Natural products as alpha-amylase and alpha-glucosidase inhibitors and their hypoglycaemic potential in the treatment of diabetes: an update (original) (raw)
Related papers
2017
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,...
α-glucosidase inhibitors from plants: A natural approach to treat diabetes
Pharmacognosy Reviews, 2011
Diabetes is a common metabolic disease characterized by abnormally high plasma glucose levels, leading to major complications, such as diabetic neuropathy, retinopathy, and cardiovascular diseases. One of the effective managements of diabetes mellitus, in particular, non-insulin-dependent diabetes mellitus (NIDDM) to decrease postprandial hyperglycemia, is to retard the absorption of glucose by inhibition of carbohydrate hydrolyzing enzymes, such as α-glucosidase and α-amylase, in the digestive organs. α-Glucosidase is the key enzyme catalyzing the final step in the digestive process of carbohydrates. Hence, α-glucosidase inhibitors can retard the liberation of d-glucose from dietary complex carbohydrates and delay glucose absorption, resulting in reduced postprandial plasma glucose levels and suppression of postprandial hyperglycemia. In recent years, many efforts have been made to identify effective α-glucosidase inhibitors from natural sources in order to develop a physiologic functional food or lead compounds for use against diabetes. Many α-glucosidase inhibitors that are phytoconstituents, such as flavonoids, alkaloids, terpenoids,anthocyanins, glycosides, phenolic compounds, and so on, have been isolated from plants. In the present review, we focus on the constituents isolated from different plants having α-glucosidase inhibitory potency along with IC50 values.
Phytochemistry Reviews
Diabetes mellitus is a multifactorial global health disorder that is rising at an alarming rate. Cardiovascular diseases, kidney damage and neuropathy are the main cause of high mortality rates among individuals with diabetes. One effective therapeutic approach for controlling hyperglycemia associated with type-2 diabetes is to target alpha-amylase and alpha-glucosidase, enzymes that catalyzes starch hydrolysis in the intestine. At present, approved inhibitors for these enzymes are restricted to acarbose, miglitol and voglibose. Although these inhibitors retard glucose absorption, undesirable gastrointestinal side effects impede their application. Therefore, research efforts continue to seek novel inhibitors with improved efficacy and minimal side effects. Natural products of plant origin have been a valuable source of therapeutic agents with lesser toxicity and side effects. The anti-diabetic potential through alpha-glucosidase inhibition of plant-derived molecules are summarized in this review. Eight molecules (Taxumariene F, Akebonoic acid, Morusin, Rhaponticin, Procyanidin A2, Alaternin, Mulberrofuran K and Psoralidin) were selected as promising drug candidates and their pharmacokinetic properties and toxicity were discussed where available.
Kumar V and Prakash O, α-Glucosidase inhibitors from plants: A natural approach to treat diabetes
Pharmacognosy Reviews
Diabetes is a common metabolic disease characterized by abnormally high plasma glucose levels, leading to major complications, such as diabetic neuropathy, retinopathy, and cardiovascular diseases. One of the effective managements of diabetes mellitus, in particular, non-insulin-dependent diabetes mellitus (NIDDM) to decrease postprandial hyperglycemia, is to retard the absorption of glucose by inhibition of carbohydrate hydrolyzing enzymes, such as α-glucosidase and α-amylase, in the digestive organs. α-Glucosidase is the key enzyme catalyzing the final step in the digestive process of carbohydrates. Hence, α-glucosidase inhibitors can retard the liberation of d-glucose from dietary complex carbohydrates and delay glucose absorption, resulting in reduced postprandial plasma glucose levels and suppression of postprandial hyperglycemia. In recent years, many efforts have been made to identify effective α-glucosidase inhibitors from natural sources in order to develop a physiologic functional food or lead compounds for use against diabetes. Many α-glucosidase inhibitors that are phytoconstituents, such as flavonoids, alkaloids, terpenoids,anthocyanins, glycosides, phenolic compounds, and so on, have been isolated from plants. In the present review, we focus on the constituents isolated from different plants having α-glucosidase inhibitory potency along with IC50 values.
Clinical Phytoscience
Background α-Amylase catalyses the hydrolysis of starch and ultimately producing glucose. Controlling the catalytic activity of this enzyme reduces glucose production in the postprandial stage, which could be a therapeutic benefit for people with diabetes. This study was conducted to evaluate α-amylase inhibition for utilizing the crude extracts of some medicinal plants traditionally used in Nepal for the treatment of diabetes and its related complications. Methods Microtiter plate approach has been used to assess inhibitory activities of in vitro α-amylase of methanolic extracts of thirty-two medicinal plants. A starch tolerance test was used in rats to investigate the in vivo study of the methanolic extract concerning glibenclamide as the positive control. Results Acacia catechu, Dioscorea bulbifera, and Swertia chirata exhibited inhibitory activity against α-amylase and with IC50 values; 49.9, 296.1, and 413.5 μg/mL, respectively. Kinetics study revealed that all the extracts dis...
