WorldWideScience

Sample records for cardiotonics

  1. Bipyridine cardiotonics: the three-dimensional structures of amrinone and milrinone.

    Science.gov (United States)

    Robertson, D W; Beedle, E E; Swartzendruber, J K; Jones, N D; Elzey, T K; Kauffman, R F; Wilson, H; Hayes, J S

    1986-05-01

    The cardiotonic drug milrinone (1,6-dihydro-2-methyl-6-oxo-[3,4'-bipyridine]-5-carbonitrile) is superior to its analogue amrinone (5-amino-[3,4'-bipyridin]-6(1H)-one) by virtue of its greater potency and reduced side effect profile. We confirmed initial reports on the potencies of milrinone and amrinone and found that after intravenous administration to phenobarbital anesthetized dogs, the drugs had cumulative inotropic ED50's of 37 and 1891 micrograms/kg, respectively; relative effects on heart rate and blood pressure were comparable. There are two structural differences between amrinone and milrinone: (1) milrinone has a pyridone 2-methyl substituent and (2) the pyridone 5-amino substituent of amrinone is replaced with a nitrile in milrinone. We confirmed structure-activity studies that indicated that the 2-methyl substituent appears to be primarily responsible for the dramatic difference in the potencies of amrinone and milrinone. A plausible explanation for the effect of the methyl substituent is an altered molecular topology resulting from its steric interaction with the 3',5'-hydrogen atoms. Consequently, we probed the three-dimensional structures of these two compounds by X-ray crystallography. The dihedral angle between the planes formed by the two aromatic rings of amrinone was 1.3 degrees. In marked contrast, the corresponding angle for milrinone was 52.2 degrees. Moreover, 1H NMR studies revealed conformational differences in solution. Whereas the 2-methyl substituent undoubtedly produces some electronic and hydrophobic perturbations in the bipyridine cardiotonic series, the most significant effect, from a global viewpoint, is the altered molecular topology. PMID:3701782

  2. The Physiological Significance of the Cardiotonic Steroid/Ouabain-Binding Site of the Na,K-ATPase

    Science.gov (United States)

    Lingrel, Jerry B

    2011-01-01

    The Na,K-ATPase is the membrane “pump” that generates the Na+ and K+ gradients across the plasma membrane that drives many physiological processes. This enzyme is highly sensitive to inhibition by cardiotonic steroids, most notably the digitalis/ouabain class of compounds, which have been used for centuries to treat congestive heart failure and arrhythmias. The amino acids that constitute the ouabain-binding site are highly conserved across the evolutionary spectrum. This could be fortuitous or could result from this site being conserved because it has an important biological function. New physiological approaches using genetically engineered mice are being used to define the biological significance of the “receptor function” of the Na,K-ATPase and its regulation by potential endogenous cardiotonic steroid-like compounds. These studies extend the reach of earlier studies involving the biochemical purification of endogenous regulatory ligands. PMID:20148682

  3. Effects of Cardiotonic Steroids on Trabecular Meshwork Cells: Search for Mediator of Ouabain-Enhanced Outflow Facility

    OpenAIRE

    Li, Ang; Banerjee, Juni; Peterson-Yantorno, Kim; Stamer, W. Daniel; Leung, Chi Ting; Civan, Mortimer M.

    2012-01-01

    Lowering intraocular pressure (IOP) is currently the only strategy documented to slow the onset and progression of glaucomatous blindness. Ouabain, a cardiotonic glycoside inhibitor of Na+, K+-activated ATPase, was recently reported to enhance outflow facility in porcine anterior segments at concentrations as low as 30 nM for ≥ 4 hrs, suggesting a novel approach to lowering IOP. The underlying mechanism is unknown, but associated cytoskeletal changes were observed in porcine trabecular meshwo...

  4. Stabilisation of Na,K-ATPase structure by the cardiotonic steroid ouabain

    Energy Technology Data Exchange (ETDEWEB)

    Miles, Andrew J. [Institute of Structural and Molecular Biology, Birkbeck College, University of London, London WC1E 7HX (United Kingdom); Fedosova, Natalya U. [Department of Biomedicine, Aarhus University, DK-8000 Aarhus (Denmark); Hoffmann, Søren V. [ISA, Department of Physics and Astronomy, Aarhus University, DK-8000 Aarhus (Denmark); Wallace, B.A. [Institute of Structural and Molecular Biology, Birkbeck College, University of London, London WC1E 7HX (United Kingdom); Esmann, Mikael, E-mail: me@biophys.au.dk [Department of Biomedicine, Aarhus University, DK-8000 Aarhus (Denmark)

    2013-05-31

    Highlights: •Ouabain binding to pig and shark Na,K-ATPase enhances thermal stability. •Ouabain stabilises both membrane-bound and solubilised Na,K-ATPase. •Synchrotron radiation circular dichroism is used for structure determination. •Secondary structure in general is not affected by ouabain binding. •Stabilisation is due to re-arrangement of tertiary structure. -- Abstract: Cardiotonic steroids such as ouabain bind with high affinity to the membrane-bound cation-transporting P-type Na,K-ATPase, leading to complete inhibition of the enzyme. Using synchrotron radiation circular dichroism spectroscopy we show that the enzyme-ouabain complex is less susceptible to thermal denaturation (unfolding) than the ouabain-free enzyme, and this protection is observed with Na,K-ATPase purified from pig kidney as well as from shark rectal glands. It is also shown that detergent-solubilised preparations of Na,K-ATPase are stabilised by ouabain, which could account for the successful crystallisation of Na,K-ATPase in the ouabain-bound form. The secondary structure is not significantly affected by the binding of ouabain. Ouabain appears however, to induce a reorganization of the tertiary structure towards a more compact protein structure which is less prone to unfolding; recent crystal structures of the two enzymes are consistent with this interpretation. These circular dichroism spectroscopic studies in solution therefore provide complementary information to that provided by crystallography.

  5. Effects on the sodium channel of some new cardiotonic drugs: the 4-, 5-, and 6-pyridyl-2(1H)-quinolone derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Grima, M.; Beguin, M.F.; Millanvoye-Van Brussel, E.M.; Decker, N.; Schwartz, J.

    1988-09-01

    To study the action of some new cardiotonic drugs, the 4-, 5-, and 6-pyridyl-2(1H)-quinolone series, on the fast Na+ channel, we compared the effects of eight compounds of this series and milrinone on /sup 22/Na uptake in rat brain synaptosomes and in rat heart muscle cells in culture. The action of tetrodotoxin, a specific Na+ channel blocker, on the positive inotropic effect of these compounds on guinea pig atria was also examined. The new positive inotropic agents enhance /sup 22/Na uptake in synaptosomes in a dose-dependent manner. The activities, expressed as percentage of the maximum activity of protoveratrine B, a classic Na+ channel agonist, reached 70% for milrinone, 60% for compound 7, 57% for compound 6, and less than 50% for the other drugs. For compound 8, but not for milrinone, it was possible to observe a stimulatory effect of the /sup 22/Na uptake on heart muscle cells in culture. Tetrodotoxin (1 and 100 microM) inhibited the stimulatory effects of the inotropic drugs on both preparations. The positive inotropic activities of protoveratrine B, milrinone, and compounds 5 and 8, in guinea pig atria, were inhibited by tetrodotoxin. The affinity and the activity of the other compounds were unchanged in the presence of tetrodotoxin. Our results showed that the stimulation of Na+ influx through the fast Na+ channel might represent a part of the mechanism of action of the inotropic effect of some new cardiotonic drugs.

  6. Molecular structure of the dihydropyridazinone cardiotonic 1,3-dihydro-3,3-dimethyl-5-(1,4,5,6-tetrahydro-6-oxo-pyridazinyl)- 2H-indol-2-one, a potent inhibitor of cyclic AMP phosphodiesterase.

    Science.gov (United States)

    Robertson, D W; Jones, N D; Krushinski, J H; Pollock, G D; Swartzendruber, J K; Hayes, J S

    1987-04-01

    The cardiotonic 1,3-dihydro-3,3-dimethyl-5-(1,4,5,6-tetrahydro-6-oxo-3- pyridazinyl)-2H-indol-2-one (1, LY195115) is a potent, competitive inhibitor (Ki = 80 nM) of sarcoplasmic reticulum derived phosphodiesterase (SR-PDE). Moreover, the compound is a potent positive inotrope both in vitro and in vivo. To assist further cardiotonic drug-design studies, we have mapped the three-dimensional structure of 1 using X-ray crystallography. From a global viewpoint, this drug was essentially planar, but two small regions of nonplanarity were apparent. These involved the geminal methyl substituents in the indol-2-one moiety and the C5' methylene unit of the dihydropyridazinone ring. Because of our previous studies involving the bipyridine cardiotonics amrinone and milrinone, the conformational relationship between the plane of the phenyl ring and the horizontal symmetry plane defined by N2', C3', and C4' of 1 was of particular interest. The C6-C5-C3'-C4' dihedral angle was -2.7 degrees, whereas the C6-C5-C3'-N2' dihedral angle was 174.6 degrees. Therefore the two rings maintain a high degree of coplanarity. Compound 4, the congener of 1 possessing a completely unsaturated pyridazinone ring was also studied. In terms of inotropic activity, this compound, devoid of any puckering in the pyridazinone moiety, was equipotent with 1. Methyl substitution at the 4-position of the dihydropyridazinone and pyridazinone rings provided disparate results. Compound 2, the 4-methyl analogue of 1, was 2-fold more potent than 1, and the methyl substituent probably caused only minor perturbations in overall molecular topology. However 5, the 4-methyl analogue of the pyridazinone 4, was 4.4-fold less active than 4, perhaps as a result of methyl-induced molecular nonplanarity. PMID:3031290

  7. Preparation of 14c- amd 180-labeled 2-[2-methoxy-4-(methylsulfinyl)phenyl]-1H-imidazo[4,5-c]-pyridine hydrochloride (LY175326), a cardiotonic with inotropic and vasodilator activities

    International Nuclear Information System (INIS)

    Two different forms of 14C-labeled 2-methoxy-4-(methyl-thio)benzoic acid were prepared and employed in the synthesis of 14C-labeled 2-:2-methoxy-4-(methylsulfinyl)phenyl:-1H-imidazo-[4,5-c]pyridine hydrochloride (LY175326), a cardiotonic with inotropic and vasodilator activities that is currently in clinical trials. The synthetic procedures described in this report allowed the introduction of the 14C-label in the antepenultimate step. Additionally, an 180-labeled form of LY175326 was synthesized to facilitate kinetic analysis of the formation of its sulfide and sulfone metabolites. (author)

  8. THE INFLUENCE OF UNDERLYING PRETRANSPLANT DISEASE ON CARDIOTONIC AND VASOACTIVE THERAPY IN EARLY PERIOD AFTER HEART TRANSPLANTATION

    Directory of Open Access Journals (Sweden)

    V. N. Poptsov

    2011-01-01

    Full Text Available In our study there were 56 patients (54 men and 2 female in age from 16 to 61 (41,2 ± 2,7 years. Severity of CHF in 36 (64,3% patients were corresponded III class NYHA, in 20 (35,7% patients – IV class. 12 (15,5% patients was in 1B status of UNOS, 44 (60,8 % patients – in II status. In all cases biatrial technique of OHT was used, total ischemic time was 107–330 (170 ± 11 min. All recipients were divided on two investigate groups. In the 1-st group (n = 31 recipients with pretransplant ischemic cardiomyopathy (ICM were included, in the 2-nd group (n = 25 – recipients with pretransplant dilated cardiomyopathy (DCM. There was no difference bet- ween groups in basic preoperative characteristic, ischemic transplant time, duration of cardiopulmonary bypass, type and severity of cardiac transplant dysfunction. Our study showed that ICM-group patients had higher level indexed systemic vascular resistance since 3 postoperative day, required more frequent use of dobutamine and isorbide dinitrate for systemic and pulmonary hemodynamic management in this category of heart recipients. Also ICM-group patients had more preferable systemic hemodynamic conditions for application of prostaglan- din E1 in more effective doses. 

  9. Comparative HPLC-DAD-ESI(+MS Fingerprint and Quantification of Phenolic and Flavonoid Composition of Aqueous Leaf Extracts of Cornus mas and Crataegus monogyna, in Relation to Their Cardiotonic Potential

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    Marius BADALICA-PETRESCU

    2014-06-01

    Full Text Available Our study aimed to compare the phenolic and flavonoid composition of two medicinal plants from the wild flora of Romania, traditionally known to be efficient in preventing cardiotoxicity: Cornus mas and Crataegus monogyna. As most previous studies have focused on fruits, our investigations aimed to fingerprint and quantify the two classes of compounds in aqueous leaf extracts, based on HPLC-DAD-ESI(+MS analysis. The specific HPLC-DAD fingerprint was coupled with UV spectra at 280 and 340 nm to discriminate between three subclasses of compounds: two hydroxycinnamic acids and a flavonoid glycoside. While the C. monogyna extract contained more than 98% vitexin isomers (2’- and 4’-O-rhamnoside, the C. mas extract was very complex, containing a mixture of phenolic derivatives and flavonoid glycosides. The spectral patterns of C. mas, combined with the molecular mass and specific fragmentations allowed the identification of epi-catechin, coumaric and caffeic acids and quercetin derivatives. Based on LC-MS peak area and parallel calibrations with gallic acid and rutin, the mean concentration for flavonoids in C. mas was 13 mg/100 ml, while aprox. 65 mg/100 ml in C. monogyna extracts. Using the Folin method, the total phenol content was 105 mg/100 ml in C. mas and around three times less in the C. monogyna extract, while the antioxidant activity was increased only 1.5-1.7 times in C. mas extract compared to C. monogyna. These findings suggest a higher stability and potential of flavonoids to act as antioxidants in hydrophilic environment.

  10. Comparative HPLC-DAD-ESI(+)MS Fingerprint and Quantification of Phenolic and Flavonoid Composition of Aqueous Leaf Extracts of Cornus mas and Crataegus monogyna, in Relation to Their Cardiotonic Potential

    OpenAIRE

    Marius BADALICA-PETRESCU; DRAGAN, SIMONA; Floricuţa RANGA; Florinela FETEA; Socaciu, Carmen

    2014-01-01

    Our study aimed to compare the phenolic and flavonoid composition of two medicinal plants from the wild flora of Romania, traditionally known to be efficient in preventing cardiotoxicity: Cornus mas and Crataegus monogyna. As most previous studies have focused on fruits, our investigations aimed to fingerprint and quantify the two classes of compounds in aqueous leaf extracts, based on HPLC-DAD-ESI(+)MS analysis. The specific HPLC-DAD fingerprint was coupled with UV spectra at 280 and 340 nm ...

  11. Design and Development of Novel 4-(4-(1H-Tetrazol-5-yl)-1H-pyrazol-1-yl)-6-morpholino-N-(4-nitrophenyl)-1,3,5-triazin-2-amine as Cardiotonic Agent via Inhibition of PDE3.

    Science.gov (United States)

    Mao, Zhi-Wei; Li, Qiao-Ling; Wang, Ping; Sun, Yang-Li; Liu, Yu

    2016-04-01

    The classical phosphodiesterase 3A (PDE3A) inhibitors provide relaxation of the vasculature system via increasing the cellular level of cyclic adenosine monophosphate (cAMP) and proved to be useful in the management of congestive heart failure. Consequently, the present paper deals with the development of novel pyrazole derivatives tethered with substituted 1,3,5-triazine derivatives in search for novel PDE3 inhibitors. The synthesis of designed inhibitors was realized in a multi-step reaction and the structures were ascertained with the help of various spectroscopic techniques. Subsequently, these analogs were tested for their inhibitory activities against PDE3 enzymes, where they exhibited considerable inhibition, revealing 9g as the most promising inhibitor of the class. In a docking study, the morpholine fragment of compound 9g was efficiently engulfed in the small pocket of the active site lined by Gly940 and Pro941. The substituted aromatic ring of the core scaffold was found to be positioned deep in the cavity bordered by Tyr829, Asn830, Leu850, Glu851, and Thr893. Moreover, it considerably improved the contractility of cardiac muscles without altering the heart beat frequency in experimental subjects. PMID:26934198

  12. Evaluating the Cancer Therapeutic Potential of Cardiac Glycosides

    OpenAIRE

    José Manuel Calderón-Montaño; Estefanía Burgos-Morón; Manuel Luis Orta; Dolores Maldonado-Navas; Irene García-Domínguez; Miguel López-Lázaro

    2014-01-01

    Cardiac glycosides, also known as cardiotonic steroids, are a group of natural products that share a steroid-like structure with an unsaturated lactone ring and the ability to induce cardiotonic effects mediated by a selective inhibition of the Na+/K+-ATPase. Cardiac glycosides have been used for many years in the treatment of cardiac congestion and some types of cardiac arrhythmias. Recent data suggest that cardiac glycosides may also be useful in the treatment of cancer. These compounds typ...

