The impact of^(60)Co-γirradiation on the chemical constituents of Chuanxiong Rhizoma

Background:In order to clarify the inmpat ofγirradiation on the chemical composition of traditional Chinese medicine,this paper carefully choosed Chuanxiong Rhizoma to carry on a demonstration study.Methods:Through a meticulous assessment,a comprehensive comparison was made between the irradiated and unirradiated Chuanxiong Rhizoma samples.The property characteristics were investigated by colorimeter and electronic nose.The changes in chemical structures and contents was analyzed by fourier infrared spectroscopy,high performance liquid chromatography and fingerprinting.In a quest to uncover the presence of any new radiolysis products,cutting-edge techniques like ultra performance liquid chromatography-quadrupole-time of flight-mass spectrometry and gas chromatography-mass spectrometry were employed.Moreover,the difference of antioxidant activity were investigated.Results:The irradiation doses within 12 kGy had no significant effects on the content of the main chemical components,characteristics and in vitro antioxidant activity of Chuanxiong Rhizoma,while changes in some functional groups and degradation of some volatile oil components containing olefins need further study.Conclusion:This study indicates that^(60)Co-γirradiation is a stable method for sterilization of Chuanxiong Rhizoma.It’s also provide a reference for the establishment of irradiation standards for Chuanxiong Rhizoma and other aromatic medicinal plants.

Exploring the mechanism of Saposhnikoviae Radix and Chuanxiong Rhizoma treating Parkinson's disease based on network pharmacology and molecular docking

Backgroud:Parkinson’s disease(PD)is a neurodegenerative disorder with an increasing global prevalence.However,the development of drugs for PD treatment has not kept pace with the continuously growing number of patients.Currently,the search for new effective substances from natural drugs is a major research direction.Two Chinese medicinal materials,Saposhnikoviae Radix(Fangfeng)and Chuanxiong Rhizoma(Chuanxiong),are commonly used in the treatment of PD in China.However,the mechanism of their combination is not clear,and further research is needed.Methods:Data were collected from publicly available databases:TCMSP,UnitProt,GeneCards OMIM,PharmGKB,Therapeutic Target Database and DrugBank.Network pharmacology and molecular docking methods was used to analyze the data to discover the possible pharmacological effects of the two drugs in the treatment of PD.Results:Beta-sitosterol,Mandenol and Wallichilide were the active components of Saposhnikoviae Radix and Chuanxiong Rhizoma(FC),and they stably bonded with PD targets,including PTGS2,CASP3,AKT1 and JUN.The target genes of FC were significantly enriched in PD-associated pathways,including calcium signaling and apoptosis pathways.Moreover,the study revealed that the active components of FC may affect cellular structures,such as membrane rafts,membrane microdomains,membrane regions,and postsynaptic membranes,which,in turn,affect a variety of molecular functions and biological processes.Conclusion:The results of this study indicate the direction for clarifying the pharmacodynamic substances of FC,the extraction method of pharmacodynamic substances,as well as the mechanism and efficacy of pharmacodynamic substances.Importantly,this study provides a strategy for developing new therapeutic drugs for PD.

The mechanism of Chuanxiong Rhizoma on glaucomatous optic nerve injury based on network pharmacology and molecular docking

Based on network pharmacology,this study predicted the potential molecular mechanism and related pathways of the protective effect of traditional Chuanxiong Rhizoma,a traditional Chinese herb,on glaucomatous optic nerve injury,and conducted in vitro experimental verification of the predicted results of network analysis.We analyzed the molecular mechanism of Chuanxiong Rhizoma in the potential treatment of glaucoma by revealing its main active ingredients and predicting its targets,so as to provide reference for subsequent basic research.Network pharmacological research results showed that the potential hub targets and key signaling pathways of Chuanxiong Rhizoma in the treatment of glaucoma were closely related to biological processes such as apoptosis,autophagy,inflammation,oxidative stress and angiogenesis.Molecular docking showed that many active ingredients,such as chrysophanol(CHR),myricanone and retinol,could combine well with their target proteins by intermolecular forces,especially CHR had strong binding ability with each target.We speculated that the main active component of Chuanxiong Rhizoma might be involved in the regulation of PI3K-Akt,Nod-like receptor,IL-4 and IL-13,MAPK,AGE-RAGE and neurotrophin signaling pathway by regulating of PI3K,Akt,TLR4,RAGE,NTRK2 and other key targets.Furthermore,it may achieve multi-directional intervention on apoptosis/autophagy,inflammation/immunity,oxidative stress and nutrient metabolism of axoplasma flow,and then delay the degeneration of optic nerve injury.In vitro experiments showed that the active component CHR of Chuanxiong Rhizoma could reverse the M1-type polarization and autophagy/apoptosis of mouse microglia(BV2)induced by lipopolysaccharide(LPS)at the transcriptional level.Meanwhile,the expression of inflammatory mediators IL-1βand TNF-αwas inhibited,and the mRNA level of anti-inflammatory factor IL-10 was significantly increased.In addition,CHR down-regulates activation of the RAGE-NOX4 pathway mediated by LPS in reducing oxidative stress.In this study,network pharmacology and molecular docking technology were integrated for the first time to explore the potential molecular mechanism of traditional Chinese herb“Chuanxiong Rhizoma”in the treatment on glaucoma,and CHR was innovatively proposed as an important ingredient in Chuanxiong Rhizoma that plays a protective role in the damage of optic nerve.Preliminary verification was conducted through in vitro experiments.The results suggest that Chuanxiong Rhizoma may interfere with autophagy and apoptosis,inhibit immune inflammation,as well as reduce oxidative stress in the treatment of glaucoma through the active components represented by CHR,so as to resist progressive optic nerve injury.Our study provides theoretical basis for the clinical use of Chinese herbal medicine or its extract in glaucoma,and also lays a solid foundation for the research of Chinese medicine in the field of optic nerve protection.

