Background:In a previous study,we found that Atractylodes macrocephala and Paeoniae radix(AM-PR)was useful for the alleviation of functional constipation(FC).However,the precise mechanism underlying the compatibility ...Background:In a previous study,we found that Atractylodes macrocephala and Paeoniae radix(AM-PR)was useful for the alleviation of functional constipation(FC).However,the precise mechanism underlying the compatibility between AM and PR in the treatment of FC remains uncertain.This study aims to analyze the pharmacokinetic differences in the active ingredients in the blood of rat models with FC when applied individually and in combination with AM-PR.It also seeks to compare the changes in the content of the active ingredient when applied individually and in combination with in vitro AM-PR,further in-depth investigation into its material foundation in terms of pharmacokinetics,as well as the composition of the substance.Methods:Blood microdialysis samples were collected using microdialysis technology.These samples from rats with FC were compared after administration of AM,PR,and AM-PR.The concentration of the main active ingredients was determined using the Ultra Performance Liquid Chromatography-Tunable Ultraviolet(UPLC-TUV)method.The concentration of the main active ingredients of the decoction compatibility before and after combining AM-PR was also determined using the UPLC-TUV method.Results:Our findings reveal that upon combination,the time to maximum concentration(T_(max))of isochlorogenic acid A(ICA-A)and ataridolide Ⅱ(ATR-Ⅱ)T_(max)was prolonged,terminal elimination half-life(T_(1/2))was reduced,and maximum plasma concentrations(C_(max))increased.The T_(max)of ataridolide Ⅲ(ATR-Ⅲ)remained consistent,whereas its T_(1/2)and C_(max)were significantly reduced.Conversely,for peoniflorin(PAE),T_(max)occurred sooner,T_(1/2)was shortened,and C_(max)increased.The T_(max)for albiflorin(ALB)remained consistent,whereas T_(1/2)and C_(max)witnessed significant increases.The area under the moment curve(AUMC)(0-t)and AUMC(0-∞)of PAE,ALB,ICA-A,ATR-Ⅱ experienced an increase after AM-PR administration in rats,attributable to the heightened C_(max).In comparison to individual herb administration,the T_(max)of ALB was advanced in combination,the T_(max)of PAE remained unchanged,and the T_(max)of ICA-A and ART-Ⅱ was delayed,with an increased area under the concentration-time curve(AUC)(0-t),indicating enhanced C_(max)and bioavailability.Furthermore,the dissolution rates of PAE,ICA-A,and ATR-Ⅱ significantly improved after compatibility.Conclusions:This study partially clarifies the rationale and compatibility of AM-PR in treating FC and offers a new perspective on the pharmacokinetic interactions of AM-PR in FC treatment.展开更多
The crude and processed Paeoniae Radix Alba-Atractylodis Macrocephalae Rhizoma herbal pairs, originated from Bai-zhu-shao-yao-san, are used to treat different diseases clinically. In order to evaluate the crude and pr...The crude and processed Paeoniae Radix Alba-Atractylodis Macrocephalae Rhizoma herbal pairs, originated from Bai-zhu-shao-yao-san, are used to treat different diseases clinically. In order to evaluate the crude and processed Paeoniae Radix-Atractylodis Macrocephalae Rhizoma herbal pairs, a simple, easy, and sensitive high-performance liquid chromatography coupled with diode array detectors was developed for simultaneous determination of nine bioactive components in the herbal pairs. The calibration curve exhibited good linearity（r2≥0.9992）. The LODs and LOQs were ≤7.30 and 11.53 μg/m L, respectively. The intra-, inter-day and repeatability RSD values of the nine compounds were less than 3.86%, 2.71%, and 4.29%, respectively. The RSD stability values were less than 3.64%. The recovery of the method was in the range of 96.70%–102.10%, with RSD values less than 3.52%. The developed method can be applied to the intrinsic quality control of crude and processed Paeoniae Radix-Atractylodis Macrocephalae Rhizoma herbal pairs.展开更多
First at all, it introduced the concept and the damages of continuous cropping obstacle. Then, it analyzed the causes of continuous cropping obstacles for Atractylodes macrocephala Koidz. In the end, in order to provi...First at all, it introduced the concept and the damages of continuous cropping obstacle. Then, it analyzed the causes of continuous cropping obstacles for Atractylodes macrocephala Koidz. In the end, in order to provide guidance for pro- moting sustainable development of Atractylodes macrocephala Koidz industry in Pingjiang County, it put forward some control methods for eliminating continuous cropping obstacles of Atractylodes macrocephala Koidz, including breeding varieties with high resistance; applying rotation cropping and intercropping reasonable; rational fertilization and soil disinfection; introducing antagonistic bacterial and eliminating au- tointoxication.展开更多
Astragalus membranaceus(Radix Astragali, RA) and Atractylodes macrocephala(Rhizoma Atractylodis Macrocephalae, RAM) are often used to treat gastrointestinal diseases. In the present study, we determined the effects of...Astragalus membranaceus(Radix Astragali, RA) and Atractylodes macrocephala(Rhizoma Atractylodis Macrocephalae, RAM) are often used to treat gastrointestinal diseases. In the present study, we determined the effects of polysaccharides extracts from these two herbs on IEC-6 cell migration and explored the potential underlying mechanisms. A migration model with IEC-6 cells was induced using a single-edged razor blade along the diameter of cell layers in six-well polystyrene plates. The cells were grown in control--media or media containing spermidine(5 μmol·L^(-1), SPD), alpha-difluoromethylornithine(2.5 mmol·L^(-1), DFMO), 4-Aminopyridine-(40 μ-mol·L^(-1), 4-AP), the polysaccharide extracts of RA or RAM(50, 100, or 200 mg·L^(-1)), DFMO plus SPD, or DFMO plus polysaccharide extracts of RA or RAM for 12 or 24 h. Next, cytosolic free Ca^(2+)([Ca^(2+)]cyt) was measured using laser confocal microscopy, and cellular polyamine content was quantified with HPLC. Kv1.1 mRNA expression was assessed using RT-qPCR and Kv1.1 and RhoA protein expressions were measured with Western blotting analysis. A cell migration assay was carried out using Image-Pro Plus software. In