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金丝桃素在大鼠体内的代谢产物

赵娟芝, 王聪, 李进典, 张东建, 张健, 殷志琦

赵娟芝, 王聪, 李进典, 张东建, 张健, 殷志琦. 金丝桃素在大鼠体内的代谢产物[J]. 中国药科大学学报, 2016, 47(4): 457-462. DOI: 10.11665/j.issn.1000-5048.20160411
引用本文: 赵娟芝, 王聪, 李进典, 张东建, 张健, 殷志琦. 金丝桃素在大鼠体内的代谢产物[J]. 中国药科大学学报, 2016, 47(4): 457-462. DOI: 10.11665/j.issn.1000-5048.20160411
ZHAO Juanzhi, WANG Cong, LI Jindian, ZHANG Dongjian, ZHANG Jian, YIN Zhiqi. Metabolites of hypericin in rats in vivo[J]. Journal of China Pharmaceutical University, 2016, 47(4): 457-462. DOI: 10.11665/j.issn.1000-5048.20160411
Citation: ZHAO Juanzhi, WANG Cong, LI Jindian, ZHANG Dongjian, ZHANG Jian, YIN Zhiqi. Metabolites of hypericin in rats in vivo[J]. Journal of China Pharmaceutical University, 2016, 47(4): 457-462. DOI: 10.11665/j.issn.1000-5048.20160411

金丝桃素在大鼠体内的代谢产物

基金项目: 国家自然科学基金资助项目(No.81473120);“华海药业研究生创新基金”资助项目

Metabolites of hypericin in rats in vivo

  • 摘要: 分离鉴定金丝桃素在大鼠胆汁中的代谢产物以及在坏死肝脏组织中的存在形式。正常大鼠和肝脏缺血再灌注损伤模型大鼠经静脉注射10 mg/kg金丝桃素后,收集正常大鼠0~12 h胆汁以及坏死模型大鼠24 h坏死肝脏组织,对生物样品预处理后,采用高效液相色谱-高分辨飞行时间质谱(HPLC-TOF/MS)联用技术进行分析。在大鼠胆汁中鉴定出金丝桃素原形(M0)和3个葡萄糖化代谢产物(M1、M2、M3),而在坏死肝脏组织中仅鉴定出金丝桃素原形。结果表明,金丝桃素在大鼠胆汁中主要以原形和葡萄糖化形式存在,在坏死组织中主要以原形存在。
    Abstract: The study aimed to separate and identify the metabolites of hypericin in the bile and necrotic tissues in rats. After intravenous injection of 10 mg/kg hypericin, 0-12 h bile of normal rats and 24 h necrotic liver of rats with reperfused hepatic infarction were collected, and metabolites of rats were analyzed by high performance liquid chromatography coupled with electrospray tandemtime of flight mass spectrometry(HPLC-TOF/MS). The prototype(M0)and three glycosylation metabolites(M1, M2, M3)of hypericin in rat bile and the parent compound in rat necrotic liver were detected and identified. Results indicated that prototype and glycosylation of hypericin were the major metabolic form in rat bile and the parent compound was found only in necrotic tissues.
  • [1] Cooper EH, Bedford AJ, Kenny TE. Cell death in normal and malignant tissues[J].Adv Cancer Res,1975,21:59-120.
    [2] Smith BA,Smith BD.Biomarkers and molecular probes for cell death imaging and targeted therapeutics[J].Bioconjug Chem,2012,23(10):1989-2006.
    [3] Chen SL, Yu LK, Jiang CY, et al. Pivotal study of iodine-131-labeled chimeric tumor necrosis treatment radioimmunotherapy in patients with advanced lung cancer[J].J Clin Oncol,2005,23(7):1538-1547.
    [4] Li J, Oyen R, Verbruggen A, et al. Small molecule sequential dual-targeting theragnosticstrategy(SMSDTTS):from preclinical experiments towards possible clinical anticancer applications[J].J Cancer,2013,4(2):133-145.
    [5] Van de Putte M,Marysael T,Fonge H,et al.Radiolabelediodohypericin as tumor necrosis avid tracer:diagnostic and therapeutic potential[J].Int J Cancer,2012,131(2):E129-E137.
    [6] Kerb R,Brockmller J,Staffeldt B,et al.Single-dose and steady-state pharmacokinetics of hypericin and pseudohypericin[J].Antimicrob Agents Chemother,1996,40(9):2087-2093.
    [7] Kamuhabwa AAR,Di Mavungu JD,Baert L,et al.Determination of hypericin in human plasma by high-performance liquid chromatography after intravesical administration in patients with transitional cell carcinoma of the bladder[J].Eur J Pharm Biopharm,2005,59(3):469-474.
    [8] Kong M,Zhang J,Jiang CH,et al.Necrosis affinity evaluation of 131I-hypericin in a rat model of induced necrosis[J].J Drug Target,2013,21(6):604-610.
    [9] Yan YT,LaiChang JS,Li P,et al.Metabolites of salvianolic acid C in rats[J].J China Pharm Univ (中国药科大学学报),2013,44(5):442-446.
    [10] Zhang YQ, Long T, Niu YJ, et al. Research progress in oral absorption and metabolism of natural anthraquinones[J].Strait Pharm J (海峡药学),2014,26(7):1-5.
    [11] Song R,Xu L,Xu FG,et al.Metabolic analysis of rhubarb extract by rat intestinal bacteria using liquid chromatography-tandem mass spectrometry[J].Biomed Chromatogr,2011,25(3):417-426.
    [12] Song R,Lin H,Zhang ZJ,et al.Profiling the metabolic differences of anthraquinone derivatives using liquid chromatography/tandem mass spectrometry with data-dependent acquisition[J].Rapid Commun Mass Spectrom,2009,23(4):537-547.
    [13] Song R,Xu FG,Zhang ZJ,et al.Structural elucidation of in vitro metabolites of emodin by liquid chromatography-tandem mass spectrometry[J].Biomed Chromatogr,2008,22(11):1230-1236.
    [14] Liu W,Zheng ZJ,Liu X,et al.Sensitive and robust UPLC-MS/MS method to determine the gender-dependent pharmacokinetics in rats of emodin and its glucuronide[J].J Pharm Biomed Anal,2011,54(5):1157-1162.
    [15] Wan JB,Bai X,Cai XJ,et al.Chemical differentiation of Da-Cheng-Qi-Tang,a Chinese medicine formula,prepared by traditional and modern decoction methods using UPLC/Q-TOFMS-based metabolomics approach[J].J Pharmaceut Biomed Analy,2013,83:34-42.
    [16] Bánó G,Staniová J,Jancura D,et al.On the diffusion of hypericin in dimethylsulfoxide/water mixtures—the effect of aggregation[J].J Phys Chem B,2011,115(10):2417-2423.
    [17] Liu XJ,Jiang CH,Li Y,et al.Evaluation of hypericin:effect of aggregation on targeting biodistribution[J].J Pharm Sci,2015,104(1):215-222.
    [18] Yang J,Qian DW,Duan JA,et al.Advances in studies on metabolism of constituents in Chinese materiamedica by intestinal bacteria[J].Chin Tradit Herb Drugs (中草药),2011,42(11):2335-2344.
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出版历程
  • 刊出日期:  2016-08-24

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