摘要
目的 研究大鼠肠道水解酶对淫羊藿所含黄酮成分淫羊藿苷、朝藿定A、朝藿定B、朝藿定C在肠道处置的影响。方法 应用大鼠在体肠灌流模型，用高效液相法测定药物浓度，比较淫羊藿黄酮苷在加入肠道乳糖酶根皮苷水解酶（LPH酶）抑制剂葡糖酸内酯（gluconolactone）前后表观渗透系数的变化。结果 加入抑制剂后，4个淫羊藿黄酮苷在大鼠十二指肠、空肠、回肠、结肠的表观渗透系数都有不同程度的下降，其中淫羊藿苷在4个肠段的水解抑制率分别为：62%，50%，40%，46%；朝藿定A分别为：55%，26%，21%，14%；朝藿定B分别为：42%，40%，74%，22%；朝藿定C分别为：42%，40%，52%，35%。结论 LPH酶抑制剂葡糖酸内酯能不同程度地抑制淫羊藿苷、朝藿定A、朝藿定B、朝藿定C在大鼠肠道的水解，说明大鼠肠黏膜上的LPH酶参与了淫羊藿苷、朝藿定A，B，C在肠道的代谢。
Abstract
OBJECTIVE To study the influence of rat intestinal hydrolase on the d ispose of flavonoids (icariin， epimedin A， epimedin B， epimedin C) in Herb Epimedii. METHODS Using the rat intestinal perfusion model， the contents of the four flavonoids in perfusates were measured by HPLC and the permeability coefficients of different intestinal segments were calculated. RESULTS After adding LPH (lactasc phlorizin hydrolase) inhibitor gluconolactone， the permeabilities of 4 flavonoid compounds decreased in different intestinal segments， and their hydrolysis inhibition ratios in duodenum， jejunum， ileum， and colon according to the sequence were as follows： icariin， 62%， 50%， 40% and 46%； epimedin A， 55%， 26%， 21% and 14%； epimedin B， 42%， 40%， 74% and 22%； epimedin C， 42%， 40%， 52% and 35%， respectively. CONCLUSION The inhibitior of LPH could inhibit the hydrolysis of icariin and epimedin A， B and C. The lactasc phlorizin hydrolase might involve in the dispose of the flavonoids in Herb Epimedii in intestines.
关键词
乳糖酶根皮苷水解酶抑制剂 /
大鼠肠灌流模型 /
淫羊藿黄酮苷 /
表观渗透系数
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Key words
inhibitior of lactasc phlorizin hydrolase /
rat intestinal perfusion model /
flavonoids in Herb Epimedii /
permeability coefficient
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陈彦 贾晓斌 谭晓斌 范晨怡 蔡垠 H Ming.
大鼠肠道水解酶对淫羊藿黄酮苷的处置影响[J]. 中国药学杂志, 2010, 45(7): 516-518
CHEN Yn;JI Xio-in;TN Xio-in;FN Chen-yi;CI Yin;HU Ming.
Influence of Rat Intestinal Hydrolase on Dispose of Flavonoids in Herb Epimedii[J]. Chinese Pharmaceutical Journal, 2010, 45(7): 516-518
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参考文献
［1］ WANG S W J， CHEN J， JIA X B， et al. Disposition of flavonoids via enteric recycling： Structural effects and lack of correlations between in vitro and in situ metabolic properties［J］. Drug Metab Dispos，2006，34(11)：1837-1848.
［2］ CHEN J， LIN H， HU M. Metabolism of flavonoids via enteric recycling： Role of intestinal disposition［J］. J Pharmacol Exp Ther，2003， 304(3)：1228-1235.
［3］ SESINK A L A， ARTS I C W， FAASSEN-PETERS M， et al. Intestinal uptake of quercetin-3-glucoside in rats involves hydrolysis by lactase phlorizin hydrolase［J］. J Nutr，2003，133(3)：773-776.
［4］ HUANG X L， ZhOU Y W， WANG W. Pharmacological advancement of flavonoids in Herb Epimedii［J］. Chin Tradit Pat Med(中成药)， 2005，27(6)：719-721.
［5］ CHEN Y， JIA X B， HU M. Absorption of flavonoids in Herb Epimedii across Caco-2 monolayer model ［J］. Chin Herb Med(中草药)，2009，40(2)： 220-224.
［6］ YE L K， CHEN J M， LIU S H， et al. Pharmacokinetics of icariin in rat［J］. Chin Pharm J(中国药学杂志)，1999， 34(1)：33-36.
［7］ LIU Z Q， JIANG Z H， LIU L， et al. Mechanisms responsible for poor oral bioavailability of paeoniflorin： Role of intestinal disposition and interactions with sinomenine［J］. Pharm Res，2006， 23(12)：2768-2780.
［8］ CHEN J， LIN H M， HU M. Metabolism of flavonoid via enteric recycling： Role of intestinal disposition［J］. Pharmacol Exp Ther，2003， 304(3)：1228-1235.
［9］ LIU Y， LIU Y， DAI Y，et al. Enteric disposition an recycling of flavonoids and ginkgo flavonoids ［J］. Alter Complement Med，2003，9(5)：631-640.
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