Intestinal Permeability of the Constituents from the Roots ofSaposhnikovia divaricatain the Human Caco-2 Cell Monolayer Model

Abstract

The bidirectional intestinal permeability of the active constituents from the roots of Saposhnikovia divaricata, including four coumarins, anomalin (1), 5-methoxy-7-(3,3-dimethylallyloxy)coumarin (2), decursin (3), and decursinol angelate (4), as well as four chromones, cimifugin (5), prim-O-glucosylcimifugin (6), 3'- O-angeloylhamaudol (7), and sec-O-glucosylhamaudol (8), was studied by using the Caco-2 cell monolayer. These compounds were assayed by HPLC, and their transport parameters, including apparent permeability coefficients (P(app)), were then calculated. The bidirectional P(app) values of the compounds were compared with those of the markers, propranolol and atenolol. Compounds 1-5 and 7 were assigned to well-absorbed compounds, while 6 and 8 were assigned to moderately absorbed compounds. The transport of 1-7 increased linearly as a function of time up to 180 min and concentration within the test range of 10-200 µM, thus their passive diffusion mechanism was proposed. The results provided some useful information for predicting the intestinal absorption in vivo of these compounds.

Development of an SPE–HPLC–MS method for simultaneous determination and pharmacokinetic study of bioactive constituents of Yu Ping Feng San in rat plasma after oral administration

“…However, its aglycone cycloastragenol can be absorbed through intestinal epithelium efficiently . This is similar to prim-O-glucosylcimifugin, 4 0 -O-b-glucopyranosyl-5-O-methylvisamminol, and their aglycone cimifugin Xue et al, 2000;Zhao et al, 2011). It has been reported that changes in telomere lengths are relevant to immune function (Weng, 2012), and cycloastragenol upregulates telomerase activity (Fauce et al, 2008;Ríos, 2010;Yung et al, 2012).…”

“…It has been used for preventing viral infections including severe acute respiratory syndrome (Lau et al, 2005;Poon et al, 2006), and is reported to have immunoregulatory and beneficial effects in allergic rhinitis, asthma, and dermatitis models (Fang et al, 2005;Makino et al, 2004Makino et al, , 2005Nakatsukasa et al, 2009). Phytochemical and serum pharmacochemical analyses have found that YPFS contains isoflavones from Radix Astragali and chromones from Radix Saposhnikoviae as major constituents (Huang et al, 2008;You, 2007;Zhao et al, 2011;Zheng et al, 2011). In Radix Astragali, astragalosides have been identified as potential bioactive compounds via intestinal absorption and cell extraction studies (Xu et al, 2006;Zhang et al, 2008).…”

Saposhnikoviae divaricata : a phytochemical, pharmacological, and pharmacokinetic review

“…Among 9 phytochemistry papers with in vitro studies [8][9][10][11][12][13][14][15][16] , 5 [11,[13][14][15][16] were selected based on their relevance, but the phytochemistry component did not adhere to the selection criteria. A total of 10 in vitro studies only were included in this review [17][18][19][20][21][22][23][24][25][26] . Fig.…”

Prevention of allergic airway hyperresponsiveness and remodeling in mice by Astragaliradix Antiasthmatic decoction

“…In addition, Psoraleae fructus is commonly used in Chinese to alleviate asthma [22]. Other herbs [23]-[29], Codonopsis radix, Cuscutae semen , Schisandrae chinensis fructus . Citri reticulatae pericarpium , and Saposhnikoviae radix , have also been shown to have effective anti-inflammatory activities and modulated immune responses, which may also exert a preventive effect in allergic airway inflammation.…”