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Huperzine

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https://www.readbyqxmd.com/read/29893085/-detection-of-huperzine-a-and-huperzine-b-in-fermentation-broth-of-endophytic-fungus-colletotrichum-gloesporioides-from-huperzia-serrate-by-hplc
#1
Liqin Hu, Xincong Kang, Pengyuan Shen, Tian Chen, Jiayin Zhang, Dongbo Liu
In this study, we established a rapid and efficient HPLC method to determine the accumulation of Huperzine A and Huperzine B in the fermentation broth of endophytic fungus Colletotrichum gloesporioides from Huperzia serrate. The chloroform extracts of fermentation broth were dissolved in methanol and filtered before injection for HPLC analysis. The analysis was performed on an Agilent Eclipse plus-C18 column (250 mm×4.6 mm, 5 μm) by isocratic elution. The mobile phase was 0.015 mol/L ammonium acetate-methanol (70:30, V/V), the flow rate was 1 mL/min and the detection wavelength was set at 308 nm...
May 25, 2018: Sheng Wu Gong Cheng Xue Bao, Chinese Journal of Biotechnology
https://www.readbyqxmd.com/read/29715428/kinetics-of-huperzine-a-dissociation-from-acetylcholinesterase-via-multiple-unbinding-pathways
#2
Jakub Rydzewski, Rafal Jakubowski, Wieslaw Nowak, Helmut Grubmüller
The dissociation of huperzine A (hupA) from Torpedo californica acetylcholinesterase (TcAChE) was investigated by 4-microsecond unbiased and biased all-atom molecular dynamics (MD) simulations in explicit solvent. We performed our study using memetic sampling (MS) for the determination of reaction pathways (RPs), metadynamics to calculate free energy, and maximum-likelihood estimation (MLE) to recover kinetic rates from unbiased MD simulations. Our simulations suggest that the dissociation of hupA occurs mainly via two RPs: a front-door along the axis of the active-site gorge (pwf) and through a new transient side-door (pws), i...
May 1, 2018: Journal of Chemical Theory and Computation
https://www.readbyqxmd.com/read/29676580/identification-of-lycopodium-alkaloids-produced-by-an-ultraviolet-irradiated-strain-of-paraboeremia-an-endophytic-fungus-from-lycopodium-serratum-var-longipetiolatum
#3
Kan'ichiro Ishiuchi, Dai Hirose, Takuma Suzuki, Waka Nakayama, Wen-Ping Jiang, Orawan Monthakantirat, Jin-Bin Wu, Susumu Kitanaka, Toshiaki Makino
12- epi-Lycopodine (1), a Lycopodium alkaloid, along with lycopodine (2) and huperzine A (3), were discovered in the mycelium of Paraboeremia sp. Lsl3KI076, a UV-irradiated strain of Paraboeremia sp. Lsl3, an endophytic fungus from Lycopodium serratum Thunb. var. longipetiolatum Spring. Additionally, a trace of 1 was isolated from Phlegmariurus nummulariifolius (Blume) Ching, and the structure was elucidated on the basis of spectroscopic data. This is the first report proving that a new naturally occurring Lycopodium alkaloid can be obtained from an endophytic fungus...
May 25, 2018: Journal of Natural Products
https://www.readbyqxmd.com/read/29670172/acetylcholine-and-necroptosis-are-players-in-follicular-development-in-primates
#4
Yongrui Du, Konstantin Bagnjuk, Maralee S Lawson, Jing Xu, Artur Mayerhofer
Acetylcholine (ACh) in the ovary and its actions were linked to survival of human granulosa cells in vitro and improved fertility of rats in vivo. These effects were observed upon experimental blockage of the ACh-degrading enzyme (ACH esterase; ACHE), by Huperzine A. We now studied actions of Huperzine A in a three-dimensional culture of macaque follicles. Because a form of programmed necrotic cell death, necroptosis, was previously identified in human granulosa cells in vitro, we also studied actions of necrostatin-1 (necroptosis inhibitor)...
April 18, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29614668/a-study-of-a-supplement-containing-huperzine-a-and-curcumin-in-dementia-patients-and-individuals-with-mild-cognitive-impairment
#5
Takeshi Tabira, Nobutoshi Kawamura
Extracts from Huperzia serrata (HS) function as a cholinesterase inhibitor and a glutamic acid receptor antagonist. We tested a supplement containing HS extracts, curcumin, and others in dementia patients and individuals with mild cognitive impairment (MCI) in an open label study. Most patients with Alzheimer's disease, dementia with Lewy bodies, and MCI individuals exhibited improvements in cognitive functions, as assessed by the Alzheimer's Disease Assessment Scale-cognitive subscale Japanese version. The scores were significantly improved at 6-12 weeks compared with baseline scores (p = 0...
