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Huperzine A

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https://www.readbyqxmd.com/read/28807620/muscarinic-acetylcholine-receptor-but-not-nicotinic-acetylcholine-receptor-plays-a-role-in-morphine-induced-behavioral-sensitization-in-rats
#1
Jinling Sun, Lin Tian, Ruisi Cui, Heng Ruan, Xinwang Li
Background and Aim The cholinergic system can affect drug reward. The present study aimed to examine the roles of muscarinic acetylcholine receptor (mAChR) and nicotinic acetylcholine receptor (nAChR) in morphine-induced behavioral sensitization. METHODS: To analyze the roles of mAChR and nAChR in behavioral sensitization induced by morphine (5mg/kg), seven experiments were designed. Experiments 1 and 2 examined the effects of 3, 1, and 0.3 mg/kg scopolamine and 0.2, 0.1, and 0.05mg/kg scopolamine, respectively, on the locomotor activity when administered alone...
August 11, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28807163/effect-of-chinese-herbal-medicine-on-alzheimer-s-disease
#2
Melanie-Jayne R Howes, Rui Fang, Peter J Houghton
Alzheimer's disease (AD) is reaching epidemic proportions yet treatment strategies are limited and are restricted to providing symptomatic relief for the cognitive and behavioral and psychological symptoms of dementia (BPSD). Chinese herbal medicine (CHM) has been a valuable source of medicines for centuries and research has burgeoned in recent years to understand the scientific basis for their use. Some plants have been used in CHM for AD symptoms (e.g., Polygala tenuifolia), while others are CHMs for different conditions, but they show mechanistic effects relevant to AD (e...
2017: International Review of Neurobiology
https://www.readbyqxmd.com/read/28748496/huperzine-a-alleviates-neuroinflammation-oxidative-stress-and-improves-cognitive-function-after-repetitive-traumatic-brain-injury
#3
Zhengrong Mei, Peiying Zheng, Xiangping Tan, Ying Wang, Bing Situ
Traumatic brain injury (TBI) may trigger secondary injury cascades including endoplasmic reticulum stress, oxidative stress, and neuroinflammation. Unfortunately, there are no effective treatments targeting either primary or secondary injuries that result in long-term detrimental consequences. Huperzine A (HupA) is a potent acetylcholinesterase inhibitor (AChEI) that has been used treatment of Alzheimer's disease (AD). This study aimed to explore the neuroprotective effects of HupA in TBI and its possible mechanisms...
July 26, 2017: Metabolic Brain Disease
https://www.readbyqxmd.com/read/28709849/effects-of-huperzin-a-on-the-beta-amyloid-accumulation-in-the-brain-and-skeletal-muscle-cells-of-a-rat-model-for-alzheimer-s-disease
#4
Cagatay Han Turkseven, Belgin Buyukakilli, Ebru Balli, Derya Yetkin, Mehmet Emin Erdal, Senay Gorucu Yilmaz, Leyla Sahin
AIMS: Alzheimer's Disease (AD) is characterized by a loss of cognitive function and also the accumulation of β-amyloid peptide (βAP) in the brain parenchyma, which plays an important role in this disease. However, it is often also associated with the non-cognitive symptoms such as loss of muscle function (Inclusion-Body Myositis-IBM). MAIN METHODS: Sprague-Dawley rats (13 weeks-n=68) were randomly assigned into five groups: Group C: Control; Group D: d-galactose; Group O+D: Bilateral oophorectomy+d-galactose; Group O: Bilateral oophorectomy; Group O+D+H: Bilateral oophorectomy+d-galactose+Hup-A...
September 1, 2017: Life Sciences
https://www.readbyqxmd.com/read/28640635/total-synthesis-of-huperzine-q
#5
Shun Tanimura, Satoshi Yokoshima, Tohru Fukuyama
The total synthesis of huperzine Q was accomplished. The synthesis features the construction of the cis-hydrindane skeleton via a Diels-Alder reaction and a ring contraction reaction of an epoxyketone.
