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Abstract Piper sarmentosum is a herbaceous shrub with numerous pharmacological benefits. However, the presence of two toxic phenylpropanoids (α- and β-asarone) limits the medicinal usage of the plant. In this study, the extraction of three asarone isomers, namely α-, β-, and -asarone was optimised using supercritical carbon dioxide extraction (SC-CO2) combined with Box-Behnken experimental design. Comparison of asarone contents in different conventional solvent extracts of P. sarmentosum leaves prior to and after SC-CO2 extraction was performed. The SC-CO2 method successfully maximised the extraction of α-, β-, and ɣ-asarone at P = 81.16 bar, T = 50.11°C, and t = 80.90 min, yielding 13.91% α-asarone, 3.43% β-asarone, and 14.95% ɣ-asarone. The SC-CO2 residue of the leaves re-extracted with conventional solvents showed a significant decrease of asarone ranging from 45% to 100% (p<0.001) compared to their counterparts without SC-CO2 treatment. α-, β-, and ɣ-asarone were completely removed in the ethanol extract of the residue. These findings suggested that the optimised SC-CO2 extraction parameters may serve as a quick treatment step for the selective removal of asarone from P. sarmentosum to develop safer extracts for the food and nutraceutical industries applications.
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Epilepsy is a recurrent neurological disease with synchronous abnormal high discharge of neurons in the brain. The pathogenesis of this disease is extremely complex， which is closely related to neurotransmitter regulation， oxidative stress response， inflammatory factors， neuroglial cell， and abnormal gene expression. Western medicine mainly uses phenobarbital， phenytoin sodium， carbamazepine， and other drugs， but long-term use also produces certain toxic and side effects. Traditional Chinese medicine （TCM） believes that the pathogenesis of epilepsy is related to wind， fire， phlegm， and blood stasis， which leads to dysfunction of viscera， disorder of Qi movement， and finally uncontrolled spirit. In recent years， TCM has achieved certain curative effects on the treatment of epilepsy. As a high-frequency antiepileptic drug， Acori Tatarinowii Rhizoma has the effects of opening orifices and eliminating phlegm， awakening spirit and benefiting intelligence， and removing dampness and opening stomach， which has been widely used in clinic. In this paper， the pathogenesis of epilepsy and the pharmacological mechanism of Acori Tatarinowii Rhizoma extract and chemical components in the treatment of epilepsy were expounded by referring to relevant pharmacological studies and animal experiments. It was found that Acori Tatarinowii Rhizoma played a role in regulating the neurotransmitter level， antioxidant stress response， scavenging oxygen free radicals， regulating the expression of c-fos gene， reducing the level of inflammatory mediators， resisting neuronal apoptosis， and regulating the neuroglial cells and the permeability of blood-brain barrier. This paper summarizes the positive effects of Acori Tatarinowii Rhizoma on the treatment of epilepsy， and provides a scientific basis for the popularization and application of Acori Tatarinowii Rhizoma in the prevention and treatment of epilepsy.
ABSTRACT
Epilepsy is a recurrent neurological disease with synchronous abnormal high discharge of neurons in the brain. The pathogenesis of this disease is extremely complex， which is closely related to neurotransmitter regulation， oxidative stress response， inflammatory factors， neuroglial cell， and abnormal gene expression. Western medicine mainly uses phenobarbital， phenytoin sodium， carbamazepine， and other drugs， but long-term use also produces certain toxic and side effects. Traditional Chinese medicine （TCM） believes that the pathogenesis of epilepsy is related to wind， fire， phlegm， and blood stasis， which leads to dysfunction of viscera， disorder of Qi movement， and finally uncontrolled spirit. In recent years， TCM has achieved certain curative effects on the treatment of epilepsy. As a high-frequency antiepileptic drug， Acori Tatarinowii Rhizoma has the effects of opening orifices and eliminating phlegm， awakening spirit and benefiting intelligence， and removing dampness and opening stomach， which has been widely used in clinic. In this paper， the pathogenesis of epilepsy and the pharmacological mechanism of Acori Tatarinowii Rhizoma extract and chemical components in the treatment of epilepsy were expounded by referring to relevant pharmacological studies and animal experiments. It was found that Acori Tatarinowii Rhizoma played a role in regulating the neurotransmitter level， antioxidant stress response， scavenging oxygen free radicals， regulating the expression of c-fos gene， reducing the level of inflammatory mediators， resisting neuronal apoptosis， and regulating the neuroglial cells and the permeability of blood-brain barrier. This paper summarizes the positive effects of Acori Tatarinowii Rhizoma on the treatment of epilepsy， and provides a scientific basis for the popularization and application of Acori Tatarinowii Rhizoma in the prevention and treatment of epilepsy.