  13. Estratégia de simplificação molecular no planejamento racional de fármacos: a descoberta de novo agente cardioativo Strategy of molecular simplification in rational drug design: the discovery of a new cardioactive agent

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    Eliezer J. Barreiro

    2002-12-01

    Full Text Available In this article are described examples of the successful use of molecular simplification strategy in the discovery of new drugs from bioactive natural products and synthetic compounds. The discovery of a new cardiotonic derivative (37, 2-thienylidene-3,4-methylenedioxybenzoylhydrazine; LASSBio-294, efficiently synthesized from Brazilian natural product and structurally designed by molecular simplification of active pyridazinone compounds reported in the literature, is described. A brief description of the pharmacological profile of this new cardiotonic lead-compound, belonging to the N-acylhydrazone (NAH class, is also reported herein.

  14. An account of phytochemicals from Plumbago zeylanica (Family: Plumbaginaceae): A natural gift to human being #

    OpenAIRE

    Navneet Kishore; Bhuwan B Mishra; Vinod K Tiwari; Vyasji Tripathi

    2012-01-01

    The semi-climbing sub-shrub Plumbago zeylanica (family: Plumbaginaceae) is a widely accepted ethnomedicine around the world including India, Pakistan, Bangladesh, Sri Lanka, and Australia. The plant is credited with potential therapeutic properties including antiatherogenic, cardiotonic, hepatoprotective, and neuroprotective properties. The present review highlights the various medicinal and pharmacological aspects along with recent updates on phytochemical contents of the plant.

  15. OUABAIN AND INSULIN INDUCE SODIUM PUMP ENDOCYTOSIS IN RENAL EPITHELIUM

    OpenAIRE

    Gupta, Shalini; Yan, Yanling; Malhotra, Deepak; Liu, Jiang; Xie, Zijian; Najjar, Sonia M.; Shapiro, Joseph I

    2012-01-01

    Cardiotonic steroids signaling through the basolateral sodium pump (Na/KATPase) have been shown to alter renal salt handling in intact animals. As the relationship between renal salt handling and blood pressure is a key determinant of hypertension, and patients with insulin resistance are frequently hypertensive, we chose to examine whether there might be competition for resources necessary for receptor mediated endocytosis.

  16. Drugs and lactation

    International Nuclear Information System (INIS)

    Different kinds of drugs who can be transferred through the mother's milk to the lactant and its effects are showed in this work. A list of them as below: cardiotonics, diuretics, anti-hypertensives, beta-blockings, anti-arrythmics, drugs with gastrintestinal tract action, hormones, antibiotics and chemotherapeutics, citostatic drugs, central nervous system action drugs and anticoagulants drugs. (L.M.J.)

  17. Morphofunctional state of the heart in children and adolescents who suffered due to Chernobyl accident (findings of ultrasound studies)

    International Nuclear Information System (INIS)

    Great incidence of intracardiac hemodynamic disorders in children and adolescents evacuated from the contaminated zone (mainly in those who resided in Zhytomir region for a long period) testifies to the possible negative effect of ionizing radiation on cardiovascular system. A rehabilitation treatment scheme for such children and adolescents should include cardiotonic and vegetotropic remedies

  18. An account of phytochemicals from Plumbago zeylanica (Family: Plumbaginaceae: A natural gift to human being #

    Directory of Open Access Journals (Sweden)

    Navneet Kishore

    2012-01-01

    Full Text Available The semi-climbing sub-shrub Plumbago zeylanica (family: Plumbaginaceae is a widely accepted ethnomedicine around the world including India, Pakistan, Bangladesh, Sri Lanka, and Australia. The plant is credited with potential therapeutic properties including antiatherogenic, cardiotonic, hepatoprotective, and neuroprotective properties. The present review highlights the various medicinal and pharmacological aspects along with recent updates on phytochemical contents of the plant.

  19. Quantitative estimation of phenolic and flavonoid content and antioxidant activity of various extracts of different parts of Plumbago zeylanica Linn

    OpenAIRE

    Sharma Ira; Mathur Manisha; Singh G.P; Rishi Anirudha

    2014-01-01

    Plumbagozeylanica (Chitrak) is used as medicinal plant in India. The root of the plant and its constituents are credited with potential therapeutic properties including anti-atherogenic,cardiotonic, hepatoprotective and neuroprotective properties. In recent times, interest hasfocused on phytochemicals as new sources of natural antioxidants. Therefore in the present study methanolic crude extracts of stem, leaves, roots of Plumbagozeylanica were screened for their antioxidant property, phenoli...

  20. Multi-modal contributions to detoxification of acute pharmacotoxicity by a triglyceride micro-emulsion

    OpenAIRE

    Fettiplace, Michael R.; Lis, Kinga; Ripper, Richard; Kowal, Katarzyna; Pichurko, Adrian; Vitello, Dominic; Rubinstein, Israel; Schwartz, David; Akpa, Belinda S.; Weinberg, Guy

    2014-01-01

    Triglyceride micro-emulsions such as Intralipid® have been used to reverse cardiac toxicity induced by a number of drugs but reservations about their broad-spectrum applicability remain because of the poorly understood mechanism of action. Herein we report an integrated mechanism of reversal of bupivacaine toxicity that includes both transient drug scavenging and a cardiotonic effect that couple to accelerate movement of the toxin away from sites of toxicity. We thus propose a multi-modal the...

  1. Study on diuretic activity of saffron (stigma of Crocus sativus L.) Aqueous extract in rat

    OpenAIRE

    Nabi Shariatifar; Shahram Shoeibi; Moslem Jaferi Sani; Amir Hossein Jamshidi; Ali Zarei; Abbas Mehdizade; Manouchehr Dadgarnejad

    2014-01-01

    Saffron is the most expensive spice in the world and consists of the dried stigmas of Crocus sativus L. It is used as food coloring and flavoring in food industry and traditional cooking and also in folk medicine as antispasmodic, carminative, stomachic, expectorant, aphrodisiac and cardiotonic. The present study has evaluated the diuretic activity of aqueous extract of dried saffron (stigma of Crocussativus) in rat. Aqueous extracts of saffron were administered to experimental rats orally as...

  2. Complex therapeutic approach in a child with syndromic morbid obesity and acute heart failure

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    Lenuţa Popa

    2011-11-01

    Full Text Available We report a case of a three years old child, a boy with acute heart failure associated at a rarecomplex genetic disorders characterized by severe obesity and hypotonia. The treatment consisted ofacute phase diuretics and cardiotonic drugs, followed by chronic angiotensin-converting-enzyme (ACEinhibitor (Enalapril and an aldosterone inhibitor. The child recovered within a few days and remainedclinically stable, with improvement of clinical, EKG and echocardiographic parameters at 2 and 6 - monthfollow-up.

  3. 1,2,4-triazine derivatives: Synthesis and biological applications

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    Mohammad Arshad

    2014-04-01

    Full Text Available 1,2,4-Triazines are the six membered heterocyclic compounds possessing three nitrogen in its structure with general formula C3H3N3. 1,2,4-Triazines and its derivatives have been found to exhibit the variety of biological applications such as antifungal, anti-HIV, anticancer, antiinflammatory, analgesic and antihypertensive, cardiotonic, neuroleptic, nootropic, antihistaminergic, tuberculostatic, antiviral, anti-protozoal, estrogen receptor modulators, antimalarial, cyclin-dependent kinase inhibitors, antimicrobial and antiparasitic activities.

  4. 1,2,4-triazine derivatives: Synthesis and biological applications

    OpenAIRE

    Mohammad Arshad; Taki Ahmed Khan; Meraj Alam Khan

    2014-01-01

    1,2,4-Triazines are the six membered heterocyclic compounds possessing three nitrogen in its structure with general formula C3H3N3. 1,2,4-Triazines and its derivatives have been found to exhibit the variety of biological applications such as antifungal, anti-HIV, anticancer, antiinflammatory, analgesic and antihypertensive, cardiotonic, neuroleptic, nootropic, antihistaminergic, tuberculostatic, antiviral, anti-protozoal, estrogen receptor modulators, antimalarial, cyclin-dependent kinase inh...

  5. Isolasi dan Identifikasi Senyawa Steroid/Triterpenoid dari Tinta Sotong (Sepia recurvirostra)

    OpenAIRE

    Aris, Suwarti

    2016-01-01

    Cuttlefish is a cephalopodeclass commonly found in the coastal waters of Europe, Africa, Asia and the South Pacific. Cuttlefish is a type of seafood with very high nutrition, but in Indonesia cuttlefish consumption just meat alone and the ink sac is still regarded as wastes. Chemical compound of meat and ink of Sepia recurvirostra contains steroid/triterpenoid. Steroids/triterpenoids as chemical compound have been widely used in medicine as cardiotonic, oral contraseption an...

  6. CD36 and Na/K-ATPase-α1 Form a Pro-inflammatory Signaling Loop in Kidney

    OpenAIRE

    Kennedy, David J.; Chen, Yiliang; Huang, Wenxin; Viterna, Jamie; Liu, Jiang; Westfall, Kristen; Tian, Jian; Bartlett, David J.; Wilson Tang, W. H.; Xie, Zi-jian; Shapiro, Joseph I; Silverstein, Roy L.

    2012-01-01

    Pro-atherogenic, hyperlipidemic states demonstrate increases in circulating ligands for scavenger receptor CD36 (e.g. oxidized LDL (oxLDL)) and the Na/K-ATPase (e.g. cardiotonic steroids). These factors increase inflammation, oxidative stress, and progression of chronic kidney disease. We hypothesized that diet-induced obesity and hyperlipidemia potentiate a CD36/ Na/K-ATPase -dependent inflammatory paracrine loop between proximal tubule cells (PTC) and their associated macrophages and thereb...

  7. Comparison between effects of caffeine and ryanodine on electromechanical coupling in myocardium of hibernating chipmunks: role of internal Ca stores.

    OpenAIRE

    Kondo, N

    1988-01-01

    1. To clarify the cause of uncoupling of Ca influx through Ca channels and the contractility of the myocardium in hibernating chipmunks, the electromechanical effects of two different internal Ca store inhibitors, caffeine and ryanodine, and a cardiotonic agent, isoprenaline, were investigated in papillary muscles of hibernating animals. 2. Ryanodine (10(-6) M), an inhibitor of internal Ca release, abolished the contraction with a marked inhibition of the action potential plateau (APp). In su...

  8. Drug: D03819 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D03819 Crude, Drug Digitalis (USP); Digiglusin (TN) Digitoxin [CPD:C06955], Gitalox...in, Gitoxin [CPD:C08866], F-Gitonin Digitalis purpurea [TAX:4164] Cardiotonic [DS: H00294] Same as: E00230 A... C01 CARDIAC THERAPY C01A CARDIAC GLYCOSIDES C01AA Digitalis glycosides C01AA03 Digitalis leaves D03819 Digitalis (USP) CAS: 8031-42-3 PubChem: 17397906 ...

  9. Cardioprotective properties of Crataegus oxycantha extract against ischemia-reperfusion injury

    OpenAIRE

    Swaminathan, Jayachandran Kesavan; Khan, Mahmood; Mohan, Iyappu K; Selvendiran, Karuppaiyah; Devaraj, S. Niranjali; Rivera, Brian K.; Kuppusamy, Periannan

    2010-01-01

    The aim of the study was to investigate the cardioprotective effect and mechanism of Crataegus oxycantha (COC) extract, a well-known natural antioxidant-based cardiotonic, against ischemia/reperfusion (I/R) injury. Electron paramagnetic resonance studies showed that COC extract was capable of scavenging superoxide, hydroxyl, and peroxyl radicals, in vitro. The cardioprotective efficacy of the extract was studied in a crystalloid perfused heart model of I/R injury. Hearts were subjected to 30 ...

  10. The determination of hyperoside in the flower and leaf of hawthorn (Crataegus oxycantha and Crataegus monogyna) by the spectrophotometric method

    OpenAIRE

    Mihajlović Dušanka; Novković Vesna; Banković Vladimir

    2006-01-01

    The flower and leaf of hawthorn contains many active components, used in the production of pharmaceutical preparations for cardiotonic, anti-hypertonic anti-hypotonic, artherosclerotic, anti-arithmic and anti-anemic groups. According to the ROTTE list (1996), 159 of 1800 pharmaceutical preparations contain components from hawthorn. Due to the remedial action of hyperoside and other flavonoids from hawthorn, their determination is important for the standardization of extract and preparation qu...

  11. On the ethnomedical significance of the Arjun tree, Terminalia arjuna (Roxb.) Wight & Arnot.

    Science.gov (United States)

    Kumar, D S; Prabhakar, Y S

    1987-07-01

    Terminalia arjuna is an important cardiotonic plant described in the Ayurveda, the ancient Indian medical science. It is also believed to have the ability to cure hepatic, urogenital, venereal and viral diseases. An attempt is made here to analyse the available drug recipes using this plant from Sanskrit literature in the light of modern scientific knowledge. The chemistry and pharmacology of T. arjuna are also discussed, and areas of future investigations are identified. PMID:3657247

  12. Na+ channels as sites of action of the cardioactive agent DPI 201-106 with agonist and antagonist enantiomers

    International Nuclear Information System (INIS)

    This paper shows the interaction of the cardiotonic agent 4-[3-(4-diphenylmethyl-1-piperazinyl)-2-hydroxypropoxy]-1H-indole-2-carbonitrile (DPI 201-106) and its optic enantiomers R-DPI (205-429) and S-DPI (205-430) with the Na+ channel of a variety of excitable cells. Voltage-clamp experiments show that DPI 201-106 acts on neuroblastoma cells and rat cardiac cells. S-DPI (205-430) increases the peak Na+ current, slows down the kinetics of Na+ channel inactivation, and is cardiotonic on heart cells. Conversely, R-DPI (205-429) reduces the peak Na+ current and blocks Na+ channel activity and cardiac contractions. Binding experiments using radioactively labeled toxins indicate that DPI 201-106 and its enantiomers do not interact with sites already identified for tetrodotoxin or sea anemone and scorpion toxins. DPI 201-106 and its enantiomers inhibit binding of a 3H-labeled batrachotoxin derivative, [3H]batrachotoxinin A 20-α-benzoate, to brain membranes. The dissociation constant of the complex formed between the Na+ channel and both R-DPI and S-DPI is K/sub d/ ∼ 100 nM. 22Na+ uptake experiments using different cell types have shown that R and S enantiomers of DPI 201-106 are active on the different Na+ channel subtypes with similar IC50 values. These results are discussed in relation with the cardiotonic properties of DPI 201-106 that are not accompanied by cardiotoxic effects

  13. Plumbagin (5-hydroxy-2-methyl-1,4-naphthoquinone), isolated from Plumbago zeylanica, inhibits ultraviolet radiation-induced development of squamous cell carcinomas

    OpenAIRE

    Sand, Jordan M.; Hafeez, Bilal Bin; Jamal, Mohammad Sarwar; Witkowsky, Olya; Siebers, Emily M.; Fischer, Joseph; Verma, Ajit K.

    2011-01-01

    Plumbagin (PL) (5-hydroxy-2-methyl-1,4-napthoquinone), a medicinal plant-derived naphthoquinone, was isolated from the roots of the Plumbago zeylanica L. (also known as Chitrak). The roots of P. zeylanica L. have been used in Indian medicine for >2500 years as an anti-atherogenic, cardiotonic, hepatoprotective and neuroprotective agent. We present here that topical application of non-toxic doses (100–500 nmol) of PL to skin elicits dose-dependent inhibition of ultraviolet radiation (UVR)-indu...

  14. Review of Astragali Radix

    Institute of Scientific and Technical Information of China (English)

    LIU Jing; ZHAO Zhong-zhen; CHEN Hu-biao

    2011-01-01

    Astragali Radix (AR), known as Huangqi in China, is one of the most popular herbal medicines learnt worldwide to reinforce Qi (the vital energy). AR is traditionally prepared from the dried roots of Astragalus membranaceus or A. membranaceus var. mongholicus. It has been reported to have cardiotonic, hepatoprotective, hypotensive, immunostimulant, anti-aging, anti-oxidative, antidiabetic, and anti-inflammatory activities. The bioactive compounds were found to be flavonoids, saponins, polysaccharides, amino acids, and some trace elements. The present paper reviews the studies on AR including history, phytochemistry studies, pharmacological functions, and clinical application in recent years.