Optimization of Extraction Process of Fagopyri Dibotryis Rhizoma by Orthogonal Experiment

[Objectives]To optimize the water extraction process of Fagopyri Dibotryis Rhizoma.[Methods]The entropy weight method was used to determine the weight of epicatechin extraction rate and dry extract rate and calculate the comprehensive score.The water extraction process of Fagopyri Dibotryis Rhizoma was optimized by orthogonal design with the comprehensive score as the indicator and the amount of water,extraction time and extraction times as the factors.[Results]The optimum extraction process of Fagopyri Dibotryis Rhizoma was as follows:adding 10 times of water,extracting 3 times,and extracting for 60 min each time.[Conclusions]The optimized extraction process is stable and feasible,and can be used for the extraction of Fagopyri Dibotryis Rhizoma.

Fingerprint Study of Polygonati Rhizoma with Steaming and Exposing to the Sun Alternatively for Different Times

[Objectives]To explore the influence of different times of steaming and exposing to the sun on the fingerprint of Polygonati Rhizoma by studying the HPLC fingerprint of Polygonati Rhizoma processed products with different times of steaming and exposing to the sun,and to provide a basis for the determination of the best processing technology of Polygonati Rhizoma.[Methods]SETSAIL II AQ-C 18(5μm×250 mm×4.6 mm)was used as the column,the column temperature was 30℃,pure water(A)and acetonitrile(B)were eluted gradually,0-10 min,B(5%-10%),10-30 min,B(10%-35%),30-40 min,B(35%-60%),40-45 min,B(60%-100%),flow rate 1 mL/min,absorption wavelength 200 nm.[Results]The relative retained peak area RSDs of the common peaks in the precision,reproducibility and stability tests were all less than 5%.There were 17 common peaks in the fingerprint of nine batches of samples,and the retention time of Peak 2 was basically the same as that of the reference peak of 5-HMF.Peak 4 mainly existed in the chromatogram of Sample 3 to Sample 5,peaks 5 and 11 mainly existed after Sample 3,peaks 9,14 and 16 mainly existed after Sample 6,and peaks 12 and 17 mainly existed after Sample 4.[Conclusions]A total of 17 common peaks were obtained,and the Peak 2 was the designated peak,and the chemical components of each processed product were different.

Mechanism of Polygoni Cuspidati Rhizoma in treating atherosclerosis based on network pharmacology and molecular docking

Background:The incidence and prevalence of atherosclerosis(AS)is increasing every year and has becoming a major health issue of global concern.Polygoni Cuspidati Rhizoma(PCR)is a Chinese herb that is widely used clinically for the treating of AS.However,its pertinent targets and probable mechanisms,still need to be completely explored.Methods:Active compounds and targets for PCR and AS targets were screened using public databases.A“drug-component-disease target”network map was created and analyzed after using the Venn online tool to identify common targets and Cytoscape software to screen drug-disease core targets.Critical targets pathway enrichment analyses are conducted using the Metascape database.Using AutoDock Vina and Pymol software,docking validation and visualization of active components and core targets were carried out.Results:PCR was obtained for ten compounds with 105 AS-related targets.Rhein,quercetin,beta-sitosterol,and luteolin may be drug candidates,and the genes for AKT1,TNF,IL-6,EGFR,TP53,IL-1,RELA,and VEGFA are potential therapeutic targets,according to network analysis.PCR might modulate the AGE/RAGE,PI3K/Akt,IL-17 and NF-ᴋB signaling pathways against the development of AS.Molecular docking indicated that quercetin has high affinity for AKT1 and TNF gene targets.Conclusion:This study provides rare information and scientific basis for further exploration of PC in the treatment of AS.