June 22, 2017: Organic Letters
https://www.readbyqxmd.com/read/28625948/anticholinesterase-activity-and-identification-of-huperzine-a-in-three-mexican-lycopods-huperzia-cuernavacensis-huperzia-dichotoma-and-huperzia-linifolia-lycopodiaceae
#6
Mariana Vázquez García, Gilsane Lino von Poser, Miriam Apel, Rosa Cerros Tlatilpa, Aniceto Mendoza-Ruiz, María Luisa Villarreal, Amelia Teresinha Henriques, Alexandre Cardoso Taketa
Huperzine A (Hup A), the alkaloid produced by the Chinese medicinal plant Huperzia serrata, has been documented to be a promising agent for the treatment of Alzheimer's disease due to its potent acetylcholinesterase inhibitory (AChEI) activity. The search for anticholinesterase natural products, as well as for alternative sources of Hup A in Mexican lycopods, prompted us to investigate these plants. The action of methanolic and alkaloidal extracts of three Huperzia species (H. cuernavacensis, H. dichotoma, and H...
January 2017: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28587984/abcb1a-but-not-abcg2-played-a-predominant-role-in-limiting-the-brain-distribution-of-huperzine-a-in-mice
#7
Jiajun Li, Mei Yue, Dandan Zhou, Meiyu Wang, Hongjian Zhang
Huperzine A has been used for improving symptoms of Alzheimer's disease. Its cholinergic side effect is thought to be an exaggerated pharmacological outcome linked to its high brain or CNS concentrations. Although Huperzine A is brain penetrable, its interaction with efflux transporters (ABCB1 and ABCG2) has not been fully investigated. The aim of the present study was to characterize roles of ABCB1 and ABCG2 in the transmembrane transport of Huperzine A and identify a rate limiting step in its brain distribution...
September 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28584293/expression-and-functional-analysis-of-the-lysine-decarboxylase-and-copper-amine-oxidase-genes-from-the-endophytic-fungus-colletotrichum-gloeosporioides-es026
#8
Xiangmei Zhang, Zhangqian Wang, Saad Jan, Qian Yang, Mo Wang
Huperzine A (HupA) isolated from Huperzia serrata is an important compound used to treat Alzheimer's disease (AD). Recently, HupA was reported in various endophytic fungi, with Colletotrichum gloeosporioides ES026 previously isolated from H. serrata shown to produce HupA. In this study, we performed next-generation sequencing and de novo RNA sequencing of C. gloeosporioides ES026 to elucidate the molecular functions, biological processes, and biochemical pathways of these unique sequences. Gene ontology and Kyoto Encyclopedia of Genes and Genomes assignments allowed annotation of lysine decarboxylase (LDC) and copper amine oxidase (CAO) for their conversion of L-lysine to 5-aminopentanal during HupA biosynthesis...
June 5, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28583576/administration-of-huperzine-a-exerts-antidepressant-like-activity-in-a-rat-model-of-post-stroke-depression
#9
Yuan Du, Haiyue Liang, Leiming Zhang, Fenghua Fu
Post-stroke depression (PSD) is the most common mood disorder following a stroke, and is also the main factor limiting recovery and rehabilitation in stroke patients. The present study was aimed to investigate whether Huperzine A (HupA) has antidepressant-like activity in a rat model of PSD, which was developed by middle cerebral artery occlusion followed by an 18-day chronic unpredictable mild stress in conjunction with isolation rearing. The sucrose preference and forced swim tests were used to assess depression-like behavior...
July 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28540173/self-microemulsifying-drug-delivery-system-for-improving-the-bioavailability-of-huperzine-a-by-lymphatic-uptake
#10
Fang Li, Rongfeng Hu, Bin Wang, Yun Gui, Gang Cheng, Song Gao, Lei Ye, Jihui Tang
Huperzine A (Hup-A) is a poorly water-soluble drug with low oral bioavailability. A self-microemulsifying drug delivery system (SMEDDS) was used to enhance the oral bioavailability and lymphatic uptake and transport of Hup-A. A single-pass intestinal perfusion (SPIP) technique and a chylomicron flow-blocking approach were used to study its intestinal absorption, mesenteric lymph node distribution and intestinal lymphatic uptake. The value of the area under the plasma concentration-time curve (AUC) of Hup-A SMEDDS was significantly higher than that of a Hup-A suspension (P<0...
May 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28440575/divergent-total-syntheses-of-huperzine%C3%A2-q-lycopladine%C3%A2-b-lycopladine%C3%A2-c-and-4-epi-lycopladine%C3%A2-d
#11
Benke Hong, Dachao Hu, Jinbao Wu, Jing Zhang, Houhua Li, Yingming Pan, Xiaoguang Lei
We report herein our synthetic efforts towards the divergent syntheses of (-)-huperzine Q (1), (+)-lycopladine B (2), (+)-lycopladine C (3), and (-)-lycopladine D (4). The 10-step total synthesis of (-)-huperzine Q (1) and the first total syntheses of (+)-lycopladines B (2) and C (3) were accomplished through a series of cascade reactions. Our approach involved a Michael addition/aldol/intramolecular C-alkylation sequence to forge the 6/9 spirocycle ring, and this was followed by an ethylene-accelerated carbonyl-olefin metathesis to construct the common 6/5/9 ring system...
