benzofurans and daidzein

The incubation system of CYP2E1 and CYP3A4 enzymes in rat liver microsomes was established to investigate the effects of psoralidin, isobavachalcone, neobavaisoflavone and daidzein from Fructus Psoraleae in vitro. The relevant metabolites were measured by the method of high performance liquid chromatography (HPLC), after probe substrates of 4-nitrophenol, testosterone and the drugs at different concentrations were added to the incubation systems. In addition, real-time RT-PCR was performed to determine the effect of psoralidin, neobavaisoflavone and daidzein on the mRNA expression of CYP3A4 in rat liver. The results suggested that psoralidin, isobavachalcone and neobavaisoflavone were Medium-intensity inhibitors of CYP2E1 with K

Topics: Animals; Benzofurans; Chalcones; Coumarins; Cytochrome P-450 CYP2E1; Cytochrome P-450 CYP2E1 Inhibitors; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Isoflavones; Microsomes, Liver; Rats, Sprague-Dawley

A simple, precise and reliable LC-MS/MS method was developed and validated for simultaneous quantification of vitexin, notoginsenoside R1, hydroxysafflor yellow A, ginsenoside Rd, puerarin, daidzein and senkyunolide I as components of Naodesheng (NDS) in rat serum. The Linearity ranges in rat serum were 0.045-4.5 μg/mL for vitexin, 0.0476-4.76 μg/mL for notoginsenoside R1, 0.0422-4.22 μg/mL for hydroxysafflor yellow A, 0.0426-4.26 μg/mL for ginsenoside Rd, 0.0436-4.36 μg/mL for puerarin, 0.026-2.6 μg/mL for daidzein, and 0.05-5 μg/mL for senkyunolide I, with the correlation coefficients greater than 0.99. The established method was validated in terms of intra- and inter-day precision and accuracy, recovery, matrix effect and stability. Furthermore, the method was successfully applied for pharmacokinetic study of these seven components in rat serum after oral administration of NDS.

Topics: Administration, Oral; Animals; Benzofurans; Calibration; Chalcone; Chromatography, Liquid; Drugs, Chinese Herbal; Ginsenosides; Isoflavones; Limit of Detection; Linear Models; Quinones; Rats; Rats, Wistar; Reproducibility of Results; Tandem Mass Spectrometry; Time Factors

Propolis has been used as a medicinal agent to treat infections and promote wound healing for centuries. The aim of the present study was to test the antimicrobial, antioxidant, and cytotoxic activities of a new type of Brazilian propolis, popularly called red propolis, as well as to analyze its chemical composition. The antimicrobial activity against Staphylococcus aureus ATCC 25923 and Staphylococcus mutans UA159 was evaluated and the chloroform fraction (Chlo-fr) was the most active with lower MIC ranging from 25 to 50 microg/ml. The hexane fraction (H-fr), having the highest concentration of total flavonoids, showed the best sequestrating activity for the free radical DPPH. The ethanolic extract of propolis (EEP) showed cytotoxic activity for the HeLa tumor cells with an IC(50) of 7.45 microg/ml. When the EEP was analyzed by GC-MS, seven new compounds were found, among which four were isoflavones. Our results showed that the red propolis has biologically active compounds that had never been reported in other types of Brazilian propolis.

Topics: Abietanes; Animals; Anti-Infective Agents; Antioxidants; Benzofurans; Benzopyrans; Brazil; Cell Survival; Chloroform; Chromatography, High Pressure Liquid; Cresols; Equol; Ethanol; Gas Chromatography-Mass Spectrometry; HeLa Cells; Hexanes; Humans; Isoflavones; Medicine, Traditional; Microbial Sensitivity Tests; Propolis; Pterocarpans; Quercetin; Staphylococcus aureus; Streptococcus mutans

A new 2-arylbenzofuran, puerariafuran (1), as well as three known compounds, coumestrol (2), daidzein (3), and genistein (4), were isolated from a MeOH extract of the roots of Pueraria lobata as active constituents, using an in vitro bioassay based on the inhibition of advanced glycation end products (AGEs) to monitor chromatographic fractionation. The structure of 1 was determined by spectroscopic data interpretation, particularly by extensive 1D and 2D NMR studies. All the isolates (1-4) were evaluated for the inhibitory activity on AGEs formation in vitro.

Topics: Benzofurans; Coumestrol; Genistein; Glycation End Products, Advanced; Glycosylation; In Vitro Techniques; Isoflavones; Magnetic Resonance Spectroscopy; Molecular Structure; Plant Roots; Pueraria; Reference Standards; Stereoisomerism

The spectroscopic parameters used to assign the structure to isoaurostatin (4',6-dihydroxyisoaurone), a metabolite isolated from Thermomonospora alba, have been reinterpreted. It is suggested that isoaurostatin is identical to the isoflavone daidzein.

Topics: Benzofurans; Isoflavones; Molecular Structure