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Sample records for quinine

  1. Quinine

    Science.gov (United States)

    ... or life-threatening illness that is spread by mosquitos in certain parts of the world). Quinine should ... how long you should wait between taking this type of antacid and taking ... deficiency (an inherited blood disease), or if you have or have ever ...

  2. 21 CFR 172.575 - Quinine.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Quinine. 172.575 Section 172.575 Food and Drugs... Agents and Related Substances § 172.575 Quinine. Quinine, as the hydrochloride salt or sulfate salt, may... beverages as a flavor Not to exceed 83 parts per million, as quinine. Label shall bear a...

  3. Quinine conjugates and quinine analogues as potential antimalarial agents.

    Science.gov (United States)

    Jones, Rachel A; Panda, Siva S; Hall, C Dennis

    2015-06-01

    Malaria is a tropical disease, prevalent in Southeast Asia and Africa, resulting in over half a million deaths annually; efforts to develop new antimalarial agents are therefore particularly important. Quinine continues to play a role in the fight against malaria, but quinoline derivatives are more widely used. Drugs based on the quinoline scaffold include chloroquine and primaquine, which are able to act against the blood and liver stages of the parasite's life cycle. The purpose of this review is to discuss reported biologically active compounds based on either the quinine or quinoline scaffold that may have enhanced antimalarial activity. The review emphasises hybrid molecules, and covers advances made in the last five years. The review is divided into three sections: modifications to the quinine scaffold, modifications to aminoquinolines and finally metal-containing antimalarial compounds.

  4. Demethylation of Quinine Using Anhydrous Aluminium Trichloride

    OpenAIRE

    Aiyi Asnawi; As’ari Nawawi; Rahmana Emran Kartasasmita; Slamet Ibrahim3)

    2011-01-01

    Quinine is a natural alkaloid having a methoxy group bound to quinoline ring and an allyl group bound to quinuclidine ring. Demethylation of quinine applying strong acid such as HBr or HI at high temperature was unsuccessful. The aim of this research was to obtain demethylated quinine by means of mild and selective demethylation procedure to prevent the addition reaction of allyl group. Selective demethylation of quinine has been carried out using anhydrous aluminium trichloride as reagent. T...

  5. Is it quinine TTP/HUS or quinine TMA? ADAMTS13 levels and implications for therapy.

    Science.gov (United States)

    Park, Yara A; Hay, Shauna N; King, Karen E; Matevosyan, Karen; Poisson, Jessica; Powers, Amy; Sarode, Ravindra; Shaz, Beth; Brecher, Mark E

    2009-01-01

    Thrombocytopenia with or without microangiopathy following quinine is often referred to as quinine "hypersensitivity." When schistocytes are present it is frequently termed "quinine-associated TTP/HUS." A severe deficiency of the vWF-cleaving protease, ADAMTS13, is associated with idiopathic TTP. A previous study of patients with "quinine-associated TTP/HUS" found that ADAMTS13 activities were not abnormal in 12/12 patients. A retrospective review of TTP patients with quinine-associated thrombotic microangiopathy (TMA) for whom ADAMTS13 was measured before plasma exchange was performed. Six patients were identified. All were females (age range: 43 to 73, mean = 61.7 years) and had taken quinine for leg cramps. Four of the six experienced renal failure requiring dialysis. Five of the patients had D-Dimers levels measured, all were elevated. In four patients the levels were > or = 18 times the upper limit of normal. ADAMTS13 was normal in four patients and mildly decreased in two patients. We conclude that while thrombocytopenia and schistocytosis can be seen in quinine-associated TTP/HUS, the pathophysiology seems to be distinct from that seen in most cases of idiopathic TTP (i.e., severely decreased ADAMTS13 with an inhibitor). We recommend that a TMA in association with quinine be consistently referred to as quinine-associated thrombotic microangiopathy (quinine-TMA) to better distinguish this entity from idiopathic TTP. The use of plasma exchange in quinine-TMA is called into question.

  6. Historical Review: Problematic Malaria Prophylaxis with Quinine.

    Science.gov (United States)

    Shanks, G Dennis

    2016-08-03

    Quinine, a bitter-tasting, short-acting alkaloid drug extracted from cinchona bark, was the first drug used widely for malaria chemoprophylaxis from the 19th century. Compliance was difficult to enforce even in organized groups such as the military, and its prophylaxis potential was often questioned. Severe adverse events such as blackwater fever occurred rarely, but its relationship to quinine remains uncertain. Quinine prophylaxis was often counterproductive from a public health viewpoint as it left large numbers of persons with suppressed infections producing gametocytes infective for mosquitoes. Quinine was supplied by the first global pharmaceutical cartel which discouraged competition resulting in a near monopoly of cinchona plantations on the island of Java which were closed to Allied use when the Japanese Imperial Army captured Indonesia in 1942. The problems with quinine as a chemoprophylactic drug illustrate the difficulties with medications used for prevention and the acute need for improved compounds.

  7. 21 CFR 862.3750 - Quinine test system.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 8 2010-04-01 2010-04-01 false Quinine test system. 862.3750 Section 862.3750....3750 Quinine test system. (a) Identification. A quinine test system is a device intended to measure quinine, a fever-reducing and pain-relieving drug intended in the treatment of malaria, in serum and...

  8. Analytics of Quinine and its Derivatives.

    Science.gov (United States)

    Kluska, Mariusz; Marciniuk-Kluska, Anna; Prukała, Dorota; Prukała, Wiesław

    2016-01-01

    The objective of this study was to perform a synthesis and analysis of the most important information on quinine and its derivatives, which are still very important in the treatment of malaria. The analysis of stereoisomers of quinine and its derivatives was conducted using two techniques, high-performance liquid chromatography and capillary electrophoresis. Particularly noteworthy is the technique used for the determination of isotachophoresis, referred to as one of the so-called green chemistry techniques. Particular attention was paid to properties and the use of quinine and its derivatives in the treatment of malaria. The analytical part will supplement knowledge about quinidine, quinine, and cinchonidine, and will contribute to the growth of research on the so-much-needed drugs against malaria.

  9. Quinine-Induced Disseminated Intravascular Coagulation

    Directory of Open Access Journals (Sweden)

    Firas Abed

    2016-01-01

    Full Text Available Every drug comes with some side effect. It is the benefit/risk ratio that determines the medical use of the drug. Quinine, a known antimalarial drug, has been used for nocturnal leg cramps since the 1930s; it is associated with severe life-threatening hematological and cardiovascular side effects. Disseminated intravascular coagulation (DIC, albeit rare, is a known coagulopathy associated with Quinine. It is imperative to inquire about the Quinine intake in medication history in patients with coagulopathy, as most patients still consider it a harmless home remedy for nocturnal leg cramps. In this report, we present a case of coagulopathy in a middle-aged woman, who gave a history of taking Quinine for nocturnal leg cramps, as her home remedy. Early identification of the offending agent led to the diagnosis, prompt discontinuation of the medication, and complete recovery and prevented the future possibility of recurrence.

  10. The antimalarial drug quinine interferes with serotonin biosynthesis and action.

    Science.gov (United States)

    Islahudin, Farida; Tindall, Sarah M; Mellor, Ian R; Swift, Karen; Christensen, Hans E M; Fone, Kevin C F; Pleass, Richard J; Ting, Kang-Nee; Avery, Simon V

    2014-01-01

    The major antimalarial drug quinine perturbs uptake of the essential amino acid tryptophan, and patients with low plasma tryptophan are predisposed to adverse quinine reactions; symptoms of which are similar to indications of tryptophan depletion. As tryptophan is a precursor of the neurotransmitter serotonin (5-HT), here we test the hypothesis that quinine disrupts serotonin function. Quinine inhibited serotonin-induced proliferation of yeast as well as human (SHSY5Y) cells. One possible cause of this effect is through inhibition of 5-HT receptor activation by quinine, as we observed here. Furthermore, cells exhibited marked decreases in serotonin production during incubation with quinine. By assaying activity and kinetics of the rate-limiting enzyme for serotonin biosynthesis, tryptophan hydroxylase (TPH2), we showed that quinine competitively inhibits TPH2 in the presence of the substrate tryptophan. The study shows that quinine disrupts both serotonin biosynthesis and function, giving important new insight to the action of quinine on mammalian cells.

  11. Sciatic nerve palsy associated with intramuscular quinine injections ...

    African Journals Online (AJOL)

    Key Words: Sciatic nerve palsy, intramuscular injections, children, quinine dil~ ... adverse effects which include ototoxicity resulting .... quinine injection into the gluteal muscles of his right ... to maintain joint movement and avoid damage to.

  12. Optical coherence tomography findings of quinine poisoning

    Directory of Open Access Journals (Sweden)

    John Christoforidis

    2011-01-01

    Full Text Available John Christoforidis, Robert Ricketts, Theodore Loizos, Susie ChangThe Ohio State University College of Medicine, Columbus, OH, USAPurpose: To report a case of acute quinine poisoning, document acute and chronic macular changes with optical coherence tomography imaging and fluorescein angiography (FA, and to review the literature on ocular toxicity of quinine.Methods: A 32-year-old white female presented to our Emergency Department after ingesting over 7.5 g of quinine. She underwent a complete ophthalmologic examination, fluorescein angiography, Stratus time-domain optical coherence tomography (OCT, and electroretinography at 72 hours and 15 months postingestion. Stratus time-domain and Cirrus spectral-domain OCT, fundus autofluorescence, and FA were obtained at 28 months postingestion.Results: Fluorescein angiography at 72 hours postingestion revealed normal filling times and vasculature. OCT showed marked thickening of the inner retina bilaterally. At 15 and 28 months follow-up, fundus photography and fluorescein angiography demonstrated optic nerve pallor, severely attenuated retinal vessels while OCT showed inner retinal atrophy. Fundus autofluorescence did not reveal any retinal pigmentary abnormalities.Conclusions: Quinine toxicity as seen by OCT reveals increased thickness with inner retinal hyperreflectivity acutely with development of significant retinal atrophy in the long-term. Fundus autofluorescence reveals an intact retinal pigment epithelial layer at 28 months. These findings suggest that quinine poisoning may produce a direct toxic effect on the inner retina in the acute phase resulting in long-term retinal atrophy.Keywords: retinal, optical coherence tomography, quinine toxicity 

  13. The antimalarial drug quinine interferes with serotonin biosynthesis and action

    DEFF Research Database (Denmark)

    Islahudin, Farida; Tindall, Sarah M.; Mellor, Ian R.

    2014-01-01

    The major antimalarial drug quinine perturbs uptake of the essential amino acid tryptophan, and patients with low plasma tryptophan are predisposed to adverse quinine reactions; symptoms of which are similar to indications of tryptophan depletion. As tryptophan is a precursor of the neurotransmit...

  14. tration of quinine on the morphology of rat testis

    African Journals Online (AJOL)

    Key-words: Quinine, Testes, Seminiferous tubules,. Seminiferous epitlzeliunz ... while QU induced tail an gulation in caudal epididymal sperms of the mice in invitro ..... Syncrgistic spcrmicidal activity of neem seed cxtract, rectha saponins and ...

  15. Quinine enhances the behavioral stimulant effect of cocaine in mice.

    Science.gov (United States)

    Huertas, Adriana; Wessinger, William D; Kucheryavykh, Yuri V; Sanabria, Priscila; Eaton, Misty J; Skatchkov, Serguei N; Rojas, Legier V; Maldonado-Martínez, Gerónimo; Inyushin, Mikhail Y

    2015-02-01

    The Na(+)-dependent dopamine transporter (DAT) is primarily responsible for regulating free dopamine (DA) concentrations in the brain by participating in the majority of DA uptake; however, other DA transporters may also participate, especially if cocaine or other drugs of abuse compromise DAT. Recently, such cocaine-insensitive low-affinity mono- and poly-amine OCT transporters were described in astrocytes which use DA as a substrate. These transporters are from a different transporter family and while insensitive to cocaine, they are specifically blocked by quinine and some steroids. Quinine is inexpensive and is often found in injected street drugs as an "adulterant". The present study was designed to determine the participation of OCTs in cocaine dependent behavioral and physiological changes in mice. Using FVB mice we showed, that daily single injections of quinine (10 mg/kg, i.p.) co-administered with cocaine (15 mg/kg, i.p.) for 10 days significantly enhanced cocaine-induced locomotor behavioral sensitization. Quinine had no significant effect on the time course of behavioral activation. In astrocytes from the ventral tegmental area of mice, transporter currents of quinine-sensitive monoamine transporters were also augmented after two weeks of cocaine administration. The importance of low-affinity high-capacity transporters for DA clearance is discussed, explaining the known ability of systemically administered DAT inhibitors to anomalously increase DA clearance.

  16. Relatively spared central multifocal electroretinogram responses in acute quinine toxicity

    Science.gov (United States)

    Saeed, Muhammad Usman; Noonan, Carmel; Hagan, Richard; Brown, Malcolm

    2011-01-01

    A 71-year-old man was investigated with electrodiagnostic testing 4 months after a deliberate quinine overdose. Initially he was admitted to intensive care unit with visual acuity (VA) of perception of light in both eyes. VA recovered to 6/6 right eye and 6/12 left eye, though severely constricted fields were noted. Slow stimulus (base period of 83 ms) multifocal electroretinogram (ERG) showed electronegative responses outside the inner 5 degrees, with a reduced but electropositive response seen in this central area. It appears that in this case of bilaterally negative ERGs that the macula/fovea (which has a vascular supply through the choroid) is relatively spared as is seen in bilateral vascular electronegative ERGs. This may indicate that quinine toxicity to the retina may be secondary to effects similar to vascular occlusion or severe ischemia during the acute phase of quinine poisoning. PMID:22693278

  17. Effects of oral and parenteral quinine on rats with ventromedial hypothalamic knife-cut obesity.

    Science.gov (United States)

    Oku, J; Bray, G A; Fisler, J S

    1984-06-01

    The addition of quinine to the food reversed the obesity in rats with hypothalamic hyperphagia induced by knife cuts. Similarly, the injection of quinine into rats with hypothalamic knife cuts reduced food intake and body weight but the effects were smaller than those observed when quinine was added to the diet. Urinary quinine excretion was similar by the oral and parenteral routes. The food intake of the knife-cut animals receiving quinine gradually fell to the same level as in the sham-operated animals receiving quinine by either route. The weights of retroperitoneal fat pads were related to the weights of the animals and were reduced in the quinine-treated groups. Plasma insulin concentrations were significantly higher in the knife-cut animals and were reduced toward control levels by quinine treatment. Gluconeogenesis, measured by incorporation of radioactivity from labeled bicarbonate into glucose, was unaffected by treatment with quinine or by knife cuts. Lipogenesis from tritiated water in vivo was not different between treatment groups in the liver or retroperitoneal fat pads. However, in vivo lipogenesis was reduced in knife-cut rats fed ad libitum compared with quinine-treated rats. The response of lipogenesis to insulin in vitro was also not different between treatment groups. These data suggest that a major part of the reduction in food intake in hyperphagic rats eating a quinine-adulterated diet is due to postingestional events.

  18. Quinine, Malaria, and the Cinchona Bureau : Marketing Practices and Knowledge Circulation in a Dutch Transoceanic Cinchona-Quinine Enterprise (1920s-30s)

    NARCIS (Netherlands)

    Roersch van der Hoogte, Arjo; Pieters, Toine

    2015-01-01

    In this study, we show how a Dutch pharmaceutical consortium of cinchona producers and quinine manufacturers was able to capitalize on one of the first international public health campaigns to fight malaria, thereby promoting the sale of quinine, an antimalarial medicine. During the 1920s and 1930s,

  19. Quinine levels in patients with uncomplicated falciparum malaria in the Amazon region of Brazil

    Directory of Open Access Journals (Sweden)

    José Luiz Fernandes Vieira

    2008-10-01

    Full Text Available We examined the plasmatic concentrations of quinine in patients with uncomplicated falciparum malaria in an endemic area of the Amazon region in Brazil in a prospective clinical trial, in which a standard three-day course of oral quinine plus doxycycline was used. We measured the quinine in the plasma samples on days 0 and 3by high performance liquid chromatography. The mean concentration of quinine was 6.04 ±2.21 µg/mL in male patients and 5.98 ±1.95 µg/mL in female patients. No significant differences in quinine concentration were observed between these two groups. All samples collected before starting treatment were negative for quinine. This information could help in the development of strategies for the rational use of antimalarial drugs in Brazil.

  20. Quinine, Malaria, and the Cinchona Bureau: Marketing Practices and Knowledge Circulation in a Dutch Transoceanic Cinchona-Quinine Enterprise (1920s-30s).

    Science.gov (United States)

    Van Der Hoogte, Arjo Roersch; Pieters, Toine

    2016-04-01

    In this study, we will show how a Dutch pharmaceutical consortium of cinchona producers and quinine manufacturers was able to capitalize on one of the first international public health campaigns to fight malaria, thereby promoting the sale of quinine, an antimalarial medicine. During the 1920s and 1930s, the international markets for quinine were controlled by this Dutch consortium, which was a transoceanic cinchona-quinine enterprise centered in the Cinchona Bureau in the Netherlands. We will argue that during the interwar period, the Cinchona Bureau became the decision-making center of this Dutch cinchona-quinine pharmaceutical enterprise and monopolized the production and trade of an essential medicine. In addition, we will argue that capitalizing on the international public health campaign in the fight against malaria by the Dutch cinchona-quinine enterprise via the Cinchona Bureau can be regarded as an early example of corporate colonization of public health by a private pharmaceutical consortium. Furthermore, we will show how commercial interests prevailed over scientific interests within the Dutch cinchona-quinine consortium, thus interfering with and ultimately curtailing the transoceanic circulation of knowledge in the Dutch empire.

  1. Treatment of severe falciparum malaria: quinine versus artesunate

    Directory of Open Access Journals (Sweden)

    Dipesh Patel

    2013-02-01

    Full Text Available Background: Malaria is the most important disease of human being. More than 40% of the world’s population is considered to be at risk of exposure of this disease. Malaria infection has been increasing over recent years due to combination of factors including increasing resistance of malarial parasite. Most of the strains of P. falciparum are now resistance to conventional drugs like chloroquine in many areas. The objective of this study was to compare the efficacy and safety of quinine and artesunate in treatment of P. falciparum malaria. Methods: This is hospital based prospective study, conducted amongst 35 randomly selected patients of severe P. falciparum malaria. Patients with any contraindications of either drug were excluded to avoid bias. Standard statistical tests were applied for qualitative as well as quantitative data. Results: As per the study end point results of difference of mortality in patients receiving either drug was not significant (p > 0.75, but difference in clinical parameters like fever clearance time (p <0.01, parasite clearance time (p < 0.001 and coma resolution time (p < 0.001 were significant among patients receiving artesunate. There were no any significant differences in adverse effects of both the drugs. Mortality was same in both arms taking either drug. Conclusions: Artesunate is as good as quinine in mortality aspect but artesunate is superior in fever clearance time (FCT & parasite clearance time (PCT. Coma resolution time is faster with quinine as compared to artesunate. There are no significant adverse effects of either drug. So artesunate is equivalent or superior for treatment for severe falciparum malaria. [Int J Basic Clin Pharmacol 2013; 2(1.000: 30-36

  2. History and Epistemology of Science in the Classroom: The Synthesis of Quinine as a Proposal

    Science.gov (United States)

    Souza, Karina Ap. F. D.; Porto, Paulo A.

    2012-01-01

    The history of the quinine synthesis can be used as a case study to emphasize that science is influenced by social and historical processes. The first efforts toward the synthesis of this substance, which until recently was the only treatment for malaria, were by Perkin in 1856 when, trying to obtain quinine, he synthesized mauveine. Since then,…

  3. Acute allergic reaction to oral quinine for malarial prevention: A case report

    Directory of Open Access Journals (Sweden)

    Sora Yasri

    2016-01-01

    Full Text Available Quinine is a classical antimalarial drug that is used worldwide. It is also used for pre-exposure of malaria before visiting to the jungle in the endemic area of malaria. In this article, the authors reported a case of acute allergic reaction to oral quinine for malarial prevention.

  4. Treatment of imported severe malaria with artesunate instead of quinine--more evidence needed?

    NARCIS (Netherlands)

    Cramer, J.P.; López-Vélez, R.; Burchard, G.D.; Grobusch, M.P.; de Vries, P.J.

    2011-01-01

    Rapid and fast acting anti-malarials are essential to treat severe malaria. Quinine has been the only option for parenteral therapy until recently. While current evidence shows that intravenous artesunate is more effective than quinine in treating severe malaria in endemic countries, some questions

  5. Treatment of imported severe malaria with artesunate instead of quinine--more evidence needed?

    NARCIS (Netherlands)

    Cramer, J.P.; López-Vélez, R.; Burchard, G.D.; Grobusch, M.P.; de Vries, P.J.

    2011-01-01

    Rapid and fast acting anti-malarials are essential to treat severe malaria. Quinine has been the only option for parenteral therapy until recently. While current evidence shows that intravenous artesunate is more effective than quinine in treating severe malaria in endemic countries, some questions

  6. Acute allergic reaction to oral quinine for malarial prevention:A case report

    Institute of Scientific and Technical Information of China (English)

    Sora Yasri; Viroj Wiwanitkit

    2016-01-01

    Quinine is a classical antimalarial drug that is used worldwide. It is also used for pre-exposure of malaria before visiting to the jungle in the endemic area of malaria. In this article, the authors reported a case of acute allergic reaction to oral quinine for malarial prevention.

  7. Diversity and severity of adverse reactions to quinine: A systematic review.

    Science.gov (United States)

    Liles, Nathan W; Page, Evaren E; Liles, Amber L; Vesely, Sara K; Raskob, Gary E; George, James N

    2016-05-01

    Quinine is a common cause of drug-induced thrombocytopenia and the most common cause of drug-induced thrombotic microangiopathy. Other quinine-induced systemic disorders have been described. To understand the complete clinical spectrum of adverse reactions to quinine we searched 11 databases for articles that provided sufficient data to allow evaluation of levels of evidence supporting a causal association with quinine. Three reviewers independently determined the levels of evidence, including both immune-mediated and toxic adverse reactions. The principal focus of this review was on acute, immune-mediated reactions. The source of quinine exposure, the involved organ systems, the severity of the adverse reactions, and patient outcomes were documented. One hundred-fourteen articles described 142 patients with definite or probable evidence for a causal association of quinine with acute, immune-mediated reactions. These reactions included chills, fever, hypotension, painful acral cyanosis, disseminated intravascular coagulation, hemolytic anemia, thrombocytopenia, neutropenia, acute kidney injury, rhabdomyolysis, liver toxicity, cardiac ischemia, respiratory failure, hypoglycemia, blindness, and toxic epidermal necrolysis. One hundred-two (72%) reactions were caused by quinine pills; 28 (20%) by quinine-containing beverages; 12 (8%) by five other types of exposures. Excluding 41 patients who had only dermatologic reactions, 92 (91%) of 101 patients had required hospitalization for severe illness; 30 required renal replacement therapy; three died. Quinine, even with only minute exposure from common beverages, can cause severe adverse reactions involving multiple organ systems. In patients with acute, multi-system disorders of unknown origin, an adverse reaction to quinine should be considered.

  8. Effect of quinine and artesunate combination therapy on platelet count of children with severe malaria.

    Science.gov (United States)

    Gupta, Parul; Narang, Manish; Gomber, Sunil; Saha, Rumpa

    2017-05-01

    There are several case reports of quinine-induced thrombocytopenia but no clinical trials to ascertain its incidence and significance in severe malaria. The primary objective was to assess the effect of quinine on the platelet count in children with severe malaria and to compare it with artesunate combination therapy (ACT), and the secondary objective was to assess outcome of treatment with quinine and ACT. An open-labelled, randomised, controlled trial was undertaken in 100 children aged 6 months to 12 years who were diagnosed with malaria by microscopy and/or rapid diagnostic test kits with at least one WHO clinical or laboratory criterion for severe malaria. All subjects were commenced on either quinine or ACT. Clindamycin was added to artesunate as a combination drug (ACT). It was also given to patients on quinine to avoid its confounding effect on the results. Platelet counts were undertaken every 24 hours for 7 consecutive days, temperature and coma score (Blantyre coma score ≥3 in children 4 years) was recorded 6-hourly and peripheral smears were taken 12-hourly until two consecutively negative smears were obtained. The primary outcome was a fall in the platelet count by ≥20% from the time of drug initiation until day 7. The secondary outcome was comparison of the efficacy, parasite clearance time, fever clearance time, coma recovery time and adverse effects of quinine vs ACT. 30.4% patients in the quinine group (n = 48) had ≥20% fall in platelet count and 10.8% of patients in the ACT group (n = 46) (P = 0.02). Despite the fall in platelet count, there was no bleeding. The efficacy of ACT was significantly better than quinine but the other treatment outcomes showed insignificant difference. Quinine should be used with caution in patients with severe malaria because of the potential risk of quinine-induced thrombocytopenia.

  9. The effect of quinine on outer hair cell shape, compliance and force.

    Science.gov (United States)

    Jarboe, J K; Hallworth, R

    1999-06-01

    Quinine intoxication causes a well-described syndrome that includes tinnitus, sensorineural hearing loss and vertigo. The pathophysiology of quinine's effects on hearing is unknown, but may include a peripheral component. The cochlear outer hair cell is known to be motile and to contribute force to amplify the vibration pattern of the organ of Corti. The outer hair cell is also a target of diseases involving tinnitus and sensorineural hearing loss, including salicylate intoxication. These effects may be mediated through changes either in motile force or in mechanical properties. Quinine's effects on outer hair cell motility and mechanical properties have therefore been examined in vitro. Quinine at 5.0 mM substantially decreased active force generation in isolated guinea pig cochlear outer hair cells. Isolated cells also elongated and dilated in diameter when exposed to 5.0 mM quinine. No consistent changes in mechanical properties were observed. 1.0 mM quinine was ineffective in either force reduction or elongation. Trifluoperazine, a calmodulin inhibitor, and ML-9, a blocker of myosin light chain kinases, were ineffective in blocking quinine-induced force reduction or elongation. Deferoxamine, a hydroxyl free radical scavenger, also failed to block either the force decrease or the elongation.

  10. Building the world's supply of quinine: Dutch colonialism and the origins of a global pharmaceutical industry.

    Science.gov (United States)

    Goss, Andrew

    2014-03-01

    Quinine, a naturally occurring alkaloid from the Cinchona tree, was one of the first drugs produced and sold by a global pharmaceutical industry during the nineteenth century. Factories in Europe and North America dominated the manufacturing industry, and between 1890 and 1940, Cinchona plantations on Java supplied most of the bark for the quinine pharmaceutical business. At the end of the nineteenth century, the Dutch colonial state kept a hands-off approach to the Cinchona enterprises, in keeping with its liberal orientation. But the persistent low-price for bark, which led to the near ruin of the Cinchona planters, eventually pushed the colonial state to actively protect the Cinchona plantations. Colonial officials sought to stabilize the colonial Cinchona export-business by encouraging the integration of the quinine industry on a global scale. Most important was the colonial state's sponsorship in 1913 of the Quinine Agreement, establishing a set price for Cinchona bark, which created the world's first pharmaceutical cartel. In the interwar period, an alliance of Dutch government officials, planters, scientists, doctors and drug-makers, working in both the motherland and the colony, actively promoted the expansion of quinine consumption, as well as the merit of the Quinine Agreement, which they argued supplied guaranteed a steady supply of quinine, all for the wellbeing of global humanity.

  11. Artemisinin derivatives versus quinine in treating severe malaria in children: a systematic review

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    de Frey Albie

    2008-10-01

    Full Text Available Abstract Background The efficacy of intravenous quinine, which is the mainstay for treating severe malaria in children, is decreasing in South East Asia and Africa. Artemisinin derivatives are a potential alternative to quinine. However, their efficacy compared to quinine in treating severe malaria in children is not clearly understood. The objective of this review was to assess the efficacy of parenteral artemisinin derivatives versus parenteral quinine in treating severe malaria in children. Methods All randomized controlled studies comparing parenteral artemisinin derivatives with parenteral quinine in treating severe malaria in children were included in the review. Data bases searched were: The Cochrane Central Register of Controlled Trials (The Cochrane Library Issue 4, 2007, MEDLINE (1966 to February 2008, EMBASE (1980 to February 2008, and LILACS (1982 to February 2008. Dichotomous variables were compared using risk ratios (RR and the continuous data using weighted mean difference (WMD. Results Twelve trials were included (1,524 subjects. There was no difference in mortality between artemisinin derivatives and quinine (RR = 0.90, 95% CI 0.73 to 1.12. The artemisinin derivatives resolved coma faster than quinine (WMD = -4.61, 95% CI: -7.21 to -2.00, fixed effect model, but when trials with adequate concealment only were considered this differences disappeared. There was no statistically significant difference between the two groups in parasite clearance time, fever clearance time, incidence of neurological sequelae and 28th day cure rate. One trial reported significantly more local reactions at the injection site with intramuscular quinine compared to artemether. None of the trials was adequately powered to demonstrate equivalence. Conclusion There was no evidence that treatment of children with severe malaria with parenteral artemisinin derivatives was associated with lower mortality or long-term morbidity compared to parenteral quinine

  12. Quinine and the ABCs of Long QT: A Patient's Misfortune with Arthritis, (Alcoholic) Beverages, and Cramps.

    Science.gov (United States)

    Sheehan, Elyce T; Frizzell, Jarrod D; Gabaldon, Jude; West, Michael B

    2016-10-01

    A 91-year-old woman presented to the emergency department by ambulance after her family found her minimally responsive. Telemetry monitoring demonstrated episodes of non-sustained polymorphic ventricular tachycardia (PMVT) associated with significantly prolonged repolarization. Her medical history revealed that she was taking quinine or a derivative in three different forms: hydroxychloroquine, quinine sulfate (for leg cramps), and her gin mixed with tonic water (containing quinine). The present case is illustrative of classic etiologies and findings of acquired long QT syndrome, and serves as an important reminder for providers to take a complete medication history, including use of duplicative and alternative medicines and type of alcohol consumption.

  13. Application of isothermal titration calorimeter for screening bitterness-suppressing molecules of quinine.

    Science.gov (United States)

    Zhang, Yifan; Zhu, Youwei; Zhao, Na; Wu, Jinhui; Hu, Yiqiao

    2016-01-01

    Bitterness-suppressing molecules have drawn ever-increasing attention these years for some unique advantages like low molecular weight, tastelessness and no interference on drug bioavailability. L-Arg was reported to suppress the bitterness of quinine, and we happened to find that the suppressing effects could be demonstrated by isothermal titration calorimeter (ITC). In this study, we investigated the possibility of using ITC to screen bitterness-suppressing molecules for quinine. Among the amino acids we screened, L-Lys bond quinine with high affinity. The results of ITC correlated well with the results of human sensory experiments. L-Arg and L-Lys could suppress the bitterness of quinine while other amino acids could not. Therefore, ITC has the potential to screen bitterness-suppressing molecules.

  14. A new trick for an ancient drug: quinine dissociates antiphospholipid immune complexes.

    Science.gov (United States)

    Bezati, E; Wu, X-X; Quinn, A S; Taatjes, D J; Rand, J H

    2015-01-01

    Quinine, a quinoline derivative, is an ancient antipyretic drug with antimalarial properties that has been phased out by more effective synthetic candidates. In previous studies we discovered that hydroxychloroquine (HCQ), a synthetic antimalarial with structural similarities to quinine, reduced the binding of antiphospholipid (aPL) immune complexes to phospholipid bilayers. We performed ellipsometry and atomic force microscopy (AFM) studies to measure the effect of quinine on dissociation of anti-β2-glycoprotein I (anti-β2GPI) immune complexes. We found that quinine desorbed pre-formed β2GPI-aPL immunoglobulin (Ig)G complexes from phospholipid bilayers at significantly lower molar concentrations than HCQ. Quinine also inhibited the formation of immune complexes with a higher efficacy than HCQ at equivalent drug concentrations of 0.2 mg/ml (0.192 ± 0.025 µg/cm(2) for quinine vs. 0.352 ± 0.014 µg/cm(2) for HCQ, p quinine disintegrated immune complexes bound to planar phospholipid layers. The desorptive and inhibitory effects of the old drug, quinine, toward β2GPI-aPL IgG complexes and β2GPI were significantly more pronounced compared to the synthetic antimalarial, HCQ. The results suggest that the quinoline core of the molecule is a critical domain for this activity and that side chains may further modulate this effect. The results also indicate that there may yet be room for considering new activities of very old drugs in devising clinical trials on potential non-anticoagulant treatments for antiphospholipid syndrome (APS).

  15. Pharmacokinetic Interactions Between Quinine and Lopinavir/Ritonavir in Healthy Thai Adults.

    Science.gov (United States)

    Rattanapunya, Siwalee; Cressey, Tim R; Rueangweerayut, Ronnatrai; Tawon, Yardpiroon; Kongjam, Panida; Na-Bangchang, Kesara

    2015-12-01

    This study aimed to investigate the pharmacokinetic interactions between quinine and lopinavir boosted with ritonavir (LPV/r) in healthy Thai adults (8 males and 12 females). Period 1 (day 1): subjects received a single oral dose of 600 mg quinine sulfate. Period 2: subjects received LPV/r (400/100 mg) twice daily. Period 3: subjects received a single quinine sulfate dose plus LPV/r twice a day. Intensive blood sampling was performed during each phase. Quinine AUC0-48h (area under the plasma concentration-time curve from time 0 to 48 hours), AUC0-∞ (area under the plasma concentration-time curve from time 0 to infinity), and Cmax (maximum concentration over the time-span specified), were 56%, 57%, and 47% lower, respectively, in the presence of LPV/r. 3-Hydroxyquinine AUC0-48h, AUC0-∞, and Cmax were significantly lower and the metabolite-to-parent ratio was significantly reduced. Lopinavir and ritonavir exposures were not significantly reduced with quinine coadministration, but Cmax of both drugs were significantly lower. The geometric mean ratio (GMR) and 90% CI of AUC0-48h, AUC0-∞, and Cmax for quinine, 3-hydroxyquinine, lopinavir, and ritonavir lay outside the bioequivalent range of 0.8-1.25. Drug treatments during all periods were generally well tolerated. The reduction in systemic exposure of quinine and 3-hydroxyquinine with concomitant LPV/r use raises concerns of suboptimal exposure. Studies in HIV/malaria coinfection patients are needed to determine the clinical impact to decide if any change to the quinine dose is warranted.

  16. Quinine blocks a calcium-activated potassium conductance in mammalian enteric neurones.

    OpenAIRE

    Cherubini, E.; North, R. A.; Surprenant, A.

    1984-01-01

    Quinine (100 microM) abolished the slow calcium-dependent afterhyperpolarization which occurs after an action potential in some neurones of the guinea-pig myenteric and submucous plexus. This occurred without any effect on the amplitude or time course of the action potential itself, or on the faster calcium-independent afterhyperpolarization. Tetraethylammonium did not reduce the slow afterhyperpolarization. Quinine also abolished the hyperpolarization which was evoked by intracellular inject...

  17. Quinine Bitterness and Grapefruit Liking Associate with Allelic Variants in TAS2R31.

    Science.gov (United States)

    Hayes, John E; Feeney, Emma L; Nolden, Alissa A; McGeary, John E

    2015-07-01

    Multiple psychophysical gene-association studies suggest a single nucleotide polymorphism (SNP) within the bitter receptor gene TAS2R19 on chromosome 12 may be functional. Previously, the Arg299Cys SNP (rs10772420) has been associated with differential bitterness of quinine and differential liking for grapefruit juice. However, quinine does not activate TAS2R19 in vitro; likewise, limonin and naringin, bitter compounds in grapefruit, do not activate TAS2R19 in vitro. Here, we examined quinine bitterness (whole-mouth swish-and-spit stimuli and regionally delivered quinine across 4 loci) and remembered liking for grapefruit juice to test whether they associate with SNPs in another nearby gene, TASR2R31. We observed SNP-phenotype associations between whole-mouth quinine bitterness and self-reported liking for grapefruit juice with SNPs in TAS2R31, and regional quinine bitterness followed a similar trend, but did not reach significance. Present data provide independent replication of prior associations reported for TAS2R19. However, we also observed strong linkage disequilibrium (LD) between TAS2R19 and TAS2R31 SNPs. When present data are considered in light of existing functional expression data, this suggests phenotypic associations reported previously for rs10772420 may potentially be due to LD between this SNP and polymorphism(s) in, or closer to, TAS2R31. If confirmed, this would reduce the number of TAS2Rs with putatively functional polymorphisms to 5.

  18. Biowaiver monographs for immediate-release solid oral dosage forms: quinine sulfate.

    Science.gov (United States)

    Strauch, Stefanie; Dressman, Jennifer B; Shah, Vinod P; Kopp, Sabine; Polli, James E; Barends, Dirk M

    2012-02-01

    The biowaiver approach permits evaluation of bioequivalence (BE) using a set of laboratory tests, obviating the need for expensive and time-consuming pharmacokinetic BE studies provided that both the active pharmaceutical ingredient and the formulations can meet the specified criteria. In the present monograph, the biowaiver-relevant data including solubility and permeability data, therapeutic use and therapeutic index, pharmacokinetic properties, reported excipient interactions, and BE/bioavailability studies of quinine sulfate are itemized and discussed. Quinine sulfate has borderline solubility characteristics and, on the whole, is highly permeable. Thus, depending on the jurisdiction, it is assigned to Biopharmaceutics Classification System class I or II. Although these characteristics would suggest a low risk of bioinequivalence among oral quinine products, a recent pharmacokinetic study showed bioinequivalence of two products. Even though quinine does not, strictly speaking, fit the definition of a narrow therapeutic index drug, it shows dose-related and, in some cases, irreversible side effects and toxicities at concentrations not far above the therapeutic concentration range. Taking all relevant aspects into consideration, a biowaiver cannot be recommended for new quinine immediate-release multisource products or major post-approval changes of already marketed quinine products, and in such cases, BE should be evaluated using an in vivo BE study.

  19. The neuronal and molecular basis of quinine-dependent bitter taste signaling in Drosophila larvae

    Directory of Open Access Journals (Sweden)

    Anthi A. Apostolopoulou

    2014-01-01

    Full Text Available Bitter sensing can alert an animal that a specific type of food is potentially harmful for the organism and should not be consumed. However, not all bitter compounds are equally toxic and some bitter tastants may even have a positive valence in certain contexts, such as self-medication. Thus, taste systems in general have likely a higher capacity than just alerting the animal. In this study, we investigate bitter sensing and processing in Drosophila larvae, using quinine, a substance perceived by humans as bitter. We show that the four different behaviors choice, feeding, survival and associative olfactory learning are directly affected by quinine. On the cellular level we show that only 12 gustatory sensory receptor neurons expressing both GR66a and GR33a are required for quinine dependent choice and feeding behavior. Interestingly these neurons are not necessary for quinine dependent survival or associative learning. On the molecular level, only the GR33a receptor but not GR66a is required for quinine dependent choice behavior. Screening for single gustatory sensory receptor neurons that trigger quinine dependent choice behavior revealed that a single GR97a positive neuron located in the peripheral terminal sense organ is necessary and sufficient. Taken together, our study shows for the first time that the elementary chemosensory system of the Drosophila larva can serve as a simple model to understand the neuronal basis of taste information processing on the single cell level with respect to different behavioral outputs.

  20. Comparative study of chloroquine and quinine on malaria rodents and their effects on the mouse testis

    Institute of Scientific and Technical Information of China (English)

    Esmail Abolghasemi; Seyed Hassan Moosa-Kazemi; Maryam Davoudi; Ahmad Reisi; Mohammad Taghi Satvat

    2012-01-01

    Objective: To evaluate the effects of quinine and chloroquine against male mice infected withPlasmodium berghei and their adverse effects on the mice testes. Methods: In this study, 48 adult male mice, (20-25 g), aged 8 to 12 weeks were divided into four groups. This study was carried out from December 2009 until May 2010 in the School of Public Health, Tehran University of Medical Sciences. Results: The results showed that 58.33% of mice treated with chloroquine were completely recovered. Parasitemia was 4% on day 8 when compared to that on day 0, whereas it was 9% on day 9. There was no orchitis found in this group. The mortality of mice after exposing to quinine on day 5 was 8.3%, whereas from day 10 to day 14 it was 91.7%. We found 75% orchitis occurred in quinine treated group. There was a significant difference between quinine and chloroquine effects on the parasite and also mice testes (P<0.05). Conclusions: In this study, It can be concluded that male mice have full resistance to the quinine. Quinine does not only make male mice recover completely, but also cause inflammation on mice testicles tissue.

  1. Protective Effect of Quinine on Chemical Kindling and Passive Avoidance Test in Rats

    Science.gov (United States)

    Faridkia, Zahra; Yaghmaei, Parichehr; Nassiri-Asl, Marjan

    2016-01-01

    Background In humans, convulsive diseases such as temporal lobe epilepsy are usually accompanied by learning and memory impairments. In recent years, the role of gap junction channels as an important target of antiepileptic drugs has been studied and discussed. Quinine, as a gap junction blocker of connexin 36, can abolish ictal epileptiform activity in brain slices. Objectives The role of quinine in memory retrieval in pentylenetetrazole (PTZ)-kindled rats was examined using a step-through passive avoidance task. Methods Forty rats were used in this experimental study in groups of 10 animals. Quinine (15, 30, and 60 mg/kg, i.p.) and PTZ (35 mg/kg, i.p.) were injected into the rats before the start of the learning test. Then, retention tests were conducted after the treatments ended. Results Quinine could attenuate seizure severity at doses of 15, 30 and 60 mg/kg compared with the control at the beginning of the kindling experiment by lowering the mean seizure stages (P 0.05). Conclusions Quinine may decrease the severity of seizure and improve the memory retrieval of animals by inhibiting the gap junction channel. However, further studies are needed to evaluate the molecular mechanism underlying the effects of quinine. PMID:28144451

  2. Clindamycin plus quinine for treating uncomplicated falciparum malaria: a systematic review and meta-analysis

    Directory of Open Access Journals (Sweden)

    Obonyo Charles O

    2012-01-01

    Full Text Available Abstract Background Artemisinin-based combinations are recommended for treatment of uncomplicated falciparum malaria, but are costly and in limited supply. Clindamycin plus quinine is an alternative non-artemisinin-based combination recommended by World Health Organization. The efficacy and safety of clindamycin plus quinine is not known. This systematic review aims to assess the efficacy of clindamycin plus quinine versus other anti-malarial drugs in the treatment of uncomplicated falciparum malaria. Methods All randomized controlled trials comparing clindamycin plus quinine with other anti-malarial drugs in treating uncomplicated malaria were included in this systematic review. Databases searched included: Cochrane Central Register of Controlled Trials, MEDLINE, EMBASE and LILACS. Two authors independently assessed study eligibility, extracted data and assessed methodological quality. The primary outcome measure was treatment failure by day 28. Dichotomous data was compared using risk ratio (RR, in a fixed effects model. Results Seven trials with 929 participants were included. Clindamycin plus quinine significantly reduced the risk of day 28 treatment failure compared with quinine (RR 0.14 [95% CI 0.07 to 0.29], quinine plus sulphadoxine-pyrimethamine (RR 0.17 [95% CI 0.06 to 0.44], amodiaquine (RR 0.11 [95% CI 0.04 to 0.27], or chloroquine (RR 0.11 [95% CI 0.04 to 0.29], but had similar efficacy compared with quinine plus tetracycline (RR 0.33 [95% CI 0.01 to 8.04], quinine plus doxycycline (RR 1.00 [95% CI 0.21 to 4.66], artesunate plus clindamycin (RR 0.57 [95% CI 0.26 to 1.24], or chloroquine plus clindamycin (RR 0.38 [95% CI 0.13 to 1.10]. Adverse events were similar across treatment groups but were poorly reported. Conclusion The evidence on the efficacy of clindamycin plus quinine as an alternative treatment for uncomplicated malaria is inconclusive. Adequately powered trials are urgently required to compare this combination with

  3. FT-Raman study of quinine aqueous solutions with varying pH: 2D correlation study

    Science.gov (United States)

    Wesełucha-Birczyńska, Aleksandra

    2007-01-01

    Quinine (C 20H 24N 2O 2) is one of the best known, for its antimalarial activity, Cinchona alkaloid. In the current study 2D correlation method was applied to analyze FT-Raman spectra of quinine aqueous solutions with varying pH, which was regarded as an external perturbation. Protonation appears to be the main cause leading to the emergence of cross peaks in the synchronous and asynchronous correlation maps. One should know that protonation process is an important step associated with quinine antimalarial activity. Methoxy group manifests its presence by creation of the respective correlation peaks and seems to be significant for quinine mode of action.

  4. Malaria and quinine resistance: a medical and scientific issue between Brazil and Germany (1907-19).

    Science.gov (United States)

    da Silva, André Felipe Cândido; Benchimol, Jaime Larry

    2014-01-01

    This article addresses the discussion about quinine-resistant malaria plasmodium in the early decades of the twentieth century. Observed by Arthur Neiva in Rio de Janeiro in 1907, the biological and social resistance of malaria sufferers to preventive and curative treatment with quinine was corroborated three years later by Oswaldo Cruz during the construction of the Madeira-Mamoré Railway in the Brazilian Amazon. Likewise in 1910, ailing German workers were transferred from Brazil to Hamburg's Institute for Maritime and Tropical Diseases, where quinine resistance was confirmed by Bernard Nocht and Heinrich Werner. When the First World War saw failures in treating and preventing malaria with quinine along with violent outbreaks of the disease on the Turkish and Balkan fronts, resistance to this alkaloid became the topic of the day within the field of experimental medicine in Germany. New attempts were made to account for the resistance, especially by the physician Ernst Rodenwaldt, who explored the topic by applying modern theories on heredity. The present article offers a preliminary survey and analysis of pronouncements about quinine resistance, shedding new light on the circulation of knowledge in the field of tropical medicine.

  5. Structure-affinity relationship of the cocaine-binding aptamer with quinine derivatives.

    Science.gov (United States)

    Slavkovic, Sladjana; Altunisik, Merve; Reinstein, Oren; Johnson, Philip E

    2015-05-15

    In addition to binding its target molecule, cocaine, the cocaine-binding aptamer tightly binds the alkaloid quinine. In order to understand better how the cocaine-binding aptamer interacts with quinine we have used isothermal titration calorimetry-based binding experiments to study the interaction of the cocaine-binding aptamer to a series of structural analogs of quinine. As a basis for comparison we also investigated the binding of the cocaine-binding aptamer to a set of cocaine metabolites. The bicyclic aromatic ring on quinine is essential for tight affinity by the cocaine-binding aptamer with 6-methoxyquinoline alone being sufficient for tight binding while the aliphatic portion of quinine, quinuclidine, does not show detectable binding. Compounds with three fused aromatic rings are not bound by the aptamer. Having a methoxy group at the 6-position of the bicyclic ring is important for binding as substituting it with a hydrogen, an alcohol or an amino group all result in lower binding affinity. For all ligands that bind, association is driven by a negative enthalpy compensated by unfavorable binding entropy.

  6. Electrochemical studies of quinine in surfactant media using hanging mercury drop electrode: a cyclic voltammetric study.

    Science.gov (United States)

    Dar, Riyaz Ahmad; Brahman, Pradeep Kumar; Tiwari, Sweety; Pitre, Krishna Sadashiv

    2012-10-01

    The electrochemical behavior of quinine was investigated by cyclic voltammetry (CV) and square wave voltammetry (SWV) using surfactant. The reduction peak current of quinine increases remarkably in presence of 1% CTAB. Its electrochemical behavior is quasi-reversible in the Britton-Robinson buffers of pH 10.38 by exhibiting the well-defined single cathodic and anodic waves and the ratio of I(p)(a)/I(p)(c) approaching one at the scan rate of 500 mVs(-1). On the basis of CV, SWV and Coulometry, electrochemical reduction mechanism of quinine has been proposed which has shown that protonation occurs on the nitrogen of the quinoline moiety. Linearity was obtained when the peak currents (I(p)) were plotted against concentrations of quinine in the range of 30.0-230.0 ng mL(-1) with a detection limit of 0.132 ng mL(-1) in SWV and 90.0-630.0 ng mL(-1) with a detection limit of 0.238 ng mL(-1) in DPV. Fast and sensitive SWV has been applied for the quantitative analysis of quinine in bark of Cinchona sp. and in soft drinks and a good recovery was obtained. The accuracy and precision of the method are determined and validated statistically. No interferences from other food additives were observed. The relative standard deviation for intraday and interday assay was 0.89 and 0.73% (n=3) respectively.

  7. Quinine, mosquitoes and empire: reassembling malaria in British India, 1890-1910.

    Science.gov (United States)

    Roy, Rohan Deb

    2013-01-01

    The drug quinine figured as an object of enforced consumption in British India between the late 1890s and the 1910s, when the corresponding diagnostic category malaria itself was redefined as a mosquito-borne fever disease. This article details an overlapping milieu in which quinine, mosquitoes and malaria emerged as intrinsic components of shared and symbiotic histories. It combines insights from new imperial histories, constructivism in the histories of medicine and literature about non-humans in science studies to examine the ways in which histories of insects, drugs, disease and empire interacted and shaped one another. Firstly, it locates the production of historical intimacies between quinine, malaria and mosquitoes within the exigencies and apparatuses of imperial rule. In so doing, it explores the intersections between the worlds of colonial governance, medical knowledge, vernacular markets and pharmaceutical business. Secondly, it outlines ways to narrate characteristics and enabling properties of non-humans (such as quinines and mosquitoes) while retaining a constructivist critique of scientism and empire. Thirdly, it shows how empire itself was reshaped and reinforced while occasioning the proliferation of categories and entities like malaria, quinine and mosquitoes.

  8. Comparative Efficacy of Quinine and Artesunate in the Treatment of Severe Malaria : A Randomized Controlled Trial

    Directory of Open Access Journals (Sweden)

    Nigil Haroon, Kalpesh Amichandwala, Mahesah G. Solu

    2005-01-01

    Full Text Available There is a paucity of head to head studies of quinine and artesunate in Indian patients. A consensus onthe best treatment for severe malaria is lacking. To compare the efficacy of quinine and artesunate insevere falciparum malaria. This is a prospective randomized controlled, opened-labeled trial, conductedin a tertiary care center in western India. Thiry-five patients above the age of 18 years, with asexualforms of plasmodium falciparum in the peripheral smear and satisfying the WHO criteria for severemalaria, formed the study population. On randomization 18 received quinine and 17 artesunate. Theend points of the study were parasite clearance time (PCT, fever clearance time (FCT, coma resolutiontime (CRT, adverse effects of the drugs and death. The FCT (p 0.023 and PCT (p=0.04 were lowerwith artesunate. The CRT was lower with quinine (p 0.03. One patient in each arm succumbed to theillness (p 0.96. There was no side effect warranting a crossover to the other arm. Thus, quinine is asgood as artesunate in the treatment of severe falciparum malaria.

  9. Preliminary study of quinine pharmacokinetics in pregnant women with malaria-HIV co-infection.

    Science.gov (United States)

    Kayentao, Kassoum; Guirou, Etienne A; Doumbo, Ogobara K; Venkatesan, Meera; Plowe, Christopher V; Parsons, Teresa L; Hendrix, Craig W; Nyunt, Myaing M

    2014-03-01

    Pregnant women bear the greatest burden of malaria-human immunodeficiency virus co-infection. Previous studies suggest that interaction with antiretroviral drugs may compromise antimalarial pharmacokinetics and treatment outcomes. We conducted a preliminary clinical study to assess quinine pharmacokinetics in Malian pregnant women with acute malaria who reported taking nevirapine-based antiretroviral therapy. Of seven women, six had stable concentrations of nevirapine in the plasma and one had none. Quinine concentrations were lower, and its metabolite 3-hydroxyquinine higher, in the six women with nevirapine than in the one without, and quinine concentrations were below the recommended therapeutic range in 50% of the women. This preliminary observation warrants further research to understand the impact of long-term antiretroviral therapy on the treatment of acute malaria.

  10. Preparation and evaluation of novel chiral stationary phases based on quinine derivatives comprising crown ether moieties.

    Science.gov (United States)

    Wang, Dongqiang; Zhao, Jianchao; Wu, Haixia; Wu, Haibo; Cai, Jianfeng; Ke, Yanxiong; Liang, Xinmiao

    2015-01-01

    The C9-position of quinine was modified by meta- or para-substituted benzo-18-crown-6, and immobilized on 3-mercaptopropyl-modified silica gel through the radical thiol-ene addition reaction. These two chiral stationary phases were evaluated by chiral acids, amino acids, and chiral primary amines. The crown ether moiety on the quinine anion exchanger provided a ligand-exchange site for primary amino groups, which played an important role in the retention and enantioselectivity for chiral compounds containing primary amine groups. These two stationary phases showed good selectivity for some amino acids. The complex interaction between crown ether and protonated primary amino group was investigated by the addition of inorganic salts such as LiCl, NH4Cl, NaCl, and KCl to the mobile phase. The resolution results showed that the simultaneous interactions between two function moieties (quinine and crown ether) and amino acids were important for the chiral separation.

  11. Effects of quinine on the mechanical frequency response of the cupula in the fish lateral line.

    Science.gov (United States)

    van Netten, S M; Karlsson, K K; Khanna, S M; Flock, A

    1994-03-01

    Quinine induces changes in the motion of the cupula in the lateral line canal of the African knife-fish in response to sinusoidal water movements. Two different phases in the action of quinine on the cupular frequency response can be discerned. In the first phase the best frequency, i.e., the frequency at which the cupular vibratory displacement is maximal in response to constant-amplitude sinusoidal canal fluid displacement, shifts toward higher frequencies. During this phase, lasting about 70-100 min, the best frequency increases by a factor between 1.3 and 1.5. In the second phase, during roughly the following 90 min, the best frequency decreases gradually to a value 0.3-0.5 times that observed before the application of quinine.

  12. Use of quinine and mortality-risk in patients with heart failure--a Danish nationwide observational study

    DEFF Research Database (Denmark)

    Gjesing, Anne; Gislason, Gunnar H; Christensen, Stefan B;

    2015-01-01

    PURPOSE: Leg cramps are common in patients with heart failure. Quinine is frequently prescribed in low doses to these patients, but safety of this practice is unknown. We studied the outcomes associated with use of quinine in a nationwide cohort of patients with heart failure. METHODS: Through in...

  13. EFFECTS OF QUININE ON THE MECHANICAL FREQUENCY-RESPONSE OF THE CUPULA IN THE FISH LATERAL-LINE

    NARCIS (Netherlands)

    van Netten, S.M.; KARLSSON, KK; KHANNA, SM; FLOCK, A

    1994-01-01

    Quinine induces changes in the motion of the cupula in the lateral line canal of the African knife-fish in response to sinusoidal water movements. Two different phases in the action of quinine on the cupular frequency response can be discerned. In the first phase the best frequency, i.e., the freque

  14. Structural basis for quinine-dependent antibody binding to platelet integrin αIIbβ3.

    Science.gov (United States)

    Zhu, Jianghai; Zhu, Jieqing; Bougie, Daniel W; Aster, Richard H; Springer, Timothy A

    2015-10-29

    Drug-induced immune thrombocytopenia (DITP) is caused by antibodies that react with specific platelet-membrane glycoproteins when the provoking drug is present. More than 100 drugs have been implicated as triggers for this condition, quinine being one of the most common. The cause of DITP in most cases appears to be a drug-induced antibody that binds to a platelet membrane glycoprotein only when the drug is present. How a soluble drug promotes binding of an otherwise nonreactive immunoglobulin to its target, leading to platelet destruction, is uncertain, in part because of the difficulties of working with polyclonal human antibodies usually available only in small quantities. Recently, quinine-dependent murine monoclonal antibodies were developed that recognize a defined epitope on the β-propeller domain of the platelet integrin αIIb subunit (GPIIb) only when the drug is present and closely mimic the behavior of antibodies found in human patients with quinine-induced thrombocytopenia in vitro and in vivo. Here, we demonstrate specific, high-affinity binding of quinine to the complementarity-determining regions (CDRs) of these antibodies and define in crystal structures the changes induced in the CDR by this interaction. Because no detectable binding of quinine to the target integrin could be demonstrated in previous studies, the findings indicate that a hybrid paratope consisting of quinine and reconfigured antibody CDR plays a critical role in recognition of its target epitope by an antibody and suggest that, in this type of drug-induced immunologic injury, the primary reaction involves binding of the drug to antibody CDRs, causing it to acquire specificity for a site on a platelet integrin.

  15. Mechanism of quinine-dependent monoclonal antibody binding to platelet glycoprotein IIb/IIIa.

    Science.gov (United States)

    Bougie, Daniel W; Peterson, Julie; Rasmussen, Mark; Aster, Richard H

    2015-10-29

    Drug-dependent antibodies (DDAbs) that cause acute thrombocytopenia upon drug exposure are nonreactive in the absence of the drug but bind tightly to a platelet membrane glycoprotein, usually α(IIb)/β3 integrin (GPIIb/IIIa) when the drug is present. How a drug promotes binding of antibody to its target is unknown and is difficult to study with human DDAbs, which are poly-specific and in limited supply. We addressed this question using quinine-dependent murine monoclonal antibodies (mAbs), which, in vitro and in vivo, closely mimic antibodies that cause thrombocytopenia in patients sensitive to quinine. Using surface plasmon resonance (SPR) analysis, we found that quinine binds with very high affinity (K(D) ≈ 10⁻⁹ mol/L) to these mAbs at a molar ratio of ≈ 2:1 but does not bind detectably to an irrelevant mAb. Also using SPR analysis, GPIIb/IIIa was found to bind monovalently to immobilized mAb with low affinity in the absence of quinine and with fivefold greater affinity (K(D) ≈ 2.2 × 10⁻⁶) when quinine was present. Measurements of quinine-dependent binding of intact mAb and fragment antigen-binding (Fab) fragments to platelets showed that affinity is increased 10 000- to 100 000-fold by bivalent interaction between antibody and its target. Together, the findings indicate that the first step in drug-dependent binding of a DDAb is the interaction of the drug with antibody, rather than with antigen, as has been widely thought, where it induces structural changes that enhance the affinity/specificity of antibody for its target epitope. Bivalent binding may be essential for a DDAb to cause thrombocytopenia.

  16. Resolution of enantiomers of novel C2 -symmetric aminobisphosphinic acids via diastereomeric salt formation with quinine.

    Science.gov (United States)

    Kaboudin, Babak; Faghihi, Mohammad Reza; Kazemi, Foad; Yokomatsu, Tsutomu

    2015-01-01

    C2 -symmetric N,N-bis(phosphinomethyl)amines were prepared by the thermal reaction of aromatic aldehydes with ammonia and hypophosphorus acid as previously described. Both enantiomers of C2 -symmetric N,N-bis(phosphinomethyl)amine were obtained in a high enantiomeric purity through the diastereomeric salt formation with (-)-quinine, and subsequent fractional crystallization. X-ray crystallographic analysis of one of the diastereomeric salts clearly revealed that (-)-quinine could be an efficient resolving agent for obtaining the single enantiomer (R,R)-N,N-bis(phosphinomethyl)amine.

  17. Free volume effects on the fluorescence characteristics of sol-gel glasses doped with quinine sulphate

    Science.gov (United States)

    Meneses-Nava, M. A.; Barbosa-García, O.; Díaz-Torres, L. A.; Chávez-Cerda, S.; King, T. A.

    1999-12-01

    The broadening of the absorption and fluorescence spectra and the red shift of the fluorescence maximum of quinine sulfate doped sol-gel glasses, before and after PMMA polymer impregnation, are investigated at different concentrations. The fluorescence decay of the quinine sulfate doped samples does not fit to a single exponential, as it does in ethanol solutions. We found that a double exponential gives a good fit to the obtained results. Introduction of solvent to fill the pores of the matrix does not only have the same effect as the polymer, but also reveals the strong attachment of the molecules to the pore walls and the influence of the interaction with the cage.

  18. Treatment of imported severe malaria with artesunate instead of quinine - more evidence needed?

    Directory of Open Access Journals (Sweden)

    Grobusch Martin P

    2011-09-01

    Full Text Available Abstract Rapid and fast acting anti-malarials are essential to treat severe malaria. Quinine has been the only option for parenteral therapy until recently. While current evidence shows that intravenous artesunate is more effective than quinine in treating severe malaria in endemic countries, some questions remain regarding safety profiles and drug resistance. For imported severe malaria, additional unanswered questions are related to generalizability of the findings from endemic countries and to legal aspects, as there is no Good Manufacturing Practice-conform drug available yet. Here, the implications of existing evidence for the treatment of imported severe malaria are discussed.

  19. Behavioural analyses of quinine processing in choice, feeding and learning of larval Drosophila.

    Directory of Open Access Journals (Sweden)

    Amira El-Keredy

    Full Text Available Gustatory stimuli can support both immediate reflexive behaviour, such as choice and feeding, and can drive internal reinforcement in associative learning. For larval Drosophila, we here provide a first systematic behavioural analysis of these functions with respect to quinine as a study case of a substance which humans report as "tasting bitter". We describe the dose-effect functions for these different kinds of behaviour and find that a half-maximal effect of quinine to suppress feeding needs substantially higher quinine concentrations (2.0 mM than is the case for internal reinforcement (0.6 mM. Interestingly, in previous studies (Niewalda et al. 2008, Schipanski et al 2008 we had found the reverse for sodium chloride and fructose/sucrose, such that dose-effect functions for those tastants were shifted towards lower concentrations for feeding as compared to reinforcement, arguing that the differences in dose-effect function between these behaviours do not reflect artefacts of the types of assay used. The current results regarding quinine thus provide a starting point to investigate how the gustatory system is organized on the cellular and/or molecular level to result in different behavioural tuning curves towards a bitter tastant.

  20. Aqueous two phase system based on ionic liquid for isolation of quinine from human plasma sample.

    Science.gov (United States)

    Flieger, J; Czajkowska-Żelazko, A

    2015-01-01

    Aqueous two phase system was applied for selective extraction of quinine from human plasma. Bi-phase was constructed from ionic liquid: butyl-methyl-imidazolium chloride after addition kosmotropic salts K₃PO₄ or KH₂PO₄. Quinine was determined in plasma samples after drinking of tonic containing quinine. Determination was performed by HPLC on 5-μm Zorbax SB-CN column and eluent containing 40% acetonitrile (v/v), 20 mM phosphate buffer at pH 3 and 40 mM NaPF₆ using external standard method. The spectrophotometric detection was set λ=214 nm. Selective fluorescence detection was performed at excitation of 325 nm and emission of 375 nm. Proposed strategy provides suitable sample purification and gives extraction yields in the range of 89-106%. The determination coefficient (R(2)) has a value ≥0.997 in the range of 50-800 ng/ml quinine concentration. The limit of quantification was set at 27.9 ng/ml and the detection limit was found to be 8.4 ng/ml under fluorescence detection.

  1. Dynamic fluorescence quenching of quinine sulfate dication by chloride ion in ionic and neutral micellar environments

    Science.gov (United States)

    Joshi, Sunita; Varma Y, Tej Varma; Pant, Debi D.

    2014-04-01

    Fluorescence quenching of Quinine sulfate dication (QSD) by chloride-ion (Cl-) in micellar environments of anionic, sodium dodecyl sulfate (SDS), cationic, cetyltrimethylammonium bromide (CTAB) and neutral, triton X-100 (TX-100) in aqueous phase has been investigated by time-resolved and steady- state fluorescence measurements. The quenching follows linear Stern-Volmer relation in micellar solutions and is dynamic in nature.

  2. Assay of Cysteine in Human Serum with Quinine-Ce4+ Chemiluminescence System

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    A sensitive and selective chemiluminescence (CL) method was developed for the determination of cysteine. This method is based on that the weak CL of cysteine oxidized with cerium (IV) can be greatly enhanced by quinine, and the total cysteine in human serum can be detected through simply diluting with water, showing a simpler analytical characteristic.

  3. Motivation for alcohol becomes resistant to quinine adulteration after 3 to 4 months of intermittent alcohol self-administration.

    Science.gov (United States)

    Hopf, Frederic Woodward; Chang, Shao-Ju; Sparta, Dennis R; Bowers, Michael S; Bonci, Antonello

    2010-09-01

    Continued consumption of alcohol despite deleterious consequences is a hallmark of alcoholism and represents a critical challenge to therapeutic intervention. Previous rat studies showed that enduring alcohol self-administration despite pairing alcohol with normally aversive stimuli was only observed after very long-term intake (>8 months). Aversion-resistant alcohol intake has been previously interpreted to indicate pathological or compulsive motivation to consume alcohol. However, given the time required to model compulsive alcohol seeking in previous studies, there is considerable interest in developing more efficient and quantitative rodent models of aversion-resistant alcohol self-administration. Outbred Wistar rats underwent 3 to 4 months or approximately 1.5 months of intermittent, home-cage, two-bottle access (IAA) to 20% alcohol (v/v) or water. Then, after brief operant training, the effect of the bitter-tasting quinine (0.1 g/l) on the motivation to seek alcohol was quantified via progressive ratio (PR). Motivation for quinine-adulterated 2% sucrose under PR was assayed in a separate cohort of 3 to 4 months IAA rats. The effects of quinine on home-cage alcohol consumption in IAA rats and rats with continuous access to alcohol were also examined. Finally, a dose-response for quinine taste preference in IAA and continuous-access animals was determined. Motivation for alcohol after 3 to 4 months IAA, measured using an operant PR procedure, was not altered by adulteration of alcohol with 0.1 g/l quinine. In contrast, after 3 to 4 months of IAA, motivation for sucrose under PR was significantly reduced by adulteration of sucrose with 0.1 g/l quinine. In addition, motivation for alcohol after only approximately 1.5 months IAA was significantly reduced by adulteration of alcohol with 0.1 g/l quinine. Furthermore, home-cage alcohol intake by IAA rats was insensitive to quinine at concentrations (0.01, 0.03 g/l) that significantly reduced alcohol drinking in

  4. Conformational analysis of quinine and its pseudo enantiomer quinidine: a combined jet-cooled spectroscopy and vibrational circular dichroism study.

    Science.gov (United States)

    Sen, Ananya; Bouchet, Aude; Lepère, Valeria; Le Barbu-Debus, Katia; Scuderi, D; Piuzzi, F; Zehnacker-Rentien, A

    2012-08-16

    Laser-desorbed quinine and quinidine have been studied in the gas phase by combining supersonic expansion with laser spectroscopy, namely, laser-induced fluorescence (LIF), resonance-enhanced multiphoton ionization (REMPI), and IR-UV double resonance experiments. Density funtional theory (DFT) calculations have been done in conjunction with the experimental work. The first electronic transition of quinine and quinidine is of π-π* nature, and the studied molecules weakly fluoresce in the gas phase, in contrast to what was observed in solution (Qin, W. W.; et al. J. Phys. Chem. C2009, 113, 11790). The two pseudo enantiomers quinine and quinidine show limited differences in the gas phase; their main conformation is of open type as it is in solution. However, vibrational circular dichroism (VCD) experiments in solution show that additional conformers exist in condensed phase for quinidine, which are not observed for quinine. This difference in behavior between the two pseudo enantiomers is discussed.

  5. Recrudescence of Plasmodium falciparum malaria contracted in Lombok, Indonesia after quinine/doxycycline and mefloquine: case report.

    Science.gov (United States)

    Tish, K N; Pillans, P I

    1997-07-11

    A patient is reported who contracted Plasmodium falciparum malaria in Lombok, Indonesia. The infection recrudesced after quinine/doxycycline and mefloquine. Treatment with halofantrine was successful after he developed cerebral malaria with recovery.

  6. A HECT ubiquitin-protein ligase as a novel candidate gene for altered quinine and quinidine responses in Plasmodium falciparum.

    Science.gov (United States)

    Sanchez, Cecilia P; Liu, Chia-Hao; Mayer, Sybille; Nurhasanah, Astutiati; Cyrklaff, Marek; Mu, Jianbing; Ferdig, Michael T; Stein, Wilfred D; Lanzer, Michael

    2014-05-01

    The emerging resistance to quinine jeopardizes the efficacy of a drug that has been used in the treatment of malaria for several centuries. To identify factors contributing to differential quinine responses in the human malaria parasite Plasmodium falciparum, we have conducted comparative quantitative trait locus analyses on the susceptibility to quinine and also its stereoisomer quinidine, and on the initial and steady-state intracellular drug accumulation levels in the F1 progeny of a genetic cross. These data, together with genetic screens of field isolates and laboratory strains associated differential quinine and quinidine responses with mutated pfcrt, a segment on chromosome 13, and a novel candidate gene, termed MAL7P1.19 (encoding a HECT ubiquitin ligase). Despite a strong likelihood of association, episomal transfections demonstrated a role for the HECT ubiquitin-protein ligase in quinine and quinidine sensitivity in only a subset of genetic backgrounds, and here the changes in IC50 values were moderate (approximately 2-fold). These data show that quinine responsiveness is a complex genetic trait with multiple alleles playing a role and that more experiments are needed to unravel the role of the contributing factors.

  7. Optimization of Extraction Conditions and HPTLC - UV Method for Determination of Quinine in Different Extracts of Cinchona species Bark

    Directory of Open Access Journals (Sweden)

    Dharam C. Jain

    2008-10-01

    Full Text Available A simple, precise and accurate high-performance thin-layer chromatographic method has been established for quantitative determination of quinine. Conditions were also optimized for best possible extraction of quinine via varying concentrations of diethyl amine in different solvents (n-hexane, chloroform, ethyl acetate and methanol for maximum recovery of quinine. Methanol modified with 20 % DEA found to be best for highest possible recovery of target analyte quinine. Chromatographic separation of quinine was performed on silica gel 60 F 254 HPTLC plates with ethyl acetate : diethyl amine in the proportion 88 : 12 (v/v, as mobile phase. The determination was carried out using the densitometric absorbance mode at 236 nm. Quinine response was found to be linear over the range 4–24 μg spot −1. The HPTLC method was evaluated in terms of specificity, precision, reproducibility, LOD – LOQ and robustness. Beside these parameters, number of theoretical plates and flow constant were also included as a part of validation

  8. Preparation,characterization and properties studies of quinine-imprinted polymer in the aqueous phase

    Institute of Scientific and Technical Information of China (English)

    He Jianfeng; Liu Lan; Yang Guilan; Deng Qinying

    2006-01-01

    The uniform-sized spherical molecularly imprinted polymers were successfully prepared through molecular imprinting technology by two-step seed swelling and mini-emulsion polymerization in the aqueous condition using quinine as template molecules and methacrylic acid (MAA)as functional monomer.The polymers were characterized by IR spectra,thermal-weight analysis,scanning electron microscope and laser particle size analysis.The properties of imprinted polymers were investigated in different organic phases and aqueous media.In the organic media,results suggested that polar interactions(hydrogen bonding,ionic interactions)between acidic monomer/polymer and template molecules are mainly responsible for the binding and recognition;whereas in the aqueous medium,a considerable recognition effect was also obtained where the ionic(electrostatic)interaction and hydrophobic interaction play an important role.The experiments of binding different substrates indicated that the MIPs possessed an excellent rebinding ability and inherent selectivity to quinine.

  9. Binding Reaction of Hemin with Chloroquine, Quinine and Quinidine in Water-propylene Glycol Mixture

    Institute of Scientific and Technical Information of China (English)

    MAVAKALA,B.K; NLANDU,B.B.; MPIANA,P.T.; GUSHIMANA,Z.Y.; 尉志武

    2003-01-01

    the interaction of hemin with chloroquine,quinine and quinidine was investigated in 50% water-propylene glycol mixture at pH=9,8.1,7.4 and 6.8using a spectrophotometric method.The data could be well fitted into a model consistent with the formation of a 1:1 complex between the reacting partners.In addition,the results indicated that hemin complexed more strongly with quinidine than with chloroquine and quinine,and the binding constants were pH-dependent.Moreover,it was proved that the water-propylene glycol mixture is well suitable to the study of the systems containing hemin and quinolinebased drugs.

  10. Iron(III) protoporphyrin IX complexes of the antimalarial Cinchona alkaloids quinine and quinidine.

    Science.gov (United States)

    de Villiers, Katherine A; Gildenhuys, Johandie; le Roex, Tanya

    2012-04-20

    The antimalarial properties of the Cinchona alkaloids quinine and quinidine have been known for decades. Surprisingly, 9-epiquinine and 9-epiquinidine are almost inactive. A lack of definitive structural information has precluded a clear understanding of the relationship between molecular structure and biological activity. In the current study, we have determined by single crystal X-ray diffraction the structures of the complexes formed between quinine and quinidine and iron(III) protoporphyrin IX (Fe(III)PPIX). Coordination of the alkaloid to the Fe(III) center is a key feature of both complexes, and further stability is provided by an intramolecular hydrogen bond formed between a propionate side chain of Fe(III)PPIX and the protonated quinuclidine nitrogen atom of either alkaloid. These interactions are believed to be responsible for inhibiting the incorporation of Fe(III)PPIX into crystalline hemozoin during its in vivo detoxification. It is also possible to rationalize the greater activity of quinidine compared to that of quinine.