April 25, 2017: Chemistry, An Asian Journal
https://www.readbyqxmd.com/read/28413513/huperzine-a-inhibits-immediate-addictive-behavior-but-not-behavioral-sensitization-following-repeated-morphine-administration-in-rats
#12
Jinling Sun, Lin Tian, Ruisi Cui, Xinwang Li
Acetylcholinesterase inhibitors are regarded as promising therapeutic agents to treat addiction. The current study aimed to examine the effects of huperzine A, a cholinesterase inhibitor, on behavioral sensitization induced by repeated morphine administration and relapse induced by contextual conditioning. The present study also assessed whether the state-dependency hypothesis may explain the results. Adult rats were divided into four groups (n=8) and intraperitoneally injected with 0.2, 0.3 or 0.4 mg/kg huperzine A or saline (1 ml/kg, control), for 5 days...
April 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28330463/global-transcriptome-analysis-of-huperzia-serrata-and-identification-of-critical-genes-involved-in-the-biosynthesis-of-huperzine-a
#13
Mengquan Yang, Wenjing You, Shiwen Wu, Zhen Fan, Baofu Xu, Mulan Zhu, Xuan Li, Youli Xiao
BACKGROUND: Huperzia serrata (H. serrata) is an economically important traditional Chinese herb with the notably medicinal value. As a representative member of the Lycopodiaceae family, the H. serrata produces various types of effectively bioactive lycopodium alkaloids, especially the huperzine A (HupA) which is a promising drug for Alzheimer's disease. Despite their medicinal importance, the public genomic and transcriptomic resources are very limited and the biosynthesis of HupA is largely unknown...
March 22, 2017: BMC Genomics
https://www.readbyqxmd.com/read/28295437/a-novel-assay-to-determine-acetylcholinesterase-activity-the-application-potential-for-screening-of-drugs-against-alzheimer-s-disease
#14
Liang Peng, Zhengxing Rong, Hao Wang, Biyun Shao, Lei Kang, Hong Qi, Hongzhuan Chen
Acetycholinesterase (AChE) that regulates hydrolysis of acetylcholine (ACh) in the brain, is an important target for treatment of Alzheimer's disease (AD), a feature of which is ACh deficiency. However, the methods to precisely determine AChE activity are still under development. We developed a new method to exploit acetylcholine-d4 as a surrogate substrate of ACh and measure product choline-d4 via liquid chromatography-tandem mass spectrometry (LC-MS/MS). This assay detected activity of AChE present in the normal mouse brain, which is consistent with the standard Ellman assay that determines products spectrophotometrically...
March 10, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28219697/effect-of-salvia-miltiorrhiza-root-extract-on-brain-acetylcholinesterase-and-butyrylcholinesterase-activities-their-mrna-levels-and-memory-evaluation-in-rats
#15
Marcin Ozarowski, Przemyslaw L Mikolajczak, Anna Piasecka, Radoslaw Kujawski, Joanna Bartkowiak-Wieczorek, Anna Bogacz, Michal Szulc, Ewa Kaminska, Malgorzata Kujawska, Agnieszka Gryszczynska, Piotr Kachlicki, Waldemar Buchwald, Andrzej Klejewski, Agnieszka Seremak-Mrozikiewicz
Salvia miltiorrhiza (Lamiaceae), one of the most important and popular plants of traditional medicine of Asia, is used for the prevention and treatment of cardiovascular diseases and in central nervous system disturbances. The main aim of this study was to assess the influence of subchronic (28-fold) administration of Salvia miltiorrhiza root extract (SE, 200mg/kg, p.o.) on behavioural activity and memory of rats and to evaluate the activities of cholinesterases (AChE and BuChE) and gene expression levels of AChE and BuChE as well as of beta-secretase (BACE1) in the hippocampus and frontal cortex in vivo...
