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Acorus tatarinowii is the dried rhizome of the Araceae plant Acorus tatarinowii Schott.Acorus tata-rinowii was first recorded in Shennong's Classic of Mate-ria Medica.It was used for the treatment of epilepsy,amnesia,insomnia,tinnitus,deafness,silent diarrhea,and other diseases.Alzheimer's disease(AD),also known as senile dementia,is a degenerative disease of the central nervous system.It is mainly manifested as neuropsychiatric symptoms such as progressive memory impairment,cognitive dysfunction,personality changes and language disorders.Acorus tatarinowii mainly con-tains phenylpropylene,lignans,alkaloids,sugars,organic acids and amino acids,among which volatile compo-nents such as β-asarone are the main active compo-nents.The main mechanism of action of Acorus tatari-nowii in the prevention and treatment of AD is as follows:① Improve memory ability.Increasing the expression of brain-derived neurotrophic factor(BDNF),extracellular signal-regulated kinase(ERK)and adenosine cyclic phosphate response element binding protein(CREB)can improve cognitive dysfunction.Studies have shown that Acorus tatarinowii can increase the expression of BDNF,ERK,CREB and tyrosine receptor kinase B in the hippo-campus of mice to varying degrees.It can significantly improve the memory ability of memory-impaired mice,so as to achieve the purpose of prevention and treatment of AD.② Anti-oxidative stress.Studies have shown that Acorus tatarinowii can reduce the production of malondi-aldehyde in skeletal muscle,increase superoxide dis-mutase activity and total antioxidant capacity,and repair the balance of oxidative stress.③ Acetylcholinesterase inhibition.The loss of consciousness caused by deficiency of kidney essence in AD patients is related to the patho-logical changes of the cholinergic nervous system.The results showed that Acorus tatarinowii could significantly increase the contents of glutamate and acetylcholine in the cerebral cortex of AD model mice,and decrease the activity of acetylcholinesterase,to achieve the anti-AD effect.④ Anti-inflammatory and neuroprotective effects.The damage of neurons in the brain of AD patients is related to the excessive inflammatory immune response of nerve cells including microglia and astrocytes.The results showed that Acorus tatarinowii can inhibit the autophagy of microglia in rats with cerebral hemorrhage,and has neuroprotective effect,to achieve the effect of anti-AD.In this study,the effects of Acorus tatarinowii on AD were reviewed to further clarify its pharmacological ef-fects,and to provide a basis for clinical application and research.
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Objective:To study the water soluble chemical constituents in rhizoma of Acorus tatarinowii and transformation pathway of nucleosides in the process of water extraction. Method:Compounds were isolated and purified by column chromatography on macroporous resin，Sephadex LH-20，ODS and preparative HPLC. Their structures were identified on the basis of physicochemical properties and spectral data. Nucleosides were identified from aqueous extract of A. tatarinowii，and their stability was investigated by HPLC. The possible transformation pathways of nucleosides in aqueous extract of A. tatarinowii were studied by nucleotide addition test. Result:Eleven compounds including four nucleosides，four phenylpropanoids，two alkaloids and a furfural were isolated，and identified as uridine（1），adenine（2），guanosine（3），adenosine（4），5-hydroxymethylfurfural（5），5-（hydroxymethyl）-1H-pyrrole-2-carboxaldehyde（6），（threo）1'，2'-dihydroxyasarone（7），（erythro）1'，2'-dihydroxyasarone（8），acoraminol A（9），acoraminol B（10），and tatarine A（11）. The chromatographic peaks of compounds 1-4 and cytidine were identified from aqueous extract of A. tatarinowii by HPLC. After ultrasonic extraction for 0.5 h，the stability of nucleosides in water was poor. After ultrasonic extraction for 3 h or refluxing extraction for 0.5 h，the stability of nucleosides in water was good. Four transformation pathways including 5'-cytidylic acid→cytidine，uridine monophosphate→uridine，guanosine monophosphate，guanosine and adenosine-5'-monophosphate，adenosine 5'-diphosphate，adenosine 5'-triphosphorate，adenosine，adenine might exist in water extract of A. tatarinowii. Conclusion:Compounds 1-4 and 6 were isolated from the genus Acorus for the first time. These compounds further enriched the chemical constituents of A. tatarinowii. The stability and transformation pathway of nucleosides in A. tatarinowii provides reference data for the analysis of nucleosides in A. tatarinowii and other traditional Chinese medicine.
