Metabolism of Echinacoside, a Good Antioxidant, in Rats: Isolation and Identification of Its Biliary Metabolites

Abstract

, 1997), which is an important traditional Chinese medicine used for the treatment of kidney deficiency and neurodegenerative diseases. ECH is also the main phenolic component in Echinacea angustifolia and Echinacea pallida roots (Perry et al., 2001), which are widely used in Europe, North America, and Australia for their immunostimulating activities. As a natural polyphenolic compound, ECH showed various bioactivities, such as antioxidative (Li et al., 1992;Xiong et al., 1996;Hu and Kitts, 2000;Cervellati et al., 2002), neuroprotective (Den et al., 2004;Koo et al., 2005;Chen et al., 2007;Geng et al., 2007), nitric oxide radical-scavenging (Xiong et al., 2000), and antihepatotoxic activities (Houghton and Hikino, 1989;Wu et al., 2007).Although ECH exhibited diverse bioactivities in in vivo and in vitro assays, only a few reports dealing with the metabolism and disposition of ECH are available. In our previous study on the pharmacokinetics and bioavailability of ECH in rat, the distribution and elimination of ECH were extremely fast (t 1/2␣ , 12.4 min; t 1/2␤ , 41.0 min), clearance was 0.0001 mg/kg/min/(ng/ml) after i.v. administration (5 mg/kg), and the bioavailability of ECH was only 0.83% (Jia et al., 2006). The very low bioavailability of ECH was consistent with the results of Matthias et al. (2004), in which ECH permeated poorly through the Caco-2 monolayers. Moreover, our pharmacokinetic data suggested that ECH was mostly metabolized after dosing. Therefore, we hypothesized that, in addition to the parent compound, some metabolic products of ECH may show biological activities, thereby contributing to the pharmacological efficacy of ECH in vivo. It was necessary to

Echinacoside improves hematopoietic function in 5-FU-induced myelosuppression mice

“…1) is a phenylethanoid compound extracted from traditional Chinese medicine Herba Cistanches that is Life Sciences 123 (2015) 86-92 widely used as a promoting agent for blood circulation, medications for kidney deficiency as well as neurodegenerative diseases [24]. ECH has multiple pharmacological activities of bone regeneration [18], antioxidation [8,14,27], immune regulation, neuroprotection, and behavioral improvement [11,16]. It was also revealed as a protective agent against hepatotoxicity [32] and acute lung injury [34].…”

Phenylethanoid Glycosides: Research Advances in Their Phytochemistry, Pharmacological Activity and Pharmacokinetics

“…Eight phase II metabolites of parent compound (methyl ethers, glucuronides, and minor sulfates) were isolated and identified unambiguously from rat bile sample after i.v. administration of 117 [123]. Unlike the metabolites in rat bile, besides the phase II metabolites of parent compound, the degradation products and their glucuronic acid, sulfate, and methyl conjugations were identified in rat urine and feces [124].…”

Effects of Herbal Supplements on Drug Glucuronidation. Review of Clinical, Animal, andIn VitroStudies

“…Among the common compounds in Echinacea are polyphenolic compounds including cichoric acid and echinacoside. Jia et al studied phase II metabolites of echinacoside in rats and isolated two glucuronide metabolites for echinacoside [64]. More in vitro studies using HLM or expressed UGT enzymes are needed to characterize the relative contribution of individual UGT enzymes to Echinacea metabolism.…”