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four new steroids from the endophytic fungus chaetomium sp. m453 derived of chinese herbal medicine huperzia serrata.an endophytic fungus, chaetomium sp. m453, was isolated from huperzia serrata (thunb. ex murray) trev. and subjected to phytochemical investigation. three unusual c25 steroids, neocyclocitrinols e-g (1-3), and 3β-hydroxy-5,9-epoxy-(22e,24r)-ergosta-7,22-dien-6-one (4) together with three known steroids were isolated from solid fermentation products of the fungus, which were elucidated by extensive spectroscopic analyses, including 1d-, 2d-nmr, and hr-esi-ms experiments. the absolute configuratio ...201728041908
jatrophihabitans huperziae sp. nov., an endophytic actinobacterium isolated from surface-sterilized tissue of the medicinal plant huperzia serrata (thunb.).a novel endophytic actinobacterium, designated strain cpcc 204076t, was isolated from surface-sterilized tissue of the medicinal plant huperzia serrata (thunb.) collected from sichuan province, south-west china. the taxonomic position of the isolate was investigated by a polyphasic approach. the strainwas aerobic, gram-stain-positive, non-motile, non-spore-forming and rod-shaped. growth was observed at 10-37 °c, at ph 5.0-10.0 and with 0-3.0 % (w/v) nacl. the polar lipid fraction consisted of di ...201627413046
isolation, diversity and acetylcholinesterase inhibitory activity of the culturable endophytic fungi harboured in huperzia serrata from jinggang mountain, china.huperzia serrata has many important medicinal properties with proven pharmacological potential. some of these properties may be mediated by its endophytic fungi. to test this hypothesis, in the present study, we provided a first insights into evaluating the species composition and acetylcholinesterase (ache) inhibitory activity of the culturable endophytic fungi of h. serrata from the regional at jinggang mountain in southeastern china. a total number of 885 fungal isolates distributed across 44 ...201626745980
molecular evolution and functional characterization of a bifunctional decarboxylase involved in lycopodium alkaloid biosynthesis.lycopodium alkaloids (las) are derived from lysine (lys) and are found mainly in huperziaceae and lycopodiaceae. las are potentially useful against alzheimer's disease, schizophrenia, and myasthenia gravis. here, we cloned the bifunctional lysine/ornithine decarboxylase (l/odc), the first gene involved in la biosynthesis, from the la-producing plants lycopodium clavatum and huperzia serrata we describe the in vitro and in vivo functional characterization of the l. clavatum l/odc (lcl/odc). the r ...201627303024
vascular contributions to cognitive impairment and treatments with traditional chinese medicine.the prevalence of cognitive impairment and dementia caused by cerebrovascular disease is likely to increase with the global aging population. vascular contributions to cognitive impairment and dementia (vcid) is a wide spectrum term used to include a diverse heterogeneous group of cognitive syndromes with vascular factors regardless of the cause of pathogenesis. vcid ranges from mild cognitive impairment to full-blown dementia with vascular dementia (vad) as the most severe stage. it is further ...201628042305
molecular cloning, expression, and functional analysis of the copper amine oxidase gene in the endophytic fungus shiraia sp. slf14 from huperzia serrata.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 ...201627476120
de novo rna sequencing and transcriptome analysis of colletotrichum gloeosporioides es026 reveal genes related to biosynthesis of huperzine a.huperzine a is important in the treatment of alzheimer's disease. there are major challenges for the mass production of huperzine a from plants due to the limited number of huperzine-a-producing plants, as well as the low content of huperzine a in these plants. various endophytic fungi produce huperzine a. colletotrichum gloeosporioides es026 was previously isolated from a huperzine-a-producing plant huperzia serrata, and this fungus also produces huperzine a. in this study, de novo rna sequenci ...201525799531
avertoxins a-d, prenyl asteltoxin derivatives from aspergillus versicolor y10, an endophytic fungus of huperzia serrata.aspergillus versicolor y10 is an endophytic fungus isolated from huperzia serrata, which showed inhibitory activity against acetylcholinesterase. an investigation of the chemical constituents of y10 led to the isolation of four new prenylated asteltoxin derivatives, named avertoxins a-d (2-5), together with the known mycotoxin asteltoxin (1). in the present study, we report structure elucidation for 2-5 and the revised nmr assignments for asteltoxin and demonstrated that avertoxin b (3) is an ac ...201526618211