Exploring the mechanism of active ingredients of Smilacis Glabrae Rhizoma in treating migraine headache through network pharmacology and animal experiments

Background:To explore the potential mechanism of action of the active ingredients of Smilacis Glabrae Rhizoma(SGR)in the treatment of migraine using network pharmacology and in vivo experiments.Methods:Through the search of Traditional Chinese Medicines Systems Pharmacology Database and Analysis Platform,Genecards,Drugbank and other databases,we obtained active ingredients,targets of SGR and related disease targets of migraine,and took the intersection for protein-protein interactions analysis.After constructing the network diagram,network topology analysis was performed to derive the core targets and key active ingredients,and Gene Ontology enrichment and Kyoto Encyclopedia of Genes and Genomes enrichment analyses were performed.Finally,molecular docking was performed and validated by in vivo experiments.In vivo experiments,18 male BALB/c mice were selected,and the SGR group was fed with SGR drinking tablet concentrate,and nitroglycerin injection was used to construct a mouse model of migraine.Enzyme-linked immunosorbent assay test was used to detect the levels of TNF-α,IL-1β,IL-6,and AKT1 in plasma.Results:The results showed that the core targets of SGR for the treatment of migraine were TNF-α,IL-1β,IL-6,and AKT1.These core targets and key active ingredients had better binding ability.Compared with the blank group,the number of head scratching in the model group increased.Compared with the model group,there was a significant reduction of the number of head scratching in the SGR group.In comparison with the blank group,the protein level in the plasma in the model group was markedly higher.Compared with the model group,the protein level in the SGR group was significantly lower.Conclusion:SGR has the characteristics of improving migraine based on multi-targets,multi-components and multi-pathways,and the mechanism of action may be related to the inhibition of the release of inflammatory factors,neuron protection,and interference with apoptosis and other processes.

Study on Rhizoma Chuanxiong based on capillary electrophoresis with amperometric detection

A high-performance capillary electrophoresis with amperometric detection(CE-AD) method has been developed for the analysis of seven bioactive ingredients,namely ferulic acid(FA),vanillin,vanillic acid,p-hydroxybenzoic acid,caffeic acid,gallic acid and protocatechuic acid,in Rhizoma Chuanxiong.The effects of several factors such as the acidity and concentration of running buffer,the separation voltage,the applied potential to working electrode and the injection time were investigated.Under the optimum condit...

Study on pharmacological effect of Chuanxiong Rhizoma on vascular neuropathic headache

Chuanxiong Rhizoma is the dry rhizome of Ligusticum chuanxiong in the umbelliferae family.Chuanxiong Rhizoma pungent,warm,go to liver,gallbladder and pericardium.Effective in promoting blood circulation,promoting Qi,dispelling wind and relieving pain,it could treat chest pain,tingling pain in chest and flank,lump,irregular menstruation,amenorrhea,symptomatic abdominal pain,headache and rheumatic pain.Neurovascular headache is a primary disease caused by dysregulation of intracranial vascular movement and nerve function.It has the characteristics of long course,intermittent recurrent attacks,lingering and difficult to heal.Attacks are often accompanied by many plant nervous system symptoms,such as rapid breathing,accelerated heart rate,vomiting,and gastrointestinal dysfunction.Vascular nerve headache is a common clinical disease,frequently bidity.Studies have shown that Chuanxiong Rhizoma has good pharmacological effects in the treatment of vascular neuropathic headache.①The action of Qi and blood circulation:vascular and neurovascular headache is caused by the evil of external wind and cold and damp heat,which leads to the disconnection of the veins,the disorder of Qi and blood,the obstruction of Qi and blood channels,the loss of brain collateral,and finally causes migraine.Modern Chinese medicine points out that"wind,blood stasis,deficiency,phlegm"are the key factors of the disease.Chuanxiong Rhizoma is the medicine of Qi in the blood.It is pungent and warm.It is good at activating blood and promoting Qi,dispelling wind,relieving pain and dispelling cold,so as to achieve the effect of treating vascular headaches.②Improve brain circulation:angioneurotic headache is caused by dysfunction of the central nervous system related to the regulation of vascular movement,which causes vasospasm or extreme vasodilation,and the decrease of intracranial blood flow causes cerebral ischemia and hypoxia.Sodium ferulate is a chemical component in Chuanxiong Rhizoma.It has a relatively good inhibitory effect on platelet aggregation and the release of 5-HT from platelets.It can ensure the normal contraction of intracranial and extracranial blood vessels,improve the patient′s brain circulation and nerve function,so as to achieve the effect of treating angioneurotic headaches.③Sedative and analgesic effect:the volatile oil and water decoction of Chuanxiong Rhizoma have sedative and analgesic effects,and the water decoction can counteract the excitatory effect of caffeine.Studies have shown that the ATP activation current of rat dorsal root ganglion neurons can be inhibited by ligustrazine in a non-competitive way,which also indicates that Chuanxiong Rhizoma has a good analgesic effect.In this study,the effects of Chuanxiong Rhizoma on angoneeurotic headache were reviewed,and the pharmacological effects of Chuanxiong Rhizoma were further elucidated,providing basis for clinical application and new drug development of Chuanxiong Rhizoma in the treatment of angoneeurotic headache.

