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Sample records for action pharmacology effects

  1. Pharmacological action and mechanisms of ginkgolide B

    XIA Shi-hai; FANG Dian-chun

    2007-01-01

    Objective To review the recent research progress in pharmacological actions and mechanisms of ginkgolide B.Data sources Information included in this article was identified by searching of PUBMED (1987-2006) online resources using the key terms "ginkgolide B", "platelet activating factor", and "pharmacological".Study selection Mainly original milestone articles and critical reviews written by major pioneer investigators of the field were selected.Results The key issues related to the pharmacological actions and mechanisms of ginkgolide B were summarized. The ginkgolide B possesses a number of beneficial effects such as anti-inflammatory, anti-allergic, antioxidant, and neuroprotective effects. Meantime, their mechaniams were discussed.Conclusions The Ginkgolide B is the most potent antagonist of platelet activating factor (PAF) and exhibits therapeutic action in a variety of diseases mainly by the PAF receptor.

  2. Immunomodulatory effects of fluoxetine: A new potential pharmacological action for a classic antidepressant drug?

    Di Rosso, María Emilia; Palumbo, María Laura; Genaro, Ana María

    2016-07-01

    Selective serotonin reuptake inhibitors are frequently used antidepressants. In particular, fluoxetine is usually chosen for the treatment of the symptoms of depression, obsessive-compulsive, panic attack and bulimia nervosa. Antidepressant therapy has been associated with immune dysfunction. However, there is contradictory evidence about the effect of fluoxetine on the immune system. Experimental findings indicate that lymphocytes express the serotonin transporter. Moreover it has been shown that fluoxetine is able to modulate the immune function through a serotonin-dependent pathway and through a novel independent mechanism. In addition, several studies have shown that fluoxetine can alter tumor cell viability. Thus, it was recently demonstrated in vivo that chronic fluoxetine treatment inhibits tumor growth by increasing antitumor T-cell activity. Here we briefly review some of the literature referring to how fluoxetine is able to modify, for better or worse, the functionality of the immune system. These results of our analysis point to the relevance of the novel pharmacological action of this drug as an immunomodulator helping to treat several pathologies in which immune deficiency and/or deregulation is present. PMID:26644208

  3. The Antihyperglycemic Effects of Rhizoma Coptidis and Mechanism of Actions: A Review of Systematic Reviews and Pharmacological Research

    Hui Wang

    2014-01-01

    Full Text Available Rhizoma Coptidis (Huang Lian in Chinese pinyin is among the most widely used traditional Chinese herbal medicines and has a profound history of more than 2000 years of being used as a therapeutic herb. The antidiabetic effects of Rhizoma Coptidis have been extensively investigated in animal experiments and clinical trials and its efficacy as a promising antihyperglycemic agent has been widely discussed. In the meantime, findings from modern pharmacological studies have contributed the majority of its bioactivities to berberine, the isoquinoline alkaloids component of the herb, and a number of experiments testing the antidiabetic effects of berberine have been initiated. Therefore, we conducted a review of the current evidence profile of the antihyperglycemic effects of Rhizoma Coptidis as well as its main component berberine and the possible mechanism of actions, in order to summarize research evidence in this area and identify future research directions.

  4. Eugenol: a natural compound with versatile pharmacological actions.

    Pramod, Kannissery; Ansari, Shahid H; Ali, Javed

    2010-12-01

    Eugenol, the major constituent of clove oil, has been widely used for its anesthetic and analgesic action in dentistry. Eugenol exhibits pharmacological effects on almost all systems and our aim is to review the research work that has identified these pharmacological actions. Eugenol possesses significant antioxidant, anti-inflammatory and cardiovascular properties, in addition to analgesic and local anesthetic activity. The metabolism and pharmacokinetics of the compound in humans have been studied. Eugenol has also been used as a penetration enhancer. The compound is a very promising candidate for versatile applications, and the design of new drugs based on the pharmacological effects of eugenol could be beneficial. PMID:21299140

  5. The Chemical Constituents and Pharmacological Actions of Cordyceps sinensis.

    Liu, Yi; Wang, Jihui; Wang, Wei; Zhang, Hanyue; Zhang, Xuelan; Han, Chunchao

    2015-01-01

    Cordyceps sinensis, also called DongChongXiaCao (winter worm, summer grass) in Chinese, is becoming increasingly popular and important in the public and scientific communities. This study summarizes the chemical constituents and their corresponding pharmacological actions of Cordyceps sinensis. Many bioactive components of Cordyceps sinensis have been extracted including nucleoside, polysaccharide, sterol, protein, amino acid, and polypeptide. In addition, these constituents' corresponding pharmacological actions were also shown in the study such as anti-inflammatory, antioxidant, antitumour, antiapoptosis, and immunomodulatory actions. Therefore can use different effects of C. sinensis against different diseases and provide reference for the study of Cordyceps sinensis in the future. PMID:25960753

  6. The Chemical Constituents and Pharmacological Actions of Cordyceps sinensis

    Yi Liu

    2015-01-01

    Full Text Available Cordyceps sinensis, also called DongChongXiaCao (winter worm, summer grass in Chinese, is becoming increasingly popular and important in the public and scientific communities. This study summarizes the chemical constituents and their corresponding pharmacological actions of Cordyceps sinensis. Many bioactive components of Cordyceps sinensis have been extracted including nucleoside, polysaccharide, sterol, protein, amino acid, and polypeptide. In addition, these constituents’ corresponding pharmacological actions were also shown in the study such as anti-inflammatory, antioxidant, antitumour, antiapoptosis, and immunomodulatory actions. Therefore can use different effects of C. sinensis against different diseases and provide reference for the study of Cordyceps sinensis in the future.

  7. Lacosamide as treatment for partial epilepsy: mechanisms of action, pharmacology, effects, and safety

    Christoph Kellinghaus

    2009-09-01

    Full Text Available Christoph KellinghausDepartment of Neurology, Klinikum Osnabrück, GermanyAbstract: Lacosamide (LCM is a novel agent that has been developed as an antiepileptic drug. In vitro studies suggest that LCM modulates voltage-gated sodium channels by enhancing their slow inactivation. In addition, LCM seems to interact with collapsin-response mediator protein 2 and thus may mediate neuronal plasticity. LCM has an elimination half-life of 13 hours, no relevant protein binding, and does not induce or inhibit enzymes of the cytochrome P450 system. No clinically significant drug–drug interactions have been discovered as yet. Experimental data suggest anticonvulsant as well as analgesic effects. Large clinical studies have demonstrated its efficacy for treatment of patients with partial seizures. LCM is well tolerated, and the most common adverse events are unspecific central nervous system and gastrointestinal effects such as dizziness, vertigo, nausea, and headache. LCM is approved for treatment of partial seizures with or without secondary generalization in the United States and the European Union within a dose range of 200 to 400 mg per day, administered twice daily. In addition to the oral formulations, an intravenous infusion solution is available.Keywords: lacosamide, epilepsy, antiepileptic drug

  8. Pharmacological actions of statins: potential utility in COPD

    T. E. Eaton

    2009-12-01

    Full Text Available Chronic obstructive pulmonary disease (COPD is characterised by minimally reversible airflow limitation and features of systemic inflammation. Current therapies for COPD have been shown to reduce symptoms and infective exacerbations and to improve quality of life. However, these drugs have little effect on the natural history of the disease (progressive decline in lung function and exercise tolerance and do not improve mortality. The anti-inflammatory effects of statins on both pulmonary and systemic inflammation through inhibition of guanosine triphosphatase and nuclear factor-B mediated activation of inflammatory and matrix remodelling pathways could have substantial benefits in patients with COPD due to the following. 1 Inhibition of cytokine production (tumour necrosis factor-, interleukin (IL-6 and IL-8 and neutrophil infiltration into the lung; 2 inhibition of the fibrotic activity in the lung leading to small airways fibrosis and irreversible airflow limitation; 3 antioxidant and anti-inflammatory (IL-6 mediated effects on skeletal muscle; 4 reduced inflammatory response to pulmonary infection; and 5 inhibition of the development (or reversal of epithelial-mesenchymal transition, a precursor event to lung cancer. This review examines the pleiotropic pharmacological action of statins which inhibit key inflammatory and remodelling pathways in COPD and concludes that statins have considerable potential as adjunct therapy in COPD.

  9. Pharmacological actions of statins: potential utility in COPD.

    Young, R P; Hopkins, R; Eaton, T E

    2009-12-01

    Chronic obstructive pulmonary disease (COPD) is characterised by minimally reversible airflow limitation and features of systemic inflammation. Current therapies for COPD have been shown to reduce symptoms and infective exacerbations and to improve quality of life. However, these drugs have little effect on the natural history of the disease (progressive decline in lung function and exercise tolerance) and do not improve mortality. The anti-inflammatory effects of statins on both pulmonary and systemic inflammation through inhibition of guanosine triphosphatase and nuclear factor-κB mediated activation of inflammatory and matrix remodelling pathways could have substantial benefits in patients with COPD due to the following. 1) Inhibition of cytokine production (tumour necrosis factor-α, interleukin (IL)-6 and IL-8) and neutrophil infiltration into the lung; 2) inhibition of the fibrotic activity in the lung leading to small airways fibrosis and irreversible airflow limitation; 3) antioxidant and anti-inflammatory (IL-6 mediated) effects on skeletal muscle; 4) reduced inflammatory response to pulmonary infection; and 5) inhibition of the development (or reversal) of epithelial-mesenchymal transition, a precursor event to lung cancer. This review examines the pleiotropic pharmacological action of statins which inhibit key inflammatory and remodelling pathways in COPD and concludes that statins have considerable potential as adjunct therapy in COPD. PMID:20956147

  10. The Chemical Constituents and Pharmacological Actions of Cordyceps sinensis

    Yi Liu; Jihui Wang; Wei Wang; Hanyue Zhang; Xuelan Zhang; Chunchao Han

    2015-01-01

    Cordyceps sinensis, also called DongChongXiaCao (winter worm, summer grass) in Chinese, is becoming increasingly popular and important in the public and scientific communities. This study summarizes the chemical constituents and their corresponding pharmacological actions of Cordyceps sinensis. Many bioactive components of Cordyceps sinensis have been extracted including nucleoside, polysaccharide, sterol, protein, amino acid, and polypeptide. In addition, these constituents’ corresponding ph...

  11. CURCUMIN- PHARMACOLOGICAL ACTIONS AND ITS ROLE IN DENTISTRY

    SHARMILA DEVI DEVARAJ, PRASANNA NEELAKANTAN

    2014-05-01

    Full Text Available Turmeric (Curcuma longa is an ancient dye, flavouring and medical herb, widely used in Asian countries. It is a herb that has been widely used in Indian medicine, cookery, and cosmetics. The main component of turmeric is curcumin. Curcumin has a surprisingly wide range of beneficial properties includes anti inflammatory, antioxidant, chemopreventive, chemotherapeutic activity etc.  The activity of curcumin derived from its complex chemistry as well as its ability to influence the multiple signalling pathways. This review article is to highlight the pharmacological action and its therapeutic role in dentistry.   

  12. Pharmacological effects of Sapindus mukorossi.

    Upadhyay, Aparna; Singh, D K

    2012-01-01

    Sapindus mukorossi is an extremely valuable medicinal plant, distributed in tropical and sub-tropical regions of Asia. The aim of present review is to form a short compilation of the phytochemical composition and pharmacological properties of this multipurpose tree. The main phytoconstituents isolated and identified from different parts of this plant are triterpenoidal saponins of oleanane, dammarane and tirucullane type. The structure and chemical names of all the types of triterpenoidal saponins reported in Sapindus mukorossi are included in this review. Many research studies have been conducted to prove the plant's potential as being spermicidal, contraceptive, hepatoprotective, emetic, anti-inflammatory and anti-protozoal. The present review highlights some of the salient pharmacological uses of Sapindus mukorossi. PMID:22983291

  13. Pharmacological effects of Sapindus mukorossi

    Aparna Upadhyay

    2012-10-01

    Full Text Available Sapindus mukorossi is an extremely valuable medicinal plant, distributed in tropical and sub-tropical regions of Asia. The aim of present review is to form a short compilation of the phytochemical composition and pharmacological properties of this multipurpose tree. The main phytoconstituents isolated and identified from different parts of this plant are triterpenoidal saponins of oleanane, dammarane and tirucullane type. The structure and chemical names of all the types of triterpenoidal saponins reported in Sapindus mukorossi are included in this review. Many research studies have been conducted to prove the plant's potential as being spermicidal, contraceptive, hepatoprotective, emetic, anti-inflammatory and anti-protozoal. The present review highlights some of the salient pharmacological uses of Sapindus mukorossi.

  14. Pharmacological effects of Sapindus mukorossi

    Aparna Upadhyay; D K Singh

    2012-01-01

    Sapindus mukorossi is an extremely valuable medicinal plant, distributed in tropical and sub-tropical regions of Asia. The aim of present review is to form a short compilation of the phytochemical composition and pharmacological properties of this multipurpose tree. The main phytoconstituents isolated and identified from different parts of this plant are triterpenoidal saponins of oleanane, dammarane and tirucullane type. The structure and chemical names of all the types of triterpenoidal sap...

  15. Cato Guldberg and Peter Waage, the history of the Law of Mass Action, and its relevance to clinical pharmacology.

    Ferner, Robin E; Aronson, Jeffrey K

    2016-01-01

    We have traced the historical link between the Law of Mass Action and clinical pharmacology. The Law evolved from the work of the French chemist Claude Louis Berthollet, was first formulated by Cato Guldberg and Peter Waage in 1864 and later clarified by the Dutch chemist Jacobus van 't Hoff in 1877. It has profoundly influenced our qualitative and quantitative understanding of a number of physiological and pharmacological phenomena. According to the Law of Mass Action, the velocity of a chemical reaction depends on the concentrations of the reactants. At equilibrium the concentrations of the chemicals involved bear a constant relation to each other, described by the equilibrium constant, K. The Law of Mass Action is relevant to various physiological and pharmacological concepts, including concentration-effect curves, dose-response curves, and ligand-receptor binding curves, all of which are important in describing the pharmacological actions of medications, the Langmuir adsorption isotherm, which describes the binding of medications to proteins, activation curves for transmembrane ion transport, enzyme inhibition and the Henderson-Hasselbalch equation, which describes the relation between pH, as a measure of acidity and the concentrations of the contributory acids and bases. Guldberg and Waage recognized the importance of dynamic equilibrium, while others failed to do so. Their ideas, over 150 years old, are embedded in and still relevant to clinical pharmacology. Here we explain the ideas and in a subsequent paper show how they are relevant to understanding adverse drug reactions. PMID:26174880

  16. Pharmacological effects of medicinal plants on skin

    Zohreh Bakhtiyari, MSc; Mohammadreza Radan, MD

    2013-01-01

    Skin is one of the most sensitive parts of the body and is important to maintain the beauty of man. Herbal products have fewer side effects than chemicals and have pharmacological effects on the skin, so are used in cosmetic preparations. Books, articles and electronic databases including ISI Web of Science, PubMed, Magiran and IranMedex were searched to identify plants with positive effects on the skin, regardless of adverse effects and their interactions. A number of plants which were...

  17. Effectiveness of Psychological and Pharmacological Treatments for Nocturnal Enuresis.

    Houts, Arthur C.; And Others

    1994-01-01

    Assesses overall effectiveness of psychological and pharmacological treatments, relative effectiveness of specific treatments, and moderators of treatment effectiveness for nocturnal enuretic children via quantitative integration of research. Findings confirm that more children benefit from psychological than from pharmacological interventions and…

  18. Êxtase (MDMA: efeitos farmacológicos e tóxicos, mecanismo de ação e abordagem clínica Ecstasy (MDMA: pharmacological and toxic effects, mechanism of action and clinical management

    Caroline Addison Carvalho Xavier

    2008-01-01

    Full Text Available CONTEXTO: O 3,4-metilenodioximetanfetamina (MDMA, êxtase é um derivado da anfetamina, cujo consumo por jovens tem aumentado. OBJETIVOS: Conduzir uma revisão de literatura sobre os aspectos farmacológicos e fisiopatológicos do MDMA, incluindo o mecanismo de ação que possa explicar os efeitos neurotóxicos e a toxicidade aguda e a longo prazo. MÉTODOS: Revisão da literatura usando as palavras-chave: 3,4-methylenedioxymethamphetamine, ecstasy, neurotoxicity, intoxication, drug abuse, por intermédio do MEDLINE e LILACS. A busca incluiu todos os artigos publicados no período entre 1985 e 2007. RESULTADOS: Ainda existem muitas questões sem respostas sobre a farmacologia do êxtase e a fisiopatologia dos efeitos tóxicos dessa substância. A simples descrição do mecanismo de ação é insuficiente para explicar todos os efeitos induzidos pelo êxtase. O mecanismo exato responsável por mediar os efeitos tóxicos do MDMA sobre os neurônios da serotonina precisa ser elucidado. CONCLUSÕES: Existem poucas informações na literatura sobre a farmacologia e o mecanismo de ação do MDMA que possam explicar os efeitos neurotóxicos e outros efeitos fisiopatológicos. São necessários mais estudos para que o profissional de saúde possa obter informações e conhecimentos a fim de combater os efeitos terríveis do êxtase na população jovem vulnerável.BACKGROUND: The consumption of the amphetamine derivative 3,4-methylenedioxymethamphetamine (MDMA, ecstasy by young people increased in the past years. OBJECTIVES: To conduct a literature review on the pharmacology of MDMA and particularly with respect to the putative mechanism of action implicated in the acute and long-term toxicity and neurotoxic effects. METHODS: A literature review using the key words: 3,4-methylenedioxymethamphetamine, ecstasy, neurotoxicity, intoxication, abuse drugs was performed in the databases MEDLINE and LILACS. The search covered all articles published between 1985

  19. Relaxin for the Treatment of Acute Decompensated Heart Failure: Pharmacology, Mechanisms of Action, and Clinical Evidence.

    Ng, Tien M H; Goland, Sorel; Elkayam, Uri

    2016-01-01

    Acute heart failure remains a major cause of morbidity, and its treatment requires an increasing investment of the health care system. Whereas success in treating chronic heart failure has been achieved over the last decades, several pharmacological approaches for acute heart failure have been introduced but have failed to demonstrate any clinical benefit. Serelaxin is a recombinant human relaxin-2 vasoactive peptide that causes systemic and renal vasodilation. Data suggest that the clinical benefits may be attributable to a potential combination of multiple actions of serelaxin, including improving systemic, cardiac, and renal hemodynamics, and protecting cells and organs from damage via neurohormonal, anti-inflammatory, antiremodeling, antifibrotic, anti-ischemic, and proangiogenic effects. Recently, a number of clinical trials have demonstrated that serelaxin infusion over 48 hours improved dyspnea with more rapid relief of congestion during the first days after admission for heart failure. In addition, administration of serelaxin diminished cardiac, renal, and hepatic damage, which were associated with improved long-term mortality. Available data support substantial clinical benefits and significant promise for serelaxin as a treatment option for patients with acute heart failure. This review focuses on the pharmacology and mechanisms of action of serelaxin and provides a detailed discussion of the clinical evidence for this novel therapy in acute heart failure. PMID:26331289

  20. Pharmacology of new oral anticoagulants: mechanism of action, pharmacokinetics, pharmacodynamics

    Luca Masotti

    2013-12-01

    Full Text Available Due to their mechanism of action, the new oral anticoagulants are named direct oral anticoagulants (DOACs. Dabigatran is a selective, competitive, direct inhibitor of thrombin (Factor IIa while rivaroxaban, apixaban and edoxaban act by directly inhibiting the activated Factor X (FXa in a selective and competitive manner. DOACs have a relatively short half-life and almost immediate anticoagulant activity, and rapidly reach the plasma peak concentration. Therefore, they do not need a phase of overlapping with parenteral anticoagulants. After their withdrawal, their removal is sufficiently rapid, although influenced by renal function. Dabigatran is the only DOACs to be administered as a pro-drug and becomes active after drug metabolization. The route of elimination of dabigatran is primarily renal, whereas FXa inhibitors are mainly eliminated by the biliary-fecal route. The drug interactions of DOACs are mainly limited to drugs that act on P-glycoprotein for dabigatran and on P-glycoprotein and/or cytochrome P3A4 for anti-Xa. DOACs have no interactions with food. Given their linear pharmacodynamics, with a predictable dose/response relationship and anticoagulant effect, DOACs are administered at a fixed dose and do not require routine laboratory monitoring.

  1. [Comparison with the pharmacological actions of Morinda officinalis, Damnacanthus officinarum and Schisandra propinqua].

    Qiao, Z S; Wu, H; Su, Z W

    1991-07-01

    There are three kinds of plants, Morinda officinalis (1), Damnacanthus officinarum (2), and Schisandra propinqua (3) whose roots have been used since the ancient time. In this paper, some of their pharmacological actions that are related to tonifying and invigorating Yang were examined and compared. The body weight, the thymus weight, the amount of leukocyte in the blood, and the continuing swimming times of the young mice could be increased with the oral administration of the water extractions of (1) and (2) (P less than 0.05-0.001). The Rt of M-receptor in the brains of the hypothyroidism mice were decreased after administration of the water extracts of (1) and (2) (P less than 0.05). (1) could also increased the amount of leukocyte in the blood of leukocytopenia mice caused by radiation of gamma-ray (P less than 0.01). (3) has not shown the obvious effects (P greater than 0.05). The results indicate that (1) and (2) have the ability of anti-fatigue, improving the immunological action of the young mice, and reducing the excitability of the para-sympathetic nervous system of the hypothyroidism mice through decreasing the Rt of M-receptor in their brains. All of them did not show acute toxicity, inducing mutation, and sexual hormone like actions. PMID:1914038

  2. Gas chromatographic mass analysis and further pharmacological actions of Cymbopogon proximus essential oil.

    Al-Taweel, A M; Fawzy, G A; Perveen, S; El Tahir, K E H

    2013-09-01

    The present study reports Gas chromatographic mass analysis (GC-MS) as well as important biological activities of Cymbopogon proximus essential oil. The chemical composition of the essential oil of Cymbopogon proximus was investigated by GC-MS. Furthermore, the effects of Cymbopogon proximus essential oil on the cardiac parasympathetic ganglia in rats, the intra-tracheal pressure in guinea-pigs and on carrageenan-induced inflammation in the rats paw, were studied. The GC-MS study led to the identification of 22 components with Piperitone representing (73.81%), Elemol (9.32%), alpha-Eudesmol (5.21%) and alpha-Terpineol (3.01%) of the oils composition. The percentage protective effect of the oil on the vagus-induced bradycardia in rats was 90.1±3.1%, which represents a significant protection. As for the effect of Cymbopogon oil on bronchoconstrictors-induced increase in intra-tracheal pressure in guinea-pigs, the oil antagonized the actions of 5-HT and histamine by 80±3.7 and 93±8.3%, respectively. Pharmacological investigations using Cymbopogon oil revealed its inherent ability to possess a bronchodilator activity mediated via blockade of both histamine and serotonin receptors. It possessed a significant ganglionic blocking action and a limited anti-inflammatory activity that seemed to involve blockade of histamine and serotonin receptors in the rats' paws. PMID:23780497

  3. Effective actions near singularities

    We study the heterotic string compactified on K3x T2 near the line T=U, where the effective action becomes singular due to an SU(2) gauge symmetry enhancement. By 'integrating in' the light W± vector multiplets we derive a quantum corrected effective action which is manifestly SU(2) invariant and non-singular. This effective action is found to be consistent with a residual SL(2,Ζ) quantum symmetry on the line T=U. In an appropriate decompactification limit, we recover the known SU(2) invariant action in five dimensions. (author)

  4. Pills or push-ups? Effectiveness and public perception of pharmacological and non-pharmacological cognitive enhancement.

    Caviola, L.; Faber, NS

    2015-01-01

    We review work on the effectiveness of different forms of cognitive enhancement, both pharmacological and non-pharmacological. We consider caffeine, methylphenidate, and modafinil for pharmacological cognitive enhancement (PCE) and computer training, physical exercise, and sleep for non-pharmacological cognitive enhancement (NPCE). We find that all of the techniques described can produce significant beneficial effects on cognitive performance. However, effect sizes are moderate, and consisten...

  5. Pills or Push-Ups? Effectiveness and Public Perception of Pharmacological and Non-Pharmacological Cognitive Enhancement

    Caviola, Lucius; Nadira S. Faber

    2015-01-01

    We review work on the effectiveness of different forms of cognitive enhancement, both pharmacological and non-pharmacological. We consider caffeine, methylphenidate, and modafinil for pharmacological cognitive enhancement (PCE) and computer training, physical exercise, and sleep for non-pharmacological cognitive enhancement (NPCE). We find that all of the techniques described can produce significant beneficial effects on cognitive performance. However, effect sizes are moderate, and consisten...

  6. Pills or push-ups? Effectiveness and public perception of pharmacological and non-pharmacological cognitive enhancement

    Lucius eCaviola; Nadira S. Faber

    2015-01-01

    We review work on the effectiveness of different forms of cognitive enhancement, both pharmacological and non-pharmacological. We consider caffeine, methylphenidate, and modafinil for pharmacological cognitive enhancement (PCE) and computer training, physical exercise, and sleep for non-pharmacological cognitive enhancement (NPCE). We find that all of the techniques described can produce significant beneficial effects on cognitive performance. However, effect sizes are moderate, and consisten...

  7. Systems pharmacology dissection of multi-scale mechanisms of action for herbal medicines in stroke treatment and prevention.

    Jingxiao Zhang

    Full Text Available Annually, tens of millions of first-ever strokes occur in the world; however, currently there is lack of effective and widely applicable pharmacological treatments for stroke patients. Herbal medicines, characterized as multi-constituent, multi-target and multi-effect, have been acknowledged with conspicuous effects in treating stroke, and attract extensive interest of researchers although the mechanism of action is yet unclear. In this work, we introduce an innovative systems-pharmacology method that combines pharmacokinetic prescreening, target fishing and network analysis to decipher the mechanisms of action of 10 herbal medicines like Salvia miltiorrhizae, Ginkgo biloba and Ephedrae herba which are efficient in stroke treatment and prevention. Our systematic analysis results display that, in these anti-stroke herbal medicines, 168 out of 1285 constituents with the favorable pharmacokinetic profiles might be implicated in stroke therapy, and the systematic use of these compounds probably acts through multiple mechanisms to synergistically benefit patients with stroke, which can roughly be classified as preventing ischemic inflammatory response, scavenging free radicals and inhibiting neuronal apoptosis against ischemic cerebral damage, as well as exhibiting lipid-lowering, anti-diabetic, anti-thrombotic and antiplatelet effects to decrease recurrent strokes. Relying on systems biology-based analysis, we speculate that herbal medicines, being characterized as the classical combination therapies, might be not only engaged in multiple mechanisms of action to synergistically improve the stroke outcomes, but also might be participated in reducing the risk factors for recurrent strokes.

  8. Psychedelic 5-methoxy-N,N-dimethyltryptamine: metabolism, pharmacokinetics, drug interactions, and pharmacological actions.

    Shen, Hong-Wu; Jiang, Xi-Ling; Winter, Jerrold C; Yu, Ai-Ming

    2010-10-01

    5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) belongs to a group of naturally-occurring psychoactive indolealkylamine drugs. It acts as a nonselective serotonin (5-HT) agonist and causes many physiological and behavioral changes. 5-MeO-DMT is O-demethylated by polymorphic cytochrome P450 2D6 (CYP2D6) to an active metabolite, bufotenine, while it is mainly inactivated through the deamination pathway mediated by monoamine oxidase A (MAO-A). 5-MeO-DMT is often used with MAO-A inhibitors such as harmaline. Concurrent use of harmaline reduces 5-MeO-DMT deamination metabolism and leads to a prolonged and increased exposure to the parent drug 5-MeO-DMT, as well as the active metabolite bufotenine. Harmaline, 5-MeO-DMT and bufotenine act agonistically on serotonergic systems and may result in hyperserotonergic effects or serotonin toxicity. Interestingly, CYP2D6 also has important contribution to harmaline metabolism, and CYP2D6 genetic polymorphism may cause considerable variability in the metabolism, pharmacokinetics and dynamics of harmaline and its interaction with 5-MeO-DMT. Therefore, this review summarizes recent findings on biotransformation, pharmacokinetics, and pharmacological actions of 5-MeO-DMT. In addition, the pharmacokinetic and pharmacodynamic drug-drug interactions between harmaline and 5-MeO-DMT, potential involvement of CYP2D6 pharmacogenetics, and risks of 5-MeO-DMT intoxication are discussed. PMID:20942780

  9. Life-history responses of Daphnia magna Straus to binary mixtures of toxic substances: Pharmacological versus ecotoxicological modes of action

    Two prevailing theoretical models: concentration addition (CA) and independent action (IA), predict mixture toxicity on the basis of known toxicities of the mixture components. To date, both models have been in most occasions evaluated using unicellular in vivo responses or biochemical in vitro responses. However, when considering more complex models such as the whole organism physiology or life-history traits, the dominant ecotoxicological mode of action, based on the exposure concentrations at which various toxicological effects become operative at the level of whole organism, should be considered. Offspring production in Daphnia magna is driven by the resources acquired from food, and the number of live offspring produced by an organism is the result of two independent factors: the number of eggs produced and the percentage of eggs that survive egg development. In this study joint toxicity effects on offspring production in D. magna were tested using binary mixtures of toxic contaminants known to specifically impair food acquisition (λ-cyhalothrin and cadmium) or to cause egg mortality during development (3,4 dichloroaniline). Tests were performed using a simplified 10-day reproduction assay initiated with gravid females. The results obtained indicate that irrespective of their primary pharmacological mode of action, the joint toxicity of cadmium and λ-cyhalothrin was predicted by the CA model, whereas the joint toxicity of cadmium and 3,4 dichloroaniline was predicted by the IA model. Thus, the results obtained indicate that for life-history traits such as reproduction responses, the dominant ecotoxicological rather than the pharmacological mode of action should be used for predicting joint mixture effects

  10. Pharmacological Actions of Glucagon-Like Peptide-1, Gastric Inhibitory Polypeptide, and Glucagon.

    Sekar, R; Singh, K; Arokiaraj, A W R; Chow, B K C

    2016-01-01

    Glucagon family of peptide hormones is a group of structurally related brain-gut peptides that exert their pleiotropic actions through interactions with unique members of class B1 G protein-coupled receptors (GPCRs). They are key regulators of hormonal homeostasis and are important drug targets for metabolic disorders such as type-2 diabetes mellitus (T2DM), obesity, and dysregulations of the nervous systems such as migraine, anxiety, depression, neurodegeneration, psychiatric disorders, and cardiovascular diseases. The current review aims to provide a detailed overview of the current understanding of the pharmacological actions and therapeutic advances of three members within this family including glucagon-like peptide-1 (GLP-1), gastric inhibitory polypeptide (GIP), and glucagon. PMID:27572131

  11. Evidence from pharmacology and pathophysiology suggests that chemicals with dissimilar mechanisms of action could be of bigger concern in the toxicological risk assessment of chemical mixtures than chemicals with a similar mechanism of action

    Hadrup, Niels

    2014-01-01

    cancer or HIV, it is generally recognised that pharmacological combination therapy targeting different mechanisms of action is more effective than a strategy where only one mechanism is targeted. Moreover, in diseases such as acute myocardial infarction and congestive heart failure, several organ systems...