  11. Two different modes for copper(II ion coordination to quinine-type ligands

    Directory of Open Access Journals (Sweden)

    Rey Nicolás A.

    2006-01-01

    Full Text Available Three new copper(II complexes with the ligands quinuclidine [Cu(C7H13N2(OH2Cl]Cl.2H 2O (1, quinine [Cu(C20H23O2N2(OH 22]ClO4 (2, and hydroquinidine [Cu(C20H27O2N2(OH 2 Cl2]Cl.fraction one-halfH2O (3 have been isolated and characterized. The binding sites were assigned on the basis of vibrational spectroscopy, electron paramagnetic resonance, and thermal analysis results. The possibility of the involvement of the quinuclidinic nitrogen in the coordination was evidenced in complex 1, in which copper(II is coordinated to two quinuclidine molecules. In the case of quinine-type ligands, if the starting material is deprotonated in both nitrogens, copper(II coordination occurs through the quinuclidinic nitrogen, as in complex 2. In contrast, if the starting material is protonated in the quinuclidinic nitrogen the binding site is the quinolinic nitrogen, as in complex 3. Therefore, both nitrogens of quinine-type ligands constitute binding sites for copper(II ions.

  12. [Aqueous and salt solutions of quinine of low concentrations: self-organization, physicochemical properties and actions on the electrical characteristics of neurons].

    Science.gov (United States)

    Murtazina, L I; Ryzhkina, I S; Mishina, O A; Andrianov, V V; Bogodvid, T Kh; Gaĭnutdinov, Kh L; Muranova, L N; Konovalov, A I

    2014-01-01

    Self-organization, the physicochemical properties of aqueous and salt solutions of quinine and the effects of salt quinine solutions in a wide range of concentrations (1 x 10(-22) - 1 x 10(-3) M) on the electrical characteristics of the edible snail's identified neurons were studied. Similar non-monotonic concentration dependencies of physicochemical properties of aqueous and salt quinine solutions at low concentrations are obtained. This allows of predicting the occurrence of biological effects at low concentrations of quinine solutions. Intrinsic (within 5% of the interval) changes in membrane potential, the amplitude and duration of the neuron action potential under the influence of quinine salt solutions at concentrations of quinine of 1 x 10(-20), 1 x 10(-18), 1 x 10(-10) M are found. For these concentrations the extreme values of specific conductivity and pH are shown.

  13. Regulation of Rac1 GTPase activity by quinine through G-protein and bitter taste receptor T2R4.

    Science.gov (United States)

    Sidhu, Crystal; Jaggupilli, Appalaraju; Chelikani, Prashen; Bhullar, Rajinder P

    2017-02-01

    Rac1 belongs to the Rho family of small GTPases and regulates actin cytoskeleton reorganization. T2R4 is a bitter taste receptor belonging to the G protein-coupled receptor family of proteins. In addition to mediating bitter taste perception from the tongue, T2R4s are found in extra-oral tissues, e.g., nasal epithelium, airways, brain, testis suggesting a much broader physiological function for these receptors. Anti-malarial drug and a bitter tasting compound, quinine, is a known agonist for T2R4, whereas BCML (Nα,Nα-Bis(carboxymethyl)-L-lysine) acts as an inverse agonist. Using western blot and Ca(++) mobilization assays, the effects of quinine on Rac1 activity in HEK293T cells stably expressing T2R4/Gα16/44, T2R4, or Gα16/44 and transiently transfected with HA-Rac1 were investigated. Quinine treatment caused a significant reduction in the amount of active Rac1, whereas in the presence of BCML, quinine failed to cause any significant change in active Rac1. No significant change in Rac1 activity was observed in BAPTA-AM plus quinine-treated Gα16/44 cells, suggesting possibility of a pathway in addition to the canonical Ca(++)-dependent pathway. A noticeable role for Gα16/44 independent of T2R4 is observed in quinine-mediated Rac1 inactivation. Further, a significant difference in quinine-induced Ca(++) response in T2R4/Gα16/44 or T2R4 cells was observed validating the partial role of calcium and importance of Gα16/44. This study is the first to show an inhibitory downstream action of a T2R4 agonist on Rac1 function. Further investigation will help in better understanding the downstream signal transduction network of T2R4 and its extra-oral physiological roles.

  14. The cost of quinine Cinchona pubescens control on Santa Cruz Island, Galapagos

    OpenAIRE

    Buddenhagen, Chris; Yanez, Patricio

    2005-01-01

    We analyse the cost of controlling the invasive quinine tree Cinchona pubescens Vahl in the highlands of Santa Cruz Island, Galapagos. Control costs in ten 400 m2 plots formed the basis for estimating the cost of control over the whole island. In the plots, densities were 2100–24,000 stems/ha (stems >150 cm tall) and 55,000–138,000 stems/ha (all size classes combined). Control involved uprooting small plants, and applying of a mix of metsulfuron methyl and picloram to cut stumps or to mach...

  15. Plasmodium falciparum Na+/H+ Exchanger 1 Transporter Is Involved in Reduced Susceptibility to Quinine

    OpenAIRE

    Henry, Maud; Briolant, Sébastien; Zettor, Agnès; Pelleau, Stéphane; Baragatti, Meili; Baret, Eric; Mosnier, Joel; Amalvict, Rémy; Fusai, Thierry; Rogier, Christophe; Pradines, Bruno

    2009-01-01

    Polymorphisms in the Plasmodium falciparum crt (Pfcrt), Pfmdr1, and Pfmrp genes were not significantly associated with quinine (QN) 50% inhibitory concentrations (IC50s) in 23 strains of Plasmodium falciparum. An increased number of DNNND repeats in Pfnhe-1 microsatellite ms4760 was associated with an increased IC50 of QN (P = 0.0007). Strains with only one DNNND repeat were more susceptible to QN (mean IC50 of 154 nM). Strains with two DNNND repeats had intermediate susceptibility to QN (mea...

  16. Access to artesunate-amodiaquine, quinine and other anti-malarials: policy and markets in Burundi

    Directory of Open Access Journals (Sweden)

    Dismas Baza

    2011-02-01

    Full Text Available Abstract Background Malaria is the leading cause of morbidity and mortality in post-conflict Burundi. To counter the increasing challenge of anti-malarial drug resistance and improve highly effective treatment Burundi adopted artesunate-amodiaquine (AS-AQ as first-line treatment for uncomplicated Plasmodium falciparum malaria and oral quinine as second-line treatment in its national treatment policy in 2003. Uptake of this policy in the public, private and non-governmental (NGO retail market sectors of Burundi is relatively unknown. This study was conducted to evaluate access to national policy recommended anti-malarials. Methods Adapting a standardized methodology developed by Health Action International/World Health Organization (HAI/WHO, a cross-sectional survey of 70 (24 public, 36 private, and 10 NGO medicine outlets was conducted in three regions of Burundi, representing different levels of transmission of malaria. The availability on day of the survey, the median prices, and affordability (in terms of number of days' wages to purchase treatment of AS-AQ, quinine and other anti-malarials were calculated. Results Anti-malarials were stocked in all outlets surveyed. AS-AQ was available in 87.5%, 33.3%, and 90% of public, private, and NGO retail outlets, respectively. Quinine was the most common anti-malarial found in all outlet types. Non-policy recommended anti-malarials were mainly found in the private outlets (38.9% compared to public (4.2% and NGO (0% outlets. The median price of a course of AS-AQ was US$0.16 (200 Burundi Francs, FBu for the public and NGO markets, and 3.5-fold higher in the private sector (US$0.56 or 700 FBu. Quinine tablets were similarly priced in the public (US$1.53 or 1,892.50 FBu, private and NGO sectors (both US$1.61 or 2,000 FBu. Non-policy anti-malarials were priced 50-fold higher than the price of AS-AQ in the public sector. A course of AS-AQ was affordable at 0.4 of a day's wage in the public and NGO sectors

  17. Motivation for alcohol becomes resistant to quinine adulteration after 3-4 months of intermittent alcohol self-administration

    Science.gov (United States)

    Hopf, F. Woodward; Chang, Shao-Ju; Sparta, Dennis R.; Bowers, M. Scott; Bonci, Antonello

    2010-01-01

    Background Continued consumption of alcohol despite deleterious consequences is a hallmark of alcoholism and represents a critical challenge to therapeutic intervention. Previous rat studies showed that enduring alcohol self-administration despite pairing alcohol with normally aversive stimuli was only observed after very long-term intake (> 8 months). Aversion-resistant alcohol intake has been previously interpreted to indicate pathological or compulsive motivation to consume alcohol. However, given the time required to model compulsive alcohol seeking in previous studies, there is considerable interest in developing more efficient and quantitative rodent models of aversion-resistant alcohol self-administration. Methods Outbred Wistar rats underwent 3-4 months or ∼1.5 months of intermittent, home-cage, two-bottle access (IAA) to 20% alcohol (v/v) or water. Then, after brief operant training, the effect of the bitter-tasting quinine (0.1 g/L) on the motivation of to seek alcohol was quantified via progressive ratio (PR). Motivation for quinine-adulterated 2% sucrose under PR was assayed in a separate cohort of 3-4 months IAA rats. The effects of quinine on home-cage alcohol consumption in IAA rats and rats with continuous access to alcohol were also examined. Finally, a dose-response for quinine taste preference in IAA and continuous-access animals was determined. Results Motivation for alcohol after 3-4 months IAA, measured using an operant PR procedure, was not altered by adulteration of alcohol with 0.1 g/L quinine. In contrast, after 3-4 month of IAA, motivation for sucrose under PR was significantly reduced by adulteration of sucrose with 0.1 g/L quinine. In addition, motivation for alcohol after only ∼1.5 months IAA was significantly reduced by adulteration of alcohol with 0.1 g/L quinine. Furthermore, home-cage alcohol intake by IAA rats was insensitive to quinine at concentrations (0.01, 0.03 g/L) that significantly reduced alcohol drinking in animals

  18. Effects of chloroquine, mefloquine and quinine on natural killer cell activity in vitro. An analysis of the inhibitory mechanism

    DEFF Research Database (Denmark)

    Pedersen, B K; Bygbjerg, I C; Theander, T G

    1986-01-01

    Natural killer (NK) cell activity against K 562 target cells was inhibited by pharmacological concentrations of chloroquine, mefloquine and quinine. The most potent were mefloquine and quinine. The drug-induced inhibition of the NK cell activity was abolished by addition of alpha-interferon (IF......) or interleukin 2 (Il-2); preincubation of mononuclear cells with IF or Il-2 followed by addition of anti-malarial drugs decreased the inhibitory effects of the drugs. The drug-induced inhibition of the NK cell activity was not dependent on the presence of monocytes. Using monocyte depleted Percoll fractionated...... NK cell enriched populations in a single cell agarose assay, it was shown that the inhibitory effects of mefloquine, but not of chloroquine and quinine were due to an inhibition of the formation of effector/target cell conjugates....

  19. 21 CFR 310.547 - Drug products containing quinine offered over-the-counter (OTC) for the treatment and/or...

    Science.gov (United States)

    2010-04-01

    ...-counter (OTC) for the treatment and/or prevention of malaria. 310.547 Section 310.547 Food and Drugs FOOD... over-the-counter (OTC) for the treatment and/or prevention of malaria. (a) Quinine and quinine salts have been used OTC for the treatment and/or prevention of malaria, a serious and potentially...

  20. Haplotypes at the Tas2r locus on distal chromosome 6 vary with quinine taste sensitivity in inbred mice

    Directory of Open Access Journals (Sweden)

    Munger Steven D

    2005-06-01

    Full Text Available Abstract Background The detection of bitter-tasting compounds by the gustatory system is thought to alert animals to the presence of potentially toxic food. Some, if not all, bitter stimuli activate specific taste receptors, the T2Rs, which are expressed in subsets of taste receptor cells on the tongue and palate. However, there is evidence for both receptor-dependent and -independent transduction mechanisms for a number of bitter stimuli, including quinine hydrochloride (QHCl and denatonium benzoate (DB. Results We used brief-access behavioral taste testing of BXD/Ty recombinant inbred (RI mouse strains to map the major quantitative trait locus (QTL for taste sensitivity to QHCl. This QTL is restricted to a ~5 Mb interval on chromosome 6 that includes 24 genes encoding T2Rs (Tas2rs. Tas2rs at this locus display in total 307 coding region single nucleotide polymorphisms (SNPs between the two BXD/Ty RI parental strains, C57BL/6J (quinine-sensitive and DBA/2J (quinine insensitive; approximately 50% of these mutations are silent. Individual RI lines contain exclusively either C57BL/6J or DBA/2J Tas2r alleles at this locus, and RI lines containing C57BL/6J Tas2r alleles are more sensitive to QHCl than are lines containing DBA/2J alleles. Thus, the entire Tas2r cluster comprises a large haplotype that correlates with quinine taster status. Conclusion These studies, the first using a taste-salient assay to map the major QTL for quinine taste, indicate that a T2R-dependent transduction cascade is responsible for the majority of strain variance in quinine taste sensitivity. Furthermore, the large number of polymorphisms within coding exons of the Tas2r cluster, coupled with evidence that inbred strains exhibit largely similar bitter taste phenotypes, suggest that T2R receptors are quite tolerant to variation.

  1. The analytical measurement of fluorescein, quinine and trace metal concentrations in solution using single bubble sonoluminescence

    Science.gov (United States)

    Wallace, P.; McCallum, K.; Barnard, C. L. R.; Clement, C.; Marshall, J.; Carroll, J.

    2007-03-01

    A single bubble was generated and levitated in a high-intensity sound field within a spherical flask excited in its fundamental mode. Under optimum experimental conditions the bubble was observed to emit light in the form of short flashes. This phenomenon is known as single bubble sonoluminescence (SBSL). Using this process, the emitted light from the bubble was monitored when solutions containing fluorescein, quinine and sodium, potassium and copper salts were placed in the cell. The results obtained indicated that reproducible signals related directly to the concentration of the species present in solution could be achieved using single bubble sonoluminescence. The results for the molecular species were compared with those obtained by fluorescence spectroscopy and, in the case of quinine, parallel determinations of concentration in a test solution were performed with consistent results. SBSL signals were also observed to exhibit a linear correlation with the concentration of several trace metal salts introduced to the solution in the measurement cell. However, it was not possible to demonstrate that the SBSL signals were derived from stimulated atomic emission or fluorescence, and it was concluded that the effect may result from an indirect effect involving the bubble excitation mechanism.

  2. Simultaneous Quantification of Ciprofloxacin, Quinine and 3-hyrdoxyquinine in Human Plasma using a HPLC Method

    Directory of Open Access Journals (Sweden)

    Adebanjo J. Adegbola, Julius O. Soyinka , Babatunde A. Adeagbo

    2016-02-01

    Full Text Available Malaria has been shown to strongly predispose patients in areas of malaria endemicity to bacteremia with severe outcomes, thus justifying the use of antibiotics in combination with antimalarial therapy in patients with severe malaria. This study describes a High-Performance Liquid Chromatographic (HPLC method for simultaneous determinations of Ciprofloxacin (CPN, Quinine (QN, and its major metabolite, 3-Hydroxyquinine (3-HQN, in human plasma. Following a simple precipitation with acetonitrile, chromatographic separation was achieved on a reversed-phase Agilent Zorbax (CN column (5 µm, 150 X 4.6 mm i.d using a mobile phase consisting of acetonitrile: potassium dihydrogen phosphate (pH = 2.8; 0.02 M (42:58, v/v. Retention times for CPN, 3-HQN, IS and QN were 2.7, 3.3, 3.6 and 4.9 minutes respectively. The limits of detection and validated lower limits of quantitation were 30 and 70 ng/ml for both QN and 3-HQN while the corresponding values were 50 and 100 ng/ml for CPN, respectively. The new HPLC method here developed, when compared with previous methods for the analysis of either or both drugs is simple, rapid, selective, reproducible and costeffective. It is also suitable for conducting a simultaneous therapeutic monitoring of quinine and ciprofloxacin in patients when concomittantly administered as demonstrated in five healthy volunteers.

  3. Investigation of imprinting parameters and their recognition nature for quinine-molecularly imprinted polymers

    Science.gov (United States)

    He, Jian-feng; Zhu, Quan-hong; Deng, Qin-ying

    2007-08-01

    A series of molecularly imprinted polymers (MIPs) was prepared using quinine as the template molecules by bulk polymerization. The presence of monomer-template solution complexes in non-covalent MIPs systems has been verified by both fluorescence and UV-vis spectrometric detection. The influence of different synthetic conditions (porogen, functional monomer, cross-linkers, initiation methods, monomer-template ratio, etc.) on recognition properties of the polymers was investigated. Scatchard analysis revealed that two classes of binding sites were formed in the imprinted polymer. The corresponding dissociation constants were estimated to be 45.00 μmol l -1 and 1.42 mmol l -1, respectively, by utilizing a multi-site recognition model. The binding characteristics of the imprinted polymers were explored in various solvents using equilibrium binding experiments. In the organic media, results suggested that polar interactions (hydrogen bonding, ionic interactions, etc.) between acidic monomer/polymer and template molecules were mainly responsible for the recognition, whereas in aqueous media, hydrophobic interactions had a remarkable non-specific contribution to the overall binding. The specificity of MIP was evaluated by rebinding the other structurally similar compounds. The results indicated that the imprinted polymers exhibited an excellent stereo-selectivity toward quinine.

  4. Endophytic Colletrotrichum spp. from Cinchona calisaya wedd. and it's potential quinine production as antibacterial and antimalaria

    Science.gov (United States)

    Radiastuti, Nani; Mutea, Dalli; Sumarlin, La Ode

    2017-02-01

    An endophytic fungus is microorganisms that live inside plant tissues without harming its host and is capable of producing the same secondary metabolites as its host plant. The endophytic fungus is very diverse and important group of microorganisms. The objectives of the study are to identify endophyte Colletotrichum spp. using ITS rDNA analyze, alkaloid cinchona and antibacterial characteristics. Phylogenetic analysis of ITS rDNA regions and morphology are used to identify the species. The Chloroform extracts of filtrate were analyzed using the High Pressure Liquid Chromatography (HPLC) to determine the production of quinine. There were 13 isolates of Colletotrichum spp as endophytes with associated with Cinchona calisaya Wedd. from fruit (6 isolates), leaf (5 isolates), twig (1 isolate) and root (1 isolate). This is the first report as endophytes are associated with C. calisaya. Based on ITS phylogenetic analysis are introduced of 7 strains Colletotrichum sp, 1 strain closely with C. aegnigma, 2 strains closely C. cordylinicola, 1 strains C arxii, 2 strains nested C. karstii. The Colletotrichum sp. M1 (leaf), M3 (bark), M8 (fruit) and C. karstii M5 (fruit) are potential alkaloid quinine. Five strains of Colletotrichum spp. have antibacterial activity are selected against Staphylococcus aureus and nine Colletotrichum spp. against Escherichia coli. The endophyte identification of Colletotrichum species needs another gene other than ITS rDNA.

  5. Crystal structure of quinine: the effects of vinyl and methoxy groups on molecular assemblies of Cinchona alkaloids cannot be ignored.

    Science.gov (United States)

    Hisaki, Ichiro; Hiraishi, Eri; Sasaki, Toshiyuki; Orita, Hideo; Tsuzuki, Seiji; Tohnai, Norimitsu; Miyata, Mikiji

    2012-11-01

    Quinine, one of Cinchona alkaloids, has been of great interest from medical, synthetic, and supramolecular viewpoints. However, unaccountably, the guest-free (GF) crystal of quinine containing no solvent or other molecules has not been reported for nearly three decades, although GF crystals of other Cinchona alkaloids, such as quinidine, cinchonidine, and cinchonine, are already known. In this study, we successfully revealed the crystal structure of quinine, which belongs to the P2(1) space group with the cell parameters of a=6.0587(1), b=19.2492(5), c=22.2824(7) Å, β=92.1646(11)°, and V=2596.83(12) Å(3). Interestingly, the crystal has three crystallographically independent molecules in the cell (Z'=3) that are connected through a N(quinoline)⋅⋅⋅H-O hydrogen bond to form a pseudo three-two-fold (3(2)) double-helical motif. The helical motif is completely different from those observed in GF crystals of other Cinchona alkaloids. Hierarchical comparison on the crystal structures of a series of Cinchona alkaloids including quinine clearly demonstrated that only small structural differences of a molecule, particularly the position of the vinyl group, cause a significant variety of assembly manner in the crystalline state. There have been no reports systematically demonstrating such steric effect in crystals of Cinchona alkaloids, and, therefore, the present system contributes to the design of desired functional crystal structures.

  6. Stereoselective inhibition by the diastereomers quinidine and quinine of uptake of cardiac glycosides into isolated rat hepatocytes

    NARCIS (Netherlands)

    Hedman, A; Meijer, D.K F

    1998-01-01

    The pharmacokinetic interaction between quinidine and digoxin in patients is well-known, in general requiring a dose reduction of digoxin in patients concomitantly treated with quinidine. Quinine, the diastereomer of quinidine, has not been as extensively studied in this respect. In addition to an i

  7. Solvent effects on the absorption and fluorescence spectra of quinine sulphate: Estimation of ground and excited-state dipole moments

    Science.gov (United States)

    Joshi, Sunita; Pant, Debi D.

    2012-06-01

    Ground and excited state dipole moments of probe quinine sulphate (QS) was obtained using Solvatochromic shift method. Higher dipole moment is observed for excited state as compared to the ground state which is attributed to the higher polarity of excited state.

  8. Halide (Cl(super -)) Quenching of Quinine Sulfate Fluorescence: A Time-Resolved Fluorescence Experiment for Physical Chemistry

    Science.gov (United States)

    Gutow, Jonathan H.

    2005-01-01

    The time-resolved fluorescence experiment investigating the halide quenching of fluorescence from quinine sulfate in water is described. The objectives of the experiment include reinforcing student understanding of the kinetics of competing pathways, making connections with microscopic theories of kinetics through comparison of experimental and…

  9. Interaction of quinine with negatively charged lipid vesicles studied by fluorescence spectroscopy Influence of the pH

    Science.gov (United States)

    Pedrós, Jesús; Porcar, Iolanda; Gómez, Clara M.; Campos, Agustín; Abad, Concepción

    1997-03-01

    The interaction of quinine with dimyristoylphosphatidic acid (DMPA) and dimyristoylphosphatidyl glycerol (DMPG) small unilamellar vesicles in the gel phase was studied by steady-state fluorescence spectroscopy at pHs 7, 6, 5 and 4 and 20°C. In aqueous solution, with excitation at 335 nm, the emission fluorescence spectrum of quinine varied with pH reflecting the occurrence of different charged species of the drug. In all cases, the emission maximum centered at 383 or 443 nm shifted to lower wavelength in the presence of vesicles. This indicates that the membrane-bound state quinine is in an environment of low polarity. Drug monocationic species were deeply buried in DMPG relative to DMPA bilayers whereas no significant differences were observed for dicationic species, the fluorophore being located in this case in a more aqueous-like environment. Experimental association isotherms generated from fluorescence intensity changes were quantitatively analyzed in terms of the binding equilibrium model. Although the binding affinity of quinine to anionic membranes was always higher for DMPG over DMPA, dicationic species showed a reduced ability to bind the negatively charged membrane. In addition, the binding model has been related with the partition model leading to a good agreement between the theoretical (calculated from the binding model) and the experimental (from the initial slope of the experimental isotherms) partition coefficient derived in each case.

  10. [Comparison of the effectiveness of artemether and quinine for treatment of severe malaria in children, Bangui, Central African Republic].

    Science.gov (United States)

    Bobossi-Serengbe, G; Gody, J-C; Fioboy, R; Elowa, J-B; Manirakiza, A

    2015-03-01

    The management of severe malaria is a major challenge in the health care services in sub-Saharan Africa. This study aimed to assess the efficacy and safety of artemether and quinine in severe malaria at Complexe pédiatrique of Bangui, Central African Republic. A total of 212 children among 1125 hospital admissions (18.8%), and aged 6 to 59 months were randomly treated with artemether and quinine. Anemia (58.5%) and seizures (33.5%) were the major syndromes observed. On the third day of follow up, a regression of clinical signs and parasite clearance were observed in 98.1% of children treated with artemether and 97.1% of children treated with quinine. The death rate was 2.3% due to anemic and neurological forms. These findings show that the artemether and quinine have similar efficacy. Hence, associated with adequate intensive health care, the use of these antimalarial drugs can significantly reduce mortality from severe malaria in the Central African Republic.

  11. Stability, compatibility and plasticizer extraction of quinine injection added to infusion solutions and stored in polyvinyl chloride (PVC) containers.

    Science.gov (United States)

    Faouzi, M A; Khalfi, F; Dine, T; Luyckx, M; Brunet, C; Gressier, B; Goudaliez, F; Cazin, M; Kablan, J; Belabed, A; Cazin, J C

    1999-12-01

    The stability of quinine was determined in various diluents and in polyvinyl chloride (PVC) containers. The release of diethyhexyl phthalate (DEHP) from PVC bags into intravenous infusions of quinine was also measured. We used an injection of two doses of quinine; quiniforme at 500 mg and quinimax at 400 mg in either 250- or 500-ml PVC infusion bags containing 5% dextrose, to give initial nominal concentrations of 2 or 1 mg ml(-1) quiniforme and 1.6 or 0.8 mg ml(-1) quinimax, the mean concentrations commonly used in clinical practice. Samples were assayed by stability-indicating high-performance liquid chromatography (HPLC) and the clarity was determined visually. Experiments were conducted to determine whether the stability and compatibility of quinine would be compromised, and whether DEHP would be leached from PVC bags and PVC administration sets during storage and simulated infusion. There was no substantial loss of quiniforme and quinimax over 1- or 2-h simulated infusion irrespective of the diluent, and storage during 8 h at 22 degrees C, 48 or 72 h at 4 degrees C and 96 h at 45 degrees C. Leaching of DEHP was also detected during simulated infusion delivery using PVC bags and PVC administration sets. The quantity was less than 2 microg ml(-1). During storage at 4 degrees C and room temperature the leaching of DEHP was low, but when the temperature was 45 degrees C the quantity was high, 21 microg ml(-1). To minimise patient exposure to DEHP, quinine solutions with all drugs should be infused immediately or stored for a maximum of 48 h at 4 degrees C.

  12. Observation of Fluorescence Emissions from Single-Bubble Sonoluminescence in Water doped with Quinine

    CERN Document Server

    Lu, J Q; Lin, F K; Liu, Y H

    2005-01-01

    Sonoluminescence is a phenomenon involving the transduction of sound into light. The detailed mechanism as well as the energy-focusing potentials are not yet fully explored and understood. So far only optical photons are observed, while emissions in the ultra-violet range are only inferred. By doping the fluorescent dye quinine into water with dilute sulphuric acid, the high energy photons can be converted into the optical photons with slower decay constants. These sonoluminescence and fluorescent emissions were observed in coincidence, and the emitted energy of the two modes can be differentiated by their respective timing profiles. Plans for using this technique as a diagnostic tool to quantitatively study ultra-violet and other high energy emissions in sonoluminescence are discussed.

  13. STUDY ON FLUORESCENCE SPECTRA OF QUININE%奎宁的荧光光谱研究

    Institute of Scientific and Technical Information of China (English)

    王惠英; 魏永巨

    2003-01-01

    @@ 奎宁(Quinine)是一种生物碱,又名金鸡纳碱,是最早使用的一种镇痛抗疟药.实际使用中多用其盐类,如盐酸奎宁、硫酸奎宁等.奎宁也是一种荧光试剂,在滴定分析中,奎宁可用作荧光指示剂.但是,文献中缺乏关于奎宁荧光光谱的详细报道.本文对奎宁的荧光性质讲行了较为详细的研究.

  14. The in vivo antimalarial activity of methylene blue combined with pyrimethamine, chloroquine and quinine

    Directory of Open Access Journals (Sweden)

    Giovanny Garavito

    2012-09-01

    Full Text Available The effectiveness of methylene blue (MB combined with pyrimethamine (PYR, chloroquine (CQ or quinine (Q was examined in a classical four-day suppressive test against a causative agent of rodent malaria, Plasmodium berghei. A marked potentiation was observed when MB was administered at a non-curative dose of 15 mg/kg/day in combination with PYR (0.19 mg/kg/day or Q (25 mg/kg/day. No synergy was found between MB (15 mg/Kg and CQ (0.75 mg/Kg. Our results suggest that the combination of MB with PYR or Q may improve the efficacy of these currently used antimalarial drugs.

  15. Quinine binding by the cocaine-binding aptamer. Thermodynamic and hydrodynamic analysis of high-affinity binding of an off-target ligand.

    Science.gov (United States)

    Reinstein, Oren; Yoo, Mina; Han, Chris; Palmo, Tsering; Beckham, Simone A; Wilce, Matthew C J; Johnson, Philip E

    2013-12-03

    The cocaine-binding aptamer is unusual in that it tightly binds molecules other than the ligand it was selected for. Here, we study the interaction of the cocaine-binding aptamer with one of these off-target ligands, quinine. Isothermal titration calorimetry was used to quantify the quinine-binding affinity and thermodynamics of a set of sequence variants of the cocaine-binding aptamer. We find that the affinity of the cocaine-binding aptamer for quinine is 30-40 times stronger than it is for cocaine. Competitive-binding studies demonstrate that both quinine and cocaine bind at the same site on the aptamer. The ligand-induced structural-switching binding mechanism of an aptamer variant that contains three base pairs in stem 1 is retained with quinine as a ligand. The short stem 1 aptamer is unfolded or loosely folded in the free form and becomes folded when bound to quinine. This folding is confirmed by NMR spectroscopy and by the short stem 1 construct having a more negative change in heat capacity of quinine binding than is seen when stem 1 has six base pairs. Small-angle X-ray scattering (SAXS) studies of the free aptamer and both the quinine- and the cocaine-bound forms show that, for the long stem 1 aptamers, the three forms display similar hydrodynamic properties, and the ab initio shape reconstruction structures are very similar. For the short stem 1 aptamer there is a greater variation among the SAXS-derived ab initio shape reconstruction structures, consistent with the changes expected with its structural-switching binding mechanism.

  16. Synthesis of R-3-quinine alcohol by CBS catalysis%CBS催化合成R-3-奎宁醇

    Institute of Scientific and Technical Information of China (English)

    任彦荣

    2012-01-01

    The chiral synthesis technique was applied to prepare R-3-quinine alcohol by catalytic reduction of 3-quinine ketone with the help of CBS catalyst. The yield and ee value were above 92% and 98% .respectively. The proposed synthesis method appeared to be convenient, high-yield, and applicable for industrial purpose.%探讨R-3-奎宁醇的合成工艺.通过手性合成的方法,以3-奎宁酮盐酸盐为原料,经CBS催化剂催化还原得R-3-奎宁醇.收率可达到92%以上,ee值可达98%以上.该合成路线操作步骤简单、收率高,具有工业应用价值.

  17. Enantioseparation of Neutral Compounds on a Quinine Carbamate-Immobilized Zirconia in Reversed-Phase Capillary Electrochromatography

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Mun Rak; Gwon, Ju Rim; Park, Jung Hag [Yeungnam University, Gyeongsan (Korea, Republic of)

    2010-01-15

    Quinine (QN) is a weak anion-exchange type chiral selector and QN-based silica stationary phases have been widely used for enantioseparation of acidic chiral analytes in HPLC and recently in CEC. In this work we report enantioseparation of non-acidic chiral analytes on a quinine carbamate-immobilized zirconia (QNZ) in reversed-phase (RP) CEC. Influences of pH, composition of the buffer, acetonitrile content and the applied voltage on enantioseparation were examined. Enantiomers of the analytes investigated are well separated in acetonitrile/phosphate buffer mobile phases. Separation data on QNZ were compared to those on QN-bonded silica (QNS). Retention was longer but better enantioselectivity and resolution were obtained on QNZ than QNS.

  18. Very small injected samples to study chloroquine and quinine in human serum using capillary-LC and native fluorescence

    OpenAIRE

    Ibrahim, H.; Bouajila, J.; Siri, N.; Rozing, G.; Nepveu, Françoise; Couderc, F.

    2007-01-01

    A comparison between HPLC with conventional fluorescence detection and capillary-LC (mu HPLC) with native laser-induced fluorescence (LIF) detection was done to determine chloroquine (CQ) and quinine (Q) in human serum. HPLC experiments were run with parameters of the conventional fluorimeter set at the highest level of sensitivity. Results were compared with those obtained on mu HPLC coupled to a ZETALIF (He-Cd 325 nm) detector which provided a 50-fold increase in sensitivity. In mu HPLC-LIF...

  19. Effective and novel enantioselective preparation of pyranopyrazoles and pyranocoumarins that is catalyzed by a quinine-derived primary amine.

    Science.gov (United States)

    Yang, Sai; Shen, Liu-lan; Kim, Yoon-Jung; Jeong, Jin-Hyun

    2016-01-14

    In this study, we executed an effective and novel enantioselective Michael/cyclodehydration sequential reaction between pyrazolin-5-one (or 4-hydroxy-2-pyrone) and chalcones that is catalyzed by a quinine-derived primary amine L7 in the presence of Boc-D-Phg-OH. Chiral pyranopyrazoles and pyranocoumarins were obtained in excellent enantioselectivities (up to 93%) with moderate yields and moderate enantioselectivities with high yields (up to 84%).

  20. Gustatory Detection of Tetrodotoxin and Saxitoxin, and Its Competitive Inhibition by Quinine and Strychnine in Freshwater Fishes

    OpenAIRE

    Hara, Toshiaki J.

    2011-01-01

    Fish detect extremely low levels of marine toxins tetrodotoxin (TTX) and saxitoxin (STX) via the specialized gustatory receptor(s). Physiological and pharmacological studies show that receptor(s) for TTX and STX are distinct from those which detect feeding stimulant amino acids and bile acids, and that TTX and STX do not share the same receptor populations, while interacting with quinine and strychnine in a competitive fashion suggestive of an antidotal relationship.

  1. Gustatory detection of tetrodotoxin and saxitoxin, and its competitive inhibition by quinine and strychnine in freshwater fishes.

    Science.gov (United States)

    Hara, Toshiaki J

    2011-01-01

    Fish detect extremely low levels of marine toxins tetrodotoxin (TTX) and saxitoxin (STX) via the specialized gustatory receptor(s). Physiological and pharmacological studies show that receptor(s) for TTX and STX are distinct from those which detect feeding stimulant amino acids and bile acids, and that TTX and STX do not share the same receptor populations, while interacting with quinine and strychnine in a competitive fashion suggestive of an antidotal relationship.

  2. Gustatory Detection of Tetrodotoxin and Saxitoxin, and Its Competitive Inhibition by Quinine and Strychnine in Freshwater Fishes

    Directory of Open Access Journals (Sweden)

    Toshiaki J. Hara

    2011-11-01

    Full Text Available Fish detect extremely low levels of marine toxins tetrodotoxin (TTX and saxitoxin (STX via the specialized gustatory receptor(s. Physiological and pharmacological studies show that receptor(s for TTX and STX are distinct from those which detect feeding stimulant amino acids and bile acids, and that TTX and STX do not share the same receptor populations, while interacting with quinine and strychnine in a competitive fashion suggestive of an antidotal relationship.

  3. Distribution of non-tasters for phenylthiocarbamide and high sensitivity to quinine hydrochloride of the non-tasters in Japanese.

    Science.gov (United States)

    Sato, T; Okada, Y; Miyamoto, T; Fujiyama, R

    1997-10-01

    The percentage of non-tasters for phenylthiocarbamide in 915 Japanese students was 9.4%. The thresholds of the edge and back of the tongue to quinine hydrochloride were significantly smaller in the non-tasters than in the tasters. The thresholds of any tongue portions to NaCl, acetic acid or sucrose did not differ between the tasters and the non-tasters.

  4. Novel chiral stationary phases based on peptoid combining a quinine/quinidine moiety through a C9-position carbamate group.

    Science.gov (United States)

    Wu, Haibo; Wang, Dongqiang; Song, Guangjun; Ke, Yanxiong; Liang, Xinmiao

    2014-04-01

    By connecting a quinine or quinidine moiety to the peptoid chain through the C9-position carbamate group, we synthesized two new chiral selectors. After immobilizing them onto 3-mercaptopropyl-modified silica gel, two novel chiral stationary phases were prepared. With neutral, acid, and basic chiral compounds as analytes, we evaluated these two stationary phases and compared their chromatographic performance with chiral columns based on quinine tert-butyl carbamate and the previous peptoid. From the resolution of neutral and basic analytes under normal-phase mode, it was found that the new stationary phases exhibited much better enantioselectivity than the quinine tert-butyl carbamate column; the peptoid moiety played an important role in enantiorecognition, which controlled the elution orders of enantiomers; the assisting role of the cinchona alkaloid moieties was observed in some separations. Under acid polar organic phase mode, it was proved that cinchona alkaloid moieties introduced excellent enantiorecognitions for chiral acid compounds; in some separations, the peptoid moiety affected enantioseparations as well. Overall, chiral moieties with specific enantioselectivity were demonstrated to improve the performance of peptoid chiral stationary phase efficiently.

  5. New insight into the stereoselective interactions of quinine and quinidine, with bovine serum albumin.

    Science.gov (United States)

    Liu, Yan; Chen, Mingmao; Wang, Shuaihua; Lin, Jingjing; Cai, Lizhen; Song, Ling

    2014-05-01

    Quinine (QN) and quinidine (QD), the chief quinoline alkaloids of various species of cinchona bark, are stereoisomers to each other. In this study, a series of appropriate and efficient methods have been applied to compare the binding modes of QN and QD with bovine serum albumin (BSA). The isothermal titration calorimetry and room temperature phosphorescence results show that both QN and QD can interact with BSA at one binding site to form drug-protein complexes, mainly through enthalpic driving force with the binding affinity order: QN > QD. The fluorescence resonance energy transfer and time-resolved fluorescence spectroscopy exhibits that QN has a larger energy transfer and more intensified binding capacity for BSA than QD. Data of dynamic light scattering reveal that the aggregate state of BSA is changed during this binding process, and the particle size distribution of QN-BSA bioconjugate is larger than that of QD. Nuclear magnetic resonance analysis indicates that aromatic protons make more contribution during ligand-protein complexation than that of aliphatic protons. The circular dichroism spectra exhibit different degrees of changes in BSA secondary structures in the presence of QN and QD, respectively.

  6. Synthesis, Crystal Structure and Luminescent Property of the One-dimensional Chain Chlorodibenzyltin 2-Quininate

    Institute of Scientific and Technical Information of China (English)

    JIANG Wu-Jiu; YANG Nian-Fa; KUANG Dai-Zhi; FENG Yong-Lan; ZHANG Fu-Xing; WANG Jian-Qiu; LIU Meng-Qin; YU Jiang-Xi

    2011-01-01

    A one-dimensional chain chlorodibenzyltin 2-quininate has been synthesized and characterized by IR, NMR spectra and elemental analysis. The crystal structure has been determined by X-ray diffraction. The crystal belongs to the monoclinic system, space group I4(—) with a = 19.1171(10), b = 19.1171(10), c = 12.5158(6) , Z = 8, V = 4574.1(4) 3, Dc = 1.477 g·cm-3, μ(MoKα) = 1.252 mm-1, F(000) = 2032, R = 0.0259 and wR = 0.0723. In the complex, the tin atom is six-coordinated to adopt a distorted octahedral configuration with bridging carboxyl of quinoline-2-carboxylic acid. The result of fluorescence spectrum analysis shows that the title complex at room temperature exhibits an intense photoluminescence with maximum emission at 364.2 nm (λex = 303.0 nm).

  7. Polymorphisms in Pfmdr1, Pfcrt, and Pfnhe1 genes are associated with reduced in vitro activities of quinine in Plasmodium falciparum isolates from western Kenya.

    Science.gov (United States)

    Cheruiyot, Jelagat; Ingasia, Luicer A; Omondi, Angela A; Juma, Dennis W; Opot, Benjamin H; Ndegwa, Joseph M; Mativo, Joan; Cheruiyot, Agnes C; Yeda, Redemptah; Okudo, Charles; Muiruri, Peninah; Bidii, Ngalah S; Chebon, Lorna J; Angienda, Paul O; Eyase, Fredrick L; Johnson, Jacob D; Bulimo, Wallace D; Andagalu, Ben; Akala, Hoseah M; Kamau, Edwin

    2014-07-01

    In combination with antibiotics, quinine is recommended as the second-line treatment for uncomplicated malaria, an alternative first-line treatment for severe malaria, and for treatment of malaria in the first trimester of pregnancy. Quinine has been shown to have frequent clinical failures, and yet the mechanisms of action and resistance have not been fully elucidated. However, resistance is linked to polymorphisms in multiple genes, including multidrug resistance 1 (Pfmdr1), the chloroquine resistance transporter (Pfcrt), and the sodium/hydrogen exchanger gene (Pfnhe1). Here, we investigated the association between in vitro quinine susceptibility and genetic polymorphisms in Pfmdr1codons 86 and 184, Pfcrt codon 76, and Pfnhe1 ms4760 in 88 field isolates from western Kenya. In vitro activity was assessed based on the drug concentration that inhibited 50% of parasite growth (the IC50), and parasite genetic polymorphisms were determined from DNA sequencing. Data revealed there were significant associations between polymorphism in Pfmdr1-86Y, Pfmdr1-184F, or Pfcrt-76T and quinine susceptibility (P quinine carried mutant alleles at these codons (Pfmdr1-86Y, Pfmdr1-184F, and Pfcrt-76T), whereas 74% of parasites susceptible to quinine carried the wild-type allele (Pfmdr1-N86, Pfmdr1-Y184, and Pfcrt-K76, respectively). In addition, quinine IC50 values for parasites with Pfnhe1 ms4760 3 DNNND repeats were significantly higher than for those with 1 or 2 repeats (P = 0.033 and P = 0.0043, respectively). Clinical efficacy studies are now required to confirm the validity of these markers and the importance of parasite genetic background.

  8. Extensive Gustatory Cortex Lesions Significantly Impair Taste Sensitivity to KCl and Quinine but Not to Sucrose in Rats.

    Science.gov (United States)

    Bales, Michelle B; Schier, Lindsey A; Blonde, Ginger D; Spector, Alan C

    2015-01-01

    Recently, we reported that large bilateral gustatory cortex (GC) lesions significantly impair taste sensitivity to salts in rats. Here we extended the tastants examined to include sucrose and quinine in rats with ibotenic acid-induced lesions in GC (GCX) and in sham-operated controls (SHAM). Presurgically, immediately after drinking NaCl, rats received a LiCl or saline injection (i.p.), but postsurgical tests indicated a weak conditioned taste aversion (CTA) even in controls. The rats were then trained and tested in gustometers to discriminate a tastant from water in a two-response operant taste detection task. Psychometric functions were derived for sucrose, KCl, and quinine. Our mapping system was used to determine placement, size, and symmetry of the lesions (~91% GC damage on average). For KCl, there was a significant rightward shift (ΔEC50 = 0.57 log10 units; pquinine sensitivity. Surprisingly, taste sensitivity to sucrose was unaffected by the extensive lesions and was comparable between GCX and SHAM rats. The fact that such large bilateral GC lesions did not shift sucrose psychometric functions relative to SHAM, but did significantly compromise quinine and KCl sensitivity suggests that the neural circuits responsible for the detection of specific taste stimuli are partially dissociable. Lesion-induced impairments were observed in expression of a postsurgical CTA to a maltodextrin solution as assessed in a taste-oriented brief-access test, but were not reflected in a longer term 46-h two-bottle test. Thus, deficits observed in rats after extensive damage to the GC are also dependent on the test used to assess taste function. In conclusion, the degree to which the GC is necessary for the maintenance of normal taste detectability apparently depends on the chemical and/or perceptual features of the stimulus.

  9. A polystyrene-supported 9-amino(9-deoxy)epi quinine derivative for continuous flow asymmetric Michael reactions.

    Science.gov (United States)

    Izquierdo, Javier; Ayats, Carles; Henseler, Andrea H; Pericàs, Miquel A

    2015-04-14

    A polystyrene (PS)-supported 9-amino(9-deoxy)epi quinine derivative catalyzes Michael reactions affording excellent levels of conversion and enantioselectivity using different nucleophiles and structurally diverse enones. The highly recyclable, immobilized catalyst has been used to implement a single-pass, continuous flow process (residence time: 40 min) that can be operated for 21 hours without significant decrease in conversion and with improved enantioselectivity with respect to batch operation. The flow process has also been used for the sequential preparation of a small library of enantioenriched Michael adducts.

  10. Effect of PMMA impregnation on the fluorescence quantum yield of sol-gel glasses doped with quinine sulfate

    Science.gov (United States)

    Meneses-Nava, M. A.; Barbosa-García, O.; Díaz-Torres, L. A.; Chávez-Cerda, S.; Torres-Cisneros, M.; King, T. A.

    2001-08-01

    The fluorescence quantum yield of quinine sulfate in sol-gel and PMMA impregnated glasses is measured. The observed quantum yield improvement in the sol-gel matrix, compared to ethanol, is interpreted as a reduction of non-radiative relaxation channels by isolation of the molecules by the cage of the glass. PMMA impregnated sol-gel glasses show an extra improvement of the fluorescence yield, which is interpreted as a reduction of the free space and the rigid fixation of the molecules to the matrix.

  11. Extensive Gustatory Cortex Lesions Significantly Impair Taste Sensitivity to KCl and Quinine but Not to Sucrose in Rats.

    Directory of Open Access Journals (Sweden)

    Michelle B Bales

    Full Text Available Recently, we reported that large bilateral gustatory cortex (GC lesions significantly impair taste sensitivity to salts in rats. Here we extended the tastants examined to include sucrose and quinine in rats with ibotenic acid-induced lesions in GC (GCX and in sham-operated controls (SHAM. Presurgically, immediately after drinking NaCl, rats received a LiCl or saline injection (i.p., but postsurgical tests indicated a weak conditioned taste aversion (CTA even in controls. The rats were then trained and tested in gustometers to discriminate a tastant from water in a two-response operant taste detection task. Psychometric functions were derived for sucrose, KCl, and quinine. Our mapping system was used to determine placement, size, and symmetry of the lesions (~91% GC damage on average. For KCl, there was a significant rightward shift (ΔEC50 = 0.57 log10 units; p<0.001 in the GCX psychometric function relative to SHAM, replicating our prior work. There was also a significant lesion-induced impairment (ΔEC50 = 0.41 log10 units; p = 0.006 in quinine sensitivity. Surprisingly, taste sensitivity to sucrose was unaffected by the extensive lesions and was comparable between GCX and SHAM rats. The fact that such large bilateral GC lesions did not shift sucrose psychometric functions relative to SHAM, but did significantly compromise quinine and KCl sensitivity suggests that the neural circuits responsible for the detection of specific taste stimuli are partially dissociable. Lesion-induced impairments were observed in expression of a postsurgical CTA to a maltodextrin solution as assessed in a taste-oriented brief-access test, but were not reflected in a longer term 46-h two-bottle test. Thus, deficits observed in rats after extensive damage to the GC are also dependent on the test used to assess taste function. In conclusion, the degree to which the GC is necessary for the maintenance of normal taste detectability apparently depends on the chemical and

  12. In vitro effect of chloroquine, mefloquine and quinine on human lymphocyte proliferative responses to malaria antigens and other antigens/mitogens

    DEFF Research Database (Denmark)

    Bygbjerg, I C; Theander, T G; Andersen, B J;

    1986-01-01

    The effect of 3 antimalarial quinoline derivatives, chloroquine, mefloquine and quinine on human blood mononuclear cells in vitro was studied. High concentrations profoundly suppressed the proliferation of mitogen- and antigen-stimulated lymphocytes, as indicated by decreased 14C-thymidine incorp......The effect of 3 antimalarial quinoline derivatives, chloroquine, mefloquine and quinine on human blood mononuclear cells in vitro was studied. High concentrations profoundly suppressed the proliferation of mitogen- and antigen-stimulated lymphocytes, as indicated by decreased 14C......-thymidine incorporation. On a weight base, the most potent drug was mefloquine. At clinically relevant doses, chloroquine and mefloquine did not affect the response to malaria antigens, but mefloquine decreased the response to phytohaemagglutinin; quinine suppressed the response to all mitogens (with the exception...

  13. Temporal and seasonal changes of genetic polymorphisms associated with altered drug susceptibility to chloroquine, lumefantrine and quinine in Guinea-Bissau between 2003 and 2012

    DEFF Research Database (Denmark)

    Jovel, Irina Tatiana; Kofoed, Poul-Erik; Rombo, Lars;

    2015-01-01

    BACKGROUND: Guinea-Bissau, West-Africa introduced artemether-lumefantrine in 2008 but quinine has also been commonly prescribed for treatment of uncomplicated Plasmodium falciparum malaria. An efficacious high-dose chloroquine treatment regimen was used previously. Temporal and seasonal changes...... of genetic polymorphisms associated with altered drug susceptibility to chloroquine, lumefantrine and quinine are described. METHODS: Pfcrt K76T, pfmdr1 gene copy numbers, N86Y, Y184F and 1034-1246 sequences were determined using PCR-based methods. Blood samples came from virtually all (n=1806) children aged.......001). CONCLUSIONS: Following the discontinuation of an effective chloroquine regimen highly artemether-lumefantrine susceptible P. falciparum (with pfcrt 76T) accumulated possibly due to suboptimal use of quinine and despite a fitness cost linked to 76T....

  14. Stereoselective Blockage of Quinidine and Quinine in the hERG Channel and the Effect of Their Rescue Potency on Drug-Induced hERG Trafficking Defect

    Directory of Open Access Journals (Sweden)

    Meng Yan

    2016-09-01

    Full Text Available Diastereoisomers of quinidine and quinine are used to treat arrhythmia and malaria, respectively. It has been reported that both drugs block the hERG (human ether-a-go-go-related gene potassium channel which is essential for myocardium repolarization. Abnormality of repolarization increases risk of arrhythmia. The aim of our research is to study and compare the impacts of quinidine and quinine on hERG. Results show that both drugs block the hERG channel, with quinine 14-fold less potent than quinidine. In addition, they presented distinct impacts on channel dynamics. The results imply their stereospecific block effect on the hERG channel. However, F656C-hERG reversed this stereoselectivity. The mutation decreases affinity of the two drugs with hERG, and quinine was more potent than quinidine in F656C-hERG blockage. These data suggest that F656 residue contributes to the stereoselective pocket for quinidine and quinine. Further study demonstrates that both drugs do not change hERG protein levels. In rescue experiments, we found that they exert no reverse effect on pentamidine- or desipramine-induced hERG trafficking defect, although quinidine has been reported to rescue trafficking-deficient pore mutation hERG G601S based on the interaction with F656. Our research demonstrated stereoselective effects of quinidine and quinine on the hERG channel, and this is the first study to explore their reversal potency on drug-induced hERG deficiency.

  15. Role of NMDA, opioid and dopamine D1 and D2 receptor signaling in the acquisition of a quinine-conditioned flavor avoidance in rats.

    Science.gov (United States)

    Rotella, Francis M; Badalia, Arzman; Duenas, Sean M; Hossain, Maruf; Saeed, Shermeen; Touzani, Khalid; Sclafani, Anthony; Bodnar, Richard J

    2014-04-10

    A conditioned flavor preference (CFP) can be produced by pairing a flavor (conditioned stimulus, CS+) with the sweet taste of fructose. Systemic dopamine (DA) D1, D2 and NMDA, but not opioid, receptor antagonists significantly reduce the acquisition of the fructose-CFP. A conditioned flavor avoidance (CFA) can be produced by pairing a CS+flavor with the bitter taste of quinine. To evaluate whether fructose-CFP and quinine-CFA share common neurochemical substrates, the present study determined the systemic effects of DA D1 (SCH23390: SCH), DA D2 (raclopride: RAC), NMDA (MK-801) or opioid (naltrexone: NTX) receptor antagonists on the acquisition of quinine-CFA. In Experiment 1, food-restricted male rats were trained over 8 alternating one-bottle sessions to drink an 8% fructose+0.2% saccharin solution (FS) mixed with one flavor (CS-, e.g., grape) and a different flavor (CS+, e.g., cherry) mixed in a solution (FSQ) containing fructose+saccharin and quinine at 0.001-0.030% concentrations. In six subsequent two-bottle choice tests (1-3: two sessions each) with the CS- and CS+ flavors presented in FS solutions, only rats trained with 0.03% quinine displayed a CS+ avoidance in Test 1. In Experiment 2, rats received vehicle (Veh), SCH (200 nmol/kg), RAC (200 nmol/kg), MK-801 (100 μg/kg) or NTX (1 mg/kg) 30 min prior to the 8 one-bottle training sessions with CS-/FS and CS+/FSQ (0.03% quinine) solutions. An additional vehicle group (Veh 0.06%) was trained with a CS+/FSQ containing 0.06% quinine. In the two-bottle choice tests, the Veh and RAC groups avoided the CS+ flavor in Test 1 only, whereas the SCH, MK801, and NTX groups significantly avoided the CS+ in Tests 1-3. The Veh.06% group trained avoided the CS+ in Tests 1 and 2, but not Test 3. In Experiment 3, Veh and SCH groups were trained as in Experiment 2, but were tested with CS flavors presented in 0.2% saccharin solutions. The SCH group avoided the CS+ flavor in Tests 1-3 while the Veh group avoided the CS+ in Test

  16. S-3-奎宁醇的合成研究%Study on the Synthesis of S-3-Quinine Alcohol

    Institute of Scientific and Technical Information of China (English)

    任彦荣

    2012-01-01

    A new method is reported for synthesizingS-3-quininealcohoL Based on a configuration transformation strategy, the raw material 3-quinineketoneis, in turn, reduced,esterified, and finally hydrolyzed into S-3-quinine alcohol by potassium borohydride, acetyl chloride, and sodium hydroxide, respectively- Subsequently, 1H NMRcharacterization is employed to confirm the S -3 -quinine alcohol and HPLC also reveals that theoverall yield of the desired product isabout 88-96%-The proposedsynthesis method appears to be convenient,high-yielding, and applicable for industrial purpose.%探讨S-3-奎宁醇的合成新工艺.通过构型转化的方法,以3-奎宁酮为原料,经硼氢化钾还原、与乙酰氯成酯、水解得S-3-奎宁醇.其结构经1H NMR等表征证实,总收率可达到88.96%.该合成路线操作步骤简单、收率高,具有工业应用价值.

  17. Non-malarial fever among pregnant women in Medani Hospital, Sudan:diagnostic uncertainty and overtreatment with quinine

    Institute of Scientific and Technical Information of China (English)

    Elhassan M Elhassan; Abd Elrahium D Haggaz; Mamoun M Magzoub; Ishag Adam

    2010-01-01

    Objective:To investigate the accuracy of malaria diagnosis among pregnant women admitted in Medani Maternity Hospital, Central Sudan during June-October 2009 and to investigate the antimalarials prescribed in this setting. Methods:Socio-demographic characteristics and obstetrics history were gathered using pre-tested questionnaires. The finger prick blood samples were collected from pregnant women who admitted as malaria case after an initial microscopic test done by general microscopists for malaria diagnosis. The antimalarial treatment prescribed by treating doctor was inquired for. Results:Only 21 (8.6%) out of 243 pregnant women admitted as malaria case after an initial microscopic test done by general microscopists for malaria were found to have blood film positive. There was no significant difference in the specificity of the microscopy accuracy between those who have been investigated in the private and governmental sector, 15/193 (8.2%) vs. 6/60(10%), (P>0.05). Quinine infusion was the prescribed drug in this setting. Conclusions: There is a very poor specificity of malaria microscopy in pregnant women admitted to Madani Maternity Hospital. Quinine was the drug received. Malaria control programme should interfere urgently to change this situation.

  18. Quinine-derived thiourea and squaramide catalyzed conjugate addition of α-nitrophosphonates to enones: asymmetric synthesis of quaternary α-aminophosphonates.

    Science.gov (United States)

    Bera, Kalisankar; Namboothiri, Irishi N N

    2015-02-01

    Conjugate addition of α-nitrophosphonates to enones was carried out in the presence of two sets of organocatalysts, viz. a quinine-thiourea and a quinine-squaramide. The quinine-thiourea provided the products possessing an α-quaternary chiral center in high enantioselectivities only in the case of electron rich enones. On the other hand, the quinine-squaramide was more efficient in that a wide variety of electron rich and electron poor enones underwent Michael addition of nitrophosphonates to afford the quaternary α-nitrophosphonates in excellent yields and enantioselectivities. The hydrogen bonding donor ability of the bifunctional catalyst, as shown in the proposed transition states, appears primarily responsible for the observed selectivity. However, a favorable π-stacking between the aryl groups of thiourea/squaramide and aryl vinyl ketone also appeared favorable. The reaction was amenable to scale up, and the enantioenriched quaternary α-nitrophosphonates could be easily transformed to synthetically and biologically useful quaternary α-aminophosphonates and other multifunctional molecules.

  19. A Quinine-Squaramide Catalyzed Enantioselective Aza-Friedel-Crafts Reaction of Cyclic Trifluoromethyl Ketimines with Naphthols and Electron-Rich Phenols.

    Science.gov (United States)

    Zhou, Ding; Huang, Zheng; Yu, Xueting; Wang, Youxin; Li, Jian; Wang, Wei; Xie, Hexin

    2015-11-20

    A highly enantioselective aza-Friedel-Crafts (aza-F-C) reaction of cyclic trifluoromethyl ketimines and naphthols/phenols was developed with fluorenyl-substituted quinine-squaramide as the catalyst. This protocol enables direct access to biologically important chiral trifluoromethyl dihydroquinazolinones with up to 99% yields and up to 99% ee's.

  20. Quinine-dependent antibodies bind a restricted set of epitopes on the glycoprotein Ib-IX complex : characterization of the epitopes

    NARCIS (Netherlands)

    Burgess, J K; Lopez, J A; Berndt, M C; Dawes, I; Chesterman, C N; Chong, B H

    1998-01-01

    Severe immune thrombocytopenia is an idiosyncratic complication of quinine therapy. Although in most cases the responsible antibody is directed against platelet membrane glycoprotein (GP) Ib-IX, specificity for GPIIb-IIIa or both epitopes has also been reported. The objective of this study was to ch

  1. A contribution to the determination of aflatoxin B1, quinine hydrochloride and L(+)-ascorbic acid in foodstuffs by quantitative in situ thin-layer chromatographic analysis

    NARCIS (Netherlands)

    Beljaars, P.R.

    1974-01-01

    The application of quantitative thin-layer chromatography (TLC) involving in situ spectrodensitometric measurements with a flying-spot densitometer is described in this study for the analysis of aflatoxin B 1 , quinine hydrochloride

  2. Science, industry and the colonial state : a shift from a German- to a Dutch-controlled cinchona and quinine cartel (1880–1920)

    NARCIS (Netherlands)

    Roersch van der Hoogte, Arjo; Pieters, Toine

    2015-01-01

    This study shows how control over delicately balanced supply chains from raw material to the final product shifted from one national industry to another. By 1920, Dutch cinchona producers and quinine manufacturers dominated the international cartel that controlled the worldwide production and distri

  3. Science, industry and the colonial state : a shift from a German- to a Dutch-controlled cinchona and quinine cartel (1880–1920)

    NARCIS (Netherlands)

    Roersch van der Hoogte, Arjo|info:eu-repo/dai/nl/31503274X; Pieters, Toine|info:eu-repo/dai/nl/188785833

    2015-01-01

    This study shows how control over delicately balanced supply chains from raw material to the final product shifted from one national industry to another. By 1920, Dutch cinchona producers and quinine manufacturers dominated the international cartel that controlled the worldwide production and

  4. From Colonial Agro-Industrialism to agro-industrialism : Game-changing evolution of the Dutch transoceanic cinchona-quinine Enterprise (1940's-1960s)

    NARCIS (Netherlands)

    Pieters, A.H.L.M.

    2016-01-01

    By the turn of the twentieth century, the Dutch colony of the Netherlands Indies dominated the worldwide supply of antifebrifuge (to reduce fever) cinchona bark, the raw material for quinine, an antimalarial medicine. Over the next four decades, the high-quality and laboratory-conditioned cultivatio

  5. A contribution to the determination of aflatoxin B1, quinine hydrochloride and L(+)-ascorbic acid in foodstuffs by quantitative in situ thin-layer chromatographic analysis

    NARCIS (Netherlands)

    Beljaars, P.R.

    1974-01-01

    The application of quantitative thin-layer chromatography (TLC) involving in situ spectrodensitometric measurements with a flying-spot densitometer is described in this study for the analysis of aflatoxin B 1 , quinine hydrochloride and L(+)-ascorbic acid (vitamin C

  6. Quinine-dependent antibodies bind a restricted set of epitopes on the glycoprotein Ib-IX complex: Characterization of the epitopes

    NARCIS (Netherlands)

    Burgess, Janette K.; Lopez, Jose A.; Berndt, Michael C.; Dawes, Ian; Chesterman, Colin N.; Chong, Beng H.

    1998-01-01

    Severe immune thrombocytopenia is an idiosyncratic complication of quinine therapy. Although in most cases the responsible antibody is directed against platelet membrane glycoprotein (GP) Ib-IX, specificity for GPIIb- IIIa or both epitopes has also been reported. The objective of this study was to c

  7. Access to artemisinin-based combination therapy (ACT) and quinine in malaria holoendemic regions of western Kenya.

    Science.gov (United States)

    Watsierah, Carren A; Ouma, Collins

    2014-07-28

    Artemisinin-based combination therapy (ACT) has been adopted as the most effective treatment against malaria in many endemic countries like Kenya while quinine has remained the second line. The objective of the current study was to assess access to Kenya's policy recommended anti-malarials, ACT and quinine in the public, private and not-for-profit drug outlets in western Kenya. A cross-sectional survey using purposive sampling of 288 outlets (126 public, 96 private, 66 not-for-profit) was conducted in western Kenya in two regions with varying Plasmodium falciparum endemicities. Information on access (availability, price, affordability) on ACT and quinine was collected using the WHO and Healthcare Associated Infection (HAI) standardized methodologies for availability, prices and affordability of drugs. From a Ministry of Health database, the following were included in the analyses: one (1) main public hospital, followed by random selection of five hospitals under this main facility. Eight other public outlets under each of the hospitals were selected, to a total of 96. Matching number of private outlets (n = 96), all (66) not-for-profit outlets and additional 30 public health facilities were sampled to get the required sample size of 288. More public 111 (88.1%) and not-for-profit 27 (40.9%) outlets stocked subsidized ACT (artemether-lumefantrine, AL). Other artemisinin-based combinations were widely available for both children 93 (96.9%) and adults 82 (85.0%) in private outlets. Frequent stock-outs were in public in 106 (84%), reporting three times or more stock-outs in three months. Subsidized ACT (AL) was sold at median price of USD 0.94 and 0.75 in private and not-for-profit outlets respectively. The costs was higher than recommended price of USD 0.5 and requiring up to 0.20-0.25 days of disposable income for households in lowest economic status. There is low availability of subsidized ACT (AL) and higher frequency of stock-outs in government facilities, while

  8. Enantiomer separation of acidic chiral compounds on a quinine-silica/zirconia hybrid monolith by capillary electrochromatography.

    Science.gov (United States)

    Tran, Le Ngoc; Park, Jung Hag

    2015-05-29

    A weak anion-exchanger chiral selector, quinine-incorporated silica/zirconia hybrid monolithic (QUI-S/ZHM) capillary column was prepared by sol-gel technology. The performance of the QUI-S/ZHM column was investigated for enantioresolution of a set of acidic chiral drugs and dinitrobenzoyl (DNB)-amino acids by capillary electrochromatography in aqueous organic mobile phases composed of acetonitrile (ACN) and triethylammonium acetate (TEAA) buffer. Effects of several parameters including the ACN content, concentration and pH of the mobile phase on the chiral separation were examined. Baseline resolutions of all the compounds were obtained in the mobile phase consisting of 70:30 ACN/TEAA (10mM, pH 6) under applied voltage of -10kV at 25°C within 20min.

  9. [Separation mechanism of chiral stationary phase based on quinine and crown ether for the direct stereoselective separation of amino acids].

    Science.gov (United States)

    Wu, Haixia; Wang, Dongqiang; Zhao, Jianchao; Ke, Yanxiong; Liang, Xinmiao

    2016-01-01

    A novel chiral stationary phase combining quinine and crown ether (QN-CR CSP) was developed to separate amino acid enantiomers. This CSP showed good enantioselectivity for some amino acids. Since the synergistic effect of ion exchange and complexation in chiral recognition of amino acids, a new adsorption isotherm was built. Using the method of frontal analysis by characteristic point (FACP), the adsorption isotherms of tryptophan (Trp) under different mobile phase conditions were determined and fitted the proposed adsorption isotherm model well. With the increase of the competition between metal cationic and amino to crown ether, the equilibrium constant of complexing adsorption was found increased. The chiral separation ability was decreased. The adsorption isotherm improved the understanding of the retention behavior of amino acids on QN-CR CSP, which was also benefit to optimize the structure of the stationary phase.

  10. In vivo and in vitro Plasmodium falciparum Resistance to Chloroquine, Amodiaquine and Quinine in the Brazilian Amazon

    Directory of Open Access Journals (Sweden)

    Aluisio Augusto Cotrim SEGURADO

    1997-03-01

    Full Text Available In order to study the chemoresistance of Plasmodium falciparum to commonly used antimalarial drugs in Brazil the authors have studied ten patients with falciparum malaria, acquired in the Brazilian Amazon region. Patients were submitted to in vivo study of drug sensitivity, after chemotherapy with either 4-aminoquinolines (chloroquine or amodiaquine or quinine. Adequate drug absorption was confirmed by standard urine excretion tests for antimalarials. Eight patients could be followed up to 28 days. Among these in vivo resistance (R I and R II responses was seen in all patients who received 4-amino-quinolines. One patient treated with quinine exhibited a R III response. Peripheral blood samples of the same patients were submitted to in vitro microtests for sensitivity to antimalarials. Out of nine successful tests, resistance to chloroquine and amodiaquine was found in 100% and resistance to quinine in 11.11% of isolates. Probit analysis of log dose-response was used to determine effective concentrations EC50, EC90 and EC99 to the studied drugs. Good correlation between in vivo and in vitro results was seen in six patients. The results emphasize high levels of P. falciparum resistance to 4- aminoquinolines and suggest an increase in resistance to quinine in the Brazilian Amazon region, reinforcing the need for continuous monitoring of drug sensitivity to adequate chemotherapy according to the most efficacious drug regimensResistência in vivo e in vitro do Plasmodium falciparum à cloroquina, amodiaquina e quinino na Amazônia Brasileira. Com o propósito de avaliar a resistência do Plasmodium falciparum às drogas antimaláricas, rotineiramente empregadas no Brasil, os autores acompanharam dez pacientes com malária falciparum adquirida na Amazônia brasileira. Os pacientes foram submetidos a estudo in vivo de sensibilidade a drogas, após tratamento com derivados 4-aminoquinoleínicos (cloroquina e amodiaquina ou quinino. A absorção das

  11. Estudio de la líqueno flora encontrada en el Cerro de Quininí, Tibacuy, Cundinamarca

    Directory of Open Access Journals (Sweden)

    Hormaza Francisco

    2000-12-01

    Full Text Available

    Se realizó un muestreo de la liquen o flora del cerro de Quininí, Tibacuy, Cundinamarca para estudiar las características morfológicas externas de los géneros de líquenes encontrados en el. A su vez se hizo la revisión bibliográfica acerca de dichos géneros, datando así la riqueza de líquenes en la zona con 8 géneros en total y con respecto al papel de bioindicadores se mostró el grado de intervención para el lugar.

  12. Isolation and characterization of quinine from Polygonatum verticillatum: A new marker approach to identify substitution and adulteration

    Directory of Open Access Journals (Sweden)

    Jaswinder Kaur Virk

    2016-01-01

    Full Text Available Polygonatum verticillatum (Mahameda is an important ingredient of Ashtawarga and Ayurvedic formulations. Nowadays, it comes under the category of endangered plants due to large scale and indiscriminate collection of wild material. To overcome the scarcity, substitutes of Mahameda are also commonly used in market. These additives are different from the authentic plant by Ayurvedic and pharmacological theory of drug action, thereby resulting in substitution/adulteration. Substitution is a critical issue in isolation and quantification of the therapeutically active ingredients that can be used as markers in the identification of substitution/adulteration. Methanolic extract of the rhizomes of P. verticillatum was subjected to preliminary phytochemical screening for the detection of phytoconstituents, followed by column chromatography for isolation of the marker. The column was first eluted with pure hexane, and polarity of the solvent was gradually increased. A total of 1180 fractions were collected and pooled on the basis of thin-layer chromatography profile. The single compound was isolated and confirmed by chemical test, melting point, spectral analysis, and comparison with literature. Phytochemical screening of the extract shows the presence of alkaloids, flavonoids, carbohydrates, terpenoids, and phenolics. A pure white crystalline powder was isolated by column chromatography which was characterized as (6-methoxyquinolin-4-yl-8-vinylquinuclidin-2-yl methanol, i.e. Quinine. The isolated compound, Quinine, was identified as a novel compound in Mahameda as it has not been reported in the genus Polygonatum, till now. It can be used as a marker for the identification of substitution/adulteration and standardization of P. verticillatum.

  13. Isolation and characterization of quinine from Polygonatum verticillatum: A new marker approach to identify substitution and adulteration

    Science.gov (United States)

    Virk, Jaswinder Kaur; Kumar, Sanjiv; Singh, Ranjit; Tripathi, Avinash C.; Saraf, Shailendra K.; Gupta, Vikas; Bansal, Parveen

    2016-01-01

    Polygonatum verticillatum (Mahameda) is an important ingredient of Ashtawarga and Ayurvedic formulations. Nowadays, it comes under the category of endangered plants due to large scale and indiscriminate collection of wild material. To overcome the scarcity, substitutes of Mahameda are also commonly used in market. These additives are different from the authentic plant by Ayurvedic and pharmacological theory of drug action, thereby resulting in substitution/adulteration. Substitution is a critical issue in isolation and quantification of the therapeutically active ingredients that can be used as markers in the identification of substitution/adulteration. Methanolic extract of the rhizomes of P. verticillatum was subjected to preliminary phytochemical screening for the detection of phytoconstituents, followed by column chromatography for isolation of the marker. The column was first eluted with pure hexane, and polarity of the solvent was gradually increased. A total of 1180 fractions were collected and pooled on the basis of thin-layer chromatography profile. The single compound was isolated and confirmed by chemical test, melting point, spectral analysis, and comparison with literature. Phytochemical screening of the extract shows the presence of alkaloids, flavonoids, carbohydrates, terpenoids, and phenolics. A pure white crystalline powder was isolated by column chromatography which was characterized as (6-methoxyquinolin-4-yl-8-vinylquinuclidin-2-yl) methanol, i.e. Quinine. The isolated compound, Quinine, was identified as a novel compound in Mahameda as it has not been reported in the genus Polygonatum, till now. It can be used as a marker for the identification of substitution/adulteration and standardization of P. verticillatum. PMID:27833896

  14. Direct enantioseparation of underivatized aliphatic 3-hydroxyalkanoic acids with a quinine-based zwitterionic chiral stationary phase.