huperzine a alleviates mechanical allodynia but not spontaneous pain via muscarinic acetylcholine receptors in mice.chronic pain is a major health issue and most patients suffer from spontaneous pain. previous studies suggest that huperzine a (hup a), an alkaloid isolated from the chinese herb huperzia serrata, is a potent analgesic with few side effects. however, whether it alleviates spontaneous pain is unclear. we evaluated the effects of hup a on spontaneous pain in mice using the conditioned place preference (cpp) behavioral assay and found that application of hup a attenuated the mechanical allodynia in ...201526697233
endophytes in the plant huperzia serrata: fungal diversity and discovery of a new pentapeptide.endophytic fungi are an underexploited resource of natural products and have a capacity to produce diverse classes of plant-derived secondary metabolites. here, we investigated the diversity of endophytic fungi from huperzia serrata and the potential for discovering novel fungal natural products. one hundred and fifty-five endophytic fungi isolates obtained from h. serrata, belonging to four classes dothideomycetes (47.3 %), sordariomycetes (36.8 %), eurotiomycetes (10.6 %) and an undefined clas ...201525526853
diterpenoids from the endophytic fungus botryosphaeria sp. p483 of the chinese herbal medicine huperzia serrata.two new tetranorlabdane diterpenoids, named botryosphaerins g (1) and h (2), were isolated from the solid fermentation products of botryosphaeria sp. p483 along with seven known tetranorlabdane diterpenes (3-9). their structures were elucidated by extensive analysis, including 1d and 2d nuclear magnetic resonance (nmr) spectroscopy, and high-resolution electrospray ionization mass spectrometry (hr-esi-ms). their absolute configuration was confirmed by single-crystal x-ray diffraction analyses us ...201526393542
efficient strategy for maintaining and enhancing the huperzine a production of shiraia sp. slf14 through inducer elicitation.huperzine a (hupa), a naturally occurring lycopodium alkaloid, is a potent, highly specific and reversible inhibitor of acetylcholinesterase and is a potential treatment for alzheimer's disease. however, isolating hupa from huperziaceae plants is inefficient; thus, extracting this compound from endophytic fungi may be more controllable and sustainable. however, the large-scale production of this chemical from endophytes is limited by the innate instability of endophytic fungi. in this study, we ...201424865990
identification of a novel endophytic fungus from huperzia serrata which produces huperzine a.huperzine a is isolated from huperzia serrata and is used for treatment of alzheimer's disease, due to its low toxicity and long effective period. the decrease in h. serrata sources means that natural huperzine a cannot meet the needs of clinical therapy. in this study, >200 endophytic fungal strains were isolated from h. serrata, and screened using high-performance liquid chromatography. strain es026 produced huperzine a. production was identified and quantified by liquid chromatography-tandem ...201425212543
[cloning, prokaryotic expression and characterization of lysine decarboxylase gene from huperzia serrata].huperzine a is a promising drug to treat alzheimer's disease (ad). to date, its biosynthetic pathway is still unknown. lysine decarboxylase (ldc) has been proposed to catalyze the first-step of the biosynthesis of huperzine a. to identify and characterize ldcs from huperzia serrata, we isolated two ldc fragments (ldc1 and ldc2) from leaves of h. serrata by rt-pcr and then cloned them into pmd 19-t vector. sequence analysis showed that ldc1 and ldc2 genes shared 95.3% identity and encoded the pro ...201425507483
[cloning, prokaryotic expression and characterization of lysine decarboxylase gene from huperzia serrata].huperzine a is a promising drug to treat alzheimer's disease (ad). to date, its biosynthetic pathway is still unknown. lysine decarboxylase (ldc) has been proposed to catalyze the first-step of the biosynthesis of huperzine a. to identify and characterize ldcs from huperzia serrata, we isolated two ldc fragments (ldc1 and ldc2) from leaves of h. serrata by rt-pcr and then cloned them into pmd 19-t vector. sequence analysis showed that ldc1 and ldc2 genes shared 95.3% identity and encoded the pro ...201425423760
multitarget drugs of plants origin acting on alzheimer's disease.the etiopathology of alzheimer's disease (ad) is extremely complex and heterogeneous, often associated with comorbidities. as a result it may be unlikely that ad may be mitigated by drug acting on a single specific target. the current tendency in drug design and discovery in ad is the rational design or "serendipitous" discovery of new drug entities challenging multiple targets. since two of the presently approved drugs for ad are based on natural products (galantamine and the physostigmine-deri ...201323410167