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In this study, solid dispersion technology was used to develop volatile oil from Acorus tatarinowii self-nanoemulsion dropping pills(VOA-SNEDDS-DP) and its protective effect on acute myocardial ischemia injury was evaluated. Taking exterior quality, weight variation and the resolving time as comprehendsive evaluation indexes, the preparation process and formulation of the dropping pills were optimized by orthogonal design, and the dissolution rate in vitro of the optimized VOA-SNEDDS-DP was investigated. The rat model of acute myocardial ischemia was induced by intraperitoneal injection of isoproterenol hydrochloride and the serum levels of superoxide dismutase(SOD), malondialdehyde(MDA), creatine kinase(CK) and pathological changes of myocardial tissue were determined to evaluate therapeutic effect of the dropping pills on acute myocardial ischemia. The results showed that the optimal formulation and preparation process of VOA-SNEDDS-DP were as follows: PEG6000-PEG8000 was 1∶1, proportion of VOA-SNEDDS and matrix was l∶2.5, the temperature of drug fluids was 75 ℃, drop rate was 35 drops/min, drop distance was 5 cm, the condensing agent temperature was 2-10 ℃. The content of β-asarone in the dropping pills was 42.46 mg·g~(-1). The accumulated dissolution rate of the dropping pills reached 93.85% in 10 min. The results of pharmacodynamic experiments showed that VOA-SNEDDS-DP could significantly increase the SOD content(P<0.05), reduce the levels of MDA and CK(P<0.05) in serum, and effectively improve the pathological morphology of myocardial tissue. These results revealed that the preparation of VOA-SNEDDS-DP by solid dispersion technology was stable and feasible, and VOA-SNEDDS-DP had protective effect on acute myocardial ischemia injury.
Subject(s)
Animals , Rats , Acorus , Chemistry , Creatine Kinase , Blood , Drugs, Chinese Herbal , Pharmacology , Malondialdehyde , Blood , Myocardial Ischemia , Drug Therapy , Oils, Volatile , Pharmacology , Plant Oils , Pharmacology , Superoxide Dismutase , BloodABSTRACT
OBJECTIVE： To isolate and identify the compositions of alkaloids in Acorus tatarinowii， and to lay the foundation for further study of its pharmacological activity. METHODS： The compositions of alkaloids from A. tatarinowii was separated by cation exchange resin. UPLC-MS method was used to identify the alkaloids. The separation was performed on a Agilent Zorbax Eclipse Plus-C18 column with mobile phase consisted of 0.1％ formic acid-acetonitrile （gradient elution） at a flow rate of 0.3 mL/min. The column temperature was 30 ℃， and the injection volume was 1 μL. ESI ion source was used to detect the fragments， the ion mode scan was positive. Peakview 1.2 and other softwares were used to analyze the compositions of alkaloids. RESULTS： 86 compositions were separated and 5 alkaloids were identified， such as tatarine A， N-trans-feruloyltyramine， N-lauryldiethanolamine， phytosphingosine and 5-butyluridine. CONCLUSIONS： The results of the study lay a foundation for the study of pharmacological activity of alkaloids from A. tatarinowii.
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OBJECTIVE: To study the chemical constituents from the stems of Acorus tatarinowii Schott. METHODS: The chemical constituents were isolated from the 70% ethanol-soluble extract of the stems of Acorus tatarinowii Schott and purified by a series of column chromatography methods, including MCI, silica gel, Sephadex LH - 20, HPLC and so on, and their structures were identified by physical chemical constants and NMR techniques. RESULTS: A total of twelve compounds were isolated and identified as (7S, 8R) -4, 9'-dihydroxyl-3, 3'-dimethoxyl-7, 8-dihydrobenzofuran-1'-propylneolignan (1), (-) -lyoniresinol (2), dihydrocubebin (3), evofolin B(4), (+) -icariol A2 (5), β-sitosterol(6), (+) -13-hydroxyspathulenol(7), aromadendrane-4β, 10β-diol(8), anomallenodiol( 9), (9CI) -cis-4-(3, 4-dihydroxy-2, 6, 6-trimethyl-1-cyclohexen-1-yl) -2-butanone (10), (3E) -rel-4-[(3R, 4S) -3, 4-dihydroxy- 2, 6, 6 -trimethyl-1-cyclohexen-1-yl]-3-buten-2-one(11), and ixerol B(12), respectively. CONCLUSION: Compounds 2 - 4 and 7 - 12 are isolated from the genus Acorus for the first time, and compound 5 is isolated from this plant for the first time.