    Science.gov (United States)

    Ianni, Federica; Pataj, Zoltán; Gross, Harald; Sardella, Roccaldo; Natalini, Benedetto; Lindner, Wolfgang; Lämmerhofer, Michael

    2014-10-10

    While aliphatic 2-hydroxyalkanoic acids have been more or less successfully enantioseparated with various chiral stationary phases by HPLC and GC, analogous applications on underivatized aliphatic 3-hydroxyalkanoic acids are completely absent in the scientific literature. With the aim of closing this gap, the enantioseparation of 3-hydroxybutyric acid, 3-hydroxydecanoic acid and 3-hydroxymyristic acid has been performed with two ion-exchange type chiral stationary phases (CSPs): one containing the anion-exchange type tert-butyl carbamoyl quinine chiral selector motif (Chiralpak QN-AX), and the other carrying the new zwitterionic variant based on trans-(S,S)-2-aminocyclohexanesulfonic acid-derivatized quinine carbamate (Chiralpak ZWIX(+)) as the chiral selector and enantiodiscriminating element, respectively. The zwitterionic enantiorecognition material provided better results in terms of enantioselectivity and resolution compared to the anion-exchanger CSP at reduced retention times due to the intramolecular counterion effect imposed by the sulfonic acid moiety and its competition with the 3-hydroxyalkanoic acid analyte for ionic interaction at the quininium-anion exchanger site. It is thus recommended as the CSP of first choice for enantioseparations of the class of aliphatic 3-hydroxyalkanoic acids. With use of polar organic eluent composed of ACN/MeOH/AcOH - 95/5/0.05 (v/v/v), a good compromise in terms of analysis time and enantioresolution quality was accomplished. The major experimental variables have been investigated for optimization of the resolution and allowed to derive information on the enantiorecognition mechanism. Corresponding Chiralpak ZWIX(-), based on pseudo-enantiomeric selector derived from quinidine and trans-(R,R)-2-aminocyclohexanesulfonic acid with opposite configurations provided reversed enantiomer elution orders. It has further to be stressed that these separations can be obtained with mass spectrometry compatible mobile phases.

  15. The thermodynamic dissociation constants of losartan, paracetamol, phenylephrine and quinine by the regression analysis of spectrophotometric data

    Energy Technology Data Exchange (ETDEWEB)

    Meloun, Milan [Department of Analytical Chemistry, University of Pardubice, 53210 Pardubice (Czech Republic)]. E-mail: milan.meloun@upce.cz; Syrovy, Tomas [Department of Analytical Chemistry, University of Pardubice, 53210 Pardubice (Czech Republic)]. E-mail: tomas.syrovy@upce.cz; Vrana, Ales [IVAX Pharmaceuticals, s.r.o. 74770 Opava (Czech Republic)]. E-mail: ales_vrana@ivax-cr.com

    2005-03-21

    The mixed dissociation constants of four drug acids - losartan, paracetamol, phenylephrine and quinine - at various ionic strengths I of range 0.01 and 1.0 and at temperatures of 25 and 37 deg. C were determined using SPECFIT32 and SQUAD(84) regression analysis of the pH-spectrophotometric titration data. A proposed strategy of efficient experimentation in a dissociation constants determination, followed by a computational strategy for the chemical model with a dissociation constants determination, is presented on the protonation equilibria of losartan. Indices of precise methods predict the correct number of components, and even the presence of minor ones when the data quality is high and the instrumental error is known. Improved identification of the number of species uses the second or third derivative function for some indices, namely when the number of species in the mixture is higher than 3 and when, due to large variations in the indicator values even at logarithmic scale, the indicator curve does not reach an obvious point where the slope changes. The thermodynamic dissociation constant pKaT was estimated by nonlinear regression of {l_brace}pK{sub a}, I{r_brace} data at 25 and 37 deg. C: for losartan pKa,1T=3.63(1) and 3.57(3), pKa,2T=4.84(1) and 4.80(3), for paracetamol pKa,1T=9.78(1) and 9.65(1), for phenylephrine pKa,1T=9.17(1) and 8.95(1), pKa,2T=10.45(1) and 10.22(1), for quinine pKa,1T=4.25(1) and 4.12(1), pKa,2T=8.72(1) and 8.46(2). Goodness-of-fit tests for various regression diagnostics enabled the reliability of the parameter estimates to be found.

  16. 几个聚合物负载的奎宁催化剂的合成%Synthesis of several polymer - supported quinines

    Institute of Scientific and Technical Information of China (English)

    马秋石; 张莲鹏; 李文; 汤峨

    2011-01-01

    基于聚合物试剂合成的后处理简单,纯化方便和易于回收的特点,分别用聚苯乙烯和聚乙二醇树脂为载体进行几个手性奎宁催化剂的固相和液相组合合成,考察了MPEG5000负载的奎宁催化剂沉降率的影响因素.%Several polymer - supported quinines as chiral catalysts were synthesized from polystyrene and polyethylene glycol as supporter. The synthesis has the advantages of easy purification and recovery. The factors to influence the sedimentation of MPEG - supported quinine were also discussed.

  17. Muscarinic and nicotinic cholinergic receptor antagonists differentially mediate acquisition of fructose-conditioned flavor preference and quinine-conditioned flavor avoidance in rats.

    Science.gov (United States)

    Rotella, Francis M; Olsson, Kerstin; Vig, Vishal; Yenko, Ira; Pagirsky, Jeremy; Kohen, Ilanna; Aminov, Alon; Dindyal, Trisha; Bodnar, Richard J

    2015-09-01

    Rats display both conditioned flavor preference (CFP) for fructose, and conditioned flavor avoidance (CFA) following sweet adulteration with quinine. Previous pharmacological analyses revealed that fructose-CFP expression was significantly reduced by dopamine (DA) D1 or D2 antagonists, but not NMDA or opioid antagonists. Fructose-CFP acquisition was significantly reduced by DA D1, DA D2 or NMDA antagonists, but not opioid antagonists. Quinine-CFA acquisition was significantly enhanced and prolonged by DA D1, NMDA or opioid, but not DA D2 antagonists. Cholinergic interneurons and projections interact with DA systems in the nucleus accumbens and ventral tegmental area. Further, both muscarinic and nicotinic cholinergic receptor signaling have been implicated in sweet intake and development of food-related preferences. Therefore, the present study examined whether systemic administration of muscarinic (scopolamine: SCOP) or nicotinic (mecamylamine: MEC) cholinergic receptor antagonists mediated fructose-CFP expression, fructose-CFP acquisition and quinine-CFA acquisition. For fructose-CFP expression, rats were trained over 10 sessions with a CS+ flavor in 8% fructose and 0.2% saccharin and a CS- flavor in 0.2% saccharin. Two-bottle choice tests with CS+ and CS- flavors mixed in 0.2% saccharin occurred following vehicle, SCOP (0.1-10mg/kg) and MEC (1-8mg/kg). For fructose-CFP acquisition, six groups of rats received vehicle, SCOP (1 or 2.5mg/kg), MEC (4 or 6mg/kg) or a limited intake vehicle control 0.5h prior to 10 CS+ and CS- training sessions followed by six 2-bottle CS+ and CS- choice tests in 0.2% saccharin. For quinine-CFA acquisition, five groups of rats received vehicle, SCOP (1 or 2.5mg/kg) or MEC (4 or 6mg/kg) 0.5h prior to 8 one-bottle CS- (8% fructose+0.2% saccharin: FS) and CS+ (fructose+saccharin+quinine (0.030%: FSQ) training sessions followed by six 2-bottle CS- and CS+ choice tests in fructose-saccharin solutions. Fructose-CFP expression was

  18. Temporal and seasonal changes of genetic polymorphisms associated with altered drug susceptibility to chloroquine, lumefantrine, and quinine in Guinea-Bissau between 2003 and 2012.

    Science.gov (United States)

    Jovel, Irina Tatiana; Kofoed, Poul-Erik; Rombo, Lars; Rodrigues, Amabelia; Ursing, Johan

    2015-02-01

    In 2008, artemether-lumefantrine was introduced in Guinea-Bissau, West Africa, but quinine has also been commonly prescribed for the treatment of uncomplicated Plasmodium falciparum malaria. An efficacious high-dose chloroquine treatment regimen was used previously. Temporal and seasonal changes of genetic polymorphisms associated with altered drug susceptibility to chloroquine, lumefantrine, and quinine have been described. P. falciparum chloroquine resistance transporter (pfcrt) K76T, pfmdr1 gene copy numbers, pfmdr1 polymorphisms N86Y and Y184F, and pfmdr1 sequences 1034 to 1246 were determined using PCR-based methods. Blood samples came from virtually all (n=1,806) childrenquinine and despite a fitness cost linked to pfcrt 76T. (The studies reported here were registered at ClinicalTrials.gov under registration no. NCT00137514 [PSB-2001-chl-amo], NCT00137566 [PSB-2004-paracetamol], NCT00426439 [PSB-2006-coartem], NCT01157689 [AL-eff 2010], and NCT01704508 [Eurartesim 2012].).

  19. Long-Chain Fatty Acids Elicit a Bitterness-Masking Effect on Quinine and Other Nitrogenous Bitter Substances by Formation of Insoluble Binary Complexes.

    Science.gov (United States)

    Ogi, Kayako; Yamashita, Haruyuki; Terada, Tohru; Homma, Ryousuke; Shimizu-Ibuka, Akiko; Yoshimura, Etsuro; Ishimaru, Yoshiro; Abe, Keiko; Asakura, Tomiko

    2015-09-30

    We have previously found that fatty acids can mask the bitterness of certain nitrogenous substances through direct molecular interactions. Using isothermal titration calorimetry, we investigated the interactions between sodium oleate and 22 bitter substances. The hydrochloride salts of quinine, promethazine, and propranolol interacted strongly with fatty acids containing 12 or more carbon atoms. The (1)H NMR spectra of these substances, obtained in the presence of the sodium salts of the fatty acids in dimethyl sulfoxide, revealed the formation of hydrogen bonds between the nitrogen atoms of the bitter substances and the carboxyl groups of the fatty acids. When sodium laurate and the hydrochloride salt of quinine were mixed in water, an equimolar complex formed as insoluble heterogeneous needlelike crystals. These results suggested that fatty acids interact directly with bitter substances through hydrogen bonds and hydrophobic interactions to form insoluble binary complexes that mask bitterness.

  20. The Use of the Schizonticidal Agent Quinine Sulfate to Prevent Pond Crashes for Algal-Biofuel Production.

    Science.gov (United States)

    Xu, Chunyan; Wu, Kangyan; Van Ginkel, Steve W; Igou, Thomas; Lee, Hwa Jong; Bhargava, Aditya; Johnston, Rachel; Snell, Terry; Chen, Yongsheng

    2015-11-17

    Algal biofuels are investigated as a promising alternative to petroleum fuel sources to satisfy transportation demand. Despite the high growth rate of algae, predation by rotifers, ciliates, golden algae, and other predators will cause an algae in open ponds to crash. In this study, Chlorella kessleri was used as a model alga and the freshwater rotifer, Brachionus calyciflorus, as a model predator. The goal of this study was to test the selective toxicity of the chemical, quinine sulfate (QS), on both the alga and the rotifer in order to fully inhibit the rotifer while minimizing its impact on algal growth. The QS LC50 for B. calyciflorus was 17 µM while C. kessleri growth was not inhibited at concentrations <25 µM. In co-culture, complete inhibition of rotifers was observed when the QS concentration was 7.7 µM, while algal growth was not affected. QS applications to produce 1 million gallons of biodiesel in one year are estimated to be $0.04/gallon or ~1% of Bioenergy Technologies Office's (BETO) projected cost of $5/gge (gallon gasoline equivalent). This provides algae farmers an important tool to manage grazing predators in algae mass cultures and avoid pond crashes.

  1. Steady state and time-resolved fluorescence spectroscopy of quinine sulfate dication bound to sodium dodecylsulfate micelles: Fluorescent complex formation

    Energy Technology Data Exchange (ETDEWEB)

    Joshi, Sunita; Pant, Debi D., E-mail: ddpant@pilani.bits-pilani.ac.in

    2014-01-15

    Interaction of quinine sulfate dication (QSD) with anionic, sodium dodecylsulphate (SDS) surfactant has been studied at different premicellar, micellar and postmicellar concentrations in aqueous phase using steady state, time-resolved fluorescence and fluorescence anisotropy techniques. At premicellar concentrations of SDS, the decrease in absorbance, appearance of an extra fluorescence band at lower wavelengths and tri-exponential decay behavior of fluorescence, are attributed to complex formation between QSD molecules and surfactant monomers. At postmicellar concentrations the red shift in fluorescence spectrum, increase in quantum yield and increase in fluorescence lifetimes are attributed to incorporation of solute molecules to micelles. At lower concentrations of SDS, a large shift in fluorescence is observed on excitation at the red edge of absorption spectrum and this is explained in terms of distribution of ion pairs of different energies in the ground state and the observed fluorescence lifetime behavior corroborates with this model. The temporal fluorescence anisotropy decay of QSD in SDS micelles allowed determination of restriction on the motion of the fluorophore. All the different techniques used in this study reveal that the photophysics of QSD is very sensitive to the microenvironments of SDS micelles and QSD molecules reside at the water-micelle interface. -- Highlights: • Probe molecule is very sensitive to microenvironment of micelles. • Highly fluorescent ion-pair formation has been observed. • Modulated photophysics of probe molecule in micellar solutions has been observed. • Probe molecules strongly bind with micelles and reside at probe–micelle interface.

  2. Nonspecifically enhanced therapeutic effects of vincristine on multidrug-resistant cancers when coencapsulated with quinine in liposomes.

    Science.gov (United States)

    Xu, Yuzhen; Qiu, Liyan

    2015-01-01

    The use of vincristine (VCR) to treat cancer has been limited by its dose-dependent toxicity and development of drug resistance after repeated administrations. In this study, we investigated the mechanism by which quinine hydrochloride (QN) acts as a sensitizer for VCR. Our experiments used three kinds of multidrug-resistant cancer cells and demonstrated that QN worked by inducing intracellular depletion of adenosine triphosphate, increasing adenosine triphosphatase activity, and decreasing P-glycoprotein expression. Based on these results, we designed and prepared a VCR and QN codelivery liposome (VQL) and investigated the effect of coencapsulated QN on the in vitro cytotoxicity of VCR in cells and three-dimensional multicellular tumor spheroids. The antitumor effects of the formulation were also evaluated in multidrug-resistant tumor-bearing mice. The results of this in vivo study indicated that VQL could reverse VCR resistance. In addition, it reduced tumor volume 5.4-fold when compared with other test groups. The data suggest that VQL could be a promising nanoscaled therapeutic agent to overcome multidrug resistance, and may have important clinical implications for the treatment of cancer.

  3. The Use of the Schizonticidal Agent Quinine Sulfate to Prevent Pond Crashes for Algal-Biofuel Production

    Directory of Open Access Journals (Sweden)

    Chunyan Xu

    2015-11-01

    Full Text Available Algal biofuels are investigated as a promising alternative to petroleum fuel sources to satisfy transportation demand. Despite the high growth rate of algae, predation by rotifers, ciliates, golden algae, and other predators will cause an algae in open ponds to crash. In this study, Chlorella kessleri was used as a model alga and the freshwater rotifer, Brachionus calyciflorus, as a model predator. The goal of this study was to test the selective toxicity of the chemical, quinine sulfate (QS, on both the alga and the rotifer in order to fully inhibit the rotifer while minimizing its impact on algal growth. The QS LC50 for B. calyciflorus was 17 µM while C. kessleri growth was not inhibited at concentrations <25 µM. In co-culture, complete inhibition of rotifers was observed when the QS concentration was 7.7 µM, while algal growth was not affected. QS applications to produce 1 million gallons of biodiesel in one year are estimated to be $0.04/gallon or ~1% of Bioenergy Technologies Office’s (BETO projected cost of $5/gge (gallon gasoline equivalent. This provides algae farmers an important tool to manage grazing predators in algae mass cultures and avoid pond crashes.

  4. Quinine dimers are potent inhibitors of the Plasmodium falciparum chloroquine resistance transporter and are active against quinoline-resistant P. falciparum.

    Science.gov (United States)

    Hrycyna, Christine A; Summers, Robert L; Lehane, Adele M; Pires, Marcos M; Namanja, Hilda; Bohn, Kelsey; Kuriakose, Jerrin; Ferdig, Michael; Henrich, Philipp P; Fidock, David A; Kirk, Kiaran; Chmielewski, Jean; Martin, Rowena E

    2014-03-21

    Chloroquine (CQ) resistance in the human malaria parasite Plasmodium falciparum is primarily conferred by mutations in the "chloroquine resistance transporter" (PfCRT). The resistance-conferring form of PfCRT (PfCRT(CQR)) mediates CQ resistance by effluxing the drug from the parasite's digestive vacuole, the acidic compartment in which CQ exerts its antiplasmodial effect. PfCRT(CQR) can also decrease the parasite's susceptibility to other quinoline drugs, including the current antimalarials quinine and amodiaquine. Here we describe interactions between PfCRT(CQR) and a series of dimeric quinine molecules using a Xenopus laevis oocyte system for the heterologous expression of PfCRT and using an assay that detects the drug-associated efflux of H(+) ions from the digestive vacuole in parasites that harbor different forms of PfCRT. The antiplasmodial activities of dimers 1 and 6 were also examined in vitro (against drug-sensitive and drug-resistant strains of P. falciparum) and in vivo (against drug-sensitive P. berghei). Our data reveal that the quinine dimers are the most potent inhibitors of PfCRT(CQR) reported to date. Furthermore, the lead compounds (1 and 6) were not effluxed by PfCRT(CQR) from the digestive vacuole but instead accumulated to very high levels within this organelle. Both 1 and 6 exhibited in vitro antiplasmodial activities that were inversely correlated with CQ. Moreover, the additional parasiticidal effect exerted by 1 and 6 in the drug-resistant parasites was attributable, at least in part, to their ability to inhibit PfCRT(CQR). This highlights the potential for devising new antimalarial therapies that exploit inherent weaknesses in a key resistance mechanism of P. falciparum.

  5. Reduction of spleen size in a child with Hyperreactive Malarious Splenomegaly (HMS treated outside the Brazilian endemic area of malaria with only one course of quinine

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    Maria Imaculada Muniz-Junqueira

    1992-12-01

    Full Text Available We report the clinical picture, treatment and evolution of a child with hyperreactive malarious splenomegaly treated outside the endemic area of malaria. The patient presented gross splenomegaly, proceeded from an area where malaria is endemic, showed increased immunoglobulins levels, high antimalarial antibody titres and hepatic sinusoidal lymphocytosis. The child did not return to an area where malaria is endemic and showed a favorable response to only one course of quinine. The response of this patient to limited antimalarial therapy suggests the importance of reinfection with malaria in the development and maintenance of this syndrome.

  6. Provider knowledge of treatment policy and dosing regimen with artemether-lumefantrine and quinine in malaria-endemic areas of western Kenya.

    Science.gov (United States)

    Watsierah, Carren A; Onyango, Rosebella O; Ombaka, James H; Abong'o, Benard O; Ouma, Collins

    2012-12-29

    Due to widespread anti-malarial drug resistance in many countries, Kenya included, artemisinin-based Combination Therapy (ACT) has been adopted as the most effective treatment option against malaria. Artemether-lumefantrine (AL) is the first-line ACT for treatment of uncomplicated malaria in Kenya, while quinine is preferred for complicated and severe malaria. Information on the providers' knowledge and practices prior to or during AL and quinine implementation is scanty. The current study evaluated providers' knowledge and practices of treatment policy and dosing regimens with AL and quinine in the public, private and not-for-profit drug outlets. A cross-sectional survey using three-stage sampling of 288 (126 public, 96 private and 66 not-for-profits) providers in drug outlets was conducted in western Kenya in two Plasmodium falciparum-endemic regions with varying malarial risk. Information on provider in-service training, knowledge (qualification, treatment policy, dosing regimen, recently banned anti-malarials) and on practices (request for written prescription, prescription of AL, selling partial packs and advice given to patients after prescription), was collected. Only 15.6% of providers in private outlets had received any in-service training on AL use. All (100%) in public and majority (98.4%) in not-for-profit outlets mentioned AL as first line-treatment drug. Quinine was mentioned as second-line drug by 47.9% in private outlets. A total of 92.0% in public, 57.3% in private and 78.8% in not-for-profit outlets stated correct AL dose for adults. A total of 85.7% of providers in public, 30.2% in private and 41.0% in not-for-profit outlets were aware that SP recommendations changed from treatment for mild malaria to IPTp in high risk areas. In-service training influenced treatment regimen for uncomplicated malaria (P = 0.039 and P = 0.039) and severe malaria (P < 0.0001 and P = 0.002) in children and adults, respectively. Most (82.3%) of private

  7. Provider knowledge of treatment policy and dosing regimen with artemether-lumefantrine and quinine in malaria-endemic areas of western Kenya

    Directory of Open Access Journals (Sweden)

    Watsierah Carren A

    2012-12-01

    Full Text Available Abstract Background Due to widespread anti-malarial drug resistance in many countries, Kenya included, artemisinin-based Combination Therapy (ACT has been adopted as the most effective treatment option against malaria. Artemether-lumefantrine (AL is the first-line ACT for treatment of uncomplicated malaria in Kenya, while quinine is preferred for complicated and severe malaria. Information on the providers’ knowledge and practices prior to or during AL and quinine implementation is scanty. The current study evaluated providers’ knowledge and practices of treatment policy and dosing regimens with AL and quinine in the public, private and not-for-profit drug outlets. Methods A cross-sectional survey using three-stage sampling of 288 (126 public, 96 private and 66 not-for-profits providers in drug outlets was conducted in western Kenya in two Plasmodium falciparum-endemic regions with varying malarial risk. Information on provider in-service training, knowledge (qualification, treatment policy, dosing regimen, recently banned anti-malarials and on practices (request for written prescription, prescription of AL, selling partial packs and advice given to patients after prescription, was collected. Results Only 15.6% of providers in private outlets had received any in-service training on AL use. All (100% in public and majority (98.4% in not-for-profit outlets mentioned AL as first line-treatment drug. Quinine was mentioned as second-line drug by 47.9% in private outlets. A total of 92.0% in public, 57.3% in private and 78.8% in not-for-profit outlets stated correct AL dose for adults. A total of 85.7% of providers in public, 30.2% in private and 41.0% in not-for-profit outlets were aware that SP recommendations changed from treatment for mild malaria to IPTp in high risk areas. In-service training influenced treatment regimen for uncomplicated malaria (P = 0.039 and P = 0.039 and severe malaria (P P = 0.002 in children and adults

  8. In vitro susceptibility to quinine and microsatellite variations of the Plasmodium falciparum Na+/H+ exchanger (Pfnhe-1 gene: the absence of association in clinical isolates from the Republic of Congo

    Directory of Open Access Journals (Sweden)

    Rogier Christophe

    2011-02-01

    Full Text Available Abstract Background Quinine is still recommended as an effective therapy for severe cases of Plasmodium falciparum malaria, but the parasite has developed resistance to the drug in some cases. Investigations into the genetic basis for quinine resistance (QNR suggest that QNR is complex and involves several genes, with either an additive or a pairwise effect. The results obtained when assessing one of these genes, the plasmodial Na+/H+ exchanger, Pfnhe-1, were found to depend upon the geographic origin of the parasite strain. Most of the associations identified have been made in Asian strains; in contrast, in African strains, the influence of Pfnhe on QNR is not apparent. However, a recent study carried out in Kenya did show a significant association between a Pfnhe polymorphism and QNR. As genetic differences may exist across the African continent, more field data are needed to determine if this association exists in other African regions. In the present study, association between Pfnhe and QNR is investigated in a series of isolates from central Africa. Methods The sequence analysis of the polymorphisms at the Pfnhe-1 ms4760 microsatellite and the evaluation of in vitro quinine susceptibility (by isotopic assay were conducted in 74 P. falciparum isolates from the Republic of Congo. Results Polymorphisms in the number of DNNND or NHNDNHNNDDD repeats in the Pfnhe-1 ms4760 microsatellite were not associated with quinine susceptibility. Conclusions The polymorphism in the microsatellite ms4760 in Pfnhe-1 that cannot be used to monitor quinine response in the regions of the Republic of Congo, where the isolates came from. This finding suggests that there exists a genetic background associated with geographic area for the association that will prevent the use of Pfnhe as a molecular marker for QNR. The contribution of Pfnhe to the in vitro response to quinine remains to be assessed in other regions, including in countries with different levels of

  9. Restoration of quinine-stimulated Fos-immunoreactive neurons in the central nucleus of the amygdala and gustatory cortex following reinnervation or cross-reinnervation of the lingual taste nerves in rats.

    Science.gov (United States)

    King, Camille Tessitore; Garcea, Mircea; Spector, Alan C

    2014-08-01

    Remarkably, when lingual gustatory nerves are surgically rerouted to inappropriate taste fields in the tongue, some taste functions recover. We previously demonstrated that quinine-stimulated oromotor rejection reflexes and neural activity (assessed by Fos immunoreactivity) in subregions of hindbrain gustatory nuclei were restored if the posterior tongue, which contains receptor cells that respond strongly to bitter compounds, was cross-reinnervated by the chorda tympani nerve. Such functional recovery was not seen if instead, the anterior tongue, where receptor cells are less responsive to bitter compounds, was cross-reinnervated by the glossopharyngeal nerve, even though this nerve typically responds robustly to bitter substances. Thus, recovery depended more on the taste field being reinnervated than on the nerve itself. Here, the distribution of quinine-stimulated Fos-immunoreactive neurons in two taste-associated forebrain areas was examined in these same rats. In the central nucleus of the amygdala (CeA), a rostrocaudal gradient characterized the normal quinine-stimulated Fos response, with the greatest number of labeled cells situated rostrally. Quinine-stimulated neurons were found throughout the gustatory cortex, but a "hot spot" was observed in its anterior-posterior center in subregions approximating the dysgranular/agranular layers. Fos neurons here and in the rostral CeA were highly correlated with quinine-elicited gapes. Denervation of the posterior tongue eliminated, and its reinnervation by either nerve restored, numbers of quinine-stimulated labeled cells in the rostralmost CeA and in the subregion approximating the dysgranular gustatory cortex. These results underscore the remarkable plasticity of the gustatory system and also help clarify the functional anatomy of neural circuits activated by bitter taste stimulation.

  10. Intravenous artesunate versus intravenous quinine in the treatment of severe falciparum malaria: a retrospective evaluation from a UK centre

    Science.gov (United States)

    Eder, Marcus; Farne, Hugo; Cargill, Tamsin; Abbara, Aula; Davidson, Robert N

    2012-01-01

    Introduction Despite evidence from developing world trials that intravenous (IV) artesunate (AS) is superior to IV quinine (Q) in severe falciparum malaria (FM), IV AS remains unlicensed in the UK with national guidelines listing it as an acceptable alternative to IV Q as the drug of choice. We retrospectively evaluate the safety and effectiveness of IV AS in returning travellers with severe FM. Methods We identified adults admitted to the Infectious Diseases unit with severe FM and treated with IV Q (1991–2009) or IV AS (2009–2011). Outcomes included adverse events, mortality, length of stay, admission to intensive care and, where data were available, parasite/fever clearance time and hypoglycaemic events. Results Of 167 patients, 24 received IV AS and 143 IV Q. There was one potential AS-associated adverse event, a case of late onset haemolysis. Median length of stay (LOS) was significantly shorter for AS (3.5 versus 5 days, P = 0.017), even after adjusting for African ethnicity (for LOS ⩾3 days, mhor = 0.33, P = 0.027; crude OR = 0.29, P = 0.013). In the AS group, there were no fatalities (versus five in Q group, NS) and fewer intensive care unit (ICU) admissions (NS). Median parasite clearance was significantly faster in AS (65 versus 85 hours in Q, P = 0.0045) with no hypoglycaemic episodes (versus five in Q). Discussion We found IV AS to be safe and effective, with shorter LOS, faster parasite and fever clearance, no fatalities or hypoglycaemic events, and fewer ICU admissions versus IV Q. This corroborates both developing world trials and smaller European case series (although these lacked comparison groups). As well as obvious benefits for patients, there are potential resource savings. A case of late-onset haemolysis may represent an adverse event, particularly as it has been documented elsewhere, warranting further investigation. Nonetheless, our experience suggests IV AS should be first-line for treating severe FM in the UK

  11. Interaction of quinine sulfate with anionic micelles of sodium dodecylsulfate: A time-resolved fluorescence spectroscopy at different pH

    Science.gov (United States)

    Joshi, Sunita; Pant, Debi D.

    2015-09-01

    Photophysical behavior and rotational relaxation dynamics of quinine sulfate (QS) in anionic surfactant, sodium dodecylsulfate (SDS) at different pH have been studied using steady state and time resolved fluorescence spectroscopy. It has been observed that the cationic form of quinine sulfate (at pH 2) forms a fluorescent ion pair complex with the surfactant molecules at lower concentrations of surfactant. However, for higher concentrations of SDS, the probe molecules bind strongly with the micelles and reside at the water-micelle interface. At pH 7, QS is singly protonated in bulk aqueous solution. At lower concentrations of SDS aggregation between probe and surfactant molecules has been observed. However, for higher concentrations of SDS, an additional fluorescence peak corresponding to dicationic form of QS appears and this has been attributed to double protonation of the QS molecule in micellar solution. At pH 7, in the presence of SDS micelles, the photophysical properties of QS showed substantial changes compared to that in the bulk water solution. At pH 12, an increase in fluorescence intensity and lifetime has been observed and this has been attributed to the increase in radiative rate due to the incorporation of QS at the micelle-water interface. The local pH at micellar surface has been found different from the pH of bulk solution.

  12. Development, validation and comparison of NIR and Raman methods for the identification and assay of poor-quality oral quinine drops.

    Science.gov (United States)

    Mbinze, J K; Sacré, P-Y; Yemoa, A; Mavar Tayey Mbay, J; Habyalimana, V; Kalenda, N; Hubert, Ph; Marini, R D; Ziemons, E

    2015-01-01

    Poor quality antimalarial drugs are one of the public's major health problems in Africa. The depth of this problem may be explained in part by the lack of effective enforcement and the lack of efficient local drug analysis laboratories. To tackle part of this issue, two spectroscopic methods with the ability to detect and to quantify quinine dihydrochloride in children's oral drops formulations were developed and validated. Raman and near infrared (NIR) spectroscopy were selected for the drug analysis due to their low cost, non-destructive and rapid characteristics. Both of the methods developed were successfully validated using the total error approach in the range of 50-150% of the target concentration (20%W/V) within the 10% acceptance limits. Samples collected on the Congolese pharmaceutical market were analyzed by both techniques to detect potentially substandard drugs. After a comparison of the analytical performance of both methods, it has been decided to implement the method based on NIR spectroscopy to perform the routine analysis of quinine oral drop samples in the Quality Control Laboratory of Drugs at the University of Kinshasa (DRC).

  13. Fluorescence Experiments with Quinine

    Science.gov (United States)

    O'Reilly, James E.

    1975-01-01

    Describes a series of experiments which illustrate the analytical capabilities of fluorescence, and outlines two straightforward analyses involving real analyses. These experiments are suitable for an undergraduate instrumental analysis course and require approximately six to seven hours of laboratory time. (MLH)

  14. Determination of phenols by flow injection and liquid chromatography with on-line quinine-sensitized photo-oxidation and quenched luminol chemiluminescence detection

    Energy Technology Data Exchange (ETDEWEB)

    Zhang Wei; Danielson, Neil D

    2003-10-01

    An on-line quinine-sensitized photo-oxidation with quenched chemiluminescence (CL) detection method is developed for phenols using flow injection (FI) and liquid chromatography (LC). This detection method is based on the decrease of light emission from the luminol CL reaction due to the photo-oxidation of phenols that scavenge the photogenerated reactive oxygen species (e.g. singlet oxygen ({sup 1}O{sub 2}) and superoxide (O{sub 2}{center_dot}{sup -})). On-line photo-oxidation is achieved using a coil photo-reactor made from fluoroethylene-propylene copolymer tubing (3048 mmx0.25 mm i.d.) coiled around a mercury UV lamp. A buffer of pH 7 and a concentration of 350 {mu}M for quinine sulfate are determined optimum for the sensitized photo-oxidation. Using a carrier system flow rate of 60 {mu}l/min, calibration curves taken by FI for 10 phenolic compounds in aqueous solutions showed this decreasing sensitivity order: 4-chlorophenol, phenol, 4-nitrophenol, 3-hydroxy-L-kynurenine, 2-nitrophenol, salicylate, 3-nitrophenol, catechol, 2,4-dinitrophenol, and 2,4-dichlorophenol. This detection method using two tandem coil photo-reactors is also applied for the LC separation of phenol, 4-nitrophenol and 4-chlorophenol on an octadecyl (C18) silica LC column using acetonitrile-H{sub 2}O (40:60, v/v) as a mobile phase. The quenched CL detection limits (about 1 {mu}M or 20 pmol) for phenol and 4-chlorophenol are comparable to those for UV detection at 254 nm. Some selectivity in the quenched CL detection is evident by no interference in the FI phenol response even when benzaldehyde and phenethanol concentrations are 8 and 15 times that of phenol.

  15. Unconditioned oromotor taste reactivity elicited by sucrose and quinine is unaffected by extensive bilateral damage to the gustatory zone of the insular cortex in rats.

    Science.gov (United States)

    King, Camille Tessitore; Hashimoto, Koji; Blonde, Ginger D; Spector, Alan C

    2015-03-01

    Rats display stereotypical oromotor and somatic responses to small volumes of intraorally infused taste solutions. These behaviors, known as taste reactivity, are categorized by their association with ingestion or rejection and are thought to reflect the palatability of the stimulus. Because supracollicular decerebrate rats display normal taste reactivity responses, it would appear that forebrain structures are not necessary for generating them. However, because moving the plane of transection rostrally, or damaging or manipulating specific ventral forebrain sites disrupts normal taste reactivity behavior, lesions of the gustatory cortex, a region that has been suggested to be involved with palatability processing, may do the same. In the current study, rats received two injections of either ibotenic acid (N=12) or vehicle (N=8), targeting the conventionally defined gustatory cortex in each hemisphere, and were implanted with intraoral cannulae. Following recovery, their responses to intraoral infusions (0.23ml in 1min) of dH2O, sucrose (1.0M and 0.1M), and quinine hydrochloride (3mM and 0.3mM) were video recorded. Analysis of brains with sufficient bilateral lesions (N=10) revealed that, on average, approximately 94% of the gustatory cortex was destroyed. These extensive bilateral lesions had no significant effect on taste reactivity; the numbers of ingestive and aversive responses to sucrose and quinine were similar between groups. Though these findings do not rule out involvement of the gustatory cortex in palatability processing, they make evident that the region of insular cortex destroyed is not necessary for the normal expression of unconditioned affective behavioral responses to taste stimuli.

  16. Artemether-lumefantrine to treat malaria in pregnancy is associated with reduced placental haemozoin deposition compared to quinine in a randomized controlled trial

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    Muehlenbachs Atis

    2012-05-01

    Full Text Available Abstract Background Data on efficacy of artemisinin-based combination therapy (ACT to treat Plasmodium falciparum during pregnancy in sub-Saharan Africa is scarce. A recent open label, randomized controlled trial in Mbarara, Uganda demonstrated that artemether-lumefantrine (AL is not inferior to quinine to treat uncomplicated malaria in pregnancy. Haemozoin can persist in the placenta following clearance of parasites, however there is no data whether ACT can influence the amount of haemozoin or the dynamics of haemozoin clearance. Methods Women attending antenatal clinics with weekly screening and positive blood smears by microscopy were eligible to participate in the trial and were followed to delivery. Placental haemozoin deposition and inflammation were assessed by histology. To determine whether AL was associated with increased haemozoin clearance, population haemozoin clearance curves were calculated based on the longitudinal data. Results Of 152 women enrolled in each arm, there were 97 and 98 placental biopsies obtained in the AL and quinine arms, respectively. AL was associated with decreased rates of moderate to high grade haemozoin deposition (13.3% versus 25.8%, which remained significant after correcting for gravidity, time of infection, re-infection, and parasitaemia. The amount of haemozoin proportionately decreased with the duration of time between treatment and delivery and this decline was greater in the AL arm. Haemozoin was not detected in one third of biopsies and the prevalence of inflammation was low, reflecting the efficacy of antenatal care with early detection and prompt treatment of malaria. Conclusions Placental haemozoin deposition was decreased in the AL arm demonstrating a relationship between pharmacological properties of drug to treat antenatal malaria and placental pathology at delivery. Histology may be considered an informative outcome for clinical trials to evaluate malaria control in pregnancy. Trial

  17. Disease-associated QT-shortage versus quinine associated QT-prolongation: age dependent ECG-effects in Ghanaian children with severe malaria

    Science.gov (United States)

    2014-01-01

    Background While several anti-malarials are known to affect the electric conduction system of the heart, less is known on the direct effects of Plasmodium falciparum infection. Some earlier studies point to a direct impact of Plasmodium falciparum infection on the electric conduction system of the heart. The aim of this study was to analyse infection- and drug-induced effects on the electric conduction system. Methods Children aged 12 months to 108 months with severe malaria were included in Kumasi, Ghana. In addition to basic demographic, clinical, biochemical and parasitological, biochemical data were measured data upon hospitalization (day 0) and 12-lead electrocardiograms were recorded before (day 0) and after (day 1) initiation of quinine therapy as well as after 42 (±3) days. Results A total of 180 children were included. Most children were tachycardic on day 0 but heart rate declined on day 1 and during follow up. The corrected QT intervals were longest on day 1 and shortest on day 0. Comparison of QT intervals with day 42 (healthy status) after stratification for age demonstrated that in the youngest (<24 months) this was mainly due to a QT shortage on day 0 while a QT prolongation on day 1 was most pronounced in the oldest (≥48 months). Nearly one third of the participating children had measurable 4-aminoquinoline levels upon admission, but no direct effect on the corrected QT intervals could be shown. Conclusion Severe P. falciparum infection itself can provoke changes in the electrophysiology of the heart, independent of anti-malarial therapy. Especially in young - thus non immune - children the effect of acute disease associated pre-treatment QT-shortage is more pronounced than quinine associated QT-prolongation after therapy. Nevertheless, neither malaria nor anti-malarial induced effects on the electrophysiology of the heart were associated with clinically relevant arrhythmias in the present study population. PMID:24902591

  18. Profil de l'hémogramme chez les enfants paludéens de 0 à 5 ans sous quinine, cas de la République Démocratique du Congo

    Science.gov (United States)

    Kabamba, Arsène Tshikongo; Lukumwena, Zet Kalala; Longanga, Albert Otshudi

    2014-01-01

    Le paludisme constitue un des problèmes de santé publique majeur en République Démocratique du Congo (RDC) à cause d'une part des risques d’épidémies dans certaines zones du pays et d'autre part à cause du nombre des malades et des décès qu'il provoque. Cette étude expose les aspects hématologiques liés à la prise de la quinine au cours du paludisme grave chez l'enfant. Pour ce faire, les prises de sang ont été effectuées à deux groupes d'enfants, dans différents centres hospitaliers de Lubumbashi: le premier groupe est constitué d'enfants gravement impaludés et sous traitement à la quinine; tandis que le second groupe, composé d'enfants impaludés aussi mais sans traitement à la quinine et sert de groupe témoin. Ces prélèvements ont été analysés pour une exploration de l'hémogramme par un dosage sérique des paramètres hématologiques ci-après: les globules rouges, l'hémoglobine, l'hématocrite et le volume globulaire moyen. Les résultats obtenus montrent une différence statistiquement significative entre les deux groupes d'enfants examinés. En effet, dans la majorité des cas, une augmentation des taux plasmatiques des paramètres hématologiques analysés a été observée dans le groupe d'enfants impaludés sous traitement à la quinine, traduisant ainsi l'apport de la quinine sur la stabilisation de l'hémogramme au cours d'un paludisme grave chez l'enfant de moins de cinq ans. PMID:25722768

  19. Antagonistic effect of alkaloids and saponins on bioactivity in the quinine tree (Rauvolfia caffra sond.): further evidence to support biotechnology in traditional medicinal plants.

    Science.gov (United States)

    Milugo, Trizah K; Omosa, Leonida K; Ochanda, James O; Owuor, Bethwell O; Wamunyokoli, Fred A; Oyugi, Julius O; Ochieng, Joel W

    2013-10-26

    The Quinine tree (Rauvolfia caffra) is used as a medicinal plant among traditional communities in many countries to manage tumors and other diseases associated with oxidative stress. To validate indigenous knowledge and possibly position this herb for technology uptake and utilization, we established the level of antioxidant activity in R. caffra, and probed for the presence of associated phytochemicals. Antioxidant activity was determined on 1,1-diphenyl-2-picrylhydrazyl (DPPH) while major phytochemicals were identified by multiple tests on methanol fractions. R. caffra showed promise as a cure, with antioxidant activity comparable to the commercially used drug quercetin (R. caffra = 79.7% ±1.9; quercetin = 82.6% ± 2.0). However, we found two phytochemicals with possible antagonistic effect: co-occurrence of alkaloids and saponins significantly reduced antioxidant activity (alkaloids only = 63%; alkaloids plus saponins = 15%; steroids, terpenoids and cardiac glycosides = 82%), thus alkaloids and saponins should be exclusive to each other in drug formulations. Antagonistic relationship among phytochemicals would affect the efficacy of crude extracts as used in traditional medicine. Unlike in herbal medicine, use of modern biotechnology in extraction, purification and design of optimal combinations will ensure efficient drug formulations with optimum bioactivity and minimum toxicity. Metabolic pathway engineering under a controlled environment may optimize availability of desired compounds.

  20. 吡咯喹啉醌毒理学安全性评价%Toxicological safety assessment of the cpyrrologuinoline quinine

    Institute of Scientific and Technical Information of China (English)

    王丽云; 赵荣; 施伟庆; 陈耿

    2012-01-01

    目的 为吡咯喹啉醌( cpyrrologuinoline quinine,PQQ)安全性评价提供毒理学依据 方法 按《保健食品检验与评价技术规范的要求》,观察PQQ对实验动物的影响 结果 雌雄小鼠急性经口LD50值分别为3 690 mg/kg和2 710 mg/kg.BW,未见雌雄小鼠骨髓嗜多染红细胞的致微核作用,未显示雄性小鼠精子的诱变活性,无论加及不加S9未见对测试菌株的诱变活性;90天喂养体重、增重、摄食量、食物利用率、肝/体、肾/体、脾/体和睾/体比、血液、生化和病理组织学检查与对照组值比较均无显著性差异(P>0.05).结论 在本试验条件下,PQQ属低毒,未见明显致突变作用,大鼠90天喂养最大末观察到有害作用剂量(NOAEL)为15 mg/kg.BW..

  1. Adsorption Behavior of Quinine Sulfate onto Medicinal Activated Carbon%药用活性炭对硫酸奎宁吸附性能的研究

    Institute of Scientific and Technical Information of China (English)

    付国家; 郭庆杰

    2011-01-01

    研究了药用活性炭对硫酸奎宁吸附性能的影响,并采用Langmuir和Freundlich 吸附等温线模型拟合了活性炭对硫酸奎宁的吸附行为.结果表明:硫酸奎宁吸附量随药用活性炭用量的增加呈上升趋势,但吸附效率却呈下降趋势.在所研究的条件下,活性炭对硫酸奎宁的吸附量随温度和初始浓度的升高而增大,在313 K吸附值最大为123.457mg·g-1.与Freundlich吸附模型(r2f<0.95)相比,Langmuir吸附等温线拟合较好(r21>0.97),说明Langmuir模型适用于所研究的体系.%In this study, the adsorption effect of medicinal activated carbon for quinine sulfate(QS) removal from aqueous solutions was investigated. The adsorption behavior of QS onto medicinal activated carbon was fitted with Langmuir and Freundlich adsorption isotherm models. The results showed that an increase the dosage of activated carbon enhanced the adsorption capacity, but failed to increase the QS removal efficiency. In the studied conditions, the adsorption of QS onto activated carbon rised with increasing temperature and the initial QS concentration, and the calculated maximum adsorption capacity of activated carbon was 123. 457 mg ? G-1 at 313 K. Compared with Freundlich model (r120. 97).

  2. Diastereo- and enantioseparation of a N(α)-Boc amino acid with a zwitterionic quinine-based stationary phase: focus on the stereorecognition mechanism.

    Science.gov (United States)

    Ianni, Federica; Carotti, Andrea; Marinozzi, Maura; Marcelli, Gloria; Di Michele, Alessandro; Sardella, Roccaldo; Lindner, Wolfgang; Natalini, Benedetto

    2015-07-23

    A chiral chromatography method enabling the simultaneous diastereo- and enantioseparation of N(α)-Boc-N(4)-(hydroorotyl)-4-aminophenylalanine [Boc-Aph(Hor)-OH, 1] was optimized with a quinine-based zwitterionic stationary phase. The polar-ionic eluent system consisting of ACN:MeOH:water-49.7:49.7:0.6 (v/v/v) with formic acid (4.0mM) and diethylamine (2.5mM), allowed the successful separation of the four acid stereoisomers: αd,d-/d,l-1=1.08; αd,l-/l,d-1=1.08; αl,d-/l,l-1=1.40. According to the in-house developed synthetic procedure and the recorded electronic circular dichroism spectra, the following stereoisomeric elution order was readily established in the optimal chromatographic conditions: d,d-1

  3. The Mu subunit of Plasmodium falciparum clathrin-associated adaptor protein 2 modulates in vitro parasite response to artemisinin and quinine.

    Science.gov (United States)

    Henriques, Gisela; van Schalkwyk, Donelly A; Burrow, Rebekah; Warhurst, David C; Thompson, Eloise; Baker, David A; Fidock, David A; Hallett, Rachel; Flueck, Christian; Sutherland, Colin J

    2015-05-01

    The emergence of drug-resistant parasites is a serious threat faced by malaria control programs. Understanding the genetic basis of resistance is critical to the success of treatment and intervention strategies. A novel locus associated with antimalarial resistance, ap2-mu (encoding the mu chain of the adaptor protein 2 [AP2] complex), was recently identified in studies on the rodent malaria parasite Plasmodium chabaudi (pcap2-mu). Furthermore, analysis in Kenyan malaria patients of polymorphisms in the Plasmodium falciparum ap2-mu homologue, pfap2-mu, found evidence that differences in the amino acid encoded by codon 160 are associated with enhanced parasite survival in vivo following combination treatments which included artemisinin derivatives. Here, we characterize the role of pfap2-mu in mediating the in vitro antimalarial drug response of P. falciparum by generating transgenic parasites constitutively expressing codon 160 encoding either the wild-type Ser (Ser160) or the Asn mutant (160Asn) form of pfap2-mu. Transgenic parasites carrying the pfap2-mu 160Asn allele were significantly less sensitive to dihydroartemisinin using a standard 48-h in vitro test, providing direct evidence of an altered parasite response to artemisinin. Our data also provide evidence that pfap2-mu variants can modulate parasite sensitivity to quinine. No evidence was found that pfap2-mu variants contribute to the slow-clearance phenotype exhibited by P. falciparum in Cambodian patients treated with artesunate monotherapy. These findings provide compelling evidence that pfap2-mu can modulate P. falciparum responses to multiple drugs. We propose that this gene should be evaluated further as a potential molecular marker of antimalarial resistance.

  4. Polymorphism of Plasmodium falciparum Na+/H+ exchanger is indicative of a low in vitro quinine susceptibility in isolates from Viet Nam

    Directory of Open Access Journals (Sweden)

    Thanh Nguyen

    2011-06-01

    Full Text Available Abstract Background The Plasmodium falciparum NA+/H+ exchanger (pfnhe1, gene PF13_0019 has recently been proposed to influence quinine (QN susceptibility. However, its contribution to QN resistance seems to vary geographically depending on the genetic background of the parasites. Here, the role of this gene was investigated in in vitro QN susceptibility of isolates from Viet Nam. Method Ninety-eight isolates were obtained from three different regions of the Binh Phuoc and Dak Nong bordering Cambodia provinces during 2006-2008. Among these, 79 were identified as monoclonal infection and were genotyped at the microsatellite pfnhe1 ms4760 locus and in vitro QN sensitivity data were obtained for 51 isolates. Parasite growth was assessed in the field using the HRP2 immunodetection assay. Results Significant associations were found between polymorphisms at pfnhe1 microsatellite ms4760 and susceptibility to QN. Isolates with two or more DNNND exhibited much lower susceptibility to QN than those harbouring zero or one DNNND repeats (median IC50 of 682 nM versus median IC50 of 300 nM; p = 0.0146 while isolates with one NHNDNHNNDDD repeat presented significantly reduced QN susceptibility than those who had two (median IC50 of 704 nM versus median IC50 of 375 nM; p pfcrt76T and wild-type pfmdr1 (> 95% thus preventing analysis of associations with these mutations. Interestingly, area with the highest median QN IC50 showed also the highest percentage of isolates carrying the pfnhe1 haplotype 7. Conclusions The haplotype 7 which is the typical Asian profile is likely well-adapted to high drug pressure in this area and may constitute a good genetic marker to evaluate the dissemination of QNR in this part of the world.

  5. Acceptability and efficacy of intra-rectal quinine alkaloids as a pre-transfer treatment of non-per os malaria in peripheral health care facilities in Mopti, Mali

    Directory of Open Access Journals (Sweden)

    Sacko Massambou

    2007-05-01

    Full Text Available Abstract Background The acceptability and efficacy of a new kit with a new formulation of quinine alkaloids designed for the intra-rectal administration in the treatment of non-per os malaria was assessed in the peripheral health care system of Mopti, Mali. Methods A single-arm trial was conducted from August 2003 to January 2004. An initial dose of diluted quinine alkaloids (20 mg/kg Quinimax® was administered by the intra-rectal route to children with presumptive non per-os malaria at six peripheral heath care centres. The children were then referred to two referral hospitals where standard inpatient care including intravenous route were routinely provided. A malaria thick smear was done at inclusion and a second malaria thick smear after arrival at the referral facility, where a more complete clinical examination and laboratory testing was done to confirm diagnosis. Confirmed cases of severe malaria or others diseases were treated according to national treatment guidelines. Cases of non per-os malaria received a second dose of intra rectal quinine alkaloids. Primary outcome was acceptability of the intra rectal route by children and their parents as well as the ease to handle the kit by health care workers. Results The study included 134 children with a median age of 33 months and 53.7% were male. Most of the children (67% and 92% of parents or guardians readily accepted the intra-rectal route; 84% of health care workers found the kit easy to use. At the peripheral health care centres, 32% of children had a coma score ≤ 3 and this was reduced to 10% at the referral hospital, following one dose of intra-rectal quinine alkaloids (IRQA. The mean time to availability of oral route treatment was 1.8 ± 1.1 days. Overall, 73% of cases were confirmed severe malaria and for those the case fatality rate was 7.2%. Conclusion IRQA was well accepted by children, their parents/guardians and by the health workers at peripheral health facilities in Mopti

  6. Diastereo- and enantioseparation of a N{sup α}-Boc amino acid with a zwitterionic quinine-based stationary phase: Focus on the stereorecognition mechanism

    Energy Technology Data Exchange (ETDEWEB)

    Ianni, Federica; Carotti, Andrea; Marinozzi, Maura; Marcelli, Gloria [Department of Pharmaceutical Sciences, University of Perugia, Via Fabretti 48, 06123 Perugia (Italy); Di Michele, Alessandro [Department of Physics and Geology, University of Perugia, Via Pascoli 1, 06123 Perugia (Italy); Sardella, Roccaldo, E-mail: roccaldo.sardella@unipg.it [Department of Pharmaceutical Sciences, University of Perugia, Via Fabretti 48, 06123 Perugia (Italy); Lindner, Wolfgang [Department of Analytical Chemistry, University of Vienna, Währinger Strasse 38, 1090 Vienna (Austria); Natalini, Benedetto [Department of Pharmaceutical Sciences, University of Perugia, Via Fabretti 48, 06123 Perugia (Italy)

    2015-07-23

    Highlights: • The ZWIX(+) column allowed getting the Boc-Aph(Hor)-OH (1) isomeric peaks resolved. • ECD studies and molecular dynamic simulations allowed to assign the elution order. • Molecular descriptors revealed the active role of achiral elements of the CSP. - Abstract: A chiral chromatography method enabling the simultaneous diastereo- and enantioseparation of N{sup α}-Boc-N{sup 4}-(hydroorotyl)-4-aminophenylalanine [Boc-Aph(Hor)-OH, 1] was optimized with a quinine-based zwitterionic stationary phase. The polar-ionic eluent system consisting of ACN:MeOH:water—49.7:49.7:0.6 (v/v/v) with formic acid (4.0 mM) and diethylamine (2.5 mM), allowed the successful separation of the four acid stereoisomers: α{sub D,D-/D,L-1} = 1.08; α{sub D,L-/L,D-1} = 1.08; α{sub L,D-/L,L-1} = 1.40. According to the in-house developed synthetic procedure and the recorded electronic circular dichroism spectra, the following stereoisomeric elution order was readily established in the optimal chromatographic conditions: D,D-1 < D,L-1 < L,D-1 < L,L-1. With the aim of better understanding the molecular basis of the retention behaviour of the four stereoisomers in the employed chromatographic system and conditions, a computational protocol consisting in molecular dynamics simulations was applied. The use of the three descriptors INTER (in kcal mol{sup −1}, encoding for the interaction energy between the selector SO unit and the whole system), INTER-SA (in kcal mol{sup −1}, encoding for the interaction energy between SO and the sole selectand SA), and SELF (in kcal mol{sup −1}, encoding for the conformational energy of SA relative to its minimum energy registered by the collected snapshots) revealed the active role of achiral sub-structural elements of the chiral stationary phase and eluent components in the overall stereorecognition mechanism.

  7. Study on the resonance light scattering spectra of the interaction of quinine dihydrochloride with perfluorooctane sulfonate and its analytical applications%盐酸奎宁与全氟辛烷磺酸体系的共振光散射光谱研究及其分析应用

    Institute of Scientific and Technical Information of China (English)

    吴飞; 谭克俊; 刘忠德

    2011-01-01

    研究了盐酸奎宁(Quinine dihydrochloride,简称Quinine)与全氟辛烷磺酸(perfluorooctane sulfonate,简称PFOS)相互作用的共振光散射(resonance light scattering,RLS)光谱,并建立了PFOS的共振光散射分析方法.在pH值为2.87的Britton-Robinson(BR)缓冲溶液中,全氟辛烷磺酸根阴离子与质子化的盐酸奎宁通过静电引力和疏水作用形成2:1的离子缔合物,引起共振光散射强度(IRLS)显著增强,最大散射波长位于283nm处,增强的散射信号强度与PFOS浓度在0.10-50.0μmol/L范围内呈线性关系,据此建立了测定PFOS的散射分析方法,检测限为9.88nmol/L.讨论了体系的最佳反应条件及外来物质的干扰,同时研究了体系的吸收光谱及荧光光谱,并探讨了反应机理.本方法用于水样及人体血清样品中PFOS的测定,RSD≤4.2%.%The resonance light scattering(RLS) spectra of the interaction Quinine dihydrochloride (Quinine)with perfluorooctane sulfonate (PFOS) was investigated. A RLS method for the determination of PFOS has been established. In pH 2.87 Britton-Robinson (BR) buffer solution, perfluorooctane sulfonate (PFOS) anions can react with the protonated Quinine by electrostatic forces and hydrophobic interactions to form 2:1 ion-association complexes and resulting in greatly enhanced resonance light scattering signals characterized by a peak at 283 nm, and the RLS intensity was proportional to the concentration of PFOS in the range of 0.10 ~ 5.00 μmol/L. The limit of detection is 9.88 nmol/L. In this paper, the optimum reaction conditions and the interference of foreign substances of the system were investigated. The absorption and fluorescence spectra of the system as well as the reaction mechanism were also discussed. This RLS method has been applied to the determination of PFOS in environmental samples and human serum samples with RSD ≤ 4.2%.

  8. Pyrroloquinoline quinine inhibits RANKL-mediated expression of NFATc1 in part via suppression of c-Fos in mouse bone marrow cells and inhibits wear particle-induced osteolysis in mice.

    Directory of Open Access Journals (Sweden)

    Lingbo Kong

    Full Text Available The effects of pyrroloquinoline quinine (PQQ on RANKL-induced osteoclast differentiation and on wear particle-induced osteolysis were examined in this study. PQQ inhibited RANKL-mediated osteoclast differentiation in bone marrow macrophages (BMMs in a dose-dependent manner without any evidence of cytotoxicity. The mRNA expression of c-Fos, NFATc1, and TRAP in RANKL-treated BMMs was inhibited by PQQ treatment. Moreover, RANKL-induced c-Fos and NFATc1 protein expression was suppressed by PQQ. PQQ additionally inhibited the bone resorptive activity of differentiated osteoclasts. Further a UHMWPE-induced murine calvaria erosion model study was performed to assess the effects of PQQ on wear particle-induced osteolysis in vivo. Mice treated with PQQ demonstrated marked attenuation of bone erosion based on Micro-CT and histologic analysis of calvaria. These results collectively suggested that PQQ demonstrated inhibitory effects on osteoclast differentiation in vitro and may suppress wear particle-induced osteolysis in vivo, indicating that PQQ may therefore serve as a useful drug in the prevention of bone loss.

  9. 吡咯喹啉醌对脂肪肝蛋鸡肝损伤的保护作用机制%Protective Mechanisms of Dietary Pyrroloquinoline Quinine on Fatty Liver Laying Hens

    Institute of Scientific and Technical Information of China (English)

    赵芹; 张海军; 武书庚; 岳洪源; 王晶; 齐广海; 孙琳琳

    2014-01-01

    This experiment was conducted to investigate the protective mechanisms of dietary pyrroloquinoline quinine ( PQQ) on laying hens with fatty liver syndrome. Two hundred and eighty eight Hy-Line brown laying hens aged 29 weeks were randomly divided into 4 groups with 6 replicates per group and 12 hens per replicate. Hens in group Ⅰ (control group) were fed a basal diet (ME 11. 03 MJ/kg; CP 16. 2%), hens in group Ⅱ( pathological model control group ) were fed a high-energy low-protein diet ( ME 12 . 75 MJ/kg; CP 13 . 0%) , and hens in groups Ⅲ and Ⅳ were fed the high-energy low-protein diet ( the same as group Ⅱ) supplemented with 0. 08 or 0. 16 mg/kg PQQ, respectively. The experiment lasted for 4 weeks. The results showed as follows:1) compared with the control group, high-energy low-protein diet in groupⅡsuccessfully induced experimental fatty liver model;there were large quantity of fat degeneration in livers from pathological model control; the contents of triglyceride and total cholesterol in liver, and the plasma alanine aminotrans-ferase activity in groupⅡwere significantly increased ( P0.05)。由此可见,饲粮PQQ可通过改善蛋鸡肝脏线粒体功能、调节脂质代谢和抗氧化功能预防蛋鸡脂肪肝综合征。

  10. In vitro evaluation of quinidine sensitivity in brazilian Plasmodium falciparum isolates: comparative analysis to quinine and chloroquine Avaliação da sensibilidade in vitro à quinidina em isolados brasileiros de Plasmodium falciparum: análise comparativa à quinina e à cloroquina

    Directory of Open Access Journals (Sweden)

    Carla M. S. MENEZES

    2001-08-01

    Full Text Available Falciparum malaria represents a serious and an increasing world public health problem due to the acquired parasite's resistance to the most available drugs. In some endemic areas, quinidine, a diastereoisomer of the antimalarial quinine, has been employed for replacing the latter. In order to evaluate the use of quinidine as an alternative to the increasing loss of quinine effectiveness in Brazilian P. falciparum strains, as has been observed in the Amazon area, we have assayed quinidine, quinine and chloroquine. The in vitro microtechnique was employed. All isolates showed to be highly resistant to chloroquine. Resistance to quinine was not noted although high MIC (minimal inhibitory concentration values have been observed. These data corroborate the decreasing sensitivity to quinine in strains from Brazil. Quinidine showed IC50 from 0.053 to 4.577 mumol/L of blood while IC50 from 0.053 to 8.132 mumol/L of blood was estimated for quinine. Moreover, clearance of the parasitemia was observed in concentrations lower than that used for quinidine in antiarrhythmic therapy, confirming our previous data. The results were similar to African isolate.Malária falciparum representa grave e crescente problema de saúde pública mundial, dada a resistência do parasito à maioria dos fármacos disponíveis. Em algumas áreas endêmicas, a quinidina, diastereoisômero do antimalárico quinina, vem sendo empregada em substituição a este último. Com o objetivo de avaliar o emprego da quinidina como alternativa à perda crescente de sensibilidade de cepas brasileiras de P. falciparum à quinina, como o observado na região Amazônica, realizamos ensaio comparativo entre quinidina, quinina e cloroquina. A técnica in vitro do microteste de sensibilidade foi utilizada. Todos os isolados mostraram-se altamente resistentes à cloroquina. Resistência à quinina não foi observada, embora altos valores de CMI (concentração mínima inibitória tenham sido

  11. Research on Synthesis of Chiral Quinine Quaternary Ammonium Ligand and Its Catalyzing Activity for Darzens Reaction%手性奎宁季铵盐配体的制备及在Darzens 反应中的催化作用研究

    Institute of Scientific and Technical Information of China (English)

    何健兴; 苏晶; 林汉森; 李建组

    2013-01-01

      文章以奎宁碱为母体,利用一系列卤代烃与奎宁碱发生季铵化反应,生成一系列手性奎宁季铵盐配体,所合成的配体结构均经1H-NMR、IR、MS 确证。并考察了该系列催化剂在不对称相转移催化2-氯代苯乙酮和苯甲醛的 Darzens 缩合反应中的催化性能,发现其手性催化性能跟取代基的立体位阻及电负性大小有关,其中由2-氟-4-溴苄基与奎宁形成的手性季铵盐不对称催化效果最好,所得缩合产物的 ee 值最高为46%。%Through using a series of halogenated hydrocarbons and quinine alkaline quaternization reaction, a series of chiral quinine quaternary ammonium salt ligand were generated with quinine as base matrix and its synthesized ligand structure were confirmed by 1H-NMR, IR, MS. And catalytic performance of ligands in Darzens condensation reaction between 2- chloroacetophenone and benzaldehyde in the asymmetric catalytic condition was investigated, implying that the chiral catalytic properties were associated with the steric size of substituents. And the best enantioselectivity for 46 %was obtained.

  12. The extracellular signal-regulated kinase was promoted by Pyrroloquinoline Quinine in cultured Schwann cells%MEK/ERK信号通路在吡咯喹啉醌促雪旺细胞增殖中的作用

    Institute of Scientific and Technical Information of China (English)

    贺斌; 刘世清; 李皓桓

    2010-01-01

    目的 探讨MEK/ERK信号通路在吡咯喹啉醌促雪旺细胞增殖过程中的作用. 方法 体外培养雪旺细胞,S-100免疫荧光鉴定;Western blot检测MEK下游因子ERK1/2磷酸化激活形式(p-ERK1/2)的表达;MEK抑制剂(PD98059)阻断该通路后检测p-ERK1/2的表达;MTT法检测经PD98059阻断MEK通路后雪旺细胞的增殖情况. 结果 吡咯喹啉醌可激活雪旺细胞内MEK/ERK信号通路,在加入吡咯喹啉醌1 h后p-ERK1/2表达最高;吡咯喹啉醌在1~500 nmol/L范围内可使p-ERK1/2表达增加,1 000 nmol/L时与对照组比较差异无统计学意义,10 000 nmol/L时则表现为抑制作用(P<0.05);经PD98059阻断MEK通路后p-ERK1/2的上调效应消失(P<0.05).而且加入PD98059阻断MEK通路后吡咯喹啉醌对雪旺细胞的促增殖效果减弱. 结论 吡咯喹啉醌可激活雪旺细胞MEK/ERK信号通路,且该通路在吡咯喹啉醌促雪旺细胞增殖过程中发挥作用.%Objective To investigate the effect of mitogen-activated protein kinase(MEK)kinase cascade,extracellular signal-regulated kinase(ERK1/2)signal pathway on Schwann cells proliferation promoted by Pyrroloquinoline Quinine(PQQ)and its molecular mechanisms. Methods Schwann cells were cultured and purified in vitro.The purity was identified by S-100.Different time and concentration of PQQ was added into culture medium.The expression of ERK1/2 and phosphorylated-ERK1/2 was detected by western blot.The expression of p-ERK1/2 after blocking of MEK signal pathway by specific inhibitor PD98059 was detected by western blot. Results Morphological change was observed in PQQ treated Schwann cells.1 ~ 500 nmol/L PQQ could up-regulate the expression of p-ERK1/2,and 1 000 nmol/Lhad no effects,while 10 000 nmol/L exhibited inhibitory effect(P<0.05).p-ERKI/2 increased to peak 1 h after PQQ added,and this up-regulation of p-ERKI/2 was inhibited by PD98059(P<0.05). Conclusions PQQ could affect morphology of Schwann cells and activation of ERKI/2

  13. Comparative Studies on Effects of Dihydroartemisinin and Quinine onPlasmodium Falciparum Gametocytes at Early Stage%双氢青蒿素和奎宁对恶性疟原虫早期配子体作用的随机比较

    Institute of Scientific and Technical Information of China (English)

    陈沛泉; 简华香; 符林春; 李国桥; 范梨盛; 王炳西

    2001-01-01

    【目的】研究双氢青蒿素对恶性疟原虫早期配子体的抑杀作用。【方法】仅骨髓带恶性疟原虫早期配子体而骨髓与外周血液均无成熟配子体的患者11例,随机分为A、B2组。A组6例口服双氢青蒿素片7d总量480mg;B组5例口服硫酸奎宁片7d总量10500mg,定时取骨髓和外周血液涂片,观察两组配子体密度的变化。【结果】A组骨髓早期配子体药后10d全部转阴;而B组全部阳性,至药后14d仍有2/5例阳性。外周血液配子体转阴时间,A组为(4.8±0.9)d;B组为(22.0±5.8)d。【结论】双氢青蒿素能杀灭恶性疟原虫早期配子体,而硫酸奎宁似无此作用。%【Objective】To study the effects of dihydroartemisinin and quinineo n plasmodium falciparum gametocytes at early stage.【Methods】Eleven patients wi th falciparum malaria who had plasmodium falciparum gametocytes at early stage(P FGe) in bone marrow but no matured plasmodium falciparum gametocytes(PFGm) in bo ne marrow and peripheral blood were allocated to two groups.Group A(n=6) were ad ministered orally with dihydroartemisinin at a total dosage of 480mg for 7 days and Group B(n=5) with quinine sulfate at a total dosage of 10500 mg for 7 days .T he number of gametocytes in bone marrow and peripheral blood was examined at reg ular time.【Results】 PFGe in bone marrow disappeared in Group A on 10th day a fter the first administration while existed in all the cases of Group B on 10 th day and still in 2 cases on 14th day.The clearance time for periphe ral PFGe was 4.8±0.9 days in Group A and 22.0±5.8 days in Group B.【Conclusion】Dihydroartemisinin can clear PFGe but quinine sho ws no this action.

  14. 活性/可控自由基聚合制备奎宁分子印迹微球及识别性能研究%Study on the preparation for quinine imprinted polymeric microsphere by living/controlled radical polymerization and its recognition properties

    Institute of Scientific and Technical Information of China (English)

    何建峰; 杨万里; 黄少梅

    2014-01-01

    以奎宁分子为模板,甲基丙烯酸( MAA)为功能单体,乙二醇二甲基丙烯酸酯( EDMA)为交联剂,二硫代四乙基秋兰姆( TED)为活性/可控引发剂,将可逆加成-断裂链转移自由基聚合与沉淀聚合相结合,制备微米级的球形奎宁分子印迹聚合物。并用扫描电镜和激光粒度扫描对聚合物粒子进行表征,结果显示,活性/可控聚合制备的分子印迹聚合物呈均匀的球形,其平均粒径最大可达2.3μm。对不同底物的结合实验表明,与传统沉淀聚合物相比,该分子印迹聚合物表现出更高的络合容量和分子选择性。%The spherical molecularly imprinted polymers with micron-size were prepared by using quinine as template,methylacrylic acid( MAA) as functional monomer,ethylene glycol dimethacrylate( EDMA) as cross-linker and dithiotetraethylthiuram( TED) as the living/controlled initiator by combining reversible addition-fragmentation chain transfer radical polymerization with precipitation pol-ymerization. The polymeric particles were characterized by scanning electron microscopy and laser particle size analysis. The results show that the polymeric particles prepared by living/controlled polymerization present uniform spherical shape and its maximum av-erage diameter reach 2. 3 μm. The binding experiment towards different substrates indicates that the living/controlled molecularly imprinted polymer shows higher binding capacity and molecular selectivity than the traditional precipitation polymers.

  15. Electrocatalytic oxidation and its electrochemical determination of quinine sulfate at SDBS - [bupy] PF_6 modified carbon paste electrode%硫酸奎宁在SDBS-[bupy]PF_6修饰碳糊电极上的电催化氧化及电分析方法

    Institute of Scientific and Technical Information of China (English)

    刘立红; 高作宁

    2010-01-01

    目的:研究了硫酸奎宁(quinine sulfate,QS)在十二烷基苯磺酸钠(sodium dodecyl benzenesulfonate,SDBS)自组装膜与离子液体N-丁基吡啶六氟磷酸盐([bupy]PF_6)复合修饰碳糊电极(SDBS-[bupy]PF_6/CPE)上的电化学行为和电化学动力学性质,建立了QS电化学定量测定方法.方法:循环伏安法(CV),计时电流法(CA),计时库仑法(CC),方波伏安法(SWV)以及电化学交流阻抗法(EIS).结果:在SDBS-[bupy]PF_6/CPE上,QS发生了受扩散控制的不可逆电化学氧化过程.测得QS在SDBS-[bupy]PF_6/CPE上的电极反应过程动力学参数.用SWV法测得QS氧化峰电流与其浓度在5.0 ×10~(-6)~1.0×10~(-4)mol·L~(-1)和1.0×10~(-4)~1.0×10~(-3)mol·L~(-1)呈线性关系,检测限为3.5×10~(-7)mol·L~(-1).采用本方法对市售二盐酸奎宁注射液进行了电化学定量测定,RSD在1.3%~3.4%之间,加标回收率在98.0%~103%之间.结论:SDBS-[bupy]PF_6/CPE对QS电化学氧化具有良好的催化作用,该方法可用于市售奎宁类药物含量的电化学定量测定,方法操作简单,测定结果令人满意.

  16. 吡咯喹啉醌对神经细胞氧糖剥夺损伤的保护作用及其机制%Protective Effect of Pyrroloquinoline Quinine on Oxygen and Glucose Deprivation Injury in Nuro2A Cells

    Institute of Scientific and Technical Information of China (English)

    郭青; 吕国枫

    2011-01-01

    Objective To investigate the neuroprotective effects of pyrroloquinoline quinine (PQQ) on oxygen and glucose deprivation (OGD) in cultured rat neuroblastoma cells Neuro2A and the possible mechanisms involved. Methods Cultured rat neuroblasroma cells Neuro2A were pretreated or not pretreated with increasingly concentrations of PQQ, were exposed to 2 h combined OGD in an anaerobic chamber followed by reoxygenation of 6 h. The results on cellular morphology, cell viability,apoptotic cells, reactive oxygen species (ROS), and glutathione (GSH) were compared between OGD and PQQ group. Results Pretreatment of PQQ (0. 4,0. 8, 1.6, 3.2, 6.4, 12. 8 μmol/L) increased the cell viability (P<0. 05) and GSH level, decreased the contents of ROS and the percentage of apoptotic cells in cortical neurons exposure to OGD (P<0. 01). Conclusion PQQ exhibits remarkable protection against hypoxia/reoxygenation injury in Neuro2A cells, which may be associated to the inhibiting the oxidative stress and subsequent apoptosis.%目的 研究吡咯喹啉醌(PQQ)的神经保护作用及其可能机制.方法 利用不同浓度PQQ预处理Neuro2A细胞后建立氧糖剥夺模型.复氧后6 h,观察Neuro2A细胞的细胞形态、存活率、凋亡率以及活性氧(ROS)和还原型谷胱甘肽(GSH)的浓度.结果 Neuro2A细胞形态出现严重损伤;经0.4、0.8、1.6、3.2、6.4、12.8、25.6 μmol/L的PQQ预处理,细胞损伤减轻;细胞存活率随PQQ浓度升高呈逐渐增高趋势;经6.4 μmol/L和12.8 μmol/L的PQQ预处理,细胞凋亡减少,细胞内ROS生成减少,GSH水平增高(P<0.05).结论 PQQ对氧糖剥夺神经细胞损伤有一定的保护作用,这一作用可能是通过减轻氧化应激反应,降低细胞凋亡率实现的.

