Graduate Program in Integrative Medicine, Chulabhorn International College of Medicine, Thammasart University (Rangsit Campus), Pathum Thani 12120, Thailand.
Division of Integrative Medicine, Chulabhorn International College of Medicine, Thammasart University (Rangsit Campus), Pathum Thani 12120, Thailand.
Molecules. 2022 Jun 17;27(12):3884. doi: 10.3390/molecules27123884.
(TL) has been traditionally used as an antidote and an antipyretic drug by folk healers for centuries in Thailand. Rosmarinic acid (RA) is major compound in TL extract and has attracted great interest due to its potential broad pharmacological effects. Herein, the permeability of RA was investigated in TL extract and as a pure compound in a Caco-2 cell model by using high-performance liquid chromatography with a photodiode array detector (HPLC-PDA). The results reveal that the apparent permeability coefficient () values of RA in TL extracts and pure RA significantly increased after deconjugation by β-glucuronidase/sulfatase enzymes. Our findings exhibit possible saturable biotransformation of RA and/or membrane transport while penetrated through Caco-2 cells. The cumulative amounts of RA as pure compounds and in TL extracts increased with the exposure time, and the efflux ratio (ER) was 0.27-1.14. RA in the TL extract has a similar absorption in the conjugated form and in the pure compound. The intestinal absorption of them is through passive diffusion. Therefore, our findings conclude that the intestinal transport of RA in TL extracts was mainly penetrated as conjugated forms with glucuronic acid and/or sulfate across Caco-2 cells and transported via passive diffusion.
（TL）在泰国，几个世纪以来一直被民间医生用作解毒剂和退烧药。迷迭香酸（RA）是 TL 提取物中的主要化合物，由于其潜在的广泛药理学作用，引起了极大的关注。在此，通过高效液相色谱-光电二极管阵列检测器（HPLC-PDA），在 Caco-2 细胞模型中，对 TL 提取物中的 RA 及其纯化合物的渗透性进行了研究。结果表明，TL 提取物中的 RA 和纯 RA 的表观渗透系数（Papp）值在经β-葡萄糖醛酸酶/硫酸酯酶去共轭化后显著增加。我们的研究结果表明，RA 可能存在可饱和的生物转化和/或透过 Caco-2 细胞的膜转运。RA 作为纯化合物和 TL 提取物的累积量随暴露时间的增加而增加，外排比（ER）为 0.27-1.14。TL 提取物中的 RA 以结合形式和纯化合物形式具有相似的吸收。它们的肠吸收是通过被动扩散。因此，我们的研究结果表明，TL 提取物中的 RA 肠内转运主要以与葡萄糖醛酸和/或硫酸盐结合的形式穿透 Caco-2 细胞，并通过被动扩散进行运输。