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Objective To explore the intestinal absorption-promoting effect of volatile oils of Shichangpu, benzoin and storax on Rhodamine-123 (Rho-123) and its mechanisms. Methods Rat in vitro everted gut sac (EGS) model was made. The EGS was filled with 1.0 mL K-R solution, and suspended in 45.0 mL 37℃ K-R solution with or without 60 μg/mL volatile oils of Shichangpu, benzoin or storax. After incubation for 30 min, Rho-123 was added in the experimental solution outside the EGS. Rho-123 content in the EGS was determined by high-performance liquid chromatography-fluorescence detector. The human colon carcinoma cell lines Caco-2 were cultured in DMEM and incubated with 80 μg/mL volatile oils of Shichangpu, benzoin or storax for 48 h. P-glycoprotein (P-gp) expression in Caco-2 cells was assessed using flow cytometry, and P-gp gene MDR1 mRNA expression was determined by qPCR. Results The volatile oils of Shichangpu, benzoin and storax each significantly increased the absorption rate constant and apparent permeability coefficient of Rho-123 in rat jejunum and ileum (P<0.01), reduced P-gp expression and MDR1 mRNA level in Caco-2 cells (the decreased rates of P-gp expression were 53.15%, 55.10% and 61.86%, and of MDR1 mRNA levels were 55.41%, 16.24% and 38.46%, P<0.01). Conclusion Inhibiting the protein and MDR1 mRNA expressions of P-gp may be one of the main mechanisms of volatile oils of Shichangpu, benzoin and storax in promoting Rho-123 intestinal absorption.
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Objective: To analyze the effect of extrusion factors such as extrusion speed, screen hole diameter, and extrusion times on the texture properties of extrudate and the quality of pellets. Methods: In this study, microcrystalline cellulose (MCC) as pelletization aid, lactose, Methocel E5 HPMC, Methocel E15 HPMC, Methocel K100 HPMC, and eight kinds of herbal extracts (extracts of Areca catechu, Patrinia scabiosae folia, Acorus tatarinowii, Sargentodoxa cuneata, Psoralea corylifolia, Dachuanxiong Decoction, Ligusticum chuanxiong, and Gastrodia elata) were used as model drugs. Extrudates were prepared under different levels of process parameters, and one part was used to measure the texture parameters, the other part used for quality evaluation after spheronization. Results: With a large screen hole diameter, it showed that hardness of extrudate became lower and the adhesiveness as well as the springiness was significantly higher, leading to a large particle size and poor roundness of pellets. Repeated extrusion could increase hardness, cohesiveness, chewiness, and resilience of extrudate. Not any strong correlation was found between the extrusion speed and texture properties in the study. Conclusion: The extrusion process could be purposefully selected to prepare ideal pellets accroding to texture properties of extrudate.
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Objective To investigate the different components of Acorus tatarinowii and Polygala tenuifolia(volatile oil, aqueous extract)on the expression of phosphorylated Tau protein at site Ser396 and Tau-5 in the hippocampus of rats with Alzheimer′s disease(AD). Methods Male Sprague Dawley rats were randomly divided into 8 groups:normal control group, model control group,low-,middle-,and high-dose groups of volatile oil of Acorus tatarinowii and Polygala tenuifolia,and low-, middle-,and high-dose groups of aqueous extract of Acorus tatarinowii and Polygala tenuifolia. The subacute aging model was established by intraperitoneal injection of D-galactose( D-gal). Rats were given different components of Acorus tatarinowii and Polygala tenuifolia(crude drug dosage,0.6,1.2,1.8 g·kg-1 )in experimental groups,and 0.9% sodium chloride solution in normal control group and model control group,by gavage for 28 days.The levels of phosphorylated Tau protein at site Ser396 and Tau-5 were detected in hippocampal tissues by Western blotting and immunohistochemistry. Results The levels of phosphorylated Tau protein at site Ser396 were significantly enhanced in the model control group,as compared with those in normal control group (P0.05). Conclusion Acorus tatarinowii and Polygala tenuifolia could promote the dephosphorylation of Ser396 site of Tau protein in the hippocampus of AD rats,with the aqueous extract component having better effects.