May 1, 2017: Physiology & Behavior
https://www.readbyqxmd.com/read/28125507/behavioural-effects-of-novel-multitarget-anticholinesterasic-derivatives-in-alzheimer-s-disease
#16
Lydia Giménez-Llort, Miriam Ratia, Belén Pérez, Pelayo Camps, Diego Muñoz-Torrero, Albert Badia, M Victoria Clos
The current pharmacological approach to Alzheimer's disease (AD) treatment, mostly based on acetylcholinesterase inhibitors (AChEIs), is being revisited, especially in terms of the temporal frames and the potential benefits of their noncanonic actions, raising the question of whether inhibitors of AChE might also act in a disease-modifying manner. Besides, in the last decades, the pharmacophoric moieties of known AChEIs have been covalently linked to other pharmacophores in the pursuit of multitarget hybrid molecules that are expected to induce long-lasting amelioration of impaired neurotransmission and clinical symptoms but also to exert disease-modifying effects...
April 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28111749/progress-report-on-new-antiepileptic-drugs-a-summary-of-the-thirteenth-eilat-conference-on-new-antiepileptic-drugs-and-devices-eilat-xiii
#17
REVIEW
Meir Bialer, Svein I Johannessen, René H Levy, Emilio Perucca, Torbjörn Tomson, H Steve White
The Thirteenth Eilat Conference on New Antiepileptic Drugs and Devices (EILAT XIII) took place in Madrid, Spain, on June 26-29, 2016, and was attended by >200 delegates from 31 countries. The present Progress Report provides an update on experimental and clinical results for drugs presented at the Conference. Compounds for which summary data are presented include an AED approved in 2016 (brivaracetam), 12 drugs in phase I-III clinical development (adenosine, allopregnanolone, bumetanide, cannabidiol, cannabidivarin, 2-deoxy-d-glucose, everolimus, fenfluramine, huperzine A, minocycline, SAGE-217, and valnoctamide) and 6 compounds or classes of compounds for which only preclinical data are available (bumetanide derivatives, sec-butylpropylacetamide, FV-082, 1OP-2198, NAX 810-2, and SAGE-689)...
February 2017: Epilepsia
https://www.readbyqxmd.com/read/28110700/huperzine-a-a-promising-anticonvulsant-disease-modifying-and-memory-enhancing-treatment-option-in-alzheimer-s-disease
#18
Ugur Damar, Roman Gersner, Joshua T Johnstone, Steven Schachter, Alexander Rotenberg
Alzheimer's disease (AD) is the most frequent cause of dementia. Besides cognitive deterioration, patients with AD are prone to seizures - more than 20% of patients diagnosed with AD experience at least one unprovoked seizure and up to 7% have recurrent seizures. Although available antiepileptic drugs (AEDs) may suppress seizures in patients with AD, they may also worsen cognitive dysfunction and increase the risk of falls. On the basis of preclinical studies, we hypothesize that Huperzine A (HupA), a safe and potent acetylcholinesterase (AChE) inhibitor with potentially disease-modifying qualities in AD, may have a realistic role as an anticonvulsant in AD...
February 2017: Medical Hypotheses
https://www.readbyqxmd.com/read/28089246/identification-and-characterization-of-l-lysine-decarboxylase-from-huperzia-serrata-and-its-role-in-the-metabolic-pathway-of-lycopodium-alkaloid
#19
Baofu Xu, Lei Lei, Xiaocen Zhu, Yiqing Zhou, Youli Xiao
Lysine decarboxylation is the first biosynthetic step of Huperzine A (HupA). Six cDNAs encoding lysine decarboxylases (LDCs) were cloned from Huperzia serrata by degenerate PCR and rapid amplification of cDNA ends (RACE). One HsLDC isoform was functionally characterized as lysine decarboxylase. The HsLDC exhibited greatest catalytic efficiency (kcat/Km, 2.11 s(-1) mM(-1)) toward L-lysine in vitro among all reported plant-LDCs. Moreover, transient expression of the HsLDC in tobacco leaves specifically increased cadaverine content from zero to 0...
April 2017: Phytochemistry
https://www.readbyqxmd.com/read/27900576/time-course-behavioral-safety-and-protective-efficacy-of-centrally-active-reversible-acetylcholinesterase-inhibitors-in-cynomolgus-macaques
#20
Lindsey R Hamilton, Steven C Schachter, Todd M Myers
Galantamine hydrobromide and (-)huperzine A, centrally active reversible acetylcholinesterase inhibitors, are potentially superior to the current standard, pyridostigmine bromide, as a pretreatment for organophosphorus chemical warfare nerve agent intoxication. Galantamine, huperzine, and pyridostigmine were compared for time course of acetylcholinesterase inhibition in 12 cynomolgus macaques. Although both galantamine and huperzine shared a similar time course profile for acetylcholinesterase inhibition, huperzine was 88 times more potent than galantamine...
July 2017: Neurochemical Research
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