  15. Pumiliotoxin B binds to a site on the voltage-dependent sodium channel that is allosterically coupled to other binding sites.

    OpenAIRE

    Gusovsky, F; Rossignol, D P; McNeal, E T; Daly, J W

    1988-01-01

    Pumiliotoxin B (PTX-B), an alkaloid that has cardiotonic and myotonic activity, increases sodium influx in guinea pig cerebral cortical synaptoneurosomes. In the presence of scorpion venom (Leiurus) or purified alpha-scorpion toxin, the PTX-B-induced sodium influx is enhanced severalfold. PTX-B alone has no effect on sodium flux in N18 neuroblastoma cells but, in the presence of alpha-scorpion toxin, stimulation of sodium influx by PTX-B reaches levels comparable to that attained with the sod...

  16. An updated review on the parasitic herb of Cuscuta reflexa Roxb.

    Directory of Open Access Journals (Sweden)

    Satish Patel

    2012-03-01

    Full Text Available ABSTRACT: Cuscuta reflexa Roxb. is a golden yellow, leafless, perennial, parasitic herb of the family Convolvulaceae. C. reflexa has been investigated for antispasmodic, hemodynamic, anticonvulsant, antisteroidogenic, antihypertensive, muscle relaxant, cardiotonic, antiviral, antibacterial, antioxidant, cholinergic, diuretic and hair growth activities. Many chemical constituents have been isolated from C. reflexa such as cuscutin, amarbelin, β-sitosterol, stigmasterol, kaempferol, dulcitol, myricetin, quercetin, coumarin and oleanolic acid. This review presents a detailed survey of the literature on pharmacognosy, phytochemistry and traditional and biological medicinal uses of C. reflexa.

  17. Drug: D00633 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D00633 Drug Dopamine hydrochloride (JP16/USP); Actopamin (TN); Intropin (TN) C8H11N...O2. HCl 189.0557 189.6394 D00633.gif Adrenergic Therapeutic category: 2119 ATC code: C01CA04 dopamine D1 recepto...zyme: MAOB [HSA:4129], COMT [HSA:1312] Transporter: SLC22A2 [HSA:6582] map07213 Dopamine recepto...dividual organs 21 Cardiovascular agents 211 Cardiotonics 2119 Others D00633 Dopamine hydrochloride (JP16/USP) Anatomical Thera...r agonist [HSA:1812] [KO:K04144]; dopamine D2 receptor agonist [HSA:1813] [KO:K04145]; dopamine D3 recepto

  18. Drug: D01573 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D01573 Drug Etilefrine hydrochloride (JP16); Etilefrine hydrochloride (TN) C10H15NO...2. HCl 217.087 217.6925 D01573.gif Antihypotensive; Sympathomimetic Therapeutic category: 2119 ATC code: C01CA01 alpha1-adr...tion hsa04270(146+147+148) Vascular smooth muscle contraction hsa04970(146+147+148) Salivary secretion Therapeutic category of dr... 211 Cardiotonics 2119 Others D01573 Etilefrine hydrochloride (JP16) Anatomical T...AC STIMULANTS EXCL. CARDIAC GLYCOSIDES C01CA Adrenergic and dopaminergic agents C01CA01 Etilefrine D01573 Etilefrine hydr

  19. Evaluating the Cancer Therapeutic Potential of Cardiac Glycosides

    Directory of Open Access Journals (Sweden)

    José Manuel Calderón-Montaño

    2014-01-01

    Full Text Available Cardiac glycosides, also known as cardiotonic steroids, are a group of natural products that share a steroid-like structure with an unsaturated lactone ring and the ability to induce cardiotonic effects mediated by a selective inhibition of the Na+/K+-ATPase. Cardiac glycosides have been used for many years in the treatment of cardiac congestion and some types of cardiac arrhythmias. Recent data suggest that cardiac glycosides may also be useful in the treatment of cancer. These compounds typically inhibit cancer cell proliferation at nanomolar concentrations, and recent high-throughput screenings of drug libraries have therefore identified cardiac glycosides as potent inhibitors of cancer cell growth. Cardiac glycosides can also block tumor growth in rodent models, which further supports the idea that they have potential for cancer therapy. Evidence also suggests, however, that cardiac glycosides may not inhibit cancer cell proliferation selectively and the potent inhibition of tumor growth induced by cardiac glycosides in mice xenografted with human cancer cells is probably an experimental artifact caused by their ability to selectively kill human cells versus rodent cells. This paper reviews such evidence and discusses experimental approaches that could be used to reveal the cancer therapeutic potential of cardiac glycosides in preclinical studies.

  20. Phytopharmacological overview of Tribulus terrestris.

    Science.gov (United States)

    Chhatre, Saurabh; Nesari, Tanuja; Somani, Gauresh; Kanchan, Divya; Sathaye, Sadhana

    2014-01-01

    Tribulus terrestris (family Zygophyllaceae), commonly known as Gokshur or Gokharu or puncture vine, has been used for a long time in both the Indian and Chinese systems of medicine for treatment of various kinds of diseases. Its various parts contain a variety of chemical constituents which are medicinally important, such as flavonoids, flavonol glycosides, steroidal saponins, and alkaloids. It has diuretic, aphrodisiac, antiurolithic, immunomodulatory, antidiabetic, absorption enhancing, hypolipidemic, cardiotonic, central nervous system, hepatoprotective, anti-inflammatory, analgesic, antispasmodic, anticancer, antibacterial, anthelmintic, larvicidal, and anticariogenic activities. For the last few decades or so, extensive research work has been done to prove its biological activities and the pharmacology of its extracts. The aim of this review is to create a database for further investigations of the discovered phytochemical and pharmacological properties of this plant to promote research. This will help in confirmation of its traditional use along with its value-added utility, eventually leading to higher revenues from the plant. PMID:24600195

  1. Phytopharmacological overview of Tribulus terrestris

    Directory of Open Access Journals (Sweden)

    Saurabh Chhatre

    2014-01-01

    Full Text Available Tribulus terrestris (family Zygophyllaceae, commonly known as Gokshur or Gokharu or puncture vine, has been used for a long time in both the Indian and Chinese systems of medicine for treatment of various kinds of diseases. Its various parts contain a variety of chemical constituents which are medicinally important, such as flavonoids, flavonol glycosides, steroidal saponins, and alkaloids. It has diuretic, aphrodisiac, antiurolithic, immunomodulatory, antidiabetic, absorption enhancing, hypolipidemic, cardiotonic, central nervous system, hepatoprotective, anti-inflammatory, analgesic, antispasmodic, anticancer, antibacterial, anthelmintic, larvicidal, and anticariogenic activities. For the last few decades or so, extensive research work has been done to prove its biological activities and the pharmacology of its extracts. The aim of this review is to create a database for further investigations of the discovered phytochemical and pharmacological properties of this plant to promote research. This will help in confirmation of its traditional use along with its value-added utility, eventually leading to higher revenues from the plant.

  2. Trichosanthes dioica Roxb.: An overview

    Directory of Open Access Journals (Sweden)

    Nitin Kumar

    2012-01-01

    Full Text Available Trichosanthes , a genus of family Cucurbitaceae, is an annual or perennial herb distributed in tropical Asia and Australia. Pointed gourd (Trichosanthes dioica Roxb. is known by a common name of parwal and is cultivated mainly as a vegetable. Juice of leaves of T. dioica is used as tonic, febrifuge, in edema, alopecia, and in subacute cases of enlargement of liver. In Charaka Samhita, leaves and fruits find mention for treating alcoholism and jaundice. A lot of pharmacological work has been scientifically carried out on various parts of T. dioica, but some other traditionally important therapeutical uses are also remaining to proof till now scientifically. According to Ayurveda, leaves of the plant are used as antipyretic, diuretic, cardiotonic, laxative, antiulcer, etc. The various chemical constituents present in T. dioica are vitamin A, vitamin C, tannins, saponins, alkaloids, mixture of noval peptides, proteins tetra and pentacyclic triterpenes, etc.

  3. Trichosanthes dioica Roxb.: An overview.

    Science.gov (United States)

    Kumar, Nitin; Singh, Satyendra; Manvi; Gupta, Rajiv

    2012-01-01

    Trichosanthes, a genus of family Cucurbitaceae, is an annual or perennial herb distributed in tropical Asia and Australia. Pointed gourd (Trichosanthes dioica Roxb.) is known by a common name of parwal and is cultivated mainly as a vegetable. Juice of leaves of T. dioica is used as tonic, febrifuge, in edema, alopecia, and in subacute cases of enlargement of liver. In Charaka Samhita, leaves and fruits find mention for treating alcoholism and jaundice. A lot of pharmacological work has been scientifically carried out on various parts of T. dioica, but some other traditionally important therapeutical uses are also remaining to proof till now scientifically. According to Ayurveda, leaves of the plant are used as antipyretic, diuretic, cardiotonic, laxative, antiulcer, etc. The various chemical constituents present in T. dioica are vitamin A, vitamin C, tannins, saponins, alkaloids, mixture of noval peptides, proteins tetra and pentacyclic triterpenes, etc. PMID:22654406

  4. Medicinal significance, pharmacological activities, and analytical aspects of solasodine:A concise report of current scientific literature

    Institute of Scientific and Technical Information of China (English)

    Kanika Patel; Ravi B Singh; Dinesh K Patel

    2013-01-01

    Alkaloids are well known phytoconstituents for their diverse pharmacological properties. Alkaloids are found in all plant parts like roots, stems, leaves, flowers, fruits and seeds. Solasodine occurs as an aglycone part of glycoalkloids, which is a nitrogen analogue to sapogenins.Solanaceae family comprises of a number of plants with variety of natural products of medicinal significance mainly steroidal lactones, glycosides, alkaloids and flavanoids. It is a steroidal alkaloid based on aC27 cholestane skeleton.Literature survey reveals that solasodine has diuretic, anticancer, antifungal, cardiotonic, antispermatogenetic, antiandrogenic, immunomodulatory, antipyretic and various effects on central nervous system.Isolation and quantitative determination was achieved by several analytical techniques.Present review highlights the pharmacological activity of solasodine, with its analytical and tissue culture techniques, which may be helpful to the researchers to develop new molecules for the treatment of various disorders in the future.

  5. Continuous monitoring of left ventricular function by VEST

    International Nuclear Information System (INIS)

    Using an ambulatory ventricular function monitor (VEST), left ventricular function (LVF) was examined in one healthy volunteer, 3 with ischemic heart disease, and one with dilated myocardiopathy (DMCP) under various conditions, such as treadmill exercise, standing, and sitting. It was also examined when two DCMP patients with associated left ventricular failure were given a nitrite (ISDM) and cardiotonic agent (E 1020). End-diastolic volume (EDV) decreased in the standing position, and increased in exercise, suggesting the involvement of venous blood pool in the legs. Ejection fraction (EF) decreased in the case of widespread ischemia during exercise. Drug tolerance test revealed decrease in EDV and end-systolic volume (ESV), no change in stroke volume (SV), and slight increase in EF on ISDM; and decrease in EDV and ESV, increase in SV, and marked increase in EF on E 1020. For EF, the VEST data were relatively well correlated with gamma camera data. (Namekawa, K.)

  6. Continuous monitoring of left ventricular function by VEST

    Energy Technology Data Exchange (ETDEWEB)

    Ohtake, Tohru; Watanabe, Toshiaki; Kosaka, Noboru and others

    1988-01-01

    Using an ambulatory ventricular function monitor (VEST), left ventricular function (LVF) was examined in one healthy volunteer, 3 with ischemic heart disease, and one with dilated myocardiopathy (DMCP) under various conditions, such as treadmill exercise, standing, and sitting. It was also examined when two DCMP patients with associated left ventricular failure were given a nitrite (ISDM) and cardiotonic agent (E 1020). End-diastolic volume (EDV) decreased in the standing position, and increased in exercise, suggesting the involvement of venous blood pool in the legs. Ejection fraction (EF) decreased in the case of widespread ischemia during exercise. Drug tolerance test revealed decrease in EDV and end-systolic volume (ESV), no change in stroke volume (SV), and slight increase in EF on ISDM; and decrease in EDV and ESV, increase in SV, and marked increase in EF on E 1020. For EF, the VEST data were relatively well correlated with gamma camera data. (Namekawa, K.).

  7. The Role of Na/K-ATPase Signaling in Oxidative Stress Related to Obesity and Cardiovascular Disease.

    Science.gov (United States)

    Srikanthan, Krithika; Shapiro, Joseph I; Sodhi, Komal

    2016-01-01

    Na/K-ATPase has been extensively studied for its ion pumping function, but, in the past several decades, has been identified as a scaffolding and signaling protein. Initially it was found that cardiotonic steroids (CTS) mediate signal transduction through the Na/K-ATPase and result in the generation of reactive oxygen species (ROS), which are also capable of initiating the signal cascade. However, in recent years, this Na/K-ATPase/ROS amplification loop has demonstrated significance in oxidative stress related disease states, including obesity, atherosclerosis, heart failure, uremic cardiomyopathy, and hypertension. The discovery of this novel oxidative stress signaling pathway, holds significant therapeutic potential for the aforementioned conditions and others that are rooted in ROS. PMID:27598118

  8. UNANI DRUGS IN THE MANAGEMENT OF CARDIOVASCULAR DISEASES: A REVIEW ON PHARMACOLOGICAL STUDIES ON ARJUN AND ZAFRAN

    Directory of Open Access Journals (Sweden)

    Rabbani Syed Arman

    2013-06-01

    Full Text Available Cardiovascular diseases (CVDs are the leading cause of death and disability in the world. They have emerged as a major health threat in develop¬ing countries contrary to the prior belief that they were confined primarily to industrialized nations. The global burden of disease due to cardiovascular diseases is escalating, principally due to a sharp rise in the developing countries which are experiencing rapid health transition. An estimated 17.3 million people died from CVDs in 2008 and over 80% of CVD deaths take place in low and middle income countries. By 2030, almost 23.6 million people will die from CVDs. Therefore, finding ways to reduce the mortality of cardiovascular disease remains an important public health goal. Traditional Medicines have been an integral part of the healthcare system since time immemorial. WHO reports indicate that around eighty percent of the global population still relies on botanical drugs and several herbal medicines have advanced to clinical use in modern times. Unani occupies an important place in the rich traditional heritage of indigenous systems of medicine in India and contributes significantly to the health care. The core of treatment in Unani System of Medicine is based on drugs of herbal, mineral and animal origin. The ancient classical literature of Unani has mention of numerous drugs possessing cardioprotective and cardiotonic activity, Arjun (Terminalia arjuna and Zafran (Crocus sativus are two of them. The Unani physicians have been using these drugs successfully since ages and this is possible only by inherent quality and safety standards specified in the system.With the advent of new techniques and recent upsurge towards scientific exploration of traditional medicines, empirical data substantiating their safety and efficacy has been generated and had led to better understanding of their role to prevent and cure diseases. The aim of this paper is to review and highlight the work done on Arjun

  9. ORM-3819 promotes cardiac contractility through Ca(2+) sensitization in combination with selective PDE III inhibition, a novel approach to inotropy.