Mechanism of volatile oil from Chuanxiong(Chuanxiong Rhizoma)-Suhexiang(Styrax)-Bingpian(Borneolum)in treating angina pectoris based on network pharmacology and its protective effects on myocardial damage in rats

Objective To explore the pharmacodynamic material basis and mechanism of action of volatile oil from Chuanxiong(Chuanxiong Rhizoma)-Suhexiang(Styrax)-Bingpian(Borneolum)(hereinafter referred to as C-S-B volatile oil)in treating angina pectoris based on network pharmacology and to detect its protective effects against rat myocardial damage.Methods Gas chromatography-mass spectrometry(GC-MS)was used to determine the constituents of volatile oils from Chuanxiong(Chuanxiong Rhizoma),Suhexiang(Styrax),and Bingpian(Borneolum),and the targets of the three main constituents were found predicted and screened using the PharmMapper server,and Gene Cards and Coo LGe N databases.The STRING database and Cytoscape software were used to draw the protein-protein interaction(PPI)network,RStudio software was used to analyze Gene Ontology(GO)and Kyoto Encyclopedia of Genome and Genome(KEGG)pathways,and Cytoscape software was used to construct the component-target-pathwaydisease network.The rat model of myocardial injury was established by intraperitoneal injection of a large dose of isoprenaline hydrochloride.After continuous intervention with C-S-B volatile oil for 14 d,the ejection fraction(EF)and short axis shortening rate(FS)of the left ventricle were detected.The indices of myocardial damage were detected after hematoxylin-eosin(HE)staining.Results Fifteen volatile oil components from the C-S-B formula were identified.There are 470 targets of these volatile oil components and 401 angina-related genes.There are 28 core targets,including CHRM4,ADRA1 A,FGFR1,CHRM2,CYP2 A6,CHRM5,CHRM1,CHRM3,HDAC2,and MPO,etc..The results of the KEGG analysis indicated that the C-S-B formula probably interferes with the following pathways:neuroactive ligand-receptor interactions,calcium signaling,cytochrome P450 metabolism of heteropoietin,among others.The results of animal experiments showed that the C-S-B formula essential oil could significantly improve the following myocardial indices in rats with myocardial injury:EF,FS,left ventricular end-systolic diameter(LVIDs),left ventricular end-diastolic diameter(LVIDd),and stroke volume(SV),and all the differences were statistically significant(P<0.01).Conclusion The mechanism of action of volatile oil components in the C-S-B formula in treating angina pectoris was analyzed using multi-component,multi-target and multi-pathway systems,which has laid a foundation for further revealing its mechanism of action.Animal experiments have shown that the volatile oil of the C-S-B formula can improve EF,FS,and other indices of myocardial damage in a rat model,thus relieving myocardial damage caused by heart hyperactivity,improving cardiac function,and protecting against myocardial damage.

