Disposition and metabolism of the flavonoid chrysin in normal volunteers
Disposition and metabolism of the flavonoid chrysin in normal volunteers
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DOI：
10.1111/j.1365-2125.2001.01317.x
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发表时间：
2001-02-01
影响因子：
3.4
通讯作者：
Halushka, PV
中科院分区：
文献类型：
--
作者：
Walle, T;Otake, Y;Halushka, PV
目的描述健康志愿者饮食中黄酮类白杨素的口服情况。方法7名受试者口服400 mg白杨素。结果血浆白杨素峰值浓度为3~16 ng m l(-1)，AUC为5~193 ng m l(-1)h，硫酸白杨素浓度高30倍(AUC 450~4220 ng m l(-1)h)。尿中白杨素和白杨素葡萄糖醛酸苷含量分别为0.2~3.1 mg和2~26 mg。大部分剂量以白杨素的形式出现在粪便中。在大鼠的平行实验中，白杨素结合物的胆汁浓度很高。结论这些发现，加上以前使用Caco-2细胞的数据，表明白杨素的口服生物利用度较低，主要是由于广泛的代谢和代谢产物回流到肠道进行水解和粪便消除。
Aims To describe the oral disposition of the dietary flavonoid chrysin in healthy volunteers.Methods Oral 400 mg doses of chrysin were administered to seven subjects. Chrysin and metabolites were assayed in plasma, urine and faeces by h.p.l.c.Results Peak plasma chrysin concentrations were only 3-16 ng ml(-1) with AUCs of 5-193 ng ml(-1) h. Plasma chrysin sulphate concentrations were 30-fold higher (AUC 450-4220 ng ml(-1) h). In urine, chrysin and chrysin glucuronide accounted for 0.2-3.1 mg and 2-26 mg, respectively. Most of the dose appeared in faeces as chrysin. Parallel experiments in rats showed high bile concentrations of chrysin conjugates.Conclusions These findings, together with previous data using Caco-2 cells, suggest that chrysin has low oral bioavailability, mainly due to extensive metabolism and efflux of metabolites back into the intestine for hydrolysis and faecal elimination.