  17. The roles of PI3K/Akt pathway in proliferation of Schwann cells promoted by Pyrroloquinoline Quinine%PI3K/Akt信号通路在吡咯喹啉醌促雪旺细胞增殖中的作用

    Institute of Scientific and Technical Information of China (English)

    贺斌; 刘世清; 李皓桓

    2010-01-01

    目的 探讨磷脂酰肌醇-3激酶/蛋白激酶B(phosphoinositide-3 kinase/Akt,PI3K/Akt)信号通路在吡咯喹啉醌促雪旺细胞增殖过程中的作用.方法 体外分离培养雪旺细胞,S-100免疫荧光鉴定;Western blot检测PI3K下游因子Akt磷酸化激活形式(p-Akt)的表达,并通过PI3K激酶抑制剂(wortmannin)阻断该通路后p-Akt的表达情况.结果 毗咯喹啉醌可使雪旺细胞发生形态学变化,加入吡咯喹啉醌后30 min即可检测到p-Akt的表达,4 h达高峰,12 h基本无表达;吡咯喹啉醌在1~100 nmol/L范围内可使p-Akt表达增加;加入wortmannin阻断PI3K后p-Akt上调表达消失(P<0.05).结论 吡咯喹啉醌可使雪旺细胞发生形态学变化,PI3K/Akt信号通路在吡咯喹啉醌促雪旺细胞增殖过程中发挥重要作用.%Objective To investigate the roles of PI3K/Akt signal pathway in Schwann cells proliferation promoted by pyrroloquinoline quinine (PQQ). Methods Schwann cells were cultured and purified in vitro. The purity was identified by immunofluorescence of S-100; the expression of Akt and phosphorylated-Akt(p-Akt) were detected by western blot, and the expression of p-Akt after blocking the PI3K signal transduction pathway by PI3K inhibitor wortmannin was detected by western blot. Results Morphological change was observed in PQQ-treated Schwann cells, p-Akt was detected 30min after PQQ treated, reached the peak at 4h, and disappeared 12 h later. 1-100 nmol/L PQQ could up-regulate the expression of p-Akt; this up-regulated expression of p-Akt was inhibited by wortmannin (P < 0.05).Conclusions PQQ could affect morphology of Schwann cells and activation of Akt. It indicates that PI3K/Akt signal pathway might be involved in Schwann cells proliferation promoted by PQQ.

  18. 奎宁-冠醚组合型手性固定相直接拆分氨基酸的机理%Separation mechanism of chiral stationary phase based on quinine and crown ether for the direct stereoselective separation of amino acids

    Institute of Scientific and Technical Information of China (English)

    吴海霞; 王东强; 赵见超; 柯燕雄; 梁鑫淼

    2016-01-01

    合成了一种新型奎宁-冠醚组合型手性固定相( QN-CR CSP)并用于氨基酸手性对映体的直接拆分,该固定相对12种氨基酸对映体有良好的手性拆分能力。基于氨基酸手性识别中离子交换和络合的协同作用,建立了一种新型的等温吸附模型。通过迎头特殊点洗脱法( FACP)测定色氨酸( Trp)在不同金属离子添加剂条件下的等温吸附线,验证了模型的合理性。流动相中的 Li+、Na+、K+等金属离子与氨基酸竞争固定相中的冠醚络合位点,随着金属离子与冠醚的络合作用力和络合吸附平衡常数增大,固定相对 Trp的手性拆分能力下降。该模型的建立对理解氨基酸在此类固定相中的手性保留行为以及固定相结构的进一步优化具有重要意义。%A novel chiral stationary phase combining quinine and crown ether( QN-CR CSP ) was developed to separate amino acid enantiomers. This CSP showed good enantioselectivity for some amino acids. Since the synergistic effect of ion exchange and complexation in chiral recognition of amino acids,a new adsorption isotherm was built. Using the method of frontal analysis by characteristic point( FACP),the adsorption isotherms of tryptophan( Trp)under different mobile phase conditions were determined and fitted the proposed adsorption isotherm model well. With the increase of the competition between metal cationic and amino to crown ether,the equilibrium constant of complexing adsorption was found increased. The chiral sepa-ration ability was decreased. The adsorption isotherm improved the understanding of the reten-tion behavior of amino acids on QN-CR CSP,which was also benefit to optimize the structure of the stationary phase.

  19. 吡咯喹啉醌对氧化应激诱导雪旺细胞凋亡的保护作用及其机制%Effects of Pyrroloquinoline quinine on oxidative stress-induced apoptosis of Schwann cells and its mechanism

    Institute of Scientific and Technical Information of China (English)

    贺斌; 陶海鹰; 卫爱林; 刘世清; 李皓桓

    2014-01-01

    目的 探讨吡咯喹啉醌(Pyrroloquinoline quinine,PQQ)对H2O2诱导雪旺细胞(Schwann cells,SCs)凋亡的保护作用及其作用机制.方法 体外原代培养、纯化及S-100免疫荧光染色鉴定SCs,将培养SCs分为空白对照组、H2O2处理组(100 μmol/L H2O2诱导组)、H2O2加PQQ处理组(10、50和100 nmoL/L PQQ处理组).检测各组细胞内超氧化物歧化酶(SOD)及丙二醛(MDA)的含量,流式细胞仪计数检测SCs早期凋亡率,Hoeehst33342染色观察凋亡SCs核碎裂及核固缩情况,亲脂性阳离子荧光染料罗丹明染色(Rhodamine 123,Rho123)观察凋亡SCs线粒体膜电位变化情况,Western blot法检测Bcl-2的表达水平.结果 经H2O2诱导,SCs组与空白对照组比较SOD含量明显减少,MDA含量明显增加(P<0.05);加入PQQ后SOD含量增加,MDA含量减少(P<0.05).流式细胞仪检测结果表明,经H2O2诱导SCs早期凋亡率为58.8%,与空白对照组(2.1%)比较差异有统计学意义(P<0.05),加入10、50、100 nmol/L PQQ后凋亡率分别降低为33.7%、18.7%、3.9%,差异有统计学意义(P<0.05).Hoeehst33342染色结果表明,H2O2诱导SCs具有典型的凋亡形态特征,表现为核染色质浓聚、细胞核体积缩小、核碎裂现象明显,经PQQ作用后凋亡形态细胞比例减少.Rho123染色结果表明,经H2O2诱导后SCs线粒体膜电位明显降低,而经PQQ作用后部分逆转.Western blot结果表明,经H2O2诱导SCs后Bcl-2表达下调,加入PQQ后Bcl-2表达有所增加,差异有统计学意义(P<0.05).结论 PQQ对氧化损伤SCs凋亡具有保护作用.%Objective To investigate the effects of Pyrroloquinoline quinine (PQQ) on hydrogen peroxide-induced apoptosis of Schwann cells (SCs) and its mechanism.Methods SCs were isolated and cultured in vitro,and identified by S-100 immunofluorescence staining.The cultured SCs were divided into control group、hydrogen peroxide-treated group、hydrogen peroxide and PQQ treated groups.The intracellular

  20. 离子对色谱法研究吡咯并喹呤醌与D-丝氨酸反应的化学动力学%Study of chemical kinetics between pyrroloquinoline quinine and D-serine in body by ion-pair liquid chromatography

    Institute of Scientific and Technical Information of China (English)

    周杏琴; 钦晓峰; 张建康; 曹国宪

    2012-01-01

    As a new neurotransmitter present in the glial cells, D-serine ( Dser) plays an important role in central nervous system diseases. Pyrroloquinoline quinine (PQQ) can promote the production of the nerve growth factor and has a protective effect on nerve injuries. The chemical kinetics of PQQ and Dser was studied by determining the free contents of PQQ using ion-pair liquid chromatography (LC) , so it can provide important information for the mechanisms of PQQ in the regulation of neurotransmitter. The PQQ and the production of the incubation were separated on an Amethyst C18-P column using tetrabutylammonium bromide as ion-pair reagent. The average recoveries were between 94. 2% and 99. 3%, and the relative standard deviations were between 1. 05% and 2. 03%. The average rate constants (K) of PQQ with Dser were 0. 032, 0. 07 and 0. 17 h-1 at 25, 37 and 50 ℃ , respectively. The average activation energy (Ea) was 54. 7 Kj/mol. The values of half life (t1/2) were 22. 0, 9. 8 and 3. 99 h at 25, 37 and 50 ℃, respectively. The results showed that PQQ can regulate the balance of Dser in the brain. The method is simple and reliable.%D-丝氨酸(DSer)作为一种新的神经递质存在于胶质细胞,在中枢神经系统疾病中发挥重要的作用;吡咯并喹呤醌(PQQ)能够促进神经因子的产生和神经保护作用.采用离子对色谱法测定吡咯并喹呤醌(PQQ)与DSer反应中游离PQQ的浓度,通过化学反应动力学研究PQQ与DSer的作用,为PQQ在神经递质的调节作用机制提供重要的信息.采用四丁基溴化铵为离子对试剂,PQQ与DSer孵育反应后各物质在Amethyst C18-P柱上的分离度较好,平均回收率为94.2%~99.3%,相对标准偏差为1.05%~2.03%.PQQ-DSer反应的平均速率常数分别为0.032 h -( 25℃)、0.07 h-1 (37℃)、0.17 h-1(50℃);平均反应活化能为54.7 kJ/mol;半衰期分别为22.0 h(25℃)、9.8 h(37℃)和3.99 h(50℃).动力学结果显示PQQ对脑内DSer的平衡具有

  1. 吡咯喹啉醌二钠对饲喂氧化鸭油肉仔鸡生长性能、血浆脂质代谢及抗氧化能力的影响%Effects of Pyrroloquinoline Quinine Disodium on Growth Performance, Plasma Lipid Metabolism and Antioxidant Ability in Broilers Fed Oxidized Duck Oil

    Institute of Scientific and Technical Information of China (English)

    张亚男; 齐博; 武书庚; 岳洪源; 王晶; 张海军; 齐广海

    2015-01-01

    本试验旨在研究吡咯喹啉醌二钠(PQQ·Na2)对饲喂氧化鸭油(ODO)肉仔鸡生长性能、血浆脂质代谢和抗氧化能力的影响. 选取270只健康、体重相近的1日龄爱拔益加肉仔鸡公雏,随机分成 3 个组,每个组 6 个重复,每个重复 15 只. 3 个组分别饲喂含有新鲜鸭油(FDO)、ODO和ODO+0.4 mg/kg PQQ·Na2(ODO+PQQ)的饲粮,油脂添加水平1~21 d 为3.0%,22~42 d为3.5%. 结果表明:1)与FDO组相比,ODO显著降低了肉仔鸡21 d的平均体重(P0.05). 与ODO组相比,ODO+PQQ组1~21 d和22~42 d 的平均日增重、42 d 平均体重具有增加的趋势( P<0. 10 ). 2 )与 FDO 组相比, PQQ·Na2显著提高了肉仔鸡42 d的全净膛率和21 d的胸肌率( P<0.05). 3)与FDO和ODO组相比,PQQ·Na2 显著降低了肉仔鸡42 d血浆总胆红素和21 d血浆葡萄糖含量( P<0.05).4) PQQ·Na2 显著抑制了ODO导致的21 d血浆总超氧化物歧化酶活性和21和42 d总抗氧化能力的降低( P<0.05) ,抑制ODO导致的21 d血浆丙二醛含量升高( P<0.05). 5) PQQ·Na2 显著抑制了ODO引起的21和42 d血浆甘油三酯含量的升高和21 d血浆高密度脂蛋白胆固醇含量的降低( P<0.05). 可见,PQQ·Na2 可通过调节血浆脂质代谢和提高机体的抗氧化能力,缓解ODO对肉仔鸡的不利影响.%The current study was conducted to investigate the effects of pyrroloquinoline quinine disodium ( PQQ·Na2 ) on growth performance, plasma lipid metabolism and antioxidant ability in broilers fed oxidized duck oil. A total of 270 one-day-old Arbor Acres broilers were randomly assigned to 3 groups ( with 6 repli-cates per group and 15 broilers per replicate) fed diets supplemented with fresh duck oil ( FDO group) , oxi-dized duck oil ( ODO group) and oxidized duck oil + 0.4 mg/kg PQQ·Na2( ODO+PQQ group) , respective-ly. The supplemental level of oil was 3.0% during 1 to 21 days and 3.5% during 22 to 42 days, respectively. The results showed as follows: 1) compared with FDO group

  2. Effects of Qyrroloquinoline Quinine on Performance, Egg Quality, Plasma Lipid Metabolism and Antioxidant Ability of Laying Hens Fed High-Energy Low-Protein Diets%吡咯喹啉醌对高能低蛋白质饲粮蛋鸡生产性能、蛋品质、血浆脂质代谢及抗氧化能力的影响

    Institute of Scientific and Technical Information of China (English)

    赵芹; 张海军; 武书庚; 岳洪源; 王晶; 齐广海; 孙琳琳

    2014-01-01

    This experiment was conducted to investigate the effects of pyrroloquinoline quinine ( PQQ) on per-formance, egg quality, plasma lipid metabolism and antioxidant ability of laying hens fed high-energy low-pro-tein diets. Two hundred and eighty-eight Hy-Line brown laying hens aged 29 weeks were randomly divided in-to 4 groups with 6 replicates per group and 12 hens per replicate. Hens in group Ⅰ ( control group) were fed a basal diet ( metabolic energy 11 . 03 MJ/kg; crude protein 16 . 2%) , hens in group II ( pathological model control group) were fed a high-energy low-protein diet ( metabolic energy 12. 75 MJ/kg; crude protein 13 . 0%) , and hens in groups Ⅲ and Ⅳ were fed the high-energy low-protein diet ( the same as group II) supplemented with 0. 08 and 0. 16 mg/kg PQQ, respectively. The experiment lasted for 4 weeks. The results showed as follows:1) compared with the control group, the high-energy low-protein diet induced fatty liver, the liver fat rate in group II was significantly increased (P<0. 05), and the contents of triglyceride (TG), total cholesterol ( TC) and low-density lipoprotein cholesterol ( LDL-C) in plasma in group II were signifi-cantly increased ( P<0 . 05 ) . 2 ) Dietary PQQ could significantly decrease the increase of average daily feed intake and the ratio of feed to egg of laying hens fed high-energy low-protein diets ( P<0 . 05 ) , it could signif-icantly inhibit the decrease of albumen height, Haugh unit and yolk color and the increase of the contents of TG, TC and LDL-C and lactate dehydrogenase (LDH) activity in plasma (P<0. 05), and all the above inde-xes could get the same levels as control group. 3) Dietary PQQ could significantly inhibit the decrease of plas-ma superoxide dismutase activity and the increase of plasma malondialdehyde content of laying hens fed high-energy low-protein diets (P<0. 05). In conclusion, dietary PQQ can decrease the liver fat content, improve the lipid metabolism and antioxidant ability of laying

  3. Dissociating pleasantness and intensity with quinine sulfate/sucrose mixtures in taste

    NARCIS (Netherlands)

    Veldhuizen, M.G.; Rooden, van A.P.A.; Kroeze, J.H.A.

    2006-01-01

    Independent experimental manipulation of subjective intensity and hedonic tone is required if one wants to study their separate effects on brain activity and behavior. This is problematic because hedonic tone and subjective intensity are related, leading to a pleasantness change each time the stimul

  4. Bananas and Balsa, Quetzals and Quinine: A Rainforest Unit for Science and Language Arts.

    Science.gov (United States)

    Pottle, Jean L.

    The destruction of rain forests and the impact this has on the earth is an important environmental issue. This book was written to help students learn why it is important to protect those areas of the world. In this activity book, students are introduced to a number of inhabitants of the rain forest. They learn about the diversity of plants and…

  5. Atovaquone and quinine anti-malarials inhibit ATP binding cassette transporter activity

    NARCIS (Netherlands)

    Rijpma, S.R.; Heuvel, J.J.; Velden, M. van der; Sauerwein, R.W.; Russel, F.G.; Koenderink, J.B.

    2014-01-01

    BACKGROUND: Therapeutic blood plasma concentrations of anti-malarial drugs are essential for successful treatment. Pharmacokinetics of pharmaceutical compounds are dependent of adsorption, distribution, metabolism, and excretion. ATP binding cassette (ABC) transport proteins are particularly involve

  6. [CAFFEINE AND QUININE IN SOFT DRINKS; CONTRIBUTION TO THE DIETARY INTAKE].

    Science.gov (United States)

    González Reyes, Ana Belén; Hardisson de la Torre, Arturo; Gutiérrez Fernández, Angel José; Rubio Armendáriz, Carmen; Frías Tejera, Inmaculada; Revert Gironés, Consuelo

    2015-12-01

    Introducción: las bebidas refrescantes son cada vez más consumidas por la sociedad. Están compuestas por una gran variedad de sustancias, de las cuales algunas, si se consumen en dosis altas y con elevada frecuencia, pueden provocar efectos negativos. Objetivos: determinar la concentración de cafeína y quinina para comprobar si sus niveles se encuentran por debajo de los máximos permitidos por la reglamentación técnico-sanitaria vigente y calcular la contribución a la ingesta dietética obteniendo la Ingesta Diaria Estimada. Método: se analizaron las concentraciones de cafeína y quinina en las principales marcas comerciales de refrescos, usando para ello la técnica de cromatografía líquida de alta resolución. Resultados: se obtuvieron concentraciones para todas las marcas analizadas, que permitieron estimar la media en cada una. Conclusiones: se ha observado que en ningún caso se superan las concentraciones máximas y que la contribución a la ingesta no genera aparición alguna de reacción adversa.

  7. Spectrophotometric Determination of Quinine by Charge-Transfer Reaction Between Quinine and Chloranilic Acid with Micelle-Sensitized%奎宁与氯冉酸的胶束增敏荷移反应及其测定

    Institute of Scientific and Technical Information of China (English)

    王孝镕; 李桂华; 唐清华; 潘琳琳; 范淑云

    2004-01-01

    提出了一种基于胶束增敏荷移反应测定奎宁的光度分析法.研究了在阳离子表面活性剂氯化十六烷基吡啶(CPC)胶束体系中电子给体奎宁与电子受体氯冉酸之间的荷移反应产物的光谱性质.发现CPC对奎宁与氯冉酸的荷移反应络合物的光吸收有显著的增强作用,使络合物的表观摩尔吸光系数提高了2.5倍(λmax=520 nm,ε=3.64×103 L·mol-1·cm-1).奎宁浓度在20~800 mg/L范围内符合比耳定律,r =0.9991.本方法用于片剂中奎宁含量的测定,其回收率为97.3% ~99.2%;5次测定的相对标准偏差为1.6% ~2.5%.

  8. Improvement of Determination Method of Quinine Hydrochloride and Caffeine in Compound Quinine Injection%复方奎宁注射液中盐酸奎宁和咖啡因含量测定方法的改进

    Institute of Scientific and Technical Information of China (English)

    陈英; 李桂峰

    2007-01-01

    目的:改进复方奎宁注射液中盐酸奎宁和咖啡因含量测定方法.方法:采用高效液相色谱法,在C18柱上,以水-乙腈一三乙胺(790:205:5)(用冰醋酸调PH值3.5)为流动相,检测波长为275nm,同时测定复方奎宁注射液中盐酸奎宁争咖啡因的含量.结果:盐酸奎宁在0.546~5.460μg范围内,其峰面积与进样量线性关系良好(r=0.9998),平均回收率为100.7%,RSD=0.7%;咖啡因在0.132~1.328μg范围内,其峰面积与进样量线性关系良好(r=0.9999),平均回收率为100.3%.RSD=0.8%.结论:建立的方法可同时测定复方奎宁注射液中两种成分的含量,较其原有药品标准方法有较大的改进.

  9. Rifampicin-dependent antibodies bind a similar or identical epitope to glycoprotein IX-specific quinine-dependent antibodies

    NARCIS (Netherlands)

    Burgess, J K; Lopez, J A; Gaudry, L E; Chong, B H

    2000-01-01

    The drug-dependent antibody of a patient with rifampicin-induced thrombocytopenia was characterized using the antigen-capture enzyme-linked immunosorbent assay (MAIPA assay), flow cytometry, and immunoprecipitation. The antibody was found to bind glycoprotein (GP) Ib-IX but not GPIIb-IIIa because (1

  10. Nature's Chiral Catalyst and Anti-Malarial Agent: Isolation and Structure Elucidation of Cinchonine and Quinine from "Cinchona calisaya"

    Science.gov (United States)

    Carroll, Anne-Marie; Kavanagh, David J.; McGovern, Fiona P.; Reilly, Joe W.; Walsh, John J.

    2012-01-01

    Nature is a well-recognized source of compounds of interest, but access is often an issue. One pertinent example is the cinchona alkaloids from the bark of "Cinchona calisaya." In this experiment, students at the third-year undergraduate level undertake the selective isolation and characterization of two of the four main alkaloids present in the…

  11. Novel carbamoyl type quinine and quinidine based chiral anion exchangers implementing alkyne-azide cycloaddition immobilization chemistry.

    Science.gov (United States)

    Hettegger, Hubert; Kohout, Michal; Mimini, Vebi; Lindner, Wolfgang

    2014-04-11

    The synthesis and chromatographic evaluation of a series of new Cinchona derived chiral weak anion exchangers is presented. Huisgen Cu(I) mediated alkyne-azide cycloaddition, so-called click chemistry, was used as an immobilization strategy. In this way it was possible to immobilize about 90% of offered selector via 1,2,3-triazole linker, which displays a more efficient way of binding the selector to modified silica compared to common radical mediated thiol-ene addition. Problems associated with potential radical scavenging properties of chiral selectors thereby could be circumvented. The evaluation of the synthesized chiral stationary phases regarding chromatographic behavior was carried out using polar organic mode mobile phase composition and a set of representative chiral organic acids. Different loading densities revealed an optimum selector density of about 310μmol/g chiral stationary phase with respect to resolution and selectivity. A decrease of performance was observed for higher loading, indicating mutual spatial influence of selector units leading to sterical hindrance. In addition, we observed that the effect of free azide groups on retention is negligible and the overall chromatographic behavior is comparable to other Cinchona derived chiral stationary phases.

  12. The stereoisomers quinine and quinidine exhibit a marked stereoselectivity in the inhibition of hepatobiliary transport of cardiac glycosides

    NARCIS (Netherlands)

    Hedman, A; Meijer, DKF

    1998-01-01

    Background / Aims: Certain basic (cationic) drugs are known to interact with the hepatic transport, and renal and/or biliary clearance of cardia glycosides. The mechanisms behind these interactions are not fully understood, In the present study our was to investigate the effects of the two diastereo

  13. 21 CFR 310.544 - Drug products containing active ingredients offered over-the-counter (OTC) for use as a smoking...

    Science.gov (United States)

    2010-04-01

    ..., povidone-silver nitrate, quinine ascorbate, silver acetate, silver nitrate, and thymol have been present as... (terpeneless), licorice root extract, menthol, methyl salicylate, quinine ascorbate, silver nitrate,...

  14. Quinine-Based Zwitterionic Chiral Stationary Phase as a Complementary Tool for Peptide Analysis: Mobile Phase Effects on Enantio- and Stereoselectivity of Underivatized Oligopeptides.

    Science.gov (United States)

    Ianni, Federica; Sardella, Roccaldo; Carotti, Andrea; Natalini, Benedetto; Lindner, Wolfgang; Lämmerhofer, Michael

    2016-01-01

    Peptide stereoisomer analysis is of importance for quality control of therapeutic peptides, the analysis of stereochemical integrity of bioactive peptides in food, and the elucidation of the stereochemistry of peptides from a natural chiral pool which often contains one or more D-amino acid residues. In this work, a series of model peptide stereoisomers (enantiomers and diastereomers) were analyzed on a zwitterionic ion-exchanger chiral stationary phase (Chiralpak ZWIX(+) 5 µm), in order to investigate the retention and separation performance for such compounds on this chiral stationary phase and elucidate its utility for this purpose. The goal of the study focused on 1) investigations of the effects of the sample matrix used to dissolve the peptide samples; 2) optimization of the mobile phase (enabling deriving information on factors of relevance for retention and separation); and 3) derivation of structure-selectivity relationships. It turned out that small di- and tripeptides can be well resolved under optimized conditions, typically with resolutions larger than 1.5. The optimized mobile phase often consisted of methanol-tetrahydrofuran-water (49:49:2; v/v/v) with 25 mM formic acid and 12.5 mM diethylamine. This work proposes some guidance on which mobile phases can be most efficiently used for peptide stereoisomer separations on Chiralpak ZWIX. Chirality 28:5-16, 2016. © 2015 Wiley Periodicals, Inc.

  15. HPLC determination of caffeine in compound quinine injection%HPLC法测定复方奎宁注射液中咖啡因的含量

    Institute of Scientific and Technical Information of China (English)

    李晓梅; 赵琪钟; 马骁

    2006-01-01

    目的:建立HPLC法测定复方奎宁注射液中咖啡因含量.方法:色谱柱为PE Validated C18(100 mm ×4.6 mm,5μm),流动相为甲醇-1%醋酸溶液(用二乙胺调节pH至3.7)(35:65),流速为1.0 mL·min-1,检测波长为272 nm,采用外标法计算含量.结果:本法简便可靠、灵敏、准确,咖啡因在5.56~55.6μg·mL-1范围内呈良好的线性关系(r=0.9998),精密度(RSD=0.26%,n=5)和重复性(RSD=0.27%,n=5)良好.结论:建立的定量方法专属性强,可用于复方奎宁注射液中咖啡因的含量测定.

  16. Determination of Quinine in Cosmetics by RP-HPLC%RP-HPLC法检测化妆品中奎宁的含量

    Institute of Scientific and Technical Information of China (English)

    陈志蓉; 刘洋; 张鹏祥; 赵华

    2011-01-01

    目的 对化妆品中奎宁的含量进行定量检测.方法采用RP-HPLC法,色谱柱为Waters sunfire-C18柱,样品经甲醇超声,以甲醇-0.01mol·L-1(NH4)2HPO (90 ∶ 10,体积比)为流动相,流速为1.0mL·min-1,检测波长为328nm,柱温为30℃,进样量为20μL.结果在此条件下,奎宁在1.0~200μg·mL-1范围内线性良好,r=0.9999,回收率在98.6%~100.4%,RSD=0.29%.结论该方法简单易行,能够快速对化妆品中奎宁含量进行定量,杂质干扰小,回收率高,重复性好.

  17. Preparation and Application of All-Solid State Quinine Selective Electrode%全固态奎宁选择电极的研制与应用

    Institute of Scientific and Technical Information of China (English)

    岳京立; 于秋泓; 汪敏; 李东辉; 毕丽华

    2000-01-01

    首次报道了以奎宁碘化物与碘化铋形成的分子缔合物为电活性物的全固态盐酸奎宁选择电极,电极的线性响应范围为1.0×10-1~1.0×10-5 mol/L,级差为40 mV/pC,检测限为2.5×10-6 mol/L.pH值在3.08~6.10范围内变化时,引起的电势变化不超过±1 mV.该电极制作简便、操作灵活、重现性好,结果与药典法相符.

  18. Drug: D08461 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D08461 Drug Quinine dihydrochloride; Quinine (TN) C20H24N2O2. 2HCl 396.1371 397.3386 D08461.gif Antiprotozoa... USP drug classification [BR:br08302] Antiparasitics Antiprotozoals Quinine D08461 Quinine dihydrochloride A

  19. Drug: D08460 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available gif Cinchona [TAX:43462], Cinchona calisaya [TAX:153742], Cinchona succirubra, Cinchona calisaya Antiprotozoa...[BR:br08302] Antiparasitics Antiprotozoals Quinine D08460 Quinine (BAN) Antiinfectives [BR:br08307] Antipara

  20. Myotonia

    Science.gov (United States)

    ... myotonia may include mexiletine, quinine, phenytoin, and other anticonvulsant drugs. Physical therapy and other rehabilitative measures may ... myotonia may include mexiletine, quinine, phenytoin, and other anticonvulsant drugs. Physical therapy and other rehabilitative measures may ...

  1. Myotonia Congenita

    Science.gov (United States)

    ... some success with medications such as quinine, or anticonvulsant drugs such as phenytoin. Physical therapy and other ... some success with medications such as quinine, or anticonvulsant drugs such as phenytoin. Physical therapy and other ...

  2. 邻氯苯基卟啉-奎宁季铵盐化合物的合成及表征%The synthesis and characterization of o-chlorophenyl porphyrin-quinine quaternary ammonium salt

    Institute of Scientific and Technical Information of China (English)

    吴银素; 刘彦钦; 韩士田

    2001-01-01

    为了寻找具有手性诱导、相转移和催化为一体的三功能卟啉催化剂,探讨氯取代基的空间位置对氯苯基卟啉-奎宁季铵盐催化性能、手性不对称诱导效应的影响,合成了邻氯苯基卟啉-奎宁季铵盐化合物,其结构用UV、IR、1HNMR、MS和元素分析得到确证,并研究了其荧光光谱性质.

  3. 青蒿琥酯与奎宁MAX治疗恶性疟疾的最小成本分析%Artesunate versus Quinine MAX for Malaria: Cost - minimization Analysis

    Institute of Scientific and Technical Information of China (English)

    孙卫华

    2008-01-01

    目的:评价青蒿琥酯(ART)与奎宁MAX(QUI)治疗恶性疟疾的经济学效果.方法:将64例恶性疟疾患者随机分为ART组与QUI组,分别应用ART和QUI依法治疗7 d,考察2种用药方案的疗效并进行最小成本分析.结果:ART组、QUI组总有效率分别为90.6%、87.5%(P>0.05),平均成本分别为341、485元,差异有统计学意义(P<0.01).结论:ART组治疗方案较佳,适宜于非洲等恶性疟疾高发区域推广使用.

  4. 全固态离子选择电极测定药物中盐酸奎宁的浓度%Using All Solid State Selective Electrode to Determine the Concentration in Quinine Hychrochloride

    Institute of Scientific and Technical Information of China (English)

    岳京立; 于秋泓; 刘中英; 李东辉; 陈尧

    2001-01-01

    使用鞣酸与六价铬形成的络合物为沉淀剂,使其与奎宁形成的分子缔和物为电活性物,制备了一种新型的全固态盐酸硅宁选择电极。电极的线性响应范围为1.0×10-1~1.0×10-5mol/L,级差为44mV/pC,检测限为8.0×10-6mol/L,pH在2.94~5.58范围内,电势随pH变化不超过±1mV。该电极制作简便,操作灵活,重现性好,结果与药典法比较无系统误差。

  5. N-乙基溴化奎宁催化合成α-甲基-α-氨基酸%Synthesis of α-Methyl-α-Amino Acids with N-Ethyl Brominized Quinine as Phase Transfer Catalyst

    Institute of Scientific and Technical Information of China (English)

    黄国华; 李洋

    2011-01-01

    文章采用N-乙基溴化奎宁为相转移催化剂,以2-丁酮等为原料合成了几种α-甲基-α-氨基酸,并考察了2-丁酮和2-戊酮等不同反应原料、不同反应温度和不同反应时长下合成反应的收率,得出了较佳的反应条件.

  6. 铈(Ⅳ)-抗坏血酸-奎宁化学发光体系的研究和应用%Determination of quinine by Ce(Ⅳ)-ascorbic acid chemiluminescence system

    Institute of Scientific and Technical Information of China (English)

    唐志华; 熊海涛; 王铎; 吴迎春

    2009-01-01

    目的:建立一种Ce(Ⅳ)-抗坏血酸-奎宁化学发光体系快速测定奎宁的化学发光分析新方法.方法:在硫酸介质中,抗坏血酸可以显著增敏Ce(SO4)2-奎宁产生的化学发光,从而试验以流动注射化学发光法测定奎宁注射液.结果:在优化的试验条件下,该法测定奎宁的线性范围4为1.0×10-6~1.0×10-4g·mL-1,检出限为3.7×10-7g·mL-1,其RSD为1.6%(c=5.0×10-6g·mL-1,n=11).结论:方法的选择性较高,线性范围较宽,并成功应用于奎宁针剂含量的测定,扩大了具有荧光特性药物的分析范围.

  7. Isopoly-Tungstic Acid Resonance Rayleigh Scattering Method for the Determination of Quinine Sulfate%同多钨酸根共振瑞利散射光谱法测定硫酸奎宁

    Institute of Scientific and Technical Information of China (English)

    孔玲; 刘忠芳; 刘绍璞

    2010-01-01

    在pH=2.2~3.4的HCl-NaAc弱酸性介质中,硫酸奎宁和同多钨酸根相结合生成离子缔合物,能引起共振瑞利散射的显著增强,且散射强度与硫酸奎宁的浓度在一定范围内成正比,检出限为7.7 ng/mL.考察了共存物质的影响,表明该方法具有较好的选择性.用于汤尼水(Tonic Water)中奎宁的测定,结果满意.并对离子缔合物的形成和RRS增强的原因进行了讨论.

  8. Design and Rehabilitation for Oxidization Column of Hydrogen Peroxide Using Anthracene and Quinine Process%蒽醌法生产过氧化氢工艺中氧化塔的设计与改造

    Institute of Scientific and Technical Information of China (English)

    施友立

    2006-01-01

    通过对当前过氧化氢生产装置氧化塔氧化收率偏低的各种因素进行分析,找出影响氧化收率的关键因素,并提出氧化塔设计或改造的方向.并列举该类塔的改造效果.

  9. Synthesis and catalytic properties of chiral quinine-porphyrin Mn*#complexes%手性奎宁-卟啉锰催化剂的合成及其催化性能

    Institute of Scientific and Technical Information of China (English)

    王亚军; 刘彦钦; 韩士田

    2003-01-01

    @@ 为了寻找催化活性、相转移活性和手性诱导为一体的卟啉配体[1-4],我们把卟啉和手性相转移源连结起来,用奎宁-卟啉化合物作配体[5],考察其锰(Ⅲ)配合物为催化剂对烯烃环氧化反应的催化性能.

  10. Study on preparation and separation of cellulose acetate-quinine molecularly imprinted composite membrane%醋酸纤维-奎宁分子印迹复合膜的制备及分离性能研究

    Institute of Scientific and Technical Information of China (English)

    张春静; 钟世安

    2008-01-01

    采用多孔醋酸纤维膜为支撑体,制备了奎宁分子印迹复合膜,并对膜的选择结合性及分离性能进行了研究.研究结果表明,奎宁分子印迹复合膜对模板分子奎宁具有较好的选择结合性,奎宁在膜上结合量达到20.6μmol/g,奎宁/辛可宁的分离因子则为5.6;膜透过实验表明辛可宁透过奎宁分子印迹复合膜速率远大于奎宁的透过速率,该透过机理符合膜渗透的"溶解一扩散"模型.

  11. Studies on Character of Adsorption and Recognition of Quinine Imprinted Polymer%奎宁印迹聚合物的吸附与识别特性的研究

    Institute of Scientific and Technical Information of China (English)

    徐伟箭; 卢彦兵; 罗鹏

    2002-01-01

    以奎宁为模板分子,利用分子印迹技术合成了一种新型的类似于人工受体的印迹聚合物,研究了它对奎宁和其它底物的吸附特性和选择性识别能力,并对其固相萃取性能做了初步的研究.

  12. 4-amine Quinine Based Ionic Liquid: an Efficient Catalyst for Knoevenagel Condensation%基于4-氨基奎宁的离子液体在Knoevenagel缩合反应中的应用

    Institute of Scientific and Technical Information of China (English)

    高晓冲; 马友光; 高瑞昶

    2016-01-01

    以4-氨基奎宁为原料,两步法制备了离子液体[ADPQ] [BF4],将其用于催化复杂的活性亚甲基化合物与芳香醛的Knoevenagel缩合反应.该反应体系在室温下就可进行,无需任何溶剂,反应时间短,收率高,后处理简单,催化剂重复使用5次后效果变化不大.

  13. Study on Quinine and Quinidine by the Time-Resolved Room Temperature Phosphorimetry%奎宁和奎尼丁的时间分辨室温磷光法研究

    Institute of Scientific and Technical Information of China (English)

    董川; 仝晓菲; 卫艳丽

    2007-01-01

    在Na2SO3化学除氧的基础上,以TINO3为重原子微扰剂诱导了奎宁和奎尼丁在胶束溶液中的室温磷光,并对影响其磷光的各种因素进行了详细研究,在此基础上利用时间分辨磷光技术,加入不同的手性识别荆,达到了对奎宁和奎尼丁的分子表征.

  14. 新型手性相转移催化剂N-苄基溴化奎宁的合成及应用%Synthesis and application of a new chiral phase transfer catalyst N-benzyl quinine bromide

    Institute of Scientific and Technical Information of China (English)

    吴建一; 赵惠明; 俞兴源

    2005-01-01

    通过对天然手性物质进行修饰合成手性相转移催化剂N-苄基溴化奎宁,并对目标分子2,5-二甲基-4-(3-硝基苯)-1,4-二氢吡啶-3-甲酸乙酯-5-甲酸甲酯(nitrendipine)进行不对称催化合成,并通过红外光谱和核磁共振氢谱对化合物进行了表征,用X射线单晶衍射法测定了该化合物的晶体结构.

  15. 铈(Ⅳ)-抗坏血酸-奎宁化学发光分析体系测定抗坏血酸%Determination of Ascorbic Acid by Ce(Ⅳ)-Ascorbic Acid-Quinine Chemiluminescence Analytical System

    Institute of Scientific and Technical Information of China (English)

    唐志华; 熊海涛

    2009-01-01

    基于在酸性条件下Ce(Ⅳ)能氧化抗坏血酸产生微弱化学发光,加入奎宁后能显著增强其发光强度,并且发光强度与抗坏血酸浓度在一定范围内呈线性关系,建立流动注射化学发光分析法测定抗坏血酸.在最佳实验条件下,该法线性范围为0.03~1.0mg/ml,检出限为0.012mg/ml,对0.3mg/ml的抗坏血酸溶液平行测定11次,其相对标准偏差(RSD)为2.5%,可成功应用于VC针剂的测定.

  16. 短孔道SBA-15固载奎宁催化不对称Michael加成反应%SHORT-MESOCHANNEL SBA-15 SUPPORTED QUININE FOR ASYMMETRIC MICHAEL ADDITION REACTIONS

    Institute of Scientific and Technical Information of China (English)

    辛翠

    2015-01-01

    合成了大小为400~500 nm片状的短孔道SBA-15,并在其表面固载奎宁,制得一种有效的非均相有机催化剂,对其进行了XRD、FT-IR、电镜表征.以查尔酮类化合物与丙二腈的不对称Michael加成反应为模型考察了非均相催化剂催化活性,结果表明:以短孔道SBA-15为载体的催化剂和以常规SBA-15为载体的催化剂对查耳酮、4-甲氧基查尔酮、4-氟查尔酮为底物的反应产物收率对比为56% vS 50%,、58% VS 45%,,60% vS 54%,对映选择性对比为56% VS 36%,37% VS 26%,41% VS 34%.与SBA-15为载体固载奎宁制备催化剂相比,短孔道SBA-15固载的奎宁催化剂表现出了高于前者的催化活性和对映选择性.

  17. 光谱法研究硫酸奎宁与小牛胸腺DNA的相互作用%Spectrometry Research about the Interaction between Quinine Sulfate and Calf Thymus DNA

    Institute of Scientific and Technical Information of China (English)

    李俊芬; 李晋增; 董川

    2013-01-01

    本文采用紫外吸收光谱、荧光光谱、荧光偏振等方法研究了硫酸奎宁(QN)与小牛胸腺DNA(ctDNA)的相互作用,考察了影响其相互作用的各种因素,探讨了作用机理和作用方式.DNA存在时,QN的荧光被显著猝灭,吸收光谱出现减色现象.荧光偏振和阴离子猝灭等实验证实QN通过嵌插方式与ctDNA作用.测得QN与DNA的本征键合常数为1.51(±0.13)×104 L/mol,结合位点数为0.997,一分子的QN可以和大约1个碱基对作用.

  18. Treatment of Plasmodium falciparum malaria with mefloquine alone or in combination with i.v. quinine at the Department of Communicable and Tropical Diseases, Rigshospitalet, Copenhagen 1982-1988

    DEFF Research Database (Denmark)

    Magnussen, P; Bygbjerg, Ib Christian

    1990-01-01

    At the Department of Communicable and Tropical Diseases, Rigshospitalet, Denmark, mefloquine has been used since 1982 for the treatment of patients with suspected or verified chloroquine and sulfadoxine-pyrimethamine resistant P. falciparum malaria. Eighty-one patients treated with mefloquine...... and effective for the treatment of P. falciparum malaria and is recommended for treatment of worldwide acquired P. falciparum malaria, although patients should be monitored closely to disclose resistance....

  19. Preparation of a Bis-Quinine Bonded Chiral Stationary Phase and Its Chiral Resolution Ability%键合偶联双奎宁手性固定相的制备和手性拆分性能

    Institute of Scientific and Technical Information of China (English)

    杜祖银; 肖如亭

    2005-01-01

    奎宁是一种天然的具有手性的生物碱(属于金鸡纳碱系列),可以作为高效液相色谱柱手性固定相的选择剂用于拆分手性化合物.奥地利的Lindner等[对金鸡纳碱类手性选择剂做了初步的研究,给出了基本的拆分机理;Lee等合成了侧链含金鸡纳碱的手性聚甲基丙烯酸酯;Krawinkler等对金鸡纳碱氨基甲酸酯型的手性选择剂与硅胶的键合方式进行了实验和理论分析.

  20. Treatment of Plasmodium falciparum malaria with mefloquine alone or in combination with i.v. quinine at the Department of Communicable and Tropical Diseases, Rigshospitalet, Copenhagen 1982-1988

    DEFF Research Database (Denmark)

    Magnussen, P; Bygbjerg, Ib Christian

    1990-01-01

    At the Department of Communicable and Tropical Diseases, Rigshospitalet, Denmark, mefloquine has been used since 1982 for the treatment of patients with suspected or verified chloroquine and sulfadoxine-pyrimethamine resistant P. falciparum malaria. Eighty-one patients treated with mefloquine are...

  1. Effect of an early bitter taste experience on subsequent feather-pecking behaviour in laying hens

    NARCIS (Netherlands)

    Harlander, A.; Beck, P.S.A.; Rodenburg, T.B.

    2010-01-01

    Recent studies showed that laying hens learn not to peck at bitter-tasting feathers from conspecifics. In the present experiment, feathers of newly hatched chicks were made distasteful by spraying them with a bitter-tasting substance (quinine). It was hypothesized that chicks could detect quinine an

  2. 1624-IJBCS -Article-Serigne Omar sarr+

    African Journals Online (AJOL)

    hp

    The method was validated for precision, accuracy and recovery studies. Limit of Detection ... of various analytical methods to determine quinine and ... The quinine standard USP (Rockville,. USA) and the ... instruments, Massachusetts, USA) connected to a Fujitsu ... Recovery studies were carried out by addition of known ...

  3. Prevalence of ototoxicity in University of Benin Teaching Hospital ...

    African Journals Online (AJOL)

    2012-01-23

    Jan 23, 2012 ... apparatus from exposure to chemical substances, resulting in hearing impairment ... caused hearing and vestibular disequilibrium in patients where it was used to treat .... Arsenic, cobalt, cyanides, benzene, propylene-glycol .... prevent quinine ototoxicity, quinine should be prescribed with caution, and if ...

  4. EVALUATION OF EFFICACY AND TOXICITY OF DIFFERENT TREATMENT REGIMENS IN PLASMODIUM FALCIPARUM MALARIA

    Directory of Open Access Journals (Sweden)

    CHOGTU BHARTI, ADIGA SACHIDANAND PRABHU MUKYAPRANA, K.L.BAIRY

    2013-09-01

    Full Text Available The efficacy and toxicity of four commonly used antimalarials was evaluated. Thecombinations evaluated were Artesunate and Doxycycline, Quinine and Doxycycline, Artesunateand Quinine, Artesunate and Mefloquine. The four combinations did not show any statisticallysignificant difference in terms of days of defervescence, parasite clearance and hospital stay. Allthe four combinations were well tolerated.

  5. Synthesis, Characterization of Pentatomic Transition Elements Molybdotugstovanadophosphoric Heteropoly Complexes, the Replaced Reaction with Quinine%过渡元素钼钨钒磷五元杂多配合物的合成、表征以及与奎宁的取代反应

    Institute of Scientific and Technical Information of China (English)

    周百斌; 韦永德; 王玉和; 马慧媛; 李中华; 郭元茹; 周宏立

    2003-01-01

    @@ 过渡元素单取代杂多配合物自1966年被合成以来[1],由于其独特的结构、化学性质和抗病毒性受到人们的重视[2~6],但含过渡元素的钼钨钒磷五元杂多配合物的设计合成至今未见报道.

  6. 铈(Ⅳ)-3,4-二羟基苯甲酸-奎宁化学发光体系的研究与应用%Study on Chemiluminescent System of Cerium(Ⅳ)-3,4-Dihydroxybenzoic Acid-Quinine and Its Application

    Institute of Scientific and Technical Information of China (English)

    唐志华; 吴迎春

    2010-01-01

    实验发现,3,4-二羟基苯甲酸与铈(Ⅳ)在酸性介质中产生弱化学发光反应,奎宁存在能增强此发光,由此建立了化学发光法测定微量3,4-二羟基苯甲酸的新方法.该方法的线性范围为8.0×10-7~1.0×10-4 mol/L,检出限为5.0×10-8,对8.0×10-6 mol/L的3,4-二羟基苯甲酸进行11次测定的相对偏差为3.0%.该法应用于测定汉江水中加入的3,4-二羟基苯甲酸,结果令人满意.

  7. Synthesis and Characterization of the Novel Multifunctional Catalysts of 6-Amino-Quinine Derivatives%一类新颖的6-氨基奎宁衍生的多功能催化剂的合成及其表征

    Institute of Scientific and Technical Information of China (English)

    侯文端; 彭云贵

    2016-01-01

    首次设计合成了一类新颖的6-氨基奎宁衍生的多功能有机小分子催化剂,该类催化剂同时具有叔氮、硫脲、磺酰胺3种基团.并通过核磁共振对其结构进行了表征.

  8. 咯萘啶、甲氟喹和奎宁对青蒿琥酯敏感株与抗性株恶性疟原虫的体外作用%EFFECT OF PYRONARIDINE, MEFLOQUINE AND QUININE ON ARTESUNATE-SENSITIVE AND ARTESUNATE-RESISTANT PLASMODIUM FALCIPARUM

    Institute of Scientific and Technical Information of China (English)

    杨恒林; 高白荷; 黄开国

    2000-01-01

    [目的]比较青蒿琥酯敏感株与抗性株恶性疟原虫对咯萘啶、甲氟喹和奎宁的敏感性;了解这3种药物与青蒿琥酯伍用对抗青蒿琥酯恶性疟原虫的体外抗疟作用.[方法]应用Rieckmann体外微量法测定敏感株与抗性株原虫对上述4种药物的敏感性,同时测定青蒿琥酯分别与咯萘啶、甲氟喹、奎宁伍用对抗性株原虫的敏感性.[结果]咯萘啶、甲氟喹、奎宁和青蒿琥酯对敏感株的ID50分别为59.0、69.7、283.8和9.6nmol/L;对抗性株的ID50依次为170.6、63.2、272.4及85.1nmol/L.咯萘啶与青蒿琥酯伍用,其ID50分别为两药单用组的1/4.7(36.6/170.6)和1/3.7(22.8/85.1).甲氟喹与青蒿琥酯伍用中,其ID50分别为两药单用组的1/4(40/160)和1/125(3.2/400).奎宁与青蒿琥酯伍用,其ID95分别为单用组的1/16(80/1280)和1/125(3.2/400).[结论]抗青蒿琥酯恶性疟原虫对甲氟喹和奎宁无交叉抗性,这两种药物分别与青蒿琥酯伍用,对抗青蒿琥酯恶性疟原虫有较明显增效作用.

  9. Inflexible and indifferent alcohol drinking in male mice.

    Science.gov (United States)

    Lesscher, Heidi M B; van Kerkhof, Linda W M; Vanderschuren, Louk J M J

    2010-07-01

    Alcoholism is characterized by compulsive alcohol intake, but this critical feature of alcoholism is seldom captured in preclinical studies. Here, we evaluated whether alcohol-preferring C57BL/6J mice develop compulsive alcohol drinking patterns, using adulteration of the alcohol solution with quinine, in a limited access choice paradigm. We assessed 2 independent aspects of compulsive drinking: (i) inflexible alcohol intake by testing whether mice would drink bitter alcohol solutions if this was their only source of alcohol and (ii) indifferent drinking by comparing intake of aversive and nonaversive alcohol solutions. Male C57BL/6J mice consumed alcohol for 2 or 8 consecutive weeks. The alcohol solution was then adulterated with graded quinine concentrations, and the effect on alcohol intake was determined. C57BL/6J mice rapidly developed compulsive alcohol drinking patterns. Adulteration of the alcohol solution with an aversive quinine concentration failed to reduce intake, indicative of inflexible drinking behavior, after only 2 weeks of alcohol experience, although quinine adulteration did suppress the acquisition of alcohol drinking in naïve mice. After 8 weeks of alcohol consumption, the mice also became indifferent to quinine. They consumed an aversive, quinine-containing alcohol solution, despite the simultaneous availability of an unadulterated alcohol solution. Prolonged alcohol ingestion did not alter the sensitivity to the bitter taste of quinine itself. These findings demonstrate the staged occurrence in mice of 2 distinct behavioral characteristics of alcoholism, i.e., inflexible and indifferent alcohol drinking.

  10. Drug: D02261 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ap07025 Quinolines Therapeutic category of drugs in Japan [BR:br08301] 6 Agents against pathologic organisms and parasites 64 Parasit...ics (systemic) 641 Antiprotozoans 6415 Quinines D02261 Q

  11. Poisoning by anti-malarial drugs

    African Journals Online (AJOL)

    The toxic effects on the cardiovascular system tend to be more severe from ... administering the quinine with glucose. However ... with attention to the Airway, Breathing and Circulation. .... neutropenia especially in children infected with HIV [7].

  12. Effect of antimalarial drugs on stimulation and interleukin 2 production of human lymphocytes

    DEFF Research Database (Denmark)

    Bygbjerg, I C; Svenson, M; Theander, T G

    1987-01-01

    Effect of pyrimethamine, an antimalarial antifolate, and of mefloquine, chloroquine, and quinine, which belong to the quinoline group of antimalarials, on proliferation and interleukin 2 (IL-2) production of human lymphocytes was studied in vitro. Pyrimethamine at concentrations above therapeutic...

  13. Microstructural Observations on Nissl Substances in the Cerebellar ...

    African Journals Online (AJOL)

    Erah

    intramuscularly with liquid quinine, 16mg/kg body weight as a start dose, followed by 8mg/kg ... Conclusion: The observed degenerative changes in the Nissl substances in the cerebellar .... conceptional development in pregnant rats in.

  14. Effects of anti-malarial alkaloids on the sperm properties and blood ...

    African Journals Online (AJOL)

    The effects of treatment with the anti-malarial alkaloids quinine and chloroquine ... properties and blood levels of selected reproductive hormones (testosterone, ... the short term use of these drugs to treat malaria may be associated with fertility ...

  15. Ocular complications of malaria treatment

    African Journals Online (AJOL)

    2011-10-08

    Oct 8, 2011 ... parenteral quinine are employed with consequent untoward effects. This article reports two cases of severe ocular toxicity, including mimicry of ... 2003 at the Ebony Eye Specialist Clinic Onitsha with a week history of double ...

  16. Tetany with Plasmodium falciparum infection.

    Science.gov (United States)

    Singh, P S; Singh, Neha

    2012-07-01

    Plasmodium falciparum is a malarial infection with high morbidity and wide spectrum of atypical presentation. Here we report an unusual presentation of malaria as tetany with alteration in calcium,phosphate and magnesium metabolism Hypocalcaemia in malaria can cause prolonged Q-Tc interval which could be arisk factor for quinine cardiotoxicity and sudden death Hence monitoring of serum calcium in severe malarial infection and cautious use of quinine in such patients is very important in management

  17. Plastic Membrane Electrodes of Coated Wire Type for Micro Determination of Quininium Cation in Pharmaceutical Tablets

    OpenAIRE

    2011-01-01

    Problem statement: Silver and copper all-solid state wire sensor electrodes of quininium cation with different ion exchangers have been prepared and used in pharmaceutical analysis. A comparative study with a reference method is applied in order to investigate the validity of the proposed method for potentiometric analysis of pharmaceutical compounds containing quinine. Approach: A Nernstian equation was proved for all electrodes of quinine in this research. Potentiometric investigations were...

  18. Observations on the Synergistic Interactions of Aqueous Oxidizers and Ultraviolet Radiation for Decontamination Applications

    Science.gov (United States)

    1986-05-20

    alkylbenzene sulfonic acids to carbon dioxide and water using UV irradiation and aqueous hypochlorite. Thus, the synergistic effect of high energy...Perhydroxyl Radicals. A Flash Photolysis Study," Cz.7 J. Cbem. 57, 3017-3022 (1979). M. Nakamura and Y.Ogata, "Photolytic Oxidation of AlkylBenzene Sulfonic ...the low concentration of quinine in the test solution, fluorescence is linear with concentration (Ewing, 1969). Since the pH of 2 x 10-4 quinine

  19. Direct solid surface fluorescence spectroscopy of standard chemicals and humic acid in ternary system.

    Science.gov (United States)

    Mounier, S; Nicolodelli, G; Redon, R; Milori, D M B P

    2017-04-15

    The front face fluorescence spectroscopy is often used to quantify chemicals in well-known matrices as it is a rapid and powerful technique, with no sample preparation. However it was not used to investigate extracted organic matter like humic substances. This work aims to fully investigate for the first time front face fluorescence spectroscopy response of a ternary system including boric acid, tryptophan and humic substances, and two binaries system containing quinine sulfate or humic substance in boric acid. Pure chemicals, boric acid, tryptophan, quinine sulfate and humic acid were mixed together in solid pellet at different contents from 0 to 100% in mass. The measurement of excitation emission matrix of fluorescence (3D fluorescence) and laser induced fluorescence were then done in the front face mode. Fluorescence matrices were decomposed using the CP/PARAFAC tools after scattering treatments. Results show that for 3D fluorescence there is no specific component for tryptophan and quinine sulfate, and that humic substances lead to a strong extinction effect for mixture containing quinine sulfate. Laser induced fluorescence gives a very good but non-specific related response for both quinine sulfate and tryptophan. No humic substances fluorescence response was found, but extinction effect is observed as for 3D fluorescence. This effect is stronger for quinine sulfate than for tryptophan. These responses were modeled using a simple absorbance versus emission model.

  20. Direct solid surface fluorescence spectroscopy of standard chemicals and humic acid in ternary system

    Science.gov (United States)

    Mounier, S.; Nicolodelli, G.; Redon, R.; Milori, D. M. B. P.

    2017-04-01

    The front face fluorescence spectroscopy is often used to quantify chemicals in well-known matrices as it is a rapid and powerful technique, with no sample preparation. However it was not used to investigate extracted organic matter like humic substances. This work aims to fully investigate for the first time front face fluorescence spectroscopy response of a ternary system including boric acid, tryptophan and humic substances, and two binaries system containing quinine sulfate or humic substance in boric acid. Pure chemicals, boric acid, tryptophan, quinine sulfate and humic acid were mixed together in solid pellet at different contents from 0 to 100% in mass. The measurement of excitation emission matrix of fluorescence (3D fluorescence) and laser induced fluorescence were then done in the front face mode. Fluorescence matrices were decomposed using the CP/PARAFAC tools after scattering treatments. Results show that for 3D fluorescence there is no specific component for tryptophan and quinine sulfate, and that humic substances lead to a strong extinction effect for mixture containing quinine sulfate. Laser induced fluorescence gives a very good but non-specific related response for both quinine sulfate and tryptophan. No humic substances fluorescence response was found, but extinction effect is observed as for 3D fluorescence. This effect is stronger for quinine sulfate than for tryptophan. These responses were modeled using a simple absorbance versus emission model.

  1. Prescription pattern of anti-malarial drugs in a tertiary care hospital

    Institute of Scientific and Technical Information of China (English)

    Santoshkumar R Jeevangi; Manjunath S; Sharanabasappa M Awanti

    2010-01-01

    Objective:To evaluate the prescribing pattern of anti malarial drugs in a tertiary care hospital. Methods:A prospective cross-sectional study was conducted for 6 months of patients visiting in Basaveshwar Teaching and General Hospital, Gulbarga. Data were analyzed for various drug use indicators. Results: A total of 212 prescriptions were collected, with 136 (64.15%) male and 76 (35.85%) female. There were 128 (60.37%) Plasmodium vivax cases and 84 (39.63%) Plasmodium falciparum cases. All Plasmodium vivax cases were treated with chloroquine alone and among these 16 (12.5%) recieved radical treatment with primaquine along with chloroquine. Among 84 patients with Pasmodium falciparum, 40 patients received single drug such as quinine/mefloquinine/artesunate/arteether. Another 44 patients received multidrug regime like, quinine+artesunate (54.54%), quinine+mefloquine (27.27%) and quinine+arteether (18.18%). Chloroquine was not administered to any of the patients with Plasmodium falciparum malaria. The most common adverse effects with chloroquine were anorexia, nausea, vomiting and tinnitus in 9.37%of the cases. With quinine it was nausea and vomiting in 17.64%, tinnitus in 11.76%and hypoglycemia in 2.1%of cases. Conclusions: Our study found the perennial favorites like chloroquine for Plasmodium vivax and quinine for Plasmodium falciparum were the most effective drug. In the severe Plasmodium falciparum cases the artesunate derivatives and combination of artesunate with quinine/mefloquine were most effective with fewer incidences of side effects.

  2. Bitter taste stimuli induce differential neural codes in mouse brain.

    Directory of Open Access Journals (Sweden)

    David M Wilson

    Full Text Available A growing literature suggests taste stimuli commonly classified as "bitter" induce heterogeneous neural and perceptual responses. Here, the central processing of bitter stimuli was studied in mice with genetically controlled bitter taste profiles. Using these mice removed genetic heterogeneity as a factor influencing gustatory neural codes for bitter stimuli. Electrophysiological activity (spikes was recorded from single neurons in the nucleus tractus solitarius during oral delivery of taste solutions (26 total, including concentration series of the bitter tastants quinine, denatonium benzoate, cycloheximide, and sucrose octaacetate (SOA, presented to the whole mouth for 5 s. Seventy-nine neurons were sampled; in many cases multiple cells (2 to 5 were recorded from a mouse. Results showed bitter stimuli induced variable gustatory activity. For example, although some neurons responded robustly to quinine and cycloheximide, others displayed concentration-dependent activity (p<0.05 to quinine but not cycloheximide. Differential activity to bitter stimuli was observed across multiple neurons recorded from one animal in several mice. Across all cells, quinine and denatonium induced correlated spatial responses that differed (p<0.05 from those to cycloheximide and SOA. Modeling spatiotemporal neural ensemble activity revealed responses to quinine/denatonium and cycloheximide/SOA diverged during only an early, at least 1 s wide period of the taste response. Our findings highlight how temporal features of sensory processing contribute differences among bitter taste codes and build on data suggesting heterogeneity among "bitter" stimuli, data that challenge a strict monoguesia model for the bitter quality.

  3. Science in the service of colonial agro-industrialism: the case of cinchona cultivation in the Dutch and British East Indies, 1852-1900.

    Science.gov (United States)

    Roersch van der Hoogte, Arjo; Pieters, Toine

    2014-09-01

    The isolation of quinine from cinchona bark in 1820 opened new possibilities for the mass-production and consumption of a popular medicine that was suitable for the treatment of intermittent (malarial) fevers and other diseases. As the 19th century European empires expanded in Africa and Asia, control of tropical diseases such as malaria was seen as crucial. Consequently, quinine and cinchona became a pivotal tool of British, French, German and Dutch empire-builders. This comparative study shows how the interplay between science, industry and government resulted in different historical trajectories for cinchona and quinine in the Dutch and British Empires during the second half of the 19th century. We argue that in the Dutch case the vectors of assemblage that provided the institutional and physical framework for communication, exchange and control represent an early example of commodification of colonial science. Furthermore, both historical trajectories show how the employment of the laboratory as a new device materialised within the colonial context of agricultural and industrial production of raw materials (cinchona bark), semi-finished product (quinine sulphate) and plant-based medicines like quinine. Hence, illustrating the 19th century transition from 'colonial botany' and 'green imperialism' to what we conceptualise as 'colonial agro-industrialism'.

  4. Rapid and Green Analytical Method for the Determination of Quinoline Alkaloids from Cinchona succirubra Based on Microwave-Integrated Extraction and Leaching (MIEL Prior to High Performance Liquid Chromatography

    Directory of Open Access Journals (Sweden)

    Farid Chemat

    2011-11-01

    Full Text Available Quinas contains several compounds, such as quinoline alkaloids, principally quinine, quinidine, cinchonine and cichonidine. Identified from barks of Cinchona, quinine is still commonly used to treat human malaria. Microwave-Integrated Extraction and Leaching (MIEL is proposed for the extraction of quinoline alkaloids from bark of Cinchona succirubra. The process is performed in four steps, which ensures complete, rapid and accurate extraction of the samples. Optimal conditions for extraction were obtained using a response surface methodology reached from a central composite design. The MIEL extraction has been compared with a conventional technique soxhlet extraction. The extracts of quinoline alkaloids from C. succirubra obtained by these two different methods were compared by HPLC. The extracts obtained by MIEL in 32 min were quantitatively (yield and qualitatively (quinine, quinidine, cinchonine, cinchonidine similar to those obtained by conventional Soxhlet extraction in 3 hours. MIEL is a green technology that serves as a good alternative for the extraction of Cinchona alkaloids.

  5. Alkaloid decomposition by DC pin-hole discharge in water solution

    Science.gov (United States)

    Klimova, Edita J.; Krcma, Frantisek; Jonisova, Lenka

    2016-08-01

    DC diaphragm discharge generated in a batch reactor was used to decompose two selected model alkaloids, caffeine and quinine in concentrations ranging from 10 to 50 ppm or 5 to 15 ppm, respectively. UV-vis spectrometry was utilized in evaluation of H2O2 production during the process as well as degradation of caffeine. Fluorescence spectrometry was used for quantification of quinine. High rates of decomposition were reached in both cases in the anode part of the reactor. On the other hand, up to four times lower decomposition was observed in the cathode part. Total removal efficiency gained up to 300 mg/kWh for caffeine and 210 mg/kWh for quinine. Contribution to the topical issue "6th Central European Symposium on Plasma Chemistry (CESPC-6)", edited by Nicolas Gherardi, Ester Marotta and Cristina Paradisi

  6. Rapid and green analytical method for the determination of quinoline alkaloids from Cinchona succirubra based on Microwave-Integrated Extraction and Leaching (MIEL) prior to high performance liquid chromatography.

    Science.gov (United States)

    Fabiano-Tixier, Anne-Sylvie; Elomri, Abdelhakim; Blanckaert, Axelle; Seguin, Elisabeth; Petitcolas, Emmanuel; Chemat, Farid

    2011-01-01

    Quinas contains several compounds, such as quinoline alkaloids, principally quinine, quinidine, cinchonine and cichonidine. Identified from barks of Cinchona, quinine is still commonly used to treat human malaria. Microwave-Integrated Extraction and Leaching (MIEL) is proposed for the extraction of quinoline alkaloids from bark of Cinchona succirubra. The process is performed in four steps, which ensures complete, rapid and accurate extraction of the samples. Optimal conditions for extraction were obtained using a response surface methodology reached from a central composite design. The MIEL extraction has been compared with a conventional technique soxhlet extraction. The extracts of quinoline alkaloids from C. succirubra obtained by these two different methods were compared by HPLC. The extracts obtained by MIEL in 32 min were quantitatively (yield) and qualitatively (quinine, quinidine, cinchonine, cinchonidine) similar to those obtained by conventional Soxhlet extraction in 3 hours. MIEL is a green technology that serves as a good alternative for the extraction of Cinchona alkaloids.

  7. D-Serine and D-Cycloserine Reduce Compulsive Alcohol Intake in Rats.

    Science.gov (United States)

    Seif, Taban; Simms, Jeffrey A; Lei, Kelly; Wegner, Scott; Bonci, Antonello; Messing, Robert O; Hopf, F Woodward

    2015-09-01

    There is considerable interest in NMDAR modulators to enhance memory and treat neuropsychiatric disorders such as addiction, depression, and schizophrenia. D-serine and D-cycloserine, the NMDAR activators at the glycine site, are of particular interest because they have been used in humans without serious adverse effects. Interestingly, D-serine also inhibits some NMDARs active at hyperpolarized potentials (HA-NMDARs), and we previously found that HA-NMDARs within the nucleus accumbens core (NAcore) are critical for promoting compulsion-like alcohol drinking, where rats consume alcohol despite pairing with an aversive stimulus such as quinine, a paradigm considered to model compulsive aspects of human alcohol use disorders (AUDs). Here, we examined the impact of D-serine and D-cycloserine on this aversion-resistant alcohol intake (that persists despite adulteration with quinine) and consumption of quinine-free alcohol. Systemic D-serine reduced aversion-resistant alcohol drinking, without altering consumption of quinine-free alcohol or saccharin with or without quinine. Importantly, D-serine within the NAcore but not the dorsolateral striatum also selectively reduced aversion-resistant alcohol drinking. In addition, D-serine inhibited EPSCs evoked at -70 mV in vitro by optogenetic stimulation of mPFC-NAcore terminals in alcohol-drinking rats, similar to reported effects of the NMDAR blocker AP5. Further, D-serine preexposure occluded AP5 inhibition of mPFC-evoked EPSCs, suggesting that D-serine reduced EPSCs by inhibiting HA-NMDARs. Systemic D-cycloserine also selectively reduced intake of quinine-adulterated alcohol, and D-cycloserine inhibited NAcore HA-NMDARs in vitro. Our results indicate that HA-NMDAR modulators can reduce aversion-resistant alcohol drinking, and support testing of D-serine and D-cycloserine as immediately accessible, FDA-approved drugs to treat AUDs.

  8. D-Serine and D-Cycloserine Reduce Compulsive Alcohol Intake in Rats

    Science.gov (United States)

    Seif, Taban; Simms, Jeffrey A; Lei, Kelly; Wegner, Scott; Bonci, Antonello; Messing, Robert O; Hopf, F Woodward

    2015-01-01

    There is considerable interest in NMDAR modulators to enhance memory and treat neuropsychiatric disorders such as addiction, depression, and schizophrenia. D-serine and D-cycloserine, the NMDAR activators at the glycine site, are of particular interest because they have been used in humans without serious adverse effects. Interestingly, D-serine also inhibits some NMDARs active at hyperpolarized potentials (HA-NMDARs), and we previously found that HA-NMDARs within the nucleus accumbens core (NAcore) are critical for promoting compulsion-like alcohol drinking, where rats consume alcohol despite pairing with an aversive stimulus such as quinine, a paradigm considered to model compulsive aspects of human alcohol use disorders (AUDs). Here, we examined the impact of D-serine and D-cycloserine on this aversion-resistant alcohol intake (that persists despite adulteration with quinine) and consumption of quinine-free alcohol. Systemic D-serine reduced aversion-resistant alcohol drinking, without altering consumption of quinine-free alcohol or saccharin with or without quinine. Importantly, D-serine within the NAcore but not the dorsolateral striatum also selectively reduced aversion-resistant alcohol drinking. In addition, D-serine inhibited EPSCs evoked at −70 mV in vitro by optogenetic stimulation of mPFC–NAcore terminals in alcohol-drinking rats, similar to reported effects of the NMDAR blocker AP5. Further, D-serine preexposure occluded AP5 inhibition of mPFC-evoked EPSCs, suggesting that D-serine reduced EPSCs by inhibiting HA-NMDARs. Systemic D-cycloserine also selectively reduced intake of quinine-adulterated alcohol, and D-cycloserine inhibited NAcore HA-NMDARs in vitro. Our results indicate that HA-NMDAR modulators can reduce aversion-resistant alcohol drinking, and support testing of D-serine and D-cycloserine as immediately accessible, FDA-approved drugs to treat AUDs. PMID:25801502

  9. A systematic review of the safety and efficacy of artemether-lumefantrine against uncomplicated Plasmodium falciparum malaria during pregnancy

    Directory of Open Access Journals (Sweden)

    Manyando Christine

    2012-05-01

    Full Text Available Abstract Malaria during pregnancy, particularly Plasmodium falciparum malaria, has been linked to increased morbidity and mortality, which must be reduced by both preventive measures and effective case management. The World Health Organization (WHO recommends artemisinin-based combination therapy (ACT to treat uncomplicated falciparum malaria during the second and third trimesters of pregnancy, and quinine plus clindamycin during the first trimester. However, the national policies of many African countries currently recommend quinine throughout pregnancy. Therefore, the aim of this article is to provide a summary of the available data on the safety and efficacy of artemether-lumefantrine (AL in pregnancy. An English-language search identified 16 publications from 1989 to October 2011 with reports of artemether or AL exposure in pregnancy, including randomized clinical trials, observational studies and systematic reviews. Overall, there were 1,103 reports of AL use in pregnant women: 890 second/third trimester exposures; 212 first trimester exposures; and one case where the trimester of exposure was not reported. In the second and third trimesters, AL was not associated with increased adverse pregnancy outcomes as compared with quinine or sulphadoxine-pyrimethamine, showed improved tolerability relative to quinine, and its efficacy was non-inferior to quinine. There is evidence to suggest that the pharmacokinetics of anti-malarial drugs may change in pregnancy, although the impact on efficacy and safety needs to be studied further, especially since the majority of studies report high cure rates and adequate tolerability. As there are fewer reports of AL safety in the first trimester, additional data are required to assess the potential to use AL in the first trimester. Though the available safety and efficacy data support the use of AL in the second and third trimesters, there is still a need for further information. These findings reinforce the

  10. Intravenous artesunate for severe malaria in travelers, Europe

    DEFF Research Database (Denmark)

    Zoller, Thomas; Junghanss, Thomas; Kapaun, Annette

    2011-01-01

    Multicenter trials in Southeast Asia have shown better survival rates among patients with severe malaria, particularly those with high parasitemia levels, treated with intravenous (IV) artesunate than among those treated with quinine. In Europe, quinine is still the primary treatment for severe...... malaria. We conducted a retrospective analysis for 25 travelers with severe malaria who returned from malaria-endemic regions and were treated at 7 centers in Europe. All patients survived. Treatment with IV artesunate rapidly reduced parasitemia levels. In 6 patients at 5 treatment centers, a self...... of malaria patients in Europe. Patients should be monitored for signs of hemolysis, especially after parasitologic cure....

  11. [Is Plasmodium falciparum, the parasite responsible for tropical malaria, resistant to fansidar?].

    Science.gov (United States)

    Holzer, B; Keller, H; Frossard, E; Stürchler, D

    1980-03-01

    A world-wide increase of malaria infections is observed. Malaria is imported into Switzerland mainly by tourists and recently by refugees from South East Asia. The strains of P. falciparum resistant to treatment are of increasing importance. A patient with P. falciparum infection from Cambodia is reported, who suffered from three episodes of malaria recrudescence within ten weeks, in spite of adequate therapy with quinine and Fansidar. The definition, the significance and the geographical distribution of resistances and the possible cause for a P. falciparum recrudescence are discussed. For the treatment of repeating recrudescence quinine and Fansidar are recommended, followed by a suppressive Fansidar prophylaxy for 4--8 weeks.

  12. Taste neophobia and palatability: the pleasure of drinking.

    Science.gov (United States)

    Lin, Jian-You; Amodeo, Leslie Renee; Arthurs, Joseph; Reilly, Steve

    2012-06-25

    Taste neophobia is manifested behaviorally as lower intake of a novel, potentially dangerous tastant relative to the same tastant when it is perceived as safe and familiar. To further characterize this phenomenon, microstructural analysis of lick patterns was used to track the transition from novel to familiar for three tastants: saccharin, quinine and Polycose. The results revealed that in addition to an increase in the amount consumed (for saccharin and quinine but not Polycose), cluster size (an index of palatability) became larger as familiarity with the benign tastants increased. The current finding suggests that the pleasure of drinking increases as the novel, potentially dangerous tastant becomes accepted as safe.

  13. Development of mini-tablets with 1mm and 2mm diameter.

    Science.gov (United States)

    Tissen, Corinna; Woertz, Katharina; Breitkreutz, Joerg; Kleinebudde, Peter

    2011-09-15

    The feasibility of formulating mini-tablets with 1mm diameter on a rotary-die press in comparison to mini-tablets of 2mm was investigated. To gain insight into the production of 1mm mini-tablets, three model drugs of different compression characteristics were chosen, namely quinine hydrochloride, ibuprofen and spray-dried gentian extract. A high drug load in combination with robust and reproducible mechanical properties was requested. Depending on the individual drug substance, mini-tablets were produced by direct compression or after roll-compaction/dry granulation. The tensile strength, mass, and their variation coefficients were determined to assess the mechanical properties of the tablets. The content uniformity and the dissolution behavior of selected batches were analyzed. For the first time 1mm mini-tablets could be successfully produced by direct compression (90% quinine hydrochloride; 90% dried gentian extract) and after roll compaction (70% ibuprofen). Depending on the applied compression pressure, 1mm mini-tablets with quinine hydrochloride exhibited robust mechanical properties (e.g. median tensile strength of 2.02N/mm(2)) with equal or lower variance of distribution compared to the 2mm compacts. With respect to content uniformity of dosage forms, 1mm mini-tablets containing 80% quinine hydrochloride met the requirements of the European Pharmacopeia (AV=6.8).