Rhizoma Chuanxiong regulates vascular endothelial growth factor production in hypoxic human umbilical vein endothelial cells in vitro and in peri-infarct rat brain tissue

BACKGROUND： Vascular endothelial growth factor （VEGF） acts as ＂molecular bridge＂ following ischemic stroke to improve and restore blood supply and reduce infarction volume. Clinical studies have demonstrated the efficacy of Rhizoma Chuanxiong （Chuanxiong） in the treatment of ischemic cerebrovascular diseases. However, whether it promotes endogenous VEGF expression in ischemic stroke remains unknown. OBJECTIVE： To investigate the influence of Rhizoma Chuanxiong on VEGF production in vitro cultured human umbilical vein endothelial cells and on VEGF expression in ischemic cerebral tissues to explore its role in angiogenesis. DESIGN, TIME AND SETTING： In vitro basic comparison of traditional Chinese drug-containing serum pharmacology; in vivo randomized, controlled, animal experiment. This study was performed at the Medical Laboratory of West China Hospital, Sichuan University between December 2002 and April 2004. MATERIALS： Two Chinese rabbits were selected. One was intragastrically perfused with 5.8 g/kg Rhizoma Chuanxiong extract twice per day for three consecutive days to prepare Rhizoma Chuanxiong extract-containing serum. The remaining rabbit was intragastrically perfused with the same volume of normal saline twice per day for three consecutive days. Rhizoma Chuanxiong extract was provided by Beijing Traditional Chinese Medicine Research Institute, predominantly composed of ligustrazine, ligustilide, and ferulic acid. ChemiKineTM human VEGF Kit was purchased from Chemicon, USA; mouse anti-VEGF monoclonal antibody and biotin-goat anti-mouse IgG were purchased from Santa Cruz Biotechnology. Inc., USA. METHODS： （1） In vitro experiment： in vitro cultured human umbilical vein endothelial cells were separately incubated in rabbit serum with 10% Rhizoma Chuanxiong extract, normal medium without rabbit serum, and rabbit serum without Rhizoma Chuanxiong extract （blank control）. In addition, cells from the three groups were incubated under normoxia （5% CO2, 95% air） and hypoxia （1% 02, 5% CO2, 94% N2）, respectively, for 24 hours. （2） In vivo experiment： a total of 4/44 Sprague Dawley rats were selected for the sham-operated group （no occlusion）, and the remaining rats were used to establish a cerebral ischemiaJreperfusion model by suture occlusion. 32 animals with ischemia/reperfusion injury were randomly divided into treatment and model groups, with 16 rats in each group. Both groups were intraperitoneally infused with 0.58 g/kg Rhizoma Chuanxiong extract and normal saline two hours following reperfusion. The sham-operated group was administrated normal saline. Animals were treated with saline or Chuanxiong extracts （0.58 g/kg） twice per day for three consecutive days. MAIN OUTCOME MEASURES： In vitro experiment： VEGF concentration was detected in each group by enzyme-linked immunosorbent assay. In vivo experiment： behavioral alterations of rats were evaluated by neurological function scale; infarct volume was assessed by hematoxylin-eosin staining; VEGF protein expression in the infarct regions was determined by immunohistochemistry. RESULTS： （1） VEGF levels were similar between the three groups under normexic condition （P 〉 0.05）; while hypoxia induced VEGF production （P 〈 0.01 ）. VEGF levels in the drug-containing serum group were particularly higher compared with the other groups （P 〈 0.01）. （2） Compared with normal saline treatment, Rhizoma Chuanxiong extract significantly improved the neurological scale and reduced cerebral infarct volumes （P〈 0.05）. The percent of VEGF-positive cells was significantly greater than the model group （P 〈 0.05）. The sham-operated group exhibited normal neurological function, with no infarct focus. CONCLUSION： Rhizoma Chuanxiong extract-containing rabbit serum effectively promoted cultured VEGF production under hypoxia. Rhizoma Chuanxiong extract upregulated VEGF expression in the infarct region, improved neurological function, and reduced infarct size.

Network pharmacology research of Chuanxiong Rhizoma-Acori Tatarinowii Rhizoma in the treatment of vascular dementia

Objective:Using network pharmacology to explore the target and mechanism of Chuanxiong Rhizoma and Acori Tatarinowii Rhizoma in the treatment of vascular dementia(VaD),so as to provide a reference for treating VaD through them.Methods:Traditional Chinese medicine systems pharmacology database and analysis platform were used to screen the main active ingredients and targets of Chuanxiong Rhizoma and Acori Tatarinowii Rhizoma.By means of Gene Cards and Online Mendelian Inheritance in Man(OMIM),targets of VaD were collected.The intersecting targets were obtained by using the Venn map.The String online database was used to build a protein-protein interactions Network and the Metascape database was used to perform GO function enrichment analysis and KEGG pathway enrichment analysis.A“drug-ingredient-target-pathway”network was constructed by Cytoscape software.Autodock vina software was used to conduct molecular docking between targets.Results:A total of 7 active ingredients in Chuanxiong Rhizoma and 4 active ingredients in Acori Tatarinowii Rhizoma were screened.There were 42 active targets of Chuanxiong Rhizoma and 70 active targets of Acori Tatarinowii Rhizoma and 1152 disease targets.After deleting the repeat value,51 drugs targets were obtained.After the intersection,with a total of 25 targets.According to GO and KEGG enrichment analysis,the main biological processes involved include cellular response to lipid,negative regulation of apoptotic signaling pathway,blood circulation,response to a steroid hormone,etc.The main pathways include pathways in cancer,PI3K-Akt signaling pathway,and AGE-RAGE signaling pathway in diabetic complications,etc.Molecular docking showed that the most active docking combinations were AKT1 and Perlolyrine,RELA and FA,MAPK14 and FA,respectively.Conclusion:Chuanxiong Rhizoma and Acori Tatarinowii Rhizoma play an important role in the treatment of VaD mainly by anti-inflammatory and anti-apoptosis.

