Microstructure, Content and in vitro Release of Brucine and Strychnine in Strychnos Nux-Vomica Powder with Different Particle Sizes

To explore the effect of particle size on the quality uniformity and in vitro release performance of Strychnos nux-vomica powder, seven samples of Strychnos nux-vomica powder with different particle sizes were prepared.Microstructures and particle sizes were analyzed, and high performance liquid chromatography(HPLC) was used to test the contents and in vitro release performances of brucine and strychnine in the samples. Results showed that the contents and the in vitro release rates of brucine(or strychnine) in different samples were different since there are different proportions of endosperms to epidermal cells in Strychnos nux-vomica powder with different particle sizes. Brucine and strychnine in each sample were promptly released in the first ten minutes and their cumulative release rates were higher than 70% after ten minutes. Eighty minutes later, the cumulative release rate tended to be a constant. Considering the quality uniformity and safety of Strychnos nux-vomica powder used as traditional Chinese medicine, it would be better to control the particle size of Strychnos nux-vomica powder between 100 and 140 mesh in which the maximum cumulative release rate in vitro of brucine and strychnine can be relatively low within this range.

Chemical constituents from processed seeds of Strychnos nux-vomica

Fifteen compounds were isolated from the processed seeds of Strychnos nux-vomica and were identified as follows：strychnine（1）,brucine（2）,pseudostrychnine（3）,pseudobrucine（4）,secoxyloganin（5）,caffeic acid（6）,p-hydroxybenzoic acid（7）,p-hydroxyphenylacetic acid（8）,uvaol（9）,stigmasta-7,22,25-triene-3-ol（10）,lupeol（11）,11-oxo-α-amyrin palmitate（12）,catechol（13）,maltol（14）,adenosine（15）.Compounds 5-15 were isolated from genus Strychnos for the first time.

Zebrafish model for assessing induced organ toxicity by Strychnos nux-vomica

OBJECTIVE:To assess the acute organ toxicity of Strychnos nux-vomica with zebrafish model visually.METHODS:To assess acute toxicity,we initially determined the lethal concentration after Strychnos nux-vomica treatment for 24 h.Zebrafish was treated with five concentrations Strychnos nux-≦vo LC10 for 24 h,and the effects ofmica on morphology,function of heart,central nervous system,liver,kidney and organ-specific cell death were assessed.Next,we assessed the reversibility of toxic effect.RESULTS:Strychnos nux-vomica has an effect on the different organs of zebrafish,including heart,central nervous system,liver,and kidney,and cadiotoxicity induced by Strychnos nux-vomica was reversible to some extent.CONCLUSION:Zebrafish model is suitable for confirming the toxic target organs for Chinese traditional medicine.

固相微萃取-高效液相色谱联用测定马钱子中士的宁、马钱子碱含量

目的:建立一种固相微萃取-高效液相色谱联用测定马钱子中士的宁、马钱子碱含量的新方法。方法:自制毛细管整体柱,用于固相微萃取-高效液相色谱联用在线测定马钱子中士的宁和马钱子碱含量。色谱柱为Hypersil ODS柱(150 mm×4.6 mm,5μm);以乙腈-0.01 mol·L^(-1)庚烷磺酸钠与0.02 mol·L^(-1)磷酸二氢钾等量混合溶液(用10%磷酸调节p H至2.8)(21∶79)为流动相;检测波长为260 nm,进样量为20μl,柱温为25℃。结果:士的宁在1.2~90.0μg·ml^(-1)(r=0.999 8)范围内,马钱子碱在1.0~75.0μg·ml^(-1)(r=0.999 6)范围内线性关系良好;平均回收率分别为100.05%(RSD=0.58%)、99.98%(RSD=0.27%)(n=6)。结论:该方法准确、高效,适用于马钱子中士的宁、马钱子碱含量的分析。

基于DNA条形码—产地—形态分析联用的巴西马钱属植物药QUINA基原鉴定研究

目的通过DNA条形码—产地—形态分析联用的方法对巴西马钱属植物药QUINA进行基原鉴定研究,为这种药材的开发利用提供依据。方法通过提取样品DNA、PCR扩增及双向测序,获得样品的内转录间隔区(internal transcribed spacer,ITS)序列,利用NCBI数据库中的BLAST功能计算相似度,对其基原进行DNA条形码鉴定;根据其产地信息对DNA条形码鉴定结果进行筛选和分析;依据其形态特征验证鉴定结果。结果本次收集的植物类药材QUINA来源于马钱科马钱属植物Strychnos pseudo quina A.St.-Hil.的根皮。结论 DNA条形码—产地—形态三者联用的方法可弥补单一鉴定方法的不足,能够快速、准确的对未知样品进行基原鉴定。

马钱子总碱脂质液晶纳米粒镇痛凝胶的研制

目的优化马钱子总碱脂质液晶纳米粒镇痛凝胶(TAB-LLCN-Gel)的制备工艺,并考察其体外渗透动力学规律,以期提高马钱子总碱(TAB)的载药量和改善其经皮渗透性能。方法采用硫酸铵主动载药技术制备马钱子脂质液晶纳米粒(TAB-LLCN),以马钱子碱含量为考察指标,单因素分析确定响应点,正交设计L_(9)(3^(4))优化制备工艺;利用Franz扩散池,通过测定24 h单位面积累积释药量(Q_(24))和皮肤滞留量(Q_(s24)),比较TAB-LLCN-Gel和马钱子凝胶(TAB-Gel)的体外药动学的差异。结果载药量为100μg/g、氮酮浓度为30 mg/mL、氮酮∶丙二醇∶桉叶油的比例为2∶2∶1时为最佳处方方案。药动学结果显示,24 h内TAB-LLCN-Gel中马钱子碱中Q_(24)和Q_(s24)均高于TAB-Gel。结论最优处方工艺制备的TAB-LLCN-Gel制剂表征稳定,质量可控。透皮吸收和缓释作用均优于TAB-Gel,具有良好的开发前景。

马钱子总碱脂质液晶纳米粒的制备及工艺优化

乙醇注入结合硫酸铵主动载药技术制备马钱子总碱脂质液晶纳米粒(LLCN)。在筛选并确定脂质体制备方法的基础上,选择磷脂-胆固醇比、脂-药比、硫酸铵浓度、乙醇的体积为影响因素,以LLCN包封率为考察指标,单因素分析确定响应值,正交设计L_(9)(3^(4))优化处方参数,电镜检测LLCD的粒径、表面电荷,分析其稳定性。实验得出的最佳工艺参数为:磷脂-胆固醇比6:1、脂-药比为10:1、硫酸铵浓度0.2 moL/L、乙醇的体积12 mL/100 g, LLCN的表证和稳定性均符合制剂标准。

Effect of Baizhu(Rhizoma Atractylodis Macrocephalae)extract on intestinal absorption of brucine and strychnine in vitro and in situ

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.