Three new α-glucosidase inhibitors from guggul, the oleogum resin of Commiphorawightii (original) (raw)
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Journal of Developing Drugs, 2015
Inhibition of α-glucosiase and the associated reduction of glucose absorption is an attractive approach for decreasing postprandial hyperglycemia and for the discovery of potent antidiabetic agents. One of the most important sources of potential α-glucosiase inhibitors represents the class of polyphenols. This paper aims to evaluate previous herbal polyphenol-rich extracts plan on the management of diabetes mellitus, to address their α-glucosidase inhibitory activity. Polyphenol-rich extracts from thirteen widely used traditionally anti-diabetic plants in Asia and Mediterranean regions were evaluated for their potential α-glucosidase inhibitory activity. Among these evaluated plants, 10 were much stronger than that of acarbose standard. Punica granatum manifested the highest inhibitory activity with IC 50 at 3.59 ± 0.11 µg/mL, followed by Psidium guajava with IC 50 at 8.08 ± 0.10 µg/mL and Cinnamomum zeylanicum with IC 50 at 9.87.08 ± 0.14 µg/mLA. A high correlation (r=0.65, p<0.001) was observed between α-glucosidase inhibition and total phenolic content of all plants. Punica granatum, P. guajava, C. zeylanicum and Ziziphus spina-christi had also the highest total phenolic content. Extracts for the above studied plant species may potentially replace acarbose in its current clinical use in improving post-prandial glycaemic control in type 2 diabetics. As a result, these polyphenol-rich extracts potentially offer a complementary approach to develop functional food and potential antidiabetic agents.
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.
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.
EVALUATION OF SELECTED MEDICINAL HERBS FOR ANTIDIABETIC ACTIVITY VIA ALPHA-GLUCOSIDASE INHIBITION
Literature and native therapies have cited bitter melon, dandelion, blueberry, and roselle, as hypoglycemic agents, however, the exact mechanisms of action are unknown. It was hypothesized that, these agents could induce hypoglycemia, through the mechanism of α-glucosidase inhibition. The aim of the present study was, to examine inhibition of alpha-glucosidase as one of the possible mechanisms of action, of bitter melon (Mormodicacharantia), dandelion (Taraxacumofficinale), blueberry (Vacciniumcorybosum), and roselle (Hibiscus sabdariffa). Each of these agents has been used in the treatment of diabetes in, different parts of the world. The study was done in vitro, using α-glucosidase, obtained from Bacillus. The inhibitory effect of different concentrations of alcoholic extracts of the plants, on α-glucosidase was studied. The extracts of the plant showed inhibitory activities, against α-glucosidase, with IC50 values in a dose dependent manner. The result demonstrated that, bitter melon, roselle, dandelion, and blueberry share similar mechanism of action with Acarbose, which is being used as an antidiabetic agent.
REVIEW ON ROLE OF NATURAL ΑLPHA-GLUCOSIDASE INHIBITORS FOR MANAGEMENT OF DIABETES MELLITUS
International Journal of Biomedical Research, 2011
Diabetes, a state of improperly regulated homeostasis of carbohydrate and lipid metabolism is one of the major killers in recent times. Most prevalent form of diabetes is non insulin dependent diabetes mellitus (NIDDM/type II). Rapid hydrolysis of starch mediated by pancreatic α-amylase and α-glucosidases followed by glucose uptake at intestine results in sudden rise in blood glucose levels, causing hyperglycemia in type II diabetes patients. Alpha-glucosidase inhibitors act as competitive inhibitors of enzymes needed to digest carbohydrates: specifically alpha-glucosidase enzymes in the brush border of the small intestines. Inhibition of these enzyme systems reduces the rate of digestion of carbohydrates. Less glucose is absorbed because the carbohydrates are not broken down into glucose molecules. Natural alpha-glucosidase inhibitors such as Acarbose and Miglitol used for management of diabetes widely, but they are associated with side effects, in this review search for more natural alpha-glucosidase inhibitors are discussed which are safer as compared to insulin and other oral hypoglycaemic drugs.