  12. Bioactive Compounds of Aristotelia chilensis Stuntz and their Pharmacological Effects.

    Romanucci, Valeria; D'Alonzo, Daniele; Guaragna, Annalisa; Di Marino, Cinzia; Davinelli, Sergio; Scapagnini, Giovanni; Di Fabio, Giovanni; Zarrelli, Armando

    2016-01-01

    Aristotelia chilensis ([Molina], Stuntz) a member of the family Eleocarpaceae, is a plant native to Chile that is distributed in tropical and temperate Asia, Australia, the Pacific Area, and South America. The juice of its berries has important medicinal properties, as an astringent, tonic, and antidiarrhoeal. Its many qualities make the maqui berry the undisputed sovereign of the family of so-called "superfruits", as well as a valuable tool to combat cellular inflammation of bones and joints. Recently, it is discovered that the leaves of the maqui berry have important antibacterial and antitumour activities. This review provides a comprehensive overview of the traditional use, phytochemistry, and biological activity of A. chilensis using information collected from scientific journals, books, and electronic searches. Anthocyanins, other flavonoids, alkaloids, cinnamic acid derivatives, benzoic acid derivatives, other bioactive molecules, and mineral elements are summarized. A broad range of activities of plant extracts and fractions are presented, including antioxidant activity, inhibition of visible light-induced damage of photoreceptor cells, inhibition of α-glucosidase, inhibition of pancreatic lipase, anti-diabetic effects, anti-inflammatory effects, analgesic effects, anti-diabetes, effective prevention of atherosclerosis, promotion of hair growth, anti-photo ageing of the skin, and inhibition of lipid peroxidation. Although some ethnobotanical uses have been supported in in vitro experiments, further studies of the individual compounds or chemical classes of compounds responsible for the pharmacological effects and the mechanisms of action are necessary. In addition, the toxicity and the side effects from the use of A. chilensis, as well as clinical trials, require attention. PMID:26778456

  13. Hordenine: pharmacology, pharmacokinetics and behavioural effects in the horse.

    Frank, M; Weckman, T J; Wood, T; Woods, W E; Tai, C L; Chang, S L; Ewing, A; Blake, J W; Tobin, T

    1990-11-01

    Hordenine is an alkaloid occurring naturally in grains, sprouting barley, and certain grasses. It is occasionally found in post race urine samples, and therefore we investigated its pharmacological actions in the horse. Hordenine (2.0 mg/kg bodyweight [bwt]) was administered by rapid intravenous (iv) injection to 10 horses. Typically, dosed horses showed a flehmen response and defecated within 60 secs. All horses showed substantial respiratory distress. Respiratory rates increased about 250 per cent and heart rates were approximately double that of resting values. All animals broke out in a sweat shortly after iv injection, but basal body temperature was not affected. These effects were transient, and the animals appeared normal within 30 mins of dosing. Treated horses were tested in a variable interval responding apparatus 30 mins after dosing and no residual stimulation or depressant effects of hordenine were apparent. Animals dosed orally with 2.0 mg/kg bwt of hordenine showed no changes in heart rate, respiratory rate, basal body temperature or behaviour. After iv injection of hordenine, (2.0 mg/kg bwt) plasma reached a maximum value of about 1.0 micrograms/ml, and declined thereafter in a biexponential fashion. Kinetics of plasma concentration satisfied the concept of a two compartment open system, with an alpha-phase half-life of about 3 mins, and a beta-phase half-life of about 35 mins. Total urinary concentrations of hordenine (free and conjugated) peaked at about 400 micrograms/ml, and then declined exponentially to background levels by 24 h after dosing.(ABSTRACT TRUNCATED AT 250 WORDS) PMID:2269269

  14. Parameter Trajectory Analysis to Identify Treatment Effects of Pharmacological Interventions

    Tiemann, Christian A.; Vanlier, Joep; Oosterveer, Maaike H.; Albert K Groen; Hilbers, Peter A. J.; Natal A W van Riel

    2013-01-01

    The field of medical systems biology aims to advance understanding of molecular mechanisms that drive disease progression and to translate this knowledge into therapies to effectively treat diseases. A challenging task is the investigation of long-term effects of a (pharmacological) treatment, to establish its applicability and to identify potential side effects. We present a new modeling approach, called Analysis of Dynamic Adaptations in Parameter Trajectories (ADAPT), to analyze the long-t...

  15. Sodium selenite and cancer related lymphedema: Biological and pharmacological effects.

    Pfister, Christina; Dawzcynski, Horst; Schingale, Franz-Josef

    2016-09-01

    A significant percentage of cancer patients develop secondary lymphedema after surgery or radiotherapy. The preferred treatment of secondary lymphedema is complex physical therapy. Pharmacotherapy, for example with diuretics, has received little attention, because they were not effective and only offered short-term solutions. Sodium selenite showed promise as a cost-effective, nontoxic anti-inflammatory agent. Treatment with sodium selenite lowers reactive oxygen species (ROS) production, causes a spontaneous reduction in lymphedema volume, increases the efficacy of physical therapy for lymphedema, and reduces the incidence of erysipelas infections in patients with chronic lymphedema. Besides biological effects in reducing excessive production of ROS, sodium selenite also displays various pharmacological effects. So far the exact mechanisms of these pharmacological effects are mostly unknown, but probably include inhibition of adhesion protein expression. PMID:27267968

  16. (-)-Carvone: antispasmodic effect and mode of action.

    Souza, Fábia Valéria M; da Rocha, Marcelly Barbosa; de Souza, Damião P; Marçal, Rosilene Moretti

    2013-03-01

    (-)-Carvone is a monoterpene ketone found in spearmint (Mentha spicata var. crispa) essential oil that is widely used as an odor and flavor additive. An intestinal antispasmodic effect was recently reported for (-)-carvone, and it has been shown to be more potent than its (+)-antipode. The mechanism of (-)-carvone action in the intestines has not been investigated. To gain a better understanding of the (-)-carvone antispasmodic effect, we investigated its pharmacological effects in the guinea pig ileum. Terminal portions of the ileum were mounted for isotonic contraction recordings. The effect of (-)-carvone was compared with that of the classical calcium channel blocker (CCB) verapamil. In isolated ileal smooth muscle, (-)-carvone did not produce direct contractile or relaxation responses and did not modify electrically elicited contractions or low K(+)-evoked contractions. The submaximal contractions induced by histamine (p<0.001), BaCl2 (p<0.05), and carbachol (p<0.01) were significantly reduced by (-)-carvone. The contractile response elicited by high concentrations of carbachol was reduced but not abolished by (-)-carvone. No additive action was detected with co-incubation of (-)-carvone and verapamil on carbachol-induced contraction. (-)-Carvone reduced the contraction induced by high K(+) and was almost 100 times more potent than verapamil. Thus, (-)-carvone showed a typical and potent CCB-like action. Many effects described for both (-)-carvone and spearmint oil can be explained as a CCB-like mode of action. PMID:23103297

  17. Carum copticum L.: a herbal medicine with various pharmacological effects.

    Boskabady, Mohammad Hossein; Alitaneh, Saeed; Alavinezhad, Azam

    2014-01-01

    Carum copticum L. commonly known as "Ajwain" is cultivated in many regions of the world including Iran and India, states of Gujarat and Rajasthan. Traditionally, C. copticum has been used in the past for various therapeutic effects including bloating, fatigue, diarrhea, abdominal tumors, abdominal pain, respiratory distress, and loss of appetite. It has other health benefits such as antifungal, antioxidant, antibacterial, antiparasitic, and hypolipidemic effects. This plant contains different important components such as carbohydrates, glucosides, saponins and phenolic compounds (carvacrol), volatile oils (thymol), terpiene, paracymene and beta-pinene, protein, fat, fiber, and minerals including calcium, phosphorus, iron, and nicotinic acid (niacin). In the previous studies, several pharmacological effects were shown for C. copticum. Therefore, in this paper, the pharmacological effects of the plant were reviewed. PMID:25089273

  18. Acetaminophen from liver to brain: New insights into drug pharmacological action and toxicity.

    Ghanem, Carolina I; Pérez, María J; Manautou, José E; Mottino, Aldo D

    2016-07-01

    Acetaminophen (APAP) is a well-known analgesic and antipyretic drug. It is considered to be safe when administered within its therapeutic range, but in cases of acute intoxication, hepatotoxicity can occur. APAP overdose is the leading cause of acute liver failure in the northern hemisphere. Historically, studies on APAP toxicity have been focused on liver, with alterations in brain function attributed to secondary effects of acute liver failure. However, in the last decade the pharmacological mechanism of APAP as a cannabinoid system modulator has been documented and some articles have reported "in situ" toxicity by APAP in brain tissue at high doses. Paradoxically, low doses of APAP have been reported to produce the opposite, neuroprotective effects. In this paper we present a comprehensive, up-to-date overview of hepatic toxicity as well as a thorough review of both toxic and beneficial effects of APAP in brain. PMID:26921661

  19. Pharmacological Drug Delivery Strategies for Improved Therapeutic Effects: Recent Advances.

    Savaliya, Reema; Singh, Poornima; Singh, Sanjay

    2016-01-01

    The latest pharmacologic research has resulted number of new molecules with the potential to modernize the prevention or treatment of different complex diseases, including cancer. The therapeutics generally include moieties such as proteins, drugs and genes, etc. Current activities in the pharmacological field include the development of novel drug-delivery systems to overcome pharmacokinetic glitches such as limited bioavailability, unwanted distribution, drug resistant, and stability, etc. Therefore, to address these issues various biotechnological and pharmacological techniques has been introduced. However, effective drug delivery with improved efficacy remains challenging. This review is focused towards different strategies such as physical and biological methods for efficacious delivery at desired tissues and even sub-cellular targeting. Emphasis is also given about nanotechnology based drug or gene delivery strategies and co-delivery of drug-drug; gene-gene or combinations of drug-gene, etc. are the current cuttingedge methods, which are under clinical or pre-clinical stage of research. Uses of biodegradable materials, such as liposomes and polymeric particles are another class of drug delivery vehicles, which have shown tremendous success, are also discussed. Towards the end, future directions of pharmacological drug delivery methods have also been summarized. PMID:26654439

  20. Verapamil for cluster headache. Clinical pharmacology and possible mode of action

    Tfelt-Hansen, Peer; Tfelt-Hansen, Jacob

    2009-01-01

    Verapamil is used mainly in cardiovascular diseases. High-dose verapamil (360-720 mg) is, however, currently the mainstay in the prophylactic treatment of cluster headache. The oral pharmacokinetics are variable. The pharmacodynamic effect of verapamil, the effect on blood pressure, also varies...... is therefore limited. The clinical use of verapamil in cluster headache is reviewed and several relevant drug interactions are mentioned. Finally, its possible mode of action in cluster headache is discussed. The effect of verapamil in cluster headache most likely takes place in the hypothalamus...... certain mode of action of the drug in cluster headache....

  1. Pharmacological effects of two cytolysins isolated from the sea anemone Stichodactyla helianthus

    T García; D Martinez; A Palmero; C Soto; M Tejuca; F Pazos; R Menéndez; C Alvarez; A Garateix

    2009-12-01

    Sticholysins I and II (St I/II) are cytolysins purified from the sea anemone Stichodactyla helianthus. In this study, we show their pharmacological action on guinea-pig and snail models in native and pH-denatured conditions in order to correlate the pharmacological findings with the pore-forming activity of both isoforms. In guinea-pig erythrocytes ( = 3), St II possessed higher haemolytic activity in comparison with St I and this activity was lost at an alkaline pH. In molluscan central neurons ( = 30), they irreversibly decreased the amplitude of the cholinergic response; St I (EC50 0.6 molL–1) was more potent than St II (EC50 > 6.6 molL–1) and they both increased the duration of the action potential; these effects were absent at an alkaline pH. In guinea-pig isolated atrium ( = 25), both increased the amplitude of the contraction force, but St II was more potent than St I (EC50 0.03 molL–1 and 0.3 molL–1, respectively) and this effect persisted at an alkaline pH. In summary, both cytolysins have neuroactive and cardioactive properties. The main mechanism in molluscan neurons seems to be associated with the cytolytic activity of these molecules, whereas in guinea-pig atrium, the existence of an additional pharmacological mechanism might be contributing to the observed effect.

  2. [Research progress of trans-cinnamaldehyde pharmacological effects].

    Zhang, Li-qing; Zhang, Zhan-gang; Fu, Yan; Xu, Ying

    2015-12-01

    Trans-cinnamaldehyde, the main component of volatile oil from cassia twig or Cinnamomum cassia, which is a traditional Chinese herbal medicine. Trans-cinnamaldehyde is a kind olefine aldehyde of organic compounds and has many pharmacological properties, such as anti-inflammatory, anti-tumor, anti-bacterial, antidiabetic, anti-obesity, and neuroprotection etc. The compound has preventive and therapeutic effects on the nervous system, cardiovascular, cancer, diabetes and other diseases. Trans-cinnamaldehyde, as a preventive care of nature medicine, has great clinical and market potential. This paper gives a review about the pharmacological effects and mechanism of trans-cinnamaldehyde researched in the latest five years. We hope to provide some basic information for further research on trans-cinnamaldehyde. PMID:27141665

  3. Effects of Security actions

    Bergman, Ramona; Andersson-Sköld, Yvonne; Nyberg, Lars; Johansson, Magnus

    2010-05-01

    In a project funded by the Swedish Civil Contingencies Agency, the effort and work to reduce different kinds of accidents are being evaluated. The project wants to illuminate the links between actions and outcome, so we can learn from today's performance and in the future select more effective measures and overall deal with accidents more efficiently. The project ESS covers the field of frequent accidents such as sliding accidents at home, in house fires and less common accidents such as chemical and land fill accidents up to even more rare accidents such as natural accidents and hazards. In the ESS project SGI (Swedish geotechnical institute) will evaluate the work and effort concerning various natural hazards limited to landslides, erosion and flooding. The aim is to investigate how municipalities handle, especially prevention, of such natural disasters today. The project includes several aspects such as: • which are the driving forces for risk analysis in a municipality • do one use risk mapping (and what type) in municipal risk analysis • which aspects are most important when selecting preventive measures • in which way do one learn from past accidents • and from previous accidents elsewhere, by for example use existing databases • etc There are many aspects that play a role in a well-functioning safety promotion work. The overall goal is to examine present work and activities, highlight what is well functioning and identify weak points. The aim is to find out where more resources are needed and give suggestions for a more efficient security work. This includes identification of the most efficient "tools" in use or needed. Such tools can be education, directives, funding, more easily available maps and information regarding previous accidents and preventive measures etc. The project will result in recommendations for more effective ways to deal with landslides, erosion and flooding. Since different kinds of problems can occur depending on level of

  4. Parameter trajectory analysis to identify treatment effects of pharmacological interventions.

    Christian A Tiemann

    Full Text Available The field of medical systems biology aims to advance understanding of molecular mechanisms that drive disease progression and to translate this knowledge into therapies to effectively treat diseases. A challenging task is the investigation of long-term effects of a (pharmacological treatment, to establish its applicability and to identify potential side effects. We present a new modeling approach, called Analysis of Dynamic Adaptations in Parameter Trajectories (ADAPT, to analyze the long-term effects of a pharmacological intervention. A concept of time-dependent evolution of model parameters is introduced to study the dynamics of molecular adaptations. The progression of these adaptations is predicted by identifying necessary dynamic changes in the model parameters to describe the transition between experimental data obtained during different stages of the treatment. The trajectories provide insight in the affected underlying biological systems and identify the molecular events that should be studied in more detail to unravel the mechanistic basis of treatment outcome. Modulating effects caused by interactions with the proteome and transcriptome levels, which are often less well understood, can be captured by the time-dependent descriptions of the parameters. ADAPT was employed to identify metabolic adaptations induced upon pharmacological activation of the liver X receptor (LXR, a potential drug target to treat or prevent atherosclerosis. The trajectories were investigated to study the cascade of adaptations. This provided a counter-intuitive insight concerning the function of scavenger receptor class B1 (SR-B1, a receptor that facilitates the hepatic uptake of cholesterol. Although activation of LXR promotes cholesterol efflux and -excretion, our computational analysis showed that the hepatic capacity to clear cholesterol was reduced upon prolonged treatment. This prediction was confirmed experimentally by immunoblotting measurements of SR-B1

  5. Effects of various pharmacological agents on exposed heart of uromastix hardwickii

    Background: The pharmacological and physiological studies on cardiac activity of reptiles specifically of Uromastix hardwickii are scarcely available in literature, as well as the effects of parasympathetic and sympathetic agonists together are also not available. Therefore, the mechanical and electrophysiological effects of pharmacological agents, like Physostigmine and its effects before and after Adrenaline administration were observed on the exposed and intact heart of a reptile, Uromastix hardwickii. Method: To work on exposed heart of Uromastix hardwickii, Physostigmine and Adrenaline were prepared by dissolving 0.01 gm in 10 ml of distilled water. Oscillograph was used to record the mechanical and electrical activity of intact heart through isotonic transducer. Result: Physostigmine was found to produce significant effect on Systolic Force (SF), Duration of cardiac cycle (DCC) and Duration of Phase 4 (DP4). Significant effect of Physostigmine was also observed on heart rate (HR) before Adrenaline administration and on DP4 after Adrenaline administration. Conclusion: It was confirmed that Physostigmine does not exhibit its normal effect on Amplitude of Action Potential, cardiac cycle (CC), Duration of action potential (DAP), Plateau Duration and DP4. Physostigmine is affecting the cardiac activity of this reptile without inhibiting the cholinesterase and not accumulating the Acetylcholine. It modulates the effects of Adrenaline when used before the administration of Adrenaline. (author)

  6. Research Progress of Pharmacological Action of Hawthorn Leaves Flavonoids%山楂叶总黄酮药理作用研究进展

    于栋华; 包顺茹; 于纯淼; 刘树民

    2013-01-01

    我国山楂叶资源丰富,价廉易得,而山楂叶总黄酮为山楂叶提取物中的主要成分,具有广泛的药理作用.现就其对心脑血管、降脂降糖降压、抗氧化等方面的研究进展做一综述,并对应用前景进行了展望.%The hawthorn leaves resource in our country is abundant and easy to get. As the major component of hawthorn leaves, hawthorn leaves flavonoids ( HLF ) has an extensive pharmacological effect. This article reviews the research progress of its pharmacological action on cardio-cerebral-vascular, conquering the blood lipid, blood glucose sugar and blood pressure, antioxidation and so on. Moreover, it puts forward the prospects for its application.

  7. How MDMA's pharmacology and pharmacokinetics drive desired effects and harms.

    Michael White, C

    2014-03-01

    3,4-Methylenedioxymethamphetamine (MDMA) is an agent of abuse that has been used by over 16 million Americans. Increased energy, elevated mood, bonding with others, and psychedelic effects are desired effects while liver damage, extended depressed mood, sexual assault, rhabdomyolysis, serotonin syndrome, multiorgan failure, cardiovascular events, arrhythmias, and death are possible adverse effects. These desirable and adverse effects of MDMA are extensions of its fascinating pharmacologic and pharmacokinetic profile. In addition to methamphatemine like effects, MDMA also has mescaline like effects and increases the release of cortisol, oxytocin, and antidiuretic hormone. The desirable effects of MDMA are accentuated by the rave or electronic dance music scene where warm temperatures, vigorous dancing, loud music, and light shows accentuate some of the responses. However, the same environment increases the risk of certain harms. Knowledge of the constellation of these factors is needed for education, prevention of harm, and treatment. PMID:24431106

  8. Pills or push-ups? Effectiveness and public perception of pharmacological and non-pharmacological cognitive enhancement

    Lucius eCaviola

    2015-12-01

    Full Text Available We review work on the effectiveness of different forms of cognitive enhancement, both pharmacological and non-pharmacological. We consider caffeine, methylphenidate, and modafinil for pharmacological cognitive enhancement (PCE and computer training, physical exercise, and sleep for non-pharmacological cognitive enhancement (NPCE. We find that all of the techniques described can produce significant beneficial effects on cognitive performance. However, effect sizes are moderate, and consistently dependent on individual and situational factors as well as the cognitive domain in question. Although meta-analyses allowing a quantitative comparison of effectiveness across techniques are lacking to date, we can conclude that PCE is not more effective than NPCE. We discuss the physiological reasons for this limited effectiveness.We then propose that even though their actual effectiveness seems similar, in the general public PCE is perceived as fundamentally different from NPCE, in terms of effectiveness, but also in terms of acceptability. We illustrate the potential consequences such a misperception of PCE can have.

  9. Pharmacological effects of saw palmetto extract in the lower urinary tract

    Mayumi SUZUKI; Yoshihiko ITO; Tomomi FUJINO; Masayuki ABE; Satomi ONOUE; Keizo UMEGAKI; Hiroshi NOGUCHI; Shizuo YAMADA

    2009-01-01

    Saw palmetto extract (SPE), an extract from the ripe berries of the American dwarf palm, has been widely used as a thera-peutic remedy for urinary dysfunction due to benign prostatic hyperplasia (BPH) in Europe. Numerous mechanisms of action have been proposed for SPE, including the inhibition of 5α-reductase. Today, α1-adrenoceptor antagonists and muscarinic cholinoceptor antagonists are commonly used in the treatment of men with voiding symptoms secondary to BPH. The improvement of voiding symptoms in patients taking SPE may arise from its binding to pharmacologically rel-evant receptors in the lower urinary tract, such as α1-adrenoceptors, muscarinic cholinoceptors, 1,4-dihyropyridine recep-tors and vanilloid receptors. Furthermore, oral administration of SPE has been shown to attenuate the up-regulation of α1-adrenoceptors in the rat prostate induced by testosterone. Thus, SPE at clinically relevant doses may exert a direct effect on the pharmacological receptors in the lower urinary tract, thereby improving urinary dysfunction in patients with BPH and an overactive bladder. SPE does not have interactions with co-administered drugs or serious adverse events in blood biochemical parameters, suggestive of its relative safety, even with long-term intake. Clinical trials (placebo-controlled and active-controlled trials) of SPE conducted in men with BPH were also reviewed. This review should contribute to the under-standing of the pharmacological effects of SPE in the treatment of patients with BPH and associated lower urinary tract symptoms (LUTS).

  10. Alcohol use disorder: pathophysiology, effects, and pharmacologic options for treatment

    Wackernah RC

    2014-01-01

    Full Text Available Robin C Wackernah,1 Matthew J Minnick,1 Peter Clapp2 1Department of Pharmacy Practice, 2Department of Pharmaceutical Sciences, School of Pharmacy, Rueckert-Hartman College for Health Professions, Regis University, Denver, CO, USA Abstract: Alcohol use disorders (AUD continue to be a concerning health issue worldwide. Harmful alcohol use leads to 2.5 million deaths annually worldwide. Multiple options exist for the management of dependence on alcohol, not all of which are approved by drug-regulating agencies. Current practice in treating AUD does not reflect the diversity of pharmacologic options that have potential to provide benefit, and guidance for clinicians is limited. Few medications are approved for treatment of AUD, and these have exhibited small and/or inconsistent effects in broad patient populations with diverse drinking patterns. The need for continued research into the treatment of this disease is evident in order to provide patients with more specific and effective options. This review describes the neurobiological mechanisms of AUD that are amenable to treatment and drug therapies that target pathophysiological conditions of AUD to reduce drinking. In addition, current literature on pharmacologic (both approved and non-approved treatment options for AUD offered in the United States and elsewhere are reviewed. The aim is to inform clinicians regarding the options for alcohol abuse treatment, keeping in mind that not all treatments are completely successful in reducing craving or heavy drinking or increasing abstinence. Keywords: abuse, alcohol, alcoholism, craving, dependence, relapse

  11. The Behavioral and Pharmacological Actions of NMDA Receptor Antagonism are Conserved in Zebrafish Larvae

    Chen, John; Patel, Roshni; Friedman, Theodore C.; Jones, Kevin S

    2010-01-01

    Dizocilpine maleate (MK-801) is one of several NMDA receptor antagonists that is widely used to pharmacologically model the symptoms of psychosis and schizophrenia in animals. MK-801 elicits behaviors in adult zebrafish (Danio rerio) that are phenotypically consistent with behaviors observed in humans and rodents exposed to tbhe drug. However, the molecular and cellular processes that mediate the psychotomimetic, cognitive and locomotive behaviors of MK-801 are unclear. We exposed zebrafish l...

  12. The Behavioral and Pharmacological Actions of NMDA Receptor Antagonism are Conserved in Zebrafish Larvae

    Chen, John; Patel, Roshni; Friedman, Theodore C.; Jones, Kevin S

    2010-01-01

    Dizocilpine maleate (MK-801) is one of several NMDA receptor antagonists that is widely used to pharmacologically model the symptoms of psychosis and schizophrenia in animals. MK-801 elicits behaviors in adult zebrafish (Danio rerio) that are phenotypically consistent with behaviors observed in humans and rodents exposed to the drug. However, the molecular and cellular processes that mediate the psychotomimetic, cognitive and locomotive behaviors of MK-801 are unclear. We exposed zebrafish la...

  13. Developmental paediatric anaesthetic pharmacology

    Hansen, Tom Giedsing

    2015-01-01

    Safe and effective drug therapy in neonates, infants and children require detailed knowledge about the ontogeny of drug disposition and action as well how these interact with genetics and co-morbidity of children. Recent advances in developmental pharmacology in children follow the increased...

  14. Pharmacological and therapeutic effects of Mentha Longifolia L. and its main constituent, menthol

    Peyman Mikaili; Sina Mojaverrostami; Milad Moloudizargari; Shahin Aghajanshakeri

    2013-01-01

    Mentha longifolia (wild mint) is a popular folk remedy. Some parts of this plant have been used in traditional medicine of Iran and other countries. Many studies have shown various pharmacological and therapeutic effects of the plant. Our aim in preparing this study was to review the traditional uses of M. longifolia together with the pharmacological and therapeutic effects of its entire extract and major compounds. Mentha longifolia is an herb with a wide range of pharmacological properties ...

  15. Effects of non-pharmacological or pharmacological interventions on cognition and brain plasticity of aging individuals.

    Pieramico, Valentina; Esposito, Roberto; Cesinaro, Stefano; Frazzini, Valerio; Sensi, Stefano L

    2014-01-01

    Brain aging and aging-related neurodegenerative disorders are major health challenges faced by modern societies. Brain aging is associated with cognitive and functional decline and represents the favourable background for the onset and development of dementia. Brain aging is associated with early and subtle anatomo-functional physiological changes that often precede the appearance of clinical signs of cognitive decline. Neuroimaging approaches unveiled the functional correlates of these alterations and helped in the identification of therapeutic targets that can be potentially useful in counteracting age-dependent cognitive decline. A growing body of evidence supports the notion that cognitive stimulation and aerobic training can preserve and enhance operational skills in elderly individuals as well as reduce the incidence of dementia. This review aims at providing an extensive and critical overview of the most recent data that support the efficacy of non-pharmacological and pharmacological interventions aimed at enhancing cognition and brain plasticity in healthy elderly individuals as well as delaying the cognitive decline associated with dementia. PMID:25228860

  16. Effects of non-pharmacological or pharmacological interventions on cognition and brain plasticity of aging individuals

    Pieramico, Valentina; Esposito, Roberto; Cesinaro, Stefano; Frazzini, Valerio; Sensi, Stefano L.

    2014-01-01

    Brain aging and aging-related neurodegenerative disorders are major health challenges faced by modern societies. Brain aging is associated with cognitive and functional decline and represents the favourable background for the onset and development of dementia. Brain aging is associated with early and subtle anatomo-functional physiological changes that often precede the appearance of clinical signs of cognitive decline. Neuroimaging approaches unveiled the functional correlates of these alterations and helped in the identification of therapeutic targets that can be potentially useful in counteracting age-dependent cognitive decline. A growing body of evidence supports the notion that cognitive stimulation and aerobic training can preserve and enhance operational skills in elderly individuals as well as reduce the incidence of dementia. This review aims at providing an extensive and critical overview of the most recent data that support the efficacy of non-pharmacological and pharmacological interventions aimed at enhancing cognition and brain plasticity in healthy elderly individuals as well as delaying the cognitive decline associated with dementia. PMID:25228860

  17. Citalopram--a review of pharmacological and clinical effects.

    Bezchlibnyk-Butler, K; Aleksic, I; Kennedy, S. H.

    2000-01-01

    OBJECTIVE: To provide clinicians with a critical evaluation of citalopram, a selective serotonin reuptake inhibitor (SSRI) that has been available in Canada since March 1999. DATA SOURCES: Commercial searches (MEDLINE and BiblioTech) and an "in-house" search (InfoDrug) were used to find published English-language references for clinical and preclinical publications. There was no restriction of publication dates. Primary index terms used were: pharmacological properties, receptors, pharmacolog...

  18. An Inquiry into the Action of Acupuncture on the Human Body by Means of Pharmacology

    LU Yong; WANG Jia-tao

    2009-01-01

    @@ The science of traditional acupuncture was the summary of the law of action of acupuncture made by our predecessors in their long term clinical practice, which plays a very important guiding role in clinic. In order to make the charm of this ancient acupuncture therapy ever lasting, bringing it into line with the modem science and technology is necessary.

  19. Early Clinical Detection of Pharmacologic Response in Insulin Action in a Nondiabetic Insulin-Resistant Population

    Sudha S. Shankar, MD

    2015-12-01

    Conclusions: Significant changes in insulin action across multiple insulin-sensitive tissues can be detected within 2 weeks of initiation of insulin-sensitizing therapy with pioglitazone in obese patients with nondiabetic insulin resistance. ClinicalTrials.gov identifier: NCT01115712.

  20. 紫菀的化学成分及其药理活性研究进展%Advances on chemical components and pharmacological actions of Aster tataricus

    房慧勇; 单高威; 秦桂芳; 甄林娜; 李旻辉; 郝丽静

    2012-01-01

      紫菀具有良好的润肺、祛痰、止咳效果,通过查阅国内外相关文献,综述了其化学成分和化痰镇咳、抗肿瘤等方面的药理作用,为紫菀的综合开发利用提供参考。%  Aster tataricus L. f. has a good effect upon moistening lung, eliminating phlegm, and suppressing cough. The literature reviews its chemical compositions and pharmacological action of eliminating phlegm, anti-tumor and etc.. The literature could provide reference for development and utilization of Aster tataricus.

  1. Effectiveness of integrated teaching module in pharmacology among medical undergraduates

    Yadav, Preeti P; Chaudhary, Mayur; Patel, Jayshree; Shah, Aashal; Kantharia, ND

    2016-01-01

    Context: Over the years with advancement of science and technology, each subject has become highly specialized. Teaching of medical students has still remained separate in various departments with no scope of integration in majority of medical institutes in India. Study was planned to have an experience of integration in institute and sensitize faculty for integrated teaching–learning (TL) method. Aims: To prepare and test effectiveness of integrated teaching module for 2nd year MBBS student in pharmacology and to sensitize and motivate faculties toward advantages of implementing integrated module. Settings and Design: Education intervention project implemented 2nd year MBBS students of Government Medical College and New Civil Hospital, Surat. Subjects and Methods: Students of second MBBS were divided into two groups. One group was exposed to integrated teaching sessions and another to traditional method. Both the groups were assessed by pre- and post-test questionnaire, feedback and focus group discussions were conducted to know their experience about process. Results: A total of 165 students of the 2nd year MBBS were exposed to the integrated teaching module for two topics in two groups. One group was taught by traditional teaching, and another group was exposed to the integrated TL session. Both the groups have shown a significant improvement in posttest scores but increase in mean score was more in integrated group. During analysis of feedback forms, it was noted that students preferred integrated TL methods since they help in better understanding. Faculty feedback shows consensus over the adaptation of integrated TL methods. Conclusions: Integrated TL sessions were well-appreciated by students and faculties. To improve the critical reasoning skills and self-directed learning of students, integrated TL is highly recommended for must know areas of curriculum.

  2. PHYTOCHEMICAL, PHARMACOLOGICAL AND PHARMACOKINETICS EFFECTS OF ROSMARINIC ACID

    Rahul Bhatt

    2013-04-01

    Full Text Available Rosmarinic acid is natural polyphenol antioxidant isolated from Rosmarinus officinalis L. and commonly found in species of the Boraginaceae and the subfamily Nepetoideae of the Lamiaceae. RA species of Labiatae named Salvia officinalis, Rosmarinus officinali. RA exhibits important biological activities include its anti-carcinogenic, antiviral, antibacterial antimicrobial, antidepressant qualities. Plants of Labiatae family have been used in traditional medicine for exhaustion, phytotherapy, weakness, depression, and memory enhancement, circulation improvement, strengthening of fragile blood vessels, inflammation, and infection CNS disorder. RA showed the highest concentrations of antioxidant all the polyphenols. It is a red-orange powder that is slightly soluble in water, but well soluble in most organic solvents. RA polyphenolic compounds have been associated with antioxidative action in biological systems, acting as scavengers of singlet oxygen and free radicals. RA protects neurons from oxidative stress significantly attenuated H2O2-induced reactive oxygen species (ROS generation and apoptotic cell death and could contribute at least in part to neuroprotective effects because this natural compound exerts neuroprotective and anti-oxidative effects against neurotoxin insult in dopaminergic cells. This review focused on pharmacokinetics and use different uses of RA as antioxidant agent, anti-inflammatory, antiviral, photo protective, anticancer, antidepressant, and possible neuroprotective agent mechanism of actions.

