BackgroundThe fruit of Elaeagnus umbellata has high medicinal values and is an excellent source of phytochemicals. This study was aimed to evaluate the antioxidant, enzyme inhibitory and antidiabetic potential of Elaeagnus umbellata.MethodsThe antioxidant potential of the crude extract and subfractions of E. umbellata fruit were determined using DPPH (2, 20-diphenyl-1-picrylhydrazyl) and ABTS (2, 2′-azinobis-3-ethylbenzothiazoline-6-sulfonic acid) assays. The enzyme inhibitory potentials of extracts against α-amylase and α-glucosidase enzymes were also determined. The in vivo anti-hyperglycemic effects of the extract in STZ-induced type 2 diabetes were determined using Sprague Dawley adult rats. HPLC system (Agilent 1260) was used for the identification of bioactive compounds present in extracts. Molecular docking was used to identify and compare the interaction between the compounds (active constituents) and standard inhibitor acarbose with the α-amylase and α-glucosidase active sites.ResultsThe chloroform, ethyl acetate, and butanol fractions showed significant antioxidant potential with IC50 values of 40, 45 and 60 μg/mL against DPPH and 57, 70 and 120 μg/mL against ABTS free radicals respectively. The chloroform and ethyl acetate were highly active against α-amylase and α-glucosidase (IC50 values 58 and 200 μg/ml against α-amylase 60 and 140 μg/ml against α-glucosidase. The crude extract, chloroform, and ethyl acetate fractions were more potent in controlling the hyperglycemia in STZ-induced type 2 diabetes in rats and considerable reduction of glucose level was observed compared to the non-treated group. Furthermore, the extracts were also found useful in controlling the secondary complications associated with type 2 diabetes mellitus which was evident from the observed substantial reduction in the blood level of serum glutamate oxaloacetate transaminase, serum glutamate pyruvate transaminase, alkaline phosphatase, total cholesterol, low-density lipoproteins, and triglycerides. The molecular docking approach indicated the favorable inhibitory interaction between the docked compounds and the active sites of the α-amylase and α-glucosidase. All docked compounds occupied the same binding site as occupied by acarbose.ConclusionIt was concluded that E. umbellata can be used in the treatment of type 2 diabetes and oxidative stress. The extracts were also found to be effective in relieving the secondary complications associated with type 2 diabetes.Graphical abstract Electronic supplementary materialThe online version of this article (10.1186/s12906-018-2381-8) contains supplementary material, which is available to authorized users.
This study reports pharmacological and physiological effects of cis-and trans-(3-aminocyclopentanyl)butylphosphinic acid . These compounds are conformationally restricted analogs of the orally active GABA B/C receptor antagonist (3-aminopropyl)-n-butylphosphinic acid (CGP36742 or SGS742). cis- [IC 50 (1) ϭ 5.06 M and IC 50 (2) ϭ 11.08 M; n ϭ 4] and trans-3-ACPMPA [IC 50 (1) ϭ 72.58 M and IC 50 (2) ϭ 189.7 M; n ϭ 4] seem competitive at GABA C receptors expressed in Xenopus laevis oocytes, having no effect as agonists (1 mM) but exerting weak antagonist (1 mM) effects on human GABA A and GABA B receptors. cis-3-ACPBPA was more potent and selective than the trans-compound, being more than 100 times more potent at GABA C than GABA A or GABA B receptors. cis-3-ACPBPA was further evaluated on dissociated rat retinal bipolar cells and dose-dependently inhibited the native GABA C receptor (IC 50 ϭ 47 Ϯ 4.5 M; n ϭ 6). When applied to the eye as intravitreal injections, cis-and trans-3-ACPBPA prevented experimental myopia development and inhibited the associated vitreous chamber elongation, in a dose-dependent manner in the chick model. Doses only 10 times greater than required to inhibit recombinant GABA C receptors caused the antimyopia effects. Using intraperitoneal administration, cis-(30 mg/ kg) and trans-3-ACPBPA (100 mg/kg) enhanced learning and memory in male Wistar rats; compared with vehicle there was a significant reduction in time for rats to find the platform in the Morris water maze task (p Ͻ 0.05; n ϭ 10). As the physiological effects of cis-and trans-3-ACPBPA are similar to those reported for CGP36742, the memory and refractive effects of CGP36742 may be due in part to its GABA C activity.GABA is an abundant neurotransmitter that mediates inhibition throughout the retina and central nervous system. Three main classes of GABA receptors exist and are termed GABA A , GABA B , and GABA C receptors (Bormann, 2000;Chebib and Johnston, 2000). The GABA A and GABA C are ionotropic receptors, belonging to the Cys-loop family of ligand-gated ion channels, which includes nicotinic acetylcholine, strychnine-sensitive glycine, serotonin type 3, and some invertebrate anionic glutamate receptors (Bormann, 2000;Chebib and Johnston, 2000). Both GABA A and GABA C receptors are chloride channels that mediate fast synaptic inhibition when activated by GABA. In contrast, GABA B receptors are members of the metabotropic receptor family; these receptors couple via G proteins (G i/o ) to interact with neuronal inwardly rectifying potassium and voltage-gated calcium channels, mediating slow synaptic inhibition by increasing ABBREVIATIONS: TPMPA, (1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid; 3-APMPA, (3-aminopropyl)-methylphosphinic acid; cis-and trans-3-ACPMPA, cis-and trans-(3-aminocyclopentanyl)methylphosphinic acid; cis-and trans-3-ACPBPA, cis-and trans-(3-aminocyclopentanyl)butylphosphinic acid; CGP36742 or SGS742, (3-aminopropyl)-n-butylphosphinic acid; GIRK, G protein-coupled inwardly rectifying potassium ...