α-Glucosidase inhibitors from the bark of Mangifera mekongensis
Chemistry Central Journal, 2016
Background: Mangifera mekongensis (Anacardiaceae) is cultivated for its edible fruit and has been used in traditional Vietnamese medicine for its anti-aging properties and for treating diabetes, vermifuge, and dysentery. As part of a search for biologically active compounds with reduction of the rate of glucose absorption, a screening has been initiated to evaluate natural product extracts for the inhibition of enzyme α-glucosidase. A n-hexane extract of the bark of M. mekongensis showed strong α-glucosidase inhibitory activity with IC 50 value of 1.71 µg/mL. Thus, the constituents of this plant were examined. Results: Two new steroids named mekongsterol A (1) and mekongsterol B (2), were isolated from the n-hexane extract of the bark of M. mekongensis (Anacardiaceae), together with seven known compounds (3-9). Their chemical structures were elucidated on the basis of spectroscopic data. All compounds possessed significant α-glucosidase inhibitory activity in a concentration-dependent manner, except for 3 and 4. Compounds 1, 2, 5-9 showed more potent inhibitory activity, with IC 50 values ranging from 1.2 to 112.0 µM, than that of a positive control acarbose (IC 50 , 214.5 µM). Conclusions: These results suggested that the traditional use of the bark of M. mekongensis for the treatment of diabetes diseases in Vietnam may be attributable to the α-glucosidase inhibitory activity of its steroid and cycloartane constituents.
Journal of Medicinal Plants Research, 2009
Gambir (Uncaria gambir) and other plants belonging to the genus Uncaria have been used in traditional medicine in southeastern Asia, Africa and South America and they have been studied widely over the past century. Gambier, the dried leaf extract from gambir is known to have antioxidant properties and some studies have attributed it to the presence of tannins and condensed tannins. The objective of this study was to investigate the potential of commercial gambier on the Indonesian market as a scavenger of reactive free radicals, evaluate its ability to inhibit-glucosidase and determine the bioactive compound responsible for these activities. An ethanolic extract of commercial gambier was extracted with ethyl acetate. The ethanol and ethyl acetate extracts as well as the aqueous extract after ethyl acetate extraction and residue from ethanol extraction were tested for free radical scavenging activity using 2,2-diphenyl-1-picrylhydrazyl (DPPH). They were also tested for-glucosidase inhibitory activity. The extracts were then studied using reverse phase HPLC, LCMS and NMR to identify the bioactive compound. It was observed that all the extracts had high activity for DPPH inhibition but moderate activity for inhibiting-glucosidase in vitro. Apart from the aqueous extract, 92% DPPH inhibition by the extracts was achievable at 30 g/ml. The ethanol and ethyl acetate extracts had significantly higher (p < 0.01) DPPH inhibitory activity than the aqueous extract. IC 50 of the organic extracts and residue ranged between 13.8 to 16.2 g/ml for DPPH inhibition while that of the aqueous extract was 27.4 g/ml. With regards to-glucosidase inhibition, however, IC 50 range of 15.2 and 49.5 g/ml was recorded. Catechin was identified as the major bioactive compound present.
Journal of Herbmed Pharmacology
Introduction: α-Glucosidase is the major enzyme implicated in intestinal glucose absorption, and its inhibition is a target for the management of diabetes mellitus. This study investigated the in vitro α-glucosidase inhibitory activity of extracts from different parts of 20 selected medicinal plants and the potential for plant-part substitution and plant species combinations used by traditional healers to treat diabetes. Methods: Acetone and petroleum ether extracts from different parts of 20 plant species traditionally used to treat diabetes were individually evaluated in vitro using an α-glucosidase assay. The potential for plant-part substitution was investigated by including leaf extracts where non-renewable parts are used traditionally. The extracts of plant species were combined and investigated as used traditionally. Results: Anthocleista grandiflora stem bark acetone, Artabotrys brachypetalus leaf petroleum ether, and Dichrostachys cinerea root petroleum ether extracts exhib...