一测多评法测定复方人参片中的8种苷类成分

目的 建立一测多评法（quantitative analysis single-marker,QAMS）测定复方人参片中8种苷类成分的含量。方法 采用Agilent XDB-C₁₈色谱柱（4.6 mm×250 mm,5 μm）,流动相水（A）-乙腈（B）,梯度洗脱;体积流量1.0 mL·min^-1;检测波长203 nm;柱温：25℃。以人参皂苷Rb₁为内标,计算人参皂苷Rg₁、人参皂苷Re、淫羊藿苷、人参皂苷Rc、人参皂苷Rb₂、人参皂苷Rb₃、人参皂苷Rd的相对校正因子,测定其含量。结果 8种成分在各自范围内线性关系良好（r ≥ 0.999 0）,加样回收率为95.6%~104.4%,RSD为1.22%~2.73%,QAMS测定结果与外标法测定结果无显著性差异。结论 该法准确度、灵敏度高、专属性好、操作简单、重复性好。     

雷公藤多苷片对高脂小鼠血脂的影响

目的 研究雷公藤多苷片对高脂小鼠血脂的影响。方法 采用高血脂小鼠模型,通过小鼠尾静脉注射不同剂量（0.5,1.0,1.5 mg·kg^-1·d^-1）雷公藤多苷,测定不同时间段小鼠体质量和血清总胆固醇（total cholesterol,TC）、甘油三酯（totaltriglyceride,TG）、高密度脂蛋白胆固醇（high density lipoprotein cholesterol,HDL-C）、低密度脂蛋白胆固醇（low densitylipoprotein cholesterol,LDL-C）的含量及卵磷脂胆固醇酰基转移酶（lecithin cholesterol acyltransferase,LCAT）、肝脂酶（hepatic lipase,HL）和脂蛋白脂酶（lipoprotein lipase,LPL）的活性,研究雷公藤多苷对小鼠体质量、血脂代谢、动脉粥样硬化指数、肝脏LCAT水平等的影响。结果 给予高脂饲料后小鼠体质量和血脂显著升高（P<0.01）,动脉粥样硬化指数显著升高（P<0.01）,抗动脉粥样硬化指数显著下降（P<0.01）。注射雷公藤多苷能显著降低高血脂模型小鼠血清TC、TG和LDL-C,同时显著降低高脂饮食所导致的动脉粥样硬化指数升高。此外,雷公藤多苷片能显著提高血清LCAT水平和HL、LPL的活性。结论 雷公藤多苷片具有一定的降血脂功能,并能有效降低动脉粥样硬化的发生几率。     

Therapeutic drug monitoring of digoxin–20 years of experience

Background

Digoxin is the oldest drug used in the pharmacotherapy of heart failure (HF). However, digoxin remains an important therapeutic option for patients with persistent symptoms of HF occurring despite the implementation of standard pharmacotherapy. Digoxin concentration serum (SCD) should equal 1–2 ng/ml. The aim of our study was to measure of SCD among the hospitalized patients as well as to determine the selected factors influencing the concentration of the digoxin in the blood.

Targeted delivery of garcinia glycosides by reconstituted high-density lipoprotein nano-complexes

Scavenger receptor class B type 1 (SR-B1) is over-expressed in tumour cells where it mediates the uptake of drug payload of reconstituted high density lipoprotein (rHDL) via the process of reverse cholesterol transport. In this study, rHDL was prepared to determine its function as a drug delivery carrier for targeting hepatocellular carcinoma by incorporating the anti-tumour drug garcinia glycosides (GG) into rHDL to yield rHDL/GG nano-complexes. Structural analysis indicated that the rHDL/GG nano-complex was similar to HDL in size. HepG2 cells treated with fluorescent-labelled rHDL/GG exhibited a time-dependent increase in cell death. Further experiment in which HepG2 cells were treated with rHDL/GG plus plasma-derived HDL showed reduction in cell death compared to treatment with rHDL/GG alone, suggesting that plasma-derived HDL compete with rHDL/GG for binding to the SR-B1 on the cell. We concluded that rHDL could not only incorporate GG but could also serve as a carrier, targeting the drug to HepG2 cells via SR-B1.     

