RP—HPLC法测定瘫痿胶囊中马钱子碱和士的宁的含量

目的建立以反相高效液相色谱法测定瘫痿胶囊中马钱子碱和士的宁含量的方法。方法色谱柱为依利特C18（4．6×150mm，5μm），流动相为：0．01mol／L庚烷磺酸钠与0．02mol／L磷酸二氢钾等量混合溶液（用10％磷酸调节pH值2．8）-乙睛（79：21），流速：1．0ml／min，检测波长：260mm，柱温：30℃。结果马钱子碱进样量在0．1296～1．9440μg（r=0．99996）范围内，士的宁的进样量在0．1338—2．0070μg（r=0．99993）的范围内与峰面积积分值呈良好的线性关系。平均加样回收率马钱子碱为99．91％，RSD=1．95％，（n=6）；士的宁为99．60％，RSD=1．48％，（n=6）。结论本方法简便、快速、准确、重现性好，可用于瘫痿胶囊的质量控制。     

马钱子碱通过抑制IL-6/STAT3信号通路诱导结肠癌SW480细胞凋亡

目的:探讨马钱子碱(brucine)在体外对人结肠癌SW480细胞生长和凋亡的影响及可能的分子机制。方法:实验以人结肠癌细胞系SW480细胞为研究对象,分为空白对照组、brucine(1μmol/L)处理组、IL-6(100μg/L)处理组和brucine(1μmol/L)与IL-6(100μg/L)联用组,用CCK-8法检测细胞活力抑制率;流式细胞术Annexin V/PI双染法检测细胞凋亡;Western blot法检测凋亡相关蛋白表达。细胞免疫荧光检测相关蛋白表达定位和强度。结果:Brucine处理组和brucine与IL-6联用组都能抑制结肠癌细胞的活力,brucine浓度相同时,联用组抑制率小于brucine处理组(P0.05)。与空白对照组相比,单用brucine处理组凋亡细胞明显增多(P0.05)。与单用brucine相比,brucine与IL-6联用组凋亡细胞明显减少(P0.05)。与对照组相比,brucine能降低p-STAT3蛋白水平。与空白对照组相比,单用brucine组p-STAT3的蛋白减少,抗凋亡蛋白Bcl-2表达减少,促凋亡蛋白Bax和执行凋亡的cleaved PARP明显增多;与空白对照组相比,单用IL-6处理组的p-STAT3明显增多(P0.05);而与单用brucine相比,brucine与IL-6联合应用组的p-STAT3蛋白增多,抗凋亡蛋白Bcl-2表达增多,促凋亡蛋白Bax和执行凋亡的cleaved PARP均相对减少(P0.05)。结论:体外细胞实验中brucine可能通过调节IL-6/STAT3通路,抑制结肠癌SW480细胞中STAT3的磷酸化激活,从而发挥抗肿瘤作用。     

RP-HPLC法同时测定祛风活络丸中士的宁和马钱子碱的含量

目的:建立祛风活络丸中士的宁和马钱子碱的反相高效液相分析法,为该药质量控制提供依据.方法:采用Techsphese-C18ODS色谱柱(4.6 mm×250mm,5μm);乙腈-甲醇-0.05 mol·L-1KH2PO4溶液-三乙胺(25:19:55:1,磷酸调pH至3.5)为流动相:流速1 mL·min-1;检测波长254 nm.结果:士的宁在0.3～3.6μg(r=0.999 9)、马钱子碱在0.2～2.4μg(r=0.999 6)范围内呈良好的线性关系:士的宁回收率为97.6%,RSD=2.0%;马钱子碱回收率为101.02%,RSD=1.4%.结论:本方法准确可靠,简便灵敏,重现性好,可用于祛风活络丸中士的宁和马钱子碱的质量控制.     

Tissue distribution and pharmacokinetics of brucine niosomal gels in rats after topical and oral application

Brucine has anti-inflammatory and analgesic effects and is the main active compound of the seeds of Strychnos nux-vomica L. To study brucine niosomal gels, a reliable and rapid LC-MS/MS method was established to quantify brucine levels in rats. Tissue distribution and pharmacokinetics of brucine were investigated after topical and oral application of brucine niosomal gels to rats. The plasma concentration versus time profiles suggested that systemic exposure of brucine for oral administration of brucine niosomal gels was higher than that for topical administration, and topical administration showed a relatively sustained release. There was a considerable amount of brucine distributed in the knee joint. These results provided a strong basis for the follow-up study of this preparation.     