molecular cloning and characterization of copper amine oxidase from huperzia serrata.a cdna encoding a novel copper amine oxidase (cao) was cloned and sequenced from the chinese club moss huperzia serrata (huperziaceae), which produces the lycopodium alkaloid huperzine a. a 2043-bp open reading frame encoded an mr 76,854 protein with 681 amino acids. the deduced amino acid sequence shared 44-56% identity with the known caos of plant origin, and contained the active site consensus sequence of asn-tyr-asp/glu. the phylogenetic tree analysis revealed that hscao from the primitive v ...201222901898
[screening of endophytic fungi from huperzia serrata for acetylcholinesterase inhibitory activity and its taxonomic identification].to screen out fungus strains with acetylcholinesterase inhibitory activity from huperzia serrata.201223627163
[cloning, expression and functional identification of a type iii polyketide synthase gene from huperzia serrata].a cdna encoding novel type iii polyketide synthase (pks) was cloned and sequenced from young leaves of chinese club moss huperzia serrata (thunb.) trev. by rt-pcr using degenerated primers based on the conserved sequences of known chss, and named as h. serrata pks2. the terminal sequences of cdna were obtained by the 3'- and 5'-race method. the full-length cdna of h. serrata pks2 contained a 1212 bp open reading frame encoding a 46.4 kda protein with 404 amino acids. the deduced amino acid seque ...201122242464
biotransformation of ursolic acid by an endophytic fungus from medicinal plant huperzia serrata.endophytic fungi were used not only for their producing bioactive products but also for their ability to transform natural compounds. an endophytic fungus, isolated from medicinal plant huperzia serrata, was identified as umbelopsis isabellina based on the internal transcribed spacer of ribosomal dna (rdna-its) region. it was used to transform ursolic acid (1), a pentacyclic triterpene. incubation of ursolic acid with u. isabellina afforded three products, 3β-hydroxy-urs-11-en-28,13-lactone (2), ...201121881267
[isolation of endophytic fungi from huperzia serrata and their acetylcholinesterase inhibitory activity].a total of 127 strains of endophytic fungi were isolated from roots, branches and leaves of huperzia serrata. these strains were identified into 19 genera based on morphological characters and ribosomal dna (rdna) sequence analysis, there into penicillium, aspergillus and podospora were dominant populations in h. serrata. from analysis results we found some endophytic fungi showed a certain degree of tissue preference. the isolation rate and colonization rate of stems were both larger than those ...201121710741
the role of phytochemicals in the treatment and prevention of dementia.dementia pathologies such as alzheimer's disease (ad) are reaching epidemic proportions, yet they are not successfully managed by effective symptomatic treatments. only five drugs have been developed to alleviate cognitive symptoms, and more effective and safe treatments are needed for both the cognitive symptoms and behavioural and psychological symptoms of dementia (bpsd). as two of these licensed drugs (cholinesterase inhibitors [cheis]) are naturally derived (galantamine and rivastigmine), t ...201121639405
are herbal compounds the next frontier for alleviating learning and memory impairments? an integrative look at memory, dementia and the promising therapeutics of traditional chinese medicines.recent advances in neuroscience have revealed a greater, in-depth understanding of the complexities associated with memory. contemporary theories hold that an integral relationship between memory formation, stabilization and consolidation revolve around plasticity of neuronal networks. the associated requisite receptors a-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (ampa) and n-methyl-d-aspartate (nmda) and cellular mechanisms surrounding plasticity (posed to incite molecular functionali ...201121305632
the role of natural products in the discovery of new drug candidates for the treatment of neurodegenerative disorders ii: alzheimer's disease.the present review is part ii in a series (part i focuses on parkinson's disease) that addresses the value of natural product chemistry in the discovery of medicines for the treatment of neurodegenerative disorders. data reviewed document that a host of products from plant species and derivatives have neuroprotectant effects in vitro and in vivo. in addition, besides neuroprotection, natural products also demonstrate biological effects that target biochemical pathways underlying associated sympt ...201120874701