addition, GC-MS was introduced to analyze the monosaccharide composition of both polysaccharide extracts. The resutls showed that treatment with polysaccharide extracts of RA or RAM significantly increased cellular polyamine content, elevated [Ca^(2+)]cyt and accelerated migration of IEC-6 cells, compared with the controls(P < 0.01). Polysaccharide extracts not only reversed the inhibitory effects of DFMO on cellular polyamine content and [Ca^(2+)]cyt, but also restored IEC-6 cell migration to control level(P < 0.01 or < 0.05). Kv1.1 mRNA and protein expressions were increased(P < 0.05) after polysaccharide extract treatment in polyamine-deficient IEC-6 cells and RhoA protein expression was increased. Molar ratios of D-ribose, D-arabinose, L-rhamnose, D-mannose, D-glucose, and D-galactose was 1.0:14.1:0.3:19.9:181.3:6.3 in RA and 1.0:4.3:0.1:5.7:2.8:2.2 in RAM. In conclusion, treatment with RA and RAM polysaccharide extracts stimulated migration of intestinal epithelial cells via a polyamine-Kv1.1 channel activated signaling pathway, which facilitated intestinal injury healing.展开更多
OBJECTIVE:To investigate the antagonistic effect of the extract of Baizhu(Rhizoma Atractylodis Macrocephalae)(RAM)on the intestinal absorption of brucine and strychnine in Strychnos nux-vomica(NUX)and propose the mech...OBJECTIVE:To investigate the antagonistic effect of the extract of Baizhu(Rhizoma Atractylodis Macrocephalae)(RAM)on the intestinal absorption of brucine and strychnine in Strychnos nux-vomica(NUX)and propose the mechanism of these effects.METHODS:The apparent permeability value(Papp)and absorption rate constant(Ka)were chosen as indices.The everted intestinal sac model and in situ single-pass intestinal perfusion model were used to study the effects of the RAM extract on the absorption of brucine and strychnine.To confirm the results,the brucine and strychnine concentrations in hepatic portal venous blood were determined.Western blotting was used to study P-glycoprotein(P-gp)expression in the Caco-2 cell line.RESULTS:Papp and Ka of brucine and strychnine were significantly increased in the presence of a P-gp inhibitor,but no significant increase was noted in the presence of a tight junction regulator.The RAM extract inhibited the absorption of brucine and strychnine and enhanced P-gp expression.CONCLUSION:The primary absorption mechanism for brucine and strychnine is passive transport,which is affected by P-gp.展开更多
Three eudesmanolide sesquiterpene-phenol hybrids,atramacronoids A-C(1-3),featuring an unusual6/6/5/5/6 skeleton furnished by forming an unexpected C-8-C-16 linkage,were obtained from the rhizomes of Atractylodes macro...Three eudesmanolide sesquiterpene-phenol hybrids,atramacronoids A-C(1-3),featuring an unusual6/6/5/5/6 skeleton furnished by forming an unexpected C-8-C-16 linkage,were obtained from the rhizomes of Atractylodes macrocephala.Their structures and absolute configurations were elucidated by spectroscopic data analysis,chemical calculations,combined with X-ray diffractions.The plausible biosynthetic pathways for compounds 1-3 are proposed.Surprisingly,compound 1 exhibited cytotoxicity against SGC-7901 cells by inducing cells apoptosis,which might relate to the promotion of synthesis of neutrophil elastase.展开更多
The study examined the inhibitory effect of Atractylodes macrocephala （AM） on the uterine contraction during premature delivery and explored its electrophysiological mechanism by studying the effects of AM on the C...The study examined the inhibitory effect of Atractylodes macrocephala （AM） on the uterine contraction during premature delivery and explored its electrophysiological mechanism by studying the effects of AM on the Ca^2＋-activated K^＋ currents of pregnant human myometrial smooth muscle cells with or without the treatment with intedeukin-6. Single cells were acutely isolated from pregnant human myometrial smooth muscles. Whole-cell Ca^2＋-activated K^＋ currents were recorded by using an Axopatchl-D amplifier. The cells were divided into three groups： group A in which AM was added into perfusate, group B, in which interleukin-6 was added into perfusate） and group C in which AM was added into perfusate after addition of interleukin-6. IL-6 10 ng/mL inhibited BKca by 36.9%±13.7% as compared with control （P〈0.01）. AM at 2 mg/mL raised BKca by 36.7%±22.6% or 45.2%±13.7% with or without the treatment of IL-6, respectively （P〈0.01）. It is concluded that AM was able to enhance the BKca of pregnant human myometrial smooth muscle cells treated or untreated with interleukin-6 and its effect on the BKca IL-treated cells was stronger that its effect on BKca of untreated cells. Our results suggested that AM can help to maintain the membrane potentials and the resting status of pregnant human myometrial smooth muscle cells.展开更多
Objectives:To provide a theoretical basis for the development of the new products of Poria cocos-Atractylodes macrocephala couplet medicine.Methods:All prescription preparations containing Poria cocos and Atractylodes...Objectives:To provide a theoretical basis for the development of the new products of Poria cocos-Atractylodes macrocephala couplet medicine.Methods:All prescription preparations containing Poria cocos and Atractylodes macrocephala were collected from the Drug Standards of the Ministry of Public Health Drug Standard·Traditional Chinese Medicine Set Prescription Preparation(called Traditional Chinese Medicine Set Prescription Preparation for short).After standardization,the information of each prescription preparation was input into the Chinese Traditional Medicine Inheritance Support Platform(V2.5),and the relevant rules of the software were adopted.Data mining methods were used to analyze the frequency of drugs,main symptoms and diseases in prescriptions,and to analyze the regularity of prescriptions.The prescription rules of top 2 high frequency attending syndromes and diseases were analyzed.Results:There were total of 337 prescription preparations containing couplet medicine of Poria cocos and Atractylodes macrocephala,107 kinds of main symptoms and 66 kinds of diseases.The high frequency syndromes were deficiency of Qi and blood and weakness of spleen and stomach,and the high frequency syndromes were anorexia and irregular menstruation.Conclusion:The couplet medicine of Poria cocos-atractylodes macrocephala prescription is mainly used to treat digestive tract diseases and gynecological diseases;it mostly takes tonifying deficiency efficat.It can treat different diseases being compatible with different medicinal materials.The study can provide theoretical basis for clinical application and new drug development of the couplet medicine of Poria cocos-atractylodes macrocephala.展开更多