We modelled the N-terminal ligand-binding domain of the rho1 GABA(C) receptor based on the Lymnaea stagnalis acetylcholine-binding protein (L-AChBP) crystal structure using comparative modelling and validated using flexible docking guided by known mutagenesis studies. A range of known rho1 GABA(C) receptor ligands comprising seven full agonists, 10 partial agonists, 43 antagonists and 12 inactive molecules were used to evaluate and validate the models. Of the 50 models identified, six models that allowed flexible ligand docking in accordance with the experimental data were selected and used to study detailed receptor-ligand interactions. The most refined model to accommodate all known active ligands featured a cavity comprising of a volume of 488 A(3). A detailed analysis of the interaction between the rho1 GABA(C) receptor model and the docked ligands revealed possible H-bonds and cation-pi interactions between the different ligands and binding site residues. Based on quantum mechanical/molecular mechanical (QM/MM) calculations, the model showed distinctive conformations of loop C that provided a molecular basis for agonist and antagonist actions. Agonists elicit loop C closure, while a more open loop C was observed upon antagonist binding. The model differentiates the role for key residues known to be involved in either binding and/or gating.
Background:The reporting of the medicinal plants and their traditional uses is important in order to prevent this knowledge from being lost. The aims of this study were to collect information concerning the traditional use of medicinal plants in the region of Tafila; identify the most important medicinal plants; determine the relative importance of the species surveyed; and calculate the informant consensus factor (Fic) in relation to medicinal plant use.Materials and Methods:Data on the traditional medicinal uses of local plants were collected using qualitative tools. The informant consensus factor (Fic) for the category of aliments and the use value (UV) of the plant species were calculated.Results and Conclusions:The survey revealed that 41 plant species are still in use in Tafila for the treatments of various diseases. Problems of the digestive system had the highest Fic values, while Allium cepa L. and Matricaria aurea (Loefl.) Sch. Bip. scored the highest UV.SUMMARY The medicinal plants used by local people of the Tafila area of Jordan their traditional uses were investigated. forty one plant species are still in use in Tafila for the traditional treatment of various diseases. The preservation of this knowledge is important not only for maintaining cultural and traditional resources but also as a resource for the future identification of leads for drug development. The use of Fic and the UV to identify plant species that are consistently used in the treatment of specific ailments assists in narrowing down the search for new effective plant-derived medicines and in validating the use of traditional medicines. Data on the traditional medicinal uses of local plants was collected using qualitative tools. The informant consensus factor (Fic) for category of aliments and the use value (UV) of the plant species were calculated. in the Tafila region, the Fic values are relatively low, indicating a low level of shared knowledge and that a number of different species are used to treat similar disorders. This may be a result of the great diversity of vegetation types found across the Tafila region, with the specific plant chosen being dependent on the species most readily available in the different vegetation zones. Interestingly, however, the UVs calculated for a number of species in the Tafila region are relatively high, compared with those recorded in other areas of Jordan. These high UVs indicate that despite the diversity of vegetation types across the Tafila region, a number of plants are highly valued for medicinal use throughout the whole region. This study contributes to the body of knowledge about the use of plants in traditional medicine, helping to document and maintain the knowledge that has been traditionally passed directly from person to person. The preservation of this knowledge is important not only for maintaining cultural and traditional resources but also as a resource for the future identification of leads for drug development. Problems of the digestive system had the highest Fic values, while Al...
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