  3. Histamine reverses IL-5-Afforded human eosinophil survival by inducing apoptosis: Pharmacological evidence for a novel mechanism of action of histamine

    Hasala, Hannele; Giembycz, Mark A.; Janka-Junttila, Mirkka; Moilanen, Eeva; Kankaanranta, Hannu

    2008-01-01

    Histamine reverses IL-5-Afforded human eosinophil survival by inducing apoptosis: Pharmacological evidence for a novel mechanism of action of histamine correspondence: Corresponding author. Tel.: +358335517318; fax: +358335518082. (Kankaanranta, Hannu) (Kankaanranta, Hannu) The Immunopharmacology Research Group--> , Medical School--> , University of Tampere--> , Tampere--> - FINLAND (Hasala, H...

  4. Effect of metal complexation to anti-inflammatory over the action against oxidative and free radicals: ketoprofen action

    Free radicals are highly reactive species generated in living organisms for the purpose of protection. However, in some circumstances, they are responsible for the occurrence or aggravation of tissue damage. Many anti-inflammatory drugs have a direct effect on free radicals and not radical reactive species, which contributes to its actions against inflammation. Ketoprofen is a nonsteroidal anti-inflammatory agent that generates free radicals by photo irradiation and has an important hemolytic effect with that. The complexation of metals to different drugs has been used as a strategy to improve the pharmacological action of different molecules and reduce their side effects. This paper presents the results of ketoprofen and their metallic complexes action on erythrocytes and free radicals. It was observed that the cerium enhances the scavenger properties of ketoprofen on free radicals, while copper enhances its action over non-radical oxidants. Copper also reduced the hemolytic effect presented by ketoprofen meanwhile its cerium derivative maintained it. (author)

  5. Pharmacological receptors of nematoda as target points for action of antiparasitic drugs

    Trailović Saša M.

    2010-01-01

    Full Text Available Cholinergic receptors of parasitic nematodes are one of the most important possible sites of action of antiparasitic drugs. This paper presents some of our own results of electrophysiological and pharamcological examinations of nicotinic and muscarinic receptors of nematodes, as well as data from literature on a new class of anthelmintics that act precisely on cholinergic receptors. The nicotinic acetylcholine receptor (nAChR is located on somatic muscle cells of nematodes and it is responsible for the coordination of parasite movement. Cholinomimetic anthelmintics act on this receptor, as well as acetylcholine, an endogenic neurotransmitter, but they are not sensitive to enzyme acetylcholineesterase which dissolves acetylcholine. As opposed to the nicotinic receptor of vertebra, whose structure has been examined thoroughly, the stoichiometry of the nicotinic receptor of nematodes is not completely known. However, on the grounds of knowledge acquired so far, a model has been constructed recently of the potential composition of a type of nematodes nicotinic receptor, as the site of action of anthelmintics. Based on earlier investigations, it is supposed that a conventional muscarinic receptor exists in nematodes as well, so that it can also be a new pharamocological target for the development of antinematode drugs. The latest class of synthesized anthelmintics, named aminoacetonitriles (AAD, act via the nicotinic receptor. Monepantel is the first drug from the AAD group as a most significant candidate for registration in veterinary medicine. Even though several groups of cholinomimetic anthelmintics (imiodazothiazoles, tetrahydropyrimidines, organophosphat anthelmintics have been in use in veterinary practice for many years now, it is evident that cholinergic receptors of nematodes still present an attractive place in the examinations and development of new antinematode drugs. .

  6. Rebound effect of drugs: fatal risk of conventional treatment and pharmacological basis of homeopathic treatment

    Marcus Zulian Teixeira

    2012-06-01

    Full Text Available The homeopathic model applies the secondary action or vital reaction of the organism as a therapeutic method and thus prescribes treatment by similitude, which consists in administering to ill individuals substances that cause similar symptoms in healthy individuals. The vital, homeostatic or paradoxical reaction of the organism might be explained scientifically by means of the rebound effect of modern drugs, which might cause fatal iatrogenic events after discontinuation of antipathic (a term used in alternative medicine for palliative treatment, also known as enantiopathic treatment. Although the rebound effect is studied by modern pharmacology, it is poorly communicated to and discussed among healthcare professionals, who are thus deprived of information needed for the safe management of modern drugs. This article presents an up-to-date review on the rebound effect of modern drugs that grounds the homeopathic principle of healing and calls the attention of doctors to this type of adverse effect that is usually unnoticed. The rebound effect of modern palliative drugs, which was pointed out by Hahnemann more than two centuries ago, might cause fatal adverse events and is illustrated by the examples of acetylsalicylic acid, anti-inflammatory agents, bronchodilators, antidepressants, statins, proton-pump inhibitors, etc. Although the rebound effect is expressed by a small fraction of (susceptible individuals and might be avoided by gradual tapering of antipathic drugs, it exhibits epidemiologic importance as a function of the massive use of such palliative drugs and the lack of knowledge in its regard.

  7. Structural and Pharmacological Effects of Ring-Closing Metathesis in Peptides

    Pål Rongved

    2010-09-01

    Full Text Available Applications of ring-closing alkene metathesis (RCM in acyclic α- and β-peptides and closely related systems are reviewed, with a special emphasis on the structural and pharmacological effects of cyclization by RCM.

  8. Structural and Pharmacological Effects of Ring-Closing Metathesis in Peptides

    Pål Rongved; Øyvind Jacobsen; Jo Klaveness

    2010-01-01

    Applications of ring-closing alkene metathesis (RCM) in acyclic α- and β-peptides and closely related systems are reviewed, with a special emphasis on the structural and pharmacological effects of cyclization by RCM.

  9. The Advances in Research on the Pharmacological Effects of Fructus Ligustri Lucidi

    Zunting Pang

    2015-01-01

    Full Text Available Fructus Ligustri Lucidi is a well-known invigorator in Chinese materia medica with hepatoprotective effect, anticancer activity, antioxidant activity, and so on. And oleanolic acids are the major pharmacologically active components in Fructus Ligustri Lucidi. So it has great value in medical health, and may be developed to a complementary and alternative medicine through further research. In this paper, the advances in research on pharmacological effects of Fructus Ligustri Lucidi were summarized by reviewing the recent related literature.

  10. Mechanisms of Action in Cognitive-Behavioral and Pharmacological Interventions for Obesity and Bulimia Nervosa.

    Craighead, Linda W.; Agras, W. Stewart

    1991-01-01

    Summarizes data pertaining to separate and combined effects of cognitive-behavioral and psychopharmacologic treatments for obesity and bulimia nervosa. Anorexiant medication appears to enhance restraint and facilitates weight loss with behavioral interventions in the treatment of obesity, but relapse occurs once medication is withdrawn.…

  11. Role of PPARγ in the nutritional and pharmacological actions of carotenoids

    Zhao WE

    2016-04-01

    Full Text Available Wen-en Zhao,1 Guoqing Shi,2 Huihui Gu,1,3 Nguyen Ba Ngoc1,4 1School of Chemical Engineering and Energy, Zhengzhou University, 2School of Food and Bioengineering, Zhengzhou University of Light Industry, 3School of Life Sciences, Zhengzhou University, Zhengzhou, People’s Republic of China; 4Faculty of Food Industry, College of Food Industry, Da Nang, Vietnam Abstract: Peroxisome proliferator-activated receptor gamma (PPARγ has been shown to play an important role in the biological effects of carotenoids. The PPARγ-signaling pathway is involved in the anticancer effects of carotenoids. Activation of PPARγ partly contributes to the growth-inhibitory effects of carotenoids (β-carotene, astaxanthin, bixin, capsanthin, lutein, and lycopene on breast cancer MCF7 cells, leukemia K562 cells, prostate cancer (LNCaP, DU145, and PC3 cells, and esophageal squamous cancer EC109 cells. PPARγ is the master regulator of adipocyte differentiation and adipogenesis. Downregulated PPARγ and PPARγ-target genes have been associated with the suppressive effects of β-carotene and lycopene on 3T3L1 and C3H10T1/2 adipocyte differentiation and adipogenesis. ß-Carotene is cleaved centrally into retinaldehyde by BCO1, the encoding gene being a PPARγ-target gene. Retinaldehyde can be oxidized to retinoic acid and also be reduced to retinol. β-Carotene can also be cleaved asymmetrically into β-apocarotenals and β-apocarotenones by BCO2. The inhibitory effects of β-carotene on the development of adiposity and lipid storage are dependent substantially on BCO1-mediated production of retinoids. The effects of β-carotene on body adiposity were absent in BCO1-knockout mice. Retinoid metabolism is connected with the activity of PPARγ in the control of body-fat reserves. Retinoic acid, retinaldehyde, retinol, and β-apocarotenals exert suppressive effects on preadipocyte differentiation and adipogenesis via downregulation of PPARγ expression in cell culture. The

  12. Pharmacological Action of Mentha piperita on Lipid Profile in Fructose-Fed Rats.

    Mani Badal, Rajendra; Badal, Divya; Badal, Pourush; Khare, Ashish; Shrivastava, Jyoti; Kumar, Vinod

    2011-01-01

    Cardiovascular diseases with an incidence of approximately 50% are the main causes of death in most advanced countries and an increasing trend in the developing world as well. The World Health Organization estimates that 12 million people per year worldwide die from cardiovascular diseases. Cardiovascular diseases are becoming an increasing problem worldwide and hypercholesterolemia has been correlated for coronary heart diseases. Nearly all lipoproteins are involved in this process including cholesterol carried by very low density lipoproteins (VLDL), remnant lipoproteins and low density lipoproteins (LDL). Currently, available hypolipidemic drugs have been associated with the number of side effects. Herbal treatment for hyperlipidemia poses no side effects and is relatively cheap and locally available. In view of this, the present study was carried out to investigate the effect of Menthe piperita on serum lipid levels of albino rats. Mentha piperita aqueous extract (100 mg/Kg, 250 mg/Kg p.o. daily) was fed for 3 weeks on fructose-fed rats and the levels of glucose, cholesterol, triglycerides, very low density lipoprotein, low density lipoprotein, and atherogenic index was measured. Twenty-four male Sprague Dawley rats were divided into four groups (6 per group). The results of present study indicate that Mentha piperita had significant beneficial effects against fructose-induced hyperlipidemia and showed good antioxidant activity. The aqueous extract of the plant produced a significant decrease (p < 0.05) in elevated levels of glucose, cholesterol, triglycerides, very low density lipoprotein, low density lipoprotein and atherogenic index and also increased the high density lipoprotein cholesterol levels and HDL-ratio without affecting serum insulin levels in fructose-fed rats. PMID:24250421

  13. Nephroprotective action of glycosaminoglycans: why the pharmacological properties of sulodexide might be reconsidered

    Antonio V Gaddi

    2010-07-01

    Full Text Available Antonio V Gaddi1, Arrigo FG Cicero1, Giovanni Gambaro21Atherosclerosis and Metabolic disease Research Unit, Internal Medicine, Aging and Kidney diseases Dept., University of Bologna, Italy; 2Nephrology and Dialysis Unit, Gemelli University Hospital, Sacred Heart Catholic University, Rome, ItalyAbstract: A relatively large body of evidence supports the notion that glomerular capillary wall and mesangial alterations in diabetic nephropathy involve biochemical alterations of glycoproteins in these structures. Evidence in experimental animals rendered diabetic reveals that the administration of heparin and other anionic glycoproteins can effectively prevent the biochemical alterations that promote albuminuria. Moreover, angiotensin II inhibits heparan sulfate synthesis, while heparins modulate angiotensin II signaling in glomerular cells, inhibiting aldosterone synthesis and lowering proteinuria in diabetes patients. Sulodexide, a mixture of heparin and dermatan sulfate, appears to be a promising treatment for diabetic proteinuria partially resistant to renin–angiotensin system blocking agents. Sulodexide prevents heparan sulfate degradation, thus allowing reconstruction of heparan sulfate content and restoration of glomerular basement membrane ionic permselectivity. The antiproteinuric effect appears to be mainly related to the basal proteinuria and consequently to the duration of treatment in a relatively large number of small clinical trials. On the other hand, several sulodexide pharmacodynamic properties could improve the prognosis of chronic kidney disease patients, also independently from its antiproteinuric effect. However, sulodexide development as an antiproteinuric drug needs to be continued, in order to define which kind of patients could better respond to this treatment.Keywords: glycosaminoglycans, sulodexide, albuminuria, proteinuria, diabetic nephropathy

  14. A novel method for imaging the pharmacological effects of antibiotic treatment on Clostridium difficile.

    Endres, Bradley T; Bassères, Eugénie; Memariani, Ali; Chang, Long; Alam, M Jahangir; Vickers, Richard J; Kakadiaris, Ioannis A; Garey, Kevin W

    2016-08-01

    Clostridium difficile is a significant cause of nosocomial-acquired infection that results in severe diarrhea and can lead to mortality. Treatment options for C. difficile infection (CDI) are limited, however, new antibiotics are being developed. Current methods for determining efficacy of experimental antibiotics on C. difficile involve antibiotic killing rates and do not give insight into the drug's pharmacologic effects. Considering this, we hypothesized that by using scanning electron microscopy (SEM) in tandem to drug killing curves, we would be able to determine efficacy and visualize the phenotypic response to drug treatment. To test this hypothesis, supraMIC kill curves were conducted using vancomycin, metronidazole, fidaxomicin, and ridinilazole. Following collection, cells were either plated or imaged using a scanning electron microscope (SEM). Consistent with previous reports, we found that the tested antibiotics had significant bactericidal activity at supraMIC concentrations. By SEM imaging and using a semi-automatic pipeline for image analysis, we were able to determine that vancomycin and to a lesser extent fidaxomicin and ridinilazole significantly affected the cell wall, whereas metronidazole, fidaxomicin, and ridinilazole had significant effects on cell length suggesting a metabolic effect. While the phenotypic response to drug treatment has not been documented previously in this manner, the results observed are consistent with the drug's mechanism of action. These techniques demonstrate the versatility and reliability of imaging and measurements that could be applied to other experimental compounds. We believe the strategies laid out here are vital for characterizing new antibiotics in development for treating CDI. PMID:27108094

  15. Anti-pressor effects of whole body exposure to static magnetic field on pharmacologically induced hypertension in conscious rabbits.

    Okano, Hideyuki; Ohkubo, Chiyoji

    2003-02-01

    Acute effects of whole body exposure to static magnetic field (SMF) on pharmacologically induced hypertension in a conscious rabbit were evaluated. Hypertensive and vasoconstrictive actions were induced by norepinephrine (NE) or a nonselective nitric oxide synthase (NOS) inhibitor, N(omega)-nitro-l-arginine methyl ester (l-NAME). The hemodynamics in a central artery of the ear lobe was measured continuously and analyzed by penetrating microphotoelectric plethysmography (MPPG). Concurrently, blood pressure (BP) changes in a central artery, contralateral to that of the MPPG measured ear lobe, were monitored. Magnetic flux densities were 5.5 mT (Bmax), the magnetic gradient peaked in the throat at the level of approximately 0.09 mT/mm, and the duration of exposure was 30 min. The results demonstrated that under normal physiological conditions without treatment of pharmacological agents, there were no statistically significant differences in the hemodynamics and BP changes between the sham and the SMF exposure alone. Under pharmacologically induced hypertensive conditions, the whole body exposure to nonuniform SMF with peak magnetic gradient in the carotid sinus baroreceptor significantly attenuated the vasoconstriction and suppressed the elevation of BPs. These findings suggest that antipressor effects of the SMF on the hemodynamics under NE or l-NAME induced high vascular tone might be, in part, dependent on modulation of NE mediated response in conjunction with alteration in NOS activity, thereby modulating BPs. PMID:12524681

  16. In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib.

    Rolf, Michael G; Curwen, Jon O; Veldman-Jones, Margaret; Eberlein, Cath; Wang, Jianyan; Harmer, Alex; Hellawell, Caroline J; Braddock, Martin

    2015-10-01

    Off-target pharmacology may contribute to both adverse and beneficial effects of a new drug. In vitro pharmacological profiling is often applied early in drug discovery; there are fewer reports addressing the relevance of broad profiles to clinical adverse effects. Here, we have characterized the pharmacological profile of the active metabolite of fostamatinib, R406, linking an understanding of drug selectivity to the increase in blood pressure observed in clinical studies. R406 was profiled in a broad range of in vitro assays to generate a comprehensive pharmacological profile and key targets were further investigated using functional and cellular assay systems. A combination of traditional literature searches and text-mining approaches established potential mechanistic links between the profile of R406 and clinical side effects. R406 was selective outside the kinase domain, with only antagonist activity at the adenosine A3 receptor in the range relevant to clinical effects. R406 was less selective in the kinase domain, having activity at many protein kinases at therapeutically relevant concentrations when tested in multiple in vitro systems. Systematic literature analyses identified KDR as the probable target underlying the blood pressure increase observed in patients. While the in vitro pharmacological profile of R406 suggests a lack of selectivity among kinases, a combination of classical searching and text-mining approaches rationalized the complex profile establishing linkage between off-target pharmacology and clinically observed effects. These results demonstrate the utility of in vitro pharmacological profiling for a compound in late-stage clinical development. PMID:26516587

  17. [Pharmacological effects of CM6912 and its main metabolites].

    Morishita, H; Kushiku, K; Furukawa, T; Yamaki, Y; Izawa, M; Shibazaki, Y; Shibata, U

    1985-07-01

    Pharmacodynamic effects of ethyl 7-chloro-2,3-dihydro-5-(2-fluorophenyl)-2-oxo-1H-1,4- benzodiazepine-3-carboxylate (CM6912), a new benzodiazepine derivative, and its main metabolites (CM6913 = M1, CM7116 = M2) on the peripheral systems were investigated in several species of animals. In pentobarbital-anesthetized rabbits, CM6912 and M2 (1 or 5 mg/kg, i.v.) had little effect on blood pressure, heart rate and ECG, but it slightly reduced the respiration rate. M1 decreased the heart rate without affecting respiration, blood pressure and ECG. In conscious rabbits, CM6912 and M2 (1 mg/kg, i.v.) did not affect respiration, blood pressure, heart rate and ECG, but M1 (1 mg/kg, i.v.) increased the heart rate. CM6912 (5 or 30 mg/kg), when administered orally, also increased heart rate. In pentobarbital-anesthetized dogs, CM6912 and its metabolites (5 mg/kg, i.v.) decreased respiration and heart rate without affecting blood pressure and ECG. CM 6912 (5 mg/kg, i.v.) did not affect cardiovascular responses to the carotid occlusion, vagus stimulation, and pre- and post-ganglionic stimulation of cardiac ganglion in anesthetized dogs. CM6912 and its metabolites affected neither the spontaneous contraction nor the heart rate of isolated rabbit atria. These compounds also had no action on isolated aortic strips from rabbits. CM6912 and its metabolites did not affect the muscle tone of isolated guinea pig intestine, and it had no effects on the contractile responses to acetylcholine, histamine, serotonin and barium chloride. In isolated rabbit intestine, CM6912 and M2 slightly reduced the amplitude of contraction, while M1 had no effect. CM6912 and its metabolites did not affect the spontaneous motility of isolated non-pregnant and pregnant rat uteri as well as in situ non-pregnant rat uterus and isolated guinea pig vas deferens, including the contractile response to adrenaline. CM6912 and M2 relaxed isolated guinea pig trachea strips only at high concentrations. CM6912 and its

  18. Effect of Pharmacologically-Induced Hypovolemia on Aerobic Capacity

    Everett, Meghan E.; Lee, S. M. C.; Platts, S. H.

    2009-01-01

    Decreased peak oxygen consumption (VO2pk) and an elevated exercise heart rate (HR) response are associated with a reduction in plasma volume (PV) after space flight and bed rest, a space flight analog. Reduced VO2pk and submaximal exercise tolerance would negatively impact an astronaut s ability to perform near maximal work that would be required in the event of an emergency. We previously have administered IV furosemide followed by a low salt diet to model PV loss and orthostatic intolerance observed after spaceflight. Purpose: To determine whether a pharmacologically-induced reduction in PV results in decreased VO2pk and elevated exercise HR response. Methods: Six subjects (5M, 1F) performed two graded peak cycle tests (work rate increased by 35 or 50 W every 3 min), once while normovolemic and once while hypovolemic. HR and expired respiratory gases were continuously measured. To induce hypovolemia, subjects were administered a single dose of IV furosemide (0.5 mg.kg-1) 30 hr before exercise testing and then consumed a low-salt diet (10 mEq.d(sup -1)). PV was measured using carbon monoxide rebreathing. Exercise HR and VO2 responses were quantified as the area under the curve (AUC) calculated over each quartile of the peak test, based on test time in the hypovolemia condition. Paired t-tests were used to test for differences in PV, VO2pk, and peak HR between conditions. Repeated-measures ANOVAs were used to test for differences in AUC between conditions. Results: PV (3.32+/-0.12 vs. 2.77+/-0.16 L, p<0.05) and VO2pk (3.30+/-0.67 vs. 2.90+/-0.57 L.min(sup -1), p<0.05) were lower during hypovolemia than during normovolemia, but peak HR was not different (187+/-5 vs. 187+/-5 bpm). The AUC for VO2 and HR was different (p<0.05) between conditions only in the highest quartile: HR was 4% higher and VO2 was 5% lower during the hypovolemia condition. Conclusion: The mean difference in VO2pk (-12%) between normovolemia and hypovolemia was similar to the mean difference in

  19. Effect of Pharmacologically-Induced Hypovolemia on Aerobic Capacity

    Everett, Meghan E.; Lee, S. M. C.; Platts, S. H.

    2009-01-01

    Decreased peak oxygen consumption (VO2pk) and an elevated exercise heart rate (HR) response are associated with a reduction in plasma volume (PV) after space flight and bed rest, a space flight analog. Reduced VO2pk and submaximal exercise tolerance would negatively impact an astronaut s ability to perform near maximal work that would be required in the event of an emergency. We previously have administered IV furosemide followed by a low salt diet to model PV loss and orthostatic intolerance observed after spaceflight. Purpose: To determine whether a pharmacologically-induced reduction in PV results in decreased VO2pk and elevated exercise HR response. Methods: Six subjects (5M, 1F) performed two graded peak cycle tests (work rate increased by 35 or 50 W every 3 min), once while normovolemic and once while hypovolemic. HR and expired respiratory gases were continuously measured. To induce hypovolemia, subjects were administered a single dose of IV furosemide (0.5 mg.kg-1) 30 hr before exercise testing and then consumed a low-salt diet (10 mEq.d(sup -1)). PV was measured using carbon monoxide rebreathing. Exercise HR and VO2 responses were quantified as the area under the curve (AUC) calculated over each quartile of the peak test, based on test time in the hypovolemia condition. Paired t-tests were used to test for differences in PV, VO2pk, and peak HR between conditions. Repeated-measures ANOVAs were used to test for differences in AUC between conditions. Results: PV (3.32+/-0.12 vs. 2.77+/-0.16 L, pbpm). The AUC for VO2 and HR was different (p<0.05) between conditions only in the highest quartile: HR was 4% higher and VO2 was 5% lower during the hypovolemia condition. Conclusion: The mean difference in VO2pk (-12%) between normovolemia and hypovolemia was similar to the mean difference in PV (-17%). Similar decreases in PV and VO2pk have been observed following short duration space flight, suggesting that pharmacologically-induced PV loss can be used to model

  20. The pharmacological effect of Bothrops neuwiedii pauloensis (jararaca-pintada snake venom on avian neuromuscular transmission

    C.R. Borja-Oliveira

    2003-05-01

    Full Text Available The neuromuscular effects of Bothrops neuwiedii pauloensis (jararaca-pintada venom were studied on isolated chick biventer cervicis nerve-muscle preparations. Venom concentrations of 5-50 µg/ml produced an initial inhibition and a secondary increase of indirectly evoked twitches followed by a progressive concentration-dependent and irreversible neuromuscular blockade. At venom concentrations of 1-20 µg/ml, the responses to 13.4 mM KCl were inhibited whereas those to 110 µM acetylcholine alone and cumulative concentrations of 1 µM to 10 mM were unaffected. At venom concentrations higher than 50 µg/ml, there was pronounced muscle contracture with inhibition of the responses to acetylcholine, KCl and direct stimulation. At 20-24ºC, the venom (50 µg/ml produced only partial neuromuscular blockade (30.7 ± 8.0%, N = 3 after 120 min and the initial inhibition and the secondary increase of the twitch responses caused by the venom were prolonged and pronounced and the response to KCl was unchanged. These results indicate that B.n. pauloensis venom is neurotoxic, acting primarily at presynaptic sites, and that enzyme activity may be involved in this pharmacological action.

  1. Wilsonian Effective Action of Superstring Theory

    Sen, Ashoke

    2016-01-01

    By integrating out the heavy fields in type II or heterotic string field theory one can construct the effective action for the light fields. This effective theory inherits all the algebraic structures of the parent theory and the effective action automatically satisfies the Batalin-Vilkovisky quantum master equation. This theory is manifestly ultraviolet finite, has only light fields as its explicit degrees of freedom, and the Feynman diagrams of this theory reproduce the exact scattering amplitudes of light states in string theory to any arbitrary order in perturbation theory. Furthermore in this theory the degrees of freedom of light fields above certain energy scale are also implicitly integrated out. This energy scale is determined by a particular parameter labelling a family of equivalent actions, and can be made arbitrarily low, leading to the interpretation of the effective action as the Wilsonian effective action.

  2. Human pharmacology of ayahuasca: subjective and cardiovascular effects, monoamine metabolite excretion, and pharmacokinetics.

    Riba, Jordi; Valle, Marta; Urbano, Gloria; Yritia, Mercedes; Morte, Adelaida; Barbanoj, Manel J

    2003-07-01

    The effects of the South American psychotropic beverage ayahuasca on subjective and cardiovascular variables and urine monoamine metabolite excretion were evaluated, together with the drug's pharmacokinetic profile, in a double-blind placebo-controlled clinical trial. This pharmacologically complex tea, commonly obtained from Banisteriopsis caapi and Psychotria viridis, combines N,N-dimethyltryptamine (DMT), an orally labile psychedelic agent showing 5-hydroxytryptamine2A agonist activity, with monoamine oxidase (MAO)-inhibiting beta-carboline alkaloids (harmine, harmaline, and tetrahydroharmine). Eighteen volunteers with prior experience in the use of psychedelics received single oral doses of encapsulated freeze-dried ayahuasca (0.6 and 0.85 mg of DMT/kg of body weight) and placebo. Ayahuasca produced significant subjective effects, peaking between 1.5 and 2 h, involving perceptual modifications and increases in ratings of positive mood and activation. Diastolic blood pressure showed a significant increase at the high dose (9 mm Hg at 75 min), whereas systolic blood pressure and heart rate were moderately and nonsignificantly increased. Cmax values for DMT after the low and high ayahuasca doses were 12.14 ng/ml and 17.44 ng/ml, respectively. Tmax (median) was observed at 1.5 h after both doses. The Tmax for DMT coincided with the peak of subjective effects. Drug administration increased urinary normetanephrine excretion, but, contrary to the typical MAO-inhibitor effect profile, deaminated monoamine metabolite levels were not decreased. This and the negligible harmine plasma levels found suggest a predominantly peripheral (gastrointestinal and liver) site of action for harmine. MAO inhibition at this level would suffice to prevent first-pass metabolism of DMT and allow its access to systemic circulation and the central nervous system. PMID:12660312

  3. On String Field Theory and Effective Actions

    Giveon, Amit

    1992-01-01

    A truncation of string field theory is compared with the duality invariant effective action of $D=4, N=4$ heterotic strings to cubic order. The three string vertex must satisfy a set of compatibility conditions. Any cyclic three string vertex is compatible with the $D=4, N=4$ effective field theory. The effective actions may be useful in understanding the non--polynomial structure and the underlying symmetry of covariant closed string field theory, and in addressing issues of background indep...

  4. Characterization and comparison of sodium-glucose cotransporter 2 inhibitors in pharmacokinetics, pharmacodynamics, and pharmacologic effects.

    Tahara, Atsuo; Takasu, Toshiyuki; Yokono, Masanori; Imamura, Masakazu; Kurosaki, Eiji

    2016-03-01

    The sodium-glucose cotransporter (SGLT) 2 offer a novel approach to treating type 2 diabetes by reducing hyperglycaemia via increased urinary glucose excretion. In the present study, the pharmacokinetic, pharmacodynamic, and pharmacologic properties of all six SGLT2 inhibitors commercially available in Japan were investigated and compared. Based on findings in normal and diabetic mice, the six drugs were classified into two categories, long-acting: ipragliflozin and dapagliflozin, and intermediate-acting: tofogliflozin, canagliflozin, empagliflozin, and luseogliflozin. Long-acting SGLT2 inhibitors exerted an antihyperglycemic effect with lower variability of blood glucose level via a long-lasting increase in urinary glucose excretion. In addition, ipragliflozin and luseogliflozin exhibited superiority over the others with respect to fast onset of pharmacological effect. Duration and onset of the pharmacologic effects seemed to be closely correlated with the pharmacokinetic properties of each SGLT2 inhibitor, particularly with respect to high distribution and long retention in the target organ, the kidney. While all six SGLT2 inhibitors were significantly effective in increasing urinary glucose excretion and reducing hyperglycemia, our findings suggest that variation in the quality of daily blood glucose control associated with duration and onset of pharmacologic effects of each SGLT2 inhibitor might cause slight differences in rates of improvement in type 2 diabetes. PMID:26970780

  5. Pharmacological assessment of the onset of action of aclidinium and glycopyrronium versus tiotropium in COPD patients and human isolated bronchi.

    Rogliani, Paola; Calzetta, Luigino; Ora, Josuel; Lipsi, Roberto; Segreti, Andrea; Matera, Maria Gabriella; Cazzola, Mario

    2015-08-15

    Preclinical studies suggested that aclidinium and glycopyrronium might have a faster onset of action than tiotropium. In this study we assessed the onset of action of aclidinium and glycopyrronium versus tiotropium, all administered at the approved clinical doses, in patients with moderate-to-severe chronic obstructive pulmonary disease (COPD) and in human isolated bronchi by using different concentrations. Sixteen COPD patients inhaled single doses of aclidinium 400µg, glycopyrronium 50μg and tiotropium 18µg and FEV1 was measured to assess their onset of action. In human isolated bronchi the time to evoke half maximal relaxation of transmural stimulation was tested from 10nM to 1µM for each drug. Nine, eight and twelve patients did not achieve 15% increase of FEV1 after inhalation of aclidinium, glycopyrronium and tiotropium, respectively. Aclidinium (15.6±7.5min) and glycopyrronium (17.9±10.4min) enhanced 15% FEV1 more rapidly than tiotropium (42.5±19.4min), with no significant difference (P>0.05). In isolated airways, glycopyrronium elicited a dose-dependent onset of action (10nM: 8.2±1.3min, 100nM: 7.1±2.1min, 1μM: 3.4±0.4min) that was faster compared to that induced by aclidinium (1μM: 6.4±0.5min) and tiotropium (1μM: 8.4±1.1min) (Pglycopyrronium was faster than that induced by tiotropium, but since our analysis was restricted to the acute effect of these LAMAs and the inhaled doses were not isoeffective, the real differences in their impact on the onset of bronchodilation will be definitely determined after a long-term challenge of these treatments at isoeffective doses in COPD patients. PMID:25952728

  6. [Pharmacological action on emotional sphere with phenazepam and caffeine changes preference of ethanol in Wistar male rats].

    2014-01-01

    Earlier we have shown that essential for formation of preference to alcohol is not that much the initial anxiety level, but rather direction of its change in the process of forced alcoholization. The goal of this work was study of effect of change in the anxiety level on formation of action on the emotional sphere. Out of four groups, for 4 months of experiment, the 1st group had access only to the 10 % ethanol solution; the 2nd group--to the 10% ethanol with addition of 0.4 g/l caffeine; the 3rd - to 10% ethanol with 0.5 mg/l phenazepam; the 4th (control)--only to water. The anxiety level and behavioral parameters were estimated prior to the experiment and after each 5 weeks with aid of the test "the open field". Preference of ethanol was determined with aid of the test "the two-glass sample" before the experiment and each 4 weeks. In experimental groups of rats the long-term consumption of ethanol, of ethanol with caffeine, and of ethanol with phenazepam led to an increase in preference of alcohol as compared with control. A decrease of motor activity at the period of forced alcoholization was found to correlate positively with the low level of preference of alcohol. The rats consuming ethanol with caffeine and sensitive to action of the psychostimulator enhancing anxiety formed faster the preference to alcohol. In rats not sensitive to action of caffeine the preference to alcohol was not formed. Rats sensitive to the sedative action of phenazepam were less anxious and subsequently did not prefer alcohol. In rats not sensitive to phenazepam, anxiety was enhanced and preference to alcohol was formed. PMID:25508949

  7. Pharmacology Information System Ready

    Chemical and Engineering News, 1973

    1973-01-01

    Discusses the development and future of Prophet,'' a specialized information handling system for pharmacology research. It is designed to facilitate the acquisition and dissemination of knowledge about mechanisms of drug action, and it is hoped that it will aid in converting pharmacology research from an empirical to a predictive science. (JR)

  8. Dissociation of the Pharmacological Effects of THC by mTOR Blockade

    Puighermanal E; Busquets-Garcia A; Gomis-Gonz\\xe1lez M; Marsicano G; Maldonado R; Ozaita A.

