Chemical composition and pharmacological activities of Atractylodes lancea:A review

Atractylodes lancea(called Cangzhu in China)is a medicinal plant that has long been used as tonic agent in various ethno-medical systems in East Asia,especially in China,for the treatment of gastrointestinal dysfunction,cancer,osteoporosis,obesity and fetal irritability.We used the TCMSP database to search for the main active ingredients and traditional Chinese medicine targets of Atractylodes macrocephala.There are a total of 38 related articles,of which 27 are closely related to chemical composition and activity.This study reviews the chemical components and pharmacological effects of A.lancea,aiming to provide reference for its further research and development.

关苍术亲脂性化学成分研究

目的:研究关苍术亲脂性成分的化学成分。方法:使用硅胶柱色谱、Sephadex LH-20柱色谱、中压液相色谱和半制备HPLC等方法对关苍术中的化学成分进行分离纯化,并通过理化性质和MS与NMR等波谱技术对其化学成分进行结构鉴定。结果:从关苍术药材中分离并鉴定了12种化合物,分别鉴定为osthol(1)、Atractylochromene(2)、6,7-二羟基-8-甲氧基香豆素(3)、8-羟基-6,7-二甲氧基香豆素(4)、7-甲氧基香豆素(5)、豆甾-4-烯-3-酮(6)、蒲公英萜醇乙酸酯(7)、白术内酯Ⅱ(8)、白术内酯Ⅰ(9)、桉叶-4(15)-烯-7β,11-二醇(10)、反式对羟基桂皮酸甲酯(11)、丁香醛(12)。结论:化合物1,3~6,10~12为首次从关苍术中分离的化合物。

Chemical components and protective effects of Atractylodes japonica Koidz.ex Kitam against acetic acid-induced gastric ulcer in rats

BACKGROUND Atractylodes japonica Koidz.ex Kitam.(A.japonica,Chinese name:Guan-Cangzhu,Japanese name:Byaku-jutsu),a perennial herb,which is mainly distributed in northeast area of China,it’s often used to treat digestive system diseases such as gastric ulcer(GU).However,the mechanism of its potential protective effects against GU remains unclear.AIM To investigate the protective effects of A.japonica on acetic acid-induced GU rats.METHODS The chemical constituents of A.japonica were determined by ultra performance liquid chromatography tandem mass spectrometry(UPLC-MS/MS)analysis.The rat model of GU was simulated by acetic acid method.The pathological changes of gastric tissues were evaluated by hematoxylin-eosin stain,the levels of epidermal growth factor(EGF),EGF receptor(EGFR),nuclear factor kappa-B(NF-κB),interleukin-1β(IL-1β),IL-10,Na^(+)-K^(+)-ATPase(NKA)in serum and gastric tissues were determined by enzyme-linked immunosorbent assay,and the mRNA expressions of EGFR,NF-κBp65,IkappaBalpha(IκBα)and Zonula Occludens-1(ZO-1)in gastric tissues were determined by real-time reverse transcription polymerase chain reaction,and the efficacy was observed.Then,plasma metabolomic analysis was performed by UPLC-MS/MS to screen the specific potential biomarkers,metabolic pathways and to explore the possible mechani-sms.RESULTS 48 chemical constituents were identified.Many of them have strong pharmacological activity,the results also revealed that A.japonica significantly improved the pathological damage of gastric tissues,increased the expression levels of IL-10,IκBαrelated to anti-inflammatory factors,decreased the expression levels of IL-1β,NF-κB,NF-κBp65,related to proinflammatory factors,restored the levels of factors about EGF,EGFR,ZO-1 associated with ulcer healing and the levels of factors about NKA associated with energy metabolism.Metabolomic analysis identified 10 potential differential metabolites and enriched 7 related metabolic pathways.CONCLUSION These findings contribute to the understanding of the potential mechanism of A.japonica to improve acetic acidinduced GU,and will be of great importance for the development and clinical application of natural drugs related to A.japonica.

