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Huperzine A

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https://www.readbyqxmd.com/read/27900576/time-course-behavioral-safety-and-protective-efficacy-of-centrally-active-reversible-acetylcholinesterase-inhibitors-in-cynomolgus-macaques
#1
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...
November 30, 2016: Neurochemical Research
https://www.readbyqxmd.com/read/27848250/pharmacological-effects-of-active-components-of-chinese-herbal-medicine-in-the-treatment-of-alzheimer-s-disease-a-review
#2
Zhi-Yong Wang, Jian-Gang Liu, Hao Li, Hui-Ming Yang
Alzheimer's disease (AD), the most common neurodegenerative disorder associated with dementia, not only severely decreases the quality of life for its victims, but also brings a heavy economic burden to the family and society. Unfortunately, few chemical drugs designed for clinical applications have reached the expected preventive or therapeutic effect so far, and combined with their significant side-effects, there is therefore an urgent need for new strategies to be developed for AD treatment. Traditional Chinese Medicine has accumulated many experiences in the treatment of dementia during thousands of years of practice; modern pharmacological studies have confirmed the therapeutic effects of many active components derived from Chinese herbal medicines (CHM)...
November 16, 2016: American Journal of Chinese Medicine
https://www.readbyqxmd.com/read/27829351/recent-updates-in-imperative-natural-compounds-for-healthy-brain-and-nerve-function-a-systematic-review-of-implications-for-multiple-sclerosis
#3
Nima Sanadgol, Shahram Shahraki Zahedani, Mohammad Sharifzadeh, Roghayeh Khalseh, Gullam Reza Barbari, Mohammad Abdollahi
BACKGROUND: The evolution of the 'Green' movement in western society has changed attitudes in the general population who now perceive natural compounds as being inherently harmless and more desirable than artificial chemical products. OBJECTIVE: Considering the growing interest towards introducing naturally emerged medicines, the purpose of this review was to overview the ongoing research into prevention and treatment of multiple sclerosis (MS) lesions. METHOD: This review was carried out by searching bibliographic databases such as PubMed and Scopus for studies reported between 1th January 2008 to 30rd January 2016 on MS patients or animal models of MS, investigating the beneficial effects of natural compounds in MS treatment...
November 8, 2016: Current Drug Targets
https://www.readbyqxmd.com/read/27799911/huperzine-a-provides-robust-and-sustained-protection-against-induced-seizures-in-scn1a-mutant-mice
#4
Jennifer C Wong, Stacey B B Dutton, Stephen D Collins, Steven Schachter, Andrew Escayg
De novo loss-of-function mutations in the voltage-gated sodium channel (VGSC) SCN1A (encoding Nav1.1) are the main cause of Dravet syndrome (DS), a catastrophic early-life encephalopathy associated with prolonged and recurrent early-life febrile seizures (FSs), refractory afebrile epilepsy, cognitive and behavioral deficits, and a 15-20% mortality rate. SCN1A mutations also lead to genetic epilepsy with febrile seizures plus (GEFS+), which is an inherited disorder characterized by early-life FSs and the development of a range of adult epilepsy subtypes...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27774814/recent-progress-in-repositioning-alzheimer-s-disease-drugs-based-on-a-multitarget-strategy
#5
M Amélia Santos, Karam Chand, Sílvia Chaves
Alzheimer's disease (AD) is a serious progressive neurological disorder, characterized by impaired cognition and profound irreversible memory loss. The multifactorial nature of AD and the absence of a cure so far have stimulated medicinal chemists worldwide to follow multitarget drug-design strategies based on repositioning approved drugs. This review describes a summary of recently published works focused on tailoring new derivatives of US FDA-approved acetylcholinesterase inhibitors, in addition to huperzine (a drug approved in China), either by hybridization with other pharmacophore elements (to hit more AD targets), or by combination of two FDA-approved drugs...
October 24, 2016: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/27751854/evaluation-of-the-in%C3%A2-vitro-and-in%C3%A2-vivo-metabolic-pathway-and-cytochrome-p450-inhibition-induction-profile-of-huperzine-a
#6
Ping-Ping Lin, Xue-Ning Li, Fei Yuan, Wei-Li Chen, Meng-Jie Yang, Hong-Rong Xu
Huperzine A (HupA), one of the reversible and selective acetylcholinesterase inhibitors derived from Chinese herb Huperzia Serrata, possesses affirmative action of ameliorating cognitive dysfunction of Alzheimer's disease. Up to now, the effects of HupA on human cytochrome P450s (CYPs) have not been fully elucidated. The purpose of the present study was to clarify the metabolic pathway of HupA in vitro and in vivo, and to evaluate the CYPs inhibition/induction profile of HupA in vitro. The catalytic activity of CYP enzymes (CYP1A2, 2A6, 2C9, 2C19, 2D6, 2E1 and 3A4) was measured by the quantification of specific enzyme substrates using validated liquid chromatography-tandem mass spectrometry (LC/MS/MS) methods...
