Angelica sinensis polysaccharide（ASP） was extracted from Angelica sinensis by boiling water. An Angelica sinensis polysaccharide-iron complex（APC） was prepared under the alkaline condition by adding a ferric chlor...Angelica sinensis polysaccharide（ASP） was extracted from Angelica sinensis by boiling water. An Angelica sinensis polysaccharide-iron complex（APC） was prepared under the alkaline condition by adding a ferric chloride solution to the ASP solution. Then some identifiable properties of the complex were studied. The content of iron（ Ⅲ ） in the complex was determined with iodometry. The thermal property, the microscopic structure, the spectral characteristics, and N, C, H contents of the complex were examined by a variety of techniques including DSC, TEM, IR, NMR, and elemental analysis. The content of iron（ Ⅲ ） in the complex ranges from 10% to 40%. The DSC result shows that the melting point of the complex is about 450 ℃. The TEM result shows that the complex has an iron（ Ⅲ ） core（β-FeOOH core） linked by hydroxy and oxy bridges, with the polysaccharide chains attached to the surface of the core. The IR and NMR results also show that there is a β-FeOOH core in the complex. The elemental analysis shows that the contents of N, C, H in the complex are, respectively, lower than those of N, C, H in ASP. All our studies indicate that the APC consists of a β-FeOOH core surrounded by ASP.展开更多
Objective： To investigate the therapeutic effects of Angelica sinensis polysaccharideiron complex （APIC） on rats with iron deficiency anemia （IDA）. Methods： The IDA rat model was established by adopting low-iron...Objective： To investigate the therapeutic effects of Angelica sinensis polysaccharideiron complex （APIC） on rats with iron deficiency anemia （IDA）. Methods： The IDA rat model was established by adopting low-iron forage with a small amount of regular bloodletting. The rats were randomly divided into a model group, three AIPC groups （high, middle, and low dosage）, an Angelica sinensis polysaccharide （ASP） group, a mixture group （ASP＋FeCl3） and a positive control group （Niferex）. Changes in hemoglobin （Hb）, red blood cell count （RBC）, hematocrit （HCT） and iron content of whole blood were observed. Results： There was a significant difference before and after administration in all treated groups and all indices were restored to near-normal levels in the APIC groups and the positive control group. There was a significant difference among the changes of the indices in all the APIC groups and those of the model group but not between those of the APIC groups and the positive control group. However, the recovery of the indices in the APIC groups was superior to that in the positive control group. Conclusion： APIC not only has a superior therapeutic effect on IDA, but also has the effect of the ASP on supplementing blood and activating blood circulation. Hence, it may be used as a new iron-supplementing agent with a double therapeutic efficacy on blood supplementation for the treatment of IDA.展开更多
目的制备当归多糖铁(Angelica sinensis Polysaccharide Iron Complex)胃内漂浮缓释胶囊,并对其体外释放度进行研究。方法以胶囊的漂浮性能和体外释放度为评价指标,对3种不同处方所制得的胶囊进行比较,筛选出最佳处方,并对此胃内漂浮缓...目的制备当归多糖铁(Angelica sinensis Polysaccharide Iron Complex)胃内漂浮缓释胶囊,并对其体外释放度进行研究。方法以胶囊的漂浮性能和体外释放度为评价指标,对3种不同处方所制得的胶囊进行比较,筛选出最佳处方,并对此胃内漂浮缓释胶囊进行质量控制研究。结果其体外持续漂浮时间超过12h,8h释药达90%以上,体外释药符合Higuchui方程,Q=0.416t1/2-0.2717(r=0.9981)。结论当归多糖铁胃内漂浮缓释胶囊具有良好的漂浮性能和理想的释放度。展开更多
当归具有良好的活血作用,但目前对其发挥“活血”功效的现代科学原理缺乏系统研究,限制了其现代化开发。该研究采用基于结构相似性的靶点反向预测、复杂网络分析、分子对接、结合自由能计算、聚类分析、ADMET计算等计算机辅助药物设计...当归具有良好的活血作用,但目前对其发挥“活血”功效的现代科学原理缺乏系统研究,限制了其现代化开发。该研究采用基于结构相似性的靶点反向预测、复杂网络分析、分子对接、结合自由能计算、聚类分析、ADMET计算等计算机辅助药物设计方法结合体外酶活性测定实验系统探讨了当归发挥活血作用的成分及作用机制。靶点反向预测以及复杂网络分析结果显示当归抗凝血的潜在作用靶点有40个。GO(Gene Ontology)和KEGG(Kyoto Encyclopedia of Genes and Genomes)富集分析表明预测靶点可能通过作用于补体与凝血级联信号通路发挥抗凝血作用。其中,凝血级联反应和血栓形成中的关键酶THR(thrombin)和FXa(coagulation factor Xa)是治疗血栓栓塞性疾病的药物靶点。全成分分子对接以及聚类分析显示当归针对FXa具有更好的选择性。结合自由能打分值筛选出8个潜在活性成分进行体外酶活实验,结果显示8个化合物分别对THR和FXa具有不同程度的抑制作用,且对FXa活性的抑制作用比对THR更强。对8个活性化合物进行药效团模型构建,得到药效特征AAHH,其中A为氢键受体,H为疏水中心。ADMET计算表明8个活性化合物都具有良好的药动学性质,且安全性较高。该研究以靶点反向预测、复杂网络分析、分子对接及结合自由能计算、体外抗凝活性、分子与靶点的空间结合构象、药效团模型构建及ADMET参数计算为依据,从大数据层面初步阐明了当归活血作用的物质基础及分子机制,并对活性成分进行了药理、毒理计算,首次从全成分计算结合酶活实验揭示了当归对不同凝血蛋白具有明显的选择性和针对性,反映出不同中药的独特功效具有其生物学基础。该研究可为当归的精准用药及其活血成分的现代化开发提供线索。展开更多
文摘Angelica sinensis polysaccharide（ASP） was extracted from Angelica sinensis by boiling water. An Angelica sinensis polysaccharide-iron complex（APC） was prepared under the alkaline condition by adding a ferric chloride solution to the ASP solution. Then some identifiable properties of the complex were studied. The content of iron（ Ⅲ ） in the complex was determined with iodometry. The thermal property, the microscopic structure, the spectral characteristics, and N, C, H contents of the complex were examined by a variety of techniques including DSC, TEM, IR, NMR, and elemental analysis. The content of iron（ Ⅲ ） in the complex ranges from 10% to 40%. The DSC result shows that the melting point of the complex is about 450 ℃. The TEM result shows that the complex has an iron（ Ⅲ ） core（β-FeOOH core） linked by hydroxy and oxy bridges, with the polysaccharide chains attached to the surface of the core. The IR and NMR results also show that there is a β-FeOOH core in the complex. The elemental analysis shows that the contents of N, C, H in the complex are, respectively, lower than those of N, C, H in ASP. All our studies indicate that the APC consists of a β-FeOOH core surrounded by ASP.