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Currently, Chinese materia medica is a research hotspot on the treatment of Alzheimer's disease (AD). The extracts from Acorus tatarinowii have a variety of pharmacological effects on the central nervous system, among which the volatile oil and β-asarone are the main active ingredients in A. tatarinowii reported on the effect on improving the learning and memory and prevention of AD. This review focuses on the main active ingredients in A. tatarinowii and progresses in their different therapeutic effects and proposed pharmacological mechanisms for AD on the basis of referring to the relevant literatures at home and abroad.
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Objective To study antidepressant effect and mechanism of different polar fraction of Acorus tatarinowii Schott.on depression mouse model and explore the mechanism. Methods Different polar fractions were prepared by systematic solvent method. The adult dose recommended by Chinese Pharmacopeia ( 10 g?d-1 ) was converted to the dose of mouse. Intragastric administration was performed.A total of 80 male mice was randomly divided into normal control group,model control group and different polar fraction groups of Acorus tatarinowii Schott.. Depression mouse model was established by chronic unpredictable mild stimulation ( CUMS) with solitary feeding,and external performance of mice of different groups was observed. After 21-day feeding,blood was harvested from eyes of the mice.Concentrations of triiodothyronine (T3),tetraiodothyronine (T4), thyroid-stimulating hormone ( TSH) ,adrenocorticotrophic hormone ( ACTH) in mouse plasma and 5-hydroxy tryptamine ( 5-HT) , ACTH in brain were measured by ELISA method. Results Concentrations of T3 , T4 and ACTH in model control group [(1.203±0.042),(44.80±2.21),(11.27±0.50) ng?mL-1] were significantly increased as compared with the normal control group [(0.794±0.028),(24.87±1.25),(7.04±0.24) ng?mL-1] (P<0.05).Concentration of 5-HT in brain (146.87±10.96) was significantly decreased as compared with that of normal group ( 237. 11 ± 21. 87 ) ng?L-1 , and concentration of ACTH (58.94±4.46) ng?L-1 was significantly increased as compared with that of normal group [(38.89±2.26) ng?L-1,P<0.05)]. Concentrations of T3[(0.824±0.067),(0.812±0.051),(0.943±0.049) ng?mL-1],T4[(25.97±1.96),(27.53±1.88), (31.26±1.97) ng?mL-1] and ACTH [(7.21±0.40),(7.58±0.39),(8.69±0.42) ng?mL-1] in extraction group,cyclohexane group and chloroform group were significantly decreased as compared with model control group. At the recommendation dose of Chinese Pharmacopeia,concentrations of 5-HT in brain [(219.59±10.48),(202.19±11.95),(186.96±10.29) ng?L-1] were significantly increased,and concentrations of ACTH [(41.65±2.65),(44.87±2.95),(47.75±3.06) ng?L-1] were decreased ( P<0.05) . Conclusion Mouse model of CUMS shows typical depression symptom,and the symptom has relationship with the concentrations of endocrine hormones of T3 , T4 , ACTH, 5-HT, etc. Extraction and low polar fractions ( cyclohexane, and chloroform) of Acorus tatarinowii Schott. can partly correct incretion disorder of depression model, which may be parts of the reasons why Acorus tatarinowii Schott.exerts anti-depressant effect.