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Aim To evaluate the protective effect of α-asarone on microglials with cerebral ischemia/reperfusion injury by measuring the expression of polar transformation and related inflammatory proteins in BV2 cells in vitro and its mechanisms.Methods The cerebral ischemia/reperfusion injury BV2 cells were pretreated by α-asarone in vitro and simulated by OGD/R model.The effect of α-asarone on the viability of damaged cells in OGD/R model was determined by CCK-8; the morphological changes of cells were observed to analyze the general morphology of cells; the levels of proinflammatory factor IL-1β, IL-18 and anti-inflammatory factor IL-10, IL-4, and ROS activity secreted by BV2 cells were detected by ELISA; the protein expressions of TGF-β, TNF-α and inflammatory related protein NLRP3, caspase 1, p-NF-κB were detected by Western blot.Results The results of in vitro experiments were as follows: the activity of damaged cells in OGD/R model was significantly increased by α-asarone, with the increase of administration dose, the cells in the low, medium and high dose groups of α-asarone decreased, and the "amoeba-like" cells and the cell body were gradually became stereoscopic and full.From the results of cell morphology, it could be seen that α-asarone had a certain proliferative effect on normal cells; the release was significantly reduced of proinflammatory factor IL-1β, IL-18 and TNF-α in OGD/R injured BV2 cells pretreated with α-asarone, also increased the release of IL-10, IL-4 and TGF-β, with a dose-effect relationship, and the high dose(16 μmol·L-1)was the best; the expressions of inflammatory related protein NLRP3, caspase 1, NF-κB and ROS activity in injured cells of OGD/R model were significantly reduced after pretreatment with α-asarone.Conclusions α-asarone has a significant protective effect on cerebral ischemia/reperfusion injury, mainly by regulating ROS activity and inhibiting phosphorylation of NF-κB, in order to reduce the excessive activation of NLRP3 inflammatory corpuscles reducing the secretion of proinflammatory factor IL-1β and IL-18, promoting the secretion of anti-inflammatory factor IL-10 and IL-4, so as to protect cerebral ischemia/reperfusion injury by anti-inflammatory reaction.
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To investigate effects of α-asarone and β-asarone on induced PC12 cell injury and related mechanisms. Aβ toxic injury cell model was induced by Aβ in PC12 cells. PC12 cells were divided into blank control group, model control group, α-asarone group (0.5, 1.0, β-asarone group (6.3, 12.5, vasoactive intestinal peptide (VIP) group, and VIP antagonist control group. Cell survival rate was detected by CCK-8 kit; cell apoptosis rate was detected by flow cytometry. The levels of inflammatory cytokines interleukin (IL)-1, , tumor necrosis factor (TNF)-α, oxidation-related inducible nitric oxide synthase (iNOS), nitric oxide (NO), apoptosis factors caspase-3 and p53 were detected by ELISA method. The expressions of C-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinase (p38MAPK) were detected by Western blotting. Compared with model control group, cell survival rates of group, β-asarone group and VIP group increased; the cell apoptosis rate decreased; levels of apoptosis-related factors caspase-3, p53, inflammatory factors IL-1, TNF-α decreased; IL-10 level increased; levels of oxidization-related factors iNOS and NO decreased; the expression of JNK and p38MAPK protein decreased (all 0.05). α-asarone and β-asarone have protective effects on PC12 cell injury induced by Aβ. β-asarone may inhibit inflammatory factors and oxidation-related factors through promoting VIP secretion, regulating JNK/MAPK pathway, and reducing PC12 cell apoptosis; however, the effect of α-asarone may be not related to VIP secretion.
