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首页> 外文期刊>Toxicological sciences: An official journal of the Society of Toxicology >Oral bioavailability and pharmacokinetics of elimination of 9-hydroxybenzo(a)pyrene and its glucoside and sulfate conjugates after administration to male and female American lobsters, Homarus americanus.
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Oral bioavailability and pharmacokinetics of elimination of 9-hydroxybenzo(a)pyrene and its glucoside and sulfate conjugates after administration to male and female American lobsters, Homarus americanus.

机译：雄性和雌性美国龙虾美国大螯虾服用后消除9-羟基苯并（a）py及其糖苷和硫酸盐结合物的口服生物利用度和药代动力学。

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摘要

The pharmacokinetics of [(3)H]-9-hydroxybenzo[a]pyrene (9-OH-BaP), a highly lipophilic primary metabolite of benzo(a)pyrene, were examined after intrapericardial (iv) or oral doses of 50 or 200 microg/kg to intermolt American lobsters, Homarus americanus. Combining data for all lobsters, the average terminal elimination half-life of parent 9-OH-BaP was 97.3 h after iv and 56.5 h after oral administration, considerably less than found previously for benzo(a)pyrene (720 h). The oral bioavailability of parent 9-OH-BaP, calculated from the area under the hemolymph concentration curve, was 15.9%. The low bioavailability and variable elimination rates were attributed to extensive first-pass conjugation and sequestration in the hepatopancreas. BaP-9-sulfate was the major metabolite. Hemolymph concentrations of BaP-9-sulfate increased up to one day after the dose, and then decreased, with a terminal elimination half-life of 45 h. BaP 9-beta-D-glucoside was a minor metabolite in most hemolymph and tissue samples; an exception was hemolymph from the iv high-dose group. Concentrations of 9-OH-BaP and metabolites in the edible muscle tissue were similar to those in hemolymph, and 9-OH-BaP residues at 10 to 16 days after the dose were 3 to 12 ng/g muscle. Sulfotransferase and UDP-glucosyltransferase (UGT) activities with 9-OH-BaP were found in the antennal gland, intestinal mucosa, and hepatopancreas (UGT only). Sulfatase activity with BaP-9-sulfate, found in both the hepatopancreas and the antennal gland, was thought to contribute to metabolite cycling. These studies showed that 9-OH-BaP was readily conjugated to sulfate and glucose in the lobster, and that despite their high lipophilicity, 9-OH-BaP and conjugates were excreted from the lobster hemolymph and tissues much more rapidly than benzo[a]pyrene.
机译：心包内（iv）或口服剂量为50或90 mg后，检查[（3）H] -9-羟基苯并[a] re（9-OH-BaP）的药代动力学，苯并（a）py的高度亲脂性主要代谢产物。 200微克/千克，可融合美洲龙虾。结合所有龙虾的数据，母体9-OH-BaP的平均终末消除半衰期为静脉注射后为97.3小时，口服后为56.5小时，大大低于先前的苯并（a）re（720小时）。由血淋巴浓度曲线下的面积计算，母体9-OH-BaP的口服生物利用度为15.9％。低的生物利用度和可变的消除率归因于肝胰腺中广泛的首过结合和螯合。 BaP-9-硫酸盐是主要的代谢产物。剂量后直至一天，BaP-9-硫酸盐的血淋巴浓度增加，然后下降，最终消除半衰期为45小时。在大多数血淋巴和组织样品中，BaP9-β-D-葡萄糖苷是次要的代谢产物。静脉注射大剂量组的血淋巴除外。食用肌肉组织中9-OH-BaP和代谢物的浓度与血淋巴中的相似，剂量后10至16天的9-OH-BaP残留量为3至12 ng / g肌肉。在触角腺，肠粘膜和肝胰腺（仅UGT）中发现具有9-OH-BaP的磺基转移酶和UDP-葡萄糖基转移酶（UGT）活性。在肝胰腺和触角腺中发现具有BaP-9-硫酸盐的硫酸酯酶活性被认为有助于代谢循环。这些研究表明9-OH-BaP易于与龙虾中的硫酸盐和葡萄糖结合，尽管它们具有高亲脂性，但9-OH-BaP和结合物从龙虾的血淋巴和组织中排泄的速度比苯并[a]要快得多。 .。

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