A polysaccharide named as AMP-1 was isolated from the root of Atractylodis macrocephalae Koidz, and purified by ethanol fractionation and gel filtration. The homogeneity of AMP-1 was determined by HPLC and capillary...A polysaccharide named as AMP-1 was isolated from the root of Atractylodis macrocephalae Koidz, and purified by ethanol fractionation and gel filtration. The homogeneity of AMP-1 was determined by HPLC and capillary electrophoresis that gave a single peak. AMP-1 is composed of galactose and mannose in a molar ratio of 1.0∶1.9. Its molecular weight is 3.8×10 3. The structure of glycan was elucidated by IR, 1H NMR, 13C NMR and methylation analysis, and on the basis of the results was suggested that AMP-1 contain a backbone of β-(1→2)-D-galactose residues with branches of single β-D-mannose residue being substituted at the O-6. Bioactivity assay of AMP-1 showed that it could inhibit growth of Sarcoma 180 and Lewis pulmonary carcinoma implanted in mice.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
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
文摘A polysaccharide named as AMP-1 was isolated from the root of Atractylodis macrocephalae Koidz, and purified by ethanol fractionation and gel filtration. The homogeneity of AMP-1 was determined by HPLC and capillary electrophoresis that gave a single peak. AMP-1 is composed of galactose and mannose in a molar ratio of 1.0∶1.9. Its molecular weight is 3.8×10 3. The structure of glycan was elucidated by IR, 1H NMR, 13C NMR and methylation analysis, and on the basis of the results was suggested that AMP-1 contain a backbone of β-(1→2)-D-galactose residues with branches of single β-D-mannose residue being substituted at the O-6. Bioactivity assay of AMP-1 showed that it could inhibit growth of Sarcoma 180 and Lewis pulmonary carcinoma implanted in mice.
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.
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.
文摘目的利用分子对接和网络药理学的方法预测桂枝芍药知母汤治疗类风湿关节炎的主要活性成分和作用靶点,结合中医方解配伍理论对其多成分-多靶点-多通路的作用进行分析。方法在TCMSP、TCM-Datebase@Taiwan、PubChen Compound数据库收集桂枝芍药知母汤中9味中药(桂枝、芍药、知母、甘草、麻黄、生姜、白术、防风、附子)的主要化学成分。通过DrugBank、TTD数据库查找与类风湿关节炎治疗相关的蛋白靶点,并上传到String在线数据库,构建蛋白互作网络关系。在PDB数据库下载合适的蛋白靶点晶体结构,采用Discovery studio 4.5.0软件进行化合物与靶点的分子对接,利用Cytoscape 3.6.1软件,构建药物-化合物-靶点可视化网络,阐释桂枝芍药知母汤抗类风湿关节炎的主要作用机制。结果分子对接结果显示桂枝芍药知母汤中存在316个潜在的抗关节炎活性成分,作用于26个靶点,其中MAPK1、ZADH2、P38、AKR1C2、DHODH、CA2、MMP3、MMP9、RANKL等蛋白是主要作用靶点。生物功能和通路分析提示,桂枝芍药知母汤的作用机制主要涉及骨吸收(28%)、组蛋白激酶活性(20%)、肽基酪氨酸磷酸化(20%)、前列腺素代谢过程(12%)等生物过程。作用通路主要是破骨细胞的分化(94.12%)。结论采用分子对接结合网络药理学的方法,从多靶点多途径的角度研究桂枝芍药知母汤治疗类风湿关节炎的药效物质基础及分子机制,为更好的临床用药提供参考和依据。
