补骨脂二氢黄酮甲醚在大鼠体内的组织分布
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摘要
目的研究补骨脂二氢黄酮甲醚在大鼠体内的组织分布。方法通过超高效液相色谱-串联质谱(UPLC-MS/MS)法,分析采用Waters ACQUITY UPLC HSS T3色谱柱(2.1 mm×100 mm, 1.8μm);流动相0.05%甲酸-乙腈,梯度洗脱;体积流量0.3 mL/min;柱温30℃;ESI离子源;正离子模式。大鼠灌胃给予补骨脂二氢黄酮甲醚(70 mg/kg)后,于不同时间点(0.083、0.25、0.5、1、4 h)测定其在心、肝、脾、肺、肾、脑、胃、小肠中的组织浓度。结果各组织中均检测到补骨脂二氢黄酮甲醚,其组织浓度依次为胃>小肠>肝>肺>肾>脾>心>脑,除胃、小肠(0.25 h)外其他组织在0.5 h达到最高浓度。结论该方法简便、稳定、可靠,可用于补骨脂二氢黄酮甲醚的体内分析。
AIM To study the in vivo tissue distribution of bavachinin in rats.METHODS Using an ultra-high performance liquid chromatography-tandem mass spectrometry(UPLC-MS/MS) method, the analysis was performed on a 30 ℃ thermostatic Waters ACQUITY UPLC HSS T3 column(2.1 mm×100 mm, 1.8 μm), with the mobile phase comprising of 0.05% formic acid-acetonitrile flowing at 0.3 mL/min in a gradient elution manner, and ESI source in a positive ionization mode was selected. Rats were given intragastric administration of bavachinin(70 mg/kg), after which the tissue concentrations in heart, liver, spleen, lung, kidney, brain, stomach and small intestine were determined at different time points(0.083, 0.25, 0.5, 1, 4 h).RESULTS Bavachinin was detected in various tissues, whose tissue concentrations were in sequence of stomach>small intestine>liver>lung>kidney>spleen>heart>brain. Except for stomach and small intestine(0.25 h), the other tissues reached the highest concentration at 0.5 h.CONCLUSION This simple, stable and reliable method can be used for the in vivo analysis of bavachinin.
AIM To study the in vivo tissue distribution of bavachinin in rats.METHODS Using an ultra-high performance liquid chromatography-tandem mass spectrometry(UPLC-MS/MS) method, the analysis was performed on a 30 ℃ thermostatic Waters ACQUITY UPLC HSS T3 column(2.1 mm×100 mm, 1.8 μm), with the mobile phase comprising of 0.05% formic acid-acetonitrile flowing at 0.3 mL/min in a gradient elution manner, and ESI source in a positive ionization mode was selected. Rats were given intragastric administration of bavachinin(70 mg/kg), after which the tissue concentrations in heart, liver, spleen, lung, kidney, brain, stomach and small intestine were determined at different time points(0.083, 0.25, 0.5, 1, 4 h).RESULTS Bavachinin was detected in various tissues, whose tissue concentrations were in sequence of stomach>small intestine>liver>lung>kidney>spleen>heart>brain. Except for stomach and small intestine(0.25 h), the other tissues reached the highest concentration at 0.5 h.CONCLUSION This simple, stable and reliable method can be used for the in vivo analysis of bavachinin.
引文
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[13] Suneetha A,Raja R K.Comparison of LC-UV and LC-MS methods for simultaneous determination of teriflunomide,dimethyl fumarate and fampridine in human plasma:application to rat pharmacokinetic study[J].Biomed Chromatogr,2016,30(9):1371-1377.
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[2] Nepal M,Choi H J,Choi B Y,et al.Anti-angiogenic and anti-tumor activity of bavachinin by targeting hypoxia-inducible factor-1α[J].Eur J Pharmacol,2012,691(1-3):28-37.
[3] Chen X,Wen T,Wei J,et al.Treatment of allergic inflammation and hyperresponsiveness by a simple compound,Bavachinin,isolated from Chinese herbs[J].Cell Mol Immunol,2013,10(6):497-505.
[4] Chen X,Shen Y,Liang Q,et al.Effect of bavachinin and its derivatives on T cell differentiation[J].Int Immunopharmacol,2014,19(2):399-404.
[5] Chopra B,Dhingra A K,Dhar K L.Psoralea corylifolia L.(Buguchi)-folklore to modern evidence:review[J].Fitoterapia,2013,90:44-56.
[6] Yin S,Fan C Q,Wang Y,et al.Antibacterial prenylflavone derivatives from Psoralea corylifolia,and their structure-activity relationship study[J].Bioorg Med Chem,2004,12(16):4387-4392.
[7] 王天晓,尹震花,张伟,等.补骨脂抗氧化、抑制α-葡萄糖苷酶和抗菌活性成分研究[J].中国中药杂志,2013,38(14):2328-2333.
[8] Chen X,Yang Y,Zhang Y.Isobavachalcone and bavachinin from Psoraleae Fructus modulate Aβ42 aggregation process through different mechanisms in vitro[J].FEBS Lett,2013,587(18):2930-2935.
[9] Guo F J,Huang C,Feng L,et al.PPAR α/γ dual agonist and its application:WO,2014/169800[P].2014-10-23.
[10] Feng L,Luo H,Xu Z,et al.Bavachinin,as a novel natural pan-PPAR agonist,exhibits unique synergistic effects with synthetic PPAR-γ and PPAR-α agonists on carbohydrate and lipid metabolism in db/db and diet-induced obese mice[J].Diabetologia,2016,59(6):1276-1286.
[11] Qian J,Xie F,Shi Y H,et al.Pharmacokinetic and metabolism studies of bavachinin through ultra-high-performance liquid chromatography coupled with electrospray ionization tandem mass spectrometry[J].Biomed Chromatogr,2018,32(10):e4293.
[12] Food Drug Administration (FDA).Bioanalytical method validation guidance for industry[R].[2018-05-24].http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInfor mation/Guidances/UCM070107.pdf.
[13] Suneetha A,Raja R K.Comparison of LC-UV and LC-MS methods for simultaneous determination of teriflunomide,dimethyl fumarate and fampridine in human plasma:application to rat pharmacokinetic study[J].Biomed Chromatogr,2016,30(9):1371-1377.
[14] 魏敏吉,赵明.创新药物药代动力学研究与评价[M].北京:北京大学医学出版社,2008:11.