  14. Bio-antioxidant of Anthraquinone Derivatives

    Institute of Scientific and Technical Information of China (English)

    CUI,Jian; LI,Zhao-Long; HONG,Xiao-Yin

    2004-01-01

    @@ The Rubiaceae family is well known for containing anthraquinones. More specifically, lapachol and its analogues are known to possess antitumor, antibiotic, antimalarial and antiulceric activities.[1] Several report indicated that some quinones containing OH in its structure were found to have higher bio-activity than quinines lacking the OH group.

  15. THE SYNTHESIS OF TWO KINDS OF POLYMERSUPPORTED ASYMMETRIC PHASE TRANSFER CATALYSITS(PS—PTCS)AND THE COMPARISON OF THEIR CATALYTIC ACTIVITIES

    Institute of Scientific and Technical Information of China (English)

    ZHANGZhengpu; HUANGJinxia; 等

    1999-01-01

    In this paper,two kinds of PS-PTCs were synthesized using different methods by introducing cinchonine and quinine to the polymer support.Their catalytic properties for the alkylation of N-diphenylmethylene glycine t-butyl ester were also compared.

  16. WHO推荐在缺少药物时抗疟疾的第二选择

    Institute of Scientific and Technical Information of China (English)

    黄敏燕

    2005-01-01

    WHO建议各国加速获得二线抗疟疾药物,通常为奎宁(quinine),直到含青蒿素(artemisinin)的复方蒿甲醚/苯芴醇(artemether/lumefantrine)(Ⅰ)的供应短缺得到解决。

  17. Intravenous artesunate reduces parasite clearance time, duration of intensive care, and hospital treatment in patients with severe malaria in Europe

    DEFF Research Database (Denmark)

    Kurth, Florian; Develoux, Michel; Mechain, Matthieu;

    2015-01-01

    Intravenous artesunate improves survival in severe malaria, but clinical trial data from nonendemic countries are scarce. The TropNet severe malaria database was analyzed to compare outcomes of artesunate vs quinine treatment. Artesunate reduced parasite clearance time and duration of intensive...

  18. Non-aqueous CE-MS of cinchona alkaloids - characterization of a novel CE-ESI-MS interface

    DEFF Research Database (Denmark)

    Hansen, Frederik André; Hansen, Steen Honoré; Petersen, Nickolaj J.

    . Furthermore, the increased conductivity of the buffer in the fracture generates field free pumping of the analytes towards the ESI spray tip. In this study the device was used to analyze the four major alkaloids (diastereomeric pairs of quinine/quinidine and cinchonine/cinchonidine) in Cinchona bark samples...

  19. A convenient microwave-assisted synthesis of cinchona alkaloid-derived ligands

    Institute of Scientific and Technical Information of China (English)

    2008-01-01

    An efficient synthesis of cinchona alkaloid-derived ligands based on solvent-free microwave-assisted reaction was described. The coupling of 1,4-dichlorophthalazine or 3,6-dichloropyridazine with quinine, cinchonine or cinchonidine provide bis- or mono-cinchona alkaloid-derived ligands in moderate to good yields (52-89%) within 15 rain under optimum microwave conditions.

  20. Continued efficacy of sulfadoxine-pyrimethamine as second line treatment for malaria in children in Guinea-Bissau

    DEFF Research Database (Denmark)

    Kofoed, Poul-Erik; Rodrigues, Amabelia; Aaby, Peter;

    2006-01-01

    sensitivity, the efficacy of S/P was studied immediately before the introduction of the drug and 6-9 years later. METHODS: Children participating in clinical in vivo studies were given S/P if having late clinical treatment failure following the treatment with quinine, chloroquine, or amodiaquine...

  1. Science in the service of colonial agro-industrialism : the case of cinchona cultivation in the Dutch and British East Indies, 1852-1900

    NARCIS (Netherlands)

    Roersch van der Hoogte, Arjo; Pieters, Toine

    2014-01-01

    The isolation of quinine from cinchona bark in 1820 opened new possibilities for the mass-production and consumption of a popular medicine that was suitable for the treatment of intermittent (malarial) fevers and other diseases. As the 19th century European empires expanded in Africa and Asia, contr

  2. Safety and efficacy of iron supplementation in pregnant Kenyan women

    NARCIS (Netherlands)

    Mwangi, M.N.

    2014-01-01

    Since the British doctor Ronald Ross received the 1902 Nobel Prize in medicine for his work on malaria, more people have died from the disease than all world wars combined. This is in spite of the fact that the French chemists Pierre Joseph Pelletier and Joseph Bienaimé Caventou made quinine

  3. In Vitro Evaluation of Drug Susceptibilities of Babesia divergens Isolates

    OpenAIRE

    Brasseur, Philippe; Lecoublet, Sophie; Kapel, Nathalie; Favennec, Loic; Ballet, Jean J.

    1998-01-01

    The susceptibilities of three bovine and two human Babesia divergens isolates to antimicrobial agents were evaluated in vitro by a tritiated hypoxanthine incorporation assay. The MICs at which 50% of isolates are inhibited (MIC50s) for mefloquine (chlorhydrate), chloroquine (sulfate), quinine (chlorhydrate), clindamycin (phosphate), pentamidine (isethionate), phenamidine (isethionate) plus oxomemazine (chlorhydrate), lincomycin (chlorhydrate monohydrate), and imidocarb (dipropionate) were det...

  4. Acalculous Cholecystitis in a Pediatric Patient with Plasmodium falciparum Infection: A Case Report and Literature Review.

    Science.gov (United States)

    Aguilera-Alonso, David; Medina, Eva María López; Del Rosal, Teresa; Arrieta, Julián Villota; Escosa-García, Luis; Hortelano, Milagros García

    2017-08-02

    Malaria has been associated with acute acalculous cholecystitis, a very uncommon complication in children. We present a 5-year-old girl, originally from Equatorial-Guinea, diagnosed with severe malaria with acute kidney injury, thrombocytopenia and acute acalculous cholecystitis. She was treated with intravenous quinine and clindamycin, plus cefotaxime and metronidazole with a full resolution without surgery.

  5. The Use Of Animals In Endocrine Research: A Synopsis | Osinubi ...

    African Journals Online (AJOL)

    Onemajor challenge in the field of endocrinology is diabetes mellitus. ... induced by chemicals or diet, surgicalmanipulations and by genetic engineering. ... The quinine-animal model for the study of male reproductive endocrinology andsome potential models for the investigations of thyroid diseases are also presented.

  6. Gustatory receptor neuron responds to DEET and other insect repellents in the yellow fever mosquito, aedes aegypti

    Science.gov (United States)

    Three gustatory receptor neurons were characterized for contact chemoreceptive sensilla on the labella of female yellow fever mosquitoes, Aedes aegypti. The neuron with the smallest amplitude spike responded to the feeding deterrent, quinine, as well as DEET and other insect repellents. Two other ...

  7. Taste perception with age: pleasantness and its relationships with threshold sensitivity and supra-threshold intensity of five taste qualities

    NARCIS (Netherlands)

    Mojet, J.; Christ-Hazelhof, E.; Heidema, J.

    2005-01-01

    The relationships between threshold sensitivity, supra-threshold intensity of NaCl, KCl, sucrose, aspartame, acetic acid, citric acid, caffeine, quinine HCl, monosodium glutamate (MSG) and inosine 5¿-monophosphate (IMP), and the pleasantness of these stimuli in products, were studied in 21 young sub

  8. Drug: D08810 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ts 722 Various function testing reagents 7229 Others D08810 Quinine hydrochloride - sodium chloride - tartaric acid - sucrose mixt PubChem: 96025493 ... ...61] Therapeutic category of drugs in Japan [BR:br08301] 7 Agents not mainly for therapeutic purpose 72 Intracorporeal diagnostic agen

  9. Neurological Limitations of Aircraft Operations: Human Performance Implications (les Limitations neurologiques des operations aeriennes: les Consequences pour les performances des equipages).

    Science.gov (United States)

    1996-04-01

    malingering Systemic lupus erythematosus Drugs (quinine, quinidine) After cerebral angiography II. PHYSIOLOGIC Narcolepsy Hypoxic Environmental irritants G...Idiopathic Antithrombin III deficiency Intracranial mass/occipital lobe tumor Protein C deficiency Protein S deficiency Cancer Pregnancy Oral...Table 3. Sources of Emboli (6, 71) Type Patient Age CARDIAC Valves Rheumatic disease Platelet/calcium* Any age Lupus Platelet Young women Acute or

  10. Taste Perception with Age: Generic or Specific Losses in Supra-threshold Intensities of Five Taste Qualities?

    NARCIS (Netherlands)

    Mojet, J.; Heidema, J.; Christ-Hazelhof, E.

    2003-01-01

    The influence of ageing on supra-threshold intensity perception of NaCl, KCl, sucrose, aspartame, acetic acid, citric acid, caffeine, quinine HCl, monosodium glutamate (MSG) and inosine 5'-monophosphate (IMP) dissolved in water and in `regular' product was studied in 21 young (19¿33 years) and 21 el

  11. Applying chemical stimuli on feathers to reduce feather pecking in laying hens

    NARCIS (Netherlands)

    Harlander Matauschek, A.; Rodenburg, T.B.

    2011-01-01

    Recent studies have shown that spraying a distasteful substance (quinine) on a bird's feather cover reduced short-term feather pecking. The present experiment evaluated if other substances offer similar or better protection against feather pecking. One hundred and twenty birds were divided into 12 g

  12. Download this PDF file

    African Journals Online (AJOL)

    ... given before quickening although it is not a disaster if it is administered in error ... pattern of baeteraemia in children with severe malaria; 2) the impact of .... from blood culture and the liquid preparation of quinine for par- enteral use was later ...

  13. Medications and Characteristics of Drugs Causing Ototoxicity.

    Science.gov (United States)

    Pappas, Dennis G.; Pappas, Dennis G., Jr.

    1997-01-01

    This article discusses medications which, by entering the confines of the inner ear, can be toxic and destroy the structures of hearing. Medications that may produce ototoxicity are explained and include aminoglycosides, quinine, salycilates, and diuretics. Factors that should be considered relating to ototoxicity are provided. Contains…

  14. Drug: D08265 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ication [BR:br08303] M MUSCULO-SKELETAL SYSTEM M09 OTHER DRUGS FOR DISORDERS OF THE MUSCULO-SKELETAL... SYSTEM M09A OTHER DRUGS FOR DISORDERS OF THE MUSCULO-SKELETAL SYSTEM M09AA Quinine and d

  15. Sustained and controlled release of lipophilic drugs from a self-assembling amphiphilic peptide hydrogel

    DEFF Research Database (Denmark)

    Briuglia, Maria-Lucia; Urquhart, Andrew; Lamprou, Dimitrios A.

    2014-01-01

    . In this work, we have investigated the diffusion properties of Pindolol, Quinine and Timolol maleate from RADA16 in PBS and in BSS-PLUS at 37°C. A sustained, controlled, reproducible and efficient drug release has been detected for all the systems, which allows to understand the dependence of release kinetics...

  16. Drug: D07153 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available amily) Cinchona bark Major component: Quinine [CPD:C06526] Therapeutic category of drugs... in Japan [BR:br08301] 5 Crude drugs and Chinese medicine formulations 51 Crude drugs 510 Crude drugs 5100 Crude drugs D07153 Cinchona bark PubChem: 51091492 ...

  17. The efficacy of artemether in the treatment of Plasmodium falciparum malaria in Sudan

    DEFF Research Database (Denmark)

    Elhassan, I M; Satti, G H; Ali, A E

    1994-01-01

    The efficacy of artemether (a qinghaosu derivative) administered intramuscularly for the treatment of Plasmodium falciparum malaria was compared to quinine in an open randomized trial including 54 patients in eastern Sudan, where chloroquine resistance is common. The artemether treatment (5 d...

  18. Perception of chloroquine efficacy and alternative treatments for uncomplicated malaria in children in a holoendemic area of Tanzania: implications for the change of treatment policy

    DEFF Research Database (Denmark)

    Tarimo, D S; Minjas, J N; Bygbjerg, I C

    2001-01-01

    and proven CQ failures in first level health facilities and the district hospital. S/P was judged to be more effective than quinine, but too strong for children, and was the least known drug in the study area. All formulations of S/P cost more per dose for a child and an adult than CQ. The implications...

  19. The Role of ABC Proteins in Drug-Resistant Breast Cancer Cells

    Science.gov (United States)

    2007-04-01

    mefloquine (A), quinine (B), chloroquine (C), and verapamil (D) profiles of wildtype (squares, solid line), Dd2 (triangles, dashed line), and 7G8 (circles...Nosten F, and Krishna S. (2004) Mefloquine resistance in Plasmodium falciparum and increased pfmdr1 gene copy number. Lancet 364 438-447. Reed MB

  20. Rational dispensing and use of artemether-lumefantrine during ...

    African Journals Online (AJOL)

    Tanzania Journal of Health Research ... quinine is used in early pregnancy unless the risks outweigh the benefits. The aim of this study was to assess dispensing practice of ALu in private pharmacies and knowledge ... pharmaceutical technicians and 35 (17.5%) sales persons with no formal education on drug dispensing.

  1. Effects of ethanol extract of Cissus quadrangularis on induced ...

    African Journals Online (AJOL)

    aghomotsegin

    2013-10-23

    Oct 23, 2013 ... linings of the stomach of rats pre-treated with the C. quadrangularis extract before induction with ethanol and ... Results from this study suggest that the extract of C, quadrangularis roots possesses antiulcer ... atropine, digoxin, morphine (pain killer), quinine and so ..... selected medicinal plants of Pakistan.

  2. Development and Application of a Method for Toxicological Assessment of Occupational Exposures to Chemicals in Marine Operations. Addendum.

    Science.gov (United States)

    1985-09-01

    protects against hepat- ic necrosis induced by carbon tetrachloride and against acute necrosis of the biliary epithelium following administration of a...retention of bile salts and bilirubin. The jaundice, resulting from retention of bilirubin, resembles that produced by extrahepatic biliary obstruction... ileus bromide Cholinesterase Transient muscle weakness inhibitors N- (pesticides) Magnesium sulfate Central depression and neuromuscular block Quinine

  3. Organocatalytic Asymmetric Domino Michael/Henry Reaction of Indolin-3-ones with o-Formyl-β-nitrostyrenes.

    Science.gov (United States)

    Mahajan, Suruchi; Chauhan, Pankaj; Loh, Charles C J; Uzungelis, Server; Raabe, Gerhard; Enders, Dieter

    2015-04-01

    A highly diastereo- and enantioselective domino Michael/Henry reaction of 1-acetylindolin-3-ones with o-formyl-(E)-β-nitrostyrenes catalyzed by low loading of a quinine-derived amine-squaramide provides the corresponding indolin-3-one derivatives bearing four adjacent stereogenic centers in good to high yields and with excellent stereoselectivities.

  4. Parkinsonism caused by adverse drug reactions: a case series

    Directory of Open Access Journals (Sweden)

    Agaba Emmanuel I

    2011-03-01

    Full Text Available Abstract Introduction Parkinsonism puts a high direct cost burden on both patient and caregiver. Several reports of drug-induced parkinsonism have been published, but to the best of our knowledge, there has not been any report of quinine or halothane inducing parkinsonism. Case presentation We describe two cases of parkinsonism possibly caused by adverse drug reaction to quinine in a 29-year-old black Nigerian woman and to halothane in a 36-year-old black Hausa (Nigerian man who received it as general anaesthesia for appendicectomy in our teaching hospital. Conclusion These are two unusual cases of parkinsonism caused by adverse drug reactions to high-dose quinine and to halothane as general anaesthesia. We consider that these two cases are important in bringing this potential side-effect to the attention of both pharmacologists and primary care physicians as these are two of the most commonly used medications in our clinics. We conclude that parkinsonism should be included among the adverse drug reactions to high-dose quinine and halothane general anaesthetic.

  5. PERCEPTION OF TASTE OF PHENYLTHIOUREA (PTC).

    Science.gov (United States)

    Examining 213 students of the first year at the faculty (3/4 women), 24.88% were found nontasting PTC . The differences between sexes are not...represented. With a quinine control test among nontasting, a small correlation to PTC was established. The results are in agreement with literature data. (Author)

  6. No de novo sulforaphane biosynthesis in broccoli seedlings

    NARCIS (Netherlands)

    Gorissen, Antonie; Kraut, Nicolai U.; de Visser, Ries; de Vries, Marcel; Roelofsen, Han; Vonk, Roel J.

    2011-01-01

    The isothiocyanate sulforaphane, present in significant amounts in broccoli (Brassica oleracea L.) seedlings in the form of its precursor glucoraphanin, has been identified as an inducer of quinine reductase, a phase-II detoxification enzyme known for its anticarcinogenic properties. Its

  7. Science in the service of colonial agro-industrialism : the case of cinchona cultivation in the Dutch and British East Indies, 1852-1900

    NARCIS (Netherlands)

    Roersch van der Hoogte, Arjo|info:eu-repo/dai/nl/31503274X; Pieters, Toine|info:eu-repo/dai/nl/188785833

    2014-01-01

    The isolation of quinine from cinchona bark in 1820 opened new possibilities for the mass-production and consumption of a popular medicine that was suitable for the treatment of intermittent (malarial) fevers and other diseases. As the 19th century European empires expanded in Africa and Asia, contr

  8. The Chemical Constituents and Pharmacological Effects of Bryophyllum calycinum. A review

    OpenAIRE

    Ali Esmail Al-Snafi

    2014-01-01

    Bryophyllum calycinum belongs to the family crassulaceae was widely used in traditional medicine especially in the tropical areas. The plant contained alkaloids, phenols, flavonoids, tannins, anthocyanins, glycosides, bufadienolides, saponins, coumarins, sitosterols, quinines, carotenoids, tocopherol and lectins . The previous pharmacological studies showed that it exerted many pharmacological effects including anticancer , antioxidant immunomodulating , antibacterial , anthelmentic , antipro...

  9. Safety and efficacy of iron supplementation in pregnant Kenyan women

    NARCIS (Netherlands)

    Mwangi, M.N.

    2014-01-01

    Since the British doctor Ronald Ross received the 1902 Nobel Prize in medicine for his work on malaria, more people have died from the disease than all world wars combined. This is in spite of the fact that the French chemists Pierre Joseph Pelletier and Joseph Bienaimé Caventou made quinine

  10. Synthesis and Evaluation of Strychnos Alkaloids as MDR Reversal Agents for Cancer Cell Eradication

    Science.gov (United States)

    2014-01-01

    quinine in combination with chemotherapy showed an increase in complete remission rates and patient survival in Pgp- positive MDS cases.8 The low...Glide’s XS docking protocol. Two cyclic peptide inhibitors (QZ59-SSS and QZ59-RRR) that were previously co-crystallized with mouse Pgp (Aller et al. Science

  11. The neural encoding of cocaine-induced devaluation in the ventral pallidum.

    Science.gov (United States)

    Chan, Chung-Lung; Wheeler, Daniel S; Wheeler, Robert A

    2016-04-01

    Cocaine experience affects motivation structures such as the nucleus accumbens (NAc) and its major output target, the ventral pallidum (VP). Previous studies demonstrated that both NAc activity and hedonic responses change reliably as a taste cue comes to predict cocaine availability. Here we extended this investigation to examine drug-experience induced changes in hedonic encoding in the VP. VP activity was first characterized in adult male Sprague-Dawley rats in response to intraoral infusions of palatable saccharin and unpalatable quinine solutions. Next, rats received 7 daily pairings of saccharin that predicted either a cocaine (20mg/kg, ip) or saline injection. Finally, the responses to saccharin and quinine were again assessed. Of 109 units recorded in 11 rats that received saccharin-cocaine pairings, 71% of responsive units significantly reduced firing rate during saccharin infusions and 64% increased firing rate during quinine exposure. However, as saccharin came to predict cocaine, and elicited aversive taste reactivity, VP responses changed to resemble quinine. After conditioning, 70% of saccharin-responsive units increased firing rate. Most units that encoded the palatable taste (predominantly reduced firing rate) were located in the anterior VP, while most units that were responsive to aversive tastes were located in the posterior VP. This study reveals an anatomical complexity to the nature of hedonic encoding in the VP.

  12. Electrophysiological responses of gustatory receptor neurons on the labella of the common malaria mosquito Anopheles quadrimaculatus Say (Diptera: Culicidae)

    Science.gov (United States)

    We recorded electrical responses from sensory cells associated with gustatory sensilla on the labella of female Anopheles quadrimaculatus to salt, sucrose, quinine (a feeding deterrent) and the insect repellent, N,N-diethyl-3-methylbenzamide (DEET). A salt-sensitive cell responded to increasing con...

  13. Reprint of "Characterisation and modelling of the thermorheological properties of pharmaceutical polymers and their blends using capillary rheometry: Implications for hot melt processing of dosage forms".

    Science.gov (United States)

    Jones, David S; Margetson, Daniel N; McAllister, Mark S; Andrews, Gavin P

    2015-12-30

    Given the growing interest in thermal processing methods, this study describes the use of an advanced rheological technique, capillary rheometry, to accurately determine the thermorheological properties of two pharmaceutical polymers, Eudragit E100 (E100) and hydroxypropylcellulose JF (HPC) and their blends, both in the presence and absence of a model therapeutic agent (quinine, as the base and hydrochloride salt). Furthermore, the glass transition temperatures (Tg) of the cooled extrudates produced using capillary rheometry were characterised using Dynamic Mechanical Thermal Analysis (DMTA) thereby enabling correlations to be drawn between the information derived from capillary rheometry and the glass transition properties of the extrudates. The shear viscosities of E100 and HPC (and their blends) decreased as functions of increasing temperature and shear rates, with the shear viscosity of E100 being significantly greater than that of HPC at all temperatures and shear rates. All platforms were readily processed at shear rates relevant to extrusion (approximately 200-300s(-1)) and injection moulding (approximately 900s(-1)). Quinine base was observed to lower the shear viscosities of E100 and E100/HPC blends during processing and the Tg of extrudates, indicative of plasticisation at processing temperatures and when cooled (i.e. in the solid state). Quinine hydrochloride (20% w/w) increased the shear viscosities of E100 and HPC and their blends during processing and did not affect the Tg of the parent polymer. However, the shear viscosities of these systems were not prohibitive to processing at shear rates relevant to extrusion and injection moulding. As the ratio of E100:HPC increased within the polymer blends the effects of quinine base on the lowering of both shear viscosity and Tg of the polymer blends increased, reflecting the greater solubility of quinine within E100. In conclusion, this study has highlighted the importance of capillary rheometry in

  14. Characterisation and modelling of the thermorheological properties of pharmaceutical polymers and their blends using capillary rheometry: Implications for hot melt processing of dosage forms.

    Science.gov (United States)

    Jones, David S; Margetson, Daniel N; McAllister, Mark S; Andrews, Gavin P

    2015-09-30

    Given the growing interest in thermal processing methods, this study describes the use of an advanced rheological technique, capillary rheometry, to accurately determine the thermorheological properties of two pharmaceutical polymers, Eudragit E100 (E100) and hydroxypropylcellulose JF (HPC) and their blends, both in the presence and absence of a model therapeutic agent (quinine, as the base and hydrochloride salt). Furthermore, the glass transition temperatures (Tg) of the cooled extrudates produced using capillary rheometry were characterised using Dynamic Mechanical Thermal Analysis (DMTA) thereby enabling correlations to be drawn between the information derived from capillary rheometry and the glass transition properties of the extrudates. The shear viscosities of E100 and HPC (and their blends) decreased as functions of increasing temperature and shear rates, with the shear viscosity of E100 being significantly greater than that of HPC at all temperatures and shear rates. All platforms were readily processed at shear rates relevant to extrusion (approximately 200-300 s(-1)) and injection moulding (approximately 900 s(-1)). Quinine base was observed to lower the shear viscosities of E100 and E100/HPC blends during processing and the Tg of extrudates, indicative of plasticisation at processing temperatures and when cooled (i.e. in the solid state). Quinine hydrochloride (20% w/w) increased the shear viscosities of E100 and HPC and their blends during processing and did not affect the Tg of the parent polymer. However, the shear viscosities of these systems were not prohibitive to processing at shear rates relevant to extrusion and injection moulding. As the ratio of E100:HPC increased within the polymer blends the effects of quinine base on the lowering of both shear viscosity and Tg of the polymer blends increased, reflecting the greater solubility of quinine within E100. In conclusion, this study has highlighted the importance of capillary rheometry in

  15. Aversive reinforcement improves visual discrimination learning in free-flying honeybees.

    Directory of Open Access Journals (Sweden)

    Aurore Avarguès-Weber

    Full Text Available BACKGROUND: Learning and perception of visual stimuli by free-flying honeybees has been shown to vary dramatically depending on the way insects are trained. Fine color discrimination is achieved when both a target and a distractor are present during training (differential conditioning, whilst if the same target is learnt in isolation (absolute conditioning, discrimination is coarse and limited to perceptually dissimilar alternatives. Another way to potentially enhance discrimination is to increase the penalty associated with the distractor. Here we studied whether coupling the distractor with a highly concentrated quinine solution improves color discrimination of both similar and dissimilar colors by free-flying honeybees. As we assumed that quinine acts as an aversive stimulus, we analyzed whether aversion, if any, is based on an aversive sensory input at the gustatory level or on a post-ingestional malaise following quinine feeding. METHODOLOGY/PRINCIPAL FINDINGS: We show that the presence of a highly concentrated quinine solution (60 mM acts as an aversive reinforcer promoting rejection of the target associated with it, and improving discrimination of perceptually similar stimuli but not of dissimilar stimuli. Free-flying bees did not use remote cues to detect the presence of quinine solution; the aversive effect exerted by this substance was mediated via a gustatory input, i.e. via a distasteful sensory experience, rather than via a post-ingestional malaise. CONCLUSION: The present study supports the hypothesis that aversion conditioning is important for understanding how and what animals perceive and learn. By using this form of conditioning coupled with appetitive conditioning in the framework of a differential conditioning procedure, it is possible to uncover discrimination capabilities that may remain otherwise unsuspected. We show, therefore, that visual discrimination is not an absolute phenomenon but can be modulated by experience.

  16. Reduced in vitro susceptibility to artemisinin derivatives associated with multi-resistance in a traveller returning from South-East Asia

    Directory of Open Access Journals (Sweden)

    Bertaux Lionel

    2011-09-01

    Full Text Available Abstract Decreased in vitro susceptibility to dihydroartemisinin (21.2 nM and artesunate (16.3 nM associated with decreased susceptibility or resistance to quinine (1131 nM, mefloquine (166 nM, lumefantrine (114 nM, pyronaridine (70.5 nM and piperaquine (91.1 nM is reported in a patient returning from South-East Asia after trekking along the Mekong from the south of Laos to the north of Thailand. Decreased in vitro susceptibility to artemisinin derivatives did not appear to be mediated by the number of copies of pfmdr1 or pfATPase6, pfcrt, pfmdr1 or pfmrp polymorphism. The high IC50 to mefloquine of this Asian isolate was not associated with pfmdr1 copy number. Pfnhe-1 microsatellite ms4760 showed a profile 7 (ms4760-7 with three repeats of DNNND and one repeat of DDDNHNDNHNN, which is associated with high quinine reduced susceptibility. The patient recovered in three days without relapse after treatment with the association of quinine and doxycycline. Decreased in vitro susceptibility to quinine and the delayed effect of doxycycline may both have contributed to the delayed parasite clearance time, D4 (0.5% and D7 (0.004%. The in vitro data, with IC50 for dihydroartemisinin and artesunate were up to ten times those of the reference clone W2, which suggests that this isolate may be resistant to artemisinin derivatives, associated with a decreased susceptibility to quinine.

  17. Taste masking analysis in pharmaceutical formulation development using an electronic tongue.

    Science.gov (United States)

    Zheng, Jack Y; Keeney, Melissa P

    2006-03-09

    The purpose of this study is to assess the feasibility for taste masking and comparison of taste intensity during formulation development using a multichannel taste sensor system (e-Tongue). Seven taste sensors used in the e-Tongue were cross-selective for five basic tastes while having different sensitivity or responsibility for different tastes. Each of the individual sensors concurrently contributes to the detection of most substances in a complicated sample through the different electronic output. Taste-masking efficiency was evaluated using quinine as a bitter model compound and a sweetener, acesulfame K, as a bitterness inhibitor. In a 0.2 mM quinine solution, the group distance obtained from e-Tongue analysis was reduced with increasing concentration of acesulfame K. This result suggests that the sensors could detect the inhibition of bitterness by a sweetener and could be used for optimization of the sweetener level in a liquid formulation. In addition, the bitterness inhibition of quinine by using other known taste-masking excipients including sodium acetate, NaCl, Prosweet flavor, and Debittering powder or soft drinks could be detected by the e-Tongue. These results further suggest that the e-Tongue should be useful in a taste-masking evaluation study on selecting appropriate taste-masking excipients for a solution formulation or a reconstitution vehicle for a drug-in-bottle formulation. In another study, the intensity of the taste for several drug substances known to be bitter was compared using the e-Tongue. It was found that the group distance was 695 for prednisolone and 686 for quinine, which is much higher than that of caffeine (102). These results indicate that the taste of prednisolone and quinine is stronger or more bitter than that of caffeine as expected. Based on the group distance, the relative intensity of bitterness for these compounds could be ranked in the following order: ranitidine HCl>prednisolone Na>quinine HCl approximately

  18. HIPOGLIKEMIA PADA SEORANG PENDERITA MALARIA

    Directory of Open Access Journals (Sweden)

    P. N. Harianto

    2012-09-01

    Full Text Available Hypoglycemia is a serious and often fatal complication of severe malaria. This condition has been reported in many parts of the world including from Thailand (1983 and from Indonesia by Hoffman (1988 and Harianto (1990. Two main causes that can lead to development of this condition are quinine administration and the severity of the malaria condition itself. A case study is presented about development of prolonged hypoglycemia after quinine administration. A 41 years old male was hospitalized with 4 days history of fever, headache vomiting and icterus. On examination he was found to be in good mental status, had a normal blood pressure, and a body temperature of 40°C. He also had icterus and hepatomegaly. Laboratory examination on admission showed malaria slide positive forRfalciparum ring 30-40, with parasite count of 3% (+ on day I. CBC showed: WBC of 21,700/mm3 and platelet count of 40,000/mm3. Blood chemistry showed glucose level of 77 mm %, serum bilirubin of 29.34 mg % (direct 21.87 mg % SGOT 31 u/l, SGPT 20 u/l, serum ureum 167 mg %, creatinine of 3.36 mg %, serum Na 123 m Eq/L and K 3.99 Eq/L. Urinalysis was normal except for specific gravity of 1.07. After diagnosis of bilious malaria was confirmed, the patient was given i.v. quinine 500 mg diluted in 500 ml 5% dextrose, infused over 4 hours and repeated every 8 hours. On day IVi.v. quinine was switched to oral preparation of 600 mg given bid and the next day quinine was changed to oral chloroquine. The day after admission (30 hours after quinine administration, blood glucose dropped to 21 mg %, 16-46 mg % on day III, and to less than 10 mg % on day IV. It gradulty returned to normal afterwards. Administration of 10% dextrose and boluses of 40% glucose were able to keep the patient in good clinical condition and prevent death. Malaria slide improved on day III, became negative by day IV and serum bilirubin also decreased on follow up. Hypoglycemia should be expected in severe malaria

  19. In vitro evaluation of drug susceptibilities of Babesia divergens isolates.

    Science.gov (United States)

    Brasseur, P; Lecoublet, S; Kapel, N; Favennec, L; Ballet, J J

    1998-04-01

    The susceptibilities of three bovine and two human Babesia divergens isolates to antimicrobial agents were evaluated in vitro by a tritiated hypoxanthine incorporation assay. The MICs at which 50% of isolates are inhibited (MIC50s) for mefloquine (chlorhydrate), chloroquine (sulfate), quinine (chlorhydrate), clindamycin (phosphate), pentamidine (isethionate), phenamidine (isethionate) plus oxomemazine (chlorhydrate), lincomycin (chlorhydrate monohydrate), and imidocarb (dipropionate) were determined. Except for imidocarb, the MIC50s observed for the different isolates were close. Imidocarb and the combination of phenamidine plus oxomemazine exhibited the highest in vitro activity, while antimalarial agents such as mefloquine, choroquine, and quinine were inactive. Other drugs had intermediate activities. The data support further in vitro evaluation of antimicrobial agents active against B. divergens for the improvement of therapeutic strategies.

  20. Stimulus preexposure reduces generalization of conditioned taste aversions between alcohol and non-alcohol flavors in infant rats.

    Science.gov (United States)

    Chotro, M Gabriela; Alonso, Gumersinda

    2003-02-01

    Results of 3 experiments showed that infant rats (age 13-17 days) generalize conditioned taste aversions between alcohol and non-alcohol tastes such as a mixture of sucrose and quinine, apple cider vinegar, or coffee. Nonreinforced preexposure to those tastes reduced generalized aversions between them. Generalization between alcohol and sucrose-quinine was reduced not only after preexposure to both tastes, but also when only the nonconditioned taste was preexposed, whereas with alcohol and vinegar, both tastes had to be preexposed to obtain that effect. In no case was generalization reduced when only the to-be-conditioned taste was preexposed. Previous experience with alcohol alone, as well as with similar gustatory stimuli, may enhance subjects' ability to differentiate them during infantile stages in rats.

  1. Complex Membrane Channel Blockade: A Unifying Hypothesis for the Prodromal and Acute Neuropsychiatric Sequelae Resulting from Exposure to the Antimalarial Drug Mefloquine

    Directory of Open Access Journals (Sweden)

    Jane C. Quinn

    2015-01-01

    Full Text Available The alkaloid toxin quinine and its derivative compounds have been used for many centuries as effective medications for the prevention and treatment of malaria. More recently, synthetic derivatives, such as the quinoline derivative mefloquine (bis(trifluoromethyl-(2-piperidyl-4-quinolinemethanol, have been widely used to combat disease caused by chloroquine-resistant strains of the malaria parasite, Plasmodium falciparum. However, the parent compound quinine, as well as its more recent counterparts, suffers from an incidence of adverse neuropsychiatric side effects ranging from mild mood disturbances and anxiety to hallucinations, seizures, and psychosis. This review considers how the pharmacology, cellular neurobiology, and membrane channel kinetics of mefloquine could lead to the significant and sometimes life-threatening neurotoxicity associated with mefloquine exposure. A key role for mefloquine blockade of ATP-sensitive potassium channels and connexins in the substantia nigra is considered as a unifying hypothesis for the pathogenesis of severe neuropsychiatric events after mefloquine exposure in humans.

  2. [Historical overview of antimalarials used in Venezuela].

    Science.gov (United States)

    Zerpa de Artiles, N

    1993-06-01

    A historical review of antimalarials used in Venezuela is presented from the time when the bark of quina was used until the massive distribution of quinine and metoquine by the Dirección de Malariología y Saneamiento Ambiental. The utility of chloroquine and primaquine against sensible parasite isolates and of sulfadoxine-pyrimethamine and quinine, currently used against P. falciparum resistant strains, is thoroughly discussed. The author suggests use of artemisimine and its derivatives as a very promising antimalarial drug. She also stresses the possibility of the application of new antimalaria vaccine against P. falciparum blood states, presently assayed in the country as an additional tool in malaria control programs.

  3. Resolution pattern of jaundice among children presenting with severe malaria in rural South-West Nigeria

    Institute of Scientific and Technical Information of China (English)

    Osonuga OA; Osonuga A; Osonuga AA; Osonuga IO

    2012-01-01

    Objective:To compare the pattern of jaundice resolution among children with severe malaria treated with quinine and artemether. Methods: Thirty two children who fulfilled the inclusion criteria were recruited for the study from two hospitals with intensive care facilities. They were divided into two groups;‘Q’ and‘A’, receiving quinine and artemether, respectively. Jaundice was assessed by clinical examination. Results:Sixteen out of 32 children recruited (representing 50%) presented with jaundice on the day of recruitment. The mean age was (7.00±2.56) years. On day 3, four patients in‘A’ and six patients in‘Q’ had jaundice. By day 7, no child had jaundice. Conclusion:The study has shown that both drugs resolve jaundice although artemether relatively resolves it faster by the third day.

  4. Salts of phenylacetic acid and 4-hydroxyphenylacetic acid with Cinchona alkaloids: Crystal structures, thermal analysis and FTIR spectroscopy

    Science.gov (United States)

    Amombo Noa, Francoise M.; Jacobs, Ayesha

    2016-06-01

    Seven salts were formed with phenylacetic acid (PAA), 4-hydroxyphenylacetic acid (HPAA) and the Cinchona alkaloids; cinchonidine (CIND), quinidine (QUID) and quinine (QUIN). For all the structures the proton was transferred from the carboxylic acid of the PAA/HPAA to the quinuclidine nitrogen of the respective Cinchona alkaloid. For six of the salts, water was included in the crystal structures with one of these also incorporating an isopropanol solvent molecule. However HPAA co-crystallised with quinine to form an anhydrous salt, (HPAA-)(QUIN+). The thermal stability of the salts were determined and differential scanning calorimetry revealed that the (HPAA-)(QUIN+) salt had the highest thermal stability compared to the other salt hydrates. The salts were also characterized using Fourier transform infrared spectroscopy. (PAA-)(QUID+)·H2O and (PAA-)(QUIN+)·H2O are isostructural and Hirshfeld surface analysis was completed to compare the intermolecular interactions in these two structures.

  5. Peripheral nervous control of cold-induced reduction in the respiratory quotient of the rat

    Science.gov (United States)

    Refinetti, Roberto

    1990-03-01

    Cold-exposed rats show a reduction in the respiratory quotient which is indicative of a relative shift from carbohydrates to lipids as substrates for oxidative metabolism. In the present study, the effects of food deprivation and cold exposure on the respiratory quotient were observed. In addition, the involvement of the three main branches of the peripheral nervous system (sympathetic, parasympathetic, and somatic) was investigated by means of synaptic blockade with propranolol, atropine, and quinine, respectively. Both propranolol and quinine blocked the cold-induced decrease in respiratory quotient and increase in heat production, whereas atropine had only minor and very brief effects. It is concluded that both the sympathetic and somatic branches are involved in the metabolic changes associated with cold-induced thermogenesis and that the increase in metabolic heat production involves a shift from carbohydrate to lipid utilization irrespective of which of the two branches is activated.

  6. Curare: the South American arrow poison.

    Science.gov (United States)

    Lee, M R

    2005-02-01

    The history of curare is both curious and convoluted. A product of South American culture it emerged in the sixteenth century from the mists of antiquity at the same time as quinine, coca, and chocolate. Like quinine, at first came the extract but no plant, and later the plant but no chemical compound. It took more than 300 years and the efforts of many explorers and scientists to resolve the problem. These included Condamine, Humboldt, Brodie, Waterton, Bernard, Dale, Walker, and King. Finally, the pure compound d-tubocurarine was isolated from the liana Chondrodendron and synthesised. Its specific physiological action was blockade of the effect of acetylcholine at the neuro-muscular junction. Such a paralytic poison could be used to kill oneself or others. The bizarre plot to kill the Prime Minister, Lloyd George, during the First World War is described. Fortunately this nefarious plan was thwarted by the Secret Service!

  7. Hedonic and sensory characteristics of odors conditioned by pairing with tastants in humans.

    Science.gov (United States)

    Yeomans, Martin R; Mobini, Sirous; Elliman, Toby D; Walker, Helen C; Stevenson, Richard J

    2006-07-01

    Animals readily acquire positive odor-taste hedonic associations, but evidence for this in humans remains weak and was explored further. Retronasal pairing of odors with sucrose or salty stimuli (Experiment 1) increased the rated sweetness of sucrose-paired odors without altering liking, although changes in odor pleasantness correlated with sucrose liking. Experience of odors with sucrose or quinine by sweet likers (Experiment 2) found increased pleasantness and sweetness for sucrose-paired odors, whereas quinine-paired odors became less liked and more bitter. Odor-sucrose pairings in sweet likers and dislikers (Experiment 3) found increased sweetness in both groups but increased odor liking only in likers. These data suggest that evaluative and sensory learning are dissociable and that evaluative changes are sensitive to individual differences in sweet liking.

  8. Hunger alters the expression of acquired hedonic but not sensory qualities of food-paired odors in humans.

    Science.gov (United States)

    Yeomans, Martin R; Mobini, Sirous

    2006-10-01

    To test whether expression of hedonic and sensory odor qualities acquired by association with sweet and bitter tastes depend on hunger state, hungry volunteers experienced odors paired with sucrose, quinine, or water and then were tested under different hunger states manipulated with energy preloads. Acquired liking for sucrose-paired odors was evident following a low-energy or control preload but not a high-energy preload; however, odor sweetness increased in all preload conditions. Acquired dislike and increased bitterness of quinine-paired odors were independent of preloading. These data demonstrate hunger-dependent expression of acquired liking for flavors through flavor-flavor associations in humans and demonstrate independence between acquired hedonic and sensory qualities of odors. Copyright 2006 APA.

  9. Polymorphism of the Plasmodium falciparum multidrug resistance and chloroquine resistance transporter genes and in vitro susceptibility to aminoquinolines in isolates from the Peruvian Amazon.

    Science.gov (United States)

    Huaman, Maria Cecilia; Roncal, Norma; Nakazawa, Shusuke; Long, Ton That Ai; Gerena, Lucia; Garcia, Coralith; Solari, Lely; Magill, Alan J; Kanbara, Hiroji

    2004-05-01

    In vitro drug sensitivity to chloroquine (CQ), mefloquine (MQ) and quinine was investigated in 60 culture-adapted Plasmodium falciparum isolates from malaria patients in Padrecocha, a village in the Amazonian Department of Loreto, Peru. All isolates showed resistance to CQ, decreased susceptibility to quinine, and sensitivity to MQ. These isolates were examined for mutations in the P. falciparum multidrug resistance 1 (pfmdr1) and chloroquine resistance transporter (pfcrt) genes previously linked to CQ resistance. The mutations N86Y and D1246Y, two of the five mutations commonly observed in the pfmdr1 gene of CQ-resistant clones, were not found. The pfcrt mutation K76T, associated with CQ resistance, was identified in all the isolates tested. Sequence analysis of codons 72-76 in the pfcrt gene showed the haplotypes SVMNT and CVMNT.

  10. A comparison of the antimalarial activity of the cinchona alkaloids against Plasmodium falciparum in vitro.

    Science.gov (United States)

    Wesche, D L; Black, J

    1990-06-01

    The effects of four major cinchona alkaloids: (-) quinine, (+) quinidine, (-)cinchonidine, and (+)cinchonine against Plasmodium falciparum FCQ-27/PNG were studied. The alkaloids were tested in vitro as either single alkaloids, racemic mixtures of stereoisomers, or as an equimolar combination of all four alkaloids. Results indicate (+)quinidine to be most effective and both (+)stereoisomers were more potent than the (-)stereoisomers. Inhibitory concentrations 50% (Ki) of racemic mixtures of stereoisomers were similar to those of the (+)stereoisomers alone. The Ki of four alkaloids in equimolar combination were similar to that of the (-) cinchonidine/(+)cinchonine racemic mixture. A total alkaloidal extract of Cinchona sp. was tested and compared with the pure alkaloids. HPLC analysis indicated that (+)cinchonine, (-)cinchonidine and (-)quinine were present in a ratio of approximately 1:1:2, respectively. The total alkaloid extract, with (-)stereoisomers predominating, was less effective than the four alkaloids in combination. The nature of the interaction between stereoisomers was investigated and appears to be one of addition.

  11. Protective efficacy of malaria case management and intermittent preventive treatment for preventing malaria mortality in children: a systematic review for the Lives Saved Tool

    Directory of Open Access Journals (Sweden)

    Steketee Richard W

    2011-04-01

    Full Text Available Abstract Background The Lives Saved Tool (LiST model was developed to estimate the impact of the scale-up of child survival interventions on child mortality. New advances in antimalarials have improved their efficacy of treating uncomplicated and severe malaria. Artemisinin-based combination therapies (ACTs for uncomplicated Plasmodium falciparum malaria and parenteral or rectal artemisinin or quinine for severe malaria syndromes have been shown to be very effective for the treatment of malaria in children. These interventions are now being considered for inclusion in the LiST model. However, for obvious ethical reasons, their protective efficacy (PE compared to placebo is unknown and their impact on reducing malaria-attributable mortality has not been quantified. Methods We performed systematic literature reviews of published studies in P. falciparum endemic settings to determine the protective efficacy (PE of ACT treatment against malaria deaths among children with uncomplicated malaria, as well as the PE of effective case management including parenteral quinine against malaria deaths among all hospitalized children. As no randomized placebo-controlled trials of malaria treatment have been conducted, we used multiple data sources to ascertain estimates of PE, including a previously performed Delphi estimate for treatment of uncomplicated malaria. Results Based on multiple data sources, we estimate the PE of ACT treatment of uncomplicated P. falciparum malaria on reducing malaria mortality in children 1–23 months to be 99% (range: 94-100%, and in children 24-59 months to be 97% (range: 86-99%. We estimate the PE of treatment of severe P. falciparum malaria with effective case management including intravenous quinine on reducing malaria mortality in children 1-59 months to be 82% (range: 63-94% compared to no treatment. Conclusions This systematic review quantifies the PE of ACT used for treating uncomplicated malaria and effective case

  12. Total Synthesis of ( - )-Kaerophyllin, ( - )-Hinokinin and (±)-Iso-hinokinin

    Institute of Scientific and Technical Information of China (English)

    夏亚穆; 梁其任; 王小龙; 曹小平; 潘鑫复

    2003-01-01

    A convenient and rapid approach for the syntheses of (-)-kaerophyllin (1), (-)-hinokinin (2) and (±)-isohinokinin (3) was described. The key steps were involved in condensation of aromatic aldehyde and alkylation of the resulting ester to give the complete skeleton of dibenzylbutyrolactone-lignan. Hydrolysis, followed by resolution with quinine, reduction and when appropriate, oxidation gave the title compound. The asynunetric total synthesis of the kaerophyllin (1) was reported for the first tlme.

  13. Interactions of mefloquine with ABC proteins, MRP1 (ABCC1) and MRP4 (ABCC4), that are present in human red cell membranes

    OpenAIRE

    Wu, Chung-Pu; Klokouzas, Antonios; Hladky, Stephen B.; Ambudkar, Suresh V.; Barrand, Margery A.

    2005-01-01

    Human erythrocyte membranes express the multidrug resistance-associated proteins, MRP1, MRP4 and MRP5, that collectively can efflux oxidised glutathione, glutathione conjugates and cyclic nucleotides. It is already known that the quinoline derivative, MK-571, is a potent inhibitor of MRP-mediated transport. We here examine whether the quinoline-based antimalarial drugs, amodiaquine, chloroquine, mefloquine, primaquine, quinidine and quinine, also interact with erythrocyte MRPs with consequenc...

  14. Treatment of African children with severe malaria - towards evidence-informed clinical practice using GRADE

    Directory of Open Access Journals (Sweden)

    English Mike

    2011-07-01

    Full Text Available Abstract Background Severe malaria is a major contributor of deaths in African children up to five years of age. One valuable tool to support health workers in the management of diseases is clinical practice guidelines (CPGs developed using robust methods. A critical assessment of the World Health Organization (WHO and Kenyan paediatric malaria treatment guidelines with quinine was undertaken, with a focus on the quality of the evidence and transparency of the shift from evidence to recommendations. Methods Systematic reviews of the literature were conducted using the Grading of Recommendations Assessment, Development and Evaluation (GRADE tool to appraise included studies. The findings were used to evaluate the WHO and Kenyan recommendations for the management of severe childhood malaria. Results The WHO 2010 malaria guidance on severe malaria in children, which informed the Kenyan guidelines, only evaluated the evidence on one topic on paediatric care using the GRADE tool. Using the GRADE tool, this work explicitly demonstrated that despite the established use of quinine in the management of paediatric cases of severe malaria for decades, low or very low quality evidence of important outcomes, but not critical outcomes such as mortality, have informed national and international guidance on the paediatric quinine dosing, route of administration and adverse effects. Conclusions Despite the foreseeable shift to artesunate as the primary drug for treatment of severe childhood malaria, the findings reported here reflect that the particulars of quinine therapeutics for the management of severe malaria in African children have historically been a neglected research priority. This work supports the application of the GRADE tool to make transparent recommendations and to inform advocacy efforts for a greater research focus in priority areas in paediatric care in Africa and other low-income settings.

  15. Food Consumption, Restraint, and Stress

    Science.gov (United States)

    1989-09-05

    the cover story of the experiment. Each subject consumed two caramels , a cup of hot bouillon soup, two dried apricots, an ounce of quinine water...subject viewed several objects (including the nuts ) and were asked to think about and feel free to touch, feel, or doodle with the toys, or eat the...manipulation of anxiety were correlated with eating salty nuts , a significant negative correlation was 13 I, . ~ :’ 14 revealed for normal weight

  16. Asymmetric Synthesis of Highly Functionalized Tetrahydropyrans via a One-Pot Organocatalytic Michael/Henry/Ketalization Sequence

    Science.gov (United States)

    Hahn, Robert; Raabe, Gerhard; Enders, Dieter

    2015-01-01

    A diastereo- and enantioselective Michael/Henry/ketalization sequence to functionalized tetrahydropyrans is described. The multicomponent cascade reaction uses acetylacetone or β-keto esters, β-nitrostyrenes, and alkynyl aldehydes as substrates affording tetrahydropyrans with five contiguous stereocenters. Employing a bifunctional quinine-based squaramide organocatalyst, the title compounds are obtained in moderate to good yields (27–80%), excellent enantiomeric excesses (93–99% ee), and high diastereomeric ratios (dr > 20:1) after one crystallization. PMID:24971998

  17. Synthesis of triazol derivatives of lupeol with potential antimalarial activity

    OpenAIRE

    Tatiane Freitas Borgati; Guilherme Rocha Pereira; Geraldo Célio Brandão; Alaíde Braga Oliveira; José Dias Souza Filho

    2012-01-01

    The goal of this project is synthesize and characterization of derivatives of lupeol and evaluated antimalarial activity. Historically, plants are important source of antimalarial medicines, highlighting quinine (1) (Figure 1), an important      alkaloid from the Cinchona calisaya bark. This compound was an important model for cloroquine  synthesis, a drug that was widely used in malaria treatment. In addition, one of the principal medicines used today is artemisinine, isolated from the Chine...

  18. Polymorphisms of the oxidant enzymes glutathione S-transferase and glutathione reductase and their association with resistance ofPlasmodium falciparum isolates to antimalarial drugs

    Institute of Scientific and Technical Information of China (English)

    Raewadee Wisedpanichkij; Wanna Chaicharoenkul; Poonuch Mahamad; Prapichaya Prompradit; Kesara Na-Bangchang

    2010-01-01

    Objective:To investigate the association between amplification of the two regulatory genes controlling glutathione(GSH)levels, glutathione reductase(PfGR)and glutathione S-transferase (PfGST) genes and sensitivity ofPlasmodium falciparum (P. falciparum)isolates collected from different malaria endemic areas of Thailand to standard antimalarial drugs.Methods: A total of70P. falciparum isolates were collected from endemic areas of multi-drug resistance (Tak, Chantaburi and Ranong Provinces) during the year2008-2009. The in vitro assessment of antimalarial activity ofP. falciparumclones (K1- and Dd2 chloroquine resistant and3D7-chloroquine sensitive) and isolates to chloroquine, quinine, mefloquine and arteusnate was performed based onSYBR Green modified assay.Results:68 (97.14%), 11 (15.71%) and28 (40%) isolates respectively were classified as chloroquine-, quinine- and mefloquine-resistant isolates. With this limited number ofP. falciparum isolates included in the analysis, no significant association between amplification ofPfGST gene and sensitivity of the parasite to chloroquine, quinine, mefloquine and quinine was found. Based onPCR analysis,Dd2, K1 and3D7clones all contained only one copy of thePfGST gene. All isolates (70) also carried only one copy number of PfGST gene. There appears to be an association between amplification ofPfGR gene and chloroquine resistance. The3D7and Dd2 clones were found to carry only onePfGR gene copy, whereas the K1 clone carried two gene copies.Conclusions: Chloroquine resistance is likely to be a consequence of multi-factors and enzymes in theGSH system may be partly involved. Larger number of parasite isolates are required to increase power of the hypothesis testing in order to confirm the involvement of both genes as well as other genes implicated in glutathione metabolism in conferring chloroquine resistance.

  19. Analysis of Investigational Drugs in Biological Fluids. Method Development and Routine Assay. Appendix A.

    Science.gov (United States)

    2007-11-02

    simultaneously on eleven projects (I-WR 238,605, 2-halofantrine (and its metabolite), 3-WR 6026 (and its metabolites), 4- mefloquine (and its metabolite), 5...chloroquine (and its metabolites), and 11-a multiple drug interaction study in dog plasma for WR 238,605, mefloquine , chloroquine, quinine,, doxycycline...245 Study Report 18, WR 6026 in Plasma ................................................................ 259 Study Report 19, Mefloquine (Free Base

  20. Fetal alcohol exposure reduces responsiveness of taste nerves and trigeminal chemosensory neurons to ethanol and its flavor components.

    Science.gov (United States)

    Glendinning, John I; Tang, Joyce; Morales Allende, Ana Paula; Bryant, Bruce P; Youngentob, Lisa; Youngentob, Steven L

    2017-08-01

    Fetal alcohol exposure (FAE) leads to increased intake of ethanol in adolescent rats and humans. We asked whether these behavioral changes may be mediated in part by changes in responsiveness of the peripheral taste and oral trigeminal systems. We exposed the experimental rats to ethanol in utero by administering ethanol to dams through a liquid diet; we exposed the control rats to an isocaloric and isonutritive liquid diet. To assess taste responsiveness, we recorded responses of the chorda tympani (CT) and glossopharyngeal (GL) nerves to lingual stimulation with ethanol, quinine, sucrose, and NaCl. To assess trigeminal responsiveness, we measured changes in calcium levels of isolated trigeminal ganglion (TG) neurons during stimulation with ethanol, capsaicin, mustard oil, and KCl. Compared with adolescent control rats, the adolescent experimental rats exhibited diminished CT nerve responses to ethanol, quinine, and sucrose and GL nerve responses to quinine and sucrose. The reductions in taste responsiveness persisted into adulthood for quinine but not for any of the other stimuli. Adolescent experimental rats also exhibited reduced TG neuron responses to ethanol, capsaicin, and mustard oil. The lack of change in responsiveness of the taste nerves to NaCl and the TG neurons to KCl indicates that FAE altered only a subset of the response pathways within each chemosensory system. We propose that FAE reprograms development of the peripheral taste and trigeminal systems in ways that reduce their responsiveness to ethanol and surrogates for its pleasant (i.e., sweet) and unpleasant (i.e., bitterness, oral burning) flavor attributes.NEW & NOTEWORTHY Pregnant mothers are advised to avoid alcohol. This is because even small amounts of alcohol can alter fetal brain development and increase the risk of adolescent alcohol abuse. We asked how fetal alcohol exposure (FAE) produces the latter effect in adolescent rats by measuring responsiveness of taste nerves and trigeminal

  1. Reconnaissance chirale dans des complexes moléculaires neutres et ioniques

    OpenAIRE

    Sen, Ananya

    2012-01-01

    The main objective of this thesis is a spectroscopic study of molecules or complexes bearing multiple chiral centres in the gas phase, to understand the effects of stereochemistry on their structural properties. Neutral cinchona alkaloids have been introduced intact in gas phase by laser-ablation. They have been studied by combining supersonic expansion with laser spectroscopy. The two pseudo-enantiomers Quinine and Quinidine show similar electronic and vibrational spectra, in line with simil...

  2. Preparation of Poly(ionic liquid)s-Supported Recyclable Organocatalysts for the Asymmetric Nitroaldol (Henry) Reaction.

    Science.gov (United States)

    Großeheilmann, Julia; Bandomir, Jenny; Kragl, Udo

    2015-12-21

    A novel strategy for the embedding of quinine-based organocatalysts in polymerized ionic liquids-based hydrogels is presented. With this technique, the encapsulated organocatalyst was successfully recovered and reused for four cycles without any loss of enantioselectivity (up to 91% ee) for the asymmetric nitroaldol (Henry) reaction. In this study, high catalyst leaching was significantly reduced (water content. After catalyst removal, evaporation of the solvent affords the product in 98% purity without any further purification.

  3. Drenched in Dirt and Drowned in Abominations: Insects and the Civil War

    Science.gov (United States)

    2008-11-16

    ridgepole produced an olfactory sensation which and mockingly barked at their victim has yet to be duplicated in the Western until he went to sleep, great...which no christian olfactory could was a filth fly smorgasbord. A Virginia withstand. Countless thousands of green private elaborated in his diary...difficult to (Library of Congress) obtain in the South, which led to quinine smuggling and a black market . Prices of Mosquito abatement was virtually $400

  4. Lead Poison Detection

    Science.gov (United States)

    1976-01-01

    With NASA contracts, Whittaker Corporations Space Science division has developed an electro-optical instrument to mass screen for lead poisoning. Device is portable and detects protoporphyrin in whole blood. Free corpuscular porphyrins occur as an early effect of lead ingestion. Also detects lead in urine used to confirm blood tests. Test is inexpensive and can be applied by relatively unskilled personnel. Similar Whittaker fluorometry device called "drug screen" can measure morphine and quinine in urine much faster and cheaper than other methods.

  5. Asymmetric Construction of Spiro[thiopyranoindole-benzoisothiazole] Scaffold via a Formal [3 + 3] Spiroannulation.

    Science.gov (United States)

    Chen, Xiang; Zhang, Jun-Qi; Yin, Shao-Jie; Li, Hai-Yan; Zhou, Wei-Qun; Wang, Xing-Wang

    2015-09-04

    An enantioselective formal thio[3 + 3] spiroannulation reaction of indoline-2-thiones to 1-azadienes has been developed by the use of a quinine-derived bifunctional tertiary amine-thiourea catalyst, which furnished a series of optically active spiro[thiopyranoindole-benzoisothiazole] heterocycles with a spiro quaternary C-N/C-S stereogenic centers in high yields with good to excellent diastereo- and enantioselectivities.

  6. [Differential diagnosis and treatment of cramps].

    Science.gov (United States)

    Diener, H C; Westphal, K

    2013-10-10

    Cramps are painful sensations caused by intense involuntary contractions of skeletal muscles, mostly in the calves, usually lasting from a few seconds to several minutes. Although cramps are mostly idiopathic, theycan bea symptom of other forms of myalgia, restless legs syndrome or spasticity. Especially nocturnal cramps can cause considerable distress for patients requiring fast pain reduction and effective prophylaxis. Stretching the calf muscles helps preventing nocturnal cramps. Pharmacological treatment of leg cramps includes magnesium and quinine.

  7. 手性两亲超支化嵌段共聚物PG-b-PBTQMO-b-PG的合成%Synthesis of chiral amphiphilic hyperbranched block copolymer PG-b-PBTQMO-b-PG

    Institute of Scientific and Technical Information of China (English)

    蒋伟伟; 李胜夏; 郭素珍; 胡志国

    2013-01-01

    以叠氮基修饰的超支化共聚物PG-b-PBAMO-b-PG和10,11-二氢化奎宁为原料,通过“click”化学反应合成了一种新型侧链含有奎宁的光学活性两亲超支化嵌段共聚物PG-b-PBTQMO-b-PG.用傅里叶转变红外光谱(FT-IR)和核磁共振氢谱(1HNMR)对产物结构和组成进行了表征,并利用圆二色谱法研究了手性共聚物的光学活性.%A new optically active amphiphilic hyperbranehed block copolymer bearing quinine pendants pol-yglyeerol-b-poly [3,3-bis(triazolyl-L-quinine) methyl oxetane]-b-polyglycerol (PG-b-PBTQMO-b-PG) was synthesized by" click" reaction of azido-modified polyglycerol-b-poly(3,3-bis(azidomethyl) oxetane)-b-polyglycerol (PG-b-PBAMO-b-PG) hyperbranched eopolymer and 10,11-didehydro quinine.The Fourier transform infrared spectrum(FT-IR) and 1H nuclear magnetic resonance spectroscopy(1HNMR)were used to confirm its structure and composition.Additionally,the solution properties of this chiral copolymer were stu-died by circular dichroism(CD) spectroscopy.

  8. Bitter-sensitive gustatory receptor neuron responds to chemically diverse insect repellents in the common malaria mosquito Anopheles quadrimaculatus

    Science.gov (United States)

    Sparks, Jackson T.; Dickens, Joseph C.

    2016-06-01

    Female mosquitoes feed on blood from animal hosts to obtain nutritional resources used for egg production. These contacts facilitate the spread of harmful human diseases. Chemical repellents are used to disrupt mosquito host-seeking and blood-feeding behaviors; however, little is known about the gustatory sensitivity of mosquitoes to known repellents. Here, we recorded electrical responses from gustatory receptor neurons (GRNs) housed within the labellar sensilla of female Anopheles quadrimaculatus to N,N-diethyl-3-methylbenzamide (DEET), picaridin, IR3535, 2-undecanone, p-menthane-3,8-diol, geraniol, trans-2-hexen-1-ol, quinine, and quinidine. A bitter-sensitive GRN responded to all tested repellents and quinine, a known feeding deterrent. Responses of the bitter-sensitive neuron to quinine and an isomer, quinidine, did not differ. Delayed bursts of electrical activity were observed in response to continuous stimulation with synthetic repellents at high concentrations. Electrophysiological recordings from bitter-sensitive GRNs associated with mosquito gustatory sensilla represent a convenient model to evaluate candidate repellents.

  9. Bioactivities examination of Cinchona leaves ethanol extracts

    Science.gov (United States)

    Artanti, Nina; Udin, Linar Z.; Hanafi, M.; Jamilah, Kurniasih, Ida Rahmi; Primahana, Gian; Anita, Yulia; Sundowo, Andini; Kandace, Yoice Sri

    2017-01-01

    Cinchona species especially the barks are commonly known for commercial production of quinine as antimalarial. Although it is also reported for treatment of depurative, whooping cough, influenza and dysentery. In this paper we reported in vitro examination of other bioactivities (antidiabetes, antioxidant and in vitro cytotoxicity) of 70% ethanol extract of Cinchona ledgeriana and C. succirubra leaves as well as qunine, quinidine, and cinchonine the major alkaloids found in Cinchona species. Antidiabetes was conducted using α-glucosidase inhibitory activity assay. Antioxidant was conducted using DPPH free radical scavenging activity assay. In vitro cytotoxic activity was concucted by microscopic observation on growth of breast cancer cell line MCF-7. The results showed that at concentration of 100 µg/ml, C. ledgeriana leaves ethanol extracts showed the best activity as antidiabetes (98% inhibitory of α-glucosidase activity) and antioxidant (92% DPPH free radical scavenging activity), whereas at the same concentration C. succirubra, quinine, quinidine and cinchonine showed very low activities of antidiabetes and antioxidant. Microscopic observation of in vitro cytotoxicity showed that C. ledgeriana also has excellent cytotoxicity to breast cancer cell line MCF-7 which better than quinine, quinidine and cinchonine, whereas C. succirubra showed low cytotoxicity. These results suggest that cinchona species have many potential as the source of drugs discovery and development other than just for malaria treatment. Therefore it is important to conduct further studies and to maintain the available Cinchona plantation in Indonesia.

  10. Constructing quality profiles for taste compounds in rats: a novel paradigm.

    Science.gov (United States)

    Grobe, Connie L; Spector, Alan C

    2008-10-20

    We developed a novel behavioral method, adapted from the work by Morrison (1967), for the assessment of taste quality in rats. Four groups of rats were trained to discriminate a standard stimulus (either NaCl, sucrose, quinine, or citric acid, which are widely thought to represent the four basic human taste qualities of salty, sweet, bitter, and sour, respectively) from the remaining three compounds (each at multiple concentrations). Animals were then tested for generalization to the standard stimuli when test compounds were presented and a quality profile was constructed. Rats generalized novel concentrations of standard stimuli completely to their training concentrations and generalized their responses to mixtures of NaCl and sucrose on the basis of the relative concentrations of the stimulus components. In general, the sugars (at high concentrations), denatonium, tartaric acid, and sodium gluconate generalized to sucrose, quinine, citric acid, and NaCl, respectively. Monosodium glutamate generalized to a mixture of sucrose and NaCl. KCl produced a complex generalization profile with notable quinine and citric acid components. Our procedure supplements the current use of the conditioned taste aversion generalization procedure which has some procedural and interpretive limitations. Although our procedure involves the use of a complex stimulus delivery and response measurement apparatus and requires substantial initial conditioning of animals, once trained, a single cohort of animals can be tested for its response to a substantial number of test stimuli over the course of many months without any ostensible loss of stimulus control.

  11. Interactions between CO2 oral pungency and taste.

    Science.gov (United States)

    Cometto-Muñiz, J E; García-Medina, M R; Calviño, A M; Noriega, G

    1987-01-01

    Two experiments are reported in which the perceptual interactions between oral pungency, evoked by CO2, and the taste of each of four tastants--sucrose (sweet), quinine sulfate (bitter), sodium chloride (salty), and tartaric acid (sour)--were explored. In experiment 1 the effect of three concentrations of each tastant on the stimulus-response function for perceived oral pungency, in terms of both rate of change (slope) and relative position along the perceived pungency axis, was determined. In experiment 2 the effect of three concentrations of CO2 on the stimulus-response function for the perceived taste intensity of each tastant was examined. Results show that the characteristics of the mutual effects of tastant and pungent stimulus depend on the particular tastant employed. Sucrose sweetness and CO2 oral pungency have no mutual effect; sodium chloride saltiness or tartaric acid sourness and CO2 oral pungency show mutual enhancement; and quinine sulfate bitterness abates CO2 oral pungency, whereas CO2 has a double and opposite effect on quinine sulfate bitterness--at low concentrations of bitter tastant CO2 enhances bitterness, and at high concentrations of bitter tastant CO2 abates bitterness. It is suggested that the perceptual attributes of saltiness and sourness are closer, from a qualitative point of view, to oral pungency than are the attributes of bitterness and sweetness.

  12. Alkoxide coordination of iron(III) protoporphyrin IX by antimalarial quinoline methanols: a key interaction observed in the solid-state and solution.

    Science.gov (United States)

    Gildenhuys, Johandie; Sammy, Chandre J; Müller, Ronel; Streltsov, Victor A; le Roex, Tanya; Kuter, David; de Villiers, Katherine A

    2015-10-14

    The quinoline methanol antimalarial drug mefloquine is a structural analogue of the Cinchona alkaloids, quinine and quinidine. We have elucidated the single crystal X-ray diffraction structure of the complexes formed between racemic erythro mefloquine and ferriprotoporphyrin IX (Fe(iii)PPIX) and show that alkoxide coordination is a key interaction in the solid-state. Mass spectrometry confirms the existence of coordination complexes of quinine, quinidine and mefloquine to Fe(iii)PPIX in acetonitrile. The length of the iron(iii)-O bond in the quinine and quinidine complexes as determined by Extended X-ray Absorption Fine Structure (EXAFS) spectroscopy unequivocally confirms that coordination of the quinoline methanol compounds to Fe(iii)PPIX occurs in non-aqueous aprotic solution via their benzylic alkoxide functional group. UV-visible spectrophotometric titrations of the low-spin bis-pyridyl-Fe(iii)PPIX complex with each of the quinoline methanol compounds results in the displacement of a single pyridine molecule and subsequent formation of a six-coordinate pyridine-Fe(iii)PPIX-drug complex. We propose that formation of the drug-Fe(iii)PPIX coordination complexes is favoured in a non-aqueous environment, such as that found in lipid bodies or membranes in the malaria parasite, and that their existence may contribute to the mechanism of haemozoin inhibition or other toxicity effects that lead ultimately to parasite death. In either case, coordination is a key interaction to be considered in the design of novel antimalarial drug candidates.

  13. Acquired liking for sweet-paired odours is related to the disinhibition but not restraint factor from the Three Factor Eating Questionnaire.

    Science.gov (United States)

    Yeomans, Martin R; Mobini, Sirous; Bertenshaw, Emma J; Gould, Natalie J

    2009-02-16

    Previous research suggests that women scoring high on dietary restraint may be insensitive to flavour-flavour learning, but no study has yet explored this using the olfactory conditioning paradigm. Accordingly, 56 women who were sweet likers were classified as either high or low on both the Three Factor Eating Questionnaire restraint and disinhibition scales. They evaluated two odours before and after disguised pairings of one odour with 10% sucrose and the other with 0.01% quinine. Liking for the quinine-paired odour decreased post-training, with no effects of restraint or disinhibition. In contrast, the increase in liking for the sucrose-paired odour was significantly greater in women classified as scoring high in disinhibition, but was unaffected by restraint. Sweetness of the sucrose paired odour increased, and bitterness of the quinine-paired odour decreased, similarly in all groups. These data suggest that sensitivity of restrained eaters to flavour-based learning may result from their attitude to the food used as reinforcer rather than some basic failure in the learning process, and also suggest that women scoring high on disinhibition may show heightened sensitivity to hedonic cues.

  14. Rational development of taste masked oral liquids guided by an electronic tongue.

    Science.gov (United States)

    Woertz, Katharina; Tissen, Corinna; Kleinebudde, Peter; Breitkreutz, Jörg

    2010-11-15

    Human taste testing is often associated with ethical concerns, organizational and validation issues. Electrochemical sensor array systems, so called electronic tongues, offer an alternative to assess the taste of multi-component liquid formulations. Therefore, it should be investigated how an electronic tongue can be implemented in the rational development of taste masked formulations. Taste masking of bitter tasting quinine hydrochloride (QH) in a liquid formulation was carried out by screening sweetening agents (sucrose, glucose, fructose, mannitol, sucralose, sodium saccharin, acesulfame potassium, and monoammonium glycyrrhizinate), strong and weak cation ion exchange (IE) resins (Amberlite™ IRP69, Amberlite™ IRP88, and Indion 234), and soluble complexing agents (α-, β-, hydroxypropyl-β-, sulfobutyl ether-β- and γ-cyclodextrin and maltodextrin). Amberlite™ IRP88 showed the best binding capacity for quinine (1.9 g quinine/1 g IE). The addition of sulfobutyl ether-β-cyclodextrin (SBE-β-CD) could significantly reduce the bitter taste of QH (79% reduction of free QH). The SBE-β-CD formulation was further improved by adding sodium saccharin as secondary taste masking agent. It could also be shown that presence of strawberry flavor and the preservative domiphen bromide does not affect evaluation of taste masking efficiency. The introduced stepwise approach was shown to be applicable to rationally develop novel taste masked formulations.

  15. Fluorescence calibration method for single-particle aerosol fluorescence instruments

    Science.gov (United States)

    Shipley Robinson, Ellis; Gao, Ru-Shan; Schwarz, Joshua P.; Fahey, David W.; Perring, Anne E.

    2017-05-01

    Real-time, single-particle fluorescence instruments used to detect atmospheric bioaerosol particles are increasingly common, yet no standard fluorescence calibration method exists for this technique. This gap limits the utility of these instruments as quantitative tools and complicates comparisons between different measurement campaigns. To address this need, we have developed a method to produce size-selected particles with a known mass of fluorophore, which we use to calibrate the fluorescence detection of a Wideband Integrated Bioaerosol Sensor (WIBS-4A). We use mixed tryptophan-ammonium sulfate particles to calibrate one detector (FL1; excitation = 280 nm, emission = 310-400 nm) and pure quinine particles to calibrate the other (FL2; excitation = 280 nm, emission = 420-650 nm). The relationship between fluorescence and mass for the mixed tryptophan-ammonium sulfate particles is linear, while that for the pure quinine particles is nonlinear, likely indicating that not all of the quinine mass contributes to the observed fluorescence. Nonetheless, both materials produce a repeatable response between observed fluorescence and particle mass. This procedure allows users to set the detector gains to achieve a known absolute response, calculate the limits of detection for a given instrument, improve the repeatability of the instrumental setup, and facilitate intercomparisons between different instruments. We recommend calibration of single-particle fluorescence instruments using these methods.

