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Total 54 results found since Jan 2013.

Neuroprotective Effects of Ginkgolide B against Ischemic Stroke: a Review of Current Literature.
Abstract Extensive evidences have shown the promising effects of Ginkgo biloba consumption on several diseases such as Alzheimer, Parkinson, ischemic stroke, etc. Several studies also reported its beneficial role on motor activity and cognitive function. This species contain unique class of diterpene, namely Ginkgolide B, which possess several pharmacological activities such as protective effect against cardiovascular disease; the most important causes of death worldwide. The promising effects of Ginkgolide B on stroke, both ischemic and hemorrhagic, are suggested by an overwhelming body of scientific evidences. M...
Source: Current Topics in Medicinal Chemistry - June 10, 2015 Category: Chemistry Authors: Nabavi SM, Habtemariam S, Daglia M, Braidy N, Loizzo MR, Tundis R, Nabavi SF Tags: Curr Top Med Chem Source Type: research

Molecules, Vol. 28, Pages 1021: Cyclic Glycine-Proline (cGP) Normalises Insulin-Like Growth Factor-1 (IGF-1) Function: Clinical Significance in the Ageing Brain and in Age-Related Neurological Conditions
ep Singh-Mallah Insulin-like growth factor-1 (IGF-1) function declines with age and is associated with brain ageing and the progression of age-related neurological conditions. The reversible binding of IGF-1 to IGF binding protein (IGFBP)-3 regulates the amount of bioavailable, functional IGF-1 in circulation. Cyclic glycine-proline (cGP), a metabolite from the binding site of IGF-1, retains its affinity for IGFBP-3 and competes against IGF-1 for IGFBP-3 binding. Thus, cGP and IGFBP-3 collectively regulate the bioavailability of IGF-1. The molar ratio of cGP/IGF-1 represents the amount of bioavailable and functional IG...
Source: Molecules - January 19, 2023 Category: Chemistry Authors: Jian Guan Fengxia Li Dali Kang Tim Anderson Toni Pitcher John Dalrymple-Alford Paul Shorten Gagandeep Singh-Mallah Tags: Review Source Type: research

The NOX1/4 Inhibitor GKT136901 as Selective and Direct Scavenger of Peroxynitrite.
Abstract NADPH oxidases (NOX), catalyzing the reduction of molecular oxygen to form the superoxide radical anion (.O2-) and hydrogen peroxide (H2O2), are involved in several pathological conditions, such as stroke, diabetes, atherosclerosis, but also in chronic neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, or multiple sclerosis. GKT136901 is a novel NOX-1/4 inhibitor with potential application in the areas of diabetic nephropathy, stroke, or neurodegeneration. In the present study, we investigated additional pharmacological activities of the compound with respect to direct free radic...
Source: Current Medicinal Chemistry - July 8, 2013 Category: Chemistry Authors: Schildknecht S, Weber A, Gerding HR, Pape R, Robotta M, Drescher M, Marquardt A, Daiber A, Ferger B, Leist M Tags: Curr Med Chem Source Type: research

Molecular mechanisms of signaling via the docosanoid neuroprotectin D1 for cellular homeostasis and neuroprotection Cell Biology
Docosahexaenoic acid, enriched in the brain and retina, generates docosanoids in response to disruptions of cellular homeostasis. Docosanoids include neuroprotectin D1 (NPD1), which is decreased in the CA1 hippocampal area of patients with early-stage Alzheimer's disease (AD). We summarize here how NPD1 elicits neuroprotection by up-regulating c-REL, a nuclear factor (NF)-κB subtype that, in turn, enhances expression of BIRC3 (baculoviral inhibitor of apoptosis repeat-containing protein 3) in the retina and in experimental stroke, leading to neuroprotection. Elucidating the mechanisms of action of docosanoids will contrib...
Source: Journal of Biological Chemistry - July 28, 2017 Category: Chemistry Authors: Aram Asatryan, Nicolas G. Bazan Tags: Minireviews Source Type: research