    Science.gov (United States)

    Nagy, László; Pollesello, Piero; Haikala, Heimo; Végh, Ágnes; Sorsa, Tia; Levijoki, Jouko; Szilágyi, Szabolcs; Édes, István; Tóth, Attila; Papp, Zoltán; Papp, Julius Gy

    2016-03-15

    This study is the first pharmacological characterization of the novel chemical entity, ORM-3819 (L-6-{4-[N'-(4-Hydroxi-3-methoxy-2-nitro-benzylidene)-hydrazino]-phenyl}-5-methyl-4,5-dihydro-2H-pyridazin-3-one), focusing primarily on its cardiotonic effects. ORM-3819 binding to cardiac troponin C (cTnC) was confirmed by nuclear magnetic resonance spectroscopy, and a selective inhibition of the phosphodiesterase III (PDE III) isozyme (IC50=3.88±0.3nM) was revealed during in vitro enzyme assays. The Ca(2+)-sensitizing effect of ORM-3819 was demonstrated in vitro in permeabilized myocyte-sized preparations from left ventricles (LV) of guinea pig hearts (ΔpCa50=0.12±0.01; EC50=2.88±0.14µM). ORM-3819 increased the maximal rate of LV pressure development (+dP/dtmax) (EC50=8.9±1.7nM) and LV systolic pressure (EC50=7.63±1.74nM) in Langendorff-perfused guinea pig hearts. Intravenous administration of ORM-3819 increased LV+dP/dtmax (EC50=0.13±0.05µM/kg) and improved the rate of LV pressure decrease (-dP/dtmax); (EC50=0.03±0.02µM/kg) in healthy guinea pigs. In an in vivo dog model of myocardial stunning, ORM-3819 restored the depressed LV+dP/dtmax and improved % segmental shortening (%SS) in the ischemic area (to 18.8±3), which was reduced after the ischaemia-reperfusion insult (from 24.1±2.1 to 11.0±2.4). Our data demonstrate ORM-3819 as a potent positive inotropic agent exerting its cardiotonic effect by a cTnC-dependent Ca(2+)-sensitizing mechanism in combination with the selective inhibition of the PDE III isozyme. This dual mechanism of action results in the concentration-dependent augmentation of the contractile performance under control conditions and in the postischemic failing myocardium. PMID:26872993

  10. PHYTOCHEMICAL AND PHARMACOLOGICAL PROFILE OF LAGENARIA SICERARIA: AN OVERVIEW

    Directory of Open Access Journals (Sweden)

    Nidhi Tyagi

    2012-03-01

    Full Text Available Cucurbitaceae family is major source of medicinal agents since ancient time. Various plants parts including fruits of this family have been established for their pharmacological potential. Lagenaria siceraria (Molina standley (family Cucurbitaceae commonly known as lauki (Hindi and bottle gourd (English is a medicinal plant. It is used as medicine in India, China, European countries, Brazil, Hawaiian island, etc. for its cardiotonic, general tonic and diuretic properties. Further the antihepatotoxic, analgesic and anti-inflammatory, hypolipidemic, antihyperglycemic, immunomodulatory and antioxidant activities of its fruit extract have been evaluated. It is used as vermifuge purgative diuretic and it is also recommended for increasing lactation for lactating women..Fruits are also used in treatment of cancer, pain, ulcer, fever, pectoral cough, asthma and other bronchial disorders. In many countries, this plant has been used traditionally as a single treatment for diabetes mellitus possess immunosuppressive, antitumour, antiviral, antiproliferative and anti-HIV activities. This study is an attempt to compile an up-to-date and comprehensive review of Lagenaria siceraria that covers its traditional and folk medicinal uses, phytochemistry and pharmacology profile.

  11. The determination of hyperoside in the flower and leaf of hawthorn (Crataegus oxycantha and Crataegus monogyna by the spectrophotometric method

    Directory of Open Access Journals (Sweden)

    Mihajlović Dušanka

    2006-01-01

    Full Text Available The flower and leaf of hawthorn contains many active components, used in the production of pharmaceutical preparations for cardiotonic, anti-hypertonic anti-hypotonic, artherosclerotic, anti-arithmic and anti-anemic groups. According to the ROTTE list (1996, 159 of 1800 pharmaceutical preparations contain components from hawthorn. Due to the remedial action of hyperoside and other flavonoids from hawthorn, their determination is important for the standardization of extract and preparation quality. The extraction of the flavonoids from a mixture of hawthorn (C. oxycantha and C. monogyna flower and leaf was carried out by percolation with 40% and 70% (v/v ethanol. In order to determine the content of total flavonoids calculated as hyperoside spectrophotometric method with aluminium(lll chloride as a colour reagent at 425 nm was applied. The total flavonoid content in the herbal material mixture was 0.483%, in 40% and 70% (v/v ethanolic liquid extract it was 138 mg/100 cm3 and 157 mg/100 cm, respectively. The extraction degree of total flavonoids with 40% and 70% (v/v ethanolic solutions was 57.14% and 65.01% respectively. The yield of total flavonoids in the dry extract was 63% in regard to the herbal mixure content.

  12. Effects of cerous nitrate on growth and tanshinone production in salvia miltiorrhiza hairy roots

    Institute of Scientific and Technical Information of China (English)

    韩名宇; 郭万里; 梁宗锁; 杨东风; 闫希军; 朱永宏; 刘岩

    2015-01-01

    Salvia miltiorrhiza, a popular traditional Chinese medicine, is widely used for treatments in cardiotonic disease. Tanshi-nones are a group of bioactive ingredients in S. miltiorrhiza. In this study, Ce3+was used as an elicitor to enhance tanshinones produc-tion in S. miltiorrhiza hairy roots. The results showed that contents of dihydrotanshinone I (DTI) and cryptotanshinone (CT) were sig-nificantly enhanced by 50μmol/L Ce3+, and reached to 0.875 mg/g and 0.271 mg/g, respectively. However, tanshinone II A (TIIA) and tanshinone I (TI) contents were significantly decreased to 59%and 62%of the control. Simultaneously, expressions of genes (HMGR, DXR, DXS1, DXS2 and GGPPS) involved in tanshinone biosynthesis were upregulated by Ce3+. Responses of DXS1, DXS2 and GGPPS to Ce3+treatments were later than HMGR and DXR. We speculated that branch pathways of DTI and CT biosynthesis were probably different from TIIA and TI. This work will help us understand biosynthetic mechanism of tanshinones in plants.

  13. Ethnobotany and research on medicinal plants in India.

    Science.gov (United States)

    Jain, S K

    1994-01-01

    Vast ethnobotanical knowledge exists in India from ancient time. Since the 1950s the study of ethnobotany has intensified; 10 books and 300 papers have been published. Our work over four decades, both in the field and literary studies, has resulted in a dictionary of Indian folk-medicine and ethnobotany that includes 2532 plants. India has about 45,000 plant species; medicinal properties have been assigned to several thousand. About 2000 figure frequently in the literature; indigenous systems commonly employ 500. Despite early (4500-1500 BC) origins and a long history of usage, in the last two centuries Ayurveda has received little official support and hence less attention from good medical practitioners and researchers. Much work is now being done on the botany, pharmacognosy, chemistry, pharmacology and biotechnology of herbal drugs. The value of ethnomedicine has been realized; work is being done on psychoactive plants, household remedies and plants sold by street drug vendors. Statistical methods are being used to assess the credibility of claims. Some recent work in drug development relates to species of Commiphora (used as a hypolipidaemic agent), Picrorhiza (which is hepatoprotective), Bacopa (used as a brain tonic), Curcuma (antiinflammatory) and Asclepias (cardiotonic). A scrutiny of folk claims found 203 plants for evaluation. Less well known ethnomedicines have been identified that are used to treat intestinal, joint, liver and skin diseases. PMID:7736852

  14. [Secondary metabolites, lethality and antimicrobial activity of extracts from three corals and three marine mollusks from Sucre, Venezuela].

    Science.gov (United States)

    Ordaz, Gabriel; D'Armas, Haydelba; Yáñez, Dayanis; Hernández, Juan; Camacho, Angel

    2010-06-01

    The study of biochemical activity of extracts obtained from marine organisms is gaining interest as some have proved to have efficient health or industrial applications. To evaluate lethality and antimicrobial activities, some chemical tests were performed on crude extracts of the octocorals Eunicea sp., Muricea sp. and Pseudopterogorgia acerosa and the mollusks Pteria colymbus, Phyllonotus pomum and Chicoreus brevifrons, collected in Venezuelan waters. The presence of secondary metabolites like alkaloids, unsaturated sterols and pentacyclic triterpenes in all invertebrates, was evidenced. Additionally, sesquiterpenlactones, saponins, tannins, cyanogenic and cardiotonic glycosides were also detected in some octocoral extracts, suggesting that biosynthesis of these metabolites is typical in this group. From the lethality bioassays, all extracts resulted lethal to Artemia salina (LC50<1000 microg/ml) with an increased of lethal activity with exposition time. P. pomum extract showed the highest lethality rate (LC50=46.8 microg/ml). Compared to the octocorals, mollusks extracts displayed more activity and a greater action spectrum against different bacterial strains, whereas octocorals also inhibited some fungi strains growth. Staphylococcus aureus was the most susceptible to the antimicrobial power of the extracts (66.7%), whereas Pseudomonas aeruginosa, Candida albicans and Aspergillus niger were not affected. The antibiosis shown by marine organisms extracts indicates that some of their biosynthesized metabolites are physiologically active, and may have possible cytotoxic potential or as a source of antibiotic components. PMID:20527468

  15. Repeated and chronic administration of Vardenafil or Sildenafil differentially affects emotional and socio-sexual behavior in mice.

    Science.gov (United States)

    Dadomo, H; Parmigiani, S; Nicolini, Y; Freschini, S; Gioiosa, L; Patrelli, T S; Palanza, P; Volpi, R

    2013-09-15

    Selective phosphodiesterases (PDEs) inhibitors have been widely studied as therapeutic agents for treatment of various human diseases, including cardiotonics, vasodilators, smooth muscle relaxants, antidepressants, antithrombotics, antiasthmatics, and agents for improving learning and memory. Although Sildenafil(®) and Vardenafil(®) have similar chemical formulae, the same target and interact with many of the same residues at the active site of phosphodiesterse-5 (PDE-5), they exhibit both in vitro and in vivo some important functional differences that could differentially affect behavior. Therefore we assessed whether repeated and chronic administration of Vardenafil and Sildenafil at a dose based upon human treatment can differentially affect aggressive, social, emotional and sexual behavior. To this aim, the effects of Sildenafil (10mg/kg) or Vardenafil (2mg/kg) (t.i.w., for 5 weeks) were observed in CD1 subordinate male mice in a low aggression and social subordination context. The results show that Sildenafil increased competitive aggression, environmental and social exploration, and reduced anxiety like behaviors as compared to controls, whereas Vardenafil had a significant major effect on appetitive and consummatory aspect of sexual behavior. This demonstrates that Sildenafil and Vardenafil, although being structurally and functionally similar, are characterized by different neuro-behavioral actions and can have differential therapeutic potentials. PMID:23850358

  16. Analysis of the Inhibitory Effect of Gypenoside on Na+,K+-ATPase in Rats' Heart and Brain and Its Kinetics

    Institute of Scientific and Technical Information of China (English)

    HAN Xiao-yan; WEI Hong-bo; ZHANG Fu-cheng

    2007-01-01

    ObjectiYe: To study the effects of gypenoside (Gyp) on the activity of microsomal Na+,K+-ATPase in rat's heart and brain in vitro. Methods: The microsomal Na+, K+-ATPase was prepared from rat's heart and brain by differential centrifugation. The activity of microsomal Na+, K+-ATPase was assayed by colorimetric technique. Enzyme kinetic analysis method was used to analyze the effect of Gyp on the microsomal Na+, K+-ATPase of rats. Results: Gyp reversibly inhibited the brain and heart's microsomal Na+, K+-ATPase in a concentration-dependent manner, and showed a more potent effect on enzyme in the brain. The IC50 of Gyp for the heart and brain were 58.79± 8.05 mg/L and 52.07 ±6.25 mg/L, respectively. The inhibition was enhanced by lowering the Na+, or K+ concentrations or increasing the ATP concentration. Enzyme kinetic studies indicated that the inhibitory effect of Gyp on the enzyme is like that of competitive antagonist of Na+, the counter-competitive inhibitor for the substrate ATP, and the mixed-type inhibitor for K+. Conclusion: Gyp displays its cardiotonic and central inhibitory effects by way of inhibiting heart and brain's microsomal Na+, K+-ATPase activities in rats.

  17. Study on diuretic activity of saffron (stigma of Crocus sativus L. Aqueous extract in rat

    Directory of Open Access Journals (Sweden)

    Nabi Shariatifar

    2014-01-01

    Full Text Available Saffron is the most expensive spice in the world and consists of the dried stigmas of Crocus sativus L. It is used as food coloring and flavoring in food industry and traditional cooking and also in folk medicine as antispasmodic, carminative, stomachic, expectorant, aphrodisiac and cardiotonic. The present study has evaluated the diuretic activity of aqueous extract of dried saffron (stigma of Crocussativus in rat. Aqueous extracts of saffron were administered to experimental rats orally as doses of 60, 120 and 240 mg/kg body weight (BW and compared with hydrochlorothiazide (10 mg/kg B.W., intraperitoneally, a potent diuretic as positive control and normal saline solution as placebo for control group. The measured parameters for diuretic activity were total urine volume, urine electrolytes concentration such as sodium and potassium, creatinine and urea concentration. The treated rats with aqueous extract of saffron as doses of 120 and 240 mg/kg BW showed higher urine output when compared to the control group. Also, it has shown a significant dose-dependent increase in the excretion of electrolytes when compared to the control group. Our findings proved the diuretic activity of saffron which is used in traditional medicine, it can be an effective and safe strategy for related dysfunction. Also further studies are needed to identify the mechanisms of action, probably other effects and interactions with other medicines.

  18. PRELIMINARY PHARMACOGNOSTICAL AND PHYTOCHEMICAL EVALUATION OF ARGYREIA NERVOSA LEAF

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    A. Krishnaveni

    2011-02-01

    Full Text Available Traditionally used by the tribal of Rajasthan to prevent conception. Roots are used as appetizer, aphrodisiac, brain tonic, cardiotonic and to treat insanity and synovitis. Leaves, seeds preparations are used to treat epilepsy, diarrhea and nootropic. Leaf materials were collected, dried and coarsely powdered and were subjected to physiochemical constants, behavioral characters of the leaf powder with chemical reagents. Pharmacognostical studies include macroscopical, microscopical observations. Physical chemical constants such as ash values, extractive values, loss on drying, foreign organic matter were determined. Ash values include total ash; acid insoluble and water soluble ash were observed. Extractive values of powder with solvents such as petroleum ether, chloroform, ethyl actetae, ethanol and water were determined. Macroscopical characters help in identifying the leaf. Anatomical observations showed the presence of trichomes, upper and lower epidermal cells with rubiaceous stomata. Sclerenchyma fibers and acicular crystal were observed. The percentage of total ash values (4.3, 1.6 and3.94 % yield of petroleum ether, ethyl acetate, chloroform, ethanol and water showed 3.16,6.4,5.8,10.2 and 7.6% respectively. Preliminary phytochemical screening reported the presence of alkaloids, tannins, phenolic compounds, glycosides and flavanoids.The reported phytoconstitutents of the plant Argyreia nervosa may be responsible for the pharmacological activities. The results obtained add credit to the existing traditional information which will further increase the usage of this plant and provokes towards the investigation of the plant.

  19. FERONIA LIMONIA – A PATH LESS TRAVELLED

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    Qureshi Absar A.

    2010-09-01

    Full Text Available From ancient days to recent civilization, human beings depend on nature for running their life smoothly from day to day. Plants remain a vital source of drugs and now a day’s much emphasis have been given to nutraceuticals. Feronia limonia belonging to family Rutaceae is well known in Indian traditional systems for its traditional uses. Various parts of the plant have astringent, constipating, tonic for liver and lung, diuretic, carminative, and cardiotonic traditional uses. Various important phytoconstituents like alkaloids, phenolic compounds, triterpenoids, coumarins, tannins, steroids etc. have been isolated from Kavith. But only few pharmacological activities like antimicrobial, antiviral, antitumour, antifungal and CNS depressant activity have been scientifically reported. From enormous traditional uses documented in various traditional system of medicine and presence of vital phytoconstituents make Kavith (Feronia limonia an important plant to be studied scientifically to prove various traditional uses. In present review we explore Kaitha’s description, traditional medicinal uses, phytoconstituents and investigated pharmacological activities in various parts of the plant to show potential ethnopharmacological importance of the plant. So that this review can serve as ready to use material for further research on the plant.

  20. Preliminary phytochemical analysis of Cupata (Strychnos schultesiana krukoff) stems and seeds

    International Nuclear Information System (INIS)

    In order to improve the knowledge of Colombian flora, particularly that belonging to the llanos orientales region, Strychnos schultesiana Krukoff was chosen for a chemical composition in-depth study to establish a potential utility in medicinal or industrial fields. For this analysis, a preliminary phytochemical study of three organs of the plant -steams, seeds and leafs- was made; the purpose was to find the main secondary metabolites associated with biological activities: alkaloids, flavonoids, tannins, saponins, antracenic derivates, steroids, coumarins, cardiotonic glycosides and terpenic lactones. The main compounds were alkaloids. This fact was expected, as this species belongs to the genus Strhychnos, widely known because of its high alkaloid content. In addition, the existence of flavonoids in the studied organs of the plant is very remarkable. These compounds are well known as scavengers, useful in prevention of diseases related with oxidative processes. Finally, the results of this work are very useful as a first approach to the knowledge and utility of the vegetal species found in this location. Furthermore, this plant has big agronomical advantages related with the culture establishment, which improves the rational use of natural resources in our country, as a means of regional and national development.