Subject(s)
Animals , Rats , Allylbenzene Derivatives , Anisoles/pharmacology , Apoptosis , PC12 CellsABSTRACT
Biotransformation of α-asarone by Alternaria longipes CGMCC 3.2875 yielded two pairs of new neolignans, (+) (7S, 8S, 7'S, 8'R) iso-magnosalicin (1a)/(-) (7R, 8R, 7'R, 8'S) iso-magnosalicin (1b) and (+) (7R, 8R, 7'S, 8'R) magnosalicin (2a)/(-) (7S, 8S, 7'R, 8'S) magnosalicin (2b), and four known metabolites, (±) acoraminol A (3), (±) acoraminol B (4), asaraldehyde (5), and 2, 4, 5-trimethoxybenzoic acid (6). Their structures, including absolute configurations, were determined by extensive analysis of NMR spectra, X-ray crystallography, and quantum chemical ECD calculations. The cytotoxic activity and Aβ
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To investigate the effect of α-asarone on the function and expression of P-glycoprotein(P-gp)in rat brain microvascular endothelial cells(rBMECs). rBMECs were exposed to L-glutamate(100 μmol/L) for 30 mins to induce the overexpression of P-gp/multidrug resistance gene 1a(Mdr1a)on the cell membranes,which mimicked the overexpression of P-gp/Mdr1a in blood brain barrier(BBB) when drug-resistant epilepsy attacked.MTT assay was used to detect the safe range of α-asarone concentration.The model cells were intervened with different concentrations of α-asarone at 12.5,25.0,and 50.0 μg/μl for 24 hours.After the treatment of α-asarone,the expression and the function of P-gp/Mdr1 were measured by Western blotting,real-time PCR,and intracellular rhodamine 123 accumulation assays. The rBMECs,stimulated by glutamine,showed a high expression of P-gp(=1.924,=0.020)/Mdr1a(=1.788,=0.019) compared to the normal rBMECs.The treatment with 25.0(=1.924,=0.025;=1.788,=0.017) and 50.0 μg/μl(=1.924,=0.035;=1.788,=0.026) α-asarone significantly depressed the expression of P-gp/Mdr1a.The treatment with 25.0 and 50.0 μg/μl α-asarone significantly increased intracellular accumulation of Rhodamine 123 by 40% and 60% respectively. α-asarone down-regulates the high expressions of P-gp and Mdr1a mRNA in rBMECs induced by L-glutamate.Moreover and increases intracellular accumulation of rhodamine-123.Thus,α-asarone may reverse drug resistance in P-gp-mediated drug-resistant epilepsy.
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Objective: The experiment was designed to reveal the extraction, distribution and influencing factors of volatile components in the extraction process of volatile oil from Acori Tatarinowii Rhizoma (ATR). Methods: Volatile oil of ATR was extracted by steam distillation and the extract was collected every 30 min to separate the aromatic water and volatile oil. Results: A total of 56 volatile compounds were determined, of which β-asarone, methyleugenol, cis-methylisoeugenol and γ-asarone were the main characteristic constituents. There were 41 kinds of components distributed only in water, four components only in oil and 11 kinds in both oil and water. Correlation analysis showed that the specific components in water were positively correlated with the dissolution/diffusion of the main components in water, but negatively correlated with the main components in volatile oil. The water solubility of the unique components in water was the highest. The results of radar and PCA showed that the water solubility and boiling point of the specific components in water were very high, the vapor pressure of the common components of oil and water was the highest, and the polar surface areas of the special components in oil were high. Conclusion: Affected by the physical and chemical properties of volatile component, some components specifically distributed in water increased the content of main components in the aromatic water, may resulting in volatile oil extraction process easy to "emulsification", in turn, leading to an important reason for the declining quality of volatile oil.
