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Progress in studies of huperzine A,a natural cholinesterase inhibitor from Chinese herbal medicine

Acta Pharmacologica Sinica 2006年第1期27卷 1-26页

作者： Rui WANG Hart YAN Xi-can TANG State Key Lahoratory of Drug Research.Shanghai Institute of Materia Medica.Shanghai Institutes for Biological Sciences Chinese Academy of Sciences.Shanghai 201203,China State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai China

Huperzine A (HupA),a novel alkaloid isolated flom the Chinese herb Huperziaserrata,is a potent,highly specific and reversible inhibitor of acetylcholinesterase(ACHE).Compared with tacrine,donepezil,and rivastigmine,HupA has betterpenetration through the blood-brain barrier,higher oral bioavailability,and longerduration of AChE inhibitory *** has been found to improve cognitivedeficits in a broad range of animal *** possesses the ability to protectcells against hydrogen peroxide,β-amyloid protein (or peptide),glutamate,ischemia and staurosporine-induced cytotoxicity and *** protec-tive effects are related to its ability to attenuate oxidative stress,regulate theexpression of apoptotic proteins ***,P53,and caspase-3,protectmitochondria,upregulate nerve growth factor and its receptors,and interfere withamyloid precursor protein *** effects of HupA on N-me-thyl-D-aspartate receptors and potassium currents may also contribute to itsneuroprotection as *** studies in rodents,canines,and healthyhuman volunteers indicated that HupA was absorbed rapidly,distributed widelyin the body,and eliminated at a moderate rate with the property of slow andprolonged release after oral *** and clinical safety tests showedthat HupA had no unexpected toxicity,particularly the dose-limiting hepalotoxic-ity induced by *** phase Ⅳ clinical trials in China have demonstratedthat HupA significantly improved memory deficits in elderly people with benignsenescent forgetfulness,and patients with Alzheimer disease and vasculardementia,with minimal peripheral cholinergic side effects and no *** can also be used as a protective agent against organophosphateintoxication.

关键词： huperzine A Alzheimer disease acetylcholinesterase cholinesterase inhibitors cognitive enhancer neuroprotect agents oxidative stress apoptosis

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Ameliorating Effects of Thyroxine and Atropine in Phosphamidon Intoxicated Chick Embryos

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Biomedical and Environmental Sciences 1999年第1期12卷 34-42页

作者： CHATTALI GHOSH AND J.N.MEDDA (Department of Zoology, Burdwan University, Burdwan 713104,West Bengal, INDIA)J.N.MEDDA (To whom all corespondences should be addressed.E-mail:zoojnm@burdwan.ernet.in.) Burdwan University 印度

The effects of thyroxine and atropine in ameliorating phosphamidon intoxication in chick embryos was studied. Treatment of phosphamidon significantly enhanced the moriality and abnormalityrates, decreased the average body weights, and cholinesterase activity in chick embryos. When thyroxine was administered to the phosphamidon intoxicated embryos, the above parameters changedsignificantly, indicating an ameliorating effect of thyroxine against phosphamidon intoxication in chick embryos. The combined thyroxine and atropine therapy did not further improve the ameliorating effect. Since in many respects chick embryo development parallels that of mammalian embryos,a short-term use of thyroxine as a protective agent against organophosphate toxicity might be useful

关键词： Animals Atropine Body Weight Central Nervous System Chick Embryo cholinesterase inhibitors cholinesterases Dose-Response Relationship, Drug Insecticides Kidney Liver Phosphamidon Thyroxine

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Effect of cholinesterase inhibitor galanthamine on circulating tumor necrosis factor alpha in rats with lipopolysaccharideinduced peritonitis

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Chinese Medical Journal 2010年第13期123卷 1727-1730页

作者： LIU Zhi-hai MA Yue-feng WU Jun-song GAN Jian-xin XU Shao-wen JIANG Guan-yu Department of Emergency Medicine Second Affiliated Hospital Zhejiang University School of Medicine and Research Institute of Emergency Medicine Hangzhou Zhejiang 310009 China

