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Effects of huperzine a on secretion of nerve growth factor in cultured rat cortical astrocytes and neurite outgrowth in rat PC12 cells

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Acta Pharmacologica Sinica 2005年第6期26卷 673-678页

作者： Li-li TANG, Rui WANG, Xi-can TANG~2 State Key Laboratory 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

Aim: To study the effects of huperzine a (HupA) on neuritogenic activity and the expression of nerve growth factor (NGF). Methods: After being treated with 10 μmol/L HupA, neurite outgrowth of PC 12 cells was observed and counted under phase-contrast microscopy. Mitogenic activity was assayed by [~3H]thymidine incorporation. Cell cytotoxicity was evaluated by lactate dehydrogenase (LDH) release. AChE activity, mRNA and protein expression were measured by the Ellman’s method, RT-PCR, and Western blot, respectively. NGF mRNA and protein levels were determined by RT-PCR and ELISA assays. Results: Treatment of PC 12 cells with 10 渭mol/L HupA for 48 h markedly increased the number of neurite-bearing cells, but caused no significant alteration in cell viability or other signs of cytotoxicity. In addition to inhibiting AChE activity, 10 渭mol/L HupA also increased the mRNA and protein levels of this enzyme. In addition, following 2 h exposure of the astrocytes to 10 渭mol/L HupA, there was a significant up-regula-tion of mRNA for NGF and P75 low-affinity NGF receptor. The protein level of NGF was also increased after 24 h treatment with HupA. Conclusion: Our findings demonstrate for the first time that HupA has a direct or indirect neurotrophic activity, which might be beneficial in treatment of neurodegenerative disorders such as Alzheimer disease.

关键词： huperzine a nerve growth factor neurite outgrowth: acetylcholinesterase inhibitors

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Self-microemulsifying drug delivery system for improving the bioavailability of huperzine a by lymphatic uptake

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Acta Pharmaceutica Sinica B 2017年第3期7卷 353-360页

作者： Fang Li Rongfeng Hu Bin Wang Yun Gui Gang Cheng Song Gao Lei Ye Jihui Tang Anhui University of Chinese Medicine Hefei 230038China National Chinese Medicinal Materials Products Quality Supervision and Inspection Center(Anhui) Bozhou 236800China Key Laboratory of Xin'an Medicine Ministry of Education Hefei 230038China Anhui“115”Xin'an Traditional Chinese Medical Research&Development Innovation Team Hefei 230038China Anhui Province Key Laboratory of R&D of Chinese Medicine Hefei 230038China School of Pharmacy Anhui Medical UniversityHefei 230022China

huperzine a(Hup-A) is a poorly water-soluble drug with low oral bioavailability. A selfmicroemulsifying 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 <0.01).The absorption rate constant(K_a) and the apparent permeability coefficient(P_(app)) for Hup-A in different parts of the intestine suggested a passive transport mechanism, and the values of K_a and P_(app) of Hup-A SMEDDS in the ileum were much higher than those in other intestinal segments. The determination of Hup-A concentration in mesenteric lymph nodes can be used to explain the intestinal lymphatic absorption of Hup-A SMEDDS. For Hup-A SMEDDS, the values of AUC and maximum plasma concentration(C_(max)) of the blocking model were significantly lower than those of the control model(P<0.05). The proportion of lymphatic transport of Hup-A SMEDDS and Hup-A suspension were about 40% and 5%,respectively, suggesting that SMEDDS can significantly improve the intestinal lymphatic uptake and transport of Hup-A.

关键词： huperzine a Self-microemulsion Drug delivery systems SMEDDS Bioavailability Single-pass intestinal perfusion Lymphatic transport

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Comparative studies of huperzine a,donepezil,and rivastigmine on brain acetylcholine,dopamine,norepinephrine,and 5-hydroxytryptamine lev-els in freely-moving rats

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Acta Pharmacologica Sinica 2006年第9期27卷 1127-1136页

作者： Yan-qi LIANG Xi-can TANG~2 State Key Laboratory of Drug Research,Shanghai Institute of Materia Medica,Shanghai Instituties for Biological Sciences,Graduate School of the Chinese Academy of Sciences,Chinese Academy of Sciences,Shanghai 201203.China State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Instituties for Biological Sciences Graduate School of the Chinese Academy of Sciences Chinese Academy of Sciences Shanghai China

