蜘蛛香35%乙醇提取物的肠吸收特性
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摘要
目的研究蜘蛛香35%乙醇提取物的肠吸收特性。方法进行大鼠单向肠灌流实验,计算提取物肠灌流液中不同质量浓度(0.5、1.0、1.5 g/mL)新绿原酸、绿原酸、隐绿原酸、异绿原酸B、异绿原酸A、橙皮苷、异绿原酸C吸收参数,考察P-糖蛋白抑制剂(维拉帕米)对提取物吸收的影响。结果除异绿原酸A、橙皮苷外,其他成分K_a、P_(app)值随着其质量浓度增加无明显变化。加入维拉帕米后,各成分(1.0 g/mL)K_a、P_(app)值显著提高(P<0.01)。结论蜘蛛香35%乙醇提取物中7种成分在小肠中呈中等吸收,可能与P-糖蛋白有关。其中,异绿原酸A、橙皮苷吸收机制可能为主动转运,其他成分为自由扩散转运。
AIM To study the intestinal absorption characteristics of 35% ethanol extract from Valeriana jatamansi Jones.METHODS The performance of single-pass intestinal perfusion experiment in rats was succeeded by the calculation of absorption parameters for different concentrations(0.5, 1.0, 1.5 g/mL) of new chlorogenic acid, chlorogenic acid, hypochlorogenic acid, isochlorogenic acid B, isochlorogenic acid A, hesperidin, isochlorogenic acid C in the intestinal perfusate of extract, and the effect of P-glycoprotein inhibitor(verapamil) on extract absorption was investigated. RESULTS The constituents' K_a and P_(app) values, except isochlorogenic acid A and hesperidin, did not obviously change with their concentration increase. Yet after the addition of verapamil, significant K_a and P_(app) values increase was observed(P<0.01).CONCLUSION The moderate small intestinal absorption of seven constituents in 35% ethanol extract from V. jatamansi may be related to P-glycoprotein, among which active transport may be the absorption mechanisms of isochlorogenic acid A and hesperidin, while free-diffusion transport may be those of the other constituents.
AIM To study the intestinal absorption characteristics of 35% ethanol extract from Valeriana jatamansi Jones.METHODS The performance of single-pass intestinal perfusion experiment in rats was succeeded by the calculation of absorption parameters for different concentrations(0.5, 1.0, 1.5 g/mL) of new chlorogenic acid, chlorogenic acid, hypochlorogenic acid, isochlorogenic acid B, isochlorogenic acid A, hesperidin, isochlorogenic acid C in the intestinal perfusate of extract, and the effect of P-glycoprotein inhibitor(verapamil) on extract absorption was investigated. RESULTS The constituents' K_a and P_(app) values, except isochlorogenic acid A and hesperidin, did not obviously change with their concentration increase. Yet after the addition of verapamil, significant K_a and P_(app) values increase was observed(P<0.01).CONCLUSION The moderate small intestinal absorption of seven constituents in 35% ethanol extract from V. jatamansi may be related to P-glycoprotein, among which active transport may be the absorption mechanisms of isochlorogenic acid A and hesperidin, while free-diffusion transport may be those of the other constituents.
引文
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[2] Singh R D, Gopichand, Meena L R, et al. Seasonal variation of bioactive components in Valeriana jatamansi from Himachal Pradesh, India[J].Ind Crops Prod, 2010, 32(3):292-296.
[3] Verma R S, Verma R K, Padalia R C, et al. Chemical diversity in the essential oil of Indian valerian (Valeriana jatamansi Jones)[J].Chem Biodivers,2011,8(10): 1921-1929.
[4] 李庆杰,王琦,都帅, 等.蜘蛛香的化学成分及其抗焦虑作用研究进展[J/OL].吉林中医药,2018,38(5):1-4[2018-12-14]. http://kns.cnki.net/kcms/detail/22.1119.R.20171128.0948.002.html.
[5] 石晋丽,刘勇,肖培根.HPLC法测定不同产地蜘蛛香中橙皮苷的含量[J].中草药,2005,36(3):449-450.
[6] 李蓉,吴莹.蜘蛛香的药理作用研究进展[J].科技资讯,2009(31):159.
[7] 伍萍,李梅,巩仔鹏,等.基于在体循环肠灌流模型分析羊耳菊提取物的肠吸收特性[J].中国实验方剂学杂志,2018,24(2):1-8.
[8] 何帅,蔺明煊,姜亦南,等.中药成分肠吸收模型研究进展与思考[J].中医药学报,2018,46(3):121-124.
[9] 杜秋,狄留庆,单进军,等.在体单向肠灌流模型研究瑞香素的大鼠肠吸收特性[J].药学学报,2009,44(8):922-926.
[10] Fagerholm U, Johansson M, Lennern?s H.Comparison between permeability coefficients in rat and human jejunum[J].Pharm Res,1996,13(9):1336-1342.
[11] 彭敏.马蹄香抗焦虑复方药效及机制初探[D].北京:北京中医药大学,2011.
[12] Ito A, Shin N, Tsuchida T,et al.Antianxiety-like effects of Chimpi (dried citrus peels) in the elevated open-platform test[J].Molecules,2013,18(8): 10014-10023.
[13] 李云,周明眉,邢丽娜,等.绿原酸的肠道菌群代谢研究进展[J].中草药,2015,46(4):610-614.
[14] Lampe J W, Chang J L. Interindividual differences in phytochemical metabolism and disposition[J].Semin Cancer Biol, 2007,17(5):347-353.
[15] 吴干斌,褚延乐.大鼠在体单向肠灌流模型研究冬凌草乙素的吸收动力学[J].中国中药杂志,2018,43(15):3192-3197.