Effects of Different Initial Processing Methods on Atractylodin Content of Atractylodes chinensis

[Objectives]The paper was to compare the effects of different initial processing methods on atractylodin content of Atractylodes chinensis.[Methods]The atractylodin content of A.chinensis obtained by different initial processing methods was determined by HPLC.The loss rate on drying was determined by weighing.[Results]In the study of drying methods,the atractylodin content varied significantly among different thicknesses of slices,and the overall content of the product with the slice thickness of 5 mm was higher.Among different drying methods,constant temperature vacuum drying and shade drying of 5 mm slice resulted in the highest content of atractylodin.In the experiment of root impacting,root impacting twice received the best effect,and there was no significant difference in the atractylosin content of A.chinensis between drying in the sun and drying in the shade after root impacting twice(P>0.05).[Conclusions]Constant temperature vacuum drying or drying in the shade with the slice thickness of 5 mm,and root impacting twice is the best initial processing method,which leads to high atractylodin content of A.chinensis and good quality of medicinal materials.

Analysis of the Causes of Continuous Cropping Obstacles for Atractylodes macrocephala Koidz in Pingjiang County and Its Control Methods

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.

关苍术的化学成分研究

目的:研究关苍术的化学成分。方法:运用硅胶柱色谱、Sephadex LH-20柱色谱、中压液相色谱和半制备高效液相色谱等方法对关苍术中化学成分进行分离纯化,结合理化性质及MS、NMR等波谱数据对化学成分进行结构鉴定。结果:从关苍术药材中分离并鉴定了12个化合物,分别鉴定为2-[(2E)-3,7-二甲基-2,6-辛二烯基]-6-甲基-2,5-环己二烯-1,4-二酮(1)、邻苯二甲酸二丁酯(2)、邻苯二甲酸二异丁酯(3)、8,9,10-三羟基百里香酚(4)、α-菠甾醇(5)、蒲公英萜醇乙酸酯(6)、β-木香酸(7)、1,8-桉叶素(8)、8,11-十八碳二烯酸甲酯(9)、对羟基苯乙酸甲酯(10)、3-羟基-4-乙酰基苯甲酸(11)和异丁香酚甲醚(12)。结论:12个化合物均为首次从关苍术中分离得到。

Effect of Three Precursors on Accumulation of Principal Volatile Oil Constituents in Tissue Culture Plantlets of Atractylodes lancea (Thunb.) DC.

[Objective] This study was to explore the effect of three precursors on the accumulation of principal volatile oil constituents in tissue culture plantlets of Atractylodes lancea （Thunb.） DC. with the aim to provide references for the improvement of artificial cultivated A. lancea quality. [Method] Three precursors were added into the MS rooting medium for A. lancea tissue culture plantlets and the volatile oil was extracted by ultrasonication after cultured for several days. The content of atractylon, atractylol, β-eucalyptol and atractydin in the volatile oil were determined by using gas chromatography method. [Result] The addition of xylose, isoprene and tetrahydrofuran impacted the growth indicators, yield of volatile oil and relative percentage content of the four constituents of A. lancea tissue culture plantlets. In the 6 g/L xylose optimized medium, the atractylon and β-eucalyptol content reached up to 4.23% and 56.34%, respectively, 1.41% and 1.66% higher than the control; although the addition of isoprene into medium raised the atractylon content, the accumulation of total volatile oil was inhibited that it decreased by 23.67%, 31.06% and 7.10% to the control; for the tetrahydrofuran optimized medium, the content of atractylon, atractylol and atractydin all increased, and the total volatile oil content increased by 49.97% to the control when the concentration of tetrahydrofuran was 0.07 g/L. [Conclusion] The addition of xylose and tetrahydrofuran promoted the accumulation of principal constituents of the volatile oil, whereas the addition of isoprene inhibited the accumulation.

Study on Rapid Propagation Medium of Atractylodes Lances by Orthogonal Design

[Objective] The aim was to protect wild resource of Atractylodes lances and to provide technical guidance for industrialization of Atractylodes lances. [Method] The test-tube seedlings were produced from seeds of Atractylodis Lances. At the same time, the effects of 6-BA, NAA and KT on the proliferation of aseptic seedling was studied through the orthogonal test. Effect of NAA concentration on the rooting of aseptic seedling was studied through nine types of light substrate groups, which consist of peat soil, fine sand and cotton seed hull, and their effects on Atractylodes lances growth were studied on with orthogonal design. [Result] The culture medium suitable for the proliferation of the Atractylodes lances tube seedling was MS＋6-BA 1.0 mg/L＋NAA 0.4 mg/L＋KT 0,4 mg/L. And the medium suitable for rooting was 1/2MS＋NAA 0.5 mg/L. The optimal ratio of soil, riversand and cotton seed hull was 3：3：2. [Conclusion] The research selected optimum culture medium, rooting medium and ratio of substrate, which provided technical guidance for laboratorial preservation of germplasm resource of Atractylodes lances and industrialization of its seedling production.