  1. Antivenom potential of ethanolic extract of Cordia macleodii bark against Naja venom

    Institute of Scientific and Technical Information of China (English)

    Pranay Soni; Surendra H. Bodakhe

    2014-01-01

    Objective: To evaluate the antivenom potential of ethanolic extract of bark of Cordia macleodii against Naja venom induced pharmacological effects such as lethality, hemorrhagic lesion, necrotizing lesion, edema, cardiotoxicity and neurotoxicity.Methods:Wistar strain rats were challenged with Naja venom and treated with the ethanolic extract of Cordia macleodii bark. The effectiveness of the extract to neutralize the lethalities ofNaja venom was investigated as recommended by WHO. Results: At the dose of 400 and 800 mg/kg ethanolic extract of Cordia macleodii bark significantly inhibited the Naja venom induced lethality, hemorrhagic lesion, necrotizing lesion and edema in rats. Ethanolic extract of Cordia macleodii bark was effective in neutralizing the coagulant and defibrinogenating activity of Naja venom. The cardiotoxic effects in isolated frog heart and neurotoxic activity studies on frog rectus abdominus muscle were also antagonized by ethanolic extract of Cordia macleodii bark.Conclusions:It is concluded that the protective effect of extract of Cordia macleodii against Naja venom poisoning may be mediated by the cardiotonic, proteolysin neutralization, anti-inflammatory, antiserotonic and antihistaminic activity. It is possible that the protective effect may also be due to precipitation of active venom constituents.

  2. Cardioprotective properties of Crataegus oxycantha extract against ischemia-reperfusion injury

    Science.gov (United States)

    Swaminathan, Jayachandran Kesavan; Khan, Mahmood; Mohan, Iyappu K; Selvendiran, Karuppaiyah; Devaraj, S. Niranjali; Rivera, Brian K.; Kuppusamy, Periannan

    2010-01-01

    The aim of the study was to investigate the cardioprotective effect and mechanism of Crataegus oxycantha (COC) extract, a well-known natural antioxidant-based cardiotonic, against ischemia/reperfusion (I/R) injury. Electron paramagnetic resonance studies showed that COC extract was capable of scavenging superoxide, hydroxyl, and peroxyl radicals, in vitro. The cardioprotective efficacy of the extract was studied in a crystalloid perfused heart model of I/R injury. Hearts were subjected to 30 min of global ischemia followed by 45 min of reperfusion. During reperfusion, COC extract was infused at a dose rate of 1 mg/ml/min for 10 min. Hearts treated with COC extract showed a significant recovery in cardiac contractile function, reduction in infarct size, and decrease in creatine kinase and lactate dehydrogenase activities. The expressions of xanthine oxidase and NADPH oxidase were significantly reduced in the treated group. A significant upregulation of the anti-apoptotic proteins Bcl-2 and Hsp70 with simultaneous downregulation of the pro-apoptotic proteins cytochrome c and cleaved caspase-3 was observed. The molecular signaling cascade including phospho-Akt (ser-473) and HIF-1α that lead to the activation or suppression of apoptotic pathway also showed a significant protective role in the treatment group. No significant change in phospho-p38 levels was observed. The results suggested that the COC extract may reduce the oxidative stress in the reperfused myocardium, and play a significant role in the inhibition of apoptotic pathways leading to cardioprotection. PMID:20171068

  3. Capillary electrophoretic analysis of flavonoids in single-styled hawthorn (Crataegus monogyna Jacq.) ethanolic extracts.

    Science.gov (United States)

    Urbonaviciūte, A; Jakstas, V; Kornysova, O; Janulis, V; Maruska, A

    2006-04-21

    Flavonoids are an important group of natural compounds, which can prevent coronary heart disease and have antioxidant properties. Hawthorn is a well known and widely used medicinal plant due to its cardiotonic activity. Previous studies refer mostly to the HPLC analysis of the flavonoids: vitexin, quercetin, hyperoside, oligomeric procyanidins, which appear to be primarily responsible for the cardiac action of the plant. Aqueous ethanolic extracts of single-styled hawthorn (Crataegus monogyna Jacq., f.: Rosaceae Juss.) leaves and sprouts were analyzed by means of capillary zone electrophoresis (CZE). Influence of vegetation period on the extract qualitative composition and flavonoids quantities was evaluated. Sample preparation by extraction using different concentration of aqueous ethanol (40-96%, v/v) and the influence of extractant composition on the recovery of flavonoids are discussed in detail. The results obtained using CZE are compared to the results of spectrophotometric and HPLC analysis of the extracts. The effect of storage conditions of extracts (solar irradiation, temperature and duration) on degradation of flavonoids was investigated. PMID:16443232

  4. A review on phytochemical, ethnomedical and pharmacological studies on genus Sophora, Fabaceae

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    Panthati Murali Krishna

    2012-10-01

    Full Text Available Sophora is a genus of the Fabaceae family, contains about 52 species, nineteen varieties, and seven forms that are widely distributed in Asia, Oceanica, and the Pacific islands, in the family Fabaceae of herbaceous (Sophora flavescens Aiton to trees (Sophora japonica L.. More than fifteen species in this genus have a long history of use in traditional Chinese medicines. In the last decades the use of this genus in traditional Chinese drugs has led to rapid increase in the information available on active components and reported to posses various pharmacological/therapeutic properties. The paper reviews the ethnopharmacology, the biological activities and the correlated chemical compounds of genus Sophora, Fabaceae. More than 300 compounds has been isolated, among them major are quinolizidine alkaloids particularly matrine and oxymatrine and flavonoids particularly prenylated and isoprenylated flavonoids. Modern pharmacological studies and clinical studies demonstrated that these chemical constituens possess wide reaching pharmacological actions like anti oxidant, anticancer, anti-asthamatic, anti-neoplastic, antimicrobial, antiviral, antidote, anti pyretic, cardiotonic, antinflammatory, diuretic and in the treatment of skin diseases like eczema, colitis and psoriasis.

  5. Antimicrobial, Anti-Inflammatory, Antiparasitic, and Cytotoxic Activities of Laennecia confusa

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    María G. Martínez Ruiz

    2012-01-01

    Full Text Available The current paper investigated the potential benefit of the traditional Mexican medicinal plant Laennecia confusa (Cronquist G. L. Nesom (Asteraceae. Fractions from the hexane, chloroform, methanol, and aqueous extracts were analyzed for antibacterial, antifungal, anti-inflammatory, and antiparasitic activities. The antimicrobial activity of the extracts and fractions was assessed on bacterial and fungal strains, in addition to the protozoa Leishmania donovani, using a microdilution assay. The propensity of the plant's compounds to produce adverse effects on human health was also evaluated using propidium iodine to identify damage to human macrophages. The anti-inflammatory activity of the extracts and fractions was investigated by measuring the secretion of interleukin-6. Chemical analyses demonstrated the presence of flavonoids, cyanogenic and cardiotonic glycosides, saponins, sesquiterpene lactones, and triterpenes in the chloroform extract. A number of extracts and fractions show antibacterial activity. Of particular interest is antibacterial activity against Staphylococcus aureus and its relative methicillin-resistant strain, MRSA. Hexanic and chloroformic fractions also exhibit antifungal activity and two extracts and the fraction CE 2 antiparasitic activity against Leishmania donovani. All bioactive extracts and fractions assayed were also found to be cytotoxic to macrophages. In addition, the hexane and methane extracts show anti-inflammatory activity by suppressing the secretion of interleukine-6.

  6. Red maca (Lepidium meyenii reduced prostate size in rats

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    Rubio Julio

    2005-01-01

    Full Text Available Abstract Background Epidemiological studies have found that consumption of cruciferous vegetables is associated with a reduced risk of prostate cancer. This effect seems to be due to aromatic glucosinolate content. Glucosinolates are known for have both antiproliferative and proapoptotic actions. Maca is a cruciferous cultivated in the highlands of Peru. The absolute content of glucosinolates in Maca hypocotyls is relatively higher than that reported in other cruciferous crops. Therefore, Maca may have proapoptotic and anti-proliferative effects in the prostate. Methods Male rats treated with or without aqueous extracts of three ecotypes of Maca (Yellow, Black and Red were analyzed to determine the effect on ventral prostate weight, epithelial height and duct luminal area. Effects on serum testosterone (T and estradiol (E2 levels were also assessed. Besides, the effect of Red Maca on prostate was analyzed in rats treated with testosterone enanthate (TE. Results Red Maca but neither Yellow nor Black Maca reduced significantly ventral prostate size in rats. Serum T or E2 levels were not affected by any of the ecotypes of Maca assessed. Red Maca also prevented the prostate weight increase induced by TE treatment. Red Maca administered for 42 days reduced ventral prostatic epithelial height. TE increased ventral prostatic epithelial height and duct luminal area. These increases by TE were reduced after treatment with Red Maca for 42 days. Histology pictures in rats treated with Red Maca plus TE were similar to controls. Phytochemical screening showed that aqueous extract of Red Maca has alkaloids, steroids, tannins, saponins, and cardiotonic glycosides. The IR spectra of the three ecotypes of Maca in 3800-650 cm (-1 region had 7 peaks representing 7 functional chemical groups. Highest peak values were observed for Red Maca, intermediate values for Yellow Maca and low values for Black Maca. These functional groups correspond among others to benzyl

  7. Chemical Composition and Antioxidant Activity of the Extract and Essential oil of Rosa damascena from Iran, Population of Guilan

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    N Yassa

    2009-10-01

    Full Text Available "nBackground and the purpose of study: Rosa damascena Mill. (Rosaceae has cooling, soothing, astringent, and anti-inflammatory effects, and has been used in the north of Iran as a cardiotonic agent. The aim of this study was to identify components of R. damascena (cultivated in Guilan Province extract and essential oil and to study their biological activities. "nMethods: Essential oil of R. damascena was prepared by hydrodistillation and analyzed with GC/MS instrument. The antioxidant activity of hydro-alcohlic extract of petals and essential oil was measured using free radical scavenging activity with 2-2-diphenyl, 1-picrylhydrazyl (DPPH and lipid peroxidation (ferric ammonium thiocyanate methods. "nResults: Hydro-alcoholic extract showed strong free radical scavenging capacity compared to lipid peroxidation inhibitory effects. IC50 values of the extract were 2.24 μg/mL and 520 μg/mL in free radical scavenging and lipid peroxidation assays, respectively. The major components of essential oil were linalool (3.8%, nerol (3.05%, geraniol (15.05%, 1-nonadecene (18.56%, n-tricosane (16.68%, hexatriacontane (24.6% and n-pentacosane (3.37%. The bioassay-guided fractionation of extract led to the isolation of three flavonol glycosides: quercetin-3-O-glucoside, kaempferol-3-O-rhamnoside and kaempferol-3-O-arabinoside. The IC 50 value of the radical scavenging activity of kaempferol-3-O-rhamnoside which was, 530 μg/mL was weaker than the extract. "nMajor conclusion: The petal of this cultivated rose has no bitter taste and because of its potential antioxidant activity and good taste, can be used as food flavor and a preventing agent for many diseases.

  8. A Chinese Herbal Preparation Containing Radix Salviae Miltiorrhizae, Radix Notoginseng and Borneolum Syntheticum Reduces Circulating Adhesion Molecules

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    Kylie A. O’Brien

    2011-01-01

    Full Text Available Circulating adhesion molecules (CAMs, surface proteins expressed in the vascular endothelium, have emerged as risk factors for cardiovascular disease (CVD. CAMs are involved in intercellular communication that are believed to play a role in atherosclerosis. A Chinese medicine, the “Dantonic Pill” (DP (also known as the “Cardiotonic Pill”, containing three Chinese herbal material medica, Radix Salviae Miltiorrhizae, Radix Notoginseng and Borneolum Syntheticum, has been used in China for the prevention and management of CVD. Previous laboratory and animal studies have suggested that this preparation reduces both atherogenesis and adhesion molecule expression. A parallel double blind randomized placebo-controlled study was conducted to assess the effects of the DP on three species of CAM (intercellular cell adhesion molecule-1 (ICAM-1, vascular cell adhesion molecule-1 and endothelial cell selectin (E-selectin in participants with mild-moderate hypercholesterolemia. Secondary endpoints included biochemical and hematological variables and clinical effects. Forty participants were randomized to either treatment or control for 12 weeks. Treatment with DP was associated with a statistically significant decrease in ICAM-1 (9% decrease, P = .03 and E-Selectin (15% decrease, P = .004. There was no significant change in renal function tests, liver function tests, glucose, lipids or C-reactive protein levels and clinical adverse effects did not differ between the active and the control groups. There were no relevant changes in participants receiving placebo. These results suggest that this herbal medicine may contribute to the development of a novel approach to cardiovascular risk reduction.

  9. Natriuretic Hormones, Endogenous Ouabain, and Related Sodium Transport Inhibitors

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    John eHamlyn

    2014-12-01

    Full Text Available The work of deWardener and colleagues stimulated longstanding interest in natriuretic hormones (NH. In addition to the atrial peptides (APs, the circulation contains unidentified physiologically-relevant NHs. One NH is controlled by the central nervous system (CNS and likely secreted by the pituitary. Its circulating activity is modulated by salt intake and the prevailing sodium concentration of the blood and intracerebroventricular fluid, and contributes to postprandial and dehydration natriuresis. The other NH, mobilized by atrial stretch, promotes natriuresis by increasing the production of intrarenal dopamine and/or nitric oxide. Both NHs have short (<35 minutes circulating half lives, depress renotubular sodium transport, and neither requires the renal nerves. The search for NHs led to endogenous cardiotonic steroids (CTS including ouabain-, digoxin-, and bufadienolide-like materials. These CTS, given acutely in high nanomole to micromole amounts into the general or renal circulations, inhibit sodium pumps and are natriuretic. Among these CTS, only bufalin is cleared sufficiently rapidly to qualify for an NH-like role. Ouabain-like CTS are cleared slowly, and when given chronically in low daily nanomole amounts, promote sodium retention, augment arterial myogenic tone, reduce renal blood flow and glomerular filtration, suppress nitric oxide in the renal vasa recta, and increase sympathetic nerve activity and blood pressure. Moreover, lowering total body sodium raises circulating endogenous ouabain. Thus, ouabain-like CTS have physiological actions that, like aldosterone, support renal sodium retention and blood pressure. In conclusion, the mammalian circulation contains two non-AP NHs. Identification of the CNS NH should be a priority.

  10. Quantitative analysis of some volatile components in Mimusops elengi L.

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    Chantana Aromdee

    2009-08-01

    Full Text Available Dried pikul flower (Mimusops elengi L., Sapotaceae is used in many recipes of Thai traditional medicine i.e. cardiotonic and stomachic. In this study, fresh and dried pikul flowers were investigated. The odour of pikul flower, even when it was dried, is very strong and characteristic. The constituents of volatile oils in fresh and dried pikul flowers extracted by ether were analysed by gas chromatography-mass spectrometry. 2-Phenylethanol, 4-hydroxybenzenemethanol and cinnamyl alcohol were mainly found in fresh flower, 10.49, 8.69 and 6.17%, respectively. Whereas those mainly found in dried flowers were long chain carboxylic acid ester and (Z-9-octadecenoic acid, 5.37 and 4.71% of ether extract, respectively.An analytical method simultaneously determining benzyl alcohol, 2-phenylethanol and methyl paraben was developed by using the GC-FID method. The percent recoveries were 91.66, 104.59 and 105.28%, respectively. The intraday variations(% RSD were 7.22, 6.67 and 1.86%; and the interday variation were 3.12, 2.52 and 3.55%, respectively. Detection limits were 0.005, 0.014 and 0.001 ppm, and quantitation limits were 0.015, 0.048 and 0.003 ppm, respectively. Benzyl alcohol, 2-phenylethanol and methyl paraben content of dried flowers (9 samples from various drug stores in Thailand and one sample from China were 6.40-13.46, 17.57-196.57 and 27.35-355.53 ppm, respectively.

