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- Volume 5, Issue 2, 2010
Recent Patents on CNS Drug Discovery (Discontinued) - Volume 5, Issue 2, 2010
Volume 5, Issue 2, 2010
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Role of Dietary Polyphenols in Attenuating Brain Edema and Cell Swelling in Cerebral Ischemia
Authors: Kiran S. Panickar and Richard A. AndersonPolyphenols are natural substances with variable phenolic structures and are enriched in vegetables, fruits, grains, bark, roots, tea, and wine. There are over 8000 polyphenolic structures identified in plants, but edible plants contain only several hundred polyphenolic structures. Recent interest in polyphenols has increased greatly due to their potential antioxidant effects. In addition, some polyphenols also have insulin-potentiating, anti-inflammatory, anticarcinogenic, anti-viral, anti-ulcer, and anti-apoptotic properties although some of these properties may be a consequence of their anti-oxidant effects. Given that oxidative stress and inflammation are hypothesized to contribute to increased neural damage in ischemia, polyphenols appear to have a tremendous potential in attenuating such injuries. One important consequence of ischemia is brain edema and oxidative stress and inflammation are implicated in its pathogenesis. Brain edema is defined as an abnormal accumulation of fluid in the brain parenchyma resulting in a volumetric enlargement of the cells or tissue and can cause further ischemic damage. The purpose of this article is to review the current literature on brain edema and/or cell swelling in ischemic injury with the goal to identify newer approaches to attenuate brain edema. A review of currently known mechanisms underlying edema/cell swelling will be undertaken and the potential of dietary polyphenols to reduce edema will be critically reviewed with the discussion of some recent patents.
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Incretin Analogues that have been Developed to Treat Type 2 Diabetes Hold Promise as a Novel Treatment Strategy for Alzheimer's Disease
More LessAnalogues of the incretins Glucagon-like peptide 1 (GLP-1) and Glucose-dependent insulinotropic peptide (GIP) have been developed to treat type 2 diabetes mellitus. They are protease resistant and have a longer biological half life than the native peptides. Some of these novel analogues can cross the blood-brain barrier, have neuroprotective effects, activate neuronal stem cells in the brain, and can improve cognition. The receptors for GIP and GLP-1 are expressed in neurons, and both GIP and GLP-1 are expressed and released as transmitters by neurons. GIP analogues such as DAla(2)GIP and GLP-1 analogues such as liraglutide enhance synaptic plasticity in the brain and also reverse the betaamyloid induced impairment of synaptic plasticity. In mouse models of Alzheimer's disease, GLP-1 analogues Val(8)GLP-1 and liraglutide prevent memory impairment and the block of synaptic plasticity in the brain. Since two GLP- 1 analogues exendin-4 (Exenatide, Byetta) and liraglutide (Victoza) are already on the market as treatments for Type 2 diabetes, and others are in late stage clinical trials, these drugs show promise as treatments for neurodegenerative diseases such as Alzheimer's disease. Currently, there are three patents covering native GLP-1 and different GLP-1 analogues and one patent for the use of GIP and different GIP analogues for the treatment of neurodegenerative diseases.
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New Devices for Treating Acute Ischemic Stroke
Authors: Neil Rosenberg, Michael Chen and Shyam PrabhakaranThe past decade has witnessed an explosion of devices available for treating acute ischemic stroke. Here, we review a range of recently patented devices and the data supporting their use. These include devices to enhance thrombolysis, thrombectomy devices, stents, devices for augmenting global brain tissue perfusion, and devices that provide neuroprotection after stroke. We discuss specific design elements of these devices and directions for future research. Ultimately, individually tailored combinations of these devices will likely prove most useful in treating patients with acute ischemic stroke.
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Highly Pure Phospholipids Based Brain Docosahexaenoic Acid Transporters
By Su ChenThe most common age-dependent neurodegenerative disorders such as dementia and Alzheimer's disease have become an urgent public health problem in the most areas of the world. The strategy of the current therapy focuses on increasing availability of brain acetylcholine concentration, and use of acetylcholinesterase inhibitors has become the main approach to symptomatic treatment. However, an ideal drug for the disorders should enable to both simultaneously delay or halt the underlying pathological process and improve memory. The present paper describes an alterative cholinergic strategy to memory enhancement by the exogenous introduction of highly enriched docosahexaenoic acid (DHA) - containing molecular species of highly pure phospholipids and highly pure ether phospholipids based brain DHA transporters to promote survival of aged basal forebrain cholinergic neurons (BFCNs) through reversing abnormal levels of neural membrane DHA aminophospholipids. This results in significantly improving neural membrane fluidity and gap capacity leading to further recovering the expression of the p75 neurotrophin receptor and then failed retrograde nerve growth factor signaling, followed by promoting the choline acetyltransferase activity in the BFCNs. The pre-clinical results shown in published patents and recent applications to support the proposed therapeutic mechanism of the brain DHA transporters are summarized. The advantage of the potential drugs in both the prevention and treatment of agedependent basal forebrain cholinergic dysfunction related neurodegenerative disorders is further discussed.
