Pharmacokinetic Study of Nobiletin and Tangeretin in Rat Serum by High-Performance Liquid Chromatography-Electrospray Ionization-Mass Spectrometry

Nobiletin (NOB) and tangeretin (TAN), two of the main polymethoxylated flavones (PMFs) in citrus, influence a number of key biological pathways in mammalian cells. Although the impacts of NOB and TAN on glucose homeostasis and cholesterol regulation have been investigated in human clinical trials, much information is still lacking about the metabolism and oral bioavailability of these compounds in animals. In this study, NOB and TAN were administered to rats by gavage and intraperitoneal (ip) injection, and the blood serum concentrations of these compounds and their main metabolites were monitored by high-performance liquid chromatography-electrospray ionization-mass spectrometry (HPLC-ESI-MS). In addition to the administered compounds, two metabolites of TAN and eight metabolites of NOB were detected and measured over 24 h. With identical oral doses, nearly 10-fold higher absorption of NOB occurred compared to TAN. For both compounds, maximum levels of glucuronidated metabolites occurred in the blood serum at later time points (similar to 5-8 h) compared to the earlier T(max) a values for NOB and TAN. In most cases the glucuronides occurred at substantially higher concentrations than the aglycone metabolites. Low levels of NOB and TAN and their metabolites were detectable in rat blood serum even at 24 h after treatment.

GLICOALCALOIDES DOS FRUTOS DO SOLANUM FLACCIDUM VELL

From the fruits of Solanum flaccidum Vell, two glycoalkaloids (solamargine and solasonine) and one aglycone (solasodine) were isolated and identified.

Isolation of lignans glycosides from Alibertia sessilis (Vell.) K. Schum. (Rubiaceae) by preparative high-performance liquid chromatography

Enantiomeric aglycone lignans contained in a mixture were separated from a fraction of the extract of the stems of Alibertia sessilis (Vell.) K. Schum. (Rubiaceae) by preparative high-performance liquid chromatography. An efficient and fast separation can be achieved with methanol-water (30:70, v/v). Their structures were identified as (+)-lyoniresinol 3α-O-β-glucopyranoside and (-)-lyoniresinol 3α-O-β-glucopyranoside, being reported for the first time in Rubiaceae.

Mutagenicidade de duas espécies do gěnero Alchornea avaliadas através de ensaios com Salmonella microssomo e teste do micronúcleo

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Effects of liver S9 enzymes on somalargine and solasodine cytotoxicity and mass spectrometric fragmentation

The steroidal glycoalkaloid solamargine and its parent aglycone solasodine, isolated from Solanum palinacanthum, were studied in vitro for cytotoxicity and biotransformation by the hepatic S9 fraction as the metabolic activating system. The MTT uptake assay was used to determine viability after 24 h in RAW 264.7 mouse macrophage-like and SiHa cells exposed to various concentrations of the alkaloids in the presence and absence of the hepatic S9 microsomal fraction. The dose-response curves were established for solamargine and solasodine in the presence and absence of external metabolizing system. From these data, the cytotoxic index (CI50) was calculated with mean values of 7.2 and 13.6 μg/mL for Raw cells and 8.6 and 26.0 μg/mL for SiHa cells, respectively. Mass spectrometry was performed to compare the fragmentation patterns of the alkaloids to predict metabolism by the S9 fraction. The mass spectra demonstrated a distinct fragmentation patterns for solamargine and solasodine after the addition of the S9 fraction. In the present study, we demonstrate that the cytotoxic effect of solamargine and solasodine and their metabolites prepared in vitro by biotransformation with the S9 fraction are comparable. These findings suggest that the metabolic activation system S9 fraction may fail to suppress the cytotoxicity of these alkaloids. © 2013 Springer-Verlag Berlin Heidelberg.

cis-Jasmone e Tween 20 na indução de metabólitos secundários em soja e seus efeitos em insetos-praga

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Bioatividade da solamargina e solasodina para diferentes sistemas celulares após metabolização in vitro por fração microssomal hepática

Pós-graduação em Biociências e Biotecnologia Aplicadas à Farmácia - FCFAR

PURIFICATION AND CHARACTERIZATION OF SOY COTYLEDON -GLUCOSIDASE

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Phenolic compounds and antioxidant, antimicrobial and antimycobacterial activities of Serjania erecta Radlk. (Sapindaceae)

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Isoflavones supplementation of a probiotic soy product: effects on quality characteristics and isoflavones profile

The aim of the present study was to investigate the effect of isofl avones supplementation of a fermented soy product on its sensory acceptance, physicochemical properties and probiotic cell viable count. Additionally we also investigated the ability of the mixed starter cultures (Enterococcus faecium CRL 183 and Lactobacillus helveticus 416) to modify the isofl avones profi le of soy product during the fermentation process. Three products were analysed: soy product fermented with E. faecium CRL 183 and L. helveticus 416, isofl avonessupplemented soy product (fermented with E. faecium CRL 183 and L. helveticus 416; 50mg/100g, Isofl avin®, Galena, Brazil) and unfermented soy product. A panel of judges evaluated the acceptability of the samples on a nine point structured hedonic scale. The chemical composition namely fat, protein, ash and total carbohydrate contents, pH, enumeration of viable Lactobacillus spp. and Enterococcus spp. and quantifi cation of isofl avones using HPLC were investigated. All determinations were conducted after 7 days storage at 10°C. The sensorial acceptance was reduced in the isofl avones-supplemented soy product, but this effect was not signifi cant compared to the sample without isofl avones addition. Chemical composition did not differ (p<0.05) among the samples. Cell viable counts were reduced and total fermentation time was longer in the isofl avonessupplemented soy product, suggesting that the isofl avone addition could inhibit the starter cultures. However, all the products may be considered probiotic since they exhibited lactic acid bacterial populations varying from 2.3 x 109 up to 1.22 x 1010 CFU/mL. Fermentation of soymilk did not change the isofl avones profi le. In conclusion, it was possible to obtain a fermented soy product containing a high isofl avones concentration, adequate sensory and chemical characteristics and lactic acid bacterial viability suffi ciently high to characterize the product as a probiotic. The mixed starter culture was not able to convert the glycoside isofl avones into aglycone or produce equol during the fermented soy product processing.