  11. Characterization of the insulin-sensitive low Km cAMP phosphodiesterase from rat adipose tissue

    International Nuclear Information System (INIS)

    Particulate, but not soluble, low K/sub m/ cAMP phosphodiesterase (PDE) activity of rat adipocytes was increased 50-100% during incubation (10 min) of intact cells with 1-3 nM insulin; activation was less with higher or lower insulin concentrations. Activation was maintained during solubilization with an alkyl polyoxyethylene non-ionic detergent C13, E12 and NaBr and chromatography on DEAE. Enzyme from DEAE was further purified by chromatography on Sepahadex G-200 and Blue-Sepharose. Activity (with 0.5 μM [3H]cAMP) was rather sensitive to inhibition by p-chloromercuribenzoate (IC50, 1 μM) and less so by 2,2'-dithiobis-(5-nitropyridine) (160 μM), N-ethylmaleimide (525 μM) and iodoacetamide (750 μM). PDE activity was also rather sensitive to inhibition by cilostamide (IC50, ∼40 nM) and the cardiotonic drugs CI 930 (450 nM) and milrinone (630 nM) but rather insensitive to RO 20-1724 (190 μM). Based on effects of these inhibitors, the hormone-sensitive low K/sub m/ particulate cAMP PDE from rat adipocytes seems to be analogous to the insulin-activated particulate PDE from 3T3-L1 adipocytes and the cilostamide-sensitive soluble low K/sub m/ cAMP PDE from bovine liver (designated as III-C), platelets, heart, and other tissues

  12. Determination the Total Flavonoids from Stem and Leaf of Artabotrys.haimanensis

    Institute of Scientific and Technical Information of China (English)

    BI He-ping; SONG Xiao-Ping; HAN Chang-ri; LI Chuan-bao

    2004-01-01

    The Annonaccac family is a main one of the tropical plants flora and there are totally 127 genus, about 2231 species in the world, wildly distributed in the tropical zone and subtropics areas.China is one of the countries where species of this family are mostly distributed, with 24 genus, 103 species and 6 variant, among which, 45 species and 1 variant are endemic to China. There are about 100 types of plants of Artabotrys genus in the world, among which, 10 species are in China. Scholars from home and abroad have found a series of new substance of biological activities in the plants of Annonaccac family with antimalarial, anti-tumor, anti-leukemia and obvious cardiotonic effects,which has aroused great interest. Plants of Artabotrys genus, Artabotrys Hainanensis are endemic to Hainan, distributed widely in Hainan Island. They have long been used among the ordinary people as medicinal plants with antipyretic, antidotal, antiphlogistic and analgesic effects. The flavonoid is a very important secondary metabolite in plants with many physiological activities such as fat-reduction, antithrombus, antioxidant and blood-sugar-reduction. This paper studies the total flavonoids from stem and leaf of Artabotrys by spectrophotometry. Artabotrys Hainanensis R.E.Fries were collected from Hainan Jianfeng Mountain and were identified. Spectrophotometry was used to determination of the total flavonoids from stem and leaf of Artabotrys. The total flavonoids of Artabotrys were tested with rutin as check sample. By adding aluminium ion agent and controling proper pH, the flavonoids and the aluminium ion were combined into complex compound and the characteristic absorption peak was obtainable in the visible spectrum. The total flavonoids from stem and leaf of Artabotrys were determined to be 2.29% in stem and 6.83% in leaf. The regression equation was Y=0.000786A+0.0058, and the correlation coefficient r=0.9997. This method is easily operated and the result determined is stable and

  13. Smart drug delivery injector microsystem based on pyrotechnical actuation

    Science.gov (United States)

    Puig-Vidal, Manel; Lopez, Jaime; Miribel, Pere; Samitier-Marti, Josep; Rossi, Carole; Berthold, Axel

    2003-04-01

    A smart drug delivery injector microsystem is presented based on small pyrotechnics to impulse drugs to be injected to a human being. The proposal refers to a feasibility demonstration of the technology for pharmaceutical chips. These chips would be around some cm2 in section and will be able to inject a drug into de subject skin responding to an electrical signal. The product derived from this activity will be useful for astronaut's health, being able to administrate emergency doses of products (for instance cardio-tonic or hypoallegic drugs) enough to survive an emergency situation (as it can be a heart attack during EVA). The system can also be used for easy administration of drugs needed for physiological research. The usefulness of the device in terrestrial applications has no doubt, allowing remote administration of drugs to patients whose biomedical parameters are remotely monitored. The concept proposed here is new in combining the idea of pharmaceutical chip with the ultrasonic droplet technology and the use of pyrotechnics to provide energy to the drug to be injected. The proposed Drug Injector Microsystem is based on 2 main blocks:- Micropyrotechnic system: defines the ignition part based on pyrotechnic.- Microfluidic system: defines the drug injection part. This part is also divided in different critical parts: Expansion chamber, membrane or piston, drug reservoir and a needle. Different sensors are placed on the expansion chamber of microfluidic system and on the micropyrotechnic system. A complete electronic module is implemented with a PC interface to define flexible and user friendly experiences showing the smart drug delivery injector microsystem principle.

  14. Determination of pharmaceutical drugs in surface water samples

    International Nuclear Information System (INIS)

    Pharmaceuticals are sometimes eliminated without metabolization by the human organism. Because of this fact they get into sewage treatment plants where they are not fully removed and can therefore reach the aquatic environment. The aim of this dissertation was the development of a method to analyze as many different compounds as possible. The analytes were not only chosen according to the amount consumed in Austria but also according to their stability within the human body and in consequence the stability in the aquatic environment. The problems were the low concentration in which the analytes occur in watercourses (less than one millionth gram per liter). Therefore all investigated water samples had to be preconcentrated and the interfering matrix compounds had to be removed. This preconcentration was done by a so called solid-phase extraction. With the use of this technique the interesting analytes could be bound selectively to the solid adsorption material, whereas the other components were not. After this, the adsorbed pharmaceuticals were eluted from the solid phase with a small volume of solvent and were used for the following analyses. In all investigated watercourses traces of pharmaceuticals were detected, whereby caffeine, antibiotics and also antirheumatic drugs and cardiotonics were the most frequently found. The concentrations occurring in water are in no proportion to the ones consumed if one takes a single tablet in cases of illness. Therefore there is no acute danger for human beings. But it is necessary to make an estimation of the possible long term impact on the aquatic environment and ecosystems for the presence of pharmaceuticals at low concentrations, the data is used. For this case the dissertation provided an important contribution. For this reason comprehensive data must be available; the present dissertation has provided an important contribution to progress in this area. (author)

  15. Pharmaceutical Importance and Synthetic Strategies for Imidazolidine-2-thione and Imidazole-2-thione Derivatives

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    Anuradha K. Gajjar

    2011-01-01

    Full Text Available Imidazole heterocycles containing oxygen or sulfur heteroatoms are of considerable pharmaceutical interest. Many synthetic strategies for imidazolidine-2-thione and imidazole-2-thione derivatives were developed in the past years. They have been well documented by a steadily increasing number of publications and patents. Substituted imidazolidine-2-thiones and imidazole-2-thiones display remarkable biological activities. For instance, imidazole-2-thione has been reported to exhibit antimicrobial, antifungal, antithyroid, antioxidant, cardiotonic, antihypertensive, Dopamine -Hydroxylase (DBH inhibitory and anti-HIV properties. Imidazolidine-2-thione derivatives have been reported to exhibit antimicrobial activity, anti-HIV activity, antifungal activity and so forth. The main purpose of this review is to present a survey of the literature on the different methods of synthesis and reactions involving imidazolidine-2-thione and imidazole-2-thione during the last few decades. This article summarizes an efficient, microwave-assisted method for the liquid-phase combinatorial synthesis of 3,5-disubstituted-thiohydantoin, also reported previously. Synthesis of metal complexes of imidazolidine-2-thione and its derivatives were reported as antimicrobial agents also discussed in the article. Some of the chiral imidazolidine-2-thione N-and C-nucleoside were reported as precursors for the synthesis of azidonucleosides and fluoronucleosides known for their anti-AIDS activity. Metal complexes of heterocyclic thione ligands were reported to possess antifungal activity. Imidazolidine-2-thione and imidazole-2-thione derivatives have found applications in diverse therapeutic areas. Imidazolidine-2-thiones are also used as a chiral auxiliary and ligand for asymmetric catalysis.

  16. Pivotal effects of phosphodiesterase inhibitors on myocyte contractility and viability in normal and ischemic hearts

    Institute of Scientific and Technical Information of China (English)

    Yuan James RAO; Lei XI

    2009-01-01

    Phosphodiesterases (PDEs) are enzymes that degrade cellular cAMP and cGMP and are thus essential for regulating the cyclic nucleotides. At least 11 families of PDEs have been identified, each with a distinctive structure, activity, expression, and tissue distribution. The PDE type-3, -4, and -5 (PDE3, PDE4, PDE5) are localized to specific regions of the cardiomyo-cyte, such as the sarcoplasmic reticulum and Z-disc, where they are likely to influence cAMP/cGMP signaling to the end effectors of contractility. Several PDE inhibitors exhibit remarkable hemodynamic and inotropic properties that may be valuable to clinical practice. In particular, PDE3 inhibitors have potent cardiotonic effects that can be used for short-term inotropic support, especially in situations where adrenergic stimulation is insufficient. Most relevant to this review, PDE in-hibitors have also been found to have cytoprotective effects in the heart. For example, PDE3 inhibitors have been shown to be cardioprotective when given before ischemic attack, whereas PDE5 inhibitors, which include three widely used erectile dysfunction drugs (sildenafil, vardenafil and tadalafil), can induce remarkable cardioprotection when administered either prior to ischemia or upon reperfusion. This article provides an overview of the current laboratory and clinical evidence, as well as the cellular mechanisms by which the inhibitors of PDE3, PDE4 and PDE5 exert their beneficial effects on normal and ischemic hearts. It seems that PDE inhibitors hold great promise as clinically applicable agents that can improve car-diac performance and cell survival under critical situations, such as ischemic heart attack, cardiopulmonary bypass surgery, and heart failure.

  17. Bibliographic Studies on the Bufonis Venenum

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    Kye-Sung Kang

    2001-06-01

    Full Text Available Objectives : Through the literatures on the effets of Bufonis Venenum, we are finding out the clinical possibility and revealing the more effective to intractable diseases. Methods : We investigated the literatures of Oriental Medicine and experimental reports about Bufonis Venenum. Results : 1. Bufonis Venenum is made of bufonidae bufo bufo gargarizans cantor or bufo melanostictus schneider of white serum which secreted from parotid gland or dermato gland, and it is dried for using. 2. In oriental medicine, Bufonis Venenum has been mainly used on the tumors, cacanthrax and dermatic disease, and then it has been clinically used on infantile athrepsia, tetanus, sore throat, toothache, and so on. 3. The pharmacological effects of Bufonis Venenum are cardiotonic, respiration stimulation, depressor or vasopressor, topical anesthcsia, hallucination, striped muscle stimulation, antiasthmatic, antibacterial, antiinflammatory, anticancer, diuretic, immuno effects, etc. 4. Bufonis Venenum is largely divided in ether binding steroid compound, hydroxyl steroid compound, carboxyl or aldehyde steroid compound, indole compound, and adrenaline, cholesterole, etc. 5. Symptoms of Bufonis Venenum poisoning in digestive system are vommitig, abdominal pain, diarrhea, dehydration, in circulatory system are palpitation, shock, bradycardia, in nervous system are vertigo, somnolentia, muscle-tendon reflex weakness, and critical conditions to tissue necrosis and heart attack. 6. Ways to treat Bufonis Venenum poisoning include gastric irrigation with 0.20.5% potassium permanganate fluid and atropine 0.5~1.0mg subcutaneous injection. From the chinese book of Bon Cho Gang Moke(本草綱目, if white serum of Bufonis Venenum enter the eyes, it happens the edema and pain. And then washed the eyes by juice of Lithospermi Radix(紫草 that the edema is removed. Conclusions and Discussion : The results from above literary studies show that prescriptions and Aqua-acupuncture of

  18. The Effect of Non-invasive Ventilation on Plasma Concentration of Brain Natriuretic Peptide, Endothelin-1 and Angiotensin II in Senior Patients with Severe Heart Failure

    International Nuclear Information System (INIS)

    To investigate the curative effects of non-invasive ventilation (NIV) on senior patients with severe heart failure and the influence on plasma brain natriuretic peptide (BNP), endothelin-1 (ET-1) and angiotensin II (Ang II), forty two senior patients with severe heart failure were randomly divided into treatment group and control group. The control group (21 cases) was treated by routine therapy include cardiotonic, diuretics, vasodilatation drugs and supplying oxygen via nasal catheter. The treatment group (21 cases) was treated by NIV combined with routine therapy 3-5 days. The clinical signs, blood pressure, heart rate, respiratory rate, blood-gas analysis (PaO2, SaO2) and left ventricular ejection fraction (LVEF) were observed before and after treatment for 3-5 days. The concentrations of plasma BNP, ET-1 and Ang II were also measured at the beginning and 3-5 days later. The results showed that the clinical symptoms and signs significantly improved; the SaO2, PaO2 and LVEF significantly elevated(P<0.05); RR significantly reduced (P<0.05) in NIV group compared with those in routine therapy group. The plasma levels of BNP, ET-1 and Ang II were significantly decreased after treatment in both groups, especially in the treatment group (P<0.01). The plasma levels of BNP, ET-1 and Ang II had a significantly negative correlation with LVEF (P<0.01). The non-invasive ventilation could significantly improve heart function on senior patients with severe heart failure and has an on neuro-endocrine mechanisms. (authors)

  19. Antinociceptive evaluation of an ethanol extract of Achyranthes aspera (agadha in animal models of Nociception.

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    Bhosale Uma

    2011-04-01

    Full Text Available Achyranthes aspera Linn., known as Chirchira (Hindi, Agadha (Marathi is an indigenous herb found in India. It is the basic composition of many traditional remedies. The herb has been reported to have variety of activities like antifertility, antihyperlipidemic, antidiabetic, immunomodulatory, anticarcinogenic, diuretic and cardiotonic, anti-inflammatory, antifungal and antibacterial activity. Present study was designed to evaluate the antinociceptive activity of ethanolic extract of A. Aspera (EEAA and to find the phytochemical responsible for this activity with possible mode of its activity. The antinociceptive activity of ethanol extract of Achyranthes aspera was investigated in albino mice. The pharmacological assays used were the tail flick, hot plate and the formalin-induced pain tests. The extract was given intraperitoneally at a dose of 400 mg/kg (our earlier study revealed no activity at the dose 200mg/kg. Pentazocine (10mg/kg body weight i.p. was used as standard. Data analyzed by ANOVA test followed by Dunnett’s test. All the results were expressed as Mean (±SEM. P <0.05 was considered significant. For formalin test the percent inhibition was calculated by using formula (C-T/C × 100 (%. Phytochemical screening revealed presence of triterpenoid saponins possessing oleanolic acid as aglycone, viz. A & B, alkaloid achyranthine, water soluble base betaine and steroids. In the tail flick & hot plate test extract treated animals showed significant analgesic activity at 30, 60, 90 and 120min. Extract (400 mg/kg i.p. reduced the formalin induced pain in both phases (i.e. neurogenic and inflammatory by 58.8% and 92.7%, respectively. Ethanol extract of A.Aspera exhibit central as well as peripheral antinociceptive activity.Keywords: Achyranthes aspera Formalin Hot plate Tail flick.