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Objective To research the correlation on high performance liquid chromatography (HPLC) and antidepressant effect of different elution fractions of acorus tatarinowii schott macroporous resin .Methods Prepared different fractions by using AB‐8 macroporous resin .Establish HPLC characteristic chromatograms of crude drugs and different elution fractions from AB‐8 acorus tatarinowii schott macroporous resin by using gradient elusion .Confirm characteristic peaks in chromatograms .despair mod‐els of male mice ,including tails suspension test (TST ) ,forced swimming test (FST ) were used to evaluate antidepressant effects by taking orally .Results HPLC chromatograms of crude drugs and different fraction of acorus tatarinowii schott showed that they had same characteristic peaks .Elution of 90% and 70% alcohol solution from AB‐8 macroporous resin can obviously reduce TST and FST time .The anti‐depressant effect were associated with characteristic peaks on chromatogram .Conclusion Acorus tatarinowii schott has anti‐depressant effect ,and mainly from 70% and 90% alcohol solution eluted from AB‐8 macroporous resin .HPLC char‐acteristic chromatography and data relationship between relative peaks can be used to judge the antidepressant effects of acorus ta‐tarinowii schott ,and give reference to research and product development .
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Objective: To study the chemical constituents from the roots and rhizomes of Acorus tatarinowii. Methods: Using different chromatographic methods to isolate and purify the constituents of A. tatarinowii, and their structures were identified by physicochemical properties and spectroscopic technology. Results: Thirteen compounds were isolated and identified as fumaric acid (1), nicotinic acid (2), p-hydroxybenzonic acid (3), uracil (4), N-trans-feruloyltyramine (5), thymine (6), variecolorquinone A (7), butanedioic acid (8), tatarol (9), tataroside-12-β-D-glucoside (10), β-sitosterol (11), 2, 5-dimethoxy- benzoquinone (12), and 5-hydroxymethyl-2-furaldehyde (13). Conclusion: Compounds 1-7 are isolated from the plants in Acorus L. for the first time.
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Objective: To investigate the influence of Acorus gramineus (Soland), a crude extract, SCP01, and a purified component, SCP02, and of Rosmarinus officinalis L., X0728 on human mast cells (HMC-1 Cell Line). Methods: Current-voltage of P2X7 receptors on human mast cell membrane activated by ATP was recorded by the whole-cell patch clamp technique. Results: The current at-100 mV mediated by P2X7was inhibited by (27.6±2.0) % in the presence of 40 μg/mL SCP01 and by (29.5±2.2) % in the presence of 40 μg/mL SCP02, which was identified as α-asarone. 42 μg/mL of the commercially available α-asarone inhibited the P2X7-mediated current by (52.2±2.0) %. In contrast to SCP01 and SCP02, 40μg/mL X0728 provoked stimulation of the current by (28.6±2.8) %. All effects were voltage-independent. Conclusion: The inhibition of P2X7by α-asarone will inhibit intracellular calcium increase and this may account for the inhibition of reported excitotoxic cell death. The pharmacological function of P2X7stimulation by X0728 needs further investigation.
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OBJECTIVE:To optimize the inclusion process of the volatile oil of Pogostemon cablin and Acorus tatarinowii in Xiaoyu anshen capsule.METHODS:The inclusion process was carried out by saturated water solution method.And the inclusion process was optimized by orthogonal experiment with the inclusion ratio and yield of the volatile oil as indexes taking the ratio of volatile oil to ?-CD,the temperature and the time of inclusion as factors.The physical phase of the inclusion complex was detected by differential scanning calorimetry(DSC).RESULTS:The optimum inclusion process was established as follows:the ratio of oil to ?-CD=1∶8;the ratio of water to ?-CD=10∶1;the inclusion time was 1h and the inclusion temperature was 50 ℃.The inclusion rate was as high as 90%.The DSC revealed that a new physical phase has been formed for the inclusion complex.CONCLUSION:The intermolecular inclusion complex with good stability and high yield of volatile oil could be obtained from the optimized inclusion process.
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Objective To observe the effect of ?-asarone combined with eugenol against PC12 cell injury induced by amyloid beta protein (A?25-35) and to explore the advantage of compatibility of monomers in herbs.Methods PC12 cells injury were induced by A?25-35.The morphological features and survival rate of PC12 cells as well as the changes of intracellular Ca2+concentration and NO concentration were observed after administration.Results The optimum combination was 10?mol/L ?-asarone+3 ?mol/L eugenol,which can decrease the concentration of intracellular Ca2+,inhibit the production of NO and increase the survival rate of PC12 cells.Conclusion The combination of effective components in Acorus tatarinowii has a better protective effect on A?25-35-induced PC12 cell injury than Acorus tatarinowii.