  16. [Drug sensitivity of falciparum malaria imported into France in 1995].

    Science.gov (United States)

    Longuet, C; Ramiliarisoa, O; Thor, R; Bouchaud, O; Basco, L K; Doury, J C; Le Bras, J

    1997-01-01

    The National Reference Centre for Malaria Chemosusceptibility (CNRCP) and the Tropical Medicine Institute of the Health Department for the Army (IMTSSA) monitor the chemosusceptibility of falciparum malaria introduced in France. In 1995, 353 isolates of P. falciparum are sent to the CNRCP and IMTSSA from malaria cases presenting in 49 civil and military hospitals distributed all over the french country. The patients are mostly Africans living in France and have mainly stayed in West Africa. Half of them did not take any chemoprophylaxis and a quarter took only chloroquine more or less regularly. The curative treatment, when known, is halofantrine alone in 52% of cases and quinine alone in 28% of cases. Three halofantrine failures are reported including 1 incorrect regimen and 4 quinine failures including 3 incorrect regimens. In 1995, in vitro resistance of P. falciparum isolates imported in France to the chemoprophylactic and therapeutic drugs is not worsening. In vitro quinine resistance is rare (1/108), mefloquine resistance (2/20) and halofantrine resistance (12/211) are limited, cycloguanil resistance (42/185) is stable and chloroquine resistance (84/230) is even decreasing (less selective pressure in Africa?).

  17. Caffeine Bitterness is Related to Daily Caffeine Intake and Bitter Receptor mRNA Abundance in Human Taste Tissue.

    Science.gov (United States)

    Lipchock, Sarah V; Spielman, Andrew I; Mennella, Julie A; Mansfield, Corrine J; Hwang, Liang-Dar; Douglas, Jennifer E; Reed, Danielle R

    2017-01-01

    We investigated whether the abundance of bitter receptor mRNA expression from human taste papillae is related to an individual's perceptual ratings of bitter intensity and habitual intake of bitter drinks. Ratings of the bitterness of caffeine and quinine and three other bitter stimuli (urea, propylthiouracil, and denatonium benzoate) were compared with relative taste papilla mRNA abundance of bitter receptors that respond to the corresponding bitter stimuli in cell-based assays ( TAS2R4, TAS2R10, TAS2R38, TAS2R43, and TAS2R46). We calculated caffeine and quinine intake from a food frequency questionnaire. The bitterness of caffeine was related to the abundance of the combined mRNA expression of these known receptors, r = 0.47, p = .05, and self-reported daily caffeine intake, t(18) = 2.78, p = .012. The results of linear modeling indicated that 47% of the variance among subjects in the rating of caffeine bitterness was accounted for by these two factors (habitual caffeine intake and taste receptor mRNA abundance). We observed no such relationships for quinine but consumption of its primary dietary form (tonic water) was uncommon. Overall, diet and TAS2R gene expression in taste papillae are related to individual differences in caffeine perception.

  18. Synergy between verapamil and other multidrug -resistance modulators in model membranes

    Indian Academy of Sciences (India)

    Madeleine Castaing; Alain Loiseau; Athel Cornish-Bowden

    2007-06-01

    Various cationic lipophilic compounds can reverse the multidrug resistance of cancer cells. Possible interaction between these compounds, which are known as modulators, has been assessed by measuring leakage of Sulphan blue from anionic liposomes, induced both by verapamil alone and by verapamil in combination with diltiazem, quinine, thioridazine or clomipramine. An equation was derived to quantify the permeation doses and Hill coefficients of the drugs and mixtures between them by simultaneous fitting of the experimental data. The interaction was tested by two methods, the competition plot and the isobole method; both showed synergy between verapamil and each of diltiazem, quinine and thioridazine. The dose factor of potentiation for verapamil determined within membranes was 4.0 ± 0.4 with diltiazem, 3.2 ± 0.4 with quinine and 2.4 ± 0.3 with thioridazine. The results suggest that the effectiveness of reversing multidrug resistance may be increased with modulators such as verapamil and diltiazem that have a much greater effect in combination than what would be expected from their effects when considered separately.

  19. Unknotting night-time muscle cramp: a survey of patient experience, help-seeking behaviour and perceived treatment effectiveness

    Directory of Open Access Journals (Sweden)

    Blyton Fiona

    2012-03-01

    Full Text Available Abstract Background Night-time calf cramping affects approximately 1 in 3 adults. The aim of this study was to explore the experience of night-time calf cramp; if and where people seek treatment advice; and perceived treatment effectiveness. Methods 80 adults who experienced night-time calf cramp at least once per week were recruited from the Hunter region, NSW, Australia through newspaper, radio and television advertisements. All participants completed a pilot-tested survey about muscle cramp. Quantitative data were analysed with independent-sample t-tests, Chi square tests and Fisher's tests. Qualitative data were transcribed and sorted into categories to identify themes. Results Median recalled age of first night-time calf cramp was 50 years. Most participants recalled being awoken from sleep by cramping, and experiencing cramping of either calf muscle, calf-muscle soreness in the days following cramp and cramping during day-time. Despite current therapies, mean usual pain intensity was 66 mm on a 100 mm visual analogue scale. Participants described their cramps as being 'unbearable', 'unmanageable' and 'cruel'. One participant stated that 'sometimes I just wish I could cut my legs open' and another reported 'getting about 2 h sleep a night due to cramps'. Most participants had sought advice about their night-time calf cramps from a health professional. Participants identified 49 different interventions used to prevent night-time calf cramp. Of all treatment ratings, 68% described the intervention used to prevent cramp as being 'useless' or of 'a little help'. Of 14 participants who provided additional information regarding their use of quinine, eight had a current prescription of quinine for muscle cramp at the time of the survey. None had been asked by their prescribing doctor to stop using quinine. Conclusion Night time calf cramps typically woke sufferers from sleep, affected either leg and caused ongoing pain. Most participants

  20. Ability of medical students to calculate drug doses in children after their paediatric attachment

    Directory of Open Access Journals (Sweden)

    Oshikoya KA

    2008-12-01

    Full Text Available Dose calculation errors constitute a significant part of prescribing errors which might have resulted from informal teaching of the topic in medical schools. Objectives: To determine adequacy of knowledge and skills of drug dose calculations in children acquired by medical students during their clinical attachment in paediatrics.Methods: Fifty two 5th year medical students of the Lagos State University College of Medicine (LASUCOM, Ikeja were examined on drug dose calculations from a vial and ampoules of injections, syrup and suspension, and tablet formulation. The examination was with a structured questionnaire mostly in the form of multiple choice questions.Results: Thirty-six (69.2% and 30 (57.7% students were taught drug dose calculation in neonatal posting and during ward rounds/ bed-side teaching, respectively. Less than 50% of the students were able to calculate the correct doses of each of adrenaline, gentamicin, chloroquine and sodium bicarbonate injections required by the patient. Dose calculation was however relatively better with adrenalin when compared with the other injections. The proportion of female students that calculated the correct doses of quinine syrup and cefuroxime suspension were significantly higher than those of their male counterparts (p<0.05 and p<0.01, respectively; Chi-square test. When doses calculated in mg/dose and mL/dose was compared for adrenalin injection and each of quinine syrup and cefuroxime suspension, there were significant differences (adrenaline and quinine, p=0.005; adrenaline and cefuroxime, p=0.003: Fischer’s exact test. Dose calculation errors of similar magnitude to injections, syrup and suspension were also observed with tablet formulation.Conclusions: LASUCOM medical students lacked the basic knowledge of paediatric drug dose calculations but were willing to learn if the topic was formally taught. Drug dose calculations should be given a prominent consideration in the undergraduate medical

  1. Antimalarial substances of an endophytic fungus isolated from cinchona tree%一株具有抗疟活性的金鸡纳树内生真菌的研究

    Institute of Scientific and Technical Information of China (English)

    周松林; 陈双林; 黄风迎; 王华; 赵焕阁

    2013-01-01

    为筛选具抗疟疾活性的的内生真菌,采用平板分离法对海南金鸡那树内生真菌进行分离纯化.利用“4日抑制疟疾”测试内生真菌发酵液的抗疟活性,采用TLC、HPLC等分析技术对内生菌发酵液等成分进行分析.从金鸡那树叶片分离到31种内生真菌,通过筛选找到了1株具有抗疟疾活性的产奎宁或奎宁类似物的内生真菌.从金鸡那树叶片中分离得到1株产奎宁的结实串孢霉属内生真菌,为奎宁的资源开发开辟了新途径.%Plate method was used to isolate and purify endophytic fungi from Cinchona sp. in Hainan Province. The anti-malaria activity of fermented liquid of the endophytic fungi was tested using "4 day inhibit malaria", and the components such as quinine or structural analogues were analysed using TLC and HPLC. Of the 31 endophytic species isolated from cinchona tree one strain producing quinine or quinine analogues with antimalarial activity was obtained. Morphological observation indicated that this endophytic fungus could be identified as Hormiscium sp.

  2. A Model of Alcohol Drinking under an Intermittent Access Schedule Using Group-Housed Mice

    Science.gov (United States)

    Smutek, Magdalena; Turbasa, Mateusz; Sikora, Magdalena; Piechota, Marcin; Zajdel, Joanna; Przewlocki, Ryszard; Parkitna, Jan Rodriguez

    2014-01-01

    Here, we describe a new model of voluntary alcohol drinking by group-housed mice. The model employs sensor-equipped cages that track the behaviors of the individual animals via implanted radio chips. After the animals were allowed intermittent access to alcohol (three 24 h intervals every week) for 4 weeks, the proportions of licks directed toward bottles containing alcohol were 50.9% and 39.6% for the male and female mice, respectively. We used three approaches (i.e., quinine adulteration, a progressive ratio schedule and a schedule involving a risk of punishment) to test for symptoms of compulsive alcohol drinking. The addition of 0.01% quinine to the alcohol solution did not significantly affect intake, but 0.03% quinine induced a greater than 5-fold reduction in the number of licks on the alcohol bottles. When the animals were required to perform increasing numbers of instrumental responses to obtain access to the bottle with alcohol (i.e., a progressive ratio schedule), they frequently reached a maximum of 21 responses irrespective of the available reward. Although the mice rarely achieved higher response criteria, the number of attempts was ∼10 times greater in case of alcohol than water. We have developed an approach for mapping social interactions among animals that is based on analysis of the sequences of entries into the cage corners. This approach allowed us to identify the mice that followed other animals in non-random fashions. Approximately half of the mice displayed at least one interaction of this type. We have not yet found a clear correlation between imitative behavior and relative alcohol preference. In conclusion, the model we describe avoids the limitations associated with testing isolated animals and reliably leads to stable alcohol drinking. Therefore, this model may be well suited to screening for the effects of genetic mutations or pharmacological treatments on alcohol-induced behaviors. PMID:24804807

  3. New Insights into Enhancing Maximal Exercise Performance Through the Use of a Bitter Tastant.

    Science.gov (United States)

    Gam, Sharon; Guelfi, Kym J; Fournier, Paul A

    2016-10-01

    It is generally acknowledged that for an orally administered ergogenic aid to enhance exercise performance it must first be absorbed by the gastrointestinal tract before exerting its effects. Recently, however, it has been reported that some ergogenic aids can affect exercise performance without prior absorption by the gastrointestinal tract. This is best illustrated by studies that have shown that rinsing the mouth with a carbohydrate (CHO) solution, without swallowing it, significantly improves exercise performance. The ergogenic effects of CHO mouth rinsing in these studies have been attributed to the activation of the brain by afferent taste signals, but the specific mechanisms by which this brain activation translates to enhanced exercise performance have not yet been elucidated. Given the benefits of CHO mouth rinsing for exercise performance, this raises the issue of whether other types of tastants, such as bitter-tasting solutions, may also improve exercise performance. Recently, we performed a series of studies investigating whether the bitter tastant quinine can improve maximal sprint performance in competitive male cyclists, and, if so, to examine some of the possible mechanisms whereby this effect may occur. These studies have shown that mouth rinsing and ingesting a bitter-tasting quinine solution can significantly improve the performance of a maximal cycling sprint. There is also evidence that the ergogenic effect of quinine is mediated, at least in part, by an increase in autonomic nervous system activation and/or corticomotor excitability. The purpose of this article is to discuss the results and implications of these recent studies and to suggest avenues for further research, which may add to the understanding of the way the brain integrates signals from the oral cavity with motor behaviour, as well as uncover novel strategies to improve exercise performance.

  4. Effects of orally self-administered bath salt constituent 3,4-methylenedioxypyrovalerone (MDPV) in mice.

    Science.gov (United States)

    Gannon, Brenda M; Russell, Lauren N; Modi, Meet S; Rice, Kenner C; Fantegrossi, William E

    2017-10-01

    Synthetic cathinones in bath salts products are psychostimulant drugs of abuse, and 3,4-methylenedioxypyrovalerone (MDPV) is a common constituent of these products. Oral MDPV has been show to stimulate locomotor activity but reinforcing, locomotor and appetitive stimulus effects of oral MDPV are unknown. Choice procedures evaluated preference for 0.03, 0.10, 0.30, and 1.00mg/mL MDPV solutions versus 0.10mg/mL quinine solution or water. To verify that oral MDPV produced pharmacological effects, locomotor activity was monitored during and after consumption of water, quinine, or MDPV solutions. Conditioned place preference (CPP) tested the apparent appetitive effects of a preferred concentration of oral MDPV with locomotor stimulant effects (0.30mg/mL), using water as a control, and compared with results from intraperitoneally-administered MDPV. Consumption of MDPV solutions (0.03-1.00mg/mL) was low when the alternative fluid was water, but a history of MDPV consumption increased MDPV choice. When paired with a quinine control solution, MDPV solutions (0.03-0.30mg/mL) were almost exclusively preferred, and treatment with the catecholamine synthesis inhibitor αMPT decreased MDPV choice. Consumption of MDPV concentrations (0.1-1.0mg/mL) stimulated locomotor activity. Chronic (10day) access to 0.30mg/mL MDPV resulted in escalated consumption, but locomotor effects did not systematically change across the access period. Finally, consumption of 0.30mg/mL MDPV elicited CPP with a magnitude similar to the preference observed following intraperitoneal administration of MDPV. Consistent with human abuse patterns, oral MDPV has reinforcing effects in the mouse which are most likely related to its psychostimulant-like pharmacological profile. Copyright © 2017 Elsevier B.V. All rights reserved.

  5. Drug-induced immune thrombocytopenia: incidence, clinical features, laboratory testing, and pathogenic mechanisms.

    Science.gov (United States)

    Curtis, Brian R

    2014-01-01

    Drug-induced immune thrombocytopenia (DIIT) is a relatively uncommon adverse reaction caused by drug-dependent antibodies (DDAbs) that react with platelet membrane glycoproteins only when the implicated drug is present. Although more than 100 drugs have been associated with causing DIIT, recent reviews of available data show that carbamazepine, eptifibatide, ibuprofen, quinidine, quinine, oxaliplatin, rifampin, sulfamethoxazole, trimethoprim, and vancomycin are probably the most frequently implicated. Patients with DIIT typically present with petechiae, bruising, and epistaxis caused by an acute, severe drop in platelet count (often to transfusion refractoriness, and must be differentiated by temporal association of exposure to a candidate drug with an acute, severe drop in platelet count. Treatment consists of immediate withdrawal of the implicated drug. Criteria for strong evidence of DIIT include (1) exposure to candidate drug-preceded thrombocytopenia; (2) sustained normal platelet levels after discontinuing candidate drug; (3) candidate drug was only drug used before onset of thrombocytopenia or other drugs were continued or reintroduced after resolution of thrombocytopenia, and other causes for thrombocytopenia were excluded; and (4) reexposure to the candidate drug resulted in recurrent thrombocytopenia. Flow cytometry testing for DDAbs can be useful in confirmation of a clinical diagnosis, and monoclonal antibody enzyme-linked immunosorbent assay testing can be used to determine the platelet glycoprotein target(s), usually GPIIb/IIIa or GPIb/IX/V, but testing is not widely available. Several pathogenic mechanisms for DIIT have been proposed, including hapten, autoantibody, neoepitope, drug-specific, and quinine-type drug mechanisms. A recent proposal suggests weakly reactive platelet autoantibodies that develop greatly increased affinity for platelet glycoprotein epitopes through bridging interactions facilitated by the drug is a possible mechanism for the

  6. Covalently {beta}-cyclodextrin modified single-walled carbon nanotubes: a novel artificial receptor synthesized by 'click' chemistry

    Energy Technology Data Exchange (ETDEWEB)

    Guo Zhen; Liang Li [Nankai University, State Key Laboratory and Institute of Elemento-Organic Chemistry (China); Liang Jiajie; Ma Yanfeng; Yang Xiaoying [Nankai University, Center for Nanoscale Science and Technology and Institute of Polymer Chemistry, College of Chemistry (China); Ren Dongmei [Nankai University, State Key Laboratory and Institute of Elemento-Organic Chemistry (China); Chen Yongsheng [Nankai University, Center for Nanoscale Science and Technology and Institute of Polymer Chemistry, College of Chemistry (China); Zheng Jianyu, E-mail: jyzheng@nankai.edu.c [Nankai University, State Key Laboratory and Institute of Elemento-Organic Chemistry (China)

    2008-08-15

    Novel {beta}-cyclodextrin covalently modified single-walled carbon nanotubes have been synthesized via a 'click' coupling reaction. The product was fully characterized with Raman, FTIR, XRD, UV-Vis-NIR spectra as well as TEM and TGA measurements. The effective functionalization via 'click' coupling has set up a facile and versatile route for modular preparation of SWNTs based functional materials. The inclusion complexation behavior of this artificial receptor with quinine has been investigated in aqueous solution by fluorescence spectroscopy.

  7. Catalytic Enantioselective 1,2-Addition of Terminal 1,3-Diynes to Trifluoromethyl Ketones

    Institute of Scientific and Technical Information of China (English)

    Yan Zheng; Hai Ma; Jun-An Ma

    2016-01-01

    A facile catalytic enantioselective 1,2-addition of diynes to trifluoromethyl ketones was developed.By a combination of Me2Zn,Ti(OPr-i)4,BaF2 and quinine,the reaction of a series of terminal diynes with trifluoromethyl ketones proceeded to afford trifluoromethylated chrial tertiary alcohols with the diyne moiety in good to high yields with moderate to high enantioselectivities.Furthermore,this catalytic asymmetric diyne addition to trifluoromethylketone was applied in the synthesis of the Efavirenz analogue.

  8. Computation of the Redox and Protonation Properties of Quinones: Towards the Prediction of Redox Cycling Natural Products.

    Energy Technology Data Exchange (ETDEWEB)

    Cape, Jonathan L.; Bowman, Michael K.; Kramer, David M.

    2006-08-01

    Quinone metabolites perform a variety of key functions in plants, including pathogen protection, oxidative phosphorylation, and redox signaling. Many of these structurally diverse compounds have been shown to exhibit potent antimicrobial, anticancer, and anti-inflammatory properties, although the exact mechanisms of action are far from understood. Redox cycling has been proposed as a possible mechanism of action for many quinine species. Experimental determination of the essential thermodynamic data (i.e. electrochemical and pKa values) required to predict the propensity towards redox cycling is often difficult or impossible to obtain due to the experimental limitations. We demonstrate a practical computational approach to obtain reasonable estimates of these parameters.

  9. 新型螺芴类蓝光材料的合成与性能%Synthesis and Optoelectric Properties of Novel Spirofluorene for Blue Light-emitting Materials

    Institute of Scientific and Technical Information of China (English)

    游红军; 李穿江; 张智勇; 关金涛; 未本美; 戴志群

    2011-01-01

    A type of spirofluorene, DCSF, was successfully synthesized through a series of organic reactions, and determined by H NMR, C NMR, MS, FT-IR. Optoelectric properties were researched by UV-Vis absorption spectra and fluorescence spectra. The photoluminescence quantum yield was measured by the relative comparison method, using quinine sulfate in 0. 05 mol/L H2SO4 as standard, which was measured to be 0.391. The energy gap of the HOMO energy and LUMO energy was calculated through cyclic voltammeter measurement, which was estimated to be 3.32 eV.

  10. One-step ligand exchange reaction as an efficient way for functionalization of magnetic nanoparticles

    Energy Technology Data Exchange (ETDEWEB)

    Mrowczynski, Radoslaw [Humboldt-University Berlin, Department of Chemistry (Germany); Rednic, Lidia; Turcu, Rodica [National Institute of Research and Development for Isotopic and Molecular Technologies (Romania); Liebscher, Juergen, E-mail: liebscher@chemie.hu-berlin.de [Humboldt-University Berlin, Department of Chemistry (Germany)

    2012-07-15

    Novel magnetic Fe{sub 3}O{sub 4} nanoparticles (NPs) covered by one layer of functionalized fatty acids, bearing entities (Hayashi catalyst, biotin, quinine, proline, and galactose) of high interest for practical application in nanomedicine or organocatalysis, were synthesized. The functionalized fatty acids were obtained by Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC) of azido fatty acids with alkynes. All the magnetic NPs show superparamagnetic behavior with high values of magnetization and high colloidal stability in DCM solution.

  11. Optical measurements of platinum based electrocatalysts for the electrooxidation of methanol

    Energy Technology Data Exchange (ETDEWEB)

    Gruber, K. [Institute for Analytical and Chemical Technologies, Department of Electrochemistry, Vienna University of Technology, A-1060 Vienna (Austria); Kronberger, H.; Fafilek, G. [ECHEM Centre of Competence in Applied Electrochemistry, Wiener Neustadt (Austria); Institute for Analytical and Chemical Technologies, Department of Electrochemistry, Vienna University of Technology, A-1060 Vienna (Austria); Nauer, G. [ECHEM Centre of Competence in Applied Electrochemistry, Wiener Neustadt (Austria); Institute of Physical Chemistry, University of Vienna, Vienna (Austria); Besenhard, J.O. [ECHEM Centre of Competence in Applied Electrochemistry, Wiener Neustadt (Austria); Institute of Chemical Technology of Inorganic Materials, Graz University of Technology, Graz (Austria)

    2003-08-01

    In a combinatorial electrochemistry experiment quinine was used as a pH sensitive fluorescing indicator to detect the catalytic activity of methanol oxidation catalysts. During electrochemical experiments the surface of the electrode array was monitored with a CCD camera. The dependence of the intensity of the fluorescence on the applied potential was used as an analytical tool; to investigate the electrochemical performance of Pt based electrocatalysts, for the electrooxidation of methanol, in both short and long term tests. (Abstract Copyright [2003], Wiley Periodicals, Inc.)

  12. 04101 奎宁在澳大利亚不再用于痛性痉挛

    Institute of Scientific and Technical Information of China (English)

    杨绍杰

    2005-01-01

    澳大利亚药物不良反应顾问委员会(ADRAC)已宣布,由于奎宁(quinine)存在发生血小板减少的危险,因此在澳大利亚不再被批准用于治疗夜间痛性痉挛。ADRAC已收到228份不良药物反应报告和6例与用该药相关的死亡报告。

  13. Access to Artemisinin-Combination Therapy (ACT) and other Anti-Malarials: National Policy and Markets in Sierra Leone

    Science.gov (United States)

    Amuasi, John H.; Diap, Graciela; Nguah, Samuel Blay; Karikari, Patrick; Boakye, Isaac; Jambai, Amara; Lahai, Wani Kumba; Louie, Karly S.; Kiechel, Jean-Rene

    2012-01-01

    Malaria remains the leading burden of disease in post-conflict Sierra Leone. To overcome the challenge of anti-malarial drug resistance and improve effective treatment, Sierra Leone adopted artemisinin-combination therapy artesunate-amodiaquine (AS+AQ) as first-line treatment for uncomplicated P. falciparum malaria. Other national policy anti-malarials include artemether-lumefantrine (AL) as an alternative to AS+AQ, quinine and artemether for treatment of complicated malaria; and sulphadoxine-pyrimethamine (SP) for intermittent preventive treatment (IPTp). This study was conducted to evaluate access to national policy recommended anti-malarials. A cross-sectional survey of 127 medicine outlets (public, private and NGO) was conducted in urban and rural areas. The availability on the day of the survey, median prices, and affordability policy and available non-policy anti-malarials were calculated. Anti-malarials were stocked in 79% of all outlets surveyed. AS+AQ was widely available in public medicine outlets; AL was only available in the private and NGO sectors. Quinine was available in nearly two-thirds of public and NGO outlets and over one-third of private outlets. SP was widely available in all outlets. Non-policy anti-malarials were predominantly available in the private outlets. AS+AQ in the public sector was widely offered for free. Among the anti-malarials sold at a cost, the same median price of a course of AS+AQ (US$1.56), quinine tablets (US$0.63), were found in both the public and private sectors. Quinine injection had a median cost of US$0.31 in the public sector and US$0.47 in the private sector, while SP had a median cost of US$0.31 in the public sector compared to US$ 0.63 in the private sector. Non-policy anti-malarials were more affordable than first-line AS+AQ in all sectors. A course of AS+AQ was affordable at nearly two days’ worth of wages in both the public and private sectors. PMID:23133522

  14. Associative learning in wild Anastrepha obliqua females (Diptera, Tephritidae) related to a protein source Aprendizagem associativa em fêmeas selvagens de Anastrepha obliqua (Diptera, Tephritidae) em relação a uma fonte protéica

    OpenAIRE

    2006-01-01

    The aim of the present study was to determine whether wild adult Anastrepha obliqua (Macquart, 1835) females are able to associate a compound (quinine sulphate - QS) not related to their habitual diet with a protein-enriched food. Females were first fed on diets based on brewer yeast and sucrose containing or not QS. The groups were then allowed to choose between their original diets and a diet with or without QS, depending on the previous treatment, and between a diet based on agar and a die...

  15. Associative learning in wild Anastrepha obliqua females (Diptera, Tephritidae) related to a protein source

    OpenAIRE

    2006-01-01

    The aim of the present study was to determine whether wild adult Anastrepha obliqua (Macquart, 1835) females are able to associate a compound (quinine sulphate - QS) not related to their habitual diet with a protein-enriched food. Females were first fed on diets based on brewer yeast and sucrose containing or not QS. The groups were then allowed to choose between their original diets and a diet with or without QS, depending on the previous treatment, and between a diet based on agar and a die...

  16. Internal heavy atom effect of Au(III) and Pt(IV) on hypocrellin A for enhanced in vitro photodynamic therapy of cancer.

    Science.gov (United States)

    Zhou, Lin; Ge, Xuefeng; Liu, Jihua; Zhou, Jiahong; Wei, Shaohua; Li, Fuyou; Shen, Jian

    2013-10-01

    Hypocrellin A (HA), an a natural perylene quinine photosensitizers (PSs), can chelate with heavy metal ions, including Au(III) and Pt(IV), to form a 1:2 complex, which exhibits enhanced (1)O2 generation quantum yield through the increased intersystem crossing efficiency mediated by internal heavy atom effect. Besides, the chelate process greatly improved the water solubility of HA. Comparative studies with HA and complexes have demonstrated that the heavy-atom effect on HA molecules enhances the efficiency of in vitro photodynamic (PDT) efficacy.

  17. [History of malaria control in the French armed forces: from Algeria to the Macedonian front during the first World War].

    Science.gov (United States)

    Migliani, R; Meynard, J-B; Milleliri, J-M; Verret, C; Rapp, C

    2014-01-01

    The French joint military health corps has long experience in malaria control. Many military physicians played an essential role in the 19th century: Maillot revolutionized malaria treatment by using quinine during the conquest of Algeria, and Laveran discovered the causal parasite (the genus Plasmodium) there. This experience continued under the direction of Laveran and the Sergent brothers on the eastern front in Greek Macedonia during World War I. The vast coordinated control plan established on this front from 1917 delivered the French infantrymen from malaria and led to victory over the Bulgarian forces, which capitulated in September 1918.

  18. Possible artemisinin-based combination therapy-resistant malaria in Nigeria: a report of three cases

    Directory of Open Access Journals (Sweden)

    Nnennaya Anthony Ajayi

    2013-07-01

    Full Text Available Artemisinin-based combination therapy-resistant malaria is rare in Sub-Saharan Africa. The World Health Organization identifies monitoring and surveillance using day-3 parasitaemia post-treatment as the standard test for identifying suspected artemisinin resistance. We report three cases of early treatment failure due to possible artemisinin-based combination therapy-resistant Plasmodium falciparum malaria. All cases showed adequate clinical and parasitological responses to quinine. This study reveals a need to re-evaluate the quality and efficacy of artemisinin-based combination therapy agents in Nigeria and Sub-Saharan Africa.

  19. Inhibition of native 5-HT3 receptor-evoked contractions in guinea pig and mouse ileum by antimalarial drugs.

    Science.gov (United States)

    Kelley, Stephen P; Walsh, Jacqueline; Kelly, Mark C; Muhdar, Simerjyot; Adel-Aziz, Mohammed; Barrett, Iain D; Wildman, Scott S

    2014-09-05

    Quinine, chloroquine and mefloquine are commonly used to treat malaria, however, with associated gastrointestinal (GI) side-effects. These drugs act as antagonists at recombinant 5-HT3 receptors and modulate gut peristalsis. These gastrointestinal side effects may be the result of antagonism at intestinal 5-HT3 receptors. Ileum from male C57BL/6 mice and guinea pigs was mounted longitudinally in organ baths. The concentration-response curves for 5-HT and the selective 5-HT3 agonist 2-Me-5-HT were obtained with 5-HT (pEC50 = 7.57 ± 0.33, 12) more potent (P = 0.004) than 2-Me-5-HT (pEC50 = 5.45 ± 0.58, n = 5) in mouse ileum. There was no difference in potency of 5-HT (pEC50 = 5.42 ± 0.15, n = 8) and 2-Me-5-HT (pIC50 = 5.01 ± 0.55, n = 11) in guinea pig ileum (P > 0.05). Quinine, chloroquine or mefloquine was applied for 10 min and inhibitions prior to submaximal agonist application. In mouse ileum, quinine, chloroquine and mefloquine antagonised 5-HT-induced contractions (pIC50 = 4.9 ± 0.17, n = 7; 4.76 ± 0.14, n = 5; 6.21 ± 0.2, n = 4, correspondingly) with mefloquine most potent (P contractions (pIC50 = 6.35 ± 0.11, n = 8; 4.64 ± 0.2, n = 7; 5.11 ± 0.22, n = 6, correspondingly) with quinine most potent (P contractions (pIC50 = 5.02 ± 0.15, n = 6; 4.54 ± 0.1, n = 7; 5.32 ± 0.13, n = 5) and 2-me-5-HT-induced contractions (pIC50 = 4.62 ± 0.25, n = 5; 4.56 ± 0.14, n = 6; 5.67 ± 0.12, n = 4) with chloroquine least potent against 5-HT and mefloquine most potent against 2-me-5-HT (P < 0.05). These results support previous studies identifying anti-malarial drugs as antagonists at recombinant 5-HT3 receptors and may also demonstrate the ability of these drugs to influence native 5-HT3 receptor-evoked contractile responses which may account for their associated GI side-effects.

  20. Long-term olfactory memories are stabilised via protein synthesis in Camponotus fellah ants

    DEFF Research Database (Denmark)

    Guerrieri, Fernando Javier; D'Ettorre, Patrizia; Deveaud, J-M.

    2011-01-01

    Ants exhibit impressive olfactory learning abilities. Operant protocols in which ants freely choose between rewarded and nonrewarded odours have been used to characterise associative olfactory learning and memory. Yet, this approach precludes the use of invasive methods allowing the dissection......-chain hydrocarbons, one paired with sucrose and the other with quinine solution. Differential conditioning leads to the formation of a long-term memory retrievable at least 72¿h after training. Long-term memory consolidation was impaired by the ingestion of cycloheximide, a protein synthesis blocker, prior...

  1. Primary amine/CSA ion pair: A powerful catalytic system for the asymmetric enamine catalysis

    KAUST Repository

    Liu, Chen

    2011-05-20

    A novel ion pair catalyst containing a chiral counteranion can be readily derived by simply mixing cinchona alkaloid-derived diamine with chiral camphorsulfonic acid (CSA). A mixture of 9-amino(9-deoxy)epi-quinine 8 and (-)-CSA was found to be the best catalyst with matching chirality, enabling the direct amination of α-branched aldehydes to proceed in quantitative yields and with nearly perfect enantioselectivities. A 0.5 mol % catalyst loading was sufficient to catalyze the reaction, and a gram scale enantioselective synthesis of biologically important α-methyl phenylglycine has been successfully demonstrated. © 2011 American Chemical Society.

  2. Solvent-driven chiral-interaction reversion for organogel formation.

    Science.gov (United States)

    Qing, Guangyan; Shan, Xingxing; Chen, Wenrui; Lv, Ziyu; Xiong, Peng; Sun, Taolei

    2014-02-17

    For chiral gels and related applications, one of the critical issues is how to modulate the stereoselective interaction between the gel and the chiral guest precisely, as well as how to translate this information into the macroscopic properties of materials. Herein, we report that this process can also be modulated by nonchiral solvents, which can induce a chiral-interaction reversion for organogel formation. This process could be observed through the clear difference in gelation speed and the morphology of the resulting self-assembly. This chiral effect was successfully applied in the selective separation of quinine enantiomers and imparts "smart" merits to the gel materials.

  3. Gustatory receptor neuron responds to DEET and other insect repellents in the yellow-fever mosquito, Aedes aegypti

    Science.gov (United States)

    Sanford, Jillian L.; Shields, Vonnie D. C.; Dickens, Joseph C.

    2013-03-01

    Three gustatory receptor neurons were characterized for contact chemoreceptive sensilla on the labella of female yellow-fever mosquitoes, Aedes aegypti. The neuron with the smallest amplitude spike responded to the feeding deterrent, quinine, as well as N, N-diethyl-3-methylbenzamide and other insect repellents. Two other neurons with differing spikes responded to salt (NaCl) and sucrose. This is the first report of a gustatory receptor neuron specific for insect repellents in mosquitoes and may provide a tool for screening chemicals to discover novel or improved feeding deterrents and repellents for use in the management of arthropod disease vectors.

  4. Functional-Group-Tolerant, Silver-Catalyzed N-N Bond Formation by Nitrene Transfer to Amines.

    Science.gov (United States)

    Maestre, Lourdes; Dorel, Ruth; Pablo, Óscar; Escofet, Imma; Sameera, W M C; Álvarez, Eleuterio; Maseras, Feliu; Díaz-Requejo, M Mar; Echavarren, Antonio M; Pérez, Pedro J

    2017-02-15

    Silver(I) promotes the highly chemoselective N-amidation of tertiary amines under catalytic conditions to form aminimides by nitrene transfer from PhI═NTs. Remarkably, this transformation proceeds in a selective manner in the presence of olefins and other functional groups without formation of the commonly observed aziridines or C-H insertion products. The methodology can be applied not only to rather simple tertiary amines but also to complex natural molecules such as brucine or quinine, where the products derived from N-N bond formation were exclusively formed. Theoretical mechanistic studies have shown that this selective N-amidation reaction proceeds through triplet silver nitrenes.

  5. An Economical, Highly Efficient and Recyclable Catalyst System for Asymmetric Dihydroxylation of Olefins

    Institute of Scientific and Technical Information of China (English)

    金瑛; 孙晓莉; 姜茹; 张生勇

    2005-01-01

    A reusable cinchona alkaloid derivative ligand, which could be easily synthesized by two step transformation with cheap 3,6-dichloropyridazine and quinine as materials, was applied to homogeneous asymmetric dihydroxylation of olefins with NMO as co-oxidant in Me2CO-H20 system and the products could be extracted with Et2O from the recyclable catalyst system. 80%---93% yield and 51%-99% ee have been obtained. When trans-stilbene was chosen as the substrate for recycling experiment, 88%-92% yield and >99% ee have been obtained for ten recycles.

  6. THE ASYMMETRIC SYNTHESIS OF AMINO ACIDS UNDER POLYMER-SUPPORTED PHASE TRANSFER CATALYTIC CONDITION

    Institute of Scientific and Technical Information of China (English)

    1998-01-01

    The optical α-amino acids were synthesized under room temperature by alkylation of N-(diphenyl methylene) glycine t-butyl ester under polymer-supported phase transfer conditions using polymer-supported cinchonine (or quinine) alkaloids as chiral phase transfer catalysts and dichloromethane as solvent, followed by hydrolysis of the above intermediates introduced to the final products-optical α-amino acids. This is a new method for the asymmetric synthesis of α-amino acids. The influences of catalyst,temperature, substrates, and organic solvents on the chemical yield and optical purities of products were studied.

  7. Polymer-Supported Cinchona Alkaloid-Derived Ammonium Salts as Recoverable Phase-Transfer Catalysts for the Asymmetric Synthesis of α-Amino Acids

    Directory of Open Access Journals (Sweden)

    Carmen Nájera

    2004-04-01

    Full Text Available Alkaloids such as cinchonidine, quinine and N-methylephedrine have been N-alkylated using polymeric benzyl halides or co-polymerized and then N-alkylated, thus affording a series of polymer-supported chiral ammonium salts which have been employed as phase-transfer catalysts in the asymmetric benzylation of an N-(diphenylmethyleneglycine ester. These new polymeric catalysts can be easily recovered by simple filtration after the reaction and reused. The best ee’s were achieved when Merrifield resin-anchored cinchonidinium ammonium salts were employed.

  8. A new subculture and nematocidal assay using a species of diplogastridae.

    Science.gov (United States)

    Yanagida, J; Matsuhashi, R; Watanabe, I; Satou, T; Koike, K; Nikaido, T; Akao, S

    1998-08-01

    A new subculture method and a novel microplate assay for nematocidal activity using a species of Diplogastridae have been developed. The assay gives results rapidly, with high sensitivity in 4 h, and indicated good correlation between action mechanism and the nematode shape when examining 15 known compounds, including the antiparasitic avermectin, antimalarial quinine, and the gamma-amino-n-butyric acidA (GABAA) activated Cl- channel antagonist picrotoxinin. Thus new assay could be used as a primary screening method for new nematocidal compounds.

  9. Malaria and colonialism in the German colonies New Guinea and the Cameroons. Research, control, thoughts of eradication.

    Science.gov (United States)

    Eckart, W U

    1998-06-01

    German malaria research during the colonial period took place between medical and political interests. In the field of zoological and clinical research of malaria Germany was not a pioneer. Nevertheless, Robert Koch forced by impressive Italian results tried to participate in malaria research on the field of acquired malaria immunity and by optimizing the therapeutic doses of quinine in German New Guinea. In the German Cameroons, on the other hand, the fight against malaria was completely dominated by racial and political arguments. The paper tries to shed light on this dichotomy, which turned out to be not very productive.

  10. Egyptian human babesiosis and general review.

    Science.gov (United States)

    El-Bahnasawy, Mamdouh M; Morsy, Tosson A

    2008-04-01

    Babesiosis is tick-borne malaria-like disease. Man is an opportuneistic host for Babesia species. This paper presented the second Egyptian human babesiosis. The signs and symptoms, CBC, liver functions and kidney functions tests and all other serologic tests did not give any definite diagnosis. Also, he was sero-negative for malaria infection. The patient was critically diagnosed by the demonstration of the typical ring forms of Babesia species in stained blood smears. He was successfully treated with Quinine and Clindamycin, and was discharged from the hospital after the clinical and parasitological improvement. The epidemiology of zoonotic babesiosis was discussed.

  11. Malaria treatment-seeking behaviour and drug prescription practices in an area of low transmission in Uganda

    DEFF Research Database (Denmark)

    Ndyomugyenyi, Richard; Magnussen, Pascal; Clarke, Siân

    2007-01-01

    to protect second-line drugs from misuse. Failure to comply with drug policy in both the private and public sectors is of concern in an era of rapidly evolving drug policy changes and highlights the need for reorientation and training of health staff and drug vendors to improve malaria diagnostic...... actually using insecticide-treated nets. Many patients (25%) had received treatment prior to visiting a health facility, with drug shops and general stores being the main sources of treatment. Some shops dispensed quinine, a second-line drug recommended for complicated malaria. Prescription practices...

  12. The Chemical Constituents and Pharmacological Effects of Bryophyllum calycinum. A review

    Directory of Open Access Journals (Sweden)

    Ali Esmail Al-Snafi

    2014-12-01

    Full Text Available Bryophyllum calycinum belongs to the family crassulaceae was widely used in traditional medicine especially in the tropical areas. The plant contained alkaloids, phenols, flavonoids, tannins, anthocyanins, glycosides, bufadienolides, saponins, coumarins, sitosterols, quinines, carotenoids, tocopherol and lectins . The previous pharmacological studies showed that it exerted many pharmacological effects including anticancer , antioxidant immunomodulating , antibacterial , anthelmentic , antiprotozoal , neurologica ( sedative and anticonvulsant , anti-inflammatory , analgesic , diuresis , antiurolithitic , nephroprotective, hepatoprotective , anti-peptic ulcer , hypotensive , antidiabetic , wound healing and other pharmacological effects. The present review was designed to highlight the chemical constituents and pharmacological effects of Bryophyllum calycinum.

  13. El discurso médico a propósito de las fiebres y de la quina en el Tratado de las Calenturas (1751) de Andrés Piquer

    OpenAIRE

    Frías Núñez, Marcelo

    2003-01-01

    In this article we analyze the historical figure of Andrés Piquer, offering a personal analysis about his medical work. We will take as a starting point the 1751 edition of his Tratado de las Calenturas (Treatise on Fever). We will use his allusions to fever and quinine as our two reflexive axes. In this analysis we will also refer to some of his Spanish and European —specially French— contemporaries. We find Piquer clearly compromised with observation and experience as the only basis for med...

  14. Organic cation secretion by Cancer borealis urinary bladder

    Energy Technology Data Exchange (ETDEWEB)

    Miller, D.S.; Holliday, C.W.

    1987-01-01

    In the crab, Cancer borealis, initial clearance studies showed a potent renal excretory system for the model organic cation, tetraethylammonium (TEA). (/sup 14/C)-TEA clearance averaged 145 +/- 32 ml/day, which was 18 times the paired polyethylene glycol clearance. TEA uptake by slices of urinary bladder was concentrative, saturable, inhibitable by N/sup 1/-methylnicotinamide chloride, and dependent on glycolytic, but not oxidative, metabolism. When mounted in flux chambers, bladders exhibited a large net secretory flux. For 0.1 mM TEA, the ratio of secretory to reabsorptive fluxes was 65. Urinary bladders from another crab, Cancer irroratus, and a lobster, Homarus americanus, also exhibited net TEA secretion. In C. borealis bladder, secretory transport was concentrative, saturable, and nearly abolished by addition of 1 mM quinine to the serosol bath. Reabsorptive transport was not concentrative and was not reduced by luminal quinine. The data are consistent with a secretory pathway that is transcellular and mediated by carriers at both the serosal and luminal membranes.

  15. INDUCTION OF DRUG RESISTANCE IN PLASMODIUM FALCIPARUM: AN INTERMITTENT DRUG EXPOSURE METHOD

    Directory of Open Access Journals (Sweden)

    M.Nateghpour

    1998-03-01

    Full Text Available The production of experimentally induced drug resistance in the laboratory provides valuable opportunities for investigators to study the nature and genetics of drug resistance mechanisms to a given agent, patterns of cross resistance and the mode of action of drugs. At the beginning the continuous drug exposure was chosen as a standard procedure to produce drug— resistant strains of P. falciparum,.but later on some other methods were also applied. An intermittent drug exposure method as a novel procedure has been introduced in this study. Intermittent exposure of chloroquine resistant Kl and chloroquine sensitive T9.96 strains of P. falciparum to halofantrine culminated in a relatively rapid reduction in sensitivity to the drug. The response of halofantrifle - resistnat K1HF and T9.96 strains and parent parasites to halofantrifle, inefloquine, quinine and chloroquine was determined. The results indicated that the effectiveness of halofantrine to K1HF and T9.96HF strains decreased 9 and 3 folds respectively, compared to the parent parasites. Cross -resistance occurred among halofantrine. mefloquine and quinine. Halofantrine resistance was associated with enhanced chloroquine sensitivity in the strain derived from chloroquine - resistant K1 strain, hut not in the strain derived from chloroquine - sensitive T9.96 parasites.

  16. Activation of lateral hypothalamus-projecting parabrachial neurons by intraorally delivered gustatory stimuli

    Directory of Open Access Journals (Sweden)

    Kenichi eTokita

    2014-07-01

    Full Text Available The present study investigated a subpopulation of neurons in the mouse parabrachial nucleus (PbN, a gustatory and visceral relay area in the brainstem, that project to the lateral hypothalamus (LH. We made injections of the retrograde tracer Fluorogold (FG into LH, resulting in fluorescent labeling of neurons located in different regions of the PbN. Mice were stimulated through an intraoral cannula with one of seven different taste stimuli, and PbN sections were processed for immunohistochemical detection of the immediate early gene c-Fos, which labels activated neurons. LH projection neurons were found in all PbN subnuclei, but in greater concentration in lateral subnuclei, including the dorsal lateral subnucleus (dl. Fos-like immunoreactivity (FLI was observed in the PbN in a stimulus-dependent pattern, with the greatest differentiation between intraoral stimulation with sweet (0.5 M sucrose and bitter (0.003 M quinine compounds. In particular, sweet and umami-tasting stimuli evoked robust FLI in cells in the dl, whereas quinine evoked almost no FLI in cells in this subnucleus. Double-labeled cells were also found in the greatest quantity in the dl. Overall, these results support the hypothesis that the dl contains direct a projection to the LH that is activated preferentially by appetitive compounds; this projection may be mediated by taste and/or postingestive mechanisms.

  17. Identification by functional MRI of human cerebral region activated by taste stimulation

    Energy Technology Data Exchange (ETDEWEB)

    Kakimoto, Naoya [Osaka Univ. (Japan). Faculty of Dentistry

    2000-09-01

    The purpose of this study was the examination of possible imaging of the primary taste region of human cerebral cortex by functional MRI (fMRI). Subjects were 19-36 years old, healthy adult male and female volunteers given information concerning the purpose, significance and method of the study. MRI equipment was 1.5 T Signa Horizon (GE) with Head Coil. Images were processed by the software FuncTool on the Advantage Windows Workstation (GE). Taste stimulation was done by swab bearing the solution of 4% quinine hydrochloride, 20% sodium chloride or distilled water (control) or by dripping from the syringe of the solutions, 8% tartaric acid or 80% sugar. Preliminary examinations with the swab suggested the possibility of the identification. Further, with use of dripping apparatus, the taste active region was shown to be identified by fMRI and of which area tended to be larger in male than in female: a significant difference was seen for the quinine hydrochloride. As above, the method was suggested to be a diagnostic mean for the taste perception. (K.H.)

  18. The Study of Optimum Extract Method of Effective Components in Zi Cao of Qing Zi Mixture%青紫合剂中紫草有效成分提取的最佳工艺研究

    Institute of Scientific and Technical Information of China (English)

    王晓玲; 张艳菊; 陈博

    2013-01-01

    Objective To investigate the influential factors of extract method of Hydroxy beta quinine in Zi Cao, Method Selecting temperature, alcohol concentration and extracting time as influential factors to make L9(34) Orthogonal test. Result The optimal method of extract of Hydroxy beta quinine in Zi Cao was 95% alcohol, 65 ℃ water bath soak for 4 hours. Conclusion The optimal extract method was stable, feasible and reasonable.%目的 优选紫草中,有效成分羟基萘醌总色素的最佳提取工艺.方法 通过L9 (34)正交试验法,以药材中羟基萘醌总色素的质量分数为评价指标,考察提取温度、溶剂浓度及提取时间3个因素,每个因素选取3个水平进行试验.结果 最佳提取工艺为95%乙醇,65℃水浴温浸4小时.结论 优选得到的工艺稳定、合理、可行.

  19. The Central Reinforcing Properties of Ethanol Are Mediated by Endogenous Opioid Systems: Effects of Mu and Kappa Opioid Antagonists.

    Directory of Open Access Journals (Sweden)

    Norman E. Spear

    2009-09-01

    Full Text Available Endogenous opioid systems are implicated in the reinforcing effects of ethanol and may play a substantial role in modulating the central reinforcing effects of ethanol early in ontogeny. This possibility was explored in the present study through the use of an olfactory conditioning paradigm with centrally administered ethanol serving as an unconditioned stimulus (US. In Experiment 1, newborn rat pups were treated with either a selective mu antagonist CTOP or kappa selective antagonist nor-BNI prior to olfactory conditioning. Experiment 2 tested the effectiveness of an alternative, shorter-duration kappa opioid antagonist GNTI in altering ethanol reinforcement. Experiment 3 investigated whether the effectiveness of pharmacological blockade of opioid receptors was due to the disruption of learning per se using an olfactory aversive conditioning paradigm with intraoral quinine serving as a US. Central administration of either mu or kappa opioid antagonists prior to conditioning disrupted the reinforcing effects of ethanol in newborn rats. The kappa opioid antagonist GNTI was as effective as nor-BNI. These effects of opioid antagonists on ethanol reinforcement are unlikely to be due to a disruption of all types of conditioning, since CTOP did not affect aversive reinforcement to intraoral infusions of quinine. The present results support the hypothesis that in newborn rats, the reinforcing properties of ethanol are mediated by the endogenous activity at mu and kappa opioid receptors.

  20. UK malaria treatment guidelines.

    Science.gov (United States)

    Lalloo, David G; Shingadia, Delane; Pasvol, Geoffrey; Chiodini, Peter L; Whitty, Christopher J; Beeching, Nicholas J; Hill, David R; Warrell, David A; Bannister, Barbara A

    2007-02-01

    Malaria is the tropical disease most commonly imported into the UK, with 1500-2000 cases reported each year, and 10-20 deaths. Approximately three-quarters of reported malaria cases in the UK are caused by Plasmodium falciparum, which is capable of invading a high proportion of red blood cells and rapidly leading to severe or life-threatening multi-organ disease. Most non-falciparum malaria cases are caused by Plasmodium vivax; a few cases are caused by the other two species of Plasmodium: Plasmodium ovale or Plasmodium malariae. Mixed infections with more than 1 species of parasite can occur; they commonly involve P. falciparum with the attendant risks of severe malaria. Management of malaria depends on awareness of the diagnosis and on performing the correct diagnostic tests: the diagnosis cannot be excluded until 3 blood specimens have been examined by an experienced microscopist. There are no typical clinical features of malaria, even fever is not invariably present. The optimum diagnostic procedure is examination of thick and thin blood films by an expert to detect and speciate the malarial parasites; P. falciparum malaria can be diagnosed almost as accurately using rapid diagnostic tests (RDTs) which detect plasmodial antigens or enzymes, although RDTs for other Plasmodium species are not as reliable. The treatment of choice for non-falciparum malaria is a 3-day course of oral chloroquine, to which only a limited proportion of P. vivax strains have gained resistance. Dormant parasites (hypnozoites) persist in the liver after treatment of P. vivax or P. ovale infection: the only currently effective drug for eradication of hypnozoites is primaquine. This must be avoided or given with caution under expert supervision in patients with glucose-6-phosphate dehydrogenase deficiency (G6PD), in whom it may cause severe haemolysis. Uncomplicated P. falciparum malaria can be treated orally with quinine, atovaquone plus proguanil (Malarone) or co-artemether (Riamet

  1. GUSTATORY RESPONSES OF NEURONS IN THE PARABRACHIAL NUCLEUS OF RATS

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    Objective:To investigate the gustatory neural response of the neurons to five basic taste stimuli in the parabrachial nucleus(PBN),Methods:Evoked responses from PBN taste neurons to tastants were recorded using standard extracellular microelectrode technique.Results:46 taste neurons were recorded in PBN,and most of them were broadly responsive.On the basis of their most effective taste stimuli,these taste neurons were classified into five types.Those are NaCl-,HCl-,quinine-sucrose-,and monosodium glutamate(MSG)-best neurons.Except for the quinine-best neurons,the responses of each best-stimulus category to its best stimulus were significantly stronger than those of others(P<0.01),The results of correlation analysis showed that the correlations between sucrose and each of the other 4 tastants were smaller than those among others.Conclusion:The results suggest that PBN taste neurons probably play an important role in discriminating for hedonic taste.

  2. GUSTATORY RESPONSES OF NEURONS IN THE PARABRACHIAL NUCLEUS OF RATS

    Institute of Scientific and Technical Information of China (English)

    黄涛; 闫剑群; 康怡

    2002-01-01

    Objective To investigate the gustatory neural r esponse of the neurons to five basic taste stimuli in the parabrachial nucleus ( PBN). Methods Evoked responses from PBN taste neurons to t astants were recorded using standard extracellular microelectrode technique. Results 46 taste neurons were recorded in PBN, and most of th em were broadly respo nsive. On the basis of their most effective taste stimuli, these taste neurons w ere classified into five types. Those are NaCl-, HCl-, quinine-, sucrose-, and monosodium glutamate (MSG)-best neurons. Except for the quinine-best neur ons, the responses of each best-stimulus category to its best stimulus were sig nificantly stronger than those of others (P<0.01). The results of correlati on analysis showed that the correlations between sucrose and each of the other 4 tastants were smaller than those among others. Conclusion Th e results suggest that PBN taste neurons probably play an important role in disc riminating for hedonic taste.

  3. Changes of Photosystem Ⅱ Electron Transport in the Chlorophyll-deficient Oilseed Rape Mutant Studied by Chlorophyll Fluorescence and Thermoluminescence

    Institute of Scientific and Technical Information of China (English)

    Jun-Wei Guo; Jin-Kui Guo; Yun Zhao; Lin-Fang Du

    2007-01-01

    The photosystem Ⅱ (PSII) complex of photosynthetic membranes comprises a number of chlorophyll-binding proteins that are important to the electron flow. Here we report that the chlorophyll b-deficient mutant has de creased the amount of light-harvesting complexes with an increased amount of some core polypeptides of PSII,including CP43 and CP47. By means of chlorophyll fluorescence and thermoluminescence, we found that the ratio of Fv/Fm, qP and electron transport rate in the chlorophyll b-deficient mutant was higher compared to the wild type.In the chlorophyll b-deficient mutant, the decay of the primary electron acceptor quinones (QA-) reoxidation was decreased, measured by the fluorescence. Furthermore, the thermolumlnescence studies in the chlorophyll b deficient mutant showed that the B band (S2/S3QB-) decreased slightly and shifted up towards higher temperatures.In the presence of dichlorophenyl-dimethylurea, which is inhibited in the electron flow to the second electron acceptor quinines (QB) at the PSII acceptor side, the maximum of the Q band (S2QA-) was decreased slightly and shifted down to lower temperatures, compared to the wild type. Thus, the electron flow within PSll of the chlorophyll b-deficient mutant was down-regulated and characterized by faster oxidation of the primary electron acceptor quinine QA- via forward electron flow and slower reduction of the oxidation S states.

  4. Use of refractometry and colorimetry as field methods to rapidly assess antimalarial drug quality.

    Science.gov (United States)

    Green, Michael D; Nettey, Henry; Villalva Rojas, Ofelia; Pamanivong, Chansapha; Khounsaknalath, Lamphet; Grande Ortiz, Miguel; Newton, Paul N; Fernández, Facundo M; Vongsack, Latsamy; Manolin, Ot

    2007-01-04

    The proliferation of counterfeit and poor-quality drugs is a major public health problem; especially in developing countries lacking adequate resources to effectively monitor their prevalence. Simple and affordable field methods provide a practical means of rapidly monitoring drug quality in circumstances where more advanced techniques are not available. Therefore, we have evaluated refractometry, colorimetry and a technique combining both processes as simple and accurate field assays to rapidly test the quality of the commonly available antimalarial drugs; artesunate, chloroquine, quinine, and sulfadoxine. Method bias, sensitivity, specificity and accuracy relative to high-performance liquid chromatographic (HPLC) analysis of drugs collected in the Lao PDR were assessed for each technique. The HPLC method for each drug was evaluated in terms of assay variability and accuracy. The accuracy of the combined method ranged from 0.96 to 1.00 for artesunate tablets, chloroquine injectables, quinine capsules, and sulfadoxine tablets while the accuracy was 0.78 for enterically coated chloroquine tablets. These techniques provide a generally accurate, yet simple and affordable means to assess drug quality in resource-poor settings.

  5. Analysis of the electrochemical reactivity of natural hemozoin and {beta}-hemozoin in the presence of antimalarial drugs

    Energy Technology Data Exchange (ETDEWEB)

    Esteban Reyes-Cruz, Victor, E-mail: reyescruz16@yahoo.com [Area Academica de Ciencias de la Tierra y Materiales, Instituto de Ciencias Basicas e Ingenieria, Universidad Autonoma del Estado de Hidalgo (Mexico); Urbano Reyes, Gustavo, E-mail: gurbano2003@yahoo.com.mx [Area Academica de Ciencias de la Tierra y Materiales, Instituto de Ciencias Basicas e Ingenieria, Universidad Autonoma del Estado de Hidalgo (Mexico); Veloz Rodriguez, Maria Aurora, E-mail: maveloz70@yahoo.com.mx [Area Academica de Ciencias de la Tierra y Materiales, Instituto de Ciencias Basicas e Ingenieria, Universidad Autonoma del Estado de Hidalgo (Mexico); Imbert Palafox, Jose Luis, E-mail: imbertox@hotmail.com [Area Academica de Medicina, Instituto de Ciencias de la Salud, Universidad Autonoma del Estado de Hidalgo (Mexico)

    2011-11-30

    We report an evaluation of the reactivity of hemozoin (HZ) and {beta}-hemozoin ({beta}-HZ) obtained from the Triatoma Meccus longipennis, alone and in combination with quinine and amodiaquine. Using cyclic voltammetry and carbon paste electrodes, the redox processes that these compounds undergo were analysed. The results indicated that the atom Fe presence, the substance concentration, the drugs existence and the nature of the electrolytic medium are important in the redox processes. The strongest reactivity was for {beta}-HZ from Triatoma, which suggests that cellular molecules are embedded in an oxidising environment due to the presence of {beta}-HZ and indicates that like HZ, {beta}-HZ could be associate with phospholipid bilayers and interfere with their physical and chemical integrity, contributing to membrane breakdown and hyper-oxidation of molecules. It was further observed that when measuring the reactivity of HZ and {beta}-HZ with quinine and amodiaquine, a more oxidative stress was generated between the second one and the {beta}-HZ, which could explain the effectiveness of amodiaquine as a better antimalarial drug. Finally, it was concluded that electrochemical evaluation may be a convenient tool in determining the efficiency of antimalarial drugs and the identification of their redox processes.

  6. Effects of indole alkaloids on multidrug resistance and labeling of P-glycoprotein by a photoaffinity analog of vinblastine.

    Science.gov (United States)

    Beck, W T; Cirtain, M C; Glover, C J; Felsted, R L; Safa, A R

    1988-06-30

    Multidrug resistant cells are characterized by decreased drug accumulation and retention, thought to be mediated by a high molecular weight glycoprotein, P-glycoprotein (P-gp). Agents such as verapamil have been shown to increase anticancer drug cytotoxicity and increase the amount of drug accumulated and retained by such cells. We show here that in addition to verapamil, reserpine, chloroquine, quinine, quinacrine, yohimbine, vindoline, and catharanthine also enhance the cytotoxicity of vinblastine (VLB) in a multidrug resistant, human leukemic cell line, CEM/VLB1K, described here for the first time. These cells express P-gp as a doublet that is photoaffinity labeled by the analog of VLB, N(p-azido-[3-125I]salicyl)-N'-beta-aminoethylvindesine ([125I]NASV). Both reserpine and, to a lesser extent, verapamil, compete with [125I]NASV for binding to P-gp. We also found that chloroquine, quinacrine, vindoline, and catharanthine, each of which enhanced VLB cytotoxicity in CEM/VLB1K cells by 10- to 15-fold, similarly inhibited [125I]NASV labeling of P-gp. However, neither quinine nor yohimbine inhibited this labeling, and the inhibition produced by catharanthine and vindoline was the greatest or exclusively on the lower band of the P-gp doublet. Our results suggest a complex relationship between the ability of a compound to modulate MDR and its ability to compete for binding to P-gp.

  7. Development of a mouse model of ethanol addiction: naltrexone efficacy in reducing consumption but not craving.

    Science.gov (United States)

    Fachin-Scheit, D J; Frozino Ribeiro, A; Pigatto, G; Oliveira Goeldner, F; Boerngen de Lacerda, R

    2006-09-01

    The aim of the present study was validating pharmacologically a mouse model of alcohol addiction. Mice (n = 60) were offered ethanol (5% and 10%) and water in a free choice paradigm consisting of four phases: free choice (10 weeks), withdrawal (2 weeks), re-exposure (2 weeks) and quinine- adulteration (2 weeks). Control mice (n = 10) had access to water. They were housed individually with food ad libitum. The animals' behaviour was evaluated at the beginning of the treatment and during the withdrawal period. After the exposure to the model, mice received i.p. naltrexone (0.0; 0.125; 2.0 and 16.0 mg/kg) or saline. Mice were characterized as: addicted (n = 15, preference for ethanol without reducing intake when ethanol were adulterated with quinine); heavy drinker (n = 14, preference for ethanol but reduced intake when ethanol were adulterated); and light drinker (n = 16, no preference for ethanol). Naltrexone reduced ethanol intake in the heavy and light groups (p effect on water intake. It is discussed that naltrexone may be acting in the positive reinforcing properties of ethanol but does not seem to have anti-craving properties. It was concluded that the addicted mice had a compulsive behavior manifested by the continued ethanol intake even under aversive conditions and under naltrexone treatment suggesting that this model might be useful to study addiction.

  8. Artesunate-induced hemoglobinuria in falciparum malaria

    Directory of Open Access Journals (Sweden)

    Avik Karak

    2016-01-01

    Full Text Available A 26-year-old male got admitted with fever of 103°F with chills and rigor for 6 days. He was diagnosed with Plasmodium falciparum infection by peripheral blood smear examination, later confirmed by polymerase chain reaction analysis. Blood smear showed 2% parasitemia. As the patient was hypotensive, intravenous artesunate was started. Two days later, he reported passing "Coca-Cola"-colored urine. Examination revealed tachycardia, anemia, and mild icterus. Serum free hemoglobin and lactate dehydrogenase was elevated whereas haptoglobin was very low. Urine showed the presence of hemoglobin without red blood cells. Glucose-6-phosphate dehydrogenase assay was normal. Chloroquine, primaquine, and quinine levels in blood were undetectable. There was no evidence of any coinfection. Artesunate was stopped suspecting a causal relationship. Intravenous quinine was started. The urine showed progressive clearance over 3 days, and the patient recovered. The strong temporal association of initiating artesunate and occurrence of hemoglobinuria suggested the possible etiological implication which is not documented before.

  9. [The struggle against malaria in the Ottoman Empire during World War I and the legal regulations made to this end].

    Science.gov (United States)

    Koylu, Zafer; Doğan, Nihal

    2010-01-01

    One of the most important disadvantages of war environmental is infectious diseases. The Ottoman Empire combated infectious diseases in addition to the war because of Balkan wars and afterwards first world war. Because of increasing migrations to Anatolia after Balkan wars spread some epidemic diseases, such as cholera, typhoid fever, plaque, dysentery, syphilis. With the start of the First World War, malaria began to spread within civilian population as well as the military. The population fell from power because of illness and therefore could not process the land tax failed to pay taxes. Founded in 1914 with the fight against epidemic diseases was initiated by the Sıhhiye ministry. Quinine was formed as tablets which was imported from Germany by legal regulation and was distributed to the public by Ziraat Bank. However, malaria epidemic could not be prevented because of long war years, lack of population, insufficiency of the preventive methods and lack of quinine, and about three quarters of the population caught malaria and in four years 412.000 soldiers had malaria and 20.000 of them died despite of measures.

  10. Behavioural differentiation induced by environmental variation when crossing a toxic zone in an amoeba

    Science.gov (United States)

    Kunita, Itsuki; Ueda, Kei-Ichi; Akita, Dai; Kuroda, Shigeru; Nakagaki, Toshiyuki

    2017-09-01

    Organisms choose from among various courses of action in response to a wide variety of environmental conditions and the mechanism by which various behaviours are induced is an open question. Interesting behaviour was recently reported: that a unicellular organism of slime mold Physarum polycephalum known as an amoeba had multiple responses (crossing, returning, etc) when the amoeba encounters a zone with toxic levels of quinine, even under carefully controlled conditions. We here examined this elegant example in more detail to obtain insight into behavioural differentiation. We found that the statistical distribution of passage times across a quinine zone switch from unimodal to bimodal (with peaks corresponding to fast crossing and no crossing) when a periodic light stimulation to modulate a biorhythm in amoeba is applied homogeneously across the space, even under the same level of chemical stimuli. Based on a mathematical model for cell movement in amoeba, we successfully reproduced the stimulation-induced differentiation, which was observed experimentally. These dynamics may be explained by a saddle structure around a canard solution. Our results imply that the differentiation of behavioural types in amoeba is modified step-by-step via the compounding of stimulation inputs. The complex behaviour like the differentiation in amoeba may provide a basis for understanding the mechanism of behaviour selection in higher animals from an ethological perspective.

  11. Antimalarial drug resistance in Bangladesh, 1996-2012.

    Science.gov (United States)

    Haque, Ubydul; Glass, Gregory E; Haque, Waziul; Islam, Nazrul; Roy, Shyamal; Karim, Jahirul; Noedl, Harald

    2013-12-01

    Malaria remains an important health problem in Bangladesh, with approximately 14 million people at risk. Antimalarial drug resistance is a major obstacle to the control of malaria in endemic countries. In 2012, Bangladesh reported an estimated 29 522 malaria episodes, of which 94% were reported as being caused by Plasmodium falciparum. In this study, we reviewed and summarized antimalarial drug resistance data from Bangladesh published until June 2013. We searched published sources for data referring to any type of P. falciparum drug resistance (in vivo, in vitro, or molecular) and found 169 articles published in peer-reviewed journals. Of these, 143 articles were excluded because they did not meet our inclusion criteria. After detailed review of the remaining 26 articles, 14 were selected for evaluation. Published studies indicate that P. falciparum shows varying levels of resistance to chloroquine, mefloquine and sulfadoxine-pyrimethamine. Combination therapy of chloroquine and primaquine has proven ineffective and combinations of sulfadoxine-pyrimethamine with either quinine or chloroquine have also shown poor efficacy. Recent studies indicate that artemisinin derivatives, such as artesunate, remain highly efficacious in treating P. falciparum malaria. Available data suggest that artemisinins, quinine, doxycyline, mefloquine-artesunate and azithromycin-artesunate combination therapy remain efficacious in the treatment of P. falciparum malaria in Bangladesh.

  12. Comparison of the Separation Performances of Cinchona Alkaloid-Based Zwitterionic Stationary Phases in the Enantioseparation of β2- and β3-Amino Acids

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    István Ilisz

    2014-12-01

    Full Text Available The enantiomers of twelve unusual β2- and β3-homoamino acids containing the same side-chains were separated on chiral stationary phases containing a quinine- or quinidine-based zwitterionic ion-exchanger as chiral selector. The effects of the mobile phase composition, the nature and concentration of the acid and base additives and temperature on the separations were investigated. The changes in standard enthalpy, ∆(∆H°, entropy, ∆(∆S°, and free energy, ∆(∆G°, were calculated from the linear van’t Hoff plots derived from the ln α vs. 1/T curves in the studied temperature range (10–50 °C. The values of the thermodynamic parameters depended on the nature of the selectors, the structures of the analytes, and the positions of the substituents on the analytes. A comparison of the zwitterionic stationary phases revealed that the quinidine-based ZWIX(−™ column exhibited much better selectivity for both β2- and β3-amino acids than the quinine-based ZWIX(+™ column, and the separation performances of both the ZWIX(+™ and ZWIX(−™ columns were better for β2-amino acids. The elution sequence was determined in some cases and was observed to be R < S and S < R on the ZWIX(+™ and ZWIX(−™ columns, respectively.

  13. Resistência in vitro de cepas do Plasmodium falciparum isoladas no sul do estado do Pará, em diferentes períodos: emergência de casos de multirresistência

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    A. A. Couto

    1993-03-01

    Full Text Available O presente estudo avalia a resposta de cepas de Plasmodium falciparum às drogas antimaláricas, através de testes in vitro, isoladas em 7 municípios do sul do Estado do Pará. Foram efetuados 69 testes para cloroquina e mefloquina, 62 para amodiaquina e 61 para quinino. Os resultados mostram elevada resistência para cloroquina (71%, relativamente baixa resistência para amodiaquina com (25,8% e para o quinino apenas 8,2%. Mefloquina revela ampla sensibilidade (100%, mas, demonstrando perda da mesma quando comparada em dois períodos distintos. Evidenciou-se também cepas multirresistentes em dois dos municípios estudados.The responses of Plasmodium falciparum to antimalarial drugs were evaluated through the in vitro test using blood sample collected from patients of 7 municipalities of the south of Pará State. Sixty nine microtests for chloroquine and mefloquine, 62 for amodiaquine and 61 for quinine were pet formed. The results showed a high resistance for chloroquine (71%, a relatively low resistance level for amodiaquine (25.8% and little resistance to quinine (8.2%. For mefloquine 100% of sensitivity was found.

  14. Additive effects of flavour-caffeine and flavour-flavour pairings on liking for the smell and flavour of a novel drink.

    Science.gov (United States)

    Yeomans, Martin R; Mobini, Sirous; Chambers, Lucy

    2007-12-05

    Previous research has established that caffeine consumption can reinforce changes in liking for caffeine-paired flavours, while pairing a novel flavour with a liked or dislike taste can also result in enduring changes in liking for the flavour. The present study examined how these two forms of flavour-learning interact. 72 habitual caffeine consumers who liked sweet tastes rated the odour and flavour of a novel tea drink before and after four training sessions where the flavour was paired with either 100 mg caffeine or placebo in one of three flavour contexts: added sweetness (aspartame), bitterness (quinine) or control. The liking for both the odour and flavour of the tea increased after pairing with caffeine regardless of flavour context, while pairing with bitterness reduced flavour liking regardless of the presence of caffeine. Pairing with quinine increased the rated bitterness of the tea odour, and reduced the rated sweetness of the tea flavour, post-training, independent of effects of caffeine. These data suggest that flavour-caffeine and flavour-flavour associations have additive effects on drink liking, while confirming that flavour-flavour associations can alter the immediate sensory experience of a flavour alone.

  15. High School Students Are a Target Group for Fight against Self-Medication with Antimalarial Drugs: A Pilot Study in University of Kinshasa, Democratic Republic of Congo

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    Ramsès Kabongo Kamitalu

    2016-01-01

    Full Text Available Aim. To assess the self-medication against malaria infection in population of Congolese students in Kinshasa, Democratic Republic of Congo (DRC. Methods. A cross-sectional study was carried out in University of Kinshasa, Kinshasa, Democratic Republic of Congo. Medical records of all students with malaria admitted to Centre de Santé Universitaire of University of Kinshasa from January 1, 2008, to April 30, 2008, were reviewed retrospectively. Results. The median age of the patients was 25.4 years (range: from 18 to 36 years. The majority of them were male (67.9%. Artemisinin-based combination treatments (ACTs was the most used self-prescribed antimalarial drugs. However, self-medication was associated with the ingestion of quinine in 19.9% of cases. No case of ingestion of artesunate/artemether in monotherapy was found. All the medicines taken were registered in DRC. In this series, self-prescribed antimalarial was very irrational in terms of dose and duration of treatment. Conclusion. This paper highlights self-medication by a group who should be aware of malaria treatment protocols. The level of self-prescribing quinine is relatively high among students and is disturbing for a molecule reserved for severe disease in Congolese health care policy in management of malaria.

  16. Development of Bitter Taste Sensor Using Ionic-Liquid/Polymer Membranes

    Science.gov (United States)

    Akutagawa, Nobuyuki; Toida, Jinichi; Amano, Yoshihiko; Ikezaki, Hidekazu; Toko, Kiyoshi; Arikawa, Yukihiko

    A taste sensor is composed of several kinds of lipid/polymer membranes as transducers which convert taste information to electric signal. Thus, the role of membranes is very important to detect various taste components. In this paper, we developed novel membranes which specifically respond to quinine that is typical bitter substances. These membranes were composed of hydrophobic ionic liquid such as N, N, N-trimethyl-N-propylammonium bis(trifluoromethansulfonyl)imide, 1-butyl-3-methylimidazolium hexafluorophosphate and 1-butylpyridinium hexafluorophosphate, a plasticizer, 2-nitrophenyl octyl ether and a polymer, polyvinyl chloride. In addition to quinine, they also showed response to both several kinds of alkaloids such as caffeine and strychnine, and non-alkaloid such as phenylthiocarbamide. The order of these responses was equal to that of the tongue glossopharyngeal nerve of flog. Furthermore, there were the other alkaloids which response to these membranes. Especially in these alkaloids, they showed high response to denatonium benzoate and berberin chloride which have a strong bitter taste.