  20. Repair of complete atrioventricular septal defect in infants with down syndrome: outcomes and long-term results.

    Science.gov (United States)

    Tumanyan, Margarita R; Filaretova, Olga V; Chechneva, Vera V; Gulasaryan, Ruben S; Butrim, Iuliia V; Bockeria, Leo A

    2015-01-01

    In clinical practice, the combination of congenital heart disease (CHD) with malformations of other organs occurs in about 10 % of cases, including chromosomal disease with heart defects, which are observed mainly with certain syndromes. In the Bakoulev SCCS (Moscow, Russian Federation), from 01.2005 to 01.2011, complete atrioventricular septal defect (CAVSD) repair was performed on 163 patients (5.6 ± 3.0 months) with Down Syndrome (DS) using the single-patch (n = 40) and the two-patch (n = 123) methods. The control group consisted of 214 infants aged 6.49 ± 3.03 months with CAVSD and normal karyotype. A retrospective cohort study was made, as well as a comparative analysis of the immediate (up to 30 days) and long-term (12-75 months, at the average of 56 ± 15) results of the repair of CAVSD in infants with DSand normal karyotype/chromosome set (NK). During the hospital treatment period, we registered the following complications: pulmonary hypertensive crises in 6 % (n = 9) of patients with DS and in 10 % (n = 21) of infants with NK, infectious complications in 21% (n = 34) of patients with DS and in 8% (n = 17) of infants with NK. Squeal structures in groups were differentiated. The doses and duration of cardiotonic support in the NK patients were significantly higher in comparison with the DS patients (7.5 ± 2.1 days vs 3.4 ± 1.15 days, p Down syndrome. Concerning the long-term results, there was no significant difference (Gehan-Wilcoxon test) in actuarial freedom from reoperation after repair of CAVSD between DS and NK groups (p Down Syndrome in patients significantly increases the risk of severe co-morbidities that have a significant impact on the recovery period, as well as on life expectancy even after successful CHD correction. PMID:25099029

  1. Importance of the Voltage Dependence of Cardiac Na/K ATPase Isozymes.

    Science.gov (United States)

    Stanley, Christopher M; Gagnon, Dominique G; Bernal, Adam; Meyer, Dylan J; Rosenthal, Joshua J; Artigas, Pablo

    2015-11-01

    Cardiac cells express more than one isoform of the Na, K-ATPase (NKA), the heteromeric enzyme that creates the Na(+) and K(+) gradients across the plasmalemma. Cardiac isozymes contain one catalytic α-subunit isoform (α1, α2, or α3) associated with an auxiliary β-subunit isoform (β1 or β2). Past studies using biochemical approaches have revealed minor kinetic differences between isozymes formed by different α-β isoform combinations; these results make it difficult to understand the physiological requirement for multiple isoforms. In intact cells, however, NKA enzymes operate in a more complex environment, which includes a substantial transmembrane potential. We evaluated the voltage dependence of human cardiac NKA isozymes expressed in Xenopus oocytes, and of native NKA isozymes in rat ventricular myocytes, using normal mammalian physiological concentrations of Na(+)o and K(+)o. We demonstrate that although α1 and α3 pumps are functional at all physiologically relevant voltages, α2β1 pumps and α2β2 pumps are inhibited by ∼75% and ∼95%, respectively, at resting membrane potentials, and only activate appreciably upon depolarization. Furthermore, phospholemman (FXYD1) inhibits pump function without significantly altering the pump's voltage dependence. Our observations provide a simple explanation for the physiological relevance of the α2 subunit (∼20% of total α subunits in rat ventricle): they act as a reserve and are recruited into action for extra pumping during the long-lasting cardiac action potential, where most of the Na(+) entry occurs. This strong voltage dependence of α2 pumps also helps explain how cardiotonic steroids, which block NKA pumps, can be a beneficial treatment for heart failure: by only inhibiting the α2 pumps, they selectively reduce NKA activity during the cardiac action potential, leading to an increase in systolic Ca(2+), due to reduced extrusion through the Na/Ca exchanger, without affecting resting Na(+) and Ca(2

  2. Dissolution Behavior and Content Uniformity of An Improved Tablet Formulation Assayed by Spectrofluorometric and RIA Methods

    Directory of Open Access Journals (Sweden)

    Morteza Rafiee-Tehrani

    1990-06-01

    Full Text Available Digoxin 0.25 mg tablets were manufactured by pregranulation of lactose-fcorn starch with 10% corn starch paste and deposition of solvent on pregranules to make digoxin granules. In the preparation of tablet A, granules of lactose-corn Starch was uniformly moistened with a 5% chloroform-ethanol solution (2:lv/vof digoxin by a simple blending. Tablet B was produced by spray granulation system on which the solvent was sprayed on the granules of lactose-corn starch by utilization of a laboratory size fluidized bed drier (Uniglatt . The content uniformity and dissolution of both tablets were determined by the spectrofluorometric and radio¬immunoassay (RIA method modified for the assay of tablet solutious. One available commercially brand of digoxin tablet (C was included in dissolution study for comparison. For the spectrofluorometric method the technique is based on the fluor-ometric measurenent of the dehydration product of the cardiotonic steroid resulting from its reaction with hydrogen peroxide in concentrated hydrochloric acid. For the RIA method, the filtrate was diluted to theoretical concentration of 2.5 ng/ml."nAliquots of this dilution were then assayed for digoxin content using a commercial digoxin125 I RIA kit. Results from both assay methods were extrapolated to the total tablet content and compared with the labeled amount of 20 individual tablets. All tablet assay results were within the USP standards for the content uniformity and"ndissolution of individual. The individual tablet deviations from labeled amount by RIA method were smaller when compared with the spectrofluorometric method.There was no significant difference between the release of digoxin from three products, and thus it is suggested that the Procedure B could be easily applied for manufacturing"nof digoxin tablets in industrial scales.It was also concluded that,the RIA method could be used for the digoxin tablet determination.

  3. Quantitative estimation of phenolic and flavonoid content and antioxidant activity of various extracts of different parts of Plumbago zeylanica Linn

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    Sharma Ira

    2014-06-01

    Full Text Available Plumbagozeylanica (Chitrak is used as medicinal plant in India. The root of the plant and its constituents are credited with potential therapeutic properties including anti-atherogenic,cardiotonic, hepatoprotective and neuroprotective properties. In recent times, interest hasfocused on phytochemicals as new sources of natural antioxidants. Therefore in the present study methanolic crude extracts of stem, leaves, roots of Plumbagozeylanica were screened for their antioxidant property, phenolic content and flavonoid content. Free radical scavenging activity (antioxidant activity was evaluated using 1, 1-diphenyl-2-picryl- hydrazyl (DPPH and was measured as decolorizing activity followed by the trapping of the unpaired electron of DPPH. The plant roots extract reveled significant antioxidant activity as compared to standard flavonoid (quercetin. IC50 values were found to be 72.3μg/ml , 32.433μg/ml and 24.6μg/ml in stem, leaf and root extracts respectively for their antioxidant activity by DPPH assay. The phytochemical investigation showed presence of flavonoids, and phenolics. The total phenolic and total flavonoid content was found to be the maximum in leaf extracts (28.25±0.001 mg of GAE/g and 2.41±0.021 CE/g respectively. A weak linear correlation between total phenolic or flavonoid content and antioxidant activity was found (correlation coefficient, R2 =0.9989 and R2 = 0.9559, respectively. The findings indicated promising antioxidant activity of crude extracts of the plant and needs further exploration for their effective use in both modern and traditional system of medicines.

  4. MODULATION OF Na + /K + , Mg 2 + and Ca 2+ ATPase ACTIVITY IN DIFFERENT REGIONS OF RAT BRAIN DURING ROTENONE INDUCED PARKINSON'S DISEASE AND PROTECTIVE ROLE OF BACOPA MONNIERI

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    Gunduluru Swathi

    2013-02-01

    Full Text Available Bacopa monnieri(BM; Family: Scrophulariaceae, also referred as Brahmi or Jalbrahmi has been used for centuries in Ayurvedic system of medicine as a brain tonic, memory enhancer, revitaliser of sensory organs, anti-anxiety, cardio-tonic, diuretic, antidepressant and anticonvulsant agent, and the pharmacological actions are mainly attributed to the saponin compounds present in the alcoholic extract of the plant. The present study was carried out with a specific aim to examine the neuroprotective effect of Bacopa monnieriduring Rotenone (RT induced Parkinson’s disease (PD with particular reference to Na+/K+, Mg2+and Ca2+-ATPase activities in different regions of rat brain. In the experiment conducted rats were divided into four groups of six in each group, group 1 received Salinewater (1 ml/kg, group 2 received RT (2.5 mg/kg through i.p. route administration for 60 days to induce PD. The third group received BM extract (180 mg/kg/day for 20 days orally before induction of PD and group 4 received Levodopa (LD (10 mg/kg/day orally which is referred as drug control. The levels of Na+/K+, Mg2+and Ca2+-ATPase activities were measured. Na+/K+, Mg2+and Ca2+-ATPase activities were significantly depleted in different brain regions of rat during RT induced PD when compared to control rats. Treatment with BM and LD caused significant elevation in the activity levels of Na+/K+, Mg2+and Ca2+-ATPase in different brain regions of rats when compared to induced PD rats. Our results suggest the ability of BM extract to modulate Na+/K+, Mg2+and Ca2+- ATPase activities in different brain regions of RT induced rodent model of PD and thus offers effective management in the treatment of PD.

  5. NEUROTROPIC AND DIURETIC ACTIVITY OF THICK EXTRACT OF THE BLOOD-RED HAWTHORN’S FRUITS

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    V. A. Kurkin

    2015-01-01

    Full Text Available Blood-red hawthorn (Crataegi fructus are a popular cardiotonic herbal materials, which widely used in medical practice in our country and abroad. In order to prevent diseases of the cardiovascular system is appropriate to prescribe herbal medicines, because they combine the breadth and softness of therapeutic action, along with the absence of a significant number of side effects and contraindications.The purpose was to study diuretic and antidepressant activity of thick fruit extract of blood-red hawthorn.Material and methods. Under laboratory conditions we obtained a thick extract of blood-red hawthorn fruits. This phytopharmaceutical was studied by us for any diuretic and antidepressant activity. Investiga- tions were carried out on white rats of both sexes weighing 200–220 g. Each experimental group consist- ed of ten animals. Study drug was administered intragastrically by stomach tube. Control in both cases served as purified water. For determination of diuretic activity, we used a thick extract of hawthorn fruits in a dose of 20 mg/kg against the background of the water load in the amount of 3% of body weight of the animal. Reference preparation was chosen dichlorthiazid 20 mg/kg. It was administered once. After ad- ministration the animals were placed in metabolic cages for urine collection for 24 hours. The study de- termined diuresis, natriuresis, kaliuresis, and kreatininuresis for 4 h and 24 h of the experiment. On the day of the experiment the animals of the control group was administered water load of 3%, and experi- enced – intragastrically drug in an identical amount. Animals were placed in a metabolic cage for a day. Collected 4 h and 24-h urine sample. Determined by renal excretion of water was recorded concentration of sodium and potassium by flame photometry in the fiery liquid analyzer PAG-1, creatinine – colorimet- ric method for photocolorimeter CFC-3. For determining antidepressant activity we used a thick hawthorn

  6. The Research of Antioxidant Activity of the Endemic Species of Onopordum Anatolicum

    Directory of Open Access Journals (Sweden)

    G. TAŞDELEN

    2014-06-01

    Full Text Available As is the case elsewhere in the world, Turkish people have long utilized plants as remedies, food, fuel, and dye, as well as for furniture, ornamentation, agricultural tools, and construction materials. Onopordum is a valuable medicinal plant that is widely used in traditional medicine in Europe. The application of Onopordum as food is limited and its main importance is due to medicine utilization. Because of having flavonoid compositions, Onopordum is an important plant. The Genus Onopordum L. (Asteraceae includes about 38 species. The representatives of the genus are native to Europe, Northern Africa, the Canary Island, the Caucasus, Southwest and Central Asia. In Turkey, this genus is represented with 20 species, 6 of which are endemic. Onopordum (cotton thistle, also known as Scots or Scotch thistle species are biennials herbaceous plants with branched, spinose winged stems. They have application in medical practice as a bactericide, cardiotonic, and hemostatic agent and are used against hypotonicity. In this study antioxidant activities of ethanol, methanol, acetone and benzen extracts of some endemic Onopordum anatolicum (Boiss. Boiss. & Heldr. ex Eig seeds which are in Denizli were examined. DPPH and β-carotene-Linoleic acid methods were used in order to determinethe antioxidant activity. The highest antioxidant activity (77% was seenin the extract which is obtained by using methanol catalyst. The lowest activity of antioxidant of the extracts is acetone (5%. In terms of impact, the strenght of antioxidant depends on the phenolic amount of it. For that purpose, O. anatolicum total fenolic content was calculated in terms of mg/ml gallic acid in the experiment performed by using Folin-Ciocaltaeu medhod. According to these values, the highest amount of phenolic compounds are in methanol and the lowest amount of phenolic compounds are in benzen. According to the results of the experiment performed by using DPPH method, it is obvious that the

  7. Identificação de espécies da família Asteraceae, revisão sobre usos e triagem fitoquímica do gênero Eremanthus da Reserva Boqueirão, Ingaí-MG Asteraceae species identification, use revision and phytochemical screening of Eremanthus genus in Boqueirão Ecological Reserve, Ingaí - Minas Gerais State, Brazil

    Directory of Open Access Journals (Sweden)

    A.O. Ribeiro

    2010-12-01

    humans. The phytochemical screening of the hydroalcoholic extracts indicated the presence of reducing sugars, carbohydrates, amino acids, tannins, flavonoids, glycosides cardiotonics, carotenoids, steroids and triterpenoids, depsides and depsidones, coumarin derivatives, soapy saponins, alkaloids, purines, polysaccharides and anthraquinones. On the other hand, organic acids, catechins, sesquiterpene lactones and azulenes were not detected.

  8. Clinical efficacy observation of nitroglycerin,dopamine and dobutamine pumped by micro-Injection pump in the treatment of refractory heart failure%微量注射泵泵入硝酸甘油、多巴胺、多巴酚丁胺治疗难治性心力衰竭的临床效果观察

    Institute of Scientific and Technical Information of China (English)

    夏清德; 王军香; 陈育山; 毛润芝; 蒋均仕

    2015-01-01

    目的:观察应用微量注射泵泵入硝酸甘油、多巴胺、多巴酚丁胺治疗难治性心力衰竭的临床疗效。方法选择2011年1月~2014年1月本院102例心功能Ⅲ~Ⅳ级(NYHA分级法)的住院患者,在卧床休息、控制饮食、吸氧、强心剂及利尿剂治疗的基础上,应用微量注射泵泵入硝酸甘油、多巴胺、多巴酚丁胺,疗程3~5d,观察患者临床症状、体征、心功能改善情况。结果102例患者用药后临床症状和心功能各项参数均明显改善,与治疗前比较,差异有统计学意义(P<0.05)。结论应用微量泵泵入硝酸甘油、多巴胺、多巴酚丁胺治疗难治性心力衰竭患者疗效明显,安全可靠。%Objective To observe the clinical efficacy of nitroglycerin,dopamine and dobutamine pumped by micro-in-jection pump for the treatment of refractory heart failure. Methods 102 hospitalized patients with Grade Ⅲ to Ⅳ(NY-HA grading method) heart function in our hospital from January 2011 to January 2014 were selected and given nitro-glycerin, dopamine and dobutamine pumped by micro-injection pump on the basis of bed rest,diet control,oxygen up-take,cardiotonic and diuretic therapy.The course of treatment was 3 to 5 days.The patients’ clinical symptoms,body signs and cardiac function improvement situation were observed. Results All 102 patients’ clinical symptoms and car-diac function parameters improved significantly after medication.Compared with before treatment,the difference was sta-tistically significant (P<0.05). Conclusion Nitroglycerin,dopamine and dobutamine pumped by micro-injection pump is significantly effective,safe and reliable for the treatment of refractory heart failure.