Therapeutic potential and pharmacological activities of Atractylodes lancea (Thunb.) DC.

The rhizome of Atractylodes Iancen(A.lancea)(Thunb.) DC.(AL)is extensively used in Chinese,Thai,and Japanese traditional medicines as crude extracts/decoctions or a component in various herbal formulations.Various pharmacological activities of Al.and its major constituents have been demonstrated in ritro.ex ciro.and in animal models.Results from the toxicity studies in animal models suggest safety profile of AL,and its active constituents.Despite extensive use with positive impression in many diseases,there has not been a clinical study that can conclusively support its efficacy and safely profile in human.This review comprehensively summarizes current information on the pharmacological activities of AL and their active constituents including anticancer,anti-inflammatory,antimicrobial and antipyretic activities,as well as activities on central nervous,cardiovascular,and gastrointestinal systems.

Two New Sesquiterpenes from Atractylodes macrocehpala

Two new sesquiterpenes: beishulenolide A 1 and peroxiatractylenolide III 2 wereisolated from Atraclylodes macrocephala Koids (compositae).Their structures were elucidated onthe basis of spectral evidence, especially 2D-NMR methods and chemical conversion.

A new polyacetylene glycoside from the rhizomes of Atractylodes lancea

A new polyacetylene glycoside,（1,3Z,11E）-tridecatriene-7,9-diyne-5-hydroxyl-6-O-β-D-glucopyranoside,was isolated from the rhizomes of Atractylodes lancea（Thunb.） DC.Its structure was elucidated on the basis of spectral analysis.

Effects of Atractylodes Macrocephala on the Cytomembrane Ca^(2+)-activated K^+ Currents in Cells of Human Pregnant Myometrial Smooth Muscles

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.

Immunomodulating Activities of Polysaccharides from ZhuQin Formula and Atractylodes in Hypoimmune Mice

[Objectives] To investigate the infrared identification of ZhuQin Formula and Atractylodes polysaccharides and its effect on immune function in immunocompromised mice. [Methods] In this experiment,the structure of polysaccharides was analyzed by Fourier transform infrared spectroscopy. The experiment was divided into the polysaccharide groups of high,medium and low dose of ZhuQin,the extraction group of ZhuQin,the polysaccharide group of Atractylodes,the positive drug group,the blank group and the model group. The model of immunosuppressed mice was established by intraperitoneal injection of cyclophosphamide. The carbon clearance index,immune organ index,serum hemolysin,spleen T and B lymphocyte transformation rate were determined. [Results]The results show that the polysaccharides have obvious absorption peaks of polysaccharides; Formula extracts and polysaccharides can enhance the immune function of immunosuppressive mice at a certain dose level,and the effect of formula polysaccharide is better than that of extract and single traditional Chinese medicine polysaccharides. [Conclusions] The results suggest that the polysaccharides of ZhuQin Formula and Atractylodes may be acidic polysaccharides containing pyran ring and furan ring. ZhuQin Formula polysaccharide may play an immunomodulatory role mainly by improving the specific immunity of the organism.

