Publications by authors named "Farong Lu"
Article Synopsis
- - Daidzein (DAN) is a poorly soluble isoflavone found in soybeans and supplements, which limits its effectiveness due to low bioavailability and first-pass metabolism.
- - A study developed and tested a series of amino acid prodrugs, with the most effective being daidzein-4'--CO--isoleucine (D-4'-I), which significantly improved water solubility and metabolic stability compared to DAN.
- - D-4'-I led to a 15.5-fold increase in oral bioavailability in rats, reduced gender differences in response, and provided dose-dependent protection against liver injury, showcasing the potential of prodrug strategies for enhancing the effectiveness of DAN.
Resveratrol (RES) suffers from poor water solubility and extensive metabolism, which lead to low bioavailability. A phospholipid complex (PC) containing RES and a UDP-glucuronosyltransferase (UGT) inhibitor was prepared to address these two limiting factors, thereby improving RES bioavailability. First, 11 natural active ingredients metabolized by similar enzyme subtypes to RES were screened in a glucuronidation assay in liver microsomes.
View Article and Find Full Text PDFTwo valine carbamate prodrugs of daidzein were designed to improve its bioavailability. To compare the pharmacokinetic behavior of these prodrugs with different protected phenolic hydroxyl groups of daidzein, a rapid and sensitive method for simultaneous quantification of daidzein, its valine carbamate prodrug, and daidzein-7-O-glucuronide in rat plasma was developed and validated in this study. The samples were processed using a fast one-step protein precipitation method with methanol added to 50 μL of plasma and were analyzed by ultra-high performance liquid chromatography with tandem mass spectrometry.
View Article and Find Full Text PDFA valine carbamate prodrug (7-P) was designed to enhance the low bioavailability of daidzein due to its low water solubility and membrane permeability. Here, we developed a high-throughput HPLC-MS/MS method to measure daidzein and its 7-O-glucuronide after oral administration of daidzein or 7-P. A HPLC-MS/MS method was validated and successfully applied to assess the pharmacokinetic behavior of daidzein and its 7-O-glucuronide after orally administrating daidzein or 7-P.
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