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Kaixin Powder, an ancient Chinese herbal decoction and is composed of Ginseng Radix et Rhizoma, Polygalae Radix, Acori Tatarinowii Rhizoma, and Poria Cocos. Its main active chemical components are ginseng ginsenosides, polygalae saponins, oligosaccharide esters, asarone, poria acid, and pachymaran, which have a variety of pharmacological effects such as anti-depression, anti-dementia, improving learning and memory, and anti-fatigue. This article mainly reviewed the literature related to Kaixin Powder published in domestic and foreign research journals, summarized the research on the pharmacological activity and their mechanisms of Kaixin Powder, and prospected the potential clinical application in the treatment of mental illness.
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To prepare and optimize the self-microemulsion co-loaded with tenuifolin and β-asarone(TF/ASA-SMEDDS) and evaluate its quality. The prescription compositions of TF/ASA-SMEDDS were screened by solubility test, single factor test and pseudo-tern-ary phase diagram, and the prescriptions were further optimized by Box-Behnken response surface method, with the drug loading and particle size as the evaluation indexes. Then the optimized TF/ASA-SMEDDS was evaluated for emulsified appearance, particle size, morphology and drug release in vitro. The optimized prescription for TF/ASA-SMEDDS was as follows: caprylic citrate triglyceride polyoxyethylene castor oil-glycerol(10.8∶39.2∶50), drug loading of(5.563±0.065) mg·g~(-1) for tenuifolin and(5.526±0.022) mg·g~(-1) for β-asarone; uniform and transparent pan-blue nanoemulsion can be formed after emulsification, with particle size of(28.84±0.44) nm. TEM showed that TF/ASA-SMEDDS can form spherical droplets with a uniform particle size after emulsification; In vitro release test results showed that the drug release rate and cumulative release of tenuifolin and β-asarone were significantly improved. The preparation process of TF/ASA-SMEDDS was simple and can effectively improve in vitro release of tenuifolin and β-asarone.
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Anisoles , Biological Availability , Diterpenes, Kaurane , Drug Delivery Systems , Emulsions , Particle Size , Solubility , Surface-Active AgentsABSTRACT
OBJECTIVE：To study the improvement effects of ginsenoside Rb 3 combined with β-asarone on vascular dementia （VD）model mice and its mechanism. METHODS ：ICR mice were randomly divided into model group ，ginsenoside Rb 3 group（10 mg/kg），β-asarone group （10 mg/kg），drug combination group （ginsenoside Rb 3 10 mg/kg+β-asarone 10 mg/kg），positive control group（donepezil hydrochloride 1 mg/kg）and Akt inhibitor group （LY294002，1 mg/kg），and sham operation group was set up ， with 10 mice in each group. Except for sham operation group ，VD model was induced by four vessel occlusion method in other groups. After modeling ，sham operation group and model group were given constant volume of normal saline ，Akt inhibitor group was given relevant medicine intraperitoneally ，and other groups were given relevant medicine intragastrically ，twice a day ，for consecutive 30 d. After last administration ，the learning and memory ability of mice was detected by avoiding darkness test. The contents of 4-hydroxydecenoic acid （4-HNE），8-hydroxydeoxyguanosine （8-OHdG） and reactive oxygen species （ROS） in hippocampus was detected by ELISA. RT-PCR assay was used ， to detect the mRNA expression of Bcl- 2 and Bax inhippocampus. The protein expression of Bcl- 2 in cortex wadetected by immunofluorescence method. Western blotting deng- assay was used to detect the protein expression of Bcl- 2 and mz1@126.com Bax in hippocampus. RESULTS ： Compared with sham operation group ，the incubation period of avoiding darkness xiaoyinlanlp@126.com test in model group was shortened significantly ； and the number of errors was increased significa ntly；4-HNE，8-OHdG and ROS contents ，mRNA and protein expression of Bax were increased significantly ，and mRNA and protein expression of Bcl- 2 was decreased significantly （P＜0.01）. Compared with model group，the incubation period of avoiding darkness test was prolonged significantly in ginsenoside Rb 3 group，β-asarone group ，drug combination group and positive control group ，the number of errors was decreased significantly ；4-HNE，8-OHdG，ROS contents ， mRNA and protein expression of Bax were decreased significantly ，and mRNA and protein expression of Bcl- 2 were increased significantly，especially in drug combination group （P＜0.05 or P＜0.01）. But the incubation period of avoiding darkness test was shortened significantly in Akt inhibitor group ，and the number of errors was increased significantly ；4-HNE，8-OHdG，ROS contents，mRNA and protein expression of Bax were increased significantly ，and mRNA and protein expression of Bcl- 2 were decreased significantly （P＜0.05）. CONCLUSIONS ：Ginsenoside Rb 3 combined with β-asarone has a protective effect on VD model mice ，and the effect was better than that of each compound alone. The mechanism of which may be associated with anti-oxidative stress and anti-apoptosis of hippocampus.