traditional chinese medicines and alzheimer's disease.traditional chinese medicines have been widely investigated for the treatment of alzheimer's disease (ad) because none of the current therapies-either the cholinesterase inhibitors or antagonist of n-methyl-d-aspartate receptors-has profound effects on halting the progression of ad. in recent years, scientists have isolated many active compounds from herbs, which can alleviate dementia and neurodegenerative syndrome with fewer side effects than conventional drugs and, thus, are regarded as promi ...201121791295
an overview on natural cholinesterase inhibitors--a multi-targeted drug class--and their mass production.cholinesterase enzyme family consisting of acetylcholinesterase (ache) and butrylcholinesterase (bche) is important in pathogenesis of alzheimer's disease (ad), explained by "cholinergic hypothesis". accordingly, deficiency of the neuromediator called "acetylcholine" excessive amount of bche has been well-described in the brains of ad patients. consequently, cholinesterase inhibition has become one of the most-prescribed treatment strategies for ad. in fact, cholinesterase inhibitors have been a ...201121762104
multihydroxylation of ursolic acid by pestalotiopsis microspora isolated from the medicinal plant huperzia serrata.the structural modification of ursolic acid by an endophytic fungus pestalotiopsis microspora, isolated from medicinal plant huperzia serrata was reported for the first time. the structure diversity was very important for the sar study of ursolic acid and its derivatives. incubation of ursolic acid 1 with p. microspora afforded four metabolites: 3-oxo-15α, 30-dihydroxy-urs-12-en-28-oic acid (2), 3β, 15α-dihydroxy-urs-12-en-28-oic acid (3), 3β, 15α, 30- trihydroxy-urs-12-en-28-oic acid (4) and 3, ...201121767617
comparison of 454-ests from huperzia serrata and phlegmariurus carinatus reveals putative genes involved in lycopodium alkaloid biosynthesis and developmental regulation.plants of the huperziaceae family, which comprise the two genera huperzia and phlegmariurus, produce various types of lycopodium alkaloids that are used to treat a number of human ailments, such as contusions, swellings and strains. huperzine a, which belongs to the lycodine type of lycopodium alkaloids, has been used as an anti-alzheimer's disease drug candidate. despite their medical importance, little genomic or transcriptomic data are available for the members of this family. we used massive ...201020854695
intrathecal huperzine a increases thermal escape latency and decreases flinching behavior in the formalin test in rats.huperzine a (hupa) is an alkaloid isolated from the chinese club moss huperzia serrata and has been used for improving memory, cognitive and behavioral function in patients with alzheimer's disease in china. it has nmda antagonist and anticholinesterase activity and has shown anticonvulsant and antinociceptive effects in preliminary studies when administered intraperitoneally to mice. to better characterize the antinociceptive effects of hupa at the spinal level, holtzman rats were implanted wit ...201020026382
isolation and characterization of endophytic huperzine a-producing fungi from huperzia serrata.huperzia serrata is a producer of huperzine a (hupa), a cholinesterase inhibitor (chei). over 120 endophytic fungi were recovered from this plant and screened for hup-a and nine were found. these nine represented seven different fungal genera with the most significant producer being shiraia sp. a total of 127 endophytic fungi isolates obtained from the root, stem, and leaf segments of h. serrata were grouped into 19 genera based on their morphological traits and sequence analysis of the internal ...201021107640
lycopodium alkaloids from huperzia serrata.a new lycopodane-type lycopodium alkaloid, 6α-hydroxy-5,15-oxide-lycopodane (1), and seven known alkaloids were isolated from the whole plants of huperzia serrata. their structures were elucidated by means of spectroscopic methods. 12-deoxyhuperzine o (2) was reported as a naturally occurring alkaloid for the first time, and showed an antagonist effect on the n-methyl-d-aspartate receptor with an ic(50) value of 0.92 μm.201021061224
a novel endophytic huperzine a-producing fungus, shiraia sp. slf14, isolated from huperzia serrata.to characterize and identify a novel huperzine a (hupa)-producing fungal strain slf14 isolated from huperzia serrata (thunb. ex murray) trev. in china.201020602655
[research advances of huperzia serrata (thunb.) trev].qiancengta, a traditional chinese medicine produced from the whole plant of the club moss huperzia serrata, has been used for a long history in china for treatment of a number of ailments, including contusions, strains, swellings, schizophrenia, myasthenia gravis and noworganophosphate poisoning. it has become known worldwide as a medicinal plant since chinese scientists discovered huperzine a from it in the 1980s, which is reversible, potent and selective acetylcholine esterase (ache) inhibitor ...200919938535