Aim:To assess the effects of cholinesterase inhibitors huperzine a,donepeziland rivastigmine on cerebral neurotransmitters in the cortex and hippocampus infreely-moving ***:Double-probe cerebral microdialysis and HPLC withelectrochemical detection were used to detect ***:Ourresults showed that huperzine a(0.***.0.5,and 0.75μmol/kg,po)dose-depen-dently elevated extracellular acetylcholine(ACh)levels in the medial prefrontalcortex(mPFC)and *** administration of donepezil(5.4μmol/kg)orrivastigmine(1μmol/kg)also elicited significant increases in ACh in the mPFC *** time course of cortical acetylcholinesterase(ACHE)inhibitionwith the 3 inhibitors minored the increases of ACh at the same *** markedelevation of ACh after oral administration of huperzine a(0.5μmol/kg)anddonepezil(5.4μmol/kg)was associated with a significantly increased release ofdopamine(DA)in the mPFC or *** of the 3 inhibitors affectednorepinephrine(NE)and 5-hydroxytryptamine(5-HT)levels in the mPFC *** effects of huperzine a and rivastigmine did not depend on theroute of administration,but donepezil was less efficacious by the oral route thanby ip *** ability of huperzine a to increase ACh levels was unchangedwhen tests were performed after multiple oral administration of the drug at 0.5μmol/kg,once per day for 30 ***:The present findings showed that,inmolar terms,huperzine a had similar potency on increasing mPFC ACh and DAlevels as compared to the 11-and 2-fold dosages of donepezil and rivastigmine,respectively,and had longer lasting effects after oral dosing.

关键词： huperzine a donepezil rivastigmine acetylcholine dopamine norepinephrine 5-hydroxy tryptamine Alzheimer’s disease rats

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Drug brain distribution following intranasal administration of huperzine a in situ gel in rats

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Acta Pharmacologica Sinica 2007年第2期28卷 273-278页

作者： Yan ZHAO Peng YUE Tao TAO~2 Qing-hua CHEN Shanghai Institute of Pharmaceutical Industry,Shanghai 200040,China Shanghai Institute of Pharmaceutical Industry Shanghai China

Aim:To determine the uptake extent of huperzine a(Hup A)into the brain afterintranasal administration of Hup A in situ gel to rats,and to compare the pharma-cokinetic parameters between intranasal administration and iv and ***:Hup A was administered to male Sprague-Dawley rats via nasal,iv and oral routesat the dose of 166.7,166.7,and 500 μg/kg,*** and brain tissuesamples including the cerebrum,hippocampus,cerebellum and olfactory bulbwere collected,and the concentrations of Hup A in the samples were assayed *** area under the concentration-time curve(AUC0→6 h)and the ratio ofthe AUCbrain to the AUCplasma(drug targeting efficiency,DTE)were calculated toevaluate the brain targeting efficiency of the drug via 3 administration ***:The AUC0→6 h of the drug in the cerebrum,hippocampus,cerebellum,left olfactory bulb and right olfactory bulb after intranasal administration of theHup A in situ gel were 1.5,1.3,1.0,1.2,and 1.0 times of those after iv administrationof the injection,and 2.7,2.2,1.9,3.1,and 2.6 times of those after administration ofthe oral *** AUCbrain0→6 h/AUCplasma0→6 h of HupAin the cerebrum,hippocampus and left olfactory bulb following the intranasal administration dosewere significantly higher(P<0.05)than the iv ***:Intranasal deliv-ery showed a viable,non-invasive strategy for delivering the drug into brain.

