Review and Research ◽

10.47583/ijpsrr.2021.v70i02.029 ◽

2021 ◽

Vol 70 (2) ◽

Author(s):

Ravi Shankar N ◽

Ram Kishore ◽

Puranik SB

Keyword(s):

Blood Glucose ◽

Glucose Uptake ◽

Aqueous Extract ◽

Insulin Level ◽

Antidiabetic Activity ◽

Albino Rats ◽

Oral Glucose ◽

In Vivo Evaluation

The purpose of current investigation was to investigate in vivo and in vitro anti-diabetic potentials of aqueous extract of Alphonsea sclerocarpa leaves against alloxan induced diabetes in albino rats. Two in vivo and one in vitro methods were performed for the evaluation of aqueous extract for antidiabetic activity. For in-vivo evaluation, diabetes was induced in albino rats by administering a single dose of alloxan. The study was designed to test the acute effect of aqueous extract of Alphonsea sclerocarpa (AEAS) to reduce blood glucose in OGTT. The chronic study of 21 days was performed against diabetic rats and blood glucose was determined at 1st , 7 th, 14th and 21st day. In chronic in vivo study, serum parameters insulin, urea, creatinine, total cholesterol, triglycerides, ALT and AST were also estimated at 21st day to determine the effects of aqueous and aqueous extracts on complications of diabetes mellitus. Glucose uptake by hemidiaphragm assay was performed to test the ability of extract to utilize glucose. In Oral Glucose Tolerance Test, standard glibenclamide and aqueous extract (200mg/kg and 400mg/kg) treated animals have shown significant reduction in blood glucose at 90 mins but at 120 mins. In chronic model the aqueous extract effectively reduced blood glucose levels (P<0.001) at 14th and 21st day of study in therapeutic groups and effect was comparable to that of standard. The extract could also significantly (P<0.001) reduce concentrations of SGOT, triglycerides, cholesterol and urea in serum and significantly (P<0.001) increased the insulin level in blood which proves beneficial effects of the extract in diabetes. The change in concentrations of SGPT and urea were less significant (P>0.01). The presence of extract in glucose uptake assay could significantly increase utilization of the glucose by rat hemidiaphragm. The aqueous extract of Alphonsea sclerocarpa possess significant antidiabetic properties against alloxan induced diabetic animals.

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Phytochemical Screening, Invitro antidiabetic activity of Muntingia calabura leaves extract on alpha-amylase and alpha-glucosidase enzymes

International Journal of Research in Pharmaceutical Sciences ◽

10.26452/ijrps.v11i1.1960 ◽

2020 ◽

Vol 11 (1) ◽

pp. 1210-1213

Author(s):

Panneerselvam G ◽

Jothi Narendiran N ◽

Vasanth S ◽

Bupesh G ◽

Prabhu K ◽

...

Keyword(s):

Methanolic Extract ◽

Antidiabetic Activity ◽

Phytochemical Screening ◽

Pharmacological Activities ◽

Standard Methods ◽

Inhibition Studies ◽

Chloroform Methanol ◽

Alpha Glucosidase ◽

Muntingia Calabura

Muntingia calabura is a medicinal plant broadly used in conventional therapeutic preparation of many pharmacological activities. In the present study, the Invitro antidiabetic property of Muntingia calabura leaves extracts was analyzed by using standard methods. An in vitro anti-diabetic study was done by inhibition of α-amylase and α - glucosidase enzymes. The phytochemical screening of Muntingia Calabura leaves revealed that the extract is rich in the secondary metabolites such as alkaloids, polyphenols and tannins. The in vitro antidiabetic capability of extracts such as Petroleum ether, Chloroform, Methanol and aqueous through α- amylase enzyme and alpha-glucosidase enzyme inhibition studies. The results of the present study concluded that the methanolic extract of Muntingia calabura exhibits 80% in α-amylase and 60% in alpha-glucosidase activity while compared to acarbose. The phytochemistry study portrays the antidiabetic activity of Muntingia calabura is due to the presence of polyphenols.

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Antidiabetic Activity ofRuellia tuberosaL., Role ofα-Amylase Inhibitor:In Silico,In Vitro, andIn VivoApproaches

Biochemistry Research International ◽

10.1155/2015/349261 ◽

2015 ◽

Vol 2015 ◽

pp. 1-9 ◽

Cited By ~ 7

Author(s):

Dyah Ratna Wulan ◽

Edi Priyo Utomo ◽

Chanif Mahdi

Keyword(s):

Single Dose ◽

In Silico ◽

Amylase Activity ◽

Alternative Therapy ◽

Antidiabetic Activity ◽

Diabetic Rat ◽

Control Group ◽

Folk Remedy

Ruellia tuberosaL. is a folk remedy in the treatment of diabetes mellitus. However, its hypoglycemic activity has not been investigated so far. In the present study, the antidiabetic mechanism of the n-hexane fraction of methanolic extract (HFME) of this plant was investigatedin silico,in vitro, andin vivo.In silicostudy was performed using AutoDock4.2 software.In vitro α-amylase inhibitory activity was investigated by starch-iodine method. A single dose of 450 mg/kg HFME for 14 days was subjected to an antidiabetic screeningin vivoby a multiple low dose streptozotocin (MLD-STZ) induced rats. Molecular modeling results show that Betulin exhibited noncompetitiveα-amylase inhibitory activities. The effect of HFME elicited significant reductions of diabetic rat blood glucose. A single dose administration of HFME inhibitedα-amylase activityin vivo(P<0.01) compared to a diabetic control group. Moreover, this extract strongly inhibited theα-amylase activityin vitro(IC500.14 ± 0.005 mg/mL). It is concluded that HFME exerted an antidiabetic effect viaα-amylase inhibitor. Our findings provide a possible hypoglycemic action ofR. tuberosaL. as an alternative therapy in the management of diabetes.

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