Coumarin-Piperazine Derivatives as Biologically Active Compounds

Publication date: Available online 7 December 2019Source: Saudi Pharmaceutical JournalAuthor(s): Kinga OstrowskaAbstractA number of psychiatric disorders, including anxiety, schizophrenia, Parkinson’s disease, depression and others CNS diseases are known to induce defects in the function of neural pathways sustained by the neurotransmitters, like dopamine and serotonin. N-arylpiperazine moiety is important for CNS-activity, particularly for serotonergic and dopaminergic activity. In the scientific literature there are many examples of coumarin-piperazine derivatives, particularly with arylpiperazines linked to a coumarin system via an alkyl liner, which can modulate serotonin, dopamine and adrenergic receptors. Numerous studies have revealed that the inclusion of a piperazine moiety could occasionally provide unexpected improvements in the bioactivity of various biologically active compounds. The piperazine analogs have been shown to have a potent antimicrobial activity and they can also act as BACE-1 inhibitors. On the other hand, arylpiperazines linked to coumarin derivatives have been shown to have antiproliferative activity against leukemia, lung, colon, breast, and prostate tumors. Recently, it has been reported that coumarin-piperazine derivatives exhibit a Fneuroprotective effect by their antioxidant and anti-inflammatory activities and they also show activity as acetylcholinesterase inhibitors and antifilarial activity. In this work we provide a summary of the l...
Source: Saudi Pharmaceutical Journal - Category: Drugs & Pharmacology Source Type: research

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This study showed an association between SNPs in IL10 and NOD2 genes. It also revealed that the genotypes of the different SNPs influence bone resorption and health. Additionally, age at first edentulism and bone height were much lower in some genotypes. This study demonstrates the need for larger multicenter trials to confirm these findings. Finally, we suggest that the results of this study may be utilized for developing novel genetic diagnostic tests and for identifying Saudi individuals who may be more susceptible to RRR development following dental extraction.
Source: Saudi Journal of Biological Sciences - Category: Biology Source Type: research
Publication date: Available online 17 January 2020Source: Saudi Journal of Biological SciencesAuthor(s): Sohrab Mamnabi, Safar Nasrollahzadeh, Kazem Ghassemi-Golezani, Yaghoub RaeiAbstractTwo separate field experiments were conducted in 2018 and 2019 as split-plot based on randomized complete block design with three replications to evaluate physiological responses of rapeseed to fertilization treatments (control, chemical fertilizer, inoculation of seeds with PGPR, vermicompost and combined fertilizers) under different irrigation levels (irrigation after 70,100, 130, and 160 mm evaporation). Water stress increased the acti...
Source: Saudi Journal of Biological Sciences - Category: Biology Source Type: research
Publication date: Available online 17 January 2020Source: Life SciencesAuthor(s): Bharati Bhattacharjee, Palash Kumar Pal, Aindrila Chattopadhyay, Debasish BandyopadhyayAbstractAimsThe aim of the present study was to evaluate the possible antioxidant role of oleic acid (OA) against Cd-induced injuries in the heart and liver tissues of male Wistar rats.Main methodsRats were treated with either vehicle (control), or OA (10 mg/kg b.w., fed orally), or Cd (0.44 mg/kg b.w., s.c.), or both (OA + Cd) for 15 days. Following completion of the treatment period, biomarkers of organ damage and oxidative stress including ROS,...
Source: Life Sciences - Category: Biology Source Type: research
Publication date: Available online 18 January 2020Source: BiologicalsAuthor(s): David GervaisAbstractErwinia chrysanthemi l-asparaginase (ErA) has been used for the treatment of acute lymphoblastic leukaemia (ALL) for decades, and its safety and efficacy have been well demonstrated. ErA drug substance and drug product contain a small proportion of acidic isoforms, with a known mechanism of formation, which have been shown to be minor conformational variants retaining enzymatic activity and function. Specifications for these acidic isoforms were set with an extremely limited data set, and with further manufacturing experien...