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Naoxing oral preparation has ho formed to be effective for ischemic stroke by preliminary clin-ical trial. To find a safe, efficient and convenient preparation Naoxing nasal spray was developed. Theeffect of Naoxing nasal spray on increasing hypoxic toleance of brain cells and improving blood circulationwas confirmed in this experiment. Twenty-eight guinea Pigs were randomly allocated to 4 groups: Group A(Naoxing nasal spray),Group B (ninodipine injection intraperitoneally), GrouP C (ligushazine injectionintrqperitoneally) and Group D(distilled water for nasal spray). After the medication for 4 days, acutecerebral ischemia was produced by the occlusion of bilatelal caretid arteries for 45 minutes. Serum NO lev-el,superoxide dismutase(SOD), glutathione superoxidase (GSH--Px) and lipid peroxide (LPO) levelsin cerebral tissue were detected. Ultrastructure of right hippocampus was oberved.The results showedthat NO, SOD, GSH-Px level in Group A is significantly higher and LPO level is significantly lower thanthere in Group D(P0.05).The damage of neuron, gliocyte and capillary under electron microscope was less thanGroup D,the differences being not significant as compared with Group B and C. It is concluded that theeffect of Naoxing nasal splay is as ed as ninodipine and ligustazine injection.
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Objective To prepare Shichangpu Double Layer Tablets. Methods The release of the sustained-release layer (SRL) was used as the response parameters and uniform design with alterable levels was used to optimize the recipe of SRL of Shichangpu Double Layper Tablets. Fast-release layer (FRL) was made from water extraction by ultra-filtration. Results The dissolution kinetics of SRL could follow zero-order equation and FRL showed good prosperities for fast release in 10 min. Conclusion The in vitro release of SRL of Shichangpu Double Layer Tablets testifies the significant sustained release action and FRL disintigrates rapidly. The preparation technology of Shichangpu Double Layer Tablet is reliable and simple.
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Objective To Study on anti-thrombosis effect of volatile oil of Acorus Tatarinowii Schott(AST) and ?-asarone.Methods Thrombosis test,blood hyperviscocity test,blood clottingtest,and in vitro fibrinolytic test were carried out to investigate the effects of volatile oil of AST and ?-asarone on the following indexes:weight of thrombus,prothrombin time(PT),activated part prothrombin time(APTT),hemorheology,clotting time,the weight of plasma fibrin clot.Results Volatile oil of AST and ?-asarone can lower the weight of venout thrombosis in rats,and prolong PT and APTT of blood plasma in rats.They can improve hemorheology in the hyperviscocity rats,especially reduce viscosity of whole blood and blood plasma obviously.They can prolong the clotting time in mice obviously;and decrease the weight of plasma fibrin clot.Conclusion Volatile oil of SCP and ?-asarone has anti-thrombosis anticoagulationand fibrinolyitc effect,and its mechanism may be related to the prolongation of PT and APTT,improving blood viscosity.
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Objective: To determine the component of naphtha from Acorus tatarinowii Schott.which can pass through the blood-brain barrier. Methods: Naphtha in rat brain was analyzed by GC-MS after gastric infusion of naphtha. Results: The methylisoeugenol,elemicin, ?-asarone and ?-asarone were detected in rat brain. Conclusion: The resuscitative effect of naphtha is resulted from the comprehensive action of multiple components.
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Objective: To establish the quality control standards of two intermediate products of Xingshen Nasal Drops:musk aromatic water and volatile oil of Acorus tatarinowii Schott so that the content of main components and composition of the different batches of ultimate products remained stable.Methods: The content limit of muskone of musk aromatic water was ascertained by GC-MS. And the characteristic finger print of volatile oil of Acorus tatarinowii Schott was established. Results: The content of muskone of musk aromatic water should be controlled at the range of 0.166～0.202mg/mL. RSD of muskone content of 3 batches of ultimate products was 4.49%, not larger than 10%. The characteristic finger point of volatile oil of Acorus tatarinowii Schott was composed of 6 main component peaks: Methyleugenol, cis-Methylisoeugenol, trans-Methylisoeugenol, Elemicin, ?-Asarone and ?-Asarone. This characteristiz finger print could be repeated when the ultimate product was determined. Conclusion: The establishment of quality control standard of intermediate product can raise the product quality of compound preparations. And GC-MS is one of effective determination methods.