雷公藤多苷临床应用及不良反应的研究进展

雷公藤多苷具有较强的抗炎、免疫调节等作用,广泛应用于自身免疫性疾病,如类风湿关节炎、难治性肾病综合征、系统性红斑狼疮、糖尿病肾病、狼疮性肾炎和干燥综合征等。雷公藤多苷的疗效显著,但不良反应发生率也较高,主要对消化道、肝脏、肾脏、生殖系统、皮肤和血液系统等引起毒副作用,影响了在临床的广泛运用,本文对近年来雷公藤多苷的临床应用和不良反应及其防治进行综述,以期为临床合理应用提供参考。     

高效液相色谱法测定银杏叶及相关产品中总黄酮醇苷含量

目的:为银杏叶及相关产品中总黄酮醇苷含量测定建立统一的方法。方法:取适量样品加甲醇-25%盐酸溶液(4∶1)混合液25 ml,加热回流30 min,放冷,转移至50 ml容量瓶中,并加甲醇至刻度,摇匀,过0.45μm的滤膜,滤液进高效液相色谱分析。结果:总黄酮醇苷的三种成分线性关系良好,槲皮素、山柰素最低检出限为0.3μg,异鼠李素最低检出限为0.4μg,总黄酮醇苷最低检出限为2.51μg。结论:该方法操作简单,结果准确可靠。     

槲皮素及其糖苷衍生物在Caco-2单层细胞上的吸收特征

目的探讨槲皮素及其糖苷衍生物在人小肠吸收模型Caco-2细胞单层上的吸收特征。方法采用Caco-2单层细胞模型,研究槲皮素、槲皮苷、异槲皮苷的肠道吸收特征,以LC-MS法测定槲皮素、槲皮苷、异槲皮苷、异鼠李亭。结果槲皮素及其糖苷衍生物孵育30～150min后,均能在透过侧检测到槲皮素、槲皮苷和异槲皮苷以及槲皮素的甲基化代谢产物之一异鼠李亭;透过的槲皮素及其代谢产物异鼠李亭含量在150min孵育时间内呈先升后降的趋势特征;而槲皮苷和异槲皮苷的透过量则随孵育时间呈持续升高的趋势,在孵育后期可检测到微量异鼠李亭。结论槲皮素、槲皮苷和异槲皮苷可以完整的分子形式被Caco-2细胞单层吸收,其吸收特征有显著差异,并在吸收过程中伴有广泛的代谢转化。[营养学报,2012,34(4):358-361,367]     

雷公藤多甙联合泼尼松治疗成人紫癜性肾炎

目的探讨雷公藤多甙联合泼尼松治疗成人过敏性紫癜性肾炎(HSPN)的效果和安全性。方法选取60例明确诊断为HSPN的成人患者,随机分2组,观察组30例,采用雷公藤多甙联合泼尼松治疗,对照组常规激素治疗。治疗6个月观察疗效,追踪24h尿蛋白定量,血白蛋白等指标。也记录不良反应。结果治疗6个月后观察组尿蛋白较治疗前明显下降,差异有统计学意义(P<0.05)。两组治疗后比较差异有统计学意义(P<0.05)。治疗6个月后观察组血白蛋白较治疗前明显升高(P<0.05)。两组治疗后比较差异有统计学意义(P<0.05)。治疗组总有效率明显高于对照组(P<0.05)。两组未见严重不良反应发生。结论雷公藤多苷联合泼尼松治疗HSPN可有效降低尿蛋白,延缓紫癜性肾炎发展,疗效明显且安全可靠。     

Antiinflammatory activities of Hungarian Stachys species and their iridoids

The antiinflammatory activities of aqueous extracts prepared from the aerial parts of ten Hungarian Stachys species were investigated in vivo in the carrageenan-induced paw oedema test after intraperitoneal and oral administration to rats. Some of the extracts were found to display significant antiphlogistic effects when administered intraperitoneally and orally; in particular, the extracts of S. alpina, S. germanica, S. officinalis and S. recta demonstrated high activity following intraperitoneal administration. At the same dose of 5.0 mg/kg, these extracts exhibited similar or greater potency than that of the positive control diclofenac-Na. The main iridoids present in the investigated extracts, ajugoside, aucubin, acetylharpagide, harpagide and harpagoside, were also assayed in the same test, and high dose-dependent antiphlogistic effects were recorded for aucubin and harpagoside. These results led to the conclusion that most probably iridoids are responsible for the antiinflammatory effect of Stachys species, but other active constituents or their synergism must also be implicated in the antiinflammatory effect.