November 11, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27725508/chemical-transformation-of-an-intermediate-in-the-synthesis-of-huperzine-a-leading-to-a-diverse-array-of-molecules
#7
Satoshi Yokoshima, Masatsugu Ishikawa, Youko Beniyama, Tohru Fukuyama
Chemical transformation of an early intermediate in our synthesis of huperzine A provided a diverse array of molecules in which a variety of functional groups could be embedded.
2016: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27712576/multiple-targets-for-management-of-alzheimer-s-disease-a-review
#8
Sayeed Ahmad, Salman Akhtar, Qazi Mohammad Sajid Jamal, Syed Mohd Danish Rizvi, Mohammad A Kamal, M Kalim A Khan, Mohd Haris Siddiqui
AD is a progressive and irreversible neurodegenerative disease and the most common cause of dementia in the elderly population. Βeta- amyloid cascade formation along with several cytoskeleton abnormalities succeeding to the hyperphosphorylation of microtubule-associated tau protein in neurons leads to the elicitation of several neurotoxic incidents. As an outcome of these phenomena, steady growth of dementia in aged population is becoming ubiquitous in both developed and developing countries. Thus, the key aspiration is to endow with stable daily life functionality to the person suffering from dementia and to cut down or slower the symptoms of disease leading to disruptive behavior...
October 3, 2016: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/27659301/anti-ageing-active-ingredients-from-herbs-and-nutraceuticals-used-in-traditional-chinese-medicine-pharmacological-mechanisms-and-implications-for-drug-discovery
#9
REVIEW
Chun-Yan Shen, Jian-Guo Jiang, Li Yang, Da-Wei Wang, Wei Zhu
Ageing, an unanswered question in the medical field, is a multifactorial process that results in a progressive functional decline in cells, tissues and organisms. Although it is impossible to prevent ageing, slowing down the rate of ageing is entirely possible to achieve. Traditional Chinese medicine (TCM) is characterized by the nourishing of life and its role in anti-ageing is getting more and more attention. This article summarizes the work done on the natural products from TCM that are reported to have anti-ageing effects, in the past two decades...
September 23, 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27642355/primary-investigation-for-the-mechanism-of-biatractylolide-from-atractylodis-macrocephalae-rhizoma-as-an-acetylcholinesterase-inhibitor
#10
Yong-Chao Xie, Ning Ning, Li Zhu, Dan-Ning Li, Xing Feng, Xiao-Ping Yang
Biatractylolide was isolated from ethyl acetate extract of dried Atractylodis Macrocephalae Rhizoma root by multistep chromatographic processing. Structure of biatractylolide was confirmed by (1)H-NMR and (13)C-NMR. The IC50 on acetylcholinesterase (AChE) activity was 6.5458 μg/mL when the control IC50 value of huperzine A was 0.0192 μg/mL. Molecular Docking Software (MOE) was used to discover molecular sites of action between biatractylolide and AChE protein by regular molecular docking approaches. Moreover, biatractylolide downregulated the expression of AChE of MEF and 293T cells in a dose-dependent manner...
2016: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/27605862/huperzine-a-for-treatment-of-cognitive-impairment-in-major-depressive-disorder-a-systematic-review-of-randomized-controlled-trials
#11
REVIEW
Wei Zheng, Ying-Qiang Xiang, Gabor S Ungvari, F K Helen Chiu, Chee H Ng, Ying Wang, Yu-Tao Xiang
BACKGROUND: Acetylcholinesterase (AChE) inhibitors have been shown to be effective in treating cognitive impairment in animal models and in human subjects with major depressive disorder (MDD). Huperzine A (HupA), a Traditional Chinese Medicine derived from a genus of clubmosses known as Huperzineserrata, is a powerful AChE inhibitor that has been used as an adjunctive treatment for MDD, but no meta-analysis on HupA augmentation for MDD has yet been reported. AIM: Conduct a systematic review and meta-analysis of randomized controlled trials (RCTS) about HupA augmentation in the treatment of MDD to evaluate its efficacy and safety...