关键词： huperzine a in situ gel brain distribution intranasal administration

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

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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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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

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Journal of Huazhong University of Science and Technology(Medical Sciences) 2017年第5期37卷 795-802页

作者：伍三兰甘珺饶静贺思洁朱雯雯赵瑛吕永宁黄建耿刘亚妮 Department of Pharmacy Union Hospital Tongji Medical College Huazhong University of Science and Technology Clinical Research Organization for Pharmaceutical Products Union Hospital Tongji Medical College Huazhong University of Science and Technology Department of Pharmaceutics School of Pharmacy Tongji Medical College Huangzhong University of Science and Technology

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. The mean（SD） pharmacokinetic parameters of the reference drug were Cmax, 1.550（0.528） ng/m L; t1/2, 12.092（1.898） h; AUC0-72 h, 17.550（3.794） ng·h/m L. Those of the test formulation A and test formulation B were Cmax, 1.412（0.467）, 1.521（0.608） ng/m L; t1/2, 12.073（2.068）, 12.271（1.678） h; AUC0-72 h, 15.286（3.434） ng·h/mL, 15.673（3.586） ng·h/m L. The 90% confidence intervals for the AUC0-72 h and Cmax were between 0.80 and 1.25. No adverse events were reported by the subjects or found with results of clinical laboratory test. The test and reference products met the regulatory criteria for bioequivalence in these fasting, healthy Chinese male volunteers. All three formulations appeared to be well tolerated.

关键词： huperzine a pharrnacokinetics bioequivalence tolerability liquid chromatography tandem mass spectrometry

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Transcellular transport characteristics of huperzine alone or in combination with ginkgolide B across Caco-2 and Madin-Darby canine kidney cell monolayer

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Asian Pacific Journal of Tropical Medicine 2014年第11期7卷 889-894页

作者： Wen-Cui Zhao Zhi-Hong Hou Qi Zhang Wei Zheng Pharmacy Department 208th Hospital of PLA. Hospital Office 208th Hospital of PLA. Infirmary 208th Hospital of PLA.

Objective:To study the various processes involved in transcellular transport(TT) of huperzine a alone or in combination with ginkgolide B in Caco-2 and Madin-Darby canine renal(MDCK)cell ***:The transepithelial passage was assayed in the apical-to-basolateral(AP to BL) direction and opposite direction(BL to AP) in both cell *** determination of huperzine a and ginkgolide B were performed by high performance liquid chromatography(HPLC).The passage rates of huperzine a and ginkgolide B were ***-directional TT(absorption and secretion) were taken in huperzine a and ginkgolide B in Caco-2 and MDCK cell ***:TT absorption and secretion kinetics of huperzine a and ginkgolide B across two cells existed at the same *** passage rates of huperzine a were increased significantly with adding different concentrations of ginkgolide ***:The compound preparations of HA in combination with CB for dementia caused by cerebral ischemic have synergistic effects on the pharmacodynamics,and improve the bioavailability through BBB.

关键词： Caco-2 huperzine a Ginkgohde B Madin-Darby canine renal Transcellular Transport

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A new approach to the bicyclo[3.3.1]nonane framework of huperzine a-like molecules via palladium-catalyzed intramolecular γ-arylation

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Science China Chemistry 2012年第6期55卷 1097-1100页

作者： DING Rui LU YunYu YAO HeQuan SUN BingFeng LIN GuoQiang CAS Key Laboratory of Synthetic Chemistry of Natural Substances Shanghai Institute of Organic Chemistry CAS Shanghai 200032 China Department of Medicinal Chemistry School of Pharmacy China Pharmaceutical University Nanjing 210009 China

In our synthetic studies toward huperzine a, a diastereoselective α＇-alkylation of the α-amido-γ-methyl hexenone 4 was real- ized through a dianion intermediate which significantly enhanced the reactivity. Under the attempted Heck reaction conditions, an unexpected and unprecedented palladium-catalyzed intramolecular T-arylation of 3 was observed, which generated 18 with bicyclo[3.3, l]nonane framework in satisfactory yield.

关键词： huperzine a bicyclo[3.3.1]nonane γ-arylation

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huperzine a protects neural stem cells against Aβ induced apoptosis in a neural stem cells and microglia co-culture system

Huperzine A protects neural stem cells against Aβ induced a...