Source: Biologicals - Category: Biology Source Type: research
This study reviews electrophysiological studies of ketamine's effects in individuals with depression as well as healthy controls, with a focus on two putative markers of synaptic potentiation: gamma oscillations and long-term potentiation. The review focuses on: 1) measures of gamma oscillations and power and their relationship to both acute, psychotomimetic drug effects as well as delayed antidepressant response in mood disorders; 2) changes in long-term potentiation as a promising measure of synaptic potentiation following ketamine administration; and 3) recent efforts to model antidepressant response to ketamine using n...
Source: Pharmacology Biochemistry and Behavior - Category: Biochemistry Source Type: research
This study analysed Cd or As effects on peroxisomes, and NO production and distribution in the root system, including primary root (PR) and lateral roots (LRs). Arabidopsis thaliana wild-type and transgenic plants enabling peroxisomes to be visualized in vivo, through the expression of the 35S-cyan fluorescent protein fused to the peroxisomal targeting signal1 (PTS1) were used. Peroxisomal enzymatic activities including the antioxidant catalase, the H2O2-generating glycolate oxidase, and the hydroxypyruvate reductase, and root system morphology were also evaluated under Cd/As exposure. Results showed that Cd and As differe...
Source: Plant Physiology and Biochemistry - Category: Biochemistry Source Type: research
In this study, cranberry pomace was consecutively fractionated by supercritical carbon dioxide (SC-CO2) and pressurized liquid (PLE) extraction for the recovery of lipophilic and polyphenolic fractions. Process parameters were optimized by response surface methodology (RSM), ethanol (EtOH) and water were used in PLE. The highest yield (11.10 ± 0.15%) in supercritical fluid extraction (SFE) was obtained at 42.4 MPa pressure, 53 °C temperature and 158 min. Linoleic (36.58%), linolenic (32.44%), oleic (21.79%) and palmitic (4.36%) acids were the major fatty acids in the oil. PLE-E...
Source: The Journal of Supercritical Fluids - Category: Chemistry Source Type: research
Publication date: April 2020Source: Phytochemistry, Volume 172Author(s): David Soba, Maren Müller, Iker Aranjuelo, Sergi Munné-BoschAbstractAlthough the biosynthesis and function of tocochromanols in leaves and seeds have been extensively studied, their occurrence and function in underground tissues, such as roots and nodules, is very poorly understood. Here, we performed a comparative study of the presence of tocochromanols in different plant organs (leaves, roots and nodules) of three legumes (soybean, alfalfa and pea plants). Additionally, we measured variations in tocochromanols as a function of the severit...
Source: Phytochemistry - Category: Chemistry Source Type: research
 Since time was invented, people have fallen into three main categories: Chronically early, on-time, or late. You don’t need mental illness to put things off until the last minute and it doesn’t take anxiety to get things done well ahead of schedule. But, there’s also no denying that living with mental illness can – and does – impact our ability to be punctual and to accomplish goals. In this episode, Gabe and Michelle discuss the difference between putting things off because we are making bad choices and putting things off because of mental health issues. Listen now! SUBSCRIBE &REVI...
Source: World of Psychology - Category: Psychiatry & Psychology Authors: Tags: A Bipolar, A Schizophrenic, and a Podcast Personal Schizophrenia Self-Help Source Type: blogs
From leisure activities to politics to relationships, people tend to be influenced by their religious beliefs. In this episode, Gabe and Michelle discuss the pros and cons of religious influence when it comes to treating mental illness and explore whether it is helpful when trying to reach recovery. SUBSCRIBE &REVIEW “They are dead (by suicide) and we are still stigmatizing their behavior.” – Gabe Highlights from ‘Religion and Mental Illness’ Episode [2:00] The intersection of religion and mental illness. [4:30] How the Jewish faith views mental illness. [10:00] How Christianity view...
Source: World of Psychology - Category: Psychiatry & Psychology Authors: Tags: A Bipolar, A Schizophrenic, and a Podcast Depression Ethics & Morality Schizophrenia Spirituality & Health Source Type: blogs
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