    2013-01-01

    The potential therapeutic benefits of cannabinoid compounds have raised interest in understanding the molecular mechanisms that underlie cannabinoid-mediated effects. We previously showed that the acute amnesic-like effects of delta9-tetrahydrocannabinol (THC) were prevented by the subchronic inhibition of the mammalian target of rapamycin (mTOR) pathway. In the present study, we assess the relevance of the mTOR pathway in other acute and chronic pharmacological effects of THC. The rapamycin ...

  9. Effects of hormone treatment on sexual functioning in postmenopausal women: pharmacological intervention and female sexuality

    Nijland, Esmé Aurelia

    2008-01-01

    Effects of hormone treatment on sexual functioning in postmenopausal women. Pharmacological intervention and female sexuality: a complex, controversial clinical and social issue. The studies presented in this thesis have been conducted to investigate the effects of hormone therapy (HT) and tibolone on sexual function in postmenopausal women. Sufficient evidence for the effects of tibolone on sexual function and dysfunction in postmenopausal women was, until now not available. As tibolone does...

  10. [STUDYING SOME PHARMACOLOGICAL EFFECTS OF NEW 3-HYDROXYPYRIDINE DERIVATIVE].

    Yasnetsov, V V; Tsublova, E G; Yasnetsov, Vic V; Skachilova, S Ya; Karsanova, S K; Ivanov, Yu V

    2016-01-01

    It was established that a new 3-hydroxypyridine (3-HP) derivative, 2-ethyl-6-methyl-3-hydroxypyridine L-aspartate (3-HP), in small doses (1 and 5 mg/kg) increased physical performance in treadmill and swimming tests on rats. The new substance showed greater or equal effects compared to the reference actoprotector drugs metaprot and ladasten in much higher doses. The gluconeogenesis inhibitor tryptophan significantly (74 ± 5%, p nootropic drug piracetam in a dose of 200 mg/kg, but had equal effect with these drugs in doses of 50 and 800 mg/kg, respectively. 3-HPA (30 mg/kg per day) had neuroprotective effect in rats with brain ischemia and decreased the neurologic deficiency more effectively than mexidol (50 mg/kg per day). PMID:27416675

  11. Cost-effectiveness of pharmacological and psychosocial interventions for schizophrenia

    Phanthunane, Pudtan; Vos, Theo; Whiteford, Harvey; Bertram, Melanie

    2011-01-01

    Background Information on cost-effectiveness of interventions to treat schizophrenia can assist health policy decision making, particularly given the lack of health resources in developing countries like Thailand. This study aims to determine the optimal treatment package, including drug and non-drug interventions, for schizophrenia in Thailand. Methods A Markov model was used to evaluate the cost-effectiveness of typical antipsychotics, generic risperidone, olanzapine, clozapine and family i...

  12. Cost-effectiveness of pharmacological and psychosocial interventions for schizophrenia

    Vos Theo; Phanthunane Pudtan; Whiteford Harvey; Bertram Melanie

    2011-01-01

    Abstract Background Information on cost-effectiveness of interventions to treat schizophrenia can assist health policy decision making, particularly given the lack of health resources in developing countries like Thailand. This study aims to determine the optimal treatment package, including drug and non-drug interventions, for schizophrenia in Thailand. Methods A Markov model was used to evaluate the cost-effectiveness of typical antipsychotics, generic risperidone, olanzapine, clozapine and...

  13. Tri-partite complex for axonal transport drug delivery achieves pharmacological effect

    Frederickson Martyn

    2010-01-01

    Full Text Available Abstract Background Targeted delivery of pharmaceutical agents into selected populations of CNS (Central Nervous System neurons is an extremely compelling goal. Currently, systemic methods are generally used for delivery of pain medications, anti-virals for treatment of dermatomal infections, anti-spasmodics, and neuroprotectants. Systemic side effects or undesirable effects on parts of the CNS that are not involved in the pathology limit efficacy and limit clinical utility for many classes of pharmaceuticals. Axonal transport from the periphery offers a possible selective route, but there has been little progress towards design of agents that can accomplish targeted delivery via this intraneural route. To achieve this goal, we developed a tripartite molecular construction concept involving an axonal transport facilitator molecule, a polymer linker, and a large number of drug molecules conjugated to the linker, then sought to evaluate its neurobiology and pharmacological behavior. Results We developed chemical synthesis methodologies for assembling these tripartite complexes using a variety of axonal transport facilitators including nerve growth factor, wheat germ agglutinin, and synthetic facilitators derived from phage display work. Loading of up to 100 drug molecules per complex was achieved. Conjugation methods were used that allowed the drugs to be released in active form inside the cell body after transport. Intramuscular and intradermal injection proved effective for introducing pharmacologically effective doses into selected populations of CNS neurons. Pharmacological efficacy with gabapentin in a paw withdrawal latency model revealed a ten fold increase in half life and a 300 fold decrease in necessary dose relative to systemic administration for gabapentin when the drug was delivered by axonal transport using the tripartite vehicle. Conclusion Specific targeting of selected subpopulations of CNS neurons for drug delivery by axonal

  14. Cost-effectiveness of pharmacological and psychosocial interventions for schizophrenia

    Vos Theo

    2011-05-01

    Full Text Available Abstract Background Information on cost-effectiveness of interventions to treat schizophrenia can assist health policy decision making, particularly given the lack of health resources in developing countries like Thailand. This study aims to determine the optimal treatment package, including drug and non-drug interventions, for schizophrenia in Thailand. Methods A Markov model was used to evaluate the cost-effectiveness of typical antipsychotics, generic risperidone, olanzapine, clozapine and family interventions. Health outcomes were measured in disability adjusted life years. We evaluated intervention benefit by estimating a change in disease severity, taking into account potential side effects. Intervention costs included outpatient treatment costs, hospitalization costs as well as time and travel costs of patients and families. Uncertainty was evaluated using Monte Carlo simulation. A sensitivity analysis of the expected range cost of generic risperidone was undertaken. Results Generic risperidone is more cost-effective than typicals if it can be produced for less than 10 baht per 2 mg tablet. Risperidone was the cheapest treatment with higher drug costs offset by lower hospital costs in comparison to typicals. The most cost-effective combination of treatments was a combination of risperidone (dominant intervention. Adding family intervention has an incremental cost-effectiveness ratio of 1,900 baht/DALY with a 100% probability of a result less than a threshold for very cost-effective interventions of one times GDP or 110,000 baht per DALY. Treating the most severe one third of patients with clozapine instead of risperidone had an incremental cost-effectiveness ratio of 320,000 baht/DALY with just over 50% probability of a result below three times GDP per capita. Conclusions There are good economic arguments to recommend generic risperidone as first line treatment in combination with family intervention. As the uncertainty interval indicates

  15. [Dizziness as a side effect of pharmacological therapy].

    Borup Johansen, Nanna; Ayadipanah, Mahnaz; Sonnenschein, Emilie Sofia; Christensen, Hanne Rolighed; Jürgens, Gesche

    2013-11-01

    Dizziness is a well-known side effect of a wide range of drugs. However, the side effects reported in the summary of product characteristics are not exclusively based on placebo-controlled trials. Based on a systematic review of the literature including randomised placebo-controlled clinical trials, antihypertensive combination drugs, methylphenidate, high doses of tramadol and serotonin-norepinephrine reuptake inhibitors were associated with an increased risk of dizziness. Antihypertensive monotherapy and selective serotonin reuptake inhibitors were generally not associated with an increased risk of dizziness when compared with placebo. PMID:24629236

  16. Pharmacological effect on pyeloureteric dynamics with a clinical perspective

    Jung, Helene U; Frimodt-Møller, Poul C; Osther, Palle J;

    2006-01-01

    the existence of different receptors in the ureter and renal pelvis. The ureteric and pelvic responses to the corresponding neurotransmitters have been determined. It seems that alpha-adrenergic and cholinergic agents are stimulating whereas beta-adrenergic agents inhibit ureteric activity. The effect...

  17. Research Progress of Chemical Compositions and Pharmacological Actions of Mentha canadensis%薄荷化学成分与药理作用研究新进展

    沈梅芳; 李小萌; 单琪媛

    2012-01-01

    Through searching literatures about Mentha canadensis at home and abroad in recent years,it is to summarize the chemical compositions,pharmacological actions and modern application in clinic, providing theory foundation for further developing of Mentha canadensis.%通过对薄荷在近几年国内外化学研究、药理作用方面相关文献的查阅,以及现代临床应用等方面的研究情况进行了总结,为进一步合理开发利用薄荷提供理论依据.

  18. Action-based effects on music perception

    Pieter-Jan eMaes

    2014-01-01

    Full Text Available The classical, disembodied approach to music cognition conceptualizes action and perception as separate, peripheral phenomena. In contrast, embodied accounts to music cognition emphasize the central role of the close coupling of action and perception. It is a commonly established fact that perception spurs action tendencies. We present a theoretical framework capturing the ways that the human motor system, and the actions it produces, can reciprocally influence the perception of music. The cornerstone of this framework is the common coding theory postulating a representational overlap in the brain between the planning, the execution, and the perception of movement. The integration of action and perception in so-called internal models is explained as a result of associative learning processes. Characteristic of internal models is that they allow intended or perceived sensory states to be transferred into corresponding motor commands (inverse modelling, and vice versa, to predict the sensory outcomes of planned actions (forward modelling. Embodied accounts typically adhere to inverse modelling to explain action effects on music perception (Leman, 2007. We extent this account by pinpointing forward modelling as an alternative mechanism by which action can modulate perception. We provide an extensive overview of recent empirical evidence in support of this idea. Additionally, we demonstrate that motor dysfunctions can cause perceptual disabilities, supporting the main idea of the paper that the human motor system plays a functional role in auditory perception. The finding that music perception is shaped by the human motor system, and the action it produces, suggests that the musical mind is highly embodied. However, we advocate for a more radical approach to embodied (music cognition in the sense that it needs to be considered as a dynamic process, in which aspects of action, perception, introspection, and social interaction are of crucial

  19. Action-based effects on music perception.

    Maes, Pieter-Jan; Leman, Marc; Palmer, Caroline; Wanderley, Marcelo M

    2014-01-01

    The classical, disembodied approach to music cognition conceptualizes action and perception as separate, peripheral processes. In contrast, embodied accounts of music cognition emphasize the central role of the close coupling of action and perception. It is a commonly established fact that perception spurs action tendencies. We present a theoretical framework that captures the ways in which the human motor system and its actions can reciprocally influence the perception of music. The cornerstone of this framework is the common coding theory, postulating a representational overlap in the brain between the planning, the execution, and the perception of movement. The integration of action and perception in so-called internal models is explained as a result of associative learning processes. Characteristic of internal models is that they allow intended or perceived sensory states to be transferred into corresponding motor commands (inverse modeling), and vice versa, to predict the sensory outcomes of planned actions (forward modeling). Embodied accounts typically refer to inverse modeling to explain action effects on music perception (Leman, 2007). We extend this account by pinpointing forward modeling as an alternative mechanism by which action can modulate perception. We provide an extensive overview of recent empirical evidence in support of this idea. Additionally, we demonstrate that motor dysfunctions can cause perceptual disabilities, supporting the main idea of the paper that the human motor system plays a functional role in auditory perception. The finding that music perception is shaped by the human motor system and its actions suggests that the musical mind is highly embodied. However, we advocate for a more radical approach to embodied (music) cognition in the sense that it needs to be considered as a dynamical process, in which aspects of action, perception, introspection, and social interaction are of crucial importance. PMID:24454299

  20. Action-effect bindings and ideomotor learning in intention- and stimulus-based actions

    ArvidHerwig

    2012-10-01

    Full Text Available According to ideomotor theory, action-effect associations are crucial for voluntary action control. Recently, a number of studies started to investigate the conditions that mediate the acquisition and application of action-effect associations by comparing actions carried out in response to exogenous stimuli (stimulus-based with actions selected endogenously (intention-based. There is evidence that the acquisition and/or application of action-effect associations is boosted when acting in an intention-based action mode. For instance, bidirectional action-effect associations were diagnosed in a forced choice test phase if participants previously experienced action-effect couplings in an intention-based but not in a stimulus-based action mode. The present study aims at investigating effects of the action mode on action-effect associations in more detail. In a series of experiments, we compared the strength and durability of short-term action-effect associations (binding immediately following intention- as well as stimulus-based actions. Moreover, long-term action-effect associations (learning were assessed in a subsequent test phase. Our results show short-term action-effect associations of equal strength and durability for both action modes. However, replicating previous results, long-term associations were observed only following intention-based actions. These findings indicate that the effect of the action mode on long-term associations cannot merely be a result of accumulated short-term action-effect bindings. Instead, only those episodic bindings are selectively perpetuated or retrieved that integrate action-relevant aspects of the processing event, i.e., in case of intention-based actions, the link between action and ensuing effect.

  1. Principles of Safety Pharmacology

    Pugsley, M. K.; Authier, S; Curtis, M J

    2008-01-01

    Safety Pharmacology is a rapidly developing discipline that uses the basic principles of pharmacology in a regulatory-driven process to generate data to inform risk/benefit assessment. The aim of Safety Pharmacology is to characterize the pharmacodynamic/pharmacokinetic (PK/PD) relationship of a drug's adverse effects using continuously evolving methodology. Unlike toxicology, Safety Pharmacology includes within its remit a regulatory requirement to predict the risk of rare lethal events. Thi...

  2. Chemical compounds and pharmacological effects of Rabdosia excisa

    PANG Jinsong; YU Qian; LIU Bao

    2007-01-01

    Many kinds of diterpenoids have been isolated from Rabdosia spp.Some of them have anti-microbial effects,counteract inflammation,and inhibit tumor progression activities.We conducted the present study in order to look for bioactive compounds in the medicinal plant Rabdosia excisa.In this study,five compounds were isolated from R.excisa;they were oridonin,isokamebakaurin,oleanolie acid,ursolic acid,and β-sitosterol.In order to identify the function of the extracts,the activity of antibiotics,antioxidation,and immunity test were carried out against these functions.Prospective results were observed in all of the tested items.

  3. Pharmacological modulation of late radio-induced side effects

    After normal tissue exposure to radiation therapy, late side effects can occur and may reduce patients' quality of life due to their progressive nature. Late toxicities occurrence is the main limiting factor of radiotherapy. Various biological disorders related to irradiation are involved in the development of late toxicities including fibrosis. The present review will focus on the recent physiopathological and molecular mechanisms described to be involved in the development of late radio-induced toxicities, that provide therapeutic perspective for pharmaco-modulation. (authors)

  4. Effect of vitamin D status on pharmacological treatment efficiency

    Karczmarewicz, Elżbieta; Czekuć-Kryśkiewicz, Edyta; Płudowski, Paweł

    2013-01-01

    At least 80% of the whole Polish population, including prepubertal children and adolescents, adults and seniors, are vitamin D deficient, defined as 25(OH)D < 50 nmol/L. 83% of Polish newborns start their lives at the state of vitamin D deficiency because 78% of their mothers are also deficient. It was observed that treating patient vitamin D deficiency to vitamin D status serum 25(OH)D) 75–100 nmol/L increased effectiveness of therapies in infectious diseases (chronic hepatitis C, tuberculos...

  5. Effective actions for anomalous hydrodynamics

    We argue that an effective field theory of local fluid elements captures the constraints on hydrodynamic transport stemming from the presence of quantum anomalies in the underlying microscopic theory. Focussing on global current anomalies for an arbitrary flavour group, we derive the anomalous constitutive relations in arbitrary even dimensions. We demonstrate that our results agree with the constraints on anomaly governed transport derived hitherto using a local version of the second law of thermodynamics. The construction crucially uses the anomaly inflow mechanism and involves a novel thermofield double construction. In particular, we show that the anomalous Ward identities necessitate non-trivial interaction between the two parts of the Schwinger-Keldysh contour

  6. Pharmacological classification of the abuse-related discriminative stimulus effects of trichloroethylene vapor

    Shelton, Keith L.; Nicholson, Katherine L.

    2014-01-01

    Inhalants are distinguished as a class primarily based upon a shared route of administration. Grouping inhalants according to their abuse-related in vivo pharmacological effects using the drug discrimination procedure has the potential to provide a more relevant classification scheme to the research and treatment community. Mice were trained to differentiate the introceptive effects of the trichloroethylene vapor from air using an operant procedure. Trichloroethylene is a chlorinated hydrocar...

  7. The effect of learning styles and study behavior on success of preclinical students in pharmacology

    Halil Asci; Esin Kulac; Mekin Sezik; F Nihan Cankara; Ekrem Cicek

    2016-01-01

    Objectives: To evaluate the effect of learning styles and study behaviors on preclinical medical students′ pharmacology exam scores in a non-Western setting. Materials and Methods: Grasha-Reichmann Student Learning Study Scale and a modified Study Behavior Inventory were used to assess learning styles and study behaviors of preclinical medical students (n = 87). Logistic regression models were used to evaluate the independent effect of gender, age, learning style, and study behavior on ph...

  8. Mining Molecular Pharmacological Effects from Biomedical Text: a Case Study for Eliciting Anti-Obesity/Diabetes Effects of Chemical Compounds.

    Dura, Elzbieta; Muresan, Sorel; Engkvist, Ola; Blomberg, Niklas; Chen, Hongming

    2014-05-01

    In the pharmaceutical industry, efficiently mining pharmacological data from the rapidly increasing scientific literature is very crucial for many aspects of the drug discovery process such as target validation, tool compound selection etc. A quick and reliable way is needed to collect literature assertions of selected compounds' biological and pharmacological effects in order to assist the hypothesis generation and decision-making of drug developers. INFUSIS, the text mining system presented here, extracts data on chemical compounds from PubMed abstracts. It involves an extensive use of customized natural language processing besides a co-occurrence analysis. As a proof-of-concept study, INFUSIS was used to search in abstract texts for several obesity/diabetes related pharmacological effects of the compounds included in a compound dictionary. The system extracts assertions regarding the pharmacological effects of each given compound and scores them by the relevance. For each selected pharmacological effect, the highest scoring assertions in 100 abstracts were manually evaluated, i.e. 800 abstracts in total. The overall accuracy for the inferred assertions was over 90 percent. PMID:27485890

  9. Review on pharmacological and toxicologyical effects of oleum azadirachti oil

    Khaled MM Koriem

    2013-01-01

    Oleum azadirachti consists of the oil obtained from dried seeds of Azadirachta indica A. Juss. (family: Meliaceae). Local names of Azadirachta indica A. Juss. are Abodua, aforo-oyinbo, anwe egyane, arista, azad dirakht, azadarakht, azedarach and bead tree. Indigenous to India, and widely distributed in South and South-East Asia and cultivated in Africa, the South Pacific Islands, South and Central America and Australia, and in southern Florida and California, United States of America, it is a straight-boled deciduous tree, which is 6-25 m high. Bark is dark-brown, externally fissured with a buff inner surface and fibrous fracture. Leaves alternately arranged, pinnately compound and up to 40 cm long, and composed of 8-18 short-petiolate narrow-ovate, pointed and curved toothed leaflets, 3-10 cm long and 1-4 cm wide arranged in alternate pairs. The major constituents are oxidized tetranortriterpenes including azadirachtin (azadirachtin A), azadiriadione, epoxyazadiradione, azadirone, nimbidin, nimbin, deacetylnimbin, salannin, gedunin, mahmoodin, 17-hydroxydiradione and related derivatives. It is of various medicinal uses, such as a contraceptive for intravaginal use, a mosquito repellent, and treatment of vaginal infections, treatment of gastric ulcers, cardiovascular disease, malaria, rheumatism and skin disorders, external applications for treatment of septic wounds,ulcers and boils, treatment of allergic skin reactions, asthma, bruises, colic, conjunctivitis, dysmenorrhoea, fever, gout, headache, itching due to varicella, kidney stones, leukorrhoea, psoriasis, scabies, sprains and muscular pain, and wounds. It is also used as an emmenagogue, tonic, stomatic and vermicide. In conclusion, the plant oil had antifertility, antihyperglycaemic, anti-inflammatory, antimicrobial, antiviral, antiulcer, estrogenic, immune, contraceptive, antibacterial, insect repellent, and skin treatment effects.

  10. Review on pharmacological and toxicologyical effects of oleum azadirachti oil.

    Koriem, Khaled M M

    2013-10-01

    Oleum azadirachti consists of the oil obtained from dried seeds of Azadirachta indica A. Juss. (family: Meliaceae). Local names of Azadirachta indica A. Juss. are Abodua, aforo-oyinbo, anwe egyane, arista, azad dirakht, azadarakht, azedarach and bead tree. Indigenous to India, and widely distributed in South and South-East Asia and cultivated in Africa, the South Pacific Islands, South and Central America and Australia, and in southern Florida and California, United States of America, it is a straight-boled deciduous tree, which is 6-25 m high. Bark is dark-brown, externally fissured with a buff inner surface and fibrous fracture. Leaves alternately arranged, pinnately compound and up to 40 cm long, and composed of 8-18 short-petiolate narrow-ovate, pointed and curved toothed leaflets, 3-10 cm long and 1-4 cm wide arranged in alternate pairs. The major constituents are oxidized tetranortriterpenes including azadirachtin (azadirachtin A), azadiriadione, epoxyazadiradione, azadirone, nimbidin, nimbin, deacetylnimbin, salannin, gedunin, mahmoodin, 17-hydroxydiradione and related derivatives. It is of various medicinal uses, such as a contraceptive for intravaginal use, a mosquito repellent, and treatment of vaginal infections, treatment of gastric ulcers, cardiovascular disease, malaria, rheumatism and skin disorders, external applications for treatment of septic wounds, ulcers and boils, treatment of allergic skin reactions, asthma, bruises, colic, conjunctivitis, dysmenorrhoea, fever, gout, headache, itching due to varicella, kidney stones, leukorrhoea, psoriasis, scabies, sprains and muscular pain, and wounds. It is also used as an emmenagogue, tonic, stomatic and vermicide. In conclusion, the plant oil had antifertility, antihyperglycaemic, anti-inflammatory, antimicrobial, antiviral, antiulcer, estrogenic, immune, contraceptive, antibacterial, insect repellent, and skin treatment effects. PMID:24075352

  11. 绿茶多酚提取纯化工艺及药理作用%Extraction and purification technologies of green tea polyphenols and its pharmacological actions

    张思佳; 黄璐; 牟峰

    2013-01-01

    绿茶多酚是绿茶的主要有效成分,多年研究发现绿茶多酚具有抗氧化、抗癌、抗肥胖、抗紫外线、抗龋齿等药理作用,且对神经退行性疾病和心血管系统疾病有一定的防治作用.本文对绿茶多酚近年来的提取纯化工艺及药理作用进行阐述,为绿茶的进一步开发提供参考.%Green tea polyphenols,which are major chemical constituents from green tea,have great pharmacological actions,such as antioxidant,anticancer,anti-obesity,anti-UV,against dental caries,improving cardiovascular function and neurodegenerative diseases.This review focused on the advances on extraction,purification technologies and pharmacological actions of green tea polyphenols in recent years.

  12. 中药成分蓝雪醌的药理作用研究进展%Research Progress on Pharmacologic Actions of Plumbagin

    冯筱巍

    2015-01-01

    由于新药研发耗资大、周期长、风险高,越来越多的学者把目光投向天然产物的研究. 中药成分蓝雪醌是一种天然的α-萘醌类化合物,主要存在于紫金标、白花丹等药用植物中. 蓝雪醌的药理作用十分广泛,具有抗氧化、消炎止痛、抗肿瘤、抗菌等作用. 该文主要对蓝雪醌的药理作用及其作用机制进行总结归纳,为蓝雪醌的进一步开发利用提供思路.%Currently more and more scholars have focused on the research of natural compounds,as research and development of new drugs costs large investment,long period,and high risk.Plumbagin is one of the natural α-naphthoquinones compounds,it mainly exists in plumbago zeylanica and radix ceratostigmatis mini.It has been reported that the pharmacologic actions of plumbagin is widespread,including anti-oxidant, anti-inflammatory,antibacterial and anticancer.Here is to make a review of the pharmacologic actions and mechanism of plumbagin in order to provide new ideas for further development .

  13. Effects of non-pharmacological or pharmacological interventions to promote cognition and brain plasticity in aging individuals

    Valentina ePieramico

    2014-09-01

    Full Text Available Brain aging and aging-related neurodegenerative disorders are major health challenges faced by modern societies. Brain aging is associated with cognitive and functional decline and represents the favourable background for the onset and development of dementia. Brain aging is associated with early and subtle anatomo-functional physiological changes that often precede the appearance of clinical signs of cognitive decline. Neuroimaging approaches unveiled the functional correlates of these alterations and helped in the identification of therapeutic targets that can be potentially useful in counteracting age-dependent cognitive decline.A growing body of evidence supports the notion that cognitive stimulation and aerobic training can preserve and enhance operational skills in elderly individuals as well as reduce the incidence of dementia. This review aims at providing an extensive and critical overview of the most recent data that support the efficacy of non-pharmacological and pharmacological interventions aimed at enhancing cognition and brain plasticity in healthy elderly individuals as well as delaying the cognitive decline associated with dementia.

  14. Assessment of the effectiveness of non-pharmacological methods in pain relief during labor

    Samara Maria Borges Osório

    2014-04-01

    Full Text Available This is a systematic review that aimed to evaluate the effectiveness of non-pharmacological methods for pain relief during labor. The articles’ selection was based on BDENF, PubMed, LILACS and Cochrane Library, published between 2007 and 2012. One analyzed seven studies that assessed the non-pharmacological methods and met the eligibility criteria. It was evident that massage, aromatherapy, immersion bath, acupuncture and acupressure are effective methods to relieve pain during labor, because besides reducing pain perception, they still lower levels of anxiety and stress. Among them, the most efficient one was the massage, mainly when done in the first stage of labor. Furthermore, the interventions don’t interfere in the kind and duration of labor, being safe to clinical practice.

  15. Effectiveness of team based learning to teach pharmacology for phase-II MBBS students

    N.K. Hashilkar; M.H. Gelula

    2014-01-01

    Background: TBL (Team based Learning) instructional methods foster applying knowledge in a highly interactive setting. Furthermore, in contrast to PBL (Problem Based Learning), it is a teacher directed method that encourages student- student interaction. Objective: The present study is aimed to assess the effectiveness of TBL over the current conventional tutorial type of teaching-learning strategy. Materials and Methods: The present study was conducted in the department of pharmacology of KL...

  16. Effect of Disposition of Mannich Antimalarial Agents on Their Pharmacology and Toxicology

    Ruscoe, J. E.; Tingle, M. D.; O’Neill, P. M.; S.A. Ward; Park, B K

    1998-01-01

    The use of the antimalarial agent amodiaquine has been curtailed due to drug-induced idiosyncratic reactions. These have been attributed to the formation of a protein-reactive quinoneimine species via oxidation of the 4-aminophenol group. Therefore, the effects of chemical modifications on the disposition of amodiaquine in relation to its metabolism, distribution, and pharmacological activity have been investigated. The inclusion of a group at the C-5′ position of amodiaquine reduced or elimi...

  17. Progress of Chemical Composition and Pharmacological Effects of Meretrix meretrix Linnaeus

    Du; Zhengcai; Hou; Xiaotao; Huang; Qing; Deng; Jiagang; Fanshi; Fangcao

    2014-01-01

    Meretrix meretrix Linnaeus is a traditional marine drug. There are more than two thousand years of history using clamshell as a component of medicine.After a review of relevant literature at home and abroad for nearly 20 years,the author summarized chemical composition and pharmacological effects of M. meretrix,in order to provide a scientific basis for further development and utilization of M. meretrix.

  18. Combined pharmacological activation of AMPK and PPAR δ potentiates the effects of exercise in trained mice

    Manio, Mark Christian C.; Inoue, Kazuo; Fujitani, Mina; Matsumura, Shigenobu; Fushiki, Tohru

    2016-01-01

    Abstract The combined activation of the cellular energy sensor AMP‐activated protein kinase (AMPK) and the nuclear transcription factor peroxisome proliferator‐activated receptor delta (PPAR δ) has been demonstrated to improve endurance and muscle function by mimicking the effects of exercise training. However, their combined pharmacological activation with exercise training has not been explored. Balb/c mice were trained on a treadmill and administered both the AMPK activator AICAR and the P...

  19. Effective boundary action in fermion string theory

    Continual Polyakov integral for the Neveu-Schwarz-Ramon (NSR) type fermion string is calculated on the Riemann Surface with special choice of local boundary conditions for the fermion fields. The derived expressions are used when studying behaviour of the string Green function in configurational space. Generalization of the effective fermion action for the case of non-Archimedean strings is discussed. 11 refs

  20. Low energy effective actions with composite fields

    We investigate a Wilson real space renormalization gorup approach for theories in which composite fields are needed at low energies. It furnishes a sequence of effective actions SΛ which depend on an UV cut-off Λ. We adopt Wilsons fundamental postulate that these effective actions should be local. This is our basic guiding principle on how to construct ''blockspins'', i.e. the fields which appear in the effective actions. Given a fundamental high energy theory which does not contain composite fields we gradually integrate out high frequency modes in order to lower the cut-off Λ. Eventually appearing nonlocalities at some cut-off value Λc indicate the necessity to introduce new composite degrees of freedom into the theory. An analysis based on Symanzik's infinite set of Bethe-Salpeter equations for all n-point functions shows that a local low energy effective action containing composite fields can be constructed at the compositeness scale Λc. Further integration of high frequency modes generates new nonlocalities which can be absorbed into the composite degrees of freedom. There are indications from an 1/N expansion that this suffices already to eliminate high energy degrees of freedom from the composite field so that no separate integration is needed to achieve this. In general the composite field will have self interactions. (orig.)

  1. Holographic effective actions from black holes

    Using the Wald's relation between the Noether charge of diffeomorphisms and the entropy for a generic spacetime possessing a bifurcation surface, we introduce a method to obtain a family of higher order derivatives effective actions from the entropy of black holes. We consider the entropy as the starting point and we analyze the procedure of derivation of the action functional. We specialize to a particular class of theories which simplifies the calculations, f(R) theories. We apply the procedure to loop quantum gravity and to a general class of log-corrected entropy formulas.

  2. Modafinil and γ-hydroxybutyrate have sleep state-specific pharmacological actions on hypocretin-1 physiology in a primate model of human sleep

    Zeitzer, Jamie M.; Buckmaster, Christine L.; Landolt, Hans-Peter; David M Lyons; Mignot, Emmanuel

    2009-01-01

    Hypocretin-1 is a hypothalamic neuropeptide that is important in the regulation of wake and the lack of which results in the sleep disorder narcolepsy. Using a monkey that has consolidated wake akin to humans, we examined pharmacological manipulation of sleep and wake and its effects on hypocretin physiology. Monkeys were given the sleep-inducing gamma-hydroxybutyrate (GHB) and the wake-inducing modafinil both in the morning and in the evening. Cerebrospinal fluid (CSF) hypocretin-1 concentra...

  3. Effect of Fuzheng Huayu formula and its actions against liver fibrosis

    Xu Lieming

    2009-06-01

    Full Text Available Abstract Liver fibrosis is a common histological process to develop into cirrhosis in various chronic liver diseases including chronic hepatitis and fatty liver. Therefore anti-liver fibrosis is very important strategy to treat chronic liver diseases. Fuzheng Huayu (FZHY, a preparation containing herbs such as Radix Salvia Miltiorrhizae, Cordyceps, Semen Persicae, was formulated on the basis of Chinese medicine theory in treating liver fibrosis and was approved. Pharmacological studies and clinical trials demonstrate that FZHY has a significant effect against liver fibrosis and that many of the pharmacological actions are attributable to the effect. This article reviews the effects and actions of FZHY, in particular the effects observed from clinical trials in treating liver fibrosis caused by chronic hepatitis B and the actions on inhibition of hepatic stellate cell activation, protection of hepatocytes and inhibition of hepatic sinusoidal capillarization. This article also reviews the coordinated effects of the constituent herbs of FZHY and the actions of their active compounds such as salvianonic acid B (SA-B on liver fibrosis.

