Red wine and components flavonoids inhibit UGT2B17 in vitro

Background The metabolism and excretion of the anabolic steroid testosterone occurs by glucuronidation to the conjugate testosterone glucuronide which is then excreted in urine. Alterations in UGT glucuronidation enzyme activity could alter the rate of testosterone excretion and thus its bioavailability. The aim of this study is to investigate if red wine, a common dietary substance, has an inhibitory effect on UGT2B17. Methods Testosterone glucuronidation was assayed using human UGT2B17 supersomes with quantification of unglucuronidated testosterone over time using HPLC with DAD detection. The selected red wine was analysed using HPLC and the inhibitory effects of the wine and phenolic components were tested independently in a screening assay. Further analyses were conducted for the strongest inhibitors at physiologically relevant concentrations. Control experiments were conducted to determine the effects of the ethanol on UGT2B17. Results Over the concentration range of 2 to 8% the red wine sample inhibited the glucuronidation of testosterone by up to 70% over 2 hours. The ethanol content had no significant effect. Three red wine phenolics, identified by HLPC analyses, also inhibited the enzyme by varying amounts in the order of quercetin (72%), caffeic acid (22%) and gallic acid (9%); using a ratio of phenolic:testosterone of 1:2.5. In contrast p-coumaric acid and chlorogenic acid had no effect on the UGT2B17. The most active phenolic was selected for a detailed study at physiologically relevant concentrations, and quercetin maintained inhibitory activity of 20% at 2 M despite a ten-fold excess of testosterone. Conclusion This study reports that in an in vitro supersome-based assay, the key steroid-metabolising enzyme UGT2B17 is inhibited by a number of phenolic dietary substances and therefore may reduce the rate of testosterone glucuronidation in vivo. These results highlight the potential interactions of a number of common dietary compounds on testosterone metabolism. Considering the variety of foodstuffs that contain flavonoids, it is feasible that diet can elevate levels of circulating testosterone through reduction in urinary excretion. These results warrant further investigation and extension to a human trial to delineate the healt

Fate of atrazine and simazine residues in polluted groundwaters: results of monitoring investigation of Poznan voivodeship wells in 1993-1998

In the period of 1993-1998 six wells known as being contaminated were monitored 3-6 times per year (a total of 143 samples) for the presence of atrazine, simazine and respective chloro-dealkyl metabolites. Samples were prepared for analysis by solid phase extraction (SPE) and determination was by HPLC/UV or GC/NPD techniques, GC/MSD and HPLC/DAD were employed as secondary (confirmatory) techniques. Residues of analysed compounds were present in more than 90% of samples with exception for DeDiA that was found in 81.6% of samples. The highest concentrations of atrazine, simazine, DeA, DiA, and DeDiA were 16.80; 18.60; 7.49; 2.98 and 3.43 μg/l respectively. New inputs of atrazine and simazine were observed in ground water of three wells occasionally, probably resulting from fresh herbicide treatments. In the other wells contamination was rather stagnant at lower levels (O.X mg/I).W okresie 1993-1998 monitorowano sześć skażonych studni 3-6 razy w roku (suma próbek 143) na obecność atrazyny i symazyny oraz ich chlorodealkilo-metabolitów. Próbki wody przygotowano do analiz stosując technikę adsorbcji/ekstrakcji na mikrokolumienkach (SPE). Końcowe oznaczenia wykonano metodami HPLC/UV lub GC/NPD do potwierdzania wyników stosując techniki (GC/MSD i HPLC/DAD). Pozostałości analizowanych związków występowały w ponad 90% próbek z wyjątkiem DeDiA znalezionym w 81,6% próbek. Najwyższe oznaczone stężenia atrazyny, symazyny, DeA, DiA, DeDiA wynosiły odpowiednio 16,80; 18,60; 7,49; 2,98 i 3,43 μg/l. W trzech studniach parokrotnie stwierdzono wzrost stężeń atrazyny i symazyny prawdopodobnie będący rezultatem aktualnych zastosowań herbicydów w praktyce rolniczej. W pozostałych studniach skażenia pozostałościami herbicydów raczej zmieniały się nieznacznie w zakresie niskich stężeń (0,X μg/l)

Pesticide residues in organic food and feed of plant origin

W latach 2004-2010 w ramach urzędowych badań kontrolnych oceniano 957 próbek, w których analizowano w zależności od roku pozostałości od 96 do 175 substancji aktywnych środków ochrony roślin i ich metabolitów. Próbki do badań pobierali próbobiorcy 7 jednostek certyfikujących w rolnictwie ekologicznym. Próbki badano w laboratoriach Instytutu ochrony Roślin - Państwowego Instytutu Badawczego (IOR-PIB) w Białymstoku, Poznaniu i Rzeszowie. Pozostałości niedozwolonych środków ochrony roślin stwierdzono w 61 próbkach, to jest w 6,4% badanych próbek. Wykryto pozostałości 11 insektycydów (alfa-cypermetryna, bifentryna, chloropiryfos, cypermetryna, DDT, diazynon, dimetoat, endosulfan, fenitrotion, lindan, pirymifos metylowy) i 15 fungicydów (azoksystrobina, chlorotalonil, cyprodynil, dichlofluanid, difenokonazol, dimetomorf, ditiokarbaminiany, fenheksamid, flusilazol, kaptan, pirymetanil, procymidon, tebukonazol, tetrakonazol, tolilofluanid). Wyniki przesyłano do jednostek certyfikujących w rolnictwie ekologicznym, które podejmowały odpowiednie decyzje. Wyniki próbek zawierających pozostałości środków ochrony roślin przesyłano również do Głównego Inspektoratu Inspekcji Jakości Handlowej Artykułów Rolno-Spożywczych.During 2004-2010 in the framework of the official testing, 957 samples were analyzed for residues, depending on the year, 96-175 pesticide active substances and their metabolites. Samples were collected by sampling officers of 7 certification bodies for organic farming. Samples were tested in the laboratories of the Institute of Plant Protection - National Research Institute (IPP-NRI) in Bialystok, Poznań and Rzeszów. Illegal residues of plant protection products were found in 61 samples, that is, 6.4% of samples tested. There were detected residues of 11 insecticides (alpha-cypermethrin, bifenthrin, chlorpyrifos, cypermethrin, DDT, diazinon, dimethoate, endosulfan, fenitrothion, lindane, methyl pirymifos) and 15 fungicides (azoxystrobin, chlorothalonil, cyprodinil, dichlofluanid difenoconazole, dimethomorph, dithiocarbamates, fenhexamid, flusilazole, captan, pyrimethanil, procymidone, tebuconazole, tetraconazole, tolylfluanid). Results were sent to the certification bodies for organic farming, which have taken the appropriate decisions. Results of samples containing pesticide residues were also forwarded to the Chief Inspectorate of Agricultural and Food Quality Inspection