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Journal articles on the topic 'Alkaloider. Alkaloids Alkaloids Benzodiazepines Benzodiazepines'

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Published: 4 June 2021

Last updated: 9 February 2022

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1

Batiha, Gaber El-Saber, Luay M. Alkazmi, Eman H. Nadwa, Eman K. Rashwan, Amany Magdy Beshbishy, Hazem Shaheen, and Lamiaa Wasef. "Physostigmine: A Plant Alkaloid Isolated from Physostigma venenosum: A Review on Pharmacokinetics, Pharmacological and Toxicological Activities." Journal of Drug Delivery and Therapeutics 10, no. 1-s (February 15, 2020): 187–90. http://dx.doi.org/10.22270/jddt.v10i1-s.3866.

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Medicinal plants have been documented as an important source for discovering new pharmaceutical molecules that have been used to treat serious diseases. Strikingly, previous reports stated that natural products and their derived compounds exhibit lesser side effects and improved efficacy than other synthetic counterparts. Physostigmine, a parasympathomimetic plant alkaloid isolated from the West African perennial shrub Physostigma venenosum, it shows a narrow therapeutic index and a short life span, despite its ability to penetrate the blood-brain barrier (BBB). It is a widely known reversible butyrylcholinesterase (BuChE) and acetylcholinesterase (AChE) inhibitor and has been documented to treat various ailments such as Alzheimer’s disease. Pharmacologically, physostigmine was first reported as an antidote for atropine scopolamine and belladonna alkaloids toxicity. Recently, it has been documented as a therapy for treating several ailments including glaucoma, myasthenia gravis and the intoxication caused by tricyclic antidepressant overdoses, anti-histamines, antipsychotics, and benzodiazepines. Physostigmine has been reported to be absorbed from the gastrointestinal tract and showed short half-life, as, after the oral administration of 2 mg of physostigmine salicylate, the peak plasma concentration reached to 30 minutes. This review examines the biological activities, pharmacokinetics, and toxicity of physostigmine extracted from P. venenosum. Keywords: Physostigma venenosum, Physostigmine, pharmacological activities, acetylcholinesterase and butyrylcholinesterase inhibitor.

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2

Nurmilatina, Nurmilatina. "Analisis Komposisi Kimia Daun Kelakai (Stenochlaena palustris Bedd.) dengan Berbagai Pelarut menggunakan GCMS (Chemical Composition Analysis of Stenochlaena palustris Bedd. Leaves using Various Solvents on GCMS)." Jurnal Riset Industri Hasil Hutan 9, no. 1 (October 1, 2017): 9–16. http://dx.doi.org/10.24111/jrihh.v9i1.2952.

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The selection of suitable solvents is essential for extracting the desired compounds from plant cells. GCMS is an instrument that can be used to identify such compounds. Therefore, this study objective is to extract kelakai leaves using various solvents and analyze the composition of chemical compounds using GCMS instrument. Kelakai leaves was extracted using three solvent variations: a1 = aquadest, a2 = ethanol, and a3 = ethanol 50%; and the maceration time variations: b1 = 1 day, b2 = 2 days, and b3 = 3 days. The best extraction method was aquadest as solvent and one day maceration. The chemical compound extracted were phenolic, alkaloids and terpenoids, such as 2,5-bis [(trimethylsilyl) oxy] benzaldehyde 1,86%, linalool 1,28%, phenethyl alcohol 3,55% and 7-chloro-5-phenyl-1-(trimethylsilyl)-1,3-dihydro-2H-1,4-benzodiazepines-2-on 1,16 % db.Keywords: composition analysis, GCMS, maceration, Stenochlaena palustris Bedd.

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3

Davidsen, Jesper Rømhild, Lars Christian Lund, Christian B. Laursen, Jesper Hallas, and Daniel Pilsgaard Henriksen. "Dynamics in diagnoses and pharmacotherapy before and after diagnosing idiopathic pulmonary fibrosis." ERJ Open Research 6, no. 4 (September 17, 2020): 00479–2020. http://dx.doi.org/10.1183/23120541.00479-2020.

