Permeability of rosmarinic acid in Prunella vulgaris and ursolic acid in Salvia officinalis extracts across Caco-2 cell monolayers.
Permeability of rosmarinic acid in Prunella vulgaris and ursolic acid in Salvia officinalis extracts across Caco-2 cell monolayers.
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DOI：
10.1016/j.jep.2011.07.037
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发表时间：
2011-10-11
影响因子：
5.4
通讯作者：
Hendrich, Suzanne
中科院分区：
文献类型：
--
作者：
Qiang, Zhiyi;Ye, Zhong;Hauck, Cathy;Murphy, Patricia A.;McCoy, Joe-Ann;Widrlechner, Mark P.;Reddy, Manju B.;Hendrich, Suzanne
迷迭香酸（RA）是一种在Prunella vulgaris（自愈）中发现的高浓度咖啡酸相关化合物，熊果酸（UA）是一种在鼠尾草（鼠尾草）中浓缩的五环三萜酸，传统上用于治疗口腔炎症，也可能对胃肠道健康有益。目的：研究RA和UA作为纯化合物以及在寻常草和officinalis乙醇提取物中对人肠上皮Caco-2细胞单层的通透性。采用高效液相色谱（HPLC）检测Caco-2细胞，比较RA和UA作为纯化合物和草药提取物的渗透性和II期生物转化。经β-葡萄糖醛酸酶/硫酸酯酶处理后，RA和RA的表观通透系数（Papp）为0.2±0.05 × 10−6 cm/s，显著提高至0.9±0.2 × 10−6 cm/s。β-葡萄糖醛酸酶/硫酸盐酶处理前后，山茱萸提取物中UA和UA的Papp分别为2.7±0.3 × 10−6 cm/s和2.3±0.5 × 10−6 cm/s。两种化合物的渗透性均不受草药提取物基质的影响。草药提取物中的RA和UA与使用纯化合物的摄取相似，这可能简化了化合物功效的预测，但明显缺乏肠道葡萄糖醛酸化/磺化UA可能进一步提高了该化合物与RA的生物利用度。
Rosmarinic acid (RA), a caffeic acid-related compound found in high concentrations in Prunella vulgaris (self-heal), and ursolic acid (UA), a pentacyclic triterpene acid concentrated in Salvia officinalis (sage), have been traditionally used to treat inflammation in the mouth, and may also be beneficial for gastrointestinal health in general. To investigate the permeabilities of RA and UA as pure compounds and in P. vulgaris and S. officinalis ethanol extracts across human intestinal epithelial Caco-2 cell monolayers. The permeabilities and Phase II biotransformation of RA and UA as pure compounds and in herbal extracts were compared using Caco-2 cells with HPLC detection. The apparent permeability coefficient (Papp) for RA and RA in P. vulgaris extracts was 0.2 ± 0.05 × 10−6 cm/s, significantly increased to 0.9 ± 0.2 × 10−6 cm/s after β-glucuronidase/sulfatase treatment. Papp for UA and UA in S. officinalis extract was 2.7 ± 0.3 × 10−6 cm/s and 2.3 ± 0.5 × 10−6 cm/s before and after β-glucuronidase/sulfatase treatment, respectively. Neither compound was affected in permeability by the herbal extract matrix. RA and UA in herbal extracts had similar uptake as that found using the pure compounds, which may simplify the prediction of compound efficacy, but the apparent lack of intestinal glucuronidation/sulfation of UA is likely to further enhance the bioavailability of that compound compared with RA.
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影响因子：
7.1
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