  4. Symmetry-improved CJT effective action

    The formalism introduced by Cornwall, Jackiw and Tomboulis (CJT) provides a systematic approach to consistently resumming non-perturbative effects in Quantum Thermal Field Theory. One major limitation of the CJT effective action is that its loopwise expansion introduces residual violations of possible global symmetries, thus giving rise to massive Goldstone bosons in the spontaneously broken phase of the theory. In this paper we develop a novel symmetry-improved CJT formalism for consistently encoding global symmetries in a loopwise expansion. In our formalism, the extremal solutions of the fields and propagators to a loopwise truncated CJT effective action are subject to additional constraints given by the Ward Identities due to global symmetries. By considering a simple O(2) scalar model, we show that, unlike other methods, our approach satisfies a number of important field-theoretic properties. In particular, we find that the Goldstone boson resulting from spontaneous symmetry breaking of O(2) is massless and the phase transition is a second-order one, already in the Hartree–Fock approximation. After taking the sunset diagrams into account, we show how our approach properly describes the threshold properties of the massless Goldstone boson and the Higgs particle in the loops. Finally, assuming minimal modifications to the Hartree–Fock approximated CJT effective action, we calculate the corresponding symmetry-improved CJT effective potential and discuss the conditions for its uniqueness for scalar-field values away from its minimum

  5. Evaluation of Behavioral and Pharmacological Effects of Hydroalcoholic Extract of Valeriana prionophylla Standl. from Guatemala

    Iandra Holzmann

    2011-01-01

    Full Text Available There are few studies on the pharmacological properties of Valeriana prionophylla Standl. (VP, known as “Valeriana del monte”, and used in Mesoamerican folk medicine to treat sleep disorders. This study examines the pharmacological effects of the hydroalcoholic extract of the dry rhizome using the open field, rota rod, elevated plus-maze (EPM, forced swimming (FST, strychnine- and pentobarbital-induced sleeping time, PTZ-induced seizures, and the inhibitory avoidance tests. VP did not show any protective effect against PTZ-induced convulsions. In the EPM, exhibited an anxiolytic-like effect through the effective enhancement of the entries (38.5% and time spent (44.7% in the open arms, when compared with control group. Time spent and the numbers of entrances into the enclosed arms were decreased, similar to those effects observed with diazepam. In the FST, acute treatment with VP, produced a dose-dependent decrease in immobility time, similarly to imipramine. VP also produced a significant dose-dependent decrease in the latency of sleeping time, while producing an increase in total duration of sleep; influenced memory consolidation of the animals only at lower doses, unlike those that produced anti-depressant and anxiolytic effects. In summary, the results suggest that VP presents several psychopharmacological activities, including anxiolytic, antidepressant, and hypno-sedative effects.

  6. Pharmacological Effects of Active Compounds on Neurodegenerative Disease with Gastrodia and Uncaria Decoction, a Commonly Used Poststroke Decoction

    Stanley C. C. Chik

    2013-01-01

    Full Text Available Neurodegenerative diseases refer to the selective loss of neuronal systems in patients. The diseases cause high morbidity and mortality to approximately 22 million people worldwide and the number is expected to be tripled by 2050. Up to now, there is no effective prevention and treatment for the neurodegenerative diseases. Although some of the clinical therapies target at slowing down the progression of symptoms of the diseases, the general effectiveness of the drugs has been far from satisfactory. Traditional Chinese medicine becomes popular alternative remedies as it has been practiced clinically for more than thousands of years in China. As neurodegenerative diseases are mediated through different pathways, herbal decoction with multiple herbs is used as an effective therapeutic approach to work on multiple targets. Gastrodia and Uncaria Decoction, a popular TCM decoction, has been used to treat stroke in China. The decoction contains compounds including alkaloids, flavonoids, iridoids, carotenoids, and natural phenols, which have been found to possess anti-inflammatory, antioxidative, and antiapoptotic effects. In this review, we will summarize the recent publications of the pharmacological effects of these five groups of compounds. Understanding the mechanisms of action of these compounds may provide new treatment opportunities for the patients with neurodegenerative diseases.

  7. 小槐花水提物药理作用研究%Study on Pharmacological Action of Aqueous Extract from Desmodium Caudatum

    李燕婧; 钟正贤; 卢文杰

    2013-01-01

      目的:观察小槐花水提物的药理作用.方法:采用对戊巴比妥钠小鼠睡眠时间的影响实验;小鼠醋酸扭体法;小鼠碳末廓清法和对正常小鼠血清SOD活性和MDA含量的影响实验,以及急性毒性试验.结果:小槐花水提物能明显促进小鼠睡眠并延长其睡眠时间,减少醋酸所致的小鼠扭体反应次数,能提高单核巨噬细胞吞噬指数,降低小鼠血清MDA含量,同时提高SOD活性.小鼠最大给药量为220.5g生药/kg.结论:提示小槐花水提物具有明显的镇静催眠,镇痛,免疫增强和抗氧化作用,且毒性较低.%Objective: To observe the pharmacological action of aqueous extract from Desmodium Caudatum. Methods: The experience was made with pentobarbital-induced hypnosis in mice, the rat's body torsion test, the rat carbo clearance method for Serum SOD and MDA in normal mice and acute toxicity test. Results: Aqueous Extract from Desmodium Caudatum can obviously facilitate sleep, extend sleep time, reduce the body torsion induced by acetic acid, enhance the mononuclear macrophage phagocytic index, reduce the blood serum content of MDA and improve the activity of SOD in mice. The maxi-mum dosage was 220.5 g crude drug/kg. Conclusion: Aqueous Extract from Desmodium Caudatum can provide obvious sedative, hypnotic, analgesia, immune enhancement and antioxygenation effects,with low toxicity.

  8. Cosmic fluctuations from quantum effective action

    Wetterich, C

    2015-01-01

    Does the observable spectrum of cosmic fluctuations depend on detailed initial conditions? This addresses the question if the general inflationary paradigm is sufficient to predict within a given model the spectrum and amplitude of cosmic fluctuations, or if additional particular assumptions about the initial conditions are needed. The answer depends on the number of e-foldings $N_{in}$ between the beginning of inflation and horizon crossing of the observable fluctuations. We discuss an interacting inflaton field in an arbitrary homogeneous and isotropic geometry, employing the quantum effective action $\\Gamma$. An exact time evolution equation for the correlation function involves the second functional derivative $\\Gamma^{(2)}$. The operator formalism and quantum vacua for interacting fields are not needed. Use of the effective action also allows one to address the change of frames by field transformations (field relativity). For not too large $N_{in}$ we find that memory of the initial conditions is preserv...

  9. Effectively Discriminating Fighting Shots in Action Movies

    Shu-Gao Ma; Wei-Qiang Wang

    2011-01-01

    Fighting shots are the highlights of action movies and an effective approach to discriminating fighting shots is very useful for many applications, such as movie trailer construction, movie content filtering, and movie content retrieval. In this paper, we present a novel method for this task. Our approach first extracts the reliable motion information of local invariant features through a robust keypoint tracking computation; then foreground keypoints are distinguished from background keypoints by a sophisticated voting process; further, the parameters of the camera motion model is computed based on the motion information of background keypoints, and this model is then used as a reference to compute the actual motion of foreground keypoints; finally, the corresponding feature vectors are extracted to characterizing the motions of foreground keypoints, and a support vector machine (SVM) classifier is trained based on the extracted feature vectors to discriminate fighting shots. Experimental results on representative action movies show our approach is very effective.

  10. Effective action in general chiral superfield model

    Petrov, A. Yu.

    2000-01-01

    The effective action in general chiral superfield model with arbitrary k\\"{a}hlerian potential $K(\\bar{\\Phi},\\Phi)$ and chiral (holomorphic) potential $W(\\Phi)$ is considered. The one-loop and two-loop contributions to k\\"{a}hlerian effective potential and two-loop (first non-zero) contribution to chiral effective potential are found for arbitrary form of functions $K(\\bar{\\Phi},\\Phi)$ and $W(\\Phi)$. It is found that despite the theory is non-renormalizable in general case two-loop contributi...

  11. Pharmacology in space. Part 2. Controlling motion sickness

    Lathers, C. M.; Charles, J. B.; Bungo, M. W.

    1989-01-01

    In this second article in the two-part series on pharmacology in space, Claire Lathers and colleagues discuss the pharmacology of drugs used to control motion sickness in space and note that the pharmacology of the 'ideal' agent has yet to be worked out. That motion sickness may impair the pharmacological action of a drug by interfering with its absorption and distribution because of alteration of physiology is a problem unique to pharmacology in space. The authors comment on the problem of designing suitable ground-based studies to evaluate the pharmacological effect of drugs to be used in space and discuss the use of salivary samples collected during space flight to allow pharmacokinetic evaluations necessary for non-invasive clinical drug monitoring.

  12. Ways of pharmacological prophylaxis of stochastic and deterministic effects of chronical radiation exposure

    The prophylactics of late effects of exposure is the actual medico-social problem, because now there are large groups of persons who were exposed during occupational contact and living on territories contaminated by radionuclides. Most probable consequences of external and internal chronic influence of radiation may be the increase of malignant tumour frequency, the development of secondary myelo- and immuno-depressions, the earlier forming of sclerous and destructive processes, and the acceleration of senescence. The role of damages in immune system was not yet understood in pathogenesis of the late effects of radiation, but there are evidences that the decreasing of the immunologic supervision in period of forming the consequences of radiation influence enables to realize the cancerogenic effect of radiation. The purposes of this investigation are to decrease the frequency or to prevent the development of radiation consequences dangerous for health and life by using the method of modification of radiogenic damages in hemopoietic and immune systems by applying the pharmacological preparations with immunomodulating effects. The investigation tasks include: the study of modifying influence of pharmacological substances with different mechanisms of effect: myelopid (immunomodulating, and regulatory), β-carotin, Calendula officinalis (immunomodulating, and antioxidant), lipamid (detoxicating); the separate or complex applications of these substances; and the development of the optimum medico-prophylactic schemes. The advantages of these indicated preparations in comparison with the known (T-activin, thymogen, cytokines, etc.) are the absence of contraindications and the possibility to use per os. (author)

  13. Botanical characteristics, pharmacological effects and medicinal compo-nents of Korean Panax ginseng C A Meyer

    Kwang-tae CHOI

    2008-01-01

    Korean Panax ginseng C A Meyer is mainly used to maintain the homeostasis of the body, and the pharmacological efficacy of Korean ginseng identified by modern science includes improved brain function, pain-relieving effects, pre-ventive effects against tumors as well as anti-tumor activity, enhanced immune system function, anti-diabetic effects, enhanced liver function, adjusted blood pressure, anti-fatigue and anti-stress effects, improved climacteric disorder and sexual functions, as well as anti-oxidative and anti-aging effects. Further clini-cal studies of these pharmacological efficacies will continue to be carried out. Korean ginseng is found to have such main properties as ginsenoside, ployacety-lene, acid polysaccharide, anti-oxidative aromatic compound, and insulin-like acid peptides. The number of ginsenoside types contained in Korean ginseng (38 ginsenosides) is substantially more than that of ginsenoside types contained in American ginseng (19 ginsenosides). Furthermore, Korean ginseng has been identified to contain more main non-saponin compounds, phenol compounds, acid polysaccharides and polyethylene compounds than American ginseng and Sanchi ginseng.

  14. Instant Attraction: Immediate Action-Effect Bindings Occur for Both, Stimulus- and Goal-Driven Actions

    Janczyk, Markus; Heinemann, Alexander; Pfister, Roland

    2012-01-01

    Flexible behavior is only possible if contingencies between own actions and following environmental effects are acquired as quickly as possible; and recent findings indeed point toward an immediate formation of action-effect bindings already after a single coupling of an action and its effect. The present study explored whether these short-term bindings occur for both, stimulus- and goal-driven actions (“forced-choice actions” vs. “free-choice actions”). Two experiments confirmed that immedia...

  15. Instant attraction: Immediate action-effect bindings occur for both, stimulus- and goal-driven actions

    MarkusJanczyk

    2012-10-01

    Full Text Available Flexible behavior is only possible if contingencies between own actions and following environmental effects are acquired as quickly as possible; and recent findings indeed point toward an immediate formation of action-effect bindings already after a single coupling of an action and its effect. The present study explored whether these short-term bindings occur for both, stimulus- and goal-driven actions (“forced-choice actions” vs. “free-choice actions”. Two experiments confirmed that immediate action-effect bindings are formed for both types of actions and affect upcoming behavior. These findings support the view that action-effect binding is a ubiquitous phenomenon which occurs for any type of action.

  16. Effective action approach to quantum chromodynamics

    Though the Lagrangian of quantum chromodynamics is well known, it has proven extremely difficult to derive precisely all its consequences to compare with experiment. Approximations based on physical reasoning must be made. One method is to calculate the effective action for some particularly simple configuration of gluons and use this to analyze an arbitrary system of interacting quarks. In the first chapter, the one-loop correction to the gluon propagator is computed in two different ways - dimensional regularization and Schwinger's proper time method. The renormalization mass parameters appearing in the two treatments can then be related and the exact one-loop effective action of a constant gluon field can be expressed in terms of the experimentally determinable Λ/sub MS/. In the following chapter, the interaction of a heavy quark-antiquark pair governed by this action is considered and it is shown how the spectrum, and, in particular, the spin splittings of the bound states can be found. Due to asymptotic freedom, a massive quarkonium is analogous to a non-relativistic electromagnetic system. At short distances, the results are the same as those derived from perturbation theory though, for example, the hyperfine structure arises in a different way. At large distances, the analysis is qualitative but our results agree with the predictions of strong coupling lattice gauge theories

  17. Effective actions for relativistic fluids from holography

    de Boer, Jan; Pinzani-Fokeeva, Natalia

    2015-01-01

    Motivated by recent progress in developing action formulations of relativistic hydrodynamics, we use holography to derive the low energy dissipationless effective action for strongly coupled conformal fluids. Our analysis is based on the study of novel double Dirichlet problems for the gravitational field, in which the boundary conditions are set on two codimension one timelike hypersurfaces (branes). We provide a geometric interpretation of the Goldstone bosons appearing in such constructions in terms of a family of spatial geodesics extending between the ultraviolet and the infrared brane. Furthermore, we discuss supplementing double Dirichlet problems with information about the near-horizon geometry. We show that upon coupling to a membrane paradigm boundary condition, our approach reproduces correctly the complex dispersion relation for both sound and shear waves. We also demonstrate that upon a Wick rotation, our formulation reproduces the equilibrium partition function formalism, provided the near-horiz...

  18. From action intentions to action effects: how does the sense of agency come about?

    Valérian Chambon; Nura Sidarus

    2014-01-01

    Sense of agency refers to the feeling of controlling an external event through one’s own action. On one influential view, agency depends on how predictable the consequences of one’s action are, getting stronger as the match between predicted and actual effect of an action gets closer. Thus, sense of agency arises when external events that follow our action are consistent with predictions of action effects made by the motor system while we perform or simply intend to perform an action. Accordi...

  19. Cosmic fluctuations from a quantum effective action

    Wetterich, C.

    2015-10-01

    Does the observable spectrum of cosmic fluctuations depend on detailed initial conditions? This addresses the question if the general inflationary paradigm is sufficient to predict within a given model the spectrum and amplitude of cosmic fluctuations, or if additional particular assumptions about the initial conditions are needed. The answer depends on the number of e -foldings Nin between the beginning of inflation and horizon crossing of the observable fluctuations. We discuss an interacting inflaton field in an arbitrary homogeneous and isotropic geometry, employing the quantum effective action Γ . An exact time evolution equation for the correlation function involves the second functional derivative Γ(2 ) . The operator formalism and quantum vacua for interacting fields are not needed. Use of the effective action also allows one to address the change of frames by field transformations (field relativity). Within the approximation of a derivative expansion for the effective action we find the most general solution for the correlation function, including mixed quantum states. For not too large Nin the memory of the initial conditions is preserved. In this case the cosmic microwave background cannot disentangle between the initial spectrum and its processing at horizon crossing. The inflaton potential cannot be reconstructed without assumptions about the initial state of the universe. We argue that for very large Nin a universal scaling form of the correlation function is reached for the range of observable modes. This can be due to symmetrization and equilibration effects, not yet contained in our approximation, which drive the short distance tail of the correlation function toward the Lorentz invariant propagator in flat space.

  20. Understanding Medicines: Conceptual Analysis of Nurses' Needs for Knowledge and Understanding of Pharmacology (Part I). Understanding Medicines: Extending Pharmacology Education for Dependent and Independent Prescribing (Part II).

    Leathard, Helen L.

    2001-01-01

    Part I reviews what nurses need to know about the administration and prescription of medicines. Part II addresses drug classifications, actions and effects, and interactions. Also discussed are the challenges pharmacological issues pose for nursing education. (SK)

  1. Studies in neuroendocrine pharmacology

    Maickel, R. P.

    1976-01-01

    The expertise and facilities available within the Medical Sciences Program section on Pharmacology were used along with informational input from various NASA sources to study areas relevant to the manned space effort. Topics discussed include effects of drugs on deprivation-induced fluid consumption, brain biogenic amines, biochemical responses to stressful stimuli, biochemical and behavioral pharmacology of amphetamines, biochemical and pharmacological studies of analogues to biologically active indole compounds, chemical pharmacology: drug metabolism and disposition, toxicology, and chemical methodology. Appendices include a bibliography, and papers submitted for publication or already published.

  2. Effective action of domain wall networks

    U(NC) gauge theory with NF fundamental scalars admits BPS junctions of domain walls. When the networks/webs of these walls contain loops, their size moduli give localized massless modes. We construct Kaehler potential of their effective action. In the large size limit Kaehler metric is well approximated by kinetic energy of walls and junctions, which is understood in terms of tropical geometry. Kaehler potential can be expressed in terms of hypergeometric functions that are useful to understand small size behavior. Even when the loop shrinks, the metric is regular with positive curvature. Moduli space of a single triangle loop has a geometry between a cone and a cigar

  3. Effective actions for statistical data assimilation

    Data assimilation is a problem in estimating the fixed parameters and state of a model of an observed dynamical system as it receives inputs from measurements passing information to the model. Using methods developed in statistical physics, we present effective actions and equations of motion for the mean orbits associated with the temporal development of a dynamical model when it has errors, there is uncertainty in its initial state, and it receives information from noisy measurements. If there are statistical dependences among errors in the measurements they can be included in this approach.

  4. The ventral surface of the medulla in the rat: pharmacologic and autoradiographic localization of GABA-induced cardiovascular effects.

    Keeler, J R; Shults, C W; Chase, T N; Helke, C J

    1984-04-16

    Experiments were done to evaluate a rat model for studying the cardiovascular effects of pharmacological manipulations of the ventral surface of the medulla. GABAergic drugs were used because of their well-characterized actions at the ventral surface of the medulla in the cat. GABA and muscimol, applied to the exposed ventral surface with filter paper pledgets, produced dose-dependent decreases in heart rate (HR) and mean arterial pressure (MAP) which were reversed with bicuculline but not with strychnine. Bicuculline alone raised HR and MAP. The GABA- or bicuculline-induced cardiovascular effects were mediated primarily by inhibition of sympathetic outflow. The most sensitive site was localized to an intermediate area on the ventral surface of the medulla, between the trapezoid body and exits of the hypoglossal nerves and just lateral to the pyramids. Topical application of [3H]GABA to the intermediate area resulted in labeling that was concentrated at the site of application, and which penetrated the parenchyma 1 mm dorsally. The heaviest labeling was found primarily in the ventral halves of the lateral paragigantocellular nuclei. No tritium was detected in peripheral blood. These data provide evidence for a neuronal system at the ventral medullary surface of the rat which influences sympathetic outflow and is modulated by GABA. PMID:6326937

  5. Effective action calculation in lattice QCD

    A method (called the effective action method) devised to make analytic calculations in Quantum Chromodynamics in the region of strong coupling is presented. First, the author deals with developing the calculation of a strong coupling expansion of the generating functional for gauge systems on a lattice with arbitrary sources. An accompanying manual describes the implementation of this calculation on a computer. The next step consists of substituting the expressions for the one-link free energies for a specific gauge group in the result of the previous calculation. This process of substitution, together with the replacement of the sources by a bilinear combination of fermion fields, is described for the group SU(3). More details on the implementation of the substitution scheme on a computer can be found in the accompanying manual. From the effective action thus obtained in terms of meson fields and baryon fields the Green functions of the theory can be derived. As an illustrative application the effective potential determining the vacuum expectation value of the meson field is calculated. (Auth.)

  6. Prenatal manipulation of the serotonergic system: Biochemical, pharmacological and behavioral effects

    Shemer, A.V.

    1988-01-01

    Rat pups were exposed in utero to pharmacological agents that stimulated or diminished serotonergic activity in vivo. Dams received 5-Methoxytryptamine 1mg/kg, from day 12 of gestation to birth, or parachlorophenylalanine, the serotonin synthesis inhibitor, from day 7 to 17 of gestation. Both groups of offspring showed significant reductions in the specific high affinity uptake of {sup 3}H-5-HT into brainstem and forebrain areas on postnatal days 1, 15, and 30, indicating reduced outgrowth of serotonin. At 15 days of age, both groups of treated offspring showed deficits in activity and in performing behaviors that required inhibition, but these deficits were no longer apparent on Day 30. Dose response experiments for 5-MT produced a dual effect: enhanced uptake in forebrain and inhibition of uptake in brainstem and forebrain on postnatal days 1, 15 and 30. Prenatal 5-MT caused deficits in avoidance and activity. Prenatal exposure to PAT, the 5-HT{sub 1a} agonist caused reduced uptake in brainstem, while exposure to TFMPP (the 5-HT{sub 1b} agonist) produced enhanced uptake in forebrain, as did the high dose of 5-MT. Sensitivity of the pharmacological response to acute 5-MT, 1 mg/kg, and apomorphine, 5 mg/kg was measured in an activity test.

  7. Effects of modified pharmacologic stress approaches on hyperemic myocardial blood flow

    Czernin, J.; Auerbach, M.; Sun, K.T. [Univ. of California, Los Angeles, CA (United States)] [and others

    1995-04-01

    Pharmacologic stress testing with 0.56 mg/kg of intravenous dipyridamole is frequently used to noninvasively detect coronary artery disease (CAD). However, high-dose dipyridamole (0.80 mg/kg) or the combination of standard-dose dipyridamole (0.56 mg/kg) with the isometric handgrip maneuver might evoke a greater coronary hyperemic response. To evaluate the effect of modified pharmacologic stress tests, myocardial blood flow was quantified in 11 male subjects (mean age: 27 {plus_minus} 7 yr) during standard-dose dipyridamole (0.56 mg/kg), high-dose dipyridamole (0.80 mg/kg) and standard-dose dipyridamole combined with the isometric handgrip exercise using dynamic PET and a two-compartment model for {sup 13}N-ammonia. Systolic blood pressure, heart rate and rate pressure product remained unchanged from standard to high-dose dipyridamole but increased with the addition of the isometric handgrip. Myocardial blood flow was unchanged from standard to high-dose dipyridamole but was lower with the addition of the isometric handgrip. The hyperemic response induced by standard-dose dipyridamole cannot be further enhanced by high-dose dipyridamole. The addition of the isometric handgrip exercise results in a modest, but significant decline in hyperemic blood flow possibly due to increased extravascular resistive forces or an increase in a mediated coronary vasoconstriction associated with exercise. 31 refs., 2 figs., 1 tab.

  8. Prenatal manipulation of the serotonergic system: Biochemical, pharmacological and behavioral effects

    Rat pups were exposed in utero to pharmacological agents that stimulated or diminished serotonergic activity in vivo. Dams received 5-Methoxytryptamine 1mg/kg, from day 12 of gestation to birth, or parachlorophenylalanine, the serotonin synthesis inhibitor, from day 7 to 17 of gestation. Both groups of offspring showed significant reductions in the specific high affinity uptake of 3H-5-HT into brainstem and forebrain areas on postnatal days 1, 15, and 30, indicating reduced outgrowth of serotonin. At 15 days of age, both groups of treated offspring showed deficits in activity and in performing behaviors that required inhibition, but these deficits were no longer apparent on Day 30. Dose response experiments for 5-MT produced a dual effect: enhanced uptake in forebrain and inhibition of uptake in brainstem and forebrain on postnatal days 1, 15 and 30. Prenatal 5-MT caused deficits in avoidance and activity. Prenatal exposure to PAT, the 5-HT1a agonist caused reduced uptake in brainstem, while exposure to TFMPP (the 5-HT1b agonist) produced enhanced uptake in forebrain, as did the high dose of 5-MT. Sensitivity of the pharmacological response to acute 5-MT, 1 mg/kg, and apomorphine, 5 mg/kg was measured in an activity test

  9. Exploring soft constraints on effective actions

    Bianchi, Massimo; Huang, Yu-tin; Lee, Chao-Jung; Wen, Congkao

    2016-01-01

    We study effective actions for simultaneous breaking of space-time and internal symmetries. Novel features arise due to the mixing of Goldstone modes under the broken symmetries which, in contrast to the usual Adler's zero, leads to non-vanishing soft limits. Such scenarios are common for spontaneously broken SCFT's. We explicitly test these soft theorems for $\\mathcal{N}=4$ sYM in the Coulomb branch both perturbatively and non-perturbatively. We explore the soft constraints systematically utilizing recursion relations. In the pure dilaton sector of a general CFT, we show that all amplitudes up to order $s^{n} \\sim \\partial^{2n}$ are completely determined in terms of the $k$-point amplitudes at order $s^k$ with $k \\leq n$. Terms with at most one derivative acting on each dilaton insertion are completely fixed and coincide with those appearing in the conformal DBI, i.e. DBI in AdS. With maximal supersymmetry, the effective actions are further constrained, leading to new non-renormalization theorems. In particu...

  10. Chemical compsition and pharmacological action of jojoba:research advances%好好芭化学组成及药理作用研究进展

    杨雪鸥; 吴然; 张林; 耿红卫

    2014-01-01

    Jojoba(the plant belonging to Simmondsiaceae)seeds are not only a kind of global special oil resources but also a type of good folk medicines because they are riched in jojoba oil and simmondsin and have many pharmacological effects such as anti-inflammatory effect,food inhibitor and promoting-antibiosis. The paper reviews the studies on jojoba chemical compositim, extraction and purification,detection and analysis methods,pharmacological activity and dosage development,in order to provide reference for further research and application.%加州西蒙得木(好好芭)属西蒙得木科植物,其种子不仅是世界特种油料的宝库,也是良好的药用资源,富含好好芭油和西蒙得木素,具有抗炎、减肥以及促抗菌等功效。本文综述了好好芭的药学研究进展,包括化学成分及提取方法、检测方法、药理作用及制剂研究等方面的内容,为好好芭的进一步研究开发提供参考。

  11. 姜黄素药理作用及其机制研究进展%Research progress of curcumin pharmacological action and mechanism

    刘红艳; 王海燕; 叶松

    2012-01-01

    Curcumin is a phenolic pigment of the ginger family Curcuma root-Curcuma longa L, it is the effective drug monomer. Turmeric is a commonly used traditional Chinese medicine, mainly growing in Japan, the United States, Africa, China and so on. Pharmacological studies suggest, curcumin possesses anti-inflammatory, antioxidant, anticoagulation, hypolipidemic, scavenging free radicals, atherosclerosis and inhibits tumor growth in many aspects such as the function, diseases of the cardiovascular system also has a certain role. This paper discusses the pharmacological effect of curcumin and its clinical application.%姜黄素是一种从姜黄提取的酚类色素,有效的药物单体.药理研究表明,姜黄素具有抗炎、抗凝、降血脂、抗氧化、清除自由基、抗动脉粥样硬化及抑制肿瘤生长等多方面的功能,对心血管系统疾病也有一定的作用.本文讨论了姜黄素的药理作用及临床应用.

  12. Curriculum Guidelines for Pharmacology.

    Shaw, David H.; And Others

    1990-01-01

    Pharmacology embraces the physical and chemical properties of drugs; the preparation of pharmaceutical agents; the absorption, fate, and excretion of drugs; and the effects of drugs on living systems. These guidelines represent a consensus on what would constitute a minimally acceptable pharmacology course for predoctoral dental students. (MLW)

  13. The effective action for composite Higgs particles

    There is reason to believe that massive composite (fermion-antifermion) scalar particles closely resembling the usual fundamental scalar Higgs fields exist in theories with dynamically broken gauge symmetries. This composite Higgs couples directly to the fermions in proportion to their symmetry-violating self-energies. Induced couplings to the gauge bosons and self-couplings are claculated as loop effects. This involves deriving the effective action in terms of the full propagators and background fields. The couplings between the composite Higgs and the gauge bosons are the same as those in models with fundamental scalars. The self-couplings are determined and fix all parameters associated with the composite scalars. Comments regarding extending work to higher orders and concerning the symmetry-violating solutions to the fermion Schwinger-Dyson equation are given in this paper

  14. The Universal One-Loop Effective Action

    Drozd, Aleksandra; Quevillon, Jérémie; You, Tevong

    2016-01-01

    We present the universal one-loop effective action for all operators of dimension up to six obtained by integrating out massive, non-degenerate multiplets. Our general expression may be applied to loops of heavy fermions or bosons, and has been checked against partial results available in the literature. The broad applicability of this approach simplifies one-loop matching from an ultraviolet model to a lower-energy effective field theory (EFT), a procedure which is now reduced to the evaluation of a combination of matrices in our universal expression, without any loop integrals to evaluate. We illustrate the relationship of our results to the Standard Model (SM) EFT, using as an example the supersymmetric stop and sbottom squark Lagrangian and extracting from our universal expression the Wilson coefficients of dimension-six operators composed of SM fields.

  15. The universal one-loop effective action

    Drozd, Aleksandra; Ellis, John; Quevillon, Jérémie; You, Tevong

    2016-03-01

    We present the universal one-loop effective action for all operators of dimension up to six obtained by integrating out massive, non-degenerate multiplets. Our general expression may be applied to loops of heavy fermions or bosons, and has been checked against partial results available in the literature. The broad applicability of this approach simplifies one-loop matching from an ultraviolet model to a lower-energy effective field theory (EFT), a procedure which is now reduced to the evaluation of a combination of matrices in our universal expression, without any loop integrals to evaluate. We illustrate the relationship of our results to the Standard Model (SM) EFT, using as an example the supersymmetric stop and sbottom squark Lagrangian and extracting from our universal expression the Wilson coefficients of dimension-six operators composed of SM fields.

  16. Action-based effects on music perception

    Maes, Pieter-Jan; Leman, Marc; Palmer, Caroline; Wanderley, Marcelo M.

    2014-01-01

    The classical, disembodied approach to music cognition conceptualizes action and perception as separate, peripheral processes. In contrast, embodied accounts of music cognition emphasize the central role of the close coupling of action and perception. It is a commonly established fact that perception spurs action tendencies. We present a theoretical framework that captures the ways in which the human motor system and its actions can reciprocally influence the perception of music. The cornerst...

  17. Action-based effects on music perception

    Pieter-Jan eMaes; Marc eLeman; Caroline ePalmer; Marcelo eWanderley

    2014-01-01

    The classical, disembodied approach to music cognition conceptualizes action and perception as separate, peripheral phenomena. In contrast, embodied accounts to music cognition emphasize the central role of the close coupling of action and perception. It is a commonly established fact that perception spurs action tendencies. We present a theoretical framework capturing the ways that the human motor system, and the actions it produces, can reciprocally influence the perception of music. The co...

  18. Pharmacological and clinical properties of curcumin

    Huang S

    2011-06-01

    Full Text Available Christopher S Beevers¹, Shile Huang²¹Department of Pharmacology, Ross University School of Medicine, Picard-Portsmouth, Commonwealth of Dominica; ²Department of Biochemistry and Molecular Biology, Louisiana State University Health Sciences Center, Shreveport, LA, USAAbstract: The polyphenol natural product curcumin has been the subject of numerous studies over the past decades, which have identified and characterized the compound's pharmacokinetic, pharmacodynamic, and clinical pharmacological properties. In in vitro and in vivo model systems, curcumin displays potent pharmacological effects, by targeting many critical cellular factors, through a diverse array of mechanisms of action. Despite this tremendous molecular versatility, however, the clinical application of curcumin remains limited due to poor pharmacokinetic characteristics in human beings. The current trend is to develop and utilize unique delivery systems, chemical derivatives, and chemical analogs to circumvent these pharmacological obstacles, in order to optimize the conditions for curcumin as a chemopreventive and chemotherapeutic agent in diseases such as cancer, diabetes, obesity, Alzheimer's disease, and inflammatory disorders. The present work seeks to review recent studies in the basic pharmacological principles and potential clinical applications of curcumin.Keywords: curcumin, pharmacological properties, signal transduction, cellular targets, cancer, inflammation

  19. Effective Action of Domain Wall Networks

    Eto, M; Nagashima, T; Nitta, M; Ohashi, K; Sakai, N; Eto, Minoru; Fujimori, Toshiaki; Nagashima, Takayuki; Nitta, Muneto; Ohashi, Keisuke; Sakai, Norisuke

    2007-01-01

    U(Nc) gauge theory with Nf fundamental scalars admits BPS junctions of domain walls. When the networks/webs of these walls contain loops, their size moduli give localized massless modes. We construct K\\"ahler potential of their effective action. In the large size limit K\\"ahler metric is well approximated by kinetic energy of walls and junctions, which is understood in terms of tropical geometry. K\\"ahler potential can be expressed in terms of hypergeometric functions which are useful to understand small size behavior. Even when the loop shrinks, the metric is regular with positive curvature. Moduli space of a single triangle loop has a geometry between a cone and a cigar.