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BackgroundIdiopathic pulmonary fibrosis (IPF) is a well-characterised interstitial lung disease. Typically, IPF diagnosis is delayed due to nonspecific symptoms, but can also be delayed due to treatment attempts on false indication or due to treatment targeting common comorbidities. This observational study aimed to assess the dynamics in the medication and diagnosis patterns in the period before and after an IPF diagnosis.MethodsWe identified all Danish patients with IPF between 2002 and 2017. We evaluated new and ongoing drug treatments and incident diagnoses 36 months before and 12 months after an IPF diagnosis by use of Danish nationwide registries. To aid interpretation, 10 random controls were recruited for each case.ResultsA total of 650 IPF patients were identified (median age 73 years (interquartile range 65–78), 70.3% males). Prior to the IPF diagnosis, the most prevalent diagnoses were dyspnoea and non-IPF interstitial lung diseases. For drug use, IPF patients had higher initiation rates for antibiotics, oral corticosteroids and mucolytics. In terms of drug volume, IPF patients used more respiratory drugs, antibiotics, immunosuppressants, corticosteroids, proton pump inhibitors, benzodiazepines and opium alkaloids within the 6 months preceding their IPF diagnosis, compared to the controls. Overall drug use decreased after an IPF diagnosis, mainly due to a reduced glucocorticoid and cardiovascular drug use.ConclusionAmong IPF patients, an increased drug use was observed for diagnoses with symptoms overlapping those of IPF, particularly this was observed during the last 6 months before an IPF diagnosis. This emphasises the need for an increased IPF awareness.

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Sudarma, I. Made, and John Bremner. "SYNTHESIS OF THE ISOQUINO-[2,1-c][1,3]-BENZODIAZEPINE DERIVATIVE FROM PAPAVERINE." Indonesian Journal of Chemistry 7, no. 3 (June 20, 2010): 324–26. http://dx.doi.org/10.22146/ijc.21677.

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The objective of this research was to synthesize isoquino[2,1-c][1,3]benzodiazepine from papaverine alkaloid. Functional Group Interconversion (FGI) and Carbon -Nitrogen bond connection approach was investigated. Papaverine (1) was nitrated by HNO3 to compound (2) and followed by reduction with Sn and HCl to afford aminonorlaudanosine (3). Formation of cyclic benzodiazepine (4) was achieved by reaction of (3) with CS2. Products of reactions were confirmed by Nuclear Magnetic Resonances (n.m.r), Mass Spectrum, and Fourier Transform Infra Red (FTIR). Keywords: isoquino[2,1-c][1,3]benzodiazepine, papaverine

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5

Cui, Chuan-Ming, Xiao-Ming Li, Chun-Shun Li, Hao-Fen Sun, Shu-Shan Gao, and Bin-Gui Wang. "Benzodiazepine Alkaloids from Marine-Derived Endophytic FungusAspergillus ochraceus." Helvetica Chimica Acta 92, no. 7 (July 2009): 1366–70. http://dx.doi.org/10.1002/hlca.200900084.

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6

Munir, Samman, Aqsa Shahid, Bilal Aslam, Usman Ali Ashfaq, Muhammad Sajid Hamid Akash, Muhammad Akhtar Ali, Ahmad Almatroudi, Khaled S. Allemailem, Muhammad Shahid Riaz Rajoka, and Mohsin Khurshid. "The Therapeutic Prospects of Naturally Occurring and Synthetic Indole Alkaloids for Depression and Anxiety Disorders." Evidence-Based Complementary and Alternative Medicine 2020 (October 16, 2020): 1–11. http://dx.doi.org/10.1155/2020/8836983.

