Effects of four polyphenols loading on the attributes of lipid bilayers
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Chrysanthemum morifolium extract (CME) has the protective effect on cardiovascular diseases. Luteolin and apigenin are two major bioactive components in vivo when CME is orally administrated to experimental animal. The present paper shows the study of the absorption and excretion of luteolin and apigenin in rats after a single oral dose of CME (200 mg/kg). The levels of luteolin and apigenin in plasma, urine, feces, and bile were measured by HPLC after deconjugation with hydrochloric acid or β-glucuronidase/sulfatase. The results showed that the plasma concentrations of luteolin and apigenin reached the highest peak level at 1.1 and 3.9 h after dosing, respectively. The area under the concentration−time curves (AUC) for luteolin and apigenin were 23.03 and 237.6 μg h mL-1, respectively. The total recovery of the dose was 37.9% (6.6% in urine; 31.3% in feces) for luteolin and 45.2% (16.6% in urine; 28.6% in feces) for apigenin. The cumulative luteolin and apigenin excreted in the bile was 2.05% and 6.34% of the dose, respectively. All of the results suggest apigenin may be absorbed more efficiently than luteolin in CME in rats, and both luteolin and apigenin have a slow elimination phase, with a quick absorption, so a possible accumulation of the two flavonoids in the body can be hypothesized. Keywords: Chrysanthemum morifolium extract (CME); luteolin; apigenin; absorption; excretion
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Flavonoids are bioactive phenolic compounds widely present in plant food and used in various nutraceutical, pharmaceutical, and cosmetic products. However, recent studies showed rising concerns of endocrine disruptions and developmental toxicities for many flavonoids. To understand the impacts of flavonoid structure on toxicity, we used a new multitiered platform to investigate the toxicities of four common flavonoids, luteolin, apigenin, quercetin, and genistein, from flavone, flavonol, and isoflavone. Weak estrogenic activity was detected for four flavonoids (genistein, apigenin, quercetin, and luteolin) at 10-12 to 10-7 M by the MCF-7 cell proliferation assay, which agreed with the molecular docking results. Consistent with the simulation results of Toxicity Estimation Software Tool, genistein and luteolin showed high developmental toxicity in the chicken embryonic assay (45-477 μg/kg) with mortality rate up to 50%. Luteolin, quercetin, and apigenin showed signs of mutagenicity at 5 × 10-3 pmol/plate. The findings showed nonmonotonic dose responses for the chemicals.
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The aims of the present study were to study the interspecies difference in the pharmacokinetics of luteolin and apigenin occurring in Chrysanthemum morifolium extract (CME) among rats, beagle dogs, mini-pigs, and humans, and compared the human pharmacokinetic parameters with the data predicted from the above three animals. The plasma concentrations of luteolin and apigenin were determined with a RP-HPLC method. An interspecies difference of pharmacokinetics was found, especially between rats and other species, the plasma concentration of luteolin was much lower than that of apigenin in rats, although the content of luteolin in CME was higherthan that of apigenin, whereas the plasma concentration of luteolin was much higher than that of apigenin in dogs, mini-pigs and humans. Animal scale-up of some pharmacokinetic parameters of luteolin and apigenin were also performed after rats, beagle dogs, mini-pigs and humans were orally given CME at dosages of 400 mg/kg, 102 mg/kg, 90 mg/kg, and 20 mg/kg, respectively. Linear relationships were obtained between log mean retention time (MRT) and log species body weight (W) (kg), and log elimination half-life (t1/2) (h) and logW. The corresponding allometric equations were MRT=9.382W(0.1711) (R2 = 0.9999) and t1/2 = 4.811W(0.1093) (R2 = 0.9013) for luteolin, MRT = 12.53W(0.0356) (R2 = 0.9980) and t1/2 = 7.940W(0.0294) (R2 = 0.9258) for apigenin, respectively. The predicted human pharmacokinetic parameters (MRT and t1/2) by an allometric approach were 18.6 h and 7.46 h for luteolin, 14.3 h and 8.95 h for apigenin, respectively, which were close to the values obtained from humans (20 mg CME/kg) in the present study. The study has demonstrated the possibility to extrapolate the pharmacokinetic behavior of flavonoids from animals to humans.