Molecules, Vol. 24, Pages 2323: Advances in Biosynthesis, Pharmacology, and Pharmacokinetics of Pinocembrin, a Promising Natural Small-Molecule Drug
ng Yang Pinocembrin is one of the most abundant flavonoids in propolis, and it may also be widely found in a variety of plants. In addition to natural extraction, pinocembrin can be obtained by biosynthesis. Biosynthesis efficiency can be improved by a metabolic engineering strategy and a two-phase pH fermentation strategy. Pinocembrin poses an interest for its remarkable pharmacological activities, such as neuroprotection, anti-oxidation, and anti-inflammation. Studies have shown that pinocembrin works excellently in treating ischemic stroke. Pinocembrin can reduce nerve damage in the ischemic area and reduce mitochon...
Source: Molecules - June 23, 2019 Category: Chemistry Authors: Xiaoling Shen Yeju Liu Xiaoya Luo Zhihong Yang Tags: Review Source Type: research

Molecules, Vol. 27, Pages 2484: Beneficial Effects of Capsaicin in Disorders of the Central Nervous System
k Capsaicin is a natural compound found in chili peppers and is used in the diet of many countries. The important mechanism of action of capsaicin is its influence on TRPV1 channels in nociceptive sensory neurons. Furthermore, the beneficial effects of capsaicin in cardiovascular and oncological disorders have been described. Many recent publications show the positive effects of capsaicin in animal models of brain disorders. In Alzheimer’s disease, capsaicin reduces neurodegeneration and memory impairment. The beneficial effects of capsaicin in Parkinson’s disease and depression have also be...
Source: Molecules - April 12, 2022 Category: Chemistry Authors: Micha ł Pasierski Bart łomiej Szulczyk Tags: Review Source Type: research

Arundic Acid a potential neuroprotective agent: biological development and syntheses.
Abstract Arundic acid has been experimented in vitro and in vivo as a potential neuroprotective agent. It modulates astrocyte activation by inhibiting the enhanced astrocytic synthesis of S-100β protein, responsible for inducing neuronal death. The phase II clinical trials for the treatment of acute ischemic stroke, as well as clinical development in other neurodegenerative diseases including amytrophic lateral sclerosis, Alzheimer's disease and Parkinson's disease are recently completed. There is no review published in this area since its discovery as potential neuroprotective agent and the various syntheses rep...
Source: Current Medicinal Chemistry - May 22, 2013 Category: Chemistry Authors: Fernandes RA, Ingle AB Tags: Curr Med Chem Source Type: research

Design and development of a novel supportive care product for the treatment of sialorrhea in Parkinson's disease.
Abstract Sialorrhea or excessive drooling is a significant medical issue in Parkinson's disease (PD) and neurodegenerative disorders, although it is often underreported by patients. Sialorrhea affects a large proportion of PD patients, ranging up to 78% in advanced stages, with many PD patients considering drooling as their worst non-motor symptom. Sialorrhea affects up to a million patients with diverse neurological impairments, including cerebral palsy, amyotrophic lateral sclerosis (ALS), Huntington's, survivors of stroke and severe traumatic brain injury. Numerous approaches have been attempted to treat sialor...
Source: Current Topics in Medicinal Chemistry - April 4, 2015 Category: Chemistry Authors: Farber NM, Perez-Lloret S, Gamzu ER Tags: Curr Top Med Chem Source Type: research

5-Aminoisoquinolin-1-one (5-AIQ), a Water-Soluble Inhibitor of the Poly¬(ADP Ribose)¬Polymerases (PARPs).
Abstract 5-Aminoisoquinolin-1-one (5-AIQ) is a water-soluble inhibitor of the poly(ADP-ribose)polymerases (PARPs), lacking isoform-selectivity. Although of only moderate potency in vitro against PARP-1, it is highly active in many assays in cells and in models in vivo, indicating excellent uptake. Optimisation of the several synthetic sequences to 5-AIQ has led to development of a short and efficient route from 1-chloroisoquinoline. It has been used widely as a biochemical and pharmacological tool to study the effects of inhibition of the PARPs. It ameliorates the damage to cells and tissues following reperfusion ...
Source: Current Medicinal Chemistry - October 2, 2015 Category: Chemistry Authors: Threadgill MD Tags: Curr Med Chem Source Type: research

Serotonin 1A Receptors on Astrocytes as a Potential Target for Treatment of Parkinson's Disease.
We reported recently that stimulation of serotonin 1A (5-HT1A) receptors on astrocytes promoted astrocyte proliferation and upregulated antioxidative molecules to act as a neuroprotectant in parkinsonian mice. PD is a progressive neurodegenerative disease with motor symptoms such as tremor, bradykinesia, rigidity and postural instability, that are based on selective loss of nigrostriatal dopaminergic neurons, and with non-motor symptoms such as orthostatic hypotension and constipation based on peripheral neurodegeneration. Although dopaminergic therapy for managing the motor disability associated with PD is being assessed ...
Source: Current Medicinal Chemistry - January 21, 2016 Category: Chemistry Authors: Miyazaki I, Asanuma M Tags: Curr Med Chem Source Type: research

