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Free and/or glucuronidated Danshensu, protocatechuic aldehyde, protocatechuic acid and caffeic acid are potentially pharmacological components in rats after oral administration of extractum for Compound DanShen Dripping Pill
引用本文:LIU Hong-tao LI Wei LIU Yong YANG Ling. Free and/or glucuronidated Danshensu, protocatechuic aldehyde, protocatechuic acid and caffeic acid are potentially pharmacological components in rats after oral administration of extractum for Compound DanShen Dripping Pill[J]. 中国临床药理学与治疗学, 2007, 12(10): 1185-1185
作者姓名:LIU Hong-tao LI Wei LIU Yong YANG Ling
作者单位:[1]Laboratory of Pharmaceutical Resource Discovery, Biotechnology Division, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, Liaoning, China [2]Graduate School, Chinese Academy of Sciences, Beijing 100049, China
摘    要:AIM: To provide primarily pharmacokinetic profiles and reveal potentially pharmacological components after oral administration of the extractum for Compund Danshen Dripping Pill (CDDP) in rats, which was mainly composed of protocatechuic aldehyde (PAL), Danshensu (DSS), lithospermic acid A, lithospermic acid B, salvianolic acid D, rosmarinic acid, salvianolic acid B and salvianolic acid A. METHODS: After orally administration of 200 mg CDDP extractum for 1 h, the portal vein blood, the femoral artery blood, the bile and urine samples were separately collected. The gastrointestinal (GI) contents and mucosa were washed with physiological saline and the washing solution was pooled. The whole GI tract was removed and homogenized for analysis. The constituents and concentrations of all above samples were determined by the LC-MS analysis combined with the β-glucuronidase and sulfatase treatment. RESULTS: The investigation after oral administration of CDDP extractum for 1 h in rats indicated that: (1)Most of polyphenolic acids have been degraded into caffeic acid (CA) and DSS in the GI tract. Next, CA could be easily absorbed into blood circulation and a trace of DSS was also transported into the portal vein. The remains of undegraded polyphenolic acids and Danshensu were detained in the GI tract lumen. (2)Part of PAL was firstly oxidized into PAC in GI epithelial cells before absorption into the portal vein. Next, PAC and the rest PAL were further transported into blood circulation. (3)PAC and PAL were distributed in blood circulation in free and conjugated forms after being glucuronidated in the liver and the kidney while only free CA and DSS appeared in vivo. After that, all of these metabolites were gradually secreted into bile and urine.[第一段]

关 键 词:葡萄糖醛酸化 丹参素 原儿茶醛 原儿茶酚 咖啡酸 复方丹参滴丸 潜在药理活性组分

Free and/or glucuronidated Danshensu, protocatechuic aldehyde, protocatechuic acid and caffeic acid are potentially pharmacological components in rats after oral administration of extractum for Compound DanShen Dripping Pill
Abstract:
Keywords:Compound Danshen Dripping Pill   Protoeatechuic Aldehyde   protoeatechuic acid   caffeic acid  glucuronidatio
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