Determination of strychnine and brucine in rat plasma using liquid chromatography electrospray ionization mass spectrometry

A simple, sensitive and selective liquid chromatography–electrospray mass spectrometric (LC–ESI-MS) method was developed and validated for simultaneous determination of strychnine and brucine in rat plasma, using tacrine as the internal standard (IS). Sample preparation involved a liquid–liquid extraction of the analytes with n-hexane, dichloromethane and isopropanol (65:30:5, v/v/v) from 0.1 mL of plasma. Chromatographic separation was carried out on a Waters C₁₈ column using a mobile phase of methanol–20 mM ammonium formate–formic acid (32:68:0.68, v/v/v). Positive selected ion monitoring mode was used for detection of strychnine, brucine and the IS at m/z 335.2, m/z 395.2 and m/z 199.2, respectively. Linearity was obtained over the concentration range of 0.5–500 ng/mL for strychnine and 0.1–100 ng/mL for brucine. The lower limit of quantification was 0.5 ng/mL and 0.1 ng/mL for strychnine and brucine, respectively. The intra- and inter-day precision for both strychnine and brucine was less than 7.74%, and accuracy ranged from −4.38% to 2.21% at all QC levels. The method has been successfully applied to a pharmacokinetic study of processed Semen Strychni after oral administration to rats.     

HPLC法测定偏瘫康复液中士的宁和马钱子碱的含量

目的 建立偏瘫康复液中士的宁和马钱子碱的含量测定方法,为其质量控制提供参考.方法 采用高效液相色谱法,采用Diamonsil ODS C18(250 mm×4.6 mm,5μm)色谱柱,流动相为乙腈-0.1％磷酸(11:89,三乙胺调pH值为2.8),流速:1.0 mL·min-1,检测波长为260 nm,柱温为室温.结果 士的宁在28～280 μg·mL-1浓度范围内线性关系良好,平均加样回收率为97.34％,RSD为2.07％;马钱子碱在24～240 μg·mL-1浓度范围内线性关系良好,平均加样回收率为98.25％,RSD为1.95％.结论 该方法能简便、灵敏、准确的测定偏瘫康复液中士的宁和马钱子碱的含量,可用于该制剂的质量控制.     

Rituals can kill – A fatal case of brucine poisoning

In some parts of India people follow a religious ritual of drinking an herbal preparation made from the bark of the Alstonia scholaris tree (Blackboard tree) on the day of the new moon in the month of July. This tree could be easily confused with the Strychnos nux vomica tree. Brucine is the predominant alkaloid present in the bark of the Strychnos nux vomica tree. The toxicological property of brucine is similar to strychnine. Brucine is a neurotoxin. A 29-year-old male presented with a history of consumption of an herbal preparation made from the bark of the Strychnos nux vomica tree confusing it for Alstonia scholaris. Soon after, he developed convulsions and later died in hospital on the same day. The aim of this case report is to highlight the fact that people must be cautious when they follow religious rituals.     

薄层扫描法测定含马钱子中成药中士的宁和马钱子碱的含量

采用双波长薄层扫描法对马钱子散、九分散、养血祛风丸、滋阴补肾丸、伤科七味片、益髓冲剂中的士的宁和马钱子碱进行含量的测定，可以有效地控制药品质量，结果准确。     

马钱子碱中毒脑神经细胞Bcl-2和Caspase-3表达的研究

目的观察马钱子碱中毒后不同时间、不同剂量Bcl-2和Caspase-3表达的变化。方法选用20只Wistar大鼠为正常对照组,44只Wistar大鼠复制马钱子中毒模型,应用免疫组织化学和图像分析方法研究大鼠脑神经细胞马钱子中毒后Bcl-2与Caspase-3蛋白表达的变化规律。结果大鼠在马钱子中毒低、中剂量后的1~7 d不同时间段内,脑神经细胞Bcl-2与Caspase-3蛋白阳性表达细胞数均高于正常对照组,与相应的对照组比较,差异均有统计学意义(P0.05)。结论Bcl-2与Caspase-3参与了马钱子中毒的病理生理过程。