Background The nervous system, through the vagus nerve and its neurotransmitter acetylcholine, can down-regulate the systemic inflammation in vivo, and recently, a role of brain cholinergic mechanisms in activating this cholinergic anti-inflammatory pathway has been indicated. Galanthamine is a cholinesterase inhibitor and one of the centrally acting cholinergic agents available in clinic. This study aimed to evaluate the effect of galanthamine on circulating tumor necrosis factor alpha （TNF-a） in rats with lipopolysaccharide-induced peritonitis and the possible role of the vagus nerve in the action of galanthamine. Methods Rat models of lipopolysaccharide-induced peritonitis and bilateral cervical vagotomy were produced. In the experiment 1, the rats were randomly divided into control group, peritonitis group, and peritonitis groups treated with three dosages of galanthamine. In the experiment 2, the rats were randomly divided into sham group, sham plus peritonitis group, sham plus peritonitis group treated with galanthamine, vagotomy plus peritonitis group, and vagotomy plus peritonitis group treated with galanthamine. The levels of plasma TNF-α were determined in every group. Results The level of circulating TNF-α was significantly increased in rats after intraperitoneal injection of endotoxin. Galanthamine treatment decreased the level of circulating TNF-α in rats with lipopolysaccharide-induced peritonitis, and there was significant difference compared with rats with lipopolysaccharide-induced peritonitis without treatment. The 3 mg/kg dosage of galanthamine had the most significant inhibition on circulating TNF-α level at all the three tested doses. Galanthamine obviously decreased the TNF-a level in rats with lipopolysaccharide-induced peritonitis with sham operation, but could not decrease the TNF-α level in rats with lipopolysaccharide-induced peritonitis with vagotomy. Conclusion cholinesterase inhibitor galanthamine has an inhibitory effect on TNF-α relea

关键词： cholinesterase inhibitors galanthamine tumor necrosis factor alpha vagus nerve

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Tetrahydroacridine inhibits voltage-dependent Na~+ current in guinea-pig ventricular myocytes

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Acta Pharmacologica Sinica 2004年第9期 36-42页

作者： Wei WANG, Yi-ping WANG, Guo-yuan HUState Key Laboratory of Drug Research, The First Department of Pharmacology, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China

AIM: To study the effects of tetrahydroacridine (tacrine) on voltage-gated Na+ channels in cardiac tissues. METHODS: Single ventricular myocytes were enzymatically dissociated from adult guinea-pig heart. Voltage-depe... 详细信息

关键词： Alzheimer disease cholinesterase inhibitors sodium channels tetrahydroacridine (tacrine) myocardium patch-clamp techniques

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Assessment of Pesticide Use against Tephritidae Fruit Fly and Other Pest among Small-scale Solanaceous Vegetable Farmers in Bugorhe-Kabare the Democratic Republic of Congo

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NASS Journal of Agricultural Sciences 2022年第2期4卷 27-35页

作者： Rubabura,K.JA. Ndatabaye,L.F. Lina,A.A. Muhigwa,B.JB. Agricultural Entomology laboratory Entomology SectionResearch Centre in Natural Sciences(CRSN-Lwiro)Democratic Republic of Congo Department of Biology State University of BukavuDemocratic Republic of Congo

Ninety-six farmers interviewed in Kabare,east of the DR Congo during *** majority were males(79.17%),ranging 30 to 60 years,used different pesticides in vegetable farms and the main solanaceous crops cultivated is *** use of insecticide and fungicide were high,with many different formulations of the different class types recorded in use,(20%)endocrine disruptors,(40%)cholinesterase inhibitors,(35%)carcinogen and potential carcinogens suspected to be.A lot of out of those pesticides are unregistered for general *** applied pesticide once a week and they didn’t have specific *** skin effects,headaches and dizziness are *** do not have a good system of pesticide packaging *** reducing pesticide application,we propose options of agro *** suggest that the Congolese government must create a quarantine,control and surveillance service for phytosanitary products,fruits and vegetables within the DRC country and at these ***,it needs urgent action from the federal and regional governments to formulate policy,design legislation,and enforcing for its implementation concerning the supply,transportation,storage,appropriateness,and application of harmful pesticides.

关键词： Pesticide Market gardeners’crops Farmer’s small holders Endocrine disruptors cholinesterase inhibitors

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