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This study investigated whether α-asarone could promote proliferation and differentiation of neural progenitor cells into the neuronal cell types in in vitro and ex vivo studies. For in vitro assay, neural progenitor cells were isolated from fetal cerebral cortex (E15) and checked cell proliferation rate and neural progenitor cell marker in neurospheres. Treatment of α-asarone, particularly at a concentration of 3 µM, promoted the proliferation of neural progenitor cells and effectively differentiated neural progenitor cells into neurons. For ex vivo assay, a hippocampi slice culture system from 7 day postnatal rat fetuses was used. Although slight tissue damage was observed in the hippocampus after the high concentration (100 µM) of α-asarone, however, α-asarone enhanced the proliferation of neural progenitor cells in dentate gyrus region and also effectively differentiated into neuroblast at concentration of 30 µM. Consequently, α-asarone promotes the proliferation of neural progenitor cells and effectively differentiates neural progenitor cells into neurons. Therefore, our results support the therapeutic benefits of α-asarone for treating neurodegenerative diseases.
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Animals , Rats , Cell Proliferation , Cerebral Cortex , Dentate Gyrus , Fetus , Hippocampus , In Vitro Techniques , Neurodegenerative Diseases , Neurons , Stem CellsABSTRACT
Objective To discuss the effect of α-asarone on the expression level of Cyt-c,Smac,Caspase3 mRNA and protein in human esophageal carcinoma Eca-109 cell mitochondria. Methods The Eca-109 cells were cultured in vitro,and divided into the negative control group and the α-asarone treatment groups(final concentration:25,50,100 μg·mL-1).After 48 h,the morphological changes of Eca-109 cells were observed by fluorescence inversion microscope.The total RNA of cells were extracted by TRIzol method,the expressions of Cyt-c、Smac and Caspase3 were measured by RT-PCR and Western blotting. Results After Eca-109 cells were treated with different concentrations of α-asarone for 48 h,and obvious changes in the morphology were observed,the expressions of Cyt-c,Smac and Caspase3 genes and protein were increased significantly compared to the negative control group( P<0.05). Conclusion α-asarone can induce the human Eca-109 cells apoptosis by regulating expressions of mitochondrial apoptosis pathway correlation genes such as Cyt-c,Smac and Caspase3.