Rhizome atractylodes macrocephalae is the dry roots of Atractylodes macrocephala Koidz.It is one of commonly used Chinese medicine.In the "Shennong′s Herbal",it was listed as the top grade.It mainly contain...Rhizome atractylodes macrocephalae is the dry roots of Atractylodes macrocephala Koidz.It is one of commonly used Chinese medicine.In the "Shennong′s Herbal",it was listed as the top grade.It mainly contains volatile oil,atractylenolides,atractylodes polysaccharides,glycosides and amino acids.And it has the medical functions of good for spleen and intestine,diuretic and dehumidification,hidroschesis,miscarriage prevention and soon.In order to provide references for further development and utilization,this paper systematic arranged the Chinese medicine atractylodes chemical composition,pharmacological effects,processing technology and effect of processing technology on chemical composition and pharmacological action.展开更多
[Objective] The paper was to explore the effective agent against seedling blight of Atractylodes macrocephala. [Method] The control effects of 60% validamycin A SP against seeding blight of A. macrocephala were studie...[Objective] The paper was to explore the effective agent against seedling blight of Atractylodes macrocephala. [Method] The control effects of 60% validamycin A SP against seeding blight of A. macrocephala were studied in the field, and compared with that of control agent 20% bismerthiazol WP. [Result] At 14 d post the third spraying, the control effect of 60% validamycin A SP at the dose of 495-540 g/hm;was 76.9%,which was equivalent to that of control agent 20% bismerthiazol WP sprayed at the dose of 270 g/hm;（76.7%）. [Conclusion] 60% Validamycin A SP could be used as the ideal agent against seedling blight of A. macrocephala, with good prospects of application and popularization.展开更多
[Objectives]The paper was to explore the pharmacodynamic substances and mechanism of Atractylodes macrocephala in treating primary dysmenorrhea(PD).[Methods]The components of A.macrocephala were qualitatively identifi...[Objectives]The paper was to explore the pharmacodynamic substances and mechanism of Atractylodes macrocephala in treating primary dysmenorrhea(PD).[Methods]The components of A.macrocephala were qualitatively identified by ultra high performance liquid chromatography quadrupole-time of flight mass spectrometry(UPLC-MS)combined with analyst TF 1.7.1 and peakview 2.2 software with reference to internal databases and literatures.The chemical components of A.macrocephala and the target of PD were collected by using network pharmacological data.The common genes were analyzed by Gene Ontology(GO)and Kyoto Encyclopedia of Genes and Genomes(KEGG)of genes and genomes with the help of String database and Metascape platform,and the affinity between core molecules and key targets was verified.[Results]A total of 23 chemical components of A.macrocephala were identified,and 301 gene targets of chemical components of A.macrocephala,614 targets of PD,and 25 intersection targets were obtained.GO analysis results obtained 505 biological processes,11 cellular components,and 33 molecular functions.KEGG pathway analysis showed that it mainly involved TNF signaling pathway,IL-17 signaling pathway,estrogen receptor signaling pathway and arachidonic acid metabolism.The top 4 targets of PPI network centrality and the top 5 compounds of A.macrocephala-component-target-disease network centrality were selected for docking.The docking results showed that atractylenolide I,Selinar-4(15),7(11)-dien-8-one,and atractylenolide II had strong binding ability.[Conclusions]A.macrocephala may exert a curative effect on PD by targeting atractylenolide I,Selinar-4(15),7(11)-dien-8-one,and atractylenolide II on key targets such as TNF,IL6,IL1β,PTGS2 to regulate cellular TNF signaling pathway,IL-17 signaling pathway,estrogen receptor signaling pathway,and arachidonic acid metabolism.展开更多
Objective: to study the effect of different conditions on the content change and internal law of Atractylenolide I, II and III. Methods: the samples of Atractylodes macrocephala Koidz were treated with different bakin...Objective: to study the effect of different conditions on the content change and internal law of Atractylenolide I, II and III. Methods: the samples of Atractylodes macrocephala Koidz were treated with different baking temperatures, baking time, humidity, open space time, sample morphology and other conditions. The contents of Atractylodes macrocephala Koidz I, II and III were determined by HPLC, and the change rules were analyzed. Results: for the original medicinal materials and decoction pieces, temperature and heating time had a certain effect on the conversion amount, but the effect was limited. However, under the influence of the appropriate heating temperature and heating time, the content of pulverized sample powder changed significantly. In the case of Atractylodes macrocephala Koidz in the form of powder, with the increase of storage time, the content of Atractylenolide I, II and III changed significantly. Conclusion: comparison of the content change law of Atractylodes macrocephala Koidz lactone I, II, III is conducive to optimizing the processing method of Atractylodes macrocephala Koidz, and provides a reference for the quality control of Atractylodes macrocephala Koidz.展开更多