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Depression and anxiety are the most common disorders among all age groups. Several antidepressant drugs including benzodiazepine, antidepressant tricyclics, azapirone, noradrenaline reuptake inhibitors, serotonin selective reuptake inhibitors, serotonin, noradrenaline reuptake inhibitors, and monoamine oxidase inhibitors have been used to treat these psychiatric disorders. However, these antidepressants are generally synthetic agents and can cause a wide range of side effects. The potential efficacy of plant-derived alkaloids has been reviewed against various neurodegenerative diseases including Alzheimer’s disease, Huntington disease, Parkinson’s disease, schizophrenia, and epilepsy. However, data correlating the indole alkaloids and antidepressant activity are limited. Natural products, especially plants and the marine environment, are rich sources of potential new drugs. Plants possess a variety of indole alkaloids, and compounds that have an indole moiety are related to serotonin, which is a neurotransmitter that regulates brain function and cognition, which in turn alleviates anxiety, and ensures a good mood and happiness. The present review is a summary of the bioactive compounds from plants and marine sources that contain the indole moiety, which can serve as potent antidepressants. The prospects of naturally occurring as well as synthetic indole alkaloids for the amelioration of anxiety and depression-related disorders, structure-activity relationship, and their therapeutic prospects have been discussed.

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7

Helbig, Florian, Jörg Steighardt, and Werner Roos. "Uric Acid Is a Genuine Metabolite of Penicillium cyclopium and Stimulates the Expression of Alkaloid Biosynthesis in This Fungus." Applied and Environmental Microbiology 68, no. 4 (April 2002): 1524–33. http://dx.doi.org/10.1128/aem.68.4.1524-1533.2002.

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ABSTRACT On searching for endogenous, low-molecular-weight effectors of benzodiazepine alkaloid biosynthesis in Penicillium cyclopium uric acid was isolated from ethanolic or autoclaved mycelial extracts of this fungus. The isolation was based on a three-step high-pressure liquid chromatography procedure guided by a microplate bioassay, and uric acid was identified by mass spectrometry and the uricase reaction. Conidiospore suspensions that were treated with this compound during the early phase of outgrowth developed emerged cultures with an enhanced rate of alkaloid production. Uric acid treatment did not increase the in vitro measurable activity of the rate-limiting biosynthetic enzyme, cyclopeptine synthetase. However, these cultures displayed a reduced rate of uptake of the alkaloid precursor l-phenylalanine into the vacuoles of the hyphal cells as assayed in situ. It is suggested that the depressed capacity of vacuolar uptake caused by the contact of outgrowing spores with uric acid liberated from hyphal cells results in an enhanced availability of the precursor l-phenylalanine in the cytoplasm and thus accounts at least in part for the increase in alkaloid production.

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Li, Jing, Yi-sheng Zhong, Jie Yuan, Xun Zhu, Yong-jun Lu, Yong-cheng Lin, and Lan Liu. "A New Terminal Cyano Group-containing Benzodiazepine Alkaloid from the Mangrove Endophytic Fungus Penicillium sp." Natural Product Communications 10, no. 9 (September 2015): 1934578X1501000. http://dx.doi.org/10.1177/1934578x1501000916.

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A new benzodiazepine alkaloid containing terminal cyano group has been isolated from a mangrove endophytic fungus, Penicillium 299#. Structure elucidation was determined by 1D and 2D NMR spectroscopy and the absolute configuration was determined by electronic circular dichroism (ECD). The new compound showed no cytotoxic activities in vitro against human cancer lines MDA-MB-435, HepG2, HCT-116, and Calu-3.

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9

Sorra, Kumaraswamy, K. Mukkanti, and Srinivas Pusuluri. "Palladium catalyzed synthesis of quinazolino [1,4] benzodiazepine alkaloids and analogous." Tetrahedron 68, no. 7 (February 2012): 2001–6. http://dx.doi.org/10.1016/j.tet.2011.12.032.