  20. Boundary Effective Action for Quantum Hall States

    Gromov, Andrey; Jensen, Kristan; Abanov, Alexander G.

    2016-03-01

    We consider quantum Hall states on a space with boundary, focusing on the aspects of the edge physics which are completely determined by the symmetries of the problem. There are four distinct terms of Chern-Simons type that appear in the low-energy effective action of the state. Two of these protect gapless edge modes. They describe Hall conductance and, with some provisions, thermal Hall conductance. The remaining two, including the Wen-Zee term, which contributes to the Hall viscosity, do not protect gapless edge modes but are instead related to the local boundary response fixed by symmetries. We highlight some basic features of this response. It follows that the coefficient of the Wen-Zee term can change across an interface without closing a gap or breaking a symmetry.

  1. Pharmacological actions of Uncaria alkaloids,rhynchophylline and isorhynchophylline%钩藤总碱、钩藤碱和异钩藤碱的药理作用

    石京山; 余俊先; 陈修平; 徐瑞霞

    2003-01-01

    The pharmacological actions of Uncaria alkaloids, rhynchophylline and isorhynchophylline extracted from Uncaria rhynchophylla Miq Jacks were reviewed. The alkaloids mainly act on cardiovascular system and central nervous system including the hypotension, brachycardia, antiarrhythmia, and protection of cerebral ischemia and sedation.The active mechanisms were related to blocking of calcium channel, opening of potassium channel,and regulating of nerve transmitters transport and metabolism,etc.%综述了钩藤总碱、钩藤碱和异钩藤碱对心血管系统和神经系统等方面的药理作用,包括降低血压、减慢心率、抗心律失常、脑缺血保护,以及镇静等作用,其作用机制与钙通道阻滞、钾通道开放、以及神经递质转运和代谢的调节有关.

  2. Methamphetamine exposure during pregnancy at pharmacological doses produces neurodevelopmental and behavioural effects in rat offspring.

    McDonnell-Dowling, Kate; Donlon, Michelle; Kelly, John P

    2014-06-01

    In recent years methamphetamine (MA) use has become more prevalent, and of particular concern is its growing popularity of MA among women of childbearing age. However, to date, studies examining MA effects on the developing offspring in laboratory animals are limited. Thus, the aim of this study was to determine if in utero MA exposure in rats at pharmacological doses can have a negative impact on neonatal neurodevelopment and behaviour. Pregnant Sprague-Dawley dams (n=10 dams/group) received MA (0, 0.625, 1.25, 2.5mg/kg) once daily via oral gavage from gestational day 7 to 21. Maternal body weight, food and water consumption were recorded daily. A range of standard neurodevelopment parameters was examined in the offspring during the neonatal period. There were no neurodevelopmental deficits observed with offspring exposed to 0.625mg/kg MA, in fact, there were enhancements of neurodevelopment in some parameters at this low dose. However, exposure to the 1.25mg/kg MA dose resulted in significant impairments in surface righting reflex and forelimb grip in both sexes. Exposure to the 2.5mg/kg MA dose resulted in a significant reduction in ano-genital distance in males, and in both sexes resulted in delayed fur appearance and eye opening, impairments in surface righting reflex and negative geotaxis, and a reduction in body length. In conclusion, this study demonstrates that pharmacologically relevant doses of MA can have profound dose-related effects on neonatal outcome. If extrapolated to the clinical scenario this will give cause for concern regarding the risks associated with this drug of abuse at relatively low doses. PMID:24667147

  3. Perception of actions performed by external agents presupposes knowledge about the relationship between action and effect.

    Raos, Vassilis; Savaki, Helen E

    2016-05-15

    We used the (14)C-deoxyglucose method to reveal changes in activity, in the lateral sulcus of monkeys, elicited by reaching-to-grasp in the light or in the dark and by observation of the same action executed by an external agent. Both visually-guided execution and observation of the same action activated the secondary somatosensory cortex, the ventral somatosensory area, the somatorecipient parietal ventral area, the retroinsula and the caudo-medial area of the auditory belt. These matching activations indicate that the somesthetic consequences of movements, generated bottom-up during action execution, may also be triggered top-down during action observation to represent the predicted sensory consequences of the perceived movement. The posterior granular part of insula found to be activated only for action execution and its anterior agranular part activated only for action observation may contribute to the attribution of action to the correct agent. Also, execution in the dark implicated all components activated by execution in the light but the retroinsula. In conclusion, activation of the somatorecipient parietal areas, not only for action-execution but also for action-observation, indicates that perception of actions performed by an external agent presupposes knowledge about the action-effect relationships, and that understanding others' actions consists of running off-line previously stored sensory-motor programs. PMID:26892857

  4. Motor imagery during action observation modulates automatic imitation effects in rhythmical actions

    Daniel Lloyd Eaves

    2014-02-01

    Full Text Available We have previously shown that passively observing a task-irrelevant rhythmical action can bias the cycle time of a subsequently executed rhythmical action. Here we use the same paradigm to investigate the impact of different forms of motor imagery (MI during action observation (AO on this automatic imitation (AI effect. Participants saw a picture of the instructed action followed by a rhythmical distractor movie, wherein cycle time was subtly manipulated across trials. They then executed the instructed rhythmical action. When participants imagined performing the instructed action in synchrony with the distractor action (AO + MI, a strong imitation bias was found that was significantly greater than in our previous study. The bias was pronounced equally for compatible and incompatible trials, wherein observed and imagined actions were different in type (e.g., face washing vs. painting or plane of movement, or both. In contrast, no imitation bias was observed when MI conflicted with AO. In Experiment 2, motor execution synchronised with AO produced a stronger imitation bias compared to AO + MI, showing an advantage in synchronisation for overt execution over MI. Furthermore, the bias was stronger when participants synchronised the instructed action with the distractor movie, compared to when they synchronised the distractor action with the distractor movie. Although we still observed a significant bias in the latter condition, this finding indicates a degree of specificity in AI effects for the identity of the synchronised action. Overall, our data show that MI can substantially modulate the effects of AO on subsequent execution, wherein: (1 combined AO + MI can enhance AI effects relative to passive AO; (2 observed and imagined actions can be flexibly coordinated across different action types and planes; and (3 conflicting AO + MI can abolish AI effects. Therefore, combined AO + MI instructions should be considered in motor training and

  5. Pharmacological Actions of NGB 2904, a Selective Dopamine D3 Receptor Antagonist, in Animal Models of Drug Addiction

    Xi, Zheng-Xiong; Gardner, Eliot L

    2007-01-01

    As a continuation of our work with SB-277011A, we have examined the effects of another highly elective dopamine (DA) D3 receptor antagonist, N-(4-[4-{2,3-dichlorophenyl}-1-piperazinyl]butyl)-2-fluorenylcarboxamide (NGB 2904), in animal models of addiction. Our results indicate that by systemic administration, NGB 2904 inhibits intravenous cocaine self-administration maintained under a progressive-ratio (PR) reinforcement schedule, cocaine-or cocaine cue–induced reinstatement of cocaine-seekin...

  6. Modulation of the Pharmacological and Biochemical Actions of Leiurusquinquestriatus (L.q Scorpion Venom by Exposure to Gamma Radiation

    Heba A. Mohamed*, Esmat A. Shaaban* , Aber M Amin** and Sanaa A. Kenawy

    2011-07-01

    Full Text Available This study was undertaken to evaluate the effect of gamma radiation (1.5 KGy & 3 KGy on L.q scorpion venom. This was carried out by studying the toxicological, biochemical & immunological properties of the venom before and after exposure to gamma radiation. Material and methods Animals, venom, antivenin, gamma radiation, 125I. Results Data revealed that the toxicity of irradiated venom (1.5 KGy & 3 KGy decreased as compared to that of the native one. LD50 of irradiated venom were 3.5 mg/kg & 7.5 mg/kg respectively while, that of the native venom was (0.39 mg/kg. Moreover, the distribution of 125I-labeled L.q venom was studied in male Swiss mice tissue using chloramine-T method by being injected intravenously. At various time intervals, urine and blood were collected and the animals were sacrificed. Brain, lungs, heart, liver, kidneys, spleen, intestine, bone and muscle were isolated in order to determine the radioactivity content. The highest contents of 125I-labeled L.q venom were found in the liver and kidney that were quickly excreted into the urinary tract. Trial to label irradiated (1.5 & 3 KGy L.q venom was unsuccessful due to its decomposition. For that reason the utilization of the labeled irradiated L.q venom is of no meaning. In immunodiffusion technique, both irradiated and native venoms exhibited prominent precipitin bands indicating high concentration of specific antibodies against polyvalent antivenin with venom. Furthermore, the effect of half the LD50 of native or irradiated (1.5 KGy L.q venom was studied on the activities of certain enzymes: ASAT, ALAT, LDH, CPK, CPK-MB, and the levels of total cholesterol, triglyceride, HDL-cholesterol, LDL-cholesterol and the oxidative stress biomarkers (plasma MDA & blood GSH. Biochemical measurements showed that scorpion venom envenomation caused significant (p < 0.05 elevation in serum ASAT, ALAT, LDH, CPK as well as CPK-MB activities, blood GSH level while, caused significant (p < 0

  7. Modulation of the Pharmacological and Biochemical Actions of Leiurusquinquestriatus (L.q) Scorpion Venom by Exposure to Gamma Radiation

    Heba A. Mohamed*, Esmat A. Shaaban* , Aber M Amin** and Sanaa A. Kenawy

    2011-01-01

    This study was undertaken to evaluate the effect of gamma radiation (1.5 KGy & 3 KGy) on L.q scorpion venom. This was carried out by studying the toxicological, biochemical & immunological properties of the venom before and after exposure to gamma radiation. Material and methods Animals, venom, antivenin, gamma radiation, 125I. Results Data revealed that the toxicity of irradiated venom (1.5 KGy & 3 KGy) decreased as compared to that of the native one. LD50 of irradiated venom were 3.5 mg/kg ...

  8. Gaultheria: Phytochemical and pharmacological characteristics.

    Liu, Wei-Rui; Qiao, Wen-Lin; Liu, Zi-Zhen; Wang, Xiao-Hong; Jiang, Rui; Li, Shu-Yi; Shi, Ren-Bing; She, Gai-Mei

    2013-01-01

    The genus Gaultheria, comprised of approximately 134 species, is mostly used in ethnic drugs to cure rheumatism and relieve pain. Phytochemical investigations of the genus Gaultheria have revealed the presence of methyl salicylate derivatives, C₆-C₃ constituents, organic acids, terpenoids, steroids, and other compounds. Methyl salicylate glycoside is considered as a characteristic ingredient in this genus, whose anti-rheumatic effects may have a new mechanism of action. In this review, comprehensive information on the phytochemistry, volatile components and the pharmacology of the genus Gaultheria is provided to explore its potential and advance research. PMID:24084015

  9. Gaultheria: Phytochemical and Pharmacological Characteristics

    Ren-Bing Shi

    2013-09-01

    Full Text Available The genus Gaultheria, comprised of approximately 134 species, is mostly used in ethnic drugs to cure rheumatism and relieve pain. Phytochemical investigations of the genus Gaultheria have revealed the presence of methyl salicylate derivatives, C6-C3 constituents, organic acids, terpenoids, steroids, and other compounds. Methyl salicylate glycoside is considered as a characteristic ingredient in this genus, whose anti-rheumatic effects may have a new mechanism of action. In this review, comprehensive information on the phytochemistry, volatile components and the pharmacology of the genus Gaultheria is provided to explore its potential and advance research.

  10. Protective Effect of Flos Lonicerae against Experimental Gastric Ulcers in Rats: Mechanisms of Antioxidant and Anti-Inflammatory Action

    Kang, Jung-Woo; Yun, Nari; Han, Hae-Jung; Kim, Jeom-Yong; Kim, Joo-Young; Lee, Sun-Mee

    2014-01-01

    Flos Lonicerae is one of the oldest and most commonly prescribed herbs in Eastern traditional medicine to treat various inflammatory diseases. In the present study, we investigated the effects of ethyl acetate fraction of Flos Lonicerae (GC-7101) on experimental gastric ulcer models and its mechanisms of action in gastric ulcer healing. The pharmacological activity of GC-7101 was investigated in rats on HCl/EtOH, indomethacin, water immersion restraint stress induced acute gastric ulcer, and ...

  11. Combined pharmacological activation of AMPK and PPARδ potentiates the effects of exercise in trained mice.

    Manio, Mark Christian C; Inoue, Kazuo; Fujitani, Mina; Matsumura, Shigenobu; Fushiki, Tohru

    2016-03-01

    The combined activation of the cellular energy sensor AMP-activated protein kinase (AMPK) and the nuclear transcription factor peroxisome proliferator-activated receptor delta (PPARδ) has been demonstrated to improve endurance and muscle function by mimicking the effects of exercise training. However, their combined pharmacological activation with exercise training has not been explored. Balb/c mice were trained on a treadmill and administered both the AMPK activator AICAR and the PPARδ agonist GW0742 for 4 weeks. AICAR treatment potentiated endurance, but the combination of AICAR and GW0742 further potentiated endurance and increased all running parameters significantly relative to exercised and nonexercised groups (138-179% and 355% increase in running time, respectively). Despite the lack of change in basal whole-body metabolism, a significant shift to fat as the main energy source with a decline in carbohydrate utilization was observed upon indirect calorimetry analysis at the period near exhaustion. Increased energy substrates before exercise, and elevated muscle nonesterified fatty acids (NEFA) and elevated muscle glycogen at exhaustion were observed together with increased PDK4 mRNA expression. Citrate synthase activity was elevated in AICAR-treated groups, while PGC-1α protein level tended to be increased in GW0742-treated groups. At exhaustion, Pgc1a was robustly upregulated together with Pdk4, Cd36, and Lpl in the muscle. A robust upregulation of Pgc1a and a downregulation in Chrebp were observed in the liver. Our data show that combined pharmacological activation of AMPK and PPARδ potentiates endurance in trained mice by transcriptional changes in muscle and liver, increased available energy substrates, delayed hypoglycemia through glycogen sparing accompanied by increased NEFA availability, and improved substrate shift from carbohydrate to fat. PMID:26997622

  12. The role of action effects in 12-month-olds' action control: a comparison of televised model and live model.

    Klein, Annette M; Hauf, Petra; Aschersleben, Gisa

    2006-12-01

    The present study investigated differences in infant imitation after watching a televised model and a live model and addressed the issue of whether action effects influence infants' action control in both cases. In a 2x2 design, 12-month-old infants observed a live or a televised model performing a three-step action sequence, in which either the 2nd or the 3rd action step was combined with an acoustical action effect. We assumed that infants would use the observed action-effect relations for their own action control in the test phase afterwards. Even though results exhibited differences in the absolute amount of imitation between the two demonstration groups, both groups showed similar result patterns regarding the action effect manipulation: infants imitated the action step that was followed by a salient action effect more often and mostly as the first target action, emphasizing the important role of action effects in infants' action control. PMID:17138306

  13. Modification of certain pharmacological effects of ethanol by lipophilic alpha-1 adrenergic agonists

    Menon, M.K.; Dinovo, E.C.; Haddox, V.G.

    1987-09-28

    The influence of four centrally-acting alpha-1 adrenoceptor agonists, namely, 2(2-chloro-5-trifluoromethylphenylimino) imidazolidine (St 587), cirazoline, (-) 1,2,3,4-tetrahydro-8-methoxy-5-methylthio-2-naphthalenamine ((-)SKF 89748A) and 2-(2-methylindazol-4-imino)imidazolidine (Sgd 101/75) on the pharmacological effects of ethanol was investigated. All four drugs reduced the duration of ethanol-induced hypnosis in C57B1/6 mice, this effect being proportional to their relative potencies to exert central alpha-1 agonism. In prazosin-pretreated mice, St 587 failed to reduce the hypnotic effect of ethanol, which provided strong evidence for the role of alpha-1 agonism for the hypnosis reducing effect of St 587. Hyperactivity induced in C57B1/6 mice by a subhypnotic dose of ethanol and St 587 was reported earlier. In the present study, St 587, cirazoline and (-)SKF 89748A produced similar response, but no correlation between this effect and ethanol hypnosis blockade could be established. 19 references, 8 figures, 2 tables.

  14. 迷迭香活性提取物的药理作用研究进展%Research progress on pharmacological action of rosemary active extract

    周慧灵; 梁婉娴; 徐道立; 陈雨; 王莹; 赵丕文

    2015-01-01

    Rosemary is a widely used traditional Chinese herb, which has the effects of tranquillization, regulating stomach and so on. At present, researches in vivo and vitro show that rosemary active extract has many significant pharmacological effects such as anti-oxidation, inhibiting the proliferation of hepatoma carcinoma cells and mammary carcinoma cells, inhibiting the growth of escherichia coli, staphylococcus aureus and plant pathogenic fungi, anti-virus, anti-inflammation, inducing T cell activation, anti-angiogenesis and so on. Meanwhile, rosemary active extract can be used in the treatment of Parkinson' s disease, Alzheimer disease and vascular dementia. By referring to the literatures and information both at home and abroad, this article summarizes the pharmacological function and mechanism of rosemary active extract.%迷迭香是一种广泛使用的中草药,具有安神、健胃等功效. 目前,体内外的研究表明,迷迭香活性提取物具有抗氧化,抑制肝癌细胞、乳腺癌细胞增殖,抑制大肠杆菌、金黄色葡萄球菌、植物病原真菌生长等作用,还具有抗病毒、抗炎、诱导T细胞活化,抗血管形成等作用,对帕金森病、阿尔茨海默病、血管性痴呆也有一定的治疗作用. 文章通过查阅国内外资料,对迷迭香活性提取物的药理作用及其机制的研究进展进行综述.

  15. Chemical constituents and pharmacologic actions of Cynomorium plants%锁阳属植物的化学成分及药理作用

    蒙昊聪; 王硕; 李颖; 况园园; 马超美

    2013-01-01

    锁阳是锁阳科植物Cynomorium songaricum的根茎,是以具有强壮作用而著名的中药材.生长在北非及地中海地区的同属植物C coccineum被阿拉伯人看作是“宝药”.研究表明锁阳属植物的主要成分为酚类、甾体和三萜类化合物等.锁阳属植物的药理作用包括抗氧化、提高免疫力、抗糖尿病及神经保护等.锁阳的一些化学成分结构容易发生变化,因此不同生产条件得到的锁阳类药物成分会有所不同.该文综述锁阳属植物的药理作用及化学成分,检索的文献截至2011年底.%The stem of Cynomorium songaricum is a traditional Chinese medicine reputed to have tonic effects.C.coccineum growing in northern Africa and the Mediterranean region is regarded in Arabian medical practice as the "treasure of drugs".The major constituents of Cynomorium plants have been revealed to be phenolic compounds,steroids,triterpenes,etc.Pharmacologic studies showed that the Cynomorium plants had antioxidant,immunity-improving,anti-diabetic,neuroprotective,and other bioactivities.Some chemical constituents in Cynomorium plants are unstable,implying that the chemical components of the herbal medicines produced under different conditions may be variable.This review covers the literature published until December,2011 and describes the pharmacologic effects and secondary metabolites of Cynomorium species.

  16. The effective action in four-dimensional CDT

    Gizbert-Studnicki, Jakub

    2015-01-01

    We present recent results concerning the measurement and analysis of the effective action in four-dimensional Causal Dynamical Triangulations. The action describes quantum fluctuations of the spatial volume of the CDT universe (or alternatively the scale factor) after integrating out other degrees of freedom. We use the covariance of volume fluctuations to measure and parametrize the effective action inside the de Sitter phase, also called the C phase. We show that the action is consistent with a simple discretization of the minisuperspace action (with a reversed overall sign). We discuss possible subleading corrections and show how to construct a more complicated effective action comprising both integer and half-integer discrete proper time layers. We introduce a new method of the effective action measurement based on the transfer matrix. We show that the results of the new method are fully consistent with the covariance matrix method inside the de Sitter phase. We use the new method to measure the effective...

  17. [Pharmacology of bone resorption inhibitor].

    Menuki, Kunitaka; Sakai, Akinori

    2015-10-01

    Currently, bone resorption inhibitor is mainly used for osteoporosis. A number of these agents have been developed. These pharmacological action are various. Bisphosphonate inhibit functions of the osteoclasts by inducing apoptosis. On the one hand, RANK-ligand inhibitor and selective estrogen receptor modulator inhibit formation of osteoclasts. It is important to understand these pharmacological action for the selection of the appropriate medicine. PMID:26529923

  18. Genetic or pharmacological blockade of noradrenaline synthesis enhances the neurochemical, behavioural, and neurotoxic effects of methamphetamine

    Weinshenker, David; Ferrucci, Michela; Busceti, Carla L.; Biagioni, Francesca; Lazzeri, Gloria; Liles, L. Cameron; Lenzi, Paola; Murri, Luigi; Paparelli, Antonio; Fornai, Francesco

    2008-01-01

    N-(2-chloroethyl)-N-ethyl-2-bromobenzylamine (DSP-4) lesions of the locus coeruleus (LC), the major brain noradrenergic nucleus, exacerbate the damage to nigrostriatal dopamine (DA) terminals caused by the psychostimulant methamphetamine (METH). However, because noradrenergic terminals contain other neuromodulators and the noradrenaline (NA) transporter, which may act as a neuroprotective buffer, it was unclear whether this enhancement of METH neurotoxicity was caused by the loss of noradrenergic innervation or the loss of NA itself. We addressed the specific role of NA by comparing the effects of METH in mice with noradrenergic lesions (DSP-4) and those with intact noradrenergic terminals but specifically lacking NA (genetic or acute pharmacological blockade of the NA biosynthetic enzyme dopamine β-hydroxylase; DBH). We found that genetic deletion of DBH (DBH −/− mice) and acute treatment of wild-type mice with a DBH inhibitor (fusaric acid) recapitulated the effects of DSP-4 lesions on METH responses. All three methods of NA depletion enhanced striatal DA release, extracellular oxidative stress (as measured by in vivo microdialysis of DA and 2,3-dihydroxybenzoic acid), and behavioural stereotypies following repeated METH administration. These effects accompanied a worsening of the striatal DA neuron terminal damage and ultrastructural changes to medium spiny neurons. We conclude that NA itself is neuroprotective and plays a fundamental role in the sensitivity of striatal DA terminals to the neurochemical, behavioural, and neurotoxic effects of METH. PMID:18042179

  19. Effectiveness and student perspective of a pilot effort in team based learning in pharmacology for medical undergraduate

    Nayana K. Hashilkar

    2016-08-01

    Conclusions: Team-Based Learning is an effective teaching-learning method to teach pharmacology to medical undergraduates. It encourages pre-class preparation, student's participation in small teams and improves their basic knowledge as well as skills of critical thinking. [Int J Basic Clin Pharmacol 2016; 5(4.000: 1413-1416

  20. System biology analysis of long-term effect and mechanism of Bufei Yishen on COPD revealed by system pharmacology and 3-omics profiling

    Li, Jiansheng; Zhao, Peng; Yang, Liping; Li, Ya; Tian, Yange; Li, Suyun

    2016-01-01

    System pharmacology identified 195 potential targets of Bufei Yishen formula (BYF), and BYF was proven to have a short-term therapeutic effect on chronic obstructive pulmonary disease (COPD) rats previously. However, the long-term effect and mechanism of BYF on COPD is still unclear. Herein, we explored its long-term effect and underlying mechanism at system level. We administered BYF to COPD rats from week 9 to 20, and found that BYF could prevent COPD by inhibiting the inflammatory cytokines expression, protease-antiprotease imbalance and collagen deposition on week 32. Then, using transcriptomics, proteomics and metabolomics analysis, we identified significant regulated genes, proteins and metabolites in lung tissues of COPD and BYF-treated rats, which could be mainly attributed to oxidoreductase-antioxidant activity, focal adhesion, tight junction or lipid metabolism. Finally, based on the comprehensive analysis of system pharmacology target, transcript, protein and metabolite data sets, we found a number of genes, proteins, metabolites regulated in BYF-treated rats and the target proteins of BYF were involved in lipid metabolism, inflammatory response, oxidative stress and focal adhension. In conclusion, BYF exerts long-term therapeutic action on COPD probably through modulating the lipid metabolism, oxidative stress, cell junction and inflammatory response pathways at system level. PMID:27146975

  1. Pharmacology of kratom: an emerging botanical agent with stimulant, analgesic and opioid-like effects.

    Prozialeck, Walter C; Jivan, Jateen K; Andurkar, Shridhar V

    2012-12-01

    Kratom (Mitragyna speciosa) is a plant indigenous to Thailand and Southeast Asia. Kratom leaves produce complex stimulant and opioid-like analgesic effects. In Asia, kratom has been used to stave off fatigue and to manage pain, diarrhea, cough, and opioid withdrawal. Recently, kratom has become widely available in the United States and Europe by means of smoke shops and the Internet. Analyses of the medical literature and select Internet sites indicate that individuals in the United States are increasingly using kratom for the self-management of pain and opioid withdrawal. Kratom contains pharmacologically active constituents, most notably mitragynine and 7-hydroxymitragynine. Kratom is illegal in many countries. Although it is still legal in the United States, the US Drug Enforcement Administration has placed kratom on its "Drugs and Chemicals of Concern" list. Physicians should be aware of the availability, user habits, and health effects of kratom. Further research on the therapeutic uses, toxic effects, and abuse potential of kratom and its constituent compounds are needed. PMID:23212430

  2. STUDENTS’ ATTITUDE TOWARDS DIFFERENT EVALUATION METHODS IN PHARMACOLOGY

    Majagi Suneel Ishwar

    2012-08-01

    Full Text Available Literature review suggests the importance and the need of students’ feedback which may be used to effectively reform evaluation methods in medical sciences. The present study has been conducted to obtain student’s attitude (perception of towards different evaluation methods of pharmacology. The sample consisted of second phase M.B.B.S (n=108 students. Students answered 115 items/questions designed according to Likert’s five point (in agreement with items scale. These items/questions assessed student’s attitude (perception of towards different constituents of evaluation methods of pharmacology like sessional exams, traditional practical exams, objective structured practical exam (OSPE, MCQs, long essays, viva voce, pharmacy practical exercise, experimental pharmacology exercise etc in relation with various aspects of pharmacology subject like understanding, retention, learning clinical applications, mechanism of action of drugs, pharmacological actions, therapeutic uses, prescribing drugs etc. Results of the present study indicated the degree to which each evaluation method like sessional/preliminary theory exams, traditional practical exams and OSPE helps to elicit different constituents of pharmacology subject (ex: mechanism of action of drugs, therapeutic uses etc and the reason for the same is discussed. Similarly usefulness of different constituents of theory exams (MCQs, long essay etc and practical exams (spotters, pharmacy exercises etc towards eliciting the understanding pharmacology is revealed. Present study indicated the merits and demerits of different evaluation methods used in pharmacology. If any reformations/changes have to be incorporated in the evaluation methods, outcomes of this study will definitely help towards improving/modifying the evaluation methods of teaching and learning of pharmacology subject.

  3. Pharmacological Action of Adenophora Polysaccharides

    李泱; 李春红; 唐富天; 李新芳

    2004-01-01

    Adenophora polysaccharides (AP), is an active principle extracted from the root of Adenophorae Potaninii Korsh originated in Gansu Province and isolated with boiling water. AP is isolated and purified from the crude drug by DEAE-cellulose and Sephadex G-200 column, with a white powder and mean molecular weight of 8.3×104 , and [α]D20 of AP is + 68. AP is only composed of glucose judging from the analysis of it with patina chromatography (PC) and gas chromatography-mass spectrometer (GC-MS) methods.