Background and aims:Metabolic dysfunction-associated fatty liver disease(MAFLD)is a common chronic condition that can lead to cancer due to its complex pathogenesis.Therapeutic agents targeting AMPactivated protein ki...Background and aims:Metabolic dysfunction-associated fatty liver disease(MAFLD)is a common chronic condition that can lead to cancer due to its complex pathogenesis.Therapeutic agents targeting AMPactivated protein kinase(AMPK)activation have been suggested as potential treatments for metabolic disorders such as metabolic dysfunction-associated steatohepatitis(MASH).Rhizoma Atractylodis Macrocephalae(RAM)has been clinically used to treat obesity-related health problems,but its therapeutic effects on MAFLD and the underlying mechanism remain unclear.Therefore,this study was conducted to evaluate the function and underlying mechanism of RAM in the treatment of MAFLD.Methods:The effect of RAM decoction on MAFLD was evaluated using a high-fat diet(HFD)-induced MAFLD mouse model.In vitro studies were conducted using a palmitic acid/oleic acid-induced lipid accumulation model in the alpha mouse liver 12 cells and RAM-containing serum.The underlying mechanisms were elucidated through a combination of network pharmacology analysis,immunohistochemistry,western blotting,and polymerase chain reaction analysis.Results:Administration of RAM decoction significantly reduced body weight gain in MAFLD mice without changing food intake.The weights of the liver and inguinal adipose tissues were also reduced after RAM treatment.Additionally,RAM administration decreased serum levels of alanine aminotransferase,aspartate transaminase,total cholesterol,triglyceride,low-density lipoprotein cholesterol,and glucose,while reducing lipid droplet accumulation in the liver tissues of MAFLD mice.The underlying mechanisms included the activation of the phosphorylation of AMPK and acetyl-CoA carboxylase(ACC),and inhibition of the expression of sterol regulatory element binding protein 1(SREBP1).However,RAM did not alter the protein expression levels of peroxisome proliferator-activated receptor a and carnitine palmitoyltransferase-1a.Furthermore,the RAM-induced upregulation of phosphorylated AMPK,phosphorylated ACC,and SREBP1 expression,as well as the downregulation of fatty acid synthase expression,were reversed by using an AMPK inhibitor.Conclusions:Through a combination of network pharmacology and experimental validation,we demonstrated that RAM may exert therapeutic effects on MAFLD by inhibiting lipid synthesis and activating phosphorylated AMPK pathways.展开更多
Background:Currently,traditional methods of treating acute gastric ulcer(AGU)have many drawbacks,necessitating an alternative therapy with fewer adverse effects.Atractylodis Macrocephalae Rhizoma(BZ)is known for stren...Background:Currently,traditional methods of treating acute gastric ulcer(AGU)have many drawbacks,necessitating an alternative therapy with fewer adverse effects.Atractylodis Macrocephalae Rhizoma(BZ)is known for strengthening the spleen and harmonizing the stomach.BZ processed with Aurantii Fructus Immaturus juice(ZSZBZ),a classic decoction since the Han Dynasty,can enhance the efficacy of BZ.However,the key active components and targets of action of ZSZBZ remain undiscovered.Aimof the study:This study aimed to investigate the bioactive chemical constituents of ZSZBZ against AGU and their possible mechanisms of action,elucidating the scientific content of ZSZBZ processing.Materials and methods:Initially,we examined rat stomach histopathology and conducted ELISA for oxidative stress and inflammation.Subsequently,we investigated underlying mechanisms using metabolomics.Further analysis of potent components and key targets in ZSZBZ was conducted through liquid chromatography-mass spectrometry analysis combined with network pharmacology.Finally,key targets were analyzed by Western blot.Results:ZSZBZ improved gastric histopathology,reversing high alcohol-induced oxidative stress(SOD,CAT)and inflammatory level(TNF-α,IL-6)disorders.This is associated with ZSZBZ’s regulation of amino acid metabolism,energy metabolism,and inflammatory response-related metabolic pathways,along with key targets PTGS2,MAPK1,and KDR.The significant increase in potency of ZSZBZ may be attributed to elevated levels of naringenin,hesperidin,hesperidin,and rhamnoceroside after concoction.Conclusions:Combining metabolomics and network pharmacology,this study elucidated that ZSZBZ enhanced gastroprotection by modulating amino acid metabolism,antioxidant,and inflammation-related targets and pathways,providing insights into the bioactive compounds and potential mechanisms of herbal concoctions.展开更多
目的旨在建立一种基于生物传感器联合超高效液相色谱/串联质谱(ultra-performance liquid chromatography with electrospray tandem mass spectrometry,UPLC-MS/MS)的中药苦味关键质量属性辨识方法。以白术内酯类成分为研究对象,通过...目的旨在建立一种基于生物传感器联合超高效液相色谱/串联质谱(ultra-performance liquid chromatography with electrospray tandem mass spectrometry,UPLC-MS/MS)的中药苦味关键质量属性辨识方法。以白术内酯类成分为研究对象,通过分子对接与生物传感技术揭示其与苦味受体的相互作用机制,实现苦味属性从传统经验判定到分子水平表征的跨越,为完善白术质量控制体系提供支撑。方法采用D101大孔吸附树脂结合紫外分光光度法,制备并筛选富含内酯类成分的白术组分;通过UPLC-MS/MS与分子对接技术,在分子水平解析白术组分与味觉受体的相互作用特征;采用生物传感器与UPLCMS/MS联用技术,实现白术组分苦味关键质量属性的精准辨识。结果成功制得白术不同极性组分11个,其中白术醇提物70%组分的总内酯含量最高,为后续性味研究的理想载体;分子对接实验显示白术组分与Ⅱ型味觉受体家族14号成员(taste receptor type 2 member 14,TAS2R14)的结合展现出明显优势,在分子层面揭示了白术组分具有强烈趋于苦味属性的作用特质;进一步构建苦味生物传感器,对白术组分的苦味属性进行表征,结果显示白术组分与TAS2R14的相互结合强度为49.0ng/L,属于强相互作用,表明以内酯类成分为主的白术组分具有显著的苦味属性,该结果与分子对接结果相互印证,增强了实验结论的可靠性;最后,联合UPLC-MS/MS技术,共辨识得到包括白术内酯Ⅱ在内的苦味关键质量属性13个,在物质基础层面表明白术组分与苦味受体TAS2R14的结合受关键质量属性驱动,为理解白术内酯类成分苦味特性提供直接证据。结论通过多技术融合的系统性研究,从分子相互作用到物质基础层面揭示了白术内酯类成分苦味属性的本质,所发现的苦味关键质量属性为建立基于苦味特征的白术质量控制方法奠定了理论基础,此外,提出的技术路线为中药苦味物质基础研究提供了新的方法学参考。展开更多
基金Natural Science Foundation of Zhejiang Province,Grant/Award Number:Y19H280022。
文摘Background:In a previous study,we found that Atractylodes macrocephala and Paeoniae radix(AM-PR)was useful for the alleviation of functional constipation(FC).However,the precise mechanism underlying the compatibility between AM and PR in the treatment of FC remains uncertain.This study aims to analyze the pharmacokinetic differences in the active ingredients in the blood of rat models with FC when applied individually and in combination with AM-PR.It also seeks to compare the changes in the content of the active ingredient when applied individually and in combination with in vitro AM-PR,further in-depth investigation into its material foundation in terms of pharmacokinetics,as well as the composition of the substance.Methods:Blood microdialysis samples were collected using microdialysis technology.These samples from rats with FC were compared after administration of AM,PR,and AM-PR.The concentration of the main active ingredients was determined using the Ultra Performance Liquid Chromatography-Tunable Ultraviolet(UPLC-TUV)method.The