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Objective To observe the efficacy of asarone injection combined with inhalation on the treatment of COPD acute phase.MethodsAccording to chronic obstructive pulmonary disease diagnosis and treatment guidelinesin the diagnostic criteria for chronic obstructive pulmonary disease in acute phase, 81 patients were randomized double-blindly divided into observation group of 40 cases and a control group 41 cases.Administering inhalation nebulizer patients in the control group, asarone injection combined with inhalation treatment in the observation group.Serum levels of interleukin-8 (IL-8), interferon-γ (IFN-γ), tumor necrosis factor (TNF-α) levels before and after treatment, using a blood gas analyzer patients arterial oxygen pressure (PaO2) and arterial carbon dioxide tension (PaCO2) level, measured using a spirometer patients accounted for one second forced expiratory percentage of predicted value (FEV1% pred) and total airway resistance, and a separate determination combination therapy regimen based on the above indicators Comparative efficacy.Results①IL-8, IFN-γ, TNF-α: After treatment, the observation group was significantly lower than the control group (t=11.498;t=10.279;t=11.576), the differences were statistically significant (P<0.05).②blood gas PaO2 and PaCO2: post-treatment observation group than the control group (t=11.021;t =8.868), the differences were statistically significant (P<0.05).③lung function FEV1% pred and total airway resistance: After treatment, the observation group than the control group (t=7.182;t=6.341), the differences were statistically significant (P<0.05).The total effective rate was significantly higher (χ2 =4.742) after ④observation group, the difference was significant (P<0.05).ConclusionAsarone injection combined with inhalation can reduce chronic inflammation in the body in patients with acute obstructive pulmonary disease, the body adjust blood gas, improve lung function, improve the treatment of patients with acute COPD.
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Objective To observe the influence state of asarone injection for the pulmonary surfactant proteins and oxygen supply state of newborns with pneumonia. Methods 72 newborns with pneumonia were selected as the study object, and they were randomly divided into control group (36 cases) and observation group (36 cases), the control group were treated with conventional treatment of pneumonia, the observation group were treated with asarone injection on the treatment method of control group, then the pulmonary surfactant protein indexes, oxygenation function indexes and blood gas analysis of two groups before and after the treatment were respectively detected and compared. Results The pulmonary surfactant protein indexes, oxygenation function indexes and blood gas analysis of two groups before the treatment all had no significant differences, while the pulmonary surfactant protein indexes, oxygenation function indexes and blood gas analysis of observation group at first, second and fifth day after the treatment were all significantly better than those of control group, all P<0.05, there were all significant differences. Conclusion The asarone injection can significantly improve the pulmonary surfactant proteins and oxygen supply of newborns with pneumonia, so its application value in the treatment of newborns with pneumonia is higher.
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This study was aimed to investigate the protective effect and mechanism of β-asarone on the animal model of Alzheimer's disease(AD) which was induced by intracerebroventricular injection of Aβ₁₋₄₂ combined cerebral ischemia. One hundred and five rats were randomly divided into seven groups including sham-operated group, AD model group, β-asarone 10 mg•kg⁻¹ group, β-asarone 20 mg•kg⁻¹ group, β-asarone 30 mg•kg⁻¹ group, donepezil group(0.75 mg•kg⁻¹) and Ginkgo biloba extract group(24 mg•kg⁻¹). Rats' learning and memory abilities, cerebric regional blood flow, pathological changes in hippocampal CA1 region, the expression level of HIF-1α and serum CAT, SOD and MDA level were detected 4 weeks later. The results showed that the application of intracerebroventricular injection of Aβ₁₋₄₂ joint 2-VO could lead to rats' dysfunction of learning and memory, decrease in regional cerebral blood flow. Neurons in CA1 region were arranged in disorder, and amyloid deposition was increased. The number of cerebral cortical cells expressing HIF-1α was increased as well. The level of serum CAT and SOD decreased, while level of serum MDA increased. However these symptoms were improved by 20 mg•kg⁻¹ and 30 mg•kg⁻¹ β-asarone. The results indicated that β-asarone could effectively relieve the symptoms of the AD model induced by intracerebroventricular injection of Aβ₁₋₄₂ combined cerebral ischemia, and the potential mechanism might be that it could attenuate damage of MDA to the body by improving the level of CAT and SOD, meanwhile the level of HIF-1α decreased as the decline of hyperoxide which might attenuate its damage to neuron, so it finally achieved alleviating Alzheimer's disease.
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Objective To understand the current state of research and clinical application of α-asarone injection.Method Literature search was conducted and the pharmacology, toxicology, preparation, clinical application and adverse reactions of α-asarone were reviewed.Results α-asarone injection has strong relieving effects on cough and asthma, but the quality of production is varying, adverse reactions are often reported, and the toxicological effects need to be further investigated.Conclusions α-asarone injection has a certain clinical effect, but the reports of related adverse reactions are gradually increased.Its toxicity remains to be further studied, and the product quality standard system and instructions need also to be further improved.
