Delivery of radix ophiopogonis polysaccharide via sucrose acetate isobutyrate-based in situ forming systems alone or combined with its mono-PEGylation

This work aimed to achieve long-lasting delivery of radix ophiopogonis polysaccharide (ROP) by sucrose acetate isobutyrate (SAIB)-based in situ forming systems (ISFSs) alone or combined with mono-PEGylation of ROP. When the ‘90%SAIB/10% solvent’ system was used, the mean residence time (MRT) of ROP was prolonged by 4.3 5?～?7.00 times and the initial release rate was reduced significantly. However, this system was only suitable for days-long sustained release of ROP in short-term therapy. As to the ‘SAIB/additives/solvent’ system containing mono-PEGylated ROP, the results indicated that SAIB/poly(d,l-lactide-co-glycolide) (PLGA)/N-methyl-2-pyrrolidone (NMP) was superior to SAIB/polylactic acid (PLA)/NMP and SAIB/PLA/ethanol in controlled release. Moreover, weeks- to months-long (16–60 d) smooth release of ROP could be achieved by varying the concentration (10–30%) and molecular weight (MW) of PLGA (10–50?kDa) or by employing a moderate MW of PEGylated ROP (～20 or ～30?kDa). With further increasing the conjugate MW to ～40?kDa, the contribution of drug elimination to its plasma retention seemed to surpass that of the SAIB-based system, resulting in that the system no longer had an obvious influence on the in vivo behavior of the conjugate. Besides, the results of host response confirmed that with less solvent being used, the SAIB-based systems showed a higher biocompatibility than the PLGA-based systems, suggesting that they could be freely chosen in the prevention and/or cure of chronic diseases.     

Phytochemical characterization,antioxidant potential,and health risk assessment of Radix Oryzae Glutinosae

Radix Oryzae Glutinosae (ROG) has been used as a traditional anhidrotic agent in China. Ten samples were systematically assessed based on four aspects of their chemical profiles and antioxidant activity. The former was achieved using ultraviolet-visible spectra (UV), infrared absorption spectra (IR), proton nuclear magnetic resonance spectroscopy (¹H NMR), and inductively coupled plasma-mass spectrometry (ICP-MS) fingerprints, and antioxidant activity was assessed using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay, the 2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) assay, and the ferric reducing antioxidant power (FRAP) assay. The presence of amino acids, flavonoids, organic acids, and sugars was indicated in all samples. A hierarchical cluster analysis and a canonical discriminant analysis were introduced to interpret the results of the multi-pattern fingerprint. The results of the correlations between the individual elements and between each element with the different types of metabolites displayed many interesting patterns. In vitro studies revealed that all samples displayed antioxidant activities. A pollution status examination and heavy metal evaluation of the ROG samples were performed. The human health risk assessment associated with the intake of potentially harmful elements in herbs was calculated in terms of the estimated daily intake, the target hazard quotient, and the lifetime cancer risk. The Nemerow multi-factor pollution index results suggested that all samples belonged to the serious pollution level. The results of the noncarcinogenic risk assessment study indicated that the pattern of consumption of this herb in China seems to suggest an excessive health hazard associated with some toxic elements studied. The carcinogenic risk results suggested that there is a potential risk due to As, Cr, Cd, and Ni for consumers, and these may contribute to the population cancer burden through ROG ingestion. This study provides insights into the organic medicinal constituents and the trace elements of the herb. The results will enable this herb to be used more effectively and safely.     

基于系统药理学探讨草乌改善Ⅱ型糖尿病的分子机制

目的 基于系统药理学、生物信息学、分子对接及体内外实验探讨草乌影响 2 型糖尿病(diabetes mellitus type 2, T2DM)的潜力及对 T2DM 相关症状的潜在机制。方法 利用数据库检索草乌相关化学成分、预测潜在作用靶点以及干预 相关疾病;GEO 数据库检索 T2DM 相对健康人的差异基因,与草乌作用靶点映射后置于 DAVIDavid 数据库进行生物功能 富集,利用单因素方差分析、二元 Logistic 回归分析及 ROC 曲线分析目标基因对于 T2DM 的敏感性。借助分子对接技术 分析草乌化学成分与靶蛋白的结合位置及相互作用力。通过体内外 T2DM 模型验证草乌及其化学成分对目标蛋白表达的 影响。 结果 通过数据库检索与分析得到草乌干预靶点相关疾病 44 种(P value<0.05,FDR<0.05),选取度值最高的 T2DM(Degree=22)进行分析。T2DM 相对健康人差异基因与草乌潜在作用靶点取交集得到 43 个目标基因,进行单因素方 差分析得到有显著性差异的基因共 9 个,二元 Logistic 回归分析得到 5 个有意义基因,ROC 曲线下面积 AUC>0.5 的基因 共 3 个。分子对接得到草乌化学成分(+)-Isoboldine 与蛋白 APEX1、CASP1、CBFB,Napelline 与蛋白 CBX1、EHMT2 结 合通过氢键相互作用、疏水相互作用、可电离性和静电相互作用等不同作用力结合,从而增加配体靶向作用蛋白的能力。 体内模型经草乌水提物治疗 2 周后,草乌可能通过改善周围神经病变进而缓解 T2DM 症状。并且草乌可以影响大鼠肝组织 中 APEX1、CASP1、CBFB、CBX1、EHMT2 的蛋白表达,草乌中(+)-Isoboldine 和 Napelline 化学成分对体外模型的目标蛋 白的影响与体内实验一致。结论 初步揭示草乌可作为改善 T2DM 周围神经病变的潜在治疗药物,为中蒙药研发以及挖掘 治疗 T2DM 新靶标药物奠定理论基础。     