concentration of the main active ingredients of the decoction compatibility before and after combining AM-PR was also determined using the UPLC-TUV method.Results:Our findings reveal that upon combination,the time to maximum concentration(T_(max))of isochlorogenic acid A(ICA-A)and ataridolide Ⅱ(ATR-Ⅱ)T_(max)was prolonged,terminal elimination half-life(T_(1/2))was reduced,and maximum plasma concentrations(C_(max))increased.The T_(max)of ataridolide Ⅲ(ATR-Ⅲ)remained consistent,whereas its T_(1/2)and C_(max)were significantly reduced.Conversely,for peoniflorin(PAE),T_(max)occurred sooner,T_(1/2)was shortened,and C_(max)increased.The T_(max)for albiflorin(ALB)remained consistent,whereas T_(1/2)and C_(max)witnessed significant increases.The area under the moment curve(AUMC)(0-t)and AUMC(0-∞)of PAE,ALB,ICA-A,ATR-Ⅱ experienced an increase after AM-PR administration in rats,attributable to the heightened C_(max).In comparison to individual herb administration,the T_(max)of ALB was advanced in combination,the T_(max)of PAE remained unchanged,and the T_(max)of ICA-A and ART-Ⅱ was delayed,with an increased area under the concentration-time curve(AUC)(0-t),indicating enhanced C_(max)and bioavailability.Furthermore,the dissolution rates of PAE,ICA-A,and ATR-Ⅱ significantly improved after compatibility.Conclusions:This study partially clarifies the rationale and compatibility of AM-PR in treating FC and offers a new perspective on the pharmacokinetic interactions of AM-PR in FC treatment.
基金The National Natural Science Foundation of China(Grant No.81202918)the Open Project of National First-Class Key Discipline for Science of Chinese Materia Medica,Nanjing University of Chinese Medicine(Grant No.2011ZYX2-006)+2 种基金the Science and Technology Project of Hangzhou,China(Grant No.20130533B68 and 20131813A23)the Chinese Medicine Research Program of Zhejiang Province,China(Grant No.2014ZQ008 and 2015ZQ011)the Science Foundation of Zhejiang Chinese Medical University(Grant No.2011ZY25 and 2013ZZ12)
文摘The crude and processed Paeoniae Radix Alba-Atractylodis Macrocephalae Rhizoma herbal pairs, originated from Bai-zhu-shao-yao-san, are used to treat different diseases clinically. In order to evaluate the crude and processed Paeoniae Radix-Atractylodis Macrocephalae Rhizoma herbal pairs, a simple, easy, and sensitive high-performance liquid chromatography coupled with diode array detectors was developed for simultaneous determination of nine bioactive components in the herbal pairs. The calibration curve exhibited good linearity（r2≥0.9992）. The LODs and LOQs were ≤7.30 and 11.53 μg/m L, respectively. The intra-, inter-day and repeatability RSD values of the nine compounds were less than 3.86%, 2.71%, and 4.29%, respectively. The RSD stability values were less than 3.64%. The recovery of the method was in the range of 96.70%–102.10%, with RSD values less than 3.52%. The developed method can be applied to the intrinsic quality control of crude and processed Paeoniae Radix-Atractylodis Macrocephalae Rhizoma herbal pairs.
文摘First at all, it introduced the concept and the damages of continuous cropping obstacle. Then, it analyzed the causes of continuous cropping obstacles for Atractylodes macrocephala Koidz. In the end, in order to provide guidance for pro- moting sustainable development of Atractylodes macrocephala Koidz industry in Pingjiang County, it put forward some control methods for eliminating continuous cropping obstacles of Atractylodes macrocephala Koidz, including breeding varieties with high resistance; applying rotation cropping and intercropping reasonable; rational fertilization and soil disinfection; introducing antagonistic bacterial and eliminating au- tointoxication.
基金supported by the National Natural Science Foundation of China(Nos.30772753,81173254,and 81673940)the Science and Technology Program of Guangzhou(No.20160701335)the First-class discipline construction major project of Guangzhou University of Chinese Medicine(Guangzhou University of Chinese Medicine Planning,2018-No.6)
文摘Astragalus membranaceus(Radix Astragali, RA) and Atractylodes macrocephala(Rhizoma Atractylodis Macrocephalae, RAM) are often used to treat gastrointestinal diseases. In the present study, we determined the effects of polysaccharides extracts from these two herbs on IEC-6 cell migration and explored the potential underlying mechanisms. A migration model with IEC-6 cells was induced using a single-edged razor blade along the diameter of cell layers in six-well polystyrene plates. The cells were grown in control--media or media containing spermidine(5 μmol·L^(-1), SPD), alpha-difluoromethylornithine(2.5 mmol·L^(-1), DFMO), 4-Aminopyridine-(40 μ-mol·L^(-1), 4-AP), the polysaccharide extracts of RA or RAM(50, 100, or 200 mg·L^(-1)), DFMO plus SPD, or DFMO plus polysaccharide extracts of RA or RAM for 12 or 24 h. Next, cytosolic free Ca^(2+)([Ca^(2+)]cyt) was measured using laser confocal microscopy, and cellular polyamine content was quantified with HPLC. Kv1.1 mRNA expression was assessed using RT-qPCR and Kv1.1 and RhoA protein expressions were measured with Western blotting analysis. A cell migration assay was carried out using Image-Pro Plus software. In addition, GC-MS was introduced to analyze the monosaccharide composition of both polysaccharide extracts. The resutls showed that treatment with polysaccharide extracts of RA or RAM significantly increased cellular polyamine content, elevated [Ca^(2+)]cyt and accelerated migration of IEC-6 cells, compared with the controls(P < 0.01). Polysaccharide extracts not only reversed the inhibitory effects of DFMO on cellular polyamine content and [Ca^(2+)]cyt, but also restored IEC-6 cell migration to control level(P < 0.01 or < 0.05). Kv1.1 mRNA and protein expressions were increased(P < 0.05) after polysaccharide extract treatment in polyamine-deficient IEC-6 cells and RhoA protein expression was increased. Molar ratios of D-ribose, D-arabinose, L-rhamnose, D-mannose, D-glucose, and D-galactose was 1.0:14.1:0.3:19.9:181.3:6.3 in RA and 1.0:4.3:0.1:5.7:2.8:2.2 in RAM. In conclusion, treatment with RA and RAM polysaccharide extracts stimulated migration of intestinal epithelial cells via a polyamine-Kv1.1 channel activated signaling pathway, which facilitated intestinal injury healing.