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2016年广东省药师周大会

作者： Ning Zhu Jizong Lin Kewan Wang Meidan Wei Qingzhuang Chen Yong Wang Department of Pharmacy Zhujiang HospitalSouthern Medical University Department of Hepatobiliary Surgery the Third Affiliated HospitalSun Yat-Sen University Department of Neurosurgery Nanfang HospitalSouthern Medical University

Objectives This study aims to explore whether huperzine a(Hup A) could protect neural stem cells against Amyloid beta-peptide Aβ induced apoptosis in a neural stem cells(NSCs) and microglia co-culture system Methods Rat NSCs and microglial cells were isolated,cultured and identified with immunofluorescence Assays(IFA).Co-culture systems of NSCs and microglial cells were employed using Transwell Permeable *** effects of Aβ1-42 on NSCs were studied in 4 groups using co-culture systems:NSCs,Aβ+NSCs,co-culture and Aβ+co-culture ***(Brd U) incorporation and flow cytometry were utilized to assess the differences of proliferation,differentiation and apoptosis of NSCs between the *** test was performed to assess the amounts of IL-6,TNF-α and MIP-α secreted,and flow cytometry and Western blotting were used to assess apoptosis of NSCs and the expressions of Bcl-2 and Bax in each *** IFA results showed that isolated rat NSCs were nestin-positive and microglial cells were CD11 b/*** all the groups,the Aβ+co-culture group has the lowest Brd U expression level,the lowest MAP2-positive,Ch AT-positive cell counts and the highest NSC apoptosis *** amounts of IL-6,TNF-α and MIP-α were being secreted by microglial cells in the Hup A+Aβ+co-culture group compared with those in the Aβ+co-culture *** the Bcl-2:Bax ratio was much higher in the Hup A+Aβ+co-culture group than in the Aβ+co-culture *** Hup A inhibits cell apoptosis through restraining microglia’s inflammatory response induced by Aβ.

关键词： huperzine a Alzheimer’s disease Amyloid beta-peptide neural stem cells microglial cells

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huperzine a ameliorates experimental autoimmune encephalomyelitis via the suppression of T cell-mediated neuronal inflammation in mice

Huperzine A ameliorates experimental autoimmune encephalomye...

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中国神经科学学会第十届全国学术会议

作者： Jun WANG Fu CHEN Yan Chen Peng ZHENG Wei-Juan DENG Jia YUAN Bo PENG Ruo-Chen WANG Wen-Jun LIU Hui Zhao Yan-Qing Wang Gen-Cheng WU Department of Integrative Medicine & Neurobiology State Key Laboratory of Medical NeurobiologyInstitute of Acupuncture ResearchSchool of Basic Medical SciencesFudan University

huperzine a(HupA),a sesquiterpene alkaloid and a potent and reversible inhibitor of acetylcholinesterase,possesses potential anti-inflammatory properties and is used for the treatment of certain neurodegenerative diseases,such as Alzheimer’s ***,it is still unknown whether this chemical is beneficial in the treatment of multiple sclerosis,a progressive inflammatory disease of the central nervous *** this study,we examined the immunomodulatory properties of HupA in experimental autoimmune encephalomyelitis(EAE),a T-cell mediated murine model of multiple *** following results were obtained:(1) Intraperitoneal injections of HupA significantly attenuate the neurological severity of EAE in mice.(2) HupA decreases the accumulation of inflammatory cells,autoimmune-related demyelination and axonal injury in the spinal cords of EAE mice.(3) HupA down-regulates mRNA levels of the pro-inflammatory cytokines(IFN-γ and IL-17) and chemokines(MCP-1,RANTES,and TWEAK)while enhancing levels of anti-inflammatory cytokines(IL-4 and IL-10) in the spinal cords of EAE mice.(4) HupA inhibits MOG stimulation-induced T-cell proliferation and IFN-γ and IL-17 secretion in cultured splenocytes.(5)HupA inhibition of T-cell proliferation is reversed by the nicotinic acetylchotinergic receptor antagonist *** conclude that HupA can ameliorate EAE by suppressing autoimmune responses,inflammatory reactions,subsequent demyelination and axonal injury in the spinal ***,HupA may have a potential therapeutic value for the treatment of multiple sclerosis and as a neuroimmunomodulatory drug to control human CNS pathology.

关键词： huperzine a spinal cord multiple sclerosis experimental autoimmune encephalomyelitis inflammation demyelination

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