Experimental Study of Emilia Sonchifolia Combined with Coptidis Rhizoma for the Prevention and Treatment of Oral Ulcer

Objective: This paper aims to investigate the therapeutic effect of the combination of Emilia Sonchifolia and Coptidis Rhizoma on oral ulcer rats. Methods: 36 SD rats of half male and half female were kept for 7 days, and 6 rats among them were selected as normal group by random sampling method, and the rest rats were randomly divided into model group, positive control group, Emilia Sonchifolia group, Coptidis Rhizoma group and combined group after the establishment of oral ulcer model. The normal group and model group were given blank film, the positive control group was given Guilin Watermelon Frost, and the Emilia Sonchifolia group, Coptidis Rhizoma group and combined group were given the corresponding oral film, which was administered to the ulcer for 7 days continuously, 2 times per day. The healing of oral ulcer was assessed at the end of the last day of administration, and the ulcer area was calculated on the 1st, 3rd, 5th and 7th days after successful modeling, and the serum levels of IL-2 and TNF-α in rats were detected by Emilia Sonchifolia. Results: The grading of ulcer healing in the positive control group and the combined group was better than the other groups, and the difference was statistically significant when compared with the model group (p Coptidis Rhizoma group, Emilia Sonchifolia group, combined group and positive control group was smaller than that in the model group, and the difference was statistically significant (p Emilia Sonchifolia group, Coptidis Rhizoma group and combined group were all effective in reducing the area of oral ulcer, among which the combined group was more effective. The level of pro-inflammatory factor TNF-α was reduced and the level of anti-inflammatory factor IL-2 was increased in the Emilia Sonchifolia group, Coptidis Rhizoma group and combined group, and the difference was statistically significant (p Conclusion: The combination of Coptidis Rhizoma and Emilia Sonchifolia is effective in the treatment of oral ulcer in rats, and the effect of the combination is better than that of the drug alone.

生姜、干姜、炮姜的性效考证及其化学成分、药理活性的研究进展

生姜为姜科植物姜的新鲜根茎,属于药食两用品,作为中药首次收载于《神农本草经》,而汉·张仲景《金匮要略》最早记载了生姜在中医临床中的应用。干姜、炮姜分别是生姜经干燥加工和砂烫后的炮制品,三者在临床上被广泛使用,但在药物属性和作用特点上却有所不同。基于不同历史时期的不同医家对三者的性效和应用的记载并不完全一致,该文从古籍本草考证、现代化学成分和药理作用等方面对生姜、干姜、炮姜(三姜)进行了总结,以系统地综述三姜的性效源流及现代研究进展,明确其临床应用范畴,为三姜性效的深入研究提供参考,亦为中医临床合理用药提供个性化参考。

Rhizoma paridis saponins protected against liver injury in diethylnitrosamine-induced mice

Background:Diethylnitrosamine,one of food additives,possessed a strong carcinogenic effect in human.Rhizoma paridis saponins,as the main active components of Paris polyphylla,have a good anti-cancer effect in our previous research.To verify their inhibitory effect on diethylnitrosamine-induced liver cancer,we carried out this study.Methods:We established diethylnitrosamine-induced mouse hepatocarcinoma models to evaluate antitumor of Rhizoma paridis saponins.Subsequently,gas chromatography-mass spectrometry was applied to analyze the metabolites in the urine and serum samples.Results:Rhizoma paridis saponins alleviated diethylnitrosamine-induced hepatocarcinogenesis.On the one hand,Rhizoma paridis saponins down-regulated the levels of liver function markers,such as alanine aminotransferase,aspartate transaminase and alpha fetoprotein.On the other hand,Rhizoma paridis saponins reduced metabolic disorders by increasing fructose and mannose metabolism,and decreasing pentose and glucuronate interconversion,inositol phosphate metabolism,and the process of saturated fatty acids transforming to unsaturated fatty acids,which based on the regulating mRNA expression of glucose transporter type 4,lactate dehydrogenase A,fatty acid synthetas,acetyl-CoA carboxylase and apolipoprotein A-I.Conclusion:Rhizoma paridis saponins has the potential application to inhibit chemical-induced hepatocarcinogenesis in the future.

