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
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
目的:基于网络药理学探讨“黄芪-白术-茯苓-当归”组方治疗糖尿病肾病(diabetic kidney disease,DKD)的作用机制。方法:通过中药系统药理学数据库与分析平台(Traditional Chinese Medicine Systems Pharmacology Database and Analysis ...目的:基于网络药理学探讨“黄芪-白术-茯苓-当归”组方治疗糖尿病肾病(diabetic kidney disease,DKD)的作用机制。方法:通过中药系统药理学数据库与分析平台(Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform,TCMSP)检索黄芪、白术、茯苓、当归的化学成分和作用靶点。借助OMIM数据库检索DKD的靶点,进而获取药物与疾病的交集靶点。采用Cytoscape 3.7.2软件绘制“药物-活性成分-靶点”网络图,并筛选关键成分。利用STRING数据库构建蛋白质-蛋白质相互作用(protein-protein interaction,PPI)网络,并筛选核心靶点。通过Metascape数据库对交集靶点进行基因本体(gene ontology,GO)和京都基因与基因组百科全书(Kyoto encyclopedia of genes and genomes,KEGG)分析。结果:“黄芪-白术-茯苓-当归”组方的活性成分44种,其中黄芪20种,白术7种,茯苓15种,当归2种。黄芪靶点413个,白术靶点20个,茯苓靶点26个,当归靶点64个。DKD靶点1024个,疾病与药物的交集靶点19个。槲皮素、刺芒柄花素、山柰酚、异鼠李素可能是关键成分。白细胞介素(interleukin)-6、IL-10、IL-1A、IL-1β、信号传导与转录激活因子1(signal transducer and activator of transcription 1,STAT1)、C-反应蛋白(C-reactive protein,CRP)等可能是核心靶点。GO分析主要涉及血管生成调节、活性氧代谢过程、细胞因子受体结合等。KEGG通路主要包括糖尿病并发症中的AGE-RAGE信号通路、MAPK信号通路、Th17细胞分化、JAK-STAT信号通路等。结论:“黄芪-白术-茯苓-当归”组方可能通过槲皮素、刺芒柄花素等活性成分,调控AGE-RAGE、MAPK等信号通路,作用于IL-6、IL-1A、IL-1β、STAT1、CRP等靶点,从而发挥治疗DKD的作用。展开更多
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.
文摘目的:基于网络药理学探讨“黄芪-白术-茯苓-当归”组方治疗糖尿病肾病(diabetic kidney disease,DKD)的作用机制。方法:通过中药系统药理学数据库与分析平台(Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform,TCMSP)检索黄芪、白术、茯苓、当归的化学成分和作用靶点。借助OMIM数据库检索DKD的靶点,进而获取药物与疾病的交集靶点。采用Cytoscape 3.7.2软件绘制“药物-活性成分-靶点”网络图,并筛选关键成分。利用STRING数据库构建蛋白质-蛋白质相互作用(protein-protein interaction,PPI)网络,并筛选核心靶点。通过Metascape数据库对交集靶点进行基因本体(gene ontology,GO)和京都基因与基因组百科全书(Kyoto encyclopedia of genes and genomes,KEGG)分析。结果:“黄芪-白术-茯苓-当归”组方的活性成分44种,其中黄芪20种,白术7种,茯苓15种,当归2种。黄芪靶点413个,白术靶点20个,茯苓靶点26个,当归靶点64个。DKD靶点1024个,疾病与药物的交集靶点19个。槲皮素、刺芒柄花素、山柰酚、异鼠李素可能是关键成分。白细胞介素(interleukin)-6、IL-10、IL-1A、IL-1β、信号传导与转录激活因子1(signal transducer and activator of transcription 1,STAT1)、C-反应蛋白(C-reactive protein,CRP)等可能是核心靶点。GO分析主要涉及血管生成调节、活性氧代谢过程、细胞因子受体结合等。KEGG通路主要包括糖尿病并发症中的AGE-RAGE信号通路、MAPK信号通路、Th17细胞分化、JAK-STAT信号通路等。结论:“黄芪-白术-茯苓-当归”组方可能通过槲皮素、刺芒柄花素等活性成分,调控AGE-RAGE、MAPK等信号通路,作用于IL-6、IL-1A、IL-1β、STAT1、CRP等靶点,从而发挥治疗DKD的作用。