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Witt, F. Anette, and Jan Bergman. "Oxygen analogues of the benzodiazepine alkaloids sclerotigenin and circumdatin F." Journal of Heterocyclic Chemistry 39, no. 2 (March 2002): 351–55. http://dx.doi.org/10.1002/jhet.5570390218.

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Witt, Anette, Annika Gustavsson, and Jan Bergan. "Studies towards the synthesis of the benzodiazepine alkaloid auranthine." Journal of Heterocyclic Chemistry 40, no. 1 (January 2003): 29–35. http://dx.doi.org/10.1002/jhet.5570400103.

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Witt, Anette, and Jan Bergman. "Total Syntheses of the Benzodiazepine Alkaloids Circumdatin F and Circumdatin C." Journal of Organic Chemistry 66, no. 8 (April 2001): 2784–88. http://dx.doi.org/10.1021/jo001696h.

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13

Hassan, Amir, Muhammad Ashfaq, Ali Khan, and Muhammad Shakeel Khan. "Isolation of Caffeine from Carbonated Beverages." Journal of Tropical Pharmacy and Chemistry 5, no. 1 (February 25, 2020): 33–38. http://dx.doi.org/10.25026/jtpc.v5i1.234.

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The work presented on the isolation of naturally occurring alkaloid from carbonated beverages. The extensive presence of caffeine in different plants plays an important role in the long-standing acceptance of caffeine-containing products. Caffeine (3,7-dihydro-1, 3,7-trimethyl-1H-purine-2,6-dione or 1,3,7-trimethylxanthine) is an alkaloid belongs to Methylxanthine family. Liquid-liquid extraction methods were used in the assay of research work. Chloroform was taken as extracting solvent. Solid residue of caffeine was recrystallized from 95% ethanol using 5ml/gram (5ml per gram). It is declared to raise caffeine, effects a number of different drugs include Paracetamol, Benzodiazepines and Aspirin and amount of plasma free Fatty acids increases. While inform that in regular sleeping interaction caffeine take place and raise the absorption of certain drugs. Changes in drug metabolizing enzymes, acts as an agent in a microsomal system of the body. The highest amount of caffeine dry crystal is extracted in sting sample while the 7up sample is free from caffeine.

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14

Roos, W., and H. P. Schmauder. "Positive feedback effect of benzodiazepine alkaloids on enzymes of the aromatic pathway." FEMS Microbiology Letters 59, no. 1-2 (May 1989): 27–30. http://dx.doi.org/10.1111/j.1574-6968.1989.tb03076.x.

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15

Witt, Anette, and Jan Bergman. "ChemInform Abstract: Oxygen Analogues of the Benzodiazepine Alkaloids Sclerotigenin and Circumdatin F." ChemInform 33, no. 38 (May 19, 2010): no. http://dx.doi.org/10.1002/chin.200238208.

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16

van Gelderen, G. J., D. Fekkes, L. Timmerman, and L. Pepplinkhuizen. "The significance of β-carbolines in psychiatry." Acta Neuropsychiatrica 6, no. 4 (December 1994): 61–65. http://dx.doi.org/10.1017/s0924270800034712.

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SummaryIn this review the naturally occurring β-carbolines norharman and harman in human beings and mammals will be discussed. These β-carbolines have been recognized as aromatic alkaloids, which can be detected in very low concentrations in human plasma. Norharman and especially harman display moderate affinity to the benzodiazepine receptor. The biosynthesis of these compounds in vivo, the localization, the biological effects and the probable involvement of these compounds in the cause of psychopathologic states will be discussed. This with a special focus on alcoholism, heroin addiction, psychosis and anxiety disorders. In some of these clinical pictures the concentration of norharman is increased. Whether this is a causality or a matter of minor importance is still unknown.