April 25, 2016: Shanghai Archives of Psychiatry
https://www.readbyqxmd.com/read/27554967/effect-of-huperzine-a-on-a%C3%AE-induced-p65-of-astrocyte-in-vitro
#12
Lushuang Xie, Cen Jiang, Zhang Wang, Xiaohong Yi, Yuanyuan Gong, Yunhui Chen, Yan Fu
Alzheimer's disease (AD) is the most common cause of dementia. Its pathology often accompanies inflammatory action, and astrocytes play important roles in such procedure. Rela(p65) is one of significant message factors in NF-κB pathway which has been reported high expression in astrocyte treated by Aβ. HupA, an alkaloid isolated from Chinese herb Huperzia serrata, has been widely used to treat AD and observations reflected that it improves memory and cognitive capacity of AD patients. To reveal its molecular mechanisms on p65, we cultured astrocytes, built Aβ-induced AD model, treated astrocytes with HupA at different concentrations, assayed cell viability with MTT, and detected p65 expression by immunohistochemistry and PCR...
December 2016: Bioscience, Biotechnology, and Biochemistry
https://www.readbyqxmd.com/read/27535978/acetylcholinesterase-inhibitors-for-alzheimer-s-disease-treatment-ameliorate-acetaminophen-induced-liver-injury-in-mice-via-central-cholinergic-system-regulation
#13
Jianqiao Zhang, Leiming Zhang, Xue Sun, Yanting Yang, Liang Kong, Chengwen Lu, Guangyao Lv, Tian Wang, Hongbo Wang, Fenghua Fu
Acetaminophen (APAP) is widely used as an analgesic and antipyretic agent, but it may induce acute liver injury at high doses. Alzheimer's disease patients, while treated with acetylcholinesterase inhibitor (AChEI), may take APAP when they suffer from cold or pain. It is generally recognized that inhibiting acetylcholinesterase activity may also result in liver injury. To clarify whether AChEI could deteriorate or attenuate APAP hepatotoxicity, the effects of AChEI on APAP hepatotoxicity were investigated. Male C57BL/6J mice were administrated with the muscarinic acetylcholine receptor (mAChR) blocker atropine (Atr), or classic α7 nicotine acetylcholine receptor (α7nAChR) antagonist methyllycaconitine (MLA) 1 hour before administration of AChEIs-donepezil (4 mg/kg), rivastigmine (2 mg/kg), huperzine A (0...
November 2016: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27498774/acetylcholinesterase-independent-protective-effects-of-huperzine-a-against-iron-overload-induced-oxidative-damage-and-aberrant-iron-metabolism-signaling-in-rat-cortical-neurons
#14
Ling-Xue Tao, Xiao-Tian Huang, Yu-Ting Chen, Xi-Can Tang, Hai-Yan Zhang
AIM: Iron dyshomeostasis is one of the primary causes of neuronal death in Alzheimer's disease (AD). Huperzine A (HupA), a natural inhibitor of acetylcholinesterase (AChE), is a licensed anti-AD drug in China and a nutraceutical in the United Sates. Here, we investigated the protective effects of HupA against iron overload-induced injury in neurons. METHODS: Rat cortical neurons were treated with ferric ammonium citrate (FAC), and cell viability was assessed with MTT assays...
November 2016: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/27476120/molecular-cloning-expression-and-functional-analysis-of-the-copper-amine-oxidase-gene-in-the-endophytic-fungus-shiraia-sp-slf14-from-huperzia-serrata
#15
Huilin Yang, Silu Peng, Zhibin Zhang, Riming Yan, Ya Wang, Jixun Zhan, Du Zhu
Huperzine A (HupA) is a drug used for the treatment of Alzheimer's disease. However, the biosynthesis of this medicinally important compound is not well understood. The HupA biosynthetic pathway is thought to be initiated by the decarboxylation of lysine to form cadaverine, which is then converted to 5-aminopentanal by copper amine oxidase (CAO). In this study, we cloned and expressed an SsCAO gene from a HupA-producing endophytic fungus, Shiraia sp. Slf14. Analysis of the deduced protein amino acid sequence showed that it contained the Asp catalytic base, conserved motif Asn-Tyr-Asp/Glu, and three copper-binding histidines...
December 2016: Protein Expression and Purification
https://www.readbyqxmd.com/read/27440195/in-vivo-blockade-of-acetylcholinesterase-increases-intraovarian-acetylcholine-and-enhances-follicular-development-and-fertility-in-the-rat
#16
Javier Urra, Jan Blohberger, Michelle Tiszavari, Artur Mayerhofer, Hernan E Lara
Growth and differentiation of ovarian follicles are regulated by systemic and local factors, which may include acetylcholine (ACh). Granulosa cells (GCs) of growing follicles and luteal cells produce ACh and in cultured GCs it exerts trophic actions via muscarinic receptors. However, such actions were not studied in vivo. After having established that rat ovarian GCs and luteal cells express the ACh-metabolizing enzyme ACh esterase (AChE), we examined the consequences of local application of an AChE inhibitor, huperzine A (HupA), by osmotic minipump delivery into the ovarian bursa of hemiovariectomized rats...