基于GEO数据库联合网络药理学研究川芎-赤芍药对治疗动脉粥样硬化的药理过程及分子机制

目的:探讨活血化瘀中药药对川芎-赤芍拮抗动脉粥样硬化的潜在分子机制及药理过程。方法:使用R语言Limma包分析GEO数据库GSE43292数据集,对有表达差异的动脉粥样硬化基因进行筛选和提取。川芎-赤芍药对所含的化学活性组分及靶点通过中药系统药理学数据库与分析平台检索。合并差异基因和药物作用靶点以获得共同的靶点。利用在线分析工具STRING和Cytoscape构建药物和靶点的调控网络以及靶点间的蛋白质-蛋白质相互作用(PPI)网络。然后利用R语言注释靶点基因的基因本体(GO)功能,分析京都基因与基因组百科全书(KEGG)通路,再进行基因集富集分析(GSEA)以验证KEGG的通路和富集的情况,确定靶点基因的调控功能和参与基因调控功能的信号转导通道。结果:共筛选出动脉粥样硬化差异基因1244个,川芎-赤芍药对含36个生物活性成分,其中靶点为环加氧酶1、肾上腺素受体、过氧化物酶体增殖物激活受体-γ、激酶插入域受体、孕激素受体、基质金属蛋白酶9、CXC趋化因子配体8、蛋白激酶Cβ、白细胞介素6、CD14、二肽基肽酶-4、PIK3CG、肾上腺素受体α1B、微管相关蛋白2、尿激酶纤溶酶原激活剂和单胺氧化酶B。靶点在GO中主要富集在合成DNA过程的调控、DNA生物合成的过程、含胶原的细胞外基质、细胞外基质、蛋白酶结合、细胞迁移、血管形成过程、膜筏结构、转录的调节等与动脉粥样硬化炎症、脂肪代谢及血管生成相关的生物学注释。脂质与动脉粥样硬化通路和核因子κB信号通路与动脉粥样硬化关系最为密切,并且在KEGG信号通路和GSEA均显示出富集。结论:川芎-赤芍药对通过潜在的13个活性成分作用于可能的16个靶点调控相关信号转导通路,通过抗炎、调脂和保护血管等方式产生抗动脉粥样硬化的作用。

川芎挥发油治疗心绞痛的网络药理学研究及实验验证

目的 基于网络药理学研究川芎挥发油抗心绞痛的作用机制,并用动物实验加以验证。方法 通过水蒸气蒸馏法、气相色谱-质谱联用仪(gas chromatography-mass spectrometry, GC-MS)、口服利用度(oral bioavailability, OB)筛出挥发油成分;使用Pubchem、SwissTarget、DisGeNET、DrugBank数据库和R语言分别获取挥发油成分的靶点、心绞痛的靶点和交集靶点;蛋白质-蛋白质相互作用通过String数据库完成;使用R语言的ClusterProfiler包对交集靶点进行基因本体分析(gene ontology, GO)和京都基因与基因组百科全书分析(Kyoto Encyclopedia of Genes and Genomes, KEGG)富集分析,并通过Cytoscape构建中药-成分-靶点-通路网络;借助AutoDock vina 1.2.3、Pymol 3.0、Discovery Studio 2016软件进行分子对接,分析关键靶点和主要挥发油成分的亲和力。最后,通过动物实验进一步验证川芎挥发油对心绞痛的治疗效果。结果 网络药理学研究共得到10个挥发油成分和22个关键靶点,这些靶点与神经递质、突触膜上的受体、物质代谢等生物过程以及神经活性配体-受体相互作用、视黄醇代谢、药物代谢-细胞色素P450等通路密切相关;分子对接结果表明3-butylidenephthalide、Alpha-selinene、Trans-ligustilide等挥发油成分与多个关键靶点结合发挥治疗作用。动物实验表明川芎挥发油通过调节射血分数(ejection fraction, EF)、短轴缩短率(fractional shortening, FS)、左室收缩末内径(left ventricular internal diameter in systole, LVIDs)和每搏输出量(stroke volume, SV)水平以及乳酸脱氢酶(lactate dehydrogenase, LDH)、肌酸激酶(creatine kinase, CK)、天冬氨酸转氨酶(aspartate aminotransferase, AST)活性,促进受损心肌细胞中ADRA1A、CHRM5蛋白的表达,改善心肌纤维状态,减小细胞间隙,减少炎性细胞浸润表现出保护心肌的作用。结论 川芎挥发油具有有效保护受损心肌组织,治疗心绞痛的作用。

