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基于化学成分和药代动力学的研究揭示了中药方剂圣涎汤中桔梗的协同作用特性。

Chemical profile- and pharmacokinetics-based investigation of the synergistic property of platycodonis radix in traditional Chinese medicine formula Shengxian decoction.

机构信息

Department of Pharmacy, Changzheng Hospital, Second Military Medical University, 415 Fengyang Road, Shanghai 200003, PR China.

Department of Pharmacognasy, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, PR China.

出版信息

J Ethnopharmacol. 2014 Mar 28;152(3):497-507. doi: 10.1016/j.jep.2014.01.033. Epub 2014 Feb 10.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

To investigate the synergistic property of Platycodonis radix (PG) in a classic traditional Chinese medicine (TCM) prescription Shengxian decoction (SXT) by combining chemical profile with pharmacokinetic analysis strategy. The synergized prescription consisted of Astragali radix, Anemarrhenae rhizoma, Bupleuri radix, and Cimicifuage rhizoma.

MATERIALS AND METHODS

Ultra-performance liquid chromatography/quadruple time-of-flight mass spectrometry (UPLC-Q-TOF/MS) was employed to investigate the chemical fingerprints of SXT and decreased SXT (SXT that removed Platycodonis radix, SXT-PG). A reliable LC-MS/MS method was developed to examine the pharmacokinetics of 9 marker compounds (including formononetin, calycosin-7-O-β-d-glucoside, ononin, caffeic acid, isoferulic acid, mangiferin, timosaponin E1, timosaponin B-II and timosaponin B) following oral administration of SXT and SXT-PG in rats. Both in vitro chemical profiles and in vivo pharmacokinetic parameters differences between SXT and SXT-PG were conducted.

RESULTS

By using UPLC-Q-TOF/MS method, a total of 25 compounds identified from SXT, including 13 triterpenoids, 5 caffeinic derivatives, 4 isoflavonoids and 3 xanthone glycosides. Comparing the chemical fingerprints between SXT and decreased SXT did not reveal significant difference in the chemical profile of other four TCMs. The improved pharmacokinetic profiles of mangiferin, timosaponin E1, timosaponin B-II and timosaponin B were found in SXT group, suggesting the quicker distribution and more effective absorption, when compared with those in the SXT-PG group.

CONCLUSIONS

These results indicated that PG did not increase the dissolution of synergized prescription when co-decocting, but guided the synergized prescription to target location, reflecting the courier role of PG, which was in line with the clinical principle of TCM. It also established a useful method for TCM synergistic property research.

摘要

民族药理学相关性

通过结合化学特征和药代动力学分析策略,研究经典中药方剂(SXT)中桔梗的协同作用。协同处方由黄芪、知母、柴胡和川芎组成。

材料和方法

采用超高效液相色谱/四重飞行时间质谱(UPLC-Q-TOF/MS)研究 SXT 和减少的 SXT(去除桔梗的 SXT,SXT-PG)的化学指纹图谱。建立了一种可靠的 LC-MS/MS 方法来检测大鼠口服 SXT 和 SXT-PG 后 9 种标记化合物(包括芒柄花素、芹菜素-7-O-β-D-葡萄糖苷、毛蕊异黄酮、咖啡酸、异阿魏酸、芒果苷、知母皂苷 E1、知母皂苷 B-II 和知母皂苷 B)的药代动力学参数。对 SXT 和 SXT-PG 的体外化学特征和体内药代动力学参数差异进行了比较。

结果

采用 UPLC-Q-TOF/MS 方法,从 SXT 中鉴定出 25 种化合物,包括 13 种三萜类、5 种咖啡酸衍生物、4 种异黄酮类和 3 种蒽酮糖苷类。比较 SXT 和减少的 SXT 的化学指纹图谱,发现其他四种中药的化学特征没有明显差异。在 SXT 组中发现芒果苷、知母皂苷 E1、知母皂苷 B-II 和知母皂苷 B 的药代动力学特征得到了改善,与 SXT-PG 组相比,分布更快,吸收更有效。

结论

这些结果表明,桔梗在共同煎煮时并没有增加协同处方的溶解,但引导协同处方到达目标位置,反映了桔梗的快递作用,这符合中医的临床原则。它还为中药协同作用的研究建立了一种有用的方法。

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