  4. Wogonin potentiates the antitumor action of etoposide and ameliorates its adverse effects.

    Enomoto, Riyo; Koshiba, Chika; Suzuki, Chie; Lee, Eibai

    2011-05-01

    Wogonin, a flavone in the roots of Scutellaria baicalensis, reduced etoposide-induced apoptotic cell death in normal cells, such as bone marrow cells and thymocytes. On the other hand, wogonin potentiated the proapoptotic or cytotoxic action of etoposide in tumor cells, such as Jurkat, HL-60, A549, and NCI-H226. These contradictory actions of wogonin on apoptosis are distinguished by normal or cancer cell types. Wogonin had no effect on apoptosis induced by other anticancer agents in the tumor cells. Thus, the potentiation effect of wogonin was observed only in etoposide-induced apoptosis in tumor cells. In a functional assay for P-glycoprotein (P-gp), wogonin suppressed excretion of calcein, a substrate for P-gp, in these tumor cells. Moreover, wogonin decreased the excretion of radiolabeled etoposide and accordingly increased intracellular content of this agent in the cells. P-gp inhibitors showed a similar potentiation effect on etoposide-induced apoptosis in these tumor cells. Thus, wogonin is likely to potentiate the anticancer action of etoposide due to P-gp inhibition and accumulation of this agent. These findings suggest that wogonin may be a useful chemotherapeutic adjuvant to potentiate the pharmacological action of etoposide and ameliorate its adverse effects. PMID:20658136

  5. Tics and other stereotyped movements as side effects of pharmacological treatment.

    Madruga-Garrido, Marcos; Mir, Pablo

    2013-01-01

    Tics and other stereotyped abnormal movements can be seen as adverse effects of some pharmacologic drugs. Among these drugs, antipsychotics may provoke tardive syndromes after a chronic exposure, primarily in the case of typical antipsychotics. These syndromes include tardive tics, tardive dyskinesia, or tardive akathisia, which present with tics or stereotyped movements as a clinical phenomenon. Psychostimulants (mainly methylphenidate) have traditionally been associated with the appearance of tics due to the increased dopamine activity caused by stimulants. Nevertheless, in recent years, several studies have concluded not only that methylphenidate does not exacerbate or reactivate tics but also that tics can improve with its use in patients with associated attention deficit and hyperactivity disorder and tic disorder. Antiepileptic drugs, although infrequently, can also induce tics, with carbamazepine and lamotrigine described as tic inducers. Other antiepileptics, including levetiracetam and topiramate, have been proposed as a potential treatment for tic disorders due to a positive effect on tics, especially in those with associated epileptic disorder. Clinical and therapeutic approaches to tics and stereotyped movements after exposure to antipsychotics, stimulants, and antiepileptic drugs will be reviewed in this chapter. PMID:24295631

  6. Modulation of the pharmacological effects of enzymatically-active PLA2 by BTL-2, an isolectin isolated from the Bryothamnion triquetrum red alga

    Nagano Celso S

    2008-06-01

    Full Text Available Abstract Background An interaction between lectins from marine algae and PLA2 from rattlesnake was suggested some years ago. We, herein, studied the effects elicited by a small isolectin (BTL-2, isolated from Bryothamnion triquetrum, on the pharmacological and biological activities of a PLA2 isolated from rattlesnake venom (Crotalus durissus cascavella, to better understand the enzymatic and pharmacological mechanisms of the PLA2 and its complex. Results This PLA2 consisted of 122 amino acids (approximate molecular mass of 14 kDa, its pI was estimated to be 8.3, and its amino acid sequence shared a high degree of similarity with that of other neurotoxic and enzymatically-active PLA2s. BTL-2 had a molecular mass estimated in approximately 9 kDa and was characterized as a basic protein. In addition, BTL-2 did not exhibit any enzymatic activity. The PLA2 and BTL-2 formed a stable heterodimer with a molecular mass of approximately 24–26 kDa, estimated by molecular exclusion HPLC. In the presence of BTL-2, we observed a significant increase in PLA2 activity, 23% higher than that of PLA2 alone. BTL-2 demonstrated an inhibition of 98% in the growth of the Gram-positive bacterial strain, Clavibacter michiganensis michiganensis (Cmm, but only 9.8% inhibition of the Gram-negative bacterial strain, Xanthomonas axonopodis pv passiflorae (Xap. PLA2 decreased bacterial growth by 27.3% and 98.5% for Xap and Cmm, respectively, while incubating these two proteins with PLA2-BTL-2 inhibited their growths by 36.2% for Xap and 98.5% for Cmm. PLA2 significantly induced platelet aggregation in washed platelets, whereas BTL-2 did not induce significant platelet aggregation in any assay. However, BTL-2 significantly inhibited platelet aggregation induced by PLA2. In addition, PLA2 exhibited strong oedematogenic activity, which was decreased in the presence of BTL-2. BTL-2 alone did not induce oedema and did not decrease or abolish the oedema induced by the 48

  7. 热毒宁注射液的药理作用、临床应用及不良反应分析%Toxic heat ning injection pharmacological action, clinical application and adverse reactions

    黄克冬

    2015-01-01

    Objective To toxic heat ning injection pharmacological action, clinical application and adverse reactions to contrast analysis. Methods The 86 patients treated by toxic heat ning injection on research and analysis, to analyze its clinical effects, pharmacological effects and adverse reactions. Results This study selected patients, the clinical total effective rate was 98.48%in patients with acute upper respiratory tract infection, viral pneumonia in patients with clinical treatment the total effective rate was 92.86%, rotavirus viral enteritis patients clinical total effective rate was 83.33%; The incidence of adverse reactions was 4.65%, allergy 2 cases,blood in the urine 1 case,damage to the skin and attachment 1 case , but no serious adverse reactions such as anaphylactic shock and acute laryngeal edema. Conclusion Patients with toxic heat ning injection used in the treatment effect is signiifcant, and less adverse reaction, improve the prognosis of patients.%目的:对热毒宁注射液的药理作用、临床应用及不良反应展开分析。方法对通过热毒宁注射液治疗的患者86例进行研究分析,分析其疗效、药理作用和出现的不良反应。结果本次研究选取患者中,急性上呼吸道感染患者治疗总有效率为98.48%,病毒性肺炎患者治疗总有效率为92.86%,轮状病毒性肠炎患者治疗总有效率为83.33%;不良反应发生率为4.65%,过敏2例,血尿1例,皮肤和附件损害1例,但均没有出现过敏性休克和急性喉头水肿等严重不良反应。结论患者在采用热毒宁注射液治疗时疗效较为显著,且出现的不良反应较少,改善患者预后。

  8. Effectiveness of the psychological and pharmacological treatment of catastrophization in patients with fibromyalgia: a randomized controlled trial

    Magallón Rosa

    2009-04-01

    Full Text Available Abstract Background Fibromyalgia is a prevalent and disabling disorder characterized by widespread pain and other symptoms such as insomnia, fatigue or depression. Catastrophization is considered a key clinical symptom in fibromyalgia; however, there are no studies on the pharmacological or psychological treatment of catastrophizing. The general aim of this study is to assess the effectiveness of cognitive-behaviour therapy and recommended pharmacological treatment for fibromyalgia (pregabalin, with duloxetine added where there is a comorbid depression, compared with usual treatment at primary care level. Method/design Design: A multi-centre, randomized controlled trial involving three groups: the control group, consisting of usual treatment at primary care level, and two intervention groups, one consisting of cognitive-behaviour therapy, and the other consisting of the recommended pharmacological treatment for fibromyalgia. Setting: 29 primary care health centres in the city of Zaragoza, Spain. Sample: 180 patients, aged 18–65 years, able to understand and read Spanish, who fulfil criteria for primary fibromyalgia, with no previous psychological treatment, and no pharmacological treatment or their acceptance to discontinue it two weeks before the onset of the study. Intervention: Psychological treatment is based on the manualized protocol developed by Prof. Escobar et al, from the University of New Jersey, for the treatment of somatoform disorders, which has been adapted by our group for the treatment of fibromyalgia. It includes 10 weekly sessions of cognitive-behaviour therapy. Pharmacological therapy consists of the recommended pharmacological treatment for fibromyalgia: pregabalin (300–600 mg/day, with duloxetine (60–120 mg/day added where there is a comorbid depression. Measurements: The following socio-demographic data will be collected: sex, age, marital status, education, occupation and social class. The diagnosis of psychiatric

  9. Evolution in pharmacologic thinking around the natural analgesic palmitoylethanolamide: from nonspecific resistance to PPAR-α agonist and effective nutraceutical

    Keppel Hesselink JM

    2013-08-01

    Full Text Available Jan M Keppel Hesselink Department of Pharmacology, University of Witten/Herdecke, Witten, Germany Abstract: The history of development of new concepts in pharmacology is a highly interesting topic. This review discusses scientific insights related to palmitoylethanolamide (PEA and its progression over a period of six decades, especially in light of the work of the science sociologists, Ludwig Fleck and Thomas Kuhn. The discovery of the cannabis receptors and the nuclear peroxisome proliferator-activated receptors was the beginning of a completely new understanding of many important homeostatic physiologic mechanisms in the human body. These discoveries were necessary for us to understand the analgesic and anti-inflammatory activity of PEA, a body-own fatty amide. PEA is a nutrient known already for more than 50 years. PEA is synthesized and metabolized in animal cells via a number of enzymes and has a multitude of physiologic functions related to metabolic homeostasis. PEA was identified in the 1950s as a therapeutic principle with potent anti-inflammatory properties. Since 1975, its analgesic properties have been noted and explored in a variety of chronic pain states. Since 2008, PEA has been available as a nutraceutical under the brand names Normast® and PeaPure®. A literature search on PEA meanwhile has yielded over 350 papers, all referenced in PubMed, describing the physiologic properties of this endogenous modulator and its pharmacologic and therapeutic profile. This review describes the emergence of concepts related to the pharmacologic profile of PEA, with an emphasis on the search into its mechanism of action and the impact of failing to identify such mechanism in the period 1957–1993, on the acceptance of PEA as an anti-inflammatory and analgesic compound. Keywords: palmitoylethanolamide, sociology, science, paradigm, peroxisome proliferator-activated receptor-alpha, nutraceutical

  10. Effects of streptozotocin-induced diabetes on the pharmacology of rat conduit and resistance intrapulmonary arteries

    Howarth Frank C

    2009-01-01

    Full Text Available Abstract Background Poor control of blood glucose in diabetes is known to promote vascular dysfunction and hypertension. Diabetes was recently shown to be linked to an increased prevalence of pulmonary hypertension. The aim of this study was to determine how the pharmacological reactivity of intrapulmonary arteries is altered in a rat model of diabetes. Methods Diabetes was induced in rats by the β-cell toxin, streptozotocin (STZ, 60 mg/kg, and isolated conduit and resistance intrapulmonary arteries studied 3–4 months later. Isometric tension responses to the vasoconstrictors phenylephrine, serotonin and PGF2α, and the vasodilators carbachol and glyceryl trinitrate, were compared in STZ-treated rats and age-matched controls. Results STZ-induced diabetes significantly blunted the maximum response of conduit, but not resistance pulmonary arteries to phenylephrine and serotonin, without a change in pEC50. Agonist responses were differentially reduced, with serotonin (46% smaller affected more than phenylephrine (32% smaller and responses to PGF2α unaltered. Vasoconstriction caused by K+-induced depolarisation remained normal in diabetic rats. Endothelium-dependent dilation to carbachol and endothelium-independent dilation to glyceryl trinitrate were also unaffected. Conclusion The small resistance pulmonary arteries are relatively resistant to STZ-induced diabetes. The impaired constrictor responsiveness of conduit vessels was agonist dependent, suggesting possible loss of receptor expression or function. The observed effects cannot account for pulmonary hypertension in diabetes, rather the impaired reactivity to vasoconstrictors would counteract the development of pulmonary hypertensive disease.

  11. Pharmacological effects of methanolic extract of Swietenia mahagoni Jacq (meliaceae seeds

    Ghosh Sruti

    2009-01-01

    Full Text Available Seeds of medicinal plants are common ingredients of many folk and herbal medicines, and seed extracts have been reported to possess pharmacological activity including anti-inflammatory activity. In the present investigation, the methanolic extract of the dried ground seeds of Swietenia mahagoni (SMSE has been evaluated for anti-inflammatory, analgesic, and antipyretic activities. The anti-inflammatory activity was evaluated using acute, sub-chronic, and chronic models of inflammation in rodents. The antipyretic and analgesic activities were evaluated in mice models. Acute toxicity studies revealed that the extract up to a dose of 1.2 g/kg intraperitoneally was nontoxic. SMSE at doses of 50 and 100 mg/kg, i.p. was found to possess anti-inflammatory, analgesic, and antipyretic activities and the effect was comparable with that produced by the standard drug, ibuprofen. The results of the experiment on arachidonic acid-induced paw edema in rat revealed that the extract produces anti-inflammatory activity through dual inhibition of the cyclo-oxygenase and lipo-oxygenase pathways of arachidonic acid metabolism. SMSE also enhanced peritoneal cell exudates along with macrophage significantly. The triterpenoids present in SMSE may be responsible for these activities. SMSE possesses anti-inflammatory, analgesic, and antipyretic activities.

  12. Comparative study of native and irradiated crotoxin. Biochemical and pharmacological effects

    Ionizing radiation is able to detoxify several venoms, including snake venom, without affecting significantly their antigenic and immunogenic properties. In order to elucidate this phenomena, we conceived a comparative biochemical and pharmacological study between native and gamma irradiated (2000Gy) crotoxin, main toxin of south american rattlesnake Crotalus durissus terrificus. Crotoxin was isolated and purified from crude venom by molecular exclusion chromatography, pI precipitation and then irradiated. Immunodiffusion, electrophoresis and gel filtration showed that the molecular integrity was preserved after irradiation with some higher molecular weight aggregate formation and maintenance of its antigenic capacity. The antibodies induced by irradiated toxin had a similar titer to the antibodies induced by native crotoxin; however with higher protective effects in mice. Crotoxin toxicity became 15 times lower after irradiation, as determined by LD sub(50) in mice. Native and irradiated crotoxin biodistribution occurred with a similar general pattern, with renal elimination. In contrast to irradiated crotoxin, the native crotoxin is initially retained in kidneys. A later concentration (2-3hs) occurs in phagocyticmononuclear cells rich organs (liver and spleen) and neural junctions rich organs (muscle and brain). (author)

  13. Statistics in Pharmacology

    Spina, D.

    2007-01-01

    Statistics is an important tool in pharmacological research that is used to summarize (descriptive statistics) experimental data in terms of central tendency (mean or median) and variance (standard deviation, standard error of the mean, confidence interval or range) but more importantly it enables us to conduct hypothesis testing. This is of particular importance when attempting to determine whether the pharmacological effect of one drug is superior to another which clearly has implications f...

  14. Faddeev-Niemi Conjecture and Effective Action of QCD

    Cho, Y. M.; Lee, H. W.; Pak, D. G.

    2001-01-01

    We calculate a one loop effective action of SU(2) QCD in the presence of the monopole background, and find a possible connection between the resulting QCD effective action and a generalized Skyrme-Faddeev action of the non-linear sigma model. The result is obtained using the gauge-independent decomposotion of the gauge potential into the topological degrees which describes the non-Abelian monopoles and the local dynamical degrees of the potential, and integrating out all the dynamical degrees...

  15. Pharmacology of cannabinoids.

    Grotenhermen, Franjo

    2004-01-01

    Dronabinol (Delta 9-tetrahydocannabinol, THC), the main source of the pharmacological effects caused by the use of cannabis, is an agonist to both the CB1 and the CB2 subtype of cannabinoid receptors. It is available on prescription in several countries. The non-psychotropic cannabidiol (CBD), some analogues of natural cannabinoids and their metabolites, antagonists at the cannabinoid receptors and modulators of the endogenous cannabinoid system are also promising candidates for clinical research and therapeutic uses. Cannabinoid receptors are distributed in the central nervous system and many peripheral tissues including spleen, leukocytes; reproductive, urinary and gastrointestinal tracts; endocrine glands, arteries and heart. Five endogenous cannabinoids have been detected so far, of whom anandamide and 2-arachidonylglycerol are best characterized. There is evidence that besides the two cannabinoid receptor subtypes cloned so far additional cannabinoid receptor subtypes and vanilloid receptors are involved in the complex physiological functions of the cannabinoid system that include motor coordination, memory procession, control of appetite, pain modulation and neuroprotection. Strategies to modulate their activity include inhibition of re-uptake into cells and inhibition of their degradation to increase concentration and duration of action. Properties of cannabinoids that might be of therapeutic use include analgesia, muscle relaxation, immunosuppression, anti-inflammation, anti-allergic effects, sedation, improvement of mood, stimulation of appetite, anti-emesis, lowering of intraocular pressure, bronchodilation, neuroprotection and antineoplastic effects. PMID:15159677

  16. Effective action for supersymmetrical chiral anomaly

    It is proved that the consistency conditions of the type of Wess-Zumino conditions are necessary and sufficient for local integrability of supersymmetrical chiral anomaly. The global integrability condition implies discreteness of the coefficient in anomalous action. Explicit formulas for consistent anomalies and corresponding functional depending on superfields of various types are obtained

  17. A Review of the Receptor-Binding Properties of p-Synephrine as Related to Its Pharmacological Effects

    Sidney J. Stohs

    2011-01-01

    Full Text Available Bitter orange (Citrus aurantium extract and its primary protoalkaloid p-synephrine are used widely in weight loss/weight management and sports performance products. Because of structural similarities, the pharmacological effects of p-synephrine are widely assumed to be similar to those of ephedrine, m-synephrine (phenylephrine, and endogenous amine neurotransmitters as norepinephrine and epinephrine. However, small structural changes result in the receptor binding characteristics of these amines that are markedly different, providing a plausible explanation for the paucity of adverse effects associated with the wide-spread consumption of p-synephrine in the form of dietary supplements as well as in various Citrus foods and juices. This paper summarizes the adrenoreceptor binding characteristics of p-synephrine relative to m-synephrine, norepinephrine, and other amines as related to the observed pharmacological effects.

  18. Conformally covariant operators and effective action in external gravitational field

    The n-dimensional expressions for the second order conformally covariant differentional operators acting on vector and tensor fields and for the fourth order conformally covariant operator acting on scalar fields are obtained. For the fourth order operator one-loop effective action is evaluated in four dimensions. The possibility of effective action evaluation for other conformally covariant operators is discussed

  19. Pharmacological effects of Eugenia uniflora (Myrtaceae) aqueous crude extract on rat's heart.

    Consolini, Alicia E; Sarubbio, Marisol Gracía

    2002-06-01

    The effect of aqueous crude extract (ACE) of Eugenia uniflora L. (Myrtaceae) was studied on rat's perfused ventricles. This plant is used in South American traditional medicine as an antihypertensive and we already demonstrated previously its hypotensive properties. In this paper, maximal left intraventriclular pressure (P) of rat's hearts beating at 0.2 Hz firstly increased to 162.1+/-11.1% of basal value during 1-3 min of perfusing ACE 0.6%. Maximum rate of contraction (+P) also increased to duplicating +P/P ratio. Both types of effect were significantly decreased by either propranolol 0.35 microM, and pre-treatment with reserpine (5 mg/kg), suggesting that they were caused by a compound that releases cathecolamines with beta-adrenergic action. Nevertheless, after 20 min of perfusing ACE, ventricles decreased P to about 50% of their basal value, suggesting a negative-inotropic compound present in the extract. The perfusion of 1.2% ACE decreased P in a pressure-[Ca](o) curve (0.5-2 mM) in a non-competitive manner, suggesting that an irreversible Ca-blocking compound is also present in the extract. In summary, E. uniflora ACE has a dual effect on the heart related to its hypotensive action and is probably responsible for the therapeutic or adverse effects in patients under cardiac risk. PMID:12020928

  20. Effectiveness of team based learning to teach pharmacology for phase-II MBBS students

    N.K. Hashilkar

    2014-07-01

    Full Text Available Background: TBL (Team based Learning instructional methods foster applying knowledge in a highly interactive setting. Furthermore, in contrast to PBL (Problem Based Learning, it is a teacher directed method that encourages student- student interaction. Objective: The present study is aimed to assess the effectiveness of TBL over the current conventional tutorial type of teaching-learning strategy. Materials and Methods: The present study was conducted in the department of pharmacology of KLE University’s J N Medical College, Belgaum for phase II MBBS students. Students were randomly assigned to either team based learning (TBL or conventional tutorial (CT groups. Teaching learning sessions were conducted on similar topics of cardiovascular system following mechanics of TBL or tutorials respectfully. Effectiveness of each session was assessed by common pre-test and post test while, the overall performance was assessed at the end by a common test for both groups. The scores of the two groups were analysed using students t-test. A feedback was obtained from the students regarding their experience with TBL. Results: There was a significant difference between the pre-CT and pre-TBL scores for Anti-hypertensives (p ≤ 0.0001 and congestive cardiac failure (p ≤0.0002 sessions while these scores were not significantly different for Anti-anginals and Renin angiotensin system. However, the comparison of post-CT and post-TBL scores were significantly different (p< 0.05 for each of the four sessions. The scores of the end of the module test showed significant difference (p <0.0001 between the two group. Most of the students appreciated the mechanics of TBL and were satisfied with it. Conclusions: The performance of the students of the TBL group improved in individual sessions as well as the entire module as opposed to the CT group.

  1. Effects of ionizing radiation on the blood brain barrier permeability to pharmacologically active substances

    Trnovec, T.; Kallay, Z.; Bezek, S. (Institute of Experimental Pharmacology, Bratislava (Yugoslavia))

    1990-12-01

    Ionizing radiation can impair the integrity of the blood brain barrier (BBB). Data on early and late damage after brain irradiation are usually reported separately, yet a gradual transition between these two types has become evident. Signs appearing within 3 weeks after irradiation are considered to be early manifestations. The mechanism of radiation-effected integrity impairment of the BBB is discussed in relation to changes in morphological structures forming the BBB, the endothelium of intracerebral vessels, and in the surrounding astrocytes. Alterations in the function of the BBB are manifested in the endothelium by changes in the ultrastructural location of the activity of phosphatases and by the activation of pinocytotic vesicular transport, and in astrocyte cytoplasm by glycogen deposition. The changes in ultrastructure were critically surveyed with regard to increasing doses of radiation to the brain in the range of 5 Gy to 960 Gy. The qualitative as well as the semiquantitative and quantitative observations on the passage of substances across the damaged BBB were treated separately. Qualitative changes are based mainly on findings of extravasation of vital stains and of labelled proteins. The quantitative studies established differences in radiation-induced changes in the permeability of the BBB depending on the structure and physico-chemical properties of the barrier penetrating tracers. Indirect evaluation of radiation-induced BBB changes is based on studies of pharmacological effects of substances acting on the CNS. In conclusion, radiation impairs significantly the integrity of the BBB following single irradiation of the brain with a dose exceeding 10-15 Gy. The response of the BBB to ionizing radiation is dependent both on the dose to which the brain is exposed and on specific properties of the tracer. 68 references.

  2. Pharmacological strategies in lung cancer-induced cachexia: effects on muscle proteolysis, autophagy, structure, and weakness.

    Chacon-Cabrera, Alba; Fermoselle, Clara; Urtreger, Alejandro J; Mateu-Jimenez, Mercè; Diament, Miriam J; de Kier Joffé, Elisa D Bal; Sandri, Marco; Barreiro, Esther

    2014-11-01

    Cachexia is a relevant comorbid condition of chronic diseases including cancer. Inflammation, oxidative stress, autophagy, ubiquitin-proteasome system, nuclear factor (NF)-κB, and mitogen-activated protein kinases (MAPK) are involved in the pathophysiology of cancer cachexia. Currently available treatment is limited and data demonstrating effectiveness in in vivo models are lacking. Our objectives were to explore in respiratory and limb muscles of lung cancer (LC) cachectic mice whether proteasome, NF-κB, and MAPK inhibitors improve muscle mass and function loss through several molecular mechanisms. Body and muscle weights, limb muscle force, protein degradation and the ubiquitin-proteasome system, signaling pathways, oxidative stress and inflammation, autophagy, contractile and functional proteins, myostatin and myogenin, and muscle structure were evaluated in the diaphragm and gastrocnemius of LC (LP07 adenocarcinoma) bearing cachectic mice (BALB/c), with and without concomitant treatment with NF-κB (sulfasalazine), MAPK (U0126), and proteasome (bortezomib) inhibitors. Compared to control animals, in both respiratory and limb muscles of LC cachectic mice: muscle proteolysis, ubiquitinated proteins, autophagy, myostatin, protein oxidation, FoxO-1, NF-κB and MAPK signaling pathways, and muscle abnormalities were increased, while myosin, creatine kinase, myogenin, and slow- and fast-twitch muscle fiber size were decreased. Pharmacological inhibition of NF-κB and MAPK, but not the proteasome system, induced in cancer cachectic animals, a substantial restoration of muscle mass and force through a decrease in muscle protein oxidation and catabolism, myostatin, and autophagy, together with a greater content of myogenin, and contractile and functional proteins. Attenuation of MAPK and NF-κB signaling pathway effects on muscles is beneficial in cancer-induced cachexia. PMID:24615622

  3. Review on the Research of the Components, Pharmacological Actions and Toxicity of Polygonum Multiflorum Thunb(Heshouwu)%何首乌成分、药理及毒副作用相关的研究进展

    楼招欢; 吕圭源; 俞静静

    2014-01-01

    [Objective] To sum up researches on components, pharmacological actions and toxicity of Polygonum multiflorum Thunb(Heshouwu). [Method] The research reference about Heshouwu in CNKI, VIP and PUBMAD database is col ected and calssified to three aspects on components, pharmacological actions and toxicity.[Result]①On components:Heshouwu contains stilbene, lecithin, anthraquinone, flavonoids, tannin and trace elements. The stilbene and anthraquinone are the mainly active components. Producing area, growth years, harvest time and processing methods are factors affecting the content of the components such as TSG in Heshouwu; Macroporous adsorption resin is the main separation method for preconcentration of TSG and anthraquinone constituents; ② On pharmacological actions and toxicity: Heshouwu has effects of hypolipidemic and liver protection, antioxidative, anti-osteoporosi, hpyerglycemic, antidepressive and antibiosis, the hypolipidemic and liver protection are the main effects which have been studied more. A reversible liver injury which displays as abnormal liver function parameter and bile metabolic disorder would be induced if the Heshouwu is administrated with a large dosage for long term. The possible components which would induce the toxicity in Heshouwu are tannin and anthraquinone, and the anthraquinone is the component with double effects of toxicity and therapy which should be considered in clinical application. [Conclusion]Reducing lipid and protecting liver is the main pharmaceutical function of the herb. As a commonly used Chinese herb for liver protection, the studies on alcoholic hepatic injury protection of Heshouwu may be a point for the researchers to focus on. The comparison studies on hypolipidemic and liver protection between Hesouwu and its processing products, and the correlations between components and pharmacological actions are worth study further.%[目的]总结何首乌在成分、药理和毒副作用方面的研究情况。[方法]查

  4. Effect of metal complexation to anti-inflammatory over the action against oxidative and free radicals: ketoprofen action; Efeito da complexacao de metais aos antiinflamatorios na acao contra agentes oxidativos e radicais livres: acao do cetoprofeno

    Manente, Francine Alessandra; Mello, Lucas Rosolen de Almeida; Vellosa, Jose Carlos Rebuglio [UEPG, Universidade Estadual de Ponta Grossa, Departamento de Analises Clinicas eToxicologicas, Ponta Grossa, PR (Brazil); Khalil, Omar Arafat Kdudsi [IFG, Instituto Federal de Goias, Campus de Formosa, Formosa - GO (Brazil); Carvalho, Claudio Teodoro de [UFGD, Universidade Federal da Grande Dourados, Faculdade de Ciencias Exatas e Tecnologias, Dourados-MS (Brazil); Bannach, Gilbert [UNESP, Universidade Estadual Paulista Julio de Mesquita Filho, Faculdade de Ciencias de Bauru, Bauru, SP (Brazil)

    2011-07-01

    Free radicals are highly reactive species generated in living organisms for the purpose of protection. However, in some circumstances, they are responsible for the occurrence or aggravation of tissue damage. Many anti-inflammatory drugs have a direct effect on free radicals and not radical reactive species, which contributes to its actions against inflammation. Ketoprofen is a nonsteroidal anti-inflammatory agent that generates free radicals by photo irradiation and has an important hemolytic effect with that. The complexation of metals to different drugs has been used as a strategy to improve the pharmacological action of different molecules and reduce their side effects. This paper presents the results of ketoprofen and their metallic complexes action on erythrocytes and free radicals. It was observed that the cerium enhances the scavenger properties of ketoprofen on free radicals, while copper enhances its action over non-radical oxidants. Copper also reduced the hemolytic effect presented by ketoprofen meanwhile its cerium derivative maintained it. (author)

  5. Research Progress about Pharmacological Effect and Mechanism of Flavonoids in Traditional Chinese Medicine%中药黄酮类化合物药理作用及作用机制研究进展

    马锐; 吴胜本

    2013-01-01

    目的 对黄酮类化合物的药理作用及其作用机制进行综述和分析.方法 对近年来有关黄酮类化合物的药理作用及其作用机制的文献进行总结与分析.结果 黄酮类化合物具有抗氧化、抗炎、镇痛、调节免疫、抗衰老、降血脂、抗肿瘤等药理作用,其作用机制可能与其抗自由基或抗氧化有关.结论 黄酮类化合物是许多中草药的有效成分,具有广泛的生物活性,其产生生物活性的作用机制有待于进一步深入的研究.%Objective To review and analyze the pharmacological effect and mechanism of flavonoids in traditional Chinese medicine. Methods The related references in recent years home and abroad about the pharmacological effect and mechanism of flavonoids in traditional Chinese medicine were summarized and analyzed. Results Flavonoids had a wide range of pharmacological effects such as antioxidant, anti-inflammatory and analgesic, regulating immunity, anti-aging, fall hematic fat, antitumor and pharmacological action and so on, and the mechanism of pharmacological effects may be related with the resistance to free radicals or antioxidant. Conclusion The flavonoid compounds were the effective composition of many Chinese herbal medicine, and had a wide range of biological activity, and its biological activity mechanism needed further in-depth research.

  6. A systematic review on the effectiveness of pharmacological interventions for chronic non-specific low-back pain

    Kuijpers, T; van Middelkoop, M.; Rubinstein, S.M.; Ostelo, R.; Verhagen, A.; Koes, B W; van Tulder, M. W

    2010-01-01

    The objective of this review was to determine the effectiveness of pharmacological interventions [i.e., non-steroid anti-inflammatory drugs (NSAIDs), muscle relaxants, antidepressants, and opioids] for non-specific chronic low-back pain (LBP). Existing Cochrane reviews for the four interventions were screened for studies fulfilling the inclusion criteria. Then, the literature searches were updated. Only randomized controlled trials on adults (≥18 years) with chronic (≥12 weeks) non-specific L...

  7. Assessment of Acute and Chronic Pharmacological Effects on Energy Expenditure and Macronutrient Oxidation in Humans: Responses to Ephedrine

    Derek J. R. Nunez; Steve O'Rahilly; Peter R. Murgatroyd; Nick Finer; Hussey, Elizabeth K.; Robert Dobbins; Antonella Napolitano

    2010-01-01

    Evidence of active brown adipose tissue in human adults suggests that this may become a pharmacological target to induce negative energy balance. We have explored whole-body indirect calorimetry to detect the metabolic effects of thermogenic drugs through administration of ephedrine hydrochloride and have assessed ephedrine's merits as a comparator compound in the evaluation of novel thermogenic agents. Volunteers randomly given ephedrine hydrochloride 15 mg QID (n = 8) or placebo (n = 6) wer...

  8. Caenorhabditis elegans as Model System in Pharmacology and Toxicology: Effects of Flavonoids on Redox-Sensitive Signalling Pathways and Ageing

    Karoline Koch

    2014-01-01

    Full Text Available Flavonoids are secondary plant compounds that mediate diverse biological activities, for example, by scavenging free radicals and modulating intracellular signalling pathways. It has been shown in various studies that distinct flavonoid compounds enhance stress resistance and even prolong the life span of organisms. In the last years the model organism C. elegans has gained increasing importance in pharmacological and toxicological sciences due to the availability of various genetically modified nematode strains, the simplicity of modulating genes by RNAi, and the relatively short life span. Several studies have been performed demonstrating that secondary plant compounds influence ageing, stress resistance, and distinct signalling pathways in the nematode. Here we present an overview of the modulating effects of different flavonoids on oxidative stress, redox-sensitive signalling pathways, and life span in C. elegans introducing the usability of this model system for pharmacological and toxicological research.

  9. Thermodynamics of pharmacological action for electron-accepting compounds on activated or damaged cell in the context of Ling's model of the living cell

    Matveev, V V; Puzyrnikova, N V

    2011-01-01

    The theory describing action of medicines explored in this paper is based on assumption that vital activity of the cell may be described in terms of the model of two states: resting state and excitation. According to available physiological data excitation state is dangerous for cell and may cause different pathological changes, including "conformational" diseases, due to protein aggregation. Normally, the excitation is completely reversible and the key role is played here by ATP (adenosine-5'-triphosphate) which disaggregates proteins of cytomatrix. The same effect ATP exerts during cell injury by eliciting a "healing" effect. Damage of cell structures we consider as "illness", whereas removal of pathological consequences caused by protein aggregation of any origin we will call "a cure". The latter is considered as physical process of cell recovering from excitation/injury to resting state, which is analyzed in terms of our generalized thermodynamics. "Cure" results in reduction of effective temperature of c...

  10. 77 FR 42746 - Advisory Committee for Pharmaceutical Science and Clinical Pharmacology; Notice of Meeting

    2012-07-20

    ... Pharmacology; Notice of Meeting AGENCY: Food and Drug Administration, HHS. ACTION: Notice. This notice... Science and Clinical Pharmacology. General Function of the Committee: To provide advice...

  11. 78 FR 58314 - Advisory Committee for Pharmaceutical Science and Clinical Pharmacology; Notice of Meeting

    2013-09-23

    ... Pharmacology; Notice of Meeting AGENCY: Food and Drug Administration, HHS. ACTION: Notice. This notice... Science and Clinical Pharmacology. General Function of the Committee: To provide advice...

  12. 78 FR 42966 - Advisory Committee for Pharmaceutical Science and Clinical Pharmacology; Notice of Meeting

    2013-07-18

    ... Pharmacology; Notice of Meeting AGENCY: Food and Drug Administration, HHS. ACTION: Notice. This notice... Science and Clinical Pharmacology. General Function of the Committee: To provide advice...

  13. 76 FR 38188 - Advisory Committee for Pharmaceutical Science and Clinical Pharmacology; Notice of Meeting

    2011-06-29

    ... Pharmacology; Notice of Meeting AGENCY: Food and Drug Administration, HHS. ACTION: Notice. This notice... Science and Clinical Pharmacology. General Function of the Committee: To provide advice...

  14. 77 FR 41790 - Advisory Committee for Pharmaceutical Science and Clinical Pharmacology; Notice of Meeting

    2012-07-16

    ... Pharmacology; Notice of Meeting AGENCY: Food and Drug Administration, HHS. ACTION: Notice. This notice... Science and Clinical Pharmacology. General Function of the Committee: To provide advice...

  15. 78 FR 58315 - Advisory Committee for Pharmaceutical Science and Clinical Pharmacology; Notice of Meeting

    2013-09-23

    ... Pharmacology; Notice of Meeting AGENCY: Food and Drug Administration, HHS. ACTION: Notice. This notice... Science and Clinical Pharmacology. General Function of the Committee: To provide advice...

  16. 75 FR 10488 - Advisory Committee for Pharmaceutical Science and Clinical Pharmacology; Notice of Meeting

    2010-03-08

    ... Pharmacology; Notice of Meeting AGENCY: Food and Drug Administration, HHS. ACTION: Notice. This notice... Science and Clinical Pharmacology. General Function of the Committee: To provide advice...

  17. 75 FR 11551 - Advisory Committee for Pharmaceutical Science and Clinical Pharmacology; Notice of Meeting

    2010-03-11

    ... Pharmacology; Notice of Meeting AGENCY: Food and Drug Administration, HHS. ACTION: Notice. This notice... Science and Clinical Pharmacology. General Function of the Committee: To provide advice...