基金the National Natural Science Foundation of China(No.81660757 and No.81303237)the Academic and Technological Foregoer Funds of Jiangxi Province,China(No.20162BCB22015)+3 种基金the Project on Cultivation of Medical Elite(Gan Po Ying Cai 555)(2013296)the Youth Science Funds of Jiangxi Province,China(No.20153BCB23019)the National Natural Science Foundation of Jiangxi Province(No.20161ACB21020)the Natural Science Research Project of Huaian(No.HAB201716)。
文摘OBJECTIVE:To investigate the antagonistic effect of the extract of Baizhu(Rhizoma Atractylodis Macrocephalae)(RAM)on the intestinal absorption of brucine and strychnine in Strychnos nux-vomica(NUX)and propose the mechanism of these effects.METHODS:The apparent permeability value(Papp)and absorption rate constant(Ka)were chosen as indices.The everted intestinal sac model and in situ single-pass intestinal perfusion model were used to study the effects of the RAM extract on the absorption of brucine and strychnine.To confirm the results,the brucine and strychnine concentrations in hepatic portal venous blood were determined.Western blotting was used to study P-glycoprotein(P-gp)expression in the Caco-2 cell line.RESULTS:Papp and Ka of brucine and strychnine were significantly increased in the presence of a P-gp inhibitor,but no significant increase was noted in the presence of a tight junction regulator.The RAM extract inhibited the absorption of brucine and strychnine and enhanced P-gp expression.CONCLUSION:The primary absorption mechanism for brucine and strychnine is passive transport,which is affected by P-gp.
基金supported by the National Natural Science Foundation of China(No.82073992)the CAMS Innovation Fund for Medical Sciences(CIFMS,No.2021-I2M-1-071)。
文摘Three eudesmanolide sesquiterpene-phenol hybrids,atramacronoids A-C(1-3),featuring an unusual6/6/5/5/6 skeleton furnished by forming an unexpected C-8-C-16 linkage,were obtained from the rhizomes of Atractylodes macrocephala.Their structures and absolute configurations were elucidated by spectroscopic data analysis,chemical calculations,combined with X-ray diffractions.The plausible biosynthetic pathways for compounds 1-3 are proposed.Surprisingly,compound 1 exhibited cytotoxicity against SGC-7901 cells by inducing cells apoptosis,which might relate to the promotion of synthesis of neutrophil elastase.
文摘The study examined the inhibitory effect of Atractylodes macrocephala （AM） on the uterine contraction during premature delivery and explored its electrophysiological mechanism by studying the effects of AM on the Ca^2＋-activated K^＋ currents of pregnant human myometrial smooth muscle cells with or without the treatment with intedeukin-6. Single cells were acutely isolated from pregnant human myometrial smooth muscles. Whole-cell Ca^2＋-activated K^＋ currents were recorded by using an Axopatchl-D amplifier. The cells were divided into three groups： group A in which AM was added into perfusate, group B, in which interleukin-6 was added into perfusate） and group C in which AM was added into perfusate after addition of interleukin-6. IL-6 10 ng/mL inhibited BKca by 36.9%±13.7% as compared with control （P〈0.01）. AM at 2 mg/mL raised BKca by 36.7%±22.6% or 45.2%±13.7% with or without the treatment of IL-6, respectively （P〈0.01）. It is concluded that AM was able to enhance the BKca of pregnant human myometrial smooth muscle cells treated or untreated with interleukin-6 and its effect on the BKca IL-treated cells was stronger that its effect on BKca of untreated cells. Our results suggested that AM can help to maintain the membrane potentials and the resting status of pregnant human myometrial smooth muscle cells.
文摘Objectives:To provide a theoretical basis for the development of the new products of Poria cocos-Atractylodes macrocephala couplet medicine.Methods:All prescription preparations containing Poria cocos and Atractylodes macrocephala were collected from the Drug Standards of the Ministry of Public Health Drug Standard·Traditional Chinese Medicine Set Prescription Preparation(called Traditional Chinese Medicine Set Prescription Preparation for short).After standardization,the information of each prescription preparation was input into the Chinese Traditional Medicine Inheritance Support Platform(V2.5),and the relevant rules of the software were adopted.Data mining methods were used to analyze the frequency of drugs,main symptoms and diseases in prescriptions,and to analyze the regularity of prescriptions.The prescription rules of top 2 high frequency attending syndromes and diseases were analyzed.Results:There were total of 337 prescription preparations containing couplet medicine of Poria cocos and Atractylodes macrocephala,107 kinds of main symptoms and 66 kinds of diseases.The high frequency syndromes were deficiency of Qi and blood and weakness of spleen and stomach,and the high frequency syndromes were anorexia and irregular menstruation.Conclusion:The couplet medicine of Poria cocos-atractylodes macrocephala prescription is mainly used to treat digestive tract diseases and gynecological diseases;it mostly takes tonifying deficiency efficat.It can treat different diseases being compatible with different medicinal materials.The study can provide theoretical basis for clinical application and new drug development of the couplet medicine of Poria cocos-atractylodes macrocephala.