2018: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/29564727/tacrine-10-hupyridone-a-dual-binding-acetylcholinesterase-inhibitor-potently-attenuates-scopolamine-induced-impairments-of-cognition-in-mice
#6
Huixin Chen, Siying Xiang, Ling Huang, Jiajia Lin, Shengquan Hu, Shing-Hung Mak, Chuang Wang, Qinwen Wang, Wei Cui, Yifan Han
Tacrine(10)-hupyridone (A10E) was designed as a dual-binding acetylcholinesterase (AChE) inhibitor from the modification of tacrine and a fragment of huperzine A. We have found that A10E effectively inhibited AChE in a mixed competitive manner, with an IC50 of 26.4 nM, which is more potent than those of tacrine and huperzine A. Most importantly, we have shown, for the first time that A10E attenuated scopolamine-induced cognitive impairments without affecting motor function in mice. A10E effectively attenuated impairments of learning and memory to a similar extent as donepezil, an inhibitor of AChE used for treating Alzheimer's disease (AD)...
March 21, 2018: Metabolic Brain Disease
https://www.readbyqxmd.com/read/29502274/the-treatment-of-cognitive-dysfunction-in-dementia-a-multiple-treatments-meta-analysis
#7
Cheng-Hwang Perng, Yue-Cune Chang, Ruu-Fen Tzang
OBJECTIVE: No cure is currently available for dementia; however, various treatments and interventions have been reported to be effective. The factors influencing the efficacy of dementia treatment have not been comprehensively evaluated. This study evaluated the factors influencing treatment effects on cognitive dysfunction in dementia by comparing the results obtained from a meta-analysis based on meta-regression. METHODS: We searched for articles, clinical trials, and meta-analyses on the efficacy of pharmacotherapy or psychosocial treatment for dementia published between 2000 and 2016 in the MEDLINE/PubMed, Cochrane Library, SCOPUS, and Airiti Library databases...
May 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29440896/intranasal-delivery-of-huperzine-a-to-the-brain-using-lactoferrin-conjugated-n-trimethylated-chitosan-surface-modified-plga-nanoparticles-for-treatment-of-alzheimer-s-disease
#8
Qingqing Meng, Aiping Wang, Hongchen Hua, Ying Jiang, Yiyun Wang, Hongjie Mu, Zimei Wu, Kaoxiang Sun
Background: Safe and effective delivery of therapeutic drugs to the brain is important for successful therapy of Alzheimer's disease (AD). Purpose: To develop Huperzine A (HupA)-loaded, mucoadhesive and targeted polylactide-co-glycoside (PLGA) nanoparticles (NPs) with surface modification by lactoferrin (Lf)-conjugated N-trimethylated chitosan (TMC) (HupA Lf-TMC NPs) for efficient intranasal delivery of HupA to the brain for AD treatment. Methods: HupA Lf-TMC NPs were prepared using the emulsion-solvent evaporation method and optimized using the Box-Behnken design...
2018: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/29329613/new-diterpenoids-isolated-from-leonurus-japonicus-and-their-acetylcholinesterase-inhibitory-activity
#9
Han-Kui Wu, Ting Sun, Feng Zhao, Li-Ping Zhang, Gang Li, Jie Zhang
Three new labdane diterpenoids, leojaponicone A (1), isoleojaponicone A (2) and methylisoleojaponicone A (3), were isolated from the herb of Leonurus japonicus. The chemical structures of these secondary metabolites were elucidated on the basis of 1D and 2D NMR, including HMQC, and HMBC spectroscopic techniques. All the new compounds were tested in vitro for their acetylcholinesterase and α-glucosidase inhibitory activity. Compounds 1-3 exhibited low inhibitory effects on α-glucosidase with respect to acarbose and exhibited high inhibitory effects on acetylcholinesterase with respect to huperzine A...
November 2017: Chinese Journal of Natural Medicines
https://www.readbyqxmd.com/read/29248451/features-and-outcomes-of-drugs-for-combination-therapy-as-multi-targets-strategy-to-combat-alzheimer-s-disease
#10
REVIEW
Atish Kumar Sahoo, Jagnehswar Dandapat, Umesh Chandra Dash, Satish Kanhar
ETHNOPHARMACOLOGICAL RELEVANCE: Alzheimer's disease (AD), a deleterious neurodegenerative disorder that impairs memory, cognitive functions and may lead to dementia in late stage of life. The pathogenic cause of AD remains incompletely understood and FDA approved drugs are partial inhibitors rather than curative. Most of drugs are synthetic or natural products as galanthamine is an alkaloid obtained from Galanthus spp. Huperzine A, an alkaloid found in Huperzia spp., gingkolides a diterpenoids from Gingko biloba and many ethnobotanicals like Withania somnifera (L...
April 6, 2018: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29219324/total-synthesis-of-huperzine-r
#11
Toshimune Nomura, Satoshi Yokoshima, Tohru Fukuyama
A total synthesis of huperzine R was accomplished. Intramolecular cycloaddition of a nitrile oxide and reductive cleavage of the resulting isoxazoline induced sequential cleavage of the C-C and C-O bonds to form the characteristic bicyclic lactam core with an enone moiety. Construction of the butenolide moiety from the enone afforded huperzine R.