Neurotrophins' Modulation by Olive Polyphenols.
CONCLUSIONS: In this context, a better understanding of the effects of polyphenols on neurotrophins and their receptors (TrkA, TrkB, p75NTR) could certainly generate interest for drug discovery and also for the potential dietary prevention of several neurological and cardiometabolic diseases. PMID: 27356540 [PubMed - as supplied by publisher]
Source: Current Medicinal Chemistry - June 25, 2016 Category: Chemistry Authors: Fiore M, Ceccanti M, Carito V, Tarani L, Ferraguti G, Chaldakov GN Tags: Curr Med Chem Source Type: research

Phthalides: Distribution in Nature, Chemical Reactivity, Synthesis, and Biological Activity.
Authors: León A, Del-Ángel M, Ávila JL, Delgado G Abstract Phthalides are a relatively small group of natural compounds confined to several plant families and some genera of fungi and liverworts. They are divided into two structural groups, the monomeric and dimeric phthalides, and known mainly as bioactive constituents of different plant species used traditionally for medicinal purposes in Asia, Europe, and North America.The first reports on the chemistry of phthalides appeared at the end of the nineteenth century, in which they were identified as the odor constituents of the essential oil of celery (Apium grav...
Source: Progress in the chemistry of organic natural products - February 7, 2017 Category: Chemistry Tags: Prog Chem Org Nat Prod Source Type: research

Molecules, Vol. 22, Pages 676: Adenosine A1 and A2A Receptors in the Brain: Current Research and Their Role in Neurodegeneration
The inhibitory adenosine A1 receptor (A1R) and excitatory A2A receptor (A2AR) are predominantly expressed in the brain. Whereas the A2AR has been implicated in normal aging and enhancing neurotoxicity in multiple neurodegenerative diseases, the inhibitory A1R has traditionally been ascribed to have a neuroprotective function in various brain insults. This review provides a summary of the emerging role of prolonged A1R signaling and its potential cross-talk with A2AR in the cellular basis for increased neurotoxicity in neurodegenerative disorders. This A1R signaling enhances A2AR-mediated neurodegeneration, and provides a p...
Source: Molecules - April 23, 2017 Category: Chemistry Authors: Jocelyn Stockwell Elisabet Jakova Francisco Cayabyab Tags: Review Source Type: research

Molecules, Vol. 22, Pages 1029: Virtual Screening against Phosphoglycerate Kinase 1 in Quest of Novel Apoptosis Inhibitors
Inhibition of apoptosis is a potential therapy to treat human diseases such as neurodegenerative disorders (e.g., Parkinson ’s disease), stroke, and sepsis. Due to the lack of druggable targets, it remains a major challenge to discover apoptosis inhibitors. The recent repositioning of a marketed drug (i.e., terazosin) as an anti-apoptotic agent uncovered a novel target (i.e., human phosphoglycerate kinase 1 (hPgk1)). I n this study, we developed a virtual screening (VS) pipeline based on the X-ray structure of Pgk1/terazosin complex and applied it to a screening campaign for potential anti-apoptotic agents. The hierarchi...
Source: Molecules - June 21, 2017 Category: Chemistry Authors: Jie Xia Bo Feng Qianhang Shao Yuhe Yuan Xiang Wang Naihong Chen Song Wu Tags: Article Source Type: research

Small molecule SUMOylation activators are novel neuroprotective agents.
Abstract Neuronal loss characterizes many of the most intractable nervous system diseases that deprive our ageing population of their quality of life. Neuroprotective pharmacological modalities are urgently needed to address this burgeoning population. Small ubiquitin-like modifier (SUMO) conjugation has been established as an endogenous neuroprotective response, and we have discovered several classes of small molecules that enhance SUMO conjugation. Herein we describe the hit to lead campaign that enabled the discovery of 3 diverse classes of drug-like SUMOylation activators. Optimized compounds were ultimately v...
Source: Bioorganic and Medicinal Chemistry Letters - December 13, 2017 Category: Chemistry Authors: Krajnak K, Dahl R Tags: Bioorg Med Chem Lett Source Type: research