CBN中葛根素、人参皂甙Rg1在正常和脑缺血再灌大鼠体内药代动力学比较

目的:探讨CBN中葛根素和人参皂甙Rg1在正常和脑缺血再灌大鼠体内的药代动力学过程。方法:脑缺血再灌组大鼠结扎双侧颈总动脉不完全脑缺血30分钟,复灌同时股静脉注射100mg·Kg-1药物。正常组注射等剂量药物。HPLC法测定给药后不同时间点血浆样品中葛根素和人参皂甙Rg1的含量,并作动力学计算。结果:CBN中葛根素在正常大鼠体内为一室模型,半衰期是17.8min;在脑缺血再灌大鼠体内为二室模型,分布和消除半衰期分别是8.0min和38.4min;药时曲线下面积(AUC,mg·L-1·min),表观分布容积(Vdss·L·kg-1),平均驻留时间(MRTmin)正常组分别为:744,4.18,26.0;脑缺血再灌组分别为:3015,1.39,40.0。人参皂甙Rg1在正常大鼠和脑缺血再灌大鼠体内为二室模型,分布和消除相半衰期分别为8.2,2,700.8min;18.6,4297min。药时曲线下面积(AUC,mg·L-1·min),表观分布容积(Vdss·L·kg-1),平均驻留时间(MRTmin)正常组分别为:531.5,7.05,164.7;脑缺血再灌组分别为:1678,2.39,73.3。结论:静脉注射CBN后,葛根素和人参皂甙Rg1在缺血再灌大鼠体内的消除时间较在正常大鼠体内延长。     

当前中药新药研制中药理应用基础研究的几个命题及其对策

本文就中药新药研制中有关药理学应用基础研究的几个命题进行了分析探讨。     

Determination of Polysaccharide in Radix pseudostellariae Extract by Size-Exclusion High-Performance Liquid Chromatography

A simple size-exclusion high-performance liquid chromatographic method was developed for rapid molecular mass screening to determine the average molecular mass, polydispersity, and quantity of Taizishen polysaccharides extract. The screening used a TOSOH TSK-GEL G3000SW high-performance liquid chromatographic column with 0.1 mol/L NaNO3 buffer as the mobile phase and refractive index detec- tor. The molecular mass calibration curve was linear for polysaccharide standards from 10 to 100 kDa with a correlation coefficient of 0.9991. The method can be used to analyze the quantity, average molecular mass, and polydispersity of polysaccharides. In addition, the screening method is suitable for quality control of polysaccharide preparations in Chinese medicines and pharmaceutical products.     

脑血管药理学与中药新药研究

目的:探讨脑血管药理学研究的必要性,及其中药在此方面的可能的优势.方法:通过对文献分析和我们研究体会,对此进行探讨.结果与结论:随着脑血管病发病率的日渐升高,对该类疾病的进行专门研究也为学术界所重视.脑血管病由于其解剖和病生理学独特性而不完全同于心血管病和神经系统疾病,它既具有心血管病的一般特性,又更具复杂性.目前针对性较强的脑血管疾病的药物不多,很大程度上与脑血管药理学研究的进展程度有关.药以其多成分多靶点作用的特点,将在脑血管病治疗扮演重要角色.     

对中药药效评价的方法学探讨

目的：对中药药效评价的方法学做一探讨。方法：通过相关文献和我们的研究工作,对中药药效评价的方法做一分析和建立。结果和结论：针对中药药效作用的特点,在总结了文献中的“水闸门”法、“总分法”的基础上,提出了“加和法”。并给出了相应的公式（1） （2）（3）     

Characteristics of Baicalin Synergy with Penicillin or Notopterygium Ethanol Extracts Against Staphylococcus aureus

Introduction Staphylococcus aureus (S. aureus) resistance to most once powerful β-lactame antibiotics is now a severe problem world wide, so agents are urgently needed to reduce or moderate resistance to existing antibiotics. Traditional medicinal herbs …     

Antioxidant Activity In Vitro of Three Constituents from Caesalpinia sappan L

Antioxidant activities of the 95% ethanol extract from Caesalpinia sappan heartwood （ECS）, protosappanin A, protosappanin B, and brazilein were studied in vitro. The inhibition of the formation of malondialdehyde （MDA） and the scavenging of superoxide anions, hydrogen peroxide, and hydroxyl radicals were assayed. The experimental results show that all four substances had antioxidant activity in vitro but their capabilities differed for the different indicators. ECS, protosappanin A, and protosappanin B show more inhibition of MDA and scavenging of hydrogen peroxide, while brazilein shows more scavenging of hydroxyl radicals. All the samples show little scavenging of superoxide anions.     

Different Kinetics of Puerarin in Plasma of Normal and Depressed Rats After Oral Administration of Chinese Medicine TZ18

The objective of this study is to quantify the puerarin in rat plasma following oral administration of TZ18 and compare the pharmacokinetics characteristics of puerarin in normal rats with that in depression model rats. A high performance liquid chromatography method was used to quantify the puerarin due to its good selectivity and linearity (coefficient correlation, r2 = 0.9991) within the tested range (0.028-0.889 μg·mL-1). Intra- and inter-day precision coefficients of variation and accuracy bias were acceptable (Maximum coeffi- cient of variation was 5.74% for intra-day and 3.09% for inter-day) over the entire range. The recoveries were found to be 98.3%, 101.4%, and 103.4% for concentrations of 0.028, 0.222, and 0.444 μg·mL-1, re- spectively. The concentration-time curves for both normal rats and depression model rats were fit to a two- compartment model with the first order absorption. The results show significant differences in the main phar- macokinetic parameters of peak time, peak concentration, and the area under the concentration-time curve between the two kinds of rats.     

Cerebral Ischemia Reperfusion Exacerbates and Pueraria Flavonoids Attenuate Depressive Responses to Stress in Mice

Previous studies have shown that mice experiencing cerebral ischemia reperfusion （CIR） and stress can serve as a model of post stroke depression （PSD）. The present study verified the acute antidepressant effects of radix puerariae extract （PE） on PSD mice through behavior and gene expression experiments. CIR was found to reduce the sucrose consumption and tyrosine hydroxylase （TH） gene expression. PE administration after CIR surgery was observed to significantly enhance the mRNA expression of TH in the hippocampus compared with the PSD group on Day 0 and Day 3 postsurgery. These findings indicate that PE contributes to the amelioration of behavior response in PSD mice, which is closely related with the protective effects of catecholamine synthesize against CIR brain damage.     

Long-Term Exposure to High Corticosterone Levels Inducing a Decrease of Adenylate Kinase 1 Activity

Corticosterone, a principal glucocorticoid synthesized in the rodent adrenal cortex, can be cumulatively toxic to hippocampal neurons, the cause of which is not known. The present study determined whether the cytosol adenylate kinase (AK) system was involved in the neuronal damage induced by long-term exposure to high corticosterone levels. We investigated the effects of long-term exposure to high corticosterone levels on AK1 activity, AK1 mRNA expression, and energy levels in cultured hippocampal neurons. The results show that long-term exposure to high corticosterone levels induces a reduction of the cultured hippocampal neuron viability, significantly reduces energy levels, and causes a time-dependant reduction of the AK1 activity. These findings indicate that changes in the AK system might be the mechanism underlying neuronal damage induced by long-term exposure to high corticosterone levels.