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Chrysanthemum morifolium
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Chrysanthemum morifolium
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Tricin
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Flavanone
Eriodictyol
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The molecular properties of apigenin, luteolin and nevadensin which are three naturally flavonoid compounds have been studied theoretically by DFT method at 6-311++G(d,p) level. Both FMO analysis, mechanism, and kinetics studied suggested that compound Luteolin (compound 3) was a promising antioxidant agent. The results indicated that HAT is thermodynamically preferred in the gas phase, and SPLET is the thermodynamically favorable pathway in methanol and water
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Objective: To establish a RP-HPLC method for the determination of luteolin and apigenin in rat bile, and study the biliary excretion of luteolin and apigenin after rat orally administrated Chrysanthemum morifolium extract (CME). Methods:Bile samples were enzymatic hydrolyzed before analysis by RP-HPLC. SB-C_(18) HPLC column (250 mm×4.6mm, 5μm)was used. The mobile phase was methanol-0.2% phosphoric acid (52:48,v/v) with the flow rate of 1.0mL·min~(-1); the UV detector was set at 350 nm. Results:A good separation was obtained. The standard curves for luteolin and apigenin in bile were linear over the range of 0.1745-6.986μg·mL~(-1) and 0.3693-11.08μg·mL~(-1), respectively. The absolute recovery for luteolin and apigenin was 84.6% to 106.2% and assay recovery was 80.1% to 106.9%. The intra -and inter -day precisions (RSD) for luteolin and apigenin were all less than 14%. The relative biliary excretion rate of intake dose Of luteolin and apigenin during 36 hours after oral administration were 2.05% and 6.34%, respectively. Conclusion:The method developed is accurate, sensitive for the determination of luteolin and apigenin in bile. Enterohepatic circulation of luteolin and apigenin associated with double peaks in the blood concentration-time curves can be proved by the biliary excretion.
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The hepatic clearance and drug-drug interactions of luteolin and apigenin were studied by using primary cultured rat hepatocytes. Luteolin and apigenin experienced extensive first-pass metabolism. The elimination percent of luteolin and apigenin was found to be 91.9% and 86.7% after 120 min of incubation. The predicted % liver blood flow was 82.3% and 85.4% for luteolin and apigenin, respectively. Total glucuronidated/sulfated conjugates of luteolin/apigenin were determined by an enzyme hydrolysis method. Compared with the elimination of pure luteolin and apigenin, the elimination of luteolin and apigenin was much lower in hydrolyzed Flos Chrysanthemi extract (FCE) containing comparable amounts of luteolin and apigenin. The effect of a series of flavonoids, including flavonols, flavones, isoflavone, flavanone, flavanonols and catechins, on the elimination of luteolin and apigenin was studied. At least four key determinants in the chemical structures of flavonoids are necessary for exerting the inhibitory effects on the conjugation: 1) catechol structure (3',4'-dihydroxylation) in the B-ring; 2) B-ring is attached to the C-2 position on the C-ring; 3) the C2-3 double bond in conjunction with the C4 carbonyl group on the C-ring; 4) no glycoside present. Investigation of clearance and interaction among flavonoids could help us better understand their bioavailability and offer insight into the approaches to be taken to minimize competitive effects, and to design appropriate bioavailability studies in humans.
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The extraction of flavonoids is of increasing interest because of their various pharmacological effects. This study is the first attempt for the ultrasonic-assisted enzymatic hydrolysis (USAEH) applied in the extraction of 2 bioactive flavonoid compounds in celery--luteolin and apigenin. The quantitative yields of luteolin and apigenin were determined by high-performance liquid chromatography (HPLC). To achieve high yields of extracted compounds, the procedure was optimized with regard to the relative parameters involved. The optimal conditions for enzymatic hydrolysis using pectinase treatment were a reaction time of 30 min and a concentration of 0.4 mg/mL at pH 3 for luteolin and pH 5.5 for apigenin. The optimal ultrasonic parameters were an exposure period of 30 min at a temperature of 25 °C using a power source of 80 W. Under these optimal conditions, the yields of luteolin and apigenin were increased to 42.5 and 25.3 mg/g, respectively, which represented a 26.1-fold and a 32.2-fold increase in the yields of these 2 compounds, respectively, compared with the control model of aqueous extraction without enzyme or ultrasonic treatment.
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