Molecules2015, 20(2), 2296-2309; doi:10.3390/molecules20022296 (registering DOI) - published 29 January 2015 Show/Hide Abstract
Abstract: A series of novel dimethoxyindanone embedded spiropyrrolidines were synthesized in ionic liquid, [bmim]Br and were evaluated for their inhibitory activities towards cholinesterases. Among the spiropyrrolidines, compound 4f exhibited the most potent activity with an IC50 value of 1.57 µM against acethylcholinesterase (AChE). Molecular docking simulation for the most active compound was employed with the aim of disclosing its binding mechanism to the active site of AChE receptor.
Molecules2015, 20(2), 2272-2295; doi:10.3390/molecules20022272 (registering DOI) - published 29 January 2015 Show/Hide Abstract
Abstract: Lectins are a group of proteins with carbohydrate recognition activity. Lectins are categorized into many families based on their different cellular locations as well as their specificities for a variety of carbohydrate structures due to the features of their carbohydrate recognition domain (CRD) modules. Many studies have indicated that the direct recognition of particular oligosaccharides on viral components by lectins is important for interactions between hosts and viruses. Herein, we aim to globally review the roles of this recognition by animal lectins in antiviral immune responses and viral pathogenesis. The different classes of mammalian lectins can either recognize carbohydrates to activate host immunity for viral elimination or can exploit those carbohydrates as susceptibility factors to facilitate viral entry, replication or assembly. Additionally, some arthropod C-type lectins were recently identified as key susceptibility factors that directly interact with multiple viruses and then facilitate infection. Summarization of the pleiotropic roles of direct viral recognition by animal lectins will benefit our understanding of host-virus interactions and could provide insight into the role of lectins in antiviral drug and vaccine development.
Molecules2015, 20(2), 2229-2271; doi:10.3390/molecules20022229 (registering DOI) - published 29 January 2015 Show/Hide Abstract
Abstract: Innate recognition of virus proteins is an important component of the immune response to viral pathogens. A component of this immune recognition is the family of lectins; pattern recognition receptors (PRRs) that recognise viral pathogen-associated molecular patterns (PAMPs) including viral glycoproteins. In this review we discuss the contribution of soluble and membrane-associated PRRs to immunity against virus pathogens, and the potential role of these molecules in facilitating virus replication. These processes are illustrated with examples of viruses including human immunodeficiency virus (HIV), hepatitis C virus (HCV) and Ebola virus (EBOV). We focus on the structure, function and genetics of the well-characterised C-type lectin mannose-binding lectin, the ficolins, and the membrane-bound CD209 proteins expressed on dendritic cells. The potential for lectin-based antiviral therapies is also discussed.
Molecules2015, 20(2), 2208-2228; doi:10.3390/molecules20022208 (registering DOI) - published 29 January 2015 Show/Hide Abstract
Abstract: The plant indole alkaloid ibogaine has shown promising anti-addictive properties in animal studies. Ibogaine is also anti-addictive in humans as the drug alleviates drug craving and impedes relapse of drug use. Although not licensed as therapeutic drug and despite safety concerns, ibogaine is currently used as an anti-addiction medication in alternative medicine in dozens of clinics worldwide. In recent years, alarming reports of life-threatening complications and sudden death cases, temporally associated with the administration of ibogaine, have been accumulating. These adverse reactions were hypothesised to be associated with ibogaine’s propensity to induce cardiac arrhythmias. The aim of this review is to recapitulate the current knowledge about ibogaine’s effects on the heart and the cardiovascular system, and to assess the cardiac risks associated with the use of this drug in anti- addiction therapy. The actions of 18-methoxycoronaridine (18-MC), a less toxic ibogaine congener with anti-addictive properties, are also considered.
Molecules2015, 20(2), 2190-2207; doi:10.3390/molecules20022190 (registering DOI) - published 29 January 2015 Show/Hide Abstract
Abstract: Grape pomace seeds and skins from different Mediterranean varieties (Grenache [GRE], Syrah [SYR], Carignan [CAR], Mourvèdre [MOU] and Alicante [ALI]) were extracted using water and water/ethanol 70% in order to develop edible extracts (an aqueous extract [EAQ] and a 70% hydro-alcoholic extract [EA70]) for potential use in nutraceutical or cosmetic formulations. In this study, global content (total polyphenols, total anthocyanins and total tannins), flavan-3-ols and anthocyanins were assessed using HPLC-UV-Fluo-MSn. In addition, extract potential was evaluated by four different assays: Oxygen Radical Absorbance Capacity (ORAC), Ferric Reducing Antioxidant Potential assay (FRAP), Trolox equivalent antioxidant capacity (TEAC) or ABTS assay and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay. As expected, seed pomace extracts contained higher amounts of polyphenols then skin pomace extracts. Indeed, seeds from Syrah contained a particularly important amount of total polyphenols and tannins in both type of extract (up to 215.84 ± 1.47 mg of gallic acid equivalent [GAE]/g dry weight (DW) and 455.42 ± 1.84 mg/g DW, respectively). These extracts also expressed the highest antioxidant potential with every test. For skins, the maximum total phenolic was found in Alicante EAQ (196.71 ± 0.37 mg GAE/g DW) and in Syrah EA70 (224.92 ± 0.18 mg GAE/g DW). Results obtained in this article constitute a useful tool for the pre-selection of grape pomace seed and skin extracts for nutraceutical purposes.
Abstract: In plants, flavonoids play an important role in biological processes. They are involved in UV-scavenging, fertility and disease resistance. Therefore, in this study, we attempted to quantify and characterize phenolic compounds in Aesculus parviflora Walt. leaves and Aesculus glabra leaves partly suffering from attack by a leaf mining insect (C. ohridella). A total of 28 phenolic compounds belonging to the hydroxycinnamic acid, flavan-3-ols and flavonol groups were identified and quantified in Aesculus parviflora and A. glabra leaf extracts. Significantly decreased concentrations of some phenolic compounds, especially of flavan-3-ols, were observed in infected leaves compared to the non-infected ones. Additionally, a higher content of polymeric procyanidins in leaves of Aesculus parviflora than in Aesculus glabra may explain their greater resistance to C. ohridella insects.