基金Supported by the Foundation of Science and Technology Department of Hubei Province(No.2005AA301C04)
文摘Objective： To investigate the therapeutic effects of Angelica sinensis polysaccharideiron complex （APIC） on rats with iron deficiency anemia （IDA）. Methods： The IDA rat model was established by adopting low-iron forage with a small amount of regular bloodletting. The rats were randomly divided into a model group, three AIPC groups （high, middle, and low dosage）, an Angelica sinensis polysaccharide （ASP） group, a mixture group （ASP＋FeCl3） and a positive control group （Niferex）. Changes in hemoglobin （Hb）, red blood cell count （RBC）, hematocrit （HCT） and iron content of whole blood were observed. Results： There was a significant difference before and after administration in all treated groups and all indices were restored to near-normal levels in the APIC groups and the positive control group. There was a significant difference among the changes of the indices in all the APIC groups and those of the model group but not between those of the APIC groups and the positive control group. However, the recovery of the indices in the APIC groups was superior to that in the positive control group. Conclusion： APIC not only has a superior therapeutic effect on IDA, but also has the effect of the ASP on supplementing blood and activating blood circulation. Hence, it may be used as a new iron-supplementing agent with a double therapeutic efficacy on blood supplementation for the treatment of IDA.
文摘目的制备当归多糖铁(Angelica sinensis Polysaccharide Iron Complex)胃内漂浮缓释胶囊,并对其体外释放度进行研究。方法以胶囊的漂浮性能和体外释放度为评价指标,对3种不同处方所制得的胶囊进行比较,筛选出最佳处方,并对此胃内漂浮缓释胶囊进行质量控制研究。结果其体外持续漂浮时间超过12h,8h释药达90%以上,体外释药符合Higuchui方程,Q=0.416t1/2-0.2717(r=0.9981)。结论当归多糖铁胃内漂浮缓释胶囊具有良好的漂浮性能和理想的释放度。
文摘当归具有良好的活血作用,但目前对其发挥“活血”功效的现代科学原理缺乏系统研究,限制了其现代化开发。该研究采用基于结构相似性的靶点反向预测、复杂网络分析、分子对接、结合自由能计算、聚类分析、ADMET计算等计算机辅助药物设计方法结合体外酶活性测定实验系统探讨了当归发挥活血作用的成分及作用机制。靶点反向预测以及复杂网络分析结果显示当归抗凝血的潜在作用靶点有40个。GO(Gene Ontology)和KEGG(Kyoto Encyclopedia of Genes and Genomes)富集分析表明预测靶点可能通过作用于补体与凝血级联信号通路发挥抗凝血作用。其中,凝血级联反应和血栓形成中的关键酶THR(thrombin)和FXa(coagulation factor Xa)是治疗血栓栓塞性疾病的药物靶点。全成分分子对接以及聚类分析显示当归针对FXa具有更好的选择性。结合自由能打分值筛选出8个潜在活性成分进行体外酶活实验,结果显示8个化合物分别对THR和FXa具有不同程度的抑制作用,且对FXa活性的抑制作用比对THR更强。对8个活性化合物进行药效团模型构建,得到药效特征AAHH,其中A为氢键受体,H为疏水中心。ADMET计算表明8个活性化合物都具有良好的药动学性质,且安全性较高。该研究以靶点反向预测、复杂网络分析、分子对接及结合自由能计算、体外抗凝活性、分子与靶点的空间结合构象、药效团模型构建及ADMET参数计算为依据,从大数据层面初步阐明了当归活血作用的物质基础及分子机制,并对活性成分进行了药理、毒理计算,首次从全成分计算结合酶活实验揭示了当归对不同凝血蛋白具有明显的选择性和针对性,反映出不同中药的独特功效具有其生物学基础。该研究可为当归的精准用药及其活血成分的现代化开发提供线索。
