In vitro and in situ evaluation of herb–drug interactions during intestinal metabolism and absorption of Baicalein

The Molecular Basis for the Pharmacokinetics and Pharmacodynamics of Curcumin and Its Metabolites in Relation to Cancer

“…The last notable type of processes that contributes to the low systemic bioavailability of curcumin and/or the generation of curcumin metabolites entails the association of curcumin with intestinal nondetoxification proteins. In some instances the binding of curcumin to a protein relays an inhibitory effect, as has been shown for several ATP-binding cassette (ABC) transporters (Wortelboer et al, 2003(Wortelboer et al, , 2005Shukla et al, 2009) and CYP isozymes (Volak et al, 2008), whereas in other instances the binding can be both antagonistic and biotransformative, as is the case for, e.g., SULTs (Eaton et al, 1996;Ireson et al, 2002;Volak et al, 2008;Fong et al, 2012), UGTs (Volak et al, 2008;Berginc et al, 2012;Dempe et al, 2012;Fong et al, 2012), and GSTs (Awasthi et al, 2000). With respect to nondetoxifying enzymes, the combined antagonistic and catalytic effects have been demonstrated for curcumin-COX-2 (Hong et al, 2004;Selvam et al, 2005;Griesser et al, 2011) and curcumin-lipoxygenase complexes (Skrzypczak-Jankun et al, 2000;Toth et al, 2000;Hong et al, 2004;Prasad et al, 2004), which result in the formation of 6-hydroxy-1-(4-hydroxy-3-methoxyphenoxy)-3-(4-hydroxy-3-methoxyphenyl)-1,3,3a,6a-tetrahydro-4H-cyclopenta[c]furan-4-one (Fig.…”

Species difference in the inhibitory potentials of non-steroidal anti-inflammatory drugs on the hepatic sulfation and glucuronidation of bioactive flavonoids: differential observations among common inhibition parameters

“…Pooled male RLCs and pooled HLCs obtained commercially were utilized for the evaluation of inhibition of B/W/OA sulfation by NSAIDs; whereas pooled male RLMs and pooled HLMs were employed to study the effects of NSAIDs on the inhibition of B/W/OA glucuronidation. The in vitro metabolism study was conducted as described in our previous studies (Fong et al, 2012;Zhang et al, 2007b). Final concentrations of 5 mM of B/W/OA were pre-incubated with RLCs, HLCs, RLMs or HLMs at 37 C for 10 min in the presence/absence of NSAIDs at their corresponding highest therapeutic concentrations (Table 1).…”

“…The concentration range of NSAIDs (inhibitors) and B/W/OA (substrates) employed for K i determinations were listed in Table 2. (OAS) in collected samples, a modified LC/MS/MS was developed (Fong et al, 2012). Mobile phases consist of solvent A (acetonitrile) and solvent C (0.04% formic acid).…”

Co-delivery of baicalein and doxorubicin by hyaluronic acid decorated nanostructured lipid carriers for breast cancer therapy

“…BCL has broad anti-tumor activity against breast, cervical and gastric cancers (Wang et al, 2014;Peng et al, 2015;Yan et al, 2015). The shortcomings of BCL which lead to poor clinical effect in vivo compared with its powerful efficacy in vitro, including extensive first-pass metabolism, low bioavailability, short half-life (10 min), poor water solubility and oxidized easily (Fong et al, 2012;Seo et al, 2014;Liu et al, 2015). DOX is an anthracycline antibiotic.…”