  17. In vitro susceptibility of Plasmodium vivax to antimalarials in Colombia.

    Science.gov (United States)

    Fernández, Diana; Segura, César; Arboleda, Margarita; Garavito, Giovanny; Blair, Silvia; Pabón, Adriana

    2014-11-01

    The in vitro susceptibilities of 30 isolates of Plasmodium vivax to a number of antimalarials (chloroquine [CQ], mefloquine, amodiaquine, quinine, and artesunate [AS]) were evaluated. The isolates came from the region of Urabá in Colombia, in which malaria is endemic, and were evaluated by the schizont maturation test. The 50% inhibitory concentration (IC50) was 0.6 nM (95% confidence interval [CI], 0.3 to 1.0 nM) for artesunate, 8.5 nM (95% CI, 5.6 to 13.0 nM) for amodiaquine, 23.3 nM (95% CI, 12.4 to 44.1 nM) for chloroquine, 55.6 nM (95% CI, 36.8 to 84.1 nM) for mefloquine, and 115.3 nM (95% CI, 57.7 to 230.5 nM) for quinine. The isolates were classified according to whether the initial parasites were mature or immature trophozoites (Tfz). It was found that the IC50s for chloroquine and artesunate were significantly different in the two aforementioned groups (P Colombia, P. vivax continues to be susceptible to antimalarials. This is the first report, to our knowledge, showing in vitro susceptibilities of P. vivax isolates to antimalarials in Colombia.

  18. The benefits of being toxic to deter predators depends on prey body size

    Science.gov (United States)

    Smith, Karen E.; Halpin, Christina G.

    2016-01-01

    Many prey have evolved toxins as a defense against predation. Those species that advertise their toxicity to would-be predators with conspicuous warning signals are known as “aposematic.” Investment in toxicity by aposematically signaling prey is thought to underpin how aversive prey are to predators; increasing toxicity means that predators learn to avoid prey faster and attack them at lower rates. However, predators’ foraging decisions on aposematic prey are determined not only by their toxicity, but also by their nutrient content: predators can trade-off the costs of ingesting toxin with the benefits of acquiring nutrients. Prey body size is a cue that positively correlates with nutrient content, and that varies within and between aposematic species. We predicted that a dose of quinine (known to be toxic to birds) would be a more effective deterrent to avian predators when prey were small compared with when they were large, and that the benefits of possessing toxin would be greater for small-bodied prey. Using an established laboratory protocol of European starlings (Sturnus vulgaris) foraging on mealworms (Tenebrio molitor), we found evidence for increased protection from a dose of quinine for small-bodied compared with large-bodied prey. This shows that larger prey need more toxin to attain the same level of defense as smaller prey, which has implications for the evolution of aposematism and mimicry. PMID:28028378

  19. Bumblebees are not deterred by ecologically relevant concentrations of nectar toxins

    Science.gov (United States)

    Tiedeken, Erin Jo; Stout, Jane C.; Stevenson, Philip C.; Wright, Geraldine A.

    2014-01-01

    Bees visit flowers to collect nectar and pollen that contain nutrients and simultaneously facilitate plant sexual reproduction. Paradoxically, nectar produced to attract pollinators often contains deterrent or toxic plant compounds associated with herbivore defence. The functional significance of these nectar toxins is not fully understood, but they may have a negative impact on pollinator behaviour and health, and, ultimately, plant pollination. This study investigates whether a generalist bumblebee, Bombus terrestris, can detect naturally occurring concentrations of nectar toxins. Using paired-choice experiments, we identified deterrence thresholds for five compounds found in the nectar of bee-pollinated plants: quinine, caffeine, nicotine, amygdalin and grayanotoxin. The deterrence threshold was determined when bumblebees significantly preferred a sucrose solution over a sucrose solution containing the compound. Bumblebees had the lowest deterrence threshold for the alkaloid quinine (0.01 mmol l−1); all other compounds had higher deterrence thresholds, above the natural concentration range in floral nectar. Our data, combined with previous work using honeybees, suggest that generalist bee species have poor acuity for the detection of nectar toxins. The fact that bees do not avoid nectar-relevant concentrations of these compounds likely indicates that it is difficult for them to learn to associate floral traits with the presence of toxins, thus maintaining this trait in plant populations. PMID:24526720

  20. Role of potassium and chloride channel blockers in apoptosis of cardiomyocytes induced by staurosporine%钾、氯离子通道阻断剂对staurosporine诱导心肌细胞凋亡的调节作用

    Institute of Scientific and Technical Information of China (English)

    王晓明; 臧益民; 龚卫琴; 高峰; 李源; 高桥信之; 岡田泰伸

    2004-01-01

    目的:探讨钾、氯离子通道在心肌细胞凋亡过程中的调节作用与Caspase-3激活的关系. 方法:在staurosporine诱导原代培养鼠心肌细胞凋亡模型中,观察钾、氯离子通道阻断剂(Quinine, BaCl2, DIDS和NPPB)对心肌细胞的存活率、DNA片断、Caspase-3活性及细胞膜完整性的影响. 实验分为阴性对照组(无药物处理)、阳性对照组(staurosporine处理)与药物干预组(staurosporine加离子通道阻断剂). 结果:①钾、氯离子通道阻断剂能有效的抑制staurosporine诱导的心肌细胞凋亡. 与阳性对照组(29.8%)相比细胞的成活率在奎宁、氯化钡、DIDS和NPPB组分别是59.7%,47.2%,58.6%和60.7%,均有显著的增加(P<0.01). 相对应的DNA片断电泳显示:Quinine, BaCl2, DIDS和NPPB组均有显著的抑制DNA的降解. ②钾、氯离子通道阻断剂能有效的抑制Caspase-3活性的激活,与阳性对照组(600.4%)相比细胞的Caspase-3活性在Quinine, BaCl2, DIDS和NPPB组分别是184.2%,216.3%,175.6%和221.4%,均有显著的抑制(P<0.01). ③细胞膜完整性实验乳酸脱氢酶水平显示各组中细胞的坏死性死亡小于10%. 结论:在staurosporine诱导的心肌细胞凋亡模型中,钾、氯离子通道阻断剂能有效的抑制Caspase-3激活所介导的心肌细胞凋亡.

  1. The Taste and Smell Protocol in the 2011–2014 US National Health and Nutrition Examination Survey (NHANES): Test–Retest Reliability and Validity Testing

    Science.gov (United States)

    Rawal, Shristi; Hoffman, Howard J.; Honda, Mallory; Huedo-Medin, Tania B.; Duffy, Valerie B.

    2016-01-01

    Introduction The US NHANES 2011–2014 protocol includes a taste and smell questionnaire (CSQ) in home-based interviews and brief assessments in mobile exam centers. We report the short- and longer-term test–retest reliability and validity of this protocol against broader chemosensory measures. Methods A convenience sample of 73 adults (age=39.5±20.8 years) underwent the NHANES protocol at baseline, 2 weeks and 6 months. For taste, participants rated intensities of two tastants (1 M NaCl, 1 mM quinine) applied to the tongue tip and three tastants (1 M NaCl, 1 mM quinine, 0.32 M NaCl) sampled with the whole mouth. Smell function was assessed with a Pocket Smell Test™ (PST; eight-item odor identification test). The CSQ asked about chemosensory problems, distortions, and age-related changes. Broader baseline measurements were a 40-item olfactometer-generated identification task and additional whole-mouth taste intensities (1 M sucrose, 32 mM citric acid, 3.2 mM propylthiouracil). Results Intraclass correlations (ICCs) for NHANES taste measures showed moderate-to-good agreement after 2 weeks and 6 months (ICCs 0.42–0.71). Whole-mouth quinine intensity was significantly correlated with other taste intensities, supporting its utility as a marker for overall taste functioning. Olfactory classification from PSTs agreed for 98.5 % of participants across 2 weeks (κ=0.85; 95 % CI 0.71–0.99) and had good correspondence with the olfactometer task. CSQ items showed good-to-excellent agreement over 6 months (ICCs 0.66–0.90). Conclusions These findings further support that the NHANES chemosensory protocol has moderate-to-good test–retest reliability when administered to healthy, educated adults. Despite being a brief procedure with limited measures, the NHANES taste and smell assessments provided good information when compared to broader measures of taste and smell function. PMID:27833669

  2. Malaria's contribution to World War One - the unexpected adversary.

    Science.gov (United States)

    Brabin, Bernard J

    2014-12-16

    Malaria in the First World War was an unexpected adversary. In 1914, the scientific community had access to new knowledge on transmission of malaria parasites and their control, but the military were unprepared, and underestimated the nature, magnitude and dispersion of this enemy. In summarizing available information for allied and axis military forces, this review contextualizes the challenge posed by malaria, because although data exist across historical, medical and military documents, descriptions are fragmented, often addressing context specific issues. Military malaria surveillance statistics have, therefore, been summarized for all theatres of the War, where available. These indicated that at least 1.5 million solders were infected, with case fatality ranging from 0.2 -5.0%. As more countries became engaged in the War, the problem grew in size, leading to major epidemics in Macedonia, Palestine, Mesopotamia and Italy. Trans-continental passages of parasites and human reservoirs of infection created ideal circumstances for parasite evolution. Details of these epidemics are reviewed, including major epidemics in England and Italy, which developed following home troop evacuations, and disruption of malaria control activities in Italy. Elsewhere, in sub-Saharan Africa many casualties resulted from high malaria exposure combined with minimal control efforts for soldiers considered semi-immune. Prevention activities eventually started but were initially poorly organized and dependent on local enthusiasm and initiative. Nets had to be designed for field use and were fundamental for personal protection. Multiple prevention approaches adopted in different settings and their relative utility are described. Clinical treatment primarily depended on quinine, although efficacy was poor as relapsing Plasmodium vivax and recrudescent Plasmodium falciparum infections were not distinguished and managed appropriately. Reasons for this are discussed and the clinical trial data

  3. [Plasmodium falciparum and Salmonella Typhi co-infection: a case report].

    Science.gov (United States)

    Sümer, Sua; Ural, Gaye; Ural, Onur

    2014-01-01

    Malaria and salmonella infections are endemic especially in developing countries, however malaria and salmonella co-infection is a rare entity with high mortality. The basic mechanism in developing salmonella co-infection is the impaired mobilization of granulocytes through heme and heme oxygenase which are released from haemoglobin due to the breakdown of erythrocytes during malaria infection. Thus, a malaria infected person becomes more susceptible to develop infection with Salmonella spp. In this report a case with Plasmodium falciparum and Salmonella Typhi co-infection was presented. A 23-year-old male patient was admitted to hospital with the complaints of diarrhea, nausea, vomiting, abdominal pain, fatigue and fever. Laboratory findings yielded decreased number of platelets and increased ALT, AST and CRP levels. Since he had a history of working in Pakistan, malaria infection was considered in differential diagnosis, and the diagnosis was confirmed by the detection of P.falciparum trophozoites in the thick and thin blood smears. As he came from a region with chloroquine-resistant Plasmodium, quinine (3 x 650 mg) and doxycycline (2 x 100 mg/day) were started for the treatment. No erythrocytes, parasite eggs or fungal elements were seen at the stool microscopy of the patient who had diarrhoea during admission. No pathogenic microorganism growth was detected in his stool culture. The patient's blood cultures were also taken in febrile periods starting from the time of his hospitalization. A bacterial growth was observed in his blood cultures, and the isolate was identified as S. Typhi. Thus, the patient was diagnosed with P.falciparum and Salmonella Typhi coinfection. Ceftriaxone (1 x 2 g/day, 14 days) was added to the therapy according to the results of antibiotic susceptibility test. With the combined therapy (quinine, doxycycline, ceftriaxone) the fever was taken under control, his general condition improved and laboratory findings turned to normal values

  4. Plastic Membrane Electrodes of Coated Wire Type for Micro Determination of Quininium Cation in Pharmaceutical Tablets

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    Laila A.A. Shatti

    2011-01-01

    Full Text Available Problem statement: Silver and copper all-solid state wire sensor electrodes of quininium cation with different ion exchangers have been prepared and used in pharmaceutical analysis. A comparative study with a reference method is applied in order to investigate the validity of the proposed method for potentiometric analysis of pharmaceutical compounds containing quinine. Approach: A Nernstian equation was proved for all electrodes of quinine in this research. Potentiometric investigations were carried out to identify the characteristic performance of the electrodes, such as the life span, pH effect and effect of the interfering ions. Chemometric and statistical studies of the chemical analysis of quinine in pharmaceutical compounds were applied using different type of electrodes compared to a reference method. Results: A Polyvinyl Chloride (PVC membrane electrodes of silver (Ag and Copper (Cu Coated Wire Electrodes (CWEs were prepared for quininium cation (Qn+. The ion exchangers were ion-pairs and ion associates of Qn+ with different counter-anions, such as reineckate (Rn-, phosphotungstate (PT3- and phosphomolybdate (PM3-. The Qn-CWEs showed a Nernstian response for a maximum 24 h at 25°C, except with that based on Cu- Qn3PM.Conclusion/Recommendations: The ion pair QnRn and the ion associates Qn3PT and Qn3PM are very efficient ion exchangers for the construction of Qn-CWEs. The performance characteristics (life span, pH effect and the selectivity proved that such electrodes can be successfully used for the potentiometric micro-determination of Qn2SO4 in its pharmaceutical preparation. The analytical application showed that the recoveries and relative standard deviation of different Qn-CWEs reveals a high degree of accuracy and precision. In spite of their high accuracy, the F- test conclude the fact that the reference method is usually more precise than proposed method introduced in this study except for Ag-Qn3PM electrode. In

  5. When a good taste turns bad: Neural mechanisms underlying the emergence of negative affect and associated natural reward devaluation by cocaine.

    Science.gov (United States)

    Carelli, Regina M; West, Elizabeth A

    2014-01-01

    An important feature of cocaine addiction in humans is the emergence of negative affect (e.g., dysphoria, irritability, anhedonia), postulated to play a key role in craving and relapse. Indeed, the DSM-IV recognizes that social, occupational and/or recreational activities become reduced as a consequence of repeated drug use where previously rewarding experiences (e.g., food, job, family) become devalued as the addict continues to seek and use drug despite serious negative consequences. Here, research in the Carelli laboratory is reviewed that examined neurobiological mechanisms that may underlie these processes using a novel animal model. Oromotor responses (taste reactivity) were examined as rats learned that intraoral infusion of a sweet (e.g., saccharin) predicts impending but delayed access to cocaine self-administration. We showed that rats exhibit aversive taste reactivity (i.e., gapes/rejection responses) during infusion of the sweet paired with impending cocaine, similar to aversive responses observed during infusion of quinine, a bitter tastant. Critically, the expression of this pronounced aversion to the sweet predicted the subsequent motivation to self-administer cocaine. Electrophysiology studies show that this shift in palatability corresponds to an alteration in nucleus accumbens (NAc) cell firing; neurons that previously responded with inhibition during infusion of the palatable sweet shifted to excitatory activity during infusion of the cocaine-devalued tastant. This excitatory response profile is typically observed during infusion of quinine, indicating that the once palatable sweet becomes aversive following its association with impending but delayed cocaine, and NAc neurons encode this aversive state. We also review electrochemical studies showing a shift (from increase to decrease) in rapid NAc dopamine release during infusion of the cocaine-paired tastant as the aversive state developed, again, resulting in responses similar to quinine

  6. Transient isotachophoretic-electrophoretic separations of lanthanides with indirect laser-induced fluorescence detection.

    Science.gov (United States)

    Church, M N; Spear, J D; Russo, R E; Klunder, G L; Grant, P M; Andresen, B D

    1998-07-01

    Indirect laser-induced fluorescence was used for the detection of several lanthanide species separated by capillary electrophoresis. Quinine sulfate was the fluorescent component of the background electrolyte, and α-hydroxyisobutyric acid was added as a complexing agent to enable the separation of analyte ions that have similar mobilities. The UV lines (333-364 nm) of an argon ion laser were used as the excitation source with a diode array detector for monitoring the fluorescent emission at 442 nm. Electrokinetic injections and transient isotachophoresis were implemented to stack the analyte ions into more concentrated zones. On-line preconcentration factors were determined to be ∼700 and resulted in limits of detection for La(3+), Ce(3+), Pr(3+), Nd(3+), Sm(3+), and Eu(3+) in the low-ppb range (6-11 nM).

  7. Attentional Modulation of Brain Responses to Primary Appetitive and Aversive Stimuli.

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    Brent A Field

    Full Text Available Studies of subjective well-being have conventionally relied upon self-report, which directs subjects' attention to their emotional experiences. This method presumes that attention itself does not influence emotional processes, which could bias sampling. We tested whether attention influences experienced utility (the moment-by-moment experience of pleasure by using functional magnetic resonance imaging (fMRI to measure the activity of brain systems thought to represent hedonic value while manipulating attentional load. Subjects received appetitive or aversive solutions orally while alternatively executing a low or high attentional load task. Brain regions associated with hedonic processing, including the ventral striatum, showed a response to both juice and quinine. This response decreased during the high-load task relative to the low-load task. Thus, attentional allocation may influence experienced utility by modulating (either directly or indirectly the activity of brain mechanisms thought to represent hedonic value.

  8. Alkaloids Induce Programmed Cell Death in Bloodstream Forms of Trypanosomes (Trypanosoma b. brucei

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    Michael Wink

    2008-10-01

    Full Text Available The potential induction of a programmed cell death (PCD in Trypanosoma b. brucei by 55 alkaloids of the quinoline, quinolizidine, isoquinoline, indole, terpene, tropane, steroid, and piperidine type was studied by measuring DNA fragmentation and changes in mitochondrial membrane potential. For comparison, the induction of apoptosis by the same alkaloids in human leukemia cells (Jurkat APO-S was tested. Several alkaloids of the isoquinoline, quinoline, indole and steroidal type (berberine, chelerythrine, emetine, sanguinarine, quinine, ajmalicine, ergotamine, harmine, vinblastine, vincristine, colchicine, chaconine, demissidine and veratridine induced programmed cell death, whereas quinolizidine, tropane, terpene and piperidine alkaloids were mostly inactive. Effective PCD induction (EC50 below 10 µM was caused in T. brucei by chelerythrine, emetine, sanguinarine, and chaconine. The active alkaloids can be characterized by their general property to inhibit protein biosynthesis, to intercalate DNA, to disturb membrane fluidity or to inhibit microtubule formation.

  9. Quantitative visualization of the chemical reacting JET

    Energy Technology Data Exchange (ETDEWEB)

    Okamoto, K.; Arata, Y.; Sasaki, T.; Madarame, H. [Nuclear Engineering Research Laboratory, Tokyo Univ., Tokai, Ibaraki (Japan)

    2000-10-01

    The sodium-water reaction should be precisely evaluated for the safety analysis of the sodium-cooled nuclear power plant. To evaluate these chemical reacting jet, the characteristics of the reaction and the mole fraction distributions of the reacting material should be known. In this study, to evaluate the basic characteristics, two fluid jet and chemical reacting jet was measured by the PIV and DELIF. The new dye pair for the dual emission LIF technique was proposed to measure the pH distribution. The Quinine for pH sensitive dye with blue emission and Rhodamine 6G for non-sensitive dye with orange emission, were excited by the third harmonic of Nd:YAG laser (355nm). The high accurate measurement could be achieved for the range of pH 4.0 to 5.5. The ammonia jet into acetic acid was measured using the proposed dye. The effectiveness of the present method was demonstrated. (author)

  10. In vitro inhibition of Plasmodium falciparum by substances isolated from Amazonian antimalarial plants

    Directory of Open Access Journals (Sweden)

    Valter F de Andrade-Neto

    2007-06-01

    Full Text Available In the present study, a quassinoid, neosergeolide, isolated from the roots and stems of Picrolemma sprucei (Simaroubaceae, the indole alkaloids ellipticine and aspidocarpine, isolated from the bark of Aspidosperma vargasii and A. desmanthum (Apocynaceae, respectively, and 4-nerolidylcatechol, isolated from the roots of Pothomorphe peltata (Piperaceae, all presented significant in vitro inhibition (more active than quinine and chloroquine of the multi-drug resistant K1 strain of Plasmodium falciparum. Neosergeolide presented activity in the nanomolar range. This is the first report on the antimalarial activity of these known, natural compounds. This is also the first report on the isolation of aspidocarpine from A. desmanthum. These compounds are good candidates for pre-clinical tests as novel lead structures with the aim of finding new antimalarial prototypes and lend support to the traditional use of the plants from which these compounds are derived.

  11. Applications of Cerium(Ⅳ) MethanesuIfonate in Organic Synthesis%甲基磺酸铈(Ⅳ)在有机合成中的应用

    Institute of Scientific and Technical Information of China (English)

    郝先库; 张瑞祥; 刘海旺; 王士智

    2011-01-01

    An overview was presented on cerium (Ⅳ) methanesulfonate used in organic synthesis and pharmaceutical intermediate synthesis. It is a effective oxidizing agent for synthesizing aromatic aldehydes or ketones from corresponding alkyl aromatic and polycyclic aromatic aldehydes, ketones, or quinines from corresponding polycyclic aromatic. The products have good yield and high selectivity.%综述了甲基磺酸铈(Ⅳ)氧化有机化合物及其在有机合成和医药中间体合成中的应用,讨论了它在烷基芳香醛、酮和多环芳香醛、酮和醌合成中是一个高效氧化试剂,产品具有高收率和高选择性.

  12. Efficacy comparison between anti-malarial drugs in Africans presenting with mild malaria in the Central Republic of Africa: a preliminary study

    Directory of Open Access Journals (Sweden)

    Nambei W.S.

    2005-03-01

    Full Text Available Drug resistance to Plasmodium falciparum contributes to major health problems in central Africa and, as a consequence, poverty. We have analyzed the efficacy of three currently available antimalarial drugs to treat symptomatic, uncomplicated P. falciparum malaria in semiimmune adults living in Bangui, Central Republic of Africa. 210 consecutive individuals were enrolled in the survey, of which 45 were excluded. Those having received dihydroartemisin proved significantly less parasitemic than those having received quinine per os or sulfadoxin-pyrimethamin (χ2 = 16.93 ; p < 0.05, and 75 % recovered in two days compared to 57 and 44 %, respectively. The 25 % who did not recover benefited from a second cure with dihydroartemisin, which proved 100 % efficient. The most accurate protocol remains to be established by analyzing clinical and parasitological data and taking into account the economics of the country.

  13. Evaluation of the Bitterness-Masking Effect of Powdered Roasted Soybeans

    Directory of Open Access Journals (Sweden)

    Yoshimasa Makita

    2016-06-01

    Full Text Available The masking of bitterness is considered important because many pharmaceutical compounds have a bitter taste. The bitterness-masking effect of powdered roasted soybeans (PRS was investigated using a bitter taste sensor. PRS was revealed to significantly suppress the bitterness of quinine hydrochloride and denatonium benzoate. Furthermore, the bitterness-masking mechanism of PRS extracts was evaluated using dynamic light scattering. These results showed that the extracted suspension consisted of particles that were several hundreds of nanometers in size. Analysis of the PRS extracts by nuclear magnetic resonance spectroscopy indicated that denatonium benzoate was entrapped in the PRS extracts. Thus, PRS may be useful as a bitterness-masking agent in orally administered pharmaceuticals.

  14. Severe human Babesia divergens infection in Norway.

    Science.gov (United States)

    Mørch, K; Holmaas, G; Frolander, P S; Kristoffersen, E K

    2015-04-01

    Human babesiosis is a rare but potentially life-threatening parasitic disease transmitted by ixodid ticks, and has not previously been reported in Norway. We report a case of severe babesiosis that occurred in Norway in 2007. The patient had previously undergone a splenectomy. He was frequently exposed to tick bites in an area endemic for bovine babesiosis in the west of Norway. The patient presented with severe haemolysis and multiorgan failure. Giemsa-stained blood smears revealed 30% parasitaemia with Babesia spp. He was treated with quinine in combination with clindamycin, apheresis, and supportive treatment with ventilatory support and haemofiltration, and made a complete recovery. This is the first case reported in Norway; however Babesia divergens seroprevalence in cattle in Norway is high, as is the risk of Ixodes ricinus tick bite in the general population. Babesiosis should be considered in the differential diagnosis of unexplained febrile haemolytic disease.

  15. Suicide by skull stab wounds: a case of drug-induced psychosis.

    Science.gov (United States)

    Jousset, Nathalie; Rougé-Maillart, Clotilde; Turcant, Alain; Guilleux, Michel; Le Bouil, Anne; Tracqui, Antoine

    2010-12-01

    Suicide by stabbing to the head and/or driving sharp objects into the skull is of extreme rarity. This article reports the case of a 27-year-old man, who committed suicide by multiple knife stabs and cuts to the head, the torso, one shoulder and the forearms. Autopsy showed a perforating wound of the skull and the 10-cm long broken blade of the knife being still embedded in the right temporal lobe of the brain. The deceased had no history of psychiatric illness but was currently treated by mefloquine, a quinine derivative associated with a high rate of psychiatric adverse effects. Toxicological examination confirmed a recent intake of mefloquine together with chloroquine, another antimalarial drug. To our knowledge, this is the first report of a completed suicide with very strong evidence of mefloquine implication. Discussion focuses upon mefloquine-induced psychiatric disorders and highlights the importance of performing toxicological investigations in cases of unusual suicides.

  16. Pengaruh Cairan Pembersih Lumut dan Pupuk Anorganik terhadap Pertumbuhan Tanaman Teh (Camellia Sinensis (L. O. Kuntze Asal Biji Setelah Dipangkas

    Directory of Open Access Journals (Sweden)

    Intan Ratna Dewi Anjarsari

    2015-08-01

    Full Text Available A study examines the effect of moss removal and inorganic fertilizers on the growth of the tea (Camellia sinensis (L. O.Kuntze derived from seed after pruning. This research was conducted at the Research Center of Tea and Quinine in Gambung, Ciwidey.The research was managed using factorial experiment that arranged in Completely Randomized Design 4 x 4 with three replications. The first factor was the concentration of moss removal i.e. 0%, 1%, 2% and 3%. The second factor was the dose of inorganic fertilizer i.e. 100%, 80%, 60% and 40%. The result showed that there was no interaction between moss removal and inorganic fertilizer. In 2 % of moss removal showed the better result than 1% and 3% of moss removal in shoot numbers, shoot fresh weight, shoot dry weight. Inorganic fertilizer with 80% doses showed better result than doses 100%, 60% and 40% in shoot numbers, shoot fresh weight, shoot dry weight.

  17. The history of 20th century malaria control in Peru.

    Science.gov (United States)

    Griffing, Sean M; Gamboa, Dionicia; Udhayakumar, Venkatachalam

    2013-08-30

    Malaria has been part of Peruvian life since at least the 1500s. While Peru gave the world quinine, one of the first treatments for malaria, its history is pockmarked with endemic malaria and occasional epidemics. In this review, major increases in Peruvian malaria incidence over the past hundred years are described, as well as the human factors that have facilitated these events, and concerted private and governmental efforts to control malaria. Political support for malaria control has varied and unexpected events like vector and parasite resistance have adversely impacted morbidity and mortality. Though the ready availability of novel insecticides like DDT and efficacious medications reduced malaria to very low levels for a decade after the post eradication era, malaria reemerged as an important modern day challenge to Peruvian public health. Its reemergence sparked collaboration between domestic and international partners towards the elimination of malaria in Peru.

  18. Anaesthetic management of a patient with hereditary angioedema

    Directory of Open Access Journals (Sweden)

    Nergis Ataol

    2015-12-01

    Full Text Available Hereditary angioedema is a rare autosomal dominant disorder caused by reduced activity of the C1 esterase inhibitor. Patients with hereditary angioedema are clinically characterized by recurrent episodes of swelling of the extremities, face, trunk, airways and abdominal organs. Attacks may occur either spontaneously or following trauma, stress, surgery, infections and hormonal fluctuations. The most common cause of death is asphyxia related to laryngeal edema. Giving C1 esterase inhibitor is the most effective method of treatment. Also fresh frozen plasma, androgen steroids, quinine pathway inhibitors, antifibrinolytics and bradykinin receptor antagonists can be used as treatment. In this paper, the anesthetic management of a patient with hereditary angioedema undergoing inguinal hernia repair surgery is reported.

  19. FIXED DRUG ERUPTION DUE TO METRONIDAZOLE: REVIEW OF LITERATURE AND A CASE REPORT

    Directory of Open Access Journals (Sweden)

    Wahlang JB

    2012-03-01

    Full Text Available Fixed drug eruption (FDE is common type of drug eruption seen in skin clinics. FDE usually occurs within hours of administration of the offending agent. Most commonly implicated are sulphonamides, salicylates, oxyphenbutazones, tetracycline, dapsone, chlordiazepoxide, barbiturates, phenolphthalein, morphine, codeine,quinine and derivatives, phenacetin, erythromycin, griseofulvin, mebendazole, meprobamate etc. We hereby report a case of fixed drug eruption on glans penis due to metronidazole, a nitroimidazole-derivative clinically indicated in trichomoniasis, amebiasis, giardiasis, anaerobic and mixed antibacterial infections. A patientadministered metronidazole IV developed erythematous superficial non-tender ulceration over the glans penis on the second day of treatment with Inj. Metronidazole. A provisional diagnosis of metronidazole induced fixed drug eruption was made, metronidazole inj. was stopped and the patient was managed with Tab. Prednisolone30mg/day tapered over 10 days and Fusidic acid+Betamethasone cream.

  20. An NPF transporter exports a central monoterpene indole alkaloid intermediate from the vacuole.

    Science.gov (United States)

    Payne, Richard M E; Xu, Deyang; Foureau, Emilien; Teto Carqueijeiro, Marta Ines Soares; Oudin, Audrey; Bernonville, Thomas Dugé de; Novak, Vlastimil; Burow, Meike; Olsen, Carl-Erik; Jones, D Marc; Tatsis, Evangelos C; Pendle, Ali; Ann Halkier, Barbara; Geu-Flores, Fernando; Courdavault, Vincent; Nour-Eldin, Hussam Hassan; O'Connor, Sarah E

    2017-01-13

    Plants sequester intermediates of metabolic pathways into different cellular compartments, but the mechanisms by which these molecules are transported remain poorly understood. Monoterpene indole alkaloids, a class of specialized metabolites that includes the anticancer agent vincristine, antimalarial quinine and neurotoxin strychnine, are synthesized in several different cellular locations. However, the transporters that control the movement of these biosynthetic intermediates within cellular compartments have not been discovered. Here we present the discovery of a tonoplast localized nitrate/peptide family (NPF) transporter from Catharanthus roseus, CrNPF2.9, that exports strictosidine, the central intermediate of this pathway, into the cytosol from the vacuole. This discovery highlights the role that intracellular localization plays in specialized metabolism, and sets the stage for understanding and controlling the central branch point of this pharmacologically important group of compounds.

  1. Attentional Modulation of Brain Responses to Primary Appetitive and Aversive Stimuli

    Science.gov (United States)

    Field, Brent A.; Buck, Cara L.; McClure, Samuel M.; Nystrom, Leigh E.; Kahneman, Daniel; Cohen, Jonathan D.

    2015-01-01

    Studies of subjective well-being have conventionally relied upon self-report, which directs subjects’ attention to their emotional experiences. This method presumes that attention itself does not influence emotional processes, which could bias sampling. We tested whether attention influences experienced utility (the moment-by-moment experience of pleasure) by using functional magnetic resonance imaging (fMRI) to measure the activity of brain systems thought to represent hedonic value while manipulating attentional load. Subjects received appetitive or aversive solutions orally while alternatively executing a low or high attentional load task. Brain regions associated with hedonic processing, including the ventral striatum, showed a response to both juice and quinine. This response decreased during the high-load task relative to the low-load task. Thus, attentional allocation may influence experienced utility by modulating (either directly or indirectly) the activity of brain mechanisms thought to represent hedonic value. PMID:26158468

  2. Evaluation of synergistic antimicrobial activity of Cinnamomum zeylancium, Trachyspermum ammi and Syzygium aromaticum

    Directory of Open Access Journals (Sweden)

    R.Reji

    2015-02-01

    Full Text Available Antimicrobial assay of acetone and ethanol extract of Cinnamomum zeylancium, Trachyspermum ammi and Syzygium aromaticum was performed using agar well diffusion method against bacterial culture. (E.coli, P.mirabilis and K.pneumoniae the acetone extract of Cinnamomum zeylancium, ethanol extract of Trachyspermum ammi and acetone extract of Syzygium aromaticum were selected to evaluate the synergistic activity. The activities were combined in the ratio of 1:1:1, 1:2:1 and 1:1:2 (Trachyspermum ammi: Cinnamonum zeylancum: Syzygium aromaticum. Phytochemical analysis was carried out for the ethanol and acetone extract of Cinnamonum zeylancium, Trachyspermum ammi and Syzygium aromaticum, to check the present of carbohydrate, proteins, sterioids, resins, tannins, glycosides, flavonoids, saponins and quinines.

  3. Carl Jung.

    Science.gov (United States)

    Kyle, R A; Shampo, M A

    1978-11-17

    Physicians should be prepared to provide prophylactic medications for travelers to malarious areas and to treat patients with malaria. Chloroquine hydrochloride is the suppressive agent of choice for treatment of mild infections due to all species of malaria except for those due to chloroquine-resistant strains of Plasmodium falciparum. For treatment of severe infections with P falciparum and for treatment of all infections due to chloroquine-resistant strains of P falciparum quinine is the suppressive agent of choice. Chloroquine is also the prophylactic agent of choice for most travelers. To prevent infection with P vivax or P ovale, primaquine must also be given. A RBC glucose-6-phosphate dehydrogenase level should be obtained before administration of primaquine. For prophylaxis of chloroquine-resistant strains of P falciparum, no completely satisfactory regime is presently available in the United States.

  4. Phylogeny predicts the quantity of antimalarial alkaloids within the iconic yellow Cinchona bark (Rubiaceae: Cinchona calisaya)

    DEFF Research Database (Denmark)

    Maldonado Goyzueta, Carla Brenda; Barnes, Christopher James; Cornett, Claus

    2017-01-01

    against herbivores and diseases and accelerate drug discovery. For centuries, Cinchona alkaloids were the primary treatment of malaria. Using Cinchona calisaya as a model, we generated genetic profiles of leaf samples from four plastid (trnL-F, matK, rps16, and ndhF) and one nuclear (ITS) DNA regions from...... twenty-two C. calisaya stands sampled in the Yungas region of Bolivia. Climatic and soil parameters were characterized and bark samples were analyzed for content of the four major alkaloids using HPLC-UV to explore the utility of evolutionary history (phylogeny) in determining variation within species...... of these compounds under natural conditions. A significant phylogenetic signal was found for the content of two out of four major Cinchona alkaloids (quinine and cinchonidine) and their total content. Climatic parameters, primarily driven by changing altitude, predicted 20.2% of the overall alkaloid variation...

  5. Antimalarial Drugs as Immune Modulators: New Mechanisms for Old Drugs.

    Science.gov (United States)

    An, Jie; Minie, Mark; Sasaki, Tomikazu; Woodward, Joshua J; Elkon, Keith B

    2017-01-14

    The best known of the naturally occurring antimalarial compounds are quinine, extracted from cinchona bark, and artemisinin (qinghao), extracted from Artemisia annua in China. These and other derivatives are now chemically synthesized and remain the mainstay of therapy to treat malaria. The beneficial effects of several of the antimalarial drugs (AMDs) on clinical features of autoimmune disorders were discovered by chance during World War II. In this review, we discuss the chemistry of AMDs and their mechanisms of action, emphasizing how they may impact multiple pathways of innate immunity. These pathways include Toll-like receptors and the recently described cGAS-STING pathway. Finally, we discuss the current and future impact of AMDs on systemic lupus erythematosus, rheumatoid arthritis, and devastating monogenic disorders (interferonopathies) characterized by expression of type I interferon in the brain.

  6. Volume regulation in rat pheochromocytoma cultured cells submitted to hypoosmotic conditions.

    Science.gov (United States)

    Delpire, E; Cornet, M; Gilles, R

    1991-02-01

    The mechanisms at work in cell volume regulation have been studied in PC12 cultured cells. Results show, for the first time to our knowledge, that the volume readjustment process occurring after application of a hypoosmotic saline is sensitive to amiloride, IBMX and forskoline. The process is also inhibited by quinine hydrochloride and trifluoperazine. Volume readjustment is concomtant with a decrease in K+ and Cl- intracellular levels. The decrease in K+ level can be related to an assymetrical change in the fluxes in and out of the ion as shown by flux kinetics studies using Rb86. These results are interpreted considering that the control of the activity of the ion channel pathways associated with volume readjustment in PC12 cells may implicate the Ca(2+)-calmodulin - cAMP system.

  7. Perspective for the reproduction of antimalarial drugs in Brazil

    Directory of Open Access Journals (Sweden)

    Benjamin Gilbert

    1992-01-01

    Full Text Available The appears to be no chemical manufacture of antimalarial drugs is Brazil. Technology at laboratory process level has been developed for chloroquine, mefloquine, pyrimethamine and cycloquanil, but not perfected nor scaled-up, largely for economic reasons and market uncertainty. Development of primaquine has been contracted but it will run into the same difficulty. Manufacturing capacity for sulfadoxine was registred in the SDI by Roche. A project to produce artemisinine and its derivates is under way at UNICAMP-CPQBA but is hampered by low content in the plant. Proguanil could be produced easily, but apparently no attempt has been made to do so. Quinine is imported on a large scale mostly for softdrink production. Since malarial treatment falls largely within responsability of the Government health authorities, manufacture of drugs in Brazil will depend on an assured medium-term purchase order made to a potential local manufacturer, since competition in the world market is scarcelyviable at the present moment.

  8. Long-term olfactory memories are stabilised via protein synthesis in Camponotus fellah ants

    DEFF Research Database (Denmark)

    Guerrieri, Fernando Javier; D'Ettorre, Patrizia; Deveaud, J-M.;

    2011-01-01

    of molecular bases of learning and memory. An open question is whether the memories formed upon olfactory learning that are retrievable several days after training are indeed based on de novo protein synthesis. Here, we addressed this question in the ant Camponotus fellah using a conditioning protocol in which......-chain hydrocarbons, one paired with sucrose and the other with quinine solution. Differential conditioning leads to the formation of a long-term memory retrievable at least 72¿h after training. Long-term memory consolidation was impaired by the ingestion of cycloheximide, a protein synthesis blocker, prior...... synthesis, long-term memories are stabilised via protein synthesis. Our behavioural protocol opens interesting research avenues to explore the cellular and molecular bases of olfactory learning and memory in ants....

  9. Medicines and Drugs from Plants

    Science.gov (United States)

    Agosta, William C.

    1997-07-01

    Natural preparations have been used for thousands of ages for a variety of purposes including as medicines, poisons, and psychotropic drugs. The largest grouped of preparations from living organisms are medicines, and historically these have come from plants. Quinine and aspirin are two examples of medicines which were extracted originally from plants. Mind-altering, or psychotropic, drugs come mostly from plants or fungi. In many traditional cultures, sickness and death are attributed to maligned spirits so that medicine and religion become inseparable. Uses of cohohba, snakeplant, coca, and peyote are discussed. The process by which new pharmaceuticals are discovered from natural products is described. The implications of an agreement between a major pharmaceutical company and a country in the tropics are discussed.

  10. Persistent and relapsing babesiosis in immunocompromised patients.

    Science.gov (United States)

    Krause, Peter J; Gewurz, Benjamin E; Hill, David; Marty, Francisco M; Vannier, Edouard; Foppa, Ivo M; Furman, Richard R; Neuhaus, Ellen; Skowron, Gail; Gupta, Shaili; McCalla, Carlo; Pesanti, Edward L; Young, Mary; Heiman, Donald; Hsue, Gunther; Gelfand, Jeffrey A; Wormser, Gary P; Dickason, John; Bia, Frank J; Hartman, Barry; Telford, Sam R; Christianson, Diane; Dardick, Kenneth; Coleman, Morton; Girotto, Jennifer E; Spielman, Andrew

    2008-02-01

    Human babesiosis is a tickborne malaria-like illness that generally resolves without complication after administration of atovaquone and azithromycin or clindamycin and quinine. Although patients experiencing babesiosis that is unresponsive to standard antimicrobial therapy have been described, the pathogenesis, clinical course, and optimal treatment regimen of such cases remain uncertain. We compared the immunologic status, clinical course, and treatment of 14 case patients who experienced morbidity or death after persistence of Babesia microti infection, despite repeated courses of antibabesial treatment, with those of 46 control subjects whose infection resolved after a single course of standard therapy. This retrospective case-control study was performed in southern New England, New York, and Wisconsin. All case patients were immunosuppressed at the time of acute babesiosis, compared with or=6 weeks to achieve cure, including 2 weeks after parasites are no longer detected on blood smear.

  11. Liebig's alkaloid analyses: the uncertain route from content to molecular formulae.

    Science.gov (United States)

    Usselman, Melvyn C

    2003-03-01

    Liebig's 1831 paper that describes a new apparatus for the analysis of organic compounds and the results of several analyses using the apparatus is a justly famous contribution to the evolution of modern chemistry. In this paper, I look at the three separate components of Liebig's combustion apparatus that collect the water, carbon dioxide and nitrogen released by the combustion of six alkaloids. Gravimetric data included in the paper reveal that very accurate results could be obtained for water by absorption in a calcium chloride tube, and even better results for carbon dioxide resulted from use of the Kaliapparat. Volumetric measurement of nitrogen gave very poor results despite Liebig's efforts to improve it. Inaccuracies in nitrogen measurement made consistent construction of accurate molecular formulae for nitrogenous substances impossible, and only fortuitous decisions intended to bring molecular formulae into agreement with measured combining weights gave formulae in agreement with modern ones, as in the case for quinine.

  12. Plasmodium falciparum In Vitro Resistance to Monodesethylamodiaquine, Dakar, Senegal, 2014.

    Science.gov (United States)

    Fall, Bécaye; Madamet, Marylin; Camara, Cheikhou; Amalvict, Rémy; Fall, Mansour; Nakoulima, Aminata; Diatta, Bakary; Diémé, Yaya; Wade, Boubacar; Pradines, Bruno

    2016-05-01

    We successfully cultured 36 Plasmodium falciparum isolates from blood samples of 44 malaria patients admitted to the Hôpital Principal de Dakar (Dakar, Senegal) during August-December 2014. The prevalence of isolates with in vitro reduced susceptibility was 30.6% for monodesethylamodiaquine, 52.8% for chloroquine, 44.1% for mefloquine, 16.7% for doxycycline, 11.8% for piperaquine, 8.3% for artesunate, 5.9% for pyronaridine, 2.8% for quinine and dihydroartemisinin, and 0.0% for lumefantrine. The prevalence of isolates with reduced in vitro susceptibility to the artemisinin-based combination therapy partner monodesethylamodiaquine increased from 5.6% in 2013 to 30.6% in 2014. Because of the increased prevalence of P. falciparum parasites with impaired in vitro susceptibility to monodesethylamodiaquine, the implementation of in vitro and in vivo surveillance of all artemisinin-based combination therapy partners is warranted.

  13. What ailed Goya?

    Science.gov (United States)

    Ravin, J G; Ravin, T B

    1999-01-01

    At age 46, Francisco de Goya (1746-1828) suffered from a severe illness that lasted several months. It caused loss of vision and hearing, tinnitus, disorientation, weakness, abdominal distress, and general malaise. After a few months he recuperated but was left deaf forever. In addition to the physical effects, his emotional health and artwork were affected. The precise cause of this illness has long been debated. One early, but unlikely, hypothesis was that he had syphilis. Later conjectures have included Vogt-Koyanagi-Harada disease and lead toxicity. Cogan's syndrome and vasculitis are additional possibilities, although neither is likely to have been Goya's diagnosis. An infectious disease such as meningitis, encephalitis, or malaria is far more likely. Quinine toxicity (cinchonism) may have complicated the illness.

  14. Saleability of anti-malarials in private drug shops in Muheza, Tanzania

    DEFF Research Database (Denmark)

    Ringsted, Frank M; Massawe, Isolide S; Lemnge, Martha M;

    2011-01-01

    prescription-only anti-malarials, in Muheza town, Tanga Region voluntarily participated from July to December 2009. Qualitative in-depth interviews were conducted with owners or shopkeepers on saleability of anti-malarials, and structured questionnaires provided quantitative data on drugs sales volume. Results......: All surveyed drug shops illicitly sold SP and quinine (QN), and legally amodiaquine (AQ). Calculated monthly sale was 4,041 doses, in a town with a population of 15,000 people. Local brands of SP accounted for 74% of sales volume, compared to AQ (13%), QN (11%) and ACT (2%). Conclusions: In community...... resistance remains high, unregulated SP dispensing to people other than pregnant women runs the risk of eventually jeopardizing the effectiveness of the IPTp strategy. Further studies are recommended to find out barriers for ACT utilization and preference for self-medication and to train private drug...

  15. 探索液相色谱仪最小检测浓度的新方法%Exploring a new method for detecting the minimum detectable concentration of liquid chromatography

    Institute of Scientific and Technical Information of China (English)

    施江焕; 余善成

    2011-01-01

    Based on the different response of naphthalene-Methanol and Quinine sulfateperchloric acid on Ultraviolet/Visible Detector and Fluorescence Detector of liquid chromatography, this paper proposed a new method for detecting the minimum detectable concentration of liquid chromatography which could improve the detection efficiency.%本文利用萘-甲醇与硫酸奎宁-高氯酸溶液在液相色谱仪的紫外/可见光检测器及荧光检测器上的响应差异,提出液相色谱仪最小检测浓度的检测新方法,提高检测效率.

  16. Blood schizontocidal activity of methylene blue in combination with antimalarials against Plasmodium falciparum

    Directory of Open Access Journals (Sweden)

    Garavito G.

    2007-06-01

    Full Text Available Methylene blue (MB is the oldest synthetic antimalarial. It is not used anymore as antimalarial but should be reconsidered. For this purpose we have measured its impact on both chloroquine sensitive and resistant Plasmodium strains. We showed that around 5 nM of MB were able to inhibit 50% of the parasite growth in vitro and that late rings and early trophozoites were the most sensitive stages; while early rings, late trophozoites and schizonts were less sensitive. Drug interaction study following fractional inhibitory concentrations (FIC method showed antagonism with amodiaquine, atovaquone, doxycycline, pyrimethamine; additivity with artemether, chloroquine, mefloquine, primaquine and synergy with quinine. These results confirmed the interest of MB that could be integrated in a new low cost antimalarial combination therapy.

  17. Severe human Babesia divergens infection in Norway

    Directory of Open Access Journals (Sweden)

    K. Mørch

    2015-04-01

    Full Text Available Human babesiosis is a rare but potentially life-threatening parasitic disease transmitted by ixodid ticks, and has not previously been reported in Norway. We report a case of severe babesiosis that occurred in Norway in 2007. The patient had previously undergone a splenectomy. He was frequently exposed to tick bites in an area endemic for bovine babesiosis in the west of Norway. The patient presented with severe haemolysis and multiorgan failure. Giemsa-stained blood smears revealed 30% parasitaemia with Babesia spp. He was treated with quinine in combination with clindamycin, apheresis, and supportive treatment with ventilatory support and haemofiltration, and made a complete recovery. This is the first case reported in Norway; however Babesia divergens seroprevalence in cattle in Norway is high, as is the risk of Ixodes ricinus tick bite in the general population. Babesiosis should be considered in the differential diagnosis of unexplained febrile haemolytic disease.

  18. Fixed drug eruption due to paracetamol

    Directory of Open Access Journals (Sweden)

    Anjali Kushwah

    2013-12-01

    Full Text Available Fixed drug eruption is a common type of drug eruption seen in dermatology OPD’s. Usually it is seen with sulphonamides, salicylates, tetracyclines, oxyphenbutazones, dapsone, barbiturates, phenolphthalein, morphine, codeine, quinine, phenacetin, erythromycin, griseofulvin, mebendazole etc. We hereby report a case of fixed drug eruption due to single dose of oral paracetamol in an otherwise healthy male after one hour of consuming it. A provisional diagnosis of Paracetamol induced fixed drug eruption was made. Paracetamol was stopped and patient advised never to take Paracetamol in future. Patient was managed with prednisolone 10mg /day, cetirizine 10 mg/day, and amoxicillin 500 mg twice a day and mometasone + fusidic acid cream to be applied over the lesions. [Int J Basic Clin Pharmacol 2013; 2(6.000: 833-835

  19. [Pandemic without drama. Influenza vaccination and Asian flu in Germany].

    Science.gov (United States)

    Witte, Wilfried

    2013-01-01

    The history of the 1957/58 Asian flu in Germany is systematically presented for the first time. The focus is on flu vaccination, which is discussed as a yardstick of the perception of the pandemic. International expertise on influenza virology was predominantly based in Anglo-Saxon countries. German microbiologists issued no clear recommendation for preventative vaccination until 1960. Instead, quinine was relied upon as the traditional medicinal prophylaxis. Antibiotics were more frequently administered. In East Germany, little fuss was made over the Asian flu. In line with the authorities' social hygiene orientation, vaccination was accepted as a matter of principle. In the Federal Republic and West Berlin, the population rejected the vaccination largely. It was seen as a scandal that many employees were on sick leave because of the flu, thus adversely affecting the economy.

  20. Synthesis and Characterization of a New Conjugated Polymer Bearing Pyrazole and Thiophene Moieties as Potent NLO Material

    Science.gov (United States)

    Vishnumurthy, K. A.; Adhikari, A. Vasudeva; Sunitha, M. S.; Philip, Reji

    2011-10-01

    In this communication we describe the design and synthesis of a new conjugated polymer (P) carrying 3,4-dialkoxythiophene, 1,3,4 oxadiazole and pyrazole units, from its monomers through condensation polymerization method. The structure of newly synthesized polymer was established by FT-IR, 1H NMR, elemental analysis and gel permeation chromatographic techniques. Further, its electrochemical, linear and nonlinear optical properties of the polymer have been investigated. The optical and electrochemical band gap was found to be 2.39 eV. Z-scan results reveal that the polymer exhibits strong optical limiting behavior due to effective three-photon absorption (3PA). The value of 3PA coefficient was found to be 1.1×10-20 m3/W2, which is comparable to that of good optical limiting materials. The fluorescence quantum yield of the polymer in solution was determined using quinine sulfate as standard and it was found to be 42%.

  1. Attentional Modulation of Brain Responses to Primary Appetitive and Aversive Stimuli.

    Science.gov (United States)

    Field, Brent A; Buck, Cara L; McClure, Samuel M; Nystrom, Leigh E; Kahneman, Daniel; Cohen, Jonathan D

    2015-01-01

    Studies of subjective well-being have conventionally relied upon self-report, which directs subjects' attention to their emotional experiences. This method presumes that attention itself does not influence emotional processes, which could bias sampling. We tested whether attention influences experienced utility (the moment-by-moment experience of pleasure) by using functional magnetic resonance imaging (fMRI) to measure the activity of brain systems thought to represent hedonic value while manipulating attentional load. Subjects received appetitive or aversive solutions orally while alternatively executing a low or high attentional load task. Brain regions associated with hedonic processing, including the ventral striatum, showed a response to both juice and quinine. This response decreased during the high-load task relative to the low-load task. Thus, attentional allocation may influence experienced utility by modulating (either directly or indirectly) the activity of brain mechanisms thought to represent hedonic value.

  2. ANALYSIS OF PHYTOCONSTIUENTS AND CYTOTOXIC ACTIVITIES OF DIFFERENT PARTS OF OCIMUM SANCTUM

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    Sushika Joshi

    2013-09-01

    Full Text Available Phytochemical screening of extracts of Ocimum Sanctum revealed the presence of fatty acids, steroids, triterpenoid, phenolic compound, flavonoid, glycoside, quinines, and carotenoids. β-sitosterol and Ursolic acid were isolated from leaves of the plant by using column chromatography and identification of these compounds were performed with the help of melting points, Co-TLC and spectroscopic techniques such as IR, 1HNMR and 13 CMR. GC-MS of hexane fraction showed presence of pentanal, sotolone, hexane-3-one, hexane-2-ol, caryphyllene, benzene 1,2 di-carbolylic acids, isoeugenol, cavracrol and eugenol compounds. The brine shrimp bio assay showed LC50 value 213.7, 97.72 and 21.87 for hexane, ethyl acetate and methanol extracts of leaves respectively, where as LC50 value 169.84, 141.25 and 151.35 for hexane, ethyl acetate and methanol extracts of stem respectively. All extracts are pharmacologically active.

  3. Effects of Teratogenic Drugs on CYP1A1 Activity in Differentiating Rat Embryo Cells.

    Science.gov (United States)

    Tayeboon, Gh S; Ostad, S N; Nasri, S; Nili-Ahmadabadi, A; Tavakoli, F; Sabzevari, O

    2015-05-01

    CYP1A1, a P450 isoenzyme, is involved in the phase I xenobiotic metabolism including teratogen drugs. In the present study, the ability of teratogens to elevate the embryonic expression of CYP1A1 was examined. Micromass cell cultures prepared from day 13 rat embryo limb buds (LB). LB cells were cultivated and exposed for 5 days to retinoic acid (RA), hydrocortisone (HC), caffeine (CA) and quinine (QN). CYP1A1 protein expression and activity were measured using immunofluorescence staining and ethoxyresorufin O-deethylation (EROD) assay, respectively. The EROD activity increased significantly following LB cells exposure to RA and HC (pteratogens have potency to increase CYP1A1 activity.

  4. Synthesis and photoluminescence behavior of difluoroboron complexes with β-diketone ligands

    Science.gov (United States)

    Wang, Dun-Jia; Kang, Yan-Fang; Fan, Ling; Hu, Yan-Jun; Zheng, Jing

    2013-12-01

    Five new difluoroboron complexes with 4-pyridyl-β-diketones were synthesized and their structures were confirmed by elemental analysis, IR, 1H NMR, ESI-MS and UV-vis spectroscopy. Their photoluminescence behavior was studied in DMF solution and solid state. The quantum yields (Φu) of complexes 2a-2e in DMF solution were measured relative to quinine sulfate and their lifetime values (τ) were calculated according to the luminescence decay curves in the solid state. From these data, the difluoroboron complexes exhibited the excellent photoluminescence properties. Especially, the complexes 2d and 2e displayed the stronger photoluminescence intensity, much higher quantum yield and longer lifetime value as compared to complexes 2a, 2b and 2c. The results indicate that the substituents at the 4-position on benzene ring have a significant impacts on the photoluminescence properties of the difluoroboron complexes.

  5. PENELITIAN OBAT ANTI MALARIA

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    Emiliana Tjitra

    2012-09-01

    Full Text Available Some sensitivity tests of antimalarial drugs had been done by National Institute of Health Research and Development in collaboration with Directorate General of Communicable Disease Control and Environment Health, Naval Medical Research Unit No.2 and Faculty of Medicine University of Indonesia. In-vivo and or in-vitro Plasmodium falciparum multidrug resistance was reported from 11 provinces : Aceh, North Sumatera, Riau, Lampung, West Java, Jakarta (imported case, Central Java, East Kalimantan, South Sulawesi, East Nusa Tenggara and Irian Jaya. Only quinine had a good response for treatment of falciparum malaria resistant to multidrug. R falciparum resistant to mefloquine or halofantrine was found although it was not available in Indonesia yet. Chloroquine prophylaxis using standard dose was still effective in Tanjung Pinang and Central Java. To support the successfulness of treatment in malaria control programme, further studies on alternative antimalaria drugs is needed.

  6. Antimalarial drug discovery: screening of Brazilian medicinal plants and purified compounds.

    Science.gov (United States)

    Krettli, Antoniana Ursine

    2009-02-01

    Malaria is the most important parasitic disease and its control depends on specific chemotherapy, now complicated by Plasmodium falciparum that has become resistant to most commonly available antimalarials. Treatment of the disease requires quinine or drug combinations of artemisinin derivatives and other antimalarials. Further drug resistance is expected. New active compounds need to be discovered. To find new antimalarials from medicinal and randomly collected plants, crude extracts are screened against P. falciparum in cultures and in malaria animal models, following bioassays of purified fractions, and cytotoxicity tests. For antimalarial research, screening medicinal plants is more efficient than screening randomly chosen plants. Biomonitored fractionation allows selection of new active molecules identified as potential antimalarials in multidisciplinary projects in Brazil; no new molecule is available for human testing. The advantages of projects based on ethnopharmacology are discussed.

  7. Formation of environmentally persistent free radicals as the mechanism for reduced catechol degradation on hematite-silica surface under UV irradiation.

    Science.gov (United States)

    Li, Hao; Pan, Bo; Liao, Shaohua; Zhang, Di; Xing, Baoshan

    2014-05-01

    Iron is rich in soils, and is recently reported to form stable complexes with organic free radicals, generating environmentally persistent free radicals (EPFRs). The observation may challenge the common viewpoint that iron is an effective catalyst to facilitate the degradation of various organic chemicals. But no study was specifically designed to investigate the possible inhibited degradation of organic chemicals because of the formation of EPFRs in dry environment. We observed that catechol degradation under UV irradiation was decreased over 20% in silica particles coated with 1% hematite in comparison to uncoated silica particles. Stabilized semiquinone or quinine and phenol radicals were involved in HMT-silica system. EPFR formation was thus the reason for the reduced catechol degradation on HMT-silica surface under UV irradiation at ambient temperature. EPFRs should be incorporated in the studies of organic contaminants geochemical behavior, and will be a new input in their environmental fate modeling.

  8. Micro-RNA detection based on fluorescence resonance energy transfer of DNA-carbon quantum dots probes.

    Science.gov (United States)

    Khakbaz, Faeze; Mahani, Mohamad

    2017-04-15

    Carbon quantum dots have been proposed as an effective platform for miRNA detection. Carbon dots were synthesized by citric acid. The synthesized dots were characterized by dynamic light scattering, UV-Vis spectrophotometry, spectrofluorimetry, transmission electron microscopy and FT-IR spectrophotometry. The fluorescence quantum yield of the synthesized dots was determined using quinine sulfate as the standard. The FAM-labeled single stranded DNA, as sensing element, was adsorbed on dots by π-π interaction. The quenching of the dots fluorescence due to fluorescence resonance energy transfer (FRET) was used for mir 9-1 detection. In the presence of the complementary miRNA, the FRET did not take place and the fluorescence was recovered.

  9. Vibrational Spectroscopic Study of the Cocrystal Products Formed by Cinchona Alkaloids with 5-Nitrobarbituric Acid

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    Harry G. Brittain

    2015-01-01

    Full Text Available X-ray powder diffraction, differential scanning calorimetry, infrared absorption spectroscopy, and Raman spectroscopy have been used to study the phenomenon of cocrystal formation in the molecular complexes formed by 5-nitrobarbituric acid with four cinchona alkaloids. The cocrystal products were found to contain varying degrees of hydration, ranging from no hydration in the nitrobarbiturate-quinidine cocrystal up to a 4.5-hydrate species in the nitrobarbiturate-cinchonine cocrystal. For the nitrobarbiturate cocrystals with cinchonine, cinchonidine, and quinidine, the predominant interaction was with the quinoline ring system of the alkaloid. However, for quinine, the predominant interaction was with the quinuclidine group of the alkaloid. These properties serve to demonstrate the utility of 5-nitrobarbituric acid as a preferred reagent for chemical microscopy, since the differing range of hydrate and structural types would serve to easily differentiate the cinchona alkaloids from each other, even when different compounds contained the same absolute configurations at their dissymmetric centers.

  10. Exogenous Ochronosis

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    Prachi A Bhattar

    2015-01-01

    Full Text Available Exogenous ochronosis (EO is a cutaneous disorder characterized by blue-black pigmentation resulting as a complication of long-term application of skin-lightening creams containing hydroquinone but may also occur due to topical contact with phenol or resorcinol in dark-skinned individuals. It can also occur following the use of systemic antimalarials such as quinine. EO is clinically and histologically similar to its endogenous counterpart viz., alkaptonuria, which, however, exhibits systemic effects and is an inherited disorder. Dermoscopy and in vivo skin reflectance confocal microscopy are noninvasive in vivo diagnostic tools. It is very difficult to treat EO, a cosmetically disfiguring and troubling disorder with disappointing treatment options.

  11. Neurogenic muscle cramps.

    Science.gov (United States)

    Katzberg, Hans D

    2015-08-01

    Muscle cramps are sustained, painful contractions of muscle and are prevalent in patients with and without medical conditions. The objective of this review is to present updates on the mechanism, investigation and treatment of neurogenic muscle cramps. PubMed and Embase databases were queried between January 1980 and July 2014 for English-language human studies. The American Academy of Neurology classification of studies (classes I-IV) was used to assess levels of evidence. Mechanical disruption, ephaptic transmission, disruption of sensory afferents and persistent inward currents have been implicated in the pathogenesis of neurogenic cramps. Investigations are directed toward identifying physiological triggers or medical conditions predisposing to cramps. Although cramps can be self-limiting, disabling or sustained muscle cramps should prompt investigation for underlying medical conditions. Lifestyle modifications, treatment of underlying conditions, stretching, B-complex vitamins, diltiezam, mexiletine, carbamazepine, tetrahydrocannabinoid, leveteracitam and quinine sulfate have shown evidence for treatment.

  12. Managing adverse events associated with vismodegib in the treatment of basal cell carcinoma.

    Science.gov (United States)

    Fife, Kate; Herd, Robert; Lalondrelle, Susan; Plummer, Ruth; Strong, Amy; Jones, Sarah; Lear, John T

    2017-01-01

    Basal cell carcinomas are the most common form of skin cancer. Some develop into advanced cases not suitable for standard therapy. Vismodegib is the first-in-class oral hedgehog pathway inhibitor (which is dysregulated in 90% of basal cell carcinomas), and has demonstrated efficacy for advanced disease in clinical trials. An UK expert panel met to discuss management strategies for adverse events associated with vismodegib (most commonly taste disturbances, muscle cramps and alopecia). Managing patient expectations and implementing treatment breaks were considered important strategies. Quinine was useful to alleviate muscle cramps. For taste disturbances, food swaps alongside dietician referral were suggested. The experts concluded that these common adverse events can be successfully managed to allow optimum treatment duration of vismodegib.

  13. In vitro action of antiparasitic drugs, especially artesunate, against Toxoplasma gondii

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    Thaís Cobellis Gomes

    2012-08-01

    Full Text Available INTRODUCTION: Toxoplasmosis is usually a benign infection, except in the event of ocular, central nervous system (CNS, or congenital disease and particularly when the patient is immunocompromised. Treatment consists of drugs that frequently cause adverse effects; thus, newer, more effective drugs are needed. In this study, the possible activity of artesunate, a drug successfully being used for the treatment of malaria, on Toxoplasma gondii growth in cell culture is evaluated and compared with the action of drugs that are already being used against this parasite. METHODS: LLC-MK2 cells were cultivated in RPMI medium, kept in disposable plastic bottles, and incubated at 36ºC with 5% CO2. Tachyzoites of the RH strain were used. The following drugs were tested: artesunate, cotrimoxazole, pentamidine, pyrimethamine, quinine, and trimethoprim. The effects of these drugs on tachyzoites and LLC-MK2 cells were analyzed using nonlinear regression analysis with Prism 3.0 software. RESULTS: Artesunate showed a mean tachyzoite inhibitory concentration (IC50 of 0.075µM and an LLC MK2 toxicity of 2.003µM. Pyrimethamine was effective at an IC50 of 0.482µM and a toxicity of 11.178µM. Trimethoprim alone was effective against the in vitro parasite. Cotrimoxazole also was effective against the parasite but at higher concentrations than those observed for artesunate and pyrimethamine. Pentamidine and quinine had no inhibitory effect over tachyzoites. CONCLUSIONS: Artesunate is proven in vitro to be a useful alternative for the treatment of toxoplasmosis, implying a subsequent in vivo effect and suggesting the mechanism of this drug against the parasite.

  14. Acute kidney injury in a shepherd with severe malaria: a case report

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    Boushab BM

    2016-10-01

    Full Text Available Boushab Mohamed Boushab,1 Fatim-Zahra Fall-Malick,2 Mamoudou Savadogo,3 Leonardo Kishi Basco,4 1Department of Internal Medicine, Aïoun Regional Hospital, Hodh El Gharbi, Mauritania; 2National Institute of Hepatology-Virology in Nouakchott, School of Medicine, Nouakchott, Mauritania; 3Department of Infectious Diseases, University Teaching Hospital Yalgado Ouédrago, Ouagadougou, Burkina Faso; 4Research Unit of Infectious and Tropical Diseases, Institut de Recherche pour le Développement (Research Institute for Development, Aix-Marseille University, Marseille, France Abstract: Malaria is one of the main reasons for outpatient consultation and hospitalization in Mauritania. Although four Plasmodium species, ie, Plasmodium (P. falciparum, P. vivax, P. malariae, and P. ovale, cause malaria in Mauritania, recent data on their frequency is ­lacking. Since infections with P. falciparum generally result in serious disease, their identification is important. We report a case of oliguric renal injury associated with malaria in a 65-year-old shepherd. Clinical manifestations included anemia, oliguria, and elevated creatinine and urea. The rapid diagnostic test for malaria and microscopic examination of blood smears were positive for P. falciparum. On the basis of this, the patient was diagnosed as having acute kidney injury as a complication of severe malaria. The patient was treated for malaria with intravenous quinine for 4 days, followed by 3 days of oral treatment. Volume expansion, antipyretic treatment, and diuretics were administered. He also had two rounds of dialysis after which he partially recovered renal function. This outcome is not always the rule. Prognosis depends much on early diagnosis and appropriate supportive treatment. Keywords: malaria, oliguric kidney injury, shepherd, quinine, dialysis

  15. Increased Expression of P-Glycoprotein Is Associated With Chlorpyrifos Resistance in the German Cockroach (Blattodea: Blattellidae).

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    Hou, Weiyuan; Jiang, Chu; Zhou, Xiaojie; Qian, Kun; Wang, Lei; Shen, Yanhui; Zhao, Yan

    2016-09-15

    A principal method for control of the German cockroach, Blattella germanica (L.), is the broad-spectrum organophosphorus insecticide, chlorpyrifos (O,O-diethyl O-3,5,6-trichloro-2-pyridyl phosphorothioate); however, extensive and repeated application has resulted in the development of resistance to chlorpyrifos in this insect. Evidence suggests that ATP-binding cassette protein transporters, including P-glycoprotein, are involved in insecticide resistance. However, little is known of the role of P-glycoprotein in insecticide resistance in the German cockroach. Here, we developed a chlorpyrifos-resistant strain of German cockroach and investigated the relationship between P-glycoprotein and chlorpyrifos resistance using toxicity assays; inhibition studies with two P-glycoprotein inhibitors, verapamil and quinine; P-glycoprotein-ATPase activity assays; and western blotting analysis. After 23 generations of selection from susceptible strain cockroaches, we obtained animals with high resistance to chlorpyrifos. When P-glycoprotein-ATPase activity was inhibited by verapamil and quinine, we observed enhanced susceptibility to chlorpyrifos in both control and chlorpyrifos-resistant cockroaches. No significant alterations of P-glycoprotein expression or ATPase activity were observed in cockroaches acutely exposed to LD50 doses of chlorpyrifos for 24 h, while P-glycoprotein expression and ATPase activity were clearly elevated in the chlorpyrifos-resistant cockroach strain. Thus, we conclude that P-glycoprotein is associated with chlorpyrifos resistance in the German cockroach and that elevated levels of P-glycoprotein expression and ATPase activity may be an important mechanism of chlorpyrifos resistance in the German cockroach.

  16. [Treatment of fulminant falciparum malaria with erythrapheresis].

    Science.gov (United States)

    Rouvier, B; Maudan, P; Debue, J F; Joussemet, M; Roué, R

    1988-01-01

    Ten days after his return from Cameroon, a twenty-six year old Frenchman, serving on voluntary service overseas, presented with fulminant falciparum malaria: shock, altered consciousness, haemolytic anaemia, threatening disseminated coagulation (platelets less than 150 X 10(-6).l-1; prothrombin time and Stuart factor less than 50%; fibrinogen less than 1.5 g.l-1). In spite of quinine therapy, parasitaemia increased from 4 to 35% within 24 h. Using an Haemonetics V50, the exchange of one and a half red blood cell masses was carried out with 17 red blood cell packs. Calcium gluconate was used to prevent the hypocalcaemia induced by the anticoagulant solution. The patient's platelets and plasma were completely reinjected. The result was very satisfactory. This kind of exchange, well tolerated clinically and biologically, would seem better than the classical exchange transfusion. When 10% of the red blood cells are infected by Plasmodium falciparum, it is necessary to exchange from one and a half to two blood masses. Lesser exchanges are always associated with important relapses and quinine therapy must be carried on during and after the exchange. Restricting this exchange only to red blood cells enabled the patient to benefit from his own coagulation factors, antibodies and platelets, and consequently to reduce the number of blood donors involved. However, metabolites (especially bilirubin and circulating immune complexes) were not eliminated. Partial plasmapheresis may be associated with erythropheresis using human albumin as plasma substitute. This technique needs to be assessed, in order to optimize immediate efficiency and post-transfusion infectious risk.

  17. Vaginal contraceptives still evolving.

    Science.gov (United States)

    Pearson, R M

    1986-01-01

    The effort to develop vaginal contraceptives began in the distant past and is still underway today. 1000 years ago, South American Indians inserted into the vagina bark strips impregnated with quinine. In medieval times women used vaginal inserts of cloth soaked in honey or vinegar. Quinine pessaries were introduced into Europe in the late 1800s, and in the early 1900s investigators began to study the effects of various chemicals on sperm motility. Following World War II, surfactant spermicides which disrupt the sperm membrane were developed and marketed. Many of these preparations contained nonoxynol-9. Currently, the D-isomer of propranolol is being examined as a spermicidal contraceptive, and several bacteriocides, e.g., benzalkonium and chlorhexidine, are being developed as spermicides which reduce the penetrability of cervical mucus. Other chemicals being investigated act by inhibiting the acrosome reaction. Advantages of vaginal contraceptives are that they are inexpensive, reversible, and relatively safe and easy to use. Generally they require no medical intervention or supervision. In addition, spermicides may kill or inhibit the growth of organisms responsible for sexually transmitted diseases. Disadvantages of spermicides are that they are generally less effective than many other methods, some interfere with sexual spontaneity, they may cause local irritations, and some women find them messy to use. Recently, concerns were expressed about the possible teratogenic effects of sperimicides. Most of these concerns proved to be unfounded. Given the many new avenues of research, the major disadvantage of sperimicides, i.e., their high failure rates, may be minimized in the near future.

  18. Quality of anti-malarial drugs provided by public and private healthcare providers in south-east Nigeria

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    Uzochukwu Benjamin

    2009-02-01

    Full Text Available Abstract Background There is little existing knowledge about actual quality of drugs provided by different providers in Nigeria and in many sub-Saharan African countries. Such information is important for improving malaria treatment that will help in the development and implementation of actions designed to improve the quality of treatment. The objective of the study was to determine the quality of drugs used for the treatment of malaria in a broad spectrum of public and private healthcare providers. Methods The study was undertaken in six towns (three urban and three rural in Anambra state, south-east Nigeria. Anti-malarials (225 samples, which included artesunate, dihydroartemisinin, sulphadoxine-pyrimethamine (SP, quinine, and chloroquine, were either purchased or collected from randomly selected providers. The quality of these drugs was assessed by laboratory analysis of the dissolution profile using published pharmacopoeial monograms and measuring the amount of active ingredient using high performance liquid chromatography (HPLC. Findings It was found that 60 (37% of the anti-malarials tested did not meet the United States Pharmacopoeia (USP specifications for the amount of active ingredients, with the suspect drugs either lacking the active ingredients or containing suboptimal quantities of the active ingredients. Quinine (46% and SP formulations (39% were among drugs that did not satisfy the tolerance limits published in USP monograms. A total of 78% of the suspect drugs were from private facilities, mostly low-level providers, such as patent medicine dealers (vendors. Conclusion This study found that there was a high prevalence of poor quality drugs. The findings provide areas for public intervention to improve the quality of malaria treatment services. There should be enforced checks and regulation of drug supply management as well as stiffer penalties for people stocking substandard and counterfeit drugs.