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Witt, Anette, and Jan Bergman. "ChemInform Abstract: Total Syntheses of the Benzodiazepine Alkaloids Circumdatin F and Circumdatin C." ChemInform 32, no. 34 (May 25, 2010): no. http://dx.doi.org/10.1002/chin.200134213.

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18

Ojika, Makoto, Tomoo Yoshida, and Kiyoyuki Yamada. "Aplysepine, a novel 1,4-benzodiazepine alkaloid from the sea hare Aplysia kurodai." Tetrahedron Letters 34, no. 33 (August 1993): 5307–8. http://dx.doi.org/10.1016/s0040-4039(00)73981-5.

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19

Boyes-Korkis, Jane M., Karen A. Gurney, Julia Penn, Peter G. Mantle, John N. Bilton, and Richard N. Sheppard. "Anacine, a New Benzodiazepine Metabolite of Penicillium aurantiogriseum Produced with Other Alkaloids in Submerged Fermentation." Journal of Natural Products 56, no. 10 (October 1993): 1707–17. http://dx.doi.org/10.1021/np50100a008.

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20

Wewalka, Marlene, Andreas Drolz, Katharina Staufer, Thomas M. Scherzer, Valentin Fuhrmann, and Christian Zauner. "Development of ARDS after Excessive Kath Consumption: A Case Report." Case Reports in Critical Care 2011 (2011): 1–3. http://dx.doi.org/10.1155/2011/291934.

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Khat is a drug widely used in the Horn of Africa and the Arabian Peninsula. Khat leaves contain, among other substances, the psychoactive alkaloid cathinone, which induce central nervous system stimulation leading to euphoria, hyperactivity, restlessness, and insomnia. However, it also could cause psychological adverse effects such as lethargy, sleepiness, psychoses, and depression necessitating pharmacologic treatment. Here we report the case of a 35-year-old man from Somalia who became unconscious and developed aspiration pneumonia and subsequent ARDS after excessive consumption of khat leaves. His unconsciousness was possibly caused by the sleepiness developed after khat consumption and a benzodiazepine intake by the patient himself. Thus, khat-induced adverse effects should not primarily be treated pharmacologically, but patients should be urged to quit khat consumption in order to eliminate or, at least, reduce the severity of present psychological adverse effects.

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Rahbæk, Lisa, Jens Breinholt, Jens C. Frisvad, and Carsten Christophersen. "Circumdatin A, B, and C: Three New Benzodiazepine Alkaloids Isolated from a Culture of the FungusAspergillus ochraceus." Journal of Organic Chemistry 64, no. 5 (March 1999): 1689–92. http://dx.doi.org/10.1021/jo981536u.

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Rault, Sylvain, Sandrine Jolivet-Fouchet, Frédéric Fabis, Philippe Bovy, and Philippe Ochsenbein. "Novel Rearrangement of Pyrrolo[2,1-c][1,4]benzodiazepines into Pyrrolo[2,1-b]quinazolinones, Analogous of Alkaloid, Vasicinone." HETEROCYCLES 51, no. 6 (1999): 1257. http://dx.doi.org/10.3987/com-98-8412.

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Ookura, Ryuhei, Keijiro Kito, Takashi Ooi, Michio Namikoshi, and Takenori Kusumi. "Structure Revision of Circumdatins A and B, Benzodiazepine Alkaloids Produced by Marine FungusAspergillus ostianus, by X-ray Crystallography." Journal of Organic Chemistry 73, no. 11 (June 2008): 4245–47. http://dx.doi.org/10.1021/jo800348d.

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Zhang, Dahai, Xiudong Yang, Jung Sook Kang, Hong Dae Choi, and Byeng Wha Son. "Circumdatin I, a New Ultraviolet-A Protecting Benzodiazepine Alkaloid from a Marine Isolate of the Fungus Exophiala." Journal of Antibiotics 61, no. 1 (January 2008): 40–42. http://dx.doi.org/10.1038/ja.2008.108.