  9. Effect of two volume responsiveness evaluation methods on fluid resuscitation and prognosis in septic shock patients

    Institute of Scientific and Technical Information of China (English)

    Xu Qianghong; Yan Jing; Cai Guolong; Chen Jin; Li Li; Hu Caibao

    2014-01-01

    Background Few studies have reported the effect of different volume responsiveness evaluation methods on volume therapy results and prognosis.This study was carried out to investigate the effect of two volume responsiveness evaluation methods,stroke volume variation (SW) and stroke volume changes before and after passive leg raising (PLR-ASV),on fluid resuscitation and prognosis in septic shock patients.Methods Septic shock patients admitted to the Department of Critical Care Medicine of Zhejiang Hospital,China,from March 2011 to March 2013,who were under controlled ventilation and without arrhythmia,were studied.Patients were randomly assigned to the SVV group or the PLR-ASV group.The SVV group used the Pulse Indication Continuous Cardiac Output monitoring of SW,and responsiveness was defined as SW->12%.The PLR-ASV group used ASV before and after PLR as the indicator,and responsiveness was defined as ASV >15%.Six hours after fluid resuscitation,changes in tissue perfusion indicators (lactate,lactate clearance rate,central venous oxygen saturation (SCVO2),base excess (BE)),organ function indicators (white blood cell count,neutrophil percentage,platelet count,total protein,albumin,alanine aminotransferase,total and direct bilirubin,blood urea nitrogen,serum creatinine,serum creatine kinase,oxygenation index),fluid balance (6-and 24-hour fluid input) and the use of cardiotonic drugs (dobutamine),prognostic indicators (the time and rate of achieving early goal-directed therapy (EGDT) standards,duration of mechanical ventilation and intensive care unit stay,and 28-day mortality) were observed.Results Six hours after fluid resuscitation,there were no significant differences in temperature,heart rate,blood pressure,SpO2,organ function indicators,or tissue perfusion indicators between the two groups (P >0.06).The 6-and 24-hour fluid input was slightly less in the SW group than in the PLR-ASV group,but the difference was not statistically significant (P >0

  10. Down 综合征患儿室间隔缺损的手术治疗%Surgical Treatment of Ventricular Septal Defect in Children with Down Syndrome

    Institute of Scientific and Technical Information of China (English)

    吴士强

    2014-01-01

    目的:总结 Down 综合征患儿室间隔缺损的外科治疗经验。方法48例 Down 综合征患儿室间隔缺损在全身麻醉低温体外循环下行一期根治术。术前对于合并肺部感染、心功能不全、肺动脉高压者,给予有效的抗感染、强心及利尿剂、降肺动脉压等治疗;加强静脉营养,提高机体免疫力。术中提高手术技巧,操作轻柔,选择合适的手术切口及修补材料,避免发生传导阻滞等并发症。术后入 CICU,加强呼吸道管理,合理使用呼吸机;合理使用血管活性药物,维持循环系统的稳定;合理使用抗生素,减少肺部感染的发生。结果48例中无1例死亡,并发呼吸机相关性肺炎10例,心律失常2例,气胸1例,心包填塞1例,低心排1例。术后随访6个月至6年,生长发育好,无死亡。结论Down 综合征室间隔缺损患儿应尽早手术,选择适当的手术时机,合理有效的围术期处理,可提高手术成功率,延长患儿寿命。%Objective To summarize the experience with the surgical treatment of ventricular septal defect in children with Down syndrome.Methods Forty-eight children with Down syn-drome underwent one-stage radical operation under general anesthesia during hypothermic car-diopulmonary bypass.Patients with lung infection,heart failure,and pulmonary hypertension were given anti-infection,cardiotonics and diuretics,and anti-pulmonary hypertension,respectively.In addition,intravenous nutrition was strengthened and immunity was improved in all patients.Dur-ing operation,gentle operation technique was carried out and appropriate surgical incision and re-pair material were selected to avoid conduction block and other complications.After operation,pa-tients were admitted to CICU,and respiratory tract management and rational use of breathing ma-chine were strengthened.Moreover,vasoactive drugs and antibiotics were rationally used to main-tain the stability of

  11. 家族性高胆固醇血症并发主动脉瓣上及颈动脉狭窄报告并文献复习%Familial Hypercholesterolemia Complicated with Aortic Valve Stenosis and Carotid Stenosis:A Case Report and Lit-erature Review

    Institute of Scientific and Technical Information of China (English)

    周佳君; 邵森

    2015-01-01

    目的:探讨家族性高胆固醇血症( familial hypercholesterolemia, FH)的临床特点及诊治要点。方法对我院收治的1例FH临床资料进行回顾性分析。结果本例17岁女性,因活动后胸闷、气促5年,加重1个月入院。4岁时皮肤出现黄色瘤,手术治疗后复发。病程中于外院就诊,考虑先天性心脏病及高脂血症,并予降血脂治疗未见明显效果入我院。经查血脂升高,心脏及颈动脉超声检查示主动脉瓣上狭窄及颈动脉狭窄,并结合有黄色瘤病史,确诊为纯合子型FH,给予降血脂、强心、利尿、抗血小板聚集等治疗,病情好转,因拒绝血浆置换治疗,继续上述治疗,随访1年血脂控制不佳,症状反复发作。结论 FH易出现心血管并发症,预后差,早期容易漏诊,早期诊断与治疗是延缓疾病进展的关键。%Objective To explore the clinical characteristics, and key points of diagnosis and treatment of familial hypercholesterolemia ( FH) . Methods Clinical date of one patient with FH in our hospital was retrospectively analyzed, and related literature was reviewed. Results A 17-year-old female patient was admitted for chest distress and shortness of breath after exercise for 5 years and aggravated for 1 month. The patient developed xanthomas at the elbows at the age of 4 and under-went surgery. However, one year later, the xanthomas relapsed. The patient was diagnosed as having congenital heart disease and hyperglycemia before admission to our hospital. Although she had been given by, the patient failed to respond to lipid-low-ering treatment. After transfer to our hospital, her concentration of cholesterol was elevated significantly. The ultrasound ex-amination indicated aortic valve stenosis and carotid stenosis. In addition, her family members were found to have hyperglyce-mia or xanthoma, then the diagnosis of homozygous FH was made. The symptoms were alleviated after the treatment of cardio-tonic, diuretic, lipid

  12. Potential pitfalls in the nuclear medicine imaging: Experimental models to evaluate the effect of natural products on the radiolabeling of blood constituents, bioavailability of radiopharmaceutical and on the survival of Escherichia coli strains submitted to the treatment with stannous ion

    Science.gov (United States)

    Soares, Scheila F.; Brito, Lavínia C.; Souza, Deise E.; Bernardo, Luciana C.; Oliveira, Joelma F.; Bernardo-Filho, Mario

    2006-12-01

    (CA) and liver (all the extracts). The alterations promoted by TC extract could be related to cardiotonic, antidiabetes and renal toxicity. The alteration in liver in EA and CA extracts could be related to its hepatoprotective activities. The extracts (EA, MI, BG) were not capable to interfere in the survival of E. coli. Moreover, these extracts have protected the E. coli against the SnCl 2 action and this fact can be related to the free radical scavenging properties of the chemical compounds of the extracts. In conclusion these findings could be worthwhile to try to understand and to avoid some pitfalls in the nuclear medicine.

  13. BiPAP无创通气辅助治疗左心衰竭的疗效评价%Therapeutic Evaluation of Noninvasive BiPAP Ventilation in Adjunctive Treatment of Acute Left Heart Failure

    Institute of Scientific and Technical Information of China (English)

    邓志辉; 于化鹏

    2011-01-01

    目的 探讨BiPAP无创通气在治疗左心衰竭合并低氧血症中的作用.方法 2008年6月至2010年9月收治的34例急性左心衰竭患者,按随机数字表法分为BiPAP无创通气组18例和常规治疗组16例.2组患者均给予心电监测,持续动脉血气分析,均给予强心、利尿、扩血管等常规药物治疗.常规治疗组选择鼻导管高流量供氧(6 L·min-1),BiPAP无创通气组选择连接BiPAP呼吸机.结果 治疗1、6h后,2组动脉血氧分压(PaO2)、末梢血氧饱和度(SaO2)显著升高,心率、呼吸频率明显降低(均P<0.01);与常规治疗组相比,治疗1、6h后BiPAP无创通气组PaO2、SaO2升高更明显,心率、呼吸频率降低更明显而至正常水平(均P<0.01).治疗1h后BiPAP无创通气组总有效率(88.9%)明显高于常规治疗组(50.0%) (P<0.05);BiPAP无创通气组有2例(11.1%)、常规治疗组有8例(50.0%)病情未见好转予以气管插管转成有创通气,2组气管插管率比较差异有统计学意义(P<0.05).结论 与常规药物治疗比较,BiPAP无创通气治疗更有利于病情缓解,对提高抢救危重心力衰竭患者的成功率有重要价值.%Objective The investigate the adjuvant treatment of acute left heart failure complicated by hypoxemia with noninvasive BiPAP ventilation. Methods Thirty-four patients with a-cute left ventricular failure treated in our hospital from June 2008 to September 2010 were randomly divided into two groups. All patients received ECG monitoring, continuous arterial blood gas analysis and the treatment with cardiotonics, diuretic, vasodilator and other conventional drugs. Control group (n=16) was given high-flow oxygen by nasal catheter(6 L ? min-1) and BiPAP treatment group(n=18) was given oxygen by BiPAP breathing machine. Results Values of PaO2 and SaO2 significantly increased but heart rate and respiratory rate obviously decreased in both groups after treatment for 1 and 6 hours(P<0. 01). Compared with control

  14. Calogênese em Cissus sicyoides L. a partir de segmentos foliares visando à produção de metabólitos in vitro Calluses from Cissus sicyoides L. leaves

    Directory of Open Access Journals (Sweden)

    F.R. Rodrigues

    2010-09-01

    faz-se necessário a adição de 6,0 mg L-1 de BAP ao meio de cultivo. Identificou-se a presença de heterosídeos cardiotônicos em calos de Cissus sicyoides L.Secondary metabolites are essentially produced and extracted from plants grown in the field under influence of seasonal variations. The use of biotechnological techniques is an alternative resource for drug production. Among these techniques, tissue culture through callus genesis is highlighted, since callus growth is desirable to induce somaclonal variation and physiological studies, especially when the presence of secondary metabolites can be related to cell growth. The aim of this work was to establish a protocol for Cissus sicyoides L. callus genesis from leaf segments in order to produce metabolites in vitro. Thus, leaf segments removed from adult plants grown in the field were used as explants. After disinfestation, the material was inoculated into MT medium + 1.0 mg L-1 NAA and kept in a BOD chamber, with controlled temperature and luminosity. After 30 days, the percentage of surviving explants and the percentage of contamination were evaluated. For culture, MT medium + 1.0 mg L-1 NAA was used, varying BAP concentrations: 2.0, 4.0, 6.0 and 12.0 mg L-1. In the cultivation, the number of compact and friable calluses was counted. For the first and second subculture, the material was introduced into MT medium + 1.0 mg L-1 NAA, varying the same BAP concentrations; the number of friable calluses formed and the size of callus mass were described. The number of replicates formed during subcultures, and fresh and dry matter (g were also obtained. Then, phytochemical tests were done in order to identify some compounds. The adopted time and concentration of sodium hypochlorite proved to be inefficient for disinfestation. For Cissus sicyoides L. callus genesis from leaf segments, the addition of 6.0 mg L-1 BAP to the culture medium is needed. Cardiotonic heterosides were detected in Cissus sicyoides L. calluses.

  15. Inhibition of gastric acid secretion by a standardized aqueous extract of Cecropia glaziovii Sneth and underlying mechanism.

    Science.gov (United States)

    Souccar, C; Cysneiros, R M; Tanae, M M; Torres, L M B; Lima-Landman, M T R; Lapa, A J

    2008-06-01

    Cecropia glazioui Sneth (Cecropiaceae) is used in folk medicine in tropical and subtropical Latin America as cardiotonic, diuretic, hypotensive, anti-inflammatory and anti-asthmatic. The hypotensive/antihypertensive activity of the plant aqueous extract (AE) and isolated butanolic fraction (BuF) has been confirmed and putatively related to calcium channels blockade in vascular smooth musculature [Lapa, A.J., Lima-Landman, M.T.R., Cysneiros, R.M, Borges, A.C.R., Souccar, C., Barreta, I.P., Lima, T.C.M., 1999. The Brazilian folk medicine program to validate medicinal plants - a topic in new antihypertensive drug research. In: Hostettman, K., Gupta, M.P., Marston, A. (Eds.), Proceedings Volume, IOCD/CYTED Symposium, Panamá City, Panamá, 23-26 February 1997. Chemistry, Biological and Pharmacological Properties of Medicinal Plants from the Americas. Harwood Academic Publishers, Amsterdam, pp. 185-196; Lima-Landman, M.T., Borges, A.C., Cysneiros, R.M., De Lima, T.C., Souccar, C., Lapa, A.J., 2007. Antihypertensive effect of a standardized aqueous extract of Cecropia glaziovii Sneth in rats: an in vivo approach to the hypotensive mechanism. Phytomedicine 14, 314-320]. Bronchodilation and antidepressant-like activities of both AE and BuF have been also shown [Delarcina, S., Lima-Landman, M.T., Souccar, C., Cysneiros, R.M., Tanae, M.M., Lapa, A.J., 2007. Inhibition of histamine-induced bronchospasm in guinea pigs treated with Cecropia glaziovi Sneth and correlation with the in vitro activity in tracheal muscles. Phytomedicine 14, 328-332; Rocha, F.F., Lima-Landman, M.T., Souccar, C., Tanae, M.M., De Lima, T.C., Lapa, A.J., 2007. Antidepressant-like effect of Cecropia glazioui Sneth and its constituents -in vivo and in vitro characterization of the underlying mechanism. Phytomedicine 14, 396-402]. This study reports the antiulcer and antisecretory gastric acid activities of the plant AE, its BuF and isolated compounds with the possible mechanism involved. Both AE and Bu

  16. Estudo comparativo da evolução e sobrevida de pacientes com claudicação intermitente, com ou sem limitação para exercícios, acompanhados em ambulatório específico Comparative study of evolution and survival of patients with intermittent claudication, with or without limitation for exercises, followed in a specific outpatient setting

    Directory of Open Access Journals (Sweden)

    Ricardo de Alvarenga Yoshida

    2008-06-01

    established, as well as the benefits of physical training in the treatment of intermittent claudication (IC. However, current data do not provide enough information about the relationship between clinical limitations and risk factors and the performance of physical training and its implications on the evolution and mortality of these patients. OBJECTIVE: To compare the claudication distance and survival of patients with IC throughout time in a specific outpatient setting, with or without limitation for exercises. METHODS: A retrospective cohort study was performed to review the protocols of 185 patients and 469 returns, from 1999 to 2005, evaluating demographic data, average claudication distance and death. The data were analyzed using the software Epi-Info, version 3.2, and SAS, version 8.2. RESULTS: Mean age was 60.9±11.1 years; 61.1% were males and 38.9% were females; 87% were Caucasians and 13% were non-Caucasians. Associated risk factors were hypertension (69.7%, smoking (44.3%, dyslipidemia (32.4%, and diabetes (28.6%. For the patients with claudicating distance lower than 500 m, mean initial distance was 154.0±107.6 m and final distance was 199.8±120.5 m. About 45% of the patients had some clinical limitation to perform the prescribed exercise program, such as angina (26.0%, stroke (4.3%, osteoarthrosis (3.8%, previous minor or major amputation (2.1%, or chronic obstructive pulmonary disease (1.6%. About 11.4% of the patients had previous myocardial infarction, and 5.4% of them were using cardiotonic drugs. Mean follow-up time was 16.0±14.4 months. Mean claudication distance increased 100% (418.47 to 817.74 m throughout 2 years in the group without limitation (p < 0.001 and in nonsmokers (p < 0.001. Survival rate of patients with IC was significantly reduced in the group with limitation for exercises. Logistic regression analysis showed that limitation to exercises was the single factor significantly influencing mortality (p < 0.001. CONCLUSION: Proper and regular

  17. 芪苈强心胶囊与西药联用治疗心衰的临床数据分析%Clinical-data analysis for the CHF patients using Qili Qiangxin capsule combined with western medicine

    Institute of Scientific and Technical Information of China (English)

    张碧华; 李寅; 杨莉萍; 胡欣

    2015-01-01

    Objective:To analyze retrospectively the status of combination treatment of Qili Qiangxin capsule with the western medicine in the Chronic Heart Failure(CHF) patients in Beijing hospital, and the clinical value and adverse drug reaction (ADR) risk of the combination use were also discussed to promote the rational drug use.Methods: With the computer system, we extracted the data of patients number, sex, age, department, disease category and the combined western medicine related with Qili Qiangxin capsule from 2011 to 2013, focused on the interaction of Qili Qiangxin capsule and western medicine, and discussed the mutual coordination or mutual antagonism of Chinese and Western medicine. Results: Qili Qiangxin capsule was used in our hospital since 2011, which number, sum and frequency had much increased during 2012 and 2013. Most of the patients were elderly (80% were above 60 years old), and the majority were male. The department with the greatest drug assumption was cardiovascular department, the second one was Traditional Chinese Medicines(TCM) department. Qili Qiangxin capsule were administrated for CHF patients mostly, combined with many western medicine which included cardiotonic drugs such as digoxin.Conclusion: Qili Qiangxin capsule were prescribed to treat CHF mostly by western medicines doctors. The combination use of Qili Qiangxin capsule and digoxin could increase the blood concentration of digoxin, so clinical pharmacists suggested the combination to be used cautiously. And ifnally the combination use of the two drugs had been prevented since 2013.%目的:通过对北京医院(以下简称我院)芪苈强心胶囊的总体用药情况及其在治疗慢性心力衰竭方面与西药的联用情况进行回顾性分析,探讨中西药物联用对于治疗慢性心衰的临床价值和不良反应风险,促进药物的安全合理使用。方法:通过我院计算机系统,提取2011—2013年芪苈强心胶囊的用药人数、性别、年