  19. Effect of genetic polymorphism on the inhibition of dopamine formation from p-tyramine catalyzed by brain cytochrome P450 2D6.

    Science.gov (United States)

    Niwa, Toshiro; Shizuku, Marina; Yamano, Kaori

    2017-04-15

    The inhibitory effects of steroid hormones, including glucocorticoids such as cortisol, and related compounds on dopamine formation from p-tyramine, catalyzed by cytochrome P450 (CYP) 2D6.2 (Arg296Cys, Ser486Thr) and CYP2D6.10 (Pro34Ser, Ser486Thr) were compared with the effects of those catalyzed by CYP2D6.1 (wild type), to investigate the effect of a CYP2D6 polymorphism on neuroactive amine metabolism in the brain. Inhibition constants (Ki) or 50% inhibitory concentrations of six steroid hormones (cortisol, cortisone, corticosterone, dehydroepiandrosterone, progesterone, and pregnenolone) and quinidine and quinine-typical potent inhibitors of the human CYP2D6 and rat CYP2D subfamily, respectively-toward dopamine formation catalyzed by CYP2D6.1, CYP2D6.2, and CYP2D6.10 expressed in recombinant Escherichia coli were compared. Although most steroid hormones had no or minor inhibitory effects on the dopamine formation by all CYP2D6 variants, progesterone inhibited the metabolism and Ki value against CYP2D6.10 was approximately twice that for CYP2D6.1 and CYP2D6.2. Quinidine exhibited stronger inhibition than quinine; however, these two compounds inhibited the CYP2D6.10-mediated reaction more weakly than the CYP2D6.1 and CYP2D6.2 reactions. These results suggest that CYP2D6 polymorphism would affect drug interaction through dopamine formation in the brain. Copyright © 2017 Elsevier Inc. All rights reserved.

  20. Differential effects of bitter compounds on the taste transduction channels TRPM5 and IP3 receptor type 3.

    Science.gov (United States)

    Gees, Maarten; Alpizar, Yeranddy A; Luyten, Tomas; Parys, Jan B; Nilius, Bernd; Bultynck, Geert; Voets, Thomas; Talavera, Karel

    2014-05-01

    Transient receptor potential cation channel subfamily M member 5 (TRPM5) is a Ca(2+)-activated nonselective cation channel involved in the transduction of sweet, bitter, and umami tastes. We previously showed that TRPM5 is a locus for the modulation of taste perception by temperature changes, and by quinine and quinidine, 2 bitter compounds that suppress gustatory responses. Here, we determined whether other bitter compounds known to modulate taste perception also affect TRPM5. We found that nicotine inhibits TRPM5 currents with an effective inhibitory concentration of ~1.3mM at -50 mV. This effect may contribute to the inhibitory effect of nicotine on gustatory responses in therapeutic and experimental settings, where nicotine is often employed at millimolar concentrations. In addition, it implies the existence of a TRPM5-independent pathway for the detection of nicotine bitterness. Nicotine seems to act from the extracellular side of the channel, reducing the maximal whole-cell conductance and inducing an acceleration of channel closure that leads to a negative shift of the activation curve. TRPM5 currents were unaffected by nicotine's metabolite cotinine, the intensive sweetener saccharin or by the bitter xanthines caffeine, theobromine, and theophylline. We also tested the effects of bitter compounds on another essential element of the sweet taste transduction pathway, the type 3 IP3 receptor (IP3R3). We found that IP3R3-mediated Ca(2+) flux is slightly enhanced by nicotine, not affected by saccharin, modestly inhibited by caffeine, theobromine, and theophylline, and strongly inhibited by quinine. Our results demonstrate that bitter compounds have differential effects on key elements of the sweet taste transduction pathway, suggesting for heterogeneous mechanisms of bitter-sweet taste interactions.

  1. Efficacy of plant extracts in controlling wheat leaf rust disease caused by Puccinia triticina

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    Yasser M. Shabana

    2017-03-01

    Full Text Available The efficacy of eight plant extracts (garlic, clove, garden quinine, Brazilian pepper, anthi mandhaari, black cumin, white cedar and neem in controlling leaf rust disease of wheat was investigated in vitro and in vivo. In vitro, all treatments inhibited spore germination by more than 93%. Neem extract recorded 98.99% inhibition of spore germination with no significant difference from the fungicide Sumi-8 (100%. Under greenhouse conditions, seed soaking application in neem extract (at concentration of 2 ml/L resulted in 36.82% reduction in the number of pustules/leaf compared with the untreated control. Foliar spraying of plant extracts on wheat seedlings decreased the number of pustules/leaf. Foliar spraying of plant extracts four days after inoculation led to the highest resistance response of wheat plants against leaf rust pathogen. Spray application of wheat seedlings with neem, clove and garden quinine extracts, four days after inoculation with leaf rust pathogen completely prevented rust development (100% disease control and was comparable with the fungicide Sumi-8. Foliar spray application of wheat plants at mature stage with all plant extracts has significantly reduced the leaf rust infection (average coefficient of infection, ACI compared with the untreated control and neem was the most effective treatment. This was reflected on grain yield components, whereas the 1000-kernel weight and the test weight were improved whether under one- or two-spray applications, with two-spray application being more effective in this regard. Thus, it could be concluded that plant extracts may be useful to control leaf rust disease in Egypt as a safe alternative option to chemical fungicides.

  2. Functional and molecular identification of a TASK-1 potassium channel regulating chloride secretion through CFTR channels in the shark rectal gland: implications for cystic fibrosis.

    Science.gov (United States)

    Telles, Connor J; Decker, Sarah E; Motley, William W; Peters, Alexander W; Mehr, Ali Poyan; Frizzell, Raymond A; Forrest, John N

    2016-12-01

    In the shark rectal gland (SRG), apical chloride secretion through CFTR channels is electrically coupled to a basolateral K(+) conductance whose type and molecular identity are unknown. We performed studies in the perfused SRG with 17 K(+) channel inhibitors to begin this search. Maximal chloride secretion was markedly inhibited by low-perfusate pH, bupivicaine, anandamide, zinc, quinidine, and quinine, consistent with the properties of an acid-sensitive, four-transmembrane, two-pore-domain K(+) channel (4TM-K2P). Using PCR with degenerate primers to this family, we identified a TASK-1 fragment in shark rectal gland, brain, gill, and kidney. Using 5' and 3' rapid amplification of cDNA ends PCR and genomic walking, we cloned the full-length shark gene (1,282 bp), whose open reading frame encodes a protein of 375 amino acids that was 80% identical to the human TASK-1 protein. We expressed shark and human TASK-1 cRNA in Xenopus oocytes and characterized these channels using two-electrode voltage clamping. Both channels had identical current-voltage relationships (outward rectifying) and a reversal potential of -90 mV. Both were inhibited by quinine, bupivicaine, and acidic pH. The pKa for current inhibition was 7.75 for shark TASK-1 vs. 7.37 for human TASK-1, values similar to the arterial pH for each species. We identified this protein in SRG by Western blot and confocal immunofluorescent microscopy and detected the protein in SRG and human airway cells. Shark TASK-1 is the major K(+) channel coupled to chloride secretion in the SRG, is the oldest 4TM 2P family member identified, and is the first TASK-1 channel identified to play a role in setting the driving force for chloride secretion in epithelia. The detection of this potassium channel in mammalian lung tissue has implications for human biology and disease.

  3. Home-based malaria management in children by women: Evidence from a malaria endemic community in sub-Saharan Africa

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    Doreen Nkiru Eugene-Ezebilo

    2015-07-01

    Full Text Available Objective: To examine the medicines and dosage that mothers who engage in home-based malaria management administer to children aged ≤ 5 years having signs and symptoms associated with malaria and to discuss the possibilities of designing an effective home-based malaria management strategy. Methods: The data were obtained from face-to-face semi-structured interviews conducted with mothers in the Ugbowo Community of Benin City, Nigeria who were selected using multistage systematic random sampling technique. The data were analyzed by qualitative content analysis, arithmetic mean, simple percentages and bar chart. Results: Approximately 90% of the interviewees engaged in home-based malaria management and 10% patronized the hospital. Most of the interviewees who engaged in home-based malaria management administered medicines that stimulates the production of red blood cells and supplies vitamins to children having signs and symptoms of malaria, followed by painkillers and anti-malaria and cough medicine was the least. Of the anti-malaria medicines administered to children, almost 80% of the interviewees administered chloroquine to children, 15% quinine and 3% halfan. Approximately 60% of the interviewees had the correct knowledge of the dosage regime for chloroquine, 38% for quinine and 9% for halfan. Conclusions: Although home-based malaria management is important, it cannot serve as a substitute to the hospital. Some diseases have signs and symptoms that are similar to that of malaria which implies that administering anti-malaria medicines to a child without confirmatory tests might lead to irredeemable complications in that child. If the strategy is to make home-based malaria management effective and sustainable mothers, community health officials should be involved in designing the strategy. Simple rapid diagnostic test kits for malaria should be made available to community health officials and pharmacists so that confirmatory tests could be

  4. Envolvimento renal na associação salmonella-Schistosoma mansoni

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    José Roberto Lambertucci

    1987-06-01

    Full Text Available Vinte pacientes com a associação Salmonella-S. mansoni (Grupo 1 e 20 com esquistossomose mansoni hepatesplênica (Grupo 2 foram selecionados para o estudo. Submeteram-se os pacientes dos Grupos le 2 a exame clínico minucioso e a uma série de exames complementares, com destaque para as provas de função renal. Em 10 pacientes do Grupo 1 e 20 do Grupo 2, realizou-se, ainda, estudo histológico do rim à microscopia óptica, de fluorescência e eletrônica. As alterações renais foram mais freqüentes nos pacientes do Grupo 1. Após o tratamento dos pacientes do Grupo 1, com antibióticos e/ou esquistossomicidas, observou-se regressão das alterações renais sob o ponto de vista clínico, laboratorial e imunopatológico. Os autores concluem pela existência de duas nefropatias distintas: a nefropatia esquistossomótica e a encontrada em pacientes com a associação Salmonella-S. mansoni.The responses of Plasmodium falciparum to antimalarial drugs were evaluated through the in vitro test using blood sample collected from patients of 7 municipalities of the south of Pará State. Sixty nine microtests for chloroquine and mefloquine, 62 for amodiaquine and 61 for quinine were pet formed. The results showed a high resistancefor chloroquine (71%, a relatively low resistance level for amodiaquine (25.8% and little resistance to quinine (8.2%. For mefloquine 100% of sensitivity wasfound.

  5. Longitudinal in vitro surveillance of Plasmodium falciparum sensitivity to common anti-malarials in Thailand between 1994 and 2010

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    Parker Daniel

    2012-08-01

    Full Text Available Abstract Background Drug and multidrug-resistant Plasmodium falciparum malaria has existed in Thailand for several decades. Furthermore, Thailand serves as a sentinel for drug-resistant malaria within the Greater Mekong sub-region. However, the drug resistance situation is highly dynamic, changing quickly over time. Here parasite in vitro drug sensitivity is reported for artemisinin derivatives, mefloquine, chloroquine and quinine, across Thailand. Methods Blood was drawn from patients infected with P. falciparum in seven sentinel provinces along Thai international borders with Cambodia, Myanmar, Laos, and Malaysia. In vitro parasite sensitivity was tested using the World Health Organization’s microtest (mark III (between 1994 and 2002 and the histidine-rich protein-2 (HRP2-based enzyme-linked immunosorbent assay (in 2010. Following World Health Organization protocol, at least 30 isolates were collected for each province and year represented in this study. Where possible, t-tests were used to test for significant differences. Results There appears to be little variation across study sites with regard to parasite sensitivity to chloroquine. Quinine resistance appears to have been rising prior to 1997, but has subsequently decreased. Mefloquine sensitivity appears high across the provinces, especially along the north-western border with Myanmar and the eastern border with Cambodia. Finally, the data suggest that parasite sensitivity to artemisinin and its derivatives is significantly higher in provinces along the north-western border with Myanmar. Conclusions Parasite sensitivity to anti-malarials in Thailand is highly variable over time and largely mirrors official drug use policy. The findings with regard to reduced sensitivity to artemisinin derivatives are supported by recent reports of reduced parasite clearance associated with artemisinin. This trend is alarming since artemisinin is considered the last defence against malaria. Continued

  6. Glycerol gelatin for 3D-printing of implants using a paste extrusion technique

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    Kempin Wiebke

    2017-09-01

    Full Text Available Fused deposition modeling as an additive manufacturing technique has gained great popularity for the fabrication of medical devices as well as pharmaceutical dosage forms over the last years. Particularly the variety of geometries that can be printed determines the attractiveness of this technique enabling a shape adaption of e.g. implants. In the presented work the soft hydrogel material glycerol gelatin was investigated towards its applicability in 3D-printing as an alternative to the commonly applied and mostly rigid polyesters. Model implants loaded with the model drug quinine and with the shape of a hollow cylinder were printed via an extrusion based technique utilizing the piston feed in a hydrogel filled heatable syringe. Glycerol gelatin hydrogels need to be crosslinked to avoid gel-sol-transition at body temperature. For this purpose three different crosslinking methods (insertion, dipping, spraying with 1-ethyl-3-(3-dimethylaminopropyl carbodiimide (EDC and N-hydroxysuccinimide (NHS were evaluated regarding their crosslinking efficiency and drug losses during the crosslinking process. Dipping of the implant into an aqueous solution with at least 50 mM EDC and 10 mM NHS was found to be the most efficient crosslinking technique in conjunction with a smaller drug loss during processing compared to inserting. However, the use of hydrogels also causes problems as an intense and highly variable swelling of the printed structures during crosslinking (120.7 % ± 11.9 % for 10 times dipping in 50mM EDC/10 mM NHS and a great dependency of the volume on storage conditions complicate the preparation of tailor-made implants. The release of the model drug quinine from printed and crosslinked implants was fast and nearly completed within 6 hours.

  7. Temporal characteristics of gustatory responses in rat parabrachial neurons vary by stimulus and chemosensitive neuron type.

    Science.gov (United States)

    Geran, Laura; Travers, Susan

    2013-01-01

    It has been demonstrated that temporal features of spike trains can increase the amount of information available for gustatory processing. However, the nature of these temporal characteristics and their relationship to different taste qualities and neuron types are not well-defined. The present study analyzed the time course of taste responses from parabrachial (PBN) neurons elicited by multiple applications of "sweet" (sucrose), "salty" (NaCl), "sour" (citric acid), and "bitter" (quinine and cycloheximide) stimuli in an acute preparation. Time course varied significantly by taste stimulus and best-stimulus classification. Across neurons, the ensemble code for the three electrolytes was similar initially but quinine diverged from NaCl and acid during the second 500 ms of stimulation and all four qualities became distinct just after 1s. This temporal evolution was reflected in significantly broader tuning during the initial response. Metric space analyses of quality discrimination by individual neurons showed that increases in information (H) afforded by temporal factors was usually explained by differences in rate envelope, which had a greater impact during the initial 2s (22.5% increase in H) compared to the later response (9.5%). Moreover, timing had a differential impact according to cell type, with between-quality discrimination in neurons activated maximally by NaCl or citric acid most affected. Timing was also found to dramatically improve within-quality discrimination (80% increase in H) in neurons that responded optimally to bitter stimuli (B-best). Spikes from B-best neurons were also more likely to occur in bursts. These findings suggest that among PBN taste neurons, time-dependent increases in mutual information can arise from stimulus- and neuron-specific differences in response envelope during the initial dynamic period. A stable rate code predominates in later epochs.

  8. Analgesia accompanying food consumption requires ingestion of hedonic foods.

    Science.gov (United States)

    Foo, H; Mason, Peggy

    2009-10-14

    Animals eat rather than react to moderate pain. Here, we examined the behavioral, hedonic, and neural requirements for ingestion analgesia in ad libitum fed rats. Noxious heat-evoked withdrawals were similarly suppressed during self-initiated chocolate eating and ingestion of intraorally infused water, sucrose, or saccharin, demonstrating that ingestion analgesia does not require feeding motivation, self-initiated food procurement, sucrose, or calories. Rather, food hedonics is important because neither salt ingestion nor quinine rejection elicited analgesia. During quinine-induced nausea and lipopolysaccharide (LPS)-induced illness, conditions when chocolate eating was presumably less pleasurable, analgesia accompanying chocolate consumption was attenuated, yet analgesia during water ingestion was preserved in LPS-injected rats who showed enhanced palatability for water within this context. The dependence of ingestion analgesia on the positive hedonics of an ingestate was confirmed in rats with a conditioned taste aversion to sucrose: after paired exposure to sucrose and LPS, rats no longer showed analgesia during sucrose ingestion but continued to show analgesia during chocolate consumption. Eating pauses tended to occur less often and for shorter durations in the presence of ingestion analgesia than in its absence. Therefore, we propose that ingestion analgesia functions to defend eating from ending. Muscimol inactivation of the medullary raphe magnus blocked the analgesia normally observed during water ingestion, showing the involvement of brainstem endogenous pain inhibitory mechanisms in ingestion analgesia. Brainstem-mediated defense of the consumption of palatable foods may explain, at least in part, why overeating tasty foods is so irresistible even in the face of opposing cognitive and motivational forces.

  9. Digital, Three-dimensional Average Shaped Atlas of the Heliothis Virescens Brain with Integrated Gustatory and Olfactory Neurons.

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    Kvello, Pål; Løfaldli, Bjarte Bye; Rybak, Jürgen; Menzel, Randolf; Mustaparta, Hanna

    2009-01-01

    We use the moth Heliothis virescens as model organism for studying the neural network involved in chemosensory coding and learning. The constituent neurons are characterised by intracellular recordings combined with staining, resulting in a single neuron identified in each brain preparation. In order to spatially relate the neurons of different preparations a common brain framework was required. We here present an average shaped atlas of the moth brain. It is based on 11 female brain preparations, each stained with a fluorescent synaptic marker and scanned in confocal laser-scanning microscope. Brain neuropils of each preparation were manually reconstructed in the computer software Amira, followed by generating the atlas using the Iterative Shape Average Procedure. To demonstrate the application of the atlas we have registered two olfactory and two gustatory interneurons, as well as the axonal projections of gustatory receptor neurons into the atlas, visualising their spatial relationships. The olfactory interneurons, showing the typical morphology of inner-tract antennal lobe projection neurons, projected in the calyces of the mushroom body and laterally in the protocerebral lobe. The two gustatory interneurons, responding to sucrose and quinine respectively, projected in different areas of the brain. The wide projections of the quinine responding neuron included a lateral area adjacent to the projections of the olfactory interneurons. The sucrose responding neuron was confined to the suboesophageal ganglion with dendritic arborisations overlapping the axonal projections of the gustatory receptor neurons on the proboscis. By serving as a tool for the integration of neurons, the atlas offers visual access to the spatial relationship between the neurons in three dimensions, and thus facilitates the study of neuronal networks in the Heliothis virescens brain. The moth standard brain is accessible at http://www.ntnu.no/biolog/english/neuroscience/brain.

  10. Digital, three-dimensional average shaped atlas of the heliothis virescens brain with integrated gustatory and olfactory neurons

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    Pål Kvello

    2009-10-01

    Full Text Available We use the moth Heliothis virescens as model organism for studying the neural network involved in chemosensory coding and learning. The constituent neurons are characterised by intracellular recordings combined with staining, resulting in a single neuron identified in each brain preparation. In order to spatially relate the neurons of different preparations a common brain framework was required. We here present an average shaped atlas of the moth brain. It is based on 11 female brain preparations, each stained with a fluorescent synaptic marker and scanned in confocal laser-scanning microscope. Brain neuropils of each preparation were manually reconstructed in the computer software AMIRA, followed by generating the atlas using the Iterative Shape Average Procedure. To demonstrate the application of the atlas we have registered two olfactory and two gustatory interneurons, as well as the axonal projections of gustatory receptor neurons into the atlas, visualising their spatial relationships. The olfactory interneurons, showing the typical morphology of inner-tract antennal lobe projection neurons, projected in the calyces of the mushroom body and laterally in the protocerebral lobe. The two gustatory interneurons, responding to sucrose and quinine respectively, projected in different areas of the brain. The wide projections of the quinine responding neuron included a lateral area adjacent to the projections of the olfactory interneurons. The sucrose responding neuron was confined to the suboesophageal ganglion with dendritic arborizations overlapping the axonal projections of the gustatory receptor neurons on the proboscis. By serving as a tool for the integration of neurons, the atlas offers visual access to the spatial relationship between the neurons in three dimensions, and thus facilitates the study of neuronal networks in the Heliothis virescens brain. The moth standard brain is accessible at http://www.nt.ntnu.no/users/kvello/H_virescens_standardbrain/

  11. Ghrelin increases the motivation to eat, but does not alter food palatability.

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    Overduin, Joost; Figlewicz, Dianne P; Bennett-Jay, Jennifer; Kittleson, Sepideh; Cummings, David E

    2012-08-01

    Homeostatic eating cannot explain overconsumption of food and pathological weight gain. A more likely factor promoting excessive eating is food reward and its representation in the central nervous system (CNS). The anorectic hormones leptin and insulin reduce food reward and inhibit related CNS reward pathways. Conversely, the orexigenic gastrointestinal hormone ghrelin activates both homeostatic and reward-related neurocircuits. The current studies were conducted to identify in rats the effects of intracerebroventricular ghrelin infusions on two distinct aspects of food reward: hedonic valuation (i.e., "liking") and the motivation to self-administer (i.e., "wanting") food. To assess hedonic valuation of liquid food, lick motor patterns were recorded using lickometry. Although ghrelin administration increased energy intake, it did not alter the avidity of licking (initial lick rates or lick-cluster size). Several positive-control conditions ruled out lick-rate ceiling effects. Similarly, when the liquid diet was hedonically devalued with quinine supplementation, ghrelin failed to reverse the quinine-associated reduction of energy intake and avidity of licking. The effects of ghrelin on rats' motivation to eat were assessed using lever pressing to self-administer food in a progressive-ratio paradigm. Ghrelin markedly increased motivation to eat, to levels comparable to or greater than those seen following 24 h of food deprivation. Pretreatment with the dopamine D1 receptor antagonist SCH-23390 eliminated ghrelin-induced increases in lever pressing, without compromising generalized licking motor control, indicating a role for D1 signaling in ghrelin's motivational feeding effects. These results indicate that ghrelin increases the motivation to eat via D1 receptor-dependent mechanisms, without affecting perceived food palatability.

  12. Formation of 4'-carboxyl acid metabolite of imrecoxib by rat liver microsomes

    Institute of Scientific and Technical Information of China (English)

    Hai-yan XU; Peng ZHANG; Ai-shen GONG; Yu-ming SUN; Feng-ming CHU; Zong-ru GUO; Da-fang ZHONG

    2006-01-01

    Aim:Imrecoxib is a novel and moderately selective COX-2 inhibitor.The aim of the present in vitro investigation was to study the formation of the major metabolite 4'-carboxylic acid imrecoxib (M2) and identify the enzyrne(s) involved in the reaction.Methods:The formation of M2 was studied in rat liver cytosol in the absence or presence of liver microsomes.The formed metabolite was identified and quantified by LC/MSn.In addition,to characterize the cytochrome P450 (CYP) isozymes involved in M2 formation,the effects of typical CYP inhibitors (such as ketoconazle,quinine,α-naphthoflavone, methylpyrazole,and cimetidine) on the formation rate of M2 were investigated.Results:The formation of M2 from 4'hydroxymethyl imrecoxib (M4) was completely dependent on rat liver microsomes and NADPH.Enzyme kinetic studies demonstrated that the formation rate of M2 conformed to monophasic Michaelis-Menten kinetics.Additional experiments showed that the formation of M2 was induced significantly by dexamethasone and lowered by ketoconazole strongly and concentration-dependently.By comparison.other CYP inhibitors.such as α-naphthoflavone,cimetidine,quinine,and methylpyrazole had no inhibitory effects on this metabolic pathway.Conclusion:These biotransformation studies of M4 and imrecoxib in rat liver at the subcellular level showed that the formation of M2 occurs in rat liver microsomes and is NADPH-dependent.The reaction was mainly catalyzed by CYP 3A in untreated rats and in dexamethasone-induced rats.Other CYP,such as CYP 1A,2C,2D,and 2E,seem unlikely to participate in this metabolic pathway.

  13. Role of rat liver cytochrome P450 3A and 2D in metabolism of imrecoxib

    Institute of Scientific and Technical Information of China (English)

    Hai-yan XU; Zhi-yong XIE; Peng ZHANG; Jin SUN; Feng-ming CHU; Zong-ru GUO; Da-fang ZHONG

    2006-01-01

    Aim: To investigate the in vitro metabolism of imrecoxib in rat liver microsomes and to identify the cytochrome P450 (CYP) forms involved in its metabolism. Methods: Liver microsomes of Wistar rats were prepared using an ultracentrifuge. The in vitro metabolism of imrecoxib was studied by incubation with rat liver microsomes. To characterize the CYP forms involved in the 4'-methyl hydroxylation of imrecoxib, the effects of typical CYP inducers (such as dexamethasone, isoniazid and (3-naphthoflavone) and of CYP inhibitors (such as ketoconazole, quinine, a-naphthoflavone, methylpyrazole, and cimetidine) on the formation rate of 4'-hydroxymethyl imrecoxib were investigated. Results: Imrecoxib wasmetabolized to 3 metabolites by rat liver microsomes: 4'-hydroxymethyl imrecoxib (M4), 4'-hydroxymethyl-5-hydoxyl imrecoxib (M3), and 4'-hydroxymethyl-5-carbonyl imrecoxib (M5). Over the imrecoxib concentration range studied (5-600 umol/L), the rate of 4'-methyl hydroxylation conformed to monophasic Michaelis-Menten kinetics. Dexamethasone significantly induced the formation of M4. Ketoconazole markedly lowered the metabolic rate of imrecoxib in a concentration-dependent manner. Moreover, a significant inhibitory effect of quinine on the formation of M4 was observed in microsomes obtained from control rats, isoniazid-induced rats, and (3-naphthoflavone-induced rats. In contrast, α-naphthoflavone, cimetidine, and methylpyrazole had no inhibitory effects on this metabolic pathway. Conclusion: Imrecoxib is metabolized via 4'-methyl hydroxylation in rat liver microsomes. The reaction is mainly catalyzed by CYP 3A. CYP 2D also played a role in control rats, in isoniazid-induced rats and in β-naphthoflavone-induced rats.

  14. Bitter taste receptor agonists alter mitochondrial function and induce autophagy in airway smooth muscle cells.

    Science.gov (United States)

    Pan, Shi; Sharma, Pawan; Shah, Sushrut D; Deshpande, Deepak A

    2017-07-01

    Airway remodeling, including increased airway smooth muscle (ASM) mass, is a hallmark feature of asthma and COPD. We previously identified the expression of bitter taste receptors (TAS2Rs) on human ASM cells and demonstrated that known TAS2R agonists could promote ASM relaxation and bronchodilation and inhibit mitogen-induced ASM growth. In this study, we explored cellular mechanisms mediating the antimitogenic effect of TAS2R agonists on human ASM cells. Pretreatment of ASM cells with TAS2R agonists chloroquine and quinine resulted in inhibition of cell survival, which was largely reversed by bafilomycin A1, an autophagy inhibitor. Transmission electron microscope studies demonstrated the presence of double-membrane autophagosomes and deformed mitochondria. In ASM cells, TAS2R agonists decreased mitochondrial membrane potential and increased mitochondrial ROS and mitochondrial fragmentation. Inhibiting dynamin-like protein 1 (DLP1) reversed TAS2R agonist-induced mitochondrial membrane potential change and attenuated mitochondrial fragmentation and cell death. Furthermore, the expression of mitochondrial protein BCL2/adenovirus E1B 19-kDa protein-interacting protein 3 (Bnip3) and mitochondrial localization of DLP1 were significantly upregulated by TAS2R agonists. More importantly, inhibiting Bnip3 mitochondrial localization by dominant-negative Bnip3 significantly attenuated cell death induced by TAS2R agonist. Collectively the TAS2R agonists chloroquine and quinine modulate mitochondrial structure and function, resulting in ASM cell death. Furthermore, Bnip3 plays a central role in TAS2R agonist-induced ASM functional changes via a mitochondrial pathway. These findings further establish the cellular mechanisms of antimitogenic effects of TAS2R agonists and identify a novel class of receptors and pathways that can be targeted to mitigate airway remodeling as well as bronchoconstriction in obstructive airway diseases. Copyright © 2017 the American Physiological

  15. Analysis of the expression of human bitter taste receptors in extraoral tissues.

    Science.gov (United States)

    Jaggupilli, Appalaraju; Singh, Nisha; Upadhyaya, Jasbir; Sikarwar, Anurag S; Arakawa, Makoto; Dakshinamurti, Shyamala; Bhullar, Rajinder P; Duan, Kangmin; Chelikani, Prashen

    2017-02-01

    The 25 bitter taste receptors (T2Rs) in humans perform a chemosensory function. However, very little is known about the level of expression of these receptors in different tissues. In this study, using nCounter gene expression we analyzed the expression patterns of human TAS2R transcripts in cystic fibrosis bronchial epithelial (CuFi-1), normal bronchial epithelial (NuLi-1), airway smooth muscle (ASM), pulmonary artery smooth muscle (PASM), mammary epithelial, and breast cancer cells. Our results suggest a specific pattern of TAS2R expression with TAS2R3, 4, 5, 10, 13, 19, and 50 transcripts expressed at moderate levels and TAS2R14 and TAS2R20 (or TASR49) at high levels in the various tissues analyzed. This pattern of expression is mostly independent of tissue origin and the pathological state, except in cancer cells. To elucidate the expression at the protein level, we pursued flow cytometry analysis of select T2Rs from CuFi-1 and NuLi-1 cells. The expression levels observed at the gene level by nCounter analysis correlate with the protein levels for the T2Rs analyzed. Next, to assess the functionality of the expressed T2Rs in these cells, we pursued functional assays measuring intracellular calcium mobilization after stimulation with the bitter compound quinine. Using PLC inhibitor, U-73122, we show that the calcium mobilized in these cells predominantly takes place through the Quinine-T2R-Gαβγ-PLC pathway. This report will accelerate studies aimed at analyzing the pathophysiological function of T2Rs in different extraoral tissues.

  16. UK malaria treatment guidelines 2016.

    Science.gov (United States)

    Lalloo, David G; Shingadia, Delane; Bell, David J; Beeching, Nicholas J; Whitty, Christopher J M; Chiodini, Peter L

    2016-06-01

    . Most patients treated for P. falciparum malaria should be admitted to hospital for at least 24 h as patients can deteriorate suddenly, especially early in the course of treatment. In specialised units seeing large numbers of patients, outpatient treatment may be considered if specific protocols for patient selection and follow up are in place. 10. Uncomplicated P. falciparum malaria should be treated with an artemisinin combination therapy (Grade 1A). Artemether-lumefantrine (Riamet(®)) is the drug of choice (Grade 2C) and dihydroartemisinin-piperaquine (Eurartesim(®)) is an alternative. Quinine or atovaquone-proguanil (Malarone(®)) can be used if an ACT is not available. Quinine is highly effective but poorly-tolerated in prolonged treatment and should be used in combination with an additional drug, usually oral doxycycline. 11. Severe falciparum malaria, or infections complicated by a relatively high parasite count (more than 2% of red blood cells parasitized) should be treated with intravenous therapy until the patient is well enough to continue with oral treatment. Severe malaria is a rare complication of P. vivax or P. knowlesi infection and also requires parenteral therapy. 12. The treatment of choice for severe or complicated malaria in adults and children is intravenous artesunate (Grade 1A). Intravenous artesunate is unlicensed in the EU but is available in many centres. The alternative is intravenous quinine, which should be started immediately if artesunate is not available (Grade 1A). Patients treated with intravenous quinine require careful monitoring for hypoglycemia. 13. Patients with severe or complicated malaria should be managed in a high-dependency or intensive care environment. They may require haemodynamic support and management of: acute respiratory distress syndrome, disseminated intravascular coagulation, acute kidney injury, seizures, and severe intercurrent infections including Gram-negative bacteraemia/septicaemia. 14. Children with

  17. 人类基本呈味物质对菜粉蝶幼虫的拒食作用%Feeding Deterrence of Six Basic Tastants against Pieris rapae Larvae

    Institute of Scientific and Technical Information of China (English)

    游秀峰; 孙淑君; 原国辉; 郭线茹; 李为争

    2013-01-01

    Tastants are serials of heavy-taste substances screened out by human beings for a long time,which may play an important role in the regulation of feeding behaviours of herbivoral insects. However,the either-or characterization of these substances with respect to their effects on feeding response of herbivores is not efficient to explain the comprehensive interactions among various tastants. This study tested the feeding deterrence of six tastants (citric acid,sucrose,quinine,NaCl,sanshool,and capsaicin) , alone or orthogonally combined, against Pieris rapae larvae. The paired bioassay with each tastant and control leaf disc indicated that citric acid, quinine, and sanshool evoked strong feeding deterrence, with feeding deterrence values of 93. 89% ,90. 33% , and 83. 33 %, respectively. When these tastants were orthogonally combined, capsaicin, sucrose, and sanshool exhibited stronger effects on the feeding amount,while quinine and NaCl acted antagonistically. Four tastants showing relatively stronger effects were orthogonally combined further and tested under selective and non-selective feeding conditions. The result showed that capsaicin exhibited the strongest feeding deterrence, and only one sample (9 μL sucrose + 9 μL sanshool + 3 μL capsaicin +12 μL citric acid) exhibited strong feeding deterrence under both conditions. A given tastant could show remarkable discrepancy when used alone or combined, suggesting that some multiple-factor experimental designs should be introduced in insect feeding bioassay to overcome the gustatory habituation of pests.%呈味物质是人类经过漫长筛选形成的味感强烈的物质,可能在调控害虫取食行为中发挥重要作用,但传统的二分式定性法难以阐明其对昆虫味觉反应的复杂相互作用.为此,以菜粉蝶为研究对象,采用叶碟法结合正交设计测试了6种人类呈味物质(柠檬酸、蔗糖、奎宁、氯化钠、山椒醇和辣椒素)对菜粉蝶幼虫取食反应的影

  18. Meta-analysis of artemether treatment for severe malaria%蒿甲醚治疗重症疟疾的Meta分析

    Institute of Scientific and Technical Information of China (English)

    单琳琳; 尚晓鹏; 宋世震; 梅勇; 卢星星; 曾周; 刘艳茹; 万力

    2013-01-01

    Objective To systematically estimate whether intramuscular artemether has advantages over other drugs as a treatment for severe malaria.Methods MEDLINE,Elsevier SDOL,Springer LINK online Journals,Embase,EBSCO ASP,VIP,CNKI,and WANFANG databases were searcbed for randomized controlled trials (RCTs) involving intramuscular injection of artemether as a treatment for severe malaria.The Cochrane system of evaluation was used to evaluate the methodological quality of the RCTs in those databases and RevMan 5.1.7 was used to analyze valid data.Results Nineteen sources describing 21 RCTs were noted.These trials were graded according to RCT quality standards recommend by the Cochrane system,and all scores were above 3.Meta-analysis of 14 RCTs that compared artemether to quinine revealed a statistically significant difference in mortality rates and analysis revealed that artemether was more efficacious than quinine [RR =0.82,95 %CI(0.67,0.99),P=0.04].Outcomes of 4 RCTs that compared artemether and artesunate revealed no differences in mortality rates.There were no statistically significant differences in the mortality rates of intramuscular artemether compared to an artemisinin suppository or intramuscular chloroquine.Intramuscular artemether and intravenous quinate had greater efficacy than intramuscular artemether.Conclusion Intramuscular artemether had greater efficacy than quinine but less efficacy than intramuscular artemether and intravenous quinate.The mortality rate for intramuscular artemether did not differ statistically from that for artemisinin or chloroquine.%目的 系统评价肌注蒿甲醚与其他药物比较治疗重症疟疾的优越性.方法 计算机检索MEDLINE、Elsevier SDOL、Springer LINK online Journals、Embase、EBSCO ASP、VIP、CNKI和万方数据库,收集肌注蒿甲醚治疗重症疟疾的随机对照试验(RCT),用Cochrane系统评价方法对纳入的RCT进行方法学质量评价并提取有效数据进行分

  19. The effect of mimicking febrile temperature and drug stress on malarial development

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    Adisakwattana Poom

    2009-06-01

    Full Text Available Abstract Background Malaria remains one of the most important tropical diseases of human with 1–2 million deaths annually especially caused by P. falciparum. During malarial life cycle, they exposed to many environmentally stresses including wide temperature fluctuation and pharmacological active molecules. These trigger malarial evolutionarily adaptive responses. The effect of febrile temperature on malarial growth, development and drug susceptibility by mimicking patient in treatment failure before and after drug uptake was examined. Methods Sensitivities of P. falciparum to antimalarial drug (chloroquine, mefloquine, quinine and artesunate were investigated based on the incorporation of [3H] hypoxanthine into parasite nucleic acids or radioisotopic technique. The number of parasites was examined under microscope following Giemsa staining and the parasite development at the end of each phase was counted and comparison of parasite number was made. The proteome was separated, blotted and hybridized with anti-Hsp70s primary antibody. The hybridized proteins were separately digested with trypsin and identified by MALDI-TOF peptide mass fingerprint. Results The results show that febrile temperature is capable of markedly inhibiting the growth of field isolate P. falciparum but not to K1 and 3D7 standard strains. K1 and 3D7 grown under heat shock developed greater and the reinfection rate was increased up to 2-folds when compared to that of non-heat shock group. The IC50 value of K1 toward chloroquine, mefloquine and quinine under heat shock was higher than that of K1 under non-heat shock which is opposite to that of 3D7. Heat shock caused death in field isolated parasite. It was also found that the febrile temperature coped with chloroquine uptake had no effect to the development, drug sensitivity and the parasite number of K1 strain. In the opposite way, heat shock and chloroquine shows extremely effect toward 3D7 and field isolate PF91 as shown

  20. Constituent of Sugars and Acids and the Flavor Trait of Megranate Fruits%石榴果实的糖酸组成及风味特点

    Institute of Scientific and Technical Information of China (English)

    秦改花; 黄文江; 赵建荣; 邓盾; 周玉丽

    2011-01-01

    The content of sugars and organic acids of ripening fruits of four megranate cultivars were detected by HPLC. The taste value and relationship between content of sugars and acids and the flavor indices of different cultivars were studied. Results showed, the soluble sugars of megranate fruits included sucrose, glucose, fructose and sorbitol. Glucose and fructose were sugars of higher concentration, they accounted for 43.84% ~48.36% and 49.18%~50.67% of total sugars respectively. "Yushizi" was the cultivar of the highest sugars, while "Baipi" was the one of lowest among the four cultivars. The main organic acids of megranate fruits were quininic acid and succinic acid. Besides, oxalic acid, L-malic acid, shikimic acid, citrate acid and D-malic acid were detected in megranate fruits. "Manaozi" was the cultivar of the highest concentration of organic acids while "Qingpi" was the one of the lowest. Fructose had the greatest sweetness taste in megranate, followed by glucose; while quininic acid had the greatest sourness taste, followed by citrate acid. It also showed that sugars/acids had significantly positive correlation with sweetness taste/ sourness. The difference of sugars/acids among cultivars was mainly based on the concentration of oxalic acid, quininic acid, L-malic acid, citrate acid and succinic acid, but little correlation with the sugars. According to the flavor traits, "Qingpi"and "Yushizi" were considered as the cultivars of more sweetness taste, while "Baipi" and "Manaozi" were the cultivars of more sweetness taste.%采用高效液相色谱法测定4种石榴成熟期果实中糖和酸的组成,并对其味感值和糖酸组分与果实风味指标间的相关性进行分析.结果表明,石榴果实中可溶性糖组分有蔗糖、葡萄糖、果糖和山梨醇,其中葡萄糖和果糖含量最高,分别占总糖含量的43.84% ~48.36%和49.18% ~50.67%.4个品种中, “玉石籽”的总糖含量最高,“白皮”的最低.石榴果实

  1. Current status of artemisinin-resistant falciparum malaria in South Asia: a randomized controlled artesunate monotherapy trial in Bangladesh.

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    Peter Starzengruber

    Full Text Available OBJECTIVE: Recent reports indicate that first cases of genuine artemisinin resistance have already emerged along the Thai-Cambodian border. The main objective of this trial was to track the potential emergence of artemisinin resistance in Bangladesh, which in terms of drug resistance forms a gateway to the Indian subcontinent. METHODS: We conducted an open-label, randomized, controlled 42-day clinical trial in Southeastern Bangladesh to investigate the potential spread of clinical artemisinin resistance from Southeast Asia. A total of 126 uncomplicated falciparum malaria patients were randomized to one of 3 treatment arms (artesunate monotherapy with 2 or 4 mg/kg/day once daily or quinine plus doxycycline TID for 7 days. Only cases fulfilling a stringent set of criteria were considered as being artemisinin-resistant. FINDINGS: The 28-day and 42-day cure rates in the artesunate monotherapy (2 and 4 mg/kg and quinine/doxycyline arms were 97.8% (95% confidence interval, CI: 87.8-99.8%, 100% (95% CI: 91.1-100%, and 100% (95% CI: 83.4-100%, respectively. One case of re-infection was seen in the artesunate high dose arm, and a single case of recrudescence was observed in the low dose group on day 26. No differences in median parasite and fever clearance times were found between the 2 artesunate arms (29.8 h and 17.9 h vs. 29.5 h and 19.1 h. Not a single case fulfilled our criteria of artemisinin resistance. Parasite clearance times were considerably shorter and ex vivo results indicate significantly higher susceptibility (50% inhibitory concentration for dihydroartemisinin was 1.10 nM; 95% CI: 0.95-1.28 nM to artemisinins as compared to SE-Asia. CONCLUSION: There is currently no indication that artemisinin resistance has reached Bangladesh. However, the fact that resistance has recently been reported from nearby Myanmar indicates an urgent need for close monitoring of artemisinin resistance in the region. TRIAL REGISTRATION: ClinicalTrials.gov NCT

  2. Efficacy and safety evaluation of a novel trioxaquine in the management of cerebral malaria in a mouse model.

    Science.gov (United States)

    Odhiambo, Onyango C; Wamakima, Hannah N; Magoma, Gabriel N; Kirira, Peter G; Malala, Bonface J; Kimani, Francis T; Muregi, Francis W

    2017-07-03

    The emergence of multidrug-resistant strains of Plasmodium falciparum poses a great threat of increased fatalities in cases of cerebral and other forms of severe malaria infections in which parenteral artesunate monotherapy is the current drug of choice. The study aimed to investigate in a mouse model of human cerebral malaria whether a trioxaquine chemically synthesized by covalent linking of a 4,7-dichloroquinoline pharmacophore to artesunate through a recent drug development approach termed 'covalent bitherapy' could improve the curative outcomes in cerebral malaria infections. Human cerebral malaria rodent model, the C57BL/6 male mice were infected intraperitoneally (ip) with Plasmodium berghei ANKA and intravenously (iv) treated with the trioxaquine from day 8 post-infection (pi) at 12.5 and 25 mg/kg, respectively, twice a day for 3 days. Treatments with the trioxaquine precursors (artesunate and 4,7-dichloroquine), and quinine were also included as controls. In vivo safety evaluation for the trioxaquine was done according to Organization for Economic Co-operation and Development (OECD) guidelines 423, where female Swiss albino mice were orally administered with either 300 or 2000 mg/kg of the trioxaquine and monitored for signs of severity, and or mortality for 14 days post-treatment. The trioxaquine showed a potent and a rapid antiplasmodial activity with 80% parasite clearance in the first 24 h for the two dosages used. Long-term parasitaemia monitoring showed a total parasite clearance as the treated mice survived beyond 60 days post-treatment, with no recrudescence observed. Artesunate treated mice showed recrudescence 8 days post-treatment, with all mice in this group succumbing to the infection. Also, 4,7-dichloroquinoline and quinine did not show any significant parasitaemia suppression in the first 24 h post-treatment, with the animals succumbing to the infection. Covalent bitherapy proves to be a viable source of urgently needed new anti

  3. INACTIVATION OF THE LATERAL ORBITOFRONTAL CORTEX INCREASES DRINKING IN ETHANOL-DEPENDENT BUT NOT NON-DEPENDENT MICE

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    den Hartog, Carolina; Zamudio-Bulcock, Paula; Nimitvilai, Sudarat; Gilstrap, Meghin; Fedarovich, Hleb; Motts, Andrew; Woodward, John J.

    2016-01-01

    Long-term consumption of ethanol affects cortical areas that are important for learning and memory, cognition, and decision-making. Deficits in cortical function may contribute to alcohol-abuse disorders by impeding an individual’s ability to control drinking. Previous studies from this laboratory show that acute ethanol reduces activity of lateral orbitofrontal cortex (LOFC) neurons while chronic exposure impairs LOFC-dependent reversal learning and induces changes in LOFC excitability. Despite these findings, the role of LOFC neurons in ethanol consumption is unknown. To address this issue, we examined ethanol drinking in adult C57Bl/6J mice that received an excitotoxic lesion or viral injection of the inhibitory DREADD (designer receptor exclusively activated by designer drug) into the LOFC. No differences in ethanol consumption were observed between sham and lesioned mice during access to increasing concentrations of ethanol (3–40%) every other day for 7 weeks. Adulterating the ethanol solution with saccharin (0.2%) or quinine (0.06 mM) enhanced or inhibited, respectively, consumption of the 40% ethanol solution similarly in both groups. Using a chronic intermittent ethanol (CIE) vapor exposure model that produces dependence, we found no difference in baseline drinking between sham and lesioned mice prior to vapor treatments. CIE enhanced drinking in both groups as compared to air-treated animals and CIE treated lesioned mice showed an additional increase in ethanol drinking as compared to CIE sham controls. This effect persisted during the first week when quinine was added to the ethanol solution but consumption decreased to control levels in CIE lesioned mice in the following 2 weeks. In viral injected mice, baseline drinking was not altered by expression of the inhibitory DREADD receptor and repeated cycles of CIE exposure enhanced drinking in DREADD and virus control groups. Consistent with the lesion study, treatment with clozapine-N-oxide (CNO

  4. EXPERIMENTS OF WATER PURIFICATION USING FORWORD OSMOSIS MEMBRANE%正渗透膜净水试验研究

    Institute of Scientific and Technical Information of China (English)

    解一君; 马睿; 夏圣骥; 高乃云

    2012-01-01

    This study investigated the variation of permeate flux and reverse solute diffusion in forward osmosis (FO) process, quinine and humic acid were chosen as the model organic fouling to evaluate the rejection of organic matter in FO process. A strong correlation between the permeate flux and concentrations of draw solution was observed, but the flux was highly non-linear with respect to the concentrations of draw solution as a result of internal concentration polarization (ICP). The effect of temperature on FO performance was also evaluated, and the result indicated that the transmembrane water flux increased from 4 IV (m2· h) to 10 U (m2 · h) with an increase in temperature from 11 ~ 36·. The anti-diffusion amount of the drive solute linear increased with prolonged operation time, due to the Donnan effect of Na+ in the inverse diffusion is greater than the divalent cation. FO membrane had good retention effects of quinine and humic acid.%研究了正渗透(FO)过程中水通量和驱动溶质扩散规律,并以奎宁和腐殖酸作为模型有机物,研究FO膜对有机物的截留性能.结果表明,FO水通量与驱动液含量正相关,但由于内部浓差极化的影响并不呈正比例;温度越高所产生的水通量也越大,在温度11~36℃时水通量从4 L/(m2·h)上升至10 L/(m· h).驱动溶质的反扩散量随运行时间的延长线性增加,由于唐南效应Na+的反扩散量大于2价阳离子.FO膜对奎宁和腐殖酸均有较好的截留效果.

  5. Simple flow cytometric detection of haemozoin containing leukocytes and erythrocytes for research on diagnosis, immunology and drug sensitivity testing

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    Grobusch Martin P

    2011-03-01

    Full Text Available Abstract Background Malaria pigment (haemozoin, Hz has been the focus of diverse research efforts. However, identification of Hz-containing leukocytes or parasitized erythrocytes is usually based on microscopy, with inherent limitations. Flow cytometric detection of depolarized Side-Scatter is more accurate and its adaptation to common bench top flow cytometers might allow several applications. These can range from the ex-vivo and in-vitro detection and functional analysis of Hz-containing leukocytes to the detection of parasitized Red-Blood-Cells (pRBCs to assess antimalarial activity. Methods A standard benchtop flow cytometer was adapted to detect depolarized Side-Scatter. Synthetic and Plasmodium falciparum Hz were incubated with whole blood and PBMCs to detect Hz-containing leukocytes and CD16 expression on monocytes. C5BL/6 mice were infected with Plasmodium berghei ANKA or P. berghei NK65 and Hz-containing leukocytes were analysed using CD11b and Gr1 expression. Parasitized RBC from infected mice were identified using anti-Ter119 and SYBR green I and were analysed for depolarized Side Scatter. A highly depolarizing RBC population was monitored in an in-vitro culture incubated with chloroquine or quinine. Results A flow cytometer can be easily adapted to detect depolarized Side-Scatter and thus, intracellular Hz. The detection and counting of Hz containing leukocytes in fresh human or mouse blood, as well as in leukocytes from in-vitro experiments was rapid and easy. Analysis of CD14/CD16 and CD11b/Gr1 monocyte expression in human or mouse blood, in a mixed populations of Hz-containing and non-containing monocytes, appears to show distinct patterns in both types of cells. Hz-containing pRBC and different maturation stages could be detected in blood from infected mice. The analysis of a highly depolarizing population that contained mature pRBC allowed to assess the effect of chloroquine and quinine after only 2 and 4 hours, respectively

  6. Radical curative efficacy of tafenoquine combination regimens in Plasmodium cynomolgi-infected Rhesus monkeys (Macaca mulatta

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    Kenworthy David

    2011-07-01

    Full Text Available Abstract Background Tafenoquine is an 8-aminoquinoline being developed for radical cure (blood and liver stage elimination of Plasmodium vivax. During monotherapy treatment, the compound exhibits slow parasite and fever clearance times, and toxicity in glucose-6-phosphate dehydrogenase (G6PD deficiency is a concern. Combination with other antimalarials may mitigate these concerns. Methods In 2005, the radical curative efficacy of tafenoquine combinations was investigated in Plasmodium cynomolgi-infected naïve Indian-origin Rhesus monkeys. In the first cohort, groups of two monkeys were treated with a three-day regimen of tafenoquine at different doses alone and in combination with a three-day chloroquine regimen to determine the minimum curative dose (MCD. In the second cohort, the radical curative efficacy of a single-day regimen of tafenoquine-mefloquine was compared to that of two three-day regimens comprising tafenoquine at its MCD with chloroquine or artemether-lumefantrine in groups of six monkeys. In a final cohort, the efficacy of the MCD of tafenoquine against hypnozoites alone and in combination with chloroquine was investigated in groups of six monkeys after quinine pre-treatment to eliminate asexual parasites. Plasma tafenoquine, chloroquine and desethylchloroquine concentrations were determined by LC-MS in order to compare doses of the drugs to those used clinically in humans. Results The total MCD of tafenoquine required in combination regimens for radical cure was ten-fold lower (1.8 mg/kg versus 18 mg/kg than for monotherapy. This regimen (1.8 mg/kg was equally efficacious as monotherapy or in combination with chloroquine after quinine pre-treatment to eliminate asexual stages. The same dose of (1.8 mg/kg was radically curative in combination with artemether-lumefantrine. Tafenoquine was also radically curative when combined with mefloquine. The MCD of tafenoquine monotherapy for radical cure (18 mg/kg appears to be biologically

  7. 不典型疟疾五例诊治分析%Atypical Malaria:Analysis of Five Cases

    Institute of Scientific and Technical Information of China (English)

    黄志英; 周维俊; 黄沛

    2014-01-01

    目的:探讨不典型疟疾的临床诊治特点。方法对2001年4月-2013年5月安徽财经大学医院诊治的5例不典型疟疾患者的临床资料、实验室检查及诊断资料进行回顾性分析。结果5例不典型疟疾患者的临床症状不典型,热型不规律;于春季和春夏之交发病,流行病学特点不明显;血涂片找疟原虫阴性;使用复方奎宁行诊断性治疗效果良好后确诊。结论临床对于排除其他恶性疾病引起的高热患者应考虑不典型疟疾的可能,疟原虫检查阴性不能排除本病的可能;本病需与上呼吸道感染、败血症等疾病鉴别,常规退热或抗感染治疗无效后可采用复方奎宁进行诊断性治疗。%Objective To explore the clinical features of atypical malaria. Methods Five patients with atypical ma-laria in Hospital of Anhui Finance and Economics University from Apirl 2001 to May 2013 were selected,the clinical data,labo-ratory results and diagnosis information were analyzed retrospectively. Results The clinical symptoms of 5 patients were atypi-cal,fever type irregular,starting in spring or at the end of spring and the beginning of summer,with unobvious epidemiological features. By blood tests,the plasmodium was negative. Compound quinine was used to perform diagnostic treatment and then di-agnosed. Conclusion The possibility of atypical malaria should be considered after excluding the other malignant diseases in hy-perpyrexia patients. Tested negative for the parasite can not exclude the possibility of this disease,this disease should be distin-guished from upper respiratory infection,septicemia and other diseases. Compound quinine can be used to do diagnostic treat-ment after ineffective treatments of conventional antipyretic or anti - infection.

  8. A multifaceted intervention to implement guidelines and improve admission paediatric care in Kenyan district hospitals: a cluster randomised trial.

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    Philip Ayieko

    2011-04-01

    Full Text Available BACKGROUND: In developing countries referral of severely ill children from primary care to district hospitals is common, but hospital care is often of poor quality. However, strategies to change multiple paediatric care practices in rural hospitals have rarely been evaluated. METHODS AND FINDINGS: This cluster randomized trial was conducted in eight rural Kenyan district hospitals, four of which were randomly assigned to a full intervention aimed at improving quality of clinical care (evidence-based guidelines, training, job aides, local facilitation, supervision, and face-to-face feedback; n  =  4 and the remaining four to control intervention (guidelines, didactic training, job aides, and written feedback; n  =  4. Prespecified structure, process, and outcome indicators were measured at baseline and during three and five 6-monthly surveys in control and intervention hospitals, respectively. Primary outcomes were process of care measures, assessed at 18 months postbaseline. In both groups performance improved from baseline. Completion of admission assessment tasks was higher in intervention sites at 18 months (mean  =  0.94 versus 0.65, adjusted difference 0.54 [95% confidence interval 0.05-0.29]. Uptake of guideline recommended therapeutic practices was also higher within intervention hospitals: adoption of once daily gentamicin (89.2% versus 74.4%; 17.1% [8.04%-26.1%]; loading dose quinine (91.9% versus 66.7%, 26.3% [-3.66% to 56.3%]; and adequate prescriptions of intravenous fluids for severe dehydration (67.2% versus 40.6%; 29.9% [10.9%-48.9%]. The proportion of children receiving inappropriate doses of drugs in intervention hospitals was lower (quinine dose >40 mg/kg/day; 1.0% versus 7.5%; -6.5% [-12.9% to 0.20%], and inadequate gentamicin dose (2.2% versus 9.0%; -6.8% [-11.9% to -1.6%]. CONCLUSIONS: Specific efforts are needed to improve hospital care in developing countries. A full, multifaceted intervention was associated

  9. The Safety of Artemisinin Derivatives for the Treatment of Malaria in the 2nd or 3rd Trimester of Pregnancy: A Systematic Review and Meta-Analysis

    Science.gov (United States)

    van Eijk, Anna Maria; Sevene, Esperanca; Dellicour, Stephanie; Weiss, Noel S.; Emerson, Scott; Steketee, Richard; ter Kuile, Feiko O.; Stergachis, Andy

    2016-01-01

    Given the high morbidity for mother and fetus associated with malaria in pregnancy, safe and efficacious drugs are needed for treatment. Artemisinin derivatives are the most effective antimalarials, but are associated with teratogenic and embryotoxic effects in animal models when used in early pregnancy. However, several organ systems are still under development later in pregnancy. We conducted a systematic review and meta-analysis of the occurrence of adverse pregnancy outcomes among women treated with artemisinins monotherapy or as artemisinin-based combination therapy during the 2nd or 3rd trimesters relative to pregnant women who received non-artemisinin antimalarials or none at all. Pooled odds ratio (POR) were calculated using Mantel-Haenszel fixed effects model with a 0.5 continuity correction for zero events. Eligible studies were identified through Medline, Embase, and the Malaria in Pregnancy Consortium Library. Twenty studies (11 cohort studies and 9 randomized controlled trials) contributed to the analysis, with 3,707 women receiving an artemisinin, 1,951 a non-artemisinin antimalarial, and 13,714 no antimalarial. The PORs (95% confidence interval (CI)) for stillbirth, fetal loss, and congenital anomalies when comparing artemisinin versus quinine were 0.49 (95% CI 0.24–0.97, I2 = 0%, 3 studies); 0.58 (95% CI 0.31–1.16, I2 = 0%, 6 studies); and 1.00 (95% CI 0.27–3.75, I2 = 0%, 3 studies), respectively. The PORs comparing artemisinin users to pregnant women who received no antimalarial were 1.13 (95% CI 0.77–1.66, I2 = 86.7%, 3 studies); 1.10 (95% CI 0.79–1.54, I2 = 0%, 4 studies); and 0.79 (95% CI 0.37–1.67, I2 = 0%, 3 studies) for miscarriage, stillbirth and congenital anomalies respectively. Treatment with artemisinin in 2nd and 3rd trimester was not associated with increased risks of congenital malformations or miscarriage and may be was associated with a reduced risk of stillbirths compared to quinine. This study updates the reviews

  10. Treatment of malaria from monotherapy to artemisinin-based combination therapy by health professionals in urban health facilities in Yaoundé, central province, Cameroon

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    Bley Daniel

    2009-07-01

    Full Text Available Abstract Background After adoption of artesunate-amodiaquine (AS/AQ as first-line therapy for the treatment of uncomplicated malaria by the malaria control programme, this study was designed to assess the availability of anti-malarial drugs, treatment practices and acceptability of the new protocol by health professionals, in the urban health facilities and drugstores of Yaoundé city, Cameroon. Methods Between April and August 2005, retrospective and current information was collected by consulting registers and interviewing health practitioners in urban health facilities using a structured questionnaire. Results In 2005, twenty-seven trade-named drugs have been identified in drugstores; quinine tablets (300 mg were the most affordable anti-malarial drugs. Chloroquine was restricted to food market places and no generic artemisinin derivative was available in public health centres. In public health facilities, 13.6% of health professionals were informed about the new guidelines; 73.5% supported the use of AS-AQ as first-line therapy. However, 38.6% apprehended its use due to adverse events attributed to amodiaquine. Malaria treatment was mainly based on the diagnosis of fever. Quinine (300 mg tablets was the most commonly prescribed first-line anti-malarial drug in adults (44.5% and pregnant women (52.5%. Artequin® was the most cited artemsinin-based combination therapy (ACT (9.9%. Medical sales representatives were the main sources of information on anti-malarials. Conclusion The use of AS/AQ was not implemented in 2005 in Yaoundé, despite the wide range of anti-malarials and trade-named artemisinin derivatives available. Nevertheless, medical practitioners will support the use of this combination, when it is available in a paediatric formulation, at an affordable price. Training, information and participation of health professionals in decision-making is one of the key elements to improve adherence to new protocol guidelines. This baseline

  11. Adenylyl cyclase-5 in the dorsal striatum function as a molecular switch for the generation of behavioral preferences for cue-directed food choices.

    Science.gov (United States)

    Kim, Hannah; Kim, Tae-Kyung; Kim, Ji-Eun; Park, Jin-Young; Lee, Yunjin; Kang, Minkyung; Kim, Kyoung-Shim; Han, Pyung-Lim

    2014-11-07

    Behavioral choices in habits and innate behaviors occur automatically in the absence of conscious selection. These behaviors are not easily modified by learning. Similar types of behaviors also occur in various mental illnesses including drug addiction, obsessive-compulsive disorder, schizophrenia, and autism. However, underlying mechanisms are not clearly understood. In the present study, we investigated the molecular mechanisms regulating unconditioned preferred behaviors in food-choices. Mice lacking adenylyl cyclase-5 (AC5 KO mice), which is preferentially expressed in the dorsal striatum, consumed food pellets nearly one after another in cages. AC5 KO mice showed aversive behaviors to bitter tasting quinine, but they compulsively chose quinine-containing AC5 KO-pellets over fresh pellets. The unusual food-choice behaviors in AC5 KO mice were due to the gain of behavioral preferences for food pellets containing an olfactory cue, which wild-type mice normally ignored. Such food-choice behaviors in AC5 KO mice disappeared when whiskers were trimmed. Conversely, whisker trimming in wildtype mice induced behavioral preferences for AC5 KO food pellets, indicating that preferred food-choices were not learned through prior experience. Both AC5 KO mice and wildtype mice with trimmed whiskers had increased glutamatergic input from the barrel cortex into the dorsal striatum, resulting in an increase in the mGluR1-dependent signaling cascade. The siRNA-mediated inhibition of mGluR1 in the dorsal striatum in AC5 KO mice and wildtype mice with trimmed whiskers abolished preferred choices for AC5 KO food pellets, whereas siRNA-mediated inhibition of mGluR3 glutamate receptors in the dorsal striatum in wildtype mice induced behavioral preferences for AC5 KO food pellets, thus mimicking AC5 KO phenotypes. Our results show that the gain and loss of behavioral preferences for a specific cue-directed option were regulated by specific cellular factors in the dorsal striatum, such

  12. Evolução temporal da resistência in vitro do Plasmodium falciparum às drogas antimaláricas em duas áreas da amazônia brasileira com distintas características sócio-econômicas e geográficas

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    Álvaro Augusto Couto

    1995-12-01

    Full Text Available Avaliou-se a evolução temporal da resistência in vitro do Plasmodium falciparum às drogas cloroquina, amodiaquina, quinino e mefloquina em duas áreas com distintas características sócio-econômicas e geográficas: Lourenço, no Estado do Amapá e Paragominas no Estado do Pará. A primeira caracteriza-se por ser uma área de garimpos a céu aberto e a segunda uma área de colonização, pecuária e extrativismo de madeiras. O estudo revela alta prevalência de resistência à cloroquina nas duas áreas (79,8% em Lourenço e 68,4% em Paragominas, enquanto que para amodiaquina e quinino observamos uma certa flutuação nas respostas para essas drogas, dependendo do período em que foi avaliada, fá para mefloquina, não foram obsewadas cepas resistentes, mas uma perda da sensibilidade ao longo do período estudado.We evaluated the temporal progression of in vitro P. falciparum resistance to chloroquine, amodiaquine, quinine and mefloquine in two areas with distinct socioeconomical and geographical characteristics: Lourenço, in Amapá state and Paragominas, in Pará state. The former region is essentially an "open" gold mining camp, whereas the latter is one currently undergoing a colonization settlement process, in addition to expanding economical activities which mainly include cattle raising and wood exploitation. Our results show high resistance rates to chloroquine in the two study areas: 79.8% and 68.4% in Lourenço and Paragominas, respectively. Variations in the response of P. falciparum to both amodiaquine and quinine were recorded throughout the study period. On the other hand, no mefloquine P. falciparum resistant strains could be identified, despite the tact we had noted a decrease in sensitivity to this antimalarial drug throughout the study period.

  13. Reactions of hexadehydro-Diels-Alder benzynes with structurally complex multifunctional natural products

    Science.gov (United States)

    Ross, Sean P.; Hoye, Thomas R.

    2017-06-01

    An important question in organic chemistry concerns the extent to which benzynes—one of the classical reactive intermediates in organic chemistry—can react in discriminating fashion with trapping reagents. In particular, whether these species can react selectively with substrates containing multiple functional groups and possible sites of reactivity has remained unanswered. Natural products comprise a palette of multifunctional compounds with which to address this question. Here, we show that benzynes produced by the hexadehydro-Diels-Alder (HDDA) reaction react with many secondary metabolites with a preference for one among several pathways. Examples demonstrating such selectivity include reactions with: phenolics, through dearomatizing ortho-substitution; alkaloids, through Hofmann-type elimination; tropolone and furan, through cycloaddition; and alkaloids, through three-component fragmentation-coupling reactions. We also demonstrate that the cinchona alkaloids quinidine and quinine give rise to products (some in as few as three steps) that enable subsequent and rapid access to structurally diverse polyheterocyclic compounds. The results show that benzynes are quite discriminating in their reactivity—a trait perhaps not broadly enough appreciated.

  14. Sodium aspartate as a specific enhancer of salty taste perception-sodium aspartate is a possible candidate to decrease excessive intake of dietary salt.

    Science.gov (United States)

    Nakagawa, Tomohiro; Kohori, Jun; Koike, Shin; Katsuragi, Yoshihisa; Shoji, Takayuki

    2014-11-01

    The excessive intake of dietary salt is a global issue in health. Attempts have been made to address this issue, including the development of salt substitutes. Yet, none of these substances are currently in wide use, because of their weak saltiness. The purpose of this study was to assess the effects of sodium aspartate (Asp-Na) on salty taste perception using the bullfrog glossopharyngeal nerve response and human sensory tests. When added to the mixture of NaCl and KCl, Asp-Na significantly enhanced the glossopharyngeal nerve response to the mixture by 1.6-fold compared to control. Asp-Na did not enhance the response to NaCl, nor did Asp-Na enhance the response to sour, bitter, or umami stimuli. The optimal concentration for Asp-Na to enhance the salt mixture was 1.7mM. The largest enhancement was induced when NaCl and KCl were mixed at equimolar concentrations. Asp-Na significantly suppressed the glossopharyngeal nerve response to quinine hydrochloride, which suggests that bitterness of KCl is suppressed by Asp-Na. The salty taste enhancing effect of Asp-Na was also confirmed with human sensory tests. The present results suggested that the mixture of NaCl and KCl containing Asp-Na can be used as a salt substitute. In addition to demonstrating that Asp-Na enhanced salt taste responses in an experimental animal and human, our findings provide clues to identify the elusive salty taste receptors.

  15. Plasmodium falciparum Malaria Complicated by Symmetrical Peripheral Gangrene, Bowel Ischemia, Repeated Candidemia, and Bacteraemia

    Directory of Open Access Journals (Sweden)

    Emeline Masse

    2014-01-01

    Full Text Available A 63-year-old Caucasian woman developed severe Plasmodium falciparum malaria when travelling back from Cameroun. No antimalarial chemoprophylaxis had been observed. The patient was immediately admitted to the intensive care unit after evidence of multiple organ failure (coma, shock, acute respiratory distress syndrome, acute renal failure, etc.. However, initial parasitemia was less than 1%. The patient was managed by intravenous quinine and norepinephrine infusion due to refractory shock. The patient developed as an early complication ischemic lesions of both arms and feet. In addition to laboratory changes consistent with disseminated intravascular coagulation, there was also evidence for a low activity of the von Willebrand factor (VWF cleaving protease ADAMTS13. Later complications included repeated candidemia and bacteraemia despite appropriate therapy; the origin appeared to be diffuse ischemic injury of the gastrointestinal tract. The patient ultimately recovered, but quadriamputation was necessary to treat symmetrical peripheral gangrene (SPG. In severe Plasmodium falciparum malaria, ischemic changes may be due to microvascular obstruction, but, in patients with low parasitemia, other endothelial factors may also be involved as observed in other groups of thrombotic microangiopathies.

  16. Pathophysiological Mechanisms in Gaseous Therapies for Severe Malaria.

    Science.gov (United States)

    Kayano, Ana Carolina A V; Dos-Santos, João Conrado K; Bastos, Marcele F; Carvalho, Leonardo J; Aliberti, Júlio; Costa, Fabio T M

    2016-04-01

    Over 200 million people worldwide suffer from malaria every year, a disease that causes 584,000 deaths annually. In recent years, significant improvements have been achieved on the treatment of severe malaria, with intravenous artesunate proving superior to quinine. However, mortality remains high, at 8% in children and 15% in adults in clinical trials, and even worse in the case of cerebral malaria (18% and 30%, respectively). Moreover, some individuals who do not succumb to severe malaria present long-term cognitive deficits. These observations indicate that strategies focused only on parasite killing fail to prevent neurological complications and deaths associated with severe malaria, possibly because clinical complications are associated in part with a cerebrovascular dysfunction. Consequently, different adjunctive therapies aimed at modulating malaria pathophysiological processes are currently being tested. However, none of these therapies has shown unequivocal evidence in improving patient clinical status. Recently, key studies have shown that gaseous therapies based mainly on nitric oxide (NO), carbon monoxide (CO), and hyperbaric (pressurized) oxygen (HBO) alter vascular endothelium dysfunction and modulate the host immune response to infection. Considering gaseous administration as a promising adjunctive treatment against severe malaria cases, we review here the pathophysiological mechanisms and the immunological aspects of such therapies.

  17. Determination of Hydrazine Hydrate in Water with Paradime Thylaminobenzaldehyde Spectrophotometric Method%对二甲氨基苯甲醛分光光度法测定水中水合肼

    Institute of Scientific and Technical Information of China (English)

    黄岭; 李叙柏

    2016-01-01

    在酸性条件下,水合肼与对二甲氨基苯甲醛作用,形成黄色醌式化合物,可用分光光度法对其进行测定。文中主要介绍对二甲氨基苯甲醛分光光度法测定的回收率、相对标准偏差及检出限的复验,并对上海水源水及其出厂水水合肼进行测定。%Hydrazine hydrate can be detected using spectrophotometer,because yellow quinine compound is produced when it reacts with paradime thylaminobenzaldehyde under acidic conditions. In this paper,the recovery rate,relative standard deviation and lowest detection limit of this method were analyzed,and the hydrazine hydrate in the raw water and processed water of three water plants were determined.

  18. Surface functional groups and redox property of modified activated carbons

    Institute of Scientific and Technical Information of China (English)

    Zhang Xianglan; Deng Shengfu; Liu Qiong; Zhang Yan; Cheng Lei

    2011-01-01

    A series of activated carbons (ACs) were prepared using HNO3, H2O2 and steam as activation agents with the aim to introduce functional groups to carbon surface in the ACs preparation process. The effects of concentration of activation agent, activation time on the surface functional groups and redox property of ACs were characterized by Temperature Program Desorption (TPD) and Cyclic Voitammetry (CV). Results showed that lactone groups of ACs activated by HNO3 increase with activation time, and the carboxyl groups increase with the concentration of HNO3. Carbonyl/quinine groups of ACs activated by H2O2 increase with the activation time and the concentration of H2O2, although the acidic groups decrease with the concentration of H2O2. The redox property reflected by CV at 0 and 0.5 V is different with any kinds of oxygen functional groups characterized by TPD, but it is consistent with the SO2 catalytic oxidization/oxidation properties indicated by TPR.

  19. Analysis on the Application and Development of Antimalarials Drugs%抗疟药物的应用与发展

    Institute of Scientific and Technical Information of China (English)

    张楠

    2016-01-01

    人类在抗疟药物的应用过程中,先后经历了蚊帐、纱窗、巫术、中草药等传统办法,由金鸡纳树皮的疗效促使了奎宁、氯喹的产生,以及DDT杀虫剂和青蒿素类药物的使用,上述治疗手段和方法都对控制疟疾的传播扩散发挥了重要作用。本文通过回顾这些抗疟药物应用历程的同时,以期展望该领域的发展前景和未来趋势。%In the history, human used several ways, such as mosquito nets, screens, witchcraft, Chinese herbal medicine and other traditional ways, and due to the curative effect of cinchona bark, human find quinine and chloroquine, later, the pesticide DDT and arte-misinin drugs also can be found.All of them played an important role to control the spread of malaria.This paper is overviewed how many treatments and methods which by human used and found, and its development is also prospected.

  20. 恶性疟疾一例报告%Falciparum malaria: A case report

    Institute of Scientific and Technical Information of China (English)

    辛淑敏; 刘曼娇; 张尚珍

    2003-01-01

    临床资料 患者,男,42岁,因发热2周,出现畏寒、寒战、高热(体温40.8℃)于2002年11月12日收治入院。患者入院前2周间歇性发作畏寒、发热、头痛,尿呈茶色,下腹痛伴腹泻、恶心、呕吐10d。病史调查:患者为2002年9月自非洲布隆迪来我国的留学人员(当地为恶性疟流行地区),此前7年间患过4次疟疾,在当地用奎宁(quinine)治疗(具体方案不详)后临床治愈。此次症状发作后在外院经外周血涂片检查未查见疟原虫,曾给予抗炎及必要的对症治疗。