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Jolivet-Fouchet, Sandrine, Frederic Fabis, Philippe Bovy, Philippe Ochsenbein, and Sylvain Rault. "ChemInform Abstract: Novel Rearrangement of Pyrrolo[2,1-c][1,4]benzodiazepines into Pyrrolo[2,1-b]quinazolinones, Analogues of Alkaloid, Vasicinone." ChemInform 31, no. 8 (June 10, 2010): no. http://dx.doi.org/10.1002/chin.200008180.

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Rahbaek, Lisa, Jens Breinholt, Jens C. Frisvad, and Carsten Christophersen. "ChemInform Abstract: Circumdatin A, B, and C: Three New Benzodiazepine Alkaloids Isolated from a Culture of the Fungus Aspergillus ochraceus." ChemInform 30, no. 29 (June 14, 2010): no. http://dx.doi.org/10.1002/chin.199929207.

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Mohammed, Z. M., Z. K. Haruna, Z. I. Abdullahi, S. A. Hussein, J. D. Habila, M. H. Abdullahi, A. Aliyu, and A. Ibrahim. "In-silico comparative study of three (3) bioactive compounds from methanol extracts of Combretum micranthum leaf, and diazepam with Gabaa receptor molecule." Bayero Journal of Pure and Applied Sciences 12, no. 1 (April 15, 2020): 235–41. http://dx.doi.org/10.4314/bajopas.v12i1.37s.

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Stress affects monoamine neurotransmitter in the central nervous system such as GABA (a major inhibitory neurotransmitter in the brain). GABAA receptor is hetero-oligomeric Cl-channel that is elective blocked by the alkaloid, bicuculline and modulated by steroids, barbiturates and benzodiazepines. The anticonvulsant activity of Diazepam may be mediated by enhancement of inhibition involving gamma-aminobutyric acid (GABA). Combretum micranthum is one of the maximum effective medicinal plants of therapeutic importance. Thus this study is to examine the effect of Combretum micranthum methanol leaf extract on GABAA Receptor via In-Silico analysis. Combretum micranthum methanol leaf extract was found using GC-MS to contain bioactive compounds (3,5-dichlorophenylhydrazine, guanidine and aminooxyacetic acid) with GABAergic functions. And the popular docking programs PatchDock and AutoDockVina were then used to predict computationally binding modes of these compounds with GABAA receptor. The molecular docking analyses indicated highly and effectively interactions (binding energy in kcal/mol) between GABAA receptor and the Combretum micranthum compounds (ligands): 3,5-dichlorophenylhydrazine (-193.85 and-5.6), guanidine (-87.63 and -3.3) and aminooxyacetic acid (-85.3 and -3.2) for both PatchDock and AutoDock Vina respectively. Results shows that 3,5-dichlorophenylhydrazine has a close binding energy in kcal/mol to that of Diazepam (-200.68 and -6.1 respectively). Findings of the study shows that the interaction between Combretum micranthum compounds (3,5-dichlorophenylhydrazine, guanidine and aminooxyacetic acid) with GABAA receptor can be explore for the development of new therapeutics to manage mental disorders. Keywords: Gamma-aminobutyric acid, Combretum micranthum , AutoDockVina, PatchDock

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Thissera, Bathini, Ahmed M. Sayed, Marwa H. A. Hassan, Sayed F. Abdelwahab, Ngozi Amaeze, Valeria T. Semler, Faizah N. Alenezi, et al. "Bioguided Isolation of Cyclopenin Analogues as Potential SARS-CoV-2 Mpro Inhibitors from Penicillium citrinum TDPEF34." Biomolecules 11, no. 9 (September 15, 2021): 1366. http://dx.doi.org/10.3390/biom11091366.