in vitro production of huperzine a, a promising drug candidate for alzheimer's disease.alzheimer's disease (ad) is growing in impact on human health. with no known cure, ad is one of the most expensive diseases in the world to treat. huperzine a (hupa), a anti-ad drug candidate from the traditional chinese medicine qian ceng ta (huperzia serrata), has been shown to be a powerful and selective inhibitor of acetylcholinesterase and has attracted widespread attention because of its unique pharmacological activities and low toxicity. as a result, hupa is becoming an important lead com ...200818538805
huperzine a from huperzia species--an ethnopharmacolgical review.huperzine a (hupa), isolated originally from a traditional chinese medicine qiang ceng ta, whole plant of huperzia serrata (thunb. ex murray) trev., a member of the huperziaceae family, has attracted intense attention since its marked anticholinesterase activity was discovered by chinese scientists. several members of the huperziaceae (huperzia and phlegmariurus species) have been used as medicines in china for contusions, strains, swellings, schizophrenia, myasthenia gravis and organophosphate ...200717644292
crystallization and preliminary crystallographic analysis of an acridone-producing novel multifunctional type iii polyketide synthase from huperzia serrata.polyketide synthase 1 (pks1) from huperzia serrata is a plant-specific type iii polyketide synthase that shows an unusually versatile catalytic potential, producing various aromatic tetraketides, including chalcones, benzophenones, phlorogulucinols and acridones. recombinant h. serrata pks1 expressed in escherichia coli was crystallized using the hanging-drop vapour-diffusion method. the crystals belonged to space group i222 or i2(1)2(1)2(1), with unit-cell parameters a = 73.3, b = 85.0, c = 137 ...200717620714
an acridone-producing novel multifunctional type iii polyketide synthase from huperzia serrata.a cdna encoding a novel plant type iii polyketide synthase was cloned and sequenced from the chinese club moss huperzia serrata (huperziaceae). the deduced amino acid sequence of hu. serrata polyketide synthase 1 showed 44-66% identity to those of other chalcone synthase superfamily enzymes of plant origin. further, phylogenetic tree analysis revealed that hu. serrata polyketide synthase 1 groups with other nonchalcone-producing type iii polyketide synthases. indeed, a recombinant enzyme express ...200717250741
progress in studies of huperzine a, a natural cholinesterase inhibitor from chinese herbal medicine.huperzine a (hupa), a novel alkaloid isolated from the chinese herb huperzia serrata, is a potent, highly specific and reversible inhibitor of acetylcholinesterase(ache). compared with tacrine, donepezil, and rivastigmine, hupa has better penetration through the blood-brain barrier, higher oral bioavailability, and longer duration of ache inhibitory action. hupa has been found to improve cognitive deficits in a broad range of animal models. hupa possesses the ability to protect cells against hyd ...200616364207
a survey of potential huperzine a natural resources in china: the huperziaceae.the huperziaceae is comprised of two genera, huperzia and phlegmariurus. because of the content of lycopodium alkaloids like huperzine a, which are used to treat a number of human ailments, plants of the huperziaceae are experiencing a rapid decline in china, mostly due to over-harvesting. because of this trend, we engaged from 1995 to 2001 in an investigation of the natural resources of the huperziaceae in china. the main objectives of this study were: to catalog huperziaceae plant resources in ...200616203116
is there a better source of huperzine a than huperzia serrata? huperzine a content of huperziaceae species in china.a precise and selective reversed phase high-performance liquid chromatographic method was developed for quantifying huperzine a (hupa) in samples of the huperziaceae in china. this method was used to quantify the levels of hupa in samples of huperzia serrata collected from a single population at different times of the year, in different organs of the same h. serrata plant, and from different geographical locations of h. serrata plants in china. for different species of huperziaceae, the highest ...200515740012
the psychopharmacology of huperzine a: an alkaloid with cognitive enhancing and neuroprotective properties of interest in the treatment of alzheimer's disease.huperzine a (hupa), extracted from a club moss (huperzia serrata), is a sesquiterpene alkaloid and a powerful and reversible inhibitor of acetylcholinesterase (ache). it has been used in china for centuries for the treatment of swelling, fever and blood disorders. it has demonstrated both memory enhancement in animal and clinical trials and neuroprotective effects. recently it has undergone double-blind, placebo-controlled clinical trials in patients with alzheimer's disease (ad), with significa ...200312895686