2016: Scientific Reports
https://www.readbyqxmd.com/read/27400829/huperzine-a-protects-sepsis-associated-encephalopathy-by-promoting-the-deficient-cholinergic-nervous-function
#17
Sen-Zhi Zhu, Wei-Ping Huang, Lin-Qiang Huang, Yong-Li Han, Qian-Peng Han, Gao-Feng Zhu, Miao-Yun Wen, Yi-Yu Deng, Hong-Ke Zeng
Neuroinflammatory deregulation in the brain plays a crucial role in the pathogenesis of sepsis associated encephalopathy (SAE). Given the mounting evidence of anti-inflammatory and neuroprotective effects of the cholinergic nervous system, it is surprising that there is little information about its changes in the brain during sepsis. To elucidate the role of the cholinergic nervous system in SAE, hippocampal choline acetyltransferase, muscarinic acetylcholine receptor-1, acetylcholinesterase and acetylcholine were evaluated in LPS-induced sepsis rats...
September 19, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/27392479/neuroprotective-effects-of-tongmai-yizhi-decoction-against-alzheimer-s-disease-through-attenuating-cyclin-dependent-kinase-5-expression
#18
Jing-Han Feng, Bao-Chang Cai, Wei-Feng Guo, Ming-Yan Wang, Yong Ma, Qiao-Xi Lu
OBJECTIVE: To explore the protective effects of Tongmai Yizhi Decoction (, TYD), a Chinese herb complex prescription against the impairment of cognitive functions and memory loss in amyloid beta 1-40 (Aβ1-40) peptide and ibotenic (IBO)-induced Alzheimer's disease (AD) model rats. METHODS: The in vivo model was established by injecting Aβ1-40 and IBO into left hippocampal CA1 area of Sprague-Dawley (SD) rat to mimic AD. Totally 32 SD rats were divided into 4 groups, including sham operation group, AD model group, TYD group [AD rats treated with TYD at the dosage of 19...
July 9, 2016: Chinese Journal of Integrative Medicine
https://www.readbyqxmd.com/read/27302211/adjunctive-huperzine-a-for-cognitive-deficits-in-schizophrenia-a-systematic-review-and-meta-analysis
#19
Wei Zheng, Ying-Qiang Xiang, Xian-Bin Li, Gabor S Ungvari, Helen F K Chiu, Feng Sun, Carl D'Arcy, Xiangfei Meng, Yu-Tao Xiang
OBJECTIVE: The aim of this study was to examine the efficacy of huperzine A (HupA), an isolate of Huperzine serrata, in the treatment of cognitive deficits in schizophrenia spectrum disorders. METHODS: PubMed, PsycINFO, Embase, Cochrane Library, Cochrane Controlled Trials Register, WanFang, Chinese Biomedical, and China Journal Net databases were searched from inception to 15 July 2015 for randomized controlled trials (RCTs) in English or Chinese of HupA augmentation of antipsychotic drug therapy versus placebo or ongoing antipsychotic treatment...
July 2016: Human Psychopharmacology
https://www.readbyqxmd.com/read/27239217/influence-of-the-melissa-officinalis-leaf-extract-on-long-term-memory-in-scopolamine-animal-model-with-assessment-of-mechanism-of-action
#20
Marcin Ozarowski, Przemyslaw L Mikolajczak, Anna Piasecka, Piotr Kachlicki, Radoslaw Kujawski, Anna Bogacz, Joanna Bartkowiak-Wieczorek, Michal Szulc, Ewa Kaminska, Malgorzata Kujawska, Jadwiga Jodynis-Liebert, Agnieszka Gryszczynska, Bogna Opala, Zdzislaw Lowicki, Agnieszka Seremak-Mrozikiewicz, Boguslaw Czerny
Melissa officinalis (MO, English: lemon balm, Lamiaceae), one of the oldest and still most popular aromatic medicinal plants, is used in phytomedicine for the prevention and treatment of nervous disturbances. The aim of our study was to assess the effect of subchronic (28-fold) administration of a 50% ethanol extract of MO leaves (200 mg/kg, p.o.) compared with rosmarinic acid (RA, 10 mg/kg, p.o.) and huperzine A (HU, 0.5 mg/kg, p.o.) on behavioral and cognitive responses in scopolamine-induced rats. The results were linked with acetylcholinesterase (AChE), butyrylcholinesterase (BuChE), and beta-secretase (BACE-1) mRNA levels and AChE and BuChE activities in the hippocampus and frontal cortex of rats...
2016: Evidence-based Complementary and Alternative Medicine: ECAM
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