关闭
 
读者在线:用户名 密码
首页 期刊简介 投稿须知 期刊目录 专家风采 编委会 特邀顾问 联系我们 移动出版
  1. 1
  2. 2
  3. 3
  4. 4
  5. 5



刊物信息

期刊名称:药物分析杂志
主管单位:中国科学技术协会
主办单位:中国药学会
承办:中国食品药品检定研究院
主编:金少鸿
地址:北京天坛西里2号
邮政编码:100050
电话:010-67012819,67058427
电子邮箱:ywfx@nicpbp.org.cn
国际标准刊号:ISSN 0254-1793
国内统一刊号:CN 11-2224/R
邮发代号:2-237
 

访问统计
您是第  4 2 9 8 4 4 6 位浏览者
您当前的位置:首页 >> 正文

GC-MS测定莪术中β-榄香烯的血药浓度及大鼠体内药代动力学研究

Determination of plasma concentration of β-elemene in Curcuma zedoaria by GC-MS and its pharmacokinetic study in rats*

作者: 李婧, 刘文静 
作者(英文):
分类号:R917
出版年·卷·期(页码):2019,39 (5):846-851
DOI: 10.16155/j.0254-1793.2017.01.01
-----摘要:-------------------------------------------------------------------------------------------

目的:建立快速灵敏的气质联用(GC-MS)法测定莪术中β-榄香烯在大鼠血浆中血药浓度,并研究β-榄香烯在大鼠体内的药代动力学特征。方法:血浆样品的处理采用正己烷液-液萃取方法,萘为内标。色谱柱:DB-5毛细管柱(30 m×0.25 mm,0.25 μm);程序升温:初始60℃,保持1 min,再以30℃·min-1的速度升温至160℃,保持3 min,再以10℃·min-1的速度升温至200℃,保持2 min。采用电子轰击离子源及选择离子扫描模式(SIM);选择监测离子:β-榄香烯m/z 93,内标m/z 128。按β-榄香烯10 mg·kg-1灌胃给药后,测定大鼠血浆中β-榄香烯的浓度,并用DAS 2.0软件计算药代动力学参数。结果:血浆中β-榄香烯质量浓度在0.05~200.0 μg·mL-1浓度范围内线性关系良好(r2=0.999 1),定量下限为0.05 μg·mL-1;低、中、高3个浓度准确度、日内及日间精密度均小于5%;提取回收率分别为91.7%、105.1%、108.8%;低、中、高3个浓度血浆样品在室温放置12 h,4℃冰箱中放置24 h及反复冻融4次后均能保持稳定。大鼠灌胃莪术提取液后β-榄香烯药-时曲线符合二室模型;主要药代学参数:AUC(0-t为(9.83±1.07)μg·L-1·h,t1/2α为(0.47±0.05)h,t1/2β为(1.82±3.11)h,Tmax为(2.06±0.37)h,Cmax为(2.61±0.17)μg·mL-1结论:该方法简便、准确,专属性强,适用于莪术中β-榄香烯在大鼠体内的药代动力学研究。

-----英文摘要:---------------------------------------------------------------------------------------

Objective:To establish a rapid, sensitive method for the determination of plasma concentration of β-elemene in Curcuma zedoaria using capillary gas chromatography coupled to mass spectrometry (GC-MS) and to study the pharmacokinetics in rats.Methods:The plasma sample was treated with a liquid-liquid extraction method of n-hexane, and naphthalene was used as an internal standard (IS).The determination was performed on DB-5 column (30 m×0.25 mm, 0.25 μm).The initial column temperature was 60℃, maintained for 1 min, then raised to 160℃ at a rate of 30℃·min-1, maintained for 3 min, and finally increased to 200℃ at a rate of 10℃·min-1 and maintained for 3 min.EI and single ion monitoring pattern (SIM) were used for ion scanning with m/z 93 (β-elemene) and m/z 128 (IS).After administration of β-elemene 10 mg·kg-1 by oral gavage, the concentration of β-elemene in rat plasma was determined, and the pharmacokinetic parameters were calculated by DAS 2.0 software.Results:There was excellent linearity of the plasma concentration of β-elemene in the range of 0.05-200.0 μg·mL-1 (r2=0.999 1), and the lowest limit of quantification was 0.05 μg·mL-1.The accuracy, intra-day and inter-day precisions of low, medium and high concentrations were less than 5% and the recovery rates were 91.7%, 105.1% and 108.8%, respectively.The plasma samples of low, medium and high concentrations were kept at room temperature for 12 h, and were stable after being placed in refrigerator at 4℃ for 34 h and repeatedly frozen and thawed for 4 times.The concentration-time curve of β-elemene of the extract of rats after administration of Curcuma zedoaria by oral gavage was consistent with the two-compartment model.The main pharmacokinetic parameters were as follows:AUC(0-t) was (9.83±1.07) μg·L-1·h, t1/2α was (0.47±0.05) h, t1/2β wss (1.82±3.11) h, Tmax was (2.06±0.37) h, and Cmax was (2.61±0.17) μg·mL-1.Conclusion:The established method is simple, accurate, specific and suitable for pharmacokinetic studies of β-elemene in curcuma zedoaria in rats.