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SARS-CoV-2 virus mutations might increase its virulence, and thus the severity and duration of the ongoing pandemic. Global drug discovery campaigns have successfully developed several vaccines to reduce the number of infections by the virus. However, finding a small molecule pharmaceutical that is effective in inhibiting SARS-CoV-2 remains a challenge. Natural products are the origin of many currently used pharmaceuticals and, for this reason, a library of in-house fungal extracts were screened to assess their potential to inhibit the main viral protease Mpro in vitro. The extract of Penicillium citrinum, TDPEF34, showed potential inhibition and was further analysed to identify potential Mpro inhibitors. Following bio-guided isolation, a series of benzodiazepine alkaloids cyclopenins with good-to-moderate activity against SARS-CoV-2 Mpro were identified. The mode of enzyme inhibition of these compounds was predicted by docking and molecular dynamic simulation. Compounds 1 (isolated as two conformers of S- and R-isomers), 2, and 4 were found to have promising in vitro inhibitory activity towards Mpro, with an IC50 values range of 0.36–0.89 µM comparable to the positive control GC376. The in silico investigation revealed compounds to achieve stable binding with the enzyme active site through multiple H-bonding and hydrophobic interactions. Additionally, the isolated compounds showed very good drug-likeness and ADMET properties. Our findings could be utilized in further in vitro and in vivo investigations to produce anti-SARS-CoV-2 drug candidates. These findings also provide critical structural information that could be used in the future for designing potent Mpro inhibitors.

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Wang, Fuqian, Zhenquan Hu, Chunshun Li, Xiaohua Wu, and Shugeng Cao. "Circumdatin M, a new benzodiazepine alkaloid with a unique pyrimidone-4-pyrone moiety from a Hawaiian marine fungus Aspergillus sp. FM242." Tetrahedron Letters 60, no. 26 (June 2019): 1724–26. http://dx.doi.org/10.1016/j.tetlet.2019.05.061.

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Al-Said, Naim H., Khaled Q. Shawakfeh, Mohammad I. Ibrahim, and Sami H. Tayyem. "A facial synthesis of quinazolino[1,4]benzodiazepine alkaloids via reductive N-heterocyclization of N-(2-nitrobenzoyl)amides: total synthesis of asperlicin C, circumdatin H, and its analogues." Arkivoc 2010, no. 9 (July 11, 2010): 282–92. http://dx.doi.org/10.3998/ark.5550190.0011.926.

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Ziablitsev, S. V., T. I. Panova, and O. O. Starodubska. "NEURODESTRUCTION OF HYPOTHALAMIC NUCLEI IN BRAIN INJURY. EFFECT OF CARBACETAM." Medical Science of Ukraine (MSU) 13, no. 3-4 (June 21, 2018): 3–9. http://dx.doi.org/10.32345/2664-4738.3-4.2017.01.

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Relevance. A key role in the pathogenesis of brain injury (BI) is played by destructive changes in the neural tissue of the brain, which consist in damage to neurons and glial cells. To date, various drugs are being intensively developed and studied, which are considered in the perspective of correction and restoration of the functional state of the brain. These substances include the neuroprotector carbacetam, an modulator of the GABA-benzodiazepine receptor complex, a derivative of the alkaloid β-carboline. Objectie. To investigate the effect of carbacetam on neurodestruction processes in the paraventricular and supraoptic nuclei of the hypothalamus in experimental BI. Material and methods. The study was carried out on 20 white non-native male rats weighing 200±10 g. To simulate the BI, rats were subjected to one stroke along the cranial vault with a free-fall load according to the V.N. Yelskyy and S.V. Ziablitsev method (2008). The energy of impact was 0.52 J, the lethality for the first 5 days after injury was 84%. In the control group (n=10) 1 ml of saline was injected intraperitoneally once daily for 10 days after injury. Animals of the experimental group (n=10) received intraperitoneally injections of carbacetam at a dose of 5 mg/kg in 1 ml of saline according to the same scheme. After the experiment was over, the animals were decapitated with the removal of the brain, from which histological preparations were made with a microtome after appropriate histological treatment. Some sections were stained with hematoxylin and eosin, others were immunohistochemically reacted with antibodies against neuronmarkers proteins NSE, S-100 and GFAP. Results. Carbacetam influenced the decrease of degenerative processes in the nervous tissue of the paraventricular and supraoptic nuclei of the hypothalamus. Neurons of animals with BI that received carbacetam, were characterized by the restoration of normal morphological features in contrast to rats not receiving the drug. Immunohistochemical study of brain neuromarkers confirmed the restoration of the functions of neurons and astrocytes in the investigated parts of the rat's hypothalamus after the administration of carbacetam. There was a decrease in the expression level of glial markers GFAP and S-100, which illustrated the decrease in degenerative changes in the nervous tissue. While the expression level of the neuron marker NSE grew, this demonstrated the high metabolic activity of nerve cells. Changes in the expression of markers of neurons and glia indicated a restoration of normal neuronal activity under the action of carbacetam. Conclusion. Further investigation of the effects of carbacetam seems promising in terms of the restoration of neuronal function at BI.