acetylcholinesterase complexed with bivalent ligands related to huperzine a: experimental evidence for species-dependent protein-ligand complementarity.acetylcholinesterase (ache) inhibitors improve the cognitive abilities of alzheimer patients. (-)-huperzine a [(-)-hupa], an alkaloid isolated from the club moss, huperzia serrata, is one such inhibitor, but the search for more potent and selective drugs continues. recently, alkylene-linked dimers of 5-amino-5,6,7,8-tetrahydroquinolinone (hupyridone, 1a), a fragment of hupa, were shown to serve as more potent inhibitors of ache than (-)-hupa and monomeric 1a. we soaked two such dimers, (s,s)-(-) ...200312517147
huperzine a attenuates amyloid beta-peptide fragment 25-35-induced apoptosis in rat cortical neurons via inhibiting reactive oxygen species formation and caspase-3 activation.huperzine a, a novel lycopodium alkaloid originally discovered in the chinese herb qian ceng ta (huperzia serrata), is a reversible, potent, and selective acetylcholinesterase (ache) inhibitor and has been extensively used for the treatment of alzheimer's disease (ad) in china. the present studies were designed to investigate effects of huperzine a on amyloid beta-peptide fragment 25-35 (abeta25-35)-induced neuronal apoptosis and potential mechanisms in primary cultured rat cortical neurons. aft ...200211754078
new lycopodium alkaloids from huperzia serrata.three new lycopodium alkaloids, 11alpha-hydroxyphlegmariurine b (2), 7alpha-hydroxyphlegmariurine b (3) and 7alpha,11alpha-dihydroxyphlegmariurine b (4) along with a known compound, phlegmariurine b (1), were isolated from the herb huperzia serrata. the structures of the above compounds were elucidated based on spectroscopic studies.200211859480
long-term potentiation in hippocampus of rats is enhanced by endogenous acetylcholine in a way that is independent of n-methyl-d-aspartate receptors.by using extracellular recordings of field potential, the exact pathway by which the endogenous ach influencing the induction of long-term potentiation (ltp) in ca1 area was analysed in slices of rat hippocampus. the results showed that: (1) the application of (-) huperzine a, an ache inhibitor extracted from chinese herb qian ceng ta (huperzia serrata), could enhance the induction of ltp, while this drug showed little effect on the second components of multiple population spikes that were recor ...200111226632
effects of huperzine used as pre-treatment against soman-induced seizures.huperzine a (hup), an alkaloid isolated from the chinese club moss, huperzia serrata is a reversible inhibitor of cholinesterases which crosses the blood-brain barrier and shows high specificity for acetylcholinesterase (ache) and a prolonged biological half-life. we tested, in vivo, its efficiency in protecting cortical ache from soman inhibition and preventing subsequent seizures. the release of acetylcholine (ach) was also followed in the cortex of freely moving rats using microdialysis techn ...200111307848
the nmda receptor ion channel: a site for binding of huperzine a.huperzine a (hup-a), first isolated from the chinese club moss huperzia serrata, is a potent, reversible and selective inhibitor of acetylcholinesterase (ache) over butyrylcholinesterase (bche) (life sci. 54: 991-997). because hup-a has been shown to penetrate the blood-brain barrier, is more stable than the carbamates used as pretreatments for organophosphate poisoning (op) and the hup-a:ache complex has a longer half-life than other prophylactic sequestering agents, hup-a has been proposed as ...200111920920
second generation cholinesterase inhibitors: effect of (l)-huperzine-a on cortical biogenic amines.l-huperzine-a (hup-a), a natural cholinesterase inhibitor (chei) derived from the chinese herb huperzia serrata, was administered systemically (i.p.) or locally through the microdialysis probe into the rat cortex. systemic hup-a significantly increased acetylcholine (ach) levels above baseline at doses of 0.1, 0.3, and 0.5 mg/kg; the increases were 54%, 129%, and 220%, respectively. norepinephrine (ne) and dopamine (da) levels were also increased 121% and 129% above baseline at 0.3 mg/kg, and 14 ...19957500384
development of natural products as drugs acting on central nervous system.we have recently studied several natural product constituents which have effects on the cns. (1) tetrahydropalmatine (thp) and its analogues were isolated from corydalis ambigua and various species of stephania. (+)-thp and (-)-thp possess not only analgesic activity, but also exert sedative-tranquilizing and hypnotic actions. results of receptor binding assay and their pre- and post-synaptic effects on dopaminergic system indicate that (-)-thp and (-)-stepholidine are dopamine receptor antagoni ...19911841995
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