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学科主题药学
Absorption and metabolism of Astragali Radix decoction: In silico, in vitro, and a case study in vivo
Xu, F; Zhang, Y; Xiao, SY; Lu, XW; Yang, DH; Yang, XD; Li, CL; Shang, MY; Tu, PF; Cai, SQ
刊名DRUG METABOLISM AND DISPOSITION
2006-06-01
DOI10.1124/dmd.105.008300
34期:6页:913-924
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Pharmacology & Pharmacy
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]CELL-CULTURE MODEL ; MEMBRANACEUS BUNGE ; LIQUID-CHROMATOGRAPHY ; SMALL-INTESTINE ; FLAVONOIDS ; TRANSPORT ; ROOTS ; MONGHOLICUS ; BIOAVAILABILITY ; IDENTIFICATION
英文摘要

To profile absorption of Astragali Radix decoction and identify its orally absorbable constituents and their metabolites, four complementary in silico, in vitro, and in vivo methods, i.e., a computational chemistry prediction method, a Caco-2 cell monolayer model experiment, an improved rat everted gut sac experiment, and a healthy human volunteer experiment, were used. According to the in silico computation result, 26 compounds of Astragali Radix could be regarded as orally available compounds, including 12 flavonoids. In the in vitro and in vivo experiments, 21 compounds were tentatively identified by high-performance liquid chromatography-diode array detection-electrospray ion trap tandem mass spectrometry data, which involved calycosin, formononetin, (6aR, 11aR)-3-hydroxy- 9,10-dimethoxypterocarpan, 7,2′-dihydroxy-3′, 4′-dimethoxyisoflavan, calycosin-7- O-beta-D-glucoside, formononetin-7-O-beta-D-glucoside, 7,2′-dihydroxy-3 , 4′-dimethoxyisoflavan-7-O-beta-D-glucoside-6"-O-malonate, (6aR, 11aR)-3-hydroxy-9,10-dimethoxypterocarpan-3-O-beta-D-glucoside, and phase II metabolites calycosin-7-O-beta-D-glucuronide, formononetin-7-O-beta-D-glucuronide, (6aR, 11aR)-3-hydroxy-9,10-dimethoxypterocarpan- 3-O-beta-D-glucuronide, 7,2′-dihydroxy-3′, 4′-dimethoxyisoflavan- 7-O-beta-D-glucuronide, and calycosin sulfate. Calycosin and formononetin were proved absorbable by four methods; (6aR,11aR)-3-hydroxy-9,10-dimethoxypterocarpan and 7,2′-dihydroxy- 3′, 4′-dimethoxyisoflavan were proved absorbable by three methods; formononetin-7-O-beta-D-glucoside and (6aR, 11aR)-3-hydroxy-9,10- dimethoxypterocarpan-3-O-beta-D-glucoside were proved absorbable by two methods. The existence of calycosin-7-O-beta-D-glucuronide, formononetin-7-O-beta-D-glucuronide, (6aR, 11aR)-3-hydroxy-9,10- dimethoxypterocarpan-3-O-beta-D-glucuronide, 7,2′-dihydroxy-3 ′, 4′-dimethoxyisoflavan-7-O-beta-D-glucuronide, and calycosin sulfate was proved by two or three methods. We found that besides isoflavones, pterocarpans and isoflavans also could be metabolized by the intestine during absorption, and the major metabolites were glucuronides. In conclusion, the present study demonstrated that the flavonoids in Astragali Radix decoction, including isoflavones, pterocarpans, and isoflavans, could be absorbed and metabolized by the intestine. These absorbable compounds, which were reported to have various bioactivities related to the curative effects of Astragali Radix decoction, could be regarded as an important component of the effective constituents of Astragali Radix decoction.

语种英语
WOS记录号WOS:000237643400004
引用统计
被引频次:62[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/61036
专题北京大学药学院_天然药物学系
作者单位1.Peking Univ, Sch Pharmaceut Sci, Dept Nat Med, Hlth Sci Ctr,State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China
2.Beijing Inst Technol, Sch Biosci & Biotechnol, Beijing 100081, Peoples R China
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GB/T 7714
Xu, F,Zhang, Y,Xiao, SY,et al. Absorption and metabolism of Astragali Radix decoction: In silico, in vitro, and a case study in vivo[J]. DRUG METABOLISM AND DISPOSITION,2006,34(6):913-924.
APA Xu, F.,Zhang, Y.,Xiao, SY.,Lu, XW.,Yang, DH.,...&Cai, SQ.(2006).Absorption and metabolism of Astragali Radix decoction: In silico, in vitro, and a case study in vivo.DRUG METABOLISM AND DISPOSITION,34(6),913-924.
MLA Xu, F,et al."Absorption and metabolism of Astragali Radix decoction: In silico, in vitro, and a case study in vivo".DRUG METABOLISM AND DISPOSITION 34.6(2006):913-924.
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