Advances in Application of Bistortae Rhizoma in Mongolian Medicine and Traditional Chinese Medicine

Mongolian medicine and traditional Chinese medicine have different interpretations of Bistortae Rhizoma,including its name,nature and taste,function and efficacy.This paper sorted out the related application of Chinese and Mongolian medicine from the records of Materia Medica.The chemical components and pharmacological effects of Bistortae Rhizoma were summarized to provide a reference for the clinical application of Bistortae Rhizoma in traditional Chinese medicine and Mongolian medicine,and for the better development and utilization of national medicines.

Integrated network pharmacology analysis and in vitro cell experiments to reveal the mechanisms of Ligusticum chuanxiong Hort.in the treatment of non-alcoholic fatty liver disease

Background:Non-alcoholic fatty liver disease(NAFLD)is a liver disease of unknown etiology.A traditional Chinese medicine Ligusticum chuanxiong Hort.(CX),it has been used about 2,000 years.Until now,the mechanism of action of CX on NAFLD remains unclear.Method:We first tested the toxicity of CX to AML12 cells with CCK-8.In vitro cell models of NAFLD were made using free fatty acid,and used Oil Red O staining tested lipid droplets.Then the active compounds of CX were collected from TCMSP and literatures,and SwissTargetPrediction,Search Tool for Interacting Chemicals,Encyclopedia of Traditional Chinese Medicin,Bioinformatics Analysis Tool for Molecular mechANism of Traditional Chinese Medicine database were used to predict the targets of the compounds.DRUGBANK,Online Mendelian Inheritance in Man,Therapeutic Target Database,DisGeNET and GeneCards database were used to predict the targets of NAFLD.Use Venn diagram to obtained the intersection targets by,and analyzed the protein-protein intersection network.Use Kyoto Encyclopedia of Genes and Genomes and Gene Ontology to forecast the function of intersection genes.Molecular docking was used to evaluate the interaction between hub gene and active ingredients.Finally,use western blotting to determine the effects of CX on PPARA,PPARG,IL1B and TNF proteins.Result:CX can reduce the production of AML12 cell lipid droplets.A total of 15 chemical components were identified from CX.Folic acid,chrysophanol and sitosterol were the main components of CX against NAFLD.ALB,TNF,PPARG and PPARA proteins were the main targets of CX in the treatment of NAFLD.PPAR signaling pathway and fatty acid degradation were closely related to anti-NAFLD.Molecular docking results shows that folic acid was the main active ingredient of CX for NAFLD treatment,and TNF is the main potential target.The cellular NAFLD model showed that CX up-regulated the expression of PPARA and PPARG protein and down-regulated inflammatory factor IL-1B and TNF expression.Conclusion:Our study suggests that CX has a therapeutic effect on NAFLDA,which may be related to the PPAR pathway and the reduction of inflammatory cytokines.

外源Cd对川芎苓种萌发及幼苗生长的影响

本研究旨在探究不同浓度镉(Cd)对川芎苓种萌发和幼苗生长的影响。采用以石英砂为基质的水培试验,施加不同浓度CdCl 2·2.5 H 2O(0、0.1、0.25、0.5、1、2 mmol/L)溶液处理川芎苓种,研究Cd胁迫对川芎苓种萌发、幼苗生长、生理代谢及Cd含量的影响。结果显示,随着Cd浓度的增加,株高抑制率、根长抑制率上升;根、叶及节盘Cd含量显著升高;株高、根长、叶鲜重、根鲜重下降;抗氧化酶(过氧化氢酶、过氧化物酶、超氧化物歧化酶)活性、非酶系统物质(可溶性蛋白、谷胱甘肽、脯氨酸)含量以及丙二醛含量先升高后降低。研究表明,0.1~2.0 mmol/L Cd对川芎苓种萌发和早期幼苗生长均有明显的毒害作用,随着Cd胁迫浓度的升高毒害作用增强,其中川芎幼苗根对Cd胁迫最敏感。Cd胁迫下川芎幼苗生理生化指标整体上呈现低促高抑的Hormesis效应。川芎幼苗通过提高抗氧化酶活性和非酶系统物质积累,减少膜系统损伤、活性氧蓄积,缓解Cd毒害作用,提高耐受性。