  18. On the influence of reward on action-effect binding

    PaulSimonMuhle-Karbe

    2012-11-01

    Full Text Available Ideomotor theory states that the formation of anticipatory representations about the perceptual consequences of an action (i.e. action-effect (A-E binding provides the functional basis of voluntary action control. A host of studies has demonstrated that A-E binding occurs fast and effortlessly, yet only little is known about cognitive and affective factors that influence this learning process. In the present study, we sought to test whether the motivational value of an action modulates the acquisition of A-E associations. To this end, we associated specific actions with monetary incentives during the acquisition of novel A-E mappings. In a subsequent test phase, the degree of binding was assessed by presenting the former effect stimuli as task-irrelevant response primes in a forced-choice response task in the absence of any reward. Binding, as indexed by response priming through the former action effects, was only found for reward-related A-E mappings. Moreover, the degree to which reward associations modulated the binding strength was predicted by individuals’ trait sensitivity to reward. These observations indicate that the association of actions and their immediate outcomes depends on the motivational value of the action during learning, as well as on the motivational disposition of the individual. On a larger scale, these findings also highlight the link between ideomotor theories and reinforcement-learning theories, providing an interesting perspective for future research on anticipatory regulation of behavior.

  19. 明党参活性成分及药理作用研究进展%Overview of studies on active constituents and pharmacological actions of Changium smy rnioides

    季晓; 宣槐斌; 黄宝康

    2015-01-01

    Changium smyrnioides (C . smyrnioides) Wolff is one species of monotypic genus in the A piaceae family w hich is a Chinese endemic species medicinal plant .It has the effect of nourishing the body ,improving health ,moiste‐ning the lung ,eliminating sputum and suppressing cough ,regulating stomach and relieving vomiting ,neutralizing toxins and subsiding swelling .C .smyrnioides as one kind of medicinal food and tonic agents ,is one of the important export medicinal ma‐terials .The tonic effect may be related with immuno‐regulatory ,anti‐fatigue and anti‐stress activities ,and polysaccharides are the main active constituents .The progress of the active constituents and pharmacological actions of C .smyrnioides are re‐viewed to provide basis for future rational development and utilization .%明党参是中国特有单种属植物,有滋补强壮、润肺化痰、养阴和胃及平肝解毒之功效,常作药膳及滋补强壮剂用,是我国外贸出口药材的重要品种之一。明党参的滋补强壮作用与其增强机体免疫功能、缓解疲劳和提高机体适应能力有关,多糖是其主要的活性成分。对近年来明党参活性成分及药理作用方面的研究进行综述,为合理开发和综合利用明党参提供依据。

  20. Study of gamma radiation from 60Co effects on Apis mellifera venom: biochemical, pharmacological and immunological aspects

    Africanized honeybees are very common insects in Brazil and frequently cause accidents followed by important immunological reactions and even deaths. Their venoms are composed of a complex mixture of substances of general biological actions. Ionizing radiation is able to modify molecular structures affecting the biological properties of proteins. It decreases toxic and enzymatic activities and so, it appears promising as a venom detoxification tool. The main objective of this work was to study the effects of gamma radiation on bee venom, regarding biochemical, pharmacological and immunological aspects. Africanized Apis mellifera whole venom (2 mg/ml) in 0.15 M NaCl solution was irradiated with 2 kGy in a 60Co source. Native and irradiated bee venoms were submitted to high performance size exclusion chromatography (Tosohaas G2000SW column), high performance reversed phase chromatography in a C-18 column under water/acetonitrile gradient, SDS-PAGE. For both venoms studies have been carried out in UV absorption spectrum, protein concentration, hemolytic activity, and PLA2 activity analysis, lethality assay (LD50). Biodistribution studies was carried out after labelling native and irradiated bee venom with 99mTc. The results showed that gamma radiation did not change the protein concentration nor its immunogenicity, although it could be observed that irradiated bee venom UV spectrum and SDS-PAGE profile presented differences when compared to native bee venom. This suggests that some structural alterations in bee venom components could have occurred after irradiation. HPLC-RP profiles showed that gamma radiation could have caused conformational changes, such as unfolding of molecule chains, changing their hydrophobic groups exposuring. The hemolytic and the PLA2 activities of irradiated bee venom were smaller than the native ones. The gamma radiation diminished the toxicity of bee venom, but did not abolish its bioactivity, like hemolysis. Biodistribution studies showed

  1. Effects of some pharmacological agents on the survival of unipedicled venous flaps: an experimental study.

    Askar, I; Saray, A; Gurlek, A; Sevin, K; Sabuncuoglu, B T

    2001-01-01

    Clinical and experimental studies have been conducted to improve the survival of venous flaps. As a result of these studies, although various survival mechanisms were raised, none obtained satisfactory information. Venous stasis, and the resultant venous thrombosis, is a factor that decreases the survival of venous flaps. In this study, we evaluated the effects of two antiinflammatory agents, etodolac and etofenamate, on the survival of unipedicled venous flaps. In this study, 35 male New Zealand white rabbits (3,500-4,000 g) (70 ears) were used. Perichondrocutaneous flaps, 3 x 4.5 cm in size, were designed and raised, keeping the central veins intact in the middle of venous flap. Central arteries and nerves were ligated and transected both proximally and distally, to prepare unipedicled venous flaps. A silicone sheet was placed between the cartilage tissue and flap, to prevent blood flow and revascularization beneath. The subjects were divided into seven groups, consisting of five rabbits (10 ears). In the negative control group (group I), the single vascular pedicle of venous flaps, central veins were ligated and flaps sutured into their own place as the composite graft. In the positive control group (group II), after venous flaps were prepared, normal saline, 0.2 mL, was given subcutaneously. In the first of five experimental groups (group III), unfractionated heparin (100 U/day) was given subcutaneously. In the second experimental group (group IV), etodolac (5 mg/kg/day) was given subcutaneously. In the third experimental group (group V), etophenamate (5 mg/kg/day) was given orally through a feeding tube. In the fourth experimental group (group VI), parnaparin (5 anti-Xa U/kg/day) was given subcutaneously. In the fifth experimental group (group VII), nadroparin (5 anti-Xa U/kg/day) was given subcutaneously, about 7 days postoperatively. At the eighth postoperative day, surviving areas of venous flaps were measured, and the results were evaluated by Kruskal

  2. Effective average action for gauge theories and exact evolution equations

    We propose a new nonperturbative evolution equation for Yang-Mills theories. It describes the scale dependence of an effective action. The running of the nonabelian gauge coupling in arbitrary dimension is computed. (orig.)

  3. World-volume Effective Actions of Exotic Five-branes

    Kimura, Tetsuji; Yata, Masaya

    2014-01-01

    We construct world-volume effective actions of exotic $5^2_2$-branes in type IIA and IIB string theories. The effective actions are given in fully space-time covariant forms with two Killing vectors associated with background isometries. The effective theories are governed by the six-dimensional $\\mathcal{N}=(2,0)$ tensor multiplet and $\\mathcal{N}=(1,1)$ vector multiplet, respectively. Performing the S-duality transformation to the $5^2_2$-brane effective action in type IIB string theory, we also work out the world-volume action of the $5^2_3$-brane. We discuss some additional issues relevant to the exotic five-branes in type I and heterotic string theories.

  4. Morphology, pharmacological activity, pharmaceutical preparation, doses and side effect of Coccinia indica (Wight & Arn.): An overview

    Mayank Kumar; Shashi Alok; Sanjay Kumar Jain; Amita Verma; Alok Mahor; Monika Sabharwal

    2013-01-01

    Traditional system of medicine consists of large number of plants with various medicinal and pharmacological importances and hence represents a priceless tank of new bioactive molecules. Coccinia indica belongs to the family Cucurbitaceae. It is a rapidly growing, perennial climber or trailing vine. Traditionally different parts of this plant namely the roots, leaves and fruits are used in folklore medicine for several purposes like jaundice, diabetes, wound healing, ulcers, stoma...

  5. Impact of Benign Prostatic Hyperplasia Pharmacological Treatment on Transrectal Prostate Biopsy Adverse Effects

    Marina Zamuner; Ciro Eduardo Falcone; Arnaldo Amstalden Neto; Tomás Bernardo Costa Moretti; Luis Alberto Magna; Fernandes Denardi; Leonardo Oliveira Reis

    2014-01-01

    Background. Benign prostatic hyperplasia (BPH) pharmacological treatment may promote a decrease in prostate vascularization and bladder neck relaxation with theoretical improvement in prostate biopsy morbidity, though never explored in the literature. Methods. Among 242 consecutive unselected patients who underwent prostate biopsy, after excluding those with history of prostate biopsy/surgery or using medications not for BPH, we studied 190 patients. On the 15th day after procedure patients w...

  6. New Development on Pharmacological Effects ofPunica Granatum L.%石榴药理研究新进展

    刘宇; 蔡霞; 曾勇; 王平; 孟宪丽; 张艺

    2015-01-01

    本文主要对近年来国内外石榴的药理研究进展进行综述.石榴药用历史悠久,不同部位在中医药与民族医药中应用广泛,其化学成分以鞣质类、黄酮类、生物碱和有机酸化合物为主,具有明显的药理活性.近年来,有关石榴的抗菌抗病毒、降血糖、抗肿瘤、调血脂及抗氧化、免疫调节等药理研究进展迅速.通过整理归纳并科学的分析石榴的功效及其新的药理学研究成果,以期能对石榴的研究、临床应用及相关产品的开发利用提供依据.%This article reviewed pharmacological study development of Punica granatum L. both at home and abroad in recent years. P. granatum has a long medical usage history. Different parts of P. granatum have wide applications in both traditional Chinese medicine (TCM) and other ethnic medicine. Its main chemical compositions were tannins, flavonoids, alkaloids and organic acids. It has obvious pharmacological activities. In recent years, the pharmacological research progress on P. granatum in terms of antibacterial, antiviral, hypoglycemic, antitumor, adjusting blood lipids, antioxidant, and immunoregulation has rapid development. The scientific collection and analysis on effects and new pharmacological research results of P. granatum are hoped to provide references for the study, clinical application, development and utilization of P. granatum and its products.

  7. Pharmacologically effective red yeast rice preparations marketed as dietary supplements illustrated by a case report.

    Venhuis, B J; van Hunsel, F; van de Koppel, S; Keizers, P H J; Jeurissen, S M F; De Kaste, D

    2016-03-01

    This paper reports a typical statin-related adverse reaction from a red yeast rice (RYR) supplement and the analytical findings from the supplement. It also examines the regulatory framework governing botanical supplements in Europe. Two key events that shaped the current regulatory framework are reviewed. First, the Hecht-Pharma judgement by the European Court of Justice (ECJ) that inverted the precautionary principle in the Medicines Act to a reactionary principle. Following the Hecht-Pharma judgement, pharmacological active dietary supplements can be sold until sufficient signals of harm show that they are an unregistered medicine, placing a huge burden on regulatory authorities. Secondly, the European Food Safety Authority (EFSA) in 2011 approved the first health claim for pharmacologically active RYR dietary supplements. If the current regulatory status for pharmacologically active RYR dietary supplements does not permit adequate warning and active monitoring of adverse drug reactions, then the current regulatory framework may not be adequate to ensure consumer safety.Copyright © 2016 John Wiley & Sons, Ltd. PMID:26810781

  8. Holographic RG flow and the quantum effective action

    The calculation of the full (renormalized) holographic action is undertaken in general Einstein-scalar theories. The appropriate formalism is developed and the renormalized effective action is calculated up to two derivatives in the metric and scalar operators. The holographic RG equations involve a generalized Ricci flow for the space-time metric as well as the standard β-function flow for scalar operators. Several examples are analyzed and the effective action is calculated. A set of conserved quantities of the holographic flow is found, whose interpretation is not yet understood. (Copyright copyright 2014 WILEY-VCH Verlag GmbH and Co. KGaA, Weinheim)

  9. Arsenic: health effects, mechanisms of actions, and research issues.

    Abernathy, C O; Liu, Y. P.; Longfellow, D; Aposhian, H V; Beck, B.; Fowler, B.; Goyer, R; Menzer, R.; Rossman, T; Thompson, C.; Waalkes, M

    1999-01-01

    A meeting on the health effects of arsenic (As), its modes of action, and areas in need of future research was held in Hunt Valley, Maryland, on 22-24 September 1997. Exposure to As in drinking water has been associated with the development of skin and internal cancers and noncarcinogenic effects such as diabetes, peripheral neuropathy, and cardiovascular diseases. There is little data on specific mechanism(s) of action for As, but a great deal of information on possible modes of action. Alth...

  10. Non-dissipative hydrodynamics : effective actions versus entropy current.

    Bhattacharya, Jyotirmoy; Bhattacharyya, Sayantani; Rangamani, Mukund

    2013-01-01

    While conventional hydrodynamics incorporating dissipative effects is hard to derive from an action principle, it is nevertheless possible to construct classical actions when the dissipative terms are switched off. In this note we undertake a systematic exploration of such constructions from an effective field theory approach and argue for the existence of non-trivial second order non-dissipative hydrodynamics involving pure energy-momentum transport. We find these fluids to be characterized ...

  11. Assessment of the pharmacological effects of alprazolam on electroencephalography using connectivity indexes not affected by volume conduction

    Joan Francesc Alonso

    2015-04-01

    The fact that the considered indexes were not able to find significant differences in the beta band might indicate that phase-coupling changes induced by the drug are weak or too subtle to be detected, given that all measures are corrected by a baseline recording. This might discourage their use in psychopharmacological studies when assessing low doses, mild effects, or when working with a reduced number of participants. However, correlations with plasma concentrations remained high, indicating that PLI, WPLI and IC should not be totally discarded as means of evaluating pharmacological effects on the brain via EEG recordings.

  12. Quantum effective action from the AdS/CFT correspondence

    Skenderis, K; Skenderis, Kostas; Solodukhin, Sergey N.

    2000-01-01

    We obtain an Einstein metric of constant negative curvature given an arbitrary boundary metric in three dimensions, and a conformally flat one given an arbitrary conformally flat boundary metric in other dimensions. In order to compute the on-shell value of the gravitational action for these solutions, we propose to integrate the radial coordinate from the boundary till a critical value where the bulk volume element vanishes. The result, which is a functional of the boundary metric, provides a sector of the quantum effective action common to all conformal field theories that have a gravitational description. We verify that the so-defined boundary effective action is conformally invariant in odd (boundary) dimensions and has the correct conformal anomaly in even (boundary) dimensions. In three dimensions and for arbitrary static boundary metric the bulk metric takes a rather simple form. We explicitly carry out the computation of the corresponding effective action and find that it equals the non-local Polyakov...

  13. Pharmacological Effects of Erythropoietin and its Derivative Carbamyl erythropoietin in Cerebral White Matter Injury

    Liu, Wei

    with translational potential for PVL, which is the primary injury underlying cerebral palsy. After confirming the neuroprotective effects of EPO and CEPO on PVL mice, we continued to study the mechanisms relating to their functions. As we learned from our lab's previous study, microglia play an important role in the pathogenesis of PVL, linking multiple effectors downstream of hypoxia-ischemia and inflammation. We found that EPO and CEPO inhibit microglial activation and reduced the severity of injury. Furthermore, we found that EPO and CEPO decreased the activity of poly (ADP-ribose) polymerase-1 (PARP-1) in activated microglia. PARP-1 activity increases in response to many insults, such as infection, ischemia and toxicity. Therefore, we hypothesized that EPO and CEPO decrease microglial activation by inhibiting PARP-1 activity, and thus leading to protection against inflammation and cell death. Besides pharmacological studies of EPO and CEPO on PVL, we also investigated other endogenous factors that may affect neonatal white matter injury. Heat shock proteins (HSPs) are important chaperones that facilitate appropriate protein folding and modification. HSP60, a chaperonin located in the mitochondria, is one of these important molecules that promote appropriate protein folding. HSP60 expression levels increased significantly in the brains of PVL mice compared with control animals. In microglial cell culture, we found that after LPS treatment, HSP60 expression levels increased both inside microglial cells and in the extracellular medium. In addition, we noted enhanced HSP60 immunoreactivity in the brains of PVL mice, which localized inside activated microglial cells and extracellularly. The rise in HSP60 activity after hypoxia-ischemia and LPS administration implies that it potentially functions as one of the triggers of microglial activation and central nervous system inflammation.

  14. The Effects of Pharmacological Inhibition of Histone Deacetylase 3 (HDAC3 in Huntington's Disease Mice.

    Haiqun Jia

    Full Text Available An important epigenetic modification in Huntington's disease (HD research is histone acetylation, which is regulated by histone acetyltransferase and histone deacetylase (HDAC enzymes. HDAC inhibitors have proven effective in HD model systems, and recent work is now focused on functional dissection of the individual HDAC enzymes in these effects. Histone deacetylase 3 (HDAC3, a member of the class I subfamily of HDACs, has previously been implicated in neuronal toxicity and huntingtin-induced cell death. Hence, we tested the effects of RGFP966 ((E-N-(2-amino-4-fluorophenyl-3-(1-cinnamyl-1H-pyrazol-4-ylacrylamide, a benzamide-type HDAC inhibitor that selectively targets HDAC3, in the N171-82Q transgenic mouse model of HD. We found that RGFP966 at doses of 10 and 25 mg/kg improves motor deficits on rotarod and in open field exploration, accompanied by neuroprotective effects on striatal volume. In light of previous studies implicating HDAC3 in immune function, we measured gene expression changes for 84 immune-related genes elicited by RGFP966 using quantitative PCR arrays. RGFP966 treatment did not cause widespread changes in cytokine/chemokine gene expression patterns, but did significantly alter the striatal expression of macrophage migration inhibitory factor (Mif, a hormone immune modulator associated with glial cell activation, in N171-82Q transgenic mice, but not WT mice. Accordingly, RGFP966-treated mice showed decreased glial fibrillary acidic protein (GFAP immunoreactivity, a marker of astrocyte activation, in the striatum of N171-82Q transgenic mice compared to vehicle-treated mice. These findings suggest that the beneficial actions of HDAC3 inhibition could be related, in part, with lowered Mif levels and its associated downstream effects.

  15. Urban Heat Island Effect Actions - Neighborhood Data

    Louisville Metro Government — The urban heat island effect — defined as the difference in temperature between the core of Louisville and its suburbs — contributes to heat-related illnesses and...

  16. Effect of mutagen combined action on Chlamydomonas reinhardtii cells. II

    The effect of UV radiation and UV radiation combined with alkylnitrosourea derivatives (N-methyl-N-nitrosourea and N-ethyl-N-nitrosourea) was observed on survival of cells of the algae Chlamydomonas reinhardtii. In particular, single parts were evaluated of the overall lethal effect - dying of cells before division and dying of cells after division. It was found that the combined action of low doses of UV radiation and alkylnitrosoureas result in a pronounced protective effect which manifests itself by a higher frequency of surviving cells than was that effected by the action of alkylnitrosoureas alone. As a result of combined action with higher doses of UV radiation this effect is lost, and the resultant values will come close to the theoretically anticipated values. This gradual transition from a protective to an additive effect mainly manifests itself by changes in the proportion of cells dying before division. (author)

  17. 牛蒡的药理作用研究进展%Advances in Pharmacological Effects of Arctium Lappa L.

    曹旭; 曹剑锋; 陈靠山

    2012-01-01

    OBJECTIVE To introduce advances in the pharmacological effects of Arctium lappa L., and to provide scientific basis for the further utilization. METHODS Consulted domestic and foreign literatures in recent 20 years and provided an overview of the pharmacological effects of burdock. RESULTS The advances in pharmacological effects such as antitumor, anti-inflammatory, immune modulation, antimicrobial, antiviral, antidiabetic, antioxidant, hepatoprotective effect, anti-fatigue, lipid-lowering and treatment erectile dysfunction of Arctium lappa L. Were given. It was universally studied that Arctium lappa L. Possess effects of immune regulation, anti-cancer and treatment diabetes with the potential development value. The research on the efficacy of burdock to treat erectile dysfunction in our laboratory provided a new direction for burdock development and utilization. CONCLUSION It's found that the pharmacological effects of burdock have great development value, especially in the treatment of chronic diseases.%目的 介绍牛蒡的药理作用研究进展,为进一步利用牛蒡提供依据.方法 通过查阅近20年的国内外文献,对牛蒡的药理作用进行概述.结果 牛蒡具有抗肿瘤、抗炎及免疫调节、抗菌、抗病毒、抗糖尿病、抗氧化、肝保护作用、抗疲劳、降血脂、治疗勃起功能障碍及其他多种药理作用,其中对牛蒡的免疫调节、抗癌作用及其治疗糖尿病的作用研究较多,具有潜在的开发应用价值.笔者所在实验室关于牛蒡治疗勃起功能障碍作用的研究为牛蒡开发利用提供了新的方向.结论 牛蒡具有较大的开发利用价值,特别是在治疗慢性疾病方面.

  18. Radiosensitizers action on Iodine 131 therapeutical effect

    Present studies were aimed to research the possible application of a radiosensitizer, nicotinamide, to increase the therapeutical effect of radioiodine. There were used goitrous and normal rats with growing dose of Iodine 131, with and without simultaneous treatment with nicotinamide. The obtained results show that the nicotinamide treatment importantly increases the thyroid radio destructive effect induced by radioiodine. Under these experimental conditions, nicotinamide induces to a significant increase of thyroid vascularisation, without changes in the proteins ADP-ribosylation activity. These results show, for the first time, the radiosensitizer effect of nicotinamide in front of Iodine 131 and give the possibility of using it in the treatment of hyperthyroid or thyroid difference cancer patients. (author)

  19. Fractional Effective Action at strong electromagnetic fields

    Kleinert, Hagen; Xue, She-Sheng

    2013-01-01

    In 1936, Weisskopf showed that for vanishing electric or magnetic fields the strong-field behavior of the one loop Euler-Heisenberg effective Lagrangian of quantum electro dynamics (QED) is logarithmic. Here we generalize this result for different limits of the Lorentz invariants \\(\\vec{E}^2-\\vec{B}^2\\) and \\(\\vec{B}\\cdot\\vec{E}\\). The logarithmic dependence can be interpreted as a lowest-order manifestation of an anomalous power behavior of the effective Lagrangian of QED, with critical exponents \\(\\delta=e^2/(12\\pi)\\) for spinor QED, and \\(\\delta_S=\\delta/4\\) for scalar QED.

  20. Background independent effective action from D=1 matrix model

    We derive the background independent form of the Das-Jevicki action. The tachyon terms are given to all orders by a generally covariant form of the Das-Jevicki action. The graviton-dilaton sector is the usual low energy effective action. This enables us to examine questions such as the back reaction of the tachyon on the metric. In particular the reason why the usual Liouville term is an exact solution of the conformal invariance conditions, as well as the fact that it has no back reaction, become manifest. We comment on the propagation of a tachyonic perturbation in the background of a black-hole metric. (orig.)

  1. Effectiveness of modified seminars as a teaching-learning method in pharmacology

    Palappallil, Dhanya Sasidharan; Sushama, Jitha; Ramnath, Sai Nathan

    2016-01-01

    Context: Student-led seminars (SLS) are adopted as a teaching-learning (T-L) method in pharmacology. Previous studies assessing the feedback on T-L methods in pharmacology points out that the traditional seminars consistently received poor feedbacks as they were not favorite among the students. Aims: This study aimed to obtain feedback on traditional SLS, introduce modified SLS and compare the modified seminars with the traditional ones. Settings and Design: This was a prospective interventional study done for 2 months in medical undergraduates of fifth semester attending Pharmacology seminars at a Government Medical College in South India. Subjects and Methods: Structured questionnaire was used to elicit feedback from participants. The responses were coded on 5-point Likert scale. Modifications in seminar sessions such as role plays, quiz, tests, group discussion, and patient-oriented problem-solving exercises were introduced along with SLS. Statistical Analysis Used: The data were analyzed using SPSS version 16. The descriptive data were expressed using frequencies and percentages. Wilcoxon signed rank test, and Friedman tests were used to compare traditional with modified seminars. Results: The participants identified interaction as the most important component of a seminar. Majority opined that the teacher should summarize at the end of SLS. Student feedback shows that modified seminars created more interest, enthusiasm, and inspiration to learn the topic when compared to traditional SLS. They also increased peer coordination and group dynamics. Students opined that communication skills and teacher-student interactions were not improved with modified seminars. Conclusions: Interventions in the form of modified SLS may be adopted to break the monotony of traditional seminars through active participation, peer interaction, and teamwork.

  2. Pharmacological activities of Curcuma caesia

    Satyendra Singh Baghel

    2013-01-01

    Full Text Available Curcuma caesia Roxb. is a perennial, erect rhizomatous herb with large leaves. Fresh rhizomes are aromatic with intense camphoraceous odour, cultivated for its rhizomes, which are used in traditional medicine. The plant is reported to contain camphor, ar-turmerone, (Z-ocimene, ar-curcumene, 1, 8-cineole, elemene, borneol, bornyl acetate and curcumene as the major constituents. The plant has been reported to have antifungal activity, anti-asthmatic, smooth muscle relaxant, antimicrobial activity, antioxidant activity, analgesic, locomotor depressant, anticonvulsant and muscle relaxant effects, anti-inflammatory properties. It is now considered as a valuable source of unique natural products for development of medicines against various diseases. This review gives a view mainly on the meditional uses, phytochemistry and pharmacological actions of the plant.

  3. Morphology, pharmacological activity, pharmaceutical preparation, doses and side effect of Coccinia indica (Wight & Arn.: An overview

    Mayank Kumar

    2013-11-01

    Full Text Available Traditional system of medicine consists of large number of plants with various medicinal and pharmacological importances and hence represents a priceless tank of new bioactive molecules. Coccinia indica belongs to the family Cucurbitaceae. It is a rapidly growing, perennial climber or trailing vine. Traditionally different parts of this plant namely the roots, leaves and fruits are used in folklore medicine for several purposes like jaundice, diabetes, wound healing, ulcers, stomach ache, skin disease, fever, asthma, cough. The leaf and its constituents have been reported to possess hypoglycaemic, hypolipidemic and antioxidant properties. This review provides adequate information to develop suitable therapeutics out of these plant parts.

  4. 76 FR 38668 - Advisory Committee for Pharmaceutical Science and Clinical Pharmacology; Notice of Meeting

    2011-07-01

    ... Pharmacology; Notice of Meeting AGENCY: Food and Drug Administration, HHS. ACTION: Notice. This notice... Science and Clinical Pharmacology. General Function of the Committee: To provide advice and... April 13, 2010, Advisory Committee for Pharmaceutical Science and Clinical Pharmacology...

  5. 76 FR 3912 - Advisory Committee for Pharmaceutical Science and Clinical Pharmacology; Notice of Meeting

    2011-01-21

    ... Pharmacology; Notice of Meeting AGENCY: Food and Drug Administration, HHS. ACTION: Notice. This notice... Science and Clinical Pharmacology. General Function of the Committee: To provide advice and... how to optimally utilize mechanistic biomarkers and apply clinical pharmacology tools, such...

  6. Renormalization and Effective Actions for General Relativity

    Neugebohrn, Falk

    2007-01-01

    Quantum gravity is analyzed from the viewpoint of the renormalization group. The analysis is based on methods introduced by J. Polchinski concerning the perturbative renormalization with flow equations. In the first part of this work, the program of renormalization with flow equations is reviewed and then extended to effective field theories that have a finite UV cutoff. This is done for a scalar field theory by imposing additional renormalization conditions for some of the nonrenormalizable couplings. It turns out that one so obtains a statement on the predictivity of the effective theory at scales far below the UV cutoff. In particular, nonrenormalizable theories can be treated without problems in the proposed framework. In the second part, the standard covariant BRS quantization program for Euclidean Einstein gravity is applied. A momentum cutoff regularization is imposed and the resulting violation of the Slavnov-Taylor identities is discussed. Deriving Polchinski's renormalization group equation for Eucl...

  7. Renormalization and effective actions for general relativity

    Quantum gravity is analyzed from the viewpoint of the renormalization group. The analysis is based on methods introduced by J. Polchinski concerning the perturbative renormalization with flow equations. In the first part of this work, the program of renormalization with flow equations is reviewed and then extended to effective field theories that have a finite UV cutoff. This is done for a scalar field theory by imposing additional renormalization conditions for some of the nonrenormalizable couplings. It turns out that one so obtains a statement on the predictivity of the effective theory at scales far below the UV cutoff. In particular, nonrenormalizable theories can be treated without problems in the proposed framework. In the second part, the standard covariant BRS quantization program for Euclidean Einstein gravity is applied. A momentum cutoff regularization is imposed and the resulting violation of the Slavnov-Taylor identities is discussed. Deriving Polchinski's renormalization group equation for Euclidean quantum gravity, the predictivity of effective quantum gravity at scales far below the Planck scale is investigated with flow equations. A fine-tuning procedure for restoring the violated Slavnov-Taylor identities is proposed and it is argued that in the effective quantum gravity context, the restoration will only be accomplished with finite accuracy. Finally, the no-cutoff limit of Euclidean quantum gravity is analyzed from the viewpoint of the Polchinski method. It is speculated whether a limit with nonvanishing gravitational constant might exist where the latter would ultimatively be determined by the cosmological constant and the masses of the elementary particles. (orig.)

  8. Renormalization and effective actions for general relativity

    Neugebohrn, F.

    2007-05-15

    Quantum gravity is analyzed from the viewpoint of the renormalization group. The analysis is based on methods introduced by J. Polchinski concerning the perturbative renormalization with flow equations. In the first part of this work, the program of renormalization with flow equations is reviewed and then extended to effective field theories that have a finite UV cutoff. This is done for a scalar field theory by imposing additional renormalization conditions for some of the nonrenormalizable couplings. It turns out that one so obtains a statement on the predictivity of the effective theory at scales far below the UV cutoff. In particular, nonrenormalizable theories can be treated without problems in the proposed framework. In the second part, the standard covariant BRS quantization program for Euclidean Einstein gravity is applied. A momentum cutoff regularization is imposed and the resulting violation of the Slavnov-Taylor identities is discussed. Deriving Polchinski's renormalization group equation for Euclidean quantum gravity, the predictivity of effective quantum gravity at scales far below the Planck scale is investigated with flow equations. A fine-tuning procedure for restoring the violated Slavnov-Taylor identities is proposed and it is argued that in the effective quantum gravity context, the restoration will only be accomplished with finite accuracy. Finally, the no-cutoff limit of Euclidean quantum gravity is analyzed from the viewpoint of the Polchinski method. It is speculated whether a limit with nonvanishing gravitational constant might exist where the latter would ultimatively be determined by the cosmological constant and the masses of the elementary particles. (orig.)

  9. Pharmacological approach to acute pancreatitis

    Bang, Ulrich-Christian; Semb, Synne; Nojgaard, Camilla;

    2008-01-01

    The aim of the present review is to summarize the current knowledge regarding pharmacological prevention and treatment of acute pancreatitis (AP) based on experimental animal models and clinical trials. Somatostatin (SS) and octreotide inhibit the exocrine production of pancreatic enzymes and may....... Evidence based pharmacological treatment of AP is limited and studies on the effect of potent anti-inflammatory drugs are warranted....

  10. An investigation of sex-linked differences to the toxic and to the pharmacological actions of difenacoum: studies in mice and rats.

    Winn, M J; Clegg, J A; Park, B K

    1987-03-01

    We have investigated the actions of the coumarin anticoagulant, difenacoum, in male and female rats and mice. In our first experiment difenacoum (0.5 mg kg-1) killed 50% of male mice within 9 days of its administration, whereas no female mice died during this study. In a second group of experiments, the anticoagulant effect of difenacoum in male and female rats was determined. Under resting conditions, the prothrombin complex activities (PCA) of male and female rats were not significantly different. Over the first 24 h after administration of difenacoum (0.4 mg kg-1 i.p.), there was a monoexponential fall in PCA in both sexes. However, 6, 12 and 24 h after difenacoum, the PCA in male rats was significantly (P less than 0.05) lower than in female rats. PCA began to recover over the subsequent 48 h in both sexes, during which time there was marked variability in recovery in female rats. The difference between the onset of action of difenacoum in male and female rats did not appear to be due to a greater rate of elimination of the drug in female rats, since the plasma concentrations of difenacoum 24 h after its administration were the same in both sexes. The concentration of vitamin K1 in rat liver was also investigated. Vitamin K1 levels were 35.1 +/- 18.6 ng (g liver)-1 (male), and 29.4 +/- 5.4 ng (g liver)-1 (females) in control rats, but 24 h after difenacoum, vitamin K1 levels were either very low, or undetectable in all rats.(ABSTRACT TRUNCATED AT 250 WORDS) PMID:2883288