-----参考文献:---------------------------------------------------------------------------------------

[1] 满伟,刘郁山,李文伟,等.莪术油药理研究及临床应用进展[J].时珍国医国药,2000,11(7):663 MAN W,LIU YS,LI WW,et al.Pharmological study and clinical application progress of Curcuma zedoaria oil[J].Lishizhen Med Mater Med Res,2000,11(7):663
[2] CHEN CC,CHEN Y,HSI YT,et al.Cytotoxic chemical constituents and anticancer activity of Curcuma zedoaria Rosc. essential oil against non-small cell lung carcinoma cells in vitro and in vivo[J].J Agric Food Chem,2013,61(47):11418
[3] CHEN HW,LEE JY,HUANG JY,et al.Curcumin inhibits lung cancer cell invasion and metastasis through the tumor suppressor H LJ1[J].Cancer Res,2008,68(18):7428
[4] 彭炳先,周欣,石京山,等.蓬莪术挥发油及其中3种成分抗肝癌和子宫内膜癌的研究[J].华西药学杂志,2007,22(3):312 PENG BX,ZHOU X,SHI JS,et al.Effects of volatile oil and three main components from Curcuma phaeocaulis valetonon liver cancer and endometrial carcinoma cell lines[J].West China J Pharm Sci,2007,22(3):312
[5] 王佳丽,王秀,夏泉,等.莪术油中3种倍半萜类化合物对肝癌HepG2细胞增殖抑制作用的研究[J].中成药,2014,36(7):1535 WANG JL,WANG X,XIA Q,et al.The proliferation inhibition effect on hepatoma HepG2 cell of three sesquiterpene components from Curcuma phaeocaulis oil[J].Chin Tradit Pat Med,2014,36(7):1535
[6] LEE JY,LEE YM,CHANG GC,et al.Curcumin induces EGFR degradation in lung adenocarcinoma and modulates p38 activation in intestine:the versatile adjuvant for gefitinib therapy[J].PLoS One,2011,6(8):e23756
[7] JAVADI S,ROSTAMIZADEH K,HEJAZI J,et al.Curcumin mediated down-regulation of αV β3 integrin and up-regulation of pyruvate dehydrogenase kinase 4(PDK4) in Erlotinib resistant SW480 colon cancer cells[J].Phytother Res,2018,32(2):355
[8] DOU H,SHEN R,TAO J,et al.Curcumin suppresses the colon cancer proliferation by inhibiting Wnt/β-catenin pathways via miR-130a[J].Front Pharmacol,2017,8:877
[9] ZOU B,LI Q,ZHAO J,et al.β-Elemene and taxanes synergis tically induce cytotoxicity and inhibit proliferation in ovarian cancer and other tumor cells[J].Anticancer Res,2013,33(3):929
[10] MU L,WANG T,CHEN Y,et al.β-Elemene enhances the efficacy of gefitinib on glioblastoma multiforme cells through the inhibition of the EGFR signaling pathway[J].Int J Oncol,2016,49(4):1427
[11] WANG J,HUANG F,BAI Z,et al.Curcumol inhibits growth and induces apoptosis of colorectal cancer LoVo cell line via IGF-1R and p38 MAPK pathway[J].Mol Sci,2015,16(8):19851
[12] YU X,XU M,LI N,et al.β-elemene inhibits tumor-promoting effect of M2 macrophages in lung cancer[J].Biochem Biophys Res Commun,2017,490(2):514
[13] CHEN Z,SONG Y,CHE J,et al.Validation of a sensitive gas chromatographic-mass spectrometric method for the simultaneous determination of β-elemene and β-elemenal in human plasma[J].J Chromatogr B Analyt Technol Biomed Life Sci, 2009,877(4):408
[14] 詹琼,周鑫莉,黄若凡,等.β-榄香烯血药浓度测定方法的建立及其药代动力学研究[J].中国药房,2017,28(2):173 ZHAN Q,ZHOU XL,HUANG RF,et al.Establishment of determination method for plasma concentration of β-elemene and its pharmacokinetic study in human[J].China Pharm,2017,28(2):173
[15] GAN YX,LUO NN,JIANG YP,et al.Simultaneous determination of beta-elemene,curcumol,germacrone and neocurdione in volatile oil of Curcuma phaeocaulis and vinegar products by GC-MS[J].China J Chin Mater Med,2015,40(7):1311

欢迎阅读《药物分析杂志》!您是该文第 213位读者!

药物分析杂志 © 2009
地址:北京天坛西里2号 邮政编码:100050; 电子邮件:ywfx@nicpbp.org.cn

本系统由北京博思汇文数字科技有限公司设计开发 技术服务电话:400-921-9838