基金supported by National Natural Science Foundation of China(81473549)National Natural Science Foundation of China Youth Fund Project(31402237)+1 种基金National "Major New Drug Creation" Major Science and Technology Projects(2014ZX09304-306-04)Ministry of Education of the Central University Basic Scientific Research Business Fee(XDJK2015D016)
文摘Rhizome atractylodes macrocephalae is the dry roots of Atractylodes macrocephala Koidz.It is one of commonly used Chinese medicine.In the "Shennong′s Herbal",it was listed as the top grade.It mainly contains volatile oil,atractylenolides,atractylodes polysaccharides,glycosides and amino acids.And it has the medical functions of good for spleen and intestine,diuretic and dehumidification,hidroschesis,miscarriage prevention and soon.In order to provide references for further development and utilization,this paper systematic arranged the Chinese medicine atractylodes chemical composition,pharmacological effects,processing technology and effect of processing technology on chemical composition and pharmacological action.
文摘[Objective] The paper was to explore the effective agent against seedling blight of Atractylodes macrocephala. [Method] The control effects of 60% validamycin A SP against seeding blight of A. macrocephala were studied in the field, and compared with that of control agent 20% bismerthiazol WP. [Result] At 14 d post the third spraying, the control effect of 60% validamycin A SP at the dose of 495-540 g/hm;was 76.9%,which was equivalent to that of control agent 20% bismerthiazol WP sprayed at the dose of 270 g/hm;（76.7%）. [Conclusion] 60% Validamycin A SP could be used as the ideal agent against seedling blight of A. macrocephala, with good prospects of application and popularization.
基金Youth Science Foundation Project of National Natural Science Foundation of China(82104384)Science and Technology Research Project of Colleges and Universities in Hebei Province(QN2021008)+3 种基金Research Start-up Fund for High-level Talents of Chengde Medical University(202103)Key Discipline Construction Project of Colleges and Universities in Hebei Province(JJG[2013]4)"Technology Innovation Guidance Special-Science and Technology Work Consultation"Project of Hebei Provincial Department of Science and TechnologyYouth PI Science and Technology Innovation Team of TCM Pharmacodynamic Substance Foundation of Chengde Medical University.
文摘[Objectives]The paper was to explore the pharmacodynamic substances and mechanism of Atractylodes macrocephala in treating primary dysmenorrhea(PD).[Methods]The components of A.macrocephala were qualitatively identified by ultra high performance liquid chromatography quadrupole-time of flight mass spectrometry(UPLC-MS)combined with analyst TF 1.7.1 and peakview 2.2 software with reference to internal databases and literatures.The chemical components of A.macrocephala and the target of PD were collected by using network pharmacological data.The common genes were analyzed by Gene Ontology(GO)and Kyoto Encyclopedia of Genes and Genomes(KEGG)of genes and genomes with the help of String database and Metascape platform,and the affinity between core molecules and key targets was verified.[Results]A total of 23 chemical components of A.macrocephala were identified,and 301 gene targets of chemical components of A.macrocephala,614 targets of PD,and 25 intersection targets were obtained.GO analysis results obtained 505 biological processes,11 cellular components,and 33 molecular functions.KEGG pathway analysis showed that it mainly involved TNF signaling pathway,IL-17 signaling pathway,estrogen receptor signaling pathway and arachidonic acid metabolism.The top 4 targets of PPI network centrality and the top 5 compounds of A.macrocephala-component-target-disease network centrality were selected for docking.The docking results showed that atractylenolide I,Selinar-4(15),7(11)-dien-8-one,and atractylenolide II had strong binding ability.[Conclusions]A.macrocephala may exert a curative effect on PD by targeting atractylenolide I,Selinar-4(15),7(11)-dien-8-one,and atractylenolide II on key targets such as TNF,IL6,IL1β,PTGS2 to regulate cellular TNF signaling pathway,IL-17 signaling pathway,estrogen receptor signaling pathway,and arachidonic acid metabolism.
文摘Objective: to study the effect of different conditions on the content change and internal law of Atractylenolide I, II and III. Methods: the samples of Atractylodes macrocephala Koidz were treated with different baking temperatures, baking time, humidity, open space time, sample morphology and other conditions. The contents of Atractylodes macrocephala Koidz I, II and III were determined by HPLC, and the change rules were analyzed. Results: for the original medicinal materials and decoction pieces, temperature and heating time had a certain effect on the conversion amount, but the effect was limited. However, under the influence of the appropriate heating temperature and heating time, the content of pulverized sample powder changed significantly. In the case of Atractylodes macrocephala Koidz in the form of powder, with the increase of storage time, the content of Atractylenolide I, II and III changed significantly. Conclusion: comparison of the content change law of Atractylodes macrocephala Koidz lactone I, II, III is conducive to optimizing the processing method of Atractylodes macrocephala Koidz, and provides a reference for the quality control of Atractylodes macrocephala Koidz.
