Institute for Pharma Technology, School of Life Sciences, University of Applied Sciences Northwestern Switzerland, Muttenz, Switzerland.
Scientific Department, Steigerwald Arzneimittelwerk GmbH, Darmstadt, Germany.
J Pharm Pharmacol. 2019 Jan;71(1):58-69. doi: 10.1111/jphp.12717. Epub 2017 Mar 12.
The major aim of this study was to get a detailed understanding of the exposure and fate of hypericin in the Caco-2 cell system when combined with various flavonoids, mixtures of flavonoids or Hypericum perforatum extract matrix (STW3-VI).
The permeation characteristics of hypericin in the absence or presence of quercetin, quercitrin, isoquercitrin, hyperoside and rutin were tested. Hypericin (5 μm) was mixed with single flavonoids (20 μm) or with different flavonoid combinations (each flavonoid 4 or 10 μm, total flavonoid concentration: 20 μm). Further, the uptake of hypericin (5 μm) in the presence of H. perforatum extract matrix (7.25, 29 and 58 μg/ml) was studied.
Following application of hypericin to the apical side of the monolayer, only negligible amounts of the compound were found in the basolateral compartment. From all tested flavonoids, only quercitrin increased the basolateral amount of hypericin. Dual flavonoid combinations were not superior compared to the single combinations. The amount of hypericin in the basolateral compartment increased concentration-dependently in the presence of extract matrix (from 0 to 7.5%).
Comparing the effects of various flavonoid mixtures vs the extract matrix, it can be concluded that, besides flavonoids, the extract seems to contain further compounds (e.g. phenolic acids or proanthocyanidins) which substantially improve the permeation characteristics of hypericin.
本研究的主要目的是详细了解贯叶金丝桃素与各种类黄酮、类黄酮混合物或贯叶连翘提取物基质（STW3-VI）结合时在 Caco-2 细胞系统中的暴露和命运。
测试了在缺乏或存在槲皮素、槲皮苷、异槲皮苷、金丝桃苷和芦丁的情况下贯叶金丝桃素的渗透特性。将金丝桃素（5μm）与单一类黄酮（20μm）或不同类黄酮组合（每种类黄酮 4 或 10μm，总类黄酮浓度：20μm）混合。此外，还研究了在贯叶连翘提取物基质（7.25、29 和 58μg/ml）存在的情况下金丝桃素（5μm）的摄取情况。
将金丝桃素应用于单层的顶端侧后，仅在基底外侧隔室中发现了可忽略不计的化合物量。在所测试的类黄酮中，只有槲皮苷增加了金丝桃素的基底外侧量。与单一组合相比，双黄酮组合并没有优势。在提取物基质存在的情况下，金丝桃素在基底外侧隔室中的量与浓度呈依赖性增加（从 0 到 7.5%）。
将各种类黄酮混合物与提取物基质的效果进行比较，可以得出结论，除了类黄酮外，提取物似乎还含有其他化合物（例如酚酸或原花青素），这些化合物可显著改善金丝桃素的渗透特性。