Journal of Medicinal Plants Research, 2013
In the present study various extracts of ten medicinal plants, collected in Iran, were examined for αglucosidase and α-amylase inhibition using an in vitro model. Also total phenol content and antioxidant activity of the extracts were investigated. Various extracts of the plants (Cinnamomum zeylanicum, Crataegus oxyacantha, Hibiscus sabdariffa, Morus alba, Portulaca oleracea, Rubus fruticosus, Syzygium aromaticum, Teucrium polium, Trigonella foenum-graecum, and Vaccinium arctostaphylos) were prepared using n-hexane, dichloromethane, chloroform, ethyl acetate and methanol. Methanol, dichloromethane and n-hexane extracts of S. aromaticum exerted high in vitro inhibitory potential against α-glucosidase and α-amylase with IC 50 ranging from 0.3 to 1.1 and 36.2 to 41.9 µg/ml, respectively. The mentioned extracts possessed the highest total phenolic contents (139.8, 119.6 and 136.1 mg GAE/g of extract). The antioxidant activities of the extracts, measured in terms of IC 50 values were 2.2, 3.9 and 0.7 µg/ml, respectively. C. zeylanicum was another traditionally used medicinal plant, which its extracts exhibited high hypoglycaemic effect by inhibition of α-glucosidase and α-amylase (IC 50 ranged from 0.5 to 8.7 and 37.1 to 52.5 µg/ml, respectively). The obtained results support the traditionally use of a number of the analyzed species.
Journal of medicinal plant research
In the present study various extracts of ten medicinal plants, collected in Iran, were examined for α-glucosidase and α-amylase inhibition using an in vitro model. Also total phenol content and antioxidant activity of the extracts were investigated. Various extracts of the plants (Cinnamomum zeylanicum, Crataegus oxyacantha, Hibiscus sabdariffa, Morus alba, Portulaca oleracea, Rubus fruticosus, Syzygium aromaticum, Teucrium polium, Trigonella foenum-graecum, and Vaccinium arctostaphylos) were prepared using n-hexane, dichloromethane, chloroform, ethyl acetate and methanol. Methanol, dichloromethane and n-hexane extracts of S. aromaticum exerted high in vitro inhibitory potential against α-glucosidase and α-amylase with ranging from 0.3 to 1.1 and 36.2 to 41.9 µg/ml, respectively. The mentioned extracts possessed the highest total phenolic contents (139.8, 119.6 and 136.1 mg GAE/g of extract). The antioxidant activities of the extracts, measured in terms of IC50 values were 2.2, 3.9 ...
2018
-Glucosidase and -amylase inhibitors are used in the treatment of type 2 diabetes mellitus. This study aims to identify the -glucosidase and -amylase inhibitors from twoThai folk anti-diabetes formularies including Mor Phon's recipe and the recipe of Wang Nam Yen hospital. Furthermore folk medicinal formulas from MorPhon's recipe were also assessed. The results indicated five plants whose ethanolic extracts exhibited highest -glucosidase inhibitory activity were Salacia chinensis, Vitex glabrata,
Antidiabetic Indian plants: a good source of potent amylase inhibitors
Evidence-Based …, 2008
Diabetes is known as a multifactorial disease. The treatment of diabetes (Type II) is complicated due to the inherent pathophysiological factors related to this disease. One of the complications of diabetes is post-prandial hyperglycemia (PPHG). Glucosidase inhibitors, particularly α-amylase inhibitors are a class of compounds that helps in managing PPHG. Six ethnobotanically known plants having antidiabetic property namely, Azadirachta indica Adr. Juss.; Murraya koenigii (L.) Sprengel; Ocimum tenuflorum (L.) (syn: Sanctum); Syzygium cumini (L.) Skeels (syn: Eugenia jambolana); Linum usitatissimum (L.) and Bougainvillea spectabilis were tested for their ability to inhibit glucosidase activity. The chloroform, methanol and aqueous extracts were prepared sequentially from either leaves or seeds of these plants. It was observed that the chloroform extract of O. tenuflorum; B. spectabilis; M. koenigii and S. cumini have significant α-amylase inhibitory property. Plants extracts were further tested against murine pancreatic, liver and small intestinal crude enzyme preparations for glucosidase inhibitory activity. The three extracts of O. tenuflorum and chloroform extract of M. koenigi showed good inhibition of murine pancreatic and intestinal glucosidases as compared with acarbose, a known glucosidase inhibitor.