关苍术醇提物乙酸乙酯部位化学成分及其抗肿瘤活性研究

目的研究关苍术的化学成分及部分化合物的抗肿瘤活性。方法使用95%乙醇水对关苍术进行提取,利用正相硅胶柱色谱、ODS柱色谱以及半制备HPLC分析方法等对其进行分离纯化,并使用HR-ESI-MS和NMR鉴定化合物的化学结构。使用人肝癌HepG-2细胞对化合物1、3~4、8~13进行抗肿瘤活性测试。结果从中共得到14个化合物,分别鉴定为7-羟基香豆素(1)、东莨菪内酯(2)、没食子酸乙酯(3)、咖啡酸甲酯(4)、4-O-咖啡酰奎宁酸甲酯(5)、5,7,4’-三羟基-6-甲氧基黄酮(6)、3,7-二羟基-4’-甲氧基黄酮(7)、1-O-阿魏酰基-(4E,6E,12E)-十四碳三烯-8,10-二炔-1,3-二醇(8)、1-O-阿魏酰基-(4E,6E,12E)-十四碳三烯-8,10-二炔-1,14-二醇(9)、(8E,15E)-十七碳-8,15-二烯-11,13-二炔酸(10)、(4E,6E,12E)-4,6,12-十四碳三烯-8,10-二炔-1-醇(11)、十七烷酸(12)、二十二烷酸(13)、蒲公英萜醇乙酸酯(14)。化合物3、4具有一定的抗肿瘤活性,IC50值分别为(68.14±26.84)、(59.80±26.40)μmol·L^(-1)。结论共得到14个化合物,其中化合物3~7、13均为首次从该药用部位中分离获得。MTT实验结果显示化合物3、4具有一定的抗肿瘤活性。

Advances in research on chemical constituents,pharmacological actions and processing of atractylodes macrocephala

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.

Control Effect of Validamycin against Seedling Blight of Atractylodes macrocephala

[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.

Seed Propagation Technique of Atractylodes lancea in Maoshan, Jiangsu

Due to over exploitation, the Atractylodes resources in such five counties and cities as Jurong, Jintan, Lishui, Liyang and Gaochun have been exhausted. This paper summarized the seed propagation technique of Atractylodes lancea in Maoshan, Jiangsu Province, aiming to provide reference for the restoration of A. lancea production in Maoshan, Jiangsu.

Research Progress of Diseases on Atractylodes lancea

According to the current situation of diseases on Atractylodes lancea , the etiology, pathogenesis, symptoms and control methods of root diseases, leaf diseases and other diseases of A. lancea are analyzed, in order to provide a reference for the diagnosis and control of diseases on A. lancea .

Study on the Mechanism of Atractylodes lancea in the Treatment of Diabetes Based on Network Pharmacology

[Objectives]To predict the mechanism of Atractylodes lancea in the treatment of diabetes by using the method of network pharmacology.[Methods]The active constituents of A.lancea were mined and their action targets were predicted by using TCMSP database,and the targets of diabetes were screened out by GeneCards,and OMIM databases.The"constituent-target-pathway-disease"network of A.lancea in the treatment of diabetes was constructed by using Cytoscape software.The target protein-related interaction network was constructed by STRING database,and the biological function annotation and pathway analysis of key targets were carried out.[Results]The 4 active constituents of A.lancea could treat diabetes by intervening in 47 targets,95 GO biological processes and 116 main biological pathways.[Conclusions]The wogonin,NSC63551,3β-acetoxy atractylone andβ-carotene in A.lancea may regulate nuclear receptor activity,transcription factor activity(directly bind to the ligand-regulated sequence-specific DNA),steroid receptor,G protein-coupled amine receptor activity,sodium-chloride transporter activity,neurotransmitter receptor activity and other pharmacological effects,by mediating AGE-RAGE pathway,IL-17 pathway,PI3K-Akt pathway,p53 pathway,etc.,so as to treat diabetes.

Quality Evaluation of Atractylodes chinensis(DC.)Koidz.in Chengde Region Based on Dual Component Analysis

[Objectives]To evaluate the quality of Atractylodes chinensis(DC.)Koidz.in Chengde region.[Methods]35 samples of A.chinensis from different growth years were collected,and a high performance liquid chromatography(HPLC)method was established for the dual components of atractylodin and atractylone,and the quality evaluation was conducted on the cultivated A.chinensis from Chengde region in terms of moisture,ash and volatile oil content.[Results]The moisture content of all samples met the regulations,and the content of volatile oil was relatively high.Among them,seven samples with atractylodin content lower than 0.3%were unqualified products(accounting for 20%),and one sample had excessive ash content(accounting for 3%).[Conclusions]The established method for the determination of the dual components of Atractylodis Rhizoma is stable,simple,fast,precise and reusable.Besides,according to the Pearson correlation analysis among the indicators,it is concluded that the atractylodin and atractylone content are significantly related to the growth period and the volatile oil content.In addition,the quality evaluation indicators of A.chinensis in Chengde region show that there are differences in the quality of Atractylodis Rhizoma,but the overall pass rate is relatively high.It is necessary to further study the reasons for the differences.