基金supported by the National Natural Science Foundation of China(No.82370582 to Xiaoni Kong)The YangFan project from the Science and Technology Commission of Shanghai Municipality(No.22YF1449600 to Jiacheng Lin)State Administration of Traditional Chinese Medicine High-level Key Disciplines Program(No.ZYYZDXK-2023060)。
文摘Background and aims:Metabolic dysfunction-associated fatty liver disease(MAFLD)is a common chronic condition that can lead to cancer due to its complex pathogenesis.Therapeutic agents targeting AMPactivated protein kinase(AMPK)activation have been suggested as potential treatments for metabolic disorders such as metabolic dysfunction-associated steatohepatitis(MASH).Rhizoma Atractylodis Macrocephalae(RAM)has been clinically used to treat obesity-related health problems,but its therapeutic effects on MAFLD and the underlying mechanism remain unclear.Therefore,this study was conducted to evaluate the function and underlying mechanism of RAM in the treatment of MAFLD.Methods:The effect of RAM decoction on MAFLD was evaluated using a high-fat diet(HFD)-induced MAFLD mouse model.In vitro studies were conducted using a palmitic acid/oleic acid-induced lipid accumulation model in the alpha mouse liver 12 cells and RAM-containing serum.The underlying mechanisms were elucidated through a combination of network pharmacology analysis,immunohistochemistry,western blotting,and polymerase chain reaction analysis.Results:Administration of RAM decoction significantly reduced body weight gain in MAFLD mice without changing food intake.The weights of the liver and inguinal adipose tissues were also reduced after RAM treatment.Additionally,RAM administration decreased serum levels of alanine aminotransferase,aspartate transaminase,total cholesterol,triglyceride,low-density lipoprotein cholesterol,and glucose,while reducing lipid droplet accumulation in the liver tissues of MAFLD mice.The underlying mechanisms included the activation of the phosphorylation of AMPK and acetyl-CoA carboxylase(ACC),and inhibition of the expression of sterol regulatory element binding protein 1(SREBP1).However,RAM did not alter the protein expression levels of peroxisome proliferator-activated receptor a and carnitine palmitoyltransferase-1a.Furthermore,the RAM-induced upregulation of phosphorylated AMPK,phosphorylated ACC,and SREBP1 expression,as well as the downregulation of fatty acid synthase expression,were reversed by using an AMPK inhibitor.Conclusions:Through a combination of network pharmacology and experimental validation,we demonstrated that RAM may exert therapeutic effects on MAFLD by inhibiting lipid synthesis and activating phosphorylated AMPK pathways.
基金funded by the Jiangxi Provincial Natural Science Foundation Youth Project(20212BAB216011)the Second National Famous ChineseMedicine Practitioner(Gong Qianfeng)Inheritance Workshop of the State Administration of Traditional ChineseMedicine(State Chinese Medicine Office Human Education Letter[2022]no.245)+2 种基金2023 National Chinese Medicine Characteristic Technology Inheritance Talent Training Program(State Chinese Medicine Human Education Letter[2023]no.96)Jiangxi Province,the young and medium-aged backbone talents of traditional Chinese medicine(the fourth batch)(Gan TCM Science and Education[2022]no.7)the seventh batch of the national old Chinese medicine experts in academic experience successors(State Chinesemedicine human education letter[2022]no.76).
文摘Background:Currently,traditional methods of treating acute gastric ulcer(AGU)have many drawbacks,necessitating an alternative therapy with fewer adverse effects.Atractylodis Macrocephalae Rhizoma(BZ)is known for strengthening the spleen and harmonizing the stomach.BZ processed with Aurantii Fructus Immaturus juice(ZSZBZ),a classic decoction since the Han Dynasty,can enhance the efficacy of BZ.However,the key active components and targets of action of ZSZBZ remain undiscovered.Aimof the study:This study aimed to investigate the bioactive chemical constituents of ZSZBZ against AGU and their possible mechanisms of action,elucidating the scientific content of ZSZBZ processing.Materials and methods:Initially,we examined rat stomach histopathology and conducted ELISA for oxidative stress and inflammation.Subsequently,we investigated underlying mechanisms using metabolomics.Further analysis of potent components and key targets in ZSZBZ was conducted through liquid chromatography-mass spectrometry analysis combined with network pharmacology.Finally,key targets were analyzed by Western blot.Results:ZSZBZ improved gastric histopathology,reversing high alcohol-induced oxidative stress(SOD,CAT)and inflammatory level(TNF-α,IL-6)disorders.This is associated with ZSZBZ’s regulation of amino acid metabolism,energy metabolism,and inflammatory response-related metabolic pathways,along with key targets PTGS2,MAPK1,and KDR.The significant increase in potency of ZSZBZ may be attributed to elevated levels of naringenin,hesperidin,hesperidin,and rhamnoceroside after concoction.Conclusions:Combining metabolomics and network pharmacology,this study elucidated that ZSZBZ enhanced gastroprotection by modulating amino acid metabolism,antioxidant,and inflammation-related targets and pathways,providing insights into the bioactive compounds and potential mechanisms of herbal concoctions.
文摘目的旨在建立一种基于生物传感器联合超高效液相色谱/串联质谱(ultra-performance liquid chromatography with electrospray tandem mass spectrometry,UPLC-MS/MS)的中药苦味关键质量属性辨识方法。以白术内酯类成分为研究对象,通过分子对接与生物传感技术揭示其与苦味受体的相互作用机制,实现苦味属性从传统经验判定到分子水平表征的跨越,为完善白术质量控制体系提供支撑。方法采用D101大孔吸附树脂结合紫外分光光度法,制备并筛选富含内酯类成分的白术组分;通过UPLC-MS/MS与分子对接技术,在分子水平解析白术组分与味觉受体的相互作用特征;采用生物传感器与UPLCMS/MS联用技术,实现白术组分苦味关键质量属性的精准辨识。结果成功制得白术不同极性组分11个,其中白术醇提物70%组分的总内酯含量最高,为后续性味研究的理想载体;分子对接实验显示白术组分与Ⅱ型味觉受体家族14号成员(taste receptor type 2 member 14,TAS2R14)的结合展现出明显优势,在分子层面揭示了白术组分具有强烈趋于苦味属性的作用特质;进一步构建苦味生物传感器,对白术组分的苦味属性进行表征,结果显示白术组分与TAS2R14的相互结合强度为49.0ng/L,属于强相互作用,表明以内酯类成分为主的白术组分具有显著的苦味属性,该结果与分子对接结果相互印证,增强了实验结论的可靠性;最后,联合UPLC-MS/MS技术,共辨识得到包括白术内酯Ⅱ在内的苦味关键质量属性13个,在物质基础层面表明白术组分与苦味受体TAS2R14的结合受关键质量属性驱动,为理解白术内酯类成分苦味特性提供直接证据。结论通过多技术融合的系统性研究,从分子相互作用到物质基础层面揭示了白术内酯类成分苦味属性的本质,所发现的苦味关键质量属性为建立基于苦味特征的白术质量控制方法奠定了理论基础,此外,提出的技术路线为中药苦味物质基础研究提供了新的方法学参考。