黄芩处方的调查和分析

目的通过处方统计探讨黄芩在医疗机构门诊处方中的使用情况、用药思维和配伍规律。方法调查北京地区医疗机构门诊处方7682张,对其中含有黄芩的处方进行统计分析。结果黄芩处方占门诊处方的15．13％,其中黄芩剂量在6-15g范围的处方占88．83％,黄芩平均剂量为9．82g,黄芩处方主要用于治疗肺系、肝胆系、脾胃系、和妇科四类病证,这四类病证的处方占88．33％,临床常配伍柴胡、黄连、金银花、鱼腥草、半夏、桑白皮、白术等药物。结论黄芩临床使用广泛,配伍药物具有多样性和规律性。     

天冬中呋甾皂苷含量测定方法的建立

目的:采用E试剂比色法建立了天冬总皂苷含量测定方法.方法:用对二甲氨基苯甲醛-HCl乙醇液的发色体系,以天冬皂苷AC-9作为指标,在波长510 nm测定天冬总皂苷含量.结果:标准曲线在0.08～0.40 mg范围内线性关系良好,平均回收率为99.79%(RSD=1.05%).结论:此法可作为评价天冬总皂苷的质量标准.     

黄芪、川芎不同比例配伍对黄酮类成分提取动力学的影响

目的 研究黄芪和川芎不同比例配伍对黄酮类成分的提取动力学过程的影响。方法 建立黄酮成分(以芦丁为对照品)的含量测定方法,分别动态测定2 h内黄芪与川芎不同比例配伍(1∶1、1∶2、1∶3、1∶4、1∶5、2∶1、3∶1、4∶1、5∶1)的提取液中黄酮类成分的浓度,并根据菲克第一扩散定律,分别建立提取动力学模型,计算其提取速率常数,比较其溶出动力学差异性。结果 黄芪与川芎不同比例配伍对黄酮类成分的提取速率和浓度均有显著影响,黄酮类成分的提取动力学模型均符合一级动力学方程特征,其中黄芪∶川芎为3∶1时提取速率最快,川芎∶黄芪2∶1时提取速率最慢,川芎∶黄芪为3∶1时黄酮类成分的平衡浓度最高,黄芪∶川芎比例为5∶1时最低。结论 黄芪与川芎的不同比例配伍对黄酮类成分的提取速率和浓度有显著影响。     

基于熵权TOPSIS法和灰色关联度分析筛选桔梗最佳采收期

目的 完善桔梗药材质量评价方法,研究3年生桔梗药材不同采收期下药材质量差异,确定桔梗药材最佳采收期。方法 以桔梗药材浸出物、灰分、水分、折干率以及所含6种皂苷类活性成分含量作为质量评价的检测指标,借助数理统计学方法,对不同采收期桔梗药材之间的差异进行表征。并结合熵权法、灰色关联度分析、TOPSIS法3种数学模型对桔梗药材质量评价指标进行统计分析,获得不同采收期桔梗药材质量排名信息。结果 采收期是影响桔梗药材质量差异的重要因素,不同采收期下3年生桔梗药材质量评价指标之间差异明显。所增加的多指标检测完善了桔梗质量评价体系,增强了药材的“性-效”联系。结合质量评价模型结果显示,3年生桔梗以10月21日(霜降)前后采收的桔梗药材综合指数得分最高。结论 为保证桔梗药材质量,结合药材外观性状特征与药材物质基础综合考虑,确定以“霜降”节气前后作为3年生桔梗的最佳采收期。     

赤芍的抑菌作用及其防治慢性牙周炎的机制研究

目的 研究赤芍提取物对牙龈卟啉单胞菌(Porphyromonas gingivalis,P.g)、具核梭杆菌(Fusobacterium nucleatum,F.n)和伴放线聚集杆菌(Actinobacillus Actinomycetes,A.a)的抑菌作用,并通过网络药理学方法分析赤芍防治慢性牙周炎(chronic...     

薄层色谱指纹图谱对熟地黄质量稳定性的研究

目的：为鉴别生熟地黄及考察熟地黄饮片质量的稳定性和一致性,建立了薄层色谱指纹图谱。方法：薄层板：自制的0.25mol磷酸二氢钠缓冲盐硅胶G板;展开系统：乙酸乙酯∶丙酮∶甲酸∶水（3∶5∶1∶1）,显色：苯胺-二苯胺-磷酸溶液为显色剂,85℃加热至斑点显色清晰。结果：色谱图谱及全通道扫描结果显示,10批清蒸和10批酒炖样品间的相似程度较高,饮片质量比较均一、稳定。结论：薄层色谱方法操作简单,图谱特征明显,可比性强,是一种可以快速鉴别药材真伪及考察药材质量是否稳定、一致的有效手段。