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Engeland, Anders, Jørgen G. Bramness, Jørg Mørland, and Svetlana Skurtveit. "Veitrafikkulykker knyttet til forskrivning av legemidler:En registerbasert kohortstudie,." Norsk Epidemiologi 18, no. 2 (September 28, 2009). http://dx.doi.org/10.5324/nje.v18i2.27.

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Purpose: The aim of this study was to examine the risk of being involved in road traffic accidents as drivers among persons using prescribed medicines by utilizing data from population-based registries. The aim of the present paper was to focus on the methodology used in the study. Methods: All Norwegians aged 18-69 in April 2004 to September 2006 (3.1 million), were included in the study. Information on prescriptions, road accidents and emigrations/deaths was obtained from three different population-based registries. A total of 22,000 accidents were observed. The incidence of accidents in exposed and unexposed person-time was compared, by the standardized incidence ratio (SIR). Results: The risk of being involved in an accident was increased in persons exposed for prescribed medicines. The risk was markedly increased in persons exposed for natural opium alkaloids, benzodiazepine tranquillizers, benzodiazepine hypnotics and carisoprodol. A marginal increase or unchanged SIRs were found for NSAIDs, selective beta-2-adrenoreceptor agonists (anti-asthmatics), calcium receptor antagonists and penicillin. Conclusions: We have tested a method using different reference groups and different exposure periods to explore the association between drug use and involvement in traffic accidents. Using these methods, we have shown that exposure for prescribed opiates, benzodiazepines and carisoprodol increased the risk of being involved in an accident as driver. The findings confirm results from other studies. Further steps should be taken to reduce car driving under the influence of these drugs.

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Witt, Anette, Annika Gustavsson, and Jan Bergman. "Studies Towards the Synthesis of the Benzodiazepine Alkaloid Auranthine. Synthesis of an Acetylated Derivative." ChemInform 34, no. 26 (July 1, 2003). http://dx.doi.org/10.1002/chin.200326225.

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Ookura, Ryuhei, Keijiro Kito, Takashi Ooi, Michio Namikoshi, and Takenori Kusumi. "ChemInform Abstract: Structure Revision of Circumdatins A and B, Benzodiazepine Alkaloids Produced by Marine Fungus Aspergillus ostianus, by X-Ray Crystallography." ChemInform 39, no. 42 (October 14, 2008). http://dx.doi.org/10.1002/chin.200842200.

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Zhang, Dahai, Xiudong Yang, Jung Sook Kang, Hong Dae Choi, and Byeng Wha Son. "ChemInform Abstract: Circumdatin I, a New Ultraviolet-A Protecting Benzodiazepine Alkaloid from a Marine Isolate of the Fungus Exophiala." ChemInform 39, no. 31 (July 29, 2008). http://dx.doi.org/10.1002/chin.200831203.

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