January 5, 2018: Organic Letters
https://www.readbyqxmd.com/read/29196177/muscarinic-receptors-in-the-nucleus-accumbens-shell-play-different-roles-in-context-induced-or-morphine-challenged-expression-of-behavioral-sensitization-in-rats
#12
Xinhe Liu, Lin Tian, Ruisi Cui, Heng Ruan, Xinwang Li
Both drug-related cues and drug priming are the main factors that induce relapse of drug addiction. Previous research has reported that blockade of the muscarinic receptors could significantly depress addictive behavior, suggesting that the muscarinic receptors might be involved in drug use and relapse behavior. The nucleus accumbens (NAc), especially the shell of the NAc, where the muscarinic receptors are expressed, is critical for craving and relapse. This study investigated the effects of microinfusion of the muscarinic receptor antagonist scopolamine into the NAc shell on context- and morphine-induced expression of behavioral sensitization...
January 15, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29068470/aspartate-%C3%AE-semialdeyhyde-dehydrogenase-as-a-potential-therapeutic-target-of-mycobacterium-tuberculosis-h37rv-evidence-from-in-silico-elementary-mode-analysis-of-biological-network-model
#13
Saif Khan, Pallavi Somvanshi, Tulika Bhardwaj, Raju K Mandal, Sajad A Dar, Mohd Wahid, Arshad Jawed, Mohtashim Lohani, Mahvish Khan, Mohammed Y Areeshi, Shafiul Haque
The emergence of multi-drug resistant strains and co-occurrence of tuberculosis with HIV creates a major burden to the human health globally. Failure of primary antibacterial therapy necessitates the identification of new mycobacterial drugs. In this study, a comprehensive analysis involving bottom-up systems biology approach was applied wherein we have identified potential therapeutic targets of Mycobacterium tuberculosis infections. Our study prioritized M. tuberculosis therapeutic targets (aspartate-β-semialdeyhde dehydrogenase [ASD], dihydrodipicolinate reductase and diaminopimelate decarboxylase) based on flux and elementary mode analysis using direct mathematical modeling of the relevant metabolic pathways...
March 2018: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/29058298/pharmacokinetics-and-tolerability-of-oral-dosage-forms-of-huperzine-a-in-healthy-chinese-male-volunteers-a-randomized-single-dose-three-period-six-sequence-crossover-study
#14
San-Lan Wu, Jun Gan, Jing Rao, Si-Jie He, Wen-Wen Zhu, Ying Zhao, Yong-Ning Lv, Jian-Geng Huang, Ya-Ni Liu
Huperzine A is a potent, reversible, and blood-brain barrier permeable acetylcholinesterase inhibitor. The aim of this study was to compare the pharmacokinetics, tolerability, and bioavailability of two formulations with the established reference formulation of huperzine A in a fasting, healthy Chinese male population. This was a randomized, single-dose, 3-period, 6-sequence crossover study. The plasma concentrations of huperzine A were determined by liquid chromatography tandem mass spectrometry. Tolerability was assessed based on subject interview, vital sign monitoring, physical examination, and routine blood and urine tests...
October 2017: Journal of Huazhong University of Science and Technology. Medical Sciences
https://www.readbyqxmd.com/read/29054135/alterations-in-the-timing-of-huperzine-a-cerebral-pharmacodynamics-in-the-acute-traumatic-brain-injury-setting
#15
Ugur Damar, Roman Gersner, Joshua T Johnstone, Kush Kapur, Stephen Collins, Steven Schachter, Alexander Rotenberg
Traumatic brain injury (TBI) may affect the pharmacodynamics of centrally acting drugs. Paired-pulse transcranial magnetic stimulation (ppTMS) is a safe and noninvasive measure of cortical gamma-aminobutyric acid (GABA)-mediated cortical inhibition. Huperzine A (HupA) is a naturally occurring acetylcholinesterase inhibitor with newly discovered potent GABA-mediated antiepileptic capacity, which is reliably detected by ppTMS. To test whether TBI alters cerebral HupA pharmacodynamics, we exposed rats to fluid percussion injury (FPI) and tested whether ppTMS metrics of cortical inhibition differ in magnitude and temporal pattern in injured rats...
January 15, 2018: Journal of Neurotrauma
https://www.readbyqxmd.com/read/28956955/a-resurging-boom-in-new-drugs-for-epilepsy-and-brain-disorders
#16
REVIEW
Iyan Younus, Doodipala Samba Reddy
Epilepsy is one of the most common neurological diseases affecting approximately 50 million people worldwide. Despite many advances in epilepsy research, nearly a third of patients with epilepsy have refractory or pharmacoresistant epilepsy. Despite the approval of a dozen antiepileptic drugs (AEDs) over the past decade, there are no agents that halt the development of epilepsy. Thus, newer and better AEDs that can prevent refractory seizures and modify the disease are needed for curing epilepsy. Areas covered: In this article, we highlight the recent advances and emerging trends in new and innovative drugs for epilepsy and seizure disorders...
January 2018: Expert Review of Clinical Pharmacology
https://www.readbyqxmd.com/read/28807620/muscarinic-acetylcholine-receptor-but-not-nicotinic-acetylcholine-receptor-plays-a-role-in-morphine-induced-behavioral-sensitization-in-rats
#17
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 12, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28807163/effect-of-chinese-herbal-medicine-on-alzheimer-s-disease
#18
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
#19
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...
December 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
#20
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
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