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The Injured Cochlea as a Target for Inflammatory Processes, Initiation of Cell Death Pathways and Application of Related Otoprotective Strategies
Authors: Ralph N. Abi-Hachem, Azel Zine and Thomas R. Van De WaterOne of the causes of sensorineural hearing loss is the loss of auditory hair cells following exposure to environmental stresses. Auditory hair cell death in response to cochlear trauma occurs via both necrosis and apoptosis. Apoptosis of hair cells involves the caspase and MAPK/JNK pathways which are activated by oxidative stress and secretion of inflammatory cytokines in response to trauma. Identification of the pathways that lead to apoptosis provides therapeutic targets for the conservation of hearing. Antioxidants reduce the level of reactive oxygen species and reactive nitrogen species generated by oxidative stress in response to acoustic trauma, aminoglycoside and platinum-based drugs. Caspase inhibitors affect both the extrinsic and intrinsic apoptotic pathways, thereby reducing cisplatin, aminoglycoside, hydraulic trauma and ischemia-induced hearing losses. Corticosteroid therapy reduces inflammation and inhibits apoptosis while activating pro-survival pathways in the organ of Corti following exposure to noise, vibration, cisplatin, aminoglycoside, ischemia/reperfusion injury, bacterial meningitis and electrode insertion trauma. Inhibitors of JNK signaling pathway prevent apoptosis of auditory hair cells following electrode insertion trauma, acute labyrinthitis, acoustic trauma and aminoglycoside ototoxicity. This review provides an overview of the different pathways involved in auditory hair cell death following an environmental stress and both traditional and newly developed drugs that are currently being studied or used for the treatment of acute hearing loss. Recent patents related to otoprotective strategies to conserve hearing and auditory hair cells are also discussed in this review.
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Herbals and Natural Dietary Supplements in Psychiatric Practice
Authors: Matteo Chiappedi and Maurizio BejorThere is some evidence that links the increase of mental disorders' prevalence with a deterioration of Western countries' nutritional habits and it is found that the use of herbal and “natural” food supplements to treat different disorders is increasing. With factors such as chronic illness, poor health, emotional distress, and quality of life influencing the desire for complementary medicine, patients with comorbid medical and psychiatric problems seem likely to turn to this approach. We reviewed the most commonly used herbal and dietary supplements for which a certain efficacy on psychiatric symptoms or disorders has been claimed, checking current Pubmed-indexed literature (the most important being St. John's wort, Omega-3 fatty acids, valerian, Kava, Ginkgo, folate, B vitamins, SAMe, Inositol). There is an evidence of efficacy for some of these herbs an supplements, but current studies are often insufficient to reach a final conclusion; still patents are being requested and registered. Many different areas (including efficacy, tolerability, optimal dosing, adequate shelf life, drug and non-pharmacological interactions) need to be thoroughly studied; moreover political decisions need to be scientifically guided in order to best serve psychiatric patients’ interests and to prevent the usage of expensive and sometimes un-useful therapies. This implies that a scientific strategy has to be used to rule out any thirdpart economical interest which could in any way influence therapeutic choices.
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Cerebrospinal Fluid Proteins in the Diagnosis of Alzheimer's Disease
Authors: Vasileios T. Papaliagkas, Magda Tsolaki and George AnogianakisAlzheimer's disease (AD) is rapidly grooving incidence that affects millions of people worldwide, therefore there is an immediate need for its' early and accurate diagnosis. Many research studies have been performed on possible accurate and reliable diagnostic biomarkers of AD. This review study provides an overview on the cerebrospinal fluid (CSF) proteins that are used as biochemical markers for the early diagnosis of AD and their future prospects, as well as relevant patents.
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Patent Selections
More LessThe patents annotated in this section have been selected from various patent databases. These recent patents are relevant to the articles published in this journal issue, categorized by therapeutic areas/agent/targets and therapeutic agents related to CNS drug discovery.
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