Bioavailability of Sulforaphane from two broccoli sprout beverages: results of a short-term, cross-over clinical trial in Qidong, China.
Bioavailability of Sulforaphane from two broccoli sprout beverages: results of a short-term, cross-over clinical trial in Qidong, China.
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DOI：
10.1158/1940-6207.capr-10-0296
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发表时间：
2011-03
期刊：
影响因子：
--
通讯作者：
Kensler TW
中科院分区：
文献类型：
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作者：
Egner PA;Chen JG;Wang JB;Wu Y;Sun Y;Lu JH;Zhu J;Zhang YH;Chen YS;Friesen MD;Jacobson LP;Muñoz A;Ng D;Qian GS;Zhu YR;Chen TY;Botting NP;Zhang Q;Fahey JW;Talalay P;Groopman JD;Kensler TW
临床化学预防试验设计中的几个挑战之一是干预剂的剂量、制剂和给药方案的选择。因此，进行了交叉临床试验以比较来自两种西兰花芽衍生饮料的莱菔硫烷的生物利用度和耐受性：一种富含葡萄糖萝卜素（GRR）和另一种富含莱菔硫烷（SFR）。萝卜硫素是通过肠道微生物菌群从GRR中含有的萝卜硫苷产生的，或者是通过用来自萝卜（Raphanus sativus）芽的黑芥子酶处理GRR以提供SFR而形成的。要求50名健康、合格的参与者避免食用十字花科蔬菜，并将其随机分为两个治疗组。研究设计如下：5天导入期、7天饮料给药、5天洗脱期和7天相反干预给药。同位素稀释质谱法用于测量在整个研究期间每天收集的尿样中的萝卜硫苷、萝卜硫素和萝卜硫素硫醇缀合物的水平。通过莱菔硫烷及其代谢物的尿排泄（给药后约12小时收集）测量的生物利用度，SFR（平均值= 70%）显著高于GRR（平均值= 5%）饮料。SFR饮料的排泄量个体间差异显著低于GRR饮料。与SFR推注给药相比，GRR允许实现稳态给药的消除速率明显较慢。未来研究中的最佳给药制剂应考虑将萝卜硫素和萝卜硫苷的混合物作为SFR和GRR混合物，以达到激活某些靶点的峰值浓度，并延长对与萝卜硫素保护作用有关的其他靶点的抑制。
One of several challenges in design of clinical chemoprevention trials is the selection of the dose, formulation and dose schedule of the intervention agent. Therefore, a cross-over clinical trial was undertaken to compare the bioavailability and tolerability of sulforaphane from two of broccoli sprout-derived beverages: one glucoraphanin-rich (GRR) and the other sulforaphane-rich (SFR). Sulforaphane was generated from glucoraphanin contained in GRR by gut microflora or formed by treatment of GRR with myrosinase from daikon (Raphanus sativus) sprouts to provide SFR. Fifty healthy, eligible participants were requested to refrain from crucifer consumption and randomized into two treatment arms. The study design was as follows: 5-day run-in period, 7-day administration of beverages, 5-day washout period, and 7-day administration of the opposite intervention. Isotope dilution mass spectrometry was used to measure levels of glucoraphanin, sulforaphane and sulforaphane thiol conjugates in urine samples collected daily throughout the study. Bioavailability, as measured by urinary excretion of sulforaphane and its metabolites (in approximately 12 hour collections after dosing), was substantially greater with the SFR (mean = 70%) than with GRR (mean = 5%) beverages. Interindividual variability in excretion was considerably lower with SFR than GRR beverage. Elimination rates were considerably slower with GRR allowing for achievement of steady state dosing as opposed to bolus dosing with SFR. Optimal dosing formulations in future studies should consider blends of sulforaphane and glucoraphanin as SFR and GRR mixtures to achieve peak concentrations for activation of some targets and prolonged inhibition of others implicated in the protective actions of sulforaphane.