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Objective To investigate the effect of β-asarone on differential protein expression in brain tissue of APPswe/PS1dE9 double transgenic mice, and to explore its mechanism in treatment of Alzheimer disease (AD). Methods The animals were divided into normal control group (C57BL/6J mice), model group (APPswe/PS1dE9 mice) and β-asarone treatment group (APPswe/PS1dE9 mice), with ten mice in each group. In a period of 90 days, the mice in β-asarone treatment group were administered with β-asarone by intragastric gavage (15 mg/[kg·d]), and the mice in normal control and model groups were administered with equal doses of normal saline. The learning and memory abilities of mice were detected by Morris water maze test. The expression of β-amyloid precursor protein (APP) in brain tissues was detected by immunohistochemistry. Proteomics analysis of brain tissues was performed by isobaric tags for relative and absolute quantification (iTRAQ). The expression of differential protein H2A and H2B was identified by Western blotting. Results Compared with the model group, the escape latency and the first latency time required to find the escaped platform of mice in the β-asarone treatment group were significantly shortened (P<0.05), the across-platform times were significantly increased (P<0.05), the expression of APP was significantly decreased (P<0.05), and the expressions of H2A 1-H, H2B 2-E and H2B 1-F/J/L were significantly decreased (P<0.05). Conclusion β-Asarone plays a therapeutic role by intervening the modification of histone, which might be one of the mechanisms to improve learning and memory abilities injured by the toxicity of β-amyloid peptide.
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Objective: To study the chemical constituents from the branches and leaves of Viburnum sargentii collected at Mountain Tai. Methods: The chemical constituents were isolated and purified by chromatographic methods, including silica gel, ODS, Sephadex LH-20 columns, and RP HPLC. The structures of the isolated compounds were identified by ESI-MS, 1D-NMR, and 2D-NMR data analyses, and compared with the literature data. Results: Thirteen compounds were obtained from the 95% ethanol extract of branches and the leaves of V. sargentii, and determined as α-amyrin (1), uvaol (2), 3α-ursolic acid (3), 11,12-dehydroursolic acid lactone (4), 3-O-acetyloleanolic aldehyde (5), oleanolic acid (6), betulinic acid (7), magnolin (8), (+)-eudesmin (9), (-)-epieudesmin (10), vibsanol (11), 3,4'-dimethoxylvibsanol (12), and α-asarone (13), respectively. Conclusion: Compound 12 (3,4'- dimethoxylvibsanol) is a new natural product, and compounds 1-11 and 13 are isolated from V. sargentii for the first time.
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Objective To observe the effect of β-asarone on the proliferation, cycle, apoptosis and migration of tumor cells A549, PC3, and PC9-R, thus to provide experimental basis for the application of β-asarone to the treatment of cancer. Methods After A549, PC3, and PC9-R were cultured with different concentrations ofβ-asarone for 24 h, 48 h, and 72 h respectively, CCK-8 was used to detect the optical density (D) of cell proliferation, and then the cell proliferation rate was calculated. The flow cytometry was used to measure the cell DNA cycle and cell apoptosis, and Transwell Chambers were used to detect the cell migration. Results After treatment with different concentrations of β-asarone for 24 h, 48 h, and 72 h respectively, the growth of A549, PC3, and PC9-R showed declining trend in concentration- and time-dependent manner. The proportion of A549, PC3, and PC9-R at G0/G1 phase was increased, the proportion of the three kinds of cells at S phase and the proliferation indexes were declined, the apoptotic rate of A549, PC3, and PC9-R was increased, and the migration of A549, PC3, and PC9-R was reduced (P<0.05 or P<0.01 compared with those of the normal control group). Conclusion β-asarone has certain effects on suppressing proliferation, blocking G0/G1 phase developing into S phrase, inhibiting DNA synthesis, promoting the apoptosis, and inhibiting the migration of A549, PC3 and PC9-R.